Sufentanil

Question 1

Sufentanil: Brand Name

Answer 1

Sufenta

Question 2

Sufentanil: drug class

Answer 2

Phenylpiperidine - synthetic opioid agonist

Question 3

Sufentanil: Mechanism of Action

Answer 3

acts on Mu.
Gi GPCR

Inhibition of adenylate cyclase

↓ cAMP

Closure of voltage-gated calcium channels

Opening of potassium channels

Hyperpolarization of neurons

Question 4

Opioid receptor that sufentanil binds to and its effects

Answer 4

Mu receptor activation.
Mu 1- Supraspinal analgesiaBradycardiaSedationPruritusNausea and vomiting
Mu 2 - Respiratory depressionEuphoriaPhysical dependencePruritusConstipation

Question 5

General pharmacokinetics

Answer 5

VERY lipophilic (2x more then fentanyl). 10x more potent then fentanyl.
Large Vd.
Highly protein bound to a1-acid glycoprotein.
Duration of action is slightly shorter then fentanyl.
Undergoes 1st pass pulmonary effect

Question 6

Sufentanil metabolism

Answer 6

Primarily through CYP enzymes into inactive metabolites

Question 7

Sufentanil elimination

Answer 7

renal excretion

Question 8

Side effects

Answer 8

similar to fentanyl, due to high lipophilicity it can also cause rigid chest syndrome.

Question 9

Dose

Answer 9

(Not stated on lecture powerpoint) per stoeltings 0.1-0.4 mcg/kg