OU Pharm D Question Papers Last 10 Years 2010-2020 || Osmania University
THIRD Year B. Pharmacy
- Name of subject : MEDICINAL CHEMISTRY-I
- Departmental objectives:
- Learning Objectives:
- To relate the structure and physical properties of drugs to their pharmacological activity.
- To demonstrate an understanding of concepts such as drug metabolism, bioavailability and pharmacokinetics and the role of medicinal chemistry in improving these parameters.
- To understand the basic biological and pharmacological interactions by using both natural products and synthetic bioactive molecules
- To learn about the characterization of drugs and drug-like molecules.
- To understand principles of drug action and the role of bonding in drug-target interactions, identification of targets for drug action.
- To describe the mechanism of action, synthesis and medicinal uses of different class of chemotherapeutic agents.
- To differentiate drugs according to their action and give examples of each class of drug.
- To describe the synthetic routes used to prepare some selected drug compounds.
- To understand simple methods of synthesis, purification and characterization of an organic medicinal compound in the laboratory.
- To train the students in basic & newer approaches in synthesis of drug molecules chemical entities.
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- Learning Outcomes:
- Learn the classification of chemotherapeutic agents based on their chemical group, their mode of action and medicinal uses.
- Understands and describes the synthesis, structure activity relationships and mode of action of drugs used in the treatment of diseases.
- Use of corresponding knowledge for the development of biologically and clinically active drugs.
- Employ scientific methodologies such as experimental design, and the critical analysis of data.
- Based on a knowledge of the biochemical details for specific drug mechanisms, to develop the ability to distinguish superior therapeutic drug mechanisms
- Describe the synthesis of important target compounds.
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- Learning Objectives:
- Annual objectives (for each year, if the subject is spread over different years): NA
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4. Content distribution as per the list of topics, time allotted for each topic, distribution for 'Must know', 'Desirable to know' and ‘Nice to know' and the probable weightage.
| Sl No | Topic | Hours | Learning content distribution | Weightage (Marks) | ||
|---|---|---|---|---|---|---|
| Must know | Desirable to know | Nice to know | ||||
| I | Basic Principles of Medicinal Chemistry | 12 | a) Effects of the following physicochemical properties of drug molecules on biological activity: Ionisation, hydrogen bonding, solubility, partition coefficient, logP, logD, protein binding, chelation and polar surface area. b) Receptor and drug receptor interactions. c) Drug metabolism: Biotransformation, sites of biotransformation, General pathways of drug biotransformation, role of cytochrome P-450 and monoamino oxygenase in oxidative biotransformation, oxidative, reductive, hydrolytic and conjugation reactions with examples. | d) History and development of Medicinal Chemistry, definition of hit, lead and drug. | 15-16 | |
| II | Central nervous system depressants | 16 | A) General Anaesthetics: Definition, mode of action Inhalation anaesthetics: Halothanes, Nitrous oxide Methoxyflurane, 1. Ultra shot acting barbiturates: Methohexitol sodium, 2. Thiopental sodium 3. Dissociative anaesthetics: Ketamine HCl | 20-21 | ||
