As can be seen from the instructions for use, "Diltiazem Retard" is a long-acting drug based on diltiazem hydrochloride. It is this substance that gave the name to the agent in question. We will understand what are the features of the medicine, in which diagnoses it is reasonable to use it, how to use it safely and effectively.
What it is?
The “Diltiazem Retard” accompanying instructions for use contain a description of the composition of the drug and a complete list of effects on the human body. The remedy differs from the simple “Diltiazem” in one peculiarity: capsules are intended for a longer action on the body. For this purpose, the manufacturer covered them with a special film coating. Inside contains 90 (180 or another amount) mg of active substance. Specific copolymers, magnesium stearate, mellose and lactose monohydrate are used for greater efficiency and ease of digestibility. The manufacturer used a 30 percent dispersion of polyacrylate.
Providing a lasting effect, the capsule shell is made of a silicon component that prevents the generation of foam, mellose and macrogol. Titanium dioxide and talc are used, as well as a 30% polyacrylate dispersion. It is especially important to evaluate the composition of Diltiazem Retard if the patient has allergic reactions to any substances used in the pharmaceutical industry. Only by eliminating the increased sensitivity and immunity of the body to the components used, you can prescribe the course of the drug in question.
Pharmacology: activity
"Diltiazem Retard" (90, 180 mg - the concentration of the active compound in one capsule) belongs to drugs that inhibit the conductivity of calcium channels. The substance belongs to the category of benzothiazepine processing products, has a pronounced antianginal effect. The drug has the ability to lower pathologically high blood pressure, to eliminate the manifestations of arrhythmia. Under the influence of the medicinal composition, the ability of the myocardium to contract decreases, atrioventricular conduction decreases, the heart rate becomes less frequent.
Regular use of the medication helps to reduce the amount of oxygen necessary for normal cardiac function, expand the coronary arteries and activate the blood flow in this part of the circulatory system. The active component lowers the muscle tone of arteries in the periphery, peripheral vascular resistance, and also improves the quality of the process of oxygen molecules entering the myocardial cells.
When will it help?
Instructions for use "Diltiazem Retard" (90 mg and in other dosages) is recommended as an element of the drug program, which is drawn up by a doctor to combat high blood pressure in the arteries. The tool is used to prevent and relieve angina attacks. It has established itself as a drug that improves the condition of patients with Prinzmetal angina pectoris.
The medicinal composition reliably prevents the manifestations of supraventricular arrhythmia. It can be taken with atrial form, atrial flutter, tachycardia with paroxysms, extrasystole.
Terms of use
The manufacturer of the drug "Diltiazem Retard" is presented as a means of long-term action, which imposes certain restrictions on the rules for its use and selected dosages. For a day, usually prescribed from 180 mg of the active compound to twice as much, and the volume is divided into two portions. If necessary, use drugs for a long time as an element of a supportive therapeutic course; change in the rules of administration is allowed: 180 mg can be used as food once in the morning.
An important condition for use: the drug is used as a whole food, without violating the integrity of the shell. It is forbidden to chew capsules, cut, break. The drug is washed down with reasonable volumes of pure water without additives. Non-compliance with this condition makes the prolonged-action program ineffective.
Technical points
Diltiazem Retard (90 mg and other dosage options) supplies the human body with an active compound that can affect the potential of L-type calcium channels, depending on potentials. Under the influence of the agent, the penetration of calcium ions into the polarization cardiomyocyte phase is inhibited, while the process of delivery of these elements to vascular smooth muscle cell structures changes. Slowing the depolarizing flow leads to inhibition of the action potential, the interconnection of excitatory and contractile reactions is interrupted, which affects the ability of the heart muscle to contract. The frequency of acts decreases, conductivity weakens, the vascular muscles relax, and peripheral resistance decreases.
As observations have shown (and this is recorded in the instructions), Diltiazem Retard gives a dosage-dependent effect, especially if it is necessary to adjust the state of increased pressure of mild or moderate severity. The severity of the antihypertensive effect is determined by the level of the pathological condition, at normal rates, the decrease is extremely small - it is considered completely insignificant.
The effect of lowering pressure is observed in a vertical, horizontal position. In the instructions for Diltiazem Retard, the manufacturer warns that reflex tachycardia is extremely rare. There is a risk of postural low blood pressure. There is practically no effect on the heart rate during physical exertion.
Course Features
Observations showed that Diltiazem Retard (180 mg and any other dosage option), even with prolonged use, is not associated with a risk of hypercatecholaminemia. The composition does not cause an increase in the activity of the renin system with aldosterone, angiotensin. Peripheral efficiency decreases, the effect on the kidneys from the second angiotensin.
