JANUVIA ® - Sitagliptin

JANUVIA ® a Sitagliptin-based drug

THERAPEUTIC GROUP: Oral hypoglycemic agents - DPP-4 inhibitors


Indications JANUVIA ® - Sitagliptin

JANUVIA ® is a drug used in the treatment of hyperglycemia of the second type diabetic patient, not adequately responsive to non-pharmacological measures such as diet and physical activity, to metformin or to thiazolidinediones.
In these cases, therefore, combined therapy with sitagliptin can ensure adequate glycemic control.

Mechanism of action JANUVIA ® - Sitagliptin

JANUVIA ® owes its therapeutic action to the presence of the active ingredient sitagliptin, active in the modulation of the concentrations of specific hormones, defined as incretins.
More precisely, these are two hormones produced at the gastrointestinal level, mainly following the introduction of food, known as GLP-1 (Glucagon-like peptide 1) and GIP (Glucose-dependent insulinotropic peptide), capable of acting at the pancreatic level stimulating, through the activation of AMP-dependent protein kinases, the production and secretion of insulin and at the same time inhibiting that of glucagon.
The sitagliptin contained in JANUVIA ® acts indirectly by increasing the concentrations of incretins, through the selective inhibition of the enzyme DPP-4 (Di-Peptidyl Peptidase IV), responsible for the irreversible hydrolysis of these hormones.
From a metabolic point of view, therefore, this drug allows to support the normal diet-fasting cycle, accentuating the release of insulin, inhibiting that of glucagon and thus ensuring the maintenance of good glycemic control.
The advantage deriving from the use of these inhibitors rather than incretin-mimetic drugs is essentially attributable to the simple method of administration, which allows the active ingredient, through oral intake, to be absorbed in the intestine, with bioavailability of the " 87% and half-life of about 12 hours, and be excreted unchanged, mainly through the urine, with minimal and insignificant hepatic metabolism.

Studies carried out and clinical efficacy

1. SITAGLIPTIN COMBINED THERAPY VS METFORMIN

Diabetes Obes Metab. 2011 Mar 15. doi: 10.1111 / j.1463-1326.2011.01390.x.

The effect of initial therapy with the fixed-dose combination of sitagliptin and metformin compared with metformin monotherapy in patients with type 2 diabetes mellitus.

Reasner C, Olansky L, Seck TL, Williams-Herman DE, Chen M, Terranella L, Johnson-Levonas AO, Kaufman KD, Goldstein BJ.


The treatment of the second type diabetic patient with sitagliptin in combination therapy with metformin, compared to metformin alone, ensured a more marked reduction in glycosylated hemoglobin (-2.4% vs-1.8%), also reducing the incidence of nausea, vomiting and abdominal pain and thus proving to be safer and more effective than monotherapy


2. SITAGLIPTIN: CLINICAL TRIAL

Diabetes Res Clin Pract. 2011 Apr 7. [Epub ahead of print]

Sitagliptin more effectively achieves a composite endpoint for A1C reduction, lack of hypoglycemia and no body weight gain compared with glipizide.

Seck TL, Engel SS, Williams-Herman DE, Sisk CM, Golm GT, Wang H, Kaufman KD, Goldstein BJ.


Although sitagliptin replicated more or less the same therapeutic successes observed for metformin in single therapy, prolonged treatment for one year ensured a further reduction in glycosylated hemoglobin by 0.5% without hypoglycemia and weight gain.


3. SITAGLIPTIN AND LIVER HEALTH

Hepatol Res. 2011 Mar 24. doi: 10.1111 / j.1872-034X.2011.00798.x.

Efficacy and safety in sitagliptin therapy for diabetes complicated by chronic liver disease caused by hepatitis C virus.

Arase Y, Suzuki F, Kobayashi M, Suzuki Y, Kawamura Y, Matsumoto N, Akuta N, Imai N, Kobayashi M, Sezaki H, Saito S, Hosaka T, Ikeda K, Kumada H, Ohmoto Y, Amakawa K, Tsuji H , Hsieh SD, Kobayashi T.


The poor hepatic metabolism of sitagliptin makes this active ingredient particularly indicated in the treatment of type II diabetic patients suffering from hepatic pathologies related to hepatitis C infection. therapeutic preserved liver function while maintaining liver function markers such as transaminases.

Method of use and dosage

JANUVIA ® sitagliptin 25 mg tablets:
the dosage generally most used in clinical practice is that of 100 mg once daily.
Although the aforementioned dosage is the most used, it should be remembered that the doctor will establish the correct therapeutic plan, which among other things will include the intake of metformin or PPAR gamma agonists, based on the physio-pathological conditions of the patient and the relative metabolic condition.

Warnings JANUVIA ® - Sitagliptin

The correct approach to the therapy of type II diabetes should not be separated from the improvement of the lifestyle, understood as both physical activity and nutrition, despite the implementation of pharmacological measures.
The use of JANUVIA ® in patients with reduced renal function could be dangerous and sometimes contraindicated.
It must be remembered that the concomitant intake of hypoglycemic drugs could increase the risk of hypoglycaemia making it dangerous to use machinery and drive vehicles.


PREGNANCY AND BREASTFEEDING

The total absence of studies relating to the intake of JANUVIA ® in pregnancy, the potential toxic effect on the fetus at high doses demonstrated by experimental models, and the possibility of opting for safer and well-characterized therapies broaden the contraindications of this medicine also in the state pregnancy and lactation period.

Interactions

The poor hepatic metabolism of sitagliptin minimizes the possible pharmacokinetic interactions between this medicine and any active ingredients, focusing essentially on the concomitant administration of cyclosporine, capable of increasing the body's exposure to sitagliptin, and digoxin.
However, it should be noted that in the case of combined therapy with other oral hypoglycemic drugs, the risk of interactions increases significantly based on the active ingredient associated with therapy with JANUVIA ®.

Contraindications JANUVIA ® - Sitagliptin

JANUVIA ® is contraindicated in case of hypersensitivity to the active substance or to one of its excipients, in patients with reduced renal function, type I diabetes and diabetic ketoacidosis, and during pregnancy and lactation.

Undesirable Effects - Side Effects

The data relating to the presence of side effects following the intake of JANUVIA ® derive essentially from the clinical trial, given the recent marketing of the drug and the short post-marketing monitoring period.
In any case, the adverse reactions recorded in the combined therapies with sitagliptin and other oral hypoglycemic drugs were generally found to be of modest clinical entity, with gastro-intestinal disturbances, peripheral edema, headache and dizziness.
The risk of hypoglycemia together with changes in the blood picture, osteoarthritis and alterations in the heart rhythm were the most clinically relevant, but fortunately rare, side effects.

Note

JANUVIA ® can only be sold under strict medical prescription


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