Valtrex (valacyclovir HCl)

Antiviral - Herpes Viruses Oral Tablet

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Valacyclovir, the l-valine ester of acyclovir, is an antiviral agent that is a prodrug of acyclovir and is active against herpes viruses.

Valacyclovir, thel-valine ester of acyclovir, is an antiviral agent. Valacyclovir is a prodrug and exhibits no antiviral activity until hydrolyzed in the intestinal wall and/or liver to acyclovir and subsequently to its active metabolite (acyclovir triphosphate). Valacyclovir is commercially available as the hydrochloride salt and differs structurally from acyclovir by the presence of the l-amino acid, valine, attached to the 5'-hydroxyl group of the nucleoside and by the presence of the monohydrochloride salt.

These structural modifications result in substantially increased GI absorption of valacyclovir and resultant plasma acyclovir concentrations compared with those achieved orally with the parent drug acyclovir, which is poorly absorbed from the GI tract.

Valacyclovir is rapidly converted to acyclovir in vivo and subsequently to the pharmacologically active triphosphate metabolite, which has in vitro and in vivo inhibitory activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2), varicella-zoster virus (VZV), and cytomegalovirus (CMV). Acyclovir triphosphate exerts its antiviral effect on HSV and VZV by interfering with DNA synthesis and inhibiting viral replication. The inhibitory activity of acyclovir triphosphate is highly selective because of its affinity for the enzyme thymidine kinase encoded by HSV and VZV; however, other mechanisms may be involved since the drug exhibits activity against viruses that apparently do not code for this enzyme.

Virus-coded thymidine kinase converts acyclovir into acyclovir monophosphate, a nucleotide analog. The monophosphate is further converted to the diphosphate via cellular guanylate kinase and then to the triphosphate via other cellular enzymes. In vitro, acyclovir triphosphate stops replication of herpes viral DNA by competitive inhibition of viral DNA polymerase, incorporation and termination of the growing viral DNA chain, and inactivation of the viral DNA polymerase.

For additional information, see Mechanism of Action in Acyclovir 8:18.32.

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information.

The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Oral valacyclovir is used for the treatment of initial and recurrent episodes of genital herpes infections in immunocompetent adults and adolescents and for the suppression of recurrent episodes of genital herpes in immunocompetent adults and adolescents and individuals infected with human immunodeficiency virus (HIV). Valacyclovir also is used for the episodic treatment of herpes labialis (perioral herpes, cold sores, fever blisters) in adults and adolescents and for the treatment of acute, localized herpes zoster (shingles, zoster) in adults and adolescents.

Generic name: valacyclovir HCl
Pronunciation: (val-uh-SYE-klo-veer)
Drug class: Antiviral - Herpes Viruses
Therapeutic class: Anti-Infective Agents

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Valtrex:

  • Chickenpox
  • Genital Herpes Simplex
  • Herpes Labialis
  • Herpes Zoster
  • Recurrent Herpes Genitalis
  • Suppression Of Recurrent Herpes Simplex Infection
  • Suppression Of Recurrent Herpes Simplex Infection In Hiv

Also known as: Herpes Genitalis, Herpes Simplex Type 1 Infection Of The Lip Or Nares, Hsv Type 1 Infection Of The Lip Or Nares, Latent Varicella Zoster Virus Infection, Latent Vzv Infection, Prophylaxis For Herpes Simplex, Recurrent Genital Herpes Simplex, Varicella.

Dosing

Dosage of valacyclovir hydrochloride is expressed in terms of valacyclovir.

Valacyclovir dosage modification according to renal function may be necessary in geriatric patients, depending on the underlying renal status of the patient. (See Dosage and Administration: Dosage in Renal and Hepatic Impairment.)

The manufacturer states that valacyclovir should be used with caution in patients receiving potentially nephrotoxic agents because this may increase the risk of renal dysfunction and/or reversible CNS manifestations. In patients with impaired renal function, doses and/or frequency of administration of valacyclovir must be modified in response to the degree of impairment.

