ETIGUANFACINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C12H13Cl2N3O3
Molecular Weight	318.156
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC(=O)NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl

InChI

InChIKey=NWKJFUNUXVXYGE-UHFFFAOYSA-N

InChI=1S/C12H13Cl2N3O3/c1-2-20-12(19)17-11(15)16-10(18)6-7-8(13)4-3-5-9(7)14/h3-5H,2,6H2,1H3,(H3,15,16,17,18,19)

HIDE SMILES / InChI

Molecular Formula	C12H13Cl2N3O3
Molecular Weight	318.156
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019032s021lbl.pdf | https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdfhttps://www.medkoo.com/products/7825

Etiguanfacine, also known as SSP-1871, is an α2-adrenoreceptor agonist.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Alpha-2a adrenergic receptor 63 Target ID: CHEMBL1867 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019032s021lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/9605427	Agonist 2678		7.03 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 567 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/019032s021lbl.pdf	Primary		Approved 8429	TENEX Approved Use Tenex (guanfacine hydrochloride) is indicated in the management of hypertension. Tenex may be given alone or in combination with other antihypertensive agents, especially thiazide-type diuretics. Launch Date 1986
Attention deficit hyperactivity disorder 68 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	Primary		Approved 8429	TENEX Approved Use INTUNIV® is a central alpha2A-adrenergic receptor agonist indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) as monotherapy and as adjunctive therapy to stimulant medications Launch Date 1986

C_max

Value	Dose	Analyte	Population
7 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: ADOLESCENT sex: UNKNOWN food status: UNKNOWN
10 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: CHILD sex: UNKNOWN food status: UNKNOWN
2.5 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
116 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: ADOLESCENT sex: UNKNOWN food status: UNKNOWN
162 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: CHILD sex: UNKNOWN food status: UNKNOWN
56 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:	GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
16 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:		GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
30% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	1 mg 1 times / day multiple, oral dose: 1 mg route of administration: Oral experiment type: MULTIPLE co-administered:		GUANFACINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
12 mg single, oral Overdose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/	unhealthy, 12 years n = 1 Health Status: unhealthy Condition: ADHD and Tourette syndrome Age Group: 12 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/	Disc. AE: Hypertensive... AEs leading to discontinuation/dose reduction: Hypertensive (1%) Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/
80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/	unhealthy, 17 years n = 1 Health Status: unhealthy Condition: ADHD Age Group: 17 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/	Disc. AE: Cardiogenic pulmonary edema... AEs leading to discontinuation/dose reduction: Cardiogenic pulmonary edema (1%) Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/
4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (6%) Fatigue (2%) Hypotension (1%) Headache (1%) Dizziness (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	unhealthy, children n = 16 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Age Group: children Population Size: 16 Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	Other AEs: Sedation, Fatigue... Other AEs: Sedation (below serious, 5 patients) Fatigue (below serious, 3 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT01069523

AEs

AE	Significance	Dose	Population
Hypertensive	1% Disc. AE	12 mg single, oral Overdose Dose: 12 mg Route: oral Route: single Dose: 12 mg Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/	unhealthy, 12 years n = 1 Health Status: unhealthy Condition: ADHD and Tourette syndrome Age Group: 12 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/23925253/
Cardiogenic pulmonary edema	1% Disc. AE	80 mg single, oral Overdose Dose: 80 mg Route: oral Route: single Dose: 80 mg Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/	unhealthy, 17 years n = 1 Health Status: unhealthy Condition: ADHD Age Group: 17 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/33069545/
Dizziness	1% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Headache	1% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Hypotension	1% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Fatigue	2% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Somnolence	6% Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf	unhealthy, children and adolescents n = 513 Health Status: unhealthy Condition: ADHD Age Group: children and adolescents Sex: M+F Population Size: 513 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022037s009lbl.pdf
Fatigue	below serious, 3 patients	4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	unhealthy, children n = 16 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Age Group: children Population Size: 16 Sources: https://clinicaltrials.gov/ct2/show/NCT01069523
Sedation	below serious, 5 patients	4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01069523	unhealthy, children n = 16 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorder Age Group: children Population Size: 16 Sources: https://clinicaltrials.gov/ct2/show/NCT01069523

