Voltaren

Voltaren is the trade name of a drug whose active ingredient is diclofenac. Diclofenac belongs to a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). It has anti-inflammatory, analgesic and antipyretic effects.

Voltaren is often used to relieve pain and inflammation in various conditions such as osteoarthritis, rheumatoid arthritis, gout, muscle pain, rheumatism and other conditions associated with inflammation and pain symptoms.

Voltaren is available in various forms: tablets, capsules, gel, cream, ointment and solution for intramuscular and intravenous administration. Depending on the form of release and the individual needs of the patient, it can be used for both local and systemic treatment.

Indications Voltarena

1. Osteoarthritis: Voltaren is effective in reducing pain and inflammation associated with osteoarthritis, helping to improve joint mobility.
2. Rheumatoid Arthritis: The drug helps reduce inflammation, pain and morning stiffness associated with rheumatoid arthritis.
3. Ankylosing spondylitis (ankylosing spondylitis): Diclofenac sodium is used to relieve pain and inflammation in this disease affecting the spine.
4. Acute gouty arthritis: The drug may be prescribed to reduce inflammation and pain during gout attacks.
5. Spinal pain syndromes: Voltaren helps reduce back pain caused by various causes, including herniated discs.
6. Pain syndrome due to injuries: For example, in cases of sprains, bruises or post-operative pain. Voltaren is effective in reducing pain and swelling.
7. Other pain and inflammatory conditions: Including dysmenorrhea (painful menstruation), toothache and pain after surgery.

Release form

1. Tablets: This is an oral form. The tablets are usually taken whole with water, usually with or after meals.
2. Capsules: Similar to tablets, capsules contain diclofenac for oral use and are taken whole with water.
3. Gels: Voltaren gels are intended for external use. They are applied to the skin at the site of pain and rubbed in with gentle massage movements.
4. Ointments: Ointments are also intended for external use and are used to relieve pain and inflammation.
5. Patches: Some manufacturers may produce patches containing diclofenac for topical application to the skin.

Pharmacodynamics

1. Cyclooxygenase (COX) inhibition: The main mechanism of action of diclofenac is the inhibition of the enzyme cyclooxygenase (COX), which is involved in the formation of prostaglandins from arachidonic acid. This leads to a decrease in the formation of prostaglandins, which in turn reduces inflammation, pain and fever.
2. Suppression of prostaglandin production: Diclofenac suppresses the production of inflammatory prostaglandins (especially PGE2), which leads to a decrease in inflammation and pain.
3. Anti-inflammatory effect: Diclofenac reduces the intensity of inflammatory reactions, including capillary permeability, migration of leukocytes to the site of inflammation and phagocytosis.
4. Analgesic effect: The drug reduces pain sensitivity by suppressing the formation of prostaglandins at the site of inflammation and reducing irritation of peripheral nerve endings.
5. Antipyretic effect: Diclofenac is able to reduce body temperature during fever due to its effect on the central thermoregulation regulators in the hypothalamus.
6. Long-term use: In the long term, diclofenac may also have an effect on inflammatory mediators and the immune response, which helps reduce chronic inflammation.
7. Selectivity of exposure: Diclofenac has a stronger effect on COX-2 than on COX-1, which is considered more favorable in terms of minimizing side effects on the gastrointestinal tract.

Pharmacokinetics

1. Absorption: Diclofenac sodium is usually well absorbed from the gastrointestinal tract after oral administration. The speed and completeness of its absorption depend on the form of the drug (for example, tablets, capsules, suppositories) and the presence of food in the stomach.
2. Distribution: It is widely distributed in the body and penetrates many tissues and organs, including joints, where it exerts its analgesic and anti-inflammatory effects.
3. Metabolism: Diclofenac is metabolized in the liver, mainly with the formation of hydroxyl metabolites. One of the main metabolites, 4'-hydroxydiclofenac, also has pharmacological activity.
4. Excretion: Most metabolites and a small amount of unchanged diclofenac are excreted from the body through the kidneys. Some is also excreted through bile into the intestines.
5. Half-life: The half-life of diclofenac is about 1-2 hours, and for its main metabolite - about 4 hours.
6. Effect on the intestinal tract: Diclofenac sodium may cause irritation of the gastric mucosa and increase the risk of developing ulcers and bleeding from the gastrointestinal tract.
7. Cumulative effect: With regular use of diclofenac, accumulation of the drug in the body may occur, which may increase the risk of side effects, especially those related to its effect on the gastrointestinal tract and kidneys.

Dosing and administration

Dosage for adults:

1. Oral administration (tablets and capsules):

   • The usual starting dose is 100-150 mg per day, divided into 2-3 doses. For less severe conditions or long-term treatment, the maintenance dose may be reduced to 75-100 mg per day.
   • In the case of retard forms (long-acting), usually take 100 mg once a day.

2. External use (gel):

   • Apply a thin layer of gel to the affected area 3-4 times a day, lightly rubbing into the skin.

3. Suppositories:

   • The usual dose is 50-100 mg per day, administered rectally, divided into 1-2 doses.

4. Injections:

   • Used for short-term treatment of acute pain, 75 mg is administered deeply intramuscularly. You can repeat the administration after a few hours, but no more than two injections in one day.

Special instructions:

• Concomitant use with other NSAIDs should be avoided to minimize the risk of gastrointestinal side effects.
• To minimize the risk of side effects, it is recommended to use the minimum effective dose for a short period of time.
• While taking Voltaren, you should take food, milk or antacids to protect your stomach.
• Patients with heart disease, kidney disease, liver disease, as well as elderly patients require special care and medical supervision.

