Ultracaine Injection

Ultracaine Injection is used for: Local or regional anesthesia, Local or regional analgesia

Local Anesthesia Local infiltration: 0.25%; may increase up to 175 mg (70 mL) OK Regional Anesthesia Sympathetic block 0.25%; 50-125 mg (20-50 mL) Retrobulbar block 0.75%; 15-30 mg (2-4 mL) Complete corneal anesthesia usually precedes onset of clinically acceptable external ocular muscle akinesia; determine readiness for surgery based on presence of akinesia rather than anesthesia alone Peripheral nerve block 0.25%; 12.5 -175 mg (5-70 mL) OR 0.5%: 25-175 mg (5-35 mL) Caudal block Use as a test dose before caudal epidural blocks when clinical conditions permit 0.25%; 15-30 mL (37.5-75 mg) OR 0.5%: 15-30 mL (75-150 mg) Lumbar epidural block Use as a test dose before lumbar epidural blocks when clinical conditions permit In obstetrics, use ONLY 0.5% and 0.25% concentrations; incremental doses of 3-5 mL of the 0.5% solution not exceeding 50-100 mg at any dosing interval are recommended Repeat doses should be preceded by a test dose containing epinephrine if not clinically contraindicated 0.25%; 10-20 mL (25-50 mg) OR 0.5%: 10-20 mL (50-100 mg) OR 0.75%: 10-20 mL (75-150 mg); for single-dose use; not for intermittent epidural technique or obstetrical anesthesia Acute pain Adult: Lumbar block in labour pain: 0.25% soln: 15-30 mg (6-12 mL); 0.375% soln: 22.5-45 mg (6-12 mL); 0.5% soln: 30-60 mg (6-12 mL). Alternatively, 0.1% soln: 10-15 mg (10-15 mL) per hr; 0.125% soln: 10-15 mg (8-12 mL) per hr via infusion. Caudal block in labour pain: 0.25% soln: 25-50 mg (10-20 mL); 0.375% soln: 37.5-75 mg (10-20 mL); 0.5% soln: 50-100 mg (10-20 mL).

Local Anesthesia <12 years: Not recommended; decreased dose by 30% in infants <6 mo, if necessary >12 years Local infiltration: 0.25%; may increase up to 2.5 mg/kg Regional Anesthesia <12 years: Limited date available; usual concentration <0.25% and dose decreased by 30% in infants <6 mo >12 years Sympathetic block 0.25%; 50-125 mg (20-50 mL) Peripheral nerve block 0.25%; 12.5 -175 mg (5-70 mL) OR 0.5%: 25-175 mg (5-35 mL) Caudal block Use as a test dose before caudal epidural blocks when clinical conditions permit 0.25%; 15-30 mg (37.5-75 mL) OR 0.5%: 15-30 mg (75-150 mL) Lumbar epidural block Use as a test dose before lumbar epidural blocks when clinical conditions permit In obstetrics, use ONLY 0.5% and 0.25% concentrations; incremental doses of 3-5 mL of the 0.5% solution not exceeding 50-100 mg at any dosing interval are recommended. Repeat doses should be preceded by a test dose containing epinephrine if not clinically contraindicated 0.25%; 10-20 mL (25-50 mg) OR 0.5%: 10-20 mL (50-100 mg) OR 0.75%: 10-20 mL (75-150 mg); for single-dose use; not for intermittent epidural technique or obstetrical anesthesia Retrobulbar block 0.75%; 15-30 mg (2-4 mL) Complete corneal anesthesia usually precedes onset of clinically acceptable external ocular muscle akinesia; determine readiness for surgery based on presence of akinesia rather than anesthesia alone

Renal impairment Pharmacokinetics not evaluated Substantially excreted by the kidneys; may increase bupivacaine exposure and risk of systemic toxicities in patients with renal impairment All severities: Use with caution; consider frequent monitoring for adverse reactions

