sitagliptin


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sitaGLIPtin

(sit-a-glip-tin) ,

Januvia

(trade name)

Classification

Therapeutic: antidiabetics
Pharmacologic: enzyme inhibitors
Pregnancy Category: B

Indications

Adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus; may be used as monotherapy or combination therapy with metformin, a thiazolidinedione, a sulfonylurea, or insulin.

Action

Inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which slows the inactivation of incretin hormones, resulting in increased levels of active incretin hormones. These hormones are released by the intestine throughout the day and are involved in regulation of glucose homeostasis. Increased/prolonged incretin levels result in an increase in insulin release and decrease in glucagon levels.

Therapeutic effects

Improved control of blood glucose.

Pharmacokinetics

Absorption: 87% absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: 79% excreted unchanged in urine, minor metabolism.
Half-life: 12.4 hr.

Time/action profile

ROUTEONSETPEAKDURATION
POrapid1–4 hr24 hr

Contraindications/Precautions

Contraindicated in: Type 1 diabetes mellitus;Diabetic ketoacidosis;Hypersensitivity.
Use Cautiously in: Renal impairment (dose ↓ required for CCr <50 mL/min);History of pancreatitis;History of angioedema to another DPP-4 inhibitor Obstetric / Use only if clearly needed. Lactation: Excretion into breast milk unknown; Pediatric: Safety not established; Geriatric: Consider age-related ↓ in renal function when determining dose.

Adverse Reactions/Side Effects

Central nervous system

  • headache

Gastrointestinal

  • pancreatitis (life-threatening)
  • nausea
  • diarrhea

Genitourinary

  • acute renal failure

Respiratory

  • upper respiratory tract infection
  • nasopharyngitis

Musculoskeletal

  • arthralgia
  • back pain
  • myalgia

Miscellaneous

  • allergic reactions including anaphylaxis (life-threatening)
  • angioedema (life-threatening)
  • exfoliative skin conditions (stevens-johnson syndrome) (life-threatening)
  • rash
  • urticaria

Interactions

Drug-Drug interaction

May slightly ↑ serum digoxin levels; monitoring recommended.↑ risk of hypoglycemia when used with insulin, glyburide, glipizide, or glimepiride (may need to ↓ dose of insulin or sulfonylurea).

Route/Dosage

Oral (Adults) 100 mg once daily.

Renal Impairment

Oral (Adults) CCr 30–<50 mL/min—50 mg once daily; CCr <30 mL/min—25 mg once daily.

Availability

Tablets: 25 mg, 50 mg, 100 mg Cost: 25 mg $801.18 / 90, 50 mg $816.93 / 90, 100 mg $816.93 / 90
In combination with: metformin (Janumet), metformin XR (Janumet XR). See combination drugs.

Nursing implications

Nursing assessment

  • Observe patient for signs and symptoms of hypoglycemic reactions (abdominal pain, sweating, hunger, weakness, dizziness, headache, tremor, tachycardia, anxiety).
  • Monitor for signs of pancreatitis (nausea, vomiting, anorexia, persistent severe abdominal pain, sometimes radiating to the back) during therapy. If pancreatitis occurs, discontinue sitagliptin and monitor serum and urine amylase, amylase/creatinine clearance ratio, electrolytes, serum calcium, glucose, and lipase.
  • Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
  • Lab Test Considerations: Monitor hemoglobin A1C prior to and periodically during therapy.
    • Monitor renal function prior to and periodically during therapy.

Potential Nursing Diagnoses

Imbalanced nutrition: more than body requirements (Indications)
Noncompliance (Patient/Family Teaching)

Implementation

  • Do not confuse sitagliptin with sumatriptan. Do not confuse Januvia (sitagliptin) with Enjuvia (estrogens, conjugated B), Jantoven (warfarin), or Janumet (sitagliptin/metformin).
  • Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
  • Oral: May be administered without regard to food.

