AMINOPHYLLINE

 AMINOPHYLLINE

BRAND NAME:-AMINOPHYLLINE 100mg tab ,250mg /10ml inj .

AMINOPHYLLINE is water soluble & is a bronchodilator consisting of theophylline that is used for the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis.

PHARMACOLOGICAL ACTION:-

Aminophylline is the ethylenediamine salt of theophylline. Theophylline stimulates the CNS, skeletal muscles, and cardiac muscle. It relaxes certain smooth muscles in the bronchi, produces diuresis, and causes an increase in gastric secretion. 

MECHANISM OF ACTION:-

Aminophylline is the ethylenediamine salt of theophylline. After ingestion, theophylline is released from aminophylline, and theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin. 

USED:- 

Bronchial asthma and COPD,Apnoea in premature infants,

Use of intravenous aminophylline in status asthmaticus is outmoded.

But not i.m or s.c. highly irritation.

DOSE:- 250-500mg oral or slow i.v. injection; Children 7.5 mg/kg i.v. ; 

SIDE EFFECTS:- Narrow margin of safety . Dose -dependents Toxicity starts from the upper part of therapeutic concentration range., reversible g.i t. ,CNS and CVS , Headache,nausea,fall in BP, 

SYNCOPE AND EVEN SUDDEN DEATH — DUE TO FALL IN BP