Glyburide by Abhishek Jaguessar

8/4/2019 Glyburide by Abhishek Jaguessar

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Glyburide (micronase, glynase, DiaBeta)

shows promise for women withgestational diabetes and pregnantwomen with type 2 diabetes

BY

ABHISHEK JAGUESSAR



• What about women with

type 2 diabetes, who aretaking diabetes pills, orwomen who have hadgestational diabetes in thepast?

• Will they need insulin, orwill diabetes pills be okay to

use during pregnancy?



glyburide

Glyburide is a sulfonylurea drug used to lowerblood sugar levels in people with type 2

diabetes(non-insulin-dependent)

Glyburide appears to lower the blood glucoseacutely by stimulating the release of insulin from

the pancreas, an effect dependent upon

functioning beta cells in the pancreatic isletsglyburide, a type of sulfonylurea drug, does not

pass through the placenta



Pharmacokinetics

• C23H28ClN3O5S glyburide

• Single dose studies with glyburide tabletsin normal subjects demonstrate significantabsorption of glyburide within 1 hour, peak

drug levels at about 4 hours (2-3 hours formicronized glyburide), and low butdetectable levels at 24 hours

• Glyburide• Also indexed as: Diabeta®, Glynase

,Prestab®, Micronase®, Pres Tab®



Sulfonylureas – First-Generation Agents:

• Generic Name: acetohexamide

Brand Name: Dymelor • Generic Name: chloropropamideBrand Name: Diabinese

• Generic Name: tolazamideBrand Name: Tolinase

• Generic Name: tolbutamide

Brand Name: Orinase • Second-Generation Agents:• Generic Name: glimepiride

Brand Name: Amaryl • Generic Name: glipizide

Brand Names: Glucotrol ,Glucotrol XL

• Generic Name: glyburideBrand Names: DiaBeta, Micronase ,Glynase

• Combination Agents:• Generic Name: glyburide plus metformin

Brand Name: GlucoVance

http://www.diabetesmonitor.com/amaryl.htm

http://www.diabetesmonitor.com/metf-qa.htm

http://www.glucovance.com/

http://www.glucovance.com/

http://www.diabetesmonitor.com/metf-qa.htm

http://www.diabetesmonitor.com/amaryl.htm



dosage

• There is no fixed dosage regimen for themanagement of diabetes mellitus with glyburideor any other hypoglycemic agent. In addition to

the usual monitoring of urinary glucose, thepatient's blood glucose must also be monitoredperiodically to determine the minimum effectivedose for the patient

• Glyburide may be taken with food to avoidgastrointestinal (GI) upset



• Glyburide is a white, crystalline compound,formulated

• as Micronase tablets of• 1.25, 2.5, and 5 mg strengths for oral

administration.

• The usual starting dose of standard glyburide

tablets is 2.5-5 mg daily• (micronized glyburide tablets: 1.5-3 mg daily),

• administered with breakfast or the first mainmeal. Those patients who may be moresensitive to hypoglycemic drugs should bestarted at 1.25 mg of standard glyburide daily(0.75 mg for micronized glyburide daily).



Maximum Dose

• Standard Glyburide: Daily doses of morethan 20 mg are not recommended.

• Micronized Glyburide: Daily doses of morethan 12 mg are not recommended

• glyburideSU generic Intermediate

acting1.25, 2.5, 5mg5 - 20mg



Dosage Interval

• Standard Glyburide: Once-a-day therapy is usually satisfactory. Some patients,particularly those receiving more than 10 mg

daily, may have a more satisfactory response with twice-a-day dosage .

• Micronized Glyburide: Once-a-day therapy is usually satisfactory. Some patients,

particularly those receiving more than 6 mg daily, may have a more satisfactory response with twice-a-day dosag



CONTRAINDICATIONS

• Glyburide Tablets are Contraindicated inPatients with:

• 1. Known hypersensitivity or allergy to the

drug.• 2. Diabetic ketoacidosis, with or without

coma. This condition should be treated

with insulin.• 3. Type I diabetes mellitus, as sole

therapy.



Pregnancy

• , Effects Teratogenic , Pregnancy Category B • Reproduction studies have been performed in rats and

rabbits at doses up to 500 times the human dose and haverevealed no evidence of impaired fertility or harm to thefetus due to glyburide. There are, however, no adequate

and well-controlled studies in pregnant women. Becauseanimal reproduction studies are not always predictive ofhuman response, this drug should be used duringpregnancy only if clearly needed.

