Ganciclovir Powder CAS 82410-32-0

Ganciclovir powder is an odorless, hygroscopic organic compound crystal with the chemical formula C9H13N5O4. It is homologous with acyclovir (ACV). Its antiviral effect is similar to that of acyclovir, but its effect is stronger, especially for cytomegalovirus in AIDS patients. Pure ganciclovir crystal powder is slightly soluble in water or glacial acetic acid, almost insoluble in methanol, insoluble in dichloromethane, and slightly soluble in hydrochloric acid solution or sodium hydroxide solution.

What is the difference between ganciclovir and acyclovir?

Acyclovir and ganciclovir refer to acyclovir preparation and ganciclovir preparation in clinic. The differences between them are different in chemical structure, mechanism of action, indications, adverse reactions, contraindications and so on. The specific use should strictly follow the doctor's instructions and product instructions, and you should go to the hospital in time if you feel unwell.

1. Different chemical structures:

Acyclovir is a second-generation broad-spectrum antiviral drug, and it is the first ring-opening nucleoside drug with specific anti-herpesvirus, which can selectively block virus replication in cells infected with cytomegalovirus (CMV). However, the disadvantage of acyclovir is that it may lead to compliance problems for HIV patients who have been given combination therapy; The biggest disadvantage in clinical use is the poor anti-cytomegalovirus effect. In order to alleviate the symptoms, it is very likely that the number and quantity of daily use will exceed the conventional dosage and cause glomerular obstruction.
pure Ganciclovir powder is a derivative of acyclovir, both of which belong to nucleoside analogues and have antiviral effects. Their chemical structures are also very similar. But it is because of the subtle differences in structure that the curative effect of the product is greatly improved.

2. Different mechanisms of action:
After ganciclovir enters cells, it is usually induced by viral kinase to generate triphosphate compounds, which competitively inhibit viral DNA polymerase and terminate the growth of viral DNA chain.
Acyclovir has strong selectivity and low cytotoxicity, which mainly inhibits viral DNA polymerase and prevents and prevents the synthesis of viral DNA in vivo.

3. Different indications：

Ganciclovir preparations are used for the treatment and prevention of cytomegalovirus infection. This virus is common in patients with impaired immune system, such as organ transplant recipients and AIDS patients, who usually suffer from cytomegalovirus retinitis, malignant tumors and other viral infections caused by severe immune dysfunction, and can also be used to treat cytomegalovirus infection in the liver and central nervous system, pneumonia, gastroenteritis and other conditions.
Acyclovir preparations are used to treat herpes simplex virus, chickenpox, and herpes zoster virus infections, as well as to prevent serious complications of cytomegalovirus infection and human herpesvirus type 4 (EB virus) infection after transplantation, such as chickenpox caused by immunodeficiency.

4.Adverse reactions are different:
Although both drugs may cause adverse reactions related to the digestive system, the specific symptoms may be different. Ganciclovir may cause problems such as abnormal liver function and ulcerative gastritis, while acyclovir is common in nausea, vomiting and diarrhea.
In addition, ganciclovir preparation may also lead to neutropenia, neutropenia, anemia, thrombocytopenia and so on; Acyclovir may cause inflammation at the site of use. Like itchy skin and urticaria or phlebitis. The uncommon adverse reactions of the two drugs include restlessness, headache, dizziness and joint pain.

5.Different taboos:
Acyclovir preparation is mainly prohibited for allergic people and pregnant women.Ganciclovir preparation is not only restricted to allergic patients and pregnant women, but also strictly restricted to patients with severe neutropenia (less than 0.5× 10 9/L) and severe thrombocytopenia (less than 25× 10 9/L).

What problems will occur when this product is used with other products?

Probenecid and other products that can inhibit renal tubular secretion and reabsorption can reduce the clearance rate of Ganciclovir by the kidneys and prolong its half-life. It can produce a synergistic effect when used in conjunction with products that inhibit rapid cell division and replication. It is used in combination with 4,4'-Diaminodiphenylsulfone, PentaMidine-d4 2HCl, Fluorocytosine, vincristine, vinblastine, Adriamycin, Amphotericin B,Trimethoxine pyrimidine, and some nucleoside products, but it increases the probability and intensity of side effects. The use of Ganciclovir and Zidovudine by AIDS patients will basically lead to severe leukopenia. It can induce epilepsy when used in combination with imipenem/cilastatin sodium salt. 

In addition to Ganciclovir and acyclovir, our company can also provide most of the raw materials for the products mentioned in this article. For example, Probenecid, 4,4'-Diaminodiphenylsulfone, vincristine, cilastatin sodium salt, and so on. If you are interested, please contact us via email: sales6@faithfulbio.com

What is the pharmacological mechanism of ganciclovir tablets?

Ganciclovir tablets are mainly used to treat diseases caused by cytomegalovirus infection in immunocompromised patients. Its pharmacological mechanism is mainly to inhibit viral DNA polymerase, thus playing an antiviral role.
Propoxyguanosine is a chemically synthesized guanine analogue, which can prevent the replication of herpes virus. Viruses sensitive to it include CMV, HSV-1, HSV-2, EBV and VZV.
Intracellular propoxyguanosine is phosphorylated into monovalent phosphate of propoxyguanosine by deoxyguanosine kinase, and can also be further phosphorylated into trivalent phosphate by some cell kinases. In cells infected by cytomegalovirus, propoxyguanosine can be preferentially phosphorylated. The metabolism of Trivalent phosphate of propoxyguanosine is very slow, and it can be preserved for 60 ~ 70% after being separated from extracellular fluid for 18 hours.
Ganciclovir is a guanosine analogue, which is competitively incorporated into the replicating viral DNA chain with thymidine. (1) Competitive inhibition of binding of trivalent phosphate of deoxyguanosine to DNA polymerase; The formation of phosphodiester bond is blocked and its continuous synthesis is terminated, thus achieving the purpose of inhibiting viral DNA polymerase. (2) The combination of trivalent phosphate of propoxyguanosine with viral DNA finally leads to the stop of DNA extension.
In clinical research, we found that it can inhibit the activity of herpes virus DNA polymerase and prevent the extension and polymerization of virus DNA chain, thus inhibiting the growth of virus, but it may produce acute drug resistance.

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