amphetamine.pptx
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Amphetamine, is a compound discovered over 100 years ago and is one of the more restricted controlled drugs. It was previously used for a large variety of conditions and this changed until this point where its use is highly restricted. Amphetamine, with the chemical formula alpha-methylphenethylamine, was discovered in 1910 and first synthesized by 1927. After being proven to reduce drug-induced anesthesia and produce arousal and insomnia, amphetamine racemic mix was registered by Smith, Kline and French in 1935. Amphetamine structure presents one chiral center and it exists in the form of dextro- and levo-isomers.1 The first product of Smith, Kline and French was approved by the FDA on 1976.12 During World War II, amphetamine was used to promote wakefulness in the soldiers. This use derived into a large overproduction of amphetamine and all the surplus after the war finalized ended up in the black market, producing the initiation of the illicit abuse.1
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- 1. AMPHETAMINE PRESENTED BY : Dr. RAJIV RANJAN DAS GUIDE : Dr. (PROF AND HOD ) U.S.P. KESHARI
- 2. The following are the LEARNING OBJECTIVES of our class : • To know about the drug Amphetamine under following headings: • Introduction • History • Pharmacokinetics • Mechanism of action • Uses • Abuse
- 3. INTRODUCTION and HISTORY • It was discovered in 1887 by German Pharmacologist L. Edeleano • There are two enantiomers : levoamphetamine and dextroamphetamine • Historically it was used as nasal decongestion and depression • The first amphetamine pharmaceutical was Benzedrine inhalors • It was widely abused 1971 for their stimulant action • Widely used in WORLD WAR II to counteract fatigue • Amphetamine increases monoamine and excitatory neurotransmission in the brain (stimulant drug) • At therapeutics doses, amphetamine causes emotional and cognitive effects such as euphoria, change in desire of sex, increased wakefullness, and improved cognitive control • EPHEDRA is the primary component used to synthesize amphetamine
- 6. PHARMACOKINETICS Bioavailability : oral 75-100% Protein binding : 20% Metabolism : CYP2D6, DBH, FMO3 Onset of action : 30-60mins Elimination t1/2: 9-11 hrs Duration of action : 3-6hrs Excretion: Renal (PH dependent )
- 8. HIGH DOSE ABUSERS • Leading to extended mental and physical hyperactivity • Continued abuse(high doses) often leads to : Seizures Kidney damage Stroke Liver damage Oral damage Skin lesions Considerable weight loss Hypertensive disorders
- 9. Summary of Effects of Amphetamines Body • Increased heartbeat • Increased BP • Decreased appetite • Increased breathing rate • Inability to sleep • Sweating • Convulsions • Chest pain • Irregular heartbeat due to overdose Mind • Decreased fatigue • Increased confidence • Increase feeling of alertness • Restlessness • Increased irritability • Fearfulness • Distrust of people • hallucination Low dose High dose Harrison,20th ed