Ropivacaine Hydrochloride for Injection

Pharmacological action According to literature reports, ropivacaine is the first pure L-acting long-acting amide local anesthetic, which has dual effects of anesthesia and analgesia. Large doses can produce surgical anesthesia, and small doses produce sensory blockade (analgesia) accompanied by only limited non-progressive motor nerve block. The addition of epinephrine does not change the intensity and duration of the blockade of ropivacaine. Ropivacaine produces a reversible blockade of impulse conduction along nerve fibers by blocking the influx of sodium ions into the cell membrane of nerve fibers. Local anesthetics may also have similar effects on excitable cell membranes such as brain cells and myocardial cells. If an excessive amount of the drug enters the systemic circulation rapidly, the central nervous system and cardiovascular system will produce symptoms and signs of poisoning. Pregnant ewes do not show greater sensitivity to ropivacaine than non-pregnant ewes. Healthy volunteers tolerate ropivacaine well after intravenous injection, and clinical experience with this drug suggests a good safety range. Depending on the degree of parasympathetic blockade, epidural use of this drug may cause indirect cardiovascular effects (hypotension, bradycardia). Toxicity studies According to literature reports, ropivacaine hydrochloride will only cause acute toxic reactions when the plasma concentration of the drug rises suddenly due to high doses or accidental injection of the drug into the blood vessels, or in the case of drug overdose (see pharmacological effects and drug overdose). There was a patient who had convulsions after accidentally injecting 200 mg of the drug into the blood vessels during brachial plexus blockade. The two generations of rats tested for reproductive toxicity showed no effects on fertility and general reproductive behavior. After the highest dose of ropivacaine hydrochloride was administered, the number of deaths of pups within three days after delivery increased due to its toxic effects on pregnant mothers, and it was listed as the second cause of neonatal death. Teratogenicity tests on rats and rabbits did not show any adverse effects of ropivacaine on organogenesis and early fetal development. Studies on perinatal and postnatal rats at the maximum tolerable dose did not show any effects on late fetal development, delivery, lactation, neonatal survival, and offspring growth. Another perinatal and postnatal study in rats compared ropivacaine with bupivacaine and found that maternal toxicity was observed at much lower doses and free plasma concentrations of bupivacaine.

Ropivacaine hydrochloride, excipient is lactose

This product is white or off-white loose mass or powder.

Surgical anesthesia, epidural anesthesia, including cesarean section, regional blocks, acute pain control, continuous epidural infusion or intermittent single-dose, such as postoperative or labor analgesia.

