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B Pharm Medicinal Chemistry Pdf Notes

Updated: Feb 15


B. Pharm Medicinal Chemistry - where molecules dance with disease, transforming into life-saving symphonies. Feeling lost in the labyrinth of drug mechanisms, target interactions, and intricate metabolic pathways? Fear not, aspiring pharmacists! We have a potent elixir to unlock these secrets – B. Pharm Medicinal Chemistry PDF notes.


B Pharm Medicinal Chemistry Notes
B Pharm Medicinal Chemistry Notes

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 subject 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


B Pharm Medicinal Chemistry Pdf Notes


Unit 1


Chapter 1

Introduction to Medicinal Chemistry, History and development of medicinal chemistry


Chapter 2 (Physicochemical properties)

Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.


Chapter 2 (Drug metabolism)

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





Unit 2


Chapter 1

Drugs acting on Autonomic Nervous System

Chapter 2 (Adrenergic Neurotransmitters)

Biosynthesis and catabolism of catecholamine. Adrenergic receptors (Alpha & Beta) and their distribution.

Chapter 3 (Sympathomimetic agents)

Direct acting: Nor-epinephrine, Epinephrine, Phenylephrine*, Dopamine, 89 Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline, Salbutamol*, Bitolterol, Naphazoline, Oxymetazoline and Xylometazoline.  Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine.  Agents with mixed mechanism: Ephedrine, Metaraminol.


Chapter 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.





Unit 3


Chapter 1 (Parasympathomimetic Agents)

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 4 (Drugs acting on Central Nervous System)


Chapter 1 (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.


Chapter 2 (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.


Chapter 3 (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 5


Chapter 1 (General anesthetics)


Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane, Sevoflurane, Isoflurane, Desflurane.

Ultra short acting barbitutrates: Methohexital sodium*, Thiamylal sodium, Thiopental sodium.

Dissociative anesthetics: Ketamine hydrochloride.*


Chapter 2 (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.


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