Respiratory Pharmacology Flashcards by Bina Malapur

In asthma, inflammatory cells release what

mast cells
eosinophils
T helper 2 cells

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what bronchospastic mediators are released in asthma

histamine
leukotriene D4
Prostaglandin D2

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what test/challenge is used to diagnose asthma

Methacholine

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what inflammatory cells are increased in COPD

neutrophils
macrophages
cytotoxic T-lymphocytes

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COPD can cause

progressive fibrosis
emphysema
ariway narrowing
excessive mucus

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what is a risk factor for COPD

smoking

- deficiency in alpha1-proteinase inhibitor

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what is allergic rhinitis and what does it activate

nasal epithelium inflammation

- IgE mediated activation of mast cells, basophils

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what are important mediators of inflammation that induce symptoms characteristic of allergic rhinitis

histamine
prostaglandins
leukotrienes

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where do most of the drugs go if they are inhaled

80-90% swallowed

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Name the drugs that are given orally

Corticosteroids
Adrenergic Agonists
Methylxanthine (theophylline)

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MOA for adrenergic agnoists

stimulates B2-adrenergic receptors

increases cAMP
activates PKA
induces bronchial smooth muscle cell relaxation

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when do short-acting B2-adrenergic receptor agonists work

quick relief during asthma attack

onset 1-5 minutes
duration of action 4-6 hrs

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Name3 long acting B2-adrenergic receptor agonists LABA

Salmeterol
Formoterol
Indacaterol

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which B2-adrenergic receptor agonist for long acting, acts the longest and is it usually used for

Indacaterol

COPD

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Why does Salmeterol have a longer duration of action than albuterol

Salmeterol has lipophilic side chain

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Name B2- selective SABA

Albuterol
Terburtaline
Pirbuterol
Metaproterenol

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what are B2-selective agonists SABA used for

all types of asthma attakcs

- not as effective in COPD

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How often is B2- receptor selective agonists SABA used

not to be used several times a day

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when one overdoses on B2- receptor selective agonist SABA, what more is needed?

need for more anti-inflammatory therapy

corticosteroids and Leukotriene inhibitor

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What can account for the diminshed activity (tolerance) of B2-receptor selective agnoist SABA

B2-recetpor downregulation

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what are adverse effects of B2-receptor selective agonist SABA

Tremor
restlessness
tachycardia
hypokalemia 
- more with oral dose than inhalation

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Name 2 non-selective SABA

Isoproterenol and Epinephrine

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MOA for Isoproterenol

nonselective B-agonist and potent bronchodilator

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MOA for epinephrine

non-selective alpha, beta agonist and potent bronchodilator

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How is Isoproterenol administered and how is it given to

acute asthma attack | -inhaled and oral

What is the law in the US for Isoproterenol

inhalation or sublingual administration is no longer marketed in the US

when is epinephrine used and how is it administered

acute asthma attack | - inhaled or subcutaneously - emergency circumstances

Name B2- selective agonists LABA

Salmeterol Formoterol Indacaterol

what is B2- selective agonists LABA used for

control (prophylaxis therapy) persistent asthma | - effective for asthma and COPD

when should one not take Salmeterol, Formoterol and Indacaterol

for acute asthma attack

what do B2- selective agonists LABA need to be taken with

anti-infammatory therapy ( corticosteroids, leukotriene, inhibitors )

Indacaterol can be specifically be used for what

COPD

Adverse effects of Salmeterol, Formoterol, and Indacaterol? how can this be helped

- airway tolerance to B2 agonists: potential problem | - Corticosteroids may prevent tolerance by increasing B2 receptor numbers within airway

Name 2 muscarinic antagonists

Ipratropium and Tiotropium

MOA of Ipratropium and Tiotropium

- reduces ACH -stimulated cyclic GMP | - inhibits mucus secretion

what is a popular combination inhaler

Ipratropium and Albuterol

Ipratroprium can specially be used for what

nasal discharge from rhinorrhea

What are adverse effects of Muscarinic antagonists

unpleasant bitter taste dryness of mouth cause glaucoma if sprayed in eye

MOA for methylxanthines

bronchodilator and anti-inflammatory activity

name a drug of Methylxanthines

Theophylline

MOA of Theophylline

- inhibits phosphodisterases - functions as adenosine-receptor antagonist - anti-inflammatory - promotes contraction of diaphragmatic muscles

Theophylline is FDA-indicated for what

Asthma and COPD

Theophhylline is used as an adjunct with what in chronic severe asthma that are not controlled by what drugs

- inhaled corticosteroids | - solely with corticosteroids and B-receptor agonsits

