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Pharmaceutical Chemistry

Class at Faculty of Pharmacy in Hradec Králové |
GAF050

Syllabus

Definition and characterization of the subject

Historical development of pharmaceutical chemistry

Sources of new drugs

Drug nomenclature

Structural factors affecting biological activity

Drug structure modifications

Physicochemical properties in relation to biological activity

Drugs affecting the central nervous system:

? General anesthetics

? Sedative-hypnotics

? Anticonvulsants

? Neuroleptics

? Anxiolytics

? Antidepressants

? Psychostimulants

? Hallucinogens

? Antiparkinsonian agents

? Opiate analgesics

? Nonopiate analgesics

? Nonsteroidal anti-inflammatory agents

? Antiemetics

? Antitussives

? Expectorants

Drugs affecting the peripheral nervous system

? Local anesthetics

? Skeletal muscle relaxants

Drugs affecting the autonomic nervous system

? Adrenergic agents

? Antiadrenergic agents

? Cholinergic agents

? Anticholinergic and antispasmodic agents

Histamine and antihistamines

Drugs affecting blood and the cardiovascular system

? Anti-arrythmic agents

? Anticoagulants

? Antihyperlipidemics

? Cardiac glycosides

? Antihypertensive agents

? Vasodilatators

? Plasma extenders

Drugs affecting the gastrointestinal tract and kidney

? Drugs influencing gastric acidity

? Adsorbents

? Oral antidiabetic agents

? Laxatives

? Diuretics

Vitamines

Hormones

? Peptide and protein hormones

? Sex hormones and analogs

? Corticoids

? Prostaglandins

Antiinfective and antiinvasive agents

? Antiseptics and disinfectants

? Antifungal agents

? Antiprotozoals

? Antimalarials

? Synthetic antibacterial agents (sulfanilamides, quinolones)

? Antibiotics

? Antimycobacterial agents

? Anthelmintics

? Antivirals

? Antineoplastic agents

Seminars

Selected topics are discussed in more detailed manner

Practical Training

? Study of relationships between physicochemical properties and biological potencies of drugs (solubility in water, solubility in lipids, log P calculations, acidobasic properties, adsorption etc.)

? Study of relationships between steric arrangement and biological activities of drugs (modelling of representative types of drugs - hybridization of carbon atom, conformation, geometric and optical isomerism, configuration)

? Syntheses of drugs (basic types of drugs, for example paracetamol, acetylsalicylic acid, analogues of benzocain etc.)

? Practical working with basic chemical literature with special view of the Pharmaceutical Chemistry (Beilstein's Handbuch der organischen Chemie, Chemical Abstracts, International Pharmaceutical Abstracts, patent literature, Pharmazeutische Stoffliste, scientific journals etc.)

Annotation

The subject Pharmaceutical chemistry employs the knowledge obtained in preceding subjects of science and medicinal character.

It affords complete overview about drugs and adjuvants of chemical character, which is necessary to well understand consequent pharmaceutical subjects, especially Drug Control and Pharmacology. Considering this view the Pharmaceutical chemistry is an interdisciplinary subject connecting the chemical, biological and specific pharmaceutical disciplines.

Pharmaceutical chemistry comprises general and systematic part. The general part includes historical aspects of drug development, sources, nomenclature and especially the aspects of chemical structure and its modifications influence on pharmaco-dynamic as well as pharmaco-kinetic processes in the course and after drug entry into body. The relations of chemical structure and stability and interactions (chemical incompatibilities) of drugs are also of concern.

Systematic part divides drugs primarily according their indications and secondarily according their chemical structure. This viewpoint enables comparison of drugs related in clinical used but different in their chemical structure and mechanism of action. This classification connect the pharmaceutical chemistry and pharmacology and it is important considering clinical aspects since it corresponds to currently commonly used division of drugs into anatomic-therapeutic-chemical classification. Specific area of interest in pharmaceutical chemistry is structure-biological activity studies and their employment in new more effective and safer drug design and development.