Patient/Family Teaching

  • Instruct patient to take sitagliptin as directed. Take missed doses as soon as remembered, unless it is almost time for next dose; do not double doses. Advise patient to read Medication Guide before starting and with each Rx refill in case of changes.
  • Explain to patient that sitagliptin helps control hyperglycemia but does not cure diabetes. Therapy is usually long term.
  • Instruct patient not to share this medication with others, even if they have the same symptoms; it may harm them.
  • Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hyperglycemic or hypoglycemic episodes.
  • Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water, and notify health care professional.
  • Instruct patient in proper testing of blood glucose and urine ketones. These tests should be monitored closely during periods of stress or illness and health care professional notified if significant changes occur.
  • Advise patient to stop taking sitagliptin and notify health care professional promptly if symptoms of hypersensitivity reactions (rash; hives; swelling of face, lips, tongue, and throat; difficulty in breathing or swallowing) or pancreatitis occur.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding. Encourage patients who become pregnant while taking sitagliptin to join the pregnancy registry by calling 1-800-986-8999.

Evaluation/Desired Outcomes

  • Improved hemoglobin A1C, fasting plasma glucose and 2-hr post-prandial glucose levels.

sitagliptin

(sĭt′ə-glĭp′tn)
n.
An oral hypoglycemic drug, C16H15F6N5O, used in its phosphate form to treat type 2 diabetes.
References in periodicals archive ?
8 In a placebo-controlled, phase 3 trial, patients of T2DM who had not received pharmacological treatment in the last 12 weeks were randomized to receive once daily dose of placebo (n=228), empagliflozin10 mg (n=224), empagliflozin 25 mg (n=224), or sitagliptin 100 mg (n=223).
Obese patients also have increase baseline CRP as compared to their lean counterparts.4 Sitagliptin is one of the oral anti diabetic drug that inhibits enzyme DPP-4.
According to the company, the 78-week, randomised, double-blind, double-dummy, active-controlled, parallel-group, multicentre, multinational PIONEER 3 trial compared the efficacy and safety of oral semaglutide 3 mg, 7 mg and 14 mg with sitagliptin 100 mg in 1,864 people with type 2 diabetes inadequately controlled with metformin, with or without sulfonylurea.
Sitagliptin (SIT) (DPP-4 inhibitor) led to reduction in A1C, when taken in addition to MET and sulfonylureas [5, 6].
Spending on drugs used by patients with diabetes, 2015 Billions of dollars Insulin glargine 1 Rosuvastatin 2 Atorvastatin 4 Insulin aspart 7 Sitagliptin 8 Insulin isophane (NPH) 9 Pregabalin 10 Gabapentin 11 Insulin detemir 12 Metformin 14 Insulin lispro 16 Metformin-sitagliptin 20 The number in each bar represents the drug's place in the top 20 for spending for all drugs.
Serum was taken from [Glp1r.sup.-/-] mice after three days of oral sitagliptin administration (n = 4 (pooled), 3 mice each sample).
Regarding medicine options, four studies [8,18-20] examined the effects of combination therapy comprising sitagliptin and insulin compared with insulin monotherapy on T1DM, and the other study [13] investigated vildagliptin.
These findings prompted us to investigate the circulating miRNA profile of elderly patients with poorly controlled T2D and to identify the changes it undergoes during DPP-IVi therapy with sitagliptin. The plasma levels of three miRNAs (miR-1208, miR-550a-3p, and miR-30c-5p) displayed directionally similar trends in responders and nonresponders during the 15 months of sitagliptin treatment.
The drugs such as linagliptin, saxagliptin, sitagliptin, and vildagliptin were obtained from pharmaceutical companies as gifted samples in pure powder form of IP grade.
There are four drugs in this subclass: alogliptin (Nesina), linagliptin (Tradjenta), saxagliptin (Onglyza), and sitagliptin (Januvia).
Previous studies have shown that sitagliptin decreases the production of proinflammatory cytokines, increases the biological availability of NO, and protects VECs, thus reducing the formation of atherosclerotic plaques [10,11].
One common API, sitagliptin phosphate--hereby referred to as sitagliptin--will be used as an example to illustrate this methodology.