Pharmacology

Anti Parkisonian Drugs Important Notes

Anti Parkinsonian Drugs Parkinsonism

• It is an extrapyramidal motor disorder
• Characterized by
  • Rigidity
  • Tremor
  • Hypokinesia
  • Excessive salivation
  • Dementia
• Mainly occurs due to the degeneration of nigrostriatal neurons which are dopaminergic
• Dopamine deficiency and cholinergic excess occur in it
• Drugs used for it are
  • Levodopa – precursor of doapmine
  • Carbidopa and benserazide – prevent decarboxylation of levodopa

Anti Parkinsonian Drugs Long Essays

Question 1. Classify the drugs used in Parkinsonism. Discuss the pharmacology and adverse effects of L-dopa.

Answer:

Anti-parkinsonian drugs:

• These are drugs that have a therapeutic effect on Parkinsonism.

Anti-Parkisonian Drugs Classification:

1. Drugs affecting the brain’s dopaminergic system.

• Dopamine precursor – levodopa (L-dopa).
• Peripheral decarboxylase inhibitors – carbidopa, benserazide.
• Dopaminergic agonists – bromocriptine, ropinirole.
• MAO-B inhibitor – selegiline.
• COMT (Catechol-O-methyl transferase) inhibitor – entacapone, touch.

Anti-Parkisonian Drugs Levodopa (L-Dopa):

• Levodopa is the precursor of dopamine.

Levodopa Mechanism of action:

Levodopa crosses the blood-brain barrier.
↓
It is taken up by pre-synaptic terminals of dopaminergic
neurons.
↓
Dehydroxylation occurs.
↓
Causes the formation of dopamine.

Levodopa Actions:

1. CNS actions.

• Causes hypokinesia and rigidity resolution.

2. CVS actions:

• Causes tachycardia and postural hypotension.

3. CTZ [Chemoreceptor trigger zone]

• Stimulates CTZ to induce vomiting.

4. Endocrine.

• It acts on pituitary mamma tropes to inhibit prolactin release.

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Levodopa Uses:

• Effective in idiopathic parkinsonism.

Levodopa Adverse effects:

• GIT symptoms – nausea, vomiting, anorexia.
• CVS affects – postural hypotension, tachycardia, palpitation, cardiac arrhythmia, and angina.
• Alteration in taste sensation.
• Abnormal movements – Dyskinesia, facial tics, grimacing, tongue thrusting.
• Behavioral effects – mild anxiety, nightmares, mania, hallucinations.
• Fluctuations in motor performance.

Anti Parkinsonian Drugs Short Essays

Question 1. Explain why levodopa is given along with carbidopa.

Answer:

Decarboxylase inhibitor i.e., carbidopa prevents the conversion of levodopa to dopamine outside the brain by inhibiting the DOPA decarboxylase enzyme, peripherally.

• This combination can cross the blood-brain barrier and reaches its site of action in the brain.
• Other benefits obtained by this combination are:
  • It reduces the dose of levodopa Upton approx 1/4^th
  • The plasma half-life of levodopa is prolonged.
  • The systemic concentration of dopamine is reduced.
  • Response to levodopa appears earlier.
  • Side effects like nausea and vomiting are reduced.
  • Cardiac complications are minimized.
  • Pyridoxine does not interfere with the treatment
  • The on-Off effect is minimized.
  • The degree of improvement may be higher.

Anti Parkinsonian Drugs Short Answers

Question 1. Is pyridoxine given with levodopa?

Answer:

Pyridoxine is not given with levodopa because.

• Pyridoxine enhances the decarboxylation of levodopa.
• Reduces the drug availability to the CNS.
• This results in the need for greater doses of levodopa for the same desired result
• Thus, pyridoxine is not combined with levodopa.

 

Anti Arrythmic Drugs Important Notes

1. Antiarrythmic Drugs Classification

Anti Arrythmic Drugs Short Question And Answers

Question 1. Classification of anti-arrhythmic drugs.

