Januvia (Sitagliptin) Flashcards

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.

Description

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.

Januvia (Sitagliptin) Flashcards

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Questions and Answers

What is the drug class of Januvia?

What is the route of administration for Januvia?

What is the recommended dose of Januvia for Type 2 diabetes mellitus?

What are the indications for using Januvia?

What is the dose adjustment for mild renal insufficiency (CrCl 50 mL/min or greater)?

Can Januvia be taken with food?

Serious hypersensitivity reactions have been reported as contraindications for Januvia.

Which of the following are precautions associated with Januvia?

What are some common adverse effects of Januvia?

What pregnancy category is Januvia classified under?

What is the bioavailability of orally administered Januvia?

What is the mechanism of action of Sitagliptin?