atomoxetine indications/contra

Stem definitionDrug idCAS RN
serotonin and/or norepinephrine reuptake inhibitors, fluoxetine derivatives 256 83015-26-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • LY139603
  • strattera
  • atomoxetine
  • tomoxetine
  • (-)-Tomoxetine
  • atomoxetine hydrochloride
  • tomoxetine hydrochloride
  • atomoxetine HCl
  • tomoxetine HCl
A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.
  • Molecular weight: 255.36
  • Formula: C17H21NO
  • CLOGP: 3.94
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 21.26
  • ALOGS: -4.82
  • ROTB: 6

Drug dosage:

DoseUnitRoute
80 mg O

Approvals:

DateAgencyCompanyOrphan
Nov. 26, 2002 FDA LILLY

FDA Adverse Event Reporting System

scroll-->
MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Suicidal ideation 1241.54 42.82 357 5086 17348 3363068
Prescribed overdose 1162.15 42.82 234 5209 2332 3378084
Aggression 842.58 42.82 240 5203 11145 3369271
Tic 795.63 42.82 149 5294 966 3379450
Abnormal behaviour 632.93 42.82 187 5256 9841 3370575
Agitation 475.65 42.82 178 5265 19528 3360888
Tachycardia 439.17 42.82 176 5267 23195 3357221
Alanine aminotransferase increased 433.75 42.82 175 5268 23465 3356951
Aspartate aminotransferase increased 413.98 42.82 164 5279 20949 3359467
Intentional self-injury 403.65 42.82 114 5329 5071 3375345
Suicide attempt 396.22 42.82 147 5296 15700 3364716
Anger 372.12 42.82 104 5339 4447 3375969
Somnolence 356.61 42.82 167 5276 32037 3348379
Nausea 339.37 42.82 265 5178 129380 3251036
Decreased appetite 336.56 42.82 174 5269 41316 3339100
Irritability 336.06 42.82 119 5324 11097 3369319
Heart rate increased 320.68 42.82 123 5320 14363 3366053
Vomiting 305.56 42.82 215 5228 89316 3291100
Headache 302.64 42.82 216 5227 91764 3288652
Depression 300.18 42.82 159 5284 39611 3340805
Anxiety 286.56 42.82 154 5289 39475 3340941
Insomnia 283.56 42.82 148 5295 35750 3344666
Psychomotor hyperactivity 269.88 42.82 75 5368 3132 3377284
Drug ineffective 268.42 42.82 221 5222 115869 3264547
Seizure 267.13 42.82 148 5295 40252 3340164
Electrocardiogram QT prolonged 265.32 42.82 99 5344 10696 3369720
Fatigue 260.11 42.82 210 5233 107030 3273386
Weight decreased 259.87 42.82 145 5298 39966 3340450
Crying 258.65 42.82 81 5362 5142 3375274
Dizziness 252.00 42.82 180 5263 76332 3304084

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC N06BA09 NERVOUS SYSTEM
PSYCHOANALEPTICS
PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
Centrally acting sympathomimetics
FDA EPC N0000175695 Norepinephrine Reuptake Inhibitor
FDA MoA N0000000102 Norepinephrine Uptake Inhibitors
MeSH PA D018663 Adrenergic Agents
MeSH PA D018759 Adrenergic Uptake Inhibitors
CHEBI has role CHEBI:35640 adrenergic uptake inhibitor
CHEBI has role CHEBI:35469 antidepressant
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014179 Neurotransmitter Uptake Inhibitors

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Attention deficit hyperactivity disorder indication 406506008
Delay when starting to pass urine contraindication 5972002
Priapism contraindication 6273006 DOID:9286
Suicidal thoughts contraindication 6471006
Sinus tachycardia contraindication 11092001
Bipolar disorder contraindication 13746004 DOID:3312
Hyperbilirubinemia contraindication 14783006 DOID:2741
Myocardial infarction contraindication 22298006 DOID:5844
Feeling agitated contraindication 24199005
Orthostatic hypotension contraindication 28651003
Hypertensive disorder contraindication 38341003 DOID:10763
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Feeling irritable contraindication 55929007
Aggressive behavior contraindication 61372001
Cerebrovascular disease contraindication 62914000 DOID:6713
Psychotic disorder contraindication 69322001
Cardiomyopathy contraindication 85898001 DOID:0050700
Structural disorder of heart contraindication 128599005
Seizure disorder contraindication 128613002 DOID:1826
Liver function tests abnormal contraindication 166603001
Cerebrovascular accident contraindication 230690007 DOID:6713
Mania contraindication 231494001
Disease of liver contraindication 235856003 DOID:409
Raynaud's phenomenon contraindication 266261006
Retention of urine contraindication 267064002
Pheochromocytoma contraindication 302835009
Angle-closure glaucoma contraindication 392291006 DOID:13550
Disorder of coronary artery contraindication 414024009
Myocardial infarction in recovery phase contraindication 418044006

