Quiz 6: Respiratory Drugs and Antihistamines Flashcards
What are the respiratory medications?
- anticholinergics
- Adreneric Agonist
- Membrane Stabilizers
- Xanhines
- Related Drugs: Tocolytics
- Corticosteriods
List the drugs that are anticholinergics:
- Atropine
- Ipratropium
- Tiotropium
- Aclidium
There are 5 muscarinic receptor subtypes what is the location, clinical effects, and is/are there selective drugs for this receptor for M1:
- CNS, Stomach
- Hydrogen ion secretion
- Yes
There are 5 muscarinic receptor subtypes what is the location, clinical effects, and is/are there selective drugs for this receptor for M2:
- Heart , CNS
- Bradycardia
- NO
There are 5 muscarinic receptor subtypes what is the location, clinical effects, and is/are there selective drugs for this receptor for M3:
-CNS, Salivary glands
Airway smooth muscles
- Salivation and Bronchodi
- NO
There are 5 muscarinic receptor subtypes what is the location, clinical effects, and is/are there selective drugs for this receptor for M4:
- CNS
- ?
- NO
There are 5 muscarinic receptor subtypes what is the location, clinical effects, and is/are there selective drugs for this receptor for M5:
- CNS
- ?
- NO
What is the mechanism of action for Atropine?
-Antagonizes ACh effects on airway smooth muscle in large and mmedium sized airways
T/F: Atropine effects airwasys that respond to vagal stimulation.
TRUE
What would you see in lung capacity if using atropine:
- Decreases in airway resistance
- Increase in dead space
T/F: Ipratropium is effective in treating bronchospasm due to the beta AGONIST.
FALSE (…due to the beta antagonist)
Ipratropium has an onset of (_______ minutes) and less effective than beta agonist in treating ______ ________.
- 30 to 90
- bronchial asthma
Ipratropium is more effective than beta agonist in ____ ____ or ________.
- chronic bronchitis
- emphysema
T/F: Ipratropium is highly soluble and results in systematic effect.
FASLE (Limited absorption results in prolonged local site effect
Atropine may have paradoxical bronchospasm due to what muscarinic receptor subtype?
M2
What is tiotropium?
Spiriva
Tiotropium mechanism of action is:
- it blocks the muscarinic receptor subtypes M1 and M3
Tiotropium would cause what reaction in the lungs?
- Facilitates bronchodilation
- Reduces mucous secretion
Tiotropium would be use in the treatment of:
-bronchospasm associated with COPD including chronic bronchitis and emphysema
Tiotropium is a long term or short term drug?
Long term
What is aclidinium?
Tudorza
What is aclidinium similar too?
tiotropium (Spiriva)
Two differences about aclidinium vs. Tiotropium.
- Given twice daily
- Faster onset to peak (2 days vs. 7 days)
What adrenergic agents are beta agonist:
- Ephedrine
- Isoproterenol
- Albuterol
- Terbutaline
Ephedrine is an _______ acting synthetic noncatecholamine that stmulates ____ and ___ receptors.
- indirect
- alpha
- beta
What receptor does ephedrine work on to cause broncho-dilatation:
Beta 2
Ephedrine can be used as a ____ oral medication to treat bronchial asthma.
chronic
Isoproterenol act at which adrenergic receptor(s):
- Beta 1
- Beta 2
What is unique about a beta 2 agonist:
- Relax bronchial smooth muscle
- Lack stimulating effects on the heart
- Structure makes them resistant to COMT (COMT break down catecholemines except synthetic are broken down only by MAO)
What are the uses of a beta 2 agonist:
- Preferred treatment for acute episodes of asthma
- Prevention of exercise induced asthma
- Improve airflow and exercise toerance in patient with COPD
- Tocolytic to stop uterine contractions
An intermediate class of a beta 2 agonist would last for:
-3 to 6 hours
An long acting class of a beta 2 agonist would last for:
- greater 12 hours
What is a long acting beta 2 agonist:
-Salmeterol (>12 hours)
What is a intermediate acting beta 2 agonist:
- Albuterol
- metaproterenol
- Terbutaline
How much inhalation medication is delivered to the lung with inhalation technique.
