| Generic Name
| Trade Name
| Usage
| Dosage
| Half-Life
Metabolism
| Properties
|
| acamprosate
| Campral, Aotal, Zulex
| 抗成瘾,酒精依存性, 诫酒, 双极性异常
| 1200-1800mg
| 13-28 hrs
renal excretion
| * homotaurine:
GLU release inhibitor
GABAergic |
| acetophenazine
| Tindal, Mepronizine, Noctran
| antipsychotic
| 20-60mg
| 20-40 hrs
| * piperazine
phenothiazine:
neuroleptic
DA antagonist |
| adinazolam
| Deracyn
| depression, anxiety, panic
| 30-90mg
| 3 hrs
CYP-3A
| * triazolo
benzodiazepine:
BZD partial agonist
NE release
5-HT release |
| adrafinil
| Olmifon
| nootropic, vigilance, depression, dysthymia
| 600-1200mg
| 1 hr
glycuroconjugation
| * diphenyl
methylsulfinyl:
GLU release |
| almodipine
| Norvasc, Lotrel, Amlor, Istin
| hypertension, angina, bipolar disorder
| 5-10mg
| 30-50 hrs
CYP-3A4
| * dihydropyridine:
CCB
Ca2+(L) channel inhibition |
| alprazolam
| Xanax, Ansiopax, Apotex, Constan, Mialin, Pazolam, Tafil,
Tranquinal, Xanor, Zanapam
| anxiety, GAD, panic disorder
| 1.5-4.0mg
(10mg max)
| 11.2 hrs (6-26 hrs)
CYP-3A
| * triazolo
benzodiazepine:
BZD agonist
5-HT release |
| amantadine
| Symmetrel, Symandine, Amantan, Mantadan, Virofral,
| Parkinsons, antiviral, depression, AP-induced EPS
| 100-300mg
| 10-22 hrs
renal excretion
| * cyclic amine:
NMDA antagonist
DA increase
DA release |
amfebutamone
(bupropion)
| Wellbutrin, Zyban
| depression, smoking cessation, AD sexual side-effects
| 75-300mg
(450mg max)
| 21 hrs
CYP-2D6 (inhibitor)
CYP-2B6
| * monocyclic aminoketone:
DA reuptake inhibition +
NE increase
ACh(n) antagonist |
| amiflamine
| N/A
| depression
| 5-10mg
| CYP-2D6
| * methylphenethylamine:
RIMA |
| amineptine
| Survector, Directim, Maneon
| depression
| 100-200mg
| 5-8 hrs
| * dibenzocycloheptene:
DA reuptake inhibition |
| amisulpride
| Solian
| antipsychotic, depression, dysthymia
| AP: 400-800mg
(1200mg max)
AD: 50-200mg
| 12 hrs
renal excretion
| * benzamide:
neuroleptic
DA2 antagonist +++
(pre > post)
DA3 antagonist +++ |
| amitriptyline
| Elavil, Endep, Etrafon, Amitril, Amitrip, Domical, Etravil,
Laroxyl, Lentizol, Levate, Miketorin, Novotriptyn, Pinsanu, Quietal,
Redomex, Saroten, Tridep, Triptizol, Tryptal, Uxen, Vanatrip
| depression, insomnia, anorexia, pain disorders, migraine
| 50-200mg
(300mg max)
| 20 hrs
(10-50 hrs)
CYP-2D6
CYP-2C19
CYP-1A2
P-gp
| * dibenzocycloheptadiene:
tertiary TCA
NE reuptake inhibition ++
5-HT reuptake inhibition ++
5-HT2 antagonist ++
ACh antagonist
H1 antagonist
NE-alpha1 antagonist |
| amitriptyline + chlordiazepoxide
| Limbitrol
(12.5+5mg)
(25+10mg)
| comorbid depression and anxiety
| (25+10mg)
3-6 per day
| N/A
| * TCA + benzodiazepine:
NE reuptake inhibition ++
5-HT reuptake inhibition ++
+ BZD agonist |
| amitriptyline + perphenazine
| Triavil, Etrafon
| comorbid depression with (agitation or anxiety)
| 200mg+16mg
max
| N/A
| * TCA + neuroleptic:
NE reuptake inhibition ++
5-HT reuptake inhibition ++
+ DA antagonist |
| amoxapine
| Asendin, Defanyl, Moxadil
| depression (psychotic)
| 200-400mg
(600mg max)
| 8 hrs
CYP-2D6
| * dibenzoxazepine:
TCA
NE reuptake inhibition ++
5-HT reuptake inhibition +
DA antagonist
5-HT2 antagonist
5-HT3 antagonist |
amphetamine
(mixed salts)
| Adderall, Biphetamine
| ADD, ADHD, narcolepsy, depression, AD sexual side-effects
| 5-40mg
(60mg max)
| 10-25 hrs
CYP-2D6
| * psychostimulant:
NE release +++
DA release ++
DA reuptake inhibition +
NE reuptake inhibition + |
amphetamine
(d-amphetamine)
| Dexedrine, DextroStat, Benzadrine
| ADD, ADHD, narcolepsy, obesity, depression
| 5-30mg
(40mg max)
| 10-25 hrs
CYP-2D6
| * psychostimulant:
NE release +++
DA release ++
DA reuptake inhibition +
NE reuptake inhibition + |
| apomorphine
| Uprima, Apokinin
| Parkinsons, sexual dysfunction (erectile), alcohol
withdrawal
| 2-3mg
| 1-2 hrs
glucuronide conjugation
| * dibenzoquinoleine:
DA agonist |
| aprepitant
| Emend
| depression, antiemetic
| N/A
| N/A
| * triazoline:
NK-1 antagonist |
| aripiprazole
| Abilify, Abilitat
| antipsychotic, depression
| 15-30mg
| 75 hrs
CYP-2D6
CYP-3A4
| * quinolinone:
DSS
DA2 partial agonist +++
DA3 antagonist +++
5-HT2a antagonist ++
5-HT1a agonist ++ |
| atenolol
| Tenormin, Antipressan, Atehexal, Atenol, Blokium, Bresben,
Ibinolo, Neatenol, Normiten, Tenif, Tenoretic
| hypertension, angina, tremor, anxiety, akathisia, migraine
| 50-200mg
| 6-7 hrs
renal excretion
| * acetamide
BB
NE-beta1 antagonist ++
NE-beta2 antagonist + |
atomoxetine
(tomoxetine)
| Strattera
| ADD, ADHD, depression
| 50-150mg
(1.2-1.8mg/kg)
| 5 hrs
(5-24 hrs)
CYP-2D6
| * tolyloxypropylamine:
NE reuptake inhibition +++ |
| befloxatone
| N/A
| depression
| 10-40mg
| N/A
| * oxazolidinone:
RIMA |
| benmoxine
| Neuralex, Nerusil
| depression, anger
| 50-75mg
| N/A
| * hydrazine:
MAOI |
benztropine
(benzatropine)
| Cogentin, Akitan, Cogentinol
| Parkinsons, AP-induced EPS, antispasmodic
| 0.5-6.0mg
| N/A
| * methanesulfonate:
anticholinergic
ACh(m) antagonist
H1 antagonist |
| bethanechol
| Urecholine
| AD-induced urinary retention
| 10-50mg dose / 3-4x per day
| N/A
| * esther:
cholinergic
ACh(m) agonist |
| binedaline
| N/A
| depression
| 50-100mg
(150mg max)
| 5 hrs
| * indole:
NE reuptake inhibition |
| biperiden
| Akineton
| Parkinsons, AP-induced EPS, AD-induced sweating
| 2-6mg
| N/A
hydroxylation
| * piperidine:
anticholinergic
ACh(m) antagonist |
| brofaromine
| Consonar
| depression, social phobia
| 50-150mg
| 15 hrs
CYP-1A2
| * piperidine:
RIMA
5-HT reuptake inhibition |
| bromazepam
| Lexotan, Lectopam, Lexotanil
| anxiolytic, muscle-relaxant, anticonvulsant, delerium
tremens
| 4.5-9mg
(36mg max)
| 19hrs
hydroxylation
| * benzodiazepine:
BZD agonist |
| bromocriptine
| Parlodel, Ergoset
| Parkinsons, depression, RLS, hyperprolactinemia,
acromegaly
| 2.5-40mg
| 2-8 hrs
| * ergot alkaloid:
DA2 agonist |
| buprenorphine
| Temgesic, Buprenex, Subutex
| analgesic, depression, opioid dependence
| 1.2-3.2mg
| 2.2 hrs
(1.2-7.2 hrs)
| * morphinane:
opioid
opioid(mu) partial agonist
opioid(kappa) antagonist |
| bupropion
| Wellbutrin, Zyban
| depression, smoking cessation, ADD, ADHD, AD sexual
side-effects
| 75-300mg
(450mg max)
| 21 hrs
CYP-2D6 (inhibitor)
CYP-2B6
| * monocyclic aminoketone:
