Aceclofenac Welfarm, 100 mg 20 pcs

Pharmacotherapeutic group: NSAIDs

ATC code: M01AB

Pharmacodynamics:

Aceclofenac is a derivative of phenylacetic acid inhibits cyclooxygenase types I and II.

It has anti-inflammatory analgesic and antipyretic effects.

It inhibits the synthesis of prostaglandins and thus influences the pathogenesis of inflammation, pain and fever. In rheumatic diseases the anti-inflammatory and analgesic activity of Aceclofenac promotes significant decrease of intensity of pain and swelling of joints which improves functional condition of the patient.

Pharmacokinetics:

Aceclofenac is quickly and completely absorbed after oral administration. The time of reaching maximum concentration is 125-3 h. It penetrates into synovial fluid where its concentration reaches 57% of the level of concentration in plasma and time of reaching maximum concentration 2-4 hours later than in plasma. The volume of distribution is 25 liters.

The binding to plasma proteins (albumin) is 99%. Aceclofenac circulates mainly unchanged its main metabolite is 4′-hydroxyacetylofenac.

Half-life period is 4 hours. It is excreted by the kidneys mainly as hydroxy derivatives (about 2/3 of the administered dose).

Indications

The drug is prescribed:

The use of Aceclofenac is not able to completely cure these diseases, but quickly reduces inflammation and pain.

Active ingredient

Composition

How to take, the dosage

The drug should be taken in the lowest effective dose for the shortest possible period of time.

Ingestion. The tablets should be swallowed whole with plenty of fluid.

The dose of the drug for all indications:

Adults are prescribed 100 mg twice daily 1 tablet in the morning and 1 in the evening.

The course of treatment is prescribed by the doctor individually.

Hepatic failure

Patients with moderate hepatic failure need to reduce the dose of aceclofenac. The recommended initial dose is 100 mg daily.

Renal failure

There is no evidence that the dose of acyclofenac should be reduced in patients with mild renal failure but it is recommended to use with caution.

Interaction

There have been no studies of drug interactions except for warfarin.

Aceclofenac is metabolized by cytochrome P450 system – CYP2C9 and the data indicate that aceclofenac may be an inhibitor of this enzyme. Therefore, there is a possible risk of pharmacokinetic interaction with phenytoin cimetidine tolbutamide phenylbutazone amiodarone miconazole and sulfaphenazole.

As with other NSAIDs, there is a risk of pharmacokinetic interactions with drugs that are metabolized in the liver, such as methotrexate and lithium preparations.

Aceclofenac binds almost completely to plasma proteins and therefore the possibility of substitution with other drugs that bind strongly to plasma proteins must be considered.

In the absence of pharmacokinetic interaction studies, the following information is based on the information from other NSAIDs:

The following combinations should be avoided

NSAIDs inhibit tubular secretion of methotrexate and in this case there may also be metabolic interaction resulting in decreased clearance of methotrexate. Therefore, administration of NSAIDs should always be avoided during treatment with high doses of methotrexate (more than 20 mg/week).

Some NSAIDs inhibit renal excretion of lithium, leading to elevated serum lithium concentrations. This combination should be avoided if serum lithium concentrations cannot be monitored frequently.

NSAIDs inhibit platelet aggregation and damage gastrointestinal mucosa, which may increase anticoagulant activity and increase the risk of gastrointestinal mucosal bleeding in patients taking anticoagulants.

The combination of acyclofenac with oral anticoagulants of the coumarin group ticlopidine thrombolytics and heparin in the absence of careful monitoring should be avoided.

The following combinations may require dose adjustments and precautions:

Possible interactions between NSAIDs and methotrexate should be considered, especially in patients with renal impairment. Renal function must be monitored when taking both drugs.

Precaution must be taken when taking NSAIDs and methotrexate concomitantly within 24 hours since methotrexate concentrations may increase leading to increased toxicity of methotrexate. It is assumed that taking NSAIDs together with cyclosporine or tacrolimus increases the risk of nephrotoxicity due to decreased synthesis of prostacyclin in the kidneys. Therefore, it is important to monitor renal function when taking these drugs concomitantly.

