Diethylcarbamazine, Uses, Dosage, Side Effects, Interactions

The mechanism of action of diethylcarbamazine is thought to involve sensitizing the microfilariae to phagocytosis. One study showed that diethylcarbamazine’s activity against Brugia malayi microfilariae is dependent on inducible nitric-oxide synthase and the cyclooxygenase pathway. It confirmed the important role of the arachidonic acid metabolic pathway in diethylcarbamazine’s mechanism of action in vivo and showed that in addition to its effects on the 5-lipoxygenase pathway, it targets the cyclooxygenase pathway and COX-1.

Indications of Diethylcarbamazine

• Used for the treatment of certain filarial diseases, including tropical pulmonary eosinophilia, loiasis, and lymphatic filariasis caused by infection with Wuchereria bancrofti, Brugia malayi, or Brugia timori.
• DEC is indicated for the treatment of individual patients with certain filarial diseases, including lymphatic filariasis caused by infection with Wuchereria bancrofti, Brugia malayi, or Brugia timori; tropical pulmonary eosinophilia; and loiasis.
• In cases of onchocerciasis, another common filarial parasite, the drug is effective.
• DEC continues to be the mainstay for treatment of patients with lymphatic filariasis and loiasis. DEC is also used to prevent heartworm in dogs.

Now, the WHO recommends prescribing DEC to patients who are infected with microfilariae of filarial parasites and also to control the transmission of infection in filariasis-endemic areas.

• Filaricides; Lipoxygenase Inhibitors
• Diethylcarbamazine citrate is usually admin by mouth as tablets. It has also been given by intramuscular injection.
• For mass treatment against microfilariae of Wucereria bancrofti and Wuchereria malayi/ with the objective of reducing microfilaremia to subinfective levels for mosquitoes, the dose is 2 mg/kg, three times daily after meals, for 7 days for treatment directed toward a possible cure, this dosage regimen is carried out for 10 to 30 days. … For practical purposes, an adequate amount seems to be a total dose of about 72 mg/kg of the citrate salt.
• For treatment against Loa loa microfilariae, a dose of 2 mg kg should be given 3 times daily after meals for 2 to 3 weeks. If repeated courses are required to produce a cure, they should be separated by periods of 3 to 4 weeks.
• For treatment against Onchocerca volvulus, treatment is effective in removing microfilariae from the skin; however, they usually return after some weeks because the adult worms are not killed. When lesions of the eye are present, the initial dose of diethylcarbamazine should not exceed 0.5 mg/kg. This is given once on the first day and twice on the second. The dose is then increased to 1 mg/kg three times daily for the third day, and therapy is continued up to a total of 14 days with a dose of 2 to 3 mg/kg in two divided doses each day.
• Diethylcarbamazine can be used effectively to treat infections caused by Wuchereria bancrofti, Wuchereria malayi, Loa loa, and Onchocerca volvulus. In the first three, radical cure can be achieved by either single or multiple courses of treatment. In onchocerciasis, the radical cure is unlikely because the drug fails to kill the adult worms. Control can be achieved by short periodic courses of treatment. The drug has also been used effectively to treat filariasis due to Tetrapetalonema perstans or Tetrapetalonema streptococcal.
• Diethylcarbamazine is also effective in clearing Ascaris infections, but it has been replaced by other agents for this purpose.
• Diethylcarbamazine, 3 mg/kg/body wt three times daily for 21 days was used successfully in 21 patients with eye infections due to Toxocara canis or Toxocara cati, which without such diagnosis would have been confused with the presence of retinoblastoma requiring removal of the affected eye. Diethylcarbamazine
• In patients with eosinophilic lung (tropical eosinophilia), treatment with diethylcarbamazine causes a rapid disappearance of symptoms. This and the finding of microfilariae in lung biopsies suggests an association between filariasis and certain pulmonary syndromes.

Contraindications of Diethylcarbamazine

• Lower seizure threshold
• Eye complications caused by the worm Onchocerca volvulus
• Kidney disease with a reduction in kidney function
• Abnormal liver function tests
• Kidney disease with a reduction in kidney function
• Diarrhea
• The high amount of magnesium in the blood
• Low amount of sodium in the blood
• Extreme loss of body water
• Appendicitis
• Stomach or intestine blockage
• Seizures
• Pregnancy
• Allergies to Diethylcarbamazine

Dosage of Diethylcarbamazine

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For Bancroft’s filariasis, loiasis, and river blindness

• Adults – Dose is based on body weight and must be determined by your doctor. The usual dose is 2 to 3 milligrams (mg) per kilogram (kg) (0.9 to 1.3 mg per pound) of body weight three times a day.
• Children – Use and dose must be determined by your doctor.

For eosinophilic lung

• Adults – Dose is based on body weight and must be determined by your doctor. The usual dose is 6 mg per kg (2.7 mg per pound) of body weight a day. This is taken for four to seven days.
• Children -Use and dose must be determined by your doctor.

Side Effects of Diethylcarbamazine

More common

• Signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
• Painful and tender glands in the neck, armpits, or groin
• Skin rash itching and swelling of the face, especially the eyes
• Fever, itching or skin rash
• Joint or muscle pain
• Burning feeling of the skin
• Dry skin
•  Itchiness
• Skin irritation
• Severe skin irritation
• Painful and tender glands in neck, armpits, or groin
• Rapid heartbeat

Less common

• swelling of the face, hands, arms, feet, or legs
• Diarrhea
• Headache
• Joint pain
• Nausea or vomiting unusual tiredness or weakness
• Dizziness
• Skin rash or itching
• Lightheadedness when getting up from a lying or sitting position

Rare

• Loss of appetite
• shaking or trembling
• sleepiness
• change in vision
• chest pain or tightness
• confusion
• a cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• a headache
• irritability
• lightheadedness

Drug Interactions of Diethylcarbamazine

Diethylcarbamazine may interact with following drugs, supplements, & may change the efficacy of the drug

• aluminum hydroxide
• aspirin
• Butalbital
• Butabarbital
• Carvedilol
• Clozapine
• Clobetasol
• Clevidipine
• Chlorpromazine
• dextroamphetamine
• albendazole
• diphenhydramine
• Chlorphenoxamine
• praziquantel
• prednisone
• pyrantel
• quinamide
• Bisoprolol
• Betamethasone
• Vitamin B Complex 100 (multivitamin)
• Vitamin B12 (cyanocobalamin)
• Vitamin D3 (cholecalciferol)
• Alprazolam
• Cetirizine
• voriconazole
• Betaxolol
• Betamethasone phosphate
• tacrolimus
• Deflazacort
• Desipramine
• desloratadine
• dexamethasone
• Hydrocortisone
• telaprevir
• telithromycin
• temsirolimus
• nelfinavir
• nevirapine
• nilotinib
• oxcarbazepine
• posaconazole
• rufinamide
• stiripentol
• escitalopram
• modafinil
• saquinavir
• nefazodone
• warfarin

Pregnancy Category of Diethylcarbamazine

FDA Pregnancy Category: X

Pregnancy

Treatment of pregnant patients with diethylcarbamazine should be deferred until after delivery. However, problems in humans have not been documented.

Breast-feeding

It is not known whether diethylcarbamazine is distributed into breast milk. However, problems in humans have not been documented. Appropriate studies on the relationship of age to the effects of diethylcarbamazine have not been performed in the pediatric population. However, no pediatrics-specific problems have been documented to date.

References