Universal reference book for medicines
Name of the drug: NAROPIN ® (NAROPIN ® )

Active substance: ropivacaine

Type: Local anesthetic

Manufacturer: ASTRAZENECA (Sweden)
Composition, form of production and packaging
Solution for injections is
transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 2 mg 20 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

10 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

Solution for injections is transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 2 mg 40 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

20 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

Solution for injections is transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 7.5 mg 75 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

10 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

Solution for injections is transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 7.5 mg 150 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

20 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

Solution for injections is transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 10 mg 100 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

10 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

Solution for injections is transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 10 mg 200 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

20 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

Solution for injections is transparent, colorless.

1 ml 1 contact.

ropivacaine hydrochloride 2 mg 200 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

100 ml - polypropylene containers.

Solution for injections is transparent, colorless.

1 ml 1 contact.

ropivacaine hydrochloride 2 mg 400 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

200 ml - polypropylene containers.

Solution for injections is transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 5 mg 100 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

20 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

Solution for injections is transparent, colorless.

1 ml of 1 amp.

ropivacaine hydrochloride 5 mg 50 mg

Excipients: sodium chloride, hydrochloric acid or sodium hydroxide (up to pH 4-6), water d / u.

10 ml - plastic ampoules (5) - packings, cell planimetric (1) - cardboard boxes.

INSTRUCTION FOR THE SPECIALIST.

The description of the drug was approved by the manufacturer for the 2006 print edition.

PHARMACHOLOGIC EFFECT

Local anesthetic of amide type of long-acting.
Reversibly blocks voltage-dependent sodium channels and, thus, prevents generation of pulses in the endings of the sensory nerves and impulses along nerve fibers.
The duration of action depends on the route of administration and the dose of the drug.

PHARMACOKINETICS

Suction

After administration, ropivacaine is completely absorbed from the epidural space.
Absorption is biphasic in nature. The concentration of ropivacaine in the blood plasma depends on the dose, the route of administration and the vascularization of the injection site. The pharmacokinetics of ropivacaine is linear, C max isproportional to the administered dose.
Distribution

pKa of ropivacaine is 8.1;
the partition coefficient is 141 (n-octanol / phosphate buffer pH 7.4).
V d is 47 liters.
The average value of hepatic extraction obtained in the experiment is 0.4. Ropivacaine binds in the blood plasma mainly with? 1- acid glycoproteins, unbound fraction - about 6%.
Long-term epidural administration of ropivacaine leads to an increase in the total content of ropivacaine in the blood plasma, which is due to a postoperative increase in the level?
1- acid glycoproteins in the blood. At the same time, the concentration of unbound, pharmacologically active, form of ropivacaine in blood plasma changes to a much lesser degree than the total concentration.
Ropivacaine passes through the placental barrier well.
Binding to blood plasma proteins in the fetus is lower than that of the mother.
Metabolism

It is actively biotransformed in the body, mainly by hydroxylation.
The main metabolite is 3-hydroxy-ropivacaine.
Excretion

T 1/2 has a two-phase character and is 14 min (? -phase) and 4 h (? -phase).
The total plasma clearance is 440 ml / min. After IV introduction, about 86% of the dose is excreted in the urine, mainly in the form of 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 in conjugated form.
INDICATIONS

Anesthesia during surgical interventions:

- epidural block during surgical interventions, including cesarean section;

- blockade of large nerves and nerve plexuses;

- blockade of individual nerves and local infiltration anesthesia.

Kupirovanie acute pain syndrome:

- a prolonged epidural infusion or a periodic bolus injection, for example to eliminate postoperative pain or anesthetic delivery;

- blockade of individual nerves and local infiltration anesthesia.

DOSING MODE

Before conducting anesthesia, it is necessary to assess the general and physical condition of the patient for choosing the optimal dose of the drug.

