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Local Anesthetics (ester and amide-type)

Disclaimer - Please see package insert for additional information and possible updates. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.   Read the disclaimer

Individual monographs (Dosing information etc)
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Clinical Pharmacology of local anesthetics
Allergic reactions (overview)
Management of Local Anesthetic Emergencies

Clinical Pharmacology

CLINICAL PHARMACOLOGY (package insert data): 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: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone.

Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems (CNS). 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, ventricular arrhythmias, and cardiac arrest, sometimes resulting in fatalities. In addition, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure. Recent clinical reports and animal research suggest that these cardiovascular changes are more likely to occur after unintended intravascular injection of bupivacaine. Therefore, incremental dosing is necessary.

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 state.

Allergic reactions

Allergic reactions: (Package insert)
Allergic-type reactions are rare and may occur as a result of sensitivity to the local anesthetic or to other formulation ingredients, such as the antimicrobial preservative methylparaben contained in multiple-dose vials or sulfites in epinephrine-containing solutions. These reactions are characterized by signs such as urticaria, pruritus, erythema, angioneurotic edema (including laryngeal edema), tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and possibly, anaphylactoid-like symptomatology (including severe hypotension).

Cross sensitivity among members of the amide-type local anesthetic group has been reported. The usefulness of screening for sensitivity has not been definitely established.

Cross sensitivity among members of the ester-type local anesthetic group has been reported. The usefulness of screening for sensitivity has not been definitely established.
 
Key points:    Ester-type local anesthetics are much more likely to cause an allergic reaction compared to the  amide-type local anesthetics because of the formation of PABA during the metabolic process.  PABA may cause allergic reactions that range from urticaria to analphylaxis.  PABA is also formed during the metabolism of methylparaben (preservative) that is usually found in multi-dose vials including lidocaine (MDV) (amide-type local anesthetic). 

Sample structure of procaine (ester-type):
Procaine:  ester of diethylaminoethanol and para-aminobenzoic acid
procaine

As mentioned above, allergic-type reactions are rare and are usually the result of sensitivity to additives such as methylparaben (preservative) or sulfites (prevent degradation of vasopressors such as epinephrine) that are present in some of the local anesthetic products.

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General approach:
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If a patient has an allergic response to either class, attempt using a product from the
other class. Example: patient develops a rash with procaine (ester-type) --> switch to
lidocaine for example (amide-type).  Alternatively, if a patient has a reaction to both classes or even a single class, try using a preservative-free formulation such as lidocaine-MPF..

Management of Local Anesthetic Emergencies

Management of Local Anesthetic Emergencies: The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient’s state of consciousness after each local anesthetic injection. At the first sign of change, oxygen should be administered.

The first step in the management of systemic toxic reactions, as well as underventilation or apnea due to unintentional subarachnoid injection of drug solution, consists of immediate attention to the establishment and maintenance of a patent 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 occurred.

If necessary, use drugs to control the convulsions. A 50 mg to 100 mg bolus IV injection of succinylcholine will paralyze the patient without depressing the central nervous or cardiovascular systems and facilitate ventilation. A bolus IV dose of 5 mg to 10 mg of diazepam or 50 mg to 100 mg of thiopental will permit ventilation and counteract central nervous system stimulation, but these drugs also depress central nervous system, respiratory, and cardiac function, add to postictal depression and may result in apnea. Intravenous barbiturates, anticonvulsant 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).

Endotracheal intubation, employing drugs and techniques familiar to the clinician, may be indicated after initial administration of oxygen by mask if difficulty is encountered in the maintenance of a patent airway, or if prolonged ventilatory support (assisted or controlled) is indicated.

Recent clinical data from patients experiencing local anesthetic-induced convulsions demonstrated rapid development of hypoxia, hypercarbia, and acidosis with bupivacaine within a minute of the onset of convulsions. These observations suggest that oxygen consumption and carbon dioxide production are greatly increased during local anesthetic convulsions and emphasize the importance of immediate and effective ventilation with oxygen which may avoid cardiac arrest.

If not treated immediately, convulsions with simultaneous hypoxia, hypercarbia, and acidosis plus myocardial depression from the direct effects of the local anesthetic may result in cardiac arrhythmias, bradycardia, asystole, ventricular fibrillation, or cardiac arrest. Respiratory abnormalities, including apnea, may occur. Underventilation or apnea due to unintentional subarachnoid injection of local anesthetic solution may produce these same signs and also lead to cardiac arrest if ventilatory support is not instituted. If cardiac arrest should occur, successful outcome may require prolonged resuscitative efforts.

