Vildagliptin apollo Vildagliptin apollo Vildagliptin apollo Vildagliptin

Transcription

1 Vildagliptin apollo Vildagliptin apollo Vildagliptin apollo Vildagliptin CAS Number : Molecular Weight : g/mol Molecular Formula : C17H25N3O2 Systematic (IUPAC) : (2S)-1-{2-[(3- hydroxyadamantan-1-yl)amino]acetyl}pyrrolidine-2- carbonitrile Type : small molecule Description : Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-

2 diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions. Categories Hypoglycemic Agents Antidiabetic Taxonomy Kingdom : Organic Classes : Adamantanes Substructures Hydroxy Compounds Aliphatic and Aryl Amines Amino Ketones Nitriles and Derivatives Pyrrolidines Adamantanes Cyanides Alcohols and Polyols

3 Heterocyclic compounds Carboxamides and Derivatives Cyclooctane and Derivatives Pharmacology Indication : Used to reduce hyperglycemia in type 2 diabetes mellitus. Pharmacodynamics : Vildagliptin belongs to a class of orally active antidiabetic drugs (DPP-IV inhibitors) that appear to have multiple functional benefits beyond simple blood-glucose control. One of these is a potential protective effect on pancreatic beta cells, which deteriorate in diabetes. Vildagliptin appears to be safe, very well tolerated, and efficacious. Following a meal, gut incretin hormones are released. The most important incretin hormones are GLP-1 and glucose-dependent insulinotropic polypeptide (GIP). These hormones, secreted in the human small intestine, are responsible for insulin release due to increased glucose levels. In contrast to agents that promote insulin secretion via glucose-independent mechanisms, GLP-1's dependence on glucose concentration is considered beneficial due to a lower risk of hypoglycemia. GLP-1 also inhibits glucagon secretion and increases beta cell mass by stimulating proliferation and neogenesis. However, the clinical utility of GLP-1 is limited by its short half-life (2 minutes). GLP-1 is rapidly degraded by the proteolytic enzyme DPP-IV. To enhance GLP-1 activity, inhibition of the DPP-IV enzyme is emerging as a novel therapeutic approach in the treatment of diabetes. Administration of vildagliptin enhances GLP-1's ability to produce insulin

4 in response to elevated concentrations of blood glucose, inhibit the release of glucagon following meals, slow the rate of nutrient absorption into the bloodstream, slow the rate of gastric emptying, and reduce food intake. Mechanism of action : Vildagliptin inhibits dipeptidyl peptidase-4 (DPP-4). This in turn inhibits the inactivation of GLP-1 by DPP-4, allowing GLP-1 to potentiate the secretion of insulin in the beta cells. Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through degradation of GIP and the degradation of GLP-1. Absorption : Rapidly absorbed following oral administration with an oral bioavailability of greater than 90%. Protein binding : 9.3% Half life : The elimination half-life is approximately 90 minutes. Affected organisms : Humans and other mammals What is it used for? Type 2 diabetes (non-insulin dependent diabetes). Vidagliptin is used for people with type 2 diabetes whose blood sugar is not sufficiently controlled by other antidiabetic medicines. It can be added to treatment with metformin; a sulphonylurea, for example gliclazide; or another type of antidiabetic medicine known as a

5 thiazolidinedione, for example pioglitazone or rosiglitazone. Warning! Hypoglycaemia (low blood glucose) has been commonly reported when this medicine is used in combination with metformin or sulphonylurea medicines, eg glimepiride. Symptoms of hypoglycaemia usually occur suddenly and may include cold sweats, cool pale skin, tremor, anxious feeling, unusual tiredness or weakness, confusion, difficulty in concentration, excessive hunger, temporary vision changes, headache, nausea and palpitations. You should talk to your doctor or diabetes specialist about this and make sure you know what to do if you experience these symptoms. Your ability to concentrate or react may be reduced if you have low blood sugar, and this can cause problems driving or operating machinery. You should take precautions to avoid low blood sugar when driving - discuss this with your doctor. This medicine may also cause dizziness or fatigue. If affected you should take care driving or operating machinery. People with diabetes have a higher risk of developing foot ulcers and blistering of the skin. It is therefore important to have a good foot care routine. Consult your doctor if you get any new blisters or ulcers while taking this medicine. Rare cases of inflammation of the liver (hepatitis) have been reported in people taking this medicine. For this reason, your liver function should be checked before starting treatment, every three months during the first year of treatment, and regularly thereafter. You should consult your doctor if you develop any of the following

