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Invirase is a brand name for Saquinavir. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: Invirase is indicated for the treatment of HIV-1 infected adult patients. Invirase should only be given in combination with ritonavir and other antiretroviral medicinal products (see section 4.2).
Verbatim from this product's EMA label. Tap a section to expand.
Posology Therapy with Invirase should be initiated by a physician experienced in the management of HIV infection. In combination with ritonavir The recommended dose of Invirase is 1000 mg (2 x 500 mg film-coated tablets) two times daily with ritonavir 100 mg two times daily in combination with other antiretroviral agents.
For treatment-naive patients initiating treatment with Invirase/ritonavir, the starting recommended dose of Invirase is 500 mg (1 x 500 mg film-coated tablet) two times daily with ritonavir 100 mg two times daily in combination with other antiretroviral agents for the first 7 days of treatment.
After 7 days, the recommended dose of Invirase is 1000 mg two times daily with ritonavir 100 mg two times daily in combination with other antiretroviral agents. 5), without a wash-out period, should however initiate and continue Invirase at the standard recommended dose of 1000 mg two times daily with ritonavir 100 mg two times daily.
Renal impairment:
No dosage adjustment is necessary for patients with mild to moderate renal impairment. 4).
Hepatic impairment:
No dosage adjustment is necessary for HIV-infected patients with mild hepatic impairment. No dosage adjustment seems warranted for patients with moderate hepatic impairment based on limited data. Close monitoring of safety (including signs of cardiac arrhythmia) and of virologic response is Medicinal product no longer authorised 3 recommended due to increased variability of the exposure in this population.
4).
Paediatric population:
The safety and activity of saquinavir boosted with ritonavir in HIV-infected patients less than 2 years have not been established. No dose recommendations for paediatric patients ≥2 years of age could be established that are both effective and below thresholds of concern for QT and PR interval prolongation.
Adults over 60 years:
The experience with Invirase in adults over 60 years is limited. 2).
a. Summary of the safety profile Limited data is available from two clinical studies where the safety of saquinavir soft capsule (1000 mg twice daily) used in combination with low dose ritonavir (100 mg twice daily) for at least 48 weeks was studied in 311 patients.
e. adverse reactions) were reported most frequently: nausea, diarrhoea, fatigue, vomiting, flatulence, and abdominal pain. The following adverse events were reported with the highest severity (grades 3 and 4): anaemia, diabetes mellitus, diarrhoea, nausea, vomiting and fatigue.
For comprehensive dose adjustment recommendations and drug-associated adverse reactions for ritonavir and other medicinal products used in combination with saquinavir, physicians should refer to the Summary of Product Characteristics for each of these medicinal products.
b. Tabulated list of adverse reactions Adverse reactions from two pivotal studies of saquinavir soft capsule (1000 mg twice daily) used in combination with low dose ritonavir (100 mg twice daily) for at least 48 weeks are summarised in Table 2.
Also included are serious and non-serious adverse reactions from post-marketing spontaneous reports for which a causal relationship to saquinavir cannot be excluded. Medicinal product no longer authorised 23 Adverse reactions are presented according to the MedDRA system organ classification.
The frequency groupings according to MedDRA convention are:
Very common (≥ 1/10); common (≥ 1/100 to <1/10); uncommon (≥ 1/1,000 to <1/100); rare (≥ 1/10,000 to <1/1,000); very rare (<1/10,000); not known (frequency cannot be estimated from the available data).
Table 2:
Incidences of Adverse Reactions and marked laboratory abnormalities in clinical studies and post-marketing experience in adult patients. Body System Frequency of reaction Adverse reactions Blood and the lymphatic system disorders Very common Decreased platelet count Common Anaemia, decreased haemoglobin, decreased lymphocyte count, decreased white blood cell count Uncommon Neutropenia Eye Disorders Uncommon Visual impairment Immune System Disorders Common Hypersensitivity Metabolism and nutrition disorders Very common Increased blood cholesterol, increased blood triglycerides Common Diabetes mellitus, anorexia, increased appetite Uncommon Decreased appetite Psychiatric Disorders Common Decreased libido, sleep disorder Nervous System Disorder Common Paraesthesia, peripheral neuropathy, dizziness, dysgeusia, headache Uncommon Somnolence, convulsions Respiratory, thoracic and mediastinal disorders Common Dyspnoea Gastrointestinal disorders Very common Diarrhoea, nausea Common Vomiting, abdominal distension, abdominal pain, upper abdominal pain, constipation, dry mouth, dyspepsia, eructation, flatulence, lip dry, loose stools Uncommon Pancreatitis Hepato-biliary disorders Very common Increased alanine aminotransferase, increased aspartate aminotransferase, increased low density lipoprotein Common Increased blood bilirubin, increased blood amylase Uncommon Hepatitis, jaundice Renal and urinary disorders Common Increased blood creatinine Uncommon Renal impairment Skin and subcutaneous tissue disorders Medicinal product no longer authorised 24 Body System Frequency of reaction Adverse reactions Common Alopecia, dry skin, eczema, lipoatrophy, pruritus, rash Uncommon Stevens Johnson syndrome, dermatitis bullous Musculoskeletal and connective tissue disorders Common Muscle spasms General disorders and administration site conditions Common Asthenia, fatigue, increased fat tissue, malaise Uncommon Mucosal ulceration c.
