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Valtrex order online

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Analog

☘ Active Ingredient: Valacyclovir

☘ Other names for this medication:
Actaval, Bagovir, Herclov, Lizhuwei, Rapivir, Talavir, Vadiral, Valaciclovir, Valaciclovirum, Valavir, Valcivir, Valcyclor, Valherpes, Valpridol, Valvir, Valvirex, Valztrex, Viramixal, Viranet, Virval, Zelitrex, Zeltrix, Zosvir

☘ Pharmachologic effect
Valacyclovir is an antiviral agent, it is an L-valine ester of acyclovir. Acyclovir is an analogue of a purine nucleoside (guanine).
In the human body, valaciclovir is rapidly and almost completely converted into acyclovir and valine, presumably under the influence of the enzyme valacyclovirhydrolase.
Valaciclovirum is a specific inhibitor of herpes viruses with in vitro activity against Herpes simplex virus types 1 and 2, Varicella zoster virus, Varicella zoster, cytomegalovirus (CMV), Epstein-Barr virus (VEB) and virus herpes simplex type 6. Acyclovir inhibits the synthesis of viral DNA immediately after phosphorylation and conversion into an active form – Valaciclovirum triphosphate.
The first stage of phosphorylation requires the activity of virus-specific enzymes. For HSV, VZV and VEB, this enzyme is viral thymidine kinase, which is present only in the cells infected with the virus. Partially, the selectivity of phosphorylation is maintained in the cytomegalovirus indirectly through the product of the phosphotransferase UL97 gene. This need to activate acyclovir with a specific viral enzyme largely explains its selectivity. The process of phosphorylation of acyclovir (conversion from mono- to triphosphate) is completed by cellular kinases.

Valaciclovirum triphosphate competitively inhibits viral DNA polymerase and, being an analogue of a nucleoside, is inserted
into viral DNA, which leads to an obligate rupture of the chain, stopping the synthesis of DNA and, consequently, to blocking the replication of the virus.

Resistance to acyclovir is usually due to a deficiency of thymidine kinase, which leads to an excessive spread of the virus in the host. In rare cases, a decrease in sensitivity to Valaciclovirum is due to the appearance of strains of the virus with a violation of the structure of viral thymidine kinase or DNA polymerase. The virulence of these varieties of the virus resembles that of its wild strain.

Based on the results of an extensive study of HSV and VZV strains selected from patients treated with Valaciclovirum or used for prevention, it was found that viruses with reduced sensitivity to valacyclovir are extremely rare, but can be detected in rare cases in patients with severe immunity, for example, bone marrow transplant recipients or organ, patients receiving chemotherapy for malignant neoplasms, and in HIV-infected patients.
Valaciclovir contributes to the relief of pain syndrome: reduces its duration and reduces the percentage of patients with pain caused by herpes zoster, including acute postherpetic neuralgia.

☘ Pharmacokinetics
Suction
After ingestion, Valaciclovirum is well absorbed from the digestive tract, rapidly and almost completely turning into Valaciclovirum and valine. This transformation is probably carried out by the enzyme of the liver with valaciclovirhydrolase.
When taking valaciclovir in a dose of 1000 mg, the bioavailability of acyclovir is 54% and does not decrease with food intake. The pharmacokinetics of Valaciclovirum are not dose-dependent. The rate and degree of absorption decrease with increasing dose, resulting in a less proportional increase in C max in blood plasma, but in comparison with the therapeutic range of doses and lower bioavailability at doses higher than 500 mg.
Results of assessing the pharmacokinetics of Valaciclovirum when taking single doses of valaciclovir from 250 mg to 2000 mg by healthy volunteers with normal liver function

➡ Cmax – maximum concentration in blood plasma;
➡ Tmax – time to reach the maximum concentration in the blood plasma;
➡ AUC is the area under the pharmacokinetic curve “concentration-time”. The values ​​of Cmax and AUC reflect the average standard deviation.

The values ​​for Tmax reflect the median value and range of values.
Cmax valaciclovir in blood plasma is only 4% of the concentration of Valaciclovirum, the median time to achieve it is 30 to 100 min after taking the drug.

