Skip to Content

UK Edition. Click here for US version.

ABFEN 600 MG EFFERVESCENT GRANULES

Active substance(s): IBUPROFEN

View full screen / Print PDF » Download PDF ⇩
Transcript
SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Abfen 600 mg Effervescent Granules

2

QUALITATIVE AND QUANTITATIVE COMPOSITION

One sachet contains 600 mg ibuprofen.
Excipients with known effect:
Sodium (197 mg/sachet)
Sucrose (3333 mg/sachet)

3

PHARMACEUTICAL FORM
Effervescent granules
Abfen 600 mg Effervescent Granules are white granules with an orange flavour.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Abfen 600 mg Effervescent Granules are indicated for their analgesic and antiinflammatory effects in the treatment of rheumatoid arthritis, ankylosing spondylitis,
osteoarthritis and other non-rheumatoid (seronegative) arthropathies.
In the treatment of non-articular rheumatic Abfen 600 mg Effervescent Granules are
indicated in peri-articular conditions such as frozen shoulder (capsulitis), bursitis,
tendinitis, tenosynovitis and low back pain; Abfen 600 mg Effervescent Granules can
also be used in soft-tissue injuries such as sprains and strains.
Abfen 600 mg Effervescent Granules are also indicated for their analgesic effect in
the relief of moderate pain such as dysmenorrhoea, dental and post-operative pain and
for symptomatic relief of headache including migraine headache.

4.2

Posology and method of administration
Posology

Undesirable effects may be minimised by using the lowest effective dose for the
shortest duration necessary to control symptoms (see section 4.4).

Adults:
The recommended dosage of ibuprofen is 1,200-1,800 mg daily in divided doses.
Some patients can be maintained on 600-1,200 mg daily. Total daily dose should not
exceed 2,400 mg.

Paediatric population:
Abfen 600 mg Effervescent Granules are not suitable for use in children and
adolescents below the age of 18 years.

Elderly:
The elderly are at increased risk of serious consequences of adverse reactions. If an
NSAID is considered necessary, the lowest effective dose should be used and for the
shortest possible duration. The patient should be monitored regularly for GI bleeding
during NSAID therapy.

Renal impairment:
Caution should be taken with ibuprofen dosage in patients with renal impairment. The
dosage should be assessed individually. The dose should be kept as low as possible
and renal function should be monitored (see sections 4.3, 4.4 and 5.2).

Hepatic impairment:
Caution should be taken with dosage in patients with hepatic impairment. The dosage
should be assessed individually and the dose should be kept as low as possible (see
sections 4.3, 4.4 and 5.2).

Method of Administration
For oral administration. To be taken preferably with or after food.
Abfen 600 mg Effervescent Granules should be constituted in water and consumed as
an oral suspension, once effervescence subsides. The minimum amount of water
required to disperse one sachet is 125 ml.
After reconstitution, the suspension has a white, translucent appearance, free from
foreign substances, with an orange odour.
A transient sensation of burning in the mouth or throat may occur with Abfen 600 mg
Effervescent Granules; ensure they are dissolved in plenty of water.

4.3

Contraindications


Hypersensitivity to the active substance or to any of the excipients listed in
section 6.1.



Ibuprofen should not be used in patients who have previously shown
hypersensitivity reactions (e.g. asthma, urticaria, angioedema or rhinitis) after
taking ibuprofen, acetylsalicylic acid (e.g. Aspirin) or other NSAIDs.



Ibuprofen is also contraindicated in patients with a history of gastrointestinal
bleeding or perforation, related to previous NSAID therapy. Ibuprofen should
not be used in patients with active, or history of, recurrent peptic ulcer or
gastrointestinal haemorrhage (two or more distinct episodes of proven
ulceration or bleeding).



Ibuprofen should not be given to patients with conditions involving an
increased tendency to bleeding.



Ibuprofen is contraindicated in patients with severe heart failure (NYHA Class
IV), hepatic failure or renal failure (see section 4.4).



Ibuprofen is contraindicated during the last trimester of pregnancy (see section
4.6).

