Paracetamol ................................. 325 mg
Chlorpheniramine maleate ............... 2 mg
Excipients: q.s ……………………………. 1 tablet
Effervescent granules.
Product description: Orange, dry, loose granules with an aroma.
Box of 24 sachets x 1.5 g.
ATC code: N02B E51
Paracetamol is an antipyretic analgesic. The mechanism of action is probably similar to that of aspirin and dependant on the inhibition of prostaglandin synthesis. This inhibition appears, however to be on a selective basis.
Clinical efficacy: In two dental pain studies, pain relief was observed at a median time of 15 minutes following administration of the 1000 mg dose of paracetamol. Paracetamol demonstrated superior pain relief at 1000 mg dose compared to placebo. Paracetamol at the 500 mg dose also demonstrated superior efficacy compared to placebo.
Chlorpheniramine is a potent histamine H1, receptor antagonist.
Antihistamines diminish or abolish the actions of histamine in the body by competitive reversible blockade of histamine H1-receptor sites on tissues. Chlorpheniramine also has anticholinergic activity.
Antihistamines act to prevent the release of histamine, prostaglandins and leukotrienes and have been shown to prevent the migration of inflammatory mediators. The actions of chlorpheniramine include inhibition of histamine on smooth muscle, capillary permeability and hence reduction of oedema and wheal in hypersensitivity reactions such as allergy and anaphylaxis.
Paracetamol is rapidly and almost completely absorbed from the gastrointestinal tract. The concentration in plasma reaches a peak in 30 to 60 minutes and the plasma half-life is 1 - 4 hours after therapeutic doses. Paracetamol is relatively uniformly distributed throughout most body fluids. Binding of the drug to plasma proteins is variable; 20 to 30% may be bound at the concentrations encountered during acute intoxication. Following therapeutic doses 90 - 100% of the drug may be recovered in the urine within the first day. However, practically no paracetamol is excreted unchanged and the bulk is excreted after hepatic conjugation.
Chlorpheniramine is readily absorbed from the GI tract, following oral administration. The effects develop within 30 minutes, are maximal within 1 to 2 hours and last 4 to 6 hours. The plasma half-life is estimated to be 12 - 15 hours.
There is significant plasma protein binding. The drug is largely inactivated in the liver and excreted as metabolites in the urine. Chlorpheniramine is metabolised to the monodesmethyl and didesmethyl derivative. About 22% of an oral dose is excreted unchanged in the urine. Only trace amounts have been found in the faeces.
The anticholinergic properties of chlorpheniramine may cause drowsiness, dizziness, blurred vision and psychomotor impairment which can seriously hamper the patient's ability to drive and use machinery.
Pregnancy
Epidemiological studies in human pregnancy have shown no ill effects due to paracetamol used in the recommended dosage, but patients should follow the advice of their doctor regarding its use.
There are no adequate data from the use of chlorphenamine maleate in pregnant women. The potential risk for humans is not known. Use during the third trimester may result in reactions in the newborn or premature neonates. Not to be used during pregnancy unless considered essentially by a physician.
Breast-feeding
Paracetamol is excreted in breast milk but not in a clinically significant amount in recommended dosages. Available published data do not contraindicate breastfeeding.
Chlorpheniramine maleate and other antihistamine may inhibit lactation and may be secreted in breast milk. Not to be used during lactation unless considered essential by a physician.
Paracetamol
The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by colestyramine. The anticoagulant effect of warfarin and other coumarins may be enhanced by prolonged regular daily use of paracetamol with increased risk of bleeding; occasional doses have no significant effect.
Chlorpheniramine
Concurrent use of chlorpheniramine and hypnotics or anxiolytics may cause an increase in sedative effects, therefore medical advice should be sought before taking chlorpheniramine concurrently with these medicines.
Chlorpheniramine inhibits phenytoin metabolism and can lead to phenytoin toxicity.
The anticholinergic effects of chlorpheniramine are intensified by MAOIs.
