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1.
J Vet Pharmacol Ther ; 31(4): 312-20, 2008 Aug.
Article in English | MEDLINE | ID: mdl-18638291

ABSTRACT

Recent outbreaks of equine herpes virus type-1 infections have stimulated renewed interest in the use of effective antiherpetic drugs in horses. The purpose of this study was to investigate the pharmacokinetics of valacyclovir (VCV), the prodrug of acyclovir (ACV), in horses. Six adult horses were used in a randomized cross-over design. Treatments consisted of 10 mg/kg ACV infused intravenously, 5 g (7.7-11.7 mg/kg) VCV delivered intragastrically (IG) and 15 g (22.7-34.1 mg/kg) VCV administered IG. Serum samples were obtained at predetermined times for acyclovir assay using high-performance liquid chromatography. Following the administration of 5 g VCV, the mean observed maximum serum ACV concentration (C(max)) was 1.45 +/- 0.38 (SD) microg/mL, at 0.74 +/- 0.43 h. At a dose of 15 g VCV, the mean C(max) was 5.26 +/- 2.82 microg/mL, at 1 +/- 0.27 h. The mean bioavailability of ACV from oral VCV was 60 +/- 12% after 5 g of VCV and 48 +/- 12% after 15 g VCV, and did not differ significantly between dose rates (P > 0.05). Superposition suggested that a loading dose of 27 mg/kg VCV every 8 h for 2 days, followed by a maintenance dose of 18 mg/kg every 12 h, will maintain effective serum ACV concentrations.


Subject(s)
Acyclovir/analogs & derivatives , Antiviral Agents/pharmacokinetics , Valine/analogs & derivatives , Acyclovir/administration & dosage , Acyclovir/blood , Acyclovir/pharmacokinetics , Administration, Oral , Animals , Antiviral Agents/administration & dosage , Antiviral Agents/blood , Area Under Curve , Biological Availability , Chromatography, High Pressure Liquid , Female , Half-Life , Horses , Infusions, Intravenous , Male , Metabolic Clearance Rate , Valacyclovir , Valine/administration & dosage , Valine/blood , Valine/pharmacokinetics
2.
J Vet Pharmacol Ther ; 28(3): 299-304, 2005 Jun.
Article in English | MEDLINE | ID: mdl-15953204

ABSTRACT

Local anesthesia and tissue inflammation associated with lidocaine infiltration and lidocaine/prilocaine topical anesthetic cream for episioplasty in mares were compared. Twenty-two mares were randomly assigned to lidocaine or lidocaine/prilocaine topical anesthetic cream treatment groups. Perineum and vulva were cleaned, 8-12 g (approximately 1 g/cm per side of vulva) of topical anesthetic cream was applied, and the area was covered by plastic wrap 30 min prior to beginning procedure. Alternately, lidocaine was injected (1 mL) every centimeter just prior to the procedure. Episioplasty was conducted using standard methods, but employing simple interrupted sutures. Horses were not sedated and use of a twitch was recorded. Four millimeter punch biopsies were harvested 1, 3, and 10 days following episioplasty and scored for degree of inflammation by a blinded pathologist. Clinical inflammation scores were assigned when biopsies were obtained. Seven of 11 horses receiving lidocaine infiltration required twitching, but none of the horses that received the anesthetic cream required twitching. Six of 11 and seven of 11 of the lidocaine and anesthetic cream groups, respectively, required twitching for episioplasty. Except for the clinical scores on day 3, no statistical differences for clinical and histopathologic scores between samples from the two treatment groups for a given day were identified. Use of lidocaine/prilocaine topical anesthetic cream was as effective as lidocaine infiltration in providing local anesthesia when performing episioplasty in mares. Its use decreased the need for twitching horses as well as the risk of deformation of the labia caused by lidocaine infiltration.


Subject(s)
Anesthesia, Local/veterinary , Anesthetics, Local/pharmacokinetics , Horses/physiology , Lidocaine/pharmacokinetics , Prilocaine/pharmacokinetics , Skin/metabolism , Administration, Cutaneous , Anesthetics, Local/administration & dosage , Anesthetics, Local/pharmacology , Animals , Episiotomy/veterinary , Female , Genitalia, Female/surgery , Horses/surgery , Lidocaine/administration & dosage , Lidocaine/pharmacology , Pain Measurement/drug effects , Pain, Postoperative/prevention & control , Prilocaine/administration & dosage , Prilocaine/pharmacology , Treatment Outcome
3.
J Vet Pharmacol Ther ; 25(2): 81-7, 2002 Apr.
Article in English | MEDLINE | ID: mdl-12000527

ABSTRACT

Isoxsuprine hydrochloride has been suggested for use in horses for treatment of navicular syndrome and laminitis. The drug has been shown to be a beta-adrenoreceptor antagonist with beta-adrenoreceptor agonistic properties, with both characteristics contributing to vasodilation and uterine relaxation. In addition, the drug is capable of decreasing blood viscosity and platelet aggregation. Studies have shown i.v. isoxsuprine to have a plasma half-life of <3 h with a large apparent volume of distribution. Cardiovascular effects resolve rapidly following i.v. administration, but are absent with oral dosing. Oral bioavailability is 2.2% with a high first pass effect. Isoxsuprine has an apparent affinity for melanin that may contribute to extended renal excretion. Clinical trials appear to support the use of isoxsuprine for treatment of navicular disease. However, poor bioavailability, lack of cardiovascular effects following oral administration, superficial support in clinical trials, and new evidence regarding the pathogenesis of navicular syndrome indicate that the use of isoxsuprine for treatment of navicular syndrome or laminitis is questionable at best.


Subject(s)
Horse Diseases/drug therapy , Horses/metabolism , Isoxsuprine/pharmacokinetics , Isoxsuprine/therapeutic use , Osteitis/veterinary , Vasodilator Agents/pharmacokinetics , Vasodilator Agents/therapeutic use , Administration, Oral , Animals , Biological Availability , Foot Diseases/drug therapy , Foot Diseases/veterinary , Infusions, Intravenous/veterinary , Isoxsuprine/administration & dosage , Lameness, Animal/drug therapy , Osteitis/drug therapy , Tarsal Bones/blood supply , Vasodilator Agents/administration & dosage
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