Pharmacology

Histamines And Antihistamines Important Notes

1. Antihistamines

• Antihistamines Uses
• • Common cold
  • Anti-allergic
  • Insect bite
  • Idiopathic pruritis
  • Motion sickness
  • Vertigo

Histamines And Antihistamines Short Essays

Question 1. Mention four newer antihistamines with their advantages.
Answer:

• Newer Antihistamines are:
  • Fexofenadine
  • Loratadine
  • Cetrizine
  • Azelastine
  • Mizolastine
  • Terfenadine

Newer Antihistamines Advantages:

• Donot impair psychomotor performance
• Produce no subjective effects
• No sedation as they poorly cross the blood-brain barrier
• No anticholinergic side effects

Question 2. Mention four therapeutic uses of HI blockers.
Answer:

Uses of H1 Blockers:

1. Allergic reactions

• • Block the effects of released histamine
  • Control Immediate types of allergies like Itching, urticaria, angioedema
  • Cetrizine has an adjuvant role In seasonal asthma

2. Prurltldes

• • Older H1 blockers are used In Idiopathic pruritus

3. Common cold

• • Provide symptomatic relief by anticholinergic and sedative actions

4. Motion sickness

• • Promethazine and diphenhydramine are used prophylactically in motion sickness
  • It should be taken one hour before the journey

5. Vertigo

• • Inhibits vestibular sensory nuclei in the inner ear

6. Preanasethetic medication

• • Promethazine is used for it
• It includes the following groups

7. Cough

• • Provide symptomatic relief

8. Parklsonism

• • Provide symptomatic relief

9. Acute muscle dystonia

• • Due to Its central anticholinergic action

10. As sedative, hypnotic, and anxiolytic

Question 3. Autocoids
Answer:

• Autocoids are substances formed in various tissues, have complex physiological and pathological actions, and act locally at the site of synthesis
• They are called local hormones
• They serve as transmitters or moderators in the nervous system
• They have brief action and are destroyed locally

Read And Learn More: Pharmacology Question and Answers

Question 4. Antihistamines
Answer:

• Antihistamines are the drugs that competitively antagonize the action of histamine at H1 receptors

Antihistamines Classification

Antihistamines Uses:

• Allergic disorders
• Priorities
• Common cold
• Cough
• Motion sickness
• Preanasethetic medication
• Vertigo
• Parkinsonism
• Acute muscle dystonia
• As sedative, hypnotic, anxiolytic
• To control mild blood transfusion and saline infusion reactions

Question 5. Enumerate two nonsedative Antihistamines and mention four uses of them.
Answer:

Non Sedative Antihistamines:

• Fexofenadine
• Loratadine
• Cetrizine
• Azelastine
• Mizolastine
• Terfenadine

Non Sedative Antihistamines Uses:

• Allergic rhinitis, conjunctivitis, hay fever
• Control sneezing and runny nose, red watering eyes
• Urticaria, dermographism, atopic eczema
• Acute allergic reactions to drugs and food

Histamines And Antihistamines Short Question And Answers

Question 1. Cyproheptadine
Answer:

Cyproheptadine is a serotonin antagonist

Cyproheptadine Actions:

• Blocks 5-HT₂
• Blocks H1 receptors
• Blocks cholinergic receptors
• Increases appetite

Cyproheptadine Uses:

• Promote weight gain in children and poor eaters
• To control intestinal manifestations of carcinoid tumors

Question 2. Non sedative Antihistamines
Answer:

Non Sedative Antihistamines:

• Fexofenadine
• Loratadine
• Cetrizine
• Azelastine
• Mizolastine
• Terfenadine

Non Sedative Antihistamines Uses:

• Allergic rhinitis, conjunctivitis, hay fever
• Control sneezing and runny nose, red watering eyes
• Urticaria, dermographism, atopic eczema
• Acute allergic reactions to drugs and food

Non-Sedative Antihistamines Advantages:

• Donot impair psychomotor performance
• Produce no subjective effects
• No sedation as they poorly cross the blood-brain barrier
• No anticholinergic side effects

Question 3. Cetrizine
Answer:

• Cetrizine is non sedative Antihistamines
• It can metabolite of hydroxyzine with a marked affinity for peripheral H1 receptors
• It is well absorbed orally
• It attains high and long-lasting concentration in the skin

Cetrizine Actions:

• Inhibits the release of histamine and cytotoxic mediators from platelets
• Inhibits Eosinophil chemotaxis during the secondary phase of the allergic response

Cetrizine Uses:

• Upper respiratory allergies, pollinosis, Urticaria, atopic dermatitis
• Adjuvant to seasonal asthma

Question 4. Ergometrine
Answer:

• Ergometrine is an amine ergot alkaloid
• It is a very weak Agonist
• It has no antagonist action on alpha-adrenergic receptors
• The emetic potential is low
• They are rapidly and completely absorbed
• The plasma half-life is 1-2 hours
• Onset of action

Ergometrine Uses:

• To control and prevent postpartum hemorrhage
• To prevent uterine atony
• To ensure normal involution

Question 5. Promethazine
Answer:

• Promethazine is a highly sedative H1 antagonist

Promethazine Uses:

• Allergic disorders
• Pruritis
• Common cold
• Preanasethetic medication
• Parkinsonism

Question 6. Prostaglandins
Answer:

• Prostaglandins are biologically active derivatives of 200-carbon atom polyunsaturated fatty acids
• They are major lipid-derived autocoids

Prostaglandins Actions:

Question 7. Uses of ergot alkaloids
Answer:

Blood Important Notes

1. Heparin

• It is a powerful anticoagulant
• Effective both in vivo and vitro
• Present in all tissues containing mast cells
• In high doses, inhibits platelet aggregation and prolongs bleeding time
• Activates plasma antithrombin III
• This inactivates dotting factors of common and intrinsic pathways
• It does not cross the blood-brain barrier or placenta
• Thus it is safer during pregnancy

2. Styptics:

• They are local hemostatic agents
• Particularly effective on oozing surfaces
• Examples: thrombin, fibrin, gelatin foam, astringents like tannic add, vasoconstrictors like adrenaline

3. Drugs and anticoagulant action

4. Contraindications of vasoconstrictors

• Hypertension
• Hyperthyroidism
• Angina
• Patients receiving beta-blockers
• During anesthesia with halothane

3. Antiplatelet drugs

• Uses
  • Coronary artery disease
  • Cerebrovascular disease
  • Coronary angioplasty, bypass implants
  • Prosthetic heart valves
  • Venous thromboembolism
  • Peripheral vascular diseases
• Examples
  • Aspirin
  • Dipyridamole
  • Ticlopidine
  • Clopidogrel
  • Abcbdmab
  • Glycoprotein receptor antagonist

4. Vitamin K

5. Anticoagulants

• In vitro – Citrate, oxalate, EDTA
• In vivo – Coumarin, warfarin
• Both Vivo and vitro – heparin

6. Antifibrinolytics

• Epsilon amino Caproic acid
• Tranexamic acid

7. Iron preparation

8. Blood substitutes

• Blood products
  • Whole blood
  • Plasma
  • Plasma proteins
• colloidal plasma substitutes
  • Dextran
  • Gelatin
• Fluid plasma substitutes
  • 0.9% saline
  • 5% dextrose

9. Daily dose of iron

• Adult male – 0.5-1 mg
• Adult female – 1-2 mg
• Pregnancy – 3-5 mg in the last two trimesters

10. Megaloblastic anemia

• Occurs due to deficiency of vitamin B12 or folic acid
• Treatment includes vitamin B12 + folic acid
• Folic acid given alone may worsen the neurological deficit

Read And Learn More: Pharmacology Question and Answers

Blood Long Essays

Question 1. Explain the mechanism of iron absorption in the body. Add a note on different iron preparations
Answer:

Iron Absorption:

• Dietary iron is in the ferric form bound to proteins or organic acids
• The acidic medium of gastric juice releases this ferric ion
• Later it is converted to ferrous form by reducing substances like ascorbic acid and cysteine
• The ferrous form is soluble and is readily absorbed by mucosal cells
• It is oxidized to ferric form by ferroxidase
• This ferric form then combines with apoferritin and forms ferritin
• Iron from the mucosal cells may enter the bloodstream
• The ferric form is- Fe3+
• The ferrous form is Fe2+
• Gastric acid, reducing substances, and amino acids facilitate iron absorption
• Antacids, tetracyclines, phosphates, and phytates decrease iron absorption

Iron Preparations:

1. Oral iron preparations

It is the preferred route of administration

Oral iron Preparations:

• Ferrous sulfate -200 mg tab
  • Contains 20% hydrated salt and 32% dried salt
  • It is inexpensive
  • Produces a metallic taste in the mouth
• Ferrous gluconate -300 mg tab
  • Contains 12% of iron
  • Causes less gastric irritation
• Ferrous fumarate -200 mg tab
  • Contains 33% iron
  • It is less water soluble and tasteless
• Ferrous succinate -100 mg tab, 35% iron
  • Better absorbed and expensive
• Iron calcium complex -5% iron
  • Better absorbed and expensive
• Ferric ammonium citrate -45 mg tab
  • Better absorbed and expensive

Iron Dose:

• Total -200 mg given daily in 3 divided doses
• Prophylactic dose -30 mg daily

Iron Indications:

• Iron deficiency anemia

Iron Preparations Adverse Effects:

• Nausea, vomiting, epigastric pain
• Heartburn
• Staining of teeth
• Metallic taste
• Constipation

2. Parenteral iron preparations

• Intramuscular injection of iron is given deep in the gluteal region using the Z technique
• Intravenous is given slowly over 5-10 minutes

Parenteral Preparations:

• Iron dextran
  • It is a colloidal solution containing 50 mg of elemental iron
  • It is given intravenously and Intramuscularly
• Iron sorbitol citric acid complex
  • Contains 50 mg of elemental iron
  • Can be given only IM
  • If given IV it quickly saturates transferrin stores
  • Due to it free iron levels in the plasma rise and cause toxicity

Parenteral Dose:

• It is calculated using the formula:
• Iron requirement (in mg] = 4.4 * body weight (in kg) * Hb deficit (in g/dl)

Parenteral Indications:

• When oral iron is not tolerated
• Failure of absorption of oral iron
• Noncompliance
• In the presence of severe deficiency with chronic bleeding
• Along with erythropoietin

Parenteral Adverse Effects:

• Pain at the site of injection
• Pigmentation of skin
• Sterile abscess
• Fever
• Headache
• Joint pain, flushing, palpitation
• Chest pain, dyspnoea
• Anaphylactic reaction

2. Systemic agents

Question 2. Enumerate the agents used to control bleeding. Discuss their actions and uses.
Answer:

• Agents that help in controlling bleeding and are used in preventing or treating hemorrhagic conditions are known as coagulants

Control bleeding Classification:

1. Local agents or styptics

Control bleeding Actions:

• These materials provide a meshwork
• This activates the clotting mechanism and checks bleeding.

Question 3. Classify Anticoagulants. Discuss the mechanism of action, uses, and adverse effects of the coumarin derivatives.
Answer:

Anticoagulants:

• Anticoagulants are drugs used to reduce the coagulability of blood

Anticoagulants Classification:

• Used in vivo

1. Parenteral Anticoagulant

• • Heparin, low molecular weight heparin, heparan sulfate

2. Oral Anticoagulants .

• • Coumarin derivatives- Dicoumarol, warfarin, acenocoumarol, ethylbiscoumacetate
  • Indandione derivative- Phenindione
• Used in vitro

1. Heparin

2. Calcium complexing agents

• • Sodium citrate, sodium oxalate, sodium edetate.

