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Mustargen (Mechlorethamine) Injection - Uses, Dose, Side effects

Mechlorethamine, also known as nitrogen mustard or mustine, is a chemotherapy drug that belongs to the class of alkylating agents. It was one of the first chemotherapy agents developed and was derived from mustard gas, a chemical warfare agent used in World War I.

Mustargen (Mechlorethamine) is a chemotherapeutic drug that belongs to the class of drugs called the alkylating agents. It is used to treat patients with Hodgkin's lymphoma.

Note: It is not available in the US.

Mustargen (Mechlorethamine) Uses:

Hodgkin lymphoma:
- Palliative treatment of Hodgkin lymphoma
Off Label Use of Mechlorethamine in Adults:
- Previously untreated Hodgkin lymphoma.

Mustargen (Mechlorethamine) Dose in Adults:

Dosage Based on Weight: When deciding how much of the medicine mechlorethamine to give, doctors should consider the person's "ideal dry weight." This means they should look at the person's weight without counting any extra fluid buildup (like swelling or fluid in the belly). This helps make sure the right amount of medicine is given.
Emetic Potential: Mechlorethamine can make people feel really sick and cause them to throw up a lot. To avoid this, doctors recommend using medicines that help prevent nausea and vomiting.

Mustargen (Mechlorethamine) Dose in the treatment of Hodgkin lymphoma, previously untreated (off-label use/dose): IV:

When treating Hodgkin lymphoma, mechlorethamine is given through an IV:

Stanford V treatment plan:

For early stage or less serious disease:
- Give 6 mg/m dose once on the first day of the month.
- Combine with several other medicines and radiation therapy.
- Do this treatment for 2 months or cycles.
For more serious or advanced disease:
- Still give 6 mg/m dose once on the first day of the month.
- Use the same combination of medicines and radiation therapy.
- This time, continue the treatment for 3 months or cycles.

Keep in mind, these doses and treatment plans aren't the official instructions. They're based on how some doctors have used the medicine in the past.

Mustargen (Mechlorethamine) Dose in Childrens:

Note:

The amount and timing of the mechlorethamine dose can change based on the treatment plan being used.
Always check the specific treatment instructions.
Mechlorethamine can make people feel very sick to their stomach.
To stop this, it's suggested to use medicine that prevents feeling sick and throwing up.

Mustargen (Mechlorethamine) Dose in the treatment of Hodgkin lymphoma:

Treating Hodgkin lymphoma with mechlorethamine:

MOPP treatment plan:
- Note: MOPP (sometimes with ABVD) is not commonly used anymore. Newer treatments have fewer side effects for Hodgkin lymphoma patients.
- For kids and teenagers: Through an IV, give 6 mg/m on the 1st and 8th day of a month-long cycle. This is combined with a few other drugs. Sometimes, additional drugs like doxorubicin, bleomycin, vinblastine, and dacarbazine might be added to the mix.
Stanford V treatment plan:
- For teenagers 16 years and older: Through an IV, give 6 mg/m just once on the first day in the 1st, 5th, and 9th weeks.

These are ways some doctors have used mechlorethamine in the past for Hodgkin lymphoma.

Pregnancy Risk Factor D

WARNING:

Mechlorethamine is very strong and dangerous. Be extremely careful when handling its powder and liquid forms.
Do not breathe in its dust or vapors. Avoid any contact with your skin, inside of your mouth or nose, and especially your eyes.
Pregnant women should stay away from it because it can harm the baby.
Before using or handling mechlorethamine, learn the safe ways to do so and always follow them.
Women who could get pregnant should avoid doing so while taking mechlorethamine.
Female patients might notice changes in their monthly periods, like getting them less often, or they might stop completely.
Male patients might face problems in producing sperm. This is more likely if mechlorethamine is used with other cancer drugs.

