Rasuvo 7.5mg/0.15ml Pf Inj, 4 Pens
WARNING: Severe side effects like bone marrow problems, liver problems, lung problems, and infections can happen with this drug. Some side effects may not go away and can be deadly. You must talk with the doctor about the risks of this drug. This drug may cause kidney problems in some patients. Talk with the doctor.Regular blood work and other exams will need to be done to check for side effects. Follow what the doctor has told you. Tell your doctor if you have kidney problems or extra fluid around your stomach area or lungs. The chance of side effects may be raised.Talk with your doctor if you are getting radiation. There may be more chance of harm to tissue and bone.New types of cancer have happened in people taking this drug. If you have questions, talk with the doctor.It is common to have diarrhea, upset stomach, throwing up, or mouth sores with this drug. However, sometimes these may be signs of severe and sometimes deadly stomach or bowel problems. Tell your doctor if you get any new or worsening signs. You may need to stop this drug.Severe skin reactions have happened with this drug. These have included Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other severe skin reactions. Sometimes these have been deadly. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin; other skin irritation (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.Very bad and sometimes deadly bone marrow problems and stomach or bowel problems have happened when this drug was taken with nonsteroidal anti-inflammatory drug (NSAIDs) like ibuprofen or naproxen.Not all methotrexate products are used to treat cancer. Talk with the doctor.This drug may cause harm to an unborn baby or loss of an unborn baby. A pregnancy test will be done before you start this drug to show that you are NOT pregnant.If you or your sex partner may become pregnant, you must use birth control while taking this drug and for some time after the last dose. Ask your doctor how long to use birth control. If you or your sex partner gets pregnant, call your doctor right away.Do not take if you are pregnant.This drug must only be used when other drugs cannot be used or have not worked. Talk with your doctor to be sure that the benefits of this drug are more than the risks. @ COMMON USES: It is used to treat some types of arthritis.It is used to treat some types of psoriasis.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antimetabolite, Disease-Modifying Antirheumatic Drug (DMARD), Antineoplastic
Pharmacologic Class
Folic acid antagonist, Immunosuppressant
Pregnancy Category
Category X
FDA Approved
Jul 2013
DEA Schedule
Not Controlled
Overview
What is this medicine?
Rasuvo is a medication used to treat severe rheumatoid arthritis and psoriasis. It works by reducing inflammation and slowing down the overactive immune system that causes these conditions. It is given as a shot under the skin, usually once a week.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered via injection into the fatty tissue of the skin, typically on the top of the thigh or in the belly area. If you will be self-administering the injection, your doctor or nurse will provide guidance on the proper technique.
Important Administration Guidelines
Do not inject the medication within 2 inches (5 cm) of the belly button.
Check the solution for cloudiness, leakage, or particles before use. If any of these conditions are present, do not use the medication.
Avoid injecting into skin that is irritated, tender, bruised, red, scaly, hard, scarred, or has stretch marks.
If you are unsure whether a dose was injected correctly or experience difficulty administering the dose, consult your doctor or pharmacist before proceeding with another dose.
Safe Disposal of Needles and Supplies
Dispose of used needles in a designated needle/sharp disposal box.
Do not reuse needles or other items.
When the disposal box is full, follow local regulations for proper disposal.
If you have any questions or concerns, consult your doctor or pharmacist.
Dosing and Frequency
Your dosage and frequency of administration will be determined by your doctor based on the specific health condition being treated.
Important: This medication should never be taken daily unless prescribed for certain types of cancer. Incorrect use of this medication can lead to serious errors. Ensure you understand your dosage and administration schedule. If you are unsure, consult your doctor.
Your doctor may adjust the dosage and administration schedule based on blood work results, side effects, and the medication's effectiveness.
Handling and Storage
Handle this medication with care. Consult your doctor or pharmacist for guidance on proper handling procedures.
Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit fluid intake.
Storage and Disposal
Store the medication at room temperature, protected from light and moisture. Do not store in a bathroom.
Missed Dose
* If you miss a dose, contact your doctor for guidance on what to do next.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered via injection into the fatty tissue of the skin, typically on the top of the thigh or in the belly area. If you will be self-administering the injection, your doctor or nurse will provide guidance on the proper technique.
Important Administration Guidelines
Do not inject the medication within 2 inches (5 cm) of the belly button.
