Vopicain

Vopicain 0.5% Injection: Each mL contains: Levobupivacaine HCl 5.9136 mg equivalent to: Levobupivacaine 5 mg.

Pharmacology: Mechanism of Action: Vopicain is a member of the amino amide class of local anesthetics. Local anesthetics block the generation and the conduction of nerve impulses by increasing the threshold for electrical excitation in the nerve, by slowing propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers.
Pharmacodynamics: Vopicain can be expected to share the pharmacodynamic properties of other local anesthetics. Systemic absorption of local anesthetics can produce effects on the central nervous and cardiovascular systems. At blood concentrations achieved with therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance have been reported. Toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block, ventricular arrhythmias, and cardiac arrest, sometimes resulting in death. In addition, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure.
Following systemic absorption, local anesthetics can produce central nervous system stimulation, depression, or both. Apparent central nervous system stimulation is usually manifested as restlessness, tremors, and shivering, progressing to convulsions. Ultimately central nervous system depression may progress to coma and cardio-respiratory arrest. However, the local anesthetics have a primary depressant effect on the medulla and on higher centers. The depressed stage may occur without a prior excited stage.

Vopicain is indicated for Surgical Anesthesia: Epidural, peripheral neural blockade; and local infiltration. Pain Management: continuous epidural infusion for continuous epidural analgesia. Vopicain may be administered in combination with epidural fentanyl or clonidine.

The rapid injection of a large volume of local anesthetic solution should be avoided and fractional (incremental) doses should always be used. The smallest dose and concentration required to produce the desired result should be administered. The dose of any local anesthetic differs with the anesthetic procedure, the area to be anesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked, the intensity of the block, the degree of muscle relaxation required, the duration of the anesthesia desired, individual tolerance, and the physical condition of the patient. Patients in poor general condition due to aging or other compromising factors such as impaired cardiovascular function, advanced liver disease, or severe renal dysfunction, require special attention.
To reduce the risk of potentially serious adverse reactions, attempts should be made to optimize the patient's condition before major blocks are performed, and the dosage should be adjusted accordingly. Use an adequate test dose (3-5 mL) of a short-acting local anesthetic solution containing epinephrine prior to induction of complete nerve block. This test dose should be repeated if the patient is moved in such a fashion as to have displaced the epidural catheter. It is recommended that adequate time be allowed for the onset of anesthesia following administration of each test dose. Disinfecting agents containing heavy metals, which cause release of ions (mercury, zinc, copper, etc.), should not be used for skin or mucous membrane disinfection since they have been related to incidents of swelling and edema.
When chemical disinfection of the container surface is desired, either isopropyl alcohol (91%) or ethyl alcohol (70%) is recommended. It is recommended that chemical disinfection be accomplished by wiping the vial stopper thoroughly with cotton or gauze that has been moistened with the recommended alcohol just prior to use.


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The doses in the table are those considered to be necessary to produce a successful block and should be regarded as guidelines for use in adults. Individual variations in onset and duration occur.
Epidural doses of up to 375 mg have been administered incrementally to patients during a surgical procedure.
The maximum dose in 24 hours for intraoperative block and post-operative pain management was 695 mg.
The maximum dose administered as a post-operative epidural infusion over 24 hours was 570 mg.
The maximum dose administered to patients as a single fractionated injection was 300 mg.

Acute emergencies from local anesthetics are generally related to high plasma levels or high dermatomal levels ("high spinal") encountered during therapeutic use of local anesthetics or to unintended intrathecal or intravascular injection of local anesthetic solution (see Adverse Reactions, Warnings, and Precautions). There was one case of suspected unintentional intravascular injection which occurred. That patient received 19 mL of 0.75% Levobupivacaine (147.5 mg) and experienced CNS excitation which was treated with thiopental. No abnormal cardiovascular changes were observed and the patient recovered without sequelae.
Management of Local Anesthetic Emergencies: The first consideration is prevention, best accomplished by incremental injection of Vopicain, careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness after each local anesthetic injection and during continuous infusion. At the first sign of change, oxygen should be administered. The first step in the management of systemic toxic reactions, as well as under-ventilation or apnea due to unintentional subarachnoid injection of drug solution, consists of immediate attention to the establishment and maintenance of a patient airway and effective assisted or controlled ventilation with 100% oxygen with a delivery system capable of permitting immediate positive airway pressure by mask. This may prevent convulsions if they have not already occured.
If necessary, use drugs to control convulsions. Intravenous barbiturates, anti-convulsant agents, or muscle relaxants should only be administered by those familiar with their use. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should be evaluated. Supportive treatment of circulatory depression may require administration of intravenous fluids, and when appropriate, a vasopressor dictated by the clinical situation (such as ephedrine or epinephrine to enhance myocardial contractile force).
If difficulty is encountered in the maintenance of a patient airway or if prolonged ventilatory support (assisted or controlled) is indicated, endotracheal intubation, employing drugs and techniques familiar to the clinician, may be indicated after initial administration of oxygen by mask. The supine position is dangerous in pregnant women at term because of aortocaval compression by the gravid uterus. Therefore, during treatment of systemic toxicity, maternal hypotension or fetal bradycardia following regional block, the parturient should be maintained in the left lateral decubitus position if possible, or manual displacement of the uterus off the great vessels should be accomplished. Resuscitation of obstetrical patients may take longer than resuscitation of non-pregnant patients and closed-chest cardiac compression may be ineffective. Rapid delivery of the fetus may improve the response to resuscitation efforts.

