Sufentanil


Generic Medicine Info
Indications and Dosage
Epidural
Analgesia during labour and vaginal delivery
Adult: In combination with 10 mL bupivacaine 0.125% with or without epinephrine: 10-15 mcg via slow inj, may be repeated twice at a minimum of 1-hour intervals until delivery. Max total dose: 30 mcg.

Intravenous
Analgesic adjunct to balanced general anaesthesia
Adult: In combination with nitrous oxide and oxygen in patients who are intubated and ventilated: For expected duration of anaesthesia of 1-2 hours: Total dose: 1-2 mcg/kg; may give ≥75% of the total dose via slow inj or infusion before intubation. Maintenance: 10-25 mcg may be given in increments as necessary. Alternatively, intermittent or continuous maintenance infusion may be given as necessary; adjust rates based on the induction dose used. Max total dose: 1 mcg/kg/hour. For expected duration of anaesthesia of 2-8 hours: Total dose: 2-8 mcg/kg; may give ≤75% of the total dose via slow inj or infusion before intubation. Maintenance: 10-50 mcg may be given in increments as necessary. Alternatively, intermittent or continuous maintenance infusion may be given as necessary; adjust rates based on the induction dose used. Max total dose: 1 mcg/kg/hour. Doses are individualised based on several factors (e.g. weight, response, underlying condition, anaesthetic used, nature and duration of surgery). Supplemental doses may be given based on patient movement and/or changes in vital signs, and adjusted based on individual needs and response and the expected remaining duration of procedure. Refer to detailed product guidelines for further information.
Elderly: Lower initial dose may be required.

Intravenous
Primary anaesthetic
Adult: For induction and maintenance of anaesthesia: In combination with 100% oxygen in patients undergoing major surgical procedures, or in those who are intubated and ventilated (e.g. CV surgery, neurosurgical procedures in sitting position): Total dose: 8-30 mcg/kg via slow inj, infusion, or inj followed by an infusion. Maintenance: 0.5-10 mcg/kg via slow inj as necessary, depending on the initial dose. Alternatively, intermittent or continuous maintenance infusion may be given as necessary; adjust rate based on the induction dose so that total dose for the procedure does not exceed 30 mcg/kg. Refer to detailed product guidelines for further information.
Child: In combination with 100% oxygen in patients undergoing CV surgery: <12 years Initially, 10-25 mcg/kg. Maintenance: Up to 25-50 mcg, as necessary based on patient response to initial dose. Doses may be given via slow inj or infusion.
Elderly: Lower initial dose may be required.

Sublingual
Postoperative pain
Adult: For management of acute moderate to severe cases: 15 mcg on a patient-controlled as needed basis at intervals of at least 20 minutes (lockout interval) between doses. Max treatment duration: 72 hours. Doses are given using the administration device provided.

