Drug information of Olopatadine

Mechanism of effect

Olopatadine is a selective histamine H1 antagonist that binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Olopatadine is devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors.

Pharmacodynamic

Used to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells.
It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells.

Pharmacokinetics

• Absorption:
ophthalmic: Limited systemic
nasal :
- Onset of action: 30 min (seasonalallergy)
- Systemic 57%
- Bioavailability 57%
- Peak Plasma Time: 0.25-2 hr
- Peak Plasma Concentration: 23.3 ng/mL
• Distribution :
ophthalmic: Protein binding: ~55%
nasal :
Protein Bound: 55%(predominantly albumin)
• Metabolites
ophthalmic: N-desmethylolopatadine; olopatadine N-oxide
nasal :
Liver; not extensive
N-desmethylolopatadine; olopatadine N-oxide
• Excretion
ophthalmic: Urine (60-70%); feces (17%) Half-Life: 3 hr
nasal :
Half-Life: 8-12 hr
Urine (60-70% unchanged); feces (17%)

Dosage

• nasal:
- nasal spray: 6% (665mcg/100 microliters spray)
- Seasonal Allergic Rhinitis :2 sprays per nostril q12hr
Seasonal Allergic Rhinitis
<6 years: Safety and efficacy not established
6-12 years: 1 spray per nostril q12hr
>12 years: 2 sprays per nostril q12hr
ophthalmic solution0.1%0.2%0.7%
Allergic Conjunctivitis
Indicated for the treatment of ocular itching associated with allergic conjunctivitis
0.1% solution (Patanol): 1 gtt BID in affected eye(s) at an interval of 6-8 hr
0.2% solution (Pataday): 1 gtt in affected eye(s) qDay
0.7% (Pazeo): 1 gtt in affected eye(s) qDay
Allergic Conjunctivitis
Indicated for the treatment of ocular itching associated with allergic conjunctivitis
<2 years (Pataday, Pazeo) or <3 years (Patanol): Safety and efficacy not established

Drug contraindications

hypersensitivity to this drug

Side effects

nausea , Headache , Blurred vision , Depression , Cough , sinusitis , Hypersensitivity , dry eyes , Weight increase , Epistaxis , difficulty urinating , tiredness , rhinitis , hyperemia , itchy eyes

Interactions

Clobazam , Bromazepam

Alerts

1. Remove contact lenses prior to administration; wait 10 min after administration before reinsertion
2. Do not use contact lenses if eyes are red
3. May cause epistaxis, nasal ulceration, or nasal septal perforation
4. Avoid with nasal disease other than allergic rhinitis
5. May impair mental/physical abilities required for hazardous tasks (eg, driving, operating machinery)
6. Avoid concurrent use of alcohol or other CNS depressants

Points of recommendation

1. You should not use olopatadine ophthalmic if you are allergic to it.
2. To make sure olopatadine ophthalmic is safe for you, tell your doctor if you have any type of infection in your eye.
3. It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.
4. It is not known whether olopatadine ophthalmic passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.
5. Do not give this medicine to a child without medical advice.
6. Before using olopatadine nasal , tell your doctor if you have any non-allergic conditions affecting the inside of your nose, such as a deviated septum.
7. Drinking alcohol can increase certain side effects of olopatadine nasal.
8. Call your doctor if your symptoms do not improve, or if they get worse while using olopatadine nasal.

Pregnancy level

C

Related drugs

Azelastine , Alcaftadine , Pemirolast-Ophthalmic , Nedocromil Sodium , Lodoxamide , Emedastine , Bepotastine , Epinastine