Naropin
Naropin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Prices in pharmacies
Latin name: Naropin
ATX code: N01BB09
Active ingredient: ropivacaine (ropivacaine)
Manufacturer: ASTRAZENECA, AB (Sweden), ASTRAZENECA, Pty. Ltd. (Australia)
Description and photo update: 2018-07-06
Prices in pharmacies: from 1129 rubles.
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Naropin is a drug for local anesthesia and pain relief.
Release form and composition
Dosage form of Naropin - solution for injection: colorless, transparent (at a concentration of 2; 5; 7.5 or 10 mg / ml - in sealed polypropylene ampoules of 10 or 20 ml, one ampoule in a cell contour packaging, 5 packs in a cardboard box; at a concentration of 2 mg / ml - in plastic infusion containers of 100 or 200 ml, in a blister contour package one container, in a cardboard box 5 packages).
Composition of 1 ml solution:
- active substance: ropivacaine hydrochloride (in the form of ropivacaine hydrochloride monohydrate) - 2; five; 7.5 or 10 mg;
- auxiliary components: sodium chloride, sodium hydroxide and / or hydrochloric acid (up to pH 4-6), water for injection.
Pharmacological properties
Pharmacodynamics
Ropivacaine is a long-acting local anesthetic of the amide series used for both anesthesia and pain relief. Low doses of the substance provide analgesia - they block the sensitivity of a certain part of the body with a non-progressive blockade of motor activity, high doses are used for surgical interventions for local anesthesia. The action of ropivacaine is explained by local blocking of nerve impulses due to its ability to reversibly reduce the permeability of nerve fiber membranes for sodium ions, which leads to an increase in the excitability threshold and a decrease in the rate of depolarization.
Excessive doses of ropivacaine have a suppressive effect on the central nervous system (CNS) and heart muscle due to impaired conduction, reduced automatism and excitability. If an excess amount of a substance reaches the systemic circulation in a short period of time, signs of systemic toxicity may appear. Signs of toxicity from the cardiovascular system (CVS) are preceded by signs from the central nervous system, as they develop at lower plasma concentrations of ropivacaine. The direct effect of a local anesthetic on the heart is to slow conduction, a negative inotropic effect, and in the case of severe overdose, arrhythmias and cardiac arrest. When high doses of intravenous ropivacaine are given, the same effect on the heart occurs.
The duration of anesthesia depends on the dosage used and the route of administration of the drug, but does not depend on the presence of a vasoconstrictor.
Indirect effects from the CVS (lowering blood pressure, bradycardia) can be observed after epidural administration of Naropin due to the arising sympathetic blockade.
Experimental studies in healthy volunteers have shown that intravenous injections of ropivacaine are well tolerated.
Pharmacokinetics
- absorption: with epidural administration, there is a complete two-phase absorption of ropivacaine from the epidural space. Plasma concentration depends on the dose, route of administration and vascularization of the injection site. Pharmacokinetics of ropivacaine is linear, C max (maximum concentration) in blood plasma is proportional to the administered dose;
- distribution: volume of distribution (V d) is 47 liters. Ropivacaine binds intensively to blood plasma proteins, mainly to α1-acid glycoproteins, the unbound fraction is approximately 6%. Long-term administration of Naropin by the epidural method leads to an increase in the total content of the active substance in the blood plasma due to the postoperative increase in the level of α1-acid glycoproteins. Moreover, the concentration of pharmacologically active (unbound) ropivacaine changes to a much lesser extent than its total plasma concentration. The substance has the property of penetrating the placental barrier with the rapid achievement of equilibrium in the active fraction. In the fetus, the degree of binding to blood plasma proteins is less than in the mother, therefore the level of the total plasma concentration of the substance in the fetus is lower than in the mother;
- metabolism: actively metabolized, mainly by hydroxylation with the formation of the main metabolite - 3-hydroxy-ropivacaine;
- excretion: T 1/2 (half-life) for the initial and terminal phases is 14 minutes and 4 hours, respectively. The total plasma clearance is 440 ml / min. After intravenous administration of ropivacaine, approximately 86% of the dose is excreted by the kidneys, mainly in the form of metabolites, and only about 1% of the dose is excreted unchanged in the urine. Approximately 37% of the main metabolite of ropivacaine is excreted by the kidneys, mainly in the form of conjugates.
