1. Name Of The Medicinal Product
Lemsip Max Cold & Flu Direct Lemon.
2. Qualitative And Quantitative Composition
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*This is equivalent to 10 mg phenylephrine base.
For excipients, see 6.1.
3. Pharmaceutical Form
Oral powder.
A white to off-white unit-dose powder with the odour and flavour of lemons.
4. Clinical Particulars
4.1 Therapeutic Indications
For relief of symptoms associated with the common cold and influenza, including the relief of aches and pains, sore throat, headache, nasal congestion and lowering of temperature.
4.2 Posology And Method Of Administration
Oral administration.
Adults and children 12 and over: One single-dose container. The product is taken orally without water.
The dose may be repeated in 4 hours.
No more than four doses should be taken in 24 hours.
Not to be given to children under 12 without medical advice.
There is no indication that dosage need be modified in the elderly.
4.3 Contraindications
Severe coronary heart disease and cardiovascular disorders. Hypertension. Hyperthyroidism. Contraindicated in patients currently receiving or within two weeks of stopping therapy with monoamine oxidase inhibitors. Hypersensitivity to paracetamol, phenylephrine or any other ingredient.
4.4 Special Warnings And Precautions For Use
Use with caution in patients with Raynaud's phenomenon or diabetes mellitus.
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. Patients should be advised not to take other paracetamol-containing products concurrently.
Due to its aspartame content this product should not be given to patients with phenylketonuria.
Phenylephrine
Phenylephrine should be used with care in patients with cardiovascular disease, diabetes mellitus, closed angle glaucoma, prostatic enlargement and hypertension.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Paracetamol
The speed of absorption of paracetamol may be increased by metoclopramide or domperidone and absorption reduced by cholestyramine.
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.
Medicinal products which induce hepatic microsomal enzymes such as alcohol, barbiturates, monoamine oxidase inhibitors and tricyclic antidepressants, may increase the hepatotoxicity of paracetamol particularly after overdose.
Phenylephrine hydrochloride
Monoamine oxidase inhibitors (including moclobemide): hypertensive interactions occur between sympathomimetic amines such as phenylephrine and monoamine oxidase inhibitors (see section 4.3).
Sympathomimetic amines: concomitant use of phenylephrine with other sympathomimetic amines can increase the risk of cardiovascular side effects.
Beta-blockers and other antihypertensives (including debrisoquine, guanethidine, reserpine, methyldopa): phenylephrine may reduce the efficacy of beta-blockers and antihypertensives. The risk of hypertension and other cardiovascular side effects may be increased (see section 4.3).
Tricyclic antidepressants (e.g. amitriptyline): may increase the risk of cardiovascular side effects with phenylephrine (see section 4.3).
Digoxin and cardiac glycosides: concomitant use of phenylephrine may increase the risk of irregular heartbeat or heart attack.
4.6 Pregnancy And Lactation
Paracetamol
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. Paracetamol is excreted in breast milk, but not in a clinically significant amount. Available published data do not contraindicate breast feeding.
Phenylephrine hydrochloride
The safety of this medicine during pregnancy and lactation has not been established but in view of a possible association of foetal abnormalities with first trimester exposure to phenylephrine, the use of the product during pregnancy should be avoided. In addition, because phenylephrine may reduce placental perfusion, the product should not be used in patients with a history of pre-eclampsia.
In view of the lack of data on the use of phenylephrine during lactation, this medicine should not be used during breast feeding.
4.7 Effects On Ability To Drive And Use Machines
Lemsip Max Cold & Flu Direct Lemon has no or negligible influence on ability to drive or use machinery.
4.8 Undesirable Effects
Paracetamol
Adverse effects of paracetamol are rare, but hypersensitivity including skin rash may occur. There have been a few reports of blood dyscrasias including thrombocytopenia, leucopenia, pancytopenia, neutropenia and agranulocytosis, but these were not necessarily causally related to paracetamol.
Acute pancreatitis after ingestion of above normal amounts.
Phenylephrine hydrochloride
High blood pressure with headache and vomiting, probably only in overdose. Rarely palpitations. Also, rare reports of allergic reactions and occasionally urinary retention in males.
