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PSYCHOPHARMACOLOGY



    By: Ahmed Albehairy, M.D
          Trainer in EBP
General Principles of
     Psychopharmacology
-   There is no one-diagnosis-one-drug
    abuse.
-   Drug selection is related not only to
    diagnosis but also to the meaning to
    patient and family influences.
-   Instructions about the treatment benefits
    and risks is a must for the patient ,
    relatives and nursing staff.
Pharmacological Actions
( Pharmacodynamics- Pharmacokinetics )


Pharmacodynamics, include:
- Receptors mechanisms( agonist, antagonist,
   partial agonist, vs. lithium) .
- The dose response curve ( dose response,
  potency, & clinical efficacy).
- Therapeutic index =        median toxic dose 
   median effective dose ( high, SSRI vs. low,
   lithium).
- Tolerance, dependence & withdrawal
  receptors.
Pharmacological Actions
    ( Pharmacodynamics- Pharmacokinetics )
Pharmacokinetics
- Absorption: Oral ( drug concentration, GIT ph, &

  motility). I.M.( DEPOT, 1- WKS). I.V( Fast, high risk of
    S.E).
-   Distribution : High (CBF, lipid solubility, & receptor
    affinity). Vary with age, sex, AT.
- Metabolism : metabolic routes( oxidation,
  reduction, hydrolysis, & conjugation). Active and
  inactive metabolites. End by liver in feces,
  sweat , saliva, etc. Half life . Clearance.
- Cytochrome P450 enzymes.
Pharmacological Actions
        ( Pharmacodynamics- Pharmacokinetics )
  Pharmacokinetics, - Cytochrome P450 enzymes.
- ?
- Rapid vs. poor metabolizers.
- Cyt P 450 Polymorphisms.
- 1A2, 2C19, 2C9, 2D6 , 3A3, 4, 5, 7.
- Tables ( substrates, inhibitors, & inducers).
- Inhibitors e.g.
   1A2 Fluvoxamine ------ clomipramine, clozapine, haloperidol.
   2C19 Fluxetine, paroxetine -----citalopram, diazepam, propranlol,
    imipramine.
-   Inducers e.g.
     2C19 Carbamezapine ------- citalopram, diazepam, propranlol,
    imipramine.
     3A3 Carbamezapine ------- carbamezapine, clozapine , TCA,
    trazodone, verapamil.
CLINICAL GUIDELINE
Optimum Results = 5 Ds.
- Diagnosis: reinvestigate.

- Drug selection : diagnosis, drug history,

  tolerable S.E, lethal dose, & abuse
  potential.
- Dose : low – slow ., effectiveness vs. S.E.

- Duration : 3 – 6 wks, long term

  administration.
- Dialogue: Drug information.
Special Considerations

- Children : high metabolism, low – slow, /kg.
- Geriatric : low metabolism , 1/3 adult dose,

  drug interaction and medical state.
- Pregnancy & lactation: avoid drugs esp. in

  1st trimester, avoid absolutely ( lithium ,
  anticonvulsant in pregnancy) . ECT is good.
- Hepatic and renal problems: half the
  dose.
TREATMENT OF COMMON S.E
-   Sexual dysfunction : bupopione , Viagra, reassurance,
    yohimbex, amantadine, cryptoheptadine.
-   Anxiety in SSRI.
-   Insomnia of SSRI.
-   GIT upset.
-   headache.
-   Wt gain .
-   somnolence.
-   Dry mouth.
-   Blurred vision.
-   Orthostatic hypotension.
-   Urinary retention , constipation.
MEDICATION – INDUCED MOVEMENT DISORDERS

Movement disorder         Drug responsible              Treatment

Tremor                    APD, sympathomimetics,        propranolol
                          TCA, alcohol, MAO

Dystonia                  APD,TCA, DIPHENYL             BZD, A CH
                          HYDRAMINE,
                          METOCLOPRAMODE
Akathesia                 APD,TCA, levo dopa,           propranolol
                          reserpine
                          METOCLOPRAMODE
Parkinsonism              APD,TCA, reserpine,            Dec medications., change, A
                          fluxetine, lithium, phenytoin, CH.
                          alcohol withdrawal.

