amphetamine dextroamphetamine ADDERALL
Class: StimulantFDA Indications: ADHD, Narcolepsy
Off-Label Use: Treatment Resistant Depression, Depressive Symptoms In Medically-ill Elderly, Post-stroke Depression, Depression, Cognitive Impairment And Severe Fatigue Patients With HIV Infection
Prescribing
FDA Schedule IIForms: 5, 10, 15, 20, 25, 30mg ER Capsules; 5, 7.5, 10, 12.5, 15, 20, 30mg IR Tablets
Dose Range: 5-60 mg/day
Starting: IR formulation- Initiate at 5 mg qd or bid, ↑ by 5 mg at weekly intervals. Usual max 40 mg daily divided in 1-3 doses; XR formulation- Initiate at 20 mg qam
Stopping: Taper to avoid withdrawal
Monitoring: Perform a targeted cardiac history, and cardiac exam before initiation. Monitor baseline blood pressure, heart rate, and ECG.
Precautions
Contraindications: Advanced atherosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyperthyroidism, glaucoma, agitated state, hx of drug abuse, use with (or within 14 days of) an MAO inhibitorSerious Side Effects: Serious cardiovascular events. Sudden cardiac death, stroke, and MI. Can exacerbate pre-existing bipolar or psychotic disorder. May lower seizure threshold.
Side Effects: decreased appetite, weight loss, nausea, tics, peripheral vasculopathy
Pharmacodynamics
1° MOA: Promotes presynaptic DA & NE releaseTarget: VMAT2 (inhibitor), NET & DAT (competitive inhibitor & pseudosubstrate), MAO (inhibitor, weak)
Pharmacokinetics
t½: 12 (9-14)° TMAX: IR- 3°, ER 7°Substrate of: 2D6
Inhibits: ∅ ; Induces: ∅
Active Metabolites: 4HA, 4-hydroxynorephedrine, PPA
DDIs
- - avoid with MAO inhibitors
- - may ↑ levels and effects of opioids and sympathomimetics
Misc
- - mixed amphetamine salts, d-amphetamine to l-amphetamine salts in a 3:1 ratio
- - IR lasts ~4-6°; XR lasts ~8-10°
- - taking with food can delay Tmax 2-3°
- - can potentially exacerbate symptoms in patients with pre-existing psychotic disorders or potentially induce mania in bipolar patients
- - an oral suspension (1 mg/mL) can be made with tablets: crush ten 10 mg tabs to a fine powder, add small portions of Ora-Sweet and mix into a paste, add liquid vehicle to make 100 mL of solution; stable for 30 days, mix well before each use
Special Populations
Category C—Majority of data based on illicit amphetamine and methamphetamine use. May increase risk for premature birth and low birth weight. Newborns may experience withdrawal. Children may experience behavioral problems.
Majority of data based on illicit amphetamine and methamphetamine use. Amphetamine are excreted into breast milk in higher concentrations than present in mothers serum. May decrease milk production. Can cause irritability, agitation, and crying in nursing infants.
Start lower, i.e. 10 mg/d (typical dose is 20 mg/d); consider a 5 mg/d starting dosage for especially frail patients; give second dose mid-afternoon to avoid insomnia
No adjustments necessary
No dosage adjustments necessary