Indometacin - Comprehensive Usage Guide: instructions, indications, composition, side effects
Composition
- Active Ingredient: Indometacin (Indomethacin)
- Excipients: May include lactose monohydrate, povidone, magnesium stearate, colloidal silicon dioxide, maize starch, and other inactive ingredients depending on the formulation.
Official Forms
- Indometacin is available in various formulations, including:
- Capsules: Available in strengths such as 25 mg and 50 mg.
- Suppositories: Available in strengths such as 50 mg and 100 mg.
- Injection: Available in vials containing sterile indometacin solution for intramuscular or intravenous administration.
- Ointment/Gel: Available for topical application containing indometacin as the active ingredient.
Pharmacological Group
- Indometacin belongs to the pharmacological group of nonsteroidal anti-inflammatory drugs (NSAIDs), specifically indoleacetic acid derivatives (ATC code: M01AB01).
Pharmacological Properties
- Pharmacodynamics: Indometacin exerts its therapeutic effects by inhibiting the synthesis of prostaglandins, thereby exerting anti-inflammatory, analgesic, and antipyretic actions. It inhibits both the cyclooxygenase (COX) enzyme isoforms, COX-1 and COX-2, leading to decreased prostaglandin production.
- Pharmacokinetics: Following oral administration, indometacin is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations reached within 2 hours. It undergoes extensive metabolism in the liver to inactive metabolites and is primarily excreted in the urine.
Indications
- Indometacin is indicated for the treatment of various inflammatory and painful conditions, including:
- Rheumatoid arthritis
- Osteoarthritis
- Ankylosing spondylitis
- Acute gouty arthritis
- Acute musculoskeletal disorders
- Postoperative pain and inflammation
- Patent ductus arteriosus in premature infants (off-label use)
Contraindications
- Indometacin is contraindicated in individuals with:
- Hypersensitivity to indometacin or any component of the formulation
- Active peptic ulcer disease or gastrointestinal bleeding
- History of gastrointestinal perforation or ulceration
- Severe heart failure
- Severe renal impairment
- Severe hepatic impairment
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
- Third trimester of pregnancy (due to the risk of premature closure of the ductus arteriosus)
- Active bleeding disorders or recent history of bleeding
Interactions
- Indometacin may interact with various medications, including anticoagulants, antiplatelet agents, selective serotonin reuptake inhibitors (SSRIs), corticosteroids, and other NSAIDs, potentially increasing the risk of bleeding or gastrointestinal adverse effects. Caution is advised when co-administering indometacin with these agents.
Specifics of Use
- Indometacin capsules should be taken orally with food or milk to minimize gastrointestinal irritation. The dosage and duration of treatment depend on the condition being treated and the response to therapy. Suppositories should be inserted rectally as directed, and the injection should be administered by a healthcare professional.
Pregnancy and Breastfeeding
- Indometacin is contraindicated in the third trimester of pregnancy due to the potential risk of premature closure of the ductus arteriosus in the fetus. It should be used with caution during the first and second trimesters and avoided during breastfeeding, as it may be excreted in breast milk.
Impact on Motor Functions
- Indometacin may cause dizziness, drowsiness, or visual disturbances in some patients. Patients should exercise caution when driving or operating machinery, especially during the initial stages of treatment.
Dosage and Administration
- The recommended dosage of indometacin varies depending on the indication, formulation, and patient characteristics. For oral capsules, the usual starting dose is 25 mg two or three times daily, with the option to increase the dose based on clinical response. Suppositories are available in strengths such as 50 mg and 100 mg, with dosing based on the severity of the condition. The injection is typically administered by a healthcare professional in a clinical setting.
Overdose
- In case of overdose, supportive measures should be initiated as needed. Symptoms of overdose may include nausea, vomiting, gastrointestinal bleeding, renal impairment, and central nervous system effects. Patients should seek medical attention if overdose is suspected.
Side Effects
- Common side effects of indometacin may include:
- Gastrointestinal disturbances (e.g., dyspepsia, nausea, abdominal pain)
- Headache
- Dizziness
- Rash or itching
- Fluid retention
- Elevated blood pressure
- Serious adverse effects such as gastrointestinal ulceration, bleeding, myocardial infarction, stroke, and renal impairment may occur, particularly with long-term use or at high doses.
Storage and Shelf Life
- Indometacin should be stored at room temperature (15-30°C) in a dry place, protected from light and moisture. Check the expiration date on the packaging and discard any expired or unused medication.
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