Buy Cardosal pills 40 pills 40 mg, 28 pcs
  • Buy Cardosal pills 40 pills 40 mg, 28 pcs

Cardosal® [Olmesartan Medoxomil]

Berlin-Chemie / Menarini
1819 Items
2019-09-19
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$35.00
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Clinical Pharmacology

Angiotensin II receptor antagonist (type AT1). Angiotensin II is the primary vasoactive hormone of the RAAS and plays a significant role in the pathophysiology of arterial hypertension through AT1-receptors. It is assumed that olmesartan blocks all effects of angiotensin II mediated by AT1receptors, regardless of the source and route of synthesis of angiotensin II.

In hypertension, olmesartan causes a dose-dependent, prolonged decrease in blood pressure. There is no evidence of the development of arterial hypotension after taking the first dose of the drug, of tachycardia during long-term treatment (for Cardosal® 20 and Cardosal® 40) and the development of withdrawal syndrome (a sharp increase in blood pressure after discontinuation of the drug).

Taking olmesartan medoxomil 1 time / day provides an effective and mild decrease in blood pressure for 24 hours, and the effect after a single dose is similar to the effect of taking the drug 2 times / day in the same daily dose.

The antihypertensive effect of olmesartan develops, as a rule, already after 2 weeks, and the maximum effect develops approximately 8 weeks after the start of therapy.

Pharmacokinetics

Suction and distribution

Olmesartan medoxomil is a prodrug. It quickly turns into a pharmacologically active metabolite of olmesartan under the action of enzymes in the intestinal mucosa and in the portal blood during absorption from the gastrointestinal tract. Olmesartan medoxomil unchanged in blood plasma was not detected. The bioavailability of olmesartan is on average 25.6%. Cmax Plasma olmesartan is achieved on average 2 hours after oral administration of olmesartan medoxomil and increases approximately linearly with an increase in a single dose to 80 mg.

Eating does not have a significant impact on the bioavailability of olmesartan, so olmesartan medoxomil can be taken regardless of the meal.

There were no clinically significant differences in pharmacokinetic parameters of olmesartan depending on gender.

Olmesartan binds to plasma proteins (99.7%), but the potential for a clinically significant shift in protein binding when olmesartan interacts with other high-binding and simultaneously used drugs is low (as evidenced by the absence of clinically significant interaction between olmesartan and warfarin). Communication olmesartan with blood cells is negligible.

Metabolism and excretion

Total plasma clearance is usually 1.3 l / h (coefficient of variation - 19%) and is relatively low compared with hepatic blood flow (approximately 90 l / h). Renal excretion is approximately 40%, with bile - about 60%. The intrahepatic circulation of olmesartan is minimal. Since most of olmesartan is excreted through the liver, its use in patients with obstruction of the biliary tract is contraindicated.

T1/2 olmesartan is 10-15 hours after repeated ingestion. A significant effect of therapy is achieved after taking the first few doses of the drug, and after 14 days of repeated use, no further cumulation is observed. Renal clearance is approximately 0.5-0.7 l / h and does not depend on the dose of the drug.

Pharmacokinetics in special clinical situations

In patients with impaired renal function, the AUC in the steady state was increased by approximately 62%, 82% and 179% in cases of mild, moderate and severe renal dysfunction, respectively, compared with healthy volunteers.

After a single oral administration, the AUC values ​​for olmesartan were 6% and 65% higher in patients with mild and moderate degrees of liver dysfunction, respectively, compared with healthy volunteers. The unbound fraction of olmesartan 2 h after dosing with the drug in healthy volunteers, in patients with mild and moderate degrees of liver dysfunction was 0.26%, 0.34% and 0.41%, respectively.

Indications

Essential arterial hypertension.

Composition

1 tablet contains:

Active substances: olmesartan medoxomil 4.0 mg.

Excipients: microcrystalline cellulose - 40 mg, low-substituted hyprolosis - 80 mg, lactose monohydrate - 246.4 mg, hyprolosis 6-10 MPa × s - 10 mg, magnesium stearate - 3.6 mg

The composition of the film shell: hypromellose 5 MPa × s - 8.64 mg, talc - 1.68 mg, titanium dioxide (E171) - 1.68 mg.

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Cardosal® [Olmesartan Medoxomil]

Dosage and Administration

It is recommended to take the drug Cardosal ® inside every day at the same time, regardless of the meal 1 time / day.

The recommended initial dose for adults is 10 mg (1 tab. Of Cardosal® 10) 1 time per day. In case of insufficient reduction of blood pressure while taking the drug at a dose of 10 mg / day, the dose of the drug can be increased to 20 mg / day (Cardosal® 20 can be used). If necessary, an additional reduction in blood pressure can be increased to a maximum dose of 40 mg / day (Kardosal® 40 may be used) or a diuretic (hydrochlorothiazide) may be added. The maximum daily dose is 40 mg.

Adverse reactions

Possible side effects are listed below in descending frequency of occurrence:

  • very often (> 1/10);
  • often (> 1/100 <1/10);
  • sometimes (> 1/1000, <1/100);
  • rarely (> 1/10 000, <1/1000);
  • very rarely (<1/10 000), including individual messages.

