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Overview of Key Pharmacological Concepts

The document provides an overview of various pharmacological concepts, including M3 receptors, classifications of drugs, and specific drug actions and uses. It discusses the roles of different drug classes, adverse effects, and therapeutic applications, along with comparisons between similar medications. Additionally, it covers important topics like pharmacogenomics, pharmacovigilance, and the management of specific medical conditions.

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0% found this document useful (0 votes)
81 views1 page

Overview of Key Pharmacological Concepts

The document provides an overview of various pharmacological concepts, including M3 receptors, classifications of drugs, and specific drug actions and uses. It discusses the roles of different drug classes, adverse effects, and therapeutic applications, along with comparisons between similar medications. Additionally, it covers important topics like pharmacogenomics, pharmacovigilance, and the management of specific medical conditions.

Uploaded by

palak7789.h81
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd

1.

M3 Receptors:
M3 receptors are primarily located in smooth muscles, glands, and endothelial cells. Their function includes promoting
smooth muscle contraction (e.g., in the gastrointestinal and urinary tracts), stimulating glandular secretions (e.g., saliva),
and causing vasodilation via nitric oxide release in blood vessels.

2. Classification of Parasympathomimetic Drugs:


Direct-acting: Acetylcholine, Pilocarpine, Bethanechol.
Indirect-acting (Cholinesterase inhibitors): Reversible (e.g., Neostigmine, Pyridostigmine) and Irreversible (e.g.,
Organophosphates like Malathion).

3. Role of Atropine in Organophosphorus Poisoning:


Atropine is used to counteract the muscarinic effects of organophosphorus poisoning by blocking acetylcholine at
muscarinic receptors. It helps reduce symptoms like bronchorrhea, bradycardia, and excessive salivation.

4. Malignant Hyperthermia:
It is a rare, life-threatening reaction to certain anesthetics, characterized by hypermetabolism, muscle rigidity, and fever.
The drug of choice for treatment is Dantrolene, which reduces calcium release from the sarcoplasmic reticulum in
muscles.

5. Z-Compounds:
Z-compounds include drugs like Zolpidem, Zaleplon, and Eszopiclone. They are non-benzodiazepine hypnotics with
advantages such as fewer side effects, shorter half-lives, and less risk of dependence compared to benzodiazepines.

6. Meaning of Akathisia and Drugs for Treatment:


Akathisia is a movement disorder characterized by a feeling of inner restlessness and an urge to move. It is often caused
by antipsychotic drugs. Treatment options include Propranolol and Benzodiazepines like Lorazepam.

1. Classification of antiarrhythmic drugs:

Class I: Sodium channel blockers (e.g., Quinidine, Lidocaine).

Class II: Beta-blockers (e.g., Propranolol, Metoprolol).

Class III: Potassium channel blockers (e.g., Amiodarone, Sotalol).

Class IV: Calcium channel blockers (e.g., Verapamil, Diltiazem).

2. Two osmotic diuretics and their uses:


Examples: Mannitol, Glycerol.
Therapeutic uses:
1. Treatment of cerebral edema.
2. Reduction of intraocular pressure in glaucoma.

3. Two phosphodiesterase inhibitors and their use:


Examples: Milrinone, Amrinone.
Therapeutic use: Used in heart failure to improve cardiac output.

4. Four second-generation antihistamines:


Examples: Loratadine, Cetirizine, Fexofenadine, Levocetirizine.

5. Angiotensin-II receptor and neprilysin inhibitor (ARNI):


Fixed-dose combination: Sacubitril + Valsartan.
Therapeutic use: Used in heart failure with reduced ejection fraction (HFrEF).

6. Two plasma expanders and their use:


Examples: Dextran, Hydroxyethyl starch.
Therapeutic use: Management of hypovolemia in shock or severe blood loss.

(a) Four differences between benzodiazepines and barbiturates:


1. Benzodiazepines enhance GABA action by increasing the frequency of chloride channel opening, while barbiturates
prolong the duration.
2. Benzodiazepines have a higher safety margin; barbiturates have a narrow therapeutic index.
3. Barbiturates are more prone to causing dependence.
4. Benzodiazepines are used as anxiolytics; barbiturates are primarily for anesthesia or epilepsy.

