Acequin - General Information
Acequin is used in the treatment of hypertension and congestive heart failure. Acequin is actually a prodrug. It is converted to its active metabolite, quinaprilat, in the liver. Acequin inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I. Angiotensin II is a powerful vasoconstrictor and increases blood pressure through a variety of mechanisms.
Pharmacology of Acequin
Acequin, an angiotensin-converting enzyme (ACE) inhibitor, is used to treat hypertension and heart failure. Like ramipril, quinapril is a prodrug that, upon deesterification, is converted to the active metabolite quinaprilat. The effect of quinapril in hypertension and in congestive heart failure (CHF) appears to result primarily from the inhibition of circulating and tissue ACE activity, thereby reducing angiotensin II formation.
Acequin for patients
Female patients of childbearing age should be told about the consequences of second- and third-trimester exposure to ACE
inhibitors, and they should also be told that these consequences do not appear to have resulted from intrauterine ACE-inhibitor
exposure that has been limited to the first trimester. These patients should be asked to report pregnancies to their physicians
as soon as possible.
Angioedema, including laryngeal edema can occur with treatment with ACE inhibitors, especially following the first dose. Patients
should be so advised and told to report immediately any signs or symptoms suggesting angioedema (swelling of face, extremities,
eyes, lips, tongue, difficulty in swallowing or breathing) and to stop taking the drug until they have consulted with their physician.
Patients should be cautioned that lightheadedness can occur, especially during the first few days of ACCUPRIL therapy, and that it
should be reported to a physician. If actual syncope occurs, patients should be told to not take the drug until they have consulted
with their physician.
All patients should be cautioned that inadequate fluid intake or excessive perspiration, diarrhea, or vomiting can lead to an
excessive fall in blood pressure because of reduction in fluid volume, with the same consequences of lightheadedness and possible
Patients planning to undergo any surgery and/or anesthesia should be told to inform their physician that they are taking an ACE
Patients should be told not to use potassium supplements or salt substitutes containing potassium without consulting their physician.
Patients should be told to report promptly any indication of infection (eg, sore throat, fever) which could be a sign of neutropenia.
NOTE: As with many other drugs, certain advice to patients being treated with ACCUPRIL is warranted. This information is intended to
aid in the safe and effective use of this medication. It is not a disclosure of all possible adverse or intended effects.
Concomitant diuretic therapy
As with other ACE inhibitors, patients on diuretics, especially those on recently instituted diuretic therapy, may occasionally experience an excessive reduction of blood pressure after initiation of therapy with ACCUPRIL. The possibility of hypotensive effects with ACCUPRIL may be minimized by either discontinuing the diuretic or cautiously increasing salt intake prior to initiation of treatment with ACCUPRIL. If it is not possible to discontinue the diuretic, the starting dose of quinapril should be reduced.
Agents increasing serum potassium
Quinapril can attenuate potassium loss caused by thiazide diuretics and increase serum potassium when used alone. If concomitant therapy of ACCUPRIL with potassium-sparing diuretics (eg, spironolactone, triamterene, or amiloride), potassium supplements, or potassium-containing salt substitutes is indicated, they should be used with caution along with appropriate monitoring of serum potassium.
Tetracycline and other drugs that interact with magnesium
Simultaneous administration of tetracycline with ACCUPRIL reduced the absorption of tetracycline by approximately 28% to 37%, possibly due to the high magnesium content in ACCUPRIL tablets. This interaction should be considered if coprescribing ACCUPRIL and tetracycline or other drugs that interact with magnesium.
Increased serum lithium levels and symptoms of lithium toxicity have been reported in patients receiving concomitant lithium and ACE inhibitor therapy. These drugs should be coadministered with caution and frequent monitoring of serum lithium levels is recommended. If a diuretic is also used, it may increase the risk of lithium toxicity.
Drug interaction studies of ACCUPRIL with other agents showed:
· Multiple dose therapy with propranolol or cimetidine has no effect on the pharmacokinetics of single doses of ACCUPRIL.
· The anticoagulant effect of a single dose of warfarin (measured by prothrombin time) was not significantly changed by quinapril coadministration twice-daily.
· ACCUPRIL treatment did not affect the pharmacokinetics of digoxin.
· No pharmacokinetic interaction was observed when single doses of ACCUPRIL and hydrochlorothiazide were administered concomitantly.
· Co-administration of multiple 10 mg doses of atorvastatin with 80 mg of ACCUPRIL resulted in no significant change in the steady-state pharmacokinetic parameters of atorvastatin.
ACCUPRIL is contraindicated in patients who are hypersensitive to this product and in patients with a history of angioedema related to previous treatment with an ACE inhibitor.
Additional information about Acequin
Acequin Indication: For the treatment of hypertension and chronic heart failure.
Mechanism Of Action: Acequinat competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to 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. Acequinat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
Drug Interactions: Amiloride Increased risk of hyperkaliemia
Drospirenone Increased risk of hyperkaliemia
Potassium Increased risk of hyperkaliemia
Spironolactone Increased risk of hyperkaliemia
Triamterene Increased risk of hyperkaliemia
Lithium The ACE inhibitor increases serum levels of lithium
Tetracycline Acequin can reduce the absorption of tetracycline
Tizanidine Tizanidine increases the risk of hypotension with the ACE inhibitor
Food Interactions: Not Available
Generic Name: Quinapril
Synonyms: Quinapril Hydrochloride; Quinapril Hcl; Quinaprilum [Latin]
Drug Category: Antihypertensive Agents; Angiotensin-converting Enzyme Inhibitors
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Quinapril: Accupril; Accuprin; Accupro; Acequin; Acuitel; Korec; Quinazil;
Absorption: Following oral administration, peak plasma quinapril concentrations are observed within one hour. Based on recovery of quinapril and its metabolites in urine, the extent of absorption is at least 60%. The rate and extent of quinapril absorption are diminished moderately (approximately 25-30%) when ACCUPRIL tablets are administered during a high-fat meal.
Toxicity (Overdose): Overdose may lead to severe hypotension. LD50=1739mg/kg (orally in mice).
Protein Binding: 97%
Half Life: 2 hours
Dosage Forms of Acequin: Tablet Oral
Chemical IUPAC Name: (3S)-2-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-3,4-dihydro-1H-isoquinoline-3-carboxylic acid
Chemical Formula: C25H30N2O5
Quinapril on Wikipedia: http://en.wikipedia.org/wiki/Quinapril
Organisms Affected: Humans and other mammals