SITI RAHMATUL AINI, S.F., APT., M.

SC
FAKULTAS KEDOKTERAN
UNIVERSITAS MATARAM
2012

Selective for b
2
-receptor subtype.
Mekanisme :direct relaxation of airway
smooth muscle and consequent
bronchodilation
Directly to airways via inhalation.
Classified as short- or long-acting.
Short-acting : symptomatic relief of asthma,
long-acting : prophylactically in treatment of
asthma

Short-Acting b
2
Adrenergic
Receptor Agonists
Example : albuterol (PROVENTIL, VENTOLIN), levalbuterol
(XOPENEX), metaproterenol (ALUPENT), terbutaline
(BRETHAIRE), and pirbuterol (MAXAIR)
Terbutaline (BRETHINE, BRICANYL), albuterol, and
metaproterenol also available in oral dosage form
Secara inhalasi :onset of action within 1 to 5 minutes and
produces bronchodilation that lasts for about 2 to 6 hours.
Secara oral : oral terbutaline duration of action of 4 to 8
hours




Salmeterol xinafoate (SEREVENT) and formoterol
(FORADIL)
Inhalation of salmeterol provides persistent
bronchodilation lasting over 12 hours

Toxicity
increased heart rate
cardiac arrhythmias

Two primary situation
- in young children (<5 years old) who cannot
manipulate metered-dose inhalers.
-patients with severe asthma exacerbations, any
aerosol, whether delivered via a metered-dose inhaler
or a nebulizer, can worsen cough owing to local
irritation


Mechanism :
not directly relax airway smooth muscle and thus
have little effect on acute bronchoconstriction
effective in inhibiting airway inflammation by
-modulation of cytokine and chemokine
production;
- inhibition of eicosanoid synthesis;
- marked inhibition of accumulation of basophils,
eosinophils, and other leukocytes in lung tissue;
-decreased vascular permeability


Inhaled Glucocorticoids
beclomethasone dipropionate (BECLOVENT,
VANCERIL), triamcinolone acetonide
(AZMACORT), flunisolide (AEROBID),
budesonide (PULMICORT), and fluticasone
propionate (FLOVENT).
used prophylactically to control asthma
Toxicity
decreases in bone mineral density
Oropharyngeal candidiasis

Systemic Glucocorticoids
- used for acute asthma exacerbations and
chronic severe asthma.
Toxicity
-mood disturbances, increased appetite,
impaired glucose control in diabetics, and
candidiasis



Leukotriene-Receptor Antagonists :
Zafirlukast (ACCOLATE) and montelukast
(SINGULAIR)
Zafirlukast and montelukast : selective high-affinity
competitive antagonists for cys-LT1 receptor
Leukotriene-Synthesis Inhibitors : Zileuton
(ZYFLO)
Zileuton :inhibitor of 5-lipoxygenase activity
inhibits formation of all 5-lipoxygenase products


prophylactic treatment for mild asthma
as alternatives to low-dose inhaled steroids
for control of mild chronic asthma.
Interaction with warfarin and theophylline ???

Omalizumab (XOLAIR)
first "biological drug" approved for asthma
Omalizumab is recombinant humanized
monoclonal antibody targeted against IgE. IgE
bound to omalizumab cannot bind to IgE
receptors on mast cells and
basophilspreventing allergic reaction at a
very early step .
indicated for adults and adolescents older
than 12 years of age with allergies and
moderate-to-severe persistent asthma.
should not be used as a rescue medication
Mechanism of Action
inhibiting mediator release from bronchial mast
cells
reversing increased functional activation in
leukocytes obtained from the blood of asthmatic
patients
suppressing the activating effects of chemotactic
peptides on human neutrophils, eosinophils, and
monocytes
inhibiting parasympathetic and cough


to prevent asthmatic attacks in individuals
with mild to moderate bronchial asthma
Nedocromil : approved for asthmatic patients
12 years of age and older
Cromolyn : approved for all ages.



Toxicity
- cough, joint swelling and pain, headache,
rash, and nausea.
-Nedocromil and cromolyn can cause a bad
taste.

Theophylline
competitive antagonist at adenosine receptors
inhibits synthesis and secretion of inflammatory
mediators from numerous cell types, including mast
cells and basophils
Indeks terapi sempit

Ipratropium bromide (ATROVENT)
Menghambat kontraksi otot polos saluran
nafas yg diatur oleh vagus dan sekresi mukus
Combination of selective b
2
adrenergic
agonist and ipratropium should be
considered in acute treatment of severe
asthma exacerbations