Glybofen 5/1000

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Indication
Oral Anti-Diabetic

Pharmaceutical Form
Film Coated Scored Tablets -

 -Micronized Glyburide 5mg 
 -Metformin HCL 1000mg

1-Glyburide

•    Its Second generation sulfonylureas
•    Possess a more rapid onset of action, and generally have shorter plasma half-lives and longer duration of action compared to the 1st generation agents
Mechanism of Action
•    The drug works by inhibiting ATP-sensitive potassium channels in pancreatic beta cells.
•    This inhibition causes cell membrane depolarization, which causes voltage-dependent calcium channels to open
•     That causes an increase in intracellular calcium in the beta cell, which stimulates insulin release
•    Enhances glucose disposal by peripheral tissues
•    In addition, glyburide augments the extraction of insulin by the liver, and such an effect might prevent the development of sustained high levels of insulin in blood

2-Metformin

•    Its from group of Biguanide
Mechanism of Action

•    The therapeutic uses derive from their tendency to reduce gluconeogenesis in the liver, and as a result, reduce the level of glucose in the blood
•     Metformin also tend to make the cells of the body more willing to absorb glucose already present in the blood stream, and there again reducing the level of glucose in the plasma.
•    Increase cells  insulin sensitivity
•    Decrease intestinal absorption of glucose

Absorption and Bioavailability

Glyburide
-Single-dose studies with glyburide tablets in normal subjects demonstrate significant absorption of glyburide within 1 hour, peak drug levels at about 4 hours, and low but detectable levels at 24 hours
-Mean serum levels of glyburide, as reflected by areas under the serum concentration-time curve, increase in proportion to corresponding increases in dose
-Bioequivalence has not been established between Glybofen and single-ingredient glyburide products

Metformin Hydrochloride
-The absolute bioavailability of 500mg Metformin given under fasting condition is approximately 50 to 60 %
-Food decreases the extent of and slightly delays the absorption of metformin, as shown by approximately a 40% lower peak concentration and a 25% lower AUC in plasma
-35-minute prolongation of time to peak plasma concentration following administration of single 850 mg tablet with food
 

Metabolism and Elimination

Glyburide
-The terminal half-life is about 10 hours.
-The major metabolite of glyburide is the 4-trans-hydroxy derivative. A second metabolite, the 3-cis-hydroxy derivative, also occurs. These metabolites probably contribute no significant hypoglycemic action in humans
-Glyburide is excreted as metabolites in the bile and urine, approximately 50% by each route. This dual excretory pathway is qualitatively different from that of other sulfonylureas, which are excreted primarily in the urine

Metformin Hydrochloride

-Following oral administration 90 % of the absorbed drug is eliminated via renal route
-Plasma elimination half-life 6.2 hours.   In blood 17.6 hours
- Therapeutic indications:
•    Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
•    Initiate therapy with a low dosage an gradually increase the dose based on efficacy and tolerability

- Dose and Method of Administration:
Dose starting by 1/2 of tablet (5/1000= 2,5/500) once daily with the main meal for 1-2 weeks then increase the dose according to therapeutic responses
-The dose should be titrated
-The response to treatment should be evaluated using HbA1C, FPG and PPG to identify the minimum effective dose for each patient
-Never use this medication without your doctors recommendations

Pregnancy and Lactation:
Pregnancy:

•    Glybofen should not be used during pregnancy, unless clearly needed. (See below)
•    There are no adequate and well-controlled studies with pregnant women with Glybofen or its individual components
Lactation:
  • There are no adequate and well-controlled studies with lactating women with Glybofen or its individual components