Check the solution for cloudiness, leakage, or particles before use. If any of these conditions are present, do not use the medication.
Avoid injecting into skin that is irritated, tender, bruised, red, scaly, hard, scarred, or has stretch marks.
If you are unsure whether a dose was injected correctly or experience difficulty administering the dose, consult your doctor or pharmacist before proceeding with another dose.
Safe Disposal of Needles and Supplies
Dispose of used needles in a designated needle/sharp disposal box.
Do not reuse needles or other items.
When the disposal box is full, follow local regulations for proper disposal.
If you have any questions or concerns, consult your doctor or pharmacist.
Dosing and Frequency
Your dosage and frequency of administration will be determined by your doctor based on the specific health condition being treated.
Important: This medication should never be taken daily unless prescribed for certain types of cancer. Incorrect use of this medication can lead to serious errors. Ensure you understand your dosage and administration schedule. If you are unsure, consult your doctor.
Your doctor may adjust the dosage and administration schedule based on blood work results, side effects, and the medication's effectiveness.
Handling and Storage
Handle this medication with care. Consult your doctor or pharmacist for guidance on proper handling procedures.
Drink plenty of non-caffeinated liquids, unless your doctor advises you to limit fluid intake.
Storage and Disposal
Store the medication at room temperature, protected from light and moisture. Do not store in a bathroom.
Missed Dose
* If you miss a dose, contact your doctor for guidance on what to do next.
Lifestyle & Tips
- Take exactly as prescribed, usually once a week. Never take daily for arthritis or psoriasis, as this can be fatal.
- Take folic acid supplementation as directed by your doctor to reduce side effects.
- Avoid alcohol consumption, as it can increase the risk of liver damage.
- Avoid prolonged sun exposure and use sunscreen, as methotrexate can increase sun sensitivity.
- Stay well-hydrated, especially during treatment.
- Report any signs of infection (fever, chills, sore throat) immediately.
- Avoid live vaccines while on methotrexate.
- Use effective contraception during treatment and for at least 6 months after stopping for both men and women, due to severe birth defect risk.
Available Forms & Alternatives
Available Strengths:
- Rasuvo 10mg/0.2ml Pf Inj, 4 Pens
- Rasuvo 12.5mg/0.25ml Pf Inj, 4 Pens
- Rasuvo 22.5mg/0.45ml Pf Inj, 4 Pens
- Rasuvo 25mg/0.5ml Pf Inj, 4 Pens
- Rasuvo 15mg/0.3ml Pf Inj, 4 Pens
- Rasuvo 17.5mg/0.35ml Pf Inj, 4 Pens
- Rasuvo 20mg/0.4ml Pf Inj, 4 Pens
- Rasuvo 30mg/0.6ml Pf Inj, 4 Pens
- Rasuvo 7.5mg/0.15ml Pf Inj, 4 Pens
- Rasuvo 15mg Inj, 0.3ml
- Rasuvo 17.5mg Inj, 0.35ml
- Rasuvo 20mg Inj, 0.4ml
- Rasuvo 7.5mg Inj, 0.15ml
Dosing & Administration
Adult Dosing
Standard Dose:
For Rheumatoid Arthritis (RA) and Psoriasis: 7.5 mg once weekly, administered subcutaneously. Dose may be gradually increased to a maximum of 20 mg once weekly.
Dose Range:
7.5 - 20 mg
Condition-Specific Dosing:
Rheumatoid Arthritis:
7.5 mg once weekly, adjusted to response and tolerability, up to 20 mg once weekly.
Psoriasis:
7.5 mg once weekly, adjusted to response and tolerability, up to 20 mg once weekly.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For Polyarticular Juvenile Idiopathic Arthritis (pJIA): 10 mg/m² once weekly, administered subcutaneously. Doses typically range from 0.4 to 0.6 mg/kg/week (max 25 mg/week).
Adolescent:
For Polyarticular Juvenile Idiopathic Arthritis (pJIA): 10 mg/m² once weekly, administered subcutaneously. Doses typically range from 0.4 to 0.6 mg/kg/week (max 25 mg/week).
Dose Adjustments
Renal Impairment:
Mild:
CrCl 51-80 mL/min: Consider 25-50% dose reduction or increased dosing interval. Monitor closely.
Moderate:
CrCl 10-50 mL/min: Consider 50-75% dose reduction or increased dosing interval. Avoid if possible.