6 symptoms while taking this medicine, so that your liver can be checked: unexplained nausea, vomiting, abdominal pain, fatigue, loss of appetite, darkened urine or yellowing of the eyes or skin (jaundice). Use with caution in People with mild heart failure. People taking ACE inhibitor medicines, eg captopril. Not to be used in Type 1 diabetes. Diabetic ketoacidosis. Decreased liver function. Pregnancy. Breastfeeding. This medicine is not recommended for people receiving dialysis or who have moderate to severe kidney disease. This medicine is not recommended for people with severe heart failure. This medicine is not recommended for children and adolescents under 18 years of age because it has not been studied in this age group. This medicine contains lactose and should not be taken by people with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucosegalactose malabsorption. This medicine should not be used if you are allergic to one or any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy. If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.

7 Pregnancy and breastfeeding Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine. The safety of this medicine for use during pregnancy has not been established. It should not be used during pregnancy. Diabetes mellitus is usually controlled using insulin during pregnancy, because this provides a more stable control of blood sugar. If you get pregnant while taking this medicine, or are planning a pregnancy, you should seek medical advice from your doctor. It is not known if this medicine passes into breast milk. The manufacturer states that it should not be used by breastfeeding mothers. Seek medical advice from your doctor. Side effects Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Just because a side effect is stated here does not mean that all people using this medicine will experience that or any side effect. Common (affect between 1 in 10 and 1 in 100 people)- Tremor (when used with metformin or a sulphonylurea). Headache (when used with metformin or a sulphonylurea).

8 Dizziness (when used with metformin or a sulphonylurea). Low blood sugar levels (when used with metformin or a sulphonylurea). Nausea (when used with metformin). Feeling weak (when used with a sulphonylurea). Weight gain (when used with a glitazone). Swelling of the legs and ankles due to excess fluid retention (when used with a glitazone). Uncommon (affect between 1 in 100 and 1 in 1000 people)- Fatigue (when used with metformin). Constipation (when used with a sulphonylurea). Headache (when used with a glitazone). Feeling weak (when used with a glitazone). Rare (affect between 1 in 1000 and 1 in 10,000 people)- Changes in liver function. Inflammation of the liver (hepatitis). Allergic reaction called angioedema, which may involve swelling of the face, tongue or throat, difficulty swallowing or breathing, rash or hives (stop taking this medicine and consult your doctor immediately if you experience these symptoms). Very rare (affects less than 1 in 10,000 people)- Inflammation of the nose and throat, causing a blocked or runny nose and sore throat (nasopharyngitis). The side effects listed above may not include all of the side effects reported by the medicine's manufacturer.

9 For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist. How can this medicine affect other medicines? It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with this medicine. Similarly, check with your doctor or pharmacist before taking any new medicines while taking this one, to ensure that thecombination is safe. Medicines that increase blood sugar levels as a side effect may make this medicine, and other antidiabetic medicines, less effective at controlling blood sugar. Medicines that can increase blood sugar levels include the following: bronchodilators (beta agonists), eg salbutamol, terbutaline, salmeterol corticosteroids, eg prednisolone levothyroxine thiazide diuretics, eg bendroflumethiazide. Other medicines containing the same active ingredient There are currently no other medicines available in the india that contain vildagliptin as the only active ingredient. Eucreas contains vildagliptin in combination with metformin.

10 apollo asia Division APOLLO Pharmaceuticals API Manufacturer INDIA [P] Ltd. asia Division Mr.Vipin Saxena CEO Cellular: Cellular: Direct : FAX : Wireline Purchase HELPDESK: Wireline Sales HELPDESK: Wireless 24x7 HELPDESK: Blackberry Pin : 32E6500D 32E C58 apollo@hotmail.co.in Sales@apollopharma.in Export@apollopharma.in purchase@apollopharma.in Chat: MSN Hotmail:VipinrSaxena Skype NAME:VipinrSaxena Rocketmail:VipinrSaxena

11 Google mail:vipinrsaxena BlackBerry:28415C58 Regd. Office :- 1104, Maker Chamber V, Nariman Point Mumbai, INDIA Pin: Industrial Office D-62, OIC India Oshiwara Industrial Centre, New Link Road, Goregoan West, Mumbai, INDIA Pin: Manufacturing Unit Address: Plot No. 117A, Village: Chamble Near MonaTona Limited.Wada, Maharashtra, PIN : INDIA apollo@hotmail.co.in Sales@apollopharma.in Export@apollopharma.in purchase@apollopharma.in

12

13

14