JAWAHARLAL NEHRU TECHNOLOGICAL UNIVERSITY HYDERABAD

Course Objective

This subject is designed to impart fundamental knowledge on the structure,

chemistry and therapeutic value of drugs. The subject emphasizes on structure activity relationships of drugs, importance of physicochemical properties, absorbtion, distribution and metabolism of drugs. The syllabus also emphasizes on chemical synthesis of important drugs under each class.

Course Outcomes

Upon completion of the course the student shall be able to

• 1. Understand the chemistry of drugs with respect to their pharmacological activity
• 2. Understand the drug metabolic pathways, adverse effect and therapeutic value of drugs
• 3. Know the Structural Activity Relationship of different class of drugs
• 4. Study the chemical synthesis of selected drugs Study of the development of the following classes of drugs, Classification, mechanism of action, uses of drugs mentioned in the course, Structure activity relationship of selective class of drugs as specified in the course and synthesis of drugs superscripted (*)

UNIT - I

Antihistaminic agents: Histamine, receptors and their distribution in the humanbody H1–antagonists: Diphenhydramine hydrochloride*, Dimenhydrinate, Doxylamines succinate, Clemastine fumarate, Diphenylphyraline hydrochloride, Tripelenamine hydrochloride, Chlorcyclizine hydrochloride, Meclizine hydrochloride, Buclizine hydrochloride, Chlorpheniramine maleate, Triprolidine hydrochloride*, Phenidamine tartarate, Promethazine hydrochloride*, Trimeprazine tartrate, Cyproheptadine hydrochloride, Azatidine maleate, Astemizole, Loratadine, Cetirizine, Levocetrazine Cromolyn sodium H2-antagonists: Cimetidine*, Famotidine, Ranitidin. Gastric Proton pump inhibitors: Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole Anti-neoplastic agents: Alkylating agents: Meclorethamine*, Cyclophosphamide, Melphalan, Chlorambucil, Busulfan, Thiotepa Antimetabolites: Mercaptopurine*, Thioguanine, Fluorouracil, Floxuridine, Cytarabine, Methotrexate*, Azathioprine Antibiotics: Dactinomycin, Daunorubicin, Doxorubicin, Bleomycin Plant products: Etoposide, Vinblastin sulphate, Vincristin sulphate Miscellaneous: Cisplatin, Mitotane.

UNIT - II

Anti-anginal: Vasodilators: Amyl nitrite, Nitroglycerin*, Pentaerythritol tetranitrate, Isosorbide dinitrite*, Dipyridamole. Calcium channel blockers: Verapamil, Bepridil hydrochloride, Diltiazem hydrochloride, Nifedipine, Amlodipine, Felodipine, Nicardipine, Nimodipine. Diuretics: Carbonic anhydrase inhibitors: Acetazolamide*, Methazolamide, Dichlorphenamide. Thiazides: Chlorthiazide*, Hydrochlorothiazide, Hydroflumethiazide, Cyclothiazide, Loop diuretics: Furosemide*, Bumetanide, Ethacrynic acid. Potassium sparing Diuretics: Spironolactone, Triamterene, Amiloride. Osmotic Diuretics: Mannitol Anti-hypertensive Agents: Timolol, Captopril, Lisinopril, Enalapril, Benazepril hydrochloride, Quinapril

R17 B. PHARMACY III YEAR

hydrochloride, Methyldopate hydrochloride,* Clonidine hydrochloride, Guanethidine monosulphate, Guanabenz acetate, Sodium nitroprusside, Diazoxide, Minoxidil, Reserpine, Hydralazine hydrochloride.

UNIT - III

Anti-arrhythmic Drugs: Quinidine sulphate, Procainamide hydrochloride, Disopyramide phosphate*, Phenytoin sodium, Lidocaine hydrochloride, Tocainide hydrochloride, Mexiletine hydrochloride, Lorcainide hydrochloride, Amiodarone, Sotalol. Anti-hyperlipidemic agents: Clofibrate, Lovastatin, Cholesteramine and Cholestipol Coagulant & Anticoagulants: Menadione, Acetomenadione, Warfarin*, Anisindione, clopidogrel Drugs used in Congestive Heart Failure: Digoxin, Digitoxin, Nesiritide Bosentan, Tezosentan.

UNIT - IV

Drugs acting on Endocrine system Nomenclature, Stereochemistry and metabolism of steroids Sex hormones: Testosterone, Nandralone, Progestrones, Oestriol, Oestradiol, Oestrione, Diethyl stilbestrol. Drugs for erectile dysfunction: Sildenafil, Tadalafil. Oral contraceptives: Mifepristone, Norgestril, Levonorgestrol Corticosteroids: Cortisone, Hydrocortisone, Prednisolone, Betamethasone, Dexamethasone Thyroid and antithyroid drugs: L-Thyroxine, L-Thyronine, Propylthiouracil, Methimazole.

UNIT - V

Antidiabetic agents: Insulin and its preparations Sulfonyl ureas: Tolbutamide*, Chlorpropamide, Glipizide, Glimepiride. Biguanides: Metformin. Thiazolidinediones: Pioglitazone, Rosiglitazone. Meglitinides: Repaglinide, Nateglinide. Glucosidase inhibitors: Acarbose, Voglibose. Local Anesthetics: SAR of Local anesthetics Benzoic Acid derivatives; Cocaine, Hexylcaine, Meprylcaine, Cyclomethycaine, Piperocaine. Amino Benzoic acid derivatives: Benzocaine*, Butamben, Procaine*, Butacaine, Propoxycaine, Tetracaine, Benoxinate. Lidocaine/Anilide derivatives: Lignocaine, Mepivacaine, Prilocaine, Etidocaine. Miscellaneous: Phenacaine, Diperodon, Dibucaine.*

Recommended Books (Latest Editions)

• 1. Wilson and Giswold’s Organic medicinal and Pharmaceutical Chemistry.
• 2. Foye’s Principles of Medicinal Chemistry.
• 3. Burger’s Medicinal Chemistry, Vol I to IV.
• 4. Introduction to principles of drug design- Smith and Williams.
• 5. Remington’s Pharmaceutical Sciences.
• 6. Martindale’s extra pharmacopoeia.
• 7. Organic Chemistry by I.L. Finar, Vol. II.
• 8. The Organic Chemistry of Drug Synthesis by Lednicer, Vol. 1to 5.
• 9. Indian Pharmacopoeia.
• 10. Text book of practical organic chemistry- A.I.Vogel. R17 B. PHARMACY III YEAR