chlorpropamide (Diabinese)

Introduction

Tradename: Diabinese. 1st generation sulfonylurea.

Dosage

start with 100-250 mg PO QD, max 750 mg/day

Tabs: 100 & 250 mg.

Pharmacokinetics

• no significant metabolism

elimination via kidney

1/2life = 36 hours

protein binding = 60-95 %

elimination by peritoneal dialysis = -

Adverse effects

• hematologic:
  • transient leukopenia, thrombocytopenia, hemolytic anemia, pancytopenia, eosinophilia
• gastrointestinal disturbances
• headache
• tinnitus
• photosensitivity
• allergic skin reactions
• intolerance to alcohol
• most serious adverse effects
  • hypoglycemia
  • hepatic dysfunction
• SIADH (only hypoglycemic to cause SIADH)

• drug adverse effects of sulfonylureas
• drug adverse effects of hypoglycemic agents

Drug interactions

• increased risk of hypoglycemia with:
  • sulfonamides, non-selective beta-blockers (propranolol), salicylates, clofibrate, phenylbutazone, probenecid, dicumarol, warfarin, chloramphenicol, MAO inhibitors, alcohol

• drug interaction(s) of sulfonylureas with warfarin
• drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
• drug interaction(s) of fluroquinolones with sulfonylureas
• drug interaction(s) of macrolides with sulfonylureas
• drug interaction(s) of salicylates with sulfonylureas
• drug interaction(s) of gliptins with sulfonylureas
• drug interaction(s) of fluoroquinolones with hypoglycemic agents

Laboratory

• specimen: serum
• methods: HPLC, GLC, color
• interferences:
  • color: hemolysis, primary & secondary amines
  • GLC: plasma lipids

More general terms

• sulfonylurea

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2727
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=528160
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=528159