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Instructions for Valcyte (Valganciclovir Hydrochloride Tablets)
Common name: Valcyte (Valganciclovir Hydrochloride Tablets)
Trade name: valcyte
All names: Valcyte, Valcyte, Valcyte, Valganciclovir, valgansiklovir
Indications:
Prevention of cytomegalovirus (CMV) in high-risk adult kidney, heart, and pancreas transplant patients (donor CMV seropositive/recipient CMV seronegative).
Prevention of cytomegalovirus (CMV) in high-risk children with kidney transplantation (4 months to 16 years old) and heart transplantation (1 month to 16 years old).
Cytomegalovirus Retinitis, Treatment (AIDS-Related): Treatment of Cytomegalovirus (CMV) Retinitis in Patients with Acquired Immunodeficiency Syndrome (AIDS).
Recommended Dosage in Pediatric Patients
Prophylaxis of Cytomegalovirus (CMV) in Pediatric Kidney Transplant Patients: For pediatric kidney transplant patients 4 months to 16 years of age, the recommended once-daily mg dose (7 × BSA (bovine serum albumin) × CrCl (creatinine clearance)) should be initiated within 10 days after transplantation and continued until 200 days after transplantation.
Prevention of Cytomegalovirus (CMV) in Pediatric Heart Transplant Patients: For pediatric heart transplant patients aged 1 month to 16 years, it is recommended that a once daily mg dose (7 × BSA (bovine serum albumin) × CrCl (creatinine clearance)) be initiated within 10 days after transplantation until 100 days after transplantation.
Adverse reactions:
>10%:
Cardiovascular: hypertension (12% to 18%)
Central nervous system: headache (6%-22% ), insomnia (6%-20%)
Gastrointestinal tract: diarrhea (16%-41%), nausea (8%-30%), vomiting (3%-21%), abdominal pain (15%)
Hematology and tumors: anemia Hematology (<31%), thrombocytopenia (<22%), neutropenia (3%-19%)
Immune: Graft rejection (24%)
Neuromuscular and skeletal: Tremor (12% to 28%)
Ophthalmology: retinal detachment (15%)
Kidney: elevated serum creatinine (Scr>1.5-2.5mg/dL: 12%-50%; Scr>2.5: 3%-1 7%)
Others: Fever (9% to 31%)
1%-10%
Cardiovascular: Hypotension (>5%), peripheral edema (>5%), arrhythmia (<5%)
Central Nervous system: peripheral neuropathy (9%), paresthesia (≤8%), anxiety (≥5%), chills (≥5%), depression (≥5%), dizziness (≥5%), fatigue (≥5%), asthenia (≥5%) , pain (≥5%), agitation (<5%), confusion (<5%), hallucinations (<5%), psychosis (<5%), epileptic seizures (<5%)
Dermatology: dermatitis (≥5%), wound secretions Increase (≥5%), night sweats (≥>5%), pruritus (≥5%), cellulitis (<5%)
Endocrine metabolism: high potassium (≥5%), low phosphorus (≥5%), weight loss (≥5%)
Gastrointestinal tract: abdominal distension (≥5%), constipation (≥5%), loss of appetite (≥5%), indigestion (≥5%), oral mucosal ulcer (≥5%), loss of appetite (<5%), pancreatitis (<5%)
Genitourinary system: hematuria (≥5%), urinary tract infection (≥5%)
Hematology and neoplasms: myelosuppression (<5%; including aplastic anemia), febrile neutropenia (< 5%), bleeding (<5%; with thrombocytopenia), pancytopenia (<5%)
Liver: hepatic insufficiency (>5%), elevated serum ALT (<5%), elevated serum AST (<5%)
Hypersensitivity: Hypersensitivity reaction (<5%)
Immunity: organ transplant rejection (6%-9%)
Infection: candidiasis (≥5%; including oral candidiasis), influenza (≥5%), wound infection (≥5%), sepsis (<5%)
Neuromuscular and skeletal: arthralgia (≥5%), back pain (≥5%), muscle spasm (≥>5%), myalgia (≥5%) ), weakness (≥5%), limb pain (<5%)
Ophthalmology: eye pain (>5%), macular edema (<5%)
Ear: deafness (<5%)
Kidney: decreased creatinine clearance ( >5%), renal impairment (>5%), renal failure (<5%)
Respiratory system: cough (≥5%), dyspnea (≥5%), pharyngitis (≥5%; including nasopharyngitis), upper respiratory tract infection (≥5%)
Others: postoperative complications (≥5%), postoperative pain (<5%), wound dehiscence (<5%)
Frequency not defined: Genitourinary system: reduced fertility
< 1%
Agranulocytosis, Anaphylaxis, Granulocytopenia
Contraindications:
Cannot be used in patients with allergic reactions to valganciclovir, ganciclovir or any other component of the drug Valganciclovir Hydrochloride Tablets
Precautions:
Acute renal failure: Acute renal failure may occur, ensure adequate hydration, use with caution in patients receiving concomitant nephrotoxic drugs.
