MIMS Summary Table

ANTIDOTES IN OPIOID TOXICITY AND SUBSTANCE DEPENDENCE

Type
Alcohol abuse and dependence

Antidote
Naltrexone

Indication / Mode of Action

Dosage

Opioid antagonist that diminishes Adult 25 mg initially, then 50 mg daily. The the positively reinforcing total wkly dose may be given in 3 divided pleasurable effects of alcohol and doses for improved compliance (eg, 100 mg reduces craving for alcohol on Mon & Wed, and 150 mg on Fri). Childn Not recommended. Gamma-amino butyric acid (GABA) Adult 18-65 yr, 60 kg 666 mg tds; agonist and inhibitor of N-methyl<60 kg 666 mg at breakfast, 333 mg at mid-day D-aspartate (NMDA) receptors and 333 mg at night. thereby reducing craving, distress Treatment period: 1 yr. and need to consume alcohol Aldehyde dehydrogenase inhibitor Adult 500 mg once daily for 1-2 wk, then causing accumulation of enough 250 mg daily. Childn Not recommended. acetaldehyde to cause unpleasant symptoms that deter alcohol ingestion Substitute source of nicotine to Chewing gum: Initially, 2 mg for smokers who achieve and sustain tobacco smoke 20 sticks daily; 4 mg for >20 sticks daily. abstinence Usual dose: 8-12 pieces to be chewed slowly daily for 3 mth before gradual reduction. Max: 24 pieces/day. Inhaler: 6-12 car tridges/day for 3 mth. Thereafter, reduce dose gradually over 6-8 wk. Use anytime when craving or withdrawal symptoms arise. Patch: Initially, apply one 30-cm2 patch daily to the skin in the morning and remove 16 hr later at bedtime. Duration of treatment: Individualised. Usually, treatment lasts 3 mth followed by a gradual dose reduction. Use one 20-cm2 patch daily for 2-3 wk.

Acamprosate

Disulfiram

Nicotine abuse and dependence (smoking)

Nicotine

Bupropion

Opioid abuse and dependence

Opioid toxicity

Antidepressant that blocks Adult including elderly Start treatment while serotonin, norepinephrine and patient is still smoking & set a "target stop date" dopamine reuptake; exact within the first 2 wk of treatment. Continue for mechanism that helps reduce 7-12 wk. If there is no significant progress smoking is unknown towards abstinence by 7th wk, discontinue treatment. Monotherapy: Initially, 150 mg daily for 3 days increased to 150 mg bd, at least 8 hr between successive doses. Max: 150 mg/dose, 300 mg/ day. Maintenance: Up to 1 yr. Combination therapy w/ nicotine transdermal system: Individualised dosage, w/ monitoring for treatment-emergent hypertension. Buprenorphine Mixed agonist-antagonist given to Adult >16 yr Initially, 0.8-4 mg sublingually as maintain opioid abstinence a single daily dose adjusted according to response. Max: 32 mg daily; withdraw gradually. Naltrexone Opioid antagonist that diminishes Adult 25 mg initially, then 50 mg daily. The the positively reinforcing total wkly dose may be given in 3 divided doses pleasurable effects of opioids for improved compliance (eg, 100 mg on Mon & Wed, and 150 mg on Fri). Childn Not recommended. Naloxone Specific antagonist that acts Adult 0.4-2 mg IV bolus, repeated at 2-3 min competitively at opioid receptors; intervals. Childn 0.1 mg/kg IV bolus, repeated used in coma or respirator y at 2-3 min intervals. depression from unknown cause If there is no response after a total dose of or from opioid overdose 2 mg, question diagnosis. Doses up to 10 mg are rarely given. After response, doses may need to be repeated every 20-60 min; or administer continuous infusion utilizing 2/3 of initial naloxone bolus on an hourly basis.

All dosage recommendations are for non-elderly adults w/ normal renal & hepatic functions unless otherwise stated. Not all products/dosage forms are available or approved for above use in all countries. Dosage may differ between brands & countries. Refer to local prescribing information. Please refer to the Contents page for more Summary Tables.
ver01032006 Copyright 2006 MIMS

Antidotes (Opioid Toxicity)