Ropivacaine hydrochloride is only for use by clinicians with anesthesia experience or under their guidance. Dissolve it with sodium chloride injection at the required dosage concentration before use. The reference doses of commonly used anesthesia are shown in the table below, or follow the doctor's advice. In general, surgical anesthesia (such as epidural medication) requires higher concentrations and doses. For analgesic medication (such as epidural medication to control acute pain), lower concentrations and doses are recommended. Recommended dose of ropivacaine hydrochloride for injection (see the table below) (Based on the results of animal tests of this product, the concentration of this product should not exceed 7.5 mg/ml) Concentration mg/ml Volume ml Total dose mg Onset time minutes Duration hours Surgical anesthesia Lumbar epidural administration Surgical operation 7.5 15-25 1 13-18 8 10-20 3-5 Caesarean section 7.5 15-20 1 13-150 10-20 3-5 Thoracic epidural administration Postoperative analgesia 7.5 5-15 3 8-11 3 10-20 n/a Regional blockade (such as peripheral nerve block and infiltration anesthesia 7.5 1-30 7.5-22 5 1-15 2-6 Acute pain control Lumbar epidural administration Single dose 2.0 10-20 20-40 10～150.5～1.5Additional dose (sufficient dose) (such as labor analgesia) 2.010～1520～30 (minimum interval 30 minutes)Lumbar epidural continuous infusion (such as labor analgesia and postoperative analgesia) 2.06～14ml/h12～28mg/hn/an/aThoracoscopic epidural continuous infusion (such as postoperative analgesia) 2.04～8ml/h8～16mg/hn/an/aRegional block (such as peripheral nerve block and infiltration anesthesia) 2.01～1002～2001～52～6The doses in the above table are necessary to provide effective anesthesia and can be used as a guide dose for adults. The onset time and duration will vary from person to person. The above data reflects the estimated range of the average dose required. . For other local anesthetic techniques, standard textbooks should be referred to. Before and during injection, careful aspiration should be performed to prevent intravascular injection. When large-dose injection is required, such as epidural anesthesia, a 3-5 ml test dose of lidocaine (2% xylocaine) containing epinephrine is recommended. If injected intravenously by mistake, it may cause a transient increase in heart rate, or if injected into the subarachnoid space by mistake, spinal anesthesia may occur. Before and during the injection of the standard dose, repeated aspiration should be performed and attention should be paid to slow injection or gradually increasing the injection speed (25-50 mg/min). At the same time, the patient's vital signs should be closely observed and the patient should be continuously talked to. If symptoms of poisoning occur, the injection should be stopped immediately. For the treatment of postoperative pain, the following techniques are recommended: If an epidural catheter has been placed before surgery, This tube can be used to administer 7.5 mg/ml of this product for epidural injection. Postoperatively, 2 mg/ml of ropivacaine hydrochloride is used to maintain analgesia. For most moderate to severe postoperative pain, clinical studies have shown that an infusion rate of 6 to 10 ml (12 to 20 mg) per hour can provide effective analgesia with only mild, non-progressive motor blockade. With this technology, the need for opioids has been significantly reduced. Clinical studies have also shown that for patients who require higher doses, an infusion rate of 12 to 14 ml (24 to 28 mg) per hour can also be better tolerated. There is no record of concentrations above 7.5 mg/ml being used for cesarean sections. Clinical experience shows that epidural infusion of ropivacaine hydrochloride injection for up to 24 hours is feasible.

Unexpected Effects Adverse reactions to ropivacaine hydrochloride are similar to those of other long-acting amide local anesthetics. Except for accidental injection into a blood vessel or overdose, adverse reactions to local anesthesia are almost uncommon. They should be distinguished from physiological reactions caused by the blockade of the nerve itself, such as hypotension and bradycardia during epidural anesthesia. Overdose and accidental injection into a blood vessel may cause serious systemic reactions (see OVERDOSE). Allergic reactions Allergic reactions are rare to amide local anesthetics. (The most serious allergic reaction is anaphylactic shock). Acute systemic toxicity Ropivacaine hydrochloride will only cause acute toxic reactions if the dose is too large or the drug is accidentally injected into the blood vessel, causing a sudden increase in the drug plasma concentration or an overdose (see PHARMACOKINETICS AND OVERDOSE).

It is contraindicated for those who are allergic to this product or any of its ingredients or to similar drugs.

Precautions for children: There is currently no research data on this product, and it should not be used in children under 12 years old. Precautions for pregnancy and lactation: There are no clinical trials on the effects of ropivacaine on fetal growth after pregnant women use it, and caution is recommended. There are sufficient experimental reports on the use of ropivacaine as obstetric anesthesia or analgesia during delivery, and no side effects have been observed. Lactation The secretion of ropivacaine or its metabolites in human milk has not been studied. Based on the ratio of milk/plasma concentrations in rat experiments, it is estimated that the daily intake of young rats is 4% of the dose of their mothers. Assuming that the ratio of human milk/plasma concentrations is the same as that of rats, the amount of ropivacaine ingested by breast-fed infants is much lower than the dose received in the pregnant woman's uterus during pregnancy. Precautions for the elderly: See [Usage and Dosage], or follow the doctor's advice.

Because toxic effects are additive, patients receiving other local anesthetics or drugs structurally related to amide local anesthetics should be used with caution if this drug is used concomitantly. Contraindications Ropivacaine is poorly soluble above pH 6.0, so it will precipitate in an alkaline environment.

Store in a cool place (not exceeding 20°C) and sealed for 18 months.

75mg (calculated as C17H26N20·HCl)

24 months