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Pronunciation |
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(GLYE
byoor
ide) |

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U.S. Brand
Names |
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Diabeta®;
Glynase™
PresTab™; Micronase® |

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Generic
Available |
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No |

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Canadian Brand
Names |
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Albert® Glyburide; Apo®-Glyburide;
Euglucon®; Gen-Glybe; Novo-Glyburide; Nu-Glyburide |

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Synonyms |
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Glibenclamide; Glybenclamide; Glybenzcyclamide |

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Pharmacological Index |
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Antidiabetic Agent (Sulfonylurea) |

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Use |
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Management of noninsulin-dependent diabetes mellitus (type
2) |

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Pregnancy Risk
Factor |
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C |

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Pregnancy/Breast-Feeding
Implications |
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Clinical effects on the fetus: Crosses the placenta. Hypoglycemia; ear
defects reported; other malformations reported but may have been secondary to
poor maternal glucose control/diabetes. Insulin is the drug of choice for the
control of diabetes mellitus during pregnancy.
Breast-feeding/lactation: No data available |

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Contraindications |
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Hypersensitivity to glyburide or any component, or other sulfonamides; type 1
diabetes mellitus, diabetic ketoacidosis with or without
coma |

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Warnings/Precautions |
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Elderly: Rapid and prolonged hypoglycemia (>12 hours) despite hypertonic
glucose injections have been reported; age and hepatic and renal impairment are
independent risk factors for hypoglycemia; dosage titration should be made at
weekly intervals. Use with caution in patients with renal and hepatic
impairment, malnourished or debilitated conditions, or adrenal or pituitary
insufficiency.
At higher dosages, sulfonylureas may block the ATP-sensitive potassium
channels, which may correspond to an increased risk of cardiovascular events. In
May, 2000, the National Diabetes Center issued a warning to avoid the use of
sulfonylureas at higher dosages (glyburide daily doses >2.5 mg).
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Adverse
Reactions |
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>10%:
Central nervous system: Headache, dizziness
Gastrointestinal: Nausea, epigastric fullness, heartburn, constipation,
diarrhea, anorexia
Ocular: Blurred vision
1% to 10%: Dermatologic: Pruritus, rash, urticaria, photosensitivity reaction
<1%: Hypoglycemia, nocturia, leukopenia, thrombocytopenia, hemolytic
anemia, aplastic anemia, bone marrow suppression, agranulocytosis, cholestatic
jaundice, arthralgia, paresthesia, diuretic effect |

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Overdosage/Toxicology |
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Symptoms of overdose include severe hypoglycemia, seizures, cerebral damage,
tingling of lips and tongue, nausea, yawning, confusion, agitation, tachycardia,
sweating, convulsions, stupor, and coma
Intoxications with sulfonylureas can cause hypoglycemia and are best managed
with glucose administration (oral for milder hypoglycemia or by injection in
more severe forms) |

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Drug
Interactions |
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CYP3A3/4 enzyme substrate
Increased effect: Possible interaction between glyburide and fluoroquinolone
antibiotics has been reported resulting in a potentiation of hypoglycemic action
of glyburide
Increased toxicity:
Since this agent is highly protein bound, the toxic potential is increased
when given concomitantly with other highly protein bound drugs (ie,
phenylbutazone, oral anticoagulants, hydantoins, salicylates, NSAIDs,
beta-blockers, sulfonamides) - increase hypoglycemic effect
Alcohol increases disulfiram reactions
Phenylbutazone can increase hypoglycemic effects
Certain drugs tend to produce hyperglycemia and may lead to loss of control
(ie, thiazides and other diuretics, corticosteroids, phenothiazines, thyroid
products, estrogens, oral contraceptives, phenytoin, nicotinic acid,
sympathomimetics, calcium channel blocking drugs, and isoniazid)
Possible interactions between glyburide and coumarin derivatives have been
reported that may either potentiate or weaken the effects of coumarin
derivatives |

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Mechanism of
Action |
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Stimulates insulin release from the pancreatic beta cells; reduces glucose
output from the liver; insulin sensitivity is increased at peripheral target
sites |

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Pharmacodynamics/Kinetics |
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Onset of action: Oral: Insulin levels in the serum begin to increase within
15-60 minutes after a single dose
Duration: Up to 24 hours
Metabolism: To one moderately active and several inactive metabolites
Plasma protein binding: High (>99%)
Half-life: 5-16 hours; may be prolonged with renal insufficiency or hepatic
insufficiency
Time to peak serum concentration: Adults: Within 2-4 hours
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Usual Dosage |
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Oral:
Initial: 2.5-5 mg/day, administered with breakfast or the first main meal of
the day. In patients who are more sensitive to hypoglycemic drugs, start at 1.25
mg/day.
Increase in increments of no more than 2.5 mg/day at weekly intervals based
on the patient's blood glucose response
Maintenance: 1.25-20 mg/day given as single or divided doses; maximum: 20
mg/day
Elderly: Initial: 1.25-2.5 mg/day, increase by 1.25-2.5 mg/day every 1-3
weeks
Micronized tablets (Glynase PresTab™): Adults:
Initial: 1.5-3 mg/day, administered with breakfast or the first main meal of
the day in patients who are more sensitive to hypoglycemic drugs, start at 0.75
mg/day. Increase in increments of no more than 1.5 mg/day in weekly intervals
based on the patient's blood glucose response.
Maintenance: 0.75-12 mg/day given as a single dose or in divided doses. Some
patients (especially those receiving >6 mg/day) may have a more satisfactory
response with twice-daily dosing.
At higher dosages, sulfonylureas may block the ATP-sensitive potassium
channels, which may correspond to an increased risk of cardiovascular events. In
May, 2000, the National Diabetes Center issued a warning to avoid the use of
sulfonylureas at higher dosages (glipizide daily doses >2.5 mg); see
Warnings/Precautions.
Dosing adjustment/comments in renal impairment: Clcr
<50 mL/minute: Not recommended
Dosing adjustment in hepatic impairment: Use conservative initial and
maintenance doses and avoid use in severe disease |

