Olopatadine Hydrochloride

Pronunciation: OH-loe-PA-ta-deen HYE-droe-KLOR-ide
Class: Antihistamine

Trade Names

Pataday
- Solution, ophthalmic 0.2%

Patanase
- Nasal spray 0.6%

Patanol
- Solution, ophthalmic 0.1%

Pharmacology

Inhibits release of histamine from mast cells and relatively selective histamine H ₁ antagonist. Inhibits type 1 immediate hypersensitivity reactions.

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Pharmacokinetics

Absorption

T _max is 30 to 60 min, C _max is 16 ng/mL, average absolute bioavailability is 57% (intranasal).

Distribution

Protein binding is approximately 55%.

Metabolism

Not extensively metabolized.

Elimination

Plasma elimination half-life is 3 h (ophthalmic) and 8 to 12 h (intranasal), mainly through urinary excretion.

Special Populations

Mean plasma AUC _0-12 is 2-fold higher. No dosage adjustment is required.

Effects have not been established. No dosage adjustment is required.

Mean C _max was approximately 2-fold less when compared with adults (intranasal).

C _max and AUC were 40% and 27% higher, respectively, in women compared with men (intranasal).

The effects of race have not been adequately investigated.

Indications and Usage

Temporary relief of itching caused by allergic conjunctivitis (ophthalmic); relief of symptoms of seasonal allergic rhinitis (intranasal).

Contraindications

None well documented.

Dosage and Administration

Ophthalmic 1 to 2 drops in affected eye(s) twice daily, 6 to 8 h apart (0.1% solution). 1 drop in affected eye(s) once daily (0.2% solution). If using other topical ophthalmic drugs, separate each medication by 5 min or more.

Intranasal 2 sprays per nostril twice daily.

Intranasal 1 spray per nostril twice daily.

General Advice

• Ophthalmic
• Do not instill while wearing contact lenses.

• Intranasal
• Prime the nasal spray by releasing 5 sprays, or until a fine mist appears. When not in use for more than 7 days, re-prime by releasing 2 sprays.
• Discard nasal device after 240 sprays have been used.

Storage/Stability

Store between 39° and 77°F. Keep bottle tightly closed.

Drug Interactions

Avoid concurrent use (intranasal) because additional reductions in alertness and impaired CNS function could occur.

Adverse Reactions

CNS

Asthenia (5% or less); headache (4%); fatigue, somnolence (1%); depression or worsening of depression.

GI

Bitter taste (13%); nausea, taste perversion.

Ophthalmic

Blurred vision; burning, dry eye, foreign body sensation, hyperemia, keratitis, lid edema, pruritus, stinging (5% or less).

Respiratory

Upper respiratory tract infection (3%); pharyngolaryngeal pain (2%); cough, nasopharyngitis (1%).

Special Senses

Epistaxis (25%); nasal ulceration (10%); postnasal drip (2%); dry mouth, throat irritation (1%); rhinitis, sinusitis.

Miscellaneous

CPK elevation, influenza, pyrexia, rash, UTI (1%); dysgeusia, flu syndrome, weight increase.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and effectiveness in children younger than 3 yr of age are not established (ophthalmic); safety and effectiveness in children younger than 6 yr of age not established (intranasal).

Elderly

Use caution in dose selection, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Patient Information

• Advise patient that usual dose is 1 drop in affected eye(s) twice daily at an interval of 6 to 8 h (0.1% solution) or 1 drop once daily in the affected eye(s) (0.2% solution).
• Teach patient proper technique for instilling eye drops: wash hands; do not allow dropper to touch eye; tilt head back, look up; pull lower eyelid down; instill prescribed number of drops; close eye for 1 to 2 min and apply gentle pressure to bridge of nose; do not rub eye.
• Advise patients who wear contact lenses to remove their lenses before instilling this medicine and to wait at least 10 min after instilling eye drop before inserting their lenses. Also, caution these patients to not wear their lens if the eye is red.
• Advise patient that if more than 1 topical ophthalmic drug is being used, to administer the drugs at least 5 min apart.
• Advise patient to inform health care provider if experiencing side effects or if eye symptoms do not improve or worsen.
• Advise patients to avoid spraying nasal spray in their eyes.
• Advise patient to avoid engaging in hazardous occupations requiring complete mental alertness (eg, driving).
• Inform patients that the nasal spray adverse reactions (eg, bitter taste, epistaxis, nasal ulcerations, postnasal drip) may occur and to inform their health care provider if these symptoms do not improve.
• Advise patients to avoid concurrent use with alcohol or other CNS depressants.

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