INSTRUCTION SHEET on Medical Application of the Preparation of Acyclovir

Registration number: Trade name of the medication: Acyclovir International nonproprietary name: Acyclovir Dosage form: oculentum Composition: 1 gram of the preparation contains: Active substance: Acyclovir – 0.03 g; Auxiliary material: vaseline. Description: ointment of white or white with a yellowish tinge, or yellow color. Pharmacotherapeutic group: antiviral agent for local administration ATC code [S01AD03] Pharmacological action Pharmacodynamics Antiviral (antiherpetic) agent - synthetical analogue of nucleoside thymidine. Phosphorylation and turning into acyclovir hydrophosphate takes place in infected cells containing vi- ral thymidine kinase. Acyclovir hydrophosphate under the influence of guanylate cyclase converts into diphosphate and under the influence of several cellular enzymes it turns into triphosphate. High selec- tiveness of activity and low toxicity for human beings are conditioned by absence of a necessary en- zyme for formation of acyclovir triphosphate in intact cells of macroorganism. Acyclovir triphosphate embedding into deoxyribonucleic acid (DNA) synthesized by the virus, blocks the virus replication. Specificity and extremely high action selectivity are also conditioned by its pre- dominant accumulation in the cells affected by herpesvirus. It is highly active against the virus of Herpes simplex types 1 and 2; the virus causing chicken pox and herpes zoster (Varicella zoster); Epstein-Barr virus (strains of viruses are specified in increasing order of magnitude of minimal inhibitory concentration of acyclovir). It is moderately active in regard to cy- tomegalovirus. In herpes prevents formation of new members of hives, decreases possibility of dermatic dissemination and viscerogenic complications, accelerates formation of scabs, decreases pain in the acute phase of herpes zoster. Pharmakokinetics Acyclovir easily works way through epithelial tissue of the keratoderma and produces therapeutic con- centration in the intraocular fluid. At the present time there are no measuring methods of acyclovir de- termination in blood in case of its application in the form of oculentum. Acyclovir in case of external application is determined only in urina at that in insignificant amount. This concentration does not have therapeutic implication.

Indications for application Herpes herpetic keratitis caused by viruse of Herpes simplex types 1 and 2.

Contra indications Hyperresponsiveness to acyclovir or valaciclovir. Period of breast feeding.

Application in pregnancy and lactation Application of the medication in pregnancy is possible provided that the potential usefulness for the mother exceeds possible risk for the fetus. The medication is found in human milk after entry in the mother’s system blood flow, therefore for the period of medical treatment the breast feeding should be ceased.

1 Mode of administration and dosages Topically. The oculentum for adults and children is put in the form of strip of the length of 1 cm. into a lower conjunctival sac 5 times a day (every 4 hours) until adhesion. The treatment should be continued with- in 3 more days after adhesion.

Side effects Adverse events are presented in accordance with frequency of occurrence in the course of clinical studies: very often – more than 10 %; often – more than 1 % and less than 10 %; unoften –more than 0.1 % and less than 1 %; seldom – more than 0.01 % and less than 0.1 %; very seldom – less than 0.01 %. Allergic reactions: very seldom – reactions of hyperresponsiveness of immediate type (including acute circumscribed edema). On the part of the visual organ: unoften - punctate surface keratopathy (it does not demand treatment cessation and disappears without consequences); often - easy burning (it disappears go in course of time); unoften - conjunctivitis; seldom - blepharitis.

Overdosage Overdosage is possible in casual ingestion. Symptoms: headache, neurological disorders, labored breathing, nausea, vomiting, diarrhea, kidney malfunction, lethargy, convulsions, coma. Medical treatment: Basic Life Support, haemodialysis.

Interaction with other medicinal preparations. Application together with immunopotentiators strengthens effect of acyclovir.

Special instructions The efference of treatment is higher the earlier it is set up (at the first signs of infection). Within the period of medical treatment by acyclovir oculentum it is not recommended to wear contact lens. Condition of immune system of the organism possesses a value for implementation of curative effect of acyclovir. The system injection of the medication should be prescribed against the back- ground of topical application of the acyclovir ointment to the patients with reduced immune resistance as well as in case of severe and recrudescent run of herpetic infection. After application of the prepara- tion temporary lowering of the precision of visual perception is possible, and until its restoration it is not recommended to drive motor vehicles and be engaged in kinds of activity requiring increased at- tention and reaction.

Product form Ophthalmic ointment 3% 5 grams in aluminum tubes. Every tube has an instruction sheet on medical application and put in a carton pack.

Expiration date 3 years. The oculentum should be used in the course of a month after opening of the tube. The prepara- tion should not be used after expiration date indicated on the pack.

Storage conditions Store at temperature from 15° up to 25°C. Keep out of reach of children.

Pharmacy purchasing terms Without prescription.

2 Manufacturer/organization that accepts claims: Open Joint Stock “Kurgan Joint Stock Company of Medical Preparations and Articles “Sintez” (Sintez Joint Stock Company); #7, Prospect Konstitutsii, city of Kurgan, Russian Federation, 640008; Tel. /fax: (3522)481689 Internet-site: http://www.kurgansintez.ru

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