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PubMed1998

Lack of interaction between valaciclovir, the L-valyl ester of aciclovir, and digoxin.

AIMS: Changes in both digoxin and aciclovir renal clearance following coadministration with some other renally eliminated drugs have been reported. The potential interaction of valaciclovir, with its antiherpetic metabolite aciclovir, and digoxin was investigated. METHODS: Twelve healthy volunteers (seven males, five females) participated in an open, randomized, four-period crossover study. Valaciclovir, 1000 mg, was given alone on one occasion, and on another, after the second of two 0.75 mg digoxin doses administered 12 h apart. Blood samples and all urine were collected up to 12 h following the valaciclovir dose for aciclovir radioimmunoassay. On a third occasion, digoxin was given alone and on a fourth, with 1000 mg valaciclovir three times/day for 8 days starting 12 h before the first digoxin dose. Blood samples were taken up to 168 h and all urine collected up to 24 h following the second dose for digoxin radioimmunoassay. RESULTS: There were no clinically significant differences in digoxin or aciclovir pharmacokinetic parameters when digoxin or valaciclovir was given alone or in combination. CONCLUSIONS: No dosage adjustment is required when valaciclovir and digoxin are coadministered.

Acyclovir↗
PubMed2003

Valaciclovir as a single dose during prodrome of herpes facialis: a pilot randomized double-blind clinical trial.

BACKGROUND: Randomized clinical trials of valaciclovir in recurrent herpes labialis are lacking. OBJECTIVES: To determine whether a single course of valaciclovir, i.e. 500, 1000 or 2000 mg, administered during the prodrome of herpes facialis, could be beneficial. METHODS: Three hundred and forty-five out-patients with herpes labialis were screened and randomized for a multicentre, double-blind clinical trial. Ninety-six patients had no recurrence after 6 months of follow-up; 249 patients were finally included in the intent-to-treat (ITT) population. The main outcome measure was the rate of aborted episodes at day 3. The three treatment groups were similar at baseline. RESULTS: There was no statistically significant difference between the groups in rates of aborted lesions at day 3 in the ITT population, in particular between the 500 mg and 2000 mg treatment groups. CONCLUSIONS: Although a placebo group was not included in this pilot study, a single dose of valaciclovir was not considered beneficial in patients with recurrent herpes facialis.

Acyclovir↗
PubMed2000

Factors influencing pain outcome in herpes zoster: an observational study with valaciclovir. Valaciclovir International Zoster Assessment Group (VIZA).

AIM OF THE STUDY: An observational study with valaciclovir was conducted to assess clinical outcome in herpes zoster, especially pain and associated neurological signs and symptoms in relation to a series of demographic and disease characteristics discernible at presentation. The safety and acceptability of valaciclovir for treatment of zoster was assessed in a wide variety of primary care and clinic referral settings. METHODS: In total, 1897 immunocompetent adults with clinically diagnosed, localized acute herpes zoster were enrolled in this international, open-label study of valaciclovir. All subjects received treatment with oral valaciclovir (1000 mg three times daily) for 7 days from entry to the study and were asked to record the presence of zoster-associated pain and abnormal sensations throughout treatment and 6 months' follow-up. They were seen frequently in clinic to verify subjective assessments and for evaluation of rash healing. Safety and tolerability were assessed by adverse event monitoring. RESULTS: Overall, 1191 subjects (63%) were aged > or = 50 years, and 203 (11%) had ophthalmic zoster. Cessation of zoster-associated pain was significantly faster in the younger age group; median times to loss of zoster-associated pain were 23 days and 9 days in the > or = 50 and < 50 years age groups, respectively. Similarly, abnormal sensations resolved significantly more rapidly in the younger subjects; the median duration of abnormal sensations was 31 days in the > or = 50 year olds and 16 days in those aged < 50 years. In cases of ophthalmic zoster, the rate of pain resolution was not different from those with zoster in other dermatomes (median duration of pain 18 vs. 16 days). However, abnormal sensations persisted significantly longer in subjects with ophthalmic zoster than in those with zoster at other sites (47 vs. 22 days). In addition to advancing age, subjects suffering moderate to severe prodromal pain or acute pain during the rash phase were at significantly greater risk of zoster-associated pain and abnormal sensations persisting for longer. Subjects with concomitant neurological disorders were also more likely to develop prolonged abnormal sensations. Valaciclovir treatment was well tolerated, and adverse events were rare and generally mild. CONCLUSION: This study confirmed the prognostic importance of advancing age and the intensity of prodromal or acute pain as risk factors for prolonged zoster-associated pain and persisting abnormal sensations in the affected dermatome. Ophthalmic zoster and pre-existing neurological disorders are also identified as highly significant risk factors for prolonged abnormal sensations in herpes zoster.

Acyclovir↗
PubMed2000

Kaposi's varicelliform eruption in a patient with healing peribucal dermabrasion.

