Hydralazine

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Structural formula
Structural formula of hydralazine
General
Non-proprietary name Hydralazine
other names
  • 1-hydrazinophthalazine ( IUPAC )
  • Hydralazinum ( Latin )
Molecular formula C 8 H 8 N 4
External identifiers / databases
CAS number
PubChem 3637
DrugBank DB01275
Wikidata Q419987
Drug information
ATC code

C02 DB02

Drug class
properties
Molar mass 160.18 g · mol -1
Physical state

firmly

Melting point

172-173 ° C

safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS labeling of hazardous substances
06 - Toxic or very toxic

danger

H and P phrases H: 301-315-319-335
P: 261-301 + 310-305 + 351 + 338
Toxicological data

90 mg kg −1 ( LD 50 ,  rat ,  oral )

As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Hydralazine is a vasodilating drug ( vasodilator ) that is used (like dihydralazine , which is more commonly used in Europe ) for high blood pressure disorders during pregnancy or for heart failure . Hydralazine is on the WHO list of essential drugs .

history

BH Ringier and J. Druey developed some phthalazine derivatives for the first time . This was examined by Franz Gross in 1950 . He found it had a strong antihypertensive effect. That is why hydralazine was introduced into therapy. However, this turned out to be unsuitable because it had severe side effects (when administered alone or in combination with a ganglion blocker ). For this reason it was replaced a short time later by dihydralazine (Nepresol®).

Pharmacodynamics

Like dihydralazine, hydralazine relaxes the cells of the smooth muscles of the blood vessels , which dilates arteries and arterioles ( vasodilation ), which leads to a reduction in peripheral resistance . This lowers blood pressure and afterload and relieves the heart.

Reflex tachycardia , decreased appetite, nausea and vomiting, diarrhea, constipation, edema formation, rhinitis and rarely lupus erythematosus-like skin changes can occur as side effects. The latter are reversible after weaning.

Pharmacokinetics

After oral administration, hydralazine is almost completely absorbed, but due to a first-pass effect in the liver the bioavailability is only 25–30%. Maximum plasma levels are reached after 0.5 to 2 hours, the duration of action is two to six hours. 90% of the degradation takes place in the liver via hydroxylation and N - acetylation . The metabolites are excreted via the kidneys together with unchanged hydralazine.

Trade names

Monopreparations

Apresoline (USA)

Combination preparations

pertenso (hydralazine, propranolol , bendroflumethiazide ), TRI-Normin ( atenolol , chlortalidone , hydralazine) (D)

Individual evidence

  1. ↑ a b Entry on hydralazine. In: Römpp Online . Georg Thieme Verlag, accessed on November 11, 2014.
  2. ↑ a b Datasheet Hydralazine hydrochloride from Sigma-Aldrich , accessed on April 4, 2011 ( PDF ).
  3. ^ Wolf-Dieter Müller-Jahncke , Christoph Friedrich , Ulrich Meyer: Medicinal history . 2., revised. and exp. Ed. Wiss. Verl.-Ges, Stuttgart 2005, ISBN 978-3-8047-2113-5 , pp. 165 .
  4. ↑ Red List online, as of October 2009.

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