Naltrexone HCL

Chemical Name: Naltrexone Hydrochloride

Synonyms: N-cyclopropyl methyl-14-hydroxy dihydro normorphine 7,8-dihydrochloride, (-)-Naltrexone hydrochloride

Appearance: White to off-white crystalline powder

Melting Point: 278-280 °C

Solubility:

* Water: Slightly soluble (1 in 2000)

* Ethanol: Freely soluble (1 in 5)

* Chloroform: Freely soluble (1 in 5)

* pH: 4.5-6.5

Stability: Stable for 24 months when stored as recommended (room temperature, 15-25°C, in a tightly closed container protected from light)

Storage: Store at room temperature (15-25°C) in a tightly closed container protected from light.

Mechanism of Action:

• Naltrexone HCl is a competitive opioid antagonist. It binds to the mu-opioid receptors in the central nervous system, preventing other opioids from binding and producing their effects. This can help to reduce cravings and prevent relapse in people with opioid use disorder.
• Naltrexone HCl also activates the kappa-opioid receptor system, which may contribute to its effects on reducing cravings and reward-seeking behavior.

Pharmacokinetics:

• Peak plasma concentration: 1-2 hours after oral administration
• Bioavailability: 50-60%
• Half-life: 4-11 hours
• Metabolism: Extensively metabolized in the liver to inactive metabolites
• Excretion: Primarily in the feces, with a small amount excreted in the urine

Uses:

• Naltrexone HCl is used to treat opioid use disorder, including both prescription opioid dependence and heroin addiction. It is available as a tablet, injectable implant, and extended-release injectable formulation.
• It is also used to reduce the risk of alcohol relapse in people with alcohol dependence.

Contraindications:

• Naltrexone HCl is contraindicated in people who are allergic to it or who have acute opioid intoxication.
• It should be used with caution in people with liver or kidney problems, pregnant or breastfeeding women, and people taking other medications that can cause respiratory depression.

Warnings and Precautions:

• Naltrexone HCl can precipitate withdrawal symptoms in people who are physically dependent on opioids. It is important to start treatment with a low dose and gradually increase it to avoid this.
• Naltrexone HCl can also cause other side effects, such as nausea, vomiting, abdominal pain, headache, and fatigue. These side effects are usually mild and go away on their own.

Disclaimer: This information is intended for educational purposes only and should not be construed as medical advice. Please consult your doctor or pharmacist for more information about Naltrexone HCl and whether it is right for you.