SANDRIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SANDRIL (SANDRIL).

How it works

Sandril (reserpine) acts by depleting catecholamines (norepinephrine, dopamine) and serotonin from central and peripheral nerve terminals via irreversible inhibition of the vesicular monoamine transporter (VMAT). This leads to reduced sympathetic output, decreased peripheral vascular resistance, and lowered blood pressure.

What the body does with it

Metabolism	Primarily metabolized by the liver via hydrolysis and conjugation; major metabolites include reserpic acid and methyl reserpate. CYP450 enzymes are not significantly involved.
Excretion	Primarily renal excretion of unchanged drug (60-70%) and glucuronide conjugate (20-30%); biliary/fecal excretion accounts for <10%.
Half-life	Terminal elimination half-life is 3-5 hours in adults; prolonged to 8-15 hours in elderly or renal impairment (CrCl <30 mL/min).
Protein binding	Approximately 95% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	3-5 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is 50-70% due to first-pass metabolism.
Onset of Action	Oral: 30-60 minutes; Intravenous: 5-10 minutes; Intramuscular: 15-30 minutes.
Duration of Action	Oral: 4-6 hours for analgesic effect; intravenous: 2-4 hours; clinical duration may be shorter due to redistribution.

Classification & Brands

Dosing & administration

Initial: 2 mg orally twice daily; increase by 2 mg/day every 1-2 weeks; usual maintenance: 4-16 mg/day in 2 divided doses; maximum: 16 mg/day.

Dosage form	INJECTABLE
Renal impairment	GFR 30-89 mL/min: no adjustment needed; GFR <30 mL/min: reduce dose by 50%; hemodialysis: administer after dialysis; peritoneal dialysis: avoid use.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated.
Pediatric use	Children 6-12 years: initial 0.5 mg/kg/day orally in 2 divided doses; increase by 0.5 mg/kg/day every 2 weeks; maximum 3 mg/kg/day up to 16 mg/day. Children >12 years: same as adult dosing.
Geriatric use	Initial dose 1 mg orally twice daily; titrate slowly; maximum 8 mg/day; monitor for hypotension and sedation.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for SANDRIL (SANDRIL).

Breastfeeding	Contraindicated due to neonatal sedation and withdrawal risk. M/P ratio not established; excreted in breast milk at concentrations 50-100% of maternal serum.
Teratogenic Risk	FDA Pregnancy Category D. First trimester: limb reduction defects, cardiac anomalies, neural tube defects. Second/third trimesters: fetal growth restriction, oligohydramnios, preterm labor. Neonatal: withdrawal syndrome, respiratory depression.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: Risk of Suicide – Reserpine may cause severe depression and suicidal ideation. Use with caution in patients with a history of depression. Discontinue if signs of depression occur.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to reserpine, history of mental depression (especially with suicidal tendencies), active peptic ulcer, ulcerative colitis, electroconvulsive therapy (ECT), and concurrent use with MAO inhibitors.

Clinical Precautions

Precautions

May cause mental depression, peptic ulcer activation (due to increased gastric acid secretion), and extrapyramidal symptoms. Avoid in patients with a history of depression, Parkinson's disease, or epilepsy. Monitor for hypotension, bradycardia, and electrolyte disturbances. Taper gradually to avoid withdrawal symptoms (e.g., severe hypertension).

Clinical Tips & Counseling

Drug interactions

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SANDRIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SANDRIL (SANDRIL).

How it works

What the body does with it

Metabolism	Primarily metabolized by the liver via hydrolysis and conjugation; major metabolites include reserpic acid and methyl reserpate. CYP450 enzymes are not significantly involved.
Excretion	Primarily renal excretion of unchanged drug (60-70%) and glucuronide conjugate (20-30%); biliary/fecal excretion accounts for <10%.
Half-life	Terminal elimination half-life is 3-5 hours in adults; prolonged to 8-15 hours in elderly or renal impairment (CrCl <30 mL/min).
Protein binding	Approximately 95% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	3-5 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is 50-70% due to first-pass metabolism.
Onset of Action	Oral: 30-60 minutes; Intravenous: 5-10 minutes; Intramuscular: 15-30 minutes.
Duration of Action	Oral: 4-6 hours for analgesic effect; intravenous: 2-4 hours; clinical duration may be shorter due to redistribution.

Classification & Brands

Dosing & administration

Initial: 2 mg orally twice daily; increase by 2 mg/day every 1-2 weeks; usual maintenance: 4-16 mg/day in 2 divided doses; maximum: 16 mg/day.

Dosage form	INJECTABLE
Renal impairment	GFR 30-89 mL/min: no adjustment needed; GFR <30 mL/min: reduce dose by 50%; hemodialysis: administer after dialysis; peritoneal dialysis: avoid use.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated.
Pediatric use	Children 6-12 years: initial 0.5 mg/kg/day orally in 2 divided doses; increase by 0.5 mg/kg/day every 2 weeks; maximum 3 mg/kg/day up to 16 mg/day. Children >12 years: same as adult dosing.
Geriatric use	Initial dose 1 mg orally twice daily; titrate slowly; maximum 8 mg/day; monitor for hypotension and sedation.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for SANDRIL (SANDRIL).

Breastfeeding	Contraindicated due to neonatal sedation and withdrawal risk. M/P ratio not established; excreted in breast milk at concentrations 50-100% of maternal serum.
Teratogenic Risk	FDA Pregnancy Category D. First trimester: limb reduction defects, cardiac anomalies, neural tube defects. Second/third trimesters: fetal growth restriction, oligohydramnios, preterm labor. Neonatal: withdrawal syndrome, respiratory depression.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: Risk of Suicide – Reserpine may cause severe depression and suicidal ideation. Use with caution in patients with a history of depression. Discontinue if signs of depression occur.