Not for intrathecal use Epidural or caudal anesthesia: Avoid use of solutions containing antimicrobial preservatives (ie, multiple-dose vials) Avoid rapid injection of large volumes; use incremental doses when possible For major regional nerve blocks (eg, brachial plexus, lower extremity), an indwelling IV catheter should be placed to assure adequate IV access Closely monitor cardiovascular and respiratory (adequacy of oxygenation and ventilation) vital signs and level of consciousness after each local anesthetic injection Carefully restrict quantities in areas of body supplied by end arteries or having otherwise compromised blood supply (eg, digits, nose, external ear, penis)

Obstetrical paracervical block anesthesia. Its use in this technique has resulted in fetal bradycardia and death. Intravenous regional anesthesia (Bier Block). Known hypersensitivity to bupivacaine or to any local anesthetic agent of the amide-type or to other components of Bupivacaine Hydrochloride Injection/Bupivacaine Hydrochloride and Epinephrine Injection.

Risk of cardiac arrest in obstetrical anesthesia Injection only Cardiac arrest with difficult resuscitation or death reported during use for epidural anesthesia in obstetrical patients Most cases occurred following use of 0.75% (7.5 mg/mL) concentration Resuscitation has been difficult or impossible despite adequate preparation and appropriate management Cardiac arrest reported after convulsions resulting from systemic toxicity, presumably following unintentional intravascular injection Marcaine 0.75% concentration is not recommended for obstetrical anesthesia and should be reserved for surgical procedures where a high degree of muscle relaxation and prolonged effect are necessary Dose-Related Toxicity: Monitor cardiovascular and respiratory vital signs and patient’s state of consciousness after injection of Bupivacaine Hydrochloride Injection/Bupivacaine Hydrochloride and Epinephrine Injection. Methemoglobinemia: Cases of methemoglobinemia have been reported in association with local anesthetic use. See full prescribing information for more detail on managing these risks. Chondrolysis with Intra-Articular Infusion: Intra-articular infusions of local anesthetics including Bupivacaine Hydrochloride Injection following arthroscopic and other surgical procedures is an unapproved use, and there have been post-marketing reports of chondrolysis in patients receiving such infusions. Risk of Cardiac Arrest with Intravenous Regional Anesthesia Use (Bier Block): There have been reports of cardiac arrest and death during the use of bupivacaine for intravenous regional anesthesia (Bier Block). Allergic-Type Reactions to Sulfites in Bupivacaine Hydrochloride and Epinephrine Injection: Bupivacaine Hydrochloride and Epinephrine 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. Risk of Systemic Toxicities with Unintended Intravascular or Intrathecal Injection: Unintended intravascular or intrathecal injection may be associated with systemic toxicities, including CNS or cardiorespiratory depression and coma, progressing ultimately to respiratory arrest. Aspirate for blood or cerebrospinal fluid (where applicable) prior to each dose and consider using a test dose of Bupivacaine Hydrochloride and Epinephrine Injection.

