Cytarabine – Uses, Dosage, Side Effects, Interactions

Last updated: February 8, 2026Reviewed date: February 8, 2026Reading time: 56 min read
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Cytarabine is a cytosine analogue and antineoplastic agent used largely in the therapy of acute leukemia. Cytarabine is associated with a low rate of transient serum enzyme and bilirubin elevations during therapy, but has only rarely been implicated in cases of clinically apparent acute liver injury with jaundice....

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Article Summary

Cytarabine is a cytosine analogue and antineoplastic agent used largely in the therapy of acute leukemia. Cytarabine is associated with a low rate of transient serum enzyme and bilirubin elevations during therapy, but has only rarely been implicated in cases of clinically apparent acute liver injury with jaundice. Cytarabine is an antimetabolite analogue of cytidine with a modified sugar moiety (arabinose instead of ribose). Cytarabine is converted to the triphosphate form within the cell...

Key Takeaways

  • This article explains Mechanism of Action in simple medical language.
  • This article explains Indications in simple medical language.
  • This article explains Contraindications in simple medical language.
  • This article explains Dosage in simple medical language.
Educational health guideWritten for patient understanding and clinical awareness.
Reviewed content workflowUse writer and reviewer profiles for stronger trust.
Emergency safety firstUrgent warning signs are highlighted below.

Seek urgent medical care if you notice

These warning signs are general safety guidance. Local emergency numbers and clinical judgment should always come first.

  • Severe symptoms, breathing difficulty, fainting, confusion, or rapidly worsening illness.
  • New weakness, severe pain, high fever, or symptoms after a serious injury.
  • Any symptom that feels urgent, unusual, or unsafe for the patient.
1

Emergency now

Use emergency care for severe, sudden, rapidly worsening, or life-threatening symptoms.

2

See a doctor

Book a professional medical evaluation if symptoms persist, worsen, recur often, affect daily activities, or occur in a high-risk patient.

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Learn safely

Use this article to understand possible causes, tests, treatment options, prevention, and questions to ask your clinician.

Cytarabine is a cytosine analogue and antineoplastic agent used largely in the therapy of acute leukemia. Cytarabine is associated with a low rate of transient serum enzyme and bilirubin elevations during therapy, but has only rarely been implicated in cases of clinically apparent acute liver injury with jaundice.

Cytarabine is an antimetabolite analogue of cytidine with a modified sugar moiety (arabinose instead of ribose). Cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. This agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. (NCI04)

Cytarabine is a pyrimidine nucleoside in which cytosine is attached to D-arabinofuranose via a beta-N(1)-glycosidic bond. Used mainly in the treatment of leukaemia, especially acute non-lymphoblastic leukaemia, cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. It also has antiviral and immunosuppressant properties. It has a role as an antineoplastic agent, an antimetabolite, an antiviral agent and an immunosuppressive agent. It is a beta-D-arabinoside, a pyrimidine nucleoside and a monosaccharide derivative. It is functionally related to a cytosine.

Mechanism of Action

Cytarabine acts through direct DNA damage and incorporation into DNA. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture. It exhibits cell phase specificity, primarily killing cells undergoing DNA synthesis (S-phase) and under certain conditions blocking the progression of cells from the G1 phase to the S-phase. Although the mechanism of action is not completely understood, it appears that cytarabine acts through the inhibition of DNA polymerase. A limited, but significant, incorporation of cytarabine into both DNA and RNA has also been reported.

Cytarabine is converted intracellularly to the nucleotide, cytarabine triphosphate (ara-CTP, cytosine arabinoside triphosphate). Although the exact mechanism(s) of action of cytarabine has not been fully elucidated, cytarabine triphosphate appears to inhibit DNA polymerase by competing with the physiologic substrate, deoxycytidine triphosphate, resulting in the inhibition of DNA synthesis. Although limited, incorporation of cytarabine triphosphate into DNA and RNA may also contribute to the cytotoxic effects of the drug.

