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7/31/2019 Psychopharmacology Lecture
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Psychopharmacology
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Main PsychopharmacologicalDrugs
AntipsychoticsAntidepresantsAnxiolyticsHypnoticsCognitives
Psychostimulants
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Overview of AntipsychoticsConventional Antipsychotics
Chem. Group Generic Name Trade Mark Dose (mg)
Phenothiazines
chlorpromazine CHLORPROMAZIN,LARGACTIL,PLEGOMAZIN,MEGAPHEN,THORAZIN
200-800
levomepromazine
TISERCIN, NOZINAN 50-400
thioridazine THIORIDAZIN,MELLERIL
100-600
periciazine NEULEPTIL 10-40
Thioxanthes
chlorprothixene CHLORPROTHIXEN,TRUXAL
100-600
clopenthixol CISORDINOL,
CLOPIXOL
20-100
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Overview of AntipsychoticsConventional Antipsychotics
Chem. Group Generic Name Trade Mark Dose (mg)
Phenothiazines
perfenazine PERFENAZIN,TRILAFON, PERATSIN
16-24
prochlorperazine
PROCHLORPERAZIN,STEMETIL
20-80
flufenazine MODITEN 2-16
trifluoperazine STELAZIN 10-50
Thioxanthenes flupenthixol FLUANXOL 6-18
Butyrophenoneshaloperidol HALOPERIDOL, HALDOL,
APO-HALOPERIDOL2,5-10
melperoneBURONIL
50-300
Diphenylbutylpiperidines
pimozide ORAP 2-10
fluspirilen IMAP 2-10
penfluridol SEMAP 2-60
Perathiepines oxyprothepin MECLOPIN 5-20
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Antipsychoticsof the 2 nd Generation
Generic Name Trade Mark Dose (mg)
D2, D3 selective antagonists
sulpiride DOGMATIL, PROSULPIN 50-1200
amisulpride SOLIAN, DENIBAN 50-1200
SDArisperidone RISPERDAL, RISPEN 4-8
ziprasidone ZELDOX 40-160
sertindole SERDOLECT 12-20
MARTA
clozapine LEPONEX 200-600
olanzapine ZYPREXA 5-20
quetiapine SEROQUEL 300-600
zotepine ZOLEPTIL 75-300
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Antipsychoticsof the 2 nd Generation
Efficacy1. Positive symptoms are influenced significantly better than
placebo, and equally or more then by the classicalantidopaminergic neuroleptics.
2. Negative symptoms are reduced significantly better than by
placebo or classical antidopaminergic neuroleptics.3. Affective symptoms are influenced better than by placebo or
classical antidopaminergic neuroleptics.4. They significantly reduce or prevent the cognitive
impairment. The reduction is higher in comparison to
classical antidopaminergic neuroleptics.5. The treatment resistant patients with schizophrenia are
improved significantly better than by placebo and at leastequally as by clozapine.
6. Maintenance treatment is more effective than maintenance
on placebo and at least as effective as maintenance onclassical neuroleptics.
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Depot AntipsychoticsGeneric Name Trade Mark Mean Dose
(mg)Interval
flufenazin MODITEN DEPOT 25
14-28days
oxyprothepin MECLOPIN 25
haloperidol HALDOL DEPOT 100
flupenthixol FLUANXOL DEPOT 40
zuclopenthixol CISORDINOLDEPOT
200
fluspirilen IMAP 6 7 days !!
risperidone RISPERDALCONSTA
20-30 14 days
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Rapid Tranquilizers
pro dosi (mg) pro die (mg)
chlorpromazin 100-200 800-1200
levopromazin
(TISERCIN)
50-100 500-600
haloperidol 5-10 40-100
chlorprothixen 100-150 500-600
zuclopenthixol(CISORDINOLACUTARD)
50-150 (24-72hours)
tiapride(TIAPRIDAL)
600-1200
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Indication of Antidepressants
Depressive DisturbancesAffective DisordersObsessive-Compulsive Disorders
Panic DisordersEating DisordersPsychosomatic DisordersPosttraumatic Stress DisorderAlcohol and Drugs Withdrawal SymptomsPain SyndromesEnuresis
Narcolepsy
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Neurotransmitter Reuptake Inhibitionand Binding Affinity to Receptors
Receptors:SE Serotonergic
NE Noradrenergic
M Muscarinic
H Histaminic
-N alpha noradrenergic
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Antidepressants:Monoamine Reuptake Inhibitors
1st Generation of Antidepressants (TCA, TeCA)
Generic Name Trade Mark Doses (mg) Mechanism of Efficacy
amitriptyline AMITRIPTYLIN 75-200
Inhibition of Serotoninand/orNorepinephrineReuptakeFollowed byIncrease of theirConcentrationsin SynapticCleft
nortriptyline NORTRILEN 50-150
imipramine MELIPRAMIN 75-250
clomipramine ANAFRANIL,
HYDIPHEN
75-225
dosulepin PROTHIADEN 100-300
dibenzepine NOVERIL 240-720
maprotiline LUDIOMIL,MAPROTILINE
75-150
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1 st Generation of Antidepressants
