99% Long Acting Narcotic Antagonist Drug Raw Powder Naltrexone Hydrochloride CAS 16676-29-2

Naltrexone Hydrochloride

Basic Details

Product Name: Naltrexone Hydrochloride
Synonyms: 17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy-morphinan-6-onehydroch;17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy-morphinan-6-onhydr;17-(cyclopropylmethyl)-4,5-alpha-oxy-3,14-dihydoxy-morphinan-6-onhydrochlo;17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-morphinan-6-onhydrochlor;en1639a;n-cyclopropylmethyl-noroxymorphonehydrochloride;nih8503;N-CYCLOPROPYLMETHYL-14-HYDROXYDI-HYDROMORPHINONE HYDROCHLORIDE
CAS: 16676-29-2
MF: C20H24ClNO4
MW: 377.86
EINECS: 240-723-0

Chemical Properties
Melting point 274-276°C
storage temp. 2-8°C
solubility H2O: 50 mg/mL, clear, colorless
form neat
Water Solubility Soluble in water at 50mg/ml.
Sensitive Light Sensitive
Merck 13,6389
BRN 3580333

Usage And Synthesis
Description Naltrexone hydrochloride is a potent, long-acting, orally-effective narcotic antagonist useful in the management of narcotic addiction.
Chemical Properties White Crystalline Powder
Originator Endo (USA)
Uses Nonselective opioid receptor antagonist; congener of naloxone
Uses Analgesic;Opioid antagonist
Uses sulfonamide, carbonic anhydrase inhibitor, anti-glaucoma agent
Uses Narcotic antagonist, In treatment of alcoholism
Biological Activity Opioid antagonist.
Purification Methods This narcotic antagonist has been purified by recrystallisation from MeOH and dried in air. The free base has m 168-170o after recrystallisation from Me2CO.

home drugs a-z list side effects drug center naltrexone hydrochloride tablets (naltrexone hydrochloride) drug
Privacy & Trust Info
Drug Description
RxList
Take the Pain Quiz

Back Pain:Myths and Facts About Back Pain
Back Pain Slideshow: Myths and Facts

Chronic Pain: Causes, Solutions and Management
Chronic Pain Slideshow

NALTREXONE HYDROCHLORIDE
(naltrexone hydrochloride) 50 mg Film Coated Tablets

DESCRIPTION

Naltrexone Hydrochloride Tablets USP, an opioid antagonist, are a synthetic congener of oxymorphone with no opioid agonist properties. Naltrexone differs in structure from oxymorphone in that the methyl group on the nitrogen atom is replaced by a cyclopropylmethyl group. Naltrexone Hydrochloride Tablets USP are also related to the potent opioid antagonist, naloxone, or n-allylnoroxymorphone. The chemical name for naltrexone hydrochloride is Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy- 3,14-dihydroxy-, hydrochloride, (5α)-.

Naltrexone hydrochloride - Structural Formula Illustration
C20H23NO4•HCl M.W. 377.86

Naltrexone Hydrochloride Tablets USP are a white, crystalline compound. The hydrochloride salt is soluble in water to the extent of about 100 mg/mL. Naltrexone Hydrochloride Tablets USP are available in scored film-coated tablets containing 50 mg of naltrexone hydrochloride. Naltrexone Hydrochloride Tablets USP also contain: colloidal silicon dioxide, crospovidone, hydroxypropyl methylcellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, red iron oxide, yellow iron oxide and titanium dioxide.

Indications & Dosage
RxList
Take the Pain Quiz

Back Pain:Myths and Facts About Back Pain
Back Pain Slideshow: Myths and Facts

Chronic Pain: Causes, Solutions and Management
Chronic Pain Slideshow

INDICATIONS

Naltrexone Hydrochloride Tablets USP are indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids.

Naltrexone Hydrochloride Tablets USP have not been shown to provide any therapeutic benefit except as part of an appropriate plan of management for the addictions.

DOSAGE AND ADMINISTRATION

To reduce the risk of precipitated withdrawal in patients dependent on opioids, or exacerbation of a preexisting subclinical withdrawal syndrome, opioid-dependent patients, including those being treated for alcohol dependence, should be opioid-free (including tramadol) before starting naltrexone hydrochloride tablets treatment. An opioid-free interval of a minimum of 7 to 10 days is recommended for patients previously dependent on short-acting opioids.

