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药品详细

Spirapril(螺普利)

化学结构式图
中文名
螺普利
英文名
Spirapril
分子式
C22H30N2O5S2
化学名
(8S)-7-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid
分子量
Average: 466.614
Monoisotopic: 466.15961346
CAS号
83647-97-6
ATC分类
C09A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Spirapril is an ACE inhibitor antihypertensive drug used to treat hypertension. Like many ACE inhibitors, this is a prodrug which is converted to the active metabolite spiraprilat following oral administration. ACE inhibitors are used primarily in treatment of hypertension and congestive heart failure.

生产厂家
  • Schering corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Hannedouche T, Ikeni A, Marques LP, Natov S, Dechaux M, Schmitt F, Lacour B, Grunfeld JP: Renal effects of angiotensin II in normotensive subjects on short-term cilazapril treatment. J Cardiovasc Pharmacol. 1992;19 Suppl 6:S25-7. Pubmed
  2. Noble S, Sorkin EM: Spirapril. A preliminary review of its pharmacology and therapeutic efficacy in the treatment of hypertension. Drugs. 1995 May;49(5):750-66. Pubmed
  3. Rosendorff C, Patton J, Radford HM, Kalliatakis B: Alpha-adrenergic and angiotensin II pressor sensitivity in hypertensive patients treated with an angiotensin-converting enzyme inhibitor. J Cardiovasc Pharmacol. 1992;19 Suppl 6:S105-9. Pubmed
  4. Shohat J, Wittenberg C, Erman A, Rosenfeld J, Boner G: Acute and chronic effects of spirapril, alone or in combination with isradipine on kidney function and blood pressure in patients with reduced kidney function and hypertension. Scand J Urol Nephrol. 1999 Feb;33(1):57-62. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Polypeptides
  • Phenylpropylamines
Substructures
  • Carboxylic Acids and Derivatives
  • Hydroxy Compounds
  • Acetates
  • Aliphatic and Aryl Amines
  • Amino Ketones
  • Pyrrolidines
  • Ethers
  • Benzene and Derivatives
  • Polypeptides
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Phenylpropylamines
  • Amino Acids
  • Acetals and Derivatives
适应症
药理
Indication Spirapril is an ACE inhibitor class drug used to treat hypertension.
Pharmacodynamics Spirapril is an angiotensin-converting enzyme (ACE) inhibitor. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. By blocking ACE, spirapril decreases angiotensin II which is a vasoconstrictor and inducer of aldosterone. So by inhibiting the enzymes, aldosterone secreation is decreased (so less sodium is reabsorbed) and there is a decrease in vasoconstriction. Combined, this leades to a decrease in blood pressure.
Mechanism of action Spiraprilat, the active metabolite of spirapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Spiraprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
Absorption Bioavailability is 50% following oral administration.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hepatic. Converted to spiraprilat following oral administration.
Route of elimination Not Available
Half life 30 to 35 hours
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00156 Spirapril Pathway SMP00156
理化性质
Properties
State solid
Experimental Properties Not Available
Predicted Properties
Property Value Source
water solubility 2.93e-02 g/l ALOGPS
logP 1.79 ALOGPS
logP 1.6 ChemAxon
logS -4.2 ALOGPS
pKa (strongest acidic) 3.62 ChemAxon
pKa (strongest basic) 5.2 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 95.94 ChemAxon
rotatable bond count 10 ChemAxon
refractivity 121.94 ChemAxon
polarizability 48.74 ChemAxon
药物相互作用
Drug Interaction
Amiloride Increased risk of hyperkalemia
Lithium The ACE inhibitor increases serum levels of lithium
Potassium Increased risk of hyperkalemia
Tizanidine Tizanidine increases the risk of hypotension with the ACE inhibitor
Triamterene Increased risk of hyperkalemia
食物相互作用
  • Avoid alcohol.
  • Do not take calcium, aluminum, magnesium or iron supplements within 2 hours of taking this medication.
  • Herbs that may attenuate the antihypertensive effect of spirapril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.
  • High salt intake may attenuate the antihypertensive effect of spirapril.
  • Spirapril may decrease the excretion of potassium. Salt substitutes containing potassium may increase the risk of hyperkalemia.

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