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Brain, Behavior & Psychopharmacology
dr. Prianto Djatmiko, Sp.KJ
The BRAIN
Limbic System
The Na+/K+ ATPase Na+/K+ ATPase is a pump that uses the energy from the hydrolysis of ATP to actively pump sodium and potassium ions against their concentration. The binding of three sodium ions to internal binding sites on the cytoplasmic side of the pump and phosphorylation of the pump induces a conformational change that releases the Na+ ions into the extracellular space. The subsequent binding of two potassium ions to the pump within the synapse followed by dephosphorylation causes it to return to its original confirmation and release the potassium ions into the cytoplasm. This pump is found in almost all cells of the body and the ionic gradient that it creates is used to carry out numerous important cellular processes, such as the transport of other molecules across membrane eg the monoamines.*
4.*Drug Action on Synaptic TransmissionAntagonist drugs are in red, Agonists are in blue
The areas of the brain affected in schizophrenia
Main Psychopharmacological DrugsAntipsychoticsAntidepresantsAnxiolyticsHypnoticsCognitive EnhancerPsychostimulants
Overview of Antipsychotics
Conventional AntipsychoticsChem. GroupGeneric NameTrade MarkDose (mg)PhenothiazineschlorpromazineCHLORPROMAZIN, LARGACTIL300-600levomepromazineNOZINAN 50-400thioridazineMELLERIL100-600
ThioxantheschlorprothixeneCHLORPROTHIXEN100-600clopenthixolCLOPIXOL20-100
Overview of Antipsychotics
Conventional AntipsychoticsChem. GroupGeneric NameTrade MarkDose (mg)PhenothiazinesperfenazinePERFENAZIN, TRILAFON16-24prochlorperazineSTEMETIL20-80flufenazineMODITEN2-16trifluoperazineSTELAZIN10-50ThioxanthenesflupenthixolFLUANXOL6-18ButyrophenoneshaloperidolHALOPERIDOL, HALDOL2,5-10melperoneBURONIL50-300DiphenylbutylpiperidinespimozideORAP2-10fluspirilenIMAP2-10penfluridolSEMAP2-60
Antipsychoticsof the 2nd Generation
Generic NameTrade MarkDose (mg)D2, D3 selective antagonistssulpirideDOGMATIL50-1200amisulprideSOLIAN, DENIBAN50-1200SDArisperidoneRISPERDAL, RISPEN, RISPERDAL QUICKLET4-8ziprasidoneZELDOX40-160sertindoleSERDOLECT12-20
clozapineCLOZARIL200-600olanzapineZYPREXA 5-20quetiapineSEROQUEL300-600zotepineZOLEPTIL75-300
Antipsychoticsof the 2nd GenerationEfficacyPositive symptoms are influenced significantly better than placebo, and equally or more then by the classical antidopaminergic neuroleptics.Negative symptoms are reduced significantly better than by placebo or classical antidopaminergic neuroleptics.Affective symptoms are influenced better than by placebo or classical antidopaminergic neuroleptics.They significantly reduce or prevent the cognitive impairment. The reduction is higher in comparison to classical antidopaminergic neuroleptics.The treatment resistant patients with schizophrenia are improved significantly better than by placebo and at least equally as by clozapine.Maintenance treatment is more effective than maintenance on placebo and at least as effective as maintenance on classical neuroleptics.