For adult doses, recommended for the most common blockade, are listed in the table.
In general, higher doses of the preparation and more concentrated solutions are required for anesthesia in surgical interventions (for example, with epidural administration); for analgesia (eg, epidural for relief of acute pain syndrome), it is recommended to use lower doses and drug concentrations.
Anesthesia during surgical interventions

Concentration of the preparation (mg / ml) Volume of the solution (ml) Dose (mg) Onset (min) Duration of action (h)

Epidural anesthesia at the lumbar level:

surgical interventions

7.5 15-25 113-188 10-20 3-5

10 15-20 150-200 10-20 4-6

cesarean section

7.5 15-20 113-150 10-20 3-5

Epidural anesthesia at the thoracic level:

for example, postoperative pain blockade

7.5 5-15 38-113 10-20 -

Blockade of major plexus:

for example, blockade of the brachial plexus

7.5 10-40 75-300 10-25 6-10

Conducting and infiltration anesthesia:

7.5 1-30 7.5-225 1-15 2-6

Coping with acute pain syndrome

Concentration of the preparation (mg / ml) Volume of the solution (ml) Dose (mg) Onset (min) Duration of action (h)

Epidural introduction at the lumbar level:

bolus administration

2.0 10-20 20-40 10-15 0.5-1.5

multiple administration (for example, for analgesia of childbirth), a minimum interval of 30 minutes

2.0 10-15 20-30 - -

Extended infusion for analgesia of delivery

2.0 6-10 ml / h 12-20 mg / h - -

prolonged infusion for postoperative analgesia

2.0 6-14 ml / h 12-28 mg / h - -

Epidural introduction at the thoracic level:

prolonged infusion (for example, for postoperative analgesia)

2.0 6-14 ml / h 12-28 mg / h - -

Conducting blockade and infiltration:

2.0 1-100 2-200 1-5 2-6

The doses indicated in the table are considered sufficient to perform a reliable blockade in adults, but the tabular data are indicative (because there is an individual variability in the rate of development of the block and its duration).

Prior to administration and at the time of drug administration (which should be done slowly or by increasing sequentially administered doses at a rate of 25-50 mg / min), a suction probe should be carefully performed to prevent the solution from entering the vessel.
A random intravascular injection is recognized by an increase in heart rate, and a random intrathecal injection on the grounds of a spinal block. When symptoms of intoxication appear, discontinue the drug immediately. When epidural blockade during surgery, a single injection of ropivacaine in a dose of up to 250 mg is usually well tolerated.
When prolonged blockade is carried out by prolonged infusion or repeated bolus administration, the possibility of creating toxic concentrations of anesthetic in the blood and local nerve damage should be considered.

It was found that the total dose of 800 mg of ropivacaine obtained within 24 hours, as well as prolonged epidural infusion at a rate of 28 mg / h for 72 hours, is well tolerated by adults.

For the relief of postoperative pain , the following scheme of drug use is recommended: if the epidural catheter was not installed during surgery, then after its installation, the epidural blockade with Naropin (7.5 mg / ml) is performed.
Analgesia is maintained by the infusion of Naropin (2 mg / ml). Infusion at a rate of 6-14 ml / h (12-28 mg / h) provides adequate analgesia with a minor and non-progressive motor blockade. This technique significantly reduces the need for opioid analgesics. Clinical studies have shown that for postoperative analgesia, epidural infusion of Naropin (2 mg / ml) without fentanyl or mixed with it (1-4 μg / ml) can be performed continuously for 72 hours. In the latter case, the appearance of effects associated with with stimulation of opioid receptors.
The use of Naropin at concentrations above 7.5 mg / ml in cesarean section has not been documented.

SIDE EFFECT

Allergic reactions: skin reactions, 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 (> 1%), the following adverse effects were noted, which were regarded as having clinical significance, regardless of whether a cause-effect relationship was established with the use of an anesthetic.
From the cardiovascular system: arterial hypertension, arterial hypotension, bradycardia, tachycardia.

From the digestive system: nausea, vomiting.

From the central nervous system 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, rather than with the action of the drug.

Other: fever, chills, urinary retention.