Indications for use
- conducting anesthesia during surgical interventions: epidural blockade during surgical operations, including caesarean section, blockade of nerve plexuses and large nerves, blockade of individual nerve fibers and infiltration anesthesia;
- relief of acute pain syndrome: periodic bolus administration or prolonged epidural infusion, for example, for pain relief of labor or prevention of postoperative pain, prolonged blockade of peripheral nerves, blockade of individual nerves and infiltration anesthesia, intra-articular injection;
- relief of acute pain syndrome in pediatrics (in newborns and children up to 12 years old inclusive): epidural caudal blockade, prolonged epidural infusion.
Contraindications
Absolute:
- individual hypersensitivity to any component of the drug;
- known hypersensitivity to local anesthetics of the amide series.
Relative (the use of Naropin requires caution):
- severe concomitant diseases and conditions: blockade of cardiac conduction of II and III degrees (intraventricular, atrioventricular, sinoatrial), severe liver dysfunction, progressive liver disease, severe chronic renal dysfunction, hypovolemic shock, weakened state in old age. In such cases, local anesthesia is often preferred. If it is necessary to carry out large blockades to reduce the risk of developing severe adverse manifestations, it is recommended to pre-stabilize the patient's condition and adjust the dose of Naropin;
- recent surgery with the opening of large areas of the joint surfaces or suspicion of recent extensive joint injury - with intra-articular administration (due to the likely increased absorption of ropivacaine and a higher level of its concentration in blood plasma);
- diseases / conditions requiring administration of the drug in the head and neck area (due to the increased frequency of serious adverse reactions);
- children's age up to 6 months;
- diets limiting sodium intake (the content of sodium in Naropin should be taken into account).
Instructions for the use of Naropin: method and dosage
Use or strictly control the use of Naropin should only be a qualified specialist with sufficient experience in conducting anesthesia.
The doctor sets the dose of the drug for each patient individually, based on general and personal experience, taking into account the indications, clinical situation, physical condition of the patient.
In general, the administration of anesthesia during surgery requires the use of higher doses and more concentrated solutions of ropivacaine than when using an anesthetic drug.
To familiarize yourself with the methods and factors affecting the implementation of various types of blockades, as well as with the features and requirements relating to certain groups of patients, it is necessary to use specialized guidelines.
The solution is intended exclusively for single use, it does not contain preservatives. After use, the solution remaining in the container must be destroyed.
Do not autoclave unopened solution containers.
Adults and children over 12 years old
The dose for blockades in adults and children over 12 years old should be selected in accordance with the patient's condition, the injection site, taking into account the individual variability in the rate of development and duration of the blockade.
Usually, for the relief of pain, the recommended concentration of ropivacaine is 2 mg / ml, for intra-articular administration - 7.5 mg / ml.
In order to avoid getting Naropin into the vessel, it is recommended to carry out an aspiration test before and during the administration of the anesthetic. If it is necessary to use a high dose of the drug, you should first enter a trial dose - 3-5 ml of lidocaine with epinephrine. Accidental intravascular injection can be recognized by a temporary increase in heart rate, and accidental intrathecal injection by signs of spinal blockage. In case of toxic symptoms, it is necessary to immediately stop the administration of Naropin.
The introduction of the drug should be carried out slowly or by a sequential increase in the administered doses at a rate of 25-50 mg / min. At the same time, before and during the introduction process, it is necessary to carefully monitor the indicators of the patient's vital functions and constantly maintain verbal contact with him.
