Compound
Coated tablets contain 10 mg of nifedipine each as an active substance. Excipients: polyvinyl butyral in an amount of 0.7 mg; talc (1 mg); 0.3 mg magnesium stearate ; 4 mg hydroxypropylcellulose ; lactose monohydrate (15 mg); croscarmellose sodium (13 mg); microcellulose (46 mg). The shell consists of hypromellose - 2.63 mg; titanium dioxide CI 77891 - 0.82 mg; yellow iron oxide - 0.3 mg and magnesium stearate - 0.25 mg.
Long-acting film-coated tablets contain the same active substance, but in a dose of 20 mg. Each of them contains the following substances as auxiliary substances: microcellulose (99 mg); lactose monohydrate (30 mg); croscarmellose sodium (26 mg); copolymers of methyl methacrylate and ethyl methacrylate in a ratio of 1:2 (1.9 mg); talc (2 mg); magnesium stearate (0.6 mg); hyprolose (0.5 mg). The film shell is made of hypromellose - 5.26 mg; titanium dioxide - 1.64 mg; red iron oxide - 0.6 mg; magnesium stearate - 0.5 mg.
Bulk laxatives
Many experts consider bulk laxatives to be the drugs of choice: they are the first thing prescribed to people with constipation if the symptom cannot be managed through lifestyle changes and diet.
Such effective laxatives retain water in the intestines, swell, and increase the volume of intestinal contents, stretching its walls. Excessive stretching increases peristalsis and speeds up the emptying process.
The group of drugs includes the following subtypes:
- laxatives based on plant fibers;
- osmotic preparations based on macrogol, lactulose, salts.
Such drugs do not have a systemic effect, are not absorbed and do not enter the blood. Doctors note their effectiveness. For example, Doctor of Medical Sciences, Professor G. A. Grigorieva points out that “laxatives, which increase the volume of intestinal contents and reduce its viscosity, promote the physiological functioning of the intestine (G. A. Grigorieva, 2003, p. 12).
Let's take a closer look at each of the subtypes of bulk laxatives.
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Based on polyethylene glycol (PEG), or macrogol
PEG is considered a poorly absorbed substance, which makes it capable of retaining water in the intestinal lumen. At the same time, macrogol does not lead to dehydration, it only delays the absorption of water. As a result, the stool acquires a more liquid consistency and the frequency of bowel movements increases.
Macrogol also has side effects: intestinal hypotension, which develops slowly, as well as potentiation of fecal incontinence. Therefore, it is recommended to take such drugs for no longer than 14 days.
Saline laxatives
These laxatives use concentrated salts:
- magnesium sulfate;
- sodium sulfate;
- Carlsbad salt.
Similar laxatives for constipation act at the level of the small intestine. They increase osmotic pressure, which allows fluid to be attracted and retained in the intestinal lumen. Under the influence of salts, feces become liquid and stools become frequent. This effect does not allow you to constantly take saline laxatives, since this is fraught with disturbances in salt metabolism and a decrease in a person’s quality of life.
People with kidney and cardiovascular diseases are also not recommended to use saline laxatives without consulting a doctor. Typically, these drugs are used in preparation for endoscopic examinations.
Lactulose based
Lactulose has a laxative effect indirectly, through beneficial intestinal flora. The component acts as food for bifidobacteria and lactobacilli. The latter release substances with an effect reminiscent of the effect of osmotic laxatives. In this case, profuse loose stools are not observed, since lactulose acts at the level of the large intestine.
With a single use, the laxative effect will occur within 1-2 days, but with systematic use it can appear within 2-4 hours. Lactulose is not absorbed in the intestine and does not have a systemic effect, but sometimes leads to bloating.
Based on dietary fiber
Dietary fiber (fiber) is a component of plant foods. Fiber is found in large quantities in bran, fresh vegetables and fruits, berries, and seaweed. There is also a lot of it in the shell of flax seeds and plantain (psyllium), and bran.
