坎地沙坦

药品

坎地沙坦（英文Candesartan），又名坎地沙坦酯C8中间体。中文别名 2-乙氧基-3-[[4-[2-(1H-四唑-5-基)苯基]苯基]甲基]-3H-苯并咪唑-4-羧酸，是一种有机化合物，分子式是 C24H20N6O3。熔点183-185℃。该药用于治疗原发性高血压。本品可单独使用，也可与其它抗高血压药物联用。

简介

中文名称坎地沙坦 ,又名坎地沙坦酯C8中间体。

中文别名 2-乙氧基-3-[[4-[2-(1H-四唑-5-基)苯基]苯基]甲基]-3H-苯并咪唑-4-羧酸

英文名称 Candesartan

英文别名 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

物化性质熔点：183-185°C

适应症

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.

不良反应

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.

药物相互作用

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.

注意事项

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.

临床研究

【功效主治】　用于治疗原发性高血压。本品可单独使用，也可与其它抗高血压药物联用。

【化学成分】【药理作用】　坎地沙坦酯在体内迅速被水解成活性代谢物坎地沙坦，坎地沙坦为选择性血管紧张素Ⅱ 受体(AT1)拮抗剂，通过与血管平滑肌AT1受体结合而拮抗血管紧张素Ⅱ的血管收缩作用，从而降低末梢血管阻力。另有认为：坎地沙坦可通过抑制肾上腺分泌醛固酮而发挥一定的降压作用。坎地沙坦不抑制激肽酶Ⅱ，不影响缓激肽降解。在高血压患者进行的实验显示：患者多次服用本品可致血浆肾素活性、血管紧张素1浓度及血管紧张素Ⅱ浓度升高;本品2-8mg每日1次连续服用，可使收缩压、舒张压下降，左室心肌重量、末梢血管阻力减少，而对心排出量、射血分数、肾血管阻力、肾血流量、肾小球滤过率无明显影响;对有脑血管障碍的原发生性高血压患者，对脑血流量无影响。

【药物相互作用】　本品与优降糖、尼莫地平、地高辛、华法令、氢氯噻嗪等药品均无明显相互作用，在健康受试者口服避孕药情形下，亦无明显相互作用。由于本品不通过P450肝药酶体系代谢，并对P450代谢无影响,因此，本品与其它能被P450代谢的或影响P450代谢功能的药物间无相互作用。

【不良反应】　(1) 血管性水肿：有时出现面部、口唇、舌、咽、喉头等水肿症状的血管形水肿，应进行仔细的观察，见到异常时，停止用药，并进行适当处理。

(2) 晕厥和失去意识：过度的降压可能引起晕厥和暂时性失去意识。在这种情况下，应停止服药，并进行适当处理。特别是正进行血液透析的患者、严格进行限盐疗法的患者、最近开始服用利尿降压药的患者，可能会出现血压的迅速降低。因此，这些患者使用本药治疗应从较低的剂量开始服用。如有必要增加剂量，应密切观察患者情况，缓慢进行。

(3) 急性肾功能衰竭：可能会出现急性肾功能衰竭，应密切观察患者情况，如发现异常，应停止服药，并进行适当处理。

(4) 高血钾患者：鉴于可能会出现高血钾，应密切观察患者情况。如发现异常，应停止服药，并进行适当处理。

(5) 肝功能恶化或黄疸：鉴于可能会出现AST(GOT)、ACT(GPTO，γ-GTP)等值升高的肝功能障碍或黄疸，应密切观察患者情况。如发现异常，应停止服药，病进行适当处理。

(6) 粒细胞缺乏症：可能会出现粒细胞缺乏症，应密切观察患者情况。如发现异常，应停止服药，并进行适当处理。

(7) 横纹肌溶解：可能会出现如表现为肌痛、虚弱、CK增加、血中和尿中的肌球蛋白。如出现上述情况，应停止服药，病进行适当处理。

(8)间质性肺炎：可能会出现伴有发热、咳嗽、呼吸困难、胸部X—线检查异常等表现的间质性肺炎。如出现上述情况，应停止服药，并进行适当处理，如用肾上腺皮质激素治疗。

【禁忌症】　1 对本制剂的成分有过敏史的患者。

2 妊娠或可能妊娠的妇女(参照【孕妇及哺乳期妇女用药】项)。

3 严重的肝、肾功能不全或胆汁淤滞患者

产品用途

血管紧张素Ⅱ受体拮抗剂，用于治疗高血压

药物过量