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Step 1 Pharmacology > Respiratory > Flashcards

Respiratory Flashcards

1
Q

What is the mechanism of H1 blockers?

A

Reversible inhibitors of H1 histamine receptors

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2
Q

What are the 1st generation H1 blockers?

A

Diphenhydramine, dimenhydrinate, chlorpheniramine.

Names contain “-en/-ine” or “-en/-ate.”

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3
Q

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

A

Allergy, motion sickness, sleep aid.

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4
Q

What are the toxicities of the 1st generation H1 blockers?

A

Sedation, antimuscarinic, anti-α-adrenergic.

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5
Q

What are the 2nd generation H1 blockers?

A

Loratadine, fexofenadine, desloratadine, cetirizine.

Names usually end in “-adine.”

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6
Q

What is the clinical use of the 2nd generation H1 blockers?

A

Allergy

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7
Q

What are the toxicities of the 2nd generation H1 blockers?

A

Far less sedating than 1st generation because of ↓ entry into CNS.

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8
Q

Expectorants - What are the features of Guaifenesin?

A

Expectorant—thins respiratory secretions; does not suppress cough reflex.

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9
Q

Expectorants - What are the features of N-acetylcysteine?

A

Mucolytic—can loosen mucous plugs in CF patients. Also used as an antidote for acetaminophen overdose.

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10
Q

What are the features of Dextromethorphan?

A

Antitussive (antagonizes NMDA glutamate receptors). Synthetic codeine analog. Has mild opioid effect when used in excess. Naloxone can be given for overdose. Mild abuse potential.

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11
Q

What is the mechanism of Pseudoephedrine and phenylephrine?

A

Sympathomimetic α-agonistic nonprescription nasal decongestants.

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12
Q

What is the clinical use of Pseudoephedrine and phenylephrine?

A

Reduce hyperemia, edema, and nasal congestion; open obstructed eustachian tubes. Pseudoephedrine also illicitly used to make methamphetamine.

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13
Q

What are the toxicity of Pseudoephedrine and phenylephrine?

A

Hypertension. Can also cause CNS stimulation/anxiety (pseudoephedrine).

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14
Q

How is Asthma therapy directed?

A

Bronchoconstriction is mediated by (1) inflammatory processes and (2) parasympathetic tone; therapy is directed at these 2 pathways.

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15
Q

Asthma (β2-agonists) - What are the features of Albuterol?

A

Relaxes bronchial smooth muscle (β2). Use during acute exacerbation.

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16
Q

Asthma (β2-agonists) - What are the features of Salmeterol and formoterol?

A

Long-acting agents for prophylaxis. Adverse effects are tremor and arrhythmia.

17
Q

Asthma - What are the features of Methylxanthines?

A

Theophylline—likely causes bronchodilation by inhibiting phosphodiesterase → ↑ cAMP levels due to ↓ cAMP hydrolysis. Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity); metabolized by cytochrome P-450. Blocks actions of adenosine.

18
Q

Asthma - What are the features of Muscarinic antagonists?

A

Ipratropium—competitive block of muscarinic receptors, preventing bronchoconstriction. Also used for COPD, as is tiotropium, a long-acting muscarinic antagonist.

19
Q

Asthma - What are the features of corticosteroids?

A

Beclomethasone, fluticasone—inhibit the synthesis of virtually all cytokines. Inactivate NF-κB, the transcription factor that induces the production of TNF-α and other inflammatory agents. 1st-line therapy for chronic asthma.

20
Q

Asthma - What are the features of Antileukotrienes?

A

Montelukast, zafirlukast—block leukotriene receptors. Especially good for aspirin-induced asthma.
Zileuton—a 5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes.

21
Q

Asthma - What are the features of Omalizumab?

A

Monoclonal anti-IgE antibody. Binds mostly unbound serum IgE and blocks binding to FcεRI. Used in allergic asthma resistant to inhaled steroids and long-acting β2-agonists.

22
Q

What are the features of Methacholine?

A

Muscarinic receptor agonist. Used in bronchial provocation challenge to help diagnose asthma.

23
Q

What are the features of Bosentan?

A

Used to treat pulmonary arterial hypertension. Competitively antagonizes endothelin-1 receptors, ↓ pulmonary vascular resistance.

24
Q

Describe the pathway towards asthma.

A

Therapy is in [ ]
Exposure to antigen (dust, pollen, etc.) [Avoidance] → Antigen and IgE on mast cells [Omalizumab] → [Steroids] Mediators (leukotrienes, histamine, etc.) →
a) [Steroids, Antileukotrienes] → Late response: inflammation → Bronchial hyperreactivity
b) [β-agonists, Theophylline, Muscarinic antagonists] → Early response: bronchoconstriction → Symptoms

25
Q

Asthma - What are the features of corticosteroids?

A

Beclomethasone, fluticasone—inhibit the synthesis of virtually all cytokines. Inactivate NF-κB, the transcription factor that induces the production of TNF-α and other inflammatory agents. 1st-line therapy for chronic asthma.

26
Q

Asthma - What are the features of Antileukotrienes?

A

Montelukast, zafirlukast—block leukotriene receptors. Especially good for aspirin-induced asthma.
Zileuton—a 5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes.

27
Q

Asthma - What are the features of Omalizumab?

A

Monoclonal anti-IgE antibody. Binds mostly unbound serum IgE and blocks binding to FcεRI. Used in allergic asthma resistant to inhaled steroids and long-acting β2-agonists.

28
Q

What are the features of Methacholine?

A

Muscarinic receptor agonist. Used in bronchial provocation challenge to help diagnose asthma.

29
Q

What are the features of Bosentan?

A

Used to treat pulmonary arterial hypertension. Competitively antagonizes endothelin-1 receptors, ↓ pulmonary vascular resistance.

30
Q

Describe the pathway towards asthma.

A

Therapy is in []
Exposure to antigen (dust, pollen, etc.) [Avoidance] → Antigen and IgE on mast cells [Omalizumab] → [Steroids] Mediators (leukotrienes, histamine, etc.) →
a) [Steroids, Antileukotrienes] → Late response: inflammation → Bronchial hyperreactivity
b) [β-agonists, Theophylline, Muscarinic antagonists] → Early response: bronchoconstriction → Symptoms

31
Q

What can Methemoglobinemia be treated with?

A

Methylene blue

32
Q

How do you treat cyanide poisoning?

A

Use nitrites to oxidize Hb to methemoglobin, which binds cyanide. Use thiosulfate to bind this cyanide, forming thiocyanate, which is renally excreted.

33
Q

A response to high altitude is ↑ renal excretion of HCO3- to compensate for respiratory alkalosis. What drug can augment this?

A

Acetazolamide

34
Q

How do you treat Deep venous thrombosis?

A

Use heparin for prevention and acute management; use warfarin for long-term prevention of DVT recurrence.

35
Q

What drugs cause interstitial lung diseases (pulmonary ↓ diffusing capacity, ↑ A-a gradient)?

A

Bleomycin, busulfan, amiodarone, methotrexate

Step 1 Pharmacology (18 decks)

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