Index of drugs

To obtain local anesthesia by peripheral nerve blockage and central nerve block (equine or epidural anesthesia), ie for specialist applications in situations requiring prolonged anesthesia. The drug is also indicated for reducing pains.

1 ml contains 2.5 mg or 5 mg bupivacaine hydrochloride. The drug contains sodium (3.15 mg / ml sodium).

Bupivacaine is a potent local amide anesthetic with long-term action. It affects the sensory nerves more than the motor nerves and is ideal for inducing anesthesia without movement blockage. Ultimate T in adults_0,5 bupivacaine is 3.5 h. C_max depends on the injection site and is the largest after intercostal nerve blockage. However, the total dose of the drug, not its concentration, is an important parameter determining the maximum concentration of the drug in the blood. Bupivacaine breaks down in the liver and only 6% are excreted unchanged with urine.

Hypersensitivity to bupivacaine hydrochloride, topical anesthetic agents or to any of the excipients. Do not use in regional intravenous anesthesia (Biera block) and for perinatal blockade in obstetrics. Contraindications for subarachnoid anesthesia: active diseases o.u.n. with acute course (i.e. meningitis, tumors, Heinrich-Medin's disease) and intracranial haemorrhage; narrowing of the spinal canal and active spine disease (eg spondylitis, tuberculosis, tumors) or recent traumatic events (eg fractures); sepsis; pernicious anemia with sub-acute course of bone marrow degeneration; skin infection with pyogenic germs at the injection site or in its environment; cardiac or oligolemic shock; coagulation disorders or currently used anticoagulant therapy.

There are cases of cardiac arrest when bupivacaine is used for epidural anesthesia or peripheral nerve blockage, in which resuscitation turned out to be difficult and lasted longer before the patient responded to it. Like all local anesthetics, bupivacaine used for local anesthetic treatments that lead to high blood levels of the drug may cause symptoms of acute poisoning by o.u.n. and circulatory system. This is especially the case if a mistakenly administered intravascularly. Due to the high concentrations of bupivacaine in the systemic circulation, there have been cases such as ventricular arrhythmia, ventricular fibrillation, sudden circulatory collapse and death. Blockages of larger peripheral nerves may require large volumes of local anesthetics in heavily vascularized places often near large vessels, which increases the risk of intravascular and / or systemic absorption. Repeated injection of bupivacaine hydrochloride may cause a significant increase in blood levels with each subsequent dosing, due to the slow accumulation of the drug. Tolerance varies depending on the patient's condition. Patients who are depleted, elderly or have an acute illness should receive doses that are reduced according to their physical condition. Patients treated with Class III anti-arrhythmic agents (such as amiodarone) should be under special supervision and ECG monitoring should be performed because adverse effects on the heart may accumulate (additive effect). The local anesthetics should be used with caution for epidural anesthesia in patients with reduced cardiovascular capacity, as they may have poorer ability to compensate for functional changes associated with prolonged AV conduction caused by these drugs. Caution should be exercised in patients with liver disease or who have reduced liver blood flow.In patients with hypovolaemia, regardless of its cause, a severe and severe pressure drop may occur during subarachnoid anesthesia. Therefore, patients with untreated hypovolaemia or severely weakened venous return to the heart should avoid using epidural anesthesia or use them with caution. Epidural anesthesia with any local anesthetic can cause hypotension and bradycardia, what to expect and take appropriate measures. From these agents, mention may be made of the prior administration of a crystalloids or colloids to the blood stream. If the pressure drops, they should be treated with a booster, such as ephedrine at a dose of 10-15 mg, given intravenously. A deep reduction in blood pressure may result from hypovolaemia due to hemorrhage or dehydration or closure of the main artery and vena cava in patients with great ascites, large tumors in the abdomen or in advanced pregnancy. Significant reduction in blood pressure should be avoided in patients with heart failure. In patients with hypovolaemia with any aetiology during the introduction of epidural anesthesia there may be a rapid and strong reduction in pressure. Epidural anesthesia can cause intercostal nerve paralysis, and patients with pleural effusion may suffer from respiratory problems. Sepsis may increase the risk of intra-spinal abscess in the post-operative period. Low doses of local anesthetics injected into the head and neck, including retrobulbar, periontial anesthesia and stellate plexus blockade, may induce systemic toxicity due to inadvertent intra-arterial injection. In rare cases, extraocular injections can reach the subarachnoid space, causing serious reactions, including transient blindness, circulatory collapse, apnea, convulsions. Intra- and periocular injection of local anesthetics carries a small risk of permanent impairment of ocular muscles. The main causes are the injury and / or local effects of muscle and / or nerve toxicity. The severity of this type of tissue reaction depends on the severity of the injury, the concentration of the local anesthetic and the duration of the local anesthetic effect on the tissue. For this reason, as with all local anesthetics, the lowest effective concentration and dose of local anesthetic should be used. Exercise caution when injecting anesthetics into inflammatory or infected areas. 1 ml of solution contains 3.15 mg (0.14 mmol) of sodium, which should be taken into account for patients on a controlled sodium diet.

