Pharmacokinetics of acyclovir after intravenous and oral administration

Miranda, Paulo de; Blum, Martin

doi:10.1093/jac/12.suppl_b.29

Cited by 350 publications

(184 citation statements)

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“…However, complete inhibition in vitro was only obtained with 100 ~tM-acyclovir (Linet al, 1984). The pharmacokinetics of ACV shows that after infusion of 10 mg/kg for 30 min there is a peak serum concentration of 60 to 80 p.M which declines to 7 to 8 p.M after 2-5 h (De Miranda & Blum, 1983). In our study, the plasma ACV concentrations assessed immediately after infusion on day 3 and day 7 showed mean peak levels of 78 ~tM (range 44 to 100) and 69 ~tM (range 39 to 120), respectively.…”

supporting

confidence: 49%

Acyclovir Efficiently Inhibits Oropharyngeal Excretion of Epstein-Barr Virus in Patients with Acute Infectious Mononucleosis

Ernberg¹,

Andersson

1986

Journal of General Virology

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SUMMARYShedding of Epstein-Barr virus (EBV) into saliva was studied in 31 patients with verified acute infectious mononucleosis. The patients had been randomized for intravenous treatment with acyclovir (ACV) at 10 mg/kg body weight at 8 h intervals for 7 days, or placebo, in a double-blind trial. EBV in centrifuged throat washings was detected by transformation of umbilical cord lymphocytes and by immunofluorescence staining for EBV-associated nuclear antigen in fixed cell smears. Saliva samples were obtained before and during treatment, and after 4 weeks and 6 months, respectively. ACV effectively but transiently interrupted EBV production (P < 0.001), but virus shedding resumed at the initial level within 3 weeks of cessation of the treatment. Initially, 93-5 ~ of the patients had detectable EBV in the saliva compared with 83 ~ in the 4th week and 58 ~o after 6 months. et al., 1977) which efficiently inhibits not only herpes simplex virus (Schaeffer et al., 1978) but also varicella-zoster virus (Biron & Elion, 1980) and Epstein-Barr virus (EBV) (Colby et al., 1979;Lin et al., 1984) replication in vitro. Both human herpes simplex virus and varicella-zoster virus direct the initial phosphorylation of ACV by the virus-specific thymidine kinase, and after two additional phosphorylations mediated by the cell, the biologically active triphosphorylated form is produced (Elion et al., 1977). This form of ACV inhibits viral DNA polymerase competitively , and also terminates the viral DNA chain because the drug is incorporated in the viral DNA molecule in place of deoxyguanosine monophosphate (Furman et al., 1979). Since an EBV-coded thymidine kinase has recently been identified At pharmacological doses acyclovir (ACV) is a non-toxic antiviral nucleoside analogue (Elion

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supporting

confidence: 49%

Acyclovir Efficiently Inhibits Oropharyngeal Excretion of Epstein-Barr Virus in Patients with Acute Infectious Mononucleosis

Ernberg¹,

Andersson

1986

Journal of General Virology

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“…Patients on thrice-weekly hemodialysis should be given 2.5-5.0 mg/kg q24h (given after dialysis on those days), while those on peritoneal dialysis should be treated with 10 mg/kg q24h [107]. Approximately 15 % (9-22 % in 1 study [108]) of drug is bound to serum proteins and therefore much of the drug can be removed by dialysis. No dosage adjustments are needed in patients with hepatic impairment.…”

Section: Antiviral Medicationmentioning

confidence: 99%

Herpes Simplex Virus-1 Encephalitis in Adults: Pathophysiology, Diagnosis, and Management

2016

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Herpetic infections have plagued humanity for thousands of years, but only recently have advances in antiviral medications and supportive treatments equipped physicians to combat the most severe manifestations of disease. Prompt recognition and treatment can be lifesaving in the care of patients with herpes simplex-1 virus encephalitis, the most commonly identified cause of sporadic encephalitis worldwide. Clinicians should be able to recognize the clinical signs and symptoms of the infection and familiarize themselves with a rational diagnostic approach and therapeutic modalities, as early recognition and treatment are key to improving outcomes. Clinicians should also be vigilant for the development of acute complications, including cerebral edema and status epilepticus, as well as chronic complications, including the development of autoimmune encephalitis associated with antibodies to the N-methyl-D-aspartate receptor and other neuronal cell surface and synaptic epitopes. Herein, we review the pathophysiology, differential diagnosis, and clinical and radiological features of herpes simplex virus-1 encephalitis in adults, including a discussion of the most common complications and their treatment. While great progress has been made in the treatment of this life-threatening infection, a majority of patients will not return to their previous neurologic baseline, indicating the need for further research efforts aimed at improving the long-term sequelae.

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“…2 The pharmacokinetic properties of acyclovir are well established. 3 The effects of dosage size on the extent of oral absorption are not well understood. Some reports suggest that absorption from the gastrointestinal tract may be a saturable, dose-dependent process.…”

Section: Introductionmentioning

confidence: 99%

Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

et al. 2007

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The purpose of this research was to prepare acyclovir niosomes in a trial to improve its poor and variable oral bioavailability. The nonionic surfactant vesicles were prepared by the conventional thin film hydration method. The lipid mixture consisted of cholesterol, span 60, and dicetyl phosphate in the molar ratio of 65:60:5, respectively. The percentage entrapment was~11% of acyclovir used in the hydration process. The vesicles have an average size of 0.95 μm, a most probable size of 0.8 μm, and a size range of 0.4 to 2.2 μm. Most of the niosomes have unilamellar spherical shape. In vitro drug release profile was found to follow Higuchi's equation for free and niosomal drug. The niosomal formulation exhibited significantly retarded release compared with free drug. The in vivo study revealed that the niosomal dispersion significantly improved the oral bioavailability of acyclovir in rabbits after a single oral dose of 40 mg kg −1 . The average relative bioavailability of the drug from the niosomal dispersion in relation to the free solution was 2.55 indicating more than 2-fold increase in drug bioavailability. The niosomal dispersion showed significant increase in the mean residence time (MRT) of acyclovir reflecting sustained release characteristics. In conclusion, the niosomal formulation could be a promising delivery system for acyclovir with improved oral bioavailability and prolonged drug release profiles.

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Pharmacokinetics of acyclovir after intravenous and oral administration

Cited by 350 publications

References 0 publications

Acyclovir Efficiently Inhibits Oropharyngeal Excretion of Epstein-Barr Virus in Patients with Acute Infectious Mononucleosis

Acyclovir Efficiently Inhibits Oropharyngeal Excretion of Epstein-Barr Virus in Patients with Acute Infectious Mononucleosis

Herpes Simplex Virus-1 Encephalitis in Adults: Pathophysiology, Diagnosis, and Management

Influence of a niosomal formulation on the oral bioavailability of acyclovir in rabbits

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