Peringatan Keamanan

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, irritability, headache, and hallucinations. In the cardiovascular site, there have been reports of arrhythmia, cardiomyopathy, myocardial infarction or ischemic stroke. Lastly, in the GI tract, there are reports if abdominal pain, vomiting, diarrhea, cramps, anorexia and GI hemorrhage. A dose of 1-2 g of amphetamine is known to cause severe intoxication but some chronic abusers can report usage of even 5-15 g per day.L5212

In animal studies, there is no evidence of carcinogenic potential, not clastogenic or to affect fertility or early embryonic development.FDA label

Amphetamine

DB00182

small molecule approved illicit investigational

Deskripsi

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.A18540 The first product of Smith, Kline and French was approved by the FDA on 1976.L5194

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.A18540

Struktur Molekul 2D

Berat 135.2062
Wujud liquid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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 to 34 hours for alkaline urine.[A174292]
Volume Distribusi Amphetamine is reported to have a high volume of distribution of 4 L/kg.[A174292]
Klirens (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.[F3244]

Absorpsi

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.A174292 The peak response of amphetamine occurs 1-3 hours after oral administration and approximately 15 minutes after injection and it presents a bioavailability of over 75%.L5206 Complete amphetamine absorption is usually done after 4-6 hours.L5209

Metabolisme

Amphetamine is known to be metabolized by the liver under the action of the CYP2D6. The metabolic pathway of amphetamine is mainly defined by aromatic hydroxylation, aliphatic hydroxylation, and n-dealkylation.L5212 The formed metabolites in this pathway are 4-hydroxyamphetamine, 4-hydroxynorephedrine, hippuric acid, benzoic acid, benzyl methyl ketone, and p-hydroxyamphetamine which is known to be a potent hallucinogen.L5206 However, a significant part of the original compound remains unchanged.A174292

Rute Eliminasi

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.A174292 The rate of elimination of amphetamine highly depends on the urine pH in which acidic pH will produce a higher excretion of amphetamine and basic pH produces a lower excretion.L5206

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1675 Data
Valsartan Amphetamine may decrease the antihypertensive activities of Valsartan.
Ramipril Amphetamine may decrease the antihypertensive activities of Ramipril.
Remikiren Amphetamine may decrease the antihypertensive activities of Remikiren.
Bethanidine Amphetamine may decrease the antihypertensive activities of Bethanidine.
Isradipine Amphetamine may decrease the antihypertensive activities of Isradipine.
Olmesartan Amphetamine may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Amphetamine may decrease the antihypertensive activities of Nitroprusside.
Diltiazem Amphetamine may decrease the antihypertensive activities of Diltiazem.
Minoxidil Amphetamine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Amphetamine may decrease the antihypertensive activities of Treprostinil.
Amlodipine Amphetamine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Amphetamine may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Amphetamine may decrease the antihypertensive activities of Nisoldipine.
Fosinopril Amphetamine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Amphetamine may decrease the antihypertensive activities of Trandolapril.
Benazepril Amphetamine may decrease the antihypertensive activities of Benazepril.
Bosentan Amphetamine may decrease the antihypertensive activities of Bosentan.
Enalapril Amphetamine may decrease the antihypertensive activities of Enalapril.
Candoxatril Amphetamine may decrease the antihypertensive activities of Candoxatril.
Guanabenz Amphetamine may decrease the antihypertensive activities of Guanabenz.
Mecamylamine Amphetamine may decrease the antihypertensive activities of Mecamylamine.
Losartan Amphetamine may decrease the antihypertensive activities of Losartan.
Moexipril Amphetamine may decrease the antihypertensive activities of Moexipril.
Lisinopril Amphetamine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Amphetamine may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Amphetamine may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Amphetamine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Amphetamine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Amphetamine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Amphetamine may decrease the antihypertensive activities of Fenoldopam.
Tadalafil Amphetamine may decrease the antihypertensive activities of Tadalafil.
Eprosartan Amphetamine may decrease the antihypertensive activities of Eprosartan.
Quinapril Amphetamine may decrease the antihypertensive activities of Quinapril.
Omapatrilat Amphetamine may decrease the antihypertensive activities of Omapatrilat.
Telmisartan Amphetamine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Amphetamine may decrease the antihypertensive activities of Methyldopa.
Guanfacine Amphetamine may decrease the antihypertensive activities of Guanfacine.
Irbesartan Amphetamine may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Amphetamine may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Amphetamine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Amphetamine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Amphetamine may decrease the antihypertensive activities of Trimethaphan.
Rescinnamine Amphetamine may decrease the antihypertensive activities of Rescinnamine.
Captopril Amphetamine may decrease the antihypertensive activities of Captopril.
Epoprostenol Amphetamine may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Amphetamine may decrease the antihypertensive activities of Hydralazine.
Cilazapril Amphetamine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Amphetamine may decrease the antihypertensive activities of Saprisartan.
Spirapril Amphetamine may decrease the antihypertensive activities of Spirapril.
Debrisoquine Amphetamine may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Amphetamine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Amphetamine may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Amphetamine may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Amphetamine may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Amphetamine may decrease the antihypertensive activities of Pinacidil.
Temocapril Amphetamine may decrease the antihypertensive activities of Temocapril.
Riociguat Amphetamine may decrease the antihypertensive activities of Riociguat.
Macitentan Amphetamine may decrease the antihypertensive activities of Macitentan.
Hexamethonium Amphetamine may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Amphetamine may decrease the antihypertensive activities of Aliskiren.
Nicorandil Amphetamine may decrease the antihypertensive activities of Nicorandil.
Lacidipine Amphetamine may decrease the antihypertensive activities of Lacidipine.
Levamlodipine Amphetamine may decrease the antihypertensive activities of Levamlodipine.
Moxonidine Amphetamine may decrease the antihypertensive activities of Moxonidine.
Rauwolfia serpentina root Amphetamine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Amphetamine may decrease the antihypertensive activities of Enalaprilat.
Selexipag Amphetamine may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Amphetamine may decrease the antihypertensive activities of Angiotensin 1-7.
Rilmenidine Amphetamine may decrease the antihypertensive activities of Rilmenidine.
Imidapril Amphetamine may decrease the antihypertensive activities of Imidapril.
BQ-123 Amphetamine may decrease the antihypertensive activities of BQ-123.
Dihydralazine Amphetamine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Amphetamine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Amphetamine may decrease the antihypertensive activities of Guanoxan.
Delapril Amphetamine may decrease the antihypertensive activities of Delapril.
Vincamine Amphetamine may decrease the antihypertensive activities of Vincamine.
Linsidomine Amphetamine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Amphetamine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Amphetamine may decrease the antihypertensive activities of Tolonidine.
Endralazine Amphetamine may decrease the antihypertensive activities of Endralazine.
Cadralazine Amphetamine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Amphetamine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Amphetamine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Amphetamine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Amphetamine may decrease the antihypertensive activities of Guanoclor.
Candesartan Amphetamine may decrease the antihypertensive activities of Candesartan.
Dexniguldipine Amphetamine may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Amphetamine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Amphetamine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Amphetamine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Amphetamine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Amphetamine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Amphetamine may decrease the antihypertensive activities of Quinaprilat.
Lercanidipine Amphetamine may decrease the antihypertensive activities of Lercanidipine.
Azilsartan medoxomil Amphetamine may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Amphetamine may decrease the antihypertensive activities of Diazoxide.
Atomoxetine The risk or severity of hypertension can be increased when Atomoxetine is combined with Amphetamine.
Ethosuximide Amphetamine can cause a decrease in the absorption of Ethosuximide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ioflupane I-123 Amphetamine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Amphetamine.

