Anti-Asthma Flashcards
Responsible for processing
the oxygen into the blood
system and exhaling
carbon dioxide
Respiratory System
2 major parts of respiratory system
Upper and Lower
Upper respiratory system comprises of
pharynx to trachea
lower respiratory system includes
lungs to alveoli
Common Respiratory Disorders
-Asthma
-Chronic Obstructive Pulmonary Disorder (COPD)
-Cystic Fibrosis
-Tuberculosis
Episodic narrowing and inflammation of the airway caused by stimuli
Asthma
Chronic bronchitis
Emphysema
Chronic Obstructive Pulmonary Disorder (COPD)
Thick secretion are excreted into the lung
Cystic Fibrosis
Infection caused by Mycobacterium tuberculosis
Tuberculosis
one of its manifestation is having barrel shoulders
COPD
T/F: COPD is irreversible and progressive
T
T/F: We don’t give NSAIDS to
asthmatic patients , We give
inhaled corticosteroid (ICS):
T
prevent asthma episodes
Controller
specifically for asthma attack
Reliever
Drugs used in Asthma
Bronchodilators
Anti-inflammatory agents
Leukotriene antagonist
Beta 2 - agonist
Methylxanthines
Muscarinic
antagonist
Bronchodilators
Release inhibitors
Antibodies
Steroids
Anti-inflammatory agents
Lipoxygenase inhibitor (Zileuton)
Receptor inhibitor (Zafirlukast, Montelukast)
Leukotriene antagonist
- Inflammation of the airways
- Constrictions
Asthma
Treatment of asthma involves:
- Dilation of airway
- Reduction of inflammation
Asthma manifestations
-tightness of chest
-shortness of breath
-wheezing
T/F: Asthma is always a reaction to allergen
T
can cause bronchodilation
B2 agonist
T/F: you should not give non-selective to asthmatic patients, give selective instead
T
Sympathomimetic Agents
Adrenoreceptor agonist
Sympathomimetic Agents stimulates ______________________
and ____________ the formation of
intracellular cAMP
adenylyl cyclase (AC); increases
Sympathomimetic Agents Binds to __________________, stimulating
the cAMP in the smooth muscle,
causing it to __________ and inhibiting
the release of bronchoconstricting
mediators from mast cells.
Binds to beta-receptor; relax
Dilation of the bronchioles
Sympathomimetic Agents
Best delivered by inhalation
Sympathomimetic Agents
more cAMP = _______ bronchodilation
more
Can you give B2 and Theophylline at the same time?
Yes
Rapid-acting bronchodilator when injected subcutaneously or as
inhaled as micro aerosol
Epinephrine
Maximal bronchodilation of epinephrine is achieved __________ minutes after inhalation and
last for ___________ minutes
15; 60 – 90
Epinephrine may cause
Tachycardia
Arrhythmia
Worsening of angina pectoris
May also be used for treating acute vasodilation, shock, and
bronchospasm of anaphylactic shock
Epinephrine
Longer duration of action compared to epinephrine
Ephedrine
A more pronounced central activity and a much lower potency
Ephedrine
Infrequently used in the management of asthma
Ephedrine
Potential non-selective B1 and B2 bronchodilator
Isoproterenol
Micro aerosol from pressurized canister
Isoproterenol
Isoproterenol at ____________ causes bronchodilation within 5 minutes
– 80 – 120 mcg
Rarely used for asthma
Isoproterenol
Albuterol, Terbutaline, Metaproterenol and Pirbuterol
Short Acting Beta -2 Agonist (SABA)
Available as a metered dose inhaler
SABA
Albuterol and Terbutaline are also available in ________ form
oral
Bronchodilation caused by SABA is maximal within ____________ and persistent for _______
15 minutes; 3 – 4
hours
SABA can be diluted in _________ for administration from a hand-held nebulizer
saline
Terbutaline is also available as ______ injection
SQ
Large doses of ____________ may sometimes be used to inhibit uterine
contraction
terbutaline
Salmeterol and Formeterol
LABA
LABA’s Duration of action 12 or more hours as a result of ___________
high lipid solubility
- Need to be taken once daily
- Used for treatment of COPD
Ultra Long-Acting Beta 2 Agonist
Purine derivatives
Methylxanthine
Caffeine, theophylline, theobromine
Methylxanthine
once a mainstay of asthma treatment
Theophylline
Inhibits phosphodiesterase → _________________ concentration of
intracellular cAMP and in some tissues cGMP
increasing
stimulates cardiac function, relaxation of smooth
muscles and reduction in the immune and inflammatory activity
cAMP
Methylxanthine that is;
-Absorbed well in the GI
-Metabolized in the liver
Theophylline
Theophylline dosing iv therapy
3 – 4 mg/kg q 6
Theophylline plasma concentration:
5
– 20 mg/L
Methylxanthine SE:
- Gastrointestinal distress
- Tremor
- Insomnia
MEthylxanthine Toxicities:
- Arrythmia
- Hypotension
- Vomiting
Antidote for methylxanthine
Beta blocker
Datura stramonium
Antimuscarinic Agents
Competitively inhibits the action of acetylcholine at the
muscarinic receptor
Antimuscarinic Agents
Antimuscarinic Agents _____________ (competitively/partially) inhibits the action of acetylcholine at the
muscarinic receptor
competitively
Blocks the contraction of airway smooth muscle and the
increased secretion of mucus
Antimuscarinic Agents
Very high concentrations are required to inhibit the response of
airway smooth muscle to non-muscarinic stimulation.
