Pulm Drugs

Question 1

Medicates for acute exacerbations?

Answer 1

SABA (albuteral) Short acting anticholinergics (ipratropium) systemic corticosteroids

Question 3

MEdications for maintenance treatment of asthma?

Answer 3

ICS LABA (+ICS) Cromolyn and nedocromil LT modifiers (Montelukast for example or Zileuton) Omalizumab (allergic asthma if all else fails)

Question 5

Medications for maintenance of COPD?

Answer 5

Long-acting anticholinergics LABA (can see ICS too)

Question 6

In general, what agents are commonly used for COPD and Asthma? Categorical

Answer 6

1) Bronchodilators: Beta2agonists, Anticholinergics, Theophylline 2) Anti-inflammatory agents: steroids, cromolyn and nedocromil, Leukotriene modifiers, or Omalizumab

Question 8

What is the mechanism of beta2 agonists?

Answer 8

stimulates B2 receptors to increase cAMP and leads to SM relaxation, bronchodilation, mast cell destabalization, and skeletal muscle stimulation

Question 10

What are the short acting beta agonists? What is their clinical use?

Answer 10

Albuterol (acute releif and treatmnent of Ashtma and COPD) Terbutaline - systemic injections and more side effects Used for acute exacerbation, Exercise-induced asthma, and Acute COPD

Question 12

What are the clinical uses for LABA?

Answer 12

maintenance therapy for prevention of bronchospasm in asthma (MUST be used with inhaled corticosteroids) Maintenance for prevention in COPD

Question 14

What are side effects of beta agonists?

Answer 14

Tachycardia and palpitations transient decrease in serum K Tremors Lactic acidosis at very high doses of Albuteral Increased risk of asthma-death with LABA used alone

Question 16

what is the mechanism for anticholinergics?

Answer 16

block M1 and M3 receptor activation so blocks Ach from activating receptor to increase cellular levels of cGMP and cause bronchodilation AND block M2 activation to stop further release of Ach

Question 18

How are the anticholinergics used clinically?

Answer 18

short acting: used for acute exacerbations of asthma and COPD and maintenance treatment of bronchospasm associated with COPD Long acting: maintenance of bronchospams in COPD only!!

Question 20

What are the anticholinergics used?

Answer 20

Short acting = Ipratropium Bromide Long acting = Tiotropium!! (and also aclidinium bromide)

Question 22

what are side effects of anti-cholinergics?

Answer 22

blurred vision, dry mouth, nausea, urinary retention, CNS effects, tachycardia Increased CV events!

Question 24

What are the Methylxanthins?

Answer 24

Theophylline (PO) and Amniphylline (IV)

Question 26

mechanism of Methylxanthines??

Answer 26

non-selective inhibitor of PDE leads to increased cAMP and cGMP for bronchodilation Has additional effects of regulating inflammatory cells and is competitive antagonist of Adenosine (so stimulates endogenous catecholamine release onto Beta 2 for additional dilation) **VERY NARROW THERAPEUTIC WINDOW

Question 28

Clinical use of methylxanthines?

Answer 28

acute exacerbation of asthma when all else fails treatment of symptoms and reversible airflow obstruction associated with chronic asthma and COPD/Emphysema

Question 30

Side Effects of Methylxanthines?

Answer 30

N/V and gastric upset (heartburn) Tachyarrhythmias!!!! (catecholamine release on heart) Jitteriness, insomnia, headache and seizures!

Question 32

mechanism of corticosteroids?

Answer 32

Glucocorticoid combines with receptor and acts as a transcription factor that leads to 1) activation of IkBeta which inhibits NFKbeta to decrease signals for production of inflammatory proteins 2) binds AP1 gene and decreases transcription of pro-inflammatory mediators like TNF and IL2

Question 34

what are the clinical effects and clinical uses of corticosteroids?

Answer 34

Effects: reduce inflammatory cell activation, recruitment, and infiltration and decrease vascular permeability Clinical use: - exacerbation of asthma/COPD - maintenance to prevent bronchospasms and symptoms of asthma and COPD -allergic rhinitis

Question 36

what are the acute side effects of steroids? more chronic side effects? What effects with inhaled steroids?

