Amtolmetin Guacil

Usage

Amtolmetin Guacil is primarily prescribed for the symptomatic relief of pain and inflammation associated with osteoarthritis and rheumatoid arthritis. It is also indicated for juvenile rheumatoid arthritis in children aged two years and older.

• Pharmacological Classification: Non-Steroidal Anti-Inflammatory Drug (NSAID)

• Mechanism of Action: Amtolmetin Guacil is a prodrug of tolmetin. It inhibits prostaglandin synthesis by blocking cyclooxygenase (COX-1 and COX-2) enzymes. This action reduces inflammation and pain. Additionally, it stimulates capsaicin receptors in the gastrointestinal tract and releases nitric oxide, which has gastroprotective effects.

Alternate Names

• International/Regional Variations: Tolecitin, Artromed, Juvisync, Niselat

How It Works

• Pharmacodynamics: Amtolmetin Guacil, after being metabolized to tolmetin, exerts its anti-inflammatory and analgesic effects by inhibiting COX-1 and COX-2 enzymes, leading to a decrease in prostaglandin synthesis.

• Pharmacokinetics: Amtolmetin Guacil is administered orally. It is absorbed in the gastrointestinal tract and metabolized into tolmetin, its active form. Elimination is primarily through renal excretion.

• Mode of Action: Inhibition of COX-1 and COX-2 enzymes.

• Receptor binding, enzyme inhibition, or neurotransmitter modulation: Primarily COX-1 and COX-2 enzyme inhibition. It also stimulates capsaicin receptors in the gastrointestinal tract.

• Elimination pathways: Primarily renal excretion.

Dosage

Standard Dosage

Adults:

• Osteoarthritis and Rheumatoid Arthritis: Initial dose: 400 mg three times a day (1200 mg daily), ideally including a dose upon waking and at bedtime.
• The dosage may be increased up to a maximum of 1800 mg/day, divided into three doses, based on patient response after one to two weeks.

Children:

• Juvenile Rheumatoid Arthritis (age 2 and above): Initial dose: 20 mg/kg/day, divided into three or four smaller doses. Maximum: 30 mg/kg/day.
• Children younger than 2 years: Use and dose must be determined by a physician.

Special Cases:

• Elderly Patients: Initiate therapy at the lowest effective dose (600 mg/day). Closely monitor renal function.
• Patients with Renal Impairment: Dose reduction may be necessary. Close monitoring is required.
• Patients with Hepatic Dysfunction: Dose reduction may be necessary. Close monitoring is required.
• Patients with Comorbid Conditions (e.g., diabetes, cardiovascular disease): Exercise caution and monitor for potential drug interactions and exacerbations of comorbid conditions.

Clinical Use Cases

Information on dosage recommendations for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations was not found in the provided sources.

Side Effects

Common Side Effects

• Dizziness
• Headache
• Nausea and vomiting
• Stomach pain
• Diarrhea
• Ringing in the ears

Rare but Serious Side Effects

• Gastrointestinal bleeding (black or tarry stools)
• Difficulty breathing
• Allergic reactions (rashes, hives)

Long-Term Effects

• Increased risk of cardiovascular events (heart attack, stroke) with prolonged use, especially in patients with pre-existing heart disease.
• Potential for renal impairment with long-term use.

Contraindications

• Known hypersensitivity to amtolmetin guacil or tolmetin.
• History of asthma or allergic-type reactions following aspirin or other NSAID intake.
• Active gastrointestinal bleeding or ulceration.
• Severe heart, liver, or kidney impairment.
• Should be avoided in patients with asthma caused by aspirin or other NSAIDS.

Drug Interactions

• Anticoagulants and Antiplatelet Drugs: Increased risk of bleeding.
• Other NSAIDs and Corticosteroids: Increased risk of gastrointestinal ulceration and bleeding.
• Antihypertensive Medications: Reduced effectiveness of antihypertensive drugs.
• SSRIs and SNRIs: Increased risk of gastrointestinal bleeding.
• Alcohol should be avoided due to increased risk of gastrointestinal bleeding.

Pregnancy and Breastfeeding

• Pregnancy: Not recommended unless absolutely necessary. Potential risk to the fetus.
• Breastfeeding: Not recommended unless absolutely necessary. Minimal amounts may be excreted in breast milk.

Drug Profile Summary

• Mechanism of Action: COX-1 and COX-2 inhibitor, reducing prostaglandin synthesis.
• Side Effects: Dizziness, headache, nausea, vomiting, stomach pain, diarrhea, GI bleeding, allergic reactions.
• Contraindications: Hypersensitivity, asthma/allergy after aspirin/NSAID use, GI bleeding/ulceration, severe heart/liver/kidney impairment.
• Drug Interactions: Anticoagulants, antiplatelets, other NSAIDs, corticosteroids, antihypertensives, SSRIs, SNRIs.
• Pregnancy & Breastfeeding: Not recommended unless absolutely necessary.
• Dosage: Adults: Up to 1800 mg/day. Children (2+): 20-30 mg/kg/day.
• Monitoring Parameters: Renal and liver function, blood pressure, signs of GI bleeding.

Popular Combinations

This information was not found in the provided sources.

Precautions

• Pre-screening for allergies, cardiovascular disease, renal/hepatic impairment, and gastrointestinal disorders is crucial.
• Use the lowest effective dose, especially in elderly patients.
• Monitor for cardiovascular events, GI bleeding, and renal function.
• Avoid alcohol.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Amtolmetin Guacil?

A: Adults: Initial dose is 400 mg three times daily, up to a maximum of 1800 mg/day. Children (2 years and older): 20-30 mg/kg/day, divided into doses. Elderly patients should start with a lower dose.

Q2: What are the common side effects?

A: Common side effects include dizziness, headache, nausea, vomiting, stomach pain, and diarrhea.

Q3: What are the serious side effects?

A: Serious side effects include gastrointestinal bleeding, difficulty breathing, and allergic reactions.

Q4: Is Amtolmetin Guacil safe during pregnancy and breastfeeding?

A: It’s generally not recommended during pregnancy and breastfeeding unless absolutely necessary due to potential risks. Discuss with your physician.

Q5: What are the contraindications for Amtolmetin Guacil?

A: Contraindications include hypersensitivity, asthma/allergy after aspirin/NSAID use, active GI bleeding/ulcers, and severe heart, liver, or kidney problems.

Q6: What drugs interact with Amtolmetin Guacil?

A: It interacts with anticoagulants, other NSAIDs, corticosteroids, antihypertensives, and SSRIs/SNRIs.

Q7: How long does it take for Amtolmetin Guacil to work?

A: The onset of action is typically within 1-2 hours, with effects lasting for an average of 12 hours.

Q8: Can patients with renal or hepatic impairment take Amtolmetin Guacil?

A: Dose adjustments and close monitoring are necessary for patients with renal or hepatic impairment.

Q9: Can I take Amtolmetin Guacil with alcohol?

A: Alcohol should be avoided as it can increase the risk of gastrointestinal bleeding.

Q10: What should I do if I miss a dose?

A: Take the missed dose as soon as you remember, unless it’s almost time for your next dose. Do not double the dose.