Bachelor of pharmacy (B. Pharm) course




НазваниеBachelor of pharmacy (B. Pharm) course
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3.1: Medicinal Chemistry – I



THEORY 75 Hours (3hrs/week)



I.

Basic Principles of Medicinal Chemistry




A.

Introduction, History and development of medicinal chemistry.

Fundamental principles of drug therapy

2 Hrs

B.

Physicochemical properties in relation to biological action:

6 Hrs




Ionization, Solubility, Partition Coefficient, hydrogen bonding, protein binding, chelation, isosterism, optical and geometrical isomerism, steric effect, redox potential and surface activity.




C.

Drug metabolism:

6 Hrs




General pathways of drug metabolism (different types of reaction in phase-I and phase-II with examples), factors affecting drug metabolism including stereochemical aspects, significance of drug metabolism in medicinal chemistry.








Study of classification, mechanism of action, structure activity relationship physiochemical properties and synthesis of selected drugs (only drugs marked with asterisk) on the following categories of drugs.
















II.

Drugs acting on CNS








A.

General anesthetics: Halothane*, Methoxyflurane*, Enflurane, Sevoflurane, Isoflurane, Desflurane, Methohexital sodium*, Thiamylal sodium*, Thiopental sodium, Etomidate, Propofol, Ketamine hydrochloride*.

2 Hrs

B.

Sedatives and Hypnotics

3 Hrs

Benzodiazepines: SAR of Benzodiazepines, Chlordiazepoxide*, Diazepam*, Oxazepam, Chlorazepate Dipotassium, Prazepam, Lorazepam, Halazepam, Flurazepam, Alprazolam, Triazolam,

Barbiturtes: SAR of barbiturates, Barbital*, Phenobarbital, Mephobarbital, Amobarbital, Butabarbital, Talbutal, Pentobarbital, Secobarbital,

Miscelleneous: Triclofos sodium*, Paraldehyde.

C.

Antipsychotics

4 Hrs

Phenothiazeines: SAR of Phenothiazeines - Promazine hydrochloride*, Chlorpromazine hydrochloride*, Triflupromazine, Thioridazine hydrochloride, Piperacetazine hydrochloride, Mesoridazine hydrochloride, , Prochlorperazine maleate*, Trifluoperazine hydrochloride

Ring analogues of phenothiazines: Chlorprothixene, Thiothixene, Loxapine succinate, Clozapine. Fluro buterophenones: Haloperidol, Droperidol, Risperidone.

Beta amino ketones: MolindoneHcl. Benzamides: Sulpieride.

D.

Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant action.

3 hrs

Hydentoins: Phenytoin*, Mephenytoin, Ethotoin,

Oxazolidine diones: Trimethadione*, Paramethadione,

Succinimides: Phensuximide, Methsuximide, Ethosuximide*,

Urea and monoacylureas: Phenacemide, Carbamazepine*,

Benzodiazepines: Clonazepam.

Miscellaneous: Primidone, Valproic acid* , Gabapentin, Felbamate

E.

CNS stimulants




Analeptics- Nikethamide*, Doxapram hydrochloride, Pentylenetetrazole, Caffeine, Theophylline, Theobromine

1 Hr

Psycomotor stimulants- Amphetamine, Dextroamphetamine sulphate*, Methamphetamine, Chorphentermine, Chlortermine., Phendimetrazine, Methylphenidate, Pemoline

2 Hrs

MAO inhibitors- Phenelzine sulphate, Isocarboxazid, Tranylcypromine, Pargyline hydrochloride.

1 Hr

Tricyclic anti-depressants - Amitriptyline hydrochloride*, Nor tryptyline, Imipramine hydrochloride*, Desipramine hydrochloride, Trimipramine maleate, Doxepin hydrochloride, Amoxapine, Fluoxetine.

2 Hrs

III.

Drugs acting on Autonomic Nervous System







A.

Adrenergic Neurotransmitters: Structure and physiochemical properties, biosynthesis and metabolism.

2 Hrs

Adrenergic receptors: alpha and beta- adrenergic receptors, their distribution in the human body.

B.

Sympathomimetic agents: SAR of Sympathomimetic agents.

3 Hrs

Direct acting: Nor-epinephrine, Epinephrine,Phenylephrine*, Dopamine, Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline*, Salmeterol, Salbutamol*, Bitolterol, Albuterol, Ritodrine, Naphazoline, Tetrahydrozoline, Oxymetazoline and Xylometazoline.

Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine, Propylhexedrine.

Agents with mixed mechanism: Ephedrine*, Metaraminol.

C.

Adrenergic Antagonists:

3 Hrs

Alpha adrenergic blockers: Tolazoline*, Phentolamine*, Phenoxybenzamine, Prazosin, Tetrazosin, Doxazosin, Ergotamine, Methysergide.




Beta adrenergic blockers: SAR of beta blockers, Propranolol*, Dichloroisoproterenol, Practolol, Metibranolol, Acebutolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol, Labetolol and Carvedilol.






D.

Cholinergic drugs and related agents:

5 Hrs

Cholinergic neurotransmitters: function, structure, biosynthesis and metabolism of acetylcholine. Cholinergic receptors: muscaranic and nicotinic receptors, their distribution in the human body

Direct acting agents: SAR, Acetylcholine*, Carbachol*, Bethanechol, Methacholine, Pilocarpine,

Cholinesterase inhibitors: Physostigmine, Neostigmine, Pyridostigmine*, Edrophonium chloride, Tacrine hydrochloride, Ambenonium chloride, Pralidoxime chloride, Isofluorphate, Echothiophate iodide, Parathione, Malathion.



