Pharmacodynamics and pharmacokinetics
Pharmacodynamics
The drug Quinidine belongs to class IA antiarrhythmic drugs . Inhibits the transfer of sodium ions through fast channels of the cell wall of cardiomyocytes, reduces the maximum rate of depolarization, increases the duration of the action potential and the effective refractory period of time. Reduces myocardial excitability, conductivity and automaticity in the AV node, atria, His bundle and other structures. It has a vagolytic effect, reduces the contractile activity of the heart, can cause a decrease in blood pressure, and also has an m-anticholinergic effect.
The negative inotropic effect is the result of inhibition of energy conversion in mitochondria. The antiarrhythmic effect is caused by the presence of an amide group in the structure of the molecule. The decrease in the speed of propagation of excitation is associated with an effect on the depolarization process. Suppression of conduction is manifested on the ECG by an increase in the QRS segment, inhibition of repolarization is expressed in an increase in the QT segment. In toxic dosages, the drug Quinidine enhances the automaticity function of Purkinje fibers.
By suppressing m-cholinergic receptors, it stimulates AV conduction. In therapeutic doses it has a hypotensive effect due to a decrease in the tone of peripheral arteries and veins and a negative inotropic effect. Demonstrates local irritating effect. It also has analgesic and antipyretic effects, which is associated with a depressant effect on the brain.
Pharmacokinetics
After oral administration, the highest concentration of the drug in the blood is achieved after an hour and a half. Reaction with proteins is 75-80%. Biotransformed in the liver. Some derivatives have a cardiotonic effect. The half-life is approximately 6 hours. It is evacuated mainly by the kidneys. The release of the drug increases when the urine becomes acidic and is inhibited when it is alkaline.
Quinidine is a class IA antiarrhythmic used for the treatment of supraventricular and ventricular extrasystoles, atrial tachycardia, AV tachycardia, paroxysmal fibrillation and atrial flutter. For the purpose of prevention, it is prescribed for paroxysms of supraventricular tachycardia (including WPW syndrome), paroxysms of ventricular tachycardia, prevention of ventricular fibrillation; maintaining sinus rhythm after cardioversion.
Synonyms Russian
Class IA antiarrhythmic.
English synonyms
Quinidine.
Research method
High performance liquid chromatography with tandem mass spectrometry.
Units
mcg/ml (micrograms per milliliter).
What biomaterial can be used for research?
Venous blood.
How to properly prepare for research?
- Children under 1 year of age should not eat for 30-40 minutes before the test.
- Do not eat for 2-3 hours before the test; you can drink clean still water.
- Do not smoke for 30 minutes before the test.
General information about the study
Quinidine is a class IA antiarrhythmic, the mechanism of action of which is to suppress the transport of sodium ions through fast sodium channels of the cell membrane of cardiomyocytes and reduce the maximum rate of depolarization. It also increases the duration of the action potential and the effective refractory period, reduces myocardial excitability, automaticity and conduction in the atria, AV node, His bundle and Purkinje fibers.
Quinidine was the first drug used to treat cardiac arrhythmias. Research in the early 20th century identified quinidine, a cinchona alkaloid, as the most potent antiarrhythmic. It has been used since the 1920s as an antiarrhythmic agent to maintain sinus rhythm after transition from atrial flutter or atrial fibrillation and to prevent recurrence of ventricular tachycardia or ventricular fibrillation. However, its value in preventing recurrent ventricular arrhythmias has been called into question following the publication of a meta-analysis showing that quinidine use increases mortality.
Due to extensive evidence of an increased risk of ventricular arrhythmia and sudden death, as well as a number of other side effects and drug interactions, quinidine has become unavailable in many countries in recent years. On the other hand, recent studies have shown that quinidine is the only drug that consistently demonstrates effectiveness in preventing arrhythmias caused by recurrent ventricular fibrillation in patients with Brugada syndrome, idiopathic ventricular fibrillation and early repolarization syndrome. It is also the only antiarrhythmic drug that normalizes QT in patients with congenital short QT syndrome. When used cautiously in appropriate patient populations, quinidine is a fairly safe and effective antiarrhythmic drug. The quinidine dosage regimen is determined individually.