Use Voltarena during pregnancy

1. FDA classification:

   • Diclofenac is FDA Category C for use in the first and second trimesters of pregnancy, which means animal studies have shown adverse effects on the fetus, but no controlled studies have been conducted in pregnant women. It becomes category D in the third trimester due to potential risks to the fetus, including the risk of premature closure of the ductus arteriosus in the fetus and possible reduction in amniotic fluid volume.

2. Third trimester:

   • Use of diclofenac and other NSAIDs during the third trimester of pregnancy is associated with an increased risk of fetal heart problems and other complications, including delayed labor and an increased risk of bleeding in the mother and baby during labor. Use during this period is contraindicated.

3. First two trimesters:

   • Although the use of Voltaren in the first two trimesters is also considered risky, in some cases the doctor may consider it acceptable if the potential benefits to the mother outweigh the risks to the fetus. All decisions about use should be made together with your doctor.

Alternatives and precautions:

• To manage pain symptoms during pregnancy, your doctor may recommend other, safer alternatives, such as paracetamol (acetaminophen), which is considered safer during pregnancy, especially in the second trimester.
• Always consult your doctor before starting or continuing to use any medications, including Voltaren, during pregnancy.

Contraindications

1. Individual intolerance: People with known individual intolerance to diclofenac sodium or any other component of the drug should avoid its use.
2. Allergic reactions: In patients with a history of allergic reactions to diclofenac or other NSAIDs, such as aspirin or ibuprofen, the use of diclofenac may be contraindicated due to the possible risk of developing allergic reactions.
3. Peptic ulcer disease: The use of diclofenac can increase the risk of developing gastric ulcer and intestinal bleeding, so the drug is contraindicated in patients with these conditions.
4. Severe heart and vascular disease: The use of diclofenac can increase the risk of cardiovascular complications, such as heart attack myocardial infarction or stroke, especially in patients with serious heart or vascular disease.
5. After coronary artery bypass grafting: Diclofenac is contraindicated in the period after coronary artery bypass grafting due to an increased risk of thrombosis, myocardial infarction and mortality.
6. Severe kidney and liver disease: Diclofenac may be contraindicated in patients with severe kidney or liver disease due to the risk of toxic damage to these organs.
7. Pregnancy and breastfeeding: Diclofenac is contraindicated during pregnancy, especially in the third trimester, and breastfeeding due to risk to the fetus or child.
8. Children: The use of diclofenac in children and adolescents may be limited due to limited data on efficacy and safety in this age group.

Side effects Voltarena

1. Gastrointestinal Damage: Includes dyspeptic symptoms such as nausea, vomiting, diarrhea, heartburn and abdominal discomfort. It is also possible to develop stomach or intestinal ulcers, bleeding and perforations.
2. Kidney Damage: Use of Voltaren may cause impairment of kidney function, especially in people with predisposition or risk factors.
3. Increased blood pressure: Voltaren may cause increased blood pressure in some patients.
4. Allergic reactions: May include skin rash, itching, angioedema, or allergic dermatitis.
5. Liver Damage: Some patients may experience changes in liver function, including increased liver enzymes.
6. Headaches and dizziness: Headache, dizziness and drowsiness may occur.
7. Blood damage: Voltaren may cause bleeding disorders, anemia, and other blood problems.
8. Damage to the cardiovascular system: There may be an increased risk of heart attack or stroke.
9. Skin side effects: Include redness, itching, rash and other skin reactions.

Overdose

1. Peptic ulcer and bleeding: Diclofenac sodium can cause ulcerative lesions of the stomach and intestines, which can lead to bleeding and perforation.
2. Kidney Damage: Overdose of diclofenac may cause acute kidney damage due to hypotension and hypovolemia associated with bleeding and dehydration.
3. Cardiac complications: Cardiac arrhythmias and heart failure may occur due to effects on the cardiovascular system.
4. Neurological symptoms: May include headache, dizziness, drowsiness, visual disturbances and other neurological symptoms.
5. Respiratory failure: In rare cases, respiratory failure may occur due to paralysis of the respiratory muscles.
6. Metabolic disturbances: May include electrolyte imbalance and metabolic acidosis.
7. Convulsive syndrome: Convulsive syndrome may develop.

Interactions with other drugs

1. Acetylsalicylic acid (aspirin) and other NSAIDs: Concomitant use of diclofenac with other nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of developing ulcers and gastrointestinal bleeding.
2. Anticoagulants (eg, warfarin): Diclofenac may increase the effect of anticoagulants such as warfarin, which may lead to an increased risk of bleeding.
3. Drugs affecting renal function: Diclofenac may worsen renal function and increase the risk of renal failure when used concomitantly with diuretics, angiotensin-converting enzyme inhibitors (ACEIs) and other drugs that affect renal function.
4. Methotrexate: Use of diclofenac together with methotrexate may increase the toxicity of the latter, especially at the renal level.
5. Cyclosporine and lithium: Diclofenac may increase the concentration of cyclosporine and lithium in the blood, which may lead to increased toxicity.
6. Other drugs affecting the gastrointestinal tract: Use of diclofenac with glucocorticosteroids, alcohol or serotonin receptor agonists may also increase the risk of developing peptic ulcers and bleeding.
7. Antihypertensive drugs: Diclofenac may reduce the effect of antihypertensive drugs such as ACE inhibitors and beta blockers.