Aceclofenac 100 mg Film-coated Tablets
1. Name of the medicinal productAceclofenac a hundred mg Film-lined Tablets
2. Qualitative and quantitative composition
Each pill carries one hundred mg aceclofenac.
For the total list of excipients, see section 6.1.
Three. Pharmaceutical form
Film-coated tablet.
Round white or off-white in shade bi-convex movie-covered capsules marked “G” on one aspect.
4. Clinical particulars
4.1 Therapeutic indicators
Aceclofenac is indicated for the relaxation of ache and inflammation in osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
Four.2 Posology and approach of management
Posology
Adults: The most advocated dose is 2 hundred mg every day, taken as separate doses of one hundred mg, one pill in the morning and one pill inside the night.
Children: There are not any medical information assisting using aceclofenac in children consequently its use isn't advocated.
Elderly: Caution should be exercised inside the remedy of aged sufferers, who are commonly more liable to destructive reactions, and who are much more likely to be tormented by impaired renal, cardiovascular or hepatic feature and receiving concomitant remedy. If an NSAID is requisite, the lowest powerful dose ought to be used and for the shortest possible period. The aged ought to be monitored for GI bleeding often for the duration of NSAID remedy. The pharmacokinetics of aceclofenac aren't altered in aged sufferers, consequently it is not considered necessary to adjust the dose or dose frequency.
Renal insufficiency: There is not any proof to suggest that the dosage wishes to be altered for sufferers with mild renal impairment, but caution need to be exercised (see segment four.Four).
Hepatic insufficiency: There is a few evidence that the dose of aceclofenac should be decreased in patients with hepatic impairment. It is recommended that an preliminary day by day dose of 100 mg is used.
Undesirable outcomes can be minimised by means of using the lowest powerful dose for the shortest duration important to govern signs and symptoms (see section 4.4).
Method of management:
For oral use. Aceclofenac Tablets ought to be swallowed complete with liquid.
When aceclofenac became administered to fasting and fed wholesome volunteers, handiest the fee and not the volume of the drug's absorption became affected. For this reason, aceclofenac may be desirous about or after food.
Four.3 Contraindications
• hypersensitive reaction to the lively substance or to any of the excipients indexed in section 6.1
• patients with history of gastrointestinal bleeding or perforation, related to preceding NSAIDs remedy
• energetic or records of recurrent peptic ulcer/haemorrhage (two or extra distinct episodes of confirmed ulceration or bleeding)
• sufferers with active bleedings or bleeding issues
• sufferers with hepatic failure and renal failure
• sufferers with installed congestive coronary heart failure (NYHA magnificence II-IV), ischaemic coronary heart ailment, peripheral arterial disorder and/or cerebrovascular disease
• patients in whom acetylsalicylic acid or NSAIDs precipitate assaults of asthma, acute rhinitis, angioedema or urticaria or who're hypersensitive to these tablets
• 0.33 trimester of pregnancy
4.Four Special warnings and precautions for use
The use of aceclofenac with other concomitant NSAIDs consisting of cyclooxygenase-2-selective inhibitors need to be prevented (see segment 4.5).
Undesirable effects may be minimised with the aid of the use of the bottom powerful dose for the shortest duration necessary to control symptoms (see phase 4.2, and GI and cardiovascular risks under).
Elderly
The aged have an improved frequency of detrimental reactions to NSAIDs specially gastrointestinal bleeding and perforation which can be fatal (see phase 4.2).
Gastrointestinal
Close clinical surveillance is needed in sufferers with the following conditions as those may be exacerbated (see section four.Eight):
- signs indicative of gastrointestinal disorder concerning both the higher or lower gastrointestinal tract
- a history suggestive of gastrointestinal ulceration, bleeding or perforation
- ulcerative colitis
- Crohn's ailment
- haematological abnormalities
GI bleeding, ulceration or perforation, which may be deadly, were pronounced with all NSAIDs at any time in the course of remedy, with or without caution signs or a preceding history of serious GI events.
The risk of GI bleeding, ulceration or perforation is better with growing NSAID doses, in sufferers with a history of ulcer, especially if complicated with haemorrhage or perforation (see phase 4.3), and within the elderly. These patients must start treatment on the lowest dose to be had. Combination therapy with defensive retailers (e.G. Misoprostol or proton pump inhibitors) need to be taken into consideration for those sufferers, and also for sufferers requiring concomitant low dose aspirin, or other drugs possibly to boom gastrointestinal chance (see below and section four.5).