Use of memorethamine while breastfeeding

We're not sure if mechlorethamine gets into human breast milk.
Because it could possibly harm a breastfeeding baby, mothers should choose between stopping the drug or stopping breastfeeding.
This decision should consider how important the treatment is for the mother.

Mustargen (Mechlorethamine) Dose in Kidney Disease:

No dosage adjustments provided in the manufacturer's labeling.

Mustargen (Mechlorethamine) Dose in Liver disease:

The manufacturer doesn't give any guidelines about changing the dose.

From other sources:

If you have a mild-to-moderate liver problem: No need to change the dose (as per Ecklund 2005).
If you have a serious liver problem: The mechlorethamine dose remains the same. However, other cancer drugs given with it might need to be adjusted until the liver gets better (as per Ecklund 2005).

Side effects of Mustargen (Mechlorethamine):

Cardiovascular:
- Local thrombophlebitis
Central nervous system:
- Brain disease (high dose)
- Drowsiness
- Headache
- Lethargy
- Metallic taste
- Sedation
- Vertigo
Dermatologic:
- Alopecia
- Diaphoresis
- Erythema multiforme
- Maculopapular rash
- Skin rash
Endocrine & metabolic:
- Amenorrhea
- Hyperuricemia
- Oligomenorrhea
Gastrointestinal:
- Anorexia
- Diarrhea
- Mucositis
- Nausea
- Vomiting
Genitourinary:
- Inhibition of spermatogenesis
Hematologic & oncologic:
- Agranulocytosis
- Granulocytopenia
- Hemolytic anemia
- Leukopenia
- Lymphocytopenia
- Pancytopenia
- Petechia
- Thrombocytopenia
Hepatic:
- Jaundice
Hypersensitivity:
- Anaphylaxis
- Hypersensitivity reaction
Infection:
- Herpes zoster
Neuromuscular & skeletal:
- Weakness
Ophthalmic:
- Lacrimation
Otic:
- Deafness
- Tinnitus
Miscellaneous:
- Fever
- Tissue necrosis (extravasation)

Contraindication to Mustargen (Mechlorethamine):

Don't use mechlorethamine if:

You've had a severe allergic reaction to it or any of its ingredients before.
You have a known infection.

Warnings and precautions

Bone Marrow Effects of Mechlorethamine:

Mechlorethamine can harm your bone marrow, leading to a drop in different types of blood cells. This means you might have fewer white blood cells, red blood cells, and platelets.
About 6 to 8 days after taking it, you might see a drop in certain white blood cells and platelets. This usually lasts 10 to 21 days.
About 2 weeks after taking it, you might have fewer red blood cells, but this is usually not too severe.
Within a day of taking the medicine, you might see a drop in another type of white blood cell.
Very rarely, some people get even worse blood problems.
People who have a lot of the disease, are weak or tired, or have had certain treatments before might be at higher risk for these blood problems.
Some people might have these bone marrow issues for a long time (50 days or more).
Always check your blood counts. If your platelet count drops a lot, you could bleed more easily.
Be extra careful if you already have low blood cell counts or if the cancer has gotten into the bone marrow. If the treatment works and the cancer in the bone marrow goes away, the bone marrow might start to work better. But if the treatment doesn’t work or if you've had a lot of treatments before, you could have more severe drops in blood counts. This can be life-threatening.
Before starting other treatments like radiation or other chemotherapy, make sure your bone marrow has had time to recover after taking mechlorethamine.

When Mechlorethamine Leaks Outside of the Vein (Extravasation):

Mechlorethamine is a vesicant, which means it can cause severe skin damage if it leaks out of the vein.
WARNING: If it leaks, it can cause painful swelling and skin damage.
If a leak happens, act fast:
- Inject the area with a special solution called 1/6 molar sodium thiosulfate.
- After that, put a dry cold compress on the area for 6 to 12 hours. This helps reduce the damage.
To make the 1/6 molar solution:
- Mix 4.14 g of sodium thiosulfate in 100 mL of sterile water.
- Or use 2.64 g of a dry form of sodium thiosulfate in 100 mL.
- Another option is to mix 4 mL of a 10% sodium thiosulfate injection with 6 mL of sterile water.
Always check that the needle or tube is in the right place in the vein before and during giving the drug. This helps prevent leaks.
It's super important to make sure the medicine doesn't leak out of the vein.

