去氧皮質酮特戊酸酯 (DOCP)
**去氧皮質酮特戊酸酯 (DOCP)** 是一種長效注射型**鹽皮質激素**,主要用於治療犬貓的典型腎上腺皮質機能減退症(愛迪生氏症)。 * **臨床要點:** 與氟氫可的松 (fludrocortisone) 不同,DOCP **完全沒有**糖皮質激素活性。因此,接受 DOCP 治療的患畜必須同時補充糖皮質激素(例如生理劑量的潑尼松或氫化可的松),特別是在面臨壓力或生病期間。 * 它被配製成微結晶儲庫型懸浮液,使其能緩慢溶解並具有延長的作用時間(通常為 21-30 天)。
作用機制: DOCP acts as an exogenous analog of aldosterone. * **Target Site:** Acts primarily at the **renal distal tubule** and collecting ducts. * **Mechanism:** Binds to mineralocorticoid receptors → upregulates **Na+/K+ ATPase** pumps and epithelial sodium channels (ENaC) → increases the absorption of **sodium (Na+)** and enhances **potassium (K+)** and **hydrogen (H+)** ion excretion. * **Requirement:** To be effective, mineralocorticoids require a functioning kidney.
各物種劑量
- Maintenance therapy of hypoadrenocorticism · 2.2 mg/kg IM every 25 days plus prednisolone (0.25-1 mg/cat PO twice daily; if daily oral dosing not feasible, may give 10 mg of methylprednisolone acetate once a month IM) · IM · q25d
- Maintenance therapy of hypoadrenocorticism · 10-12.5 mg (total dose) IM per month. Adjust dose based-upon follow-up serum electrolyte concentrations monitored every 1-2 weeks during initial maintenance period. Normal electrolyte values 2 weeks following injection, suggests adequate dosing, but does not provide information regarding duration of action. Prednisone at 1.25 mg PO once a day or IM methylprednisolone acetate 10 mg once a month can provide long-term glucocorticoid supplementation. · IM · monthly
- Hypoadrenocorticism · 2.2 mg/kg IM every 25 days · IM · q25d · Dosage requirements are variable and should be individualized to the patient.
- Hypoadrenocorticism · Initially, inject 2.2 mg/kg IM or SC every 25 days. Reevaluate at 12 and 25 days after initial injection. If hyponatremia and/or hyperkalemia are noted at 12 days, increase dose by 10%. If they are noted at 25 days (but not on day 12), shorten dosing interval by 2 days. · IM/SC · q25d
- Hypoadrenocorticism · 1.5-2.2 mg/kg IM q20-30 days · IM · q20-30d
- Hypoadrenocorticism · Initially, 2.2 mg/kg IM q25 days. If electrolytes remain in normal range at 30 days, reduce dose by 10% a month. In our clinic, we have used a dose of DOCP as low as 1 mg/kg q30 days with good control of hypoadrenocorticism. · IM · q25-30d
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給藥途徑
禁忌症
- Congestive heart failure
- Severe renal disease
- Edema
不良反應
- Injection site irritation
- Polyuria (PU)
- Polydipsia (PD)
- Hypernatremia
- Hypokalemia
- Hypertension
- Edema
- Weight gain (fluid retention)
藥物相互作用
- Amphotericin B · Patients may develop hypokalemia if mineralocorticoids are administered concomitantly.
- Aspirin · DOCP may reduce salicylate levels.
- Digoxin · Because DOCP may cause hypokalemia, it should be used with caution and increased monitoring when used in patients receiving digitalis glycosides.
- Insulin · Potentially, DOCP could increase the insulin requirements of diabetic patients.
- Potassium-depleting diuretics (e.g., furosemide, thiazides) · Patients may develop hypokalemia if administered concomitantly; as diuretics can cause a loss of sodium, they may counteract the effects of DOCP.
監測
- Serum electrolytes (Na+, K+)
- BUN and Creatinine (initially every 1-2 weeks, then once stabilized, every 3-4 months)
- Body weight
- Physical examination for edema
過量
Overdosage may cause polyuria, polydipsia, hypernatremia, hypertension, edema, and hypokalemia. Cardiac enlargement is possible with prolonged overdoses. Excessive weight gain may be indicative of fluid retention secondary to sodium retention. **Treatment:** * Electrolytes should be aggressively monitored. * Potassium may need to be supplemented. * Discontinue the drug in patients until clinical signs associated with overdosage have resolved, then restart the drug at a lower dosage.
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