Dosing and uses of Diabinese (chlorpropamide)
Adult dosage forms and strengths
tablet
- 100mg
- 250mg
Dosage should be individualized based upon patient's response
Type 2 Diabetes
Administer 30 minutes before meal to improve absorption
Middle-aged stable diabetic
- 250 mg/day PO initially; may increase or decrease PRN by 50-125 mg/day at 3- to 5-day intervals
Older patients
- 100-125 mg/day PO initially; may increase or decrease PRN by 50-125 mg/day at 3- to 5-day intervals
Maintenance dose
- 100-250 mg/day; a higher dose of 500 mg/day may be required in severe diabetes; should avoid doses >750 mg/day
Renal Impairment
CrCl <50 mL/minute: Avoid use
CrCl >50 mL/minute: Monitor therapy closely; initial and maintenance dosing should be conservative to avoid hypoglycemia
Hepatic Impairment
Use lower initial and maintenance dose in liver impairment; chlorpropamide undergoes extensive hepatic metabolism
Other Indications & Uses
Off-label: Neurogenic diabetes insipidus
Pediatric dosage forms and strengths
Safety and efficacy not established
Geriatric dosage forms and strengths
Not drug of choice in elderly; increased risk of hypoglycemia and drug interactions because of long half-life
Type 2 Diabetes
100-125 mg PO qDay initially; may increase or decrease PRN by 50-125 mg/day at 3-5 day intervals
Diabinese (chlorpropamide) adverse (side) effects
Frequency not defined
Dermatologic reactions
Hypoglycemia
Dizziness
Headache
Hepatic porphyria
Liver failure
Anorexia
Agranulocytosis
Aplastic anemia
Nausea
Disulfiram-like reactions
Vomiting
Blood dyscrasias
Associated with greater number of side effects in the geriatric and renally impaired; should not be used as first line agent in these populations
Cholestatic jaundice and hepatitis may occur rarely which may progress to liver failure
Warnings
Contraindications
Type I diabetes
Diabetes ketoacidosis
Hypersensitivity, sulfa allergy
Severe renal impairment
Cautions
Half life prolonged in renal failure
Efficacy may decrease with prolonged use
Patients with risk of severe hypoglycemia, especiall elderly, debilitated, or malnourished patients, patients with risk factors for cardiovascular events, severe liver impairment
Pregnancy and lactation
Pregnancy category: C
Lactation: Excretion in milk unknown/not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Diabinese (chlorpropamide)
Mechanism of action
Initial effect to increase beta-cell insulin secretion; may also decrease rate of hepatic glucose production, increases insulin receptor sensitivity, and increases number of insulin receptors
Pharmacokinetics
Half-Life: 25-48 hr
Duration: 24 hr
Initial effect: Diabetes mellitus: 1 hr; Diabetes insipidus: 1 d
Maximum effect: Diabetes mellitus: 3-6 hr; Diabetes insipidus: 4-5 d
Protein Bound: 60-90%
Vd: 0.13-0.23 L/kg
Metabolism: Moderately to extensively metabolized in the liver
Metabolites: Hydroxychlorpropamide, chlorobenzene-sulfonylurea (inactive)
Excretion: Mainly in urine (80-90%)
Dialyzable: PD: no, HD: no
