이소소르비드 디니트레이트 / 이소소르비드 모노니트레이트
Isosorbide Dinitrate / Isosorbide Mononitrate
1,4:3,6-dianhydro-D-glucitol 2,5-dinitrate / 1,4:3,6-dianhydro-D-glucitol 5-nitrate
다른 이름: Isordil · Ismo · Imdur · Isochron · Dilatrate-SR · Monoket · Titradose · ISDN · EV-151 · sorbide nitrate · AHR-4698 · BM-22145 · IS5-MN · isosorbide-5-mononitrate
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
동물 종별 용량
🌎 NA — North America🌍 EU — Europe
개
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors | Isosorbide dinitrate at 0.5-2 mg/kg PO twice daily OR isosorbide mononitrate at 0.25-2 mg/kg PO twice daily | PO | twice daily | — | 🌎 NA |
- Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors: Efficacy is unknown. It is unknown if nitrate-free periods are required to prevent nitrate tolerance.
고양이
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| Adjunctive treatment of heart failure associated with thyroid storm | Isosorbide dinitrate at 0.5-2 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors | Isosorbide dinitrate at 0.5-2 mg/kg PO twice daily OR isosorbide mononitrate at 0.25-2 mg/kg PO twice daily | PO | twice daily | — | 🌎 NA |
- Adjunctive treatment of heart failure associated with thyroid storm: Start at lowest level and titrate upward.
- Refractory heart failure or in combination with hydralazine or amlodipine in patients unable to tolerate ACE inhibitors: Efficacy is unknown.
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
이소소르비드 디니트레이트(ISDN) 및 이소소르비드 모노니트레이트(ISMN)는 주로 심장의 전부하를 감소시키는 데 사용되는 강력한 정맥 확장제인 유기 질산염입니다. 인의에서는 협심증 및 울혈성 심부전(CHF)에 널리 사용되지만, 소동물 임상에서의 경험과 입증된 효능은 아직 제한적입니다. 난치성 심부전의 보조 요법이나 ACE 억제제를 견디지 못하는 환자에게 간혹 사용됩니다. 개는 사람에 비해 치료적 혈역학적 효과를 얻기 위해 훨씬 더 높은 용량이 필요한 것으로 보입니다. 지속적인 사용은 질산염 내성을 유발할 수 있습니다.
작용 기전
Organic nitrates act as prodrugs that donate nitric oxide (NO) to vascular smooth muscle, leading to profound vasodilation (predominantly venous, with some arterial effects at higher doses).
Mechanism Pathway: Organic Nitrate → converted to free radical Nitric Oxide (NO) → activates soluble guanylate cyclase (sGC) → increases intracellular cyclic GMP (cGMP) → activates Protein Kinase G (PKG) → decreases intracellular calcium and dephosphorylates myosin light chain → Vascular Smooth Muscle Relaxation.
- Hemodynamic Effects: By dilating the venous capacitance vessels, nitrates significantly decrease venous return to the heart (reduced preload), which lowers ventricular filling pressures and helps alleviate pulmonary edema in CHF.
- Additional Effects: Nitrates functionally antagonize acetylcholine, norepinephrine, and histamine. They also relax non-vascular smooth muscle, including biliary, bronchial, gastrointestinal, ureteral, and uterine tissues.
안전성·주의사항
금기사항
- Cardiogenic or hypovolemic shock
- Severe hypotension
- Hypovolemia
- Use as a sole agent for treating heart failure
- Concurrent use with selective phosphodiesterase inhibitors (e.g., sildenafil)
부작용
- Postural hypotension
- Reflex tachycardia
- Lethargy or weakness (secondary to hypotension)
- Gastrointestinal upset
- Restlessness
- Headache (well-documented in humans, difficult to assess in animals)
- Hypersensitivity reactions (rare)
주의
Hemodynamic Warning: Use with extreme caution in patients with low blood pressure or uncorrected hypovolemia.
- Nitrate Tolerance: Continuous exposure may lead to tolerance. Consider dosing strategies that allow for a nitrate-free interval if chronic use is intended.
- Laboratory Interference: Serum cholesterol levels may be falsely decreased by nitrates when using the Zlatkis-Zak color reaction method.
