簡介
中文名稱 坎地沙坦 ,又名坎地沙坦酯C8中間體。
中文別名 2-乙氧基-3-[[4-[2-(1H-四唑-5-基)苯基]苯基]甲基]-3H-苯並咪唑-4-羧酸
英文名稱 Candesartan
英文別名 2-Ethoxy-3-[[4-[2-(1H-tetrazol-5-yl)phenyl]phenyl]methyl]-3H-benzoimidazole-4-carboxylic acid; Ethyl(2-ethoxy-1-benzimidazole)-7-carboxylate; 1H-Benzimidazole-7-carboxylic acid; 2-ethoxy-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-; 2-Ethoxy-1-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)-7-benzimidazolecarboxylic acid; 2-ethoxy-1-({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl)-1H-benzimidazole-7-carboxylic acid; Blopress; Blopress (TN); C07468; Candesartan (USAN); Candesartan [USAN:INN]; CHEBI:3347; CV 11974; D00522; 1-{[(cyclohexyloxy)carbonyl]oxy}ethyl 2-ethoxy-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylate; 2-ethoxy-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid; (4S)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
CAS RN 139481-59-7
分 子 式 C24H20N6O3
分 子 量 440.45
物化性質 熔點：183-185°C
適應症
1.Candesartan is in a class of drugs called angiotensin II receptor antagonists. Candesartan prevents the constriction (narrowing) of blood vessels (veins and arteries).2.Candesartan is used to treat high blood pressure (hypertension).
3.Candesartan may also be used for purposes other than those listed in this medication guide.
用法用量
1. Take candesartan exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.2. Take each dose with a full glass (8 ounces) of water.
3. You can take candesartan with or without food.
4. Do not stop taking candesartan unless your doctor approves. If you stop taking your medication, your condition could become much worse.
5.Store candesartan at room temperature away from moisture and heat.
注意事項
1. Do not take candesartan if you are pregnant or planning a pregnancy. When used during the second and third trimesters of pregnancy, candesartan can cause injury and even death to the developing fetus. Notify your doctor immediately if you think you might be pregnant.2. Use caution when driving, operating machinery, or performing other hazardous activities. Rarely, candesartan may cause dizziness or drowsiness. If you experience dizziness or drowsiness, avoid these activities. Also use caution when rising from a sitting or lying position.
3. Use alcohol cautiously. Alcohol may further lower blood pressure and increase drowsiness and dizziness while you are taking candesartan.
If Miss a Dose: 1.Take the missed dose as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and take only your next regularly scheduled dose. Do not take a double dose of this medication.
Contraindications: 1.Before taking candesartan, tell your doctor if you
*have kidney disease;
*have liver disease;
*are on a salt-restricted diet or have high levels of potassium in your blood; or
*are taking potassium supplements (e.g., K-Dur, Klor-Con, others), or a potassium-sparing diuretic such as amiloride (Midamor), triamterene (Dyrenium, Dyazide, Maxzide), or spironolactone (Aldactone).
2.You may not be able to take candesartan, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.
3.Candesartan is in the FDA pregnancy category D. This means that it is known to harm an unborn baby. When used during the second and third trimesters of pregnancy, candesartan can cause injury and even death to the developing fetus. Do not take candesartan if you are pregnant.
4. It is not known whether candesartan passes into breast milk. Do not take candesartan without first talking to your doctor if you are breast-feeding a baby.
Special Concerns: 1.Use caution when driving, operating machinery, or performing other hazardous activities. Rarely, candesartan may cause dizziness or drowsiness. If you experience dizziness or drowsiness, avoid these activities. Also use caution when rising from a sitting or lying position.
2.Use alcohol cautiously. Alcohol may further lower blood pressure and increase drowsiness and dizziness while you are taking candesartan.
3. Do not use salt substitutes or take potassium supplements without first talking to your doctor. Candesartan can affect potassium levels in your body.
不良反應
1.If you experience any of the following serious side effects, stop taking candesartan and call your doctor immediately or seek emergency medical treatment.*an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives); or
*little or no urine.
2.Other side effects are less serious. Continue to take candesartan and talk to your doctor if you experience
*headache,
*dizziness,
*fatigue,
*diarrhea or upset stomach,
*muscle or joint pain or cramps,
*insomnia, or
*congestion or cough.
3.Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.
相互作用
1.Before taking candesartan, tell your doctor if you*take a potassium supplement such as K-Dur, Klor-Con, and others;
*take a potassium-sparing diuretic (water pill) such as amiloride (Midamor), spironolactone (Aldactone), or triamterene (Dyrenium, Dyazide, Maxzide); or
*use a salt substitute.
