(and dosage form):
Each 5 mL contains 10 mg oxethazaine (N,N-bis-(N-methyl-N-phenyl-1-butylacetamido)-beta-hydroxyethylamine) in alumina gel containing aluminium hydroxide (Al(OH)3) 291 mg, magnesium hydroxide (Mg(OH)2) 98 mg, sodium benzoate 0,45% and benzoic acid 0,05% as preservatives.
Category A,11.4.3 - Antacids - Other
Alumina gel and magnesium hydroxide react chemically to neutralize or buffer existing quantities of acid, but have no direct effect on its production. This action increases gastric pH.
Gastroscopic observations reveal that alumina gel, especially when swallowed undiluted, forms a diffuse coating over the inflamed gastric mucosa for a variable period of time. Because of this adherent vehicle; oxethazaine exerts a prolonged topical anaesthetic action.
Oxethazaine is a topical anaesthetic, which, when applied to the mucous membranes produces a more potent anaesthesia of longer duration than either cocaine hydrochloride or lidocaine hydrochloride.
In vitro, oxethazaine produces antispasmodic action on smooth muscle. It antagonises the action of serotonin on smooth muscle as demonstrated on isolated rabbit jejunum strips. The clinical relevance of this effect is not known.
Studies have shown that a small amount of aluminium from aluminium hydroxide is absorbed from the intestine. Approximately 10% of the magnesium in magnesium hydroxide is absorbed from the intestine.
After oral administration of 20 mg oxethazaine contained in 10 mL of alumina gel with magnesium hydroxide, the peak oxethazaine plasma level was approximately 20 ng/mL and occurred about one hour after dosing.
Oxethazaine undergoes rapid and extensive biotransformation resulting in a short plasma half-life of approximately one hour. Less than 0,1% unchanged oxethazaine was recovered in the urine within 24 hours. Major metabolites were beta-hydroxy-mephentermine and beta-hydroxy-phentermine. Mephentermine and phentermine appeared in the plasma in pharmacologically insignificant amounts and their cumulative 24-hour urinary excretion was less than 0,1% of the dose administered.
MUCAINE acts as an antacid in dyspepsia and is used for the symptomatic relief of hyperacidity associated with peptic ulceration, gastritis, oesophageal reflux with heartburn and gastric hyperacidity. MUCAINE may be of benefit if symptomatic relief could not be obtained with antacid therapy alone.
Do not use this product if you are presently taking a prescription antibiotic drug containing any form of tetracycline.
This medicine should not be given to any patient who has demonstrated a sensitivity to it.
The use of aluminium- or magnesium-containing antacids is contra-indicated in patients with symptoms of appendicitis since these medicines may increase the danger of perforation or rupture due to their constipating or laxative effects. The use of aluminium-containing antacids (except those containing aluminium phosphate) is contra-indicated in patients with hypophosphataemia due to the phosphate binding properties of aluminium salts.
The use of magnesium-containing antacids is contra-indicated in patients with severe renal function impairment due to increased danger of occurrence of hypermagnesaemia.
Safety in pregnancy and lactation has not been established.
DOSAGE AND DIRECTIONS FOR USE:
Shake well before use. The recommended adult oral dose is one to two 5 mL measures, four times daily, 15 minutes before meals and at bedtime. Do not exceed the recommended dosage. MUCAINE suspension should preferably be taken undiluted; however, if desired, it may be followed by a sip of water. The maximum dose recommended may be decreased following adequate control of the symptoms.
Adequate diagnostic studies are recommended. The possibility of gastrointestinal carcinoma should be considered in patients with protracted or recurrent indigestion.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
If the dose of MUCAINE exceeds 60 mL per day, some patients may experience dizziness, faintness or drowsiness.
Sensitivity reactions including skin eruptions (dermatitis, urticaria), pruritus, glossitis, angioedema and collapse have been reported.
Magnesium-containing antacids may cause diarrhoea. Aluminium-containing antacids may cause constipation.
The use of magnesium-containing antacids in patients with mild to moderate renal impairment should be carefully monitored due to a possible increased danger of hypermagnesaemia.
In patients with chronic renal failure, hyperaluminaemia may occur. Encephalopathy and dementia may occur in patients with poor renal function or patients on dialysis, due to an increase in plasma concentration of aluminium.
Hypophosphataemia may occur with prolonged administration or large doses of aluminium-containing antacids (except aluminium phosphate) especially in patients with an inadequate dietary intake of phosphorus.
Laboratory Tests Serum phosphate levels should be monitored at monthly or bi-monthly intervals in patients on maintenance haemodialysis who are receiving chronic antacid therapy.
Use in children The safety and effectiveness of MUCAINE in children has not been established.
Drug Interactions The rate and/or extent of absorption of many medicines may be increased or decreased. Therefore, medication should not be taken within one to two hours of MUCAINE.
An incomplete list of substances for which the above statement has been shown to apply includes: tetracycline, iron salts, isoniazid, ethambutol, some anti-muscarinic drugs, benzodiazepines, phenothiazines ranitidine, indomethacin, phenytoin, nitrofurantoin, Vitamin A, fluoride and phosphate. An increase in the plasma level of quinidine and possible toxicity may result it alkalisation of the urine occurs following antacid therapy.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Treatment is symptomatic and supportive.
Clear, white, viscous suspension, having a characteristic mint odour, free from foreign odour and taste.
Amber glass bottles of 100 mL, 200 mL and 500 mL.
Keep bottle tightly closed in a cool (below 25°C) place, but keep from freezing. Protect from direct sunlight. Keep out of reach of children.
NAME AND BUSINESS ADDRESS OF APPLICANT:
Akromed Products (Pty) Ltd.
20 Spanner Road
Trademark and product under licence from
WYETH-AYERST LABORATORIES, USA.
DATE OF PUBLICATION OF THIS PACKAGE INSERT:
7 February 1994
Updated on this site: February 2002
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