Asthma/COPD medications

Question 1

Albuterol

Answer 1

SABA** this is drug of choice in tx of asthma

used as a rescue inhaler, onset is <15 minutes - they are fast acting but have a relatively short duration of action

Question 2

Salmeterol

Answer 2

LABA

• slower onset, duration >12 hours of bronchodilation
• useful for nighttime asthma attacks
• NOT suitable for tx of acute bronchospastic attacks because onset of action is too slow

*** LABA should be used in asthma only in combination with inhaled corticosteroid

Question 3

Formoterol

Answer 3

LABA

• slower onset, duration >12 hours of bronchodilation
• useful for nighttime asthma attacks
• NOT suitable for tx of acute bronchospastic attacks because onset of action is too slow

*** LABA should be used in asthma only in combination with inhaled corticosteroid

Question 4

Epinephrine

Answer 4

non-selective Beta agonist used in times of emergency

** Epinephrine is the drug of choice for treatment of anaphylactic reactions.
Give SQ

• Causes bronchodilation via B2, vasoconstriction via alpha1 (maintains BP and decreased edema), inhibition of mediator release via B2

Question 5

Ipratropium Bromide

Answer 5

• a quaternary muscarinic antagonist, drug of choice with COPD**
• only give as *inhaled aerosol** (few SE’s when swallowed b/c its poorly absorbed, quaternary amine does not diffuse across membranes)

Parasympathetic - mediated bronchospasm is a significant component of airway resistance in some asthmatics and COPD patients, especially *psychogenic exacerbations]

Therapeutic use:

• see greater amount of bronchodilation that beta agonists: thus used for COPD
• also used for allergic rhinitis and chronic postnasal drip syndrome

Question 6

tiotropium

Answer 6

• longer acting muscarinic antagonist
• used for maintenance therapy in chronic bronchitis and emphysema
• dry powder inhaler device

Question 7

Theophylline

Answer 7

= it is a methylxanthine

• bronchodilator - used to be main stay of tx to treat COPD, formerly a fist-line agent for tx of asthma (now has been replaced to low benefit, narrow therpuetic window)
• still used for nocturnal asthma with slow release formula (but corticosteroids and salmeterol are probably more effective)

Other effects: CNS stimulation, modest peripheral vasodilation, improved skeletal muscle contractility, and a thiazide-like diuresis

** know its drug/drug interactions, and that it is dosing related SE’s

Question 8

Beclomethasone

Answer 8

inhaled corticosteroids

Question 9

Budesonide

Answer 9

**inhaled corticosteroids

Question 10

Ciclesonide

Answer 10

inhaled corticosteroids

Question 11

Flunisolide

Answer 11

inhaled corticosteroids

Question 12

Fluticasone

Answer 12

**inhaled corticosteroids

Question 13

Mometasone

Answer 13

inhaled corticosteroids

Question 14

Triamcinolone

Answer 14

inhaled corticosteroids

Question 15

methylprednisolone

Answer 15

oral corticosteroid

Question 16

prednisone

Answer 16

oral corticosteroid

Question 17

montelukast

Answer 17

Luekotriene receptor antagonist (LTRA)

Alternative or adjunctive therapy to low-dose corticosteroids for mild persistent asthma.

Useful as oral prophylaxis in exercise-induced asthma

Question 18

zafirlukast

Answer 18

Luekotriene receptor antagonist (LTRA)

Question 19

Cromolyn sodium

Answer 19

Cromolyn compound= anti-inflammatory agent that indirectly inhibits antigen-induced bronchospasm and directly inhibits the release of histamine and other autocoids from sensitized mast cells.

• *** do not directly relax smooth muscle, therefore they are not useful for control of acute bronchospasm.
• • Cromolyn compounds are primarily prophylactic - . When inhaled several times daily, they inhibit both the immediate and late asthmatic responses to antigenic challenge or exercise.
• May suppress the activating effects of chemoattractant peptides on eosinophils, neutrophils, and monocytes.

Question 20

Omalizumad

Answer 20

Anti-IgE Antibody

Question 21

degranulation from mast cells?

Answer 21

histamine, kinins, leukotrienes (SRS), prostaglandins, serotonin, PAF

• see that there are so many things released: the corticosteroids suppress inflammation at this level (rather than antihistamines which only act on one mediator )

Question 22

histamine, TNFalpha, proteases, heparin

Answer 22

immediate mediators that cause bronchoconstriction, cough, vasodilation, edema

Question 23

Luekotrienes/Prostaglandins

Answer 23

ex. Motelukast

lipids releaesed in minutes that cause bronchoconstriction , chemotaxis, mucus secretion

Question 24

Interleukins, GM-CSF

Answer 24

cytokines that are released in hours that cause bronchoconstriction, chemotaxis, inflamm. cell proliferation

Question 25

what is the stepwise tx that increases with severity?

