Perindopril-Vertex, tablets 4 mg 30 pcs

Perindopril is an ACE inhibitor. It is a prodrug from which the active metabolite perindoprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I into angiotensin II, which is a powerful vasoconstrictor.

The decrease in angiotensin II concentration results in a secondary increase in plasma renin activity by eliminating the negative feedback of renin release and directly reducing aldosterone secretion.

Because of its vasodilator effect, it reduces ROSS (post-load), congestion pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; it increases cardiac minute volume and exercise tolerance.

Hypotensive effects develop within the first hour of perindopril administration, peak by 4-8 hours and last for 24 hours.

Pharmacokinetics

Perindopril is rapidly absorbed from the gastrointestinal tract after oral administration. Cmax is reached after 1 h. Bioavailability is 65-70%.

In metabolism perindopril is biotransformed to form the active metabolite – perindoprilat (about 20%) and 5 inactive compounds. Cmax of perindoprilat in plasma is reached between 3 and 5 hours after intake.

The binding of perindoprilat to plasma proteins is insignificant (less than 30%) and depends on the concentration of the active substance. Vd of free perindoprilat is close to 0.2 l/kg.

It does not cumulate. Repeated administration does not lead to cumulation and T1/2 corresponds to the period of its activity.

The metabolism of perindopril is slowed when taken with food.

The T1/2 of perindopril is 1 hour.

Perindoprilat is excreted by the kidneys; T1/2 of its free fraction is 3-5 h.

In elderly patients and in renal and heart failure, excretion of perindoprilat is slower.

Indications

Arterial hypertension, chronic heart failure.

Active ingredient

Composition

Active ingredient:

perindopril erbumin – 4 mg

Excipients:

Lactose (milk sugar),

Microcrystalline cellulose,
.

croscarmellose sodium (primellose),

magnesium stearate;

How to take, the dosage

The initial dose is 1-2 mg per day at 1 administration. Maintenance doses – 2-4 mg per day in congestive heart failure, 4 mg (less frequently – 8 mg) – in arterial hypertension at 1 visit.

In case of impaired renal function, the dosage regimen needs to be adjusted depending on the CK values.

Interaction

In concomitant use with antihypertensive agents, muscle relaxants, anesthetic agents may increase the antihypertensive effect.

Concomitant use with loop diuretics, thiazide diuretics may increase the antihypertensive effect. Significant arterial hypotension, especially after the first dose of diuretic appears to be due to hypovolemia, which leads to transient enhancement of hypotensive effect of perindopril. There is an increased risk of impaired renal function.

Concomitant use with sympathomimetics may decrease the antihypertensive effect of perindopril.

Concomitant use with tricyclic antidepressants, antipsychotics (neuroleptics) increases the risk of postural hypotension.

Concomitant use with indomethacin decreases antihypertensive effect of perindopril, probably due to inhibition by NSAIDs of prostaglandin synthesis (which is believed to play a role in development of hypotensive effect of ACE inhibitors).

Concomitant use with insulin and hypoglycemic agents with sulfonylurea derivatives may lead to hypoglycemia due to increased glucose tolerance.

In concomitant use with potassium-saving diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and food supplements containing potassium, hyperkalemia may develop (especially in patients with impaired renal function).Because ACE inhibitors decrease the content of aldosterone, which leads to potassium retention in the body against the background of potassium excretion restriction or its additional intake.

Concomitant use with lithium carbonate may decrease the excretion of lithium from the body.

Special Instructions

With caution use in renal insufficiency and severe arterial hypertension.

Before treatment with perindopril, renal function tests are recommended in all patients.

During treatment with perindopril renal function, hepatic enzyme activity in blood should be monitored regularly, peripheral blood tests should be performed (especially in patients with diffuse connective tissue diseases, in patients who receive immunosuppressive agents, allopurinol). Patients with sodium and fluid deficiency should undergo correction of water-electrolyte disorders before starting treatment.

Hemodialysis with polyacrylonitrile membranes should not be performed during treatment with perindopril (increased risk of anaphylactic reactions).

Perindopril should be used with caution concomitantly with drugs that may cause increased blood potassium levels (indomethacin, cyclosporine). Concomitant use with potassium-saving diuretics and potassium preparations is not recommended.

Contraindications

An history of angioedema, pregnancy, lactation, childhood, hypersensitivity to perindopril.

Side effects

Respiratory system: possible dry cough.

Digestive system disorders: dyspeptic phenomena, dry mouth, taste disorders.

CNS disorders: headache, sleep and/or mood disorders, dizziness; in some cases – seizures.

Hematopoietic system: decrease in hemoglobin levels (especially at the beginning of treatment); rarely – decrease in the number of red blood cells and/or platelets.

Key kidney disorders: reversible increase in creatinine and uric acid.

Allergic reactions: angioedema, skin rash, pruritus, erythema.

Other: sexual disorders.

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