Buy Rytmonorm pills 150 mg, 50 pcs
  • Buy Rytmonorm pills 150 mg, 50 pcs

Propafenone

Abbott
1138 Items
2019-09-19
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$39.31
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Clinical Pharmacology

Antiarrhythmic. Rytmonorm blocks sodium channels and is a beta-blocker (applies to IC and Class II), reduces the maximum depolarization rate of phase 0 of the action potential and its amplitude.

Indications

Symptomatic, treatment requiring supraventricular tachycardias, incl. with WPW syndrome, or paroxysmal atrial fibrillation. Severe and life-threatening symptomatic ventricular tachycardias.

Composition

Active substance: propafenone hydrochloride 150 mg;

Excipients:microcrystalline cellulose - 25.4 mg, corn starch - 20 mg, croscarmellose sodium - 10 mg, hypromellose 2910 - 8 mg, magnesium stearate - 0.5 mg, water - 6.1 mg;

The composition of the film shell:macrogol 400 - 0.52 mg, macrogol 6000 - 4.176 mg, hypromellose 2910 - 6.264 mg, titanium dioxide - 1.04 mg.

Propafenone is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Rytmonorm Abbott USA pills
Propanorm PRO.MED.CS Praha a.s Czech pills

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Propafenone

Dosage and Administration

For introductory anesthesia, regardless of the presence or absence of sedation, adult patients (medium-sized, with a satisfactory general condition) are injected intravenously by titrating 4 ml (40 mg) every 10 seconds until clinical signs of anesthesia appear.

For most patients under the age of 55, the average dose of Diprivan is 1.5-2.5 mg / kg.

Patients older than 55 years usually require lower doses. Patients at risk of anesthesia for ASA classes 3 and 4 should be administered by titration: approximately 2 ml (20 mg) every 10 seconds.

Children older than 8 years of age Diprivan is administered slowly IV until the onset of clinical signs of the onset of anesthesia. The dose should be adjusted according to age and / or body weight.

The average dose is 2.5 mg / kg. For children under 8 years of age, the dose may be higher.

Children at risk of anesthesia 3 and 4 classes of ASA prescribe the drug in smaller doses.

To maintain anesthesia, Diprivan is administered either by continuous infusion or by repeated bolus injections.

When conducting a continuous infusion, the rate of administration of the drug is set individually. As a rule, a rate in the range of 4-12 mg / kg / h ensures the maintenance of adequate anesthesia.

With repeated bolus injections, depending on the clinical need, Diprivan is prescribed in doses of 25 mg (2.5 ml) to 50 mg (5.0 ml).

For children to maintain adequate anesthesia, the drug is administered at a rate of 9–15 mg / kg / h or through repeated bolus doses required to maintain the required depth of anesthesia.

To ensure a sedative effect during intensive care in adult patients on mechanical ventilation, it is recommended that the drug be administered by IV infusion. The infusion rate is set individually, taking into account the desired depth of sedation. As a rule, the infusion rate in the range of 0.3-4.0 mg / kg / h ensures the achievement of a satisfactory sedative effect.

To ensure a sedative effect with preservation of consciousness in adult patients during surgical and diagnostic procedures, the speed of administration and dose should be chosen individually and titrated depending on the patient's clinical response; most patients require the introduction of 0.5-1 mg / kg body weight for 1-5 minutes. Infusion rate to maintain sedation set individually. As a rule, infusion rate within 1.5-4.5 mg / kg / h is sufficient. For a rapid increase in the depth of sedation, a bolus of 10–20 mg Diprivan can be used as an adjunct to the infusion. For patients at risk of anesthesia for ASA classes 3 and 4, a reduction in dose and rate of administration may be required.

Application of undiluted solution

Diprivan can be used undiluted using plastic syringes or glass infusion bottles. In cases where Diprivan is used undiluted to maintain anesthesia, it is recommended to always use perfusors or infusomats in order to control the speed of administration.

Introduction of Diprivan after preliminary breeding

Mix 1 part of Diprivan and up to 4 parts of a 5% dextrose solution for IV infusion in PVC bags or in glass vials. The concentration of the active substance in the diluted solution should not be less than 2 mg / ml. When breeding in PVC bags, it is recommended to fill the bag completely; Preparation of the diluted solution should be carried out by removing the solution for infusion and replacing it with an equivalent volume of Diprivan. The solution is prepared under aseptic conditions immediately before use. The mixture is stable for 6 hours.

