Acovil - General Information
A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.
Pharmacology of Acovil
Acovil is an angiotensin-converting enzyme (ACE) inhibitor similar to benazepril, fosinopril, and quinapril. An inactive prodrug, ramipril is converted to ramiprilat in the liver and is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients.
Acovil for patients
Pregnancy: 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: 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, eyes, lips, or tongue, or difficulty in breathing) and to take no more drug until they have consulted with the prescribing physician.
Symptomatic Hypotension: Patients should be cautioned that lightheadedness can occur, especially during the first days of therapy, and it should be reported. Patients should be told that if syncope occurs, ramipril should be discontinued until the physician has been consulted.
All patients should be cautioned that inadequate fluid intake or excessive perspiration, diarrhea, or vomiting can lead to an excessive fall in blood pressure, with the same consequences of lightheadedness and possible syncope.
Hyperkalemia: Patients should be told not to use salt substitutes containing potassium without consulting their physician.
Neutropenia: Patients should be told to promptly report any indication of infection (e.g., sore throat, fever), which could be a sign of neutropenia.
With nonsteroidal anti-inflammatory agents: Rarely, concomitant treatment with ACE inhibitors and nonsteroidal anti-inflammatory agents have been associated with worsening of renal failure and an increase in serum potassium.
With Diuretics: Patients on diuretics, especially those in whom diuretic therapy was recently instituted, may occasionally experience an excessive reduction of blood pressure after initiation of therapy with ramipril. The possibility of hypotensive effects with ramipril can be minimized by either discontinuing the diuretic or increasing the salt intake prior to initiation of treatment with ramipril. If this is not possible, the starting dose should be reduced.
With Potassium Supplements and Potassium-sparing Diuretics: Ramipril can attenuate potassium loss caused by thiazide diuretics. Potassium-sparing diuretics (spironolactone, amiloride, triamterene, and others) or potassium supplements can increase the risk of hyperkalemia. Therefore, if concomitant use of such agents is indicated, they should be given with caution, and the patient's serum potassium should be monitored frequently.
With Lithium: Increased serum lithium levels and symptoms of lithium toxicity have been reported in patients receiving ACE inhibitors during therapy with lithium. These drugs should be coadministered with caution, and frequent monitoring of serum lithium levels is recommended. If a diuretic is also used, the risk of lithium toxicity may be increased.
Other: Neither ramipril nor its metabolites have been found to interact with food, digoxin, antacid, furosemide, cimetidine, indomethacin, and simvastatin. The combination of ramipril and propranolol showed no adverse effects on dynamic parameters (blood pressure and heart rate). The co-administration of ramipril and warfarin did not adversely affect the anticoagulant effects of the latter drug. Additionally, co-administration of ramipril with phenprocoumon did not affect minimum phenprocoumon levels or interfere with the subjects' state of anti-coagulation.
ALTACE is contraindicated in patients who are hypersensitive to this product or any other angiotensin converting enzyme inhibitor (e.g., a patient who has experienced angioedema during therapy with any other ACE inhibitor.
Additional information about Acovil
Acovil Indication: For diuretics and digitalis in congestive heart failure as adjunctive therapy and for use in prophylaxis in post MI.
Mechanism Of Action: Acovilat, the active metabolite, 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 an increase in plasma renin. Acovilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
Drug Interactions: Drospirenone Increased risk of hyperkaliemia
Amiloride Increased risk of hyperkaliemia
Potassium Increased risk of hyperkaliemia
Lithium The ACE inhibitor increases serum levels of lithium
Spironolactone Increased risk of hyperkaliemia
Triamterene Increased risk of hyperkaliemia
Tizanidine Tizanidine increases the risk of hypotension with the ACE inhibitor
Food Interactions: Not Available
Generic Name: Ramipril
Synonyms: Ramiprilum [Latin]
Drug Category: Antihypertensive Agents; Angiotensin-converting Enzyme Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Ramipril: Acovil; Altace; Carasel; Cardace; Delix; Hytren; Lostapres; Pramace; Quark; Ramace; Triatec; Tritace; Unipril; Vesdil;
Absorption: The extent of absorption is at least 50-60% and is not significantly influenced by the presence of food in the GI tract, although the rate of absorption is reduced.
Toxicity (Overdose): The most likely clinical manifestations would be symptoms attributable to hypotension. LD50 = 10933 mg/kg (orally in mice).
Protein Binding: Protein binding of ramipril is about 73% and that of ramiprilat about 56%. The absolute bioavailabilities of ramipril and ramiprilat were 28% and 44%, respectively.
Biotransformation: Hepatic. Ramipril is a prodrug and is converted to the active metabolite ramiprilat by liver esterase enzymes.
Half Life: 2-4 hours
Dosage Forms of Acovil: Capsule Oral
Chemical IUPAC Name: (2S,3aS,6aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-3,3a,4,5,6,6a-hexahydro-2H-cyclopenta[d]pyrrole-2-carboxylic acid
Chemical Formula: C23H32N2O5
Ramipril on Wikipedia: http://en.wikipedia.org/wiki/Ramipril
Organisms Affected: Humans and other mammals