4.4
Special warnings and precautions for use
Undesirable effects may be minimised by using the lowest effective dose for the
shortest duration necessary to control symptoms (see section 4.2, and GI and
cardiovascular risks below).
Each Abfen 600 mg Effervescent Granules sachet contains 3333 mg of sucrose per
dose. This should be taken into account in patients with diabetes mellitus. Patients with
rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or
sucrase-isomaltase insufficiency should not take this medicine.
As with other NSAIDs, ibuprofen may mask the signs of infection.
Each Abfen 600 mg Effervescent granules sachet contains 8.6 mmol (197 mg) sodium
per dose. To be taken into consideration by patients on a controlled sodium diet.
The use of ibuprofen with concomitant NSAIDs, including cyclooxygenase-2 selective
inhibitors, should be avoided due to the increased risk of ulceration or bleeding (see
section 4.5).
Prolonged use of any type of painkiller for headaches can make them worse. If this
situation is experienced or suspected, medical advice should be obtained and
treatment should be discontinued. The diagnosis of medication overuse headache

(MOH) should be suspected in patients who have frequent or daily headaches despite
(or because of) the regular use of headache medications.
The habitual intake of painkillers, particularly the combination of several painkillers,
may lead to permanent renal damage with the risk of renal failure. This risk may be
increased by salt loss and dehydration.
Elderly
The elderly have an increased frequency of adverse reactions to NSAIDs, especially
gastrointestinal bleeding and perforation, which may be fatal (see section 4.2).
Gastrointestinal bleeding, ulceration and perforation
GI bleeding, ulceration or perforation, which can be fatal, has been reported with all
NSAIDs at any time during treatment, with or without warning symptoms or a previous
history of serious GI events.
The risk of GI bleeding, ulceration or perforation is higher with increasing NSAID
doses, in patients with a history of ulcer, particularly if complicated with haemorrhage
or perforation (see section 4.3), and in the elderly. These patients should commence
treatment on the lowest dose available. Combination therapy with protective agents
(e.g. misoprostol or proton pump inhibitors) should be considered for these patients,
and also for patients requiring concomitant low dose acetylsalicylic acid (e.g. Aspirin),
or other drugs likely to increase gastrointestinal risk (see below and section 4.5).
Patients with a history of gastrointestinal disease, particularly when elderly, should
report any unusual abdominal symptoms (especially gastrointestinal bleeding)
particularly in the initial stages of treatment.
Caution should be advised in patients receiving concomitant medications which could
increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants
such as warfarin, selective serotonin-reuptake inhibitors or anti-platelet agents such as
acetylsalicylic acid (e.g. Aspirin) (see section 4.5).
When GI bleeding or ulceration occurs in patients receiving ibuprofen, the treatment
should be withdrawn.
NSAIDs should be given with care to patients with a history of ulcerative colitis or
Crohn’s disease as these conditions may be exacerbated (see section 4.8).
Respiratory disorders
Caution is required if ibuprofen is administered to patients suffering from, or with a
previous history of, bronchial asthma since NSAIDs have been reported to precipitate
bronchospasm in such patients.
Cardiovascular, renal and hepatic impairment
The administration of an NSAID may cause a dose dependent reduction in
prostaglandin formation and precipitate renal failure. Patients at greatest risk of this
reaction are those with impaired renal function, cardiac impairment, liver dysfunction,
those taking diuretics and the elderly. Renal function should be monitored in these
patients (see section 4.3).

Ibuprofen should be given with care to patients with a history of heart failure or
hypertension since oedema has been reported in association with ibuprofen
administration.
Cardiovascular and cerebrovascular effects
Appropriate monitoring and advice are required for patients with a history of
hypertension and/or mild to moderate congestive heart failure as fluid retention and
oedema have been reported in association with NSAID therapy.
Clinical studies suggest that use of ibuprofen, particularly at a high dose (2400
mg/day) 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. ≤ 1200 mg/ day) is associated with an increased
risk of arterial thrombotic events.
Patients with uncontrolled hypertension, congestive heart failure (NYHA II-III),
established ischaemic heart disease, peripheral arterial disease, and/or cerebrovascular
disease should only be treated with ibuprofen after careful consideration and high doses
(2400 mg/day) should be avoided. Careful consideration should also be exercised
before initiating long-term treatment of patients with risk factors for cardiovascular
events (e.g. hypertension, hyperlipidaemia, diabetes mellitus, smoking), particularly if
high doses of ibuprofen (2400 mg/day) are required.