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 be accomplished.

Esters

Chloroprocaine HCL (Nesacaine®) Procaine HCL (Novocain®)
Tetracaine HCL (Pontocaine®) --

Amides

Bupivacaine (Marcaine®, Sensorcaine® ) Mepivacaine (Carbocaine®, Polocaine®)
Lidocaine (Xylocaine®) c/o epi Lidocaine HCL (Xylocaine-MPF) Preservative free
Lidocaine (Xylocaine®) with epi Ropivacaine (Naropin)®
Topical Ester
Topical Amide
Benzocaine Dibucaine®
 

Esters

Chloroprocaine (Nesacaine®): top of page

DESCRIPTION
Chloroprocaine Hydrochloride Injection, USP is a sterile, nonpyrogenic, isotonic, isobaric solution. Each milliliter of 2% solution contains 20 mg of chloroprocaine hydrochloride; 4 mg sodium chloride; with 1.8 mg sodium metabisulfite added in water for injection. Each milliliter of 3% solution contains 30 mg of chloroprocaine hydrochloride; 2.1 mg sodium chloride; with 1.8 mg sodium metabisulfite added in water for injection. May contain hydrochloric acid and/or sodium hydroxide for pH adjustment. It contains no bacteriostat, antimicrobial agent or added buffer. Discard unused portion.

It is intended for production of local anesthesia by nerve block, infiltration, caudal or other epidural blocks.

Chloroprocaine Hydrochloride Injection has a pH of 3.1 (2.7 to 4.0).

Sodium Chloride, USP is chemically designated NaCl, a white crystalline compound freely soluble in water.

INDICATIONS AND USAGE:
Chloroprocaine Hydrochloride Injection in single-dose containers without preservative and without EDTA, is indicated for the production of local anesthesia by infiltration, peripheral and central nerve block, including lumbar and caudal epidural blocks.

Chloroprocaine Hydrochloride Injection is not to be used for subarachnoid administration.

DOSAGE AND ADMINISTRATION:
Chloroprocaine may be administered as a single injection or continuously through an indwelling catheter. As with all local anesthetics, the dose administered varies with the anesthetic procedure, the vascularity of the tissues, the depth of anesthesia and degree of muscle relaxation required, the duration of anesthesia desired, and the physical condition of the patient. The smallest dose and concentration required to produce the desired result should be used. Dosage should be reduced for children, elderly and debilitated patients and patients with cardiac and/or liver disease. The maximum single recommended doses of chloroprocaine in adults are: without epinephrine, 11 mg/kg, not to exceed a maximum total dose of 800 mg; with epinephrine (1:200,000), 14 mg/kg, not to exceed a maximum total dose of 1000 mg. 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. Chloroprocaine is not approved for this use (see WARNINGS and DOSAGE AND ADMINISTRATION).

Caudal and Lumbar Epidural Block:

In order to guard against adverse experiences sometimes noted following unintended penetration of the subarachnoid space, the following procedure modifications are recommended:

1. Use an adequate test dose (3 mL of 3% or 5 mL of 2% Chloroprocaine Hydrochloride Injection) prior to induction of complete block. This test dose should be repeated if the patient is moved in such a fashion as to have displaced the epidural catheter. Allow adequate time for onset of anesthesia following administration of each test dose. 2. Avoid the rapid injection of a large volume of local anesthetic injection through the catheter. Consider fractional doses, when feasible. 3. In the event of the known injection of a large volume of local anesthetic injection into the subarachnoid space, after suitable resuscitation and if the catheter is in place, consider attempting the recovery of drug by draining a moderate amount of cerebrospinal fluid (such as 10 mL) through the epidural catheter.

As a guide for some routine procedures, suggested doses are given below:

1. Infiltration and Peripheral Nerve Block: Chloroprocaine Hydrochloride Injection

Anesthetic Procedure

Solution Concentration %

Volume (mL)

Total Dose (mg)

Mandibular

2

2 - 3

40 - 60

Infraorbital

2

0.5 - 1

10 - 20

Brachial plexus

2

30 - 40

600 - 800

Digital (without epinephrine)

1

3 - 4

30 - 40

Pudendal

2

10 each side

400

Paracervical

1

3 per each of 4 sites

up to 120


2. Caudal and Lumbar Epidural Block: For caudal anesthesia, the initial dose is 15 to 25 mL of a 2% or 3% solution. Repeated doses may be given at 40 to 60 minute intervals.