Severe:
CrCl <10 mL/min: Contraindicated.
Dialysis:
Methotrexate is dialyzable, but standard weekly dosing for RA/psoriasis is generally contraindicated due to prolonged exposure and toxicity risk. Consult specialist.
Hepatic Impairment:
Mild:
Use with caution. Monitor liver function tests closely.
Moderate:
Significant liver disease (e.g., cirrhosis, fibrosis): Contraindicated.
Severe:
Significant liver disease (e.g., cirrhosis, fibrosis): Contraindicated.
Pharmacology
Mechanism of Action
Methotrexate is an antimetabolite that inhibits dihydrofolate reductase (DHFR), an enzyme essential for DNA synthesis, repair, and cellular replication. By inhibiting DHFR, methotrexate prevents the reduction of dihydrofolate to tetrahydrofolate, a critical cofactor for purine and pyrimidine synthesis. In rheumatologic and dermatologic conditions, its mechanism is thought to involve immunosuppressive and anti-inflammatory effects, possibly through inhibition of lymphocyte proliferation, induction of adenosine release, and effects on cytokine production.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80-94% (subcutaneous)
Tmax:
1-2 hours (subcutaneous)
FoodEffect:
Not significantly affected by food when administered subcutaneously.
Distribution:
Vd:
0.4-0.8 L/kg (initial), 0.2-0.3 L/kg (steady state)
ProteinBinding:
Approximately 50% (primarily to albumin)
CnssPenetration:
Limited at typical low doses; significant penetration at high doses (e.g., oncology) or in presence of inflammation.
Elimination:
HalfLife:
3-10 hours (low dose, non-oncologic); can be prolonged in renal impairment or with high doses.
Clearance:
Primarily renal (glomerular filtration and active tubular secretion).
ExcretionRoute:
Renal (approximately 80-90% unchanged), small amount via bile.
Unchanged:
80-90%
Pharmacodynamics
OnsetOfAction:
For RA/Psoriasis: 3-6 weeks, with full effect potentially taking 3-6 months.
PeakEffect:
For RA/Psoriasis: 3-6 months.
DurationOfAction:
Effects persist as long as treatment is continued; cessation leads to gradual loss of effect.
Safety & Warnings
BLACK BOX WARNING
Methotrexate has been associated with severe toxic reactions, including death. Patients should be closely monitored for bone marrow, liver, lung, and kidney toxicities. Methotrexate can cause: 1) Bone marrow suppression (myelosuppression), 2) Liver damage (hepatotoxicity), 3) Lung disease (pneumonitis), 4) Kidney damage (renal toxicity), 5) Gastrointestinal toxicity (e.g., mucositis, diarrhea), 6) Opportunistic infections, 7) Tumor lysis syndrome, 8) Severe dermatologic reactions, 9) Secondary malignancy (lymphoma). Methotrexate is teratogenic and abortifacient; it is contraindicated in pregnant women with non-oncologic diseases. Concomitant use with NSAIDs may increase methotrexate toxicity. Administer once weekly for non-oncologic indications; daily administration can be fatal.
Side Effects
Urgent 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 immediately or seek emergency medical attention:
Allergic Reaction: Rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infection: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or discolored sputum, painful urination, mouth sores, or a wound that won't heal.
Bleeding: 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 enlarge, or uncontrollable bleeding.
Pancreatitis: Severe stomach pain, severe back pain, or severe nausea and vomiting.
Kidney Problems: Inability to urinate, changes in urine output, blood in the urine, or sudden weight gain.
Liver Problems: Dark urine, fatigue, decreased appetite, nausea or stomach pain, light-colored stools, vomiting, or yellow skin and eyes.
Lung or Breathing Problems: Shortness of breath, difficulty breathing, cough, or fever.
Nerve Problems: Abnormal burning, numbness, or tingling sensations; weakness; or paralysis (inability to move a body part).
Other Serious Symptoms: Pinpoint red spots on the skin, severe dizziness or fainting, seizures, confusion, excessive sleepiness, changes in vision, bone pain, swelling, warmth, numbness, color changes, or pain in a leg or arm, weakness on one side of the body, speech or thinking difficulties, balance problems, drooping on one side of the face, or blurred vision.
