BUPIVACAINE HYDROCHLORIDE

(byoo-piv'a-kane)
Marcaine, Sensorcaine
Classifications: CENTRAL NERVOUS SYSTEM AGENT; LOCAL ANESTHETIC (AMIDE-TYPE)
Prototype: Procaine
Pregnancy Category: C

Availability

0.25%, 0.5%, 0.75% injection

Actions
Anesthetic of the amide type. Decreases sodium flux into nerve cell, inhibiting initial
depolarization, and prevents propagation and conduction of the nerve impulse. Progression of
anesthesia, related to diameter, myelination, and conduction velocity of affected fibers is
manifested clinically as sequential loss of nerve function. May stimulate or depress the CNS or
do both.

Therapeutic Effects

Primary depressant effect is in medulla and higher centers affecting patient's reaction to pain,
temperature, and touch, as well as proprioception and skeletal muscle tone.

Uses

Infiltration anesthesia; peripheral, sympathetic nerve, and epidural (including caudal) block
anesthesia; 0.75% bupivacaine solution in dextrose is used for spinal anesthesia.

Contraindications

Known sensitivity to bupivacaine, local anesthetics, other amide-type anesthetics. Parabens, or

metabisulfites; acidosis; heart block; severe hemorrhage; hypotension and shock; hypertension,
cerebrospinal diseases; obstetrical paracervical anesthesia or spinal anesthesia in septicemia;
topical or IV regional anesthesia; intercurrent use with chloroprocaine; history of malignant
hyperthermia. Safety during pregnancy (category C) other than during labor, lactation, or
children <12 y is not established.

Cautious Use

Older adults or debilitated patients; hepatic or renal disease; known drug allergies and
sensitivities; dysrhythmias; children >12 y; obstetrical delivery.
Route & Dosage
Infiltration Anesthesia
Adult: IM Local infiltration, sympathetic block 0.25% solution; Lumbar epidural 0.25%, 0.5%, 0.75%
solutions; Caudal block, peripheral nerve block 0.25%, 0.5% solutions; Retrobulbar block 0.75%
solution
Child: IM 1–3.7 mg/kg

Administration
Intramuscular

 Inject slowly with frequent aspirations to avoid intravascular injection.

Intrathecal

 Do not use preparations containing preservatives for epidural or spinal anesthesia.

 Do not use multiple-dose vial for lumbar or caudal epidural block.
 Store ampuls at 15°–30° C (59°–86° F); protect from freezing. Solutions with epinephrine should
be protected from light.

INCOMPATIBILITIES Solution/additive: Sodium bicarbonate

Adverse Effects ( 1%)

Body as a Whole: Hypersensitivity [cutaneous lesions, urticaria, sneezing, diaphoresis, syncope,
hyperthermia, angioneurotic edema (including laryngeal edema), anaphylaxis, anaphylactoid
reaction]. CNS: Nervousness, unusual anxiety, excitement, dizziness, drowsiness, tremors, convulsions,
unconsciousness, respiratory arrest. Special Senses: Pupillary constriction; blurred or double vision;
tinnitus. GI: Nausea, vomiting. Other: Inflammation or sepsis at injection site, chills, pupillary
constriction. Associated with Epidural Anesthesia, Body as a Whole: Total spinal block, persistent
analgesia, paresthesia. Urogenital: Urinary retention, fecal incontinence, loss of perineal sensation and
sexual function. Other: Slowing of labor, increased incidence of forceps delivery, cranial nerve palsies
(with inadvertent intrathecal injection).

Interactions
Drug: CNS DEPRESSANTS augment CNS depression; with isoproterenol, ergonovine there is persistent
hypertension and a risk of CVA if bupivacaine used with epinephrine. MAO INHIBITORS, TRICYCLIC
ANTIDEPRESSANTS, PHENOTHIAZINES cause severe or prolonged hypotension or hypertension if
bupivacaine used with epinephrine.

Pharmacokinetics
Onset: 4–17 min for epidural, caudal, peripheral, or sympathetic block; within 1 min for spinal
block. Duration: 3–5 h for epidural, caudal, peripheral, or sympathetic block; 1.25–2.5 h for spinal
block. Distribution: Crosses placenta. Metabolism: Metabolized in liver. Elimination: 6% excreted
unchanged in urine. Half-Life: 1.5–5.5 h in adults, 8.1 h in neonates.

