Anagrelide

Registered South African indications:

• Essential thrombocythemia
• Polycythemia vera 
• Other myeloproliferative disorders

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Moderate to severe renal impairment
• Moderate to severe hepatic impairment

Cautions

• Pregnancy
• Breastfeeding
• Mild renal impairment
• Mild hepatic impairment
• Elderly
• Risk factors for QT prolongation
• Known or suspected cardiac disease
• Underlying cardiopulmonary disease 
• Galactose intolerance
• Lapp lactase deficiency 
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: cap

Essential thrombocythemia
Polycythemia vera
Other myeloproliferative disorders

• Oral (cap): Initial: 0.5-1mg/day, in 2-3 divided doses; Titrate by 0.5mg per day at intervals of 1 week; Maintenance: 1.5-3mg/day; Max: 2.5mg/dose

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Platelet count begins to respond within 7 to 14 days at the proper dosage

Not established for use in children below 18 years

Pregnancy

• FDA Pregnancy Category C

Breastfeeding

• Caution; not recommended

Renal Impairment

• Mild: Caution; no dose adjustment recommended 
• Moderate to severe: Contraindicated

Hepatic Impairment

• Mild: Caution; no dose adjustment recommended
• Moderate to severe: Contraindicated

Elderly

• Caution; no dose adjustment recommended

Central Nervous System Disorders

• Headache
• Dizziness
• Depression
• Amnesia
• Confusion
• Insomnia
• Paraesthesia
• Hypoaesthesia
• Nervousness
• Dry mouth
• Migraine
• Dysarthria
• Somnolence
• Fatigue
• Abnormal coordination

Cardiovascular Disorders

• Tachycardia
• Palpitations
• Chest pain
• Ventricular tachycardia
• Congestive cardiac failure
• Atrial fibrillation
• Supraventricular tachycardia
• Arrhythmia
• Hypertension
• Syncope
• Myocardial infarction
• Cardiomyopathy
• Cardiomegaly
• Pericardial effusion
• Angina pectoris
• Postural hypotension
• Vasodilatation
• Torsade de pointes

Respiratory Disorders

• Pulmonary hypertension
• Pneumonia
• Pleural effusion
• Dyspnoea
• Epistaxis
• Pulmonary infiltrates
• Interstitial lung disease

Gastrointestinal Disorders

• Diarrhoea
• Nausea and vomiting 
• Abdominal pain
• Flatulence
• Gastrointestinal haemorrhage
• Pancreatitis
• Anorexia
• Dyspepsia
• Constipation
• Gastrointestinal disorder
• Colitis
• Gastritis
• Gingival bleeding

Hepatobiliary Disorders

• Increased hepatic enzymes 
• Hepatitis

Genitourinary Disorders

• Impotence
• Renal failure
• Nocturia
• Tubulointerstitial nephritis
• Increased creatinine

Endocrine and Metabolic Disorders

• Fluid retention
• Oedema
• Weight loss
• Weight gain

Musculoskeletal Disorders

• Arthralgia
• Myalgia
• Back pain

Skin and Subcutaneous Tissue Disorders

• Rash
• Dry skin
• Alopecia
• Pruritus
• Skin discoloration

Immune, Blood and Lymphatic System Disorders

• Pancytopenia
• Thrombocytopenia
• Fever
• Chills
• Flu-like syndrome
• Haemorrhage
• Ecchymosis
• Anaemia

Sensory Disorders

• Diplopia
• Abnormal vision 
• Tinnitis

• CYP1A2 inhibitors
• CYP1A2 inducers
• Milrinone
• Enoximone
• Amrinone
• Olprinone 
• Cilostazol
• Agents which inhibit or modify platelet function
• Hormonal oral contraceptives

• Full blood count with differential
• Renal function
• Hepatic function
• Electrolytes
• Vital signs
• Cardiovascular examination
• Echocardiography 
• ECG

Anagrelide causes a dose dependent decrease in platelet count but the mechanism of action is unknown. Anagrelide exerts its action via reducing the size and ploidy of megakaryocytes in the post mitotic phase of maturation. When administered in high, non therapeutic doses anagrelide inhibits the c-AMP phosphodiesterase and ADP and collagen induced platelet aggregation.

Capsule 0.5mg

• Agrylin 0.5mg (Takeda) originator
• Thromboreductin (Key Oncologics)