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2C8 911 CYP2C19 1478 CYP3A4/5 278 CYP2B6 810	CYP3A4/5 85 P-gp 1537	CYP3A 129 CYP1A2 701 CYP2B6 547

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no
CYP3A 298	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf#page=16 Page: 16.0	no
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=15 Page: 15.0	no

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0	major	yes (co-administration study) Comment: There was a significant decrease in the rate and extent of guanfacine exposure when co-administered with rifampin, a CYP3A4 inducer. The exposure to guanfacine decreased by 70% (AUC) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0
P-gp 1537	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3173033/ Page: 18.0	weak
CYP3A4/5 85	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0	yes	yes (co-administration study) Comment: There was a substantial increase in the rate and extent of guanfacine exposure when administered with ketoconazole; the guanfacine exposure increased 3-fold (AUC) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022037lbl.pdf#page=10 Page: 10.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.tga.gov.au/sites/default/files/auspar-guanfacine-180503.pdf#page=30

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY546722	https://www.001chemical.com/chem/29110-47-2
AHH Chemical co.,ltd	MR-1013815	http://www.ahhchemical.com/product/MR-1013815.html
Alsachim	928	http://www.alsachim.com/product-C1246-glo.bal-view.html
Ambinter	Amb10843802	http://www.ambinter.com/reference/10843802
Angel Pharmatech	AG302778	http://www.angelpharmatech.com/29110-47-2.html
Angene	AGN-PC-04XZ20	http://www.angenechemical.com/productshow/AGN-PC-04XZ20.html
BLD Pharm	BD132435	http://www.bldpharm.com/products/29110-47-2.html
BioChemPartner	BCP09647	http://www.biochempartner.com/29110-47-2-BCP09647
BioCrick	BCC5180	http://www.biocrick.com/Guanfacine-BCC5180.html
BioSynth	J-017394	https://www.biosynth.com/en/products/all-products/products/J-017394.html
CSNpharm	CSN11127	https://www.csnpharm.com/products/guanfacine.html
Chem Scene	CS-2787	http://www.chemscene.com/29110-47-2.html
Clearsynth	CS-T-25721	https://www.clearsynth.com/en/CST25721.html
DC Chemicals	DC23226	http://www.dcchemicals.com/product_show-DC23226.html
Finetech	FT-0669068	http://www.finetechnology-ind.com/prod/detail/pub/1189924-28-4.html
Finetech	FT-0669067	http://www.finetechnology-ind.com/prod/detail/pub/29110-47-2.html
Hairui	HR141314	http://www.hairuichem.com/en/product/29110-47-2.html
Lab Network	LN01308386	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01308386
MedChem Express	HY-17416A	https://www.medchemexpress.com/guanfacine.html
Molcore	MC546722	https://www.molcore.com/product/29110-47-2
MuseChem	I003012	https://www.musechem.com/product/I003012.html
Smolecule	S576275	https://www.smolecule.com/products/s576275
Smolecule	S905071	https://www.smolecule.com/products/s905071
THE BioTek	bt-305246	https://www.thebiotek.com/product/others/bt-305246
Yuhao Chemical	RT3442	http://www.chemyuhao.com/29110-47-2.html

