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120 X 100 mg
60 X 200 mg
INTELENCE must always be given in combination with other antiretroviral medicinal products.
Adults: The recommended dose of INTELENCE is 200 mg (one 200 mg tablet or two 100 mg tablets) taken
orally twice daily (b.i.d.), following a meal (see section 5.2). Patients should be instructed to swallow the
tablet(s) as a whole with a liquid such as water. Patients who are unable to swallow the INTELENCE
tablet(s) whole may disperse the tablet(s) in a glass of water. Once the tablet(s) is(are) dispersed, patients should stir the dispersion well, and drink it immediately. The glass should be rinsed with water several times, and each rinse completely swallowed to ensure the entire dose is consumed.
Children (less than 12 years of age) and adolescents (12 to 17 years of age): Treatment with INTELENCE is not recommended in children and adolescents. The safety and efficacy of INTELENCE in these populations are under investigation .
Elderly: Limited information is available in this population.
Hepatic impairment: No dose adjustment is required in patients with mild or moderate hepatic impairment (Child-Pugh score A or B). The pharmacokinetics of INTELENCE have not been studied in patients with severe hepatic impairment (Child-Pugh score C).
Renal impairment: No dose adjustment is required in patients with renal impairment.
If the patient misses a dose of INTELENCE within 6 hours of the time it is usually taken, the patient should be told to take INTELENCE following a meal as soon as possible and then take the next dose of INTELENCE at the regularly scheduled time. If a patient misses a dose of INTELENCE by more than 6 hours of the time it is usually taken, the patient should be told not to take the missed dose and simply resume the usual dosing schedule.
For full details see prescribing information.
In combination with other antiretroviral medicdbinal products, for the treatment of HIV-1 infection in antiretroviral treatment-experienced adult patients, including those with non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance. Treatment history and, when available, resistance testing should guide the use. In patients who have experienced virological failure on an NNRTI and nucreoside or nucleotide reverse transcriptase inhibitor (NtRTI)-containing regimen. Not recommended for use in combination with (NtRTI)’s only.
Hypersensitivity to etravirine or to any of the excipients.
Patients should be advised that current antiretroviral therapy does not cure HIV and has not been proven to prevent the transmission of HIV to others through blood or sexual contact. Appropriate precautions should continue to be employed. Clinical studies are ongoing in HIV-1 infected children and adolescents (between the ages of 6 and 17 years, inclusive).
Severe Skin and Hypersensitivity Reactions: Severe, potentially life-threatening, and fatal skin reactions have been reported with INTELENCE; Stevens-Johnson Syndrome and toxic epidermal necrolysis have been rarely (< 0.1%) reported. Hypersensitivity reactions including DRESS (Drug Rash with Eosinophilia and Systemic Symptoms) have also been reported and were characterized by rash, constitutional findings, and infrequently organ dysfunction, including hepatic failure. Discontinue INTELENCE immediately if signs or symptoms of severe skin reactions or hypersensitivity reactions develop (including, but not limited to, severe rash or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, eosinophilia). Clinical status including liver transaminases should be monitored and appropriate therapy initiated. Delay in stopping INTELENCE treatment after the onset of severe rash may result in a life-threatening reaction.
Rash: Rash has been reported with INTELENCE. Most frequently, rash was mild to moderate, occurred in the second week of therapy and was infrequent after week 4. Rash was mostly self-limiting and generally resolved within 1 to 2 weeks on continued therapy. The incidence of rash was higher in female.
Elderly: Experience in geriatric patients is limited: In the Phase III trials, 6 patients aged 65 years or older and 53 patients aged 56-64 years received INTELENCE. The type and incidence of adverse events in patients > 55 years of age were similar to the ones in younger patients.
Patients with coexisting conditions
Liver disease: No dose adjustment is required in patients with mild or moderate hepatic impairment (Child-Pugh score A or B). The pharmacokinetics of INTELENCE have not been studied in patients with severe hepatic impairment (Child-Pugh score C).
