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What are the pharmacokinetics of tirofiban?

Tirofiban is an antiplatelet medication that belongs to the class of glycoprotein IIb/IIIa inhibitors. It's primarily used in the treatment of acute coronary syndrome and during percutaneous coronary intervention. Let's discuss the pharmacokinetics of tirofiban:

1. Absorption:
- Tirofiban is administered intravenously, so absorption is not applicable.
- It has 100% bioavailability due to its route of administration.

2. Distribution:
- The drug is rapidly distributed throughout the body.
- The volume of distribution at steady state is approximately 30 liters.
- Plasma protein binding is about 65%, primarily to albumin.

3. Metabolism:
- Tirofiban undergoes limited metabolism in the liver.
- The primary metabolic pathway is believed to be de-alkylation.

4. Elimination:
- The drug is primarily eliminated by the kidneys.
- About 65-75% of an administered dose is excreted in urine, with about 40-50% as unchanged drug.
- The remainder is excreted in feces.
- The plasma elimination half-life is approximately 2 hours in patients with normal renal function.

5. Clearance:
- The total body clearance of tirofiban is about 250 mL/min.
- Renal clearance accounts for 39-69% of total body clearance.

6. Special populations:
- In patients with renal impairment, the plasma clearance of tirofiban decreases.
- Dose adjustment is necessary for patients with severe renal impairment (creatinine clearance <30 mL/min).
- No significant differences in pharmacokinetics have been observed based on age, gender, or race.

7. Onset and duration of action:
- The onset of action is rapid, with platelet aggregation inhibition observed within 5 minutes of starting the infusion.
- The antiplatelet effect is reversible, with platelet function returning to normal within 4-8 hours after discontinuation of the infusion.

Understanding the pharmacokinetics of tirofiban is crucial for its proper use in clinical settings, especially concerning dosing in patients with renal impairment and the timing of invasive procedures due to its antiplatelet effects.