In the article we will consider the side effects of “Acyclovir”, and also tell you what kind of medicine and what it is used for.
Pharmacological drug is an antiviral agent used in the treatment of herpes infection. The drug is used in the treatment of patients of any age categories. The success of treatment depends on the stage of the disease, the characteristics of the pathological process and individual characteristics.
The list of likely side effects in “Acyclovir” tablets is impressive. But negative reactions can cause other forms of release.
Composition and release form
This medicine 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 each.
- Eye ointment 3% – available in aluminum tubes, packaging for 5 g.
- Lyophilisate for the manufacture of solutions for intravenous infusions – produced in bottles of 500 mg and 250 mg.
- Tablets for oral use – 400 mg and 200 mg and 100 mg – blisters of 10 tablets.
The active element of this drug 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 ointment for eyes – 30 mg;
- 1 tablet – 200 mg.
About side effects of “Acyclovir” information can be clarified in the instructions.
The drug is an antiviral medicine for parenteral, oral, topical and topical use, and is a synthetic substance identical to an acyclic purine nucleoside. This drug has a greater specificity for viral agents Herpes simplex (type 1 and type 2), Epstein-Barr virus, cytomegalovirus and Varicella zoster. The greatest activity of the active element is observed to HSV-1, then in descending order – to HSV-2, VZV, EBV and CMV. The principle 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 acyclovir triphosphate is that it is a substrate for this enzyme, which allows 3’– 5 ‘to be linked. It is necessary to extend the chain of DNA. As a consequence, there is a premature break of the DNA chain.
Side effects from “Acyclovir” in both adults and children can develop equally often.
The medicine “Acyclovir” in pill form after administration is orally absorbed in the intestine only partially. After five times daily use of 200 mg, the highest and minimum concentration of a substance in the body is 0.8 and 0.5 μg / ml, respectively. The composition of the cerebrospinal fluid level of acyclovir reaches 50% of plasma. The drug is relatively low bound to plasma proteins (9–34%) and is excreted mainly by the kidneys in unchanged form.
When externally applied ointment on the intact skin, the main substance has a minimum absorption, in the composition of urine and blood is not determined. In the case of its use on the affected skin 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 insufficiency, this figure rises to 0.78 µg / ml. Isolation from the body by the kidneys.
The medicine “Acyclovir” in the form of an ophthalmic ointment easily penetrates the corneal epithelium, providing a therapeutic level in the intraocular fluid. There is no way to determine the substance in the blood when using this dosage form.
The equilibrium maximum concentration of an acyclovir infusion solution after administration for an hour at a dose of 2.5; five; 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 in the indicated dosages are 0.6; 0.8; 2.4 and 2.1 μg / ml, respectively. After intravenous infusion in adults, the half-life is approximately 2.9 hours. The main part of the active substance is excreted by the kidneys. Its main metabolite is considered 9-carboxymethoxymethylguanine.
Indications for use of the drug
According to the annotations to use, the medical drug “Acyclovir” is administered orally and parenterally in the treatment of the following pathological conditions:
- recurrent forms or genital herpes of the primary type, which proceeds with severe symptoms;
- primary herpes, as well as recurrent manifestations of it, in which there is damage to the skin and mucous membranes caused by Herpes simplex type 1 and 2, in patients with low immunity;
- herpes zoster (Varicella zoster virus);
- herpes zoster, in which there is damage to the eyes.
Internally, the use of the drug “Acyclovir” is indicated for the prevention of frequent recurrences of genital herpes, as well as herpes zoster and herpes simplex (Varicella zoster virus), in cases of impaired immune functions. Parenterally, this drug is prescribed for the treatment of encephalitis (Herpes simplex virus of two types), in the treatment of generalized infection in infants (Herpes simplex). In the treatment of chickenpox during the first days after the occurrence of a typical rash with immunity disorders, the medicine is taken orally or administered parenterally.
Side effects of tablets “Acyclovir”, as well as other forms of release develop especially often, if you do not observe the existing contraindications to receive.
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 pills are:
- lactose intolerance;
- lack of lactase;
- glucose or galactose malabsorption;
- age less than 3 years;
- neurological reactions to the use of cytotoxic pharmacological agents (including in the presence of burdened anamnesis);
- impaired renal function;
- large dosages, especially against the background of severe dehydration;
- gestation period;
- elderly age.
In the form of relative contraindications for ointments and creams for topical use are pregnancy, lactation. The drug in this case is used strictly under the supervision of a physician.
It is better to get acquainted with contraindications of “Acyclovir” and side effects in advance.
For eye ointment, an absolute contraindication to use is breastfeeding. During pregnancy, ointment for the eyes can be applied only on the recommendation of a doctor and under his supervision.
