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Dextroamphetamine Sulfate

Pronunciation

Class: Amphetamines
VA Class: CN801
CAS Number: 51-63-8
Brands: Adderall, Dexedrine, DextroStat

Warning(s)

  • Abuse Potential
  • Amphetamines have a high potential for abuse.101 102 103

  • Administration of amphetamines for prolonged periods of time may lead to drug dependence.101 102 103 b

  • Particular attention should be paid to the possibility of individuals obtaining amphetamines for nontherapeutic use or distribution to others, and the drugs should be prescribed or dispensed sparingly.101 102 103

  • The possibility that family members may abuse the patient’s medication should be considered.e

  • Sudden Death and Serious Cardiovascular Events
  • Possible sudden death and serious cardiovascular events, particularly in individuals who abuse amphetamines.101 102 103 h (See Sudden Death and Serious Cardiovascular Events under Cautions.)

Introduction

Dextrorotatory isomer of amphetamine; noncatechol, sympathomimetic amine with CNS-stimulating activity.102 b

Uses for Dextroamphetamine Sulfate

Attention Deficit Hyperactivity Disorder

Used as an adjunct to psychological, educational, social, and other remedial measures in the treatment of attention deficit hyperactivity disorder (ADHD) (hyperkinetic disorder, hyperkinetic syndrome of childhood, minimal brain dysfunction).101 102 103 b e

Can be used for ADHD in pediatric (children, adolescents) as well as adult patients.d e

Almost all studies comparing behavioral therapy versus stimulants alone have shown a much stronger therapeutic effect from stimulants than from behavioral therapy, and stimulants (e.g., amphetamines, methylphenidate) remain the drugs of choice for the management of ADHD.d e

Slideshow: Does Your Child Have ADHD? Recognizing Signs & Treatment Options

Drug therapy is not indicated in all patients with ADHD, and such therapy should be considered only after a complete evaluation including medical history has been performed.b e

Use should depend on age, adequate diagnosis (based on medical, special psychological, educational, and social resources), and the clinician’s assessment of the severity and duration of symptoms and should not depend solely on one or more behavioral characteristics.103 b e

Not recommended for ADHD symptoms associated with acute stress reactions.b

Narcolepsy

Used as a stimulant to reduce daytime sleepiness in the management of narcolepsy.101 102 b

Amphetamines remain the mainstay of treatment for narcolepsy based on a long record of clinical experience.f

Tolerance to the clinical effects may develop with long-term therapy, particularly at high dosages.f

Exogenous Obesity

Has been used as an adjunct to caloric restriction and behavioral modification in the short-term treatment of exogenous obesity.d However, because of the limited efficacy (short-lived) and risk of abuse, such use no longer is included in the FDA-approved labeling101 102 103 and is discouraged.d

The anorexigenic effect appears to be temporary, seldom lasting more than a few weeks, and tolerance may occur.d

Obesity usually is a chronic disease, and short-term or intermittent therapy with anorexigenic drugs is unlikely to maintain a long-term benefit.

Dextroamphetamine Sulfate Dosage and Administration

Administration

Oral Administration

When used as an anorexigenic, the dose is given 30–60 minutes before meals.d

Conventional Tablets (Adderall, Dexedrine, and Generic Equivalents)

Administer initial dose on awakening;101 102 b when administered in divided doses, additional doses are given at intervals of 4–6 hours.101 102 b Because of potential for insomnia, avoid administering in the late evening.101 102 b

Extended-release Capsules (Dexedrine Spansules and Generic Equivalents)

Administer initial dose on awakening.b Because of potential for insomnia, avoid administering in the late evening.102

Fixed-combination Extended-release Capsules (Adderall XR)

Administer on awakening.103 Because of potential for insomnia, avoid administering in the afternoon.103

Administer capsules with or without food;103 capsules may be swallowed intact or the entire contents of a capsule(s) may be sprinkled on a small amount of applesauce immediately prior to administration.103 Do not subdivide the capsule contents.103 Do not chew or crush the pellets contained in the capsules and do not store the sprinkle/food mixture for later use.103

Dosage

Dosages of dextroamphetamine sulfate alone and of total amphetamine base equivalence are the same.101 103 e f

Dextroamphetamine sulfate extended-release capsules or fixed-combination extended-release capsules containing various salts of dextroamphetamine and amphetamine can be substituted for their respective conventional short-acting preparations if less-frequent daily dosing is desirable.102 103 b

Dosage of fixed-combination preparations containing various salts of dextroamphetamine and amphetamine is expressed as total amphetamine base equivalence.101 103 b

Adjust dosage according to individual response and tolerance; the smallest dose required to produce the desired response should always be used.101 102 103 b

When possible, therapy should be interrupted occasionally to determine if there is a recurrence of behavioral symptoms sufficient to require continued treatment.101 102 103 b

Pediatric Patients

Attention Deficit Hyperactivity Disorder

Dosage titration usually requires 2–4 weeks.e

Conventional Tablets (Adderall, Dexedrine, and Generic Equivalents)
Oral

Dosing in pediatric patients may begin with once-daily administration in the early morning, adding a noon dose if the effect does not last throughout the school day.e Increasing the morning dose may extend its duration.e A third dose may be added at around 4 p.m. if necessary.e

Children 3–5 years of age: Initially, 2.5 mg daily; the daily dosage is increased in 2.5-mg increments at weekly intervals until the optimum response is attained.101 102 b e

Children ≥6 years of age: Initially, 5 mg once or twice daily; the daily dosage is increased in 5-mg increments at weekly intervals until the optimum response is attained.101 102 b e Total daily dosage rarely should exceed 40 mg.101 102 b e

Extended-release Capsules (Dexedrine Spansules and Generic Equivalents)
Oral

Total daily dosage of dextroamphetamine sulfate is the same for extended-release capsules (Dexedrine Spansules) and conventional tablets (Dexedrine).102

Although extended-release capsules usually are administered once daily,102 some patients may benefit from dividing the dosage into 2 doses daily.