Additional Serious Symptoms: Headache, neck stiffness.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you're bothered by any of the following side effects or if they persist, contact your doctor:
Decreased appetite
Hair loss
Dizziness, tiredness, or weakness
Stomach pain
* Common cold symptoms
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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 immediately or seek emergency medical attention:
Allergic Reaction: Rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infection: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or discolored sputum, painful urination, mouth sores, or a wound that won't heal.
Bleeding: 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 enlarge, or uncontrollable bleeding.
Pancreatitis: Severe stomach pain, severe back pain, or severe nausea and vomiting.
Kidney Problems: Inability to urinate, changes in urine output, blood in the urine, or sudden weight gain.
Liver Problems: Dark urine, fatigue, decreased appetite, nausea or stomach pain, light-colored stools, vomiting, or yellow skin and eyes.
Lung or Breathing Problems: Shortness of breath, difficulty breathing, cough, or fever.
Nerve Problems: Abnormal burning, numbness, or tingling sensations; weakness; or paralysis (inability to move a body part).
Other Serious Symptoms: Pinpoint red spots on the skin, severe dizziness or fainting, seizures, confusion, excessive sleepiness, changes in vision, bone pain, swelling, warmth, numbness, color changes, or pain in a leg or arm, weakness on one side of the body, speech or thinking difficulties, balance problems, drooping on one side of the face, or blurred vision.
Additional Serious Symptoms: Headache, neck stiffness.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you're bothered by any of the following side effects or if they persist, contact your doctor:
Decreased appetite
Hair loss
Dizziness, tiredness, or weakness
Stomach pain
* Common cold symptoms
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Unusual bleeding or bruising
- Severe fatigue or weakness
- Fever, chills, or signs of infection
- Persistent cough, shortness of breath, or difficulty breathing
- Yellowing of skin or eyes (jaundice)
- Dark urine
- Severe nausea, vomiting, or diarrhea
- Sores in the mouth or throat
- Severe skin rash, redness, or peeling
- Swelling in the legs or ankles
- Severe abdominal pain
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.
Certain health conditions, including:
+ Alcohol use disorder
+ Bone marrow disease, such as low white blood cell count, low platelet count, or anemia
+ Kidney disease
+ Liver disease
+ A weakened immune system
If you are breast-feeding, please note that you should not breast-feed while taking this medication. Additionally, you may need to avoid breast-feeding for a period after your last dose. Consult your doctor to determine the necessary duration of breast-feeding avoidance after completing the medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. This will help ensure your safety while taking this medication. Do not initiate, stop, or modify the dosage of any medication without first consulting 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.
Certain health conditions, including:
+ Alcohol use disorder
+ Bone marrow disease, such as low white blood cell count, low platelet count, or anemia
+ Kidney disease
+ Liver disease
+ A weakened immune system
If you are breast-feeding, please note that you should not breast-feed while taking this medication. Additionally, you may need to avoid breast-feeding for a period after your last dose. Consult your doctor to determine the necessary duration of breast-feeding avoidance after completing the medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. This will help ensure your safety while taking this medication. Do not initiate, stop, or modify the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in activities that require alertness, wait until you understand how this drug affects you. Be aware that you may have a higher risk of developing an infection. To minimize this risk, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
Due to the potential for increased bleeding, exercise caution to prevent injuries. Use a soft-bristled toothbrush and an electric razor for shaving.
Consult your doctor before receiving any vaccinations, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication. Additionally, discuss the consumption of alcohol with your doctor.
You may be more susceptible to sunburn; therefore, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use protective measures such as sunscreen, clothing, and eyewear to shield yourself from the sun. Continue to protect yourself from sunburn for the duration recommended by your doctor.
Notify your doctor if you experience excessive fluid loss, unusual sweating, vomiting, diarrhea, decreased appetite, or abnormal thirst. Be aware that this medication can cause severe nervous system problems, which may be temporary or long-lasting and potentially life-threatening. If you have concerns, discuss them with your doctor.
If you have undergone radiation therapy, inform your doctor. Elderly patients (65 years and older) should use this medication with caution, as they may be more prone to side effects.
This drug may affect fertility, potentially leading to infertility. It is unclear whether fertility will return to normal if this occurs. If you miss a menstrual period, have unprotected sex, or suspect that your birth control has failed, contact your doctor immediately.