PubMed

Title	Date	PubMed
[Effect of 5-month guanfacine treatment on the renin-angiotensin-aldosterone system and some metabolic factors in patients with diabetes mellitus type II and hypertension].	1992 Nov 16-30	1305723
Pharmacological options for the treatment of Tourette's disorder.	2001	11772131
Respiratory pattern and hypoxic ventilatory response in mice functionally lacking alpha2A-adrenergic receptors.	2001	11729878
Pharmacokinetic and pharmacodynamic drug interactions in the treatment of attention-deficit hyperactivity disorder.	2001	11707061
Tourette syndrome: clinical characteristics and current management strategies.	2001	11393328
Alpha2A-adrenoceptor mediated tachypnea in awake goats.	2001 Apr	11282385
Effects of alpha(2)-adrenergic agonists on lipopolysaccharide-induced aqueous flare elevation in pigmented rabbits.	2001 May-Jun	11369369
Clonidine-induced nitric oxide-dependent vasorelaxation mediated by endothelial alpha(2)-adrenoceptor activation.	2001 Nov	11682443
Guanfacine treatment of cognitive impairment in schizophrenia.	2001 Sep	11522468
[Prescribing ritalin in combined modality management of hyperactivity with attention deficit].	2001 Sep-Oct	11760693
Effects of rilmenidine and guanfacine in acute renal denervated rats.	2002	12434513
Role of alpha 2-adrenoceptors and imidazoline receptors in the A5 region in the regulation of renal function in the rat.	2002	12434511
Testosterone dependence of salt-induced hypertension in Sabra rats and role of renal alpha(2)-adrenoceptor subtypes.	2002 Jan	11752095
Actions of alpha-2 noradrenergic agonists on spatial working memory and blood pressure in rhesus monkeys appear to be mediated by the same receptor subtype.	2002 Jul	12122489
Imidazoline drugs stabilize lysosomes and inhibit oxidative cytotoxicity in astrocytes.	2002 Mar 1	11864779
Seizures and extrapyramidal symptoms in a patient with Tourette's syndrome, Asperger's syndrome, and multiple sclerosis treated with interferon beta-1a and clomipramine.	2002 Nov	12432978
Epidemiology and toxicity of pediatric guanfacine exposures.	2002 Nov	12398562
Neuropsychiatric effects of guanfacine in children with mild tourette syndrome: a pilot study.	2002 Nov-Dec	12469007
Psychopharmacology of ADHD in adolescents.	2002 Oct	12270803
Mutation of the alpha2A-adrenoceptor impairs working memory performance and annuls cognitive enhancement by guanfacine.	2002 Oct 1	12351753
Enhancement of alpha-adrenoceptor-mediated responses in prostate of testosterone-treated rat.	2002 Oct 25	12398922
Assessing the molecular genetics of attention networks.	2002 Oct 4	12366871
Why have drug treatments been so disappointing?	2003	14521196
Non-stimulant treatment of attention-deficit/hyperactivity disorder.	2003 Apr	12679740
Stimulation of interleukin-12 production in mouse macrophages via activation of p38 mitogen-activated protein kinase by alpha2-adrenoceptor agonists.	2003 Apr 25	12706479
Frontotemporal dementias: clinical features and management.	2003 Jan	12567333
Pharmacological characterization of unique prazosin-binding sites in human kidney.	2003 Jul	12827214
The alpha2-adrenergic agonist guanfacine reduces excitability of human motor cortex through disfacilitation and increase of inhibition.	2003 Oct	14499745
Epinephrine reduces the nerve conduction blockage induced by high-potassium in mammalian sciatic nerve.	2003 Sep 5	12914987
Pharmacotherapy of pervasive developmental disorders in children and adolescents.	2004	15584771
The Leeds Evaluation of Efficacy of Detoxification Study (LEEDS) project: an open-label pragmatic randomised control trial comparing the efficacy of differing therapeutic agents for primary care detoxification from either street heroin or methadone [ISRCTN07752728].	2004 Apr 29	15117415
[Tourette syndrome: an analysis of its comorbidity and specific treatment].	2004 Feb	15011166
The alpha(2A)-adrenergic agonist guanfacine improves visuomotor associative learning in monkeys.	2004 Jan	12931141
Evidence-based pharmacotherapy for attention-deficit hyperactivity disorder.	2004 Mar	14733627
Loss of glutamatergic pyramidal neurons in frontal and temporal cortex resulting from attenuation of FGFR1 signaling is associated with spontaneous hyperactivity in mice.	2004 Mar 3	14999075
Potential noradrenergic targets for cognitive enhancement in schizophrenia.	2004 May	15115947
Noradrenergic alpha-2 agonists have anxiolytic-like actions on stress-related behavior and mesoprefrontal dopamine biochemistry.	2004 Nov 19	15494168
Methylphenidate an effective treatment for ADHD?	2004 Oct	15628613
Mania induction associated with atomoxetine.	2004 Oct	15349024
Alpha2 adrenergic agonists for the management of opioid withdrawal.	2004 Oct 18	15495025
Clonidine and guanfacine-induced antinociception in visceral pain: possible role of alpha 2/I2 binding sites.	2004 Oct 6	15464067
Aripiprazole in children and adolescents: clinical experience.	2005 Jul	16159529
G-protein-coupled alpha2A-adrenoreceptor agonists differentially alter citrus leaf and fruit abscission by affecting expression of ACC synthase and ACC oxidase.	2005 Jul	15928018
Yohimbine disrupts prepulse inhibition in rats via action at 5-HT1A receptors, not alpha2-adrenoceptors.	2005 Jul	15719216
An open-label, prospective study of guanfacine in children with ADHD and tic disorders.	2005 Nov	16856436
Recent pharmacologic updates.	2005 Oct	16262586
Central sympathetic inhibition augments sleep-related ultradian rhythm of parasympathetic tone in patients with chronic heart failure.	2005 Sep	16127185
Mechanism of action of agents used in attention-deficit/hyperactivity disorder.	2006	16961428
Syncope in children with Tourette's syndrome treated with guanfacine.	2006 Mar	16229000
Differential noradrenergic influence on seizure expression in genetically Fast and Slow kindling rat strains during massed trial stimulation of the amygdala.	2007 Feb	17027042