Answer:

Arrhythmic Drugs Classification:

1. Class – 1 – Sodium channel blockers.

• Prolong repolarization – Quinidine, procainamide,
• Shorten repolarization – Lignocaine, mexiletine.
• Little or no repolarization – Propafenone, Flecainide.

2. Class 2 – β blockers.

• Propranolal, esmolol.

3. Class – 3 – Potassium channel blockers.

• Amiodarone, Dofetilide.

4. Class – 4 – Calcium channel blockers.

• Verapamil, diltiazem.

Question 2. Why procainamide is preferred to procaine?

Answer:

Procainamide is a derivative of procaine.

• It is preferred to procaine because.

1. It has weak anticholinergic action.
2. Has antiarrhythmic action, while procaine has only a local anesthetic effect
3. It is better tolerable.

Anti-Epileptic Drugs Important Notes

1. Anti-Epileptic Drugs Types of seizures and drugs used in it

2. Anti-Epileptic Drugs Classification of anti-anxiety drugs

3. Anti-Epileptic Drugs Phenytoin

• It is the drug of choice for grand mal epilepsy and generalized seizures
• Adverse effects
  • Insomnia, headache, giddiness
  • Gingival hyperplasia
  • Produces fetal hydantoin syndrome in pregnancy characterized by deft lip and palate and microcephaly
  • Hirsutism
  • Megaloblastic anaemia
• Used to treat digitalis-induced ventricular arrhythmias

Read And Learn More: Pharmacology Question and Answers

4. Anti-Epileptic Drugs Carbamazepine

• Used in
  • Temporal lobe epilepsy
  • Grand mal epilepsy
  • Trigeminal neuralgia

5. Anti-Epileptic Drugs Diazepam

• Useful in
  • Acute pain
  • Anxiety
  • Status epileptics
• Has a high therapeutic index
• Dose: 2-5 mg BID

Anti-Epileptic Drugs Long Essays

Question 1. Classify the drugs used in epilepsy. Write the mechanism of action and adverse effects of diphenylhydantoin sodium.

Answer:

Anti-Epileptic Drugs:

• Anti-epileptic drugs are used during epilepsy.

Anti-Epileptic Drugs Classification:

1. Barbiturate – phenobarbitone, mephobarbitone.
2. Deoxybarbiturate – primidone.
3. Hydration – Phenytoin, mephenytoin.
4. Iminostilbene – Carbamazepine, oxcarbazepine.
5. Succinimide – Ethosuximide.
6. Aliphatic carboxylic acid – valproic acid.
7. Benzodiazepine s- Clonazepam. Diazepam.
8. Phenyltriazine – Lamotrigine.
9. Cyclic – GABA analogue – Gabapentin, pregabalin.
10. Newer drugs – Vigabatrin, topiramate.

Diphenylhydantoin/Phenytoin sodium:

• It is a major antiepileptic drug.

Diphenylhydantoin/Phenytoin sodium Mechanism of action:

Diphenylhydantoin/Phenytoin sodium Adverse effects:

1. At therapeutic doses:

• Gum hypertrophy – is common in younger patients.
• Nausea, vomiting, epigastric pain, anorexia.
• Diplopia, ataxia, nystagmus.
• Peripheral neuropathy on prolonged use.
• Hypersensitivity.
• Endocrine disorders – hirsutism, acne, hyperglycaemia, decreased release of ADH, osteomalacia, hypocalcaemia.
• Megaloblastic anaemia, pancytopenia, neutropenia.
• Teratogenicity – causes foetal hydantoin syndrome.

2. At high doses.

• Prominent cerebellar and vestibular effects.
• Drowsiness, hallucinations, mental confusion, delirium, altered behaviour.

Question 2. Enumerate antiepileptic drugs. Mention the actions of phenytoin sodium. How do you manage a case of convulsion precipitated during tooth extraction?

Answer:

Anti-epileptic drugs:

Phenytoin sodium:

• It is a major anti-epileptic drug.

Phenytoin sodium Actions:

• It has CNS actions.

1. Anti-seizure.
2. Effective against generalised tonic-clonic seizures and partial seizures.
3. Doesn’t cause generalised CNS depression.