-12%
What are the side effects of a beta 2 agonist:
- Tremor
- Tachycardia
- Metabolic Response
Where do the tremors come from on when using a beta 2 agonist?
-Stimulation of the beta 2 receptors on skeletal muscle
Where does the tachycardia come from on when using a beta 2 agonist
- Direct stimulation of receptors on the heart
- REFLEX TACHYCARDIA due to Beta2 induced vasodilitation
What type of metabolic response would be seen with a beta 2 atagonist.
- Hyperglycemia
- Hypokalemia
- Hypomagnesemia
What is the preferred beta 2 agonist for bronchospasm?
Albuterol
What would be the side effect albuterol?
- tachycardia
- hypokalemia
What is levoalbuerol?
-xopenex
Levoalbuterol is a ____________ of racemic albuterol.
(R)-enantiomer of racemic albuterol
T/F: Levoalbuterol has little or no clinically significant difference in adverse effects compared to albuterol.
TRUE
Metaproterenol is a selective _________ _______.
beta 2 agonist
Terbutaline has two uses what are they for:
- Treatment of asthma
- Tocololytic
Terbutaline is a Selective ______ ______.
beta 2 agonist
What would salmeterol be given for:
Prophylaxis of asthma
What is a membrane stabilizer?
-Inhibits antigen induced release of histamine and other mediators from pulmonary mast cells during antibody mediated allergic responses
What drug would be a membrane stabilizer?
-Cromolyn Sodium (INTAL)
Does cromolyn sodium (Intal) have a use in ACUTE asthma attack.
NO
Cromolyn Sodium (_____) does ___ relax the bronchial or vascular smooth muscle.
- intal
- NOT
What does cromolyn sodium (INTAL) suppress and what does in NOT interact with?
- Secretory response
- Ag-Ab
What drugs are methylxanthines?
- Theophylline/aminophylline
- caffiene
- theobromine
What are the uses of methylxanthines?
- stimulate the CNS
- INCREASE B/P
- Increase myocardial contractility and heart rate
- Relax smooth muscle (airways)
Methylxanthines are a competitive antagonist of ______ receptor.
adenosine
Which of the methylxanthines is most active?
theophylline
What replaced theophyllines when treating an acute exacerbation of asthma.
-Beta 2 agonist
An infant has apnea how would you treat it:
Theophylline
Theophylline toxicity of 15-25 mcg/ml would cause:
- GI upset
- N/V
- tremor
Theophylline toxicity of 26 - 35 would cause:
- Tachycardia
- PVC
Theophylline toxicity of >35 would cause:
- VTach
- seizures
What are the effects of caffeine?
- CNS stimulant
- Cerebral vasoconstrictor
- Secretion of gastric acid
What are the uses of caffeine?
- apnea of prematurity
- post dural puncture headache
- Cold rememdies (offset sedation from antihistamines)
Ritodine is a ____.
Tocolytic
What is the mechanism of action for ritodine?
-beta 2 agonist stimulated and activates adenyl cyclase
T/F: Ritodrine has some beta 1 effects.
TRUE
T/F: Ritodrine is okay to use after the first trimester of a pregnancy.
FALSE (NO teratogenic effet when used after 20 weeks of EGA)
What are some side effect of ritodrine?
- Tachycardia
- Elevated cardiac output
- Increase in RENIN secretion
- Exaggerated systemic BP decrease
- Hyperglycemia in mother may cause reavtive hypoglycemia in fetus.
What will the renin increase do to the parturient which is on ritodrine?
- Decreased NA and water secretion
- Increase K and H loss (hypokalemia)
- Pulmonary edema may occur
What would be the definition of a histamine?
