Dehydroemetine

Janessa Smith, Pharm.D., BCPS
Pediatric Dosing Author: Alice Jenh Hsu, PharmD, BCPS, AQ-ID

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

Entamoeba histolytica

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

  1. 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

  1. Jain NK et al: Hepatopulmonary amoebiasis. Efficacy of various treatment regimens containing dehydroemetine and/or metronidazole. J Assoc Physicians India 38:269, 1990  [PMID:2202709]

    Comment: The best therapeutic results were obtained with a combination of dehydroemetine and metronidazole. However, metronidazole was found to be comparable dehydroemetine.

  2. Yang WC, Dubick M: Mechanism of emetine cardiotoxicity. Pharmacol Ther 10:15, 1980  [PMID:6996003]

    Comment: Addresses major toxicity with this drug.

  3. Scragg JN, Powell SJ: Emetine hydrochloride and dehydroemetine combined with chloroquine in the treatment of children with amoebic liver abscess. Arch Dis Child 43:121, 1968  [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.

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Last updated: April 9, 2018

Citation

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TY - ELEC T1 - Dehydroemetine ID - 540187 A1 - Smith,Janessa,Pharm.D., BCPS Y1 - 2018/04/09/ PB - Johns Hopkins ABX Guide UR - https://www.hopkinsguides.com/hopkins/view/Johns_Hopkins_ABX_Guide/540187/all/Dehydroemetine ER -