remifentanil

Absorption: IV administration results in complete bioavailability.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Metabolized by blood and tissue esterases, metabolites are excreted by the kidneys.

Half-Life: 3–10 min.

Time/Action Profile ⬆ ⬇

(analgesia‡)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	3–5 min	5–10 min

‡Respiratory depression may last longer than analgesia.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity (cross-sensitivity with other opioid analgesic agents may occur);
Known intolerance.

Use Cautiously in:

Morbidly obese patients (determine dose by ideal body weight [IBW] if weight >30% over IBW);
Diabetes;
Severe pulmonary or hepatic disease;
CNS tumors;
Increased intracranial pressure;
Head trauma;
Adrenal insufficiency;
Undiagnosed abdominal pain;
Hypothyroidism;
Alcoholism;
Cardiac disease;
OB: Use during pregnancy only if the potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children for use as a postoperative analgesic or as an analgesic component of monitored anesthesia care;
Geri: starting dose of remifentanil by 50%.

Adv. Reactions/Side Effects ⬆ ⬇

CV: arrhythmias, bradycardia, circulatory depression, hypotension

Derm: facial itching

EENT: blurred/double vision

GI: biliary spasm, nausea/vomiting (↑ in children)

MS: skeletal and thoracic muscle rigidity, shivering (↑ in children)

Neuro: confusion, paradoxical excitation/delirium

Resp: allodynia, APNEA, LARYNGOSPASM, opioid-induced hyperalgesia, RESPIRATORY DEPRESSION, allergic bronchospasm

Interactions ⬆ ⬇

Drug-drug:

Avoid use in patients who have received MAO inhibitors within the previous 14 days; may produce unpredictable, potentially fatal reactions.
Use with benzodiazepines or other CNS depressants, including otheropioids, non-benzodiazepine sedative/hypnotics, anxiolytics, general anesthetics, muscle relaxants, antipsychotics, and alcohol, may cause profound sedation, respiratory depression, coma, and death; reserve concurrent use for when alternative treatment options are inadequate.
Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SSRIs, SNRIs, MAO inhibitors, TCAs, tramadol, trazodone, mirtazapine, 5-HT3 receptor antagonists, linezolid, methylene blue, and triptans, ↑ risk of serotonin syndrome.
Nalbuphine or buprenorphine may ↓ analgesia.

Route/Dosage ⬆ ⬇

Induction of Anesthesia

IV (Adults ): 0.5–1 mcg/kg/min continuous infusion (an initial dose of 1 mcg/kg may be given over 30–60 sec).

Maintenance of Anesthesia

IV (Adults ): With nitrous oxide 66%: 0.4 mcg/kg/min continuous infusion (range 0.1–2 mcg/kg/min); With isoflurane (0.4–1.5 MAC) or propofol (100–200 mcg/kg/min): 0.25 mcg/kg/min continuous infusion (range 0.05–2 mcg/kg/min). Supplemental bolus doses of 1 mcg/kg may be given.
IV (Children 1–12 yr): With halothane 0.3–1.5 MAC, sevoflurane 0.3–1.5 MAC or isoflurane 0.4–1.5 MAC : 0.25 mcg/kg/min continuous infusion (range 0.05–1.3 mcg/kg/min); supplemental doses of 1 mcg/kg may be given.
IV (Infants birth–2 mo): With nitrous oxide 70%: 0.4 mcg/kg/min continuous infusion (range 0.4–1 mcg/kg/min); supplemental doses of 1 mcg/kg may be given.

Continuation as an Analgesic in Immediately Postoperative Period

IV (Adults ): 0.1 mcg/kg/min continuous infusion (range 0.025–0.2 mcg/kg/min).

Monitored Anesthesia Care (Remifentanil Alone)

IV (Adults ): Single IV dose: 1 mcg/kg given 90 sec before local anesthetic orContinuous infusion: 0.1 mcg/kg/min continuous infusion beginning 5 min before local anesthetic, then 0.05 mcg/kg/min after local anesthetic (range 0.025–0.2 mcg/kg/min).

