Nalbuphine

Nalbuphine Uses, Dosage, Side Effects, Food Interaction and all others data.

Nalbuphine Hydrochloride is a synthetic potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis. Receptor studies show that Nalbuphine binds to mu, kappa, and delta receptors, but not to sigma receptors. Nalbuphine is primarily a kappa agonist/partial mu antagonist analgesic.

Nalbuphine is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. Nalbuphine's analgesic potency is essentially equivalent to that of morphine on a milligram basis. The opoioid antagonist activity of nalbuphine is about one-fourth to that of nalorphine and 10 times to that of pentazocine. Nalbuphine 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. Nalbuphine may precipitate withdrawal in patients dependent on opioid drugs. Nalbuphine should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis.

Trade Name Nalbuphine
Availability Prescription only
Generic Nalbuphine
Nalbuphine Other Names Nalbufina, Nalbuphin, Nalbuphine, Nalbuphinum
Related Drugs Buprenex, aspirin, acetaminophen, tramadol, naproxen, Tylenol, oxycodone, fentanyl, lidocaine, ketamine
Weight 10mg/ml, 20mg/ml,
Type Injection, Injectable Solution
Formula C21H27NO4
Weight Average: 357.4434
Monoisotopic: 357.194008357
Protein binding

Not appreciably bound.

Groups Approved
Therapeutic Class Opioid analgesics
Manufacturer Dosaco Laboratories
Available Country Pakistan, United States,
Last Updated: September 19, 2023 at 7:00 am
Nalbuphine
Nalbuphine

Uses

Nalbuphine Hydrochloride is a synthetic opioid analgesic, which binds with mu, kappa and delta receptor. Its analgesic potency is equivalent to Morphine on a milligram basis and 10 times more than that of Pentazocine but has lower side effects and less abuse potential than Morphine. The onset of action of Nalbuphine occurs within 2 to 3 minutes after intravenous administration and in less than 15 minutes following intramuscular injection. The plasma half-life of Nalbuphine is 5 hours and the duration of analgesic activity is 3 to 6 hours.

Nalbuphine Hydrochloride is used for the relief of moderate to severe pain. It is used for relief of moderate to severe pain associated with myocardial infarction (MI). Nalbuphine Hydrochloride can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery.

Nalbuphine is also used to associated treatment for these conditions: Severe Pain, Moderate Pain, Obstetrical analgesia during labor and delivery therapy, Perioperative analgesia, Obstetric analgesia

How Nalbuphine works

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.

Dosage

Nalbuphine dosage

The usual recommended adult dose is 10 mg for a 70 kg individual, administered subcutaneously, intramuscularly or intravenously; this dose may be repeated every 3 to 6 hours as necessary. Dosage should be adjusted according to the severity of the pain, physical status of the patient, and other medications which the patient may bereceiving.

Moderate to severe pain: by intravenous or intramuscular injection 10-20 mg for 70 kg patient, adjusted as required; child up to 0.3 mg/kg repeated once or twice as necessary.

Preoperative anesthesia: by intravenous or intramuscular injection 0.1-0.2 mg/kg.

Obstetrical analgesia during labor & delivery: by intravenous injection 0.3-1 mg/kg over 10-15 minutes with maintenance doses of 0.25-0.5 mg/kg in single intravenous administration as required.

Intraoperative analgesia: by intravenous injection 0.25-0.5 mg/kg at 30 minutes intervals.

Myocardial infarction: By slow intravenous injection 10-20 mg, repeated after 30 minutes if necessary. Larger dose is required when used as supplement of anesthesia than that required for analgesia.

Children from 18 months to 15 years old: usually 0.2 mg/ kg body-weight, given preferably by intravenous or intramuscular injection. Maintenance doses may be given at intervals of 4 to 6 hours or the dose must be determined by the physician.

Side Effects

Generally Nalbuphine is well tolerated. However few side-effects like sedation, sweating, nausea, vomiting, dizziness, vertigo, dry mouth, headache, respiratory depression, dyspnea and asthma may be seen.

Toxicity

Oral, acute LD50 is 1100 mg/kg in dog. Symptoms of overdose include primarily sleepiness and mild dysphoria.

Precaution

Caution should be taken in the following conditions: impaired respiration, impaired renal or hepatic function, billiary tract surgery, myocardial infarction and hypotension.

Interaction

No hazardous interactions have been identified with Nalbuphine; however, interactions described with other opioids may be anticipated. Patient receiving a narcotic analgesic, general anesthesia, phenothiazines or other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with Nalbuphine may exhibit an additive effect.

Food Interaction

  • Avoid alcohol. Ingesting alcohol may increase the sedative and CNS depressant effects of nalbuphine.

Nalbuphine Alcohol interaction

[Moderate] GENERALLY AVOID:

Ethanol may potentiate the central nervous system (CNS) depressant effects of opioid analgesics.

Concomitant use may result in additive CNS depression and impairment of judgment, thinking, and psychomotor skills.

In more severe cases, hypotension, respiratory depression, profound sedation, coma, or even death may occur.

Concomitant use of opioid analgesics with ethanol should be avoided.

Elimination Route

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. Clinical studies show that the duration of analgesic activity of the drug can range from 3 to 6 hours.

Half Life

The plasma half-life of nalbuphine is about 5 hours.

Pregnancy & Breastfeeding use

Pregnancy category B. The placental transfer of Nalbuphine is high and rapid. There are no well-controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. Limited data suggest that Nalbuphine 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 Nalbuphine is administered to a nursing woman.

Contraindication

Known hypersensitivity to Nalbuphine Hydrochloride.

Acute Overdose

Sleepiness & mild dyspnea may occur due to overdose. The immediate intravenous administration of an opiate antagonist such as Naloxone or Nalmefene is a specific antidote. Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated

Storage Condition

Keep it in a cool and dry place, protected from light and moisture.

Innovators Monograph

You find simplified version here Nalbuphine

Nalbuphine contains Nalbuphine see full prescribing information from innovator Nalbuphine Monograph, Nalbuphine MSDS, Nalbuphine FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
Share