Cordafen tablets: instructions for use, price and reviews

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

The drug belongs to dihydropyridine and is part of the group of “slow” calcium channel blockers. Affects the process of calcium entry into smooth muscle cells of peripheral and coronary arteries; suppresses the process of release of calcium ions from depots inside cells. The drug reduces the number of functioning channels, but does not affect the time and speed of their activation and restoration. It influences the processes of contraction and excitation of myocardial muscles and vascular smooth muscles.

In therapeutic doses, it normalizes the disturbed transmembrane current of calcium ions that forms during arterial hypertension . Increases blood flow in the heart muscle, does not affect venous tone, normalizes the functioning of collaterals, improves blood supply to ischemic heart muscle, reduces myocardial tone and peripheral vascular resistance, as well as the need for oxygen in the heart muscle, afterload. Causes moderate natriuresis , improves renal blood flow, has virtually no effect on heart rate, atrioventricular and sinoauricular nodes.

Pharmacokinetics

The drug is almost completely absorbed from the gastrointestinal tract . Bioavailability is 40 - 70%. High connection with blood proteins ( albumin ). Metabolized intensively in the liver (40-60%) to pharmacologically inactive metabolites. Cmax when taking 10 mg of the drug orally is achieved after one hour. The half-life is about four hours. Penetrates through the BBB . Excreted by the kidneys and through the intestines.

Cordafen 10mg n50 tab.

Dosage form:

dragees, oral drops, capsules, solution for infusion, tablets, film-coated tablets, extended-release tablets, extended-release film-coated tablets, rapid-retard tablets, controlled-release tablets

Pharmachologic effect:

Selective BMCC, a derivative of 1,4-dihydropyridine. It has a vasodilating, antianginal and hypotensive effect. Reduces Ca2+ current in cardiomyocytes and smooth muscle cells of coronary and peripheral arteries; in high doses suppresses the release of Ca2+ from intracellular stores. Reduces the number of functioning channels without affecting the time of their activation, inactivation and recovery. It uncouples the processes of excitation and contraction in the myocardium, mediated by tropomyosin and troponin, and in vascular smooth muscles, mediated by calmodulin. In therapeutic doses, it normalizes the transmembrane Ca2+ current, which is disturbed in a number of pathological conditions, primarily in arterial hypertension. Does not affect the tone of the veins. Strengthens coronary blood flow, improves blood supply to ischemic areas of the myocardium without developing the “steal” phenomenon, and activates the functioning of collaterals. By dilating peripheral arteries, it reduces peripheral vascular resistance, myocardial tone, afterload, myocardial oxygen demand and increases the duration of LV diastolic relaxation. It has virtually no effect on the SA and AV nodes and does not have antiarrhythmic activity. Increases renal blood flow, causes moderate natriuresis. The negative chrono-, dromo- and inotropic effects are overlapped by reflex activation of the sympathoadrenal system and an increase in heart rate in response to peripheral vasodilation. Time of onset of effect: 20 minutes for oral administration, 5 minutes for sublingual administration of capsule contents; duration of effect: 4-6 hours - for tablets and capsules, 12-24 hours - for prolonged forms.

Indications:

Angina pectoris (tension, stable without vasospasm, stable vasospastic, unstable vasospastic with ineffectiveness of beta-blockers and nitrates); arterial hypertension (including renovascular), relief of hypertensive crisis; Raynaud's disease and syndrome; spasm of the coronary arteries (during diagnostic or therapeutic interventions - percutaneous transluminal coronary angioplasty, vascular recanalization or coronary artery bypass grafting); differential diagnosis between functional and organic stenosis of the coronary arteries; hypertension in the “lesser” circulation.

Contraindications:

Hypersensitivity, severe arterial hypotension (systolic blood pressure below 90 mm Hg), pregnancy, lactation. With caution. Severe stenosis of the aortic orifice or mitral valve, HOCM, severe bradycardia or tachycardia, SSSU, CHF, mild or moderate arterial hypotension, severe cerebrovascular accidents, myocardial infarction with LV failure, gastrointestinal obstruction (for sustained-release forms), liver failure, renal insufficiency (especially patients on hemodialysis - a high risk of excessive and unpredictable decrease in blood pressure), older age, children under 18 years of age (the effectiveness and safety of use have not been studied).

