Pharmacological properties of the drug Cardosal
Olmesartan medoxomil is a potent, selective angiotensin II receptor antagonist (type AT1), which inhibits the effects of angiotensin II mediated by AT1 receptors, regardless of the source and route of angiotensin II synthesis. Selective antagonism of AT1 receptors and angiotensin II leads to an increase in the concentrations of renin, angiotensin I and II in the blood plasma, as well as a slight decrease in the concentration of aldosterone. In hypertension (arterial hypertension), olmesartan medoxomil causes a dose-dependent, long-lasting decrease in blood pressure. There is no data regarding the development of arterial hypotension after taking the first dose of the drug, tachyphylaxis during prolonged treatment and withdrawal syndrome. Dosing olmesartan medoxomil once a day provides an effective and gentle reduction in blood pressure over 24 hours. The maximum antihypertensive effect is achieved after 8 weeks from the start of therapy, although a significant effect of lowering blood pressure is noted after 2 weeks of treatment. Olmesartan medoxomil is a prodrug. It is rapidly converted to the pharmacologically active metabolite olmesartan by esterases in the intestinal mucosa and in the blood of the portal vein during absorption in the digestive tract. Undegraded olmesartan medoxomil or the intact side chain of the medoxomil group was not detected in plasma or secretions. The average absolute bioavailability of olmesartan when used in tablet dosage form is 25.6%. The maximum concentration of olmesartan in blood plasma is on average reached approximately 2 hours after oral administration of the drug and increases almost linearly with an increase in the single oral dose taken to 80 mg. Concomitant food intake has virtually no effect on the bioavailability of olmesartan. The binding of olmesartan to plasma proteins is 99.7%, however, the potential for a clinically significant shift in protein binding when olmesartan interacts with other highly protein-bound drugs is low (this is confirmed by the fact that there is no clinically significant interaction between olmesartan and warfarin). Olmesartan is excreted in urine (approximately 40%) and bile (approximately 60%), its half-life is 10–15 hours. Cumulation of olmesartan was not observed.
How can dietary changes help prevent diabetes?
When it comes to preventing diabetes, many people think about the need to almost completely limit carbohydrates in their diet. And at first glance, this looks quite logical - after all, it is carbohydrates that increase blood sugar levels. But still there is no need to rush into this. Firstly, carbohydrates are different, and secondly, they perform many useful functions in our body. You just need to understand what carbohydrates you can afford and at what time.
Carbohydrates differ from each other in the rate of absorption, that is, in the time they enter the blood. Therefore, they can be divided into “fast”, “medium” and “long” carbohydrates. “Fast” include foods and drinks to which sugar is added, including products that contain “natural sugars” (fructose) - honey, fruit juices, concentrates. They appear in the blood literally a few minutes after their consumption, sharply increasing blood sugar levels. These carbohydrates have the highest glycemic index*. “Medium” include : bread, cereals, pasta, potatoes, beets, carrots, corn. This kind of carbohydrates is absorbed much more slowly, and accordingly, glucose in the blood will also increase more slowly. But, if they are subjected to prolonged cooking, their absorption will be significantly accelerated. “Long” carbohydrates contain a large amount of plant fiber: tomatoes, cucumbers, zucchini, eggplant, cabbage, lettuce, and, of course, greens. And they are the most difficult for the body to process, so the sugar level will rise very slowly and evenly. Long carbohydrates have the lowest glycemic index.
*The glycemic index is a relative indicator that reflects the rate at which blood sugar levels rise after digesting certain foods.
Use of the drug Cardosal
Adults. The initial daily dose of olmesartan medoxomil is 10 mg. If blood pressure does not decrease sufficiently, the dose of the drug is increased to the optimal daily dose of 20 mg. If necessary, the dose of the drug can be increased to a maximum of 40 mg/day. The drug is taken daily at the same time, regardless of meals. Elderly patients. There is usually no need for dose adjustment in elderly patients (see recommended doses for patients with impaired renal function). If it is necessary to increase the daily dose to a maximum of 40 mg/day, the increase should be carried out under close monitoring of blood pressure. mild or moderate renal impairment The maximum daily dose for these patients is 20 mg. To enhance the effect of the drug, hydrochlorothiazide is used.
Compound
One tablet of Cardosal 40 contains 40 mg of medoxomil olmesartan.
One tablet of Cardosal 20 contains 20 mg of medoxomil olmesartan.
One tablet of Cardosal 10 contains 10 mg of medoxomil olmesartan.
Additional substances: hyprolose, microcrystalline cellulose, lactose monohydrate, magnesium stearate.
Shell composition: hypromellose, talc, titanium dioxide.