Renal disease: Since the renal clearance of etravirine is negligible (< 1.2%), a decrease in total body clearance is not expected in patients with renal impairment. No special precautions or dose adjustments are required in patients with renal impairment. As etravirine is highly bound to plasma proteins, it is unlikely that it will be significantly removed by haemodialysis or peritoneal dialysis.
Fat redistribution: Combination antiretroviral therapy (CART) has been associated with redistribution of body fat (lipodystrophy) in HIV infected patients. The long-term consequences of these events are currently unknown. Knowledge about the mechanism is incomplete. A connection between visceral lipomatosis and PIs and lipoatrophy and nucleoside reverse transcriptase inhibitors (NRTIs) has been hypothesised. A higher risk of lipodystrophy has been associated with individual factors such as older age and with drug related factors such as longer duration of antiretroviral treatment and associated metabolic disturbances. Clinical examination should include evaluation for physical signs of fat redistribution.
Immune reconstitution syndrome: In HIV infected patients with severe immune deficiency at the time of institution of CART, an inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise and cause serious clinical conditions, or aggravation of symptoms. Typically, such reactions have been observed within the first weeks or months of initiation of CART. Relevant examples are cytomegalovirus retinitis, generalised and/or focal mycobacterial infections and Pneumocystis jirovecii pneumonia. Any inflammatory symptoms should be evaluated and treatment instituted when necessary. Autoimmune disorders (such as Graves’ disease and autoimmune hepatitis) have also been reported to occur in the setting of immune reactivation; however, the time to onset is more variable, and can occur many months after initiation of treatment.
Lactose intolerance and lactase deficiency: Each tablet of intelence 100 mg contains 160 mg of lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
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The most frequent (incidence ≥ 10%) adverse reactions of all intensities reported for etravirine were rash, diarrhoea, nausea and headache. In the Phase III studies, the rates of discontinuation due to any adverse reaction were 7.2% in patients receiving etravirine. The most common adverse reaction leading to discontinuation was rash.
See prescribing information for full details.
Medicinal products that affect etravirine exposure: Etravirine is metabolised by cytochrome P450 (CYP) 3A, CYP2C9 and CYP2C19 followed by glucuronidation of the metabolites by uridine diphosphate glucuronosyl transferase (UDPGT). Medicinal products that induce CYP3A, CYP2C9, or CYP2C19 may increase the clearance of etravirine resulting in lowered plasma concentrations of etravirine. Co-administration of INTELENCE and medicinal products that inhibit CYP3A, CYP2C9, or CYP2C19 may decrease the clearance of etravirine and may result in increased plasma concentrations of etravirine.
Medicinal products that are affected by the use of etravirine: Etravirine is a weak inducer of CYP3A. Co-administration of INTELENCE with medicinal products primarily metabolised by CYP3A may result in decreased plasma concentrations of such medicinal products, which could decrease or shorten their therapeutic effects. Etravirine is a weak inhibitor of CYP2C9 and CYP2C19. Etravirine is also a weak inhibitor of P-glycoprotein but not a substrate. Co-administration with medicinal products primarily metabolised by CYP2C9 or CYP2C19 or transported by P-glycoprotein may result in increased plasma concentrations of such medicinal products, which could increase or prolong their therapeutic effect or adverse events profile.
For full details see prescribing information.
Pregnancy and Lactation
Pregnancy: There are no adequate and well-controlled studies with etravirine in pregnant women. Studies in animals have not shown evidence of developmental toxicity or effect on reproductive function and fertility. INTELENCE should be used during pregnancy only if the potential benefit justifies the potential risk.
Lactation: Etravirine is excreted in human milk. As a general rule, it is recommended that mothers infected by HIV do not breastfeed their babies
under any circumstances in order to avoid transmission of HIV.
Fertility: No human data on the effect of etravirine on fertility are available. In rats, there was no effect on mating or fertility with INTELENCE treatment.
There is no specific antidote for overdose with INTELENCE. Human experience of overdose with INTELENCE is limited. Treatment of overdose with INTELENCE consists of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient. If indicated, elimination of unabsorbed active substance is to be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid in removal of unabsorbed active substance. Since etravirine is highly protein bound, dialysis is unlikely to result in significant removal of the active substance.