The simultaneous introduction of Diprivan and other solutions using a tee with a valve
As additives or solvents, use 5% dextrose solution for IV injection, 0.9% sodium chloride solution for IV injection or 4% dextrose solution with 0.18% sodium chloride solution for IV injection. The tee with a valve should be placed near the site of the introduction of Diprivan.

The diluted Diprivan solution can be administered using controlled infusion systems, but this does not completely avoid the risk of accidentally introducing large amounts of diluted Diprivan. Burettes, drop counters or metering pumps must always be part of the infusion line.
Infusion at the target concentration - the introduction of Diprivan using the ICC "Dipripuyzor"

It is used to induce and maintain general anesthesia in adults. Not recommended for sedation in intensive care, to ensure sedation with preservation of consciousness, as well as use in children.

The ICC systems enable the anesthesiologist to achieve the desired induction rate and depth of anesthesia and control them by setting and adjusting the target (predicted) concentration of propofol in the patient's blood. Diprivan can be entered using the ISC method only with the help of the “Diprivateur” system, which includes the corresponding software. The system will function only after recognizing an electronic tag on a ready-to-use glass syringe with Diprivan.

The DIPC system will automatically adjust the Diprivan's injection rate to the concentration that was recognized by the system. Medical personnel should be familiar with the manual for working with an infusion pump, with the introduction of Diprivan by the ICC method, with the correct use of a syringe recognition system.

Due to individual differences in the pharmacokinetics and pharmacodynamics of propofol, the target concentration should be titrated depending on the patient's clinical response in order to achieve the required anesthesia depth.

In adult patients under the age of 55, anesthesia can usually be induced at target concentrations of propofol from 4 to 8 μg / ml. The initial target concentration of propofol 4 mcg / ml is recommended for patients who have received premedication, for patients without premedication a concentration of 6 mcg / ml is recommended. The induction time at these target concentrations is 60-120 seconds. Higher values ​​will lead to faster induction of anesthesia, but may be associated with more pronounced inhibition of hemodynamics and respiratory function.

In patients older than 55 years of age and in patients at risk of anesthesia for ASA classes 3 and 4, lower initial target concentrations should be used, which can then be gradually increased by 0.5-1 μg / ml at intervals of 1 min to achieve gradual induction of anesthesia.

The magnitude of the decrease in target concentrations to maintain anesthesia will depend on the amount of additional analgesic agents administered. Targeted concentrations of propofol ranging from 3 to 6 μg / ml usually maintain a sufficient level of anesthesia.

The predicted concentration of propofol upon awakening is in the range of 1-2 μg / ml and depends on the level of analgesia during the period of maintenance of anesthesia.

Adverse reactions

Systemic reactions: As a rule, induction anesthesia proceeds smoothly, with minimal signs of arousal. During induction, depending on the dose and on the means used for sedation, hypotension and temporary apnea may occur. Hemodynamic parameters usually remain stable during the maintenance of anesthesia.

Other side effects during induction anesthesia, the period of its maintenance and recovery rarely occur.

There have been rare cases of epileptiform movements, including convulsions and opisthotonus. Pulmonary edema was observed.

During the awakening period, only a small number of patients had nausea, vomiting, and headache.After prolonged use of Diprivan, cases of discoloration of urine were sometimes observed.

In very rare cases, after the introduction of Diprivan, there are clinical signs of anaphylaxis, including bronchospasm, angioedema, erythema and hypotension. In some cases - postoperative fever. As with other anesthetics, sexual disinhibition may occur.

With the appointment of Diprivan in doses of more than 4 mg / kg / h, individual cases of the development of rhabdomyolysis were reported.

Local reactions: rarely - thrombosis and phlebitis at the injection site.

Contraindications

Hypersensitivity.

Drug interactions

Diprivan It is well combined with spinal and epidural anesthesia; with drugs used for sedation; with muscle relaxants and analgesics.

In cases where general anesthesia is used as a supplement to the applied methods of regional anesthesia, Diprivan can be used in smaller doses than usual.

With simultaneous use of Diprivan with drugs that reduce heart rate, the risk of developing severe bradycardia increases.
Pharmacological incompatibility is not marked.

Before use, Diprivan should not be mixed with any other injection or infusion solutions, except with a 5% dextrose solution in PVC bags or in glass infusion bottles, lignocaine for injection or alfentanil for injection in plastic syringes.

