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Avapro

Avapro
Avapro Irbestan is used for arterial hypertension, nephropathy in arterial hypertension and type 2 diabetes mellitus (as part of combined antihypertensive therapy).

Brand: Irbesartan

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: September 2023
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Avapro 300 mg
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Avapro 150 mg
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Product description

Pharmacological action of Avapro Irbestan

Buy Avapro Irbestan tablets in Canada

Antihypertensive agent, angiotensin II receptor antagonist. Blocks AT1-receptors, which leads to a decrease in the biological effects of angiotensin II, incl. vasoconstrictor action, stimulating effect on the release of aldosterone and activation of the sympathetic nervous system. As a result, blood pressure decreases.

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.

Does not affect the concentration of triglycerides, cholesterol, glucose, uric acid in the blood plasma or the excretion of uric acid in the urine.

Pharmacokinetics

Avapro Irbestan logo

After oral administration, it is well absorbed from the gastrointestinal tract. Cmax of irbesartan in blood plasma is reached within 1.5-2 hours after oral administration. Bioavailability is 60-80%. Concomitant food intake does not affect the bioavailability of irbesartan.

Plasma protein binding is about 96%. Vd - 53-93 l. Css is reached within 3 days after the start of taking irbesartan 1 time / day. With repeated doses 1 time / day, there is a limited accumulation of irbesartan in plasma (less than 20%).

After ingestion of14C-irbesartan, 80-85% of the radioactivity in the circulating blood falls on unchanged irbesartan.

Irbesartan is metabolized in the liver by conjugation to form glucuronide and by oxidation. The main metabolite is irbesartan glucuronide (about 6%).

In the therapeutic dose range, irbesartan is characterized by linear pharmacokinetics, and T1/2 in the terminal phase is 11-15 hours. Total clearance and renal clearance are 157-176 ml / min and 3-3.5 ml / min, respectively. Irbesartan and its metabolites are excreted in bile and urine.

In patients with impaired renal function, cirrhosis of the liver of moderate severity, the pharmacokinetic parameters of irbesartan do not change significantly.

Indications of the active substances of the drug Irbesartan

  • Arterial hypertension.
  • Nephropathy in patients with arterial hypertension and type 2 diabetes mellitus (as part of combination antihypertensive therapy).

Dosing regimen of Avapro Irbestan

Appearance of Avapro Irbestan tablets

The initial dose is 150 mg, if necessary, the dose is increased to 300 mg. In some cases (hypochlorite diet, treatment with certain diuretics, vomiting or diarrhea preceding treatment, hemodialysis), a lower initial dose is used.

Irbesartan is taken orally 1 time / day, preferably at the same time of the day.




Interaction

Diuretics and other antihypertensive drugs. Thiazide diuretics enhance the effect. Previous treatment with high doses of diuretics can lead to dehydration and increase the risk of arterial hypotension at the beginning of treatment with irbesartan. Irbesartan is compatible with other antihypertensive drugs (beta-blockers, calcium channel blockers).

Potassium supplements and potassium-sparing diuretics. Increases the risk of developing hyperkalemia when used together with potassium-sparing diuretics and potassium preparations.

Lithium: A reversible increase in serum lithium concentrations or toxicity has been observed with concomitant use of lithium with angiotensin-converting enzyme inhibitors. For irbesartan, similar effects have so far been extremely rare, but during concomitant use of the drugs, careful monitoring of serum lithium levels is recommended.

NSAIDs: with the simultaneous administration of angiotensin II antagonists and NSAIDs (for example, selective COX-2 inhibitors, acetylsalicylic acid> 3 g / day and non-selective NSAIDs), a weakening of the hypotensive effect may occur.

As with ACE inhibitors, the combined use of angiotensin II antagonists and NSAIDs may increase the risk of impaired renal function, including the likelihood of acute renal failure, and lead to an increase in serum potassium, especially in patients with already impaired renal function. When administering this combination, precautions should be taken, especially in elderly patients. Patients need to undergo appropriate hydration and during the entire combination therapy and periodically after its completion, monitor renal function.

Hydrochlorothiazide. The pharmacokinetics of irbesartan does not change when used together with hydrochlorothiazide.

Irbesartan is metabolized mainly with the participation of CYP2C9 and, to a lesser extent, glucuronidation. No significant pharmacokinetic or pharmacodynamic interactions were observed with the combined administration of irbesartan with warfarin, a drug metabolized by CYP2C9. The effect of CYP2C9 stimulants such as rifampicin on the pharmacokinetics of irbesartan has not been evaluated.

Irbesartan does not alter the pharmacokinetics of digoxin.

Overdose

Symptoms: arterial hypotension, tachycardia or (less often) bradycardia.

Treatment: induction of vomiting and / or gastric lavage, administration of activated charcoal, symptomatic therapy; hemodialysis is ineffective.

Routes of administration

Inside.

Precautions for the substance

Irbesartan should be used with caution in patients with hyponatremia (diuretic treatment, restriction of salt intake with diet, diarrhea, vomiting), in patients on hemodialysis (symptomatic hypotension may develop), as well as in dehydrated patients. Caution should be exercised in patients with renovascular hypertension due to bilateral renal artery stenosis or renal artery stenosis of a solitary kidney (increased risk of severe hypotension and renal failure), aortic or mitral stenosis, obstructive hypertrophic cardiomyopathy, severe heart failure (III-IV classification NYHA) and ischemic heart disease (increased risk of myocardial infarction, angina pectoris). In the presence of impaired renal function, monitoring of serum potassium and creatinine levels is recommended. It is not recommended for use in patients with primary hyperaldosteronism, with severe renal failure (no experience of clinical use), in patients with recent kidney transplantation (no experience of clinical use).


Side effects of the substance Irbesartan

From the nervous system and sensory organs: ≥1% - headache, dizziness, fatigue, anxiety / excitability.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): ≥1% - tachycardia.

Respiratory system: ≥1% - upper respiratory tract infections (fever, etc.), sinusopathy, sinusitis, pharyngitis, rhinitis, cough.

From the digestive tract: ≥1% - diarrhea, nausea, vomiting, dyspeptic symptoms, heartburn.

On the part of the musculoskeletal system: ≥1% - musculoskeletal pain (including myalgia, pain in the bones, chest).

Allergic reactions: ≥1% - rash.

Others: ≥1% - abdominal pain, urinary tract infections.