DA reuptake inhibition +
NE increase
ACh(n) antagonist |
| buspirone
| Buspar
| anxiety, GAD, IBS, AD Augment
| 20-30mg
(60mg max)
| 2-3 hrs
CYP-3A4
| * azapirone:
5-HT1a full agonist (pre)
5-HT1a partial agonist (post)
DA2 partial agonist
* 1-PP metabolite:
NE-alpha2 antagonist |
| butriptyline
| Evadyne, Evadene, Centrolyse
| depression
| N/A
| N/A
| * TCA:
NE reuptake inhibition
5-HT reuptake inhibition |
| cabergoline
| Dostinex
| Hyperprolactinemia, Parkinsons, Depression, RLS
| 0.25-1.0mg
Twice a week
| 60 hrs
hydrolysis
| * ergoline:
DA2 agonist |
| caffeine
| Vivarin, Cafcit,
No Doz,
BL Stay Awake
| stimulant, analeptic
| 50-200mg
| 3-4 hrs
CYP-1A2
| * methylxanthine:
adenosine antagonist
cAMP PDE inhibition |
| calcium carbimide
| Temposil, Abstem
| alcoholism
| 100-200mg
| 1.5 hrs
| * carbimide:
acetaldehyde-deshydrogenase inhibition |
| carbamazepine
| Tegretol, Epitol, Atretol, Carbatrol, Carbium, Teril,
Sirtal, Telestin, Timonil
| anticonvulsant, pain disorders, aggression
| 600-1200mg
| 12-17 hrs
CYP-3A4
CYP-2C19
| * tricyclic
iminostilbene:
Na+ channel inhibition
adenylyl cyclase inhibition |
| caroxazone
| N/A
| depression
| N/A
| 36 hrs
| * benzoxazine:
RIMA |
| carpipramine
| Prazinil, Defekton
| antipsychotic, drug detoxification
| 50-400mg
| N/A
| * dibenzoazepine:
neuroleptic
DA2 antagonist |
| cericlamine
| N/A
| depression
| N/A
| N/A
| * dimethyloamine:
5-HT reuptake inhibition |
| chloral hydrate
| Aquachloral, Nortec
| insomnia
| 500 - 1000mg
| 8-10 hrs
| * trichloroethanol:
CNS depressant:
GABA-A increase |
| chlordiazepoxide
| Librium, Libritabs, Tropium
| anxiolytic, alcohol withdrawal, IBS
| 10-40mg
| 24-48 hrs
CYP-3A
| * 2-keto benzodiazepine:
BZD agonist |
| chlorpromazine
| Thorazine, Chlomazine, Dormazine, Fenactil, Hibernal,
Ormazine, Promaz, Prozil, Solidon, Sonazine, Taroctyl
| antipsychotic, hiccups, nausea, porphyria
| 75-200mg
(900mg max)
| 30 hrs
CYP-2D6 (inhibitor)
CYP-1A2
UGT-1A4
| * phenothiazine:
neuroleptic
DA1 antagonist +
DA2 antagonist ++
5-HT2a antagonist ++
NE-alpha1 antagonist ++
H1 antagonist ++ |
| chlorprothixene
| Taractan, Chlorprothixen, Cloxan, Minithixen, Truxal,
Truxaletten
| antipsychotic
| 300-600mg
| N/A
| * thioxanthene
neuroleptic
DA1 antagonist
DA2 antagonist
5-HT2 antagonist |
| ciclazindol
| N/A
| depression, obesity
| 100-150mg
| 32 hrs
| * tetrahydropyrimide:
DA reuptake inhibition
NE reuptake inhibition
K+(ATP) channel inhibition |
| cimoxatone
| N/A
| depression
| N/A
| N/A
| * oxazolidinone:
RIMA |
| citalopram
| Celexa, Cipramil, Seropram
| depression
| 20-60mg
| 35 hrs
CYP-2C19
| * bicyclic phthalane:
SSRI
5-HT reuptake inhibition +++ |
| clobazam
| Frisium, Mystan
| epilepsy, anxiolytic
| 20-60mg
| 18-26 hrs
| * benzodiazepine:
BZD agonist |
| clomipramine
| Anafranil, Clofranil, Clomifril, Clopress, Gromin,
Hydiphen, Placil
| depression, OCD
| 50-250mg
| 19-37 hrs
CYP-1A2
| * dibenzazepine:
tertiary TCA
5-HT reuptake inhibition +++
NE reuptake inhibition +
5-HT2a antagonist ++
ACh antagonist
NE-alpha antagonist |
| clonazepam
| Klonopin, Rivotril
| anxiolytic, anticonvulsant, hypnotic, bipolar disorder,
agoraphobia, panic disorder, Lennox-Gastaut Syndrome
| anxiety: 0.5-4mg
AC: 1.5-10mg
(20mg max)
| 30-40 hrs
CYP-3A4
| * 3-hydroxy
benzodiazepine:
BZD agonist
5-HT increase |
| clonidine
| Catapres, Dixarit
| hypertension, ADD, ADHD, anxiety, aggression, opioid
withdrawal, motor tics, Tourette's, migraine
| 0.2-0.6mg
(2.4mg max)
| 12-16 hrs
| * imidazoline:
NE-alpha2 agonist |
| clopenthixol
| Clopixol
| antipsychotic
| 10-50mg
(200mg max)
| 20 hrs
| * thioxanthene:
neuroleptic
DA1 antagonist
DA2 antagonist |
| clorazepate
| Tranxene
| anxiolytic, partial seizures, alcohol withdrawal
| 15-60mg
| 30-40 hrs
(norclorazepate)
| * 2-keto benzodiazepine:
BZD agonist |
| clorgyline
| N/A
| depression, ADD, ADHD
| 5-15mg
(30mg max)
| N/A
| * propargyl:
MAO-A inhibitor +++ |
| clovoxamine
| N/A
| depression
| 100-300mg
| N/A
| * aminoethyloxime:
SSRI
5-HT reuptake inhibition +++
NE reuptake inhibition + |
| clozapine
| Clozaril
| antipsychotic, reduce TD, AD augmentor
| 150-900mg
| 12 hrs
(4-66 hrs)
| * dibenzodiazepine:
neuroleptic
DA2 antagonist +
DA4 antagonist +
5-HT2a/b/c ++
5-HT6/7 +
NE-alpha1 antagonist ++
H1 antagonist +++
Ach(m) antagonist +++ |
| cocaine
| N/A
| topical anesthetic (oral, laryngeal and nasal cavities)
| N/A
| 30-90 minutes
CYP-3A4
| * psychostimulant:
DA reuptake inhibition ++
NE reuptake inhibition + |
| cyproheptadine
| Periactin, Dronactin, Cipractin, Nuran, Oractin,
Periactinol
| allergy, pruritis, urticaria, AD sexual side-effects,
appetite stimulant, migraine
| 4-20mg
(32mg max)
| 1-4 hrs
renal excretion
| * dibenzocycloheptene:
5-HT2a antagonist +++
5-HT2c antagonist ++
H1 antagonist +++
H4 antagonist ++
ACh(m) antagonist |
| dapoxetine
| N/A
| depression, premature ejaculation
| N/A
| N/A
| * benzenemethanamine:
SSRI
5-HT reuptake inhibition |
| demexiptiline
| Tinoran, Deparon
| depression
| 50-75mg
| 35 hrs
desmethylation
| * dibenzocycloheptene:
NE reuptake inhibition +++
5-HT reuptake inhibition +
ACh antagonist |
l-deprenyl
(selegiline)
| Eldepryl, Carbex, Jumex, Emsam
| Parkinsons, depression, dementia, neuroprotective
| 5-30mg
(60mg max)
| 2-10 hrs
CYP-2C19
CYP-2B6
| * propargyl:
MAOI
MAO-B inhibition ++
MAO-A inhibition + |
| deramciclane
| N/A
| anxiolytic
| 30-50mg
| 25 hrs
| * trimethyl-bicycloheptane:
5-HT2a antagonist
5-HT2c inverse agonist |
| desipramine
| Norpramin, Pertrofane, Metylyl, Nortimil, Pertofrane,
Pertofrin, Sertofren
| depression, ADD, ADHD, bulimia, IBS, pain disorders
| 50-200mg
(300mg max)
| 20-25 hrs
CYP-2D6
| * dibenzazepine:
secondary TCA
NE reuptake inhibition +++
ACh(m) antagonist +
NE-alpha1 antagonist |
| dexmethylphenidate
| Focalin
| ADD, ADHD, depression, CFS
| 5-20mg
| N/A
| * psychostimulant:
DA reuptake inhibition
NE reuptake inhibition
NE release |
dextroamphetamine
(d-amphetamine)
| Dexedrine, DextroStat
| ADD, ADHD, narcolepsy, obesity
| 5-30mg
(40mg max)
| 10-25 hrs
CYP-2D6
| * psychostimulant:
NE release +++
DA release ++
DA reuptake inhibition +
NE reuptake inhibition + |
| diazepam
| Valium, Dizac
| anxiolytic, muscle relaxant, seizures, status epilepticus,