What is the research used for?
- To determine the concentration of the drug in the blood.
- To select an individual dosage of the drug.
- To optimize treatment control through dose adjustments.
- To assess drug interactions.
- To diagnose overdose.
- To identify violations of the drug regimen.
- To prevent the toxic effect of the drug.
When is the study scheduled?
- When prescribing quinidine for the treatment of arrhythmias.
- If necessary, determine the concentration of the drug and monitor its fluctuations in the blood.
- If the effectiveness of the drug used is insufficient and the issue of dose adjustment is decided.
- When changing the dosage and dosage form of the drug.
- If a drug overdose is suspected.
What do the results mean?
Reference values: 2 - 6 µg/ml.
Therapeutic concentrations of quinidine usually range from 2 to 6 mcg/ml.
The results of the study are assessed by the attending physician, taking into account the dose of quinidine, its regimen, the patient’s age, concomitant pathology and individual tolerability of the drug.
What can influence the result?
- Serum quinidine concentrations may increase in patients with hepatic or renal failure, as well as in the elderly.
- The concentration of quinidine in the blood serum may increase when used simultaneously with potassium preparations, amiodarone, and erythromycin.
- The concentration of quinidine in the blood serum may be reduced when used simultaneously with anticonvulsants, laxatives, and verapamil.
Indications for use
The use of Quinidine is justified for the following conditions:
- atrial tachycardia , ventricular and supraventricular extrasystole, AV tachycardia, attacks of atrial flutter and fibrillation;
- to maintain sinus rhythm after cardioversion ;
- to prevent attacks of supraventricular tachycardia and ventricular tachycardia , and to prevent ventricular fibrillation .
Hydro-Quinidine (Kinidin Durules, Quinidine) tab. 150mg No. 40 – Instructions
Compound
The main functional substance is hydroquinidine hydrochloride.
Other Ingredients: Corn starch, lactose, gum arabic, talc, magnesium stearate.
Release form
The medicine is produced in tablets. Supplied in packs of 40 pieces each.
pharmachologic effect
Hydroquinidine has all the properties of quinidine to a greater extent and has a better gastrointestinal tolerability profile. Quinidine is an antiarrhythmic drug belonging to class 1A (membrane stabilizers) according to the Vaughan Williams classification. It acts at the level of sodium and potassium channels, influencing the depolarization and repolarization of myocardial cells. In addition, quinidine has anticholinergic (acts on M2 muscarinic receptors) and alpha-blocking properties.
Its effect is manifested by a decrease in cardiac automaticity both normally and in pathology, a decrease in conduction velocity at the level of the atria, the His-Purkinje system and the intraventricular system, as well as a decrease in excitability. Conduction into the atrioventricular node may be accelerated after administration of quinidine. Quinidine slows down the repolarization phase, lengthening the effective refractory period in the atrium, His-Purkinje system and ventricle. This also causes the arterial vessels to dilate.
Pharmacokinetics
Absolute bioavailability studies of hydroquinidine hydrochloride ready-release tablets showed absorption of 89%. The peak in the blood is reached within 4-5 hours. The plasma half-life is 10.8 ± 4.7 hours. Hydroquinidine hydrochloride is metabolized primarily in the liver; in fact, only 21% of the substance is unchanged in the kidneys. The therapeutic range for hydroquinidine blood levels (Kramer and Isaksson method) should be 1 to 2 mg/L.
Indications for use
- supraventricular extrasystole;
- ventricular extrasystole;
- atrial fibrillation and flutter;
— maintenance of sinus rhythm after pharmacological or electrical cardioversion of atrial tachyarrhythmias;
- prevention of paroxysmal supraventricular tachyarrhythmias and ventricular tachycardias.
Contraindications
The drug is contraindicated in the following conditions:
- known hypersensitivity to quinidine;
— violations of sinus automatism;
- complete atrioventricular block, if the patient is not protected by a “pacemaker”;
- long QT;
- blockade of branches or other disturbances of intraventricular conduction;
— digitalis intoxication;
- uncompensated heart failure;
- recent heart attack;
- history of thrombocytopenic purpura after previous use of quinidine;
- myasthenia.
