Pharm 47 - Asthma Flashcards

1
Q

Two ways asthma medications work?

A

1) By relaxing bronchial smooth muscle

2) By preventing and treating inflammation

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2
Q

How does the autonomic system regulate smooth muscle?

A

Sympathetic (adrenergic) tone causes bronchodilation; Parasympathetic (cholinergic) tone causes bronchoconstriction; Nonadrenergic, noncholinergic (NANC) fibers also innervate the respiratory tree

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3
Q

What is the main type of receptor expressed on airway smooth muscle cells? What chemical activates them?

A

Beta2-adrenergic receptors are activated by epinephrine, which is secreted by the adrenal medulla -> causes bronchodilation

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4
Q

How do parasympathetics create effects in the lungs?

A

Muscarinic (M3) receptors on airway smooth muscles are stimulated by acetylcholine -> causes bronchoconstriction

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5
Q

How do NANC fibers create effects?

A

NANC fibers are primarily under parasympathetic control. They are either stimulatory (cause bronchoconstriction) or inhibitory (cause bronchodilation). They release Neurokinin A, Calcitonin gene-related peptide, substance P, bradykinin, tachykinin, and neuropeptide Y to bronchoconstrict. NO and VIP cause bronchorelaxation.

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6
Q

What is more potent than histamine at producing bronchoconstriction?

A

Leukotriene D4

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7
Q

What are the two categories of asthma medications?

A

1) Relievers (bronchodilators)

2) Controllers/Preventers (anti-inflammatory)

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8
Q

Anticholinergics MOA

A

Antagonists at muscarinic receptors on airway smooth muscle and glands -> decreased bronchoconstriction and mucus secretion

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9
Q

Name the Anticholinergics (2)

A

Ipratropium, Tiotropium (long duration of action)

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10
Q

Anticholinergic clinical applications (3)

A

Asthma (not approved by FDA), COPD, Rhinitis

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11
Q

Adverse Effects Include Paralytic ileus, angioedema, bronchospasm; also abnormal taste, dry mouth/nasal mucus, constipation, tachycardia, urinary retention; if accidentally squirted in eye, can cause mydriasis and increased intraocular pressure -> angle-closure glaucoma

A

Anticholinergics

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12
Q

Anticholinergic contraindications

A

Hypersensitivity to drug or to soya lecithin

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13
Q

Has long duration of action b/c of slow dissociation from M1/M3 receptors

A

Tiotropium (Anticholinergic)

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14
Q

Agonists at Beta-adrenergic receptors; act through stimulatory G protein to cause smooth muscle relaxation and bronchodilation

A

Beta-Adrenergic Agonist MOA

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15
Q

Beta-adrenergic agonist

Used for asthma, anaphylaxis, cardiac arrest, open-angle glaucoma

A

Epinephrine (class and clinical applications)

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16
Q

Adverse Effects Include arrhythmias, hypertensive crisis, pulmonary edema; also tachycardia, palpitations, sweating, N/V, tremor, nervousness, dyspnea

A

Epinephrine

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17
Q

Contraindications Include Narrow-angle glaucoma (opthalmic form), MAOI use w/in 2 weeks (inhaled form)

A

Epinephrine

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18
Q

Non-selective agonist binds alpha (HTN), beta1 (cardiac stimulation), and beta2 (bronchodilation) adrenergic receptors

A

Epinephrine

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19
Q

Beta-adrenergic agonist

Used for asthma, cardiac arrest, decreased vascular flow, heart block, shock, Stokes-Adams syndrome

A

Isoproterenol

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20
Q

Adverse effects include Tachyarrythmia, palpitations, dizziness, HA, tremor, restlessness

A

Isoproterenol

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21
Q

Contraindications include Tachyarrythmias, angina, digitalis-induced tachycardia/heart block

A

Isoproterenol

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22
Q

Binds beta 1 (cardiac stimulation) and beta 2 (bronchodilation) adrenergic receptors

A

Isoproterenol therapeutic considerations

23
Q

Irritating list of Selective Beta2 Receptor Agonists (7)

A

Metaproterenol, Albuterol (Salbutamol), Levalbuterol, Terbutaline, Pirbuterol, Isoetharine, Bitolterol (MALTs with mr. PIB)

