Kristensmith

Local Anaesthesia Important Notes

Local Anaesthesia Classification:

1. Based on the Site of Action:

• Class A: Agents acting on the Exampleternal surface of the membrane: Example- Biotoxins
• Class B: Agents acting on the internal surface of the membrane. Example- Quaternary ammonium compounds
• Class C- Agents acting by independent mechanism- Example- Benzocaine
• Class D- Agents acting by combination mechanisms- Example- Articaine, Bupivacaine

2. Based On Group of Drugs:

• ESTERS

Esters of Benzoic Acids:

• • Butacaine
  • Cocaine
  • HExampleylcaine
  • Tetracaine

Esters of Paraamino Acids:

B Pharmacy Important Questions

• • Chloroquine
  • Procaine
• AMIDES
  • Atricaine
  • Bupivacaine
  • Etidocaine
• Quinolone- Centbucridine

Local Anaesthesia Parts:

• Aromatic lipophilic group
• Hydrophilic amino group
• An intermediate chain

Local Anaesthesia Biotransformation:

• Ester group – hydrolysis by plasma cholinesterases
• Amide group – hydrolysis and hydroxylation by microsomal enzymes of the liver

Local Anaesthesia Safe dose:

• A safe dose of 2% lignocaine is
  • 4.5 mg/kg or 300 mg without vasoconstrictor
  • 7 mg/kg or 500 mg with vasoconstrictor
• Safely dose of adrenaline for dental use
  • In normal patients – 0.2 mg
  • For cardiac patients – 0,04 mg

Safe dose Actions:

B Pharmacy Important Questions

• Anaesthesia of smaller nerve fibres
• Stimulation of CNS
• Produces vasodilatation
• Produces depressant effect on the myocardium

Read And Learn More: Pharmacology Question and Answers

Local Anaesthesia Adverse drug reactions:

• Intolerance
• Cardiovascular depression
• CNS stimulation
• CNS depression
• Malignant hyperpyrExampleia

Local Anaesthesia Uses:

• Surface anaesthesia – for pain due to burns, ulcers and fissures
• Infiltration anaesthesia
• Nerve block anaesthesia
• Spinal anaesthesia
• Systemic use for anti-arrhythmic effect

B Pharmacy Important Questions Local Anaesthesia Long Essays

Question 1. Classify local anaesthetics and write in detail about xylocaine/lignocaine.

Answer:

Local Anaesthetics:

Local anaesthetics are drugs which cause a reversible loss of sensation in the restricted area of the body either by depression in the Excitation of conducting nerves or suppression of Examplecitation of peripheral nerves.

Local Anaesthetics Classification:

1. Based on chemical structure.

• Amides – Lignocaine, mepivacaine.
• Esters.
  • Esters of benzoic acid – Butaaine, cocaine.
  • Esters of para-aminobenzoic acid – chloride- caine.
• Quinolones – Centbucridine.

2. Based on the duration of action.

• Injectable anaesthetics.
  • Low potency and short duration,
    • Procaine, chlorprocain.
  • Intermediate potency and duration.
    • Lignocaine and prilocaine.
  • High potency and long duration.
    • Tetracaine, bupivacaine.
• Surface anaesthetic.
  • Soluble – cocaine, lignocaine, tetracaine.
  • Insoluble – benzocaine, tetracaine.

3. Based on biological site and mode of action.

• Class A
  • Agents acting at receptor site on Exampleternal surface of nerve membrane.
    • Example: biotoxin.
• Class B.
  • Agents act at receptor sites on the internal surface of the nerve membrane.
    • Example: quaternary ammonium compounds.
• Class C.
  • Agents act by a receptor-independent physical-chemical mechanism.
    • Example: Benzocaine.
• Class D.
  • Agents act by a combination of receptor and receptor-independent mechanisms.
    • Examples: Atricaine, lidocaine, mepivacaine.

B Pharmacy Important Questions Local Anaesthetics Mechanism of Action:

Displacement of calcium ions from sodium channel receptor site which permits.
↓
The binding of the LA molecule to this site produces.
↓
Blockade of the sodium channel and decrease in sodium conductance.
↓
Leads to depression in the rate of electrical depolarization.
↓
Failure to achieve the threshold potential level along with.
↓
Lack of development of propagated action potential called.
↓
Conduction Blockade

Xylocaine/Llgnocaine:

• It is the most widely used local anaesthesia.
• It is fast and long-lasting.
• It blocks nerve conduction within 3 min.

B Pharmacy Important Questions Xylocaine/Llgnocaine Actions:

1. Local actions:

• Blocks sensory nerve endings, nerve trunk, neuromuscular junction, ganglionic synapse and receptors.
• Reduces the release of acetylcholine.
• Causes anaesthesia of the skin and paralysis of voluntary muscles.

2. Systemic actions.

• CNS [Central Nervous System]
  • Produces stimulation followed by depression.
  • Causes blood-brain barrier (BBB).
  • Depresses cortical inhibitory pathway.
• Cardiovascular system (CVS).
  • Lignocaine decreases Examplecitability, conduction rate and force of contraction.
  • Causes hypotension due to vasodilatation and myocardial depression.
• Smooth muscles
  • Depresses contraction of intact bowel.

Xylocaine/Llgnocaine Uses:

1. Anaesthesia.

• Used in all types of anaesthesia.

2. Anti-arrhythmia.

Xylocaine/Llgnocaine Adverse Effects:

1. CNS effects.

• Drowsiness, mental clouding, altered tastes, tinnitus.

2. CVS effects.

• Hypotension, bradycardia, cardiac arrhythmia, vascular collapse.

3. Overdose.

• Causes muscle twitching, convulsions, and cardiac arrhythmia.

4. Injections are painful and may delay wound healing.

Question 2. Mention the types of local anaesthetics.

Answer:

Types of Methods of Local Anaesthesia:

Question 3. Classify local anaesthetics. Compare lignocaine and cocaine.

Answer:

local anaesthetics Classification:

Question 4. Explain how the action of lignocaine can be prolonged.

Answer:

Prolonging Action of Lignocaine:

• The action of lignocaine can be prolonged by the addition of adrenaline.
• Adrenaline reduces the rate of absorption of lignocaine from the site to systemic circulation.
• This prolongs the duration of the action.
• It also reduces the systemic toxicity of lignocaine because of its slow absorption.
• As it gets absorbed, it is metabolized.

Question 5. Write a note on the advantages of lignocaine.

Answer:

lignocaine Advantages:

• Most widely used.
• Versatile, used for all types of blocks.
• Fast and long-lasting.
• Blocks nerve conduction within 3 min.
• More intense.
• Its effect last for 30 – 45 min.
• Available in various forms like spray, gel ointment, and injection.
• Cross sensitivity is not seen with it

B Pharmacy Important Questions Local Anaesthesia Short Essays

Question 1. Uses of adrenaline with lignocaine.
(or)
The rationale of combining adrenaline with Lignocaine.

Answer:

Combining adrenaline with lignocaine has some advantages as well as disadvantages.

Lignocaine Advantages:

• Decreases rate of absorption of lignocaine.
• This prolongs its duration of action.
• Reduces systemic toxicity.
• Increases intensity of nerve block.
• Provides a bloodless field for surgery.

Lignocaine Disadvantages:

• Intense vasospasm and ischaemia in the tissues with end arteries cause gangrene.
• Absorption of adrenaline may cause systemic toxicity.
• It may delay wound healing.

