[Drug Name]

Generic name: Valaciclovir hydrochloride tablets

Chinese Pinyin: Yansuan Faxiluowei Pian

English name: Valacyclovir Hydrochloride Tablets

[Ingredients] Main components The main component of this product is valacyclovir hydrochloride.

Chemical name: L-valine-2-[(6-oxo-2-amino-1,6-dihydro-9H-purin-9-yl)methoxy]ethyl ester hydrochloride.

Chemical Structure: 

Molecular formula: C13H20N6O4? HCL

Molecular weight: 360.80

[Properties] This product is a film-coated tablet, white or almost white after removing the coating.

[Indications] For the treatment of varicella-zoster and type I and type II herpes simplex virus infections, including initial and recurrent genital herpes virus infections.

[Specifications] 0.3g

[Usage and Dosage] Orally, 0.3g each time, 2 times a day, take it on an empty stomach before meals. Herpes zoster has been taken for 10 consecutive days. Herpes simplex has been taken for 7 consecutive days.

[Adverse reactions] Occasionally dizziness, headache, arthralgia, nausea, vomiting, diarrhea, stomach upset, loss of appetite, thirst, decreased white blood cells, proteinuria and slight increase in urea nitrogen, skin itching, etc., long-term administration occasionally See acne, insomnia, menstrual disorders.

[Taboo] People who are allergic to this product and acyclovir should not be used.

[Precautions]

1. People who are allergic to ganciclovir may also be allergic to this product.

2. Use with caution if you are dehydrated or have liver or kidney dysfunction. Patients with renal insufficiency need to adjust the dose according to the creatinine clearance rate when receiving the treatment of this product.

3. Patients with severe immune deficiency may cause resistance to the product after long-term or repeated application of this product to herpes simplex virus and herpes zoster virus. If patients with herpes simplex have no improvement in skin lesions after applying this product, they should test the sensitivity of the herpes simplex virus to this product.

4. Follow-up examination: Since most patients with genital herpes are susceptible to cervical cancer, they should be checked at least once a year for early detection.

5. Once the symptoms and signs of herpes appear, the drug should be administered as soon as possible.

6. The patient should be given adequate water during the medication to prevent acyclovir from precipitating in the renal tubules.

7. A hemodialysis can reduce the blood concentration of acyclovir by 60%, so one dose should be given after dialysis.

8. Intermittent short-term therapy is effective for recurrent genital herpes infections. Since animal experiments have found that this product has an impact on fertility and mutagenesis, the oral dose and treatment duration should not exceed the recommended standards. Long-term treatment of recurrent genital herpes should not exceed 6 months.

9. This product has no obvious effect on the latent infection of herpes simplex virus and cannot eradicate the virus.

[Medication for pregnant women and lactating women] Acyclovir can pass through the placenta, and pregnant women need to weigh the pros and cons of medication. The concentration of acyclovir in breast milk is 0.6 to 4.1 times the blood concentration, and women who are breastfeeding should use it with caution.

[Children's medication] The safety and effectiveness of children's medication has not been determined.

[Medication for the elderly] Due to the decline of physiological renal function, the dosage of this product and the medication interval need to be adjusted.

[medicine interactions]

1. Combined use with Zidovudine can cause nephrotoxicity, manifesting as deep lethargy and fatigue.

2. Competitively with probenecid to inhibit the secretion of organic acids, combined with probenecid can slow down the excretion of acyclovir, prolong the half-life, and accumulate drugs in the body.

[Drug overdose] Symptoms and signs: The data on overdose of this product is limited. However, some patients used acyclovir as a single dose at a dose of up to 20g, and after partial absorption through the gastrointestinal tract, there were no common toxic reactions. After accidental repeated oral overdose of acyclovir for a few days, gastrointestinal reactions (such as nausea, vomiting) and neurological reactions (headache and confusion) related to it were observed. Disposal: The patient's symptoms of poisoning should be closely observed. Hemodialysis can significantly increase the clearance rate of acyclovir from the blood. Therefore, it can be used as an overdose treatment option.

[Pharmacology and Toxicology] Pharmacological effects: This product is a prodrug of acyclovir, which is quickly absorbed after oral administration and quickly converted into acyclovir in the body. Its antiviral effect is exerted by acyclovir, acyclovir After entering the herpes infected cells, Lovir competes with deoxynucleosides for viral thymidine kinase or cell kinase, and the drug is phosphorylated into activated acyclovir triphosphate, which acts as a substrate for viral replication to compete with deoxyguanine triphosphate for viruses DNA polymerase inhibits the synthesis of viral DNA and shows antiviral effects. The antiviral activity of this product is better than that of acyclovir, and the therapeutic index of herpes simplex virus type I and type II is 42.91% and 30.13% higher than that of acyclovir, respectively. It also has a high curative effect on varicella-zoster virus. Toxicological research: General toxicity: Very low toxicity to mammalian host cells. The LD50 of rats and mice by intragastric administration was 4.4g/kg and 1.51g/kg, respectively. Since this product is quickly converted into acyclovir in the body, its metabolites do not accumulate in the body. In different stages of long-term toxicity tests, this product has the same safety as acyclovir. Genotoxicity: In the mouse micronucleus test, 250mg/Kg is not mutagenic, while 500mg/Kg (acyclovir concentration is 26 to 51 times the human plasma level) is mutagenic.

[Pharmacokinetics] Literature data: After oral administration, this product is quickly absorbed and transformed into acyclovir, and the peak time of acyclovir in the blood is 0.88 to 1.75 hours. Oral bioavailability is 67±13%, which is 3 to 5 times that of acyclovir. The drug is widely distributed after entering the body, and can be distributed in a variety of tissues, among which the concentration in stomach, small intestine, kidney, liver, lymph node and skin tissue is the highest, and the concentration in brain tissue is the lowest. This product is completely converted into acyclovir in the body, and the metabolites are mainly eliminated from the urine, of which acyclovir accounts for 46%～59%, 8-hydroxy-9-guanine accounts for 25%～30%, and 9-hydroxyl Methoxyguanine accounts for 11% to 12%. The original form of acyclovir is single-phase elimination, and the blood elimination half-life (t1/2β) is 2.86±0.39 hours.

[Storage] Sealed and stored in a dry place.

[Packing] Aluminum-plastic blister packaging, 6 pieces/box or 12 pieces/box. 120 boxes/carton.

[Valid period] 24 months

[Executive Standard] Chinese Pharmacopoeia 2010 Edition Two

[Approval Number] National Medicine Zhunzi H20093559

[manufacturer]    

Company Name: Anshi Pharmaceutical (Zhongshan) Co., Ltd.

Production address: National Health Technology Industry Base, Zhongshan City, Guangdong Province

Postal Code: 528437

phones number: 0760-23898866

Fax number: 0760-23898833

Website: http://www.qidongs.com