What is Gleostine?

Gleostine, also known as lomustine, is a prescription medication used in the treatment of certain types of brain tumors, including gliomas and astrocytomas. It belongs to the class of chemotherapy drugs called alkylating agents. Gleostine works by interfering with the growth and reproduction of cancer cells, helping to slow down the progression of the tumor. This medication is taken orally in the form of capsules and is typically prescribed in a specific dosage regimen based on individual patient factors. While using Gleostine, it is crucial to closely follow the healthcare professional’s instructions and undergo regular medical check-ups to monitor the response and manage any potential side effects, such as nausea, vomiting, fatigue, and low blood cell counts.

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Lomustine
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What is Gleostine (Lomustine)?

Gleostine (lomustine) is an anti-cancer medication and alkylating agent used in the treatment of brain tumors that are either metastatic or primary and may also be prescribed to treat Hodgkin’s lymphoma alongside additional medications and therapies when those initial treatment methods have proven to be insufficient.

How is Gleostine Used?

Gleostine is taken orally as a single dose once every six weeks. Patients should not take this medication more often than once within a six-week period due to the risk of serious and potentially fatal results of ingesting additional doses of Gleostine.

This medication should be taken on an empty stomach to ensure proper absorption, and most patients are recommended to either take it in the evenings before bed to avoid vomiting or nausea or to take the dose about three hours after a meal, ensuring they do not consume additional foods or snacks for at least one to two hours after taking the medication.

Patients will often be advised to take their dose of Gleostine with an 8-ounce glass of water, but the directions provided by prescribing physicians may vary based on the patient’s condition, symptoms, and other relevant factors. Individuals taking Gleostine should follow their doctor’s exact instructions regarding administration and ingestion of the medication.

Storage

Gleostine capsules should be stored at an average temperature of 77°F (25°C) with only temporary exposure to low temperatures not dropping below 59°F (15°C) or high temperatures not exceeding 86°F (30°C).

Keep this medication out of the reach of children and pets at all times.

Due to the cytotoxic nature of Gleostine, this medication should be handled with utmost care to avoid skin or other exposure to the active ingredients. It is recommended that patients or those administering the medications wear protective gloves when handling the medication to avoid potential health risks.

Gleostine capsules should not be broken, and exposure to damaged Gleostine capsules should be avoided.

Pregnant individuals or those who may become pregnant should not be exposed to this medication. These individuals should avoid breathing in any dust that may come from the capsules and should not handle the medication for any reason.

Uses

Gleostine is prescribed for the treatment of two primary conditions:

  • Brain tumors
  • Hodgkin’s lymphoma

This medication is used in the treatment of brain tumors after a patient has already received radiotherapeutic or surgical procedures for their condition. It is used to treat both metastatic as well as primary brain tumors.

For patients diagnosed with Hodgkin’s lymphoma, this medication may be used alongside chemotherapy treatment if their condition has continued to progress after having received their initial chemotherapy treatment.

How Does Gleostine Work?

Gleostine is a type of medication classified as an alkylating agent. This type of medication functions by directly affecting the DNA molecules within the body and preventing the linkage of the DNA’s double helix strands. This effectively causes the strands to break, thereby eliminating the cells.

When this medication is used against cancer cells, it causes them to break apart and become unable to multiply and spread. However, due to the mechanism of action of alkylating agent medications, they must be administered with caution to avoid serious and potentially fatal side effects resulting from their impact on the cells of the body.

Dosage

Gleostine comes in the form of a capsule with the following strength options:

  • 10 mg
  • 40 mg
  • 100 mg

The most commonly prescribed dosage of Gleostine for both pediatric and adult patients is a single dose of 130 mg/m2 administered every six weeks. Only one dose should be administered orally and should not be repeated until at least six weeks have passed since the prior dose.

Doctors administering this medication are recommended to use doses that round up to the nearest 10 mg, and the prescribed dosage may need to be adjusted if the patient using the medication is simultaneously using additional myelosuppressive medications for treatment.

Patients that have impaired function related to bone marrow should be given a reduced dose of Gleostine every six weeks compared to those receiving the medication under other circumstances related to the condition for which it is being administered as well as any preexisting health conditions. The recommended dose for these individuals is 100 mg/m2 each time the medication is administered.