2.Candesartan can affect potassium levels in your body. You may not be able to take candesartan, or you may require a dosage adjustment or special monitoring if you are taking any of the medicines listed above.
3.Tell your doctor about any other medicines you take to treat high blood pressure or other heart conditions. Candesartan may cause very low blood pressure if it is taken with other heart medications.
4.Drugs other than those listed here may also interact with candesartan or affect your condition. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines.
藥物過量
1.Seek emergency medical attention.2.Symptoms of a candesartan overdose are not well known but might include dizziness, weakness, fainting, and fatigue.
臨床研究
【功效主治】 用於治療 原發性高血壓。本品可單獨使用，也可與其它抗 高血壓藥物聯用。【化學成分】 【藥理作用】 坎地沙坦酯在體內迅速被水解成活性代謝物坎地沙坦，坎地沙坦為選擇性 血管緊張素Ⅱ受體(AT1)拮抗劑，通過與血管平滑肌AT1受體結合而拮抗血管 緊張素Ⅱ的血管收縮作用，從而降低末梢血管阻力。另有認為：坎地沙坦可通過抑制腎上腺分泌醛固酮而發揮一定的降壓作用。坎地沙坦不抑制激肽酶Ⅱ，不影響緩激肽降解。在 高血壓患者進行的實驗顯示：患者多次服用本品可致血漿腎素活性、血管緊張素1濃度及血管緊張素Ⅱ濃度升高;本品2-8mg每日1次連續服用，可使收縮壓、舒張壓下降，左室心肌重量、末梢血管阻力減少，而對心排出量、射血分數、腎血管阻力、腎血流量、 腎小球濾過率無明顯影響;對有腦血管障礙的原發生性 高血壓患者，對腦血流量無影響。
【 藥物相互作用】 本品與 優降糖、 尼莫地平、 地高辛、 華法令、 氫氯噻嗪等藥品均無明顯相互作用，在健康受試者口服避孕藥情形下，亦無明顯相互作用。由於本品不通過P450肝藥酶體系代謝，並對P450代謝無影響,因此，本品與其它能被P450代謝的或影響P450代謝功能的藥物間無相互作用。
【不良反應】 (1) 血管性水腫：有時出現面部、口唇、舌、咽、喉頭等 水腫症狀的血管形水腫，應進行仔細的觀察，見到異常時，停止用藥，並進行適當處理。
(2) 暈厥和失去意識：過度的降壓可能引起 暈厥和暫時性失去意識。在這種情況下，應停止服藥，並進行適當處理。特別是正進行血液透析的患者、嚴格進行限鹽療法的患者、最近開始服用 利尿降壓藥的患者，可能會出現血壓的迅速降低。因此，這些患者使用本藥治療應從較低的劑量開始服用。如有必要增加劑量，應密切觀察患者情況，緩慢進行。
(3) 急性腎功能衰竭：可能會出現急性 腎功能衰竭，應密切觀察患者情況，如發現異常，應停止服藥，並進行適當處理。
(4) 高血鉀患者：鑒於可能會出現高血鉀，應密切觀察患者情況。如發現異常，應停止服藥，並進行適當處理。
(5) 肝功能惡化或 黃疸：鑒於可能會出現AST(GOT)、ACT(GPTO，γ-GTP)等值升高的肝功能障礙或 黃疸，應密切觀察患者情況。如發現異常，應停止服藥，病進行適當處理。
(6) 粒細胞缺乏症：可能會出現粒細胞缺乏症，應密切觀察患者情況。如發現異常，應停止服藥，並進行適當處理。
(7) 橫紋肌溶解：可能會出現如表現為肌痛、虛弱、CK增加、血中和尿中的肌球蛋白。如出現上述情況，應停止服藥，病進行適當處理。
(8)間質性 肺炎： 可能會出現伴有 發熱、 咳嗽、 呼吸困難、胸部X—線檢查異常等表現的間質性肺炎。如出現上述情況，應停止服藥，並進行適當處理，如用 腎上腺皮質激素治療。
【禁忌症】 1 對本製劑的成分有過敏史的患者。
2 妊娠或可能妊娠的婦女(參照【 孕婦及哺乳期婦女用藥】項)。
3 嚴重的肝、腎功能不全或膽汁淤滯患者
產品用途
血管緊張素Ⅱ受體拮抗劑，用於治療高血壓