Switching From Buprenorphine, Buprenorphine/Naloxone, Or Methadone

There are no systematically collected data that specifically address the switch from buprenorphine or methadone to naltrexone hydrochloride tablets; however, review of postmarketing case reports have indicated that some patients may experience severe manifestations of precipitated withdrawal when being switched from opioid agonist therapy to opioid antagonist therapy (see WARNINGS). Patients transitioning from buprenorphine or methadone may be vulnerable to precipitation of withdrawal symptoms for as long as 2 weeks. Healthcare providers should be prepared to manage withdrawal symptomatically with non-opioid medications.

Treatment Of Alcoholism

A dose of 50 mg once daily is recommended for most patients. The placebo-controlled studies that demonstrated the efficacy of naltrexone hydrochloride tablets as an adjunctive treatment of alcoholism used a dose regimen of naltrexone hydrochloride tablets 50 mg once daily for up to 12 weeks. Other dose regimens or durations of therapy were not evaluated in these trials.

Naltrexone hydrochloride tablets should be considered as only one of many factors determining the success of treatment of alcoholism. Factors associated with a good outcome in the clinical trials with naltrexone hydrochloride tablets were the type, intensity, and duration of treatment; appropriate management of comorbid conditions; use of community-based support groups; and good medication compliance. To achieve the best possible treatment outcome, appropriate compliance-enhancing techniques should be implemented for all components of the treatment program, especially medication compliance.

Treatment Of Opioid Dependence

Treatment should be initiated with an initial dose of 25 mg of naltrexone hydrochloride tablets. If no withdrawal signs occur, the patient may be started on 50 mg a day thereafter.

A dose of 50 mg once a day will produce adequate clinical blockade of the actions of parenterally administered opioids. As with many non-agonist treatments for addiction, naltrexone hydrochloride tablets are of proven value only when given as part of a comprehensive plan of management that includes some measure to ensure the patient takes the medication.

Naloxone Challenge Test

Clinicians are reminded that there is no completely reliable method for determining whether a patient has had an adequate opioid-free period. A naloxone challenge test may be helpful if there is any question of occult opioid dependence. If signs of opioid withdrawal are still observed following naloxone challenge, treatment with naltrexone hydrochloride tablets should not be attempted. The naloxone challenge can be repeated in 24 hours.

The naloxone challenge test should not be performed in a patient showing clinical signs or symptoms of opioid withdrawal, or in a patient whose urine contains opioids. The naloxone challenge test may be administered by either the intravenous or subcutaneous routes.

Intravenous

Inject 0.2 mg naloxone.

Observe for 30 seconds for signs or symptoms of withdrawal.

If no evidence of withdrawal, inject 0.6 mg of naloxone.

Observe for an additional 20 minutes.

Subcutaneous

Administer 0.8 mg naloxone.

Observe for 20 minutes for signs or symptoms of withdrawal.

Note: Individual patients, especially those with opioid dependence, may respond to lower doses of naloxone. In some cases, 0.1 mg IV naloxone has produced a diagnostic response.

Interpretation Of The Challenge

Monitor vital signs and observe the patient for signs and symptoms of opioid withdrawal. These may include, but are not limited to: nausea, vomiting, dysphoria, yawning, sweating, tearing, rhinorrhea, stuffy nose, craving for opioids, poor appetite, abdominal cramps, sense of fear, skin erythema, disrupted sleep patterns, fidgeting, uneasiness, poor ability to focus, mental lapses, muscle aches or cramps, pupillary dilation, piloerection, fever, changes in blood pressure, pulse or temperature, anxiety, depression, irritability, backache, bone or joint pains, tremors, sensations of skin crawling or fasciculations. If signs or symptoms of withdrawal appear, the test is positive and no additional naloxone should be administered.

Warning

If the test is positive, do NOT initiate naltrexone hydrochloride tablets therapy.

Repeat the challenge in 24 hours. If the test is negative, naltrexone hydrochloride tablets therapy may be started if no other contraindications are present. If there is any doubt about the result of the test, hold naltrexone hydrochloride tablets and repeat the challenge in 24 hours.

Alternative Dosing Schedules

A flexible approach to a dosing regimen may need to be employed in cases of supervised administration. Thus, patients may receive 50 mg of naltrexone hydrochloride tablets every weekday with a 100 mg dose on Saturday, 100 mg every other day, or 150 mg every third day. The degree of blockade produced by naltrexone hydrochloride tablets may be reduced by these extended dosing intervals.

There may be a higher risk of hepatocellular injury with single doses above 50 mg, and use of higher doses and extended dosing intervals should balance the possible risks against the probable benefits (see WARNINGS).

Patient Compliance

Naltrexone hydrochloride tablets should be considered as only one of many factors determining the success of treatment. To achieve the best possible treatment outcome, appropriate complianceenhancing techniques should be implemented for all components of the treatment program, including medication compliance.