athetosus, tetanus, alcohol withdrawal, surgical sedation
| 10-40mg
| 20 hrs
CYP-2C19
CYP-3A4
| * 2-keto benzodiazepine:
BZD agonist |
| dibenzepine
| Noveril, Ecotril, Victoril
| depression
| 240-480mg
| N/A
| * dibenzepine:
TCA
NE reuptake inhibition ++
5-HT reuptake inhibition + |
| dihydroergocryptine (DHEC)
| Almirid, Hydergine (includes ergoloid mesylates)
| nootropic, cerebrovascular insufficiency, dementia,
neuroprotection, migraine
| Almirid: 10-40mg
Hydergine: 1-3mg
| 2.6-5.1 hrs
| * ergot alkaloid:
DA agonist
NE-alpha antagonist
MAOI |
| diphenhydramine
| Benadryl
| allergy, sedative, Parkinsonism, AP-induced EPS
| 75-200mg
| 2.4-9.3 hrs
| * ethanolamine:
antihistamine
H1 antagonist
ACh(m) antagonist |
| disulfiram
| Antabuse, Alcophobin, Anticol, Aversan, Etiltox
| alcoholism
| 125-500mg
| 54-72 hrs
renal clearance
| * diethylthiocarbamoyl:
acetaldehyde-deshydrogenase inhibition |
| divalproex sodium
| Depakote, Epival, Elvetium, Everiden, Novoseven, Valcote,
Valnar
| anticonvulsant, migraine, bipolar disorder
(mood-stabilizer)
| 750-3000mg
(50-125mcg/ml)
| 9-16 hrs
CYP-2C9 (inhibitor)
CYP-2A6
glucoronidation
| * carboxylic acid:
Na+ channel inhibition
Ca2+(T) channel inhibition
GABA increase:
1. GABA transaminase inhibition
2. SSAD dehydrogenase inhibition |
| donepezil
| Aricept
| Alzheimer's, enhance memory and cognition
| 5-10mg
| 70 hrs
CYP-2D6
CYP-3A4
| * piperidine:
cholinergic
ACh acetylcholinesterase inhibitor |
| dothiepin (dosulepin)
| Prothiaden, Arpin, Idom
| depression
| 50-225mg
| 22 hrs
(11-30 hrs)
CYP-1A2
CYP-2D6
| * dibenzothiepine:
TCA
NE reuptake inhibition
5-HT reuptake inhibition
ACh(m) antagonist |
| dosulepin (dothiepin)
| Prothiaden, Arpin, Idom
| depression
| 50-225mg
| 22 hrs
(11-30 hrs)
CYP-1A2
CYP-2D6
| * dibenzothiepine:
TCA
NE reuptake inhibition
5-HT reuptake inhibition
ACh(m) antagonist |
| doxepin
| Sinequan, Adapin, Aponal, Poldoxin, Quitaxon, Desidox,
Doneurin, Doxal, Doxedyn
| depression, anxiety,
| 75-150mg
(300mg max)
| 8-24 hrs
CYP-2D6
| * dibenzoxepin:
tertiary TCA
NE reuptake inhibition ++
5-HT reuptake inhibition +
5-HT2a antagonist ++
ACh(m) antagonist
H1 antagonist +++
H2 antagonist +++
NE-alpha1 antagonist |
| droperidol
| Inapsine
| antipsychotic, antiemetic
| injectable
| 2 hrs
| * butyrophenone:
neuroleptic
DA2 antagonist |
| duloxetine
| Cymbalta
| depression
| 40-120mg
| 10-15 hrs
| * thiophenepropanamine:
SNRI
NE reuptake inhibition ++
5-HT reuptake inhibition ++ |
| entacapone
| Comtan, Comtess
| Parkinsons
| 400-1600mg
| 1 hr
glucuronidation
| * nitrocatechol:
COMT inhibition |
| escitalopram
| Lexapro, Cipralex
| depression, panic disorder
| 10-30mg
| 27-32 hrs
CYP-2C19
| * bicyclic phthalane:
SSRI
5-HT reuptake inhibition +++ |
| estazolam
| Prosom, DEprinocte, Domnamid, Esilgan, Kainever, Nuctalon
| insomnia
| 1-2mg
| 10-24 hrs
CYP-3A4
| * triazolo
benzodiazepine:
BZD agonist |
| eszopiclone
| Estorra
| insomnia
| 2-3mg
| N/A
| *
GABA receptor agonist |
ethopropazine
(profenamine)
| Pardidol, Parsidol, Parsitan, Dibutil, Lysivane, Rodipal
| Parkinsons, AP-induced EPS
| 100-600mg
| N/A
| * phenothiazine:
ACh(m) antagonist |
| ethosuximide
| Zarontin
| anticonvulsant
| 1000-1500mg
| 30-50 hrs
CYP-3A4
| * succinimide:
Na+ channel inhibition
Ca+2 channel inhibition |
| etoperidone
| N/A
| depression
| 150mg
| 21 hrs
CYP-3A4
| * phenylpiperazine:
NE-alpha2 antagonist
5-HT1a antagonist
5-HT2a/c antagonist |
| etryptamine
| Monase
| depression
| N/A
| N/A
| * ndolalkylamine:
MAOI |
| femoxetine
| N/A
| depression, obesity, migraine, narcolepsy
| 400-600mg
| N/A
| * methylpiperidine:
5-HT reuptake inhibition |
| felbamate
| Felbatol
| epilepsy, biopolar disorder
| 600-2400mg
(3600mg max)
| 20-23 hrs
CYP-2E1
CYP-2C19 (inhibitor)
| * phenylpropanediol:
NMDA antagonist |
| fengabine
| N/A
| depression
| 900-1800mg
| N/A
| * benzylidene:
GABA increase |
| flerobuterol
| N/A
| depression
| N/A
| N/A
| * butylamino ethanol:
NE-beta agonist
5-HT increase |
| flesinoxan
| N/A
| depression, anxiety
| 0.6-2.4mg
| N/A
| * phenylpiperazine:
5-HT1a agonist
NE-alpha1 antagonist |
| flibanserin
| Ectris
| depression
| 50-200mg
| 5.0-6.5 hrs
| * benzimidazol:
5-HT1a agonist
5-HT2a antagonist |
| flunitrazepam
| Rohypnol, Hipnosedon
| anxiolytic, hypnotic
| 0.5-2.0mg
(3.0mg max)
| 22 hrs
(16-35 hrs)
CYP-3A
UGT-UB7
| * benzodiazepine:
BZD agonist |
| fluoxetine
| Prozac, Sarafem, Lovan, Prodep, Deproxin, Fluoxac, Fluoxil,
Zactin
| depression, PMDD, OCD, bulimia
| 20-60mg
(120mg max)
| 4-6 days
(norfluoxetine 9-14 days)
CYP-2D6 (inhibitor)
CYP-2C9
CYP-2D6 (inhibitor)
CYP-2C9
| * propylamine:
SSRI
5-HT reuptake inhibition +++
NE reuptake inhibition +
5-HT2c antagonist
NE increase |
| fluparoxan
| N/A
| depression
| N/A
| N/A
| * benzodioxino:
NE-alpha2 antagonist +++
5-HT1a partial agonist + |
| flupenthixol
| Fluanxol, Depixol
| antipsychotic
| 3-6mg
(12mg max)
| 14-17 days (injectable)
| * thioxanthene:
neuroleptic
DA1 antagonist +
DA2 antagonist ++
5-HT2a antagonist ++ |
| fluphenazine
| Prolixin, Modecate, Permitil
| antipsychotic
| 2.5-20.0mg
(40mg max)
| 4-14 days (injectable)
CYP-2D6
P-gp
| * piperazine
phenothiazine:
neuroleptic
DA1 antagonist ++
DA2 antagonist +++
5-HT2a antagonist + |
| flurazepam
| Dalmane
| insomnia
| 15-30mg
| 2-3 hrs
(N-desalkylflurazepam: 80 hrs)
CYP-3A4
| * 2-keto benzodiazepine:
BZD agonist |
| fluvoxamine
| Luvox, Floxyfral
| OCD, depression
| 100-300mg
| 15.6 hrs
CYP-2C9
CYP-3A4 (inhibitor)
| * valerophenone:
SSRI
5-HT reuptake inhibition +++ |
| gabapentin
| Neurontin
| anticonvulsant, bipolar disorder, anxiety disorders, pain
disorders, migraine
| 600-2400mg
(5400mg max)
| 5-7 hrs
renal excretion
| * cyclohexonacetic acid:
GABA increase
Ca2+(L) channel inhibition |
| galantamine
| Reminyl, Nivalin
| Alzheimer's
| 8-16mg
(24mg max)
| 7 hrs
CYP-2D6
CYP-3A4
glucuronidation
| * tertiary alkaloid:
cholinergic
ACh acetylcholinesterase inhibitor
ACh(n) agonist |
| gepirone
| Ariza, Variza
| depression, anxiety
| 10-90mg
| 1-2 hrs
CYP-3A
CYP-2D6 (metabolite)
| * azapirone:
5-HT1a full agonist (pre)
5-HT1a partial agonist (post)
NE-alpha2 antagonist
(1-PP metabolite) |
GHB
(oxybate)
| Xyrem, Somsanit
