Minaker, tablets 250 mg, 21 pcs.

Pharmgroup:

an antiviral agent.

Pharmic action:

Antiviral agent. Prodrug; is a 6-deoxydiacetyl analog of the active antiviral agent penciclovir. Being transformed in the body into active compound – penciclovir, it acts on viruses Herpes simplex (types 1 and 2), Varicella zoster, Epstein-Barr virus.

Infiltrating into virus-infected cells, penciclovir is phosphorylated by viral thymidine kinase to penciclovir monophosphate, which is then converted into penciclovir triphosphate under the action of cellular kinases. Penciclovir triphosphate is retained in the infected cell for more than 12 hours and suppresses viral DNA replication.

It has no effect on uninfected cells. It is active against some acyclovir-resistant Herpes simplex virus strains that have an altered DNA polymerase.

Pharmacokinetics:

After oral administration it is quickly and almost completely absorbed and quickly converted to active penciclovir. Bioavailability is 77%. TCmax – 45 min, Cmax after a single dose of 500 mg – 3.3-4.2 mcg/ml. Volume of distribution – 1 l/kg. Binding to 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 hours. T1/2 at a CKR of less than 30 ml/min is 10-13 hours.

Extracted by kidneys through glomerular filtration and tubular secretion, in the urine (60-65% as penciclovir), 27% – in the faeces. It does not accumulate. It is excreted with hemodialysis.

Indications

Infections caused by Herpes simplex (type I and II):
primary infection, exacerbation of chronic, prophylaxis;
herpes shingles (Varicella zoster),
postherpetic neuralgia,
recurrent genital herpes.

Active ingredient

Composition

Active substance:

famcyclovir 125, 250 and 500 mg;

How to take, the dosage

Orally, in adults with acute herpes infection – 250 mg 3 times a day for 7 days.

In shingles (Varicella zoster) and a high risk of post-herpetic neuralgia – 250 mg 3 times a day for 7 days. The treatment should be started as soon as the diagnosis is established.

In genital herpes caused by Herpes simplex (type II): in primary infection – 250 mg 3 times daily for 5 days, in relapses of chronic infection – 1000 mg 2 times daily once or by 125 mg 2 times daily for 5 days. The treatment should be started as soon as the first symptoms of the disease appear.

For prophylaxis it is 250 mg 2 times a day. It is recommended to periodically discontinue the preparation with 6-12 months intervals in order to evaluate possible changes of disease course.

In patients with impaired renal excretory function it is necessary to correct the dosage:
In IQ 30-59 ml/min – 250 mg 2 times per day;
In IQ less than 30 ml/min – 125 mg 3 times per day.

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 plasma concentration of penciclovir decreases by approximately 75%.

Interaction

The drugs that block tubular secretion increase plasma concentrations.

Special Instructions

In the presence of clinical manifestations of genital herpes, patients should avoid sexual intercourse during antiviral treatment.

Contraindications

Hypersensitivity, pregnancy, lactation, childhood.

With caution: renal failure.

Side effects

Headache, nausea, dizziness, vomiting, diarrhea, allergic reactions;

In the elderly, confusion, hallucinations;

In immunocompromised patients, abdominal pain, fever and rarely granulocytopenia and thrombocytopenia.

Overdose

Symptoms: acute renal failure if dose reduction recommendations are not followed with regard to renal function.

Treatment: symptomatic, hemodialysis.

Pregnancy use

The FDA fetal action category is B.

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