Metformin hydrochloride

Exposure related observations in humans: other data

Administrative data

Endpoint:

exposure-related observations in humans: other data

Type of information:

other: Pharmacological Dose in Humans

Adequacy of study:

weight of evidence

Reliability:

1 (reliable without restriction)

Rationale for reliability incl. deficiencies:

other: see Remark

Remarks:

Metformin hydrochloride is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose by decreasing hepatic glucose production and intestinal absorption of glucose, and improving insulin sensitivity via increased peripheral glucose uptake and utilization (FDA, 2008). The pharmacological activity of Metformin hydrochloride leads to the lowest therapeutic dose of 500 mg/day.

Data source

Reference

Reference Type:

study report

Title:

Unnamed

Year:

2008

Report date:

2001

Materials and methods

Type of study / information:

Data from clinical studies in humans.

Endpoint addressed:

repeated dose toxicity: oral

Test guideline

Guideline:

other: Guidelines for clinical studies

Test material

Test material information

Constituent 1

Reference substance name:

Metformin hydrochloride

EC Number:

214-230-6

EC Name:

Metformin hydrochloride

Cas Number:

1115-70-4

Molecular formula:

C4H11N5.ClH

IUPAC Name:

N,N-dimethylimidodicarbonimidic diamide hydrochloride

Test material form:

solid: bulk

Remarks:

migrated information: powder

Method

Ethical approval:

confirmed, but no further information available

Details on study design:

The lowest therapeutic dose of Metformin hydrochloride was investigated based on data from the literature and own expertise.

Results and discussion

Results:

Metformin hydrochloride is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose by decreasing hepatic glucose production and intestinal absorption of glucose, and improving insulin sensitivity via increased peripheral glucose uptake and utilization (FDA, 2008). The pharmacological activity of Metformin hydrochloride leads to the lowest therapeutic dose of 500 mg/day.

Any other information on results incl. tables

From Product information of Metformin hydrochloride:

The usual starting dose is 500 mg or 850 mg metformin hydrochloride 2 or 3 times daily given during or after meals.

After 10 to 15 days the dose should be adjusted on the basis of blood glucose measurements. A slow increase of dose may improve gastrointestinal tolerability.

In patients receiving a high metformin hydrochloride dose (2 to 3 grams per day), it is possible to replace two Glucophage 500 mg film-coated tablets with one Glucophage 1000 mg film-coated tablet. The maximum recommended dose of metformin hydrochloride is 3 g daily, taken as 3 divided doses.

Applicant's summary and conclusion

Conclusions:

The minimum pharmacological dose of metformin in humans is 500 mg

Executive summary:

Metformin hydrochloride is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes, lowering both basal and postprandial plasma glucose by decreasing hepatic glucose production and intestinal absorption of glucose, and improving insulin sensitivity via increased peripheral glucose uptake and utilization (FDA, 2008). The pharmacological activity of Metformin hydrochloride leads to the lowest therapeutic dose of 500 mg/day.