Pregnancy Contraindicated for obstetrical paracervical block anesthesia; use has resulted in fetal bradycardia and death Data are unavailable on use in pregnant women to inform a drug-associated risks of adverse developmental outcomes Local anesthetics rapidly cross placenta, and when used for epidural, caudal, or pudendal block anesthesia, can cause varying degrees of maternal, fetal, and neonatal toxicity Incidence and degree of toxicity depend upon procedure performed, type, and amount of drug used, and technique of drug administration Adverse reactions in parturient, fetus, and neonate involve alterations of CNS, peripheral vascular tone, and cardiac function If this drug is used during pregnancy, or if patient becomes pregnant while taking this drug, inform patient of potential hazard to fetus Maternal hypotension Maternal hypotension has resulted from regional anesthesia; local anesthetics produce vasodilation by blocking sympathetic nerves The supine position is dangerous in pregnant women at term because of aortocaval compression by 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; elevating the patient’s legs will also help prevent decreases in blood pressure The fetal heart rate also should be monitored continuously and electronic fetal monitoring is highly advisable Animal data Embryofetal lethality was noted when administered SC to pregnant rabbits during organogenesis at clinically relevant doses Decreased pup survival was observed in rat pre-and postnatal developmental study at a dose level comparable to daily maximum recommended human dose on body surface area basis Advise pregnant women of potential risks to fetus Labor or delivery Epidural, caudal, or pudendal anesthesia may alter forces of parturition through changes in uterine contractility or maternal expulsive efforts. Epidural anesthesia has been reported to prolong the second stage of labor by removing the parturient’s reflex urge to bear down or by interfering with motor function The use of obstetrical anesthesia may increase the need for forceps assistance;the use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life; this has not been reported with bupivacaine It is extremely important to avoid aortocaval compression by the gravid uterus during administration of regional block to parturients; to do this, the patient must be maintained in the left lateral decubitus position or a blanket roll or sandbag may be placed beneath the right hip and gravid uterus displaced to the left Lactation Not studied in nursing mothers Bupivacaine can persist in plasma for up to 168 hr and benzyl alcohol, a Posimir excipient, for up to 12 hr after administration Bupivacaine and benzyl alcohol (in Posimir only) reported to be excreted in human milk Consider developmental and health benefits of breastfeeding along with mother’s clinical need for bupivacaine and any potential adverse effects on breastfed child from drug or underlying maternal condition Bupivacaine has been reported to be excreted in human milk suggesting that the nursing infant could be theoretically exposed to a dose of the drug; administer to lactating women only if clearly indicated Studies assessing the effects of the drug in breastfed children have not been performed; studies to assess the effect on milk production or excretion have not been performed

Local Anesthetics: The toxic effects of local anesthetics are additive. Monitor for neurologic and cardiovascular effects when additional local anesthetics are administered. Monoamine Oxidase Inhibitors and Tricyclic Antidepressants: Administration of Bupivacaine Hydrochloride and Epinephrine Injection to patients receiving monoamine oxidase inhibitors or tricyclic antidepressants may produce severe, prolonged hypertension. Concurrent use of these agents should generally be avoided. Ergot-Type Oxytocic Drugs: Concurrent administration of Bupivacaine Hydrochloride and Epinephrine Injection and ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents. Nonselective Beta-Adrenergic Antagonists: Administration of Bupivacaine Hydrochloride and Epinephrine Injection (containing a vasoconstrictor) in patients receiving nonselective beta-adrenergic antagonists may cause severe hypertension and bradycardia. Concurrent use of these agents should generally be avoided. Drugs Associated with Methemoglobinemia: Patients are at increased risk of developing methemoglobinemia when concurrently exposed to nitrates, nitrites, local anesthetics, antineoplastic agents, antibiotics, antimalarials, anticonvulsants, and other drugs. Potent Inhalation Anesthetics: Serious dose-related cardiac arrhythmias may occur if preparations containing a vasoconstrictor such as epinephrine are used in patients during or following the administration of potent inhalation anesthetics. Contraindicated (0) Serious (2) bupivacaine implant ponesimod

Side effects of Bupivacaine : CNS excitation may be followed by depression. Hypotension, bradycardia, arrhythmias and cardiac arrest; methaemoglobinaemia; seizures, restlessness, dizziness. Hypersensitivity. Prolonged block, Edema, Headache, Hypotension, Hypoventilation, Nausea, Nervousness, Palpitation, Respiratory arrest, Tachycardia, Tinnitus, Tremors, Vomiting Potentially Fatal: Cardiac and sudden respiratory arrest.

Bupivacaine blocks both the initiation and conduction of nerve impulses reducing the permeability of neuronal membranes to Na ions resulting in inhibition of depolarization w/ resultant blockade of conduction.

Ultracaine 0.5% Injection manufactured by Jayson Pharmaceuticals Ltd.. Its generic name is Bupivacaine. Ultracaine is availble in Bangladesh. Farmaco BD drug index information on Ultracaine Injection is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.