Management of convulsion precipitated during tooth extraction:

1. Drugs used.

• Diazepam 10 mg IV bolus injection followed by fractional doses every 10 min or slow infusion titrated to control the fits. Or.
• Phenobarbitone 100 – 200 mg 1M/1V or.
• Phenytoin 25 mg/min. IV.

2. Maintain patent airway, oxygen, fluid and electrolyte balance, BP, cardiac rhythm, and care of unconsciousness.

Question 3. Mention the clinical uses of dilantin sodium.

Answer:

Uses of dilantin sodium:

• In generalised tonic-clonic seizures.
• In simple and complex partial seizures.
• Status epilepticus – 25 mg/min, slow IV. Used as an alternative to diazepam.
• Trigeminal neuralgia – second choice of drug, next to carbamazepine.
• Used in digitalis-induced cardiac arrhythmia – 100 mg IV every 10 min or 100 – 200 mg orally 2 – 6 hourly followed by 400 mg/day for maintenance.

Anti-Epileptic Drugs Short Essays

Question 1. Sodium valproate.

Answer:

Sodium valproate is a broad-spectrum anticonvulsant drug.

Sodium valproate Mechanism:

1. Enhances the level of GABA by.

• Increasing its synthesis.
• Decreasing its metabolism.

2. Blocks Na⁺ channels.

• Delays its recovery from inactivated states.

3. Decreases low threshold Ca⁺⁺ current in the thalamus.

Sodium valproate Uses:

• In absence seizures – drug of choice.
• Adjuvant drug for generalized tonic-clonic seizures, simple and complex partial seizures.
• Myoclonic and atonic seizures.
• As a mood stabilizer in bipolar mood disorders.
• Tried as a prophylactic measure in migraine.

Sodium valproate Adverse Effects:

• GIT symptoms – nausea, vomiting, epigastric pain.
• CNS symptoms – Ataxia, drowsiness, tremors. Sedation.
• Rashes, alopecia, curling of hair, increased bleeding.
• Rarely fulminant hepatitis.
• Teratogenicity-neural tube-defects in newborns.

Question 2. Enlist the advantages and disadvantages of tone sodium.

Answer:

Thiopentone sodium:

• It is ultra short-acting thiobarbiturate.

Thiopentone sodium Advantages:

• Highly soluble in water.
• Produces unconsciousness within 15-20 sc.
• Highly lipid soluble.

Thiopentone sodium Disadvantages:

• Poor analgesic.
• Weak muscle relaxant.
• Produces CNS depression.
• Causes respiratory depression.
• Required to prepare freshly every time.
• Extravasation of solution causes intense pain, necrosis and gangrene.

Question 3. Phenytoin sodium in grand mal epilepsy.

Answer:

Phenytoin prolongs the inactivated state of the voltage-sensitive neuronal Na⁺ channel and it also governs the refractory period of the neurons.

• As a result, high-frequency discharges are inhibited with little effect on normal low-frequency discharges.
• It has a stabilizing influence on the neuronal membrane and thus prevents repetitive detonation.
• This stabilizing influence consists of a synchronous and unusually large depolarization over which action potentials are superimposed.
• At high doses.

1. Reduces ^Caz₊ influx.
2. Inhibits glutamate.
3. Facilitates GABA responses.
4. Prevents intracellular accumulation of Na⁺ occurring during repetitive firing.

• Therefore, phenytoin sodium is used in grand mal epilepsy.

Question 5. BDZ (benzodiazepines) as anticonvulsants.

Answer:

• Benzodiazepine have useful anticonvulsant property

Benzodiazepine Mechanism of Action:

• Inhibits GABA metabolism
• Enhances GABA-mediated inhibition
• At large doses, high-frequency discharges are inhibited

Anti-Epileptic Drugs Short Question And Answers

Question 1. Phenobarbitone.

Answer:

Phenobarbitone is an important drug used in epilepsy.

• It inhibits the neurotransmitter’s action by enhancing the GABA receptors thus facilitating them to open chloride ion channels.
• It raises the seizure threshold and thus prevents epileptic attacks.
• It is preferred due to its efficacy and low cost.