Anticoagulants Coumarin Derivatives:

• Coumarin derivatives are
• Bishydroxycoumarin- Dicoumarol
• Warfarin
• Acenocoumarol- nicoumalone
• Ethylbiscoumacetate

Anticoagulants Mechanism of Action:

• They act only in vivo
• They interfere with the synthesis of vitamin K-dependent clotting factors in liver
• Act as a competitive antagonist of vitamin K
• Reduces plasma levels of clotting factors
• Interferes with the regeneration of the active hydro, quinone form of vitamin K.
• Blocks the gamma-carboxylation of glutamate residues in prothrombin, factors VII, IX, and X
• This gamma-carboxylation is needed by these factors for coagulation

Anticoagulants Uses:

• Deep vein thrombosis and pulmonary embolism
• Myocardial infarction
• Unstable angina,
• Rheumatic heart disease, atrial fibrillation
• Vascular surgery, prosthetic heart valves, retinal vessel thrombosis, extracorporeal circulation, hemodialysis

Anticoagulants Adverse Effects:

• Bleeding- ecchymosis, epistaxis, hematuria, bleeding in the GIT, intracranial bleeding
• Gastrointestinal disturbances
• Teratogenicity
• Skin necrosis

Question 4. Classify styptics. Describe the role of vitamin K when bleeding is due to oral anticoagulant therapy.
Answer:

Styptics:

• Styptics are local hemostatic substances used to stop bleeding from a local approachable site
• Commonly used styptics are
  • Thrombin
  • Fibrin
  • Oxidized cellulose
  • Gelatin foam
  • Adrenaline
  • Astringents

Role of Vitamin K

• Oral Anticoagulants interfere with the synthesis of vitamin K-dependent clotting factors in liver
• Act as a competitive antagonist of vitamin K
• Reduces plasma levels of clotting factors
• Interferes with the regeneration of the active hydroquinone form of vitamin K.
• Blocks the gamma-carboxylation of glutamate residues in prothrombin, factors VII, IX, and X ‘
• This gamma-carboxylation is essential for the ability of the clotting factors to bind Ca ions and to get the bound phospholipid surface necessary for the coagulation sequence to proceed
• Vitamin K acts as an antidote for Warfarin
• Administration of vitamin K by competitive antagonism with oral Anticoagulants reduces the anticoagulant action and brings about carboxylation of glutamate residues of prothrombin and factor VII, IX, and X necessary for the coagulation sequence to proceed.
• Hence vitamin K is used for bleeding due to oral Anticoagulants

Question 5. Describe how heparin and dicumarol act as Anticoagulants. Indicate their route of administration, duration of action and name their antagonists.
Answer:

• Heparin
  • It is a mucopolysaccharide found in the mast cells of the liver, lungs, and intestinal mucosa

Heparin Mechanism of Action:

• Heparin activates plasma antithrombin III
• Anti-thrombin III binds and inhibits activated Thrombin and coagulation factors Xa and IXa
• Heparin antithrombin III complex inhibits activated factor X and thrombin
• Low molecular weight heparin inhibits only factor X and not thrombin

Heparin Route of Administration:

• Heparin is given IV or SC

Heparin Duration of Action:

Heparin Antagonists:

• • Protamine sulfate is an antagonist of heparin
  • It is a low molecular-weight protein
  • When given IV it neutralizes heparin
  • It is used when heparin action needs to be terminated rapidly
• Dicoumarol:
  • Dicoumarol is a Coumarin derivative

Dicoumarol Mechanism of Action:

• It interferes with the synthesis of vitamin K-dependent clotting factors in liver
• Act as a competitive antagonist of vitamin K
• Reduces plasma levels of clotting factors
• Interferes with the regeneration of the active hydro-quinone form of vitamin K
• Blocks the gamma-carboxylation of glutamate residues in prothrombin, factors VII, IX, and X
• This gamma-carboxylation is needed by these factors for coagulation

Dicoumarol Route of Administration:

• It is given orally

Dicoumarol Duration of Action:

• Duration of action -4-7 day

Dicoumarol Antagonists:

• Vitamin K acts as an antagonist for Dicoumarol
• Administration of vitamin K by competitive antagonism reduces the anticoagulant action and brings about carboxylation of glutamate residues of prothrombin and factor VII, IX, and X necessary for the coagulation sequence to proceed

Question 6. Explain in detail about pharmacological action, pharmacodynamics, therapeutic uses, and toxicity of heparin.
Answer:

Anticoagulants:

• Anticoagulants are drugs used to reduce the coagulability of blood

Heparin

• It is a mucopolysaccharide found in the mast cells of the liver, lungs, and intestinal mucosa

Heparin Pharmacological Actions:

1. Anticoagulants

• Heparin is a powerful anticoagulant
• It is effective in vivo and in vitro
• At low concentrations, it prolongs activated partial thromboplastin time
• At high concentrations, it prolongs prothrombin time as well as partial thromboplastin time

2. Antiplatelet action

• Heparin inhibits platelet aggregation
• this prolongs the bleeding time

3. Lipaemia clearing

• Heparin activates lipoprotein lipase
• This hydrolyses triglycerides present in the plasma and thus clears the plasma of lipids

Heparin Pharmacodynamics:

• Heparin activates plasma antithrombin III
• Anti-thrombin III binds and inhibits activated Thrombin and coagulation factors Xa and IXa
• Heparin antithrombin III complex inhibits activated factor X and thrombin
• Low molecular weight heparin inhibits only factor X and not thrombin

Heparin Uses:

Heparin Low molecular weight heparin is used in:

• Prophylaxis of deep vein thrombosis and pulmonary embolism
• Treatment of established deep vein thrombosis
• Unstable angina
• To maintain patency of cannula and shunts in dialysis patients

Heparin Toxicity:

• Bleeding
• Thrombocytopenia
• Osteoporosis
• Alopecia
• Hypersensitivity reactions
• Hypoaldosteronism

Blood Short Essays

Question 1. Cyanocobalamin
Answer:

Coenzyme Forms:

• 5′- Deoxyadenosyl cobalamin
• Methylcobalamin

Functions:

1. Synthesis of methionine from homocysteine

• Vitamin B12 is used as Methylcobalamin in this reaction

2. Isomerization of methyl malonyl CoA to succinyl CoA

• It occurs in the presence of vitamin B12 Coenzyme, deoxy adenosylcobalamin

Cyanocobalamin Dietary Requirements:

• Adults- 3 micrograms/day
• Children-0.5-1.5 microgram/day
• During pregnancy and lactation- 4 micrograms/day

Cyanocobalamin Uses:

• Prevention and treatment of B12 deficiency
• Mega doses used in neuropathies, psychiatric disorders, cutaneous sarcoid

Question 3. List two Anticoagulants acting by different mechanisms. Mention any two uses of them.
Answer:

• Heparin
  • It is a mucopolysaccharide found in the mast cells of the liver, lungs, and intestinal mucosa

Heparin Mechanism of Action:

• Heparin activates plasma antithrombin III
• Anti-thrombin III binds and inhibits activated Thrombin and coagulation factors Xa and IXa
• Heparin antithrombin III complex inhibits activated factor X and thrombin
• Low molecular weight heparin inhibits only factor X and not thrombin

Heparin Uses:

Heparin Low molecular weight heparin is used in:

• • Prophylaxis of deep vein thrombosis and pulmonary embolism
  • Treatment of established deep vein thrombosis
  • Unstable angina
  • To maintain patency of cannula and shunts in dialysis patients
• Dicoumarol
  • Dicoumarol is a Coumarin derivative

Dicoumarol Mechanism of Action:

• It interferes with the synthesis of vitamin K-dependent clotting factors in liver
• Act as a competitive antagonist of vitamin K
• Reduces plasma levels of clotting factors
• Interferes with the regeneration of the active hydro-quinone form of vitamin K.
• Blocks the gamma-carboxylation of glutamate residues in prothrombin, factors VII, IX, and X
• This gamma-carboxylation is needed by these factors for coagulation.

Dicoumarol Uses:

• Deep vein thrombosis and pulmonary embolism
• Myocardial infarction.
• Unstable angina.
• Rheumatic heart disease, atrial fibrillation
• Vascular surgery, prosthetic heart valves, retinal vessel thrombosis, extracorporeal circulation, hemodialysis

Question 4. Iron-sorbitol-citric acid
Answer:

• Iron sorbitol citric acid complex is parenteral iron preparation.
• Contains 50 mg of elemental iron
• Can be given only IM
• If given IV it quickly saturates transferrin stores
• Due to it free iron levels in the plasma rise and cause toxicity

Iron-sorbitol-citric acid Dose:

• It is calculated using the formula:
• Iron requirement ( in mg) = 4.4 * body weight (in kg) * Hb deficit (in g/dl)

Iron-sorbitol-citric acid Indications:

• When oral iron is not tolerated
• Failure of absorption of oral iron
• Noncompliance
• In the presence of severe deficiency with chronic bleeding
• Along with erythropoietin

Iron-sorbitol-citric acid Adverse Effects:

• Pain at the site of injection
• Pigmentation of  skin
• Sterile abscess
• Fever
• Headache
• Joint pain, flushing, palpitation
• Chest pain, dyspnoea
• Anaphylactic reaction

Question 5. Anticoagulants
Answer:

• Anticoagulants are drugs used to reduce the coagulability of blood

Anticoagulants Classification:

• Used in vivo

1. Parenteral Anticoagulant

• • Heparin, low molecular weight heparin, heparan sulfate

2. Oral Anticoagulants

• • Coumarin derivatives- Dicoumarol, warfarin, acenocoumarol, ethylbiscoumacetate
  • Indandione derivative- Phenindione
• Used in vitro

1. heparin

2. Calcium complexing agents

• • Sodium citrate, sodium oxalate, sodium edetate.

Question 6. Compare heparin and oral anticoagulants.
(or)
Compare heparin and dicumarol
Answer:

Question 7. Explain the mechanism of action of streptokinase and mention one use of it.
Answer:

Streptokinase:

• Streptokinase is a fibrinolytic drug

Streptokinase Mechanism of Action:

• Streptokinase is antigenic
• It combines with plasminogen to form tissue plasminogen activator complex
• This complex then causes limited proteolysis of other plasminogen molecules to plasmin
• Plasmin degrades fibrin thereby dissolving the clot

Streptokinase Uses:

• Acute Myocardial infarction
• Deep vein thrombosis
• Pulmonary embolism

Question 8. Name two oral anticoagulants. Mention one drug treating toxicity of oral anticoagulants.
(or)
Dicumoral poisoning
Answer:

Oral Anticoagulants:

1. Coumarin derivatives- Dicoumarol, warfarin, acenocoumarol, ethylbiscoumacetate

2. Indandione derivative- Phenindione

Drug Used to Treat Toxicity of Oral Anticoagulants:

• Vitamin K is used to treat toxicity of oral anticoagulant
• Administration of vitamin K by competitive antagonism with oral Anticoagulants reduces the anticoagulant action and brings about carboxylation of glutamate residues of prothrombin and factor VII, IX, and X necessary for coagulation sequence to proceed

Question 9. Heparin and Warfarin.
Answer:

Blood Short Question And Answers

Question 1. Drugs for anemia.
Answer.

Question 2. Ferrous sulfate.
Answer:

Ferrous sulfate is oral iron preparation

Ferrous sulfate Dose:

• 200 mg tab, 3-4 tablets daily

Ferrous sulfate Indication:

• Prophylactic use in iron deficiency Anemia

Ferrous sulfate Adverse Effects:

• Nausea, vomiting, epigastric pain
• Heartburn
• Staining of teeth
• Metallic taste
• Constipation

Question 3. Folic acid
Answer:

Folic acid is important in one-carbon metabolism

Folic acid Sources:

• Green vegetables, liver, yeast, egg, milk, and some fruits

Folic acid Functions:

• The Coenzyme of it, tetrahydrofolate( THF], serves as an acceptor or donor of one carbon units
• It is involved in the synthesis of important compounds like
• Purines- Incorporated into DNA and RNA
• Pyrimidine nucleotide- deoxythymidylic acid- Involved in the synthesis of DNA
• Aminoacids- Glycine, serine, ethanolamine, and choline
• N-Formylmethionine- Initiator of protein biosynthesis

Folic acid Deficiency Manifestations:

• Megaloblastic anemia
• Glossitis
• Diarrhea
• Weakness

Question 4. Drugs used in microcytic anemia.
Answer.

