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Naltrexone

Sold under the brand names ReVia and Vivitrol among others, is a medication primarily used to manage alcohol or opioid dependence. More

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Description

Sold under the brand names ReVia and Vivitrol among others, is a medication primarily used to manage alcohol or opioid dependence.

Generic Name

Naltrexone

Chemical names

Naltrexone; 16590-41-3; Vivitrex; ReVia; N-Cyclopropylmethylnoroxymorphone

Brand names

Naltima, Nodict

IUPAC name

(1S,5R,13R,17S)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0¹,¹³.0?,¹?.0?,¹?]octadeca-7(18),8,10-trien-14-one

Pharmacokinetics

Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%.

Actions

NA

Dosage/Dosage form

  • Initial: 25 mg for Opioid dependence as PO. 
  • 50 mg/day for adjunct in alcohol dependence. 
  • IM- Adjunct in alcohol dependence- 380 mg 4 weekly.

Therapeutic uses

  • Used as an opiate cessation
  • Also used for the management of alcohol dependence in conjunction with a behavioural modification program.

Adverse effects/Side effects

Abdominal pain, nausea, vomiting; anxiety, insomnia, lethargy, headache, musculoskeletal pain; anorexia, diarrhoea, constipation; increased thirst; chest pain; chills, dizziness; sexual dysfunction; rash, liver function abnormalities and reversible idiopathic thrombocytopenia. Inj-site reactions.

Interaction

  • With thioridazine increased risk of naltrexone-induced lethargy and somnolence.
  • May reduce effects of opiate-containing preparations e.g. those used for cough and cold, diarrhoea and pain.
  • Potentially increased hepatotoxic effects with disulfiram.
  • Decreased or increased serum levels with drugs that alter hepatic metabolism.
  • May increase insulin requirements.

Contraindications

Patients concurrently dependent on opioids; acute hepatitis or hepatic failure; acute opioid withdrawal; patients on therapeutic opioid analgesics.

Storage

Store at 20-25°C

Information

Molecular weight

341.4009

Molecular formula

C20H23NO4

CAS number

16590-41-3

Precautions

  • Hepatic or renal impairment.
  •  Monitor LFTs regularly.
  • Pregnancy, lactation.
  • Monitor for inj-site reactions.
  • History of bleeding disorders (including thrombocytopenia).