For lumbar epidural anesthesia, 2 to 2.5 mL per segment of a 2% or 3% solution can be used. The usual total volume of Chloroprocaine Hydrochloride Injection is from 15 to 25 mL. Repeated doses 2 to 6 mL less than the original dose may be given at 40 to 50 minute intervals.

The above dosages are recommended as a guide for use in the average adult. Maximum dosages of all local anesthetics must be individualized after evaluating the size and physical condition of the patient and the rate of systemic absorption from a particular injection site.

Pediatric Dosage:
It is difficult to recommend a maximum dose of any drug for children, since this varies as a function of age and weight. For children over 3 years of age who have a normal lean body mass and normal body development, the maximum dose is determined by the child’s age and weight and should not exceed 11 mg/kg (5 mg/lb). For example, in a child of 5 years weighing 50 lbs (23 kg), the dose of chloroprocaine HCl without epinephrine would be 250 mg. Concentrations of 0.5 - 1% are suggested for infiltration and 1 - 1.5% for nerve block. In order to guard against systemic toxicity, the lowest effective concentration and lowest effective dose should be used at all times. Some of the lower concentrations for use in infants and smaller children are not available in pre-packaged containers; it will be necessary to dilute available concentrations with the amount of 0.9% sodium chloride injection necessary to obtain the required final concentration of chloroprocaine injection.

Preparation of Epinephrine Injections:
To prepare a 1:200,000 epinephrine-chloroprocaine HCl injection, add 0.15 mL of 1 to 1000 Epinephrine Injection to 30 mL of Chloroprocaine Hydrochloride Injection.

Chloroprocaine is incompatible with caustic alkalis and their carbonates, soaps, silver salts, iodine and iodides.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever injection and container permit. As with other anesthetics having a free aromatic amino group, Chloroprocaine Hydrochloride Injection is slightly photosensitive and may become discolored after prolonged exposure to light. It is recommended that this product be stored in the original outer containers, protected from direct sunlight. Discolored injection should not be administered. If exposed to low temperatures, Chloroprocaine Hydrochloride Injection may deposit crystals of chloroprocaine HCl which will redissolve with shaking when returned to room temperature. The product should not be used if it contains undissolved (e.g., particulate) material.


CONTRAINDICATIONS:
Chloroprocaine Hydrochloride Injection is contraindicated in patients hypersensitive (allergic) to drugs of the PABA ester group.

Lumbar and caudal epidural anesthesia should be used with extreme caution in persons with the following conditions: existing neurological disease, spinal deformities, septicemia and severe hypertension.

WARNINGS:
 LOCAL ANESTHETICS SHOULD ONLY BE EMPLOYED BY CLINICIANS WHO ARE WELL VERSED IN DIAGNOSIS AND MANAGEMENT OF DOSE-RELATED TOXICITY AND OTHER ACUTE EMERGENCIES WHICH MIGHT ARISE FROM THE BLOCK TO BE EMPLOYED, AND THEN ONLY AFTER ENSURING THE IMMEDIATE AVAILABILITY OF OXYGEN, OTHER RESUSCITATIVE DRUGS, CARDIOPULMONARY RESUSCITATIVE EQUIPMENT, AND THE PERSONNEL RESOURCES NEEDED FOR PROPER MANAGEMENT OF TOXIC REACTIONS AND RELATED EMERGENCIES (See also ADVERSE REACTIONS and PRECAUTIONS.) DELAY IN PROPER MANAGEMENT OF DOSE-RELATED TOXICITY, UNDERVENTILATION FROM ANY CAUSE AND/OR ALTERED SENSITIVITY MAY LEAD TO THE DEVELOPMENT OF ACIDOSIS, CARDIAC ARREST AND, POSSIBLY, DEATH.

Chloroprocaine Hydrochloride Injection, contains no preservative; discard unused injection remaining in vial after initial use.

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.

Vasopressors should not be used in the presence of ergot-type oxytocic drugs, since a severe persistent hypertension may occur.

To avoid intravascular injection, aspiration should be performed before the anesthetic solution is injected. The needle must be repositioned until no blood return can be elicited. However, the absence of blood in the syringe does not guarantee that intravascular injection has been avoided.

