化合物详情

Not known whether emtricitabine is distributed into human milk; ... .

ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), emtricitabine, which has an estimated vapor pressure of 1.7X10-8 mm Hg at 25 °C(SRC), determined from a fragment constant method(2), will exist in both the vapor and particulate phases in the ambient atmosphere. Vapor-phase emtricitabine is degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals(SRC); the half-life for this reaction in air is estimated to be 2.6 hours(SRC), calculated from its rate constant of 1.3X10-10 cu cm/molecule-sec at 25 °C(SRC) that was derived using a structure estimation method(3). The rate constant for the vapor-phase reaction of emtricitabine with ozone has been estimated as 7.0X10-19 cu cm/molecule-sec at...

Using a structure estimation method based on molecular connectivity indices(1), the Koc of emtricitabine can be estimated to be 55(SRC). According to a classification scheme(2), this estimated Koc value suggests that emtricitabine is expected to have high mobility in soil.

An estimated BCF of 3 was calculated in fish for emtricitabine(SRC), using a log Kow of -0.43(1) and a regression-derived equation(2). According to a classification scheme(3), this BCF suggests the potential for bioconcentration in aquatic organisms is low(SRC).

The Henry's Law constant for emtricitabine is estimated as 1.1X10-17 atm-cu m/mole(SRC) using a fragment constant estimation method(1). This Henry's Law constant indicates that emtricitabine is expected to be essentially nonvolatile from water and moist soil surfaces(2). Emtricitabine is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 1.7X10-8 mm Hg(SRC), determined from a fragment constant method(3).

The rate constant for the vapor-phase reaction of emtricitabine with photochemically-produced hydroxyl radicals has been estimated as 1.3X10-10 cu cm/molecule-sec at 25 °C(SRC) using a structure estimation method(1). This corresponds to an atmospheric half-life of about 2.6 hours at an atmospheric concentration of 5X10+5 hydroxyl radicals per cu cm(1). The rate constant for the vapor-phase reaction of emtricitabine with ozone has been estimated as 7.0X10-19 cu cm/molecule-sec at 25 °C(SRC) that was derived using a structure estimation method(1). This corresponds to an atmospheric half-life of about 16 days at an atmospheric concentration of 7X10+11 ozone molecules per cu cm(2). Emtricitabine is not expected to undergo hydrolysis in the environment due to the lack of functional groups th...

While data specific to emtricitabine were not located(2013, SRC), the literature suggests that some pharmaceutically active compounds originating from human and veterinary therapy are not eliminated completely in municipal sewage treatment plants and are therefore discharged into receiving waters(1). Wastewater treatment processes often were not designed to remove them from the effluent(2). Selected organic waste compounds may be degrading to new and more persistent compounds that may be released instead of or in addition to the parent compound(2).

EXPERIMENTAL: The aim was to evaluate emtricitabine (FTC) and tenofovir (TFV) neonatal ingestion through breast milk. Median TFV and FTC breast milk doses represented 0.03% and 2%, respectively, of the proposed oral infant doses. Neonatal simulated plasma concentrations were extremely low for TFV but between the half-maximal inhibitory concentration and the adult minimal expected concentration for FTC. The rare children who will acquire HIV despite TDF-FTC therapy will need to be monitored for viral resistance acquisition.

Emtricitabine's production and use as an antiviral(1) and in the treatment of AIDS(2) may result in its release to the environment through various waste streams(SRC).

Occupational exposure to emtricitabine may occur through inhalation of dust and dermal contact with this compound at workplaces where entecavir is produced or used. Use data indicate that the general population may be exposed to emtricitabine via medical administration of this compound for the treatment of viral infection. (SRC)

Emtricitabine's production and use as an antiviral and in the treatment of AIDS may result in its release to the environment through various waste streams. If released to air, an estimated vapor pressure of 1.7X10-8 mm Hg at 25 °C indicates emtricitabine will exist in both the vapor and particulate phases in the atmosphere. Vapor-phase emtricitabine will be degraded in the atmosphere by reaction with photochemically-produced hydroxyl radicals and ozone; the half-lives for these reactions in air are estimated to be 2.6 hours and 16 days. Particulate-phase emtricitabine will be removed from the atmosphere by wet or dry deposition. Emtricitabine does not absorb light at wavelengths >290 nm and, therefore, is not expected to be susceptible to direct photolysis by sunlight. If released to so...

The potential for drug interactions with emtricitabine has been studied in combination with indinavir, stavudine, famciclovir, and tenovir disoproxil fumarate. There were no clinically significant drug interactions for any of these drugs.

There is little evidence for direct hepatotoxicity of emtricitabine and it has not been specifically implicated in cases of lactic acidosis with steatosis and hepatic failure. However, patients with chronic hepatitis B can experience a flare of the underlying hepatitis during emtricitabine therapy. These flares occur either at the start therapy (treatment flares), with the development of antiviral resistance (breakthrough flares), or when therapy is abruptly stopped (withdrawal flares). Treatment flares occur in 5% to 10% of patients, are usually transient and asymptomatic, and rarely require dose modification or discontinuation of therapy. In contrast, withdrawal flares occur in 15% to 30% of patients, but can be symptomatic and severe, in rare instances (~1%) leading to acute liver fa...

Emtricitabine combined with tenofovir used as pre-exposure prophylaxis (PrEP) is safe with short-term use of about 2 to 3 years. The common adverse effects associated with this combination include gastrointestinal symptoms, headache, nausea, and depression. This combination has correlated with a decreased creatine clearance that improves with discontinuation of the drug. PrEP can cause a decline in GFR initially, but this decline becomes more gradual the longer a person takes PrEP. PrEP was not associated with severe renal dysfunction, but a decreased GFR was a common presenting finding in patients over the age of 40. This combination has also correlated with a decrease in bone mineral density that returned to normal levels with discontinuation of the drug. Research has not shown the de...

Emtricitabine, along with the other drugs in the nucleoside reverse transcriptase inhibitor (NRTI) category, interacts with mitochondrial DNA polymerase, causing myopathy and neuropathy. This toxic interaction also has associations with hepatic steatosis and lactic acidosis. Emtricitabine has not shown any adverse effects on the mitochondrial function of developing fetuses and is not known to be teratogenic. There has been no evidence of emtricitabine affecting the fertility rates of women taking the drug.

/SIGNS AND SYMPTOMS/ Lactic acidosis and severe hepatomegaly with steatosis, including fatalities, have been reported in patients receiving nucleoside reverse transcriptase inhibitors (NRTIs), including emtricitabine, in conjunction with other antiretroviral agents. Most reported cases have involved women; obesity and long-term therapy with a nucleoside analog also may be risk factors.

References: DOI:10.1016/j.drudis.2019.09.022

/GENOTOXICITY/ Emtricitabine was not genotoxic in the reverse mutation bacterial test (Ames test), mouse lymphoma or mouse micronucleus assays.

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontaminati...

Relevant published information was not found as of the revision date.