Renal effects
Caution should be used when initiating treatment with ibuprofen in patients with
considerable dehydration.
As with other NSAIDs, long-term administration of ibuprofen has resulted in renal
papillary necrosis and other renal pathologic changes. Renal toxicity has also been seen
in patients in whom renal prostaglandins have a compensatory role in the maintenance
of renal perfusion. In these patients, administration of an NSAID may cause a dosedependent reduction in prostaglandin formation and, secondarily, in renal blood flow,
which may precipitate overt renal decompensation. Patients at greatest risk of this
reaction are those with impaired renal function, heart failure, liver dysfunction, those
taking diuretics and ACE inhibitors and the elderly. Discontinuation of NSAID therapy
is usually followed by recovery to the pre-treatment state.
SLE and mixed connective tissue disease
In patients with systemic lupus erythematosus (SLE) and mixed connective tissue
disorders, there may be an increased risk of aseptic meningitis (see below and section
4.8).
Dermatological effects
Serious skin reactions, some of them fatal, including exfoliative dermatitis, StevensJohnson syndrome, and toxic epidermal necrolysis, have been reported very rarely in
association with the use of NSAIDs (see section 4.8). Patients appear to be at highest

risk of these reactions early in the course of therapy, the onset of the reaction occurring
within the first month of treatment in the majority of cases. Ibuprofen should be
discontinued at the first appearance of skin rash, mucosal lesions, or any other sign of
hypersensitivity.
Haematological effects
Ibuprofen, like other NSAIDs, can interfere with platelet aggregation and has been
shown to prolong bleeding time in normal subjects.
Aseptic meningitis
Aseptic meningitis has been observed on rare occasions in patients on ibuprofen
therapy. Although it is probably more likely to occur in patients with systemic lupus
erythematosus and related connective tissue diseases, it has been reported in patients
who do not have an underlying chronic disease.
Impaired female fertility
The use of ibuprofen may impair female fertility and is not recommended in women
attempting to conceive. In women who have difficulties conceiving or who are
undergoing investigation
of infertility, withdrawal of ibuprofen should be considered.
4.5

Interaction with other medicinal products and other forms of interaction

Care should be taken in patients treated with any of the following drugs as
interactions have been reported in some patients.
Antihypertensives, betablockers and diuretics:

Cardiac glycosides:
Cholestyramine:

Lithium:
Probenecid:
Methotrexate:
Ciclosporin:
Mifepristone:

NSAIDs may reduce the effect of anti-hypertensives,
such as ACE inhibitors, beta-blockers, angiotensin-II
receptor antagonists and diuretics.
Diuretics can also increase the risk of nephrotoxicity
of NSAIDs.
NSAIDs may exacerbate cardiac failure, reduce GFR
and increase plasma cardiac glycoside levels.
The concomitant administration of ibuprofen and
cholestyramine may reduce the absorption of
ibuprofen in the gastrointestinal tract. However, the
clinical significance is unknown.
Decreased elimination of lithium.
Medicinal products that contain probenecid may
delay the excretion of NSAIDs.
NSAIDs may inhibit the tubular secretion of
methotrexate and reduce clearance of methotrexate.
Increased risk of nephrotoxicity.
A decrease in the efficacy of the medicinal product
can theoretically occur due to the antiprostaglandin
properties of NSAIDs. Limited evidence suggests
that coadministration of NSAIDs on the day of
prostaglandin administration does not adversely

Other analgesics and
cyclooxygenase-2 selective
inhibitors:
Acetylsalicylic acid (e.g.
Aspirin):

Corticosteroids:
Anticoagulants:
Phenytoin:
Quinolone antibiotics:

Sulfonylureas:

