Pharmacology of Nalmefene Hydrochloride Mechanism of action Pharmacokinetics Uses Effects

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Nalmefene hydrochloride is an opioid antagonist used to reverse opioid overdoses and reduce alcohol consumption in adults with alcohol dependence. Here are some key points about its pharmacology: • Mechanism of Action: Nalmefene acts as an antagonist at the μ-opioid receptors (MOR) and δ-opioid receptors (DOR), and as a partial agonist at the κ-opioid receptors (KOR). This helps to reverse the effects of opioids and reduce cravings1. • Formulations: It is available as an intravenous (IV) injection and a nasal spray. The IV form is used for immediate reversal of opioid overdose, while the nasal spray provides a more accessible option for emergency use1. • Dosage: The typical dose for opioid overdose is 0.5-1 mg IV or 2 mg nasal spray, with additional doses administered if needed2. • Metabolism: Nalmefene is metabolized in the liver and has a longer duration of action compared to naloxone, making it effective for sustained reversal of opioid effects. • Adverse Effects: Common side effects include dizziness, headache, nausea, and vomiting. It can also precipitate withdrawal symptoms in opioid-dependent individuals1. • Clinical Uses: Besides treating opioid overdoses, nalmefene is used to reduce alcohol consumption in adults with alcohol dependence. It is often prescribed alongside psychosocial support to help patients reduce their drinking • #Nalmefene

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