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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	Orphan
Oct. 27, 1986	FDA	PROMIUS PHARMA
March 30, 2017	PMDA	Shionogi & Co., Ltd.

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
Product substitution issue	126.72	26.41	39	2014	14018	50589053
Aggression	81.33	26.41	31	2022	21085	50581986
Somnolence	62.54	26.41	51	2002	154934	50448137
Abnormal behaviour	51.89	26.41	22	2031	19636	50583435
Impulsive behaviour	51.85	26.41	12	2041	1446	50601625
Intentional overdose	49.34	26.41	31	2022	62473	50540598
Psychomotor hyperactivity	44.39	26.41	16	2037	9285	50593786
Suicidal ideation	42.53	26.41	27	2026	55358	50547713
Product administered to patient of inappropriate age	40.13	26.41	11	2042	2619	50600452
Bradycardia	36.48	26.41	26	2027	64400	50538671
Atrioventricular dissociation	32.92	26.41	6	2047	220	50602851
Irritability	32.68	26.41	18	2035	28408	50574663
Educational problem	29.82	26.41	6	2047	373	50602698
Sinus arrhythmia	26.92	26.41	7	2046	1362	50601709

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	354.58	31.33	105	4255	9067	29561100
Aggression	246.83	31.33	115	4245	35426	29534741
Agitation	121.64	31.33	82	4278	51222	29518945
Psychomotor hyperactivity	115.51	31.33	44	4316	8169	29561998
Abnormal behaviour	112.97	31.33	59	4301	23068	29547099
Irritability	101.06	31.33	54	4306	22098	29548069
Tic	93.05	31.33	26	4334	1809	29568358
Impulsive behaviour	87.08	31.33	25	4335	1918	29568249
Somnolence	80.01	31.33	83	4277	93872	29476295
Drug ineffective	79.19	31.33	168	4192	363002	29207165
Bradycardia	68.84	31.33	65	4295	65564	29504603
Anger	56.62	31.33	29	4331	10861	29559306
Educational problem	53.66	31.33	13	4347	514	29569653
Dystonia	50.79	31.33	26	4334	9723	29560444
Disturbance in attention	50.06	31.33	34	4326	21390	29548777
Brugada syndrome	49.97	31.33	13	4347	688	29569479
Insomnia	44.71	31.33	60	4300	88701	29481466
Negativism	42.05	31.33	10	4350	365	29569802
Product quality issue	41.41	31.33	27	4333	15868	29554299
Sinus bradycardia	41.16	31.33	24	4336	11579	29558588
Emotional disorder	40.53	31.33	18	4342	4913	29565254
Suicidal ideation	39.46	31.33	36	4324	34680	29535487
Attention deficit hyperactivity disorder	38.95	31.33	14	4346	2203	29567964
Affective disorder	37.73	31.33	15	4345	3111	29567056
Sinus arrest	36.59	31.33	12	4348	1435	29568732
Product administered to patient of inappropriate age	36.49	31.33	14	4346	2641	29567526
Defiant behaviour	36.18	31.33	5	4355	4	29570163
Anxiety	35.98	31.33	53	4307	85312	29484855
Hallucination	35.27	31.33	38	4322	44674	29525493
Disturbance in social behaviour	34.68	31.33	12	4348	1690	29568477
Drug dose titration not performed	34.65	31.33	8	4352	256	29569911
Autism spectrum disorder	32.60	31.33	12	4348	2020	29568147
Priapism	32.50	31.33	15	4345	4473	29565694