Anti-platelet agents and
selective serotonin reuptake
inhibitors (SSRIs):
Tacrolimus:
Zidovudine:

Aminoglycosides:
Herbal extracts:

influence the effects of mifepristone or the
prostaglandin on cervical ripening or uterine
contractility and does not reduce the clinical efficacy
of medicinal termination of pregnancy.
Avoid concomitant use of two or more NSAIDs,
including Cox-2 inhibitors, as this may increase the
risk of adverse effects (see section 4.4).
Concomitant administration of ibuprofen and
acetylsalicylic acid is not generally recommended
because of the potential of increased adverse effects.
Experimental data suggest that ibuprofen may
competitively inhibit the effect of low dose
acetylsalicylic acid on platelet aggregation when
they are dosed concomitantly. Although there are
uncertainties regarding extrapolation of these data to
the clinical situation, the possibility that regular,
long-term use of ibuprofen may reduce the
cardioprotective effect of low-dose acetylsalicylic
acid cannot be excluded. No clinically relevant
effect is considered to be likely for occasional
ibuprofen use (see section 5.1).
Increased risk of gastrointestinal ulceration or
bleeding with NSAIDs (see section 4.4).
NSAIDs may enhance the effects of anticoagulants,
such as warfarin (see section 4.4).
Concomitant use of ibuprofen with phenytoin may
increase serum levels of phenytoin.
Animal data indicate that NSAIDs can increase the
risk of convulsions associated with quinolone
antibiotics. Patients taking NSAIDs and quinolones
may have an increased risk of developing
convulsions.
NSAIDs may potentiate the effects of sulfonylurea
medications. There have been rare reports of
hypoglycaemia in patients on sulfonylurea
medications receiving ibuprofen.
Increased risk of gastrointestinal bleeding with
NSAIDs (see section 4.4).
Possible increased risk of nephrotoxicity when
NSAIDs are given with tacrolimus.
Increased risk of haematological toxicity when
NSAIDs are given with zidovudine. There is
evidence of an increased risk of haemarthroses and
haematoma in HIV(+) haemophiliacs receiving
concurrent treatment with zidovudine and ibuprofen.
NSAIDs may decrease the excretion of
aminoglycosides.
Ginkgo biloba may potentiate the risk of bleeding
with NSAIDs.

CYP2C9 inhibitors:

4.6

Concomitant administration of ibuprofen with
CYP2C9 inhibitors may increase the exposure to
ibuprofen (CYP2C9 substrate). In a study with
voriconazole and fluconazole (CYP2C9 inhibitors),
an increased S(+)-ibuprofen exposure by
approximately 80 to 100% has been shown.
Reduction of the ibuprofen dose should be
considered when potent CYP2C9 inhibitors are
administered concomitantly, particularly when highdose ibuprofen is administered with either
voriconazole or fluconazole.

Fertility, Pregnancy and lactation
Fertility
The use of ibuprofen may impair fertility and is not recommended in women
attempting to conceive. In women who have difficulties conceiving or who are
undergoing investigation of infertility, withdrawal of ibuprofen should be considered
(see section 4.4).

Pregnancy
Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or
embryo/foetal development. Data from epidemiological studies suggest an increased
risk of miscarriage and of cardiac malformation and gastroschisis after the use of a
prostaglandin synthesis inhibitor in early pregnancy. The absolute risk of
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
the administration of a prostaglandin synthesis inhibitor has been shown to result in
increased pre- and post-implantation losses and embryo/foetal lethality. In addition,
increased incidences of various malformations, including cardiovascular, have also
been reported in animals given a prostaglandin synthesis inhibitor during the
organogenetic period. During the first and second trimesters of pregnancy, Abfen 600
mg Effervescent Granules should not be given unless clearly necessary. If Abfen 600
mg Effervescent Granules are used by a woman attempting to conceive or during the
first and second trimester, the dose should be kept as low and duration of treatment as
short as possible.
During the third trimester, 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 oligohydramnios.