Lignocaine Contraindications:

• The adrenaline + lignocaine combination is contraindicated in
• Cardiovascular disorders.
• Hypertension.
• Congestive cardiac failure.
• Ischaemic heart disease.

Question 2. Differentiate between general anaesthesia and local anaesthesia.

Answer:

Question 3. Techniques of local anaesthesia with examples

Answer:

B Pharmacy Important Questions Local Anaesthesia Short Answers

Question 1. Lidocaine/Lignocaine/xylocain.

Answer:

Lidocaine is a long-lasting amide local anaesthetic agent.

• Lidocaine is the most widely used local anaesthetic.
• Lidocaine causes vasodilation in the area of injection.
• Lidocaine is used in all types of blocks.
• Lidocaine is available in various forms.
• Lidocaine effects occur within 3 min and last for 30 – 45 min.
• Lidocaine action can be prolonged by the addition of adrenaline.
• Lidocaine is metabolized in the liver.
• Lidocaine is used in 0.5 – 2% concentration.

Question 2. Cocaine.

Answer:

Cocaine is a natural alkaloid obtained from leaves of Erythroxylon coca.

• Cocaine is an ester local anaesthetic agent.
• Earlier it was used for ocular anaesthesia.
• Cocaine is well observed.
• As Cocaine is a protoplasmic poison, it is never injected.
• In the periphery, it blocks noradrenaline and adrenaline into adrenergic nerve endings.
• Cocaine causes.

1. Local vasoconstriction.
2. Tachycardia.
3. Rise in BP.
4. Mydriasis.

Question 3. Procaine.

Answer:

It is an ester local anaesthetic agent.

• It is the first synthetic local anaesthetic.
• It is metabolized in plasma.
• It is not surface anaesthetic.

Procaine Mechanism:

Hydrolysis of procaine.
↓
Release of para-aminobenzoic acid (PABA)
↓
This antagonises the antibacterial action of sulphonamide.

Question 4. Topical local anaesthetics.

Answer:

• Also known as surface anaesthetics.
• They are available as solutions, ointments, gels, creams, sprays, lozenges, etc.

Topical local anaesthetics Drugs used:

Topical local anaesthetics Uses:

• Applied topically on the mucous membrane of the nose, mouth, eyes, throat, upper respiratory tract, oesophagus, and urethra.
• During endoscopy
• In tonometry of eye.

Question 5. Intravenous anaesthesia.

Answer:

Also known as Bier’s block.

• It allows an extremely rapid induction.
• There is no route of quick elimination like lungs for it
• Thus it is used for induction.
• During it, anaesthesia is maintained by an inhalational agent

 

Question 6. Lidocain and mepivacaine.

Answer:

 

General Anaesthesia Important Notes

1. General Anaesthesia Classification

• Inhalation general anaesthesia
  • Liquids – chloroform, diethyl ether, halothane
  • Gases – cyclopropane, nitrous oxide
• Intravenous anaesthesia
  • Ultra short-acting barbiturates – thiopentone sodium, methohexital
  • Non barbiturates – ketamine, benzodiazepines

2. General Anaesthesia Stages

• Stage 1 – stage of analgesia
• Stage 2 – stage of delirium
• Stage 3 – stage of surgical anaesthesia
• Stage 4 – stage of respiratory paralysis

3. General Anaesthesia Drugs used

4. General Anaesthesia Neuroleptoanalgesia

• Consists of a combination of a major tranquiliser and a potent opioid analgesic
• Droperidol + fentanyl
• The patient remains conscious but assumes a trance-like state in which he is immobile apparently free from pain
• The addition of 65% N₂O + 35% O₂ converts neuroleptanalgesia to neurolept anaesthesia

General Anaesthesia Long Essays

Question 1. Classify general anaesthetics and describe pharmacological actions, merits and demerits of nitrous oxide.
(or)
Describe stages of general anaesthesia. Discuss nitrous oxide.

Answer:

Stages of Anaesthesia:

• Guedel describes four stages of ether anaesthesia.

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1. General anaesthesia Stage of analgesia.

• It is a stage from the beginning of anaesthetic inhalation to loss of consciousness.
• Some minor procedures can be performed during it

2. General anaesthesia Stage of delirium.

• It is the stage from loss of consciousness to the beginning of regular respiration.
• It is associated with excitement, struggling, shouting, crying, and sympathetic stimulation.
• No procedure can be carried out during this stage.

3. General anaesthesia Surgical anaesthesia.

• it is the stage from the onset of regular respiration to a cessation of spontaneous breathing.
• This has IV planes.
• There is a gradual loss of reflexes and relaxation of skeletal muscles.
• Most dental/surgical procedures are carried out in planes 1 or 2.

4. General anaesthesia Medullary paralysis.

• it is the stage from the cessation of breathing to failure of circulation and death.
• it is seen only with overdose
• it is never attempted.

General anaesthesia Classification:

General anaesthetics are classified into.

1. General anaesthesia Inhalation:

• Gas- Nitrous oxide, cyclopropane.
• Liquids.
  • Ether, halothane, isoflurane, desflurane.

2. General anaesthesia Intravenous.

• Inducing agents.
  • Thiopentone sodium
  • Methohexitone sodium
  • Propofol
• Slower-acting drugs.
  • Benzodiazepines.
    • Diazepam, lorazepam, midazolam.
  • Dissociative anaesthesia.
    • Ketamine
  • Opioid analgesia – Fentanyl.

Nitrous oxide:

• Nitrous oxide is a colourless, odourless, heavier-than-air, noninflammable gas.

Nitrous oxide Actions:

• A moderate increase in pain threshold.
• Slight amnesia effect.
• Euphoria is frequent.
• Decreased sense of smell.
• improved hearing.
• Slight myocardial depression.
• Minimal effect on respiration.
• Reduces minimal alveolar concentration.

Nitrous oxide Advantages:

• Non-inflammable, non-irritating.
• Rapid and smooth induction.
• Strong analgesic.
• Rapid recovery.
• No postoperative nausea.
• Has little effect on respiration and cardiovascular function.
• it is non-toxic to the liver, kidneys and brain.

Nitrous oxide Disadvantages:

• Less potent
• Poor muscle relaxant
• Enters the air-filled cavities faster.
• Repeated use causes bone marrow depression.
• Long-term exposure to low doses impairs DNA synthesis.

General Anaesthesia Short Essays

Question 1. Pre-anaesthetic medication.

Answer:

Pre-anaesthetic medication is the use of drugs before anaesthesia to make it more pleasant and safe.

Pre-anaesthetic medication AIMS:

• Relief of anxiety and apprehension preoperatively.
• Facilitate smooth muscle induction.
• Produce amnesia.
• Reduces secretion.
• Decreases vagal stimulation,
• Reduces postoperat4e nausea and vomiting.
• Decreases acidity and volume of gastric juice.
• Enhances hypnotic effects of drugs.

Pre-anaesthetic medication Drugs used for it:

• Sedative – hypnotic.
• Opioids.
• Anticholinergic.
• Neuroleptic.
• Antihistamine.
• Antiemetics.
• Antacids.

Question 2. Compart nitrous oxide and diethyl ether.

Answer:

Question 3. Compare nitrous oxide and halothane.

Answer:

Question 4. Ether.

Answer:

Ether is a highly volatile, colourless, inflammable liquid.

• Vapours produced by it are irritating.

