Misoprostol is a synthetic prostaglandin E1 analogue used in equine medicine primarily for its gastroprotective properties. It is employed to manage and prevent gastric ulcers in horses by promoting mucosal blood flow and enhancing mucus and bicarbonate secretion in the gastrointestinal tract. Misoprostol is also investigated for its effects on reducing inflammation and modulating immune responses in equine patients. This page compiles peer-reviewed research studies and scholarly articles that explore the pharmacological effects, therapeutic applications, and safety considerations of misoprostol use in horses.
Kimura S, McCoy AM, Boothe DM, Wooldridge AA, Graff E, Hammack SM, Cresci L, Hofmeister E, Lascola KM.To describe misoprostol pharmacokinetics and anti-inflammatory efficacy when administered orally or per rectum in endotoxin-challenged horses. Methods: 6 healthy geldings. Methods: A randomized 3-treatment crossover design was performed with a minimum washout period of 28 days between treatment arms. Prior to endotoxin challenge (lipopolysaccharide, 30 ng/kg IV over 30 minutes), horses received misoprostol (5 µg/kg once) per os (M-PO) or per rectum (M-PR) or water as control (CON). Clinical parameters were evaluated and blood samples obtained to measure plasma misoprostol free acid concentrat...
Lopp CT, McCoy AM, Boothe D, Schaeffer DJ, Lascola K.To characterize the pharmacokinetics of a clinically relevant dose of misoprostol administered PO or per rectum (PR) to horses. Methods: 8 healthy adult horses. Methods: In a randomized 3-way crossover design, horses received a single dose of misoprostol (5 μg/kg) administered PO (with horses fed and unfed) and PR, with a minimum 3-week washout period separating the experimental conditions. Blood samples were obtained before and at various points after drug administration (total, 24 hours), and plasma concentrations of misoprostol free acid were measured. Results: Mean maximum plasma concentr...
Varley G, Bowen IM, Habershon-Butcher JL, Nicholls V, Hallowell GD.Previous studies have demonstrated a poor response to healing of gastric glandular lesions with oral omeprazole and other medications. Objective: To evaluate the efficacy of two novel treatments (misoprostol [M] and combined omeprazole-sucralfate [OS]) in horses for gastric glandular disease. Methods: Prospective, clinical study. Methods: Sixty-three sports horses with grade >1/4 glandular disease were identified by gastroscopy. Horses received either 5 μg/kg of misoprostol per os BID 1 h prior to feeding or a combination of 4 mg/kg enteric coated omeprazole per os SID and 12 mg/kg sucral...
Martin EM, Messenger KM, Sheats MK, Jones SL.Pro-inflammatory cytokines including tumor necrosis factor α (TNFα), IL-1β, IL-6, and IL-8 are potent immune mediators that exacerbate multiple equine diseases such as sepsis and laminitis. Unfortunately, safe and effective cytokine-targeting therapies are lacking in horses; therefore, novel mechanisms of inhibiting cytokine production are critically needed. One potential mechanism for inhibiting cytokine synthesis is elevation of intracellular cyclic AMP (cAMP). In human leukocytes, intracellular cAMP production is induced by activation of E-prostanoid (EP) receptors 2 and 4. These recepto...
Martin EM, Till RL, Sheats MK, Jones SL.In many equine inflammatory disease states, neutrophil activities, such as adhesion, migration, and reactive oxygen species (ROS) production become dysregulated. Dysregulated neutrophil activation causes tissue damage in horses with asthma, colitis, laminitis, and gastric glandular disease. Non-steroidal anti-inflammatory drugs do not adequately inhibit neutrophil inflammatory functions and can lead to dangerous adverse effects. Therefore, novel therapies that target mechanisms of neutrophil-mediated tissue damage are needed. One potential neutrophil-targeting therapeutic is the PGE1 analog, m...
Jacobson CC, Sertich PL, Mc Donnell SM.To investigate effects of a 5-day oral misoprostol regimen recommended for use in horses as a gastrointestinal mucosal cytoprotectant during colic on mid-gestation pregnancies. Objective: To monitor cervical tone, ultrasonographic characteristics of the uterus, cervix and conceptus, as well as serum progesterone and oestrone sulphate concentrations, and observations of general health, behaviour and comfort of mid-gestation mares given a 5-day course of misoprostol or control treatment. Methods: Eleven light horse and pony mares with known breeding dates were administered 5 µg/kg bwt misoprost...
Aleman M, Nieto JE, Higgins JK.A 15-year-old Quarter Horse gelding and a 26-year-old Thoroughbred gelding were evaluated because of hematuria of 4 to 6 days' duration following prolonged oral administration of phenylbutazone. Results: The horses had received either treatment with phenylbutazone for 3 months or intermittent long-term phenylbutazone treatment prior to development of hematuria. Each horse was systemically stable but had orthopedic or neurologic problems. Clinicopathologic findings included normochromic normocytic anemia in both horses and hypoalbuminemia and high BUN concentration in 1 horse. In both horses, u...
Sangiah S, MacAllister CC, Amouzadeh HR.The basal gastric pH and free acid contents from five young adult healthy horses were determined at one hour intervals for eight hours. The basal gastric pH and free acid contents varied from 1.63 +/- 0.06 to 1.97 +/- 0.11 and 26.42 +/- 4.14 to 17.92 +/- 5.28 mmol litre-1, respectively. Misoprostol, a methylester analogue of prostaglandin (5 micrograms kg-1, orally) produced a time-dependent increase in the basal gastric pH to above 3.5 (P less than 0.05) at three, four and five hours after administration with a concomitant reduction of 80 to 90 per cent in the basal gastric free acid contents...
