Dicloratio

Leaflet attached to the packaging: information for the user

Dicloratio, (75 mg + 20 mg)/2 ml solution for injection

Diclofenac sodium + Lidocaine hydrochloride

Read the leaflet carefully before using the medicine, as it contains important information for the patient.

• Keep this leaflet, so you can read it again if you need to.
• In case of any doubts, consult a doctor or pharmacist.
• This medicine has been prescribed specifically for you. Do not pass it on to others. The medicine may harm another person, even if their symptoms are the same as yours.
• If the patient experiences any side effects, including any side effects not listed in this leaflet, they should tell their doctor or pharmacist. See section 4.

Table of contents of the leaflet:

• 1. What is Dicloratio and what is it used for
• 2. Important information before using Dicloratio
• 3. How to use Dicloratio
• 4. Possible side effects
• 5. How to store Dicloratio
• 6. Contents of the packaging and other information

1. WHAT IS DICLORATIO AND WHAT IS IT USED FOR

Dicloratio contains diclofenac, which is a derivative of aminophenylacetic acid. It belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). It also has analgesic properties. Due to the presence of lidocaine hydrochloride, Dicloratio has a local anesthetic effect, which reduces the pain of injection.

Dicloratio is used to treat:

• inflammatory or degenerative forms of rheumatic disease:
• rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, extra-articular rheumatism (muscle, tendon, fascia, bursa, and tendon sheath inflammation)
• acute gout attacks
• pains caused by post-traumatic and post-operative inflammatory and edematous conditions.

2. IMPORTANT INFORMATION BEFORE USING DICLORATIO

When not to use Dicloratio

• if the patient is hypersensitive to diclofenac, lidocaine hydrochloride, or any of the other ingredients of this medicine (listed in section 6).
• if the patient has been diagnosed with hypersensitivity to other non-steroidal anti-inflammatory drugs
• if the patient has been diagnosed with hypersensitivity to acetylsalicylic acid, manifested by bronchospasm, asthma attacks, chest pain, skin reactions, or allergic rhinitis
• if the patient has blood disorders and coagulation disorders of unknown etiology
• if the patient has active or recurrent peptic ulcer disease of the stomach and/or duodenum
• if the patient is in the third trimester of pregnancy
• if the patient has severe liver, kidney, or heart failure
• if the patient has a history of bleeding or perforation of stomach and/or duodenal ulcers after using NSAIDs
• if the patient has been diagnosed with heart disease and/or cerebrovascular disease, such as myocardial infarction, stroke, transient cerebral ischemia, or vascular surgery
• if the patient has circulatory disorders (peripheral vascular disease)
• if the patient has active cerebral or other bleeding

Due to the presence of lidocaine, Dicloratio is contraindicated if:

• the patient has severe conduction disorders of the heart
• the patient has been diagnosed with cardiogenic or hypovolemic shock
• the patient has severe congestive heart failure
• the patient has first- or second-degree atrioventricular block
• the patient has bradycardia (bradycardia)
• the patient is hypersensitive to lidocaine or local anesthetics of the amide type.

Do not use in patients under 18 years of age.

Warnings and precautions

Before starting Dicloratio, discuss it with your doctor or pharmacist:

• if the patient is in the first or second trimester of pregnancy
• if the patient is breastfeeding
• if the patient has been diagnosed with porphyria
• if the patient has been diagnosed with systemic lupus erythematosus (SLE) or mixed connective tissue disease (collagenosis)
• if the patient has a history of gastrointestinal diseases, ulcers, or inflammation of the intestines (ulcerative colitis, Crohn's disease)
• if the patient has hypertension and/or heart disease
• if the patient has kidney function disorders
• if the patient has liver function disorders
• if the patient has recently undergone major surgery
• if the patient has hay fever, nasal polyps, or chronic obstructive pulmonary disease, which are a group at increased risk of allergic reactions. They may manifest as asthma attacks, angioedema, or urticaria
• if the patient is hypersensitive to other substances. In such patients, the use of the medicine is associated with an increased risk of allergic reactions
• if the patient is elderly.

