Trisha Shetty (Editor)

Hydralazine

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AHFS/Drugs.com
  
Monograph

License data
  
US FDA: Hydralazine

CAS ID
  
86-54-4

MedlinePlus
  
a682246

Routes of administration
  
By mouth, intravenous

Molar mass
  
160.176 g/mol

Hydralazine

Trade names
  
Apresoline, BiDil, others

Pregnancy category
  
AU: C US: C (Risk not ruled out)

Hydralazine nursing considerations side effects and mechanism of action pharmacology for nurses


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

Contents

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

Hydralazine was discovered while scientists at Ciba were looking for a treatment for malaria. It was patented in 1949. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. The wholesale cost in the developing world is about 2.78 to 9.11 USD per month. In the United States treatment costs about 50 to 100 USD per month.

Scenario 04 hydralazine and imdur


Medical use

Hydralazine is not used as a primary drug for treating hypertension because it elicits a reflex sympathetic stimulation of the heart (the baroreceptor reflex). The sympathetic stimulation may increase heart rate and cardiac output, and in people with coronary artery disease may cause angina pectoris or myocardial infarction. Hydralazine may also increase plasma renin concentration, resulting in fluid retention. To prevent these undesirable side effects, hydralazine is usually prescribed in combination with a β-blocker (e.g., propranolol) and a diuretic. Beta-blockers licensed to treat heart failure in the UK include bisoprolol, carvedilol, and nebivolol.

Hydralazine is used to treat severe hypertension, but again, it is not a first-line therapy for essential hypertension. However, hydralazine is the first-line therapy for hypertension in pregnancy, with methyldopa.

Hydralazine is commonly used in combination with isosorbide dinitrate for the treatment of congestive heart failure in self-identified African American populations. This preparation, BiDil, was the first race-based prescription drug.

It should not be used in people with tachycardia, heart failure, who have constrictive pericarditis, who have lupus, a dissecting aortic aneurism, or porphyria.

Adverse effects

Prolonged treatment may cause a syndrome similar to lupus which can become fatal if the symptoms are not noticed and drug treatment stopped.

Very common (>10% frequency) side effects include headache, high heart rate, and palpitations.

Common (1–10% frequency) side effects include flushing, hypotension, anginal symptoms, aching or swelling joints, muscle aches, positive tests for ANP, stomach upset, diarrhea, nausea, and vomiting, and Edema (sodium and water retention).

Interactions

It may potentiate the antihypertensive effects of:

Drugs subject to a strong first-pass effect such as β-blockers may increase the bioavailability of hydralazine. Epinephrine (adrenaline)'s heart rate-accelerating effects are increased by hydralazine, hence may lead to toxicity.

Mechanism of action

It is a direct-acting smooth muscle relaxant and acts as a vasodilator primarily in resistance arterioles; the molecular mechanism was unknown as of 2011. By relaxing vascular smooth muscle, vasodilators act to decrease peripheral resistance, thereby lowering blood pressure and decreasing afterload.

Chemistry

Hydralazine belongs to the hydrazinophthalazine class of drugs.

History

The antihypertensive activity of hydralazine was discovered by scientists at Ciba who were trying to discover drugs to treat malaria; it was initially called C-5968 and 1-hydrazinophthalazine; Ciba's patent application was filed in 1945 and issued in 1949, and the first scientific publications of its blood-pressure lowering activities appeared in 1950. It was approved by the FDA in 1953.

It was one of the first antihypertensive medications that could be taken by mouth.

Research

Hydralazine has also been studied as a treatment for myelodysplastic syndrome in its capacity as a DNA methyltransferase inhibitor.

References

Hydralazine Wikipedia