Index of drugs

Anesthesia in surgery, in adults and adolescents> 12 years: epidural anesthesia in surgery, including Caesarean section; blockages of large nerves; local blocks.

1 ml of solution contains 7.5 mg or 10 mg of ropivacaine hydrochloride (and 3 mg of sodium).

A long-acting local anesthetic of the amide group, in the form of a pure enantiomer. At high doses, ropivacaine has an anesthetic effect in surgery, while at lower doses, it causes sensory blockade with a limited and non-impinging motor blockade. The mechanism of action is based on the reversible reduction of the permeability of the nerve fiber sheath to sodium ions. As a result, the speed of depolarization is reduced, and the increased threshold of excitability is reduced, which causes local blocking of nerve impulses. The concentration of ropivacaine in the blood depends on the dose, the route of administration and the vascularity at the injection site. The epidural space is completely absorbed, with a half-life running in two phases of 14 min and 4 h. It is mainly associated with acid α₁glycoprotein. Ropivacaine readily crosses the placenta and rapidly attains the equilibrium state of the unbound fraction. It is metabolized in the liver mainly by hydroxylation of aromatic rings. After intravenous administration, 86% of the dose is excreted via the kidneys, of which 1% is unchanged. The main metabolite is 3-hydroxypivacaine, 37% of which is excreted via the kidneys, mainly in conjugated form. Other metabolites excreted in the urine (1-3%). Final T_0,5 ropivacaine is 1.8 hours.

Hypersensitivity to the active substance, other topical anesthetics of the amide group or to any of the excipients. General contraindications for epidural anesthesia, regardless of the type of anesthetic used. Sectional intravenous anesthesia. Peri-cutal anesthesia in obstetrics. Hypovolemia.

Particular caution must be paid to patients: elderly and / or in poor general condition; with a complete or partial block of the heart (anesthetics may inhibit the conductivity of the myocardium); treated with class III anti-arrhythmics, e.g. Amiodarone (additive effects on the heart may occur, patients should be observed and monitored by ECG); with porphyria (risk of worsening the disease; in patients with acute porphyria, ropivacaine should be used only if necessary); with advanced liver disease (ropivacaine is metabolised in the liver, the risk of slowing down the excretion of the drug); with severe renal failure. Acidosis and reduced plasma protein levels, often seen in patients with chronic renal failure, may increase the risk of drug toxicity. Long-term administration of ropivacaine should be avoided in patients concomitantly receiving strong CYP1A2 inhibitors. Rare cases of cardiac arrest during the use of epidurals or during peripheral nerve blockade have been reported, especially after unintended intravascular administration, in elderly patients and in patients with concomitant cardiac disease. In case of injections within the head and neck, serious side effects may occur more frequently. Blockages of large peripheral nerves may require a large volume of local anesthetic to highly vascularised areas, often near large vessels, which is associated with a higher risk of intravascular and / or rapid absorption of the drug, which in turn may lead to high plasma concentrations of the drug . Continuous intraarticular infusions are not an approved indication for ropivacaine; continuous intraarticular infusions of ropivacaine should be avoided, as efficacy and safety have not been established, and there is a risk of chondrolysis. The sodium content (3 mg / ml) should be considered for patients on a controlled sodium diet. The safety and efficacy of the medicine (7.5 mg / ml and 10 mg / ml) in children under 12 years of age have not been established.

In addition to the epidural anesthesia used in obstetrics, there are insufficient data on the use of ropivacaine in pregnant women. There are no data on the excretion of ropivacaine in breast milk.

Very common: hypotension, nausea. Common: paraesthesia, headache, dizziness, bradycardia, tachycardia, hypertension, vomiting, urinary retention, fever, stiffness, back pain. Uncommon: anxiety, CNS toxicity (convulsions, grand mal seizures, dizziness, numbness around the mouth, numbness of the tongue, auditory hypersensitivity, tinnitus, visual disturbances, dysarthria, muscle spasms, tremor), hypoaesthesia, syncope, dyspnea hypothermia. Rarely: cardiac arrest, arrhythmia, hypersensitivity reactions (anaphylactic shock, angioneurotic edema, urticaria). Symptoms of systemic toxicity mainly affect the CNS and cardiovascular system, are caused by high levels of local anesthetic in the blood, which may occur due to (accidental) intravascular administration, overdose or extremely rapid absorption from richly vascularised parts of the body. In addition, neuropathy and spinal cord dysfunction (e.g., anterior spinal artery syndrome, arachnoiditis, horse's tail syndrome) have been observed during the spinal anesthesia, which may rarely disappear. A full subarachnoid block may occur if the epidural dose is accidentally administered subarachnoidly. The use of epidural anesthesia and brachial plexus block is associated with a greater risk of seizures. Chondrolysis has been reported in patients receiving post-operative continuous intra-articular infusion of local anesthetics, including ropivacaine.

Adults and children> 12 years: individually, taking into account the physical condition of the patient, administer the lowest effective dose. The doses presented below are the minimum effective doses and should be considered as guidelines for use in adult patients; individual differences in the induction and duration of the dose effect are possible.Anesthesia in surgery. Epidural in the lumbar region. Surgical procedures: 15-25 ml of a 7.5 mg / ml solution, i.e. 113-188 mg (induction time 10-20 min, duration 3-5 min) or 15-20 ml of a 10 mg / ml solution , i.e. 150-200 mg (induction time 10-20 min, duration 4-6 min). Caesarean section: 15-20 ml of 7.5 ml solution, i.e. 113-150 mg (induction time 10-20 min, duration 3-5 min) - increasing dose should be used: initial dose approx. 100 mg (13 or 14 ml) administered for 3-5 min; you can give 2 additional doses - max. 50 mg in total.Epidural in the thoracic region. Blockade in the treatment of post-operative pain: 5-15 ml (depending on the level of administration) of a 7.5 mg / ml solution, i.e. 38-113 mg (induction time 10-20 min).Big nerve blockage. Shoulder plexus blockade: 30-40 ml of a 7.5 mg / ml solution, i.e. 225-300 mg (induction time 10-25 min, duration 6-10 min).Local block (eg small nerve blockage and infiltration): 1-30 ml of a 7.5 mg / ml solution, i.e. 7.5-225 mg (induction time 1-15 min, duration 2-6 min).Way of giving. Epidural and perineural administration. Careful aspiration before and during injection is recommended to avoid intravascular administration. If high doses are required, a test dose of 3-5 ml of adrenaline Lidocaine solution is recommended. Unintentional intravascular administration can be diagnosed based on transient cardiac acceleration and unintentional subarachnoid administration based on the symptoms of the spinal block. Aspiration should be repeated before and during the administration of the main dose, which should be injected slowly or in increasing doses at a rate of 25-50 mg / min. At the same time, life activities should be carefully monitored. In case of toxic effects, the drug should be stopped immediately. Maximum doses up to 250 mg of ropivacaine were used for maxillary surgical anesthesia, they were well tolerated. Single doses to 300 mg of ropivacaine were used to block the brachial plexus in individual patients, and they were well tolerated. Access to trained personnel, equipment and medicines should be provided for resuscitation. Exercise caution and do not inject into the inflamed area.