Psychopharmacology-1

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Unformatted text preview: Psychopharmacology Psychopharmacology Department of Psychiatry 1st Faculty of Medicine Charles University, Prague Head: Prof. MUDr. Jiří Raboch, DrSc. Main Psychopharmacological Drugs Drugs Antipsychotics Antidepresants Anxiolytics Hypnotics Cognitives Psychostimulants Overview of Antipsychotics Overview Chem. Group Conventional Antipsychotics Generic Name Trade Mark Dose (mg) CHLORPROMAZIN, LARGACTIL, PLEGOMAZIN, MEGAPHEN, THORAZIN TISERCIN, NOZINAN 200­800 thioridazine THIORIDAZIN, MELLERIL 100­600 periciazine NEULEPTIL chlorprothixene CHLORPROTHIXEN, TRUXAL clopenthixol CISORDINOL, CLOPIXOL chlorpromazine Phenothiazines Thioxanthes levomepromazine 50­400 10­40 100­600 20­100 Overview of Antipsychotics Overview Chem. Group Conventional Antipsychotics Generic Name Trade Mark Dose (mg) 16­24 flufenazine PERFENAZIN, TRILAFON, PERATSIN PROCHLORPERAZIN, STEMETIL MODITEN trifluoperazine STELAZIN 10­50 flupenthixol FLUANXOL 6­18 haloperidol melperone HALOPERIDOL, HALDOL, APO­HALOPERIDOL BURONIL pimozide ORAP 2­10 fluspirilen IMAP 2­10 penfluridol SEMAP 2­60 oxyprothepin MECLOPIN 5­20 perfenazine Phenothiazines Thioxanthenes Butyrophenones Diphenylbutyl piperidines Perathiepines prochlorperazine 20­80 2­16 2,5­10 50­300 Antipsychotics Antipsychotics of the 2nd Generation Generic Name Trade Mark Dose (mg) D2, D3 selective antagonists sulpiride DOGMATIL, PROSULPIN 50­1200 amisulpride SOLIAN, DENIBAN 50­1200 SDA risperidone 4­8 ziprasidone RISPERDAL, RISPEN, RISPERDAL QUICKLET ZELDOX sertindole SERDOLECT 12­20 40­160 MARTA clozapine LEPONEX 200­600 olanzapine ZYPREXA i.m. inj. 10 mg 5­20 quetiapine SEROQUEL 300­600 zotepine ZOLEPTIL 75­300 Antipsychotics Antipsychotics of the 2nd Generation Efficacy 1. Positive symptoms are influenced significantly better than placebo, and equally or more then by the classical antidopaminergic 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 least equally as by clozapine. 6. Maintenance treatment is more effective than maintenance on placebo and at least as effective as maintenance on classical neuroleptics. Antipsychotics of the 3rd Antipsychotics generation generation Generic Name název aripiprazol Trade Mark Dose (mg) Mechanism of Efficacy Dopamine­serotonin stabiliser ABILIFY 15­30 Parcial agonist of D2 and 5­HT1A receptors Antagonist of 5­HT2A receptors Depot Antipsychotics Generic Name Generic Name Trade Mark Mean Dose (mg) flufenazin MODITEN DEPOT oxyprothepin MECLOPIN 25 haloperidol HALDOL DEPOT 100 flupenthixol FLUANXOL DEPOT 40 zuclopenthixol CISORDINOL DEPOT 200 fluspirilen IMAP risperidone RISPERDAL CONSTA Interval 25 14­28 days 6 7 days !! 20­30 14 days Rapid Tranquilizers pro dosi (mg) pro dosi (mg) pro die (mg) chlorpromazin 100­200 800­1200 levopromazin 50­100 500­600 (TISERCIN) haloperidol 5­10 40­100 chlorprothixen 100­150 500­600 zuclopenthixol 50­150 (24­72 hours) (CISORDINOL ACUTARD) tiapride 600­1200 Indication of Antidepressants Indication Depressive Disturbances Affective Disorders Obsessive­Compulsive Disorders Panic Disorders Eating Disorders Psychosomatic Disorders Posttraumatic Stress Disorder Alcohol and Drugs Withdrawal Symptoms Pain Syndromes Enuresis Narcolepsy Neurotransmitter Reuptake Inhibition and Binding Affinity to Receptors and Receptors: SE Serotonergic NE Noradrenergic M Muscarinic H Histaminic α­N alpha noradrenergic Antidepressants: Antidepressant Monoamine Reuptake Inhibitors 1st Generation of Antidepressants (TCA, TeCA) Generic Name Trade Mark Doses (mg) amitriptyline AMITRIPTYLIN 75­200 nortriptyline NORTRILEN 50­150 imipramine MELIPRAMIN 75­250 clomipramine 