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guanfacine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antihypertensives, guanidine derivatives	1343	29110-47-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: guanfacine guanfacine hydrochloride guanfacine HCl guanfacine monohydrochloride	A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. Molecular weight: 246.09 Formula: C9H9Cl2N3O CLOGP: 1.37 LIPINSKI: 0 HAC: 4 HDO: 3 TPSA: 78.97 ALOGS: -3.25 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

guanfacine
guanfacine hydrochloride
guanfacine HCl
guanfacine monohydrochloride

A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.

Molecular weight: 246.09
Formula: C9H9Cl2N3O
CLOGP: 1.37
LIPINSKI: 0
HAC: 4
HDO: 3
TPSA: 78.97
ALOGS: -3.25
ROTB: 2

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
3	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.35 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	81 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	5.60 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	4.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.28 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	15 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company
March 30, 2017	PMDA	Shionogi & Co., Ltd.
Oct. 27, 1986	FDA	PROMIUS PHARMA
Sept. 17, 2015	EMA	Takeda Pharmaceuticals International AG Ireland Branch

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intentional overdose	182.08	26.07	80	2650	74072	63412220
Product substitution issue	119.43	26.07	39	2691	15957	63470335
Aggression	79.76	26.07	32	2698	23466	63462826
Distributive shock	79.26	26.07	17	2713	1366	63484926
Somnolence	77.81	26.07	63	2667	178622	63307670
Bradycardia	72.85	26.07	43	2687	73184	63413108
Impulsive behaviour	66.04	26.07	15	2715	1568	63484724
Bradypnoea	54.01	26.07	15	2715	3535	63482757
Suicidal ideation	50.15	26.07	32	2698	62389	63423903
Abnormal behaviour	48.81	26.07	22	2708	21404	63464888
Psychomotor hyperactivity	48.58	26.07	18	2712	10645	63475647
Intentional self-injury	48.02	26.07	23	2707	25664	63460628
Sinus bradycardia	46.54	26.07	19	2711	14532	63471760
Cerebral disorder	41.85	26.07	13	2717	4513	63481779
Product administered to patient of inappropriate age	41.53	26.07	12	2718	3256	63483036
Hypotension	40.54	26.07	54	2676	272550	63213742
Electrocardiogram QT prolonged	39.28	26.07	27	2703	59503	63426789
Coma	37.38	26.07	27	2703	64337	63421955
Suicide attempt	34.11	26.07	25	2705	60893	63425399
Atrioventricular dissociation	32.57	26.07	6	2724	220	63486072
Irritability	32.48	26.07	19	2711	31675	63454617
Sinus arrhythmia	30.79	26.07	8	2722	1465	63484827
Educational problem	29.06	26.07	6	2724	400	63485892
Overdose	27.33	26.07	29	2701	115049	63371243

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product substitution issue	350.07	32.83	106	4983	9989	34941853
Aggression	300.24	32.83	135	4954	38829	34913013
Psychomotor hyperactivity	148.55	32.83	55	5034	9567	34942275
Agitation	142.59	32.83	94	4995	57305	34894537
Abnormal behaviour	120.69	32.83	63	5026	24906	34926936
Irritability	104.41	32.83	57	5032	24633	34927209
Impulsive behaviour	98.06	32.83	28	5061	2134	34949708
Tic	94.90	32.83	27	5062	2031	34949811
Somnolence	89.97	32.83	95	4994	111021	34840821
Drug ineffective	86.28	32.83	198	4891	456553	34495289
Bradycardia	76.65	32.83	73	5016	75345	34876497
Dystonia	62.96	32.83	31	5058	10814	34941028
Anger	60.28	32.83	31	5058	11853	34939989
Educational problem	52.99	32.83	13	5076	549	34951293
Brugada syndrome	48.41	32.83	13	5076	788	34951054
Electrocardiogram QT prolonged	48.06	32.83	43	5046	40909	34910933
Disturbance in attention	46.80	32.83	35	5054	25910	34925932
Autism spectrum disorder	46.25	32.83	16	5073	2280	34949562
Insomnia	45.14	32.83	65	5024	103842	34848000
Suicidal ideation	44.63	32.83	41	5048	40347	34911495
Product use issue	42.30	32.83	49	5040	63167	34888675
Emotional disorder	41.30	32.83	19	5070	5697	34946145
Negativism	41.07	32.83	10	5079	409	34951433
Attention deficit hyperactivity disorder	40.83	32.83	15	5074	2544	34949298
Product quality issue	40.00	32.83	27	5062	17008	34934834
Sinus bradycardia	38.97	32.83	24	5065	12939	34938903
Sinus arrest	38.47	32.83	13	5076	1727	34950115
Product administered to patient of inappropriate age	37.16	32.83	15	5074	3276	34948566
Distractibility	37.03	32.83	9	5080	365	34951477
Hallucination	36.27	32.83	41	5048	51457	34900385
Defiant behaviour	34.80	32.83	5	5084	7	34951835
Disturbance in social behaviour	33.84	32.83	12	5077	1839	34950003
Affective disorder	33.09	32.83	15	5074	4345	34947497

