Nalbuphinum [INN-Latin] - General Information
A narcotic used as a pain medication. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors. [PubChem]
Pharmacology of Nalbuphinum [INN-Latin]
Nalbuphinum [INN-Latin] is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. Nalbuphinum [INN-Latin]'s analgesic potency is essentially equivalent to that of morphine on a milligram basis. The opioid antagonist activity of nalbuphine is one-fourth as potent as nalorphine and 10 times that of pentazocine. Nalbuphinum [INN-Latin] by itself has potent opioid antagonist activity at doses equal to or lower than its analgesic dose. When administered following or concurrent with mu agonist opioid analgesics (e.g., morphine, oxymorphone, fentanyl), nalbuphine may partially reverse or block opioid-induced respiratory depression from the mu agonist analgesic. Nalbuphinum [INN-Latin] may precipitate withdrawal in patients dependent on opioid drugs. Nalbuphinum [INN-Latin] should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis.
Nalbuphinum [INN-Latin] for patients
Patients should be advised of the following information:
- NUBAIN is associated with sedation and may impair mental and physical abilities required for the performance of potentially dangerous tasks such as driving a car or operating machinery.
- NUBAIN is to be used as prescribed by a physician. Dose or frequency should not be increased without first consulting with a physician since NUBAIN may cause psychological or physical dependence.
- The use of NUBAIN with other opioids can cause signs and symptoms of withdrawal.
- Abrupt discontinuation of NUBAIN after prolonged usage may cause signs and symptoms of withdrawal.
NUBAIN may interfere with enzymatic methods for the detection of opioids depending on the specificity/sensitivity of the test. Consult the test manufacturer for specific details.
Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis
Long term carcinogenicity studies were performed in rats (24 months) and mice (19 months) by oral administration at doses up to 200 mg/kg (1180 mg/m2) and 200 mg/kg (600 mg/m2) per day, respectively. There was no evidence of an increase in tumors in either species related to NUBAIN administration. The maximum recommended human dose (MRHD) in a day is 160 mg subcutaneously, intramuscularly or intravenously, or approximately 100 mg/m2/day for a 60 kg subject.
NUBAIN did not have mutagenic activity in the AMES test with four bacterial strains, in the Chinese Hamster Ovary HGPRT assays or in the Sister Chromatids Exchange Assay. However, NUBAIN induced an increased frequency of mutation in the mouse lymphoma assay. Clastogenic activity was not observed in the mouse micronucleus test of the cytogenicity bone marrow assay in rats.
Impairment of Fertility
A reproduction study was performed in male and female rats at subcutaneous doses up to 56 mg/kg/day or 330 mg/m2/day. NUBAIN did not affect either male or female fertility rats.
Usage in Pregnancy
Teratogenic Effects: Pregnancy Category B: Reproduction studies have been performed in rats by subcutaneous administration of nalbuphine up to 100 mg/kg/day, or 590 mg/m2/day which is approximately 6 times the MRHD, and in rabbits by intravenous administration of nalbuphine up to 32 mg/kg/day, or 378 mg/m2/day which is approximately 4 times the MRHD. The results did not reveal evidence of developmental toxicity, including teratogenicity, or harm to the fetus. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Non-teratogenic Effects: Neonatal body weight and survival rates were reduced at birth and during lactation when nalbuphine was subcutaneously administered to female and male rats prior to mating and throughout gestation and lactation or to pregnant rats during the last third of gestation and throughout lactation at doses approximately 4 times the maximum recommended human dose.
Use During Labor and Delivery.
Limited data suggest that NUBAIN is excreted in maternal milk but only in a small amount (less than 1% of the administered dose) and with a clinically insignificant effect. Caution should be exercised when NUBAIN is administered to a nursing woman.
Safety and effectiveness in pediatric patients below the age of 18 years have not been established.
Nalbuphinum [INN-Latin] Interactions
No specific information available.
Nalbuphinum [INN-Latin] Contraindications
NUBAIN should not be administered to patients who are hypersensitive to nalbuphine hydrochloride, or to any of the other ingredients in NUBAIN.
Additional information about Nalbuphinum [INN-Latin]
Nalbuphinum [INN-Latin] Indication: For the relief of moderate to severe pain.
Mechanism Of Action: Receptor studies show that nalbuphine exerts its action via binding to mu, kappa, and delta receptors, but not to sigma receptors. Nalbuphinum [INN-Latin] is primarily a kappa agonist/partial mu antagonist analgesic.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Nalbuphine
Synonyms: Not Available
Drug Category: Analgesics, Opioid; Narcotic Antagonists; Narcotics
Drug Type: Small Molecule; Approved
Other Brand Names containing Nalbuphine: Nalbufina [DCIT]; Nalbuphine HCL; Nalbuphinum [INN-Latin]; Nubain;
Absorption: The mean absolute bioavailability was 81% and 83% for the 10 and 20 mg intramuscular doses, respectively, and 79% and 76% following 10 and 20 mg of subcutaneous nalbuphine.
Toxicity (Overdose): ORAL (LD50): Acute: 1100 mg/kg [Dog]. Symptoms of overdose include primarily sleepiness and mild dysphoria.
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: The plasma half-life of nalbuphine is 5 hours, and in clinical studies the duration of analgesic activity has been reported to range from 3 to 6 hours.
Dosage Forms of Nalbuphinum [INN-Latin]: Solution Intravenous
Chemical IUPAC Name: Not Available
Chemical Formula: C21H27NO4
Nalbuphine on Wikipedia: https://en.wikipedia.org/wiki/Nalbuphine
Organisms Affected: Humans and other mammals