Nalbuphin (Solution) Instructions for Use

Instructions
Dosage forms

ATC Code

N02AF02 (Nalbuphine)

Active Substance

Nalbuphine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Opioid receptor agonist-antagonist. Analgesic

Pharmacotherapeutic Group

Opioid analgesic agent: opioid receptor agonist-antagonist

Pharmacological Action

An opioid analgesic, an agonist-antagonist of opioid receptors. It activates the endogenous antinociceptive system primarily through opioid κ-receptors and thus disrupts interneuronal transmission of pain impulses at various levels of the CNS, and also changes the emotional coloring of pain by affecting the higher parts of the brain.

It has an analgesic effect comparable to morphine, exerts a sedative effect, stimulates the vomiting center, causes miosis, and inhibits conditioned reflexes. It depresses the respiratory center to a lesser extent than agonists of opioid μ-receptors (morphine, promedol, fentanyl). It does not have a significant effect on hemodynamics and on the motility of the gastrointestinal tract organs.

The analgesic effect develops quickly: with IV administration – within a few minutes; with IM administration – within 10-15 minutes. The maximum effect is achieved in 1-2 hours, the duration of action is 3-6 hours.

Pharmacokinetics

Metabolized in the liver.

T_1/2 is 2.5-3 hours. Unchanged Nalbuphine is excreted mainly in the urine (about 70%), in the form of metabolites – mainly with bile.

Indications

Severe pain syndrome of various origins (including in the postoperative period, in myocardial infarction, during gynecological interventions, in malignant neoplasms); premedication before inhalation anesthesia, as a component of IV anesthesia.

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
R52.0	Acute pain
R52.2	Other chronic pain
Z51.4	Preparatory procedures for subsequent treatment or examination, not elsewhere classified

ICD-11 code	Indication
MG30.Z	Chronic pain syndrome, unspecified
MG31.Z	Acute pain, unspecified
QB9A	Preparatory procedures for subsequent treatment

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Determine the dosage individually based on the patient’s weight, severity of pain, and clinical response.

Administer the solution via intravenous (IV), intramuscular (IM), or subcutaneous (SC) routes.

For adult patients, administer a single dose ranging from 100 mcg/kg to 1 mg/kg of body weight.

For pediatric patients, the initial single dose is 300 mcg/kg.

Adjust the frequency of administration according to the indication and the patient’s clinical situation; repeat doses as necessary to maintain analgesia.

For premedication before anesthesia, administer a dose of 100-200 mcg/kg IV or 300 mcg/kg IM.

As a component of balanced anesthesia, administer an initial IV dose of 300-500 mcg/kg; provide supplemental doses of 100-200 mcg/kg as required.

For postoperative pain management, administer 300-500 mcg/kg IV, IM, or SC every 3-6 hours as needed.

Do not exceed a maximum daily dose without careful reassessment of the patient’s condition.

Limit the duration of therapy to a maximum of three days for acute pain management to mitigate the risk of tolerance and dependence.

Exercise extreme caution and initiate therapy at the lower end of the dosage range for elderly, debilitated patients, and those with hepatic or renal impairment.

Monitor all patients closely for signs of respiratory depression, especially during the initial dosing period and following any dose increase.

Adverse Reactions

From the CNS and peripheral nervous system frequent – drowsiness, lethargy; possible – dizziness, balance disorders, headache; rare – nervousness, depression, confusion, dysphoria; in some cases – difficulty speaking, blurred vision.

From the digestive system nausea, vomiting, dry mouth are possible.

From the cardiovascular system in some cases – arterial hypertension or hypotension, bradycardia, tachycardia.

Allergic reactions in some cases – urticaria.

Other increased sweating is possible.

Contraindications

Hypersensitivity to nalbuphine.

Use in Pregnancy and Lactation

Use during pregnancy is possible only for strict indications.