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	389.67	24.47	116	5368	17745	64475503
Aggression	305.76	24.47	123	5361	46109	64447139
Psychomotor hyperactivity	140.48	24.47	51	5433	14400	64478848
Impulsive behaviour	131.73	24.47	33	5451	2630	64490618
Abnormal behaviour	122.75	24.47	59	5425	33563	64459685
Agitation	114.85	24.47	79	5405	88288	64404960
Irritability	111.91	24.47	57	5427	36689	64456559
Bradycardia	98.54	24.47	81	5403	118138	64375110
Tic	98.05	24.47	26	5458	2593	64490655
Somnolence	86.31	24.47	96	5388	203549	64289699
Educational problem	76.24	24.47	15	5469	389	64492859
Suicidal ideation	60.45	24.47	48	5436	66494	64426754
Anger	58.54	24.47	28	5456	15713	64477535
Intentional overdose	55.51	24.47	52	5432	89892	64403356
Brugada syndrome	51.52	24.47	13	5471	1065	64492183
Disturbance in attention	46.95	24.47	34	5450	41040	64452208
Sinus bradycardia	46.01	24.47	27	5457	22866	64470382
Electrocardiogram QT prolonged	45.33	24.47	44	5440	79404	64413844
Hypotension	44.40	24.47	99	5385	380875	64112373
Priapism	42.27	24.47	15	5469	3955	64489293
Dystonia	39.90	24.47	23	5461	18842	64474406
Mood swings	38.82	24.47	22	5462	17446	64475802
Autism spectrum disorder	38.37	24.47	10	5474	931	64492317
Defiant behaviour	37.09	24.47	5	5479	8	64493240
Product administered to patient of inappropriate age	36.49	24.47	14	5470	4587	64488661
Drug ineffective	36.36	24.47	154	5330	840093	63653155
Sedation	35.70	24.47	29	5455	41433	64451815
Attention deficit hyperactivity disorder	35.42	24.47	12	5472	2758	64490490
Disturbance in social behaviour	35.08	24.47	13	5471	3874	64489374
Affective disorder	34.91	24.47	15	5469	6565	64486683
Product quality issue	34.81	24.47	25	5459	29774	64463474
Sinus arrest	34.13	24.47	12	5472	3078	64490170
Overdose	32.93	24.47	53	5431	159513	64333735
Insomnia	32.02	24.47	59	5425	197777	64295471
Drug dose titration not performed	31.47	24.47	8	5476	675	64492573
Emotional disorder	31.08	24.47	17	5467	12590	64480658
Hallucination	30.18	24.47	34	5450	72754	64420494
Homicidal ideation	29.79	24.47	11	5473	3246	64490002
Hyperammonaemia	29.06	24.47	15	5469	9889	64483359
Tachycardia	28.59	24.47	48	5436	149531	64343717
Lethargy	26.90	24.47	32	5452	72562	64420686
Atrioventricular dissociation	26.31	24.47	6	5478	319	64492929

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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 1MG BASE	INTUNIV	TAKEDA PHARMS USA	N022037	Sept. 2, 2009	RX	TABLET, EXTENDED RELEASE	ORAL	6811794	July 4, 2022	TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER
EQ 2MG BASE	INTUNIV	TAKEDA PHARMS USA	N022037	Sept. 2, 2009	RX	TABLET, EXTENDED RELEASE	ORAL	6811794	July 4, 2022	TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER
EQ 3MG BASE	INTUNIV	TAKEDA PHARMS USA	N022037	Sept. 2, 2009	RX	TABLET, EXTENDED RELEASE	ORAL	6811794	July 4, 2022	TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER
EQ 4MG BASE	INTUNIV	TAKEDA PHARMS USA	N022037	Sept. 2, 2009	RX	TABLET, EXTENDED RELEASE	ORAL	6811794	July 4, 2022	TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER

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	0228-2851	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	0228-2855	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	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	16714-192	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 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 Extended-Release	HUMAN PRESCRIPTION DRUG LABEL	1	24979-533	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	27 sections
Guanfacine Extended-Release	HUMAN PRESCRIPTION DRUG LABEL	1	24979-534	TABLET, EXTENDED RELEASE	2 mg	ORAL	ANDA	27 sections
Guanfacine Extended-Release	HUMAN PRESCRIPTION DRUG LABEL	1	24979-536	TABLET, EXTENDED RELEASE	3 mg	ORAL	ANDA	27 sections
Guanfacine Extended-Release	HUMAN PRESCRIPTION DRUG LABEL	1	24979-538	TABLET, EXTENDED RELEASE	4 mg	ORAL	ANDA	27 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	29300-458	TABLET	1 mg	ORAL	ANDA	21 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	29300-459	TABLET	2 mg	ORAL	ANDA	21 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42291-310	TABLET	1 mg	ORAL	ANDA	20 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42291-310	TABLET	1 mg	ORAL	ANDA	20 sections
Guanfacine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42291-311	TABLET	2 mg	ORAL	ANDA	20 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-324	TABLET, EXTENDED RELEASE	1 mg	ORAL	ANDA	29 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-325	TABLET, EXTENDED RELEASE	2 mg	ORAL	ANDA	29 sections
guanfacine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-326	TABLET, EXTENDED RELEASE	3 mg	ORAL	ANDA	29 sections