It is these components that are the basis of bulk laxatives. Some of the products with a similar effect contain cellulose.
Fiber swells in the intestinal lumen and increases the volume of feces. This leads to irritation of the intestinal walls due to distension. Insoluble dietary fiber gently stimulates the walls and improves peristalsis. Since dietary fiber actively absorbs water, it is important to drink enough fluids when taking fiber-based laxatives.
Such drugs can rightfully be considered mild laxatives - they do not provoke the so-called drastic effect, and their use is not accompanied by pain and cramps. However, they may not begin to work immediately and have a delayed effect.
A significant advantage of such laxatives is the possibility of long-term or even permanent use. In addition, these drugs have a minimum of contraindications, they are not addictive and act as physiologically as possible.
When choosing between bran-based preparations and psyllium-based laxatives, you should take into account that taking the former may be accompanied by increased gas formation. Therefore, in most cases, it is more advisable to use dietary supplements based on plantain seeds. One of these drugs is Fitomucil Norm.
Release form
There are two options for the release form of the drug:
- Coated tablets, weighing 10 mg. Every 100 tablets are placed in a brown glass bottle. The bottles are individually packaged in cardboard boxes.
- Film-coated tablets with prolonged action. Each tablet weighs 20 mg. Place 30 or 60 tablets in brown glass bottles. Vials must be sealed with polyethylene caps that have a first-opening control. The bottle is packed in a cardboard box.
Softening laxatives
These drugs include the following:
- glycerol;
- oils: vaseline, almond;
- liquid paraffin;
- docusate sodium.
Softening substances help soak stool with water, make its consistency softer, and facilitate the passage of stool. Such laxatives literally lubricate the intestinal mucous membranes. However, today drugs of this group are used relatively rarely, which is associated with side effects when taking them.
In the work of Doctor of Medical Sciences, Professor Minushkin O.N., there is the following information about this: “The costs of drugs that soften fecal matter (or “lubricate”) <…> reduce the absorption of fat-soluble vitamins” (Minushkin O.N., 2003, p. 52).
Pharmacodynamics and pharmacokinetics
Nifedipine is a selective blocker of slow calcium channels, one of the 1,4-dihydropyridine derivatives. Its effect is manifested in a decrease in the flow of extracellular calcium ions into cardiomyocytes and smooth muscle cells of the arteries. Nifedipine can also increase renal blood flow, causing moderate natriuresis .
After taking one tablet of Cordaflex, which has a prolonged action, the clinical effect usually develops after 20 minutes, the effect lasts from 12 to 24 hours.
After administration, it is quickly, almost completely (at least 90%) absorbed from the digestive tract. And the bioavailability of the drug is in the range of 40-70%.
The maximum concentration of the active substance in the blood is found 30-60 minutes after taking the drug.
After taking one tablet with a prolonged action, the therapeutic concentration in the blood plasma is achieved within an hour and remains at an equal level for up to 6 hours; over the next 30-36 hours, a gradual decrease in concentration is observed.
Nifedipine has the property of binding to blood plasma proteins, in particular albumins , penetrating the blood-brain barrier (in small quantities - no more than 5%), through the placenta , and can be excreted in breast milk.
The half-life is 2 hours for a 10 mg tablet; for a 20 mg extended-release tablet it is approximately 3.8-16.9 hours.
conclusions
Cordaflex is a highly effective antianginal and antihypertensive agent from the group of calcium channel blockers. Due to this, as well as its low cost, it has become widespread in the treatment of acute attacks of cardiovascular diseases.
However, it has a number of contraindications and can also cause various adverse reactions. The most common is a sharp drop in blood pressure. To avoid them, you must strictly adhere to dosages and recommendations for use.
Contraindications
Contraindications are:
- intolerance to nifedipine , other 1,4-dihydropyridine , additional components included in the tablets;
- arterial hypotension;
- unstable angina;
- the current or recent presence of acute myocardial infarction or severe aortic stenosis ;
- idiopathic subaortic stenosis;
- chronic heart failure during the period of decompensation;
- childhood.
