Alental^® (Tablets, Cream, Powder) Instructions for Use

ATC Code

M01AB16 (Aceclofenac)

Active Substance

Aceclofenac (Rec.INN registered by WHO)

Clinical-Pharmacological Group

NSAID

Pharmacotherapeutic Group

Anti-inflammatory and antirheumatic agents; non-steroidal anti-inflammatory and antirheumatic agents; acetic acid derivatives and related substances

Pharmacological Action

NSAID, a derivative of phenylacetic acid. It has anti-inflammatory, analgesic, and antipyretic effects, which are due to the inhibition of COX-1 and COX-2 and the suppression of prostaglandin synthesis.

In rheumatic diseases, the anti-inflammatory and analgesic effect of aceclofenac contributes to a significant reduction in the severity of pain, morning stiffness, and joint swelling, which improves the patient’s mobility.

Pharmacokinetics

After oral administration, the absorption of Aceclofenac is high. C_max is reached within 1.25-3 hours. It penetrates into the synovial fluid, where its concentration reaches 57% of the plasma concentration level, and the time to reach C_max is 2-4 hours later than in plasma. V_d is 25 L. Plasma protein binding (albumin) is 99%. Aceclofenac circulates mainly unchanged; its main metabolite is 4′-hydroxyaceclofenac. T_1/2 is 4 hours. It is excreted by the kidneys, mainly in the form of hydroxy derivatives (about 2/3 of the administered dose).

Indications

Symptomatic treatment of musculoskeletal disorders, including: rheumatoid arthritis; osteoarthritis; ankylosing spondylitis.

For the relief of inflammation and pain: lumbago; scapulohumeral periarthritis; rheumatic soft tissue lesions; toothache.

ICD codes

Dosage Regimen

Cream

Aceclofenac in the form of a cream is intended for external use only. The cream should not be applied under occlusive dressings.

The cream should be applied with light massaging movements to the affected area 3 times/day. The applied dose depends on the size of the affected area and is 1.5-2 g of cream.

Tablets, Powder

Aceclofenac is intended for symptomatic therapy, to reduce pain and inflammation at the time of use; it does not affect the progression of the disease.

To reduce the risk of adverse events, Aceclofenac should be used at the lowest effective dose for the shortest possible duration.

For oral administration – 100 mg 2 times/day, morning and evening.

The duration of therapy without a doctor’s prescription is no more than 7 days.

In patients with hepatic insufficiency, the initial dose of aceclofenac is 100 mg/day.

Adverse Reactions

Definition of frequency of adverse reactions: very common (≥ 1/10); common (from ≥ 1/100 to < 1/10); uncommon (from ≥ 1/1000 to < 1/100), rare (from ≥ 1/10,000 to < 1/1000), very rare (< 1/10,000).

Blood and lymphatic system disorders: rare – anemia; very rare – bone marrow function depression, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia.

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

Metabolism and nutrition disorders: very rare – hyperkalemia.

Psychiatric disorders: very rare – depression, abnormal dreams, insomnia.

Nervous system disorders: common – dizziness; very rare – paresthesia, tremor, somnolence, headache, dysgeusia (taste disturbance).

Eye disorders: rare – visual disturbance.

Ear and labyrinth disorders: very rare – vertigo, tinnitus.

Cardiac disorders: rare – increased blood pressure, worsening of arterial hypertension, heart failure; very rare – hyperemia, “flushing”, vasculitis, palpitations.

Respiratory, thoracic and mediastinal disorders: rare – dyspnea; very rare – bronchospasm.

Gastrointestinal disorders: common – dyspepsia, abdominal pain, nausea, diarrhea; uncommon – flatulence, gastritis, constipation, vomiting, ulcerative stomatitis; rare – melena, formation of gastric and intestinal ulcers, hemorrhagic diarrhea, gastrointestinal bleeding; very rare – stomatitis, hematemesis, intestinal perforation, exacerbation of Crohn’s disease and ulcerative colitis, pancreatitis.

Hepatobiliary disorders: common – increased liver enzyme activity; very rare – liver disease (including hepatitis), increased alkaline phosphatase activity.

Skin and subcutaneous tissue disorders: uncommon – pruritus, rash, dermatitis, urticaria; rare – angioedema; very rare – purpura, eczema, severe mucocutaneous reactions (including Stevens-Johnson syndrome and toxic epidermal necrolysis).

Renal and urinary disorders: uncommon – increased serum urea concentration, increased serum creatinine concentration; very rare – nephrotic syndrome, renal failure.

General disorders and administration site conditions: very rare – edema, asthenia, muscle spasms.