Answer 25

Mild: SABA PRN, ie. albuterol Mild +: Low dose ICS Moderate: ICS + LABA i.e. Formoterol/Salmeterol Severe: high dose ICS + LABA Very Severe: high dose ICS + LABA + oral corticosteroid they still have a SABA, short acting, because the corticosteroid is not good for immediate acting

Question 26

Beta adrenergic agonists

Answer 26

Albuterol (SABA), Formoterol, Salmeterol (LABA) Uses: - drug of choice for rapid relief of bronchospasm - Highly effective and safe for intermittent, prophylactic treatment of asthma. - Intermittent use on an as-needed basis for relief of acute, severe bronchospasm. Not general prophylaxis. Overuse: - Side effects intensify will overuse, but a greater danger is the tendency to continue to self-medicate during periods when symptoms are escalating. - To avoid a medical emergency, patients should be encouraged to seek medical attention as soon as possible after they detect a decline in the efficacy of their usual therapeutic regimen. MOA: - Beta2-adrenergic receptor couples to Gs protein and activates adenylyl cyclase enzyme leading to increased cellular levels of cyclic AMP. Cyclic AMP stimulates phosphorylation cascade that leads to decreased intracellular calcium and smooth muscle relaxation. Oral therapy: - Oral administration increases incidence of adverse side effects: muscle tremor, cramps, cardiac tachyarrhythmias, metabolic disturbances, hypokalemia - Appropriate situations for oral therapy: brief therapy in children with upper respiratory tract infections who cannot manipulate inhaler or in severe asthma exacerbations where inhaler cannot be used or when aerosol is irritating

Question 27

Long term use of LABA

Answer 27

***** LABA should be used in asthma only in combination with an inhaled corticosteroid. Continued use of a LABA may cause down-regulation of b2 receptors with loss of the protective effect from rescue therapy with a short-acting agent. LABA should not be used for monotherapy in patients with persistent asthma, especially in children. Stop use of a LABA, if possible, once asthma control is achieved and maintain the use of an asthma-controller medication such as an inhaled corticosteroid”.

Question 28

SE of Beta adrenergic Agonists?

Answer 28

*** Patients with cardiovascular disease or diabetes are at higher risk of adverse effects. **** Skeletal muscle tremor (most frequent side effect) CVS: ***tachycardia, dysrhythmias, hyper- or hypotension (see tachycardia from hypotension caused by Beta2, and in high doses will actually stimulate Beta1) ((hypokalemia, worsen hyperglycemia in diabetics, CNS: restlessness, apprehension, anxiety, tremors, drug interactions with thyroid, digitalis, methylxanthines))

Question 29

Combivnet

Answer 29

Albuterol + Ipratropium bromide - used in COPD and severe asthma

Question 30

Anaphylaxis tx?

Answer 30

starts with epi ``` Albuterol via nebulizer IV fluids Oxygen Secondary therapy H1 antagonist - diphenhydramine H2 antagonist - ranitidine Corticosteroid - hydrocortisone, methylprednisolone Aminophylline NE, glucagon - for hypotension ```

Question 31

Corticosteroids

Answer 31

- block the steps involved in the inflammatory cascade and used In asthma (and some COPD) MOA: general anti-inflammatory response, steroid receptor agonists that bind to intracellular receptors and regulate gene txn --> thus this takes time to build up SE's: aerosol delivery has greatly improved the safety of this tx. ** Asthmatics who require inhaled beta-adrenergic agonist therapy 3 - 4 or more times weekly are candidates for inhaled steroid therapy: asthmatic patients maintained on inhaled corticosteroids show improvement of sx and lower requirements for "rescue" with a bronchodilator Potential SE's: HPA suppression - low risks until high doses Bone resorption - modest risks Carbohydrate and lipid - minor risks Cataracts and skin thinning - dose-related Purpura - dose-related Dysphonia - usually resolves Candidiasis - use spacer device and rinse mouth **Growth retardation - of concern in children

Question 32

what is used most to tx patients with COPD?

Answer 32

- Inhaled ipratropium bromide or tiotropium- especially useful in patients with a vagally-mediated psychogenic component. - Inhaled beta2-adrenergic agonists- As with asthma, continuous (overuse) of bronchodilators may be associated with worsening of symptoms. - A subgroup of COPD patients may benefit from corticosteroid therapy, but generally mixed results of steroids in COPD.