Acyclovir ointment and tablets - detailed instructions for use, reviews

From this article you will learn:

what does Acyclovir help with?
instructions for use of acyclovir (in children and adults),
what analogues are there?
tablets, ointment or cream acyclovir – price 2021.

Acyclovir is the first specific antiviral drug, which since 1981 has been widely used in the treatment of herpes simplex virus (types HSV-1, HSV-2), as well as herpes zoster and chickenpox. Type of virus HSV-1 - causes herpes on the lips, facial skin and oral mucosa. The HSV-2 virus type is predominantly genital herpes only, but in 10% of patients it can also cause both herpetic stomatitis and herpes labialis.

Acyclovir has a rather weak effect on other representatives of the herpevirus family (Epstein-Barr virus, cytomegalovirus). The drug is very well tolerated by children, even the youngest, and can also be used during pregnancy. Acyclovir cream or ointment is intended for external use and is available without a prescription, but Acyclovir tablets or vials for intravenous administration should be used only as prescribed by a doctor!

Acyclovir: photos of several release options

Composition and release form –

Pharmacological action of the drug -

Acyclovir itself is not an active substance. Acyclovir acquires its antiviral activity only after it enters virus-infected cells, in which (under the influence of the enzyme “viral thymidine kinase”), acyclovir is converted first into acyclovir monophosphate, and then into acyclovir triphosphate. The latter is already an active component, which suppresses the reproduction of the herpes simplex virus - by incorporating acyclovir triphosphate into the viral DNA.

When will acyclovir be effective?

The use of acyclovir will give a pronounced effect only if several conditions are met. Firstly, if you started using the drug - during the prodromal period of the development of a herpetic infection (i.e. when there are no actual clinical manifestations yet, but there is already a burning, tingling or distension of tissue - in places where herpetic blisters will soon appear). Secondly, the effectiveness will be high even if therapy is started - within the first 12 hours from the moment the rash appears. By starting treatment this early, it is possible to reduce the duration of herpes symptoms by approximately 20 to 50%.

If the use of acyclovir begins from 12 to 72 hours (from the moment the rash appears), then its effectiveness will be very moderate. If more than 72 hours have passed and/or the herpetic blisters have already opened, acyclovir will not have a significant effect on the course of the disease at all. But when prescribing antiviral drugs (this applies to both creams and tablets), it is also important to take into account the potential risk of resistance of your herpes virus to acyclovir. All of the above is true for both tablets and Acyclovir ointment.

Important: with Acyclovir cream for the treatment of herpes on the skin or red border of the lips - everything is quite simple, and the main thing is to observe the correct timing of the start of therapy. But for acyclovir tablets for oral administration, it is also important to choose the correct dosage. Recent clinical studies (source) have shown the ineffectiveness of systemic therapy - using the basic standard dosage of acyclovir (200 mg 5 times a day, for 5 days). And below we will tell you what dosages are now recognized by the medical community as effective.

Resistance of the herpes virus to acyclovir -

In patients with good immunity, resistance to Acyclovir is rare - approximately 1 to 3% of cases. However, there is a clear relationship: the risk of developing resistance to acyclovir is directly proportional to the frequency and duration of its use. Resistance occurs especially often - 1) in immunocompromised patients who in the past regularly used drugs with acyclovir for treatment or prophylactic purposes, 2) in patients with HIV infection, 3) in patients with a history of bone marrow transplantation.

In the above groups, resistance can range from 7 to 27%, and according to some sources, even reach 30-36%. If any of the above applies to you, then you should not waste precious time taking acyclovir, choosing its stronger analogues. We are talking about antiviral tablet drugs based on Famciclovir or Valaciclovir. If we are talking about the form in the form of a cream (for external use), then it is better to use Fenistil-Pentsivir cream (contains penciclovir).

Side effects

From the blood and lymphatic system: anemia, thrombocytopenia, leukopenia.

From the immune system: anaphylaxis.

Mental disorders and disorders of the nervous system: headache, dizziness, agitation, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms, convulsions, drowsiness, encephalopathy, coma.

The above neurological reactions are generally reversible and usually occur in patients with renal failure or other risk factors.

From the respiratory system and chest organs: shortness of breath.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain.

