Description
Pharmacological action
Long-acting local amide type anesthetic, which is a pure enantiomer. It has both anesthetic and analgesic effects. By reversibly blocking voltage-gated Na + channels, it prevents the generation of impulses at the ends of sensory nerves and the conduction of impulses along nerve fibers.
High concentrations of the drug are used for local anesthesia during surgical interventions. Getting into the systemic circulation in low concentrations, can cause a sensory block (analgesia) with a minimal and non-progressive motor block, getting in excess, has a depressing effect on the central nervous system (CNS) and myocardium (reduces its excitability, automatism and conductivity). Epinephrine has practically no effect on the duration and intensity of the blockade caused by ropivacaine.
Signs of toxicity from the central nervous system precede signs of toxicity from the cardiovascular system, as observed at lower concentrations of the drug in plasma. Ropivacaine has a wide therapeutic range (the range between doses that have a therapeutic and toxic effect).
In vivo animal studies have shown that ropivacaine has a lower toxic effect on the myocardium compared to bupivacaine. Indirect cardiovascular effects (arterial hypotension, bradycardia) can occur after epidural administration of ropivacaine and are due to the occurrence of sympathetic blockade.
The onset and duration of anesthesia with ropivacaine Kabi depends on the concentration and location of the drug.
Indications
At a concentration of 7.5 mg / 1 ml and 10 mg / 1 ml Ropivacaine Kabi is used in adults and children over 12 years of age according to the following indications:
Surgical anesthesia:
epidural block during surgical interventions, including cesarean section of large
block nerve and nerve plexus
blockade of individual nerves and infiltration anesthesia.
Intra-articular injection for arthroscopy of the knee.
At a concentration of 2 mg / 1 ml, ropivacaine Kabi is used according to the following indications:
Relief of acute pain in adults and children over 12 years of age.
prolonged epidural infusion or intermittent bolus administration, for example, to eliminate postoperative pain or labor anesthesia
blockade of individual nerves and infiltration anesthesia
prolonged blockade of peripheral nerves by infusion or bolus injection (for postoperative pain).
Relief of acute pain in children from 1 year to 12 years (inclusive):
– a single and prolonged blockade of peripheral nerves.
In infants and children under 12 years of age (inclusive)
caudal epidural block
prolonged epidural infusion.
Contraindications
hypersensitivity to the active substance, to any of the excipients or other local anesthetics of the amide type
, it is also necessary to take into account general contraindications for each specific type of anesthesia, irrespective of the
anesthetic used, ropivacaine Kabi is contraindicated for intravenous regional anesthesia of large blockade in patients with hypovolemia and paracervical anesthesia in obstetrics.
Caution
Elderly patients, patients in a weakened state, or patients with severe concomitant diseases, including blockade of intracardiac conduction of the II and III degree (sinoatrial, atrioventricular, intraventricular), progressive liver diseases, severe liver failure, severe chronic renal failure, acute porphyria, in the treatment of hypovolemia, debilitated patients, old age, childhood, pregnancy and lactation.
Regional anesthesia is preferred for these patient groups. When carrying out large blockades in order to reduce the risk of developing severe adverse events, it is recommended to stabilize the patient s condition and adjust the dose of anesthetic.
Caution should be exercised when injecting local anesthetics in the head and neck, due to the possible increased incidence of serious adverse events.
Patients on a sodium-restricted diet should consider the sodium content of the drug.
Special instructions
Anesthesia should be carried out by experienced professionals in specially equipped rooms. Mandatory availability of equipment and drugs for resuscitation. The patient must be given an intravenous catheter before conducting conduction blockades.
The specialist should be familiar with the precautions and have appropriate experience in diagnosing and treating possible side effects, systemic toxicity and other complications, such as irreversible subarachnoid administration, which can cause severe spinal blockade with apnea and hypotension.
Seizures often occur after brachial plexus blockade and epidural blockage. Most likely, this may be the result of accidental intravascular administration or rapid absorption at the injection site.
Performing peripheral nerve blockades may require the introduction of a large volume of local anesthetic into areas with a large number of vessels, often near large vessels, which increases the risk of intravascular injection and / or rapid systemic absorption, which can lead to a high plasma concentration of the drug.
Some local anesthetic procedures, such as injections in the head and neck, can be associated with an increased frequency of serious adverse reactions, regardless of the anesthetic used. Care must be taken to prevent injection into the area of inflammation.
elderly and debilitated patients, patients with blockade of intracardiac conduction of the II and III degrees, patients with severe renal failure require special attention, however, such patients are often shown local anesthesia.