The profile of side effects with Naropin is similar to that of other local anesthetics of the amide type.
With proper use of the drug side effects are very rare.
CONTRAINDICATIONS

- Hypersensitivity to local anesthetics of the amide type.

PREGNANCY AND LACTATION

Naropin can be used during pregnancy only if it is justified by the clinical situation.
However, in obstetrics, the use of the drug for anesthesia or analgesia is well justified.
Ropivacaine in a small amount can penetrate into breast milk, which should be considered when it is necessary to use the drug during lactation (breastfeeding).

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution should be administered to patients with significant impairment of kidney function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Caution should be given to patients with severe progressive cirrhosis of the liver.

APPLICATION FOR CHILDREN

It is not recommended to use Naropin in children under the age of 12 due to the lack of sufficient clinical observations.

SPECIAL INSTRUCTIONS

The procedure for regional anesthesia should be carried out by experienced specialists.
It is necessary to have equipment and medicines for resuscitation. Before the beginning of the execution of large blockades should be installed in / in the catheters.
With caution, the drug should be administered to 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, the drug should be used with caution; in some cases, due to a violation of elimination, it may be necessary to reduce doses with repeated administration of the drug. Typically, patients with impaired renal function with a single injection of the drug or with a short-term infusion do not need a dose adjustment. However, acidosis, often developing in patients with chronic renal failure, and a decrease in plasma protein concentration may increase the risk of systemic toxic effects of the drug. In such cases, the dose of the drug should be reduced.
Use in Pediatrics

It is not recommended to use Naropin in children under the age of 12 due to the lack of sufficient clinical observations.

Impact on the ability to drive vehicles and manage mechanisms

The use of Naropin 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.

OVERDOSE

Symptoms: a random intravascular injection of an anesthetic can cause symptoms of intoxication, manifested immediately or in a delayed period.

The ingestion of excessive amounts of the drug in the systemic blood stream exerts a depressing effect on the central nervous system and myocardium (reduces excitability and automatism, impairs conductivity).

Neurological manifestations are discrete.
First, there are disorders of vision and hearing, dysarthria, increased muscle tone, muscle twitching. With the progression of intoxication, loss of consciousness, seizures of a duration from a few seconds to several minutes, which is accompanied by the rapid development of hypoxia and hypercapnia and respiratory failure, up to its stop in severe cases, are possible. Respiratory and metabolic acidosis potentiate the toxic effects of anesthetic.
Subsequently, due to the redistribution of the anesthetic from the central nervous system and its subsequent metabolism and excretion, restoration of functions takes place, which can occur quite quickly, unless the drug has been administered in a high dose.

Violations of the function of the cardiovascular system in the form of arterial hypotension and arrhythmia usually follow the initial manifestations of neurologic disorders, unless the patient is under general anesthesia or there was a premedication with benzodiazepines or barbiturates.

Treatment: when the first signs of systemic intoxication should immediately stop the drug.
When convulsions should be maintained adequate intake of oxygen through a bag or mask. If convulsions do not stop after 15-20 sec, anticonvulsants (IV 100-120 mg of thiopental or 5-10 mg of diazepam should be used, suxamethonium can be administered after intubation and the onset of mechanical ventilation). When oppression of the cardiovascular system (arterial hypotension, bradycardia), it is necessary to inject iv ephedrine in a dose of 5-10 mg, if necessary, repeat the introduction 2-3 minutes later. When cardiac arrest, standard resuscitation should be performed. It is necessary to maintain optimal gas composition of blood with simultaneous correction of acidosis.
DRUG INTERACTION

With the simultaneous use of Naropin with other local anesthetics or drugs structurally similar to local anesthetics of the amide type, toxic effects can be summarized.

Pharmaceutical interaction

Raising the pH of the solution above 6.0 can lead to the formation of precipitate due to the poor solubility of ropivacaine under these conditions.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored at a temperature of no higher than 30 ° C;
Do not freeze. Shelf life of the drug in plastic ampoules - 3 years, in plastic infusion bags - 2 years.
Conditions of leave from pharmacies

The drug is released by prescription.

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