local anesthetics(slide show)
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y Are the second class of anaesthetics. They are also calledregional anaesthetics because they render a specificportion of the body insensitive to pain without major
reduction of CNS function and level of consciousness.y The most local anaesthetics belong to one of two major
groups of organic compounds, esters and amides, and areclassified as either topical and parenteral (injectable)anaesthetics. Topical anaesthetics are applied directly to
the skin and mucous membrane. They are available in theform of solutions, gel, cream or powder
y Parenteral anaesthetics can be administered intravenously or by various spinal injection techniques
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y Short-acting- last for 30 minutes to one hour.
Ex. Chloroprocaine, procaine(novocaine)
y Moderate-acting- one to three hours duration of Action
Ex. Lidocaine(xylocaine)
y Long-acting-last for three to ten hours
Ex. Bupivacaine(sensorcaine), tetracaine HCI(pontocaine)
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y Generic Name: Nesacaine®Brand Name: (chloroprocaine HCl) Injection, USP
y Nesacaine®-MPF(chloroprocaine HCl) Injection, USP
y INDICATIONSy Nesacaine (chloroprocaine) 1% and 2% Injections, in multidosevials
with methylparaben as preservative, are indicated for the production of local anesthesia by infiltration and peripheral nerve block. They arenot to be used for lumbar or caudal epidural anesthesia.
y Nesacaine (chloroprocaine) -MPF 2% and 3% Injections, in single dose vials without preservative and without EDTA, are indicated for theproduction of local anesthesia by infiltration, peripheral and centralnerve block, including lumbar and caudal epidural blocks.
y Nesacaine (chloroprocaine) and Nesacaine (chloroprocaine) -MPFInjections are not to be used for subarachnoid administration.
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y DOS A GE A ND A DMINISTRATIONy 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 andconcentration required to produce the desired result should beused. Dosage should be reduced for children, elderly anddebilitated patients and patients with cardiac and/or liverdisease.
y Caudal and Lumbar Epidural Block: In order to guard againstadverse experiences sometimes noted following unintendedpenetration of the subarachnoid space, the following proceduremodifications are recommended:
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y Use an adequate test dose (3 mL of Nesacaine(chloroprocaine) -MPF 3% Injection or 5 mL of Nesacaine (chloroprocaine) -MPF 2% Injection) priorto induction of complete block. This test dose shouldbe repeated if the patient is moved in such a fashion asto have displaced the epidural catheter. Allowadequate time for onset of anesthesia following
administration of each test dose.y Avoid the rapid injection of a large volume of local
anesthetic injection through the catheter. Considerfractional doses, when feasible.
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y Pediatric Dosage: It is difficult to recommend amaximum dose of any drug for children, since this varies asa 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 thechild's age and weight and should not exceed 11 mg/kg (5mg/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% aresuggested for infiltration and 1-1.5% for nerve block. Inorder to guard against systemic toxicity, the lowest effectiveconcentration and lowest effective dose should be used atall times.
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y SIDE EFFECTSy Central Nervous System R eactions: These are characterized by
excitation and/or depression.Restlessness, anxiety , dizziness, tinnitus, blurred vision or tremors may
occur, possibly proceeding to convulsions.y Cardiovascular System R eactions: High doses, or unintended
intravascular injection, may lead to high plasma levels and relateddepression of the myocardium, hypotension,bradycardia, and, possibly,cardiac arrest. Allergic: Allergic type reactions are rare and may occuras a result of sensitivity to the local anesthetic or to other formulationingredients, such as the antimicrobial preservative methylparaben,contained in multiple dose vials. These reactions are characterized by signs such as tachycardia, sneezing, nausea, vomiting,dizziness,excessive sweating, elevated temperature, andpossibly,(including severe hypotension).
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y Pharmacokinetics
y The rate of systemic absorption of local anesthetic drugs isdependent upon the total dose and concentration of drug
administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic injection. Epinephrineusually reduces the rate of absorption and plasmaconcentration of local anesthetics and is sometimes addedto local anesthetic injections in order to prolong the
duration of action.y The onset of action with chloroprocaine is rapid (usually
within 6 to 12 minutes), and the duration of anesthesia,depending upon the amount used and the route of administration, may be up to 60 minutes.
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Novocainy Generic Name:Procainey Brand Name: Novocainy Descriptiony
It is a white crystalline, odorless powder that is freely soluble in water,but less soluble in alcohol. Each mL contains 100 mg procainehydrochloride and 4 mg acetone sodium bisulfite as antioxidant
y Clinical Pharmacology y Novocain stabilizes the neuronal membrane and prevents the initiation
and transmission of nerve impulses, thereby effecting local anesthesia.Novocain lacks surface anesthetic activity. The onset of action is rapid(2 to 5 minutes) and the duration of action is relatively short (average1 to 1½ hours), depending upon the anesthetic technique, the type of block, the concentration, and the individual patient.