Patients with a records of GI toxicity, particularly whilst elderly, ought to report any unusual belly symptoms (in particular GI bleeding) especially inside the initial tiers of remedy. Caution ought to be recommended in patients receiving concomitant medicinal drugs that could growth the chance of ulceration or bleeding, which includes systemic corticosteroids, anticoagulants along with warfarin, selective serotonin-reuptake inhibitors or anti-platelet marketers which includes aspirin (see section 4.5).
When GI bleeding or ulceration occurs in sufferers receiving aceclofenac, the remedy should be withdrawn.
SLE and mixed connective tissue sickness
In sufferers with systemic lupus erythematosus (SLE) and mixed connective tissue problems there can be an multiplied danger of aseptic meningitis (see phase 4.4).
Hypersensitivity and skin reactions
As with different NSAIDs, hypersensitive reactions, consisting of anaphylactic/anaphylactoid reactions, can also arise with out earlier publicity to the drug. Serious skin reactions, some of them fatal, including exfoliative dermatitis, Stevens-Johnson syndrome, and poisonous epidermal necrolysis, have been said very rarely in association with using NSAIDs (see phase 4.Eight).
Patients look like at highest threat of those reactions early within the course of therapy, the onset of the reaction happening in the majority of instances inside the first month of remedy. Aceclofenac should be discontinued at the first look of pores and skin rash, mucosal lesions, or another signal of allergic reaction.
Exceptionally, varicella can trigger serious cutaneous and tender tissues infections complications. To date, the contributing position of NSAIDs within the worsening of those infections can not be dominated out. Thus, it's far advisable to avoid use of aceclofenac in case of varicella.
Cardiovascular and cerebrovascular
Appropriate tracking and advice are required for sufferers with a history of hypertension and/or slight to slight congestive coronary heart failure, as fluid retention and oedema were pronounced in association with NSAID therapy.
Patients with congestive heart failure (NYHA-I), and sufferers with large hazard factors for cardiovascular occasions (e.G. Hypertension, hyperlipidaemia, diabetes mellitus, smoking) have to most effective be treated with aceclofenac after cautious attention. As the cardiovascular risks of aceclofenac can also boom with dose and period of exposure, the shortest length feasible and the lowest powerful each day dose need to be used. The patient's want for symptomatic relief and reaction to remedy ought to be re-evaluated periodically.
Aceclofenac should also be administered with warning and below near medical surveillance to sufferers with a history of cerebrovascular bleeding.
Clinical trial and epidemiological facts advise that use of a few NSAIDs (specifically at high doses and in long time treatment) can be associated with a small accelerated hazard of arterial thrombotic occasions (as an instance myocardial infarction or stroke). There are inadequate facts to exclude this sort of risk for aceclofenac.
Cardiovascular, renal and hepatic impairment
The management of an NSAID may additionally purpose a dose dependent reduction in prostaglandin formation and precipitate renal failure. The importance of prostaglandins in maintaining renal blood flow should be taken under consideration in sufferers with impaired cardiac or renal function, liver disorder, the ones being handled with diuretics or convalescing from main surgical operation and the aged.
Renal feature have to be monitored in those sufferers (see additionally section 4.3)
Renal
Patients with slight to slight renal or cardiac impairment and the aged should be saved under surveillance, since the usage of NSAIDs can also bring about deterioration of renal feature. The lowest effective dose have to be used and renal characteristic monitored frequently. Effects on renal function are normally reversible on withdrawal of aceclofenac.
Hepatic
Close medical surveillance is needed in sufferers affected by mild to moderate hepatic feature impairment. Aceclofenac ought to be discontinued if peculiar liver function assessments persist or get worse, medical signs or signs constant with liver disease expand or if other manifestations occur (eosinophilia, rash). Hepatitis may additionally arise without prodromal symptoms.
Use of NSAIDs in sufferers with hepatic porphyria might also trigger an assault.
Haematological
Aceclofenac may also reversibly inhibit platelet aggregation (see phase 4.Five, anticoagulants).
Respiratory problems
Caution is needed if administered to patients laid low with or with a preceding records of bronchial asthma when you consider that NSAIDs have been pronounced to precipitate bronchospasm in such patients.
Long-time period remedy
All sufferers who are receiving lengthy-term remedy with NSAIDs have to be monitored as a precautionary degree (e.G. Renal, hepatic characteristic (elevation of liver enzymes may also occur) and blood counts).
4.Five Interaction with other medicinal products and different styles of interaction
Lithium: Several NSAID tablets inhibit the renal clearance of lithium, resulting in improved serum concentrations of lithium. The mixture must be averted until frequent monitoring of lithium can be carried out.
Cardiac glycosides: NSAIDs may exacerbate cardiac failure, reduce the GFR (glomerular filtration fee) and inhibit the renal clearance of glycosides, resulting in extended plasma glycoside levels. The combination should be prevented unless frequent monitoring of glycosides can be completed.