Side effects:

From the cardiovascular system: tachycardia, arrhythmias, peripheral edema (ankles, feet, legs), manifestations of excessive vasodilation (asymptomatic decrease in blood pressure, “flushes” of blood to the facial skin, flushing of the facial skin, feeling of heat), excessive decrease in blood pressure (rarely), fainting , development or worsening of heart failure (usually worsening of an existing one). In some patients (especially with severe obstructive lesions of the coronary arteries), at the beginning of treatment or when the dose is increased, attacks of angina pectoris may occur, including the development of myocardial infarction (requires discontinuation of the drug). From the nervous system: headache, dizziness, increased fatigue, asthenia, drowsiness. With long-term ingestion in high doses - paresthesia of the limbs, tremor, extrapyramidal (parkinsonian) disorders (ataxia, mask-like face, shuffling gait, stiffness of the arms or legs, tremor of the hands and fingers, difficulty swallowing), depression. From the digestive system: dry mouth, increased appetite, dyspepsia (nausea, diarrhea or constipation); rarely - gum hyperplasia (bleeding, pain, swelling), with long-term use - liver dysfunction (intrahepatic cholestasis, increased activity of liver transaminases). From the musculoskeletal system: rarely - arthralgia, swelling of the joints, myalgia. From the hematopoietic organs: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, asymptomatic agranulocytosis. From the urinary system: increased daily diuresis, deterioration of renal function (in patients with renal failure). Allergic reactions: rarely - itching, urticaria, exanthema, autoimmune hepatitis. Local reactions: burning at the site of intravenous administration. Other: rarely - visual impairment (including transient loss of vision against the background of Cmax in plasma), gynecomastia (in elderly patients, completely disappearing after withdrawal), galactorrhea, hyperglycemia, pulmonary edema (difficulty breathing, cough, wheezing), weight gain. Overdose. Symptoms: headache, flushing of the facial skin, prolonged pronounced decrease in blood pressure, suppression of sinus node function, bradycardia, bradyarrhythmia. Treatment: in case of severe poisoning (collapse, depression of the sinus node), gastric lavage is performed and activated charcoal is prescribed. The antidote is Ca2+ preparations: slow intravenous administration of 10% CaCl2 or calcium gluconate is indicated, followed by switching to a long-term infusion. With a pronounced decrease in blood pressure, dopamine or dobutamine is administered intravenously. For conduction disorders - atropine, isoprenaline or an artificial pacemaker. With the development of heart failure - intravenous administration of strophanthin. Catecholamines should be used only when there is a threat to life (due to their reduced effectiveness, a high dosage is required, which increases the risk of developing arrhythmia). It is recommended to monitor blood concentrations of glucose (insulin release may decrease) and electrolytes (K+, Ca2+). Hemodialysis is ineffective.

Directions for use and dosage:

Orally, sublingually, intravenously, intracoronarily. The maximum daily dose of short-acting nifedipine is 40 mg. For continuous use, it is recommended to use prolonged forms of nifedipine, the maximum single dose is 30 mg, the daily dose is 180 mg. Sublingual: for hypertensive crisis - 10 mg every 30 minutes (in a total dose of up to 40 mg) under careful monitoring of blood pressure and heart rate. After administration, it is recommended that the patient remain in the “lying” position for 30-60 minutes. Orally, during or after meals, with a small amount of water, 10 mg 2-4 times a day. If the effect is not sufficiently pronounced, it is possible to increase the dose of the drug (subject to switching to prolonged forms) to 80-120 mg/day (depending on the drug) for 7-14 days. For exertional angina, it is recommended to start therapy with 10 mg 3 times a day, with a gradual increase in dose by 10 mg after 4-5 days. For vasospastic angina, prolonged forms are prescribed at a dose of 80 mg/day. For other genesis of unstable angina - only in combination with beta-blockers, at a dose of 80 mg/day. For extended-release tablets - 30-60 mg once a day. In elderly patients or patients receiving combination (antianginal or antihypertensive) therapy, smaller doses are usually prescribed. If liver function is impaired, in patients with severe cerebrovascular accidents, the dose should be reduced. IV drip, to relieve a hypertensive crisis or an attack of angina: the infusion rate should be 0.6-1.2 mg/h; the maximum daily dose is 30 mg, treatment period is 2-3 days. To continue therapy, it is advisable to switch to long-acting oral forms. Intracoronary: for spasm of coronary vessels - 0.1-0.2 mg. In patients with severe stenosis of the main trunk of the coronary artery, therapy should begin with a dose of 0.05-0.1 mg, using extreme caution. The total dose of 1.2 mg should not be exceeded over 3 hours. The duration of action is 5-15 minutes. Intracoronary administration is carried out during invasive procedures through a coronary catheter located directly in the coronary artery. The introduction must be carried out evenly, slowly, over 90-120 s. If there is obstruction of 2 vessels, you cannot inject into the third, open vessel, because Usually a small negative inotropic effect in this case can cause serious complications.