(b) Disulfiram-like reaction with alcohol:


Drugs like metronidazole and cephalosporins inhibit aldehyde dehydrogenase, causing acetaldehyde accumulation.
This leads to symptoms like flushing, nausea, and vomiting when alcohol is consumed.

(c) Zero-order kinetics of elimination:


In zero-order kinetics, drugs are eliminated at a constant rate irrespective of plasma concentration.
Example: Phenytoin and ethanol exhibit zero-order elimination at higher doses.

(d) Dose-dependent action of dopamine:


At low doses, dopamine acts on D1 receptors to cause renal vasodilation.
At moderate doses, it acts on β1 receptors to increase cardiac output
At high doses, it stimulates α1 receptors, causing vasoconstriction.

(e) Pharmacological basis of allopurinol in chronic gout:


Allopurinol inhibits xanthine oxidase, reducing uric acid synthesis.
This decreases uric acid levels, preventing crystal deposition in joints.

(f) Pharmacological basis of contraindication of morphine in head injury:


Morphine increases intracranial pressure by causing CO2 retention and cerebral vasodilation.
This worsens brain edema and neurological outcomes.

(a) Four differences between Verapamil and Nifedipine:


1. Verapamil is a non-dihydropyridine; Nifedipine is a dihydropyridine calcium channel blocker.
2. Verapamil affects both the heart and blood vessels, while Nifedipine predominantly acts on blood vessels.
3. Verapamil decreases heart rate; Nifedipine may cause reflex tachycardia.
4. Verapamil is used in arrhythmias; Nifedipine is preferred for hypertension.

(b) Pharmacological basis of antiplatelet activity of low-dose aspirin:


Aspirin irreversibly inhibits COX-1, blocking thromboxane A2 synthesis.
This reduces platelet aggregation and prevents thrombus formation.

(c) Therapeutic uses and adverse effects of statins:


Therapeutic uses: Treatment of hyperlipidemia and prevention of cardiovascular events.
Adverse effects: Myopathy, liver enzyme elevation, and rhabdomyolysis.

(d) Four differences between Heparin and Warfarin:


1. Heparin acts via antithrombin III; Warfarin inhibits vitamin K-dependent clotting factors.
2. Heparin is used parenterally; Warfarin is oral.
3. Heparin has an immediate onset; Warfarin takes 2–3 days.
4. Heparin is safer in pregnancy; Warfarin is teratogenic.

(e) Define pharmacogenomics and pharmacogenetics with examples:


Pharmacogenomics studies how the genome affects drug response (e.g., cancer treatments like trastuzumab).
Pharmacogenetics focuses on single gene variations affecting drug metabolism (e.g., CYP2C19 polymorphism with
clopidogrel).

(f) Adverse effects of amiodarone:


Pulmonary fibrosis, thyroid dysfunction (hypo- or hyperthyroidism), liver toxicity, and corneal deposits.

1. Signs of Atropinization:
Signs include dry mouth, blurred vision, tachycardia, urinary retention, and flushing. Patients may also experience
photophobia, dry skin, and decreased sweating due to muscarinic receptor blockade.

2. Adverse Effects of Lignocaine:


Common side effects include dizziness, nausea, and drowsiness. At higher doses, it can cause CNS toxicity (seizures,
tremors) and cardiovascular effects like bradycardia or hypotension.

3. Drugs Causing Malignant Hyperthermia and Treatment:


Drugs such as succinylcholine and halothane can trigger malignant hyperthermia. The specific treatment involves
administering dantrolene sodium and supportive measures like cooling and electrolyte management.

4. Drugs with High Plasma Protein Binding:


Examples include warfarin, phenytoin, diazepam, and ibuprofen. These drugs extensively bind to plasma proteins,
affecting their pharmacokinetics.

5. Drugs Requiring Therapeutic Drug Monitoring:


Examples are digoxin and lithium. Monitoring is essential to maintain efficacy and avoid toxicity due to their narrow
therapeutic index.

6. Adverse Effects of Sertraline:


Side effects include nausea, diarrhea, insomnia, and sexual dysfunction. In some cases, it may cause serotonin syndrome
or withdrawal symptoms upon abrupt discontinuation.

