Caduet 5/10

Kaduet 5/10 is a drug that belongs to a group of drugs that can directly affect the heart and the vascular system.

According to the ATC code, Kaduet refers to a combination of hypolipidemic drugs, in particular, atorvastatin and amlodipine. The international name sounds like Atorvastatin and Amlodipine. Pharmacological group - inhibitors of HMG CoA reductase.

Kaduet 5/10 proved to be effective and widely used in cardiological practice. Thanks to the combined composition, the drug simultaneously has a double effect - it lowers blood pressure and reduces the level of cholesterol, which is very convenient in application. 

Indications Caduet 5/10

The drug is used in the presence of arterial hypertension, which has three or more risk factors for the development of concomitant cardiac and non-cardiac pathologies, for example, myocardial infarction, transient ischemic attack, stroke.

Indications for use of Kaduet 5/10 are the need for combined administration of such drugs as hypocholesterolemic and antihypertensive drugs.

In addition, Kaduet can be combined with other medicines, when the level of cholesterol remains high, and the doses of antihypertensive drugs do not bring the desired result.

Indications for the use of Kaduet 5/10 are due to combined pathology, when the level of cholesterol rises to a level when atherosclerotic plaques begin to form. In turn, the latter decrease the internal diameter of the blood vessel.

As a result, there is a spasm of blood vessels and an increase in intravascular resistance, which increases blood pressure. As the number and volume of atherosclerotic plaques increase, there is an increasing burden on the heart, as it must push blood through the vessels against high vascular resistance.

Release form

The tableted form of the release of the drug allows you to control the dosage and avoid the occurrence of adverse reactions if it is not taken properly.

The main active ingredients of the drug are amlodipine and atorvastatin. Each tablet contains 5 mg of amlodipine and 10 mg of atorvastatin. In addition, it should be noted the presence of auxiliary components, such as calcium carbonate, starch, colloidal anhydrous silicon dioxide, hydroxypropylcellulose, magnesium stearate and many others.

The form of the release is a tablet coated with a film membrane. The main physicochemical properties of the tablet preparation are white, oval, film-coated with the inscription "Pfizer" on the surface of one side and the drug code ("CDT" and "051") on the other.

Packaging of the drug is 3 blisters in the outer carton, each of which has 10 tablets.

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Pharmacodynamics

Combined drug preparation is characterized by double mechanisms of action, which determines the pharmacodynamics of Kaduet 5/10.

It is necessary to consider separately the two active components of the drug. Thus, the effect of amlodipine is based on its ability to act on muscle fibers by blocking slow calcium channels, being a representative of a group of calcium ion antagonists.

The amlodipin part of Kaduet oppresses the flow of calcium ions through the membrane into the middle of cells of smooth muscle fibers of blood vessels and heart.

On the other hand, atorvastatin has a inhibitory effect on HMG-CoA reductase. It is a potent selective inhibitor of this enzyme, whose main task is the conversion of 3-hydroxy-3-methylglutaryl coenzyme A into a melatonite. The latter is a precursor of sterols, among which is cholesterol.

Pharmacodynamics Kaduet 5/10 causes the absence of modifications from both amlodipine and atorvastatin. Influence of amlodipine on the level of arterial pressure is noted in the same volume as when it is used as monotherapy. In turn, atorvastatin in the composition of Cadet also affects the level of cholesterol, as when taking it separately.

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Pharmacokinetics

In connection with the fact that the medicine consists of two main components, it is necessary to consider the work of each separately. Pharmacokinetics Kaduet 5/10 is due to the action of amlodipine and atorvastatin.

After admission, Cadet Absorption of amlodipine at a therapeutic dose provides a peak concentration in the plasma in the interval of 6 to 12 hours after a single application. Bioavailability is observed in the range of 64-80%. The distribution volume is about 21 l / kg. In addition, the bioavailability of amlodipine is not affected by eating.

 In vitro studies, it was noted that in the human body, suffering from hypertension, the drug by 97.5% circulates along the bloodstream in conjunction with plasma proteins.

Approximately 90% of the dose of amlodipine taken passes the metabolism in the liver and turns into inactive metabolites. Drug withdrawal is a process consisting of 2 stages. About 10% of amlodipine and 60% of its metabolites are excreted in the urine. After a week of regular intake of the drug in plasma, its stable level is noted.