Children 3–5 years of age: Dosage must be initiated and titrated with conventional tablets in this age group.102 Can substitute with once-daily dosing only when the total daily dose is divisible by 5 mg.102

Children ≥6 years of age: Initially, 5 or 10 mg once daily; the daily dosage is increased in 5-mg increments at weekly intervals until the optimum response is attained.102 b Total daily dosage rarely should exceed 40 mg.102 b

Fixed-combination Extended-release Capsules (Adderall XR)
Oral

Children 6–12 years of age: Initially, 10 mg once daily; daily dosage may be increased in 5- or 10-mg increments at weekly intervals to a maximum dosage of 30 mg daily.103 b Alternatively, initiate with 5 mg once daily when lower initial dosage is appropriate.103 b

Adolescents 13–17 years of age: Initially, 10 mg once daily.103 Increase to 20 mg once daily after 1 week if symptoms not adequately controlled.103 No evidence that dosages >20 mg daily provide any additional benefit.103

When switching from fixed-combination conventional tablets (Adderall) to fixed-combination extended-release capsules (Adderall XR), the total daily dosage may remain the same but may be given once daily.103 b

Narcolepsy

When intolerable adverse effects occur (e.g., insomnia, anorexia), dosage should be reduced.101 102 b

Conventional Tablets (Adderall, Dexedrine, and Generic Equivalents)
Oral

Children 6–12 years of age: Initially, 5 mg daily; daily dosage is increased in 5-mg increments at weekly intervals until the optimum response is attained.101 102 b

Children ≥12 years of age: Initially, 10 mg daily; daily dosage is increased in 10-mg increments at weekly intervals until the optimum response is attained.101 102 b

Maintenance: Usually, 5–60 mg daily, depending on patient age and response, given in divided doses.101 102 b

Extended-release Capsules (Dexedrine Spansules and Generic Equivalents)
Oral

Total daily dosage of dextroamphetamine sulfate is the same for extended-release capsules (Dexedrine Spansules) and conventional tablets (Dexedrine).102

Although extended-release capsules usually are administered once daily,102 some patients may benefit from dividing the dosage into 2 doses daily.

Children 6–12 years of age: Initially, 5 mg once daily; daily dosage is increased in 5-mg increments at weekly intervals until the optimum response is attained.102 b

Children ≥12 years of age: Initially, 10 mg once daily; daily dosage is increased in 10-mg increments at weekly intervals until the optimum response is attained.102 b

Maintenance: Usually, 5–60 mg once daily, depending on patient age and response, given in divided doses.102 b

Adults

Attention Deficit Hyperactivity Disorder
Conventional Tablets (Adderall, Dexedrine, and Generic Equivalents)

Dosage titration usually requires 2–4 weeks.e

Oral

Initially, 5 mg once or twice daily; the daily dosage is increased in 5- to 10-mg increments at weekly intervals until the optimum response is attained.101 102 b e Total daily dosage rarely should exceed 40 mg.101 102 b e

Extended-release Capsules (Dexedrine Spansules and Generic Equivalents)
Oral

Total daily dosage of dextroamphetamine sulfate is the same for extended-release capsules (Dexedrine Spansules) and conventional tablets (Dexedrine).102

Although extended-release capsules usually are administered once daily,102 some patients may benefit from dividing the dosage into 2 doses daily.

Initially, 5 or 10 mg once daily; the daily dosage is increased in 5-mg increments at weekly intervals until the optimum response is attained.102 b e Total daily dosage rarely should exceed 40 mg.102 b e

Fixed-combination Extended-release Capsules (Adderall XR)
Oral

20 mg once daily as initial therapy or when switching from other drugs.103 No evidence that dosages >20 mg daily provide any additional benefit.103

When switching from fixed-combination conventional tablets (Adderall) to fixed-combination extended-release capsules (Adderall XR), the total daily dosage may remain the same but may be given once daily.103 b

Narcolepsy

When intolerable adverse effects occur (e.g., insomnia, anorexia), dosage should be reduced.101 102 b

Conventional Tablets (Adderall, Dexedrine, and Generic Equivalents)
Oral

Initially, 10 mg daily; daily dosage is increased in 10-mg increments at weekly intervals until the optimum response is attained.101 102 b

Maintenance: Usually, 5–60 mg daily, depending on response, given in divided doses.101 102 b

Prescribing Limits

Pediatric Patients

Attention Deficit Hyperactivity Disorder

Excessive dosage can cause pediatric patients to become overfocused on the medication or to appear dull or overly restricted. Rarely, psychotic reactions, mood disturbances, or hallucinations can occur.