Side effects
During therapy with quinidine, side effects are possible due to overdose or, in therapeutic doses, individual hypersensitivity to the product.
Signs of synconism: headache, dizziness, ringing in the ears, hearing loss, visual impairment (diplopia, photophobia).
Cardiovascular signs: increased QRS, trioventricular conduction disturbances, torsade pointe, ventricular extrasystoles, idioventricular rhythms (including tachycardia and tachycardia), cardiac arrest, syncope, arterial embolism, hypotension.
Intestinal signs: nausea, vomiting, diarrhea, abdominal pain.
Hematological signs: hemolytic anemia, thrombocytopenic purpura, agranulocytosis.
Dermatological signs: skin rash accompanied by itching, photosensitivity.
Ocular signs: optic neuritis.
Other manifestations of hypersensitivity: angioedema, asthma, cardiovascular collapse.
Drug interactions
Contraindicated combinations:
- with other antiarrhythmics that may cause pointe torsades (eg, cepridil, sotalol, amiodarone) due to an increased risk of torsades de pointes;
- with lidoflazine, prenylamine, vincamine to increase the risk of pointe shoes.
Communications related to precautions for use:
- with drugs that alkalinize the urine (eg, acetazolamide, sodium bicarbonate, trismetalol, or THAM) due to increased plasma concentrations of hydroquinidine and risk of overdose.
The use of stimulant laxatives during treatment with hydroquinidine is not recommended.
Application and dosage
The average dosage is 3-4 tablets per day. It can be increased according to the opinion of the attending physician, whose recommendations must be strictly followed.
Overdose
Symptoms of overdose observed after excessive doses (≥ 4 g of hydroquinidine) are as follows: digestive disorders, neurosensory (visual, auditory), respiratory (apnea), agitation, hypotension.
In case of poisoning, it is recommended to apply the usual measures of symptomatic treatment, such as: induction of vomiting and gastric lavage, maintenance of breathing (assisted ventilation), maintenance of cardiac function (cardiac massage, cardiac stimulation), blood pressure control (fluid infusion for hypotension), correction of changes in fluid -electrolyte balance.
special instructions
Before starting quinidine therapy, the patient's potassium and sensitivity should be checked using a test dose, followed by electrocardiographic analysis 4 hours later.
Monitoring fluid and electrolyte balance should be very careful in patients with renal impairment, in whom dosage should be adjusted based on residual renal function and plasma drug levels.
Use during pregnancy and breastfeeding
Due to the lack of clinical studies conducted during pregnancy or lactation, the medication is not recommended in these conditions.
Impact on the ability to drive vehicles and operate machinery
If, during treatment with hydroquinidine hydrochloride, manifestations of zinconism occur, characterized by dizziness, tremor, visual impairment, the patient undergoing therapy is prohibited from driving vehicles or operating machinery, inattention of which may cause accidents.
Terms of sale
As prescribed by a doctor.
Storage conditions
The medication should be stored in its original packaging at room temperature in a dark place out of reach of children.
Contraindications
- AV blockade 2-3 degrees;
- thrombocytopenic purpura after taking Quinidine;
- severe intraventricular conduction disorders;
- intoxication with glycosides with conduction disturbances;
- cardiogenic shock;
- bundle branch block;
- allergy to Quinidine or quinine;
- myasthenia gravis.
Side effects
- Reactions from the circulation: arterial thromboembolism , expansion of the QRS segment, ventricular extrasystole of the ectopic type , increase in the QT segment on the ECG, paroxysmal ventricular tachycardia, asystole, ventricular fibrillation , decreased blood pressure, sinus bradycardia.
- Digestive reactions: loss of appetite, bitter taste in the mouth, spastic pain in the epigastric region, gastralgia , vomiting, nausea, hepatitis , diarrhea .
- Reactions from the nervous system: confusion, headache, dizziness.
- Sensory reactions: hearing loss, tinnitus, visual impairment.
- Hematopoietic reactions: thrombocytopenia, hemolytic anemia.
- Allergic reactions: lupus-like syndrome, fever, urticaria, skin rash, skin hyperemia, itching.
- Other reactions: myasthenia, asthenia.