1. Oral iron preparation

• Ferrous sulfate-200 mg tab
• Ferrous fumarate -200 mg tab

2. Parenteral iron preparation

• Iron dextran containing 50 mg of elemental iron
• Iron sorbitol citric acid complex containing 50 mg of elemental iron

Question 5. Drugs used for pernicious anemia.
Answer:

1. Vitamin B12 supplements
2. 1-5 mg of folic acid and iron preparation

Question 8. Indications for parenteral use of iron.
Answer:

• When oral iron is not tolerated
• Failure of absorption of oral iron
• Noncompliance
• In the presence of severe deficiency with chronic bleeding
• Along with erythropoietin

Question 6. Mention two oral and parenteral preparations.
Answer:

Oral Preparations:

• Ferrous sulfate
• ferrous gluconate
• Ferrous fumarate
• Colloidal ferric hydroxide

Parenteral Preparations:

• Iron dextran
• Iron sorbitol citric acid complex

Question 7. Vitamin C is given with iron in the treatment of anemia.
Answer:

• Vitamin C Improves Absorption Of Iron In The Intestine
• It maintains ferrous salts in a reduced state
• So vitamin C is used in the treatment of anemia along with iron,

Question 8. Vitamin K deficiency.
Answer:

Causes of Vitamin K Deficiency:

• Liver diseases
• Obstructive jaundice
• Malabsorption
• Long-term antimicrobial therapy altering intestinal flora

Vitamin K Deficiency Manifestations:

• Bleeding tendencies- hematuria, GIT bleeding, epistaxis, ecchymosis

Question 9. Heparin
Answer:

• It is a mucopolysaccharide found in the mast cells of the liver, lungs, and intestinal mucosa

Heparin Uses:

• Low molecular weight heparin is used in:
• Prophylaxis of deep vein thrombosis and pulmonary embolism
• Treatment of established deep vein thrombosis
• Unstable angina
• To maintain patency of cannula and shunts in dialysis patients

Heparin Toxicity:

• Bleeding
• Thrombocytopenia
• Osteoporosis
• Alopecia
• Hypersensitivity reactions
• Hypoaldosteronism

Question 10. Vitamin K
Answer:

• It is a fat-soluble vitamin

Vitamin K Sources:

Vitamin K

1. Animals sources

• Egg yolk, meat, liver, cheese and dairy products

2. Plant sources

• Cabbage, cauliflower, tomatoes, alfa, spinach

Vitamin K Functions:

• It helps in blood coagulation

Vitamin K Daily Requirements:

• 70-140 micrograms/day

Question 11. Fibrinolytic
Answer:

• Fibrinolytic are drugs that lose the clot or thrombus by activating the natural fibrinolytic system
• Fibrinolytic agents are:
  • Streptokinase
  • Urokinase
  • Alteplase
  • Replace
  • Tenecteplase

Fibrinolytic Uses:

• Acute Myocardial infarction
• Deep vein thrombosis
• Pulmonary embolism

Fibrinolytic Adverse Effects:

• Bleeding
• Hypotension
• Fever
• Anaphylactic reactions

Fibrinolytic Contraindications:

• In recent surgeries
• Injury
• GIT bleeding
• Stroke
• Severe hypertension
• Bleeding disorders

Question 12. Hemostasis
Answer:

• Hemostasis is the process of stopping bleeding postsurgically or from a site of injury
• It can be achieved by
  • Applying pressure at the bleeding site
  • Suturing
  • Use of styptics
• It occurs by
  • Contraction of the injured vessel wall
  • Adhesion and aggregation of platelets to form a plug
  • Formation of a blood clot
  • Dissolution of the clot by fibrinolysis

Question 13. Warfarin sodium
Answer:

• It is a Coumarin derivative

Warfarin sodium Uses:

• Deep vein thrombosis and pulmonary embolism
• Myocardial infarction
• Unstable angina
• Rheumatic heart disease, atrial fibrillation
• Vascular surgery, prosthetic heart valves, retinal vessel thrombosis, extracorporeal circulation, hemodialysis

Warfarin sodium Adverse Effects:

• Bleeding- ecchymosis, epistaxis, hematuria, bleeding in the git, intracranial bleeding
• Gastrointestinal disturbances
• Teratogenicity
• Skin necrosis

Question 14. Oral anticoagulants
Answer:

• Oral anticoagulants are:
  • Coumarin derivatives- Dicoumarol, warfarin, acenocoumarol, ethylbiscoumacetate
  • Indandione derivative- Phenindione

Question 15. Uses of vitamin K
Answer:

• Act as a cofactor for the synthesis of coagulation proteins- Ffrothrombin, factor VII, IX, and X
• Required for carboxylation of glutamic acid residues of osteocalcin
• Participates in the coagulation cascade

Question 16. Vitamin K used in the overdosage of Warfarin
Answer:

• Warfarin interferes with the synthesis of vitamin K-dependent clotting factors in liver
• Act as a competitive antagonist of vitamin K
• Reduces plasma levels of clotting factors
• Interferes with the regeneration of the active hydro-quinone form of vitamin K
• Blocks the gamma-carboxylation of glutamate residues in prothrombin, factors VII, IX, and X v
• This gamma-carboxylation is essential for the ability of the clotting factors to bind Ca ions and to get the bound phospholipid surface necessary for the coagulation sequence to proceed
• Vitamin K acts as an antidote for Warfarin
• Administration of vitamin K by competitive antagonism with Warfarin reduces the anticoagulant action and brings about carboxylation of glutamate residues of prothrombin and factor VII, IX, and X necessary for the coagulation sequence ta proceed

Question 17. Adverse effects of vitamin B12.
Answer:

• Vitamin B12 is used
• In the treatment of vitamin B12 deficiency
• Cyanacobalamine -100 ml in. daily
• Hydroxocobalamin -100-500,1000 mg daily
• Multivitamins for oral use
• B12 deficiency – Prophylaxis 3-10 mg daily
• Treatment of megaloblastic anemia
  • B12 neuropathies, psychiatric disorders, cutaneous sarcoid, and as a general tonic to allay fatigue and improve growth

vitamin B12 Adverse Effects:

• Anaphylactoid reaction on IV injection occurs due to sulfite contained in the formulation

Question 18. Name two oral anticoagulants. Mention two adverse effects.
Answer:

Drugs Acting On Kidney Important Notes

1. Classification of diuretics

• High ceiling diuretics
  • Furosemide
  • Bumetanide
  • Torsemide
• Moderate efficacy diuretics
  • Thiazides – chlorothiazides, hydrochlorothiazides
  • Thiazide related agents – chlorthalidone,, clopamide
• Low efficacy diuretics
  • Potassium sparing diuretics – triamterene, amiloride, spironolactone
  • Carbonic anhydrase inhibitor – acetazolamide .
  • Osmotic diuretics – Mannitol, urea
  • Methylxanthines – theophylline
• Newer agents
  • Vasopressin antagonists
  • Conivaptan

Diuretics Drugs

2. Complications of high ceiling diuretics and thiazides

• Hypokalaemia
• Dilutional hyponatremia
• GIT and CNS disturbances
• Hearing loss
• Magnesium depletion
• Hyperuricaemia
• Hyperglycaemia
• Hyperlipidaemia
• Acute saline depletion
• Fall in BP

3. Drugs contraindicated in renal failure are

• Cephalothin
• Cephaloridine
• Nalidixic acid
• Nitrofurantoin
• Talampicillin
• Tetracyclines

Diuretics Drugs

4. Drugs that require dose reduction in renal failure are:

Drugs Acting On Kidney Short Essays

Question 1. Classify diuretics. Write the mechanism of action of thiazides
Answer:

Diuretics:

• Drugs that increase urine and solute excretion causing loss of sodium and water from the body are called diuretics.

Diuretics Classification:

1. High efficacy or loop diuretics

• Furosemide, Bumetanide, Torasemide

2. Medium efficacy diuretics

• Benzothiadiazine or thiazides
  • Hydrochlorothiazide, Benzthiazide
• Thiazides like drugs
  • Chlorthalidone, Metolazone

Diuretics Drugs

3. Low efficacy or weak diuretics

• Carbonic anhydrase inhibitors
  • Acetazolamide
• Potassium sparing diuretic
  • Aldosterone antagonist- spironolactone
  • Inhibitors of renal epithelial sodium channel- Triamterene, amiloride
• Osmotic diuretics
  • Mannitol, isosorbide, Glycerol

Mechanism of Action of Thiazides:

Question 2. Compare acetazolamide and frusemide.
Answer:

Question 3. Compare frusemide and spironolactone
Answer:

Question 4. Compare chlorothiazide and spironolactone
Answer:

Diuretics Drugs

Question 5. Compare Hydrochlorothiazide and frusemide
Answer:

Question 6. Chlorothiazide
Answer:

• Chlorothiazide is a medium efficacy thiazide diuretics

Chlorothiazide Uses:

• Hypertension
• Congestive cardiac failure
• Hepatic or renal edema –
• Hypercalciuria with renal stones
• Diabetes insipidus

Chlorothiazide Adverse Effects:

• Hypokalaemia
• Carbohydrate intolerance
• Fatigue, loss of energy
• Impotence
• Hyperlipidaemia, hyperuricemia
• Decreased libido

Read And Learn More: Pharmacology Question and Answers

Question 7. Mention two therapeutic uses and two adverse effects of frusemide.
Answer:

Frusemide:

• It is high efficacy diuretics

Frusemide Uses:

• Edema
• Hypertension
• Forced diuresis
• Hypercalcaemia
• Renal stones
• During blood transfusions

Frusemide Adverse Effects:

• Acute salt depletion
• Hepatic coma
• Photosensitivity
• Headache
• Giddiness
• Nausea, vomiting
• Paresthesia, impotence

Question 8. Complications of diuretics.
Answer:

1. Hypokalaemia

• Occurs with high ceiling diuretics and thiazides
• Characterized by weakness, fatigue, muscle cramps, cardiac arrhythmias
• Treatment:
  • High dietary potassium intake
  • Supplements of KC1
  • Concurrent use of potassium-sparing diuretics

2. Acute saline depletion

• Causes dehydration and a fall in blood pressure

3. Hyponatremia – more with high ceiling diuretics

4. GIT disturbances – nausea, vomiting, diarrhea

5. CNS disturbances – headache, giddiness, weakness, paraesthesia

6. Hearing loss – with high-ceiling diuretics

7. Hypersensitivity – skin rashes, feverhyperuricaemia – with long-term use of thiazides

8. Hyperglycaemia, hyperlipidemia – when diuretics are used as antihypertensives

9. Magnesium depletion – due to prolonged use

10. Hyperkalaemia – with potassium-sparing diuretics

Drugs Acting On Kidney Short Question And Answers

Question 1. Potassium-sparing diuretics
Answer:

• Potassium-sparing diuretics are:
  • Spironolactone
  • Triamterene
  • Amiloride

Potassium-sparing diuretics Mechanism:

• Act as aldosterone antagonists
• Directly inhibit ion channels

Potassium-sparing diuretics Site of Action:

• Act as aldosterone antagonists
• Directly inhibits ion channels

Potassium-sparing diuretics Uses:

• Used along with thiazides and loop diuretics to prevent potassium loss
• Edema
• Hypertension
• Aldosteronism

Question 4. Mannitol
Answer:

• Mannitol is an osmotic diuretics
• It helps to retain water in the proximal convoluted tubule and the descending limb of the Henle’s loop by osmosis
• This causes water diuresis and loss of sodium
• They are ineffective when given orally
• So it is given IV

Mannitol Uses:

• To maintain urine volume and prevent oliguria during hemolysis and shock.
• Used in the reduction of intracranial and intraocular pressure

Mannitol Adverse Effects:

• Dehydration
• ECF volume expansion
• Headache
• Hyperallergic reactions

Question 5. Spironolactone
Answer:

• Spironolactone is a potassium-sparing diuretic
• It is low efficacy diuretics
• It is an aldosterone antagonists

Spironolactone Uses:

• In the treatment of Hypercalcaemia and renal stones
• Along with other diuretics in the treatment of hypertension, to reduce hypokalaemia
• In the treatment of aldosteronism

Spironolactone Adverse Effects:

• Drowsiness
• Hyperkalemia in patients with renal insufficiency
• Gynaecomastia
• Skin rashes

Question 6. Loop diuretics
(or)
High ceiling diuretics
Answer:

• Loop diuretics are high efficacy diuretics
• They act by inhibiting sodium chloride reabsorption in the ascending limb of Henle’s loop
• They include
  • Frusemide
  • Bumetanide
  • Piretanide

Loop diuretics Uses:

• Edema- cardiac, cerebral, hepatic, renal, pulmonary
• Hypertension
• Hypercalcaemia, Renal stones
• Hyperkalemia
• Barbiturate poisoning to induce forced diuresis

Question 7. Osmotic diuretics
Answer:

• Osmotic diuretics include inert drugs like
  • Mannitol
  • Urea
  • Glycerol
• It helps to retain water in the proximal convoluted tubule and the descending limb of the Henle’s loop by osmosis
• This causes water diuresis and loss of sodium
• They are ineffective when given orally
• So it is given IV

Osmotic diuretics Uses:

• To maintain urine volume and prevent oliguria during hemolysis and shock.
• Used in the reduction of intracranial and intraocular pressure

Osmotic diuretics Adverse Effects:

• Dehydration
• ECF volume expansion
• Headache
• Hyperallergic reactions

Question 8. Triamterene and frusemide
Answer:

Question 9. Rationale of combining thiazides with spironolactone
(or)
The rationale for combining spironolactone with frusemide
Answer:

• Frusemide and Thiazides cause excess excretion of potassium from the body
• The sodium present in the distal convoluted tubule may also be exchanged for potassium ions which may be excreted in the urine
• This may lead to hypokalaemia
• Spironolactone reduces potassium loss by inhibiting the action of aldosterone which is responsible for potassium secretion
• So spironolactone is combined with Frusemide or Thiazide

Question 10. Enlist three diuretic drugs and one different use for each.
Answer:

Question 11. Name two loop diuretics. Mention two uses of them.
Answer:

Loop Diuretics:

• Frusemide
• Bumetanide
• Torasemide

Loop Diuretics Uses:

• Edema
• Acute Pulmonary Edema
• Hypertension

Gastrointestinal Important Notes

1. Drugs used in peptic ulcer

2. Cimetidine

• Inhibits several cytochrome P-450 isoenzyme
• Reduces hepatic blood flow
• Inhibits the metabolism of many drugs

3. Kaolin

• It is a hydrated aluminum silicate
• Used in the treatment of diarrhea
• Act as an absorbent of bacteria and bacterial toxin

4. Antacids

• They are salts of magnesium, calcium, and aluminum
• Produces laxatives or constipating effects

5. H2 receptor antagonist

• They are ranitidine, cimetidine, famotidine
• Inhibit gastric secretion
• Adverse effects
  • Gynaecomastia
  • Impotence

6. Omeprazole

• Inhibits proton pump
• It is powerful
• Totally abolishes HC1 secretion

7. Drugs used in motion sickness

• Scopolamines
• Antihistamines

Gastrointestinal Long Essays

Question 1. What is an antacid? Classify with suitable examples. Mention the merits and demerits of NaHC03 as an antacid.
Answer:

Antacids

• Antacids are basic substances that neutralize gastric acid and raise the pH of gastric contents

Antacids Classification

1. Systemic antacids

• Sodium bicarbonate
• Sodium citrate

2. Non-systemic antacids

• Magnesium hydroxide
• Magnesium trisilicate
• Aluminum hydroxide gel
• Magaldrate

Sodium Bicarbonate as Antacids:

Sodium Bicarbonate Merits:

• Water soluble
• Acts instantly
• Potent neutralizer
• Raises pH above 7

Sodium Bicarbonate Demerits:

• Absorbed systemically
• Acid rebounds occur
• Increases sodium load

Gastrointestinal Short Essays

Question 1. Classify drugs used in peptic ulcer
Answer:

Peptic ulcer occurs in that part of the gastrointestinal tract which is exposed to gastric acid and pepsin. Produces carbon dioxide in the stomach

Classify drugs used in peptic ulcer  Classification:

• Drugs used in the treatment of peptic ulcer are:

1. Reduction of gastric acid secretion

• H2 Antihistamines
  • Cimetidine, Ranitidine, Famotidine, Roxatidine, Loxatidine
• Proton pump inhibitors
  • Omeprazole, Lansoprazole, Pantoprazole, Rabepra- zole
• Anticholinergic
  • Pirenzepine, Propantheline
• Prostaglandin analogs
  • Misoprostol

2. Neutralization of gastric acid- antacids

• Systemic antacids
  • Sodium bicarbonate
  • Sodium citrate
• Nonsystemic antacids
  • Magnesium hydroxide
  • Magnesium trisilicate
  • Aluminum hydroxide gel
  • Magaldrate

3. Ulcer protective

• Sucralfate, colloidal bismuth substrate

4. Anti-H pylori drugs

• Amoxicillin, metronidazole, Clarithromycin

Question 2. Antihistaminic drugs used in peptic ulcer.
(or)
H2 blockers
Answer:

• Antihistaminic drugs or H2 blockers are:
  • Cimetidine, Ranitidine, Famotidine, Roxatidine, Loxatidine
• They are highly effective drugs

H2 blockers  Actions:

1. H2 blockade-Causes:

• Blockade of histamine-induced gastric secretion
• Cardiac stimulation
• Uterine relaxation
• Bronchial relaxation
• Fall in BP

2. Gastric secretion

• Inhibition of gastric secretion
• Prevention of gastric ulceration occurring due to stress and drugs

H2 blockers  Uses:

• Duodenal ulcer- provides rapid and marked pain relief
• Gastric ulcer- Heal NSAID-associated ulcers
• Stress ulcers- Occurring in situations like severe burns, trauma, prolonged surgery, etc.
• Zollinger-Elison syndrome
• Gastroesophageal reflux disease
• Prophylaxis of aspiration pneumonia

H2 blockers  Adverse Effects:

• Headache, dizziness, bowel upset, dry mouth, rashes
• CNS effects- confusion, restlessness, hallucinations
• Antiandrogenic effect of cimetidine

Question 3. Ranitidine
Answer:

• Ranitidine is an H2 receptor blocker

Read And Learn More: Pharmacology Question and Answers

Ranitidine  Uses:

• Duodenal ulcer- provides rapid and marked pain relief
• Gastric ulcer- Heal NSAID-associated ulcers
• Stress ulcers- Occurring in situations like severe burns, trauma, prolonged surgery, etc.
• Zollinger-Elison syndrome
• Gastroesophageal reflux disease
• Prophylaxis of aspiration pneumonia

Ranitidine  Advantages:

• More potent
• Longer-acting
• Has no antiandrogenic effects
• No CNS effects as it does not cross BBB
• Does not inhibit microsomal enzymes
• Has mild side effects

Question 4. Antacids
Answer:

Antacids:

• Antacids are basic substances that neutralize gastric acid and raise the pH of gastric contents.

Antacids Classification:

1. Systemic antacids

• Sodium bicarbonate
• Sodium citrate

2. Nonsystemic antacids

• Magnesium hydroxide
• Magnesium trisilicate
• Aluminum hydroxide gel
• Magaldrate

Antacids Uses:

• For intercurrent pain relief and acidity
• Nonulcer dyspepsia
• Minor episodes of heartburn
• Reflux esophagitis

Antacids Disadvantages:

• Needed in large and frequent dose
• Inconvenient
• Can cause acid rebound and bowel upset
• Poor patient acceptability

Question 5. Compare promethazine and Ranitidine
Answer:

Question 6. Emetics
Answer:

Emetics are drugs that produce vomiting

Emetics  Mechanism:

Emetics  Uses:

• To induce vomiting when noxious substances are ingested

Emetics  Drugs Used:

• Mustard powder-1 teaspoon with water
• Hypertonic salt solution
• Apomorphine- SC/ IM
• Ipecacuanha-15-20 ml

Emetics  Contraindications:

• Corrosive poisoning
• CNS stimulant drug poisoning
• Kerosene or petroleum poisoning
• In unconscious patients

Question 7. Metoclopramide
Answer:

• Metoclopramide is widely used as antiemetic

Metoclopramide  Actions:

• Increases gastric peristalsis
• Relaxes the pylorus and the first part of the duodenum
• Speeds up gastric emptying

Metoclopramide  Mechanism of Action:

• Blocks D₂ dopamine receptors in the CTZ
• Enhances acetylcholine release from the cholinergic neurons in the gut

Metoclopramide  Uses:

• Antiemetic- in postoperative, drug-induced, disease-associated vomiting
• Gastrokinetic- To accelerate gastric emptying
  • Before induction of general anesthesia
  • To assist the passage of the tube into the duodenum
  • To relieve diabetes-associated gastric stasis
• Dyspepsia
• Gastroesophageal reflux disease- provides symptomatic relief

Metoclopramide  Adverse Effects:

• Sedation
• Dizziness
• Diarrhea
• Muscle dystonia
• Long-term use causes:
  • Parkinsonism
  • Galactorrhoea
  • Gynaecomastia

Question 8. Prokinetic Agents
Answer:

Drugs that promote gastrointestinal and speedy gastric emptying are called prokinetic agents.

They are as follows:

Question 9. Rationale of using domperiodone as antiemetics
(or)
Domperidone is preferred over Metaclopra- mide in vomiting
Answer:

• Domperidone is D₂ antagonist
• Its action is not blocked by atropine
• It crosses the blood-brain barrier poorly
• It does not have extrapyramidal side effects
• Side effects of Domperidone are much less than that with Metadopramide
• It includes only dry mouth, loose stools, headache, rashes, galactorrhoea
• Thus it is preferred over Metadopramide as an Antiemetic

Question 10. Mention two antiemetics.
Answer:

Antiemetics:

1. Metoclopramide
2. Domperidone

Question 11. Drugs used as purgatives
Answer:

• Purgatives are drugs that promote defecation
• They are also called laxatives

Purgatives  Classification:

1. Bulk-forming

• Dietary fiber- Bran, plantago seeds, is Paula, methylcellulose

2. Stool softener

• Docusates, liquid paraffin

3. Stimulant Purgatives

• Diphenylmethanes
  • Phenolphthalein, bisacodyl
• Anthraquinones
  • Senna, cascara sagrada
• 5-HT₄ agonist
  • Tegaserod

4. Osmotic Purgatives

• Magnesium salts- sulfate, hydroxide
• Sodium salts- sulfate, phosphate
• Sodium potassium tartrate

Purgatives Mechanisms:

Increases water content of feces by

1. Osmotic action

3. Secondary effects

• Increases propulsive activity
• Decreases time for absorption

Purgatives Uses:

• In functional constipation
• In bedridden patients
• To avoid straining at stools
• Preparation of bowel for surgery, colonoscopy, abdominal X-ray
• After certain antihelminthic

Question 12. ORS
Answer:

• Oral rehydration solution is used in patients with diarrhea to replenish the lost water

ORS  Composition:

• NaCl -3.5 g
• KC1 -1.5 g
• Trisodium citrate -2.9 g
• Glucose -20 g
• Water-1 liter

ORS  Uses:

• To replace fluids and salts lost from the body during diarrhea
• To restore and maintain hydration
• Maintain electrolyte and pH balance
• Maintain hydration in patients postsurgically after burns, trauma, and in heat stroke

Question 13. The rationale for using loperamide in diarrhea
Answer:

• Loperamide is an opiate analog
• It is the potent constipating agent
• It has a poor water solubility
• Entry of it into the brain is negligible
• So it has no CNS effects occur
• It also inhibits GIT secretions
• Abdominal cramps and rashes are common adverse effects.
• Thus it is preferred for diarrhea

Question 14. PPIs (proton pump inhibitors)
Answer:

• Proton pump inhibitors are the most efficient inhibitors of the gastric acid secretion
• They are given as enteric-coated granules to avoid degeneration by the acid in the stomach
• They are:
  • Omeprazole
  • Lansoprazole
  • Pantoprazole
  • Rabeprazole
  • Dexrabeprazole
  • Esomeprazole

PPIs (proton pump inhibitors)  Mechanism of Action:

• Proton pump inhibitors get accumulated in the parietal cells

PPIs (proton pump inhibitors)  Uses:

1. Peptic ulcers

• Given for 4-8 weeks
• Ulcers heal fast
• Relief of pain is rapid and excellent

2. Gastroesophageal reflux disease

• Produces rapid symptomatic relief
• It is more effective than H2 blockers

3. Use in H. pylori treatment regimen

4. Zollinger- Ellison syndrome

PPIs (proton pump inhibitors)  Adverse Effects:

• Adverse effects are minimal
• They occur rarely
• It includes:
  • Nausea
  • Loose stools
  • Headache
  • Abdominal pain
  • Muscle and joint pain
  • Dizziness
  • Rashes
  • Leucopenia
  • Hepatic dysfunction

Gastrointestinal Short Question and Answers

Question 1. H2 antagonist
Answer:

• Antihistaminic drugs or H2 blockers are:
  • Cimetidine, Ranitidine, Famotidine, Roxatidine, Loxatidine
• They are highly effective drugs

Question 2. Cimetidine
Answer:

• Cimetidine is an H2 blocker
• It was the first H2 blocker to be introduced

Cimetidine  Uses:

• Duodenal ulcer- provides rapid and marked pain relief
• Gastric ulcer- Heal NSAID-associated ulcers
• Stress ulcers- Occurring in situations like severe burns, trauma, prolonged surgery, etc.
• Zollinger-Elison syndrome
• Gastroesophageal reflux disease
• Prophylaxis of aspiration pneumonia

Question 3. Antacids
Answer:

Antacids are basic substances that neutralize gastric acid and raise the pH of gastric contents.

