Acyclovir: instructions for use, indications,contraindications, side effects

Update: February 2019

Acyclovir is a popular antiviral drug that has
selective activity against herpes simplex viruses
(Herpes simplex) 1 and 2 types, Varicella zoster viruses and
Epstein-Barr, as well as cytomegalovirus. Antiviral activity
acyclovir is achieved by suppressing viral reproduction
particles.

Most often used for the treatment of herpes and has a high
efficacy when applied to the bubble stage rash. With
later use speeds up healing and resolution
items. The instructions for use of acyclovir indicated that
The drug has an immunostimulating effect.

Pharmacological group: Antiviral drugs

Composition, physico-chemical properties, cost

Acyclovir is available in four dosage forms:
lyophilisate, cream, ointment, tablets.

Lyophilisate

Cream 5 %

Ointment 3%

Pills Ацикловир

Main substance Acyclovir 250 mg or 500, 1000 mg in 1 bottle Acyclovir 50 mg in 1 g of cream Acyclovir 30 mg in 1 g ointment Acyclovir 200 mg or 400 mg
Excipients Sodium hydroxide Medical vaseline oil, petrolatum, cetostearyl alcohol,
propylene glycol, poloxamer 407, purified water, dimethicone
Emulsifier, lipocomp “C”, polyethylene oxide 400, nipazol,
nipagin, purified water
Milk sugar, potato starch, aerosil,
polyvinylpyrrolidone weight, calcium
stearic
Physicochemical properties Powder white or white and cream color Cream практически белого цвета Ointment бело-желтого цвета Pills плоские, белого цвета
Packaging Glass Bottles, Packaged Cardboard Aluminum tube of 5 gr, in a cardboard box Aluminum tube of 5 gr, in a cardboard box On 10 tablets in cellular packing planimetric, in packs
cardboard
Price 130-410 rub. 40-70 rubles 20-30 rub. 30-150 rubles

pharmachologic effect

Antiviral activity ацикловира объясняется его
the ability to inhibit the synthesis of virus DNA, i.e. due to
suppression of replication of drug-sensitive viral particles.
Genetic apparatus – nucleic acids DNA and RNA are
complex compounds with nitrogenous bases included in them.
Each individual has its own sequence of nitrogenous
grounds.

Nitrogenous bases when combined with carbohydrates (deoxyribose
and ribose) form nucleosides. One of them, called thymidine,
is activated in deoxythymidine by the action of the enzyme thymidine kinase.
Deoxythymidine is incorporated into the chain of replicated DNA. Acyclovir
being a synthetic substance, similar in structure to thymidine.
As a result, it interacts with the enzyme
thymidine kinase, turning into mono-, di- and triphosphate. Exactly
Acyclovir triphosphate is able to integrate into a chain of replicated
DNA and cause its damage. At the same time oppression occurs.
viral DNA polymerase, viral synthesis is violated and viral
the particle does not multiply.

Clinically, the effect of acyclovir is manifested by stopping.
spreading of skin herpes rash and healing available
bubbles, reducing pain and itching, elimination of the phenomena of common
intoxication, if any. Treatment ацикловиром позволяет
prevent complications of herpes infection on internal
organs.

Acyclovir помимо противовирусного действия, укрепляет
immunity. The drug manifests its qualities both locally and in
the whole body in internal administration or in / in the introduction, without damaging
at the same time, human cells, i.e. purposefully affects only
on the genetic material of viruses.

Pharmacokinetics

Lyophilisate и таблетки

With внутреннем приеме биодоступность препарата составляет около
15-30%. Actively distributed in body fluids and tissues.
person Associated with plasma proteins at 9-33%. Metabolism
Acyclovir is administered in the liver. Период half-life при
oral administration – about 3 hours, with a / in use – about 2.5
hours Excreted in urine and in small quantities through the intestines with
feces.

Ointment и крем

The drug quickly penetrates the corneal epithelium, creating
required therapeutic concentration of acyclovir in
intraocular fluid, and quickly absorbed into the affected skin during
external use. With данных способах применения создаваемая
drug concentration in the blood has not been studied. Minor part
acyclovir is detected in the urine.

Indications for use

Cream — инфекции кожи, спровоцированные вирусами Varicella zoster
and Herpes simplex (zoster, herpes skin, chicken pox). Ointment —
herpetic keratitis and other eye damage caused by herpes
simplex 1 or 2 tons

Pills:

  • Viral infections of mucous and skin (Herpes simplex viruses 1 and 2)
    m.), primary and secondary, including herpes genital;
  • Prevention of exacerbations of recurrent viral infections
    (Herpes simplex 1 and 2 tons.) In the normal state of immunity and in
    people and immunodeficiency;
  • As a drug for complex treatment in groups of patients with
    pronounced immunodeficiency and people after bone transplantation
    brain;
  • Therapy for acute and recurrent diseases caused by the virus
    Varicella zoster and herpes zoster).

Lyophilisate:

  • Viral infections, the etiological factor of which are
    Herpes simplex viruses 1 and 2 tons and Varicella zoster;
  • Prevention of diseases caused by these viruses;
  • Severe immunodeficiency (as a complex drug
    treatment);
  • Treatment of patients after bone marrow transplantation
    (prevention of cytomegalovirus infection).