This medication should never be taken in excess, and patients should not be given additional doses before the end of the six-week period due to the high risk of fatal outcomes as well as severe toxicity.

Overdose

Taking additional doses and overdosing on Gleostine can result in fatal consequences. Patients who have overdosed or suspect that they may have overdosed on this medication should seek emergency medical attention and contact either their doctor or their local Poison Control Center immediately.

Symptoms of overdose of Gleostine include the following:

  • abdominal pain
  • abnormal hepatic function
  • bone marrow suppression
  • cough
  • diarrhea
  • dizziness
  • infection symptoms
  • lethargy
  • loss of appetite
  • liver issues
  • shortness of breath
  • vomiting

There are currently no known antidotes for an overdose of Gleostine, so seeking prompt medical attention in the event of an overdose is essential to ensure supportive treatment methods are able to be sufficiently used before the patient experiences severe or fatal repercussions.

Side Effects

The most common side effects of taking Gleostine are as follows:

  • diarrhea
  • hair loss
  • loss of appetite
  • mouth or lip sores
  • nausea
  • infection
  • vomiting

Many patients taking Gleostine for treatment have reported struggling with intense nausea and vomiting after taking a dose of the medication, and these individuals’ physicians will often prescribe additional medication to help alleviate the symptoms of vomiting and severe nausea. The highest intensity of these side effects typically only lasts for 24 hours, but some patients may have these symptoms continue for several days.

Some of the following more serious side effects may occur and should be reported to your doctor if they occur while taking Gleostine:

  • confusion
  • swelling of the feet or legs
  • vision changes

Patients that experience any of the following serious side effects while taking Gleostine should seek out immediate medical attention:

  • abdominal pain (that doesn’t resolve)
  • black stools
  • chest pain
  • cough
  • dark urine
  • difficulty breathing
  • jaundice (yellowing of the skin or eyes)
  • pain when breathing
  • urine changes (frequency, color)
  • vomit that looks similar to coffee grounds

Although rare, there is also the risk of an allergic reaction when taking any medication. If you experience the following symptoms of an allergic reaction after taking Gleostine, seek out emergency medical attention immediately:

  • difficulty breathing
  • dizziness
  • itching
  • rash on the skin
  • swelling of the throat, tongue, mouth, or face

Additionally, Gleostine is also reported to cause optic atrophy and blindness in some individuals. Please consult with your physician regarding the visual risks of taking this medication.

Warnings & Precautions

As a cytotoxic medication, Gleostine has a number of warnings and precautions for those taking the medication or who may be exposed to the medication during handling. Individuals who currently have an infection, are pregnant or may become pregnant, or have a blood disorder or disease of the lungs, liver, or kidneys are those who are most at risk in regard to adverse effects of ingestion or exposure to Gleostine.

Delayed Myelosuppression

A common risk of most anti-cancer medications is myelosuppression, which results in a patient having decreased activity of their bone marrow resulting in a lowered number of platelets, white blood cells, and red blood cells. Gleostine has been closely linked to delayed myelosuppression, which may occur after prolonged treatment or after a patient has already finished treatment with the medication. The patient’s prescribing physician will use regular blood testing to monitor the individual’s blood cells both during and after treatment. A severe decrease in bone marrow activity may be fatal.

Those who are taking or have previously taken Gleostine should report any of the following symptoms of delayed myelosuppression to their doctor immediately:

  • black or dark-colored stools
  • bruising
  • bleeding gums
  • clotting issues
  • chills
  • diarrhea
  • difficulty breathing
  • fatigue
  • fever
  • dizziness
  • headaches
  • nosebleeds
  • oral sores
  • paleness of the lips, nails, or skin
  • rapid heart rate
  • red or pink urine
  • shaking or shivering
  • small purple or red spots on the body
  • shortness of breath
  • sore throat
  • stuffy nose
  • weakness

Hepatotoxicity

Patients using Gleostine for treatment will need to have their liver function monitored for the duration of treatment as well as a period after the use of this medication has ended. Gleostine has been proven to increase a patient’s levels of bilirubin, alkaline phosphatase, and transaminases. Those with a history of diabetes, alcohol abuse, hepatitis, or a family history of liver disease are most at risk for developing these abnormalities.