Antimuscarinic Agents
prototypic muscarinic antagonis
Atropine
SAMA
Ipratropium
Selective quaternary ammonium derivative of atropine
SAMA
Greater bronchodilation with less toxicity from systemic absorption
SAMA
Can be delivered into the circulation and does not readily enter the
CNS
SAMA
T/F: SAMA is as effective as albuterol in patients with COPD
T
Tiotropium, Aclidinium
LAMA
Binds to the M1, M2, and M3 receptors with equal affinity, but
dissociates most rapidly from M2 receptor
LAMA
LAMA dissociates most rapidly from ___________ receptor
M2
LAMA is taken by
inhalation
A single dose of 18 mcg of __________ – 24 hours duration,
Tiotropium
400
mcg of _________ – 12 hours duration thus taken 2x daily
aclidinium
Daily inhalation of ____________ has been shown to improve the
functional capacity of patients with COPD as well as reduce
_____________
Tiotropium; exacerbation frequency
T/F: LAMA is not part of maintenance
medications for patients with Asthma but only given as add ons
T
frequently used corticosteroids
Inhaled corticosteroids
Inhibit phospholipase A2 and COX-2 expression
Corticosteroids
effect of Corticosteroids
Reduce inflammatory cytokines
* The thickness of the respiratory mucosa is reduced
* Does not have an effect on dilation
Used routinely in combination with β agonist
Corticosteroids
Urgent treatment corticosteroid
Prednisolone (oral) - 30 – 60 mg per day or
Methylprednisolone (IV) - 1mg/kg every 6 – 12 hours
Beclomethasone, Budesonide, Ciclesonide, Flunisolide, Fluticasone,
Mometasone, Triamcinolone
Inhalational Corticosteroid (ICS)
minimal systemic absorption
Inhalational Corticosteroid (ICS)
An Average daily dose of ___________________ is equivalent to
10 – 15mg/day of oral prednisolone
800 mcg of Beclomethasone
__________ oral therapy slowly before switching from oral to ICS to avoid
adrenal insufficienc
Taper
commonly occurs in patients using inhaled
topical corticosteroid
Oropharyngeal candidiasis
it inhibits early and later
response to antigen on mast cells and eosinophil
Release Inhibitor
Block bronchoconstriction caused by allergen inhalation,
exercise, sulfur dioxide and variety of causes of occupational
asthma
Release Inhibitor
When taken regularly (2-4 puffs 2-4x daily) it significantly
reduces sympathomimetic severity and the need for
bronchodilator medications particularly in young patients with
allergic asthma
Release Inhibitor
Useful in reducing allergic rhinnoconjunctivitis
Release Inhibitor
Side effects are minor and localized to the site of deposition
Release Inhibitor
Release inhibitor se
- Throat irritation, cough, and mouth dryness
- Rarely, chest tightness and wheezing
- Administering B2 agonist before Cromolyn or Nedocromil treatment
prevents these symptoms
Cromolyn, Nedocromil
Release Inhibitors
- Inhibiting the mast cell and have no direct bronchodilator effect
Cromolyn, Nedocromil
Low solubility and poorly absorbed from the GI tract thus, it must be
inhaled as microfine powder or microfine suspension
Cromolyn, Nedocromil
Has no effect on the airway’s smooth muscle tone and is thus
ineffective in reversing asthmatic bronchospasm but effective in
inhibiting both antigen and exercise-induced asthma
Cromolyn, Nedocromil
from the action of 5-lipoxygenase on arachidonic
acid is synthesized by various inflammatory cells in the airways.
Leukotriene
potent neutrophil chemoattractan
LTB4
exert many effects known to occur in asthma,
including bronchoconstriction, increased bronchial reactivity,
mucosal edema, and mucus hypersecretion
LTC4 and LTD4
Leukotriene Pathway Inhibitor approaches
- Inhibition of 5-lipoxygenase thereby preventing leukotriene synthesis
- Inhibition of the binding of LTD4 to its receptor on target tissue
– lipoxygenase inhibitor
Zileuton
– LTD4 receptor antagonist
Zafrilukast and Montelukast
Leukotriene inhibitor is usually taken
orally
Leukotriene inhibitor that is Approved for children as young as 12 months
- Montelukast
most prescribed leukotriene inhibitor
Montelukast
T/F: Montelukast can be taken without regard to meals
T
Montelukast is taken ______ daily
once
Least prescribed due to liver toxicity
Zileuton
Not as effective as an inhaled steroid
Leukotriene inhibitor
Not recommended for acute asthma
Leukotriene inhibitor
Leukotriene inhibitor is effective in
- Exercise-induced bronchospasm
- Antigen 2induced bronchospasm and aspirin allergy
- Aspirin-induced bronchospasm
Leukotriene inhibitor Toxicity
Generally low
occasional elevation of liver enzyme
Zileuton
Anti-IgE Monoclonal Antibodies
Omalizumab
Humanized murine monoclonal antibody
Omalizumab
Prevents the activation by asthma trigger antigens
Omalizumab
Inhibits the binding of IgE but does not activate IgE already bound to
the mast cells and thus does not provoke mast cell degranulation
Omalizumab
Omalizumab is given ___________ every 2- 4 weeks to asthmatic patients
subcutaneously
Mepolizumab & Reslizumab
Anti-IL5 Therapy
targeting IL- 5 receptor
Benralizumab
T2 cells secrete IL 5 as pro-eosinophilic cytokine, resulting in
_________
eosinophilic airway inflammation
Prevent exacerbation in asthmatic patients with peripheral
eosinophilia, add on maintenance therapy of severe asthma in
patient with an eosinophilic asthma.
Anti-IL5 Therapy