Sem4 Syl
Sem4 Syl
Sem4 Syl
45
UNIT-V
Name Reactions of synthetic importance
Pinacol-Pinacolone, Hofmann, Baeyer-Villiger oxidation, Benzilic acid rearrangement 12
reaction, Beckmann’s rearrangement and Schmidt rearrangement, Claisen-Schmidt Hours
condensation, Clemmensen reduction, Wolff rearrangement, Oppenauer-oxidation and
Dakin reaction, and Birch reduction.
Recommended Books
1. Morrison, R. T. & Boyd, R. D., Textbook of Organic Chemistry, VI (ed.) ELBS, London,
1996
2. Advanced General Organic Chemistry-A Modern Approach by Sachin Kumar Ghosh, 3/Ed.
2009, New Central Book Agency (P) Ltd.
3. Pine, S. H, Organic Chemistry, V, Tata McGraw Hill, New Delhi, 2003
4. Finar, I. L., Organic Chemistry Vol. I, V (ed.), ELBS, Pearson Education, New Delhi, 2003
5. Joule and Mills, Heterocyclic Chemistry, IV (ed.), Blackwell Publishing House, Oxford, UK,
2004
6. Li, J. J., Name Reactions, III (ed.), Springer, Berlin, 2006
7. Stereochemistry of Organic Compound Principles and Applications by Nasipuri, Revised Edition,
New Age International Publishers.
8. Stereochemistry Conformation and Mechanism by P.S. Kalsi, 7/Ed 2008, New Age International
Publishers, New Delhi.
9. Stereochemistry of Organic Compound Principles and Applications by Nasipuri, Revised Edition,
New Age International Publishers.
46
BP402T. MEDICINAL CHEMISTRY – I (Theory) 45 hours
Scope
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 and metabolism of drugs. The syllabus also
emphasizes on chemical synthesis of important drugs under each class.
Objectives
Upon completion of the course the student shall be able to
Understand the chemistry of drugs with respect to their pharmacological activity.
Understand the drug metabolic pathways, adverse effect and therapeutic value of
Drugs.
Know the Structural Activity Relationship (SAR) of different class of drugs.
Write the chemical synthesis of some drugs.
COURSE CONTENT
Note: Study of the development of the following classes of drugs, classification, mechanism
of action, Structure activity relationship, uses of drugs mentioned in the course.
The synthesis of drugs mentioned in bracket [] only needs to be covered.
UNIT-I 06 hours
Introduction to Medicinal Chemistry
a) History and development of medicinal chemistry
b) Physicochemical properties in relation to biological action Ionization,
Solubility, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation,
Bioisosterism, Optical and Geometrical isomerism.
c) Drug metabolism
Drug metabolism principles - Phase I and Phase II.
Factors affecting drug metabolism including stereo chemical aspects.
UNIT-II
Drugs acting on Autonomic Nervous System 10 hours
a) Adrenergic Neurotransmitters: Biosynthesis and catabolism of
catecholamine. Adrenergic receptors (Alpha & Beta) and their distribution.
b) Sympathomimetic agents: SAR of Sympathomimetic agents Direct
acting: Nor-epinephrine, Epinephrine, Dopamine, Phenylephrine, Methyldopa,
Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol, Oxymetazoline and
Xylometazoline
Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine
Agents with mixed mechanism: Ephedrine, Amphetamine.
c) Adrenergic Antagonists:
Alpha adrenergic blockers: Tolazoline, Phentolamine, Phenoxybenzamine,
Prazosin.
Beta adrenergic blockers: SAR of beta blockers, Propranolol, Atenolol,
Labetolol, Carvedilol.
[Phenylephrine, Salbutamol, Tolazoline, Propranolol]
47
UNIT-III 10 hours
a) Cholinergic neurotransmitters: Biosynthesis and catabolism of
acetylcholine.
Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.
b) Parasympathomimetic agents: SAR of Parasympathomimetic agents
Direct acting agents: Acetylcholine, Carbachol, Bethanechol, Pilocarpine.
Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible):
Physostigmine, Neostigmine, Edrophonium chloride, Donepezil, Tacrine
hydrochloride, Parathion, Malathion.
Cholinesterase reactivator: Pralidoxime chloride.