Patents

Sample Use Guides

In Vivo Use Guide

Usual Adult Dose for Hypertension Initial dose: 1 mg orally once a day at bedtime; may increase to 2 mg once a day if satisfactory result not achieved after 3 to 4 weeks. Usual Pediatric Dose for Attention Deficit Disorder 6 YEARS TO LESS THAN 18 YEARS: Initial dose: 1 mg orally once a day, either in the morning or evening, at approximately the same time each day; may adjust in increments of no more than 1 mg/week. Recommended target dose: 0.05 to 0.12 mg/kg/day (total daily dose between 1 and 7 mg) once a day, depending on clinical response and tolerability Maximum dose: 6 to 12 years: Doses above 4 mg/day have not been evaluated; 13 to 17 years: Doses above 7 mg/day have not been evaluated.

Route of Administration: Oral

In Vitro Use Guide

Guanfacine and clonidine at relatively high concentrations (10(-6)-10(-4) M) produced contractions of the rat vas deferens which were antagonized by prazosin.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 01:41:57 GMT 2023` Edited by `admin` on `Sat Dec 16 01:41:57 GMT 2023`
Record UNII	48412X0J21
Record Status	`Validated (UNII)`
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Name

Type

Language

ETIGUANFACINE

Official Name

English

Etiguanfacine [WHO-DD]

Common Name

English

SSP-1871

Code

English

CARBAMIC ACID, N-(((2-(2,6-DICHLOROPHENYL)ACETYL)AMINO)IMINOMETHYL)-, ETHYL ESTER

Systematic Name

English

etiguanfacine [INN]

Common Name

English

ETIGUANFACINE [USAN]

Common Name

English

Ethyl {[2-(2,6-dichlorophenyl)acetyl]carbamimidoyl}carbamate

Systematic Name

English

Code System Code Type Description

ChEMBL

CHEMBL3039532