Acyclovir Suspension

Acyclovir Suspension

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Questions & Answers

Side Effects & Adverse Reactions

Acyclovir 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.

Legal Issues

There is currently no legal information available for this drug.

FDA Safety Alerts

There are currently no FDA safety alerts available for this drug.

Manufacturer Warnings

There is currently no manufacturer warning information available for this drug.

FDA Labeling Changes

There are currently no FDA labeling changes available for this drug.

Uses

Herpes Zoster Infections:

Acyclovir oral suspension, USP is indicated for the acute treatment of herpes zoster (shingles).

Genital Herpes:

Acyclovir oral suspension, USP is indicated for the treatment of initial episodes and the management of recurrent episodes of genital herpes.

Chickenpox:

Acyclovir oral suspension, USP is indicated for the treatment of chickenpox (varicella).

History

There is currently no drug history available for this drug.

Other Information

Acyclovir is a synthetic nucleoside analogue active against herpesviruses.

Each teaspoonful (5 mL) of acyclovir oral suspension, USP, for oral administration, contains 200 mg of acyclovir and the inactive ingredients artificial banana flavor, carboxymethylcellulose sodium, glycerin, methylparaben 0.1% (added as a preservative), microcrystalline cellulose, propylparaben 0.02% (added as a preservative), purified water, and sorbitol.

Acyclovir is a white, crystalline powder with the molecular formula C8H11N5O3 and a molecular weight of 225. The maximum solubility in water at 37°C is 2.5 mg/mL. The pka’s of acyclovir are 2.27 and 9.25.

The chemical name of acyclovir is 2-amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]- 6H-purin-6-one; it has the following structural formula:

image of chemical structure

VIROLOGY: 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.

Antiviral Activities:

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.

Drug Resistance:

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 Manufacturers


  • Physicians Total Care, Inc.
    Acyclovir Suspension [Physicians Total Care, Inc.]
  • Hi-tech Pharmacal Co., Inc.
    Acyclovir Suspension [Hi-tech Pharmacal Co., Inc.]
  • Preferred Pharmaceuticals, Inc.
    Acyclovir Suspension [Preferred Pharmaceuticals, Inc.]
  • Actavis Mid Atlantic Llc
    Acyclovir Suspension [Actavis Mid Atlantic Llc]
  • Preferred Pharmaceuticals, Inc
    Acyclovir Suspension [Preferred Pharmaceuticals, Inc]
  • Atlantic Biologicals Corps
    Acyclovir Suspension [Atlantic Biologicals Corps]
  • Renaissance Pharma, Inc.
    Acyclovir Suspension [Renaissance Pharma, Inc.]

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