Comparative Pharmacology
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus PROMETHAZINE W CODEINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus PROMETHAZINE W CODEINE.
FOSAPREPITANT DIMEGLUMINE vs PROMETHAZINE W/ CODEINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Fosaprepitant dimeglumine is a prodrug of aprepitant, a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. It inhibits emesis by blocking NK1 receptors in the central nervous system, particularly in the area postrema and the nucleus tractus solitarius.
Codeine is a prodrug converted to morphine, a mu-opioid receptor agonist, which inhibits nociceptive transmission; promethazine is a phenothiazine derivative with H1-receptor antagonism, anticholinergic, and antiemetic effects.
150 mg intravenous over 30 minutes on day 1, combined with dexamethasone and a 5-HT3 antagonist; alternatively, 115 mg IV on day 1 followed by 80 mg IV on day 2 and 80 mg IV on day 3, or 150 mg oral (as fosaprepitant dimeglumine or aprepitant) on day 1 and 80 mg oral on days 2 and 3.
10 mL (1 mg codeine, 6.25 mg promethazine per 5 mL) orally every 4-6 hours as needed for cough. Maximum: 60 mL per day. Do not exceed 5 days.
None Documented
None Documented
Terminal elimination half-life of aprepitant is approximately 9 to 13 hours; clinical significance includes once-daily dosing for prevention of chemotherapy-induced nausea and vomiting.
Promethazine: 10-19 hours (terminal). Codeine: 2.5-3.5 hours (terminal); prolonged in renal impairment.
Fosaprepitant is rapidly converted to aprepitant. Aprepitant is eliminated primarily by metabolism; <5% of the dose is excreted unchanged in urine. Fecal excretion accounts for approximately 58% of the dose, and urinary excretion accounts for 43% (mostly as metabolites).
Promethazine: renal (70% as metabolites, <1% unchanged), fecal (20-30%). Codeine: renal (90%, of which 5-10% unchanged, rest as metabolites), fecal (minor).
Category C
Category A/B
Antiemetic
Antihistamine / Antiemetic