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product substitution issue	380.35	24.12	117	6601	20139	79717531
Aggression	350.03	24.12	139	6579	50819	79686851
Psychomotor hyperactivity	173.86	24.12	62	6656	16787	79720883
Intentional overdose	165.92	24.12	106	6612	105854	79631816
Impulsive behaviour	149.09	24.12	37	6681	2863	79734807
Bradycardia	140.03	24.12	105	6613	135452	79602218
Agitation	139.54	24.12	93	6625	99622	79638048
Abnormal behaviour	127.70	24.12	62	6656	36359	79701311
Irritability	117.65	24.12	61	6657	41083	79696587
Somnolence	109.74	24.12	117	6601	238864	79498806
Electrocardiogram QT prolonged	104.51	24.12	75	6643	90311	79647359
Tic	104.25	24.12	28	6690	2958	79734712
Sinus bradycardia	76.68	24.12	39	6679	25208	79712462
Educational problem	76.01	24.12	15	6703	399	79737271
Suicidal ideation	71.81	24.12	56	6662	76284	79661386
Anger	62.48	24.12	30	6688	17132	79720538
Distributive shock	56.67	24.12	17	6701	2670	79735000
Hypotension	56.14	24.12	118	6600	440199	79297471
Intentional self-injury	54.54	24.12	34	6684	32385	79705285
Brugada syndrome	49.85	24.12	13	6705	1225	79736445
Product administered to patient of inappropriate age	48.19	24.12	18	6700	5535	79732135
Dystonia	47.93	24.12	27	6691	21372	79716298
Overdose	46.72	24.12	67	6651	184139	79553531
Autism spectrum disorder	45.92	24.12	12	6706	1140	79736530
Disturbance in attention	42.90	24.12	35	6683	50766	79686904
Attention deficit hyperactivity disorder	41.12	24.12	14	6704	3295	79734375
Priapism	40.55	24.12	15	6703	4490	79733180
Drug ineffective	39.32	24.12	187	6531	1080726	78656944
Mood swings	38.96	24.12	23	6695	19857	79717813
Sedation	38.14	24.12	33	6685	51862	79685808
Bradypnoea	36.25	24.12	15	6703	6037	79731633
Sinus arrest	36.09	24.12	13	6705	3609	79734061
Emotional disorder	34.53	24.12	19	6699	14368	79723302
Defiant behaviour	33.12	24.12	5	6713	24	79737646
Product quality issue	32.10	24.12	25	6693	33915	79703755
Disturbance in social behaviour	32.09	24.12	13	6705	4957	79732713
Suicide attempt	31.73	24.12	37	6681	82895	79654775
Affective disorder	31.67	24.12	15	6703	8304	79729366
Product use issue	31.14	24.12	60	6658	209762	79527908
Distractibility	30.85	24.12	8	6710	737	79736933
Cerebral disorder	30.73	24.12	13	6705	5525	79732145
Hallucination	30.73	24.12	37	6681	85708	79651962
Hyperammonaemia	30.40	24.12	16	6702	11077	79726593
Tachycardia	30.35	24.12	54	6664	177714	79559956
Insomnia	30.32	24.12	65	6653	245105	79492565
Drug dose titration not performed	30.19	24.12	8	6710	802	79736868
Homicidal ideation	29.25	24.12	11	6707	3446	79734224
Coma	29.06	24.12	39	6679	100610	79637060
Pain	28.29	24.12	12	6706	703790	79033880
Lethargy	27.38	24.12	34	6684	81258	79656412
Atrioventricular dissociation	25.99	24.12	6	6712	340	79737330
Accidental overdose	24.78	24.12	23	6695	39558	79698112

