Olopatadinum
Olopatadinum Uses, Dosage, Side Effects, Food Interaction and all others data.
Olopatadinum, an antihistamine, works by blocking the action of histamine in the body, which reduces allergy symptoms. Olopatadinum Hydrochloride treats sneezing, itching, runny nose, and other nasal symptoms of allergies. Olopatadinum Nasal Spray contains 0.6% w/v Olopatadinum (base) in a nonsterile aqueous solution with pH of approximately 3.7. After initial priming (5 sprays), each metered spray from the nasal applicator delivers 100 microliters of the aqueous solution containing 665 mcg of olopatadine Hydrochloride, which is equivalent to 600 mcg of Olopatadinum (base). Olopatadinum Nasal Spray also contains benzalkonium chloride (0.01%), dibasic sodium phosphate, edetate disodium, sodium chloride, hydrochloric acid and/or sodium hydroxide (to adjust pH), and purified water.
Inflammatory reactions in response to various stimuli are mediated by endogenous mediators and other pro-inflammatory factors. Histamine receptor activation and mast cell degranulation are primary mechanisms that cause inflammatory reactions such as ocular itching, hyperemia, chemosis, eyelid swelling, and tearing of seasonal allergic conjunctivitis. Olopatadinum is an anti-allergenic molecule and mast cell stabilizer that inhibits the in vivo type 1 immediate hypersensitivity reaction. By blocking the effects of histamine, olopatadine works to reduce the symptoms of allergies and inflammation at various sites of administration, including the eyes and nose. It has shown to exert antihistaminic effects in isolated tissues, animal models, and humans. Olopatadinum also demonstrated dose-dependent inhibition of immunologically-stimulated release of histamine from rat basophilic leukemia cells and human conjunctival mast cells in vitro. Olopatadinum has a relatively rapid onset of action and prolonged duration, where it was shown to mediate anti-histaminic effects at 5 minutes to 24 hours post-administration.
While olopatadine is a non-sedating antihistamine agent, there have been reports of somnolence in some patients taking nasal olopatadine during clinical trials. Temporary blurred vision or other visual disturbances were observed following ophthalmic administration. Olopatadinum has negligible effects on alpha-adrenergic, dopamine, muscarinic type 1 and 2, and serotonin receptors. In clinical trials, there was no evidence of any effect of olopatadine on QT prolongation was observed following intranasal administration.
| Trade Name | Olopatadinum |
| Availability | Rx and/or OTC |
| Generic | Olopatadine |
| Olopatadine Other Names | Olopatadin, Olopatadina, Olopatadine, Olopatadinum |
| Related Drugs | ketorolac ophthalmic, Patanol, Pataday, Lotemax, Acular, loteprednol ophthalmic |
| Type | |
| Formula | C21H23NO3 |
| Weight | Average: 337.4122 Monoisotopic: 337.167793607 |
| Protein binding | About 55% of total olopatadine is bound to human serum proteins, with serum albumin being the primary protein of binding. |
| Groups | Approved |
| Therapeutic Class | Nasal Anti-histamine preparations |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Olopatadinum Nasal Spray is an H1 receptor antagonist used for the relief of the symptoms of seasonal allergic rhinitis in adults and children 6 years of age and older.
Olopatadinum is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis
How Olopatadinum works
Histamine is a biogenic vasoactive amine that binds to its receptors, which are G-protein coupled receptors. Signaling through the histamine H1 receptor is thought to primarily promote the activation of inflammatory reactions, such as allergy, asthma, and autoimmune diseases. H1 receptor signaling activates the intracellular transcription factors, such as IP3, PLC, PKC, DAG, and intracellular calcium ions, which all work to activate further downstream cascades. Activated downstream cascades lead to the production of cytokines, the release of mast cell inflammatory mediators, synthesis of prostacyclins, activation of platelet factor, as well as the synthesis of nitric oxide, arachidonic acid, and thromboxane, which all contribute to inflammatory reactions.
Olopatadinum is an anti-allergic molecule that works via several mechanisms. As a mast cell stabilizer, it stabilizes rodent basophils and human conjunctival mast cells and inhibits the immunologically-stimulated release of histamine. Olopatadinum acts as an antagonist at the histamine H1 receptors with high selectivity, which is explained by a unique receptor binding pocket that consists of the aspartate residue in the third transmembrane helix and other sites in the H1 receptor. Upon binding, olopatadine blocks the H1 receptor signaling pathway, inhibiting the release of inflammatory mediators, such as tryptase, prostaglandin D2, TNF-alpha, as well as pro-inflammatory cytokines. It also decreases chemotaxis and inhibits eosinophil activation. In vitro, olopatadine was shown to inhibit epithelial cell intercellular adhesion molecule-1 (ICAM-1), which promotes the recruitment of migrating pro-inflammatory mediators.
Dosage
Olopatadinum dosage
Adults and Adolescents 12 years of age and older: Two sprays per nostril twice daily.
Children 6 to 11 years of age: One spray per nostril twice daily.
Administer OlopatadinumNasal Spray by the intranasal route only.
Side Effects
A bitter taste in the mouth, nosebleeds, or irritation/soreness in the nose may occur. Drowsiness may rarely occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Toxicity
Based on the findings of an acute toxicity study in animals, the oral LD50 of olopatadine was >1150 mg/kg in mice and >3870 mg/kg in rats. The Lowest published toxic dose via the oral route was 20 mg/kg in rat and 0.1 mg/kg in mouse.
There are no known reports on overdosage following oral, ophthalmic, or intranasal administration of olopatadine. Likely symptoms of antihistamine overdose may include drowsiness in adults and, initially, agitation and restlessness, followed by drowsiness in children. In case of suspected overdose, supportive and symptomatic treatment is recommended.