Ether Actions:

• Stimulates the sympathetic system.
• increases heart rate
• Depresses vagus nerve;
• Decreases BP.
• Stimulates salvation.
• it is irritating to the respiratory tract.
• increases CSF pressure and blood glucose level.
• Potent analgesic, anaesthetic.
• Marked muscle relaxant.

Ether Advantages:

• Potent and reliable anaesthetic.
• Good analgesia.
• Provide full muscle relaxation.
• Bronchodilator.
• Easy to administer.
• Cheaper.
• No significant effect on cardiovascular and respiratory function.
• Does not sensitize the heart to adrenaline.

Ether Disadvantages:

• inflammable.
• Highly soluble in blood.
• Slow and unpleasant induction.
• Produce irritating vapours.
• Slow recovery.
• Postoperative nausea and vomiting are frequent.
• Enhances salivation and respiratory secretion.
• Due to this atropine is given for pre-medication.

Ether Status in Anaesthesia:

• Due to the above disadvantages, ether is not preferred.
• But due to easy administration and low cost, it is used in peripheral areas.

Question 5. Benzodiazepine.

Answer:

Benzodiazepines are one of the drugs used for premedication.

• it includes drugs like diazepam, midazolam. Oxazepam, lorazepam.

Benzodiazepine Actions:

• Mild decrease in BP.
• Minimal changes in respiration.
• Antiemetic.
• Produces amnesia.
• Relieves anxiety.
• Produces emotional responses in adolescent, females.

Benzodiazepine Uses:

• Induce, maintain and supplement anaesthesia.
• For conscious sedation.
• Slow-acting general anaesthetic.
• Used for endoscopy, cardiac catheterization, angiographic, mandibular fractures, etc.

Benzodiazepine Advantages:

• No significant respiratory depression.
• No postoperative nausea and vomiting.
• Absence of stimulation of involuntary movements.
• Also used as.

1. Sedatives hypnotics.
2. Antianxiety drugs.
3. Centrally acting skeletal muscle relaxant
4. Combined with analgesic and used for rheumatoid disorders.
5. Antiepileptic.

Question 6. Halothane.

Answer:

Halothane is a colourless, volatile liquid.

Halothane Advantages:

• Sweet odour.
• Non-irritant and non-inflammable.
• intermediate solubility in blood.
• Potent anaesthetic.
• Quick and pleasant induction.
• Rapid recovery
• Less chances of postoperative nausea and vomiting.

Halothane Disadvantages:

• Poor analgesic.
• Poor muscle relaxation.
• Causes direct depression of myocardial contractility.
• Reduce cardiac output, BP, and heart rate.
• Causes respiratory depression.
• Causes malignant hyperthermia.
• Severe hepatitis.
• Reduces renal blood flow and GFR.
• Expensive.
• Status in Anaesthesia:
• Halothane is a routinely used anaesthetic.
• Analgesic and muscle relaxant are used as adjuvant.

Question 7. Compare ether and halothane.

Answer:

Question 8. Diazepam.

Answer:

Diazepam belongs to benzodiazepine.

Diazepam Dose:

• 0.2 – 0.5 mg/kg.

Calcium Channel Blockers Important Notes

1. Calcium Channel Blockers Nifedipine

• It causes relaxation by decreasing the intracellular availability of calcium ions
• Causes arteriolar dilatation
• Have a mild effect on veins
• Do not depress the SA node or AV conduction

Calcium Channel Blockers Short Essays

Question 1. Uses of calcium channel blockers.

Answer:

1. Angina pectoris.

• Calcium channel blockers [CCB] reduce the frequency and severity of classical and variant angina.

2. Hypertension.

• CCBs are first-line hypertensive drugs.

3. Arrhythmias

• Verapamil controls ventricular rate in atrial flutter or fibrillation.

4. Peripheral vascular disease.

• Used in Raynaud’s disease for its vasodilator effects.

Question 2. Verapamil.

Answer:

Verapamil is a phenylethylamine that acts as are calcium channel blocker.

Verapamil Mechanism:

• Blocks all types of calcium channels.
• Inhibits calcium movement inside the cell in the depolarization phase.
• Inhibits muscle contraction.
• Decrease calcium currents and calcium entry into cardiac and vascular smooth muscle cells.

Verapamil Actions:

• Vasodilatation.
• Cardiac depression.
• Reduces BP
• Bradycardia.
• Reduces AV – conduction.

Question 3. Nifedipine.

Answer:

Nifedipine is a rapidly acting dihydropyridine drug.

Nifedipine Mechanism:

Read And Learn More: Pharmacology Question and Answers

• Decreases intracellular availability of Ca^++.
• Releases nitric oxide from the vascular endothelium.
• Inhibits cAMP – phosphodiesterase.
• Results in raised smooth muscle cAMP.

Nifedipine Uses:

• Angina pectoris.
• Hypertension.
• The alternative in premature labor.

Nifedipine Adverse effects:

• Flushing, palpitation, headache, ankle edema
• Hypotension.
• Increases frequency of angina.
• Increases urine voiding.

Question 4. Classify calcium channel blockers.

Answer:

calcium channel blockers Classification:

1. Phenylalkylamines – Verapamil.
2. Benzothiazepine – Diltiazem.
3. Dihydropyridine – Nifedipine, Felodipine, Amlodip- ine, Nitrendipine, Lacidipine, Nimodipine.

calcium channel blockers Actions:

1. Smooth muscle relaxation.
2. Negative chronotropic, inotropic, and dromotropic action on the heart

Calcium Channel Blockers Short Question And Answers

Question 1. Amlodipine.

Answer:

1. It is a dihydropyridine calcium channel blocker
2. It has higher vascular selectivity
3. It is longer acting drug
4. It is absorbed very slowly
5. Used in hypertension

Plasma Expanders And Pharmacotherapy Of Shock Short Answers

Question 1. Pharmacotherapy of shock.

Answer:

Shock is an acute circulatory failure with under-perfusion of tissues.

Pharmacotherapy of shock Types:

Pharmacotherapy of shock Treatment:

• Elevation of the foot end of the bed.
• Maintenance of BP and plasma level.
• Treat the cause.
  • Antibiotics – given the septic shock.
  • 4 morphine – given in cardiogenic shock.
  • 0.3 – 0.5 ml of 1:1000 solution of adrenaline IM was given in anaphylactic shock.
• Correction of acid-base and electrolyte balance.

Read And Learn More: Pharmacology Question and Answers

Question 2. Plasma expanders.

Answer:

Plasma expanders are high molecular weight substances that exert colloidal osmotic pressure.

• When infused 4, they retain fluid in the vascular compartments.