Mixtures of local anesthetics are sometimes employed to compensate for the slower onset of one drug and the shorter duration of action of the second drug. Experiments in primates suggest that toxicity is probably additive when mixtures of local anesthetics are employed, but some experiments in rodents suggest synergism. Caution regarding toxic equivalence should be exercised when mixtures of local anesthetics are employed.

Chloroprocaine Hydrochloride Injection contains sodium metabisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in nonasthmatic people.

DOSAGE FORMS AND STRENGTHS:
Chloroprocaine Hydrochloride Injection, USP is supplied in single-dose containers as follows:
Concentration  NDC No. Container Container Size
2% 0409-4169-01 Vial 30 mL
3% 0409-4170-01 Vial 30 mL


Store at 20 to 25°C (68 to 77°F). [See USP Controlled Room Temperature.]

SOURCE:
Package insert data:
Hospira, Inc., Lake Forest, IL 60045 USA
Revised: March, 2010

Procaine (Novocain®): top of page

novocain (Procaine Hydrochloride) injection, solution
Local Anesthetic for Local Infiltration and Peripheral Nerve Block

THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL OR EPIDURAL ANESTHESIA OR DENTAL USE

DESCRIPTION
Procaine hydrochloride is benzoic acid, 4-amino-, 2-(diethylamino) ethyl ester, monohydrochloride, the ester of diethylaminoethanol and para-aminobenzoic acid.
The solutions are made isotonic with sodium chloride and the pH is adjusted between 3 and 5.5 with sodium hydroxide and/or hydrochloric acid.

Procaine hydrochloride is related chemically and pharmacologically to the ester-type local anesthetics. It contains an ester linkage between the aromatic nucleus and the amino group.

NOVOCAIN is available as sterile solutions in concentrations of 1% and 2% for injection via local infiltration and peripheral nerve block.

INDICATIONS AND USAGE:
NOVOCAIN is indicated for the production of local or regional analgesia and anesthesia by local infiltration and peripheral nerve block techniques.

The routes of administration and concentrations are: for local infiltration use 0.25% to 0.5% (via dilution) and for peripheral nerve blocks use 0.5% (via dilution), 1%, and 2%. (See DOSAGE AND ADMINISTRATION for additional information.)

Standard textbooks should be consulted to determine the accepted procedures and techniques for the administration of NOVOCAIN.

DOSAGE AND ADMINISTRATION:
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 NOVOCAIN 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.

For infiltration anesthesia, 0.25% or 0.5% solution; 350 mg to 600 mg is generally considered to be a single safe total dose. To prepare 60 mL of a 0.5% solution (5 mg/mL), dilute 30 mL of the 1% solution with 30 mL sodium chloride injection 0.9%. To prepare 60 mL of a 0.25% solution (2.5 mg/mL), dilute 15 mL of the 1% solution with 45 mL sodium chloride injection 0.9%. An anesthetic solution of 0.5 mL to 1 mL of epinephrine 1:1,000 per 100 mL may be added for vasoconstrictive effect (1:200,000 to 1:100,000). (See WARNINGS and package insert for PRECAUTIONS.)

For peripheral nerve block, 0.5% solution (up to 200 mL), 1% solution (up to 100 mL), or 2% solution (up to 50 mL). The use of the 2% solution should usually be limited to cases requiring a small volume of anesthetic solution (10 mL to 25 mL). An anesthetic solution of 0.5 mL to 1 mL of epinephrine 1:1,000 per 100 mL may be added for vasoconstrictive effect (1:200,000 to 1:100,000). (See WARNINGS and package insert for PRECAUTIONS.)

THE USUAL TOTAL DOSE DURING ONE TREATMENT SHOULD NOT EXCEED 1,000 MG.

This product should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. Do not use solutions if crystals, cloudiness, or discoloration is observed. Examine solution carefully before use. Reautoclaving increases likelihood of crystal formation. Solutions which are discolored or which contain particulate matter should not be administered.

Unused portions of solutions not containing preservatives should be discarded.

Pediatric Use:
In pediatric patients 15 mg/kg of a 0.5% solution for local infiltration is the maximum recommended dose.

CONTRAINDICATIONS:
NOVOCAIN is contraindicated in patients with a known hypersensitivity to procaine, drugs of a similar chemical configuration, or para-aminobenzoic acid or its derivatives.

It is also contraindicated in patients with a known hypersensitivity to other components of solutions of NOVOCAIN.