From the hepatobiliary system: reversible increase in the level of bilirubin and liver enzymes, jaundice, hepatitis.

From the skin and subcutaneous tissue: itching, rash (including photosensitivity), urticaria, increased diffuse hair loss (since hair loss can be associated with a large number of diseases and medications, a clear connection with acyclovir was not found), angioedema.

From the kidneys and urinary system: increased levels of urea and creatinine in the blood, acute renal failure, pain in the kidneys.

Kidney pain may be associated with renal failure and crystalluria.

Acyclovir ointment: instructions for use

Let's now figure out what Acyclovir ointment or cream helps with. This drug can only be used externally, and indications for its use:

infections of the skin and mucous membranes caused by the herpes simplex virus (types HSV-1 and HSV-2), i.e. First of all, this is herpes on the lips and skin around the mouth, as well as as part of complex therapy for the treatment of genital herpes.

We have already said above that the key to the effectiveness of treatment with acyclovir is the earliest possible start of using the drug (24stoma.ru). For example, in the prodromal period (when the feeling of itching and bloating is just beginning to appear), or during the first 12 hours from the moment herpetic blisters erupt. If acyclovir ointment or cream is started to be used only after 48 hours or even after the herpetic blisters have opened, this will not reduce the duration of symptoms at all.

Application regimen - the effective concentration of acyclovir for the treatment of herpes of the lips and facial skin is 5%. It is very important to strictly follow the application regimen. For acyclovir ointment, the instructions for use state that the drug should be applied to the skin and red border of the lips 5-8 times a day (i.e., preferably every 2 hours while you are awake). The cream is applied in a thin layer to the areas of herpetic rashes and the adjacent skin - with careful massaging movements. The usual course of use is 5-6 days, but with severe clinical manifestations - up to 10 days.

How to choose ointment or cream with acyclovir –

Please note that acyclovir ointment and acyclovir cream differ in their properties. The ointment is absorbed much less well, which means the acyclovir contained in it will penetrate much worse into the skin cells affected by herpes, which reduces the effectiveness of the drug. The ointment is much cheaper to produce (than cream), and therefore 5% acyclovir ointment - the price starts from only 35 rubles.

The disadvantage of Acyclovir is also its rather poor penetration through the stratum corneum of the epidermis of the skin. To increase skin permeability to acyclovir, a number of manufacturers add propylene glycol to the composition. This component is added to the original acyclovir preparations - Zovirax cream and Zovirax Duo-Active cream, as well as to generics - Acyclovir-Belupo, Acyclovir-Sandoz and the Russian ointment Acyclovir-Acri.

If we compare the effectiveness of cream and ointment with the same 5% concentration of acyclovir, then the effectiveness of the cream will be higher. The cream tends to be absorbed faster, which means that acyclovir will better penetrate from the cream into the skin cells affected by the virus. Zovirax cream also contains dimethicone (silicone), which allows even cosmetics to be applied immediately after the cream is absorbed. On the other hand, Acyclovir-Acri 5% ointment will cost you only 40 rubles, and Zovirax cream will cost you 190 rubles. By the way, dimethicone is also included in the Acyclovir-Sandoz cream, which costs from 150 rubles.

Zovirax or Acyclovir: which is better? So, Zovirax cream is certainly better - when compared with Acyclovir Acri or similar drugs from other manufacturers. In addition to the classic Zovirax cream, which contains 5% acyclovir, propylene glycol and dimethicone, there is also Zovirax Duo-Active cream (it additionally contains 1% hydrocortisone). For example, if you start using this cream early in the prodromal period, due to hydrocortisone it can reduce the number and size of herpetic blisters that form, and sometimes even prevent their formation.

In our opinion, Zovirax Duo-Active cream is the best option for ointment or cream with acyclovir for herpes on the lips or facial skin. This cream has only 2 disadvantages - the price starts from 350 rubles (only 2 g per tube) and the age limit is up to 12 years. But, if we consider good herpes creams not only based on acyclovir, then Fenistil-Pentsivir (based on penciclovir) is also a very good cream. But the latter is currently temporarily unavailable in pharmacies - most likely due to the re-registration of the drug in Russia.

