This product mainly consists of A Silowe, the chemical name: 9- (2- hydroxyethyl methyl) guanine.
The structural formula:
Molecular formula: C Eight
Molecular weight: 225.21
This product is white or white sweet.
1 herpes simplex virus infection for genital herpes virus infection of primary and recurrent cases of recurrent cases, this product is used for the prevention of oral.
2: the treatment of herpes zoster treated in immunocompetent individuals with herpes zoster and immunocompromised patients with mild.
Treatment of 3 immunocompromised patients with varicella.
Bonner usage and dosage
Oral, direct water, also can chew and swallow the dose is as follows:
(a) commonly used dose
1, acute herpes zoster: Adults take 200 ~ 800mg (a 0.5 to 2), every 4 hours for 1 times, 5 times a day, for 7 ~ 10 days.
2, genital herpes:
Primary genital herpes: each adult 200mg (a 0.5), every 4 hours for 1 times, 5 times a day for 10 days.
Chronic recurrent genital herpes: Adults take 200 ~ 400mg (a 0.5 to 1), 2 times a day, for 4 ~ 6 months or 12 months of treatment, re evaluation. According to the evaluation results, select each 200mg (0.5 at a time), 3 times a day, each time 200mg (or 0.5 at a time) treatment, 5 times a day. Genital herpes untreated seizure frequency and severity may change over time. After 1 years of treatment, to genital herpes infection and severe seizure frequency re evaluation, to determine whether to continue to use this product for.
Intermittent treatment: in the early stage of recurrent symptoms should be given and treatment, each adult 200mg (a 0.5), every 4 hours for 1 times, 5 times a day, taking more than 5 days.
3, chicken pox:
2 children over the age of each oral dose was 20mg/kg, 4 times a day, a total of 1 80mg/kg.
Adults and children weighing 40 kg or more: a 800mg (a 2), 4 times a day, and even served 5 days.
(two) dose adjustment
1, acute and chronic renal failure patients: the usage and dosage of these patients see table 1.
Table 1 dose adjustment in patients with renal failure.
The commonly used dose adjustment
Creatinine clearance rate dose (mg)
200mg every time, every 4 hours for 1 times, 10 200mg each time, every 4 hours for 1 times, 5 times a day
0-10 200mg every 12 hours, 1 times, 2 times a day
400mg every time, every 12 hours for 1 times, 10 400mg each time, 12 hours, 1 times, 2 times a day
0-10 200mg every 12 hours, 1 times, 2 times a day
800mg every time, every 4 hours for 1 times, 25 800mg each time, every 4 hours for 1 times, 5 times a day
10-25 800mg every time, every 8 hours for 1 times, 3 times a day
0-10 800mg every 12 hours, 1 times, 2 times a day
2, hemodialysis: the need for dialysis patients, hemodialysis during the acyclovir plasma half-life is about 5 hours, 6 hours of hemodialysis. Blood drug concentration decreased by 60%, so the patient dose should be adjusted in time after additional dialysis.
3, peritoneal dialysis: no dose adjustment during the period of delivery.
Bonner Adverse reaction
1, digestive system reactions include nausea, vomiting, diarrhea, etc..
2, allergic reactions: fever, headache, including Zhou Hongzhong etc..
3, neural responses that include headache, euphoria, ataxia, coma, confusion, loss of consciousness, delirium, hallucinations, dizziness, brain pain, paresis, drowsiness etc..
4, the blood and lymphatic system: including anemia, leukopenia and thrombocytopenia.
5, liver and pancreas: including hepatitis, hyperbilirubinemia, jaundice etc..
6, musculoskeletal system: muscle pain reaction.
7, hair loss, skin rash, photosensitivity, epidermal necrosis, rash, pruritus.
8, local reactions: eye discomfort.
9, others: high disease, renal failure, blood and urine protein creatinine, hematuria.
To disable acyclovir allergy.
Bonner Matters needing attention
Renal damage treated with acyclovir, which may cause death.
Immune function damage in patients treated with acyclovir can occur, thrombosis, thrombocytopenic purpura and hemolytic uremic syndrome, (TT1/HUS), and can lead to death.
2, the renal function damage in patients with the dosage should be adjusted.
