-
What are some common sisde effects of the adrenergic bronchodilators?
headache, nervousness, irritability, anxiety, and insomnia.
-
A decrease in arterial oxygen pressure has been noted with isoproterenol administration during?
asthmatic brinchospam as ventilation improves
-
It is known that regional alveolar hypoxia produces regional pulmonary vasoconstriction in an effort to shunt perfusion to lung areas of higher oxygen tension. This vasoconstriction is probably accomplished by?
Alpha-sympathetic receptors
-
Administration of inhaled ____________ may reverse hypoxic pulmonary vasoconstriction by Beta 2 stimulation, increasing perfusion to underventilated lung regions.
Beta agonist
-
Oxygen tensions usually return to baseline within?
30mins
-
can increase blood glucose and insulin levels and decrease serum potassium levels.
Adrenergic bronchodilators
-
Diabetics using sympathomimetics or adrenergic bronchodilators should be aware of?
possible effect on glucose and insulin levels.
-
The use of MDIs powered by CFC (e.g., Freon) can cause?
bronchospasms of the airway
-
is an ideal alternative formulation to an MDI if sensitivity to propellants exists, assuming drug availability and adequate inspiratory flow rate.
Use of a dry powder formula (use of a SVN can be concidered)
-
An increasingly publicized problem for individuals with hyperreactive airways is sensitivity to sulfite preservatives result in?
bronchospasms
-
sodium or potassium sulfite, bisulfite, and metabisulfites are all?
Sulfites
-
when a ________ is placed in solution, at warm temperature in an acid pH such as saliva, it converts to sulfurous acid and sulfur dioxide.
Sulfite
-
Sulfur dioxide is known to cause?
bronchoconstriction in asthmatic patients
-
Modification of the catecholamine structure produces?
noncatecholamines
-
What are some examples of noncatecholamines?
metaproterenol, albuterol, and levalbuterol
-
metaproterenol, albuterol, and levalbuterol have a duration of? And what kind of preferential?
4-6 hrs and Beta 2
-
A different modification of the catechol nucleus at the carbon-3 site resulted in the saligenin albuterol, referred to as?
Salbutanmol
-
Albuterol is available in various pharmaceutical vehicles in the United States, including:
Tab, Syr, neb. sol., and MDI.
-
this drug has a beta 2-preferential effect; is effective via oral administration; and has a duration of up to 6 hours, with a peak effect in 30 to 60 minutes.
albuterol
-
is another noncatecholamine adrenergic agent currently available in an MDI formulation with a breath-actuated inhaler delivery device.
Pirbuterol
-
What is the strength of Pirbuterol and the usual dose?
0.2mg per puff and 2 puffs
-
What is the onset, peak effect, and duration of Pirbuterol?
5-8 mins, 30 mints, and 5 hrs
-
is a prodrug, must be converted in the body to be activated, consists of two toluate ester groups on the aromatic ring at the carbon-3 and carbon-4, prtectected from COMT.
Bitolterol
-
The large N-tertiary butyl substituent on the amine side chain on bitolterol prevents oxidation by?
Monoamine oxidase (MAO)
-
Bitolterol's process of activation beginss with the drug being?
administered and gradually continues over time.
-
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
-
Anticholinergic agents given by inhalation offer a second class of?
Bronchodilating agents
-
are indicated as bronchodilators for maintenance treatment in COPD, including chronic bronchitis, emphysema, an asthma
Ipratropium and tiotropium
-
is also commonly used in severe asthma in addition to Beta agonists, especially bronchoconstriction that does not respond well to Beta-agonist therapy.
Ipratropium
-
s indicated for symptomatic relief of allergic and nonallergic perennial rhinitis and the common cold.
Nasal Spray Formulation
-
Parasympatholytic (anticholinergic, or antimuscarinic) agents that are given by aerosol include:
ipratropium, a combination of ipratropium and albuterol, and tiotropium.
-
had been administered as a nebulized solution, using either the injectable solution or, preferably, solutions marketed for aerosolization; however, this agent is no longer aerosolized.
Atropine Sulfate
-
Atropine sulfate Dosages for children based on dose-response curves had been given as _____ mg/kg three or four times daily
0.05
-
Atropine sulfate Dosages for adults are based on a schedule of _________ mg/kg three or four times daily.2 Although greater bronchodilation and duration were seen with dosage schedules of 0.05 or 0.1 mg/kg for adults, the side effects of dry mouth, blurred vision, and tachycardia became unacceptable.
0.025
-
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).
Ipratropium bromide (Atrovent)
-
What is the dose if ipratropium bromide in an inhaler?
17ug/puff
-
What is the solution for nebulization of ipratropium bromide.
0.02% in 2.5mL
-
Specific effects differ for tertiary and quaternary ammonium compounds because of their?
absorption differences
-
Tertiary compounds include
atropine sulfate, scopolamine, and hyoscyamine sulfate
-
a prototype tertiary compound, inhibits and reduces mucociliary clearance, as shown by Groth and associates. It seems to block hypersecretion stimulated by cholinergic agonists in both the lower airway and the nose (upper airway) more than basal secretion. Also, relaxes airway smooth muscle, the basis for its use in asthma.
Atropine
-
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.
-
Tertiary anticholinergic compounds can effect:
Eyes, Cardiac, Gastrointestinal, and Genitourinary
-
Quaternary compounds include
ipratropium and tiotropium and glycopyrrolate.
