์ค๋ฉํ๋ผ์กธ
์ค๋ฉํ๋ผ์กธ์ ์์ํ์์ ์์ญ์ด์ง์ฅ ๊ถค์ ๋ฐ ๋ฏธ๋์ ์น๋ฃ์ ์๋ฐฉ์ ๋๋ฆฌ ์ฌ์ฉ๋๋ ๋งค์ฐ ํจ๊ณผ์ ์ธ **ํ๋กํค ํํ ์ต์ ์ (PPI)**์ ๋๋ค. * **์ฐ์ํ ํจ๋ฅ:** ์๋์ค์นด ์ฐ๋งค๊ฒฌ์ ์ด๋ ์ ๋ฐ์ฑ ์์ผ ์๋ฐฉ ์ฐ๊ตฌ์์ ์ ์ฆ๋์๋ฏ, ์๋ด pH๋ฅผ ๋์ด๋ ๋ฐ ์์ด H2 ์์ฉ์ฒด ๊ธธํญ์ (์: ํ๋ชจํฐ๋)๋ณด๋ค ์ฐ์ํ ๊ฒ์ผ๋ก ๊ฐ์ฃผ๋ฉ๋๋ค. * **๋ง์์์ ์ฌ์ฉ:** ๊ฒฝ๊ตฌ์ฉ ํ์ด์คํธ ์ ์ ๋ ๋ง์ ์๊ถค์(EGUS) ์น๋ฃ ๋ฐ ์๋ฐฉ์ฉ์ผ๋ก ์น์ธ๋์์ผ๋ฉฐ ๋งค์ฐ ํจ๊ณผ์ ์ ๋๋ค. * **๊ด๋ฒ์ํ ์ ์ฉ:** ๊ฐ, ๊ณ ์์ด, ํ๋ฟ, ๋ผ์ง ๋ฑ ๋ค์ํ ์ข ์์ ์๋ ์ฑ ์๋ณ์ฆ, ์๋์ผ, ํฌ๋ฆฌ์ฝ๋ฐํฐ ๊ฐ์ผ, NSAID/์ฝ๋ฅดํฐ์ฝ์คํ ๋ก์ด๋ ์ ๋ฐ์ฑ ๊ถค์ ๋ฑ์ ๊ด๋ฆฌํ๋ ๋ฐ ์ฌ์ฉ๋ฉ๋๋ค. > **์์ ํ:** ์ค๋ฉํ๋ผ์กธ์ ํ์ฑํ๋ฅผ ์ํด ์ฐ์ฑ ํ๊ฒฝ์ด ํ์ํ์ง๋ง ํก์ ์ ์์ฐ์ ์ํด ๋ถํด๋ ์ ์์ผ๋ฏ๋ก ์ธ์ฒด์ฉ ๊ฒฝ๊ตฌ ์ ์ ๋ ์ฅ์ฉ ์ฝํ ์ด ๋์ด ์์ต๋๋ค. ์ฝ๋ฌผ์ ์์ฒด ์ด์ฉ๋ฅ ์ ํ๊ดดํ ์ ์์ผ๋ฏ๋ก **์ ๋ ๋ถ์๊ฑฐ๋ ์น์ด์ ๋จน์ฌ์๋ ์ ๋ฉ๋๋ค**.
์์ฉ ๊ธฐ์ : Omeprazole is a **prodrug** that acts as a substituted benzimidazole gastric acid pump inhibitor. 1. **Absorption & Distribution:** After absorption, it diffuses from the blood into the highly acidic secretory canaliculi of the gastric **parietal cells**. 2. **Activation:** In this acidic environment (pH < 3), it is protonated and rearranged into its active form, a **sulphenamide derivative**. 3. **Irreversible Binding:** The active sulphenamide binds **irreversibly** via disulfide bonds to the **Hโบ/Kโบ ATPase enzyme** (the proton pump) at the secretory surface. 4. **Acid Suppression:** This blocks the final common pathway of gastric acid secretion, inhibiting the transport of hydrogen ions into the stomach lumen during both basal and stimulated conditions. > **Pharmacological Note:** Because the binding is irreversible, acid secretion only resumes when new Hโบ/Kโบ ATPase enzymes are synthesized. This explains why its duration of action (24-72 hours) far outlasts its short plasma half-life (~1 hour). Omeprazole also inhibits the hepatic **cytochrome P-450** mixed-function oxidase system, which can lead to drug interactions.
