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40 Cards in this Set

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  • Back

What histamine receptor can be blocked to treat respiratory problems?

H1 receptor blockers
What are the types of H1 blockers?
- 1st generation: Diphenhydramine, Dimenhydrinate, Chlorpheniramine
- 2nd generation: Loratadine, Fexofenadine, Desloratadine, Cetirizine
What kind of drug are Diphenhydramine, Dimenhydrinate, and Chlorpheniramine? Uses?
1st generation H1 blocker
- Used for allergies, motion sickness, and as a sleep aid
What kind of drug are Loratadine, Fexofenadine, Desloratadine, and Cetirizine? Uses?
2nd generation H1 blocker
- Used for allergies
What are the side effects of Diphenhydramine, Dimenhydrinate, and Chlorpheniramine?
- Sedation
- Anti-muscarinic
- Anti-α-adrenergic
What are the side effects of Loratadine, Fexofenadine, Desloratadine, and Cetirizine?
Far less sedating than the 1st generation because of ↓ entry into the CNS
What type of drug can thin respiratory secretions? Types?
Expectorants: Guaifenesin and N-acetylcysteine
What is the effect of Guaifenesin?
Expectorant - thins respiratory secretions, does not suppress cough reflex
What is the effect of N-acetylcysteine?
- Mucolytic - can loosen mucus plugs in CF patients

- Also used as an antidote for acetaminophen overdose
Which drug can be used to loosen mucus plugs in cystic fibrosis patients?
N-acetylcysteine
Which drug can be used as an antidote for acetaminophen overdose?
N-acetylcysteine
Which drug has anti-tussive action? Mechanism?
Dextromethorphan - antagonizes NMDA glutamate receptors
What is the mechanism of Dextromethorphan? Effect?
- Antitussive - antagonizes NMDA glutamate receptors
- Synthetic codeine analog
- Has mild opioid effect when used in excess (mild abuse potential)
What can you give for overdose of Dextromethorphan?
Naloxone
What drugs can be used as a nasal decongestant? Mechanism?
Pseudophedrine and Phenylephrine
- Sympathomimetic α-agonist
What are the clinical uses of Pseudophedrine and Phenylephrine?
- Reduces hyperemia (an excess of blood in the vessels supplying an organ or other part of the body)
- Reduces edema
- Reduces nasal congestion
- Opens obstructed eustachian tubes
What is an illicit use of Pseudophedrine?
Used to make methamphetamine
What are the toxic side effects of Pseudophedrine and Phenylephrine?
- Hypertension
- Can also cause CNS stimulation / anxiety (pseudophedrine)
What mediates bronchoconstriction in asthma?
- Inflammation
- Parasympathetic tone
What are the types of asthma drugs?
- β2-agonists
- Methylxanthines
- Muscarinic antagonists
- Corticosteroids
- Anti-leukotrienes
- Omalizumab
What are the types of β2-agonists used for asthma?
- Albuterol
- Salmeterol and Formoterol
What is the mechanism and effect of Albuterol?
- β2-agonist → relaxes bronchial smooth muscle
- Use during acute exacerbation of asthma
What is the mechanism and effect of Salmeterol?
- β2-agonist → relaxes bronchial smooth muscle
- Long-acting agents used for prophylaxis
- Adverse effects are tremor and arrhythmia
What is the mechanism and effect of Formoterol?
- β2-agonist → relaxes bronchial smooth muscle
- Long-acting agents used for prophylaxis
- Adverse effects are tremor and arrhythmia
What drug is a methylxanthine? Mechanism?
Theophylline
- Causes bronchodilation by inhibiting phosphodiesterase → ↑ cAMP levels due to ↓ cAMP hydrolysis
- Also blocks action of adenosine
What are the side effects of Theophylline?
- Usage is limited because of a narrow therapeutic index → cardiotoxicity, neurotoxicity
- Metabolized by cytochrome P-450
What asthma drug is a muscarinic antagonist? Mechanism?
Ipratropium
- Competitive block of muscarinic receptors, preventing bronchoconstriction
What are the uses of Ipratropium?
- Asthma
- COPD
What is the mechanism and use of Tiotropium?
- Long-acting muscarinic antagonist
- Used for COPD
What corticosteroids are used for asthma?
- Beclomethasone
- Fluticasone
What is the mechanism of Beclomethasone and Fluticasone?
Corticosteroids
- Inhibits the synthesis of virtually all cytokines
- Inactivates NF-κB, the transcription factor that induces the production of TNF-α and other inflammatory agents
What drug is the first line therapy for chronic asthma?
Corticosteroids: Beclomethasone and Fluticasone
What are the types of anti-leukotrienes used for asthma? Mechanism?
- Montelukast and Zafirlukast: blocks leukotriene receptors
- Zileuton: a 5-lipoxygenase pathway inhibitor
What is the mechanism of Montelukast and Zafirlukast? Uses?
- Blocks leukotriene receptors
- Especially good for aspirin-induced asthma
What is the mechanism of Zileuton?
- 5-lipoxygenase pathway inhibitor
- Blocks conversion of arachidonic acid to leukotrienes
What is the mechanism of Omalizumab?
Monoclonal anti-IgE antibody
- Binds mostly to unbound serum IgE and blocks binding to FcεRI
What are the uses of Omalizumab?
Used in allergic asthma resistant to inhaled steroids and long-acting β2-agonists
What is the mechanism of Methacholine? Use?
- Muscarinic receptor AGONIST
- Used in bronchial provocation challenge to help diagnose asthma
What drug can be used to treat pulmonary artery hypertension?
Bosentan
What is the mechanism of Bosentan? Use?
- Competitively antagonizes endothelin-1 receptors, which ↓ pulmonary vascular resistance
- Used to treat pulmonary arterial hypertension