Zafirlukast

Zafirlukast Brand names, Zafirlukast Analogs

Zafirlukast Brand Names Mixture

No information avaliable

Zafirlukast Chemical_Formula

C₃₁H₃₃N₃O₆S

Zafirlukast RX_link

http://www.rxlist.com/cgi/generic/zafirlukast.htm

Zafirlukast fda sheet

Zafirlukast FDA

Zafirlukast msds (material safety sheet)

Zafirlukast MSDS

Zafirlukast Synthesis Reference

F. J. Brown et al., Eur. pat. Appl. 199,543; P. R. Bernstein et al., U.S. pat. 4,859,692 (1986, 1989 both to ICI)

Zafirlukast Molecular Weight

575.676 g/mol

Zafirlukast Melting Point

139 ^oC

Zafirlukast H₂O Solubility

No information avaliable

Zafirlukast State

Solid

Zafirlukast LogP

5.787

Zafirlukast Dosage Forms

Tablet

Zafirlukast Indication

For the prophylaxis and chronic treatment of asthma.

Zafirlukast Pharmacology

Zafirlukast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA) indicated for the prophylaxis and chronic treatment of asthma. Patients with asthma were found in one study to be 25-100 times more sensitive to the bronchoconstricting activity of inhaled LTD₄ than nonasthmatic subjects. In vitro studies demonstrated that zafirlukast antagonized the contractile activity of three leukotrienes (LTC₄, LTD₄ and LTE₄) in conducting airway smooth muscle from laboratory animals and humans. Zafirlukast prevented intradermal LTD₄-induced increases in cutaneous vascular permeability and inhibited inhaled LTD₄-induced influx of eosinophils into animal lungs.

Zafirlukast Absorption

Rapidly absorbed following oral administration, reduced following a high-fat or high-protein meal.

Zafirlukast side effects and Toxicity

Side effects include rash and upset stomach.

Zafirlukast Patient Information

Patients should be told that a rare side effect of ACCOLATE is hepatic dysfunction, and to contact their physician immediately if they experience symptoms of hepatic dysfunction (eg. right upper quadrant abdominal pain, nausea, fatigue, lethargy, pruritus, jaundice, flu-like symptoms, and anorexia). Liver failure resulting in liver transplantation and death has occurred in patients taking zafirlukast .

ACCOLATE is indicated for the chronic treatment of asthma and should be taken regularly as prescribed, even during symptom-free periods. ACCOLATE is not a bronchodilator and should not be used to treat acute episodes of asthma. Patients receiving ACCOLATE should be instructed not to decrease the dose or stop taking any other antiasthma medications unless instructed by a physician. Women who are breast-feeding should be instructed not to take ACCOLATE. Alternative antiasthma medication should be considered in such patients.

The bioavailability of ACCOLATE may be decreased when taken with food. Patients should be instructed to take ACCOLATE at least 1 hour before or 2 hours after meals.

Eosinophilic Conditions: In rare cases, patients on ACCOLATE therapy may present with systemic eosinophilia, eosinophilic pneumonia, or clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic steroid therapy. These events usually, but not always, have been associated with the reduction of oral steroid therapy. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. A causal association between ACCOLATE and these underlying conditions has not been established .

Zafirlukast Organisms Affected

Humans and other mammals