Remifentanil


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Continuation of analgesia into immediate postoperative period
Adult: Initially, 0.1 mcg/kg/min continuous infusion, may be adjusted to 0.025 mcg/kg/min increments every 5 minutes to balance respiratory rate and level of analgesia.
Elderly: >65 years Decrease initial adult dose by 50% with careful titration.

Intravenous
Analgesia
Adult: As an analgesic component for monitored anaesthetic care: 0.5-1 mcg/kg over 30-60 seconds as single dose given 90 seconds before the local anaesthetic, initial continuous infusion rate of 0.1 mcg/kg/min beginning 5 minutes prior to local anaesthetic. Infusion rate may be decreased to 0.05 mcg/kg/minute following the local anaesthetic block with rate adjustments of 0.025 mcg/kg/min at 5-minute intervals.
Elderly: >65 years Decrease initial adult dose by 50% with careful titration.

Intravenous
Induction and maintenance of general anaesthesia
Adult: Induction of anaesthesia: 0.5-1 mcg/kg/minute; for endotracheal intubation occurring in <8 minutes, an initial dose of 1 mcg/kg is administered over 30-60 seconds. Maintenance of anaesthesia: Infusion rate may be titrated every 2-5 minutes upward in increments of 25-100% or downward in decrements of 25-50%, 1 mcg/kg as supplemental bolus dose may be given every 2-5 minutes. Infusion rate of >1 mcg/kg/min may increase concomitant anaesthetic agent to increase the dept of anaesthesia.
Elderly: >65 years Decrease initial adult dose by 50% with careful titration.
Special Patient Group
Obese Patients:
Initial dose should be based in ideal body weight (IBW).
Hướng dẫn pha thuốc
Add 1 mL of sterile water for inj, 5% dextrose inj, 5% dextrose and 0.9% sodium chloride inj, 0.9% sodium chloride injection, 0.45% sodium chloride injection, Lactated Ringer's and 5% Dextrose inj to make a concentration of 20-250 mcg/mL. Shake well to dissolve.
Tương kỵ
Admixed with Lactated Ringer’s injection or Lactated Ringer’s with glucose solution for injection, propofol admixture solution. Not recommended for administration into to the same IV line with blood products.
Chống chỉ định
Opioid addiction, abuse and misuse. Administration via epidural or intrathecal due to glycine component in the formulation.
Thận trọng
Patient with acute abdominal conditions, biliary tract dysfunction (e.g. acute pancreatitis, constriction of sphincter of Oddi), bradycardia, delirium tremens, head injury, intracranial lesions, or elevated intracranial pressure (ICP), morbidity obese, prostatic hyperplasia and/or urinary structure, toxic psychosis, chronic obstructive pulmonary disease or cor pulmonale, seizure, thyroid dysfunction. Elderly, cachectic and debilitated patients. Children. Pregnancy and lactation. Not recommended as the sole agent for induction of anaesthesia.
Phản ứng phụ
Significant: Hypotension, bradycardia, apnoea, skeletal muscle rigidity, nausea, vomiting, headache, dizziness.
General disorders and administration site conditions: Postoperative shivering, postoperative occurring hypertension.
Skin and subcutaneous tissue disorders: Pruritus.
Potentially Fatal: Respiratory depression.
IV/Parenteral: C
Thông tin tư vấn bệnh nhân
This drug may cause drowsiness and impair cognitive function, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor pain relief, blood pressure, heart rate, CNS and respiratory status; signs of addiction, abuse and misuse.
Quá liều
Symptoms: Respiratory depression, airway obstruction, atypical snoring, somnolence developing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, miosis and, often pulmonary oedema; bradycardia, hypotension, and death. Management: Supportive treatment. Re-establish patient airway with controlled ventilation. Employ supportive measures (including oxygen and vasopressor) in the management of circulatory shock and pulmonary oedema. Cardiac arrest or arrhythmias will require advanced life support techniques. May administer naloxone or nalmefene as an antidote to respiratory depression.
Tương tác
Reduced analgesic effect and/or precipitate withdrawal symptoms with mixed agonist/antagonist and partial agonist opioid analgesics (e.g. butorphanol, nalbuphine, pentazocine, buprenorphine).
Potentially Fatal: Increased risk of hypotension, profound sedation, respiratory depression, coma and death with concomitant use of benzodiazepines or other CNS depressants (e.g. non-benzodiazepine sedative/hypnotics, tranquilizers, muscle relaxants, general anaesthetics, antipsychotics, other opioids or anxiolytics). Increased risk of serotonin syndrome with concomitant use of serotonergic drugs (e.g. SSRIs, serotonin and norepinephrine reuptake inhibitors, TCA, triptans, 5-HT3 receptor antagonists), mirtazapine, trazodone, tramadol, MAOIs, and other drugs such as linezolid and methylene blue IV.
Food Interaction
Increased risk of extreme sedation, hypotension, respiratory depression and death with alcohol.
Tác dụng
Description: Remifentanil, an anilidopiperidine derivative, is an opioid analgesic which inhibits ascending pain pathway by binding to µ-opioid receptor in the CNS, increasing pain threshold and altering pain reception.
Onset: 1-3 minutes.
Duration: 3-10 minutes.
Pharmacokinetics:
Distribution: Crosses placenta. Central volume of distribution: 100 mL/kg, steady-state volume of distribution: 350 mL/kg. Plasma protein binding: Approx 70% mainly to α1-acid-glycoprotein.
Metabolism: Undergoes hydrolysis by non-specific blood and tissue esterases to inactive carboxylic acid metabolite.
Excretion: Via urine as metabolites (approx 95%). Elimination half-life: Approx 3-10 minutes.
Đặc tính

Chemical Structure Image
Remifentanil

Source: National Center for Biotechnology Information. PubChem Database. Remifentanil, CID=60815, https://pubchem.ncbi.nlm.nih.gov/compound/Remifentanil (accessed on Jan. 22, 2020)

Bảo quản
Store between 2-25°C.
Phân loại ATC
N01AH06 - remifentanil ; Belongs to the class of opioid anesthetics. Used as general anesthetics.
References
Anon. Remifentanil Hydrochloride. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 29/11/2018.

Anon. Remifentanil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 29/11/2018.

Buckingham R (ed). Remifentanil Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 29/11/2018.

Ultiva (Mylan Institutional LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 29/11/2018.

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