Hydralazine

Not to be confused with hydrazine.

Hydralazine
Clinical data
Trade namesApresoline, BiDil, others
AHFS/Drugs.comMonograph
MedlinePlusa682246
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth, intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability26–50%
Protein binding85–90%
MetabolismLiver
Onset of action5 to 30 min[2]
Elimination half-life2–8 hours, 7–16 hours (renal impairment)
Duration of action2 to 6 hrs[2]
ExcretionUrine
Identifiers
IUPAC name
  • 1-hydrazinylphthalazine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.001.528
Chemical and physical data
FormulaC8H8N4
Molar mass160.180 g·mol−1
3D model (JSmol)
SMILES
  • NNc1c2ccccc2cnn1
InChI
  • InChI=1S/C8H8N4/c9-11-8-7-4-2-1-3-6(7)5-10-12-8/h1-5H,9H2,(H,11,12) Y
  • Key:RPTUSVTUFVMDQK-UHFFFAOYSA-N Y
  (verify)

Hydralazine, sold under the brand name Apresoline among others, is a medication used to treat high blood pressure and heart failure.[2] This includes high blood pressure in pregnancy and very high blood pressure resulting in symptoms.[3] It has been found to be particularly useful in heart failure, together with isosorbide dinitrate, for treatment of people of African descent.[2] It is given by mouth or by injection into a vein.[3] Effects usually begin around 15 minutes and last up to six hours.[2]

Common side effects include headache and fast heart rate.[2] It is not recommended in people with coronary artery disease or in those with rheumatic heart disease that affects the mitral valve.[2] In those with kidney disease a low dose is recommended.[3] Hydralazine is in the vasodilator family of medications, so it is believed to work by causing the dilation of blood vessels.[2]

Hydralazine was discovered while scientists at Ciba were looking for a treatment for malaria.[4] It was patented in 1949.[5] It is on the World Health Organization's List of Essential Medicines.[6] In 2022, it was the 121st most commonly prescribed medication in the United States, with more than 5 million prescriptions.[7][8]

  1. ^ "Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 30 March 2024.
  2. ^ a b c d e f g h "Hydralazine Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
  3. ^ a b c World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. p. 280. hdl:10665/44053. ISBN 9789241547659.
  4. ^ Wermuth CG (2 May 2011). The Practice of Medicinal Chemistry. Academic Press. p. 12. ISBN 9780080568775. Archived from the original on 26 February 2017.
  5. ^ Progress in Drug Research/Fortschritte der Arzneimittelforschung/Progrés des recherches pharmaceutiques. Birkhäuser. 2013. p. 206. ISBN 9783034870948. Archived from the original on 20 December 2016.
  6. ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
  7. ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
  8. ^ "Hydralazine Drug Usage Statistics, United States, 2013 – 2022". ClinCalc. Retrieved 30 August 2024.
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