Stomach Issues with Mechlorethamine:

Mechlorethamine can strongly make people feel like throwing up.
To help prevent this feeling of sickness, it's suggested to take medicines that stop nausea and vomiting.
This feeling of nausea can last for a whole day.

Allergic Reaction to Mechlorethamine:

Some people have had allergic reactions to mechlorethamine.
In serious cases, people experienced a severe allergic reaction called anaphylaxis.

Effects on the Immune System from Mechlorethamine:

Mechlorethamine can weaken the immune system.
This means patients might be more likely to get infections, whether from bacteria, viruses, or fungi.

Risk of New Cancers from Mechlorethamine:

Drugs like mechlorethamine, called alkylating agents, can increase the chance of getting another type of cancer.
The risk might be higher if patients also get radiation or other cancer drugs at the same time.

Problem from Rapid Breakdown of Tumors with Mechlorethamine:

Patients might get high levels of uric acid in their blood, especially if they have lymphoma.
To help prevent this, make sure patients drink enough water.
If needed, give them medicine to lower the uric acid levels.

Issue with Mechlorethamine and Amyloidosis:

Drugs like mechlorethamine might speed up the development of a condition called amyloidosis.
Only use mechlorethamine if there aren't any areas of infection or long-term inflammation in the body.

Tumors that Don't Respond to Mechlorethamine:

Bone and nerve tumors usually don't get better with mechlorethamine.
It's not recommended to use mechlorethamine for tumors that have spread widely in the body.

Mechlorethamine(systemic) (United States: Not available): Drug Interaction

Risk Factor C (Monitor therapy)
Chloramphenicol (Ophthalmic)	May enhance the adverse/toxic effect of Myelosuppressive Agents.
CloZAPine	Myelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for neutropenia may be increased.
Coccidioides immitis Skin Test	Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test.
Denosumab	May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased.
Mesalamine	May enhance the myelosuppressive effect of Myelosuppressive Agents.
Ocrelizumab	May enhance the immunosuppressive effect of Immunosuppressants.
Pidotimod	Immunosuppressants may diminish the therapeutic effect of Pidotimod.
Promazine	May enhance the myelosuppressive effect of Myelosuppressive Agents.
Siponimod	Immunosuppressants may enhance the immunosuppressive effect of Siponimod.
Smallpox and Monkeypox Vaccine (Live)	Immunosuppressants may diminish the therapeutic effect of Smallpox and Monkeypox Vaccine (Live).
Tertomotide	Immunosuppressants may diminish the therapeutic effect of Tertomotide.
Trastuzumab	May enhance the neutropenic effect of Immunosuppressants.
Risk Factor D (Consider therapy modification)
Baricitinib	Immunosuppressants may enhance the immunosuppressive effect of Baricitinib. Management: Use of baricitinib in combination with potent immunosuppressants such as azathioprine or cyclosporine is not recommended. Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted.
Deferiprone	Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely.
Echinacea	May diminish the therapeutic effect of Immunosuppressants.
Fingolimod	Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections).
Leflunomide	Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly.
Lenograstim	Antineoplastic Agents may diminish the therapeutic effect of Lenograstim. Management: Avoid the use of lenograstim 24 hours before until 24 hours after the completion of myelosuppressive cytotoxic chemotherapy.
Lipegfilgrastim	Antineoplastic Agents may diminish the therapeutic effect of Lipegfilgrastim. Management: Avoid concomitant use of lipegfilgrastim and myelosuppressive cytotoxic chemotherapy. Lipegfilgrastim should be administered at least 24 hours after the completion of myelosuppressive cytotoxic chemotherapy.
Nivolumab	Immunosuppressants may diminish the therapeutic effect of Nivolumab.
Palifermin	May enhance the adverse/toxic effect of Antineoplastic Agents. Specifically, the duration and severity of oral mucositis may be increased. Management: Do not administer palifermin within 24 hours before, during infusion of, or within 24 hours after administration of myelotoxic chemotherapy.
Roflumilast	May enhance the immunosuppressive effect of Immunosuppressants.
Sipuleucel-T	Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Management: Evaluate patients to see if it is medically appropriate to reduce or discontinue therapy with immunosuppressants prior to initiating sipuleucel-T therapy.
Tofacitinib	Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants.
Vaccines (Inactivated)	Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation.
Risk Factor X (Avoid combination)
BCG (Intravesical)	Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical).
BCG (Intravesical)	Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical).
Cladribine	May enhance the immunosuppressive effect of Immunosuppressants.
Cladribine	May enhance the myelosuppressive effect of Myelosuppressive Agents.
Dipyrone	May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased
Natalizumab	Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased.
Pimecrolimus	May enhance the adverse/toxic effect of Immunosuppressants.
Tacrolimus (Topical)	May enhance the adverse/toxic effect of Immunosuppressants.
Upadacitinib	Immunosuppressants may enhance the immunosuppressive effect of Upadacitinib.
Vaccines (Live)	Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants. Exceptions: Smallpox and Monkeypox Vaccine (Live).