4.9 Overdose
Paracetamol
Liver damage is possible in adults who have taken 10 g or more of paracetamol. Ingestion of 5 g of more of paracetamol may lead to liver damage if the patient has risk factors (see below).
Risk factors
If the patient:
(a) Is on long-term treatment with carbamazepine, phenobarbitone, phenytoin, primidone, rifampicin, St John's Wort or other drugs that induce liver enzymes.
Or
(b) Regularly consumes ethanol in excess of recommended amounts.
Or
(c) Is likely to be glutathione depleted, e.g. eating disorders, cystic fibrosis, HIV infection, starvation, cachexia.
Symptoms
Symptoms of paracetamol overdose 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 N-acetylcysteine, 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 24 hours from ingestion should be discussed with the NPIS or a liver unit.
Phenylephrine hydrochloride
Features of severe overdose of phenylephrine include haemodynamic changes and cardiovascular collapse with respiratory depression. Treatment includes early gastric lavage and symptomatic and supportive measures. Hypertensive effects may be treated with an i.v. alpha-receptor blocking agent.
Phenylephrine overdose is likely to result in: nervousness, headache, dizziness, insomnia, increased blood pressure, nausea, vomiting, mydriasis, acute angle closure glaucoma (most likely to occur in those with closed angle glaucoma), tachycardia, palpitations, allergic reactions (e.g. rash, urticaria, allergic dermatitis), dysuria, urinary retention (most likely to occur in those with bladder outlet obstruction, such as prostatic hypertrophy).
Additional symptoms may include, hypertension, and possibly reflex bradycardia. In severe cases confusion, hallucinations, seizures and arrhythmias may occur. However the amount required to produce serious phenylephrine toxicity would be greater than that required to cause paracetamol-related liver toxicity.
Treatment should be as clinically appropriate. Severe hypertension may need to be treated with alpha blocking medicinal products such as phentolamine.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Paracetamol: Paracetamol has both analgesic and antipyretic activity which is believed to be mediated principally through its inhibition of prostaglandin synthesis within the central nervous system.
Phenylephrine: Phenylephrine is a post-synaptic α-receptor agonist with low cardioselective β - receptor affinity and minimal central stimulant activity. It is a recognised decongestant and acts by vasoconstriction to reduce oedema and nasal swelling.
5.2 Pharmacokinetic Properties
Paracetamol: Paracetamol is absorbed rapidly and completely mainly from the small intestine producing peak plasma levels after 15-20 minutes following oral dosing. The systemic availability is subject to first-pass metabolism and varies with dose between 70% and 90%. The drug is rapidly and widely distributed throughout the body and is eliminated from plasma with a T½ of approximately 2 hours. The major metabolites are glucuronide and sulphate conjugates (>80%) which are excreted in urine.
Phenylephrine: Phenylephrine is absorbed from the gastrointestinal tract, but has reduced bioavailability by the oral route due to first-pass metabolism. It retains activity as a nasal decongestant when given orally, the drug distributing through the systemic circulation to the vascular bed of nasal mucosa. When taken by mouth as a nasal decongestant phenylephrine is usually given at intervals of 4-6 hours.
5.3 Preclinical Safety Data
No preclinical findings of relevance have been reported.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Ethyl cellulose, ascorbic acid, glyceryl tristearate, tartaric acid, sodium carbonate anhydrous, aspartame, lemon flavour, sweet flavour and xylitol.
6.2 Incompatibilities
None known.
6.3 Shelf Life
Twenty-four months.
6.4 Special Precautions For Storage
Do not store above 25°C and store in the original package.
6.5 Nature And Contents Of Container
Polyethylene terephthalate / aluminium / polyethylene sachets.
Pack size: 1, 8 and 10.
6.6 Special Precautions For Disposal And Other Handling
There are no special instructions for handling.
7. Marketing Authorisation Holder
Reckitt Benckiser Healthcare (UK) Limited
Dansom Lane
Hull
HU8 7DS
United Kingdom.
8. Marketing Authorisation Number(S)
PL 00063/0114
9. Date Of First Authorisation/Renewal Of The Authorisation
19 July 2002
10. Date Of Revision Of The Text
28/06/2011
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