Precaution
Before initial use, Olopatadinum Nasal Spray by releasing 5 sprays or until a fine mist appears. When Olopatadinum Nasal Spray has not been used for more than 7 days, re-prime by releasing 2 sprays. Avoid spraying Olopatadinum Nasal Spray into the eyes. Patients should be informed to avoid spraying Olopatadinum Nasal Spray in their eyes.
Interaction
Interaction with other medications have not been investigated.
Food Interaction
No interactions found.Volume of Distribution
In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent volume of distribution was 133.83 L.
Elimination Route
Ocular administration of olopatadine in healthy subjects resulted in the Cmax of 1.6 ± 0.9 ng/mL, which was reached after about 2.0 hours. The AUC was 9.7 ± 4.4 ngxh/mL.
The average absolute bioavaiability of intranasal olopatadine is about 57%. Following intranasal administration in healthy subjects, the Cmax of 6.0 ± 8.99 ng/mL at steady-state was reached between 30 minutes to 1 hour after twice daily intranasal administration. The average AUC was 66.0 ± 26.8 ng·h/mL. In patients with seasonal allergic rhinitis, the Cmax of 23.3 ± 6.2 ng/mL at steady-state was reached between 15 minutes and 2 hours post-dosing and the average AUC was 78.0 ± 13.9 ng·h/mL.
Half Life
Following ocular administration, the elimination half-life of olopatadine was 3.4 ± 1.2 hours. In oral pharmacokinetics study, the elimination half-life was reported to be 8 to 12 hours.
Clearance
In an open-label study consisting of healthy Chinese subjects receiving oral administration of olopatadine, the mean apparent oral clearance (CL/F) was 23.45 L/h.
Elimination Route
Olopatadinum is mainly eliminated through urinary excretion. Following oral administration, about 70% and 17% of the total dose was recovered in the urine and feces, respectively.
Pregnancy & Breastfeeding use
Pregnancy Category C; No adequate and well-controlled studies in pregnant women have been conducted. Olopatadinum Nasal Spray should be used in pregnant women only if the potential benefit to the mother justifies the potential risk to the embryo or fetus.
Lactation: It is not known whether topical nasal administration could result in sufficient systemic absorption to produce detectable quantities in human breast milk. Olopatadinum Nasal Spray should be used by nursing mothers only if the potential benefit to the patient outweighs the potential risks to the infant.
Special Warning
There have been no reported overdoses with Olopatadinum Nasal Spray.
Innovators Monograph
You find simplified version here Olopatadinum
Olopatadinum contains Olopatadine see full prescribing information from innovator Olopatadinum Monograph, Olopatadinum MSDS, Olopatadinum FDA label
FAQ
What is Olopatadinum used for?
Olopatadinum is a medication used to decrease the symptoms of allergic conjunctivitis and allergic rhinitis. It is used as eye drops or as a nasal spray. The eye drops generally result in an improvement within half an hour.
How safe is Olopatadinum?
Olopatadinum 0.2% administered once-daily for 6 weeks is safe and well tolerated in children and adolescent patients.
How does Olopatadinum work?
Olopatadinum works by preventing the release of substances that cause eye itching.
What are the common side effects of Olopatadinum?
Common side effects of Olopatadinum are include:
- headache,
- blurred vision,
- burning/stinging/redness/dryness/ irritation/itching of the eye,
- swollen or puffy eyelids,
- stuffy or runny nose,
- cough,
- sore throat,
- weakness,
- back pain,
- a feeling as if something is in your eye, or
- unusual or unpleasant taste in your mouth.
Is Olopatadinum safe during pregnancy?
Olopatadinum are not recommended for use in patients who are pregnant.
Is Olopatadinum safe during breastfeeding?
Because absorption from the eye is limited, olopatadine would not be expected to cause any adverse effects in breastfed infants.
Can I drink alcohol with Olopatadinum?
Drinking alcohol can increase certain side effects of Olopatadinum nasal.
Can I drive after taking Olopatadinum?
Do not drive, use machinery, or do any activity that requires clear vision until you are sure you can perform such activities safely.
How long does Olopatadinum take to work?
Olopatadinum hydrochloride 0.1% ophthalmic solution reduced itching as early as 30 minutes after the instillation and a higher percentage of patients reported improvement with Olopatadinum hydrochloride 0.1% ophthalmic solution than with ketotifen fumarate 0.05% ophthalmic solution.
How long does Olopatadinum stay in my system?
Olopatadinum effect lasts 24 hours.
Can I use Olopatadinum every day?
Adults and children 2 years of age and older, put one drop in each affected eye once a day. Children younger than 2 years of age, use and dose must be determined by your doctor.
How often can I use Olopatadinum ?
Put one drop in each affected eye two times a day, at least 6 to 8 hours apart.
How long can I take Olopatadinum?
Olopatadinum usually given for up to 14 weeks.
Who should not take Olopatadinum?
You should not use Olopatadinum ophthalmic if you are allergic to it. Ask a doctor or pharmacist if Olopatadinum ophthalmic is safe to use if you have any type of eye infection. Tell your doctor if you are pregnant or breastfeeding. Olopatadinum ophthalmic is not approved for use by anyone younger than 2 years old.
What happens if I use too much Olopatadinum?
An overdose of Olopatadinum ophthalmic is not expected to be dangerous. Seek emergency medical attention if anyone has accidentally swallowed the medication. Avoid wearing contact lenses while your eyes are red or irritated.
What happens if I miss a dose?
Use the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not use two doses at one time.
What happen If I stop taking Olopatadinum?
If you stop using the Olopatadinum suddenly or don’t use it at all: Your itchy eyes caused by allergies may get worse.
Is Olopatadinum an antihistamine?
Olopatadinum is in a class of medications called antihistamines.
