revex- nalmefene hydrochloride injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

nalmefene hydrochloride (UNII: K7K69QC05X) (nalmefene - UNII:TOV02TDP9I)

Available from:

Baxter Healthcare Corporation

INN (International Name):

nalmefene hydrochloride

Pharmaceutical form:

INJECTION, SOLUTION

Composition:

1 mg in 1 mL

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

REVEX is indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. REVEX is indicated in the management of known or suspected opioid overdose. REVEX is contraindicated in patients with a known hypersensitivity to the product. REVEX is an opioid antagonist with no agonist activity. It has no demonstrated abuse potential, is not addictive, and is not a controlled substance.

Product summary:

REVEX (nalmefene hydrochloride injection) is available in the following presentations: An ampul containing 1 mL of 100 µg/mL nalmefene base (Blue Label) Box of 10 (NDC 10019-315-21) An ampul containing 2 mL of 1 mg/mL nalmefene base (Green Label) Box of 10 (NDC 10019-311-22) Store at controlled room temperature. REVEX is a registered trademark of Ivax Laboratories, Inc. Baxter is a registered trademark of Baxter International Inc. Manufactured for Baxter Healthcare Corporation Deerfield, IL 60015 USA by: Taylor Pharmaceuticals Decatur, IL 62525 For Product Inquiry 1 800 ANA DRUG (1-800-262-3784) U.S. Patent No. 4,535,157 June 2006

Summary of Product characteristics

REVEX- NALMEFENE HYDROCHLORIDE INJECTION, SOLUTION
BAXTER HEALTHCARE CORPORATION
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REVEX (NALMEFENE HYDROCHLORIDE INJECTION)
RX ONLY
DESCRIPTION
REVEX (nalmefene hydrochloride injection), an opioid antagonist, is a
6-methylene analogue of
naltrexone. The chemical structure is shown below:
Molecular Formula: C
H NO •HCl
Molecular Weight: 375.9, CAS # 58895-64-0
Chemical Name:
17-(Cyclopropylmethyl)-4,5α-epoxy-6-methylenemorphinan-3,14-diol,
hydrochloride
salt.
Nalmefene hydrochloride is a white to off-white crystalline powder
which is freely soluble in water up
to 130 mg/mL and slightly soluble in chloroform up to 0.13 mg/mL, with
a pK
of 7.6.
REVEX is available as a sterile solution for intravenous,
intramuscular, and subcutaneous administration
in two concentrations, containing 100 µg or 1.0 mg of nalmefene free
base per mL. The 100 µg/mL
concentration contains 110.8 µg of nalmefene hydrochloride and the
1.0 mg/mL concentration contains
1.108 mg of nalmefene hydrochloride per mL. Both concentrations
contain 9.0 mg of sodium chloride
per mL and the pH is adjusted to 3.9 with hydrochloric acid.
Concentrations and dosages of REVEX are expressed as the free base
equivalent of nalmefene.
CLINICAL PHARMACOLOGY
PHARMACODYNAMICS
REVEX prevents or reverses the effects of opioids, including
respiratory depression, sedation, and
hypotension. Pharmacodynamic studies have shown that REVEX has a
longer duration of action than
naloxone at fully reversing doses. REVEX has no opioid agonist
activity.
REVEX is not known to produce respiratory depression, psychotomimetic
effects, or pupillary
constriction. No pharmacological activity was observed when REVEX was
administered in the absence
of opioid agonists.
REVEX has not been shown to produce tolerance, physical dependence, or
abuse potential.
REVEX can produce acute withdrawal symptoms in individuals who are
opioid dependent.
PHARMACOKINETICS
Nalmefene exhibited dose proportional pharmacokinetics following
intravenous administration of 0.5
mg to 2.0 mg. Pharmacoki