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glyburide; glibenclamide (Micronase, DiaBeta, Glynase)

Tradename: Micronase, DiaBeta. 2nd generation sulfonylurea. Indication: 1) treatment of non insulin-dependent diabetes 2) may be useful for gestational diabetes [4] Contraindications: - NOT recommended if creatinine clearance < 50 mL/min [6] Dosage: start with 2.5-5 mg PO QD, max 20 mg/day, QD or divided BID Geriatric patients: - begin 1.25 mg QD, QD dosing - not recommended, long 1/2life & risk of hypoglycemia - glipzide is safer Tabs: 1.25, 2.5, 5 mg. Micronized glyburide. Tradename: Glynase Press Tab. - start 1.5-3 mg PO QD, max 12 mg/day. Pharmacokinetics: 1) onset of action 2-4 hours [2], 15-60 min [3] 2) duration up to 24 hours 3) > 99% plasma protein binding 4) metabolism to 2 active & several inactive metabolites [5, 7] -> active metabolites probably excreted via kidneys [7] 5) up to 50% eliminated unchanged in the urine [6] 6) biphasic elimination: 1/2 life of terminal phase is 10 hours [2], 5-16 hours [3], prolonged with renal insufficiency 7) very little crosses placenta [4] Adverse effects: 1) common (> 10%) - headache - constipation - diarrhea - heartburn - anorexia - epigastric fullness - dizziness 2) less common (1-10%) - skin rash, hives, photosensitivity 3) uncommon (< 1%) - aplastic anemia, hemolytic anemia, cholestatic jaundice, thrombocytopenia, agranulocytosis, hypoglycemia 4) risk of hypoglycemia seems to be highest among sulfonylureas - RR=7.5 vs 2.0 for other sulfonylureas relative to metformin [9] Drug interactions: 1) alcohol may cause disulfiram reactions 2) thiazides & beta adrenergic receptor antagonists decrease effectiveness of glyburide 3) non-steroidal anti-inflammatory agents, warfarin, phenytoin & other highly protein-bound agents may displace glyburide from plasma protein binding & increase toxicity 4) hypoglycemia may occur in combination with clarithromycin [8] Laboratory: - glyburide in specimen - glyburide in serum/plasma - glyburide in urine Mechanism of action: 1) increases release of insulin from the pancreas 2) reduces glucose production from the liver

Interactions

drug interactions drug adverse effects (more general classes) monitor with sulfonylureas

General

sulfonylurea

Properties

MISC-INFO: elimination route LIVER KIDNEY 1/2life 10 HOURS pregnancy-category B safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Prescriber's Letter 7(12):71 2000 Journal Watch 20(24):192, 2000 Langer et al, N Engl J Med 343:1134, 2000
  5. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  6. Drug Evaluation Monograph, Micromedex
  7. Ryberg T et al, Diabetes Car 17(9): 1026, 1994 PMID: 95079919
  8. Paauw DS Dangerous and Deadly Drug Combinations Medscape. June 30, 2016 http://www.medscape.com/features/slideshow/dangerous-drug-combinations
  9. van Dalem J et al Risk of hypoglycaemia in users of sulphonylureas compared with metformin in relation to renal function and sulphonylurea metabolite group: population based cohort study. BMJ 2016;354:i3625 PMID: 27413017 Free full text http://www.bmj.com/content/354/bmj.i3625

Component-of

glyburide/metformin (Glucovance)