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y Indications and Usage for Novocain
y Novocain is indicated for spinal anesthesia.
y Contraindications
y Spinal anesthesia with Novocain is contraindicated inpatients with generalized septicemia: sepsis at the
proposed injection site; certain diseases of thecerebrospinal system, meningitis, syphilis; and aknown hypersensitivity to the drug.
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y A dverseR eactionsy Use of inappropriate doses or techniques may result in extensive spinal
blockade leading to hypotension and respiratory arrest.y A small number of reactions may result from hypersensitivity,
diminished tolerance to normal dosage.y CNS effects (nervousness, dizziness, blurred vision, tremors)
commonly represent the initial signs of local anesthetic systemictoxicity. However, these reactions may be very brief or absent in somepatients in which case the first manifestation of toxicity may bedrowsiness or convulsions merging into unconsciousness and
respiratory arrest.y Cardiovascular system reactions include depression of the
myocardium, hypotension (or sometimes hypertension), bradycardia,and even cardiac arrest.
y Allergic reactions are characterized by cutaneous lesions of delayedonset,edema, and other manifestations of allergy.
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Generic Name: Lidocaine hydrochloride
Brand Name: Xylocaine
y Indications and Usage for Lidocaine
y Lidocaine Hydrochloride Injection, is indicated for production of local or regionalanesthesia by infiltration techniques such as percutaneous injection and
intravenous regional anesthesia by peripheral nerve block techniques such asbrachial plexus and intercostal and by central neural techniques.
y Dosages
y ADULTS:50-100mg(1 to 1.5mg/kg)by I.V. Bolus at 25-50 mg/minute.
y CHILDREN: 1 mg/kg by I.V. Bolus.
y Elderly pt.: reduce dosage and rate of infusion by 50%.
y A dministrationy Injection(addictive syringes and single use vials)containing 40, 100, or 200mg/ml
are for the preparation of I.V. Infusion solutions only and must be diluted beforeuse.
y Use a more concentrated solution of up to 8mg/ml if pt. Is fluid restricted.
y Avoid giving injections containing preservative
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y A dverse R eactions
y CNS: confusion, restlessness, tremor, lethargy, anxiety,
hallucinations, nervousness, seizures.y CV : hypotension, bradycardia, cardiac arrest.
y GI: vomiting.
y R espiratory: respiratory depression and arrest.
y SKIN: soreness and injection site
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y CONTRAINDICATIONS & CA UTIONSy Contraindicated in pt. Hypersensitive to the amide type of local
anesthetics.y
Use cautiously and at reduced dosages in pt. With complete orsecond degree heart block, in elderly pt. , in those with heartfailure or renal or hepatic disease, and in those weighing lessthan 50kg(110 lb.)
y NUR SING CONSIDERATIONS
y Give I.M. Injections in the deltoid muscle only.y Monitor drug level. Therapeutic levels are 2-5 mcg/ml.y Monitor patients response, especially blood pressure and
electrolytes. Notify prescriber promptly if abnormalities develop.
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Generic Name: Bupivacaine
Brand Name: sensorcainey Indicationy Bupivacaine Spinal is indicated for the production of
subarachnoid block (spinal anesthesia).
y Contraindicationsy contraindicated in patients with a known hypersensitivity to it or
to any local anesthetic agent of the amide-type.
y The following conditions preiclude the use of spinal anesthesia:y Severe hemorrhage, severe hypotension or shock and such as
complete heart block, which severely restrict cardiac output.y Local infection at the site of proposed lumbar puncture.y Septicemia.
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y A dverseR eactionsy Respiratory System: Respiratory paralysis or underventilation may be noted as
a result of upward extension of the level of spinal anesthesia and may lead tosecondary hypoxic cardiac arrest if untreated. Preanesthetic medication,
intraoperative analgesics and sedatives, as well as surgical manipulation, may contribute to underventilation.y Cardiovascular System: Hypotension due to loss of sympathetic tone is a
commonly encountered extension of the clinical pharmacology of spinalanesthesia. Nausea and vomiting are frequently associated with hypotensiveepisodes following the administration of spinal anesthesia. High doses, orinadvertent intravascular injection, may lead to high plasma levels and relateddepression of the myocardium, decreased cardiac output, bradycardia, heart
block, and, possibly, cardiac arrest.y High doses or inadvertent intravascular injection may lead to high plasma
levels and related central nervous system toxicity characterized by excitementand/or depression. Restlessness, anxiety, dizziness,blurred vision or tremorsmay occur, possibly proceeding to convulsions.
y Nausea and vomiting may occur during spinal anesthesia.
