Product Overview
Composition
1 tablet contains irbesartan 300 mg;
auxiliary substances :
lactose monohydrate,
pregelatinized corn starch,
croscarmellose sodium,
poloxamer 188,
colloidal aqueous silicon dioxide,
microcrystalline cellulose,
magnesium stearate.
pharmachologic effect
Antihypertensive drug, specific antagonist of angiotensin II receptors (type AT 1 ). Eliminates the vasoconstrictor effect of angiotensin II and reduces the concentration of aldosterone in the blood plasma. Does not inhibit kinase II, an enzyme that breaks down bradykinin.
Reduces OPSS, reduces afterload. Reduces blood pressure (with a minimal change in heart rate) and pressure in the pulmonary circulation, and the decrease in blood pressure is dose-dependent.
The maximum effect of the drug develops within 3-6 hours after a single dose. The antihypertensive effect lasts for 24 hours. A stable clinical effect is achieved after 1-2 weeks of using the drug, the maximum effect is achieved by 4-6 weeks after the start of treatment. After stopping the drug intake, blood pressure gradually returns to its original value. There is no withdrawal syndrome (the effect of recoil hypertension).
April has no effect on the concentration of triglycerides, the content of cholesterol, glucose, uric acid in blood plasma or on the excretion of uric acid in the urine.
Indications
- Essential hypertension
- Nephropathy in arterial hypertension and type 2 diabetes mellitus (as part of combined antihypertensive therapy).
Application during pregnancy and lactation
Aprovel is contraindicated for use during pregnancy. If pregnancy occurs during treatment, the drug should be discontinued immediately.
If it is necessary to prescribe the drug during lactation, the issue of stopping breastfeeding should be resolved.
Contraindications
- pregnancy;
- lactation;
- children and adolescents up to 18 years old;
- hypersensitivity to the components of the drug Aprovel.
Side effects
In placebo-controlled studies (1965 patients received irbesartan), the following adverse reactions were noted.
From the side of the central nervous system: often - dizziness.
From the side of the cardiovascular system: sometimes - tachycardia, hot flashes.
From the respiratory system: sometimes - cough.
From the digestive system: often - nausea, vomiting; sometimes - diarrhea, dyspepsia, heartburn.
From the reproductive system: sometimes - sexual dysfunction.
From the side of the body as a whole: often - fatigue; sometimes - chest pain.
On the part of laboratory parameters: often - a significant increase in CPK (1.7%), not accompanied by clinical manifestations from the musculoskeletal system.
In patients with arterial hypertension and type 2 diabetes mellitus and microalbuminuria with normal renal function, orthostatic dizziness and orthostatic hypotension were observed in 0.5% of patients (more often than with placebo). In diabetic patients with high blood pressure with microalbuminuria and normal renal function, hyperkalemia (more than 5.5% mmol / L) occurred in 29.4% of patients in the group receiving irbesartan at a dose of 300 mg, and 22% of patients in the group receiving placebo.
In patients with arterial hypertension with diabetes mellitus, chronic renal failure and severe proteinuria, the following additional adverse reactions were observed in 2% of patients (more often than when taking placebo).
From the side of the central nervous system: often - orthostatic dizziness.
From the side of the cardiovascular system: often - orthostatic hypotension.
From the musculoskeletal system: often - pain in the bones and muscles.
On the part of laboratory parameters: hyperkalemia (more than 5.5% mmol / l) occurred in 46.3% of patients in the group of patients receiving irbesartan and in 26.3% of patients in the placebo group. A decrease in hemoglobin levels, which was not clinically significant, was noted in 1.7% of patients receiving irbesartan.
In the post-marketing period, the following adverse reactions were also identified:
Allergic reactions: rarely - rash, urticaria, angioedema (as in other angiotensin II receptor antagonists).
From the side of metabolism: very rarely - hyperkalemia.
From the side of the central nervous system: very rarely - headache, ringing in the ears.
From the digestive system: very rarely - dyspepsia, liver dysfunction, hepatitis.
From the musculoskeletal system: very rarely - myalgia, arthralgia.
From the urinary system: very rarely - impaired renal function (including isolated cases of renal failure in predisposed patients).
Interaction
With the simultaneous use of the drug Aprovel and thiazide diuretics, the hypotensive effect of the drugs is additive.
The simultaneous use of Aprovel with potassium-sparing diuretics, potassium preparations can lead to an increase in serum potassium.
How to take, course of administration and dosage
The initial and maintenance doses are 150 mg 1 time / day.
If necessary, the dose can be increased to 300 mg 1 time / day.
Aprovel can be taken with meals or on an empty stomach. The tablets should be swallowed whole with water.
Overdose
When taking the drug at a dose of up to 900 mg / day for 8 weeks, no toxicity was detected.
Treatment: in case of accidental intake of the drug in high doses, gastric lavage and symptomatic therapy are indicated.
Irbesartan is not removed from the body by hemodialysis.
Special instructions
Aprovel should be prescribed with caution in patients with bilateral renal artery stenosis due to the possible risk of severe arterial hypotension and acute renal failure.
Prior to the appointment of the drug Aprovel, treatment with diuretics in high doses can lead to dehydration and increases the risk of arterial hypotension at the beginning of treatment with the drug Aprovel. In dehydrated patients or in patients with sodium ion deficiency as a result of intensive diuretic treatment, restriction of salt intake from food, diarrhea or vomiting, as well as in patients on hemodialysis, dose adjustment is necessary towards its reduction.
Experimental results
In studies conducted on laboratory animals, the mutagenic, clastogenic and carcinogenic effects of the drug Aprovel have not been established.
Use in pediatrics
The safety and efficacy of the drug in children have not been established.
Influence on the ability to drive vehicles and use mechanisms
There are no indications about the effect of taking the drug Aprovel on the ability to drive vehicles and control mechanisms.
Release form
Film-coated tablets.