After 3 hours after taking the drug, the Valaciclovirum concentration reaches the level of quantitation or lower.
Valaciclovir and acyclovir have similar pharmacokinetic parameters after a single and multiple administration. VZV and HSV significantly do not change the pharmacokinetics of valaciclovir and acyclovir after taking Valaciclovirum inwards.

☘ Distribution
The degree of binding of Valaciclovirum to plasma proteins is very low (15%). The degree of penetration into the cerebrospinal fluid (CSF) is defined as the ratio of AUC in CSF to AUC in blood plasma and is about 25% for Valaciclovirum and 8-hydroxyacyclovir metabolite (8-OH-ACV); about 2.5% for the metabolite 9- (carboxymethoxy) methyl guanine (CMMG).

☘ Metabolism
After ingestion, Valaciclovirum is converted into Valaciclovirum and L-valine through presystemic metabolism in the intestine and / or hepatic metabolism. Valaciclovirum is converted into small metabolites: CMMG under the influence of ethyl alcohol and aldehyde dehydrohease; 8-OH-ACV under the influence of aldehyde oxidase. Approximately 88% of the total cumulative effect on blood plasma is accounted for by acyclovir, 11% by CMMG and 1% by 8-OH-ACV.  Valaciclovir and acyclovir are not metabolized by isoenzymes of the cytochrome P450 system.

☘ Excretion
In patients with normal renal function T1 / 2, acyclovir from the blood plasma after a single or multiple administration of valaciclovir is about 3 hours. Less than 1% of the accepted dose of valaciclovir is excreted by the kidneys unchanged. Valaniclovir is excreted from the body by the kidneys mainly in the form of Valaciclovirum (more than 80% of the dose) and the metabolite of acyclovir – CMMG

☘ Special patient groups
Patients with impaired renal function. Excretion of adiklovir correlates with renal function, the exposure of Valaciclovirum increases with increasing severity of renal failure. In patients with end-stage renal disease, the mean T1 / 2 Valaciclovirum after valaciclovir is approximately 14 hours compared to approximately 3 hours with normal kidney function.

Exposure of Valaciclovirum and its metabolites CMMG and 8-OH-ACV in blood plasma and CSF was evaluated in stable state after multiple administration of valacyclovir in 6 patients with normal renal function (mean CC 111 ml / min, range 91-144 ml / min) 2000 mg every 6 hours, and in 3 patients with severe renal failure (mean SC 26 ml / min, range 17-31 ml / min) receiving 1500 mg every 12 hours. With severe renal failure compared with normal renal function in blood plasma, as well as in the CSF, the concentrations of Valaciclovirum, CMMG and 8-OH-ACV would be whether in 2, 4 and 5-6 times higher, respectively. There was no difference in the degree of penetration of Valaciclovirum in the CSF (defined as the ratio of AUC to CSF ​​to AUC in plasma), CMMG or 8-GH-ACV between two populations with severe renal failure and normal renal function.

Patients with impaired liver function. Pharmacokinetic data show that in patients with hepatic insufficiency, the rate of conversion of Valaciclovirum to acyclovir is reduced, but not the degree of this transformation. T1 / 2 Valaciclovirum does not depend on liver function.

Pregnancy. A study of the pharmacokinetics of Valaciclovirum and acyclovir in late pregnancy established an increase in the daily AUC value in a stable state with a daily intake of valaciclovir 1000 mg / day, which was approximately 2 times higher than the AUC when administered at a dose of 1200 mg per day of Valaciclovirum.

HIV infection. In patients with HIV infection, the distribution and pharmacokinetic characteristics of acyclovir following oral administration of one or more doses of 1000 mg or 2000 mg of Valaciclovirum remain unchanged compared to healthy volunteers.
Organ transplantation. The scales of Valaciclovirum in patients after organ transplantation who received 2000 mg of valaciclovir 4 times / day were comparable or higher than Cmax observed in healthy volunteers who received the same dose. The established daily AUC values ​​can be characterized as significantly higher.

☘ Indications

Adults and adolescents aged 12 to 18 years
➢ treatment of infections of the skin and mucous membranes caused by HSV, including the newly identified and recurring genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis);
➢ prevention (suppression) of recurrences of infections of the skin and mucous membranes caused by HSV, including genital herpes, incl. in adults with immunodeficiency;
➢ Prevention of infections caused by cytomegalovirus (CMV), and
diseases after transplantation of parenchymal organs.

