Rapinov (Solution) Instructions for Use

Marketing Authorization Holder

Pharmasintez, JSC (Russia)

ATC Code

N01BB09 (Ropivacaine)

Active Substance

Ropivacaine (Rec.INN registered by WHO)

Dosage Forms

	Rapinov	Solution for injection 2 mg/1 ml: 10 ml amp. 5, 10 or 25 pcs.
		Solution for injection 5 mg/1 ml: 10 ml amp. 5, 10 or 25 pcs.
		Solution for injection 7.5 mg/1 ml: 10 ml amp. 5, 10 or 25 pcs.
		Solution for injection 10 mg/1 ml: 10 ml amp. 5, 10 or 25 pcs.

Dosage Form, Packaging, and Composition

Solution for injection transparent, colorless.

Excipients : sodium chloride – 8.6 mg, sodium hydroxide solution 2M and/or hydrochloric acid solution 2M to pH 4.0-6.0, water for injection – up to 1 ml.

10 ml – polyethylene ampoules (5), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (10), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (25), connected in cassettes – cardboard packs.

Solution for injection transparent, colorless.

Excipients : sodium chloride – 8 mg, sodium hydroxide solution 2M and/or hydrochloric acid solution 2M to pH 4.0-6.0, water for injection – up to 1 ml.

10 ml – polyethylene ampoules (5), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (10), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (25), connected in cassettes – cardboard packs.

Solution for injection transparent, colorless.

Excipients : sodium chloride – 7.5 mg, sodium hydroxide solution 2M and/or hydrochloric acid solution 2M to pH 4.0-6.0, water for injection – up to 1 ml.

10 ml – polyethylene ampoules (5), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (10), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (25), connected in cassettes – cardboard packs.

Solution for injection transparent, colorless.

Excipients : sodium chloride – 7.1 mg, sodium hydroxide solution 2M and/or hydrochloric acid solution 2M to pH 4.0-6.0, water for injection – up to 1 ml.

10 ml – polyethylene ampoules (5), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (10), connected in cassettes – cardboard packs.
10 ml – polyethylene ampoules (25), connected in cassettes – cardboard packs.

Clinical-Pharmacological Group

Local anesthetic

Pharmacotherapeutic Group

Local anesthetic agent

Pharmacological Action

It is a local anesthetic of the amide type. It causes anesthesia and has an analgesic effect. In high doses, it causes surgical anesthesia; in lower doses, it causes sensory blockade with limited non-progressive motor blockade.

The mechanism of action is associated with a reversible decrease in the permeability of the nerve fiber membrane to sodium ions. As a result, the rate of depolarization decreases and the excitation threshold increases, leading to a local blockade of nerve impulses.

At significantly increased doses, it has a depressant effect on the CNS and myocardium (reduces excitability and automaticity, impairs conductivity). Ropivacaine is characterized by a long duration of action. The duration of anesthesia depends on the dose and route of administration but does not depend on the presence of a vasoconstrictor.

Pharmacokinetics

After epidural administration, Ropivacaine is completely absorbed from the epidural space. Absorption is biphasic. The concentration of ropivacaine in blood plasma depends on the dose, route of administration, and vascularity of the injection area.

The pharmacokinetics of ropivacaine are linear; C_max in blood plasma is proportional to the dose.

The V_d of ropivacaine is 47 L. Binding in blood plasma occurs mainly with α₁-acid glycoproteins; the unbound fraction is about 6%.

Prolonged epidural infusion of ropivacaine leads to an increase in the total ropivacaine content in blood plasma, which is due to a postoperative increase in the level of α₁-acid glycoproteins in the blood. However, the concentration of unbound, pharmacologically active ropivacaine changes to a much lesser extent than its total plasma concentration.

It is actively metabolized in the body, mainly by hydroxylation. The main metabolite is 3-hydroxy-Ropivacaine.

T_1/2 in the initial and terminal phases is 14 min and 4 h, respectively. Total plasma clearance is 440 ml/min. After IV administration, about 86% of the dose is excreted in the urine, mainly as metabolites, and only about 1% of the dose is excreted unchanged in the urine. About 37% of 3-hydroxy-ropivacaine is excreted in the urine, mainly as conjugates.

Indications

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

Relief of acute pain syndrome: prolonged epidural infusion or intermittent bolus administration, for example, for postoperative pain relief or labor analgesia; blockade of individual nerves and local infiltration anesthesia.

