Mechlorethamine
**Mechlorethamine** (also known as nitrogen mustard) is a highly potent, cell-cycle nonspecific antineoplastic agent. It is historically significant as the first nitrogen mustard alkylating agent used in chemotherapy. In veterinary medicine, it is primarily utilized as an adjunctive treatment for lymphoreticular neoplasms, most notably as the "M" in the **MOPP rescue protocol** (Mechlorethamine, Oncovin [vincristine], Procarbazine, Prednisone) for relapsing canine and feline lymphoma. > **Clinical Pearl:** Mechlorethamine is a severe vesicant. Extreme care must be taken during intravenous administration to avoid extravasation, which can lead to devastating tissue necrosis and sloughing. Due to significant price increases and availability issues, some veterinary oncologists substitute dactinomycin or lomustine (CCNU) in rescue protocols. It can also be administered intracavitarily to treat malignant pleural and peritoneal effusions, where it acts as a sclerosing agent to cause adherence of serosal surfaces.
กลไกการออกฤทธิ์: Mechlorethamine is a **bifunctional alkylating agent**. * **Mechanism:** It undergoes intramolecular cyclization to form a highly reactive aziridinium ion. This ion reacts with nucleophilic sites on DNA (primarily the N7 position of guanine). * **Pathway:** Alkylation → **Cross-linking of DNA strands** (interstrand and intrastrand) → Inhibition of DNA replication and RNA transcription → Cell death (apoptosis). * It is **cell cycle-phase nonspecific**, meaning it can kill cells in any phase of the cell cycle, though it is most toxic to rapidly dividing cells. * When given intracavitarily, it induces a strong inflammatory response on serous membranes, leading to sclerosis and obliteration of the cavity space.
ขนาดยาตามชนิดสัตว์
- Lymphoma rescue (MOPP protocol) · 3 mg/m2 IV · IV · given on days 0 and 7 (or days 0 and 14) of a 28 day protocol · 28 day cycles · Given as part of a protocol that includes vincristine (or vinblastine), procarbazine, and prednisone (or prednisolone).
- Lymphoma rescue (MOPP protocol) · 3 mg/m2 IV · IV · given on days 0 and 7 (or days 0 and 14) of a 28 day protocol · 28 day cycles · Given as part of a protocol that includes vincristine (or vinblastine), procarbazine, and prednisone (or prednisolone).
ขนาดยาเป็นข้อมูลอ้างอิงทางคลินิกสำหรับสัตวแพทย์ผู้มีใบอนุญาต โปรดตรวจสอบกับฉลากล่าสุดและผู้ป่วยแต่ละรายเสมอ
วิธีการให้ยา
ข้อห้ามใช้
- Known infection
- Prior anaphylactic reaction to mechlorethamine
- Pregnancy (Category D teratogen)
- Anemia (relative)
- Bone marrow depression (relative)
- Tumor cell infiltration into bone marrow (relative)
- Patients who have received previous extensive chemotherapy or radiotherapy (relative)
อาการไม่พึงประสงค์
- Bone marrow depression (leukopenia, thrombocytopenia)
- Vomiting
- Nausea
- Ototoxicity (with high doses or regional perfusion)
- Alopecia
- Hyperuricemia
- Hepatotoxicity
- Peripheral neuropathy
- GI ulcers
- Severe tissue sloughing (if extravasated)
อันตรกิริยาระหว่างยา
- Immunosuppressant drugs (e.g., azathioprine, cyclophosphamide, corticosteroids) · May increase the risk of severe infection.
- Myelosuppressive drugs (e.g., chloramphenicol, flucytosine, amphotericin B, colchicine) · Additive bone marrow depression; use with extreme caution.
- Live vaccines · Increased risk of vaccine-induced infection or decreased vaccine efficacy; use with caution or avoid.
การติดตาม
- CBC with platelets (at least every 1-2 weeks until stable; then every 3 months)
- Liver function tests (initially before starting treatment and then every 3-4 months)
- Injection site for any signs of extravasation (redness, swelling, pain)
การได้รับยาเกินขนาด
Because of the extreme toxic potential of this agent, overdoses must be strictly avoided. Dosages must be calculated carefully (usually based on Body Surface Area in m2). Overdose will likely result in profound, potentially fatal myelosuppression and severe gastrointestinal toxicity.
ข้อมูลอ้างอิงยาของ VetSheet มีไว้สำหรับสัตวแพทย์ผู้มีใบอนุญาตเพื่อช่วยในการตัดสินใจทางคลินิก ไม่ใช่สิ่งทดแทนการวินิจฉัยของผู้เชี่ยวชาญหรือฉลากล่าสุดของผู้ผลิต