Addiction Aids

Acamprosate (Campral ® ) buprenorphine (Buprenex®, Subutex ®)
Disulfiram (Antabuse ® ) Naltrexone (ReVia®, Vivitrol™)
Suboxone ® (Buprenorphine and naloxone) varenicline (Chantix ® )

Acamprosate  (Campral ® ) top of page icon

CAMPRAL is indicated for the maintenance of abstinence from alcohol in patients with alcohol dependence who are abstinent at treatment initiation. Treatment with CAMPRAL should be part of a comprehensive management program that includes psychosocial support.
CAMPRAL is not known to cause alcohol aversion and does not cause a disulfiram-like reaction as a result of ethanol ingestion. Pharmacodynamic studies have shown that acamprosate calcium reduces alcohol intake in alcohol-dependent animals in a dose-dependent manner and that this effect appears to be specific to alcohol and the mechanisms of alcohol dependence. The efficacy of CAMPRAL in promoting abstinence has not been demonstrated in subjects who have not undergone detoxification and not achieved alcohol abstinence prior to beginning CAMPRAL treatment. The efficacy of CAMPRAL in promoting abstinence from alcohol in polysubstance abusers has not been adequately assessed.
Dosage: two 333 mg tablets (each dose should total 666 mg) taken three times daily. A lower dose may be effective in some patients.

Treatment with CAMPRAL should be initiated as soon as possible after the period of alcohol withdrawal, when the patient has achieved abstinence, and should be maintained if the patient relapses.

Dosage in Renal Impairment
[30-50 mL/min]: starting dose: 333 mg tid.
[<30 ml/min]: AVOID USE.

Supplied: 333mg tablet

MOA: While its mechanism is not completely understood, it is believed that Acamprosate is effective on the neurotransmitters GABA (gamma-aminobutyric acid) and glutamate. These chemicals function in the Nucleus accumbens of the brain where the alcohol reward center is located. Chronic alcohol dependence alters the levels and interaction of GABA and glutamate with their receptors, and treatment with Acamprosate calcium is believed to normalize this system in the brain. It often takes several months to “re-train” the brain to become accustomed to normal levels.

Treatment with Acamprosate calcium typically starts between 2 and 7 days after ceasing alcohol consumption. The medication is taken orally, in a 333mg pill, taken three times daily, and treatment traditionally lasts around six months. It is important to note that all studies of this drug included behavioral therapy and other forms of treatment. All current recommendations include a multi-specialty approach to treatment when using this medication.

buprenorphine (Buprenex®,  Subutex ®) top of page icon

Dosing (Adults)
Acute pain (moderate to severe):    I.M.: Initial: Opiate-naive: 0.3 mg every 6-8 hours as needed; initial dose (up to 0.3 mg) may be repeated once in 30-60 minutes after the initial dose if needed; usual dosage range: 0.15-0.6 mg every 4-8 hours as needed.   Slow I.V.: Initial: Opiate-naive: 0.3 mg every 6-8 hours as needed; initial dose (up to 0.3 mg) may be repeated once in 30-60 minutes after the initial dose if needed.

Opioid dependence: Sublingual:  Induction: Range: 12-16 mg/day (doses during an induction study used 8 mg on day 1, followed by 16 mg on day 2; induction continued over 3-4 days). Treatment should begin at least 4 hours after last use of heroin or short-acting opioid, preferably when first signs of withdrawal appear. Titrating dose to clinical effectiveness should be done as rapidly as possible to prevent undue withdrawal symptoms and patient drop-out during the induction period.   Maintenance: Target dose: 16 mg/day; range: 4-24 mg/day; patients should be switched to the buprenorphine/naloxone combination product for maintenance and unsupervised therapy.

Supplied:
Injection, solution:
Buprenex®: 0.3 mg/mL (1 mL)

Tablet, sublingual:
Subutex®: 2 mg, 8 mg
Oval white tablets containing 2mg  or  8 mg buprenorphine.