Conventional Tablets (Adderall, Dexedrine, and Generic Equivalents)
Oral

Dosage rarely should exceed a total daily dosage of 40 mg.101 b e Individual doses rarely should exceed 10 mg each in children <25 kg.e

Extended-release Capsules (Dexedrine Spansules and Generic Equivalents)
Oral

Dosage rarely should exceed a total daily dosage of 40 mg.102 b e Individual doses rarely should exceed 10 mg each in children <25 kg.e

Fixed-combination Extended-release Capsules (Adderall XR)
Oral

Children 6–12 years of age: Dosages >30 mg daily have not been studied systematically.103 b

Adolescents 13–17 years of age: Dosages up to 40 mg daily in individuals weighing ≤75 kg or 60 mg daily in those weighing >75 kg have been used in clinical studies; however, no evidence that dosages >20 mg daily provide any additional benefit.103

Long-term use (>3 weeks in children or >4 weeks in adolescents) has not been studied systematically.103 If used for long-term therapy, periodically reevaluate the usefulness of the drug.103

Adults

Attention Deficit Hyperactivity Disorder
Conventional Tablets (Adderall, Dexedrine, and Generic Equivalents)
Oral

Dosages up to 0.9 mg/kg daily but rarely exceeding 40 mg daily.101 102 b e Such higher doses may be more likely in adults than in school-aged children because of increased dosing frequency to cover a longer work day.e

Tolerance is more likely with relatively high dosages.e

Extended-release Capsules (Dexedrine Spansules and Generic Equivalents)
Oral

Dosages up to 0.9 mg/kg daily but rarely exceeding 40 mg daily.102 b e Such higher doses may be more likely in adults than in school-aged children because of increased dosing frequency to cover a longer work day.e

Tolerance is more likely with relatively high dosages.e

Fixed-combination Extended-release Capsules (Adderall XR)
Oral

Dosages up to 60 mg daily have been evaluated in clinical studies; however, no evidence that dosages >20 mg daily provide any additional benefit.103

Long-term use (>4 weeks) has not been studied systematically.103 If used for long-term therapy, periodically reevaluate the usefulness of the drug.103

Special Populations

Hepatic Impairment

No specific hepatic dosage recommendations.101 102 103

Renal Impairment

No specific renal dosage recommendations.101 102 103

Geriatric Patients

No specific geriatric dosage recommendations.101 103

Cautions for Dextroamphetamine Sulfate

Contraindications

  • Contraindicated in patients with hypersensitivity or idiosyncrasy to the sympathomimetic amines,101 102 103 d symptomatic cardiovascular disease,101 102 103 d hyperthyroidism,101 102 103 d moderate to severe hypertension,101 102 103 d glaucoma,101 102 103 d e or advanced arteriosclerosis;101 102 103 d within 14 days of MAO inhibitor therapy;101 102 103 d e and in agitated patients.101 102 103 d

  • Although amphetamines generally should not be used in patients with a history of drug abuse,101 102 103 d e some experts state that this is not an absolute contraindication, provided the patient can be monitored more carefully than would otherwise be indicated.e

Warnings/Precautions

Warnings

Sudden Death and Serious Cardiovascular Events

Sudden unexplained death, stroke, and MI reported in adults with ADHD receiving usual dosages of stimulants; sudden death also reported in children and adolescents with structural cardiac abnormalities or other serious cardiac conditions receiving usual dosages of the drugs.102 103 h

Epidemiologic data suggest a possible association between use of stimulants and sudden unexplained death in healthy children and adolescents.i j k FDA unable to conclude that these data affect evaluation of overall risk and benefit of stimulants used to treat ADHD in children and adolescents.i FDA is conducting an ongoing safety review of amphetamines and other stimulants to evaluate possible link between use of these agents and sudden death in children.i j k Pediatric patients with ADHD and their parents should avoid discontinuing the child’s use of such stimulants before consulting a clinician.i

Thoroughly review medical history (including evaluation for family history of sudden death or ventricular arrhythmia) and perform physical examination in all children, adolescents, and adults being considered for stimulant therapy; if initial findings suggest presence of cardiac disease, perform further cardiac evaluation (e.g., ECG, echocardiogram).102 103

In general, avoid use of CNS stimulants in patients with known serious structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, CAD, or other serious cardiac conditions.102 103 (See Contraindications under Cautions.)

Patients who develop exertional chest pain, unexplained syncope, or other manifestations suggestive of cardiac disease during stimulant therapy should undergo prompt cardiac evaluation.102 103

Effects on BP and Heart Rate

Possible modest increases in average BP (i.e., by about 2–4 mm Hg) and heart rate (i.e., by about 3–6 bpm); larger increases may occur.102 103 Modest increases not expected to have short-term sequelae; however, monitor all patients for larger changes in BP and heart rate.102 103

Caution advised in patients with underlying medical conditions that might be affected by increases in BP or heart rate (e.g., hypertension, heart failure, recent MI, ventricular arrhythmia).102 103

Exacerbation or Precipitation of Psychotic Symptoms

May exacerbate symptoms of behavior disturbance and thought disorder in patients with preexisting psychotic disorder.102 103

Psychotic symptoms (e.g., hallucinations, delusional thinking) may occur with usual dosages in children and adolescents without prior history of psychotic illness.102 103 If psychotic symptoms occur, consider causal relationship to stimulants, and discontinue therapy as appropriate.102 103

Precipitation of Manic Symptoms

May precipitate mixed or manic episodes in ADHD patients with comorbid bipolar disorder; use with caution in these patients.102 103 Prior to initiating therapy, carefully screen patients with ADHD and comorbid depressive symptoms to identify risk for bipolar disorder; screening should include a detailed psychiatric history (e.g., family history of suicide, bipolar disorder, or depression).102 103

Manic symptoms may occur with usual dosages in children and adolescents without prior history of mania.102 103 If manic symptoms occur, consider causal relationship to stimulants, and discontinue therapy as appropriate.102 103

Aggression

Aggressive behavior and hostility (frequently observed in children and adolescents with ADHD) reported in patients receiving drug therapy for ADHD.102 103 No systematic evidence that stimulants cause these adverse effects; however, monitor patients beginning treatment for ADHD for onset or worsening of aggressive behavior or hostility.102 103

Growth Suppression

Long-term (i.e., >14 months) administration expected to cause at least a temporary suppression of normal weight and/or height patterns in some children and adolescents.102 103 Dose-related weight loss reported in adolescents during first 4 weeks of therapy with fixed-combination extended-release capsules.103

Manufacturers recommend monitoring growth during treatment; patients not growing or gaining weight as expected may require temporary discontinuance of treatment.101 102 103 However, AAP states that studies of stimulants in children found little or no decrease in expected height, with any decrease in growth early in treatment being compensated for later on.