Contraindications

  • Lactation period;
  • Hypersensitivity to the components of acyclovir or
    valacyclovir;
  • Children’s age up to 3 years (tablets).

The pills and lyophilisate are prescribed with caution:

  • during pregnancy;
  • for the treatment of the elderly;
  • kidney dysfunction;
  • with a history of various neurological reactions in
    response to cytotoxic drugs.

Dosage

Before use Dosage A course of treatment

Cream

Wash hands with a cream before and after treatment.
soap Do not rub damaged skin.

Adults and children:

Applying the cream to the affected parts five times a day after 4
h, except at night time of day.

Course – 5 days, maximum – 10 days. The greatest effect
is achieved at the beginning of treatment in the prodromal period (up to
rash).

Ointment

До процедуры и после нее тщательно вымывают руки с soap Adults and children: полоску глазной мази длиной 1 см помещают в
lower conjunctival sac every 4 hours, five times a day.
A course of treatment – до полного заживления плюс еще 3 дня после
healing.

Lyophilisate

The drug after preparation of the solution is administered intravenously
drip.
Adults and children from 12 liters: 5-10 mg per 1 kg of weight, with an interval
between injections – 8 hours. Children 2 months-12 l: 250-500 mg / m2
body surfaces, with an interval between injections of 8 hours. Dei 0-3 months:
10 mg per 1 kg of weight, with an interval between injections – 8 hours.
The duration of treatment is set individually.

Pills

Accepted during or immediately after a meal, drinking water.

Treatment of diseases of the mucous and skin (Herpes simplex 1 and 2
t):
Adults: 200 mg five times a day for 5 days in a row, observing
4-hour break between receptions (night break – 8 hours). In heavy
cases, the course is extended to 10 days.
Severe immunodeficiency, condition after transplantation
CM:
Adults: 400 mg five times a day.
Prevention of recurrence of infections, Herpes simplex 1 and 2 tons.
people with normal immunity:
200 mg four times a day or 400 mg twice a day.
Prevention of infections that cause Herpes simplex 1 and 2 tons.
in immunocompromised patients:
200 mg four times a day or 400 mg five times a day
(in severe condition). Preventive course is set to
individually based on the risk of developing infections.
Treatment of Varicella zoster virus infections:
  • Adults: 800 mg five times a day every 4 hours with an 8-hour
    break for the night, the course of 7-10 days.
  • Children: 20 mg per 1 kg of body weight four times a day. for 5
    days
Treatment for Herpes zoster virus infections: Adults and children from 3 years: 800 mg four times a day every
шесть часов for 5 days
Treatment and prevention of infections caused by Herpessimplex 1 and
2 tons in children with normal immunity and immunodeficiency:
  • Children 3-6 years: 400 mg four times a day;
  • Children from 6 liters: 800 mg four times a day. Курс 5 days

special instructions

  • In oral and intravenous use of the drug in the elderly
    patients need to organize adequate intake
    liquids;
  • When treating patients with end-stage renal
    failure dose is reduced to 200-800 mg of acyclovir twice per
    day (depending on the pathology);
  • The use of acyclovir in pregnant women is possible when exceeding
    real benefit for the mother over the possible risks to the fetus.
  • The external forms of acyclovir should be avoided.
    mucous membranes;
  • In the treatment of the eyes can not use lenses for
    treatment period.

Side effect

  • Allergic local reactions: in extremely rare cases.
    hypersensitivity reactions develop (urticaria, edema
    Quincke). Often there is itching, redness, peeling.
  • Eye with the application: rarely – keratopathy
    superficial punctate, conjunctivitis, blepharitis. More common
    slight burning sensation.
  • Oral administration: nausea, diarrhea, soreness in
    stomachache, vomiting, fatigue, skin rash, headaches,
    dizziness, hallucinations, insomnia or drowsiness, fever.
    Rarely observed hair loss and changes in the blood picture.
  • With the / in the introduction: crystalluria, acute renal
    insufficiency, encephalopathy, inflammation of the veins at the injection site,
    vomiting and nausea.

Overdose

Possible with parenteral and internal medication.
forms and accidental ingestion of cream and ointment.
Симптомы: неврологические нарушения, головная боль, одышка,
vomiting, diarrhea, nausea, kidney dysfunction, convulsions, coma. Treatment
stationary.

Drug interactions

  • In combination with immunostimulants enhanced effect
    acyclovir.
  • In combination with probenecid the period increases half-life
    acyclovir.
  • With simultaneous treatment with nephrotoxic drugs
    increases the risk of kidney dysfunction.

Analogs

Zovirax, Virolex, Acyclovir-Teva, Gerperax, Medovir,
Acyclostad In the instructions to the ointment Acyclovir-Akri specified composition
similar ointment Acyclovir.

Medovir

2200 rub.

Zovirax

cream 180-280 rub, bottles 1700 rub.

Virolex

tabl 250 rub, bottles 1500 rub.

Gerperax

ointment 50- 70 rubles.

Acyclostad

Автор: врач-гигиенист, эпидемиолог

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