In the article, we will consider the side effects of Acyclovir, and also tell you what kind of medicine it is and what it is used for.
A pharmacological preparation is an antiviral agent used in the treatment of herpes infection. The medication is used in the treatment of patients of any age category. The success of treatment depends on the stage of the disease, the characteristics of the pathological process and individual characteristics.
The list of possible side effects of Acyclovir in tablets is impressive. But negative reactions can cause other forms of release.
Composition and form of release
This medication is available in several dosage forms:
- Cream for external application of 5% - packaged in aluminum tubes of 10 g, 5 g and 2 g.
- Ointment for external use 5% - aluminum tubes of 10 g, 5 g, 3 g and 2 g, as well as glass jars of 20 g, 10 g, 5 g.
- Eye ointment 3% - available in aluminum tubes, packaged in 5 g.
- Lyophilisate for the manufacture of solutions for intravenous infusion - is produced in bottles of 500 mg and 250 mg.
- Tablets for oral administration - 400 mg and 200 mg and 100 mg - blisters of 10 tablets.
The active element of this medication is the substance acyclovir, which is contained in different dosage forms in the following dosages:
- 1 g of ointment or cream - 50 mg;
- 1 bottle of lyophilisate - 1,000 mg, 500 mg and 250 mg;
- 1 g of ointment for the eyes - 30 mg;
- 1 tablet - 200 mg.
The side effects of Acyclovir can be clarified in the instructions.
pharmachologic effect
The drug is an antiviral medication for parenteral, oral, external and topical use, and is a synthetic substance identical to the acyclic purine nucleoside. This medication has great specificity for the viral agents Herpes simplex (type 1 and type 2), Epstein-Barr virus, cytomegalovirus and Varicella zoster. The highest activity of the active element is observed to HSV-1, then in descending order to HSV-2, VZV, EBV and CMV. The principle of action of the drug is due to the penetration of the active substance directly into those cells that are infected with the virus and produce thymidine kinase, as a result of which acyclovir begins to phosphorylate to acyclovir monophosphate.
The functionality of viral thymidine kinase to acyclovir is significantly higher than the effect of cell enzymes on it (the level of acyclovir monophosphate in infected cells is about 40-100 times higher). Subsequently, the process of formation of acyclovir triphosphate, which acts as a selective and sufficiently active inhibitor of viral DNA polymerase, occurs. Most likely, the principle of inhibition of deoxyribonucleic acid by acyclovir triphosphate is that it is a substrate for this enzyme, which allows the 3'– 5 'bond to be made. It is necessary to extend the DNA chain. As a result, premature rupture of the DNA chain is observed.
Side effects from Acyclovir in both adults and children can develop equally often.
Pharmacokinetic properties
The medicine "Acyclovir" in tablet form after oral administration is only partially absorbed in the intestine. After five times daily administration of 200 mg, the highest and minimum concentrations of the substance in the body are 0.8 and 0.5 μg / ml, respectively. In the composition of the cerebrospinal fluid, the level of acyclovir reaches 50% of the plasma. The drug binds relatively low to plasma proteins (9–34%) and is excreted mainly through the kidneys unchanged.
With external use of the ointment on the intact skin, the main substance has minimal absorption, it is not determined in the composition of urine and blood. In case of using it on the affected skin, it is absorbed to a moderate degree. In the absence of impaired renal function, the concentration in the blood reaches 0.28 μg / ml, in people with chronic renal failure, this indicator rises to 0.78 μg / ml. Excretion from the body is carried out by the kidneys.
The medicine "Acyclovir" in the form of an eye ointment easily penetrates the corneal epithelium, providing a therapeutic level in the intraocular fluid. There are no methods for determining a substance in the blood when using this dosage form.
Equilibrium maximum concentrations of the acyclovir infusion solution after administration for an hour at a dose of 2.5; 5; 10 and 15 mg / kg are 5.1; 9.7; 20.8 and 23.6 μg / ml, respectively. The lowest concentrations after 8 hours after intravenous administration at the indicated dosages are 0.6; 0.8; 2.4 and 2.1 μg / ml, respectively. After intravenous infusion in adults, the elimination half-life is approximately 2.9 hours. The main part of the active substance is excreted by the kidneys. Its main metabolite is 9-carboxymethoxymethylguanine.
