Guanfacine

Identification

Summary

Guanfacine is an alpha-2A adrenergic receptor agonist used to treat ADHD.

Brand Names

Intuniv, Tenex

Generic Name

Guanfacine

DrugBank Accession Number

DB01018

Background

Guanfacine, or BS 100-141,^8,9 is a selective alpha-A2 adrenergic receptor agonist initially indicated for the treatment of hypertension¹⁰ but is now indicated as an extended release tablet for the treatment of ADHD.¹¹ Guanfacine was first described in the literature in 1974.⁹

Guanfacine was granted FDA approval on 27 October 1986.¹⁰

Type

Small Molecule

Groups

Approved, Investigational

Structure

Similar Structures

Weight: Average: 246.093
Monoisotopic: 245.012267339
Chemical Formula: C₉H₉Cl₂N₃O

Synonyms

Guanfacina
Guanfacine
Guanfacinum

External IDs

SPD 503

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Pharmacology

Indication

Guanfacine is indicated alone or as an adjunct with stimulants to treat ADHD.¹¹

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Associated Conditions

Indication Type	Indication	Approval Level	Age Group	Patient Characteristics	Dose Form
Adjunct therapy in management of	Attention deficit disorder with hyperactivity (adhd)	••••••••••••	••••••••••• ••••••••		••••••• •••••••• •••••••
Management of	Attention deficit disorder with hyperactivity (adhd)	••••••••••••	••••••••••• ••••••••	••••••••• •• •••••••••••	••••••• •••••••• •••••••
Management of	Hypertension	••• •••••			••••••
Prophylaxis of	Migraine	••• •••••
Management of	Tourette syndrome	••• •••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Guanfacine is a selective alpha-2A adrenergic receptor agonist but it is unclear how this translates to the treatment of ADHD.¹¹ It has a long duration of action as it is given once daily and a wide therapeutic window as fatal overdoses have not been described in literature.¹¹ Patients should be counselled regarding the risk of hypotension, bradycardia, and syncope.¹¹

Mechanism of action

Guanfacine is a selective alpha-2A adrenergic receptor agonist, which reduces the effects of the sympathetic nervous system on the heart and circulatory system.¹¹ The link between guanfacine’s molecular mechanism and it’s effect on the treatment of ADHD has not been determined.¹¹

Target	Actions	Organism
AAlpha-2A adrenergic receptor	agonist	Humans
UAlpha-2B adrenergic receptor	binder	Humans

Absorption

Guanfacine is 80% orally bioavailable.¹

1mg immediate release oral guanfacine reaches a C_max of 2.5±0.6ng/mL with a T_max of 3.0h and an AUC of 56±15ng*h/mL.¹¹ 1mg extended release oral guanfacine reaches a C_max of 1.0±0.3ng/mL with a T_max of 6.0h and an AUC of 32±9ng*h/mL.¹¹

In adults, a 4mg oral extended release dose reaches a C_max of 3.58±1.39ng/mL with a T_max of 5.5h; in children, a 2mg oral extended relsease dose reaches a C_max of 2.6±1.03ng/mL with a T_max of 4.98h; in adolescents, a 2mg oral extended release dose reaches a C_max of 1.7±0.43ng/mL with a T_max of 4.96h.⁷

Volume of distribution

Guanfacine has a volume of distribution of 6.3L/kg.¹

Protein binding

Guanfacine is approximately 70% protein bound in serum.^1,11

Metabolism

Guanfacine is oxidized by CYP3A4⁶ to it's main metabolite, 3-hydroxyguanfacine.⁴ 3-hydroxyguanfacine is then either glucuronidated or sulphated.^4,5

Hover over products below to view reaction partners

Guanfacine
- 3-hydroxyguanfacine
  - Guanfacine 3-sulfate
  - Guanfacine 3-glucuronide

Route of elimination

Guanfacine is 57.0±32.0% eliminated in the urine in patients with normal renal function.² Patients with a glomerular filtration rate (GFR) of 10-30mL/min eliminate 14.0±9.0% of a dose in the urine, while patients with a GFR of <1mL/min eliminate 7.5±2.4% of a dose in the urine.²