 Adults
➢ Treatment of herpes zoster (Herpes zoster) and ophthalmic herpes zoster.

☘ Dosing regimen
The drug Valtrex⋇ can be taken regardless of the meal, the tablets should be washed with water.
Treatment of infections of the skin and mucous membranes caused by HSV, including first identified and recurrent genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis)

Immunocompetent adults and adolescents aged 12 to 18 years
The recommended dose is 500 mg 2 times / day.
In case of relapse, treatment should last 3 or 5 days. In the case of a primary herpes, which can flow more severe, treatment should start as early as possible, and its duration should be increased from 5 to 10 days. In cases of recurrence of HSV, the most valid treatment is Valtrex⋇ in the prodromal period or immediately after the appearance of the first symptoms of the disease. The use of valaciclovir can prevent the development of the lesion if it is used at the first signs of symptoms of a recurrence caused by HSV.

As an alternative treatment for labial herpes, the effective use of Valtrex⋇ in a dose of 2000 mg 2 times / day for 1 day is effective. The second dose should be taken after approximately 12 hours (but not earlier than 6 hours) after taking the first dose. When using this mode of dosing, the duration of treatment should not exceed 1 day, because The excess of the duration of this course of treatment does not lead to additional clinical benefit.

Therapy should be initiated with the appearance of the earliest symptoms of herpes labialis (eg tingling, itching, burning).
Prevention (suppression) of recurrences infections of the skin and mucous membranes caused by HSV, including genital herpes, including in adults with immunodeficiency.

Immunocompetent adults and adolescents aged 12 to 18 years
In immunocompetent patients, the recommended dose is 500 mg 1 time / day. After 6-12 months of treatment, it is necessary to evaluate the effectiveness of therapy.

☘ Adults with immunodeficiency
In adults with immunodeficiency recommended, the dose is 500 mg 2 times / day. After 6-12 months of treatment, it is necessary to evaluate the effectiveness of therapy.

Prevention of infections caused by CMV and diseases after transplantation of parenchymal organs
Adults and adolescents aged 12 to 18 years
The recommended dose is 2000 mg 4 times a day, prescribed as soon as possible after transplantation. The dose should be lowered depending on the creatinine clearance. The duration of treatment is usually 90 days, but in patients with high-risk treatment can be extended.

Treatment of herpes zoster (Herpes zoster) and ophthalmic herpes zoster
Adults
The recommended dose is 1000 mg 3 times / day for 7 days.

☘ Special patient groups
Children
The effectiveness of treatment with Valtrex⋇ in children has not been studied.

☘ Elderly patients
It is necessary to take into account the possible violation of kidney function in elderly patients, the dose of Valtrex⋇ should be adjusted accordingly. It is necessary to maintain an adequate water-electrolyte balance.

☘ Patients with impaired renal function
The dose of Valtrex⋇ should be reduced in patients with severe renal impairment. Such patients need to maintain an adequate water-electrolyte balance.

◈Additional information for indications: treatment of infections of the skin and mucous membranes caused by HSV, including newly diagnosed and recurring genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis)
The experience of using Valtrex⋇ in children with CC values less than 50 ml / min / 1.73 m2 is not available.

◈Additional information for indications: prevention of infections caused by CMV and diseases after transplantation of parenchymal organs
It is often necessary to determine QC, especially at a time when the kidney function is changing rapidly, for example, immediately after transplantation or engraftment, while the dose of Valtrex⋇ is adjusted in accordance with QC values.
Additional information for indications: treatment of herpes zoster (Herpes zoster) and ophthalmic herpes zoster
Valtrex⋇ should be used after hemodialysis in patients undergoing periodic hemodialysis.