| B. Tranquilizers, sedatives and hypnotics 1. Major tranquilizers: SAR of Phenothiazines, Promethazine HCl, Chlorpromazine HCl, Prochlorperazine, thioridazine HCl Thioxanthenes: clozapine, Chlorprothixene, thiothixine, Fluorobutyrophenones: Haloperidols, Resperidone Beta amino ketones: Molindone HCl, Benzamaide surpieride Minor tranquilizers: SAR of Benzodiazepines, Chlordiazepoxide, Diazepam, Orazepam, Chlorazepam, Lorazepam, Flurazepam, Alprazolam, Triazolam 2.Barbiturates: Classification and SAR, Barbitals, Methobarbital, Phenobarbital, Amobarbital, Butarbital, Pentobarbital, Secobarbital 3.Miscellaneous sedative hypnotics: a)Amides and imides: Glutethimides, Methyprylon, Methaqualone b) Alcohols and their carbamate derivatives: Ethchlorvynol, Ethinamate, Meprobamate c) Aldehydes and their derivatives: Chloral hydrate, Paraldehyde C.Skeletal muscle relaxants: Chlorphenesin, Methocarbamol, Chlorzoxazone | ||||||
| III | Adrenergic agents | 9 | A.Adrenergic Neurotransmitters and their biosynthesis and metabolism, adrenergic receptors their distribution and actions mediated by them B.Sympathomimetics 1.Direct acting: Endogenous catecholamines, a) Alpha adrenergic agonists: Phenylephrine, Methoxamine, Naphazoline, Xylometazoline, Oxymetazoline, Clonidine, Guanabenz, Methyldopa b) Dual agonist/ antagonist: Dobutamine c) Beta adrenergic agonists: Isoproterenol, Metaproterenol, Terbutaline, Albuterol, | 11-12 | ||
| D. Drugs used in spasticity: Baclofen, Buspirone E.Anticonvulsants: Structural requirement for anticonvulsant activity, mechanism of anticonvulsant action 1.Barbiturates: Phenobarbitone, Mepobarbitone 2.Hydantoins:Phenytoin, Ethotoin, Mephenytoin 3.Oxazolidinediones: Trimethadione, Paramethadione 4.Succinimides: Phensuximide, Methsuximide, Ethsuximide 5.Urea and monoacyl ureas: Phenacemide, Carbamazepine 6.Benzodiazepines: Clonazepam, 7.Miscellaneous: Primidone, Valproic acid | ||||||
| IV | Cholinergic drugs and related agents | 12 | 1.Cholinergic neurotransmitter: Biosynthesis, metabolism and functions of acetylcholine 2.Cholinergic receptors: Nicotinic, muscarinic and their subtypes A. Cholinergic agonists: 1.Stereochemistry and SAR, Acetylcholine, Methacholine, Carbachol, Bethanechol, Pilocarpine 2. Cholesterase inhibitors: a) Reversible: Mode of action, Physostigmine, Neostigmine, Ambenonium, Demecarium, Edrophonium, Tacrine b) Irreversible: Mode of action, Isoflurophate, Ecothiophate, Malathion, Parathion, Pralidoxime. B.Cholinergic blockers: SAR 1.Postganglionic blockers: Structural considerations of solanaceous alkaloids and analogs, Atropine, Hyoscyamine, Scopolamine, Homatropine, Ipratropium 2.Synthetic agents: Clidinium, Dicyclomine, Glycopyrrolate, Methantheline, Propantheline, Benztropine, Procyclidine, Tropicamide 3.Ganglionic blockers: Mode of action, Trimethaphan, Mecamylamine 4.Neuromuscular blockers: Mode of action, Tubocurarine, Metocurine, Gallamine, Pancuronium, Vecuronium. | 15-16 | ||
| V | Local anesthetics | 4 | A. Definition, classification, and mechanism of action B. SAR of lidocaine derivatives C. 1. Benzoic acid derivatives: Hexylcaine, Cyclomethicaine, Piperocaine. 2. Aminobenzoic acid derivatives: Benzocaine, Procaine, Procainamide 3. Lidocaine derivatives (Anilides): Lidocaine, Prilocaine 4. Miscellaneous: Dimethisoquin, Dibucaine | 5-6 | ||
| VI | Histamine and antihistaminic agents | 6 | B. Antihistaminics: H1 antagonists a) Aminoalkyl ethers: Diphenhydramine HCl, Bromodiphenhydramine, Doxylamine b) Ethylene diamines: Tripelenamine Pyrilamine c) Propylamine derivatives: Pheniramine, Chlorpheniramine d) Phenothiazine derivatives: Promethazine, Trimeprazine e) Piperazine derivatives: Cyclizine, Meclizine, Cetrizine f) Miscellaneous compounds: Phenindamine, Cyproheptadine C.H2 Antagonists: Mechanism, Cimetidine, Ranitidine, Famotidine D. Gastric proton pump inhibitors: Mechanism of action, Omeprazole, Pentaprazole, Rabiprazole, Lansoprazole. | A. Histamine: receptors and its actions | 8-9 | |
