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Omeprazole Oral Paste
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Detailed description
Omeprazole Oral Paste
For Veterinary Use
[Main Ingredient] Omeprazole.
[Description] A light yellow to brownish-yellow semi-solid paste.
[Pharmacological Action] Proton pump inhibitor.
Pharmacodynamics: This product is a lipophilic weak base that readily accumulates in acidic environments. After oral administration, it is specifically distributed to the secretory canaliculi of gastric parietal cells, where it is converted to the active sulfenamide form under the highly acidic conditions. It then forms an irreversible disulfide bond with the sulfhydryl group of the H^+^-K^+^-ATPase (proton pump) in the secretory membrane, generating a sulfenamide‑proton pump complex, thereby inhibiting enzyme activity and blocking the final step of gastric acid secretion. However, the steady‑state plasma concentration of omeprazole is not correlated with the amount bound to H^+^-K^+^-ATPase. The relationship between omeprazole and plasma concentration is a rate‑limiting function of the activity/turnover of the enzyme. Only after all enzymes are bound to the drug can acid secretion be restored by synthesis of new H^+^-K^+^-ATPase in parietal cells (i.e., the rate of new enzyme synthesis exceeds the inhibition rate). In gastric intubation pharmacodynamic studies, daily administration of 4 mg/kg inhibited gastric acid secretion in horses. After maximal inhibition of acid secretion was reached (day 5), actual acid secretion was reduced by 99%, 95%, and 90% at 8, 16, and 24 hours, respectively.
Pharmacokinetics: Omeprazole oral paste shows significant first‑pass effect after oral administration, with rapid absorption, wide distribution, and rapid elimination. It is mainly excreted via urine and a small portion via feces. No accumulation has been observed after repeated administration. Absorption in horses is reduced by approximately half in the fed state compared to the fasted state, but elimination rate is not affected. In 18 healthy Mongolian horses under fasted conditions, a single dose of omeprazole oral paste (4 mg/kg as omeprazole) was administered; individual pharmacokinetic parameters (AUC~0-t~, C~max~ and t~max~) indicated high intra‑individual variability in the rate and extent of absorption. The time to peak (t~max~) was 1.64±0.94 h, peak plasma concentration (C~max~) was 142.89±38.70 ng/ml, half‑life (t~1/2~) was 2.28±1.67 h, and area under the plasma concentration‑time curve (AUC~0-t~) was 505.38±140.68 ng·h/ml.
[Drug Interactions]
This product may delay the elimination of drugs metabolized by the liver, such as diazepam, phenytoin sodium, warfarin, nifedipine, etc. When used concomitantly with these drugs, the dosage of the latter should be reduced.
[Indications] For the treatment of gastric ulcers in adult horses and foals aged 4 weeks and older, and for the prevention of recurrence of gastric ulcers.
[Dosage and Administration]
Calculated as omeprazole. Oral administration: for treatment of gastric ulcers in horses, 4 mg per kg body weight once daily for 4 consecutive weeks; for prevention of recurrence, 2 mg per kg body weight once daily for at least an additional 4 weeks following the treatment course.
[Adverse Reactions] No adverse reactions have been observed at the recommended dosage and administration.
[Precautions] 1. Do not use in horses intended for human consumption.
2.Safety in pregnant or lactating mares has not been established.
3.Keep out of reach of children; in case of accidental ingestion, seek medical attention and show this package insert.
[Withdrawal Period] Not required.
[Strengths] 6.16 g : 2.279 g
[Packaging] Polypropylene pre-filled syringe, 6.16 g/syringe
[Storage] Keep sealed.
[Shelf Life] 24 months.
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