Plasma expanders Types:

Cortico Steroids Important Notes

1. Classification of corticosteroids

• Based on half-life
  • Short-acting – cortisone, hydrocortisone
  • Intermediate-acting – prednisolone, triamcinolone
  • Long-acting – dexamethasone, betamethasone
• Based on action
  • Primary glucocorticoid only – hydrocortisone, prednisolone, methylprednisolone, triamcinolone, dexamethasone, betamethasone
  • Mineralocorticoids only – desocxycorticosterone acetate
  • Primary mineralocorticoid – fludrocortisone, aldosterone
• Based on route
• Inhalation – beclomethasone, disproportionate, budesonide, flunisolide
• Systemic – hydrocortisone, prednisolone

2. Corticosteroids Actions:

• Anti-inflammatory
• Anti-allergic
• Vasopressor
• Water excretion
• Increase glucose
• Lipolysis

3. Corticosteroids Uses

• Addison’s disease
• Allergic diseases
• Skin diseases
• Autoimmune diseases
• Rheumatoid arthritis
• Rheumatic fever
• Dental uses
  • Desquamtive gingivitis
  • Autoimmune diseases
  • Oral submucous fibrosis

4. Corticosteroids Adverse effects

• Mineralocorticoid
  • Sodium and water retention
  • Hypokalaemia alkalosis
• Glucocorticoids
  • Cushing’s habitus
  • Fragile skin
  • Hyperglycaemia
  • Increased susceptibility to infection
  • Delayed wound healing
  • Peptic ulceration
  • Osteoporosis
  • Growth retardation
  • Psychiatric disturbances
  • HPA axis suppression

Read And Learn More: Pharmacology Question and Answers

5. Corticosteroids Contraindications

• Cushing’s syndrome
• Acute inflammatory diseases

Cortico Steroids Long Essays

Question 1. Classify glucocorticoids. Describe the mechanism of action, adverse effects, and therapeutic uses.
Answer:

1. Short-acting – hydrocortisone.
2. Intermediate-acting – prednisolone, methylprednisolone.
3. Long-acting – dexamethasone, betamethasone.

Mechanism of action:

Glucocorticoids Uses:

1. Replacement therapy.

2. Pharmacotherapy.

• Arthritis
  • Rheumatoid arthritis.
    • Used along with NSAIDS
  • Osteoarthritis.
    • Used as intra-articular injections.
• Rheumatic carditis.
  • Used in severely ill patients with fever.
• Acute gout
• Allergic diseases.
• Bronchial asthma.

• Collagen diseases.
  • Prednisolone was used for 6 weeks,
• Eye diseases.
• Renal diseases.
• Skin diseases.
• Gastrointestinal diseases.
• Liver diseases.
• Hematologic disorders.
• Cerebral edema.
  • Large doses of dexamethasone are used.
• Malignancies
  • Provide rapid symptomatic relief.
• Lung diseases
• Organ transplantation.
• Other uses:
  • Sarcoidosis.
  • Pneumocystis jirovici.
  • Hemolytic anemia.

Glucocorticoids Adverse Effects:

• Cushing’s syndrome.
• Hyperglycaemia.
• Increased susceptibility to infections.
• Osteoporosis.
• Avascular necrosis.
• Peptic ulceration.
• Mental disturbances.
• Cataract, glaucoma.
• Delayed wound healing.
• H PA axis suppression.
• Mineralocorticoid effects:
  • Salt and water retention
  • Edema
  • Weight gain
  • Hypokalemia
  • Hypertension.

Question 2. Enumerate synthetic corticosteroids. Mention their pharmacology, uses, and toxicity.
Answer:

Synthetic corticosteroids:

• They are more selective corticosteroids
• They are more potent than, natural ones.
• They do not have mineralocorticoid action
• They include.

1. Synthetic corticosteroids Prednisolone.

• Intermediate acting.
• Used for allergic, inflammatory, autoimmune diseases and malignancies.
• High doses cause fluid retention.
• Causes less HPA axis suppression.

2. Synthetic corticosteroids Methylprednisolone.

• More potent and more selective.
• 4 – 32 mg/day is given orally.
• Used in rheumatoid arthritis, renal transplant, and pemphigus.

3. Synthetic corticosteroids Triamcinolone.

• Highly selective
• Used 4 – 32 mg/day orally, 5 – 40 mg IM, as intra- articular injections as well as topically.

4. Synthetic corticosteroids Dexamethasone.

• Long action
• Used in
  • Inflammatory conditions,
  • Allergic conditions.
  • Shock.
  • Cerebral edema.
• Adverse effects
  • Marked HPA suppression
  • Less fluid retention and hypertension.

5. Synthetic corticosteroids Betamethasone.

• Similar to dexamethasone.
• Uses:
  • Cerebral edema
  • Use where fluid retention is required.

6. Synthetic corticosteroids Deflazacort

• Highly selective.
• Less potent
• Causes fewer adverse effects

Question 3. Name adrenocorticosterolds.
Answer:

Adrenocorticosteroids:

•They are compounds created by the adrenal cortex that have distant metabolic effects.

•They include.

1. Glucocorticoids
2. Mineralocorticoids and
3. Androgens.

Cortico Steroids Short Essays

Question 1. Difference between natural and synthetic glucocorticoids.
Answer:

Question 2. Adverse effects of glucocorticoids.
(or)
Adverse effects of prednisolone.
Answer:

1. Cushing’s syndrome.
   • Characterized by a moon face, supraclavicular or hump, obesity of trunk, muscle wasting, thin limbs and skin, and easy brushing.
   • Cutaneous atrophy, purple striae, acne.
2. Hyperglycaemia, precipitation of diabetes mellitus.
3. Increased susceptibility to infections. Opportunistic infections, due to immune suppression.
4. Muscle weakness, myopathy occasionally.
5. Osteoporosis, especially of vertebrae.
6. Peptic ulceration on prolonged use.
7. Avascular necrosis.
8. Growth retardation in children due to prolonged use.
9. Mental disturbances.
   • With high doses of steroids.
10. Delayed wound healing.
11. Cataract and glaucoma – when used as eye drops.
12. Foetal abnormalities.
    • When administered during pregnancy, it causes cleft palate and other defects.
13. HPA (Hypothalamo-pituitary adrenal) axis suppression.
    • It is withdrawal syndrome.
    • Causes reactivation of disease.

Question 3. Explain why glucocorticoid therapy should not be stopped abruptly.
(or)
Abrupt cessation of prolonged administration of glucocorticoids is hazardous. Explain.
Answer:

After prolonged administration of glucocorticoids, it should be tapered before withdrawal.

• Sudden cessation may cause suppression of the hypothalamic-pituitary-adrenal axis suppression.
• This leads to.
  • Precipitation of underlying disease.
  • Reactivation of disease.
  • Withdrawal symptoms like fever, myalgia, arthralgia, and malaise.
  • Such patients may be subjected to stress and can go to acute adrenal insufficiency.
  • Characterized by anorexia, nausea, vomiting, abdominal pain, hypotension, dehydration, and hyper-kalaemia.
• Any patient who has received more than 20 – 25 mg per day of hydrocortisone, needs tapering of the dose.
• If a patient has received long-term steroids within the previous six months, hydrocortisone is administered pro-prophylactically in such patients.

Cortico Steroids Short Question And Answer

Question 1. Adverse effects of glucocorticoids.
Answer:

glucocorticoids Adverse Effects:

• Cushing’s syndrome.
• Hyperglycaemia.
• Increased susceptibility to infections.
• Osteoporosis.
• Avascular necrosis.
• Peptic ulceration.
• Mental disturbances.
• Cataract, glaucoma.
• Delayed wound healing.
• H PA axis suppression.
• Mineralocorticoid effects:
  • Salt and water retention
  • Edema
  • Weight gain
  • Hypokalemia
  • Hypertension.

Question 2. Prednisolone.
Answer:

Prednisolone is a synthetic glucocorticoid.

• It is more selective and four times more potent than hydrocortisone.

Prednisolone Uses:

• Allergic reactions.
• Inflammatory conditions.
• Autoimmune diseases.
• Malignancies.

Prednisolone Adverse Effects:

• Fluid retention in high doses
• Less HPA axis suppression.

Question 3. Betamethasone.
Answer:

Betamethasone is long acting glucocorticoid.