Caffeine (Methylxanthine) used to treat what

apnea in preterm infants

what are routes of administration for Theophylline

- intravenous - tablets Not inhaled

What are adverse effects of theophylline

low therapeutic index | toxicity is dose dependant

low level toxicity of theophylline causes

nausea vomiting headache restlessness

higher level toxicity of theophylline causes

cardiac arrhythmias and seizers

what enzyme increases the clearance of Theophylline

CYP1A2

Name corticosteroids

Beclomethasone Triamicinolone acetate Budesonide Fluticasone propionate

MOA for corticosteroids

anti-inflammatory agents - act through glucocorticoid receptor - increases B2 receptors - decreases cytokines

What is a use for corticosteriods?

inhaled corticosteroids are front-line therapy for persistent asthma - less effective in COPD (reserved for COPD)

What are corticosteroid combination inhalers

Fluticasone/Salmeterol | Budesonide/formoterol

how do synergistic interactions between corticosterids and B2-agonists occur

corticosteroids up-regulate B2 receptor expression

nasal spray corticosteroid is used for what

allergic rihinits

What are adverse effects of Corticosteroids

Dysphonia cough oropharyngeal candidiasis

Leukotriene inhibitor is FDA indicated for what

asthma | not front-line therapy for asthma

name 3 Leukotriene inhibitors

Zafirlukast and Montelukast | Zileuton

MOA of Zafirlukast and Montelukast

Antagonize Leukotriene receptor (LT1) - blocks cysteinyl leukotrienes - inhibits bronchoconstriction and airway inflammation

When are leukotriene inhibitors used

potential alternative to medium-dose inhaled corticosteroids ( if corticosteroids are not tolerated) for prophylaxis of mild persistent asthma

what is Montelukast used for

allergic rhinitis

what is MOA for Zileuton

inhibits 5-lipooxygenase, (rate-limiting enzyme in leukotriene biosynthesis)

what is the dosing for Montelukast, Zafirlukast and Zileuton

Montelukast: once daily Zafirlukast: twice daily Zileuton: 4 times daily

how are anti-leukotrienes administered

oral

how are Montelukast, Zafirlukast and Zileuton metabolized

CYPs

what are adverse effects of Anti-leukotrienes

hepatic toxicity

drug interaction of Zafirlukast

Warfarin, causes headache

which anti-leukotriene does not inhibit hepatic CYPs

Montelukast

Name Mast cell stabilizers

Cromolyn and Nedocromil

MOA for Cromolyn and Nedocromil

inhibit mast cell degranulation and histamine release

Name an anti-IgE therapy

Omalizumab

MOA for Omalizumab

humanized monoclonal antibody against IgE. | - inhibits IgE binding to Ige receptors on mast cells

when are anti-IgE therapy used

- not font line asthma therapy | - reserved for severe asthma not controlled by corticosteroids

what is the dosing for Omalizumab

subcutaneous injection every 2-4 weeks

adverse effect of anti-IgE therapy

anaphylaxis

What is alpha-1 proteinase inhibitor FDA-indicated for

COPD patients with deficiency in alpha 1 proteinase inhibitor

what are the effects of alpha-1 proteinase inhibitor?

inhibits the activity of elastase | -excess elastase destroys lung parenchyma

name an opioid found in common cold medications

Hydrocodone and codeine

MOA for hydrocodone and codeine

suppresses cough by direct central action in medulla

what are opioids used for

high doses used for pain | lower doses used for antitussive effects

adverse effects of Hydrocodone and codeine

respiratory depression constipation dysphoria

what is Benzonatate used for and MOA

- cough - peripheral action, targets cough receptors of vagal afferent fibers , located in respiratory passages, lungs and pleura

adverse effect of Benzonatate

Dizziness

what is Expectorant/Guaifenesin used for and adverse effect

- cough | - emetic

Name 2 Mucolytics that are used for cough

N-acetylcysteine | Dornase Alpha

what is Dornase Alpha FDA-indicated for

adjunct for cystic fibrosis

Antihistamines (H1-receptor blockers) are used for what

rhinitis

what Antihistamines (H1-receptor blockers) is used as sleep aid (Tylenol PM)

Diphenhydramine

what are adverse effects of Antihistamines (H1-receptor blockers)

caution with glaucoma and prostate hypertrophy | CNS effects

what are adverse effects of second generation antihistamines

lack significant anticholinergic actions | penetrate poorly into the CNS

what is Ipratropium used for

rhinitis

Name adrenergic agonists that treat Rhinitis

Oxymetazoline pseudoephedrine phenylephrine

MOA for oxymetazoline, pseudophedrine, and phenylephrine

Phanylephrine: selective alpha 1 receptor agonist Oxymetazoline: alpha receptor ( alpha 1 and 2) agonist Pseudoephedrine ( alpha and beta agonist)

Adverse effect of adrenergic agonist

rebound nasal congestion tachycardia hypertension

who should avoid Oxymetazoline, Pseudophedrine, and Phenylephrine

patients with uncontrolled hypertension or ischemic heart disease