QuickView for Spirapril (compound)

Summary
General Info

PubChem

PubChem Compound 10577143

Name:	spirapril
PubChem Compound ID:	10577143
Molecular formula:	C₂₆H₂₆N₂O₆S
Molecular weight:	494.561 g/mol

DrugBank

Identification

Name:	spirapril
Name (isomeric):	DB01348
Drug Type:	small molecule
Brand:	Renormax
Category:	Angiotensin-converting Enzyme Inhibitors, Antihypertensive Agents
CAS number:	83647-97-6

Pharmacology

Indication:	Spirapril is an ACE inhibitor class drug used to treat hypertension.
Pharmacology:	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 ... show more » 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. show less «
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 con... show more » 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. show less «
Absorption:	Bioavailability is 50% following oral administration.
Biotransformation:	Hepatic. Converted to spiraprilat following oral administration.
Half Life:	30 to 35 hours
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Avoid alcohol.

High salt intake may attenuate the antihypertensive effect of spirapril.

Herbs that may attenuate the antihypertensive effect of spirapril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice.

Spirapril may decrease the excretion of potassium. Salt substitutes containing potassium may increase the risk of hyperkalemia.

Do not take calcium, aluminum, magnesium or iron supplements within 2 hours of taking this medication.

Drug interaction:

Lithium	The ACE inhibitor increases serum levels of lithium
Tizanidine	Tizanidine increases the risk of hypotension with the ACE inhibitor
Potassium	Increased risk of hyperkalemia
Amiloride	Increased risk of hyperkalemia
Triamterene	Increased risk of hyperkalemia

Targets

Angiotensin-converting enzyme

Transporters

Oligopeptide transporter, small intestine isoform

Oligopeptide transporter, kidney isoform