anticholinergic Flashcards
Anticholinergic AKA
Parasympatholytic
Anticholinergic Agents
Atropine
Atrovent
Spiriva
What do these drugs block?
(Ach) Cholinergic-induced bronchoconstriction
When are these drugs effective?
If bronchoconstriction is due to cholinergic activity
What disease are anticholinergic drugs approved for?
COPD ONLY
used a bronchodilator for maintenance treatment for copd including chronic bronchitis and emphysema.
May be used for severe asthma in addition to beta agonist- especially if patient does not respond well to beta agonist therapy.
BUT ONLY APPROVED FOR COPD!!!!
Specific anticholinergic agents
Atropine
Ipratropium bromide
Combination Ipratropium Bromide/Albuterol
Tiotropium bromide
How would you administer Atropine?
Injection
Why wouldn’t you use Atropine?
Because of the systemic side effects
What kind of membranes do Atropine cross over?
Lipid Membranes
When does the onset begin for Ipratropium Bromide begin?
in several minutes
When does Ipratropium bromide peak?
1-2 hours
When can B2 agonist peak?
20-30 minutes
In asthma patients how long will the Ipratropium Bromide’s duration last?
about the same length of time as the B2 agonist drugs.
In COPD patients how long will the Ipratropium Bromide’s duration last?
1-2 hours longer
What would you use for symptomatic relief of allergic/non-allergic perennial rhinitis AND the common cold?
Anticholinergic Nasal Spray
What kind of effect do you get when mixing Albuterol and Ipratropium Bromide?
Synergistic Effect
What are the trade names for Albuterol and Ipratropium Bromide mixed?
Combivent
Duo-Neb
What is the long acting anti-cholinergic?
Tiotropium Bromide
What is the Trade name for Tiotropium Bromide
Spiriva
How is Spiriva given?
DPI
When does Spiriva Peak?
1-3 hours (says the book)
Easily absorbed in the blood stream?
Tertiary
Poorly absorbed into the bloodstream
Quaternary
Why is Quaternary poorly absorbed into the bloodstream?
Low lipid solubility
Crosses the Blood brain barrier?
Tertiary
CNS
Teritary
Does not cross into the Blood brain barrier?
Quaternary
What kind of compound is Quaternary?
Ipratropium Bromide
Atrovent
Spiriva
Effects of Tertiary (Atropine)
Bronchodilation Decreased Mucus Clearance Block Hypersecretion Altered CNS Heart rate (increases or decreases) dry mouth dysphagia dysphonia Urinary retention
Effects of Quarternary (Ipa)
Bronchodilation
Dry mouth
Blocks hypersecretion
(MOA) How does it enter the lung?
Vagus Nerve
(MOA) Where is it found
Epithelium
Submucosal Glands
Smooth Muscle
Mast Cells
(MOA) Automapping on what sized airways?
Large to Midsized (3-8mm)
(MOA) Are there receptors in the smaller proximal airways or bronchioles?
NO!
(MOA) Basal level of bronchomotor tone is caused by what kind of activity?
Parasympathetic
(MOA) Metacholine stimulates what?
constriction
(MOA) the effects of anticholinergic agents depend upon the degree of tone present that can be?
Blocked
(MOA) In health subjects, there is minimal airway dilation with an anticholinergic agent because there is only what kind of tone being blocked
basal or resting
IF THERE IS NO PARASYMPATHETIC ACTIVITY what kind of effect will the drug have?
MINIMAL!!!!
Bronchoconstriction in COPD may be due in part by what kind of reflex innervation of airway smooth muscle.
Vagally Mediated Relex
What kind of irritants can cause the sensory C-fibers to respond
Aerosols cold air high flows cigarette smoke histamine
When C-fibers are activated they produce what kind of impulse to the CNS?
Afferent Nerve
When C-fibers are activated they produce an afferent impulse to the CNS that results in an ______ impulse to cause _______ of muscle?
Efferent; Constriction
When C-fibers are activated they produce an afferent impulse to the CNS that results in an efferent impulse to cause constriction of muscle, _____ and _______?
Mucus secretion; Cough
When C-fibers are activated they produce an afferent impulse to the CNS that results in an efferent impulse to cause constriction of muscle, mucus secretion and cough. What is this doing?
