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:
Anesthesia for surgical interventions:
epidural block during surgical interventions, including cesarean section
blockade of large nerves and nerve plexuses
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 II and III degree,o Local anesthesia is indicated.
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 may need to 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
The drug is used for perineural administration (spinal and conduction anesthesia).
Ropivacaine Kabi should be administered only by specialists with sufficient experience in conducting local anesthesia or under their supervision, in the presence of equipment and drugs for resuscitation.
Adults and children over 12 years of age
In general, anesthesia for surgical interventions requires higher doses and more concentrated solutions of the drug than when using an anesthetic for pain relief. For analgesia (e.g. epidural administration to suppress acute pain), lower concentrations and doses are recommended and a dose of 2 mg / 1 ml is usually recommended. For intraarticular administration, a dose of 7.5 mg / 1 ml is recommended. Ropivacaine Kabi 10 mg / 1 ml is recommended for epidural anesthesia, when complete motor blockade is necessary for operations.
The following tables provide guidance on dosage selection for more commonly used blockades. The minimum dosage should be used, sufficient to form an effective blockade. When deciding on a dose choice, the experience of a clinical specialist and knowledge of the patient ² ¢s physical condition are important.
Table 1. Dosage recommendations for ropivacaine Kabi for adults and children over 12 years of age
The dosages given in table 1 are considered sufficient for successful blockade and should serve as a guide for use in adult patients, as there are individual deviations in the time of the blockade and its duration. The values ² ¹ ² ¹in the Dose column reflect the expected range of averaged required doses.
Dosage recommendations for the drug Ropivacaine Kabi for adults and children over 12 years of age:
Drug concentration (mg / ml) Solution volume (ml) Dose (mg) Onset of action (min) Duration of action (h)
Surgical anesthesin:
Lumbar epidural anesthesia:
Surgical interventions 7.5 15-25 113-188 10-20 3-5
10 15-20 150-200 10-20 4-6
Caesarean section 7.5 15-20 113-1501 10-20 3-5
Epduralpic anesthesia at the thoracic level
Postoperative analgesic blockade and surgical procedures 7.5 5-15 38-113 10-20 n / a 2
Blockade of the large nerve plexuses
For example, brachial plexus block * 7.5 30-40 225-300 10-25 6-10
Conduction and infiltration anesthesia 7.5 1-30 7.5-225 1-15 2-6
Relief of acute pain
Epidural administration at the lumbar level
Bolus 2.0 10-20 20-40 10-15 0.5-1. 5
Intermittent administration (e.g. during labor pain relief) 2.0 10-15 (minimum 30 min interval) 20-30
Extended infusion for:
labor pain relief 2.0 6-10 ml / h 12-20 mg / h n / a n / e
postoperative analgesia 2.0 6-14 ml / h 12-28 mg / h n / a n / a
Peripheral nerve blockade
For example, femoral block or interstitial block (prolonged infusion or re-injection) 2.0 5-10 ml / h 10-20 mg / h n / a n / a
Thoracic epidural administration
Prolonged infusion (e.g. for postoperative pain management) 2.0 6-14 ml / h 12-28 mg / h n / d n / a
Conduction blockade and infiltration anesthesia 2.0 1-100 ml / h 2-200 1-5 2-6
Intra-articular injection
Knee arthroscopy ** 7. 5 20 150 *** n / a 2-6
* Dosage for conduction anesthesia should be determined in accordance with the place of use and the condition of the patient. The staircase and supraclavicular block of the brachial plexus can lead to a higher incidence of adverse reactions, regardless of the local anesthetic used.
** Cases of chondrolysis in postoperative prolonged intra-articular infusion of local anesthetics have been reported. Ropivacaine Kabi should not be used for prolonged intra-articular administration.
*** If Ropnvacaine Kabi was additionally used for other types of anesthesia, the maximum dose should not exceed 225 mg.
1 – Step-by-step dosing should be used, the initial dose of about 100 mg (97.55 mg = 13 ml, 105 mg = 14 ml) and administered within 3-5 minutes. Two additional doses, a total of an additional 50 mg, may be administered as needed.
2 – N / A = not really.
Standard guidelines should be used to familiarize oneself with the factors that influence the method of performing individual blockades and the requirements for specific patient groups.
To prevent the anesthetic from entering the bloodstream, an aspiration test must be performed before and during the administration of the drug. If it is necessary to administer a large dose of the drug, it is recommended that a test dose of 3-5 ml of lidocaine with epinephrine be administered. Accidental intravascular administration is recognized by a temporary increase in heart rate, and accidental intrathecal administration by signs of the spinal block. In case of toxic symptoms, the drug should be discontinued immediately.
Aspiration should be carried out before and during administration, the main dose, which must be entered slowly or step by step, at the level of 25-50 mg / min, carefully observing the patient’s vital functions and maintaining verbal contact with him.
A single administration of ropivacaine Kabi with epidural blockade for surgical intervention in a dose of up to 250 mg is usually well tolerated by patients.
When blocking the brachial plexus with 40 ml of the drug Ropivacaine Kabi 7.5 mg / 1 ml, the maximum plasma concentrations of ropivacaine in some patients can reach a value characterized by mild symptoms of toxicity from the central nervous system. Therefore, the use of a dose higher than 40 ml of the drug Ropivacaine Kabi 7.5 mg / 1 ml (300 mg of ropivacaine) is not recommended.