Acyclovir tablets: instructions for use

The instructions for use on Acyclovir tablets contain information that these are prescription drugs, i.e. They should be used in children and adults only as prescribed by a doctor. Let's look at the indications for use.

Indications for use –

treatment of infections caused by the herpes simplex virus (herpes of the lips and facial skin, genital herpes),
prevention of infections caused by the herpes simplex virus in patients with immunodeficiency,
treatment of chickenpox (chickenpox),
treatment of herpes zoster,
prevention of cytomegalovirus infection (during bone marrow transplantation).

We have already said above that taking the drug will be effective if you start taking it - either in the prodromal period (i.e. when there are no actual herpetic vesicles yet, but there is already itching or burning), or in the first 12 hours from the moment of appearance rashes. Moderate effectiveness can be achieved with a later dose, but no later than 72 hours from the moment the rash appears. If the herpetic blisters have already opened, taking acyclovir will no longer reduce the severity of symptoms and will not speed up healing.

A very important question is the dosage of acyclovir when taken orally. Very often in the instructions you can find information that in children over 2 years of age and adults, the standard dosage is used to treat herpes - 200 mg 5 times a day, for 5 days. Clinical studies (source) show that this dosage regimen has no effect at all - neither on the duration of the disease, nor on the healing time of ulcerations that form at the site of opened herpetic vesicles.

Acyclovir tablets: instructions for use adults for herpetic lesions of the lips, facial skin and herpetic stomatitis in children over 2 years of age and adults - you need to take 400 mg 5 times a day, for 5 days (we explained above why this particular dosage). How to take acyclovir in children under 2 years of age and infants - the dosage is reduced by 2 times, i.e. An effective dosage regimen would be 200 mg 5 times a day for 5 days. If necessary and with the recommendation of a doctor, taking the drug can be extended up to 10 days.

Acyclovir for chickenpox -

For the treatment of chickenpox (chickenpox) in children and adults over 6 years of age, the dosage of acyclovir is 800 mg 5 times a day, and in children from 3 to 6 years old - 400 mg 5 times a day. Thus, the drug must be taken every 4 hours, except during night sleep. The duration of treatment is 7 days.

What drugs to choose -

Reviews for acyclovir tablets are more positive when using the original acyclovir from GlaxoSmithKline (UK). The drug is called Zovirax tablets 200 mg, and the cost of 1 package of 25 tablets will be about 260 rubles. Thus, taking into account the optimal single dosage of 400 mg, which is 2 tablets per dose, you will need 2 packages of the drug for a 5-day course of treatment. An alternative option is Acyclovir Akrikhin tablets of 200 or 400 mg (Russian production), which will cost from 70 rubles and from 200 rubles, respectively.

Zovirax tablets instructions for use (view PDF)
Acyclovir tablets instructions for use 200 mg (view PDF)
Acyclovir tablets instructions 400 mg (view PDF)

Note!

Description of the drug Acyclovir 400 Herds table. 400 mg No. 35 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Acyclovir: price for 2021

The price of the drug acyclovir in 2021 has not increased compared to previous years, which is most likely due to high competition between manufacturers, as well as the appearance in pharmacies of a large number of more modern and effective analogues of acyclovir. The highest price is the original Acyclovir from GlaxoSmithKline (UK), sold under the Zovirax brand.

Ointment and cream Acyclovir 5% –

Acyclovir-Acri ointment, 5 g – from 35 rubles,
Acyclovir-Belupo cream, 5 g – from 70 rubles,
Acyclovir-Sandoz cream, 5 g – from 150 rubles (2 g tube – from 75 rubles),
Zovirax cream, 5 g – from 190 rub.
Zovirax Duo-Active cream, 2 g – from 350 to 400 rubles.

Please note that all of the above products contain propylene glycol (to enhance the penetration of acyclovir into tissues). However, despite this, the ointment will in any case be inferior in effectiveness to the cream. The second point is that only Acyclovir-Sandoz cream and both Zovirax creams contain dimethicone, which will allow you to easily apply cosmetics over the absorbed cream.

Eye ointment Acyclovir 3% –

Acyclovir-Sintez (Russia) – from 150 rubles,
Acyclovir-Akos (Russia) – from 150 rubles,
Zovirax 3% (UK) – from 240 rubles.

