Benzocaine Chemical Properties
 

Benzocaine  Description
Benzocaine (ethyl p-aminobenzoate) is used topically by itself or in combination with menthol or phenol in nonprescription dosage forms such as gels, creams, ointments, lotions, aerosols, and lozenges to relieve pain or irritation caused by such conditions as sunburn, insect bites, toothache, teething, cold sores or canker sores in or around the mouth, and fever blisters. Benzocaine is a lipophilic local anesthetic agent with a short duration of action.
Like most amino ester-type local anesthetics, it is easily hydrolyzed by plasma cholinesterase. Because of its low pKa, however, it is un-ionized under most physiological conditions and, therefore, can only bind to the lipid side of the local anesthetic receptor. It also can easily cross membranes into systemic circulation to cause systemic toxicities. Furthermore, being a PABA derivative, it has similar allergenic properties to procaine and is contraindicated with sulfonamide antibacterial agents.


Benzocaine  Chemical Properties
white odourless crystals


Benzocaine  Fuction
1.   Benzocaine is used as an anesthetic (local).
2.    ocal and topical anesthetic used in products such as burn and sunburn remedies, hemorrhoidal creams, suppositories, creams for treatment of poison ivy, oral and gingival products, sore-throat sprays/lozenges, astringents, appetite suppressants, callus and wart remedies, athlete's-foot remedies, toothache- and denture-irritation products.
3.      Apply to a maximum of three to four times a day to the affected area, as directed by the physician.


Benzocaine  Uses

1.     Benzocaine is a local anaesthetic of the ester type with a poor solubility in water. The drug benzocaine is normally used as a topical pain reliever or as a common ingredient in cough drops. Benzocaine is used in multiple forms including lotion, gel, liquid, lozenges, and sprays. When 2.     2.    Benzocaine is applied in any form it temporarily numbs or blocks the nerve endings, which leads to a decreases in the amount of pain. It is used in cattle, sheep, swine and horses for local and prolonged low epidural anaesthesia. Standard therapeutic doses of benzocaine ranged from 150 to 750 mg per animal. Benzocaine is also currently used as surface anaesthetic as ointments (0.5% benzocaine) for wounds and ulcerated surfaces in horses, cattle and sheep applied twice a day until healing.
3.     A commonly used topical pain reliever. Main active ingredient in anesthetic ointments.
Anesthetic;Na+ channel blocker
4.     Benzocaine acts on the central nervous system, cardiovascular system, neuromuscular junctions and ganglion synapse. Its mechanism of action is to prevent the generation and conduction of the nerve impulse. Local anaesthetics block conduction by decreasing or preventing the large transient increase in the permeability of excitable membranes to Na+ that is produced by a slight depolarisation. This action of local anaesthetics is due to their direct interaction with voltage-sensitive Na+ channels. Benzocaine is mainly hydroxylated in the metabolite para-aminobenzoic acid (PABA) that inhibits the action of sulphonamides.
5.       Benzocaine is distributed in the body, crosses the placenta and is metabolised in the liver and in the plasma by non-specific cholinesterases. 6.     Benzocaine and its main metabolite (para-aminobenzoic acid) are excreted into urine.
7.       Benzocaine appears as a moderately toxic compound after single administration. The acute intraperitoneal LD50 value was 216 mg/kg bw in mice. Benzocaine may induce methemoglobinemia in several species such as sheep, cats and dogs.


What is Benzocaine?

Benzocaine is a fat soluble surface anaesthetic. Compared with several other local anesthetics such as lidocaine, tetracaine, etc., the strength of effect is small. Owing to its playing role in mucosal, people feel comfort. It is a fat soluble and strong drug, therefore it is easy to combine with the lipid layer of the mucosa or skin, but not easily go through the human body to produce toxic.


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