General
Impaired renal function: As a consequence of inhibiting the renin-angiotensin-aldosterone system,
changes in renal function may be anticipated in susceptible individuals. In
patients with
severe heart failure whose renal function may depend on the activity of the
renin-angiotensin-
aldosterone system, treatment with ACE inhibitors, including ACCUPRIL, may
be associated
with oliguria and/or progressive azotemia and rarely acute renal failure and/or
death.
In clinical studies in hypertensive patients with unilateral or bilateral renal
artery stenosis,
increases in blood urea nitrogen and serum creatinine have been observed in
some patients
following ACE inhibitor therapy. These increases were almost always reversible
upon
discontinuation of the ACE inhibitor and/or diuretic therapy. In such patients,
renal function
should be monitored during the first few weeks of therapy.
Some patients with hypertension or heart failure with no apparent preexisting
renal vascular
disease have developed increases in blood urea and serum creatinine, usually
minor and transient,
especially when ACCUPRIL has been given concomitantly with a diuretic. This
is more likely to
occur in patients with preexisting renal impairment. Dosage reduction and/or
discontinuation of
any diuretic and/or ACCUPRIL may be required.
Evaluation of patients with hypertension or heart failure should always include
assessment
of renal function (see DOSAGE AND ADMINISTRATION).
Hyperkalemia and potassium-sparing diuretics: In clinical trials, hyperkalemia
(serum
potassium =5.8 mmol/L) occurred in approximately 2% of patients receiving ACCUPRIL.
In
most cases, elevated serum potassium levels were isolated values which resolved
despite
continued therapy. Less than 0.1% of patients discontinued therapy due to hyperkalemia.
Risk
factors for the development of hyperkalemia include renal insufficiency, diabetes
mellitus, and
the concomitant use of potassium-sparing diuretics, potassium supplements,
and/or potassium-
containing salt substitutes, which should be used cautiously, if at all, with
ACCUPRIL (see
PRECAUTIONS, Drug Interactions).
Cough: Presumably due to the inhibition of the degradation of endogenous bradykinin,
persistent
non-productive cough has been reported with all ACE inhibitors, always resolving
after
discontinuation of therapy. ACE inhibitor-induced cough should be considered
in the differential
diagnosis of cough.
Surgery/anesthesia: In patients undergoing major surgery or during anesthesia
with agents that
produce hypotension, ACCUPRIL will block angiotensin II formation secondary
to
compensatory renin release. If hypotension occurs and is considered to be due
to this mechanism,
it can be corrected by volume expansion.
Information 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,
extremities, eyes,
lips, tongue, difficulty in swallowing or breathing) and to stop taking the
drug until they have
consulted with their physician (see WARNINGS).
Symptomatic hypotension: 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 (see WARNINGS).
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 syncope.
Patients planning to undergo any surgery and/or anesthesia should be told to
inform their
physician that they are taking an ACE inhibitor.
Hyperkalemia: Patients should be told not to use potassium supplements or salt
substitutes
containing potassium without consulting their physician (see PRECAUTIONS).
Neutropenia: 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.
Drug Interactions
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
(see DOSAGE AND
ADMINISTRATION).
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 (see PRECAUTIONS).
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.
Lithium: 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.
Other agents: 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.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Quinapril hydrochloride was not carcinogenic in mice or rats when given in
doses up to 75 or
100 mg/kg/day (50 to 60 times the maximum human daily dose, respectively, on
an mg/kg basis
and 3.8 to 10 times the maximum human daily dose when based on an mg/m
2
basis) for 104
weeks. Female rats given the highest dose level had an increased incidence
of mesenteric lymph
node hemangiomas and skin/subcutaneous lipomas. Neither quinapril nor quinaprilat
were
mutagenic in the Ames bacterial assay with or without metabolic activation.
Quinapril was also
negative in the following genetic toxicology studies: in vitro mammalian cell
point mutation,
sister chromatid exchange in cultured mammalian cells, micronucleus test with
mice, in vitro
chromosome aberration with V79 cultured lung cells, and in an in vivo cytogenetic
study with rat
bone marrow. There were no adverse effects on fertility or reproduction in
rats at doses up to 100
mg/kg/day (60 and 10 times the maximum daily human dose when based on mg/kg
and mg/m
2
,
respectively).
Pregnancy
Pregnancy Categories C (first trimester) and D (second and third trimesters):
See
WARNINGS, Fetal/Neonatal Morbidity and Mortality.
Nursing Mothers
Because ACCUPRIL is secreted in human milk, caution should be exercised when
this drug is
administered to a nursing woman.
Pediatric Use
The safety and effectiveness of ACCUPRIL in pediatric patients have not been
established.
Geriatric Use
Clinical studies of ACCUPRIL did not include sufficient numbers of subjects
aged 65 and over
to determine whether they respond differently from younger subjects. Other
reported clinical
experience has not identified differences in responses between the elderly
and younger patients.
In general, dose selection for an elderly patient should be cautious, usually
starting at the low end
of the dosing range, reflecting the greater frequency of decreased hepatic,
renal or cardiac
function, and of concomitant disease or other drug therapy.
This drug is known to be substantially excreted by the kidney, and the risk
of toxic reactions to
this drug may be greater in patients with impaired renal function. Because
elderly patients are
more likely to have decreased renal function, care should be taken in dose
selection, and it may
be useful to monitor renal function.
Elderly patients exhibited increased area under the plasma concentration time
curve and peak
levels for quinaprilat compared to values observed in younger patients; this
appeared to relate to
decreased renal function rather than to age itself.
Quinapril drug information Cardiac glycoside Pharmacodynamics and clinical effects Thiazide side effects Phytosterols Mechanisms of hypokalemia Indications and usage Inhibitor effects Cardenolides Adverse effects Thiazide Digoxin Warnings Inhibitor adverse effects Clinical pharmacology Ace inhibitor Digoxin clinical use Quinapril faq Precautions Steroid