Seizures

Possible lowering of seizure threshold in patients with history of seizures, in those with prior EEG abnormalities but no history of seizures, and, very rarely, in those without history of seizures and with no prior evidence of EEG abnormalities.102 103 If seizures occur, discontinue therapy.102 103

Visual Effects

Visual disturbances (difficulty with accommodation, blurred vision) reported with stimulants.102 103

Sensitivity Reactions

Tartrazine Sensitivity

Some commercially available preparations of dextroamphetamine (e.g., DextroStat, Dexedrine tablets) contain the dye tartrazine (FD&C yellow No. 5), which may cause allergic reactions including bronchial asthma in susceptible individuals.102 b Incidence of tartrazine sensitivity is low, but it frequently occurs in patients who are sensitive to aspirin.b

General Precautions

Least amount of amphetamine feasible should be prescribed or dispensed at one time in order to minimize possible overdosage.101 102 103

Tics

Amphetamines reported to exacerbate motor and phonic tics and Tourette’s syndrome.101 102 103 However, a history of tics or their development during therapy is not an absolute contraindication to continued use.e Several controlled studies have not found stimulants to worsen or precipitate tics or Tourette’s syndrome.e Nevertheless, evaluate for presence of tics and Tourette’s syndrome in children and their families prior to initiating stimulant therapy.102 103 d

Specific Populations

Pregnancy

Category C.101 102 103 f

Risk of prematurity, low birth weight, and withdrawal symptoms (e.g., dysphoria, lassitude, agitation) in infants born to dependent women.101 102 103 f

Lactation

Distributed into milk.101 103 f Discontinue nursing or the drug.101 103

Pediatric Use

Not recommended for ADHD in children <3 years of age.101 102 103 e

Aggressive behavior, hostility, and psychotic (e.g., hallucinations, delusional thinking) or manic symptoms reported in children and adolescents receiving stimulants for management of ADHD.102 103 (See Warnings under Cautions.)

Sudden death reported in children and adolescents with structural cardiac abnormalities or other serious cardiac conditions receiving usual dosages of stimulants.102 103 Epidemiologic data also suggest a possible association between use of stimulants and sudden death in healthy children and adolescents.i j k (See Sudden Death and Serious Cardiovascular Events under Cautions.)

Long-term administration expected to cause at least a temporary suppression of normal weight and/or height patterns in some children and adolescents.102 103 (See Growth Suppression under Cautions.)

Hepatic Impairment

Possible inhibition of drug elimination, resulting in prolonged exposure.103

Renal Impairment

Possible inhibition of drug elimination, resulting in prolonged exposure.103

Common Adverse Effects

Most commonly abdominal pain (stomachache), loss of appetite, insomnia.103

Also, palpitations,101 102 103 tachycardia,101 102 103 elevation of BP,101 102 103 overstimulation,101 102 103 restlessness,101 102 103 dizziness,101 102 103 euphoria,101 102 103 dyskinesia,101 102 103 dysphoria,101 102 103 tremor,101 102 103 headache,101 102 103 dryness of mouth,101 102 103 taste aberration,101 103 diarrhea,101 102 103 constipation,101 102 103 abdominal bloating,101 103 impotence,101 102 103 changes in libido.101 102 103

Isolated reports of cardiomyopathy associated with chronic amphetamine use.101 102 103

Anorexia and weight loss may occur as undesirable effects when amphetamines are used for other than the anorectic effect.101 102 103

Interactions for Dextroamphetamine Sulfate

Inhibits MAO.103

Amphetamine or metabolites modestly inhibit CYP2D6, 1A2, and 3A4 in vitro.103 In vivo effects on metabolism of drugs metabolized by CYP isoenzymes not known.103

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

Acidifying agents, GI (ascorbic acid, glutamic acid hydrochloride, reserpine)

Decreases absorption, serum concentrations, and efficacy of amphetamines101 102 103

Acidifying agents, urinary (ammonium chloride, sodium acid phosphate)

Increases urinary excretion and decreases serum concentrations and efficacy of amphetamines101 102 103

Adrenergic blockers

Potential inhibition of adrenergic blockade101 102 103

Alkalinizing agents, GI (antacids, sodium bicarbonate)

Increases absorption and serum concentrations and potentiates the effects of amphetamines101 102 103

Avoid concomitant use103

Alkalinizing agents, urinary (acetazolamide and some thiazides)

Decreases urinary excretion and increases serum concentrations and potentiates the effects of amphetamines101 102 103

Antidepressants, tricyclic (desipramine, protriptyline)

Enhanced activity of tricyclic antidepressants; desipramine or protriptyline cause striking and sustained increases in the concentration of dextroamphetamine in the brain; cardiovascular effects can be potentiated101 102 103

Antihistamines

May counteract the sedative effects of antihistamines101 102 103

Antihypertensives

May antagonize the hypotensive effects of antihypertensives101 102 103

Chlorpromazine

Inhibits the central stimulant effects of amphetamines by blocking dopamine and norepinephrine receptors101 102 103