Antacids Classification:

1. Systemic antacids

• Sodium bicarbonate
• Sodium citrate

2. Nonsystemic antacids

• Magnesium hydroxide
• Magnesium trisilicate
• Aluminum hydroxide gel
• Magaldrate

Question 4. Sucralfate
Answer:

Sucralfate is an ulcer protective agent

Sucralfate Mechanism:

• In an acidic medium, Sucralfate polymerizes to form a sticky, viscid gel
• This adheres firmly to the base of the ulcer
• Act as a physical barrier preventing acid, pepsin, and bile from coming in contact with ulcer base
• Stimulates prostaglandin secretion and promotes healing

Sucralfate Uses:

• Duodenal ulcer
• Gastric ulcer

Sucralfate Adverse Effects:

• Constipation
• Dry mouth

Question 5. Carbenoxolone sodium
Answer:

• Carbenoxolone sodium is a steroid-like compound
• It is obtained from glycyrrhizic acid

Carbenoxolone sodium Mechanism of Action:

• It alters the composition of mucous
• Makes it more viscid
• Gets adheres to the gastric mucosa
• Protects the ulcer base
• Inhibits pepsin activity
• Prolong action of prostaglandin

Carbenoxolone sodium Adverse Effects:

• It causes salt and water retention so it is not preferred

Question 6. Omeprazole is used in peptic ulcer
Answer:

• Omeprazole is a proton pump inhibitor
• It is used in the treatment of peptic ulcer due to the following mechanism

Question 7. Ranitidine
Answer:

• Ranitidine is an H2 receptor blocker

Ranitidine Uses:

• Duodenal ulcer- provides rapid and marked pain relief
• Gastric ulcer- Heal NSAID-associated ulcers
• Stress ulcers- Occurring in situations like severe burns, trauma, prolonged surgery, etc.
• Zollinger-Elison syndrome
• Gastroesophageal reflux disease
• Prophylaxis of aspiration pneumonia

Question 8. Magnesium sulfate
Answer:

• Magnesium sulfate is a uterine relaxant

Magnesium sulfate  Uses:

• To control convulsions
• To reduce BP in toxemia of pregnancy
• To suppress uterine contractions

Magnesium sulfate  Adverse Effects:

• Cardiac arrhythmias
• Muscular paralysis
• CNS depression
• Respiratory depression

Question 9. Prokinetic drugs
Answer:

• Drugs that promote gastrointestinal motility and speed gastric emptying are called prokinetic agents
• Drugs that are used as prokinetic drugs are
  • Metoclopramide
  • Domperidone
  • Cisapride
  • Mosapride
  • Tegaserod

Question 10. Aluminum hydroxide
Answer:

• Aluminum hydroxide is a weak and slow-acting antacid
• Food interferes with its action
• It is an astringent, so it forms a protective coating over the ulcers
• The aluminum ions relax smooth muscle
• It delays gastric emptying
• It binds to phosphate and prevents its absorption
• It causes constipation

Question 11. Metoclopramide
Answer:

• Metoclopramide is widely used as antiemetic

Metoclopramide  Uses:

• Antiemetic- in postoperative, drug-induced, disease-associated vomiting
• Gastrokinetic- To accelerate gastric emptying
  • Before induction of general anesthesia
  • To assist the passage of the tube into the duodenum
  • To relieve diabetes-associated gastric stasis
• Dyspepsia
• Gastroesophageal reflux disease- provides symptomatic relief

Metoclopramide  Adverse Effects:

• Sedation
• Dizziness
• Diarrhea
• Muscle dystonia
• Long-term use causes:
  • Parkinsonism
  • Galactorrhoea
  • Gynaecomastia

Question 12. Cimetidine and Ranitidine
Answer:

• Cimetidine and ranitidine are H2 blockers

Cimetidine and Ranitidine  Uses:

• Duodenal ulcer- provides rapid and marked pain relief
• Gastric ulcer- Heal NSAID-associated ulcers
• Stress ulcers- Occurring in situations like severe burns, trauma, prolonged surgery, etc.
• Zollinger-Elison syndrome
• Gastroesophageal reflux disease
• Prophylaxis of aspiration pneumonia

Cimetidine and Ranitidine  Adverse Effects

• Headache, dizziness, bowel upset, dry mouth, rashes
• CNS effects- confusion, restlessness, hallucinations
• Antiandrogenic effect of cimetidine

Question 13. Ranitidine preferred over Cimetidine
Answer:

• Ranitidine is preferred over cimetidine because it is:
• More potent
• Longer-acting
• Has no antiandrogenic effects
• No CNS effects as it does not cross BBB
• Does not inhibit microsomal enzymes
• Has mild side effects

Question 14. Classify drugs used in peptic ulcers
Answer:

• Drugs used in the treatment of peptic ulcer are:

1. Reduction of gastric acid secretion

1. H2 Antihistamines

• Cimetidine, Ranitidine, Famotidine, Roxatidine, Loxatidine

2. Proton pump inhibitors

• Omeprazole, Lansoprazole, Pantoprazole, Rabepra- zole

3. Anticholinergic

• Pirenzepine, Propantheline

4. Prostaglandin analogs

• Misoprostol

2. Neutralization of gastric acid- antacids

1. Systemic antacids

• Sodium bicarbonate
• Sodium citrate

2. Non-systemic antacids

• Magnesium hydroxide
• Magnesium trisilicate
• Aluminum hydroxide gel
• Magaldrate

3. Ulcer protection.

• Sucralfate, colloidal bismuth substrate

4. Anti-H pylori drugs

• Amoxicillin, metronidazole, Clarithromycin

Question 15. The rationale of combining aluminum hydroxide gel and magnesium trisilicate as antacids
Answer:

• Aluminum hydroxide gel is slow-acting and delays gastric emptying
• Magnesium trisilicate is fast acting and hastens gastric emptying.
• Combining both leads to:
  • Prolongs the action of the drug
  • Makes it intermediate-acting
  • Maximizes the wanted effects
  • Minimizes the adverse effects
  • Neutralizes luxating effect of magnesium trisilicate
  • Neutralizes constipating effect of aluminum hydroxide

Question 16. Proton pump inhibitors
Answer:

• Protons pump Inhibitors are the most efficient. Inhibitors of the gastric add secretions
• They act by blocking the final step in gastric acid secretions
• They are inactive at neutral pH and only get activated at a pH less than 5
• They are
  • Omeprazole
  • Lansoprazole
  • Pantoprazole
  • Rabeprazole

Proton pump inhibitors Uses:

• Peptic ulcer
• Severe Gastroesophageal reflux disease
• The component in the H.pylori treatment regimen
• Zollinger Ellison syndrome

Question 17. Aspirin is contraindicated in peptic ulcers
Answer:

• Aspirin is contraindicated in peptic ulcer because:
• It irritates gastric mucosa
• It causes gastric distress, nausea, vomiting
• It stimulates CTZ
• In the acidic pH of the stomach, it remains in an unionized form
• Drug particles get attached to the gastric mucosa
• They promote back diffusion of acid in the stomach
• It inhibits prostaglandin synthesis
• Inhibits gastric acid secretions
• Increases production of the mucosa
• This leads to the occurrence of ulcers
• This leads to reduced platelet aggregation
• Promotes bleeding in ulcers

Question 18. Name two drugs used to suppress vomiting
Answer:

• Drugs used to suppress vomiting are called antiemetics

Suppress Vomiting  Classification:

• Anticholinergics- Hyoscine, Dicyclomine
• HI antihistaminics- Promethazine, Diphenhydramine, Dimenhydrinate.
• Neuroleptics- Chlorpromazine, prochlorperazine
• Prokinetic drugs- Metoclopramide, Domperidone, Cisapride
• 5-HT3 antagonists- Ondansetron
• Adjuvant antiemetics- Dexamethasone, benzodiazepines

Question 19. The rationale for using Metoclopramide in vomiting
Answer:

• Metoclopramide is used in vomiting because it
• Increases gastric peristalsis
• Relaxes the pylorus and the first part of the duodenum
• Speeds up gastric emptying
• Blocks D₂ dopamine receptors in the CTZ
• Enhances acetylcholine release from the cholinergic neurons in the gut

Question 20. Promethazine
Answer:

• Promethazine is a highly sedative H1 antagonist

Promethazine  Uses:

• Allergic disorders
• Pruritis
• Common cold
• Preanasethetic medication
• Parkinsonism

Question 21. Bulk purgatives
Answer:

• Bulk purgatives include
  • Bran
  • Plantago seeds
  • Agar
  • Methylcellulose
  • Ispaghula husk
• These are indigestible vegetable fiber and hydrophilic colloids
• It increases volume and lowers the viscosity of intestinal contents
• Used for prevention and treatment of functional constipation
• It requires daily administration for at least 3-4 days
• It forms a large, soft, and solid stool
• A large amount of water must be taken with it

Question 22. Name two osmotic purgatives
(or)
Osmotic purgatives
Answer:

• Osmotic purgatives are solutes that are not absorbed in the intestine
• They retain water osmotically, increase the bulk of intestinal contents, distend bowel, and increase peristalsis to evacuate a fluid stool
• They include

1. Nonabsorbable salts- saline Purgatives

• Magnesium hydroxide
• Magnesium sulfate
• Sodium potassium tartrate
• Sodium sulfate
• Phosphate

2. Nonabsorbable sugars- lactulose

3. Polyethyleneglycol

Question 23. Mention two drugs used in noninfective diarrhea
Answer:

• Drugs used in noninfective diarrhea are:
  • Codeine
  • Diphenoxylate
  • Loperamide

Question 24. Loperamide
Answer:

• Loperamide is an opiate analog
• It is a potent constipating agent
• It has a poor water solubility
• Entry of it into the brain is negligible
• So no CNS effects occur
• It also inhibits GIT secretions
• Abdominal cramps and rashes are common adverse effects
• It is preferred for diarrhea

Question 25. Liquid paraffin
Answer:

Liquid paraffin Advantages

• Liquid paraffin is a viscous inert mineral oil
• It is a mixture of petroleum hydrocarbons
• It lubricates and softens feces
• It is taken for 2-3 days

Liquid paraffin  Disadvantages:

• Unpleasant to swallow
• Interferes with the absorption of fat-soluble vitamins
• Aspiration may cause lipoid pneumonia
• May leak out of the anus causing discomfort
• If absorbed in the intestines causes foreign body granulomas

Question 26. Saline purgatives
Answer:

• Saline Purgatives are nonabsorbable salts
• It includes
  • Magnesium hydroxide
  • Magnesium surface
  • Sodium potassium tartrate
  • Sodium sulfate
  • Phosphate
• They produce 1-2 fluid evacuations within 1-3 hours with mild cramping
• Causes nearly complete emptying of the bowel

Saline purgatives Uses:

• For the preparation of the bowel before surgery and colonoscopy
• In food/drug poisoning
• In the treatment of tapeworm infestations

Question 27. Anthraquinone preparations
Answer:

• Senna and Cascara sagrada are popular anthraquinone preparations
• They contain anthraquinone glycosides
• They are usually administered at bedtime to produce their effect in the morning
• They take 6-8 hours to act
• They are not absorbed in the small intestine
• They pass to the colon where bacteria liberate the active natural form which is later absorbed into the circulation

Anthraquinone preparations  Adverse Effects:

• Skin rashes
• Black pigmentation of colonic mucosa
• Discoloration of urine
• Cramps and excessive purging

Anthraquinone preparations  Contraindications:

• It is contraindicated in lactating mothers

Question 28. Hazards of use of purgatives
Answer:

• Regular use of purgatives may cause
  • Gastrointestinal disturbances
  • Irritable bowel syndrome
  • Loss of electrolytes
  • Loss of salts like calcium in stools
  • Malabsorption
  • Excessive dehydration may lead to death

Question 29. List two purgatives giving an indication for each.
Answer:

Question 30. Mechanism of action and two uses of Domperidone.
Answer:

Domperidone Mechanism of Action:

• It blocks the D₂ receptor in CTZ

Domperidone Uses:

• As an antiemetic – alternative to metoclopramide
• As pre-anesthetic medication – to reduce postoperative vomiting

Drugs And Cough And Bronchial Asthma Important Notes

1. Drugs used in bronchial asthma

• Bronchodilators
  • Sympathomimetics
    • Selective β2 agonists
  • Short-acting – salbutamol, Terbutaline
  • Longer acting – salmeterol
    • Non-selective agents – adrenaline, aminophylline
  • Methylxanthines – Heophylline, aminophylline
  • Anticholinergics – ipratropium bromide, atropine
• Anti-inflammatory
  • Systemic – glucocorticoids, hydrocortisone, prednisolone
  • Inhalational – beclomethasone, triamcinolone
• Mast cell stabilizer – disodium cromoglycate
• Leukotriene receptor antagonists – Montelukast
• Anti – IgE antibody – Omalizumab