Before operating a vehicle or engaging in activities that require alertness, wait until you understand how this drug affects you. Be aware that you may have a higher risk of developing an infection. To minimize this risk, practice good hygiene by washing your hands frequently and avoid close contact with individuals who have infections, colds, or flu.
Due to the potential for increased bleeding, exercise caution to prevent injuries. Use a soft-bristled toothbrush and an electric razor for shaving.
Consult your doctor before receiving any vaccinations, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication. Additionally, discuss the consumption of alcohol with your doctor.
You may be more susceptible to sunburn; therefore, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use protective measures such as sunscreen, clothing, and eyewear to shield yourself from the sun. Continue to protect yourself from sunburn for the duration recommended by your doctor.
Notify your doctor if you experience excessive fluid loss, unusual sweating, vomiting, diarrhea, decreased appetite, or abnormal thirst. Be aware that this medication can cause severe nervous system problems, which may be temporary or long-lasting and potentially life-threatening. If you have concerns, discuss them with your doctor.
If you have undergone radiation therapy, inform your doctor. Elderly patients (65 years and older) should use this medication with caution, as they may be more prone to side effects.
This drug may affect fertility, potentially leading to infertility. It is unclear whether fertility will return to normal if this occurs. If you miss a menstrual period, have unprotected sex, or suspect that your birth control has failed, contact your doctor immediately.
Overdose Information
Overdose Symptoms:
- Severe bone marrow suppression (e.g., severe leukopenia, thrombocytopenia, anemia)
- Severe mucositis (mouth sores, gastrointestinal ulceration)
- Hepatotoxicity
- Renal failure
What to Do:
Immediately contact emergency services or a poison control center (1-800-222-1222). Leucovorin rescue is the primary antidote, administered as soon as possible. Hydration and urinary alkalinization may also be used to enhance methotrexate excretion.
Drug Interactions
Contraindicated Interactions
- Live vaccines (during methotrexate therapy)
- Trimethoprim/sulfamethoxazole (increased myelosuppression)
- Probenecid (decreased renal excretion of methotrexate)
- Salicylates (high dose, increased methotrexate levels)
- Non-steroidal anti-inflammatory drugs (NSAIDs) in high-dose methotrexate regimens (can increase methotrexate levels and toxicity); caution with low-dose methotrexate.
Major Interactions
- NSAIDs (especially with high-dose methotrexate, but caution with low-dose due to potential for increased methotrexate levels and toxicity)
- Proton pump inhibitors (PPIs) (e.g., omeprazole, pantoprazole) (may increase methotrexate levels, particularly at high doses, but also reported with low doses)
- Penicillins (e.g., amoxicillin, penicillin G) (may decrease renal clearance of methotrexate)
- Ciprofloxacin (may decrease renal clearance of methotrexate)
- Folic acid antagonists (e.g., pyrimethamine, trimethoprim) (additive antifolate effects, increased toxicity)
- Hepatotoxic agents (e.g., azathioprine, retinoids, sulfasalazine, alcohol) (increased risk of hepatotoxicity)
- Nephrotoxic agents (e.g., aminoglycosides, cisplatin) (increased risk of renal toxicity, impaired methotrexate excretion)
- Phenytoin (decreased phenytoin levels, increased methotrexate toxicity)
- Theophylline (decreased theophylline clearance)
- Nitrous oxide (functional folate deficiency, increased myelosuppression)
Moderate Interactions
- Oral antibiotics (e.g., tetracyclines, chloramphenicol) (may alter gut flora, affecting methotrexate absorption/enterohepatic recirculation)
- Sulfonylureas (may increase hypoglycemic effect)
- Digoxin (decreased digoxin absorption)
- Colchicine (increased risk of myelosuppression)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential and platelets
Rationale: To establish baseline hematologic parameters and detect pre-existing cytopenias.
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs) including AST, ALT, albumin, bilirubin
Rationale: To establish baseline liver function and detect pre-existing hepatic impairment.
Timing: Prior to initiation of therapy.
Renal Function Tests (serum creatinine, BUN, eGFR)
Rationale: To establish baseline renal function, as methotrexate is primarily renally cleared.
Timing: Prior to initiation of therapy.
Chest X-ray (CXR)
Rationale: To establish baseline pulmonary status and rule out pre-existing interstitial lung disease.
Timing: Prior to initiation of therapy.
Hepatitis B and C serology
Rationale: To screen for chronic viral hepatitis, which can increase risk of hepatotoxicity.