E.

Cholinergic Blocking agents:

4 Hrs

SAR of cholinolytic agents.




Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine sulphate, Scopolamine hydrogenbromide, Homatropine hydrogenbromide*, 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, and Ethopropazine hydrochloride







IV.

Drugs acting on Cardiovascular System

3 Hrs

A.

Anti-anginal: Vasodilators: Amyl nitrite, Nitroglycerin*, Pentaerythritol tetranitrate, Isosorbide dinitrite*, Dipyridamole. Cardiotonics: Digoxin, Digitoxin, Deslanoside.





Calcium channel blockers: Verapamil, Diltiazem hydrochloride, Nifedipine, Amlodipine, Bepridil hydrochloride, Felodipine, Nicardipine, Nimodipone.

B.

Anti-arrythmic Drugs:

2 Hrs

Quinidine sulphate, Procainamide hydrochloride, Disopyramide phosphate*,

Phenytoin sodium, Lidocaine hydrochloride, Tocainide hydrochloride Mexiletine hydrochloride, , Lorcainide hydrochloride, amiodarone and Sotalol.



C.

Anti-hypertensive Agents: Propranolol, timolol, Captopril, Lisinopril, Enalapril, Benazepril hydrochloride, Quinapril hydrochloride, Methyldopate hydrochloride,* Clonidine hydrochloride, Guanethidine monosulphate*, Guanabenz acetate, Sodium nitroprusside, Diazoxide, Minoxidil.Reserpine, Hydralazine hydrochloride



3 Hrs

D.

Diuretics:

5 Hrs

  1. Carbonic anhydrase inhibitors: Acetazolamide*, Methazolamide, Dichlorphenamide.

  2. Thiazides: Chlorthiazide*, Hydrochlorothiazide*, Hydroflumethiazide, Cyclothiazide,

  3. Loop diuretics: Furosemide*, Bumetanide, Ethacrynic acid.

  4. Potassium sparing Diuretics: Spironolactone, Triamterene, Amiloride*

  5. Miscelleneous: Mannitol, and Theophylline

E.

  1. Anti-hyperlipidemic agents: Clofibrate, lovastatin, cholesteramine and cholestipol

  2. Anticoagulants: Warferin*, phenindione.

  3. Synthetic hypoglycemic agents: tolbutamide, metformin, glipizide, pioglitazone, acarabose

3 Hrs

V.




Local Anesthetics: SAR of Local anaesthetics; Cocaine, Hexylcaine, Meprylcaine, Cyclomethycaine, Piperocaine,Benzocaine*, Butamben, Procaine*, Butacaine, Propoxycaine, Tetracaine, Benoxinate, Lignocaine*,Mepivacaine, Prilocaine, Etidocaine, Phenacaine, Diperodon, Dibucaine* and Dyclonine.

3 Hrs

VI.

Analgesics, antipyretics and anti-inflammatory drugs

4 Hrs

A.

Morphine and related drugs: SAR of morphine analogues; Morphine sulphate, Codeine phosphate. Hydromorphone hydrochloride, Meperidine hydrochloride*, Alphaprodine hydrochloride, Anilerdine hydrochloride, Diphenoxylate hydrochloride, Loperamide hydrochloride, Fentanyl citrate*, Methadone hydrochloride*, Propoxyphene hydrochloride, Pentazocine, Levorphanol tartarate, Narcotic antagonists: Nalorphine hydrochloride, Levallorphan tartarate and Naloxone hydrochloride,

Anti-tussives: Noscapine, Dextromethorphan hydrobromide and Benzonatate, Carbetapentane.





B.

Anti-inflammatory agents: Sodium salicylate, Aspirin, Salsalate*, Mefenamic acid, Meclofenamate sodium, Indomethacin*, Sulindac, Tolmetin sodium, Zomepriac sodium, Diclofenac sodium, Ketorolac, Ibuprofen*, Naproxen*, Piroxicam, Phenacetin, Acetaminophen, Antipyrine, Aminopyrine, Phenylbutazone* and Oxyphenbutazone.

3 Hrs



3.1: Medicinal Chemistry – I (Practicals)

3 Hours/Week


1. Preparation of medicinally important compounds or intermediates required for synthesis of drugs (10 drugs)

  1. Phenothiazine from Diphenylamine

  2. Phenytoin from Benzoin.

  3. Paracetomol from P-amino phenol.

  4. Benzocaine from PABA.

  5. 4-hydroxy coumarin from resorcinol.

  6. Mefenamic acid from anthranilic acid.

  7. 1,4 - Napthoquinone from naphthalene.

  8. 2,4,5 Triphenyl imidazole from Benzoin,

  9. Cinnamic acid from Perkin’s reaction.

  10. Aryloxy acetic acid from phenols

  11. o-iodo benzoic acid from anthranilic acid

  12. Dimethyl amino propiophenone from acetophenone


2. Monograph analysis of selected drugs from course content (5 experiments)

3. Assay of Selected drugs from course content prescribed as per I.P or B.P. (8 drugs)

  1. Assay of Ibuprofen by alkalimetry.

  2. Assay of Diclofenac by alkalimetry

  3. Assay of Analgin by Iodimetry.

  4. Assay of Ephedrine hydrochloride by non aqueous titrimetry.

  5. Assay of Phenobarbitone by non aqueous titrimetry.

  6. Assay of Procaine or Benzocaine by diazotization.

  7. Assay of Chlorpromazine by cerrimetry.


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