Liraglutide
| Liraglutide | ||
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| Mass / length primary structure | 31 amino acids , 3751 Da | |
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| Drug information | ||
| ATC code | A10 BJ02 | |
| DrugBank | DB06655 | |
| Drug class | Antidiabetic drug | |
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| EC number |
810-818-7 |
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Liraglutide is a drug that is marketed under the name Victoza as a drug against type 2 diabetes and under the name Saxenda for weight loss in the case of obesity and overweight. A combination drug consisting of liraglutide and insulin is available internationally under the name Xultophy , but the latter has been withdrawn from the market in Germany. The only manufacturer of liraglutide is the Danish pharmaceutical company Novo Nordisk .
application
Liraglutide is used as a subordinate drug in type 2 diabetes, for example when metformin is not tolerated or does not achieve the desired effect. Liraglutide can be used as monotherapy and also in combination with various other antidiabetic agents.
The drug is sold in a pre-filled pen and is injected under the skin ( subcutaneously ) by the patient himself / herself once a day . The recommended dose is 1.2 or 1.8 mg. Liraglutide must be crept in with a starting dose of 0.6 mg for at least a week. For use in type 2 diabetes, it is covered by health insurance companies. As a drug that is supposed to support weight loss, it should be injected at a dose of 3.0 mg daily after several weeks of creeping up. In contrast to other slimming products, it requires a prescription for overweight . The prescription is permissible above a body mass index of 30, in the case of concomitant diseases from 27. However, for the purpose of weight loss, it is not covered by health insurance companies. The patient has to bear the costs himself, in the EU they are around € 290 per month for 3 mg per day (as of 2019). When used against obesity, it is recommended to discontinue the treatment if the patient has not lost at least 5% of his body weight after 12 weeks.
effect
Liraglutide is a branched-chain peptide with the empirical formula C 172 H 265 N 43 O 51 . It is a genetically engineered analogue of incretin GLP-1 . The sequence homology is 97%. Lys 34 was replaced by Arg and a C16 fatty acid was attached to Lys 26 via a Glu spacer. These modifications made it possible to greatly extend the half-life of GLP-1 (2 minutes) to 13 hours. The fatty acid was used because it binds to albumin , which increases the retention time in the plasma.
It has an antidiabetic effect by increasing the release of insulin from the beta cells of the pancreas and reducing the release of glucagon from the alpha cells and thus the release of glucose from the liver. It also increases the body's cells' sensitivity to insulin, delays gastric emptying and thus the speed with which glucose can get into the blood. It sends heightened satiety messages to the brain that reduce hunger. Since it only develops its full effect when the glucose level is increased, hypoglycaemia is less common with liraglutide than with some other antidiabetic drugs.
Side effects
Common side effects are (nevertheless) hypoglycaemia, as well as nausea, diarrhea, dizziness, abdominal pain and pain at the injection site. Serious side effects are very rare, including medullary thyroid cancer, angioedema, pancreatitis, gallbladder disease, and kidney problems. Use during pregnancy and breastfeeding has not been researched and is therefore not recommended. Since it slightly delays gastric emptying, it can affect the absorption of concomitantly administered drugs.
history
Liraglutide was approved for medical use in Europe in 2009 and the US in 2010. In 2016, it was the 188th most-prescribed drug in the US with more than 3 million drugs prescribed. It is now recognized worldwide as one of the most important, most effective and low-risk drugs for reducing overweight and obesity.
The closely related successor to liraglutide, semaglutide , is being developed as the first GLP-1 receptor agonist in tablet form (orally). In January 2020, semaglutide received a positive recommendation from the European Medicines Agency (EMA) for approval in the EU. The European Commission usually follows this recommendation.
Individual evidence
- ↑ a b CaymanChem: Liraglutide , accessed on 3 December of 2019.
- ^ A b c Ulrich Schwabe, Dieter Paffrath: Drug Ordinance Report 2010 Current data, costs, trends and comments . Springer-Verlag, 2011, ISBN 978-3-642-13380-0 , pp. 79 ( limited preview in Google Book search).
- ↑ a b Wolfgang Piper: Internal medicine . Springer-Verlag, 2012, ISBN 978-3-642-33108-4 , pp. 970 ( limited preview in Google Book search).
- ↑ Meeting highlights from the Committee for Medicinal Products for Human Use (CHMP) 27-30 January 2020 EMA PM of January 31, 2020, accessed on February 3, 2020.