Phenobarbitone Uses:

• Generalized tonic-clonic seizures.
• Partial seizures.

Question 2. Carbamazepine.

Answer:

Carbamazepine is anti-epileptic drug.

Carbamazepine Uses:

• Epilepsy – generalized tonic-clonic seizure and partial seizures.
• Neuralgia – trigeminal and glossopharyngeal neuralgia.
• Manic depressive illness and acute mania.
• Chronic neuropathic pain.

Carbamazepine Adverse effects:

• Dose-related neurotoxicity – sedation, dizziness vertigo, diplopia and ataxia.
• GIT disturbance, vomiting, diarrhoea.
• Hypersensitivity reactions – rashes, photosensitivity agranulocytosis, aplastic anaemia.
• Minor foetal abnormalities.

Question 3. Sodium valproate.

Answer:

Sodium valproate Uses:

• In absence seizures – drug of choice.
• Adjuvant drug for generalized tonic-clonic seizures, simple and complex partial seizures.
• Myoclonic and atonic seizures.
• As a mood stabilizer in bipolar mood disorders.
• Tried as a prophylactic measure in migraine.

Sodium Valproate Adverse Effects:

• GIT symptoms-nausea, vomiting, epigastric pain.
• CNS symptoms – Ataxia, drowsiness, tremors. Sedation.
• Rashes, alopecia, curling of hair, increased bleeding.
• Rarely fulminant hepatitis.
• Teratogenicity – neural tube defects in newborns.

Question 4. Phenytoin sodium/Dipbenyl hydantoin sodium.

Answer:

Diphenyihydantoin/Phenytoin sodium:

It is a major antiepileptic drug

Diphenyihydantoin/Phenytoin sodium Adverse effects:

1. At therapeutic doses:

• Gum hypertrophy – is common in younger patients.
• Nausea, vomiting epigastric pain, anorexia.
• Diplopia, ataxia, nystagmus.
• Peripheral neuropathy on prolonged use.
• Hypersensitivity.
• Endocrine disorders – hirsutism, acne, hyperglycaemia, decreased release of ADH, osteomalacia, hypocalcaemia.
• Megaloblastic anaemia, pancytopenia, neutropenia.
• Teratogenicity – causes foetal hydantoin syndrome.

2. At high doses.

• Prominent cerebellar and vestibular effects.
• Drowsiness, hallucinations, mental confusion, delirium, altered behaviour.

Question 5. Phenytoin sodium contra-indicated in pregnancy.

Answer:

Phenytoin sodium causes teratogenicity. When taken by the pregnant lady.

• It produces foetal hydantoin syndrome.
• It is characterized by.

1. Hypoplastic phalanges.
2. Cleft palate.
3. Harelip.
4. Microcephaly.

Question 6. Adverse effects of Phenytoin.

Answer:

1. Phenytoin At therapeutic doses

• Gum hypertrophy
• Nausea, vomiting epigastric pain
• Diplopia
• Ataxia, nystagmus
• Hypersensitivity
• Peripheral neuropathy
• Endocrine disorders: hirsutism, acne, hyperglycaemia
• Megaloblastic anaemia, pancytopenia, neutropenia
• Teratogenicity

2. Phenytoin At high doses

• Prominent cerebellar and vestibular effects
• Drowsiness, hallucinations, mental confusion, delirium, altered behaviour

Question 7. Name three uses and three adverse effects of Diazepam.

Answer:

Diazepam Uses:

• Status epilepticus
  • 5-10 mg IV every 10-15 min upto 30 mg
• IV anaesthesia
  • Dose – 0.2-0.5 mg/kg IV
• For conscious sedation
  • 1-2 mg IV is given in repeated doses or by slow infusion until the desired level of sedation is achieved
• As sedative and hypnotic
• Centrally acting skeletal muscle relaxant
• Combined with analgesic
• As antiepileptic

Diazepam Adverse Effects:

• Drowsiness
• Confusion
• Amnesia
• Impaired motor coordination
• Blurred vision
• Ataxia
• Headache

Question 8. Enlist three adverse effects of Sodium Valproate.