| narcoleptic cataplexy, anesthesia, insomnia, stroke
| 6-9grams
| 0.5-1.0 hrs
tricarboxylic acid
(Krebs cycle)
| * gamma hydroxybutyrate
GABA-B agonist
GABA increase |
| halazepam
| Paxipam, Alapryl, Pacinone
| anxiolytic
| 60-160mg
| oxidation
| * benzodiazepine:
BZD agonist |
| haloperidol
| Haldol
| antipsychotic, Tourette's syndrome
| 2-20mg
(40mg max)
| 18-25 hrs
CYP-2D6 (inhibitor)
glucuronidation
| * butyrophenone:
neuroleptic
DA2 antagonist +++
DA3/4 antagonist ++
5-HT2a +
NE-alpha1 ++ |
| hydroxyzine
| Atarax, Vistaril
| allergy, sedative
| 50-100mg
| 20 hrs
| * piperazine:
antihistamine
H1 antagonist
ACh(m) antagonist |
| idazoxan
| N/A
| depression
| 40-120mg
| 4 hrs
| * imidazoline:
NE-alpha2 antagonist |
| igmesine
| N/A
| depression
| 200mg
| N/A
| * diphenylamine:
sigma1 agonist
NMDA antagonist |
| iloperidone
| Zomaril
| antipsychotic
| 4-24mg
| 14 hrs
CYP-2D6
| * benzisoxazole:
neuroleptic
DA2 antagonist
5-HT2a antagonist |
| imipramine
| Tofranil, Janimine, Antideprin, Ethipramine, Imavate,
Melipramine, Mipralin, Pryleugan, Sedacoroxen, Venefon
| depression, ADD, ADHD, IBS
| 75-300mg
| 19 hrs
(8-20 hrs)
| * dibenzazepine:
tertiary TCA
NE reuptake inhibition ++
5-HT reuptake inhibition ++
ACh(m) antagonist
NE-alpha1 antagonist |
| indalpine
| Upstene
| depression, anxiety
| 100-150mg
| 10 hrs
| * indole:
5-HT reuptake inhibition |
| indeloxazine
| Elen
| depression, Alzheimer's, hypoxia, nootropic
| 40-120mg
| N/A
| * morpholine:
NE reuptake inhibition ++
5-HT reuptake inhibition
5-HT release
ACh release |
| incazane
| N/A
| depression
| 150-300mg
| N/A
| *
RIMA |
| iprindole
| N/A
| depression
| 90mg
| N/A
| * tricyclic
5-HT2 antagonist +
aromatic hydroxylase inhibition |
| iproniazid
| Iprozid, Ipronid, Marsilid, Rivivol, Propilniazida
| tuberculosis, depression
| 50-150mg
| 2-3 hrs
| * hydrazine:
MAOI |
| iproclozide
| Sursum
| depression, hypertension
| 10-30mg
| N/A
| * hydrazine:
MAOI |
| ipsapirone
| N/A
| depression, anxiety
| 10mg
| 2-5 hrs
CYP-3A
CYP-2D6 (metabolite)
| * azapirone:
5-HT1a full agonist (pre)
5-HT1a partial agonist (post)
* 1-PP metabolite:
NE-alpha2 antagonist |
| isocarboxazid
| Marplan, Enerzer, Marplon
| depression
| 30-80mg
| N/A
| * hydrazine:
MAOI |
| isradipine
| Dynacirc, Lomir, Icaz
| hypertension, bipolar disorder, depression
| 5-10mg
(20mg max)
| 8 hrs
CYP-3A4
| * dihydropyridine:
CCB
Ca2+(L) channel inhibition |
| ketanserin
| Sufrexal, Aseranox, Ketensin, Ketenserina, Perketan,
Serepress, Sparfloxacine
| hypertension, preeclampsia, Raynaud's
| 60-120mg
(160mg max)
| 15 hrs
| * quinazolinedione:
NMDA antagonist
NE-alpha1 antagonist
H1 antagonist |
| ketazolam
| Anxon
| anxiolytic, insomnia, alcohol withdrawal
| 15-60mg
(120mg max)
| 2 hrs
| * benzodiazepine
BZD agonist |
l-dopa
(levodopa)
| Larodopa, Dopar, Sinemet (carbidopa/l-dopa)
| Parkinsons, depression
| 2-8grams
| 1-2 hrs
| * catecholamine:
DA increase |
| lamotrigine
| Lamictal
| anticonvulsant, depression, bipolar disorder
| 50-500mg
| 25 hrs
(48 hrs with valproate)
(12 hrs with carbamazepine)
UGT-1A4
| * phenyltriazine:
Na+ channel inhibition
GLU decreased
Ca2+(N) channel inhibition
Ca2+(P) channel inhibition |
| levetiracetam
| Keppra
| anticonvulsant, bipolar disorder
| 1000-3000mg
(5000mg max)
| 6-8 hrs
| * pyrrolidine:
Ca2+(N) channel inhibition |
levomepromazine
(methotrimeprazine)
| Levoprome, Nozinan, Neurocil, Veractil, Sinogan
| antipsychotic, migraine, surgical sedation, pain disorders
| 50-200mg
(500mg max)
| 15-30 hrsCYP-2D6
CYP-3A4 (inhibitor)
| * phenothiazine:
neuroleptic
DA1 antagonist
DA2 antagonist
|
| levoprotiline
| N/A
| depression
| 100-200mg
| 18 hrs
| * tetracyclic:
NE reuptake inhibition |
liothyronine (T3)
(also triiodothyronine)
| Cytomel
| hypothyroidism, depression, bipolar disorder
| 25-100mcg
| 1-2 days
| * thyroid hormone:
NE receptor sensitivity increase
MAO inhibition
|
| lithium
| Eskalith, Lithobid, Carbolith, Carbolithium, Contemnol,
Duralith, Hypnorex, Lentolith, Liskonum, Litarex, Lithane, Lithicarb,
Lithizine, Maniprex, Milithin, Neurolepsin, Neurolithium, Phasal,
Quilonorm, Teralithe
| bipolar disorder, depression (augmentor), schizoaffective,
neuroprotection, neurotrophic
| bipolar:
900-1500mg
(0.8-1.2 mEq/L)
unipolar:
300-600mg
(0.4-0.6 mEq/L)
| 14-30 hrs
renal excretion
| * alkali metal Li+ ion:
5-HT autoreceptor antagonist
GLU decreased
PI turnover decreased
PKC decreased
GSK-3b decreased
MAP kinase increase
Bcl-2 increase
BDNF increase
NFG increase |
| litoxetine
| N/A
| depression
| 10-25mg
| N/A
| *
5-HT reuptake inhibition
5-HT3 antagonist
ACh(m) antagonist |
| lofepramine
| Emdalen, Gamanil, Lomont, Tymelyt
| depression
| 70 - 210mg
| 4-6 hrs
CYP-2D6
| * TCA:
NE reuptake inhibition |
| lorazepam
| Ativan, Alzapam, Almazine, Durazolam, Loraz, Tavor,
Temesta
| anxiolytic, insomnia
| 2-10mg
| 9-24 hrs
UGT-UB7
| * 3-hydroxy
benzodiazepine:
BZD agonist |
| loprazolam
| Dormonoct, Havlane, Sonan
| insomnia
| 1-2mg
| 8 hrs
| * benzodiazepine:
BZD agonist |
| lormetazepam
| Noctomid, Noctamide, Ergocalm,
| insomnia
| 1-2mg
| 10 hrs
| * benzodiazepine:
BZD agonist |
| loxapine
| Loxitane, Loxapac, Desconex
| antipsychotic
| 60-100mg
(250mg max)
| 3 hrs
20-30 hrs (active metabolite)
UGT-1A4
glucuronidation
| * dibenzoxazepine:
neuroleptic
DA antagonist |
| maprotiline
| Ludiomil, Aneural, Retinyl, Deprilept, Maludil, Melodil
| depression, lumbago
| 75-150mg
| 27-58 hrs
CYP-2D6
| * tetracyclic:
NE reuptake inhibition ++
ACh(m) antagonist |
| mazindol
| Mazanor, Sanorex, Sanjorex, Teronac
| obesity, EDS, depression
| 1-3mg
| 12 hrs
| * imidazoline:
DA reuptake inhibition
NE reuptake inhibition |
| mebanazine
| Actomol
| depression
| N/A
| N/A
| * hydrazine:
MAOI |
| mecamylamine
| Inversine, Mevasine, Prexion
| hypertension, Tourette's, ADD, ADHD, smoking cessation,
bipolar disorder
| 5-25mg
| renal excretion
| * amine
ACh(n) antagonist |
| medazepam
| Nobrium, Rusedal
| anxiolytic, anticonvulsant, muscle-relaxant
| 10-30mg
| 2-5 hrs
1-15 hrs (biphasic)
| * benzodiazepine:
BZD agonist |
| medifoxamine
| Cledial, Gerdasyl
| depression
| 100-150mg
| 1 hr
| * amine
DA reuptake inhibition
5-HT2a antagonist
5-HT2c antagonist |
