objective 2.3 (2) Flashcards by Kaitlyn Dominie

 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

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 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

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Progressive respiratory disorder
Characterized by chronic airflow limitation, systematic
manifestations, and significant comorbidities

chronic obstructive pulmonary disease

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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

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Relax bronchial smooth muscle, which causes dilation of the
bronchi and bronchioles that are narrowed as a result of the
disease process

bronchodilators

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what three classes of bronchodilators?

 β-adrenergic agonists,
 anticholinergics, and
 xanthine derivatives

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what are short acting B agonist inhalers?

salbutamol (Ventolin®)
Terbutaline sulphate (Bricanyl®)

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what are long acting B agonist inhalers?

formoterol (Foradil®, Oxeze®)
salmeterol (Serevent®)

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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

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what are the 3 subtypes of B-adrenergic agonists?

nonselective adrenergic
nonselective B-adrenergic
selective B2 drugs

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Stimulate ß-, ß1- (cardiac), and ß2- (respiratory) receptors
Example: epinephrine (EpiPen®)

nonselective adrenergic

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Stimulate both ß1- and ß2-receptors
Example: isoproterenol hydrochloride

nonselective B-adrenergic

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Stimulate only ß2-receptors
Example: salbutamol (Ventolin®)

selective B2 drugs

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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.

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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

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what are the contraindications of B-adrenergic agonists?

Known drug allergy
Uncontrolled cardiac dysrhythmias
High risk of hypertension/ stroke

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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)