Last Updated on February 19, 2017 by Dr.Derek Fhisher
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Valacyclovir general information
Valacyclovir generic is an effective kind of treatment because this drug intends to inhibit the reproduction of the virus in the body. Although prescription medications, like valacyclovir, might help to minimize outbreaks there are several other considerations. The very best drugs are prescription anti-virals. Like valacyclovir, acyclovir too will not pose any fantastic danger of drug interactions.
Shingles is a painful, blistering skin rash brought on by the varicella-zoster virus, that is the identical virus which causes chickenpox. Genital herpes blisters are usually painful and full of liquid. Painful sores too can develop bit in addition, there are individuals who hardly feel any symptoms of herpes. Presently, infected individuals can certainly deal with the herpes symptoms.
Within this article we’ll look at a few of the prescription drugs for herpes options your doctor may be available to you personally. Daily therapy could be costly too, and many prescription medications cause one side effect or another. Herpes simplex medication may also be found in nutritional supplements, including herbal form. Your physician can help in fixing the specific treatment that is appropriate for your needs.
Type 2, called HSV-2 is the principal cause of genital herpes. This results from the varicella zoster virus. It will be possible to become genital herpes from cold sores.
Even though there’s no cure, there are a couple of medications which help keep outbreaks in order. There is absolutely no medication accessible that can in fact kill the virus within the nerve cells. This kind of treatment can be extremely effective, but can likewise be expensive and might cause unwanted side results. In addition, There are home remedies that someone may utilize to assist in the treatment of cold sores. There are plenty of anti-viral medications accessible to treat this virus as a portion of shingles treatment. Scientists have demonstrated the effectiveness of several pure cures for the virus, and such options are getting to be a popular method to fight the virus and see to the symptoms.
These medicines are employed to lower the pain and discomfort that results from shingles. They’re able to arrange for the gentle stream of air as part of the shingle treatment to trim the pain due to shingles. They cannot get shingles, but instead chickenpox.
It’s very important to know that there’s no cure for herpes in the present time. Speak with your doctor to determine what herpes medicine is suitable for you. Since people don’t always ask what are the symptoms of genital herpes, consistently make sure you tell everyone you’re intimate with that you’re infected, be sure you always make use of a condom, and steer clear of sex when you’re in the middle of an outbreak. In case it’s herpes, it will certainly reach a particular stage where it’s going to either not resemble a pimple in any way or be the ugliest-ass pimple you’ve ever seen.
Once you feel an outbreak coming, begin the lysine, other supplements and also a topical treatment. In the event the blisters usually do not heal within the designated time, the physician will require the extension of antiviral medicines. It also lessens irritation and itching. Cool wet compresses may be used to lessen pain.
Happily there are a few very effective methods to swiftly banish cold sores. This is a huge all-natural healer and will surely help to eliminate your infection fast. If you concentrate on protecting yourself when you’re in physical contact with others, then you’ve got an extremely good chance of preventing the herpes virus.
Valacyclovir (Valaciclovir) – instructions for use, description of the pharmacological action, indications for use, dosage and mode of administration, contraindications, side effects
Code CAS: 124832 – 26 – 4
Description
Characteristics: is a Valacyclovir hydrochloride salt of L – valyl ester of acyclovir. Valacyclovir hydrochloride ; white or almost white powder; maximum solubility in water (at 25 ° C) ; 174 mg / ml; the molecular weight of 360,80.
Mode of action
Pharmacology: Mode of action – Antiviral (antiherpethetical). Valacyclovir ; prodrug in the body is rapidly and almost completely converted to acyclovir after phosphorylation which acquires specific activity. Acyclovir is a structural analogue of purine nucleosides (normal components of DNA) interacts with the viral DNA – polymerase and blocks the multiplication of viruses. Election antiherpethetical activity is due to affinity for thymidine kinase Herpes simplex, Varicella zoster virus and Epstein – Barr virus. Under the action of viral thymidine kinase transforms into atsiklovirmonofosfat, with the participation of human cells guanilatkinazy ; in atsiklovirdifosfat and then ; the active form atsiklovirtrifosfat. Triphosphate blocking viral DNA replication by competitive inhibition of viral DNA – polymerase and DNA chain elongation inhibition. Acyclovir in vitro active against viruses Herpes simplex type 1 and 2, Varicella zoster (less active than against Herpes simplex, due to the more efficient phosphorylation corresponding thymidine kinase), Epstein – Barr virus, CMV and human virus type 6 herpes
resistant strains Herpes simplex and Varicella zoster develops due to the phenotypic deficiency virus thymidine kinase, either – for hidden changes in the thymidine kinase or DNA – polymerase; resistance occurs in exceptional cases, in patients with normal immune status and significantly more on the background of severe immunodeficiency (HIV during infection, in patients receiving chemotherapy for malignant tumors, and others.).