Varley G, Bowen IM, Habershon-Butcher JL, Nicholls V, Hallowell GD.Previous studies have demonstrated a poor response to healing of gastric glandular lesions with oral omeprazole and other medications. Objective: To evaluate the efficacy of two novel treatments (misoprostol [M] and combined omeprazole-sucralfate [OS]) in horses for gastric glandular disease. Methods: Prospective, clinical study. Methods: Sixty-three sports horses with grade >1/4 glandular disease were identified by gastroscopy. Horses received either 5 μg/kg of misoprostol per os BID 1 h prior to feeding or a combination of 4 mg/kg enteric coated omeprazole per os SID and 12 mg/kg sucral...
Martin EM, Messenger KM, Sheats MK, Jones SL.Pro-inflammatory cytokines including tumor necrosis factor α (TNFα), IL-1β, IL-6, and IL-8 are potent immune mediators that exacerbate multiple equine diseases such as sepsis and laminitis. Unfortunately, safe and effective cytokine-targeting therapies are lacking in horses; therefore, novel mechanisms of inhibiting cytokine production are critically needed. One potential mechanism for inhibiting cytokine synthesis is elevation of intracellular cyclic AMP (cAMP). In human leukocytes, intracellular cAMP production is induced by activation of E-prostanoid (EP) receptors 2 and 4. These recepto...
Sangiah S, MacAllister CC, Amouzadeh HR.The basal gastric pH and free acid contents from five young adult healthy horses were determined at one hour intervals for eight hours. The basal gastric pH and free acid contents varied from 1.63 +/- 0.06 to 1.97 +/- 0.11 and 26.42 +/- 4.14 to 17.92 +/- 5.28 mmol litre-1, respectively. Misoprostol, a methylester analogue of prostaglandin (5 micrograms kg-1, orally) produced a time-dependent increase in the basal gastric pH to above 3.5 (P less than 0.05) at three, four and five hours after administration with a concomitant reduction of 80 to 90 per cent in the basal gastric free acid contents...
Aleman M, Nieto JE, Higgins JK.A 15-year-old Quarter Horse gelding and a 26-year-old Thoroughbred gelding were evaluated because of hematuria of 4 to 6 days' duration following prolonged oral administration of phenylbutazone. Results: The horses had received either treatment with phenylbutazone for 3 months or intermittent long-term phenylbutazone treatment prior to development of hematuria. Each horse was systemically stable but had orthopedic or neurologic problems. Clinicopathologic findings included normochromic normocytic anemia in both horses and hypoalbuminemia and high BUN concentration in 1 horse. In both horses, u...
Jacobson CC, Sertich PL, Mc Donnell SM.To investigate effects of a 5-day oral misoprostol regimen recommended for use in horses as a gastrointestinal mucosal cytoprotectant during colic on mid-gestation pregnancies. Objective: To monitor cervical tone, ultrasonographic characteristics of the uterus, cervix and conceptus, as well as serum progesterone and oestrone sulphate concentrations, and observations of general health, behaviour and comfort of mid-gestation mares given a 5-day course of misoprostol or control treatment. Methods: Eleven light horse and pony mares with known breeding dates were administered 5 µg/kg bwt misoprost...
Kimura S, McCoy AM, Boothe DM, Wooldridge AA, Graff E, Hammack SM, Cresci L, Hofmeister E, Lascola KM.To describe misoprostol pharmacokinetics and anti-inflammatory efficacy when administered orally or per rectum in endotoxin-challenged horses. Methods: 6 healthy geldings. Methods: A randomized 3-treatment crossover design was performed with a minimum washout period of 28 days between treatment arms. Prior to endotoxin challenge (lipopolysaccharide, 30 ng/kg IV over 30 minutes), horses received misoprostol (5 µg/kg once) per os (M-PO) or per rectum (M-PR) or water as control (CON). Clinical parameters were evaluated and blood samples obtained to measure plasma misoprostol free acid concentrat...
Lopp CT, McCoy AM, Boothe D, Schaeffer DJ, Lascola K.To characterize the pharmacokinetics of a clinically relevant dose of misoprostol administered PO or per rectum (PR) to horses. Methods: 8 healthy adult horses. Methods: In a randomized 3-way crossover design, horses received a single dose of misoprostol (5 μg/kg) administered PO (with horses fed and unfed) and PR, with a minimum 3-week washout period separating the experimental conditions. Blood samples were obtained before and at various points after drug administration (total, 24 hours), and plasma concentrations of misoprostol free acid were measured. Results: Mean maximum plasma concentr...
Martin EM, Till RL, Sheats MK, Jones SL.In many equine inflammatory disease states, neutrophil activities, such as adhesion, migration, and reactive oxygen species (ROS) production become dysregulated. Dysregulated neutrophil activation causes tissue damage in horses with asthma, colitis, laminitis, and gastric glandular disease. Non-steroidal anti-inflammatory drugs do not adequately inhibit neutrophil inflammatory functions and can lead to dangerous adverse effects. Therefore, novel therapies that target mechanisms of neutrophil-mediated tissue damage are needed. One potential neutrophil-targeting therapeutic is the PGE1 analog, m...