Before taking the medicine, inform your doctor

• if the patient smokes
• if the patient has diabetes
• if the patient has angina pectoris, thrombosis, hypertension, elevated cholesterol levels, or elevated triglyceride levels.

Before using Dicloratio, tell your doctor if the patient has recently undergone or is scheduled to undergo stomach or gastrointestinal surgery, as Dicloratio may sometimes cause impaired wound healing in the intestines after surgery.

Taking the medicine may rarely (especially at the beginning of treatment) cause life-threatening skin reactions, such as exfoliative dermatitis, Stevens-Johnson syndrome with widespread rash, high fever, and joint pain, as well as toxic epidermal necrolysis with skin and mucous membrane changes, high fever, and severe general condition.

When the first signs of rash, mucous membrane changes, or other symptoms of an allergic reaction appear, the medicine should be discontinued and a doctor consulted.

The medicine may mask infection symptoms (e.g., headache, increased body temperature) and make it difficult to diagnose. During medical examinations, the doctor should be informed about the use of the medicine.

Avoid concomitant use of Dicloratio with systemic NSAIDs, including selective cyclooxygenase-2 inhibitors, due to the lack of evidence of benefits from concomitant use and potential increased risk of adverse reactions.

Dicloratio should be used with caution in elderly patients. In the case of elderly patients and those with low body weight, the use of the smallest effective dose is recommended.

Patient with asthma

In patients with asthma, seasonal allergic rhinitis, nasal polyps, chronic obstructive pulmonary disease, or chronic respiratory infections (especially if they have symptoms similar to those of allergic rhinitis), exacerbations of asthma are more common after using NSAIDs (intolerance to painkillers), angioedema, or urticaria.

Particular caution is recommended for patients with allergies to other substances, such as skin reactions, itching, or urticaria, as well as for patients with asthma, due to the possibility of worsening disease symptoms.

Effect on hematological parameters

Diclofenac may transiently inhibit platelet aggregation. Therefore, in patients with coagulation disorders, the doctor will recommend monitoring coagulation parameters.

If the medicine is used for a long time, regular checks of liver and kidney function, as well as blood count, should be performed.

Taking the medicine in the smallest effective dose for the shortest necessary period to alleviate symptoms reduces the risk of adverse reactions.

Effect on the gastrointestinal tract

Taking the medicine may cause gastrointestinal bleeding, ulceration, or perforation (with possible fatal outcome). This effect may be particularly dangerous in the case of high doses of the medicine and in elderly patients or those with a history of gastrointestinal ulcers.

If any unusual symptoms in the abdominal cavity (especially gastrointestinal bleeding) occur during Dicloratio use, the medicine should be discontinued immediately and a doctor consulted.

Patient with ulcerative colitis or Crohn's disease should be under close medical supervision due to the possibility of worsening their condition.

Effect on liver function

In patients with liver function disorders, the medicine may worsen the course of the disease.

It is necessary to strictly follow the doctor's recommendations for performing liver function tests.

In patients with porphyria, the medicine may cause a porphyria attack.

Effect on kidney function

Due to the treatment with NSAIDs, cases of fluid retention and edema have been reported, so particular caution is recommended in patients with impaired heart or kidney function, with a history of hypertension, in elderly patients, in patients taking diuretics or drugs that significantly affect kidney function, and in patients with excessive fluid loss of various etiologies, e.g., in the postoperative period after major surgery.

In such cases, as a precautionary measure, monitoring of kidney function is recommended during Dicloratio use.

Discontinuation of Dicloratio treatment usually leads to a return to the pre-treatment state.

During intramuscular injections of lidocaine-containing drugs, care should be taken to avoid injecting the medicine into blood vessels during injection.

Effect on the cardiovascular system and cerebral vessels

Taking such medicines as Dicloratio may be associated with an increased risk of heart attack (myocardial infarction) or stroke.

This risk increases with long-term use of high doses of the medicine.

Do not use higher doses or longer treatment than recommended.

In case of heart problems, a history of stroke, or suspected risk of these disorders (e.g., increased blood pressure, diabetes, elevated cholesterol levels, smoking), the treatment method should be discussed with a doctor or pharmacist.

