protein synthesis inhibitors
Treatment of chronic or accelerated phase chronic myeloid leukemia (CML) that has become resistant or intolerant to at least 2 tyrosine kinase inhibitors.
Inhibits protein synthesis.
Improved hematologic parameters and survival in CML.
Absorption: Absorbed following subcutaneous administration.
Distribution: Widely distributed.
Metabolism and Excretion: Metabolized by enzymes in plasma; not metabolized by the liver; 37 % excreted unchanged in urine.
Half-life: 6 hr.
TIME/ACTION PROFILE (response in Chronic Phase CML)
|Subcut||3.5 mo||unknown||12.5 mo|
TIME/ACTION PROFILE (response in Accelerated Phase CML)
|Subcut||2.3 mo||unknown||4.7 mo|
- OB: Lactation: Pregnancy or lactation.
Use Cautiously in:
- Geri: ↑ risk of hematologic toxicity
- Pedi: Safety and effectiveness not established.
Adverse Reactions/Side Effects
CNS: fatigue, headache, insomnia, anxiety, depression, mental status changes
EENT: epistaxis, ear pain, tinnitus
CV: angina, arrhythmias, peripheral edema
GI: diarrhea, anorexia, mucositis, nausea, constipation, stomatitis, ↑ liver function tests, upper abdominal pain, vomiting
Derm: alopecia, rash, hyperpigmentation, pruritus
Hemat: ANEMIA, NEUTROPENIA, THROMBOCYTOPENIA, lymphopenia
Local: injection site reactions
MS: arthralgia, myalgia, musculoskeletal pain
Metabolic: INFECTION, fever
Misc: hypersensitivity reactions, night sweats
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
SC (Adults): Induction– 1.25 mg/m2 twice daily for 14 consecutive days of a 28-day cycle; maintenance– 1.25 mg/m2 twice daily for 7 consecutive days of a 28-day cycle. Modifications required for toxicity, treatment should be continued as long as benefit is noted.
Lyophilized powder for subcutaneous injection: 3.5 mg/vial
- Monitor for bone marrow depression. Assess for bleeding (bleeding gums; bruising; petechiae; blood in stools, urine, and emesis; confusion, slurred speech, altered vision) and avoid IM injections and taking rectal temperatures if platelet count is low. Apply pressure to venipuncture sites for 10 min. Assess for signs of infection during neutropenia. Anemia may occur. Monitor for increased fatigue, dyspnea, and orthostatic hypotension.
- Assess for non-hematologic toxicities. Manage symptomatically and interrupt or delay therapy until toxicity is resolved.
Lab Test Considerations:
Monitor CBC and platelet count weekly during induction and maintenance cycles. After initial maintenance cycles, monitor CBC and platelet count every 2 wks or as clinically indicated. If Grade 4 neutropenia occurs (ANC <0.5 × 109 /L) or Grade 3 thrombocytopenia (platelet count <50 × 109 /L) during a cycle, delay starting next cycle until ANC is ≥1.0 × 109 /L and platelet count is ≥50 × 109 /L. For next cycle, also reduce number of days by 2 days (e.g. to 12 or 5 days).
- Monitor blood glucose levels frequently, especially in patients with diabetes or risk factors for diabetes. Avoid use in patients with poorly controlled diabetes mellitus until glycemic control is established.
- May cause ↓ hemoglobin, leukocytes, neutrophils, and platelets. May cause ↑ ALT, bilirubin, serum creatinine, glucose, and uric acid.
- Risk for infection (Adverse Reaction)
- Reconstitute with 1 mL of 0.9% NaCl prior to use. Swirl gently until solution is clear; usually <1 minute. Concentration: 3.5 mg/mL.Do not administer solutions that are discolored or contain particulate matter. Avoid contact with skin; immediately wash affected area with soap and water. Protect from light. Use solution within 12 hr at room temperature or 6 days if refrigerated. Discard unused solution.
- Solution should be prepared in a biologic cabinet. Wear gloves, gown, and mask while handling medication. Discard IV equipment in specially designated containers.
- SC Inject twice daily. Avoid areas that are tender, red, bruised, hard, or that have scars or stretch marks.
- Instruct patient to notify health care professional promptly if fever; chills; cough; hoarseness; sore throat; signs of infection; lower back or side pain; painful or difficult urination; bleeding gums; bruising; petechiae; blood in stools, urine, or emesis; increased fatigue; dyspnea occurs. Caution patient to avoid crowds and persons with known infections. Instruct patient to use soft toothbrush and electric razor and to avoid falls. Caution patient not to drink alcoholic beverages or take medication containing aspirin or NSAIDs; may precipitate gastric bleeding.
- May cause fatigue; caution patient to avoid driving and other activities requiring alertness until response to medication is known.
- Advise patients with diabetes to monitor blood glucose levels closely; may cause hyperglycemia.
- May cause rash, nausea, diarrhea, abdominal pain, constipation, and vomiting. Advise patient to notify health care professional if symptoms persist or if rash is severe.
- Discuss with patient the possibility of hair loss. Explore methods of coping. May also cause darkening of skin and fingernails.
- Advise female patient to that omacetaxine is teratogenic. Avoid pregnancy and breastfeeding during therapy.
- Home Care Issues: If patient is to administer omacetaxine at home, teach patient proper technique for injection, storage, and disposal of equipment. Provide solution prepared by health care professional, protective eye wear, and sharps container.
Improved hematologic parameters in CML.
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