Clinical use of dopamine antagonist sulpiride to advance first ovulation in transitional mares

Panzani, Duccio; Zicchino, I.; Taras, Andrea; Marmorini, P; Crisci, A; Rota, Alessandra; Camillo, Francesco

doi:10.1016/j.theriogenology.2010.07.019

Cited by 31 publications

(29 citation statements)

References 15 publications

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“…The lack of adverse effects in jennies given 1 mg/kg concurs with a previous study in nurse mares [12] and with the good tolerance previously reported in human beings [5]. This also supports clinical reports showing no adverse effects in horses after a 3-week treatment period with this dose regimen [10]. Of relevance however, is the fact that SLP probably does not bind to plasma proteins [20], and it is likely to be predominantly excreted by the kidneys, mainly by glomerular filtration [15].…”

Section: Discussionsupporting

confidence: 92%

“…This dose was chosen according to recent studies assessing the effectiveness of SLP when administered daily for a 21-day period [9,10] and the PK profile after a single-dose administration in horses [12]. No adverse effects were observed during the present study.…”

Section: Resultsmentioning

confidence: 99%

“…In subsequent studies, SLP has been used to induce lactation in cycling and noncycling mares (0.5-1 mg/kg twice a day) [7] or to hasten the first ovulation of the breeding season in noncycling mares (1 mg/kg once a day) [8][9][10][11].…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetic Evaluations of Sulpiride After Intravenous, Intramuscular, and Oral Single-Dose Administration in Jennies (Equus asinus)

Giorgi¹,

Vullo²,

Vito³

et al. 2015

Journal of Equine Veterinary Science

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a b s t r a c tSulpiride is an antipsychotic human drug. It is commonly used to encourage ovulation in noncycling mares and to stimulate lactation in adoptive mares. No pharmacokinetic data are available for donkeys. The aim of this study was to assess the pharmacokinetics profile of sulpiride after intravenous (IV), intramuscular (IM), and oral (PO) administrations in healthy jennies. Animals (n ¼ 6) were treated with sulpiride, 1 mg/kg by IV, IM, and PO routes according to a randomized cross-over design (3 Â 3 Latin square). Blood samples (5 mL) were collected at predetermined times and analyzed using a validated high performance liquid chromatography with fluorescence detection method. IV and IM administrations gave similar curves, but they were not bioequivalent. The IM average bioavailability was 73.5%. After PO administration, the drug plasma concentrations were low and consequently both area under the curve and bioavailability (9.4%) were low. This finding could be because of the physicochemical features of the drug. Indeed, considering that sulpiride is a weak base, existing in the ionized form at gastric and physiological pH, it is unsurprising that it is poorly absorbable, especially in equine species whose gastric pH is particularly acidic. In conclusion, injective routes are definitely preferable to PO dosing because of the very low F% via this route.

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Section: Discussionsupporting

confidence: 92%

Section: Resultsmentioning

confidence: 99%

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Pharmacokinetic Evaluations of Sulpiride After Intravenous, Intramuscular, and Oral Single-Dose Administration in Jennies (Equus asinus)

Giorgi¹,

Vullo²,

Vito³

et al. 2015

Journal of Equine Veterinary Science

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“…In order to compare the pharmacokinetics of LSP at a dose of 50 mg (irrespective of the animal body weight), a 3 × 3 cross-over study was carried out, so that at the end of the study each animal had been given the drug by each of the three different routes. The dose range was 1.29-1.92 mg/kg in line with the range (0.5-2 mg/kg) reported in earlier studies on its racemate sulpiride (Daels, Fatone, Hansen, & Concannon, 2000;Duchamp & Daels, 2002;Giorgi et al, 2013Giorgi et al, , 2015Guillaume et al, 2003;Mari et al, 2009;Panzani et al, 2011) to stimulate ovulation/lactation and evaluate the pharmacokinetics in veterinary species.…”

Section: Discussionsupporting

confidence: 71%

Pharmacokinetics of levosulpiride after single‐dose administration in goats (Capra hircus) by different routes of administration

Łebkowska‐Wieruszewska

Barsotti

Camillo

et al. 2019

Vet Pharm & Therapeutics

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Levosulpiride (LSP) is the l‐enantiomer of sulpiride, and LSP recently replacing sulpiride in several EU countries. Several studies about LSP in humans are present in the literature, but neither pharmacodynamic nor pharmacokinetic data of LSP is present for veterinary species. The aim of this study was to assess the pharmacokinetic profile of LSP after intravenous (IV), intramuscular (IM), and oral (PO) administration in goats. Animals (n = 6) were treated with 50 mg LSP by IV, IM, and PO routes according to a randomized cross‐over design (3 × 3 Latin‐square). Blood samples were collected prior and up to 24 hr after LSP administration and quantified using a validated HPLC method with fluorescence detection. IV and IM administration gave similar concentration versus time curve profiles. The IM mean bioavailability was 66.97%. After PO administration, the drug plasma concentrations were detectable only in the time range 1.5–4 hr, and the bioavailability (4.73%) was low. When the AUC was related to the administered dose in mg/kg, there was a good correlation in the IV and IM groups, but very low correlation for the PO route. In conclusion, the IM and IV administrations result in very similar plasma concentrations. Oral dosing of LSP in goats is probably not viable as its oral bioavailability was very low.

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“…These latter results were similar to those reported by Donadeu and Thompson [89], in which daily treatment of seasonally anovulatory mares from January 14 to February 14 with sulpiride did not stimulate ovarian size or activity, although prolactin concentrations were increased and hair shedding was stimulated relative to control mares. Panzani et al [93] treated mares with sulpiride for 21 days when the first follicle of 25 mm or larger was attained (transitional mares) and reported that treatment hastened first ovulation by 25 days (median of 18 days for treated mares and 43 for controls).…”

Section: Induction Of Ovarian Activity and Ovulation In Wintermentioning

confidence: 99%

Prolactin in the Horse: Historical Perspective, Actions and Reactions, and Its Role in Reproduction

Thompson

Oberhaus

2015

Journal of Equine Veterinary Science

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Clinical use of dopamine antagonist sulpiride to advance first ovulation in transitional mares

Cited by 31 publications

References 15 publications

Pharmacokinetic Evaluations of Sulpiride After Intravenous, Intramuscular, and Oral Single-Dose Administration in Jennies (Equus asinus)

Pharmacokinetic Evaluations of Sulpiride After Intravenous, Intramuscular, and Oral Single-Dose Administration in Jennies (Equus asinus)

Pharmacokinetics of levosulpiride after single‐dose administration in goats (Capra hircus) by different routes of administration

Prolactin in the Horse: Historical Perspective, Actions and Reactions, and Its Role in Reproduction

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