雙氯芬胺
**雙氯芬胺 (Dichlorphenamide)** 是一種全身性**碳酸酐酶抑制劑 (CAI)**,傳統上在獸醫眼科中用於**青光眼**的內科治療。 * **臨床要點**:由於顯著的全身性副作用(如代謝性酸中毒和低血鉀)以及市面上普遍缺貨,全身性 CAI 已在很大程度上被局部替代藥物(如**多佐胺 (dorzolamide)** 和 **布林佐胺 (brinzolamide)**)所取代。 * 目前若需開立此藥,通常需要透過調劑藥局 (compounding pharmacy) 取得。 * 它具有輕微的抗癲癇和利尿特性,但在現代獸醫學中很少用於這些適應症。
作用機制: Dichlorphenamide exerts its effects via noncompetitive, reversible inhibition of the enzyme **carbonic anhydrase (CA)**. * **In the ciliary body**: Inhibition of **CA-II** → decreased formation of bicarbonate (HCO3-) and hydrogen (H+) ions from carbon dioxide and water → reduced active transport of sodium into the posterior chamber → decreased aqueous humor production → **lowered intraocular pressure (IOP)**. * **In the kidneys**: Inhibits CA in the proximal convoluted tubule → increased renal tubular secretion of Na+, K+, and HCO3- → alkaline diuresis and potential metabolic acidosis. * **In the CNS**: Exhibits mild anticonvulsant activity, likely secondary to localized metabolic acidosis or direct CA inhibition in the brain.
各物種劑量
- Adjunctive treatment of glaucoma · 0.5-1.5 mg/kg PO two to three times daily · PO · q8-12h
- Adjunctive treatment of glaucoma · 1-2 mg/kg PO q8-12h · PO · q8-12h
- Adjunctive treatment of glaucoma · 2.2-4.4 mg/kg PO two to three times daily (q8-12h) · PO · q8-12h
- Adjunctive treatment of glaucoma · 10-15 mg/kg per day divided 2-3 times daily · PO · divided 2-3 times daily
- Adjunctive treatment of glaucoma · 2-5 mg/kg PO q8-12h · PO · q8-12h
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
給藥途徑
禁忌症
- Significant hepatic disease (may precipitate hepatic coma)
- Renal or adrenocortical insufficiency
- Hyponatremia
- Hypokalemia
- Hyperchloremic acidosis
- Electrolyte imbalance
- Severe pulmonary obstruction (unable to increase alveolar ventilation)
- Hypersensitivity to carbonic anhydrase inhibitors
- Chronic, noncongestive, angle-closure glaucoma (long-term use)
不良反應
- Panting
- GI disturbances (inappetence, vomiting, diarrhea)
- CNS effects (sedation, depression, excitement)
- Hematologic effects (bone marrow depression)
- Renal effects (crystalluria, dysuria, renal colic, polyuria)
- Metabolic acidosis
- Hypokalemia
- Hyperglycemia
- Hyponatremia
- Hyperuricemia
- Hepatic insufficiency
- Dermatologic effects (rash)
- Hypersensitivity reactions
藥物相互作用
- Antidepressants, Tricyclic · Alkaline urine caused by dichlorphenamide may decrease excretion of tricyclic antidepressants.
- Aspirin (or other salicylates) · Increased risk of dichlorphenamide accumulation and toxicity; increased risk for metabolic acidosis; dichlorphenamide increases salicylate excretion.
- Digoxin · Dichlorphenamide may cause hypokalemia, leading to an increased risk for digoxin toxicity.
- Insulin · Rarely, carbonic anhydrase inhibitors interfere with the hypoglycemic effects of insulin.
- Methenamine compounds · Dichlorphenamide may negate the effects of methenamine in the urine due to alkalinization.
- Potassium-depleting drugs (corticosteroids, amphotericin B, corticotropin, diuretics) · Concomitant use may exacerbate potassium depletion.
- Phenobarbital · Increased urinary excretion, which may reduce phenobarbital levels.
- Primidone · Decreased primidone concentrations.
- Quinidine · Alkaline urine caused by dichlorphenamide may decrease quinidine excretion.
監測
- Intraocular pressure (IOP) / tonometry
- Serum electrolytes (may need to supplement potassium)
- Baseline CBC with differential and periodic retests if using chronically
- Clinical signs of adverse effects (GI upset, panting, CNS changes)
過量
Information regarding acute toxicity of dichlorphenamide is limited. * **Clinical Signs**: Likely extensions of adverse effects, including severe electrolyte derangements (hypokalemia, hyponatremia), profound metabolic acidosis, CNS depression, and dehydration. * **Treatment**: * Monitor serum electrolytes, blood gases, volume status, and CNS status. * Provide aggressive supportive care, including IV fluid therapy to correct dehydration and acid-base/electrolyte imbalances (e.g., potassium supplementation). Treat symptomatically.
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。