Half-life

Guanfacine has a half life of 17 hours, but this may range from 10-30 hours.¹ The half life is largely independant of renal function.²

Clearance

Guanfacine has a total body cleraance of 360±262mL/min and a renal clearance of 233±245mL/min in patients with normal renal function. Patients with a glomerular filtration rate (GFR) of 10-30mL/min had a total body clearance of 308±274mL/min and a renal clearance of 34±22mL/min.² Patients with a GFR of <1mL/min had a total body clearance of 257±187mL/min and a renal clearance of 18±15mL/min.²

Adverse Effects

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Toxicity

The oral LD₅₀ in rats is 142mg/kg and 15.3mg/kg in mice.¹² The subcutaneous LD₅₀ in rats is 114mg/kg and 46mg/kg in mice.¹²

Patients experiencing and overdose may present with hypotension, drowsiness, lethargy, and bradycardia.¹¹ Overdose should be managed by first calling local poison control. Patients may require intravenous saline to maintain blood pressure.³

Pathways

Not Available

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Interactions

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This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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1,2-Benzodiazepine	The risk or severity of CNS depression can be increased when Guanfacine is combined with 1,2-Benzodiazepine.
Abacavir	Guanfacine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abaloparatide	The risk or severity of adverse effects can be increased when Guanfacine is combined with Abaloparatide.
Abametapir	The serum concentration of Guanfacine can be increased when it is combined with Abametapir.
Acebutolol	The therapeutic efficacy of Guanfacine can be decreased when used in combination with Acebutolol.

Food Interactions

Avoid alcohol.
Do not take with or immediately after a high-fat meal. High fat meals increase drug exposure.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Guanfacine hydrochloride	PML56A160O	29110-48-3	DGFYECXYGUIODH-UHFFFAOYSA-N

Product Images

International/Other Brands

Estulic (Egis)

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Intuniv	Tablet, extended release	2 mg	Oral	Takeda Pharmaceuticals International Ag Ireland Branch	2016-09-08	Not applicable
Intuniv	Tablet, extended release	1 mg	Oral	Takeda Pharmaceuticals International Ag Ireland Branch	2016-09-08	Not applicable
Intuniv	Tablet, extended release	4 mg/1	Oral	Takeda Pharmaceuticals America, Inc.	2009-09-02	Not applicable
Intuniv	Tablet, extended release	1 mg/1	Oral	Takeda Pharmaceuticals America, Inc.	2009-09-02	Not applicable
Intuniv	Tablet, extended release	3 mg	Oral	Takeda Pharmaceuticals International Ag Ireland Branch	2016-09-08	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Ag-guanfacine XR	Tablet, extended release	3 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Ag-guanfacine XR	Tablet, extended release	1 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Ag-guanfacine XR	Tablet, extended release	2 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Ag-guanfacine XR	Tablet, extended release	4 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Apo-guanfacine XR	Tablet, extended release	4 mg	Oral	Apotex Corporation	2022-01-31	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Intuniv	Guanfacine hydrochloride (1 mg/1) + Guanfacine hydrochloride (2 mg/1)	Kit	Oral	Shire US Manufacturing Inc.	2009-09-02	2011-06-15
Intuniv	Guanfacine hydrochloride (1 mg/1) + Guanfacine hydrochloride (2 mg/1)	Kit; Tablet, extended release	Oral	Takeda Pharmaceuticals America, Inc.	2009-09-02	2015-10-29
Intuniv	Guanfacine hydrochloride (1 mg/1) + Guanfacine hydrochloride (2 mg/1)	Kit	Oral	Shire US Manufacturing Inc.	2009-09-02	2011-06-15
Intuniv	Guanfacine hydrochloride (1 mg/1) + Guanfacine hydrochloride (2 mg/1)	Kit; Tablet, extended release	Oral	Takeda Pharmaceuticals America, Inc.	2009-09-02	2015-10-29

Chemical Identifiers

UNII: 30OMY4G3MK
CAS number: 29110-47-2
InChI Key: INJOMKTZOLKMBF-UHFFFAOYSA-N
InChI: InChI=1S/C9H9Cl2N3O/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13/h1-3H,4H2,(H4,12,13,14,15)
IUPAC Name: N-carbamimidoyl-2-(2,6-dichlorophenyl)acetamide
SMILES: NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl

References

Synthesis Reference

U.S. Patent 3,632,645.