Indications for the use of the medication
According to the annotation for use, the drug Acyclovir is orally and parenterally prescribed in the treatment of the following pathological conditions:
- recurrent forms or genital herpes of the primary type, which occurs with severe symptoms;
- primary herpes, as well as relapsing manifestations of it, in which there is damage to the skin and mucous membranes caused by Herpes simplex types 1 and 2 in patients with low immunity;
- herpes zoster (Varicella zoster virus);
- herpes zoster, in which eye damage occurs.
Inside, the use of the medicine “Acyclovir” is indicated for the prevention of frequent relapses of genital herpes, as well as herpes zoster and herpes simplex (Varicella zoster virus), in case of impaired immune functions. Parenteral this drug is prescribed for the treatment of encephalitis (two types of Herpes simplex virus), in the treatment of generalized infections in infants (Herpes simplex). In the treatment of chickenpox, the drug is taken orally or administered parenterally during the first days after the appearance of a typical rash in case of immune disorders.
Side effects of the Acyclovir tablets, as well as other forms of release, develop especially often if the existing contraindications are not observed.
List of contraindications
The use of all dosage forms of the drug "Acyclovir" is contraindicated in the presence of high sensitivity to the components of its composition. Absolute contraindications for taking tablets are:
- lactose intolerance;
- lack of lactase;
- glucose or galactose malabsorption;
- age less than 3 years;
- lactation.
Relative contraindications:
- neurological reactions to the use of cytotoxic pharmacological agents (including in the presence of a burdened history);
- impaired renal function;
- large dosages, especially against the background of severe dehydration;
- pregnancy period;
- elderly age.
In the form of relative contraindications for ointment and cream for topical use, pregnancy, lactation. The medication in this case is used strictly under the supervision of a doctor.
It is better to familiarize yourself with Acyclovir contraindications and side effects in advance.
For eye ointment, an absolute contraindication to use is the period of breastfeeding. During pregnancy, eye ointment can be used only on the advice of a doctor and under his supervision.
For the infusion solution, the main contraindication is lactation, the list of relative restrictions includes:
- dehydration of the body;
- kidney or liver failure;
- neurological disorders;
- complex forms of hypoxia;
- electrolyte disturbances;
- reactions to the use of cytotoxic medicines (including a medical history);
- combination therapy with medications that can impair renal function, in particular, with tacrolimus, cyclosporine (kidney function monitoring is necessary);
- complex treatment with mycophenolate mofetil (immunosuppressive drug used in organ transplantation);
- period of pregnancy.
To avoid side effects from "Acyclovir" in children and adults, it is important to strictly follow the instructions.
Instructions for use
Adults in the treatment of relapses and primary infections of Herpes simplex mucous membranes and skin are prescribed 1 tablet 5 times a day - 5 days. Longer treatment may be necessary in severe cases of the disease. With weakened immunity, intravenous administration of this drug or a 2-fold increase in dosage is possible. To suppress relapse with the proper functioning of the body's immune defense, 1 tablet is prescribed 4 times a day.
Topically, Acyclovir cream and ointment are applied to the affected areas with clean hands or with a cotton swab in a thin layer 5 times a day. Treatment should be continued until crusts form on the vesicles or until they completely heal. The duration of therapy is up to 10 days. Eye ointment is placed in a small amount under the lower eyelid in the conjunctival sac in the form of a strip. The procedure is carried out 5 times a day until absolute healing, then treatment should be continued for another 2-3 days.
Drip intravenously to patients after 12 years of age is usually prescribed at 5-10 mg / kg with an interval of 8 hours. For children from 3 months to 12 years, the dose is calculated taking into account the surface area of the skin - 250 mg / m2, for newborn babies - 10 mg / kg.
Side effects of Acyclovir
A medication in any dosage form can cause such negative reactions:
- Allergic skin rashes.
- Anaphylactic reactions.
- Increased activity of liver enzymes.
- Confusion.
- The development of hallucinations.
- Fever.
- Lymphadenopathy
- Cephalgia
- Leukopenia
- Peripheral edema.
- Visual impairment.
If any of the symptoms occur, you must immediately stop taking the drug.
With parenteral administration of this pharmacological agent, the following may occur:
- Phlebitis.
- Acute renal failure.
- Signs of encephalopathy.
- Hematuria
- Hematologic disorders.
- Hemolysis.
- Lowering blood pressure.
- DIC syndrome.
- Mental disorders.
- Psychosis or depression.
- Digestive dysfunction.
If negative reactions are ignored, the consequences can be very serious. It is better to consult a doctor immediately.
Side effects of Acyclovir tablets:
- Malaise.
- Paresthesia.
- Digestive disorders.
- Alopecia.
- Agitation.
- Dizziness, cephalalgia.