Can be used to treat amphetamine poisoning101 102 d

Ethosuximide

Intestinal absorption may be delayed by amphetamines101 102 103

Haloperidol

Inhibits the central stimulant effects of amphetamines by blocking dopamine receptors101 102 103

Lithium carbonate

May inhibit the anorectic and stimulatory effects of amphetamine101 102 103

MAO inhibitors

Slow the metabolism of amphetamines, increasing their effect on the release of norepinephrine and other monoamines leading to headaches and other signs of hypertensive crisis101 102 103

Toxic neurologic effects, hypertensive crisis, and malignant hyperpyrexia can occur, sometimes with fatal results101 102 103

Amphetamines contraindicated in patients currently or recently (within 14 days) receiving MAO inhibitor101 102 103

Meperidine

Amphetamines potentiate the analgesic effect of meperidine101 102 103

Methenamine

Acidifying agents used with methenamine increase urinary excretion and decrease efficacy of amphetamines101 102 103

Norepinephrine

Amphetamines enhance the adrenergic effects of norepinephrine101 102 103

Phenobarbital

Amphetamines may delay absorption of phenobarbital; concomitant use may produce a synergistic anticonvulsant action101 102 103

Phenytoin

Amphetamines may delay absorption of phenytoin; concomitant use may produce a synergistic anticonvulsant action101 102 103

Propoxyphene

In propoxyphene overdosage, amphetamine CNS stimulation is potentiated and fatal convulsions can occur101 102 103

Sympathomimetic agents

Enhanced activity of sympathomimetic agents102 103

Test, plasma corticosteroids

Can elevate plasma corticosteroid concentrations; this increase is greatest in the evening101 102 103

Test, urinary steroids

May interfere with urinary steroid determinations101 102 103

Veratrum alkaloids

Amphetamines inhibit the hypotensive effect of veratrum101 102 103

Dextroamphetamine Sulfate Pharmacokinetics

Absorption

Bioavailability

Similar for dextroamphetamine sulfate extended-release capsules versus immediate-release tablets.102

Plasma concentration-time profiles for fixed combinations containing various salts of dextroamphetamine and amphetamine are similar for single 20-mg extended-release dose versus two 10-mg immediate-release doses given 4 hours apart.103

Peak plasma concentration and AUC of amphetamines decrease with increasing body weight in individuals receiving fixed-combination extended-release capsules (Adderall XR).103

Duration

Therapeutic effects persist for 4–24 hours.PDH

Food

Food does not affect the rate or extent of absorption of dextroamphetamine sulfate from the extended-release capsules (e.g., Dexedrine Spansules).102

Food does not affect the extent of absorption of the fixed-combination extended-release preparation (Adderall XR), but prolongs Tmax by 2.5 hours (for d-amphetamine) and 2.1 hours (for l-amphetamine).103 Opening the capsule and sprinkling the contents on applesauce results in comparable absorption to the intact capsule taken in the fasted state.103

Plasma Concentrations

Tmax, immediate-release dextroamphetamine sulfate: About 3 hours.101 102

Tmax, extended-release dextroamphetamine sulfate: About 8 hours.102

Tmax, immediate-release fixed combinations containing various salts of dextroamphetamine and amphetamine: About 3 hours.103

Tmax, extended-release fixed combinations containing various salts of dextroamphetamine and amphetamine: About 7 hours.103

Therapeutic plasma concentrations are 5–10 mcg/dL.PDH

Distribution

Extent

Distributed widely throughout body, with high levels in the brain.PDH

Apparently crosses the placenta since withdrawal manifestations have occurred in neonates.101 102 103 f

Distributed into milk in concentrations 3–7 times maternal blood concentrations.f

Volume of distribution increases with increasing body weight in individuals receiving fixed-combination extended-release capsules.103

Elimination

Metabolism

Metabolized to several active metabolites.103

Enzymes involved in metabolism not clearly defined; however, CYP2D6 is involved with formation of at least one metabolite.103 Because CYP2D6 is genetically polymorphic, potential variability in metabolism among patients exists.103

Elimination Route

With normal urinary pH, excreted in urine as unchanged drug (approximately 30–40%) and metabolites (approximately 50%).103 Changes in urinary pH may alter excretion; urinary recovery of unchanged drug reported to range from 1–75%, depending on urinary pH.103 (See Specific Drugs and Laboratory Tests under Interactions.)

Clearance increases with increasing body weight in individuals receiving fixed-combination extended-release capsules.103 On a mg/kg basis, however, children have higher clearance than adolescents or adults.103

Half-life

Children 6–12 years of age: 9 hours (for d-amphetamine) or 11 hours (for l-amphetamine).103

Adolescents 13–17 years of age: 11 hours (for d-amphetamine) or 13–14 hours (for l-amphetamine).103

Adults: 10 hours (for d-amphetamine) or 13 hours (for l-amphetamine).102 103

Elimination half-life increases with increasing body weight in individuals receiving fixed-combination extended-release capsules.103

Stability

Storage

Oral

Conventional Tablets

Tight, light-resistant containers at 15–30°C.102

Extended-release Capsules

Tight, light-resistant containers at 20–25°C.102

Fixed-combination Conventional Tablets and Extended-release Capsules

Tight, light-resistant containers at 25°C (may be exposed to 15–30°C).101 103

Actions

  • Amphetamines are sympathomimetic amines with CNS stimulant activity.d

  • May block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneural space.d

  • Pharmacologic actions of amphetamines are qualitatively similar to those of ephedrine and include CNS and respiratory stimulation and sympathomimetic activity including pressor response, mydriasis, bronchodilation, and contraction of the urinary bladder sphincter.d