Considerations when initiating Invirase therapy:
Invirase should not be given as the sole protease inhibitor. 2). Invirase is not recommended for use in combination with cobicistat as dosing recommendations for this combination have not been established. Patients should be informed that saquinavir is not a cure for HIV infection and that they may continue to acquire illnesses associated with advanced HIV infection, including opportunistic infections.
Patients should also be advised that they might experience undesirable effects associated with co- administered medications. 1). 3). Medicinal product no longer authorised 4 Since the magnitude of QT and PR prolongation increases with increasing concentrations of saquinavir, the recommended dose of ritonavir-boosted Invirase should not be exceeded.
Ritonavir- boosted Invirase at a dose of 2000 mg once daily with ritonavir 100 mg once daily has not been studied with regard to the risk of QT prolongation and is not recommended. Other medicinal products known to increase the plasma concentration of ritonavir-boosted Invirase should be used with caution.
Women and elderly patients may be more susceptible to drug-associated effects on the QT and/or PR interval. g. 5). If signs or symptoms suggesting cardiac arrhythmia occur, continuous monitoring of ECG should be performed. Ritonavir-boosted Invirase should be discontinued if arrhythmias are demonstrated, or if prolongation occurs in the QT or PR interval.
Patients initiating therapy with ritonavir-boosted Invirase: - An ECG should be performed on all patients prior to initiation of treatment: patients with a QT interval > 450 msec should not use ritonavir-boosted Invirase. For patients with a QT interval < 450 msec, an on treatment ECG is recommended.
- For treatment-naïve patients initiating treatment with Invirase/ritonavir 500/100 mg two times daily for the first 7 days of treatment followed by Invirase 1000 mg two times daily with ritonavir 100 mg two times daily after 7 days and with a baseline QT interval < 450 msec, an on-treatment ECG is suggested after approximately 10 days of therapy.
g. 5). 5)
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
Other brands of Saquinavir in European Union.
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4). 4). Increased CPK, myalgia, myositis and rarely, rhabdomyolysis have been reported with protease inhibitors, particularly in combination with nucleoside analogues. Cases of osteonecrosis have been reported, particularly in patients with generally acknowledged risk factors, advanced HIV disease or long-term exposure to combination antiretroviral therapy (CART).
4). In HIV-infected patients with severe immune deficiency at the time of initiation of combination antiretroviral therapy (CART), an inflammatory reaction to asymptomatic or residual opportunistic infections may arise. 4). d. 5 mg/kg bid for body weight from 15 to 40 kg and 100 mg bid for body weight >40 kg) has been studied in paediatric patients aged 4 months to 6 years old.
Four patients in the study experienced five adverse events that were considered related to trial treatment. These events were vomiting (3 patients), abdominal pain (1 patient) and diarrhoea (1 patient). No unexpected adverse events were observed in this study.
Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system listed in Appendix V.
- Patients demonstrating a subsequent increase in QT-interval to > 480 msec or prolongation over pre-treatment by > 20 msec should discontinue ritonavir-boosted Invirase. 5). - For patients with a baseline QT interval < 450 msec, an on-treatment ECG should be performed.
For patients demonstrating a subsequent increase in QT-interval to > 480 msec or increase by > 20 msec after commencing concomitant therapy, the physician should use best clinical judgment to discontinue either ritonavir-boosted Invirase or the concomitant therapy or both.
, chest palpitations, syncope, presyncope) to their physician. - Physicians should enquire about any known familial history of sudden death at a young age as this may be suggestive of congenital QT prolongation. - Patients should be advised of the importance not to exceed the recommended dose.
- Each patient (or patient’s caregiver) should be reminded to read the Package Leaflet included in the Invirase Package.
Liver disease:
The safety and efficacy of saquinavir/ritonavir has not been established in patients with significant underlying liver disorders, therefore saquinavir/ritonavir should be used cautiously in this patient population. 3). Patients with chronic hepatitis B or C and treated with combination antiretroviral therapy are at an increased risk for severe and potentially fatal hepatic adverse events.
In case of concomitant antiviral therapy for hepatitis B or C, please refer also to the relevant product information for these medicinal products. Patients with pre-existing liver dysfunction including chronic active hepatitis have an increased frequency of liver function abnormalities during combination antiretroviral therapy and should be monitored according to standard practice.
If there is evidence of worsening liver disease in such patients, interruption or discontinuation of treatment must be considered. No dosage adjustment seems warranted for patients with moderate hepatic impairment based on limited data.
Close monitoring of safety (including signs of cardiac arrhythmia) and of virologic response is recommended due to increased variability of […]