objective 2.3 (2) Flashcards
A sudden and dramatic onset is referred to as an asthma attack.
Prolonged asthma attack that does not respond to typical drug therapy is
known as status asthmaticus
asthma
Recurrent and reversible shortness of breath
The airways of the lungs become narrow as a result of:
Bronchospasms, Inflammation and edema of the bronchial mucosa,Production of viscous
mucus
The alveolar ducts and alveoli remain open, but airflow to them is obstructed
bronchial asthma
Progressive respiratory disorder
Characterized by chronic airflow limitation, systematic
manifestations, and significant comorbidities
chronic obstructive pulmonary disease
Presence of cough and sputum for at least 3 months in each of 2
consecutive years
Separate disease from chronic obstructive pulmonary disease
chronic bronchitis
Relax bronchial smooth muscle, which causes dilation of the
bronchi and bronchioles that are narrowed as a result of the
disease process
bronchodilators
what three classes of bronchodilators?
β-adrenergic agonists,
anticholinergics, and
xanthine derivatives
what are short acting B agonist inhalers?
salbutamol (Ventolin®)
Terbutaline sulphate (Bricanyl®)
what are long acting B agonist inhalers?
formoterol (Foradil®, Oxeze®)
salmeterol (Serevent®)
what are the long acting B agonist and glucocorticoid steroid combo inhaler?
budesonide/formoterol fumarate dihydrate (Symbicort®)
Use as a reliever or rescue treatment for moderate to severe asthma when
symptoms worsen
what are the 3 subtypes of B-adrenergic agonists?
nonselective adrenergic
nonselective B-adrenergic
selective B2 drugs
Stimulate ß-, ß1- (cardiac), and ß2- (respiratory) receptors
Example: epinephrine (EpiPen®)
nonselective adrenergic
Stimulate both ß1- and ß2-receptors
Example: isoproterenol hydrochloride
nonselective B-adrenergic
Stimulate only ß2-receptors
Example: salbutamol (Ventolin®)
selective B2 drugs
what is the MOA of B-adrenergic agonists?
Used during acute phase of asthmatic attacks
Quickly reduce airway constriction and restore normal airflow
Agonists, or stimulators, of the adrenergic receptors in the sympathetic
nervous system
Sympathomimetics bronchodilators– relax smooth muscle and inhibit inflammatory
response.
what are the indications of B-adrenergic agonists
Relief of bronchospasm (asthma, chronic obstructive pulmonary disease
(COPD), and other pulmonary diseases)
Treatment and prevention of acute attacks
what are the contraindications of B-adrenergic agonists?
Known drug allergy
Uncontrolled cardiac dysrhythmias
High risk of hypertension/ stroke
what are the AE of B-adrenergic agonists?
α and ß (epinephrine): Insomnia, Restlessness, Anorexia, Vascular headache,
Hyperglycemia, Tremor, Cardiac stimulation
ß1 and ß2 : Cardiac stimulation, tachycardia, Tremor, Anginal pain, Vascular headache
ß2 (salbutamol): Hypotension or hypertension, Vascular headache, Tremor
what are the interactions of B-adrenergic agonists?
Diminished bronchodilation when nonselective ß-blockers are used
with the ß-agonist bronchodilators
Monoamine oxidase inhibitors
Sympathomimetics
Monitor patients with diabetes; an increase in blood glucose levels
can occur.
Short-acting ß2-specific bronchodilating ß-agonist
Most commonly used drug in this class
Don’t exceed max. daily dosage.
Oral, parenteral, and inhalational use
Inhalational dosage forms include metered-dose inhalers as well as solutions for
inhalation (aerosol nebulizers)
salbutamol sulphate
Long-acting ß2-agonist bronchodilator
Never to be used alone but in combination with an inhaled glucocorticoid steroid
Used for the maintenance treatment of asthma and COPD; salmeterol maximum daily
dose (one puff twice daily) should not be exceeded.
salmeterol
what is the MOA of anticholinergics?
Acetylcholine (ACh) causes bronchial constriction and narrowing of the
airways.
Anticholinergics bind to the ACh receptors, preventing ACh from binding.
Result: bronchoconstriction is prevented, airways dilate
what are the AE of anticholinergics?
Dry mouth or throat, Nasal congestion, Heart palpitations, Gastrointestinal
distress, Urinary retention, Increased intraocular pressure, Headache,
Coughing, Anxiety
Oldest and most commonly used anticholinergic bronchodilator
Available both as a liquid aerosol for inhalation and as a multidose inhaler
Usually dose 2 puffs tid-qid
Child (5-12 years)125-250mcg /puff
Adult: 250-500mcg/ puff
ipratropium bromide
Indirectly cause airway relaxation and dilation
Help reduce secretions in COPD patients
Indications: prevention of the bronchospasm associated with COPD; not for the
management of acute symptoms
ipratropium, tiotropium bromide monohydrate
theophylline and caffeine are currently used clinically
plant alkaloids
what is action of xanthine derivatives?
smooth muscle relaxation, bronchodilation, and increased
airflow
what are the indications of xanthine derivatives?
