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60 Cards in this Set

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An agent that blocks parasympathetic nervous fibers, which allow relaxation of smooth muscle in the airway

Anticholinergic bronchodilator

Same as anticholinergic bronchodilator: an agent that blocks the effect of acetylcholine at the cholinergic site

Antimuscarinic bronchodilator

An agent that produces the effect of acetylcholine

Cholinergic

Same as cholinergic: an agent that produces the effect of acetylcholine or an agent that mimicks acetylcholine

Muscarinic

Blocking parasympathetic nervous fibers

Parasympatholytic

Producing effects similar to those of the parasympathetic nervous system


Parasympathomimetic

Beta Adrenergic Adverse side effects

1. Tremor


2. Cardiac effects


3. Tolerance to bronchodilator effect


4. Loss of bronchoprotection


5. CNS effects


6. Fall in PaO2


7. Metabolic disturbances


8. Propellant toxicity and paradoxical bronchospasm


9. sensitivity to additives



Parasympathomimetic =

Muscarinic

Parasympatholytic =

Antimuscarinic or Muscarinic Antagonist

Indication for Anticholinergic Bronchodilator

Maintenance COPD


-Chronic bronchitis


-Emphysema

Indication for combined Anticholinergic & B-Agonist Bronchodilators

1. Maintenance COPD with additional relief requirement for airflow obstruction


2. Commonly used in severe Asthma exacerbation



Indication for Anticholinergic Nasal spray

Symptomatic relief of allergic/nonallergic perennial rhinitis

Specific Anticholinergic (parasympatholytic) agents

1. Ipratropium bromide


2. Ipratropium bromide and albuterol


3. Tiotropium bromide

Drug name for Atrovent



Ipratropium bromide



Atrovent HFA MDI Dosage

17 μg/puff 2 puffs qid

Atrovent SVN Dosage

0.02% solution (0.2mg/ml), 500 μg tid, qid

Atrovent Nasal spray Dosage

21 μg: 42 μg: 2 sprays per nostrils 2 to 4 times daily (dosage varies)

Atrovent (time course) Onset, Peak, Duration

Onset: 15 min


Peak: 1-2 hr


Duration: 4-6 hr

Drug name for combivent

Ipratropium bromide and albuterol

Combivent MDI Dosage

ipratropium 18μg/puff and albuterol 90 μg/puff, 2 puff qid

Combivent (Time course) Onset, Peak, Duration

Onset: 15 min


Peak: 1-2 hr


Duration: 4-6 hr

Spiriva Drug name

Tiotropium bromide

Spiriva DuoNeb (SVN) Dosage

Ipratropium 0.5 mg and albuterol 2.5 mg

Spiriva DPI Dosage

18 μg/inhalation, 1 inhalation daily (one capsule)

Spiriva (Time Course) Onset, Peak, Duration

Onset: 30 min


Peak:1-3 hr


Duration:24 hr

Aclidinium bromide

Tudorza pressair (LAMA)

Glycopyrrolate bromide

Lonhala magnair, seebri neohaler (LAMA)

Glycopyrrolate bromide and formoterol

Bevespi Aerosphere (LAMA+ICS)

Glycopyrrolate bromide and Indacterol

Ubitron Neohaler (LAMA+ ICS)

Tiotropium Bromide and olodaterol

Striolto Respimat (LAMA+LABA)

Umeclidinium bromide

Incruse Ellipta (LAMA)

Specific parasympatholytic (anticholinergic/Antimuscarinic) Agent


-Not recommended for inhalation


-Bronchodilator effect seen, side effects prominent

Atropine Sulfate

Specific parasympatholytic (anticholinergic/Antimuscarinic) Agent


-Available as MDI, SVN solution, and nasal spray


-Quaternary ammonium derivative of atropine


-Distribution is limited to lung when inhaled


-Maintenance treatment of COPD


-Quick Onset, peak effect 1-2 hr

Ipratropium bromide

-synergistic effect in COPD


-Combivent

Ipratropium and albuterol

-Used parenterally to reverse neuromuscular blockade


-Quaternary ammonium derivative

Glycopyrrolate

-Longer acting (up to 24 hours) quaternary ammonium derivative of atropine

Tiotropium bromide (Spiriva)

-Contains 2 long-acting bronchodilators in 1 inhaler


-Combines an anticholinergic (umeclidinium) and a long-acting beta2 adrenergic agonist (LABA) medicine (vilanterol)

Anoro Elipta

These anticholinergics are the only ones on the list approved for aerosolization by the FDA


A. Glycopyrrolate


B. Albuterol Sulfate


C. Ipratropium bromide


D. Atropine


E. Aclidinium bromide


F. Tiotropium



A. Glycopyrrolate


C. Ipratropium bromide


D. Atropine


E. Aclidinium bromide


F. Tiotropium

Structure-activity relations


Atropine and Scopolamine

1. Tertiary ammonium compounds


2. Easily absorbed in bloodstream


3. Cross the blood -barrier> CNS

Structure-activity relations


Quaternary forms (Atrovent)

1. Poorly absorbed in the bloodstream or CNS


2. Better for inhalation, less systemic side effects

Tertiary ammonium Compound effects


(Atropine)


