Entry

D00606                      Drug

Name

Guanfacine hydrochloride (JAN/USP);
Intuniv (TN);
Tenex (TN)

Product

INTUNIV (Takeda Pharmaceuticals America)

Generic

GUANFACINE HYDROCHLORIDE (A-S Medication Solutions), GUANFACINE (A-S Medication Solutions), GUANFACINE (Actavis Pharma), GUANFACINE (Actavis Pharma), GUANFACINE HYDROCHLORIDE (Amneal Pharmaceuticals LLC), GUANFACINE HYDROCHLORIDE (Amneal Pharmaceuticals of New York LLC), GUANFACINE EXTENDED-RELEASE (Apotex Corp.), GUANFACINE (AvKARE), GUANFACINE HYDROCHLORIDE (AvPAK), GUANFACINE (Bryant Ranch Prepack), GUANFACINE (Bryant Ranch Prepack), GUANFACINE (Bryant Ranch Prepack), GUANFACINE (Bryant Ranch Prepack), GUANFACINE (Epic Pharma), GUANFACINE (Golden State Medical Supply), GUANFACINE (Major Pharmaceuticals), GUANFACINE (NORTHSTAR RXLLC), GUANFACINE (Precision Dose), GUANFACINE (Proficient Rx LP), GUANFACINE (Proficient Rx LP), GUANFACINE (PuraCap Laboratories LLC dba Blu Pharmaceuticals), GUANFACINE (REMEDYREPACK), GUANFACINE (REMEDYREPACK), GUANFACINE (REMEDYREPACK), GUANFACINE HYDROCHLORIDE (REMEDYREPACK), GUANFACINE (Slate Run Pharmaceuticals), GUANFACINE (Sun Pharmaceutical Industries), GUANFACINE (TWi Pharmaceuticals), GUANFACINE HYDROCHLORIDE (American Health Packaging), GUANFACINE HYDROCHLORIDE (AvKARE), GUANFACINE HYDROCHLORIDE (NuCare Pharmaceuticals), GUANFACINE HYDROCHLORIDE (Unichem Pharmaceuticals (USA))

Formula

C9H9Cl2N3O. HCl

Exact mass

280.9889

Mol weight

282.5542

Structure

Simcomp

Class

Cardiovascular agent
DG01738  Centrally-acting antiadrenergic
DG01456  Adrenergic receptor agonist
  DG01450  alpha-Adrenergic receptor agonist
   DG01449  alpha2-Adrenergic receptor agonist
Metabolizing enzyme substrate
DG01633  CYP3A/CYP3A4 substrate
  DG02913  CYP3A4 substrate
DG02925  CYP3A5 substrate

Remark

Therapeutic category:

1179

ATC code:

C02AC02

Chemical structure group:

DG00250

Product (DG00250):

D00606<JP/US>

Efficacy

Antihypertensive, alpha2-Adrenergic receptor agonist

Disease

Attention deficit hyperactivity disorder [DS:H01895]
Hypertension [DS:H01633]

Comment

Guanidine derivative

Target

ADRA2A [HSA:150] [KO:K04138]

Pathway

hsa04022

cGMP-PKG signaling pathway

hsa04080

Neuroactive ligand-receptor interaction

Metabolism

Enzyme: CYP3A4 [HSA:1576], CYP3A5 [HSA:1577]

Interaction

Structure map

map07215

alpha-Adrenergic receptor agonists/antagonists

Brite

Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
C CARDIOVASCULAR SYSTEM
  C02 ANTIHYPERTENSIVES
   C02A ANTIADRENERGIC AGENTS, CENTRALLY ACTING
    C02AC Imidazoline receptor agonists
     C02AC02 Guanfacine
      D00606  Guanfacine hydrochloride (JAN/USP) <JP/US>
USP drug classification [BR:br08302]
Cardiovascular Agents
  Alpha-adrenergic Agonists
   Guanfacine
    D00606  Guanfacine hydrochloride (JAN/USP)
Central Nervous System Agents
  Attention Deficit Hyperactivity Disorder Agents, Non-amphetamines
   Guanfacine
    D00606  Guanfacine hydrochloride (JAN/USP)
Therapeutic category of drugs in Japan [BR:br08301]
1  Agents affecting nervous system and sensory organs
  11  Agents affecting central nervous system
   117  Psychotropics
    1179  Others
     D00606  Guanfacine hydrochloride (JAN/USP)
Drug groups [BR:br08330]
Cardiovascular agent
  DG01738  Centrally-acting antiadrenergic
   DG00250  Guanfacine
    D00606  Guanfacine hydrochloride
  DG01456  Adrenergic receptor agonist
   DG01450  alpha-Adrenergic receptor agonist
    DG01449  alpha2-Adrenergic receptor agonist
     DG00250  Guanfacine
      D00606  Guanfacine hydrochloride
Metabolizing enzyme substrate
  DG01633  CYP3A/CYP3A4 substrate
   DG02913  CYP3A4 substrate
    DG00250  Guanfacine
     D00606  Guanfacine hydrochloride
  DG02925  CYP3A5 substrate
   DG00250  Guanfacine
    D00606  Guanfacine hydrochloride
Target-based classification of drugs [BR:br08310]
G Protein-coupled receptors
  Rhodopsin family
   Adrenaline
    ADRA2A
     D00606  Guanfacine hydrochloride (JAN/USP) <JP/US>
New drug approvals in Europe [br08329.html]
European public assessment reports (EPAR) authorised medicine
  D00606
New drug approvals in Japan [br08318.html]
Drugs with new active ingredients
  D00606
Drug metabolizing enzymes and transporters [br08309.html]
Drug metabolizing enzymes
  D00606
Drug groups [BR:br08330]
Cardiovascular agent
  DG01738  Centrally-acting antiadrenergic
   DG00250  Guanfacine
  DG01456  Adrenergic receptor agonist
   DG01450  alpha-Adrenergic receptor agonist
    DG01449  alpha2-Adrenergic receptor agonist
     DG00250  Guanfacine
Metabolizing enzyme substrate
  DG01633  CYP3A/CYP3A4 substrate
   DG02913  CYP3A4 substrate
    DG00250  Guanfacine
  DG02925  CYP3A5 substrate
   DG00250  Guanfacine

Other DBs

CAS:	29110-48-3

PubChem:

7847672

ChEBI:

5559

LigandBox:

D00606

NIKKAJI:

J262.680B

KCF data

ATOM        16
            1   C8y C    24.2186  -16.1239
            2   C1b C    23.0015  -15.4193
            3   C8y C    24.2070  -17.5156
            4   C8y C    25.4239  -15.4134
            5   C5a C    21.7961  -16.1239
            6   C8x C    25.4239  -18.2144
            7   X   Cl   22.9956  -18.2087
            8   C8x C    26.6353  -16.1122
            9   X   Cl   25.4182  -14.0101
            10  N1b N    20.5848  -15.4193
            11  O5a O    21.7961  -17.5215
            12  C8x C    26.6353  -17.5156
            13  C2c C    19.3677  -16.1239
            14  N1a N    18.1565  -15.4193
            15  N2a N    19.3677  -17.5215
            16  X   Cl   29.0752  -16.4966
BOND        15
            1     1   2 1
            2     1   3 2
            3     1   4 1
            4     2   5 1
            5     3   6 1
            6     3   7 1
            7     4   8 2
            8     4   9 1
            9     5  10 1
            10    5  11 2
            11    6  12 2
            12   10  13 1
            13   13  14 1
            14   13  15 2
            15    8  12 1