Vildagliptin

Uses and Administration

Like sitagliptin ( Refer to ), vildagliptin is an inhibitor of dipeptidylpeptidase-4 and is used in the treatment of type 2 diabetes mellitus ( Refer to ). It is given orally in a usual dose of 50 mg twice daily with or without food. A total daily dose of more than 100 mg of vildagliptin is not recommended. When given with metformin and a sulfonylurea, the usual dose of vildagliptin may be used; in dual therapy with a sulfonylurea, a dose of vildagliptin 50 mg once daily in the morning is recommended because higher doses were found to be no more effective. The dose of sulfonylurea may need to be lowered when used with vildagliptin. Dosage may need to be adjusted in patients with renal impairment (see Refer to ).

(last reviewed 2013-04-26; last modified 2013-05-14)

References.

(last reviewed 2013-04-26; last modified 2011-11-23)

References

1. Pratley RE, et al.. Management of type 2 diabetes in treatment-naive elderly patients: benefits and risks of vildagliptin monotherapy.Diabetes Care. 2007; 30: 3017–22. PubMed

2. Scherbaum WA, et al.. Evidence that vildagliptin attenuates deterioration of glycaemic control during 2-year treatment of patients with type 2 diabetes and mild hyperglycaemia.Diabetes Obes Metab. 2008; 10: 1114–24. PubMed

3. Croxtall JD, Keam SJ. Vildagliptin: a review of its use in the management of type 2 diabetes mellitus.Drugs. 2008; 68: 2387–2409. PubMed

4. Banerjee M, et al.. Vildagliptin in clinical practice: a review of literature.Expert Opin Pharmacother. 2009; 10: 2745–57. PubMed

5. Matthews DR, et al.. Vildagliptin add-on to metformin produces similar efficacy and reduced hypoglycaemic risk compared with glimepiride, with no weight gain: results from a 2-year study.Diabetes Obes Metab. 2010; 12: 780–9. PubMed

6. Keating GM. Vildagliptin: a review of its use in type 2 diabetes mellitus.Drugs. 2010; 70: 2089–2112. PubMed

7. Schweizer A, et al.. Clinical experience with vildagliptin in the management of type 2 diabetes in a patient population ≥ 75 years: a pooled analysis from a database of clinical trials.Diabetes Obes Metab. 2011; 13: 55–64. PubMed

8. Baetta R, Corsini A. Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences.Drugs. 2011; 71: 1441–67. PubMed

Administration in renal impairment

UK licensed product information says that no dose adjustment is required in patients with mild renal impairment (creatinine clearance 50 mL/min or more). In patients with more severe renal impairment or with end-stage renal disease (ESRD), the recommended oral dose of vildagliptin is 50 mg once daily.

(last reviewed 2013-04-26; last modified 2012-03-27)

Adverse Effects, Treatment and Precautions

As for Sitagliptin Phosphate, Refer to . Arthralgia has also been reported for vildagliptin. Dosage should be reduced in patients with moderate or severe renal impairment or end-stage renal disease.

Rare cases of hepatic dysfunction, including hepatitis, have been reported. Vildagliptin should not be used in patients with hepatic impairment; liver function should be tested before starting the drug, and monitored during therapy (every 3 months in the first year and periodically thereafter). Vildagliptin should be stopped if there is a persistent increase of 3 or more times the upper limit of normal in alanine aminotransferase (ALT) or aspartate aminotransferase (AST), or if the patient develops jaundice or other signs of liver dysfunction; in such cases, it should not be restarted.

(last reviewed 2013-04-26; last modified 2012-03-23)

References.

(last reviewed 2013-04-26; last modified 2011-10-25)

Overdosage

In the UK, the National Poisons Information Service states that oral activated charcoal may be considered in adults and children who have ingested more than 15 mg/kg of vildagliptin and present within 1 hour, provided they are conscious and the airway can be protected. Hypoglycaemia should be treated with urgency; the general management of hypoglycaemia is described under insulin (see Refer to ).

(last reviewed 2013-04-26; last modified 2011-10-25)

Interactions

The efficacy of vildagliptin may be affected by other drugs that have an independent effect on blood glucose. For more details and examples of drugs that can increase or decrease blood-glucose concentrations, see Interactions under Sulfonylureas, Refer to .

(last reviewed 2013-04-26; last modified 2013-04-29)

Pharmacokinetics

Vildagliptin is rapidly absorbed from the gastrointestinal tract and peak plasma concentrations occur about 1.7 hours after an oral dose. It has a bioavailability of 85%. About 69% of a dose is metabolised, mainly by hydrolysis in the kidney. About 85% of a dose is excreted in the urine (23% is unchanged drug), and 15% in the faeces. The elimination half-life of vildagliptin is about 2 hours after intravenous injection, and about 3 hours after an oral dose.

(last reviewed 2013-04-26; last modified 2011-10-25)

References.

