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The Latin name of the substance Aciclovir
Aciclovir
Chemical name
2-Amino-1 ,9-dihydro-9-[(2-hydroxyethoxy) methyl]-6H-purine-6-one (and as sodium salt)
Gross formula
C8H11N5O3
Pharmacotherapeutic group substances Acyclovir
Antivirals (excluding HIV) means
Nosological classification (ICD-10)
A60 Anogenital herpes viral infection [herpes simplex]
B00 Infections caused by herpes simplex virus [herpes simplex]
B00.5 Herpetic eye disease
B01 Varicella [varicella]
B02 Shingles [herpes zoster]
Code CAS
59277-89-3
Characteristics of substance Aciclovir
Acyclovir - a white crystalline powder with a maximum solubility in water (at 37 ° C) 2,5 mg / ml, the molecular weight of 225.21. Acyclovir sodium salt - the maximum solubility in water (at 25 ° C) higher than 100 mg / ml, molecular weight 247.19; prepared solution (50 mg / ml) has a pH of about 11.
Pharmacology
Pharmacological action - an antiviral, antiherpethetical. Is a synthetic analogue of purine nucleosides. After entering the infected cells containing a viral thymidine kinase, acyclovir is phosphorylated and converted into acyclovir monophosphate, which is under the influence of cell guanilatkinazy converted into diphosphate, and then under the action of several cell enzymes - a triphosphate. Acyclovir triphosphate interacts with the viral DNA polymerase, included in the chain of viral DNA, causing chain termination and blocks further replication of viral DNA without damaging the host cells.
Acyclovir inhibits the in vitro and in vivo replication of human herpes viruses, including the following (listed in order of antiviral activity of acyclovir in cell culture): Herpes simplex virus types 1 and 2, the virus Varicella zoster, Epstein-Barr virus and CMV.
With prolonged treatment or re-use of acyclovir in patients with severe immunodeficiency viruses develop resistance Herpes simplex and Varicella zoster to acyclovir. In most clinical isolates derived from acyclovir-resistant patients, found a relative deficiency virus thymidine kinase, or disturbance of viral thymidine kinase or DNA polymerase.
Herpes prevents the formation of new elements rashes, reduces the likelihood of cutaneous dissemination and visceral complications, speeds up the formation of crusts and reduces pain in the acute phase of herpes zoster. Exerts immunostimulatory effects.
Pharmacokinetics
If ingestion is partially absorbed from the gastrointestinal tract, bioavailability - 20% (15-30%) does not depend on the dosage form decreases with increasing dose, the food has no significant effect on the absorption of acyclovir. After ingestion of 200 mg of acyclovir every 4 hours for adults mean equilibrium value Cmax - 0,7 mg / ml and Cmin - 0,4 mg / ml; Tmax - 1,5-2 hours
After IV drip of adult average C max at 1 h after infusion at a dose of 2.5, 5 and 10 mg / kg were 5.1, 9.8 and 20.7 ug / ml, respectively. Smin after 7 h after infusion, respectively, were equal to 0.5, 0.7 and 2.3 mg / ml. In children older than 1 year and Cmax values of Smin at a dose of 250 and 500 mg / m 2 were similar to those in adults at doses of 5 and 10 mg / kg, respectively. In newborns and infants up to 3 months, which acyclovir was administered at a dose of 10 mg / kg in infusion over 1 h every 8 h, Cmax was 13.8 micrograms / ml), Cmin - 2,3 mg / ml.
Protein binding is low (9-33%). Passes through the blood-brain barrier, placental barrier, detected in breast milk (at a dose of 1 g / day inside the mother's milk to the baby arrives 0,3 mg / kg). Well into the organs, tissues and body fluids, including the brain, kidneys, liver, lungs, aqueous humor, tear fluid, intestine, muscle, spleen, uterus, mucosa and the secret of the vagina, semen, cerebrospinal fluid, the contents of herpetic vesicles . The highest concentrations detected in kidney, liver and intestine. Concentration in the cerebrospinal fluid is 50% of that in blood plasma. Metabolized in the liver under the influence of alcohol and aldehyde dehydrogenase and to a lesser extent, aldehyde oxidase to inactive metabolites. Metabolism of acyclovir is not associated with cytochrome P450.
The main path of elimination - the kidneys by glomerular filtration and tubular secretion. When administered in unchanged output by about 14%, at / in the introduction - 45-79%. The main metabolite found in urine - 9-карбоксиметоксиметилгуанин. The share of the main metabolite responsible for up to 14% (with normal renal function). Less than 2% excreted in the feces, trace amounts are determined in the exhaled air.
T1 / 2 by ingestion in adults - 2,5-3,3 hours T1 / 2 at / in the introduction: adults - 2.9 hours in children and adolescents from 1 year to 18 years - 2,6 h in children aged 3 months - 3.8 hours (when administered IV drip of 10 mg / kg over 1 h, 3 times a day). In patients with chronic renal insufficiency T1 / 2 - 19.5 hours, during hemodialysis - 5,7 h, with continuous ambulatory peritoneal dialysis - 14-18 h. In a single session of hemodialysis for 6 h the concentration of acyclovir in plasma is reduced by 60% in peritoneal dialysis clearance of acyclovir did not significantly change.
When applied to damaged skin (such as herpes zoster), a moderate intake, patients with normal renal function, serum concentrations of up to 0.28 mg / ml, with impaired renal function - up to 0.78 mg / ml. Excreted by the kidneys (approximately 9% of daily dose).
Eye ointment can easily penetrate through the epithelium of the cornea and creates a therapeutic concentration in ocular fluid.
Carcinogenicity, mutagenicity, effects on fertility, teratogenicity