Target Protein

Synaptic vesicular amine transporter SLC18A2
Sodium-dependent dopamine transporter SLC6A3
Cocaine- and amphetamine-regulated transcript protein CARTPT
Trace amine-associated receptor 1 TAAR1
Monoamine oxidase MAOA
Sodium-dependent noradrenaline transporter SLC6A2
Alpha adrenergic receptor ADRA1A
Beta adrenergic receptor ADRB1
D(2) dopamine receptor DRD2
Amine oxidase [flavin-containing] B MAOB
Sodium-dependent serotonin transporter SLC6A4

Referensi & Sumber

Synthesis reference: Guohong Wang, "Composition and methods for synthesis of novel tracers for detecting amphetamine and methamphetamine in samples." U.S. Patent US20020090661, issued July 11, 2002.
Artikel (PubMed)
  • PMID: 23539642
    Heal DJ, Smith SL, Gosden J, Nutt DJ: Amphetamine, past and present--a pharmacological and clinical perspective. J Psychopharmacol. 2013 Jun;27(6):479-96. doi: 10.1177/0269881113482532. Epub 2013 Mar 28.
  • PMID: 20780662
    Guttmann E, Sargant W: Observations on Benzedrine. Br Med J. 1937 May 15;1(3984):1013-5.
  • PMID: 4564954
    Arnold LE, Wender PH, McCloskey K, Snyder SH: Levoamphetamine and dextroamphetamine: comparative efficacy in the hyperkinetic syndrome. Assessment by target symptoms. Arch Gen Psychiatry. 1972 Dec;27(6):816-22.
  • PMID: 19199083
    Robertson SD, Matthies HJ, Galli A: A closer look at amphetamine-induced reverse transport and trafficking of the dopamine and norepinephrine transporters. Mol Neurobiol. 2009 Apr;39(2):73-80. doi: 10.1007/s12035-009-8053-4. Epub 2009 Feb 6.
  • PMID: 17020775
    Easton N, Steward C, Marshall F, Fone K, Marsden C: Effects of amphetamine isomers, methylphenidate and atomoxetine on synaptosomal and synaptic vesicle accumulation and release of dopamine and noradrenaline in vitro in the rat brain. Neuropharmacology. 2007 Feb;52(2):405-14. doi: 10.1016/j.neuropharm.2006.07.035. Epub 2006 Oct 3.
  • PMID: 10767057
    Baumann MH, Ayestas MA, Dersch CM, Brockington A, Rice KC, Rothman RB: Effects of phentermine and fenfluramine on extracellular dopamine and serotonin in rat nucleus accumbens: therapeutic implications. Synapse. 2000 May;36(2):102-13. doi: 10.1002/(SICI)1098-2396(200005)36:2<102::AID-SYN3>3.0.CO;2-#.
  • PMID: 20997404
    BETT WR: Benzedrine sulphate in clinical medicine; a survey of the literature. Postgrad Med J. 1946 Aug;22:205-18.
  • PMID: 24725022
    Tarver J, Daley D, Sayal K: Attention-deficit hyperactivity disorder (ADHD): an updated review of the essential facts. Child Care Health Dev. 2014 Nov;40(6):762-74. doi: 10.1111/cch.12139. Epub 2014 Apr 14.
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