| mefexamide
| Timodyne, Perneuron
| depression, asthenia
| 300-600mg
| 4-6 hrs
| psychostimulant |
| melitracen
| Dixoran, Melixeran, Trausabun
| depression, analeptic
| 75-225mg
| N/A
| * TCA: |
| melperone
| Buronil, Eunerpan
| antipsychotic
| 100mg
| N/A
| * butyrophenone:
neuroleptic
DA2 antagonist
5-HT2 antagonist |
| memantine
| Namenda, Axura, Akatinol, Ebixa, Neuroplus
| Alzheimer's, Parkinson's, depression, pain disorders,
neuroprotective
| 20-40mg
| 60-80 hrs
| * cyclic amine:
NMDA antagonist |
| meprobamate
| Miltown, Equanil, Meprotabs, Meprospan, Meptran, Novalm,
Pertranquil, Promate, Vio-Bamate
| anxiolytic, sedative, hypnotic
| 1200-1600mg
(2400 max)
| 6-17 hrs
glucuronide conjugation
| * carbamate:
CNS depressant |
| mesoridazine
| Serentil, Lidanil
| antipsychotic, alcoholism, chronic brain syndrome:
| 100-400mg
| 24-48 hrs
CYP-2D6
| * piperidine
phenothiazine:
neuroleptic
DA antagonist |
| metaclazepam
| Talis
| anxiolytic
| 5-20mg
| N/A
| * benzodiazepine:
BZD agonist |
| metapramine
| Timaxil
| depression
| 150-450mg
| 7 hrs
desmethylation
| * dibenzoazepine:
NE synthesis
NE release
NMDA antagonist |
| methadone
| Dolophine, Physeptone, Methadose, Physeptone
| opioid dependence, analgesic
| 15-40mg
| 28-35 hrs
CYP-2D6
(inhibitor)
CYP-3A
UGT-UB7
| * diphenylheptane:
opioid:
opioid(mu) agonist |
| methamphetamine
| Desoxyn, Methampex, Methedrine, Pervitin, Temmler
| ADD, ADHD, obesity
| 10-25mg
| 10-25 hrs
CYP-2D6
| * psychostimulant:
5-HT release +++
NE release +++
DA release ++
DA reuptake inhibition
NE reuptake inhibition |
methotrimeprazine
(levomepromazine)
| Levoprome, Nozinan, Neurocil, Veractil, Sinogan
| antipsychotic, anxiolytic, sedative, antiemetic, analgesic
| anxiolytic: 10-25mg
AP: 50-200mg
(500 max)
| 15-30 hrs
CYP-2D6
| * phenothiazine:
DA antagonist
NE-alpha antagonist
H1 antagonist |
| methylphenidate
| Ritalin, Concerta, Metadate, Methylin, Methylphen
| ADD, ADHD, depression, CFS
| 20-30mg
(60mg max)
| 2.9 hrs
| * psychostimulant:
DA reuptake inhibition
NE reuptake inhibition
NE release |
| mexiletine
| Mexitil
| antiarrhythmic, anticonvulsant, bipolar disorder, pain
disorders,
| 300-1200mg
| 10 hrs
CYP-2D6
CYP-1A2 inhibitor
| * ethylamine:
Na+ channel inhibitor |
| mianserin
| Athymil, Bolvidon, Norval, Tolvin
| depression
| 30-90mg
| 10-17 hrs
CYP-2D6
CYP-1A2
(inhibitor)
UGT-1A4
| * tetracyclic:
NE-alpha2 antagonist
5-HT2 antagonist
H1 antagonist |
| midazolam
| Versed, Dormicum, Hypnovel
| preoperative sedation
| 5mg injectable
| 2.9-4.5 hrs
CYP-3A4
| * benzodiazepine:
BZD agonist |
mifepristone
(RU-486)
| Mifeprex, Corlux
| terminate pregnancy, bipolar disorder, psychotic
depression
| 600-1200mg
| 18 hrs
CYP-3A4
| * proponyl-estra-diene
cortisol receptor antagonist
progesterone receptor antagonist |
| milnacipran
| Ixel, Toledomin
| depression
| 50-200mg
| 8 hrs
glucuronidation
renal excretion
| * cyclopropane:
NE reuptake inhibition
5-HT reuptake inhibition |
| minaprine
| Cantor
| depression, nootropic
| 100-250mg
| 2-3 hrs
| * phenylpyridazine:
DA increase
ACh increase
ACh(m) agonist
5-HT2b antagonist
PKC activation |
| mirtazapine
| Remeron, Norset, Zipsin
| depression
| 15 - 45mg
(75mg max)
| 20-40 hrs
CYP-1A2
CYP-3A
| * piperazinoazepine:
NE-alpha2 antagonist
5-HT2a antagonist ++
5-HT2c antagonist
5-HT3 antagonist
H1 antagonist |
| moclobemide
| Aurorix, Manerix, Moclamine
| depression, social phobia
| 150 - 600mg
(1200 max)
| 1-2 hrs
CYP-2C19
| * benzamide:
RIMA |
| modafinil
| Provigil, Alertec, Modiodal
| narcolepsy, EDS, depression
| 200-400mg
| 15 hrs
hydrolysis
| * diphenyl
methylsulfinyl:
GLU release
GABA decrease
hypocretin (orexin)agonist |
| molindone
| Moban, Lindone
| antipsychotic
| 20-225mg
| 1.5 hrs
| * dihydroindolone:
neuroleptic
DA2 antagonist ++
ACh(m) antagonist ++ |
| nalmefene
| Revex, Cervene
| opioid overdose, opioid dependence, alcohol dependence,
OCD, SI
| 20-80mg
| 7-10 hrs
UGT-UB7
| * morphinane:
opioid(mu) antagonist +++
opioid(kappa) antagonist +++
opioid(delta) antagonist ++ |
| naltrexone
| Revia, Trexan
| opioid overdose, opioid dependence, alcohol dependence,
OCD, SI, depression
| 50-100mg
| 4 hrs
(6-(beta)-naltrexol 13 hrs)
UGT-UB7
| * morphinane:
opioid(mu) antagonist +++
opioid(kappa) antagonist + |
| nefazodone
| Serzone, Dutonin, Nefadar
| depression
| 300-600mg
| 2-4 hrs
CYP-3A
(mCPP 4-8 hrs CYP-2D6)
| * phenylpiperazine:
5-HT reuptake inhibition +
NE reuptake inhibition +
5-HT2a antagonist ++
5-HT1a antagonist ++
NE-alpha1 antagonist ++
* mCPP metabolite:
5-HT2b agonist ++
5-HT2c agonist ++ |
| nemifitide
| N/A
| depression
| 18mg
| N/A
| * pentapeptide: |
| nialamide
| Niamid
| depression
| 150-200mg
| N/A
| * hydrazine:
MAOI |
| nifedipine
| Procardia, Adalat
| antihypertensitive, MAOI-tyramine hypertensive crisis,
angina, migraine, bipolar disorder
| 30-120mg
(180 max)
| 2 hrs
CYP-3A (inhibitor)
| * dihydropyridine:
CCB
Ca2+(L) channel inhibition |
| nimodipine
| Nimotop, Admon, Bloquel, Norton, Oxigen, Periplum,
Regental, Vasoactin
| cerebral ischemia, subarachnoid hemorrhage, bipolar
disorder
| 180-360mg
| 8-9 hrs
CYP-3A
| * dihydropyridine:
CCB
Ca2+(L) channel inhibition |
| nisoxetine
| N/A
| depression
| 20-40mg
| N/A
| * methylpropylamine:
NE reuptake inhibition ++ |
| nitrazepam
| Mogadon, Benzolin, Eunoctin, Imeson, Insomin, Somnased,
Somnite, Sonebon,
| insomnia
| 2.5 - 10mg
| 23 hrs
(18-28 hrs)
CYP-3A
CYP-2D6
| * benzodiazepine:
BZD agonist |
| nitroxazepine
| Sintamil
| depression, nocturnal enuresis
| 75-225mg
| N/A
| * TCA |
| nomifensine
| Merital, Alival
| depression
| 100-200mg
| 2 hrs
| * tetrahydroisoquinoline:
DA reuptake inhibition +++
NE reuptake inhibition ++ |
| nortriptyline
| Pamelor, Aventyl
| depression, pain disorders
| 20 hrs (18-90 hrs)
CYP-2D6
| 50-100mg
(150mg max)
blood level:
50-150 ng/mL
| * dibenzocycloheptadiene:
secondary TCA
NE reuptake inhibition +++
5-HT reuptake inhibition +
5-HT2a antagonist ++
ACh antagonist
H1 antagonist
NE-alpha antagonist |
| noxiptiline
| Nogedal
| depression
| 25-200mg
| N/A
| * dibenzocycloheptene:
TCA
NE reuptake inhibition
5-HT reuptake inhibition
NE-alpha1 antagonist
H1 antagonist |
| olanzapine
| Zyprexa, Lanzac