• It is potent and highly selective.

Betamethasone Uses:

• Cerebral edema.
• Inflammatory conditions.
• Allergic reactions.
• Shock.

Betamethasone Adverse Effects:

• Marked HPA axis suppression.
• But does not cause fluid retention.

Question 4. Hydrocortisone.
Answer:

Hydrocortisone is a short-acting corticosteroid.

• It may be natural or synthetic.
• It has mineralocorticoid activity.
• The normal rate of secretion – 10 mg/day.

Hydrocortisone Uses:

• Anti-inflammatory.
• Allergic reactions.

Hydrocortisone Disadvantages:

• Delays wound healing.

Question 5. Uses of glucocorticoids.
Answer:

glucocorticoids Use:

1. Endocrinal uses.

• Replacement therapy.
  • Acute adrenal insufficiency.
  • Chronic adrenal insufficiency.
  • Congenital adrenal hyperplasia.

2. Non-endocrinal uses.

• Arthritis – rheumatoid arthritis, osteoarthritis, rheumatic fever, acute gout
• Allergic reactions.
• Bronchial asthma.
• Collagen diseases
• Eye diseases.
• Skin diseases.
• Renal diseases
• Liver diseases
• Lung diseases
• Gastrointestinal diseases.
• Cerebral edema.
• Organ transplantation.
• Malignancies
• Hematological disorders.
• Other – sarcoidosis, pneumocystis jiroveci, hemolytic anemia.

Question 6. Adrenocorticotropic hormone (ACTH).
Answer:

ACTH is a 39 amino acid single-chain peptide.

• It promotes steroidogenesis in the adrenal cortex by stimulating cAMP formation.
• Absence of ACTH results in adrenal atrophy.
• Hypothalamus regulates ACTH release from the pituitary.
• Excess production of ACTH causes Cushing’s syndrome.

ACTH Uses:

• Used primarily for the diagnosis of disorders of the pituitary-adrenal axis.
• When used IV, it increases plasma cortisol if the adrenals are functional.
• It serves as a diagnostic tool for differentiating between primary and secondary adrenal insufficiency.

Question 7. Difference between hydrocortisone and dexamethasone.
Answer:

Question 8. Name four glucocorticoids.
Answer:

1. Short-acting – cortisone, hydrocortisone.
2. Intermediate acting.
   • Prednisolone, methylprednisolone.
3. Long-acting.
   • Dexamethasone, betamethasone.

Estrogen Progestins And Hormonal Contraceptives Short Essays

Question 1. Combination of estrogen and progesterone in oral contraceptives.
Answer:

Combined pills contain low doses of estrogen and progestin.

• Estrogen used is ethinylestradiol or mestranol.
• Progestrin used are desogestre and norgestimate.
• They are highly efficacious.

Combination of estrogen and progesterone in oral contraceptives Schedule:

• Starts on the 5th day of the menstrual cycle.
• One tablet daily for 21 days.
• The next course started after a gap of 7 days.

Combination of estrogen and progesterone in oral contraceptives Combined effect:

• Inhibits ovulation.
• Progestin ensures prompt bleeding at the end of a cycle.
• Blocks risk of developing endometrium carcinoma due to estrogen.
• Reduces incidence of pelvic inflammatory disease and ectopic pregnancy.
• Reduces risk of ovarian cancers.

Estrogen Progestins And Hormonal Contraceptives Short Notes

Question 1. Oral contraceptives.
Answer:

Various types of oral contraceptives are

1. Oral contraceptives Combined pill.

• Contains low doses of estrogen and progestin.
• It is highly efficacious.
• Monophasic, diphasic, and triphasic preparation are available.
• Started on the 5th day of the menstrual cycle for 21 days.

2. Oral contraceptives Mini pill.

• Contains a low dose of progestin-only.
• Taken daily continuously without any gap.
• Has low efficacy.

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3. Oral contraceptives Postcoital contraceptives.

• Combined use of estrogen and progesterone is preferred.
• Should be used as an emergency method.
• They act by preventing implantation.
• Should be started within 72 hours of coitus.
• Has 90 – 98% efficacy.

Question 2. Oxytocin.
Answer:

Oxytocin is a non-peptide secreted by the posterior pituitary along with ADH.

Oxytocin Actions:

• Increases force and frequency of uterine contractions.
• With low doses full relaxation occurs between contractions.
• Contracts myoepithelium of mammary gland
• Helps in milk ejection.

Oxytocin Uses:

• Before delivery to induce labor.
• Used to control postpartum hemorrhage.

Oxytocin Adverse effects:

• Improper administration or overdosage causes.
  • Maternal and fetal soft tissue injury.
  • Rupture of the uterus.
  • Fetus asphyxia.
  • Death.

Opioid Analgesics Important Notes

1. Opioid Analgesics  Classification

2. Opioid Analgesics Morphine

• It is obtained from papaver somniferum
• Actions
  • Relieves severe pain like visceral pain
  • Produces sleep
  • Produces euphoria
  • Produces miosis
  • Respiratory depression
  • Causes vomiting by stimulating the chemoreceptor trigger zone (CTZ)
• Opioid Analgesics Morphine Adverse effects
  • Euphoria, dysphoria, and mental clouding
  • Respiratory depression
  • Tolerance and drug dependence
  • Acute morphine poisoning – is characterized by
    • Respiratory depression
    • Pinpoint pupils
    • Hypotension
    • Shock
    • Coma
• Opioid Analgesics Morphine Uses
  • Analgesics
  • For producing sleep and sedation
  • As pre-anesthetic medication
  • As antitussive
  • In the treatment of acute left ventricular failure.
• Opioid Analgesics Morphine Contraindications
  • Asthma
  • Head injuries
  • Undiagnosed acute abdominal pain
  • infants and elders
  • Hypothyroidism
  • COPD
  • Unstable personalities

Read And Learn More: Pharmacology Question and Answers

• Opioid Analgesics Morphine Withdrawal symptoms
  • Lacrimation
  • Yawning
  • Anxiety
  • Abdominal colic
  • Diarrhea
  • Mydriasis
  • Palpitation, rise in BP
  • Weight loss

3. Opioid Analgesics Fentanyl

• It is short acting IV opioid analgesic
• Used for general anesthesia and conscious sedation

4. Opioid Analgesics Remifentanil

• Indicated as an opioid analgesic adjunct for induction and maintenance of general anesthesia
• It should not be used alone
• Should not be used for epidural or intrathecal administration as glycine in it may cause neurotoxicity

Opioid Analgesics Long Essays

Question 1. Classify the narcotic analgesic group of drugs and write about morphine.

Answer:

Narcotic/Opioid Analgesic:

• Opioid analgesics are analgesics that are either derived from opium or resemble opium in action.

Opioid Analgesic Classification:

1. Natural opium alkaloids – morphine, codeine.

2. Semi-synthetic opiates – diacetylmorphine, pholcodine.

3. Synthetic opioids – pethidine, fentanyl, methadone.

Morphine: Morphine is a natural opioid and the principal alkaloid in opium.

Morphine Actions:

1.  Morphine CNS actions:

• Morphine is potent analgesic.
• Produces euphoria, sedation, and hypnosis.
• Morphine has a calming effect, a feeling of detachment.
• Depresses respiratory center.
• Depresses cough center.
• Depresses the temperature regulating center and causes hypothermia.
• Depresses vasomotor centre and reduces BP.
• Morphine stimulates.
  • CTZ – induces vomiting.
  • Edinger Westphal nucleus – produces miosis.
  • Vagal center – causes bradycardia.
  • Cortical areas and hippocampal cells.