Acyclovir tablets: price

Zovirax 200 mg (25 tablets) – from 250 rubles,
Acyclovir Acri 200 mg (20 tablets) – from 70 rubles,
Acyclovir Acri 400 mg (20 tablets) – from 220 rubles.

Ointment, cream, tablets Acyclovir: reviews

Acyclovir is one of the first antiviral drugs.
Of course, this is not the best antiherpetic drug, but in principle it works well in children, as well as in adults who have not received long-term regular treatment with acyclovir in the past (especially against the background of reduced immunity, since in this case one can expect the development of virus resistance herpes to acyclovir). In addition, for Acyclovir tablets, reviews will be good only if you start taking them early (the same applies to ointment and cream forms). Clinical studies have shown that the best treatment results are achieved when patients begin to use acyclovir, either in the prodromal period or in the first 12 hours from the onset of herpetic eruptions.

It makes sense to start using acyclovir cream or ointment only during the first 48 hours from the moment of illness, until the herpetic blisters burst (after this point, use will no longer speed up recovery). As for tablets with acyclovir, you can start using them no later than 72 hours, but you need to keep in mind that the later you start taking them by the end of this period, the less the result of treatment will be.

The main disadvantages of the drug Acyclovir are:

1) Low bioavailability of the drug - it is only 10 to 20% of the amount taken. In this regard, Acyclovir must be taken 5 times a day, which is not very convenient (this applies to both tablet forms and forms in the form of an ointment or cream). Valacyclovir and famciclovir have a bioavailability of 50 to 74%, which is why they usually need to be used only 2 times a day.

2) Poor penetration into the skin - products in the form of ointments or creams for external use have a significant drawback, which is that acyclovir does not penetrate very well through the most superficial layer of the skin (the stratum corneum of the epidermis). This certainly reduces the effectiveness of the drug. Some manufacturers, in order to increase the permeability of acyclovir, add propylene glycol to the ointment or cream.

3) Low tropism of acyclovir to the virus - acyclovir equally penetrates both healthy and cells infected with the herpes virus. If there is a “viral thymidine kinase” (enzyme) in the cell, acyclovir is activated and blocks the reproduction of the virus. However, the problem is that acyclovir has low tropism for viral thymidine kinase, so it may not find it in infected cells. Accordingly, in this case it simply does not convert into the active form of acyclovir-3-phosphate, which blocks the reproduction of the herpes virus.

4) Resistance to the drug - compared to all other modern antiviral drugs - resistance to the herpes virus most often occurs to acyclovir. According to statistics, in people with weakened immune systems, resistance occurs in 7-10% of cases, and in some groups of patients with immunodeficiency conditions it even reaches 27% or more of cases.

5) Intracellular half-life - acyclovir has a very short intracellular half-life (about 1 hour), which leads to a complete cessation of blocking viral replication - immediately after taking the drug. For example, the antiviral drug Penciclovir has a longer intracellular half-life (up to 20 hours), which ensures sufficient clinical antiviral effectiveness for up to 2 days after discontinuation of the drug.

Below you will find information about modern analogues of Acyclovir.

Overdose

Symptoms

Acyclovir is only partially absorbed from the gastrointestinal tract. Patients have been reported to accidentally ingest up to 20 g of acyclovir internally without causing toxic effects. In case of accidental repeated oral overdose of oral acyclovir, gastroenterological (such as nausea and vomiting) and neurological symptoms (headache and confusion) occur over several days. In case of an overdose of intravenous acyclovir, the level of serum creatinine and blood urea nitrogen increases, which leads to renal failure. Neurological manifestations of overdose may include confusion, hallucinations, agitation, seizures and coma.

Treatment

The patient must be carefully examined to identify symptoms of intoxication. Since acyclovir is well removed from the blood by hemodialysis, the latter should be used in case of overdose.

Contraindications to Acyclovir and features of its use -

The drug should not be taken if you are hypersensitive to acyclovir or valacyclovir. Do not use the intravenous route of administration of the drug during breastfeeding. The drug should also not be used in cases of severe renal impairment. Forms of the drug for external use (creams and ointments) cannot be used to treat the mucous membranes of the mouth, eyes, and vagina.