To relieve pain after surgery, the following drug administration scheme is recommended: if an epidural catheter was not installed during surgery, after its installation, epidural blockade is performed using a bolus injection of Naropin at a concentration of 7.5 mg / ml, anesthesia is maintained by infusion of the drug at a concentration of 2 mg / ml. As a rule, to prevent moderate to severe postoperative pain, an infusion of Naropin at a rate of 6-14 ml / h (12-28 mg / h) provides adequate pain relief with minimal non-progressive motor blockade.
For postoperative analgesia, the drug at a concentration of 2 mg / ml can be administered as an epidural infusion continuously for 72 hours in combination with or without fentanyl (1–4 mcg / ml). The introduction of Naropin at a concentration of 2 mg / ml at a rate of 6-14 ml / hour provides adequate pain relief in most patients. The use of ropivacaine in combination with fentanyl leads to increased analgesia, but at the same time causes undesirable effects inherent in narcotic analgesics.
In case of epidural blockade during surgical operations, a single injection of Naropin in a dose of not more than 250 mg is usually well tolerated by patients.
In the case of brachial plexus blockade, the use of more than 40 ml of Naropin at a concentration of 7.5 mg / ml (300 mg of ropivacaine hydrochloride) is not recommended, since higher doses can cause symptoms of toxicity from the central nervous system.
It is necessary to take into account the likelihood of creating toxic concentrations of the drug in the blood and local nerve damage during long-term blockade by prolonged infusion or repeated bolus injection. The administration of anesthetic within 24 hours at a total dose of up to 800 mg for surgery and for postoperative pain relief, as well as prolonged epidural infusion for 72 hours at a rate not exceeding 28 mg / hour are usually well tolerated by patients.
For caesarean section, the use of Naropin at a concentration of more than 7.5 mg / ml has not been studied.
Children under 12 years old
For any patient under 12 years of age, the volume of solution for caudal epidural block and the volume of the bolus for epidural administration should not exceed 25 ml.
To prevent accidental intravascular administration of the drug, a thorough aspiration test is required before and during the administration of the anesthetic. During the administration of Naropin, the vital functions of the patient should be constantly monitored. In the event of toxic symptoms, you must immediately stop the drug administration.
A single administration of ropivacaine at a concentration of 2 mg / ml (at the rate of 2 mg / kg or 1 ml / kg solution) for postoperative caudal analgesia provides adequate analgesia below the level of the ThXII spinal cord segment in most patients. Children from 4 years of age tolerate well, as a rule, doses up to 3 mg / kg. To achieve varying sensory block prevalence, the volume of fluid injected for an epidural caudal block can be varied as described in the specific manual.
In patients under 12 years of age, a bolus administration of a calculated dose of Naropin is recommended, regardless of the type of anesthesia being administered.
In overweight children, a gradual reduction in the dose of anesthetic is often required, while the patient's ideal body weight should be guided.
Intrathecal use of Naropin, as well as the introduction of ropivacaine at a concentration of more than 5 mg / ml in children has not been studied. The use of the drug in premature infants has not been studied.
Side effects
Side effects when using Naropin should be distinguished from physiological reactions that occur against the background of epidural anesthesia due to blockade of sympathetic nerves (lowering blood pressure, bradycardia), or reactions associated with the technique of drug administration (local nerve damage, post-puncture headache, meningitis, epidural abscess).
Adverse reactions to ropivacaine are similar to those to other local anesthetics of the amide group.
Effects such as neuropathy and dysfunctions of the spinal cord (including anterior spinal artery syndrome, cauda equina syndrome, arachnoiditis) are usually associated not with the action of the drug, but with the technique of anesthesia.
Inadvertent intrathecal administration of an epidural dose of Naropin can lead to total spinal block.
With systemic overdose and accidental intravascular administration of ropivacaine, serious complications can occur.