Quinidine, instructions for use (Method and dosage)
The tablets are taken orally an hour before or 2 hours after a meal with a glass of water (or milk if necessary to reduce the irritant effect on the digestive organs); Extended-release tablets should not be chewed or cracked.
Quinidine sulfate in standard cases is taken 200–300 mg up to 4 times a day. When treating attacks of supraventricular tachycardia, take 400–600 mg every 3 hours until the paroxysm stops. When treating attacks of atrial fibrillation , take 200 mg every 3 hours (and so on up to 5-8 times a day), the maintenance dose is 200-300 mg up to 4 times a day.
Long-acting tablets are taken 300–600 mg 2-3 times a day.
Publications in the media
(Quinidinum)
Synonyms. Quinidine.
Composition and release form. Tablets of 0.1 and 0.2 g of quinidine sulfate.
Indications. Atrial fibrillation, atrial flutter, paroxysmal supraventricular tachycardia, frequent atrial and ventricular extrasystole, ventricular tachycardia.
Pharmachologic effect. Quinidine blocks open “fast” sodium channels of the cell membrane, reduces its permeability and disrupts the transport of potassium, sodium and calcium ions, and also has an anticholinergic effect. The drug reduces heart rate, inhibits ectopic foci of excitation, lengthens conduction through the AV node, increases the duration of the action potential and the effective refractory period. The blocking effect of quinidine on alpha-adrenergic receptors often leads to increased effects due to activation of beta-adrenergic receptors and, as a result, to peripheral vasodilation.
Pharmacokinetics. The bioavailability of quinidine varies between patients and averages 70-80%. When taking the drug orally, peak plasma concentration is reached after 1-1.5 hours. Highly bound by plasma proteins - from 70 to 80%. Metabolized in the liver. T 1/2 is about 6 hours; excreted by the kidneys (unchanged - from 10 to 50%). Quinidine excretion increases in acidic urine and decreases with increasing urine pH.
Side effects. Arrhythmogenic effects, heart block, hypotension; visual impairment; allergic reactions; dizziness; loss of appetite, hepatitis; thrombocytopenia.
Contraindications. Hypersensitivity to the drug; bronchial asthma; complete and incomplete AV block; a history of thrombocytopenic purpura. Not recommended for use during pregnancy and breastfeeding.
Adverse reactions when interacting with other drugs. With simultaneous use of quinidine and drugs that increase urine pH (antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate), the toxicity of quinidine may increase due to an increase in its concentration in the blood, which is associated with increased reabsorption of the drug in the kidneys. Taking anticholinergics and quinidine may increase atropine-like side effects. Antagonism between quinidine and drugs for the treatment of myasthenia gravis has been noted. The combined use of quinidine and cimetidine leads to a decrease in the total clearance of quinidine and an increase in its T1/2; this is due to the inhibition of liver microsomal enzymes by cimetidine. Quinidine increases the concentration of digoxin in the blood serum. The effects of muscle relaxants may be enhanced by quinidine. Concomitant use of pimozide and quinidine may enhance the arrhythmogenic effects of the latter.
Information for the patient. Recommended doses of quinidine correspond to the severity of the disease, are individualized and are used taking into account the patient's sensitivity to the drug. To improve absorption, the drug should be taken one hour before meals or 2 hours after meals. If an irritating effect on the gastric mucosa occurs, the drug can be washed down with milk. If you missed taking the drug, take it as quickly as possible (within 2 hours after you remembered to take it); if you remember it too late, then do not take the drug at all; do not take double doses.
Overdose
Signs of overdose: depression of cardiac function, atrial flutter against the background of ventricular tachycardia , quinidine shock ( asystole and severe rhythm disturbances ), diplopia , decreased blood pressure, ringing in the ears, dizziness, hearing loss.
Treatment of overdose: gastric lavage, taking hypertensive drugs , oxygen supply, use of cardiac pacing, mechanical ventilation, administration of intravenous solutions, hemodialysis.
Quinidine sulfate - instructions, composition, dosage, side effects of use
Quinidine sulfate
Quinidine sulfate . Chinidini sulfas. Quinidini Sulfas.