At the end of pregnancy, prostaglandin synthesis inhibitors may expose the
mother and the neonate 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, ibuprofen is contraindicated during the last trimester of pregnancy.
Breastfeeding
In the limited studies so far available, NSAIDs can appear in the breast milk in very
low concentrations. NSAIDs should, if possible, be avoided when breastfeeding.

4.7

Effects on ability to drive and use machines
Undesirable effects such as dizziness, drowsiness, fatigue and visual disturbances are
possible after taking NSAIDs. If affected, patients should not drive or operate
machinery. This applies to a greater extent in combination with alcohol.

4.8

Undesirable effects

The most commonly observed adverse events are gastrointestinal in nature. Peptic
ulcers, perforation or GI bleeding, sometimes fatal, particularly in the elderly, may
occur (see section 4.4). Nausea, vomiting, diarrhoea, flatulence, constipation,
dyspepsia, abdominal pain, melaena, haematemesis, ulcerative stomatitis,
exacerbation of colitis and Crohn’s disease (see section 4.4) have been reported
following ibuprofen administration. Less frequently, gastritis has been observed.
Hypersensitivity: Hypersensitivity reactions have been reported following treatment
with NSAIDs. These may consist of (a) non-specific allergic reactions and
anaphylaxis (b) respiratory tract reactivity comprising asthma, aggravated asthma,
bronchospasm or dyspnoea, or (c) assorted skin disorders, including rashes of various
types, pruritus, urticaria, purpura, angioedema and, more rarely, exfoliative and
bullous dermatoses (including Stevens-Johnson syndrome, toxic epidermal necrolysis
and erythema multiforme).
Adverse events at least possibly related to ibuprofen are displayed by MedDRA
frequency convention and system organ class database. The following frequency
groupings are used: Very common (≥1/10), Common (≥1/100 to <1/10), Uncommon
(≥1/1000 to <1/100), Rare (≥1/10,000 to <1/1000), Very rare (<1/10,000) and Not
known (cannot be estimated from the available data).
System organ class

Frequency

Adverse reaction

Infections and infestations

Uncommon

Rhinitis

Blood and lymphatic system
disorders

Immune system disorders
Psychiatric disorders
Nervous system disorders

Eye disorders
Ear and labyrinth disorders
Respiratory, thoracic and
mediastinal disorders
Gastrointestinal disorders

Rare
Uncommon

Rare
Uncommon
Rare
Common
Uncommon
Rare
Uncommon
Rare
Uncommon
Rare
Uncommon
Common

Uncommon

Hepatobiliary disorders

Very rare
Not known
Uncommon

Skin and subcutaneous tissue
disorders

Rare
Very rare
Common
Uncommon

Very rare

Renal and urinary disorders

Uncommon

General disorders and
administration site conditions

Common
Rare

Meningitis aseptic
Leukopenia, thrombocytopenia,
neutropenia, agranulocytosis,
aplastic anaemia , haemolytic
anaemia
Anaphylactic reaction
Insomnia, anxiety
Depression, confusional state
Headache, dizziness
Paraesthesia, somnolence
Optic neuritis
Visual impairment
Toxic optic neuropathy
Hearing impaired
Tinnitus, vertigo
Asthma, bronchospasm,
dyspnoea
Dyspepsia, diarrhoea, nausea,
vomiting, abdominal pain,
flatulence, constipation,
melaena, haematemesis,
gastrointestinal haemorrhage
Gastritis, duodenal ulcer, gastric
ulcer, mouth ulceration,
gastrointestinal perforation
Pancreatitis
Colitis and Crohn´s disease
Hepatitis, jaundice, hepatic
function abnormal
Liver injury
Hepatic failure
Rash
Urticaria, pruritus, purpura,
angioedema, photosensitivity
reaction
Bullous dermatoses, including
Stevens-Johnson syndrome,
toxic epidermal necrolysis and
erythema multiforme
Tubulointerstitial nephritis,
nephrotic syndrome and renal
failure
Fatigue
Oedema

Clinical studies suggest that use of ibuprofen, particularly at a high dose (2400
mg/day ) may be associated with a small increased risk of arterial thrombotic events
(for example myocardial infarction or stroke) (see section 4.4).

