Page last updated: 2024-12-06

endralazine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

BQ 22-708: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID47608
CHEMBL ID254193
CHEBI ID135105
SCHEMBL ID308557
MeSH IDM0063831

Synonyms (31)

Synonym
arritlan
endralazine
miretilan
endralazina [inn-spanish]
endralazine [inn:ban]
bq 22-708
6-benzoyl-3-hydrazino-5,6,7,8-tetrahydropyrido(4,3-c)pyridazin
pyrido(4,3-c)pyridazin-3(2h)-one, 6-benzoyl-5,6,7,8-tetrahydro-, 3-hydrazone
3-hydrazino-5,6,7,8-tetrahydropyrido(4,3-c)pyridazin-6-yl-phenyl-keton
endralazinum [inn-latin]
CHEBI:135105
CHEMBL254193
(3-hydrazinyl-7,8-dihydro-5h-pyrido[4,3-c]pyridazin-6-yl)-phenylmethanone
endralazine (inn)
39715-02-1
D08254
unii-l44741f05p
endralazina
endralazinum
l44741f05p ,
endralazine [who-dd]
endralazine [inn]
endralazine [mi]
6-benzoyl-5,6,7,8-tetrahydropyrido(4,3-c)pyridazin-3(2h)-one hydrazone
pyrido(4,3-c)pyridazin-3(2h)-one, 6-benzoyl-5,6,7,8-tetrahydro-, hydrazone
SCHEMBL308557
6-benzoyl-3-hydrazino-5,6,7,8-tetrahydropyrido[4,3-c]pyridazine
ALAXZYHFVBSJKZ-UHFFFAOYSA-N
DTXSID40192791
Q5376588
DB13435

Research Excerpts

Overview

Endralazine is a peripherally-acting vasodilator with chemical and pharmacological similarities to hydralazine. Endralazine appears to be a useful new drug for the treatment of hypertension.

ExcerptReferenceRelevance
"Endralazine appears to be a useful new drug for the treatment of hypertension."( Endralazine, a new peripheral vasodilator--a randomized cross-over trial against dihydralazine.
Axthelm, T; Kirch, W,
)
2.3
"Endralazine is a peripherally-acting vasodilator with chemical and pharmacological similarities to hydralazine. "( Clinical pharmacological studies with the vasodilator endralazine in normotensive subjects and essential hypertensives.
Elliott, HL; Howden, CW; Lawrie, CB; Meredith, PA; Reid, JL, 1984
)
1.96
"Endralazine is a peripherally-acting vasodilator similar to hydralazine. "( Pharmacodynamic and pharmacokinetic studies with the vasodilator endralazine.
Elliott, HL; Meredith, PA; Reid, JL, 1984
)
1.95
"Endralazine (I) is a new antihypertensive which is chemically and pharmacologically related to hydralazine and dihydralazine. "( Sensitive high-performance liquid chromatographic assay for endralazine and two of its metabolites in human plasma.
Cozamanis, I; Reece, PA; Zacest, R, 1981
)
1.95
"Endralazine is an effective antihypertensive agent with adverse symptoms similar to those experienced with hydralazine."( Evaluation of once daily endralazine in hypertension.
Carruthers, SG; Spence, JD; Wu, R, 1986
)
1.3

Toxicity

ExcerptReferenceRelevance
" a) In mice, a single ip administration of the LD50 of the three drugs caused a small but statistically significant increase over controls in DNA elution rate, ie, a modest amount of DNA fragmentation, in three of the four organs (liver, lung, kidney, and spleen) tested, DNA damage being absent in lung for hydralazine and endralazine and in liver for dihydralazine."( In vivo and in vitro genotoxicity of three antihypertensive hydrazine derivatives (hydralazine, dihydralazine, and endralazine).
Bennicelli, C; Brambilla, G; Cajelli, E; Camoirano, A; Cavanna, M; de Flora, S; Faggin, P; SciabĂ , L; Zanacchi, P, 1982
)
0.65

Pharmacokinetics

The mean terminal elimination half-life for endralazine of 136 min in hypertensive patients did not differ significantly from the 155 min in normotensive subjects. The possibility to apply impedance cardiography technique and individual statistical analysis based on Dixon's criterion to pharmacodynamic studies of single hydralazine ( apressine ), prazosine ( pratsiol ), endralazines ( mirethilan ), propranolol (obsidan) is discussed.