The dextrorotatory isomer is [6′-methoxyquinolyl-(4)] - [5-vinylquinoclidyl-(2)]-carbinol sulfate.
Medicine release form . Powder, tablets of 0.1 and 0.2 g.
Application and dosage of the drug . Orally 30 minutes before meals, 0.2 g of quinidine sulfate once a day, if well tolerated, on the 3rd-4th day the dose is increased to 0.2 g 3-4 times a day, gradually increasing it by 0.2 g per day up to a total dose of 1.2-2 g per day. The course of treatment is up to 20 g. Sometimes the drug is prescribed in large quantities according to the following scheme: on the first day - 0.2 g 2 times; on the second - 0.4 g 2 times; on the third and fourth - 0.4 g 3 times; on the fifth and eighth days - 0.4 g 4 times a day, if well tolerated, the daily dose is adjusted to 2-4 g. To prevent relapses of atrial fibrillation, quinidine is prescribed 0.03-0.05 g 2 times a day. Quinidine sulfate is used together with digitalis preparations, bromides, camphor, vitamins (with ECG control).
IBUPROFEN-DARNITSA, Darnitsa description and instructions for use of the drug.
Action of the medicine . Quinidine sulfate inhibits the excitability of the heart muscle, reduces the excitability of the atria, slows down the speed of impulses in the sinoauricular node, reduces the strength of heart contractions and myocardial tone, increases the duration of the refractory period, inhibits the conduction of impulses along the His bundle, which leads to a slowdown in heart rate. In large doses it can cause heart block. The action of quinidine is based on its ability to inhibit oxidative processes, change the balance of sodium and potassium ions and the exchange of acetylcholine in the myocardium. Quinidine produces local anesthetic and vasodilating effects and has an anticholinergic effect. Quinidine sulfate is highly toxic.
Indications for use . Paroxysmal tachycardia and atrial fibrillation, extrasystole, ventricular extrasystole.
Contraindications . Idiosyncrasy, decompensation of cardiac activity with an increase in heart size, infective endocarditis, organic heart disease, angina pectoris (appearing at the onset of atrial fibrillation), severe stenosis of the left atrioventricular valve, heart block, hyperthyroidism, old age.
Possible side effects . Nausea, vomiting, diarrhea, cardiac depression, sometimes ventricular fibrillation, thrombosis or embolism, diplopia, tremor, tinnitus, dizziness, respiratory depression, allergic skin reactions.
Dibunol - instructions, composition, dosage, side effects of use
Treatment of complications and poisonings . Rinse the stomach with a suspension of activated carbon. Saline laxative. Forced diuresis. Alkalinization of urine. Eliminate hypokalemia. Hemodialysis and hemosorption are ineffective, since quinidine binds to proteins. Children are given artificial ventilation. Oxygen therapy. Angiotensinamide. When convulsions occur - sibazon, hexenal. Transfusion therapy. Isotonic solution of sodium chloride or sodium lactate, 250 ml. Orciprenaline sulfate, xicaine, ornid (intravenously), caffeine. Vitamins (retinol acetate, thiamine). Nicotinamide 0.003-0.05 g per day slowly intravenously or 0.05 g subcutaneously.
Interaction
When taken together with antiarrhythmic drugs, it is possible that the cardiodepressive effect may increase.
When used together, it is possible that the effect of anticholinesterase drugs ; with potassium-containing drugs, an increase in the effects of Quinidine is detected.
When used simultaneously with anticonvulsants, it is possible to reduce the content of Quinidine in the blood and reduce its effectiveness due to stimulation of its metabolism.
When taken simultaneously with laxatives, the concentration of Quinidine in the blood and its effectiveness are reduced; with medications that alkalize urine (for example, sodium bicarbonate, acetazolamide ), the likelihood of toxic reactions of quinidine increases.
When used together, the action of drugs that suppress neuromuscular transmission is stimulated.
When used together with tricyclic antidepressants, the elimination of Nortriptyline, Desipramine, Imipramine, Trimipramine , which leads to an increase in their content in the blood and the risk of toxic reactions.
When taken together with Amiloride, the effectiveness of the described drug decreases; with Amiodarone - the QT segment is prolonged due to the additive effect of the drugs and there is an increased likelihood of ventricular arrhythmias. The concentration of the active substance in the blood also increases and its undesirable effects intensify.
