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Perindopril Erbumine

Pronouncation: (per-IN-doe-pril er-BUE-mine)
Class: Angiotensin-converting enzyme (ACE) inhibitor

Trade Names:
Aceon
- Tablets 2 mg
- Tablets 4 mg
- Tablets 8 mg

Coversyl (Canada)

Pharmacology

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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 a decrease in BP, reduced sodium resorption, and potassium retention.

Pharmacokinetics

Absorption

Rapid absorption. Bioavailability is approximately 75% (perindopril) and approximately 25% (active metabolite perindoprilat). Food reduces bioavailability 35%. Steady state is 3 to 6 days. T _max is approximately 1 h (perindopril) and 3 to 7 h (active metabolite perindoprilat).

Distribution

Protein binding is 60% (perindopril) and 10% to 20% (active metabolite perindoprilat).

Metabolism

Extensively metabolized in liver to active metabolite perindoprilat and other metabolites by glucuronidation and cyclization via dehydration.

Elimination

Urine (4% to 12% unchanged, 4.5% to 22% as metabolites). Mean total body Cl is 219 to 362 mL/min and mean renal Cl is 23.3 to 28.6 mL/min (perindopril). The t _½ is 0.8ߙto 1 h (perindopril). Apparent mean t _½ is 30 to 120 h (metabolite perindoprilat).

Special Populations

Renal Function Impairment

CrCl is 30 to 80ߙmL/min; metabolite AUC is approximately doubled.

Hepatic Function Impairment

Bioavailability of metabolite is increased, and plasma concentrations are approximately 50% higher.

Elderly

Plasma concentrations of perindopril and metabolite are approximately twice those observed in younger patients; renal excretion of metabolite decreases (70 yr of age and older).

Heart failure patients

Metabolite Cl is reduced in CHF, resulting in 40% higher dose interval AUC.

Indications and Usage

Reduce risk of CV mortality or nonfatal MI in patients with stable coronary artery disease; treatment of essential hypertension.

Contraindications

Hypersensitivity or history of angioedema related to ACE inhibitor treatment.

Dosage and Administration

Renal Function Impairment
Adults (CrCl above 30ߙmL/min)

PO Initial dose is 2 mg/day (max, 8 mg/day).

Stable Coronary Artery Disease
Adults

PO Initial dosage 4 mg once daily for 2 wk; then increase as tolerated to a maintenance dosage of 8 mg once daily. In patients older than 70 yr of age, start with 2 mg once daily for the first week, followed by 4 mg once daily the second week, and 8 mg once daily for maintenance as tolerated.

Uncomplicated Hypertension
Adults

PO Initial dosage 4 mg once daily; then titrate upward until BP, measured just before the next dose, is controlled (max, 16 mg/day). Usual maintenance dose is 4 to 8 mg/day.

Patients older than 65 yr of age

PO Initial dose 4 mg/day in 1 or 2 divided doses; then titrate upward until BP, measured just before the next dose, is controlled (max, 8ߙmg/day).

Use with Concomitant Diuretics
Adults

PO If BP is not adequately controlled with perindopril alone, a diuretic may be added. In patients being treated with a diuretic, to reduce the likelihood of the occurrence of symptomatic hypotension, discontinue the diuretic 2ߙto 3 days prior to beginning perindopril. If the diuretic cannot be discontinued, use an initial dose of perindopril 2 to 4 mg/day and titrate the dose as previously described.

General Advice

Administer without regard to meals. Administer with food if GI upset occurs.

Storage/Stability

Store tablets at controlled room temperature (68° to 77°F). Protect from moisture.

Drug Interactions

Capsaicin

May increase cough.

Digoxin

May cause increased or decreased digoxin levels.

Diuretics

Increased risk of excessive BP reduction.

Drugs capable of increasing serum potassium (eg, cyclosporine, heparin, indomethacin), potassium-sparing diuretics (eg, spironolactone), potassium supplements

Increased risk of hyperkalemia.

Indomethacin

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

Lithium

Increased risk of lithium toxicity.

Loop diuretics

Effects of loop diuretics may be decreased.

Phenothiazines

Enhanced hypotensive effects.

Salicylates (eg, aspirin)

The hypotensive and vasodilator effects of perindopril may be reduced.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitation (1%).

CNS

Dizziness (8%); cerebrovascular accident (0.2%).

EENT

Sinusitis (5%); ear infection (1%).

GI

Dyspepsia (2%).

Genitourinary

Proteinuria (2%).

Hematologic

Agranulocytosis; neutropenia.

Metabolic

Hyperkalemia.

Respiratory

Cough (12%); pulmonary fibrosis (less than 0.1%).

Miscellaneous

Back pain (6%); hypertonia, upper extremity pain, viral infection (3%); fever (2%); anaphylactoid reactions (0.3% to 1%); angioedema (0.1%).

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.

Monitor

In hypertensive patients with unilateral or bilateral renal artery stenosis, increases in BUN and serum creatinine may occur; therefore, monitor renal function during the first few weeks of therapy.

Pregnancy

Category C (first trimester); Category D (second and third trimesters).

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Changes in renal function may occur in susceptible individuals.

Angioedema

May occur and is potentially fatal if laryngeal edema occurs. Use drug with extreme caution in patients with history of angioedema.

CHF

In CHF patients, where renal function may depend on renin angiotensin-aldosterone system activity, perindopril treatment may be associated with oliguria and progressive azotemia, and, rarely, acute renal failure or death.

Cough

Chronic nonproductive cough may occur.

Hepatic failure

Hepatic failure has occurred rarely with other ACE inhibitors.

Hypotension

Symptomatic hypotension may occur.

Neutropenia and agranulocytosis

Has occurred rarely with other ACE inhibitors; risk appears greater with renal function impairment, heart failure, or immunosuppression. Ensure that CBC with differential is evaluated prior to starting therapy, at 2-wk intervals for 3 mo and then periodically thereafter in patients at risk.

Overdosage

Symptoms

Circulatory arrest, death, hypotension, hypothermia.

Patient Information

Advise patient to take once or twice daily as prescribed, 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 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 BP medications 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 if abnormal measurements are 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 importance of the following other modalities on BP control: moderate intake of alcohol and salt, regular exercise, smoking cessation, and weight control.
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 ultraviolet (UV) light (eg, 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: chest pains; difficulty breathing; fainting; fever; irregular heartbeat; sore throat; swelling of the hands or feet; swelling of the face, lips, eyelids, or tongue.
Instruct patient to inform health care provider if a persistent cough develops while taking medication.
Caution patient not to take any prescription or OTC medications, potassium-containing salt substitutes, potassium supplements, herbal preparations, or dietary supplements unless advised by health care provider.