Kaposi varicelliform eruption (KVE) is the name given to a distinct cutaneous eruption caused by Herpesvirus hominis types 1 and 2, vaccinia virus, or coxsackie A16 virus, superimposed on a preexisting dermatosis. A delay in diagnosing this condition may result in intense pain and rapid spread of the cutaneous lesions. We report a patient who underwent perioral dermabrasion for wrinkles who developed KVE secondary to herpes simplex virus infection.

Acyclovir↗
PubMed2002

Herpes simplex virus infection.

Herpes simplex virus (HSV) infections are among the infections most frequently encountered by humans. Two types of HSV infections have been identified-HSV-1, which usually causes orolabial disease, and HSV-2, which is associated more frequently with genital and newborn infections. Usually, HSV causes mild and self-limited disease of the mouth and lips or at genital sites. However, on occasion, the disease can be life-threatening. Such is the case with neonatal HSV infection and HSV infections of the central nervous system. Furthermore, in the immunocompromised host, severe infection has been encountered and is a source of morbidity. Even in the immunocompetent host, frequent recurrences, particularly those of the genital tract, can be debilitating. Because HSV does cause genital ulcerative disease, it is associated with an increased risk of acquiring a human immunodeficiency virus infection. During the past 2 decades, selective and specific inhibitors of HSV replication have been developed. These agents, acyclovir, valaciclovir, and famciclovir, all accelerate the events of healing and decrease the probability of excreting the virus when they are taken in a suppressive fashion. The long-term safety of acyclovir has been unequivocally established. Its prodrug, valaciclovir, and the prodrug of penciclovir, famciclovir, have not been used in practice as long and, therefore, less is known about these agents; however, neither is available as a pediatric formulation.

2-Aminopurine↗
PubMed1999

[Bilateral neuroretinitis with zoster infection].

BACKGROUND: Infections with varicella zoster virus may involve the optic nerve and the retina. Different pathomechanisms have been discussed. We present a case with an autoimmune inflammatory reaction according to the clinical course. PATIENT: A 69-year-old female was referred to our clinic because of suspected bilateral anterior ischemic optic neuropathy. She complained of severe visual loss the day before admission. Her ophthalmological and general history was unremarkable apart from treatment with 5 to 7.5 mg prednisolone alternately because of rheumatoid arthritis. Best corrected visual acuity was 1/15 OD and 0.1 OS. A relative afferent pupillary defect on the right eye was present. Optic disc oedema with multiple hemorrhages of the retina extending into the peripheral funds, slightly attenuated retinal arteries and macular oedema were seen fundoscopically in both eyes. THERAPY AND CLINICAL OUTCOME: After immediate treatment with steroids (initial dose 250 mg prednisolone per day) visual acuity improved. Because of a clinically suspected and serologically proven active varicella-zoster infection an additional virostatic therapy with valaciclovir was started and steroids were lowered gradually. Within 2 months, visual acuity increased to 0.8 OD and 1.0 OS. Oedema of optic discs and macula resolved and retinal hemorrhages disappeared. CONCLUSION: A severe hemorrhagic neuro-retinitis involving the optic discs was seen in the course of a varicella-zoster infection, possibly reactivated by chronic steroid therapy of a rheumatoid arthritis. Because of the normalization of visual function an ischemic pathogenesis is unlikely. An autoimmune inflammatory reaction seems to be the predominant mechanism, supported by the good effect of steroid and valaciclovir therapy.

Acyclovir↗
PubMed2002

Antiviral agents: Non-antiretroviral [correction of Nonantiviral] drugs.

The current arsenal of antiviral agents available to the practitioner is expanding rapidly, such that by the time this article goes to press, new drugs may have already been added. Although the majority of approved drugs have been developed for use in only a few viral infections (eg, HIV, herpesviruses, and papillomavirus), discoveries made in the development of these drugs may lead to antiviral agents effective against other viruses. In addition, new uses for the currently available drugs are under evaluation. This review of antiviral agents discusses the treatments available for viral infections such as herpes simplex virus, varicella zoster virus, cytomegalovirus, human papillomavirus, chronic viral hepatitis, and others.

2-Aminopurine↗
PubMed2002

Topical 5% imiquimod for the therapy of actinic cheilitis.

BACKGROUND: Tissue-destructive and more selective cytotoxic therapies are the main methods used to treat actinic cheilitis. A topical immune stimulant, 5% imiquimod cream, has recently been used for treatment of cutaneous epithelial malignancies including squamous cell carcinoma in situ and basal cell carcinoma. OBJECTIVE: Our aim was to review the results in patients who had been treated for actinic cheilitis with imiquimod cream. METHODS: A review identified 15 patients with biopsy-proven actinic cheilitis who had been treated with topical imiquimod 3 times weekly for 4 to 6 weeks. All patients with histories consistent with facial herpes simplex or documented prior facial herpes simplex eruptions were treated with oral valcyclovir, 1 g/d, during imiquimod therapy. RESULTS: All 15 patients showed clinical clearing of their actinic cheilitis at 4 weeks after discontinuation of the topical imiquimod. Sixty percent of the patients experienced a moderate to marked increased local reaction consisting of increased erythema, induration, and erosions or ulcerations, which in some cases continued through the period of therapy. CONCLUSION: Imiquimod appears to have a role in the treatment of actinic cheilitis. However, the dose and duration of therapy, as well as the long-term efficacy, need to be established; and local reactions are to be expected and may not improve during therapy.

