amphetamine

Absorption: Well absorbed after oral administration.

Distribution: Widely distributed in body tissues, with high concentrations in the brain and CSF.

Metabolism/Excretion: Some metabolism by the liver. Urinary excretion is pH-dependent. Alkaline urine promotes reabsorption and prolongs action.

Half-Life: 10–15 hr.

Time/Action Profile ⬆ ⬇

(CNS stimulation)

ROUTE	ONSET	PEAK	DURATION
PO	1–2 hr	unknown	4–10 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Concurrent use of or within 14 days of discontinuing MAO inhibitor therapy;
Hyperexcitable states;
Hyperthyroidism;
Patients with psychotic personalities or suicidal or homicidal tendencies;
Glaucoma;
Lactation: Lactation.

Use Cautiously in:

History of cardiovascular disease (sudden death has occurred in children with structural cardiac abnormalities or other serious heart problems);
Hypertension;
Diabetes mellitus;
Tics or family history/diagnosis of Tourette's syndrome (may worsen condition);
Continual use (may result in psychological or physical dependence);
Seizure disorders (may lower seizure threshold);
OB: Use during pregnancy only if maternal benefit outweighs potential fetal risk; use may lead to premature delivery, low birth weight infants, and withdrawal symptoms in newborns;
Pedi: Growth suppression may occur in children with long-term use;
Geri: Initiate with lower dose in older adults due to age-related decline in organ function.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, palpitations, tachycardia, cardiomyopathy (↑ with prolonged use, high doses), hypotension, peripheral vasculopathy, SUDDEN DEATH

Derm: urticaria

Endo: growth inhibition (with long term use in children)

GI: anorexia, constipation, diarrhea, cramps, dry mouth, intestinal ischemia, metallic taste, nausea, vomiting

GU: erectile dysfunction, ↑libido

Neuro: hyperactivity, insomnia, restlessness, tremor, dizziness, headache, irritability, tics, Tourette's syndrome

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA), physical dependence, psychological dependence, tolerance

Interactions ⬆ ⬇

Drug-drug:

Use with MAO inhibitors or vasopressors may result in hypertensive crisis; concurrent use or use within 14 days of MAO inhibitors contraindicated.
Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, MAO inhibitors, SSRIs, SNRIs, fentanyl, buspirone, lithium, tramadol, and triptans, ↑ risk of serotonin syndrome.
↑adrenergic effects with other adrenergics or thyroid preparations.
Drugs that alkalinize urine, including sodium bicarbonate or acetazolamide, may ↓ excretion and ↑ effects.
Drugs that acidify urine, including large doses of ascorbic acid, may ↓ effects.
↑risk of hypertension and bradycardia with beta blockers.
↑risk of arrhythmias with digoxin.
Tricyclic antidepressants may ↑ effect of amphetamine and may ↑ risk of arrhythmias, hypertension, or hyperpyrexia.

Drug-Natural Products:

St. John's wort may ↑ risk of serotonin syndrome.

Foods that alkalinize the urine (e.g., cranberry juice) can ↑ effects.

Route/Dosage ⬆ ⬇

Attention-Deficit/Hyperactivity Disorder

PO (Adults ): Adzenys XR-ODT: 12.5 mg once daily; Dyanavel XR: 2.5–5 mg once daily in AM; may ↑ by 2.5–10 mg/day every 4–7 days (max dose = 20 mg/day).
PO (Children ≥6 yr): Adzenys XR-ODT: 6.3 mg once daily in AM; may ↑ by 3.1 mg/day or 6.3 mg/day at weekly intervals (max dose = 18.8 mg/day for age 6–12 yr; 12.5 mg for age 12–17 yr); Dyanavel XR: 2.5–5 mg once daily in AM; may ↑ by 2.5–10 mg/day every 4–7 days (max dose = 20 mg/day); Evekeo: 5 mg 1–2 times daily; may ↑ by 2.5–5 mg/day at weekly intervals until optimal response obtained (max dose = 40 mg/day).
PO (Children 3–5 yr): Evekeo: 2.5 mg once daily; may ↑ by 2.5 mg/day at weekly intervals until optimal response obtained (max dose = 40 mg/day).

Narcolepsy

PO (Adults and Children ≥12 yr): Evekeo: 10 mg once daily; ↑ by 10 mg/day at weekly intervals (usual dose = 5–60 mg in divided doses).
PO (Children 6–12 yr): Evekeo: 5 mg once daily; may ↑ by 5 mg/day at weekly intervals (usual dose = 5–60 mg in divided doses).

Obesity

PO (Adults and Children ≥12 yr): Evekeo: Up to 30 mg/day in divided doses (5–10 mg per dose given 30–60 min before a meal).