When used simultaneously with acetylsalicylic acid, an increase in bleeding time, the occurrence of petechiae and bleeding from the digestive organs is possible.
When taken simultaneously with Warfarin , its anticoagulant effect is enhanced; with Verapamil - the rate of elimination of Quinidine decreases and the likelihood of side effects increases.
When used together, the content of Haloperidol in the blood increases and the likelihood of adverse reactions increases.
When taken simultaneously with Hydroxyzine, arrhythmias increases ; with Dextromethorphan - its content in the blood increases due to inhibition of metabolism in the liver under the influence of Quinidine.
When used together with Digoxin, its concentration in the blood increases; with Disopyramide - it is possible that there is an increase in the level of Quinidine in the blood and an increase in the QT segment on the ECG.
When taken together with Dicoumarol, a decrease in its effectiveness has been reported; with Itraconazole , Ketoconazole – increase in the concentration of Quinidine in the blood; with Codeine – the analgesic effect of codeine is reduced; with Metoclopramide – change in the concentration of quinidine sulfate in the blood; with mefloquine - increased QT interval on the ECG.
When taken together with Nifedipine, a change in the concentrations of Quinidine and Nifedipine in the blood is possible.
When used together with Propranolol, the work of the CYP2D6 isoenzyme , which causes inhibition of the metabolism of Propranolol and a decrease in its excretion. It is also possible that the beta-blocking effect may increase and orthostatic hypotension may develop.
When used together with Rifampicin, the concentration of Quinidine in the blood decreases and, consequently, its effectiveness; with Fluvoxamine - it is possible to block the biotransformation of Quinidine and slow down its elimination.
When taken simultaneously with Erythromycin, the concentration of Quinidine in the blood increases and the QT segment on the ECG slightly lengthens.
Quinidine sulfate (Chinidinisulfas)
Home Medical Encyclopedia Medicines in alphabet X
Synonyms: Quinidine, Quinidine sulfate, Colchicine sulphate, Quinidine sulfate, Conchicine sulfate.
Pharmachologic effect. Quinidine has strong antiarrhythmic activity and is effective against various types of arrhythmias, but relatively often causes side effects. However, in some cases the drug is effective when other antiarrhythmic drugs have insufficient effect, and with proper dosage it is safe. Belongs to class IA antiarrhythmics.
Indications for use. Quinidine is prescribed for the relief of attacks and especially for the prevention of relapses (reappearance of signs) of atrial fibrillation, as well as for paroxysmal supraventricular tachycardia, frequent extrasystole and ventricular tachycardia (various heart rhythm disturbances).
Method of administration and dose. Take quinidine sulfate orally (30 minutes before meals) in tablet form. The maximum antiarrhythmic effect develops after 2-3 hours, the effect lasts 4-6 hours. Various schemes for the use of quinidine have been proposed. Previously, quinidine was prescribed, starting with small doses (0.1 g) several times a day (6 times) with a gradual increase in dose to 0.25-0.3 g, also 6 times a day.
However, studies of the pharmacokinetics (distribution in the body) of quinidine show that it is necessary to start with relatively high doses in order to achieve optimal concentrations of the drug in the blood.
For the treatment of arrhythmias in coronary heart disease: 0.4 g is prescribed for the first dose, then, if the attack is not stopped, 0.2 g every hour until the attack stops or until the total dose of quinidine is 1 g. In the absence of side effects, the first dose at the next attack can be increased to 0.6 g. For frequent attacks of ventricular arrhythmia, quinidine is prescribed at 0.4-0.6 g every 2-3 hours.
For all schemes of its use, the daily dose (for adults) should not exceed 4 g.
Side effect. In case of overdose and increased individual sensitivity, depression of cardiac activity, nausea, vomiting, diarrhea, allergic reactions; in some cases, atrial fibrillation (chaotic contractions of the atria).
Contraindications. Idiosyncrasy (hereditary hypersensitivity) to the drug, cardiac decompensation (heart failure / inability to provide the necessary blood supply to organs/), pregnancy.
Release form. Powder; tablets of 0.1 and 0.2 g.