| antipsychotic, mania, mood stabilizer, depression, reduce
TD
| 5-15mg
(20mg max)
| 30 hrs
(21-54 hrs)
CYP-1A2
UGT-1A4
glucuronidation
| * thienobenzodiazepine:
neuroleptic:
DA2 antagonist +
DA1 antagonist +
5-HT2a antagonist ++
5-HT2c antagonist +
NE-alpha1 antagonist +
ACh(m) antagonist ++
H1 antagonist ++ |
| omega-3 fatty acids
| OmegaBrite, Fisol
| bipolar disorder
| 2-10g
| N/A
| * phospholipid:
EPA (eicosapentaenoic acid)
DHA (docosahexaenoic acid)
enhances membrane integrity
PKC inhibition
G-Protein transduction decrease |
| ondansetron
| Zofran, Zophren
| antiemetic
| 8-16mg22
| 2.9-4.5 hrs
CYP-3A4
| * imidazole:
5-HT3 antagonist |
| opipramol
| Insidon, Oprimol
| depression
| 150-300mg
| N/A
| * dibenzoazepine:
TCA
sigma antagonist +++
5-HT2 antagonist
H1 antagonist |
| oxaflozane
| Conflictan
| depression
| 15-30mg
| 5 hrs
| * morpholine:
5-HT increase |
| oxaprotiline
| N/A
| depression
| 100-200mg
| 23-29 hrs
| * tetracyclic:
NE reuptake inhibition |
| oxazepam
| Serax, Adumbran, Alepam, Murelax, Serepax, Seresta, Vaben
| anxiolytic, alchohol withdrawal
| 20-60mg
(120mg max)
| 8 hrs
(5.7-10.9 hrs)
UGT-UB7 (inhibitor)
| * 3-hydroxy
benzodiazepine:
BZD agonist |
| oxcarbazepine
| Trileptal
| anticonvulsant, bipolar disorder, pain disorder
| 1200-2400mg
| 2 hrs
9 hrs MHD (active)
| * tricyclic
iminostilbene:
Na+ channel inhibition
Ca2+ channel inhibition |
| oxitriptan (5-HTP)
| Levotonine, Pretonine, Serotonyl, Triptene
| depression
| 150-250mg
| 4 hrs
| * 5-hydroxytryptophan:
5-HT precursor |
oxybate
(GHB)
| Xyrem, Somsanit
| narcoleptic cataplexy, anesthesia, insomnia, stroke
| 6-9grams
| 0.5-1.0 hrs
tricarboxylic acid
(Krebs cycle)
| * gamma hydroxybutyrate
GABA-B agonist
GABA increase |
| oxycodone
| Oxycontin, Ducodal, Eubine, Eucodal, Eukodal, Pancodine,
Percolone, Roxicodone, Roxilox
| analgesic, depression
| 60-180mg
(10-30mg every 4 hours)
| 3-5 hrs
CYP-2D6
UGT-2B7
| * morphinane:
opioid
opioid(mu) agonist |
| pagoclone
| N/A
| anxiolytic, GAD, panic disorder
| 0.15-0.60mg
| N/A
| * cyclopyrrolone:
GABA-A partial agonist/modulator |
| pargyline
| Eutonyl, Eudatine, Tenalin
| depression, hypertension
| 90mg
| N/A
| * propargyl:
MAOI
MAO-B inhibition ++
MAO-A inhibition + |
| paroxetine
| Paxil, Seroxat, Aropax, Deroxat
| depression, OCD, GAD, social anxiety, PTSD, panic disorder
| 20-60mg
| 15-21 hrs
CYP-2D6
(inhibitor)
| * phenylpiperidine:
SSRI
5-HT reuptake inhibition +++
ACh(m) antagonist |
| pemoline
| Cylert, Deltamine, Kethamed, Ronyl, Sigmadyn, Stimul,
Stimuzol, Tradon, Volital
| ADD, ADHD, narcolepsy, depression
| 56.25-75mg
(112.5mg max)
| 12 hrs
| * oxazolidinedione:
DA increase |
| pergolide
| Permax, Celance
| Parkinsons, depression, RLS, hyperprolactinemia
| 0.25-5mg
| CYP-2D6
(inhibitor only)
| * ergot alkaloid:
DA1 agonist
DA2 agonist |
| perphenazine
| Trilafon, Avomit, Decetan, Fentazin, Mutabon
| antipsychotic, antiemetic
| 4-16mg
(64mg max)
| 8-12 hrs
| * piperazinyl
phenothiazine:
neuroleptic
DA antagonist |
| phenelzine
| Nardil, Stinerval, Monofen, Fenelzin, Kalgan, Nardelzine
| depression, social anxiety, GAD, panic disorder, OCD
| 30-60mg
(90 mg max)
| 2 hrs
| * hydrazine:
MAOI
GABA transaminase inhibition |
| phenoxypropazine
| Drazine
| depression
| N/A
| N/A
| *
MAOI |
| phentermine
| Adipex, Banobese, Fastin, Ionamin, Zantryl
| obesity, depression
| 20-30mg
| 20 hrs
(7-20 hrs)
| * phenethylamine:
NE release ++
DA release + |
| phentolamine
| Regitine
| antihypertensive, MAOI-tyramine hypertensive crisis,
Raynaud Syndrome
| 5mg injectable
| 19 min
| * imidazoline:
NE alpha antagonist |
| phenytoin
| Dilantin, Di-Hydan, Epanutin, Epilantin, Phenhydan,
Zentropil
| anticonvulsant, aggression, mood disorders
| 300-600mg
blood-level:
10-20 mcg/mL
| 22 hrs
(7-42 hrs)
CYP-2C19
CYP-2C8/9
UGT-2B15
| * imidazolidinedione:
Na+ channel inhibition
Ca2+ channel inhibition |
| pimozide
| Orap, Antalon, Opiran, Pirium, Oralep
| antipsychotic, Tourette's
| 2-12mg
(20mg max)
| 110 hrs
CYP-3A
CYP-2D6 (inhibitor only)
| * diphenylbutylpiperidine:
neuroleptic
DA2 antagonist +++
DA3 antagonist ++
5-HT2a antagonist ++
5-HT7 antagonist
Ca2+(T) channel inhibitor |
| pinazepam
| Domar
| anxiolytic
| 10mg
| N/A
| * propargylic:
benzodiazepine
BZD agonist |
| pindolol
| Visken, Durapindol, Pectobloc Pinbetol,
| hypertension, angina, depression
| 10-60mg
| 8 hrs
(7-15 hrs)
CYP-2D6 (inhibitor)
| * aryloxypropanolamine:
BB
NE-beta antagonist
5-HT1a antagonist |
| pipamperone
| Dipiperon, Piperonyl
| antipsychotic, antiemetic
| 20-160
(400mg max)
| N/A
| * butyrophenone:
neuroleptic
DA2 antagonist
5-HT2a antagonist
NE-alpha antagonist |
| pipotiazine
| Piportil
| antipsychotic
| 5-20mg
| 11-12 hrs
| * piperidine
phenothiazine:
neuroleptic
DA2 antagonist +++
DA3 antagonist +++ |
| piracetam
| Nootropil, Axonyl, Cerebrospan, Myocalm, Stimucortex,
Normabrain
| nootropic, Alzheimer's, cerebral ischemia, myoclonus
| 1500-2500mg
| 6-8 hrs
| * pyrrolidine:
membrane fluidity increase |
| piribedil
| Trivastal
| cerebral ischemia, Parkinsons, depression
| 50-100mg
| 2-7 hrs
| * piperazine:
DA agonist |
pirlindole
(pyrazidol)
| N/A
| depression
| 150-300mg
| N/A
| * pyrazino carbazole:
RIMA
NE reuptake inhibition
5-HT reuptake inhibition |
| pivhydrazine
| Neomarsilid, Tersavid
| N/A
| N/A
| N/A
| * hydrazine:
MAOI |
| pramipexole
| Mirapex, Sifrol
| Parkinsons, depression, RLS, hyperprolactinemia
| 1.5-4.5mg
| 8-12 hrs
renal excretion
| * benzthiazole:
DA2 agonist ++
(pre > post)
DA3 agonist +++ |
| prazepam
| Centrax
| anxiolytic, hypnotic
| 5-30mg
| 60 hrs
glucuronoconjugation
| * benzodiazepine:
BZD agonist |
| prazosin
| Minipress, Alpress, Hypotens, Hypovase, Sinetens
| antihypertensive, MAOI-tyramine hypertensive crisis
| 6-20mg
(40mg max)
| 2-3 hrs
demethylation
conjugation
| * quinazoline:
NE alpha1 antagonist |
| pregabalin
| Lyrica
| anticonvulsant, anxiety disorders, depression, bipolar
disorder, pain disorders
| 150-600mg
| 6 hrs
| * isobutylgaba:
GABA increase
Ca2+(L) channel inhibition |
| primidone
| Mysoline
| anticonvulsant, bipolar disorder
| 250-1000mg
| 10 hrs
CYP-2C19
| * pyrimidinedione:
barbiturate
CNS depressant |
| prochlorperazine
| Compazine, Stemetil
