Description

Simple

A medication used to treat ADHD.

Clinical

A CNS stimulant and sympathomimetic agent indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD).

Overview

Amphetamine, a compound discovered over 100 years ago, 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.[Read more

Pharmacology

Indication

Amphetamine is indicated for the treatment of attention-deficit/hyperactivity disorders (ADHD) as well as for the treatment of central nervous system disorders such as narcolepsy.[ Read more

Pharmacodynamic

From its mechanism of action, it has been demonstrated that amphetamine augments the concentration of noradrenaline in the prefrontal cortex and dopamine in the striatum on a dose and time-dependent manner. The indistinct release of neurotransmitters which include adrenaline is known to produce card... Read more

Mechanism of action

It is important to consider that amphetamine has a very similar structure to the catecholamine neurotransmitters mainly on the presence of a long planar conformation, the presence of an aromatic ring and nitrogen in the aryl side chain. Amphetamine, as well as other catecholamines, is taken into pre... Read more

Absorption

Amphetamine is well absorbed in the gut and as it is a weak base hence the more basic the environment the more of the drug is found in a lipid-soluble form and the absorption through lipid-rich cell membranes is highly favored.[ Read more

Protein binding

The reported protein binding of amphetamine is relatively low and register to be of 20%.[ Read more

Volume of distribution

Amphetamine is reported to have a high volume of distribution of 4 L/kg.[ Read more

Clearance

The reported normal clearance rate is of 0.7 L.h/kg. This clearance has been shown to get significantly reduced in patients with renal impairment reaching a value of 0.4 L.h/kg.[17]

Half life

The half-life of amphetamine highly depends on the isomer. For d-amphetamine, the reported half-life is of approximately 9-11 hours while for l-amphetamine the half-life is reported to be of 11-14 hours. The urine pH can modify this pharmacokinetic parameter which can vary from 7 hours in acid urine... Read more

Route of elimination

The elimination of amphetamine is mainly via the urine from which about 40% of the excreted dose is found as unchanged amphetamine. About 90% of the administered amphetamine is eliminated 3 days after oral administration.[ Read more

Toxicity

The mean lethal serum concentration is reported to be of 6.4 mg/l. Acute amphetamine overdose can lead to hyperthermia, respiratory depression, seizures, metabolic acidosis, renal failure, hepatic injury, and coma. Some of the neurologic effects have been shown to be agitation, aggressive behavior,... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Loss of Appetite US
  • adolescent
  • Kind: experimental
    • Percent: 36%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: 35%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Loss of Appetite US
    • adult
  • Kind: experimental
    • Percent: 33%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Insomnia US
    • adult
  • Kind: experimental
    • Percent: 27%
  • Kind: placebo
    • Percent: 13%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 26%
  • Kind: placebo
    • Percent: 13%
  • Clinical Trial
    Loss of Appetite US
    • pediatric
  • Kind: experimental
    • Percent: 22%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Insomnia US
    • pediatric
  • Kind: experimental
    • Percent: 17%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Insomnia US
    • adolescent
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Abdominal Pain US
    • adolescent
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Weight Loss US
    • adult
  • Kind: experimental
    • Percent: 10%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Weight Loss US
    • adolescent
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Emotional Lability US
    • pediatric
  • Kind: experimental
    • Percent: 9%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Anxiety US
    • adult
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Agitation US
    • adult
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Vomiting US
    • pediatric
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Asthenia US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Tachycardia US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Nervousness US
    • pediatric
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Urinary Tract Infection US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Fever US
    • pediatric
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Nausea US
    • pediatric
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Dysmenorrhea US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Impotence US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Emotional Lability US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Decreased libido US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Somnolence US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Speech disorder (stuttering, excessive speech) US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Palpitation US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Twitching US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Dyspnea US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Sweating US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Somnolence US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Vomiting US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Emotional Lability US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Nausea US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Dry Mouth US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Dyspepsia US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Accidental injury US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Asthenia US
    • adolescent
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Tooth disorder (eg. teeth clenching, tooth infection) US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Constipation US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Photosensitivity US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Infection US
    • adult
  • Kind: experimental
    • Percent: 2-4%
  • Clinical Trial
    Infection US
    • pediatric
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Allergic Rhinitis US
    • pediatric
  • Kind: experimental
    • Percent: 3.8%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Upper Abdominal Pain US
    • pediatric
  • Kind: experimental
    • Percent: 3.8%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Epistaxis US
    • pediatric
  • Kind: experimental
    • Percent: 3.8%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial

    Contraindications

    • Hypersensitivity:
      • true
    • Regions: Canada
    • Regions: US
    • With Categories:
        • Name: Monoamine Oxidase Inhibitors
        • Drugbank Id: DBCAT001004
        • Mesh Id: D008996
    • Regions: US
    • Patient Conditions:
        • Name: Advanced arteriosclerosis
        • Drugbank Id: DBCOND0107486
    • Regions: US
    • Patient Conditions:
        • Name: History of drug abuse
        • Drugbank Id: DBCOND0107489
    • Regions: US
    • Patient Conditions:
        • Name: Moderate to Severe Hypertension
        • Drugbank Id: DBCOND0042937
    • Regions: US
    • Patient Conditions:
        • Name: Symptomatic cardiovascular disease
        • Drugbank Id: DBCOND0107487
        • Modification Of:
          • Base:
            • Name: Cardiovascular Disease
            • Drugbank Id: DBCOND0028376
          • Severity:
            • Includes:
              • symptomatic
    • Regions: US
    • Patient Conditions:
        • Name: Agitated state
        • Drugbank Id: DBCOND0107488
    • Regions: US
    • Patient Conditions:
        • Name: Hyperthyroidism
        • Drugbank Id: DBCOND0009048

    Food Interactions

    Take with or without food.