Monitored Anesthesia Care (Remifentanil + Midazolam)

IV (Adults ≥2 yr): Single IV dose: 0.5 mcg/kg given 90 sec before local anesthetic orContinuous infusion: 0.05 mcg/kg/min continuous infusion beginning 5 min before local anesthetic, then 0.025 mcg/kg/min after local anesthetic (range 0.025–0.2 mcg/kg/min).

Coronary Artery Bypass Surgery

IV (Adults ): Induction and maintenance of anesthesia: 1 mcg/kg/min continuous infusion (range for maintenance 0.125–4 mcg/kg/min; Continuation as an analgesic into ICU: 1 mcg/kg/min continuous infusion (range 0.05–1 mcg/kg/min).

Availability ⬆ ⬇

(Generic available)

Powder for injection: 1 mg/vial; 2 mg/vial; 5 mg/vial

Assessment ⬆ ⬇

Monitor respiratory rate and BP frequently during therapy. Report significant changes immediately. The respiratory depressant effects of remifentanil may last longer than the analgesic effects. Reduce initial doses of other opioids by ¼–⅓ of the usually recommended dose. Monitor closely.
Assess type, location, and intensity of pain before and 3–5 min after administration when used to treat pain.

Lab Test Considerations:

May cause ↑ serum amylase and lipase concentrations.

Toxicity and Overdose:

Symptoms of toxicity include respiratory depression, hypotension, arrhythmias, bradycardia, and asystole. Atropine may be used to treat bradycardia. If respiratory depression persists after surgery, prolonged mechanical ventilation may be required. If an opioid antagonist is required to reverse respiratory depression or coma, naloxone is the antidote. Dilute the 0.4-mg ampule of naloxone in 10 mL of 0.9% NaCl and administer 0.5 mL (0.02 mg) by IV push every 2 min. For children and patients weighing <40 kg, dilute 0.1 mg of naloxone in 10 mL of 0.9% NaCl for a concentration of 10 mcg/mL and administer 0.5 mcg/kg every 2 min. Titrate dose to avoid withdrawal, seizures, and severe pain. Administration of naloxone in these circumstances, especially in cardiac patients, has resulted in hypertension and tachycardia, occasionally causing left ventricular failure and pulmonary edema.

Implementation ⬆ ⬇

Accidental overdosage of opioid analgesics has resulted in fatalities. Before administering, clarify all ambiguous orders; have second practitioner independently check original order, dose calculations, and infusion pump settings.
Benzodiazepines may be administered before or after administration to reduce the induction dose requirements, decrease the time to loss of consciousness, and produce amnesia. This combination may also increase the risk of hypotension.
- Opioid antagonist, oxygen, and resuscitative equipment should be readily available during the administration of remifentanil. Administer remifentanil IV only in monitored anesthesia care settings (operating room, emergency department, ICU) with immediate access to life support equipment. Should be administered only by personnel trained in resuscitation and emergency airway management.

IV Administration:

Reconstitution: Reconstitute each vial by adding 1 mL of sterile water for injection, 0.9% NaCl, or D5W to each milligram of remifentanil (1 mL for 1 mg vial, 2 mL for 2 mg vial, or 5 mL for 5 mg vial).Concentration: 1 mg/mL..
Rate: Administer over 30–60 sec.
Intermittent Infusion: Diluent: May be diluted in sterile water, D5W, D5/0.9% NaCl, 0.9% NaCl, or 0.45% NaCl.Concentration: May be 20–250 mcg/mL depending on amount of diluent.
Rate: For induction of anesthesia administer at a rate of 0.5 to 1 mcg/kg/min. Titrate to lower rate for maintenance of anesthesia.

Patient/Family Teaching ⬆ ⬇

Discuss the use of anesthetic agents and the sensations to expect with the patient before surgery.
Explain pain assessment scale to patient.
Caution patient to change positions slowly to minimize orthostatic hypotension.
Medication causes dizziness and drowsiness. Advise patient to call for assistance during ambulation and transfer and to avoid driving or other activities requiring alertness for 24 hr after administration during outpatient surgery.
Instruct patient to avoid alcohol or other CNS depressants for 24 hr after administration for outpatient surgery.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