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Astelin (Azelastine)
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Astelin

Astelin is a nasal spray which is used for treating allergy symptoms and symptoms of nasal passage inflammation. Astelin contains azelastine, an antihistamine. It blocks the effects of the chemical histamine in your body. Astelin prevents sneezing, itching, runny nose, and other nasal symptoms of allergies.

Other names for this medication:
Adomessen, Afluon, Afluon nasal, Alager, Allergodil, Allergospray, Amsler, Antalerg, Armin, Astepro, Asutoputin, Az ofteno, Azel, Azelastin, Azelastina, Azelastine, Azelastinum, Azelone, Azen, Azep, Azepit, Azeptin, Bifertin, Brixia, Cobatect, Corifina, Lasticom, Lastin, Oculastin, Optilast, Optivar, Otrivin azelastine, Otrivin heuschnupfen, Otrivine, Prorhinite, Raspjine, Rhinolast, Rinalin, Rino-lastin, Snizex, Sophistina, Xanaes

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Also known as: Azelastine.

Description

Astelin belongs to a group of medicines called antihistamines.

Astelin provides relief from bothersome nasal symptoms such as congestion, itchy/runny nose, sneezing and postnasal drip due to seasonal allergens or environmental irritants.

Astelin is steroid-free, does not contain pseudoephedrine, and relieves your symptoms by blocking the effects of histamine - the primary cause of allergy symptoms.

What makes Astelin unique is that it is a steroid-free antihistamine nasal spray that provides symptom relief whether the trigger is an allergen (grass, trees, pollen, mold, etc.), an irritant (cigarette smoke, perfume, cleaning agents, car exhaust, cold air, etc.), or both.

Astelin is also know as Azelastine, Arzep, Rhinolast, Alerdual, Allergodil, Rinalin.

Generic name of Astelin is Azelastine.

Dosage

Follow the directions for using this medicine provided by your doctor. Use Astelin exactly as directed.

Astelin can be used by patients as young as 5 years of age, depending on what type of rhinitis they have been diagnosed with.

For those with seasonal allergic rhinitis, patients from 5 to 11 years of age should administer 1 spray in each nostril twice daily.

Patients 12 years of age and older with seasonal allergic rhinitis should administer 2 sprays of Astelin in each nostril twice daily.

For those with nonallergic vasomotor rhinitis, patients 12 years of age and older should administer 2 sprays of Astelin in each nostril twice daily.

Before using Astelin for the first time, remove the child-resistant screw cap and replace with the pump unit. Prime the delivery system (pump unit) with four sprays or until a fine mist appears. If 3 days or more have elapsed since your last use of the nasal spray, reprime the pump with two sprays or until a fine mist appears.

Overdose

If you overdose Astelin and you don't feel good you should visit your doctor or health care provider immediately.

Storage

Store at a room temperature between 15 and 30 degrees C (59 and 86 degrees F) away from moisture and sunlight. Keep in a tightly closed container. Throw away the after the expiration date. Keep out of the reach of children.

Side effects

The most common side effects associated with Astelin are:

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Side effect occurrence does not only depend on medication you are taking, but also on your overall health and other factors.

Contraindications

Do not take Astelin if you are allergic to Astelin components.

It is not known whether Astelin will harm an unborn baby. Do not use this medicine without your doctor's advice if you are pregnant or breast-feeding.

The medicine has a antihistamine in it. Before you start any new medicine, check the label to see if it has an antihistamine (e.g., diphenhydramine) in it too. If it does or if you are not sure, check with your doctor or pharmacist.

Astelin may cause harm if it is swallowed. If you may have taken it by mouth, contact your poison control center or emergency room right away.

Astelin should be used with extreme caution in children younger than 5 years old; safety and effectiveness in these children have not been confirmed.

Do not drink alcohol or use medicines that may cause drowsiness (e.g., sleep aids, muscle relaxers) while you are using Astelin; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness.

