4 UNIT IV 08

Synthesis, reactions and medicinal uses of following compounds/derivatives

Pyrazole, Imidazole, Oxazole and Thiazole.
Pyridine, Quinoline, Isoquinoline, Acridine and Indole. Basicity of pyridine
Synthesis and medicinal uses of Pyrimidine, Purine, azepines and their
derivatives
5 UNIT V - Reactions of synthetic importance 07
5.1 Metal hydride reduction (NaBH4 and LiAlH4), Clemmensen reduction, 2
Birch reduction, Wolff Kishner reduction

5.2 Oppenauer-oxidation and Dakin reaction. 2

5.3 Beckmanns rearrangement and Schmidt rearrangement 2

5.4 Claisen-Schmidt condensation 1

Total 45

Reference Books (Latest Editions to be adopted)

1. Organic chemistry by I.L. Finar, Volume-I & II.
2. A text book of organic chemistry – Arun Bahl, B.S. Bahl.
3. Heterocyclic Chemistry by Raj K. Bansal
4. Organic Chemistry by Morrison and Boyd
5. Heterocyclic Chemistry by T.L. Gilchrist

79
BP402T MEDICINAL CHEMISTRY – I (Theory) 3 L + 1T / Week
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:

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 (SAR) of different class of drugs
4. write the chemical synthesis of some drugs

Sr. Content Hours

No. 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*
1 UNIT I - Introduction to Medicinal Chemistry 10
1.1 History and development of medicinal chemistry 1
1.2 Physicochemical properties in relation to biological action 4
Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein
binding, Chelation, Bioisosterism, Optical and Geometrical isomerism
1.3 Drug metabolism 5
 Drug metabolism principles- Phase I and Phase II.
 Factors affecting drug metabolism including stereo chemical aspects
2 UNIT II - Drugs acting on Autonomic Nervous System 10
2.1 Adrenergic Neurotransmitters: 2
 Biosynthesis and catabolism of catecholamine.
 Adrenergic receptors (Alpha & Beta) and their distribution.
2.2 Sympathomimetic agents: SAR of Sympathomimetic agents 4
 Direct acting: Nor-epinephrine, Epinephrine, Phenylephrine*,
Dopamine
 Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline,
Salbutamol*, Bitolterol, Naphazoline, Oxymetazoline and

80
 Xylometazoline
 Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine,
Propylhexedrine.
 Agents with mixed mechanism: Ephedrine, Metaraminol.
2.3 Adrenergic Antagonists: 4
 Alpha adrenergic blockers: Tolazoline*, Phentolamine,
Phenoxybenzamine, Prazosin, Dihydroergotamine, Methysergide.
 Beta adrenergic blockers: SAR of beta blockers, Propranolol*,
Metibranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol,
Labetolol, Carvedilol.
3 UNIT III - Cholinergic neurotranimitters 10
3.1 Biosynthesis and catabolism of acetylcholine. 2
Cholinergic receptors (Muscarinic & Nicotinic) and their distribution
3.2 Parasympathomimetic agents: SAR of Parasympathomimetic agents 4
 Direct acting agents: Acetylcholine, Carbachol*, Bethanechol,
Methacholine, Pilocarpine.
 Indirect acting/ Cholinesterase inhibitors (Reversible &
Irreversible): Physostigmine, Neostigmine*, Pyridostigmine,
Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride,
Isofluorphate, Echothiophate iodide, Parathione, Malathion.
 Cholinesterase reactivator: Pralidoxime chloride.
3.3 Cholinergic Blocking agents: SAR of cholinolytic agents 4
 Solanaceous alkaloids and analogues: Atropine sulphate,
Hyoscyamine sulphate, Scopolamine hydrobromide, Homatropine
hydrobromide, Ipratropium bromide*.
 Synthetic cholinergic blocking agents: Tropicamide, Cyclopentolate
hydrochloride, Clidinium bromide, Dicyclomine hydrochloride*,
Glycopyrrolate, Methantheline bromide, Propantheline bromide,
Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride,
Procyclidine hydrochloride*, Tridihexethyl chloride, Isopropamide
iodide, Ethopropazine hydrochloride.