๋๋ฌผ ์ข ๋ณ ์ฉ๋
- Adjunctive treatment of esophagitis or gastric ulcers ยท 0.5-1 mg/kg PO q24h ยท PO ยท q24h
- GI ulcer management/prevention ยท 0.7-1.5 mg/kg PO q12-24h ยท PO ยท q12h-q24h
- Adjunctive treatment of uremic gastropathy ยท 0.7 mg/kg PO q24h ยท PO ยท q24h ยท Dosage may need to be modified in moderate or severe renal failure.
- Short-term treatment of gastroenteritis ยท 0.7 mg/kg PO q24h ยท PO ยท q24h ยท Short-term
- Treatment of gastric ulcers ยท 4 mg/kg PO once daily for 4 weeks; to prevent recurrence treat for at least another 4 weeks at 2 mg/kg PO once daily ยท PO ยท q24h ยท 8 weeks total ยท ARCI UCGFS Class 5 Drug
- Foals: Preventative dose ยท 1 mg/kg PO q24h ยท PO ยท q24h ยท There has been a recent shift to not administering prophylactic antiulcer medication routinely to sick foals.
- Foals: Treatment dose ยท 4 mg/kg PO q24h ยท PO ยท q24h ยท Will reduce gastric pH in a few hours.
- Treatment or prophylaxis of gastric ulcers in foals ยท 4 mg/kg PO once daily for treatment, 1-2 mg/kg PO once daily for prophylaxis ยท PO ยท q24h
- Foals: Gastric ulcers ยท 4 mg/kg PO q24h ยท PO ยท q24h ยท Commonly foals will be started on ranitidine (1.5 mg/kg IV q8h; 6.6 mg/kg PO q8h) and omeprazole together.
ํฌ์ฌ ๊ฒฝ๋ก
๊ธ๊ธฐ
- Known hypersensitivity to omeprazole
์ด์๋ฐ์
- GI distress (anorexia, colic, nausea, vomiting, flatulence, diarrhea)
- Hematologic abnormalities (rare)
- Urinary tract infections
- Proteinuria
- CNS disturbances
- Urticaria (rare in horses)
์ฝ๋ฌผ ์ํธ์์ฉ
- Benzodiazepines (e.g., diazepam) ยท Omeprazole may potentially alter benzodiazepine metabolism and prolong CNS effects
- Clarithromycin ยท Increased levels of omeprazole, clarithromycin and 14-hydroxyclarithromycin are possible
- Cyanocobalamin (oral) ยท Omeprazole may decrease oral absorption
- Cyclosporine ยท Omeprazole may reduce cyclosporine metabolism
- Ketoconazole, Itraconazole, Iron, Ampicillin esters ยท Omeprazole increases gastric pH, which may decrease the absorption of these drugs that require an acidic environment
- Warfarin ยท Omeprazole may increase anticoagulant effect
๋ชจ๋ํฐ๋ง
- Clinical efficacy (resolution of clinical signs of ulcers/esophagitis)
- Adverse effects (GI distress)
- Liver enzymes (may increase)
- Serum gastrin levels (will increase early in therapy)
๊ณผ์ฉ๋
The LD50 in rats after oral administration is reportedly >4 grams/kg. Humans have tolerated oral dosages of 360 mg/day without significant toxicity. Should a massive overdose occur, treat symptomatically and supportively. Due to its wide safety margin, acute toxicity from accidental ingestion is generally mild.
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