Acyclovir is not effective against influenza and ARVI, because it has no effect on these types of viruses at all. The drug is prescribed with great caution for dehydration and renal failure. When taking tablets, they should be washed down with a full glass of water (regardless of meals, since simultaneous food intake does not affect the absorption of the drug in the intestines). Acyclovir and alcohol: the compatibility of taking antibacterial and antiviral drugs with alcohol consumption reduces the effectiveness of treatment.

Important: taking acyclovir has nuances that are important for patients with gastrointestinal diseases. For diseases that occur with impaired absorption in the gastrointestinal tract, it is necessary to either increase the dosage of acyclovir, or (optimally) switch to intravenous administration of the drug.

Acyclovir during pregnancy and breastfeeding -

Acyclovir tablets during pregnancy can only be used as directed and under the supervision of a physician. The drug can be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus. But acyclovir ointment or cream during pregnancy (i.e. forms for external use) can be used without a doctor’s prescription.

When breastfeeding - there are no contraindications for using Acyclovir cream or ointment during lactation, i.e. You can use such drugs without a doctor’s recommendation. But with the exception of the drug Acyclovir Duo-Active, which in addition to acyclovir also contains 1% hydrocortisone (here it is advisable to obtain a doctor’s permission).

Acyclovir tablets can be used during breastfeeding, but only as prescribed by a doctor (and here you need to pay attention to some details). For example, according to the instructions, the original drug with acyclovir - Zovirax 200 mg tablets - can be used during breastfeeding, but the Russian tablets Acyclovir-Akrikhin cannot be used in nursing according to the instructions.

There are clinical studies that show that when a breastfeeding woman uses high dosages of tableted acyclovir, the dosage of acyclovir contained in breast milk will be only about 1% of the standard pediatric dosage taken for children (source). This is due to the fact that the baby receives acyclovir orally in breast milk, and acyclovir, in turn, has low bioavailability (only 10 to 20% of the total volume of the drug enters the blood from the intestines). In principle, this should prevent any negative side effects from occurring in breastfed babies, but you should still get a doctor's prescription.

Features of application

Pregnant

There was no increase in the number of birth defects in children whose mothers used acyclovir during pregnancy compared to the general population. However, acyclovir tablets should be used only when the potential benefit of the drug for the mother outweighs the possible risk to the fetus.

When taken orally 200 mg of acyclovir 5 times a day, acyclovir passes into breast milk in concentrations of 0.6-4.1% of the corresponding level of acyclovir in the blood plasma. Potentially, a child fed with this milk can absorb acyclovir at a dose of up to 0.3 mg/kg body weight per day. Therefore, prescribing acyclovir to breastfeeding women should be done with caution, taking into account the risk/benefit ratio.

Drivers

When deciding whether to drive a car or operate machinery, the clinical status of the patient and the side effect profile of the drug should be taken into account. Studies of the effect of acyclovir on the reaction rate when driving vehicles or operating other mechanisms have not been carried out. In addition, the pharmacology of acyclovir does not give reason to expect any negative effects.

Acyclovir - modern analogues of the drug

Below we will talk about several of the most common tablet analogues of acyclovir, the effectiveness of which is higher, and the resistance of the herpes virus to these drugs is lower. In addition, they have a very convenient dosage regimen. Please note that all tablet drugs discussed below are prescription drugs and should be used only as prescribed by a doctor.

Valacyclovir –

Valacyclovir is a precursor substance to acyclovir, i.e. this drug is converted into acyclovir after it enters the body. The most famous drug in the world based on valacyclovir is Valtrex (manufactured by GlaxoSmithKline, UK).

Valacyclovir and Acyclovir: what is the difference? It is the higher bioavailability of valacyclovir compared to acyclovir - 50% instead of only 10-20%. This allows, when taking valacyclovir tablets, to create a very high concentration of acyclovir in the tissues, which, when taking the conventional drug Acyclovir, can only be achieved when administered intravenously. In addition, the high bioavailability of valacyclovir also makes it possible to reduce the frequency of dosing to just 2 times a day.

