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Carbocaine
Overview
What is Carbocaine?
Mepivacaine hydrochloride is 2-Piperidinecarboxamide, -(2,6-dimethylphenyl)-1-methyl, monohydrochloride and has the following structural formula:
CHNO • HCl
It is a white crystalline odorless powder, soluble in water, but very resistant to both acid and alkaline hydrolysis.
CARBOCAINE is a local anesthetic available as sterile isotonic solutions (clear, colorless) in concentrations of 1%, 1.5%, and 2% for injection via local infiltration, peripheral nerve block, and caudal and lumbar epidural blocks.
Mepivacaine hydrochloride is related chemically and pharmacologically to the amide-type local anesthetics. It contains an amide linkage between the aromatic nucleus and the amino group.
What does Carbocaine look like?
What are the available doses of Carbocaine?
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What should I talk to my health care provider before I take Carbocaine?
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How should I use Carbocaine?
CARBOCAINE is indicated for production of local or regional analgesia and anesthesia by local infiltration, peripheral nerve block techniques, and central neural techniques including epidural and caudal blocks.
The routes of administration and indicated concentrations for CARBOCAINE are:
See for additional information. Standard textbooks should be consulted to determine the accepted procedures and techniques for the administration of CARBOCAINE.
The dose of any local anesthetic administered varies with the anesthetic procedure, the area to be anesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked, the depth of anesthesia and degree of muscle relaxation required, the duration of anesthesia desired, individual tolerance and the physical condition of the patient. The smallest dose and concentration required to produce the desired result should be administered. Dosages of CARBOCAINE should be reduced for elderly and debilitated patients and patients with cardiac and/or liver disease. The rapid injection of a large volume of local anesthetic solution should be avoided and fractional doses should be used when feasible.
For specific techniques and procedures, refer to standard textbooks.
There have been adverse event reports of chondrolysis in patients receiving intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures. CARBOCAINE is not approved for this use (See and ).
The recommended single dose (or the total of a series of doses given in one procedure) of CARBOCAINE for unsedated, healthy, normal-sized individuals should not usually exceed 400 mg. The recommended dosage is based on requirements for the average adult and should be reduced for elderly or debilitated patients.
While maximum doses of 7 mg/kg (550 mg) have been administered without adverse effect, these are not recommended, except in exceptional circumstances and under no circumstances should the administration be repeated at intervals of less than 1 1/2 hours. The total dose for any 24-hour period should not exceed 1,000 mg because of a slow accumulation of the anesthetic or its derivatives or slower than normal metabolic degradation or detoxification with repeat administration (See and ).
Unused portions of solutions not containing preservatives, i.e., those supplied in single-dose vials, should be discarded following initial use.
This product should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. Solutions which are discolored or which contain particulate matter should not be administered.
What interacts with Carbocaine?
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What are the warnings of Carbocaine?
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What are the precautions of Carbocaine?
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What are the side effects of Carbocaine?
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What should I look out for while using Carbocaine?
CARBOCAINE is contraindicated in patients with a known hypersensitivity to it or to any local anesthetic agent of the amide-type or to other components of solutions of CARBOCAINE.
Local anesthetic solutions containing antimicrobial preservatives (i.e., those supplied in multiple-dose vials) should not be used for epidural or caudal anesthesia because safety has been established with regard to intrathecal injection, either intentionally or inadvertently, of such preservatives.
Intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures is an unapproved use, and there have been post-marketing reports of chondrolysis in patients receiving such infusions. The majority of reported cases of chondrolysis have involved the shoulder joint; cases of gleno-humeral chondrolysis have been described in pediatric and adult patients following intra-articular infusions of local anesthetics with and without epinephrine for periods of 48 to 72 hours. There is insufficient information to determine whether shorter infusion periods are not associated with these findings. The time of onset of symptoms, such as joint pain, stiffness and loss of motion can be variable, but may begin as early as the 2nd month after surgery. Currently, there is no effective treatment for chondrolysis; patients who experienced chondrolysis have required additional diagnostic and therapeutic procedures and some required arthroplasty or shoulder replacement.