Timing: Prior to initiation of therapy.
Routine Monitoring
Complete Blood Count (CBC) with differential and platelets
Frequency: Every 2-4 weeks for the first 3 months, then every 1-2 months.
Target: Within normal limits; monitor for significant drops in cell counts.
Action Threshold: Hold methotrexate if WBC <3,000/mm³, ANC <1,500/mm³, or platelets <100,000/mm³.
Liver Function Tests (AST, ALT, albumin)
Frequency: Every 2-4 weeks for the first 3 months, then every 1-2 months.
Target: Within normal limits or stable.
Action Threshold: Hold methotrexate if AST/ALT persistently >2-3 times ULN; consider liver biopsy if persistent elevation or cumulative dose concerns.
Renal Function Tests (serum creatinine, eGFR)
Frequency: Every 2-4 weeks for the first 3 months, then every 1-2 months.
Target: Within normal limits or stable.
Action Threshold: Hold or reduce dose if creatinine increases significantly or eGFR decreases.
Symptom Monitoring
- Unusual bleeding or bruising (signs of myelosuppression)
- Fever, chills, sore throat (signs of infection/myelosuppression)
- Persistent cough, shortness of breath, dyspnea (signs of pulmonary toxicity/pneumonitis)
- Yellowing of skin or eyes, dark urine, severe fatigue (signs of hepatotoxicity)
- Severe nausea, vomiting, diarrhea, oral sores/ulcers (signs of gastrointestinal toxicity/mucositis)
- Severe skin rash or peeling (signs of severe dermatologic reactions)
- Unusual lumps or swelling (lymphoma risk)
Special Patient Groups
Pregnancy
Contraindicated in pregnant women with non-oncologic diseases due to significant risk of fetal death and severe birth defects (teratogenic and abortifacient).
Trimester-Specific Risks:
First Trimester:
High risk of major congenital malformations (e.g., craniofacial, cardiovascular, limb abnormalities) and fetal death.
Second Trimester:
Risk of fetal death and growth restriction.
Third Trimester:
Risk of fetal death and growth restriction.
Lactation
Contraindicated during breastfeeding. Methotrexate is excreted into breast milk and can cause serious adverse reactions in a breastfed infant, including myelosuppression.
Infant Risk:
High risk (L5 - Contraindicated)
Pediatric Use
Used in pediatric patients for polyarticular juvenile idiopathic arthritis (pJIA) and certain oncologic indications. Dosing is weight or body surface area-based. Close monitoring for toxicity is essential, similar to adults.
Geriatric Use
Use with caution in elderly patients due to increased likelihood of decreased renal and hepatic function, and potential for concomitant diseases or other drug therapies. Dose adjustments may be necessary based on renal function. Increased susceptibility to toxicity.
Clinical Information
Clinical Pearls
- Emphasize weekly dosing for non-oncologic indications; daily dosing can be fatal.
- Folic acid supplementation (typically 1-5 mg/week, not on the same day as methotrexate) is crucial to reduce common side effects like mucositis, nausea, and liver enzyme elevations.
- Patients must be educated on the importance of regular laboratory monitoring (CBC, LFTs, renal function) and to report any new or worsening symptoms promptly.
- Avoid alcohol completely due to increased risk of hepatotoxicity.
- Ensure patients understand proper subcutaneous injection technique and needle disposal.
- Counsel on contraception for both male and female patients due to teratogenicity.
Alternative Therapies
- Other conventional synthetic DMARDs (csDMARDs): Hydroxychloroquine, Sulfasalazine, Leflunomide.
- Biologic DMARDs (bDMARDs): TNF inhibitors (e.g., Adalimumab, Etanercept, Infliximab), IL-6 inhibitors (e.g., Tocilizumab), T-cell costimulation modulators (e.g., Abatacept), B-cell depleting agents (e.g., Rituximab).
- Targeted Synthetic DMARDs (tsDMARDs): JAK inhibitors (e.g., Tofacitinib, Baricitinib, Upadacitinib).
- For Psoriasis: Other systemic agents (e.g., Cyclosporine, Acitretin), Biologics, Phototherapy.
Cost & Coverage
Average Cost:
Varies widely by pharmacy and insurance plan per 4 pens
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Specialty drug, may require prior authorization)
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 reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.