Paracetamol
Adverse events from historical clinical trial data are both infrequent and from small patient exposure. Accordingly, events reported from extensive post-marketing experience at therapeutic/labelled dose and considered attributable are tabulated below by system class. Due to limited clinical trial data, the frequency of these adverse events is not known (cannot be estimated from available data), but post-marketing experience indicates that adverse reactions to paracetamol are rare and serious reactions are very rare.
Blood and lymphatic system disorders: thrombocytopenia, agranulocytosis.
Immune system disorders: anaphylaxis, cutaneous hypersensitivity reactions including skin rashes, angioedema and Stevens-Johnson syndrome, toxic epidermal necrolysis.
Respiratory, thoracic and mediastinal disorders: bronchospasm (There have been cases of bronchospasm with paracetamol, but these are more likely in asthmatics sensitive to aspirin or other NSAIDs).
Hepatobiliary disorders: hepatic dysfunction.
Chlorpheniramine
Adverse reactions which have been observed in clinical trials and which are considered to be common (occurring in 1% to <10% of subjects) or very common (occurring in ≥ 10% of subjects) are listed below. The frequency of other adverse reactions identified during post-marketing use is not known.
Blood and lymphatic system disorders: Not known: haemolytic anaemia, blood dyscrasias.
Immune system disorders: Not known: allergic reaction, angioedema, anaphylactic reactions.
Metabolism and nutritional disorders: Not known: anorexia.
Psychiatric disorders: Not known: confusion*, excitation*, irritability*, nightmares*, depression.
Nervous system disorders*:
Very common: sedation, somnolence.
Common: disturbance in attention, abnormal coordination, dizziness, headache.
Eye disorders: Common: blurred vision.
Ear and labyrinth disorders: Not known: tinnitus.
Cardiac disorders: Not known: palpitations, tachycardia, arrhythmias.
Vascular disorders: Not known: Hypotension.
Respiratory, thoracic and mediastinal disorders:
Not known: thickening of bronchial secretions.
Gastrointestinal disorders: Common: nausea, dry mouth.
Not known: vomiting, abdominal pain, diarrhoea, dyspepsia
Hepatobiliary disorders: Not known: hepatitis, jaundice.
Skin and subcutaneous disorders:
Not known: exfoliative dermatitis, rash, urticaria, photosensitivity.
Musculoskeletal and connective tissue disorders:
Not known: muscle twitching, muscle weakness.
Renal and urinary disorders:
Not known: urinary retention.
General disorders and administration site conditions:
Common: fatigue. Not known: chest tightness.
*Children and the elderly are more likely to experience neurological anticholinergic effects and paradoxical excitation (e.g. increased energy, restlessness, nervousness).
Please inform your doctor of all undesirable effects upon drug administration.
Paracetamol
Liver damage is possible in adults who have taken 10 g or more of paracetamol. Ingestion of 5 g or more of paracetamol may lead to liver damage if the patient has risk factors:
If the patient
- is on long-term treatment with carbamazepine, phenobarbitone, phenytoin, primidone, rifampicin, St John's Wort or other drugs that induce liver enzymes. Or
- regularly consumes ethanol in excess of recommended amounts. Or
- is likely to be glutathione depleted e.g. eating disorders, cystic fibrosis, HIV infection, starvation, cachexia.
Symptoms
Symptoms of paracetamol overdosage in the first 24 hours are pallor, nausea, vomiting, 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, haemorrhage, hypoglycaemia, cerebral oedema, and death. Acute renal failure with acute tubular necrosis, strongly suggested by loin pain, haematuria and proteinuria, may develop even in the absence of severe liver damage. Cardiac arrhythmias and pancreatitis have been reported.
Management
Immediate treatment is essential in the management of paracetamol overdose. Despite a lack of significant early symptoms, patients should be referred to hospital urgently for immediate medical attention. Symptoms may be limited to nausea or vomiting and may not reflect the severity of overdose or the risk of organ damage. Management should be in accordance with established treatment guidelines, see BNF overdose section.