When using a prolonged blockade, either by continuous infusion or by repeated bolus administration, the risks of achieving a toxic plasma concentration or the occurrence of local nerve damage should be taken into account. The introduction of ropnvacaine for 24 hours in a dose of up to 800 mg in total during surgical interventions and for postoperative pain relief, as well as prolonged epidural infusion after surgery at a rate of up to 28 mg / h for 72 hours, is well tolerated by adult patients.
For the relief of postoperative pain, the following method is recommended: if an epidural catheter was not installed during surgery, after its installation an epidural block is performed with a bolus injection of Ropivacaine Kabi 7.5 mg / 1 ml. Analgesia is supported by the infusion of the drug Ropivacaine Kabi 2 mg / 1 ml. In most cases, for relief of moderate to severe postoperative pain, infusion at a rate of 6-14 ml / h (12-28 mg / h) provides adequate analgesia with minimal non-progressive motor blockade (using this technique, a significant decrease in the need for opioid analgesics was observed ) For postoperative analgesia, ropivacaine Kabi 2 mg / 1 ml can be administered continuously as an epidural infusion for 72 hours without fentanyl or in combination with it (1-4 Ñg / ml). When using the drug Ropivacaine Kabi 2 mg / 1 ml (6-14 ml / h), adequate pain relief was provided in most patients.
The combination of ropivacaine Kabi and fentanyl resulted in improved analgesia, while causing side effects inherent in narcotic analgesics.
The use of a concentration of Ropivacaine Kabi over 7.5 mg / 1 ml for caesarean section has not been studied.
Renal failure
As a rule, when a single dose or short-term therapy is administered to patients with impaired night function, a dose change is not required.
Hepatic insufficiency
Ropivacaine is metabolized in the liver and, therefore, should be used with caution in patients with serious liver diseases. Repeated doses may need to be reduced due to delayed elimination.
Hypovolemia patients
Hypovolemia patients may develop acute and severe hypotension during epidural anesthesia for any reason, regardless of the use of a local anesthetic.
table 2. Dosage recommendations for the drug Ropivacaine Kabi for children from 0 to 12 years old
Concentration mg / ml Volume mg / kg Dose mg / kg
Relief of acute pain (pre- and postoperative analgesia)
Caudaly epidural administration 2.0 1 2
Blockade below T12. in children with a body weight of up to 25 kg
Extended epduralia iifusion in children with a body weight of up to 25 kg
Age from 0 to 6 months
Bolus administration 2.0 0.5-1 1-2
Infusion up to 72 h 2.0 0.1 ml / kg / h 0.2 ml / kg / h
Age from 6 to 12 months
Bolus administration 2.0 0.5-1 1-2
Infusion up to 72 h 2.0 0.2 ml / kg / h 0.4 ml / kg / h
Age from 1 to 12 years inclusive
Boluspoi introduction 2.0 2.0 2
Infusion up to 72 h 2.0 0.2 ml / kg / h 0. 4 ml / kg / h
a – Smaller doses from the suggested dosing interval are recommended for thoracic and epidural blocks, while large ones for lumbar and caudal epidural blocks.
b – Recommended for lumbar epidural block. It is justified to reduce the bolus dose in case of analgesia at the chest level.
Dosages in table 2 should be considered a guide to the use of the drug in pediatric practice. At the same time, there is an individual variability in the rate of development of the block and its duration. In children with increased body weight, a gradual decrease in the dose of the drug is often required, and the ideal body weight of the patient should be considered as the basis. For factors affecting specific blockade techniques and individual patient requirements, data should be considered, given in standard manuals. The volume for a single caudal blockade and the volume for epidural bolus dosages should not exceed 25 ml in any patient.
Careful aspiration is recommended before and during injection to prevent intravascular injection. During the administration of the drug, it is necessary to carefully monitor the vital functions of the patient. In case of toxic symptoms, the infusion should be stopped immediately. A single caudal epidural injection of ropivacaine at a dose of 2 mg / 1 ml (based on 2 mg / kg, solution volume 1 ml / kg) forms an adequate postoperative analgesia below the T1 / 2 level in most patients.
Children over 4 years old tolerate doses of 3 mg / kg. The volume of the injected solution for epidural administration at the caudal level can be changed in order to achieve different prevalence of the sensory block, which is described in specialized manuals.
Regardless of the type of anesthesia, a bolus of a calculated dose is recommended.
The use of the drug in concentrations above 5 mg / 1 ml, as well as the intrathecal use of the drug Ropivacaine Kabi in children has not been studied.
Regardless of the route of administration, the use of ropivacaine has not been studied in premature infants.
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 drug administration technique (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 (convulsions, large seizures, paresthesia in the near-mouth zone, numbness of the tongue, hyperacusis, tinnitus, visual impairment, dysarthria, muscle twitching, tremor) *, hypesthesia. Disorders of 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. Common 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.
The simultaneous use of the drug 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 the drugs.
patients, those taking class III antiarrhythmic drugs (for example, 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, 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.
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
