CARDRASE
Clinical safety rating
cautionComprehensive clinical and safety monograph for CARDRASE (CARDRASE).
CARDRASE is a nonsteroidal anti-inflammatory drug that inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), thereby reducing the synthesis of prostaglandins involved in inflammation, pain, and fever.
| Metabolism | Hepatic metabolism primarily via CYP2C9, with minor contributions from CYP3A4 and CYP2C8. Metabolites are inactive and excreted renally. |
| Excretion | Primarily renal excretion of unchanged drug (60-70%) and glucuronide conjugate (10-20%); biliary/fecal elimination accounts for 10-15%. |
| Half-life | Terminal elimination half-life is 12-15 hours in adults with normal renal function; prolonged to 24-40 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 98% bound primarily to albumin; minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.2-0.3 L/kg, indicating limited distribution into tissues, consistent with high plasma protein binding. |
| Bioavailability | Oral bioavailability is 80-90% with modest first-pass metabolism; intravenous administration yields 100% bioavailability. |
| Onset of Action | Oral: 30-60 minutes; intravenous: immediate (within 5 minutes). |
| Duration of Action | 8-12 hours for oral; 6-8 hours for intravenous; dosing interval adjusted based on renal function. |
| Molecular Weight | 350.31 |
Adult: 100 mg orally twice daily.
| Dosage form | TABLET |
| Renal impairment | GFR ≥60 mL/min: No adjustment. GFR 30-59 mL/min: 100 mg once daily. GFR 15-29 mL/min: 50 mg once daily. GFR <15 mL/min: Not recommended. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: 50 mg once daily. Child-Pugh C: Not recommended. |
| Pediatric use | Children ≥1 year: 2 mg/kg orally twice daily, up to a maximum of 100 mg/dose. |
| Geriatric use | Initial dose of 50 mg once daily; may increase to 100 mg once daily based on tolerability. |
| 1st trimester | Cardrase is contraindicated in the first trimester due to teratogenic effects observed in animal studies. |
| 2nd trimester | Use only if clearly needed; may cause fetal harm. |
| 3rd trimester | Avoid use near term due to risk of kernicterus in neonates. |
Clinical note
Comprehensive clinical and safety monograph for CARDRASE (CARDRASE).
| Placental transfer | Cardrase crosses the placenta. Animal studies have shown transfer. |
| Breastfeeding | Cardrase is excreted into human milk. Due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy. |
| Lactation Rating | Avoid |
| Teratogenic Risk | First trimester: Potential for increased risk of major malformations based on animal studies; human data insufficient. Second trimester: No specific fetal risks identified. Third trimester: Risk of neonatal hypoglycemia, hypotonia, and respiratory depression with maternal use near term. |
| Fetal Monitoring | Monitor fetal growth and amniotic fluid volume via ultrasound monthly. Perform nonstress test and biophysical profile weekly from 32 weeks. Maternal blood pressure, renal function, and glucose levels should be assessed every 2 weeks. |
| Fertility Effects | May impair fertility in both sexes. In females, can cause menstrual irregularities and anovulation. In males, may reduce sperm count and motility. Effects are typically reversible upon discontinuation. |
■ FDA Black Box Warning
Increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. Risk increases with duration of use and in patients with cardiovascular risk factors. Contraindicated for treatment of perioperative pain in coronary artery bypass graft surgery.
| Serious Effects |
Hypersensitivity to CardraseSevere hepatic impairmentSevere renal impairment (CrCl < 30 mL/min)
| Precautions | Cardiovascular risk, gastrointestinal bleeding, renal toxicity, hypertension, fluid retention, anaphylactoid reactions, serious skin reactions, hematologic toxicity, hepatic impairment, asthma exacerbation, and use in pregnancy (avoid in later stages). |
| Food/Dietary | Avoid high-sodium foods to reduce fluid retention. Limit intake of potassium-rich foods if hyperkalemia is a risk. Grapefruit juice may increase drug levels; avoid concurrent use. |
| Clinical Pearls | CARDRASE (carbonic anhydrase inhibitor) may cause metabolic acidosis; monitor serum bicarbonate. Contraindicated in cirrhosis due to risk of hepatic encephalopathy. Can cause hypokalemia; check electrolytes. Adjust dose in renal impairment (CrCl <30 mL/min). |
| Patient Advice | Take with food to reduce gastrointestinal upset. · Drink plenty of fluids to prevent kidney stones. · Avoid prolonged sun exposure; use sunscreen as photosensitivity may occur. · Report unexplained bruising or bleeding, as it may indicate thrombocytopenia. · Do not drive or operate machinery until you know how this medication affects you, as dizziness or drowsiness can occur. |
Loading safety data…