Astelin may cause drowsiness. These effects may be worse if you take it with alcohol or certain medicines. Use Astelin with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.

Do not stop taking Astelin suddenly.

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Both ANS and LNS were effective and safe in the treatment of moderate-to-severe persistent allergic rhinitis. Moreover, LNS reached a higher symptom relief rate within 30 min of administering the first dose.

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In anaesthetized domestic pigs a filter paper sampling technique was applied to estimate basal and histamine induced nasal secretion. Histamine (0.2 mg/nostril) increased secretion more than twofold, a dose of 2 mg/nostril more than 10 fold. Intranasally instilled azelastine (A-5610, CAS 58581-89-8) prevented this histamine induced rhinorrhea without reduction of basal secretion. The protective effect remained for more than 2 h even when histamine challenge was repeated.

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Azelastine nasal spray is a topical antihistaminic drug for the symptomatic treatment of allergic rhinitis. This study aimed to investigate the effects of azelastine on nasal and nasopharyngeal microflora.

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Thirty patients of laryngopharyngeal reflux disease were diagnosed in ENT outpatient department in our hospital. All patients have symptoms of sneeze, nasal discharge as chief complaint and they responded no effect for other normal treatment for nasal-sinusitis at least three months. Orally before meals, a dose of 5 mg Mosapride citrate each time, three times a day for 7 days. Orally before meals, a dose of 20 mg Esomeprazole each time, two times a. day for 2-3 months. Nasal spray, one spray of azelastine hydrochloride once, two times a day for 2 month.

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Azelastine is used for symptomatic relief of allergic rhinitis and asthma bronchiale. In vitro studies in smooth muscle cells from guinea pig trachea and ileum demonstrate that the drug blocks L-type Ca(2+) current (I(Ca, L)). However, for safety reasons, it is important to know whether azelastine also affects cardiac I(Ca, L) in therapeutically relevant concentrations. We have therefore studied the effects of azelastine on I(Ca, L) in guinea pig ventricular myocytes using standard whole-cell patch-clamp technique. Force of contraction and action potentials from isolated papillary muscles of the same species were also investigated at physiological temperature (36 degrees C). Azelastine (30 microM) significantly reduced force of contraction, shortened action potential duration, and depressed maximum upstroke velocity. I(Ca, L) was elicited by 200-ms-long clamp steps from -100 to 0 mV (one pulse every 3 s). Azelastine blocked I(Ca, L) reversibly and concentration-dependently with an IC(50) of 20.2+/-1.3 microM and a Hill coefficient of 1.1. At 10 microM, azelastine shifted steady-state inactivation by 5 mV (n=7) to more negative potentials. The time course of I(Ca, L) inactivation could be described by a double exponential function. Azelastine (10 microM) significantly shortened the slow inactivation time constant (tau(s)) from 54.2+/-2.8 ms under control conditions to 38.7+/-2.9 ms (n=16) in the presence of drug. Azelastine also reduced low-voltage-activated Ca(2+) currents with a similar IC(50) value (24 microM, at -35 mV). Since the therapeutic plasma concentrations are in the order of 10-100 nM, we conclude that azelastine does indeed affect also cardiac I(Ca, L), but the concentrations required are at least two orders of magnitude larger than those obtained during drug therapy.

