Fospropofol

Question 1

What are the trade names for Fospropofol?

Answer 1

Aquavan, Lusedra

Question 2

What is Fospropofol approved for?

Answer 2

MAC sedation

Question 3

What is Fospropofol? (ie. how does it work?)

Answer 3

-H2O soluble prodrug of propofol (eliminates the need for lipid formulation- responsible for the risk of pain on injection, infection, hypertriglycerides, PE)

Question 4

How is Fospropofol metabolized?

Answer 4

Hydrolyzed after injection to propofol via endothelial cell alkaline phosphatases

Question 5

What are the advantages of Fospropofol?

Answer 5

• avoiding lipid formulation related complications

- if using low doses less episodes of apnea (slower onset of peak effect)

Question 6

What are the disadvantages to Fospropofol?

Answer 6

• SLOWER peak effect, LONGER duration; may be more difficult to titrate (b/c different metabolism variability)
• Short period of tachycardia
• transient paresthesias and pruritis

Question 7

Why is Fospropofol hard to titrate?

Answer 7

Delayed time to peak effect- increases the difficulty of titrating a drug with a steep response curve and narrow margin of safety

Question 8

What type of metabolism does Fospropofol go through?

Answer 8

Non-linear metabolism to active drug:

• the higher the dose the more hydrolyzed
• the lower the dose the less hydrolyzed (less of the active metabolite propofol released)

Question 9

Compared with propofol, Fospropofol is:

Answer 9

• more potent

- higher Vd (because it is more lipid soluble once in the body)