Spiramycin concentrations in plasma and genital‐tract secretions after intravenous administration in the ewe*

Cester, C. C.; Laurentie, Michel; Garcia‐Villar, R.; Toutain, P. L.

doi:10.1111/j.1365-2885.1990.tb00741.x

Cited by 7 publications

(5 citation statements)

References 5 publications

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“…In addition, the clearance (Cl_obs) value of spiramycin obtained from this research (0.68 L/h/kg) was in line with that found in ewes (0.757 L/h/kg) [ 12 ]. However, this value was lower than that published for cows (1.18 L/h/kg) [ 7 ], and pigs (2.6 L/h/kg) [ 11 ] receiving IV spiramycin at 10 mg/kg.…”

Section: Discussionsupporting

confidence: 84%

“…The high lipid solubility and the moderate plasma protein binding features of spiramycin are probably the main reasons beyond its high Vz. However, the value found for Vz in this study was lower than that reported in pigs (5.6 L/Kg) receiving IV spiramycin at 10 mg/kg [ 11 ], ewes (16.56 L/kg) receiving IV spiramycin at 20 mg/kg [ 12 ], calves (23.5 L/kg) receiving spiramycin IV at 15 mg/kg [ 34 ], and cattle (11.97 L/Kg) receiving spiramycin IV at 15.6 mg/kg [ 35 ].…”

Section: Discussioncontrasting

confidence: 77%

“…Similar to other macrolides, spiramycin is recognized by its high tissue distribution [ 9 ]. The pharmacokinetics (PK) of spiramycin have been assessed in cattle [ 7 , 10 ], pigs [ 11 ], ewes [ 12 ], and monkeys [ 13 ]. To date, no reports exist concerning the PK of spiramycin in chickens, despite the fact that it is efficacious in the control of mycoplasmosis in this species [ 8 ].…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetic/Pharmacodynamic Modeling of Spiramycin against Mycoplasma synoviae in Chickens

et al. 2021

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This research aimed to assess the pharmacokinetics/pharmacodynamics (PK/PD) and tissue residues of spiramycin in chickens. The PK of spiramycin were determined in 12 chickens using a parallel study design in which each group of chickens (n = 6) received a single dose of spiramycin at 17 mg/kg intravenously (IV) or orally. Plasma samples were collected at assigned times for up to 48 h to measure spiramycin concentrations. Additionally, a tissue depletion study was performed in 42 chickens receiving spiramycin at 17 mg/kg/day orally for 7 days. The area under the plasma concentration–time curve values were 29.94 ± 4.74 and 23.11 ± 1.83 µg*h/mL after IV and oral administrations, respectively. The oral bioavailability was 77.18%. The computed withdrawal periods of spiramycin were 11, 10, and 7 days for liver, muscle, and skin and fat, respectively. The minimum inhibitory concentration for spiramycin against Mycoplasma synoviae (M. synoviae) strain 1853 was 0.0625 µg/mL. Using the PK/PD integration, the appropriate oral dose of spiramycin against M. synoviae was estimated to be 15.6 mg/kg. Thus, we recommend an oral dose of 15.6 mg spiramycin/kg against M. synoviae in chickens and a withdrawal period of 11 days following oral treatment with 17 mg spiramycin/kg/day for 7 days.

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Section: Discussionsupporting

confidence: 84%

Section: Discussioncontrasting

confidence: 77%

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetic/Pharmacodynamic Modeling of Spiramycin against Mycoplasma synoviae in Chickens

et al. 2021

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“…In ruminants the volume of distribution is higher. Cester et al . (1990) found in ewes a volume of distribution of 16.56 L/kg body weight and Friis et al .…”

Section: Discussionmentioning

confidence: 99%

Bioavailability of spiramycin and lincomycin after oral administration to fed and fasted pigs