 Pharmacokinetics Kaduet 5/10, considering atorvastatin, provides the first peak concentration in just 1-2 hours after a single dose of the drug. The degree of absorption depends directly on the dose of atorvastatin. The absolute level of bioavailability is approximately 12%, and the systemic level is 30%.

Low systemic bioavailability is due to the work of the digestive tract (stomach, intestine, liver). The intake of the drug affects the intake of food, which slows it down.

However, despite this, the cholesterol reduction is made to the same extent, regardless of the food intake and the time of use of the drug.

Approximately 95% of the drug is in a bound state with plasma proteins and thus circulate through the bloodstream.

The excretion of atorvastine and metabolites is carried out mainly by bile after passing the metabolism in the liver. Only 2% of the drug is excreted in the urine.

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Dosing and administration

The medicine in the form of its tablet form of release is taken orally. At the beginning of the therapeutic course, the dose should not exceed 1 tablet per day.

The method of application and dose are set depending on the stage of hypertension, the level of cholesterol in the blood and the presence of concomitant pathology.

If this dosage does not give the expected result (subject to daily intake of Kaduet 5/10 for 7-10 days), then the dosage can be increased to 10 mg of amlodipine and 1 mg of atorvastatin.

The drug can be taken at any time of the day, regardless of the meal.

A cadouette can be used in combination with other antihypertensive drugs, but with the exception of drugs that are related to calcium channel blockers.

As for lipid-lowering drugs, it is not recommended to use Cadet in parallel with an additional dosage of statins (drugs that lower blood cholesterol levels).

You can not accept Kaduet at the same time as fibrates. In addition, one should carefully use the medicine for people with hepatic and renal pathology.

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Use Caduet 5/10 during pregnancy

In the course of pregnancy, women require strength and nutrients to form and develop the fetal organ and systems. An important component of fetal growth is cholesterol and its derivatives.

Given the mechanism of action of atorvastatin, which is the inhibition of HMG-CoA reductase, and correspondingly a decrease in the level of cholesterol, there is a danger to the fetus.

Women who take Kadueta for life need to use contraceptive methods of protection. If a woman finds out that she is pregnant, the drug should be withdrawn.

Using Kaduet 5/10 during pregnancy is prohibited, since the benefit for a future mother does not exceed the level of threat to the fetus.

In addition, there is no reliable evidence that amlodipine has the ability to penetrate breast milk, but based on evidence of atorvastatin penetration, therefore, the use of Kaduet is contraindicated during lactation.

Contraindications

It is necessary to identify the main contraindications to the use of Kaduet 5/10 in order to avoid the development of adverse reactions and deterioration of well-being.

Among the contraindications is the increased sensitivity to the group of dehydropyridine drugs, atorvastatin and amlodipine, as well as their excipients.

 In addition, avoid taking the drug with severe liver disease, an elevated level of transaminases that exceeds the upper norm by 3 or more times.

It is not recommended at the same time to take Kaduet with itraconazole, ketoconazole and telithromycin.

Contraindications to the use of Kaduet 5/10 also include a severe degree of arterial hypertension, shock of various origins, aortic obstruction, unstable hemodynamics and the presence of unstable angina after myocardial infarction.

In the course of the therapeutic course, it is necessary to monitor the level of hepatic enzymes and compare with the baseline values that were recorded before the admission of Cadet.

Care should be taken to use the drug for people who suffer from alcohol dependence, as well as in the presence of severe history of liver dysfunction in the anamnesis.

Atorvastanin is able to affect the skeletal muscles, causing pain, myositis and myopathy. Of course, throughout the therapeutic course, it is not necessary to control the level of CKK, but in people with a tendency to acute skeletal muscle necrosis and with the presence of muscle symptoms, it is nevertheless recommended to follow the dynamics of CK.

Side effects Caduet 5/10

An assessment of adverse events was performed in 1092 patients who underwent a course of treatment for hypertension and dyslipidemia compared with the placebo group.

Thus, the most frequent side effects of Kaduet 5/10 were identified. Of the neurological symptoms should be distinguished dizziness, drowsiness and headache in the occipital region. The digestive tract can react with dyspeptic disorders, nausea and pain in the abdomen. In addition, there was swelling of the joints, an increase in the level of hepatic enzymes and CK.