3, to accept the potential renal toxic substances in patients with acyclovir should pay special attention to, because this can increase the risk of renal dysfunction, and increased central nervous system symptoms are reversible.
4, note: if patients feel serious adverse reactions or disturbing, are pregnant or become pregnant for lactating women, or have other problems of patients should consult with a doctor, under the guidance of a doctor's medication.
Study on the data of 5, there is no acute herpes zoster 72 hours before the start of treatment, so the herpes zoster patients should be treated early for diagnosis.
6, genital herpes infection: the product of genital herpes can cure. No data to prove whether this product can prevent the disease to others. Because genital herpes is a sexually transmitted disease, patients should avoid contact with the affected area, and to avoid sexual intercourse, in order to avoid the infection of spouse. Genital herpes can be transmitted in the absence of symptoms, exhausted by asymptomatic virus. If it is found that the recurrence of genital herpes, the patient should be treated immediately after the discovery of the first symptoms or signs.
7, for the health of children: varicella, varicella is a self limiting disease and mild to moderate, adolescents and adults are more serious. In the acute attack of chickenpox treatment should be carried out within 24 hours, there is no effective treatment data of late onset began treatment.
Bonner Pregnant and lactating women use
Pregnant women with caution. A pregnant woman using the A Silowe effect of epidemiological record established from 1984 to April 1994, the results of 756 experiments for 3 months in 749 pregnant women were taking system A Silowe, its teratogenic effects on infants is similar to the general population. But these data are not sufficient to prove the acyclovir for pregnant women and the fetus is completely safe. Only when the treatment effect of A Silowe on the fetus is far greater than the risk when taking A Silowe.
A Silowe concentration in milk for the blood concentration of 0.6 ~ 4.1 times. When lactating women dose per day 0.3mg/kg may influence the development of the baby. Only in the necessary circumstances, lactating women can use A Silowe.
Bonner Medication for children
Children under 2 years old with caution.
Bonner Elderly patients
At present there is no research data show the people over the age of 65 young people with drug medication are significantly different. Generally speaking. The elderly medication should be effective medication dose range, reduce the occurrence of renal dysfunction or other adverse reactions caused by the increased number of pills.
Bonner Drug interactions
Probenecid and intravenous acyclovir when used together, the average half-life of acyclovir and AUC increased urinary excretion decreased, reduced renal clearance.
Bonner Drug overdose
The dose is greater than 20 grams, can be exciting, coma, tremor, weakness. Given the high dose of intravenous injection of acyclovir, due to its concentration in renal tubules is too large and the accumulation of crystallization (2.5mg/ml) as a result of creatinine and blood urea nitrogen increased while the secondary causes of renal failure, once the occurrence of renal failure and anuria, patients need to do hemodialysis until functional recovery.
Bonner pharmacology and toxicology
This product is a synthetic nucleoside antiviral, in vivo and in vitro of herpes simplex virus type I (HSV-1), II (HSV-2) and varicella zoster virus (VZV) were inhibited. The cell culture results showed that the inhibition of HSV-1 virus was the strongest, followed by HSV-2 and VZV virus.
Because of this product by thymidine kinase HSV and VZV encoding (TK) affinity, inhibition due to its high selectivity. The virus will translate into A Silowe A Silowe enzyme single phosphate, namely nucleoside analogues. Single phosphate was further guanylate kinase in cells transformed into two phosphate, again through the transformation of a variety of enzymes in the cell for three phosphate. In vitro, acyclovir herpes virus replication of DNA three phosphate suspension is to complete the following three ways: 1) competitive inhibition of viral DNA polymerase; 2) to enter and terminate the extension of the virus DNA chain; 3) inactivated virus DNA polymerase. Compared with VZV, the product of the antiviral activity of HSV is stronger, this is because the virus thymidine kinase (TK) phosphorylation stronger.
Genetic toxicity: 16 genetic toxicity tests, no mutagenic effect in 4 microbiological research results; 2 in vitro genetic test in mouse lymphoma cells and human lymphocytes showed that this product has mutagenic effect. In the 5 cell genetic testing (3 ovarian cells, China hamster 2 mouse lymphoma cells), no mutagenic effect. Is homologous immune dysfunction in weaning, rats after administration of the 2 cell transformation in vitro experiments, of which 1 were positive, the cells changed from the morphology of tumor cells, while in another experiment, there is no similar results (may be due to sensitive doses when administered, no significant changes in chromosome damage); mice dominant lethal test (in person with dose of 36 ~ 73 times the dosage) were negative.