There are few reports of cardiac arrest with ropivacaine for epidural anesthesia or peripheral nerve block, especially after accidental intravascular administration to elderly patients and patients suffering from concomitant heart disease.
In some cases, resuscitation may be difficult. When cardiac arrest stops, effective resuscitation measures may require a long time.
Ropivacaine is metabolized in the liver and, therefore, should be used with caution in patients with liver disease, repeated doses, possibly must be reduced due to delayed elimination.
There is usually no need to adjust the dosage in patients with renal and hepatic insufficiency with a single or short-term therapy. However, acidosis and decreased plasma protein concentrations, often seen in patients with chronic renal failure, may increase the risk of systemic intoxication.
Spinal anesthesia can lead to lower blood pressure (BP) and bradycardia. The introduction of vasoconstrictor drugs or an increase in circulating blood volume can reduce the risk of developing such side effects. Arterial hypotension should be corrected in a timely manner by introducing 5-10 mg of ephedrine, if necessary, the introduction can be repeated.
Patients taking class III antiarrhythmic drugs (e.g., amiodarone), should be under constant medical supervision and ECG monitoring, as side effects from the cardiovascular system may occur. Long-term use of ropivacaine should be avoided by patients concurrently taking strong inhibitors of the CYP1A2 isoenzyme, such as fluvoxamine and enoxacin.
Possible cross-hypersensitivity with other amide type anesthetics should be taken into account – the type of local anesthetic should be taken into account.
Patients on a sodium-restricted diet should consider the sodium content of the drug.
The use of the drug in concentrations above 5 mg / ml, as well as the intrathecal use of the drug Ropivacaine Kabi in children has not been studied.
Kabi ropivacaine injection may have porphyrinogenic properties and can only be used in patients with acute porphyria if there is no safer alternative. In case of hypersensitivity of patients, the necessary precautions should be taken.
Indication of special precautions, if necessary, when disposing of unused medicines
Unused solution must be disposed of in accordance with the applicable requirements for the disposal of medicines accepted in this hospital.
Impact on the ability to drive transp. Wed and fur .:
It is necessary to refrain from potentially hazardous activities that require increased attention and speed of psychomotor reactions, as motor functions are temporarily impaired, coordination of movements and reaction rate.
Dosage and administration of
For perineural administration (spinal and conduction anesthesia)
IV catheters must be inserted before large blockages are performed.
Ropivacaine Kabi is administered slowly or by increasing sequentially administered doses of the drug at a rate of 25-50 mg / min.
To prevent the entry of anesthetic into the vessel, it is imperative to conduct an aspiration test before and during the administration of the drug. Accidental intravascular administration is recognized by a temporary increase in heart rate.
The following table provides a guideline for selecting a dosage for intrathecal blockade, relief of acute pain, and peripheral nerve blockade. A minimum dosage sufficient to form an effective blockade should be used. When deciding on a dose choice, the experience of a clinical specialist and knowledge of the patient ² ¢s physical condition are important.
Dosing recommendations for ropivacaine Kabi for adults and children over 12 years of age (see table 2)
Table 2
Indications
Drug concentration, mg / ml Solution volume, ml Dose, mg Onset of action, min Duration of action, h
Intrathecal block surgical interventions
5 3 ² 5 15 ² 25 1 ² 5 2 ² 6
Dosing recommendations for Ropivacaine Kabi for children from 1 year to 12 years of age (see table 3)
Table 3
Indications
Concentration of the preparation, mg / ml Solution volume, mg / kg Dose, mg
Relief of acute pain (intraoperative and postoperative) blockade of peripheral nerves, for example, the iliac inguinal nerve
5 0.5 ² 0 , 6 2.5 ² 3
The doses indicated in the table are considered sufficient to achieve reliable blockade and are indicative of the use of the drug in adults, as there is an individual variability in the rate of development of the block and its duration.
For anesthesia with caesarean section, the intrathecal route of administration of ropivacaine hydrochloride has not been studied.
There are individual differences in the onset of the blockade and its duration.
The values ² ¹ ² ¹in the Dose column reflect the estimated average range of dosages needed. For information on factors affecting the method of blockade, and the individual characteristics of patients should refer to standard benefits.
Due to the lack of a sufficient number of clinical observations, it is not recommended to use ropivacaine Kabi in children under the age of 1 year.
Side effects
Adverse reactions to ropivacaine Kabi are similar to reactions to other local amide type anesthetics. Adverse reactions must be distinguished from the physiological effects of the blockade itself, for example, hypotension and bradycardia during subdural anesthesia, or effects associated with the technique of administration of the drug (for example, spinal hematoma, local nerve damage, headache after subdural puncture, meningitis and epidural abscess).