General References

Cruz MP: Guanfacine Extended-Release Tablets (Intuniv), a Nonstimulant Selective Alpha(2A)-Adrenergic Receptor Agonist For Attention-Deficit/Hyperactivity Disorder. P T. 2010 Aug;35(8):448-51. [Article]
Kirch W, Kohler H, Braun W: Elimination of guanfacine in patients with normal and impaired renal function. Br J Clin Pharmacol. 1980;10 Suppl 1:33S-35S. doi: 10.1111/j.1365-2125.1980.tb04902.x. [Article]
Minns AB, Clark RF, Schneir A: Guanfacine overdose resulting in initial hypertension and subsequent delayed, persistent orthostatic hypotension. Clin Toxicol (Phila). 2010 Feb;48(2):146-8. doi: 10.3109/15563650903505174. [Article]
Kiechel JR: Pharmacokinetics and metabolism of guanfacine in man: a review. Br J Clin Pharmacol. 1980;10 Suppl 1:25S-32S. doi: 10.1111/j.1365-2125.1980.tb04901.x. [Article]
Guerret M, Julien-Larose C, Kiechel JR, Lavene D: Determination of 3-hydroxy-guanfacine in biological fluids by electron-capture gas-liquid chromatography. J Chromatogr. 1982 Dec 10;233:181-92. doi: 10.1016/s0378-4347(00)81745-4. [Article]
Inoue Y, Morita H, Nozawa K, Kanazu T: Metabolite profiling of guanfacine in plasma and urine of healthy Japanese subjects after oral administration of guanfacine extended-release tablets. Biopharm Drug Dispos. 2019 Sep;40(8):282-293. doi: 10.1002/bdd.2201. Epub 2019 Aug 7. [Article]
Martin P, Satin L, Vince BD, Padilla AF, White C, Corcoran M, Stevenson A, Ermer J: Pharmacokinetics and pharmacodynamics of guanfacine extended release in adolescents aged 13-17 years with attention-deficit/hyperactivity disorder. Clin Pharmacol Drug Dev. 2014 Jul;3(4):252-61. doi: 10.1002/cpdd.124. Epub 2014 May 17. [Article]
Dubach UC, Huwyler R, Radielovic P, Singeisen M: A new centrally action antihypertensive agent guanfacine (BS 100-141). Arzneimittelforschung. 1977;27(3):674-6. [Article]
Scholtysik G: Proceedings: Inhibition of effects of accelerator nerve stimulation in cats and rabbits by BS 100-141 and guanabenz. Naunyn Schmiedebergs Arch Pharmacol. 1974;282(Suppl):suppl 282:R86. [Article]
FDA Approved Drug Products: Tenex Guanfacine Hydrochloride Oral Tablets (Discontinued) [Link]
FDA Approved Drug Products: Intuniv Guanfacine Hydrochloride Extended Release Oral Tablets [Link]
Cayman Chemical: Guanfacine MSDS [Link]

External Links

Human Metabolome Database: HMDB0015153
KEGG Drug: D08031
KEGG Compound: C07037
PubChem Compound: 3519
PubChem Substance: 46506169
ChemSpider: 3399
BindingDB: 81984
RxNav: 40114
ChEBI: 5558
ChEMBL: CHEMBL862
ZINC: ZINC000003872738
Therapeutic Targets Database: DAP000900
PharmGKB: PA449825
Guide to Pharmacology: GtP Drug Page
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
PDRhealth: PDRhealth Drug Page
Wikipedia: Guanfacine