2. Morphine Neuro-endocrine actions.

• Morphine weakens hypothalamic influence on the pituitary.

3. Morphine CVS action.

• Morphine causes vasodilatation due to.
  • Histamine release.
  • Depression of vasomotor center.
  • Decreases tone of blood vessels.

4. Morphine GIT action.

• Morphine causes constipation.
• Decreases propulsive movements.
• Decreases GIT secretions.

5. Morphine Smooth muscles.

• The biliary tract causes spasms of the sphincter of Oddi.
• Urinary bladder increases the tone of the detrusor and sphincter.
• Bronchi-causes bronchoconstriction.

Morphine Uses:

1. As analgesic.

• Morphine is used in traumatic, visceral, ischaemic, postoperative, burn, and cancer pain.
• Adequate use of morphine is indicated in an emergency.

2. As pre-anesthetic medication.

• Used in selected patients.

3. Balanced anesthesia and surgical analgesia.

• An important component of anesthetic techniques.

4. Relief of anxiety and apprehension.

• Used in myocardial infarction.

5. Acute left ventricular failure.

• Used to alleviate dyspnea.

6. Diarrhea.

• Used for symptomatic treatment

Morphine Adverse Effects:

• Nausea, vomiting, constipation, urinary retention.
• Dizziness, mental clouding, dysphoria.
• Respiratory depression, hypotension.
• Apnea – when administered to a pregnant woman in labor.
• Allergic reactions – skin rashes, pruritis, and wheal at the site of injection.
• Tolerance and dependence develop.
• Withdrawal symptoms in newborns – irritability, excessive crying, tremors diarrhea, sneezing, yawning, vomiting, and fever.

Question 2. Discuss the uses and toxic effects of morphine. Name morphine antagonists available.

Answer:

Morphine Antagonists:

1. Morphine Antagonists Naloxone.

• It is the competitive antagonist.
• It Is devoid of any agonist actions.
• Injected Intravensouly It antagonizes all actions of morphine.
  • Analgesia.
  • Normalizes and stimulates respiration.

2. Morphine Antagonists Naltrexone.

• It Is orally active.
• More potent
• Have a longer duration of act Ion
• It Is used for ‘opioid blockade
• It reduces alcoholic cravings.

3. Morphine Antagonists Nalmefene.

• Effective orally.
• Used In opioid overdosage.

Question 3. Classify analgesics. Discuss Indications. Contraindications for the use of morphine giving reason.

Answer:

Analgesics:

• Analgesics is a drug that relieves pain without loss of consciousness.

Analgesics Classification:

They are classified into two classes.

1. Opioid analgesics:

•  Natural opioid.
  • Morphine, codeine, noscapine.
• Semisynthetic derivatives.
  • Heroin, oxymorphone, pholcodine.
•  Synthetic opioids.
  • Pethidine, fentanyl, diphenoxylate, loperamide, dextropropoxyphene, methadone, and tramadol.

2. Non-opioid Analgesics:

• Non-selective Cox inhibitor.
  • Salicylates – aspirin.
  • Proprionic acid derivative – Ibuprofen.
  • Anthranilic acid derivative – mefenamic acid
  • Aryl-acetic acid derivatives – diclofenac, ace- clofenac.
  • Oxicam derivatives – piroxicam, tenoxicam.
  • Pyrrolo – pyrrole derivative – ketorolac.
  • Indole derivative – indomethacin.
  • Pyrazolone derivative – phenylbutazone.
• Preferential COX-2 inhibitors.
  • Nemisulide, meloxicam, nabumetone.
• Selective COX-2 inhibitors.
  • Celecoxib, etoricoxib, parecoxib.
• Analgesic – antipyretic.
  • Para-amino phenol derivative – paracetamol.
  • Pyrazolone derivative – metamizol.
  • Benzoxazocine derivative – nefopam.

Morphine: Morphine is a natural opioid and the principal alkaloid in opium.

Opioid Analgesics Short Essays

Question 1. Pentazocine.

Answer:

Pentazocine is the first agonist-antagonists to be used as analgesic.

Pentazocine Properties:

• Has weak p antagonist action and more k agonist action.
• Has less addiction liability.
• 20 mg pentazocine is effective to 10 mg morphine. Analgesia is caused primarily spinal.
• It increases heart rate and BP and thereby increases cardiac work.

Dose and route of administration:

• 50 -100 mg – orally.
• 30 – 60 mg – IM

Pentazocine Uses:

• Used in postoperative and chronic pain – bums trauma, fracture, cancer.

Pentazocine Adverse effects:

• Sedation, dizziness.
• Sweating, dysphoria.
• Nausea, nightmares, hallucinations.
• Tolerance and dependence develop.
• Pain and sterile abscess – at the site of injection.

Question 2. Dextropropoxyphene.

Answer:

Dextropropoxyphene is a congener of methadone.

• It binds to opioid receptors and produces effects similar to morphine.
• It has poor antitussive action.
• Its metabolite is cardiotoxic.

Dextropropoxyphene Uses:

• Use in mild to moderate pain.
• Used in combination with aspirin – dextropropoxyphene 32 mg + aspirin 600 mg.

Dextropropoxyphene Adverse effects:

• Has abuse potential.
• High doses cause rapid-onset respiratory depression, delirium, and convulsions.

Question 3. Compare morphine and pethidine.

Answer:

Question 3. Tramadol.

Answer:

• It is a centrally-acting analgesic
• Tramadol Mechanism of Action
  • Weak opioid agonist
  • Inhibits reuptake of noradrenaline and serotonin → activates mono-aminergic spinal inhibition of pain
• Tramadol Pharmacokinetics
  • Good oral bioavailability
  • Plasma half-life – 3-5 hours
  • The effect lasts for 4-6 hours
• Tramadol Uses
  • Acute pain – diagnostic procedures, dental pain
  • Chronic pain – including cancer pain
• Tramadol Adverse reactions
  • Mild respiratory depression
  • Dryness of mouth, sweating
  • Dizziness, sedation
  • Drug dependence

Opioid Analgesics Short Answers

Question 1. Actions of morphine.

Answer:

1. CNS actions.

• Potent analgesic.
• Produces euphoria sedation, and hypnosis.

2. Respiration.

• Depresses respiratory center.

3. Cough center – depression

4. CVS action

• Reduces BP
• Causes vasodilatation.

5. Nausea and emesis.

• Directly stimulates CTZ.

6. Pupils – produce miosis.

7. GIT actions.

• Decreases propulsive movements.
• Decreases GIT secretions.

8. Neuroendocrine action.

• Weakens hypothalamic influence on the pituitary.

Question 2. Uses of morphine.

Answer:

Morphine is used as

• Analgesic
• Pre-anesthetic medication.
• To relieve anxiety and apprehension.
• Balanced anesthesia and surgical analgesia.
• Acute left ventricular failure.
• Diarrhea.

Question 3. Contraindications of morphine.

Answer:

• In extreme ages.
• In patients with respiratory insufficiency.
• Bronchial asthma.
• Head injury.
• Hypovolemic shock.
• Undiagnosed acute abdominal pain.
• Elderly males.
• Hypothyroidism, liver, and renal diseases.
• Unstable personalities.

Question 4. Codeine.

Answer:

Codeine is methyl-morphine.

