Ibuprofen Tablets 200mg
Out of date information, search anotherSUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Dentogen Ibuprofen Tablets 200mg
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Ibuprofen 200mg For excipients, see 6.1.
3 PHARMACEUTICAL FORM
Film coated tablets.
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
For the relief of toothache pain and pain and swelling following minor oral surgery.
4.2 Posology and method of administration
For oral administration and short-term use only.
Adults, the elderly and children over 12 years
The minimum effective dose should be used for the shortest time necessary to relieve symptoms. The patient should consult a doctor or dentist if symptoms persist or worsen, or if the product is required for more than 10 days.
An initial dose of 2 tablets to be taken with water. If the dental pain continues the initial dose may be followed by further doses of 1 or 2 tablets. Leave at least four hours between doses and do not take more than 1200mg (6 tablets) in any 24 hour period.
Children
Not suitable for children under 12 years of age.
4.3 Contraindications
Hypersensitivity to ibuprofen or any of the constituents in the product.
Patients who have previously shown hypersensitivity reactions (e.g. asthma, rhinitis, angioedema or urticaria) in response to aspirin or other non-steroidal antiinflammatory drugs.
Active or previous peptic ulcer.
History of upper gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
Use with concomitant NSAIDs including cyclo-oxygenase-2 specific inhibitors (See section 4.5 Interactions).
Severe hepatic failure, renal failure or heart failure (See section 4.4, Special warnings and precautions for use).
Last trimester of pregnancy (See section 4.6 Pregnancy and lactation).
Severe heart failure.
4.4 Special warnings and precautions for use
Bronchospasm may be precipitated in patients suffering from or with a previous history of bronchial asthma or allergic disease.
Undesirable effects may be minimised by using the minimum effective dose for the shortest possible duration.
The elderly are at increased risk of the serious consequences of adverse reactions.
Systemic lupus erythematosus and mixed connective tissue disease increased risk of aseptic meningitis (see section 4.8 Undesirable effects).
Chronic inflammatory intestinal disease (ulcerative colitis, Crohn’s disease) - as these conditions may be exacerbated (See section 4.8 Undesirable effects).
Hypertension and/or cardiac impairment as renal function may deteriorate and/or fluid retention occur.
Renal impairment as renal function may further deteriorate (See section 4.3 Contraindications and Section 4.8 Undesirable effects).
Hepatic dysfunction (See section 4.3 Contraindications and Section 4.8 Undesirable effects).
There is limited evidence that drugs which inhibit cyclo-oxygenase/prostaglandin synthesis may cause impairment of female fertility by an effect on ovulation. This is reversible upon withdrawal of treatment.
GI bleeding, ulceration or perforation, which can be fatal, has been reported with all NSAIDs at anytime during treatment, with or without warning symptoms or a previous history of serious GI events.
Patients with a history of GI toxicity, particularly when elderly, should report any unusual abdominal symptoms (especially GI bleeding) particularly in the initial stages of treatment.
Caution should be advised in patients receiving concomitant medications which could increase the risk of gastrotoxicity or bleeding, such as corticosteroids, or anticoagulants such as warfarin or anti-platelet agents such as aspirin (see section
4.5 Interactions).
When GI bleeding or ulceration occurs in patients receiving ibuprofen, the treatment should be withdrawn.
Caution (discussion with doctor or pharmacist) is required prior to starting treatment in patients with a history of hypertension and/or heart failure as fluid retention, hypertension and oedema have been reported in association with NSAID therapy.
Undesirable effects may be minimised by using the lowest effective dose for the shortest duration necessary to control symptoms (see GI and cardiovascular risks below).
Cardiovascular and cerebrovascular effects
Clinical trial and epidemiological data suggest that use of ibuprofen, particularly at high doses (2400mg daily) and in long-term treatment may be associated with a small increased risk of arterial thrombotic events (for example myocardial infarction or stroke). Overall, epidemiological studies do not suggest that low dose ibuprofen (e.g. <1200mg daily) is associated with an increased risk of myocardial infarction.
The label will include:
Read the enclosed leaflet before taking this product.
Do not take if you -
• have or have ever had a stomach ulcer, perforation or bleeding.
• are allergic to ibuprofen or any other ingredient of the product, aspirin or other related painkillers.
• are taking other NSAID painkillers, or aspirin with a daily dose above 75mg.
• are in the last 3 months of pregnancy.
Speak to a pharmacist or your doctor or dentist before taking this product if you • have asthma, liver, heart, kidney or bowel problems.
• are in the first 6 months of pregnancy.
If symptoms persist or worsen, consult your dentist or doctor.
4.5 Interaction with other medicinal products and other forms of interaction
Experimental data suggest that ibuprofen may inhibit the effect of low dose aspirin on platelet aggregation when they are dosed concomitantly. However, the limitations of these data and the uncertainties regarding extrapolation of ex-vivo data to the clinical situation imply that no firm conclusions can be made for regular ibuprofen use, and no clinically relevant effect is considered to be likely for occasional ibuprofen use (see section 5.1).