Cholinergic Blocking agents: SAR of cholinolytic agents :Solanaceous alkaloids
and analogues: Atropine sulphate, Scopolamine hydrobromide, Ipratropium
bromide
Synthetic cholinergic blocking agents: Tropicamide, Cyclopentolate
hydrochloride, Dicyclomine, Glycopyrrolate, Propantheline bromide
[Neostigmine, Dicyclomine hydrochloride]
UNIT-IV 10 hours
Drugs acting on Central Nervous System
a) Sedatives and Hypnotics:
Benzodiazepines: SAR of Benzodiazepines, Chlordiazepoxide, Diazepam,
Oxazepam, Chlorazepate, Lorazepam, Alprazolam, Zolpidem
Barbiturtes: SAR of barbiturates, Barbital, Amobarbital, Butabarbital,
Pentobarbital, Secobarbital Miscelleneous:Amides & imides Alcohol & their
carbamate derivatives Aldehyde & their derivatives
b) Antipsychotics Phenothiazeines: SAR of Phenothiazines - Chlorpromazine
hydrochloride, Triflupromazine, Thioridazine hydrochloride, Trifluoperazine
hydrochloride
Ring Analogues of Phenothiazeines: Thiothixene, Loxapine succinate, Clozapine.
Fluro buterophenones: Haloperidol, Droperidol, Risperidone.
Benzamides: Sulpiride.
c) Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant
action
Barbiturates: Phenobarbitone, Mephobarbital
Hydantoins: Phenytoin, Mephenytoin
Oxazolidine diones: Trimethadione
Succinimides:Phensuximide, Methsuximide
Urea and monoacylureas: Phenacemide, Carbamazepine
Benzodiazepines: Clonazepam
Miscellaneous: Levetiracetam, Valproic acid , Gabapentin ,Felbamate
d) General anesthetics:
Inhalation anesthetics: Halothane, Enflurane
Ultra short acting barbitutrates: Methohexital sodium, Thiopental sodium.
Dissociative anesthetics: Ketamine hydrochloride.
[Diazepam, Barbital, Chlorpromazine hydrochloride, Phenytoin,
Carbamazepine, Halothane, Ketamine hydrochloride]
48
UNIT-V 07 hours
Centrally Acting analgesics
a) Narcotic and non-narcotic analgesics Morphine and related drugs: SAR
of Morphine analogues, Morphine sulphate, Codeine, Meperidine hydrochloride,
Diphenoxylate hydrochloride,Loperamide hydrochloride, Fentanyl citrate,
Methadone hydrochloride, Propoxyphene hydrochloride, Pentazocine, Levorphanol
tartarate.
Narcotic antagonists: Nalorphine hydrochloride, Levallorphan tartarate, Naloxone
hydrochloride.
b) Anti-inflammatory agents: Sodium salicylate, Aspirin, Mefenamic acid,
Indomethacin, Sulindac, Diclofenac,Ketorolac, Ibuprofen, Piroxicam,
Acetaminophen, Phenylbutazone.
[Fentanyl citrate, Methadone hydrochloride, Mefenamic acid, Ibuprofen]
49
BP406P. MEDICINAL CHEMISTRY – I (Practical) 4Hrs/week
50
BP 403 T. PHYSICAL PHARMACEUTICS-II (Theory) 45 Hours
Scope: The course deals with the various physical and physicochemical properties, and
principles involved in dosage forms/formulations. Theory and practical components of the
subject help the student to get a better insight into various areas of formulation research and
development, and stability studies of pharmaceutical dosage forms.
1.Relate various physicochemical properties of drug and excipient molecules in designing the
dosage forms
2.Distinguish the principles of chemical kinetics & to use them for stability testing and
determination of expiry date of formulations
3.Demonstrate the behavior and mechanism of drugs and excipients in the formulation
development and evaluation of dosage forms.
Course Content:
UNIT-I 07 Hours
Colloidal dispersions: Classification of dispersed systems & their general characteristics, size &
shapes of colloidal particles, classification of colloids & comparative account of their general
properties. Optical, kinetic & electrical properties. Effect of electrolytes, coacervation,
peptization& protective action.
UNIT-II 10 Hours
Rheology: Newtonian systems, law of flow, kinematic viscosity, effect of temperature, non-
Newtonian systems, pseudoplastic, dilatant, plastic, thixotropy, thixotropy in formulation,
determination of viscosity, capillary, falling sphere, rotational viscometers,Visco elasticity
Deformation of solids: Plastic and elastic deformation, Heckel equation, Stress, Strain, Elastic
Modulus
UNIT-III 10 Hours
51
UNIT-IV 08 Hours
Micromeretics: Particle size and distribution, mean particle size, number and weight
distribution, particle number, methods for determining particle size by different methods,
counting and separation method, particle shape, specific surface, methods for determining
surface area, permeability, adsorption, derived properties of powders, porosity, packing
arrangement, densities, bulkiness & flow properties.
