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ONCOLOGY & ANTINEOPLASTIC MONOGRAPH CODE: [ONC-04] ID: TIP-MED-000553 ⚠️ HIGH-ALERT / SPECIALIST SUPERVISION

Cytarabine (Ara-C)

Active Ingredient / Scientific Identity: Cytarabine • Class: Antimetabolite (S-Phase Specific) • Pyrimidine Nucleoside Analogue Antimetabolite

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Generic / Entity NameCytarabine (Ara-C) ([ONC-04])
Verified Indian Brands / RefCytosar (Pfizer Ltd), Bioarac (Biochem), Arasid (Intas Pharmaceuticals)
Pharmacological ClassAntimetabolite (S-Phase Specific) • Pyrimidine Nucleoside Analogue Antimetabolite
Available Dosage FormsSolution for Injection: 100 mg/mL, 500 mg vial, 1 g vial
Regulatory ClassificationSchedule H (Prescription Only — Specialist Oncology Supervision)
Key Warning & Review DateHigh-Dose Cytarabine (HiDAC) Syndrome: cerebellar neurotoxicity (ataxia, dysarthria, nystagmus — increased risk if age >60 or
Reviewed: 2026-11-10
Safety Matrix:⚖️ Legal Status: Schedule H (Prescription Only — Specialist Oncology 🚨 Clinically High-Alert: Independent Dose & Route Verification Required☣️ Hazardous / Reproductive Precaution: Strict Handling & Contraception Protocol👨‍⚕️ Specialist-Supervised Therapy

1. Clinical & Scientific Overview

Cytarabine (Ara-C) (TIP-MED-000553, Reference Code [ONC-04]) is classified under Oncology & Antineoplastic Medicines as a Antimetabolite (S-Phase Specific) • Pyrimidine Nucleoside Analogue Antimetabolite. Within the Indian regulatory and compendial framework, it is governed under Schedule H (Prescription Only — Specialist Oncology Supervision).

Verified Indian Market Examples / Compendial Status:
Cytosar (Pfizer Ltd), Bioarac (Biochem), Arasid (Intas Pharmaceuticals)
Representative Indian Oncology Formulations (Educational Identification Only): Cytosar (Pfizer Ltd), Bioarac (Biochem), Arasid (Intas Pharmaceuticals) — Solution for Injection: 100 mg/mL, 500 mg vial, 1 g vial.
Dosage Forms & Available Strengths:
Solution for Injection: 100 mg/mL, 500 mg vial, 1 g vial
Routes: Intravenous / Subcutaneous / Oral / Intramuscular strictly per oncology protocol

Oncology Specialisation & Cytotoxic Safety Protocol

Oncology Subclass:
Antimetabolite (S-Phase Specific)
Therapeutic Role Distinction:
Antineoplastic Cytotoxic

Standard Regimen & Cycle Context: 7+3 AML Induction: 100–200 mg/m2/day continuous IV infusion for 7 days + Daunorubicin Days 1–3; HiDAC Consolidation: 1.5–3 g/m2 IV over 3 hours q12h on Days 1, 3, 5.

Signature Dose-Limiting Toxicities & Organ Monitoring: High-Dose Cytarabine (HiDAC) Syndrome: cerebellar neurotoxicity (ataxia, dysarthria, nystagmus — increased risk if age >60 or CrCl <60 mL/min), chemical haemorrhagic conjunctivitis (prevented by prophylactic prednisolone/dexamethasone eye drops q6h starting before first HiDAC dose), and Cytarabine Syndrome (fever, myalgia, bone pain, maculopapular rash 6–12 h post-infusion).

Extravasation, Premedication & Safe Cytotoxic Handling: Perform finger-to-nose and gait cerebellar exam before EVERY HiDAC dose (discontinue immediately if ataxia or nystagmus develops); instil corticosteroid eye drops q6h during HiDAC and for 48 hours after completion.

3. Mechanism of Action & Pharmacodynamics

Phosphorylated intracellularly by deoxycytidine kinase to Ara-CTP, which competitively inhibits DNA polymerase alpha/delta and incorporates into replicating DNA strands, terminating chain elongation during S-phase.