Answer:

• GIT symptoms – nausea, vomiting, epigastric pain
• CNS symptoms – ataxia, drowsiness, tremors, sedation
• Rashes, alopecia, curling of hairs, increased bleeding
• Teratogenicity – neural tube defects in newborns

Alcohol Short Essays

Question 1. Ethyl alcohol is used in methyl alcohol poisoning. Why?

Answer:

Methyl alcohol is converted to formaldehyde by alcohol dehydrogenase.

• This formaldehyde is converted to formic acid by alkaline dehydrogenase.
• Formic acid is the toxic metabolite of methyl alcohol which leads to.
• Vomiting, headache, vertigo, severe abdominal pain, hypotension, delirium, acidosis, and coma.
• To treat it ethyl alcohol-loading dose of 0.6 g/kg is given followed by an infusion of lOg/hour.

The action of ethyl alcohol:

• It competes with methyl alcohol for alcohol dehydrogenase as it has a high affinity for it
• Saturates the enzymes.
• Prevents the formation of toxic metabolites like formaldehyde and formic acid.
• Slows down the metabolism of methanol.
• Thus, methanol gets excreted unchanged in the urine.

Alcohol Short Question And Answers

Question 1. Ethyl alcohol/ethanol.

Answer:

Ethyl alcohol is monohydroxy alcohol manufactured by the fermentation of sugar.

• It is a colorless, volatile, inflammable liquid.

Ethyl alcohol/ethanol Used:

• As an antiseptic and disinfectant
• Counter-irritant for sprains, and joint pain.
• Prevent bedsores.
• Reduces body temperatures via sponges.
• Treats interactable neuralgia like trigeminal neuralgia.
• As appetite stimulant
• To treat methanol poisoning.

Question 2. Methyl alcohol/methanol.

Answer:

Methanol is a CNS depressant

• It is metabolized to formaldehyde and formic acid by alcohol and alkaline dehydrogenase.
• Methanol poisoning occurs mainly due to formic acid.
• It follows zero-order kinetics.
• The plasma half-life is 20 – 60 hours.

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Methyl alcohol/methanol Uses:

• To denatured ethyl alcohol.
• No therapeutic use.

Question 3. Methanol poisoning.

Answer:

Methanol poisoning occurs due to toxic metabolites of methanol.

Methanol poisoning Manifestations:

• Vomiting.
• Headache, vertigo, delirium.
• Severe abdominal pain, and hypotension.
• Acidosis coma.
• Retinal damage, blindness.
• Death due to respiratory failure.

Methanol poisoning Treatment:

• Protection of eyes from light
• Gastric lavage with sodium bicarbonate.
• IV sodium bicarbonate infusion to treat acidosis.
• Maintain ventilation and BP.
• Potassium chloride infusion to treat hypokalemia.
• Ethanol is used to reduce the generation of toxic metabolites.
• Hemodialysis is a severe case.
• Fomepizole is an antidote. It is an inhibitor of alcohol dehydrogenase.
• Folate therapy. Calcium leucovorin injected repeatedly reduces blood formate levels.

B Pharmacy Important Questions Sedative And Hypnotics Important Notes

1. Sedative And Hypnotics Classification of barbiturates

• Long-acting
  • Phenobarbitone
  • Mephobarbitone
• Short-acting
  • Pentobarbitone
  • Secobarbitone
  • Butobarbitone
• Ultra short-acting
  • Thiopentone
  • Hexobarbitone
  • Methohexitone

2. Classification of sedatives and hypnotics Newer benzodiazepine hypnotics

3. Sedative And Hypnotics Benzodiazepines

• They have a high therapeutic index
• Causes less distortion of sleep
• Do not alter the disposition of other drugs
• Lowers abuse liability
• Withdrawal symptoms are less marked
• Do not affect respiration or cardiovascular functions

4. Sedative And Hypnotics Thiopentone sodium

• It is ultra short-acting
• When injected 4 as 2.5% solution, it produces unconsciousness in 15-20 sec
• Its undissociated form has high lipid solubility and enters the brain almost instantly

Read And Learn More: Pharmacology Question and Answers

B Pharmacy Important Questions Sedative And Hypnotics Long Essays

Question 1. Classify hypnotics. Mention the mechanism, actions, and management of barbiturates.

