Short Acting Beta2-Agonists Role in therapy - medications of choice for relief of bronchospasm during acute exacerbations of asthma and

for the pretreatment of exercise-induced bronchoconstriction Sample Drugs Generic Name Brand name Albuterol/Salbutamol Proventil, Ventolin, Resdil, Asmalin Tab Terbutaline Pulmoxcel, Pulmonyl, Terbulin Levalbuterol Xopenex Fenoterol Berotec Inhalation Aerosol Metaproterenol Alupent Pirbuterol Maxair Albuterol, Terbutaline, Metaproterenol, and Pirbuterol Are available as metered-dose inhalers. 2.5-mg nebulizer or 100-400 mcg aerosol inhaler Cause bronchodilation which is maximal within 15-30 minutes and persists for 3-4 hours. All can be diluted in saline for administration from a hand-held nebulizer but will require much higher doses. Nebulized therapy should be reserved for patients unable to coordinate inhalation from a metered-dose inhaler. Albuterol and Terbutaline Are also available in tablet form. Usual regimen: 1 tablet 2 or 3 times daily the principal adverse effects (skeletal muscle tremor, nervousness, and occasional weakness) may be reduced by starting the patient on halfstrength tablets for the first 2 weeks of therapy Terbutaline: available in SQ injection (0.25mg) indicated for emergency treatment of severe asthma when aerosol therapy is unavailable *** Inhaled route has faster onset and is more effective than tablets or syrup Dosage schedule: Asthma Attack: Begin for 2-4 puffs every 20 minutes for the first hour: 2-4 puffs every 3 to 4 hours

DRUGS GROUP
Short Acting 1. Beta2Agonists 2. 3. 4. 5. 6.

EFFICACY PHARMACODYNAMICS
It stimulates b2 adrenergic receptors binding to b2 receptors in the lungs which results in relaxation of bronchial smooth muscles. Inhibit histamine release by mast cells.

SAFETY SIDE-EFFECTS
Body as A Whole: hypersensitivity reaction CNS: tremor, anxiety, nervousness, restlessness, convulsions, weakness, headache CV: palpitations, hypertension, hypotension, bradycardia, reflex tachycardia Special Senses: blurred vision , dilated pupils GI: nausea, vomiting Other: muscle cramps, hoarseness, mouth and throat irritation At very high dose: Hyperglycemia, hypokalemia

SUITABILITY CONTRAINDICATIONS
Patients with a history of hypersensitivity to any of the components of drug tablet, inhaler, nebules and rotacaps. Threatened st abortion during 1 nd or 2 trimester of pregnancy, toxemia of pregnancy, antepartum hemorrhage, and placenta previa

COST

SAMPLE
Albuterol/ Salbutamol Terbutaline Fenoterol Metaproterenol Pirbuterol Levalbuterol

PHARMACOKINETICS
Well absorbed after oral administration but rapidly undergoes extensive metabolism Extensively metabolized by the liver and other tissues may cross the placenta Majority (76%) of dose given in IV, orally or by inhalation are eliminated in 3d (72hrs) Primarily excreted in the urine feces are minor route excretion Half life oral 2.75hr; inhalation 3-8 hr

DRUG-DRUG INTERACTION
Salbutamol Inhaler (P280) Salbutamol Nebule 2.5mg (P9.25) Salbutamol Syrup 2mg 60ml (P26) Salbutamol Tab 2mg (P0.75) Salbutamol Tab 4mg (P1.25) Terbutaline tab 2.5mg (P1.25) Terbutaline Syrup 60ml (P33)