Mechanism of action:Blockade of muscarine receptorsHistamine H1 receptors
Alpha 1 Adrenergic ReceptorsAlpha 2 Adrenergic Receptors
Many Side EffectsDanger of IntoxicationMany Interactions
Prolonged Effect (after 3-6 Weeks)
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2nd Generation of Antidepressants
2 nd Generation of Antidepressants
Generic Name Trade Mark Mean Doses(mg)
Mechanism
viloxazine VIVALAN 100-300 Norepinephrine
ReuptakeInhibition
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3 rd Generation of Antidepressants
Generic Name Trade Mark Mean Doses(mg)
Mechanism
SSRI
fluvoxamine FEVARIN 100-300
SelectiveSerotonin
ReuptakeInhibition
fluoxetine DEPREX, DEPRENON,PROZAC, PORTAL,FLOXET, FLUXONIL,MAGRILAN
20-60
citalopram SEROPRAM, CITALEC 20-60
escitalopram CIPRALEX 10-20
paroxetine SEROXAT, PAROLEX 20-60
sertraline ZOLOFT, SERLIFT,ASENTRA 50-200
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3 rd Generation of Antidepressants
Generic Name Trade Mark Mean Doses(mg) Mechanism
SARIAntidepressants with Doubled Serotonergic Efficacy
trazodone TRITTICO AC 4-8
Double SerotonergicEfficacynefazodone SERZONE,
DUTONIN100-300
NARI
reboxetine EDRONAX 4-8 NorepinephrineReuptake Inhibition
tianeptine COAXIL 75 Increasing of Serotonin
Reuptake
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4 th Generation of AntidepressantsDual acting antidepressants
Mixed reuptake inhibitors
Generic Name Trade Mark Mean Doses(mg)
Mechanism
SNRI
venlafaxine EFECTIN 75-375
Serotonin andNorepinephrineReuptake Inhibition
venlafaxineER (extendedrelesase)
EFECTIN ER 75-225
milnaciprane IXEL 50-100
DNRI
bupropione WELLBUTRINZYBAN
150-300 Dopamine andNorepinephrine
Reuptake Inhibition
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4 th Generation of Antidepressants
Generic Name Trade Mark Mean Doses(mg)
Mechanism
Blockade of 2 -adrenoceptors
mianserin LERIVON,
MIABENE
60-90 Increasing Synthesis and
Releasing of Norepinephrine, BlockadeAlpha-2 Adrenoceptorson Serotonergic Neuronsand Increasing
Production and Releasingof Serotonin
mirtazapine REMERON 15-45
Other Monoamine Reuptake Inhibitors
hypericum
perforatum
JARSIN 900 Weak Inhibitor of NA, 5-
HT, DA
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MAO Inhibitors
Non Selective and Irreversible: (IMAO A, IMAO B) phenelzine NARDIL
isocarboxazid MARPLAN
nialamide NIAMID, NUREDALtranylcypromine PARNATE
Selective and Reversible
MAO A
moclobemide AURORIXbrofaromine CONSONAR
toloxatone HUMORYL
MAO B selegiline (L-deprenyl) SEPATREM, JUMEX
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Other Psychotropics with Antidepressant Effect
Thymoprophylacticslithium LITHIUM CARBONICUM, CONTEMNOL
Antiepilepticsof 2ndGeneration
carbamazepine BISTON, TEGRETOL, FINLEPSIN,TIMONILsalts of valproic
acid
EVERIDEN, CONVULEX, ORFIRIL,DEPAMID
Antiepilepticsof 3rdGeneration
lamotrigine LAMICTAL
gabapentine GABAPENTIN, NEURONTIN
topiramate TOPAMAX
Atypical Antipsychotics - SDAclozapine LEPONEX, CLOZARIL, ALEMOXAN
olanzapine ZYPREXA
quetiapine SEROQUEL
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Thymoprophylactics
Generic Name Trade Mark Doses (mg) Blood SerumConcentration
lithiumcarbonicum
LITHIUMCARBONICUM 900
1000 0.5 0.8
mmol/l
CONTEMNOL 1000 - 1500 0.8 1.2
mmol/l
carbamazepineBISTON,TEGRETOL,TIMONIL
400 - 1500 5
10ng/ml
valproic acid EVERIDEN,ORFIRIL, 900 - 200050 - 100
ng/ml
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Action Profiles of Benzodiazepines
Relief of anxiety
Anticonvulsant Sedationaction Induction of sleep
Muscle relaxation
Ansseau, M., Doumont, A., Diricq, S.: Methodology required to show clinical
differences between benzodiazepines. Curr Med Res Opin 8 , Suppl. 4, 108-114 (1984). (Except and )
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Benzodiazepine Anxiolytics
Indication:States of AnxietySleeplessnessWithdrawal SymptomsDepressive StatesEpilepsyConvulsionsTetanus NeonatorumExtrapyramidal Undesirable Side Effects of AntipsychoticsPremedication in AnaestesiologyPanic States (Alprazolam, Bromazepam,Clonazepam in High Doses)
Algidic Syndromes (Stomatodynie, NeuralgieTrigemini, Cephalgia)
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AnxiolyticsGeneric Name Trade Mark Form Mean Doses (mg)
Propandiol Derivates
guaiphenesine GUAJACURAN drg. 200, 400 mginj. 1 g
400 - 3000
Mephenoxalone DORSIFLEX,DIMEXOL
tbl. 200 mg 400 - 1200
meprobamate MEPROBAMATLIVA
tbl. 400 mg 800 - 2400
Piperazin Derivates
hydroxyzine ATARAX tbl. 10, 25 mginj. 100 mgsir.