4 UNIT IV - Drugs acting on Central Nervous System 08

4.1 Sedatives and Hypnotics: 3
 Benzodiazepines: SAR of Benzodiazepines, Chlordiazepoxide,
Diazepam*, Oxazepam, Chlorazepate, Lorazepam, Alprazolam,
Zolpidem
 Barbiturtes: SAR of barbiturates, Barbital*, Phenobarbital,

81
 Mephobarbital, Amobarbital, Butabarbital, Pentobarbital, Secobarbital
 Miscelleneous:
Amides and imides:Glutethmide.
Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol.
Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.

4.2 Antipsychotics 3
 Phenothiazeines: SAR of Phenothiazeines - Promazine hydrochloride,
Chlorpromazine hydrochloride*, Triflupromazine, Thioridazine
hydrochloride, Piperacetazine hydrochloride, Prochlorperazine maleate,
Trifluoperazine hydrochloride.
 Ring Analogues of Phenothiazeines: Chlorprothixene, Thiothixene,
Loxapine succinate, Clozapine.
 Fluro buterophenones: Haloperidol, Droperidol, Risperidone.
 Beta amino ketones: Molindone hydrochloride.
 Benzamides: Sulpieride.
4.3 Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant 2
action
 Barbiturates: Phenobarbitone, Methabarbital.
 Hydantoins: Phenytoin*, Mephenytoin, Ethotoin
 Oxazolidine diones: Trimethadione, Paramethadione
 Succinimides: Phensuximide, Methsuximide, Ethosuximide*
 Urea and monoacylureas: Phenacemide, Carbamazepine*
 Benzodiazepines: Clonazepam
 Miscellaneous: Primidone, Valproic acid , Gabapentin, Felbamate
5 UNIT V- Drugs acting on Central Nervous System 07
5.1 General anesthetics: 3
 Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane,
Sevoflurane, Isoflurane, Desflurane.
 Ultra short acting barbitutrates: Methohexital sodium*, Thiamylal
sodium, Thiopental sodium.
 Dissociative anesthetics: Ketamine hydrochloride.*
5.2  Narcotic and non-narcotic analgesics 2
 Morphine and related drugs: SAR of Morphine analogues, Morphine
sulphate, Codeine, Meperidine hydrochloride, Anilerdine hydrochloride,
Diphenoxylate hydrochloride, Loperamide hydrochloride, Fentanyl
citrate*, Methadone hydrochloride*, Propoxyphene hydrochloride,
Pentazocine, Levorphanol tartarate.
82
  Narcotic antagonists: Nalorphine hydrochloride, Levallorphan
tartarate, Naloxone hydrochloride
5.3 Anti-inflammatory agents: Sodium salicylate, Aspirin, Mefenamic acid*, 2
Meclofenamate, Indomethacin, Sulindac, Tolmetin, Zomepriac, Diclofenac,
Ketorolac, Ibuprofen*, Naproxen, Piroxicam, Phenacetin, Acetaminophen,
Antipyrine, Phenylbutazone
Total 45

Reference Books (Latest Editions to be adopted)

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. 1-5.
9. Indian Pharmacopoeia.
10. Text book of practical organic chemistry- [Link].

83
BP403T PHYSICAL PHARMACEUTICS-II (Theory) 3 L + 1T / Week
Scope: The course deals with the various physical and physicochemical properties,
andprinciples 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.
Objectives: Upon the completion of the course student shall be able to:
1. Understand various physicochemical properties of drug molecules in the designing the
dosage forms
2. Know the principles of chemical kinetics & to use them for stability testing and
determination of expiry date of formulations
3. Demonstrate use of physicochemical properties in the formulation development and
evaluation of dosage forms
Sr. Content Hours
No.
1 UNIT I 7
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.
2 UNIT II 10
2.1 Rheology: Newtonian systems, law of flow, kinematic viscosity, effect of 7
temperature, non-Newtonian systems, pseudoplastic, dilatants, plastic,
thixotropy, thixotropy in formulation, determination of viscosity, capillary,
falling Sphere, rotational viscometers
2.2 Deformation of solids: Plastic and elastic deformation, Heckel equation, 3
Stress, Strain, Elastic Modulus
3 UNIT III - Coarse dispersion 10
3.1 Suspension, interfacial properties of suspended particles, settling in 7
suspensions, formulation of suspensions. Emulsions and theories of
emulsification, microemulsion and multiple emulsions;
3.2 Physical stability of emulsions, preservation of emulsions, rheological 3
properties of emulsions, phase equilibria and emulsion formulation.
4 UNIT IV 8
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,
84
 specific surface, methods for determining surface area, permeability,
adsorption, derived properties of powders, porosity, packing arrangement,
densities, bulkiness & flow properties.
5 UNIT V 10
5.1 Drug stability: Reaction kinetics: zero, pseudo-zero, first & second order,
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
Total 45

