Dibucaine

343.46

343.46

201-632-1

L6JW2TJG99

159055

DTXSID3045271

C28984

Colorless or almost colorless powder

C - Cardiovascular system|D - Dermatologicals|N - Nervous system|S - Sensory organs

2933499090

54.5

4.2

Solid

1.1±0.1 g/cm3

64 °C

491.5±55.0 °C at 760 mmHg

251.1±31.5 °C

1.549

68.01mg/L(temperature not stated)

Odorless

8.85None

8.85

196.2 Ų [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]

BITTER, ACRID TASTE; PROLONGED ANESTHETIC ACTION WHEN APPLIED TO TONGUE /DIBUCAINE HYDROCHLORIDE/|Somewhat hygroscopic.

22-41

26-39

GD3150000

Xn

SENSITIVE TO LIGHT

P261, P264, P270, P272, P273, P280, P301+P312, P302+P352, P305+P351+P338, P310, P321, P330, P333+P313, P363, P391, P501

H302

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

|Danger|H302 (95%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P280, P301+P312, P305+P351+P338, P310, P330, and P501|Aggregated GHS information provided by 40 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Subcutaneous LD50 in rat is 27 mg/kg. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.

... DURATION OF ACTION /OF SPINAL ANESTHESIA/ ... MAY BE INCREASED ... BY ADDING EPINEPHRINE TO THE SOLUTION. /LOCAL ANESTHETICS/|BY DECREASING THE RATE OF ABSORPTION, /EPINEPHRINE/ NOT ONLY LOCALIZES THE ANESTHETIC AT THE DESIRED SITE BUT ALSO ALLOWS THE RATE AT WHICH IT IS DESTROYED IN THE BODY TO KEEP PACE WITH THE RATE AT WHICH IT IS ABSORBED INTO THE CIRCULATION. THIS REDUCES ITS SYSTEMIC TOXICITY. /LOCAL ANESTHETICS/

LD50 Mouse ip 24,500 ug/kg|LD50 Mouse sc 28,500 ug/kg|LD50 Rabbit sc 8500 ug/kg|LD50 Rabbit iv 2500 ug/kg

For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.

Anesthetics, Local|MOST POTENT, MOST TOXIC, & LONGEST-ACTING OF COMMONLY EMPLOYED LOCAL ANESTHETICS. ACTS LIKE COCAINE WHEN APPLIED TO MUCOUS MEMBRANES BUT IS SEVERAL TIMES MORE ACTIVE. ...ACTS LIKE PROCAINE OR COCAINE WHEN INJECTED...MORE ACTIVE THAN PROCAINE...INJECTED SC & ABOUT 5 TIMES MORE TOXIC THAN COCAINE WHEN INJECTED IV. /HCL/|DIBUCAINE, A QUINOLINE DERIVATIVE ... IS NOW RARELY USED. ... ONSET OF ACTION IS RELATIVELY SLOW (UP TO 15 MIN); DURATION OF SPINAL ANESTHESIA IS 3-4 HR, BUT THIS CAN BE PROLONGED UP TO 6 HR BY ADDITION OF EPINEPHRINE.|Epidural anesthesia can be performed in the sacral hiatus (caudal anesthesia) or in the lumbar, thoracic, or cervical regions of the spine. /Local anesthetics/|For more Therapeutic Uses (Complete) data for DIBUCAINE (6 total), please visit the HSDB record page.

Topical dibucaine preparations should not be used in or near the eyes. The preparations should not be used in large quantities, especially over denuded surfaces or blistered areas. Topical dibucaine preparations are not intended for prolonged or extensive use. If dibucaine preparations are used for self-medication and the condition worsens or symptoms persist for more than 7 days or clear and occur again within a few days, the drug should be discontinued and a physician consulted. If rectal bleeding occurs during use of dibucaine ointment for pain, itching, and burning of hemorrhoids or if rash, irritation, swelling, pain, bleeding, or other symptoms develop or increase during use of dibucaine preparations, the drug should be discontinued and a physician consulted. Dibucaine should not be used in individuals with known hypersensitivity to the drug or other amide-type local anesthetics.|Some commercially available rectal and topical formulations of dibucaine contain acetone sodium bisulfite, a sulfite that may cause allergic-type reactions, including anaphylaxis and life-threatening or less severe asthmatic episodes, in certain susceptible individuals.|... AGENTS OF THE AMIDE TYPE ARE ESSENTIALLY FREE OF ... /HYPERSENSITIVITY/ PROBLEM ... /AMIDE LOCAL ANESTHETICS/|ANIMALS WITH EXPTL PRODUCED HEPATIC DAMAGE ARE MUCH MORE SUSCEPTIBLE TO TOXIC ACTIONS OF LOCAL ANESTHETICS, SO THAT EXTENSIVE USE OF LOCAL ANESTHETIC IN PT WITH SEVERE HEPATIC DAMAGE SHOULD PERHAPS BE AVOIDED. /LOCAL ANESTHETICS/

Dibucaine is an amide-type local anesthetic, similar to lidocaine.

Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. (See all compounds classified as Anesthetics, Local.)

