Remifentanil

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Ultiva; Belgium: Ultiva; Czech Republic: Ultiva; Denmark: Ultiva; Estonia: Remifentanil; Finland: Ultiva; France: Ultiva; Germany: Ultiva; Greece: Ultiva; Ireland: Ultiva; Italy: Ultiva; Latvia: Remifentanil; Lithuania: Ultiva; Luxembourg: Ultiva; Malta: Ultiva; Netherlands: Remifentanil, Ultiva; Poland: Ultiva; Portugal: Ultiva; Romania: Remifentanil, Ultiva; Slovakia: Remifentanil, Ultiva; Slovenia: Ultiva; Spain: Ultiva; Sweden: Ultiva; UK: Ultiva.

North America

Canada: Ultiva; USA: Ultiva.

Latin America

Argentina: Remicit, Remifentanilo, Ultiva; Brazil: Ultiva; Mexico: Ultiva.

Asia

Japan: Ultiva.

Drug combinations

Chemistry

Remifentanil Hydrochloride: C~20~H~28~N~2~O~5~ HCl. Mw: 412.91. (1) 1-Piperidinepropanoic acid, 4-(methoxycarbonyl)-4-[(1-oxopropyl)phenylamino]-, methyl ester, monohydrochloride; (2) 4-Carboxy-4-(N-phenylpropionamido)-1-piperidine propionic acid, dimethyl ester, monohydrochloride. CAS-132539-07-2; CAS-132875-61-7 (remifentanil)(1992).

Pharmacologic Category

Analgesics and Antipyretics; Opiate Agonists. Anilidopiperidine Opioid. (ATC-Code: N01AH06).

Mechanism of action

Binds with stereospecific μ-opioid receptors at many sites within CNS, increases pain threshold, alters pain reception, inhibits ascending pain pathways.

Therapeutic use

Analgesic for use during induction and maintenance of general anesthesia. For continued analgesia into immediate postoperative period. Analgesic component of monitored anesthesia.

Pregnancy and lactiation implications

Has been shown to cross placenta. Neonatal respiratory depression and sedation may occur. Use with caution in nursing women.

Unlabeled use

Management of pain in mechanically-ventilated patients.

Contraindications

Not for intrathecal or epidural administration, due to presence of glycine in formulation. Hypersensitivity to remifentanil, fentanyl, or fentanyl analogs, or any component of the formulation.

Warnings and precautions

Remifentanil may cause hypotension (use with caution in hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics)). Intraoperative awareness reported. Shares toxic potentials of opiate agonists. Use with caution when administering to patients with bradycardia, and in morbidly obese patients. Interruption of infusion will result in offset of effects within 5-10 minutes. Not recommended as sole agent in general anesthesia, as loss of consciousness cannot be assured. Rapid I.V. infusion may result in skeletal muscle and chest wall rigidity, impaired ventilation, or respiratory distress/arrest. High incidence of apnea, hypotension, tachycardia and muscle rigidity.

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