Ibuprofen can cause prolongation of bleeding time through reversible inhibition of
platelet aggregation.
In the majority of cases where aseptic meningitis has been reported, there has been
some form of underlying autoimmune disease (in particular, systemic lupus
erythematosus and related connective tissue diseases).
Oedema, hypertension and heart failure as well as deterioration of ulcerative colitis
and Crohn’s disease have been reported in connection with NSAID treatment.
A transient sensation of burning in the mouth or throat may occur with Abfen 600 mg
Effervescent Granules.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is
important. It allows continued monitoring of the benefit/risk balance of the medicinal
product. Healthcare professionals are asked to report any suspected adverse reactions
via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard

4.9

Overdose
Toxicity
Signs and symptoms of toxicity have generally not been observed at doses below 100
mg/kg in the paediatric population or in adults. However, supportive care may be
needed in some cases. Paediatric populations have been observed to manifest signs
and symptoms of toxicity after ingestion of 400 mg/kg or greater.

Symptoms
Most patients who have ingested significant amounts of ibuprofen will manifest
symptoms within 4 to 6 hours.
The most frequently reported symptoms of overdose include nausea, vomiting,
abdominal pain, lethargy and drowsiness. Central nervous system (CNS) effects
include headache, tinnitus, dizziness, convulsion, and loss of consciousness.
Nystagmus, metabolic acidosis, hypothermia, renal effects, gastrointestinal bleeding,
coma, apnoea, diarrhoea and depression of the CNS and respiratory system have also
been rarely reported. Disorientation, excitation, fainting and cardiovascular toxicity,
including hypotension, bradycardia and tachycardia have been reported. In cases of
significant overdose, renal failure and liver damage are possible. Large overdoses are
generally well tolerated when no other drugs are being taken.
Therapeutic measures
Patients should be treated symptomatically as required. Within one hour of ingestion
of a potentially toxic amount, activated charcoal should be considered. Alternatively,
in adults, gastric lavage should be considered within one hour of ingestion of a
potentially life-threatening overdose.

Good urine output should be ensured.
Renal and liver function should be closely monitored.
Patients should be observed for at least four hours after ingestion of potentially toxic
amounts.
Frequent or prolonged convulsions should be treated with intravenous diazepam.
Other measures may be indicated by the patient’s clinical condition.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties

Pharmacotherapeutic classification: Anti-inflammatory and antirheumatic products,
nonsteroids; propionic acid derivatives.
ATC code: M01AE01
Ibuprofen belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). It
contains the propionic acid derivative p-isobutyl-hydratropic acid with the generic
name ibuprofen. Ibuprofen has anti-inflammatory, analgesic and antipyretic effects.
The antiphlogistic effect is comparable with that of acetylsalicylic acid (e.g. Aspirin)
and indometacin. The pharmacological effect of ibuprofen is probably associated with
its ability to inhibit prostaglandin synthesis. Ibuprofen prolongs bleeding time through
reversible inhibition of platelet aggregation.
Experimental data suggest that ibuprofen may competitively inhibit the effect of low
dose acetylsalicylic acid on platelet aggregation when they are dosed concomitantly.
Some pharmacodynamic studies show that when single doses of ibuprofen 400 mg
were taken within 8 h before or within 30 min after immediate release acetylsalicylic
acid dosing (81 mg), a decreased effect of acetylsalicylic acid on the formation of
thromboxane or platelet aggregation occurred. Although there are uncertainties
regarding extrapolation of these data to the clinical situation, the possibility that
regular, long-term use of ibuprofen may reduce the cardioprotective effect of lowdose acetylsalicylic acid cannot be excluded. No clinically relevant effect is
considered to be likely for occasional ibuprofen use (see section 4.5).
Ibuprofen inhibits renal prostaglandin synthesis. In patients with normal renal
function this effect is of no particular significance. In patients with chronic renal
insufficiency, decompensated heart or liver insufficiency as well as conditions

involving changes in plasma volume, the inhibited prostaglandin synthesis can lead to
acute renal insufficiency, fluid retention and heart failure (see section 4.3).