Answer:

Hypnotics Classification:

1. Hypnotics Barbiturates.

• Long-acting – Phenobarbitone
• Short-acting – Pentobarbitone.
• Ultrashort acting – Thiopentone sodium.

2. Hypnotics Benzodiazepine.

3. Hypnotics Newer hypnotics.

• • Zopiclone, Zolpidem, Zaleplon.

Newer hypnotics Barbiturates:

• Barbiturates are drugs derived from barbituric acid. They are non-selective CNS depressants

Barbiturates Mechanism of Action:

Barbiturate
↓
Bind of GABAa receptor Cl- Channel complex.
↓
Potentiate GABAergic inhibition.
↓
Duration of Cl- channel kept open increases
↓
Increased chloride conductance.
↓
Membrane hyperpolarization.
↓
CNS depression.

Barbiturates Actions:

1. Barbiturates CNS.

• In hypnotic doses, barbiturates induce sleep and prolong the duration of sleep.
• Sedative doses given during the daytime can produce drowsiness, reduction in anxiety, and excitability.
• Barbiturates have anticonvulsant property.
• At higher doses, it produces general anesthesia.

2. Barbiturates Respiration.

• Depresses respiration.

3. Barbiturates CVS.

• Produces a slight decrease in BP and heart rate.

4. Barbiturates Skeletal muscles.

• Depress the excitability of the neuromuscular junction.

5. Barbiturates Kidney.

• The tone and motility of the bowel are decreased.
• Reduces urine flow

Barbiturate poisoning:

• The dosage of barbiturates above 6 -10 g causes acute barbiturate poisoning.

Barbiturate poisoning Management:

• Maintain airway, BP, adequate ventilation, and oxygen administration.
• Maintain blood volume by fluid infusion.
• Use of vasopressor.
• Gastric lavage.
• Hemodialysis is done in severe cases.
• Forced alkaline diuresis with mannitol, frusemide, or sodium bicarbonate is done.

Question 2. Describe the Barbiturate’s uses and adverse effects.

Answer:

Barbiturates:

Barbiturates Uses:

• As pre-anesthetic medication.
• As sedative and hypnotic.
• Thiopentone is used for induction of general anesthesia.
• Phenobarbitone is used in epilepsy.
• Used in the treatment of congenital non-hemolytic jaundice.
• Occasionally employed as an adjuvant in psychosomatic disorders.

Barbiturates Adverse Effects:

1. CNS effects.

• Hangover, mental confusion, impaired performed traffic accidents, distortions of mood.

2. Respiratory.

• Respiratory depression occurs.

3. Hypersensitivity.

• Skin rashes and swelling of the eyelids and lips occur.

4. Tolerance and dependence develop.

5. Withdrawal symptoms.

• Anxiety, restlessness, abdominal cramps, hallucinations, delirium, and convulsions occur.

6. Idiosyncrasy.

7. Megaloblastic anemia – due to prolong used of phenobarbitone.

Question 3. Classify barbiturates. Discuss thiopentone sodium.

Answer:

Barbiturates Classification:

1. Long-acting:

• Phenobarbitone, mephobarbitone.

2. Short-acting.

• Pentobarbitone, butobarbitone.

3. Ultra-short acting.

• Thiopentone, Hexobarbltone, Methohexltone.

Thiopentone sodium:

• Thiopentone sodium is ultra short-acting thiobarblturate

Thiopentone sodium Onset of Action:

• 15-20 sec.

Thiopentone sodium Duration of Action:

• 4 – 7 min.

Thiopentone sodium Properties:

• Highly soluble in water.
• Produces unconsciousness in 15 – 20 s.
• Produces CNS depression.
• Poor analgesic.
• Weak muscle relaxant.
• Causes respiratory depression.
• Highly lipid soluble.
• Prepared freshly before use.
• Extravasation of solution causes Intense pain, necrosis, and gangrene.

