Lisdexamfetamine Dimesylate

Trade Names:
Vyvanse
- Capsules 20 mg
- Capsules 30 mg
- Capsules 40 mg
- Capsules 50 mg
- Capsules 60 mg
- Capsules 70 mg

Pharmacology

User Reviews & Ratings As a treatment for... Avg User Ratings [?] Oppositional Defiant Disorder 1 reviews Rate it! 10 Narcolepsy 1 reviews Rate it! 9.2 Attention Deficit Hyperactivity Disorder 112 reviews Rate it! 8.4 Showing 3 of 4 conditions - Show All... Compare with other drugs.

Prodrug for dextroamphetamine, which is thought to block the reuptake of norepinephrine and dopamine into presynaptic neurons and to increase the release of these monoamines into the extraneuronal space.

Pharmacokinetics

Absorption

Rapidly absorbed from the GI tract. T _max of lisdexamfetamine is 1 h. T _max of dextroamphetamine is 3.5 h. Food prolongs the T _max of dextroamphetamine by approximately 1 h (from 3.8 h at fasted state to 4.7 h after a high-fat meal).

Metabolism

Converted to dextroamphetamine and L-lysine by first-pass intestinal and/or hepatic metabolism.

Elimination

Approximately 96% of the oral dose is recovered in the urine, with 42% related to amphetamine, 25% to hippuric acid, and 2% to intact lisdexamfetamine. Plasma half-life of lisdexamfetamine is less than 1 h.

Special Populations

Has not been studied in elderly patients.

Systemic exposure is similar for men and women.

Pharmacokinetic studies have not been conducted.

The pharmacokinetics are similar in healthy patients from 6 y of age to adult.

Indications and Usage

Treatment of attention deficit hyperactivity disorder (ADHD).

Contraindications

Advanced arteriosclerosis; symptomatic CV disease; moderate to severe hypertension; hyperthyroidism; known hypersensitivity or idiosyncrasy to sympathomimetic amines; glaucoma; agitated states; history of drug abuse; concomitant MAOI use or use within 14 days.

Dosage and Administration

PO Start with 30 mg once daily in the morning. Dosage may be adjusted in 10 or 20 mg/day increments at approximately weekly intervals (max, 70 mg/day).

General Advice

• Patient should take in the morning to avoid potential insomnia.
• May be taken without regard to food.
• Capsules may be taken whole or opened and the entire contents dissolved in a glass of water and taken immediately; do not store mixture for use at later time.
• Patient should not take less than 1 capsule daily.
• Interrupt therapy occasionally to determine if there is recurrence of behavioral symptoms sufficient to require continued therapy.

Storage/Stability

Store at 59° to 86°F. Dispense in a tightly closed, light-resistant container.

Drug Interactions

Effects may be inhibited by amphetamines.

Sedative effects may be decreased by amphetamines.

Hypotensive effect may be antagonized by amphetamines.

Intestinal absorption may be delayed by amphetamines.

Risk of hypertension may be increased.

Central stimulant effects of amphetamines may be inhibited. Do not use amphetamines for weight reduction in patients receiving phenothiazines.

Anorectic and stimulatory effects of amphetamines may be inhibited.

Increased risk of hypertensive crisis, malignant hyperpyrexia, and death; coadministration of MAOIs and amphetamines is contraindicated during or within 14 days following the administration of MAOIs.

Analgesic effect of meperidine may be potentiated.

Enhanced urinary excretion of amphetamines, decreasing the efficacy.

Adrenergic effect may be enhanced by amphetamine.

Absorption may be delayed by amphetamines; synergistic anticonvulsant activity may occur.

Amphetamine CNS stimulation may be potentiated, increasing the risk of fatal seizures.

Increased risk of serotonin syndrome.

Amphetamines may enhance the activity of sympathomimetrics.

Activity may be enhanced by amphetamines; d-amphetamine brain concentrations may be increased and sustained; CV effects may be potentiated.

Decreased urinary excretion of amphetamines, prolonging the effects and possible toxicity of amphetamines.

