BPH-401: PHARMACEUTICAL CHEMISTRY – VIII
(MEDICINAL CHEMISTRY-II)
THEORY
Max. Marks: 80 Total Hours: 50 (2hrs/week)Note: Examiner to set eight questions and the candidates are required to attempt any five.
- Drug Metabolism:Activation of oxygen and electron transport system. Role of cytochrome P-450 monoxygenases. Drug metabolising reactions: phase-I (Oxidative, reductive & hydrolytic) and phase-II (conjugative) reactions. Drug activation and consequences for human health. Factors effecting drug metabolism. Models mimicking drug metabolising enzymes. (4)
- Prodrug Approach: Basic concept. Common pro-moietics. Reversal of prodrugs chemical & enzymatic. Applications of prodrug approach to alter taste and odour, reduction of pain at injection site, reduction of gastrointestinal irritability, alteration of drug stability, increasing chemical stability, prevention of presystemic metabolism, prolongation of drug action, site specific drug delivery, reduction in toxicity, and allernation of drug metabolism. (4)
- Classification, mode of action, uses and structure activity relationship of the following classes of drugs. Study of synthesis of compounds mentioned against each class.
i. Sulphonamides: Sulphadiazine, Sulphamethoxazole, Sulphacetamide Sodium, Sulphurguanidine, Sulphasalazine.
ii. Antibiotics: General study including classification, synthesis of Methicillin, Ampicillin, Amoxycillin and Chloramphenicol, Structure of cloxacilin, clavulanic acid, cephalexin, doxicyclin.
iii. Antifungal agents: Griseofulvin, Nystatin, Ketoconazole, Amphotericin B, Miconazole.
iv. Anti Malarial Drugs: Chloroquine, Primaquine, Mepacrine, Proguanil, Pyrimethamine.
v. Antineoplastic agents: Chlorambucil, Thiotepa, Busulfan, 5-Flurouracil, Cyclophosphomide, Mephalan, Methotraxate.
vi. Anti-TB and anti-leprosy Drugs: Isoniazid, Ethambutrol, Pyrazinamide, Dapsone, Structure of clofazimine and streptomycin.
vii. Antiamoebic agents: Metronidazole, Tinidazole, Diloxanide furoate
viii. Anthelmentics: Thiabendazole, Mebendazole, Niclosamide, Piperazine, Albendazole.
ix. Anti-viral including anti-HIV agents: Acyclovir, Zidovudine
x. Immunosupressives and immunostimulants: To study only the general concept
xi. Diagnostic Agents: Propyliodone, Sodium diatrizoate, Fluorescein sodium.
xii. Anticoagulants: Heparin, Coumarins, Phenindione derivatives.
xiii. Amino acids: Peptide, nucleotides and related drugs.
xiv. Thyroid and Anti thyroid drugs: Thyroxine, Liothyronine, Propythiouracil, Carbimazole
xv. Insulin, Insulin preparations and oral hypoglycaemic agents: Chloropropamide, Tolbutamide, Glibenclamide, Phenformin, Metformine, Tolazamide.
xvi. Cardiovascular Drugs: Clonidine, Methyldopa, Procainamide, Nifedipine, Isosorbide dinitrate, Prazocin, clofibrate.
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