Nursing Implications

Assessment & Drug Effects

 Monitor for signs of inadvertent intravascular injection, which can produce a transient
"epinephrine response" (increased heart rate or systolic BP or both, circumoral pallor,
palpitations, nervousness) within 45 seconds in the unsedated patient and an increase by 20
bpm or more in heart rate for at least 15 seconds in sedated patient.
 Vasoconstrictor-containing solution should be administered cautiously, if at all, to areas with
end arteries (e.g., digits, penis) or to areas that have a compromised blood supply; ischemia and
gangrene can result. Inspect areas for evidence of reduced perfusion because of vasospasm:
pale, cold, sensitive skin.
 Note: Systemic reactions (toxicity) are more apt to occur in children or older adults and may
develop rapidly or be delayed for as long as 30 min after administration.
 Monitor for toxicity: CNS stimulation (unusual anxiety, excitement, restlessness) usually occurs
first, followed by CNS depression (drowsiness, unconsciousness, respiratory arrest). However,
because stimulation is apt to be transient or absent, drowsiness may be the first sign in some
patients (especially children and older adults).
 Monitor BP and fetal heart rate continuously during labor because maternal hypotension may
accompany regional anesthesia. Place mother on left side with legs elevated.
 Monitor cardiac and respiratory status continuously in patients receiving retrobulbar and dental
blocks.

Patient & Family Education

 After spinal anesthesia, sensation to lower extremities may not return for 2.5–3.5 h.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications
in SMALL CAPS;   Canadian drug name;   Prototype drug

LIDOCAINE HYDROCHLORIDE 
(lye'doe-kane)
Anestacon, Dilocaine, L-Caine, Lidoderm, Lida-Mantle, Lidoject-1, LidoPen Auto
Injector, Nervocaine, Octocaine, Xylocaine, Xylocard 
Classifications: CARDIOVASCULAR AGENT; ANTIARRHYTHMIC, CLASS IB; CENTRAL NERVOUS SYSTEM
AGENT; LOCAL ANESTHETIC (AMIDE TYPE)
Pregnancy Category: B

Availability

Antidysrhythmic 300 mg/3 mL auto-injector; 0.2%, 0.4%, 0.8%, 1%, 2%, 4%, 10%, 20%
injections

Local Anesthetic 0.5%, 1%, 1.5%, 2%, 4%

Topical 2%, 2.5%, 4%, 5% solution; 2.5%, 5% ointment; 0.5%, 4% cream; 0.5%, 2.5% gel;
0.5%, 10% spray; 2% jelly; 0.5% patch

Actions

Similar to those of procainamide and quinidine, but has little effect on myocardial contractility,
AV and intraventricular conduction, cardiac output, and systolic arterial pressure in equivalent
doses. Exerts antiarrhythmic action (Class IB) by suppressing automaticity in His-Purkinje
system and by elevating electrical stimulation threshold of ventricle during diastole. Action as
local anesthetic is more prompt, more intense, and longer lasting than that of procaine.

Therapeutic Effects

Suppresses automaticity in His-Purkinje system and elevates electrical stimulation threshold of

ventricle during diastole. Prompt, intense, and long-lasting local anesthetic.

Uses

Rapid control of ventricular arrhythmias occurring during acute MI, cardiac surgery, and cardiac
catheterization and those caused by digitalis intoxication. Also as surface and infiltration
anesthesia and for nerve block, including caudal and spinal block anesthesia and to relieve local
discomfort of skin and mucous membranes. Patch for relief of pain associated with post-herpetic
neuralgia.

Unlabeled Uses

Refractory status epilepticus.

Contraindications

History of hypersensitivity to amide-type local anesthetics; application or injection of lidocaine

anesthetic in presence of severe trauma or sepsis, blood dyscrasias, supraventricular arrhythmias,
Stokes-Adams syndrome, untreated sinus bradycardia, severe degrees of sinoatrial,
atrioventricular, and intraventricular heart block. Safe use during pregnancy (category B),
lactation, or in children is not established.

Cautious Use

Liver or kidney disease, CHF, marked hypoxia, respiratory depression, hypovolemia, shock;
myasthenia gravis; debilitated patients, older adults; family history of malignant hyperthermia
(fulminant hypermetabolism). Topical use in eyes, over large body areas, over prolonged
periods, in severe or extensive trauma or skin disorders.

