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 a variety of 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 Voltaren

1. Osteoarthritis: Voltaren is effective in reducing pain and inflammation associated with osteoarthritis, helping to improve joint mobility.
2. Rheumatoid Arthritis: This medication helps reduce inflammation, pain and morning stiffness associated with rheumatoid arthritis.
3. Ankylosing spondylitis (Bechterew's disease): Diclofenac sodium is used to relieve pain and inflammation in this condition, which affects 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 to reduce back pain caused by various reasons, including intervertebral hernias.
6. Pain syndrome in injuries: For example, in cases of sprains, bruises or postoperative pain. Voltaren is effective in reducing pain and swelling.
7. Other painful and inflammatory conditions: Including algomenorrhea (painful menstruation), toothache and pain after surgery.

Release form

1. Tablets: This is the oral form. 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 make 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 results in 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 reduction in inflammation and pain.
3. Anti-inflammatory action: 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 by acting on the central regulators of thermoregulation in the hypothalamus.
6. Long-term use: In the long term, diclofenac may also have effects on inflammatory mediators and the immune response, which may help reduce chronic inflammation.
7. Selectivity of action: 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 generally well absorbed from the gastrointestinal tract after oral administration. The rate and extent of absorption depend on the form of the drug (e.g. tablets, capsules, suppositories) and the presence of food in the stomach.
2. Distribution: It is widely distributed in the body and penetrates into many tissues and organs, including joints, where it exerts its analgesic and anti-inflammatory effects.
3. Metabolism: Diclofenac is metabolized in the liver, mainly to 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 via the kidneys. Some is also excreted via bile into the intestine.
5. Half-life: The half-life of diclofenac is about 1-2 hours, and for its major metabolite it is about 4 hours.
6. Effect on the gastrointestinal tract: Diclofenac sodium may cause irritation of the gastric mucosa and an increased risk of ulcers and bleeding from the gastrointestinal tract.
7. Cumulative effect: With regular use of diclofenac, the drug may accumulate in the body, which may increase the risk of side effects, especially those associated with its effect on the gastrointestinal tract and kidneys.

Dosing and administration

Dosage for adults:

1. Oral use (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 (prolonged action), 100 mg is usually taken once a day.

2. External use (gel):

   • Apply a thin layer of gel to the affected area 3-4 times a day, rubbing gently 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 syndrome, 75 mg is administered deep intramuscularly. The administration can be repeated 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 the shortest possible time.
• While taking Voltaren, you should take food, milk or antacids to protect your stomach.
• Patients with heart, kidney, liver disease, as well as elderly patients require special caution and medical supervision.

Use Voltaren during pregnancy

1. FDA Classification:

   • Diclofenac is in the FDA's category C classification for use in the first and second trimesters of pregnancy, meaning that animal studies have shown harmful effects on the fetus, but controlled studies in pregnant women have not been conducted. It moves to category D in the third trimester because of potential risks to the fetus, including the risk of premature closure of the ductus arteriosus in the fetus and possible decreased 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 cardiac problems and other complications, including delayed labor and an increased risk of maternal and fetal bleeding 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 benefit to the mother outweighs the risks to the fetus. All decisions about use should be made in consultation with the 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 medicines, 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 using it.
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: Diclofenac may increase the risk of developing peptic ulcer disease and bleeding from the stomach and intestines, so the drug is contraindicated in patients with these conditions.
4. Severe heart and vascular disease: Using diclofenac may increase the risk of cardiovascular complications such as myocardial infarction or stroke, especially in patients with severe heart or vascular disease.
5. After coronary artery bypass grafting: Diclofenac is contraindicated in the period following coronary artery bypass grafting due to an increased risk of thrombosis, myocardial infarction and mortality.
6. Severe kidney and liver disease: The use of 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 the risk to the fetus or child.
8. Paediatric population: 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 Voltaren

1. Gastrointestinal damage: Includes dyspeptic symptoms such as nausea, vomiting, diarrhea, heartburn, and abdominal discomfort. Ulcers of the stomach or intestines, bleeding, and perforation may also develop.
2. Kidney damage: Use of Voltaren may result in impairment of kidney function, especially in people with a predisposition or risk factors.
3. Increased blood pressure: In some patients, Voltaren may cause increased blood pressure.
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: Headaches, dizziness and drowsiness may occur.
7. Blood damage: Voltaren may cause bleeding disorders, anemia and other blood function disorders.
8. Cardiovascular damage: 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. Ulcers and bleeding: Diclofenac sodium may cause ulcers in the stomach and intestines, which may lead to bleeding and perforation.
2. Renal injury: Overdose of diclofenac may cause acute kidney injury 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: Development of convulsive syndrome is possible.

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 ulcerative lesions and gastrointestinal bleeding.
2. Anticoagulants (eg, warfarin): Diclofenac may enhance the effect of anticoagulants such as warfarin, which may lead to an increased risk of bleeding.
3. Drugs affecting kidney function: Diclofenac may worsen kidney function and increase the risk of kidney failure when used concomitantly with diuretics, angiotensin-converting enzyme inhibitors (ACE inhibitors) and other drugs affecting kidney function.
4. Methotrexate: The 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 that affect the gastrointestinal tract: Using diclofenac with glucocorticosteroids, alcohol, or serotonin receptor agonists may also increase the risk of developing peptic ulcers and bleeding.
7. Antihypertensive agents: Diclofenac may reduce the effect of antihypertensive agents such as ACE inhibitors and beta blockers.