For the treatment of first episodes of genital herpes in immunocompetent adults with impaired renal function, the manufacturer states that patients with creatinine clearances of 30 mL/minute per 1.73 m2 or greater may receive the usual oral valacyclovir dosage of 1 g every 12 hours; however, those with creatinine clearances of 10-29 or less than 10 mL/minute per 1.73 m2 should receive 1 g or 500 mg, respectively, once every 24 hours. For the episodic treatment of recurrent genital herpes in immunocompetent adults with impaired renal function, patients with creatinine clearances of 30 mL/minute per 1.73 m2 may receive the usual dosage of 500 mg every 12 hours, but those with clearances of 29 mL/minute per 1.73 m2 or less should receive 500 mg once every 24 hours.

For chronic suppression of recurrent episodes of genital herpes in immunocompetent adults with renal impairment, those with creatinine clearances of 30 mL/minute per 1.73 m2 or greater may receive the usually recommended dosage of oral valacyclovir. Patients with creatinine clearances less than 30 mL/minute per 1.73 m2 should receive 500 mg once every 24 hours; alternatively, those with a history of 9 or fewer recurrences per year may receive 500 mg once every 48 hours.

For chronic suppression of recurrent episodes of genital herpes in HIV-infected adults with renal impairment, those with creatinine clearances of 30 mL/minute per 1.73 m2 or greater may receive the usually recommended dosage of oral valacyclovir and those with creatinine clearances less than 30 mL/minute per 1.73 m2 should receive 500 mg once every 24 hours.

For the treatment of herpes labialis (cold sores) in patients with renal impairment, patients with creatinine clearances of 50 mL/minute or greater per 1.73 m2 may receive the usual oral valacyclovir dosage of 2 g every 12 hours for 1 day. Those with creatinine clearances of 30-49 mL/minute per 1.73 m2 should receive 1 g every 12 hours for 1 day, those with creatinine clearances of 10-29mL/minute per 1.73 m2 should receive 500 mg every 12 hours for 1 day, and those with creatinine clearances less than 10 mL/minute per 1.73 m2 should receive a single 500-mg dose.

For the treatment of acute, localized herpes zoster in adults, the manufacturer states that patients with creatinine clearances of 50 mL/minute or greater per 1.73 m2 may receive the usual oral valacyclovir dosage of 1 g every 8 hours. Those with creatinine clearances of 30-49 mL/minute per 1.73 m2 should receive 1 g every 12 hours, and those with creatinine clearances of 10-29 or less than 10 mL/minute per 1.73 m2 should receive 1 g or 500 mg, respectively, once every 24 hours.

Because acyclovir is removed by hemodialysis, the manufacturer states that patients undergoing hemodialysis may require a supplemental dose of valacyclovir after each dialysis period. However, if usual dosing coincides with a valacyclovir dose being administered soon after hemodialysis and subsequent dialysis takes place toward the end of the dosing interval, a supplemental dose would not be necessary.

Information regarding use of valacyclovir in patients undergoing peritoneal dialysis is not available. Based on experience with acyclovir, the manufacturer states that supplemental doses of valacyclovir do not appear to be necessary following peritoneal dialysis, either continuous ambulatory peritoneal dialysis (CAPD) or continuous arteriovenous hemofiltration/dialysis (CAVHD).

The rate but not the extent of conversion of valacyclovir to acyclovir may be reduced in patients with moderate (biopsy-proven cirrhosis) or severe (with and without ascites and biopsy-proven cirrhosis) hepatic impairment. Therefore, the manufacturer states that dosage modification is not necessary for patients with cirrhosis.

Drug interactions

There is no enhanced messaging for this drug.

Contraindications

Known hypersensitivity or intolerance to valacyclovir, acyclovir, or any component of the formulation.

Adverse reactions

Headache, nausea, vomiting.

Precautions

No enhanced messaging available.

