Mega Lemon Professional Information

1. NAME OF THE MEDICINE:

Mega Lemon

 

2. QUALITATIVE AND QUANTITATIVE COMPOSITION

Each serving size (5 g scoop) of Mega Lemon contains:

Active Ingredients:                     5 g scoop

Aspirin                                          500 mg

Ascorbic Acid (Vitamin C)          250 mg

 

Inactive Ingredients:

Maltodextrin, Citric Acid, Sodium Bicarbonate, Lemon Flavour, Silicon Dioxide, Sucralose, Quinoline Yellow and Menthol Powder.

Contains antioxidant: Ascorbic Acid (Vitamin C)

Contains sweetener: Sucralose 25 mg

                       

3. PHARMACEUTICALFORM

Orange powder with characteristic odour.

 

4. CLINICAL PARTICULARS

4.1 Therapeutic indications

Effective treatment and relief of fever associated with colds and flu, headaches and pain.

                       

4.2 Posology and method of administration

Dissolve one (1) level scoop of Mega Lemon in a cup of 200ml hot or coldwater. Mega Lemon can be used in the morning and at night every 12 hours.

Do not exceed three (3) doses every 24 hours.

Elderly: A lower dose is recommended.

Do not exceed daily dose without consulting a relevant health care provider.

                       

Paediatric population

Do not give to children aged under 16 years, unless specifically indicated (eg for Kawasaki’s disease).

                       

4.3 Contraindications

Hypersensitivity to the active substance or to any of the excipients or residues from the manufacturing process.

Aspirin is contraindicated in patients with:

• active peptic ulceration or a history of peptic ulceration.

• Haemophilia, haemorrhagic disease or a history of bleeding disorders.

• Gout or a history of gout.

• Hypersensitivity to aspirin (e.g. asthma, rhinitis, angioedema or urticaria), other NSAIDs or other excipients.

• Patients with severe renal or hepatic function impairment.

• During the third trimester of pregnancy.

• Patients receiving oral anticoagulant therapy.

• Ascorbic acid supplements should not be given to patients with hyperoxaluria.

See section “4.5 Interaction with other medicines and other forms of interaction” and “4.4 Special warnings and precautions for use”.

                       

4.4 Special warnings and precautions for use

Do not use continuously for pain for more than 10 days unless directed by a medical practitioner. If the pain or fever persists or gets worse, or if new symptoms occur, a registered healthcare practitioner should be consulted.

There is a possible association between aspirin and Reye’s syndrome when given to children. Reye’s syndrome is a very rare disease, which affects the brain and liver and can be fatal. For this reason, aspirin should not be given to children under 16 years unless specifically indicated (e.g.for Kawasaki’s disease).

Patients with rare hereditary problems of galactose intolerance, the Lapp lactose deficiency or glucose- galactose

malabsorption should not take aspirin.

Patients should be warned:

• not to exceed the stated dose.

• not to take aspirin if they have ever suffered from stomach ulcers.

• to keep medicines out of the reach of children.

Caution is required if administrated to patients suffering from, or with a previous history of bronchial asthma.

May produce haemolysis is some glucose-6-phoshate dehydrogenase deficient individuals.

Increased intake of ascorbic acid over a prolonged period may result in anincreased renal clearance of ascorbic acid, and deficiency may result if the intake is reduced or withdrawn rapidly.

                       

See Section 4.8 Undesirable effects.

                       

Interference with serological testing

Ascorbic acid may interfere with tests and assays for urinary glucose, giving false-negative results with methods utilising glucose oxidase with indicator (e.g.Labstix, Tes-Tape) and false-positive results with neocuproine methods. Estimation of uric acid by phosphotungstate or uricase with copper reduction and measurement of creatinine in non deproteinised serum may also be affected. High doses of ascorbic acid may give false-negative readings in faecal occult blood tests. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.

                       

4.5 Interaction with other medicines and other forms of interaction

If you are taking prescription medication, consult a relevant health care provider prior to use.

Aspirin should not be used in combination with other NSAIDS as this may increase the risk of side-effects.