It is prescribed with special caution to elderly patients, those with impaired renal function, and patients with diabetes mellitus .
Cordaflex rd tab p/o with counter-highlight. 40 mg 30 pcs
Arterial hypotension: Nifedipine dilates peripheral arteries, reduces blood pressure and can lead to severe arterial hypotension. The drug should be used with caution in patients with severe arterial hypotension (blood pressure below 90 mm Hg), especially in patients with coronary artery disease or cerebrovascular diseases, in whom an excessive decrease in blood pressure can lead to the development of myocardial infarction or stroke. Particular caution and careful medical supervision are also necessary in patients on hemodialysis (risk of a significant decrease in blood pressure), during pregnancy (the drug is contraindicated during pregnancy, but in exceptional cases its use is necessary). In case of severe arterial hypotension, reduce the dose or temporarily stop taking nifedipine. The risk of developing arterial hypotension is higher in patients taking beta-blockers. The simultaneous use of nifedipine and beta-blockers must be carried out under conditions of careful medical supervision, since this may cause an excessive decrease in blood pressure, and in some cases, aggravation of the symptoms of CHF. Severe hypotension and/or high fluid requirements have been reported in patients receiving nifedipine and beta-blocker therapy during coronary artery bypass graft surgery under general anesthesia with high doses of fentanyl. If during therapy the patient requires surgical intervention under general anesthesia, then it is necessary to inform the anesthesiologist about the nature of the therapy being performed. If surgery is planned under general anesthesia using high doses of fentanyl, it is recommended to stop taking Cordaflex® RD at least 36 hours before surgery. Arterial hypertension: There is no experience in the clinical use of nifedipine drugs for malignant hypertension. The drug Cordaflex® RD should not be used to lower blood pressure during a hypertensive crisis.
Chronic ischemic heart disease: The drug Cordaflex® RD should not be used for the relief of acute attacks of angina and for the secondary prevention of cardiovascular complications in patients who have had an MI.
Unstable angina and/or myocardial infarction: In rare cases, in patients with coronary artery disease (especially with severe obstructive lesions of the coronary arteries), an increase in the frequency, duration and/or severity of angina attacks was noted, as well as, in isolated cases, the development of myocardial infarction after starting the use of BMCC (including nifedipine) or after increasing their dosage. The mechanism of development of this phenomenon has not been studied. Nifedipine immediate-release tablets are contraindicated in acute MI. There is no experience in the clinical use of nifedipine preparations in the form of extended-release tablets for acute MI and unstable angina, and therefore their use in these diseases is contraindicated.
Chronic heart failure (CHF): BMCC (including nifedipine) should be used with extreme caution in patients with CHF. In case of decompensated CHF, the use of Cordaflex® RD is not recommended.
Beta-blocker withdrawal syndrome: In patients with angina, stopping beta-blockers may lead to a withdrawal syndrome (increased frequency, duration and/or severity of angina attacks), possibly due to increased sensitivity to catecholamines. Prescribing nifedipine does not prevent the development of beta-blocker withdrawal syndrome, but can even lead to its intensification due to the reflex release of catecholamines in response to peripheral vasodilation. Nifedipine does not have an antiarrhythmic effect and does not prevent the occurrence of cardiac arrhythmias when beta-blockers are abruptly discontinued. If it is necessary to discontinue therapy with a beta-blocker, its dose should be gradually reduced over 8-10 days before prescribing nifedipine.
Discontinuation of therapy: Discontinuation of nifedipine drugs should be carried out gradually (there is a risk of developing withdrawal syndrome).
Aortic stenosis / mitral stenosis / hypertrophic obstructive cardiomyopathy: As with all drugs that have a vasodilating effect, nifedipine should be used with caution in patients with aortic stenosis, mitral stenosis or hypertrophic obstructive cardiomyopathy. In patients with hemodynamically significant obstruction of the LV outflow tract (for example, with severe aortic stenosis), the use of the drug is contraindicated. Patients with obstructive cardiomyopathy are at risk of increased frequency, severity, and duration of angina attacks after taking nifedipine. In this case, discontinuation of the drug is necessary.
