Ropivacaine Cabi, 5 mg/ml 10 ml 5 pcs

A long-acting local anesthetic of the amide type, which is a pure enantiomer. It has both anesthetic and analgesic effect. By reversibly blocking potential-dependent Na+-channels it prevents generation of impulses in the endings of sensitive nerves and conduction of impulses along the nerve fibers. Signs of CNS toxicity precede signs of cardiovascular toxicity because they are observed at lower concentrations of the drug in plasma. Ropivacaine has a wide therapeutic range (range between therapeutic and toxic doses).
In vivo studies on animals have shown that ropivacaine has less toxic effects on the myocardium compared to bupivacaine. Indirect cardiovascular effects (arterial hypotension, bradycardia) may occur after epidural administration of ropivacaine and are due to the resulting sympathetic blockade.

The onset and duration of anesthesia with Ropivacaine Cabi depend on the concentration and site of administration of the drug.

Indications

At concentrations of 7.5 mg/1 ml and 10 mg/1 ml, Ropivacaine Cabi is used v adults and children over 12 years of age for the following indications:

Anesthesia in surgical procedures:

• epidural blockade in surgical procedures, including cesarean section;
• blockade of major nerves and nerve plexuses;
• blockade of individual nerves and infiltration anesthesia.

Intraarticular injection in knee arthroscopy.

At a concentration of 2 mg/1 ml, Ropivacaine Kabi is used for the following indications:

Capitation of acute pain syndrome in adults and children over 12 years of age.

• prolonged epidural infusion or intermittent bolus administration, such as for postoperative pain or labor pain;
• extended peripheral nerve block by infusion or bolus injections (for postoperative pain).

Acute pain control in children from 1 to 12 years (inclusive):

Single and prolonged peripheral nerve blockade.

In newborns and children under 12 years of age (inclusive);

• caudal epidural block;
• extended epidural infusion.

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Active ingredient

Ropivacaine

How to take, the dosage

For perineural administration (spinal and conduction anesthesia)

Intravenous catheters must be inserted before large blockades can be performed.

Ropivacaine Kabi is administered slowly or by increasing successive doses of the drug at a rate of 25-50 mg/min.

In order to prevent the anesthetic from entering the vessel, aspiration testing should always be performed prior to and during the administration of the drug. Accidental intravascular injection is recognized by a temporary increase in heart rate.

The following table is a guide to dosage selection for intrathecal blockade, acute pain relief, and peripheral nerve blocks. A minimum dosage sufficient to produce an effective block should be used. The clinical professional’s experience and knowledge of the patient’s physical condition is important in deciding which dose to use.

Ropivacaine Kabi dosing recommendations for adults and children older than 12 years (see Table 2). Table 2)

Table 2

The dosing recommendations for Ropivacaine Kabi for children 1 to 12 years of age (see Table 3. Table 3)

Table 3

The doses listed in the table are considered sufficient to achieve a reliable blockade and are indicative when using the drug in adults because there is individual variability.There is individual variability in the rate of block and its duration.

Intrathecal administration of ropivacaine hydrochloride has not been studied for anesthesia in caesarean section.

Individual differences occur with respect to the onset of the blockade and its duration.

The values in the Dose column represent an estimated average range of required doses. Please refer to the standard manuals for information about factors that affect block technique and individual patient characteristics.

In the absence of sufficient clinical evidence, we do not recommend the use of Ropivacaine Cabi in children less than 1 year of age.

Interaction

This medicinal product should not be mixed with other medicinal products.

The concomitant use of Ropivacaine Cabi with local anesthetics, drugs structurally similar to local amide anesthetics or drugs depressing the central nervous system (CNS) may increase the toxic effects of the drugs.

Patients taking class III antiarrhythmic drugs (e.g., amiodarone) should be under constant medical supervision and ECG monitoring, as cardiovascular side effects may occur.