Side effects of the drug Cardosal
By frequency of occurrence, side effects are distributed as follows: very often (≥1/10); often (≥1/100, but ≤1/10); sometimes (≥1/1000, but ≤1/100); rare (≥1/10,000, but ≤1/1000); very rare (≤1/10,000), including isolated reports. During clinical trials and post-marketing, the following adverse events were reported with olmesartan medoxomil:
Class of system violations | Nature of manifestations | Frequency of occurrence |
| From the cardiovascular system | Arterial hypotension | Rarely |
| Angina pectoris | Sometimes | |
| From the blood system | Thrombocytopenia | Very rarely |
| From the nervous system | Dizziness when turning head | Sometimes |
| Dizziness, headache | Very rarely | |
| From the respiratory system | Bronchitis, pharyngitis, rhinitis | Often |
| Cough | Very rarely | |
| From the digestive tract | Diarrhea, dyspepsia, gastroenteritis | Often |
| Abdominal pain, nausea, vomiting | Very rarely | |
| From the skin | Itching, rash, angioedema, allergic dermatitis, facial swelling, urticaria | Very rarely |
| From the musculoskeletal system | Arthritis, back pain, bone pain | Often |
| Muscle cramps, myalgia | Very rarely | |
| From the kidneys and urinary tract | Hematuria, urinary tract infection | Often |
| surge arrester | Very rarely | |
| General violations | Chest pain, flu-like symptoms, peripheral edema | Often |
| Asthenic syndrome (increased fatigue, drowsiness, general malaise) | Very rarely | |
| From the laboratory parameters | Increased CPK activity, hypertriglyceridemia, hyperuricemia | Often |
| Hyperkalemia | Rarely | |
| Increased serum creatinine and urea levels, increased liver enzyme activity | Very rarely |
Special instructions for the use of the drug Cardosal
Due to the lack of sufficient clinical experience, the use of olmesartan medoxomil is not recommended in patients with severe renal failure (creatinine clearance ≤20 ml/min) or in patients with impaired liver function. If the patient, before prescribing olmesartan medoxomil, received intensive diuretic therapy, followed a salt-free diet, or had diarrhea and/or vomiting, then after taking the first dose of the drug, arterial hypotension may develop as a result of a decrease in blood volume. Therefore, it is necessary to eliminate the possibility of hypovolemia before starting treatment with olmesartan medoxomil. Olmesartan medoxomil should be prescribed with caution to patients with heart failure, kidney disease, or stenosis of the renal artery of both or a single kidney, since there is a risk of developing acute hypotension, azotemia, oliguria, and acute renal failure. When treating patients with impaired renal function, it is recommended to periodically monitor the level of potassium and creatinine in the blood serum. Caution should be exercised when using olmesartan medoxomil in patients with aortic or mitral valve stenosis or obstructive hypertrophic cardiomyopathy. Patients with primary hyperaldosteronism do not respond to the use of ACE inhibitors, therefore it is not recommended to prescribe them olmesartan medoxomil. It should be remembered that an excessive decrease in blood pressure in patients with coronary artery disease or cerebral atherosclerosis can lead to the development of myocardial infarction or ischemic stroke. When using olmesartan medoxomil, dizziness or increased fatigue may occasionally occur, which must be taken into account in patients driving vehicles and/or servicing technical equipment. The drug contains lactose, so it should not be used in patients with hereditary galactose intolerance, lactase deficiency or glucose/galactose malabsorption syndrome.
Indications for use, restrictions
Cardosal is prescribed for hypertension, which is marked by a persistent increase in systolic and diastolic blood pressure. As a rule, it is prescribed for primary (essential) hypertension. This pathology has no connection with disease of the organs that regulate blood pressure. It is based on hereditary predisposition.
At risk are people who are obese, abuse alcohol, have a nicotine addiction, suffer from stress, as well as pregnant women and representatives of the black race.
Reasons for the development of headache
The medicine has a number of contraindications that should be taken into account before prescribing it. It is strictly forbidden to take it in the following conditions:
- individual intolerance to components;
- obstruction of the bile ducts;
- malabsorption or lactase deficiency;
- severe kidney damage in the period after transplantation of this organ;
- pregnancy;
- breastfeeding.
Also, you should not use the drug to treat small children and adolescents before they reach adulthood. It is possible to take the drug with extreme caution for the following pathologies:
- cardiac ischemia;
- cardiomyopathic conditions;
- disruption of the heart valves;
mild kidney failure;- narrowing of the lumen of the renal arteries;
- liver dysfunction;
- hyperkalemia;
- hyponatremia;
- diabetes;
- bronchial asthma;
- chronic heart failure;
- dehydration (for example, after diarrhea, severe vomiting);
- cerebrovascular pathologies;
- aldosteronism.
If there are restrictions, you should carefully study the patient’s health status and medical record. If the expected benefits are higher than the possible risks, the medicine may be prescribed. In this case, the attending physician must constantly monitor the patient’s condition.
Interactions of the drug Cardosal
When used with other antihypertensive drugs, the effect of olmesartan medoxomil may be enhanced. When olmesartan medoxomil is used simultaneously with NSAIDs, its antihypertensive effect may be reduced and there may be a risk of acute renal failure. After therapy with antacids (magnesium-aluminum hydroxide), a decrease in the bioavailability of olmesartan medoxomil was noted. The combined use of warfarin and digoxin does not change the pharmacokinetics of olmesartan. It is not recommended to use olmesartan medoxomil with lithium preparations due to the increased toxicity of the latter. Due to the possibility of developing hyperkalemia, it is not recommended to use olmesartan medoxomil with potassium-sparing diuretics, drugs containing potassium, or with other drugs that can lead to an increase in serum potassium levels (for example, heparin). When using olmesartan medoxomil with pravastatin, no clinically significant interactions were observed. The interactions of olmesartan medoxomil with drugs that are metabolized by the cytochrome P450 enzyme have not been determined.