Availability ⬆ ⬇

(Generic available)

Immediate-release tablets (Evekeo): 5 mg; 10 mg
Extended-release tablets (Dyanavel XR): 5 mg; 10 mg; 15 mg; 20 mg
Extended-release orally disintegrating tablets (Adzenys XR-ODT): 3.1 mg; 6.3 mg; 9.4 mg; 12.5 mg; 15.7 mg; 18.8 mg
Extended-release oral suspension (Dyanavel XR) bubble gum flavor: 2.5 mg/mL

Assessment ⬆ ⬇

Assess for presence and family history of cardiac disease (sudden death, ventricular arrhythmia), tics, or Tourette's syndrome prior to starting therapy.
Monitor BP, pulse, and respiration before and periodically during therapy.
May produce a false sense of euphoria and well-being. Provide frequent rest periods and observe patient for rebound depression after the effects of the medication have worn off.
Assess for risk of abuse prior to starting therapy. Monitor during therapy. Has high dependence and abuse potential. Tolerance to medication occurs rapidly; do not increase dose.
Assess for serotonin syndrome (mental changes [agitation, hallucinations, coma], autonomic instability [tachycardia, labile BP, hyperthermia], neuromuscular aberrations [hyperreflexia, incoordination], and/or GI symptoms [nausea, vomiting, diarrhea]), especially in patients taking other serotonergic drugs (SSRIs, SNRIs).
ADHD: Monitor weight biweekly for significant loss. Monitor height periodically in children; inform health care professional of growth inhibition.
Assess attention span, impulse control, motor and vocal tics, and interactions with others in children with ADHD.
Narcolepsy: Observe and document frequency of narcoleptic episodes.
May produce a false sense of euphoria and well-being. Provide frequent rest periods and observe patient for rebound depression after the effects of the medication have worn off.
Has high dependence and abuse potential. Tolerance to medication occurs rapidly; do not increase dose.

Lab Test Considerations:

Implementation ⬆ ⬇

To switch from Adderall XR to Adzenys XR-ODT, use following equivalencies: Adderall XR 5 mg = Adzenys XR-ODT 3.1 mg; 10 mg = 6.3 mg; 15 mg = 9.4 mg; 20 mg = 12.5 mg; 25 mg = 15.7 mg; 30 mg = 18.8 mg respectively. To switch from other amphetamine products, discontinue therapy and titrate Adzenys XR-ODTusing titration schedule under Route/Dosage. Do not substitute on an mg/mg basis.
PO: Administer in the morning. May be taken without regard to food. Individualize dose to therapeutic needs and response of patient. Use the lowest effective dose. Keep tablet in blister pack until administration. Use dry hands to open blister. Do not push tablet through foil. Remove tablet and place on tongue; allow to disintegrate without chewing or crushing.
- Shake solution well before administering. Use calibrated measuring device for accurate dose.
- Orally disintegrating tablets should be left in the package until use. Remove from the blister pouch. Remove tablet by pushing it through back of foil-lined blister pack. Place tablet on tongue. Tablet will dissolve rapidly and be swallowed with saliva. No liquid is needed to take orally disintegrating tablet; may move tablet around mouth until it disintegrates. DNC: Do not crush or chew orally disintegrating tablets.
ADHD: When symptoms are controlled, dose reduction or interruption of therapy may be possible during summer mo or may be given on each of the 5 school days, with medication-free weekends and holidays.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication once in the morning as directed. Do not double doses. Instruct patient not to alter dose without consulting health care professional. Abrupt cessation of high doses may cause extreme fatigue and mental depression. Advise patient to read the Medication Guide before starting medication and with each Rx refill in case of changes.
Inform patient that the effects of drug-induced dry mouth can be minimized by rinsing frequently with water or chewing sugarless gum or candies.
Advise patient to limit caffeine intake.
May impair judgment. Advise patient to use caution when driving or during other activities requiring alertness until response to medication is known.
Advise patient/parent to notify health care professional promptly if signs and symptoms of heart problems (chest pain, shortness of breath, fainting), mental problems (new or worsening behaviors, thoughts, or mental symptoms; hearing voices; believing things that are not true; being suspicious; new manic symptoms), serotonin syndrome, or circulation problems in fingers and toes (numb, cool, painful, change from pale to blue or red, unexplained wounds on fingers or toes) occur.
Advise patient that amphetamine is a drug with known abuse potential. Store in safe place, protect it from theft, and never give to anyone other than the individual for whom it was prescribed.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort.
Inform patient that periodic holidays from the drug may be used to assess progress and decrease dependence.
Advise patient to notify health care professional if nervousness, restlessness, insomnia, dizziness, anorexia, or dry mouth becomes severe.
Rep: May cause fetal harm. Advise female patient to notify health care professional if pregnancy is planned or suspected or and to avoid breastfeeding during therapy. May increase risk or premature birth and low birth weight. Monitor infants born to mothers taking amphetamines for symptoms of withdrawal (feeding difficulties, irritability, agitation, excessive drowsiness). Encourage patients exposed to amphetamines during pregnancy to join the registry. Health care professionals may call the National Pregnancy Registry for Psychiatric Medications at 1-866-961-2388 or online at https://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/othermedications/ to register patients.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