Ibuprofen should not be used in combination with: Aspirin: Unless low-dose aspirin (not above 75mg daily) has been advised by a doctor, as this may increase the risk of adverse reactions (See section 4.3 Contraindications).
Other NSAIDs: As these may increase the risk of adverse effects (See section 4.3 Contraindications).
Ibuprofen should be used with caution in combination with: Anticoagulants: NSAIDs may enhance the effects of anti-coagulants, such as warfarin (See section 4.4).
Antihypertensives and diuretics: NSAIDs may diminish the effect of these drugs. Corticosteroids: May increase the risk of adverse reactions in the adverse reactions in the gastrointestinal tract (See section 4.4 Special warnings).
Lithium: There is evidence for potential increases in plasma levels of lithium. Methotrexate: There is a potential for an increase in plasma methotrexate.
Zidovudine: There is evidence of an increased risk of haemarthroses and
haematoma in HIV (+) haemophiliacs receiving concurrent treatment with zidovudine and ibuprofen.
4.6 Pregnancy and lactation
Whilst no teratogenic effects have been demonstrated in animal experiments, the use of Dentogen Ibuprofen Tablets should, if possible, be avoided during the first 6 months of pregnancy.
During the 3rd trimester, ibuprofen is contraindicated as there is a risk of premature closure of the foetal ductus arteriosus with possible persistant pulmonary hypertension. The onset of labour may be delayed and the duration increased with an increased bleeding tendency in both mother and child (See section 4.3 Contraindications).
In limited studies, ibuprofen appears in the breast milk in very low concentration and is unlikely to affect the breast-fed infant adversely.
See section 4.4 regarding female fertility.
4.7 Effects on ability to drive and use machines
None expected at recommended doses and duration of therapy.
4.8 Undesirable effects
Hypersensitivity reactions have been reported and these may consist of:
(a) Non-specific allergic reactions and anaphylaxis.
(b) Respiratory tract reactivity, e.g. asthma, aggravated asthma, bronchospasm, dyspnoea
(c) Various skin reactions, e.g. pruritis, urticaria, angioedema and more rarely exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme).
The following list of adverse effects relates to those experienced with ibuprofen at OTC doses, for short-term use. In the treatment of chronic conditions, under longterm treatment, additional adverse effects may occur.
Hypersensitivity reactions: Uncommon: Hypersensitivity reactions with urticaria and pruritus.
Very rare: severe hypersensitivity reactions. Symptoms could be: facial, tongue and laryngeal swelling, dyspnoea, tachycardia, hypotension, (anaphylaxis, angioedema or severe shock).
Exacerbation of asthma or bronchospasm.
Gastrointestinal: Uncommon: abdominal pain, nausea, and dyspepsia. Rare: diarrhoea, flatulence, constipation and vomiting.Very rare: peptic ulcer, perforation or gastrointestinal haemorrhage,sometimes fatal, particularly in the elderly.
Exacerbation of ulcerative colitis and Crohn’s disease (See section 4.4).
Nervous system:
Uncommon: Headache.
Renal: Very rare: Acute renal failure, papillary necrosis, especially in long-term use, associated with increased serum urea and oedema.
Hepatic: Very rare: liver disorders.
Haematological: Very rare: Haematopoietic disorders (anaemia, leucopenia, thrombocytopenia, pancytopenia, agranulocytosis). First signs are: fever, sore throat, superficial mouth ulcers, flu-like symptoms, severe exhaustion, unexplained bleeding and bruising.
Skin:
Uncommon: Various skin rashes.
Very rare: Severe forms of skin reactions such as erythema multiforme and epidermal necrolysis can occur.
Immune System: In patients with existing auto-immune disorders (such as systemic lupus erythematosus, mixed connective tissue disease) during treatment with ibuprofen, single cases of symptoms of aseptic meningitis, such as stiff neck, headache, nausea, vomiting, fever or disorientation have been observed (See section 4.4).
Oedema, hypertension, and cardiac failure, have been reported in association with NSAID treatment.
Clinical trial and epidemiological data suggest that use of ibuprofen (particularly at high doses 2400mg daily) and in long-term treatment may be associated with a small increased risk of arterial thrombotic events (for example myocardial infarction or stroke) (see section 4.4).
4.9 Overdose
In children, ingestion of more than 400 mg/kg may cause symptoms. In adults the dose response effect is less clear cut. The half-life in overdose is 1.5-3 hours.
