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AZENAP

Quick Overview

The pedigree of SAVA Medica Ltd stands tall as our Nasal spray and Dry powder inhaler technology and expertise.


Our aim is to reach out to the globe within shortest possible time frame


To promote this objective, not only we distribute and market our respiratory range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as Azenap which contains  Azelastine Hydrochloride B.P... 0.1%w/v.


This Azenap contains same active ingredient as Astelin® Nasal Spray from MEDA Pharmacuticals 


 

AZENAP

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Details

Each spray delivers:

Azelastine Hydrochloride BP….. 140mcg

Composition:

Azelastine Hydrochloride BP  0.1%w/v

Excipients      q.s.

Pharmacology:

Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. AZENAP NASAL SPRAY is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity.

Indications:

AZENAP NASAL SPRAY is indicated for the treatment of the symptoms of seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus in adults and children 5 years and older, and for the treatment of the symptoms of vasomotor rhinitis, such as rhinorrhea, nasal congestion and postnasal drip in adults and children 12 years and older.

Dosage and Administration:

Seasonal Allergic Rhinitis

The recommended dose of AZENAP NASAL SPRAY in adults and children 12 years and older with seasonal allergic rhinitis is one or two sprays per nostril twice daily. The recommended dose of AZENAP NASAL SPRAY in children 5 years to 11 years of age is one spray per nostril twice daily.

Vasomotor Rhinitis

The recommended dose of AZENAP NASAL SPRAY in adults and children 12 years and older with vasomotor rhinitis is two sprays per nostril twice daily.

Before initial use, the delivery system should be primed with 4 sprays or until a fine mist appears. When 3 or more days have elapsed since the last use, the pump should be reprimed with 2 sprays or until a fine mist appears.

CAUTION: Avoid spraying in the eyes.

Directions for Use: Illustrated patient instructions for proper use accompany each package of AZENAP NASAL SPRAY.

Side Effects:

Cardiovascular: flushing, hypertension, tachycardia.

Dermatological: contact dermatitis, eczema, hair and follicle infection, furunculosis, skin Iaceration.

Digestive: constipation, gastroenteritis, glossitis, ulcerative stomatitis, vomiting, increased SGPT, aphthous stomatitis, diarrhea, toothache.

Metabolic and Nutritional: increased appetite.

Musculoskeletal: myalgia, temporo-mandibular dislocation, rheumatoid arthritis.

Neurological: hyperkinesia, hypo-esthesia, vertigo.

Psychological: anxiety, depersona-lization, depression, nervousness, sleep disorder, thinking abnormal.

Respiratory: bronchospasm, coughing, throat burning, Iaryngitis, bronchitis, dry throat, nocturnal dyspnea, naso-pharyngitis, nasal congestion, pharyngolaryngeal pain, sinusitis, nasal dryness, paranasal sinus hyper-secretion, post nasal drip.

Special Senses: conjunctivitis, eye abnormality, eye pain, watery eyes, taste loss.

Urogenital: albuminuria, amenorrhea, breast pain, hematuria, increased urinary frequency.

Whole Body: allergic reaction, back pain, herpes simplex, viral infection, malaise, pain in extremities, abdominal pain, pyrexia

Drug Interaction:

Concurrent use of AZENAP NASAL SPRAY with alcohol or other CNS depressants should be avoided because additional reductions in alertness

and additional impairment of CNS performance may occur.

Cimetidine (400 mg twice daily) increased the mean Cmax and AUC of orally administered azelastine hydro-chloride (4 mg twice daily) by approximately 65%. Ranitidine hydro-chloride (150 mg twice daily) had no effect on azelastine pharmacokinetics.

Interaction studies investigating the cardiac effects, as measured by the corrected QT interval (Qtc), of con-comitantly administered oral azelastine hydrochloride and erythromycin or ketoconazole were conducted. Oral erythromycin (500 mg three times daily for seven days) had no effect on azelastine pharmacokinetics or Qtc based on analyses of serial electro-cardiograms. Ketoconazole ( 200 mg twice daily for seven days ) interfered with the measurement of azelastine plasma concentrations; however, no effects on QTc were observed.

No significant pharmacokinetic inter-action was observed with the co administration of an oral 4 mg dose of azelastine hydrochloride twice daily and theophylline 300 mg or 400 mg twice daily.

Warnings:

No information provided.

Precautions:

Activities Requiring Mental Alertness: In clinical trials, the occurrence of somnolence has been reported in some patients taking AZENAP NASAL SPRAY; due caution should therefore be exercised when driving a car or operating potentially dangerous machinery while using AZENAP NASAL SPRAY. Concurrent use of AZENAP NASAL SPRAY with alcohol or other CNS depressants should be avoided because additional reductions in alertness and additional impairment of CNS performance may occur.

Contraindications:

AZENAP NASAL SPRAY is contra-indicated in patients with a known hypersensitivity to azelastine hydro-chloride or any of its components.

Pharmacokinetics:

After intranasal administration, the systemic bioavailability of azelastine hydrochloride is approximately 40%. Maximum plasma concentrations (Cmax) are achieved in 2-3 hours. Based on intravenous and oral administration, the elimination half-life, steady- state volume of distribution, and plasma clearance are 22 hours, 14.5 L/kg, and 0.5 L/h/kg, respectively. Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine is oxidatively metabolized to the principal active metabolite, desmethylazelastine, by the cytochrome P450 enzyme system. The specific P450 isoforms responsible for the biotransformation of azelastine have not been identified; however, clinical interaction studies

with the known CYP3A4 inhibitor erythromycin failed to demonstrate a pharmacokinetic interaction. In a multipledose, steady state drug interaction study in normal volunteers, cimetidine (400 mg twice daily), a nonspecific P450 inhibitor, raised orally administered mean azelastine (4mg twice daily) concentrations by approximately 65%.

The major active metabolite, desmethyl-azelastine, was not measurable (below assay limits) after single-dose intranasal administration of azelastine hydrochloride. After intranasal dosing of azelastine hydrochloride to steady-state, plasma concentrations of desmethyl-azelastine range from 20-50% of azelastine concentrations. When azelastine hydrochloride is administered orally, desmethylazelastine has an elimination half-life of 54 hours. Limited data indicate that the metabolite profile is similar when azelastine hydrochloride is administered via the intranasal or oral route.

In vitro studies with human plasma indicate that the plasma protein binding of azelastine and desmethylazelastine are approximately 88% and 97%, respectively.

Azelastine hydrochloride administered intranasally at doses above two sprays per nostril twice daily for 29 days resulted in greater than proportional increases in Cmax and area underthe curve (AUC) for azelastine.

Studies in healthy subjects administered oral doses of azelastine hydrochloride demonstrated linear responses in Cmax and AUC.

Special Populations

Following oral administration, pharma-cokinetic parameters were not influenced by age, gender, or hepatic-impairment.

Based on oral, single-dose studies, renal insufficiency (creatinine clearance < 50 mL/min) resulted in a 70-75% higher Cmax and AUC compared to normal subjects. Time to maximum concentration was unchanged.

Oral azelastine has been safely administered to over 1400 asthmatic subjects, supporting the safety of administering AZENAP NASAL SPRAY to allergic rhinitis patients with asthma.

Storage: Store at a temperature not exceeding 30OC.

Protect from light. Do not freeze.

Keep out of reach of children.

Packaging:

10 ml in glass vial.

 
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