Cytarabine liposome injection is a sustained-release formulation of the active ingredient cytarabine designed for direct administration into the cerebrospinal fluid (CSF). Cytarabine is a cell cycle phase-specific antineoplastic agent, affecting cells only during the S-phase of cell division. Intracellularly, cytarabine is converted into cytarabine-5′-triphosphate (ara-CTP), which is the active metabolite. The mechanism of action is not completely understood, but it appears that ara-CTP acts primarily through inhibition of DNA polymerase. Incorporation into DNA and RNA may also contribute to cytarabine cytotoxicity. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture.

Indications

  • Cytarabine is a medication used in the management and treatment of leukemias and lymphomas.It belongs to the antimetabolic group of medications. This activity reviews the indications, action, and contraindications for cytarabine as a valuable agent in treating acute myeloid leukemia (and other leukemias)
  • For the treatment of acute non-lymphocytic leukemia, acute lymphocytic leukemia and blast phase of chronic myelocytic leukemia. Cytarabine is indicated in combination with [daunorubicin] for the treatment of newly-diagnosed therapy-related acute myeloid leukemia (t-AML) or AML with myelodysplasia-related changes (AML-MRC) in adults and pediatric patients 1 year and older.
  • Intrathecal treatment of lymphomatous meningitis. In the majority of patients such treatment will be part of symptomatic palliation of the disease.
  • Antimetabolites, Antineoplastic; Antiviral Agents; Immunosuppressive Agents; Teratogens
  • DepoCyt (cytarabine liposome injection) is indicated for the intrathecal treatment of lymphomatous meningitis. This indication is based on demonstration of increased complete response rate compared to unencapsulated cytarabine. There are no controlled trials that demonstrate a clinical benefit resulting from this treatment, such as improvement in disease-related symptoms, or increased time to disease progression, or increased survival.
  • Cytarabine is indicated, in combination with other antineoplastic agents, for treatment of acute nonlymphocytic leukemia in adults and children.
  • Cytarabine is indicated for treatment of acute lymphocytic leukemia and chronic myelocytic leukemia (blast phase).
  • Agents used in the prophylaxis or therapy of VIRUS DISEASES. Some of the ways they may act include preventing viral replication by inhibiting viral DNA polymerase; binding to specific cell-surface receptors and inhibiting viral penetration or uncoating; inhibiting viral protein synthesis; or blocking late stages of virus assembly.
  • Antimetabolites that are useful in cancer chemotherapy.
  • Acute Lymphoblastic Leukemia (ALL)
  • Acute Myeloid Leukemia (AML)
  • Acute Myeloid Leukemia With Myelodysplasia-Related Changes
  • Acute Promyelocytic Leukemia (APL)
  • Meningeal leukemia
  • Metastatic Malignant Neoplasm to the Leptomeninges
  • Non-Hodgkin’s Lymphoma (NHL)
  • Therapy-Related Acute Myeloid Leukemia
  • Blast phase Chronic myelocytic leukemia

Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging.

Use in Cancer

Cytarabine is approved to be used with other drugs to treat:

  • Acute non-lymphocytic leukemia in adults and children.

Cytarabine is also approved to prevent and treat:

  • Meningeal leukemia (leukemia that has spread to the meninges). It is given as intrathecal therapy.

Cytarabine may also be used to treat:

  • Acute lymphoblastic leukemia (ALL).
  • Chronic myelogenous leukemia (CML) in the blastic phase.

Cytarabine is also being studied in the treatment of other types of cancer.

Cytarabine is also available in a different form, combined with Daunorubicin Hydrochloride

Contraindications

  • Cytarabine is contraindicated in patients who have had a hypersensitivity reaction to it or any of the fundamental ingredients used in the preparation of the drug. With active meningeal infections, liposomal cytarabine is also contraindicated.