Side effects of local anesthetics
From the central and peripheral nervous system
Possible neuropathy and impaired spinal cord function (anterior spinal artery syndrome, arachnoiditis, cauda equina syndrome) are usually associated with regional anesthesia technique, and not with the effect of the drug.
As a result of accidental intrathecal administration of a dose exceeding the recommended total spinal block may occur. Serious complications are possible with systemic overdose and inadvertent intravascular administration of the drug (see section Overdose).
Acute systemic toxicity
Ropivacaine Kabi can cause acute systemic toxic reactions when using high doses or when its concentration in the blood rises rapidly if the drug is accidentally administered intravascularly or overdosed (see Pharmacological Properties and Overdose).
The most common side effects of
Various side effects of the drug have been reported, the vast majority of which were associated not with the effects of the anesthetic used, but with regional anesthesia techniques.
Most often (> 1%), the following side effects were noted, which were regarded as of clinical importance, regardless of whether a causal relationship was established using an anesthetic: decreased blood pressure *, nausea, bradycardia, vomiting, paresthesia, fever, headache, urinary retention, dizziness, chills, increased blood pressure, tachycardia, hyposthesia, anxiety.
The frequency of occurrence of undesirable effects is presented as follows: very often -> 1/10 often -> 1/100 to <1/10 infrequently -> 1/1000 to <1/100 rarely -> 1/10 000 to <1/1 000 is very rare - <1/10 000 is unknown - cannot be established based on available data. Disorders of the nervous system: often – headache, paresthesia, dizziness infrequently – anxiety, symptoms of toxic effects on the central nervous system (seizures very often -> 1/10 often -> 1/100 to <1/10 infrequently -> 1/1000 to <1/100 rarely -> 1/10 000 to <1/1 000 very rarely - <1/10 000 unknown - cannot be established based on available data. Disorders of the nervous system: often – headache, paresthesia, dizziness infrequently – anxiety, symptoms of toxic effects on the central nervous system (seizures very often -> 1/10 often -> 1/100 to <1/10 infrequently -> 1/1000 to <1/100 rarely -> 1/10 000 to <1/1 000 very rarely - <1/10 000 unknown - cannot be established based on available data. Disorders of the nervous system: often – headache, paresthesia, dizziness infrequently – anxiety, symptoms of toxic effects on the central nervous system (seizuresand, large convulsive seizures, paresthesia in the near-mouth zone, numbness of the tongue, hyperacusis, tinnitus, visual impairment, dysarthria, muscle twitching, tremors) *, hypesthesia. Disturbances from the heart: very often – decreased blood pressure (hypotension) often – bradycardia, tachycardia, increased blood pressure infrequently – fainting rarely – cardiac arrest, arrhythmias. Disorders of the respiratory system, chest and mediastinal organs: infrequently – shortness of breath, shortness of breath. Gastrointestinal disturbances: very often – nausea often – vomiting. Disorders of the kidneys and urinary tract: often – urinary retention. General disorders and disorders together with the introduction: often – back pain, hyperthermia, chills infrequently – hypothermia rarely – allergic reactions (anaphylactic reactions. angioedema and urticaria). * These symptoms are usually associated with accidental intravascular administration, overdose, or rapid absorption. a – Hypotension in children is common (> 1/100).
b – Vomiting in children is very common (> 1/10).
Drug Interactions
This medicine should not be mixed with other medicines.
Concomitant use of ropivacaine Kabi with local anesthetics, drugs structurally similar to local amide type anesthetics or drugs that inhibit the central nervous system (CNS) can enhance the toxic effects of drugs.
Patients taking class III antiarrhythmic drugs (eg, amiodarone) should be under constant medical supervision and ECG monitoring, as side effects from the cardiovascular system may occur.
In alkaline solutions of ropivacaine, hydrochloride may precipitate because it is slightly soluble at pH> 6.0).
In vivo with the simultaneous use of fluvoxamine, a potent selective inhibitor of the CYP1A2 isoenzyme, the plasma clearance of ropivacaine hydrochloride was reduced by 77%. Thus, potent inhibitors of the CYP1A2 isoenzyme, such as fluvoxamine and enoxacin, when combined with ropivacaine Kabi, they can interact with ropivacaine hydrochloride. Long-term administration of ropivacaine hydrochloride should be avoided in patients receiving treatment with potent inhibitors of the CYP1A2 isoenzyme.
In vivo with the simultaneous use of ketoconazole, a potent selective inhibitor of the CYP3A4 isoenzyme, the plasma clearance of ropivacaine hydrochloride was reduced by 15%. However, inhibition of this isoenzyme is unlikely to be clinically significant.