Side effects from systems and organs and their frequency in accordance with a special classification [very often (≥ 1/10); often (from ≥ 1/100 to <1/10); infrequently (from ≥ 1/1000 to <1/100); rarely (from ≥ 1/10 000 to <1/1000); very rare (<1/10 000), including isolated messages]:
- CVS: very often - lowering blood pressure (often in children); often - hypertension, tachycardia, bradycardia; infrequently - fainting; rarely - arrhythmia, cardiac arrest;
- gastrointestinal tract: very often - nausea; often - vomiting (in children - very often);
- CNS: often - dizziness, headache, paresthesia; infrequently - anxiety, paresthesia in the perioral zone, numbness of the tongue, dysarthria, ringing in the ears, visual impairment, tremors, convulsions, seizures, hypesthesia;
- genitourinary system: often - urinary retention;
- respiratory system: infrequently - difficulty breathing, shortness of breath;
- general: often - chills, back pain, fever; infrequently - hypothermia; rarely - allergic reactions (urticaria, angioedema, anaphylactic reactions).
Overdose
Since the concentration of local anesthetic in the blood plasma rises slowly, the symptoms of systemic toxicity in case of overdose during regional anesthesia do not appear immediately, but 15–60 minutes after injection. With general toxicity, symptoms from the central nervous system and CVS are manifested primarily. Such reactions are facilitated by high concentrations of local anesthetic in the blood, which can develop due to overdose, intravascular (inadvertent) administration, or high absorption from areas with high vascularization. Overdose reactions on the part of the central nervous system are similar for all local amide anesthetics, and the reactions on the part of the CVS largely depend on the drug and the dose administered.
Accidental intravascular injection of Naropin can lead to an immediate toxic reaction. During the blockade of the nerve plexuses, as well as other peripheral blockades, with the unintentional introduction of the drug into the vessel, there have been cases of seizures.
In case of incorrect intrathecal administration of an epidural dose of the drug, the occurrence of a total spinal block is likely.
Systemic toxicity from the central nervous system appears gradually. First of all, there are visual impairments, numbness in the mouth, tongue, hyperacusis, dizziness, ringing in the ears. More serious symptoms of systemic toxicity, such as tremors, dysarthria and muscle twitching, may precede the development of generalized seizures (these signs cannot be regarded as neurotic behavior of the patient). The progression of intoxication can lead to loss of consciousness, seizures lasting up to several minutes, accompanied by respiratory failure, the rapid development of hypercapnia and hypoxia due to high muscle activity and insufficient ventilation. In severe cases, respiratory arrest may occur. The toxic effects of Naropin intensify the emerging acidosis, hypocalcemia, hyperkalemia.
The restoration of functions subsequently occurs rather quickly due to the redistribution of ropivacaine from the central nervous system and its further metabolism and excretion from the body (provided that a high dose of the drug has not been administered).
CVS disorders are signs of more serious disorders. High systemic concentration of local anesthetics can cause a decrease in blood pressure, bradycardia, arrhythmias, and in some cases even cardiac arrest. Studies in healthy volunteers have shown that intravenous infusion of Naropin causes inhibition of the contractility and conduction of the heart muscle. Usually, symptoms of CVS toxicity are preceded by symptoms from the central nervous system, which may go unnoticed if the patient is under the influence of psycholeptics (barbiturates or benzodiazepines) or under anesthesia. Cardiac arrest in rare cases may not be accompanied by previous central nervous system symptoms.
Early signs of systemic local anesthetic toxicity in children are sometimes more difficult to identify due to difficulties in describing symptoms or in administering a combination of regional and general anesthesia.
If the first signs of systemic toxicity appear, it is necessary to immediately stop the administration of Naropin.
In the case of the development of seizures and symptoms from the central nervous system, appropriate treatment is required to maintain oxygenation, arrest seizures, and maintain the functioning of the CVS. The patient must be provided with oxygen oxygenation or the transition to artificial ventilation. If after 15-20 seconds the seizures do not stop, it is recommended to use anticonvulsants: sodium thiopental at a dose of 1-3 mg / kg intravenously (rapid relief of seizures) or diazepam at a dose of 0.1 mg / kg intravenously (compared with the action of sodium thiopental more slow effect). Suxamethonium at a dose of 1 mg / kg has the property of fairly rapid relief of seizures, but its use requires intubation and mechanical ventilation.