With the introduction of muscle relaxants atrakuria besylate and mivakuriya chloride should not use the same infusion line as for Diprivan, without first washing it.

Pregnancy and Lactation

Diprivan should not be used during pregnancy, but the drug is used during termination of pregnancy in the first trimester as a means for general anesthesia.

Propofol penetrates the placental barrier and can cause neonatal depression, so the drug should not be used in obstetric practice as an anesthetic.

When applying Diprivan to the mother during the breastfeeding period, safety for the infant was not established.

Special instructions

Diprivan should be used by personnel trained in anesthesia (or, in appropriate situations, by physicians trained in assisting patients during intensive care). Patients should be continuously monitored. Equipment for maintaining a free airway, for artificial ventilation, oxygen enrichment, as well as other resuscitation means must be constantly ready for use. Diprivan should not be administered by a specialist performing a diagnostic or surgical procedure.

Application DiprivanaAs a rule, requires the additional appointment of analgesics.
Diprivan should be used with caution in patients with epilepsy (due to the risk of seizures), in violation of the functions of the cardiovascular and respiratory systems, kidneys and liver, as well as in patients with hypovolemia or severely weakened patients.

Proper attention should be given to patients with impaired lipid metabolism, as well as other conditions requiring careful use of fat emulsions.

It is recommended that blood lipid levels be monitored in cases where Diprivan is prescribed to patients who are considered to be at particular risk of excessive fat accumulation. In the event that monitoring indicates an insufficient removal of fats from the body, the use of Diprivan should be adjusted appropriately. At the same time IV the introduction of Diprivan and other means containing lipids, their doses should be adjusted, given that 1 ml of Diprivan contains approximately 100 mg of fat.

The risk of pain along the vein during induction anesthesia can be significantly reduced with the introduction of the drug in the veins of large caliber (veins of the forearm or elbow bend) or with a joint introduction with a solution of lignocaine hydrochloride.

Diprivan does not have sufficient vagolytic action, and its use is associated with cases of bradycardia (sometimes pronounced), as well as with asystole. In cases where the vagus nerve tone prevails, or when the drug is used in combination with other drugs that may cause bradycardia, it seems appropriate to / in the administration of anticholinergic before anesthesia or during maintenance.

In some cases, during the period of maintenance of anesthesia, arising hypotension may necessitate / in the introduction of fluid or reduce the rate of Diprivan injection.

Individual cases of extravasal administration of the drug in the clinic and experimental studies in animals indicate a minimal tissue reaction. In animals, intra-arterial injection of Diprivan did not have a local effect on the tissue.
Diprivan in therapeutic doses does not suppress the synthesis of adrenal hormones.

The use of Diprivan can only be carried out by personnel who are trained in the field of anesthesia (or, if necessary, by doctors who have been trained to conduct intensive therapy); continuous monitoring is required with appropriate equipment to maintain free airway, mechanical ventilation, oxygen enrichment, and other resuscitation facilities. Diprivan is not allowed to be administered by a person performing diagnostic or surgical intervention.

An adequate patient follow-up period is required to ensure complete recovery from general anesthesia.
Part of the preparation of EDTA forms chelate complexes with metal ions, including zinc ions. The possibility of additional zinc administration with long-term use of Diprivan should be considered, especially in patients who are prone to zinc deficiency, for example, for burns, diarrhea and / or sepsis.
Diprivan does not contain preservatives and can serve as a favorable medium for the reproduction of microorganisms. When filling with a sterile syringe or infusion line with Diprivan, follow the rules of asepsis; The preparation must be taken immediately after opening the ampoule or after removing the protective seal from the bottle. Introduction should begin immediately. Aseptic conditions must be provided for both Diprivan and the equipment to be administered during the entire infusion period. Any infusion solutions added to the infusion line with Diprivan should be administered as close as possible to the location of the cannula. Diprivan can not be administered through a microbiological filter. The syringe with Diprivan is disposable and is intended for use in one patient. In accordance with the rules established for other lipid emulsions, the duration of continuous administration of Diprivan should not exceed 12 hours. Upon termination of the drug infusion or after the 12-hour period, it is necessary to replace both the Diprivan container and the infusion line.
If Diprivan is inserted manually using a ready-to-use glass syringe, the system for infusion between the syringe and the patient cannot be left open in the absence of observation by medical personnel. When using a glass syringe in a syringe pump, appropriate compatibility must be ensured.
Before using the container with Diprivan should be shaken. Any remaining contents of the container after use must be destroyed.
Use in Pediatrics
Diprivan is not recommended for use in children under 3 years of age.
Diprivan is not recommended for use in children as a sedative because there is no evidence of its safety and efficacy in this indication. Although a causal relationship with the use of Diprivan was not established, in some cases unlicensed use in children who underwent mechanical ventilation, serious adverse events were noted (including deaths); These phenomena were most often observed in children with the presence of infections of the respiratory tract, which were administered doses of Diprivan that exceed the recommended doses for adults.
Influence on ability to drive motor transport and control mechanisms
After applying Diprivan, care should be taken when driving vehicles and other activities requiring increased attention.

