Loading in 2 Seconds...
Loading in 2 Seconds...
BRONCHI A L AST H MA Ph arma c ol o g y a nd C linic al A spe c t s. DEFIN ITION AB.
Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author.While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server.
Asthma bronchiale is chronic inflammatory disease of airways connected with bronchial hyperreactivity andtotally or partiallyreversible obstruction of airways, which in the most casesdissapears spontaneously or with treatment.
1995, 2002, 2006
bronchoconstriction, mucus secretion, plasma exudation and bronchial hyperreactivity, airway remodelation
insufficient anti-inflammatory therapy => progressive destructive changes fixing of airway obstruction to emphysematous changes
Clasification of Asthma according to clinical symptoms and lung function:
CH O P D
A S T H M A
relieving = fastactingbronchodilators
C: OTHER ANTIASTHMATIC DRUGS
(long-acting betaagonists )LABA, (8-15h.)
the most effectiveantiinflammatory antiasthmatics
1.inhibition of cytokine transcription antiinflam. ef.
2.inhibition of mediators of inflam. release
3.decrease of airways reactivity
4.restriction of vasodilation antioedematic ef.
5.affect synthesis of eikosanoids
6.control activation of adhesive molecules
7.increase of susceptibilityresp. protection of 2 receptors against down-regulation at long-term treatment with 2 mimetics
1. ICS need to be administered at each new dg.AB
2. Treatment is essential to start early
3. We administerattack doses of ICS
4. Reduction of dose only after longer stabilisation
(6 months) – than minimal effective dose
5. If not sufficient ICS, we add as the drug of the first choice LABA, alternatives are leucotriene modifiers ( the first choice add-on therapy for children younger than 5 years), methylxanthines, slow release β2-agonists tablets
6. To adult patients are administered max. 200-800 mcg BDP/day and to children max. 400 mcg BDP/day, than you should start on with add-on therapy
*BDP = Beclomethasonedipropionate CFC
BDP 800 mcg/day
3. LABA ineffective →quit LABA, increase the dose of ICS to
BDP 800 mcg/day → ifstillinadequatecontrol→ add other anti-asthmatics (leucotrienemodifiers, methylxanthines)
(long-acting betaagonists )= LABA
(short-acting betaagonists )= SABA
speed of effect beginning
salbutamol rtd. cps.
duration of action
Anti M -cholinergic = PsL
activate sympathic NS
block parasympathic NS
duration of action>12 hours
MA:Bronchodilation through β2 => relaxation of smooth muscle
Modulate release of mediators from mastocytes a bazophils
Provide long-term safety against bronchoconstriction
Length of this bronchodilation effect at long-term regular administration decreases sign oftollerance for down regulation of β2 receptors => inhibition = concomitant administration of ICS
LABA in long-term therapy of asthma never can administer lonely, without ICS!
LABA: zlepšenie utilizácie KS a internalizácie GR do jadra (translokácia GR)
ICS: prevencia desenzitizácie a znižovania expresie β2 receptora
Relieversofthesecondchoice, at AE
competitiveantagonists on M1, M2 and M3receptorsofparasympathicus
Nicotinový receptor (+)
M1 receptor (+)
M2 receptor (–)
M3 receptor (+)
Barnes PJ. Eur Respir Rev 1996