Vopicain is contraindicated in patients with a known hypersensitivity to vopicain or to any local anesthetic agent of the amide type; Vopicain solutions are contraindicated in patients with severe hypotension such as cardiogenic or hypovolaemic shock. Contraindication for use in Bier Block, paracervical block, and 0.75% Vopicain use in obstetric procedure. Vopicain also should not be used for intravenous regional anesthesia (i.e Bier Block).

In performing Vopicain blocks, unintended intravenous injection is possible and may result in cardiac arrest. Despite rapid detection and appropriate treatment, prolonged resuscitation may be required. The resuscitability relative to bupivacaine is unknown at this point in time as it has not been studied. As with all local anesthetics of the amide type, Vopicain should be administered in incremental doses. Since Vopicain should not be injected rapidly in large doses, it is not recommended for emergency situations, where a fast onset of surgical anesthesia is necessary.
Historically, pregnant patients were reported to have a high risk for cardiac/circulatory arrest, and death when bupivacaine was inadvertently rapidly injected intravenously. Avoid 0.75% Vopicain in obstetrical patients. This concentration is indicated only for non-obstetrical surgery requiring profound muscle relaxation and long duration. For cesarean section, the 5 mg/mL (0.5%) Vopicain solution in doses up to 150 mg is recommended.
Local anesthetics should only be administered by clinicians who are well versed in the diagnosis and management of drug-related toxicity and other acute emergencies which might arise from the block being administered. The immediate availability of oxygen, other resuscitative drugs, cardiopulmonary resuscitative equipment, and the personnel resourcer needed for proper management of toxic reaction and related emergencies must be ensured (see Adverse Reactions and Precautions). Delay in proper management of drug-related toxicity, underventilation from any cause, and/or altered sensitivity may lead to the development of acidosis, cardiac arrest, and possibly death.
Solutions of Vopicain should not be used for the production of obstetrical paracervical block anesthesia. There are no data to support such use and there is the additional risk of fetal bradycardia and death.
Intravenous regional anesthesia (Bier Block) should not be performed using Vopicain because of the lack of clinical experience and the risk of attaining toxic blood levels of levobupivacaine.
It is essential that aspiration for blood or cerebrospinal fluid (where applicable), be done prior to injecting any local anesthetic, both before the original dose and all subsequent doses, to avoid intravascular or intrathecal injection. However, a negative aspiration does not ensure against intravascular or intrathecal injection. Vopicain should be used with caution in patients receiving other local anesthetics or agents structurally related to amide-type local anesthetics, since the toxic effects of these drugs are additive.
When contemplating a peripheral nerve block, where large volumes of local anesthetic are needed, caution should be exercised when using the higher mg/mL concentrations of Vopicain. Animal studies demonstrate CNS and cardiac toxicity that is dose related, thus equal volumes of higher concentration will be more likely to produce cardiac toxicity.