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1. The ability of dextro-mequitamium iodide (d-Meq) to antagonize bronchomotor and inflammatory effects mediated by histamine and antigen challenge in the upper or lower guinea pig airways or both and its potential activity against the recruitment and activation of eosinophils in the bronchial wall have been evaluated in comparison with azelastine. 2. In receptor-binding studies, d-Meq displayed a nanomolar affinity for H1 and muscarinic receptors, and it was endowed with potent bronchodilating properties in the nanomolar range toward tonic contractions induced by histamine and carbachol. 3. d-Meq (100-1,000 nmol/guinea pig) and azelastine (100-5,000 nmol/guinea pig) administered by aerosol significantly inhibited histamine- and antigen-induced increases in insufflation pressure in sensitized animals. 4. d-Meq (1,000-6,000 nmol/kg i.v.) dose dependently inhibited the histamine- or antigen-induced increase in vascular permeability in the upper airways. 5. d-Meq was more effective against histamine than antigen challenge, and its potency was similar or greater than that of azelastine. 6. Aerosolized d-Meq (1,000 nmol/animal) reduced antigen-induced eosinophil accumulation in the bronchoalveolar lavage (BAL) fluid from sensitized guinea pigs. 7. Eosinophils recovered from the BAL fluid of antigen-challenged animals showed an increased chemotaxis in response to LTB4 or platelet-activating factor. Both d-Meq and azelastine (300 nmol/animal) reduced this increase without affecting direct chemotaxis induced by leukotriene B4 (LTB4). 8. These findings provide evidence that local administration of d-Meq might be useful in the treatment of allergic disorders, such as rhinitis and asthma.

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The study was designed to compare the effectiveness and safety of two dosages of azelastine nasal spray (2 sprays per nostril once daily and twice daily) with that of placebo in the treatment of patients with symptomatic seasonal allergic rhinitis.

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We have investigated the effect of azelastine on bronchial responsiveness in 25 asthmatics, using methacholine inhalation challenge, (Astograph). Three parameters, initial respiratory resistance (RrsC), bronchial sensitivity (Dmin), and bronchial reactivity (SGrs/GrsC) were studied. After 8 weeks' treatment with 2 mg azelastine b.i.d., Dmin was increased significantly and after 4 weeks an insignificant increase was observed. RrsC and SGrs/GrsC did not change significantly during the 8 week treatment. Recent advances have revealed that various chemical mediators, especially leukotrienes, are closely related to bronchial hyperresponsiveness. Accordingly, the improvement of Dmin observed during azelastine treatment might be ascribed to its inhibitory action on the synthesis and release of leukotrienes.

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Azelastine (AZE) in a novel, eye drop, formulation, was compared with topically applied sodium cromoglycate (SCG) and placebo (PLA) in the treatment of seasonal allergic conjunctivitis or rhino-conjunctivitis in a multicentre, parallel group study.

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The mechanism of inhibitory effects of azelastine, an antiallergic and antiasthmatic agent, on depolarization- and alpha-1 adrenergic agonist-induced contractions of intact smooth muscle was studied. The effects of azelastine on membrane currents were determined in isolated guinea pig ileum smooth muscle cells with the whole-cell clamp technique; the effects on contraction were evaluated in receptor- and G-protein-coupled, alpha-toxin-permeabilized rabbit femoral artery and portal vein smooth muscle strips. Azelastine (1-20 microM), like dihydropyridines, inhibited spontaneous rhythmic and high K(+)-induced contractions, mainly through inhibition of the voltage-dependent (L-type) Ca++ current. The tonic component of high K+ contractions was inhibited more than the phasic component, correlating to voltage-dependent inhibition of Ca++ current by the drug. Azelastine (IC50 of 0.25 microM), a known histamine blocker, also reversibly inhibited alpha-1 agonist-induced contractions in the presence and absence of extracellular Ca++. Both major pathways of pharmacomechanical coupling, agonist-induced Ca++ release from the sarcoplasmic reticulum and Ca++ sensitization of the regulatory/contractile apparatus were blocked by the same concentration of drug in permeabilized as in intact muscle. Inositol 1,4,5-trisphosphate-induced Ca++ release and guanosine 5'-O-(tau-thiotriphosphate)-induced Ca++ sensitization, however, were not inhibited. Azelastine at high (greater than 10 microM) concentrations reversibly inhibited Ca(++)-activated contraction, more potently at lower Ca++ concentration and in phasic smooth muscle, but inhibited neither adenosine 5'-O-(tau-thiotriphosphate)-induced, Ca(++)-independent nor phorbol ester-induced contractions. These results indicate that azelastine is a genuine Ca++ antagonist that inhibits voltage-gated Ca++ inward current and agonist-induced Ca++ release and Ca++ sensitization.