Dosage

Dosage Forms

  • Solution, Injection: 10 mg/ml, 20 mg/mL (25 mL), 100 mg/ml
  • Intrathecal injection, liposomal: 50 mg/5ml

Administration – Rapid intravenous infusion, infuse over 1 to 3 hours intravenously or subcutaneously or intrathecally.

Storage – Store at room temperature.

Dosing: Adult

  1. Acute lymphoblastic leukemia (off-label dosing):

    • Induction regimen, relapsed or refractory- Administer 3,000 mg/sq.meter of cytarabine over 3 hours by intravenous infusion daily for five days in combination with idarubicin for three days.
    • Dose-intensive regimen- 3,000 mg/sq.meter of cytarabine over 2 hours by intravenous infusion. This dose is to be given every 12 hours on days 2 and 3 (4 doses/cycle) of even-numbered cycles in combination with methotrexate.
  2. Acute myeloid leukemia (remission induction chemotherapy):

    • Administer standard dose 100 mg/sq.meter/day of cytarabine by continuous intravenous infusion for 7 days or give 200 mg/sq.meter/day by continuous intravenous infusion for 7 days(as 100 mg/m2 over 12 hours every 12 hours).
  3. Acute myeloid leukemia consolidation therapy (off-label use):

    • 5+2 regimen: Administer 100 mg/sq.meter/day of cytarabine for five days by intravenous infusion in combination with daunorubicin or idarubicin, or mitoxantrone.
  4. Acute myeloid leukemia salvage treatment (off-label use):

    • CLAG-M regimen: Administer 2,000 mg/sq.meter/day of cytarabine by intravenous infusion over 4 hours for five days in combination with cladribine, G-CSF, and mitoxantrone.
  5. Acute promyelocytic leukemia consolidation therapy (off-label use):

    • First consolidation course: Administer 200 mg/sq.meter/day of cytarabine by intravenous infusion for seven days in combination with daunorubicin.
    • Second consolidation course:

      • If age is ≤60 years and low risk (WBC <10,000/cubic mm), then administer 1,000 mg/sq.meter of cytarabine every 12 hours for four days (8 doses) by intravenous infusion.
      • If age is <50 years and high risk (WBC ≥10,000/cubic mm), then administer 2,000 mg/sq.meter of cytarabine every 12 hours for five days (10 doses) by intravenous infusion.
      • If age is 50 to 60 years and high risk (WBC ≥10,000/cubic mm), then administer 1500 mg/sq.meter of cytarabine every 12 hours for five days (10 doses) by intravenous infusion.
      • If age is >60 years and high risk (WBC ≥10,000/cubic mm) then administer 1,000 mg/sq.meter every 12 hours for four days (8 doses) by intravenous infusion.
  6. Acute promyelocytic leukemia induction (off-label dosing):

    • Administer 200 mg/sq.meter/day of cytarabine by continuous intravenous infusion for seven days, beginning on the third day of treatment in combination with tretinoin and daunorubicin.

Usual Adult Dose for

Acute Nonlymphocytic Leukemia

Induction as part of combination chemotherapy:

  • 100 mg/m2/day by continuous IV infusion (Days 1 through 7) or 100 mg/m2 IV every 12 hours (Days 1 through 7)

Meningeal Leukemia

  • The dose ranges from 5 mg/m2 to 75 mg/m2 intrathecally once a day for 4 days to once every 4 days (30 mg/m2 every 4 days until cerebrospinal fluid findings are normal, followed by one additional treatment is the most frequently used dose)

Usual Pediatric Dose for

Acute Nonlymphocytic Leukemia

Induction as part of combination chemotherapy:

  • 100 mg/m2/day by continuous IV infusion (Days 1 through 7) or 100 mg/m2 IV every 12 hours (Days 1 through 7)

Acute Lymphocytic Leukemia

  • The literature and/or local protocol should be consulted.

