Chemical formula: C₃₂H₄₅N₃O₄S Molecular mass: 567.782 g/mol PubChem compound: 64143
Nelfinavir interacts in the following cases:
No treatment-related adverse reactions were seen in animal reproductive toxicity studies in rats at doses providing systemic exposure comparable to that observed with the clinical dose. Clinical experience in pregnant women is limited. Nelfinavir should be given during pregnancy only if the expected benefit justifies the possible risk to the foetus.
It is recommended that HIV-infected women must not breast-feed their infants under any circumstances in order to avoid transmission of HIV. Studies in lactating rats showed that nelfinavir is excreted in breast milk. There is no data available on nelfinavir excretion into human breast milk. Mothers must be instructed to discontinue breast-feeding if they are receiving nelfinavir.
Nelfinavir has no or negligible influence on the ability to drive and use machines.
The safety of the nelfinavir 250 mg tablet was studied in controlled clinical trials with over 1300 patients. The majority of patients in these studies received either 750 mg TID either alone or in combination with nucleoside analogues or 1250 mg BID in combination with nucleoside analogues. The following adverse events with an at least possible relationship to nelfinavir (i.e. adverse reactions) were reported most frequently: diarrhoea, nausea, and rash. Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.
Adverse reactions in clinical studies are summarised in Table 1. The list also includes marked laboratory abnormalities that have been observed with nelfinavir (at 48 weeks).
Table 1. Incidences of Adverse Reactions and marked laboratory abnormalities from the phase II and phase III studies. (Very common (≥10%); common (≥1% and <10%):
A total of approximately 400 patients received nelfinavir in paediatric treatment trials (Studies 524, 556, PACTG 377/725, and PENTA-7) for up to 96 weeks. The adverse reaction profile seen during paediatric clinical trials was similar to that for adults. Diarrhoea was the most commonly reported adverse event in children. Neutropenia/leukopenia was the most frequently observed laboratory abnormality. During these trials less than 13% of patients in total discontinued treatment due to adverse events.
Serious and non-serious adverse reactions from post-marketing spontaneous reports (where nelfinavir was taken as the sole protease inhibitor or in combination with other antiretroviral therapy), not mentioned previously in section 4.8, for which a causal relationship to nelfinavir cannot be excluded, are summarised below. As these data come from the spontaneous reporting system, the frequency of the adverse reactions is not confirmed.
Uncommon (≥0.1% - ≤1%): hypersensitivity including bronchospasm, pyrexia, pruritus, facial oedema and rash maculo-papular or dermatitis bullous.
Uncommon – rare (≥0.01% - ≤1%): Combination antiretroviral therapy has been associated with redistribution of body fat (Lipodystrophy aquired) in HIV patients including the loss of peripheral and facial subcutaneous fat, increased intra-abdominal and visceral fat, breast hypertrophy and dorsocervical fat accumulation (lipohypertrophy buffalo hump).
Rare (≥0.01% - ≤0.1%): new onset diabetes mellitus, or exacerbation of existing diabetes mellitus.
Uncommon (≥0.1% - ≤1%): vomiting, pancreatitis/blood amylase increased.
Rare (≥0.01% - ≤0.1%): abdominal distension,
Rare (≥0.01% - ≤0.1%): hepatitis, hepatic enzymes increased and jaundice when nelfinavir is used in combination with other antiretroviral agents.
Rare (≥0.01% - ≤0.1%): Blood creatine phosphokinase increased, myalgia, myositis and rhabdomyolysis have been reported with PIs, particularly in combination with nucleoside analogues.
Rare (≥0.01% - ≤0.1%): increased spontaneous haemorrhage in patients with haemophilia.
Very rare (≤0.01%), including isolated reports: Erythema multiforme.
Additional adverse reactions have been reported in the post-marketing experience and are listed below. As these data come from the spontaneous reporting system, the frequency of the adverse reactions is unknown: hypertriglyceridemia, anaemia, blood lactic acid increased, and pneumonia.
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). The frequency of this is unknown.
Combination antiretroviral therapy has been associated with metabolic abnormalities such asblood triglycerides increased, blood cholesterol increased, insulin resistance, hyperglycaemia and hyperlactaemia. The frequency of this is unknown.
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. The frequency of this is unknown.
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