Route & Dosage

Ventricular Arrhythmias
Adult: IV 50–100 mg bolus at a rate of 20–50 mg/min, may repeat in 5 min, then start infusion of 1–4
mg/min immediately after first bolus IM/SC 200–300 mg IM,  may repeat once after 60–90 min
Child: IV 0.5–1 mg/kg bolus dose, then 10–50 mcg/kg/min infusion

Anesthetic Uses
Adult: Infiltration 0.5–1% solution Nerve Block 1–2% solution Epidural 1–2% solution Caudal 1–1.5%
solution Spinal 5% with glucose Saddle Block 1.5% with dextrose Topical 2.5–5% jelly, ointment,
cream, or solution

Post-Herpetic Neuralgia
Adult: Topical Apply up to 3 patches over intact skin in most painful areas once for up to 12 h per 24 h
period

Administration
Intramuscular

 Give in deltoid muscle as preferred site.

Topical

 Do not apply topical lidocaine to large areas of skin or to broken or abraded surfaces. Consult
physician about covering area with a dressing.
 Avoid topical preparation contact with eyes.

Intravenous

 Note: Do not use lidocaine solutions containing preservatives for spinal or epidural (including
caudal) block. Use ONLY lidocaine HCl injection without preservatives or epinephrine that is
specifically labeled for IV injection or infusion.
PREPARE: Direct: Give undiluted.  IV Infusion: • Use D5W for infusion. For adults, add 1 g to
250 or 500 mL to yield 2 or 4 mg/mL, respectively; for children, add 120 mg to 100 m to yield
1.2 mg/mL.• Do not use solutions with particulate matter or discoloration. 

ADMINISTER: Direct: Give at a rate of 50 mg or fraction thereof over 1 min.  IV Infusion: Use

microdrip and infusion pump. Rate of flow is usually  4 mg/min.  

INCOMPATIBILITIES Solution/additive: Phenytoin, ampicillin, cefazolin. Y-site: Amphoterici
n B cholesteryl complex, phenytoin, thiopental.

 Discard partially used solutions of lidocaine without preservatives.

Adverse Effects ( 1%)

CNS: Drowsiness, dizziness, light-headedness, restlessness, confusion, disorientation, irritability,
apprehension, euphoria, wild excitement, numbness of lips or tongue and other paresthesias including
sensations of heat and cold, chest heaviness, difficulty in speaking, difficulty in breathing or swallowing,
muscular twitching, tremors, psychosis. With high doses: convulsions, respiratory depression and
arrest. CV: With high doses, hypotension, bradycardia, conduction disorders including heart
block, cardiovascular collapse, cardiac arrest. Special Senses: Tinnitus, decreased hearing; blurred or
double vision, impaired color perception. Skin: Site of topical application may develop erythema,
edema. GI: Anorexia, nausea, vomiting. Body as a Whole: Excessive perspiration, soreness at IM site,
local thrombophlebitis (with prolonged IV infusion), hypersensitivity reactions (urticaria, rash,
edema, anaphylactoid reactions).

Diagnostic Test Interference

Increases in creatine phosphokinase (CPK) level may occur for 48 h after IM dose and may
interfere with test for presence of MI.

Interactions
Drug: Lidocaine patch may increase toxic effects of tocainide, mexiletine; BARBITURATES decrease
lidocaine activity; cimetidine, BETA BLOCKERS, quinidine increase pharmacologic effects of
lidocaine; phenytoin increases cardiac depressant effects; procainamide compounds neurologic and
cardiac effects.

Pharmacokinetics
Absorption: Topical application is 3% absorbed through intact skin. Onset: 45–90 sec IV; 5–15 min
IM; 2–5 min topical. Duration: 10–20 min IV; 60–90 min IM; 30–60 min topical; >100 min injected for
anesthesia. Distribution: Crosses blood–brain barrier and placenta; distributed into breast
milk. Metabolism: Metabolized in liver. Elimination: Excreted in urine. Half-Life: 1.5–2 h.
Nursing Implications

Assessment & Drug Effects

 Stop infusion immediately if ECG indicates excessive cardiac depression (e.g., prolongation of PR
interval or QRS complex and the appearance or aggravation of arrhythmias).
 Monitor BP and ECG constantly; assess respiratory and neurologic status frequently to avoid
potential overdosage and toxicity.
 Auscultate lungs for basilar rales, especially in patients who tend to metabolize the drug slowly
(e.g., CHF, cardiogenic shock, hepatic dysfunction).
 Watch for neurotoxic effects (e.g., drowsiness, dizziness, confusion, paresthesias, visual
disturbances, excitement, behavioral changes) in patients receiving IV infusions or with high
lidocaine blood levels.
 Note: Lidocaine blood levels of 1.5–6 mcg/mL are reported to provide "usually effective"
antiarrhythmic activity. Blood levels greater than 7 mcg/mL are potentially toxic.

