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Bronchodilators Notes

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BRONCHODILATO RS B2adrenoreceptor agonists (BAAs)

Clinical effects/use

Adverse effects

Mechanism of action

Examples

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Activate B2-adrenoreceptor o Increases intracellular cAMP o Activates K+ channel o Activates Na+/K+ ATPase o Reduces Ca2+ dependent coupling of actin and myosin Inhibits cholinergic neurotransmission o Activate muscarinic receptors= smooth muscle contraction

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Unclear Inhibition of cyclic nucleotide phosphodiesterases o Inhibit type IV PDE o Increasing cAMP/cGMP levels- SM relaxation Interaction with G proteins Antagonise adenosine receptors Stimulates CNS/ respiratory centres

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Cholinergic stimulation o Increases SM contraction/
secretion (M3 receptors)

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Xanthine drugs

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Bronchodilatation (most effective) o Increased density of receptors on smooth muscles of trachea to small bronchioles Other effects o Inhibit release of histamine and other inflammatory mediators o Reduce vascular permeability &
mucosal oedema In addition to steroids in patients non-responsive to BAAs In acute severe asthma

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Muscarinic receptor antagonists

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Cysteinyl

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Inhibits mucus secretion Ineffective against late phase asthma Used as adjunct to BAAs/steroids

Generally avoided as given via inhaler Tachycardia and palpitations Pulmonary vasodilatation

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Narrow therapeutic window o 30-100umol/L= Benefit o >120umol/L= Adverse o >200umol/L=
Significant adverse CNS effects o Insomnia, nervousness, seizures CVS effects o Palpitations, tachy, dysrythmia Minimal side effects

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Nausea, sleeplessness, flu,

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Act on 5-lipo-oxygenase pathway

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Short acting: SALBUTAMOL & TERBU o Max. effect in 30 mins o Duration= 3-5 hours o Used "as needed" Long acting: SALMETEROL &
FORMOTEROL o Duration= 8-12 hours o Twice daily o Adjunctive therapy in patients wi chronic asthma Non selective: ISOPRENALINE &
ADRENALINE o Severe asthma

Theophyline o Oral o Metabolises P450 enzymes in liv Drugs induce P450 enzymes red action and vice-versa Aminophyline o Slow IV followed by infusion

Ipratropium Bromide (Atrovent) o Administration: Aerosol intake, n absorbed, max. effect in 30 mins 5h Tiotropium o Longer acting, used in COPD Zileutin

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