From the hemopoietic system: very rarely - thrombocytopenia.

From the side of the central nervous system: sometimes dizziness; very rarely - headache.

On the part of the respiratory system: often - pharyngitis, rhinitis; very rarely - cough, bronchitis.

From the digestive system: often - diarrhea, dyspepsia, gastroenteritis; very rarely - abdominal pain, nausea, vomiting.

On the part of the skin: very rarely - pruritus, rash, angioedema, allergic dermatitis, urticaria.

From the musculoskeletal system: often - back pain, bone pain, arthralgia, arthritis; very rarely - muscle cramps, myalgia.

From the urinary system: often - hematuria, urinary tract infection; very rarely, acute renal failure.

From the laboratory indicators: very rarely - an increase in serum creatinine and urea levels, an increase in liver enzymes.

Since the cardiovascular system: sometimes - angina, tachycardia; rarely - a pronounced decrease in blood pressure.

Metabolism: often - increased levels of CPK, hypertriglyceridemia, hyperuricemia; rarely - hyperkalemia.

On the part of the body as a whole: often - chest pain, flu-like symptoms, peripheral edema; very rarely - asthenia, fatigue, malaise, drowsiness.

The drug should be used with caution in the following conditions or diseases: stenosis of aortic or mitral valves; hypertrophic obstructive cardiomyopathy; primary aldosteronism; hyperkalemia, hyponatremia (risk of dehydration, hypotension, renal failure); renal failure (QC more than 20 ml / min); chronic heart failure; bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney; CHD; cerebrovascular diseases; old age (over 65); abnormal liver function; conditions accompanied by a decrease in the BCC (including diarrhea, vomiting), as well as subject to a sodium restricted diet; simultaneous use with diuretics.

Drug interactions

Combined use with potassium-sparing diuretics, potassium preparations, salt substitutes containing potassium, or other drugs that can increase the level of potassium in the blood serum (eg, heparin) is not recommended, this may lead to an increase in the level of potassium in the blood serum.

The antihypertensive effect of olmesartan therapy can be enhanced when combined with other antihypertensive drugs.

NSAIDs, including acetylsalicylic acid in doses of more than 3 g / day, as well as COX-2 inhibitors, and angiotensin II receptor antagonists can act synergistically, reducing glomerular filtration. With simultaneous use of NSAIDs and angiotensin II receptor antagonists, there may be a risk of developing acute renal failure, therefore, monitoring renal function at the beginning of treatment is recommended, as well as regular intake of a sufficient amount of fluid. However, simultaneous treatment can reduce the antihypertensive effect of angiotensin II receptor antagonists, leading to a partial loss of their therapeutic efficacy.

When used simultaneously with antacids (magnesium and aluminum hydroxide), a moderate decrease in the bioavailability of olmesartan is possible.

There are reports of a reversible increase in serum lithium concentration and toxicity during simultaneous use of lithium preparations with ACE inhibitors and angiotensin II receptor antagonists, therefore, the use of olmesartan medoxomil in combination with lithium preparations is not recommended. If necessary, the use of appropriate combination therapy is recommended to regularly monitor the level of lithium in the serum.

Pregnancy and Lactation

Experience with olmesartan medoxomil in pregnant women is absent. However, due to the existing reports of severe teratogenic effects of drugs acting directly on the renin-angiotensin system, like any drug of this class, olmesartan is contraindicated during pregnancy. If pregnancy occurs during treatment with Cardosal®, the drug should be withdrawn.

There is no evidence whether olmesartan is excreted in breast milk, so if you need to use the drug Cardosal® during lactation, breastfeeding for the period of taking the drug should be stopped.

Special instructions

Symptomatic arterial hypotension, especially after taking the first dose of the drug, can occur in patients with reduced BCC and / or reduced sodium levels due to intensive diuretic therapy, restriction of salt intake with food in the diet, and also due to diarrhea or vomiting. Relevant factors should be eliminated before the use of the drug Cardosal®.

In patients whose vascular tone and kidney function depend to a large extent on the activity of the RAAS (for example, in patients with severe chronic heart failure or impaired renal function, including renal artery stenosis), treatment with other drugs acting on this system is associated with the possibility of the development of acute arterial hypotension, azotemia, oliguria or, in rare cases, acute renal failure. The possibility of a similar effect cannot be excluded when using angiotensin II receptor antagonists.

There is an increased risk of developing severe arterial hypotension and renal failure if a patient with bilateral renal artery stenosis or arterial stenosis of the only functioning kidney is receiving therapy with drugs that affect the RAAS.

At use of the drug Kardosal® for patients with a renal failure it is recommended to carry out periodic control of level of potassium and creatinine in blood serum. The experience of using Cardosal® in patients with recently performed kidney transplantation or in patients with the last stage of impaired renal function (for example, CC less than 12 ml / min) is absent.