Storage conditions. List B. In a dry place, protected from light.
| print version | This information is not a guide to self-treatment. A doctor's consultation is required. |
special instructions
It is recommended to use the described medicine with caution in case of ventricular tachyarrhythmia with prolongation of the QT segment, AV block , with chronic heart failure stage 2-3, weakness of the sinus node, bronchial asthma, arterial hypotension, thyrotoxicosis, emphysema, hypokalemia, thrombocytopenia , acute infectious diseases, prostate hyperplasia , liver failure, angle-closure glaucoma , chronic renal failure , psoriasis , pregnancy and lactation.
Persons with myocarditis or other serious myocardial diseases require constant medical supervision when using the drug. hypokalemia should be corrected .
During treatment, it is regularly necessary to monitor ECG, hemodynamic parameters and peripheral blood analysis data.
Description of the drug DIGOXIN
It is believed that aluminum and magnesium containing antacids cause a slight decrease in digoxin absorption.
When used simultaneously with aminoglycoside antibiotics (including neomycin, kanamycin, paromomycin), the concentration of digoxin in the blood plasma decreases, apparently due to a violation of its absorption from the gastrointestinal tract.
With the simultaneous use of digoxin with macrolide antibiotics (azithromycin, clarithromycin, erythromycin or roxithromycin), a significant increase in the concentration of digoxin in the blood plasma and an increased risk of developing glycoside intoxication is possible.
When used simultaneously with anticholinergic drugs, memory and attention problems may occur in elderly patients.
When used simultaneously with beta-blockers, there is a risk of developing additive bradycardia. There are reports of increased bioavailability of digoxin under the influence of talinol and carvedilol.
GCS cause an increase in the excretion of potassium and sodium from the body and water retention, which leads to an increased risk of developing glycoside intoxication when used simultaneously with digoxin.
When used simultaneously with diuretics, insulin, calcium preparations, sympathomimetics, the risk of developing glycoside intoxication increases.
When used simultaneously with thiazide and loop diuretics, there is some risk of developing glycoside intoxication.
It is believed that due to damage to the intestinal epithelium under the influence of cytotoxic agents, the absorption of digoxin from the gastrointestinal tract may be impaired.
When used simultaneously with rauwolfia alkaloids (including reserpine), there is a risk of developing severe bradycardia and heart rhythm disturbances (especially atrial fibrillation).
With simultaneous use, amiloride causes a slight increase in the concentration of digoxin in the blood plasma, which may be more pronounced in patients with impaired renal function. Under the influence of amiloride, a slight decrease in the positive inotropic effect of digoxin is possible (clinical significance has not been established).
When used simultaneously with amiodarone, the concentration of digoxin in the blood plasma significantly increases due to a decrease in its clearance and, as a result, glycoside intoxication develops.
When used simultaneously with amphotericin B, the excretion of potassium from the body increases and the risk of developing severe glycoside intoxication increases.
When used simultaneously with atorvastatin, the concentration of digoxin in the blood plasma slightly increases.
When used simultaneously with acetylsalicylic acid, diclofenac, indomethacin, ibuprofen, lornoxicam, an increase in the concentration of digoxin in the blood plasma is possible, which may be due to some impairment of renal function under the influence of NSAIDs.
When used simultaneously with verapamil, the concentration of digoxin in the blood plasma increases, the risk of developing glycoside intoxication increases, and cases of death are described.
When used simultaneously with hydroxychloroquine, the concentration of digoxin in the blood plasma increases.
When used simultaneously with diltiazem, an increase in the concentration of digoxin in the blood plasma is possible.
When used simultaneously with St. John's wort extract, the concentration of digoxin in the blood plasma decreases by 1/3-1/4.
When used simultaneously with itraconazole, the development of glycoside intoxication is possible, which is associated with an increase in the concentration of digoxin in the blood plasma, apparently due to a decrease in its clearance; It is also assumed that itraconazole inhibits the activity of P-glycoprotein, which is involved in the transport of digoxin from renal tubular cells into the urine. Itraconazole may reduce the positive inotropic effect of digoxin.