Aspirin should be used with caution in combination with:

• ACE Inhibitors and Angio-II Receptor Antagonists: due to risk of renalimpairment and the hypotensive effect is antagonize.

• Antacids: excretion of Aspirin is increased by alkaline urine due to some antacids.

• Anti-depressants, SSRI’s: increased risk of bleeding.

• Anticoagulants: the risk of bleeding is increased with Aspirin due to the antiplatelet effect.

• Corticosteroids: increased risk of gastrointestinal bleeding.

• Anti-epileptic drug (eg phenytoin, sodium valproate): will be enhanced by Aspirin.

• Diuretics: effect will be antagonised by aspirin.

• Gout treatments such as probenecid, sulphinpyrazone: will be antagonised by aspirin.

• Methotrexate: excretion can be reduced with increased risk of toxicity.

• Metoclopramide: may enhance the effect of aspirin.

• Barbiturates and other sedatives may mask the respiratory symptoms of aspirin overdosage and have been reported to            enhance its toxicity.

Ascorbic acid increases the renal excretion of amphetamine. The plasma concentration of ascorbate is decreased by smoking and oral contraceptives.

                       

Ascorbic acid increases the absorption of iron.

Concomitant administration of aspirin and ascorbic acid may interfere with absorption of ascorbic acid. Renal excretion of salicylate is not affected and does not lead to reduced anti-inflammatory effects of aspirin. Concomitant administration of

aluminium-containing antacids may increase urinary aluminium elimination. Concurrent administration of antacids and ascorbic acid is not recommended, especially in patients with renal insufficiency. Co-administration with amygdalin (a complementary medicine) can cause cyanide toxicity. Concurrent administration of ascorbic acid with desferrioxamine enhances urinary iron excretion. Cases of cardiomyopathy and congestive heart failure have been reported in patients with idiopathic haemochromatosis and thalassaemias receiving desferrioxamine who were subsequently given ascorbic acid. Ascorbic acid should be used with caution in these patients and cardiac function monitored. Ascorbic acid may interfere with biochemical determinations of creatinine, uric acid and glucose in samples of blood and urine.

                       

See section 4.4 Special warnings and precautions for use.

                       

4.6 Fertility, pregnancy and lactation

Low doses (up to 100 mg/day):

Clinical studies indicate that doses up to 100 mg/day for restricted obstetrical use, which require specialised monitoring, appear safe.

                       

Doses of 100- 500 mg/day:

There is insufficient clinical experience regarding the use of doses above 100 mg/day up to 500 mg/day. Therefore, the recommendations below for doses of 500 mg/d and above apply also for this dose range.

 

Doses of 500 mg/day and above:

Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/foetal development. Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5 %. The risk is believed to increase with dose and duration of therapy. In animals, administration of a prostaglandin synthesis inhibitor has been shown to result in increased pre and post-implantation loss and embryo-foetal lethality. In addition, increased incidences of various malformations, including cardiovascular, have been reported in animals given a prostaglandin synthesis inhibitor during the organogenetic period. During the first and second trimester of pregnancy, acetyl salicylic acid should not be given unless clearly necessary. If acetylsalicylic acid is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept as low and duration of treatment as short as possible.

                       

During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose the foetus to:

- cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension);

- renal dysfunction, which may progress to renal failure with oligohydroamniosis; the mother and the neonate, at the end of                   pregnancy, to:

- possible prolongation of bleeding time, an anti-aggregating effect which may occur even at very low doses.

- inhibition of uterine contractions resulting in delayed or prolonged labour.

Consequently, acetylsalicylic acid at doses of 100 mg/day and higher is contraindicated during the third trimester of pregnancy.

                       

Lactation: Aspirin should not be taken when breast feeding as it impairs platelet function and increases the risk of

haemorrhage to the baby, i.e. intracranial haemorrhage.

                       

4.7 Effects on ability to drive and use machines

Effects on ability to drive and use machines has not been established.

                       

4.8 Undesirable effects

The frequencies of adverse reactions are ranked according to the following:

frequent > 1/100 

less frequent< 1/100

                       

Gastrointestinal disorders:

Frequent:

Nausea, vomiting, dyspepsia.

