DESOXYN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DESOXYN (DESOXYN).

How it works

Desoxyn (methamphetamine) is a sympathomimetic amine that promotes release of catecholamines (primarily dopamine and norepinephrine) from presynaptic nerve terminals, blocks their reuptake, and inhibits monoamine oxidase (MAO) activity. It produces CNS stimulation and peripheral alpha- and beta-adrenergic effects.

What the body does with it

Metabolism	Hepatic metabolism via aromatic hydroxylation, N-dealkylation, and deamination; primarily metabolized by CYP2D6; minor pathways include CYP1A2 and CYP3A4.
Excretion	Renal: ~90% as unchanged drug and metabolites (primarily 4-hydroxyephedrine and 4-hydroxynorephedrine) within 48 hours; urinary pH-dependent: acidic urine increases elimination. Biliary/fecal: minor.
Half-life	Terminal elimination half-life: 9–14 hours (mean 12 hours) in adults; prolonged in alkaline urine (up to 25–30 hours). Clinically, twice-daily dosing maintains steady state after 2–3 days.
Protein binding	Low: ~15–20% bound primarily to albumin; minimal binding to alpha-1 acid glycoprotein.
Volume of Distribution	Apparent Vd: 3–5 L/kg (range 2.5–5.5 L/kg). Indicates extensive tissue distribution, particularly to brain (CNS) and lungs; exceeds total body water.
Bioavailability	Oral: ~95% (immediate-release); well absorbed, but first-pass metabolism in liver (minor). Rectal: ~80–90%. Intranasal: ~70–80%. Parenteral (IM/IV): 100%.
Onset of Action	Oral immediate-release: 30–60 minutes; extended-release: 1–2 hours. Parenteral (IM): 15–30 minutes. Nasal/oral inhalation: rapid (within minutes).
Duration of Action	Oral immediate-release: 4–6 hours; extended-release: 8–12 hours. Parenteral (IM): 6–8 hours. Duration depends on dose and individual metabolism; tolerance may develop.

Classification & Brands

Dosing & administration

Adults: 5-60 mg/day orally in divided doses, typically starting at 5 mg twice daily; maximum 60 mg/day.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 30-59 mL/min: reduce dose by 50%; GFR <30 mL/min: use is contraindicated.
Liver impairment	Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use.
Pediatric use	Children ≥6 years: 0.2-0.5 mg/kg/day orally divided every 12 hours; maximum 60 mg/day.
Geriatric use	Initiate at 2.5 mg once or twice daily; increase slowly due to increased sensitivity and risk of adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DESOXYN (DESOXYN).

Breastfeeding

Contraindicated during breastfeeding. Methamphetamine is excreted in breast milk. M/P ratio not well established but expected high. Infant exposure can cause irritability, agitation, poor feeding, and potential neurodevelopmental effects.

Teratogenic Risk

Pregnancy Category C. Methamphetamine (DESOXYN) may cause premature delivery, low birth weight, and neonatal withdrawal. First trimester: potential for congenital malformations (cardiac, cleft palate) based on animal data; human data limited. Second/third trimester: increased risk of intrauterine growth restriction, placental abruption, and preterm labor. Neonatal effects include irritability, poor feeding, and tremors.

Warnings & precautions

■ FDA Black Box Warning

High potential for abuse; prolonged administration may lead to drug dependence; misuse can cause sudden death or serious cardiovascular events. Prescribe sparingly and monitor for signs of abuse.

Side Effect Profile

Serious Effects

Absolute Contraindications

Advanced arteriosclerosis; symptomatic cardiovascular disease; moderate to severe hypertension; hyperthyroidism; glaucoma; agitated states; history of drug abuse; during or within 14 days of MAOI therapy (hypertensive crisis).

Clinical Precautions

Precautions

Serious cardiovascular events (sudden death, stroke, MI) especially in patients with structural cardiac abnormalities; exacerbation of psychiatric disorders (psychosis, mania); seizures; growth suppression in children; peripheral vasculopathy (Raynaud's phenomenon); serotonin syndrome when combined with other serotonergic drugs.

Clinical Tips & Counseling

Drug interactions

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DESOXYN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DESOXYN (DESOXYN).

How it works

What the body does with it

Metabolism	Hepatic metabolism via aromatic hydroxylation, N-dealkylation, and deamination; primarily metabolized by CYP2D6; minor pathways include CYP1A2 and CYP3A4.
Excretion	Renal: ~90% as unchanged drug and metabolites (primarily 4-hydroxyephedrine and 4-hydroxynorephedrine) within 48 hours; urinary pH-dependent: acidic urine increases elimination. Biliary/fecal: minor.
Half-life	Terminal elimination half-life: 9–14 hours (mean 12 hours) in adults; prolonged in alkaline urine (up to 25–30 hours). Clinically, twice-daily dosing maintains steady state after 2–3 days.
Protein binding	Low: ~15–20% bound primarily to albumin; minimal binding to alpha-1 acid glycoprotein.
Volume of Distribution	Apparent Vd: 3–5 L/kg (range 2.5–5.5 L/kg). Indicates extensive tissue distribution, particularly to brain (CNS) and lungs; exceeds total body water.
Bioavailability	Oral: ~95% (immediate-release); well absorbed, but first-pass metabolism in liver (minor). Rectal: ~80–90%. Intranasal: ~70–80%. Parenteral (IM/IV): 100%.
Onset of Action	Oral immediate-release: 30–60 minutes; extended-release: 1–2 hours. Parenteral (IM): 15–30 minutes. Nasal/oral inhalation: rapid (within minutes).
Duration of Action	Oral immediate-release: 4–6 hours; extended-release: 8–12 hours. Parenteral (IM): 6–8 hours. Duration depends on dose and individual metabolism; tolerance may develop.

Classification & Brands

Dosing & administration

Adults: 5-60 mg/day orally in divided doses, typically starting at 5 mg twice daily; maximum 60 mg/day.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 30-59 mL/min: reduce dose by 50%; GFR <30 mL/min: use is contraindicated.
Liver impairment	Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use.
Pediatric use	Children ≥6 years: 0.2-0.5 mg/kg/day orally divided every 12 hours; maximum 60 mg/day.
Geriatric use	Initiate at 2.5 mg once or twice daily; increase slowly due to increased sensitivity and risk of adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DESOXYN (DESOXYN).

Breastfeeding

Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

High potential for abuse; prolonged administration may lead to drug dependence; misuse can cause sudden death or serious cardiovascular events. Prescribe sparingly and monitor for signs of abuse.