General: The safe and effective use of local anesthetics depends on proper dosage, correct technique, adequate precautions, and readiness for emergencies. Resuscitative equipment, oxygen and resuscitative drugs should be available for immediate use (see Warnings and Adverse Reactions). The lowest dosage that results in effective anesthesia should be used to avoid high plasma or dermatomal levels and serious adverse effects. Injections should be made slowly and incrementally, with frequent aspirations before and during the injection to avoid intravascular injection. When a continuous catheter technique is used, syringe aspirations should also be performed before and during each supplemental injection. During the administration of epidural anesthesia, it is recommended that a test dose of a local anesthetic with a fast onset be administered initially and that the patient be monitored for central nervous system and cardiovascular toxicity, as well as for signs of unintended intrathecel administration before proceeding. When clinical conditions permit, consideration should be given to employing local anesthetic solutions that contain epinephrine for the test dose because circulatory changes compatible with epinephrine may also serve as a warning sign of unintended intravascular injection. An intravascular injection is still possible even if aspirations for blood are negative.
Injection of repeated doses of local anesthetics may cause significant increases in plasma levels with each repeated dose due to slow accumulation of the drug or its metabolites or to slow metabolic degradation. Tolerance to elevated blood levels varies with the physical condition of the patient. Local anesthetics should also be used with caution in patients with hypotension, hypovolemia, or impaired cardiovascular function, especially heart block.
Careful and constant monitoring of cardiovascular and respiratory vital signs (adequacy of ventilation) and the patient's state of consciousness should be performed after each local anesthetic injection. The clinician must be aware that restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, tinnitus, dizziness, blurred vision, tremors, twitching, depression, or drowsiness may be early warning signs of central nervous system toxicity. Amide-type local anesthetics such as Vopicain are metabolized by the liver, therefore these drugs, especially repeat doses, should be used cautiously in patient with hepatic disease. Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at a greater risk for developing toxic plasma concentrations. Local anesthetics should also be used with caution in patients with impaired cardiovascular functions they may be less able to compensate for functional changes associated with prolonged A-V conduction caused by these drugs.
Many drugs used during the conduct of anesthesia are considered potential triggering agents for malignant hyperthermia. Amide-type local anesthetics are not known to trigger this reaction.
Epidural Anesthesia: During epidural administration, Vopicain should be administered in incremental volumes of 3 to 5 mL with sufficient time between doses to detect toxic manifestations of unintentional intravascular or intrathecal injection. Syringe aspirations should also be performed before and during each supplemental injection in continuous catheter techniques. An intravascular injection is still possible even if aspirations for blood are negative. During the administration of epidural anesthesia, it is recommended that a test dose is administered initially and the effects monitored before the full dose is given. A test dose of a short-acting amide anesthetic, such as 3 mL of Lidocaine, is recommended to detect unintentional intrathecal administration. This will be manifested within a few minutes by signs of a subarachnoid block (e.g., decreased sensation of the buttocks, paresis of the legs or, in the sedated patient, absent knee jerk). Unintentional intrathecal injection of local anesthetics can lead to very high spinal anesthesia, possibly apnea, severe hypotension, and loss of consciousness. An intravascular or intrathecal injection is still possible even if the results of the test dose are negative. The test dose itself may produce a systemic toxic reaction, extensive subarachnoid block, or cardiovascular effects.
Use in Head and Neck Area: Small doses of local anesthetics injected into the head and neck area may produce adverse reactions similar to systemic toxicity seen with unintentional intravascular injections of larger doses. The injection procedures require the utmost care. Confusion, convulsions, respiratory depression, and/or respiratory arrest and cardiovascular stimulation or depression have been reported. These reactions may be due to intraarterial injection or the local anesthetic with retrograde flow to the cerebral circulation. Patients receiving these blocks should have their respirations and circulation monitored and be constantly observed. Resuscitative equipment and personnel for treating adverse reactions should be immediately available. Dosage recommendations should not be exceeded (see Dosage & Administration).
Information for Patients: When appropriate, patients should be informed in advance that they may experience temporary loss of sensation and motor activity in the anesthetized part of the body following correct administration of regional anesthesia. Also when appropriate, the physician should discuss other information including adverse reactions in the Vopicain package insert.

Reactions to Vopicain are characteristic of those associated with other amide-type local anesthetics. A major cause of the adverse reactions to this group of drugs is associated with excessive plasma levels, or high dermatomal levels, which may be due to overdose, unintentional intravascular injection, or slow metabolic degradation.
Body as a Whole: asthenia, edema.
Cardiovascular Disorders: General: postural hypotension.
Central and Peripheral Nervous System Disorders: hypokinesia, involuntary muscle contraction, spasm (generalized), tremor, syncope.
Heart Rate and Rhythm Disorders: arrhythmia, extrasystoles, fibrillation (atrial), cardiac arrest.
Gastrointestinal System Disorders: ileus.
Liver and Biliary System Disorders: elevated bilirubin.
Psychiatric Disorders: confusion.
Respiratory System Disorders: apnea, bronchospasm, dyspnea, pulmonary edema, respiratory insufficiency.
Skin and Appendage Disorders: increased sweating, skin discoloration.

Vopicain should be used with caution in patients receiving other local anesthetics or agents structurally related to amide-type local anesthetics since the toxic effects of these drugs could be additive. Vopicain should be used with caution in patients receiving anti-arrhythmic agents with local anesthetics activity e.g, mexilitine, or class III anti-arrhythmic agents since their use may be additive.

Store below 25°C.

Anaesthetics - Local & General

N01BB10 - levobupivacaine ; Belongs to the class of amides. Used as local anesthetics.

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