  • On a weight basis, dextroamphetamine has a stronger CNS action and a lesser activity on the peripheral nervous system than does the racemic amphetamine.d The CNS stimulating effect of dextroamphetamine is approximately twice that of amphetamine.d

  • Mechanism of action on peripheral structures is thought to be a combination of release of norepinephrine from stores in adrenergic nerve terminals and a direct action on both alpha and beta receptor sites.d

  • Mechanism of action involved in the central effect has not been determined.d The main sites of CNS action appear to be the cerebral cortex and possibly the reticular-activating system; stimulation by an amphetamine causes an increase in motor activity, mental alertness, diminished sense of fatigue, brighter spirits, and mild euphoria.d

  • Theories of dysfunction in ADHD focus on the prefrontal cortex, which controls many executive functions (e.g., planning, impulse control).e Stimulants have putative effects on central dopamine and norepinephrine pathways that are crucial in frontal lobe function.e

  • Produces an anorexigenic effect, leading to loss of weight.d No primary effect on appetite has been demonstrated in humans and it has been postulated that anorexigenic effects are secondary to increased sympathetic activity resulting from release of norepinephrine and dopamine. May also cause a loss of acuity of smell and taste, which may contribute to the anorexigenic effect of the drugs.d

Advice to Patients

  • Provide patient or caregiver with a copy of the manufacturer’s patient information (medication guide); discuss and answer questions about its contents as needed.102 103 Instruct patient or caregiver to read and understand contents of medication guide before initiating therapy and each time the prescription is refilled.102 103

  • Advise parents with concerns about long-term effects (e.g., effects on weight) and the need for continued therapy that drug holidays can be considered in consultation with the patient’s clinician.e PDH However, the benefits versus risks of such interruptions in therapy have not been established.e

  • Advise to take drug, particularly extended-release capsules, early in the day to minimize insomnia.102 b PDH

  • Advise not to chew or crush the pellets contained in the capsules and not to store the sprinkle/food mixture for later use.103

  • Advise not to increase dosage unless instructed by their clinician.PDH

  • Advise that appetite suppression may occur.101 102 103 d e Giving the morning dose with a meal and providing a high-caloric drink or snack late in the evening when the stimulant effects have subsided may be helpful.e

  • Question about possible substance abuse,102 103 including in other family members (since they may abuse the patient’s medication supply).e

  • Advise to inform clinician immediately if adverse cardiovascular (e.g., chest pain, shortness of breath, fainting) or psychiatric effects (e.g., hallucinations, delusional thinking, mania) occur.102 103

  • Instruct about the potential for dextroamphetamine to impair patient’s ability to perform potentially hazardous activities, such as driving or operating heavy machinery.101 102 103

  • Advise narcoleptic patients with severe sleepiness as a manifestation of their disease to avoid potentially dangerous activities at home and work and to not operate a motor vehicle until sleepiness is appropriately controlled by stimulant drug therapy.f

  • Advise narcoleptic patients about occupational and social accommodation for disabilities associated with their disease (e.g., advise about legal guidance provided by the Americans with Disabilities Act).f

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, dietary supplements, and herbal products, as well as any concomitant illnesses/conditions (e.g., cardiac/cardiovascular disease, thyroid disease, glaucoma, suicidal ideation or behaviors, mental/psychiatric disorder, seizures, hepatic or renal disease).101 102 103 d

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.101 102 103 f

  • Importance of informing patients of other important precautionary information. (See Cautions.)101 102 103 b

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Subject to control under the Federal Controlled Substances Act of 1970 as schedule II (C-II) drugs.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Dextroamphetamine Sulfate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules, extended-release

5 mg*

Dexedrine Spansule ( C-II; with povidone and propylene glycol)

GlaxoSmithKline

Dextroamphetamine Sulfate Capsules SR ( C-II)

Barr

10 mg*

Dexedrine Spansule ( C-II; with povidone and propylene glycol)

GlaxoSmithKline

Dextroamphetamine Sulfate Capsules SR ( C-II)

Barr

15 mg*

Dexedrine Spansule ( C-II; with povidone and propylene glycol)

GlaxoSmithKline

Dextroamphetamine Sulfate Capsules SR ( C-II)

Barr

Tablets

5 mg*

Dexedrine ( C-II; with tartrazine, scored)

GlaxoSmithKline

Dextroamphetamine Sulfate Tablets ( C-II; scored)

Barr, Ethex, Mallinckrodt

DextroStat ( C-II, scored)

Shire

10 mg*

Dextroamphetamine Sulfate Tablets ( C-II; scored)

Barr, Ethex, Mallinckrodt

DextroStat ( C-II; with tartrazine, double-scored)

Shire

Dextroamphetamine Sulfate Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules, extended-release

5 mg total amphetamine (as 1.25 mg with Amphetamine Sulfate 1.25 mg, Amphetamine Aspartate 1.25 mg, and Dextroamphetamine Saccharate 1.25 mg)

Adderall XR ( C-II)

Shire

10 mg total amphetamine (as 2.5 mg with Amphetamine Sulfate 2.5 mg, Amphetamine Aspartate 2.5 mg, and Dextroamphetamine Saccharate 2.5 mg)

Adderall XR ( C-II)

Shire

15 mg total amphetamine (as 3.75 mg with Amphetamine Sulfate 3.75 mg, Amphetamine Aspartate 3.75 mg, and Dextroamphetamine Saccharate 3.75 mg)

Adderall XR ( C-II)

