Buy Generic Avapro (Irbesartan) 150, 300 mg online

Last Updated on February 19, 2017 by Dr.Derek Fhisher

Most popular brand: Avapro
Active ingredient: Irbesartan
Available dosage forms: 150, 300 mg

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Irbesartan general information

If the degree of albumin present in urine is past the normal assortment, tests should be conducted at fixed intervals with the purpose to analyze the kidney function. As cited earlier, albumin is really a serum protein that’s found within the blood plasma. All treatments were similar in their own ability to reduce blood pressure. You might need to get going on the standard and least expensive cure, diuretics.

In case your blood pressure isn’t controlled with a diuretic, you might need to bring another medication. Scroll down to learn concerning the circumstances under which albumin could possibly be present in urine alongside information on the best way to decrease albumin in urine. These topical preparations are approved by the FDA for the therapy for androgenic alopecia. Don’t drink alcohol in excessive quantities.

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Avapro (Irbesartan)

Avapro (Irbesartan original) – the official instruction manual. Prescription drug information is intended only for healthcare professionals!

Clinico – pharmacological group:

angiotensin II receptor antagonists

Mode of action

antihypertensive drug, a selective angiotensin II receptor (AT1 type).

Blocks all physiologically relevant effects of angiotensin II of, realized through the AT1 – receptors, regardless of the source or route of synthesis of angiotensin II. Specific antagonizing AT1 – receptors leads to increased concentrations of renin and angiotensin II in the blood plasma concentration and a decrease in plasma aldosterone. When used in the recommended doses of the drug potassium ion concentration in the serum does not change.

Irbesartan not inhibit kininase II (ACE), with which, the formation of angiotensin II and destruction of bradykinin to inactive metabolites. For the manifestation of its effects Irbesartan does not require metabolic activation.

Irbesartan lowers blood pressure with minimal change in heart rate. When taken in doses up to 300 mg 1 time per day reduction in blood pressure is dose-dependent, but with further increase in the dose of the hypotensive effect of irbesartan growth is negligible.

The maximum reduction in blood pressure is achieved within 3 – 6 hours after ingestion of the drug and the antihypertensive effect persists for at least for 24 hours after 24 hours after taking the recommended dose reduction of blood pressure is 60 -. 70% in comparison with the maximum decrease in diastolic and systolic blood pressure in response to use of the drug. When you receive a 1 time a day at a dose of 150 – 300 mg of the degree of blood pressure reduction (systolic / diastolic) at the end of the dosing interval (ie 24 hours after dosing) with the patient lying or sitting by an average of 8 – 13/5 – 8 mm Hg. Art. (Respectively) compared with placebo.

The drug at a dose of 150 mg 1 time per day is the same hypotensive response (decrease in blood pressure before taking the next dose and mean blood pressure reduction over 24 hours) as well as receiving the same dose divided into 2 doses.

The antihypertensive effect of the drug Avapro ® It develops within 1 – 2 weeks, and maximum therapeutic effect is achieved after 4 – 6 weeks after the start of treatment. The antihypertensive effect is maintained in long-term treatment. After cessation of treatment blood pressure gradually returns to the initial value, withdrawal symptoms were observed.

Irbesartan has no effect on uric acid in the serum or on the excretion of uric acid in the urine.

The effectiveness of the drug Avapro ® It does not depend on age and sex.

Patients blacks less responsive to monotherapy Avapro ® (As well as all other drugs that affect the RAAS).

Pharmacokinetics

Once inside well absorbed from the gastrointestinal tract. Cmax of irbesartan in plasma achieved through 1.5 – 2 hours after ingestion. The absolute bioavailability is 60 – 80%. Simultaneous food intake does not significantly affect the bioavailability of the drug.

Irbesartan has linear pharmacokinetics and dose proportional in the dose range from 10 to 600 mg; at doses greater than 600 mg (2-fold higher than the maximum recommended dose) becomes nonlinear kinetics of irbesartan (decrease absorption).

The binding to plasma proteins is approximately 96%. Binding to cellular components of blood is insignificant. Vd – 53 – 93 liters. When taken daily 1 times a day Css achieved within 3 days. Repeated receptions 1 time per day is celebrated a limited accumulation of irbesartan in plasma (less than 20%).

Once inside, or on / in the 14C – irbesartan is 80 – 85% of the radioactivity in the circulation falls on unchanged irbesartan.

Irbesartan biotransformed in the liver by oxidation and conjugation with glucuronic acid. Irbesartan is oxidized mainly by isoenzyme CYP2C9, CYP3A4 isozyme involved in the metabolism of irbesartan is negligible. The main metabolite, which is in the systemic circulation – irbesartan glucuronide (about 6%).

The total clearance and renal clearance was 157 – 176 ml / min and 3 – 3.5 ml / min, respectively. The final T1 / 2 is 11 – 15 hours Irbesartan and its metabolites are excreted in the bile and urine.. After ingestion or on / in the 14C – about 20% irbesartan radioactivity found in the urine and the rest – in the feces. Less than 2% of the administered dose is excreted in the urine as unchanged irbesartan.

