Amphetamine
- Atc Codes:N06BA01
- CAS Codes:60-13-9#300-62-9
- PHARMGKB ID:60-13-9#300-62-9
Table of contents
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Pharmacokinetics and Pharmacodynamics
Brand Names
Drug combinations
Amphetamine and Dextroamphetamine
Chemistry
Amphetamine sulfate: (C~9~H~13~N)~2~ H~2~SO~4~. Mw: 368.49. (1) Benzeneethanamine, α-methyl-, sulfate (2:1), (±)-; (2)(±)-α-Methylphenethylamine sulfate (2:1). CAS-60-13-9. CAS-300-62-9.
Pharmacologic Category
Anorexigenic Agents and Respiratory and Cerebral Stimulants; Amphetamines. (ATC-Code: N06BA01).
Mechanism of action
Mechanism of action on peripheral structures is thought to be a combination of release of norepinephrine from stores in adrenergic nerve terminals and direct action on both α- and β- receptor sites. Mechanism of action involved in the central effect has not been determined. The main sites of CNS action appear to be the cerebral cortex and possibly the reticular-activating system. Stimulation by an amphetamine causes an increase in motor activity, mental alertness, diminished sense of fatigue, brighter spirits, and mild euphoria.
Therapeutic use
Used as an adjunct to psychological, educational, social, and other remedial measures in the treatment of attention-deficit hyperactivity disorder (hyperkinetic disorder, hyperkinetic syndrome of childhood, minimal brain dysfunction). Used as a stimulant to reduce daytime sleepiness in the management of narcolepsy.
Pregnancy and lactiation implications
Risk of prematurity, low birthweight, and withdrawal symptoms (e.g. dysphoria, lassitude, agitation) in infants born to dependent women. Distributed into milk.
Unlabeled use
Contraindications
Contraindicated in hypersensitivity or idiosyncrasy to sympathomimetic amines. Symptomatic cardiovascular disease. Hyperthyroidism. Moderate to severe hypertension. Glaucoma. Advanced arteriosclerosis. Within 14 days of MAO inhibitor therapy. In agitated patients.
Warnings and precautions
In general, use of CNS stimulants should be avoided in known serious structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, CAD, or other serious cardiac conditions. Possible modest increases in average blood pressure and heart rate. Larger increases may occur. May exacerbate symptoms of behavior disturbance and thought disorder in pre-existing psychotic disorder. Psychotic symptoms (e.g. hallucinations, delusional thinking) may occur with usual dosages in children and adolescents without prior history of psychotic illness. May precipitate mixed or manic episodes in ADHD patients with comorbid bipolar disorder. Aggressive behavior and hostility (frequently observed in children and adolescents with ADHD) reported in patients receiving drug therapy for ADHD. Long-term (i.e. >14 months) administration expected to cause at least a temporary suppression of normal weight and/or height patterns in some children and adolescents. Possible lowering of seizure threshold in patients with history of seizures, in those with prior EEG abnormalities but no history of seizures, and, very rarely, in those without history of seizures and with no prior evidence of EEG abnormalities. Visual disturbances (difficulty with accommodation, blurred vision) reported with stimulants. Amphetamines reported to exacerbate motor and phonic tics and Tourette’s syndrome. Several controlled studies have not found stimulants to worsen or precipitate tics or Tourette’s syndrome. Not recommended for ADHD in children <3 years of age. Aggressive behavior, hostility, and psychotic (e.g. hallucinations, delusional thinking) or manic symptoms reported in children and adolescents receiving stimulants for management of ADHD. Sudden death reported in children and adolescents with structural cardiac abnormalities or other serious cardiac conditions receiving usual dosages of stimulants. Possible inhibition of drug elimination in hepatic and renal impairment, resulting in prolonged exposure. Isolated reports of cardiomyopathy associated with chronic amphetamine use.