Sublingual
Acute pain
Adult: In patients whom alternative treatment options are or may be intolerable or inadequate: Initially, 30 mcg; may be repeated as needed with at least 1 hour between doses. Max: 360 mcg daily. Max treatment duration: 72 hours. Doses are given using the administration device provided. Dosing recommendations may vary among individual products and countries (refer to specific product guidelines).
Special Patient Group
IV:
Debilitated patients: Lower initial dose may be required.
Contraindications
Sublingual tab: Significant respiratory depression, acute or severe bronchial asthma (in an unmonitored setting or absence of resuscitative equipment), known or suspected gastrointestinal obstruction (including paralytic ileus).
Special Precautions
Patient with adrenal insufficiency (e.g. Addison disease); significant COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia or pre-existing respiratory depression; increased intracranial pressure, impaired consciousness, coma, delirium tremens, brain tumours, head injury, intracranial lesions, toxic psychosis; history of seizure disorder; prostatic hyperplasia and/or urinary stricture; previous or pre-existing bradyarrhythmias; hypovolaemia, CV disease (including acute MI); sleep-related disorders; biliary tract disease (including acute pancreatitis); uncontrolled hypothyroidism; personal or family history of drug abuse, acute alcoholism, or mental illness. Morbidly obese, cachectic or debilitated patients. Avoid use in patient with circulatory shock (sublingual tab). Avoid abrupt withdrawal following prolonged use. Renal and hepatic impairment. Children (IV use) and elderly. Pregnancy and lactation. Concomitant use with sedating drugs (e.g. benzodiazepine or other CNS depressants), CYP3A4 inhibitors or inducers, serotonergic agents (e.g. SSRI). Concomitant use with or within 14 days after MAOI therapy is not recommended.
Adverse Reactions
Significant: CNS depression, sleep-related breathing disorders (including central sleep apnoea and sleep-related hypoxaemia), severe bradycardia, severe hypotension (including orthostatic hypotension and syncope); secondary hypogonadism (long-term use); increase risk or exacerbate pre-existing seizure disorder; spasm of sphincter of Oddi.
Cardiac disorders: Tachycardia or sinus tachycardia.
Gastrointestinal disorders: Nausea, vomiting, dyspepsia, constipation, dry mouth, flatulence.
General disorders and administration site conditions: Pyrexia.
Investigations: Oxygen saturation decreased.
Musculoskeletal and connective tissue disorders: Muscle spasms or twitching.
Nervous system disorders: Headache, sedation, dizziness, somnolence.
Psychiatric disorders: Confusional state, insomnia, anxiety.
Renal and urinary disorders: Urinary retention.
Respiratory, thoracic and mediastinal disorders: Hypoxia.
Skin and subcutaneous tissue disorders: Pruritus.
Vascular disorders: Hypertension.
Potentially Fatal: Respiratory depression; neonatal withdrawal syndrome (long-term use during pregnancy).
Epidural/IV/Parenteral: C
Patient Counseling Information
This drug may cause dizziness, somnolence, or visual disturbance, if affected, do not drive or operate machinery. Do not eat or drink and minimise talking for 10 minutes after taking the sublingual tab.
Monitoring Parameters
Assess patient's risks of opioid addiction, abuse, and misuse prior to prescribing treatment. Monitor blood pressure, heart rate; effectiveness of pain relief, respiratory and CV status. Evaluate patient's physical and/or psychological dependence. Monitor for signs and symptoms of respiratory depression before and periodically during treatment.
Overdosage
Symptoms: Loss of consciousness, cold and clammy skin, constricted pupils, CV shock, muscle rigidity or flaccidity, hypoventilation, respiratory arrest, coma; in some cases, pulmonary oedema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring. Management: Symptomatic and supportive treatment. Re-establish patent and protected airway, initiate assisted or controlled ventilation if necessary. In case of circulatory shock and pulmonary oedema, administer oxygen and vasopressors as clinically indicated. Administer opioid antagonist (e.g. naloxone, nalmefene) for clinically significant respiratory depression; may be given repeatedly or by infusion if necessary. If respiratory depression is associated with muscular rigidity, IV neuromuscular blockers may be required.
Drug Interactions
May decrease plasma concentration or opioid efficacy, possibly resulting in withdrawal syndrome (for those who have developed dependence) with CYP3A4 inducers or when concomitant CPY3A4 inhibitor is discontinued. Concurrent use with Ca channel blockers and/or β-blockers (particularly in patients on chronic therapy with these drugs) may increase the incidence and degree of bradycardia and hypotension. May reduce analgesic effect and/or precipitate withdrawal symptoms with mixed agonist/antagonist and partial agonist opioid analgesics (e.g. butorphanol, nalbuphine, pentazocine, buprenorphine). May enhance the neuromuscular blocking action of skeletal muscle relaxants. May decrease efficacy of diuretics. May increase risk of urinary retention and/or severe constipation with anticholinergic drugs.
Potentially Fatal: May result in hypotension, profound sedation, coma, and respiratory depression with sedating drugs (e.g. benzodiazepines or other CNS depressants). Concomitant use with CYP3A4 inhibitors such as macrolide antibiotics (e.g. erythromycin), azole-antifungal drugs (e.g. ketoconazole), protease inhibitors (e.g. ritonavir) or discontinuation of concomitant CYP3A4 inducer (e.g. rifampicin, carbamazepine, phenytoin) may increase the plasma concentrations and prolong opioid adverse effects of sufentanil, which may result in respiratory depression. Risk of serotonin syndrome with SSRIs, serotonin-norepinephrine reuptake inhibitors, triptans, MAOIs (including linezolid and IV methylene blue), 5-HT3 receptor antagonists, drugs affecting the serotonin neurotransmitter system (e.g. mirtazapine, trazodone, tramadol), certain muscle relaxants (e.g. cyclobenzaprine, metaxalone).
Food Interaction
Concomitant use with alcohol may result in hypotension, profound sedation, coma, and respiratory depression.
Action
Description: Sufentanil is a synthetic phenylpiperidine derivative, potent opioid that has high affinity and selectivity for μ-opioid receptors and acts as a full opioid agonist. After binding to the receptors, it exerts effects by opening K channels and inhibiting Ca channels. This results in increased threshold for pain, altered pain perception, and suppressed ascending pain pathways.
Onset: Analgesia: 1-3 minutes (IV); 5-10 minutes (epidural); approx 30 minutes (sublingual).
Duration: Dose dependent. Anaesthesia adjunct doses: 1.7 hours (epidural; 10-15 mcg dose with bupivacaine 0.125%); approx 3 hours (sublingual).
Pharmacokinetics:
Absorption: Bioavailability: Approx 53% (sublingual). Time to peak plasma concentration: 1 hour (sublingual); within 10 minutes (epidural).
Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: 91-93%, mainly to α1-acid glycoprotein.
Metabolism: Primarily metabolised in the liver and small intestine by CYP3A4 isoenzyme via O-demethylation and N-dealkylation to inactive metabolites.
Excretion: IV/epidural: Via urine and faeces (approx 80%; 2% as unchanged drug) within 24 hours. Elimination half-life: 164 minutes (IV); 2.5 ± 0.85 hours (sublingual).
Chemical Structure

Chemical Structure Image
Sufentanil

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 41693, Sufentanil. https://pubchem.ncbi.nlm.nih.gov/compound/Sufentanil. Accessed Oct. 26, 2021.

Storage
Store between 20-25°C. Protect from light.
MIMS Class
Anaesthetics - Local & General / Analgesics (Opioid)
ATC Classification
N01AH03 - sufentanil ; Belongs to the class of opioid anesthetics. Used as general anesthetics.
References
Anon. Sufentanil Citrate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 22/07/2021.

Anon. Sufentanil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/07/2021.

Buckingham R (ed). Sufentanil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/07/2021.

Dsuvia Tablet (AcelRx Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 22/07/2021.

Dzuveo 30 mcg Sublingual Tablet (FGK Representative Service). European Medicines Agency [online]. Accessed 22/07/2021.

Sufenta (PT Kimia Farma). MIMS Indonesia. http://www.mims.com/indonesia. Accessed 23/07/2021.

Sufentanil Citrate Injection, Solution (Hospira, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 22/07/2021.

Zalviso 15 mcg Sublingual Tablets (Grunenthal GmbH). European Medicines Agency [online]. Accessed 22/07/2021.

Disclaimer: This information is independently developed by MIMS based on Sufentanil from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 MIMS. All rights reserved. Powered by MIMS.com
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