Due to the presence of lidocaine, caution is recommended in cases of:

• increased risk of seizures
• conduction disorders and first-degree atrioventricular block
• myasthenia (rapid fatigue and muscle weakness)
• injection into an inflamed area (infection)

The occurrence of adverse reactions can be limited by using the medicine in the smallest effective dose and for no longer than necessary.

Dicloratio and other medicines

Tell your doctor or pharmacist about all medicines you are currently taking or have recently taken, as well as any medicines you plan to take.

Lithium, digoxin, phenytoin

Concomitant use of diclofenac and medicines containing digoxin, phenytoin, or lithium may increase the levels of these substances in the blood.

Diuretics, ACE inhibitors, and angiotensin II antagonists

Diclofenac may reduce the effect of diuretics and antihypertensive drugs.

Concomitant use of diclofenac and potassium-sparing diuretics may lead to hyperkalemia.

Therefore, potassium levels in the blood should be monitored during diclofenac treatment.

Due to the increased risk of nephrotoxicity, patients should be properly hydrated, and kidney function should be monitored periodically after starting and during concomitant treatment, especially when using diuretics and ACE inhibitors.

ACE inhibitors

Concomitant use of diclofenac and ACE inhibitors may reduce their effect and increase the risk of kidney function disorders.

Antihypertensive drugs

Diclofenac may exhibit antagonistic effects against antihypertensive drugs.

Non-steroidal anti-inflammatory drugs (NSAIDs), including COX-2 inhibitors, salicylates, and corticosteroids

Concomitant use of diclofenac and other NSAIDs or analgesic and anti-inflammatory corticosteroids increases the risk of adverse reactions related to the gastrointestinal tract.

Concomitant administration of acetylsalicylic acid reduces the level of diclofenac in the blood and reduces its effect.

Methotrexate

Caution is recommended when using NSAIDs during the period less than 24 hours before or after methotrexate treatment, as increased methotrexate levels in the blood and increased toxicity may occur.

Probenecid, sulfinpyrazone

Use of medicines containing probenecid or sulfinpyrazone may cause delayed excretion of diclofenac.

Anticoagulant and antiplatelet drugs

Clinical studies have not shown interactions between diclofenac and anticoagulant drugs; however, concomitant use of diclofenac and anticoagulant drugs increases the risk of bleeding.

Therefore, to ensure safety, coagulation parameters should be monitored during concomitant therapy.

Selective serotonin reuptake inhibitors

Concomitant use of NSAIDs and selective serotonin reuptake inhibitors may increase the risk of gastrointestinal bleeding.

Cyclosporine and tacrolimus

Diclofenac may enhance the nephrotoxic effect of cyclosporine and tacrolimus.

Sulfonylurea derivatives

Some reports indicate that diclofenac administration may affect blood glucose levels, requiring modification of the antidiabetic drug dose.

Blood glucose levels should be monitored.

Quinolone antibacterial drugs

Concomitant administration of diclofenac and quinolone antibiotics may sometimes enhance the adverse reactions of quinolone antibiotics (seizures).

Cholestyramine and colestipol

These medicines induce prolonged or reduced absorption of diclofenac.

Therefore, it is recommended to take diclofenac at least 1 hour before or 4-6 hours after taking cholestyramine or colestipol.

Strong CYP2C9 inhibitors

Caution is recommended when prescribing diclofenac with strong CYP2C9 inhibitors (such as sulfinpyrazone and voriconazole), due to the possible significant increase in diclofenac levels and exposure resulting from the inhibition of diclofenac metabolism.

Mifepristone

NSAIDs should not be administered for 8 to 12 days after mifepristone treatment, as they may reduce the effect of mifepristone.

Phenytoin

During concomitant use of phenytoin and diclofenac, monitoring of phenytoin levels in the blood is recommended, due to the possible increased exposure to phenytoin.

Alcohol

In the case of concomitant use of NSAIDs and alcohol, adverse reactions related to the administration of the medicine (especially those related to the gastrointestinal tract or central nervous system) may be enhanced.

Additional notes related to the presence of lidocaine

Lidocaine, in combination with antiarrhythmic drugs, beta-blockers, or calcium antagonists, may exhibit additional inhibitory effects on atrioventricular conduction, conduction of the cardiac impulse, and contractile force.