Dilation of airways in asthmas and COPD
Mild to moderate cases of acute asthma
Not for management of acute asthma attack
Adjunct drug in the management of COPD
Not used as frequently because of potential for drug interactions and
variables related to drug levels in the blood
what are the contraindications of xanthine derivatives?
Known drug allergy, Uncontrolled cardiac dysthymias, Seizure
disorders, Hyperthyroidism, Peptic ulcers
what are the AE of xanthine derivatives?
Nausea, vomiting, anorexia
Gastroesophageal reflux during sleep
Sinus tachycardia, extrasystole, palpitations, ventricular dysrhythmias
Transient increased urination
Hyperglycemia
Most commonly used xanthine derivative
Oral and injectable (as aminophylline) dosage forms
Aminophylline: intravenous (IV) treatment of patients with status asthmaticus
who have not responded to fast-acting ß-agonists such as epinephrine
Body weight is used to calculate dosage
theophylline
Used without prescription as a central nervous system stimulant or analeptic to
promote alertness (e.g., for long-duration driving or studying)
Cardiac stimulant in infants with bradycardia
Enhancement of respiratory drive in infants in NICUs
caffeine
Newer class of asthma medications
Nonbronchodilating
Currently available drugs: montelukast (Singulair®), zafirlukast (Accolate®)
leukotriene receptor antagonists
what is the MOA of leukotriene receptor antagonists?
Leukotrienes are substances released when a trigger, such as cat hair or
dust, starts a series of chemical reactions in the body and cause
inflammation, bronchoconstriction, and mucus production.
Result: coughing, wheezing, shortness of breath
Leukotriene receptor antagonists prevent leukotrienes from attaching to
receptors on cells in the lungs and in circulation.
Inflammation in the lungs is blocked, and asthma symptoms are relieved.
what are the indications of leukotriene receptor antagonists?
Prophylaxis and long-term treatment and prevention of asthma in adults and children
Montelukast safe in children 2 years of age and older; Zafirlukast safe in children 12 years of age and
older
Not meant for management of acute asthmatic attacks
Montelukast is also approved for treatment of allergic rhinitis
Improvement with their use is typically seen in about 1 week
what are the contraindications of leukotriene receptor antagonists?
Known drug allergy, Previous adverse drug reaction
Allergy to povidone, lactose, titanium dioxide, or cellulose derivatives—important to note
because these are inactive ingredients in these drugs
Usage may lead to liver dysfunction.
Anti-inflammatory properties, Used in treatment of pulmonary diseases
Oral or inhaled forms, may be administered intravenously
Inhaled forms reduce systemic effects.
May take several weeks before full effects are seen
corticosteroids
what is the MOA of corticosteroids?
Stabilize membranes of cells that release harmful broncho constricting
substances
These cells are called leukocytes (white blood cells).
Increase responsiveness of bronchial smooth muscle to ß-adrenergic
stimulation
Dual effect of both reducing inflammation and enhancing the activity of ß-
agonists
what are the indications of inhaled corticosteroids?
Primary treatment of bronchospastic disorders to control the
inflammatory responses that are believed to be the cause of these
disorders
Persistent asthma
Often used concurrently with the ß-adrenergic agonists
Systemic corticosteroids are generally used only to treat acute
exacerbations or severe asthma.
IV corticosteroids: acute exacerbation of asthma or other COPD
what are the contraindications of inhaled corticosteroids?
Drug allergy, Not intended as sole therapy for acute asthma attacks, Hypersensitivity to
glucocorticoids, Patients whose sputum tests are positive for Candida organisms ,
Patients with systemic fungal infection
what are the AE of inhaled corticosteroids?
Pharyngeal irritation, Coughing, Dry mouth, Oral fungal infections
Systemic effects are rare because low doses are used for inhalation therapy
what are the interactions of inhaled corticosteroids?
Drug interactions are more likely to occur with systemic (versus inhaled) corticosteroids.
May increase serum glucose levels, possibly requiring adjustments in dosages of antidiabetic drugs
May raise the blood levels of the immunosuppressants cyclosporine and tacrolimus; itraconazole may
reduce clearance of the steroids
phenytoin, phenobarbital, and rifampin
Greater risk of hypokalemia with concurrent diuretic use (e.g., furosemide, hydrochlorothiazide)