Depot Antipsychotics
Generic NameTrade MarkMean Dose (mg)IntervalflufenazinMODECATE DEPOT2514-28 daysoxyprothepinMECLOPIN25haloperidolHALDOL DECANOAT100flupenthixolFLUANXOL DEPOT40zuclopenthixolCISORDINOL DEPOT200risperidoneRISPERDAL CONSTA20-3014 days
Rapid Tranquilizers
pro dosi (mg)pro die (mg)chlorpromazin100-200800-1200haloperidol5-1040-100zuclopenthixol (CISORDINOL ACUTARD)50-150(24-72 hours)
Indication of AntidepressantsDepressive DisturbancesAffective DisordersObsessive-Compulsive DisordersPanic DisordersEating DisordersPsychosomatic DisordersPosttraumatic Stress DisorderAlcohol and Drugs Withdrawal SymptomsPain SyndromesEnuresisNarcolepsy
Antidepressants:Monoamine Reuptake Inhibitors
1st Generation of Antidepressants (TCA, TeCA)Generic NameTrade MarkDoses (mg)Mechanism of Efficacyamitriptyline AMITRIPTYLIN75-200Inhibition of Serotonin and/or Norepinephrine Reuptake Followed by Increase of their Concentrations in Synaptic CleftnortriptylineNORTRILEN50-150imipramineTOFRANIL75-250clomipramineANAFRANIL75-225dosulepinPROTHIADEN100-300dibenzepineNOVERIL240-720maprotilineLUDIOMIL75-150
1st Generation of AntidepressantsMechanism of action:Blockade of muscarine receptorsHistamine H1 receptorsAlpha 1 Adrenergic ReceptorsAlpha 2 Adrenergic Receptors
Many Side EffectsDanger of IntoxicationMany InteractionsProlonged Effect (after 3-6 Weeks)
2nd Generation of Antidepressants
Generic NameTrade MarkMean Doses (mg)MechanismSSRIfluvoxamineLUVOX 100-300Selective Serotonin Reuptake InhibitionfluoxetinePROZAC20-60citalopramSEROPRAM20-60escitalopramCIPRALEX 10-20paroxetineSEROXAT20-60sertralineZOLOFT50-200
2nd Generation of Antidepressants
Generic NameTrade MarkMean Doses (mg)MechanismSARIAntidepressants with Doubled Serotonergic EfficacytrazodoneTRAZONE50-100Double Serotonergic EfficacynefazodoneSERZONE100-300
tianeptineSTABLON75Increasing of Serotonin Reuptake
2nd Generation of AntidepressantsDual acting antidepressantsMixed reuptake inhibitors
Generic NameTrade MarkMean Doses (mg)MechanismSNRIvenlafaxineEFEXOR75-375Serotonin and Norepinephrine Reuptake Inhibitionvenlafaxine ER (extended relesase)EFEXOR75-225milnacipraneDALCIPRAN50-100DNRIbupropioneWELLBUTRIN 150-300Dopamine and Norepinephrine Reuptake Inhibition
2nd Generation of Antidepressants
Generic NameTrade MarkMean Doses (mg)MechanismBlockade of 2-adrenoceptorsmianserinLERIVON, MIABENE60-90Increasing Synthesis and Releasing of Norepinephrine, Blockade Alpha-2 Adrenoceptors on Serotonergic Neurons and Increasing Production and Releasing of Serotonin mirtazapineREMERON, ESPRITAL, REMERON sol. tab.15-45Other Monoamine Reuptake Inhibitorshypericum perforatumJARSIN900Weak Inhibitor of NA, 5-HT, DA
MAO Inhibitors
Selective and Reversible: (RIMA)
MAO AmoclobemideAURORIXbrofaromineCONSONARtoloxatoneHUMORYLMAO Bselegiline (L-deprenyl)SEPATREM, JUMEX
Other Psychotropics with Antidepressant Effect
ThymoprophylacticslithiumLITHIUM CARBONICUM, CONTEMNOLAntiepileptics of 2nd GenerationcarbamazepineBISTON, TEGRETOL, FINLEPSIN, TIMONILsalts of valproic acidEVERIDEN, CONVULEX, ORFIRIL, DEPAMIDAntiepileptics of 3rd GenerationlamotrigineLAMICTALgabapentineGABAPENTIN, NEURONTINtopiramateTOPAMAXAtypical Antipsychotics - SDAclozapineLEPONEX, CLOZARIL, ALEMOXANolanzapineZYPREXAquetiapineSEROQUEL
Action Profiles of BenzodiazepinesRelief of anxiety
Anticonvulsant Sedationaction Induction of sleep
Muscle relaxationAnsseau, 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 )
Benzodiazepine AnxiolyticsIndication:States of AnxietySleeplessnessWithdrawal SymptomsDepressive StatesEpilepsyConvulsionsTetanus NeonatorumExtrapyramidal Undesirable Side Effects of AntipsychoticsPremedication in AnaestesiologyPanic States (Alprazolam, Bromazepam, Clonazepam in High Doses)Algidic Syndromes (Stomatodynie, Neuralgie Trigemini, Cephalgia)