Dosage regimen - clinical studies have shown that taking high dosages of the drug for 1 day was most effective for the treatment of herpes on the lips, facial skin, and herpetic stomatitis. The dosage regimen is 2000 mg 2 times a day, with an interval of 12 hours (1 day in total), but this regimen is effective if treatment begins no later than 12 hours from the onset of herpetic rashes, and also if you have satisfactory or good immunity.

If more than 12 hours have passed, or you have a weakened immune system, it would be optimal to use the standard treatment regimen: 500 mg 2 times a day for 3-5 days (for severe herpes infection - up to 10 days).

Valaciclovir: price 2021 cost of the original drug “Valtrex” (UK) – from 1350 rubles for 10 tablets. 500 mg each. The drug Valvir (Bulgaria) - costs from 750 rubles per pack of 10 tablets. 500 mg each. The price for Valacyclovir-Akos, produced in Russia, starts from 450 rubles (for a package of 10 tablets of 500 mg). When choosing a drug, keep in mind that if your herpes virus is resistant to acyclovir, taking valacyclovir will also be ineffective.

Famciclovir (Favirox, Famvir) –

Famciclovir is the most effective remedy for herpes, and is a tablet form of penciclovir (penciclovir is also contained in Fenistil-Pentsivir cream for the treatment of herpes on the lips and facial skin). The bioavailability of the drug is about 77%, and the tropism of penciclovir to the virus is at least 2 times higher than that of acyclovir. All this makes famciclovir one of the most effective drugs. Experts consider it even more effective - even compared to valacyclovir.

Dosage regimen - for herpes of the lips, facial skin and herpetic stomatitis, this drug can also be taken for only 1 day. The most effective dosage regimen is 750 mg 2 times a day, with an interval of 12 hours (1 day in total). However, a single dose of 1500 mg of the drug is possible, although clinical studies have shown a slightly worse result of such therapy (compared to the previous regimen). It should be noted that such short regimens will be effective only if taking the drug begins no later than 12 hours from the moment the herpetic rash appears, and also if you do not have a weakened immune system.

If more time has passed, or you have a weak immune system, in this case herpes of the lips, facial skin and herpetic stomatitis are best treated using the traditional full treatment regimen for 5 days. Standard regimen: 250 mg 2 times a day, for 5 days (for severe herpes infection - up to 7-10 days). But I would like to add that numerous clinical studies have revealed the weak effectiveness of this regimen - especially in patients with a poor immune system.

Studies have shown that the effectiveness of therapy increases significantly if famciclovir is prescribed in higher dosages. In patients with good immunity, it is better to use the regimen - 500 mg 2 times a day (for 5 days), and in patients with weakened immunity - 500 mg 3 times a day (for 7 days).

Important: once again we draw your attention to the fact that short one-day treatment regimens for herpetic infections work well - 1) only if you start taking medications no later than 12 hours from the moment the herpetic rash appears, 2) if you have a more or less normal immune system. In patients with poor immunity, short courses of therapy are ineffective, even if treatment is started early. And therefore, in patients with weak immunity, standard full treatment regimens should always be used - preferably famciclovir.

Fenistil-Pentsivir cream –

The drug Fenistil-Pentsivir is the same famciclovir, but not in tablets, but in the form of a cream. Intended for the treatment of herpes on the lips and facial skin in adults and children over 12 years of age. The peculiarity of this cream is that it will be effective even if you do not start using it immediately from the moment the herpetic rash appears (but after a longer time).

For Fenistil-Pentsivir the price will be from 430 rubles (per tube of 2 g). After use, the drug still remaining in the cells will continue to have an antiviral effect for another 2 days. The only drawback is the frequency of application - 8 times a day for 4 days (at 2 hour intervals during the daytime).

But there is an excellent effect, and almost complete absence of the risk of herpes virus resistance to this drug. In addition, the drug contains cetomacrogol and propylene glycol, which facilitate the penetration of penciclovir into infected skin cells. We hope that our article on the topic “Acyclovir - price, instructions for use” was useful to you!

Sources:

1. Higher medical education of the author of the article, 2. National Library of Medicine (USA), 3. The National Center for Biotechnology Information (NCBI, USA), 4. “Modern approaches to the treatment of herpes (HSV) infections in adults” (Khokhlova N.I.), 5. Composition of drugs taken from the official websites of manufacturers.