Complete Guide to Dolutegravir Pharmacokinetics
Overview
Dolutegravir is a Integrase Strand Transfer Inhibitor (INSTI) used in the HIV / Infectious Disease therapeutic area. It is indicated for HIV-1 infection. Population PK simulator for dolutegravir, an oral HIV integrase inhibitor used in combination antiretroviral therapy. Includes pregnancy and drug interaction effects relevant to HIV treatment exposure.
Mechanism of Action
Dolutegravir exerts its pharmacological effect by targeting HIV integrase. As a Integrase Strand Transfer Inhibitor (INSTI), it modulates this target to achieve therapeutic efficacy in HIV-1 infection. Understanding the target engagement is critical for interpreting the pharmacokinetic-pharmacodynamic (PK/PD) relationship and optimizing dosing regimens.
Key Pharmacokinetic Parameters
The following parameters are derived from published Population PK models for Dolutegravir:
| Parameter | Value |
|---|---|
| ka | 2.24 h⁻¹ |
| CL F | 0.901 L/h |
| Cmax | ~3.67 µg/mL (50 mg QD, steady state) |
| Vc F | 17.4 L |
| dose | 50 mg QD or 50 mg BID |
| brand | Tivicay |
| route | Oral |
| t lag | 0.263 h |
| t half | ~14 h |
| Ctrough | ~1.11 µg/mL (50 mg QD) |
| IC90 PA | 0.064 µg/mL (protein-adjusted) |
| protein binding | >98.9% |
| pregnancy 2nd tri | CL/F ↑72% vs non-pregnant |
| pregnancy 3rd tri | CL/F ↑85% vs non-pregnant |
Parameters represent typical population estimates from published literature. Individual values may vary.
Dosing & Administration
Dolutegravir is administered via the Oral route. Oral administration involves absorption from the gastrointestinal tract, and bioavailability may be affected by food intake, formulation, and first-pass metabolism.
Dosing recommendations should always follow approved prescribing information. The interactive simulator allows you to explore different dosing scenarios and their impact on drug exposure metrics such as AUC, Cmax, and Ctrough.
Clinical Considerations
In the HIV / Infectious Disease therapeutic area, for the treatment of HIV-1 infection, understanding the pharmacokinetics of Dolutegravir is essential for dose optimization and therapeutic drug monitoring. Key clinical factors that may affect Dolutegravir pharmacokinetics include:
- •Body weight and body composition
- •Renal and hepatic function
- •Drug-drug interactions and concomitant medications
- •Age, sex, and genetic polymorphisms
Interactive Dolutegravir PK Simulator
Explore Dolutegravir pharmacokinetics interactively. Adjust doses, dosing intervals, and patient covariates to visualize concentration-time profiles in real time.
Frequently Asked Questions
What is the half-life of Dolutegravir?
The elimination half-life of Dolutegravir depends on patient-specific factors. Based on published models, the typical half-life is approximately ~14 h.
How is Dolutegravir administered?
Dolutegravir is administered via the Oral route. It is indicated for HIV-1 infection. As a Integrase Strand Transfer Inhibitor (INSTI), dosing regimens should follow approved prescribing information and clinical guidelines.
What are the key PK parameters of Dolutegravir?
Key pharmacokinetic parameters for Dolutegravir include clearance (CL), volume of distribution (Vd), and elimination half-life. See the PK Parameters section above for specific values from published models.
Can I simulate Dolutegravir dosing scenarios for free?
Yes! PKPDBuilder offers a completely free, interactive Dolutegravir PK simulator based on published pharmacometric models. No login required. Use it to explore different doses, dosing intervals, and patient covariates.
⚠️ Disclaimer
This guide is for research and educational purposes only. It is not intended for clinical decision-making or patient dosing. Parameters are derived from published literature and represent population estimates. Always consult approved prescribing information for clinical use.