Lesson 1: Adrenergic Bronchodilators, Anticholinergics & Xanthines Flashcards
Binds to a receptor and produces a physiological response
Agonist
Binds to a receptor and does NOT produce a physiological response
Antagonist
What is a adrenergic bronchodialator
Drug that stimulates the sympathetic nervous system
What effect does a adrenergic bronchodilator cause
Smooth muscle relaxation
Sympathomimetic is another word for….
Adrenergic
Indication for use of adrenergic bronchodilators is
Reversible airflow obstruction
a- receptor stimulation
-Location
-Action
Location: Pulmonary and bronchial blood vessles
Action: Vasoconstriction effect
B1- Receptor stimulation
-Location
-Action
Location: Heart
Action: Increased HR and contractile force
B2- Receptor stimulation
-Location
-Action
Location: Bronchial smooth muscle, pulmonary and bronchial blood vessles
Action: bronchodilator, vasodialation
Sympathomimetic bronchodilators are this or derivatives of this
Catecholamines
Catecholamines mimic what neurotransmitter
Epinephrine (fight or flight)
Catecholamine symptoms
Tachycardia
Elevated BP
Smooth muscle relaxation
Skeletal muscle tremor
CNS stimulation
Stereoisomers are
Non-superimposable molecular mirror images
2 types:
(R)-Isomer (right isomer)
(S)-Isomer (left isomer)
These have similar physical and chemical properties but different physiological effects
Stereoisomers
If a drug contains a equal amount of both left and right isomers it is…
Racemic
What is the racemic version of levalbuterol
Albuterol
What are the ultra short acting B2 bronchodilators
Epinephrine and Racemic Epinephrine
What is the duration of a ultra short acting B2 bronchodilators
Less than 3 hours
Epinephrine:
-Brand name
-MDI brand name
-Routes of admin
Brand name: Adrenaline Chloride
MDI Brand name: Primatene Mist
Routes of Admin: SVN, MDI, IV, IO, IM
When to use epinephrine
Cardiac stimulant, anaphylactic reactions, acute asthma
What is the onset of epinephrine
Approx. 3 min
Racemic epinephrine
-Brand name
-Route of admin
-Use
Brand name: asthmanefrin
Route of admin: SVN
Use: reduce swelling in upper airways (croup and epiglottitis) and tx of bleeding during bronchs
What is the keyhole theory
Theory that explains the B2 specificity of sympathomimetic bronchodilators
SABA is used for
Relief of reversible acute airway obstructions
LABA is used for
Maintenance bronchodilation, nocturnal symptoms for asthma and COPD
SABA duration
LABA duration
SABA: 4-6 hrs
LABA: 12-24 hrs
What are the 3 types of SABAs
Albuterol
Levalbuterol
Metaproterenol
What are the 5 types of LABAs
Salmeterol : Severent Diskus
Formoterol: Perforomist
Arformeterol: Brovana
Indacaterol: Arcapta Neohaler
Olodaterol: Stiverdi-Respimat
Where in the national asthma guidelines is a LABA reccomended?
Step 3
Stimulation of a and b receptors causes what response?
Adrenergic response
What types of receptors are types of G protein liked receptors?
a and b
Increase in cAMP is the goal of ________, through the stimulus of _________, causing __________.
Adrenergic bronchodilators, B2 receptors, bronchodilation
The difference of how SABAs and LABAs work is due to what?
How the drug binds to the G-protein linked receptor
When giving high doses of albuterol, what should you monitor?
Heart rate, glucose, potassium
What happens to a patients glucose or potassium with high doses of albuterol?
Glucose: levels may increase bc of the fight or flight response that albuterol gives. More energy is needed during FoF, so if the pt isn’t expending that energy it can lead to hyperglycemia
Potassium: levels may decrease bc albuterol stimulates the Na/K/ATPase pump cause of shift of potassium from serum into the intracellular space.
What are the two cholinergic receptors?
Muscarinic and Nicotinic
Stimulation of what receptors cause activation of the parasympathetic system?
Muscarinic and Nicotinic
What is the neurotransmitter for the parasympathetic system?
Acetylcholine
3 main muscarinic receptors
M1, M2, M3 are found in the lung
What are the muscarinic receptors (M1, M2, M3) found
M1 receptors: are present at the parasympathetic ganglion on the post junctional membrane
M2 receptors: are localized at the presynaptic membrane of postganglionic parasympathetic nerve endings
M3 receptors: are found on submucosal glands and airway smooth muscle
How do anticholingerics cause bronchodilation
By blocking the M1 receptors at the parasympathetic ganglia, which facilitates neurotransmission to M3, which cause bronchoconstriction
Bronchodilation will only occur if the bronchoconstriction is due to cholinergic activity
Duration of action for anticholinergics
Atrovent: 6 hrs
Others: 12 or 24 hrs
What common allergen is used in Atrovent HFA and Combivent Respimat (inhaler version of Atrovent)?
Soy lecithin
Umeclidinium bromide and vilanterol
Brand name and duration
Anoro Ellipta
24 hrs
Glycopyrrolate bromide and formoterol
Brand name and duration
Bevespi Aerosphere
12 hrs
Glycopyrrolate bromide and indacaterol
Brand name and duration
Utibron neohaler
12 hrs
What is atropine used for
Anticholinergic used for bradycardia
What is the dose of atropine
1 mg IV push with epi or vasopressin
What is the parasympathomimetic drug we use in the bronchial challenge test
Methacholine
What is methacholine used to do
promote bronchoconstriction to diagnose asthma
What is edrophonium
Drug used for the Tensilon Test to diagnose Myasthenia Gravis
How does edrophonium work
Inhibits acetylocholineesterase which is the enzyme that breaks down acetylcholine.
By inhibiting this, ACh will not be broken down, leading to an increase in the amount of ACh available, and greater likelihood of attaching to receptors.
What causes cholinergic toxicity
Nerve gasses: such as sarin
Organophosphates: insecticides
What syndrome does cholinergic toxicity lead to
SLUDGE syndrome
What does SLUDGE stand for
Salivation
Lacrimation
Urination
Defecation
Gastrointestinal cramping
Emesis
How do you treat SLUDGE syndrome
Atropine (Anticholinergic)
What are the two forms of xanthines
Theophylline and Caffeine
What are effects of xanthines
CNS stimulation
Cardiac muscle stimulation
Diuresis
Bronchial, uterine, and vascular smooth muscle relaxation
Peripheral and coronary vasodilation
Cerebral vasoconstriction
Theophylline has a _______ therapeutic index so dosage must be titrated to clinical effectiveness
small
What group of people will need higher doses of theophylline
Smokers bc smoking decreases theophylline levels
What are the recommended dosages for asthma and COPD with theophylline
Asthma: 5-15 μg/mL ( for pts 5 yrs and older)
COPD: 5-10 μg/mL (O and 10 together, to remember)
How to treat apnea of prematurity
Xanthines are given to stimulate CNS bc preterm infants do not have a fully developed CNS
Theophylline was used in the past, now caffeine is the preferred method bc of the fewer side effects
What does of caffeine would you give of AOP
Loading dose: 20 mg/kg
Daily maintenance dose: 5 mg/kg