Treatment with activated charcoal should be considered if the overdose has been taken within 1 hour. Plasma paracetamol concentration should be measured at 4 hours or later after ingestion (earlier concentrations are unreliable). Treatment with N-acetylcysteine may be used up to 24 hours after ingestion of paracetamol, however, the maximum protective effect is obtained up to 8 hours post-ingestion. The effectiveness of the antidote declines sharply after this time. If required the patient should be given intravenous Nacetylcysteine, in line with the established dosage schedule. If vomiting is not a problem, oral methionine may be a suitable alternative for remote areas, outside hospital. Management of patients who present with serious hepatic dysfunction beyond 24h from ingestion should be discussed with the NPIS or a liver unit.
Chlorpheniramine
Symptoms and signs
The estimated lethal dose of chlorpheniramine is 25 to 50 mg per kg body weight. Symptoms and signs include sedation, paradoxical excitation of the CNS, toxic psychosis, apnoea, convulsions, anticholinergic effects, dystonic reactions and cardiovascular collapse including arrhythmias.
Treatment
Symptomatic and supportive measures should be provided with special attention to cardiac, respiratory, renal and hepatic functions, and fluid and electrolyte balance.
If overdosage is by the oral route, treatment with activated charcoal should be considered provided there are no contraindications for use and the overdose has been taken recently (treatment is most effective if given within an hour of ingestion).
Hypotension and arrhythmias should be treated vigorously; CNS convulsions may be treated with I.V. diazepam. Haemoperfusion may be used in severe cases.
Store in dry places, not exceeding 30oC, protect from light.
Paracetamol
Care is advised in the administration of paracetamol to patients with severe renal or severe hepatic impairment. The hazard of overdose is greater in those with non-cirrhotic alcoholic liver disease.
Do not exceed the stated dose.
Do not use with any other paracetamol-containing products.
Patients should be advised to consult a doctor if they suffer from non-serious arthritis and need to take painkillers every day or headache and symptoms persist.
For the paracetamol-containing drugs, the physician should warn patients of serious signs of skin reactions such as Steven-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN) or Lyell’s syndrome, acute generalized exanthematous pustulosis (AGEP).
Chlorpheniramine
Chlorpheniramine is a common antihistamine; therefore, it should be used with caution in epilepsy, raised intra-ocular pressure including glaucoma, prostatic hypertrophy; severe hypertension or cardiovascular disease; bronchitis, bronchiectasis or asthma; hepatic impairment; renal impairment. Children and the elderly are more likely to experience neurological anticholinergic effects and paradoxical excitation (e.g. increased energy, restlessness, nervousness).
The anticholinergic properties of chlorpheniramine may cause drowsiness, dizziness, blurred vision and psychomotor impairment in some patients which may seriously affect ability to drive and use machinery.
The effects of alcohol may be increased and therefore concurrent use should be avoided.
Should not be used with other antihistamine-containing products, including antihistamine-containing cough and cold medicines.
Keep out of the sight and reach of children.
Excipients
This medicine contains less than 1 mmol sodium (23 mg) per sachet, that is to say essentially “sodium-free”.
Sucrose: Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
Aspartame: This medicine contains 47 mg aspartame in each sachet. Aspartame is a source of phenylalanine. It may be harmful if you have phenylketonuria (PKU), a rare genetic disorder in which phenylalanine builds up because the body cannot remove it properly.
Sunset yellow: may cause allergic reactions.
Temporarily relieves the symptoms: headache, runny nose and sneezing, minor aches, sore throat.
Temporarily reduces fever.
Hypersensitivity to any of the ingredients of the drug.
The anticholinergic properties of chlorpheniramine are intensified by monoamine oxidase inhibitors (MAOIs). The medicinal product is therefore contra-indicated in patients who have been treated with MAOIs within the last fourteen days.
Adults and children aged >12 years: oral dose of 1 - 2 sachets every 4 - 6 hours. Do not take more than 12 sachets in one day.
Children aged 6 - 12 years: oral dose of 1 sachet every 4 - 6 hours. Do not take more than 5 sachets in one day.
Children aged less than 6 years: not applicable.
Or as directed by the physician.
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