U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 11 - 20 of 21 results

Status:
US Approved OTC
Source:
21 CFR 346.10(i) anorectal:local anesthetic tetracaine hydrochloride
Source URL:
First marketed in 1932

Class (Stereo):
CHEMICAL (ACHIRAL)



Tetracaine (INN, also known as amethocaine; trade name Pontocaine. Ametop and Dicaine) is a potent local anesthetic of the ester group. It is mainly used topically in ophthalmology and as an antipruritic, and it has been used in spinal anesthesia. Tetracaine blocks sodium ion channels required for the initiation and conduction of neuronal impulses thereby affecting local anesthesia. In biomedical research, tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. Tetracaine is an allosteric blocker of channel function. At low concentrations, tetracaine causes an initial inhibition of spontaneous calcium release events, while at high concentrations, tetracaine blocks release completely.
Status:
US Approved OTC
Source:
21 CFR 346.10(c) anorectal:local anesthetic dibucaine
Source URL:
First marketed in 1930
Source:
Dibucaine; Nupercaine by Society of Chemical Industry in Basle, Basle, Switzerland (Ciba Company, Inc., New York, distributor).
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Dibucaine is used as a local anesthetic for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. Dibucaine is used to temporarily relieve pain and itching due to: hemorrhoids or other anorectal disorders, sunburn, minor burns, minor cuts; scrapes, insect bites, minor skin irritation. This drug acts via blocking of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions through sodium channel blocking. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
Status:
US Approved OTC
Source:
21 CFR 346.10(a) anorectal:local anesthetic benzocaine
Source URL:
First marketed in 1895
Source:
Americaine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Benzocaine is a local anesthetic. It acts by blocking voltage-gated sodium ion channels in nerve endings. Benzocaine is available over-the counter for local anesthesia of oral and pharyngeal mucous membranes (sore throat, cold sores, mouth ulcers, toothache, sore gums, denture irritation), otic pain, and as a local anesthetic for surgical or diagnostic procedures. As a spray, benzocaine is used for temporary relief of pain and itching associated with minor burns, sunburn, minor cuts or scrapes, insect bites, or minor skin irritations. Topical application of benzocaine to gums or mouth may cause rare, but serious and potentially fatal adverse effect methemoglobinemia.
Status:
US Approved Allergenic Extract (1941)
First marketed in 1921

Class (Stereo):
CHEMICAL (ACHIRAL)


There is not much information about ammonium phenolate. It is known, that this a salt of phenol and it is toxic if swallowed and is toxic in contact with skin.
Status:
US Previously Marketed
First approved in 1999

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Levobupivacaine (CHIROCAINE®) is a (S)-enantiomer of bupivacaine and it is related chemically and pharmacologically to the amino amide class of local anesthetics. Local anesthetics block the generation and the conduction of nerve impulses by increasing the threshold for electrical excitation in the nerve, by slowing 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. Levobupivacaine (CHIROCAINE®) is a safer alternative for regional anesthesia than bupivacaine. It demonstrated less affinity and strength of depressant effects onto myocardial and central nervous vital centers in pharmacodynamic studies, and a superior pharmacokinetic profile.
Status:
US Previously Marketed
First approved in 1976

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Etidocaine, marketed under the trade name Duranest, is a local anesthetic given by injection during surgical procedures and labor and delivery. Etidocaine has a long duration of activity, and the main disadvantage of using during dentistry is increased bleeding during surgery. Etidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.
Status:
US Previously Marketed
Source:
ethyl chloride/ethylene
(1923)
Source URL:
First marketed in 1921
Source:
Ethyl Chloride U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ethyl chloride is a colourless flammable gas at ordinary temperature and pressure. It has a characteristic ether-like odour and a burning taste. Ethyl chloride is used as a chemical intermediate, in solvents, aerosols, and anaesthesia. Currently, chloroethane is largely used as a blowing agent in foamed plastics. In the past, chloroethane was used in the production of tetraethyl lead, an anti-knock additive to leaded gasoline. Chloroethane has also been used in the production of ethyl cellulose and for miscellaneous applications including use as a solvent, for phosphorus, sulfur, fats, oils, resins and waxes; in insecticides; and as an ethylating agent in the manufacture of dyes and drugs, refrigerant, and topical anaesthetic and use in the manufacture of dyes, chemicals, and pharmaceuticals. Other uses of chloroethane are as a pulp vitality tester in dentistry, as a medication to alleviate pain associated with insect burns and stings, as an adjunct in the treatment of tinea lesions and creeping eruptions, and as a counterirritant for relief of myofacial and visceral pain syndromes. Chloroethane is also used as a solvent, as a refrigerant, and in the production of ethyl cellulose, dyes, medicinal drugs, and other commercial chemicals. It is also used to numb skin prior to medical procedures such as ear piercing and skin biopsy, and in sports injuries.
Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Butanilicaine (Hostacain) is a local anesthetic. It uses may associate with a risk of allergy. Butanilicaine has a vasodilator effect.

Showing 11 - 20 of 21 results