Butadion

Butadione, also known by its international nonproprietary name phenylbutazone, is a nonsteroidal anti-inflammatory drug (NSAID) commonly used to treat pain and inflammation associated with rheumatic diseases such as rheumatoid arthritis and gout. Phenylbutazone acts by inhibiting cyclooxygenase enzymes (COX-1 and COX-2), which are involved in the synthesis of prostaglandins, important mediators of inflammation and pain.

Phenylbutazone was widely used in the mid-20th century to treat rheumatism and other inflammatory conditions, but its use has declined over time due to serious side effects and the emergence of safer alternatives.

Indications Butadiona

1. Rheumatoid arthritis: This is a chronic inflammatory disease that affects the joints and can cause pain, inflammation and joint deformity. Butadione may help reduce inflammation and pain symptoms in rheumatoid arthritis.
2. Osteoarthritis: This is a joint disease in which cartilage tissue breaks down, leading to pain, stiffness and poor joint mobility. Butadione may help reduce pain and inflammation in joints due to osteoarthritis.
3. Gout: This is a form of arthritis caused by a disorder in the body's uric acid metabolism, leading to the formation of uric acid crystals in the joints. Butadione can be used to relieve inflammation and pain due to gout.
4. Other inflammatory conditions: Butadione may also be used to treat other inflammatory conditions such as ankylosing spondylitis and vasculitis.

Release form

Phenylbutazone, commercially known as Butadione, is usually available in tablet form for oral administration. Phenylbutazone tablets can come in different strengths depending on the country and manufacturer, usually 100 mg or 200 mg.

Pharmacodynamics

1. Anti-inflammatory effect: Phenylbutazone has the ability to reduce inflammation by inhibiting the activity of cyclooxygenase (COX), an enzyme involved in the synthesis of prostaglandins from arachidonic acid. This leads to a decrease in the formation of prostaglandins, which play a key role in the mediation of inflammatory processes.
2. Anti-rheumatic effects: Phenylbutazone also has the ability to reduce pain and inflammation associated with rheumatic diseases such as rheumatoid arthritis and osteoarthritis. It may help reduce swelling and inflammation in the joints, leading to improved symptoms and functional status.
3. Anti-inflammatory effect in the bladder: Phenylbutazone can be used to treat urolithiasis and other inflammatory conditions of the bladder.
4. Analgesic effects: In addition to its anti-inflammatory effect, phenylbutazone may also have analgesic effects, reducing pain associated with inflammation and various rheumatic conditions.
5. Long-term effects: Unlike some other NSAIDs, the effects of phenylbutazone may persist for a long time after stopping its use.
6. Possible side effects: It is important to note that, like other NSAIDs, phenylbutazone may cause unwanted side effects, including dyspeptic disorders, stomach and intestinal ulcers, and an increased risk of cardiovascular complications and kidney damage.

Pharmacokinetics

1. Absorption: Phenylbutazone is usually rapidly and completely absorbed from the gastrointestinal tract after oral administration.
2. Distribution: It is well distributed throughout the tissues and organs of the body, including the joints, where it is based to exert its anti-inflammatory and analgesic effects.
3. Metabolism: Phenylbutazone is metabolized in the liver to form active metabolites. The main metabolic pathway is hydroxylation, which leads to the formation of 4-hydroxyphenylbutazone and 4-hydroxyethylbutazone.
4. Excretion: Phenylbutazone and its metabolites are excreted from the body primarily through the kidneys.
5. Half-life: The half-life of phenylbutazone is approximately 5-8 hours.

Dosing and administration

1. Oral administration (tablets):

   • Adults: The initial dose is usually 200-400 mg per day, divided into several doses (for example, 100 mg 2-4 times a day). The maintenance dose may be reduced to 100 mg per day depending on clinical response and patient tolerance.
   • Children: The use of phenylbutazone in children is not recommended due to the high risk of serious side effects.

2. Intravenous and intramuscular administration:

   • The injections are intended for short-term use in acute conditions and are usually performed in a hospital setting. The dosage and method of administration must be strictly controlled by medical personnel.

Use Butadiona during pregnancy

Risks of using phenylbutazone during pregnancy:

1. Effect on the fetus:

   • NSAIDs, including phenylbutazone, can cause cardiopulmonary complications in the fetus, including premature closure of the ductus arteriosus, which can cause serious cardiovascular problems in the fetus.
   • There is a risk of low amniotic fluid (oligohydramnios), which can affect the development of the lungs and other vital organs in the fetus.

2. Effect on pregnancy:

   • Phenylbutazone may increase the risk of bleeding during pregnancy and childbirth, which threatens the health of both mother and baby.
   • NSAIDs may delay labor or increase the risk of preeclampsia.

