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Glibenclamide

Hypoglycemic Agents
CATEGORIES

Hypoglycemic Agents, Anti-Arrhythmia Agents, Antidiabetic Agents


ALIASES

Daonil®, Euglucon®, Glibenklamid Recip, Euglucon, Glyburide, Glynase, Micronase, Novo-Glyburide, Semi-Daonil


SUBSTANCES

glibenclamide


ENVIRONMENTAL CONCERN: HIGH
Glyburide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Glyburide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Glyburide appears to be completely metabolized, likely in the liver. Although its metabolites exert a small hypoglycemic effect, their contribution to glyburide's hypoglycemic effect is thought to be clinically unimportant. Glyburide metabolites are excreted in urine and feces in approximately equal proportions. The half-life of glyburide appears to be unaffected in those with a creatinine clearance of greater than 29 ml/min/1.73m2.

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HIGH
In Sweden, glibenclamide has been found in wild fish in concentrations close to therapeutic concentrations in humans, which also is reasonable based on the substance solubility in fat and measured concentration in wastewater. Mechanism based efficacy data is lacking.

Glibenclamide is included in the Stockholm County Council's table of pharmaceuticals with a negative environmental impact according to the environmental programme 2017-2021.

Suggestions on how to reduce the release of glibenclamide
Concrete proposals on how to work to reduce emissions of environmentally harmful pharmaceuticals on the list have been developed in close cooperation with the Stockholm Drug and Therapeutics Committee's expert advice. The action proposals were developed from an environmental perspective. The patient's best always goes first and several pharmaceuticals on the list are also included in the Wise List. However, for such pharmaceuticals, there may be measures that could reduce the environmental impact.

Concrete proposal for glibenclamide:
•Glibenclamide is not recommended in the Wise List.
• Individual pharmaceutical adjustment in the treatment of diabetes mellitus type 2 is important to optimize the treatment and avoid side effects.
• Alternatives may be glimepiride (recommended in the Wise List) or repaglinide (recommended in the Wise List and is better from an environmental point of view than glibenclamide).
• Healthy living habits such as weight loss in obesity, increased physical activity, well-balanced diet and avoiding over-consumption of alcohol could help reduce pharmaceutical use in some patients.

The risk insignificant, according to Fass.se, is calculated on total sold amount (kg) of the substance in Sweden during the year 2015 and the toxicity of the substance, i.e. consideration has not been given to measured levels in the environment.

REFERENCES

  1. Goodpoint. Prioritering av läkemedel med miljörisk inom SLL. Stockholm: Goodpoint; 2016. Rapport LS 2016–0634.
  2. IVL Swedish Environmental Research Institute Ltd. Fick J, Lindberg RH, Kaj L, Brorström-Lundén E. Results from the Swedish National Screening Programme 2010. Subreport 3. Pharmaceuticals.
  3. IVL Swedish Environmental Research Institute Ltd Fick J, Lindberg RH, Fång J, Magnér J, Kaj L, Brorström-Lundén E. Screening 2014. Analysis of pharmaceuticals and hormones in samples from WWTPs and receiving waters. Rapport C 135.
  4. Fick J, Lindberg RH, Tysklind M, Larsson DG. Predicted critical environmental concentrations for 500 pharmaceuticals. Regul Toxicol Pharmacol. 2010;58:516-23.
  5. Stockholms läns landsting. Förteckning över miljöbelastande läkemedel med åtgärdsförslag framtagen inom ramen för SLL:s miljöprogram 2017–2021.
  6. Fass.se för vårdpersonal
  7. Socialstyrelsen. Statistikdatabas för läkemedel.
  8. Stockholms läns landsting. Janusinfo: Läkemedelsuppföljning