TAB-PROFEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TAB-PROFEN (TAB-PROFEN).
Non-selective cyclooxygenase (COX-1 and COX-2) inhibitor; reduces prostaglandin synthesis.
| Metabolism | Hepatic via CYP2C9; minor pathways include glucuronidation and CYP3A4. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 70-90% of the administered dose, with the remainder eliminated as glucuronide conjugates in urine. Biliary/fecal elimination is minimal (<5%). |
| Half-life | The terminal elimination half-life is 2-4 hours in adults with normal renal function. In elderly patients or those with renal impairment, half-life may be prolonged up to 8-12 hours, requiring dose adjustment. |
| Protein binding | Approximately 99% bound to serum albumin, with minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.15-0.2 L/kg, indicating limited extravascular distribution and primarily restricted to the central compartment. |
| Bioavailability | Oral: 85-95% (rapidly absorbed with first-pass metabolism <10%); rectal: 70-80%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: 5-15 minutes; intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 4-6 hours; intravenous/intramuscular: 4-6 hours. Analgesic effect may persist longer (up to 8 hours) with higher doses. |
| Molecular Weight | 206.28 |
400-800 mg orally every 6-8 hours as needed; maximum 3200 mg/day.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-59 mL/min: reduce dose by 50% and increase interval to every 8-12 hours; eGFR <30 mL/min: avoid use. |
| Liver impairment | Child-Pugh class A: no adjustment; Child-Pugh class B: reduce dose by 50%; Child-Pugh class C: avoid use. |
| Pediatric use | 5-10 mg/kg/dose orally every 6-8 hours; maximum 40 mg/kg/day. |
| Geriatric use | Initiate at lowest effective dose (e.g., 200-400 mg every 8-12 hours); maximum 2000 mg/day; monitor renal function. |
| 1st trimester | Avoid during first trimester due to potential teratogenic effects (e.g., NSAID use linked to cardiac defects and gastroschisis). |
| 2nd trimester | Use only if clearly needed; may cause oligohydramnios and fetal renal dysfunction; avoid prolonged use. |
| 3rd trimester | Contraindicated in third trimester due to risk of premature closure of ductus arteriosus and oligohydramnios. |
Clinical note
Comprehensive clinical and safety monograph for TAB-PROFEN (TAB-PROFEN).
| Placental transfer | Ibuprofen crosses the placenta; fetal plasma concentrations are approximately 1-2% of maternal levels. |
| Breastfeeding | Ibuprofen is excreted into breast milk in very low concentrations (less than 1% of maternal dose). It is considered compatible with breastfeeding; however, avoid use in mothers with infants who have bleeding disorders or thrombocytopenia. |
■ FDA Black Box Warning
Increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal; increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines.
| Serious Effects |
Third trimester pregnancyHistory of hypersensitivity to ibuprofen or other NSAIDsActive peptic ulcer disease or gastrointestinal bleedingSevere renal failure (eGFR <30 mL/min/1.73m²)Severe heart failure (NYHA class III-IV)History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsPerioperative pain in coronary artery bypass graft (CABG) surgery
| Precautions | Cardiovascular risk (especially in patients with established CVD or risk factors); GI bleeding and ulceration; renal toxicity; hypertension; fluid retention; anaphylactoid reactions; serious skin reactions (e.g., Stevens-Johnson syndrome); avoid in late pregnancy. |
| Food/Dietary | Avoid alcohol. May be taken with food or milk to minimize gastrointestinal irritation. Grapefruit juice has no significant interaction with ibuprofen. |
Loading safety data…
| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | FDA Pregnancy Category D. First trimester: Increased risk of cardiac defects (OR 1.3-3.4) and gastroschisis (OR 2.4). Second/third trimester: Premature closure of ductus arteriosus, oligohydramnios, necrotizing enterocolitis, intracranial hemorrhage. Avoid after 30 weeks. |
| Fetal Monitoring | Monitor fetal heart rate, amniotic fluid index (weekly after 32 weeks if used >48h), ductus arteriosus Doppler if prolonged use. Maternal: renal function, liver enzymes, CBC, signs of bleeding. |
| Fertility Effects | Reversible inhibition of prostaglandin synthesis may impair implantation and ovulation. Use may delay time to conception. Discontinue if pregnancy is planned. |
| Clinical Pearls | TAB-PROFEN (ibuprofen) is an NSAID; avoid in patients with severe renal impairment (CrCl <30 mL/min) or active peptic ulcer disease. Use with caution in elderly and those on anticoagulants. Discontinue 48 hours prior to elective surgery due to bleeding risk. Max single dose 800 mg, max daily dose 3200 mg. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not exceed 3200 mg per day or use for more than 10 days for pain unless directed by a doctor. · Avoid alcohol while taking this medication to reduce risk of stomach bleeding. · Stop taking and seek medical help if you experience signs of stomach bleeding (black/tarry stools, vomit that looks like coffee grounds) or allergic reaction (rash, swelling, difficulty breathing). · Do not combine with other NSAIDs (e.g., naproxen, aspirin) without consulting a healthcare provider. |