Dolaren

Dolaren is a combination drug that contains two active ingredients: diclofenac sodium and paracetamol. These two substances act in synergy to provide analgesic, anti-inflammatory and antipyretic effects, making it an effective treatment for a variety of conditions associated with pain and inflammation.

Diclofenac sodium is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits the enzymes cyclooxygenase 1 and 2 (COX-1 and COX-2), which are involved in the synthesis of prostaglandins, substances that play a key role in the development of inflammation, pain and fever. For this reason, diclofenac is effective in treating symptoms such as back pain, osteoarthritis, rheumatoid arthritis and other musculoskeletal disorders.

Paracetamol (or acetaminophen) acts primarily in the central nervous system, increasing the pain threshold and having an antipyretic effect. It is added to many combination drugs to enhance the analgesic effect and for a broader spectrum of action against fever and inflammation.

Dolaren is often used to reduce pain and inflammation in arthritis, toothache, headache, menstrual pain and other conditions. It can also be used to temporarily reduce body temperature in fever.

Indications Dolarena

1. Osteoarthritis: Dolaren may be used to relieve pain and inflammation associated with osteoarthritis, a chronic joint disease.
2. Rheumatoid arthritis: This drug may help reduce inflammation and pain in rheumatoid arthritis, an inflammatory disease of the joints.
3. Muscle Pain: Dolaren is often used to relieve pain and inflammation from muscle strains, sprains, strains and other muscle injuries.
4. Post-surgical pain: After surgeries such as orthopedic surgery or dental procedures, using Dolaren may help reduce pain and inflammation.
5. Cold or flu-related pain: Paracetamol, one of the ingredients in Dolaren, can be used to reduce fever and relieve pain associated with headaches, muscle aches and other cold or flu symptoms.
6. Other conditions: Dolaren can also be used to treat other conditions involving pain and inflammation, such as ankylosing spondylitis, gout, etc.

Release form

1. Tablets: The most common form of medication, tablets are convenient for adults to take and are generally preferred for regular use. They may be coated to protect the stomach or dissolve.
2. Chewable tablets: This form may be more pleasant to take, especially for those who have difficulty swallowing regular tablets.
3. Soluble/effervescent tablets: These tablets dissolve in water to create a pleasant drink, making them easier to take and more acceptable to a wide range of patients, including those who suffer from dysphagia (difficulty swallowing).
4. Suspensions and Syrups: These forms are especially suitable for children and adults who have difficulty taking solid dosage forms. Syrups often have a pleasant taste, making the medication easier to take.
5. Gels or creams for external use: Although the main focus in this issue is on systemic forms of release, Dolaren may also contain diclofenac in the form of a gel or cream for local use for pain in joints, muscles or injuries.

Pharmacodynamics

1. Diclofenac sodium:

   • Mechanism of action: Diclofenac belongs to the class of anti-inflammatory, analgesic and antirheumatic drugs - NSAIDs (non-steroidal anti-inflammatory drugs). It acts by inhibiting the enzyme cyclooxygenase (COX), especially COX-1 and COX-2. These enzymes are involved in the process of converting arachidonic acid into prostaglandins, substances that play a key role in the inflammatory process. Inhibition of COX leads to a decrease in the synthesis of prostaglandins and, therefore, to a decrease in inflammation, pain and fever.
   • Pharmacological effects: Diclofenac has anti-inflammatory, analgesic and antipyretic effects. It can reduce inflammation, pain and fever.

2. Paracetamol:

   • Mechanism of action: The mechanism of action of paracetamol is not fully understood, but it is thought to bind to COX-3 in the central nervous system and block its activity. In addition, it is thought that paracetamol may modulate endogenous pain perception systems.
   • Pharmacological effects: Paracetamol has analgesic (pain-relieving) and antipyretic (antipyretic) effects. It reduces pain and fever, but unlike NSAIDs, it does not have an anti-inflammatory effect.

Pharmacokinetics

1. Diclofenac sodium:

   • Absorption: Diclofenac sodium is generally well absorbed from the gastrointestinal tract after oral administration. It can be absorbed from both the stomach and intestine.
   • Distribution: Diclofenac sodium has a high affinity for plasma proteins and is widely distributed in body tissues, including joints.
   • Metabolism: Diclofenac is metabolized in the liver, mainly via hydroxylation and conjugation with glucuronides.
   • Elimination: Diclofenac is primarily excreted via the kidneys as metabolites. Its elimination half-life is approximately 2 hours.

2. Paracetamol:

   • Absorption: Paracetamol is rapidly and completely absorbed from the gastrointestinal tract. Its absorption is not affected by food intake.
   • Distribution: Paracetamol is widely distributed in the body and crosses the placental barrier. It is also present in breast milk.
   • Metabolism: Paracetamol is metabolized in the liver. It undergoes mainly glucuronidation and sulfation.
   • Elimination: Paracetamol is primarily excreted via the kidneys as conjugated metabolites. Its half-life in the body is about 2-3 hours.

Dosing and administration

For adults:

• Tablets: The usual recommendation is to take 1 tablet (the content of diclofenac and paracetamol may vary, but is usually 50 mg diclofenac and 500 mg paracetamol) every 8 hours. The maximum dose of paracetamol of 3000 mg per day and diclofenac of 150 mg per day should not be exceeded.
• Suspension or syrup: The dosage is calculated individually based on the patient's weight and age.