Reference Books (Latest Editions to be adopted)

1. Physical Pharmacy by Alfred Martin, Sixth edition
2. Experimental pharmaceutics by Eugene, Parott.
3. Tutorial pharmacy by Cooper and Gunn.
4. Stocklosam J. Pharmaceutical calculations, Lea & Febiger, Philadelphia.
5. Liberman H.A, Lachman C., Pharmaceutical Dosage forms, Tablets, Volume-1 to 3,
Marcel Dekkar Inc.
6. Liberman H.A, Lachman C, Pharmaceutical dosage forms. Disperse systems, volume 1, 2,
3. Marcel Dekkar Inc.
7. Physical Pharmaceutics by Ramasamy C, and Manavalan R.

85
BP404T PHARMACOLOGY-I (Theory) 3 L + 1T / Week
Scope: The main purpose of the subject is to understand what drugs do to the livingorganisms
and how their effects can be applied to therapeutics. The subject covers the information about
the drugs like, 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 routes of administration of different classes of drugs.

Objectives: Upon completion of this course the student should be able to

1. Understand the pharmacological actions of different categories of drugs
2. Explain the mechanism of drug action at organ system/sub cellular/ macromolecular
levels.
3. Apply the basic pharmacological knowledge in the prevention and treatment of various
diseases.
4. Observe the effect of drugs on animals by simulated experiments
5. Appreciate correlation of pharmacology with other bio medical sciences
Sr. No. Content Hours
1 UNIT I - General Pharmacology 8
1.1 Introduction to Pharmacology- Definition, historical landmarks and scope 4
of pharmacology, nature and source of drugs, essential drugs concept and
routes of drug administration, Agonists, antagonists( competitive and non-
competitive), spare receptors, addiction, tolerance, dependence,
tachyphylaxis, idiosyncrasy, allergy
1.2 Pharmacokinetics- Membrane transport, absorption, distribution, 4
metabolism and excretion of drugs .Enzyme induction, enzyme inhibition,
kinetics of elimination
2 UNIT II - General Pharmacology 12
2.1 Pharmacodynamics- Principles and mechanisms of drug action. Receptor 6
theories and classification of receptors, regulation of receptors. drug
receptors interactions signal transduction mechanisms, G-protein–coupled
receptors, ion channel receptor, transmembrane enzyme linked receptors,
transmembrane JAK-STAT binding receptor and receptors that regulate
transcription factors, dose response relationship, therapeutic index,
combined effects of drugs and factors modifying drug action.
2.2 Adverse drug reactions. 2
2.3 Drug interactions (pharmacokinetic and pharmacodynamic) 2
2.4 Drug discovery and clinical evaluation of new drugs -Drug discovery phase, 2
preclinical evaluation phase, clinical trial phase, phases of clinical trials and

86
 pharmacovigilance
3 UNIT III –Pharmacology of peripheral nervous system 10
3.1 Organization and function of ANS, Neurohumoral transmission,co- 1
transmission and classification of neurotransmitters
3.2 Parasympathomimetics, Parasympatholytics, Sympathomimetics, 3
sympatholytics
3.3 Neuromuscular blocking agents and skeletal muscle relaxants (peripheral). 2
3.4 Local anesthetic agents 3
3.5 Drugs used in myasthenia gravis and glaucoma 1
4 UNIT IV - Pharmacology of central nervous system 08
4.1 Neurohumoral transmission in the [Link] emphasis on importance of 1
various neurotransmitters like with GABA, Glutamate, Glycine, serotonin,
dopamine.
4.2 General anesthetics and pre-anesthetics. 2
4.3 Sedatives, hypnotics and centrally acting muscle relaxants 2
4.4 Anti-epileptics 2
4.5 Alcohols and disulfiram 1
5 UNIT V - Pharmacology of central nervous system 07
5.1 Psychopharmacological agents: Antipsychotics, antidepressants, anti- 2
anxiety agents, anti-manics and hallucinogens
5.2 Drugs used in Parkinsons disease and Alzheimer‘s disease. 1
5.3 CNS stimulants and nootropics 1
5.4 Opioid analgesics and antagonists 2
5.5 Drug addiction, drug abuse, tolerance and dependence. 1
Total 45
Reference Books (Latest Editions to be adopted)
1. Rang H. P., Dale M. M., Ritter J. M., Flower R. J., Rang and Dale‘s
Pharmacology,.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. [Link]. 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