                       

Less frequent:

Abdominal pain, melaena, peptic ulcers, perforation or gastrointestinal bleeding, which may be fatal.

                       

Frequency unknown: Diarrhoea, flatulence, constipation, haematemesis, ulcerative stomatitis, exacerbation of colitis and Crohn’s disease, gastritis.

                       

Immune system disorder:

Less frequent:

Hypersensitivity:

Patients, especially those with asthma, chronic urticaria, or chronic rhinitis exhibit notable sensitivity to aspirin which may

provoke various hypersensitivity reactions which may include urticaria and other skin eruptions, angioedema, rhinitis and severe or even fatal paroxysmal bronchospasm and 10uthori. Patients sensitive to aspirin may exhibit cross-sensitivity to other NSAIDs.

                       

Blood disorders:

Frequency unknown:

Aspirin increases bleeding time, decreases platelet adhesiveness and in large doses may cause hypoprothrombinaemia. It may cause other blood disorders including thrombocytopaenia.

                       

Liver disorders:

Frequency unknown: Aspirin may cause hepatotoxicity particularly in patients with juvenile idiopathic arthritis or other connective tissue disorders.

                       

Cardiac disorders:

Frequency unknown:

Oedema, hypertension and cardiac failure.

Skin and subcutaneous tissue disorders:

 

Less frequent:

Bullous reactions, including Stevens-Johnson syndromeand toxic epidermal necrolysis. Redness of skin.

 

Renal and urinary disorders:

Less frequent:

Renal and urinary disorders: Patients known to be at risk of hyperoxaluria should not ingest ascorbic acid doses exceeding 1g daily as there may be increased urinary oxalate excretion. However, such risk has not been demonstrated in normal, non-hyper oxaluric individuals. Ascorbic acid has been implicated in precipitating haemolytic anaemia in certain individuals deficient of glucose-6-phosphate dehydrogenase.

                       

Increased intake of ascorbic acid over a prolonged period may result in increased renal clearance of ascorbic acid, and deficiency may result if the intake is reduced or withdrawn rapidly. Doses of more than 600 mg daily have a diuretic effect.

                       

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicine is important. It allows continued monitoring of the benefit/risk balance of the medicine. Health care providers are asked to report any suspected adverse reactions to SAHPRA via the “6.04 Adverse Drug Reactions Reporting Form”, found online under SAHPRA’s publications: https://www.sahpra.org.za/Publications/Index/8.

                       

4.9 Overdose

 

Aspirin

Symptoms:

Mild chronic salicylate intoxication includes dizziness, tinnitus, deafness, sweating, nausea, vomiting, headache, mental confusion and may be controlled by reducing the dosage. Symptoms of more severe intoxication or acute poisoning following overdosage include hyperventilation, fever, restlessness, ketosis, respiratory alkalosis and metabolic acidosis. Depression of the central nervous system may lead to coma, cardiovascular collapse, respiratory failure and death.

 

In children:

Drowsiness and metabolic acidosis commonly occur, hypoglycaemia may be severe, serious signs of overdosage may develop rapidly.

                       

Treatment:

In acute salicylate overdosage the stomach should be emptied by gastric lavage. Salicylate remaining in the stomach may be absorbed by activated charcoal. Fluid and electrolyte management is the mainstay treatment with the immediate aim being correction of acidosis, hyperpyrexia, hypokalaemia and dehydration. Alkaline diuresis, haemodialysis, or haemoperfusion are effective methods of removing salicylate from the plasma.

                        .

Ascorbic Acid (Vitamin C)

Symptoms:

At doses of over 3 g per day unabsorbed ascorbic acid is mainly excreted unmetabolized in the faeces. Absorbed ascorbic acid additional to the body’s needs is rapidly eliminated. Large doses of ascorbic acid may cause diarrhoea and the formation of renal oxalate calculi. Symptomatic treatment may be required. Ascorbic acid may cause acidosis or haemolytic anaemia in certain individuals with a deficiency of glucose 6 phosphate dehydrogenase. Renal failure can occur with massive ascorbic acid overdosage.