In rats and mice treated during the life of acyclovir at doses of 450 mg / kg / day by gavage (the Cmax values were higher than observed in humans in 3-6 times in mice and 1-2 fold in rats), carcinogenic actions were detected.
Acyclovir showed mutagenic effects in some tests: from 16 in vivo and in vitro tests for genetic toxicity of acyclovir results of 5 tests were positive.
Acyclovir had no effect on fertility and reproduction in mice when administered orally at doses of 450 mg / kg / day in rats after subcutaneous administration at a dose of 50 mg / kg / day, while plasma levels were 9-18 times higher ( mice) or 8-15 times (in rats) than in humans. At the highest dose (50 mg / kg / day sc) in rats and rabbits (plasma levels were 11-22 or 16-31 such a person) is set to reduce the effectiveness of implantation.
Teratogenicity. Acyclovir had no teratogenic effects when administered during organogenesis mice (450 mg / kg / day, orally), rabbits (50 mg / kg / day, sc and IV), as well as in the standard test in rats (50 mg / kg / d, n / k).
Carcinogenicity studies of acyclovir in the external application was not performed.
In humans, disruption of spermatogenesis, motility, or sperm morphology were not registered. However, high doses of acyclovir - 80 or 320 mg / kg / day intraperitoneally in rats, as well as 100 or 200 mg / kg / day / to the dogs - causes atrophy of the testes and aspermatogenez. Testicular disorders were not observed at iv administration of acyclovir to dogs at doses of 50 mg / kg / day for 1 month or 60 mg / kg / day orally for 1 year.
Application of the substance Aciclovir
For systemic use: primary and recurrent infections of the skin and mucous membranes caused by the herpes simplex virus (types 1 and 2), including genital herpes, herpes lesions in patients with immunodeficiencies (treatment and prevention); shingles, chicken pox.
For external use: Herpes Simplex skin and mucous membranes, genital herpes (primary and recurrent) localized zoster (adjuvant treatment).
For local use in ophthalmology: herpetic keratitis.
Contraindications
Hypersensitivity to acyclovir or valacyclovir.
Restrictions apply
With / in the introduction: dehydration, renal insufficiency (risk of nephrotoxicity), neurological disorders, or neurological reactions to receiving cytotoxic drugs, including history.
Ingestion: dehydration, kidney failure.
Application of pregnancy and breastfeeding
Pregnancy. Perhaps, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of safety in pregnant women has not conducted). Acyclovir passes through the placenta. Data on the outcome of pregnancy in women taking acyclovir systemic action in the I trimester of pregnancy showed no increase in congenital malformations in children compared with the general population. Since the observation was included few women, reliable and definitive conclusions about the safety of acyclovir in pregnancy can be done.
Breast-feeding. Acyclovir passes into breast milk. After receiving acyclovir by mouth, it was determined in breast milk in concentrations, the ratio of which with concentrations in blood plasma was 0,6-1,4. At these concentrations in breast milk of children who are breastfed may receive acyclovir at a dose of 0.3 mg / kg / day. Given this, should be administered acyclovir lactating women with caution, only when necessary.
Side effects of substance Aciclovir
In system use:
From the digestive tract: with / in the introduction - anorexia, nausea and / or vomiting if swallowed - nausea and / or vomiting, diarrhea, abdominal pain.
The nervous system: at / in the introduction - dizziness, symptoms of encephalopathy (confusion, hallucinations, convulsions, tremors, coma), delirium, depression or psychosis (neurological disorders are commonly observed in patients with predisposing conditions); ingestion - malaise, headache, dizziness, agitation, drowsiness.
With the cardiovascular system and blood: at / in the introduction - anemia, neutropenia / neutrophilia, thrombocytopenia / thrombocytosis, leukocytosis, hematuria, DIC, hemolysis, decreased blood pressure.
From the urogenital system: at / in the introduction - a transient increase in blood urea nitrogen and serum creatinine levels (due to the magnitude of Cmax in the plasma and the state of the water balance of the patient), acute renal failure (often during rapid intravenous injection) .
Other: anaphylactic reactions, allergic skin reactions (itching, rash, Lyell syndrome, urticaria, erythema multiforme, and others), visual disturbances, fever, leukopenia, lymphadenopathy, peripheral edema, transient elevation of liver transaminases and bilirubin levels, with I / O Introduction - site reactions to intravenous injection: local phlebitis, or inflammation (pain, swelling or redness), necrosis (in contact with the drug under the skin), ingestion - myalgia, paresthesia, alopecia.
For external use: pain, burning, itching, skin rash, vulvitis.
When applying eye ointment: burning at the site of application, blepharitis, conjunctivitis, superficial keratopathy point.
Interaction
Other nephrotoxic drugs increase the risk of nephrotoxicity. In an application with probenecid (blocks tubular secretion) increased T1 / 2 and AUC of acyclovir, reduced renal clearance and slow excretion, may increase the toxic effect.
Overdose
Symptoms: headache, neurological disorders, shortness of breath, nausea, vomiting, diarrhea, kidney failure, lethargy, convulsions, coma.
Treatment: symptomatic therapy, the maintenance of vital functions, adequate hydration, hemodialysis (especially in acute renal failure and anuria).
No evidence of an overdose when applied topically.

 

 
 

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