(last reviewed 2013-04-26; last modified 2013-05-03)

References

1. He Y-L. Clinical pharmacokinetics and pharmacodynamics of vildagliptin.Clin Pharmacokinet. 2012; 51: 147–62. PubMed

Hepatic impairment

Although much of a dose of vildagliptin is hydrolysed by the kidney, the liver is also an important site for its metabolism. A small pharmacokinetic study1 found that exposure to vildagliptin was decreased in subjects with mild (Child-Pugh score 5 or 6) or moderate (score 7 to 9) hepatic impairment, and increased in those with severe impairment (score 10 to 12), compared with healthy subjects. However, the differences were less than 30% and not consistent with the severity of hepatic impairment. The authors did not consider the differences to be clinically meaningful and concluded that initial dose adjustment of vildagliptin would not be necessary. Nevertheless, licensed product information cautions against its use in diabetic patients with hepatic impairment (see Refer to ).

(last reviewed 2013-04-26; last modified 2009-09-23)

References

1. He Y-L, et al.. The influence of hepatic impairment on the pharmacokinetics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin.Eur J Clin Pharmacol. 2007; 63: 677–86. PubMed

Preparations: Single-Ingredient

The following preparations list represents a compilation of all available salt forms or related substances for this drug product.

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

ARGENTINA: Galvus; Glucemix; Zomarist;AUSTRALIA: Galvus;AUSTRIA: Galvus;BELGIUM: Galvus;BRAZIL: Galvus;CHILE: Galvus; Jalra;CHINA: Galvus (佳维乐);CZECH REPUBLIC: Galvus; Jalra; Xiliarx;DENMARK: Galvus; Jalra;FINLAND: Galvus;FRANCE: Galvus;GERMANY: Galvus¤; Jalra¤;GREECE: Galvus; Jalra; Xiliarx¤;HONG KONG: Galvus;HUNGARY: Galvus;INDIA: Galvus;INDONESIA: Galvus;IRELAND: Galvus; Jalra¤; Xiliarx¤;ISRAEL: Galvus;ITALY: Galvus;JAPAN: Equa;MALAYSIA: Galvus;MEXICO: Galvus; Xiliarxs;NETHERLANDS: Galvus; Jalra; Xiliarx;NORWAY: Galvus;NEW ZEALAND: Galvus;PHILIPPINES: Galvus; Proglin;POLAND: Agnis; Galvus; Glypvilo; Jalra; Saxotin;PORTUGAL: Galvus; Jalra; Xiliarx;RUSSIAN FEDERATION: Galvus (Галвус);SOUTH AFRICA: Galvus;SINGAPORE: Galvus;SPAIN: Galvus; Jalra; Xiliarx;SWEDEN: Galvus;SWITZERLAND: Galvus;THAILAND: Galvus;TURKEY: Galvus;UNITED KINGDOM: Galvus;UKRAINE: Galvus (Гальвус);

Preparations: Multi-Ingredient

The following preparations list represents a compilation of all available salt forms or related substances for this drug product.

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

ARGENTINA: Galvus Met; Glucemix Met; Zomarist Met;AUSTRALIA: Galvumet;AUSTRIA: Eucreas;BELGIUM: Eucreas;BRAZIL: Galvus Met;CHILE: Galvus Met; Jalra M;CHINA: Eucreas (宜合瑞);CZECH REPUBLIC: Eucreas; Icandra; Zomarist;DENMARK: Eucreas;FINLAND: Eucreas;FRANCE: Eucreas;GERMANY: Eucreas¤; Icandra¤;GREECE: Eucreas; Icandra¤; Zomarist;HONG KONG: GalvusMet;HUNGARY: Eucreas;INDIA: Galvus Met;INDONESIA: Galvusmet;IRELAND: Eucreas; Icandra¤; Zomarist;ISRAEL: Eucreas;ITALY: Eucreas;JAPAN: EquMet;MALAYSIA: Galvus Met;MEXICO: Galvus Met; Jalra-M; Xiliarxs Duo;NETHERLANDS: Eucreas; Icandra; Zomarist;NORWAY: Eucreas;PHILIPPINES: Galvusmet; ProglinMet;POLAND: Eucreas; Vilspox; Zomarist;PORTUGAL: Eucreas; Icandra; Zomarist;RUSSIAN FEDERATION: Galvus Met (Галвус Мет);SOUTH AFRICA: Galvus Met;SINGAPORE: Galvusmet;SPAIN: Eucreas; Icandra; Zomarist;SWEDEN: Eucreas;SWITZERLAND: Galvumet;THAILAND: Galvus Met;TURKEY: Galiptin Met; Galvus Met;UNITED KINGDOM: Eucreas;UKRAINE: Galvusmet (Гальвусмет);

Therapeutic Use

• Antidiabetics

Last Updated 1/21/20