Do not use bupivacaine for injections during pregnancy unless the expected benefits outweigh the risks. There is little data on the use of bupivacaine in pregnant women. Animal studies have shown reduced survival of the offspring and embryotoxic effects. Bupivacaine in the form of a solution is contraindicated for use in perinatal blockades in obstetrics (risk of bradycardia in the fetus). Bupivacaine passes into breast milk, but in such small amounts that there is no risk to the child in the therapeutic dose range.

Very often: nausea, hypotension. Common: paraesthesia, dizziness; bradycardia; hypertension; vomiting; urinary retention. Uncommon: toxic effects from o.u.n. (convulsions, paresthesia around the mouth, numbness of the tongue, increased hearing acuity, blurred vision, loss of consciousness, trembling of the extremities, a feeling of emptiness in the head, tinnitus, dysarthria). Rare: allergic reactions, anaphylactic shock; neuropathy, damage to the peripheral nerve, arachnoiditis; double vision; cardiac arrest, arrhythmias; respiratory depression.

The dosage depends on the area to be anesthetized, tissue vasculature, the number of neuronal segments to be blocked, individual tolerability and the method of anesthesia used. The maximum dose should be determined by assessing the patient's weight and physical condition, and taking into account the expected rate of systemic absorption from a specific injection site.Experience to date suggests that a single dose up to 150 mg of bupivacaine hydrochloride is the appropriate dose. Then doses up to 50 mg can be administered every 2 hours. The maximum dose of 2 mg / kg should not be exceeded in a four-hour period. When using long-term anesthesia, whether by continuous infusion or by repeatedly administering the drug in the whole dose once (in a bolus), the risk of toxic concentration in the plasma or induction of local nerve damage should be considered.Adults.  Surgical anesthesia. Intraluminal administration for epidural anesthesia (dose includes a test dose): surgical operation, caesarean section - 15-30 ml of solution at a concentration of 5 mg / ml.Doppler administration for epidural anesthesia (dose includes a test dose): surgery - 5-15 ml of solution with conc. 2.5 mg / ml or 5-10 ml of solution with conc. 5 mg / ml.Epidural anesthesia of the equine tail (dose includes the test dose): 20-30 ml of solution with conc. 2.5 mg / ml or 5 mg / ml.Block more nerves (dose should be adjusted depending on the place of administration and the patient's condition): 10-35 ml of solution with conc. 5 mg / ml.Auxiliary anesthesia of the operating field (e.g. small nerve blockages): <60 ml of solution with a concentration of 2.5 mg / ml or ≤ 30 ml with conc. 5 mg / ml.Fighting acute pain. Administration of the lumbar drug for epidural anesthesia: periodic injections (e.g., postoperative pain relief) - 6-15 ml (minimum interval 30 min) with conc. 2.5 mg / ml (in total ≤500 mg / 24 h);continuous infusion - 5-7,5 ml (per hour) of solution with conc. 2.5 mg / ml (the drug is often used for epidural administration together with the appropriate opioid, total dose ≤500 mg / 24 h).Doppler administration for epidural anesthesia: continuous infusion - 4-7.5 ml (per hour) solution with conc. 2.5 mg / ml.Delivery anesthesia (eg after colonoscopy): ≤40 ml of solution with conc. 2.5 mg / ml (if bupivacaine is additionally introduced by any other method in the same patient, a total dose of 150 mg should not be exceeded).Auxiliary anesthesia around the operating field (eg small nerve blockages): ≤60 ml of solution with conc. 2.5 mg / ml. The doses given above should be reduced in young, elderly or poor patients.Children 1-12 years old. Relief of acute pain (pre- and post-operative): epididymal tract administration, lumbar epidural administration, intrathecal epidural administration - 0.6-0.8 ml dil. with conc. 2.5 mg / ml. In children of high body weight, there is often a need to gradually reduce the dose based on ideal body weight. In children, the dose (up to 2 mg / kg) should be calculated based on body weight.
In order to avoid intravascular injection, the aspiration of air should be repeated frequently before and during the main dose, and the main dose should be injected slowly or in small portions at a rate of 25-50 mg / min. During the procedure, the vital functions of the patient should be closely observed, with whom verbal contact should be maintained. Before the injection of the dose for epidural anesthesia, a test dose of 3-5 ml of bupivacaine with the addition of adrenaline is recommended.