Naloxone Hcl (naloxone HCl)

Naloxone is commercially available as naloxone hydrochloride; dosage is expressed in terms of the salt.

Naloxone may be administered by IV, subcutaneous, or IM injection; by IV infusion; or intranasally. The drug also has been administered via endotracheal tube+ and by intraosseous+ (IO) injection.

Naloxone is metabolized in the liver primarily by glucuronide conjugation.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

*Patients with known hypersensitivity to the drug or any ingredient in the formulation.

There are no contraindication contraindications for this drug.

• Opioid withdrawal symptoms

• Opioid dependence
• Tachyarrhythmia

Intranasal naloxone: Adverse effects reported in clinical trials of intranasally administered naloxone include abdominal pain, asthenia, dizziness, headache, increased blood pressure, constipation, toothache, muscle spasms, musculoskeletal pain, nasal congestion, nasal discomfort, nasal dryness, nasal edema, nasal inflammation, presyncope, rhinalgia, and xeroderma.

Parenteral naloxone: Adverse effects, including serious and fatal cases, reported in clinical trials of parenterally administered naloxone for postoperative patients include cardiac arrest, dyspnea, hypotension, hypertension, pulmonary edema, and ventricular tachycardia and fibrillation. Excessive doses of naloxone in postoperative patients may result in agitation caused by significant reversal of analgesia. Adverse effects reported in clinical trials of parenterally administered naloxone after abrupt reversal of dependence are related to acute withdrawal syndrome, which may include the following signs and symptoms: abdominal cramps, body aches, diarrhea, fever, increased blood pressure, nausea or vomiting, nervousness, runny nose, piloerection, restlessness or irritability, shivering or trembling, sneezing, sweating, tachycardia, weakness, yawning. Abrupt reversal of opioid depression may result in cardiac arrest, increased blood pressure, nausea, pulmonary edema, seizures, sweating, tachycardia, tremulousness, ventricular tachycardia and fibrillation, and vomiting. In the neonate, opioid withdrawal may also include convulsions, excessive crying, and hyperactive reflexes. Adverse effects reported in clinical trials of naloxone hydrochloride injection for IM or subcutaneous use (Zimhi(R)) included dizziness, elevated bilirubin, lightheadedness, and nausea.

More Frequent

• Hypertension

Less Frequent

• Dyspnea
• Hypotension
• Ventricular fibrillation
• Ventricular tachycardia

Rare or Very Rare

• Cardiac arrest
• General weakness
• Opioid withdrawal symptoms
• Pulmonary edema

More Frequent

• Dry nose
• Headache disorder
• Musculoskeletal pain
• Nasal congestion
• Nasal mucosa edematous
• Oral paresthesia

Less Frequent

• Acute abdominal pain
• Constipation
• Dizziness
• Hyperhidrosis
• Irritability
• Muscle spasm
• Nausea
• Presyncope
• Toothache
• Vomiting

Rare or Very Rare

• Dry skin

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Naloxone hydrochloride injection may be used to reverse the effects of opioids in pediatric patients, including neonates. In addition, safety and efficacy of naloxone hydrochloride prefilled syringes for IM or subcutaneous use (Zimhi(R)) or nasal spray (e.g., Narcan(R), Kloxxado(R)) have been established in pediatric patients of all ages for the emergency treatment of known or suspected opioid overdosage manifested by respiratory and/or CNS depression. Use of naloxone for reversal of opioid effects in pediatric patients is supported by adult bioequivalence studies and evidence from the safe and effective use of other naloxone hydrochloride products.

As in adults, naloxone may precipitate opiate withdrawal in pediatric patients who are physically dependent on opiates; however, unlike opiate withdrawal in adults, neonatal opiate withdrawal may be life-threatening and should be treated according to protocols developed by neonatology experts. To avoid abrupt precipitation of neonatal opiate withdrawal syndrome, use of a naloxone preparation that can be dosed based on weight and titrated to effect may be preferred over a preparation that delivers a fixed dose of the drug (e.g., auto-injector, nasal spray) in neonates with known or suspected exposure to maternally administered opiates.

Absorption of naloxone following intranasal administration or IM or subcutaneous injection in pediatric patients may be erratic or delayed. Pediatric patients who have responded to naloxone must be carefully monitored for at least 24 hours, since relapse may occur as the opioid antagonist is metabolized.

Safety and efficacy of naloxone hydrochloride injection in the management of hypotension associated with septic shock have not been established in pediatric patients. In a study of 2 neonates with septic shock, treatment with naloxone produced a positive pressor response; however, one patient subsequently died after intractable seizures.

There are limited data to date on use of naloxone in pregnant women. Naloxone should be used during pregnancy only when clearly needed. Reproduction studies in mice and rats using naloxone hydrochloride dosages of 4 and 8 times, respectively, a human dosage of 10 mg daily in a 50-kg individual demonstrated no embryotoxic or teratogenic effects. Furthermore, no adverse effects were reported in the offspring of rats receiving naloxone hydrochloride subcutaneously at dosages of 2 or 10 mg/kg (up to 12 times a human dosage of 8 mg daily) from gestation day 15 to postnatal day 21. No embryotoxic or teratogenic effects were observed in mice and rats during the period of organogenesis with the 8 mg/0.1 mL nasal spray at doses 3 and 6 times a human dose of 16 mg.

The risk-benefit ratio must be considered before naloxone is administered to a pregnant woman who is known or suspected to be dependent on opioids, since maternal dependence may often be accompanied by fetal dependence. Naloxone crosses the placenta and may precipitate withdrawal symptoms in both the fetus and the pregnant woman. Use of naloxone in opioid-dependent pregnant women should be accompanied by monitoring for fetal distress.

It is not known if naloxone affects the duration of labor and/or delivery. However, published reports indicate that administration of naloxone during labor did not adversely affect maternal or neonatal status. Carefully monitor patients with mild to moderate hypertension who receive naloxone during labor, as severe hypertension may occur.

It is not known whether naloxone is distributed into milk or has any effect on the breast-fed infant or on milk production; use naloxone with caution in nursing women. The drug does not affect prolactin or oxytocin concentrations in nursing women, and oral bioavailability of naloxone is minimal.

The manufacturers recommend using caution when selecting a dose of naloxone for geriatric patients.

Clinical studies of naloxone did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients. While other clinical experience has not revealed age-related differences in response, drug dosage generally should be titrated carefully in geriatric patients, usually initiating therapy at the low end of the dosage range. The greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly also should be considered.