Nalbuphine Hydrochloride

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Cat Number

API0232099

CAS Number

23277-43-2

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CAS Number

23277-43-2

EINECS

245-549-9

Storage

Store at room temperature

Synonyms

Nalbuphine HCL; EN-2234A; Nalbufine hydrochloride; Nalbufina clorhidrato; NSC-757829; ZU4275277R

Molecular Formula

C21H28ClNO4

Molecular Weight

393.9

Smiles

C1CC(C1)CN2CC[C@]34[C@@H]5[C@H](CC[C@]3([C@H]2CC6=C4C(=C(C=C6)O)O5)O)O.Cl

Appearance

White to off-white crystalline powder

Melting Point

230.5°C

Boiling Point

566.6°C at 760 mmHg

General Description

Nalbuphine hydrochloride is a semisynthetic opioid derivative of the phenanthrene series, structurally related to naloxone and oxymorphone. It has a cyclobutylmethyl substituent on the nitrogen atom, which confers mixed agonist‑antagonist properties. The molecule is a pure kappa‑opioid receptor agonist and a partial mu‑opioid receptor antagonist.

Mechanism of Action

Nalbuphine produces analgesia by activating kappa‑opioid receptors in the spinal cord and supraspinal sites, while its antagonist activity at mu receptors reduces the risk of respiratory depression, euphoria, and dependence.

Application

Nalbuphine is indicated for moderate to severe pain, including postoperative, obstetrical, and cancer pain. It is also used as an anesthetic adjunct and for reversal of mu‑agonist‑induced respiratory depression without completely abolishing analgesia. The drug has a favorable hemodynamic profile, causing minimal changes in heart rate or blood pressure, making it useful in cardiovascular surgery.

In a prospective randomized double‑blind trial, 69 patients undergoing lower limb orthopedic surgery received epidural bupivacaine with either nalbuphine 10 mg, dexmedetomidine 100 μg, or saline. Dexmedetomidine provided the fastest onset (12.2 min) and longest duration of postoperative analgesia (365.9 min), followed by nalbuphine (318.4 min) and control (241.3 min). Patient satisfaction was highest with dexmedetomidine, which also reduced top‑up analgesic requirements. Both adjuvants were effective, but dexmedetomidine was superior.

Fig. 1 Flow chart of patients in the study groups. (Farmawy MSE, et al., 2023)

References

Farmawy MSE, et al. Epidural nalbuphine versus dexmedetomidine as adjuvants to bupivacaine in lower limb orthopedic surgeries for postoperative analgesia: a randomized controlled trial. BMC Anesthesiol. 2023;23(1):401.

A Cochrane systematic review of 10 RCTs (658 children) found low‑quality evidence that nalbuphine reduces moderate/severe postoperative pain compared with placebo (RR 0.1 at 1 hour) and may reduce rescue analgesic requirements. Comparisons with morphine, tramadol, and pethidine were inconclusive due to wide confidence intervals. Postoperative nausea and vomiting did not differ significantly from placebo or morphine. The authors conclude that evidence is insufficient to definitively establish nalbuphine’s efficacy or superiority over other opioids in children.

Fig. 2 Comparison 1 Nalbuphine versus placebo, Outcome 1 Number of patients with moderate/severe pain (1h postop). (Schnabel A, et al., 2014)

References

Schnabel A, et al. Nalbuphine for postoperative pain treatment in children. Cochrane Database Syst Rev. 2014;2014(7):CD009583.

Does Nalbuphine Hydrochloride require protection from light during long-term storage?

Yes, it is photosensitive. Light exposure can cause discoloration and degradation. Store in light-resistant containers, preferably amber glass.

What is the recommended storage temperature for Nalbuphine Hydrochloride?

Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which can accelerate oxidation of the phenolic group.

Is Nalbuphine Hydrochloride stable in solution for injectable use?

Aqueous solutions are stable when protected from light and stored at room temperature for up to 24 hours.

How is the impurity nalbuphine pseudodimer (oxidative coupling product) monitored?

This degradation product is quantified using a stability-indicating HPLC method with electrochemical detection, ensuring it remains below pharmacopoeial limits.