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Naltrexone

$6.69 USD
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Naltrexone hydrochloride is a pure opioid antagonist. It markedly attenuates or completely blocks, reversibly, the subjective effects of intravenously administered opioids.
8.95$. Delivery period 14-21 days.
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27.95$. Delivery period 5-7 days.
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Naltrexone 50 mg

Name Quantity Price Each Total Price Save
Naltrexone 50 mg 10 pills $8.81 USD $88.10 USD
Naltrexone 50 mg 20 pills $7.62 USD $152.40 USD
+ Bonus - 12 pills
$23.80 USD
Naltrexone 50 mg 30 pills $7.22 USD $216.60 USD
+ Bonus - 12 pills
Free AirMail Delivery
$47.70 USD
Naltrexone 50 mg 60 pills $6.83 USD $409.80 USD
+ Bonus - 12 pills
Free Courier Delivery.
$118.80 USD
Naltrexone 50 mg 90 pills $6.69 USD $602.10 USD
+ Bonus - 12 pills
Free Courier Delivery.
$190.80 USD
  • Product overview

Naltrexone - Clinical Pharmacology

Pharmacodynamic Actions

Naltrexone hydrochloride is a pure opioid antagonist. It markedly attenuates or completely blocks, reversibly, the subjective effects of intravenously administered opioids.

When coadministered with morphine, on a chronic basis, Naltrexone hydrochloride blocks the physical dependence to morphine, heroin and other opioids.

Naltrexone hydrochloride has few, if any, intrinsic actions besides its opioid blocking properties. However, it does produce some pupillary constriction, by an unknown mechanism.

The administration of Naltrexone hydrochloride is not associated with the development of tolerance or dependence. In subjects physically dependent on opioids, Naltrexone hydrochloride will precipitate withdrawal symptomatology.

Clinical studies indicate that 50 mg of Naltrexone hydrochloride will block the pharmacologic effects of 25 mg of intravenously administered heroin for periods as long as 24 hours. Other data suggest that doubling the dose of Naltrexone hydrochloride provides blockade for 48 hours, and tripling the dose of Naltrexone hydrochloride provides blockade for about 72 hours.

Naltrexone hydrochloride blocks the effects of opioids by competitive binding (i.e., analogous to competitive inhibition of enzymes) at opioid receptors. This makes the blockade produced potentially surmountable, but overcoming full Naltrexone blockade by administration of very high doses of opiates has resulted in excessive symptoms of histamine release in experimental subjects.

The mechanism of action of Naltrexone hydrochloride in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone hydrochloride, an opioid receptor antagonist, competitively binds to such receptors and may block the effects of endogenous opioids. Opioid antagonists have been shown to reduce alcohol consumption by animals, and Naltrexone hydrochloride has been shown to reduce alcohol consumption in clinical studies.

Naltrexone hydrochloride is not aversive therapy and does not cause a disulfiram-like reaction either as a result of opiate use or ethanol ingestion.

Pharmacokinetics

Naltrexone hydrochloride is a pure opioid receptor antagonist. Although well absorbed orally, Naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%. The activity of Naltrexone is believed to be due to both parent and the 6-ß-naltrexol metabolite. Both parent drug and metabolites are excreted primarily by the kidney (53% to 79% of the dose), however, urinary excretion of unchanged Naltrexone accounts for less than 2% of an oral dose and fecal excretion is a minor elimination pathway. The mean elimination half-life (T-1/2) values for Naltrexone and 6-ß-naltrexol are 4 hours and 13 hours, respectively. Naltrexone and 6-ß-naltrexol are dose proportional in terms of AUC and Cmax over the range of 50 to 200 mg and do not accumulate after 100 mg daily doses.

 

Absorption

Following oral administration, Naltrexone undergoes rapid and nearly complete absorption with approximately 96% of the dose absorbed from the gastrointestinal tract. Peak plasma levels of both Naltrexone and 6-ß-naltrexol occur within one hour of dosing.

Distribution

The volume of distribution for Naltrexone following intravenous administration is estimated to be 1350 liters. In vitro tests with human plasma show Naltrexone to be 21% bound to plasma proteins over the therapeutic dose range.

Metabolism

The systemic clearance (after intravenous administration) of Naltrexone is ~ 3.5 L/min, which exceeds liver blood flow (~ 1.2 L/min). This suggests both that Naltrexone is a highly extracted drug (>98% metabolized) and that extra-hepatic sites of drug metabolism exist. The major metabolite of Naltrexone is 6-ß-naltrexol. Two other minor metabolites are 2-hydroxy-3-methoxy-6-ß-naltrexol and 2-hydroxy-3-methyl-Naltrexone. Naltrexone and its metabolites are also conjugated to form additional metabolic products.

Elimination

The renal clearance for Naltrexone ranges from 30 to 127 mL/min and suggests that renal elimination is primarily by glomerular filtration. In comparison the renal clearance for 6-ß-naltrexol ranges from 230 to 369 mL/min, suggesting an additional renal tubular secretory mechanism. The urinary excretion of unchanged Naltrexone accounts for less than 2% of an oral dose; urinary excretion of unchanged and conjugated 6-ß-naltrexol accounts for 43% of an oral dose. The pharmacokinetic profile of Naltrexone suggests that Naltrexone and its metabolites may undergo enterohepatic recycling.

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