Astelin

Astelin is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis.

Astelin - Pharmacology:

Antihistamines such as azelastine appear to compete with histamine for histamine H1- receptor sites on effector cells (mast cells). The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.

Astelin mini report

Astelin NDA
NDA - A product marketed under an approved New Drug Application
Astelin SPRAY, METERED
SPRAY, METERED
Astelin HUMAN PRESCRIPTION DRUG
HUMAN PRESCRIPTION DRUG
Astelin global name
azelastine hydrochloride
Astelin global name
Azelastine Hydrochloride
Start - Stop data
START DATA:
1996-Nov-15
Start - Stop data
STOP DATA
2016-Nov-30

Astelin for patients

To prevent contaminating the dropper tip and solution, care should be taken not to touch any surface, the eyelids or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use. This product is sterile when packaged.

Patients should be advised not to wear a contact lens if their eye is red. OPTIVAR™ should not be used to treat contact lens related irritation. The preservative in OPTIVAR™, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red, should be instructed to wait at least ten minutes after instilling OPTIVAR™ before they insert their contact lenses.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

Astelin hydrochloride administered orally for 24 months was not carcinogenic in rats and mice at doses up to 30 mg/kg/day and 25 mg/kg/day, respectively. Based on a 30 µl drop size, these doses were approximately 25,000 and 21,000 times higher than the maximum recommended ocular human use level of 0.001 mg/kg/day for a 50 kg adult.

Astelin hydrochloride showed no genotoxic effects in the Ames test, DNA repair test, mouse lymphoma forward mutation assay, mouse micronucleus test, or chromosomal aberration test in rat bone marrow. Reproduction and fertility studies in rats showed no effects on male or female fertility at oral doses of up to 25,000 times the maximum recommended ocular human use level. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level), the duration of the estrous cycle was prolonged and copulatory activity and the number of pregnancies were decreased. The numbers of corpora lutea and implantations were decreased; however, the implantation ratio was not affected.

Pregnancy:

Teratogenic Effects: Pregnancy Category C. Astelin hydrochloride has been shown to be embryotoxic, fetotoxic, and teratogenic (external and skeletal abnormalities) in mice at an oral dose of 68.6 mg/kg/day (57,000 times the recommended ocular human use level). At an oral dose of 30 mg/kg/day (25,000 times the recommended ocular human use level), delayed ossification (undeveloped metacarpus), and the incidence of 14th rib were increased in rats. At 68.6 mg/kg/day (57,000 times the maximum recommended ocular human use level) azelastine hydrochloride caused resorption and fetotoxic effects in rats. The relevance to humans of these skeletal findings noted at only high drug exposure levels is unknown.

There are no adequate and well-controlled studies in pregnant women. OPTIVAR™ should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers:

It is not known whether azelastine hydrochloride is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when OPTIVAR™ is administered to a nursing woman.

Pediatric Use:

Safety and effectiveness in pediatric patients below the age of 3 have not been established.

Geriatric Use:

No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.

Astelin Interactions

Data is temporarily not available

Astelin Contraindications

OPTIVAR™ is contraindicated in persons with known or suspected hypersensitivity to any of its components.

Astelin tags categories:

Generic name, Overdose, Half Life Astelin, Food Interactions, Chemical, etc..

Astelin see also FDA report Stinging Nettle

Brand Names containing Azelastine
Allergy