Remifentanil

What it is and how it works

Mechanism of Action Remifentanil HCl is a μ-opioid agonist with rapid onset and peak effect, and short duration of action. The μ-opioid activity of remifentanil HCl is antagonized by opioid antagonists such as naloxone. Unlike other opioids, remifentanil HCl is rapidly metabolized by hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases. Remifentanil HCl is not a substrate for plasma cholinesterase (pseudocholinesterase) and, therefore, patients with atypical cholinesterase are expected to have a normal duration of action.

Indications

Remifentanil hydrochloride (HCl) for injection is indicated for intravenous (IV) administration: • As an analgesic agent for use during the induction and maintenance of general anesthesia for inpatient and outpatient procedures. • For continuation as an analgesic into the immediate postoperative period in adult patients under the direct supervision of an anesthesia practitioner in a postoperative anesthesia care unit or intensive care setting. • As an analgesic component of monitored anesthesia care in adult patients. Remifentanil hydrochloride for injection is an opioid agonist indicated for intravenous administration: • As an analgesic agent for use during the induction and maintenance of general anesthesia for inpatient and outpatient procedures. • For continuation as an analgesic into the immediate postoperative period in adult patients under the direct supervision of an anesthesia practitioner in a postoperative anesthesia care unit or intensive care setting. • As an analgesic component of monitored anesthesia care in adult patients.

Dosage and administration (summary)

• Monitor patients closely for respiratory depression when initiating therapy and following dosage increases and adjust the dosage accordingly. • Initial Dosage in Adults : See full prescribing information for recommended doses in adult patients. ( 2.2 , 2.3 ) • Initial Dosage in Pediatric Patients : See full prescribing information for recommended doses in pediatric patients. • Geriatric Patients : The starting doses should be decreased by 50% in elderly patients (> 65 years). Important Dosage and Administration Instructions Monitor patients closely for respiratory depression when initiating therapy and following dosage increases with remifentanil HCl and adjust the dosage accordingly .

Contraindications

Remifentanil HCl is contraindicated: • For epidural or intrathecal administration due to the presence of glycine in the formulation . • In patients with hypersensitivity to remifentanil (e.g., anaphylaxis) . Remifentanil hydrochloride for injection is contraindicated: • For epidural or intrathecal administration due to the presence of glycine in the formulation. • In patients with hypersensitivity to remifentanil (e.g., anaphylaxis).

Warnings and precautions

• Respiratory Depression in Spontaneously Breathing Patients : Monitor closely, particularly during initiation and titration. • Risks from Use as Postoperative Analgesia with Concomitant Benzodiazepines or other CNS Depressants : Hypotension, profound sedation, respiratory depression, coma, and death may result from the concomitant use of Remifentanil hydrochloride for injection with benzodiazepines or other CNS depressants. • Serotonin Syndrome : Potentially life-threatening condition could result from concomitant serotonergic drug administration.

Pregnancy

Pregnancy Risk Summary Prolonged use of opioid analgesics during pregnancy may cause neonatal opioid withdrawal syndrome. Available data with remifentanil hydrochloride in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage.

Storage and supply

Remifentanil HCl for injection should be stored at 2° to 25°C (36° to 77°F). Remifentanil HCl for IV use is supplied as follows: Product Code Unit of Sale Strength Each PRX723103 NDC 63323-723-06 Unit of 10 1 mg per vial NDC 63323-723-04 3 mL Single Dose Vial Discard unused portion. The container closure is not made with natural rubber latex.

Source: Remifentanil Hydrochloride (Remifentanil Hydrochloride) — US FDA prescribing information, 2025-02-13, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.