Respiratory, CNS, Eye, Cardiac, Gastrointestinal, Genitourinary

1. Respiratory tract- inhibits mucocilliary clearance


2. CNS-irritability, Fatigue


3. Eyes- Iris contraction, pupil dilation, ciliary muscle paralysis


4. Cardiac- Slowing HR at LOW DOSE, increase of HR at HIGH DOSE


5. Gastrointestinal- dry mouth. decreased motility


6. Genitourinary- urinary retention

Quaternary ammonium compound effects

(Ipatropium, Tiotropium, Glycopyrolate)


Respiratory, CNS, Eye, Cardiac, Gastrointestinal, Genitourinary

1. Respiratory tract- bronchodilation

2. Central nervous system- none


3. Eyes- only if sprayed directly into eye


4. Cardiac- none


5. Gastrointestinal- dry mouth


6. Genitourinary- minimal to none


- Side effects are localized to the site of drug exposure

Tertiary (Atropine) Side effects


Respiratory, CNS, Eye, Cardiac, Gastrointestinal, Genitourinary

1. Respiratory tract: Bronchodilation, decreased mucociliary clearance, blockage of hypersecretion


2. CNS: Altered CNS (dose related)


3. Eye: Mydriasis, cycloplegia, increased intraocular pressure


4. Cardiac: Slowing HR (small dose), Increasing HR (larger dose)


5.Gastrointestinal: Dry mouth, Dysphagia; slows motility


6. Genitourinary: Urinary retention

Quaternary (Ipratropium And Tiotropium) Side effects


Respiratory, CNS, Eye, Cardiac, Gastrointestinal, Genitourinary

1. Respiratory tract: Bronchodilation, Little to no change in mucocilliary clearance, blockage of nasal hypersecretions

2. CNS: No effect


3. Eye: Usually no effect


4. Cardiac: no effect


5.Gastrointestinal: Dry mouth


6. Genitourinary: Usually no effect

*Mode of action

1. Parasympathetic innervation causes basal level bronchomotor tone


2. parasympatholytic bronchodilators block this tone. (can be abolished by Anticholinergic agents)


-Competition for muscarinic receptor site block Ach action


3. Degree of bronchodilation depends on the amount of parasympathetic activity or tone present

-Decreased HR


-Miosis (contraction of iris, eye)


-Contraction (thickening) of lens eye


-Salivation


-Lacrimation


-Urination


-Defecation


-Secretion of mucus


-Bronchoconstriction

Cholinergic effect (parasympathomimetic)

-Increased HR


-Mydriasis (pupil dilation)


-Cycloplegia (lens flattened)


-Drying of upper airway


-inhibition of tear formation


-urinary retention


-Antidiarrheal or constipation


-Mucociliary slowing


-Inhibition of constriction

Anticholinergic Effect (parasympatholytic)

In the normal airway what can cause bronchomotor tone and how can it be stopped?

Parasympathetic activity


Can be stopped by anticholinergics

What intensifies the activity of normal airway bronchomotor tone? 2 Example

Parasympathomimetics


1. Methacholine -Constriction


2. Cholinergic stimulation of muscarinic receptors- Contraction & release of mucus

In Anticholinergics, what "competitively blocks" Ach @ receptors & what does this help accomplish?

Antimuscarinic


-Block cholinergic induced bronchoconstriction

Definition


-bronchoconstriction in COPD may be due to:


Irritant aerosols, cold air, high flow rates, cigarette smoke, noxious fumes, histamine

Vagally mediated reflex bronchoconstriction

Vagally mediated reflex bronchoconstriction mechanism

1. Afferent impulse to CNS


2. Reflex cholinergic


3. Constriction of airway smooth muscle


4. Mucus and cough

What are the three muscarinic receptor subtypes?


-Anticholinergics block these receptors

-M1(Ach) and bronchoconstriction


-M2 (bronchodilation)


-M3 (smooth airway muscle) (cause bronchoconsrtiction) nasal gland secretion rhinitis

This anticholinergic is the only one on the list approved for aerosolization by the FDA:



Ipratropium bromide

All anticholinergics agents used in respiratory therapy

1. Ipratropium bromide (Atrovent)


2. Ipratropium bromide & albuterol


3. Aclidinium bromide


4. Aclidinium bromide & formoterol


5. Gylcopyrrolate bromide


6. Glycopyrrolate bromide & formoterol


7. Glycopyrrolate bromide & indacaterol


8. Revefenacin


9. Tiotropium bromide


10. Tiotropium bomide & olodaterol


11. Umeclidinium bromide


12. Umeclidinium bromide & vilanterol



Side effects with anticholinergic MDI and SVN

* ipratropium

1. Dry mouth


2. Cough

Which type of anticholinergic agent are you most likely to observe systemic side effects?: Tertiary ammonium or quaternary ammonium compounds?

Tertiary; these are less ionized and are better absorbed and distributed through body tissue

What precautions should you observe if administering ipratropium by SVN?

protect the eyes from exposure to nebulized drug by using mouth piece instead.'


-Avoids ocular effects of mydraisis

What is the usual recommended dose of ipratropium by MDI and by SVN?

MDI: 34 mcg , 2 puff (each 17 mcg)


SVN: 500mcg, (2.5 mL of a 0.02%)

Ipratropium bromde (atrovent) is a non selective antagonist of which of the following receptors?

has select affinity for M1 and M3 receptors