CYKLOKAPRON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CYKLOKAPRON (CYKLOKAPRON).
Competitive inhibition of plasminogen activation, reducing fibrinolysis by blocking the binding of plasminogen to fibrin.
| Metabolism | Primarily renal excretion; minimal hepatic metabolism (3-5% through oxidative deamination). |
| Excretion | Renal: >95% as unchanged drug via glomerular filtration; minimal biliary/fecal (<5%). |
| Half-life | Terminal elimination half-life: 2-3 hours (renal impairment extends to 10-20 hours). |
| Protein binding | Approximately 3% (primarily to albumin); negligible binding. |
| Volume of Distribution | 0.3-0.7 L/kg; reflects distribution mainly into extracellular fluid. |
| Bioavailability | Oral: 30-50% (due to incomplete absorption); IV: 100%. |
| Onset of Action | IV: Immediate (within minutes); Oral: 2-3 hours after ingestion. |
| Duration of Action | IV: 3-8 hours (dependent on renal function); Oral: 6-8 hours. |
| Action Class | Antifibrinolytic |
| Brand Substitutes | T Syl 100mg Injection, Tranarest 100mg Injection, Coastat 100mg Injection, Tromic 100mg Injection, Trim 100mg Injection |
1 g (10 mL) IV over 5-10 minutes every 6-8 hours; or 25-50 mg/kg/day IV divided every 6-8 hours. Oral: 1-1.5 g 3-4 times daily.
| Dosage form | TABLET |
| Renal impairment | GFR 30-50 mL/min: 50% of dose every 12 hours. GFR 10-30 mL/min: 50% of dose every 24 hours. GFR <10 mL/min: 50% of dose every 48 hours or 25% of dose every 24 hours. |
| Liver impairment | No specific guidelines; caution in severe hepatic impairment due to risk of accumulation. |
| Pediatric use | IV: 25-50 mg/kg/day divided every 6-8 hours; max 3 g/day. Oral: 25 mg/kg/dose every 6-8 hours; max 1.5 g/dose. |
| Geriatric use | No specific adjustment but consider renal function; reduce dose per renal guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CYKLOKAPRON (CYKLOKAPRON).
| Breastfeeding | Excreted in human milk in low concentrations; no adverse effects reported in nursing infants. M/P ratio unknown. Caution advised. |
| Teratogenic Risk | FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but no adequate human studies in pregnant women. Use only if clearly needed. |
| Fetal Monitoring | Monitor for thrombotic events, changes in menstrual bleeding pattern, and fetal growth if used during pregnancy. |
■ FDA Black Box Warning
None
| Serious Effects |
["Active thromboembolic disease","History of venous or arterial thrombosis","Intravascular clotting","Severe renal impairment (CrCl <30 mL/min)"]
| Precautions | ["Increased risk of thromboembolic events (e.g., venous/arterial thrombosis)","Seizures with high doses or prolonged use","Cerebral edema (intrathecal injection)","Renal impairment requires dose adjustment"] |
| Food/Dietary | No clinically significant food interactions. Can be taken with or without food. |
| Clinical Pearls |
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| Fertility Effects | No known adverse effects on fertility. May be used to reduce menorrhagia but does not impair ovulation or conception. |
| Cyklokapron (tranexamic acid) is an antifibrinolytic. For heavy menstrual bleeding, prescribe 1300 mg orally three times daily for up to 5 days. Avoid in patients with subarachnoid hemorrhage, active thromboembolic disease, or acquired defective color vision. Monitor for thrombotic events, especially in patients with a history of thrombosis. Do not combine with factor IX complex concentrates or anti-inhibitor coagulant concentrates due to increased thrombosis risk. For trauma patients, early administration (within 3 hours) reduces mortality in bleeding patients. |
| Patient Advice | Take this medication exactly as prescribed, usually 2 to 3 times daily with or without food. · For heavy menstrual bleeding, start taking the tablet on the first day of your period and continue for up to 5 days. · Avoid this medication if you have had a blood clot, stroke, or are allergic to tranexamic acid. · Seek immediate medical attention if you experience symptoms of a blood clot: leg pain/swelling, sudden chest pain, trouble breathing, or sudden vision changes. · This medication may cause dizziness or blurred vision; avoid driving until you know how it affects you. Inform your doctor if you are pregnant, breastfeeding, or planning to become pregnant. |