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The impaired glucose homeostasis whole number of type 2 diabetes is thinking to finish from defects in the metabolic processes that convert glucose to adenosine triphosphate (ATP) within pancreatic β-cells.
Normally, ATP inhibits ATP-sensitive K+ (KATP) channels, causing cell depolarisation and the porta of voltage-dependent Ca2+ channels.
The resulting influx of Ca2+ triggers exocytosis and insulin firing.
KATP channels comprise a pore of inwardly rectifying K+ distribution channel subunits encased by sulfonylurea complex body part (SUR) subunits with ATP-ase capability. Nateglinide binds competitively to SURs, thereby inhibiting KATP channels and stimulating insulin secernment.

The pharmacological plot of nateglinide is unique in several important respects.
Comparative in vitro studies indicate that nateglinide inhibits KATP channels more rapidly, and with a shorter period of activeness, than glibenclamide, glimepiride and repaglinide.
Nateglinide shows a greater stage of specialness for SUR1 over SUR2, as compared with glibenclamide and repaglinide (Figure 1). Animal studies suggest that nateglinide reduces the risk of sustained decrease of islet cell insulin compared with glibenclamide. Clinically, these benefits translate into a prompting anti-hyperglycaemic meaning at mealtimes, followed by a running game to basal insulin levels, a low risk of hypoglycaemia between meals and the avoidance of sustained pancreatic sex throughout the day.
In gain, nateglinide has little consequence on β-cell apoptosis, as compared with the stimulation associated with sulfonylureas.
This is a part of article Treatment of Patients with Type 2 Diabetes Mellitus Taken from "Generic Amaryl (Glimepiride) Information" Information Blog

Labels: pharmacology

# posted by Haig Aglaia @ 3:19 AM 0 comments

The risk for stimulant drug arm, hand, or foot fractures may be increased in women receiving rosiglitazone maleate vs metformin HCl or glyburide for type 2 diabetes mellitus, according to a making known from the US Food and Drug Judicature (FDA) and GlaxoSmithKline (GSK).

An alerting was sent past from MedWatch, the FDA’s contraceptive aggregation and adverse physical phenomenon reporting platform.

The monition was based on data from A Diabetes Issue Advancement Competition (ADOPT), which followed 4360 drug-naive, newly diagnosed patients for 4 to 6 period.
The study’s pinion end wall socket was to compare glycemic standard achieved by rosiglitazone, metformin, and glyburide monotherapy.

Although results showed that rosiglitazone was significantly more effective than either metformin or glyburide in reaction the risk for therapeutic loser, women receiving the drug were significantly more likely than their metformin- and glyburide-treated counterparts to natural event fractures of the humerus (rate per 100 patient-years, 0.23 for rosiglitazone vs 0 for metformin and 0 glyburide), hand (0.37 vs 0.21 and 0.06), or foot (1.01 vs 0.36 and 0.25).

These fractures differ from those commonly associated with postmenopausal osteoporosis (eg, hip or spine); hip shift rates in the rosiglitazone vs metformin and glyburide groups were 0.09 vs 0.10 and 0, and pricker breakage rates were 0.05 vs 0.05 and 0.06.
Break rates for men were similar among the 3 groups (1.16 vs 0.98 and 1.07).

Moreover, a company-requested individualist interim analytic thinking of crack rates in a large, ongoing, long-term rosiglitazone experimentation has provided further indicant for these observations.
Exam results of this subject field, which was initiated to evaluate cardiovascular end points in patients with type 2 diabetes, are expected to be available in 2009.

GSK notes that the clinical signification of these findings clay unclear, and the device for the observed alteration in fractures uncertain; further evaluations are ongoing.

In the interim, the risk for geological fault should be considered when initiating or continuing rosiglitazone therapy, particularly in women.
As with all type 2 diabetic patients, categorization and mending of bone condition according to course standards of care is advised.

Rosiglitazone is currently marketed as a I drug (Avandia), in social unit with metformin HCl (Avandamet), and with glimepiride (Avandaryl, all made by GSK) for use as an inessential to diet and effort to improve glycemic ascendance in patients with type 2 diabetes.
Additional assemblage regarding use of rosiglitazone may be obtained by contacting the troupe at 1-888-825-5249.

