Olopat Ax

Olopat Ax Uses, Dosage, Side Effects, Food Interaction and all others data.

Ambroxol is a metabolite of Bromhexine. It possesses mucokinetic (improvement in mucus transport) and secretolytic (liquefies secretions) properties. Ambroxol stimulates the serous cells of the glands of the mucous membrane of bronchi, increasing the content of mucus secretion. The mucolytic effect is associated with depolymerization and splitting of mucoproteins and mucopolysaccharide fibres, which leads to reduction in the viscosity of mucus. Expectoration of mucus is facilitated and breathing is eased considerably. Ambroxol stimulates production of phospholipids of surfactant by alveolar cells. Ambroxol has anti-inflammatory properties. In patients with COPD, it improves airway patency. Beside these, Ambroxol also exhibits anti-oxidant activity. Long-term use is possible because of the good tolerability of the preparation.

Olopatadine, an antihistamine, works by blocking the action of histamine in the body, which reduces allergy symptoms. Olopatadine Hydrochloride treats sneezing, itching, runny nose, and other nasal symptoms of allergies. Olopatadine Nasal Spray contains 0.6% w/v Olopatadine (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 Olopatadine (base). Olopatadine 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. Olopatadine 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. Olopatadine also demonstrated dose-dependent inhibition of immunologically-stimulated release of histamine from rat basophilic leukemia cells and human conjunctival mast cells in vitro. Olopatadine 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. Olopatadine 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.

Olopat Ax
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Olopat Ax
Generic	Ambroxol + Olopatadine
Weight	30mg
Type	Tablet
Therapeutic Class
Manufacturer	Ajanta Pharma Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

• Acute and chronic diseases of respiratory tracts associated with viscid mucus including acute and chronic bronchitis
• Productive cough
• Inflammatory diseases of Rhinopharyngeal tract (e.g. Laryngitis, Pharyngitis, Sinusitis and Rhinitis) associated with viscid mucus
• Asthmatic bronchitis, Bronchial asthma with difficult departure of mucus
• Bronchiectasis
• Chronic pneumonia.

Olopatadine 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.

Olopat Ax is also used to associated treatment for these conditions: Airway secretion clearance therapyAllergic Rhinitis (AR), Seasonal Allergic Conjunctivitis, Seasonal Allergic Rhinitis

How Olopat Ax works

Ambroxol is a mucolytic agent. Excessive Nitric oxide (NO) is associated with inflammatory and some other disturbances of airways function. NO enhances the activation of soluble guanylate cyclase and cGMP accumulation. Ambroxol has been shown to inhibit the NO-dependent activation of soluble guanylate cyclase. It is also possible that the inhibition of NO-dependent activation of soluble guanylate cyclase can suppress the excessive mucus secretion, therefore it lowers the phlegm viscosity and improves the mucociliary transport of bronchial secretions.

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.

Olopatadine 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. Olopatadine 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

Olopat Ax dosage

Average daily dose (preferably after meal):Pediatric Drops:

0-6 months: 0.5 ml 2 times a day
6-12 months: 1 ml 2 times a day
1-2 years: 1.25 ml 2 times a day

Syrup:

2-5 years: 2.5 ml (1/2 teaspoonful) 2-3 times a day
5-10 years: 5 ml (1 teaspoonful) 2-3 times a day
10 years and adults: 10 ml (2 teaspoonful) 3 times a day.

Sustained release capsule:

Adult and children over 12 years old: 1 capsule once daily

Specific application features: Ambroxol may be prescribed to patients suffering from diabetes mellitus.

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 OlopatadineNasal Spray by the intranasal route only.

Side Effects

Gastrointestinal side-effects like epigastric pain, gastric fullness may occur occasionally. Rarely allergic responses such as eruption, urticaria or angioneurotic edema may occur.

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

Ambroxol should be given cautiously to patients with gastric and duodenal ulceration or convulsive disorders. Patients with hepatic and renal insufficiency should take it with caution.

Before initial use, Olopatadine Nasal Spray by releasing 5 sprays or until a fine mist appears. When Olopatadine Nasal Spray has not been used for more than 7 days, re-prime by releasing 2 sprays. Avoid spraying Olopatadine Nasal Spray into the eyes. Patients should be informed to avoid spraying Olopatadine Nasal Spray in their eyes.

Interaction

Ambroxol has no interaction with cardioactive glycosides, corticosteroids, bronchodilators, diuretics and antibiotics (normally used in the treatment of bronchopulmonary affections). But Ambroxol should not be taken simultaneously with antitussives (e.g. Codeine) because mucus, which has been liquefied by Ambroxol, might not be expectorated.

Interaction with other medications have not been investigated.

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

Rapid and almost complete.

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

7-12 hours

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

Olopatadine 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: Teratogenic and fetal toxicity studies have shown no harmful effect of Ambroxol. However, it is advised not to use during pregnancy, especially in the 1st trimester.

Lactation: Safety during lactation has not been established.

Pregnancy Category C; No adequate and well-controlled studies in pregnant women have been conducted. Olopatadine 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. Olopatadine Nasal Spray should be used by nursing mothers only if the potential benefit to the patient outweighs the potential risks to the infant.