WARNINGS:
Contains acetone sodium bisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in nonasthmatic people.

LOCAL ANESTHETICS SHOULD ONLY BE EMPLOYED BY CLINICIANS WHO ARE WELL VERSED IN DIAGNOSIS AND MANAGEMENT OF DOSE-RELATED TOXICITY AND OTHER ACUTE EMERGENCIES WHICH MIGHT ARISE FROM THE BLOCK TO BE EMPLOYED, AND THEN ONLY AFTER INSURING THE IMMEDIATE AVAILABILITY OF OXYGEN, OTHER RESUSCITATIVE DRUGS, CARDIOPULMONARY RESUSCITATIVE EQUIPMENT, AND THE PERSONNEL RESOURCES NEEDED FOR PROPER MANAGEMENT OF TOXIC REACTIONS AND RELATED EMERGENCIES. (See also ADVERSE REACTIONS and PRECAUTIONS.) DELAY IN PROPER MANAGEMENT OF DOSE-RELATED TOXICITY, UNDERVENTILATION FROM ANY CAUSE, AND/OR ALTERED SENSITIVITY MAY LEAD TO THE DEVELOPMENT OF ACIDOSIS, CARDIAC ARREST, AND, POSSIBLY, DEATH.

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, even in the absence of a history of hypersensitivity. Large doses of local anesthetics should not be used in patients with heartblock.

NOVOCAIN 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 NOVOCAIN 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 or disturbances of cardiac rhythm may occur.

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 NOVOCAIN cannot be recommended because of insufficient data on the clinical use of such mixtures.

DOSAGE FORMS AND STRENGTHS:
Single-dose containers and multiple-dose containers of NOVOCAIN may be sterilized by autoclaving at 15-pound pressure, 121°C (250°F) for 15 minutes. Do not use solutions if crystals, cloudiness, or discoloration is observed. Examine solution carefully before use. Reautoclaving increases likelihood of crystal formation. Do not administer solutions which are discolored or which contain particulate matter. Protect solutions from light.

Unused portions of solutions not containing preservatives, i.e., those supplied in ampuls, should be discarded following initial use.

THESE SOLUTIONS ARE NOT INTENDED FOR SPINAL OR EPIDURAL ANESTHESIA OR DENTAL
List Container Concentration Fill Quantity
1808 Uni-Amp® unit dose pak 1 % 2 mL 25
1808 Single-Dose Ampuls 1 % 6 mL 50
1824 Multiple-Dose Vials 1 % 30 mL 1
1825 Multiple-Dose Vials 2 % 30 mL 1

SOURCE:
Package insert data:
©Hospira 2004 EN-0665 Printed in USA
HOSPIRA, INC., LAKE FOREST, IL 60045 USA
Rev: November, 2004

Tetracaine HCL (Pontocaine®): top of page

 Tetracaine HCl Injection, USP for Prolonged Spinal Anesthesia

Description
Tetracaine hydrochloride is 2-(Dimethylamino)ethyl p-(butylamino)benzoate monohydrochloride. It is a white crystalline, odorless powder that is readily soluble in water, physiologic saline solution, and dextrose solution.

Tetracaine hydrochloride is a local anesthetic of the ester-linkage type, related to procaine.
1% Solution: A sterile, isotonic, isobaric solution.
Each mL contains:
Active: 10 mg Tetracaine Hydrochloride
Inactives: 7.5 mg Sodium Chloride, Hydrochloric Acid and/or Sodium Hydroxide may be added to adjust pH (3.2 to 6.0) and Water for Injection, USP.

Nitrogen gas has been used to displace the air in the ampules.
This formulation does not contain preservatives.

INDICATIONS AND USAGE:
Tetracaine hydrochloride is indicated for the production of spinal anesthesia for procedures requiring two to three hours.

DOSAGE AND ADMINISTRATION:
As with all anesthetics, the dosage varies and depends upon the area to be anesthetized, the number of neuronal segments to be blocked, individual tolerance, and the technique of anesthesia. The lowest dosage needed to provide effective anesthesia should be administered. For specific techniques and procedures, refer to standard textbooks.

