Each 100 g contains: Acyclovir (Aciclovir) 5 g (5% w/w).
Excipients/Inactive Ingredients: Dibasic sodium phosphate anhydrous, Cetomacrogol 1000, Crodacol-CS (Cetostearyl alcohol), White petrolatum, Liquid paraffin, Propylene glycol, Citric acid anhydrous and Propylene glycol/Diazolidinyl urea/Methylparaben/Propylparaben (Germaben II/Unigerm G-2).
Pharmacology: Acyclovir is an antiviral agent which is highly active in vitro against herpes simplex virus (HSV) types I and II and varicella zoster virus. Toxicity to mammalian host cells is low.
Acyclovir is phosphorylated after entry into herpes infected cells to the active compound Acyclovir triphosphate. The first step in this process is dependent on the presence of the HSV-coded thymidine kinase. Acyclovir triphosphate acts as an inhibitor of, and substrate for, the herpes-specified DNA polymerase, preventing further viral DNA synthesis without affecting normal cellular processes.
Pharmacokinetics: Pharmacology studies have shown only minimal systemic absorption of Acyclovir following repeated topical administration of Acyclovir cream.
Indicated for the treatment of Herpes Simplex virus infections of the skin including initial and recurrent genital herpes and herpes labialis.
Adults and Children: Acyclovir cream should be applied five times daily at approximately four hourly intervals, omitting the night time application.
Acyclovir cream should be applied to the lesions or impending lesions as soon as possible, preferably during the early stages (prodrome or erythema). Treatment can also be started during the later (papule or blister) stages.
Treatment should be continued for at least 4 days for herpes labialis and for 5 days for genital herpes. If healing has not occurred then treatment may be continued for up to an additional 5 days.
Use in the elderly: No special comment.
No untoward effects would be expected if the entire contents of a 5 gram tube of Acyclovir cream containing 250 mg of Acyclovir were ingested orally. However the accidental, repeated overdose of oral Acyclovir, over several days has resulted in gastrointestinal effects (nausea and vomiting) and neurological effects (headache and confusion). Acyclovir is dialyzable by hemodialysis.
Contraindicated in patients known to be hypersensitive to Acyclovir, Valaciclovir or any of the excipients.
Acyclovir cream is not recommended for application to mucous membranes such as in the mouth, eye or vagina, as it may be irritant.
Particular care should be taken to avoid accidental introduction into the eye.
In severely immunocompromised patients (e.g. AIDS patients or bone marrow transplant recipients) oral Acyclovir dosing should be considered. Such patients should be encouraged to consult a physician concerning the treatment of any infection.
Pregnancy: A post-marketing Acyclovir pregnancy registry has documented pregnancy outcomes in women exposed to any formulation of Acyclovir. The registry findings have not shown an increase in the number of birth defects amongst Acyclovir exposed subjects compared with the general population, and any birth defects showed no uniqueness or consistent pattern to suggest a common cause. Systemic administration of Acyclovir in internationally accepted standard tests did not produce embryotoxic or teratogenic effects in rabbits, rats or mice.
In a non-standard test in rats, fetal abnormalities were observed but only following such high subcutaneous doses that maternal toxicity was produced. The clinical relevance of these findings is uncertain.
The use of Acyclovir cream should be considered only when the potential benefits outweigh the possibility of unknown risks however the systemic exposure to Acyclovir from topical application of Acyclovir cream is very low.
Teratogenicity: Effects in non-clinical studies were observed only at exposures considered sufficiently in excess of the maximum human exposure to indicate little relevance to clinical use.
Breastfeeding: Limited human data show that the drug does pass into breast milk following systemic administration. However, the dosage received by a nursing infant following maternal use of Acyclovir cream would be insignificant.
Fertility: There is no information on the effect of Acyclovir on human female fertility.
In a study of 20 male patients with normal sperm count, oral Acyclovir administered at doses of up to 1 g per day for up to six months has been shown to have no clinically significant effect on sperm count, motility or morphology.
The following convention has been used for the classification of undesirable effects in terms of frequency: very common ≥1/10, common ≥1/100 and <1/10, uncommon ≥1/1000 and <1/100, rare ≥1/10,000 and <1/1000, very rare <1/10,000.
Immune system disorders:
Very rare: Immediate hypersensitivity reactions including angioedema and urticaria.
Skin and subcutaneous tissue disorders:
Uncommon: Transient burning or stinging following application of Acyclovir cream; Mild drying or flaking of the skin; Itching.
Rare: Erythema; Contact dermatitis following application. Where sensitivity tests have been conducted, the reactive substances have most often been shown to be components of the cream rather than Acyclovir.
No clinically significant interactions have been identified.
Store at temperature not more than 30°C.
D06BB03 - aciclovir ; Belongs to the class of topical antivirals used in the treatment of dermatological diseases.
Cream 5 g (5% w/w) x 5 g.