Questions and Answers
What is the drug class of Januvia?
What is the route of administration for Januvia?
oral
What is the recommended dose of Januvia for Type 2 diabetes mellitus?
100 mg orally once daily
What are the indications for using Januvia?
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What is the dose adjustment for mild renal insufficiency (CrCl 50 mL/min or greater)?
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Can Januvia be taken with food?
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Serious hypersensitivity reactions have been reported as contraindications for Januvia.
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Which of the following are precautions associated with Januvia?
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What are some common adverse effects of Januvia?
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What pregnancy category is Januvia classified under?
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What is the bioavailability of orally administered Januvia?
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What is the mechanism of action of Sitagliptin?
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Study Notes
Januvia (Sitagliptin) Overview
- Belongs to antidiabetic drug class as a DPP4 inhibitor.
- Administered via oral route.
Dosing Information
- Used for Type 2 diabetes only; not for Type 1 diabetes or diabetic ketoacidosis.
- General dosing: 100 mg orally once daily with or without food.
- Dosage may need adjustment when combined with sulfonylureas or insulin.
Dose Adjustments
- For renal insufficiency:
- Mild (CrCl ≥ 50 mL/min): no adjustment necessary.
- Moderate (CrCl 30-50 mL/min): 50 mg orally once daily.
- Severe (CrCl < 30 mL/min): 25 mg orally once daily.
- ESRD on dialysis: 25 mg orally once daily, regardless of dialysis timing.
- Mild to moderate hepatic insufficiency: no adjustment needed.
- No adjustments based solely on age for elderly patients.
Administration Guidelines
- Can be taken with or without food.
Contraindications
- Serious hypersensitivity reactions to sitagliptin, such as angioedema or anaphylaxis.
Precautions
- Watch for angioedema; potential for cross-sensitivity with other DPP-4 inhibitors unknown.
- Monitor for acute pancreatitis; therapy should be discontinued if symptoms develop.
- Serious hypersensitivity reactions, including Stevens-Johnson syndrome, can occur, especially within the first three months.
- Reported severe joint pain may necessitate discontinuation and could recur with rechallenge.
- Regularly monitor renal function, especially in cases of worsening renal function or ESRD.
Adverse Effects
- Common effects:
- Hypoglycemia (0.6% to 12.2%)
- Headache (1.1% to 5.9%)
- Nasopharyngitis (5.2% to 6.3%); Upper respiratory infections (4.5% to 6.3%)
- Serious effects:
- Pancreatic cancer, pancreatitis, anaphylaxis, angioedema, Stevens-Johnson syndrome, and rhabdomyolysis.
Drug Interactions
- Interactions with somatostatin, digoxin (Lanoxicaps, Lanoxin), insulin, and several oral diabetes medications.
- Potential interactions with fluoroquinolones.
Pregnancy Category
- Rated category B, indicating no known risk in human studies.
Monitoring Requirements
- Regular assessments of glycemic control through HbA1c:
- Every 6 months in patients meeting goals.
- Every 3 months if therapy changes or goals not met.
- Self-monitoring of blood glucose as needed.
- Periodic renal function assessments.
Mechanism of Action (MOA)
- Inhibits DPP-4 enzyme, preserving incretin hormones like GLP-1 and GIP that regulate glucose homeostasis post-meal.
- Enhances insulin release and decreases glucagon levels in a glucose-dependent manner.
Pharmacokinetics
- Absorption: Bioavailability is 87% when taken orally.
- Distribution: 38% protein binding, volume of distribution is approximately 198 L.
- Metabolism: Primarily hepatic through CYP3A4 and minor contributions from CYP2C8.
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Test your knowledge on Januvia (Sitagliptin) with these flashcards. This quiz covers essential details such as drug class, administration routes, and dosing guidelines. Perfect for students and healthcare professionals alike.