Meningeal Leukemia

  • The dose ranges from 5 mg/m2 to 75 mg/m2 intrathecally once a day for 4 days to once every 4 days (30 mg/m2 every 4 days until cerebrospinal fluid findings are normal, followed by one additional treatment is the most frequently used dose)

Side Effects

The Most Common

  • ongoing pain that begins in the stomach area but may spread to the back
  • redness, pain, swelling, or burning at the site where the injection was given
  • nausea
  • vomiting
  • diarrhea
  • stomach pain
  • loss of appetite
  • sores in the mouth and throat
  • hair loss
  • muscle or joint pain
  • tiredness
  • sore or red eyes

More Common

  • pale skin
  • fainting
  • dizziness
  • fast or irregular heartbeat
  • rash
  • hives
  • itching
  • difficulty breathing or swallowing
  • chest pain
  • yellowing of the skin or eyes
  • dark-colored urine or decreased urination
  • shortness of breath
  • sudden change or loss of vision
  • seizures
  • confusion
  • numbness, burning, or tingling in the hands, arms, feet, or legs

Rare

  • Headache
  • Low blood counts. Your white and red blood cells and platelets may temporarily decrease. This can put you at risk for infection, anemia and/or bleeding. Nadir: White blood cells: 7-10 days, platelets: 12-15 days.
  • Nausea and vomiting
  • Mouth sores (usually occur 7-10 days after therapy).
  • Increases in blood tests measuring liver function. These return to normal once treatment is discontinued. More often associated with high-dose regimens.
  • Diarrhea
  • Loss of appetite
  • Skin rash, redness and itching
  • Flu-like symptoms (fever, chills, generalized aches and pains) within the first few days of treatment.
  • Pain, redness and skin peeling of the palms of hands and soles of feet (hand-foot syndrome) may occur with high-dose therapy (rare). Use of steroid creams or moisturizers may be helpful.
  • Blood test abnormalities: Increase in blood level of uric acid. A medication called allopurinal may be given to decrease these levels.
  • Temporary hair loss (uncommon, but thinning may occur).
  • Eye pain, tearing, sensitivity to light and blurred vision may occur with high-dose therapy. Often steroid drops or ointment to the eyes are used to prevent or relieve this condition.
  • Dizziness, headache, excessive sleepiness, confusion, loss of balance may occur in up to 10% of patients receiving high dose therapy. Onset is usually 5 days after treatment and may last up to 1 week. More often these toxicities are mild and reversible.

Drug interactions

Pregnancy and Lactation

What special precautions should I follow?

Before receiving cytarabine injection,

  • tell your doctor and pharmacist if you are allergic to cytarabine or any of the ingredients in cytarabine injection. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: digoxin (Lanoxin), flucytosine (Ancobon), or gentamicin. Other medications may also interact with cytarabine, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • tell your doctor if you have or have ever had kidney or liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. You should not become pregnant while you are receiving cytarabine injection. If you become pregnant while receiving cytarabine, call your doctor. Cytarabine may harm the fetus.

When To Contact Your Doctor or Health Care Provider:

Contact your health care provider immediately, day or night, if you should experience any of the following symptoms:

  • Fever of 100.4°F (38°C) or higher or chills (possible signs of infection).
  • Chest pain or heart palpitations
  • Inability to pass urine

The following symptoms require medical attention, but are not an emergency. Contact your health care provider within 24 hours of noticing any of the following:

  • Diarrhea (4-6 episodes in a 24 hour period)
  • Nausea (unable to drink fluids and unrelieved with prescription medication).
  • Vomiting (more than 4-5 times in a 24 hour period)
  • Unusual bleeding or bruising
  • Black or tarry stools, or blood in your stools or urine
  • Extreme fatigue (unable to carry on self-care activities)
  • Mouth sores (painful redness, swelling or ulcers)
  • Cough and/or shortness of breath
  • Excessive sleepiness or confusion
  • Changes in balance and coordination
  • Yellowing of the skin or eyes
  • Changes in vision or burning/or tearing of eyes
  • Swelling, redness and pain in one leg or arm and not the other
  • Stomach pains

Always inform your health care provider if you experience any unusual symptoms.