Anxiolytics
Generic NameTrade MarkFormMean Doses (mg) Propandiol DerivatesguaiphenesineGUAJACURANdrg. 200,400mginj. 1 g400 - 3000MephenoxaloneDORSIFLEX, DIMEXOLtbl. 200 mg400 - 1200meprobamateMEPROBAMAT LIVAtbl. 400 mg800 - 2400 Piperazin DerivateshydroxyzineATARAXtbl. 10, 25 mginj. 100 mgsir.20 100300 - 400 Azapiron DerivatesbuspironeANXIRON, BUSPIRON-EGIS tbl. 5, 10 mg15-30
Anxiolytics (Benzodiazepine Derivates)
Generic NameTrade MarkFormMean Doses (mg)diazepamDIAZEPAM SLOVAKOFARMAAPO-DIAZEPAMAPAURIN, SEDUXENDIAZEPAM DESITINDIAZEPAM DESITIN SUPP.tbl.2.5; 10 mginj. 10 mg
supp. 5 mg10 - 60chlordiazepoxideDEFOBIN, ELENIUMRAPEDURtbl. a drg.10 mg 20 - 60oxazepamOXAZEPAM LIVA tbl. 10 mg10 - 60alprazolamNEUROLXANAXFRONTIN, HELEX tbl. 0.25 mg ; 1 mgtbl. 0.25; 0.5; 1; 2 mg1 - 10bromazepamLEXAURINtbl. 1; 5; 3 mg3 - 36medazepamANSILAN, RUDOTELtbl. 10 mg20 - 40tofisopamGRANDAXINtbl. 50 mg100 - 400K+ clorazepateTRANXENEtbl. 5; 10; 50 mginj. 20; 50; 100 mg15 3050 - 300lorazepamTAVORtbl. 1; 2,5 mg2clobazamFRISIUMtbl. 10 mg20 - 60prazepamDEMETRINtbl. 10 mg20 - 40clonazepamRIVOTRIL
ANTELEPSINtbl. 0.5 ; 2 mggttae 10-25 mg/mlinj. 1 mgtbl. 0.25; 1 mg1 - 4
Anxiolytics
Hypnotics
Generic NameTrade MarkFormMean Doses (mg)1st GenerationbarbiturateschloralhydrateCHLORALOURAT500 1000glutethimideNOXYRONtbl. 250 mg250 - 5002nd GenerationnitrazepamNITRAZEPAM SLOVAKOFARMA FORTEtbl. 5; 10 mg5 - 20flunitrazepamROHYPNOL, SOMNUBENEtbl. 1 a 2 mginj. 2 mg0.5 21 - 2triazolamHALCIONtbl. 0.125 mg0.125 0.5midazolamDORMICUMtbl. 7.5 a 15 mginj. 5 mg7.5 15cinolazepamGERODORMtbl. 40 mg20 403rd GenerationzolpidemSTILNOX, HYPNOGEN, EANOXtbl. 10 mg10 - 20zopicloneIMOVANEtbl. 7.5 mg3.75 7.5zaleptoneSONATAtbl. 10 mg5 10Other Drugs with Hypnotic EfficacyAntihistaminics (promethazine PROTHAZIN)Antidepressants (mirtazapine, trazodone)AntipsychoticsMelatonins
Cognitives
ACETYLCHOLINESTERASE INBITORS rivastigmine EXELON 8 -12 mg donepezil ARICEPT 5 - 10 mg galantamine REMINYL 8 - 24 mg NMDA (N-methyl-D-aspartate) RECEPTOR ANTAGONISTSmemantineEBIXA 10 - 30 mg
Nootropics
Indication: Organic Disturbances of Memory and Intellect, Primary States, Efficacy after 2-3 MonthspyritinolENERBOLENCEPHABOL300 - 900piracetamNOOTROPIL, PYRAMEM, KALICOR3000 - 9000Nootropics and Vasodilators(Improve Rheologic Blood Quality and Cerebral Perfusion)cinarizineSTUGERON50-100vinpocetineCAVINTON15- 30flunarizineSIBELIUM10natridrofurylENELBINDUSODRIL200-300pentoxiphylinexanthinolErgot AlkaloidsdihydroergotoxineSECATOXINnicergoline
Psychostimulants
Generic NameTrade MarkDoses (mg)amphetaminePSYCHOTON, ADDERAL5 50dexamphetamineDEXEDRON5 30ephedrineEPHEDRIN12,5 50mezocarbSYDNOCARB5 50methylphenidateRITALIN10 40modafinilVIGIL200 400
The Na+/K+ ATPase Na+/K+ ATPase is a pump that uses the energy from the hydrolysis of ATP to actively pump sodium and potassium ions against their concentration. The binding of three sodium ions to internal binding sites on the cytoplasmic side of the pump and phosphorylation of the pump induces a conformational change that releases the Na+ ions into the extracellular space. The subsequent binding of two potassium ions to the pump within the synapse followed by dephosphorylation causes it to return to its original confirmation and release the potassium ions into the cytoplasm. This pump is found in almost all cells of the body and the ionic gradient that it creates is used to carry out numerous important cellular processes, such as the transport of other molecules across membrane eg the monoamines.*