med org lec 2

• Emperor Shen Nung


  Father of Chinese agriculture and Chinese medicine, tasted hundreds of medicinal herbs to test their medicinal value
• Ipecacuanha is used for the treatment of Dysentery and Amoebiasis
• MEDICINAL CHEMISTRY is the chemistry discipline concerned with the design, development and synthesis of pharmaceutical drugs
• PARACELSUS, also known as Philippus Aureolus Theophrastus Bombastus Von Hohenheim, was one of the first scientists to introduce chemistry to medicine
• 19th-century discoveries

  • Isolated cocaine from Erythroxylon coca
  • Isolated physostigmine from Calabar bean
• Psychopharmacologic agents

  • Stimulants and Depressants
  • Anxiolytics & hypnotics
  • Antipsychotics
  • Antimanic agents
  • Anticonvulsants
  • Antidepressants
• Penicillin was discovered by Alexander Fleming in 1929
• MEDICINAL CHEMISTRY


  Combines expertise from chemistry and pharmacology to identify, develop and synthesize chemical agents that have a therapeutic use and to evaluate the properties of existing drugs
• Ma Huang (Ephedra sinica) is one of the drugs tasted by Emperor Shen Nung, from which Ephedrine was isolated
• Diseases of protozoal and spirochetal origin responded to synthetic chemotherapeutic agents
• Subsequent examination by Howard Florey and Ernst Chain led to a water-soluble powder of much higher antibacterial potency and lower toxicity
• Emphasis shifted from finding new medicaments from plants to finding the active ingredients that accounted for their pharmacologic properties
• Mushrooms contain tryptamine as hallucinogens
• Stimulants and Depressants


  Used to modify the mood and mental states of psychiatric patients
• William Withering used Digitalis for the treatment of edema and currently for heart conditions
• The oldest records of the use of therapeutic plants and minerals were derived from ancient civilizations such as the Chinese, the Hindus, the Mayans, and the Mediterranean peoples of antiquity
• In ancient Greek apothecary shops, herbs such as Opium, squill, and Hyoscyamus, viper toxin, and metallic drugs like copper and zinc ores, iron sulfate, and cadmium oxide could be found
• Chaulmoogra Fruit is used for the treatment of skin conditions like psoriasis and eczema
• PSYCHOPHARMACOLOGIC AGENTS AND THE ERA OF BRAIN RESEARCH
• Prontosil® (2,4-diaminoazobenzene-4’-sulfonamide) cured dangerous systemic gram-positive bacterial infections in man and animals
• Antidepressants

  Include Tricyclic antidepressants (TCA’s) and Selective serotonin reuptake inhibitors (SSRI’s)
• Anesthetic agents


  • Inhales, intravenous, local agents
• Anxiolytics & hypnotics

  • Benzodiazepam
  • Barbiturates
• Led to a series of compounds including phenelzine (Nardil) and tranylcypromine (Parnate)
• Tricyclic Antidepressants (TCA’s)


  • Inhibit the reuptake of 5-HT & NE
  • Other examples: Nortriptyline, Desipramine, Trimipramine
• Discovery of the antidepressant effects of iproniazid
• Anti-anxiety or anxiolytic agents

  • Examples of serendipitous discovery of new drugs: Benzodiazepines(hypnotics) - (e.g. chlordiazepoxide (Librium®), diazepam (Valium®)
  • Carbamate - (e.g. meprobamate (Miltown®)
• MAO-A

  • Phenelzine, tranylcypromine
• ENDOCRINE THERAPY AND STEROIDS - Maintains homeostasis hormones are transported through the blood
• During clean-up, one had crystallized and submitted to L.O. Randall and was later reported to have hypnotic, sedative and had antistrychnine effects (similar to meprobamate)
• Amphetamine, sedatives, and hypnotics were used to stimulate or depress the mental states of patients
• Iproniazid exhibits MAO (monoamine oxidase) - inhibiting activity or also called as MAOIs
• MAO inhibitors

  • Are used as antidepressants
  • Increases NE, 5-HT, and DA
  • Depression: Lack of NE, 5-HT, and DA
• Leo Sternback synthesized 40 compounds, all of which were disappointing in pharmacologic tests
• Antidepressants

  • Tricyclic antidepressants (TCA’s)
  • Selective Serotonin Reuptake Inhibitors (SSRI’s)
  • Monoamine oxidase inhibitors (MAOI’s)
• CNS agents

  • Used to modify the mood and mental states of psychiatric patients
• Subsequently, nor
• Anxiety: ↑ catecholamines, Unpleasant emotional state consisting of apprehension and feeling of danger, without real or logical cause
• Tricyclic Antidepressants (TCA’s) are not antipsychotic, but instead elevate mood by blocking the transport inactivation of monoamine neurotransmitters including norepinephrine and serotonin
• Structural modifications were undertaken and a compound 5-10 times more potent than chlordiazepoxide was synthesized and named as diazepam (Valium®)