Olopatadine
Drug class: Antineoplastic Agents
Usage of Olopatadine
Allergic Conjunctivitis
Used ophthalmically for symptomatic management of ocular itching associated with allergic conjunctivitis.
Seasonal Allergic Rhinitis
Used intranasally to provide symptomatic relief of seasonal allergic rhinitis (e.g., hay fever).
Provides symptomatic relief of nasal congestion, rhinorrhea, nasal itching, and sneezing.
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How to use Olopatadine
Administration
Administer intranasally or topically to the eye.
Intranasal Administration
Administer intranasally twice daily, using a metered-dose nasal spray pump. Avoid spraying into the eyes.
Before initial use, prime the pump by releasing 5 sprays or until a fine mist appears. If nasal spray has not been used for >7 days, reprime the pump by releasing 2 sprays.
To actuate the pump, hold the bottle in one hand; with forefinger and middle finger on the shoulders of the pump unit and the thumb on the bottom of the bottle, press down on the shoulders of the pump to produce a fine mist.
Prior to administration, gently blow the nose to clear nasal passages. To administer, close one nostril; then, with head tipped down (chin toward chest), insert nasal applicator ¼ to ½ inch into the other nostril, hold bottle vertically upright, and aim spray tip toward the cheek side of the nose (away from the center of the nose). While gently breathing in through the nose, press firmly and quickly on the pump to release the spray. Breathe out through the mouth.
Do not tip head back or blow the nose immediately after dosing; tipping head back may produce a bitter taste in the mouth.
Repeat procedure for the other nostril. Alternate nostrils between each actuation.
Following administration, wipe nasal applicator with a clean tissue and replace the blue plastic cap.
If nasal applicator becomes clogged, do not attempt to clean by inserting a sharp object. Instead, remove nasal applicator by gently pulling it upward; once removed, wash (while pointing nasal applicator downward) by running warm tap water for about one minute. Shake the applicator to remove any water and place the applicator back on the bottle. Prime by spraying 2 times or until a fine mist appears.
Discard after 240 sprays.
Ophthalmic Administration
Apply topically to the eye as an ophthalmic solution. Not for injection or oral use.
If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.
Avoid contamination of the solution container.
Dosage
Available as olopatadine hydrochloride; dosage expressed in terms of olopatadine.
Nasal spray delivers about 665 mcg of olopatadine hydrochloride (equivalent to 600 mcg of olopatadine) per metered spray and about 240 metered sprays per 30.5-g bottle.
Pediatric Patients
Allergic Conjunctivitis Ophthalmic0.1% ophthalmic solution: In children ≥3 years of age, 1 drop in the affected eye(s) twice daily (at an interval of 6–8 hours).
0.2% ophthalmic solution: In children ≥2 years of age, 1 drop in the affected eye(s) once daily.
Once symptomatic improvement is established, continue therapy for as long as necessary to sustain improvement.
Seasonal Allergic Rhinitis IntranasalChildren 6–11 years of age: 1 spray (600 mcg) in each nostril twice daily.
Children ≥12 years of age: 2 sprays (1200 mcg) in each nostril twice daily.
Adults
Allergic Conjunctivitis Ophthalmic0.1% ophthalmic solution: 1 drop in the affected eye(s) twice daily (at an interval of 6–8 hours).
0.2% ophthalmic solution: 1 drop in the affected eye(s) once daily.
Once symptomatic improvement is established, continue therapy for as long as necessary to sustain improvement.
Seasonal Allergic Rhinitis Intranasal2 sprays (1200 mcg) in each nostril twice daily.
Special Populations
Hepatic Impairment
Nasal spray: Dosage adjustment not necessary.
Hepatic Impairment
Nasal spray: Dosage adjustment not necessary.
Geriatric Patients
Nasal spray: Select dosage with caution. (See Geriatric Use under Cautions.)
Warnings
Contraindications
Nasal spray: Manufacturer states none known.
Warnings/Precautions
Proper Handling to Avoid Contamination of Ophthalmic Solution
To avoid contamination of the dropper tip and solution, do not to touch the eye, eyelids, or surrounding areas with the dropper tip. Close container tightly when not in use.
Contact Lenses
Ophthalmic solution not indicated for contact lens-related ocular irritation. Do not wear contact lenses if eyes are red.
Remove soft contact lenses prior to administration of each ophthalmic dose, since benzalkonium chloride preservative may be absorbed by soft contact lenses; lenses may be reinserted after ≥10 minutes following administration.
Nasal Effects
Epistaxis, nasal ulcerations, and nasal septal perforations reported with nasal spray. Perform nasal examination prior to initiating intranasal olopatadine therapy to ensure absence of nasal diseases (other than allergic rhinitis). Perform nasal examinations periodically for signs of adverse effects on the nasal mucosa. If nasal ulcerations occur, consider discontinuing nasal spray.
CNS Effects
Somnolence reported with nasal spray. Avoid engaging in activities requiring complete mental alertness and motor coordination (e.g., driving or operating machinery) after administration of nasal spray. Concomitant use of nasal spray with alcohol or other CNS depressants may result in additive CNS depression; therefore, avoid such concomitant use.
Specific Populations
PregnancyCategory C.
LactationDistributed into milk in rats following oral administration.
Ophthalmic solution: Not known whether distributed into human milk following topical application to the eye. Use with caution.
Nasal spray: Use only if potential benefits outweigh risks.
Pediatric Use0.1% ophthalmic solution: Safety and efficacy not established in children <3 years of age. Appears to be well-tolerated in children 3–16 years of age.
0.2% ophthalmic solution : Safety and efficacy not established in children <2 years of age.
Nasal spray: Safety and efficacy not established in children <6 years of age. In clinical studies, incidence of epistaxis was higher in children 6–11 years of age (5.7%) compared with adolescents or adults (3.2%).
Geriatric UseOphthalmic solution: No substantial differences in safety and efficacy relative to younger adults.
Nasal spray: Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults. Other clinical experience has not identified differences in responses between geriatric and younger patients. Select dosage with caution because of age-related decreases in hepatic, renal, or cardiac function and potential for concomitant disease and drug therapy.
Common Adverse Effects
0.1% ophthalmic solution: Headache.
0.2% ophthalmic solution: Symptoms similar to cold syndrome, pharyngitis.
Nasal spray: In adults and children ≥12 years of age, bitter taste, headache, epistaxis, pharyngolaryngeal pain, postnasal drip, cough, urinary tract infection. In children 6–11 years of age, epistaxis, headache, upper respiratory tract infection, bitter taste, pyrexia, rash.
What other drugs will affect Olopatadine
No formal drug interaction studies involving ophthalmic solution or nasal spray to date.
Does not inhibit in vitro metabolism of substrates of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4.
Drugs Affecting or Metabolized by Hepatic Enzymes
Interactions with drugs that inhibit hepatic enzymes (e.g., CYP microsomal enzymes) unlikely because olopatadine is eliminated predominantly by renal excretion.
Potential for olopatadine and its metabolites to act as inducers of CYP isoenzymes not evaluated.
Protein-bound Drugs
Interactions with protein-bound drugs (e.g., possible displacement of other protein-bound drugs) unlikely because olopatadine is modestly protein bound.
Specific Drugs
Drug
Interaction
Comments
CNS depressants (e.g., alcohol)
Possible additive CNS depression when used concomitantly with nasal spray
Avoid concomitant use with nasal spray
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