In alkaline solutions, ropivacaine hydrochloride may precipitate because it is weakly soluble at pH >6.0). In vivo, concomitant use of ketoconazole, a potent selective inhibitor of CYP3A4 isoenzyme, decreased plasma clearance of ropivacaine hydrochloride by 15%. However, inhibition of this isoenzyme is unlikely to be clinically significant.

In vitro ropivacaine hydrochloride is a competitive inhibitor of CYP2D6 isoenzyme, while inhibition of this isoenzyme is not achieved at the plasma concentrations of the drug used in practice.

Special Instructions

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Contraindications

• hypersensitivity to the active ingredient, any of the excipients or other local anesthetics of the amide type;
• also the general contraindications for each specific type of anesthesia should be considered, regardless of the anesthetic used;
• The drug Ropivacaine Cabi is contraindicated for intravenous regional “large” blockade anesthesia in patients with hypovolemia and paracervical anesthesia in obstetrics.

With caution

Elderly patients, patients in a weakened state or patients with severe comorbidities, including Grade II and III intracardiac conduction blockages (sinoatrial, atrioventricular, intraventricular), advanced liver disease, severe hepatic failure, severe chronic renal failure, acute porphyria, during therapy of hypovolemia, frail patients, elderly, childhood, pregnancy and during lactation.

The use of regional anesthesia is preferable for these groups of patients. When performing “large” blocks, in order to reduce the risk of severe adverse events, it is recommended to stabilize the patient’s condition beforehand and to adjust the anesthetic dose.

Caution should be exercised when injecting local anesthetics into the head and neck region because of the possible increased frequency of serious adverse events.

Patients on a sodium-restricted diet should consider the sodium content of the drug.

Side effects

Adverse reactions to Ropivacaine Kabi are similar to those to other amide-type local anesthetics. Adverse reactions must be distinguished from physiological effects of the block itself, such as hypotension and bradycardia during subdural anesthesia, or effects associated with the technique of drug administration (e.g., spinal hematoma, local nerve damage, headache after subdural puncture, meningitis and epidural abscess).

Side effects common to local anesthetics

Central and peripheral nervous system disorders

Neuropathy and spinal cord dysfunction (anterior spinal artery syndrome, arachnoiditis, cauda equina syndrome) are possible, usually related to the technique of regional anesthesia rather than the action of the drug.

The accidental intrathecal administration of a dose in excess of the recommended dose may result in complete spinal block. Serious complications are possible with systemic overdose and unintentional intravascular administration of the drug (see section “Overdose”).

Acute systemic toxicity

Ropivacaine Kabi may cause acute systemic toxic reactions if high doses are used or if its blood concentration rises rapidly if the drug is inadvertently administered intravascularly or in overdose (see “Pharmacological properties” and “Overdose”).

The most frequently reported side effects of the drug

A variety of side effects have been reported, with the vast majority not related to the anesthetic agent used but to the regional anesthetic technique.

The most frequently reported adverse effects (>1%) were the following, which were considered to be clinically significant regardless of whether a causal relationship with anesthetic use was established: decreased BP*, nausea, bradycardia, vomiting, paresthesia, increased body temperature, headache, urinary retention, dizziness, chills, increased BP, tachycardia, hypoesthesia, anxiety.

The incidence of adverse effects is as follows: Very common – >1/10; common – >1/100 to <1/10; infrequent – >1/1000 to <1/100; rare – >1/10,000 to <1/1,000; very rare – <1/10,000; unknown – cannot be determined based on available data.

Nervous system disorders: frequent – headache, paresthesia, dizziness; infrequent – anxiety, symptoms of CNS toxicity (seizures, grand convulsive seizures, peroral paresthesia, tongue numbness, hyperacusis, tinnitus, visual disturbances, dysarthria, muscle twitching, tremor)*, hypoesthesia.

Chronic disorders: very common – decreased BP (hypotension); common – bradycardia, tachycardia, increased BP; infrequent – syncope; rare – cardiac arrest, arrhythmia.

