Nalbuphine

Mechanism :

The exact mechanism of action is unknown but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor but may also be a result of other mechanisms. Nalbuphine is thought primarily to be a kappa agonist. It is also a partial mu antagonist analgesic, with some binding to the delta receptor and minimal agonist activity at the sigma receptor.

Indication :

• Treatment of moderate to severe pain

Contraindications :

Hypersensitivity, Abrupt withdrawal.

Caution in hepatic, renal or pulmonary disease.

Dosing :

Adverse Effect :

Common Reactions: sedation, clamminess, dizziness, headache, dysphoria, nausea, vomiting, xerostomia, diaphoresis, urticaria, pruritus.

Serious Reactions: respiratory depression, bradycardia, hypotension, anaphylaxis/anaphylactoid reaction, hypersensitivity reaction, shock, laryngeal edema, dependency, abuse, withdrawal seizures if abruptly discontinued after prolonged use.

Interaction :

Alvimopan: Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
Cimetidine: Increases the effect of the narcotic.
Triprolidine: The CNS depressants, Triprolidine and Nalbuphine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.

Hepatic Dose :