PROFENID 50mg caps.

Egypt - English - EDA (Egyptian Drug Authority)

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Available from:
SANOFI AVENTIS-FRANCE
Dosage:
50 mg
Pharmaceutical form:
capsule
Units in package:
24 capsules
Manufactured by:
ALEXANDRIA
Authorization number:
18735
Authorization date:
1995-08-01

Documents in other languages

Patient Information leaflet Patient Information leaflet - Arabic

29-10-2020

20/07/2011 16:28 - VISTAlink folder 730160 - Page 1/4

Cardiovascular Risk

NSAIDs may cause an increased risk of serious cardiovascular

thrombotic events, myocardial infarction, and stroke, which

can be fatal. This risk may increase with duration of use. Patients

with cardiovascular disease or risk factors for cardiovascular disease

may be at greater risk NSAIDs is contraindicated for the treatment

of peri-operative pain in the setting of coronary artery bypass graft

(CABG) surgery.

Gastrointestinal Risk

NSAIDs cause an increased risk of serious gastrointestinal adverse

events including inflammation, bleeding, ulceration, and perforation

of the stomach or intestines, which can be fatal. These events can

occur at any time during use and without warning symptoms.

Elderly patients are at greater risk for serious gastrointestinal events.

Composition

Each capsule contains

Active ingredient: Ketoprofen ………..50mg

Inactive ingredient: Lactose & magnesium stearate.

Pharmaceutical form

Capsules.

Pharmacological action

Pharmacodynamics: Ketoprofen is a non-steroidal, anti-inflammatory

arylcarboxylic acid derivative belonging to the propionic acid group of

NSAIDs. Ketoprofen has anti-inflammatory, antipyretic properties and has

central and peripheral analgesic activity. However, its mode of action is

not fully explained. It inhibits prostaglandin synthetase and platelet

aggregation.

Pharmacokinetics:

Absorption: Ketoprofen is rapidly and completely absorbed from the

gastrointestinal tract. Maximal plasma levels are reached within 60 to 90

minutes after oral administration (45 to 60 minutes after rectal

administration). When ketoprofen is administered with food, the rate of

absorption is slowed, resulting in delayed and reduce peak concentration

(Cmax); however, its total bioavailibility is not altered.

*Sustained-released formulations: when administered with high caloric

food, a slight decrease of bioavailibility (13%) has been observed. For the

different slow-release formulations available in the different countries, a

specific statement should be provided by each affiliate to describe the

particular absorption characteristics.

Distribution: The drug is 99% bound to plasma protein. Ketoprofen diffuses

into synovial fluid and in intraarticular, capsular, synovial and tendon

tissues. Ketoprofen crosses the blood brain barrier and the placental

barrier. The plasma elimination half-life is approximately 2 hours.The

volume of distribution is approximately 7 L.

*Sustained-release formulations (i.e. Profenid L.P. 200 mg): after the

plateau (fifth to twelfth hour), ketoprofen levels decrease with an

apparent half-life of 3 to 4 hours. No accumulation of the drug was

found after repeated doses.

Metabolism: The biotransformation of ketoprofen is characterised by

two main processes, hydroxylation and conjugation with glucuronic acid,

the latter being the main pathway in man. Excretion of ketoprofen as

unchanged drug is very low (less than 1%). Almost all administered

ketoprofen is excreted as metabolites in urine, of which 65 to 85% of

administered dose is excreted as a glucuronide metabolite.

Elimination: 50% of the administered dose is excreted in the urine within

6 hours following drug administration. Within five days following the

oral administration, approximately 75 to 90% of the dose is mainly

excreted in the urine. Fecal excretion is very low (1 to 8%).

Indications

The indications of ketoprofen are based on its anti-inflammatory,

analgesic and antipyretic properties. Ketoprofen is indicated for

symptomatic treatment of:

- Rheumatoid arthritis

- Degenerative joint diseases

- Musculoskeletal and joint disorders such as tendinitis and sprain

- Pain, regardless of the origin, such as dental pain, headache and

primary dysmenorrhea.

Dosage and administration

General

Anti-inflammatory dosage: The recommended starting dose is 150 to

300 mg/day in 3 divided doses. Once the maintenance dosage has been

established (usually 100 to 200 mg/day), the patient may be tried on a

twice daily dose regimen. Alternatively, switching to the once daily form

at the same dosage may be considered. The recommended maximum

daily dose is 300mg.

