Chemical: Drug
amphetamine

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for amphetamine

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA
rs12364283 NC_000011.10:g.113476233A>G, NC_000011.9:g.113346955A>G, NG_008841.1:g.4047T>C, NM_000795.3:c.-1189T>C, NM_016574.3:c.-1189T>C, XM_005271425.1:c.-607T>C, XR_948023.1:n.205-380T>C, rs57156756
A > G
SNP
No VIP available CA VA
rs2281617 NC_000006.11:g.154487421C>T, NC_000006.12:g.154166286C>T, NG_021208.1:g.160786C>T, NM_001008503.2:c.1164+74814C>T, NM_001130699.1:c.1104+1634G>A, NM_001130700.1:c.1104+1634G>A, NM_015553.2:c.1101+1634G>A, XM_005266919.1:c.1104+1634G>A, XM_005266919.3:c.1104+1634G>A, XM_005266920.1:c.1104+1634G>A, XM_005266920.3:c.1104+1634G>A, XM_005266921.1:c.1104+1634G>A, XM_005266921.3:c.1104+1634G>A, XM_005266922.1:c.1104+1634G>A, XM_005266922.3:c.1104+1634G>A, XM_005266923.1:c.1101+1634G>A, XM_005266923.2:c.1101+1634G>A, XM_011535739.1:c.1104+1634G>A, XM_011535740.1:c.1104+1634G>A, XM_011535741.1:c.1104+1634G>A, XM_011535742.1:c.1101+1634G>A, XM_011535744.1:c.720+1634G>A, rs58886669
C > T
SNP
No VIP available No Clinical Annotations available VA
rs460000 NC_000005.10:g.1432710G>T, NC_000005.9:g.1432825G>T, NG_015885.1:g.17719C>A, NM_001044.4:c.419-12C>A, NT_187547.1:g.77063C>A, rs386593951, rs58561391
G > T
SNP
No VIP available CA VA
rs510769 NC_000006.11:g.154362019C>T, NC_000006.12:g.154040884C>T, NG_021208.1:g.35384C>T, NM_000914.4:c.290+1050C>T, NM_001008503.2:c.290+1050C>T, NM_001008504.3:c.290+1050C>T, NM_001008505.2:c.290+1050C>T, NM_001145279.3:c.569+1050C>T, NM_001145280.3:c.-11+29866C>T, NM_001145281.2:c.47+30325C>T, NM_001145282.2:c.290+1050C>T, NM_001145283.2:c.290+1050C>T, NM_001145284.3:c.290+1050C>T, NM_001145285.2:c.290+1050C>T, NM_001145286.2:c.290+1050C>T, NM_001285522.1:c.290+1050C>T, NM_001285523.1:c.290+1050C>T, NM_001285524.1:c.569+1050C>T, NR_104348.1:n.424+1050C>T, NR_104349.1:n.424+1050C>T, NR_104350.1:n.424+1050C>T, NR_104351.1:n.424+1050C>T, XM_005267002.1:c.476+1050C>T, XM_006715497.2:c.476+1050C>T, XM_011535849.1:c.569+1050C>T, XR_245534.1:n.476+1050C>T, XR_245535.1:n.476+1050C>T, XR_245536.1:n.476+1050C>T, XR_245537.1:n.476+1050C>T, rs17174649, rs3778144, rs386597658, rs52810976, rs61175746
C > T
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • (+/-)-Benzedrine
  • (+/-)-Desoxynorephedrine
  • (+/-)-beta-Phenylisopropylamine
  • 1-Methyl-2-phenylethylamine
  • 1-Phenyl-2-aminopropane
  • 3-Methoxy-a-methylbenzeneethanamine
  • 3-Methoxyamphetamine
  • 3-Methoxyphenylisopropylamine
  • Amfetamine
  • Amphetamine Sulfate
  • DL-alpha-Methylphenethylamine
  • Fenylo-izopropylaminyl
  • Methamphetamine HCL
  • Phenylisopropylamine
  • [1-(3-Methoxyphenyl)-2-propyl]amine
  • alpha-Methylbenzeneethaneamine
  • beta-Aminopropylbenzene
  • beta-phenyl-isopropylamine
  • dl-1-Phenyl-2-aminopropane
  • dl-Amphetamine
  • dl-Benzedrine
  • m-Methoxy-a-methylphenethylamine
  • m-Methoxyamphetamine
Trade Names
  • Actedron
  • Adipan
  • Allodene
  • Anorexide
  • Anorexine
  • Benzebar
  • Benzedrine
  • Benzolone
  • Desoxyn
  • Dexampex
  • Dexedrine
  • Dextrostat
  • Elastonon
  • Fenamin
  • Ferndex
  • Finam
  • Isoamycin
  • Isoamyne
  • Isomyn
  • Mecodrin
  • Methampex
  • Norephedrane
  • Novydrine
  • Oktedrin
  • Ortedrine
  • Paredrine
  • Percomon
  • Phenamine
  • Phenedrine
  • Profamina
  • Propisamine
  • Psychedrine
  • Raphetamine
  • Rhinalator
  • Simpatedrin
  • Simpatina
  • Sympamin
  • Sympamine
  • Sympatedrine
  • Weckamine
Brand Mixture Names
  • Adderall (amphetamine + dextroamphetamine)
  • Adderall XR 10mg (Amphetamine Aspartate + Amphetamine Sulfate + Dextroamphetamine Saccharate + Dextroamphetamine Sulfate)
  • Adderall XR 15mg (Amphetamine Aspartate + Amphetamine Sulfate + Dextroamphetamine Saccharate + Dextroamphetamine Sulfate)
  • Adderall XR 20mg (Amphetamine Aspartate + Amphetamine Sulfate + Dextroamphetamine Saccharate + Dextroamphetamine Sulfate)
  • Adderall XR 25mg (Amphetamine Aspartate + Amphetamine Sulfate + Dextroamphetamine Saccharate + Dextroamphetamine Sulfate)
  • Adderall XR 30mg (Amphetamine Aspartate + Amphetamine Sulfate + Dextroamphetamine Saccharate + Dextroamphetamine Sulfate)
  • Adderall XR 5mg (Amphetamine Aspartate + Amphetamine Sulfate + Dextroamphetamine Saccharate + Dextroamphetamine Sulfate)