Pharmacokinetics in special clinical situations

The somewhat higher plasma concentrations of irbesartan were observed in women (compared to men). However, the differences in the value of T1 / 2 and accumulation of irbesartan are not revealed. Correction doses of irbesartan in women is required. The values ​​of AUC and Cmax of irbesartan were slightly higher in elderly patients (≥ 65 years) than in younger patients, but the values ​​of the final T1 / 2 were not significantly different. Correction doses of irbesartan in elderly patients is not required.

In patients with impaired renal function or patients undergoing hemodialysis, pharmacokinetics of irbesartan are not significantly altered. Irbesatan not removed from the body during hemodialysis.

In patients with cirrhosis of mild or moderate flow pharmacokinetic parameters of the drug did not significantly change. Pharmacokinetic studies in patients with severe hepatic impairment have not been conducted.

Indications

• Essential hypertension;
• nephropathy in patients with hypertension and type 2 diabetes (as part of combination antihypertensive therapy).

Dosage

The drug, taken orally, the tablet is swallowed whole with water.

The initial and maintenance dose is 150 mg 1 time per day regardless of the meal. Use of the drug in a dose provides a more optimal 24 – hour blood pressure control than 75 mg per day. However, in some cases, especially in patients who are on hemodialysis or in patients over the age of 75 years, the starting dose should be 75 mg (may use Avaproya in tablets of 75 mg).

In case of insufficient therapeutic effect of the application of the drug Avapro ® 150 mg 1 time per day, the dose can be increased to 300 mg or to assign another antihypertensive agent. In particular it has been shown that administration of a diuretic such as hydrochlorothiazide, increases the effects of Avaproya.

In patients with hypertension and type 2 diabetes, treatment should be started at a dose of 150 mg 1 time per day and gradually increase to 300 mg – dose, which is the preferred maintenance dose for the treatment of nephropathy.

Evidence of the beneficial effects of the drug Avapro ® the kidneys in patients with hypertension and type 2 diabetes comes from studies in which it was used in combination with other antihypertensive drugs necessary to achieve target levels of blood pressure.

In patients with impaired water – electrolyte balance before you start taking Avaproya to restore the BCC and / or eliminate hyponatremia.

In patients with impaired renal function correct dosing regimen is required. For patients on hemodialysis, the initial dose should be 75 mg per day (possible use of the drug Avapro ® in tablets of 75 mg).

In patients with impaired hepatic function or mild to moderate severity is not required correction mode. Clinical experience with the drug in patients with severe hepatic impairment is not.

Although the recommended treatment for patients over the age of 75 years, starting with a dose of 75 mg (possible use of the drug Avapro ®. In Table 75 mg), usually elderly patients correct dosing regimen is not required.

The safety and efficacy of the drug in patients with children and youth are not set.

Side effects

Determination of the frequency of adverse reactions: very often (> 1/10), often (> 1/100,> 1/10), occasionally (> 1/1000,> 1/100), rare (> 1/10 000,> 1/1000), very rare (> 1/10 000), including isolated cases.

The frequency of adverse events in the placebo – kontoliruemyh studies did not depend on the dose (in the recommended dose range), gender, age, race, duration of patient care or.

In the placebo – controlled studies (1965 patients received irbesartan) were observed following adverse reactions.

On the part of the central nervous system: often – dizziness.

Cardio – vascular system: sometimes – tachycardia, flushing of the skin.

With the respiratory system: sometimes – cough.

From the digestive system: often – nausea, vomiting; sometimes – diarrhea, dyspepsia, heartburn.

From the reproductive system: sometimes – sexual dysfunction.

On the part of the body as a whole: often – fatigue; sometimes – pain in the chest.

From the laboratory parameters: often – a significant increase in creatine kinase (1.7%), not accompanied by clinical manifestations on the part of the bone – muscular system.

Hypertension and type 2 diabetes with renal disease

Besides adverse reactions identified in patients with hypertension in patients with hypertension, type 2 diabetes with microalbuminuria without disrupting kidney function when taking irbesartan orthostatic dizziness and orthostatic hypotension were observed in 0.5% of patients (compared to the frequency of occurrence of these side reactions with placebo).

In patients with hypertension, type 2 diabetes with severe proteinuria and chronic renal insufficiency the following adverse reactions were observed in> 2% of patients (compared to the frequency of their occurrence with placebo).

From the nervous system: often – orthostatic dizziness.

Cardio – vascular system: often – orthostatic hypotension.

From the bone – muscular system: often – pain in the muscles and bones.

From the laboratory parameters: hyperkalemia when taking irbesartan patients with diabetes are more common than with placebo. Diabetic patients with high blood pressure and microalbuminuria with normal renal function, hyperkalemia (> 5.5% mmol / l) while taking irbesartan 300 mg was observed in 29.4% of patients (often) in the placebo group – 22% of patients. Diabetic patients with high blood pressure, chronic renal failure and severe proteinuria, hyperkalemia (> 5.5% mmol / l) while taking irbesartan was observed in 46.3% of patients (often) in the placebo group – in 26.3% of patients. In patients with high blood pressure and diabetic nephropathy treated with irbesartan, from 1.7% of patients with clinically non-significant decrease in hemoglobin concentration (often).