Patients experiencing the following symptoms of hepatotoxicity should report the symptoms to and consult with their prescribing physician:

  • abdominal pain
  • dark-colored urine
  • nausea
  • fatigue
  • itchiness
  • jaundice (yellowing of the eyes or skin)
  • loss of appetite
  • light-colored bowel movements
  • vomiting

Infection Risk

Individuals taking Gleostine who currently have an active infection will likely experience a worsening of that infection due to the impact this medication has on the patient’s white blood cells and overall immunity. Due to the changes that occur in a patient’s immune system when taking this medication, they are also at a higher risk of getting an infection during treatment with Gleostine. Patients taking Gleostine should exercise additional caution when trying to avoid others who may have a contagious condition or infection (e.g., influenza, measles, chickenpox, etc.). If you are currently taking Gleostine and have been exposed to someone with an infection, you should inform your doctor as soon as possible.

Immunizations

Due to this medication resulting in impaired immunity, it is advised that these individuals do not receive any vaccinations or immunizations during treatment. However, if such proactive treatments as these are deemed medically necessary for the individual, they should be sure to inform their physician that they are currently using Gleostine for treatment before receiving any immunizations. Additionally, patients taking Gleostine that have an impaired immune system should avoid exposure to other individuals who have recently received any live vaccines (e.g., the intranasal flu vaccine).

Nephrotoxicity

Gleostine has been linked to patients experiencing a decrease in kidney size and progressive renal failure after receiving treatment with this medication. Those with a history of kidney disease or other kidney-related conditions should discuss this aspect of their medical history with their doctor before beginning treatment with this medication. Patients using Gleostine should have their renal function monitored for the duration of treatment as well as a period after treatment has stopped.

Pregnancy and Breastfeeding

Individuals who are pregnant are strongly advised against using this medication during pregnancy. Those who may become pregnant should either not take Gleostine or take appropriate measures to prevent pregnancy throughout the duration of their treatment with this medication. The minimum recommendations for those who remain sexually active during treatment with Gleostine are to use multiple forms of birth control throughout the duration of treatment as well as for a two-week period afterward. Generally, these practices should be continued for at least four months after treatment has ended to ensure a reduced and ideally nonexistent risk of harm to an unborn child conceived by a partner who has been treated with Gleostine. The impacts of Gleostine on a patient’s reproductive health while using this medication apply to both male and female patients.

Those currently taking Gleostine who become pregnant or suspect they may be pregnant should contact their doctor immediately.

Those who are currently pregnant and at risk of exposure to this medication should exercise extreme caution and avoid handling the medication as well as breathing in any dust from the capsules to avoid harm occurring to the unborn child.

It has not been determined whether this medication is passed through breastmilk, so patients taking Gleostine who may want to breastfeed a child should consult their physician before doing so. Often, it is recommended that breastfeeding be avoided during treatment with Gleostine and for a period of at least two weeks after treatment has ended.

Pulmonary Toxicity

The use of Gleostine has been linked to a high risk of pulmonary toxicity, especially in patients who have already finished treatment with the medication. The effects of this medication on the lungs may result in lung damage stemming from inflammation or scarring. This damage may either impact the patient’s ability to breathe in enough air or cause a reduction in the amount of oxygen that may be absorbed by the lungs. Patients who are currently taking or have previously taken Gleostine that develop symptoms such as chest pain, difficulty breathing, cough, or pain when trying to breathe should report these symptoms to their physician and seek emergency medical attention.

Secondary Malignancies

The long-term use of Gleostine for treatment has been commonly linked to the development of secondary malignancies, specifically myelodysplasia and acute myeloid leukemia. These conditions are most likely to develop within three to five years of exposure to medications such as Gleostine, with a decreased risk of development once a patient has reached the ten-year mark.

Additional Medical Conditions

If you have any of the following medical conditions, exercise caution when taking Gleostine and discuss your medical history with your doctor before beginning this medication:

  • an active infection
  • blood disorders
  • kidney disease
  • liver disease
  • lung disease
  • risk of pregnancy

Drug Interactions

Speak to your doctor about any medications or herbal supplements you are currently taking before beginning treatment with Gleostine. Discuss any concerns you may have with your doctor or a trusted pharmacist.

Although no specific medications are currently contraindicated with the use of Gleostine, those who have a medical history of kidney, liver, or lung disease that may be taking medications for these conditions should consult with their doctor regarding any potential modifications that may need to take place during treatment with Gleostine to ensure that their current medications and medical conditions remain appropriately treated.