Suggested Dosage for Spinal Anesthesia Using 1% Tetracaine HCl Injection, USP
Extent of Anesthesia Dose of solution (mL) Volume of spinal fluid (mL) Site of injection  (lumbar interspace)
Perineum 0.5 (= 5 mg)* 0.5 4th
Perineum and lower extremities 1.0 (= 10 mg) 1.0 3rd or 4th
Up to costal margin (=15 mg to 20 mg) 1.5 to 2.0 1.5 to 2.0 2nd, 3rd, or 4th

The extent and degree of spinal anesthesia depend upon dosage, specific gravity of the anesthetic solution, volume of solution used, force of the injection, level of puncture, position of the patient during and immediately after injection, etc.

When spinal fluid is added to 1% tetracaine hydrochloride injection, some turbidity results, the degree depending on the pH of the spinal fluid, the temperature of the solution during mixing, as well as the amount of drug and diluent employed. Liberation of base (which is completed within the spinal canal) is held to be essential for satisfactory results with any spinal anesthetic.

The specific gravity of spinal fluid at 25°C/25°C varies under normal conditions from 1.0063 to 1.0075. The 1% concentration in saline solution has a specific gravity of 1.0060 to 1.0074 at 25°C/25°C.

A hyperbaric solution may be prepared by mixing equal volumes of the 1% solution and Dextrose Solution 10%.

Examine ampules carefully before use. Do not use solution if crystals, cloudiness, or discoloration is observed.

This formulation of tetracaine hydrochloride does not contain antimicrobial or bacteriostatic agents; therefore, unused portions should be discarded.

Sterilization of Ampules
The tetracaine hydrochloride injection is sterile within an undamaged ampule. To destroy bacteria on the exterior of ampules use heat sterilization (autoclaving) before opening. Immersion in antiseptic solution is not recommended.

Autoclave at 15-pounds pressure, at 121°C (250°F), for 15 minutes.

Autoclaving increases likelihood of crystal formation. Unused autoclaved ampules should be discarded. Under no circumstances should unused ampules which have been autoclaved be returned to stock.

CONTRAINDICATIONS:
Spinal anesthesia with tetracaine hydrochloride is contraindicated in patients with known hypersensitivity to tetracaine hydrochloride or to drugs of a similar chemical configuration (ester-type local anesthetics), or aminobenzoic acid or its derivatives; and in patients for whom spinal anesthesia as a technique is contraindicated.

The decision as to whether or not spinal anesthesia should be used for an individual patient should be made by the physician after weighing the advantages with the risks and possible complications. Contraindications to spinal anesthesia as a technique can be found in standard reference texts, and usually include generalized septicemia, infection at the site of injection, certain diseases of the cerebrospinal system, uncontrolled hypotension, etc.

WARNINGS:
RESUSCITATIVE EQUIPMENT AND DRUGS SHOULD BE IMMEDIATELY AVAILABLE WHENEVER ANY LOCAL ANESTHETIC DRUG IS USED.

Large doses of local anesthetics should not be used in patients with heartblock.

Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics, even in the absence of a history of hypersensitivity.

DOSAGE FORMS AND STRENGTHS:
1% isotonic isobaric solution: 2 mL Ampules, box of 25.

NDC 17478-045-32
Storage: Store under refrigeration. Protect ampules from light.

SOURCE:
Package insert data:
Akorn, Inc.
Lake Forest, IL 60045
Rev. 12/08

Benzocaine: top of page

Available in multiple dosage forms: gel, ointment, liquid, cream

Allergy alert
Do not use this product if you have a history of allergy to local anesthetics, such as procaine, butacaine, benzocaine, or other “caine” anesthetics due to the possibility of anaphylactic shock.

Active Ingredient (in each gram)
Benzocaine 0.2% to 20.0% (w/w) depending on site of application and formulation.

Depending on formulation, may have multiple uses:
-------------------------
Creams, sprays, etc may be indicated for the following:
For Temporary Relief of Pain and Itching associated with minor burns scrapes and insect bites.
-------------------------
Gel:
For the temporary relief of minor pain and sore mouth associated with toothache, minor dental procedures and irritations from dentures or orthodontic appliances.

When using this product
Do not use for more than 7 days unless directed by a dentist or doctor. If sore mouth symptoms do not improve in 7 days; if irritation, pain or redness persists or worsens; or if swelling, rash, fever or other allergic reaction develops, see your doctor or dentist promptly. Do not exceed recommended dosage.
-------------------------

SOURCE:
Package insert data

Disclaimer top of page icon

Disclaimer - Please see package insert for additional information and possible updates. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.   Read the disclaimer
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