SANDRIL
Clinical safety rating
cautionComprehensive clinical and safety monograph for SANDRIL (SANDRIL).
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.
| 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. |
| Molecular Weight | 340.42 |
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. |
| 1st trimester | Avoid; animal studies show teratogenic effects; limited human data suggests increased risk of congenital malformations. |
| 2nd trimester | Use only if maternal benefit outweighs fetal risk; may cause fetal growth restriction. |
| 3rd trimester | Avoid near term; may cause neonatal adverse effects (e.g., respiratory depression, withdrawal symptoms). |
Clinical note
Comprehensive clinical and safety monograph for SANDRIL (SANDRIL).
| Placental transfer | Crosses human placenta readily; detected in cord blood and amniotic fluid. |
| Breastfeeding | Excreted in breast milk; monitor infant for sedation, poor feeding, and weight loss; consider alternative agents. |
| Lactation Rating | L4 (Possibly Hazardous) |
| 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 | Maternal: hepatic function, CBC, creatinine, urine toxicology. Fetal: ultrasound for growth and anatomy, nonstress test from 32 weeks, biophysical profile if growth restriction. |
| Fertility Effects | May cause menstrual irregularities, anovulation, and hyperprolactinemia in females; decreased libido, erectile dysfunction, and gynecomastia in males. Reversible upon discontinuation. |
■ 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.
| Serious Effects |
Hypersensitivity to drug or any componentConcurrent use with MAOIsSevere hepatic impairment
| 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). |
| Food/Dietary | Avoid excessive intake of potassium-rich foods (bananas, oranges, spinach) unless directed by prescriber. May increase alcohol-induced hypotensive effects. Caffeine may enhance diuretic effect. Grapefruit juice has not been reported to interact, but caution with high-sodium foods as they may reduce antihypertensive efficacy. |
| Clinical Pearls | SANDRIL is a brand name for hydrochlorothiazide, a thiazide diuretic. Monitor serum potassium and magnesium levels, as hypokalemia and hypomagnesemia are common. Avoid use in patients with anuria or sulfonamide allergy. Start at low dose (12.5-25 mg daily) to minimize electrolyte disturbances. Onset of action is 2 hours, peak 4-6 hours, duration 6-12 hours. Use caution in patients with renal impairment (CrCl <30 mL/min is contraindicated). |
| Patient Advice | Take this medication exactly as prescribed, usually in the morning to avoid nighttime urination. · Avoid prolonged sun exposure; use sunscreen as this drug may increase sensitivity to sunlight. · Report symptoms of electrolyte imbalance: muscle cramps, weakness, irregular heartbeat, excessive thirst, or confusion. · Do not take with other medications that lower blood pressure without consulting your doctor. · This drug may increase blood sugar and uric acid levels; monitor if diabetic or gout-prone. |
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