Efficacy and Tolerance of Intravitreal Ganciclovir in Cytomegalovirus Retinitis in Acquired Immune Deficiency Syndrome

Cochereau-Massin, I; LeHoang, Phuc; Lautier-Frau, M; Zazoun, Lydie; Marcel, Patricia; Robinet, M; Matheron, Sophie; Katlama, Christine; Gharakhanian, Shahin; Rozenbaum, Willy; Ingrand, D.; Gentilini, M

doi:10.1016/s0161-6420(91)32135-3

Cited by 154 publications

(40 citation statements)

References 38 publications

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“…However, frequent intravitreal injections are required to maintain therapeutic levels of GCV due to the short half-life of the drug. These continuous administrations bring about the risk of retinal detachments, hemorrhages, or endophthalmitis [6]. Hence, a sustained release by a biodegradable device would decrease these risks and produce a longer therapeutic effect.…”

Section: Introductionmentioning

confidence: 99%

Effect of Ganciclovir on the Hydrolytic Degradation of Poly(lactide-co-glycolide) Microspheres

Chen

Ooi

2006

J Biomater Appl

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Ganciclovir (GCV)-loaded poly(lactide-co-glycolide) (PLGA) microspheres, 125 AE 11 mm in diameter, are produced using the emulsification/ solvent evaporation technique. The release rate of the drug is studied for 20 weeks in a phosphate-buffered solution of pH 7 at 37 C. The release of the drug shows a triphasic release pattern, i.e., an initial burst, a diffusive phase, and a second burst. The initial burst occurs within the first 2 days of immersion. After the burst, the release is by diffusion for up to 13 weeks, followed by another burst release, which signals the onset of bulk degradation of the PLGA polymer. The presence of GCV molecules decreases the hydrolytic rate of PLGA degradation. Gel permeation chromatography (GPC), differential scanning calorimetry (DSC), field emission scanning electron microscopy (FESEM), and ultraviolet (UV) spectroscopy are used to assess the hydrolytic degradation and drug release rate of the microspheres.

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Section: Introductionmentioning

confidence: 99%

Effect of Ganciclovir on the Hydrolytic Degradation of Poly(lactide-co-glycolide) Microspheres

Chen

Ooi

2006

J Biomater Appl

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“…Other toxic effects include granulocytopenia, thrombocytopenia, azoospermia, and rise in the serum creatinine (Faulds and Heel, 1990). Relatively high systemic toxicity caused by intravenous therapy has lead to the intravitreal administration of GCV (Henry et al, 1987;Daikos et al, 1988;Ussery et al, 1988;Cantrill et al, 1989;Cochereau-Massin et al, 1991), which enabled considerable improvement and/or stabilization of HCMV retinitis in most (80 -100%) of the patients. Intravitreal administration has the advantage of maintaining high concentrations of the drug for effective control of ocular infections with minimal systemic adverse effects.…”

mentioning

confidence: 99%

“…Intravitreal administration has the advantage of maintaining high concentrations of the drug for effective control of ocular infections with minimal systemic adverse effects. Clinical trials reported good response rates to intravitreal induction therapy with GCV (Cochereau-Massin et al, 1991). However, very few studies have been carried out to date delineating the intravitreal pharmacokinetics of GCV (Henry et al, 1987;Ashton et al, 1992;Morlet et al, 1996).…”

mentioning

confidence: 99%

Ocular Disposition of Ganciclovir and Its Monoester Prodrugs following Intravitreal Administration Using Microdialysis

Macha¹,

Mitra²

2002

Drug Metab Dispos

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ABSTRACT:The present study was carried out to delineate the ocular pharmacokinetics of ganciclovir (GCV) following intravitreal administration. Another objective was to achieve sustained therapeutic concentrations of GCV in the vitreous over a prolonged period of time using its acyl monoester prodrugs (acetate, propionate, butyrate, and valerate). New Zealand albino male rabbits (2-2.5 kg) were kept under anesthesia. A concentric microdialysis probe was implanted in the vitreous using a 21-guage needle, and a linear microdialysis probe was implanted in the anterior chamber across the cornea using a 25-guage needle. The probes were perfused with isotonic phosphate buffer saline (pH 7.4) at a flow rate of 2 l/min. The drugs were administered (0.2 moles) intravitreally and the samples were collected every 20 min over a period of 10 h. The vitreal terminal elimination half-life (t 1/2 ␤) of GCV was found to be 426 ؎ 109 min. The hydrolysis rate and vitreal clearance of the prodrugs increased with the ascending ester chain length. The vitreal elimination half-lives (t 1/2k10 ) of GCV, acetate, propionate, butyrate, and valerate esters of GCV were 170 ؎ 37, 117 ؎ 50, 122 ؎ 13, 55 ؎ 26, and 107 ؎ 14 min, respectively. A parabolic relationship was observed between the vitreal elimination rate constant and the ester chain length. Mean residence time (MRT) of the regenerated GCV following prodrug administration was found to be three to four times the value obtained after GCV injection. In conclusion, these studies have shown that the ester prodrugs generated therapeutic concentrations of GCV in vivo, and the MRT of GCV could be enhanced by 3-to 4-fold through prodrug modification.

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“…Além da endoftalmite bacteriana, a retinite viral por citomegalovírus também requer tratamento com injeção intravítrea, neste caso com ganciclovir. Realizada sob condições de assepsia, é considerada a mais eficiente via de administração de medicamentos para o tratamento de doenças inflamatórias, infecciosas e proliferativas do segmento posterior (1,3,(20)(21) . Medicamentos hidrofílicos introduzidos no vítreo são preferencialmente eliminados através da hialóide anterior para a câmara anterior e para fora do olho pela drenagem pelo trabeculado.…”

Section: Via Intravítrea De Adminstração De Fármacosunclassified

Farmacologia ocular aplicada no tratamento de doenças do vítreo, retina e coróide

Filho¹,

Maia²,

Rodrigues³

et al. 2010

Arq. Bras. Oftalmol.

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Efficacy and Tolerance of Intravitreal Ganciclovir in Cytomegalovirus Retinitis in Acquired Immune Deficiency Syndrome

Cited by 154 publications

References 38 publications

Effect of Ganciclovir on the Hydrolytic Degradation of Poly(lactide-co-glycolide) Microspheres

Effect of Ganciclovir on the Hydrolytic Degradation of Poly(lactide-co-glycolide) Microspheres

Ocular Disposition of Ganciclovir and Its Monoester Prodrugs following Intravitreal Administration Using Microdialysis

Farmacologia ocular aplicada no tratamento de doenças do vítreo, retina e coróide

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