Monograph
A10BH01 - Sitagliptin |
Propably not porphyrinogenic |
PNP |
Rationale
Sitagliptin is devoid of the capacity for Cyp-interaction, and thus for pharmacokinetic porphyrogenicity.
Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in carbohydrate intake. Infections are also a common reported side effect, and infections are well known triggers of acute porphyric attacks.
Chemical description
Trifluorophenyl-triazolpyrazine salt.
Therapeutic characteristics
Sitagliptin is indicated to improve glycaemic control in adult patients with type 2 diabetes mellitus, and can be used in mono therapy or as part of combination therapy with other anti-diabetic drugs.
Sitagliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor. It is administered orally.
The pharmacodynamic effects on glucose homeostasis, with inhibition of pancreatic glucagon release, are theoretically anti-porphyrogenic
Side effects such as nausea and vomiting may be potentially porphyrinogenic through reduction in carbohydrate intake.
Upper respiratory tract infection and nasopharyngitis are also common reported side effects of sitagliptin, and such infections might trigger of acute porphyric attacks.
Metabolism and pharmacokinetics
Approximately 79 per cent of sitagliptin is excreted unchanged in the urine.
Nonclinical studies indicate that the small portion of sitagliptin that undergoes biotransformation is metabolized by Cyp3A4 with the help of Cyp2C8.
In vitro data has shown that sitagliptin is not an inhibitor of CYP isozymes CYP3A4, 2C8, 2C9, 2D6, 1A2, 2C19 or 2B6, and is not an inducer of CYP3A4 and CYP1A2
References
# | Citation details | PMID |
---|---|---|
* | Scientific articles | |
1. | Pharmacokinetics of dipeptidylpeptidase-4 inhibitors.
Scheen AJ. Diabetes Obes Metab. 2010 Aug; 12(8):648-58. |
20590741 |
2. | Sitagliptin phosphate: a DPP-4 inhibitor for the treatment of type 2 diabetes mellitus.
Zerilli T, Pyon EY et al. Clin Ther. 2007 Dec;29(12):2614-34. |
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* | Drug reference publications | |
3. | McEvoy GK, editor. Sitagliptin phosphate. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (06.12.2012).
|
|
* | Summary of Product Characteristics | |
4. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Januvia.
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Netherlands
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Januvia · Januvia 100 mg compr. pellic. · Januvia 25 mg compr. pellic. · Januvia 50 mg compr. pellic. · Ristaben · Ristaben 100 mg compr. pellic. · Ristaben 25 mg compr. pellic. · Ristaben 50 mg compr. pellic. · Ristfor · Ristfor 50 mg - 1 000 mg compr. pellic. · Ristfor 50 mg - 850 mg compr. pellic. · Sitagliptin · Sitagliptin Accord 100 mg compr. pellic. · Sitagliptin Accord 25 mg compr. pellic. · Sitagliptin Accord 50 mg compr. pellic. · Sitagliptin EG 100 mg compr. pellic. · Sitagliptin Grindeks 100 mg compr. pellic. · Sitagliptin Grindeks 25 mg compr. pellic. · Sitagliptin Grindeks 50 mg compr. pellic. · Sitagliptin Sandoz 100 mg compr. pellic. · Sitagliptin Sandoz 25 mg compr. pellic. · Sitagliptin Sandoz 50 mg compr. pellic. · Sitagliptin Sun 100 mg compr. pellic. · Sitagliptin Sun 25 mg compr. pellic. · Sitagliptin Sun 50 mg compr. pellic. · Sitagliptine · Sitagliptine AB 100 mg compr. pellic. · Sitagliptine AB 25 mg compr. pellic. · Sitagliptine AB 50 mg compr. pellic. · Sitagliptine Krka 100 mg compr. pellic. · Sitagliptine Krka 25 mg compr. pellic. · Sitagliptine Krka 50 mg compr. pellic. · Tesavel · Tesavel 100 mg compr. pellic. · Tesavel 25 mg compr. pellic. · Tesavel 50 mg compr. pellic. · Xelevia · Xelevia 100 mg compr. pellic. · Xelevia 25 mg compr. pellic. · Xelevia 50 mg compr. pellic.United Kingdom
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