It is essential that aspiration for blood or cerebrospinal fluid (where applicable) be done prior to injecting any local anesthetic, both the original dose and all subsequent doses, to avoid intravascular or subarachnoid injection. However, a negative aspiration does not ensure against an intravascular or subarachnoid injection.
Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics.
CARBOCAINE with epinephrine or other vasopressors should not be used concomitantly with ergot-type oxytocic drugs, because a severe persistent hypertension may occur. Likewise, solutions of CARBOCAINE containing a vasoconstrictor, such as epinephrine, should be used with extreme caution in patients receiving monoamine oxidase inhibitors (MAOI) or antidepressants of the triptyline or imipramine types, because severe prolonged hypertension may result.
CARBOCAINE, along with other local anesthetics, may produce methemoglobinemia. The clinical signs of methemoglobinemia are cyanosis of the nail beds and lips, fatigue and weakness.
Local anesthetic procedures should be used with caution when there is inflammation and/or sepsis in the region of the proposed injection.
Mixing or the prior or intercurrent use of any local anesthetic with CARBOCAINE cannot be recommended because of insufficient data on the clinical use of such mixtures.
What might happen if I take too much Carbocaine?
Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics or to unintended subarachnoid injection of local anesthetic solution (See , , and ).
How should I store and handle Carbocaine?
Single-dose vials and multiple-dose vials of CARBOCAINE may be sterilized by autoclaving at 15 pound pressure, 121°C (250°F) for 15 minutes. Solutions of CARBOCAINE may be reautoclaved when necessary. Do not administer solutions which are discolored or which contain particulate matter.THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL ANESTHESIA OR DENTAL USEStore at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]Distributed by Hospira, Inc., Lake Forest, IL 60045 USALAB-0996-3.001/2018Single-dose vials and multiple-dose vials of CARBOCAINE may be sterilized by autoclaving at 15 pound pressure, 121°C (250°F) for 15 minutes. Solutions of CARBOCAINE may be reautoclaved when necessary. Do not administer solutions which are discolored or which contain particulate matter.THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL ANESTHESIA OR DENTAL USEStore at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]Distributed by Hospira, Inc., Lake Forest, IL 60045 USALAB-0996-3.001/2018Single-dose vials and multiple-dose vials of CARBOCAINE may be sterilized by autoclaving at 15 pound pressure, 121°C (250°F) for 15 minutes. Solutions of CARBOCAINE may be reautoclaved when necessary. Do not administer solutions which are discolored or which contain particulate matter.THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL ANESTHESIA OR DENTAL USEStore at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]Distributed by Hospira, Inc., Lake Forest, IL 60045 USALAB-0996-3.001/2018Single-dose vials and multiple-dose vials of CARBOCAINE may be sterilized by autoclaving at 15 pound pressure, 121°C (250°F) for 15 minutes. Solutions of CARBOCAINE may be reautoclaved when necessary. Do not administer solutions which are discolored or which contain particulate matter.THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL ANESTHESIA OR DENTAL USEStore at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]Distributed by Hospira, Inc., Lake Forest, IL 60045 USALAB-0996-3.001/2018Single-dose vials and multiple-dose vials of CARBOCAINE may be sterilized by autoclaving at 15 pound pressure, 121°C (250°F) for 15 minutes. Solutions of CARBOCAINE may be reautoclaved when necessary. Do not administer solutions which are discolored or which contain particulate matter.THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL ANESTHESIA OR DENTAL USEStore at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]Distributed by Hospira, Inc., Lake Forest, IL 60045 USALAB-0996-3.001/2018Single-dose vials and multiple-dose vials of CARBOCAINE may be sterilized by autoclaving at 15 pound pressure, 121°C (250°F) for 15 minutes. Solutions of CARBOCAINE may be reautoclaved when necessary. Do not administer solutions which are discolored or which contain particulate matter.THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL ANESTHESIA OR DENTAL USEStore at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]Distributed by Hospira, Inc., Lake Forest, IL 60045 USALAB-0996-3.001/2018
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Local anesthetics block the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the 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. Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone.
Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems. At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal. However, toxic blood concentrations depress cardiac conduction and excitability, which may lead to atrioventricular block and ultimately to cardiac arrest. 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 stimulation is manifested as restlessness, tremors, and shivering, progressing to convulsions, followed by depression and coma progressing ultimately to 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.
A clinical study using 15 mL of 2% epidural mepivacaine at the T 9-10 interspace in 62 patients, 20-79 years of age, demonstrated a 40% decrease in the amount of mepivacaine required to block a given number of dermatomes in the elderly (60-79 years, N=13) as compared to young adults 20-39 years).
Another study using 10 mL of 2% lumbar epidural mepivacaine in 161 patients, 19-75 years of age, demonstrated a strong inverse relationship between patient age and the number of dermatomes blocked per cc of mepivacaine injected.
Non-Clinical Toxicology
CARBOCAINE is contraindicated in patients with a known hypersensitivity to it or to any local anesthetic agent of the amide-type or to other components of solutions of CARBOCAINE.Local anesthetic solutions containing antimicrobial preservatives (i.e., those supplied in multiple-dose vials) should not be used for epidural or caudal anesthesia because safety has been established with regard to intrathecal injection, either intentionally or inadvertently, of such preservatives.
Intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures is an unapproved use, and there have been post-marketing reports of chondrolysis in patients receiving such infusions. The majority of reported cases of chondrolysis have involved the shoulder joint; cases of gleno-humeral chondrolysis have been described in pediatric and adult patients following intra-articular infusions of local anesthetics with and without epinephrine for periods of 48 to 72 hours. There is insufficient information to determine whether shorter infusion periods are not associated with these findings. The time of onset of symptoms, such as joint pain, stiffness and loss of motion can be variable, but may begin as early as the 2nd month after surgery. Currently, there is no effective treatment for chondrolysis; patients who experienced chondrolysis have required additional diagnostic and therapeutic procedures and some required arthroplasty or shoulder replacement.
It is essential that aspiration for blood or cerebrospinal fluid (where applicable) be done prior to injecting any local anesthetic, both the original dose and all subsequent doses, to avoid intravascular or subarachnoid injection. However, a negative aspiration does not ensure against an intravascular or subarachnoid injection.
Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics.
CARBOCAINE with epinephrine or other vasopressors should not be used concomitantly with ergot-type oxytocic drugs, because a severe persistent hypertension may occur. Likewise, solutions of CARBOCAINE containing a vasoconstrictor, such as epinephrine, should be used with extreme caution in patients receiving monoamine oxidase inhibitors (MAOI) or antidepressants of the triptyline or imipramine types, because severe prolonged hypertension may result.
CARBOCAINE, along with other local anesthetics, may produce methemoglobinemia. The clinical signs of methemoglobinemia are cyanosis of the nail beds and lips, fatigue and weakness.
Local anesthetic procedures should be used with caution when there is inflammation and/or sepsis in the region of the proposed injection.
Mixing or the prior or intercurrent use of any local anesthetic with CARBOCAINE cannot be recommended because of insufficient data on the clinical use of such mixtures.
The administration of local anesthetic solutions containing epinephrine or norepinephrine to patients receiving monoamine oxidase inhibitors or tricyclic antidepressants may produce severe, prolonged hypertension. Concurrent use of these agents should generally be avoided. In situations when concurrent therapy is necessary, careful patient monitoring is essential.
Concurrent administration of vasopressor drugs and of ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.
Phenothiazines and butyrophenones may reduce or reverse the pressor effect of epinephrine.
