LUQMAN COLLEGE OF PHARMACY, GULBARGA

MEDICINAL CHEMISTRY-I – 3^RD B-Pharm (75 Hours)

First Sessional

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Topic

Sub Topic

Hours

01.

Chapter No-01

Chapter No-02

Chapter No-03

Central nervous system depressants

Local anesthetic

Analgesic agents

A. General anesthetics:

1. Inhalation anesthetics: Halothane, Methoxy flurane,

Nitrous oxide.

2. Ultra short acting barbiturates: Methohextial sodium,

Thiopental sodium.

3. Dissociative anaesthtics: Ketamine hydrochloride.

B. Anxiolytic, sedative and hypnotic agents:

1. SAR of Benzodiazpine Chloriazepoxide, Diazepam, Oxazepam, Chlorazepam, Lorazepam, Flurazepam, Alprazolam.

2. SAR of Barbiturates:

a) Barbital, methabarbital, Phenobarbital,

b) Amobarbital, Butabarbital,

c) Pentobarbital, Secobarbital

3. Miscellaneous sedative hypnotics:

a) Amides and Imides: Glutehmide, Methprylon, Methaqualone.

b) Alcohols and their carbomate derivatives: Ethchlorvynol, Ethinamate, Meprobomate.

c) Aldehydes and their derivatives: Chloral hydrate, paraldehyde.

d) Skeletal muscle relaxants: Chlorphensin, Methocarbamol,

e) Drugs used in spasticity: Baclofen, Buspirone.

f) Anticonvulsants:

1. Mechanism of anticonvulsant action.

2. Barbiturates ; Phenobarbitone.

3. Hydantoins : phenytoin sodium, Ethitoin, Mephenytoin.

4. Oxazolidine diones : Trimethadone, Paramethadone.

5. Succinimides : Phensuximides, Methsuximide, Ethosuximide, Trimethadone.

6. Urea and monoacylureas : Phenacetamide,

7. Miscellaneous : Primidone, Valproic acid.

8. Benzodiazepines : Clonazepam, Diazepam, Chlorazepam.

Local anaesthetics

a) Histroical development, mechanism of action of local anaesthetics.

b) SAR of- Benzoic acid derivatives, Lidocaine derivatives.

c) 1. Benzoic acid derivatives, Hexylcaine, Cylomethycaine, Pierocaine.

2. Amino benzoic acid derivatives: Benzocaine, Procaine, Procainanmide.

3. Lidocaine derivatives (Anilides): Lidocaine,Prilocaine.

4. Miscellaneous: Dimethisoquin, Dibucaine. Carbamazepam.

Analgesic agents

A) Structure and use of morphine, codeine and diacetyl morphine.

b) Narcotic Antagonists: Structure and uses of Nalorphine, Levalorphan.

c) Antitussive agents: Structure and uses of Noscapine, Dextromethorphan.

d) Peripheral and Nuclear modification of Morphine.

e) Anti-Inflammatory agents.

1. Salicylic acid derivatives: Sodium Salicylate.

2. N-aryl anthranilic derivatives: mefenimic acid, diclofenac sod.

3. Aryl Acetic acid derivatives:

Indomethacin,Ibuprofen, Piroxican.

4. aniline and p.aminophenol derivatives: , acetaminophen phenacetin

5. pyrazololone and pyrazolidinedione: Antipyrin, aminopyrin, oxypenbutazone, phenylbutazone

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Second Sessional

Sl.No.

Chapter No

Topic

Sub Topic

Hours

Chapter No-04

Adrenergic agents:

a) Adrenergic neurotransmitters: function structure and

physicochemical Properties, biosynthesis and

metabolism of noradrenaline.

b) Adrenergic receptors: alpha and beta-adrenergic

receptors, their distribution in the human body.

c) Sympathomimetic agents:

1. Direct acting agents; Definition and examples:

Phenylethylamine, Noradrenaline.

2. Indirect acting agents: Definition and example:

Isoproterneol, Trbutalin.

3. Agents with mixed mechanism : examples: Clonidine.

4. Alpha Adrenergic receptor agonists:

Example: Ergotamine.