After oral administration, valacyclovir is rapidly absorbed from the gastrointestinal tract, and as a result of metabolism in « first pass » through the intestine and / or liver as a result of enzymatic hydrolysis is rapidly and almost completely (99%) converted to acyclovir and L – valine.
The pharmacokinetics of valaciclovir and aciclovir after oral administration was investigated in 14 studies in healthy adult volunteers (n = 283).
When receiving valacyclovir hydrochloride at a dose of 1000 mg absolute bioavailability of acyclovir is (54,5 & plusmn; 9,1)% and is independent of food intake. Pharmacokinetic parameters after administration of different doses of valacyclovir hydrochloride is not proportional to dose. Thus, after a single dose of valacyclovir hydrochloride in doses of 100, 250, 500, 750 and 1000 mg of acyclovir C_mah reaches 0.83; 2.15; 3.28; 4.17 and 5.65 mcg / ml, AUC ; 2.28; 5.76; 11.59; 14.11 and 19.52 am · ug / ml, respectively. Following multiple administration of valacyclovir hydrochloride in doses of 250, 500 and 1000 mg four times a day for 11 days C_mah ; 2.11; 3.69 and 4.96 mcg / mL and AUC ; 5.66; 9.88 and 15.70 am · ug / ml, respectively. T_max is 1.6 – 2.1 parts The plasma concentrations of unchanged valaciclovir low C_mah below 0.5 mcg / ml at all doses tested, over 3 hours valacyclovir is not determined in the plasma;. binding of valacyclovir to plasma proteins ; 13.5 – 17.9%. Acyclovir is biotransformed by the action of alcohol – and aldehyde and, to a lesser extent, aldehyde oxidase into inactive metabolites. Metabolism valaciclovir / acyclovir is not associated with cytochrome P450.
T_1 / 2 valacyclovir ; less than 30 minutes, T_1 / 2 acyclovir after administration of valacyclovir hydrochloride is 2.5 – 3.3 hours (in healthy volunteers with normal renal function), in elderly patients (age 65 – 83 goda) ; 3.3 – 3.7 hours, is increased in patients with end stage renal failure. Valacyclovir is excreted in the urine (45.6%) and faeces (47.12%) for 96 hours Renal clearance .; about 255 ml / min. Of the total amount of valaciclovir outputted kidneys, 80 – 89% is eliminated in the form of acyclovir. Less than 1% of valaciclovir is excreted unchanged. After the re-use of valaciclovir in patients with normal renal function acyclovir does not accumulates.
The dependence of the pharmacokinetics parameters of some of the factors
Liver disease. In patients with secondary liver diseases (cirrhosis, proven by biopsy) or severe (biopsy proven cirrhosis with / without ascites) severity rate but not in the degree of conversion of valacyclovir acyclovir reduced; T_1 / 2 acyclovir does not change.
HIV – infected patients. In 9 patients with HIV (the number of CD4 cells < 150 cells / mm ^ 3) upon receipt of valacyclovir hydrochloride in a dose of 1000 mg four times per day did not differ from those observed in healthy volunteers for 30 days pharmacokinetic valaciclovir and acyclovir
Teratogenicity. Valaciclovir not teratogenic in rats or rabbits when administered at doses of 400 mg / kg during the period of organogenesis (the plasma concentrations exceeded those of the person 10 and 7 times, respectively).
Fertility. Valaciclovir not cause disturbances in fertility in male and female rats treated inside dose of 200 mg / kg / day (the concentration in the blood higher than that in humans is 6 times).
Indications for use
Application: Shingles; infections of the skin and mucous membranes, caused by herpes simplex virus (including genital herpes); relapse prevention of diseases caused by the herpes simplex virus.
Contraindications
Contraindications:: Hypersensitivity (including to acyclovir), bone marrow transplantation, kidney transplantation (. Cm « Precautions »).
Restrictions on the use of renal dysfunction, symptomatic forms of HIV – infection, children under 12 years of age (safety and efficacy have not been identified).
Pregnancy and lactation: Pregnancy. Perhaps if the expected effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety in pregnant women has not carried out).
Data on the outcome of pregnancy in women who received systemic effects of acyclovir in the I trimester of pregnancy (Acyclovir is an active metabolite of valaciclovir), showed no increase in the number of birth defects in children compared with the general population. As the observation was included a small number of women, credible and specific about valacyclovir safety conclusions can not be done during pregnancy.
