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Quinapril Hydrochloride

Pronunciation: (KWIN-uh-PRILL HIGH-droe-KLOR-ide)
Class: Angiotensin-converting enzyme (ACE) inhibitor

Trade Names:
Accupril
- Tablets 5 mg
- Tablets 10 mg
- Tablets 20 mg
- Tablets 40 mg

Pharmacology

Competitively inhibits angiotensin I-converting enzyme, resulting in prevention of angiotensin I conversion to angiotensin II, a potent vasoconstrictor that also stimulates aldosterone release. Clinical consequences are decrease in BP, reduced sodium resorption, and potassium retention.

Pharmacokinetics

Absorption

T _max is 1 h for the parent drug, quinapril. T _max is 2 h for the metabolite, quinaprilat. Food decreases rate 25% and extent of absorption 30% when administered with a high-fat meal.

Distribution

Protein binding is about 97%.

Metabolism

De-esterified to major active metabolite quinaprilat (about 38% of dose).

Elimination

Renal (96% of quinaprilat) IV dose. The t _½ accumulation is about 3 h for quinaprilat; t _½ elimination is about 2 h for quinaprilat; and t _½ prolonged terminal phase is about 25 h for quinaprilat.

Onset

Within 1 h.

Peak

2 to 4 h.

Duration

24 h.

Special Populations

Renal Function Impairment

When CrCl decreases, the elimination t _½ increases for quinaprilat.

Elderly

Elimination of quinaprilat is decreased.

Heart failure

Elimination of quinaprilat is decreased.

Alcoholic cirrhosis

Quinaprilat concentrations are decreased because of impaired de-esterification of quinapril.

Indications and Usage

Treatment of hypertension; adjunctive therapy of CHF.

Contraindications

Hypersensitivity to ACE inhibitors; history of angioedema related to previous treatment with an ACE inhibitor.

Dosage and Administration

CHF
Adults

PO 5 mg twice daily initially; may increase dose weekly for clinical control, usually 20 to 40 mg in 2 equally divided doses.

Renal Function Impairment

Initial dose is 5 mg with CrCl more than 30 mL/min or 2.5 mg with CrCl 10 to 30 mL/min. If well tolerated, it may be given the following day as a twice daily regimen. In the absence of excessive hypotension or significant deterioration of renal function, the dose may be increased at weekly intervals based on clinical and hemodynamic response.

Hypertension
Adults

PO 10 or 20 mg every day initially; adjust dosage at intervals of at least 2 wk.

Adults (maintenance)

PO 20, 40, or 80 mg/day as single dose or 2 equally divided doses.

Elderly

PO 10 mg every day followed by titration to the optimal response.

Renal Function Impairment

Initial dose varies based on CrCl: more than 60 mL/min is 10 mg; 30 to 60 mL/min is 5 mg; 10 to 30 mL/min is 2.5 mg.

Storage/Stability

Store tablets at controlled room temperature (59° to 89°F). Protect from light.

Drug Interactions

Antacids

Quinapril bioavailability may be decreased. Separate administration times by 1 to 2 h.

Capsaicin

Cough may be exacerbated.

Digoxin

May cause increased or decreased digoxin levels.

Diuretics

Increased risk of hypotension.

Food

Food (especially fat) reduces bioavailability of quinapril.

Indomethacin, salicylates (eg, aspirin)

May reduce hypotensive effects, especially in low renin or volume-dependent hypertensive patients.

Lithium

May cause increased lithium levels and symptoms of lithium toxicity.

Loop diuretics

Effects of loop diuretics may be decreased.

Phenothiazines

Enhanced hypotensive effect.

Potassium supplements and potassium-sparing diuretics

Hyperkalemia.

Tetracycline

Decreased tetracycline absorption.

Laboratory Test Interactions

False elevation of liver enzymes, serum bilirubin, uric acid, and blood glucose may occur.

Adverse Reactions

Cardiovascular

Hypotension (3%).