2. Drugs causing bronchospasm

• ACE inhibitors
• Aspirin and other NSAIDs
• Beta-blockers
• Cholinergic drugs
• Bulk-forming laxatives
• Quinine
• Morphine

3. Ipratropium bromide

• It is an anticholinergic drug
• Produces slower response
• Used for regular prophylactic use

4. Mechanism of adrenergic as a bronchodilator

• Stimulation of β2 receptor
• Increased cAMP formation in bronchi muscle cells
• Relaxation of bronchi

5. Salbutamol

• It is β2 receptor agonist
• Safer than adrenaline and isoprenaline in the treatment of asthma
• Uses
  • In acute exacerbation of asthma
  • COPD
  • For short-term relief of bronchoconstrictor

Drugs And Cough And Bronchial Asthma Short Essays

Question 1. Mention two drugs used to suppress dry cough
Answer:

Drugs Used To Suppress Dry Cough:

1. Pharyngeal demulcents

• Lozenges
• Cough drops
• Glycerine

2. Expectorants

• Bronchial secretion enhancers
  • Sodium or potassium citrate
  • Potassium iodide
  • Balsum of tolu
• Mucolytic
  • Bromhexine
  • Acetylcysteine

3. Antitussives

• Opioids
  • Codeine
  • Pholcodine
• Non Opioids
  • Noscapine
  • Dextromethorphan
• Antihistamines
  • Chlorpheniramine
  • Diphenhydramine
  • Promethazine

4. Adjuvant Antitussives

• Bronchodilators- Salbutamol, terbutalin

Read And Learn More: Pharmacology Question and Answers

Question 2. Noscapine
Answer:

• Noscapine is a natural opium alkaloid
• It is a potent Antitussive
• It is highly effective and safe
• It may cause bronchoconstriction due to the release of histamine
• It acts by inhibiting the cough center In the medulla

Noscapine Use:

• Cough suppressant

Noscapine Adverse Effects:

• Nausea
• Headache

Noscapine Dose:

• 15-30 mg 6 hourly

Question 3. Disodium cromoglycate
Answer:

• Disodium cromoglycate is a synthetic derivative
• It belongs to a group of antiasthmatic drugs
• It is administered as an aerosol through metered dose inhaler

Disodium cromoglycate Mechanism of Action:

• Inhibits degranulation of mast cells
• Inhibits the release of inflammatory mediators
• Inhibits the release of cytokines
• Depresses neuronal reflexes

Disodium cromoglycate Adverse Effects:

• Throat irritation
• Cough
• Rarely bronchospasm and allergic reactions

Disodium cromoglycate Uses:

1. Prophylactic in bronchial asthma

• It is used for longer periods in mild to moderate asthma
• 2 puffs, 3-4 times daily

2. Allergic rhinitis

• Used as a nasal spray to produce symptomatic improvement

3. Allergic conjunctivitis

• Used as eyedrops
• 1-2 drops, 3-4 times daily

Question 4. Salbutamol
Answer:

• Salbutamol is a sympathomimetic drug
• It is fast acting bronchodilator
• The onset of action-1-5 min
• Duration of action- short

Salbutamol Actions:

• Bronchodilator
• Relaxation of the pregnant uterus
• Dilatation of blood vessels supplying the skeletal muscles
• Promote peptic glycogenolysis and uptake of potassium

Salbutamol Uses:

• In bronchial asthma- 100-200 meg every 6 hours through metered dose inhaler
• To delay premature labor
• In hyperkalemia

Salbutamol Adverse Effects:

• Tachycardia, palpitation
• Muscle tremors
• Tolerance
• Restlessness, nervousness
• Throat irritation
• Ankle edema
• Hyperglycaemia, hypokalaemia

Question 5. Pharmacotherapy of status asthmatics
Answer:

Treatment of status asthmaticus is as follows:

Question 6. Mention three groups of drugs used in bronchial asthma with an example.
Answer:

Drugs Used in Bronchial Asthma:

Question 7. Write the rationale for using any one drug for asthma.
Answer:

The Rationale of Using Sympathomimetic Drugs in Bronchial Asthma:

• Sympathomimetic drugs like adrenaline have the following mechanism

• It has a rapid onset and a short duration of action
• Hence it is used in acute asthmatic attacks as aerosol

Drugs And Cough And Bronchial Asthma Short Question And Answers

Question 1. Aminophylline
Answer:

• Aminophylline is one of the methylxanthines

Aminophylline Mechanism of Action:

• Enhances cAMP levels
• Causes bronchodilatation
• Inhibits the release of inflammatory mediators

Aminophylline Actions:

• CNS stimulant
• CVS stimulant
• Relaxes smooth muscles
• Mild diuretic
• Enhances secretion of acid and pepsin in the stomach
• Inhibits the release of inflammatory mediators

Aminophylline Uses:

• Bronchial asthma and COPD
• Apnea in the premature infant

Aminophylline Adverse Effects:

• Dyspepsia, vomiting, nervousness, tremor, delirium, hypotension, arrhythmia, and convulsions

Question 2. Nasal decongestants.
Answer:

• Nasal decongestants stimulate the alpha receptors and cause vasoconstriction in the nasal mucous membrane and relieve nasal congestion

Drugs Used As Nasal Decongestants:

• Naphazoline
• Pseudoephedrine
• Phenylephrine
• Imidazole

Nasal decongestants Use:

• Allergic rhinitis
• Common cold
• Sinusitis

Nasal decongestants Adverse Effects:

• Atrophic rhinitis
• Anosmia
• Local irritation

Question 3. The rationale for using Salbutamol in bronchial asthma
Answer:

• Salbutamol is used in asthma to reduce cardiac side effects
• Inhaled Salbutamol produces bronchodilatation within 5 min
• Its action lasts for 2-4 hours
• It is the most effective, convenient, and relatively safe
• Hence it is used to terminate the attacks of asthma.

Question 4. Beclomethasone
Answer:

• Beclomethasone is long acting glucocorticoid

Beclomethasone Mechanism of Action:

• Suppresses inflammatory response to antigen-antibody reaction
• Reduces mucosal edema and hyper irritability

Beclomethasone Uses:

• Prophylactic use to prevent acute attacks of asthma
• Prevent bronchial hypersensitivity
• Controls the symptoms

Beclomethasone Available As:

• Nasal spray- For allergic rhinitis
• Ointment- For skin and mucous membrane

Beclomethasone Dose:

• Beclate inhaler- 50,100,200 microgram
• Metered dose-1-2 puffs 3-4 times a day

Beclomethasone Adverse Effects:

• Hoarseness of voice
• Sore throat
• Oropharyngeal Candidiasis

Question 5. Ipratropium.
Answer:

• It is a semi-synthetic anticholinergic drug
• Given by inhalation

Ipratropium Uses:

• Bronchial asthma
• COPD
• Inhaled ipratropium – used as a prophylactic agent
• Nebulized ipratropium mixed with salbutamol – used in refractory asthma

Question 5. Name four bronchodilators.
Answer:

• Sympathomimetics – adrenaline, isoprenaline, salbutamol
• Methyl xanthine – theophylline, aminophylline
• Anticholinergic – ipratropium bromide, tiotropium bromide

Anti Cancer Drugs Important Notes

1. Methotrexate

• It is the folic acid antagonist
• Has antineoplastic activity
• Extensively used as a chemotherapeutic agent

Anti Cancer Drugs Short Essays

Question 1. Toxic effects of alkylating agents.
Answer:

Alkylating agents produce highly reactive carbonium ion intermediates which transfer alkyl groups to cellular macromolecules by forming covalent bonds.
They are:

1. Nitrogen mustards.

• Cyclophosphamide
• Ifosfamide.
• Chlorambucil.
• Melphalan.

2. Alkyl sulfonate-busulfan.

3. Nitrosoureas – lomustine.

4. Triazine – dacarbazine.

Toxic effects of alkylating agents:

1. Bone marrow depression.

• It results in granulocytopenia, agranulocytosis, thrombocytopenia, and aplastic anemia.

2. Immunosuppression.

• Lymphocytopenia and inhibition of lymphocyte function result in suppression of immunity.

3. GIT disturbances.

• Stomatitis, diarrhea, shedding of mucosa, and hemorrhages occur.
• Nausea and vomiting are prominent

4. Skin and hair.

• Alopecia – loss of hair and dermatitis occurs.

5. Gonads.

• Inhibition of gonadal cells causes.
  • Oligozoospermia and impotence – in males.
  • Inhibition of ovulation and amenorrhoea in females.

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6. Foetus.

• Damages foetus.
• Leads to abortion, fetal death, and teratogenesis.

7. Carcinogenicity.

• Secondary cancers appear frequently due to immunosuppression.

8. Hyperuricaemia.

• Massive cell destruction produces uric acid.
• Gout and urate stones in the urinary tract may develop.

Question 2. Vinca alkaloids.
Answer:

• Vinca alkaloids are spindle poison.
• They are mitotic inhibitors.

Vinca alkaloids Mechanism of action:

Vinca alkaloids: are

• Vincristine
• Vinblastine
• Vinorelbine.

Question 3. Two antimetabolites are used in cancer therapy.
Answer:

Antimetabolites are analogs related to the normal components of DNA. Involved in nucleic acid synthesis.

• They competitively inhibit the utilization of normal substrate.

1. Folate antagonist – methotrexate.

Folate antagonist- methotrexate Action:

• Cytotoxic actions on bone marrow, skin, gastrointestinal m synthesis.

Folate antagonist- methotrexate Uses:

• Choriocarcinoma.
• Acute leukemia.
• Carcinoma of tongue/pharynx/lung.
• Rheumatoid arthritis.
• Psoriasis.
• Organ transplantation.

Folate antagonist- methotrexate Treatment of toxicity:

• Methotrexate toxicity is treated with folinic acid.
• It reverses the effects of methotrexate.

2. Purine antagonists – mercaptopurine.

Treatment of toxicity mercaptopurine Mechanism of action:

Treatment of toxicity Uses:

• Acute leukemia in children.
• Choriocarcinoma.
• Some solid tumors.

Treatment of toxicity Adverse effects:

• Bone marrow depression.
• Anorexia.
• Nausea, vomiting.
• Stomatitis.
• Jaundice.
• Dermatitis.

Question 4. Methods to ameliorate the toxicity of anticancer drugs.
Answer:

Question 5. Methotrexate.
Answer:

• It is an anticancer drug
• It is a folate antagonist

Methotrexate Mechanism:

• Binds to dihydrofolate reductase
• Prevents the formation of tetrahydrofolate

Methotrexate Action:

• Cytotoxic actions on bone marrow, skin, GIT, and synthesis

Methotrexate Dose:

• Initial 7.5 mg once weekly
• Increased by 2.5 mg weekly
• Maximum weekly dose – 30 mg

Methotrexate Uses:

• Choriocarcinoma
• Acute leukemia
• Carcinoma of tongue/ pharynx/ lung
• Rheumatoid arthritis
• Psoriasis
• Organ transplantation

Methotrexate Adverse Effects:

• Nausea
• Vomiting
• Mucosal ulcers
• Hepatotoxicity
• Treatment of Toxicity:
• Methotrexate toxicity is treated with folinic acid
• It reverses the effects of methotrexate

Anti Cancer Drugs Short Question And Answers

Question 1. Nitrogen mustards.
Answer:

Nitrogen mustards are alkylating agents.

Question 2. Name antibiotics used in cancer therapy.
Answer:

Antibiotics used in cancer therapy are.

1. Actinomycin D.
2. Daunorubicin.
3. Doxorubicin.
4. Bleomycin.

Question 3. Name vinca alkaloids.
Answer:

Vinca alkaloids are mitotic inhibitors.

• They are.

1. Vincristine
2. Vinblastine
3. Vinorelbine.

Question 4. Antimetabolites.
Answer:

Antimetabolites are analogs related to the normal components of DNA involved in nucleic acid synthesis.

They are:

1. Folate antagonist.

• Methotrexate.

2. Purine antagonist

• Mercaptopurine.
• Thioguanine.
• Azathioprine.

3. Pyrimidine antagonists.

• Fluorouracil.
• Cytarabine.

Question 5. Cyclophosphamide.
Answer:

• Cyclophosphamide is an alkylating agent
• It is converted to its active metabolite aldophosphamide in the body.
• It is more effective on B cells than T cells.