-Low molecular weight , naturally occurring hydrophilic endogenous amine that produces a variety of physiologic and pathologic responses
Where are histamine found?
- skin
- lungs
- GI tract
- circulating basophils
Histamine act through ______ couple membrane receptors.
G protein
Histamines are released to what kind of response:
- Certain drugs
- AG-AB reaction
T/F: Histamine do no easily cross the blood brain barrier.
TRUE
H-1 receptors cause:
- evoke smooth muscle contraction in the respiratory and G.I tracts
- Cause pruritus and sneezing by sensory nerve stimulation
- Cause nitric oxide mediated vasodilitation
- Slow the heart rate by decreasing A-V nodal conduction
- Mediate epicardial coronary vasoconstriction
H-2 receptors cause:
- activates adenyl cyclase and increases intracellular cAMP
- Increase myocardial contractility and heart rate
- With H1 receptors increase capillary permeability and vasodilitation
An H-2 has what effect on the gastric parietal cells.
-causes them to secrete hydrogen ions
H-2 have a vasodilating effects on coronary vasculature that ______the vasoconstricting effects of H-1 receptors.
-opposes
What do both the H1 and H2 receptor histamines cause:
- Increased capillary permeability
- Hypotension
- Tachycardia
- Flushing
- Headache
Triple response (Wheal and Flare) is:
- Edema due to increased permeability
- Dilated arteries around the edema (FLARE)
- Pruitus due to histamine in the superficial layers of the skin
What will H1 receptor activation do within the lungs?
-Constricts bronchial smooth muscle
What will H2 receptor activation do within the lungs?
-Relax bronchial smooth muscle
H1 activation within the lung of a normal patient is usually ________.
negligible
H1 activation within the lungs of a asthmatic or bronchitis patient is more likely to develop increases in _____ _____.
-airway resistance
Other than H2 receptor what else can increase H secretions.
Vagal activity
Histamine receptor antagonists do ___ inhibit the release of histamine, but rather ___ to receptors and prevent the responses mediated by histamine.
- NOT
- attach
H1 receptor antagonist have two generation, the first generation will cause ______ and may also activate ______, _______, or _________ receptors.
- SEDATION
- muscarinic
- serotonin
- alpha-adrenergic
The H1 receptor antagonist that is a first generation will do what to the CNS:
- Somnolence
- Decreased alertness,
- Slowed reaction time
- Impaired cognitive function
The H1 receptor antagonist that is a first generation will do what to anticholinergic:
- dry mouth
- blurred vision
- urinary retention
- impotence
The H1 receptor antagonist that is a first generation will do what to cardiovascular:
- tachycardia
- QT prolongation
- heart block
- cardiac dysrhythmias
The H1 receptor antagonist the is a second generation will have what effects:
-Unlikely to produce CNS side effects UNLESS recommended doses are exceeded
T/F: The H1 receptor antagonist that is a second generation enhancement of sedative or alcohol is unlikely.
TRUE
What are the H1 histamine receptor antagonist clinical uses:
- prevent and relieve the symptoms of allergic rhinoconjunctivitis
- Pretreatment may provide some protection against bronchospasm induced by various stimuli
- Antipruitic
- Sedative
- Antiemetic
Diphenhydramine (_____) is a H1 antihistamine which is a _ generation.
- Benadryl
- 1st
Dimenhydrinate (______) is a H1 antihistamine which is a __ generation.
- Dramamine
- 1st
What would Diphenhydramine be used for:
- sedative
- antipruritic
- antiemetic
- anaphylaxis
What would dimenhydrinate be used for:
-motion sickness
-PONV
-
How does dimenhydrinate work within the body:
-inhibits the integrative functioning of vestibular nuclei by decreasing vestibular and visual input.
List some H1 antihistamines that are 2nd generations:
- Zyrtex/xyzal = cetirizine/levovetirizine
- Claritin = Loratidine
- Allegra = fexofenadine