For an infusion solution, lactation is the main contraindication, the list of relative restrictions includes:
- kidney or liver failure;
- neurological disorders;
- complex forms of hypoxia;
- electrolyte disturbances;
- reactions to the use of cytotoxic medical devices (including history);
- combination therapy with drugs that can impair the function of the kidneys, in particular, with tacrolimus, cyclosporine (control of renal function is necessary);
- complex treatment with mycophenolate mofetil (an immunosuppressive drug used for organ transplantation);
- gestation period.
To avoid side effects from “Acyclovir” in children and adults, it is important to strictly follow the instructions.
Instructions for use
Adults with the treatment of relapses and primary infections Herpes simplex mucous membranes and skin assigned 1 tablet 5 times a day – 5 days. Longer treatment may be necessary for severe illness. When immunity is weakened, intravenous administration of this drug or a 2-fold increase in dosage is possible. To suppress recurrence with the proper functioning of the body’s immune defense, 1 tablet is prescribed 4 times a day.
Externally, the cream and ointment “Acyclovir” are applied to the affected areas with clean hands or with a cotton swab with a thin layer 5 times a day. Treatment must be continued until the formation of crusts on the vesicles or until their complete healing. The duration of therapy is up to 10 days. Eye ointment is laid in a small amount under the lower eyelid in the conjunctival sac in the form of a strip. The procedure is performed 5 times a day until absolute healing, then the treatment should be continued for another 2-3 days.
Intravenous drip in patients after 12 years 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
The drug in any dosage form can cause such negative reactions:
- Allergic skin rash.
- Anaphylactic reactions.
- Increased liver enzymes.
- Confusion of consciousness.
- The development of hallucinations.
- Feverish condition.
- Peripheral edema.
- Violations of visual functions.
If any of the symptoms occur, you should immediately stop taking the drug.
When parenteral administration of this pharmacological agent may occur:
- Acute renal failure.
- Signs of encephalopathy.
- Hematological disorders.
- Lowering blood pressure.
- DIC syndrome.
- Mental disorders.
- Psychosis or depression.
- Violation of digestive functions.
If negative reactions are ignored, the consequences can be very serious. It is better to consult a doctor immediately.
Side effects of Acyclovir tablets:
- Disorders of digestion.
- Dizziness, cephalgia.
- Drowsiness, myalgia.
Of course, the probability of manifestations of such reactions depends on the individual characteristics of the organism. 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.
Signs of overdose
The most common signs of overdose are: agitation, coma, the occurrence of seizures, lethargy. If the concentration of the main substance is higher than the solubility in the renal tubules, its precipitation may occur. With the development of side effects from Acyclovir, symptomatic treatment is prescribed. In case of overdose with an infusion solution, there is an increase in the concentration of creatinine, urea and nitrogen in the blood, the occurrence of renal failure. Neurological symptoms are agitation, confusion, hallucinations, convulsions, and coma. In this case, hemodialysis is prescribed.
Prolonged use of the drug “Acyclovir” or a repeated course in patients with reduced immunity can provoke the occurrence 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 it is necessary to refrain from sexual contact, even if there are no clinical manifestations of the pathology.
In the period of use of this medical device orally in pill form when driving a car, patients are advised to use caution. Infusion solution is intended for stationary use only.
During pregnancy and lactation
During pregnancy and lactation therapy may be carried out under medical supervision. In the form of tablets, eye ointment and infusion solution, the drug 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 may appear brighter than in adults.
When combined, the probenecid increases the average half-life and decreases the clearance of the drug. When taken with nephrotoxic drugs, the risk of developing impaired renal function increases, while immunostimulants increase the effect of acyclovir. When mixing solutions should take into account the alkaline reaction of the main active element.
The side effects of Akyclovir Akrikhin are the same.
The main analogues of the drug drug “Acyclovir” on the active substance are the following drugs:
Analogues on the mechanism of therapeutic action are:
Reviews of side effects of “Acyclovir”
Most reviews of this drug are positive. It is considered inexpensive, effective and affordable. The rapidity of the therapeutic effect of the ointment (cream) for external use is characterized differently. Some patients say that improvement occurs quickly, other people indicate that relief does not occur immediately and note that the use of this medication may 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 tablets “Acyclovir” side effects provoke more often than other forms of release.
They are applied, as a rule, in cases where it was not possible to eliminate the pathological signs of herpes with the help of external agents. 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 an ointment for the eyes are its effectiveness, convenient packaging and an acceptable cost. The disadvantages of patients include a small amount of tuba.
The most effective is the drug “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, reviews about the side effects of “Acyclovir” a bit. The most common were headache, nausea, indigestion, diarrhea.
Parents of children who have been treated with the drug, note that the remedy was excellent for the treatment of herpes, in most cases there were no negative effects. Children tolerated the drug well.
The cost of a medical product is:
- tablets – 19-25 rubles or 160-220 rubles (depending on the 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.