Dehydroemetine
INDICATIONS
FDA
- Amoebic dysentery as an alternative to metronidazole IV in patients unable to take oral agents or unresponsive to metronidazole
- Amoebic liver abscess unresponsive to metronidazole [no longer available from the CDC]
FORMS
brand name | preparation | manufacturer | route | form | dosage^ | cost* |
Dehydroemetine | Dehydroemetine | Roche (not available from CDC) | IV | ampule | 65/ml (1ml) | N/C |
*Prices represent cost per unit specified, are representative of "Average Wholesale Price" (AWP).
^Dosage is indicated in mg unless otherwise noted.
USUAL ADULT DOSING
1 mg/kg/day (up to 60mg/day) IM injection for up to 4-6 days. Reduce the dose by 50% in elderly and severely ill patients. All patients should also receive diloxanide PO to eliminate surviving organisms in the colon.
- Amoebic dysentery: supplementary treatment with tetracycline reduces the risk of bacterial superinfection
- Hepatic abscess:
- Supplementary treatment with chloroquine may be given concurrently or immediately afterwards.
- A repeat dose may be given 6 weeks later in patients with extensive hepatic abscesses.
- Should only be administered in a hospital setting with telemetry monitoring
ADULT RENAL DOSING
DOSING FOR GLOMERULAR FILTRATION OF 50-80
No data.
DOSING FOR GLOMERULAR FILTRATION OF 10-50
Not recommended.
DOSING FOR GLOMERULAR FILTRATION OF < 10 ML/MIN
Not recommended.
DOSING IN HEMODIALYSIS
No data.
DOSING IN PERITONEAL DIALYSIS
No data.
DOSING IN HEMOFILTRATION
No data.
PEDIATRIC DOSING
USUAL PEDIATRIC DOSING
- Children: 1 mg/kg/day IM for no more than 5 days
ADVERSE DRUG REACTIONS
GENERAL
- Note: should only be used as a last resort in patients with neuromuscular, renal or cardiac impairments given significant toxicity
- Telemetry/ECG cardiac monitoring recommended with administration; treatment should be stopped immediately if tachycardia, severe hypotension or ECG changes occur.
- Weakness and muscular pain often precede more serious toxic effects and should serve as a warning to reduce dose by 50%.
COMMON
- Arrhythmia
- Precordial pain
- Pain at injection site
- Muscle weakness
OCCASIONAL
- GI: diarrhea; vomiting
- Neuropathy
- Heart failure
- Headache
- Dyspnea
DRUG INTERACTIONS
Cardiotoxic drugs may potentiate cardiotoxicity leading to dysrhythmias.
SPECTRUM
PHARMACOLOGY
MECHANISM
Drug is similar to emetine but with fewer side effects. Inhibits polypeptide chain elongation and mammalian cells.
PHARMACOKINETIC PARAMETERS
Absorption
Rapid absorption after intramuscular administration.
Metabolism and Excretion
Slow renal excretion.
Protein Binding
No data.
Cmax, Cmin, and AUC
No data.
T1/2
Unchanged emetine may be excreted in the urine for 40-60 days after administration.
Distribution
Well distributed into liver. Also distributed into spleen, lung and kidney.
DOSING FOR DECREASED HEPATIC FUNCTION
No data.
PREGNANCY RISK
X-Contraindicated, animal and human studies shows potential of teratogenicity.
BREAST FEEDING COMPATIBILITY
Contraindicated in breast feeding.
COMMENTS
- Dehydroemetine (synthetic derivative of emetine) 65mg/ml IV (no longer available from CDC). Emetine was originally derived from ipecac root.
- Rarely used for invasive amebiasis due to severe local and systemic side effects most famously heart failure and arrhythmia (close ECG monitoring recommended) and availability of less toxic agents (e.g., metronidazole).
- May be an option in the treatment of amebic dysentery and/or extraintestinal amebiasis that fails to respond to metronidazole.
- Dehydroemetine is toxic to the fetus and is generally considered contraindicated during pregnancy. However, in cases of fulminant amoebic dysentery in late pregnancy treatment with dehydroemetine may be life-saving to the mother
Basis for recommendation
- WHO Model Prescribing Information: Drugs Used in Parasitic Diseases.
Comment: http://apps.who.int/medicinedocs/en/d/Jh2922e/2.1.3.html. Accessed 2/17/18.
References
- Jain NK, Madan A, Sharma TN, et al. Hepatopulmonary amoebiasis. Efficacy of various treatment regimens containing dehydroemetine and/or metronidazole. J Assoc Physicians India. 1990;38(4):269-71. [PMID:2202709]
Comment: The best therapeutic results were obtained with a combination of dehydroemetine and metronidazole. However, metronidazole was found to be comparable dehydroemetine.
- Yang WC, Dubick M. Mechanism of emetine cardiotoxicity. Pharmacol Ther. 1980;10(1):15-26. [PMID:6996003]
Comment: Addresses major toxicity with this drug.
- Scragg JN, Powell SJ. Emetine hydrochloride and dehydroemetine combined with chloroquine in the treatment of children with amoebic liver abscess. Arch Dis Child. 1968;43(227):121-3. [PMID:5642979]
Comment: Dehydroemetine doses as high as 2 mg/kg/day for 10 days have been given in combination with PO chloroquine for the treatment of amoebic liver abscesses in children, however, the WHO recommends a max dose of 1 mg/kg/day for a max of 5 days in children.