Ibuprofen Lysine 200 & 400 mg F.C tablet
Category:
Anti-inflammatory Drugs, Nonsteroidal
Chemistry:
Chemical name : (2S)-2,6-diaminohexanoic acid; 2-[4-(2-methylpropyl)phenyl]propanoic acid. It has the following structural formula:
The molecular formula is C19H32N2O4, representing a molecular weight of 352.475g/mol.
Pharmacokinetics:
Most pharmacokinetic data obtained following the administration of ibuprofen acid also apply to ibuprofen lysine.
Ibuprofen is well absorbed from the gastrointestinal tract. Ibuprofen is extensively bound to plasma proteins. Maximum plasma concentrations are reached 45 minutes after ingestion if taken on an empty stomach. When taken with food peak serum concentration occurs 1 - 2 hours after administration. However, ibuprofen is more rapidly absorbed from the gastrointestinal tract following the administration of Ibuprofen Lysine 400mg Tablets, with peak serum concentration occurring approximately 38 minutes after administration when taken on an empty stomach.
Ibuprofen is metabolised in the liver to two major metabolites with primary excretion via the kidneys, either as such or as major conjugates, together with a negligible amount of unchanged ibuprofen. Excretion by the kidney is both rapid and complete.
Elimination half-life is approximately 2 hours.
Indications:
For the relief of headache and migraine.
Contraindications:
- Hypersensitivity to ibuprofen or any of the excipients 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 anti-inflammatory drugs.
- Active or history of recurrent peptic ulcer/haemorrhage (two or more distinct episodes of proven ulceration or bleeding).
- History of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
- Severe heart failure (NYHA Class IV), renal failure or hepatic failure.
- Last trimester of pregnancy.
Warnings & Precautions:
-The elderly have an increased frequency of adverse reactions to NSAIDs .
-Bronchospasm may be precipitated in patients suffering from, or with a history of, bronchial asthma or allergic disease.
-The use of Ibuprofen with concomitant NSAIDs including cyclooxygenase-2 selective inhibitors should be avoided.
-Systemic lupus erythematosus and mixed connective tissue disease – increased risk of aseptic meningitis .
-Renal impairment as renal function may further deteriorate.
-Hepatic dysfunction .
-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.
-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.
-There is some evidence that drugs which inhibit cyclooxygenase/ prostaglandin synthesis may cause impairment of female fertility by an effect on ovulation. This is reversible on withdrawal of treatment.
-NSAIDs should be given with care to patients with a history of gastrointestinal disease (ulcerative colitis, Crohn's disease) as these conditions may be exacerbated.
-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 aspirin.
-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 for 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. Ibuprofen should be discontinued at the first appearance of skin rash, mucosal lesions, or any other sign of hypersensitivity.
Pregnancy and Breast – feeding:
Pregnancy
During the first and second trimester of pregnancy, ibuprofen should not be given unless clearly necessary. It is contraindicated during the third trimester of pregnancy.
Breastfeeding
Ibuprofen appears in the breast milk in very low concentration and is unlikely to affect the breast-fed infant adversely.
Drug Interactions:
Ibuprofen (like other NSAIDs) should be avoided in combination with:
-Concomitant administration of ibuprofen and acetylsalicylic acid is not generally recommended because of the potential of increased adverse effects, unless low-dose aspirin (not above 75mg daily) has been advised by a doctor.
-Avoid concomitant use of two or more NSAIDs as this may increase the risk of adverse effects. Ibuprofen should be used with caution in combination with:
Corticosteroids, Antihypertensives (ACE inhibitors and Angiotensin II Antagonists) and diuretics, Anticoagulants: NSAIDs may enhance the effects of anti-coagulants, such as warfarin.
Antiplatelet agents , selective serotonin reuptake inhibitors (SSRIs), Cardiac glycosides, Lithium,
Methotrexate, Ciclosporin, Tacrolimus.
Mifepristone: NSAIDs should not be used for 8-12 days after mifepristone administration as NSAIDs can reduce the effect of mifepristone.
Zidovudine: Increased risk of haematological toxicity when NSAIDs are given with zidovudine. There is evidence of an increased risk haemarthroses and haematoma in HIV (+) haemophiliacs receiving concurrent treatment with zidovudine and ibuprofen.
Quinolone antibiotics: Patients taking NSAIDs and quinolones may have an increased risk of developing convulsions.
Adverse Reactions:
Severe
intraventricular hemorrhage , apnea , enterocolitis , renal failure (unspecified) , seizures , heart failure , oliguria , GI perforation , ileus , GI bleeding , pulmonary hypertension .
Moderate
anemia , hyperuricemia , edema , hematuria , sinus tachycardia , hypotension , hyperglycemia , bleeding , prolonged bleeding time , gastritis , skin ulcer , jaundice , hepatitis , cholestasis , hyperbilirubinemia , thrombocytopenia , neutropenia .
Mild
gastroesophageal reflux , skin irritation , infection .
OVERDOSE:
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. 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.
DOSAGE AND ADMINISTRATION:
For oral administration and short-term use only.
Undesirable effects may be minimised by using the lowest effective dose for the shortest duration necessary to control symptoms.
If in children and adolescents this medicinal product is required for more than 3 days, or if symptoms worsen a doctor should be consulted.
Adults should consult a doctor if symptoms persist or worsen, or if the product is required for more than 10 days.
Children and Adolescents between 12 and 18 years: Take 1 Tablet with water, up to three times a day as required.
Adults: Take 1 Tablet with water, up to three times a day as required.
Leave at least 4 hours between doses.
Do not take more than 3 Tablets in any 24 hour period.
Storage:
store below 30˚ C and keep away from humidity & light.
How supplied:
White opaque PVC (300 micron), Blister of 10 tablets in Paper boxes of 20 tablets ,Paper leaflet in a shrink wrap
References:
1) PDR.net 2019
2) medicines.org.uk 2019
3) drugbank 2019