TARDIVE DYSKINESIA        APD, > 4 Y, age, female       ????


Neuroleptic M. syndrome   APD                           Dantrium, fluid,
                                                        bromocriptine,
DRUG TREATMENT OF
      EXTRAPYRAMIDAL DISORDERS

Drug name         Usual daily dose       indications

benztropine       1-4 mg , twice per day Acute dystonia,
                                         parkinsonism,
biperdin          2- 6 mg, tid           akathesia.
procyclidine      2.5 – 5 mg 2-4 /d
Dipheny hydramine 25 mg QID              Acute dystonia,
                                         parkinsonism, rabbit
                                         syndrome.
Amantadine        100 – 300 mg           parkinsonism, rabbit
                                         syndrome.

CLONAZEPAM        1mg bid                dystonia, akathesia.
LORAZEPAM         1mg tid
Classification of
Psychotherapeutic Drugs

-   Antipsychotic drugs.
-   Antidepressant .
-   Anti manic or mood stabilizers.
-   Anti anxiety , anxiolytic drugs.
-   Others ( geriatric , child , addiction , general
    medications).

    ??????? Less valid categories
PREPRATIONS OF BZD RECEPTORS AGONIST AND ANTAGONIST

DRUG          DOSE         HALF LIFE      USUAL ADULT
              EQUAVILANT                  DOSE
CLONAZEPAM    0.5          LONG           1-6 MG /D BID

DIAZEPAM      5            LONG           4-40MG /D BID - QID

ALPRAZOLAM    0.25         INTERMEDIATE   0.5-10MG/DBID TO
                                          QID

LORAZEPAM     1            INTERMEDIATE   1-6 MG /D TID

CHLORDIAZEPO 10            INTERMEDIATE   10 – 150 MG TID OE
XIDE                                      QID

FLURAZEPAM    5            SHORT          15-30 MG

CLORAZEOATE   7.5MG        SHORT          15 – 60 MG BID OR
                                          QID

MIDAZOLAM     1.25- 1.7    SHORT          5 – 50 MG
                                          PARENTRAL

FLUMEZANIL    0.05         SHORT          0.2- 0.5 MG
                                          /MININJECTION
                                          OVER 3- 10 MIN
TYPICAL ANTIPSYCHOTICS
DRUG       POTENCY   EQUIVALA   ADULT     SEDATION   EXTRAPYRAMIDAL
                     NCY TO     DOSE                 EFFECT
                     100MG OF   MG
                     CLORPRO
                     MAZINE

CHLORPR    LOW       100        300-800   HIGH       LOW
OMAZINE

TRIFLUPE   HIGH      3.5        6-20      MEDIUM     HIGH
RAZINE

FLUPHENA   HIGH      1.5-3      1-20      MEDIUM     HIGH
ZINE

THIORIDA   LOW       100        200-700   HIGH       LOW
ZINE

HALOPERI   HIGH      2.5        6-20      LOW        HIGH
DOL

PIMOZIDE   HIGH      1          1-10      LOW        HIGH
ATYPICAL ANTIPSYCHOTICS

- NAME .
- ?????

- CLOZAPINE - RISPERIDONE-

  OLANZAPINE – QUITIAPINE –
  ZIPRASIDONE – ARIPIPRAZOLE.
- DOSE.