Disorders of the respiratory system, thorax and mediastinum: infrequent – dyspnea, difficulty in breathing.

Gastrointestinal disorders: very common – nausea; common – vomiting.

River and urinary tract disorders: frequently – urinary retention.

General disorders and disorders with administration: frequently – 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).

Overdose

Acute systemic toxicity

Inadvertent intravascular administration during plexus blocks or other peripheral blockages has resulted in cases of seizures.

If an intrathecal epidural dose of anesthetic is inappropriately administered, a complete spinal block may occur.

The accidental intravascular administration of anesthetic may cause an immediate toxic reaction.

In case of overdose during regional anesthesia, symptoms of a systemic toxic reaction appear delayed 15-60 minutes after injection due to a slow increase in plasma concentration of the local anesthetic.

Systemic toxicity is primarily manifested by symptoms of the central nervous system (CNS) and cardiovascular system (CVS). These reactions are caused by high concentrations of the local anesthetic in the blood, which may occur due to (accidental) intravascular administration, overdose or exceptionally high adsorption from highly vascularized areas.

CNS reactions are similar for all amide-type local anesthetics, whereas cardiovascular reactions are more dependent on the injected drug and its dose.

Central nervous system

The central nervous system manifestations of systemic toxicity develop gradually: first there are visual disturbances, numbness around the mouth, tongue numbness, hyperacusis, tinnitus, dizziness. Dysarthria, tremors and muscle twitching 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 progression of intoxication there may be loss of consciousness, seizures lasting from several seconds to several minutes, accompanied by respiratory disorders, rapid development of hypoxia and hypercapnia due to increased muscle activity and inadequate ventilation. In severe cases, respiratory arrest may even occur. Arising acidosis, hyperkalemia, hypocalcemia increase toxic effects of anesthetic.

Thereafter, due to redistribution of the anesthetic from the CNS and its subsequent metabolism and excretion, there is a fairly rapid recovery of function, unless a large dose of the drug was administered.

Cardiovascular system

Cardiovascular system disorders are signs of more serious complications. Decreased BP, bradycardia, arrhythmias, and in some cases even cardiac arrest can occur due to high systemic concentrations of local anesthetics. In rare cases, cardiac arrest is not accompanied by preceding CNS symptoms. In studies on volunteers, intravenous infusion of ropivacaine resulted in inhibition of conduction and cardiac contractility.

The cardiovascular symptoms are usually preceded by CNS toxicity that may not be seen if the patient is under sedation (benzodiazepines or barbiturates) or general anesthesia.

In children, early signs of systemic toxicity of local anesthetics may be more difficult to detect due to difficulties in describing symptoms in children or when regional anesthesia is combined with general anesthesia.

The treatment of acute toxicity

In case of the first signs of acute systemic toxicity, the drug should be stopped immediately.

In case of convulsions and CNS depression symptoms, the patient requires adequate treatment to maintain oxygenation, arrest convulsions, maintain cardiovascular activity. Oxygenation with oxygen should be provided, and if necessary, transfer to artificial lung ventilation. If seizures do not stop after 15-20 seconds, anticonvulsants should be used: sodium thiopental 1-3 mg/kg IV (provides rapid relief of seizures) or diazepam 0.1 mg/kg IV (action is slower compared to that of sodium thiopental). Suxamethonium 1 mg/kg quickly stops seizures, but intubation and ventilatory support are required.

In case of depressed cardiovascular activity (decreased BP, bradycardia) intravenous injection of 5-10 mg of ephedrine is necessary, repeat the injection after 2-3 minutes if necessary. If circulatory failure or cardiac arrest develops, standard resuscitation measures should be started immediately. It is vital to maintain optimal oxygenation, ventilation and blood circulation, and to correct acidosis. Longer resuscitation interventions may be necessary in cardiac arrest.

In therapy of systemic toxicity in children, doses should be adjusted according to the patient’s age and body weight.