Ropivacaine - instructions for use, dose, side effects, contraindications

Blockade of initiation and conduction of nerve impulses: decrease in permeability of neuronal cell membranes for Na ions⁺, probably by attachment to sodium channels; increase in permeability for K⁺, which reversibly stabilizes the cell membrane and depresses its depolarization, disrupts the propagation of the action potential and leads to a blockade of conductivity. For blockade of large nerve trunks, a higher concentration of the drug is required than for small peripheral nerves. Blockade of motor nerves is less pronounced than with bupivacaine.

Pharmacokinetics:

The drug is completely subjected to systemic absorption,the speed of which depends on the vascularization of the injection site and the blood flow velocity in it, from the route of administration and the dose (volume and concentration) used, the duration of application when topically applied and combined with vasoconstrictors. The volume of distribution is 0.67 l / kg. When epidurally administered, the distribution is biphasic. Communication with plasma proteins is 94%, predominantly with α1-acid glycoprotein. Biotransformation in the liver, mainly cytochrome CYP1A to 3-hydroxypyvacaine and other metabolites. Half-life (distribution from the epidural space) 14 min (fast phase), 4.2 h (slow phase); half-life (terminal elimination phase) 4.2 h (with epidural administration), 1.8 h (with intravascular injection). Elimination by the kidneys (less than 1% in unchanged form, 86% in the form of metabolites: almost 37% in the form of 3-hydroxypropvacaine, 1-3% in the form of 4-hydroxyropivacaine, N-dealkylated metabolites and 4-hydroxydealkylated ropivacaine). The addition of epinephrine does not affect the pharmacokinetics of ropivacaine in blockade of the brachial plexus, but lengthens its effect with intradermal injection.

Indications:

Anesthesia during surgical interventions: epidural blockade in surgical interventions, including cesarean section; blockade of large nerves and nerve plexuses; blockade of individual nerves and local infiltration anesthesia.

Pain relief of acute pain syndrome: prolonged epidural infusion or intermittent bolus administration, for example, to eliminate postoperative pain or anesthetic delivery; blockade of individual nerves and local infiltration anesthesia.

ICD-10

XVIII.R50-R69.R52.0 Acute pain

XXI.Z40-Z54.Z51.4 Preparatory procedures for subsequent treatment, not elsewhere classified

Contraindications:

Hypersensitivity to any amide local anesthetics; children under 12 years.

Carefully:Blockade of intracardiac conduction of II and III degrees (sinoatrial, atrioventricular, intraventricular), progressive liver diseases, severe hepatic insufficiency, severe chronic renal failure, with hypovolemic shock therapy.

Pregnancy and lactation:

Penetrates through the placenta. Controlled studies in humans have not been conducted.In rats and rabbits, in doses exceeding those recommended for humans in 2.5 and 5 times, respectively, does not exhibit teratogenicity. The relationship between ropivacaine and fetal plasma proteins is less than that of the mother, so the concentration of the drug in fetal plasma is less than the total concentration of the drug in the mother's plasma. There is no information on the penetration into breast milk, but the negative impact on the child is not described.

Recommendations for FDA - Category B.

Dosing and Administration:Lumbar anesthesia:

- for surgical interventions: 75-150 mg of a 0.5% solution (5 mg / ml), 113-188 mg of a 0.75% solution (7.5 mg / ml) or 150-200 mg of a 1% solution (10 mg / ml) with a gradual increase in the dose.

- with caesarean section: 100-150 mg of a 0.5% solution (5 mg / ml) with a gradual increase in the dose.

Anesthesia in obstetrics: 20-40 ml of a 0.2% solution (2 mg / ml) followed by a prolonged infusion at a rate of 12-28 mg / h or 20-30 mg / h in fractional increments.

Postoperative analgesia: 12-28 mg / h 0.2% solution (2 mg / ml) as a continuous infusion.

Thoracic anesthesia:

- anesthesia during surgery: 25-75 mg of a 0.5% solution (5 mg / ml) with a gradual increase in the dose.