Of the infrequent side effects can be identified allergic reactions, reduced sugar levels, weight gain, insomnia, depression, changes in the sensitivity of the skin and tinnitus.

Rare side effects of Kaduet 5/10 include changes in the circulatory system in the form of a decrease in the level of leukocytes, platelets, vascular disorders - tachycardia, syncope, myocardial infarction and arrhythmia.

It is very rare to observe a violation of breathing, discharge from the nasal cavities of a mucous nature, coughing, vomiting, bowel dysfunction with periodic constipation and diarrhea, as well as various disorders in the organs of the digestive and urinary systems.

Overdose

Cases of drug overdose are quite rare, since the drug is very simple in dosage and, with its observance, is well tolerated by the body.

An overdose of amlodipine is threatened by excessive expansion of blood vessels, which can lead to a significant reduction in blood pressure. Thus, for some time, hypotension of varying degrees will be observed.

Such a state necessarily requires the control of a doctor and constant monitoring of the work of the heart. In order to increase the pressure, it is possible to use medicines that are capable of narrowing the vessels (vasoconstrictors).

However, it is worth carefully using them, so as not to cause a sharp increase in blood pressure. In addition, amlodipine is well amenable to dialysis, which also reduces its concentration in the blood and reduces its therapeutic effect.

An overdose of atorvastatin is rare and does not have a specific antidote. Symptomatic treatment is necessary, including not forgetting the control of the baking function, the study of its enzymes and the level of CK. Dialysis in this case will not lead to the expected result, since atorvastatin in a small amount binds to blood proteins.

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Interactions with other drugs

Simultaneous use of Cadet and certain medicines may provoke the development of many adverse reactions that adversely affect the state of human health.

Interaction Cadqueta 5/10 with other drugs such as fibrates is not recommended, especially with gemfibrozil and infusion dantrolene.

Since the drug in its composition has atorvastatin, therefore there is a risk, as with other representatives of the group of anticholinergic drugs (statins), the development of acute necrosis of muscle tissue and myopathy.

This is possible in the case when Cadouette is used in combination with drugs that are capable of increasing the concentration in the plasma of atorvastatin. Among them, immunosuppressive agents (ciclosporin), macrolide antibiotics (erythromycin, clarithromycin), azole antifungals (intraconazole, ketoconazole and nefazodone), lipid modifying doses of niacin, gemfibrozil, as well as other fibroic acid derivatives or HIV protease inhibitors are worth mentioning.

In addition, joint intake of Cadet and fusidic acid is not recommended. If its use can not be avoided, atorvastatin should be withdrawn during the course of its therapeutic course.

In addition, amlodipine should be taken with caution at the same time with baclofen, anticonvulsants - inducers CYP3A4, alpha-1 blockers, amifostine, imipramine antidepressants, beta-blockers, hormonal drugs, other antihypertensive agents and sildenafil.

With regard to atorvastatin, caution is necessary when used in conjunction with cytochrome P450 3A4 inhibitors, protease inhibitors, warfarin, fusidic acid, niacin, antacids, grapefruit juice, hormonal contraceptives, colestipol, diltiazem and phenazone.

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Storage conditions

For each drug it is expected to fulfill certain conditions for its storage. Thus, the storage conditions of Kaduet 5/10 must be performed in order that the drug does not lose its medicinal properties before the expiration date.

Storage conditions assume the maintenance of the optimum level of temperature, humidity and illumination of the room, where it is planned to find a drug for a long period of time.

The storage conditions of Kaduet 5/10 imply a temperature that does not exceed 30 degrees, as well as the absence of direct sunlight to avoid premature loss of useful properties.

In the case when certain conditions are not observed, then the drug can change its structure, which in turn makes changes in its pharmacokinetics and pharmacodynamics.

A prerequisite for storage of the drug is the lack of access to it for children, as it threatens to poison or develop more serious consequences that threaten the lives of babies.

Shelf life

When manufacturing a medicinal product, the date of manufacture and the last application of the drug must be indicated. This is indicated by the so-called expiration date.

It implies a certain period of time during which the drug retains its medicinal properties, but only if the rules of its storage are observed.

Shelf life Kaduet is 3 years. It is indicated on the outer carton for quick access, as well as on each blister, in order to know the date of the last reception if the package is lost.

After the expiration date, it is forbidden to use the medicine.

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