Special instructions:

During the treatment period it is necessary to refrain from taking ethanol. Despite the absence of withdrawal syndrome in BMCC, a gradual dose reduction is recommended before stopping treatment. The simultaneous administration of 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 heart failure. It is not recommended to simultaneously administer IV therapy with beta-adrenergic blockers and intracoronary administration of nifedipine. During treatment, positive results are possible with direct Coombs test and laboratory tests for antinuclear antibodies. Regularity of treatment is important, regardless of how you feel, since the patient may not feel the symptoms of arterial hypertension. The diagnostic criteria for prescribing the drug for vasospastic angina are: classic clinical picture, accompanied by an increase in the ST segment; the occurrence of ergonovine-induced angina or coronary artery spasm; detection of coronary spasm during angiography or detection of an angiospastic component without confirmation (for example, with a different voltage threshold or with unstable angina, when ECG data indicate transient vasospasm). It should be borne in mind that angina pectoris may occur at the beginning of treatment, especially after recent abrupt withdrawal of beta-blockers (the latter are recommended to be withdrawn gradually). Caution should be used when co-administering disopyramide and flecainamide due to a possible increase in inotropic effect. If during therapy the patient requires surgical intervention under general anesthesia, it is necessary to inform the anesthesiologist about the nature of the therapy being performed. Caution should be exercised in elderly patients due to the greater likelihood of age-related renal impairment. During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction:

Reduces the concentration of quinidine in plasma. Increases the concentration of digoxin in plasma, and therefore the clinical effect and concentration of digoxin in plasma should be monitored. Inducers of microsomal liver enzymes (rifampicin, etc.) reduce the concentration of nifedipine. The severity of the decrease in blood pressure is enhanced by other antihypertensive drugs, nitrates, cimetidine (suppression of metabolism; ranitidine and famotidine do not have a significant effect on the metabolism of BMCC), inhalational anesthetics, diuretics and tricyclic antidepressants. In combination with nitrates, tachycardia increases. The hypotensive effect is reduced by sympathomimetics, NSAIDs (suppression of Pg synthesis in the kidneys and Na+ and fluid retention in the body), estrogens (fluid retention in the body). Ca2+ preparations can reduce the effect of BMCC. It can displace drugs characterized by a high degree of binding from their connection with proteins (including indirect anticoagulants - derivatives of coumarin and indanedione, anticonvulsants, NSAIDs, quinine, salicylates, sulfinpyrazone), as a result of which their concentrations in plasma may increase. Suppresses the metabolism of prazosin and other alpha-blockers, as a result of which the hypotensive effect may be enhanced. Li+ preparations can increase toxic effects (nausea, vomiting, diarrhea, ataxia, tremor, tinnitus). Procainamide, quinidine and other drugs that cause prolongation of the QT interval enhance the negative inotropic effect and may increase the risk of significant prolongation of the QT interval. The infusion solution of nifedipine uses ethanol as a solvent, which must be taken into account when combining with drugs that are incompatible with it. Intracoronary administration of nifedipine simultaneously with other drugs is unacceptable.

Contraindications

High sensitivity to the drug, aortic stenosis , unstable angina , collapse , age under 18 years, myocardial infarction , CHF , first trimester of pregnancy , cardiogenic shock , lactose intolerance, lactation, arterial hypotension .

Use with caution in patients with mitral valve stenosis , sinus node weakness, bradycardia , cerebrovascular accidents, liver/kidney diseases, hemodialysis , and over the age of 60 years.

