Pharmacological action Benicar 40 mg
Benicar Olmesartan medoxomil – a potent, selective antagonist of angiotensin II (type AT 1), which inhibits the effects of angiotensin II, AT1 receptor-mediated, regardless of the source and path of synthesis of angiotensin II. Selective antagonism of AT1 receptors and ngiotenzina II leads to increased concentrations of renin, angiotensin I and II in plasma, as well as some reduction in the concentration of aldosterone. Olmesartan medoxomil for hypertension causes a dose-dependent, prolonged reduction in blood pressure. No information about the development of arterial hypotension after the first dose of the drug, tachyphylaxis during prolonged treatment and withdrawal.
Dosing of olmesartan medoxomil once a day provides effective and smooth blood pressure reduction over 24 h. The maximum antihypertensive effect was achieved after 8 weeks of therapy, although a significant effect of BP reduction observed after 2 weeks of treatment.
Pharmacokinetics Benicar 40 mg
Olmesartan medoxomil is a prodrug. It quickly turns into a pharmacologically active metabolite of olmesartan under the action of esterases in the intestinal mucosa and blood in the portal vein during absorption in the digestive tract. In blood plasma, or allotments olmesartan medoxomil non-decayed or unmodified side chain medoksomilnoy group was not determined.
The average value of the absolute bioavailability of olmesartan when used in tablet dosage form is 25.6%. The maximum concentration of olmesartan in plasma reached an average of approximately 2 hours after oral administration and increases almost linearly with increasing oral dose taken once to 80 mg. Simultaneous food intake does not affect the bioavailability of olmesartan. Binding of olmesartan to plasma proteins is 99.7%, but the potential for clinically significant shift values of binding to proteins in the interaction of olmesartan with other drugs that have a high degree of protein binding, low (this is confirmed by the fact that there is no clinically significant interaction between olmesartanom and warfarin). Olmesartan is excreted in the urine (approximately 40%) and bile (approximately 60%), during its half-life of 10-15 hours of cumulation of olmesartan did not notice.
Statement Benicar 40 mg
Hypertension.
Dosage regimen Benicar 40 mg
Adults
The initial daily dose of olmesartan medoxomil – 10 mg. If blood pressure is reduced sufficiently, the dose was increased to the optimal daily – 20 mg. If necessary, the dose may be increased to the maximum – 40 mg / day. The drug is taken daily at the same time, with or without food.
Elderly patients
There is usually no need for correction of dose for elderly patients (see the recommended dose for patients with impaired renal function). If necessary, increase the daily dose to a maximum of 40 mg / day increase should be under careful control of blood pressure.
Patients with impaired renal function, mild or moderate (creatinine clearance – 20-60 ml / min).
The maximum daily dose for these patients is 20 mg. To enhance the action of drugs used hydrochlorothiazide.
Contraindications Benicar 40 mg
Hypersensitivity to the active ingredient or one of the other components of the drug during pregnancy and lactation, obstruction of the biliary tract, children and adolescents under the age of 18 years.
Side effects of Benicar 40 mg
Olmesartan medoxomil safety evaluation was performed in 3825 patients, including 3275 patients treated in controlled clinical trials. At the same time 900 patients therapy was carried out at least 6 months, more than 525 patients – at least 1 year.
Side effects were observed in placebo-controlled clinical trials with a frequency of more than 1% of patients treated with olmesartan medoxomil, but also were marked with the same or greater frequency in patients receiving placebo: back pain, bronchitis, increased creatine, diarrhea , headache, hematuria, hyperglycemia, hypertriglyceridemia, influenza-like symptoms, pharyngitis, rhinitis, and sinusitis.
The frequency of cough was similar in the placebo group (0.7%) and patients treated with olmesartan medoxomil (0.9%).
Below are some other (potentially important) side effects that occurred with a frequency of 0.5% and could be related to treatment were observed in the treatment of more than 3100 patients with hypertension when monotherapy olmesartanom medoksomilom in controlled or open trials.
The nervous system and sensory organs: vertigo.
Cardio-vascular system and blood (hematopoiesis, hemostasis): chest pain, tachycardia.
From the digestive tract: abdominal pain, dyspepsia, gastroenteritis, nausea, high cholesterol.
On the part of the musculoskeletal system: arthralgia, arthritis, myalgia.
For the skin: rash.
Other: Peripheral edema, hyperlipemia, hyperuricemia.
Allergic reaction: swelling of the face was recorded in 5 patients receiving olmesartan medoxomil.
Laboratory tests: a slight decrease in hemoglobin and hematocrit, elevated liver enzymes and / or bilirubin. In controlled clinical trials, clinically important changes in standard laboratory parameters were associated with receiving olmesartan medoxomil is very rare.
Post-marketing experience
Asthenia, vomiting, rhabdomyolysis, acute renal failure, increase in serum creatinine level, alopecia, urticaria, pruritus, angioedema.
Cautions Benicar 40 mg
Due to the lack of sufficient clinical experience does not recommend the use of olmesartan medoxomil in patients with severe renal insufficiency (creatinine clearance ≤ 20 mL / min) in patients with impaired liver function.
If the patient before the appointment of olmesartan medoxomil received intensive therapy with diuretics, salt-free diet or to comply, he had diarrhea and / or vomiting after the first dose of the drug may develop hypotension as a result of reducing the BCC. It is therefore necessary to eliminate the possibility of hypovolemia before starting treatment olmesartan medoksomilom.
It should be used with caution olmesartan medoxomil in patients with heart failure, kidney disease, renal artery stenosis in both kidneys or only because of the risk of acute hypotension, azotemia, oliguria, acute renal failure. When treating patients with impaired renal function is recommended that periodic monitoring of potassium levels and serum creatinine.
Caution should be exercised when using olmesartan medoxomil in patients with stenosis of the aortic or mitral valves or obstructive hypertrophic cardiomyopathy.
Patients with primary hyperaldosteronism do not respond to ACE inhibitors, therefore, olmesartan medoxomil assign them is not recommended.
Keep in mind that excessive lowering of blood pressure in patients with coronary artery disease or atherosclerosis of cerebral vessels can lead to myocardial infarction or ischemic stroke.
Olmesartan medoxomil at application time to time there may be dizziness or fatigue, which must be considered in patients driving or / and service facilities.
The drug contains lactose, so it should not be used in patients with hereditary intolerance to galactose lactase deficiency or malabsorption syndrome glucose / galactose.
Overdose Benicar 40 mg
Data on overdose are limited. Most likely it is a manifestation of arterial hypotension. In case of overdose, the patient requires medical supervision and on the testimony of symptomatic, supportive therapy to increase blood pressure. Data on the possibility of removing olmesartan medoxomil by dialysis does not.
Drug Interactions Benicar 40 mg
When used with other antihypertensive drugs olmesartan medoxomil effect can be amplified.
When olmesartan medoxomil simultaneous use of NSAID may reduce its antihypertensive effect and risk of acute renal failure occur.
After therapy, antacids (magnesium-aluminum hydroxide) have noted the decrease in the bioavailability of olmesartan medoxomil.
Combined use of warfarin and digoxin pharmacokinetics of olmesartan does not change. Not recommended for olmesartan medoxomil with lithium therapy due to increased toxicity of the latter.
Due to the possibility of hyperkalemia is not recommended olmesartan medoxomil with potassium-sparing diuretics, preparations containing potassium, or with other drugs that can lead to increased levels of serum potassium (eg heparin).
Olmesartan medoxomil When applied with pravastatin clinically significant interactions are not observed. Olmesartan medoxomil interaction with drugs that are metabolized by the enzyme cytochrome P450, are not defined.