The concomitant use of acetylsalicylic acid and other NSAIDs may increase the rate of adverse reactions, and therefore caution is required when taking them together.

NSAIDs may decrease the diuretic effect of furosemide bumetanide and the hypotensive effect of thiazide diuretics. Concomitant treatment with potassium-saving diuretics may be associated with increased serum potassium concentrations; therefore, blood potassium levels should be monitored.

NSAIDs may also decrease the effect of some hypotensive drugs.

Angiotensin converting enzyme inhibitors or angiotensin II receptor antagonists in combination with NSAIDs may lead to renal failure. The risk of acute renal failure, which is usually reversible, may increase in some patients with impaired renal function such as elderly patients or patients with fluid deficiency. Therefore, the combination of these drugs with NSAIDs should be used with caution Patients should receive sufficient fluids with food and renal function should be monitored.

Aceclofenac has not been found to affect blood pressure when taken simultaneously with bendroflumethiazide although interactions with other hypotensive drugs such as beta-adrenoblockers cannot be excluded.

Other possible interactions

In isolated cases of hypoglycemia and hyperglycemia have been reported. Therefore, the dose of drugs causing hypoglycemia must be adjusted for aceclofenac.

In concomitant use with the drug Aceclofenac Wellfarm:

– digoxin phenytoin or lithium drugs – plasma concentrations of these drugs may be increased;

– diuretics and hypotensive drugs – the effects of these drugs may be impaired;

Special Instructions

The severity of adverse reactions can be corrected by reducing the effective single dose required for symptom control.

Patients with a history of arterial hypertension and/or chronic heart failure NYMA functional class I-II require proper monitoring and physician consultation as fluid retention and edema have been reported with NSAID treatment. Data from clinical and epidemiological studies suggest that the use of some NSAIDs (especially in high doses and long-term use) may increase the risk of arterial thrombosis (e.g., myocardial infarction or stroke). There is insufficient data to rule out this risk for aceclofenac.

Patients with uncontrolled arterial hypertension congestive heart failure coronary heart disease peripheral artery disease and/or cerebrovascular disease should take aceclofenac only after careful analysis of the clinical situation. The same caution should be exercised before starting long-term treatment in patients with cardiovascular risk (e.g., hypertension, hyperlipidemia, diabetes mellitus, and smokers).

Aceclofenac should be used with caution and under close medical supervision in patients with gastrointestinal disorders peptic ulcer history after acute stroke systemic lupus erythematosus porphyria hematopoietic disorders and clotting disorders.

Aceclofenac may cause reversible inhibition of platelet aggregation.

Patients with Crohn’s disease ulcerative colitis are not recommended to prescribe the drug. Caution should be exercised in patients with hepatic renal heart failure and in patients with other diseases predisposed to the development of edema. Administration of NSAIDs by this category of patients may lead to worsening of renal excretion and edema development.

Patients taking diuretics or those at increased risk of hypovolemia also require caution when taking Aceclofenac Wellfarm.

Elderly patients need to be cautious because they are more likely to have side effects. Gastrointestinal bleeding and/or perforation may occur during treatment especially if there is a history of gastrointestinal disease. In addition, elderly patients are more likely to have liver, kidney, and cardiovascular disorders.

All patients on long-term treatment with NSAIDs should be monitored to decrease the risk of adverse reactions (e.g., urinalysis and blood chemistry).

The concomitant use of Aceclofenac Welfarm with any cyclooxygenase/prostaglandin inhibitor medication may decrease fertility and is not recommended for women who are planning to become pregnant.

Women with a history of infertility should stop taking Aceclofenac Wellfarm.

When taking this medicine, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and quick psychomotor reactions.