Answer 36

Salt/water retention, hyperglucemia, HTN Chronic - HPA axis suppression, bone resporption, skel muscle myopathy, pancreatitis, cataracts, skin thinning, growth retardation, etc Inhaled - oral thrush and hoarseness

Question 38

what is the mechanism of cromolyn and nedocromil?

Answer 38

Mast cell stabilizers inhibit degranulation in response to stimuli, activation and release of mediators, and neurally mediated bronchoconstriction as additional dilatory effect

Question 40

clinical use for cromolyn and nedocromil?

Answer 40

long term for prevention of symptoms of asthma - good for mild asthma Preventative treatment prior to exposure to allergen or exercise

Question 42

Side effects of cromolyn and nedocromil?

Answer 42

relatively safe! cough and wheezing and bad taste in mouth with nedocromil

Question 44

What are the leukotriene modifiers?

Answer 44

LT receptor Antagonists: Zafirlukast and Montelukast (=singular - 1/day!) 5-LPO inhibitor (block conversion of arachadonic acit to LT) = Zileuton

Question 46

clinical use for LT modifiers?

Answer 46

long term control and prevention of symptoms in mild-persistent asthma allergic rhinitis

Question 48

Side effects of LT modifiers?

Answer 48

LT receptor antagonists (Zafirlukast and montelukast) = HA, nausea and abdominal pain 5-LPO inhibitor (Zileuton) = Liver toxicity and Hyperbilirubinemia

Question 50

Mechanism of Omalizumab?

Answer 50

blocks Fc portion of IgE antibody and prevents its binding to mast cells etc blocks IgE release of mast cells and decreases levels of IgE given as subcutaneous injections

Question 52

clinical use of omalizumab?

Answer 52

treatment of allergic asthma that’s not well controlled with use of corticosteroids Dosing depends on baseline IgE

Question 54

Side effects of OMalizumab?

Answer 54

ANAPHYLAXIS!!!!!! given as Sub-Q injection in monitored setting

Question 56

Where are the 3 different H receptors found?

Answer 56

H1 = lung, vascular SM, vascular endothelial cells, and nerves H2= stomach H3 = CNS

Question 58

mechanism of antihistamines? Differences between generations?

Answer 58

competitive antagonist for H1 receptor and prevents binding of histamine First Generation = lipophilic and non-selective with anticholinergic effects (ex. anti-emetic) Second Generation = specific to peripheral H receptors

Question 60

clinical use of anti-histamines?

Answer 60

*most effective if taken BEFORE allergen exposure allergic reactions and rhinitis, and first generation are anti-emetic

Question 62

Side effects of anti-histamines?

Answer 62

Anti-cholinergic “mad as a hatter….” GI - nausea and ab pain CNS - sedation and drowsiness

Question 64

common drugs that are anti-histamines?

Answer 64

Diphenhydramine = benedryl Alkylamines = anticholinergic effect so used in cough medicines Promethazine = High sedation and high anti-cholinergic Cetrizine = Zyrtec Loratidine = Clariton Fexofenatidine = Allegra

Question 66

what are the classes of anti-tussives?

Answer 66

1) Opioids 2) Dextromethorphan 3) Benzonatate (Tesslon pearls) 4) Expectorant = Guaifenesin

Question 68

Mechanism of opioids? Dextromethorphan?

Answer 68

[Opioids = used at lower doses than analgesics and so risk of resp distress is low] both: increases threshold to cough in respiratory cough centers in medulla and nucleus tractus solitarous

Question 70

side effects of dextromethorphan?

Answer 70

CNS effects at high doses include confusion, excitation, nervousness, and irritability … can even see respiratory depression at high doses = bc some NMDA receptor antagonist activity DO NOT USE in patients with MAOIs or SSRIs bc can cause Serotonin Syndrome

Question 72

Mechanism of Benzonatate?

Answer 72

anesthetic effect on stretch receptors of vagal afferent fibers in bronchi, alveoli and pleura - blocks cough reflex and stops transmission of signal of cough reflex

Question 74

mechanism, use and side effects of Guaifenesin?

Answer 74

mechanism - loosens and thins lower resp secretions Used for symptomatic relief of productive coughs Side effects - dizziness, N/V, and diarrhea (from sugar its given with)