4. Therapeutic Indications & Evidence-Supported Uses

  • Acute Myeloid Leukaemia (AML — 7+3 induction at 100–200 mg/m2/day and HiDAC consolidation at 1.5–3 g/m2 q12h)
  • CNS leukaemic meningitis (intrathecal preservative-free formulation only)

🇮🇳 Jurisdiction & Indication Note: Indications and schedules reflect Indian compendial and regulatory records (CDSCO / Indian Pharmacopoeia & NFI / NLEM 2022). Where international reference labels (US FDA DailyMed / NCBI StatPearls) are cited for pharmacokinetic or mechanistic parameters, international approvals do not automatically imply CDSCO approval in India.

5. Educational Dosage Context, Formulations & Administration

Educational Dosing & Regimen Summary: Educational Oncology Regimen Context (Specialist Reference Only): 7+3 AML Induction: 100–200 mg/m2/day continuous IV infusion for 7 days + Daunorubicin Days 1–3; HiDAC Consolidation: 1.5–3 g/m2 IV over 3 hours q12h on Days 1, 3, 5.

Administration & Meal Timing: 7+3 AML Induction: 100–200 mg/m2/day continuous IV infusion for 7 days + Daunorubicin Days 1–3; HiDAC Consolidation: 1.5–3 g/m2 IV over 3 hours q12h on Days 1, 3, 5.

6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment

Absorption & Disposition:
Specialist oncology pharmacokinetic profile; dosing depends on Body Surface Area (BSA in m2), Calvert GFR formula, or flat targeted dosing with strict organ-function adjustments.
Metabolism & Biotransformation:
Hepatic enzymatic activation/inactivation or proteolytic degradation (for monoclonal antibodies); see specific polymorphism and interaction notes.
Elimination & Renal Adjustment:
Verify serum creatinine and eGFR before every cycle; see drug-specific renal dosing and uroprotection rules.
Hepatic Impairment Considerations:
Check total bilirubin, AST, and ALT prior to each cycle; taxanes, anthracyclines, and TKIs require strict hepatic dose modification.

7. Contraindications, Precautions & High-Risk Warnings

Contraindications & Red-Flag Precautions:
  • Severe hypersensitivity to Cytarabine or formulation vehicle
  • Pregnancy and lactation (potent teratogen/embryotoxic class warning unless explicitly evaluated by oncology specialist)
  • Severe unrecovered bone marrow aplasia or decompensated organ failure per protocol thresholds

Key Clinical Precautions: High-Dose Cytarabine (HiDAC) Syndrome: cerebellar neurotoxicity (ataxia, dysarthria, nystagmus — increased risk if age >60 or CrCl <60 mL/min), chemical haemorrhagic conjunctivitis (prevented by prophylactic prednisolone/dexamethasone eye drops q6h starting before first HiDAC dose), and Cytarabine Syndrome (fever, myalgia, bone pain, maculopapular rash 6–12 h post-infusion).

8. Adverse Effects Profile

Common & Mechanism-Related Adverse Effects:
  • High-Dose Cytarabine (HiDAC) Syndrome: cerebellar neurotoxicity (ataxia, dysarthria, nystagmus — increased risk if age >60 or CrCl <60 mL/min), chemical haemorrhagic conjunctivitis (prevented by prophylactic prednisolone/dexamethasone eye drops q6h starting before first HiDAC dose), and Cytarabine Syndrome (fever, myalgia, bone pain, maculopapular rash 6–12 h post-infusion).
Serious / Dose-Limiting Adverse Effects:
  • High-Dose Cytarabine (HiDAC) Syndrome: cerebellar neurotoxicity (ataxia, dysarthria, nystagmus — increased risk if age >60 or CrCl <60 mL/min), chemical haemorrhagic conjunctivitis (prevented by prophylactic prednisolone/dexamethasone eye drops q6h starting before first HiDAC dose), and Cytarabine Syndrome (fever, myalgia, bone pain, maculopapular rash 6–12 h post-infusion).

9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions

  • High-Dose Cytarabine (HiDAC) Syndrome: cerebellar neurotoxicity (ataxia, dysarthria, nystagmus — increased risk if age >60 or CrCl <60 mL/min), chemical haemorrhagic conjunctivitis (prevented by prophylactic prednisolone/dexamethasone eye drops q6h starting before first HiDAC dose), and Cytarabine Syndrome (fever, myalgia, bone pain, maculopapular rash 6–12 h post-infusion).
  • Avoid live-attenuated vaccines during immunosuppressive chemotherapy; verify CYP3A4, UGT1A1, DPD, and QTc interactions before each cycle.