Alternative Medications

For patients who are unable to take Gleostine or experiencing significant adverse side effects, alternative medications may be used to treat some of the associated conditions for which this medication is commonly prescribed:

  • procarbazine (Matulane)
  • vincristine (Marqibo, Vincasar PFS)

Additionally, there are other brand-name medications of lomustine available that a patient may be prescribed:

  • CeeNu
  • CCNU

Frequently Asked Questions

Gleostine may result in a number of different side effects, and hair loss has been reported among those who have taken the medication. This is a relatively common side effect of this medication, and the hair loss is often temporary, with hair growth returning after treatment has ended.

Since this medication may impact the body and its functions even after treatment has ended, a patient’s prescribing physician will monitor their functioning with the use of regular blood tests both during and after treatment. Patients should also be sure to report any unusual symptoms to their doctor even after treatment with Gleostine has stopped due to the risk of long-term health impacts and eventual development of other health conditions that have been reported by those who stopped using Gleostine.

If you’ve missed a dose of Gleostine, you will need to contact your prescribing physician. This medication should be taken on a fixed schedule.

Gleostine functions by damaging cancer cells and preventing further growth. As it damages the cancerous cells within the body, the cells are eventually destroyed and removed by the body and the additional medications and therapies used in the treatment process.

Most patients taking Gleostine will show signs of improvement in their condition within three to five days. However, some individuals may not experience a response to the medication until nearly two weeks after their first dose.

Yes. Gleostine’s ability to cross the blood-brain barrier has made it an effective medication for the treatment of brain tumors, one of the main reasons the medication is prescribed.

Patients are advised to avoid alcohol consumption on the days they take their recurring dose of Gleostine as alcohol is known to interact with the medication.

Gleostine will remain in a patient’s body for an extended period of time, and a patient’s prescribing physician will continue to order regular blood testing for at least six weeks after treatment with the medication has stopped. Individuals desiring to conceive a child after treatment with Gleostine are advised to postpone such attempts for at least four months after completing treatment with the medication.

Gleostine has been determined to affect the fertility of both male and female patients. Those desiring to eventually become pregnant or father a child should discuss the risks of this medication with their doctor before beginning treatment.

Most patients taking Gleostine experience the most common side effects of the medication—nausea and vomiting—for the first 24 hours after taking a dose. It is recommended that patients take the medication at bedtime and on an empty stomach to reduce the likelihood of experiencing these symptoms. Many patients report a loss of appetite lingering for multiple days after taking the medication, but these symptoms generally resolve within the span of about a week.

As of the beginning of 2021, Gleostine is no longer covered by Medicare.

This medication targets DNA and RNA, damaging the double helix strands and preventing further growth or spread of cancer cells. Gleostine essentially breaks apart the cells for the body and other medications to expel from the patient.

Gleostine is an anti-cancer medication known as an alkylating agent.

Gleostine contains lomustine as its primary active ingredient. The capsules also contain the following ingredients alongside lomustine: mannitol USP and magnesium stearate NF. The capsules themselves are composed of gelatin, which is an inactive ingredient, as well as additional inactive ingredients used strictly for coloring. Depending upon the strength of the medication and the assigned color of that particular capsule, the inactive coloring ingredients may be Indigotine (F&C Blue No. 2), yellow iron oxide, or titanium dioxide.

CCNU is an abbreviation for “cyclohexyl-chloroethyl-nitrosourea,” referring to the chemical compound for lomustine.

When taking your prescribed dose of Gleostine, your doctor will determine the appropriate dosage for you, and this may be provided in the form of a combination of the various Gleostine capsules available in order to provide your exact required dosage.

The use of Gleostine for long-term treatment comes with a significant risk of pulmonary toxicity. Patients using Gleostine or who have used Gleostine in the past should report any changes in lung function, chest pain, or breathing difficulties to their physician immediately.

Gleostine overdose is extremely dangerous and can often be fatal. Patients should not take any additional amounts of Gleostine aside from what has specifically been prescribed by their doctor for treatment of their condition. Individuals who have overdosed on this medication should seek emergency medical attention immediately as there is no antidote for Gleostine overdose, and supportive treatment will be required to manage the adverse symptoms of ingesting too much of this medication.