In vitro ropivacaine hydrochloride is a competitive inhibitor of the CYP2D6 isoenzyme, while inhibition of this isoenzyme is not achieved with plasma concentrations of the drug used in practice.
Overdose of
Acute systemic toxicity of
In the event of accidental intravascular administration during cases of nerve plexus blockade or other peripheral blockade, seizures have been reported.
In case of improper administration of an epidural dose of anesthetic intrathecally, a complete spinal block may occur.
Accidental intravascular anesthetic administration can cause an immediate toxic reaction.
In case of an overdose during regional anesthesia, symptoms of a systemic toxic reaction appear in a delayed order 15-60 minutes after injection due to a slow increase in the concentration of local anesthetic in the blood plasma.
Systemic toxicity is primarily manifested by symptoms of the central nervous system (CNS) and the cardiovascular system (CVS). These reactions are caused by high concentrations of local anesthetic in the blood, which can occur as a result of (accidental) intravascular injection, overdose or extremely high adsorption from highly vascularized areas.
CNS reactions are similar for all local amide type anesthetics, while reactions from the cardiovascular system are more dependent on the drug administered and its dose.
Central nervous system
Manifestations of systemic toxicity from the central nervous system develop gradually: first there are visual disturbances, numbness around the mouth, numbness of the tongue, hyperacusis, ringing in the ears, dizziness. Dysarthria, tremors and muscle twitches are more serious manifestations of systemic toxicity and may precede the appearance of generalized seizures (these signs should not be mistaken for the patient s neurotic behavior). With the progression of intoxication, loss of consciousness, seizures lasting from several seconds to several minutes, accompanied by respiratory failure, the rapid development of hypoxia and hypercapnia due to increased muscle activity and inadequate ventilation, can be observed. In severe cases, respiratory arrest may even occur. Emerging acidosis, hyperkalemia, hypocalcemia enhance the toxic effects of anesthetic.
Subsequently, due to the redistribution of the anesthetic from the central nervous system and its subsequent metabolism and excretion, a fairly quick recovery of functions occurs, unless a large dose of the drug has been administered.
Cardiovascular system
Disorders of the cardiovascular system are signs of more serious complications. A decrease in blood pressure, bradycardia, arrhythmia and, in some cases, even cardiac arrest can occur due to the high systemic concentration of local anesthetics. In rare cases, cardiac arrest is not accompanied by previous symptoms of the central nervous system. In studies on volunteers, intravenous infusion of ropivacaine led to inhibition of conduction and contractility of the heart muscle.
Symptoms from the cardiovascular system are usually preceded by manifestations of toxicity from the central nervous system, which may not be noticed if the patient is under the influence of sedatives (benzodiazepines or barbiturates) or under general anesthesia.
In children, the early signs of systemic toxicity of local anesthetics are sometimes more difficult to detect due to difficulties experienced by children in describing the symptoms, or when regional anesthesia is used in combination with general anesthesia.
Treatment of acute toxicity
When the first signs of acute systemic toxicity appear, the drug should be discontinued immediately.
When seizures and symptoms of central nervous system depression occur, the patient needs adequate treatment, the purpose of which is to maintain oxygenation, stop seizures, and maintain the activity of the cardiovascular system. Oxygenation should be provided with oxygen, and, if necessary, the transition to mechanical ventilation. If convulsions do not stop after 15-20 seconds, anticonvulsants should be used: thiopental sodium 1-3 mg / kg iv (provides rapid relief of seizures) or diazepam 0.1 mg / kg iv (the effect develops more slowly compared to the action of sodium thiopental). Suxamethonium 1 mg / kg quickly stops cramps, but its use requires intubation and mechanical ventilation.
In case of inhibition of the cardiovascular system (lowering blood pressure, bradycardia), intravenous administration of 5-10 mg of ephedrine is necessary, if necessary, repeat the administration after 2-3 minutes. With the development of circulatory failure or cardiac arrest, standard resuscitation measures should immediately begin. It is vital to maintain optimal oxygenation, ventilation and blood circulation, and to correct acidosis. With cardiac arrest, longer resuscitation measures may be required.
When treating systemic toxicity in children, it is necessary to adjust the dose according to the age and body weight of the patient.
Storage conditions
Store at a temperature not exceeding 25 ° C.
Do not freeze.
Keep out of the reach of children.
Shelf life
Polypropylene ampoules – 3 years.
Do not use the drug after the expiration date printed on the package.
active ingredient
Ropivacaine
Terms and conditions
prescription
lekarstvennaja form
Solution for