Cyclophosphamide Uses:

• Bone marrow transplantation.
• Hodgkin’s lymphoma.
• Leukemia.
• Maintenance therapy in pemphigus, systemic lupus erythematosus, and idiopathic thrombocytopenic purpura.

Cyclophosphamide Toxic effects:

• It causes cystitis due to its active metabolite caroline.
• Prevent by.

1. IV mesna.
2. Irrigating bladder with acetylcysteine.
3. Intake of excessive fluids.

Question 6. Oxythiamine.
Answer:

• It is an irreversible inhibitor of transketolase
• It is an antivitamin derivative of thiamine which after phosphorylation to oxy thiamine pyrophosphate can bind to the active centers of thiamine-dependent enzymes

Oxythiamine Action:

• It is analog to antimetabolite
• Suppresses the nonoxidative synthesis of ribose
• Induces cell apoptosis

Oxythiamine Mechanism of Action:

Inhibits transketolase
↓
Suppresses pentose phosphate pathway
↓
Interrupts the synthesis of coenzymes, RNA, and DNA in
cancer cells

Anti Helminitics Short Essays

Question 1. Treatment of hookworm infestations.
Answer:

Hookworm infections are more common in developing countries.

• It is seen in people with poor hygiene.
• It is caused by ancylostoma duodenale and necator americanus.

Hookworm infections Drugs used:

• Mebendazole and albendazole are used in hookworm infections.

1. Mebendazole:

• It is broad spectrum antihelmintic.
• Bioavailability-20 %.
• Given orally 100 mg BD for 3 days.

Mebendazole Mechanism of action:

• Binds to b-tubulin with high affinity
• Inhibits glucose uptake in parasites

Mebendazole Uses:

• Hookworm infections.
• Roundworm infections.
• Trichuriasis.
• Trichinella spiralis.
• Hydatid disease.

Read And Learn More: Pharmacology Question and Answers

Mebendazole Adverse effects:

• Nausea, diarrhea, abdominal pain.
• Prolonged use causes headaches, fever, alopecia, jaundice, and neutropenia.

2. Albendazole:

• It is congener of mebendazole.
• Absorption is Moderate.
• It is widely distributed in the body.

Albendazole Uses:

• Trichuriasis.
• Trichinosis.
• Tapeworms and strongyloidosis.
• Neurocysticercosis.
• Hydatid disease.
• Filariasis.

Albendazole Adverse effects:

• Nausea, diarrhea, abdominal pain.
• Prolonged Use Causes Headache, Fever, Alopecia, Jaundice And Neutropenia.

Anti Helminitics Short Question And Answers

Question 1. Advantages of albendazole over mebendazole.
Answer:

• Albendazole is well tolerated.
• Effective in a single dose
• Superior to mebendazole in hookworm infections.
• The active metabolite of albendazole achieves a higher concentration than mebendazole.
• It also has some activity against T. vaginalis, giardia, lamblia, and Wuchereria bancrofti.

Question 2. Peprlzine citrate.
Answer:

Paperizine citrate is narrow-spectrum antihelmintic.

Peprlzine citrate Mechanism:

Peprlzine citrate Uses:

• Roundworm infestation.
• Pinworm infestations.

Peprlzine citrate Adverse effects:

• Nausea, vomiting, abdominal discomfort, urticaria.
• At high doses-dizziness, excitement.
• At toxic doses – produces – convulsions.

Question 3. Uses and adverse effects of Albendazole.
Answer:

Albendazole Uses:

• Ascaris
• Hookworm infections
• Trichuriasis
• Tapeworm and strongyloidiasis
• Neurocysticercosis
• Hydatid disease
• Filariasis

Albendazole Adverse effects:

• Nausea, diarrhea, abdominal pain
• Prolonged use causes a headache, fever, alopecia, jaundice, and neutropenia

Anti Fungal Drugs Important Notes

1. Antifungal drugs

• Topically applied
  • Nystatin
  • Trichomycin
• Systemically employed
  • Griseofulvin
  • Amphotericin B
  • Ketoconazole
  • Fluconazole
  • Miconazole

2. Nystatin- 5 lakh units are used in the treatment of

• Local candidiasis of the mouth, skin, vagina, and gut

Read And Learn More: Pharmacology Question and Answers

3. Griseofulvin

• It is used to treat ringworm infections of the scalp, groin, and feet and fungal infections of the nails
• It causes antabuse like action in the presence of alcohol

4. Ketoconazole

• It produces serious hepatotoxicity.
• Contraindicated in pregnancy
• Maximum endocrinal side effects are seen

Anti Fungal Drugs Short Essays

Question 1. Antifungal drugs
Answer:

Antifungal drugs are drugs used for superficial and deep fungal infections.

Antifungal drugs Classification:

1. Antibiotics:

• Polyenes – amphotericin B, nystatin, natamycin.
• Heterocyclic benzofuran – griseofulvin.

2. Antimetaboljte – flucytosine.

3. Azoles.

• Imidazoles – clotrimazole, econazole.
• Triazoles – fluconazole, itraconazole.

4. Alkylamine – terbinafine.

5. Topical agents.

• Tolnaftate, undecylenic acid, Benzoic acid, butenafine, sod. Thiosulfate.

Antifungal drugs Site of action:

• Antifungal drugs may act on
  • Fungal cell wall
  • Cell membrane
  • On the nucleus

Question 2. Amphotericin B.
Answer:

• Amphotericin B is a polyene antifungal agent
• It is obtained from streptomyces nodosus.

Antifungal spectrum:

• Amphotericin B is active against a wide range of yeast and fungi.
• It is fungicidal at high and fungi-static at low concentrations.

Antifungal spectrum Mechanism of action:

Antifungal spectrum Adverse effects:

1. Acute reactions:

• Fever, chills, aches, pain.
• Nausea, vomiting, dyspnoea.
• Thrombophlebitis of the injected vein.

2. Long-term toxicity.

• Nephrotoxicity – reduced GFR, acidosis, hypo-kalaemia, inability to concentrate urine.
• Neurotoxicity.
• Anaemia due to decreased production of erythropoietin and bone marrow depression.

Antifungal Spectrum Uses:

• Amphotericin B-used topically for oral, vaginal, and cutaneous candidiasis and otomycosis.
• To prevent relapse of cryptococcosis and histoplasmosis in patients with AIDS.
• Leishmaniasis.
• Orally in fungal infections of the gut.

Question 3. Griseofulvin.
Answer:

• Griseofulvin is antifungal antibiotic.
• It is fungistatic.
• It is derived from penicillium griseofulvum.

Griseofulvin Mechanism of action:

Griseofulvin Uses:

• It is used orally in superficial dermatophytosis
• Dose – 1 g daily.
• Duration of treatment – varies from 3 weeks to 1 year.

Griseofulvin Adverse effects:

• Headache.
• Git disturbances.
• Neurotoxicity – peripheral neuritis.
• Allergic reactions.
• Hepatitis.

Question 4. Ketoconazole.
Answer:

• It is the first orally effective broad-spectrum antifungal drug
• It is more soluble at lower pH in the blood
• Food and low gastric pH enhance its absorption
• In blood, it is largely bound to albumin and RBC
• Metabolites are excreted in urine and feces
• Plasma half-life -1 %-6 hours
• Penetration into CSF is poor

Ketoconazole Uses:

• Dermatophytosis
• Superficial candidiasis
• Deep mycosis
• High doses have been used in Cushing’s syndrome

Ketoconazole Adverse Effects:

• Nausea, vomiting, gastric irritation, loss of apatite
• Headache, paraesthesia
• Rashes
• Hair loss
• Allergic reaction
• Decreases androgen production – Gynaecomastia, loss of libido, azoospermia, menstrual irregularities

Ketoconazole Drug Interactions:

• H2 blockers. Proton pump inhibitors and antacids – decrease the oral absorption of ketoconazole
• Rifampicin, phenobarbitone, carbazepine and phenytoin – induces ketoconazole metabolism and reduces its efficacy

Anti Fungal Drugs Short Question And Answers

Question 1. Name two broad-spectrum antifungal drugs.
Answer:

Broad-spectrum antifungal drugs are used against a large variety of fungi and yeasts like C. Albican, H. Capsulation, and Cryptococcus. Neoformans, Blastomyces dermatitis, coccidiosis immits, coreopsis, rhodotorula, aspergillus, deep mycosis, trichophyton.

• They are:

1. Polyenes – amphotericin – B, nystatin, natamycin.
2. Heterocyclic benzofuran – griseofulvin.

Question 2. Amphotericin B.
Answer:

• Nystatin is a polyene antifungal agent
• It is obtained from the streptomyces course
• It is not absorbed when given orally, so used topically.

Amphotericin B Uses:

1. Local candidiasis

• 5 ml oral suspension should be swished in the mouth and then swallowed 4 times a day.

2. Vaginal candidiasis.

• 1 lac unit tab inserted twice daily.

3. Used as an ointment for corneal, conjunctival, and cutaneous candidiasis.

Amphotericin B Adverse effects:

• Bitter foul taste
• Nausea.

Question 4. Griseofulvin.
Answer.

Griseofulvin Uses:

• Dermatophytosis
• Superficial candidiasis
• Deep mycosis
• High doses have been used in Cushing’s syndrome

Griseofulvin Adverse Effects:

• Nausea, vomiting, gastric irritation, loss of apatite
• Headache, paraesthesia
• Rashes
• Hair loss
• Allergic reaction
• Decreases androgen production – Gynaecomastia, loss of libido, azoospermia, menstrual irregularities

Question 5. Ketoconazole.
Answer:

• Ketoconazole is the first orally effective broad-spectrum antifungal drug.
• It is more soluble at lower pH in the blood.
• Metabolites are excreted in urine and feces.
• Plasma t ½ varies from 1½ to 6 hours.

Ketoconazole Uses:

• Dermatophytosis.
• Superficial candidiasis.
• Deep mycosis.

Ketoconazole Adverse effects:

• Nausea, vomiting, gastric irritation, loss of appetite.
• Headache, paresthesia.
• Rashes, hair loss.
• Allergic reactions.
• Decreases androgen production – gynecomastia, loss of libido, azoospermia, menstrual irregularities.

Chemotherapy Of Tuberculosis and Leprosy Important Notes

1. Anti-tuberculous drugs

• First-line drugs are highly effective with low toxicity
• Second-line drugs have low efficacy with high toxicity

2. Drug regimen for tuberculosis

• INH 300 mg + Rifampicin 600 mg + Pyrazinamide 2 g or Ethambutol 15 mg/kg taken daily for 2 months
• Followed by INH 300 mg + Rifampicin 600 mg daily for 4 months

Chemotherapy of Tuberculosis

3. Peripheral neuritis

• It is caused by isoniazid
• Can be prevented by taking pyridoxine 10 mg/day prophylactically
• Can be treated by taking pyridoxine 100 mg/day
• Drugs causing peripheral neuritis are:
  • Griseofulvin
  • Nitrofurantoin.
  • Vincristine

4. Lepra reaction

• It is seen in lepromatous chemotherapy
• Occurs due to the release of antigens from bacilli
• Drugs used to control it are:
  • Clofazimine
  • Chloroquine
  • Thalidomide

Chemotherapy Of Tuberculosis and Leprosy Long Essays

Question 1. Classify drugs used in tuberculosis. Write the pharmacology of any two commonly used drugs.
Answer:

Tuberculosis:

• Tuberculosis is a chronic granulomatous disease.

Tuberculosis Anti-tubercular drugs:

• According to their clinical utility, the anti-tuberculosis drugs are divided into.

1. First-line drugs.

• They have high antitubercular efficacy.
• Have low toxicity.
• They are:
  1. Isoniazid (H)
  2. Rifampicin (R)
  3. Pyrazinamide (Z)
  4. Ethambutol (E)
  5. Streptomycin (S)

2. Second-line drugs.

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• They have low antitubercular efficacy.
• Have high toxicity.
• They are:
  1. Thiacetone (Tzn)
  2. Para-aminosalicylic acid (PAS)
  3. Ethionamide (Etm)
  4. Kanamycin (Kmc)
  5. Amikacin (Am)
• Newer drugs are:
• Ciprofloxacin, ofloxacin, clarithromycin, azithromycin.

Chemotherapy of Tuberculosis

Isoniazid: (INH):

• It is the most effective and cheapest primary antitubercular drug.
• It is effective against both intra and extracellular organisms.

Isoniazid Mechanism of action:

Isoniazid Pharmacokinetics:

• Completely absorbed orally.
• Penetrates all tissues.
• Metabolized by acetylation.
• Metabolites are excreted in the urine.