Side effects

blood pressure , development of heart failure, arrhythmia , facial skin flushing, peripheral edema , feeling of heat, tachycardia , pain, palpitations dizziness , weakness, fatigue, headache , drowsiness , anxiety, increased appetite, gum hyperplasia , dyspepsia , dryness in the mouth, agranulocytosis , anemia , allergic reactions, arthritis , myalgia , arthralgia , increased daily diuresis , weight gain.

Cordafen

From the nervous system: headache, dizziness, increased fatigue, asthenia, drowsiness. With long-term ingestion in high doses - paresthesia of the limbs, tremor, extrapyramidal (parkinsonian) disorders (ataxia, mask-like face, shuffling gait, stiffness of the arms or legs, tremor of the hands and fingers, difficulty swallowing), depression.

From the digestive system: dry mouth, increased appetite, dyspepsia (nausea, diarrhea or constipation); rarely - gum hyperplasia (bleeding, pain, swelling), with long-term use - liver dysfunction (intrahepatic cholestasis, increased activity of liver transaminases).

From the musculoskeletal system: rarely - arthralgia, swelling of the joints, myalgia.

From the hematopoietic organs: anemia, leukopenia, thrombocytopenia, thrombocytopenic purpura, asymptomatic agranulocytosis.

From the urinary system: increased daily diuresis, deterioration of renal function (in patients with renal failure).

Allergic reactions: rarely - itching, urticaria, exanthema, autoimmune hepatitis.

Local reactions: burning at the site of intravenous administration.

Other: rarely - visual impairment (including transient loss of vision against the background of Cmax in plasma), gynecomastia (in elderly patients, completely disappearing after withdrawal), galactorrhea, hyperglycemia, pulmonary edema (difficulty breathing, cough, wheezing), weight gain. Overdose. Symptoms: headache, flushing of the facial skin, prolonged pronounced decrease in blood pressure, suppression of sinus node function, bradycardia, bradyarrhythmia.

Treatment: in case of severe poisoning (collapse, depression of the sinus node), gastric lavage is performed and activated charcoal is prescribed. The antidote is Ca2+ preparations: slow intravenous administration of 10% CaCl2 or calcium gluconate is indicated, followed by switching to a long-term infusion.

With a pronounced decrease in blood pressure, dopamine or dobutamine is administered intravenously. For conduction disorders - atropine, isoprenaline or an artificial pacemaker. With the development of heart failure - intravenous administration of strophanthin. Catecholamines should be used only when there is a threat to life (due to their reduced effectiveness, a high dosage is required, which increases the risk of developing arrhythmia). It is recommended to monitor blood concentrations of glucose (insulin release may decrease) and electrolytes (K+, Ca2+).

Hemodialysis is ineffective.

Interaction

When taking the drug together with other antihypertensive drugs, nitrates , tricyclic antidepressants and inhalational anesthetics, the severity of the decrease in blood pressure increases. Nifedipine reduces the concentration of quinidine and increases the concentration of digoxin and theophylline in the blood.

Taking the drug in combination with nitrates leads to increased tachycardia . Nifedipine inhibits the metabolism of alpha-blockers , which leads to increased hypotensive effects. Nifedipine vincristine from the body , which increases its side effects. The hypotensive effect of the drug is reduced by NSAIDs , sympathomimetics, and estrogens . Calcium supplements weaken the effect of nifedipine .

Instructions for use: medications and their generics (5)

Murzaeva Irina Yurievna

Endocrinologist, Preventive Medicine Doctor

June 5, 2015

Among the drugs used to treat thyroid dysfunction, the main group consists of hormonal drugs. Selecting them for farm. The Russian market, unfortunately, is not large. And in recent years it has also decreased.

Today I want to talk about drugs for the treatment of hypothyroidism, low thyroid function. This group of drugs consists of 3 subgroups, if they are divided conventionally like this. Thyroxine (T4) preparations replace the T4 hormone, better known as L-thyroxine, which will be discussed separately later.

Triiodothyronine (T3) preparations that replace the T3 hormone - I really want to talk about it now, and group 3 - combination drugs that include T4 and T3, sometimes also iodine (at a dose of 100-200 mcg).

If with T4 drugs on the farm. The market is still fine, the drug is available, and most importantly, in different doses. Things are getting worse with T3 drugs – they simply don’t exist. For several years, T3 drugs were not sold in our country. Some of the tablets did not undergo the procedure for re-registration of the drug in Russia with regulatory organizations, while others were completely discontinued from production.