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C02AC02	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, CENTRALLY ACTING Imidazoline receptor agonists
FDA MoA	N0000009918	Adrenergic alpha2-Agonists
FDA EPC	N0000175554	Central alpha-2 Adrenergic Agonist
CHEBI has role	CHEBI:176497	geroprotectors
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D000322	Adrenergic Agonists
MeSH PA	D058647	Adrenergic alpha-2 Receptor Agonists
MeSH PA	D000316	Adrenergic alpha-Agonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Attention deficit hyperactivity disorder	indication	406506008
Constipation	contraindication	14760008	DOID:2089
Myocardial infarction	contraindication	22298006	DOID:5844
Alcohol intoxication	contraindication	25702006
Orthostatic hypotension	contraindication	28651003
Dehydration	contraindication	34095006
Depressive disorder	contraindication	35489007
Low blood pressure	contraindication	45007003
End stage renal disease	contraindication	46177005	DOID:784
Bradycardia	contraindication	48867003
Cerebrovascular disease	contraindication	62914000	DOID:6713
Heart block	contraindication	233916004
Disease of liver	contraindication	235856003	DOID:409
Syncope	contraindication	271594007
Drowsy	contraindication	271782001
Chronic myocardial ischemia	contraindication	413844008	DOID:3393

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.71	acidic
pKa2	8.15	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	AGONIST	EC50	7.16	WOMBAT-PK	DRUG LABEL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.88	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.12	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	AGONIST	EC50	5.93	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.07	DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.26	DRUG MATRIX
Nischarin	Membrane receptor	Q9Y2I1	NISCH_HUMAN		Ki	7.72	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	AGONIST	EC50	5.68	WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	5.87	CHEMBL

External reference:

ID	Source
4019771	VUID
N0000147862	NUI
D00606	KEGG_DRUG
29110-48-3	SECONDARY_CAS_RN
4019438	VANDF
4019771	VANDF
C0079466	UMLSCUI
CHEBI:5558	CHEBI
CHEMBL862	ChEMBL_ID
DB01018	DRUGBANK_ID
CHEMBL1200494	ChEMBL_ID
D016316	MESH_DESCRIPTOR_UI
3519	PUBCHEM_CID
522	IUPHAR_LIGAND_ID
3999	INN_ID
30OMY4G3MK	UNII
203142	RXNORM
4809	MMSL
521	MMSL
6549	MMSL
d00717	MMSL
000650	NDDF
004497	NDDF
108553003	SNOMEDCT_US
108554009	SNOMEDCT_US
372507007	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5960	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5961	TABLET, EXTENDED RELEASE	2 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5963	TABLET, EXTENDED RELEASE	3 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5964	TABLET, EXTENDED RELEASE	4 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2850	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2850	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2851	TABLET, EXTENDED RELEASE	2 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2851	TABLET, EXTENDED RELEASE	2 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2853	TABLET, EXTENDED RELEASE	3 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2853	TABLET, EXTENDED RELEASE	3 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2855	TABLET, EXTENDED RELEASE	4 mg	ORAL	ANDA	28 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2855	TABLET, EXTENDED RELEASE	4 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0444	TABLET	1 mg	ORAL	ANDA	24 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-0453	TABLET	2 mg	ORAL	ANDA	24 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7140	TABLET	1 mg	ORAL	ANDA	24 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7140	TABLET	1 mg	ORAL	ANDA	24 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-190	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-190	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-191	TABLET, EXTENDED RELEASE	2 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-191	TABLET, EXTENDED RELEASE	2 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-192	TABLET, EXTENDED RELEASE	3 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-192	TABLET, EXTENDED RELEASE	3 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-193	TABLET, EXTENDED RELEASE	4 mg	ORAL	ANDA	28 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	16714-193	TABLET, EXTENDED RELEASE	4 mg	ORAL	ANDA	28 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	17856-0711	TABLET	1 mg	ORAL	ANDA	13 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	24658-730	TABLET	1 mg	ORAL	ANDA	24 sections
Guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	24658-731	TABLET	2 mg	ORAL	ANDA	24 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	24979-198	TABLET	1 mg	ORAL	ANDA	13 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	24979-199	TABLET	2 mg	ORAL	ANDA	13 sections
Guanfacine Extended-Release	HUMAN PRESCRIPTION DRUG LABEL	1	24979-533	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	28 sections