| antipsychotic, antiemetic, M駭i鑽e's Disease,
labyrinthitis, vertigo
| 10-20mg
(40mg max)
| 9 hrs
| * piperazine
phenothiazine:
neuroleptic
DA2 antagonist +++
DA3 antagonist ++
NE-alpha1 antagonist ++ |
| procyclidine
| Kemadren, Arpicoline, Osnervan, Procyclid
| Parkinson's, AP-induced EPS
| 10-30mg
| 12 hrs
| * pyrrolidinyl:
ACh(m) antagonist |
profenamine
(ethopropazine)
| Pardidol, Parsidol, Parsitan, Dibutil, Lysivane, Rodipal
| Parkinsons, AP-induced EPS
| 100-600mg
| N/A
| * phenothiazine:
neuroleptic
ACh(m) antagonist |
| promazine
| Sparine
| antipsychotic, antiemetic, hiccups, alcoholic
hallucinations
| 50-1200mg
| N/A
| * phenothiazine:
neuroleptic
DA1 antagonist +
DA2 antagonist +
NE-alpha1 antagonist ++
H1 antagonist ++ |
| propranolol
| Inderal
| hypertension, angina, arrhythmia, tremor, migraine, panic
disorder, akathisia, pheochromocytoma
| 40-240mg
(640 max)
| 4 hrs
CYP-1A2
CYP-2D6 (inhibitor)
UGT-2B7
UGT-1A9
| * aryloxypropanolamine:
NE-beta antagonist |
| propizepine
| Vagran
| depression, parasympatholytic
| 50-200mg
| 8 hrs
| * benzopyridodiazepine:
TCA
NE reuptake inhibition
5-HT reuptake inhibition
ACh(m) antagonist |
| propoxyphene
| Darvon, Dolene, Margesic, Propoxy
| analgesic
| 65-390mg
| 6-12 hrs
(norpropoxyphene 30-36 hrs)
CYP-3A (inhibitor)
CYP-2C8/9
| * diphenylbutanol:
opioid
opioid agonist |
| protriptyline
| Vivactal, Triptil, Concordin, Concordine, Maximed
| depression
| 15-60mg
| 55-198 hrs
| * dibenzocycloheptene:
secondary TCA
NE reuptake inhibition +++
5-HT reuptake inhibition +
ACh(m) antagonist
NE-alpha1 antagonist |
pyrazidole
(pirlindole)
| N/A
| depression
| 150-300mg 75-225mg
| N/A
| * pyrazino carbazole:
RIMA
NE reuptake inhibition
5-HT reuptake inhibition |
| pyrovalerone
| Centroton, Thymergix
| psychostimulant, depression
| 20-80mg
| 1 hr
| * pyrrolidine:
DA reuptake inhibition |
| quazepam
| Doral, Dormalin, Prosedar, Quazium, Selepam, Temodal
| insomnia
| 7.5-15mg
(30mg max)
| 39 hrs
| * trifluoroethyl
benzodiazepine:
BZD agonist |
| quetiapine
| Seroquel
| antipsychotic
| 300-500mg
(800mg max)
| 6 hrs
CYP-3A
glucuronidation
| * dibenzothiazepine:
neuroleptic:
DA2 antagonist +
5-HT2a antagonist ++
NE-alpha1 antagonist ++
H1 antagonist +
sigma antagonist |
| quinupramine
| Kinupril, Adeprim, Kevopril,
| depression
| 2.5-15mg
| 9 hrs
| * dibenzoazepine:
TCA
NE reuptake inhibition ++
5-HT reuptake inhibition +
ACh(m) antagonist |
| reboxetine
| Edronax, Vestra
| depression
| 4-12mg
| 12 hrs
CYP-3A
| * benzyl morpholine
NE reuptake inhibition +++ |
| remoxipride
| Roxiam
| antipsychotic
| 50-150mg
| 4-6 hrs
CYP-2D6
| * substituted benzamide:
neuroleptic
DA2 antagonist +
sigma antagonist +++ |
| riluzole
| Rilutek
| ALS, depression, bipolar disorder
| 100mg
| 12 hrs
CYP-1A2
| * benzothiazole:
glutamate release inhibitor
Na+ channel inhibition |
| risperidone
| Risperdal, Risperidal, Belivon, Risperin, Rispolept,
Rispolin
| antipsychotic, depression
| AP: 4-16mg
AD: 0.5mg-2mg
| RM: 3 hrs
SM: 20 hrs
CYP-3A
P-gp
| * benzisoxazole:
neuroleptic
DA2 antagonist ++
5-HT2a antagonist +++
NE-alpha antagonist ++
H1 antagonist + |
| ritanserin
| Tisterton
| sleep architecture (increase slow-wave; decrease REM),
depression (AD augmentation), dysthymia, schizophrenia (AP
augmentation), AP-induced EPS
| 5-10mg
(30mg max)
| 39 hrs
(20-60 hrs)
| * thiazolopyrimidine:
5-HT2a antagonist +++
5-HT2b antagonist +++
5-HT2c antagonist +++ |
| rolipram
| N/A
| depression, multiple sclerosis, AIDS
| 0.75-1.5mg
| 12 hrs
| * pyrrolidinone:
cAMP PDE-IV inhibition
TNF release inhibition |
| ropinirole
| Requip
| Parkinsons, depression, RLS
| 0.75-3.0mg
| 6 hrs
CYP-1A2
CYP-3A
CYP-2D6 (inhibitor only)
| * dipropylamine:
DA3 agonist ++
DA2 agonist + |
| roxindole
| N/A
| depression
| 7.5-30mg
| N/A
| * tetrahydropyridine:
DA2 agonist +
(pre > post)
DA3 agonist ++
5-HT1a agonist ++
5-HT reuptake inhibition |
| safrazine
| Safra
| depression, social anxiety, GAD, OCD
| 5mg
| N/A
| * pyrimidine:
MAOI |
| selegiline (l-deprenyl)
| Eldepryl, Jumex, Carbex, Eldeprine, Atapryl, Jumexal,
Lesotal, Movergan, Emsam
| Parkinsons, depression, Alzheimer's
| 5-30mg
(60mg max)
| 2-10 hrs
CYP-2C19
CYP-2B6
| * propargyl:
MAOI
MAO-B inhibition ++
MAO-A inhibition + |
| sertindole
| Serlect, Serdolect
| antipsychotic
| 20-24mg
| 60-73 hrs
| * imidazolidinone:
neuroleptic
DA2 antagonist
5-HT2a/c antagonist +++
NE-alpha1 antagonist ++
|
| sertraline
| Zoloft, Lustral
| depression, PTSD, OCD, panic disorder
| 50-200mg
| 26 hrs
CYP-2C19 (inhibitor)
CYP-2D6
CYP-2B6
| * naphtalamine:
5-HT reuptake inhibition +++
DA reuptake inhibition + |
| sibutramine
| Meridia, Reductil
| obesity, depression
| 5-15mg
| 1-2 hrs
CYP-3A
| * dimethylamine+
5-HT reuptake inhibition ++
NE reuptake inhibition ++
DA reuptake inhibition + |
| sodium valproate
| Depacon, Epilim, Valpro
| anticonvulsant, migraine, bipolar disorder
(mood-stabilizer)
| 750-3000mg
(50-125mcg/ml)
| 9-16 hrs
CYP-2C9 (inhibitor)
CYP-2A6
glucoronidation
| * carboxylic acid:
Na+ channel inhibition
Ca2+(T) channel inhibition
GABA increase:
1. GABA transaminase inhibition
2. SSAD dehydrogenase inhibition |
| sulpiride
| Sulparex, Dogmatil, Dolmatil, Valirem
| antipsychotic, depression, dysthymia
| AP: 400-2400mg
AD: 50-200mg
| 8 hrs
renal excretion
| * benzamide:
neuroleptic
DA2 antagonist +
(pre > post)
DA3/4 antagonist ++ |
| tandospirone
| N/A
| depression, anxiolytic
| N/A
| N/A
| * azapirone:
5-HT1a partial agonist |
| talipexole
| N/A
| Parkinsons, depression, PTSD
| N/A
| N/A
| *
D2 agonist
NE alpha2 agonist |
| temazepam
| Restoril
| insomnia
| 10 - 20mg
| 8 hrs
CYP-2B6
CYP-3A
UGT-2B7
| * benzodiazepine:
BZD agonist |
| tetrindole
| N/A
| depression
| 150-300mg
| N/A
| * pyrazino-indole
tetracyclic:
RIMA
Ca2+ channel inhibition |
| thioridazine
| Mellaril
| antipsychotic
| 30-200mg
(800mg max)
| 7-9 hrs
CYP-2D6 (inhibitor)
| * phenothiazine:
neuroleptic
DA1 antagonist
DA2 antagonist |
| thiothixene
| Navane
| antipsychotic
| 15-30mg
(60 max)
| 34 hrs
CYP-1A2
| * thioxanthene:
neuroleptic
DA1 antagonist
DA2 antagonist |
| thyroxine (T4)
| Synthroid, Levoxyl, Levothroid
| hypothyroidism, depression, bipolar disorder
| 100-400mcg
| 6-7 days