☘ Patients with impaired hepatic function
Based on the study using a single dose of valaciclovir 1000 mg in adult patients with cirrhosis of mild or moderate severity (with preserved synthetic function of the liver), the dose adjustment of Valtrex⋇ is not required.
Pharmacokinetic data in adult patients with severe liver dysfunction (decompensated cirrhosis), with a violation of the synthetic function of the liver and the presence of portocaval anastomoses also do not indicate the need for correction of Valtrex dose, but the clinical experience with these pathologies is limited.
Information on doses more than 4000 mg / day for patients with infections caused by HSV and CMV is indicated in the section “Special instructions“.

☘ Side effect
Undesirable reactions are listed below in accordance with the classification of the main systems and organs and the frequency of occurrence, which is defined as follows: very often (≥1 / 10), often (≥1 / 100, <1/10) infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10,000, <1/1000), very rarely (<10,000).

☘ Clinical Trials Data
From the nervous system: often – a headache.
From the side of the digestive system: often – nausea.

☘ Post-marketing research data
On the part of the blood system and hemopoiesis: very rarely – leukopenia, thrombocytopenia. In general, leukopenia was observed in patients with reduced immunity.
From the immune system: very rarely – anaphylaxis.
From the nervous system and psyche: rarely – dizziness, confusion, hallucinations, depression of consciousness; very rarely – agitation, tremor, ataxia, dysarthria, psychotic symptoms, convulsions, encephalopathy, coma. The above symptoms are mostly reversible and are usually observed in patients with impaired renal function or against a background of other predisposing conditions. In adult patients with a transplanted organ who receive high doses (8 g / day) of Valtrex⋇ for the prevention of CMV infection, neurologic reactions develop more often than with lower doses.
◈From the respiratory system and mediastinal organs: infrequently – shortness of breath.
◈From the digestive system: rarely – discomfort in the abdomen, vomiting, diarrhea.
◈From the liver and bile ducts: very rarely – reversible violations of functional liver tests, which are sometimes regarded as manifestations of hepatitis.
From the skin and subcutaneous fat: rarely – rashes, including photosensitivity manifestations; rarely – itching; very rarely – hives, angioedema.
◈From the urinary system: infrequently – hematuria (often associated with other disorders of the kidneys); rarely – renal dysfunction; very rarely – acute renal failure, renal colic. Renal colic can be associated with impaired renal function. Cases of precipitation of Valaciclovirum crystals in the lumen of renal tubules have been reported. Adequate drinking regimen should be observed during treatment.
Other: In patients with severe impairment of immunity, especially in adults with advanced HIV infection receiving high doses of Valaciclovirum (8 g / day) for a long period of time, there have been cases of renal failure, microangiopathic hemolytic anemia, and thrombocytopenia (sometimes in combination). Similar complications were observed in patients with the same underlying and / or concomitant diseases, but not receiving Valaciclovirum.

☘ Contraindications for use
➢ hypersensitivity to Valaciclovirum, acyclovir and any other component included in the preparation;
➢ children’s age till 12 years;
➢ Children under 18 years of age in the treatment of herpes zoster and ophthalmic herpes zoster.
With caution: in patients with renal insufficiency; patients with clinically expressed forms of HIV infection; with the simultaneous administration of nephrotoxic drugs.

☘ Application in pregnancy and lactation
Fertility
In animal studies, Valaciclovirum did not affect fertility. However, the use of high doses of acyclovir for parenteral administration caused testicular effects in rats and dogs.
Studies of the effects of Valaciclovirum on fertility in humans have not been conducted. However, there were no changes in the number, motility and morphology of spermatozoa in 20 patients after 6 months of daily use of Valaciclovirum in doses ranging from 400 mg to 1000 mg.
Pregnancy
There are limited data on the use of Valtrex⋇ during pregnancy. The drug should be used during pregnancy only if the potential benefit to the mother exceeds the potential risk to the fetus.
Pregnant registries documented pregnancy outcomes in women taking Valaciclovirum or other drugs containing acyclovir (acyclovir is the active metabolite of Valtrex⋇), 111 and 1246 cases, respectively (of which 29 and 756 took drugs in the first trimester of pregnancy), represented pregnancy outcomes recorded prospectively. Analysis of the data presented in the register of pregnant women exposed to acyclovir did not reveal an increase in the number of birth defects in their children compared to the general population, none of the developmental defects showed any specificity or patterns indicating a common cause. Since a small number of women taking Valaciclovirum during pregnancy were included in the register of pregnant women, it is impossible to make reliable and definite conclusions about the safety of valaciclovir during pregnancy.