PROTECTING
These agents also ______ exercise induced asthma, psychogenic bronchoconstriction, and bronchoconstriction caused by beta blockade and cholinergic agents
Inhibit
These agents also inhibit ___________, psychogenic bronchoconstriction, and bronchoconstriction caused by beta blockade and cholinergic agents
exercise induced asthma
These agents also inhibit exercise induced asthma, ____________, and bronchoconstriction caused by beta blockade and cholinergic agents
psychogenic bronchoconstriction
These agents also inhibit exercise induced asthma, psychogenic bronchoconstriction, and ___________ caused by beta blockade and cholinergic agents
bronchoconstriction
These agents also inhibit exercise induced asthma, psychogenic bronchoconstriction, and bronchoconstriction caused by ________and ________
beta blockade and cholinergic agents
What else inhibits reflex bronchoconstriction by blocking irritant receptors?
Aerosolized Lidocaine
Changes in airway may also make cough mechanism more _____?
sensitive
Airways are hypersensitive to deep breaths that result in a cough or increase in
bronchomotor tone
At least a portion of the obstruction in COPD may be due to?
VAGALLY MEDIATED REFLEX BRONCHOCONSTRICITON
Stimuation by afferent ______, trigger reflex efferent vagal nerve activity and constriction
C-Fibers
Anticholinergic agents are ______ antagonists for acetylcholine at muscarinic receptors on airway smooth muscle and M1 receptors at the parasympathetic ganglia
competitive
Anticholinergic agents are competitive antagonists for ______ at muscarinic receptors on airway smooth muscle and M1 receptors at the parasympathetic ganglia
acetylcholine
Anticholinergic agents are competitive antagonists for acetylcholine at ______ receptors on airway smooth muscle and M1 receptors at the parasympathetic ganglia
muscarinic
Anticholinergic agents are competitive antagonists for acetylcholine at muscarinic receptors on ___________ and M1 receptors at the parasympathetic ganglia
airway smooth muscle
Anticholinergic agents are competitive antagonists for acetylcholine at muscarinic receptors on airway smooth muscle and ____ receptors at the parasympathetic ganglia
M1
Anticholinergic agents are competitive antagonists for acetylcholine at muscarinic receptors on airway smooth muscle and M1 receptors at the _____________?
parasympathetic ganglia
They block the action of ________ at the M3 receptor in the airway reversing bronchoconstriction due to cholinergic activity.
acetylcholine
They block the action of acetylcholine at the ____ receptor in the airway reversing bronchoconstriction due to cholinergic activity.
M3
They block the action of acetylcholine at the M3 receptor in the airway ________ bronchoconstriction due to cholinergic activity.
reversing
They block the action of acetylcholine at the M3 receptor in the airway reversing _______ due to cholinergic activity.
bronchoconstriction
They block the action of acetylcholine at the M3 receptor in the airway reversing bronchoconstriction due to ________
cholinergic activity
Atrovent blocks
m1, m2, and m3
Spiriva blocks
M1, M2, and M3
Spriva blocks more slowly from
M1 and M3
Spiriva last for how many hours
24 Hours, because it blocks M1 and M3 more slowly
Ipratropium Bromide trade name?
Atrovent
Ipratropium Bromide routes?
MDI
SVN
Dosages for MDI Atrovent
18ug/2puffs
Dosages for SVN Atrovent
0.5mg, 0.02%
Frequency of Ipratropium Bromide?
QID
Duration of Atrovent
4-6 hours
Tiotropium Bromide trade name?
Spiriva
Route for Spiriva?
DPI
Dosage for Spiriva
18ug/1 puff
Frequency for Spiriva
Once a day
Duration of Spriva
24 hours
Oxtropium bromide trade name?
Oxivent
Oxivent route?
MDI
Dosage for Oxivent
100ug/2 puff
Frequency for Oxivent
BID
Duration of Oxivent
8 hours
Common Side Effects of Atrovent MDI and SVN
Dry mouth
Cough
Occasional Side effects of MDI atrovent?
Nervousness Irritation Dizziness Headache Palpitation Rash
Occasional side effects of SVN atrovent
pharyngitis dyspnea flulike symptoms bronchitis upper respiratory infection nausea eye pain bronchoconstriction urinary retention
Use with caution in patients with?
prostatic hypertrophy
urinary retention
glaucoma
For what disease is proper use of MDI and SVN essential. Use of mouthpiece and reservoir?
Glaucoma
LEARN THE COMPARISON OF
Anticholinergic and Beta Agonist
(receptor types) Airway smooth muscle. Ipratropium and tiotropium block.
M3
(receptor types) ganglionic synapse. Enhance cholinergic nerve transmission. Ipratropium and Tiotropium block?
M1
(receptor types) auto-receptor, inhibition further release of acetycholine so that blocade can increase ach release and may offset the bronchodilating effect of ipratropium
M2
What percent strength is Ipratropium Bromide SVN?
0.02%. 2.5ml vial
parasympatholytic aka
antimuscaranic
What are C-fibers?
Nerves that respond to various stimuli
Sub mucosal gland
M3 receptor