Sitagliptin

What is Sitagliptin

Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor and is used in the treatment of adults with type 2 diabetes mellitus (DM) in adults. DPP-4 inhibitors potentiate the effects of the incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), by inhibiting their breakdown by DPP-4.

Clinical studies of sitagliptin demonstrated mean hemoglobin A1C reductions of 0.6% to 1.05%; in patients with an A1C of 9% or more at baseline, the reduction can be as high as 1.5%.

 Metformin is first-line in the treatment of type 2 DM. In patients with established cardiovascular (CV) disease, heart failure (HF), or chronic kidney disease (CKD), a sodium-glucose co-transporter 2 (SGLT2) inhibitor or GLP-1 receptor agonist (GLP-1 RA) with proven CV benefit and reduction of CKD progression is recommended for add-on therapy, independent of baseline A1C or individualized A1C target.

In patients without indicators of high-risk or established CVD, HF, or CKD, DPP-4 inhibitors are a therapeutic option which are generally well tolerated, have a neutral effect on weight, and have minimal risk of hypoglycemia when used as monotherapy

Brand Name

Januvia

Indications

  • type 2 diabetes mellitus

For the treatment of type 2 diabetes mellitus in combination with diet and exercise

Side Effects

  1. abdominal pain
  2. anaphylactoid reactions
  3. angioedema
  4. arthralgia
  5. back pain
  6. bullous rash
  7. constipation
  8. diarrhea
  9. elevated hepatic enzymes
  10. exfoliative dermatitis
  11. headache
  12. heart failure
  13. hypoglycemia
  14. infection
  15. myalgia
  16. nausea
  17. oral ulceration
  18. pancreatitis
  19. pemphigus
  20. peripheral edema
  21. pharyngitis
  22. pruritus
  23. rash
  24. renal failure (unspecified)
  25. rhabdomyolysis
  26. Stevens-Johnson syndrome
  27. stomatitis
  28. urticaria
  29. vasculitis
  30. vomiting

Monitoring Parameters

  • blood glucose
  • glycosylated hemoglobin A1c (HbA1c)
  • serum creatinine/BUN

Contraindications

  • adrenal insufficiency
  • arthralgia
  • breast-feeding
  • burns
  • children
  • diabetic ketoacidosis
  • diarrhea
  • exfoliative dermatitis
  • fever
  • gastroparesis
  • geriatric
  • GI obstruction
  • heart failure
  • history of angioedema
  • hypercortisolism
  • hyperglycemia
  • hyperthyroidism
  • hypoglycemia
  • hypothyroidism
  • ileus
  • infection
  • malnutrition
  • pancreatitis
  • pituitary insufficiency
  • pregnancy
  • renal failure
  • renal impairment
  • serious rash
  • surgery
  • trauma
  • type 1 diabetes mellitus
  • vomiting

Interactions

  • Acebutolol
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Dichloralphenazone; Isometheptene
  • Acetaminophen; Guaifenesin; Phenylephrine
  • Acetaminophen; Pseudoephedrine
  • Acrivastine; Pseudoephedrine
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amphetamine
  • Amphetamine; Dextroamphetamine
  • Amprenavir
  • Androgens
  • Articaine; Epinephrine
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atenolol
  • Atenolol; Chlorthalidone
  • atypical antipsychotic
  • Azelastine; Fluticasone
  • Beclomethasone
  • Bendroflumethiazide; Nadolol
  • Benzphetamine
  • Beta-blockers
  • Betamethasone
  • Betaxolol
  • Bisoprolol
  • Bisoprolol; Hydrochlorothiazide, HCTZ
  • Bortezomib
  • Brimonidine; Timolol
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Brompheniramine; Pseudoephedrine
  • Budesonide
  • Budesonide; Formoterol
  • Bumetanide
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Guaifenesin; Phenylephrine
  • Carbetapentane; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pseudoephedrine
  • Carbinoxamine; Dextromethorphan; Pseudoephedrine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Carbinoxamine; Phenylephrine
  • Carbinoxamine; Pseudoephedrine
  • Carbonic anhydrase inhibitors
  • Carteolol
  • Carvedilol
  • Cetirizine; Pseudoephedrine
  • Chlophedianol; Dexchlorpheniramine; Pseudoephedrine
  • Chlophedianol; Guaifenesin; Phenylephrine
  • Chloroquine
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorthalidone; Clonidine
  • Chromium
  • Ciclesonide
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  • Clonidine
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  • Deflazacort
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  • Dexamethasone
  • Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Dexmethylphenidate
  • Dextroamphetamine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Guaifenesin; Phenylephrine
  • Dextromethorphan; Guaifenesin; Pseudoephedrine
  • Diazoxide
  • Dienogest; Estradiol valerate
  • Diethylpropion
  • Diethylstilbestrol, DES
  • Digoxin
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Phenylephrine
  • Disopyramide
  • Dobutamine
  • Dopamine
  • Dorzolamide; Timolol
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  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Elagolix; Estradiol; Norethindrone acetate
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  • Epinephrine
  • Erythromycin; Sulfisoxazole
  • Esmolol
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  • Estrogens
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  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Fenofibrate
  • Fenofibric Acid
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  • Garlic, Allium sativum
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  • Green Tea
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Guaifenesin; Phenylephrine
  • Guaifenesin; Pseudoephedrine
  • Hydantoins
  • Hydrochlorothiazide, HCTZ; Metoprolol
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydrocortisone
  • Hydroxychloroquine
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  • Monoamine oxidase inhibitors
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  • Naproxen; Pseudoephedrine
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  • Nicotine
  • Norepinephrine
  • Octreotide
  • Ombitasvir; Paritaprevir; Ritonavir
  • Orlistat
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  • Prilocaine; Epinephrine
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  • Sofosbuvir
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  • Somatropin, rh-GH
  • Sotalol
  • Sparfloxacin
  • Sulfadiazine
  • Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
  • Sulfasalazine
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  • Sympathomimetics
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  • Tegaserod
  • Thiazide diuretics
  • Thyroid hormones
  • Timolol
  • Tipranavir
  • tobacco
  • Torsemide
  • Triamcinolone
  • Triamterene
  • Trovafloxacin, Alatrofloxacin
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