Gleostine 100mg (hundred Mg) Caps

Manufacturer NEXTSOURCE BIOTECHNOLOGY Active Ingredient Lomustine(loe MUS teen) Pronunciation loe-MUS-teen
WARNING: This drug may lower the ability of the bone marrow to make blood cells that the body needs. If blood cell counts get very low, this can lead to bleeding problems, infections, or anemia. Some infections have been severe and even deadly. If you have questions, talk with the doctor.Most of the time, this drug is to be taken as 1 dose every 6 weeks. Taking more often than you are told may raise your chance of very bad and sometimes deadly side effects. Do not take a dose of this drug more than 1 time within a 6 week period without talking with your doctor.Have your blood work checked often for at least 6 weeks after a dose. Talk with your doctor. @ COMMON USES: It is used to treat a type of brain tumor.It is used to treat a type of lymphoma.
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Drug Class
Antineoplastic Agent
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Pharmacologic Class
Alkylating Agent, Nitrosourea
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Pregnancy Category
Category D
FDA Approved
Aug 2010
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Lomustine is a type of chemotherapy medication used to treat certain cancers, like brain tumors and Hodgkin's lymphoma. It works by damaging the cancer cells' genetic material, preventing them from growing and multiplying. It is taken by mouth as a capsule, usually once every six weeks.
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How to Use This Medicine

To take this medication correctly, follow your doctor's instructions and read all accompanying information carefully. Your prescribed dose may consist of two or more different strengths and colors of capsules.

To minimize the risk of stomach upset or vomiting, consider taking this medication on an empty stomach. However, consult with your doctor before doing so.

When handling this medication, exercise caution and follow the guidance provided by your doctor or pharmacist. It is recommended to wear gloves when touching the capsules. If you come into contact with a broken capsule or the medication inside, wash the affected area with soap and water immediately.

To store this medication properly, keep it at room temperature in a dry location, avoiding storage in a bathroom.

If you miss a dose, contact your doctor for advice on the best course of action.
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Lifestyle & Tips

  • Avoid contact with people who are sick or have infections, as your immune system will be weakened.
  • Practice good hand hygiene.
  • Avoid activities that could cause cuts or bruises due to increased bleeding risk.
  • Report any signs of infection (fever, chills, sore throat) or unusual bleeding/bruising immediately.
  • Maintain good hydration.
  • Discuss any planned vaccinations with your doctor, as live vaccines are generally not recommended.
  • Use effective contraception during treatment and for a period after, as lomustine can cause birth defects.

Dosing & Administration

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Adult Dosing

Standard Dose: 130 mg/m² orally as a single dose every 6 weeks. Dose adjustments are made based on nadir blood counts from the previous dose.

Condition-Specific Dosing:

Hodgkin's Lymphoma: 130 mg/m² orally every 6 weeks.
Brain Tumors: 130 mg/m² orally every 6 weeks.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: 130 mg/m² orally as a single dose every 6 weeks. Dose adjustments based on nadir blood counts.
Adolescent: 130 mg/m² orally as a single dose every 6 weeks. Dose adjustments based on nadir blood counts.
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Dose Adjustments

Renal Impairment:

Mild: Use with caution; monitor blood counts closely. No specific dose adjustment guidelines.
Moderate: Use with caution; monitor blood counts closely. No specific dose adjustment guidelines.
Severe: Use with caution; monitor blood counts closely. No specific dose adjustment guidelines.
Dialysis: Not available. Use with extreme caution; monitor blood counts closely.

Hepatic Impairment:

Mild: Use with caution; monitor blood counts closely. No specific dose adjustment guidelines.
Moderate: Use with caution; monitor blood counts closely. No specific dose adjustment guidelines.
Severe: Use with caution; monitor blood counts closely. No specific dose adjustment guidelines.

Pharmacology

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Mechanism of Action

Lomustine is a nitrosourea alkylating agent. It acts by alkylating DNA and RNA, leading to cross-linking of DNA strands and inhibition of DNA synthesis, RNA synthesis, and protein synthesis. It also carbamoylates proteins, which may contribute to its cytotoxic effects. Its highly lipophilic nature allows it to readily cross the blood-brain barrier.
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Pharmacokinetics

Absorption:

Bioavailability: Not explicitly quantified as a percentage, but rapidly and completely absorbed from the gastrointestinal tract.
Tmax: Parent drug: 3-4 hours; Active metabolites: 1-6 hours
FoodEffect: Not significantly affected by food.

