HETRAZAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HETRAZAN (HETRAZAN).

How it works

Diethylcarbamazine (HETRAZAN) sensitizes microfilariae to phagocytosis by immobilizing them and altering their surface, making them more susceptible to destruction by host immune cells. It also has anthelminthic activity against adult worms.

What the body does with it

Metabolism	Diethylcarbamazine is rapidly absorbed and extensively metabolized in the liver via N-oxidation and N-demethylation, involving multiple CYP enzymes. The major metabolite is diethylcarbamazine N-oxide.
Excretion	Renal excretion of unchanged drug accounts for approximately 50-60% of elimination; the remainder is metabolized hepatically with metabolites excreted in urine. Fecal elimination is minimal (<5%).
Half-life	Terminal elimination half-life is 8-12 hours in patients with normal renal function; may be prolonged in renal impairment.
Protein binding	Protein binding is approximately 10-20%, primarily to albumin.
Volume of Distribution	Volume of distribution is 1.5-2.5 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is approximately 90% due to well absorption from the gastrointestinal tract.
Onset of Action	Oral: Onset of action occurs within 1-2 hours after administration for microfilaricidal effect.
Duration of Action	Duration of action is approximately 12-24 hours following a single oral dose; repeat doses are needed for sustained effect in filarial infections.

Classification & Brands

Action Class	Antiprotozoal agents
Brand Substitutes	Banocide 120mg Syrup, Deecee 120mg Syrup, Decee Syrup, Deecee AD 120mg Syrup

Dosing & administration

2 mg/kg orally three times daily after meals for 3 weeks (total dose 120 mg/kg per course). Maximum single dose: 10 mg/kg.

Dosage form	TABLET
Renal impairment	No specific GFR-based dose modifications available; use with caution in renal impairment due to potential accumulation. Monitor for adverse effects.
Liver impairment	Child-Pugh A: No adjustment needed. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Contraindicated.
Pediatric use	2 mg/kg orally three times daily after meals for 3 weeks (total dose 120 mg/kg per course). Maximum single dose: 10 mg/kg. For children <15 kg, dosage based on 1 mg/kg initially, then increase gradually.
Geriatric use	Initiate at lower end of dosing range (2 mg/kg per dose) due to potential age-related decrease in renal function. Monitor closely for adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for HETRAZAN (HETRAZAN).

Breastfeeding	Excreted into breast milk; M/P ratio unknown. Use with caution due to potential for adverse effects in infant.
Teratogenic Risk	Animal studies have not been conducted; no adequate human data. Use only if benefit outweighs risk. No known teratogenic effects in first trimester; limited data in second and third trimesters.
Fetal Monitoring	Monitor for maternal hypersensitivity reactions, hepatotoxicity, and renal function. No specific fetal monitoring required.

Warnings & precautions

■ FDA Black Box Warning

HETRAZAN is contraindicated in patients with onchocerciasis (river blindness) due to the risk of severe Mazzotti reaction, including ocular damage and encephalopathy. Treatment should not be initiated in areas where onchocerciasis is endemic or in patients with suspected onchocerciasis.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Onchocerciasis (active or suspected)","High-grade Loa loa microfilaremia (>8000 microfilariae/mL)","Hypersensitivity to diethylcarbamazine or any component of the formulation"]

Clinical Precautions

Precautions

Severe allergic or inflammatory reactions (Mazzotti reaction) in patients with onchocerciasis; encephalopathy in loiasis with high microfilarial loads; ocular damage (e.g., uveitis, optic neuritis) in onchocerciasis; thrombocytopenia; aminotransferase elevations; use in pregnancy only if clearly needed.

Clinical Tips & Counseling

Drug interactions

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HETRAZAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HETRAZAN (HETRAZAN).

How it works

What the body does with it

Metabolism	Diethylcarbamazine is rapidly absorbed and extensively metabolized in the liver via N-oxidation and N-demethylation, involving multiple CYP enzymes. The major metabolite is diethylcarbamazine N-oxide.
Excretion	Renal excretion of unchanged drug accounts for approximately 50-60% of elimination; the remainder is metabolized hepatically with metabolites excreted in urine. Fecal elimination is minimal (<5%).
Half-life	Terminal elimination half-life is 8-12 hours in patients with normal renal function; may be prolonged in renal impairment.
Protein binding	Protein binding is approximately 10-20%, primarily to albumin.
Volume of Distribution	Volume of distribution is 1.5-2.5 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is approximately 90% due to well absorption from the gastrointestinal tract.
Onset of Action	Oral: Onset of action occurs within 1-2 hours after administration for microfilaricidal effect.
Duration of Action	Duration of action is approximately 12-24 hours following a single oral dose; repeat doses are needed for sustained effect in filarial infections.

Classification & Brands

Action Class	Antiprotozoal agents
Brand Substitutes	Banocide 120mg Syrup, Deecee 120mg Syrup, Decee Syrup, Deecee AD 120mg Syrup

Dosing & administration

2 mg/kg orally three times daily after meals for 3 weeks (total dose 120 mg/kg per course). Maximum single dose: 10 mg/kg.

Dosage form	TABLET
Renal impairment	No specific GFR-based dose modifications available; use with caution in renal impairment due to potential accumulation. Monitor for adverse effects.
Liver impairment	Child-Pugh A: No adjustment needed. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Contraindicated.
Pediatric use	2 mg/kg orally three times daily after meals for 3 weeks (total dose 120 mg/kg per course). Maximum single dose: 10 mg/kg. For children <15 kg, dosage based on 1 mg/kg initially, then increase gradually.
Geriatric use	Initiate at lower end of dosing range (2 mg/kg per dose) due to potential age-related decrease in renal function. Monitor closely for adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for HETRAZAN (HETRAZAN).

Breastfeeding	Excreted into breast milk; M/P ratio unknown. Use with caution due to potential for adverse effects in infant.
Teratogenic Risk	Animal studies have not been conducted; no adequate human data. Use only if benefit outweighs risk. No known teratogenic effects in first trimester; limited data in second and third trimesters.
Fetal Monitoring	Monitor for maternal hypersensitivity reactions, hepatotoxicity, and renal function. No specific fetal monitoring required.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["Onchocerciasis (active or suspected)","High-grade Loa loa microfilaremia (>8000 microfilariae/mL)","Hypersensitivity to diethylcarbamazine or any component of the formulation"]