dextroamphetamine

Contraindicated in:

Hypersensitivity (some products contain tartrazine);
Concurrent use or use within 14 days of MAO inhibitors or MAO-like drugs (linezolid or methylene blue);
Hyperexcitable states, including hyperthyroidism;
Psychotic personalities;
Suicidal or homicidal tendencies;
Glaucoma;
Lactation: Lactation.

Use Cautiously in:

Structural cardiac abnormalities, HF, cardiac arrhythmias, or coronary artery disease (sudden death has occurred in children with structural cardiac abnormalities or other serious heart problems);
Hypertension;
Diabetes mellitus;
History of substance abuse;
Tourette's syndrome or tics (may worsen conditions);
Continual use (may produce psychological dependence or physical addiction);
OB: Use during pregnancy only if potential maternal benefit outweighs potential fetal risk;
Pedi: Growth suppression may occur in children with long-term use; children <6 yr (↑ risk of adverse reactions, particularly weight loss in children 4–<6 yr; safety of transdermal product not established).

Adv. Reactions/Side Effects ⬆ ⬇

CV: palpitations, tachycardia, arrhythmias, hypertension, MI, peripheral vasculopathy, SUDDEN DEATH

Derm: allergic contact dermatitis (transdermal), alopecia, erythema (transdermal), pruritus (transdermal), STEVENS-JOHNSON SYNDROME, urticaria

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

GU: ↓libido, erectile dysfunction, priapism

MS: RHABDOMYOLYSIS

Neuro: hyperactivity, insomnia, restlessness, tremor, behavioral disturbances, depression, dizziness, hallucinations, headache, irritability, mania, paresthesia, STROKE, thought disorder, tics, Tourette's syndrome

Misc: hypersensitivity reactions (including anaphylaxis and angioedema), physical dependence, psychological dependence

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with MAO inhibitors or MAO-inhibitor-like drugs, such as linezolid or methylene blue, may result in serious, potentially fatal reactions; wait at least 14 days following discontinuation of MAO inhibitor before initiation of amphetamine mixtures.
↑adrenergic effects with other adrenergics.
Drugs that affect serotonergic neurotransmitter systems, including MAO inhibitors, tricyclic antidepressants, SSRIs, SNRIs, fentanyl, buspirone, tramadol, lithium, and triptans, ↑ risk of serotonin syndrome.
Alkalinizing the urine (sodium bicarbonate, acetazolamide) prolongs effect.
Acidification of urine (large doses of ascorbic acid) ↓ effect.
Phenothiazines may ↓ effect of dextroamphetamine.
May antagonize the response to antihypertensives.
↑risk of cardiovascular side effects with beta blockers or tricyclic antidepressants.

Drug-Natural Products:

St. John's wort may ↑ serious side effects; concurrent use is not recommended.
Use with caffeine-containing herbs (guarana, tea, coffee) ↑ stimulant effect.

Availability ⬆ ⬇

(Generic available)

Immediate-release tablets (Zenzedi): 2.5 mg; 5 mg; 7.5 mg; 10 mg; 15 mg; 20 mg; 30 mg
Extended-release capsules (Dexedrine): 5 mg; 10 mg; 15 mg
Oral solution (Procentra)bubblegum flavor: 1 mg/mL
Transdermal patch (Xelstrym): 4.5 mg/9 hr; 9 mg/9 hr; 13.5 mg/9 hr; 18 mg/9 hr

Route/Dosage ⬆ ⬇

Attention-Deficit Hyperactivity Disorder

PO (Adults ): 5–40 mg/day in divided doses. Sustained-release capsules should not be used as initial therapy.
PO (Children ≥6 yr): 5 mg 1–2 times daily; ↑ by 5 mg daily at weekly intervals (maximum: 40 mg/day). Sustained-release capsules should not be used as initial therapy.
Transdermal (Adults ): Apply one 9-mg patch initially (should be applied 2 hr before desired effect and removed within 9 hr after application); may be titrated based on response and tolerability; may ↑ to 18-mg patch after 1 wk.
Transdermal (Children ≥6 yr): Apply one 4.5-mg patch initially (should be applied 2 hr before desired effect and removed within 9 hr after application); may be titrated based on response and tolerability; may ↑ to 9-mg patch after 1 wk, and then to 13.5-mg patch after another wk, and then to 18-mg patch after another wk.