Management of pain and primary dysmenorrhea: The usual

recommended dose is 25 to 50 mg, every 6 to 8 hours as necessary. The

total daily dose should not exceed 300mg.

Special Populations

Patients with impaired renal function and the elderly: It is advisable to

reduce the initial dosage and maintain such patients on the minimal

effective dose. Individual adjustment may be considered, only after good

individual tolerance has been ascertained.

Patients with impaired hepatic function: These patients should be

carefully monitored and kept at the minimal effective daily dosage.

Children: The safety and effectiveness of ketoprofen suppositories have

not been established.

Administration: Food effect: The oral forms should be taken with fluids,

preferably with food.

Contraindications

Ketoprofen is contraindicated in patients, who have a history of

hypersensitivity reactions such as asthmatic attacks or other allergic-type

reactions to ketoprofen, ASA or other NSAIDs. Severe, rarely fatal,

anaphylactic reactions have been reported in such patients. Ketoprofen

is also contraindicated in the following cases:

- Severe heart failure

- Active or history of peptic ulcer/hemorrhage

- History of gastrointestinal bleeding or perforation, related to

previous NSAIDs therapy

- Severe hepatic insufficiency

- Severe renal insufficiency

- Third trimester of pregnancy

Side Effects

Gastrointestinal effects:

− Gastralgia, dyspepsia, abdominal pain, nausea, vomiting,

diarrhea, constipation, flatulence.

− Gastritis, stomatitis, exacerbation of colitis and Crohn’s disease.

− Peptic ulcer, gastrointestinal bleeding and perforation.

Hypersensitivity reactions:

− Dermatological reactions: rash, pruritus, urticaria, angioedema

− Respiratory reactions: asthmatic attack, bronchospasm

(particularly in patients with known hypersensitivity to ASA and

other NSAIDs).

− Anaphylactic reactions (including shock).

Skin reactions: Photosensitivity, alopecia, bullous eruptions including

Stevens-Johnson and toxic epidermal necrolysis.

Peripheral and central nervous system: Dizziness, paresthesia,

convulsions.

Psychotic disorders: Somnolence, mood disorders.

Vision disorders: Visual disturbances such as blurred vision (see section 6).

Hearing disorders: Tinnitus.

Renal system: Abnormal renal function tests, acute renal failure,

interstitial nephritis, nephritic syndrome.

Liver system: Elevation of transaminase levels, rare cases of hepatitis.

Haematology: Thrombocytopenia, anemia due to bleeding,

agranulocytosis, bone marrow aplasia.

Cardiovascular system: Hypertension, vasodilatation.

Body as a whole: Headache, oedema, weight gain, taste perversion.

Drug Interactions

Not recommended drug associations: Other NSAIDs (including

cyclooxygenase-2 selective inhibitors) and high dose salicylates:

Increased risk of gastrointestinal ulceration and bleeding.

Anticoagulants (heparin and warfarin) and platelet aggregation inhibitors

(i.e.ticlopidine, clopidogrel): Increased risk of bleeding. If coadministration

is unavoidable, patient should be closely monitored.

Lithium: Risk of elevation of lithium plasma levels, sometimes reaching

toxic levels due to decreased lithium renal excretion. Where necessary,

plasma lithium levels should be closely monitored and the lithium

dosage levels adjusted during and after NSAID therapy.

Methotrexate at doses greater than 15mg/week: Increased risk of

haematologic toxicity of methotrexate, particularly if administered at

high doses (> 15 mg/week), possibly related to displacement of

protein-bound methotrexate and to its decreased renal clearance.

Drug associations requiring precautions for use.

Corticosteroids: increased risk of gastrointestinal ulceration or bleeding.

Diuretics: Patients and particularly dehydrated patients taking diuretics

are at a greater risk of developing renal failure secondary to a decrease

in renal blood flow caused by prostaglandin inhibition. Such patients

should be rehydrated before initiating coadministration therapy and

renal function monitored when the treatment is started.

ACE inhibitors and Angiotensin II Antagonists: In patients with

compromised renal function (e.g. dehydrated patients or elderly patients

the co-administration of an ACE inhibitor or Angiotensin II antagonist

and agents that inhibit cyclo-oxygenase may result in further

deterioration of renal function, including possible acute renal failure.