Overdosage

Symptoms: accidental overdose can probably cause depression of cardiac activity and respiration.

Treatment: in case of respiratory depression it is necessary to carry out IVL using oxygen. When oppressing the cardiovascular activity, the head of the patient should be lowered, and, if necessary, plasma substitutes and vasopressor agents should be used.

  • Brand name: Rytmonorm
  • Active ingredient: Propafenone
  • Dosage form: Pills
  • Manufacturer: Abbott
  • Country of Origin: USA

Studies and clinical trials of Propafenone (Click to expand)

  1. A Comparative Molecular Field Analysis of Propafenone-type Modulators of Cancer Multidrug Resistance
  2. Enantioselective HPLC analysis of propafenone and of its main metabolites using polysaccharide and protein-based chiral stationary phases
  3. Stereoselective determination of propafenone enantiomers in transgenic Chinese hamster CHL cells expressing human cytochrome P450
  4. Enantioseparation of antiarrhythmic drugs propafenone and diprafenone, their metabolites and analogs by capillary electrophoresis
  5. New Benzothiophene Compounds Related to Propafenone
  6. Studies on Propafenone-type Modulators of Multidrug-Resistance IV: Synthesis and Pharmacological Activity of 5-Hydroxy and 5-Benzyloxy Derivatives
  7. Intramolecular Distribution of Hydrophobicity Influences Pharmacological Activity of Propafenone-type MDR Modulators
  8. Apparent stereoselectivity in propafenone uptake by human and rat erythrocytes
  9. Bioavailability of an extemporaneous suspension of propafenone made from tablets
  10. Determination of propafenone hydrochloride by flow-injection analysis coupled with resonance light scattering detection
  11. Direct enantiomeric high performance liquid chromatographic separation of propafenone and its major metabolite in serum on a cellulose tris-3,5-dimethylphenyl carbamate chiral stationary phase
  12. Identification and determination of propafenone and its principal metabolites in human urine using capillary gas chromatography/mass spectrometry
  13. ChemInform Abstract: Improved Synthesis of the Enantiomers of Propafenone Using Chiral Building Blocks.
  14. ChemInform Abstract: New Benzothiophene Compounds Related to Propafenone.
  15. ChemInform Abstract: Studies on Propafenone-Type Modulators of Multidrug-Resistance. Part 4. Synthesis and Pharmacological Activity of 5-Hydroxy and 5-Benzyloxy Derivatives.
  16. ChemInform Abstract: Synthesis and Pharmacological Activity of the Stereoisomers of GP-88, a Propafenone-Type Modulator of Multidrug Resistance.
  17. ChemInform Abstract: Studies on Propafenone-Type Modulators of Multidrug Resistance. Part 8. Synthesis and Pharmacological Activity of Indanone Analogues.
  18. Enantioselective plasma protein binding of propafenone: Mechanism, drug interaction, and species difference
  19. Interaction of propafenone enantiomers with human α1-acid glycoprotein
  20. The hERG Potassium Channel and Drug Trapping: Insight from Docking Studies with Propafenone Derivatives
  21. Canine plasma concentration-cardiovascular effect relationships for bidisomide, a new antiarrhythmic drug, and disopyramide, cibenzoline, and propafenone
  22. Validated capillary electrophoresis assay for the simultaneous enantioselective determination of propafenone and its major metabolites in biological samples
  23. Capillary electrophoretic investigation of the enantioselective metabolism of propafenone by human cytochrome P-450 SUPERSOMES: Evidence for atypical kinetics by CYP2D6 and CYP3A4
  24. Plasma and saliva propafenone concentrations at steady state

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