INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION
LENAPAIN TABLETS

SCHEDULING STATUS:
S2

PROPRIETARY NAME
(and dosage form:)

LENAPAIN TABLETS

COMPOSITION:
Each tablet contains:

Doxylamine Succinate	5,00 mg
Codeine Phosphate	10,00 mg
Caffeine, Anhydrous	30,00 mg
Paracetamol	450,00 mg

PHARMACOLOGICAL CLASSIFICATION:
A - 2.9 : Special analgesic combination

PHARMACOLOGICAL ACTION:
Lenapain tablets have analgesic, antipyretic and antihistaminic action.

INDICATIONS:
Relief of mild to moderate pain associated with tension.

CONTRA-INDICATIONS:
Sensitivity to any of the ingredients. The dosage in renal functional impairment must be reduced. Should be taken only with caution by asthmatics. Severe liver function impairment. Lenapain should not be administered to patients with acute intermittent porphyria. Asthma, respiratory depression especially in the presence of cyanosis and excessive bronchial secretion, head injuries and conditions in which intracranial pressure is raised, heart failure secondary to chronic lung disease, a history of cardiac disease, epilepsy, and all convulsive states, patients taking monoamine oxidase inhibitors or within 14 days of stopping such treatment, acute alcoholism. Lenapain should not be taken during pregnancy, nor whilst breast-feeding.

WARNINGS:
Dosages in excess of those recommended may cause severe liver damage. Patients suffering from liver or kidney disease should take Paracetamol under medical supervision. Consult your doctor if no relief is obtained with the recommended dosage. This medicine may lead to drowsiness and impaired concentration, which may be aggravated by simultaneous intake of alcohol or other central nervous system depressant agents. Patients should be warned against taking charge of vehicles or machinery and performing potentially hazardous tasks where loss of concentration may lead to accidents. Do not use continuously for longer than 10 days without consulting your doctor.
KEEP OUT OF REACH OF CHILDREN.

