Pulmonary Medications Part 2 PDF

Pulmonary Medications Part 2 Debra Forzese, Pharm. D. Methylxanthine Drugs Methylxanthine Agents Theophylline (Theo-24) Aminophylline Caffeine Methylxanthine Drugs š Indication – treatment of symptoms associated with chronic asthma or other chronic lung diseases such as emphysema, chronic b...

Pulmonary Medications Part 2 Debra Forzese, Pharm. D. Methylxanthine Drugs Methylxanthine Agents Theophylline (Theo-24) Aminophylline Caffeine Methylxanthine Drugs š Indication – treatment of symptoms associated with chronic asthma or other chronic lung diseases such as emphysema, chronic bronchitis qClinically used for bronchodilation and stimulatory effects š New GOLD criteria for treatment of COPD (2018) removed these drugs from treatment algorithm because of side effect risk outweighs benefits Methylxanthines - Theophylline š Mechanism of Action – multifactorial qInduces smooth muscle relaxation resulting in bronchodilation from inhibition of phosphodiesterase enzymes qSuppresses response of the airways to stimuli (histamine, adenosine, allergens) Methylxanthines - Theophylline š Narrow therapeutic range with a high incidence of adverse effects š Relatively weak bronchodilator Theophylline š Pharmacokinetics – children clear theophylline faster than adults š Metabolized by the liver š Drug levels need to be monitored - Toxic levels can produce seizures and arrhythmias, can be fatal Antimuscarinic Drugs Antimuscarinic Drugs – Short Acting Ipratropium (Atrovent) Ipratropium š Indications § Can be used as monotherapy or as combination with other bronchodilators, especially beta adrenergic § Used as bronchodilator for maintenance treatment of bronchospasm associated with COPD, including chronic bronchitis and emphysema o Off Label – moderate to severe asthma exacerbations Antimuscarinics – Short Acting š Ipratropium is an antimuscarinic bronchodilator § Derivative of atropine § Bronchodilation variable between patients § Poorly absorbed systemically after inhalation Ipratropium š Mechanism of action • Acetylcholine antagonist through muscarinic cholinergic receptors, causing decrease in production of cGMP leading to dilation of bronchial smooth muscle Ipratropium Formulations š Oral inhalation š Nebulizer solution – can be combined with albuterol in same nebulizer, within an hour Ipratropium Adverse Effects Serious Adverse Effects o Bronchitis o Hypersensitivity o Dry mouth o Paradoxical bronchospasm o Dyspnea o Closed angle glaucoma o Dizziness, headache o Tachycardia Ipratropium Warnings o Paradoxical bronchospasm – can be life threatening o CNS – dizziness, blurred vision o Hypersensitivity – angioedema, bronchospasm, urticaria, anaphylaxis o Can increase IOP – use with caution in closed angle glaucoma o Can cause urinary retention – use with caution in prostatic hyperplasia, bladder neck obstruction Ipratropium Pharmacokinetic/Pharmacodynamic Factors o Bronchodilation within 15 minutes and peak effect 1-2 hours o Duration – 2-4 hours MDI, 4-8 hours nebulizer solution o Half life 2 hours Ipratropium š Drug interactions qAnticholinergic agents – can increase anticholinergic effects (drowsiness, urinary retention, confusion, dry mouth, constipation) of anticholinergic agents qCannabinoid containing products – enhance tachycardia effects of cannabinoids qOpiods – increased constipation and urinary retention of opiods qThiazide diuretics – increased level of thiazide diuretics Ipratropium š Pregnancy – maternal use of inhaler not expected to result in fetal exposure, data suggests no risk of major birth defects š Lactation – breast milk drug levels expected to be low, according to manufacturer decision to breastfeed during therapy should consider risk of infant exposure, benefits of breast feeding, benefits of treatment to mother Ipratropium š Monitoring šPulmonary function tests šSigns/symptoms glaucoma šHypersensitivity reaction šUrinary retention Antimuscarinics for Asthma – Long Acting Tiotropium (Spiriva) Aclidinium (Tudorza Pressair) Glycopyrrolate ( Seebri Neohaler) Revefenacin (Yupelri) Antimuscarinic – Long Acting š Tiotropium Indications qAsthma moderate to severe in patients > 6 years old qMaintenance treatment of bronchospasm of COPD Antimuscarinic – Tiotropium Dosing • Adult – 1 capsule daily (used in HandiHaler device), NOT FOR ORAL USE • Pediatric • Renal impairment – no dose adjustment • Hepatic impairment – no dose adjustment • In patients with more symptoms can use in combination with long -acting beta agonist Tiotropium š Mechanism of action qSame as ipratropium Tiotropium š Pharmacokinetic/Pharmacodynamic Factors qMinimal hepatic metabolism qTime to peak - 5-7 minutes Tiotropium Adverse Effects šXerostomia (up to 16%) šPharyngitis (9-16%) šCV – angina, edema, palpitations šCNS – headache, dizziness, insomnia Tiotropium Warnings/Cautions o Paradoxical bronchospasm o CNS – dizziness, blurry vision o Hypersensitivity – angioedema, anaphylaxis o Capsule for inhalation may contain lactose o Not indicated as rescue inhaler for acute bronchospasm Tiotropium Drug Interactions – similar as ipratropium Pregnancy and breastfeeding – similar as ipratropium Monitoring – same as ipratropium Antimuscarinic Agent with Beta Agonist š Ipratropium/albuterol – Combivent inhaler