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Unit I: Introduction to Medicinal Chemistry And Drug Metabolism

Syllabus Topics to Learn

Introduction to Medicinal Chemistry: History and development of medicinal chemistry Physicochemical properties in relation to biological action Ionization

Solubility

Partition Coefficient

Hydrogen bonding

Protein binding

Chelation

Bioisosterism

Optical and Geometrical isomerism. Drug metabolism: Drug metabolism principles- Phase I and Phase II. Factors affecting drug metabolism including stereo chemical aspects.

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Unit II: Drugs Acting on the Autonomic Nervous System (Adrenergic Drugs)

Syllabus Topics to Learn

Drugs acting on Autonomic Nervous System Adrenergic Neurotransmitters: Biosynthesis and catabolism of catecholamine. Adrenergic receptors (Alpha & Beta) and their distribution. Sympathomimetic agents: SAR of sympathomimetic agents Direct acting: Nor-epinephrine

Epinephrine

Phenylephrine*

Dopamine

Methyldopa

Clonidine

Dobutamine

Isoproterenol

Terbutaline

Salbutamol*

Bitolterol

Naphazoline

Oxymetazoline and Xylometazoline. Indirect acting agents: Hydroxyamphetamine

Pseudoephedrine

Propylhexedrine. Agents with mixed mechanism: Ephedrine

Metaraminol. Adrenergic Antagonists: Alpha adrenergic blockers: Tolazoline*

Phentolamine

Phenoxybenzamine

Prazosin

Dihydroergotamine

Methysergide. Beta adrenergic blockers: SAR of beta blockers

Propranolol*

Metipranolol

Atenolol

Betazolol

Bisoprolol

Esmolol

Metoprolol

Labetolol

Carvedilol.

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Unit III: Drugs Acting on the Cholinergic System (Cholinergic Drugs)

Syllabus Topics to Learn

Cholinergic neurotransmitters: Biosynthesis and catabolism of acetylcholine. Cholinergic receptors (Muscarinic & Nicotinic) and their distribution. Parasympathomimetic agents: SAR of Parasympathomimetic agents Direct acting agents: Acetylcholine

Carbachol*

Bethanechol

Methacholine

Pilocarpine. Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible): Physostigmine

Neostigmine*

Pyridostigmine

Edrophonium chloride

Tacrine hydrochloride

Ambenonium chloride

Isofluorphate

Echothiophate iodide

Parathion

Malathion. Cholinesterase reactivator: Pralidoxime chloride. Cholinergic Blocking agents: SAR of cholinolytic agents Solanaceous alkaloids and analogues: Atropine sulphate

Hyoscyamine sulphate

Scopolamine hydrobromide

Homatropine hydrobromide

Ipratropium bromide*. Synthetic cholinergic blocking agents: Tropicamide

Cyclopentolate hydrochloride

Clidinium bromide

Dicyclomine hydrochloride*

Glycopyrrolate

Methantheline bromide

Propantheline bromide

Benztropine mesylate

Orphenadrine citrate

Biperidine hydrochloride

Procyclidine hydrochloride*

Tridihexethyl chloride

Isopropamide iodide

Ethopropazine hydrochloride.

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Unit IV: Drugs acting on Central Nervous System

Syllabus Topics to Learn

Drugs acting on Central Nervous System A. Sedatives and Hypnotics: Benzodiazepines: SAR of Benzodiazepines

Chlordiazepoxide

Diazepam*

Oxazepam

Chlorazepate

Lorazepam

Alprazolam

Zolpidem Barbiturates: SAR of barbiturates

Barbital*

Phenobarbital

Mephobarbital

Amobarbital

Butabarbital

Pentobarbital

Secobarbital. Miscellaneous: Amides & imides: Glutethimide. Alcohol & their carbamate derivatives: Meprobamate

Ethchlorvynol. Aldehyde & their derivatives: Triclofos sodium

Paraldehyde. B. Antipsychotics Phenothiazines: SAR of Phenothiazines- Promazine hydrochloride

Chlorpromazine hydrochloride*

Triflupromazine

Thioridazine hydrochloride

Piperacetazine hydrochloride

Prochlorperazine maleate

Trifluoperazine hydrochloride. Ring Analogues of Phenothiazines: Chlorprothixene

Thiothixene

Loxapine succinate

Clozapine. Fluoro buterophenones: Haloperidol

Droperidol

Risperidone. Beta amino ketones: Molindone hydrochloride. Benzamides: Sulpiride. C. Anticonvulsants: SAR of Anticonvulsants

Mechanism of anticonvulsant action. Barbiturates: Phenobarbitone

Metharbital. Hydantoins: Phenytoin*

Mephenytoin

Ethotoin. Oxazolidine diones: Trimethadione

Paramethadione. Succinimides: Phensuximide

Methsuximide

Ethosuximide.* Urea and monoacylureas: Phenacemide

Carbamazepine.* Benzodiazepines: Clonazepam. Miscellaneous: Primidone

Valproic acid

Gabapentin

Felbamate.

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Unit V: Drugs Acting on the Central Nervous System (CNS Drugs)

Syllabus Topics to Learn

General anesthetics: Inhalation anesthetics: Halothane*

Methoxyflurane

Enflurane

Sevoflurane

Isoflurane

Desflurane. Ultra-short acting barbitutrates: Methohexital sodium*

Thiamylal sodium

Thiopental sodium. Dissociative anesthetics: Ketamine hydrochloride. * Narcotic and non-narcotic analgesics Morphine and related drugs: SAR of Morphine analogues

Morphine sulphate

Codeine

Meperidine hydrochloride

Anileridine hydrochloride

Diphenoxylate hydrochloride

Loperamide hydrochloride

Fentanyl citrate*

Methadone hydrochloride*

Propoxyphene hydrochloride

Pentazocine

Levorphanol tartrate. Narcotic antagonists: Nalorphine hydrochloride

Levallorphan tartrate

Naloxone hydrochloride. Anti-inflammatory agents: Sodium salicylate

Aspirin

Mefenamic acid*

Meclofenamate

Indomethacin

Sulindac

Tolmetin

Zomepirac

Diclofenac

Ketorolac

Ibuprofen*

Naproxen

Piroxicam

Phenacetin

Acetaminophen

Antipyrine

Phenylbutazone.

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Subject Overview

Course Code BP402T

Syllabus Status 100% PCI Aligned

Total Units 5 Units

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