5.2

Pharmacokinetic properties
Absorption
Ibuprofen is rapidly absorbed from the gastrointestinal tract with a bioavailability of
80-90%. Peak serum concentrations occur one to two hours after administration. If
administered with food, peak serum concentrations are lower and achieved more
slowly than when taken on an empty stomach Food does not affect markedly total
bioavailability.

Distribution
Ibuprofen is extensively bound to plasma proteins (99%). Ibuprofen has a small
volume of distribution being about 0.12-0.2 L/kg in adults.

Biotransformation
Ibuprofen is rapidly metabolized in the liver through cytochrome P450, preferentially
CYP2C9, to two primary inactive metabolites, 2-hydroxyibuprofen and 3carboxyibuprofen. Following oral ingestion of the drug, slightly less than 90% of an
oral dose of ibuprofen can be accounted for in the urine as oxidative metabolites and
their glucuronic conjugates. Very little ibuprofen is excreted unchanged in the urine.
Elimination
Excretion by the kidney is both rapid and complete. The elimination half-life is
approximately 2 hours. The excretion of ibuprofen is virtually complete 24 hours
after the last dose.

Special populations
Elderly
Given that no renal impairment exists, there are only small, clinically insignificant
differences in the pharmacokinetic profile and urinary excretion between young and
elderly.

Paediatric population
The systemic exposure of ibuprofen following weight adjusted therapeutic dosage (5
mg/kg to 10 mg/kg bodyweight) in children aged 1 year or over, appears similar to
that in adults.
Children 3 months to 2.5 years appeared to have a higher volume of distribution
(L/kg) and clearance (L/kg/h) of ibuprofen than did children >2.5 to 12 years of age.

Renal impairment
For patients with mild renal impairment, increased unbound (S)-ibuprofen, higher
AUC values for (S)-ibuprofen and increased enantiomeric AUC (S/R) ratios as
compared with healthy controls have been reported.
In end-stage renal disease patients receiving dialysis the mean free fraction of
ibuprofen was about 3% compared with about1% in healthy volunteers. Severe
impairment of renal function may result in accumulation of ibuprofen metabolites.
The significance of this effect is unknown. The metabolites can be removed by
haemodialysis (see sections 4.2, 4.3 and 4.4).
Hepatic impairment
Alcoholic liver disease with mild to moderate hepatic impairment did not result in
substantially altered pharmacokinetic parameters.
In cirrhotic patients with moderate hepatic impairment (Child Pugh’s score 6-10)
treated with racemic ibuprofen an average 2-fold prolongation of the half-life was
observed and the enantiomeric AUC ratio (S/R) was significantly lower compared to
healthy controls suggesting an impairment of metabolic inversion of (R)-ibuprofen to
the active (S)-enantiomer (see sections 4.2, 4.3 and 4.4).

5.3

Preclinical safety data
There are no preclinical data of relevance for the safety assessment, apart from what
has already been taken into account in this summary of product characteristics.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients

Croscarmellose sodium
Malic acid
Microcrystalline cellulose
Saccharin sodium
Sucrose
Povidone
Orange flavour
Sodium laurilsulfate

Sodium hydrogen carbonate
Sodium carbonate, anhydrous

6.2

Incompatibilities
Not applicable.

6.3

Shelf life

3 years

6.4

Special precautions for storage
Do not store above 25°C. Store in the original package in order to protect from light
and moisture.

6.5

Nature and contents of container
A heat-sealed sachet consisting of a paper/polythene/aluminium foil/polythene
laminate.
Pack sizes: 10, 20, 30, 40, 50 sachets.
Not all pack sizes may be marketed.

6.6

Special precautions for disposal
No special requirements for disposal.

7

MARKETING AUTHORISATION HOLDER
BGP Products Ltd.
Abbott House
Vanwall Business Park
Vanwall Road
Maidenhead
Berkshire
SL6 4XE
United Kingdom

8

MARKETING AUTHORISATION NUMBER(S)
PL 43900/0008

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
09/05/2013

10

DATE OF REVISION OF THE TEXT
18/02/2016

Expand view ⇕

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

Hide