ICD codes

Dosage Regimen

Determine the dosage individually based on the surgical procedure, anesthesia technique, and the patient’s physical status and cardiac condition.

For epidural anesthesia in lumbar region for surgery, administer 15 to 20 mL of the 7.5 mg/mL solution. For cesarean section, administer a 20 to 30 mL total volume of the 7.5 mg/mL solution.

For major nerve block such as brachial plexus, administer 30 to 40 mL of the 7.5 mg/mL solution. The onset of surgical anesthesia typically occurs within 10 to 25 minutes.

For labor analgesia via lumbar epidural, administer an initial dose of 10 to 20 mL of the 2 mg/mL solution. For continuous infusion or intermittent bolus, use 10 to 15 mL/hour of the 2 mg/mL solution.

For postoperative pain management, initiate epidural infusion at 6 to 10 mL/hour of the 2 mg/mL solution. Adjust the infusion rate based on the patient’s analgesic response and vital signs.

For field block and infiltration anesthesia, use doses up to 150 mg of the 2 mg/mL or 5 mg/mL solution. The maximum recommended dose is 200 mg for a single administration.

Reduce dosage for elderly or debilitated patients and those with severe hepatic impairment or chronic renal failure with acidosis. Monitor for signs of systemic toxicity.

Always use the lowest effective dose and lowest effective concentration to achieve the desired anesthetic or analgesic effect.

Adverse Reactions

Allergic reactions skin manifestations, anaphylactic shock.

Most side effects occurring during anesthesia are associated not with the effect of the anesthetic used, but with the technique of performing regional anesthesia. The following adverse effects were most frequently (more than 1%) noted and were considered clinically significant regardless of whether a causal relationship with the use of the anesthetic was established.

Cardiovascular system arterial hypertension, arterial hypotension, bradycardia, tachycardia.

Digestive system nausea, vomiting.

Central and peripheral nervous system headache, dizziness, paresthesia.

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

Other increased body temperature, chills, urinary retention.

Contraindications

Children under 12 years of age, hypersensitivity to local anesthetics of the amide type.

Use in Pregnancy and Lactation

Use during pregnancy is possible in cases where the potential benefit of therapy for the mother outweighs the existing risk to the fetus. There is data on the absence of negative effects when using ropivacaine in obstetrics for anesthesia or analgesia. Ropivacaine penetrates the placental barrier well. Binding to plasma proteins in the fetus is lower than in the mother.

If use during lactation is necessary, it should be taken into account that Ropivacaine is excreted in breast milk in small amounts.

Use in Hepatic Impairment

Ropivacaine should be administered with caution to patients with progressive liver cirrhosis. In patients with severe liver diseases, due to impaired elimination, it may be necessary to reduce the dose of ropivacaine with repeated administrations.

Use in Renal Impairment

Ropivacaine should be administered with caution to patients with significant renal impairment. Usually, in patients with renal impairment, no dose adjustment is required for single administration or short-term infusion. However, acidosis and hypoproteinemia are often observed in chronic renal failure, which increases the risk of systemic toxic effects of ropivacaine. In such cases, the doses of ropivacaine should be reduced.

Pediatric Use

Contraindicated in children under 12 years of age.

Special Precautions

The procedure of regional anesthesia should be performed by an experienced specialist with the availability of equipment and medications for resuscitation. IV catheters should be placed before performing major blocks.

Ropivacaine should be administered with caution to patients with severe concomitant diseases (including partial or complete heart block, progressive liver cirrhosis, significant renal impairment). To reduce the risk of developing severe side effects, pre-treatment of concomitant diseases before performing major blocks, as well as adjustment of the anesthetic dose used, is necessary. In patients with severe liver diseases, due to impaired elimination, it may be necessary to reduce the dose of ropivacaine with repeated administrations. Usually, in patients with renal impairment, no dose adjustment is required for single administration or short-term infusion. However, acidosis and hypoproteinemia are often observed in chronic renal failure, which increases the risk of systemic toxic effects of ropivacaine. In such cases, the doses of ropivacaine should be reduced.

Accidental intravascular injection of ropivacaine may lead to the development of intoxication symptoms, appearing immediately or after a delay.

Effect on ability to drive vehicles and operate machinery

The use of ropivacaine may lead to temporary impairment of motor functions, coordination of movements, and speed of psychomotor reactions. The period of time after which one can engage in potentially hazardous activities requiring increased attention is determined individually.

Drug Interactions

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

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.