CAP-PROFEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CAP-PROFEN (CAP-PROFEN).
CAP-PROFEN is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes, reducing prostaglandin synthesis and resulting in anti-inflammatory, analgesic, and antipyretic effects.
| Metabolism | Primarily hepatic via CYP2C9. Minor pathways include CYP2C8 and CYP3A4. Conjugation with glucuronic acid also occurs. |
| Excretion | Primarily renal (70-80% as unchanged drug and glucuronide conjugate), with 10-15% biliary/fecal. Less than 5% unchanged in urine. |
| Half-life | 2-4 hours (terminal half-life); prolonged in elderly (up to 6 h) and renal impairment. |
| Protein binding | 99% bound to albumin. |
| Volume of Distribution | 0.15-0.2 L/kg; low Vd indicates limited tissue distribution, primarily confined to plasma and interstitial fluid. |
| Bioavailability | Oral: 80-100% (complete absorption); IM: 90-100%; IV: 100%. |
| Onset of Action | Oral: 30-60 minutes; IM: 15-30 minutes; IV: 5-10 minutes. |
| Duration of Action | 4-6 hours (oral); 4-6 hours (IM); 4-6 hours (IV). Duration correlates with dose and pain severity. |
| Molecular Weight | 206.28 |
200-400 mg orally every 4-6 hours as needed; maximum 1200 mg/day.
| Dosage form | TABLET |
| Renal impairment | CrCl 30-59 mL/min: reduce dose by 50% and extend interval to every 6-8 hours; CrCl <30 mL/min: avoid use. |
| Liver impairment | Child-Pugh class B: reduce dose by 50% and monitor; Child-Pugh class C: contraindicated. |
| Pediatric use | 5-10 mg/kg/dose orally every 6-8 hours; maximum 40 mg/kg/day. |
| Geriatric use | Initiate at lowest effective dose (100-200 mg every 6-8 hours); maximum 800 mg/day; monitor renal function. |
| 1st trimester | Avoid: Risk of spontaneous abortion and congenital malformations; NSAIDs are generally avoided in first trimester unless essential. |
| 2nd trimester | Use with caution: Associated with oligohydramnios and premature ductus arteriosus closure; limit use to lowest effective dose and shortest duration. |
| 3rd trimester | Avoid: High risk of premature closure of ductus arteriosus, oligohydramnios, and fetal renal impairment. |
Clinical note
Comprehensive clinical and safety monograph for CAP-PROFEN (CAP-PROFEN).
| Placental transfer | Ibuprofen crosses the placenta; fetal serum levels are approximately 1% of maternal levels. |
| Breastfeeding | Ibuprofen is excreted in breast milk in very low concentrations (less than 1% of maternal dose); considered compatible with breastfeeding. However, due to theoretical risks, avoid prolonged use or high doses. |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may occur early in treatment and may increase with duration of use. CAP-PROFEN is contraindicated in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
History of hypersensitivity to ibuprofen or any NSAIDActive peptic ulcer disease or gastrointestinal bleedingSevere heart failure (NYHA IV)Coronary artery bypass graft (CABG) surgery perioperative painThird trimester of pregnancy
| Precautions | Cardiovascular risk: increased risk of thrombotic events. Gastrointestinal risk: serious GI adverse events including bleeding, ulceration, and perforation. Renal effects: potential for renal toxicity, especially in patients with impaired renal function. Hepatic effects: elevation of liver enzymes and potential for severe hepatic reactions. Anaphylactoid reactions: may occur in patients without prior exposure. Pregnancy: avoid in third trimester due to risk of premature closure of ductus arteriosus. |
| Food/Dietary |
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| Lactation Rating | L1 - Safe |
| Teratogenic Risk | CAP-PROFEN (captopril, profen combination) is contraindicated in pregnancy. First trimester: increased risk of congenital malformations (cardiovascular, central nervous system). Second and third trimesters: fetal renal dysfunction, oligohydramnios, skull calcification, neonatal hypotension, renal failure, and death. Risk is dose-dependent. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN), serum electrolytes, and fetal ultrasound for amniotic fluid index, fetal growth, and renal function. In neonates, monitor for hypotension and renal function if exposure occurred in the third trimester. |
| Fertility Effects | Captopril may cause reversible fertility effects in males (decreased libido, erectile dysfunction, decreased sperm motility/viability) and females (menstrual irregularities, possible ovulation interference). Long-term data on fertility effects are limited. |
| No significant food interactions. However, a high-fiber diet and adequate fluid intake may enhance efficacy. Avoid concurrent use with mineral oil as it may increase risk of lipid pneumonia if aspirated. Do not take with dairy products or antacids within 1 hour as they may reduce effectiveness. |
| Clinical Pearls | CAP-PROFEN is a combination of docusate and sennosides; docusate is a stool softener that works by increasing water and fat penetration in the stool, while sennosides stimulate peristalsis. Onset of action for sennosides is 6-12 hours orally; administer at bedtime for morning bowel movement. Avoid use in patients with suspected bowel obstruction, undiagnosed abdominal pain, or acute surgical abdomen. Do not use for more than 1 week unless directed by a clinician; chronic use may lead to electrolyte imbalances or laxative dependency. |
| Patient Advice | Take this medication exactly as prescribed. Do not exceed the recommended dose or duration. · This drug is used for short-term relief of constipation. If constipation persists for more than 7 days, contact your healthcare provider. · Drink plenty of water while taking this medication to help prevent dehydration. · You may experience abdominal cramps or diarrhea; if severe or if you notice rectal bleeding, stop the medication and seek medical attention. · Do not take other laxatives or stool softeners concurrently without consulting your doctor. · Store at room temperature, away from moisture and heat. Keep out of reach of children. |