Medicinal Chemistry-I Book B.Pharm 4th Semester

                                                                         (BP402T)- MEDICINAL CHEMISTRY - I

Module-1                                                                                    (10 Hours)

Medicinal Chemistry

• Introduction, 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.

Drug metabolism

• Drug metabolism principles-Phase I and Phase II.
• Factors affecting drug metabolism including stereo chemical aspects.

Module-2                                                                                    (10 Hours)

Drugs acting on Autonomic Nervous System

• Adrenergic Neurotransmitters: Biosynthesis and catabolism of catecholamine.
• Adrenergic receptors (Alpha and 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.

Module-3                                                                                    (10 Hours)

Cholinergic Neurotransmitters

• Biosynthesis and catabolism of acetylcholine.
• Cholinergic receptors (Muscarinic and Nicotinic) and their distribution.

Parasympathomimetic Agents: SAR of Parasympathomimetic Agents

• Direct Acting Agents: Acetylcholine, Carbachol*, Bethanechol, Methacholine, Pilocarpine.
• ‘Indirect acting/ Cholinesterase inhibitors (Reversible and 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.

Module-4                                                                                    (08 Hours)

Drugs acting on Central Nervous System

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 and Imides: Glutethmide.
• Alcohol and their Carbamate Derivatives: Meprobomate, Ethchlorvynol. Aldehyde and their derivatives: Triclofos sodium, Paraldehyde.

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.

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.

Module-5                                                                                    (07 Hours)

Drugs acting on Central Nervous System

General Anaesthetics

• 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.