Kocitaf

Dolutegravir 50 mg, emtricitabine 200 mg, tenofovir alafenamide 25 mg

HIV-1 in adult & adolescent ≥12 yr weighing at least 40 kg.

1 tab once daily. Missed dose w/in 18 hr of the time: Take 1 tab as soon as possible & resume normal dosing schedule. If >18 hr, patient should not take missed dose & resume usual dosing schedule.

May be taken with or without food: Do not chew/crush/split. For patients w/ integrase class resistance, preferably taken w/ food.

Hypersensitivity. Co-administration w/ dofetilide & organic cation transporter substrates.

Integrase class resistance. Discontinue treatment if signs & symptoms of hypersensitivity reactions develop; if there is evidence of worsening liver disease. Monitor clinical status eg, liver aminotransferases & bilirubin. Patients w/ chronic hepatitis B or C treated w/ antiretroviral therapy. Co-infection w/ HIV-1 & HCV. Closely monitor patients co-infected w/ HIV & HBV for at least several mth upon discontinuation of treatment. Do not administer in concomitant use w/ drugs containing tenofovir disoproxil (as fumarate), lamivudine or adefovir dipivoxil. Patients w/ significant underlying liver disorders. Monitor patients w/ preexisting liver dysfunction during combination of antiretroviral therapy (CART) & consider discontinuation or interruption of treatment upon worsening of liver disease. Wt gain & increase in blood lipids & glucose levels may occur. Mitochondrial dysfunction in HIV -ve infants exposed in utero &/or postnatally to nucleoside analogues. Perform clinical & lab follow-up & investigate for possible mitochondrial dysfunction in childn (including HIV -ve childn), exposed in utero to nucleoside & nucleotide analogues. Immune reactivation syndrome in HIV infected patients treated w/ CART. Avoid treatment in antiretroviral-experienced patients w/ HIV-1 harboring the K65R mutation. Triple nucleoside therapy. Closely observe patients for opportunistic infections. Avoid co-administration w/ Mg- or Al-containing antacid, Fe & Ca supplements, multivitamins & inducing agents, etavirine (w/o boosted PIs), tipranavir/ritonavir, rifampicin, St. John's wort & certain antiepileptics. Consider dose adjustment of metformin when starting & stopping co-administration of dolutegravir; monitor renal function during treatment. Increased risk of lactic acidosis in patients w/ moderate renal impairment (CrCl 45-59 mL/min). Osteonecrosis in patients w/ advanced HIV disease &/or long-term CART exposure. Nephrotoxicity. Rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Not recommended w/ certain anticonvulsants (eg, carbamazepine, oxcarbazepine, phenobarb & phenytoin), antimycobacterials (eg, rifampicin, rifabutin, rifapentine), boceprevir, telaprevir, St. John's wort & HIV PIs other than atazanavir, lopinavir & darunavir; medicinal products containing tenofovir disoproxil (as fumarate), emtricitabine, lamivudine or adefovir dipivoxil. Do not initiate in patients w/ estimated CrCl <30 mL/min. Severe hepatic impairment (Child-Pugh Class C). Perform pregnancy testing prior to initiation of treatment in adolescents & adults of childbearing potential. Use effective contraception during treatment. May affect ability to drive and operate machinery. Avoid use of dolutegravir from the time of conception until the 1st trimester of pregnancy. Lactation. Childn <12 yr, or weighing <40 kg. Elderly ≥65 yr.

Nausea. Abnormal dreams, insomnia, depression; headache, dizziness; diarrhoea, vomiting, abdominal pain & discomfort, flatulence; rash, pruritus; fatigue; ALT, AST or creatine phosphokinase elevations.

Dolutegravir: Increased AUC, C_max & C_t w/ lopinavir/ritonavir + etravirine, rilpivirine, PIs (atazanavir, atazanavir/ritonavir), other antivirals (eg, telaprevir, boceprevir, daclastavir), prednisone. Increased conc of dofetelide. Increase AUC & C_max of metformin. Decreased AUC, C_max & C_t w/ etravirine w/o boosted PIs, darunavir/ritonavir & etravirine, tipranavir/ritonavir, fosamprenavir, carbamazepine, rifampicin, rifabutin. Decreased conc w/ nevirapine, oxcarbazepine, phenytoin, phenobarb, St. John's wort. Decreased AUC & C_max w/ Mg- or Al-containing antacids. Decreased AUC, C_max, C₂₄ w/ Ca & Fe supplements, & multivitamins. Tenofovir alafenamide: Increased plasma conc w/ ketoconazole, itraconazole, fluconazole, isavuconazole. May decrease plasma conc w/ rifabutin, rifampicin, rifapentine, oxcarbazepine, phenobarb, phenytoin & St. John's wort. Concomitant use w/ boceprevir, telaprevir. May increase AUC, C_max, C_min of ledipasvir & AUC & C_max of sofosbuvir. Increased AUC & C_max w/ atazanavir/cobicistat, atazanavir/ritonavir, darunavir/cobicistat, darunavir/ritonavir. Increased AUC & C_max of setraline. Increased plasma conc w/ ciclosporin.

Antivirals

J05AR17 - emtricitabine and tenofovir alafenamide ; Belongs to the class of antivirals for treatment of HIV infections, combinations.

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