- Postoperative analgesia: 12-28 mg / h 0.2% solution (2 mg / ml) as a continuous infusion.

Side effects:

Allergic reactions: skin manifestations, anaphylactic shock.

Most of the side effects arising from anesthesia are not due to the effect of the anesthetic used, but to the technique of conducting regional anesthesia. Most often (more than 1%), the following adverse effects were noted, which were regarded as having clinical significance, regardless of whether a causal relationship was established with the use of an anesthetic.

From the side of cardio-vascular system: Arterial hypertension, arterial hypotension, bradycardia, tachycardia.

From the side digestive system: nausea, vomiting.

From the side CNS and peripheral nervous system: headache, dizziness, paresthesia.

Neuropathy and impaired spinal cord function (anterior spinal artery syndrome, arachnoiditis) are usually associated with the technique of conducting regional anesthesia, and not with the action of ropivacaine.

Other: fever, chills, urinary retention.

Overdose:

Initial manifestations of acute overdose - impaired vision and hearing, numbness around the mouth, dizziness, paresthesia, dysarthria, muscle tone increase, muscle twitching, arrhythmias.With progression - apnea, cyanosis of the lips and / or skin, circulatory collapse, convulsions, cardiac arrest. Early signs of neurotoxicity - anxiety, blurred vision, chills, dizziness, blockage, headache, slurred speech, nausea, numbness or tingling of the lips or mucous membrane of the mouth, anxiety, tremor, muscle twitching.

Treatment: cessation of the administration of ropivacaine; Infusion therapy and the use of vasopressors in the collapse. In case of hypotension, the woman in labor should put it on her left side in order to eliminate the pressure of the pregnant uterus on the aorta and inferior vena cava; Delivery can improve the response to ongoing activities. With convulsions ensure patient safety and oxygen supply; in the absence of the effect of respiratory support - intravenous administration of benzodiazepines (diazepam with an increment of 2.5 mg) or barbiturates of ultrashort action (thiopental sodium, thiamylal with an increment of 50-100 mg; with intravenous administration of barbiturates, inhibition of hemocirculation is possible) with an interval of 2-3 minutes; with nekupiruemyh convulsions and the presence of mechanical ventilation are shown muscle relaxants; for a short time after the onset of seizures, rapid development of hypoxia, hypercapnia, and acidosis is possible; monitoring of blood pressure,heart rate, neurological status and respiratory function continuously. Supportive therapy: providing and maintaining airway patency, if necessary - endotracheal intubation, IVL.

Interaction:

With the simultaneous use of ropivacaine with other local anesthetics or drugs structurally similar to local anesthetics of the amide type, a summation of effects is possible.

Special instructions:

The procedure of regional anesthesia should be carried out by an experienced specialist in the presence of equipment and drugs for resuscitation. Prior to the execution of large blockades, intravenous catheters should be installed.

With caution should be entered ropivacaine patients with severe concomitant diseases (including partial or complete blockade of the heart, progressive cirrhosis of the liver, a significant impairment of kidney function). To reduce the risk of serious side effects, it is necessary to pre-treat co-morbidities before carrying out large blockages, as well as correct the used dose of anesthetic.In patients with severe liver disease due to elimination of elimination, it may be necessary to reduce the dose of ropivacaine with repeated injections. Usually, patients with impaired renal function with a single administration or with a short-term infusion do not need a dose adjustment. However, in chronic renal failure, acidosis and hypoproteinemia are often observed, which increases the risk of systemic toxic effects of ropivacaine. In such cases, doses of ropivacaine should be reduced.

In case of accidental intravascular injection of ropivacaine, the development of symptoms of intoxication, manifested immediately or in a delayed period, is possible.

The use of ropivacaine can lead to a temporary disruption of motor functions, coordination of movements and the speed of psychomotor reactions. The period of time through which it is possible to engage in potentially hazardous activities requiring increased attention is established individually.

Instructions

Ropivacaine (Ropivacainum)