Eflornithine
Eflornithine (HCl) is an antiprotozoal agent. Eflornithine (HCl) is used in the treatment of African trypanosomiasis and is effective in early and more importantly in late stages of this disease when there is CNS involvement. It acts as an irreversible inhibitor of ornithine decarboxylase, the rate-limiting enzyme in the biosynthesis; trypanosomas are more susceptible yo the effect of eflornithine. It also has activity against Pneuocystis carinii.
Primary Characteristics
Eflornithine is also known as Eflornithine (HCl).
It is of Synthetic origin and belongs to Difluoromethyl Ornithine.
Molecular Weight: 236.6 · Solubility in Water: freely soluble · Solubility in Alcohol: sparingly soluble · Non-proprietary name: Eflornithine.

Pharmacokinetics
Absorption: Eflornithine has an oral bioavailability is 27.5% (±27.5%).
Distribution: Eflornithine has a volume of distribution is 0.34 l/kg. plasma protein binding is not significant.
Elimination: plasma half-life is 3.4 hr, renal excretion is 80% (IV), 45% (oral) unchanged.
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Indications
Eflornithine is primarily indicated in conditions like Meningoencephalitic intrypanosoma brucei infection, Sleeping sickness., Trypanosomiasis.
Contraindications
Eflornithine is contraindicated in conditions like Hypersensitivity to the drug.
Dosage
Eflornithine's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 100 mg/kg | 100 mg/kg | — | IV | every 6hr for 7-14 day. |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
None recorded.
Side Effects
Eflornithine in overdosage may give rise to further complications which include Anemia , Anemia , Thrombocytopenia , Skin rashes , Leucopenia, Seizures , Irritation , Anemia, Anemia.
Eflornithine produces potentially life-threatening effects which include Cardiac Arrest , Cardiac arrest. Careful monitoring is needed with proper medical management.
Eflornithine is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Alopecia, Anorexia , Asthenia , Diarrhea, Dizziness, Facial edema, Folliculitis, Headache, Vomiting .
Warnings / Precautions
Interference in Pathology
Eflornithine may interfere in the diagnosis of Increased in Serum Aminotransferase.
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.6.4.4 — Antitrypanosomal drugs