Pharmacology Flashcards
Name the 1st generation H1-blockers (antihistamines)
- Diphenhydramine
- Dimenhydrinate
- Chlorpheniramine
- Doxylamine
- AMine
- Hydrinate
What are the uses of 1st generation H1-blockers (antihistamines)?
- Allergy
- Motion sickness
- Vomitting in pregnancy
- Sleep aid
What are the adverse effects of 1st generation H1-blockers (antihistamines)?
- Sedation
- Antimuscarinic
- Anti-alpha adrenergic
NAme the 2nd generation H1-blockers (antihistamines)?
- Loratadine
- Fexofenadine
- Desloratadine
- Cetirizine
- Mostly end in “-adine”
Setirizine is Second gen
What is the clinical use of 2nd generation H1-blockers (antihistamines)?
Allergy
What is the advantage of 2nd generation H1-blockers (antihistamines)?
Far less sedating than 1st generation because of decreased entry into CNS
What is dextromethorphan used for clinically?
Antitussive - (cough medicine)
What are the adverse effects of dextromethorphan?
- Opioid effects (naloxone given in overdose)
- Serotonin syndrome if combined w. other serotonergic agents
What does dextromethorphan bind to?
Antagonises NMDA glutamate receptors
What is dextromethorphan a synthetic analog of?
Codeine
What is the mechanism of action of pseudoephedrine and phenylephrine?
Activates alpha-adrenergic receptors in nasal mucosa -> vasoconstriction
What is the clinical use of pseudoephedrine and phenylephrine?
- Reduce hyperemia
- Edema (used as nasal decongestant)
- Open obstructed eustachian tubes
What are the adverse effects of pseudoephedrine and phenylephrine?
- Hypertension
- Rebound congestion (rhinitis medicamentosa) if used for more than 4-6 days)
- Tachyphylaxis
- CNS stimulation and anxiety (pseudoephedrine)
What are examples of muscarinic agonists (used in asthma and COPD)?
- Tiotropium (long acting)
- Ipratropium
What is the MOA of muscarinic agonists (ipratropium and tiotropium)?
Competitively block muscarinic receptors preventing bronchoconstriction
What are examples of inhaled corticosteroids?
- Fluticasone
- Budesonide
What is the MOA of inhaled corticosteroids?
Inhibit the synthesis of virtually all cytokines
- Inactivate NF-kB, the transcription factor that induces production of TNF-alpha and other inflammatory agents
What is albuterol?
Short acting B2-agonist
What is Formoterol?
Long-acting B2-agonist
What are Montelukast and Zafirlukast and what receptor do they block?
Antileukotrienes
- Block leukotriene receptors (CysLTI)
What is Zileuton?
Antileukotriene
- 5-Lipoxygenase pathway inhibitor (blocks arachadonic acid -> leukotrienes)
What is the major adverse effect of Zileuton (5-Lipoxygenase pathway inhibitor)?
Hepatotoxic
What are Montelukast and Zafirlukast especially good for treating?
- Antileukotrienes, Block leukotriene receptors (CysLTI)
Aspirin-induced and exercise-induced asthma
What does Omalizumab bind to?
Binds mostly to unbound serum IgE and blocks binding to FcERI
What is an example of a Methylxanthine?
Theophylline
What is the MOA of Methylxanthines (e.g. Theophylline)?
Bronchodilation by inhibiting phosphodiesterase -> incr cAMP levels due to to decreased cAMP hydrolysis
What are Methylxanthines (e.g. Theophylline) metabolised by?
Cytochrome P-450
- Leads to narrow therapeutic index
What are the adverse effects of Methylxanthines (e.g. Theophylline)?
- Cardiotoxicity, neurotoxicity (narrow therapeutic index)
- Also blocks the action of adenosine
What is an example of a chromone (prevents mast cell degranulation - rarely used)?
Cromolyn
- Prevents acute asthma symptoms
What are examples of Anti-IL-5 monoclonal therapies?
- Mepolizumab, Reslizumab - IL-5
- Benralizumab - IL-5, receptor alpha
What is the MOA of Anti-IL-5 monoclonal antiB?
Prevents eosinophil differentiation, maturation, activation and survival mediated by IL-5 stimulation
What are Anti-IL-5 monoclonal therapies (Mepolizumab, Reslizumab, Benralizumab) used for?
Maintenance therapy in severe eosinophilic asthma
