Nurses Compass
Drug Guide
Naloxone Hydrochloride and Pentazocine Hydrochloride
Classification
Therapeutic: Opioid antagonist and opioid analgesic combination
Pharmacological: Naloxone as an opioid antagonist; Pentazocine as a partial opioid agonist
FDA Approved Indications
- Treatment of opioid overdose
- Preoperative analgesia in some cases
Mechanism of Action
Naloxone competitively binds to opioid receptors, displacing opioids and reversing their effects. Pentazocine binds primarily to kappa and mu opioid receptors, providing analgesia while partially blocking mu receptors to reduce abuse potential.
Dosage and Administration
Adult: Typically, 0.4 mg to 2 mg IV/IM/Subcutaneously every 2-3 minutes as needed; maximum dose usually 10 mg.
Pediatric: Dosage based on weight and clinical condition; consult current guidelines.
Geriatric: Adjust dose for renal and hepatic function; generally start at lower end of dosing.
Renal Impairment: Use with caution; may prolong effects.
Hepatic Impairment: Use with caution; dose adjustments may be necessary.
Pharmacokinetics
Absorption: Rapid IV absorption; variable IM and subcutaneous absorption.
Distribution: Wide distribution including into the CNS.
Metabolism: Hepatic metabolism for pentazocine; naloxone undergoes extensive first-pass hepatic metabolism.
Excretion: Renal excretion of metabolites.
Half Life: Naloxone approximately 30-120 minutes; pentazocine approximately 2-3 hours.
Contraindications
- Hypersensitivity to components
- Use caution in opioid-dependent patients due to withdrawal risk.
Precautions
- Monitor respiratory status closely during use.
- Potential for precipitating withdrawal in opioid-dependent individuals.
Adverse Reactions - Common
- Nausea (Common)
- Vomiting (Common)
- Sweating (Common)
- Tachycardia (Common)
Adverse Reactions - Serious
- Precipitation of withdrawal symptoms (Uncommon)
- Cardiac arrhythmias (Rare)
Drug-Drug Interactions
- Other CNS depressants, benzodiazepines, other opioids.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor respirations, blood pressure, heart rate, and level of consciousness.
Diagnoses:
- Potential ineffective breathing pattern.
- Acute pain.
Implementation: Administer as prescribed; be prepared for repeated doses in high-dose overdoses.
Evaluation: Assess for reversal of respiratory and CNS depression, and relief from pain.
Patient/Family Teaching
- Instruct on signs of overdose and the importance of seeking emergency care.
- Warn about precipitating withdrawal symptoms.
- Advise that naloxone may need to be administered multiple times.
Special Considerations
Black Box Warnings:
- Risk of opioid withdrawal symptoms, including severe reactions.
Genetic Factors: None specified.
Lab Test Interference: None known.
Overdose Management
Signs/Symptoms: Rapid onset of withdrawal, increased blood pressure, sweating, nausea, vomiting, tremors, seizures, or cardiac arrest.
Treatment: Supportive care, airway management, intravenous fluids, and IV vasopressors if needed; administration of additional doses of naloxone.
Storage and Handling
Storage: Store at room temperature, away from heat and light.
Stability: Stable under recommended storage conditions.