Respiratory Pharmacology Flashcards by Clare Burke

When can long acting beta 2 agonists be used alone?

COPD

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What is the mechanism of H1 blockers?

Reversible inhibitors of H1 histamine receptors

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What are three examples of 1st generation H1 blockers?

Diphenhydramine
Dimenhydrinate
Chlorpheniramine

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What are the clinical uses for 1st generation H1 blockers?

Allergy, motion sickness, sleep aid

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What are toxicities associated with 1st generation H1 blockers?

Sedation, anti-muscarinic, anti-alpha-adrenergic

urinary retention, dry mouth, blurry vision, delirium

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What are four examples of 2nd generation H1 blockers?

Loratadine
Fexofenadine
Desloratadine
Cetirizine

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What are the clinical uses for 2nd generation H1 blockers?

Allergies

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What is the major difference between between 1st and 2nd generation H1 blockers?

2nd generation H1 blockers cause far less sedation because of decreased entry into CNS

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What is the mechanism of action of Guaifenesin?

Expectorant that thins mucus secretions

Think “fenesin” sounds like fenestrate like it is poking holes in the mucus to break it up

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Does Guaifenesin suppress the cough reflex?

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What is the mechanism of action of N-acetylcysteine?

Mucolytic that can loosen mucous plugs in CF patients by disrupting disulfide bonds

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Besides its mucolytic properties, what else is N-acetylcysteine effective in treating?

acetaminophen overdose

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What is the mechanism of action of Dextromethorphan?

Antitussive, which antagonizes the NMDA glutamate receptors. It’s a synthetic codeine analog.

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What do you use to treat a Dextromethorphan overdose?

Naloxone

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What are the side effects of Dextromethorphan?

Has mild opioid effect when used in excess, so has mild abuse potential

May cause serotonin syndrome if combined with other serotonergic agents

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What is the mechanism of action for Pseudoephedrine and Phenylephrine?

alpha-adrenergic agonists, used as nasal decongestants (act as vasoconstrictors of nasal arteries)

What are the clinical uses for Pseudoephedrine and Phenylephrine?

Reduce hyperemia, edema, nasal congestion; open obstructed eustachian tubes

Pseudoephedrine is also illicitly used to make methamphetamine

What are the toxicities associated with Pseudoephedrine and Phenylephrine?

Hypertension

Can also cause CNS Stimulation/anxiety (pseudoephedrine)

What are the three classes of drugs used to treat pulmonary hypertension?

Endothelian Receptor Antagonists
PDE-5 inhibitors
Prostacyclin Analogs

What is an example and what is the mechanism of an endothelial receptor antagonist?

Bosentan (primary drug used to treat pulmonary hypertension)

Competitively antagonize endothelin-1 receptors (decreased pulmonary vascular resistance)

What toxicity is associated with endothelial receptor antagonists?

Hepatotoxic (monitor LFTs)

What is an example and what is the mechanism of an PDE-5 inhibitors?

Sildenafil

Inhibit cGMP PDE5 and prolong vasodilatory effect of nitric oxide

(also used to treat erectile dysfunction)

What are two examples of and what is the mechanism of prostacyclin analogs?

Epoprostenol and Iloprost

Prostacyclins (PGI2) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds. Inhibit platelet aggregation

What are the side effects associated with prostacyclin analogs?

flushing, jaw pain

What are the two ways in which bronchoconstriction in asthma is mediated?

1. inflammatory processes 2. parasympathetic tone (asthma therapy is directed at these two pathways)

What type of drug is used during an acute exacerbation of asthma?

Beta 2 agonists (relax bronchial smooth muscle) Example: Albuterol

What type of drug is used for prophylaxis of asthma?

Long acting Beta 2 agonists Ex. Salmeterol, formoterol

What are the side effects associated with long acting Beta 2 agonists?

Tremor and arrhythmias

What are two examples of corticosteroids that act as front line therapy for chronic asthma and what is the mechanism of action?

Fluticasone, Budesonide Inhibit the synthesis of virtually all cytokines. Inactivate NF-kB, the transcription factor that induces the production of TNF-alpha and other inflammatory agents.

What is an example of a short-acting and a long-acting muscarinic antagonist and what is their mechanism of action?

Short-acting: Ipratropium Long-acting: Tiotropium Competitively blocks muscarinic receptors, preventing bronchoconstriction (also used to treat COPD)

Which antileukotriene drugs block leukotriene receptors (CYsLT1) and are especially good for treating aspirin-induced asthma?

Montelukast, zarfirlukast

What antileukotriene drug is a 5-lipoxygenase pathway inhibitor and what is its main side effect?

Zileuton (blocks the conversion of arachidonic acid to leukotriences) Hepatoxic

What kind of drug is Omalizumab, what is its mechanism of action, and when is it used?

Monoclonal anti-IgE antibody; binds mostly unbound serum IgE and blocks binding to FcERI (on mast cells and basal cells) Used in allergic asthma that is resistant to inhaled steroids and long acting beta 2 agonists

Do increased or decreased levels of cAMP lead to bronchodilation?

Increased (both beta 2 agonists which increase AC and theophyline which inhibits the breakdown of cAMP, increase the levels of cAMP in cells thus increasing bronchodilation)

What is the main example of methylxanthines used to treat asthma and COPD and what's its mechanism of action?

Theophylline; likely causes bronchodilation by inhibiting phosphodiesterase, increasing the levels of cAMP by decreasing cAMP hydrolysis

What are the toxicities associated with Theophylline?

Usage is limited due to the narrow therapeutic index (cardiotoxicity and neurotoxicity + nausea, vomiting arrhythmias, seizures) metabolized by cytochrome P-450

What drug does theophylline block the action of?

Adenosine

What drug is used in the bronchial challenge test to help diagnose asthma?

Methacholine (Muscarinic receptor M3 agonist)