Therapeutic Management of Asthma
By: Pharma Tips |
Views: 3079 |
Date: 04-Jul-2011
BRONCHODILATORS DRUGSANTI LEUKOTRIENE DRUGSANTI INFLAMMATORY DRUGS
BRONCHODILATORS DRUGS:-
a) B2-adrenergic:
Examples:-
Salbutamol,Terbutaline,Ephedrine, Salmeterol,Formoterol,Bambuterol.
Mecanism of action:-
Dilate the bronchi by direct action on B2 adreno-receptors on smooth muscles. They relaxes bronchial muscles whatever spasmogen are involved. They also inhibit release of TNF- release from monocytes, and increase mucus clearance by an action on cilia.
Unwanted effects:-
The commonest adverse effect of these drugs include: tremors; other side effects are tachycardia, cardiac dysrhythmia.
b) Methylxanthines:
Examples:-
Theophylline, Aminophyline,Choline theophyllinate.
Mecanism of action:-
1>Release of Ca+2 from sarcoplasmic reticulum, especially in skeletal and cardiac muscles.
2>Inhibition of phosphodiesterase enz.which degrades cyclic neucleotide intracellulary, so dilation occur.
Unwanted effects:-
The serious CVS effect is dysrhythmia; other effects are CNS & GIT disturbances.
c)Anticholinergics:
Examples:-
Atropine, Ipratropium bromide[Atrovent]
Mecanism of action:-
It causes bronchodilation by blocking cholinergic tone through blockadge of cholinergic receptor; act primarly in larger airways.
Unwanted effects:-
Dry mouth ,urinary retention ,hyperthermia etc.
ANTI LEUKOTRIENE DRUGS:-
Examples:-
Montelukast, Zarfirlukast, Zileuton.(also inhibit LTB4 synthesis)
Mecanism of action:-
LT-C4 & LT-D4 are important mediators for bronchial asthma, these drugs competitively antagonize cys LT1 receptor mediated bronchoconstriction, increased vascular permeability & recruitment of eosinophils.
Unwanted effects:-
Headache, skin rashes. Sometimes few cases of Churg-Strauss syndrome(vasculitis with eosinophilia)
ANTI INFLAMMATORY DRUGS
Corticosteroids:
Examples:-
Beclomethasone[Vanceril,Beclovent],Triamcinolone[Azmacort],Flunisolide[Aerobid],Fluticasone [Flovent] Dexamethasone
Mecanism of action:-
Corticosteroids penetrates into cells, bind to high affinity Cytoplasmic Receptor Protein (CRP) a structural change occur in steroid receptor complex that allow migration into nucleus & binding to Glucocorticoid Response Elements(GRE)-thereby inhibit transcription of specific m-RNA, they are not bronchodilators.
Unwanted effects:-
Regular high dose can produces adrenal suppression in children .Other side effects are osteoporosis, susceptible to infection , palpitation of heart.
ANTI IgE DRUGS:-
Examples:-
Omalizumab.
Mecanism of action:-
Omalizumab is a recombinant humanized monoclonal antibody directed against IgE to inhibit the immune response to allergen exposure. This anti-IgE is directed against the binding site of IgE (Cepsilon3 domain) for the high-affinity receptor, and, as a result, prevents free-serum IgE from attaching to mast cells and other IgE receptor-expressing cells, preventing IgE-mediated responses.
Following allergen cross-linking of mast cell-bound IgE, these cells are activated and virtually immediately release a granule-associated substance, such as histamine. Within minutes, de novo synthesis of important lipid mediators (cysteinyl leukotrienes) is initiated from membrane phospholipids. Following a few hours, the activated mast cells are also capable of the transcription, translation, synthesis, and release of a large number of cytokines, including interleukin (IL)-4, IL-6, IL-9, IL-13, and tumor necrosis factor (TNF)-alpha.
Unwanted effects:-
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, tongue or throat); anxiety; cough; dizziness; fainting; fast or weak heartbeat; feeling unusually warm; flushing; hoarseness; new or worsening breathing problems, shortness of breath; numbness or tingling; symptoms of sinus or lung infection(congestion, cough, or fever); trouble swallowing; unusual lumps, growths, or moles; unusual swelling of the hands or feet; wheezing.
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