Pregnancy, breastfeeding, and fertility

If the patient is pregnant or breastfeeding, suspects that they may be pregnant, or plans to have a child, they should consult a doctor or pharmacist before using this medicine.

Pregnancy

The use of diclofenac in pregnant women has not been studied.

Therefore, Dicloratio should not be used during the first 6 months of pregnancy unless the benefit to the mother outweighs the risk to the fetus.

In the case of diclofenac use in women planning to become pregnant or in the first and second trimesters of pregnancy, the smallest possible dose and the shortest treatment period should be used.

In the third trimester of pregnancy, the use of Dicloratio is contraindicated due to the likelihood of inhibiting uterine contractions and/or premature closure of the ductus arteriosus in the fetus (Botall's duct).

Diclofenac may cause difficulties in becoming pregnant.

A doctor should be consulted in case of planned pregnancy, becoming pregnant, or problems with becoming pregnant while using the medicine.

Lidocaine may be administered to pregnant women only in cases of absolute necessity.

No controlled studies have been conducted in pregnant women.

Data from a limited number of cases of exposure of pregnant women do not indicate that lidocaine causes congenital malformations.

Animal studies have shown toxic effects on fertility.

Lidocaine quickly crosses the placenta.

Breastfeeding

Diclofenac passes into breast milk in small amounts.

Therefore, diclofenac should not be used during breastfeeding to avoid adverse reactions in the child.

Lidocaine is excreted in small amounts into breast milk.

It is unlikely to pose a risk to the infant when used in therapeutic doses.

However, since adverse reactions in infants are unknown, short-term use of diclofenac with lidocaine usually does not require discontinuation of breastfeeding.

In the case of long-term use of high doses of the medicine for the treatment of rheumatic diseases, discontinuation of breastfeeding should be considered.

Fertility

Dicloratio may cause difficulties in becoming pregnant.

A doctor should be informed if the patient plans to become pregnant or is having problems becoming pregnant.

Driving and using machines

Patient using Dicloratio, who experience vision disturbances, drowsiness, dizziness, fatigue, or other central nervous system disorders, should stop driving vehicles or operating machinery and inform their doctor or pharmacist.

Taking Dicloratio may cause side effects such as fatigue and dizziness.

In individual cases, the ability to drive vehicles or operate machinery may be impaired.

Important information about some ingredients of the medicine

The medicine contains 480 mg of propylene glycol in each 2 ml solution for injection.

• Pregnant or breastfeeding women should not take this medicine without a doctor's recommendation.
• Patient with liver or kidney function disorders should not take this medicine without a doctor's recommendation.
• Propylene glycol in this medicine may cause symptoms similar to those after alcohol consumption and increase the likelihood of adverse reactions.
• The medicine should only be used on a doctor's prescription.

The medicine contains sodium

The medicine contains less than 1 mmol (23 mg) of sodium per 2 ml, which means the medicine is considered "sodium-free".

3. HOW TO USE DICLORATIO

Dicloratio should always be used as directed by a doctor.

In case of doubts, consult a doctor or pharmacist again.

The doctor will recommend using the medicine in the smallest effective dose for the shortest period necessary to alleviate symptoms.

Adults

Dicloratio is usually administered in a dose of 75 mg (single injection) per day.

In severe cases, the dose can be increased to 150 mg per day (2 injections), with a few hours' interval between injections and a change in the injection site.

The use of diclofenac in solution for injection is indicated only when rapid analgesic effect is necessary or when oral or rectal administration is not possible.

The use of the medicine should be limited to a single injection.

After the acute pain has subsided, treatment should be continued with other forms of diclofenac, such as enteric-coated tablets, capsules, or suppositories.

In the case of injections and other forms of the medicine, the daily dose of diclofenac should not exceed 150 mg.

Lidocaine hydrochloride

Lidocaine hydrochloride, a component of the medicine, is used as a local anesthetic.

In local anesthesia, the dose depends on the area to be anesthetized, tissue perfusion, the number of neuronal segments to be blocked, individual tolerance to the medicine, and the anesthesia technique used.

It is recommended to administer the smallest therapeutic anesthetic dose.

