miltefosine

Contraindicated in:

Hypersensitivity;
Sjögren-Larsson syndrome (due to metabolic defect);
OB: Pregnancy;
OB: Lactation.

Use Cautiously in:

Renal impairment;
Hepatic impairment;
Rep: Women of reproductive potential;
Pedi: Children <12 yr (safety and effectiveness not established).

Adv. Reactions/Side Effects ⬆ ⬇

Derm: pruritus, STEVENS-JOHNSON SYNDROME, urticaria

F and E: volume depletion

GI: ↓appetite, abdominal pain, diarrhea, vomiting, ↑liver enzymes, abdominal distention, constipation, dysphagia, flatulence, nausea

GU: ↓fertility (males), ↑serum creatinine, testicular pain/swelling

Hemat: anemia, thrombocytopenia

Neuro: dizziness, drowsiness, headache, weakness

Misc: fever, lymphadenopathy, lymphangitis

Interactions ⬆ ⬇

Drug-drug:

Vomiting and/or diarrhea may ↓ absorption and effectiveness of oral contraceptives..

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults and Children ≥12 yr and ≥45 kg): 50 mg three times daily for 28 consecutive days.
PO (Adults and Children ≥12 yr and 30–<45 kg): 50 mg twice daily for 28 consecutive days.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Interacts with lipids and sterols in the Leishmania membrane resulting in inhibition of mitochondria and apoptotic cell death.

Therapeutic effects:

Resolution of Leishmania infections.

Spectrum:

Active against the following organisms:
- Leishmania braziliensis,
- Leishmania donovani,
- Leishmania guyanensis,
- Leishmania panamensis.

Classifications ⬆ ⬇

Therapeutic Classification: antileishmanials

Pharmacologic Classification: alkylphosphocholines

Pharmacokinetics ⬆ ⬇

Absorption: Absorption is prolonged and may persist for 8–12 hr.

Distribution: Unknown.

Protein Binding: 98%.

Metabolism/Excretion: Slowly broken down in the liver, releasing choline; remaining portion is further metabolized and enters fatty acid metabolism; <0.2% excreted in urine.

Half-Life: >6 days.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4–7 hr (blood level)	unknown‡

‡Persists in the body for up to 5 mo.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed for 28 consecutive days.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise patient to notify health care professional immediately if skin rash with blisters occurs. Discontinue therapy if exfoliative or bullous rash occurs.
May cause dizziness and drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
Instruct patient to notify health care professional if abdominal pain, nausea, vomiting, or diarrhea are persistent or severe. Advise to maintain hydration to prevent kidney damage.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception and avoid breastfeeding during and for ≥5 mo after last dose of therapy. Nausea and vomiting may ↓ absorption of oral hormonal contraceptives. Advise patient to use a nonhormonal or alternative method of effective contraception. May cause scrotal pain and ↓ or absent ejaculation in males, impairing fertility, usually improved within 3–6 mo. May also impair female fertility.

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Indications ⬇

Contraind./Precautions ⬆ ⬇