Description
Release form
Film-coated tablets.
packaging 21 pcs
Pharmacological action
Minaker – antiviral. The prodrug is a 6-deoxydiacetyl analogue of the active antiviral substance penciclovir. Transforming in the body into the active compound – penciclovir, acts on Herpes simplex viruses (types 1 and 2), Varicella zoster, Epstein-Barr virus.
Penetrating into virus-infected cells, penciclovir is phosphorylated by viral thymidine kinase to penciclovir monophosphate, which is then converted by action of cell kinases to penciclovir triphosphate. Penciclovir triphosphate is retained in an infected cell for more than 12 hours and inhibits viral DNA replication.
Has no effect on uninfected cells. It is active against some acyclovir-resistant strains of the Herpes simplex virus with altered DNA polymerase.
Pharmacokinetics
After oral administration, it is rapidly and almost completely absorbed and rapidly turns into active penciclovir. Bioavailability is 77%. TCmax – 45 min, Cmax after taking a single dose of 500 mg – 3.3-4.2 μg / ml. Distribution volume – 1 l / kg. Communication with plasma proteins – 20%.
T1 / 2 – 2.1-3 hours. T1 / 2 of penciclovir triphosphate from cells infected with herpes simplex virus type 1 – 10 hours, from cells infected with herpes simplex virus type 2 – 20 hours, from cells infected with varicella zoster virus – 7 h. T1 / 2 with CC less than 30 ml / min – 10-13 h.
Excreted by the kidneys by glomerular filtration and tubular secretion with urine (60-65% in the form of penciclovir), 27% with feces. Does not cumulate. It is excreted during hemodialysis.
Indications
Herpes zoster
postherpetic neuralgia
recurrent genital herpes.
Contraindications
Hypersensitivity, pregnancy, lactation, childhood.
Precautions: renal failure.
Use during pregnancy and lactation
FDA category of effect on the fetus is B.
Composition
1 tablet contains:
Active ingredient: 250 mg.
Dosage and administration of
Inside, for adults with acute herpetic infection – 250 mg 3 times a day for 7 days.
With herpes zoster (Varicella zoster) and high risk of developing postherpetic neuralgia – 250 mg 3 times a day for 7 days. Treatment should begin immediately after diagnosis.
For genital herpes caused by Herpes simplex (type II): for primary infection – 250 mg 3 times a day for 5 days, for relapses of chronic infection – 1000 mg 2 times a day once or 125 mg 2 times a day for 5 days. Treatment should begin immediately after the onset of the first symptoms of the disease.
For prevention – 250 mg 2 times a day. Periodic discontinuation of the drug at intervals of 6-12 months is recommended to assess possible changes in the course of the disease.
In patients with impaired renal excretory function, dose adjustment is required: with KK 30-59 ml / min – 250 mg 2 times a day
with KK less than 30 ml / min – 125 mg 3 times a day.
For patients on hemodialysis, 250 mg (for patients with Varicella zoster) and 125 mg (for patients with genital herpes), the dose should be taken immediately after the procedure, because after 4 hours of hemodialysis, the concentration of penciclovir in the plasma is reduced by approximately 75%.
Side effects of
Headache, nausea, dizziness, vomiting, diarrhea, allergic reactions of
in the elderly – confusion, hallucinations of
with reduced immunity – abdominal pain, fever and rarely – granulocytopenia and thrombocytopenia.
Drug interaction
drugs blocking tubular secretion, increase the plasma concentration.
Overdose
Symptoms: Failure to follow dose reduction guidelines with kidney function – Acute renal failure.
Treatment: symptomatic, hemodialysis.
Storage conditions
In a dry place, at a temperature not exceeding 30 ° C.
Expiration
3 years.
pharmacy leave sdflfp70 p17rod3 p17rod3 p17products1317 vocational
dosage form
dosage form
tablets
Apothex Inc., Canada