Diuretics: Aceclofenac, like different NSAIDs, might also inhibit the hobby of diuretics. Although it was not proven to affect blood stress control when co-administered with bendroflumethiazide, interactions with other diuretics can not be ruled out. When concomitant management with potassium-sparing diuretics is employed, serum potassium should be monitored. Diuretics can boom the hazard of nephrotoxicity of NSAIDs.
Antihypertensives: NSAIDs may additionally lessen the effect of antihypertensives. The danger of acute renal insufficiency, that is usually reversible, can be expanded in a few patients with compromised renal function (e.G. Dehydrated patients or aged sufferers) when ACE- inhibitors or angiotensin II receptor antagonists are mixed with NSAIDs. Therefore, the aggregate ought to be administered with warning, specially in the aged. Patients need to be properly hydrated and consideration have to take delivery of to tracking of renal feature after initiation of concomitant remedy, and periodically thereafter.
Anticoagulants: Like different NSAIDs, aceclofenac may additionally beautify the activity of anticoagulants including warfarin (see segment four.Four). Close tracking of patients on combined anticoagulant and Aceclofenac remedy need to be undertaken.
Antidiabetic retailers: Clinical studies have shown that diclofenac can be given collectively with oral antidiabetic agents without influencing their scientific effect. However, there were remoted reviews of hypoglycaemic and hyperglycaemic effects. Thus with aceclofenac, consideration must accept to adjustment of the dosage of hypoglycaemic dealers.
Methotrexate: The feasible interplay among NSAIDs and methotrexate need to be borne in thoughts additionally when low doses of methotrexate are used, especially in patients with reduced renal feature. When mixture remedy has to be used, the renal characteristic have to be monitored. Caution ought to be exercised if each an NSAID and methotrexate are administered within a 24-hour duration, since the methotrexate levels may additionally boom and result in elevated toxicity.
Mifepristone: NSAIDs need to now not be used for 8-12 days after mifepristone management as NSAIDs can lessen the impact of mifepristone.
Other NSAIDs: Concomitant therapy with acetylsalicylic acid and different NSAIDs, which include cyclo-oxygenase-2 selective inhibitors, ought to be averted as they'll boom the frequency of side outcomes, consisting of GI bleeding (see phase 4.Four).
Corticosteroids: improved chance of gastrointestinal ulceration or bleeding (see segment 4.4).
Anti-platelet sellers and selective serotonin reuptake inhibitors (SSRIs): blended with NSAIDs can also increase the risk of gastrointestinal bleeding (see phase 4.Four).
Ciclosporin, tacrolimus: Administration of NSAID tablets together with ciclosporin or tacrolimus is thought to growth the threat of nephrotoxicity due to decreased synthesis of prostacyclin in the kidney. During aggregate therapy it's far consequently vital to cautiously display renal feature.
Quinolone antimicrobials: Convulsions may additionally occur because of an interplay between quinolones and NSAIDs. This may additionally arise in patients without or with a preceding records of epilepsy or convulsions. Therefore, caution have to be exercised whilst thinking about using a quinolone in sufferers who are already receiving a NSAID.
Zidovudine: When NSAIDs are given with zidovudine there may be an elevated danger of haematological toxicity. There are indications of an elevated threat of haemoarthroses and haematoma in HIV(+) haemophiliacs receiving concurrent remedy with zidovudine and ibuprofen.
4.6 Fertility, pregnancy and lactation
Pregnancy
There is not any facts on using aceclofenac throughout pregnancy. Inhibition of prostaglandin synthesis may also adversely have an effect on the being pregnant and/or the embryo/foetal development. Data from epidemiological studies endorse an accelerated threat of miscarriage, cardiac malformation or gastroschisis after use of prostaglandin synthesis inhibitor in early being pregnant. The absolute threat for cardiovascular malformation changed into accelerated from less than 1%, up to about 1.5%. The threat is thought to increase with dose and period of remedy.
In animals, management of a prostaglandin synthesis inhibitor has been proven to bring about accelerated pre- and put up-implantation loss and embryo-foetal lethality. In addition, accelerated incidences of numerous malformations, such as cardiovascular, were pronounced in animals given a prostaglandin synthesis inhibitor at some stage in the organogenetic period. During the primary and 2nd trimester of being pregnant, aceclofenac must not be given unless honestly necessary. If aceclofenac is utilized by a lady trying to conceive, or in the course of the first and 2d trimester of pregnancy, the dose ought to be saved as low and length of remedy as brief as feasible.
