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JULUCA is a brand name for Dolutegravir, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Verbatim from this product's HC label. Tap a section to expand.
) The effect of a high fat, high calorie meal on the absorption of dolutegravir and rilpivirine when administered as a fixed-dose combination tablet has not been assessed in an appropriately designed study. 9%) to human plasma proteins based on in vivo data and binding is independent of plasma dolutegravir concentration.
4 L based on population pharmacokinetic analysis. 7%) to plasma proteins in vitro, primarily to albumin. Cerebrospinal Fluid (CSF) In 12 treatment-naïve patients on dolutegravir plus abacavir/lamivudine, the median dolutegravir concentration in CSF was 18 ng/mL (ranging from 4 to 23 ng/mL) 2 to 6 hours post-dose after 2 weeks of treatment.
The clinical relevance of this finding has not been established. 7% of total dose administered in a human mass balance study). Dolutegravir is the predominant circulating compound in plasma; renal elimination of unchanged drug is low (<1% of the dose).
In vitro experiments indicate that rilpivirine primarily undergoes oxidative metabolism mediated by the cytochrome P450 (CYP) 3A system.
Elimination:
Dolutegravir has a terminal half-life of ~14 hours. Fifty-three percent of total oral dose is excreted unchanged in the faeces. It is unknown if all or part of this is due to unabsorbed drug or biliary excretion of the glucuronidate conjugate, which can be further degraded to form the parent compound in the gut lumen.
Rilpivirine has a terminal elimination half-life of approximately 45 hours. 1% of the radioactivity could be retrieved in feces and urine, respectively. In feces, unchanged rilpivirine accounted for on average 25% of the administered dose.
Only trace amounts of unchanged rilpivirine (< 1% of total dose) were detected in urine. JULUCA, dolutegravir and rilpivirine Page 25 of 43 Protected B / Protégé B Special Populations and Conditions Pediatrics: JULUCA has not been studied in the pediatric population.
Geriatrics:
Population pharmacokinetic analysis using data in HIV-1-infected adults showed that there was no clinically relevant effect of age on dolutegravir or rilpivirine exposures. Pharmacokinetic data in patients >65 years old are limited.
Sex:
Population pharmacokinetic analyses revealed no clinically relevant effect of gender on the exposure of dolutegravir or rilpivirine.
Pregnancy and Breast-feeding:
Pregnancy and Postpartum The exposure to total rilpivirine after intake of rilpivirine 25 mg once daily as part of an antiretroviral regimen was lower during pregnancy (similar for the 2nd and 3rd trimester) compared with postpartum.
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The decrease in unbound (active) rilpivirine pharmacokinetic parameters during pregnancy compared with postpartum was less pronounced than for total rilpivirine. In women receiving rilpivirine 25 mg once daily during the 2nd trimester of pregnancy, mean intra-individual values for total rilpivirine Cmax, AUC24h and Cmin values were 21%, 29% and 35%, respectively, lower as compared with postpartum; during the 3rd trimester of pregnancy, Cmax, AUC24h and Cmin values were 20%, 31% and 42%, respectively, lower as compared with postpartum.
There are no pharmacokinetic data on the use of dolutegravir in pregnancy.
Genetic Polymorphism:
In a meta-analysis using pharmacogenomics samples collected in clinical studies in healthy subjects, subjects with UGT1A1 (n=7) genotypes conferring poor dolutegravir metabolism had a 32% lower clearance of dolutegravir and 46% higher AUC compared with subjects with genotypes associated with normal metabolism via UGT1A1 (n=41).
Rilpivirine pharmacokinetics are not anticipated to be impacted by polymorphisms in drug metabolising enzymes.
Ethnic origin:
Population pharmacokinetic analyses of both dolutegravir and rilpivirine in HIV infected patients indicated that race had no clinically relevant effect on exposure to either dolutegravir or rilpivirine.
Hepatic Insufficiency:
Dolutegravir and rilpivirine are primarily metabolized and eliminated by the liver. No dosage adjustment is necessary for patients with mild to moderate hepatic insufficiency (Child-Pugh score A or B). In a study comparing 8 patients with moderate hepatic insufficiency (Child-Pugh score B) to 8 matched healthy adult controls, the single 50 mg dose exposure of dolutegravir was similar between the two groups.
In a study comparing 8 patients with mild hepatic insufficiency (Child-Pugh score A) to 8 matched controls, and 8 patients with moderate hepatic insufficiency (Child-Pugh score B) to 8 matched controls, the multiple dose exposure of rilpivirine was 47% higher in patients with mild hepatic insufficiency and 5% higher in patients with moderate hepatic insufficiency.
The effect of severe hepatic insufficiency (Child-Pugh score C) on the pharmacokinetics of dolutegravir or rilpivirine have not been studied.
Renal Insufficiency:
Population pharmacokinetic analyses indicated that mild and moderate renal impairment had no clinically relevant effect on the exposure of dolutegravir. Dolutegravir AUC, Cmax, and C24 were lower by 40%, 23%, and 43%, respectively, in subjects (n = 8) with severe renal impairment (creatinine clearance less than 30 mL/min) as compared with matched healthy controls.
There is limited information on dolutegravir in patients requiring dialysis. Population pharmacokinetic analyses indicated that mild renal impairment had no clinically relevant effect on the exposure of rilpivirine. There is JULUCA, dolutegravir and rilpivirine Page 26 of 43 Protected B / Protégé B limited or no information regarding the pharmacokinetics of rilpivirine in patients with moderate or severe renal impairment, end-stage renal disease, […]