Monitoring parameters:

Blood Tests:

Check complete blood count (CBC) to see all types of blood cells.
Specifically, look at different white blood cells (differential) and platelets.

Kidney and Liver Check:

Test how well the kidneys and liver are working.

Allergic Reactions:

Watch for signs like rash, itching, or trouble breathing which might mean the patient is allergic to the drug.

Infections:

Keep an eye out for symptoms of infections since the drug can weaken the immune system.

Giving the Drug:

Make sure the drug isn't leaking out of the vein, which is called extravasation. This can harm the skin around the injection site.

How to administer Mustargen (Mechlorethamine)?

Giving the Drug:

Inject slowly into an IV that's flowing well over a few minutes.
Mechlorethamine can make people feel very nauseous. So, give medicines to prevent this feeling and throwing up.

Preparation:

Mix and get the drug ready right before giving it.

Handling Leaks (Extravasation):

Mechlorethamine can damage skin if it leaks out of the vein.
Always make sure the needle or tube is in the right spot in the vein.
If the drug starts leaking:
- Stop the drug and unhook it, but leave the needle in place.
- Try to gently suck out any leaked drug (but don't flush the area with more liquid).
- Take out the needle and lift up the arm or leg.

Treating Leaks:

If there's a leak, treat with a special solution called Sodium thiosulfate 1/6 M.
- Inject this solution into the skin area where the drug leaked.
- Use 2 mL of the solution for every mg of mechlorethamine that might have leaked out.
After that, put ice on the area for 6 to 12 hours. Or, you can use a cold dry cloth for 20 minutes, 4 times a day for 1 to 2 days.

This is how you give mechlorethamine safely and handle any issues if they happen.

Mechanism of action of Mustargen (Mechlorethamine):

What It Does: Mechlorethamine is a type of medicine that messes up the building blocks of our genetic material (DNA and RNA).
How It Works: It creates something called carbonium ions, which stop the DNA and RNA from being made properly.
Cross-Links in DNA: It also makes connections between different parts of the DNA. These connections can mess up the code and cause breaks in the DNA.
DNA Damage and Replication: All this trouble makes it hard for cells to copy their DNA correctly. It also messes up the process of making new cells.
Cell Phase Effects: Although it doesn't stick to a specific phase, it mostly works when cells are copying DNA (S phase) and can stop cells from growing (G phase).