Renal Impairment

(Adults and Children ≥6 yr): Severe renal impairment (CCr 15–30 mL/min): Not to exceed patch dose of 13.5 mg/9 hr. End-stage renal disease (CCr <15 mL/min): Not to exceed patch dose of 9 mg/9 hr.

Narcolepsy

PO (Adults ): 5–60 mg/day single dose or in divided doses. Sustained-release capsules should not be used as initial therapy.
PO (Children ≥12 yr): 10 mg/day, ↑ by 10 mg/day at weekly intervals until response is obtained or 60 mg is reached.
PO (Children 6–12 yr): 5 mg/day, ↑ by 5 mg/day at weekly intervals until response is obtained or 60 mg is reached.

US Brand Names ⬆ ⬇

Dexedrine, Procentra, Xelstrym, Zenzedi

Action ⬆ ⬇

Produces CNS stimulation by releasing norepinephrine from nerve endings. Pharmacologic effects:
- CNS and respiratory stimulation,
- vasoconstriction,
- mydriasis (pupillary dilation),
- Contraction of the urinary bladder sphincter.

Therapeutic effects:

Increased attention span in ADHD.
Increased motor activity and mental alertness and decreased fatigue in narcoleptic patients.

Classifications ⬆ ⬇

Therapeutic Classification: central nervous system stimulants

Pharmacologic Classification: amphetamines

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration. 90% absorbed following transdermal administration.

Distribution: Widely distributed; high concentrations in brain and CSF.

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

Half-Life: PO: 10–12 hr (6.8 hr in children); Transdermal: 6–12 hr.

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

(CNS stimulation)

ROUTE	ONSET	PEAK	DURATION
PO	1–2 hr	3 hr	2–10 hr
PO-ER	unknown	unknown	up to 24 hr
TD	1–2 hr	3 hr	9–12 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication at least 6 hr before bedtime to avoid sleep disturbances. Take missed doses as soon as remembered up to 6 hr before bedtime. Do not double doses. Advise patient and parents to read the Medication Guide prior to starting therapy and with each Rx refill. Instruct patient not to alter dose without consulting health care professional. Abrupt cessation of high doses may cause extreme fatigue and mental depression.
- Inform patient that sharing this medication may be dangerous. Educate patients about abuse potential and how to monitor for signs of abuse and overdose. Advise patient or parents to keep dextroamphetamine in a safe place to prevent misuse or abuse.
- Inform patients starting therapy of risk of peripheral vasculopathy. Instruct patients to notify health care professional of any new numbness; pain; skin color change from pale, to blue, to red; or coolness or sensitivity to temperature in fingers or toes, and call if unexplained wounds appear on fingers or toes. May require rheumatology consultation.
- Inform patient that the effects of drug-induced dry mouth can be minimized by rinsing frequently with water or chewing sugarless gum or candies.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort. Advise patient to avoid the intake of large amounts of caffeine.
- Medication may impair judgment. Advise patients to use caution when driving or during other activities requiring alertness.
- Advise patient to notify health care professional if nervousness, restlessness, insomnia, dizziness, anorexia, or dry mouth becomes severe. If reduced appetite and weight loss are a problem, advise parents to provide high calorie meals when drug levels are low (at breakfast and/or bedtime).
- Advise patient and/or parents to notify health care professional of behavioral changes.
- Inform patient that periodic holiday from the drug may be ordered to assess progress and decrease dependence.
- Advise patient to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Encourage patients who become pregnant while taking dextroamphetamine to enroll in registry with the National Pregnancy Registry of ADHD Medications at 1-866-961-2388 or visit online at https://womensmentalhealth.org/adhd-medications/. Registry collects information about the health of females exposed to dextroamphetamine and their baby. Infants born to mothers dependent on amphetamines have an increased risk of premature delivery and low birth weight and may have symptoms of withdrawal (dysphoria, agitation, lassitude). Growth suppression may occur in children with long-term use.
- Emphasize the importance of routine follow-up exams to monitor progress.
Home Care Issues: Advise parents to notify school nurse of medication regimen.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