Thiopentone sodium Uses:

• Common inducing agent
• Used for short non-painful operations.
• Used to control convulsions.
• Adverse effects:
• Laryngospasm.
• Shivering.
• Deliriums

Thiopentone sodium Dose:

• Injected IV dosage – 3 – 5 mg/kg as 2 – 5% solution.

Question 4. Discuss the mechanism, actions, uses, and adverse effects of benzodiazepines.

Answer:

Benzodiazepines:

• Benzodiazepines are a group of drugs used for sedatives and hypnotics.

Benzodiazepines Mechanism of Action:

Benzodiazepines bind to the specific site on GABAa – BZD
receptors Cl- Channel complex.
↓
This potentiates the inhibitory effect of GABA.
↓
Leads to an increase in the frequency of opening of Cl Channels.
↓
Increased Cl- conductance.
↓
Membrane hyperpolarization.
↓
CNS depression.

Benzodiazepines Actions:

1. CNS actions.

• Hypnosis – increases the duration of sleep.
• Anxiolytic – reduces anxiety.
• Causes CNS depression.
• Anticonvulsant – increases the seizure threshold.
• Amnesia – produces loss of memory for the events happening after drug administration.

2. Skeletal muscle.

• Reduces muscle tone.

3. CVS action.

• At high doses, it decreases BP and heart rate.

4. GIT.

• Decreases gastric acid secretion.

5. Respiration.

• At high doses, causes respiratory depression.

Benzodiazepines Uses:

• As hypnotic – to treat insomnia.
• As anxiolytic – to reduce anxiety.
• As anticonvulsant – 4 diazepam is used.
• As a centrally-acting muscle relaxant
• As pre-anesthetic medication.
• IV midazolam or diazepam is used as an intravenous anesthetic.
• For minor procedures.
• For initial control of mania.
• During alcohol withdrawal.
• Along with analgesics, NSAIDs, spasmolytics, antiulcer, and many other drugs.

Benzodiazepines Adverse effects:

• Benzodiazepines are well-tolerated drugs.
• Common side effects are.
  • Drowsiness, dizziness, vertigo, ataxia, amnesia.
  • The blurring of vision.
  • Dry mouth, sweating.
  • Headache, daytime sedation.
  • Tolerance and dependence.
  • Drug given during labor causes hypotonia and respiratory depression in new-born.

Question 5. Define sedative hypnotics classify. What are the advantages of benzodiazepines over barbiturates as sedative-hypnotics?

Answer:

Definition:

Sedative:

A sedative is a drug that reduces excitement and calms the subject without inducing sleep.

Hypnotics:

Hypnotic is a drug that induces and/or maintains sleep similar to normal sleep.

Advantages of Benzodiazepine over barbiturates:

• Benzodiazepine has a high therapeutic index.
• It induces sleep similar to natural sleep.
• Hypnotic doses do not affect respiration or cardiovascular functions.
• BZDs have practically no action on another body system.
• Causes less distortion of sleep architecture.
• Do not cause microsomal enzyme induction.
• Do not alter the blood level of other drugs.
• Have low abuse liability.
• Tolerance is mild.
• Psychological and physical dependence is less marked.
• Specific BZD antagonist flumazenil is present to use in the cause of poisoning.
• The rebound phenomenon is less marked.

Sedative And Hypnotics Short Essays

Question 1. Classify barbiturates. Write it dose.

Answer:

Barbiturates:

• Barbiturates are non-selective CNS depressants.

Barbiturates Classification:

1. Long-acting.

• Phenobarbitone, mephobarbitone.

2. Short acting.

• Pentobarbitone, secobarbitone, Butobarbitone.

3. Ultra-short acting.

• Thiopentone, methohexitone, and hexobarbitone.

Barbiturates Dose:

• The dose depends on lipid solubility.
• Higher lipid solubility indicates a lower dose.