PharmGKB Accession Id

PA448408

Type(s):

Drug

Description

Amphetamine is a chiral compound. The racemic mixture can be divided into its optical antipodes: levo- and dextro-amphetamine. Amphetamine is the parent compound of its own structural class, comprising a broad range of psychoactive derivatives, e.g., MDMA (Ecstasy) and the N-methylated form, methamphetamine. Amphetamine is a homologue of phenethylamine.

Source: Drug Bank

Indication

For treatment of Attention Deficit Disorder with Hyperactivity (ADDH) and narcolepsy in children.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Amphetamines stimulate the release of norepinephrine from central adrenergic receptors. At higher dosages, they cause release of dopamine from the mesocorticolimbic system and the nigrostriatal dopamine systems. Amphetamine may also act as a direct agonist on central 5-HT receptors and may inhibit monoamine oxidase (MAO). In the periphery, amphetamines are believed to cause the release of noradrenaline by acting on the adrenergic nerve terminals and alpha- and beta-receptors. Modulation of serotonergic pathways may contribute to the calming affect. The drug interacts with VMAT enzymes to enhance release of DA and 5-HT from vesicles. It may also directly cause the reversal of DAT and SERT.

Source: Drug Bank

Pharmacology

Amphetamine and dextroamphetamine, non-catechloamine sypathomimetic agents, are used in combination to treat attention-deficit hyperactivity disorder (ADHD) or narcolepsy. Adderall consists of equivalent amounts of amphetamine aspartate, amphetamine sulfate, dextroamphetamine saccharate, and dextroamphetamine sulfate.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

15-40%

Source: Drug Bank

Absorption

Amphetamine forms easily absorbed molecules that are highly lipid soluble

Source: Drug Bank

Half-Life

10 hours

Source: Drug Bank

Toxicity

LD 50=180 mg/kg(subcutaneous injection in rat). The most common presenting symptoms seen are agitation, hallucinations, suicidal behaviour, and chest pain.

