Article: Hydroxyurea

Hydroxyurea
Systematic (IUPAC) name
hydroxyurea
Identifiers
CAS number	127-07-1
ATC code	L01XX05
PubChem	3657
DrugBank	APRD00023
Chemical data
Formula	CH4N2O2
Mol. weight	76.0547 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	Liver
Half life	3-4 hours
Excretion	Renal and lungs
Therapeutic considerations
Pregnancy cat.	D (USA)
Legal status
Routes	Oral

Hydroxyurea or hydroxycarbamide (the latter being the recommended International Non-Proprietary Name), (brand names include Hydrea®) is an antineoplastic drug used in hematological malignancies. It is also used as an antiretroviral agent (e.g., against HIV). Its mechanism of action is believed to be based on its inhibition of the enzyme ribonucleotide reductase.

Uses

• Polycythemia vera
• Chronic myelogenous leukemia
• Essential thrombocytosis
• Sickle-cell disease (selectively breaks down cells that are prone to sickle, as well as increasing fetal hemoglobin content)
• AIDS as an adjunct to ddI in combination antiretroviral therapies
• Biochemical research as an agent that causes ribonucleotide depletion and results in DNA double strand breaks near replication forks (see DNA repair)

Dose

500 milligrams once or twice a day, or more if pancytopenia does not develop.

Side effects

Reported side-effects are: drowsiness, nausea, vomiting and diarrhea, constipation, mucositis, anorexia, stomatitis, bone marrow toxicity (which may take 7-21 days to recover after the drug has been discontinued), alopecia (hair loss), skin changes, abnormal liver enzymes, creatinine and blood urea nitrogen.

Due to its effect on the bone marrow, regular monitoring of the full blood count is vital, as well as early response to possible infections. In addition, renal function, uric acid and electrolytes, as well as liver enzymes, are commonly checked.

Use in Pregnancy

Category D - investigational or post-marketing data show risk to the fetus. However, potential benefits may outweigh the potential risk. Generally this rating is reserved for drugs with no safer alternatives.

Contraindications

Contraindications are: severe anemia, bone marrow depression or neutropenia.