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Pronunciation |
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(meth
a KOLE
leen) |
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U.S. Brand
Names |
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Provocholine® |
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Generic
Available |
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No |
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Synonyms |
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Methacholine Chloride |
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Pharmacological Index |
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Diagnostic Agent |
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|
Use |
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Diagnosis of bronchial airway hyperactivity in subjects who do not have
clinically apparent asthma |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Concomitant use of beta-blockers; hypersensitivity to the drug; because of
the potential for severe bronchoconstriction, methacholine challenge should not
be performed on any patient with clinically apparent asthma, wheezing, or very
low baseline pulmonary function tests (forced expiratory volume in one second
less than 70% of predicted value). |
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Warnings/Precautions |
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Methacholine is a bronchoconstrictor for diagnostic purposes only. Perform
inhalation challenge under the supervision of a physician trained in and
thoroughly familiar with all aspects of the technique, all contraindications,
warnings, and precautions of methacholine challenge and the management of
respiratory distress. Have emergency equipment and medication immediately
available to treat acute respiratory distress. Administer only by inhalation;
severe bronchoconstriction and reduction in respiratory function can result.
Patients with severe hyper-reactivity of the airways can experience
bronchoconstriction at a dosage as low as 0.025 mg/mL (0.125 cumulative units).
If severe bronchoconstriction occurs, reverse immediately by administration of a
rapid-acting inhaled bronchodilator (beta-agonist). |
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Adverse
Reactions |
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<1%: Hypotension, complete heart block, substernal pain, tightness of the
chest, syncope, headache, lightheadedness, throat irritation, itching, cough,
dyspnea, wheezing |
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Stability |
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Store unreconstituted powder at 59°F to
86°F; store dilutions in refrigerator
(36°F to 46°F) for up to 2
weeks |
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Mechanism of
Action |
|
Methacholine chloride is a cholinergic (parasympathomimetic) synthetic
analogue of acetylcholine. The drug stimulates muscarinic, postganglionic
parasympathetic receptors, which results in smooth muscle contraction of the
airways and increased tracheobronchial secretions. |
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Pharmacodynamics/Kinetics |
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Onset of action: Rapid
Peak effect: Within 1-4 minutes
Duration: 15-75 minutes or 5 minutes if the methacholine challenge is
followed with a beta-agonist agent |
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Usual Dosage |
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Before inhalation challenge, perform baseline pulmonary function tests; the
patient must have an FEV1 of at least 70% of the predicted value. The
following is a suggested schedule for administration of methacholine challenge.
Calculate cumulative units by multiplying number of breaths by concentration
given. Total cumulative units is the sum of cumulative units for each
concentration given. (See breakdown below)
Serial concentration 0.025 mg/mL; No. of breaths 5; cumulative units per
concentration 0.125; total cumulative units 0.125
Vial D:
Serial concentration 0.25 mg/mL; No. of breaths 5; cumulative units per
concentration 1.25; total cumulative units 1.375
Vial C:
Serial concentration 2.5 mg/mL; No. of breaths 5; cumulative units per
concentration 12.5; total cumulative units 13.88
Vial B:
Serial concentration 10 mg/mL; No. of breaths 5; cumulative units per
concentration 50; total cumulative units 63.88
Vial A:
Serial concentration 25 mg/mL; No. of breaths 5; cumulative units per
concentration 125; total cumulative units 188.88
Determine FEV1 within 5 minutes of challenge, a postive challenge
is a 20% reduction in FEV1 |
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Dosage Forms |
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Powder for reconstitution, inhalation, as chloride: 100 mg/5
mL |
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