2 PHARMACEUTICAL CHEMISTRY

PHARMACEUTICAL CHEMISTRY – THEORY

 

Course Code: ER20-12T                                                         75 Hours (3 Hours/week)

Scope: This course is designed to impart basic knowledge on the chemical structure, storage conditions and medicinal uses of organic and inorganic chemical substances used as drugs and pharmaceuticals. Also, this course discusses the impurities, quality control aspects of chemical substances used in pharmaceuticals.

Course Objectives: This course will discuss the following aspects of the chemical substances used as drugs and pharmaceuticals for various disease conditions

  1. Chemical classification, chemical name, chemical structure
  2. Pharmacological uses, doses, stability and storage conditions
  3. Different types of formulations / dosage form available and their brand names
  4. Impurity testing and basic quality control tests

Course Outcomes: Upon successful completion of this course, the students will be able to

  1. Describe the chemical class, structure and chemical name of the commonly used drugs and pharmaceuticals of both organic and inorganic nature
  2. Discuss the pharmacological uses, dosage regimen, stability issues and storage conditions of all such chemical substances commonly used as drugs
  3. Describe the quantitative and qualitative analysis, impurity testing of the chemical substances given in the official monographs
  4. Identify the dosage form & the brand names of the drugs and pharmaceuticals popular in the marketplace

Chapter

Topic

Hours

1

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.

8

2

Volumetric analysis: Fundamentals of volumetric analysis, Acid-base titration, non-aqueous titration, precipitation titration, complexometric titration, redox titration

Gravimetric analysis: Principle and method.

8

 

 

3

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

7

4

Introduction to nomenclature of organic chemical systems with   particular    reference    to    heterocyclic   compounds

containing up to Three rings

2

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

5

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

9

6

Drugs Acting on Autonomic Nervous System

  • Sympathomimetic    Agents:    Direct    Acting:    Nor- Epinephrine*,            Epinephrine,                                    Phenylephrine,

9

 

 

 

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*

 

7

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

5

8

Diuretics:     Acetazolamide,    Frusemide*,     Bumetanide, Chlorthalidone,    Benzthiazide,    Metolazone,    Xipamide,

Spironolactone

2

9

Hypoglycemic Agents: Insulin and Its Preparations, Metformin*,    Glibenclamide*,   Glimepiride,                        Pioglitazone,

Repaglinide, Gliflozins, Gliptins

3

10

Analgesic And Anti-Inflammatory Agents: Morphine Analogues, Narcotic Antagonists; Nonsteroidal Anti- Inflammatory Agents (NSAIDs) - Aspirin*, Diclofenac, Ibuprofen*, Piroxicam, Celecoxib, Mefenamic Acid,

Paracetamol*, Aceclofenac

3

11

Anti-Infective Agents

  • Antifungal     Agents:    Amphotericin-B,    Griseofulvin,

Miconazole,             Ketoconazole*,             Itraconazole, Fluconazole*, Naftifine Hydrochloride

8

 

 

 
  • 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*

 

12

Antibiotics: Penicillin G, Amoxicillin*, Cloxacillin, Streptomycin, Tetracyclines: Doxycycline, Minocycline, Macrolides: Erythromycin, Azithromycin, Miscellaneous:

Chloramphenicol* Clindamycin

8

13

Anti-Neoplastic Agents: Cyclophosphamide*, Busulfan, Mercaptopurine,             Fluorouracil*,             Methotrexate, Dactinomycin, Doxorubicin Hydrochloride, Vinblastine

Sulphate, Cisplatin*, Dromostanolone Propionate

3

 

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

1

Limit test for

  • Chlorides; sulphate; Iron; heavy metals

2

Identification tests for Anions and Cations as per Indian Pharmacopoeia

3

Fundamentals of Volumetric analysis

Preparation    of    standard    solution    and    standardization    of                        Sodium Hydroxide, Potassium Permanganate

4

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

5

Fundamentals of preparative organic chemistry

Determination of Melting point and boiling point of organic compounds

6

Preparation of organic compounds

  • Benzoic acid from Benzamide
  • Picric acid from Phenol

7

Identification and test for purity of pharmaceuticals

Aspirin, Caffeine, Paracetamol, Sulfanilamide

8

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