- Pregnancy: FDA Category C. Use only if the potential benefit justifies the potential risk to the fetus.
약물 상호작용
Possible additive hypotensive effects; monitor blood pressure closely.
Possible additive hypotensive effects due to alpha-adrenergic blockade.
Concurrent use with sildenafil can cause profound, life-threatening hypotension and is strictly contraindicated. Use with pimobendan (a PDE3 inhibitor) is common in vet med but requires monitoring for excessive vasodilation.
모니터링
- Clinical efficacy (improvement in respiratory rate/effort, resolution of pulmonary edema)
- Systemic blood pressure (monitor for hypotension)
- Heart rate (monitor for reflex tachycardia)
- Renal values and electrolytes (if used concurrently with diuretics and ACE inhibitors)
약동학
반감기
흡수
Dogs: Isosorbide mononitrate oral bioavailability is approximately 70%. Oral doses >2 mg/kg yield peak plasma levels >100 ng/mL (believed to be the minimum required for hemodynamic effects). Humans: Both ISDN and ISMN are well absorbed orally; food may delay the rate but not the extent of absorption.
분포
Widely distributed. Hemodynamic effects require minimum serum concentrations of approximately 100 ng/mL, though some canine studies showed no hemodynamic changes even at much higher peak levels.
대사
Isosorbide dinitrate undergoes extensive first-pass hepatic metabolism primarily to isosorbide mononitrate. Isosorbide mononitrate is metabolized primarily in the liver but does not undergo first-pass metabolism.
배설
Metabolites do not appear to have pharmacologic activity and are principally excreted in the urine.
과다투여
Toxicity Profile: Isosorbide mononitrate caused significant lethality in rats and mice at massive dosages (2000 mg/kg and 3000 mg/kg, respectively).
Clinical Signs of Overdose:
- Profound venous pooling
- Decreased cardiac output
- Severe hypotension
- Reflex tachycardia
- Collapse or syncope
Treatment:
- Treatment is primarily supportive.
- Avoid Epinephrine: Drug therapies with agents such as epinephrine are NOT recommended as they may exacerbate the cardiovascular collapse.
- Fluid Therapy: Increasing central fluid volume may be useful to counteract venous pooling, but in patients with pre-existing congestive heart failure (CHF), IV fluids must be administered with extreme caution to avoid precipitating fulminant pulmonary edema.
제품
제형
- Oral tablets
- Sublingual tablets
- Extended-release tablets
- Sustained-release capsules
인용의약품
- Isosorbide Dinitrate Oral Tablets: 5 mg, 10 mg, 20 mg, 30 mg, & 40 mg
- Isosorbide Dinitrate Sublingual Oral Tablets: 2.5 mg, & 5 mg
- Isosorbide Dinitrate Extended-Release Oral Tablets: 40 mg
- Isosorbide Dinitrate Sustained-Release Oral Capsules: 40 mg
- Isosorbide Mononitrate Tablets: 10 mg, & 20 mg
- Isosorbide Mononitrate Extended-Release Tablets: 30 mg, 60 mg, & 120 mg
규제 현황
규제 데이터 없음: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
Isosorbide dinitrate and standard isosorbide mononitrate tablets should be stored in well-closed/tight containers below 40°C (preferably between 15°-30°C). Isosorbide mononitrate extended-release tablets should be stored between 2°-30°C. Heat and moisture accelerate the loss of potency.
보호자 정보
이 약물은 수의학에서 사용 경험이 제한적이며, 일반적으로 진행되었거나 치료하기 어려운 심장 질환에 사용됩니다. 식사와 관계없이 투여할 수 있습니다. 신체가 약물에 대한 내성을 갖는 것을 방지하기 위해 특정 투여 간격이 필요할 수 있으므로 수의사의 투여 일정을 정확히 따르십시오. 이 약은 혈압을 낮추기 때문에 반려동물에게 쇠약, 무기력, 비틀거림 또는 실신의 징후가 있는지 주의 깊게 관찰하십시오. 이러한 증상이 나타나면 즉시 수의사에게 연락하십시오. 약효가 떨어지는 것을 방지하기 위해 열과 습기를 피해 원래의 용기에 단단히 밀폐하여 보관하십시오.
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