Comparative Pharmacology
Head-to-head clinical analysis: CLOPRA versus FOSAPREPITANT DIMEGLUMINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CLOPRA versus FOSAPREPITANT DIMEGLUMINE.
CLOPRA vs FOSAPREPITANT DIMEGLUMINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Clopra (metoclopramide) is a dopamine D2 receptor antagonist and a 5-HT4 receptor agonist, enhancing gastrointestinal motility and having antiemetic effects via central and peripheral actions.
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.
Clopra (metoclopramide) 10 mg orally or intramuscularly 30 minutes before meals and at bedtime; maximum 30 mg/day. For intravenous administration, give 10 mg over 1-2 minutes.
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.
None Documented
None Documented
Clinical Note
moderateMetoclopramide + Haloperidol
"The risk or severity of adverse effects can be increased when Metoclopramide is combined with Haloperidol."
Clinical Note
moderateMetoclopramide + Quinagolide
"The therapeutic efficacy of Quinagolide can be decreased when used in combination with Metoclopramide."
Clinical Note
moderateMetoclopramide + Cyclosporine
"Metoclopramide can cause an increase in the absorption of Cyclosporine resulting in an increased serum concentration and potentially a worsening of adverse effects."
Clinical Note
moderateTerminal elimination half-life 6-8 hours (prolonged in renal impairment; up to 20 hours in severe CKD)
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.
Renal (50-70% as unchanged drug and metabolites); fecal (20-30%); biliary (minor ~5%)
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).
Category C
Category C
Antiemetic/Prokinetic Agent
Antiemetic
Metoclopramide + Clotrimazole
"The metabolism of Clotrimazole can be decreased when combined with Metoclopramide."