Distribution:

Vd: Not available (highly lipophilic, widely distributed)
ProteinBinding: Approximately 50%
CnssPenetration: Yes (readily crosses blood-brain barrier)

Elimination:

HalfLife: Parent drug: 10-20 minutes; Active metabolites: 16-48 hours
Clearance: Not available
ExcretionRoute: Primarily renal excretion of metabolites (approximately 50% within 12 hours, 75% within 96 hours); small amount excreted in feces.
Unchanged: Less than 1%
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Pharmacodynamics

OnsetOfAction: Cytotoxic effects are delayed due to the mechanism of action and delayed myelosuppression.
PeakEffect: Myelosuppression nadir typically occurs 4-6 weeks after a dose.
DurationOfAction: Single dose effects last for approximately 6 weeks due to prolonged myelosuppression.
Confidence: Medium

Safety & Warnings

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BLACK BOX WARNING

Severe myelosuppression (including leukopenia and thrombocytopenia) is a common and dose-limiting toxicity of lomustine, which may be delayed and prolonged. Nadirs typically occur 4-6 weeks after a dose. Cumulative myelosuppression may occur with repeated doses. Pulmonary toxicity, including fatal pulmonary fibrosis, has been reported. Renal toxicity and hepatotoxicity have also been reported.
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Side Effects

Serious Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or discolored sputum
+ Painful urination
+ Mouth sores
+ Wounds that won't heal
Signs of bleeding, such as:
+ Vomiting or coughing up blood
+ Coffee ground-like vomit
+ Blood in the urine
+ Black, red, or tarry stools
+ Bleeding gums
+ Abnormal vaginal bleeding
+ Unexplained bruises or bruises that get bigger
+ Uncontrollable bleeding
Signs of liver problems, including:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of lung or breathing problems, including:
+ Shortness of breath or other breathing difficulties
+ Cough
+ Fever
Chest pain
Confusion
Extreme fatigue or weakness
Balance problems
Speech difficulties
Mouth irritation or mouth sores
Changes in vision
Loss of vision

Other Possible Side Effects

Like all medications, this drug can cause side effects. Many people may not experience any side effects or may only have mild ones. If you're bothered by any of the following side effects or if they don't go away, contact your doctor or seek medical attention:

Upset stomach or vomiting
Hair loss

This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, talk to your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Fever (100.4°F or higher) or chills
  • Sore throat, cough, or other signs of infection
  • Unusual bleeding (nosebleeds, bleeding gums) or bruising
  • Extreme fatigue or weakness
  • Shortness of breath or persistent cough
  • Yellowing of skin or eyes (jaundice)
  • Dark urine or light-colored stools
  • Significant nausea, vomiting, or diarrhea that doesn't improve
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are breastfeeding or plan to breastfeed. You should not breastfeed while taking this medication and for 2 weeks after your last dose.

Potential Interactions with Other Medications or Health Conditions

This medication may interact with other medications or worsen certain health conditions. To ensure your safety, it is crucial to:

Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss any health problems you have, as they may affect the safety or efficacy of this medication.
* Check with your doctor before starting, stopping, or changing the dose of any medication to avoid potential interactions or adverse effects.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regularly check your lung function as directed by your doctor and discuss any concerns with them.

As this medication may increase your risk of developing infections, it is crucial to practice good hygiene by washing your hands frequently and avoiding close contact with individuals who have infections, colds, or flu.

You may experience an increased risk of bleeding due to this medication. To minimize this risk, be cautious and avoid injuries. Additionally, use a soft toothbrush and an electric razor to reduce the risk of bleeding.

Long-term use of this medication may elevate your risk of developing other types of cancer. If you have any questions or concerns, consult your doctor.

If you experience gastrointestinal side effects such as stomach upset, vomiting, diarrhea, or decreased appetite, discuss them with your doctor, as there may be ways to mitigate these effects.

Before receiving any vaccinations, consult your doctor, as certain vaccines may not be effective or may increase your risk of infection when taken with this medication.

This medication should be used with caution in children, and your doctor should be consulted to discuss the potential risks and benefits.

It is also important to note that this medication may affect fertility, potentially leading to difficulties in becoming pregnant or fathering a child. If you plan to conceive, discuss this with your doctor before initiating treatment.

If you are pregnant or may become pregnant, it is crucial to be aware that this medication may harm the unborn baby. To prevent pregnancy, you and your partner must use effective birth control methods while taking this medication and for a specified period after the last dose. Your doctor will advise you on the duration of birth control use. If you or your partner becomes pregnant, notify your doctor immediately.
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Overdose Information

Overdose Symptoms:

  • Severe myelosuppression (very low white blood cell, red blood cell, and platelet counts)
  • Severe nausea and vomiting
  • Neurological symptoms (e.g., confusion, seizures)
  • Liver or kidney dysfunction

What to Do:

There is no specific antidote for lomustine overdose. Management is supportive, including blood product transfusions for myelosuppression, antiemetics for nausea/vomiting, and close monitoring of vital signs and organ function. Call 1-800-222-1222 (Poison Control) immediately.