Method of administration

To avoid nerve damage or damage to other tissues at the injection site, the instructions for injection must be followed.

The solution should be injected deeply into the gluteus maximus muscle, in the upper outer quadrant.

Due to the possibility of anaphylactic reactions, including anaphylactic shock, properly functioning equipment necessary for emergency situations must be available.

The doctor will monitor the patient for at least 1 hour after injecting the medicine.

Use in children and adolescents

Dicloratio solution for injection is not recommended for use in children and adolescents under 18 years of age.

Overdose of Dicloratio

In case of accidental ingestion of a larger amount of medicine than prescribed, a doctor, pharmacist, or hospital emergency department should be consulted immediately.

Overdose may manifest as headache, dizziness, drowsiness, and loss of consciousness; in children, seizures may occur.

Additional symptoms may include gastrointestinal disorders (abdominal pain, nausea, and vomiting) and cardiac rhythm disorders, decreased blood pressure to the level observed in shock, bradycardia, gastrointestinal bleeding, and liver and kidney function disorders.

There is no specific antidote.

Treatment of acute poisoning with non-steroidal anti-inflammatory drugs (NSAIDs) is primarily aimed at maintaining the function of vital organs and symptomatic treatment.

The doctor will monitor vital functions; control and correct water and electrolyte balance.

Supportive and symptomatic treatment should be used in case of complications such as significant decrease in blood pressure, kidney failure, seizures, gastrointestinal disorders, and respiratory disorders.

Specific measures such as forced diuresis, dialysis, or blood transfusion are not helpful in accelerating the elimination of non-steroidal anti-inflammatory drugs (NSAIDs), due to their high protein binding and extensive metabolism.

Missed dose of Dicloratio

A double dose should not be used to make up for a missed dose.

Discontinuation of Dicloratio

In case of doubts about the use of the medicine, a doctor or pharmacist should be consulted.

4. POSSIBLE SIDE EFFECTS

Like all medicines, Dicloratio can cause side effects, although not everybody gets them.

If any of the side effects get serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

You should immediately inform your doctor if you experience any of the following symptoms:

• chest pain, which may be a symptom of a potentially serious allergic reaction called Kounis syndrome

The following side effects have occurred during Dicloratio use with the following frequency:

Very common: 1 in 10 patients; common: 1 in 100 patients; uncommon: 1 in 1000 patients; rare: 1 in 10,000 patients; very rare: less than 1 in 10,000 patients; frequency not known: frequency cannot be estimated from the available data.

Very common:

• nausea, vomiting, diarrhea, minor gastrointestinal bleeding, which can occasionally cause anemia

Common:

• hypersensitivity reactions, such as rash and itching
• headache, dizziness, drowsiness, excitement, irritability, or fatigue
• indigestion, bloating, abdominal cramps, abdominal pain, loss of appetite, and stomach ulcers (sometimes with bleeding and perforation)
• increased liver enzyme activity
• rash
• irritation, pain, induration at the injection site

Uncommon:

• urticaria
• gastritis, gastrointestinal bleeding, melena, or bloody diarrhea
• liver damage, especially with long-term treatment, acute hepatitis with or without jaundice.

Regular liver function tests should be performed.

• hair loss
• edema, especially in patients with hypertension or kidney failure

Rare:

• asthma, bronchospasm (dyspnea)
• hepatitis, liver function disorders

Very rare:

• abscesses at the injection site, symptoms of aseptic meningitis with neck stiffness, headache, nausea, vomiting, fever, and altered consciousness
• decreased platelet count (thrombocytopenia), decreased white blood cell count (leukopenia), anemia (including hemolytic anemia), decreased neutrophil count (agranulocytosis), pancytopenia, The first symptoms may include: fever, sore throat, superficial mouth ulcers, flu-like symptoms, severe fatigue, nosebleeds, and bruising
• depression, insomnia, nightmares, anxiety, psychotic disorders.
• angioedema (including facial, tongue, or laryngeal edema), Quincke's edema, anaphylactic shock, allergic vasculitis, and allergic pneumonia
• psychotic reactions, depression, anxiety, nightmares
• tremor, sensory disturbances, taste disturbances, memory disturbances, disorientation, seizures
• vision disturbances, blurred vision, double vision
• tinnitus, temporary hearing loss
• palpitations, chest pain, heart failure, hypertension
• pneumonitis
• colitis (including bloody colitis and exacerbation of ulcerative colitis or Crohn's disease), constipation, oral mucosal inflammation (including ulcerative stomatitis), glossitis, esophageal disorders, intestinal stricture, pancreatitis, lower abdominal discomfort
• fulminant hepatitis without preceding symptoms, liver necrosis, liver failure
• rash, blistering rash, urticaria, erythema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, photosensitivity reactions, purpura, Henoch-Schönlein purpura, pruritus.
• hematuria, proteinuria, nephrotic syndrome, kidney tissue damage (interstitial nephritis, renal papillary necrosis), which may be associated with acute kidney failure.

Decreased urine output and general malaise may be symptoms of kidney disease, including kidney failure.

If such symptoms occur or worsen, the medicine should be discontinued.

Frequency not known:

• ischemic colitis
• necrosis at the injection site

Intramuscular injection may often cause local adverse reactions at the injection site (burning sensation) or tissue damage, such as sterile abscess, fat necrosis, or skin necrosis (Nicolau's syndrome).

Additional effects of lidocaine:

Rarely, hypersensitivity reactions have been reported in the form of urticaria, angioedema, bronchospasm, or respiratory failure syndrome.

Due to the presence of lidocaine, rapid administration of the medicine (unintentional intravenous injection, injection into well-perfused tissue) or overdose may cause systemic reactions, such as dizziness, drowsiness, seizures, confusion, nausea, vomiting, bradycardia, arrhythmias, decreased blood pressure to the level observed in shock.

NSAID treatment has been associated with reports of edema, hypertension, and heart failure.

Clinical studies and epidemiological data suggest that diclofenac use, especially in high doses (150 mg per day) and for a long time, may be associated with a small increase in the risk of arterial thrombosis (e.g., myocardial infarction or stroke).

Reporting side effects

If you experience any side effects, including any side effects not listed in this leaflet, please tell your doctor or pharmacist.

Side effects can be reported directly to the Department of Drug Safety Monitoring of the Office for Registration of Medicinal Products, Medical Devices, and Biocidal Products

Al. Jerozolimskie 181C, 02-222 Warsaw

Tel.: +48 22 49 21 301

Fax: +48 22 49 21 309

Website: https://smz.ezdrowie.gov.pl

Side effects can also be reported to the marketing authorization holder.

By reporting side effects, you can help provide more information on the safety of this medicine.

5. HOW TO STORE DICLORATIO

Store in the original packaging to protect from light.

Store out of sight and reach of children.

Do not use this medicine after the expiry date stated on the packaging.

The expiry date refers to the last day of the month.

Medicines should not be disposed of via wastewater or household waste.

Ask your pharmacist how to dispose of medicines that are no longer needed.

This will help protect the environment.

6. CONTENTS OF THE PACKAGING AND OTHER INFORMATION

What Dicloratio contains

• The active substances of the medicine are diclofenac sodium and lidocaine hydrochloride.
• The other ingredients are disodium edetate, N-acetylcysteine, sodium hydroxide, Macrogol 400, propylene glycol, water for injections.

What Dicloratio looks like and contents of the pack

Ampoules with a capacity of 2 ml, made of brown glass of hydrolytic class I, with a white point, containing a clear, colorless to pale yellow solution for injection, free from visible impurities.

Packaging

3 or 30 ampoules in a cardboard box.

Marketing authorization holder and manufacturer

Marketing authorization holder:

ratiopharm GmbH, Graf-Arco-Strasse 3, 89079 Ulm, Germany

Manufacturer:

Merckle GmbH, Ludwig-Merckle-Strasse 3, 89143 Blaubeuren, Germany

In order to obtain more detailed information about the medicine, please contact the local representative of the marketing authorization holder.

Teva Pharmaceuticals Polska Sp. z o.o.,

ul. Emilii Plater 53,

00-113 Warsaw,

tel. +48 22 345 93 00

Date of last revision of the leaflet: