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Product Code: 121314
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Price: 2,670EGP
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- Indications: Sofosbuvir is indicated in combination with other medicinal products for the treatment of chronic hepatitis C (CHC) in adults.

- Pharmacotherapeutic group: Direct-acting antiviral.

- Mechanism of action: Sofosbuvir is a pan-genotypic inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is essential for viral replication. Sofosbuvir is a nucleotide prodrug that undergoes intracellular metabolism to form the pharmacologically active uridine analog triphosphate (GS-461203), which can be incorporated into HCV RNA by the NS5B polymerase and acts as a chain terminator. In a biochemical assay, GS-461203 inhibited the polymerase activity of the recombinant NS5B from HCV genotype 1b, 2a, 3a and 4a with a 50% inhibitory concentration (IC50) value ranging from 0.7 to 2.6 ?M. GS-461203 (the active metabolite of sofosbuvir) is not an inhibitor of human DNA and RNA polymerases nor an inhibitor of mitochondrial RNA polymerase.

- Dose: . The recommended dose is one 400 mg tablet, taken orally, once daily with food. . Sofosbuvir should be used in combination with other medicinal .

especial describtion :

Pharmacokinetic data
Bioavailability 92%
Protein binding 61–65%
Metabolism Quickly activated to triphosphate
Biological half-life 0.4 hrs (sofosbuvir)
27 hrs (active metaboliteGS-331007)
Excretion 80% feces, 14% urine (mostly as GS-331007)

 

Sofosbuvir is a prodrug using the ProTide biotechnology strategy. It is metabolized to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-triphosphate. The triphosphate serves as a defective substrate for the NS5B protein, which is the viral RNA polymerase, thus acts as an inhibitor of viral RNA synthesis. Although sofosbuvir has a 3' hydroxyl group to act as a nucleophile for an incoming NTP, a similar nucleotide analogue, 2'-deoxy-2'-α-fluoro-β-C-methylcytidine, is proposed to act as a chain terminator because the 2' methyl group of the nucleotide analogue causes a steric clash with an incoming NTP.Sobosbuvir would act in a similar way.

Prior to the discovery of sofosbuvir, a variety of nucleoside analogs had been examined as antihepatitis C treatments, but these exhibited relatively low potency. This low potency arises in part because the enzymatic addition of the first of the three phosphate groups of the triphosphate is slow. The design of sofosbuvir, based on the protide approach, avoids this slow step by building the first phosphate group into the structure of the drug during synthesis. Additional groups are attached to the phosphorus to temporarily mask the two negative charges of the phosphate group, thereby facilitating entry of the drug into the infected cell. The NS5B protein is a RNA-dependent RNA polymerase critical for the viral reproduction cycle.

Adverse effects

As sofosbuvir was combined with other drugs such as ribavirin and interferon in clinical safety trials, only the adverse effects of these combinations have been evaluated. Common side effects are fatigue, headache, nausea, rash, and irritability. Most side effects are significantly more common in interferon-containing regimens as compared to interferon-free ones. For example, fatigue and headache are nearly cut in half, influenza-like symptoms are reduced to 3–6% as compared to 16–18%, and neutropenia is almost absent in interferon-free treatment .

Pregnancy :

Sofosbuvir alone has been assigned a Pregnancy Category B by the FDA. Animal studies in pregnant rats and rabbits showed no effects on the development of the fetus and there have been no similar studies for Sofosbuvir in pregnant women.

Sofosbuvir used in combination with ribavirin or peginterferon and ribavirin has been assigned a Pregnancy Category X by the FDA. Ribavirin has been shown to cause fetal birth defects and possibly death and should be avoided in both the pregnant female and her sexual partner. Since sofosbuvir is commonly used together with ribavirin and/or peginterferon, it is recommended that sofosbuvir used in combination should be avoided in pregnant females and their male sexual partners in order to reduce harmful fetal defects caused by ribavirin. Females who could potentially become pregnant should undergo a pregnancy test 2 months prior to starting the sofosbuvir/ribavirin/peginterferon combination treatment, monthly throughout the duration of the treatment, and 6 months post-treatment to reduce the risk of fetal harm in case of accidental pregnancy.Positive pregnancy results should be reported to the patient's health care provider immediately.

DRUG INTERACTIONS OF SOFOSBUVIR

Many patients with HCV have concomitant illnesses such as HIV requiring anti-retroviral therapy, or hepatocellular carcinoma/decompensated liver disease requiring liver transplants along with immunosuppressant medication. Thus, it is very important to study the possible drug interactions that may occur in these patients, who also require treatment of HCV. Studies have shown no clinically significant interactions between sofosbuvir and the following drugs: Cyclosporine, tacrolimus, methadone, efavirenz, rilpivirine, darunavir/ritonavir, raltegravir, and tenofovir. No dose adjustments are required in patients receiving these drugs along with sofosbuvir. As sofosbuvir is being tried for all-oral regimens combined with other directly acting antiviral agents, interactions with these drugs have also been studied. No clinically significant interactions have been found between sofosbuvir and daclatasvir, ledipasvir, or GS-9669. A 54-year-old liver transplant recipient with HCV type 1b and severe recurrent cholestatic hepatitis was given daclatasvir (HCV NS5A inhibitor) plus sofosbuvir for 24 weeks; SVR at 36 was achieved, and the level and dose of tacrolimus remained stable in this patient

 

 

 

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