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27 Respiratory tract > Leukotriene inhibitors + phosphodiesterase inhibitor > Flashcards

Leukotriene inhibitors + phosphodiesterase inhibitor Flashcards

1
Q

Leukotriene inhibitors - 2 groups

A

Leukotriene receptor antagonists.

5-lipoxygenase inhibitors

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2
Q

Leukotriene receptor antagonists - 2 drugs

5-lipoxygenase inhibitor - 1 drugs

A

Leukotriene receptor antagonists - montelukast, zafirlukast.

5-lipoxygenase inhibitor - Zileuton.

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3
Q

Montelukast and zafirlukast - MOA

A

Structurally similar to cysteinyl leukotrienes. Competative inhibition of CysLT1. Inhibit early and late phases of asthma.
Do not inhibit effects of leukotriene B4.

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4
Q

Leukotriene receptor antagonists - adm

A

Oral.

Zafirlukast - 2 hours after food

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5
Q

Leukotriene receptor antagonists - interactions

A

Enhance bronchodilating effect of β2-agonitst
Zafirlukast: metabolized by P450 enzymes. Inhibits CYP2C9 (phenytoin, warfarin) and CYP3A4 (felodipine, lovastatin, triazolam)

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6
Q

Montelukast and zafirlukast - indications

A

Asthma: pt unable/unwilling to take steroids. Asthma that is not adequately controlled by steroids alone.
Allergic, aspirin-sensitive, and exercised-induced asthma.

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7
Q

Montelukast and zafirlukast are most effective for which pts?

A

Young children

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8
Q

Leukotriene receptor antagonists - onset

A

Maximal effect after weeks/months.

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9
Q

Leukotriene receptor antagonists - adverse effects

A

Rarely cause side effects.
Liver injury and failure.
Churg-Strauss syndrome (allergic granulomatous vasculitis) - if montelukast or zafirlukast replaces glucocorticoids.

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10
Q

Zileuton - MOA

A

Inhibits 5-lipoxygenase, blocking formation of all leukotrienes

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11
Q

Zileuton is most effective for …

A

Severe asthma

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12
Q

Zileuton - adverse effects

A 
Flulike syndrome.
Headache.
Drowsiness.
Dyspepsia.
Hepatitis.
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13
Q

Zileuton - contraindications

A

Caution in high alcohol consumption.

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14
Q

Zileuton - interactions

A

Inhibits CYP1A3 and CYP3A4 - elevate theophylline and warfarin

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15
Q

Leukotriene receptor antagonist preferred in concomitant drug therapy

A

Montelukast.

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16
Q

Phosphodiesterase inhibitor - 1 drug

A

Roflumilast

17
Q

Roflumilast - MOA

A

Selective inhibitor of PDE in lungs. Increases cAMP intracellularly

18
Q

Roflumilast - indications

A

Reduce risk of COPD exacerbations in chronic bronchitis in pts with history of exacerbations.

19
Q

Roflumilast - adverse effects

A

Diarrhea, nausea, weight loss.

Anxiety, insomnia, depression.

20
Q

Roflumilast - interactions

A

Metabolized by CYP3A4 and CYP1A2

21
Q

Roflumilast - contraind

A 
Strong inducers (rifampin) and inhibitors (erythromycin) of CYP enzymes. 
Acute respiratory episodes (has no function in these cases)
22
Q

Roflumilast - adm

A

Orally

27 Respiratory tract (8 decks)

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