CNS

Dizziness (8%); headache (6%); fatigue (3%).

Dermatologic

Rash (1%).

GI

Nausea, vomiting, diarrhea (2%).

Hematologic

Neutropenia; agranulocytosis.

Lab Tests

BUN (11%); serum creatinine (8%).

Metabolic

Hyperkalemia (2%).

Respiratory

Cough (4%).

Miscellaneous

Chest pain (2%); abdominal pain, back pain (1%); angioedema (0.1%); anaphylactoid reactions.

Precautions

Warnings

Pregnancy

When used in pregnancy during the second and third trimesters, ACE inhibitors can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.

Pregnancy

Category D (second, third trimester); Category C (first trimester). Avoid use in pregnant patients and discontinue drug as soon as pregnancy is detected; closely observe infants with histories of in utero exposure.

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

May show higher peak blood levels of metabolite.

Renal Function

May further decrease renal function with elevations in BUN and serum creatinine because of decreased renal perfusion. Furthermore, dosage should be reduced to compensate for reduced drug elimination.

Hepatic Function

Use drug with caution; dosage reduction may be necessary because of impaired metabolism.

Angioedema

May occur and is potentially fatal if laryngeal edema occurs. Intestinal angioedema has occurred. Use drug with extreme caution in patients with hereditary angioedema.

Cough

Chronic cough may occur during treatment; more common in women.

Hepatic failure

Rarely, ACE inhibitors have been associated with a syndrome that starts with cholestatic jaundice and progresses to fulminant hepatic necrosis and sometimes death.

Hypotension/first-dose effect

Significant decreases in BP may occur after first dose, especially in severely salt- or volume-depleted patients (eg, patients on aggressive diuretic therapy) or in those with heart failure.

Neutropenia and agranulocytosis

Have occurred rarely; risk appears greater with renal function impairment, heart failure, or immunosuppression.

Proteinuria

Has occurred with similar agents, especially with high doses or prior renal disease.

Overdosage

Symptoms

Hypotension.

Patient Information

Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
Advise patient to try to take each dose at about the same time each day
Inform hypertensive patient that drug controls, but does not cure, hypertension and to continue taking drug as prescribed even when BP is not elevated.
Caution patient not to change the dose or stop taking unless advised by health care provider.
Instruct patient to continue taking other medications for condition as prescribed by health care provider.
Instruct patient in BP and pulse measurement skills.
Advise patient to monitor and record BP and pulse at home and to inform health care provider should abnormal measurements be noted. Also advise patient to take record of BP and pulse to each follow-up visit.
Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
Instruct patient to lie or sit down if experiencing dizziness or lightheadedness when standing.
Emphasize to hypertensive patient the importance of the following other modalities on BP control: weight control, regular exercise, smoking cessation, and moderate intake of alcohol and salt.
Emphasize to heart failure patient the importance of the following other modalities that can help control heart failure symptoms: weight control, progressive exercise program, smoking cessation, and moderate intake of alcohol and salt.
Advise heart failure patient to weigh daily, keep a record of daily weights, and notify health care provider if rapid weight gain (eg, 5 pounds in 1 wk) is noted or if edema or shortness of breath worsen.
Caution patient that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to excessive fall in BP resulting in lightheadedness or fainting.
Advise patient that medication may cause dizziness or lightheadedness and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
Caution patient to avoid unnecessary exposure to UV light (sunlight, tanning booths) and to use sunscreen and wear protective clothing when exposed to UV light to avoid photosensitivity reaction.
Instruct patient to stop taking drug and immediately report any of the following symptoms to health care provider: sore throat, fever, swelling of the hands or feet, irregular heartbeat, chest pains, fainting, swelling of the face, lips, eyelids, or tongue, difficulty breathing
Instruct patient to inform health care provider if a persistent cough develops while taking this medication.
Caution patient not to take any prescription or OTC medications, potassium-containing salt substitutes, potassium supplements, or dietary supplements unless advised by health care provider.