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Pronunciation |
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(meth
a ZOE la
mide) |
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U.S. Brand
Names |
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GlaucTabs®;
Neptazane® |
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Generic
Available |
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No |
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Pharmacological Index |
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Carbonic Anhydrase Inhibitor; Diuretic, Carbonic Anhydrase Inhibitor; Ophthalmic
Agent, Antiglaucoma |
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Use |
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Adjunctive treatment of open-angle or secondary glaucoma; short-term therapy
of narrow-angle glaucoma when delay of surgery is desired |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Marked kidney or liver dysfunction, severe pulmonary obstruction,
hypersensitivity to methazolamide or any component |
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Warnings/Precautions |
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Sulfonamide-type reactions, melena, anorexia, nausea, vomiting, constipation,
hematuria, glycosuria, urinary frequency, renal colic, renal calculi,
crystalluria, polyuria, hepatic insufficiency, various CNS effects, transient
myopia, bone marrow suppression, thrombocytopenia/purpura, hemolytic anemia,
leukopenia, pancytopenia, agranulocytosis, urticaria, pruritus, rash,
Stevens-Johnson syndrome, weight loss, fever, acidosis; use with caution in
patients with respiratory acidosis and diabetes mellitus; impairment of mental
alertness and/or physical coordination. Malaise and complaints of tiredness and
myalgia are signs of excessive dosing and acidosis in the
elderly. |
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Adverse
Reactions |
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>10%:
Central nervous system: Malaise
Gastrointestinal: Metallic taste, anorexia
Genitourinary: Polyuria
Neuromuscular & skeletal: Weakness
1% to 10%:
Central nervous system: Mental depression, drowsiness, dizziness
Genitourinary: Crystalluria
<1%: Fever, headache, seizures, fatigue, rash, sulfonamide rash,
Stevens-Johnson syndrome, hyperchloremic metabolic acidosis, hypokalemia,
hyperglycemia, GI irritation, constipation, xerostomia, black tarry stools, bone
marrow suppression, dysuria, paresthesia, trembling, unsteadiness, myopia,
tinnitus, loss of smell, hypersensitivity |
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Drug
Interactions |
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Increased toxicity:
May induce hypokalemia which would sensitize a patient to digitalis toxicity
May increase the potential for salicylate toxicity
Hypokalemia may be compounded with concurrent diuretic use or steroids
Primidone absorption may be delayed
Decreased effect: Increased lithium excretion and altered excretion of other
drugs by alkalinization of the urine, such as amphetamines, quinidine,
procainamide, methenamine, phenobarbital, salicylates |
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Mechanism of
Action |
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Noncompetitive inhibition of the enzyme carbonic anhydrase; thought that
carbonic anhydrase is located at the luminal border of cells of the proximal
tubule. When the enzyme is inhibited, there is an increase in urine volume and a
change to an alkaline pH with a subsequent decrease in the excretion of
titratable acid and ammonia. |
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Pharmacodynamics/Kinetics |
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Onset of action: Slow in comparison with acetazolamide (2-4 hours)
Peak effect: 6-8 hours
Duration: 10-18 hours
Absorption: Slowly from GI tract
Distribution: Distributes well into tissue
Protein binding: ~55%
Half-life: ~14 hours
Elimination: ~25% excreted unchanged in urine |
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Usual Dosage |
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Adults: Oral: 50-100 mg 2-3 times/day |
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Mental Health: Effects
on Mental Status |
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Sedation is common; may cause dizziness or depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause bone marrow suppression; use caution with clozapine and
carbamazepine; may increase lithium excretion but overall effect is minimal; if
lithium toxicity is severe, hemodialysis is the treatment of
choice |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take with food; swallow whole, do not chew or crush. You may experience
gastrointestinal upset and loss of appetite; frequent small meals are advised to
reduce these effects and the metallic taste that sometimes occurs with this
medication. You may experience lightheadedness, depression, dizziness, or
weakness for a few days; use caution when driving or engaging in tasks that
require alertness until response to drug is known. Report excessive tiredness;
loss of appetite; cramping, pain, or weakness in muscles; acute GI symptoms;
changes in CNS (depression, drowsiness); difficulty or pain on urination; visual
changes; or skin rash. Pregnancy/breast-feeding precautions: Inform
prescriber if you are or intend to be pregnant. Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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May cause an alteration in taste, especially when drinking carbonated
beverages |
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Dosage Forms |
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Tablet: 25 mg, 50 mg |
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