Antianginal action is associated with a decrease in the need for myocardium in oxygen molecules. The drug shows an effect on the epicardial vascular system, creating a vasodilating effect, reduces coronary spasm. Vascular muscle relaxation is not associated with negative inotropic effects.
It is allowed to use the medication for supraventricular tachycardia. The effectiveness of the drug in patients with this condition is explained by an increase of approximately one fifth of the effectiveness of the refractory stage of the AV node in combination with a longer pulse duration.
Pay attention: complex effect
According to the instructions, "Diltiazem Retard" lowers the rate of ventricular rhythm against the background of an increased frequency of contraction of this element of the heart system. This is especially important for patients with fluttering, flickering. Sinus rhythm normalizes with certain forms of tachycardia. The condition of patients suffering from the symptomatic Wolf-Parkinson-White complex is facilitated. Long-term use leads to an insignificant increase in the period of PR, which shows regularly taken ECG.
The attenuation of the sinus node is corrected by using the described means by lengthening the activity cycle. In the presence of pronounced deformities in the ventricle on the left, the medicine does not provoke the correction of contractility or diastolic outlet pressure. The drug has an extremely weak effect on the muscles of the digestive tract. Prolonged use does not lead to adjustment of the fat profile of blood serum, does not provoke tolerance. In hypertrophic processes in the ventricle on the left, Diltiazem Retard (180 mg, 90 mg - dosage options for the active compound in the tablet) initiates regressive changes.
Studies have shown that the use of the composition in a therapeutic dosage does not correct the death rate in patients with high blood pressure. If pulmonary congestion is detected, the likelihood of complications in the heart or blood vessels increases by approximately 40%. In acute heart attack, therapy with thrombolytics with the choice of plasminogen activating substances, the risk of hemorrhagic complications increases - approximately five times, compared with the general group of patients.
Pharmacokinetics: features
In the description of Diltiazem Retard, the manufacturer mentions a good level of absorption when the drug passes through the gastrointestinal tract. The average level is estimated at 90%. Bioavailability is approximately 40%, there is a bright effect of the first passage. The maximum concentration in the circulatory system is recorded six hours after taking the dose. The volume of distribution reaches 5.3 l / kg. The half-life is about six hours with a deviation of one hour up or down.
The ability to bind to serum proteins is estimated at 80%, approximately 30% of the reactions occur in albumin. Efficiency can be observed several hours after taking the capsule, which has a lasting effect. The result is stored for 12-24 hours.
Transformation processes are localized in the liver. Studies have shown demethylation, deacetylation reactions. These proceed with the involvement of cytochrome P450. The reaction products are desmethyldyldiazem, deacetyldyldiazem. The second substance has the quality of a vasodilator, in serum it is observed in a concentration of up to 20%, it can accumulate. A single intake of the drug in question does not give such a number of metabolites that they can be determined even by the most sensitive modern methods of blood analysis.
Kinetic subtleties
As studies have shown, the active component of Diltiazem Retard tablets is concentrated primarily in substances secreted into the gallbladder. The substance is inherent in the ability to participate in the enterohepatic movement. Excretion of the main compound and its metabolites mainly occurs through the digestive tract - up to 65% of all drugs. About 3% are excreted by the renal system. Urine contains up to 4% of unchanged starting material.
It is established that the active compound "Diltiazem Retard" seeps into breast milk. A positive therapeutic course leads to an increase in bioavailability while reducing clearance. As a result, the therapeutic effect becomes more pronounced, along with this, the negative consequences of taking it are amplified.
And if for a long time, how will it end?
Like the analogues based on diltiazem, Diltiazem Retard does not have carcinogenic qualities and does not provoke mutations in the body. To confirm this fact, two-year experiments on mice and rats were organized. Bacterial laboratory tests showed similar results. The use of dosages in experiments involving experimental animals, which were 5-10 times higher than those recommended for humans per day, caused the death of fruits and embryos. Among newborns, the ability to survive decreased. Some were born with skeletal abnormalities.
When using the drug in doses that are 20 times higher than those recommended for humans, the percentage of dead-born babies increased.
Like some analogues, the instructions for Diltiazem Retard contain an indication of the possibility of its use by patients who underwent an organ transplant operation. In particular, kidney transplantation, associated with the possibility of transplant organ failure, requires the use of a composition to prevent this condition. You can use "Diltiazem Retard" as an element of immunosuppressive therapy in order to reduce the toxic effects on the kidneys of drugs containing cyclosporin A.
Is there an alternative?
