Resprn in Humns-KDB by on Scribd
Friday, February 22, 2019
Thursday, February 21, 2019
Monday, February 4, 2019
SYLLABUS
MEDICINAL
CHEMISTRY – I (Practical)
Subject code: BP406P.
Duration:
4 Hours/Week
I Preparation of
drugs/ intermediates
1. 1,3-pyrazole
2. 1,3-oxazole
3. Benzimidazole
4. Benztriazole
5. 2,3- diphenyl
quinoxaline
6. Benzocaine
7. Phenytoin
8. Phenothiazine
9. Barbiturate
II Assay of
drugs
1.
Chlorpromazine
2.
Phenobarbitone
3. Atropine
4. Ibuprofen
5. Aspirin
6. Furosemide
III
Determination of Partition coefficient for any two drugs
Recommended
Books (Latest Editions)
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- A.I.Vogel.
.
SYLLABUS
MEDICINAL
CHEMISTRY – I (Theory)
Subject code: BP402T
Duration:
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
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
Course
Content:
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 (*)
UNIT- I 10
Hours
Introduction to
Medicinal Chemistry
History and
development of medicinal chemistry
Physicochemical
properties in relation to biological action
Ionization,
Solubility, Partition Coefficient, Hydrogen bonding, Protein binding,
Chelation, ioisosterism, Optical and
Geometrical isomerism.
Drug metabolism
Drug metabolism
principles- Phase I and Phase II.
Factors
affecting drug metabolism including stereo chemical aspects.
UNIT- II 10
Hours
Drugs acting on
Autonomic Nervous System
Adrenergic
Neurotransmitters:
Biosynthesis and
catabolism of catecholamine.
Adrenergic
receptors (Alpha & Beta) and their distribution.
Sympathomimetic
agents: SAR of Sympathomimetic agents
Direct
acting: Nor-epinephrine, Epinephrine, Phenylephrine*,
Dopamine, Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol*,
Bitolterol, Naphazoline, Oxymetazoline and Xylometazoline.
Indirect
acting agents: Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine.
Agents
with mixed mechanism: Ephedrine, Metaraminol.
Adrenergic
Antagonists:
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.
UNIT-III 10
Hours
Cholinergic
neurotransmitters:
Biosynthesis and
catabolism of acetylcholine.
Cholinergic
receptors (Muscarinic & Nicotinic) and their distribution.
Parasympathomimetic
agents: SAR of Parasympathomimetic agents
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.
Cholinergic
Blocking agents: SAR of cholinolytic agents
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.
UNIT- IV 08
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*, Phenobarbital, Mephobarbital, Amobarbital,
Butabarbital, Pentobarbital, Secobarbital
Miscelleneous:
Amides &
imides: Glutethmide. Alcohol & their carbamate derivatives: Meprobomate,
Ethchlorvynol.
Aldehyde &
their derivatives: Triclofos sodium, Paraldehyde.
B.
Antipsychotics
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.
C.
Anticonvulsants: SAR of Anticonvulsants, mechanism
of anticonvulsant 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
UNIT – V 07
Hours
Drugs acting on
Central Nervous System
General
anesthetics:
Inhalation
anesthetics: Halothane*, Methoxyflurane, Enflurane, Sevoflurane,
Isoflurane, Desflurane.
Ultra short
acting barbitutrates: Methohexital sodium*, Thiamylal sodium,
Thiopental sodium.
Dissociative
anesthetics: Ketamine hydrochloride.*
Narcotic and
non-narcotic analgesics
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.
Narcotic
antagonists: Nalorphine hydrochloride, Levallorphan
tartarate, Naloxone hydrochloride.
Anti-inflammatory
agents: Sodium salicylate, Aspirin, Mefenamic acid*, Meclofenamate,
Indomethacin, Sulindac, Tolmetin, Zomepriac, Diclofenac, Ketorolac, Ibuprofen*,
Naproxen, Piroxicam, Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone.
Subscribe to:
Posts (Atom)