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Chronic Pain	1
4	Completed	Basic Science	Attention Deficit Hyperactivity Disorder (ADHD)	1
4	Completed	Treatment	ADHD - Inattentive Type / Childhood Aggression / Defiant Disorder, Oppositional / Intermittent Explosive Disorder	1
4	Completed	Treatment	Adult Attention Deficit Hyperactivity Disorder (ADHD)	1
4	Completed	Treatment	Attention Deficit Hyperactivity Disorder (ADHD)	5

Pharmacoeconomics

Manufacturers

Shire development inc
Amneal pharmaceutical
Mikah pharma llc
Mylan pharmaceuticals inc
Watson laboratories inc
Promius pharma llc

Packagers

Actavis Group
Advanced Pharmaceutical Services Inc.
Amerisource Health Services Corp.
Amneal Pharmaceuticals
Atlantic Biologicals Corporation
Cardinal Health
Industriale Chimica S.R.L.
Major Pharmaceuticals
Murfreesboro Pharmaceutical Nursing Supply
Mylan
Par Pharmaceuticals
Patheon Inc.
Pharmaceutical Utilization Management Program VA Inc.
Pharmedix
Physicians Total Care Inc.
Promius Pharma
Qualitest
Resource Optimization and Innovation LLC
Shire Inc.
Southwood Pharmaceuticals
Watson Pharmaceuticals

Dosage Forms

Form	Route	Strength
Tablet, extended release	Oral
Tablet, extended release	Oral	3 mg/1
Tablet, extended release	Oral	4 mg/1
Tablet	Oral	1 mg/1
Tablet	Oral	2 mg/1
Tablet, film coated, extended release	Oral	1 mg/1
Tablet, film coated, extended release	Oral	2 mg/1
Tablet, film coated, extended release	Oral	3 mg/1
Tablet, film coated, extended release	Oral	4 mg/1
Kit	Oral
Kit; tablet, extended release	Oral
Tablet, extended release	Oral	1 mg/1
Tablet, extended release	Oral	2 mg/1
Tablet, extended release	Oral	1 mg
Tablet, extended release	Oral	2 mg
Tablet, extended release	Oral	3 mg
Tablet, extended release	Oral	4 mg

Prices

Unit description	Cost	Unit
Intuniv 1 mg 24 Hour tablet	5.72USD	tablet
Intuniv 2 mg 24 Hour tablet	5.72USD	tablet
Intuniv 3 mg 24 Hour tablet	5.72USD	tablet
Intuniv 4 mg 24 Hour tablet	5.72USD	tablet
Intuniv er 1 mg tablet	5.5USD	tablet
Intuniv er 2 mg tablet	5.5USD	tablet
Intuniv er 3 mg tablet	5.5USD	tablet
Intuniv er 4 mg tablet	5.5USD	tablet
Tenex 2 mg tablet	4.3USD	tablet
Tenex 1 mg tablet	2.9USD	tablet
Guanfacine HCl 2 mg tablet	1.22USD	tablet
Guanfacine 2 mg tablet	1.18USD	tablet
Guanfacine HCl 1 mg tablet	0.91USD	tablet
Guanfacine 1 mg tablet	0.87USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US5854290	Yes	1998-12-29	2016-03-21
US6811794	Yes	2004-11-02	2023-01-04
US6287599	Yes	2001-09-11	2021-06-20

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	213-216	U.S. Patent 3,632,645.
water solubility	1mg/mL	FDA Label
logP	0.857	ChemSpider

