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Asthma Drugs
IUSM
20
Pharmacology
Professional
02/09/2015

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Term
albuterol (asthma)
Definition
Class: asthma, beta2 receptor agonist

Mechanism: short-acting beta2 selective receptor agonist, bronchodilates, activates cAMP in SMC

Indication: rescue inhaler

Contraindication: cardiac disease, MAO-inhibitors

Adverse Effects: tachycardia, mild hypotension, tremor
Term
salmeterol (asthma)
Definition
Class: asthma, beta2 agonist

Mechanism: long-acting beta2 selective agonist, bronchodilates via cAMP activation; long action due to absorption into epithelial lung cells

Indication: prophylactic tx

Contraindication: cardiac disease, MAO-inhibitors

Adverse Effects: tachycardia, mild hypotension, tremor
Term
theophylline
Definition
Class: asthma, methylxanthine

Mechanism: bronchodilates via increase cAMP and blocks adenosine A2 receptors

Indication: maintenance therapy for asthma/COPD (less use now b/c of beta2)

Adverse Effects: insomnia, agitation, tachycardia, tremor [think caffeine side effects]
Term
ipratropium
Definition
Class: asthma, muscarinic antagonist

Mechanism: muscarinic antagoonists --> bronchodilation; antagonizes PSNS induced constriction

Indication: COPD, combo bronchodilators for asthma (esp. pt who can't take Beta2 agonists)

Adverse Effects: minimal CNS effects (poor absorption)
Term
cromolyn
Definition
Class: asthma, mast cell stabilizer

Mechanism: inhibit mast cell degranulation, prevents release of autocoids (histamine and leukotriences, etc)

Indication: inhalation prophylaxis of mild-moderate asthma; with glucocorticoids in moderate-severe

Adverse Effects: bad taste, cough, wheeze, bronchospasm, HA
Term
zafirlukast
Definition
Class: asthma, LT receptor antagonism

Mechanism: prevents action of leukotrienes; bronchodilates and reduces inflammation

Indication: prophylactic tx in mild asthma

Adverse Effects: rare inflammatory condition (pulm infiltrates, neuropathy, skin rashes, vasculitis)
Term
zileuton
Definition
Class: asthma, lipoxygenase inhibitor

Mechanism: inhibits 5-lipoxygenase, prevent formation of leukotrienes; bronchodilates and reduces inflammation

Indication: prophylactic tx for mild asthma

Adverse Effects: rare elevated liver enzymes
Term
omalizumab
Definition
Class: asthma, anti-IgE antibody

Mechanism: binds Fc domain of IgE and prevents interaction w/ receptor on mast cells; IV or subq every 2-4wks; reduce airway responsiveness and decrease need for other drugs

Indication: asthma severe and refractive to other therapy

Adverse Effects: infection/pain on injection, very expensive
Term
cortisol (hydrocortisone)
Definition
Class: asthma, glucocorticoid; endogenous

Mechanism: decrease inflammatory reponse, reduce cytokine release, reduce eicosanoid production

Indication: asthma reduce inflammation
Term
prednisone
Definition
Class: asthma, glucocorticoid

Mechanism: decrease inflammatory reponse, reduce cytokine release, reduce eicosanoid production; 4-6X MORE POTENT THAN CORTISOL FOR ANTI-INFLAMMATORY (little mineralocorticoid activity)

Indication: asthma reduce inflammation
Term
dexamethosone
Definition
Class: asthma, glucocorticoid

Mechanism: suppress ACTH production; 18X MORE POTENT THAN CORTISOL, no mineralocorticoid activity

Indication: diagnosis of cortisol disorders
Term
beclomethasone
Definition
Class: asthma, glucocorticoid inhaler

Mechanism: suppress inflammation,

Indication: daily inhaler for suppression of inflammation in asthma

Adverse Effects: hoarse voice, oral candidiasis
Term
asthma drugs that bronchodilate
Definition
beta2 receptor agonists
methylxanthines
muscarinic antagonists
leukotriene antagonism
Term
asthma drugs that reduce inflammation
Definition
glucocorticoids
inhibit mast cell degranulation
leukotriene antagonism
anti-IgE antibody
Term
glucocorticoid general actions
Definition
antagonize insulin, promotes gluconeogenesis
increases muscle catabolism
augment GH action on lipolysis, increase TGs
decrease inflammatory response
reduce cytokine release
reduce production of eicosanoids
Term
glucocorticoid pharmacokinetics
Definition
well absorbed in GI tract
cortisol highly ppb (cortisol-binding globulin and albumin, synthetics are less so)
lipophilic
metabolized by liver (11B-hydroxysteroid dehydrogenase I activates prednisone)
Term
glucocorticoid uses
Definition
replacement therapy (Addison's)
anti-inflammatory (immune suppression)
inhaled for asthma
topical for psoriasis and dermatitis
depot injections for arthritis/gout
immunosuppression for transplant and adjunct in blood cancer tx
Term
glucocorticoid side effects
Definition
inc. susceptibility to infection
increased glucose levels and DM
2* hyperparathyroidism
osteoporosis
edema
suppression of linear bone growth in kids
steroid psychosis (rare)
Cushing's syndrome
withdrawal rebound phenomenon (adrenal insufficiency)
myopathy
Term
glucocorticoids + beta blocer combos for asthma
Definition
fluticasone + salmeterol
budesonide + formoterol
mometasone + formoterol
Term
severity of asthma + managment
Definition
mild/intermittent: beta2 agon as needed
mild/persistent: inhaled glucocorticoid/cromolyn/LT receptor antag + beta2 agon as needed
moderate/persistent: inhaled glucocorticoid/LABA/theophylline + beta2 agon as needed
severe/persistent: inhaled glucocorticoid/LABA/theophylline/systemic glucocorticoid/anti-IgE Ab
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