Sufentanil
- Atc Codes:N01AH03
- CAS Codes:56030-54-7#60561-17-3
- PHARMGKB ID:56030-54-7#60561-17-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Sufentanil; Belgium: Sufenta, Sufentanil; Bulgaria: Sufentanil; Czech Republic: Sufenta, Sufentanil; Denmark: Sufenta, Sufentanil; Finland: Sufenta, Sufentanil; France: Sufenta, Sufentanil; Germany: Sufenta, Sufentanil; Hungary: Sufentanil; Italy: Disufen, Fentatienil, Sufentanil; Luxembourg: Sufenta; Netherlands: Sufenta, Sufentanil; Poland: Sufenta, Sufentanil; Portugal: Sufenta, Sufentanil; Romania: Sufentanil; Slovakia: Sufenta, Sufentanil; Slovenia: Sufentanil; Sweden: Sufenta.
North America
Canada: Sufentanil; USA: Sufenta, Sufentanil.
Latin America
Argentina: Sufenta; Brazil: Fastfen, Sufenta.
Drug combinations
Chemistry
Sufentanil: C~22~H~30~N~2~O~2~S. Mw: 386.55. (1) Propanamide, N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenyl-; (2) N-[4-(Methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidyl]propionanilide. CAS-56030-54-7 (1976).
Sufentanil Citrate: C~22~H~30~N~2~O~2~S C~6~H~8~O~7~. Mw: 578.67. Propanamide, N-[4-(methoxymethyl)-1-[2-(thienyl)ethyl]-4-piperidinyl]-N-phenyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1). CAS-60561-17-3 (1984).
Pharmacologic Category
Analgesics and Antipyretics; Opiate Agonists. Anilidopiperidine Opioid. General Anesthetic. (ATC-Code: N01AH03).
Mechanism of action
A potent analgesic. Shares actions of opiate agonists. Pain perception is altered in spinal cord and higher CNS levels (substantia gelatinosa, spinal trigeminal nucleus, periaqueductal gray, periventricular gray, medullary raphe nuclei, hypothalamus). Opiate agonists act at specific receptor binding sites in CNS and other tissues. Effects are exerted by opening K^+^ channels and inhibiting Ca^2+^ channels. Opiate receptors are concentrated in limbic system, thalamus, striatum, hypothalamus, midbrain, and spinal cord. High affinity and selectivity for μ-opiate receptor in CNS (higher than fentanyl). Produces dose-related analgesia. At doses up to 8 µg/kg, drug has potent analgesic effect, but higher doses usually produce substantial CNS depression resulting in hypnosis and anesthesia. Appears to have little effect on histamine release. May have centrally-mediated vagal effect.
Therapeutic use
Analgesic supplement in maintenance of balanced general anesthesia. Primary anesthetic for induction and maintenance of anesthesia in patients undergoing major surgical procedures. Epidural anesthetic in conjunction with bupivacaine in labor and delivery.
Pregnancy and lactiation implications
Animal studies suggest embryocidal effects when given I.V. for period of 10 days to >30 days. No evidence of teratogenic effects observed in animals. Administration of epidural sufentanil with bupivacaine with or without epinephrine indicated in labor and delivery. Intravenous use or larger epidural doses not recommended in pregnant women.
Unlabeled use
Contraindications
Hypersensitivity to sufentanil or any component of the formulation.
Warnings and precautions
Use with caution when administering with bradycardia. Use with extreme caution in head injury, intracranial lesions, or elevated intracranial pressure (exaggerated elevation of intracranial pressure may occur). Use with caution in hepatic impairment, in morbidly obese patients, in renal impairment, and in pre-existing respiratory compromise (hypoxia and/or hypercapnia), chronic obstructive pulmonary disease or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function (critical respiratory depression may occur). Rapid I.V. infusion may result in skeletal muscle and chest wall rigidity, impaired ventilation, or respiratory distress/arrest. Use with caution in debilitated patients (higher risk for critical respiratory depression), in the elderly (higher sensitivity to adverse effects), and in neonates (clearance of sufentanil is much slower than adults).