1. Pharmacological Basis for Sublingual Glyceryl Trinitrate in Angina:


Glyceryl trinitrate releases nitric oxide, which causes vasodilation and reduces myocardial oxygen demand. Its sublingual
route ensures rapid absorption and onset of action, making it effective for acute angina relief.

2. Drugs Used in Megaloblastic Anemia:


Commonly used drugs include vitamin B12 (cyanocobalamin) and folic acid. These address deficiencies responsible for
defective DNA synthesis in red blood cells.

3. Adverse Effects of Osmotic Diuretics:


Side effects include dehydration, electrolyte imbalance, and pulmonary edema. Rapid administration may also increase
intracranial pressure temporarily.

4. Drugs for Prophylaxis of Migraine:


Prophylactic drugs include propranolol, topiramate, valproate, and amitriptyline. These help reduce the frequency and
severity of migraine attacks.

5. Differences Between Low-Dose and High-Dose Aspirin:


Low-dose aspirin (75–100 mg/day) inhibits platelet aggregation and is used for cardiovascular prevention. High-dose
aspirin (300–600 mg/day) has anti-inflammatory and analgesic effects but carries a higher risk of gastrointestinal side
effects.

6. Prostaglandin Analogues:
Examples include misoprostol, latanoprost, bimatoprost, and dinoprostone. They are used for various purposes, including
labor induction, glaucoma treatment, and gastric ulcer prevention.

1. Compare fentanyl and morphine


Fentanyl: Synthetic opioid, 100 times more potent than morphine, rapid onset, short duration, commonly used in
anesthesia.
Morphine: Natural opioid, longer duration, used for chronic and severe pain.

2. Mechanism of alpha-methyldopa in hypertension


Alpha-methyldopa is converted to alpha-methylnorepinephrine in the CNS. This metabolite acts as a false
neurotransmitter and stimulates central alpha-2 adrenergic receptors, reducing sympathetic outflow and lowering blood
pressure.

3. Compare fluoxetine and imipramine


Fluoxetine: SSRI, selective inhibition of serotonin reuptake, fewer side effects, used in depression, anxiety, and OCD
Imipramine: TCA, inhibits serotonin and norepinephrine reuptake, more sedative, used in depression and nocturnal
enuresis.

4. Define pharmacovigilance
Pharmacovigilance is the science of detecting, assessing, understanding, and preventing adverse drug reactions or other
drug-related problems to ensure safe medication use.

5. Prodrugs and examples


Prodrugs are inactive compounds that are metabolized into active forms in the body.
Examples:
1. Enalapril: Converted to enalaprilat, an active ACE inhibitor for hypertension.
2. Clopidogrel: Metabolized into an active form for antiplatelet action.

6. Beta-blockers in heart failure


Beta-blockers (e.g., Carvedilol, Metoprolol) reduce myocardial oxygen demand, inhibit sympathetic overactivation, prevent
arrhythmias, and improve survival in chronic heart failure.

1. Zero-order kinetics and drugs


In zero-order kinetics, a constant amount of drug is eliminated per unit time, regardless of plasma concentration.
Examples: Phenytoin, Aspirin (high doses), Ethanol.

2. Non-cardiac uses of beta-blockers


Examples:
1. Migraine prophylaxis: Propranolol.
2. Essential tremor: Propranolol.
3. Glaucoma: Timolol (topical).

3. Barbiturates vs. Benzodiazepines


Barbiturates: Longer action, narrow safety margin, high dependence risk, used in epilepsy (e.g., Phenobarbital).
Benzodiazepines: Safer, faster onset, used in anxiety, insomnia, seizures (e.g., Diazepam).

4. Why is Dimercaprol used in heavy metal poisoning?


Dimercaprol chelates heavy metals (e.g., lead, arsenic, mercury) by forming stable complexes that are excreted in the
urine, reducing metal toxicity.

5. Streptokinase and its use


Streptokinase is a fibrinolytic agent that dissolves blood clots. It is used in myocardial infarction, pulmonary embolism,
and deep vein thrombosis.

6. Phase IV clinical trials


Phase IV trials are post-marketing studies to monitor drug safety, detect rare adverse effects, and assess long-term
effectiveness in larger populations

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