3. Recommendations:

   • The use of phenylbutazone during pregnancy, especially in the third trimester, is strictly contraindicated due to the high risks to the health of the mother and child.
   • If a woman taking phenylbutazone plans to become pregnant or finds out she is pregnant, she should consult her doctor immediately to discuss safe treatment alternatives and possible precautions.

Treatment alternatives:

It is important for women during pregnancy to consider other, safer alternatives to manage pain and inflammation. A healthcare professional can help you choose the right drug or treatment that will be safe during pregnancy.

Contraindications

1. Individual intolerance: People with known individual intolerance to phenylbutazone or any other component of the drug should avoid its use.
2. History of allergic reactions: In patients with a history of allergic reactions to phenylbutazone or other drugs, including aspirin or other NSAIDs (non-steroidal anti-inflammatory drugs), the use of phenylbutazone may be contraindicated.
3. Blood disorders: Phenylbutazone can cause agranulocytosis (a sharp decrease in the number of white blood cells) and other disorders of blood formation. Therefore, the drug is contraindicated in patients with hematopoiesis disorders, including agranulocytosis, leukopenia, and aplastic anemia.
4. Liver and kidney disease: The use of phenylbutazone may be contraindicated in patients with severe liver or kidney disease due to the risk of developing toxic damage to these organs.
5. Peptic ulcer disease: The use of phenylbutazone may increase the risk of developing gastric and intestinal ulcers and bleeding from them, so the drug is contraindicated in patients with these conditions.
6. Pregnancy and breastfeeding: Phenylbutazone is contraindicated during pregnancy and breastfeeding due to the risk to the fetus or child.
7. Children: The use of phenylbutazone in children and adolescents may be contraindicated due to the lack of data on efficacy and safety in this age group. Group.

Side effects Butadiona

1. Dyspeptic symptoms: Include nausea, vomiting, diarrhea, heartburn and stomach discomfort. Patients may also experience decreased appetite.
2. Peptic ulcer: Butadione may increase the risk of developing stomach and intestinal ulcers, especially in patients with a predisposition to this condition or when taking other NSAID drugs at the same time.
3. High blood pressure: Some patients may experience increased blood pressure when taking butadione.
4. Allergic reactions: May include skin rashes, itching, angioedema or allergic dermatitis.
5. Increased uric acid levels: In some patients, butadione may increase uric acid levels in the blood, which may be undesirable for gout.
6. Renal impairment: Impaired renal function may occur in some patients, especially with long-term use and high doses.
7. Bleeding: Butadione may increase the risk of gastrointestinal bleeding, especially in patients with arterial hypertension or a predisposition to bleeding.

Overdose

1. Peptic ulcers and bleeding: Phenylbutazone can cause ulcers of the stomach and intestines, which can lead to bleeding and perforation. Overdose may increase the risk of these complications.
2. Kidney damage and functional impairment: In case of phenylbutazone overdose, acute renal failure may occur due to hypotension and hypovolemia caused by bleeding and dehydration.
3. Cardiac complications: Overdose of phenylbutazone may cause cardiac arrhythmias and heart failure due to the drug's potential effects on the cardiovascular system.
4. Neurological symptoms: Headache, dizziness, drowsiness, visual disturbances and other neurological symptoms may occur.
5. Respiratory failure: Respiratory failure may develop due to paralysis of the respiratory muscles.
6. Metabolic disorders: Possible electrolyte imbalance, as well as metabolic acidosis.
7. Convulsions and convulsive syndrome: In rare cases, convulsive syndrome may occur.

Interactions with other drugs

1. Individual intolerance: People with a known individual intolerance to phenylbutazone or any other component of the drug should avoid its use.
2. History of allergic reactions: In patients with a history of allergic reactions to phenylbutazone or other drugs, including aspirin or other NSAIDs (nonsteroidal anti-inflammatory drugs), the use of phenylbutazone may be contraindicated.
3. Blood diseases: Phenylbutazone can cause agranulocytosis (a sharp decrease in the number of white blood cells) and other disorders of blood formation. Therefore, the drug is contraindicated in patients with hematopoietic disorders, including agranulocytosis, leukopenia and aplastic anemia.
4. Liver and kidney disease: The use of phenylbutazone may be contraindicated in patients with severe liver or kidney disease due to the risk of toxic damage to these organs.
5. Gastric and intestinal ulcers: The use of phenylbutazone may increase the risk of developing gastric and intestinal ulcers and bleeding, so the drug is contraindicated in patients with these conditions.
6. Pregnancy and breastfeeding: Phenylbutazone is contraindicated during pregnancy and breastfeeding due to risk to the fetus or child.
7. Children: The use of phenylbutazone in children and adolescents may be contraindicated due to the lack of data on efficacy and safety in this age group.