Pharmaniaga Aciclovir tablet 200 mg
Shield-shaped yellow tablet.
Aciclovir tablet 400 mg
Shield-shaped pink tablet.
Each tablet contains Aciclovir 200 mg or 400 mg.
Aciclovir is converted to aciclovir monophosphate, a nucleotide, by the
viral thymidine kinase of herpes simplex virus (HSV) and varicella-zoster
virus (VZV). Aciclovir monophosphate is converted to the diphosphate by
cellular guanylate kinase and to the triphosphate by a number of cellular
enzymes. Aciclovir triphosphate interferes with HSV and VZV DNA polymerase
and inhibits viral DNA replication. The triphosphate can be incorporated
into growing chains of DNA by viral DNA polymerase, resulting in termination
of the DNA chain.
Absorption: Bioavailability 20 % (range, 15 to 30 %). Poorly absorbed from
the gastrointestinal tract. Not significantly affected by food.
Distribution: Widely distributed to tissues and body fluids, including
brain, kidneys, lungs, liver, aqueous
humor, tears, intestines, muscle, spleen, breast milk, uterus, vaginal
mucosa, vaginal secretions, semen, amniotic fluid, cerebrospinal fluid (CSF)
and herpetic vesicular fluid. Highest concentrations are found in kidneys,
liver, and intestines. CSF concentrations are approximately 50% of plasma
concentrations. Crosses the placenta, also.
Adults: Approximately 48 litres (L) per square meter of body surface (m2)
(range, 37 to 57 L per m2).
Children and adolescents (1 to 18 years old): Approximately 45 L per m2.
Neonates (0 to 3 month old): Approximately 28 L per m2 (range, 24 to 30 L
End stage renal disease: Approximately 41 L per m2.
Protein binding: Low (9
Biotransformation: Hepatic, only major metabolites found in urine is
9-carboxymethoxymethylguanine, which accounts for approximately 9 to 14% of
the dose. This metabolite has no known antiviral activity.
Half-life: Oral - 3.3 hours.
Time to peak serum concentration: Oral - 1.7 hours.
ambulatory peritoneal dialysis
Renal : Excreted by both glomerular filtration and
Oral : Approximately 14% of total dose excreted
unchanged in urine.
Faecal : Insignificant amounts (< 2%).
Lungs : Trace amounts in exhaled CO2.
Dialysis : Haemodialysis : A single 6-hour period of
haemodialysis reduces plasma aciclovir
concentration by approximately 60%.
Peritoneal dialysis: Peritoneal dialysis does not substantially alter aciclovir clearance.
Treatment and prophylaxis of herpes genitalis, treatment of herpes zoster,
herpes simplex and varicella (chicken-pox).
Aciclovir is contraindicated in patients who have developed hypersensitivity
or intolerance to the drug.
General : fever, headache, pain, peripheral oedema, and rarely anaphylaxis.
Nervous : confusion, dizziness, hallucinations, paraesthesia, somnolence
(These symptoms may be marked, particularly in older adults). Digestive : diarrhoea, elevated liver function test, gastrointestinal distress, nausea.
Haemic and Lymphatic : leucopenia, lymphadenophathy.
Musculoskeletal : myalgia.
Skin : alopecia, pruritus, rash, urticaria.
Special Senses : visual
Urogenital : elevated creatinine.
Acute renal insufficiency may occur due to precipitation of aciclovir in the
renal tubules. It is most likely to occur if aciclovir is given by rapid
intravenous injection, concurrently with known nephrotoxic medications, to
patients who are inadequately hydrated, or to patients with renal function
impairment without appropriate dosage reduction. However, acute renal
failure has also been reported in patients receiving oral aciclovir.
Neuropsychiatric toxicity has been associated with high plasma aciclovir
concentrations, which may occur when high doses are used, or when patients
with renal function impairment are not given an appropriately lowered dose.
Neuropsychiatric toxicity may also be more likely to occur in
immunocompromised patients and geriatric patients.
Pregnancy / Reproduction
Fertility - Impairment of spermatogenesis, sperm motility, or morphology has
not been documented in humans. However, high doses of parenteral aciclovir
have caused testicular atrophy in rats and dogs. Some evidence of sperm
production recovery was evident 30 days post-dose. Studies in mice given
oral doses up to 450 mg/kg per day have shown that aciclovir does not impair
fertility or reproduction. Studies in female rabbits given aciclovir
subcutaneously subsequent to mating have shown a significant decrease in
implantation efficiency, but no decrease in litter size at doses of 50 mg/kg