Drug spotlight- Zafirlukast

New Drug Approvals

Zafirlukast.svg

ZAFIRLIKAST 

cyclopentyl 3-{2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl}-1-methyl-1H-indol-5-ylcarbamate107753-78-6

Matassa, V.G. et al, J. Med. Chem., v. 33, 1781 (1990);

U. S. Patent No. 4,859,692;

U. S. Patent No. 5,993,859;

http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020547s031lbl.pdf

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), taken once daily. Zileuton (Zyflo), also used in the treatment of asthma via its inhibition of 5-lipoxygenase, is taken four times per day.

Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs andinflammation of the breathing passages.

Zafirlukast is marketed by Astra Zeneca with the brand names AccolateAccoleit, and Vanticon. It was the…

View original post 2,001 more words

Advertisements

Drug spotlight- Zafirlukast

New Drug Approvals

Zafirlukast.svg

ZAFIRLIKAST 

cyclopentyl 3-{2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl}-1-methyl-1H-indol-5-ylcarbamate107753-78-6

Matassa, V.G. et al, J. Med. Chem., v. 33, 1781 (1990);

U. S. Patent No. 4,859,692;

U. S. Patent No. 5,993,859;

http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020547s031lbl.pdf

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), taken once daily. Zileuton (Zyflo), also used in the treatment of asthma via its inhibition of 5-lipoxygenase, is taken four times per day.

Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs andinflammation of the breathing passages.

Zafirlukast is marketed by Astra Zeneca with the brand names AccolateAccoleit, and Vanticon. It was the…

View original post 2,001 more words

DRUG SPOTLIGHT …… DOXOFYLLINE

New Drug Approvals

DOXOFYLLINE

LAUNCHED 1987, Istituto Biologico Chemioterapico ABC

69975-86-6  CAS NO

7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethylpurine-2,6-dione

1H-Purine-2,6-dione, 3,7-dihydro-7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl- (9CI)

7-(1,3-Dioxolan-2-ylmethyl)-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione; 7-[1,3-(Dioxolan-d4)-2-ylmethyl)]theophylline; 2-(7�-Theophyllinemethyl)-1,3- dioxolane; ABC 12/3; ABC 1213; Ansimar; Dioxyfilline; Doxophylline; Maxivent; Ventax;

Synonyms

  • 2-(7′-Teofillinmetil)-1,3-diossolano
  • 2-(7′-Teofillinmetil)-1,3-diossolano [Italian]
  • 2-(7′-Theophyllinemethyl)-1,3-dioxolane
  • 5-26-14-00120 (Beilstein Handbook Reference)
  • 7-(1,3-Dioxolan-2-ylmethyl)theophylline
Formula C11H14N4O4 
Mol. mass 266.25 g/mol
  • ABC 12/3
  • Ansimar
  • BRN 0561195
  • Dioxyfilline
  • Doxofilina
  • Doxofilina [INN-Spanish]
  • Doxofylline
  • Doxofyllinum
  • Doxofyllinum [INN-Latin]
  • Doxophylline
  • EINECS 274-239-6
  • Maxivent
  • UNII-MPM23GMO7Z
  • Ventax

Doxofylline (INN), (also known as doxophylline) is a xanthine derivative drug used in the treatment of asthma.[1]

Doxofylline is a xanthine molecule that appears to be both bronchodilator and anti-inflammatory with an improved therapeutic window over conventional xanthines such as Theophylline and the evidence supporting the effects of Doxofylline in the treatment of lung diseases

It has antitussive and bronchodilator[2] effects, and acts as aphosphodiesterase inhibitor.[3]

In animal and human studies, it…

View original post 2,080 more words