UNIT-V 10 Hours
Drug stability: Reaction kinetics: zero, pseudo-zero, first & second order(complex
reaction:reversible, parallel and side reactions), units of basic rate constants, determination of
reaction order. Physical and chemical factors influencing the chemical degradation of
pharmaceutical product: temperature, solvent, ionic strength, dielectric constant, specific &
general acid base catalysis,Simple numerical problems.Stabilization of medicinal agents against
common reactions like hydrolysis & oxidation.Accelerated stability testing in expiration dating
of pharmaceutical dosage forms.Photolytic degradation and its prevention
52
BP 407P. PHYSICAL PHARMACEUTICS- II (Practical) 4 Hours/week
Recommended Books:
53
BP 404 T. PHARMACOLOGY-I (Theory) 45Hours
Scope: The main purpose of the subject is to understand what drugs do to the living organisms
and how their effects can be applied to therapeutics. The subject covers the information about the
drugs, mechanism of action, physiological and biochemical effects (Pharmacodynamics) as well
as absorption, distribution, metabolism and excretion (pharmacokinetics) along with the adverse
effects, clinical uses, interactions, doses, contraindications and route of administration of
different classes of drugs.
54
Drug discovery and clinical evaluation of new drugs:
Introduction to drug discovery, Preclinical evaluation and Clinical trials
Introduction to Pharmacovigilance
Unit III Pharmacology of drugs acting on Peripheral Nervous System 08 Hrs
Introduction to Autonomic Nervous System, Parasympathomimetics,
Parasympatholytics, Sympathomimetics and Sympatholytics.
Neuromuscular blocking agents and skeletal muscle relaxants (peripheral).
Local anaesthetic agents.
Drugs used in myasthenia gravis and glaucoma
Unit-IV Pharmacology of drugs acting on central nervous system 09 Hrs
Neurohumoral transmission in the C.N.S.-
Special emphasis tobe given on importance of various neurotransmitters
like with GABA, Glutamate, Glycine, Serotonin, Dopamine.
General anaesthetics and pre-anaesthetics
Sedatives, Hypnotics and Centrally acting muscle relaxants
Anti-epileptics
Alcohol and Disulfiram
Unit-V Pharmacology of drugs acting on Central Nervous System 08 Hrs
Psychopharmacological agents:Antipsychotics, Antidepressants, Anti-
anxiety agents, anti-manics and Hallucinogens
Drugs used in Parkinson’s disease and Alzheimer’s disease
CNS stimulants and Nootropics
Opioid analgesics and antagonists (including addiction, abuse, tolerance
and dependence)
REFERENCES:
1. Rang H. P., Dale M. M., Ritter J. M., Flower R. J., Rang and
Dale’sPharmacology,.Churchil Livingstone Elsevier.
2. Katzung B. G., Masters S. B., Trevor A. J., Basic and clinical pharmacology, Tata Mc
Graw-Hill
3. Goodman and Gilman’s, The Pharmacological Basis of Therapeutics
4. Marry Anne K. K., Lloyd Yee Y., Brian K. A., Robbin L.C., Joseph G. B., Wayne A.
K., Bradley R.W., Applied Therapeutics, The Clinical use of Drugs, The Point
Lippincott Williams &Wilkins
5. Mycek M.J, Gelnet S.B and Perper M.M. Lippincott’s Illustrated Reviews-Pharmacology
6. K.D.Tripathi. Essentials of Medical Pharmacology, JAYPEE Brothers Medical
Publishers (P) Ltd, New Delhi.
7. Sharma H. L., Sharma K. K., Principles of Pharmacology, Paras medical publisher
8. Modern Pharmacology with clinical Applications, by Charles R. Craig & Robert,
9. Ghosh MN. Fundamentals of Experimental Pharmacology. Hilton & Company,Kolkata.
55
10. Barar, F.S.K., Essentials of Pharmacotherapeutics; S. Chand and Company, New Delhi.
11. A textbook of Pathophysiology, Bodhankar, SL and Vyawahare, NS, NiraliPrakashan,
Pune.
