Course Identification

Preferable a basic course in organic chemistry

Introduction

   a) Drugs

   b) Receptors: General considerations

   c) Stereochemistry

   d) Structure Activity Relationships (SAR's)

   e) Absorption, Distribution and Elimination of Drugs – Lipinski Rules

   f) Drug Delivery through the blood brain barrier (BBB)

   g) Drug Metabolism

   h) Drug Toxicity

   i) Drug Tolerance and Addiction

   j) Pro-Drugs, Soft-Drugs and Hard-Drugs

   k) Patents in the Pharmaceutical Industry

Antimicrobial Agents and Antibiotics

1. Penicillins, Cephalosporins, b-Lactamase Inhibitors
2. Vancomycin
3. Tetracyclines

Anticancer Agents

1. Alkylating Agents: N-Mustards, Nitroso ureas, Pt complexes, Mitomycin
2. Antimetabolites: 5-FU, Methotrexate, Ara-C, Mercaptopurine
3. Intercalators: Actinomycin D, Adriamycin and Daunomycin
4. Epothilone
5. Antiestrogens – Tamoxifen
6. Miscellaneous Antitumor Agents: Etoposide, Taxol
7. Bisphosphonates

Anesthetics

   a) General

   b) Local

Hypnotics and Sedatives

   a) Alcohol

   b) Barbiturates

   c) Benzodiazepines

   d) Drugs of abuse

Neuropharmacological Agents

a) Adrenergics: Epi, Nor-Epi, Isoproterenol, metaproterenol, salbutamol

b) Stimulants - Amphetamines and Anorexics

c) Artificial Sweeteners

  1) Saccharin

  2) Maltitol, xylitol

  3) Acesulfame K

  4) Cyclamates

  5) Aspartame

  6) Sucralose

d) Cholinergics and Anticholinesterases

e) Choline esterase inhibitors - Nerve Gases

f) Cholinesterase Reactivators

Histamine, H-1 and H-2 Antihistamines

Prazoles

Analgesics

   1) Salicylates - Aspirin

   2) Fenamates

   3) Indomethacin and Congeners

   4) Phenyl Propionic Acids

   5) Enolic and other Acidic Agents

   6) COX2 Inhibitors

Antiviral Agents

     Ergosterol inhibitors

     Amphotericin B

     Diazoles, triazoles

Podophyllotoxin

Xanthines

    Caffeine, theophylline, theobromine

Thyroid Hormones

    T3 and T4

Topical Drugs

1. Sun blockers
2. Insect repellants
3. 5-Aminolevulinic acid PDT

Drug Delivery Systems- Prodrugs (PD's)

             1) PD's Introduction

 2) First Pass Metabolism

 3) Toxicity

 4) Hard-Drugs

 5) Ester PD's

 6) Acyloxyalkyl Ester PD's

 7) Carbamate PD's

 8) Water Solubilization via PD's

 9) Soft-Drugs

10) N-Mannic Bases

11) Amides as Amine PD's 

12) N-Hydroxymethyl PD

13) Site-specific drug delivery

14) ADEPT

15) Ring-opened PD's

16) Mutual PD's

17) Multi-pharmacophores

Hormones and Steroids.

1. Gluco- and Mineralo-corticoids – Cortisone
2. Estrogens and Progestins. The Pill.
3. Antiestrogens

4. Aromatase inhibitors
5. Bisphosphonates
6. Androgens - DHT inhibitors
7. Viagra

Cardiovascular Drugs

a) Cardiac Glycosides

b) Nitrites and Nitrates - Nitroglycerine

c) b-Blockers - Propranolol

d) Calcium-Blockers – Dihydropyridines, Diltiazem, Verapamil

e) Antihypertensive Agents

1. ACE inhibitors – “Prils”
2. Non-peptide Angiotensin II inhibitors – “Sartans”
3. Clonidine
4. Drugs affecting the Nor-Epi pathway

f) Cholesterol

 1. Antilipidemic and Anticholesterolemic agents: Vile acid sequestrants, Gemfibrozil

                        2. HMG-CoA-Reductase inhibitors: “Statins”

Major Analgesics

            1) Morphinoids: Morphine, Heroin

            2) Antitussives - Codeine

            3) Enkephalins and Endorphins

            4) Cannabinoids: THC

Antimicrobial Agents and Antibiotics

1. Sulfanilamides
2. Fluoroquinolones
3. Miscellaneous Antibiotics
4. Linezolid
5. Bacterial resistance

Antiepileptics

             a) Phenytoin

 b) Valproic acid

Antipsychotic Agents

 a) Tricyclic Antidepressants – Typical and atypical antipsychotics

 b) Non-Tricyclic Antidepressants

 c) Prozac

Upon successful completion of the course- students should be able to:

1. Demonstrate proficiency in a large variety of drugs and recognize their clinical use from their basic structures and names.
2. Describe drugs' mechanisms of action, the diseases against which the compounds are used, possible side effects, and drug interactions.
3. Explain basic principles of toxicology, structure-activity relationships, and drug design.

List of suggested literature will be presented in the first lecture