ExcerptReferenceRelevance
"The possibility to apply impedance cardiography technique and individual statistical analysis based on Dixon's criterion to pharmacodynamic studies of single hydralazine ( apressine ), prazosine ( pratsiol ), endralazine ( mirethilan ), propranolol (obsidan) doses is discussed."( [Methodologic approach to individual evaluation of the pharmacodynamic effects of single doses of hydralazine, endralazine, prazosine and propranolol in hypertension patients].
Izotov, AI; Postol'nikov, SF; Vygodin, VA, 1984
)
0.67
" The mean terminal elimination half-life for endralazine of 136 min in hypertensive patients did not differ significantly from the 155 min in normotensive subjects."( The pharmacokinetics of endralazine in essential hypertensives and in normotensive subjects.
Elliott, HL; Kelman, AW; McSharry, DR; Meredith, PA; Reid, JL, 1983
)
0.83
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
"5 h and the oral bioavailability was 75%."( Clinical pharmacological studies with the vasodilator endralazine in normotensive subjects and essential hypertensives.
Elliott, HL; Howden, CW; Lawrie, CB; Meredith, PA; Reid, JL, 1984
)
0.52
"5 h and the oral bioavailability was 75%."( Pharmacodynamic and pharmacokinetic studies with the vasodilator endralazine.
Elliott, HL; Meredith, PA; Reid, JL, 1984
)
0.51
" E had high system bioavailability (73."( Endralazine - a new hydralazine-like antihypertensive with high systemic bioavailability.
Cozamanis, I; Reece, PA; Zacest, R, 1983
)
1.71
" In normal subjects the mean oral bioavailability for endralazine was 75% and the mean clearance was 780 ml/min."( The pharmacokinetics of endralazine in essential hypertensives and in normotensive subjects.
Elliott, HL; Kelman, AW; McSharry, DR; Meredith, PA; Reid, JL, 1983
)
0.82
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34

Dosage Studied

The acetylator phenotype does not affect the therapeutic efficacy or dosage requirement of endralazine. Dosage ranged from 10 mg to 30 mg endralazines per day and from 75 mg to 200 mg hydralazine per day according to patient response. During chronic dosing, the terminal elimination half-life significantly increased to a mean of 7.

ExcerptRelevanceReference
" Blood pressure was measured 2 h and 24 h after dosing and the drug dose doubled at 2 and 4 weeks if the 24-h MAP remained greater than 110 mg Hg."( Comparison of once daily endralazine with placebo in the treatment of hypertension uncontrolled by a beta-blocker and diuretic.
McGourty, JC; Pidgeon, J; Silas, JH, 1985
)
0.57
" Dosage ranged from 10 mg to 30 mg endralazine per day and from 75 mg to 200 mg hydralazine per day according to patient response."( Comparative study of endralazine and hydralazine for the treatment of hypertension uncontrolled by a beta-blocker and diuretic.
Chazan, BI; Duff, DA; McCallum, A; Whaley, K, 1986
)
0.87
" It is concluded that the acetylator phenotype does not affect the therapeutic efficacy or dosage requirement of endralazine."( Endralazine, a new peripheral vasodilator: absence of effect of acetylator status on antihypertensive effect.
Bogers, WA; Holmes, DG; Huunan-Seppala, A; Wideroe, B; Wideroe, TE, 1983
)
1.92
" Blood pressure control remained good during this time, and the dosage was slightly reduced."( Endralazine, a new peripheral vasodilator--a randomized cross-over trial against dihydralazine.
Axthelm, T; Kirch, W,
)
1.57
" It is concluded that the differences between endralazine and hydralazine in dosage and metabolism may explain the lower immunogenic activity of endralazine."( Endralazine, a new peripheral vasodilator. Evaluation of safety and efficacy over a 3 year period.
Bogers, WA; Meems, L, 1983
)
1.97
" Dose-response relationships for endralazine, hydralazine and diazoxide, administered intravenously, were compared, and the interactions of endralazine with the ganglionic blocking agent, pentolinium, or with adrenaline, noradrenaline and angiotensin II were examined."( Studies in the rat on endralazine, a new antihypertensive drug structurally related to hydralazine.
Oates, HF; Stoker, LM,
)
0.73
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzamides
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (48)

TimeframeStudies, This Drug (%)All Drugs %
pre-199046 (95.83)18.7374
1990's0 (0.00)18.2507
2000's2 (4.17)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 102.11

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index102.11 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index4.14 (4.65)
Search Engine Demand Index184.36 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (102.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials14 (26.92%)5.53%
Reviews1 (1.92%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other37 (71.15%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]