-
quaternary ammonium compounds do not crosss ___________ easily and do not distribute throughout the body when inhaled.
lipid membranes
-
Agents such as ipratropium produce an anticholinergic effect at the site of delivery; with inhalation, this would be the:
nose/mouth and the upper/lower airway
-
Ipratropium has minimal or no effect on_____________ or ___________, despite the fact that the aerosol is delivered topically to the airways.
mucociliary clearance or mucus viscosity
-
Because quaternary compounds do not cross the blood-brain barrier, they do not?
cause CNS effects
-
As long as ipratropium and other quaternary agents are not ________ in the eye, there are no effects on intraocular pressure, pupil size, or lens accommodation when inhaled as an aerosol.
Sprayed
-
has minimal effects on heart rate or blood pressure when given by inhaled aerosol. Currently, no information has been conclusive in showing that these agents have any adverse effects on the cardiovascular system.
Ipratropium
-
What is ipratropiums effects on gastrointestinal and genitourinary?
None
-
causes the breakdown of phosphoinositides into inositol triphosphate (IP3) and diacylglycerol (DAG); this ultimately leads to an increase in the cytoplasmic concentration of free calcium and smooth muscle contraction or gland exocytosis
PLC
-
The blockade of M1 receptor subtypes by anticholinergic agents also inhibits nerve transmission by?
acetylcholine at the ganglionic synapse.
-
Both ipratropium and tiotropium also block the M2 receptor. This receptor inhibits continued release of?
acetycholine
-
blockade of the M2 receptor can enhance acetylcholine release, possibly counteracting the bronchodilator effect of?
M3 receptor blockade
-
As noted in the discussion of ipratropium and tiotropium, tiotropium has selective affinity for M1 and M3 receptors because it dissociates much more rapidly from the M2 receptor and remains bound
M1 and M3 subtypes
-
are nonspecific blockers of muscarinic receptor subtypes (M1, M2, and M3) in the airway.
Anticholinergic Bronchodilators
-
Blockade of the M3 receptor subtype on bronchial smooth muscle prevents activation of the linking:
Gq protein, its effector system phospholipase C (PLC), and subsequent increase in free calcium with bronchoconstriction or gland exocytosis.
-
Blockade of M1 and M3 receptors in the nasal passages prevents
gland secretion and rhinitis
-
It has been stated that the safety profile of quaternary ammonium antimuscarinic bronchodilators (e.g., ipratropium and tiotropium) is superior to that of � agonists, particularly with regard to
cardiovascular effects ( usually no issues in ECG,BP, and worsening of COPD)
-
The side effects seen with the MDI and small volume nebulizer (SVN) formulations of ipratropium, the agent with the most clinical experience, are primarily related to
the local, topical delivery to the upper and lower airway with inhalation.
-
The most common side effect seen with Ipratropium and antimuscarinic agents of bronchodilator is
dry mouth
-
The SVN solution of Ipratropium and antimuscarinic has also been associated with additional side effects in a few patients, including
pharyngitis, dyspnea, flulike symptoms, bronchitis, and upper respiratory infection
-
Systemic side effects such as tachycardia, palpitations, urinary hesitancy, constipation, blurred vision, and increased ocular pressure are less likely with quaternary agents such as ____________ than with tertiary agents such as atropine
ipratropium or tiotropium
-
Although ipratropium is not contraindicated in subjects with prostatic hypertrophy, urinary retention, or glaucoma, the drug should be used with caution and adequate evaluation for possible
Side effects in there PT's
-
Antimuscarinic agents were found to be more potent bronchodilators than Beta-adrenergic agents in
bronchitis/emphysema
-
Ipratropium has been approved by the FDA specifically for use in the treatment of COPD, although the drug is also prescribed for treatment of
asthma
-
Tiotropium, an antimuscarinic bronchodilator, offers a prolonged duration of action of 24 hours with
a single dose inhalation
-
In dose-ranging trials, an inhaled dose of _____ once per day has been found to give significant bronchodilation in patients with COPD with few side effects
18ug
-
Perhaps one of the more important effects of a long-acting drug such as tiotropium is the elevation in baseline, predose
FEV1
-
is indicated as an alternative for maintenance (step 2) therapy of mild, persistent asthma and higher in patients older than 5 years of age and is listed as an alternative in step 3 and higher for patients older than 5 years of age in combination with an inhaled corticosteroid (ICS).
Sustained-release theophylline
-
is considered a less preferred alternative to low-dose ICS, cromolynlike agents, or antileukotrienes as second-line maintenance drug therapy in stable asthma
Sustained-release theophylline
-
Theophylline is not recommended in the guidelines for children younger than
5 or person' w/ acute exacerbation of asthma
-
The Global Initiative for Chronic Obstructive Lung Disease (GOLD) states that inhaled __________ are preferred when available
bronchodilators
-
Theophylline is considered effective in COPD but, because of potential toxicity, is recommended as an alternative to inhaled bronchodilators such as
Beta 2 agonists or anticholonergic agents
-
If pharmacologic therapy is needed to stimulate breathing in apnea of prematurity, ______________ are considered the first-line agents of choice.
methylxanthines
-
penetrates the cerebrospinal fluid better and has a higher therapeutic index with fewer side effects compared with theophylline.
Caffeine citrate
-
Theophylline is related chemically to the natural metabolite xanthine, which is a precursor of uric acid. Figure 8-1 shows the general xanthine structure and the structures of theophylline (1,3-dimethylxanthine) and caffeine (1,3,7-trimethylxanthine). Because of their methyl attachments, these agents are often referred to as:
methylxanthines
-
theobromine is a
methylxanthines
-
generally have stimulant properties,
Xanthines
-
What are some other effects of xanthines?
diuresis and smooth muscle relaxation
-
The xanthine group has the following general physiologic effects in humans:
CNS stimulation, cardiac stimulation, and diuresis
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