Respiratory Drugs Flashcards
Cromolyn Sodium: Mechanism of Action
Inhibits Mast cell degranulation
Theophylline: Mechanism of Action
Adenosine receptor antagonist, PDE inh
Albuterol: Mechanism of Action
Beta-2 adrenergic receptor agonist (short acting)
Salmeterol: Mechanism of Action
Beta-2 adrenergic receptor agonist (long acting)
Ipratropium: Mechanism of Action
Muscarinic antagonist
Fluticasone: Mechanism of Action
Inhaled corticosteroid
Prednisone: Mechanism of Action
Systemic corticosteroid
Montelukast: Mechanism of Action
Leukotriene receptor antagonist
Zileuton: Mechanism of Action
5-Lipoxygenase inhibitor
Which drugs are antiinflammatory?
(1) Fluticasone
(2) Prednisone
(3) Montelukast
(4) Zileuton
What drugs reverse bronchoconstriction?
(1) Theophylline
(2) Albuterol
(3) Salmeterol
(4) Ipratropium
What drugs inhibit mast cell degranulation (good as a phrophylaxis)?
(1) Cromolyn
What are the treatment goals of respiratory drugs?
(1) To reverse acute episodes
(2) To control recurrent episodes
(3) To reduce bronchial inflammation
What are released in asthma attacks? What do they do?
Autocoids; produce bronchoconstriction and increase vascular permeability in bronchi and cause mucosal edema (histamines, leukotrienes, adenosine)
What is bronchial tone innervated by?
Autonomic nervous system; Adrenergic(alpha-constriction; beta-dilation) and Cholinergic (muscarinic-constriction)
What types of drugs are bronchodilators? What do they do?
(1) Beta-adrenergic agonists- relax bronchial smooth muscle and decrease microvascular permeability
(2) Muscarinic antagonists- inhibit the effects of endogenous ACh
(3) Theophylline- reduces the frequency of recurrent bronchospasm
What types of drugs are non-bronchodilators?
(1) Corticosteroids- control mucus production and edema
(2) Cromolyn- controls mediator response
(3) Leukotriene modulators- antagonize mediator receptors or decrease their synthesis
What are the most effective bronchodilators?
Beta-adrenergic agonists
How are beta-adrenergic agonists given? Why?
Inhalation; to avoid systemic effects
What are the 2 beta-adrenergic agonists and which is slow/fast acting? Which is number 1 drug during acute asthma attack? Which is used for maintenance treatment?
(1) Albuterol- FAST (3-6 hr); ACUTE
(2) Salmeterol- LONG (>12 hr); MAINTENANCE
What drugs are useful in prevention of exercise-induced asthma?
Beta-adrenergic agonists
What may happen with continuous use of beta-adrenergic agonists? How can you combat this?
Patient may result in desensitization of adrenergic receptors; prevented or reversed by using corticosteroids
What may happen in high doses of beta-adrenergic agonists?
Tachycardia, palpitations, tremor (more systemic effects)
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| What type of drug is Ipratropium? What is it a synthetic analog of?</p>
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| A muscarinic receptor antagonist; synthetic analog of atropine</p>
T/F Ipratroprium has some anti-inflammatory activity.
FALSE
When is Ipratroprium used?
(1) In COPD to decrease cholinergic tone
(2) In asthma in combination with beta-adrenergic agonists- Different mechanism of action!
How is Ipratroprium given?
Inhaled (has negligible side effects)
T/F Ipratroprium is a weak bronchodilator and inhibitor of airway secretory glands.
TRUE
Why do you use Ipratroprium with Beta-adrenergic agonists?
The combination is more effective and less toxic than either drug alone (can use lower doses of each)
What drug is a methylxanthine? What are some other examples of this?
Theophylline; Caffeine, theo bromine (found in chocolate)
What does Theophylline do?
Relaxes smooth muscles of the body, especially if bronchi have been constricted by a spasmogen as in asthma
How is Theophylline given?
Orally, it is ineffective by aerosol
What are the 2 different mechanisms Theophylline works in?
(1) Adenoside receptor blockade
(2) Phosphodiesterase inhibition
When is Theophylline used?
In chronic asthma
Which drug is more effect and faster? Theophylline or beta-adrenergic agonists?
Beta-adrenergic agonists
What are the mild, potentially serious, and severe toxicities within Theophylline?
(1) Mild (30mg/L)- nausea, vomiting, headache, insomnia, and nervousness
(2) Potentially serious- sinus tachycardia
(3) Severe- cardiac arrythmias, seizures
Why does Theophylline need to be monitored?
It has a clearance variability with a narrow safety index (10-20 mg/L); clearance is influenced by smoking and other drugs metabolized in the liver
What are Fluticasone’s 2 mechanisms of action?
(1) Block release of arachidonic acid and it’s metabolites (leukotrienes)
(2) Inhibits production of pro-inflammatory cytokines
When is Fluticasone used?
In chronic asthma, lowers the frequency of acute episodes
What is the most important part of the arachidonic acid synthesis?
Leukotrienes
Fluticasone- Adverse effects?
Dysphonia and/or esophageal candidiasis
What are the most effective drugs for asthma unresponsive to bronchodilators and inhaled steroids?
Oral or injected Prednisone
How long do you want to continue Prednisone after recovery from exacerbation? How would you continue use?
8-10 days; every other day to decrease side effects
Prednisone- Adverse Effects
glucose intolerance, sodium and water retention, increased BP, peptic ulcer, immunosuppression, etc.
What is Cromolyn Sodium useful for?
Prophylaxis; it stabilizes mast cells and decreases airway responsiveness to spasmogens (if you’re having an asthma attack, the mast cells have already degranulated)
What population is Cromolyn Sodium effective for?
Children and adolescents
When does the Cromolyn become effective? (How long do you have to take it?)
After 4-6 weeks of treatment
T/F Cromolyn Sodium does not have any bronchodilating activity.
TRUE
Cromolyn Sodium- Adverse Effects
Virtually no toxicity!
What are the 2 types of Leukotriene modulators? Which drugs go with each?
(1) Inhibitors of LT synthesis- block the production: Zileuton
(2) LT receptor (LTD4) antagonists- block the response to leukotrienes: Montelukast
What are leukotriene modulators used for?
Maintenance therapy; they reduce frequency of acute episodes; useful in children in chronic treatment of mild to moderate asthma
Zileuton: Drug Interactions
- It can elevate liver enzymes and increases the concentrations of theophylline and warfarin because it inhibits P450 in the liver
Which are more effective antiinflammatory agents? Corticosteroids, Leukotriene modulators?
Corticosteroids
How are Leukotriene modulators given?
Orally
Why do asthmatics have severe response to ASA sometimes?
because ASA inhibits cyclooxygenase which is part of the arachidonic pathway