Patient & Family Education

 Swish and spit out when using lidocaine solution for relief of mouth discomfort; gargle for use in
pharynx, may be swallowed (as prescribed).
 Oral topical anesthetics (e.g., Xylocaine Viscous) may interfere with swallowing reflex.
Do NOT ingest food within 60 min after drug application; especially pediatric, geriatric, or
debilitated patients. Do not chew gum while buccal and throat membranes are anesthetized to
prevent biting trauma.
 Do not breast feed while taking this drug without consulting physician.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications
in SMALL CAPS;   Canadian drug name;   Prototype drug

TETRACAINE HYDROCHLORIDE
(tet'ra-kane)
Pontocaine
Classifications: CENTRAL NERVOUS SYSTEM AGENT; LOCAL ANESTHETIC (ESTER TYPE)
Prototype: Procaine HCl
Pregnancy Category: C

Availability

1%, 0.2%, 0.3% injection; 20 mg powder; 2% solution; 1%, 2% cream; 2% gel; 1% ointment;
0.5% ophthalmic solution
Actions

Local anesthetic that depresses the initial depolarization phase of the action potential, thus
preventing propagation and conduction of the nerve impulse. Local anesthetic approximately 10
times more potent and toxic than procaine.

Therapeutic Effects

Indicated by loss of sensation and motor activity in circumscribed body areas close to injection
or application site.

Uses

Spinal anesthesia (high, low, saddle block) and topically to produce surface anesthesia. Eye: To
anesthetize conjunctiva and cornea prior to superficial procedures (including tonometry,
gonioscopy, removal of foreign bodies or sutures, corneal scraping). Nose and Throat: To
abolish laryngeal and esophageal reflexes prior to bronchoscopy, esophagoscopy. Skin: To
relieve pruritus, pain, burning.

Contraindications

Older adult and debilitated patients; prolonged use of ophthalmic preparations; known
hypersensitivity to tetracaine or other local anesthetics of ester type (e.g., procaine,
chloroprocaine, cocaine) or to PABA or its derivatives; infection at application or injection site.

Cautious Use

Shock; cachexia, cardiac decompensation; lactation. Safety during pregnancy (category C) or in

children is not established.

Route & Dosage

Local Anesthesia
Adult: Topical Before procedure, 1–2 drops of 0.5% solution or 1.25–2.5 cm of ointment in lower
conjunctival fornix or 0.5% solution or ointment to nose or throat Spinal 1% solution diluted with equal
volume of 10% dextrose injected in subarachnoid space

Administration
Topical

 Avoid use of solutions that are cloudy, discolored, or crystallized.

  When tetracaine is used on mucosa of larynx, trachea, or esophagus, the manufacturer
recommends adding 0.06 mL of a 0.1% epinephrine solution to each mL tetracaine solution to
slow absorption of the anesthetic.
 Store ophthalmic solution and ointment at 15°–30° C (59°–86° F); refrigerate topical. Avoid
freezing. Use tight, light-resistant containers.

Adverse Effects ( 1%)

Body as a Whole: Anaphylactic reactions, convulsions, faintness, syncope. CNS: Postspinal
headache, headache, spinal nerve paralysis, anxiety, nervousness, seizures. CV: Bradycardia,
arrhythmias, hypotension. Special Senses: Stinging; corneal erosion, retardation or prevention of
healing of corneal abrasion, transient pitting and sloughing of corneal surface, dry corneal epithelium;
dry mucous membranes, prolonged depression of cough reflex.

Interactions
Drug: May antagonize effects of SULFONAMIDES.

Pharmacokinetics
Onset: 1 min eye; 3 min mucosal surface; 3 min spinal. Duration: Up to 15 min eye; 30–60 min
mucosal surface; 1.5–3 h spinal. Metabolism: Metabolized in liver and plasma. Elimination: Excreted
in urine.