• Effects Nonteratogenic

• :4-10 days Prolonged severe hypoglycemia (has beenreported in neonates born to mothers who were receiving asulfonylurea drug at the time of delivery. This has beenreported more frequently with the use of agents withprolonged half-lives. If glyburide is used during pregnancy, it

should be discontinued at least 2 weeks before the expecteddelivery date.



HOW SUPPLIED

Micronase Tablets are Supplied as Follows • Micronase Tablets 1.25 mg: White, round, scored and imprinted

MICRONASE 1.25.• Micronase Tablets 2.5 mg: Dark pink, round, scored and

imprinted MICRONASE 2.5.• Micronase Tablets 5 mg: Blue, round, scored and imprinted

MICRONASE 5. Storage: Store at controlled room temperature 20-25°C (68-77°F).

Keep container tightly closed. Dispensed in well-closed containerswith safety closures.

Glynase PresTab Tablets are Supplied as Follows

• Glynase PresTab Tablets 1.5 mg: White, ovoid, imprintedGLYNASE 1.5/PT Score PT, contour, scored.• Glynase PresTab Tablets 3mg: Blue, ovoid, imprinted

GLYNASE 3/PT Score Pt, contour, scored.• Glynase PresTab Tablets 6 mg: Yellow, ovoid, imprinted

GLYNASE 6/PT Score PT, contour,



• insulin is considered the drug ofchoice for the treatment of

gestational diabetes; however, it isexpensive and its administration is

inconvenient• "Women with gestational diabetes

mellitus are rarely treated with a

sulfonylurea drug, because ofconcern about teratogenicity and

neonatal hypoglycemia .



• . Gestational diabetes is rarely diagnosedduring the first trimester of pregnancy, the

period when organogenesis and moresevere malformations occur. Therefore itseems unlikely that a pregnant femalewould receive treatment for gestational

diabetes during this time period. Eventhough the results of this study showpromise with regards to the use of second-generation sulfonylureas for the treatmentof gestational diabetes, more studies needto be conducted before these medicationscan be considered safe in pregnancy.

A C i f Gl b id d

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11036118&dopt=Abstract




A Comparison of Glyburide and Insulin in Women with Gestational

Diabetes Mellitus. • The new sulphonylurea called glyburide

does not cross the placental barrier









published in The New EnglandJournal of Medicine

Volume 343 October 19, 2000Number 16

• Of the 404 womenwith singleton pregnancies andgestational diabetes that required treatmen , 201received glyburide and 203 received human insulin

• between 11 and 33 weeks of gestation

• The mean (± SD) serum glucose concentrationobserved during routine visits to the clinic was 102 ±24mg/dl in the glyburide group and 99 ±22 mg/dl in

the insulin group .



• In addition, 82% of women in the glyburidegroup and 88% of women in the insulin grouphad home blood glucose measurements that fell

into the desired range

• .No significant differences existed between thetwo groups with regards to perinatal outcome .



• The incidence of macrosomia between thegroups was similar; 11% in the glyburidegroup and 10% in the insulin group

• .The cord serum of all infants wasmeasured for the presence of glyburide;

however, the drug was not detected in anyof the infants .



• There were no significant differences betweenthe glyburide and insulin groups in thepercentage of infants who were large forgestational age (12 percent and 13 percent,

respectively) • who had macrosomia, defined as a birth weight

of 4000 g or more (7 percent and 4 percent• ); who had lung complications (8 percent and 6

percent

• ); who had hypoglycemia (9 percent and 6percent

• who were admitted to a neonatal intensive careunit (6 percent and 7 percent

• who had fetal anomalies (2 percent and 2 percent)

• The cord-serum insulin concentrations weresimilar in the two groups)



REFERENCES

• Langer OD, Conway DL, Berkus MD, XenakisEMJ, and Gonzales O. A comparison ofglyburide and insulin in women with gestational

diabetes. N Engl J Med 2000;343:1134-38.• Greene MF. Oral hypoglycemic drugs for

gestational diabetes. N Engl J Med2000;343:1178-79.

• Briggs GK, Freeman RK, Yaffe SJ, editors.Drugs in Pregnancy and Lactation. 5th ed.Baltimore: Williams & Wilkins. 1998





• The percentage of newborns who werelarge for their gestational age was similarin both groups of women. In addition, there

were no statistically significant differencesin the infants' rates of birth defects, lungcomplications or low blood sugar.



But• We must still exercise caution in

applying these findings to clinical

practice. Results need to beduplicated and the risk for fetalmalformations with the use of

these agents during pregnancyremains a concern."

Glyburide by Abhishek Jaguessar

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