The safety and effectiveness of local anesthetics depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use (See and ). During major regional nerve blocks, the patient should have intravenous fluids running via an indwelling catheter to assure a functioning intravenous pathway. The lowest dosage of local anesthetic that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects. Injections should be made slowly, with frequent aspirations before and during the injection to avoid intravascular injection. Current opinion favors fractional administration with constant attention to the patient, rather than rapid bolus injection. Syringe aspirations should also be performed before and during each supplemental injection in continuous (intermittent) 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 be administered initially and the effects monitored before the full dose is given. When using a "continuous" catheter technique, test doses should be given prior to both the original and all reinforcing doses, because plastic tubing in the epidural space can migrate into a blood vessel or through the dura. When clinical conditions permit, an effective test dose should contain epinephrine (10 mcg to 15 mcg have been suggested) to serve as a warning of unintended intravascular injection. If injected into a blood vessel, this amount of epinephrine is likely to produce an "epinephrine response" within 45 seconds, consisting of an increase of pulse and blood pressure, circumoral pallor, palpitations, and nervousness in the unsedated patient. The sedated patient may exhibit only a pulse rate increase of 20 or more beats per minute for 15 or more seconds. Therefore, following the test dose, the heart rate should be monitored for a heart rate increase. The test dose should also contain 45 mg to 50 mg of CARBOCAINE to detect an unintended intrathecal administration. This will be evidenced within a few minutes by signs of spinal block (e.g., decreased sensation of the buttocks, paresis of the leg, or, in the sedated patient, absent knee jerk).
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 status of the patient. Debilitated, elderly patients, and acutely ill patients should be given reduced doses commensurate with their age and physical status. Local anesthetics should also be used with caution in patients with severe disturbances of cardiac rhythm, shock, heart block, or hypotension.
Careful and constant monitoring of cardiovascular and respiratory (adequacy of ventilation) vital signs, and the patient's state of consciousness should be performed after each local anesthetic injection. It should be kept in mind at such times 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.
Local anesthetic solutions containing a vasoconstrictor should be used cautiously and in carefully restricted quantities in areas of the body supplied by end arteries or having otherwise compromised blood supply such as digits, nose, external ear, penis. Patients with hypertensive vascular disease may exhibit exaggerated vasoconstrictor response. Ischemic injury or necrosis may result.
Mepivacaine should be used with caution in patients with known allergies and sensitivities.
Because amide-type local anesthetics such as CARBOCAINE are metabolized by the liver and excreted by the kidneys, these drugs, especially repeat doses, should be used cautiously in patients with hepatic and renal disease. Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at a greater risk of developing, toxic plasma concentrations. Local anesthetics should also be used with caution in patients with impaired cardiovascular function because they may be less able to compensate for functional changes associated with the prolongation of AV conduction produced by these drugs.
Serious dose-related cardiac arrhythmias may occur if preparations containing a vasoconstrictor such as epinephrine are employed in patients during or following the administration of potent inhalation anesthetics. In deciding whether to use these products concurrently in the same patient, the combined action of both agents upon the myocardium, the concentration and volume of vasoconstrictor used, and the time since injection, when applicable, should be taken into account.
Many drugs used during the conduct of anesthesia are considered potential triggering agents for familial malignant hyperthermia. Because it is not known whether amide-type local anesthetics may trigger this reaction and because the need for supplemental general anesthesia cannot be predicted in advance, it is suggested that a standard protocol for management should be available. Early unexplained signs of tachycardia, tachypnea, labile blood pressure, and metabolic acidosis may precede temperature elevation. Successful outcome is dependent on early diagnosis, prompt discontinuance of the suspect triggering agent(s), and institution of treatment, including oxygen therapy, indicated supportive measures, and dantrolene. (Consult dantrolene sodium intravenous package insert before using.)
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 intra-arterial injection of the local anesthetic with retrograde flow to the cerebral circulation. Patients receiving these blocks should have their circulation and respiration monitored and be constantly observed. Resuscitative equipment and personnel for treating adverse reactions should be immediately available. Dosage recommendations should not be exceeded.
Reactions to CARBOCAINE are characteristic of those associated with other amide-type local anesthetics. A major cause of adverse reactions to this group of drugs is excessive plasma levels, which may be due to overdosage, inadvertent intravascular injection, or slow metabolic degradation.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72Tips
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Interactions
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