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 |
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Loss of Appetite | US |
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Clinical Trial |
Dry Mouth | US |
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Clinical Trial |
Loss of Appetite | US |
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Clinical Trial |
Insomnia | US |
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Clinical Trial |
Headache | US |
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Loss of Appetite | US |
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Insomnia | US |
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Insomnia | US |
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Abdominal Pain | US |
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Weight Loss | US |
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Weight Loss | US |
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Emotional Lability | US |
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Nausea | US |
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Anxiety | US |
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Agitation | US |
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Dizziness | US |
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Vomiting | US |
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Asthenia | US |
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Tachycardia | US |
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Diarrhea | US |
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Nervousness | US |
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Urinary Tract Infection | US |
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Clinical Trial |
Fever | US |
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Clinical Trial |
Nausea | US |
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Dysmenorrhea | US |
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Impotence | US |
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Emotional Lability | US |
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Decreased libido | US |
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Somnolence | US |
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Speech disorder (stuttering, excessive speech) | US |
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Palpitation | US |
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Twitching | US |
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Dyspnea | US |
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Sweating | US |
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Somnolence | US |
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Vomiting | US |
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Clinical Trial |
Emotional Lability | US |
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Clinical Trial |
Nausea | US |
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Clinical Trial |
Dry Mouth | US |
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Clinical Trial |
Dyspepsia | US |
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Accidental injury | US |
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Asthenia | US |
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Tooth disorder (eg. teeth clenching, tooth infection) | US |
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Constipation | US |
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Photosensitivity | US |
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Infection | US |
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Infection | US |
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Allergic Rhinitis | US |
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Upper Abdominal Pain | US |
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Epistaxis | US |
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Contraindications
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Food Interactions
Take with or without food.