Breastfeeding. Acyclovir, the major metabolite of valaciclovir, is excreted in breast milk. After assigning valaciclovir oral dose of 500 mg acyclovir C_max in breast milk of 0.5 – 2.3 times (an average 1.4 times) higher than the corresponding concentration in maternal blood. The ratio of AUC of acyclovir present in breast milk, to the AUC of acyclovir in maternal plasma was 1.4 – 2.6 (mean 2.2). The average value of the concentration of acyclovir in breast milk ; 2.24 g / ml. When assigning a nursing mother valaciclovir 500 mg 2 times a day child undergo a similar treatment of acyclovir as when taking it orally at a dose of about 0.61 mg / kg / day. Valacyclovir in unmodified form is not detected in the blood and breast milk of the mother or the child’s urine. Valaciclovir should be used with caution lactating women only if necessary.
Side Effects
Side effects: Table 1 shows the side effects frequently observed in the treatment with valacyclovir (1 g 3 times a day) in immunocompetent patients with herpes zoster during the randomized, double-blind clinical trials
Adverse events observed in clinical trials in patients with herpes zoster
When suppressive (prophylactic, preventive) treatment for the prevention of recurrence in HIV – infected patients who received valaciclovir 500 mg two times a day (n = 194) or placebo (n = 99), frequently observed side effects , headache (13 and 8%, respectively), fatigue (8/5%), rash (8/1%). In patients treated with valacyclovir, were also noted laboratory abnormalities (compared to placebo): increased levels of alkaline phosphatase (4/2%), ALT (14/10%), AST (16/11%), reduction in the number of neutrophils (18 / 10%) and platelet count (3/0%).
Interactions: No clinically significant interaction in patients with normal renal function has been established. Cimetidine and Probenecid (individually or together) after receiving a single dose of valaciclovir 1000 mg C_mah increased AUC and decrease renal clearance and acyclovir. The pharmacokinetics of valaciclovir is not altered by simultaneous administration with digoxin, aluminum / magnesium-containing antacids, thiazide diuretics.
nephrotoxic drugs increase the risk of renal failure and disorders of the central nervous system.
Symptoms: acyclovir sediment deposition in the renal tubules.
The treatment: hemodialysis (acute renal failure and anuria).
Dosage and method of administration
Dosage and administration: Inside (regardless of the meal). Dosage is determined individually, depending on the evidence. Therapy is recommended to begin as early as possible, the greatest efficiency is observed if treatment was started within 48 hours of the first appearance of signs or symptoms (rash, pain or burning sensation). When shingles ; 1000 mg 3 times daily for 7 days.
When simplex virus, including genital herpes is recurrent, ; 500 mg 2 times a day for 5 – 10 days.
In patients with renal insufficiency dose reduced: with herpes zoster ; 1000 mg every 12 hours at creatinine Cl 30 – 49 ml / min or 1 time per day, Cl Creatinine 10 – 29 mL / min and 500 mg 1 time per day, Cl creatinine less than 10 ml / min; in simple (including genital) herpes ; 500 mg every 12 hours at creatinine Cl 30 – 49 ml / min or 1 time per day, Cl creatinine less than 30 ml / min; in the case of hemodialysis drug prescribed after him.
Caution: With caution is prescribed for any conditions involving immune deficiency, especially in HIV – infected patients. During the clinical trial when receiving valacyclovir in high doses (8 g / day) for prolonged periods recorded thrombocytopenic purpura and / or hemolytic uremic syndrome, in rare instances fatal, in patients with symptomatic forms of HIV – infection after transplantation bone marrow or kidneys (see «. Contraindications » and « Restrictions on the use »). Do not set the application of the efficacy and safety of valacyclovir in immunocompromised patients (except for suppressive therapy of genital herpes in HIV – infected patients) for the suppressive therapy of recurrent genital herpes in patients with symptomatic forms of HIV – infection (CD4 cell count < 100 cells / mm ^ 3) for treating genital herpes in HIV – infected patients to treat herpes zoster generalized to reduce the possibility of infection with genital herpes healthy partner.
To use caution with impaired renal function (lengthens T_1 / 2 acyclovir), requires a correction mode, depending on the degree of their functions (see «. Dosing and Administration »). Patients with kidney disease, receiving high doses of valaciclovir, there have been cases of acute renal failure and disorders of the central nervous system.
Older patients during treatment is recommended to increase fluid intake.
During the treatment of genital herpes should avoid sexual intercourse (drug does not protect against transmission of infection).
Other medications and drugs used together and / or instead of the “Valacyclovir (Valaciclovir)” in the treatment and / or prevention of the following diseases.
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