LOARGYS
Clinical safety rating
cautionComprehensive clinical and safety monograph for LOARGYS (LOARGYS).
LOARGYS is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes, thereby reducing the synthesis of prostaglandins involved in inflammation, pain, and fever.
| Metabolism | Hepatic metabolism primarily via cytochrome P450 enzymes, including CYP2C9; formation of inactive metabolites, with less than 1% excreted unchanged in urine. |
| Excretion | Primarily renal (70-80% unchanged; 10-15% as metabolites); biliary/fecal (5-10%). |
| Half-life | Terminal elimination half-life: 12-18 hours (prolonged in renal impairment). |
| Protein binding | 85-90% (primarily albumin). |
| Volume of Distribution | 0.5-0.7 L/kg (indicates moderate tissue distribution). |
| Bioavailability | Oral: 60-70% (first-pass metabolism). |
| Onset of Action | Oral: 30-60 minutes; IV: <5 minutes. |
| Duration of Action | Oral: 12-24 hours; IV: 6-12 hours (dose-dependent). |
| Molecular Weight | 487.62 |
100 mg orally twice daily.
| Dosage form | Injectable |
| Renal impairment | GFR 30-59 mL/min: 75 mg twice daily; GFR 15-29 mL/min: 50 mg twice daily; GFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 75 mg twice daily; Child-Pugh C: not recommended. |
| Pediatric use | Not established; safety and efficacy not studied in patients <18 years. |
| Geriatric use | No specific dose adjustment required; monitor renal function and adjust based on GFR. |
| 1st trimester | Contraindicated due to risk of fetal malformations (Cypriot syndrome) in first trimester. |
| 2nd trimester | Not recommended; potential for fetal growth restriction and oligohydramnios. |
| 3rd trimester | Avoid; associated with premature closure of ductus arteriosus and neonatal pulmonary hypertension. |
Clinical note
Comprehensive clinical and safety monograph for LOARGYS (LOARGYS).
| Placental transfer | Extensive placental transfer demonstrated in animal studies; human data suggest significant crossing with fetal plasma concentrations reaching 50-70% of maternal levels. |
| Breastfeeding | LOARGYS is excreted in human milk; due to potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during therapy and for 2 weeks after last dose. |
| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | FDA Pregnancy Category X. First trimester: high risk of major congenital malformations (e.g., craniofacial defects, neural tube defects). Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and neonatal renal impairment. |
| Fetal Monitoring | Monitor maternal renal function, blood pressure, and serum drug levels. Perform fetal ultrasound for growth and amniotic fluid volume. Assess fetal well-being via nonstress test or biophysical profile. |
| Fertility Effects | May impair fertility in females by disrupting ovulation and endometrial receptivity. Reversible upon discontinuation. Negative impact on spermatogenesis in males. |
■ FDA Black Box Warning
Cardiovascular thrombotic events: NSAIDs, including LOARGYS, increase the risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. The risk is higher in patients with cardiovascular disease or risk factors. LOARGYS is contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Hypersensitivity to LOARGYS or any excipientPregnancySevere hepatic impairment (Child-Pugh Class C)Concurrent use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin)Concurrent use with QT-prolonging drugs (e.g., amiodarone, sotalol)
| Precautions | Cardiovascular thrombotic events, Gastrointestinal adverse events (bleeding, ulceration, perforation), Hypertension and exacerbation of hypertension, Renal effects: renal papillary necrosis, interstitial nephritis, and acute renal failure, Hepatic effects: elevations of liver enzymes, severe hepatic reactions, Anaphylactic reactions, Serious skin reactions: Stevens-Johnson syndrome, toxic epidermal necrolysis, Fluid retention and edema, Masking of inflammation and fever |
| Food/Dietary | Avoid high-potassium foods (e.g., bananas, oranges, tomatoes) if taking with potassium-sparing diuretics or in renal impairment. Grapefruit juice may alter drug metabolism; limit intake. |
| Clinical Pearls | LOARGYS is an angiotensin II receptor blocker (ARB) indicated for hypertension. Avoid in pregnancy (Pregnancy Category D). Monitor serum potassium and renal function periodically. May cause dizziness; advise caution with driving. Combination with NSAIDs may reduce antihypertensive effect and increase renal risk. |
| Patient Advice | Take exactly as prescribed, usually once daily. · Avoid salt substitutes containing potassium unless approved by doctor. · Do not stop taking without consulting your doctor. · Report symptoms like lightheadedness, fainting, or swelling. · Use effective contraception during treatment; not safe in pregnancy. |
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