During the 0.33 trimester of pregnancy, all prostaglandin synthesis inhibitors might also reveal:
The foetus to:
- cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary high blood pressure);
- renal dysfunction, which can also development to renal failure with oligo-hydroamniosis;
The mother and the neonate, at the stop of pregnancy, to:
- feasible prolongation of bleeding time, an anti-aggregating impact which may occur even at very low doses;
- inhibition of uterine contractions resulting in delayed or extended labour.
Consequently, aceclofenac is contraindicated in the course of the third trimester of pregnancy (see phase four.Three).
Breast-feeding
There isn't any information at the secretion of aceclofenac to breast milk; there has been but no first-rate switch of radio-labelled (14C) aceclofenac to the milk of lactating rats.
The use of aceclofenac ought to consequently be prevented in lactation except the potential blessings to the mom outweigh the possible risks to the foetus.
Fertility
The use of aceclofenac can also impair female fertility and is not recommended in women attempting to conceive. In women who've problems conceiving or who're present process investigations for infertility, withdrawal of aceclofenac have to be taken into consideration.
4.7 Effects on potential to power and use machines
Patients tormented by dizziness, drowsiness, vertigo, fatigue, visible disturbances or other important nervous system problems at the same time as taking NSAIDs need to refrain from driving or coping with dangerous equipment.
4.Eight Undesirable consequences
Gastrointestinal: The maximum generally discovered destructive occasions are gastrointestinal in nature. Peptic ulcers, perforation or GI bleeding, every now and then fatal, in particular inside the aged, may additionally occur (see segment 4.Four). Nausea, vomiting, diarrhoea, flatulence, constipation, dyspepsia, belly pain, melaena, haematemesis, ulcerative stomatitis, exacerbation of colitis and Crohn's disease (see phase four.Four) have been said following management. Less regularly, gastritis has been determined.
Pancreatitis has been suggested very not often.
Hypersensitivity: Hypersensitivity reactions were suggested following treatment with NSAIDs. These may consist of (a) non-unique allergic reactions and anaphylaxis (b) respiratory tract reactivity comprising bronchial asthma, aggravated bronchial asthma, bronchospasm or dyspnoea, or (c) assorted skin disorders, including rashes of numerous types, pruritus, urticaria, purpura, angiodema and, more rarely exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme).
Cardiovascular and cerebrovascular: Oedema, hypertension and cardiac failure had been suggested in association with NSAID remedy.
Exceptionally, occurrence of significant cutaneous and gentle tissues infections headaches throughout varicella has been reported in association with NSAID treatment.
Aceclofenac is both structurally associated and metabolised to diclofenac for which a more amount of clinical and epidemiological information always factor closer to an accelerated hazard of standard arterial thrombotic activities (myocardial infarction or stroke, specifically at high doses and in long remedy). Epidemiological information has additionally found an elevated danger of acute coronary syndrome and myocardial infarction associated with the usage of aceclofenac, (see sections four.3 and four.4).
Other detrimental reactions stated less typically consist of:
Renal: Interstitial nephritis
Neurological and special senses: Optic neuritis, reports of aseptic meningitis (in particular in patients with present automobile immune issues, which include systemic lupus erythematosus, combined connective tissue ailment), with signs and symptoms together with stiff neck, headache, nausea, vomiting, fever or disorientation (see section four.Four), confusion, hallucinations, malaise and drowsiness.
Haematological: Agranulocytosis, aplastic anaemia
Dermatological: Bullous reactions including Stevens-Johnson syndrome and poisonous epidermal necrolysis (very uncommon), erythema multiforme, exfoliative dermatitis, photosensitivity
If critical negative reactions arise, aceclofenac ought to be withdrawn.
The following is a table of unfavourable reactions said from clinical trials and publish- authorisation use of aceclofenac, grouped via System-Organ Class and envisioned frequencies. Very common (≥1/10); common (≥1/a hundred to <1/10); unusual (≥1/1,000 to <1/one hundred), uncommon (≥1/10,000 to <1/1,000), very rare (<1/10,000).