Nielsen

Gyrd‐Hansen

1998

Vet Pharm & Therapeutics

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The disposition of spiramycin and lincomycin was measured after intravenous (i.v.) and oral (p.o.) administration to pigs. Twelve healthy pigs (six for each compound) weighing 16-43 kg received a dose of 10 mg/kg intravenously, and 55 mg/kg (spiramycin) or 33 mg/kg (lincomycin) orally in both a fasted and a fed condition in a three-way cross-over design. Spiramycin was detectable in plasma up to 30 h after intravenous and oral administration to both fasted and fed pigs, whereas lincomycin was detected for only 12 h after intravenous administration and up to 15 h after oral administration. The volume of distribution was 5.6 +/- 1.5 and 1.1 +/- 0.2 L/kg body weight for spiramycin and lincomycin, respectively. For both compounds the bioavailability was strongly dependent on the presence of food in the gastrointestinal tract. For spiramycin the bioavailability was determined to be 60% and 24% in fasted and fed pigs, respectively, whereas the corresponding figures for lincomycin were 73% and 41%. The maximum plasma concentration of spiramycin (Cmax) was estimated to be 5 microg/mL in fasted pigs and 1 microg/mL only in fed pigs. It is concluded that an oral dose of 55 mg/kg body weight is not enough to give a therapeutically effective plasma concentration of spiramycin against species of Mycoplasma, Streptococcus, Staphylococcus and Pasteurella multocida. The maximum plasma concentration of lincomycin was estimated to be 8 microg/mL in fasted pigs and 5 microg/mL in fed pigs, but as the minimum inhibitory concentration for lincomycin against Actinobacillus pleuropneumoniae and P. multocida is higher than 32 microg/mL a therapeutically effective plasma concentration could not be obtained following oral administration of the drug. For Mycoplasma the MIC90 is below 1 microg/mL and a therapeutically effective plasma concentration of lincomycin was thus obtained after oral administration to both fed and fasted pigs.

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“…Along that line, dose response and drug stability experiments are needed to evaluate the potential of SorA for systemic application against Chlamydia [40]. However, SorA may also just not be secreted to the female genital tract after systemic antibiotic application, as other antibiotic investigations showed that plasma concentrations would not always be indicative of the antibiotic efficacy in the target tissue [41]. In principle, intraperitoneally applied SorA is systemically transported and active, which could be proven by analyzing the stool microbiota of these animals.…”

Section: Discussionmentioning

confidence: 99%

Sorangicin A Is Active against Chlamydia in Cell Culture, Explanted Fallopian Tubes, and Topical In Vivo Treatment

et al. 2023

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Current treatment of Chlamydia trachomatis using doxycycline and azithromycin introduces detrimental side effects on the host’s microbiota. As a potential alternative treatment, the myxobacterial natural product sorangicin A (SorA) blocks the bacterial RNA polymerase. In this study we analyzed the effectiveness of SorA against C. trachomatis in cell culture, and explanted fallopian tubes and systemic and local treatment in mice, providing also pharmacokinetic data on SorA. Potential side effects of SorA on the vaginal and gut microbiome were assessed in mice and against human-derived Lactobacillus species. SorA showed minimal inhibitory concentrations of 80 ng/mL (normoxia) to 120 ng/mL (hypoxia) against C. trachomatis in vitro and was eradicating C. trachomatis at a concentration of 1 µg/mL from fallopian tubes. In vivo, SorA reduced chlamydial shedding by more than 100-fold within the first days of infection by topical application corresponding with vaginal detection of SorA only upon topical treatment, but not after systemic application. SorA changed gut microbial composition during intraperitoneal application only and did neither alter the vaginal microbiota in mice nor affect growth of human-derived lactobacilli. Additional dose escalations and/or pharmaceutical modifications will be needed to optimize application of SorA and to reach sufficient anti-chlamydial activity in vivo.

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Spiramycin concentrations in plasma and genital‐tract secretions after intravenous administration in the ewe*

Cited by 7 publications

References 5 publications

Pharmacokinetic/Pharmacodynamic Modeling of Spiramycin against Mycoplasma synoviae in Chickens

Pharmacokinetic/Pharmacodynamic Modeling of Spiramycin against Mycoplasma synoviae in Chickens

Bioavailability of spiramycin and lincomycin after oral administration to fed and fasted pigs

Sorangicin A Is Active against Chlamydia in Cell Culture, Explanted Fallopian Tubes, and Topical In Vivo Treatment

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