For children:

• Suspension or syrup: The dosage should be strictly calculated by the doctor. Usually it is about 15 mg of diclofenac and 150-200 mg of paracetamol per kilogram of body weight per day, divided into several doses.

Special instructions:

• The drug should be taken during or after meals to minimize stomach irritation.
• It is important to drink plenty of water while taking the medication.
• With prolonged use, it is necessary to monitor liver and kidney function, as well as blood counts.

Use Dolarena during pregnancy

The use of the combination drug Dolaren, which contains diclofenac sodium and paracetamol, during pregnancy requires caution. Paracetamol is widely used during pregnancy as it is considered relatively safe for the treatment of pain and fever, but some studies have pointed to possible risks, such as an increased likelihood of hyperactivity and other behavioral problems in children if it is used long-term or in high doses (Liew et al., 2014).

With regard to diclofenac, its use may be associated with risks to the fetus, including possible effects on the baby's cardiovascular system, such as premature closure of the ductus arteriosus and pulmonary hypertension of the newborn. Diclofenac should be avoided in the third trimester of pregnancy and used with caution in the first two trimesters (Siu & Lee, 2004).

Before using Dolaren or any other medication during pregnancy, it is important to consult with your doctor to evaluate all potential risks and benefits.

Contraindications

1. Allergic reactions to diclofenac, paracetamol or any other component of the drug.
2. Severe liver dysfunction. Both diclofenac and paracetamol are metabolized in the liver, and their use may worsen existing liver disease or cause new liver disease.
3. Severe renal impairment. These substances are excreted through the kidneys, and their accumulation can be dangerous in renal impairment.
4. Peptic ulcer or active bleeding in the gastrointestinal tract. Diclofenac may worsen or cause these conditions.
5. Severe heart failure, hypertension, or other cardiovascular disease. NSAIDs may worsen these conditions.
6. Last trimester of pregnancy. Diclofenac may adversely affect the fetus and complicate the course of pregnancy and childbirth.
7. Breastfeeding period. Diclofenac and paracetamol can pass into breast milk and affect the baby.

Side effects Dolarena

1. Gastrointestinal disorders: The most common side effects include dyspepsia (indigestion), nausea, vomiting, diarrhea, stomach pain and dyspeptic symptoms.
2. Gastrointestinal ulcers and bleeding: Diclofenac, especially in high doses or with prolonged use, may increase the risk of developing stomach or intestinal ulcers and bleeding.
3. Increased blood pressure: In some patients, the use of diclofenac may lead to an increase in blood pressure.
4. Kidney damage: Long-term use of Dolaren may cause kidney damage, especially in people with a predisposition to kidney failure.
5. Liver damage: Dolaren may cause toxic liver damage, especially in patients with pre-existing liver disease or who consume alcohol.
6. Allergic reactions: May include skin rash, itching, redness of the skin, angioedema (swelling of the skin, mucous membranes, sometimes subcutaneous tissue) and anaphylactic shock (very rare).
7. Increased potassium levels in the blood: Diclofenac can cause an increase in potassium levels in the blood, which is especially dangerous in patients with heart or kidney disease.
8. Impaired function of the hematopoietic organs: Changes in the blood may be observed, such as anemia, leukopenia, thrombocytopenia.
9. Headaches and dizziness: These symptoms may also be a side effect of Dolaren.

Overdose

1. For diclofenac:

   • Gastrointestinal complications: stomach ulcers, gastrointestinal bleeding, perforation of the gastrointestinal tract.
   • Toxic liver damage: Liver damage can be severe and even fatal.
   • Kidney failure: People with pre-existing kidney disease are particularly vulnerable to overdose.
   • Neurological symptoms: headache, dizziness, convulsions, drowsiness and other symptoms.

2. For paracetamol:

   • Liver failure: Paracetamol in high doses can cause toxic liver damage, which can be fatal.
   • Analgesic non-rebound: Unlike other NSAIDs, paracetamol does not cause inflammation and is a poor pain reliever in overdose.
   • Methemoglobinemia: a rare but serious complication that can be caused by paracetamol in high doses.

Interactions with other drugs

1. Drugs affecting the gastrointestinal tract: NSAIDs, including diclofenac sodium, may increase the risk of developing gastric and intestinal ulcers. Taking Dolaren together with other NSAIDs or glucocorticosteroids, as well as with anticoagulants or antiplatelet agents, may increase the risk of gastrointestinal bleeding.
2. Drugs affecting renal function: Diclofenac sodium may worsen renal function or lead to acute renal failure, especially in patients predisposed to this condition. The combination of Dolaren with other drugs affecting renal function, such as angiotensin-converting enzyme (ACE) inhibitors or diuretics, may increase this risk.
3. Medicines that affect liver function: Paracetamol is metabolized in the liver, so taking Dolaren together with other drugs that can also have a hepatotoxic effect (eg alcohol or anti-tuberculosis drugs) may increase the risk of liver damage.
4. Medicines that affect the blood clotting system: Diclofenac sodium may enhance the effects of anticoagulants such as warfarin, which may lead to increased bleeding time and an increased risk of bleeding.
5. Drugs affecting the central nervous system: Combination of Dolaren with other drugs that can also have a sedative or stimulant effect on the central nervous system (eg, alcohol or hypnotics) may enhance these effects.
6. Drugs that affect intestinal microflora: Taking antibiotics that change intestinal microflora in combination with Dolaren may increase the risk of developing diarrhea or superinfection.