Apresoline

Apresoline Uses, Dosage, Side Effects, Food Interaction and all others data.

Originally developed in the 1950s as a malaria treatment, hydralazine showed antihypertensive ability and was soon repurposed. Apresoline is a hydrazine derivative vasodilator used alone or as adjunct therapy in the treatment of hypertension and only as adjunct therapy in the treatment of heart failure. Apresoline is no longer a first line therapy for these indications since the development of newer antihypertensive medications.

Apresoline hydrochloride was FDA approved on 15 January 1953.

Apresoline interferes with calcium transport to relax arteriolar smooth muscle and lower blood pressure. Apresoline has a short duration of action of 2-6h. This drug has a wide therapeutic window, as patients can tolerate doses of up to 300mg. Patients should be cautioned regarding the risk of developing systemic lupus erythematosus syndrome.

Trade Name Apresoline
Availability Prescription only
Generic Hydralazine
Hydralazine Other Names 1-Hydrazinophthalazine, 1-Phthalazinylhydrazine, 6-Hydralazine, Hidralazina, Hydralazin, Hydralazine, Hydralazinum, Hydrallazine, Hydrazinophthalazine, Hypophthalin, Idralazina
Related Drugs amlodipine, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, spironolactone, nifedipine, captopril
Weight 10mg, 100mg, 25mg, 50mg,
Type Injection, Oral Tablet
Formula C8H8N4
Weight Average: 160.1759
Monoisotopic: 160.074896276
Protein binding

Hydralazine is 87% protein bound in serum likely to human serum albumin.

Groups Approved
Therapeutic Class
Manufacturer
Available Country Australia, United States,
Last Updated: September 19, 2023 at 7:00 am
Apresoline
Apresoline

Uses

Apresoline is an antihypertensive agent used for the management of essential hypertension or severe hypertension associated with conditions requiring immediate action, heart failure, and pre-eclampsia or eclampsia .

Apresoline is indicated alone or adjunct to standard therapy to treat essential hypertension. A combination product with isosorbide dinitrate is indicated as an adjunct therapy in the treatment of heart failure.

Apresoline is also used to associated treatment for these conditions: Heart Failure, Hypertension,Essential, Hypertensive crisis, Severe Hypertension

How Apresoline works

Apresoline may interfere with calcium transport in vascular smooth muscle by an unknown mechanism to relax arteriolar smooth muscle and lower blood pressure. The interference with calcium transport may be by preventing influx of calcium into cells, preventing calcium release from intracellular compartments, directly acting on actin and myosin, or a combination of these actions. This decrease in vascular resistance leads to increased heart rate, stroke volume, and cardiac output.

Apresoline also competes with protocollagen prolyl hydroxylase (CPH) for free iron. This competition inhibits CPH mediated hydroxylation of HIF-1α, preventing the degradation of HIF-1α. Induction of HIF-1α and VEGF promote proliferation of endothelial cells and angiogenesis.

Toxicity

The oral LD50 in rats is 173-187mg/kg and the highest known dose an adult human has survived is 10g orally.

Patients experiencing an overdose may present with hypotension, tachycardia, headache, flushing, myocardial ischemia, myocardial infarction, cardiac arrhythmia, and shock. Overdose can be treated through emptying the gastric contents and administering activated charcoal, though these treatments may cause further arrhythmias and shock. Supportive and symptomatic treatment should be administered.

Food Interaction

  • Take with or without food. Food increases exposure to hydralazine, though this may not be clinically significant.

Volume of Distribution

The volume of distribution is 1.34±0.79L/kg in congestive heart failure patients and 1.98±0.22L/kg in hypertensive patients.

Elimination Route

Taking oral hydralazine with food improves the bioavailability of the drug. An intravenous dose of 0.3mg/kg leads to an AUC of 17.5-29.4µM*min and a 1mg/kg oral dose leads to an AUC of 4.0-30.4µM*min. The Cmax of oral hydralazine is 0.12-1.31µM depending on the acetylator status of patients.

Half Life

Apresoline has a half life of 2.2-7.8h in rapid acetylators and 2.0-5.8h in slow acetylators. The half life in heart failure patients is 57-241 minutes with an average of 105 minutes and in hypertensive patients is 200 minutes for rapid acetylators and 297 minutes for slow acetylators.

Clearance

The majority of hydralazine clearance is extrahepatic- 55% for rapid acetylators and 70% for slow acetylators. The average clearance in congestive heart failure patients is 1.77±0.48L/kg/h, while hypertensive patients have an average clearance of 42.7±8.9mL/min/kg.

Elimination Route

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Innovators Monograph

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http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0004150
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http://www.genome.jp/dbget-bin/www_bget?cpd:C07040
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3637
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507533
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http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=81461
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=5470
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=5775
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL276832
https://zinc.docking.org/substances/ZINC000012360535
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000728
http://www.pharmgkb.org/drug/PA449894
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/HLZ
http://www.rxlist.com/cgi/generic/hydralazine.htm
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https://en.wikipedia.org/wiki/Hydralazine
*** Taking medicines without doctor's advice can cause long-term problems.
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