Tuesday, July 18, 2023

amphetamine mixtures, Amphetamine Salt, Adderall, Adderall XR

 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.

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