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fospropofol (Lusedra)

 

Classes: General Anesthetics, Systemic

Dosing and uses of Lusedra (fospropofol)

 

Adult dosage forms and strengths

This drug has been discontinued in the United States

 

Pediatric dosage forms and strengths

N/A

 

Lusedra (fospropofol) adverse (side) effects

>10%

Paresthesia

Pruritus

Hypoxemia

 

1-10%

Headache

Hypotension

Nausea/vomiting

Unresponsiveness to tactile or nociceptive stimuli

 

Warnings

Contraindications

Hypersensitivity

Situations where general anesthesia is contraindicated

 

Cautions

May cause loss of spontaneous respiration, hypoxemia, hypotension

Not recommended for labor & delivery

Caution in respiratory disease

Patient may become unresponsive or minimally responsive to painful stimuli

Caution in hepatic or renal impairment

 

Pregnancy and lactation

Pregnancy category: B

Lactation: enters breast milk; not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Lusedra (fospropofol)

Mechanism of action

Sedative-hypnotic, prodrug of propofol; interacts with GABA A receptor

 

Pharmacokinetics

Peak Plasma Time: 2-4 min to propofol; 8-12 min of propofol from fospropofol:

Protein Bound: 98%

Onset: ~8 min

Half-life: 0.8-0.96 hr

Duration: ~5 min (time to fully alert)

Vd: 0.26-0.4 L/kg

Metabolism: by alk phos to propofol, formaldehyde & phosphate

Excretion: Urine

 

Administration

IV Incompatibilities: midazolam; meperidine

 

IV Administration

Ready-to-use formulation

Administer through a secure, freely flowing, peripheral line

Flush infusion line with NS before & after administration

Compatible common fluids: D5W, D5/0.2%NaCl, D5/0.5NS, D5/LR, LR, NS, 0.5Ns

Do not coadminister other drugs