Indications
ADHD. Narcolepsy.
Action
Causes release of norepinephrine from nerve endings.
Pharmacologic effects are: CNS and respiratory stimulation,
Vasoconstriction, Mydriasis (pupillary dilation).
Therapeutic Effects: Increased motor activity,
mental alertness, and decreased fatigue in narcoleptic
patients. Increased attention span in ADHD.
Pharmacokinetics
Absorption: Well absorbed after oral administration.
Distribution: Widely distributed in body tissues,
with high concentrations in the brain and CSF. Crosses
placenta and enters breast milk.
Metabolism and Excretion: Some metabolism by
the liver. Urinary excretion is pH-dependent. Alkaline
urine promotes reabsorption and prolongs action.
Half-life: Children 6–12 yrs: 9–11 hr; Adults: 10–
13 hr (depends on urine pH).
TIME/ACTION PROFILE (CNS stimulation)
ROUTE ONSET PEAK DURATION
PO tablet: 0.5–1
hr
tablet: 3 hr
capsule: 7
hr
4–6 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Hyperexcitable
states including hyperthyroidism; Psychotic personalities;
Concurrent use or use within 14 days of MAO inhibitors
or MAO-like drugs (linezolid or methylene
blue); Suicidal or homicidal tendencies; Chemical dependence;
Glaucoma; Structural cardiac abnormalities
(mayqthe risk of sudden death); OB: Potentially embryotoxic.
Use Cautiously in: Cardiovascular disease (sudden
death has occurred in children with structural cardiac
abnormalities or other serious heart problems); History
of substance use disorder (misuse may result in serious
cardiovascular events/sudden death); Hypertension;
Diabetes mellitus; Tourette’s syndrome (may
exacerbate tics); Geri: Geriatric or debilitated patients
may be more susceptible to side effects.
Adverse Reactions/Side Effects
CNS: hyperactivity, insomnia, restlessness, tremor, aggression,
anger, behavioral disturbances, dizziness, hallucinations, headache, mania, irritability, skin pick- A
ing, talkativeness, thought disorder, tics. EENT:
blurred vision, mydriasis. CV: SUDDEN DEATH, palpitations,
tachycardia, cardiomyopathy (increased with
prolonged use, high doses), hypertension, hypotension,
peripheral vasculopathy. GI: anorexia, constipation,
cramps, diarrhea, dry mouth, metallic taste, nausea,
vomiting. GU: erectile dysfunction, libido changes, priapism.
Derm: alopecia, urticaria. Endo: growth inhibition
(with long term use in children). MS: RHABDOMYOLYSIS.
Neuro: paresthesia. Misc:
HYPERSENSITIVITY REACTIONS (including anaphylaxis and
angioedema), 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. Drugs that affect serotonergic neurotransmitter
systems, including MAO inhibitors, tricyclic antidepressants,
SSRIs, SNRIs, fentanyl, buspirone,
tramadol, lithium, and triptansqrisk of serotonin
syndrome.qadrenergic effects with other adrenergics
or thyroid preparations. Drugs that alkalinize
urine (sodium bicarbonate, acetazolamide)pexcretion,
qeffects. Drugs that acidify urine (large
doses of ascorbic acid)qexcretion,peffects.qrisk
of hypertension and bradycardia with beta blockers.
qrisk of arrhythmias with digoxin. Tricyclic antidepressants
mayqeffect of amphetamine but mayqrisk
of arrhythmias, hypertension, or hyperpyrexia. Proton
pump inhibitors mayqeffects.
Drug-Natural Products: Use with St. John’s
wort mayqrisk of serotonin syndrome.
Drug-Food: Foods that alkalinize the urine
(fruit juices) canqeffect of amphetamine.
Route/Dosage
Dose is expressed in total amphetamine content (amphetamine
dextroamphetamine).
ADHD
PO (Children 6 yr): 5 mg/day 1–2 times daily;q
daily dose by 5 mg at weekly intervals. Sustained-release
capsules can be given once daily, tablets every 8–
12 hr. If starting therapy with extended-release capsules,
start with 10 mg once daily andqby 10 mg/day at
weekly intervals (up to 40 mg/day).
PO (Adults): 20 mg/day initially (as extended-release
product).
PO (Children 3–5 yr): 2.5 mg/day in the morning;q
daily dose by 2.5 mg at weekly intervals not to exceed
40 mg/day.
Narcolepsy
PO (Adults and Children 12 yr): 10–60 mg/day in
divided doses; start with 10 mg/day,qby 10 mg/day at
weekly intervals. Sustained-release capsules can be
given once daily, tablets every 8–12 hr.
PO (Children 6–12 yr): 5 mg once daily; mayqby 5
mg/day at weekly intervals to a maximum of 60 mg/day.
Availability (generic available)
Amount is expressed in total amphetamine content
(amphetamine dextroamphetamine).
Tablets: 5 mg, 7.5 mg, 10 mg, 12.5 mg, 15 mg, 20 mg,
30 mg. Cost: Generic—All strengths $171.40/100.
Extended-release capsules: 5 mg, 10 mg, 15 mg, 20
mg, 25 mg, 30 mg. Cost: Generic—All strengths
$613.15/100.
No comments:
Post a Comment