The reproductive toxicity of mice: (450mg/kg/ days, PO) and rabbits (250mg/kg/ days, SC) test results showed that the product of its fertility and reproductive function has no effect. Mice and rats plasma drug concentrations were human blood drug level of 9 ~ 18 and 8 ~ 15 times. Mice and rabbits were given higher dose (50mg/kg/ day, SC, with the level of 11 ~ 22 and 16 ~ 31 times respectively), can reduce the implantation, but does not affect the same litter size. The rats in the prenatal and postnatal taking this product (50mg/kg/ days, SC) significantly decreased the average total group between corpus luteum, implantation location and survival fetal had statistical significance.
The dog for 1 months to give the goods (50mg/kg/ day, IV, for people with the dose of 21 ~ 41 times) (the blood concentration of people 21 to 41 times) or 1 consecutive years (60mg/kg/ days, PO, for people with the dose of 6 ~ 12 times), the results were not found in testicular abnormalities. At the higher doses to rats and dogs, visible testicular atrophy and reduced sperm.
(450mg/kg/, PO) mice and rabbits (50mg/kg/ days, SC or IV) and rats (50mg/kg/ days, SC) given exposure dose respectively with the dose of 9 ~ 18, 16 ~ 106, 11 ~ 22 times, the results showed that there were no teratogenic effects.
In pregnant women is not fully and strictly controlled study, but that a epidemiological survey tracked 756 pregnant women with systemic administration, the incidence is similar to the general population of birth defects in babies, but these data are not enough to prove that it is safe for pregnant women and fetuses. Only when the product of the fetal treatment far outweigh the risks, you may consider taking.
Lactating women use, this product in milk concentration of the blood concentration of 0.6 ~ 4.1 times. When lactating women dose was 0.3mg/kg/ days, the concentration may affect the baby, breast-feeding women should be used with caution, and should be used only when necessary.
Carcinogenicity: in rats and mice by gavage throughout the life period, give this product 450mg/kg/ days, the results show that the significant difference between the number of animal drug group and control group of cancer was not statistically significant, nor reduced tumor latency. The maximum plasma concentration in rats and mice respectively with dose level of 3 ~ 6 and 1 ~ 2 times.
1 of China's current lack of research with the data of pharmacokinetics of Aciclovir Chewable Tablets. Bioequivalence studies in 8 healthy male volunteers showed that a single dose of Aciclovir Chewable Tablets 800mg, the average peak plasma concentration was 853.67 + 214.52ng/ml, the average peak time was 1.37 + 0.66h.
2 according to the Physician's Desk Reference (54 Edition), acyclovir pharmacokinetic study results are as follows:
Study the existing evaluation of healthy volunteers and patients with herpes zoster or simple oral acyclovir drug, its pharmacokinetics are shown in Table 2
The research data of 23 healthy volunteers, single dose crossover design of oral acyclovir showed that increased serum concentrations of acyclovir increased with the dosage of the inconsistent (see Table 3), the lower bioavailability depends on the dose and dosage form.
Study on 6 subjects. The results showed that no effect on the absorption of acyclovir in food. Therefore, acyclovir may be taken with food. This product is only the urinary metabolites of 9-[(Suo Jiayang) methyl] guanine.
The special crowd:
Renal injury in adults: the half-life of acyclovir and total elimination rate of time depends on the renal function. Renal insufficiency patients should adjust the dosage.
Children: General A Silowe, in the children's pharmacokinetics similar to adults. 7 months to 7 year old children's oral 300mg/m[sup]2[/sup] and 600mg/m[sup]2[/sup] A Silowe, the average half-life of 2.6 hours, in the range of (1.59 to 3.74 hours).
Sealed in a dry place.
Plastic packaging, 0.4g/ tablets, 10 tablets / plate, 1 plate / box, 2 / box board.
Bonner Term of validity
Bonner The implementation of standards
"Chinese Pharmacopoeia" in 2010 two edition
Bonner Approval number
Bonner manufacturing enterprise
Shandong Zibo Xinda Pharmaceutical Co. Ltd.
Bonner Revision date
05 2009 06 July