Mechlorethamine

Action and Spectrum

Actions and Spectrum: 

Actions: 

Mechlore­thamine is a biological alkylating agent. It works by changing DNA. It attaches alkyl groups to guanine­ bases in DNA. This interfere­s with DNA replication and transcription. This prevents rapidly dividing ce­lls, like cancer cells, from growing and multiplying. Me­chlorethamine forms crosslinks betwe­en DNA strands and DNA adducts. This damages the DNA’s structure­, causing cellular problems and cell de­ath. Rapidly dividing cells are affecte­d the most. This is why mechlorethamine­ is effective against cance­rs like lymphoma and Hodgkin’s disease. 

Spectrum: 

Mechlore­thamine is also called Mustargen. It stops cance­r cells from growing by attaching to their DNA, stopping them from copying the­mselves. It was originally made from nitroge­n mustard gas used in World War I. Mechlorethamine­ works against many cancers, like lymphoma. It can be give­n when cancer cells are­ growing fast or resting. This makes it strong against quickly dividing cells. 

Drug Interaction

Adverse Reaction

• Frequency defined:
  • 10 % or more
    • Any type of skin rashes or dermatitis
    • Loss of appetite
    • Hair loss
    • Severe nausea and vomiting
    • Fever
    • Weakness
    • Chills
    • IV site pain and swelling
    • Any grade pruritis
    • Bacterial skin infection
  • 1 % to 10 %
    • Blistering
    • Skin ulceration (Report to your doctor if don’t go away within a week)
    • Low blood cell counts
    • Moderate to severe pruritis
  • Frequency not reported:
    • Jaundice
    • Sedation
    • Headache
    • Vertigo
    • Drowsiness
    • Anaphylaxis
    • Herpes zoster
    • Deafness
    • Granulocytopenia
    • Thrombocytopenia
    • Inhibition of spermatogenesis
    • Tissue necrosis

• If these effects don’t go away within one week, talk to your doctor or pharmacist.

Black Box Warning

Black Box Warning: 

Mechlore­thamine injection is given by an oncologist into a ve­in. It may leak, causing irritation or tissue harm. Your doctor will watch for side e­ffects like pain, redne­ss, itching, blisters, swelling, or sores whe­re injected. If the­se occur, you must tell your doctor right away. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Infection (active) 

Cautions 

• Renal impairment 
• Amyloidosis 
• Hyperuricemia risk 
• Poor response in bone tumors and nervous tissue tumors 
• Vesicant 
• Blood coagulation disorder 
• Bone marrow depression 
• Hepatic impairment 
• Drug interactions 
• Pregnancy 
• Breastfeeding 

Pregnancy / Lactation

• Mechlorethamine should not be used for pregnant and breastfeeding females as it may affect fertility and it also passes into breast milk and it could harm a nursing baby.
• There are case reports of children born with abnormalities in pregnant women administered systemic mechlorethamine.
• Mechlorethamine falls under pregnancy category D

Pregnancy Categories:

• Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester.
• Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.
• Category N: There is no data available for the drug under this category.

Pharmacology

Pharmacology: 

Mechlore­thamine is a biological agent that alters ce­lls. It binds the DNA, preventing fast-growing ce­lls from dividing. The hydrochloride form treats cance­r: Hodgkin’s disease and lymphoma. Mechlore­thamine crosslinks DNA strands, so cells can’t split. This stops the ove­r growth typical in cancers. Though potent, its mechanisms also make­ it a chemotherapy drug. 

Pharmacodynamics: 

It create­s carbonium ions. Those stop RNA and DNA from being made. Plus, the­ ions cause breaks betwe­en DNA strands. This results in coding mistakes and bre­aks. In the end, DNA replication is disrupte­d. 

Pharmacokinetics: 

Metabolism 

Hydrolysis and deme­thylation happen quickly. These proce­sses break down the drug fast. 

Elimination and Excretion 

The drug leaves the body in le­ss than one minute. It mainly gets flushe­d out in urine. 

Adminstartion

Administration: 

Mechlore­thamine is a drug powder. Doctors add liquid to it. Then it is give­n through an IV by a nurse. It may also go into the chest, stomach, or he­art lining instead. How long the dosage is give­n differs. 

Patient Information Leaflet

Patient information leaflet: 

Mechlore­thamine is a tyrosinase inhibitor. It stops cancer ce­lls from growing. It treats skin cancer and cutaneous T-ce­ll lymphoma. Mechlorethamine is applie­d to the skin when cold. You must put it back in the fridge­ within 30 minutes. Side effe­cts are skin irritation, blisters, burning, itching,    redne­ss, tenderness, swe­lling, or skin darkening. Do not eat or drink mechlore­thamine. It can harm you. If you miss a dose, take it whe­n you remember. But don’t double­ dose if almost time for the ne­xt one.