Shire

20 mg total amphetamine (as 5 mg with Amphetamine Sulfate 5 mg, Amphetamine Aspartate 5 mg, and Dextroamphetamine Saccharate 5 mg)

Adderall XR ( C-II)

Shire

25 mg total amphetamine (as 6.25 mg with Amphetamine Sulfate 6.25 mg, Amphetamine Aspartate 6.25 mg, and Dextroamphetamine Saccharate 6.25 mg)

Adderall XR ( C-II)

Shire

30 mg total amphetamine (as 7.5 mg with Amphetamine Sulfate 7.5 mg, Amphetamine Aspartate 7.5 mg, and Dextroamphetamine Saccharate 7.5 mg)

Adderall XR ( C-II)

Shire

Tablets

5 mg total amphetamine (as 1.25 mg with Amphetamine Aspartate 1.25 mg, Amphetamine Sulfate 1.25 mg, and Dextroamphetamine Saccharate 1.25 mg)

Adderall ( C-II; double-scored)

Shire

Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate, and Amphetamine Sulfate Tablets ( C-II; double-scored)

Barr, Eon, Ranbaxy

7.5 mg total amphetamine (as 1.875 mg with Amphetamine Aspartate 1.875 mg, Amphetamine Sulfate 1.875 mg, and Dextroamphetamine Saccharate 1.875 mg)

Adderall ( C-II; double-scored)

Shire

Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate, and Amphetamine Sulfate Tablets ( C-II; double-scored)

Barr

10 mg total amphetamine (as 2.5 mg with Amphetamine Aspartate 2.5 mg, Amphetamine Sulfate 2.5 mg, and Dextroamphetamine Saccharate 2.5 mg)

Adderall ( C-II; double-scored)

Shire

Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate, and Amphetamine Sulfate Tablets ( C-II; double-scored)

Barr, Eon, Ranbaxy

12.5 mg total amphetamine (as 3.125 mg with Amphetamine Aspartate 3.125 mg, Amphetamine Sulfate 3.125 mg, and Dextroamphetamine Saccharate 3.125 mg)

Adderall ( C-II; double-scored)

Shire

Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate, and Amphetamine Sulfate Tablets ( C-II; double-scored)

Barr

15 mg total amphetamine (as 3.75 mg with Amphetamine Aspartate 3.75 mg, Amphetamine Sulfate 3.75 mg, and Dextroamphetamine Saccharate 3.75 mg)

Adderall ( C-II; double-scored)

Shire

Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate, and Amphetamine Sulfate Tablets ( C-II; double-scored)

Barr

20 mg total amphetamine (as 5 mg with Amphetamine Aspartate 5 mg, Amphetamine Sulfate 5 mg, and Dextroamphetamine Saccharate 5 mg)

Adderall ( C-II; double-scored)

Shire

Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate, and Amphetamine Sulfate Tablets ( C-II; double-scored)

Barr, Eon, Ranbaxy

30 mg total amphetamine (as 7.5 mg with Amphetamine Aspartate 7.5 mg, Amphetamine Sulfate 7.5 mg, and Dextroamphetamine Saccharate 7.5 mg)

Adderall ( C-II; double-scored)

Shire

Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine Sulfate Tablets ( C-II; double-scored)

Barr, Eon, Ranbaxy

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Adderall 10MG Tablets (TEVA PHARMACEUTICALS USA): 20/$85.99 or 30/$123.97

Adderall 15MG Tablets (TEVA PHARMACEUTICALS USA): 20/$84.99 or 30/$123.97

Adderall 20MG Tablets (TEVA PHARMACEUTICALS USA): 20/$84.99 or 30/$122.97

Adderall 30MG Tablets (TEVA PHARMACEUTICALS USA): 20/$83.99 or 30/$121.97

Adderall 5MG Tablets (TEVA PHARMACEUTICALS USA): 20/$87.99 or 30/$130.98

Adderall XR 10MG 24-hr Capsules (SHIRE US INC.): 20/$158.26 or 30/$237.39

Adderall XR 15MG 24-hr Capsules (SHIRE US INC.): 20/$162.00 or 30/$241.96

Adderall XR 20MG 24-hr Capsules (SHIRE US INC.): 20/$158.26 or 30/$237.39

Adderall XR 25MG 24-hr Capsules (SHIRE US INC.): 20/$158.26 or 30/$237.39

Adderall XR 30MG 24-hr Capsules (SHIRE US INC.): 20/$158.26 or 30/$237.39

Adderall XR 5MG 24-hr Capsules (SHIRE US INC.): 20/$156.99 or 30/$235.49

Amphetamine-Dextroamphetamine 10MG 24-hr Capsules (GLOBAL PHARMACEUTICAL CORP): 20/$121.99 or 30/$181.98

Amphetamine-Dextroamphetamine 10MG Tablets (SANDOZ): 20/$38.99 or 30/$51.97

Amphetamine-Dextroamphetamine 12.5MG Tablets (TEVA PHARMACEUTICALS USA): 20/$45.99 or 30/$68.97

Amphetamine-Dextroamphetamine 15MG 24-hr Capsules (GLOBAL PHARMACEUTICAL CORP): 30/$171.99 or 90/$483.96

Amphetamine-Dextroamphetamine 15MG Tablets (TEVA PHARMACEUTICALS USA): 20/$32.99 or 30/$49.49

Amphetamine-Dextroamphetamine 20MG 24-hr Capsules (GLOBAL PHARMACEUTICAL CORP): 20/$114.99 or 30/$164.98

Amphetamine-Dextroamphetamine 20MG Tablets (COREPHARMA LLC): 20/$26.99 or 30/$40.49