75­225 dosulepin ANAFRANIL, HYDIPHEN PROTHIADEN 100­300 dibenzepine NOVERIL 240­720 maprotiline LUDIOMIL, MAPROTILINE 75­150 Mechanism of Efficacy Inhibition of Serotonin and/or Norepinephrine Reuptake Followed by Increase of their Concentrations in Synaptic Cleft 1st Generation of Antidepressants Mechanism of action: Blockade of muscarine receptors Histamine H1 receptors Alpha 1 Adrenergic Receptors Alpha 2 Adrenergic Receptors Many Side Effects Danger of Intoxication Many Interactions Prolonged Effect (after 3­6 Weeks) 2nd Generation of Antidepressants 2nd Generation of Antidepressants Generic Name viloxazine Trade Mark VIVALAN Mean Doses (mg) 100­300 Mechanism Norepinephrine Reuptake Inhibition 3rd Generation of Antidepressants Generic Name Trade Mark Mean Doses (mg) Mechanism SSRI fluvoxamine FEVARIN fluoxetine DEPREX, DEPRENON, PROZAC, PORTAL, FLOXET, FLUXONIL, MAGRILAN SEROPRAM, CITALEC, CEROTER, PRAM CIPRALEX 20­60 SEROXAT, PAROLEX, APO­PAROX, REMOD ZOLOFT, SERLIFT, ASENTRA, STIMULOTON 20­60 citalopram escitalopram paroxetine sertraline 100­300 20­60 10­20 50­200 Selective Serotonin Reuptake Inhibition 3rd Generation of Antidepressants Generic Name Trade Mark Mean Doses (mg) Mechanism SARI Antidepressants with Doubled Serotonergic Efficacy TRITTICO AC 4­8 trazodone Double Serotonergic SERZONE, 100­300 nefazodone Efficacy DUTONIN NARI reboxetine EDRONAX 4­8 Norepinephrine Reuptake Inhibition tianeptine COAXIL 75 Increasing of Serotonin Reuptake 4th Generation of Antidepressants Dual acting antidepressants Mixed reuptake inhibitors Generic Name Trade Mark Mean Doses (mg) Mechanism SNRI venlafaxine EFECTIN 75­375 venlafaxine ER (extended EFECTIN ER 75­225 IXEL, DALCIPRAN 50­100 relesase) milnaciprane Serotonin and Norepinephrine Reuptake Inhibition DNRI bupropione WELLBUTRIN ZYBAN 150­300 Dopamine and Norepinephrine Reuptake Inhibition 4th Generation of Antidepressants Generic Name Trade Mark Mean Doses (mg) Mechanism Blockade of α 2­adrenoceptors mianserin mirtazapine hypericum perforatum LERIVON, MIABENE 60­90 Increasing Synthesis and Releasing of Norepinephrine, Blockade Alpha­2 Adrenoceptors on Serotonergic Neurons and Increasing Production and Releasing of Serotonin REMERON, 15­45 ESPRITAL, REMERON sol. tab. Other Monoamine Reuptake Inhibitors JARSIN 900 Weak Inhibitor of NA, 5­ HT, DA MAO Inhibitors Non Selective and Irreversible: (IMAO A, IMAO B) Non Selective and Irreversible: (IMAO A, IMAO B) phenelzine NARDIL isocarboxazid MARPLAN nialamide NIAMID, NUREDAL tranylcypromine PARNATE Selective and Reversible moclobemide MAO B brofaromine CONSONAR toloxatone MAO A AURORIX HUMORYL selegiline (L­deprenyl) SEPATREM, JUMEX Other Psychotropics with Antidepressant Effect Antidepressant Thymoprophylactics lithium Antiepileptics of 2nd Generation Antiepileptics of 3rd Generation LITHIUM CARBONICUM, CONTEMNOL carbamazepine salts of valproic acid lamotrigine BISTON, TEGRETOL, FINLEPSIN, TIMONIL EVERIDEN, CONVULEX, ORFIRIL, DEPAMID LAMICTAL gabapentine GABAPENTIN, NEURONTIN topiramate TOPAMAX Atypical Antipsychotics ­ SDA clozapine LEPONEX, CLOZARIL, ALEMOXAN olanzapine ZYPREXA quetiapine SEROQUEL Thymoprophylactics Thymoprophylactics Generic Name Trade Mark Doses (mg) Blood Serum Concentration LITHIUM CARBONICUM 900 – 1000 0.5 – 0.8 mmol/l CONTEMNOL 1000 ­ 1500 0.8 – 1.2 mmol/l carbamazepine BISTON, TEGRETOL, TIMONIL 400 ­ 1500 5 – 10 ng/ml valproic acid EVERIDEN, ORFIRIL, 900 ­ 2000 50 ­ 100 ng/ml lithium carbonicum Action Profiles of Benzodiazepines Action Relief of anxiety Anticonvulsant action Sedation 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, 108­114 (1984). (Except <Dormicum> and <Dalmadorm>) Benzodiazepine