Hematological disorders: Severe leukopenia, neutropenia, anemia, thrombocytopenia, pancytopenia and bone marrow failure, including aplastic anemia. May occur at any time during treatment and worsen with continued use; cell counts usually begin to recover within 3-7 days of stopping treatment. Do not use if the absolute neutrophil count is <500 cells/MM3, platelet count <25,000/m3, or hemoglobin <8 g/dl; use with caution in patients with myelosuppression, cytopenia, or patients receiving myelosuppressive drugs/radiation. Monitor CBC and platelet counts at baseline and frequently during treatment, especially in infants and patients with renal impairment, patients with prior drug-induced leukopenia, and patients with neutrophil counts <1000 cells/mm3 at the start of treatment.
Carcinogenicity/Teratogenicity: May temporarily or permanently inhibit sperm production and suppress fertility; may cause birth defects and cancer in humans. Due to its teratogenicity, women should take a pregnancy test before initiating pregnancy and use effective contraception during treatment and for 30 days after treatment; men should use barrier contraception during treatment and for 90 days after treatment.
Renal Impairment: Use with caution in patients with impaired renal function; dose adjustment required.
Geriatric: Acute renal failure may occur in elderly patients with or without renal impairment, use with caution and adjust dose based on renal function.
Liver Transplant Recipients: Not suitable for liver transplant patients (a higher incidence of tissue-infiltrating cytomegalovirus (CMV) was observed in the trial compared with oral ganciclovir).
Pediatrics: The preferred dosage form for pediatric patients is the oral solution; however, valganciclovir hydrochloride tablets may be used as long as the calculated dose is within 10% of the available tablet strength (450 mg). The use of valganciclovir hydrochloride tablets in the treatment of congenital cytomegalovirus disease has not been evaluated.
Benzyl alcohol and sodium benzoate; benzoic acid (benzoic acid) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (99 mg/kg/day) are associated with potentially fatal neonatal toxicity (wheezing syndrome); "wheezing syndrome" includes metabolic acidosis, respiratory distress coercion, wheezing, central nervous system dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular failure; some data suggest that benzoates replace bilirubin at protein binding sites; avoid or use with caution in neonates dosage forms containing benzyl alcohol derivatives.
Storage:
Oral Solution
Store dry powder at a temperature of 20°C to 25°C (68°F to 77°F); deviations of 15°C to 30°C (59°F to 86°F) are allowed.
Store reconstituted oral solution at 2°C to 8°C (36°F to 46°F); do not freeze.
Throw away any unused medication after 49 days.
Tablets
Store at 20°C to 25°C (68°F to 77°F); deviations allowed from 15°C to 30°C (59°F to 86°F).
Mechanism of action:
Valganciclovir hydrochloride tablets are the L-valyl ester (prodrug) of ganciclovir. After oral administration, it is rapidly converted into ganciclovir by esterases in the small intestine and liver. Ganciclovir is a synthetic analog of 2’-deoxyguanosine that inhibits herpes virus replication in vitro and in vivo. Susceptible human viruses include human cytomegalovirus (HCMV), herpes simplex virus-1 and herpes simplex virus-2 (HSV-1, HSV-2), human herpesvirus-6, 7, 8 (HHV-6, 7, 8), Epstein-Barr virus, varicella-zoster virus (VZV), and hepatitis B virus. In cells infected with cytomegalovirus (CMV), ganciclovir is first phosphorylated by the viral protein kinase UL97 to ganciclovir monophosphate. It is further phosphorylated by intracellular protein kinases into ganciclovir triphosphate, which is then slowly metabolized within the cell. After removal of extracellular ganciclovir, the half-life of ganciclovir in HSV- or HCMV-infected cells is 18 hours and 6 to 24 hours, respectively. Since phosphorylation is largely dependent on viral protein kinases, ganciclovir phosphorylation occurs preferentially in virus-infected cells.
Ganciclovir inhibits viral activity mainly by inhibiting the synthesis of viral DNA:
(a) competitively inhibits viral DNA polymerase, preventing deoxyguanosine triphosphate from binding to DNA,
(b) ganciclovir triphosphate binds to viral DNA to terminate or limit the elongation of the DNA chain. The IC50 (concentration of the inhibitor at which the "response" is inhibited by half) of the antiviral effect of ganciclovir on cytomegalovirus (CMV) in vitro ranges from 0.14μM (0.04ug/ml) to 14μM (3.5ug/ml).