- Drowsiness, myalgia.
Of course, the likelihood of manifestations of such reactions depends on the individual characteristics of the body. It is very important to follow the instructions, then the risk of their development will be minimal.
Side effects of Acyclovir ointment are extremely rare.
Overdose Signs
The most common signs of overdose are: agitation, coma, seizures, lethargy. If the concentration of the basic substance is higher than the solubility in the renal tubules, its precipitation may be noted. With the development of side effects from Acyclovir, symptomatic treatment is prescribed. With an overdose of an infusion solution, an increase in the concentration of creatinine, urea and blood nitrogen, the occurrence of renal failure. Neurological symptoms are agitation, confusion, hallucinations, convulsions, and coma. In this case, hemodialysis is prescribed.
Special recommendations
Long-term use of the drug "Acyclovir" or a second course in patients with reduced immunity can provoke the emergence of strains of viruses that do not show sensitivity to the effects of the drug. With oral administration of the drug in large doses, it is necessary to monitor the flow of fluid into the body. The use of the drug does not prevent the transmission of the herpes pathogen through sexual contact, therefore, during therapy, you should refrain from sexual contact, even if there are no clinical manifestations of the pathology.
During the period of use of this medication inside in tablet form, it is recommended that patients be careful when driving vehicles. The solution for infusion is intended only for use in stationary conditions.
During pregnancy and lactation
During pregnancy and lactation, therapy can be carried out under medical supervision. In the form of tablets, ophthalmic ointment and infusion solution, the medication is contraindicated. In other forms (ointment and cream) - under the supervision of a specialist.
Use in children
In childhood, the pharmacological drug "Acyclovir" in the form of tablets up to three years is not prescribed. Side effects of "Acyclovir" in a child can manifest itself brighter than in adults.
Drug interaction
With the combined use of probenecid, the average half-life increases and the clearance of the drug decreases. During administration with nephrotoxic drugs, the risk of developing renal function impairment increases, with immunostimulants, the effect of acyclovir is enhanced. When mixing solutions, the alkaline reaction of the main active element should be taken into account.
Side effects of Acyclovir Akrikhin are the same.
Analogs
The main analogues of the drug Acyclovir for the active substance are the following drugs:
- Herperx.
- Vivorax.
- "Acyclostad."
- "Virolex".
- "Sagged."
Analogs for the mechanism of therapeutic action are:
- Rebetol.
- "Ribavirin."
- "Valcite".
- "Trivorin."
- "Virazole."
- Arviron.
- Valtrex
- "Valacyclovir."
- "Vatsireks".
- "Valogard."
- "Ribavin."
- "Vairova."
- "Famvir."
- Medovir.
- Zovirax.
- "Minaker."
- "Ribapeg."
- Valvir
Reviews on the side effects of Acyclovir
Most reviews about this drug are positive. It is considered inexpensive, effective and affordable. The speed of the therapeutic effect of an ointment (cream) for external use is characterized in different ways. Some patients say that improvement comes quickly, other people indicate that relief does not occur immediately and note that the use of this medication can lead to the development of some side effects (edema, dermatosis). In addition, there are negative reviews regarding the bitter taste and consistency of the ointment. According to reviews of the Acyclovir tablets, side effects provoke more often than other forms of release.
They are used, as a rule, in cases where it was not possible to eliminate the pathological signs of herpes with the help of external means. Patients note that the best results were achieved when using the drug with the appearance of the first signs of the disease. The main advantages of the drug in the form of ointments for the eyes are its effectiveness, convenient packaging and reasonable cost. The disadvantages of patients include a small volume of tube.
The most effective drug is Acyclovir in the form of solutions for intravenous administration, however, this dosage form has many contraindications and a large number of adverse reactions. However, patients note that after administration, the condition improves rapidly, the symptoms of the disease begin to disappear.
In general, there are few reviews of the side effects of Acyclovir. The most common were headache, nausea, indigestion, and diarrhea.
Parents of children who were treated with the drug note that the remedy was excellent in the treatment of herpes, in most cases there were no negative effects. Children tolerated the medication well.
Price
The cost of a medical device is:
- tablets - 19-25 rubles or 160-220 rubles (depending on dosage);
- ointment 5% - 15-25 rubles;
- eye ointment 3% - 80-120 rubles;
- lyophilisate for infusion solution - 190 rubles.
We reviewed the instructions for the drug "Acyclovir", side effects and reviews. However, it is worth remembering that any use of drugs without a doctor's prescription is dangerous to health.