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Wedgewood compounds 1.4gm Naltrexone pellets Naltrexone is rapidly absorbed, with peak blood levels achieved approximately one hour following oral administration.[9] It is primarily metabolized by the liver, and converted to 6-β-naltrexol, which has a plasma half life of 10 hours. Approximately 20 percent of the active metabolite is bound to plasma protein and distributed widely, with relatively high amounts found in the brain, fat, spleen, heart, testes, kidney and urine.[9] Naltrexone and its metabolite 6-β-naltrexol, with less than 1 percent of naltrexone, are excreted unchanged. Despite the relatively short half lives of both compounds, the duration of naltrexone blockade is much longer. Typically, an oral dose of 50mg naltrexone as been shown to produce 80 percent inhibition of radiolabeled carfentanyl binding for 72 hours.[10] In alcohol dependence, naltrexone is considered a safe medication. Control
of liver values prior to initiation of treatment is recommended. There
has been some controversy regarding the use of opioid-receptor antagonists,
such as naltrexone, in the long-term management of opioid dependence due
to the effect of these agents in sensitizing opioid receptors. Following
therapy, the opioid receptors continue to have increased sensitivity for
a period during which the patient is at increased risk of opioid overdose.
This effect reinforces the necessity of monitoring of therapy and provision
of patient support measures by medical practitioners. References
The information contained on this site is general in nature and is intended for use as an informational aid. It does not cover all possible uses, actions, precautions, side effects, or interactions of the products shown, nor is the information intended as medical advice or diagnosis for individual health problems or for making an evaluation as to the risks and benefits of using a particular product. You should consult your doctor about diagnosis and treatment of any health problems. Information and statements have not been evaluated by the Food and Drug Administration ("FDA"), nor has the FDA approved the products to diagnose, cure or prevent disease. Compound Medications | Veterinary Medicine | Compounding Pharmacy Wedgewood
Pharmacy |
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Naltrexone
is an opiate antagonist that reduces the euphoric effect of opiates and
alcohol. It was approved by the FDA in 1984 for the treatment of opiate
addiction, in 1994 for the treatment of alcoholism and in 2006 as a depot
injectable. Naltrexone and its active metabolite, 6-β-naltrexol,
are inverse agonists of µ-and κ-opiod receptors, and to a
lesser extent at δ-opioid receptors.