Amphetamine-Dextroamphetamine 25MG 24-hr Capsules (GLOBAL PHARMACEUTICAL CORP): 20/$114.99 or 30/$164.98

Amphetamine-Dextroamphetamine 30MG 24-hr Capsules (GLOBAL PHARMACEUTICAL CORP): 20/$114.99 or 30/$172.49

Amphetamine-Dextroamphetamine 30MG Tablets (TEVA PHARMACEUTICALS USA): 20/$33.32 or 30/$49.98

Amphetamine-Dextroamphetamine 5MG 24-hr Capsules (GLOBAL PHARMACEUTICAL CORP): 20/$116.00 or 30/$165.97

Amphetamine-Dextroamphetamine 5MG Tablets (SANDOZ): 20/$35.99 or 30/$49.98

Amphetamine-Dextroamphetamine 7.5MG Tablets (TEVA PHARMACEUTICALS USA): 20/$32.99 or 30/$49.49

Dexedrine 10MG 24-hr Capsules (AMEDRA PHARMACEUTICALS): 20/$155.99 or 30/$227.97

Dexedrine 15MG 24-hr Capsules (AMEDRA PHARMACEUTICALS): 20/$153.99 or 30/$225.98

Dexedrine 5MG 24-hr Capsules (AMEDRA PHARMACEUTICALS): 20/$149.99 or 30/$224.98

Dextroamphetamine Sulfate 10MG Tablets (TEVA PHARMACEUTICALS USA): 20/$20.21 or 30/$30.32

Dextroamphetamine Sulfate 5MG Tablets (ETHEX): 20/$14.99 or 30/$17.97

Dextroamphetamine Sulfate CR 10MG 24-hr Capsules (TEVA PHARMACEUTICALS USA): 20/$100.99 or 30/$151.48

Dextroamphetamine Sulfate CR 15MG 24-hr Capsules (TEVA PHARMACEUTICALS USA): 20/$128.99 or 30/$190.98

Dextroamphetamine Sulfate CR 5MG 24-hr Capsules (TEVA PHARMACEUTICALS USA): 20/$80.99 or 30/$120.84

DextroStat 10MG Tablets (SHIRE US INC.): 20/$21.99 or 30/$32.99

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions June 1, 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. American Academy of Pediatrics Committee on Quality Improvement and Subcommittee on Attention-Deficit/Hyperactivity Disorder. Clinical treatment guideline: treatment of the school-aged child with attention-deficit/hyperactivity disorder. Pediatrics. 2001; 108:1033-44. [IDIS 470916] [PubMed 11581465]

101. Shire US Inc. Adderall (mixed salts of a single-entity amphetamine product) prescribing information (dated 2006 Jun). In: Physicians’ desk reference. From the Thomson Healthcare website. Accessed 2006 Dec 6.

102. GlaxoSmithKline . Dexedrine (dextroamphetamine sulfate) Spansule sustained-release capsules and tablets prescribing information. Research Triangle Park, NC; 2007 Mar.

103. Shire US Inc. Adderall XR (mixed salts of a single-entity amphetamine product) capsules prescribing information. Wayne, PA; 2007 Mar.

PDH. Schilling McCann JA, Publisher. Pharmacists drug handbook. 2nd ed. Philadelphia, PA: Lippincott Williams and Wilkins and American Society of Health-System Pharmacists; 2003.

HID. Trissel LA. Handbook on injectable drugs. 12th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2003:175-80.

b. AHFS drug information 2007. McEvoy GK, ed. Dextroamphetamine. Bethesda, MD: American Society of Health-System Pharmacists; 2007:2475-6.

d. AHFS drug information 2007. McEvoy GK, ed. Amphetamines general statement. Bethesda, MD: American Society of Health-System Pharmacists; 2007:2468-72.

e. American Academy of Child and Adolescent Psychiatry. Practice parameter for the use of stimulant medications in the treatment of children, adolescents and adults. J Am Acad Child Adolesc Psychiatry. 2002; 41(2 Suppl):26S-49S. [IDIS 476108] [PubMed 11833633]

f. Littner M, Johnson SF, McCall WV et al for the American Academy of Sleep Medicine Standards of Practice Committee. Practice parameters for the treatment of narcolepsy: an update for 2000. Sleep. 2001; 24:451-66. [PubMed 11403530]

h. US Food and Drug Administration. Adderall and Adderall XR (amphetamine). Rockville, MD; 2005 Feb 9. Alert for Healthcare Professionals.

i. Food and Drug Administration. FDA Alert: Information for healthcare professionals: Communication about an ongoing safety review of stimulant medications [dexmethylphenidate (marketed as Focalin, Focalin XR), dextroamphetamine (marketed as Dexedrine, Dexedrine Spansules, Dextrostat, and generics), lisdexamfetamine (marketed as Vyvanse), methamphetamine (marketed as Desoxyn), methylphenidate (marketed as Concerta, Daytrana, Metadate CD, Metadate ER, Methylin, Methylin ER, Ritalin, Ritalin-LA, and Ritalin-SR), mixed salts amphetamine (marketed as Adderall and Adderall XR), and pemoline (marketed as Cylert and generics)] used in children with attention-deficit/hyperactivity disorder (ADHD). Rockville, MD; 2009 Jun 23. From the FDA website.

j. Gould MS, Walsh BT, Munfakh JL et al. Sudden death and use of stimulant medications in youths. Am J Psychiatry. 2009; 166:992-1001. [PubMed 19528194]

k. Vitiello B, Towbin K. Stimulant treatment of ADHD and risk of sudden death in children. Am J Psychiatry. 2009; 166:955-7. [PubMed 19528196]

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