Remifentanil Hydrochloride

Pronunciation: reh-mih-FEN-tah-nill HIGH-droe-KLOR-ide
Class: Opioid analgesic

Trade Names

Ultiva
- Powder for injection, lyophilized 1 mg/mL after reconstitution

Pharmacology

Opioid agonist.

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Pharmacokinetics

Absorption

Plasma concentrations are proportional to the administered dose.

Distribution

Initial Vd is approximately 100 mL/kg and distributes into peripheral tissue with a Vd at steady state of approximately 350 mL/kg. Plasma protein binding is approximately 70%.

Metabolism

Metabolized by nonspecific esterases in blood and tissue.

Elimination

Elimination t ½ is approximately 3 to 10 minutes.

Special Populations

Elderly

The clearance is reduced approximately 25%.

Children

In children, 5 days to 17 yr of age, the clearance and Vd are increased.

Indications and Usage

Analgesic for use during the induction and maintenance of general anesthesia for inpatient and outpatient procedures and for continuation as an analgesic into the immediate postoperative period under supervision of an anesthesia practitioner; as an analgesic component of monitored anesthesia care.

Contraindications

Epidural or intrathecal administration; hypersensitivity to fentanyl analogs; any component of the product.

Dosage and Administration

General Anesthesia

Not recommended as the sole agent in general anesthesia.

Adults

Induction of anesthesia through intubation:

IV 0.5 to 1 mcg/kg/min by continuous infusion. If endotracheal intubation is to occur less than 8 min after the start of infusion, then an initial dose of 1 mcg/kg may be given over 30 to 60 sec.

Maintenance Of Anesthesia With Nitrous Oxide (66%)
Adults

IV 0.4 mcg/kg/min by continuous infusion (range, 0.1 to 2 mcg/kg/min), supplemental bolus dose of 1 mcg/kg.

Maintenance of Anesthesia with Isoflurane (0.4 to 1.5 MAC) or Propofol (100 to 200 mcg/kg/min)
Adults

IV 0.25 mcg/kg/min (range, 0.05 to 2 mcg/kg/min), supplemental bolus of 1 mcg/kg.

Continuation As An Analgesic Into Immediate Postoperative Period
Adults

IV 0.1 mcg/kg/min (range, 0.025 to 0.2 mcg/kg/min), supplemental bolus not recommended.

Analgesic Component Of Monitored Anesthesia Care

Supplemental oxygen should be supplied.

Adults

Single dose: IV 0.5 to 1 mcg/kg administered over 30 to 60 sec given 90 sec before placement of the local or regional anesthetic block.

Adults

Continuous infusion: IV 0.1 mcg/kg/min beginning 5 min before placement of local or regional anesthetic block.

Individualization of Dosage
Elderly (over 65 yr of age)

IV Decrease the starting dose by 50% and cautiously titrate to effect.

Children (2 yr and over)

IV Same doses per kg as adults.

Obesity

IV Base starting dose on ideal body weight in patients more than 30% over ideal body weight.

General Advice

  • For IV administration only. Do not administer via epidural, intrathecal, intradermal, IM, or subcutaneous routes.
  • Follow manufacturer's instructions for reconstitution of powder and dilution of reconstituted solution.
  • Refer to manufacturer's insert for compatibility with IV fluids and other medications.
  • Inspect solution visually before administration. Do not administer if solution is cloudy, discolored, or contains particulate matter.
  • IV infusion must be administered by an infusion device.
  • IV bolus administration should be used only during maintenance of general anesthesia.
  • Bolus injections or infusion should be made into IV tubing at or close to the venous cannula.
  • Following IV bolus dose or discontinuation of IV infusion flush tubing to clear residual medication to prevent inadvertent administration at a later time.
  • Do not administer in same IV tubing with blood.

Storage/Stability

Store powder for injection in refrigerator (36° to 46°F) or at room temperature (less than 78°F). Reconstituted and diluted solutions are stable for up to 24 hr at room temperature.

Drug Interactions

Agonist/Antagonist analgesics

Withdrawal may be precipitated.

Barbiturate anesthetics

May cause increased CNS and respiratory depression.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Bradycardia; hypotension; tachycardia; hypertension; premature ventricular beats; MI; atrial fibrillation; atrial flutter; decreased cardiac output; arrhythmia; ventricular fibrillation; third degree heart block.

CNS

Dizziness; agitation; headache; somnolence; anxiety; hallucinations; decreased mental acuity.

Dermatologic

Pruritus.

EENT

Visual disturbance; pharyngitis.

GI

Nausea; vomiting; constipation.

Genitourinary

Oliguria.

Hematologic

Coagulation disorder; hemorrhage; anemia; thrombocytopenia.

Respiratory

Respiratory depression; apnea; pleural effusion; pneumonia; cough; dyspnea.

Miscellaneous

Skeletal muscle rigidity; shivering; chills; fever; postoperative pain; hypoxia; sweating; flushing; warm sensation; pain at IV site; postoperative and perioperative complications; involuntary movements; edema; heartburn.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 2 yr of age.

Elderly

Reduce dose in patients older than 65 yr of age.

Drug dependence

Has abuse potential of the morphine type.

Overdosage

Symptoms

Extension of the pharmacologic effects including, apnea, chest-wall rigidity, seizures, hypoxemia, hypotension, bradycardia

Patient Information

  • Advise patient, family, or caregiver that medication will be prepared and administered by a health care provider in a health care setting.
  • Reassure patient, family, or caregiver that breathing will be closely monitored and supported while medication is being administered and that breathing and function will quickly return to normal after medication has been discontinued.
  • Advise patient, family, or caregiver that nausea, vomiting, itching, or headache may occur during recovery period and to inform health care provider if noted and bothersome.

Copyright © 2009 Wolters Kluwer Health.

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