AGRYLIN 0.5MG/ 1MG CAPSULE (ANAGRELIDE)

Agrylin is used to treat a blood cell disorder called thrombocythemia (also called thrombocytosis), which occurs when your body produces too many platelet cells. Agrylin may also                     be used for purposes not listed in this medication guide.

📌 Brand & Composition

• Brand Name: Agrylin

• Generic Name (Salt): Anagrelide hydrochloride

• Chemical Formula: C₁₀H₇Cl₂N₃O · HCl · H₂O; MW ≈ 310.55

• Formulation: Oral 0.5 mg capsule (containing 0.61 mg anagrelide HCl); inactive ingredients include lactose, crospovidone, microcrystalline cellulose, gelatin

🧬 Mechanism of Action

Anagrelide selectively reduces platelet counts by inhibiting maturation of megakaryocytes—it suppresses transcription factors (e.g., GATA‑1, FOG‑1) and inhibits PDE‑3 activity, lowering megakaryocyte proliferation

🏥 Indication

• Essential thrombocythemia (ET): Used when platelet counts are high or when cytoreduction is needed, including cases resistant or intolerant to first-line agents like hydroxyurea .

💊 Dosage & Administration

• Initial dose: 0.5 mg four times daily or 1 mg twice daily  for at least 7 days

• Titration: Adjust weekly based on platelet response, up to a maximum of 10 mg/day (2.5 mg per dose of no more than four doses) .

• Monitoring: Platelets typically respond within 1–2 weeks; ongoing CBC monitoring is essential .

• Administration advice: Capsules may be taken with or without food; do not crush or chew.

• Missed dose: Take as soon as remembered unless close to next dose; do not double doses .

⚠️ Warnings & Precautions

• Cardiovascular: Risk of tachycardia, palpitations, cardiomyopathy, CHF, arrhythmias, QT prolongation—monitor via ECG and vital signs .

• Respiratory: Monitor for dyspnea, pulmonary hypertension, pleural effusion, fibrosis, pneumonitis

• Liver: Metabolized via CYP1A2; exposure increases eightfold in moderate hepatic impairment. Avoid in severe hepatic disease; check LFTs

• Bleeding risk: Caused by thrombocytopenia; caution with aspirin or anticoagulants

• Hypotension: PDE‑3 inhibition may cause vasodilation; monitor blood pressure and heart rate

• Renal & CNS: Monitor kidney function, cognitive state; dizziness and headache may occur .

• Pregnancy/Breastfeeding: Avoid use unless necessary; breastfeeding is not recommended during treatment and for at least one week after discontinuation

• Avoid Driving: It may cause dizziness—advise caution .

⚕️ Side Effects

Common

• Headache (up to 44%), arrhythmias (e.g., palpitations 26%), tachycardia 8%, chest pain 8%

• Gastrointestinal: Diarrhea 26%, nausea 17%, abdominal pain 16%, vomiting 10%, constipation, dyspepsia

• Edema: Peripheral edema 9%, generalized edema 21%

• Fatigue/weakness, back pain, fever, cough, dyspnea

• Dizziness, paresthesia, rash, pruritus, hair loss

Serious 

• Major cardiac complications (CHF, MI, heart block), cerebrovascular events, pericardial effusion

• Pulmonary disorders (fibrosis, infiltrates, hypertension), pancreatitis

• Hepatic injury, renal failure, seizures, serious bleeding

⚠️ Overdose

• Symptoms: Hypotension, sinus tachycardia, vomiting, severe thrombocytopenia—risk of bleeding

• Management: Discontinue immediately, monitor vitals and platelet counts, and provide supportive care .

🔄 Drug Interactions

• CYP1A2 substrates/inhibitors (e.g., fluvoxamine, theophylline) may alter anagrelide metabolism .

• Antiplatelet drugs (aspirin) may potentiate bleeding risk .

• Cardiac medications (e.g., milrinone, digoxin) may interact via PDE‑3 effects .

• Gastrointestinal modifiers (omeprazole, sucralfate) may alter absorption .

📌 Special Considerations

• Elderly: Higher exposure; exercise caution

• Pediatrics: Similar safety profile; dose per kg used in trials (0.5 mg up to QID)

• Renal impairment: No dosage adjustment typically needed

✅ Summary

Agrylin  is an effective oral platelet-lowering agent for essential thrombocythemia, particularly when hydroxyurea isn’t suitable. It requires careful dosing, monitoring of blood counts, cardiovascular, liver, renal, and pulmonary function, and vigilance for both common side effects and serious complications. Dose titration and supportive care are critical to safe long-term use.