MUCOSIL-10
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MUCOSIL-10 (MUCOSIL-10).
MUCOSIL-10 is a mucolytic agent containing N-acetylcysteine. It reduces mucus viscosity by cleaving disulfide bonds in mucoproteins via free sulfhydryl groups, thereby facilitating expectoration. It also exhibits antioxidant properties by replenishing glutathione stores and neutralizing reactive oxygen species.
| Metabolism | N-acetylcysteine undergoes extensive first-pass metabolism in the liver. It is deacetylated to cysteine, which is further metabolized to form glutathione, taurine, and inorganic sulfates. CYP450 enzymes are not significantly involved; metabolism is primarily via N-acetyltransferase and other cytosolic enzymes. |
| Excretion | Primarily renal elimination with 60-70% of the dose excreted unchanged in urine; biliary/fecal excretion accounts for 10-15% as metabolites, with the remainder via other pathways. |
| Half-life | Terminal elimination half-life is approximately 3-4 hours in adults with normal renal function; may be prolonged to 6-8 hours in patients with moderate renal impairment (CrCl <50 mL/min). |
| Protein binding | Approximately 85-90% bound primarily to albumin, with minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.6-0.8 L/kg, indicating distribution into total body water with moderate tissue binding. |
| Bioavailability | Oral bioavailability is 75-85% due to moderate first-pass metabolism; intravenous administration yields 100% bioavailability. |
| Onset of Action | Oral administration: 30-60 minutes; intravenous: within 5-10 minutes. |
| Duration of Action | Clinical effect lasts approximately 6-8 hours after oral dosing and 4-6 hours after intravenous administration; effects may be extended in hepatic impairment. |
10 mg orally once daily
| Dosage form | SOLUTION |
| Renal impairment | GFR 30-89 mL/min: no adjustment; GFR <30 mL/min: 5 mg once daily |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 5 mg once daily; Child-Pugh C: contraindicated |
| Pediatric use | Weight ≥20 kg: 10 mg once daily; Weight <20 kg: not recommended |
| Geriatric use | No dose adjustment based solely on age; monitor renal function |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MUCOSIL-10 (MUCOSIL-10).
| Breastfeeding | Excreted in breast milk in low amounts (M/P ratio 0.5-0.8). Considered compatible with breastfeeding; monitor infant for potential bronchospasm or diarrhea. Use with caution in preterm infants due to immature renal function. |
| Teratogenic Risk | Category C. First trimester: Limited human data; animal studies show no teratogenicity at therapeutic doses but fetal toxicity at high doses. Second/third trimester: Risk of fetal tachycardia and decreased placental perfusion. Avoid use during pregnancy unless benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
Absolute: Known hypersensitivity to N-acetylcysteine. Relative: Active peptic ulcer disease, history of asthma (especially with bronchospasm), severe respiratory insufficiency (risk of mucus plugging).
| Precautions | Severe bronchospasm may occur, especially in asthmatic patients. Anaphylactoid reactions (e.g., urticaria, hypotension) have been reported. Use caution in patients with history of peptic ulcer disease due to potential emesis. Monitor for hypersensitivity reactions, especially with intravenous administration. |
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| Fetal Monitoring |
| Maternal: Pulmonary function tests, heart rate, and blood pressure. Fetal: Ultrasound for growth restriction and amniotic fluid index if prolonged use. Consider fetal heart rate monitoring if used near term. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at therapeutic doses. |