As in the case of other angiotensin II receptor antagonists and ACE inhibitors, hyperkalemia can develop with Cardosal® treatment if the patient has impaired renal function and / or chronic heart failure. In patients of this risk group, it is recommended to control the level of potassium in the blood serum.

As in the case of other angiotensin II receptor antagonists, a combination of lithium preparations and Cardosal® is not recommended.

As in the case of other angiotensin II receptor antagonists, in patients of the Negroid race suffering from hypertension, the effectiveness of therapy with Cardosal® is slightly lower than in patients of other races.

As in the case of any antihypertensive agent, an excessive decrease in blood pressure in patients with coronary artery disease or with cerebrovascular insufficiency can lead to myocardial infarction or stroke.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration of attention

The effect of Kardosal® on the ability to drive vehicles and control mechanisms has not been studied, therefore, during treatment with Kardosal®, care should be taken when driving vehicles and practicing potentially hazardous activities requiring increased concentration and psychomotor speed (dizziness and weakness are possible).

Overdosage

Symptoms: pronounced decrease in blood pressure.

Treatment: with a marked decrease in blood pressure, it is recommended to lay the patient on his back, raising his legs. Recommended gastric lavage and / or reception of activated carbon, therapy aimed at correcting dehydration and disorders of water-salt metabolism, replenishment of the BCC.

  • Brand name: Cardosal
  • Active ingredient: Olmesartan Medoxomil
  • Dosage form: pills, film coated.
  • Manufacturer: Berlin-Chemie / Menarini
  • Country of Origin: Germany

Studies and clinical trials of Olmesartan Medoxomil (Click to expand)

  1. ChemInform Abstract: Efficient Synthesis of Olmesartan Medoxomil, an Antihypertensive Drug.
  2. Identification of a degradation product in stressed tablets of olmesartan medoxomil by the complementary use of HPLC hyphenated techniques
  3. Development of a novel 96-microwell assay with high throughput for determination of olmesartan medoxomil in its tablets
  4. Modifications by Olmesartan medoxomil treatment of the platelet protein profile of moderate hypertensive patients
  5. An angiotensin II type-I receptor blocker, olmesartan medoxomil, attenuates lipid peroxidation in renal injury induced by subtotal nephrectomy
  6. Pharmacokinetics of olmesartan medoxomil in hemodialysis patients: little effect of dialysis upon its pharmacokinetics
  7. Solubilized formulation of olmesartan medoxomil for enhancing oral bioavailability
  8. Pharmacokinetics and safety of olmesartan medoxomil in combination with either amlodipine or atenolol compared to respective monotherapies in healthy subjects
  9. Clinical and Experimental Aspects of Olmesartan Medoxomil, a New Angiotensin II Receptor Antagonist
  10. An angiotensin II type 1 receptor antagonist, olmesartan medoxomil, improves experimental liver fibrosis by suppression of proliferation and collagen synthesis in activated hepatic stellate cells
  11. Antihypertensive efficacy and safety of olmesartan medoxomil compared with amlodipine for mild-to-moderate hypertension
  12. Ratio Spectra Derivative and Zero-Crossing Difference Spectrophotometric Determination of Olmesartan Medoxomil and Hydrochlorothiazide in Combined Pharmaceutical Dosage Form
  13. Development and Validation of a DiscriminatingIn VitroDissolution Method for a Poorly Soluble Drug, Olmesartan Medoxomil: Comparison Between Commercial Tablets
  14. Development of a CZE Method for the Determination of Olmesartan Medoxomil in Tablets
  15. Stability-Indicating LC Determination of a New Antihypertensive, Olmesartan Medoxomil in Tablets
  16. RP-LC and HPTLC Methods for the Determination of Olmesartan Medoxomil and Hydrochlorothiazide in Combined Tablet Dosage Forms
  17. Antihypertensive efficacy of olmesartan medoxomil or valsartan in combination with amlodipine: A review of factorial-design studies
  18. Efficacy/Safety of Olmesartan Medoxomil Versus Losartan Potassium in Naïve Versus Previously Treated Subjects With Hypertension
  19. Comparison of Olmesartan Medoxomil Versus Amlodipine Besylate on Regression of Ventricular and Vascular Hypertrophy
  20. Management of Hypertension in Patients With Diabetes Using an Amlodipine-, Olmesartan Medoxomil-, and Hydrochlorothiazide-Based Titration Regimen
  21. Effects of combination olmesartan medoxomil plus azelnidipine versus monotherapy with either agent on 24-hour ambulatory blood pressure and pulse rate in japanese patients with essential hypertension: Additional results from the REZALT study
  22. Triple therapy with olmesartan medoxomil, amlodipine besylate, and hydrochlorothiazide in adult patients with hypertension: The TRINITY multicenter, randomized, double-blind, 12-week, parallel-group study
  23. The relative bioavailability and fasting pharmacokinetics of three formulations of olmesartan medoxomil 20-mg capsules and tablets in healthy Chinese male volunteers: An open-label, randomized-sequence, single-dose, three-way crossover study
  24. Pharmacological and pharmacokinetic study of olmesartan medoxomil in animal diabetic retinopathy models

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