Asthma/COPD medications Flashcards
Albuterol
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
Salmeterol
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
Formoterol
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
Epinephrine
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
Ipratropium Bromide
- 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
tiotropium
- longer acting muscarinic antagonist
- used for maintenance therapy in chronic bronchitis and emphysema
- dry powder inhaler device
Theophylline
= 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
Beclomethasone
inhaled corticosteroids
Budesonide
**inhaled corticosteroids
Ciclesonide
inhaled corticosteroids
Flunisolide
inhaled corticosteroids
Fluticasone
**inhaled corticosteroids
Mometasone
inhaled corticosteroids
Triamcinolone
inhaled corticosteroids
methylprednisolone
oral corticosteroid
prednisone
oral corticosteroid
montelukast
Luekotriene receptor antagonist (LTRA)
Alternative or adjunctive therapy to low-dose corticosteroids for mild persistent asthma.
Useful as oral prophylaxis in exercise-induced asthma
zafirlukast
Luekotriene receptor antagonist (LTRA)
Cromolyn sodium
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.
Omalizumad
Anti-IgE Antibody
degranulation from mast cells?
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 )
histamine, TNFalpha, proteases, heparin
immediate mediators that cause bronchoconstriction, cough, vasodilation, edema
Luekotrienes/Prostaglandins
ex. Motelukast
lipids releaesed in minutes that cause bronchoconstriction , chemotaxis, mucus secretion
Interleukins, GM-CSF
cytokines that are released in hours that cause bronchoconstriction, chemotaxis, inflamm. cell proliferation
what is the stepwise tx that increases with severity?
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
Beta adrenergic agonists
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
Long term use of LABA
***** 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”.
SE of Beta adrenergic Agonists?
*** 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))
Combivnet
Albuterol + Ipratropium bromide
- used in COPD and severe asthma
Anaphylaxis tx?
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
Corticosteroids
- 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
what is used most to tx patients with COPD?
- 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.