Peripheral edema: When using nifedipine drugs, mild or moderate peripheral edema associated with dilatation of peripheral arteries was observed. Edema is usually localized in the lower extremities and sometimes decreases with the use of diuretics. In patients with concomitant CHF, peripheral edema associated with the use of nifedipine should be carefully differentiated from symptoms of progression of LV dysfunction.
Diabetes mellitus: In patients with diabetes mellitus, when using nifedipine preparations, the body's response to insulin and glucose may change, which may require changes in the therapy of such patients.
Liver dysfunction: In rare cases, when using nifedipine preparations, an increase in the activity of certain enzymes, such as alkaline phosphatase, creatine phosphokinase, lactate dehydrogenase, aspartate aminotransferase (AST) and alanine aminotransferase (ALT), was observed, which is usually transient, but can sometimes be significant. A cause-and-effect relationship with nifedipine is uncertain in most cases, but is highly likely in some cases. These changes in laboratory parameters are rarely accompanied by clinical symptoms. However, cases of cholestasis with or without jaundice have been described, as well as rare cases of autoimmune hepatitis. Patients with impaired liver function are closely monitored and, if necessary, the dose of the drug is reduced and/or other dosage forms of nifedipine are used.
Impaired renal function: The use of nifedipine drugs in patients with impaired renal function is safe; No dose adjustment of nifedipine is required. In some cases, patients with chronic renal failure experienced a transient increase in serum urea nitrogen and creatinine concentrations. A cause-and-effect relationship with nifedipine is uncertain in most cases, but is highly likely in some cases. In patients with malignant hypertension undergoing hemodialysis, hypovolemia (decrease in circulating blood volume) after the dialysis procedure may enhance the antihypertensive effect of nifedipine and lead to a sharp decrease in blood pressure. In such patients, Cordaflex RD should be used with extreme caution; if necessary, the dose of the drug should be reduced.
Drug interactions: Nifedipine is metabolized by the CYP3A4 isoenzyme. Drugs that suppress or induce CYP3A4 may affect the first-pass effect through the liver or the clearance of nifedipine. Medicines that are weak or moderate inhibitors of the CYP3A4 isoenzyme that increase the concentration of nifedipine in the blood plasma include: macrolides (for example, erythromycin); HIV protease inhibitors (eg, ritonavir); azole antifungals (for example, ketoconazole); antidepressants (nefazodone and fluoxetine); quinupristin/dalfopristin; valproic acid; cimetidine When using nifedipine and these drugs simultaneously, it is necessary to monitor blood pressure and, if necessary, adjust the dose of nifedipine.
Surgery/general anesthesia: Inhalational anesthetics may enhance the reduction in blood pressure. If during therapy the patient requires surgery under general anesthesia, the anesthesiologist must be informed that the patient is taking nifedipine.
Diagnostic tests: During treatment, positive results are possible with direct Coombs test (with or without hemolytic anemia) and laboratory tests for antinuclear antibodies. Nifedipine, like other BMCCs, inhibits platelet aggregation in vitro. A small number of clinical studies support data on a statistically significant decrease in platelet aggregation and an increase in bleeding time. Presumably, the cause of such changes is the blockade of calcium transport across the platelet membrane. The clinical significance of this effect is unknown. Nifedipine may cause a false increase in the concentration of vanillylmandelic acid in urine when determined by the spectrophotometric method, but does not affect the measurement results when using the high-performance liquid chromatography (HPLC) method.
Alcohol: During treatment, it is not recommended to drink alcoholic beverages due to the risk of an excessive decrease in blood pressure.
