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

Course: B. Pharmacy  IVth Semester / 2nd year

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

Subject Code: BP402T

Sr. No.

Contents of the Topic

Learning Objectives Teaching Guidelines Methodology Time (Hrs)
1 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, Bioisosterism, Optical and Geometrical isomerism.

 To describe the fundamental of medicinal chemistry and different aspects of physicochemical properties of drug molecules.
To Study the effect of physicochemical properties on biological activity of drug molecules.
Explain about the introduction and historical background of medicinal chemistry.
Brief discussion about the terms like solubility,  Ionization, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.
Instructive

Power point presentation

 

Tutorials

05
2 Drug metabolism
Drug metabolism principles- Phase I and Phase II.

Factors affecting drug metabolism including stereo chemical aspects.

To describe the drug metabolic pathways, adverse drug reactions.
To Know the therapeutic applications of drug metabolism
Process of drugs metabolism and types of metabolism processes. Instructive

Power point presentation

 

Group discussion

05
2 Drugs acting on Autonomic Nervous System
Adrenergic Neurotransmitters:

Biosynthesis and catabolism of catecholamine.

Adrenergic receptors (Alpha & Beta) and their distribution.

 To Impart their knowledge on the structure, chemistry and therapeutic value of drugs acting on Autonomic Nervous System.

To describe the biosynthesis and catabolism of catecholamines.  Study the physicochemical properties and metabolism of drugs

Introduction about the autonomic nervous system and different receptors available for the mechanism. Instructive

Power point presentation

 

Tutorials

 

03
3 Sympathomimetic agents: SAR of Sympathomimetic agents

Direct  acting:  Norepinephrine,  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.

To describe the chemistry of drugs with respect to their pharmacological activity.
To explain  the Structure Activity Relationship (SAR) studies of Sympathomimetic drugs.
Describe  the chemical synthesis of some drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship of sympathomimetic agents and its uses. Instructive

Power point presentation

 

Tutorials

04
4 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.
To describe the definition, mechanism of action, classification,
structure, chemistry and therapeutic value of α and β adrenergic blockers.
To explain the Structure Activity Relationship (SAR) studies of Adrenergic Antagonists.
Describe the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship of adrenergic antagonists and its uses. Instructive

Power point presentation

 

Tutorials

03
5 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.

To describe the definition, mechanism of action, classification, chemistry, pharmacological activity and Structure Activity Relationship studies of Cholinergic neurotransmitters.
Describe the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship of cholinergic agents and its uses. Instructive

Power point presentation

 

Tutorials

05
6 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.

To Explain the definition, classification, chemistry, structure, mechanism of action, pharmacological activity and Structure Activity Relationship studies of Cholinergic blocking agents.
Enumerate the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship of cholinergic blocking agents and its uses. Instructive

Power point presentation

 

Group discussion

05
7 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

Miscellaneous:
Amides & imides: Glutethmide.
Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol.
Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.

To describe the definition, classification, chemistry, mechanism of action and therapeutic value of drugs acting on Central Nervous System.
Discuss about Structure Activity Relationship (SAR) studies of these drugs.
Describe the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship of Hypnotics and sedative agents and its uses. Instructive

Power point presentation

 

Group discussion

03
8 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.
To describe the definition, classification, chemistry, mechanism of action, pharmacological activity and Structure Activity Relationship studies of Antipsychotics.
Explain the chemical synthesis of selected antipsychotic drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship of Antipsychotics agents and its uses. Instructive

Power point presentation

 

Tutorials

03
9 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
To describe the definition, classification, mechanism of action,  structure, chemistry and therapeutic value of drugs acting on Central Nervous System.
Discuss about Structure Activity Relationship (SAR) studies of these drugs.
Enumerate the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship, mechanism of action of Anticonvulsants agents and its uses. Instructive

Power point presentation

 

Group discussion

02
10 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.*

 

To Explain the definition, structure, mechanism of action, chemistry and therapeutic value of drugs acting on Central Nervous System and to discuss the Structure Activity Relationship (SAR) studies of these drugs.
To Describe the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship, mechanism of action of Anesthetics agents and its uses. Instructive

Power point presentation

 

Group discussion

02
11 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.

To describe the definition, classification, mechanism of action, structure, chemistry and Structure Activity Relationship studies of narcotic agonist drugs and narcotic antagonists.
Describe the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis and structure activity relationship, mechanism of action of Narcotic and non-narcotis analgesics agents and its uses. Instructive

Power point presentation

 

Tutorials

02
12 Anti-inflammatory agents: Sodium salicylate, Aspirin, Mefenamic acid*, Meclofenamate, Indomethacin, Sulindac, Tolmetin, Zomepriac, Diclofenac, Ketorolac, Ibuprofen*, Naproxen, Piroxicam, Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone. To describe the definition, classification, mechanism of action, structure, chemistry and Structure Activity Relationship studies of Anti-inflammatory agents.
Describe the chemical synthesis of selected drugs marked with asterisk
Classification, methods of synthesis, structure activity relationship and mechanism of action of Anti-inflammatory agents and its uses. Instructive

Power point presentation

Group discussion

03