Other: very rare – increased body weight

Contraindications

Hypersensitivity to aceclofenac and other NSAIDs; “aspirin triad” (combination of bronchial asthma, recurrent nasal and sinus polyposis, and intolerance to acetylsalicylic acid and pyrazolone drugs); erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase); gastrointestinal bleeding or suspicion thereof; inflammatory bowel diseases; severe renal failure (creatinine clearance <30 ml/min); progressive kidney diseases; active liver disease; thyroid gland diseases; confirmed hyperkalemia; acute myocardial infarction; period after coronary artery bypass surgery; arterial hypotension; arterial hypertension; acute cerebrovascular accidents (ischemic, hemorrhagic stroke); hematopoiesis disorders and blood diseases (leukopenia, including history, thrombocytopenia, hemophilia); severe myopathy, severe myasthenia; pregnancy; lactation (breastfeeding); children and adolescents under 18 years of age.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

There are no clinical data on the use of aceclofenac during pregnancy. Regular use of NSAIDs in the third trimester of pregnancy may lead to a decrease in uterine tone and weaker contractions. The use of NSAIDs may lead to premature closure of the fetal ductus arteriosus and, possibly, to persistent pulmonary hypertension in the newborn, delayed onset of labor, and increased duration of labor.

Epidemiological studies in humans have not obtained data indicating embryotoxicity of NSAIDs. However, in experimental studies in rabbits administered aceclofenac (10 mg/kg/day), morphological changes in the fetus were observed in some cases. There are no data on the presence of a teratogenic effect in rats.

There are no data on the excretion of aceclofenac into human breast milk. In experimental studies with the administration of radioactive ¹⁴C-aceclofenac to lactating rats, no significant transfer of radioactivity into the milk was observed.

NSAIDs can affect fertility and are not recommended for use in women planning pregnancy.

Use in Hepatic Impairment

Contraindicated in active liver disease.

Use with caution in patients with a history of liver disease. There are no data on the need to change the daily dose of aceclofenac when used in patients with renal insufficiency. When prescribing aceclofenac to this category of patients, as with the use of other NSAIDs, caution is required.

Use in Renal Impairment

Contraindicated in severe renal failure, progressive kidney diseases.

Use with caution in patients with a history of kidney disease.

Due to the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing to patients with moderate renal insufficiency.

Pediatric Use

Contraindicated: children and adolescents under 18 years of age.

Geriatric Use

For elderly patients, no change in the daily dose of aceclofenac or the frequency of its use is required.

Special Precautions

Use with caution in patients with a history of liver, kidney, and gastrointestinal diseases, bronchial asthma, arterial hypertension, coronary artery disease, history of gastrointestinal ulceration, presence of Helicobacter pylori infection, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smokers, elderly patients, with long-term use of NSAIDs, with frequent alcohol consumption, with severe somatic diseases.

Prostaglandins play an important role in maintaining renal blood flow, therefore, special caution should be exercised when prescribing to patients with cardiac or renal failure, the elderly, those taking diuretics, and patients in whom there is a decrease in circulating blood volume for any reason (for example, after major surgery). If Aceclofenac is prescribed in such cases, it is recommended to monitor renal function as a precaution. In patients with hepatic insufficiency (chronic hepatitis, compensated liver cirrhosis), the kinetics and metabolism do not differ from those in patients with normal liver function. During long-term therapy, it is necessary to monitor liver function, peripheral blood picture, and stool test for occult blood.

Effect on ability to drive vehicles and operate machinery

During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Digoxin, phenytoin, lithium preparations – a possible increase in the plasma concentration of these drugs.

Diuretics, antihypertensive agents – a possible weakening of the effect of diuretics and antihypertensive agents.

Potassium-sparing diuretics – possible development of hyperkalemia. With this combination, control of plasma potassium levels is necessary.

Other NSAIDs, oral corticosteroids (prednisolone) – increased risk of gastrointestinal adverse events.

Selective serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline) – increased risk of gastrointestinal bleeding.

Cyclosporine, tacrolimus – a possible increase in the toxic effect of the drugs on the kidneys.

Hypoglycemic agents – both hypoglycemia and hyperglycemia are possible. With this combination, blood glucose monitoring is necessary.

Methotrexate – taking aceclofenac within 24 hours before or after taking methotrexate may lead to an increase in its plasma concentration and an increase in toxic effects.

Acetylsalicylic acid – decrease in the plasma concentration of aceclofenac.

Antiplatelet agents and anticoagulants (warfarin, clopidogrel) – increased risk of bleeding. With this combination, regular monitoring of blood coagulation is necessary.

Mifepristone – Aceclofenac, like other NSAIDs, should not be taken within 8-12 days after using mifepristone due to the risk of reducing its effect.

Antimicrobial agents of the fluoroquinolone group – increased risk of seizures.

Zidovudine – increased risk of bleeding, possible occurrence of hemarthrosis and hematomas.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.