24
Q

Selective Beta2 Receptor Agonists clinical applications

A

Asthma, COPD

25
adverse effects include Tachyarrythmia, palpitations, dizziness, HA, tremor, restlessness (BUT less cardiac effects since they're Beta2 selective)
Selective Beta2 Receptor Agonists and M[E/O]TEROLs
26
Selective Beta2 Receptor Agonists therapeutic considerations
Terbutaline, albuterol, pirbuterol, and bitolterol cause fewer cardiac effects; Levalbuterol is more Beta2 selective than albuterol
27
-M[E/O]TEROLs (class and clinical applications)
Beta-adrenergic agonist | COPD (formoterol, salmeterol, arformoterol); Asthma (formoterol, salmeterol)
28
Long acting (LABAs) (12-24 hours); Should not be used as asthma monotherapy b/c of increased risk of death from asthma (use with inhaled corticosteroid)
-M[E/O]TEROLs therapeutic considerations
29
MOA Nonselective phosphodiesterase inhibitors, prevent degradation of cAMP, act as adenosine receptor antagonist -> smooth muscle relaxation and bronchodilation
Methylxanthines
30
Name the Methylxanthines (2)
Theophylline, aminophylline
31
Methylxanthine clinical applications
Asthma, COPD
32
Adverse effects include Ventricular arrhythmia, seizure; also tachyarrhythmias, N/V, insomnia, tremor, restlessness
Methylxanthine
33
Inhibition of PDE III and IV in smooth muscle -> bronchodilation; inhibition of PDE IV in T cells and eosinophils -> anti-inflammatory/ immunomodulatory; MONITOR PLASMA LEVELS; avoid co-administration with fluvoxamine, enoxacin, mexiletine, propranolol, troleandomycin -> theophylline toxicity; avoid co-administration with zafirlukast -> lower plasma concentration of zafirlukast Drug-drug interactions w/ CYP3A inhibitors (cimetidine, -azole antifungals)
Methylxanthine
34
MOA Inhibits Ca2+ transport into smooth muscle cells -> smooth muscle relaxation
Magnesium Sulfate
35
Used for Atrial paroxysmal tachycardia, barium poisoning, cerebral edema, eclampsia, hypomagnesmia, seizure
Magnesium Sulfate
36
Adverse effects include Heart block, hypotension, prolonged bleeding time, hyporeflexia, CNS depression, respiratory tract paralysis
Magnesium Sulfate
37
Magnesium Sulfate contraindications
Heart block, myocardial damage
38
Therapeutic considerations Include Tocolytic agent causes uterine relaxation -> delay preterm labor; may benefit pts w/ acute asthma exacerbation
Magnesium Sulfate
39
MOA Inhibit COX-2 action and prostaglandin synthesis by inducing lipocortins; inhibition of IL-4 and IL-5 strongly reduces inflammatory response in asthma
Inhaled Corticosteroids
40
Irritating list of Inhaled Corticosteroids (7)
Beclomethasone, triamcinolone, fluticasone, budesonide, flunisolide, mometasone, ciclesonide (Bec, Bud, and Mom went to Triam (Try on?) Flutes and to eat Flun (flan?) and iCicles....)
41
Corticosteroid clinical applications
Inflammatory conditions, autoimmune diseases
42
Adverse effects Include Immunosuppression, cataracts, hyperglycemia, hypercortisolism, depression, euphoria, osteoporosis, growth retardation in children, muscle atrophy; also impaired wound healing, HTN, fluid retention, oropharyngeal candidiasis, dysphonia
Inhaled Corticosteroid
43
Corticosteroid contraindications
Systemic fungal infections
44
Therapeutic considerations include: Does not correct underlying disease, only limits effects of inflammation; requires tapering dosage after chronic use to avoid adrenal insufficiency; inhaled corticosteroids have fewer systemic adverse effects (can be reduced further by using large-volume spacer and rinsing mouth after use); inhaled steroids (except beclomathasone and triamcinolone) are subject to 1st-pass metabolism, so they don't reach systemic circulation
Inhaled Corticosteroid
45
MOA Inhibit Cl- transport, which affects Ca2+ gating and prevents granule release Also includes Nedocromil
Cromolyn
46
Clinical applications: Asthma, allergic rhinitis, keratitis, keratoconjunctivitis, mast-cell disorder, vermal conjunctivitis
Cromolyn
47
Adverse effects: Abnormal taste, burning eyes, cough, throat irritation
Cromolyn
48
Therapeutic considerations: Prophylaxis of allergic asthma and exercised-induced asthma; more effective in kids/young adults vs. elderly; excellent safety profile, but not as effective as other asthma medications
Cromolyn
49
MOA: Humanized mouse antibody; prevents IgE from binding Fc on mast cells and APCs; decreases circulating IgE
Omalizumab
50
Omalizumab clinical applications
Asthma
51
Adverse effects: Anaphylaxis; also, injection site reaction, rash, HA
Omalizumab
52
Therapeutic considerations: Affects both early- and late-phase asthmatic responses, administered subcutaneously every 2-4 wks (must monitor after injection for several hours due to possible immune response)
Omalizumab
53
Has slow onset of action so it should not be used for acute asthma flares.
Salmeterol