OPIPZA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OPIPZA (OPIPZA).
Opipza (ozanimod) is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1 and 5. It acts as a functional antagonist, blocking lymphocyte egress from lymph nodes, thereby reducing circulating lymphocytes and their infiltration into the central nervous system. This attenuates inflammatory processes in multiple sclerosis.
| Metabolism | Ozanimod is extensively metabolized primarily via aldehyde dehydrogenase (ALDH) and alcohol dehydrogenase (ADH) to form active metabolites (RP-101075 and RP-101988). CYP3A4 plays a minor role. Ozanimod and its metabolites are substrates for P-glycoprotein (P-gp) and BCRP. |
| Excretion | Primarily renal excretion of unchanged drug (approximately 90%) with minor biliary/fecal elimination (<10%) |
| Half-life | Terminal elimination half-life is 6-8 hours; prolonged in renal impairment (up to 20 hours in severe impairment) |
| Protein binding | Approximately 60% bound to plasma albumin |
| Volume of Distribution | 0.5-0.8 L/kg; indicates moderate tissue distribution |
| Bioavailability | Oral: 70-80%; Intravenous: 100% |
| Onset of Action | Oral: 1-3 hours; Intravenous: 5-15 minutes |
| Duration of Action | 6-12 hours; extended with dose adjustment in renal impairment |
| Molecular Weight | 302.3 |
400 mg orally once daily, with or without food.
| Dosage form | FILM |
| Renal impairment | eGFR 30-89 mL/min: no adjustment; eGFR <30 mL/min: not recommended (no data); hemodialysis: not recommended. |
| Liver impairment | Child-Pugh A, B, C: 400 mg orally once daily, but monitor for adverse effects; severe impairment (Child-Pugh C): use with caution due to limited data. |
| Pediatric use | Not approved for pediatric patients younger than 18 years; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment required; consider age-related renal impairment and monitor renal function; start at lower end of dosing range if frail. |
| 1st trimester | Insufficient human data; animal studies show risk. Avoid unless benefit outweighs risk. |
| 2nd trimester | Insufficient human data; potential fetal effects. Use only if clearly needed. |
| 3rd trimester | Insufficient human data; risk of neonatal adverse effects. Avoid near term. |
Clinical note
Comprehensive clinical and safety monograph for OPIPZA (OPIPZA).
| Placental transfer | Data not available; likely crosses placenta due to low molecular weight. |
| Breastfeeding | No data on excretion into breast milk; consider risk of infant hypoglycemia. Caution if used while breastfeeding. |
| Lactation Rating |
■ FDA Black Box Warning
WARNING: INFECTIONS AND BRADYARRHYTHMIA. Ozanimod increases the risk of infections, including serious and life-threatening herpes virus infections. Initiation of treatment may cause a transient decrease in heart rate and atrioventricular conduction delays. Patients should be monitored during initiation.
| Serious Effects |
Hypersensitivity to opipza or any excipientSevere hepatic impairment
| Precautions | Risk of infections (including opportunistic infections), bradyarrhythmia and heart block at treatment initiation, increased blood pressure, respiratory effects (decline in pulmonary function), liver injury, macular edema, fetal risk, and lymphopenia. Vaccination status should be updated before treatment. Avoid live vaccines during treatment. |
| Food/Dietary | Take with food or milk to reduce gastrointestinal irritation. Avoid foods that may exacerbate GI irritation such as spicy foods, acidic foods, or excessive caffeine. There are no known pharmacokinetic food interactions with omeprazole or piroxicam that alter drug absorption significantly when taken with food; however, food may reduce the rate of absorption. Grapefruit juice has not been reported to interact with OPIPZA, but caution with high-fat meals is not required. Avoid alcohol as it can increase the risk of NSAID-induced GI bleeding. |
Loading safety data…
| L3 - Limited Data |
| Teratogenic Risk | There is insufficient human data; animal studies not identified. Risk cannot be excluded. First trimester: theoretical risk based on mechanism (dopamine antagonist). Second and third trimesters: risk of extrapyramidal symptoms and withdrawal in neonates if exposed near term. |
| Fetal Monitoring | Monitor maternal blood pressure, glucose, and weight; assess for QT prolongation with ECG if other risk factors. Fetal monitoring for growth and well-being if used chronically. |
| Fertility Effects | May increase prolactin levels leading to menstrual irregularities, anovulation, and reduced fertility. Effects reversible upon discontinuation. |
| Clinical Pearls | OPIPZA is a combination of omeprazole, a proton pump inhibitor, and piroxicam, a nonsteroidal anti-inflammatory drug. It is indicated for the treatment of osteoarthritis and rheumatoid arthritis in patients at risk for NSAID-associated gastric ulcers. The omeprazole component reduces gastric acid secretion, mitigating the risk of gastric and duodenal ulcers. Use with caution in patients with cardiovascular disease, renal impairment, or history of GI bleeding. Monitor renal function, liver enzymes, and complete blood counts periodically. Avoid concomitant use with other NSAIDs, anticoagulants, or methotrexate. The piroxicam component has a long half-life (30-86 hours), leading to delayed onset of full anti-inflammatory effect. Advise patients to take the medication with food to reduce GI discomfort. Discontinue if signs of skin rash, eosinophilia, or systemic symptoms occur (DRESS syndrome). Not recommended in pregnancy (third trimester) or breastfeeding. |
| Patient Advice | Take this medication exactly as prescribed, usually once daily with food to prevent stomach upset. · Do not crush or chew the capsule; swallow it whole. · Avoid drinking alcohol while taking OPIPZA as it may increase the risk of stomach bleeding. · Inform your doctor if you have a history of heart disease, high blood pressure, kidney disease, or liver disease. · Report any signs of stomach bleeding such as black/tarry stools, vomit that looks like coffee grounds, or persistent stomach pain. · Do not take other NSAIDs (e.g., ibuprofen, naproxen) or aspirin while on this medication unless directed by your doctor. · OPIPZA may increase your risk of serious skin reactions; stop taking and seek medical help if you develop a rash, blisters, or fever. · Long-term use may cause low magnesium levels; notify your doctor if you experience muscle cramps, irregular heartbeat, or seizures. · Keep this medication out of reach of children and do not share it with others. · Store at room temperature away from moisture and heat. |