Nalbuphine classification

Nalbuphine solution is classified as a synthetic opioid agonist-antagonist that is chemically related to naxolone (narcotic antagonist) and oxymorphone (strong narcotic analgesic).

Nalbuphine indications for use

Nalbuphine injection is used to treat severe to moderate pain associated with certain acute and chronic conditions such as: cancer, renal or biliary colic, migraine and vascular pain, and for obstetrical analgesia during childbirth. This drug does not cause respiratory depression, at least in a dose-dependent manner.

Mechanism of action of the drug

Nalbuphine has mixed agonist/antagonist activity against opioid receptors. These include µ (mu), k (kappa) and d (delta) receptors, which have recently been reclassified as OP1 (delta), OP2 (kappa) and OP3 (µ).

Exposure to kappa receptors is thought to cause changes in pain perception as well as in the emotional response to pain, possibly by altering the release of neurotransmitters from afferent nerves sensitive to painful stimuli.

An intramuscular dose of 10 mg of Nalbuphine produces analgesia equivalent to 10 mg of morphine. When administered intravenously, its analgesic effect begins after 2-3 minutes, peaks after 30 minutes and lasts for 3-4 hours. With intramuscular and subcutaneous injection, the results begin after 15 minutes and last for 3 to 6 hours. Its half-life is 5 hours.

Nalbuphine dosage

The usual dose for an adult with a body weight of 70 kg is 10 mg.

Nalbuphine schedule

Nalbuphine 10mg/1ml is administered intramuscularly, subcutaneously, or intravenously every 6-8 hours. The dose may be repeated depending on the need for anesthesia and should be adjusted according to the clinical condition of the patient and the use of other drugs.

The use of Nalbuphine as part of a balanced general anesthetic requires higher doses than those recommended as an analgesic. Which requires the explicit recommendation of the physician.

Nalbuphine side effects

The most common adverse reactions to Nalbuphine include:

• sedation;
• dizziness;
• vertigo;
• headache;
• constriction of the pupils;
• nausea/vomiting;
• xerostomia.

Other observed adverse reactions include:

• blurred vision;
• abdominal cramps;
• dyspepsia;
• unpleasant taste in the mouth;
• shortness of breath;
• hot flashes;
• respiratory depression;
• asthma;
• the imperative urge to urinate.

Central nervous system side effects observed when taking Nalbuphine :

• nervousness;
• depression;
• tearfulness;
• euphoria;
• intoxication;
• hostility;
• nightmares;
• confusion.

However, these effects have been reported in less than 1% of patients and are dose-dependent.

Warning! Drugs of the class of opioid agonists/antagonists may have some ability to be addictive.

Symptoms accompanying withdrawal symptoms include:

• nausea and vomiting;
• diarrhea;
• coughing;
• lacrimation;
• runny nose;
• sweating and piloerection (goosebumps).

There may also be an increase in temperature, respiratory rate, and blood pressure.

Nalbuphine: allergy

The drug may cause allergic reactions: anaphylactic, anaphylactoid reactions or severe hypersensitivity reactions have been reported when using Nalbuphine. In such cases, seek medical advice immediately.

Nalbuphine: contraindications

Because of the effects on the digestive tract, Nalbuphine should be used with caution in patients with digestive disorders, including gastrointestinal obstruction, ulcerative colitis, and constipation.

Patients with acute ulcerative colitis or other acute inflammatory diseases of the digestive tract are more sensitive to the constipating effects of opioids.

Nalbuphine is contraindicated in diarrhea secondary to cases of poisoning or infection, and should not be administered until the infectious or toxic agent is eliminated.

Nalbuphine should be administered with caution in patients with acute myocardial infarction, as its possible effects in such patients are unknown. The drug may increase the tone of the biliary tract, especially the sphincter of Oddi, causing biliary spasms. Therefore, it should be used with caution in patients with biliary tract disorders or who have undergone surgery on the biliary tract.

Caution in application

1. Caution should be exercised when administering Nalbuphine solution to patients:
2. With asthma and/or respiratory failure because, like other opioid analgesics, it can aggravate these conditions.
3. With craniocerebral trauma, Nalbuphine should be administered with caution because of the risk of hypoxia and increased cerebrospinal fluid pressure.
4. Children and the elderly, because they are more prone to respiratory depression. Nalbuphine may induce a state of paradoxical arousal when administered with other opioid analgesics, especially in children. Can cause urinary retention in the elderly.

Interactions

Nalbuphine is not recommended for patients using alcohol or other drugs affecting the nervous system because of its depressing effect on respiration. Respiratory and nerve depression are cumulative, and hypotension may also occur if both types of agents are used together.

Nalbuphine pregnancy

This drug should be used in pregnancy only if clearly indicated. Among the side effects associated with the administration of Nalbuphine during labor, neonatal respiratory depression, apnea, cyanosis, and bradycardia have been reported.