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Nalsup (NALTREXONE)

brandsClassNalsup commonly prescribed forHow Nalsup worksHow long until Nalsup worksNotable Side EffectsLife Threatening Side Effectsweight gainsedationWhat to do about Nalsup side effectsusual dosage rangeDosage Formslong term usehabit formingRenal ImpairmentHepatic ImpairmentCardiac ImpairmentElderlyChildren and AdolescentsPregnancyBreast Feeding

THERAPEUTICS

brands

  • Naltima
  • Nodict
  • Nalsup

Class

  • Neuroscience-based Nomenclature: opioid receptor antagonist (O-RAn)
  • Alcohol dependence treatment; mu opioid receptor antagonist

Nalsup commonly prescribed for

(Bold for FDA approved)

• Alcohol dependence
• Blockade of effects of exogenously administered opioids
• Prevention of relapse to opioid dependence
• Impulse Control Disorders(off-label, under study)

How Nalsup works

• Blocks mu opioid receptors, preventing exogenous opioids from binding there and thus preventing the pleasurable effects of opioid consumption

• Reduces alcohol consumption through modulation of opioid systems, thereby reducing the reinforcing effects of alcohol

How long until Nalsup works

• Can begin working within a few days but maximum effects may not be seen for a few weeks

SIDE EFFECTS

Notable Side Effects

• Nausea, vomiting, decreased appetite

• Dizziness, dysphoria, anxiety

• Injection site reactions (pain, tenderness, pruritis, induration, swelling, erythema, or bruising); in some cases injection site reactions may be very severe

Life Threatening Side Effects

• Eosinophilic pneumonia

• Hepatocellular injury (at excessive doses)

• Severe injection site reactions requiring surgery

weight gain

unusual

unusual

sedation

not usual

not usual

What to do about Nalsup side effects

• Wait

• Adjust dose

• If side effects persist, discontinue use

DOSING AND USE

usual dosage range

• Oral: 50 to 150 mg/day

• Injection: 380 mg every 4 weeks

Dosage Forms

• Tablet 25 mg, 50 mg, 100 mg

• Intramuscular formulation 380 mg/vial

long term use

• Has been studied in trials up to 1 year

habit forming

• No

SPECIAL POPULATIONS

Renal Impairment

• Dose adjustment not generally necessary for mild impairment

• Not studied in moderate to severe renal impairment

Hepatic Impairment

• Has the potential to cause hepatocellular injury when given in excessive doses

• Dose adjustment not generally necessary for mild impairment

• Not studied in severe hepatic impairment

• Contraindicated in acute hepatitis or liver failure

Cardiac Impairment

• Limited available data

Elderly

• Safety and efficacy have not been established

• Some patients may tolerate lower doses better

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Pregnant women needing to stop drinking may consider behavioral therapy before pharmacotherapy

• Not generally recommended for use during pregnancy, especially during first trimester

Breast Feeding

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or bottle feed

Based on data Published online by Cambridge University Press

Compiled by Dr. Jash Ajmera