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Dietary
Considerations |
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Alcohol: A disulfiram-like reaction characterized by flushing, headache,
nausea, vomiting, sweating, or tachycardia; avoid use
Food: Food does not affect absorption; glyburide may be taken with food
Glucose: Decreases blood glucose concentration. Hypoglycemia may occur.
Educate patients how to detect and treat hypoglycemia. Monitor for signs and
symptoms of hypoglycemia. Administer glucose if necessary. Evaluate patient's
diet and exercise regimen. May need to decrease or discontinue dose of
sulfonylurea.
Sodium: Reports of hyponatremia and SIADH. Those at increased risk include
patients on medications or who have medical conditions that predispose them to
hyponatremia. Monitor sodium serum concentration and fluid status. May need to
restrict water intake. |

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Monitoring
Parameters |
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Signs and symptoms of hypoglycemia, fasting blood glucose, hemoglobin
A1c, fructosamine |

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Reference Range |
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Target range: Adults:
Glycosylated hemoglobin: <7% |

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Mental Health: Effects
on Mental Status |
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Dizziness is common |

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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause agranulocytosis; use caution with clozapine and
carbamazepine; phenothiazines and TCAs may antagonize glimepiride hypoglycemic
effects; MAOIs and TCAs may enhance hypoglycemic effects |

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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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Glyburide-dependent diabetics (noninsulin dependent, type 2) should be
appointed for dental treatment in morning in order to minimize chance of
stress-induced hypoglycemia |

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Patient
Information |
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This medication is used to control diabetes; it is not a cure. Other
components of treatment plan are important: follow prescribed diet, medication,
and exercise regimen. Take exactly as directed; 30 minutes before meal(s) at the
same time each day. Do not change dose or discontinue without consulting
prescriber. Avoid alcohol while taking this medication; could cause severe
reaction. Inform prescriber of all other prescription or OTC medications you are
taking; do not introduce new medication without consulting prescriber. Do not
take other medication within 2 hours of this medication unless so advised by
prescriber. If you experience hypoglycemic reaction, contact prescriber
immediately. Maintain regular dietary intake and exercise routine and always
carry quick source of sugar with you. You may be more sensitive to sunlight (use
sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). You
may experience side effects during first weeks of therapy (headache, nausea);
consult prescriber if these persist. Report severe or persistent side effects,
extended vomiting or flu-like symptoms, skin rash, easy bruising or bleeding, or
change in color of urine or stool. Pregnancy/breast-feeding precautions:
Inform prescriber if you are or intend to be pregnant. Do not
breast-feed. |

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Nursing
Implications |
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Patients who are anorexic or NPO, may need to have their dose held to avoid
hypoglycemia |

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Dosage Forms |
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Tablet (Diabeta®,
Micronase®): 1.25 mg, 2.5 mg, 5 mg
Tablet, micronized (Glynase™
PresTab™): 1.5 mg, 3 mg, 4.5 mg, 6 mg
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References |
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Brodows RG,
"Benefits and Risks With Glyburide and Glipizide in Elderly NIDDM Patients,"
Diabetes Care, 1992, 15(1):75-80.
Gavin JR 3d,
"Glyburide: New Insights Into Its Effects on the Beta Cell and Beyond - Introduction,"
Am J Med, 1990, 89(2A):1S-2S.
Nataas OB and Nesthus I,
"Immune Haemolytic Anaemia Induced by Glibenclamide in Selective IgA Deficiency,"
Br Med J (Clin Res Ed), 1987, 295(6594):366-7.
Pearson JG, "Pharmacokinetics of Glyburide," Am J Med, 1985,
79(3B):67-71.
Rosenstock J, Corrao PJ, Goldberg RB, et al,
"Diabetes Control in the Elderly: A Randomized, Comparative Study of Glyburide Versus Glipizide in Noninsulin-Dependent Diabetes Mellitus,"
Clin Ther, 1993, 15(6):1031-40.
Schwinghammer TL, Antal EJ, Kubacka RT, et al,
"Pharmacokinetics and Pharmacodynamics of Glyburide in Young and Elderly Nondiabetic Adults,"
Clin Pharm, 1991, 10(7):532-8.
Sillence DO and Court JM, "Glibenclamide-Induced Hypoglycemia," Br Med
J, 1975, 3(5981):490-1.
Sonnenblick M and Shilo S,
"Glibenclamide Induced Prolonged Hypoglycaemia," Age Ageing, 1986,
15(3):185-9.
"Standards of Medical Care for Patients With Diabetes Mellitus. American Diabetes Association,"
Diabetes Care, 1994, 17(6):616-23. |

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