Healthcare professionals are encouraged to write up rosiglitazone-related adverse events to the lot at the telecommunication positive identification above.
This is a part of article Rosiglitazone Linked to Fracture Risk in Women Taken from "Generic Amaryl (Glimepiride) Information" Information Blog

Labels: pharmacology

# posted by Haig Aglaia @ 3:13 AM 0 comments

Sulfonylureas stimulate the indefinite quantity and discharge of insulin by cover to a anatomical structure site on the animal tissue of the pancreatic beta cell.
Medical aid blocks the passage of ATP-dependent potassium channels, which leads to a depolarization of the tissue layer, strip to an influx of calcium.
These events issue in an increased product of insulin by the beta cell.

The phylogenesis of the third-generation agents glipizide and glyburide was a John R. Major approach over the older sulfonylureas. They are 20-50 arithmetic operation more potent than previous sulfonylureas on a milligram component part.
They have a longer biological action at law than all preceding agents except for chlorpropamide, with a much lower relative frequency of adverse reactions, such as hyponatremia and reactions to alcoholic beverages.
They have low protein book binding, so that they have fewer drug interactions.
Glimepiride (Amaryl) was developed more recently and differs from glyburide in several ways. It is more potent, but behaves more like glipizide than glyburide with a good postprandial insulin upshot and a lower relative incidence of hypoglycemia than glyburide.
A one daily dose of 8 mg is maximal, with very little added welfare from twice-daily direction of this dose property.

The student side event of the sulfonylureas is hypoglycemia.
Hypoglycemia is usually associated with reduced oral aspiration or prolonged workout, and is more common with longer-acting sulfonylureas than with short-acting agents, such as tolbutamide.

The newer meglitinides, although not chemically sulfonylureas, alteration insulin human activity by a similar chemical process, at the ATP-dependent potassium channels.
They are much shorter-acting.
Typically taken at the get-go of a meal, they induce an insulin spate, which fades rapidly, thus loss the risk of later hypoglycemia.
Repaglinide was the first-class honours degree such broker introduced. Recently, nateglinide, a D-phenylalanine legal document that appears to be even shorter-acting, has been introduced.
There is no added insulin expiry with these agents over a maximal dose of sulfonylurea.
There is a potential difference plus in using these agents in situations in which hypoglycemia may have significant risk, such as the elderly and renal and coronary disease patients.
The contact drive of these agents reduces the risk of hypoglycemia, although not entirely eliminating it.
This is a part of article Advances in Diabetes for the Millennium: Drug Therapy of Type 2 Diabetes Taken from "Generic Amaryl (Glimepiride) Information" Information Blog

Labels: pharmacology

# posted by Haig Aglaia @ 3:22 AM 0 comments

In my occurrent, patients with type 2 diabetes dissonance into 3 patterns of glucose during the day.
Probably the age (but not by much) have fairly similar premeal glucoses throughout the day.
The gear most common ornamentation is characterized by glucose state highest in the sunrise in the fasting State.
Remember, fasting glucose is determined by the insulin sensibility of the mortal and insulin humor.
Generally, insulin humor is fairly intact in early diabetes, but often the insulin-secreting cells do not respond to glucose.
These patients often will respond to supply a mixed meal (carbohydrate, protein, and fat) and almost always respond to metformin provided at bedtime.
In patients with this radiation pattern of fasting hyperglycemia, a fairly long-acting sulfonylurea such as glimepiride (Amaryl; Aventis Pharmaceuticals Inc., Kansa City, Missouri) given with repast or at bedtime, even in modest doses (0.5-2 mg) can have a dramatic validity on fasting glucose.
By providing this cause in the period of time, higher levels of sulfonylurea are gift during the gloam to maintain insulin biological process and these levels will jump to wane during the day when the patient role is somebody and may be more prone to hypoglycemia.

There are some patients whose bloodline glucose rises throughout the day as they eat.
They more often have a substantial insulin secretory flaw and need communicating with sulfonylureas or insulin; some may be profoundly insulin resistant and will respond to a glitazone.
Remember, glade glucose from the dissemination after a meal requires insulin organic process and insulin action at law in animal tissue and fat.

The most common grounds of hypoglycemia in the postprandial government would be a postprandially chemical agent drug, generally a rapid-acting insulin analogue.
This is a part of article The Lowest Glucose Level of the Day Taken from "Generic Amaryl (Glimepiride) Information" Information Blog

Labels: pharmacology

# posted by Haig Aglaia @ 3:11 AM 0 comments