Precautions:

  • Before starting cytarabine treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.). Do not take aspirin, products containing aspirin unless your doctor specifically permits this.
  • Do not receive any kind of immunization or vaccination without your doctor’s approval while taking cytarabine.
  • Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. Pregnancy category D (cytarabine may be hazardous to the fetus. Women who are pregnant or become pregnant must be advised of the potential hazard to the fetus).
  • For both men and women: Use contraceptives, and do not conceive a child (get pregnant) while taking cytarabine. Barrier methods of contraception, such as condoms, are recommended.

Self-Care Tips:

  • Drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise.
  • You may be at risk of infection so try to avoid crowds or people with colds, and report fever or any other signs of infection immediately to your health care provider.
  • Wash your hands often.
  • To help treat/prevent mouth sores, use a soft toothbrush, and rinse three times a day with 1/2 to 1 teaspoon of baking soda and/or 1/2 to 1 teaspoon of salt mixed with 8 ounces of water.
  • Use an electric razor and a soft toothbrush to minimize bleeding.
  • Avoid contact sports or activities that could cause injury.
  • To reduce nausea, take anti-nausea medications as prescribed by your doctor, and eat small, frequent meals.
  • Keeps palms of hands and soles of feet moist using emollients such as Aveeno®, Udder Cream, Lubriderm® or Bag Balm®.
  • Avoid sun exposure. Wear SPF 30 (or higher) sunblock and protective clothing.
  • In general, drinking alcoholic beverages should be kept to a minimum or avoided completely. You should discuss this with your doctor.
  • Get plenty of rest.
  • Maintain good nutrition.
  • If you experience symptoms or side effects, be sure to discuss them with your health care team. They can prescribe medications and/or offer other suggestions that are effective in managing such problems.

References

Doctor visit helper

Prepare before seeing a doctor

A simple rural-patient checklist to help you explain symptoms clearly, ask better questions, and avoid unsafe self-treatment.

Safety note: This is not a prescription or diagnosis. For severe symptoms, pregnancy danger signs, children with serious illness, chest pain, breathing difficulty, stroke-like weakness, or major injury, seek urgent care.

Which doctor may help?

Start with a registered doctor or the nearest qualified health center.

What to tell the doctor

  • Write when the problem started and how it changed.
  • Bring old prescriptions, investigation reports, and current medicines.
  • Write allergies, pregnancy status, diabetes, kidney/liver disease, and major past illnesses.
  • Bring one family member if the patient is weak, elderly, confused, or a child.

Questions to ask

  • What is the most likely cause of my symptoms?
  • Which danger signs mean I should go to hospital quickly?
  • Which tests are necessary now, and which can wait?
  • How should I take medicines safely and what side effects should I watch for?
  • When should I come for follow-up?

Tests to discuss

  • Vital signs: temperature, pulse, blood pressure, oxygen saturation
  • Basic physical examination by a clinician
  • CBC, urine test, blood sugar, or imaging only when clinically needed

Avoid these mistakes

  • Do not use antibiotics, steroid tablets/injections, or strong painkillers without proper medical advice.
  • Do not hide pregnancy, kidney disease, ulcer, allergy, or blood thinner use.
  • Do not delay emergency care when danger signs are present.

Medicine safety and first-aid guide

This section is for patient education only. It does not replace a doctor, pharmacist, or emergency care.

Safe first steps

  • Avoid heavy lifting, sudden bending, and prolonged bed rest.
  • Use comfortable posture and gentle movement as tolerated.
  • Discuss physiotherapy, X-ray, or MRI only when clinically needed.