| VII | Analgesic agents | 9 | A. 1. Narcotic analgesics: Opoid receptors, SAR, Morphine, Codiene, Diacetylmorphine, Levorphanol, Dextromethorphan, Pentazocine, Meperidine, Loperamide, Fentanyl, Methadone, Propoxyphene, Tramadol 2. Narcotic antagonists: Butorphanol, Nalorphine, Levalorphan, Naltrexone, Naloxone B. Non narcotic analgesics: 2.Non steroidal anti-inflammatory agents: Mechanism of action | 1.Steroidal Antiinflammator agents: Cortisone, Hydrocortisone, Dexamethasone Betamethasone, Triamcinolone, Fluocinolone | 11-12 | |
| VIII | Structure and medicinal uses of important prostaglandins | 1 | Structure and medicinal uses of important prostaglandins | 1-2 | ||
| IX | Natural Products | 6 | A. Alkaloids: Definition, Classifications. B. Purines: Definition, Interrelation among caffeine, theophylline, theobromine C. Terpenoids: Definition, classification, isoprene and special isoprene rule, Interrelationship among monocyclic monoterpenoids like limonene, dipentene, alphaterpenoid, alpha terpenolene, terpenion, terpin, terpene hydrate, carvone and cineone. | Structural elucidation of ephedrine. Structural elucidation of caffeine, | 8-9 |
5. Blueprint of question paper, for each QP..
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| Sl No | Chapter | Marks distribution | Total Marks | |||||
|---|---|---|---|---|---|---|---|---|
| Must Know | Desirable to Know | Long Essay | Short Essay | Short Answer | ||||
| I | Basic Principles of Medicinal Chemistry | Physico-chemical properties of drug molecules | History and development of Medicinal Chemistry, definition of hit, lead and drug. | 10 | -- | 2 | 12 | |
| II | Central nervous system depressants | Definition, Mechanism of action, classification with structures and synthesis SAR. | 10 | -- | 2+2 | 14 | ||
| III | Adrenergic agents | Definition, Mechanism of action, classification with structures and synthesis SAR | 5 | 2 | 7 | |||
| IV | Cholinergic drugs and related agents | Definition, Mechanism of action, classification with structures and synthesis SAR | 5 | 2+2 | 9 | |||
| V | Local anesthetics | Definition, Mechanism of action, classification with structures and synthesis SAR | 5 | 5 | ||||
| VI | Histamine and antihistaminic agents | Definition, classification with structures and synthesis | Histamine structure, biosynthesis and biological activity. Histamine receptors and its actions | 5 | 2 | 7 | ||
| VII | Analgesic agents | Definition, Mechanism of action, classification with structures and synthesis SAR | Steroidal Antiinflammator agents: Cortisone, Hydrocortisone, Dexamethasone Betamethasone Triamcinolone, Fluocinolone | 5 | 2+2 | 9 | ||
| VIII | Structure and medicinal uses of important prostaglandins | Structure and medicinal uses of important prostaglandins | -- | 2 | 2 | |||
| IX | Natural Products | Definition, classification with structures and synthesis | Structural elucidation of ephedrine. Structural elucidation of caffeine, | 5 | 5 | |||
| Total | 20 | 30 | 20 | 70 |
* 80 % of the questions shall be from the Must Know area and 20 % shall be from the Desirable to know area of the Curriculum
6. Question paper layout to show which question number will represent which chapter (s)
Long Essay: 2X 10 = 20
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- Basic Principles of medicinal chemistry
- Central nervous system depressant
Short Essays: 5x 6 = 30
| 3 | Adrenergic drugs |
| 4 | Cholinergic drugs and related agents |
| 5 | Local anaesthetics |
| 6 | Histamine and antihistaminic agents |
| 7 | Analgesic agents |
| 8 | Natural products |
Short Answers: 2X10 = 20
| 9 | Basic Principles of medicinal chemistry |
| 10 | Central nervous system depressant |
| 11 | Central nervous system depressant |
| 12 | Adrenergic drugs |
| 13 | Cholinergic drugs and related agents |
| 14 | Cholinergic drugs and related agents |
| 15 | Histamine and antihistaminic agents |
| 16 | Analgesic agents |
| 17 | Analgesic agents |
| 18 | Structure and medicinal uses of important prostaglandins |
7. Scheme of Practical / Clinical Teaching and Assessment:
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List the expected practical / clinical competencies.
