USMLE (Fach) / Pharmacology - Respiratory (Lektion)

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  • Histamine-1 blockers Reversible inhibitors of H1 histamine receptors. First generation: Diphenhydramine, dimenhydrinate, chlorpheniramine ("-en/-ine" or "-en/-ate")- Clinical use: Allergy, motion sickness, sleep aid- Adverse ...
  • Guaifenesin Expectorant – thins respiratory secretions; does not suppress cough reflex.
  • N-acetylcysteine Mucolytic – liquifies mucus in chronic bronchopulmonary diseases (eg, COPD, CF) by disrupting disulfide bonds. Also used as an antidote for acetaminophen (paracetamol) overdose.
  • Dextromethorphan Antitussive (antagonizes NMDA glutamate receptors). - Synthetic codeine analog.- Has mild opioid effect when used in excess. - Mild abuse potential. - Nalaxone can be given for overdose. Adverse effects:- ...
  • Pseudoephedrine, phenylephrine α-adrenergic agonists, used as nasal decongestants. Clinical use: Reduce hyperemia, edema, nasal congestion; open obstructed eustachian tubes. Adverse effects: Hypertension. Rebound congestion if used ...
  • Pulmonary hypertension drugs Endothelin receptor antagonists (Bosentan): - Competitively antagonizes endothelin-1 receptors → ↓ pulmonary vascular resistance.- Heptatotoxic (monitor LFTs) PDE-5 inhibitors (Sidenafil):- Inhibits ...
  • β2-agonists Albuterol – relaxes bronchial smooth muscle (short acting β2-agonist). Used during acute exacerbation. Salmeterol, formoterol – long-acting agents for prophylaxis. Adverse effects are tremor and ...
  • Inhaled corticosteroids Fluticasone, budesonide – inhibit the synthesis of virtually all cytokines. Inactivate NF-κB, the transcription factor that induces production of TNF-α and other inflammatory agents.  1st-line therapy ...
  • Muscarinic antagonists Tiotropium, ipratropium – competitively block muscarinic receptors, preventing bronchoconstriction. - Also used for COPD. - Tiotropium is long acting.
  • Zileuton 5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotriens. Hepatotoxic.
  • Omalizumab Anti-IgE monoclonal therapy.Binds mostly unbound serum IgE and blocks binding to FcεRI. Used in allergic asthma with ↑ IgE levels resistant to inhaled steroids and long-acting β2-agonists.
  • Methylxanthines Theophylline – likely causes bronchodilation by inhibiting phosphodiesterase → ↑ cAMP levels due to ↓ cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity). ...
  • Methacholine Nonselective muscarinic receptor (M3) agonist. Used in bronchial challenge test to help diagnose asthma.
  • Diphenhydramine First generation histamine-1 blocker
  • Dimenhydrinate First generation histamine-1 blocker
  • Loratadine Second generation histamine-1 blocker
  • Montelukast, zafirlukast Block leukotriene receptors (CysLT1). Especially good for aspirin-induced and exercise-induced asthma.
  • Fexofenadine Second generation histamine-1 blocker
  • Desloratadine Second generation histamine-1 blocker
  • Cetirizine Second generation histamine-1 blocker
  • Mast cell stabilizers Cromolyn, nedocromil – prevent release of inflammatory mediators from mast cells. Used for prevention of bronchospasm, not for acute bronchodilation.
  • Chlorpheniramine First generation histamine-1 blocker
  • Nedocromil Mast cell stabilizer
  • Cromolyn Mast cell stabilizer
  • Promethazine Histamine-1 blocker
  • Hydroxyzine Histamine-1 blocker