Acyclovir↗
PubMed2002

Acyclovir concentrations in human breast milk after valaciclovir administration.

OBJECTIVE: The purpose of this study was to determine the valaciclovir and acyclovir pharmacokinetic profiles in serum and breast milk after valaciclovir administration to women after delivery. STUDY DESIGN: Valaciclovir (500 mg twice daily for 7 days) was given to 5 women after delivery who were breast-feeding healthy term infants. Matched serum and breast milk samples were obtained after the initial dose, on day 5 and 24 hours after the drug was discontinued. Infant urine was obtained on day 5. RESULTS: Valaciclovir was rapidly converted to acyclovir. The peak serum acyclovir concentration occurred 3 hours before the peak breast milk concentration (2.7 microg/mL at 1 hour vs 4.2 microg/mL at 4 hours). The serum acyclovir elimination half-life was 2.3 hours. The ratio of breast milk to serum acyclovir concentration was highest 4 hours after the initial dose at 3.4 and reached steady state ratio at 1.85. The median infant urine acyclovir concentration at steady state was 0.74 microg/mL. CONCLUSION: Valaciclovir is rapidly converted to acyclovir and concentrates in breast milk. However, the amount of acyclovir in breast milk after valaciclovir administration is considerably less (2%) than that used in therapeutic dosing of neonates.

Acyclovir↗
PubMed1995

Purification and characterization of a rat liver enzyme that hydrolyzes valaciclovir, the L-valyl ester prodrug of acyclovir.

Valaciclovir is an oral prodrug of the antiherpetic agent acyclovir. An enzyme that hydrolyzes valaciclovir to acyclovir, valaciclovir hydrolase (VACVase), was purified from rat liver and characterized. VACVase was a basic (pI 9.4) protein associated with mitochondria. It was monomeric and had a molecular mass of 29 kDa. Amino acid sequences of six VACVase peptides, including its NH2 terminus (13 amino acids) and accounting for approximately 20% of its complete sequence, were not found in the SwissProt protein data base. VACVase hydrolyzed other amino acid esters of acyclovir in addition to valaciclovir (kcat/Km = 58 mM-1 s-1), with a preference for the L-alanyl (kcat/Km = 226 mM-1 s-1) and L-methionyl (kcat/Km = 200 mM-1 s-1) esters. It did not hydrolyze other types of esters or numerous di- and tripeptides and aminoacyl-beta-naphthylamides. Hydrolysis of valaciclovir by VACVase was not inhibited by amastatin, antipain, aprotinin, bestatin, chymostatin, E-64, EDTA, ebelactone A, ebelactone B, elastatinal, leupeptin, pepstatin, or phosphoramidon. It was neither inhibited nor activated by Ca2+, Co2+, Mg2+, Mn2+, or Zn2+. Therefore, this enzyme is not a typical esterase or peptidase and, to our knowledge, it has not been described previously. Its physiological function is not known; however, it may play a significant role in the biotransformation of valaciclovir to acyclovir.

Acyclovir↗
PubMedDate not supplied

Novel dipeptide prodrugs of acyclovir for ocular herpes infections: Bioreversion, antiviral activity and transport across rabbit cornea.

PURPOSE: A series of dipeptide prodrugs of antiviral nucleoside acyclovir (ACV) were designed to target the oligopeptide transporter on the cornea with an aim of improving the ocular bioavailability and therapeutic activity of ACV. METHODS: Aqueous stability, ocular bioreversion kinetics in various tissues, in vitro antiviral activity, cell proliferation assay and corneal transport characteristics of the dipeptide prodrugs were studied. Results. ACV dipeptide prodrugs were found to be more stable at pH 5.6 in comparison to L-Val-ACV, an amino acid prodrug of ACV. The prodrugs exhibited higher solubility than ACV. Val-Val-ACV and Val-Tyr-ACV were found to have excellent antiviral activity against herpes simplex virus-1 (HSV-1). All the dipeptide prodrugs exhibited lower cytotoxicity as compared to currently approved anti-HSV agent, trifluorothymidine (TFT). Transport of [(3)H] Val-ACV was inhibited significantly in the presence of the dipeptide prodrugs of ACV. Corneal permeabilities of all the ACV dipeptide prodrugs were observed to be higher than ACV possibly due to recognition of the prodrugs by the oligopeptide transporter on the cornea. CONCLUSIONS: The dipeptide prodrugs were found to be more permeable than the parent drug, ACV. More permeable, less cytotoxic ACV dipeptide prodrugs exhibited excellent chemical stability and antiviral activity against herpes simplex virus thereby rendering these lead compounds promising drug candidates against herpes virus infections.

Acyclovir↗