@Critter Mom
@Elizabeth and Bertie
@Nan & Amber (GA)
From:
Plumb's Veterinary Drug Handbook (6th ed., 2008)
I apologize for the weird look. I did clean it up somewhat. It was copied and pasted from a pdf.
Bold emphasis mine.
GLIMEPIRIDE (glye-meh-per-ide) Amaryl® SuLfONyLuReA ANTIDIAbeTIc AGeNT
prescriber Highlights
Oral, once-daily, anti-hyperglycemic agent; could be useful in the adjunctive treatment of non-insulin dependent diabetes mellitus (NIDDM) in cats
Very limited experience in cats
Contraindicated: Patients hypersensitive to it or with diabetic ketoacidosis
Hypoglycemia may occur
Potentially, significant drug interactions
Do not confuse glipizide, glimepiride & glyburide
uses/indications
Glimepiride may potentially be a useful adjunct in the treatment of non-insulin dependent diabetes mellitus (NIDDM) in cats. Its duration of action in humans allows it to be dosed once daily, which could be of benefit in cats. It may also have fewer side effects than glipizide in cats.
pharmacology/actions
Glimepiride increases pancreatic release of insulin from function- ing beta cells and, with continued use, may also increase peripheral tissue sensitivity to insulin. The exact mechanism for these effects is not well understood.
pharmacokinetics
No pharmacokinetic data for cats was located. In humans, glimepiride is completely absorbed from the GI tract. Peak levels occur in 2–3 hours; food delays the peak somewhat and lowers AUC by about 9%. Volume of distribution is 0.11 L/kg; the drug is greater than 99% bound to plasma proteins. Glimepiride is hepatically metabolized to at least two major metabolites. One of these, M1, has activity at about N that of the parent compound; clearance is 48 mL/min and elimination half-life about 9 hours. Approximately 60% of the drug (as metabolites) are excreted into the urine and the remainder in the feces. The drug has a 24-hour duration of activity in humans.
contraindications/precautions/Warnings
Glimepiride is contraindicated in patients hypersensitive to it or with diabetic ketoacidosis.
adverse effects
Hypoglycemia has been reported in about 1% of human patients taking the drug. Dizziness and asthenia have been reported; rarely, liver function impairment, dermatologic reactions, or hematologic reactions have been reported in humans.
Reproductive/nursing Safety
In humans, the FDA categorizes glimepiride as a category C drug for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans). In rabbits and rats, glimepiride did not cause teratogenic effects when given at high dosages. There were some intrauterine deaths when maternal hypoglycemia was induced by the drug.
Some glimepiride is excreted into maternal milk of rats. The manufacturer states to discontinue the drug in nursing, human mothers.
overdosage/acute toxicity
Overdoses may result in hypoglycemia, ranging from mild to severe. Treatment consists of glucose administration and intensive monitoring. Because of the drug’s long duration of activity, patients may need to be supported with glucose for a least 48 hours post-ingestion, even after apparent recovery.
Drug interactions
The following drug interactions have either been reported or are theoretical in humans or animals receiving glimepiride and may be of significance in veterinary patients:
antiFungalS, azole (ketoconazole, itraconazole, fluconazole): May increase plasma levels of glimepiride
beta-blocKeRS: May potentiate hypoglycemic effect
cHloRampHenicol: May displace glimepiride from plasma proteins
coRticoSteRoiDS: May reduce efficacy
DiuReticS, tHiaziDe: May reduce hypoglycemic efficacy
iSoniaziD: May reduce hypoglycemic efficacy
niacin: May reduce hypoglycemic efficacy
pHenotHiazineS: May reduce hypoglycemic efficacy
pHenytoin: May reduce hypoglycemic efficacy
SulFonamiDeS: May displace glimepiride from plasma proteins
SympatHomimetic agentS: May reduce hypoglycemic efficacy
WaRFaRin: May displace glimepiride from plasma proteins
laboratory considerations
No specific laboratory interactions or considerations were noted.
Doses
catS: For treatment of NIDDM:
a) 2 mg (total dose) per cat once daily (Bruyette 2004)
b) 1 – 2 mg (total dose per cat) PO once daily (Scherk 2005c)
monitoring
Efficacy: Standard methods of monitoring efficacy for diabetes treatment should be followed (e.g., fasting blood glucose, appetite, attitude, body condition, PU/PD resolution and, perhaps, serum fructosamine and/or glycosylated hemoglobin levels)
Adverse effects
client information
Clients should understand the “investigational” nature of using this drug in cats and report any untoward effects to the veterinarian.
chemistry/Synonyms
A sulfonylurea antidiabetic agent, glimepiride occurs as a white to yellowish-white, crystalline, odorless to practically odorless powder. It is practically insoluble in water.
Glimepiride may also be known as: HOE-490, Amarel®, Amaryl®, Amarylle®, Euglim®, Glimepil®, Solosa®, and Roname®.
Storage/Stability/compatibility
Glimepiride tablets should be stored between 15 – 30°C (59 – 86°F) in well closed containers.
Dosage Forms/Regulatory Status
VeteRinaRy-labeleD pRoDuctS: None
Human-labeleD pRoDuctS: Glimepiride Tablets: 1 mg, 2 mg, & 4 mg; Amaryl® (Aventis); generic; (Rx)