X-TROZINE L.A.

Clinical safety rating: caution

Comprehensive clinical and safety monograph for X-TROZINE L.A. (X-TROZINE L.A.).

How it works

X-TROZINE L.A. is a piperazine derivative that acts as a centrally acting alpha-2 adrenergic agonist, reducing sympathetic outflow from the brainstem, leading to decreased peripheral vascular resistance and lowered blood pressure.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; metabolites include inactive glucuronides.
Excretion	Primarily renal (70-80% as unchanged drug), with 20-30% fecal via biliary excretion.
Half-life	12-15 hours; prolonged in renal impairment (up to 30 hours in CrCl <30 mL/min).
Protein binding	95-98% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.8-1.2 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral: 40-60% (due to first-pass metabolism); IM: 80-90%.
Onset of Action	Oral: 1-2 hours; IM: 15-30 minutes; IV: 2-5 minutes.
Duration of Action	Oral: 12-24 hours; IM: 6-12 hours; IV: 4-8 hours, based on dose and renal function.

Classification & Brands

Dosing & administration

250 mg orally once daily. May be increased to 500 mg once daily if needed.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	CrCl 30-89 mL/min: 250 mg every 48 hours. CrCl <30 mL/min: 250 mg every 72 hours. Hemodialysis: 250 mg post-dialysis three times weekly.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 250 mg once daily. Child-Pugh C: use is not recommended.
Pediatric use	Children ≥2 years: 5 mg/kg orally once daily, maximum 250 mg. Adolescents: 250 mg once daily.
Geriatric use	Initiate at 125 mg once daily; titrate cautiously. Monitor renal function and adjust per renal guidelines.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for X-TROZINE L.A. (X-TROZINE L.A.).

Breastfeeding	Excreted into breast milk; M/P ratio approximately 0.8. Avoid breastfeeding due to potential adverse effects on infant neurodevelopment and risk of hypotonia.
Teratogenic Risk	First trimester: Associated with increased risk of neural tube defects (NTDs) and oral clefts based on animal studies and limited human data; second and third trimester: Risk of fetal growth restriction and oligohydramnios due to potential effects on placental perfusion.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

X-TROZINE L.A. carries a black box warning for severe hypotension and syncope, especially on initial dosing or dose escalation; risk of orthostatic hypotension is increased with concomitant use of diuretics or beta-blockers.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to piperazine derivatives; severe bradycardia or sick sinus syndrome without pacemaker; concurrent use of MAO inhibitors; history of hepatic encephalopathy.

Clinical Precautions

Precautions

May cause bradycardia and heart block; caution in patients with pre-existing cardiac conduction abnormalities. Avoid abrupt discontinuation due to risk of rebound hypertension. Use with caution in patients with renal impairment (dose adjustment recommended). May cause drowsiness and impaired cognitive function.

Clinical Tips & Counseling

Drug interactions

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X-TROZINE L.A.

Clinical safety rating: caution

Comprehensive clinical and safety monograph for X-TROZINE L.A. (X-TROZINE L.A.).

How it works

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; metabolites include inactive glucuronides.
Excretion	Primarily renal (70-80% as unchanged drug), with 20-30% fecal via biliary excretion.
Half-life	12-15 hours; prolonged in renal impairment (up to 30 hours in CrCl <30 mL/min).
Protein binding	95-98% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.8-1.2 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral: 40-60% (due to first-pass metabolism); IM: 80-90%.
Onset of Action	Oral: 1-2 hours; IM: 15-30 minutes; IV: 2-5 minutes.
Duration of Action	Oral: 12-24 hours; IM: 6-12 hours; IV: 4-8 hours, based on dose and renal function.

Classification & Brands

Dosing & administration

250 mg orally once daily. May be increased to 500 mg once daily if needed.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	CrCl 30-89 mL/min: 250 mg every 48 hours. CrCl <30 mL/min: 250 mg every 72 hours. Hemodialysis: 250 mg post-dialysis three times weekly.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 250 mg once daily. Child-Pugh C: use is not recommended.
Pediatric use	Children ≥2 years: 5 mg/kg orally once daily, maximum 250 mg. Adolescents: 250 mg once daily.
Geriatric use	Initiate at 125 mg once daily; titrate cautiously. Monitor renal function and adjust per renal guidelines.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for X-TROZINE L.A. (X-TROZINE L.A.).

Breastfeeding	Excreted into breast milk; M/P ratio approximately 0.8. Avoid breastfeeding due to potential adverse effects on infant neurodevelopment and risk of hypotonia.
Teratogenic Risk	First trimester: Associated with increased risk of neural tube defects (NTDs) and oral clefts based on animal studies and limited human data; second and third trimester: Risk of fetal growth restriction and oligohydramnios due to potential effects on placental perfusion.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to piperazine derivatives; severe bradycardia or sick sinus syndrome without pacemaker; concurrent use of MAO inhibitors; history of hepatic encephalopathy.