20
100300 - 400
Azapiron Derivatesbuspirone BUSPIRON,
BUSPAR,ANXIRON
tbl. 5, 10 mg 15-30
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Anxiolytics (Benzodiazepine Derivates)Generic Name Trade Mark Form Mean Doses
(mg)diazepam DIAZEPAM SLOVAKOFARMA
APO-DIAZEPAMAPAURIN, SEDUXENDIAZEPAM DESITINDIAZEPAM DESITIN SUPP.
tbl.2.5; 10 mginj. 10 mg
supp. 5 mg
10 - 60
chlordiazepoxide DEFOBIN, ELENIUMRAPEDUR
tbl. a drg.10 mg
20 - 60
oxazepam OXAZEPAM LIVA tbl. 10 mg 10 - 60
alprazolam NEUROLXANAXXANAX SR
tbl. 0.25 mg ; 1 mgtbl. 0.25; 0.5; 1; 2 mgtbl. 1; 2; 3 mg
1 - 10
bromazepam LEXAURIN tbl. 1; 5; 3 mg 3 - 36
medazepam ANSILAN, RUDOTEL tbl. 10 mg 20 - 40
tofisopam GRANDAXIN tbl. 50 mg 100 - 400
K+ clorazepate TRANXENE tbl. 5; 10; 50 mginj. 20; 50; 100 mg 15 3050 - 300lorazepam TAVOR tbl. 1; 2,5 mg 2
clobazam FRISIUM tbl. 10 mg 20 - 60
prazepam DEMETRIN tbl. 10 mg 20 - 40
clonazepam RIVOTRIL
ANTELEPSIN
tbl. 0.5 ; 2 mggttae 10-25 mg/mlinj. 1 mgtbl. 0.25; 1 mg
1 - 4
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Anxiolytics
32
60 60
8
32
24
6
20
63
0
10
20
30
40
50
60
diazepam alprazolam bromazepam clonazepam clobazam
Anxiolytic (eventuallyAntidepressive) EffectInhibition
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HypnoticsGeneric Name Trade Mark Form Mean Doses
(mg)
1st
Generation barbiturateschloralhydrate CHLORALOURAT 500 1000glutethimide NOXYRON tbl. 250 mg 250 - 500
2 nd Generation nitrazepam NITRAZEPAMSLOVAKOFARMAFORTE
tbl. 5; 10 mg 5 - 20
flunitrazepam ROHYPNOL tbl. 1 a 2 mginj. 2 mg
0.5 21 - 2
triazolam HALCION tbl. 0.125 mg 0.125 0.5midazolam DORMICUM tbl. 7.5 a 15 mg
inj. 5 mg7.5 15
cinolazepam GERODORM tbl. 40 mg 20 403 rd Generation zolpidem STILNOX,
HYPNOGENtbl. 10 mg 10 - 20
zopiclone IMOVANE tbl. 7.5 mg 3.75 7.5zaleptone SONATA tbl. 10 mg 5 10
Other Drugswith HypnoticEfficacy
Antihistaminics (promethazine PROTHAZIN)Antidepressants (mirtazapine, trazodone)AntipsychoticsMelatonins
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Cognitives
ACETYLCHOLINESTERASE INBITORS
rivastigmine EXELON 8 -12 mg
donepezil ARICEPT 5 - 10 mg
galantamine REMINYL 8 - 24 mg
NMDA (N-methyl-D-aspartate) RECEPTOR ANTAGONISTS
memantine EBIXA 10 - 30 mg
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Psychostimulants
Generic Name Trade Mark Doses (mg)
amphetamine PSYCHOTON,ADDERAL
5 50
dexamphetamine DEXEDRON 5
30
ephedrine EPHEDRIN 12,5 50
mezocarb SYDNOCARB 5 50
methylphenidate RITALIN,CENTEDRIN
10 40
modafinil VIGIL,PROVIGIL
200 400
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