Respiratory: B2RAs Flashcards
Types of Respiratory Drugs:
Bronchodilators: Beta2-Receptor Agonists:
Basic Understanding:
Abbreviation for Beta2-Receptor Agonists
B2RAs
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Basic Understanding:
Are Bronchodilators widely used?
Yes
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Basic Understanding:
What population uses B2RAs?
All ages
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Basic Understanding:
What are B2RAs used to treat?
Reversible bronchoconstriction caused by:
1. Asthma
2. Reactive airway disease
RAD
3. COPD
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Basic Understanding:
Are many types of B2RAs available?
If so, what types are there?
Yes
- Many forms
- Many delivery systems
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Examples:
What are the categories of B2RAs needed to know for the Quiz?
What are the categories we need to know exist but do not need to memorize for the quiz?
- Most commonly prescribed
2. Other sympathomimetic B2RA medications
Types of Respiratory Drugs:
Bronchodilators:B2RAs:
Examples:
What are the Most commonly prescribed drug in this class?
INN/Generic Name?
Brand/Trade Names?
INN/Generic Name:
- Albuterol or salbutamol
Brand/Trade Names:
- ProAir
- Ventolin
- Proventil
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Examples:
What are the other sympathomimetic B2RAs medication categories?
- Short Acting
2. Long Acting
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Examples:
DO NOT NEED TO KNOW FOR QUIZ
What are examples of Short Acting B2RAs?
- metaproterenol (Alupent)
- terbutaline (Brethine, Brethaire)
- bitolterol (Tornalate)
- pirbuterol (Maxair)
- levalbuterol (Xopenex)
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Examples:
DO NOT NEED TO KNOW FOR QUIZ
What are examples of Long Acting B2RAs?
- arformoterol (Brovana)
- formoterol (Foradil)
- indacaterol (Arcapta)
- salmeterol (Serevent).
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What type of tissue do B2RAs act on?
Muscle
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics
What type of muscle do B2RAs act on?
Smooth muscle
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What type of smooth muscles does Albuterol act on to achieve target effect?
Bronchial tree smooth muscle
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Where are the smooth
What do B2RAs stimulate the smooth muscles in the bronchial tree to do?
Reverse bronchospasm
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Reversal of bronchospasm of B2RAs is achieved by decreasing __1___ / __2___ and increasing __3___/__4___.
- Airway resistance
- Residual volume
- Vital capacity
- Airflow
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Physiology/Dynamics of B2RAs
- Stimulate beta2 adrenergic receptors in the lungs which
- Activates adenyl cyclase (enzyme that converts ATP) which
- Increases production of cyclic adenosine monophosphate
(cAMP) - Increased cAMP
- relaxes muscles
- inhibits release of mediators of immediate hypersensitivity from cells (esp. mast cells)
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What would the perfect B2RA do?
Work only on the beta 2 receptors in the lungs
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Are B2RAs perfect?
Why or why not?
No
All of the currently available B2RA preparations
have some effects on other body systems
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Is Albuterol selective or non selective?
Selective
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What does Albuterol effect in order to categorize it as a selective B2RA?
- Beta2 agonist
2. Some minor beta1 activity
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Other than beta 2 receptors found on the smooth muscle in the lungs, what other type of smooth muscle beta 2 receptors are stimulated when using Albuterol?
CNS and..
Smooth Muscle:
- Vascular
- Skeletal
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Which beta 2 receptors on vascular smooth muscle are stimulated when using Albuterol?
Cardiac beta2 receptors
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Stimulation of the cardiac beta2 receptors causes what to happen when using Albuterol?
- Vasodilation
2. Decrease in diastolic blood pressure
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What does vasodilation and a decrease in diastolic blood pressure caused by the stimulation of cardiac beta2 receptors when using Albuterol cause to occur?
Reflex increased HR
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What must be achieved when using Albuterol to cause Reflex increased HR?
High serum levels of Albuterol
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Why are high serum levels of Albuterol needed to cause increased HR?
- Albuterol has a low affinity for cardiac beta2 receptors
2. Fewer beta2 receptors than beta1 receptors in the heart
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
When beta 2 receptors on skeletal smooth muscle are stimulated by Albuterol what occurs?
Tremors
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
Compared to other agonists does Albuterol have less or more effects on the cardiac system and the CNS?
Fewer effects
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What line of therapy is Albuterol considered (first, second, etc…)?
First line
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacodynamics:
What contributes to Albuterol being considered first line therapy?
Fewer cardiac and CNS effects
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Absorption and Distribution:
How is Albuterol most commonly administered?
Inhaled
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Absorption and Distribution:
Other than inhaled Albuterol, in which other way can Albuterol be administered?
Orally
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Absorption and Distribution:
Where is inhaled Albuterol absorbed?
In the bronchi
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Absorption and Distribution:
Where is oral Albuterol absorbed?
- In the GI tract where is reaches the
- Bloodstream which
- Widely distributes it
in body fluids and tissues
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Absorption and Distribution:
Which variation of albuterol is formulated to be absorbed more slowly?
Extended-release oral albuterol
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Absorption and Distribution:
Does Albuterol excrete into breast milk?
It is unknown
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
Where is Albuterol metabolized?
Hepatic/Liver
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
How is Albuterol Excreted?
- Renal/Urine
2. Fecal
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
What is Albuterol metabolized into?
Albuterol 49-O-sulfate
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
What effect does albuterol 49-O-sulfate have?
- Little or no beta adrenergic–stimulating effect
2. No beta adrenergic–blocking effect
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
How much inhaled Albuterol is excreted in urine within 24 hours of inhalation?
Approximately 72%
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
In what forms is inhaled Albuterol excreted in urine within 24 hours of inhalation?
- 28% unchanged drug
2. 44% metabolite
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
How much inhaled Albuterol is excreted in feces within 24 hours of inhalation?
Approximately 10%
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
How much oral Albuterol is excreted in urine within 24 hours of taking it?
The majority
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
How much oral Albuterol is excreted in urine within 3 days of taking it?
65%-90%
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacokinetics: Metabolism and Excretion:
How much oral Albuterol is excreted in feces?
About 4%
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacotherapeutics: Precautions and Contraindications:
Do B2RAs have many contraindications to use?
Relatively few
Types of Respiratory Drugs:
Bronchodilators: B2RAs:
Pharmacotherapeutics: Precautions and Contraindications:
What are the contraindications of use with B2RAs?
Patients with cardiac arrhythmias associated with tachycardia or heart block caused by:
- Digitalis intoxication
- Angina
- Narrow-angle glaucoma
- Organic brain damage (epinephrine only)
- Shock during general anesthesia with halogenated agents