Adult: As management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate: Initially, 2 mg as a single dose (in patients who will be able to remain recumbent if drowsiness or dizziness occurs), repeated 3-4 hourly as needed. Usual dosing range: 1-4 mg 3-4 hourly based on the severity of pain. Elderly: Half of the usual initial dose. Subsequent doses are based on patient's response and given at intervals of at least 6 hours.
Intramuscular, Intravenous Pain during labour
Adult: In patients at full term (fetus ≥37 weeks of gestation) and without signs of fetal distress: 1-2 mg via IV or IM inj, repeated after 4 hours if necessary. Alternative analgesic is used for pain associated with delivery or if delivery is expected within 4 hours.
Intramuscular Preoperative sedation
Adult: 2 mg given 60-90 minutes before surgery.
Intravenous Acute pain
Adult: As management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate: Initially, 1 mg as a single dose, repeated 3-4 hourly as needed. Usual dosing range: 0.5-2 mg 3-4 hourly based on the severity of pain. Elderly: Half of the usual initial dose. Subsequent doses are based on patient's response and given at intervals of at least 6 hours.
Intravenous Adjunct in balanced anaesthesia
Adult: 2 mg given shortly before induction and/or 0.5-1 mg in increments during anaesthesia. Usual total dose: 4-12.5 mg.
Nasal Acute pain
Adult: As management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate: Initially, 1 mg (1 spray in one nostril); if adequate pain relief is not obtained within 60-90 minutes, may give an additional dose of 1 mg (1 spray in one nostril). Initial dose sequence may be repeated 3-4 hours after the last dose, as necessary. Alternative dosing recommendation: Initially, 2 mg (1 spray in each nostril) may be given in patients who will be able to remain recumbent if drowsiness or dizziness occurs; may repeat dose after 3-4 hours from the initial dose. Elderly: Initially, 1 mg (1 spray in one nostril); if adequate pain relief is not obtained within 90-120 minutes, may give an additional dose of 1 mg (1 spray in one nostril). Initial dose sequence may be repeated at intervals of at least 6 hours based on the patient's response.
What are the brands available for Butorphanol in Philippines?
Intravenous/Intramuscular: Acute pain; Pain during labour:
Half of the usual initial dose. Subsequent doses are based on patient's response and given at intervals of at least 6 hours.
Nasal: Acute pain:
Initially, 1 mg (1 spray in one nostril); if adequate pain relief is not obtained within 90-120 minutes, may give an additional dose of 1 mg (1 spray in one nostril). Initial dose sequence may be repeated at intervals of at least 6 hours based on the patient's response.
Hepatic Impairment
Intravenous/Intramuscular: Acute pain; Pain during labour:
Half of the usual initial dose. Subsequent doses are based on patient's response and given at intervals of at least 6 hours.
Nasal: Acute pain:
Initially, 1 mg (1 spray in one nostril); if adequate pain relief is not obtained within 90-120 minutes, may give an additional dose of 1 mg (1 spray in one nostril). Initial dose sequence may be repeated at intervals of at least 6 hours based on the patient's response.
Contraindications
Acute or severe bronchial asthma (in the absence of resuscitative equipment or in an unmonitored setting), significant respiratory depression, known or suspected gastrointestinal obstruction (including paralytic ileus).
Special Precautions
Patient with hypovolaemia, CV disease (e.g. acute MI), circulatory shock; acute abdominal conditions, adrenal insufficiency (including Addison's disease), biliary tract dysfunction (e.g. acute pancreatitis), impaired consciousness; delirium tremens, head injury, intracranial lesions, elevated intracranial pressure; mental health conditions (e.g. depression, anxiety, post-traumatic stress disorder); prostatic hyperplasia, urinary stricture, toxic psychosis, significant COPD or cor pulmonale, substantially decreased respiratory reserve, hypoxia, hypercapnia, history of seizure disorders, sleep-related disorders (e.g. sleep apnoea), thyroid dysfunction, history of substance abuse disorder. Morbidly obese, cachectic or debilitated patients. Avoid abrupt withdrawal. Renal and hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: CNS depression, opioid-induced hyperalgesia (OIH), severe hypotension (including orthostatic hypotension and syncope), secondary hypogonadism leading to mood disorders and osteoporosis (prolonged use); constriction of sphincter of Oddi; increased intracranial pressure; seizure; serious withdrawal symptoms (abrupt discontinuation); risk of addiction, abuse and misuse; decreased bowel motility. Cardiac disorders: Palpitations. Ear and labyrinth disorders: Tinnitus. Eye disorders: Blurred vision. Gastrointestinal disorders: Nausea, vomiting, constipation, dry mouth, stomach pain, unpleasant taste. General disorders and administration site conditions: Asthenia. Metabolism and nutrition disorders: Anorexia. Nervous system disorders: Somnolence, dizziness, drowsiness, lethargy, headache, paraesthesia. Psychiatric disorders: Anxiety, confusion, euphoria, nervousness; insomnia (nasal). Respiratory, thoracic and mediastinal disorders: Cough, dyspnoea; epistaxis, nasal congestion or irritation (nasal). Skin and subcutaneous tissue disorders: Pruritus. Potentially Fatal: Respiratory depression.