In general, ionized forms (salts) of local anesthetics are not readily absorbed through intact skin. However, both nonionized (bases) and ionized forms of local anesthetics are readily absorbed through traumatized or abraded skin into the systemic circulation.|THE DRUG IS PARTIALLY METABOLIZED & A PORTION IS ELIMINATED UNCHANGED.|... RADIOACTIVE /SPINAL/ LOCAL ANESTHETICS ARE CONCN WITHIN SPINAL NERVE ROOTS AS WELL AS POSTERIOR & LATERAL COLUMNS OF SPINAL CORD. ... RATE OF ENZYMATIC HYDROLYSIS OF LOCAL ANESTHETIC AGENTS BY SPINAL FLUID IS SLOW. /LOCAL ANESTHETICS/|DURATION ... DEPENDS UPON RATE @ WHICH DRUG IS REMOVED FROM CEREBROSPINAL FLUID & FROM NERVE ROOTS WHERE IT EXERTS ITS ACTION. /LOCAL ANESTHETICS/|AT AUTOPSY, DIBUCAINE WAS DEMONSTRATED FROM UPPER SPINAL CORD (3.11 MUG/0.1 G), LOWER SPINAL CORD (7.15 MUG/0.1 G), LIVER (0.299 MUG/1.0 G) & KIDNEY (0.181 MUG/1.0 G).

Primarily hepatic.|METABOLISM OF AMIDE-LINKED LOCAL ANESTHETICS IS MORE COMPLEX /THAN ESTER TYPES/ ...

Local anesthetics block both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions through sodium channel inhibition. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.|... PREVENT THE GENERATION & THE CONDUCTION OF THE NERVE IMPULSE. THEIR PRIMARY SITE OF ACTION IS THE CELL MEMBRANE. ... BLOCK CONDUCTION BY DECREASING OR PREVENTING THE TRANSIENT INCREASE IN THE PERMEABILITY OF EXCITABLE MEMBRANES TO NA IONS THAT IS NORMALLY PRODUCED BY A SLIGHT DEPOLARIZATION ... /LOCAL ANESTHETICS/|AS ANESTHETIC ACTION PROGRESSIVELY DEVELOPS IN A NERVE, THE THRESHOLD FOR ELECTRICAL EXCITABILITY GRADUALLY INCREASES, THE RATE OF RISE OF THE ACTION POTENTIAL DECLINES, IMPULSE CONDUCTION SLOWS, & THE SAFETY FACTOR FOR CONDUCTION DECREASES; THESE FACTORS DECREASE PROBABILITY OF PROPAGATION OF THE ACTION POTENTIAL, AND NERVE CONDUCTION FAILS. /LOCAL ANESTHETICS/|... CAN BLOCK K ION CHANNELS. ... BLOCKADE OF CONDUCTION IS NOT ACCOMPANIED BY ANY LARGE OR CONSISTENT CHANGE IN RESTING MEMBRANE DUE TO BLOCK OF K ION CHANNELS. /LOCAL ANESTHETICS/|... SITE AT WHICH LOCAL ANESTHETICS ACT, AT LEAST IN THEIR CHARGED FORM, IS ACCESSIBLE ONLY FROM THE INNER SURFACE OF THE MEMBRANE. ... LOCAL ANESTHETICS APPLIED EXTERNALLY FIRST MUST CROSS THE MEMBRANE BEFORE THEY CAN EXERT A BLOCKING ACTION. /LOCAL ANESTHETICS/|... ACT ON ANY PART OF NERVOUS SYSTEM & ON EVERY TYPE OF NERVE FIBER. /LOCAL ANESTHETICS/

DIBUCAINE HCL CAUSED PHOTOALLERGIC DERMATITIS IN 13-YR-OLD GIRL WHEN USED AS LOCAL ANESTHETIC IN TREATMENT OF DENTAL CARIES.|A 2-year-old child apparently ingested dibucaine hydrochloride (0.5% Nupercainal Cream), acted strangely, staggered, then seized, became cyanotic, vomited, developed a cardiorespiratory arrest, and died. /Dibucaine hydrochloride/

Cincain

NUPERCAINAL (CIBA), TOPICAL: CREAM 0.5% WITH ACETONE SODIUM BISULFITE 0.37% IN 1.5 OZ CONTAINERS; OINTMENT 1% WITH ACETONE BISULFITE 0.5% IN 1 & 2 OZ CONTAINERS; AEROSOL SPRAY 0.25% WITH ALCOHOL 46% IN 6 OZ CONTAINERS; SUPPOSITORIES 2.5 MG /DIBUCAINE HCL/|BUCACET (LEMMON): EACH LOZENGE CONTAINS DIBUCAINE HCL 0.5 MG & CETALKONIUM CHLORIDE 4 MG. /DIBUCAINE HCL/|Grade: NF|Also available as the hydrochloride.

A SPECTROPHOTOMETRIC TEST /FOR ATYPICAL CHOLINESTERASE/ WAS DEVELOPED BY KALOW & GENEST (1957) WHICH INCL DIBUCAINE AS AN INHIBITOR...MADE IT POSSIBLE TO IDENTIFY TYPE OF ESTERASE PRESENT IN TEST SERA...ALSO...TO DETECT HETEROZYGOUS CARRIERS OF /ATYPICAL ESTERASE/ TRAIT.|...toxicity resulted in its removal from the U.S. market as an injectable preparation ... It is currently available as a cream and an ointment for use on the skin.

QUANTITATIVE DETERMINATIION OF DIBUCAINE HCL IN SPINAL ANESTHETIC (NEO-PERCAMINE S) BY HIGH-SPEED LIQ CHROMATOGRAPHY.|GAS CHROMATOGRAPHIC-MASS SPECTROMETRIC DETERMINATION OF DIBUCAINE IN WATER.|FLUORIMETRIC DETERMINATIOIN OF DIBUCAINE.

GAS CHROMATOGRAPHIC-MASS SPECTROMETRIC DETERMINATION OF DIBUCAINE IN PLASMA, LIVER, KIDNEY, & SPINAL CORD.|GAS CHROMATOGRAPHIC-MASS SPECTROMETRIC DETERMINATION OF DIBUCAINE IN BLOOD SERUM.

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