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There is no shortage of pharmacologic treatments available for the management of allergic rhinitis (AR), but none regularly provide full relief from all symptoms. MP29-02 (Dymista®) is a novel intranasal formulation of azelastine hydrochloride (AZE) and fluticasone propionate (FP), benefiting from an enhanced formulation Zithromax Online Order and improved device characteristics compared to marketed intranasal corticosteroid (INS) formulations. Results from large, randomized, double-blind, placebo-controlled, head-to-head trials versus first-line therapies, confirmed MP29-02 as the evidence-based drug-of-choice for AR treatment. MP29-02 was twice as effective as AZE or FP for nasal and ocular symptom relief in moderate to severe seasonal AR patients, with superiority documented regardless of season, and in more severe patients. More MP29-02-treated patients experienced clinically relevant responses (i.e., halving of nasal symptom burden and complete/near-to-complete relief) days faster than those on INS or intranasal antihistamine monotherapy. MP29-02's efficacy was sustained long-term versus FP (up to 52 weeks) in chronic rhinitis patients (perennial AR or nonallergic rhinitis), with 7 out of 10 patients first becoming symptom-free following 1 month's treatment with MP29-02, and days faster than with the INS. These results confirm MP29-02's superiority over the historical gold-standard therapy for AR (i.e., INS), and position it now as first-line treatment for moderate to severe AR patients, the majority of whom are uncontrolled on existing medications.

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Azelastine hydrochloride nasal spray is available worldwide for Propecia Buy the treatment of seasonal allergic rhinitis (SAR) and perennial allergic rhinitis. One spray per nostril twice daily is the most commonly recommended dose.

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The objective of this 8-week, double-blind, placebo-controlled study was to determine whether topical Diamox Cost India nasal azelastine was effective at decreasing congestion, daytime somnolence, and improving sleep.

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These results suggest that antihistamines, especially FEX, suppress CC chemokine production from CD14+ cells through interference with antigen-mediated signaling and result in favorable Priligy Online Pharmacy modification of allergic disease states or conditions.

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The degranulation capacity of primary mast cells, as well as gene expression and release of inflammatory mediators from human lung epithelial cells (A549 cells) were analyzed in relation to the synthetic drugs azelastine and dexamethasone. Gene and protein expression of cyclooxygenase-2 were investigated by semi-quantitative RT-PCR and western blotting, respectively. The involvement of phosphorylated mitogen-activated protein kinases and NF-κB signaling in regulation Asacol Generic of these molecules were characterized by western blotting and electrophoretic mobility shift assays. Characteristic extract components were identified by LC-MS and verminoside was quantified by HPLC analysis.

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Allergen challenge of subjects with asthma produces an Imitrex Injection Cost early asthmatic response, late asthmatic response, and increases bronchial responsiveness. Histamine partly mediates the early asthmatic response, and may play a role in late-phase responses. Azelastine has antiallergic properties and has been proposed as a treatment for asthma. We therefore investigated the contribution of histamine to late-phase responses with the use of the potent H1-receptor antagonist azelastine.

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A reliable model of allergy has been created in the Brown Norway rat. In this model, allergen presentation to the middle ear causes functional disruption of the eustachian tube Zetia Generic Canada , predisposing to the development of otitis media with effusion. The purpose of this study was to study the effects of ototopical antihistamine on lipopolysaccharide (LPS)-induced otitis media in the allergic rat model.

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In this 2-week study in patients with moderate to severe SAR, azelastine nasal spray was well tolerated and produced significantly greater Zithromax Generic Name improvements in TNSS and total RQLQ score compared with cetirizine.