OTC medicine safety

  • For mild back pain, pain-relief medicine may be discussed with a doctor or pharmacist.
  • Avoid repeated painkiller use if you have kidney disease, stomach ulcer, uncontrolled blood pressure, or are taking blood thinners.

Avoid these mistakes

  • Do not start antibiotics without a proper medical decision.
  • Do not use steroid tablets or injections casually for quick relief.
  • Do not delay emergency care because of home remedies.

Get urgent help if

  • Back pain with leg weakness, numbness around private area, loss of urine/stool control, fever, cancer history, or major injury needs urgent care.
Medicine names, dose, and timing must be decided by a qualified clinician or pharmacist after checking age, pregnancy, allergy, other diseases, and current medicines.

For rural patients and family caregivers

Patient health record and symptom diary

Write your symptoms, medicines already taken, test results, and questions before visiting a doctor. This note stays on your device unless you print or copy it.

Doctor to discuss: Medicine doctor / pediatrician for children / qualified clinician
Tests to discuss with doctor
  • Temperature chart and hydration assessment
  • CBC with platelet count if fever persists or dengue/other infection is possible
  • Urine test, malaria/dengue tests, chest evaluation, or blood culture only when clinically indicated
Questions to ask
  • What is the most likely cause of my symptoms?
  • Which warning signs mean I should go to emergency care?
  • Which tests are really needed now?
  • Which medicines are safe for my age, pregnancy status, allergy, kidney/liver/stomach condition, and current medicines?
  • Do I need antibiotics, or is this more likely viral?

Emergency warning signs such as chest pain, severe breathing difficulty, sudden weakness, confusion, severe dehydration, major injury, or loss of bladder/bowel control need urgent medical care. Do not wait for online information.

Safe pathway to proper treatment

Care roadmap for: Cytarabine – Uses, Dosage, Side Effects, Interactions

Use this simple roadmap to understand the next safe steps. It is educational and does not replace examination by a doctor.

Go to emergency care if you notice:
  • Severe or rapidly worsening symptoms
  • Breathing difficulty, chest pain, fainting, confusion, severe weakness, major injury, or severe dehydration
Doctor / service to discuss: Qualified healthcare provider; specialist depends on symptoms and examination.
  1. Step 1

    Check danger signs first

    If danger signs are present, seek emergency care and do not wait for online information.

  2. Step 2

    Record the symptom story

    Write when symptoms started, severity, medicines already taken, allergies, pregnancy status, and test results.

  3. Step 3

    Visit a qualified clinician

    A doctor, nurse, or qualified healthcare provider can examine you and decide which tests or treatment are needed.

  4. Step 4

    Do only useful tests

    Do tests after clinical assessment. Avoid unnecessary tests, random antibiotics, or repeated medicines without diagnosis.

  5. Step 5

    Follow up and return early if worse

    If symptoms worsen, new warning signs appear, or treatment is not helping, return for review quickly.

Rural patient practical tips
  • Take a written symptom diary and all previous prescriptions/test reports.
  • Do not hide medicines already taken, even herbal or over-the-counter medicines.
  • Ask which warning signs mean urgent referral to hospital.

This roadmap is for education. A real diagnosis and treatment plan requires history, examination, and clinical judgment.

RX Patient Help

Ask a health question safely

Write your symptom story. A health professional or site editor can review it before any answer is prepared. This box is not for emergency care.

Emergency first: Severe chest pain, breathing trouble, unconsciousness, stroke signs, severe injury, heavy bleeding, or rapidly worsening symptoms need urgent local medical care now.

Frequently Asked Questions

Is this article a replacement for a doctor?

No. It is educational content only. Patients should consult a qualified clinician for diagnosis and treatment.

When should I seek urgent care?

Seek urgent care for severe symptoms, rapidly worsening condition, breathing difficulty, severe pain, neurological changes, or any emergency warning sign.

References

Add references, clinical guidelines, textbooks, journal articles, or trusted medical sources here. You can edit this area from the RX Article Professional Blocks panel.

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