Buprenorphine is a partial opiate agonist (agonist and antagonist properties.). Like most partial agonists, it has a safer profile than that of a full agonist. It exhibits a ceiling effect, which means that once a certain receptor occupancy desired dosage level has been achieved, additional dosing does not produce additional effects, including eliminating the typical possible opiate overdose effects of respiratory depression and/or death. By combining it with Naloxone, in a 4:1 ratio, it is hoped that it will prevent both diversion of the drug and intravenous injection. The withdrawal syndrome seen with buprenorphine is much milder than that of other full agonist opiates.

Buprenorphine has been approved by the FDA for use in the United States as an opiate detoxification and opiate maintenance agent. There will be two forms of the medication (available in 2 mg and 8 mg sublingual tablets: Subutex - buprenorphine alone and Suboxone, which is Buprenorphine combined with Naloxone. This combination form prevents intravenous use of the tablet after crushing; in which the user would get an antagonist effect of the naloxone, or at the least, a diminished opiate effect. Doses for opioid dependence will range from 2 mg to 32 mg, with the average being approximately 16 mg. and the medication can be used for detoxification or maintenance treatment.

Disulfiram  (Antabuse ® ) top of page icon

Aldehyde Dehydrogenase Inhibitor.
Indications
: Disulfiram is an aid in the management of selected chronic alcohol patients who want to remain in a state of enforced sobriety so that supportive and psychotherapeutic treatment may be applied to best advantage. Disulfiram is not a cure for alcoholism. When used alone, without proper motivation and supportive therapy, it is unlikely that it will have any substantive effect on the drinking pattern of the chronic alcoholic. Disulfiram should never be administered until the patient has abstained from alcohol for at least 12 hours.
Initial Dosage Schedule: In the first phase of treatment. a maximum of 500 mg daily is given in a single dose for one to two weeks. Although usually taken in the morning, Disulfiram may be taken on retiring by patients who experience a sedative effect. Alternatively, to minimize, or eliminate, the sedative effect, dosage may be adjusted downward. 
Maintenance Regimen: The average maintenance dose is 250 mg daily (range, 125 to 500 mg). Maximum daily dose is 500 mg.  Duration of therapy is to continue until the patient is fully recovered socially and a basis for permanent self control has been established. Maintenance therapy may be required for months or even years.
Supplied: 250 mg, 500mg tablet.

Antabuse is an older medication that is worth considering in some patients to help them remain in recovery. Antabuse produces a sensitivity to alcohol which results in a highly unpleasant reaction when the individual under treatment ingests alcohol. MOA: Antabuse blocks the oxidation of alcohol. A product of this oxidation is acetaldehyde. If antabuse is taken, the metabolism stops at the point of acetaldehyde production and there will be an increase in the concentration of acetaldehyde 5 - 10 times higher than in normal alcohol metabolism. The accumulation of acetaldehyde produces the " ANTABUSE - ALCOHOL REACTION". This reaction can range from a flush and throbbing in the head and neck to nausea, vomiting, breathing difficulty, chest pain, heart failure and possible death.
Contraindications
: This medication must be prescribed by a physician and cannot be given to anyone with a history of severe heart disease, psychosis, allergy to antabuse, pregnancy, paraldehyde use, or metronidazole use. It must be used with caution in the patient with a history of diabetes, seizures, and liver disease.

Naltrexone  (ReVia®, Vivitrol™) top of page icon

Dosing (Adults)
Alcohol dependence
Oral: A dose of 50 mg once daily is recommended for most patients (administer with food or antacids or after meals). The placebo-controlled studies that demonstrated the efficacy of REVIA as an adjunctive treatment of alcoholism used a dose regimen of REVIA 50 mg once daily for up to 12 weeks. Other dose regimens or durations of therapy were not evaluated in these trials.  Alt: 25 mg; if no withdrawal signs within 1 hour give another 25 mg; maintenance regimen is flexible, variable and individualized (50 mg/day to 100-150 mg three times per week). 