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y Management of Local Anesthetic Emergencies: Thefirst consideration is prevention, best accomplished by
careful and constant monitoring of cardiovascular andrespiratory vital signs and the patients state of consciousness after each local anesthetic injection. Atthe first sign of change, oxygen should beadministered.
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y Bupivacaine Dosage and A dministrationy The dose of any local anesthetic administered varies with the
anesthetic procedure, the area to be anesthetized, the vascularityof thetissues, 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 producethe desired result should be administered. Dosages of BupivacaineSpinal (Bupivacaine in Dextrose Injection,) should be reduced forelderly and debilitated patients and patients with cardiac and/or liverdisease.
y Obstetrical Use: Doses as low as 6 mg Bupivacaine hydrochloride havebeen used for vaginal delivery under spinal anesthesia. The dose rangeof 7.5 mg to 10.5 mg (1 mL to 1.4 mL) Bupivacaine hydrochloride hasbeen used for Cesarean section under spinal anesthesia.
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Generic Name: tetracaine HCI
Brand Name: Pontocaine
y Tetracaine is a local anesthetic (numbing medication).It works by blocking nerve signals in your body.
y
Tetracaine topical cream or ointment is used to reducepain or discomfort caused by minor skin irritations,cold sores or fever blisters, sunburn or other minorburns, insect bites or stings, and many other sources of
minor pain on a surface of the body.
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y Important informationy An overdose of numbing medications can cause fatal side effects if too much of
the medicine is absorbed through your skin and into your blood. This is morelikely to occur when using a numbing medicine without the advice of a medical
doctor (such as during a cosmetic procedure like laser hair removal). Overdosesymptoms may include uneven heartbeats, seizure (convulsions), coma, slowedbreathing, or respiratory failure (breathing stops). Your body may absorb moreof this medication if you use too much, if you apply it over large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skin that is cutor irritated may also absorb more topical medication than healthy skin.
y Use the smallest amount of this medication needed to numb the skin or relievepain. Do not use large amounts of tetracaine topical, or cover treated skin areas
with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.
y Do not use this medication if you are allergic to tetracaine or other numbingmedicines such as lidocaine, benzocaine, or prilocaine.
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y Indications and dosage
y Do not use the medication in larger or smaller amounts, or use it for longer thanrecommended.
y Your body may absorb more of this medication if you use too much, if you apply it overlarge skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skinthat is cut or irritated may also absorb more topical medication than healthy skin.
y Use the smallest amount of medicine needed to numb the skin or relieve pain. Do not uselarge amounts of tetracaine topical, or cover treated skin areas with a bandage or plastic
wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.
y This medication comes with instructions for safe and effective application. Follow thesedirections carefully. Ask your doctor or pharmacist if you have any questions.
y To treat minor skin conditions, apply a thin layer of tetracaine topical to the affected areaup to 4 times per day.
y Do not use tetracaine topical to treat large skin areas or deep puncture wounds. Avoidusing the medicine on skin that is raw or blistered, such as a severe burn or abrasion.
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y side effectsy Get emergency medical help if you have any of these signs of an allergic reaction: hives;
difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using tetracainetopical and call your doctor at once if you have any of these serious side effects:
y severe burning, stinging, or sensitivity where the medicine is applied;y swelling, warmth, or redness;y oozing, blistering, or any signs of infection; ory eye irritation, watering, or increased sensitivity to light.y Rare but serious side effects may include:y nervousness, dizziness, blurred vision;y drowsiness, feeling like you might pass out;y breathing problems;y fast or slow heart rate; andy weak pulse, fainting, slow breathing (breathing may stop).y Less serious side effects may include:y mild stinging, burning, or itching where the medicine is applied;y skin tenderness or redness; ory dry white flakes where the medicine was applied.
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y A dministrationy Use this medication exactly as directed on the label, or as it has been prescribed by your
doctor. Do not use the medication in larger or smaller amounts, or use it for longer thanrecommended.
y Your body may absorb more of this medication if you use too much, if you apply it over
large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skinthat is cut or irritated may also absorb more topical medication than healthy skin.y Use the smallest amount of medicine needed to numb the skin or relieve pain. Do not use
large amounts of tetracaine topical, or cover treated skin areas with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.
y This medication comes with instructions for safe and effective application. Follow thesedirections carefully. Ask your doctor or pharmacist if you have any questions.
y To treat minor skin conditions, apply a thin layer of tetracaine topical to the affected areaup to 4 times per day.
y Do not use tetracaine topical to treat large skin areas or deep puncture wounds. Avoidusing the medicine on skin that is raw or blistered, such as a severe burn or abrasion.