Anxiolytics Benzodiazepine Indication: States of Anxiety Sleeplessness Withdrawal Symptoms Depressive States Epilepsy Convulsions Tetanus Neonatorum Extrapyramidal Undesirable Side Effects of Antipsychotics Premedication in Anaestesiology Panic States (Alprazolam, Bromazepam, Clonazepam in High Doses) Algidic Syndromes (Stomatodynie, Neuralgie Trigemini, Cephalgia) Anxiolytics Anxiolytics Generic Name Trade Mark Form Mean Doses (mg) Propandiol Derivates guaiphenesine GUAJACURAN DORSIFLEX, DIMEXOL MEPROBAMAT meprobamate LÉČIVA Piperazin Derivates Mephenoxalone hydroxyzine ATARAX Azapiron Derivates ANXIRON, buspirone BUSPIRON­EGIS drg. 200,400mg inj. 1 g tbl. 200 mg 400 ­ 3000 tbl. 400 mg 800 ­ 2400 tbl. 10, 25 mg inj. 100 mg sir. 20 – 100 300 ­ 400 tbl. 5, 10 mg 15­30 400 ­ 1200 Anxiolytics (Benzodiazepine Derivates) (Benzodiazepine Generic Name Trade Mark Form Mean Doses (mg) 10 ­ 60 DIAZEPAM SLOVAKOFARMA APO­DIAZEPAM APAURIN, SEDUXEN DIAZEPAM DESITIN DIAZEPAM DESITIN SUPP. DEFOBIN, ELENIUM RAPEDUR OXAZEPAM LÉČIVA tbl. 2.5; 10 mg inj. 10 mg tbl. 0.25 mg ; 1 mg tbl. 0.25; 0.5; 1; 2 mg 1 ­ 10 bromazepam NEUROL XANAX FRONTIN, HELEX 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 lorazepam TAVOR tbl. 5; 10; 50 mg inj. 20; 50; 100 mg tbl. 1; 2,5 mg 15 – 30 50 ­ 300 2 clobazam FRISIUM tbl. 10 mg 20 ­ 60 prazepam DEMETRIN tbl. 10 mg 20 ­ 40 clonazepam RIVOTRIL tbl. 0.5 ; 2 mg gttae 10­25 mg/ml inj. 1 mg diazepam chlordiazepoxide oxazepam alprazolam supp. 5 mg tbl. a drg. 10 mg tbl. 10 mg 20 ­ 60 10 ­ 60 1 ­ 4 Anxiolytics Anxiolytics 60 60 60 Anxiolytic (eventually Antidepressive) Effect Inhibition 50 40 32 32 30 24 20 20 10 8 6 6 3 0 diazepam alprazolam bromazepam clonazepam clobazam Hypnotics Hypnotics Generic Name 1st Generation 2nd Generation barbiturates chloralhydrate glutethimide nitrazepam flunitrazepam triazolam midazolam cinolazepam zolpidem Trade Mark CHLORALOURAT NOXYRON NITRAZEPAM SLOVAKOFARMA FORTE ROHYPNOL, SOMNUBENE HALCION DORMICUM Form tbl. 250 mg tbl. 5; 10 mg tbl. 1 a 2 mg inj. 2 mg tbl. 0.125 mg tbl. 7.5 a 15 mg inj. 5 mg tbl. 40 mg tbl. 10 mg GERODORM 3rd Generation STILNOX, HYPNOGEN, EANOX zopiclone IMOVANE tbl. 7.5 mg zaleptone SONATA tbl. 10 mg Other Drugs with Antihistaminics (promethazine – PROTHAZIN) Hypnotic Antidepressants (mirtazapine, trazodone) Efficacy Antipsychotics Melatonins Mean Doses (mg) 500 – 1000 250 ­ 500 5 ­ 20 0.5 – 2 1 ­ 2 0.125 – 0.5 7.5 – 15 20 – 40 10 ­ 20 3.75 – 7.5 5 – 10 Cognitives Cognitives ACETYLCHOLINESTERASE INBITORS rivastigmine EXELON 8 ­12 mg donepezil ARICEPT 5 ­ 10 mg galantamine REMINYL 8 ­ 24 mg NMDA (N­methyl­D­aspartate) RECEPTOR ANTAGONISTS memantine EBIXA 10 ­ 30 mg Nootropics Nootropics Indication: Organic Disturbances of Memory and Intellect, Primary States, Efficacy after 2­3 Months pyritinol ENERBOL 300 ­ 900 ENCEPHABOL piracetam NOOTROPIL, 3000 ­ 9000 PYRAMEM, KALICOR Nootropics and Vasodilators (Improve Rheologic Blood Quality and Cerebral Perfusion) cinarizine STUGERON 50­100 vinpocetine CAVINTON 15­ 30 flunarizine SIBELIUM 10 natridrofuryl ENELBIN DUSODRIL 200­300 pentoxiphyline xanthinol dihydroergotoxine nicergoline Ergot Alkaloids SECATOXIN Psychostimulants Psychostimulants Generic Name amphetamine Trade Mark Doses (mg) 5 – 50 dexamphetamine PSYCHOTON, ADDERAL DEXEDRON ephedrine EPHEDRIN 12,5 – 50 mezocarb SYDNOCARB 5 – 50 methylphenidate RITALIN, 10 – 40 CENTEDRIN VIGIL, PROVIGIL 200 – 400 modafinil 5 – 30 ...
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This note was uploaded on 12/24/2011 for the course STEP 1 taught by Professor Dr.aslam during the Fall '11 term at Montgomery College.

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