5. Beta Adrenergic receptor agonists:

Example Pseudoephidrine.

6. Aliphatic amines: Triaminoheptane, Cyclopentamine,

7. Imidazoline derivatives : Naphazoline, Tetrahydrazoline,

Oxymetazoline, Xylometaxazoline.

D) Adrenergic blocking agents

1. Neuronal blocking agents: Alpha-Adrenergic blocking agents –ergot alkaloids

2. Beta halo alkyl amines: Dibenzamine, Phenoxybenzamine.

3.Imidazolines: Talazoline, Phentolamine, Prazocin.

4. Beta Adrenergic blocking agents: Propanlol, 4-hydroxy propranolol practolol, Metaprolol.

(02 Hours)

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Chapter No-05

Cholinergic drugs and related agents

Cholinergic drugs and related agents

1. Cholinergic neurotransmitter: function, structure, physiochemical properties, biosynthesis and metabolism of Acetylcholine. Cholinergic receptors: muscarnic and nicotinic receptor, their distribution in the human body.

2. Indirectly acting Cholinergic agonists:

a) Cholinestrase inhibitors: Physostigmine, Neostigmine, Pyridostigmine.

b) Irreversible inhibitors : Malathion, Parathion.

b) Cholinergic blocking agents: Parasympathetic Postganglionic blocking agents: Atropine, Hyoscyamine, Scoplamine, Homatropine, Methscopolamine.

C) Synthesis Cholinergic blocking agents: Cidinium bromide, Dicyclomine, Propantheline, Benzotropine Chlorphenoxamine,

d) Ganglionic blocking agents: Trimethaphan camsylate, Mecamylamine.

e) Neuromuscular blocking agents: d-Tubocurarine chloride, Metocurine iodide synthetic compounds with curare form activity-Decamethonium bromide.

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Third Sessional

Sl.No		Chapter No	Topic	Sub Topic	Hours
06 07		Chapter No-06 Chapter No-07	Basic Principles Medicinal Chemistry Prostaglandins and other Eicosaniods	A) A brief introduction to the subject, history and development of medicinal Chemistry, definition and fundamental principal of drug therapy. B) Effects of the following physicochemical properties of drug molecules on biological activity: Solubility, partition coefficient, hydrogen bonding, protein binding, chelation, Geometrical and potical isomers, redox potential, ionization and surface activity. C) Principles of drug design (theoretical aspects) General principles of drug action and drug receptor interaction. D) Drug metabolism: General pathways of drug metabolism, sites of drug biotransformations, role of cytochrome P-450 and monoaminooxygenase in oxidative biotransformations. Oxidative, reductive, hydrolytic and conjugation reaction. Factors affecting drug metabolism. E) Study of the development of the following classes of drugs including structure activity realationship (SAR),mechanisms of action, synthesis of compounds underlined and superscribed by “s” chemical nomenclature, generic, names, brand names (a few important markted products and side effects. a) History and discovery b) Eicosaniods biosynthesis c) Drug action mediated by Eicosaniods. d) Design of Eicosaniods drug. e) Eicosaniods approved for human clinical use. f) Prostaglandin F2 a, Prostaglandin E2,15-(s)-methyl-PG. F2 a Prostaglandin E1, 16-(R,S) methyl-16-hydroxy-methyl ster.	(02Hours) (06Hours) (02Hours) (07Hours) (05Hours)
08	Chapter No-08		Histamines and anti histaminic agents	a) Histamine, receptors and their distribution in the human body. b) Antihistaminic agents: H1 antagonists. 1) Amino alkyl eithers: Diphenhydramine hydrochloride, Bromodiphenhydramine, Doxylamine. 2) Ethylene diamines: Tripelennamine, Pyrilamine. 3) Peopylamine derivatives: Pheniramine, Chlorpheniramine. 4) Phenothiazine derivatives: Promethazine, Trimeprazine. 5) Piperazine derivatives: Cyclizine, Meclizine. 6) Miscellaneous compounds : Phenindamine, Cyproheptidine.C H2-Antogonists: Mechanism of H2-Antogonists Cemetidine, Rantidine. Gastric proton pump inhibitor-an introduction Omeprazole.	(03Hours)