MedDRA system organ class
Common
≥1/100 to <1/10
Uncommon
≥1/1,000 to <1/a hundred
Rare
≥1/10,000 to <1/1,000
Very uncommon
<1/10,000
Blood and lymphatic system disorders
Anaemia
Bone marrow depression
Granulocytopenia
Thrombocytopenia
Neutropenia
Haemolytic anaemia
Immune system disorders
Anaphylactic reaction (including shock)
Hypersensitivity
Metabolism and nutrition disorders
Hyperkalaemia
Psychiatric disorders
Depression
Abnormal dreams
Insomnia
Nervous system disorders
Dizziness
Paraesthesia
Tremor
Somnolence
Headache
Dysgeusia (abnormal taste)
Eye disorders
Visual disturbance
Ear and labyrinth disorders
Vertigo
Tinnitus
Cardiac disorders
Cardiac failure
Palpitations
Vascular disorders
Hypertension
Flushing
Hot flush
Vasculitis
Respiratory, thoracic and mediastinal disorders
Dyspnoea
Bronchospasm
Stridor
Gastrointestinal disorders
Dyspepsia
Abdominal pain
Nausea
Diarrhoea
Flatulence
Gastritis
Constipation
Vomiting
Mouth ulceration
Melaena
Gastrointestinal haemorrhage
Gastrointestinal ulceration
Stomatitis
Haematemesis
Intestinal perforation
Exacerbation of Crohn's disease and Colitis Ulcerative
Pancreatitis
Hepatobiliary disorders
Hepatic injury (including hepatitis) Jaundice
Skin and subcutaneous tissue disorders
Pruritus
Rash
Dermatitis
Urticaria
Angioedema
Purpura
Dermatitis bullous
Severe mucocutaneous skin reaction (including Stevens Johnson Syndrome and Toxic Epidermal Necrolysis)
Renal and urinary disorders
Renal failure
Nephrotic syndrome
General disorders and administration site conditions
Oedema
Fatigue
Cramps in legs
Investigations
Hepatic enzyme increased
Blood urea increased
Blood creatinine increased
Weight increase
Blood alkaline phosphatase increased
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
Symptoms
Symptoms include headache, nausea, vomiting, epigastric pain, gastrointestinal irritation, gastrointestinal bleeding, rarely diarrhoea, disorientation, excitation, coma, drowsiness, dizziness, tinnitus, hypotension, respiratory depression, fainting, occasionally convulsions. In cases of significant poisoning acute renal failure and liver damage are possible.
Management
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.
Specific therapies such as dialysis or haemoperfusion are probable of no help in eliminating NSAIDs due to their high rate of protein binding and extensive metabolism.
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.
In case of frequent or prolonged convulsions, patients should be treated with intravenous diazepam.
Other measures may be indicated by the patient's clinical condition.
Management of acute poisoning with oral aceclofenac essentially consists of supportive and symptomatic measures for complications such as hypotension, renal failure, convulsions, gastrointestinal irritation, and respiratory depression.
5. Pharmacological properties
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Anti-inflammatory and antirheumatic products, non steroids, acetic acid derivatives and related substances, ATC code: M01AB16
Aceclofenac is a non-steroidal agent with marked anti-inflammatory and analgesic properties.
The mode of action of aceclofenac is largely based on the inhibition to prostaglandin synthesis. Aceclofenac is a potent inhibitor of the enzyme cyclo-oxygenase, which is involved in the production of prostaglandins.
5.2 Pharmacokinetic properties
Absorption
After oral administration, aceclofenac is rapidly and completely absorbed as unchanged drug. Peak plasma concentrations are reached approximately 1.25 to 3.00 hours following ingestion.
Distribution
Aceclofenac penetrates into the synovial fluid, where the concentrations reach approximately 57% of those in plasma. The volume of distribution is approximately 25 L. The mean plasma elimination half-life is around 4 hours. Aceclofenac is highly protein-bound (> ninety nine%).
Biotransformation and removal
Aceclofenac circulates mainly as unchanged drug. 4'-Hydroxyaceclofenac is the main metabolite detected in plasma. Approximately -thirds of the administered dose is excreted through the urine, mainly as hydroxymetabolites.
Elderly
No modifications inside the pharmacokinetics of aceclofenac have been detected inside the elderly.
Five.Three Preclinical protection records
The effects from preclinical research carried out with aceclofenac are steady with those anticipated for NSAIDs. The principal goal organ was the gastro-intestinal tract. No sudden findings had been recorded.
Aceclofenac became now not taken into consideration to have any mutagenic pastime in three in vitro research and an in vivo study in the mouse.
Aceclofenac become no longer observed to be carcinogenic in both the mouse or rat.
Animal research suggest that there was no evidence of teratogenesis in rats even though the systemic exposure was low and in rabbits, treatment with aceclofenac (10 mg/kg/day) led to a sequence of morphological adjustments in some foetuses.
6. Pharmaceutical particulars
6.1 List of excipients
Tablet center:
Cellulose, microcrystalline
Povidone Stearic acid
Croscarmellose sodium
Magnesium stearate
Tablet coating:
Titanium dioxide
Hypromellose three cp
Hypromellose five cp
Macrogol 400
Polysorbate eighty (E433)
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