Acyclovir Oral Suspension
Name: Acyclovir Oral Suspension
Mechanism of Antiviral Action:
Acyclovir is a synthetic purine nucleoside analogue with in vitro and in vivo inhibitory activity against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV).
The inhibitory activity of acyclovir is highly selective due to its afﬁnity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme converts acyclovir into acyclovir monophosphate, a nucleotide analogue. The monophosphate is further converted into diphosphate by cellular guanylate kinase and into triphosphate by a number of cellular enzymes. In vitro, acyclovir triphosphate stops replication of herpes viral DNA. This is accomplished in 3 ways: 1) competitive inhibition of viral DNA polymerase, 2) incorporation into and termination of the growing viral DNA chain, and 3) inactivation of the viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared with VZV is due to its more efﬁcient phosphorylation by the viral TK.
The quantitative relationship between the in vitro susceptibility of herpes viruses to antivirals and the clinical response to therapy has not been established in humans, and virus sensitivity testing has not been standardized. Sensitivity testing results, expressed as the concentration of drug required to inhibit by 50% the growth of virus in cell culture (IC50), vary greatly depending upon a number of factors. Using plaque-reduction assays, the IC50 against herpes simplex virus isolates ranges from 0.02 to 13.5 mcg/mL for HSV-1 and from 0.01 to 9.9 mcg/mL for HSV-2. The IC50 for acyclovir against most laboratory strains and clinical isolates of VZV ranges from 0.12 to 10.8 mcg/mL. Acyclovir also demonstrates activity against the Oka vaccine strain of VZV with a mean IC50 of 1.35 mcg/mL.
Resistance of HSV and VZV to acyclovir can result from qualitative and quantitative changes in the viral TK and/or DNA polymerase. Clinical isolates of HSV and VZV with reduced susceptibility to acyclovir have been recovered from immunocompromised patients, especially with advanced HIV infection. While most of the acyclovir-resistant mutants isolated thus far from immunocompromised patients have been found to be TK-deﬁcient mutants, other mutants involving the viral TK gene (TK partial and TK altered) and DNA polymerase have been isolated. TK-negative mutants may cause severe disease in infants and immunocompromised adults. The possibility of viral resistance to acyclovir should be considered in patients who show poor clinical response during therapy.
Acyclovir Suspension is intended for oral ingestion only. Renal failure, in some cases resulting in death, has been observed with acyclovir therapy (see ADVERSE REACTIONS: Observed During Clinical Practice and OVERDOSAGE). Thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), which has resulted in death, has occurred in immunocompromised patients receiving acyclovir therapy.
Overdoses involving ingestion of up to 100 capsules (20 g) have been reported. Adverse events that have been reported in association with overdosage include agitation, coma, seizures, and lethargy. Precipitation of acyclovir in renal tubules may occur when the solubility (2.5 mg/mL) is exceeded in the intratubular ﬂuid. Overdosage has been reported following bolus injections or inappropriately high doses and in patients whose ﬂuid and electrolyte balance were not properly monitored. This has resulted in elevated BUN and serum creatinine and subsequent renal failure. In the event of acute renal failure and anuria, the patient may beneﬁt from hemodialysis until renal function is restored (see DOSAGE AND ADMINISTRATION).
Principal display panel
1 pint (473 mL)
Each 5 mL (1 teaspoonful) contains acyclovir 200 mg and (added as preservatives) methylparaben 0.1% and propylparaben 0.02%.
SHAKE WELL BEFORE USING.
See prescribing information for dosage information.
Store at 15° to 25°C (59° to 77°F).
Dispense in tight container as defined in the USP.
|Product Information |
|Product Type ||HUMAN PRESCRIPTION DRUG LABEL ||Item Code (Source) ||NDC:40085-842 |
|Route of Administration ||ORAL ||DEA Schedule || |
|Active Ingredient/Active Moiety |
|Ingredient Name ||Basis of Strength ||Strength |
|ACYCLOVIR (ACYCLOVIR) ||ACYCLOVIR ||200 mg in 5 mL |
|Inactive Ingredients |
|Ingredient Name ||Strength |
|METHYLPARABEN || |
|PROPYLPARABEN || |
|CARBOXYMETHYLCELLULOSE SODIUM || |
|GLYCERIN || |
|CELLULOSE, MICROCRYSTALLINE || |
|SORBITOL || |
|Product Characteristics |
|Color ||WHITE (off-white) ||Score || |
|Shape || ||Size || |
|Flavor ||BANANA ||Imprint Code || |
|Contains || |
|# ||Item Code ||Package Description |
|1 ||NDC:40085-842-96 ||473 mL in 1 BOTTLE |
|Marketing Information |
|Marketing Category ||Application Number or Monograph Citation ||Marketing Start Date ||Marketing End Date |
|NDA AUTHORIZED GENERIC ||NDA019909 ||09/03/2014 || |
|Labeler - Renaissance Pharma, Inc. (078290398) |
|Registrant - Denco Asset, LLC (965099505) |
|Name ||Address ||ID/FEI ||Operations |
|Confab Laboratories Inc. || ||241754217 ||MANUFACTURE(40085-842) |
|Name ||Address ||ID/FEI ||Operations |
|GlaxoSmithKline Inc || ||205556368 ||MANUFACTURE(40085-842) |
Revised: 09/2014 Renaissance Pharma, Inc.