anagrelide

General

Pronunciation:
a-na-gre-lide


Trade Name(s)

  • Agrylin

Ther. Class.
platelet-reducing agent

Indications

Treatment of thrombocythemia secondary to myeloproliferative disorders.

Action

Decreases maturation of megakaryocytes (platelet precursors).

Therapeutic Effect(s):

Reduction in platelet count with reduced risk of complications associated with thrombocythemia (thrombosis).

Pharmacokinetics

Absorption: Well absorbed after oral administration.

Distribution: Unknown.

Metabolism and Excretion: Extensively metabolized; <1% excreted unchanged in urine.

Half-life: 1.3 hr.

TIME/ACTION PROFILE (↓ in platelet count)

ROUTEONSETPEAKDURATION
PO7–14 days4–12 wk4 days†
†Increase in platelet count after discontinuation.

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity
  • Severe hepatic impairment
  • Congenital long QT syndrome
  • Concurrent use of other drugs known to prolong the QT interval
  • QTc interval ≥440 msec;
  • Lactation.

Use Cautiously in:

  • Cardiovascular, renal or mild to moderate hepatic impairment (monitor closely during treatment)
  • OB:   Use during pregnancy only if potential maternal benefit justifies potential fetal risk
  • Pedi:   Children < 7 yr (safety and effectiveness not established).

Adverse Reactions/Side Effects

CV: CEREBROVASCULAR ACCIDENT, COMPLETE HEART BLOCK, HF, MI, TORSADE DE POINTES, VENTRICULAR TACHYCARDIA, chest pain, edema, palpitations, angina, atrial fibrillation, pericarditis, pericardial effusion, orthostatic hypotension, tachycardia

Derm: alopecia, pruritus, rash

EENT: abnormal vision

GI: GI BLEEDING, HEPATOTOXICITY, PANCREATITIS, abdominal pain, diarrhea, flatulence, anorexia, constipation, dyspepsia, nausea, vomiting

GU: RENAL FAILURE, dysuria, hematuria, ↓ fertility (females)

Hemat: anemia

MS: arthralgia, back pain, myalgia, weakness

Neuro: paresthesia, SEIZURES, dizziness, headache, malaise

Resp: EOSINOPHILIC PNEUMONIA, INTERSTITIAL PNEUMONITIS, PULMONARY FIBROSIS, PULMONARY HYPERTENSION, cough, dyspnea, pharyngitis

Misc: fever

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

Route/Dosage

PO (Adults): 0.5 mg 4 times daily or 1 mg twice daily; may be ↑ weekly by 0.5 mg/day (not to exceed 10 mg/day or 2.5 mg as a single dose).

PO (Children ≥7 yr): 0.5 mg daily; may be ↑ weekly by 0.5 mg/day (not to exceed 10 mg/day or 2.5 mg as a single dose.Hepatic Impairment 
PO (Adults): Initiate at 0.5 mg daily; may be ↑ weekly by 0.5 mg/day.

Availability (generic available)

Capsules: 0.5 mg, 1 mg

Assessment

  • Monitor BP during initial therapy and periodically thereafter. May cause hypotension, especially upon standing.
  • Assess cardiovascular status and for underlying cardiopulmonary disease, and obtain at ECG before initiation of therapy and periodically during therapy. May cause QTc interval prolongation, vasodilation, tachycardia, palpitations, and heart failure. Hepatic impairment increases risk of CV side effects; monitor closely.
  • Monitor for signs and symptoms of interstitial lung diseases (progressive dyspnea with lung infiltrations). May occur from 1 wk to several years after initiating anagrelide. Symptoms usually improve after discontinuation of anagrelide.
  • Monitor for signs and symptoms of bleeding (vomit blood, pass bloody or black stools, unusual or unexplained bruising), especially in patients taking other drugs that may increase risk of bleeding.

Lab Test Considerations:

Monitor platelet count every 2 days during first wk of therapy and weekly until maintenance dose is reached. Platelet count usually begins to drop within 7–14 days.

  • Monitor AST and ALT prior to and periodically during therapy.
  • Monitor hemoglobin, WBC, BUN, and serum creatinine during the first 2 wk of therapy.

Potential Diagnoses

Implementation

  • Reduce dose to lowest possible to maintain platelet count of <600,000/mcl. Most patients experience an adequate response at a dose of 1.5–3 mg/day.

    • Interruption of therapy is usually followed by an increase in platelet count within 4 days.
  • PO May be taken without regard to food.

Patient/Family Teaching

  • Instruct patient to take medication as directed.
  • May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known. Caution patient to stand slowly.
  • Advise patient to notify health care professional promptly if signs and symptoms of bleeding, cardiovascular effects (chest pain, palpitations, irregular heartbeat), or pulmonary hypertension (shortness of breath, swelling in legs or ankles, lips and skin turn bluish color) occur.
  • Instruct patient to limit alcohol intake; may worsen side effects of anagrelide.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially anticoagulants, PDE3 inhibitors, NSAIDs, antiplatelet agents, selective serotonin reuptake inhibitors.
  • Rep:  Advise patient to notify health care professional if pregnancy is planned or suspected, and to avoid breastfeeding during and for 1 wk after last dose. May impair female fertility.

Evaluation/Desired Outcomes

Maintenance of platelet count at <600,000/mcl or decrease of ≥50% from baseline. Initial response is expected in 7–14 days with complete response in 4–12 wks.

anagrelide is a sample topic from the Davis's Drug Guide.

To view other topics, please or .

Medicine Central™ is a quick-consult mobile and web resource that includes diagnosis, treatment, medications, and follow-up information on over 700 diseases and disorders, providing fast answers—anytime, anywhere. .