Barbituratesv Examples:

Question 2. Uses of benzodiazepines (BZDs).

Answer:

Benzodiazepines Uses:

1. As hypnotics

• BZDs are used to treat insomnia.
• They shorten sleep latency and reduce nocturnal awakening.
• In dentistry, it is used to ensure sleep the night before the dental procedure in an apprehensive patient.

2. As anxiolytics and for daytime sedation.

• Reduces anxiety.
• Produces calming effects.

3. As an anticonvulsant

• Increases seizure threshold.
• Used especially in emergency control of status epileptic- cities, febrile convulsions, tetanus, etc

4. Muscle relaxant

• BZDs reduce muscle tone by centrally acting.
• Reduces muscle tone and aches associated with anxiety.

5. As IV anesthesia.

• BZDs induce, maintain and supplement anesthetic

6. As pre-anesthetic medication.

• Used due to its sedative and anxiolytic effects.

7. During alcohol withdrawal

• Reduces the intensity of withdrawal symptoms.
• an In minor procedures like endoscopies, fracture reduction, and cardiac catheterization.

9. In psychiatry.

• For initial control of mania.

Question 3. Barbiturate poisoning.

Answer:

Barbiturate poisoning:

• The dosage of barbiturates above 6 – 10 g causes acute barbiturate poisoning.

Barbiturate poisoning Manifestations:

• Excessive CNS depression.
• Respiration depression with slow and shallow breathing.
• Hypotension.
• Bullous eruptions.
• Cardiovascular collapse.
• Renal shutdown.
• Pulmonary complications.

Question 4. Benzodiazepine as pre-anesthetic medication.

Answer:

Benzodiazepine is used for pre-anesthetic medication because it

• Reduces anxiety.
• Produces sedation.
• Produces amnesia.
• Relieves post-operative pain.
• Make anesthesia safer.
• Sraoothens induction with little respiratory depression.
• Reduces side effects of anesthesia like gastric acidity.
• Diazepam 5 -10 mg is given orally.

Sedative And Hypnotics Short Answers

Question 1. Flumazenil.

Answer:

Flumazenil is benzodiazepine antagonist

• It rarely is a benzodiazepine antagonist
• It rarely induces seizures.
• Its action starts seconds after IV administration and lasts for 1 – 2 hours.

Flumazenil Mechanism:

• It competes with BZD agonists and reverses depressant effects.
• Competes with inverse agonists for BZD receptor and reverses stimulant effects.
• It abolishes the hypnogenic, psychomotor, cognitive, and EEC effects of BZD.

Flumazenil Uses:

• To reverse actions of BZD.
• In benzodiazepine overdosage or poisoning.

Question 2. Define sedatives, hypnotics, and tranquilizers.

Answer:

Sedative:

A sedative is a drug that reduces excitement and calms the subject without inducing sleep.

Hypnotics:

Hypnotic is a drug that induces and/or maintains sleep similar to normal sleep.

Tranquilizer:

• It is an old term.
• It means a drug that reduces mental tension and produces calmness without inducing sleep or depressing mental faculties.

Question 3. Urine should be alkalized in acute barbiturate poisoning? Why?

Answer:

The dosage of barbiturates above 6 -10 g causes acute barbiturate poisoning.

• There is no specific antidote for it, only an alkaline diet- sis is the main treatment for it.
• It is done with mannitol, sodium bicarbonate, and frusemide.
• Barbiturates are weakly acidic drugs.
• But in alkaline urine, they exist in ionized form.
• Thus, they are not reabsorbed while passing through renal tubules.
• As a result, they are rapidly excreted in the urine.

Question 4. Midazolam

Answer:

• It is an ultra-short-acting benzodiazepine
• Duration of action is < 6 hours
• Dose: 7.5-10 mg
• It is used as IV anesthesia because
  • It is faster
  • Short-acting
  • More potent
  • Does not cause respiratory and CVS depression
  • Does not cause pain or irritation at the injection site
  • Used as an adjuvant to general anesthesia

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

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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:

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• 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.

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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

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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.

Read And Learn More: Pharmacology Question and Answers

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.