In the case of suppression of the CVS (bradycardia, lowering blood pressure), intravenous administration of ephedrine at a dose of 5-10 mg is recommended, after 2-3 minutes, if necessary, the administration can be repeated. If circulatory failure or cardiac arrest occurs, immediate standard resuscitation is required. Maintaining optimal oxygenation, ventilation and blood circulation, and correcting acidosis are vital measures. In the event of cardiac arrest, resuscitation may take longer.
In children, treatment of systemic toxicity requires the use of doses appropriate to the patient's age and weight.
special instructions
Anesthesia should be performed by experienced medical professionals with the obligatory availability of equipment and appropriate drugs to provide resuscitation measures. An intravenous catheter should be placed in the patient prior to major blockages.
Often, peripheral nerve blockade requires the introduction of a significant volume of local anesthetics into areas of high vascularization near large vessels, which increases the risk of high plasma concentrations of Naropin due to accidental intravascular administration and / or rapid systemic absorption.
Inadvertent subarachnoid administration may result in spinal block with a decrease in blood pressure and respiratory arrest. Convulsions are more likely to develop with brachial plexus block or epidural block, possibly due to accidental injection into a vessel or rapid absorption at the injection site.
There is information about rare cases of cardiac arrest during peripheral nerve blockade or epidural anesthesia with Naropin, especially in elderly patients, with concomitant CVD diseases, as well as as a result of unintentional intravascular injection.
The risk of systemic toxic effects of ropivacaine increases when the drug is used in patients with hypovolemic shock and in patients with low body weight.
Epidural anesthesia often causes a decrease in blood pressure and bradycardia. The introduction of vasoconstrictor drugs or an increase in the volume of circulating fluid can reduce the risk of such adverse reactions. It is recommended to correct the decrease in blood pressure in a timely manner by introducing intravenous ephedrine at a dose of 5-10 mg, if necessary, repeated.
Patients taking class III antiarrhythmic drugs (for example, amiodarone) require careful medical supervision with mandatory monitoring of the electrocardiogram due to the increased risk of side effects of cardiovascular effects.
Long-term use of ropivacaine in patients taking strong inhibitors of cytochrome P4501A2 (including enoxacin, fluvoxamine) should be avoided.
It is necessary to take into account the likelihood of cross-hypersensitivity in the case of the simultaneous use of Naropin with other local amide anesthetics.
Patients on a diet with limited sodium intake should take into account that the preparation contains sodium.
Since Naropin has the potential to lead to porphyria, it can be used in patients with acute porphyria only when there is no safer option for anesthesia or pain relief. In the presence of hypersensitivity in patients, the necessary precautions should be taken.
In some cases, chondrolysis has been reported with prolonged postoperative intra-articular infusion of topical anesthetics. In most of these cases, the infusion was in the shoulder joint. Although a causal relationship with the use of anesthetics has not been confirmed, Naropin is not recommended for prolonged intra-articular infusion.
Influence on the ability to drive vehicles and complex mechanisms
In addition to the analgesic effect, Naropin is able to have a weak transient effect on coordination and motor function. It is necessary to take into account the likelihood of adverse reactions when using the drug and be careful when driving or performing actions that require a high concentration of attention and a quick motor / mental reaction.
Application during pregnancy and lactation
During pregnancy, Naropin can be used when the clinical situation requires it (the use of the drug in obstetrics for analgesia or anesthesia is well justified).
The teratogenic effect of ropivacaine, as well as its effect on reproductive function and fertility, has not been identified. Studies to assess the likely effect of Naropin on fetal development in women have not been conducted.
Experimental studies carried out on rats have shown that the drug does not affect reproduction and fertility in two generations. After the administration of maximum doses of anesthetic to pregnant rats, an increase in offspring mortality was noted in the first three days after birth, which may be explained by a violation of the maternal instinct due to the toxic effect of Naropin on the mother. Side effects of ropivacaine, affecting organogenesis and development of the fetus in the early stages, were also not identified as a result of experiments on rabbits and rats. Perinatal and postnatal studies on rats treated with the drug in the maximum tolerated doses did not show any effect on fetal development at late stages, labor, lactation, viability and growth of offspring.