10. Clinical Monitoring, Patient Counselling & Storage

Clinical & Laboratory Monitoring: Perform finger-to-nose and gait cerebellar exam before EVERY HiDAC dose (discontinue immediately if ataxia or nystagmus develops); instil corticosteroid eye drops q6h during HiDAC and for 48 hours after completion.

Pharmacist Patient Counselling Points:

  • Perform finger-to-nose and gait cerebellar exam before EVERY HiDAC dose (discontinue immediately if ataxia or nystagmus develops); instil corticosteroid eye drops q6h during HiDAC and for 48 hours after completion.
  • Report fever >=38.0°C (100.4°F) immediately (medical emergency: possible febrile neutropenia).
  • Follow strict reproductive contraception and safe cytotoxic oral handling instructions.

Storage, Stability & Dispensing Safeguards: Perform finger-to-nose and gait cerebellar exam before EVERY HiDAC dose (discontinue immediately if ataxia or nystagmus develops); instil corticosteroid eye drops q6h during HiDAC and for 48 hours after completion.

11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)

THE 12-STEP ORAL DRUG JOURNEY THROUGH THE HUMAN BODY (LADME) Note: IV bolus enters Step 6 directly (F = 100%); Sublingual & Transdermal routes bypass Step 4–5 Portal First-Pass Metabolism 1. Oral Administration • Tablet / Capsule swallowed • Gastric emptying to duodenum pH 1.5–3.5 (Stomach) 2. Disintegration & Dissolution • Tablet breaks into granules • API dissolves in GI fluid Noyes-Whitney Dissolution Rate 3. GI Epithelial Absorption • Crosses intestinal villi • Passive / Active / P-gp efflux Small Intestine (Large Surface Area) 4. Portal Circulation • Mesenteric veins → Portal vein • Delivers blood to liver sinusoids Pre-systemic Venous Conduit 5. First-Pass Metabolism • Gut & hepatic CYP450 extraction • High: GTN, Propranolol, Morphine Determines Bioavailability (F = f_a × (1-E_H)) 6. Systemic Circulation • Hepatic vein → IVC → Heart • Unbound vs Albumin-bound drug Only FREE drug is active 7–8. Tissue Distribution (Vd) • Capillary permeation to organs • Blood-Brain & Placental barriers Vd = Dose / C_0 (L or L/kg) 9. Target Site of Action • Receptors (GPCR, Ion channel) • Enzymes & Carrier Transporters Pharmacodynamic Effect (E_max, EC50) 10. Hepatic Biotransformation • Phase I (CYP450 Oxidation/Hydrolysis) • Phase II (Glucuronidation/Sulfation) Converts lipophilic drug → hydrophilic metabolite 11. Renal & Biliary Elimination • Nephron: Filtration + Secretion − Reabsorption • Biliary excretion & Enterohepatic recycling Total Clearance CL_tot = CL_renal + CL_hepatic 12. Excretion from the Body • Urine (Primary polar metabolite route) • Bile/Faeces, Expired Air, Sweat, Milk Elimination Half-Life t1/2 = (0.693 × Vd) / CL
svg-v339-01-adme-12-step-journey — 8.1 Complete 12-Step Journey of an Orally Administered Drug (ADME): Figure 8.1: The 12-step physiological journey of a typical orally administered solid dosage form through Liberation, Absorption, Distribution, Metabolism, and Excretion (LADME). Note: Parenteral (IV), sublingual, and inhalational routes bypass gastrointestinal absorption and/or hepatic first-pass metabolism.

12. Authoritative References, Regulatory Sources & Editorial Disclaimer

Primary Compendial & Guideline Reference: National Cancer Grid (NCG) India Consensus Guidelines; NLEM 2022 Antineoplastic Section; Indian Pharmacopoeia (IP) & CDSCO Approved Oncology Prescribing Information.

Official Verification Portals: National Cancer Grid (NCG) India — Evidence-Based Oncology Guidelines • CDSCO — Central Drugs Standard Control Organization Approved Drug Data • Indian Pharmacopoeia Commission (IPC)

Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: VERIFIED_EDUCATIONAL_CONTENT

Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.