Predicted Properties

Property	Value	Source
Water Solubility	0.139 mg/mL	ALOGPS
logP	2.28	ALOGPS
logP	1.74	Chemaxon
logS	-3.2	ALOGPS
pKa (Strongest Acidic)	11.64	Chemaxon
pKa (Strongest Basic)	8.65	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	3	Chemaxon
Hydrogen Donor Count	3	Chemaxon
Polar Surface Area	78.97 Å²	Chemaxon
Rotatable Bond Count	2	Chemaxon
Refractivity	69.63 m³·mol^-1	Chemaxon
Polarizability	22.44 Å³	Chemaxon
Number of Rings	1	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9313
Blood Brain Barrier	+	0.9567
Caco-2 permeable	-	0.5101
P-glycoprotein substrate	Non-substrate	0.6778
P-glycoprotein inhibitor I	Non-inhibitor	0.8782
P-glycoprotein inhibitor II	Non-inhibitor	0.9833
Renal organic cation transporter	Non-inhibitor	0.6443
CYP450 2C9 substrate	Non-substrate	0.7572
CYP450 2D6 substrate	Non-substrate	0.7948
CYP450 3A4 substrate	Non-substrate	0.6475
CYP450 1A2 substrate	Non-inhibitor	0.9046
CYP450 2C9 inhibitor	Non-inhibitor	0.8893
CYP450 2D6 inhibitor	Inhibitor	0.8931
CYP450 2C19 inhibitor	Non-inhibitor	0.7376
CYP450 3A4 inhibitor	Non-inhibitor	0.831
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.6619
Ames test	Non AMES toxic	0.7223
Carcinogenicity	Non-carcinogens	0.8107
Biodegradation	Not ready biodegradable	0.9843
Rat acute toxicity	2.7408 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9677
hERG inhibition (predictor II)	Non-inhibitor	0.9285

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-0a4l-5900000000-766dd9f92ab525fb3d7f
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0002-0090000000-50a2b041228c1ef7c8d4
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0udi-0190000000-14ce6bf26b6072d3b6b3
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0006-9100000000-004c9a6dc06583cf69a5
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0006-9100000000-255a7a3dcd356cc46e1b
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0006-9000000000-0c3e14d9066e2d3fd1a9
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0006-9500000000-6e112e5aeb6150468df0
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	147.3237162	predicted	DarkChem Lite v0.1.0
[M-H]-	147.56963	predicted	DeepCCS 1.0 (2019)
[M+H]+	147.6717162	predicted	DarkChem Lite v0.1.0
[M+H]+	149.92763	predicted	DeepCCS 1.0 (2019)
[M+Na]+	147.1192162	predicted	DarkChem Lite v0.1.0
[M+Na]+	156.22723	predicted	DeepCCS 1.0 (2019)

Targets

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Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	50.3	N/A	N/A	A28265
Ki (nM)	93.33	N/A	N/A	A28266

Details1. Alpha-2A adrenergic receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

General Function: Thioesterase binding
Specific Function: Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name: ADRA2A
Uniprot ID: P08913
Uniprot Name: Alpha-2A adrenergic receptor
Molecular Weight: 48956.275 Da

References

Avery RA, Franowicz JS, Studholme C, van Dyck CH, Arnsten AF: The alpha-2A-adrenoceptor agonist, guanfacine, increases regional cerebral blood flow in dorsolateral prefrontal cortex of monkeys performing a spatial working memory task. Neuropsychopharmacology. 2000 Sep;23(3):240-9. [Article]
Sagvolden T: The alpha-2A adrenoceptor agonist guanfacine improves sustained attention and reduces overactivity and impulsiveness in an animal model of Attention-Deficit/Hyperactivity Disorder (ADHD). Behav Brain Funct. 2006 Dec 15;2:41. [Article]
Yuan R, Wu Z, Kostenyuk IA, Burns JK: G-protein-coupled alpha2A-adrenoreceptor agonists differentially alter citrus leaf and fruit abscission by affecting expression of ACC synthase and ACC oxidase. J Exp Bot. 2005 Jul;56(417):1867-75. Epub 2005 May 31. [Article]
Birnbaum SG, Podell DM, Arnsten AF: Noradrenergic alpha-2 receptor agonists reverse working memory deficits induced by the anxiogenic drug, FG7142, in rats. Pharmacol Biochem Behav. 2000 Nov;67(3):397-403. [Article]
Millan MJ: Evidence that an alpha 2A-adrenoceptor subtype mediates antinociception in mice. Eur J Pharmacol. 1992 May 14;215(2-3):355-6. [Article]
Stahl SM: Mechanism of action of alpha 2A-adrenergic agonists in attention-deficit/hyperactivity disorder with or without oppositional symptoms. J Clin Psychiatry. 2010 Mar;71(3):223-4. doi: 10.4088/JCP.09bs05899pur. [Article]
FDA Approved Drug Products: Intuniv Guanfacine Hydrochloride Extended Release Oral Tablets [Link]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	1020	N/A	N/A	A28265
Ki (nM)	1380.38	N/A	N/A	A28266

