Aircec^® (Tablets) Instructions for Use

Marketing Authorization Holder

Diamed-Pharma, LLC (Russia)

Manufactured By

Pharmproekt, JSC (Russia)

ATC Code

M01AB16 (Aceclofenac)

Active Substance

Aceclofenac (Rec.INN registered by WHO)

Dosage Form

Aircec®

Film-coated tablets 100 mg: 10, 20, 30, 40, 60, 90, or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, round, biconvex; the core on the cross-section is white to almost white.

Excipients: microcrystalline cellulose (type 102), croscarmellose sodium, povidone K30, sodium stearyl fumarate.

Film coating composition Opadry II white (03A280002): hypromellose (hydroxypropyl methylcellulose), microcrystalline cellulose, titanium dioxide, macrogol (polyethylene glycol).

10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (4) – cardboard packs.
10 pcs. – blister packs (6) – cardboard packs.
10 pcs. – blister packs (9) – cardboard packs.
10 pcs. – blister packs (10) – cardboard packs.

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 is 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 – 25 L. Plasma protein binding (albumin) – 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 diseases, 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

Aceclofenac is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the regression of the disease.

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

For oral administration – 100 mg 2 times/day in the 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).

From the blood and lymphatic system: rare – anemia; very rare – bone marrow function depression, granulocytopenia, thrombocytopenia, neutropenia, hemolytic anemia.

From the immune system: rare – anaphylactic reactions (including shock), hypersensitivity.

From metabolism and nutrition: very rare – hyperkalemia.

From the psyche: very rare – depression, unusual dreams, insomnia.

From the nervous system: common – dizziness; very rare – paresthesia, tremor, drowsiness, headache, dysgeusia (taste perversion).

From the organ of vision: rare – visual disturbance.

From the hearing organ and labyrinthine disorders: very rare – dizziness, tinnitus.

From the cardiovascular system: rare – increased blood pressure, worsening of arterial hypertension, heart failure; very rare – hyperemia, “hot flashes”, vasculitis, palpitations.

From the respiratory system, thoracic and mediastinal organs: rare – dyspnea; very rare – bronchospasm.

From the digestive system: 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, vomiting blood, intestinal perforation, exacerbation of Crohn’s disease and ulcerative colitis, pancreatitis.

From the liver and biliary tract: common – increased activity of liver enzymes; very rare – liver disease (including hepatitis), increased ALP activity.

From the skin and subcutaneous tissues: uncommon – itching, rash, dermatitis, urticaria; rare – angioedema; very rare – purpura, eczema, severe mucocutaneous reactions (including Stevens-Johnson syndrome and toxic epidermal necrolysis).

From the urinary system: uncommon – increased serum urea concentration, increased serum creatinine concentration; very rare – nephrotic syndrome, renal failure.

General reactions: very rare – edema, weakness, muscle spasms.

Other: very rare – weight gain.

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 of it; inflammatory bowel diseases; severe renal failure (creatinine clearance <30 ml/min); progressive kidney diseases; active liver disease; thyroid 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 in history, thrombocytopenia, hemophilia); severe myopathy, severe myasthenia; pregnancy; lactation period (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 prolonged pulmonary hypertension in the newborn, delayed onset of labor and increased duration of labor.

In human epidemiological studies, no data were obtained indicating embryotoxicity of NSAIDs. However, in experimental studies on rabbits with the administration of 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 in human breast milk. In experimental studies with the administration of radioactive ¹⁴C-aceclofenac to lactating rats, no significant transfer of radioactivity into milk was observed.

NSAIDs can affect fertility and are not recommended for use by 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 ulcerative gastrointestinal lesions, in the presence of Helicobacter pylori infection, in cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral artery diseases, in smokers, in 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, so special caution should be exercised when prescribing to patients with cardiac or renal failure, the elderly, those taking diuretics, and patients who have a reduced 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 analysis for occult blood.

Effect on ability to drive vehicles and mechanisms

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 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 – a decrease in the plasma concentration of aceclofenac.

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