                       

Treatment:

Gastric lavage may be given if ingestion is recent otherwise general supportive measure should be employed as required.

                       

See section 4.8. Undesirable effects.

                       

5. PHARMACOLOGICAL PROPERTIES

Category A: Allopathic Medicine

Classification: 2.8 Analgesic Combinations.

                       

5.2 Pharmacodynamic properties

Acetylsalicylic acid (aspirin) has analgesic, anti-inflammatory and antipyretic actions. It is an inhibitor of the enzyme cyclo-

oxygenase, which results in the inhibition of the biosynthesis of prostaglandins.

Ascorbic acid, coupled with dehydroascorbic acid to which it is reversiblyoxidised, has a variety of functions in cellular oxidation processes. Ascorbic acid is required in several important hydroxylations, including the conversion of proline to hydroxyproline (and thus in collagen formation e.g.for intercellular substances and during wound healing); the formation of the neurotransmitters 5-hydroxytryptamine from tryptophan and noradrenaline from dopamine, and the biosynthesis of carnitine from lysine and methionine. Ascorbic acid appears to have an important role in metal ion metabolism, including the gastrointestinal absorption of iron and its transport between plasma and storage organs. There is evidence that ascorbic acid is required for normal leucocyte functions and that it participates in the detoxification of numerous foreign substances by the hepatic microsomal system. Deficiency of ascorbic acid leads to scurvy, which may be manifested by weakness, fatigue, dyspnoea, aching bones, perifollicular hyperkeratosis, petechia and ecchymosis, swelling and bleeding of the gums, hypochromic anaemia and other haematopoietic disorders, together with reduced resistance to infections and impaired wound healing.

                       

5.2 Pharmacokinetic properties

                       

Aspirin

Absorption of non-ionised aspirin occurs in the stomach. Acetysalicylates and Salicylates are also readily absorbed from the intestine. Hydrolysis to salicylic acid occurs rapidly in the intestine and in the circulation.Salicylates are extensively bound to plasma proteins; aspirin to a lesser degree. Aspirin and salicyates are rapidly distributed to all body tissues; they appear in milk and cross the placenta. The rate of excretion of aspirin varies as the pH rises, being greatest at 7.5 and above. Aspirin is also excreted as salicylic acid and as glucuronide conjugate, and as salicylic acid and gentisic acid.

                       

Ascorbic Acid (Vitamin C)

Absorption

Ascorbic acid is well absorbed from the gastrointestinal tract.

                       

Distribution

Ascorbic acid is widely distributed to all tissues. Body stores of ascorbic acid normally are about 1,5g. The concentration is higher in leucocytes and platelets than in erythrocytes and plasma.

                       

Elimination

Ascorbic acid additional to the body’s needs, generally amounts above 200mg daily, is rapidly eliminated; unmetabolized

ascorbic acid and its inactive metabolic products are chiefly excreted in the urine. The amount of ascorbic acid excreted unchanged in the urine is dose-dependent and may be accompanied by mild diuresis.

                       

5.3 Preclinical safety data

No data available.

                       

6. PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Mega Lemon

Maltodextrin, Citric Acid, Sodium Bicarbonate, Lemon Flavour, Silicon Dioxide, Sucralose, Quinoline Yellow and Menthol Powder.

                       

6.2 Incompatibilities

Not applicable.

                       

6.3 Shelf life

24 months.

                       

6.4 Special precautions for storage

Store in cool, dry place at or below 25 ˚C.

                       

6.5 Nature and contents of the container

Mega Lemon

White HD tub containing 150 g of yellow powder with characteristic Lemon odour and aluminum seal with a yellow screw lid.

                                               

6.6 Special precautions for disposal

No special requirements

                       

7. HOLDER OF CERTIFICATE OF REGISTRATION:

MC Pharma (PTY) Ltd

62 Constantia Avenue

Mnandi

Centurion, 0157

South Africa

                       

8. REGISTRATION NUMBER:

This unregistered medicine has not been evaluated by the SAHPRA for its quality, safety or intended use.

                       

9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION

Not applicable.

                       

10. DATE OF REVISION OF TEXT

Not applicable.