fosamprenavir
Regulatory sources consulted
Approved indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents.
Contraindications
Absolute
- Hypersensitivity to fosamprenavir or amprenavir; expressly contraindicated CYP3A/CYP2D6 combinations, including rifampin, alfuzosin, pimozide, oral midazolam, triazolam, ergots, simvastatin/lovastatin, and sildenafil for PAH.
Clinical warnings
- It may cause severe rash, SJS/TEN, and hypersensitivity reactions; discontinue for severe reactions. It contains a sulfonamide group. — DailyMed, set_id 5cd1eead-9fc1-426c-bee8-214ffa7d9dc1
- Major warning · It may cause hepatotoxicity, hyperglycemia, dyslipidemia, hemolytic anemia, and increased bleeding in hemophilia. — DailyMed, set_id 5cd1eead-9fc1-426c-bee8-214ffa7d9dc1
Drug interactions
- HighCYP3A substrates, inhibitors, or inducers
Mechanism: Fosamprenavir/amprenavir and ritonavir cause relevant bidirectional interactions.
Recommendation: Perform complete reconciliation; do not use contraindicated combinations and adjust others according to labeling.
DailyMed, set_id 5cd1eead-9fc1-426c-bee8-214ffa7d9dc1
Adverse events
Common (≥1%)
Nausea, diarrhea, vomiting, headache, and rash
Rare but serious
SJS/TEN, hepatotoxicity, hemolytic anemia, and pancreatitis
Pregnancy and lactation
During pregnancy, fosamprenavir 700 mg with ritonavir 100 mg twice daily should be continued only if the person was already stable on it before pregnancy and had a viral load <50 copies/mL; close virologic monitoring is required. Do not breastfeed if you have HIV and receive treatment.
Recent literature (PubMed)
Laryngopharyngeal reflux (LPR) manifests as a variety of nonspecific upper aerodigestive tract symptoms. Rather than a single disorder, LPR may be conceived of as a spectrum of subtypes with varying clinical presentations. LPR signs and symptoms arise from the direct and/or indirect effects of refluxate, physical and molecular injury of the mucosa, and neurologic responses to esophageal events. Specific constituents of refluxate exert distinct mucosal responses and immediate or delayed effects resulting in transient or persistent symptoms and/or laryngeal hypersensitivity. While the complex etiology of LPR presents challenges to its diagnosis and management, tools that aid the identification of LPR subtypes can provide insight into treatment decision-making. Hypopharyngeal-esophageal multichannel intraluminal impedance-pH monitoring provides detailed analysis of reflux events, enabling the development of individualized treatment plans, yet cost and availability limit its widespread use. Alginates offer temporary symptom relief and antireflux surgery may provide benefit when symptoms are recalcitrant to other approaches. Pepsin inhibitors hold promise as a medical therapy when surgery is not an option. Laryngeal hypersensitivity should be considered as part of a comprehensive therapeutic approach. Promising medical and scientific research continues to yield new insights into the complex etiology of LPR and novel strategies for its diagnosis and management.
Multiple factors may affect combined antiretroviral therapy (cART). We investigated the impact of food, beverages, dietary supplements, and alcohol on the pharmacokinetic and pharmacodynamic parameters of 33 antiretroviral drugs. Systematic review in adherence to PRISMA guidelines was performed, with 109 reports of 120 studies included. For each drug, meta-analyses or qualitative analyses were conducted. We have found clinically significant interactions with food for more than half of antiretroviral agents. The following drugs should be taken with or immediately after the meal: tenofovir disoproxil, etravirine, rilpivirine, dolutegravir, elvitegravir, atazanavir, darunavir, lopinavir, nelfinavir, ritonavir, saquinavir. Didanosine, zalcitabine, zidovudine, efavirenz, amprenavir, fosamprenavir, and indinavir should be taken on an empty stomach for maximum patient benefit. Antiretroviral agents not mentioned above can be administered regardless of food. There is insufficient evidence available to make recommendations about consuming juice or alcohol with antiretroviral drugs. Resolving drug-food interactions may contribute to maximized cART effectiveness and safety. Múltiples factores pueden afectar la terapia antirretroviral combinada (cART). Investigamos el impacto de los alimentos, las bebidas, los suplementos dietéticos y el alcohol en los parámetros farmacocinéticos y farmacodinámicos de 33 medicamentos antirretrovirales. Se realizó la revisión sistemática en apego a las guías PRISMA, con 109 reportes de 120 estudios incluidos. Para cada fármaco se realizaron metanálisis o análisis cualitativos. Hemos encontrado interacciones clínicamente significativas con alimentos para más de la mitad de los fármacos antirretrovirales. Los siguientes medicamentos deben tomarse durante o inmediatamente después de comer: tenofovir, disoproxil, etravirina, rilpivirine, dolutegravir, elvitegravir, atazanavir, darunavir, lopinavir, nelfinavir, ritonavir, saquinavir. Didanosina, zalc
Background: Protease inhibitors (PIs) are believed to affect insulin sensitivity. We aimed to analyze the effect of PIs on insulin sensitivity and the onset of diabetes mellitus (DM) in patients with HIV. Methodology: We searched PubMed, Google Scholar, ClinicalTrals.gov, and the WHO International Clinical Trials Registry Platform till November 2020 for randomized controlled trials (RCTs) that studied the effects of PIs on insulin sensitivity and DM in patients with HIV. We followed the PRISMA and PICOS frameworks to develop the search strategy. We used the random-effects meta-analysis model to estimate the mean difference (MD), standardized mean difference (SMD), and risk ratios for our outcomes, using Stata 14 software. Results: We included nine RCTs that enrolled 1,000 participants, with their ages ranging from 18 to 69 years. The parameters and investigations used in the studies to determine insulin sensitivity were glucose disposal rates, hyperglycemia, and mean glucose uptake. The majority of results showed an association between PIs and insulin sensitivity. The pooled analysis showed no statistically significant difference in insulin sensitivity with atazanavir, whether the study was performed on healthy individuals for a short term or long term in combination with other drugs like tenofovir or emtricitabine [SMD = 0.375, 95% CI (0.035, 0.714)]. The analysis showed reduced glucose disposal rates and hence reduced insulin sensitivity with lopinavir (heterogeneity chi-squared = 0.68, I-squared [variation in SMD attributable to heterogeneity] = 0.0%, p = 0.031). The heterogeneity with chi-squared was substantial (61-80%), while with I-squared was not significant (0-40%), p = 0.031). Less adverse events were observed with atazanavir than with lopinavir [RR = 0.987, 95% CI (0.849, 1.124)]. Darunavir and indinavir did not demonstrate any significant changes in insulin sensitivity. Most of the studies were found to have a low risk of bias. Conclusions: There are sig
Advances in antiretroviral therapy led to an increase in life expectancy among people living with human immunodeficiency virus (HIV). As aging is characterized by several physiological changes that can influence pharmacokinetics (PK), this systematic review aims to describe the impact of aging on the PK of antiretrovirals (ARV) approved by the Food and Drug Administration (FDA) before 2005. Searches were performed in BVS, EMBASE, and PubMed databases for publications until June 2024. Peer-reviewed published studies were included if they met the following criteria: adults (≥ 18 years) living with HIV; reporting at least one PK parameter or plasma concentration of any ARV approved by the US FDA before 2005 and still used in the clinic: lamivudine (3TC), emtricitabine (FTC), tenofovir disoproxil fumarate (TDF), abacavir (ABC), zidovudine (ZDV), efavirenz (EFV), nevirapine (NVP), atazanavir (ATV), lopinavir (LPV), ritonavir (RTV), tipranavir (TPV), and fosamprenavir (FPV); PK parameters stratified per age group as young (aged 18-49 years) or older (age ≥ 50 years) adults; and manuscripts published in English, Portuguese, or Spanish. All studies were evaluated for risk of bias. The review protocol was registered in the PROSPERO database (registration no. CRD42023463092). Among 106 studies included, only 22 evaluated the PK of participants aged 50 years or older and only 5 studies compared the PK between young and older adults for ATV, RTV, EFV, and 3TC. Our analysis revealed an increase in minimal concentration (Cmin) values for LPV, RTV, and ATV in older adults. While increased values of the area under the curve (AUC) and maximum concentration (Cmax) were observed in older adults using ATV, 3TC, and FTC, no differences in PK were apparent between young and older adults for ABC and EFV, with no estimation possible for ZDV. Exposure to 3TC, TDF, FTC, ATV, LPV, and RTV increases with age, while exposure to ABC and EFV appears to be unaffected. Despite the large quantity of