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.
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Antidotes (Opioid Toxicity)

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