Drug Interactions

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Major Interactions

  • Live vaccines (increased risk of infection)
  • Other myelosuppressive agents (additive myelosuppression)
  • Phenytoin (decreased phenytoin levels, potential for seizures)
  • Cimetidine (may increase myelosuppression)
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Moderate Interactions

  • Digoxin (decreased digoxin levels)
  • Theophylline (decreased theophylline levels)

Monitoring

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Baseline Monitoring

Complete Blood Count (CBC) with differential and platelet count

Rationale: To establish baseline hematologic status and assess for pre-existing myelosuppression.

Timing: Prior to initiation of therapy.

Liver Function Tests (LFTs)

Rationale: To assess baseline hepatic function, as lomustine is hepatically metabolized and can cause hepatotoxicity.

Timing: Prior to initiation of therapy.

Renal Function Tests (Creatinine, BUN)

Rationale: To assess baseline renal function, as lomustine and its metabolites are renally excreted and can cause nephrotoxicity.

Timing: Prior to initiation of therapy.

Pulmonary Function Tests (PFTs)

Rationale: Consider for patients with pre-existing pulmonary disease or risk factors for pulmonary toxicity.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Complete Blood Count (CBC) with differential and platelet count

Frequency: Weekly for at least 6 weeks after each dose.

Target: Depends on nadir and recovery; generally, ANC > 1500/mm³, platelets > 100,000/mm³ for next dose.

Action Threshold: Dose adjustment or delay if ANC < 1500/mm³ or platelets < 100,000/mm³.

Liver Function Tests (LFTs)

Frequency: Periodically, or as clinically indicated.

Target: Within normal limits or stable baseline.

Action Threshold: Elevations may require dose adjustment or discontinuation.

Renal Function Tests (Creatinine, BUN)

Frequency: Periodically, or as clinically indicated.

Target: Within normal limits or stable baseline.

Action Threshold: Elevations may require dose adjustment or discontinuation.

Pulmonary Function Tests (PFTs)

Frequency: If clinically indicated (e.g., new or worsening respiratory symptoms).

Target: Stable.

Action Threshold: Significant decline may indicate pulmonary toxicity and require discontinuation.

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Symptom Monitoring

  • Signs of infection (fever, chills, sore throat)
  • Unusual bleeding or bruising
  • Severe nausea, vomiting, or diarrhea
  • Fatigue, weakness
  • Shortness of breath, cough, or other respiratory symptoms
  • Jaundice, dark urine, or other signs of liver problems
  • Signs of kidney problems (changes in urination)

Special Patient Groups

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Pregnancy

Lomustine is classified as Pregnancy Category D. It can cause fetal harm when administered to a pregnant woman. Women of childbearing potential should be advised to avoid becoming pregnant during therapy. If the drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Trimester-Specific Risks:

First Trimester: High risk of teratogenicity and fetal malformations.
Second Trimester: Risk of fetal toxicity, including myelosuppression and growth restriction.
Third Trimester: Risk of fetal toxicity, including myelosuppression and growth restriction.
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Lactation

It is not known whether lomustine is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from lomustine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Breastfeeding is generally contraindicated.

Infant Risk: High risk of serious adverse effects, including myelosuppression and potential carcinogenicity.
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Pediatric Use

Lomustine has been used in pediatric patients for certain brain tumors and Hodgkin's lymphoma. Dosing is typically weight or body surface area-based. Pediatric patients may be more susceptible to certain toxicities, particularly pulmonary fibrosis. Close monitoring of blood counts and organ function is essential.

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Geriatric Use

Clinical studies of lomustine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Elderly patients may have reduced renal or hepatic function and may be more susceptible to myelosuppression and other toxicities. Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Clinical Information

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Clinical Pearls

  • Lomustine causes delayed and prolonged myelosuppression, with nadirs typically occurring 4-6 weeks after a dose. Blood counts must be monitored weekly for at least 6 weeks after each dose.
  • Cumulative myelosuppression is common, requiring careful dose adjustments based on nadir counts from the previous cycle.
  • Pulmonary toxicity, including fatal pulmonary fibrosis, is a serious and delayed complication. Patients should be monitored for respiratory symptoms.
  • Lomustine is highly lipophilic and readily crosses the blood-brain barrier, making it useful for brain tumors.
  • Administer on an empty stomach to minimize nausea and vomiting, though antiemetics are often required.
  • Capsules should be swallowed whole; do not chew or open.
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Alternative Therapies

  • Carmustine (another nitrosourea)
  • Temozolomide (for brain tumors)
  • Procarbazine (part of MOPP/ABVD for Hodgkin's)
  • Other alkylating agents (e.g., cyclophosphamide, ifosfamide)
  • Radiation therapy (for brain tumors, Hodgkin's lymphoma)
  • Other chemotherapy regimens depending on specific cancer type and stage
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Cost & Coverage

Average Cost: Highly variable, typically several thousand USD per 100mg capsule
Generic Available: Yes
Insurance Coverage: Specialty Tier (requires prior authorization, often subject to high co-pays or co-insurance)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to ensure you receive the best possible care.