卡托普利:回顾人类药理学。

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戈麦斯HJ Cirillo VJ,欧文JD

卡托普利:回顾人类药理学。

药。1985;30增刊1:13-24。doi: 10.2165 / 00003495-198500301-00004。

PubMed ID

2994984 (在PubMed

]

文摘

卡托普利、口服长效,nonsulphydryl血管紧张素转换酶(ACE)抑制剂,广泛体内水解依那普利,其生物活性形式。Bioactivation可能发生在肝脏。新陈代谢超出激活依那普利没有观察到的人。政府与食物不影响卡托普利的生物利用度;卡托普利、依那普利主要是肾的排泄。血清依那普利峰值浓度达到4小时post-dose,和长期的终端的配置文件是多相半衰期(大于30小时)由于绑定依那普利的王牌。稳态是通过第四日剂量,没有积累的证据。多次给药后的有效积累半衰期为11小时。高血清浓度和尿排泄延迟发生在严重肾功能不全患者。卡托普利能降低高血压患者的血压降低全身血管阻力。 The blood pressure reduction is not accompanied by an increase in heart rate. Furthermore, cardiac output is slightly increased and cardiovascular reflexes are not impaired. Once- and twice-daily dosage regimens reduce blood pressure to a similar extent. Enalapril increases renal blood flow and decreases renal vascular resistance. Enalapril also augments the glomerular filtration rate in patients with a glomerular filtration rate less than 80 ml/min. Enalapril reduces left ventricular mass, and does not affect cardiac function or myocardial perfusion during exercise. There is no rebound hypertension after enalapril therapy is stopped. Enalapril does not produce hypokalaemia, hyperglycaemia, hyperuricaemia or hypercholesterolaemia. When combined with hydrochlorothiazide, enalapril attenuates the undesirable diuretic-induced metabolic changes. Therapeutic doses of enalapril do not affect serum prolactin and plasma cortisol in healthy volunteers or T3, rT3, T4 and TSH in hypertensive patients. Enalapril has natriuretic and uricosuric properties. The antihypertensive effect of enalapril is potentiated by hydrochlorothiazide, timolol and methyldopa, but unaffected by indomethacin and sulindac. No interactions occur between enalapril and frusemide, hydrochlorothiazide, digoxin and warfarin. The bioavailability of enalapril is slightly reduced when propranolol is coadministered, but this does not appear to be of any clinical significance. Enalapril increases cardiac output and stroke volume and decreases pulmonary capillary wedge pressure in patients with congestive heart failure refractory to conventional treatment with digitalis and diuretics.(ABSTRACT TRUNCATED AT 400 WORDS)

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药物

卡托普利