I.M.:: 380 mg once every 4 weeks (Administer I.M. into the upper outer quadrant of the gluteal area. Injection should alternate between the two buttocks.)

A patient is a candidate for treatment with REVIA if:

1) The patient is willing to take a medicine to help with alcohol dependence.
2) The patient is opioid free for 7-10 days.
3) The patient does not have severe or active liver or kidney problems (Typical guidelines suggest liver function tests no greater than 3 times the upper limits of normal, and bilirubin normal.)
4) The patient is not allergic to REVIA , and no other contraindications are present

Opioid antidote (do not give until patient is opioid-free for 7-10 days as required by urinalysis): Oral: 25 mg; if no withdrawal signs within 1 hour give another 25 mg; maintenance regimen is flexible, variable and individualized (50 mg/day to 100-150 mg three times per week).

Supplied:
Injection, powder for suspension [extended-release microspheres]:
Vivitrol™: 380 mg

Tablet: 50 mg
Depade®: 25 mg, 50 mg, 100 mg
ReVia®: 50 mg

Suboxone ® (Buprenorphine and naloxone) top of page icon

Indication: Treatment of opioid dependence. Not recommended for use during the induction period. SUBUTEX or SUBOXONE is administered sublingually as a single daily dose in the range of 12 to 16 mg/day. When taken sublingually, SUBOXONE and SUBUTEX have similar clinical effects and are interchangeable. There are no adequate and well-controlled studies using SUBOXONE as initial medication.
Initial treatment should begin using buprenorphine oral tablets (Subutex). Patients should be switched to the combination product for maintenance and unsupervised therapy.
Maintenance: Target dose (buprenorphine): 16 mg/day (range: 4-24 mg/day.)

Adjusting the dose until the maintenance dose is achieved:
The recommended target dose of SUBOXONE is 16 mg/day. Clinical studies have shown that 16mg of SUBUTEX or SUBOXONE is a clinically effective dose compared with placebo and indicate that doses as low as 12 mg may be effective in some patients. The dosage of SUBOXONE should be progressively adjusted in increments / decrements of 2mg or 4mg to a level that holds the patient in treatment and suppresses opioid withdrawal effects. This is likely to be in the range of 4mg to 24mg per day depending on the individual.

Supplied: sublingual tablet: Buprenorphine 2 mg and naloxone 0.5 mg; buprenorphine 8 mg and naloxone 2 mg.

varenicline  (Chantix ® ) top of page icon

MOA: partial agonist selective for α4β2 nicotinic acetylcholine receptor subtypes. Indications: aid to smoking cessation treatment.
Usual Dosage for Adults: The patient should set a date to stop smoking. CHANTIX dosing should start one week before this date.
The recommended dose of CHANTIX is 1 mg twice daily following a 1-week titration as follows (CHANTIX should be taken after eating and with a full glass of water.) :
Days 1 – 3: 0.5 mg once daily
Days 4 – 7: 0.5 mg twice daily
Day 8 through End of treatment: 1 mg twice daily

Patients who cannot tolerate adverse effects of CHANTIX may have the dose lowered temporarily or permanently. Patients should be treated with CHANTIX for 12 weeks. For patients who have successfully stopped smoking at the end of 12 weeks, an additional course of 12 weeks treatment with CHANTIX is recommended to further increase the likelihood of long-term abstinence.
Patients who do not succeed in stopping smoking during 12 weeks of initial therapy, or who relapse after treatment, should be encouraged to make another attempt once factors contributing to the failed attempt have been identified and addressed.

DOSING: RENAL IMPAIRMENT
CRCL  >/=30 mL/minute: No adjustment required.

CRCL <30 mL/minute: Initiate: 0.5 mg once daily; maximum dose: 0.5 mg twice daily.

Hemodialysis: Maximum dose: 0.5 mg once daily.


Supplied: 0.5mg, 1 mg tablet.

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.