• It is a naturally occurring opium alkaloid.
• It depresses the cough center in sub-analgesic doses.
• It is effective orally and well absorbed.
• It has a very low affinity for opioid analgesics.
• Single oral dose acts for 4 – 6 hours.
• It is given at bedtime.

Codeine Uses:

• Used as antitussive.
• Used in combination with paracetamol for analgesia – codeine 30 mg + paracetamol 500 mg

Codeine Adverse effects:

• Constipation.
• Less addictive.

Question 5. Morphine poisoning.

Answer:

Acute morphine poisoning may be accidental, suicidal, or homicidal.

• In non-tolerant adults; 50 mg of morphine IM produces it.

Morphine poisoning Manifestations:

• Respiratory depression with shallow breathing.
• Stupor or coma.
• Flaccidity.
• Cyanosis.
• Pinpoint pupil.
• Fall in BP, shock.
• Hypothermia.
• Death due to respiratory failure.

Morphine poisoning Treatment:

• Maintenance of BP. By IV fluids.
• Positive pressure respiration.
• Gastric lavage with potassium permanganate.
• Naloxone – 0.4 – 0.8 mg IV repeated every 10 -15 min.

Question 6. Four adverse effects of fentanyl.

Answer:

• Nausea
• Vomiting
• Respiratory depression
• Muscle rigidity

Viva Voce

1. Codeine is used for the treatment of cough
2. The antidote for morphine poisoning is naloxone
3. Opioids are also called narcotic analgesics
4. Naloxone is a competitive antagonist on all types of opioids receptors
5. Opioids receptors are mu, kappa, and delta

Adrenergic Antagonist Important Notes

1. Sympathetic blocking drugs

2. Uses of alpha-blockers 

• Pheochromocytoma
• Hypertension
• Peripheral vascular diseases
• Congestive cardiac failure
• Benign hypertrophy of the prostate

3. Abrupt withdrawal of beta-blocker after chronic use causes

• Rebound hypertension
• Worsening of angina
• Sudden death

Beta 2 Adrenergic Antagonist

Adrenergic Antagonist Long Essays

Question 1. Classify beta-adrenergic receptor blockers. Describe the pharmacological actions, uses and adverse effects of propranolol.

Answer:

Beta-adrenergic receptor blockers:

β-blockers are drugs that block the actions of catecholamines mediated through β -receptors.

Beta-Adrenergic Receptor Blockers Classification:

1. Nonselective

• Without intrinsic sympathomimetic activity
  • Propranolol, sotalol, timolol.
• With intrinsic sympathomimetic activity
  • Pindolol, oxprenolol
• With additional blocking property.
  • Labetalol, carvedilol.

Beta 2 Adrenergic Antagonist

2. Cardioselective

• Metoprolol, atenolol, bisoprolol, esmolol, betaxolol
• Propranolol-Propranolol is a first-generation non-selective β-blocker with intrinsic sympathomimetic activity.

Pharmacological actions:

1. CVS:

• Decreases heart rate, force of contraction and cardiac output.
• Decreases BP.
• Cardiac work and oxygen consumption are reduced.
• AV conduction is delayed
• Blocks cardiac stimulant action of adrenergic drugs.
• Improves exercise tolerance in angina patients.

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2. Blood vessels.

• Blocks vasodilation produced by isoprenaline.

3. Respiratory tract

• Blocks β2 receptors in bronchial smooth muscles
• Increases bronchial resistance.

4. CNS.

Mild central effects like behavioural changes, forgetfulness, increased dreaming and nightmares occur.

5. Local anaesthetic.

• Potent anaesthetic agent but not used due to irritation.

Beta 2 Adrenergic Antagonist

6. Eye:

• Reduces intraocular pressure.
• Decreases secretion of aqueous humour.

7. Metabolic:

• Blocks adrenergic ally-induced lipolysis.
• Inhibits glycogenolysis.

8. Sekeletal muscle.

• Inhibits adrenergic ally-provoked tremors.

B Adrenergic Antagonist

Beta-Adrenergic Receptor Blockers Uses:

• Hypertension
• Prophylaxis of exertional angina.
• Congestive cardiac failure.
• Dissecting aortic aneurysm.
• Cardiac arrhythmia.
• Myocardial infraction.
• Pheochromocytoma.
• Prophylaxis of migrane.
• Glaucoma.
• Anxiety.
• Essential tremor.
• Hypertrophic obstructive cardiomyopathy.

Beta-Adrenergic Receptor Blockers Adverse effects:

• Hypotension.
• Impairment of myocardial function.
• Cold extremities.
• Precipitate acute asthmatic attacks
• Fatigue, weakness.
• Abrupt withdrawal causes rebound hypertension.
• Impairment of carbohydrate tolerance.

B Adrenergic Antagonist

Adrenergic Antagonist Short Essays

Question 1. Adrenergic alpha-blockers.

Answer:

Adrenergic alpha-blockers are drugs that block the adrenergic responses mediated through alpha-adrenergic receptors.

Adrenergic alpha-blockers Classification:

1. Non-equilibrium.

• Phenoxybenzamine.

2. Equilibrium or competitive.

• Non-selective.
  • Ergot alkaloids – ergotamine, ergotoxine.
  • Hydrogenated ergot alkaloids – dihydro- ergotamine.
  • Imidazolines – tolazoline.
  • Miscellaneous – chlorpromazine
• α1- selective.
  • Prazosin, Terazosin, Doxazosin.
• α2 – selective. – yohimbine.

Adrenergic alpha-blockers Actions:

• Inhibits vasoconstriction, leads to vasodilatation and decreases BP.
• Enhances release of noradrenaline by α2 blocked
• Reflex tachycardia.
• Nasal stiffness and miosis.
• Increased intestinal motility.
• Reduced tone of smooth muscle.

Adrenergic alpha-blockers Uses:

• Pheochromocytoma.
• Hypertension.
• Secondary shock.
• Peripheral vascular diseases.
• Benign hypertrophy of the prostate.

Adrenergic alpha-blockers Adverse effects:

• Postural hypotension, palpitation.
• Nasal stiffness, miosis.
• Impaired ejaculation.
• Impotence.

Question 2. Cardioselective beta blockers.

Answer:

Cardioselective beta blockers Actions:

• Selectively block β1 receptors.
• Bronchospasm is less or negligible.
• Less interference with carbohydrate metabolism.
• Lower incidence of cold extremities.
• Impaired exercise performance.
• Lesser chances of peripheral vascular disease.

Drugs included in it:

Adrenergic Antagonist Short Answers

Question 1. Uses of alpha and beta blockers.

Answer:

Alpha 2 Adrenergic Antagonist

Question 2. Prazosin.

Answer:

It is a potent highly selective α1 blocker

Prazosin Actions:

• Blocks sympathetically mediated vasoconstriction.
• Causes fall in BP.
• Dilates arterioles more than veins which result in decreased peripheral vascular resistance and cardiac output

Prazosin Uses:

• Hypertension.
• Left ventricular failure.
• Raynaud’s disease.
• Prostatic hypertrophy.
• Improve urine flow thereby reducing residual urine in the bladder.

Question 3. Timolol.

Answer:

• It is a non-selective β blocker.
• It is short acting.
• Orally it is a potent β – blocker.
• Its ocular hypotensive action is smooth and well-sustained.

Timolol Uses:

1. Topically.

• In the treatment of glaucoma.

