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Details

Stereochemistry RACEMIC
Molecular Formula 2C10H19N3O2.H2O4S
Molecular Weight 524.632
Optical Activity ( + / - )
Defined Stereocenters 0 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GUANADREL SULFATE

SMILES

OS(O)(=O)=O.NC(=N)NCC1COC2(CCCCC2)O1.NC(=N)NCC3COC4(CCCCC4)O3

InChI

InChIKey=RTEVGQJRTFFMLL-UHFFFAOYSA-N
InChI=1S/2C10H19N3O2.H2O4S/c2*11-9(12)13-6-8-7-14-10(15-8)4-2-1-3-5-10;1-5(2,3)4/h2*8H,1-7H2,(H4,11,12,13);(H2,1,2,3,4)

HIDE SMILES / InChI

Description

Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via the norepinephrine pump or transporter. Guanadrel slowly displaces norepinephrine from its storage in nerve endings and thereby blocks the release of norepinephrine normally produced by nerve stimulation. The reduction in neurotransmitter release in response to sympathetic nerve stimulation, as a result of catecholamine depletion, leads to reduced arteriolar vasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position. Guanadrel is used to treat and control hypertension.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Hylorel

Cmax

ValueDoseCo-administeredAnalytePopulation
42 ng/mL
25 mg single, oral
GUANADREL plasma
Homo sapiens
73 ng/mL
25 mg single, oral
GUANADREL plasma
Homo sapiens
89.6 ng/mL
50 mg single, oral
GUANADREL plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
234 ng × h/mL
25 mg single, oral
GUANADREL plasma
Homo sapiens
627 ng × h/mL
25 mg single, oral
GUANADREL plasma
Homo sapiens
404.9 μg × h/mL
50 mg single, oral
GUANADREL plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
3.69 h
25 mg single, oral
GUANADREL plasma
Homo sapiens
6.8 h
25 mg single, oral
GUANADREL plasma
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
For high blood pressure: Adults—At first, 5 milligrams (mg) two times a day. Then, may be increased up to 20 to 75 mg a day, divided into two to four doses.
Route of Administration: Oral
In Vitro Use Guide
Unknown