300884 Pharmacology

Table of Contents


Write an essay about Sitagliptin.


Sitagliptin is an antihyperglycemic and antidiabetic drug that is used to treat Type 2 Diabetic Mellitus (Inamdar & Mhaske 2012).

Merck & Co. developed this drug. It is used to treat patients with T2D, with or without the addition of metformin or thiazolidinedione.

The drug was created in 2006 and approved by the United States Food and Drug administration on October 17, 2006.

The FDA approved the marketing of this drug by Merck and Co. on April 2, 2007.

Sitagliptin was also combined with other drugs, which produced positive results for patients with T2D.

The company also promoted this drug under the generic name Janumet, where Sitagliptin and metformin were present.

The molecular formula of the active pharmaceutical ingredient, as well as its chemical form and physical properties.

Januvia or Sitagliptin has a molecular formula C16H15F6N5O. It is a pyrazine-derived Dipeptidylpeptidase inhibitor (Inamdar & Mhaske 2012).

Sitagliptin Phosphate monohydrate is the active pharmaceutical ingredient. It is an off-white, hygroscopic, powdery substance that is soluble in water.

When discussing the physical properties, it is important to mention the chiral centers, molecular weight, solubility, melting point, and solubility.

The drug’s melting point is between 216 and 219degC. Its molecular weight of 407.32g/mol is also discussed. However, its solubility at 25degC is 179.2 mg/L (Russell Jones et al.

The drug is a viscous liquid and is given to patients in solid form.

It is important to mention the stability of the drug. The drug can be stored according to the directions and without the use of strong oxidizing agents.

Thermal decomposition is not recommended for the drug’s decomposition, as it can release toxic gases like carbon monoxide or carbon dioxide (Sin, Mahe, and Sigal 2012).

Crystallization Properties of the API

Additionally, it is important to discuss the crystallization properties of the API drug (Sin, Mahe, and Sigal 2012).

Crystallization is the process by which the drug’s crystal salts form the monophosphate version of the drug.

There are currently four crystallized versions of drugs that are available in the pharmaceutical industry. These variants have been patented and are ready for patients to use.

These stable forms of drug, which include solvates, hydrolyzes, and polymorphics, are a few of the most bioavailable. They also provide a higher level of bioavailability than the free base variants.

Administration Routes and Dosage Forms with Pharmacokinetic Data

Patients with type 1 diabetes should not receive this drug. Instead, patients with type 2 should receive it in tablets of 25 mg, 50mg, and 100mg strengths (Sin, Mahe, and Sigal 2012).

Inamdar and Mhaske (2012) also recommend that the doses be administered orally as intravenous routes and other methods are ineffective in maintaining the enzymatic balance of the body.

Sitagliptin, a drug that is easily absorbed by the body, has a half-life of 8 to 14 hours. This should be noted when discussing the drug’s pharmacokinetics.

The drug’s excretion rate is greater than 80% and it works differently depending on how much you take (Russell Jones et al.

Description of the Formulation

The tablet dosage form has many advantages and disadvantages.

The oral administration of sitagliptin has the advantage of helping to lower hyperglycemia.

Sitagliptin, unlike other medications, does not cause weight gain and is therefore safe for patients with type 2 diabetes. (Ghislieri and al.

The manufacturing process described

This is how the final pharmacological drug is made.

Refer to

Ghislieri D., Green A.P. Pontini M.. Willies S.C. Rowles I. Frank A. Grogan G. Turner N.J.

Engineering an enantioselective amino oxidase to synthesize pharmaceutical building blocks and alkaloid naturally products.

Journal of the American Chemical Society 135(29), pages 10863-10869.

Mhaske, A.A. (2012).

International Journal of Pharmaceutical Sciences and Research 3(9), P.3267

DURATION-4 Study Group (2012).

A 26-week double-blind study comparing exenatide once a week with metformin, pioglitazone and sitagliptin as monotherapy for type 2 diabetics (DURATION-4).

Diabetes care, 35(2): pp.252-258.

Sin, C., Mahe E., and Sigal M.L. (2012)

Sitagliptin-induced drug reaction in a patient with eosinophilia.

Diabetes & metabolism 38(6): pp.571-573.

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