Details2. Alpha-2B adrenergic receptor

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Binder
Curator comments: Guanfacine binds to Alpha-2B adrenergic receptors with such low affinity that it is not clinically relevant.

General Function: Epinephrine binding
Specific Function: Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name: ADRA2B
Uniprot ID: P18089
Uniprot Name: Alpha-2B adrenergic receptor
Molecular Weight: 49565.8 Da

References

Uhlen S, Wikberg JE: Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound. Eur J Pharmacol. 1991 Sep 17;202(2):235-43. [Article]

Enzymes

Details1. Cytochrome P450 2C19

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name: CYP2C19
Uniprot ID: P33261
Uniprot Name: Cytochrome P450 2C19
Molecular Weight: 55930.545 Da

References

Clement B, Demesmaeker M: Microsomal catalyzed N-hydroxylation of guanfacine and reduction of N-hydroxyguanfacine. Arch Pharm (Weinheim). 1997 Oct;330(9-10):303-6. [Article]
Guillouzo A, Le Bigot JF, Guguen-Guillouzo C, Kiechel JR: Presence of phase I and phase II drug metabolizing enzymes in cultured human foetal hepatocytes. Biochem Pharmacol. 1982 Jul 15;31(14):2427-30. [Article]

Details2. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Clement B, Demesmaeker M: Microsomal catalyzed N-hydroxylation of guanfacine and reduction of N-hydroxyguanfacine. Arch Pharm (Weinheim). 1997 Oct;330(9-10):303-6. [Article]
Guillouzo A, Le Bigot JF, Guguen-Guillouzo C, Kiechel JR: Presence of phase I and phase II drug metabolizing enzymes in cultured human foetal hepatocytes. Biochem Pharmacol. 1982 Jul 15;31(14):2427-30. [Article]
FDA Approved Drug Products: Intuniv Guanfacine Hydrochloride Extended Release Oral Tablets [Link]

Transporters

Details1. Multidrug and toxin extrusion protein 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Monovalent cation:proton antiporter activity
Specific Function: Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name: SLC47A1
Uniprot ID: Q96FL8
Uniprot Name: Multidrug and toxin extrusion protein 1
Molecular Weight: 61921.585 Da

References

FDA Approved Drug Products: Intuniv Guanfacine Hydrochloride Extended Release Oral Tablets [Link]

Details2. Solute carrier family 22 member 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Secondary active organic cation transmembrane transporter activity
Specific Function: Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name: SLC22A1
Uniprot ID: O15245
Uniprot Name: Solute carrier family 22 member 1
Molecular Weight: 61153.345 Da

References

FDA Approved Drug Products: Intuniv Guanfacine Hydrochloride Extended Release Oral Tablets [Link]

Details3. Solute carrier family 22 member 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Quaternary ammonium group transmembrane transporter activity
Specific Function: Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name: SLC22A2
Uniprot ID: O15244
Uniprot Name: Solute carrier family 22 member 2
Molecular Weight: 62579.99 Da

References

FDA Approved Drug Products: Intuniv Guanfacine Hydrochloride Extended Release Oral Tablets [Link]

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55

Guanfacine

Identification

Structure for Guanfacine (DB01018)

Pharmacology

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Pharmacoeconomics

Properties

Spectra

Collision Cross Sections (CCS)

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Enzymes

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Transporters

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