Pharmacological Class:
ACE inhibitor + calcium channel blocker (dihydropyridine).

Active Ingredient(s):
Perindopril arginine, amlodipine; 3.5mg/2.5mg, 7mg/5mg, 14mg/10mg; tablets.

Company
Symplmed
Indication(s):
Hypertension.

Pharmacology:
Perindopril is a prodrug of perindoprilat, which inhibits angiotensin converting enzyme (ACE) in humans and animals. Inhibition of ACE results in decreased plasma angiotensin II, leading to decreased vasoconstriction, increased plasma renin activity and decreased aldosterone secretion.

Amlodipine is a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. It is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.

Clinical Trials:
The efficacy of Prestalia was eva luated in two randomized controlled trials. The highest strength of Prestalia (14mg/10mg) was studied in a double-blind, active controlled study in a total of 837 hypertensive patients randomized to receive Prestalia 14mg/10mg, perindopril erbumine 16mg, or amlodipine 10mg once daily for 6 weeks. At Week 6, Prestalia 14mg/10mg demonstrated statistically significantly greater reductions in blood pressure than the other treatment groups. Treatment with Prestalia reduced 10.1/6.3mmHg more than the perindopril erbumine 16mg group and 3.9/2.5mmHg more than the amlodipine 10mg group.

In a second study, the lowest strength of Prestalia (3.5mg/2.5mg) was assessed in a total of 1,581 hypertensive patients randomized to receive Prestalia 3.5mg/2.5mg, perindopril arginine 3.5mg, perindopril arginine 5mg, amlodipine 2.5mg, amlodipine 5mg, or placebo. At Week 8, Prestalia 3.5mg/2.5mg demonstrated statistically significantly greater reductions in blood pressure than the perindopril arginine 3.5mg and amlodipine 2.5mg treatment groups. Treatment with Prestalia 3.5mg/2.5mg reduced 7.2/4.1mmHg more than the placebo group.

For more clinical trial data, see full labeling.

Legal Classification:
Rx

Adults:
Initially 3.5mg/2.5mg once daily. Adjust at 7–14 day intervals; max 14mg/10mg once daily.

Children:
Not established.

Contraindication(s):
History of ACEI-associated or other angioedema. Concomitant aliskiren in patients with diabetes.

Warnings/Precautions:
Fetal toxicity may develop; discontinue if pregnancy is detected. Discontinue if angioedema, laryngeal edema occurs. Severe obstructive coronary artery disease. Salt/volume depletion. Severe aortic stenosis. Surgery. Monitor for hyperkalemia. Diabetes. Renal artery stenosis. Severe CHF. Post-MI. Monitor renal function periodically during treatment; consider withholding or discontinuing if significant renal dysfunction occurs. Dialysis. Heart failure, hepatic or renal (CrCl <60mL/min) impairment, elderly (>65yrs): not recommended. Pregnancy (Cat.D). Nursing mothers: not recommended.

Interaction(s)
See Contraindications. Potentiated by diuretics. Risk of hyperkalemia with K+ supplements, K+ sparing diuretics, or other drugs (eg, indomethacin, heparin, cyclosporine). May increase lithium levels; monitor. Nitritoid reactions with concomitant injectable gold (eg, sodium aurothiomalate); rare. May be antagonized by, and renal toxicity potentiated by, NSAIDs, including selective COX-2 inhibitors (monitor renal function periodically in elderly and/or volume depleted). Dual inhibition of the renin-angiotensin system with ARBs, ACEIs, or aliskiren may increase risk of hypotension, hyperkalemia, renal function changes; monitor closely. Concomitant aliskiren in renal impairment (CrCl <60mL/min): not recommended. Potentiates simvastatin; limit simvastatin dose to 20mg daily. Monitor cyclosporine levels. May be potentiated by moderate or strong CYP3A inhibitors (eg, diltiazem, itraconazole). Monitor BP if coadministered with CYP3A4 inducers.

Adverse Reaction(s)
Edema, cough, headache, dizziness; angioedema, hypotension, hyperkalemia.

How Supplied:
Tabs—90

LAST UPDATED:
8/7/2015