2. Orally.

• Hypertension.
• Angina
• Prophylaxis of myocardial infarction.

Alpha 2 Adrenergic Antagonist

Question 4. Name cardioselective p blockers.

Answer:

• Cardioselective beta blockers:
• Metoprolol – bisoprolol – celiprolol
• Atenolol esmolol – nebivolol.
• Acebutolol – betaxolol.

Question 5. Propranolol is contraindicated in bronchial asthma Why?

Answer:

1. Blockade of β2 receptors of smooth muscles by propranolol causes.
2. Increases in airway resistance.
3. Precipitation of acute attacks in asthmatics.
4. Worsens chronic obstructive lung diseases.
   • Thus, it is contraindicated in bronchial asthma.

Question 6. Labetalol.

Answer:

Labetalol is the first adrenergic antagonist capable of blocking both α and β receptors.

• It is effective orally.

Labetalol Actions:

• Vasodilation
• Fall in BP
• Reduction in cardiac output, heart rate, and peripheral vascular resistance.

Alpha 2 Adrenergic Antagonist

Labetalol Uses:

• Pheochromocytoma.
• Clonidine withdrawal.
• Essential hypertension.

Labetalol Adverse effects:

• Postural hypotension.
• GI disturbances.

Viva Voce:

Beta-blocker is contraindicated in asthmatic patients

Introduction And Sources Of Drugs Important Notes

Pharmacology

• It is the science that deals with drugs
• It consists detailed study of drugs and their actions on living organisms

Introduction And Sources Of Drugs Short Essays

Question 1. Sources of drugs.

Answer:

Sources of drugs:

They can be natural or synthetic.

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1. Natural:

2. Synthetic:

Anticholinergic Drugs  Important Notes

1. Anticholinergic drugs

• They inhibit the muscarinic actions of acetylcholine
• Examples
  • Atropine
  • Scopolamine
  • Propantheline
  • Methantheline

2. Actions of atropine

• • Decreases all secretions
  • Mydriasis of pupil
  • Increased heart rate
  • Bronchial dilation
  • Relieves hypermotility

3. Drugs causing mydriasis

• • Anticholinergic drugs – atropine
  • Adrenergic drugs – ephedrine, phenylephrine

4. Scopolamine/ Hyosine

• • It is an anticholinergic drug
  • Most effective drug for motion sickness
  • Causes sedation

Anticholinergic Drugs Long Essays

Question 1. Classify anticholinergic drugs. Discuss pharmacological actions, uses & adverse effects of atropine. Mention symptoms of atropine poisoning and the line of treatment.

Answer:

Anticholinergic drugs:

• Anticholinergic drugs are agents which block the effects of acetylcholine on cholinergic receptors.

Anticholinergic drugs Classification:

1. Natural alkaloids – atropine, hyoscine.

2. Semisynthetic derivatives.

• Homatropine, atropine mononitrate hyoscine butyl bromide.

3. Synthetic compounds.

• Mydriatics – cyclopentolate.
• Antisecretory – antispasmodics.
  • Quaternary compounds – propantheline.
  • Tertiary amines – dicyclomine, pirenzepine.
• Vasicoselective – Oxybutynin, flavoxate.
• Anti parkinsonian – trihexyphenidyl, biperiden.

Atropine:

• It is the chief alkaloid of belladonna.
• Pharmacological actions.

Atropine Uses:

1. Preanaesthetic medication.
   • Atropine is administered 30 min before surgery.
   • This reduces salivary and respiratory secretions which prevent laryngospasm and bradycardia.
2. As antispasmodic.
   • In diarrhea and dysentery – reduces abdominal pain.
   • Overcomes spasm of the sphincter of Oddi.
   • In nocturnal enuresis – causes urinary retention.
3. As mydriatic and cycloplegic.
   • Used topically during refractory testing.
   • Used in the treatment of iritis, keratitis, and corneal ulcer.
   • Prevents adhesion between the iris and lens or the iris and cornea.
4. In organophosphorus poisoning.
5. In bronchial asthma, peptic ulcer
6. Used in motion sickness.
7. Used during labor to produce sedation and amnesia.
8. Used in myocardial infarction to block vagal bradycardia.
9. Pulmonary embolism – as it reduces reflex respiratory secretions.

Atropine Adverse effects:

• Adverse effects are common.
• It includes blurring of vision, dry mouth, dysphagia, dry skin, fever, constipation & urinary retention.

Read And Learn More: Pharmacology Question and Answers

• High doses lead to atropine poisoning.

Features of atropine poisoning:

• Palpitation.
• Excitement, psychotic behavior, ataxia, delirium, hallucination.
• Hypotension, weak and rapid pulse.
• Respiratory depression.
• Dilated pupil, photophobia, blurring of vision.
• Cardiovascular collapse, convulsions, coma.

Atropine Treatment:

• Ingested poison was removed by gastric lavage.
• Use cold sponging or ice bags to reduce body temperature.
• A drug used is physostigmine – 1 – 3 mg SC or IV, re¬peated 4-6 hourly.
• It antagonizes control and peripheral effects.

Question 2. Discuss atro¬pine. Mention some atropine substitutes and their uses in therapy.

Answer:

Atropine substitutes:

They aim at producing more selective action on certain functions.

Anticholinergic Drugs Short Essays

Question 1. Compare atropine and cocaine.

Answer:

Question 2. Compare atropine and scopolamine.

Answer:

Anticholinergic Drugs Short Answers

Question 1. Homatropine.

Answer:

Homatropine is an atropine substitute that is used on the eye.

• It causes mydriasis & cycloplegia that last for about 6 – 24 hours.
• They have shorter actions.
• It is used in atropine intolerance.
• It is formed to overcome the lack of sensitivity of belladonna alkaloids.

Question 2. Uses of atropine.

Answer:

• As pre-anesthetic medication.
• As antispasmodic
• As mydriatic and cycloplegic.
• In organophosphorus poisoning.
• In bronchial asthma.
• Used in motion sickness.
• Used during labor to produce sedation and amnesia.
• Used in myocardial infarction.
• Pulmonary embolism.

Question 3. Adverse effects of atropine.

Answer:

• Adverse effects of atropine are common. It includes.
• The blurring of vision.
• Dry mouth and skin.
• Dysphagia.
• Fever
• Constipation.
• Urinary retention.

Question 4. Mention atropine substitutes.

Answer:

• Hyoscine butyl bromide.
• Ipratropium bromide.
• Propantheline.
• Glycopyrrolate
• Pirenzepine.
• Homatropine.

Question 5. The rationale of using atropine as pre-anesthetic medication.

Answer:

Atropine is administered 30 minutes before any surgery because.

• It reduces salivary and respiratory secretion.
  • This prevents laryngospasm.
• It prevents bradycardia during surgery.
• It acts as a bronchodilator.
  • This reduces the risk of bronchial asthma related to anaphylactic shock.

Question 6. Enlist six uses of anticholinergic drugs.

Answer:

1. Preanaesthetic medication – to reduce secretions
2. Antispasmodic – in diarrhea and colic
3. Asmydriatric
4. Parkinsonism – reduces tremors and rigidity
5. Organophosphorous poisoning – atropine is used
6. Motion sickness – hyoscine is given 30 minutes before the journey
7. During labor – hyoscine is used to produce sedation and amnesia

Viva Voce:

1. Atropine is used in organophosphorus poisoning
2. Atropine is a CNS stimulant
3. Scopolamine is CNS depressant