DARUVIR 600MG TABLET IS USED IN THE TREATMENT OF HIV INFECTION. IT STOPS THE VIRUS FROM PRODUCING NEW VIRUSES AND CLEARS UP YOUR INFECTION.

Daruvir 600mg Tablet should be used in the dose and duration as advised by your doctor. Do not skip any doses and finish the full course of treatment even if you feel better. Take it with food, as this increases the absorption of the medicine into the body.

Some people may experience nausea, diarrhea and increased cholesterol or triglyceride levels, as side effects of this medicine. Please consult your doctor if these side effects persist for a longer duration. Inform your doctor if you have diabetes as it can increase sugar levels in the blood. Inform your doctor before taking this drug if you are an elderly patient, of, or above 65 years of age, if you have a history of liver disease including hepatitis B or C or have hemophilia or if you are allergic to sulfa drugs.

USES OF DARUVIR TABLET

HIV Infection

SIDE EFFECTS OF DARUVIR TABLET

Common

Nausea

Diarrhea

Increased cholesterol level in blood

Increased triglyceride level in blood

HOW TO USE DARUVIR TABLET

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Daruvir 600mg Tablet is to be taken with food.

HOW DARUVIR TABLET WORKS

Daruvir 600mg Tablet is an anti-HIV medication. It works by interfering with an enzyme (protease), which is required by HIV-infected cells to make new viruses. This stops the production of new viruses.

SAFETY ADVICE

warnings

Alcohol

CAUTION

Caution is advised when consuming alcohol with Daruvir 600mg Tablet. Please consult your doctor.

warnings

Pregnancy

SAFE IF PRESCRIBED

Daruvir 600mg Tablet is generally considered safe to use during pregnancy. Animal studies have shown low or no adverse effects to the developing baby; however, there are limited human studies.

warnings

Breastfeeding

SAFE IF PRESCRIBED

Daruvir 600mg Tablet is probably safe to use during breastfeeding. Limited human data suggests that the drug does not represent any significant risk to the baby.

warnings

Driving

UNSAFE

Daruvir 600mg Tablet may decrease alertness, affect your vision or make you feel sleepy and dizzy. Do not drive if these symptoms occur.

warnings

Kidney

SAFE IF PRESCRIBED

Daruvir 600mg Tablet is safe to use in patients with kidney disease. No dose adjustment of Daruvir 600mg Tablet is recommended.

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warnings

Liver

CAUTION

Daruvir 600mg Tablet should be used with caution in patients with severe liver disease. Dose adjustment of Daruvir 600mg Tablet may be needed. Please consult your doctor.

Limited information is available on use of Daruvir 600mg Tablet in these patients. Dose adjustment may not be required in patients with mild to moderate liver disease.

Composition

Each film-coated tablet contains:

Darunavir Ethanolate equivalent to Darunavir 600 mg

Colours: Titanium Dioxide & Sunset Yellow FCF

Dosage Form

Oral tablet

Pharmacology

Pharmacodynamics

Mechanism of Action

Darunavir is an inhibitor of the human immunodeficiency virus (HIV)-1 protease. It selectively inhibits the cleavage of HIV-1 encoded Gag-Pol polyproteins in infected cells, thereby preventing the formation of mature virus particles.

Cardiac Electrophysiology

In a thorough QT/QTc study in 40 healthy subjects, darunavir/ritonavir doses of 1.33 times the maximum recommended dose did not affect the QT/QTc interval.

Pharmacokinetics

Pharmacokinetics in Adults

General

Darunavir is primarily metabolized by CYP3A. Ritonavir inhibits CYP3A, thereby increasing the plasma concentrations of darunavir. When a single dose of darunavir 600 mg was given orally in combination with 100 mg ritonavir twice daily, there was an approximate 14-fold increase in the systemic exposure of darunavir. Therefore, darunavir should only be used in combination with 100 mg of ritonavir to achieve sufficient exposures of darunavir.

The pharmacokinetics of darunavir, co-administered with low-dose ritonavir (100 mg), has been evaluated in healthy adult volunteers and in HIV-1-infected subjects. Table 1 displays the population pharmacokinetic estimates of darunavir after oral administration of darunavir/ritonavir 600/100 mg twice daily (based on sparse sampling in 285 patients in trial TMC114-C214, 278 patients in trial TMC114-C229 and 119 patients from trials TMC114-C202 and TMC114-C213).

Table 1: Population pharmacokinetic estimates of darunavir at darunavir/ritonavir 600/100 mg twice daily (Trial TMC114-C214, 48-week analysis, Trial TMC114-C229, 48-week analysis and integrated data from Trials TMC114-C213 and TMC114-C202, primary 24-week analysis)

Parameter

Darunavir/ritonavir 600/100 mg twice daily

Study TMC114-C214  

N = 285

Study TMC114-C229

N = 278

Studies TMC114-C213 and TMC114-C202 (integrated data)

N =119

AUC24h (ng·h/mL)*

Mean ± Standard Deviation

116796 ± 33594

114302 ± 32681

124698 ± 32286

Median (Range)

111632

(64874–355360)

109401

(48934-323820)

123336

(67714–212980)

C0h (ng/mL)

Mean ± Standard Deviation

3490 ± 1401

3386 ± 1372

3578 ± 1151

Median (Range)

3307 (1517–13198)

3197 (250-11865)

3539 (1255–7368)

N=number of subjects with data

* AUC24h is calculated as AUC12h*2.

Absorption and Bioavailability

Darunavir, co-administered with 100 mg ritonavir twice daily, was absorbed following oral administration with a Tmax of approximately 2.5–4 hours. The absolute oral bioavailability of a single 600 mg dose of darunavir alone and after co-administration with 100 mg ritonavir twice daily was 37% and 82%, respectively. In vivo data suggest that darunavir/ritonavir is an inhibitor of the p-glycoprotein (p-gp) transporters.

Effects of Food on Oral Absorption

When darunavir tablets were administered with food, the Cmax and AUC of darunavir, co-administered with ritonavir, is approximately 40% higher relative to the fasting state. Within the range of meals studied, darunavir exposure is similar. The total caloric content of the various meals evaluated ranged from 240 Kcal (12 gms fat) to 928 Kcal (56 gms fat).

Distribution