☘ Breastfeeding period
Valaciclovirum, the main metabolite of Valaciclovirum, penetrates into breast milk. After taking Valaciclovirum 500 mg inwards, Cmax in breast milk was 0.5-2.3 times (1.4 times on average) higher than the corresponding concentrations of acyclovir in the mother’s blood plasma. The ratio of AUC values ​​of acyclovir in breast milk to AUC in the mother’s serum ranged from 1.4 to 2.6 (mean 2.2).
The mean concentration of acyclovir in breast milk was 2.24 μg / ml (9.95 μmol / L). When taking a Valaciclovirum mother at a dose of 500 mg 2 times / day, children who are breastfed are exposed to the same effect of Valaciclovirum as when taking it inside at a dose of about 0.61 mg / kg / day. T1 / 2 Valaciclovirum from breast milk is the same as from plasma blood.
Valaciclovirum in unchanged form was not determined in the blood plasma of the mother, breast milk or urine of the child. Valaciclovirum should be administered with caution to women during breastfeeding. Nevertheless, Valaciclovirum for intravenous administration is used to treat HSV in infants at a dose of 30 mg / kg / day.

☘ Application for violations of kidney function
With renal failure, the dosing regimen is set depending on the creatinine clearance and indications.
Use in children

Contraindications:
➢ children’s age till 12 years;
➢ Children under 18 years of age in the treatment of herpes zoster and ophthalmic herpes zoster.

☘ Application in elderly patients
Older patients are not required to adjust the dose, except in cases of significant renal dysfunction. It is necessary to maintain an adequate water-electrolyte balance.

☘ Special instructions
Hydration
In patients at risk of dehydration, especially in elderly patients, an adequate water-electrolyte balance must be ensured.
Use in patients with impaired renal function and in elderly patients
Because Valaciclovirum is excreted by the kidneys, it is necessary to reduce the dose of Valtrex⋇ in patients with impaired renal function. In elderly patients, there may be a disturbance in the function of the nights, so a dose reduction for this group of patients should be considered. Both elderly patients and patients with impaired renal function are at increased risk of developing neurological complications, such patients need to ensure thorough medical supervision. As a rule, these reactions are mostly reversible in the case of drug discontinuation.
Treatment of labial herpes and prevention of CMV infections and diseases
The use of high doses of Valtrex⋇ in cases of impaired liver function and liver transplant. There is no data on the use of Valtrex⋇ in high doses (4000 mg / day or higher) in patients with liver disease, so patients should be given high doses of Valtrex⋇ with caution. Special studies to study the effects of Valtrex⋇ during liver transplant were not performed. However, it was found that the prophylactic administration of Valaciclovirum in high doses reduces the manifestations of CMV infection and disease.
Use in genital herpes
Patients should be advised to refrain from having sex if symptoms occur, even if treatment with Valtrex⋇ antiviral drug has already been started. Suppressive therapy with Valtrex⋇ reduces the risk of transmission of genital herpes, but does not completely exclude the risk of infection and does not lead to complete cure. Therapy with Valtrex⋇ is recommended in combination with reliable barrier contraception.
Impact on the ability to drive vehicles and manage machinery
It is necessary to take into account the clinical state of the patient and the profile of adverse reactions of Valaciclovirum in assessing the patient’s ability to drive or move vehicles.

☘ Overdose
Symptoms: Acute renal failure and neurological disorders, including confusion, hallucinations, agitation, oppression and coma, as well as nausea and vomiting, were observed in patients who received doses of valaciclovir exceeding those recommended. Similar conditions were more frequent in patients with impaired renal function and elderly patients who received repeated higher recommended doses of valaciclovir due to non-compliance with the dosing regimen.
Treatment: patients should be under close medical supervision. Hemodialysis greatly contributes to the excretion of Valaciclovirum from the blood and can be considered a method of choice for patients with an overdose of Valtrex⋇.

☘ Terms and conditions of storage
The drug should be stored at a temperature not higher than 30 ° C in a place inaccessible to children. Shelf life – 3 years.

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