Methotrexate at doses lower than 15mg/week: During the first weeks of

combination treatment, full blood count should be monitored weekly. If

there is any alteration of the renal function or if the patient is elderly,

monitoring should be done more frequently.

Pentoxifyllin: There is an increased risk of bleeding. More frequent

clinical monitoring and monitoring of bleeding time is required.

Drug associations to be taken into account

Antihypertensive agents (beta-blockers, angiotensin converting enzyme

inhibitors, diuretics): Risk of decreased antihypertensive potency

(inhibition of vasodilator prostaglandins by NSAIDs).

Thrombolytics: Increased risk of bleeding.

Probenecid: Concomitant administration of probenecid may markedly

reduce the plasma clearance of ketoprofen.

Selective serotonin reuptake inhibitors (SSRIs): Increased risk of

gastrointestinal bleeding

Pregnancy

During the first and second trimester: In mice and rats, there is no

evidence of teratogenic or embryotoxicity. In the rabbit, slight

embryotoxicity likely related to maternal toxicity has been reported.

As the safety of ketoprofen in pregnant women has not been evaluated,

the use of ketoprofen during the first and second trimester of pregnancy

should be avoided.

During the third trimester of pregnancy: All prostaglandin synthetase

inhibitors including ketoprofen may induce cardiopulmonary and renal

toxicity in the fetus. At the end of the pregnancy, prolonged bleeding

time in both the mother and child may occur. Therefore, ketoprofen is

contraindicated during the last trimester of pregnancy.

Lactation

No data are available on excretion of ketoprofen in human milk.

Ketoprofen is not recommended in nursing mothers.

Warnings

Undesirable effects may be minimized by using the minimum effective

dose for the shortest duration necessary to control symptoms. Caution

should be advised in patients receiving concomitant medications which

could increase the risk of ulceration or bleeding, such as oral corticoster-

oids, anticoagulants such as warfarin, selective serotonin-reuptake

inhibitors or antiplatelet agents such as aspirin.

Gastrointestinal bleeding, ulceration and perforation: 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.

Elderly: The elderly have an increased frequency of adverse reactions to

NSAIDs especially gastrointestinal bleeding and perforation which may

be fatal. Serious skin reactions, some of them fatal, including exfoliative

dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis,

have been reported very rarely in association with the use of NSAIDs.

Patients appear to be at highest risk of these reactions early in the course

of therapy, the onset of the reaction occurring in the majority of cases

within the first month of treatment.

Precautions

Patients with active or a past history of peptic ulcer. NSAIDs should be

given with care to patients with a history of gastrointestinal disease

(ulcerative colitis, Crohn’s disease) as their condition may be exacerbated.

At the start of treatment, renal function must be carefully monitored in

patients with heart failure, cirrhosis and nephrosis, in patients receiving

diuretic therapy, in patients with chronic renal impairment, particularly

if the patient is elderly. In these patients, administration of ketoprofen

may induce a reduction in renal blood flow caused by prostaglandin

inhibition and lead to renal decomposition. Caution is required in

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. As with all NSAIDs, careful

consideration should be given when treating patients with existing

uncontrolled hypertension, congestive heart failure, established

ischaemic heart disease, peripheral arterial disease, and/or cerebrovascu-

lar disease, as well as, before initiating long term treatment in patients

with risk factors for cardiovascular disease (e.g. hypertension, hyperlipi-

daemia, diabetes mellitus, smoking). As with other NSAIDs, in the

presence of an infectious disease, it should be noted that the

anti-inflammatory, analgesic and the antipyretic properties of

ketoprofen may mask the usual signs of infection progression such as

fever. In patients with abnormal liver function tests or with a history of

liver disease, transaminase levels should be evaluated periodically,

particularly during long term therapy. Rare cases of jaundice and

hepatitis have been described with ketoprofen. If visual disturbances

such a blurred vision occur, treatment should be discontinued. The use

of NSAIDs 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 the NSAIDs should be considered.

Storage

Store at a temperature not exceeding 30º C in a dry place.

Keep all medicines out of reach of children

Package

Profenid ® 50mg: Cartoon box containing 2 strips, each strip

contains 12 capsules and an inner leaflet

Economy pack: Cartoon box containing 50 strips, each strip

contains 4 capsules and an inner leaflet

Produced by sanofi-aventis Egypt s.a.e.

Under license of sanofi-aventis / France

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