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Hydroxyurea

Antimetabolite · Antineoplastic

Also known as Hydroxycarbamide, HYDREA

AntimetaboliteAntineoplasticATC null
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
X
FDA category + note
Top interactionssee all 12
  • AdalimumabSevereDatabaseDDInter
  • BaricitinibSevereDatabaseDDInter
  • CertolizumabSevereDatabaseDDInter
  • CladribineSevereDatabaseDDInter

Mechanism

Hydroxyurea inhibits ribonucleotide reductase by quenching the tyrosyl free radical at the active site of the M2 subunit, blocking the conversion of ribonucleotides to deoxyribonucleotides required for DNA synthesis. This produces S-phase specific cytotoxicity. In sickle cell disease, hydroxyurea's therapeutic benefit derives from its ability to reactivate fetal hemoglobin (HbF) gene expression through a mechanism involving nitric oxide generation and soluble guanylate cyclase activation, reducing sickling episodes.

Indications

Polycythaemia vera (specialist use only)Essential thrombocythaemia (specialist use only)Chronic myeloid leukaemia (specialist use only)Cancer of the cervix (specialist use only)sickle cell anemiacancerMyeloproliferative syndromes (particularly chronic myelogenous leukemia, polycythemia vera, myeloid metaplasia, essential thrombocytosis)Sickle cell disease (in adults)Thalassemia HbC and HbC/S (to induce HbF)Cervical carcinoma (with concurrent irradiation)Primary brain tumors (with concurrent irradiation)Head and neck cancer (with concurrent irradiation)Non–small cell lung cancer (with concurrent irradiation)Chronic myeloid leukaemiaPsoriasisPolycythaemia veraSome solid tumoursSickle cell disease (adults)

Dosing

Adult
Polycythaemia vera: Oral, initially 15–20 mg/kg daily, adjusted according to response; usual dose 500–1000 mg daily, dosage should be based on actual or ideal body weight, whichever is less. Essential thrombocythaemia: Oral, initially 15 mg/kg daily, adjusted according to response, based on actual or ideal body weight, whichever is less.…

Pharmacokinetics

Half-life
3.5 to 4.5 h (disappears from plasma)
Bioavailability
80% to 100% (oral)
Protein binding
Readily crosses the blood-brain barrier; significant quantities appear in human breast milk.
Excretion
From 40% to 80% of the drug is recovered in the urine within 12 h after administration.

Contraindications

  • Women with childbearing potential (due to teratogenicity)

Side effects

Common
Leukopenia (major toxic effect)AnemiaThrombocytopenia (occasionally)Gastrointestinal disturbancesMild dermatological reactionsStomatitis (rarely)Alopecia (rarely)Increased skin and fingernail pigmentationCutaneous reactionsPigmentation
Serious
  • Desquamative interstitial pneumonitis
  • Neurological manifestations (more rarely)
  • Painful leg ulcers (especially in elderly patients or those with renal dysfunction)
  • Myelosuppression

Pregnancy & lactation

Pregnancy

X

Drug interactions

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Certolizumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cladribine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clozapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Deferiprone
Severe
Database

Clinical effect not specified

Source: DDInter

Didanosine
Severe
Database

.

Source: DDInter

Etanercept
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Fingolimod
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Golimumab
Severe
Database

Clinical effect not specified

Source: DDInter

Infliximab
Severe
Database

Clinical effect not specified

Source: DDInter

Leflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Other Antimetabolite drugs

Ask House about Hydroxyurea

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung·Verified: 2026-05-13 · House clinical team