MESNA
Clinical safety rating: safe
Animal studies have demonstrated safety
Mesna acts as a chemoprotectant. It is metabolized to dimesna, which is reduced in the kidneys to free mesna, binding to urotoxic acrolein and other toxic metabolites of cyclophosphamide and ifosfamide, thereby preventing hemorrhagic cystitis.
| Metabolism | Mesna is rapidly oxidized in the plasma to dimesna (disulfide form). Dimesna is reduced back to mesna in the kidneys by glutathione reductase and other thiols. Unchanged mesna and dimesna are eliminated renally. |
| Excretion | Renal: ~80% as mesna and its dimer dimesna; fecal: minimal (<5%) |
| Half-life | 0.36 hours (mesna); 1.17 hours (dimesna); rapid elimination requires continuous infusion for sustained uroprotection |
| Protein binding | ~69-75% (mesna); primarily to albumin |
| Volume of Distribution | 0.65 L/kg (mesna); indicates distribution into total body water, not extensive tissue binding |
| Bioavailability | Oral: 45-79% (variable due to first-pass metabolism; dimer dimesna is reduced back to mesna in kidney) |
| Onset of Action | Intravenous: immediate; oral: onset within 1 hour |
| Duration of Action | Intravenous: ~2-4 hours; oral: ~6 hours; clinical use: repeated dosing or continuous infusion covers entire chemotherapy |
| Action Class | Cytoprotective agents- Bladder |
| Brand Substitutes | Uromitexan 200mg Injection, Mesolit Injection |
Intravenous: 60 mg/kg (total dose) as a 15-minute infusion or 3 divided doses (20 mg/kg at 0, 4, and 8 hours after cyclophosphamide or ifosfamide). Oral: 400-800 mg/m2 every 4 hours x 3 doses starting 2 hours before ifosfamide.
| Dosage form | INJECTABLE |
| Renal impairment | GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: reduce dose to 75% of standard; GFR <10 mL/min: reduce dose to 50% of standard. |
| Liver impairment | No specific Child-Pugh based adjustments; use with caution in severe hepatic impairment due to limited data. |
| Pediatric use | IV: 20 mg/kg/dose at 0, 4, and 8 hours after cyclophosphamide/ifosfamide (60 mg/kg total). Oral: 400-800 mg/m2 every 4 hours x 3 doses. |
| Geriatric use | No specific dose adjustment based on age alone; monitor renal function and adjust per renal criteria. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
No significant drug interactions Used to prevent hemorrhagic cystitis caused by ifosfamide.
| Breastfeeding | No data on mesna excretion in human milk. M/P ratio unknown. Due to low molecular weight (164.2 g/mol) and high water solubility, excretion into breast milk is possible but likely minimal. Caution: consider benefits vs risks; manufacturer recommends discontinue breastfeeding or drug. |
| Teratogenic Risk | Mesna is not teratogenic in animal studies; human data insufficient. Theoretical risk low as it is a sulfhydryl compound without known embryotoxic effects in first trimester. Second and third trimester: no fetal toxicity reported. Use if clearly needed. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Known hypersensitivity to mesna or any component of the formulation."]
| Precautions | ["Hypersensitivity reactions (including anaphylaxis) have been reported, especially in patients with autoimmune disorders.","May cause false-positive ketone tests (urinary dipsticks) due to presence of thiol groups.","Not intended to reduce other toxicities of chemotherapy."] |
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| Fetal Monitoring |
| Monitor maternal renal function (mesna is renally eliminated) and liver function tests. Monitor for hypersensitivity reactions (e.g., rash, urticaria). No fetal-specific monitoring required; follow standard obstetric care. |
| Fertility Effects | Mesna is not known to affect human fertility. No reproductive toxicity in animal studies at clinical doses. In males: no effect on spermatogenesis. In females: no effect on ovulation or implantation. |