Contraindications

– Gastrointestinal erosive-ulcerative lesions in the acute phase of gastrointestinal bleeding or suspected;

– Complete or incomplete combination of bronchial asthma recurrent polyposis of the nose and sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (includingч. history);

– hypersensitivity to acetylaclofenac or components of the drug;

– period after coronary artery bypass grafting;

– significant hepatic impairment or active liver disease;

– significant renal impairment (creatinine clearance less than 30 ml/.min) progressive renal disease hyperkalemia;

– inflammatory bowel disease (Crohn’s disease ulcerative colitis) in the acute phase;

– decompensated heart failure;

– hematopoiesis and coagulation disorders;

– pregnancy and breastfeeding period;

– lactose deficiency lactose intolerance glucose-galactose malabsorption;

– childhood under 18 years of age.

Hepatic renal and gastrointestinal diseases in the history of bronchial asthma arterial hypertension decreased circulating blood volume (including After operative interventions) ischemic heart disease chronic renal insufficiency of mild and moderate degree of severity (CK from 30 to 60 ml/min) hepatic insufficiency of mild and moderate degree of severity chronic heart insufficiency cerebrovascular diseases dislipidemia/hyperlipidemia diabetes mellitus peripheral arterial disease smoking elderly age long history of use of NSAIDs presence of Helicobacter pylori infection frequent use of alcohol concomitant therapy with the following drugs:

Side effects

The undesirable effects listed below are presented by system-organ classes according to MedDRA classification with the following frequency: often: ≥1/100 to < 1/10; infrequent: ≥1/1000 to < 1/100; rare: ≥1/10000 to < 1/1000; very rare: < 1/10000.

Allergic reactions: skin rash urticaria eczema erythroderma systemic anaphylactoid reactions bronchial asthma in some cases – vasculitis pneumonitis polymorphic exudative erythema (including Stevens-Johnson syndrome) toxic epidermal necrolysis (Lyell syndrome).

Immune system disorders: rare – anaphylactic reaction (including shock) hypersensitivity.

Gastrointestinal tract disorders: frequent – dyspepsia abdominal pain nausea diarrhea; infrequent – flatulence gastritis constipation vomiting oral mucosa ulceration; rare – melena gastrointestinal tract ulceration diarrhea with blood gastrointestinal bleeding; very rare – stomatitis vomiting blood stomach ulcer perforation small bowel worsening the course of Crohn’s disease and ulcerative colitis pancreatitis.

The cardiovascular system: rare – heart failure increased blood pressure; very rare – tachycardia “hot flashes” vasculitis.

Hepatic and biliary tract disorders: often – increased activity of “liver” enzymes; very rare – liver damage (including hepatitis) increased blood alkaline phosphatase activity.

Nervous system disorders: common – dizziness; very rare – paresthesias tremors somnolence headache increased fatigue dysgeusia.

Psychiatric disorders: very rare – depression atypical dreams insomnia.

Skin and subcutaneous tissue disorders: infrequent – itching rash dermatitis urticarial rash; rare – angioedema; very rare – purpura skin and mucous membrane reactions bullous skin reactions.

Hematopoietic organs: thrombocytopenia leukopenia agranulocytosis hemolytic anemia aplastic anemia.

As to the blood and lymphatic system: rare – anemia; very rare – bone marrow suppression granulocytopenia neutropenia hemolytic anemia.

Key kidneys and urinary tract: infrequent – increase of concentration of blood urea – increase of concentration of blood creatinine; very rare – interstitial nephritis nephrotic syndrome – renal failure.

Respiratory system of the chest and mediastinum: rarely – shortness of breath; very rarely – bronchospasm.

An organ of vision: rare – visual disturbances.

Hearing organ and labyrinth: very rare – vertigo tinnitus.

Metabolism and nutrition: very rare – hyperkalemia increase in body weight.

Systemic disorders: very rarely – spasms of the muscles of the lower extremities.

Overdose

Symptoms: dizziness headache hyperventilation of the lungs with increased seizure readiness nausea vomiting abdominal pain.

Treatment: gastric lavage administration of activated charcoal symptomatic therapy. There is no specific antidote. Forced diuresis hemodialysis blood transfusion is ineffective.

Similarities