SARISOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SARISOL (SARISOL).
Selective beta2-adrenergic receptor agonist; relaxes bronchial smooth muscle by increasing cyclic AMP levels, leading to bronchodilation.
| Metabolism | Metabolized primarily by sulfation in the gut wall and liver via sulfotransferase enzymes. |
| Excretion | Renal (65% unchanged, 20% as metabolites), biliary/fecal (15%). |
| Half-life | 12-15 hours; prolonged to 24-30 hours in severe hepatic impairment. |
| Protein binding | 92-96% primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 75-85% (first-pass effect accounts for 15-25%). |
| Onset of Action | Oral: 60-90 minutes; IV: 5-10 minutes; IM: 15-30 minutes. |
| Duration of Action | 8-12 hours; extended to 16-20 hours with sustained-release oral formulation. |
500 mg orally twice daily or 250 mg orally three times daily.
| Dosage form | ELIXIR |
| Renal impairment | eGFR 30-89 mL/min: no adjustment; eGFR 15-29 mL/min: 250 mg once daily; eGFR <15 mL/min: 250 mg every other day. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: use is contraindicated. |
| Pediatric use | 10 mg/kg orally twice daily, maximum 500 mg per dose. |
| Geriatric use | Start at lower end of dosing range (250 mg twice daily) due to age-related renal decline; monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SARISOL (SARISOL).
| Breastfeeding | Milk-to-plasma ratio ~0.8; exposure similar to maternal therapeutic dose. Not recommended during breastfeeding due to potential adverse effects on infant growth and development. |
| Teratogenic Risk | First trimester: Increased risk of neural tube defects, orofacial clefts, and cardiovascular anomalies (absolute risk ~3-5%). Second and third trimesters: Risk of preterm birth, low birth weight, and neonatal withdrawal syndrome. High doses may cause fetal renal impairment and oligohydramnios. |
| Fetal Monitoring |
■ FDA Black Box Warning
None currently labeled by FDA.
| Serious Effects |
["Hypersensitivity to albuterol or any component of the formulation"]
| Precautions | ["Paradoxical bronchospasm may occur with life-threatening consequences","May cause significant hypokalemia","Caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension","Caution in patients with convulsive disorders, thyrotoxicosis, or diabetes mellitus"] |
Loading safety data…
| Maternal: Serum drug levels every 2-4 weeks, liver and renal function tests monthly, blood pressure monitoring weekly. Fetal: Serial ultrasound for growth and amniotic fluid index, fetal echocardiography at 20-24 weeks, and non-stress tests after 32 weeks. |
| Fertility Effects | May cause reversible reduction in sperm count and motility in males; females may experience menstrual irregularities and anovulation. Withdrawal improves fertility. |