Nursing Implications

Assessment & Drug Effects

 Recovery from anesthesia to the pharyngeal area is complete when patient has feeling in the
hard and soft palates and when muscles in the faucial (tonsillar) pillars contract with stimulation.
 Do not give food or liquids until these normal pharyngeal responses are present (usually about 1
h after anesthetic administration). The first small amount of liquid (water) should be given under
supervision of care provider.
 Be aware that increased blood concentration of the drug may result from excess application of
tetracaine to the skin (to relieve pruritus or burning), application to debrided or infected skin
surfaces, or too rapid injection rate.
 High blood concentrations of tetracaine can lead to adverse systemic effects involving CNS and
CV systems: Convulsions, respiratory arrest, dysrhythmias, cardiac arrest.

Patient & Family Education

 Do not use ophthalmic drug longer than prescribed period. Prolonged use to eye surface may
cause corneal epithelial erosions and retard healing of corneal surface.
 Natural barriers to eye infection and injury are removed by the anesthesia. Do not rub eye after
drug instillation until anesthetic effect has dissipated (evidenced by return of blink reflex).
Patching for temporary protection of the corneal epithelium may be ordered.
 Wash or disinfect hands before and after self-administration of solutions or ointment.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications
in SMALL CAPS;   Canadian drug name;   Prototype drug

ROPIVACAINE HYDROCHLORIDE
(ro-piv'i-cane)
Naropin
Classifications: CENTRAL NERVOUS SYSTEM AGENT; LOCAL ANESTHETIC (ESTER-TYPE)
Prototype: Procaine HCl
Pregnancy Category: B

Availability

2 mg/mL, 5 mg/mL, 7.5 mg/mL, 10 mg/mL injection

Actions

Blocks the generation and conduction of nerve impulses, probably by increasing the threshold for
electrical excitability.

Therapeutic Effects

Local anesthetic action produces loss of sensation and motor activity in areas of the body close to
the injection site.

Uses

Local and regional anesthesia, postoperative pain management, anesthesia/pain management for
obstetric procedures.

Contraindications

Hypersensitivity to ropivacaine or any local anesthetic of the amide type; generalized septicemia,
inflammation or sepsis at the proposed injection site; cerebral spinal diseases (e.g., meningitis);
heart block, hypotension, hypertension, GI hemorrhage.

Cautious Use

Pregnancy (category B), lactation, debilitated, older adult, or acutely ill patients; arrhythmias,
shock.
Route & Dosage
Surgical Anesthesia
Adult: Epidural 25–200 mg (0.5–1% solution) Nerve block 5–250 mg (0.5%, 0.75% solution)

Labor Pain
Adult: Epidural 20–40 mg (0.2% solution)

Postoperative Pain Management

Adult: Epidural 12–20 mg/h (0.2% solution) Infiltration 2–200 mg (0.2–0.5% solution)

Administration
Intrathecal

 Avoid rapid injection of large volumes of ropivacaine. Incremental doses should always be used
to achieve the smallest effective dose and concentration.
 Use an infusion concentration of 2 mg/mL (0.2%) for postoperative analgesia.
 Do not use disinfecting agents containing heavy metal ions (e.g., mercury, copper, zinc, etc.) on
skin insertion site or to clean the ropivacaine container top.
 Discard continuous infusions solution after 24 h; it contains no preservatives.
 Store unopened at 20°–25° C (68°–77° F).

Adverse Effects ( 1%)

Body as a Whole: Pain, fever, rigors, hypoesthesia. CNS: Paresthesia, headache, dizziness,
anxiety. CV: Hypotension, bradycardia, hypertension, tachycardia, chest pain, fetal
bradycardia. GI: Nausea. Skin: Pruritus. Urogenital: Urinary retention,
oliguria. Hematologic: Anemia.

Interactions
Drug: Additive adverse effects with other LOCAL ANESTHETICS.

Pharmacokinetics
Onset: 1–30 min (average 10–20 min) depending on dose/route of administration. Duration: 0.5–8 h
depending on dose/route of administration. Distribution: 94% protein
bound. Metabolism: Metabolized in the liver by CYP1A. Elimination: Excreted in urine. Half-
Life: 1.8–4.2 h.

Nursing Implications

Assessment & Drug Effects

 Monitor carefully cardiovascular and respiratory status throughout treatment period. Assess for
hypotension and bradycardia.
  Report immediately S&S of CNS stimulation or CNS depression.

Patient & Family Education

 Report any of the following to physician immediately: restlessness, anxiety, tinnitus, blurred
vision, tremors.
 Do not breast feed without consulting physician.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications
in SMALL CAPS;   Canadian drug name;   Prototype drug