PHARMACOLOGICAL CLASSIFICATION: Category A,11.4.3- Antacids - Other
PHARMACOLOGICAL ACTION: Oxethazaine is a topical anaesthetic. A dilute solution of oxethazaine hydrochloride applied to mucous membranes produces anaesthesia of longer duration than either cocaine hydrochloride or lignocaine hydrochloride. A solution of 0,0005% oxethazaine hydrochloride induces anaesthesia of rabbit cornea for the same duration as a 0,25% solution of cocaine hydrochloride, a 1% solution of lignocaine hydrochloride, or a 2% solution of procaine hydrochloride. The high potency of oxethazaine permits clinical use of dilute solutions; a 0,2% concentration of oxethazaine in alumina gel is therapeutically effective. In vitro oxethazaine produces an antispasmodic action on smooth muscle. It antagonizes the action of histamine serotonin, physostigmine and barium sulphate on smooth muscle. In vivo, with a balloon in a dogs duodenum, oxethazaine hydrochloride given intravenously does not affect the motility of the intestine nor does it inhibit the action of neostigmine bromide on this motility.
A wide margin of safety exists between the effective dose of oxethazaine in alumina gel and the oral toxic dose of this compound. In mice, the oral LD50 of oxethazaine is approximately 400 mg of base per kg; when suspended in alumina gel as a vehicle the oral LD50 in mice is 1012 mg of base per kg. The effective dose, five or ten mL, contains 10 or 20 mg of oxethazaine respectively; this is only 0,2 or 0,4 mg per kg of body mass for a human weighing 50 kg. In humans, toxic effects have not been observed on continued ingestion of recommended therapeutic doses.
INDICATIONS: For the treatment of chronic oesophagitis without stricture, chronic gastritis, peptic ulcer, the irritable bowel syndrome and heartburn of pregnancy.
Symptoms of oesophageal or gastric irritation are usually relieved in patients who do not respond to antacid therapy.
CONTRA-INDICATIONS: Previous hypersensitivity to oxethazaine.
DOSAGE AND DIRECTIONS FOR USE: The recommended adult dose is 2 to 4 tablets four times daily 15 minutes before meals and at bedtime. The tablets should not be chewed but swallowed with water.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS: Adequate diagnostic studies are recommended. The possibility of gastro-intestinal carcinoma should be considered in patients with protracted or recurrent indigestion. If the dose of this product exceeds 24 tablets per day some patients may experience dizziness, faintness or drowsiness.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT: Treatment is symptomatic and supportive.
CONDITIONS OF REGISTRATION: To be determined by the Council.
IDENTIFICATION: MUCAINE* tablets are white, round, flat and bevelled.
PRESENTATION: Boxes of 50 tablets, each tablet individually sealed in cellophane.
STORAGE DIRECTIONS: Store in a cool (below 25°C), dry place.
Keep out of reach of children.
REFERENCE NUMBER: E 1224 (Act 101/1965)
NAME AND BUSINESS ADDRESS OF APPLICANT: AKROMED PRODUCTS (PTY) LTD.
(Co. Reg. no. 05/13586/07)
Electron Avenue, ISANDO 1600
* Registered Trademark.
* Under licence from
WYETH-AYERST LABORATORIES, U.S.A.
DATE OF PUBLICATION OF THIS PACKAGE INSERT: August 1972
* Registered Trademark Davbar Dbn.