Symptoms
Most patients who have ingested clinically important amounts of NSAIDs will develop no more than nausea, vomiting, epigastric pain, or more rarely diarrhoea. Tinnitus, headache and gastrointestinal bleeding are also possible. In more serious poisoning , toxicity is seen in the central nervous system, manifesting as drowsiness, occasionally excitation and disorientation or coma. Occasionally patients develop convulsions. In serious poisoning metabolic acidosis may occur and the prothrombin time/INR may be prolonged, probably due to interference with the actions of circulating clotting factors. Acute renal failure and liver damage may occur. Exacerbation of asthma is possible in asthmatics.
Management
Management should be symptomatic and supportive and include the maintenance of a clear airway and monitoring of cardiac and vital signs until stable. Consider oral administration of activated charcoal if the patient presents within 1 hour of ingestion of a potentially toxic amount. If frequent or prolonged, convulsions should be treated with intravenous diazepam or lorazepam. Give bronchodilators for asthma.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Ibuprofen is a propionic acid derivative NSAID that has demonstrated its efficacy by inhibition of prostaglandin synthesis. In humans ibuprofen reduces inflammatory pain, swellings and fever. Furthermore, ibuprofen reversibly inhibits platelet aggregation.
Experimental data suggest that ibuprofen may inhibit the effect of low dose aspirin on platelet aggregation when they are dosed concomitantly. In one study, when a single dose of ibuprofen 400mg was taken within 8 hours before or within 30 minutes after immediate release aspirin dosing (81mg), a decreased effect of aspirin on the formation of thromboxane or platelet aggregation occurred. However, the limitations of these data and the uncertainties regarding extrapolation of ex vivo data to the clinical situation imply that no firm conclusions can be made for regular ibuprofen use, and no clinically relevant effect is considered to be likely for occasional ibuprofen use.
5.2 Pharmacokinetic properties
Ibuprofen is rapidly absorbed following administration and is rapidly distributed throughout the whole body. The excretion is rapid and complete via the kidneys.
Maximum plasma concentrations are reached 45 minutes after ingestion if taken on an empty stomach. When taken with food peak levels are observed after 1 to 2 hours. These times may vary with different dosage forms.
The half-life of ibuprofen is about 2 hours.
In limited studies, ibuprofen appears in the breast milk in very low concentrations.
The relationship between the administered dose and the area of the total ibuprofen concentration-time curve appears to be non-linear, though a linear relationship does exist between free ibuprofen plasma concentration and dose. This, plasma protein binding of the drug may be non-linear. Total urinary excretion of ibuprofen and its metabolites is a linear function of dosage.
Except at very high concentrations, about 99% of ibuprofen is bound to a single site on plasma albumin although a second primary site can be occupied. The high plasma protein binding of ibuprofen results in relatively low volume of distribution, about 0.11kg"1 . Only very small amounts of ibuprofen are excreted in breast milk, not sufficient to have any effect on the infant. It is not known if the drug crosses the placenta.
Ibuprofen is extensively metabolised in the liver, with more than 90% of the dose excreted in the urine and the remainder presumably in the faeces. Less than 10% of the dose is excreted unchanged. Excretion is essentially complete within 24 hours.
Renal impairment has no effect of the kinetics of the drug, rapid elimination still occurring as a consequence of metabolism.
There is no accumulation of ibuprofen or its metabolites in normal subjects on repeated administration of the drug. Old age has no significant effect on the elimination of ibuprofen.
|
Summary |
Oral absorption: |
>95% |
|
Plasma half life: |
2h | |
|
Volume of distribution: |
0.11kg | |
|
Plasma protein binding: |
99% |
5.3 Preclinical safety data
None stated.
6 PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Core
Lactose
Ac-di-sol
Methylcellulose (Celacol M450)
Magnesium Stearate
Coating
Methylcellulose (Methocel E15)
Polyethylene Glycol 400 Sepisperse Rose AP 5002
6.2 Incompatibilities
None stated.
Shelf life
6.3
36 months unopened.
6.4 Special precautions for storage
In a glass bottle - Store at or below 25°C.
In blister pack - store below 25°C in a dry place.
6.5 Nature and contents of container
15 ml amber glass universal tablet bottle fitted with child resistant cap containing 18 tablets.
30ml amber glass universal tablet bottle fitted with child resistant cap containing 36 tablets.
Thermoformed blister pack of 12 tablets constructed of :-
(a) Plain 250 . white rigid UPVC
(b) 20 hard temper aluminium foil
Packs consist of:
(a) 1 x 12 tablets
(b) 2 x 12 tablets
(c) 4 x 12 tablets
all in an outer carton
6.6
Special precautions for disposal
None.
7 MARKETING AUTHORISATION HOLDER
Ayrton Saunders Limited,
North Way,
Walworth Industrial Estate,
Andover,
SP10 5AZ United Kingdom
8 MARKETING AUTHORISATION NUMBER(S)
PL 16431/0085
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
24 October 1985 / 1 October 1998
10 DATE OF REVISION OF THE TEXT
17/02/2009