dr. Elly Nurus Sakinah

2010

Bronchodiator

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Bronchodilation

Bronchial tone

AcethycholineAcethycholine AdenosineAdenosine

Muscarinic Muscarinic antagonistsantagonists TheophyllineTheophylline

Bronchoconstriction

cAMP

AC

ATP

AMPPDE

+ +

+

_ _

ßAR ßAR agonistagonist

+

TheophyllineTheophylline_

Beta-2 Adrenergic Agonists – Short acting agents Rute Pemberian

Inhalasi/ parenteral cegah efek sistemik Bronkodilator paling efektif

Mekanisme kerjaMeningkatkan cAMP pada sel otot

polos bronkus menurunkan tonus otot bronkodilatasi

Merelaksasikan otot polos jln nafasmempertahankan fungsi mukosiliarMenurunkan permeabilitas vaskular

β Adrenergic Bronchodilators – Short-Acting (3-6 h) inhalasi Catecholamines

EpinephrineIsoproterenolIsoetharine

Resorcinol agentsMetaproterenol ( Alupent))

Saligenin agentsAlbuterol (ventolin)

Fenoterol (berotec) Terbutaline

Long Acting β Adrenergic Bronchodilators (>12 h) Salmeterol xinafoate (serevent) dan

Formoterol Higher lipophilicity and have a higher

affinity and selectivity Salmeterol long side chain to

ahydrophobic site bind to specific site within the β Adrenergic receptor (an exoreceptor near β receptor site)

Formoterol retained in the plasmalemma lipid bilayer of airway smooth muscle

Indication and clinical use Short acting RELIEVER exacerbation of

atshma, acute exacerbation of chronic obstructive bronchitisMild bronchoconstriction : 2 puffs MDI every 4-6

h bisa ditingkatkan sesuai kondisi seranganSevere attacks emergency care contnous

nebulizedOral prep nocturnal asmaTx COPD

Long acting bersama-sama dg antiinflamasi sebagai CONTROLLER asma

Side Effects Seen with Beta Agonist Tremor Papitations and tachycardia , aritmia Rise in blood pressure Nervousness Dizziness Nausea and vomiting Hypokalemia Rarely :Headache, Insomnia

Anticholinergic (Parasympatholytic) Bronchodilators Tertiary Ammonium Compounds

Atropine sulfateScopalamine

Quaternary Ammonium CompoundsIpratropiumTiotropium

Anticholinergic (Parasympatholytic) Bronchodilators Rute pemberian

Inhalasi (MDI, solution for nebulization, nasal spray)

Mekanisme kerjaBlock reseptor muskarinik M1 dan M3 Hambat

efek release asetilkolin (hambat bronkokonstriksi) menurunkan tonus otot polos jalan nafas.

Kurang potent jikan dibanding inhaled beta-2 agonists,

onset of action lambat (30-60 min after inhalation persists for up to 8 h).

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Bronchodilation

Bronchial tone

AcethycholineAcethycholine AdenosineAdenosine

Muscarinic Muscarinic antagonistsantagonists

TheophyllineTheophylline

Bronchoconstriction

cAMP

AC

ATP

AMPPDE

+ +

+

_ _

ßAR ßAR agonistagonist

+

TheophyllineTheophylline_

Anticholinergic (Parasympatholytic) Bronchodilators Role in therapy

Menambah efek short-acting beta-2 agonist pada kasus eksaserbasi asma○ Combivent®

Tx COPD Digunakan pada pasien yang tidak toleran dg efek

samping dari beta agonis seperti tachycardia, arrhythmias, and tremor.

Tx vasomotor rhinitis : Ipratoprium nasal spray Menurunkan sekresi kelenjar (decongestan)

Side effects Dryness of the mouth and bitter taste, blurred vision,

urinary retention

Theophylline

Nonselective phosphodiesterase inhibitor increasing cAMP realaksasi otot polos bronkus bronchodilator

Efektif pada konsentrasi serum 10-20 mg/dL

< 10 mgdL : low effect AND > 25 mg/dL : adverse effect NARROW THERAPY RANGE

Rapidly and completely absorbed Factors that affect Theophylline clearance

Menurunkan clearance○ Hambat enzim (cimetidine, eritromisin, ciprofloksasin)○ CHF○ Iiver dis’○ Pneumonia○ High carbohydrate diet○ Old age

Menaikkan clearance○ Enzim induction ( rifampicin, phenobarbital, ethanol)○ Smoking○ High protein, low KH○ Youth

Efek samping

Nausea and vomiting GIT disturbance Headache Restlesness GERD Diuresis Cardiac arrhytmia Epileptic seizures

GLUCOCORTICOID have anti-inflammatory action, so reduce

the responsiveness of airways. do not reverse bronchospasm thought to work mainly via inhibition of the

production of cytokines can be delivered either orally or inhaled --agents include:

beclomethasone (Beclovent, Vanceril)triamcinolone (Azmacort)fluticasone (Flovent)

Decongestant

α-adrenergic agonists vasoconstriction of nasal blood vessels,

reducing the volume of the nasal mucosa and opening up the airways.

Topical or systemic

Decongestants (cont). Ephedrine Epinephrine (adrenaline) Naphazoline Oxymetalozone (Afrin, Neo-Synephrine) Phenylephrine (Neo-Synephrine) Pseudoephedrine (Sudafed) Tetrahydrozolone Xylometazoline

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Antitussives Mechanism of action is either central

(suppressing cough center in the medulla oblongata) or peripheral (lessen irritation of the respiratory tract).

Therapeutic objective is to decrease the intensity and frequency of the cough.

Narcotic (opioid) and non-narcotic (non-opioid) agents are used.

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Opioid Antitussives

Codeine: most effective antitussive available Can suppress respirationsPotential for abuse

Hydrocodone: More potent than codeinePotential for abuse

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Non-Opioid Antitussives Dextromethorphan

Derivative of codeine, acts in CNS Diphenhydramine

Has sedation and anticholinergic properties Benzonatate (Tessalon)

Decreases sensitivity of respiratory tract stretch receptors

May have CNS effect

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Mucolytics/Expectorants Break up respiratory mucoprotein into

smaller strands. Facilitate coughing and the removal of

mucus from the respiratory tract.Acetylcysteine (Mucomyst) is used in cystic

fibrosis, atelectasis, acetaminophen overdose.

Guaifenesin (Robitussin - Mucinex) decreases cough frequency and reduces sputum thickness.

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