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.32 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent noradrenaline transporter Transporter INHIBITOR Kd 8.69 CHEMBL CHEMBL
Sodium-dependent dopamine transporter Transporter Kd 5.97 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.68 CHEMBL
Sodium-dependent serotonin transporter Transporter Kd 8.05 CHEMBL
Kir3.1/Kir3.2 Ion channel IC50 4.48 WOMBAT-PK
Kir3.1/Kir3.4 Ion channel IC50 4.84 WOMBAT-PK
G protein-activated inward rectifier potassium channel 2 Ion channel IC50 4.28 WOMBAT-PK
Cytochrome P450 2D6 Enzyme Ki 4.77 WOMBAT-PK
Krueppel-like factor 10 Unclassified IC50 4 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 7.37 CHEMBL
Transporter Transporter Ki 8.40 CHEMBL
Transporter Transporter Ki 9.15 CHEMBL
Sodium-dependent dopamine transporter Transporter Ki 5.85 CHEMBL

External reference:

scroll-->
IDSource
DB00289 DRUGBANK_ID
C1176420 UMLSCUI
7118 IUPHAR_LIGAND_ID
D02574 KEGG_DRUG
CHEMBL641 ChEMBL_ID
57WVB6I2W0 UNII
82248-59-7 SECONDARY_CAS_RN
54841 PUBCHEM_CID
38400 RXNORM
4024296 VANDF
N0000022300 NDFRT
009862 NDDF
407037005 SNOMEDCT_US
407038000 SNOMEDCT_US
d04827 MMSL
5354 INN_ID
CHEBI:127342 CHEBI
CHEMBL1702 ChEMBL_ID
D000069445 MESH_DESCRIPTOR_UI

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Strattera HUMAN PRESCRIPTION DRUG LABEL 1 0002-3227 CAPSULE 10 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 1 0002-3228 CAPSULE 25 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 1 0002-3229 CAPSULE 40 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 1 0002-3238 CAPSULE 18 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 1 0002-3239 CAPSULE 60 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 1 0002-3250 CAPSULE 80 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 1 0002-3251 CAPSULE 100 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5800 KIT 18 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5800 KIT 10 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5800 KIT 40 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5800 KIT 25 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5801 KIT 60 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5801 KIT 18 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5801 KIT 25 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5801 KIT 40 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5802 KIT 60 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5802 KIT 25 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5802 KIT 40 mg ORAL NDA 20 sections
Strattera HUMAN PRESCRIPTION DRUG LABEL 4 0002-5802 KIT 80 mg ORAL NDA 20 sections
Atomoxetine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3542 CAPSULE 10 mg ORAL ANDA 19 sections
Atomoxetine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3543 CAPSULE 18 mg ORAL ANDA 19 sections
Atomoxetine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3544 CAPSULE 25 mg ORAL ANDA 19 sections
Atomoxetine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3545 CAPSULE 40 mg ORAL ANDA 19 sections
Atomoxetine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3546 CAPSULE 60 mg ORAL ANDA 19 sections
Atomoxetine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3547 CAPSULE 80 mg ORAL ANDA 19 sections
Atomoxetine HUMAN PRESCRIPTION DRUG LABEL 1 0093-3548 CAPSULE 100 mg ORAL ANDA 19 sections
Atomoxetine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-2260 CAPSULE 10 mg ORAL ANDA 20 sections
Atomoxetine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-2261 CAPSULE 18 mg ORAL ANDA 20 sections
Atomoxetine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-2262 CAPSULE 25 mg ORAL ANDA 20 sections
Atomoxetine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0781-2263 CAPSULE 40 mg ORAL ANDA 20 sections