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sufentanil (Sufenta,Dsuvia)
Tradename: Sufenta. DEA-controlled substance: class 2.
Indications:
- analgesic component of monitored/general anesthesia
Contraindications: concurrent use of MAO inhibitors
Dosage:
1) initial dose: 1-8 ug/kg
2) maintenance: 10-50 ug IV
3) epidural: 25-50 ug
4) sublingual (Dsuvia) 30 ug
Injection: 50 ug/mL (1 mL, 2 mL, 5 mL).
Pharmacokinetics:
1) rapid onset of action (1-3 minutes)
2) duration of action 45-90 minutes
3) metabolized by the liver by cyt P450 3A4
4) eliminated mostly as inactive drug in the urine
5) triphasic elimination
6) terminal 1/2life of 2-2.5 hours
Adverse effects:
1) common (> 10%)
- bradycardia, hypotension, drowsiness, nausea/vomiting, respiratory depression
2) less common (1-10%)
- cardiac arrhythmias, orthostatic hypotension, confusion, CNS depression, biliary tract spasm, blurred vision
3) uncommon (< 1%)
- circulatory depression, convulsions, dysesthesia, paradoxical CNS excitement, delirium, mental depression, dizziness, rash, urticaria, itching, urinary tract spasm, laryngospasm, bronchospasm, cold, clammy skin, addiction with prolonged use
4) other
- headache
- shivering
- constipation
- muscle rigidity (dose-related)
5) overdose:
- management:
- airway support
- IV administration of naloxone
- 2 mg (0.01 mg/kg in children)
- may repeat up to a total of 10 mg
Drug interactions:
1) benzodiazepines, barbiturates, alcohol: in combination increase CNS adverse effects
2) MAO inhibitors: in combination is contraindicated; fatal reactions have occurred
3) naloxone: direct opiate antagonist
4) scorpion venom: in combination decreases toxic effects of the venom
5) any drug that inhibits cyt P450 3A4 may increase levels of sufentanil
6) any drug that induces cyt P450 3A4 may diminish levels of sufentanil
Mechanism of action:
1) opiate agonist
2) phenenylpiperidine derivative
Interactions
drug interactions
drug adverse effects (more general classes)
Related
cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
General
opiate
opioid receptor agonist (narcotic)
Properties
MISC-INFO: elimination route LIVER
1/2life 2-2.5 HOURS
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Prescriber's Letter 13(3): 2006
Cytochrome P450 drug interactions
Detail-Document#: 220233
(subscription needed) http://www.prescribersletter.com
- Brooks M
FDA Goes Ahead With Approval of Sufentanil Despite Controversy.
Medscape - Nov 02, 2018.
https://www.medscape.com/viewarticle/904330
- FDA Statement. Nove 2, 2018
Statement from FDA Commissioner Scott Gottlieb, M.D., on agency's
Dsuvia and the FDA's future consideration of new opioids.
https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm624968.htm
- FDA ADVISORY COMMITTEE BRIEFING DOCUMENT
DSUVIA (sufentanil) sublingual tablet, 30 mcg
AcelRx Briefing Document. FDA Advisory Committee Meeting
Nov, 2018
https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/AnestheticAndAnalgesicDrugProductsAdvisoryCommittee/UCM622858.pdf
Component-of
bupivacaine/citrate/sufentanil
bupivacaine/sufentanil
citrate/ropivacaine/sufentanil
ropivacaine/sufentanil