The penetration of ropivacaine or its metabolites into breast milk has not been studied. Experimental data have shown that the dose of Naropin received by newborns is 4% of the amount administered to the mother. The total dose of anesthetic that can affect a baby during breastfeeding is significantly less than the dose that a fetus can receive when the mother is administered ropivacaine during childbirth.
If it is necessary to use Naropin during lactation, the ratio of the likely benefits to the mother and the potential risk to the child should be taken into account.
Pediatric use
For background information on the methods, factors and conditions for performing individual blockades with the use of local anesthetics in children, refer to the specialized manual.
When using Naropin in newborns and children under 6 months old, it is necessary to take into account the possible immaturity of organs and physiological functions at this age. The clearance of the free fraction of ropivacaine depends on the patient's weight and age in the first years of life. Age influences the development and maturity of liver function; clearance reaches its maximum value at the age of 1 to 3 years. In newborns T 1/2ropivacaine is 5–6 hours compared to 3 hours in older children. The systemic exposure of ropivacaine in newborns is higher, in children 1–6 months - moderately higher than in older children. Significant differences in the concentration of the drug in the blood plasma of newborns observed in clinical trials suggest the presence of an increased risk of systemic toxicity in this group of patients, especially during prolonged epidural infusion.
In newborns, when using Naropin, it is necessary to monitor systemic toxic reactions (control of signs of toxicity from the central nervous system, electrocardiogram, control of blood oxygenation) and local neurotoxicity reactions. Monitoring should be continued after infusion because of the slow excretion of ropivacaine in this patient population.
With impaired renal function
According to the instructions, Naropin should be used with caution in patients with severe chronic renal failure.
As a rule, in patients with impaired renal function, when ropivacaine is administered once or when the drug is used for a short time, the dose does not need to be adjusted. However, in patients with chronic renal failure, acidosis and a decrease in the concentration of proteins in the blood plasma can often develop, which increases the risk of systemic toxicity of Naropin.
For violations of liver function
Since ropivacaine is metabolized in the liver, caution should be exercised when administering the drug to patients with severely impaired liver function, as well as with progressive liver diseases. Sometimes, due to delayed elimination, it becomes necessary to adjust the repeated doses of Naropin downward.
Use in the elderly
Anesthetic should be used with caution in elderly, debilitated patients.
Drug interactions
The simultaneous use of ropivacaine with other local anesthetics or drugs similar in structure to local anesthetics of the amide series may lead to the summation of their toxic effects.
Analogs
The analogues of Naropin are Ropivacaine and Ropivacaine Kabi.
Terms and conditions of storage
Store at a temperature not exceeding 30 ° C. Do not freeze.
Keep out of the reach of children.
The shelf life of the drug in polypropylene ampoules is 3 years, in plastic infusion containers - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Naropin
There are few reviews of Naropin, but they indicate that the effectiveness and degree of manifestation of unwanted side effects when using the drug primarily depend on the qualifications and personal experience of the anesthesiologist.
The price of Naropin in pharmacies
The approximate price for Naropin on average per package is: 5 ampoules of 20 ml at a concentration of 2 mg / ml - 1080 rubles; 5 ampoules of 10 ml each at a concentration of 7.5 mg / ml - 1100 rubles; 5 ampoules of 10 ml at a concentration of 10 mg / ml - 1,500 rubles; 5 containers of 100 ml at a concentration of 2 mg / ml - 2800 rubles.
Naropin: prices in online pharmacies
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Drug name Price Pharmacy |
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Naropin 7.5 mg / ml solution for injection 10 ml 5 pcs. 1129 RUB Buy |
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Naropin 10 mg / ml solution for injection 10 ml 5 pcs. 1149 RUB Buy |
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Naropin 5 mg / ml solution for injection 10 ml 5 pcs. 1629 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
