Pharmaceutical Chemistry

Chapter Topic Introduction to Pharmaceutical chemistry: Scope and objectives Sources and types of errors: Accuracy, precision, significant figures Impurities in Pharmaceuticals: Source and effect of impurities in Pharmacopoeial substances, importance of limit test, Principle and procedures of Limit tests for chlorides, sulphates, iron, heavy metals and arsenic.

Volumetric analysis:

Fundamentals of volumetric analysis, Acid-base titration, non-aqueous titration, precipitation titration, complexometric titration, redox titration Gravimetric analysis: Principle and method.

Inorganic Pharmaceuticals:

Pharmaceutical formulations, market preparations, storage conditions and uses of ● Haematinics: Ferrous sulphate, Ferrous fumarate, Ferric ammonium citrate, Ferrous ascorbate, Carbonyl iron ● Gastro-intestinal Agents:

Antacids :Aluminium hydroxide gel, Magnesium hydroxide, Magaldrate, Sodium bicarbonate, Calcium Carbonate, Acidifying agents, Adsorbents, Protectives, Cathartics ● Topical agents:

Silver Nitrate, Ionic Silver, Chlorhexidine Gluconate, Hydrogen peroxide, Boric acid, Bleaching powder, Potassium permanganate ● Dental products:

Calcium carbonate, Sodium fluoride, Denture cleaners, Denture adhesives, Mouth washes ● Medicinal gases: Carbon dioxide, nitrous oxide, oxygen Introduction to nomenclature of organic chemical systems with particular reference to heterocyclic compounds containing up to Three rings Study of the following category of medicinal compounds with respect to classification, chemical name, chemical structure (compounds marked with*) uses, stability and storage conditions, different types of formulations and their popular brand names Drugs Acting on Central Nervous System • Anaesthetics:

Thiopental Sodium*, Ketamine Hydrochloride*, Propofol ● Sedatives and Hypnotics: Diazepam*, Alprazolam*, Nitrazepam, Phenobarbital* ● Antipsychotics:

Chlorpromazine Hydrochloride*, Haloperidol*, Risperidone*, Sulpiride*, Olanzapine, Quetiapine, Lurasidone ● Anticonvulsants:

Phenytoin*, Carbamazepine*, Clonazepam, Valproic Acid*, Gabapentin*, Topiramate, Vigabatrin, Lamotrigine ● Anti-Depressants:

Amitriptyline Hydrochloride*, Imipramine Hydrochloride*, Fluoxetine*, Venlafaxine, Duloxetine, Sertraline, Citalopram, Escitalopram, Fluvoxamine, Paroxetine Drugs Acting on Autonomic Nervous System ● Sympathomimetic Agents: Direct Acting: Nor- Epinephrine*, Epinephrine, Phenylephrine, Dopamine*, Terbutaline, Salbutamol (Albuterol), Naphazoline*, Tetrahydrozoline.

Indirect Acting Agents: Hydroxy Amphetamine, Pseudoephedrine.

Agents With Mixed Mechanism:

Ephedrine, Metaraminol ● Adrenergic Antagonists: Alpha Adrenergic Blockers:

Tolazoline, Phentolamine ● Phenoxybenzamine, Prazosin.

Beta Adrenergic Blockers: Propranolol*, Atenolol*, Carvedilol ● Cholinergic Drugs and Related Agents: Direct Acting Agents:

Acetylcholine*, Carbachol, And Pilocarpine. Cholinesterase Inhibitors: Neostigmine*, Edrophonium Chloride, Tacrine Hydrochloride, Pralidoxime Chloride, Echothiopate Iodide ● Cholinergic Blocking Agents: Atropine Sulphate*, Ipratropium Bromide Synthetic Cholinergic Blocking Agents:

Tropicamide, Cyclopentolate Hydrochloride, Clidinium Bromide, Dicyclomine Hydrochloride* Drugs Acting on Cardiovascular System ● Anti-Arrhythmic Drugs:

Quinidine Sulphate, Procainamide Hydrochloride, Verapamil, Phenytoin Sodium*, Lidocaine Hydrochloride, Lorcainide Hydrochloride, Amiodarone and Sotalol ● Anti-Hypertensive Agents: Propranolol*, Captopril*, Ramipril, Methyldopate Hydrochloride, Clonidine Hydrochloride, Hydralazine Hydrochloride, Nifedipine, ● Antianginal Agents: Isosorbide Dinitrate Diuretics:

Acetazolamide, Frusemide*, Bumetanide, Chlorthalidone, Benzthiazide, Metolazone, Xipamide, Spironolactone Hypoglycemic Agents: Insulin and Its Preparations, Metformin*, Glibenclamide*, Glimepiride, Pioglitazone, Repaglinide, Gliflozins, Gliptins Analgesic And Anti-Inflammatory Agents: Morphine Analogues, Narcotic Antagonists; Nonsteroidal Anti- Inflammatory Agents (NSAIDs) - Aspirin*, Diclofenac, Ibuprofen*, Piroxicam, Celecoxib, Mefenamic Acid, Paracetamol*, Aceclofenac Anti-Infective Agents ● Antifungal Agents: Amphotericin-B, Griseofulvin, Miconazole, Ketoconazole*, Itraconazole, Fluconazole*, Naftifine Hydrochloride ● Urinary Tract Anti-Infective Agents: Norfloxacin, Ciprofloxacin, Ofloxacin*, Moxifloxacin, ● Anti-Tubercular Agents: INH*, Ethambutol, Para Amino Salicylic Acid, Pyrazinamide, Rifampicin, Bedaquiline, Delamanid, Pretomanid* ● Antiviral Agents:

Amantadine Hydrochloride, Idoxuridine, Acyclovir*, Foscarnet, Zidovudine, Ribavirin, Remdesivir, Favipiravir ● Antimalarials:

Quinine Sulphate, Chloroquine Phosphate*, Primaquine Phosphate, Mefloquine*, Cycloguanil, Pyrimethamine, Artemisinin ● Sulfonamides: Sulfanilamide, Sulfadiazine, Sulfametho xazole, Sulfacetamide*, Mafenide Acetate, Cotrimoxazole, Dapsone* Antibiotics: Penicillin G, Amoxicillin*, Cloxacillin, Streptomycin, Tetracyclines: Doxycycline, Minocycline, Macrolides: Erythromycin, Azithromycin, Miscellaneous:

Chloramphenicol* Clindamycin Anti-Neoplastic Agents: Cyclophosphamide*, Busulfan, Mercaptopurine, Fluorouracil*, Methotrexate, Dactinomycin, Doxorubicin Hydrochloride, Vinblastine Sulphate, Cisplatin*, Dromostanolone Propionate PHARMACEUTICAL CHEMISTRY – PRACTICAL Course Code: ER20-12P 75 Hours (3 Hours/week) Scope: This course is designed to impart basic training and hands-on experiences to synthesis chemical substances used as drugs and pharmaceuticals. Also, to perform the quality control tests, impurity testing, test for purity and systematic qualitative analysis of chemical substances used as drugs and pharmaceuticals.

Course Objectives: This course will provide the hands-on experience on the following aspects of chemical substances used as drugs and pharmaceuticals

1. Limit tests and assays of selected chemical substances as per the monograph

2. Volumetric analysis of the chemical substances

3. Basics of preparatory chemistry and their analysis

4. Systematic qualitative analysis for the identification of the chemical drugs Course Outcomes: Upon successful completion of this course, the students will be able to

1. Perform the limit tests for various inorganic elements and report

2. Prepare standard solutions using the principles of volumetric analysis

3. Test the purity of the selected inorganic and organic compounds against the monograph standards

4. Synthesize the selected chemical substances as per the standard synthetic scheme

5. Perform qualitative tests to systematically identify the unknown chemical substances Practicals S. No.

Experiment Limit test for ● Chlorides; sulphate; Iron; heavy metals Identification tests for Anions and Cations as per Indian Pharmacopoeia Fundamentals of Volumetric analysis Preparation of standard solution and standardization of Sodium Hydroxide, Potassium Permanganate Assay of the following compounds ● Ferrous sulphate- by redox titration ● Calcium gluconate-by complexometric ● Sodium chloride-by Modified Volhard's method ● Ascorbic acid by iodometry ● Ibuprofen by alkalimetry Fundamentals of preparative organic chemistry Determination of Melting point and boiling point of organic compounds Preparation of organic compounds • Benzoic acid from Benzamide • Picric acid from Phenol Identification and test for purity of pharmaceuticals Aspirin, Caffeine, Paracetamol, Sulfanilamide Systematic Qualitative analysis experiments (4 substances) Assignments The students shall be asked to submit the written assignments on the following topics (One assignment per student per sessional period. i.e., a minimum of THREE assignments per student)

1. Different monographs and formularies available and their major contents

2. Significance of quality control and quality assurance in pharmaceutical industries

3. Overview on Green Chemistry

4. Various software programs available for computer aided drug discovery

5. Various instrumentations used for characterization and quantification of drug