With simultaneous use of carbenoxolone, blood pressure increases, fluid retention occurs in the body, and the concentration of potassium in the serum decreases.
When taken at intervals of 1.5 hours, cholestyramine does not have a significant effect on the concentration of digoxin in the blood plasma. A decrease in the concentration of digoxin in the blood plasma is possible with long-term combined use with cholestyramine.
When used simultaneously with lithium carbonate, a slight short-term decrease in the effectiveness of lithium carbonate is possible. A case of severe bradycardia has been described.
When used simultaneously with methyldopa, cases of bradycardia in elderly patients have been described.
When used simultaneously with metoclopramide, a decrease in the concentration of digoxin in the blood plasma is possible.
It is believed that when used simultaneously with moracizine, a significant increase in the QT interval is possible, which can lead to AV block.
When used simultaneously with nefazodone, a slight increase in the concentration of digoxin in the blood plasma is possible.
When used simultaneously with nifedipine, a slight increase in the concentration of digoxin in the blood plasma is possible. The risk of adverse effects appears to be increased in patients with renal impairment or in cases of previous digoxin overdose.
It is believed that when used simultaneously with omeprazole, a slight increase in the concentration of digoxin in the blood plasma is possible.
When used simultaneously with penicillamine, the concentration of digoxin decreases.
When used simultaneously with prazosin, the concentration of digoxin in the blood plasma quickly and noticeably increases.
When used simultaneously with propafenone, the concentration of digoxin in the blood plasma and the risk of developing glycoside intoxication significantly increases.
When used simultaneously with rabeprazole, a decrease in the concentration of digoxin in the blood plasma is possible.
There are reports of a decrease in the concentration of digoxin in the blood plasma when used simultaneously with rifampicin.
When used simultaneously with salbutamol, the concentration of digoxin in the blood plasma slightly decreases.
Concomitant use of beta-agonists can cause hypokalemia, which increases the risk of developing glycoside intoxication.
When used concomitantly, spironolactone inhibits the renal excretion of digoxin and likely reduces its volume of distribution. This may cause an increase in plasma digoxin concentrations.
With the simultaneous use of suxamethonium chloride and pancuronium chloride, severe cardiac arrhythmias may develop.
When used simultaneously with sulfasalazine, a decrease in the concentration of digoxin in the blood plasma is possible.
When used simultaneously with telmisartan, it is possible to increase the concentration of telmisartan in the blood plasma.
When used simultaneously with topiramate, a slight decrease in the concentration of digoxin in the blood plasma is possible.
When used simultaneously with trimethoprim and co-trimoxazole, a slight increase in the concentration of digoxin in the blood plasma is possible, especially in elderly patients.
When used simultaneously with phenytoin, the concentration of digoxin in the blood plasma decreases. There is a report of the development of bradycardia and cardiac arrest with intravenous administration of phenytoin in a patient with cardiac arrhythmias caused by glycoside intoxication.
When used simultaneously with flecainide, a moderate increase in the concentration of digoxin in the blood plasma is possible.
When used concomitantly with fluoxetine, there is a report of increased plasma concentrations of digoxin in patients with heart failure.
When used simultaneously with cyclosporine, an increase in the concentration of digoxin in the blood plasma is possible.
When used simultaneously with cimetidine, both an increase and a decrease in the concentration of digoxin in the blood plasma is possible.
When used simultaneously with quinidine, the concentration of digoxin in the blood plasma increases by 2 times and the risk of developing glycoside intoxication increases. This is due to the fact that quinidine reduces the renal and extrarenal clearance of digoxin, displaces digoxin from sites of binding to plasma proteins, and significantly changes its volume of distribution. It is believed that changes in the rate and extent of absorption of digoxin from the intestine play a small role.
Digoxin may cause some reduction in the renal clearance of quinidine.
When used concomitantly with quinine, a significant increase in the concentration of digoxin in the blood plasma is possible, apparently due to changes in the metabolism of digoxin or its excretion in the bile.
Analogs
Level 4 ATC code matches:
Novocainamide
Novocainamide, Lidocaine, Propanorm, Verapamil, Amiodarone, Kinidin Durules, Propranolol, Ritmonorm, Bretylat, Amiocordin, Ethacizin.