Use in elderly patients: Caution should be exercised when using nifedipine drugs in elderly patients due to the high likelihood of age-related impairment of renal function. Effect on the ability to drive. In some patients, especially at the beginning of treatment, nifedipine may cause dizziness, which reduces the ability to drive vehicles and other mechanisms. In the future, the degree of restrictions depends on the individual tolerance of nifedipine. During the treatment period, especially at the beginning of treatment or when changing the dose, care must be taken when driving, engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Side effects
Cordaflex is usually well tolerated. Side effects appear rarely, more often at the beginning of treatment (then they may become weaker or disappear).
There are such side effects:
- On the heart and blood vessels: decreased blood pressure, flushing of the face and torso, swelling in the extremities , accelerated heart rate, paradoxical attack of angina , development of acute heart failure .
- On the nervous system: increased fatigue , dizziness , weakness , emotional lability , sleep disturbances, headache, tremor , paresthesia .
- On the gastrointestinal tract: the occurrence of heartburn , nausea , vomiting , flatulence , stool disorders, dryness or inflammation of the oral mucosa, intrahepatic cholestasis , as well as increased activity of certain liver enzymes.
- On the circulatory system: thrombocytopenia , leukopenia , anemia .
- On the urinary system: increased daily diuresis, night urination , decreased renal function.
Allergic reactions may occur in the form of urticaria , exanthema , and skin itching .
Stimulant laxatives
Peristalsis-stimulating laxatives for constipation are so named because they irritate intestinal receptors. They act directly on the nerve endings of the intestinal mucous membranes, and some of them (castor oil) activate the motility of the small intestine, others activate the large intestine. The latter include drugs based on senna, buckthorn, sulfur, etc. There are also drugs that acquire an active form under the influence of intestinal enzymes. They work in both the large and small intestines.
It should be remembered that stimulant drugs, if used inappropriately, can cause serious side effects. The main complications include the effect itself: diarrhea may begin, accompanied by cramping abdominal pain. Due to diarrhea, the volume of fluid in the body and the amount of salts - potassium and sodium ions - decrease. Therefore, it is under no circumstances possible to maintain this state for a long time with the help of intestinal stimulants.
Chief gastroenterologist of the Main Medical Directorate Minushkin O.N. in his work emphasizes that “irritant laxatives, which realize the effect of their action through the receptor apparatus, ultimately lead to dependence of the intestinal function on their intake, to the deposition of melanin in epithelial cells and melanosis, dystrophic changes in the mucous membrane and toxic effects on the kidneys and liver. The final effect is an “inert gut”” (Minushkin O.N., 2003, p. 52).
The inert gut we are talking about is the so-called lazy bowel phenomenon. Due to excessive stimulation, the colon loses tone and requires more and more stimulating substances. Without a laxative, it simply loses its ability to contract and move feces.
Such constipation will progress, and this is an irreversible process. Doctors do not prescribe stimulant medications for more than 2 weeks due to rapid addiction. And in most cases, it is advisable to choose a safer laxative.
Instructions for use of Cordaflex (Method and dosage)
The drug is taken orally. 10 mg film-coated tablets are swallowed whole before meals with water.
The dosage is set individually, as it very much depends on the severity of the disease, the type of disease and the body’s response to the therapy. Start with 1 tablet (10 mg) 3 times a day. There should be at least 2 hours between doses of the drug. The maximum dose per day is 40 mg.
Long-acting film-coated tablets are swallowed whole and washed down with water. In this case, the initial dose is 1 tablet 2 times a day. In any case, the daily dose is divided into 2 doses, between which a 12-hour interval must be observed.
According to the instructions for use of Cordaflex, discontinuation of the drug should be carried out gradually.
Comparison of safety of Cordaflex and Nifedipine
The safety of a drug includes many factors.
At the same time, in Cordaflex it is quite similar to Nifedipine. It is important where the drug is metabolized: drugs are excreted from the body either unchanged or in the form of products of their biochemical transformations. Metabolism occurs spontaneously, but most often involves major organs such as the liver, kidneys, lungs, skin, brain and others. When assessing the metabolism of Cordaflex, as well as Nifedipine, we look at which organ is the metabolizing organ and how critical the effect on it is.