DOSAGE AND DIRECTIONS FOR USE:
Adults: One to two tablets every 4 to 6 hours. Do not exceed 8 tablets per day.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Doxylamine Succinate
The most common side-effect is sedation, varying from slight drowsiness to deep sleep, and including lassitude, dizziness and in-coordination. Other side-effects include gastro-intestinal disturbances such as nausea, vomiting, diarrhoea or constipation, anorexia or increased appetite and epigastric pain. Doxylamine succinate may also produce antimuscarinic effects including blurred vision, difficulty in micturition, dysuria, dryness of the mouth and tightness of the chest. Other central effects include hypotension, muscular weakness, tinnitus, euphoria or depression, headache, irritability and nightmares.
Paradoxical central nervous system stimulation may occur with insomnia, nervousness, tachycardia, tremors and convulsions. Doxylamine succinate may precipitate epileptiform seizures in patients with local lesions of the cerebral cortex.
Allergic reactions and cross-sensitivity to related medicines my occur. Blood disorders, including agranulocytosis, leucopenia and haemolytic anaemia have been reported.
Special Precautions:
Doxylamine should be used with care in the elderly, and in conditions such as closed-angle glaucoma, urinary retention, liver impairment, prostatic hypertrophy or pyloroduodenal obstruction.
Use with care in cardiac failure, hypertension, oedema and cardiovascular disease.
Interactions:
Doxylamine succinate may enhance the sedative effects of central nervous system depressants including alcohol, tricyclic antidepressants, barbiturates, hypnotics, narcotic analgesics, sedatives and tranquillisers. Monoamine oxidase (MAO) inhibitors may enhance the antimuscarinic effects of doxylamine succinate, and it has additive effects with other antimuscarinic agents, such as atropine and tricyclic antidepressants. It has been suggested that doxylamine succinate could mask the warning signs of damage caused by ototoxic medicines such as aminoglycoside antibiotics.
Codeine Phosphate
The most common side-effects are nausea, vomiting, constipation, drowsiness and confusion, tolerance usually develops with long-term use, but not to constipation. Micturition may be difficult and there may be ureteric or billiary spasm as well as an antidiuretic effect. Dry mouth, facial flushing, vertigo, bradycardia, palpitations, orthostatic hypotension, hypothermia, restlessness, changes of mood, hallucinations and miosis may occur. These effects are more common in ambulant patients and in those without severe pain. Raised intracranial pressure occurs in some patients. Its euphoric activity has led to abuse. A dose-related histamine-releasing effect which may be responsible in part for reactions such as urticaria, pruritis as well as hypotension and flushing may occur.
Interactions:
Monoamine oxidase (MAO) inhibitors or within 14 days of taking such a treatment. The depressant effects of codeine are enhanced by depressants such as alcohol, anaesthetics, hypnotics, sedatives, tricyclic antidepressants and phenothiazines. The gastro-intestinal effects may delay absorption as with mexiletine or may be counteractive as with metoclopramide.
Caffeine Anhydrous
Gastro-intestinal irritation including nausea, vomiting, abdominal pain, diarrhoea and gastro-intestinal bleeding, insomnia, headache, anxiety, restlessness, dizziness and palpitations.
Paracetamol
Haematological reactions including thrombocytopenia, leucopenia, pancytopenia, neutropenia, angranulocytosis and anaemia have been reported. Pancreatitis, skin rashes and other allergic reactions, hepatitis, renal colic, renal failure and sterile pyuria occur occasionally.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Doxylamine Succinate component
In children central nervous system stimulation, resulting in ataxia, excitement, tremors, psychoses, hallucinations and convulsions, occurs. Hyperpyrexia may also occur. Deepening coma and cardiorespiratory collapse may follow. Death may occur from respiratory failure. In adults, central nervous system depression is more common, with drowsiness, coma and convulsions, progressing to respiratory failure or possible cardio-vascular collapse.
Treatment:
Treatment is supportive and symptomatic.
Codeine Phosphate component
Large doses may cause excitement and convulsions, respiratory depression and hypotension with circulatory failure and deepening coma. Rhabdomyolysis progressing to renal failure has been reported in overdosage. Death may occur from respiratory failure. Toxic doses vary considerably with the individual and regular users may tolerate large doses. The threat of coma, pinpoint pupils and respiratory depression is considered indicative of overdosage, dilation of the pupils occurs as hypoxia develops. Pulmonary oedema after overdosage is a common cause of fatalities among addicts.
Treatment:
In acute poisoning, the stomach should be emptied. A laxative may be given to aid peristalsis. Intensive supportive therapy may be required to correct respiratory failure and shock. In addition a specific antagonist, naloxone hydrochloride, is used to counteract very rapidly the severe respiratory depression and coma produced by excessive doses of opioid analgesics. A dose of 0,4 to 2 mg is given by intravenous injection, repeated at intervals of 2 to 3 minutes if necessary, up to 10 mg. Naloxone may also be given by subcutaneous injection, intra-muscular injection or by intravenous infusion. The effect of naloxone may be of shorter deviation than that of the opioid analgesic and additional doses may be required to prevent relapses. Nalorphine and Levallorphan have also been used to antagonise adverse effects of opioid analgesics. These antagonists may induce withdrawal symptoms in persons physically dependent on morphine related analgesics.
Caffeine Anhydrous component
Severe overdosage or idiosyncrasy may lead to maniacal behaviour, diuresis and repeated vomiting with extreme thirst, tremor, delirium, hyperthermia, tachycardia, tachypnoea, electrolyte disturbances, convulsions and death. Severe toxicity may not be preceded by milder symptoms.
Treatment:
In cases of overdosage, consult a doctor immediately. Treatment is supportive and symptomatic.
Paracetamol component
Symptoms of paracetamol overdosage in the first 24 hours are pallor, increased sweating, nausea, vomiting, diarrhoea, anorexia and abdominal pain. Liver damage may become apparent 12 to 48 hours after ingestion. Abnormalities of glucose metabolism and metabolic acidosis may occur. In severe poisoning, hepatic failure may progress to encephalopathy, convulsions, respiratory depression, coma, cerebral oedema, coagulation defects, gastro-intestinal bleeding, disseminated intravascular coagulation, hypoglycaemia, metabolic acidosis, cardiac arrhythmia and cardiovascular collapse may occur. Acute renal failure with tubular necrosis may develop even in the absence of severe liver damage.
Treatment:
Prompt treatment is essential in the management of paracetamol overdosage. Any patient who has ingested about 7,5 g or more in the preceding 4 hours should undergo gastric lavage. The plasma or serum-paracetamol concentration should be determined as soon as possible, but no sooner than 4 hours after ingestion. Generally, treatment is required if the paracetamol concentration is higher than a line [the '200' line] drawn on semi-log/linear paper joining the points 200 mg per litre [1.32 mmol per litre] at 4 hours and 30 mg per litre [0,20 mmol per litre] at 15 hours. Acetylcysteine is given either intravenously or by mouth and tends to be preferred to methionine which is given by mouth to increase glutathione stores and stimulate the nontoxic metabolism of paracetamol.
Acetylcysteine should be started as soon as possible, preferably within 8 hours of overdosage. Oral treatment is usually given for 72 hours and intravenous therapy for 20 hours [up to 48 hours]. It has been suggested that the 72 hour oral regimen may be more effective than the 20 hour IV regimen if the treatment is delayed.

IV:	An initial dose of 150 mg/kg in 200 mL glucose injection, given intravenously over 15 minutes, followed by an intravenous infusion of 50 mg/kg in 500 mL glucose injection over the next 4 hours and then 100 mg/kg in 1000 mL over the next 16 hours. The volume of intravenous fluids should be modified for children.
Orally:	140 mg/kg as a 5 % solution initially, followed by a 70 mg/kg solution every 4 hours for 17 doses. Acetylcysteine is effective if administered within 8 hours of overdosage.

IDENTIFICATION:
A yellow, circular, flat, bevelled-edged tablet, scored on one side.

PRESENTATION:
Blister packs of 18 tablets.
Securitainers of 100 and 500 tablets.

STORAGE INSTRUCTIONS:
Store below 25°C. Protect from light.
Exposure to air should be MINIMUM.
KEEP OUT OF REACH OF CHILDREN

REGISTRATION NUMBER:
Q/2.9/0301

NAME AND BUSINESS ADDRESS OF APPLICANT:
PHARMACARE LIMITED
7 Fairclough Road
Korsten
Port Elizabeth
6020

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
April 1998

D372
A&S PRINTERS

Current: February 2004
Source: Community Pharmacy
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