glucuronoconjugation
| * thyroid hormone:
NE receptor sensitivity increase
MAO inhibition
|
| tiagabine
| Gabitril
| anticonvulsant, bipolar disorder
| 32-56mg
| 7-9 hrs
CYP-3A
| * piperidine:
GABA reuptake inhibition |
| tianeptine
| Ardix, Stablon
| depression
| 25-50mg
| 2-3 hrs
b-oxidation
n-desmethylation
| * dibenzothiazepine:
5-HT reuptake accelerator |
| tiospirone
| N/A
| antipsychotic
| 50-75mg
| N/A
| *
neuroleptic
DA2 antagonist +++
5-HT2a/c antagonist +++
sigma ligand |
| tolcapone
| Tasmar
| Parkinsons, depression
| 200-600mg
| 3 hrs
glucuronidation
| * nitrobenzophenone:
COMT inhibition |
| toloxatone
| Humoryl, Perenum
| depression
| 600mg
| 1-2 hrs
| * oxazolidinone:
RIMA |
tomoxetine
(atomoxetine)
| Strattera
| ADD, ADHD, depression
| 50-150mg
(1.2-1.8mg/kg)
| 5 hrs
(5-24 hrs)
CYP-2D6
| * tolyloxypropylamine:
NE reuptake inhibition +++ |
| topiramate
| Topomax
| anticonvulsant, bipolar disorder
| 200-400mg
(1600 max)
| 21 hrs
glucuronidation
CYP-2C19
| * monosaccharide:
Na+ channel inhibition
Ca2+(L) channel inhibition
GABA-A receptor enhancement
GLU antagonist |
| tramadol
| Ultram, Contramal, Topalgic, Zamudol, Zumalgic
| analgesic
| 100-400mg
| 6-8 hrs
CYP-2D6
CYP-3A
glucuronidation
| * opioid:
opioid(mu) agonist
NE reuptake inhibition +
5-HT reuptake inhibition + |
| tranylcypromine
| Parnate, Parmodalin, Sicoton, Transamin, Transapin,
Tylciprine
| depression
| 20-60mg
(120mg max)
| 2 hrs
CYP-2C19 (inhibitor only)
| * cyclopropylamine:
MAOI |
| trazodone
| Desyrel, Molipaxin, Pragmarel, Thombran, Trazodil,
Trazolan, Trittico
| depression, insomnia
| AD: 100-600mg
hypnotic: 25-150mg
| 5-9 hrs
CYP-3A
mCPP: CYP-2D6
| * phenylpiperazine:
5-HT reuptake inhibition +
5-HT2a antagonist ++
5-HT1a antagonist ++
NE-alpha1 antagonist ++
* mCPP metabolite:
5-HT2b agonist ++
5-HT2c agonist ++ |
| triazolam
| Halcion, Songar, Triazoral, Alpralid
| insomnia
| 0.125-0.5mg
| 3 hrs
(1.5-5.5)
CYP-3A
| * triazolo
benzodiazepine:
BZD agonist |
| trifluoperazine
| Stelazine, Terfluzine, Stalabid, Eskazinyl, Jatroneural,
Sedizine
| antipsychotic, anxiolytic
| 4-20mg
(40 max)
| 10-14 hrs
UGT-1A4
| * piperazine
phenothiazine:
neuroleptic
DA1 antagonist
DA2 antagonist |
| trifluopromazine
| Vesprin, Psyquil, Psiquil, Siquil, Vesprin
| antipsychotic, antiemetic
| 25-200mg
| N/A
| * phenothiazine:
neuroleptic
DA antagonist |
| trihexyphenidyl
| Artane
| Parkinsons, AP-induced EPS, antispasmodic
| 1.5-15.0mg
| 8-10 hrs
| * ACh(m) antagonist
H1 antagonist |
triiodothyronine (T3)
(also liothyronine)
| Cytomel
| hypothyroidism, depression, bipolar disorder
| 25-100mcg
| 1-2 days
| * thyroid hormone:
NE receptor sensitivity increase
MAO inhibition
|
| trimipramine
| Surmontil, Rhotrimine
| depression
| 50-200mg
(300mg max)
| 24 hrs
CYP-2D6
CYP-3A
CYP-2C19
| * dibenzazepine:
tertiary TCA
DA2 antagonist
5-HT2a antagonist ++
NE-alpha1 antagonist
Ca2+ channel inhibition
ACh(m) antagonist
H1 antagonist |
| valproate
| Depakote, Epival, Elvetium, Everiden, Novoseven, Valcote,
Valnar
| anticonvulsant, migraine, bipolar disorder
(mood-stabilizer)
| 750-3000mg
(50-125mcg/ml)
| 9-16 hrs
CYP-2C9 (inhibitor)
CYP-2A6
glucoronidation
| * carboxylic acid:
Na+ channel inhibition
Ca2+(T) channel inhibition
GABA increase:
1. GABA transaminase inhibition
2. SSAD dehydrogenase inhibition |
| valproic acid
| Depakene, Convulex, Depakine, Depalept, Epilim, Ergenyl,
Leptilan, Orfiril, Valporal
| anticonvulsant
| 750-3000mg
(50-125mcg/ml)
| 9-16 hrs
CYP-2C9 (inhibitor)
CYP-2A6
glucoronidation
| * carboxylic acid:
Na+ channel inhibition
Ca2+(T) channel inhibition
GABA increase:
1. GABA transaminase inhibition
2. SSAD dehydrogenase inhibition |
| venlafaxine
| Effexor, Efexor, Trevilor, Vandral
| depression, anxiety disorders, GAD, ADD, ADHD, OCD,
fibromyalgia
| 75-300mg
(600mg max)
| 5-7 hrs
CYP-2D6
| *
cyclohexanol:
SNRI
5-HT reuptake inhibition +++
NE reuptake inhibition ++
DA reuptake inhibition + |
| verapamil
| Calan, Isoptin, Azupamil, Cardibeltin, Civicor, Cordilox,
Durasoptin, Veramex, Verelen
| hypertension, angina, arrhythmia, bipolar disorder
| 240-480mg
| 5-12 hrs
CYP-2C19
CYP-3A (inhibitor)
CYP-2C8/9
| * valeronitrile:
CCB
Ca2+(L) channel inhibition |
| vigabatrin
| Sabril
| anticonvulsant, bipolar disorder
| 2000-4000mg
| 5-8 hrs
| * gamma-vinyl-GABA:
GABA increase
GABA transaminase inhibition |
| vilazodone
| N/A
| depression
| N/A
| N/A
| * phenylpiperazine:
5-HT reuptake inhibitor
5-HT1a partial agonist |
| viloxazine
| Vivalan
| depression
| 15-30mg
| 2-5 hrs
| * morpholine:
NE reuptake inhibitor +++ |
| viqualine
| N/A
| depression, alcohol dependency
| 100-200mg
| 12 hrs
| * quinoline:
5-HT reuptake inhibition
5-HT release |
| yohimbine
| Aphrodyne, Procomil, Procamil, Yocon
| sympathicolytic, myDA reuptake inhibitionatic, penile
dysfunction, depression
| 8.1-16.2mg
| 30-60 minutes
CYP-2D6
| * indole alkaloid:
NE-alpha2 antagonist
5-HT1a agonist
5-HT1b/d antagonist
DA increase
NE increase
5-HT decreased |
| zaleplon
| Sonata
| insomnia
| 5-20mg
| 1.5 hrs
CYP-3A
aldehyde oxidase
| * pyrazolopyrimidine:
GABA-A BZD(1) agonist |
| zimeldine
| Zelmid
| depression, migraine, obesity
| 75-300mg
| 8 hrs
| * dimethylallylamine:
SSRI
5-HT reuptake inhibition +++ |
| ziprasidone
| Geodon, Zeldox
| antipsychotic, depression
| 40-160mg
(200mg max)
| 7 hrs
aldeyde oxidase
| *
neuroleptic
DA2 antagonist ++
DA3 antagonist ++
5-HT1a agonist ++
5-HT1d antagonist
5-HT2a antagonist +++
NE reuptake inhibition
5-HT reuptake inhibition |
| zolpidem
| Ambien, Stilnox
| insomnia
| 5 - 10mg
| 2.6 hrs
CYP-1A2
CYP-3A
CYP-2C8/9
| * imidazopyridine:
GABA-A BZD(1) agonist |
| zonisamide
| Zonegran
| anticonvulsant, bipolar disorder
| 100-600mg
| 50-70 hrs
CYP-3A
glucuronidation
| * sulfonamide:
Na+ channel inhibition
Ca2+(T) channel inhibition
DA increase |
| zopiclone
| Imovane, Rhovane, Zimovane
| insomnia
| 3.75-7.5mg
| 5 hrs
CYP-2C8/9
CYP-3A
| * cyclopyrrolone:
GABA-A BZD(1) agonist |
| zotepine
| Zoleptil
| antipsychotic
| 100-300mg
| N/A
| *
neuroleptic
DA antagonist
5-HT2a antagonist |
| zuclopenthixol
| Clopixol
| antipsychotic
| 10-50mg
(200mg max)
| 20 hrs
| * thioxanthene:
neuroleptic
DA1 antagonist
DA2 antagonist |