Use with caution in premature birth and suspected fetal immaturity (since Nalbuphine crosses the placental barrier and can cause respiratory depression in the newborn).

Use with caution during lactation (breastfeeding).

Nalbuphine is excreted in breast milk in very small, clinically insignificant amounts (less than 1% of the administered dose).

Use in Hepatic Impairment

In hepatic insufficiency, Nalbuphine should be carefully dosed and the possibility of rapid discontinuation of administration should be provided.

Use in Renal Impairment

In renal insufficiency, Nalbuphine should be carefully dosed and the possibility of rapid discontinuation of administration should be provided.

Geriatric Use

Should be used with caution in elderly persons.

Special Precautions

Should be used with caution in cases of respiratory function impairment (including obstructive pulmonary diseases, emphysema), since Nalbuphine can cause a reduction in minute respiratory volume by approximately 20-25% (when administered at a dose of 20 mg per 70 kg of body weight), in uremia, in elderly persons, and in cases of severe exhaustion.

Nalbuphine should be used with caution and under constant supervision in cases of skull injuries (due to the possible development of respiratory depression), increased intracranial pressure and cerebrospinal fluid pressure in the spinal canal.

In renal and hepatic insufficiency, Nalbuphine should be carefully dosed and the possibility of rapid discontinuation of administration should be provided.

Nalbuphine should not be combined with other opioid analgesics due to the risk of weakening analgesia and the possibility of provoking withdrawal syndrome in patients with opioid dependence.

Nalbuphine should be used under careful supervision and in reduced doses against the background of the action of anesthetic agents, hypnotics, anxiolytics, antidepressants, and antipsychotic agents (neuroleptics) to avoid excessive CNS depression and suppression of respiratory center activity.

Effect on the ability to drive vehicles and operate machinery

Use with caution in outpatient settings in patients engaged in potentially hazardous activities that require increased attention and high speed of psychomotor reactions.

Drug Interactions

With simultaneous use with anesthetic agents, hypnotics, sedatives, anxiolytics (tranquilizers), antipsychotic agents (neuroleptics), antidepressants, antihistamines with sedative effect, ethanol, the depressant effect on the CNS is enhanced.

Storage Conditions

Store at 15°C (59°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Nalbuphin [International Pharmaceutical Services Ltd. (USA)]
Solution for intravenous and intramuscular administration 10 mg/1 ml: amp. 5 or 10 pcs.

Marketing Authorization Holder

International Pharmaceutical Services Ltd. (USA)

Manufactured By

N.A. Semashko Moscow Chemical Pharmaceutical Preparations, JSC (Russia)

Dosage Form

Nalbuphine

Solution for intravenous and intramuscular administration 10 mg/1 ml: amp. 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for IV and IM administration	1 ml
Nalbuphine	10 mg

1 ml – ampoules (5) – cardboard packs.
1 ml – ampoules (10) – cardboard packs.

Nalbuphin [Moscow Endocrine Plant FSUE (Russia)]
Injection solution 10 mg/1 ml: 1 ml amp. 5 or 10 pcs.

Marketing Authorization Holder

Moscow Endocrine Plant FSUE (Russia)

Dosage Form

Nalbuphine

Injection solution 10 mg/1 ml: 1 ml amp. 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for injection in the form of a transparent, colorless or yellowish liquid.

	1 ml
Nalbuphine hydrochloride (calculated as anhydrous)	10 mg

Excipients : sodium chloride – 1 mg, sodium disulfite (sodium metabisulfite) – 1 mg, sodium citrate dihydrate – 7.74 mg (equivalent to 9.4 mg of sodium citrate pentasesquihydrate), citric acid monohydrate (or citric acid calculated as citric acid monohydrate) – 12.6 mg, water for injections – up to 1 ml.

1 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
1 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.

Nalbuphin [Moscow Endocrine Plant FSUE (Russia)]
Solution for injection 20 mg/1 ml: amp. 1 ml 5 or 10 pcs.