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deck_3452463 Flashcards

1
Q

How do H1 blockers work?

A

Reversible inhibitors of H1 histamine receptors.

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2
Q

What are the 1st generation H1 blockers?

A
  1. Diphenhydramine2. Dimenhydrinate3. Chlorpheniramine
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3
Q

Diphenhydramine

A

first generation H1 blocker

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4
Q

Dimenhydrinate

A

first generation H1 blocker

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5
Q

Chlorpheniramine

A

first generation H1 blocker

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6
Q

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

A
  • Allergy- Motion skickness- sleep aid
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7
Q

What are first generation H1 blocker toxicities?

A
  • sedation- antimuscarinic- anti alpha adrenergic
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8
Q

What are the 2nd generation H1 blockers?

A
  1. Loratadine2. Fexofenadine3. Desloratadine4. Cetirizine
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9
Q

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

A

Allergy

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10
Q

What are the second generation H1 blocker toxicities?

A

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

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11
Q

Loratadine

A

2nd generation H1 blocker

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12
Q

Fexofenadine

A

2nd generation H1 blocker

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13
Q

Desloratadine

A

2nd generation H1 blocker

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14
Q

Cetirizine

A

2nd generation H1 blocker

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15
Q

Expectorant

A
  • thins respiratory secretions - does not suppress cough reflex
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16
Q

Guaifenesin

A

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

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17
Q

N-acetylcystein

A

Mucolytic - can loosen mucous plugs in CF patients by disrupting disulfide bonds. Also used as an antidote for acetaminophen overdose.

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18
Q

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. May cause serotonin syndrome if combined with other serotonergic agents.

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19
Q

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. May cause serotonin syndrome if combined with other serotonergic agents.

A

Dextromethorphan

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20
Q

Mucolytic - can loosen mucous plugs in CF patients by disrupting disulfide bonds. Also used as an antidote for acetaminophen overdose.

A

N-acetylcystein

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21
Q

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

A

Guaifenesin

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22
Q

Pseudoephedrine, phenylephrine mechanism

A

α-adrenergic agonists, used as nasal decongestants

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23
Q

α-adrenergic agonists, used as nasal decongestants

A

pseudoephedrine, phenylephrine

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24
Q

Pseudoephedrine, phenylephrine clinical use

A
  1. reduce hyperemia, edema, nasal congestion2. open obstructed eustachian tubesPseudoephedrine also illicitly used to make methamphetamine.
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25
Q

Pseudoephedrine, phenylephrine toxicity

A

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

26
Q

What are the pulmonary hypertension drugs?

A
  1. Endothelin receptor antagonist2. PDE-5 inhibitors3. Prostacyclin analogs
27
Q

An example of Endothelin receptor antagonists

28
Q

An example of PDE-5 inhibitors

A

Sildenafil

29
Q

An example of Prostacyclin analogs

A

Epoprostenoliloprost

30
Q

Endothelin receptor antagonists

A

Include bosentan.Competitively antagonize endothelin-1 receptors → ↓ pulmonary vascular resistance.Hepatotoxic (monitor LFTs).

31
Q

PDE-5 inhibitors

A

Include sildenafil. Inhibit cGMP PDE5 and prolong vasodilatory effect of nitric oxide. Also used to treat erectile dysfunction.

32
Q

Prostacyclin analogs

A

Include epoprostenol, iloprost. Prostacyclins (PGI2) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds. Inhibit platelet aggregation.Side effects: flushing, jaw pain.

33
Q

How do asthma drugs work?

A

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

34
Q

Classes of asthma drugs

A
  1. β2-agonists2. Corticosteroids3. Muscarinic antagonists4. Antileukotrienes5. Omalizumab6. Methylxanthines
35
Q

Methacholine

A

Muscarinic receptor (M3) agonist. Used in bronchial challenge test to help diagnose asthma.

36
Q

Short term Beta-2 agonists

A

Albuterol.

37
Q

Albuterol

A

Short term Beta-2 agonist. Relaxes bronchial smooth muscle (β2). Used during acute exacerbation.

38
Q

Long term Beta-2 agonists

A

Salmeterol and formoterol.

39
Q

Salmeterol

A

Long term beta 2 agonist. Long-acting agents for prophylaxis. Adverse effects are tremor and arrhythmia.

40
Q

Formoterol

A

Long term beta 2 agonist. long-acting agents for prophylaxis. Adverse effects are tremor and arrhythmia.

41
Q

What do beta 2 agonists do?

A

Relax bronchial smooth muscle (note that we’re talking about sympathetic stimulation relaxing bronchioles).Atp → [adenylyl cyclase] → cAMP → bronchodilation. Beta 2 agonists activate adenylyl cyclase to cause bronchodilation.

42
Q

What do corticosteroids do?

A

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 for chronic asthma.

43
Q

Corticosteroids

A

Fluticasone and budesonide

44
Q

fluticasone

A

Corticosteroid. Inhibits 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 for chronic asthma.

45
Q

budesonide

A

Corticosteroid. Inhibits 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 for chronic asthma.

46
Q

Muscarinic receptor (M3) agonist. Used in bronchial challenge test to help diagnose asthma.

A

Methacholine

47
Q

Muscarinic antagonists

A

Ipatropium and tiotropium.

48
Q

What do muscarinic antagonists do?

A

Competitively blocks muscarinic receptors, preventing bronchoconstriction. Also used for COPD. (Remember that parasympathetics are going to constrict the bronchioles).

49
Q

Ipratropium

A

Muscarinic antagonist. Competitively blocks muscarinic receptors, preventing bronchoconstriction. Also used for COPD. (Remember that parasympathetics are going to constrict the bronchioles).

50
Q

Tiotropium

A

Long acting muscarinic antagonist. competitively blocks muscarinic receptors, preventing bronchoconstriction. Also used for COPD. (Remember that parasympathetics are going to constrict the bronchioles).

51
Q

Antileukotrienes

A

Montelukast, zafirlukast, and zileuton.

52
Q

Montelukast

A

Antileukotriene. Block leukotriene receptors (CysLT1). Especially good for aspirin-induced asthma.

53
Q

Zafirlukast

A

Antileukotriene. Block leukotriene receptors (CysLT1). Especially good for aspirin-induced asthma.

54
Q

Zileuton

A

5-lipoxygenase pathway inhibitor. Blocks conversion of arachidonic acid to leukotrienes. Hepatotoxic.

55
Q

Draw a diagram and show where antileukotrienes work

56
Q

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.

57
Q

Mexylthanthines

A

Theophylline

58
Q

Theophylline

A

Mexylthanthine. Inhibits phosphodiesterase → ↑ cAMP levels due to ↓ cAMP hydrolysis.Atp → [adenylyl cyclase] → cAMP → bronchodilation.Usually PDE breaks down cAMP to AMP, theophylline prevents this from happening to increase cAMP.Usage is limited because of narrow therapeutic index (cardiotoxicity, neurotoxicity); metabolized by cytochrome P-450.Blocks actions of adenosine (causes bronchoconstriction).

59
Q

What do mexylthanthines do?

A

Likely cause bronchodilation by inhibiting phosphodiesterase → ↑ cAMP levels due to ↓ cAMP hydrolysis.Narrow therapeutic index. Metabolized by P-450. Blocks the actions of adenosine.

60
Q

Draw a diagram and show where beta agonists, mexylthanthines, and muscarinic antagonists work

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