LIPO GANTRISIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIPO GANTRISIN (LIPO GANTRISIN).

How it works

Lipo Gantrisin is a liposomal formulation of sulfisoxazole, a sulfonamide antibiotic. It inhibits bacterial dihydropteroate synthase, blocking folate synthesis and thereby bacterial DNA replication.

What the body does with it

Metabolism	Primarily metabolized via acetylation and glucuronidation in the liver; undergoes enterohepatic recirculation.
Excretion	Lipo Gantrisin is excreted primarily renally (70-80%) as unchanged drug and its acetylated metabolite. Biliary/fecal elimination accounts for 20-30%, with enterohepatic recirculation present.
Half-life	The terminal elimination half-life is approximately 7-12 hours in adults with normal renal function; prolonged to 20-50 hours in renal impairment (CrCl <30 mL/min). This necessitates dose adjustment in renal disease.
Protein binding	Approximately 60-70% bound to plasma albumin.
Volume of Distribution	Apparent volume of distribution is 0.2-0.4 L/kg, indicating distribution primarily into extracellular fluid. It does not significantly penetrate the CNS or prostate.
Bioavailability	Oral bioavailability is 85-95% after tablet administration. Suspension has slightly lower bioavailability (80-90%) due to food effects.
Onset of Action	Peak serum concentrations occur within 2-4 hours after oral administration; bacteriostatic effect begins within 12-24 hours after achieving therapeutic levels. For intravenous administration, onset is immediate with therapeutic levels reached within 30 minutes.
Duration of Action	The bacteriostatic effect persists for 12-24 hours, supporting twice-daily dosing. Clinical improvement in urinary tract infections is typically seen within 48-72 hours.

Classification & Brands

Dosing & administration

2-4 mL (80-160 mg sulfisoxazole equivalent) intramuscularly every 12 hours for 5-7 days.

Dosage form	EMULSION
Renal impairment	CrCl 30-60 mL/min: administer every 18-24 hours; CrCl 15-29 mL/min: administer every 24-48 hours; CrCl <15 mL/min or dialysis: administer every 48-72 hours.
Liver impairment	Child-Pugh class A: no adjustment; Child-Pugh class B: reduce dose by 25%; Child-Pugh class C: reduce dose by 50%.
Pediatric use	Infants and children: 50-75 mg/kg of sulfisoxazole equivalent intramuscularly every 12 hours; maximum 6 mL per dose.
Geriatric use	Reduce dose by 25-50% due to age-related decline in renal function; monitor renal function and serum levels.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for LIPO GANTRISIN (LIPO GANTRISIN).

Breastfeeding	Sulfisoxazole (component) excreted in breast milk; M/P ratio approximately 0.3. Avoid in nursing mothers of ill, premature, or glucose-6-phosphate dehydrogenase deficient infants due to potential kernicterus and hemolysis. Although low levels, caution recommended.
Teratogenic Risk	FDA Pregnancy Category C. In animals, sulfonamides cause cleft palate and other fetal malformations at high doses. Human data limited: first trimester use associated with small increased risk of neural tube defects; third trimester use contraindicated due to risk of kernicterus in newborn. Avoid in pregnancy near term.

Warnings & precautions

■ FDA Black Box Warning

Sulfonamides, including sulfisoxazole, have been associated with fatal reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Hypersensitivity reactions may occur even with prior use.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to sulfonamides or any component of the formulation","Infants <2 months of age (except for congenital toxoplasmosis)","Pregnancy at term and breastfeeding (risk of kernicterus)","Concurrent use with methenamine (risk of crystalluria)","Severe renal or hepatic impairment"]

Clinical Precautions

Precautions

Monitor for severe hypersensitivity reactions (e.g., Stevens-Johnson syndrome). Use caution in patients with renal impairment (dose adjustment required), hepatic impairment, G6PD deficiency (risk of hemolytic anemia), and porphyria. Avoid use in infants <2 months due to risk of kernicterus. Maintain adequate hydration to prevent crystalluria.

Clinical Tips & Counseling

Drug interactions

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LIPO GANTRISIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIPO GANTRISIN (LIPO GANTRISIN).

How it works

Lipo Gantrisin is a liposomal formulation of sulfisoxazole, a sulfonamide antibiotic. It inhibits bacterial dihydropteroate synthase, blocking folate synthesis and thereby bacterial DNA replication.

What the body does with it

Metabolism	Primarily metabolized via acetylation and glucuronidation in the liver; undergoes enterohepatic recirculation.
Excretion	Lipo Gantrisin is excreted primarily renally (70-80%) as unchanged drug and its acetylated metabolite. Biliary/fecal elimination accounts for 20-30%, with enterohepatic recirculation present.
Half-life	The terminal elimination half-life is approximately 7-12 hours in adults with normal renal function; prolonged to 20-50 hours in renal impairment (CrCl <30 mL/min). This necessitates dose adjustment in renal disease.
Protein binding	Approximately 60-70% bound to plasma albumin.
Volume of Distribution	Apparent volume of distribution is 0.2-0.4 L/kg, indicating distribution primarily into extracellular fluid. It does not significantly penetrate the CNS or prostate.
Bioavailability	Oral bioavailability is 85-95% after tablet administration. Suspension has slightly lower bioavailability (80-90%) due to food effects.
Onset of Action	Peak serum concentrations occur within 2-4 hours after oral administration; bacteriostatic effect begins within 12-24 hours after achieving therapeutic levels. For intravenous administration, onset is immediate with therapeutic levels reached within 30 minutes.
Duration of Action	The bacteriostatic effect persists for 12-24 hours, supporting twice-daily dosing. Clinical improvement in urinary tract infections is typically seen within 48-72 hours.

Classification & Brands

Dosing & administration

2-4 mL (80-160 mg sulfisoxazole equivalent) intramuscularly every 12 hours for 5-7 days.

Dosage form	EMULSION
Renal impairment	CrCl 30-60 mL/min: administer every 18-24 hours; CrCl 15-29 mL/min: administer every 24-48 hours; CrCl <15 mL/min or dialysis: administer every 48-72 hours.
Liver impairment	Child-Pugh class A: no adjustment; Child-Pugh class B: reduce dose by 25%; Child-Pugh class C: reduce dose by 50%.
Pediatric use	Infants and children: 50-75 mg/kg of sulfisoxazole equivalent intramuscularly every 12 hours; maximum 6 mL per dose.
Geriatric use	Reduce dose by 25-50% due to age-related decline in renal function; monitor renal function and serum levels.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for LIPO GANTRISIN (LIPO GANTRISIN).

Breastfeeding	Sulfisoxazole (component) excreted in breast milk; M/P ratio approximately 0.3. Avoid in nursing mothers of ill, premature, or glucose-6-phosphate dehydrogenase deficient infants due to potential kernicterus and hemolysis. Although low levels, caution recommended.
Teratogenic Risk	FDA Pregnancy Category C. In animals, sulfonamides cause cleft palate and other fetal malformations at high doses. Human data limited: first trimester use associated with small increased risk of neural tube defects; third trimester use contraindicated due to risk of kernicterus in newborn. Avoid in pregnancy near term.