State the objectives for each competency.
Assign content for the objectives.
Describe the teaching – learning processes.
| Sl No | Skills | Duration | Learning methods |
|---|---|---|---|
| 1 | Demonstrate the methods of synthesis of simple organic compounds used as drugs or starting materials. | ||
| 2 | Demonstrate the various methods of filtration, crystallization, purification. | ||
| 3 | Reason critically and logically and make independent judgments | ||
| 4 | Employ scientific methodologies such as experimental design, and the critical analysis of data | ||
| 5 | Interact effectively as part of a team in order to work towards a common outcome | ||
| 7 | Demonstrate an understanding of the chemical industry and the way it operates, especially the pharmaceutical industry and others involving synthesis such as the petrochemical, polymer and agrichemical industries |
Scheme of examination with the distribution of marks as per the prioritisation of competencies.
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| S1 No | Competency | Assessment criteria | Marks |
|---|---|---|---|
| A | Knowledge | Synopsis | 10 |
| B | Cognitive and intellectual skills | ||
| C | Subject specific practical skills | Major & Minor Experiment-I, Minor experiment-II | 25+15+10 |
| D | Transferable professional skills | Viva-voce | 10 |
| Total | 70 |
8. Suggested references (as per Vancouver style):
- Basic references
- Advanced references (may also include journals / web / other electronic sources)
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MEDICINAL CHEMISTRY II TEXT BOOKS (THEORY)
Latest editions and all volumes of
- Foye's principles of Medicinal chemistry
- Wilson and Griswold's Text book of Organic and Pharmaceutical chemistry
- Rama Rao Nadendla, Medicinal Chemistry
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MEDICINAL CHEMISTRY II REFERENCE BOOKS (THEORY)
Latest editions and all volumes of
- Burger's medicinal chemistry
- The Martindale's Extra Pharmacopoeia
- A.I.Vogel, Text Book of practical organic chemistry including the qualitative analysis
- A.H.Becket and J.B.Stanlake, Practical Pharmaceutical chemistry
- M Raghuprasad, Advanced medicinal chemistry: A laboratory guide
- J.G.Mann and Saunders, Practical organic chemistry, ELBS Longman, London
- I.P.1985, Ministry of Health, Govt. of India
- LedniserMitzsher, Organic drug synthesis, Vol.1 and 2
- I.L. Finar, Text Book organic chemistry
- T. Robinson, Organic constituents of higher plants
- Feiser and Feiser Steroids
- Drug design by Ariens
- Smith and Williams, Introduction to principle of drug design
- Purcell, Strategy of drug design
- CIMS
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MEDICINAL CHEMISTRY [ REFERENCE BOOKS (PRACTICALS)
- A.I.Vogel, Text Book of practical organic chemistry
- A.H. Beckett and Stanlake, Practical pharmaceutical chemistry
- J.G.Mann and Saunders, Practical organic chemistry
- Jayaveera KN, Practical medicinal chemistry
- Raghuprasad M, Advanced medicinal Chemistry
- Feiser and Feiser, Steroids
- IP 1985
- I.L.Finar, Textbook of organic chemistry
- CIMS
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