Since the introduction of irbesartan on the market the following adverse reactions have also been identified:

Allergic reactions: seldom – rash, urticaria, angioedema.

On the part of metabolism: rarely – hyperkalemia.

From the nervous system: very rarely – headache.

On the part of the organ of hearing: very rarely – ringing in the ears.

From the digestive system: very rarely – dysgeusia (taste perversion), hepatic dysfunction, hepatitis.

From the bone – muscular system: very rarely – myalgia, arthralgia (sometimes in combination with an increase in creatine kinase levels), convulsions.

From the urinary system: rarely – renal dysfunction, including isolated cases of renal failure in patients at risk.

Contraindications

• hereditary galactose intolerance, lactase deficiency or malabsorption of glucose and galactose;
• pregnancy;
• lactation;
• childhood and adolescence to 18 years (effectiveness and safety have installed);
• increased sensitivity to the drug.

With care use in patients with stenosis of the aortic or mitral valve, hypertrophic obstructive cardiomyopathy, dehydration, hyponatremia, diarrhea, vomiting, a diet with limited consumption of salt, diuretic therapy, bilateral renal artery stenosis, unilateral stenosis of the artery to a solitary kidney, chronic heart failure III – IV NYHA functional class classification, ischemic heart disease and / or atherosclerotic lesions of the brain vessels, hyperkalemia, renal failure, hemodialysis, a recent kidney transplantation (lack of clinical application experience), severe hepatic insufficiency (lack of clinical application experience)

Pregnancy and lactation

Avapro ® (Like any other drug that acts directly on the RAAS) is contraindicated during pregnancy. If pregnancy occurs during treatment with the drug should be discontinued immediately.

Go to the appropriate alternative therapy should be carried out before the start of pregnancy planning.

It is not known whether irbesartan is excreted in breast milk. Avapro ® contraindicated during lactation (breastfeeding).

Application for violations of liver function

In patients with mild to moderate impaired liver function dose adjustment is required. Data on the use of the drug in patients with hepatic impairment is not severe.

Application for violations of renal function

Be wary appointed during hemodialysis, l unilateral or bilateral renal artery stenosis, renal failure.

In patients with renal insufficiency (without electrolyte metabolism disorders) dose adjustment is required. For patients on hemodialysis, the recommended starting dose is 75 mg per day.

The use in elderly patients

Although the recommended treatment for patients over the age of 75 years, starting with a dose of 75 mg (possible use of the drug Avapro ® in tablets of 75 mg), usually elderly patients correct dosing regimen is not required.

The use in children under the age of 12 years

is contraindicated: childhood and adolescence to 18 years (effectiveness and safety have not been established).

Cautions

violation of water – electrolyte balance

When dehydration and / or hyponatremia (as a result of intensive treatment with diuretics, diarrhea or vomiting, limit dietary salt intake), and in patients on hemodialysis can develop clinically significant hypotension, especially after the first dose of the drug. These pathological conditions need to be adjusted before the start of the use of the drug Avapro ®.

Patients with bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, taking other drugs that affect the RAAS, are at high risk with regard to the development of severe arterial hypotension or renal failure. Although the development of such complications for Avapro drug ® does not disclose the possibility of this effect must be considered in applying the angiotensin II receptor antagonists.

Kidney failure and kidney transplant

In the application Avaproya in patients with renal impairment is recommended periodic monitoring of potassium and creatinine serum. No clinical data regarding the use of Avapro drug ® in patients undergoing kidney transplantation.

Hypertension and type 2 diabetes with renal disease

The noted in the application of the drug Avapro ® a beneficial effect against progression of renal and cardio – vascular lesions had varying degrees of severity in different groups of patients: less pronounced were women and persons who do not belong to the European race.

Perhaps the development of hyperkalemia when using the drug Avapro ® (As well as the use of other agents affecting RAAS), especially in patients with renal failure and / or heart disease. For patients at risk is recommended adequate control of the level of potassium in the blood serum.

stenosis of the aortic or mitral valve, obstructive hypertrophic cardiomyopathy

As with other vasodilators, in the appointment of the drug Avapro ® patients with aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy requires caution.

Patients with primary aldosteronism generally do not respond to anti-hypertensive drugs that inhibit the renin system – angiotensin. Therefore, the use Avaproya in such cases is not advisable.

In the group of patients who vascular tone and renal function is predominantly dependent on the activity of the RAAS (e.g., patients with chronic heart failure III and IV functional class classification NYHA or concomitant renal disease, including renal artery stenosis), treatment with ACE inhibitors has been associated with acute hypotension, azotemia, oliguria, and in rare cases – acute renal insufficiency. As with other antihypertensive agents, a significant reduction in blood pressure in patients with coronary artery disease can lead to myocardial infarction or stroke. Treatment should be under the control of blood pressure.