Isoniazid Adverse effects:

1. Peripheral neuritis.

• Occurs due to increased excretion of pyridoxine.
• Characterized by paraesthesia, numbness, mental disturbances, and convulsions.
• Avoided by prophylactic uses of pyridoxine with INH.

2. Hepatitis.

• Occurs due to dose-related damage to liver cells.
• More common in alcoholics and elders.

3. CNS effects – psychosis, seizures.

4. Hemolysis. In GePD deficiency patients.

5. Other effects.

• Anorexia, GIT disturbances, fever, rashes, acne, arthralgia.

Chemotherapy of Tuberculosis

Rifampicin:

• It is a semisynthetic derivative of rifamycin B.
• It is highly effective.
• Acts on both intracellular and extracellular organisms.

Rifampicin Mechanism of action:

Rifampicin Pharmacokinetics:

• Well-absorbed orally.
• Has good tissue penetrability.
• Metabolized in the liver, excreted in bile.
• It is a microsomal enzyme inducer.
• Appears in saliva, tears, and sweat.

Rifampicin Adverse effects:

1. Hepatotoxicity.

• Causes hepatitis in patients With pre-existing liver disease.

2. Respiratory syndrome.

• Breathlessness, shock, collapse.

3. Purpura, hemolysis, renal failure.

4. GIT disturbances.

• Epigastric distress, nausea, Vomiting, Abdominal cramps, diarrhea.

5. Flu-hike synthesis drome.

• Fever, body ache, chills; hemolytic anemia.

6. CNS effects.

• Headache, drowsiness, dizziness ataxia.

7. Cutaneous syndrome.

• Flushing, pruritis, rash, redness, watering of eyes.

Rifampicin Other Uses:

• Leprosy.
• Prophylaxis Of H.influenza And Meningitis.
• Resistantstephylococcal infections.
• Brucellosis.
• To eradicate the nasal carrier state of meningitis.

Chemotherapy Of Tuberculosis and Leprosy Short Essays

Question 1. DOTS chemotherapy in tuberculosis.
Answer:

• DOTS in directly observed treatment short course.
• It was recommended by WHO in 1995.
• It is found to be effective.
• It involves providing the most effective medicine and confirming that it is taken.
• Antitubercular drugs during the intensive phase are administered under the direct supervision of peripheral health staff or through voluntary workers.
• It ensures a high cure rate through its following components.

1. Appropriate medical treatment.
2. Supervision and Motivation by health and non-health workers.
3. Monitoring of disease status by health services.

DOTS chemotherapy in tuberculosis Category:

• According to DOTS, patients are grouped into two categories

1. Category -1 – new patients

• New sputum smear positive.
• New sputum smear negative.
• New extrapulmonary.
• New others.

2. Category – II – previously treated patients.

• Smear positive relapse.
• Smear positive failure.
• SmeOr positive treatment after default.

Question 2. Mention six drugs for tuberculosis.
Answer:

1. First-line drugs.

• Isoniazid.
• Rifampicin
• Pyrazinamide
• Streptomycin.

2. Second-line drugs

• Thiacetazoue.
• Paia-aminosalicylic acid
• Ethionamide
• Cycloserine
• Kanamycin
• Amikacin

3. Newer Drugs.

• Ciprofloxacin.
• Ofloxacin.
• Clarithromycin.
• Azithromycin.
• Rifabutin.

Question 3. Explain why multidrug therapy is used in the treatment of tuberculosis.
Answer:

Tuberculosis is one of the most difficult infections to curve.

• Its treatment is problematic due to

1. Slow division of mycobacteria.
2. Development of resistance.
3. Ability to remain as persisters for years.
4. Intracellular location of barley.
5. Presence of caseous material.
6. Long term therapy
7. Expensive treatment
8. Drug toxicity.
9. Drug toxicity.

Tuberculosis Aim of treatment:

1. Kill dividing bacilli – to make sputum negative
2. To destroy persisters – to prevent relapse.

Tuberculosis Combination of Drugs:

• Drugs are combined to

1. Delay development of resistance.
2. Reduce toxicity.
3. Shorten the course of treatment

Chemotherapy of Tuberculosis

Question 4. Dapsone (DDS).
Answer:

• Dapsone is diamino diphenyl sulfone (DDS)
• It is a simple, old, cheap, and active antileprotic drug.

Dapsone Mechanism of action:

• Dapsone is chemically related to sulphonamide.
• It is a structural analog of PABA.
• It competitively inhibits bacterial folate synthetase.
• It also inhibits the union of PABA with pteridine residue to form dihydropetroic acid.

Dapsone Pharmacokinetics:

• Dapsone is completely absorbed orally.
• It is widely distributed.
• It is metabolized in the liver and excreted in bile.
• It is acetylated.
• It is leprostatic.

Dapsone Uses:

• Leprosy – a primary drug for leprosy.
• Used in combination with pyrimethamine for chloroquine-resistant malaria.
• Dermatitis is herpetiform.
• Used along with trimethoprim in P.jiroveci infections in patients with AIDS.

Question 5. Treatment schedule for leprosy.
Answer:

• Treated by multidrug therapy regime introduced by WHO in 1981.
• Drugs used are dapsone, rifampicin, and clofazime.
• All are administered orally.

Leprosy Duration:

• 2- years – for multibacillary/infectious leprosy.
• 6 months – for paucibacillary/non-infectious leprosy.

Leprosy Schedule:

Leprosy Alternative regimen:

1. Clofazimine 50 mg with any two newer drugs daily for 6 months.

• Followed by clofazimine 50 mg with anyone new drug daily for 18 months.

2. In single lesion paucibacillary leprosy,

• Single dose of
  • Rifampicin – 600mg.
  • Ofloxacin-400 mg.
  • Minocycline – 100 mg.

Chemotherapy of Tuberculosis

Question 6. Lepra reactions.
Answer:

Lepra reactions are immunologically-mediated reactions that occur during the course of the disease.

Types:

1. Type I reaction – reversal reaction.

• Seen in tuberculoid leprosy.
• They are cell-mediated, delayed hypersensitivity reactions.
• Characterized by cutaneous ulceration, multiple nerve involvement with pain and tenderness.

Type I reaction – reversal reaction Treatment:

• Treated with corticosteroids or clofazimine.

2. Type II reactions – lepra reaction.

• Seen in lepromatous leprosy.
• It is Jarischherxheimertypeofireaction.
• It is a type III hypersensitivity reaction due to the release of antigens from killed bacilli.
• It is abrupt in onset.
• Old lesion – enlarges, becomes red, swollen, and painful.
• New lesions also appear.
• Fever, malaise, lymphadenitis, myositis, and neuralgia occur.

Type II reactions – lepra reaction Treatment:

• Temporary discontinuation of dapsone in severe cases.
• Administration of analgesics, antipyretics, and antibiotics.
• Clofazimine – 200 mg daily in most severe cases.
• Corticosteroids are used in severe cases.

Chemotherapy Of Tuberculosis And Leprosy Short Question And Answers

Question 1. Adverse effects of rifampicin.
Answer:

• Hepatitis.
• Respiratory syndrome.
• Purpura, hemolysis, shock, renal failure.
• Cutaneous syndrome.
• Flu-like syndrome.
• GIT disturbances.
• Staining of secretions.
• Hypersensitivity reactions.

Question 2. Pyridoxine should be administered with INH.
Answer:

• Isoniazid (INH) is anti-tubercular drug.
• It causes peripheral neuritis due to interference with utilization and increased excretion of pyridoxine.
• It is characterized by paresthesia, numbness, mental disturbances, and convulsions.
• It is avoided by prophylactic use of pyridoxine 10-50 mg.
• Hence, pyridoxine should be administered with INH to prevent peripheral neuritis.

Question 3. Streptomycin.
Answer:

• Streptomycin is an anti-tuberCuter drug.
• It is tuberculocidal.
• It acts only against extracellular organisms.
• It does not cross CSF.
• When used alone resistance develops rapidly.

Streptomycin Disadvantages:

• The rapid development of resistance.
• Has to be given IM.
• Causes ototoxicity and nephrotoxicity.
• Thus, streptomycin is the least preferred.

Chemotherapy of Tuberculosis

Question 4. Pyrazinamide.
Answer:

• Pyrazinamide is tuberculocidal.
• It is more active at acidic pH.
• Has good sterilizing activity.
• Highly effective during the first 2 months of therapy.
• It is well-absorbed orally.
• Metabolized in the liver, excreted in urine.

Pyrazinamide Adverse effects:

• Hepatotoxicity.
• Hyperuricaemia.
• Arthralgia.
• Anorexia, vomiting.
• Rashes.
• Fever, flushing.
• Loss of diabetes control.

Question 5. Isoniazid acetylation status in tuberculosis chemotherapy.
Answer:

• Isoniazid is metabolized by acetylation.
• Depending on the genetic variations, patients can be fast or slow acetylation.

• metabolites are excreted in the urine.

Question 6. Drugs used in the treatment of leprosy.
Answer:

1. Sulfone-dapsone.
2. Phenazine derivative – clofazimine.
3. Antitubercular drugs – rifampin, ethionamide.
4. Other antibiotics-Oflaxacin, minocycline.

Question 7. Dapsone.
Answer:

• Dapsopne is diamino dlpheyl sulfone (DDS).
• It is a simple, cheap, old, and more active anti-leprotic drug.

Question 8. Treatment of lepra reactions.
Answer:

Antiviral Drugs Important Notes

1. Antiviral drugs

• Amantadine
• Acyclovir
• Vidarabine
• Zidovudine
• Idoxuridine

2. Classification of anti-retroviral drugs

• Nucleoside reverse transcriptase inhibitors
  • Zidovudine
  • Didanosine
  • Lamivudine
• Non-nucleoside reverse transcriptase inhibitors
  • Nevirapine
  • Efavirenz
• Protease inhibitors
  • Ritonavir
  • Saquinavir

3. Acyclovir

• It is available as IV, oral and topical application
• Used in the treatment of
  • Genital herpes
  • Herpes zoster infection

4. Zidovudine and Didanosine

• Used in the treatment of AIDS
• They block the action of reverse transcriptase in HIV infection 5

Antiviral Drugs Short Essays

Question 1. Antiviral drugs.
Answer:

Viruses are intracellular parasites which depend on the host cells for their food, growth and multiplication.

• Antiviral drugs interfere with the steps of the viral reproduction cycle within host cells.

Antiviral drugs Classification:

1. Anti-herpesvirus.

• Idoxuridine, acyclovir, valacyclovir.

2. Anti-retrovirus.

• Nucleoside reverse transcriptase inhibitors.
  • Zidovudine, Didanosie, abacavir
• Non-nucleoside reverse transcriptase inhibitors.
  • Nevirapine, efavirenz.
• Protease inhibitors.
  • Ritonavir, indinavir, nelfinavir.

Read And Learn More: Pharmacology Question and Answers

3. Anti-influenza virus.

• Amantadine, rimantadine.

4. Nonselective antiviral drugs.

• Ribavirin, lamivudine.

Antiviral Drugs Short Question And Answers

Question 1. Acyclovir.
Answer:

Acyclovir is antiviral agent.

The spectrum of activity:

• Herpes simplex virus – type 1 and type 2.
• Varicella zoster virus.
• Epstein – Barr virus.

Mechanism of action:

Acyclovir Uses:

• Mucocutaneous herpes simplex – type I
• Genital herpes.
• H. Simplex encephalitis.
• H. Simplex keratitis.
• Herpes zoster.
• Chickenpox.

Acyclovir Adverse effects:

1. Oral use.

• Headache, nausea, malaise, diarrhoea.

2. Topical use.

• Stinging and burning sensation.

3. Intravenous use.

• Rashes, sweating, emesis, fall in BP

Question 2. Zidovueline.
Answer:

• It is the first drug to be used in the treatment of HIV infection.

Zidovueline Mechanism of Action:

Zidovueline Uses:

• Used in HIV – infected patients along with other antiretroviral drugs.
• Its effects are
  • Reduces HIV – RNA titre.
  • Increases CD4 count
  • Improves immune status.
  • Reduces chances of opportunistic infections.

Zidovueline Adverse effects:

• Bone marrow depression – anaemia neutropenia.
• Headache.
• Nausea.
• Myalgia, fatigue.
• Insomnia.
• Myopathy.
• Neurotoxicity.

Question 3. Mention the drugs used in Typhoid fever.
Answer:

• First choice of drugs
  • Ciprofloxacin
  • Ceftriaxone
• Alternative drugs
  • Chloramphenicol
  • Ampicillin
  • Cotrimoxazole