ICD codes

CodeTypeDescription
Chickenpox
B01ICD10CMVaricella [chickenpox]
B01.9ICD10CMVaricella without complication
Genital herpes simplex
A60ICD10CMAnogenital herpesviral [herpes simplex] infections
A60.0ICD10CMHerpesviral infection of genitalia and urogenital tract
A60.00ICD10CMHerpesviral infection of urogenital system, unspecified
A60.01ICD10CMHerpesviral infection of penis
A60.02ICD10CMHerpesviral infection of other male genital organs
A60.03ICD10CMHerpesviral cervicitis
A60.04ICD10CMHerpesviral vulvovaginitis
A60.09ICD10CMHerpesviral infection of other urogenital tract
A60.9ICD10CMAnogenital herpesviral infection, unspecified
Herpes labialis
B00.1ICD10CMHerpesviral vesicular dermatitis
Herpes zoster
B02ICD10CMZoster [herpes zoster]
B02.0ICD10CMZoster encephalitis
B02.1ICD10CMZoster meningitis
B02.2ICD10CMZoster with other nervous system involvement
B02.3ICD10CMZoster ocular disease
B02.30ICD10CMZoster ocular disease, unspecified
B02.31ICD10CMZoster conjunctivitis
B02.32ICD10CMZoster iridocyclitis
B02.33ICD10CMZoster keratitis
B02.34ICD10CMZoster scleritis
B02.39ICD10CMOther herpes zoster eye disease
B02.7ICD10CMDisseminated zoster
B02.8ICD10CMZoster with other complications
B02.9ICD10CMZoster without complications
Recurrent herpes genitalis
A60ICD10CMAnogenital herpesviral [herpes simplex] infections
A60.0ICD10CMHerpesviral infection of genitalia and urogenital tract
A60.00ICD10CMHerpesviral infection of urogenital system, unspecified
A60.01ICD10CMHerpesviral infection of penis
A60.02ICD10CMHerpesviral infection of other male genital organs
A60.03ICD10CMHerpesviral cervicitis
A60.04ICD10CMHerpesviral vulvovaginitis
A60.09ICD10CMHerpesviral infection of other urogenital tract
A60.9ICD10CMAnogenital herpesviral infection, unspecified
Suppression of recurrent herpes simplex infection
A60ICD10CMAnogenital herpesviral [herpes simplex] infections
A60.0ICD10CMHerpesviral infection of genitalia and urogenital tract
A60.00ICD10CMHerpesviral infection of urogenital system, unspecified
A60.01ICD10CMHerpesviral infection of penis
A60.02ICD10CMHerpesviral infection of other male genital organs
A60.03ICD10CMHerpesviral cervicitis
A60.04ICD10CMHerpesviral vulvovaginitis
A60.09ICD10CMHerpesviral infection of other urogenital tract
A60.1ICD10CMHerpesviral infection of perianal skin and rectum
A60.9ICD10CMAnogenital herpesviral infection, unspecified
B00.2ICD10CMHerpesviral gingivostomatitis and pharyngotonsillitis
B00.89ICD10CMOther herpesviral infection
B00.9ICD10CMHerpesviral infection, unspecified
Suppression of recurrent herpes simplex infection in HIV
A60ICD10CMAnogenital herpesviral [herpes simplex] infections
A60.0ICD10CMHerpesviral infection of genitalia and urogenital tract
A60.00ICD10CMHerpesviral infection of urogenital system, unspecified
A60.01ICD10CMHerpesviral infection of penis
A60.02ICD10CMHerpesviral infection of other male genital organs
A60.03ICD10CMHerpesviral cervicitis
A60.04ICD10CMHerpesviral vulvovaginitis
A60.09ICD10CMHerpesviral infection of other urogenital tract
A60.1ICD10CMHerpesviral infection of perianal skin and rectum
A60.9ICD10CMAnogenital herpesviral infection, unspecified
B00.0ICD10CMEczema herpeticum
B00.1ICD10CMHerpesviral vesicular dermatitis
B00.2ICD10CMHerpesviral gingivostomatitis and pharyngotonsillitis
B00.5ICD10CMHerpesviral ocular disease
B00.50ICD10CMHerpesviral ocular disease, unspecified
B00.51ICD10CMHerpesviral iridocyclitis
B00.52ICD10CMHerpesviral keratitis
B00.53ICD10CMHerpesviral conjunctivitis
B00.59ICD10CMOther herpesviral disease of eye
B00.89ICD10CMOther herpesviral infection

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data