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. |
| Molecular Weight | 373.87 Da (olopatadine hydrochloride) |
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 | Insufficient human data; animal studies show no teratogenicity at high doses. Use only if potential benefit justifies potential risk to fetus. |
| 2nd trimester | No evidence of fetal harm from topical intranasal use; systemic absorption minimal. |
| 3rd trimester | No known risks; minimal systemic exposure. |
Clinical note
Comprehensive clinical and safety monograph for PATANASE (PATANASE).
| Placental transfer | Unknown; molecular weight suggests possible transfer, but systemic bioavailability is extremely low (<0.1%) after intranasal use, likely resulting in negligible fetal exposure. |
| Breastfeeding | Systemic absorption of patanase (olopatadine) following intranasal administration is minimal; however, caution is advised due to potential for anticholinergic effects in infants. Consider benefits of breastfeeding and importance of drug to mother. |
■ 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. |
| Food/Dietary | No specific food interactions. Avoid grapefruit juice if concurrent use of CYP3A4 substrates (minimal interaction with olopatadine). Alcohol may potentiate CNS depressant effects; limit use. |
Loading safety data…
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
| Clinical Pearls |
| Patanase (olopatadine hydrochloride) is an intranasal antihistamine for allergic rhinitis. Onset of action within 30 minutes. Avoid use in patients with narrow-angle glaucoma or urinary retention. May cause epistaxis, nasal ulceration, or nasal septal perforation with prolonged use. Monitor for drowsiness; concurrent CNS depressants may exacerbate sedation. Not for oral or ophthalmic use. |
| Patient Advice | Use exactly as prescribed; do not exceed 2 sprays per nostril twice daily. · Prime pump before first use or after 7 days of non-use by spraying 5 times or until a fine mist appears. · Avoid spraying into eyes; if contact occurs, rinse eyes with water for 10 minutes. · Common side effects include mild nosebleeds, nasal burning, or headache. · Report persistent nosebleeds, severe nasal pain, or changes in vision. · May cause drowsiness; avoid driving or operating machinery until you know how it affects you. |