Laboratory Test Interactions

Interference with urinary steroid determinations.

Adverse Reactions

Cardiovascular

Increased BP (3%); increased heart rate (2%); palpitation (postmarketing).

Cardiomyopathy; MI; palpitation; stroke; tachycardia.

CNS

Insomnia (27%); irritability (10%); anxiety (6%); dizziness (5%); feeling jittery, initial insomnia (4%); affect lability, agitation, restlessness (3%); somnolence, tic, tremor (2%); aggression, depression, dyskinesia, dysphoria, euphoria, hallucination, logorrhea, mania, psychotic episodes, seizure (postmarketing).

Changes in libido, exacerbation of motor and phonic tics and Tourette syndrome, headache, overstimulation.

Dermatologic

Hyperhidrosis, rash (3%); urticaria (postmarketing).

Stevens-Johnson syndrome, toxic epidermal necrolysis.

EENT

Mydriasis, vision blurred (postmarketing).

GI

Dry mouth (26%); upper abdominal pain (12%); vomiting (9%); diarrhea, nausea (7%).

Constipation, unpleasant taste.

Genitourinary

Impotence.

Metabolic-Nutritional

Decreased appetite (39%); decreased weight (9%); anorexia (5%).

Respiratory

Dyspnea (2%).

Miscellaneous

Pyrexia (2%); angioedema (postmarketing).

Anaphylaxis, sudden death.

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in children younger than 6 or older than 12 yr of age. Amphetamines are not recommended for children younger than 3 yr of age. Consistently treated children have a temporary slowing in growth rate without evidence of growth rebound. Do not use stimulant products in patients with known serious structural abnormalities, cardiomyopathy, serious heart rhythm abnormalities, or other serious cardiac problems.

Abrupt cessation

Abruptly stopping prolonged, high-dose administration may result in extreme fatigue and mental depression.

Aggression

Aggressive behavior and hostility have been associated with treatment in children and adolescents.

Bipolar illness

Use with caution because of possible induction of mixed/manic episodes.

CV events

Sudden death associated with CNS stimulant treatment at usual doses in children and adolescents with structural cardiac abnormalities or other serious heart problems have occurred. Sudden death, stroke, and MI have occurred in adults taking stimulant drugs in ADHD doses. Do not use stimulant products in patients with known serious structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, or other serious cardiac problems.

Dependence

Amphetamines have a high potential for dependence and abuse.

Hypertension and heart rate

Increases in BP and heart rate may occur.

Manic or psychotic symptoms

Treatment-emergent manic or psychotic symptoms (eg, delusional thinking) may occur.

Prescribing

To minimize the possibility of an overdose, prescribe the least amount feasible.

Psychosis

Symptoms of behavioral disturbance and thought disorders in patients with preexisting psychotic disorders may be exacerbated.

Seizures

The seizure threshold may be lowered in patients with a history of seizures.

Tics

Motor and phonic tics as well as Tourette syndrome may be exacerbated.

Tolerance

Because tolerance can occur, do not exceed the recommended dose.

Visual disturbances

Difficulties in accommodation and blurred vision have been reported with stimulant treatment.

Overdosage

Symptoms

Abdominal cramps, arrhythmias, assaultiveness, circulatory collapse, confusion, depression, diarrhea, fatigue, hallucinations, hyperpyrexia and rhabdomyolysis, hyperreflexia, hypertension, hypotension, nausea, panic states, rapid respiration, restlessness, seizures and coma, tremor, vomiting.

Patient Information

• Advise patient to read the Medication Guide before using product the first time and with each refill.
• Inform patient that this medication may impair ability to engage in potentially hazardous activities, such as operating machinery or vehicles.
• Advise patients that stimulant therapy at usual doses may cause treatment-emergent psychotic or manic symptoms in patients without a history of these conditions.
• Inform patients who are not growing or gaining weight as expected that they may need to have their treatment interrupted.
• Advise patients of the potential for serious CV risk (including hypertension, MI, stroke) with lisdexamfetamine.

Link to Page

Print Page

Email Page

Add to List