12. Das, M. M. and Dutta S. K. : R. Ghosh,s Modern Concepts on pharmacology and
Therapeutics, ( HILTON and Co. Calcutta )
13. Satoskar , R.S. and Bhandarkar S.D. Pharmacology and Pharmacotherapeutics
(PopularPrakashan, Bombay).
14. Craig, C.R. and Stitzel, B.E.; Modern Pharmacology, Little Brown and Co, Boston.
15. JamesCrossland. Lewis,s Pharmacology Basis of Therapeutics, Pergamon Press, New
York.
16. Harrison’s Principle and Practice of Medicine, 18th Edition, Churchill, Livingston,
.London.
17. Roger and Walker. Clinical Pharmacy and Therapeutics, Churchill, Livingston, London.
18. Dipiro Joseph L. A pathphysiological Approach, Elsevier.
19. Davidson’s Principle of Internal Medicine, McGraw-Hill companies.
20. Guyton AC. Textbook of medical Physiology. W. B. Sanders CO., Philadelphia, USA.
21. Chatterjee, C.C., Human Physiology. Medical Allied Agency, Kolkata.
22. Ganong, W.F., Review of Medical Physiology. Prentice-Hall International, London.
56
BP 408 P.PHARMACOLOGY-I (Practical) 4 Hours/week
REFERENCES:
57
BP 405 T.PHARMACOGNOSY AND PHYTOCHEMISTRY I (Theory) - 45 Hours
COURSE CONTENT 45
Hours
UNIT-I
Introduction to Pharmacognosy:
(a) Definition, history, scope and development of Pharmacognosy
(b) Sources of Drugs – Plants, Animals, Marine & Tissue culture
(c) Organized drugs, unorganized drugs (dried latex, dried juices, dried extracts,
gums and mucilages, oleoresins and oleo- gum -resins).
Classification of drugs:
Alphabetical, morphological, taxonomical, chemical, pharmacological, chemo and 10
sero taxonomical classification of drugs Hours
Quality control of Drugs of Natural Origin:
Adulteration of drugs of natural origin. Evaluation by organoleptic, microscopic,
physical, chemical and biological methods and properties.
Quantitative microscopy of crude drugs including lycopodium spore method, leaf
constants, camera lucida and diagrams of microscopic objects to scale with camera
lucida.
UNIT-II
Cultivation, Collection, Processing and storage of drugs of natural origin:
Cultivation and Collection of drugs of natural origin
10
Factors influencing cultivation of medicinal plants.
Hours
Plant hormones and their applications.
Polyploidy, mutation and hybridization with reference to medicinal plants
Conservation of medicinal plants
UNIT-III
Plant tissue culture:
Historical development of plant tissue culture, types of cultures, Nutritional
07
requirements, growth and their maintenance.
Hours
Applications of plant tissue culture in pharmacognosy.
Edible vaccines
58
UNIT-IV
Plant description, morphology and anatomy:
Leaves, Roots, Barks, Wood, Flowers, Fruits, Seeds, subterranean organs 10
Introduction to secondary metabolites: Hours
Definition, classification, properties and test for identification of Alkaloids,
Glycosides, Flavonoids, Tannins, Volatile oil and Resins
UNIT-V
Study of biological source, chemical nature and uses of drugs of natural origin
containing following drugs
Plant Products:
Fibers - Cotton, Jute, Hemp
Hallucinogens, Teratogens, Natural allergens
59
BP408 P. PHARMACOGNOSY AND PHYTOCHEMISTRY I (Practical):
4Hrs/week
Recommended Books:
1. W.C.Evans, Trease and Evans Pharmacognosy, 16th edition, W.B. Sounders & Co.,
London, 2009.
2. Tyler, V.E., Brady, L.R. and Robbers, J.E., Pharmacognosy, 9th Edn., Lea and Febiger,
Philadelphia, 1988.
3. Text Book of Pharmacognosy by T.E. Wallis
4. Mohammad Ali. Pharmacognosy and Phytochemistry, CBS Publishers & Distribution,
New Delhi.
5. Text book of Pharmacognosy by C.K. Kokate, Purohit, Gokhlae (2007), 37th Edition,
Nirali Prakashan, New Delhi.
6. Herbal drug industry by R.D. Choudhary (1996), Ist Edn, Eastern Publisher, New Delhi.
7. Essentials of Pharmacognosy, Dr.SH.Ansari, IInd edition, Birla publications, New Delhi,
2007
8. Practical Pharmacognosy: C.K. Kokate, Purohit, Gokhlae
9. Anatomy of Crude Drugs byM.A. Iyengar
60