This drug may impair physical or mental abilities, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood pressure. Evaluate pain relief, bowel function, respiratory and mental status. Assess for signs and symptoms of drug use disorder, abuse or misuse; hypogonadism or hypoadrenalism.
Overdosage
Symptoms: Respiratory depression, somnolence progressing to coma or stupor, skeletal muscle flaccidity, constricted pupils, cold and clammy skin, pulmonary oedema, hypotension, bradycardia, partial or complete airway obstruction, atypical snoring and marked mydriasis with hypoxia. Management: Supportive treatment. Institute assisted or controlled ventilation and reestablish patent and protected airway. Perform advanced life-support techniques for cardiac arrest or arrhythmias. Administer opioid antagonists (e.g. naloxone, nalmefene) for clinically significant respiratory or circulatory depression.
Drug Interactions
Potentially Fatal: Increased risk of serotonin syndrome with SSRIs, SNRIs, triptans, TCAs, 5-HT3 receptor antagonists, fentanyl, lithium, IV methylthioninium chloride (also known as methylene blue), tramadol, mirtazapine, trazodone, MAOIs, certain muscle relaxants (e.g. cyclobenzaprine, metaxalone). Increased risk of hypotension, respiratory depression, profound sedation and coma with benzodiazepines or other CNS depressants (e.g. other sedatives/hypnotics, anxiolytics, tranquilisers, muscle relaxants, general anaesthesia, antipsychotics, other opioids).
Food Interaction
Increased risk of hypotension, respiratory depression, profound sedation and coma with alcohol. Increased risk of serotonin syndrome with St. John's wort.
Action
Description: Mechanism of Action: Butorphanol is an agonist of kappa opiate receptors and partial agonist of mu opiate receptors in the central nervous system (CNS). This causes inhibition of ascending pain pathways, therefore altering pain perception and response. Onset: Within 15 minutes (IM or nasal); within a few minutes (IV). Duration: 3-4 hours (IM or IV); 4-5 hours (nasal). Pharmacokinetics: Absorption: Rapidly and well absorbed. Bioavailability: 60-70% (nasal). Time to peak plasma concentration: 20-40 minutes (IM); 30-60 minutes (nasal). Distribution: Crosses the placenta and enters breast milk. Volume of distribution: 305-901 L. Plasma protein binding: Approx 80%. Metabolism: Extensively metabolised in the liver via hydroxylation, N-dealkylation and conjugation into hydroxybutorphanol (major metabolite). Excretion: Mainly via urine (70-80%; approx 5% as unchanged drug); faeces (approx 15%). Elimination half-life: Approx 2-9 hours (IV or nasal).
Chemical Structure
Butorphanol Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5361092, Butorphanol. https://pubchem.ncbi.nlm.nih.gov/compound/Butorphanol. Accessed Nov. 25, 2024.
N02AF01 - butorphanol ; Belongs to the class of morphinan derivative opioids. Used to relieve pain.
References
Anon. Butorphanol. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/11/2024.Brayfield A, Cadart C (eds). Butorphanol Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/11/2024.Butorphanol Tartrate Injection, Solution (Hikma Pharmaceuticals USA Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/11/2024.Butorphanol Tartrate Spray (Apotex Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/11/2024.Butorphanol. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 04/11/2024.Butorphanol. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 04/11/2024.Zinol 2 mg/mL Solution for Injection (Hanlim Pharmaceutical Co., Ltd.). MIMS Philippines. http://www.mims.com/philippines. Accessed 13/11/2024.Ziphanol 2 mg/mL Solution for Injection (Myungmoon Pharmaceutical Co., Ltd.). MIMS Philippines. http://www.mims.com/philippines. Accessed 13/11/2024.
Sign Out