87
8. Modern Pharmacology with clinical Applications, by Charles [Link]& Robert,
9. Ghosh MN. Fundamentals of Experimental Pharmacology. Hilton & Company, Kolkata.
10. Kulkarni SK. Handbook of experimental pharmacology. VallabhPrakashan

88
BP405T PHARMACOGNOSY AND PHYTOCHEMISTRY I (Theory)

3 L + 1T / Week
Scope: The subject involves the fundamentals of Pharmacognosy like scope, classification of
crude drugs, their identification and evaluation, phytochemicals present in them and their
medicinal properties.

Objectives: Upon completion of the course, the student shall be able:

1. to know the techniques in the cultivation and production of crude drugs
2. to know the crude drugs, their uses and chemical nature
3. know the evaluation techniques for the herbal drugs
4. to carry out the microscopic and morphological evaluation of crude drugs

Sr. Content Hour

No. s
1 UNIT I 10
1.1 Introduction to Pharmacognosy: 3
(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).
1.2 Classification of drugs: 2
Alphabetical, morphological, taxonomical, chemical, pharmacological,
chemo and sero taxonomical classification of drugs
1.3 Quality control of Drugs of Natural Origin: 5
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,
leafconstants, camera lucida and diagrams of microscopic objects to scale
with camera lucida.
2 UNIT II 12
2.1 Cultivation, Collection, Processing and storage of drugs of natural 10
origin:
Cultivation and Collection of drugs of natural origin
Factors influencing cultivation of medicinal plants.
Plant hormones and their applications.
Polyploidy, mutation and hybridization with reference to medicinal plants
2.2 Conservation of medicinal plants 2
3 UNIT III 7
89
 Plant tissue culture:
Historical development of plant tissue culture, types of cultures, Nutritional
requirements, growth and their maintenance.
Applications of plant tissue culture in pharmacognosy.
Edible vaccines
4 UNIT IV 10
4.1 Pharmacognosy in various systems of medicine: 3
Role of Pharmacognosy in allopathy and traditional systems of medicine
namely, Ayurveda, Unani, Siddha, Homeopathy and Chinese systems of
medicine
4.2 Introduction to secondary metabolites: 7
Definition, classification, properties and test for identification of Alkaloids,
Glycosides, Flavonoids, Tannins, Volatile oil and Resins
5 UNIT V - Study of biological source, chemical nature and uses of drugs of 08
natural origin containing following drugs
(a) Plant Products: 3
Fibers - Cotton, Jute, Hemp
Hallucinogens, Teratogens, Natural allergens

(b) Primary metabolites: 3

General introduction, detailed study with respect to chemistry, sources,
preparation, evaluation, preservation, storage, therapeutic used and
commercial utility as Pharmaceutical Aids and/or Medicines for the
following Primary metabolites:
(c) Carbohydrates: Acacia, Agar, Tragacanth, Honey
(d) Proteins and Enzymes :Gelatin, casein, proteolytic enzymes (Papain,
bromelain, serratiopeptidase, urokinase, streptokinase, pepsin).
(e) Lipids(Waxes, fats, fixed oils) : Castor oil, Chaulmoogra oil, Wool Fat, 2
Bees Wax
(f) Marine Drugs:
Novel medicinal agents from marine sources

Total 45

Reference Books (Latest Editions to be adopted)

1. [Link], 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.

90
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, [Link], IInd edition, Birla publications, New Delhi,
2007
8. Practical Pharmacognosy: C.K. Kokate, Purohit, Gokhlae
9. Anatomy of Crude Drugs by M.A. Iyengar

91