The risk-benefit ratio is when the prescription of a drug is undesirable, but justified under certain conditions and circumstances, with the obligatory observance of caution in use. At the same time, Cordaflex does not have any risks when used, just like Nifedipine.
Also, when calculating safety, it is taken into account whether only allergic reactions occur or possible dysfunction of the main organs. In other matters, as well as the reversibility of the consequences of using Cordaflex and Nifedipine.
Overdose
An overdose of nifedipine may cause the following consequences:
- arterial hypotension;
- chest pain (similar to an angina );
- tachycardia;
- loss of consciousness;
- collapse;
- ventricular or nodal extrasystole ;
- bradycardia.
In severe cases, the development of metabolic alkalosis , cardiogenic shock with pulmonary edema, hypoxia , hyperkalemia , as well as disturbances of consciousness, which can progress to coma .
Interaction
Cordaflex should not be administered with alcohol-containing medications.
Orthostatic hypotension may develop when used with methyldopa , clonidine , as well as prazosin and octadine .
Cimetidine , ranitidine and tricyclic antidepressants will potentiate the antihypertensive effect .
When Cordaflex is combined with theophylline and digoxin , it is necessary to monitor the plasma concentrations of these drugs, as they may increase.
Phenytoin , calcium supplements and rifampicin reduce the effect of nifedipine .
Cordaflex reduces the rate of elimination of vincristine , which increases the risk of side effects. Therefore, dose adjustment is necessary.
Erythromycin , diltiazem , grapefruit juice in large quantities, azole antimicrobial drugs when taken with nifedipine significantly slow down its metabolism.
Comparison of addiction between Cordaflex and Nifedipine
Like safety, addiction also involves many factors that must be considered when evaluating a drug.
So, the totality of the values of such parameters as “o syndrome” in Cordaflex is quite similar to the similar values in Nifedipine. Withdrawal syndrome is a pathological condition that occurs after the cessation of intake of addictive or dependent substances into the body. And resistance is understood as initial immunity to a drug; in this it differs from addiction, when immunity to a drug develops over a certain period of time. The presence of resistance can only be stated if an attempt has been made to increase the dose of the drug to the maximum possible. At the same time, Cordaflex has a fairly low “syndrome” value, just like Nifedipine.
Cordaflex analogues (drugs that have a similar effect)
Level 4 ATC code matches:
Lacipil
Cordafen
Azomex
Nimodipine
Felodipin
Nifedipine
Farmadipin
Amlotop
Nimotop
Tenox
Nifecard HL
Cordipin
Felodip
Normodipine
Phenigidine
Norvask
Lerkamen
Corinfar
Vero-Amlodipine
Amlodipine
Analogs are the following drugs: Adalat , Vero-Nifedipine , Calcigard Retard , Zanifed , Cordafen , Cordaflex Retard , Cordipin , Cordipin Retard , Cordipine XL Corinfar , Nifedicap , Nifedipine and some other drugs.
Cordaflex Retard has particularly similar pharmaceutical characteristics and therapeutic applications.
Cordaflex price, where to buy
The price for 10 mg tablets is 72-95 rubles for 10 pieces, for 20 mg tablets – 63-139 rubles for 30 pieces, 74-168 rubles for 60 pieces.
- Online pharmacies in RussiaRussia
ZdravCity
- Cordaflex tab.
p.o 10 mg n100Egis 97 rub. order - Cordaflex RD tablets p.p.o. with control release 40 mg 30 pcs Arena Pharmaceuticals GmbH/Egis
RUB 217 order
- Cordaflex tablets p.p.o. prolonged action 20 mg 30 pcs. Egis
91 rub. order
- Cordaflex tablets p.p.o. prolonged action 20 mg 60 pcs. Egis
127 RUR order
