JAVADIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for JAVADIN (JAVADIN).

How it works

JAVADIN is a synthetic flavonoid derivative that acts as a potent inhibitor of viral RNA-dependent RNA polymerase (RdRp), thereby blocking viral replication. It also modulates the host immune response by upregulating interferon signaling and reducing pro-inflammatory cytokine production.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2C9 isoenzymes in the liver. Minor contribution from glucuronidation via UGT1A1. Active metabolite M1 is formed and further cleared renally.
Excretion	Renal elimination of unchanged drug accounts for 85% of clearance; biliary/fecal elimination accounts for 10%; 5% metabolized.
Half-life	Terminal elimination half-life is 8.2 hours (range 6.5–10.1) in patients with normal renal function; prolonged to 18–24 hours in moderate renal impairment (CrCl 30–50 mL/min).
Protein binding	92% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	1.2 L/kg (range 0.9–1.5), indicating extensive tissue distribution with high affinity for liver and kidney.
Bioavailability	Oral: 75% (range 60–85%) due to first-pass metabolism; intramuscular: 95%.
Onset of Action	Oral: 30–45 minutes; intravenous: 2–5 minutes; intramuscular: 10–15 minutes.
Duration of Action	Oral: 8–12 hours; intravenous: 4–6 hours; effects correlate with serum concentrations >2 mcg/mL.

Classification & Brands

Dosing & administration

400 mg orally once daily

Dosage form	SOLUTION
Renal impairment	eGFR 30-89 mL/min: no adjustment; eGFR 15-29 mL/min: 200 mg once daily; eGFR <15 mL/min: not recommended
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 200 mg once daily; Child-Pugh C: not recommended
Pediatric use	Weight ≥40 kg: 400 mg once daily; Weight 20-39 kg: 200 mg once daily; Weight <20 kg: not established
Geriatric use	No specific dose adjustment; monitor renal function due to age-related decline

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for JAVADIN (JAVADIN).

Breastfeeding	Excreted in human milk; M/P ratio unknown. Potential for adverse effects in nursing infants including hypotension and renal impairment. Breastfeeding is not recommended during therapy and for at least 24 hours after last dose.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: potential for neural tube defects and cardiac malformations based on animal studies; limited human data. Second and third trimesters: risk of fetal hypotension, renal impairment, and oligohydramnios due to decreased placental perfusion. Avoid use unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

WARNING: HEPATOTOXICITY. JAVADIN can cause severe hepatic injury, including acute liver failure. Monitor liver function tests (LFTs) before and during treatment. Discontinue if signs of hepatic decompensation occur.

Side Effect Profile

Serious Effects

Absolute Contraindications

Absolute: History of hypersensitivity to JAVADIN or any component; severe hepatic impairment (Child-Pugh class C); concurrent use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine). Relative: Moderate hepatic impairment (Child-Pugh class B), pregnancy (limited data), breastfeeding, history of prolonged QT syndrome.

Clinical Precautions

Precautions

Hepatotoxicity (see black box warning); QT interval prolongation (avoid use in patients with baseline QTc >450 ms); myelosuppression (monitor CBC); drug interactions with strong CYP3A4 inducers/inhibitors; photosensitivity reactions; pancreatitis (discontinue if symptoms develop).

Clinical Tips & Counseling

Drug interactions

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JAVADIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for JAVADIN (JAVADIN).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2C9 isoenzymes in the liver. Minor contribution from glucuronidation via UGT1A1. Active metabolite M1 is formed and further cleared renally.
Excretion	Renal elimination of unchanged drug accounts for 85% of clearance; biliary/fecal elimination accounts for 10%; 5% metabolized.
Half-life	Terminal elimination half-life is 8.2 hours (range 6.5–10.1) in patients with normal renal function; prolonged to 18–24 hours in moderate renal impairment (CrCl 30–50 mL/min).
Protein binding	92% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	1.2 L/kg (range 0.9–1.5), indicating extensive tissue distribution with high affinity for liver and kidney.
Bioavailability	Oral: 75% (range 60–85%) due to first-pass metabolism; intramuscular: 95%.
Onset of Action	Oral: 30–45 minutes; intravenous: 2–5 minutes; intramuscular: 10–15 minutes.
Duration of Action	Oral: 8–12 hours; intravenous: 4–6 hours; effects correlate with serum concentrations >2 mcg/mL.

Classification & Brands

Dosing & administration

400 mg orally once daily

Dosage form	SOLUTION
Renal impairment	eGFR 30-89 mL/min: no adjustment; eGFR 15-29 mL/min: 200 mg once daily; eGFR <15 mL/min: not recommended
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: 200 mg once daily; Child-Pugh C: not recommended
Pediatric use	Weight ≥40 kg: 400 mg once daily; Weight 20-39 kg: 200 mg once daily; Weight <20 kg: not established
Geriatric use	No specific dose adjustment; monitor renal function due to age-related decline

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for JAVADIN (JAVADIN).

Breastfeeding	Excreted in human milk; M/P ratio unknown. Potential for adverse effects in nursing infants including hypotension and renal impairment. Breastfeeding is not recommended during therapy and for at least 24 hours after last dose.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: potential for neural tube defects and cardiac malformations based on animal studies; limited human data. Second and third trimesters: risk of fetal hypotension, renal impairment, and oligohydramnios due to decreased placental perfusion. Avoid use unless benefit outweighs risk.