Amphetamine Group Members: Kwong Ka Yi Mak Cheuk Kin
Lead Compound Discovery First synthesized in 1887 By Lazar Edelearnu But have no pharmacological use Resynthesized in 1927 By Gordon Alles Used as a decongestant
Molecular modification Ephedrine (2-methylamino-1-phenylpropan-1-ol) Amphetamine (1-phenylpropan-2-amine)
Ephedrine Amphetamine
Formulation Development Psychostimulant Increased wakefulness Decreased fatigue Examples of popular brands Containing amphetamine as active ingredient Adderall Vyvanse Dexedrine
Adderall Developed by Shire Pharmaceutical in 1996 Available in 2 formulations: Immediate release Extended release Formulations modified Strong effect on absorption & excretion of the racemic DL-amphetamine IIncreased reabsorption dangerously high amphetamine serum level
At molecular level A mixture of amphetamine salts Racemic amphetamine aspartate monohydrate Dextroamphetamine saccharide Detroamphtetamine sulphate Racemic amphetamine sulphate Active ingredients Dextroamphetamine Racemic DL-amphetamine
Vyvanse Developed by New River Pharmaceutical in 2005 Available formulations Pills of several dosages Formulation modified Single-enantiomer amphetamine Reduce side effect
At molecular level Active ingredients: Lisdexamphetamine Dextroamphetamine Amphetamine dextroamphetamine lisdexamphetamine
Dissociate ions Covalent amide bond hydrolysis Lisdexamphetamine Dextroamphetamine
Dexedrine Formulations available Tablet Sustained-release capsules Formulation modified Exhibit better preventive effect on the neurotransmitters more obvious fatigue reduction
At molecular level Amphetamine Dextroamphetamine DDextroamphetamine = enantiomer of amphetamine
Safety tests & Human Trials
Adderall Test Duration : 2 years Treatment : ADHD Result : Adderall XR – better tolerability Significant long-term ADHD sympton control
Vyvanse Test Duration : 1 year Treatment : ADHD Result : Fairly good tolerability Side effects frequently reported Decreased appetite Headache Decreased weight Insomnia
Dexedrine Treatment : ADHD Narcolepsy Depression Psychiatric syndrome
Result : Improve attention span & behaviour Reduce fatigue in some patients
Approval for Marketing
Adderall Potential addictive property Powerful ability to raise blood pressure Approved for the treatment of ADHD ONLY
Vyvanse DateApproval 23th February 2007 U.S. Food and Drug Administration (FDA) 3rd January 2008 U.S. Food and Drug Administration (FDA) 19th February 2009Health Canada
Dexedrine ADHD Narcolepsy Depression Weight Loss