QUIZ 1 FINALS Flashcards
(38 cards)
Agent that blocks parasympathetic nervous fibers, which allow relaxation of smooth muscle in the airway.
Anticholinergic bronchodilator
Same as anticholinergic bronchodilator—agent that blocks the effect of acetylcholine at the cholinergic site.
Antimuscarinic bronchodilator
Agent that produces the effect of acetylcholine.
Cholinergic
Same as cholinergic—agent that produces the effect of acetylcholine or an agent that mimics acetylcholine.
Muscarinic
Blocking parasympathetic nervous fibers.
Parasympatholytic
Producing effects similar to the parasympathetic nervous system.
Parasympathomimetic
- Are indicated as bronchodilators for maintenance treatment in COPD, including chronic bronchitis and emphysema.
- is used and may
be indicated in some individuals with asthma
- Ipratropium and tiotropium
- Ipratropium
- A combination anticholinergic and B agonist indicated for use in patients receiving regular treatment for COPD who require additional bronchodilation for relief of airflow obstruction.
- also commonly used in severe asthma in addition to B agonists, especially bronchoconstriction that does not respond well to
B agonist therapy.
- Ipratropium and Albuterol (combivert)
- Ipratropium
is indicated for symptomatic relief of allergic and nonallergic perennial rhinitis and the common cold.
nasal spray formulation
(anticholinergic, or antimuscarinic) agents that are given by aerosol include ipratropium, a combination of ipratropium and albuterol, and tiotropium.
Parasympatholytic
Administered as a nebulized solution, using either the injectable solution or, preferably, solutions marketed for aerosolization; however, this agent is no longer aerosolized.
Dosages for children based on dose-response curves had been given as 0.05 mg/kg three or four times daily.1 Dosages for adults are based on a schedule of 0.025 mg/kg three or four times daily.
The drug is not recommended for inhalation as a bronchodilator because of its widespread distribution in the body and the availability of the approved agents ipratropium and tiotropium.
Atropine sulfate
Is a nonselective antagonist of M1, M2, and M3 receptors.
is currently available in two formulations for bronchodilator use: as a hydrofluoroalkane propelled metered dose inhaler (HFA MDI) and the soft-mist, propellant-free Respimat inhaler.
As a quaternary ammonium derivative of atropine, _______ is fully ionized and does not distribute well across lipid membranes, limiting its distribution more to the lung when inhaled. It is approved specifically for the maintenance treatment of airflow obstruction
in COPD.
Ipratropium bromide (Atrovent)
The onset of bronchodilation begins within minutes but proceeds more slowly to
a peak effect 1 to 2 hours after inhalation. B agonists can peak between 20 minutes and 30 minutes depending on the agent. In asthma, the duration of bronchodilator effect is about the same for ipratropium as for
B agonists. In COPD,
the duration is longer by 1 to 2 hours.
just read under Ipratropium bromide (Atrovent)
is also available for treatment of rhinopathies and rhinorrhea, including nonallergic perennial rhinitis, viral infectious rhinitis (colds), and allergic rhinitis, if intranasal corticosteroids
fail to control symptoms.
The 0.03% strength is given as two sprays per nostril two or three times daily, and the 0.06% strength is given as two sprays per nostril three or four times daily.
Side effects with the nasal spray are largely local and have included nasal dryness, itching, and epistaxis in a few patients. Dry mouth and dry throat have also occurred. Systemic symptoms such as blurred vision or urinary hesitancy are rare.
Ipratropium bromide (Atrovent nasal spray)
- is a combination MDI product, with the usual doses of each agent (18 “g/ puff of ipratropium, 90 “g/puff of albuterol). The combination therapy has been shown to be more effective in stable COPD than either agent alone.
- Another agent, DuoNeb, is available as a combination of ipratropium (0.5 mg) and albuterol base (2.5 mg). Another option for the delivery of _____t is the soft-mist, propellant-free, Respimat inhaler.
- Ipratropium and albuterol (Combivent)
- Combivent
a muscarinic receptor antagonist, is a long-acting bronchodilator. It is a quaternary ammonium compound structurally related to ipratropium.
Similar to ipratropium, this is poorly absorbed after inhalation. Inhalation of a single dose gives a peak plasma level within 5 minutes, with a rapid decline to very low levels within 1 hour.
Tiotropium bromide (Spiriva)
Are specifically parasympatholytic, that is, antimuscarinic agents, blocking the effect of acetylcholine at the cholinergic (muscarinic) receptors on bronchial smooth muscle.
Anticholinergic bronchodilators
- The only approved anticholinergic agents for inhalation as an aerosol at this time are ______ and ________.
- Formulation of Ipratropium (atrovent):
- Formulation of Tiotropium (spiriva)
- ipratropium (Atrovent) and tiotropium (Spiriva)
- SVN, Nasal spray (4-6hrs), MDI
- DPI
Chemical structures of the two naturally occurring belladonna alkaloids, atropine and scopolamine (also called _____.
hyoscine
Atropine, including its sulfate (atropine sulfate), and scopolamine are both _______.
They are easily absorbed in the in the blood stream, , distribute throughout the body, and in particular cross the blood-brain barrier to cause CNS changes.
tertiary ammonium compounds.
Derivatives of atropine include atropine, ipratropium, glycopyrrolate, and tiotropium are ______.
Are fully ionized and poorly absorbed into the bloodstream or CNS.
Given by inhalation generally are poorly absorbed from the lung. They are not rapidly removed from the aerosol deposition site and do not cross the blood brain barrier as atropine sulfate does, giving them wider
therapeutic margin in relation to side effects.
Quaternary ammonium
Another quaternary atropine derivative, which has been administered experimentally as a bronchodilator by aerosol, is _______.
glycopyrrolate (Robinul)
Atropine sulfate, a prototype tertiary compound, inhibits and reduces mucociliary clearance, as shown by Groth and associates. Atropine seems to block hypersecretion stimulated by cholinergic agonists in both the lower airway and the nose (upper airway) more than basal secretion. Atropine relaxes airway smooth muscle, the basis for its use in asthma.
Respiratory tract effects
Tertiary compounds cross the blood-brain barrier and produce dose-related effects. Small doses of 0.5 to 1.0 mg can cause effects that include restlessness, irritability, drowsiness, fatigue, or, alternatively, mild excitement. Increased doses can cause disorientation, hallucinations, or coma. Inhaled atropine has been reported to cause an acute psychotic reaction.
Central nervous system effects.