Source: Drug Bank

Chemical Properties

Chemical Formula

C9H13N

Source: Drug Bank

Isomeric SMILES

CC(Cc1ccccc1)N

Source: OpenEye

Canonical SMILES

CC(N)CC1=CC=CC=C1

Source: Drug Bank

Average Molecular Weight

135.2062

Source: Drug Bank

Monoisotopic Molecular Weight

135.104799421

Source: Drug Bank

SMILES

CC(N)CC1=CC=CC=C1

Source: Drug Bank

InChI String

InChI=1S/C9H13N/c1-8(10)7-9-5-3-2-4-6-9/h2-6,8H,7,10H2,1H3

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ADRA1A (source: Drug Bank )
ADRA2A (source: Drug Bank )
CARTPT (source: Drug Bank )
SLC18A2 (source: Drug Bank )
SLC6A3 (source: Drug Bank )
TAAR1 (source: Drug Bank )

Drug Interactions

Interaction Description
chlorpromazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
chlorpromazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
fluoxetine - amphetamine Risk of serotoninergic syndrome (source: Drug Bank )
fluoxetine - amphetamine Risk of serotoninergic syndrome (source: Drug Bank )
fluphenazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
fluphenazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
guanethidine - amphetamine The agent decreases the effect of guanethidine (source: Drug Bank )
guanethidine - amphetamine Amphetamine may decrease the effect of guanethidine. (source: Drug Bank )
isocarboxazid - amphetamine Possible hypertensive crisis (source: Drug Bank )
isocarboxazid - amphetamine Possible hypertensive crisis (source: Drug Bank )
mesoridazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
mesoridazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
methotrimeprazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
perphenazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
perphenazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
phenelzine - amphetamine Possible hypertensive crisis (source: Drug Bank )
phenelzine - amphetamine Possible hypertensive crisis (source: Drug Bank )
prochlorperazine - amphetamine Decreased anorexic effect, may increase pyschotic symptoms (source: Drug Bank )
prochlorperazine - amphetamine Decreased anorexic effect, may increase pyschotic symptoms (source: Drug Bank )
promethazine - amphetamine Decreased anorexic effect, may increase pyschotic symptoms (source: Drug Bank )
promethazine - amphetamine Decreased anorexic effect, may increase pyschotic symptoms (source: Drug Bank )
propericiazine - amphetamine Decreased anorexic effect, may increase pyschotic symptoms (source: Drug Bank )
rasagiline - amphetamine Possible hypertensive crisis (source: Drug Bank )
thioridazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
thioridazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
trifluoperazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )
trifluoperazine - amphetamine Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank )

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to amphetamine: 5

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Use of magnetic resonance imaging in pharmacogenomics. British journal of clinical pharmacology. 2014. Viviani Roberto, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
OPRM1 gene variants modulate amphetamine-induced euphoria in humans. Genes, brain, and behavior. 2011. Dlugos A M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Polymorphisms in dopamine transporter (SLC6A3) are associated with stimulant effects of D-amphetamine: an exploratory pharmacogenetic study using healthy volunteers. Behavior genetics. 2010. Hamidovic Ajna, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Evaluation of genetic variability in the dopamine receptor D2 in relation to behavioral inhibition and impulsivity/sensation seeking: an exploratory study with d-amphetamine in healthy participants. Experimental and clinical psychopharmacology. 2009. Hamidovic Ajna, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00182
ChEBI:
2679
KEGG Compound:
C07514
PubChem Compound:
5826
PubChem Substance:
148619
IUPHAR Ligand:
2146
2147
Drugs Product Database (DPD):
2248813
Therapeutic Targets Database:
DAP001146

Clinical Trials

These are trials that mention amphetamine and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.