Self-replacement of the drug prescribed by the doctor is undesirable and can cause a negative effect of the therapeutic course on a person. The choice of an alternative without coordination with a specialist is fraught with the danger of the absence of any effect from the treatment. If it is not possible to buy a product recommended by a professional, you should immediately check with your doctor what can be replaced with it, or make an appointment for a consultation as soon as possible to get accurate information. As a rule, patients who are prescribed this medication thoroughly study the list of analogues, instructions and reviews about Diltiazem Retard before taking it. The list of possible alternatives usually mentions tablets:
- "Altiazem PP."
- "Diacordin Retard."
- Cardil.
What do patients say?
As you can see from the reviews, the Diltiazem Retard instruction is simple and understandable for people, and the remedy itself shows a good effect with relatively mild side effects. Opinions on the effectiveness of the composition are most positive in people who used the drug under the supervision of a physician and in strict accordance with the program developed by him. But those who took Diltiazem Retard at their own discretion often faced with ineffective composition and an abundance of side effects.
In order to minimize the risks, before starting the treatment program it is reasonable to study not only the list of substitutes, the description and instructions for use of Diltiazem Retard, but also consult a doctor. The drug is indicated for rather severe pathological conditions, which means that its unjustified use or poorly selected dose can greatly harm the human body. There are no reports of such consequences from patients who used the drug under the supervision of a doctor.
When is it prescribed?
As can be seen from the reviews, "Diltiazem Retard" gives a good pronounced effect with stable angina pectoris and vasospastic form of this pathological condition. The substance is used for increased danger of coronary spasm, prescribed if surgery to install a shunt in the aorta is recommended. You can use the medicine as the only one to combat high blood pressure, you can combine it with other drugs with a similar effect. It is allowed to use tablets during the recovery period after a heart attack, if beta-blockers are contraindicated to the patient.
According to reviews, "Diltiazem Retard" gives a good effect for angina pectoris, high blood pressure, if the patient cannot be corrected with beta-blockers. It is reasonable to prescribe for nephropathy due to diabetes, since patients should not use ACE inhibitors.
It is impossible!
In the accompanying documentation for Diltiazem Retard, the manufacturer indicates the impossibility of taking the pills in question with a weak sinus node, atrioventricular blockade of the second and third degree, if the patient has not yet been given a stimulator of the heart muscle. The ban is imposed by severe bradycardia and cardiogenic shock, arrhythmia, expressed by atrial fibrillation. A categorical contraindication is a heart attack, accompanied by pulmonary congestion.
The considered tool is unacceptable to use with low blood pressure and chronic heart failure in the functioning of the second and third stages, as well as in the acute form of such a phenomenon. Restrictions on the therapeutic course are imposed by aortic stenosis, if such affects blood flow. The drug is not used for severe functional hepatic, renal failure. It is contraindicated in pregnant and lactating women. Limitations impose susceptibility, increased sensitivity of the body to all products of the processing of benzothiazepine.
Maximum accuracy
In the case of the first degree of atrioventricular blockade, "Diltiazem Retard" is prescribed if it is possible to regularly check the patient's condition. A similar approach requires problems with conduction inside the ventricles and a tendency to low blood pressure. The drug is carefully taken in the period after a heart attack, with some forms of tachycardia and insufficiency of the liver or kidneys in an unexpressed form. Special observation is required by elderly people and minor patients. So far, no studies have been conducted to prove the effectiveness of the medicinal composition and the safety of its use by this group of patients.
Undesirable consequences
As observations have shown, "Diltiazem Retard" can cause a negative effect and negative reaction of the body to a therapeutic program. , , . , , , . . , , . , , , . . .
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Too much!
Excessive use of prolonged-action capsules "Diltiazem Retard" indicates heart failure, atrioventricular block. Overdose can cause low blood pressure and hypotension. If excessive use is detected, it is necessary to rinse the patient's stomach, prescribe antacids, blood perfusion, and a plasma infusion. Antidotes include calcium gluconate injected into a vein. Recommended therapy aimed at eliminating the symptoms characteristic of the case. The patient is shown atropine or dopamine, a diuretic. Usually, an intravenous infusion of fluids is practiced. Sometimes doctors use dobutamine, isoproterenol. If an overdose has caused severe atrioventricular blockade, the cardiac system should be stimulated with electric current.
Mutual influence
The manufacturer in the instructions to "Diltiazem Retard" clarifies: the combination of the drug with beta-blockers can cause an increased inhibitory effect on the heart system. At the same time, the antianginal effect is activated. If previously left ventricular malfunctions were detected, conduction disturbances were detected, the combined therapeutic course can cause severe bradycardia.
The drug in question inhibits the processing of metoprolol, propranolol. No effects were found on the transformation of atenolol. The combination of the described drug and preparations containing amiodarone is accompanied by an increase in the negative inotropic effect. Bradycardia becomes more pronounced, conductivity worsens, and the likelihood of atrioventricular blockade increases.