Curriculum | MEDICINAL CHEMISTRY – II (Theory) | B. Pharmacy

Course: B. Pharmacy  Vth Semester / 3rd Year

Name of the Subject: MEDICINAL CHEMISTRY – II (Theory)

Subject Code: BP501T

Unit Sub Units Topic Learning Objectives Teaching Guidelines Methodology Time (Hrs)
1 1.1 Antihistaminic agents: Histamine, receptors and their distribution in the human body: Diphenhydramine hydrochloride*, Dimenhydrinate, Doxylamines cuccinate, 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
Describe the definition, classification, mechanism of action, chemistry and Structure Activity Relationship studies of antihistaminic agents and antiulcer drugs. Describe the chemical synthesis of selected drugs marked with asterisk
  • H1 And H2 Receptors
  • H1 antagonist-classification
  • mechanism of action Structure Activity Relationship,
  • H2 antagonist-classification
  • Serotonin And Serotonin antagonists
  • Classification of drugs
  • Mode of action
  • Mechanism
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Instructive
  • Lecture-demonstration by another instructor
  • Power point

Presentation

  • Tutorials
  • Assignment
  • Quiz session
05
  1.2 Anti-neoplastic agents:
Alkylating              agents:
Meclorethamine*,CyclophosphamideMelphalan, 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
To Explain the definition, mechanism of action, classification, chemistry and Structure Activity Relationship studies of antineoplastic agents.
Enumerate the chemical synthesis of some drugs marked with asterisk
  • History of cancer chemotherapy
  • Structures of important alkylating agents
  • Mechanism of action of nitrogen mustards
  • Official compounds and preparation ,description assay ,uses, side effects and dose
  • Classification of drugs
  • Mode of action
  • Mechanism
  • Synthesis
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Antimetabolites agents
  • Natural products used as anticancer agents
  • Instructive
  • Power point presentation
  • Group discussion
  • Presentations by student panels from the class
05
2 2.1 Anti-anginal: Vasodilators: Amyl nitrite, Nitroglycerin*, Pentaerythritol tetranitrate, Isosorbide dinitrite*, Dipyridamole.
Calcium channel blockers: Verapamil, Bepridil hydrochloride, Diltiazem hydrochloride, Nifedipine, Amlodipine, Felodipine, Nicardipine, Nimodipine.
Describe the definition, classification, chemistry and Structure Activity Relationship studies of vasodilators.
Explain the chemical synthesis of selected drugs marked with asterisk
  • Vasodilators
  • Classification of drugs
  • Official compounds and preparation ,description assay ,uses, side effects and dose
  • Pharmacology and biotransformation
  • Synthesis
  • Mode of action
  • Mechanism
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Instructive
  • Power point presentation
  • Tutorials
  • Group discussion
  • Presentations by student panels from the class

 

04
  2.2 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
To Discuss the definition, classification, mechanism of action, chemistry and Structure Activity Relationship studies of Diuretics. To know the chemical synthesis of selected drugs marked with asterisk
  • Introduction
  • Water and osmotic agents
  • Classification of drugs
  • Mode of action
  • Mechanism
  • Synthesis
  • Drug interaction and contraindication
  • Dose and
  • Therapeutic uses of diuretics
  • Structure activity relationship of selective class of drugs
  • Instructive
  • Power point presentation
  • Student reports by individuals
03
  2.3 Anti-hypertensive Agents: Timolol, Captopril, Lisinopril, Enalapril, Benazepril hydrochloride, Quinapril hydrochloride, Methyldopate hydrochloride,* Clonidine hydrochloride, Guanethidine monosulphate, Guanabenz acetate, Sodium nitroprusside, Diazoxide, Minoxidil, Reserpine, Hydralazine hydrochloride. Explain the definition, mechanism, classification, structure, chemistry and Structure Activity Relationship studies of antihypertensive drugs. To describe the chemical synthesis of selected drugs marked with asterisk
  • Introduction
  • Classification of drugs
  • Mode of action
  • Mechanism
  • Synthesis
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Instructive
  • Power point presentation
  • Class discussion
  • Student reports by individuals

 

03
3   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.
 Explain the definition, classification, mechanism of action, structure, chemistry and Structure Activity Relationship studies of cardiovascular drugs. To describe the chemical synthesis of selected drugs marked with asterisk
  • Introduction of Anti-arrhythmic , Anti-hyperlipidemic, Coagulant & Anticoagulants
  • Classification of drugs
  • Mode of action
  • Mechanism
  • Synthesis
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Sugars in heart glycosides
  • Digitalis glycosides
  • Strophanthus glycoside
  • Scilla glycosides
  • Official compounds
  • Digitoxin
  • Digoxin
  • Instructive
  • Power point presentation
  • Tutorials
  • Student reports by individuals
  • Group discussion

Presentations by student panels from the class

10
4 08 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.
Explain the Nomenclature, Stereochemistry and metabolism of drugs acting on endocrine system. Know the importance of Structure Activity Relationship studies of drugs.
  • Introduction
  • Types of hormones
  • Structure and metabolism
  • Synthesis
  • Classification of drugs
  • Mode of action
  • Mechanism
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Instructive
  • Group discussion
  • Presentation by a panel of instructors or students
  • Class discussions conducted by a student or student committee
  • Group discussion
  • Presentations by student panels from the class

 

05
5 5.1 Antidiabetic agents:

Insulin and its preparations

Sulfonyl ureas: Tolbutamide*, Chlorpropamide, Glipizide, Glimepiride. Biguanides: Metformin.

Thiazolidinediones: Pioglitazone, Rosiglitazone. Meglitinides: Repaglinide, Nateglinide. Glucosidase inhibitors: Acrabose, Voglibose.

Describe the definition, classification, structure, mechanism of action, chemistry and Structure Activity Relationship studies of antidiabetic drugs. To know the chemical synthesis of selected drugs marked with asterisk
  • Introduction of hypoglycemic agents
  • Insulin
  • Types of diabetes
  • Oral antidiabetic agents
  • Classification of drugs
  • Mode of action
  • Mechanism
  • Drug Synthesis
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Instructive
  • Power point presentation
  • Group discussion
  • Class discussions conducted by a student or student committee

 

03
  5.2 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.*
To Explain the definition, classification, mechanism of action, chemistry and Structure Activity Relationship of local anesthetic drugs. To know the chemical synthesis of selected drugs marked with asterisk
  • Introduction
  • Classification of drugs
  • Mode of action
  • Drug Synthesis
  • Mechanism
  • Drug interaction and contraindication
  • Dose and uses of each drugs
  • Structure activity relationship of selective class of drugs
  • Instructive
  • Power point presentation
  • Flowcharts
07
Admission 2017