PATANASE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PATANASE (PATANASE).
Olopatadine is a selective histamine H1 receptor antagonist and mast cell stabilizer, inhibiting release of histamine and other inflammatory mediators. It also antagonizes histamine at H1 receptors.
| Metabolism | Olopatadine is not extensively metabolized; the primary metabolic pathway is via direct glucuronidation by UGT1A3 and UGT2B7, with minor involvement of CYP3A4. The major circulating metabolites are olopatadine N-oxide and olopatadine glucuronide. |
| Excretion | Primarily renal excretion of unchanged drug (74%) and metabolites, with biliary/fecal elimination accounting for approximately 10%. |
| Half-life | Terminal elimination half-life is 2.5 hours in adults; clinically, dosing every 12 hours maintains effective concentrations. |
| Protein binding | Approximately 40% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd is approximately 4.5 L/kg, indicating extensive distribution beyond plasma. |
| Bioavailability | Intranasal: approximately 60% absolute bioavailability compared to intravenous administration. |
| Onset of Action | Intranasal: symptom relief begins within 30 minutes, with maximal effect at 1 hour. |
| Duration of Action | Duration is 12 hours, supporting twice-daily dosing. |
1 spray (137 mcg olopatadine hydrochloride per spray) in each nostril twice daily.
| Dosage form | SPRAY, METERED |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment; for severe renal impairment (CrCl <30 mL/min), use with caution as safety not established. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment; for severe hepatic impairment (Child-Pugh class C), use with caution as safety not established. |
| Pediatric use | Children 6-11 years: 1 spray per nostril twice daily. Children 12 years and older: same as adult. |
| Geriatric use | No specific adjustment required; use same dose as younger adults, but monitor for adverse effects due to potential age-related comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PATANASE (PATANASE).
| Breastfeeding | It is not known whether olopatadine is excreted in human breast milk. In animal studies, olopatadine was detected in the milk of lactating rats following oral administration. Because many drugs are excreted in human milk, caution should be exercised when Patanase is administered to a nursing woman. The M/P ratio is not available for humans. |
| Teratogenic Risk | Patanase (olopatadine hydrochloride) is classified as FDA Pregnancy Category C. In animal studies, olopatadine was not teratogenic in rats or rabbits at oral doses up to 600 mg/kg/day (approximately 10,000 times the maximum recommended human intranasal dose). However, because adequate and well-controlled studies in pregnant women are lacking, Patanase should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. There are no known specific fetal risks associated with intranasal olopatadine use in any trimester. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to olopatadine or any component of the formulation."]
| Precautions | ["Epistaxis (nosebleed) and nasal ulceration: monitor for nasal mucosal erosions; discontinue if severe.","Somnolence: may impair ability to drive or operate machinery.","Avoid use in patients with severe hepatic impairment (Child-Pugh Class C) due to lack of data.","Pregnancy: limited data; use only if benefit outweighs risk.","Lactation: caution due to possible excretion in breast milk."] |
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| Fetal Monitoring | No specific maternal or fetal monitoring is routinely required during Patanase use. However, as with any medication during pregnancy, standard obstetrical monitoring is appropriate. Patients should be observed for adverse effects such as nasal irritation, epistaxis, or somnolence. |
| Fertility Effects | There are no known effects of Patanase on human fertility. In animal studies, oral olopatadine did not impair fertility in rats at doses up to 200 mg/kg/day. No human data are available. |