During these years, a small percentage of patients began to experience insensitivity to T4, and, accordingly, persistent hypothyroidism, which also required additional replacement with drugs containing T3. Considering the huge prevalence of thyroid pathology, the total number of people in need of T3 turned out to be quite large.

The drug T3 is also very important for children with hypothyroidism (congenital or acquired), who are actively growing and developing, especially for the “maturation” of brain cells, for the development of memory, attention, and intelligence.

T3 can also be used in the complex treatment of diffuse non-toxic goiter and multinodular goiter with nodule size less than 2 cm, after operations on the thyroid gland, with AIT in combination with hypothyroidism, with a hypertrophic form or multinodular form.

To understand the importance of T3 in the body, below is a simplified diagram of the formation of thyroid hormones.

The diagram shows that T3 is formed in the body by transition from T4, it is more active, and directly “works” at the level of tissues and target organs, also due to the fact that the ratio of T4 and T3 in the body is 1:10, then there should be 10 times more trioidthyronine, which is taken into account during treatment.

That is why, with a full replacement dose of T4 for hypothyroidism and a “normal” TSH level, malaise persists - lethargy, weakness, poor weight loss, absent-minded attention, that is, there is not enough T3 in the body.

There are drugs that can compensate for T3 deficiency in the body.

these are preparations of liothyronine or triiodothyronine , they are not available in Russia and are not produced, but abroad they are available under the names:
Tibon 100 mcg and 20 mcg, Sanofi,
Triiodine Thyronine 50 mcg, Berlin Hemi (Germany),
Cytomel 5 mcg, 24 mcg, Uhlimann-Eyrard (Switzerland).
Cytomel 25 mcg, Merrel Dau France, Dinkel (Türkiye).
Cyronin 25 mcg, 50 mcg, Meija (USA).
Cytomel 5 mcg, Smif Kleim USA S Kleim French (Canada, Holland).
Cytomel 25 mcg, S.T. Riet Belgium SK USA, SK French (Canada, Holland).
Cytomel 50 mcg, Smith Kleim (USA).
Linomel 25 mcg, Smith Kleim (Argentina).
Neotiroimad 5 mcg, 25 mcg, (Portugal).
Ro-theranine 25 mcg, 50 mcg, Robinson (USA).
Tertoxin 25 mcg (injection solution), Glaxo (Denmark).
Tertoxin 20 mcg, Glaxo Denmark, UK, (South Africa).
Tibon-forte 20 mcg, 100 mcg, Hoechst (Germany).
Tyrotardine injection 100 mcg (dry matter), Henning Berlin (Germany).
Ti-tre 5 mcg, 20 mcg, Glaxo (Italy).
Tiromel 25 mcg, Ibrahim (Türkiye).
Tyranin 25 mcg, Abello (Spain)
Triiodothyronine 20 mcg, Nycomed (Sweden).
Triiodine Sanabo 25 mcg, Sanabo (Austria).
Triiodine 50 50 mcg, Berlin-Chemie (Germany).
Triiodine Leo 25 mcg, Leo (Spain).
Cytover T3 50 mcg, Vermodje

Triiodothyronine tablets are not used on their own (there are “narrow” indications for this); in the treatment of thyroid diseases, a combination of T4 and T3 in the ratio is usually selected; they are selected only by the attending physician.

Cordafen's analogs

Level 4 ATC code matches:
Lacipil

Azomex

Nimodipine

Felodipin

Nifedipine

Farmadipin

Amlotop

Nimotop

Tenox

Nifecard HL

Cordipin

Felodip

Normodipine

Phenigidine

Norvask

Cordaflex

Lerkamen

Corinfar

Vero-Amlodipine

Amlodipine

Preparations with similar active ingredients include: Adalat , Anifed , Vero-Nifedipine , Cordaflex , Hypernal , Zenusin , Depin-E , Calcigard , Corinfar , Nicardia , Cordipine , Nifebene , Nifehexal , Nifedicor , Nifedex , Nifedipine , Myogard , Nifecard , Nifesan , Ronian , Fenamon , Sanfidipin , Fenigidin , Ecodipin and others.