- PRCAUTIONS ( MEDICAL STATE OF THE
  PATIENT , S.E, DRUG INTERACTIONS).
DEPOT FORMS??
MODECATE
FLUNOXOL
CLOPOXOL
HALOPERIDOL
PERIDOL
IMAP
RISPERIDAL
  GENERIC NAME, DOSE, DURATION
CLO   IMI   NOR    CITA   FLU    FLU   SER    PAR    TRA   BUP   VEN   MIR   TIAA
       MIP   PRA   TIPT   LO     XETI   VOX   TER    OXE    ZOD   ROP   LAF   TAZ   NEP
       RAM   MIN   VLLI          NE     AMI   ALIN   TINE   ONE   ION   AXI   API   TIN
       INE   E     NE                   NE    E                   E     NE    NE
NE R   +++ +++ +++         +     ++     ++    ++     +++     +     +    ++     +     -
I               +
5HT    +++ +++     ++     +++ +++ +++ +++ +++               ++    +-    +++    +     -
RI      +                  +       +   +   ++
DRI     +     +     +      +-     +      +     +      +     +-    ++     +     -     -
5HT1    +     +    ++      +-     +-    +-     +-     +-    +++   +-    +-     -     -
BL
5HT2   +++ +++ +++         +     ++      +     +      +-    +++   +-    +-    +++    -
BL                                                           +                 +
ACH    +++ +++     ++      -      +     +-     +-     +-     -     -     -    ++     -
BL
H1     +++ +++ +++        ++      +      -     -      +-    ++     -     -    +++    -
BL                                                                             ++
A1     +++ +++ +++         +      +      +     +      +     +++    -     -    ++     -
BL
A2      +     +     +      +-     +-     +     +      +     ++    +-    +-    +++    -
BL
D2     ++     +     +      +-     +     ++     +-     +-     +     -     -     +     -
BL
LITHIUM

MECHANISM
INDICATIONS
PRECATIONS
INTERACTIONS
STOP??????
PSYCHOTROPICS IN PROBLEM AREAS
            APD          AD        ANXIOLY      ANTI       OTHERS
                                     TICS      CNVALSE
                                                  N
 HEART  SULPRIDE,O MIANSERIN         BZD,         BZD,     ACOMPRO
PROBLEM LANZAPINE,     E,           BUSPAR     LAMOTRIGI    SATE ,
          QUATIAPIN   MIRTAZEPI                    N,      MEMANTI
              E,       NE, SSRI,               TOPRAMAIT      NE
          ZUCLOPENT   TRAZODONE                    E,
              H                                VALPROATE

 LIVER    SULPRIDE,   MIANSERIN    LORAZEPAM   CARBAMEZ,   LITHIUM,
          PIMOZIDE,       E,           ,       TOPRAMAIT   MEMANTI
          ARIPEPRA,   PAROXETIN    TEMAZEPAM       E          NE
           HALDOL         E

 RENAL    LOXAPINE    MIANSERIN       BZD      PHENYTOIN   ANTICHOL
                        E, TCA,                    N       INEESTRA
                      TRAZODON                                SE

DIABETU   ARIPIPAZ,      SSRI.       BZD,                  ACOMPRO
          SULPRIDE,   TRAZODONE     BUSPAR                  SATE ,,
   S
          PIMOZIDE,                                        MODAFINI
           HALDOL                                             L
PSYCHOTROPICS IN PROBLEM AREAS
             APD          AD       ANXIOLY    ANTI       OTHER
                                     TICS    CNVALSE       S
                                                N
BREAST     SULPRIDE       TCA,       BZD     CARBAMEZ
                       FLUPENTHE               APINE,
 FEED
                          XOLE               VALPROATE

EPILEPSY   SULPRIDE,     SSRI        BZD
           AMISULPRI
              DE,
            HALDOL,
           PIMOZIDE,
           QUATIAPIN
               E
           RISPERIDO
               NE
GLAUCO      HALDOL,    TRAZODON                          ACOMPR
           RISPERIDO       E,                             OSATE ,
  MA
              NE,      VENLAFAXI                         MEMANT
           SULPRIDE       NE                               INE
                                                         LITHIUM
AVOID THE FOLLOWINGS

  BREAST FEEDING: ARIPRPRAZOLE, CLOZAPINE, OLANZAPINE,
  RISPERIDONE, MAAOI, VENLAFAXINE, BUSPIRONE, OTHER
  ANTIEPILEPTICS.

 HEAR PROBLEM , CLOZAPINE, PIMOZIDE, THIORIDAZINR, ZIPRASIDONE,
  TCA, VENLAFAXINE, DISULFRAM , .
 DIABETUS: OLANZAPINE, MAOI.

 EPILEPSY, CHLORPROMAZINE, CLOZAPINE, BUPROPION
 GLAUCOMA: OLANZAPINE, TCA.

 LIVER PROBLEM: ZOTEPINE, MAOI, BZD, VALPROATE,
PHENYTOIN, BARBITURATE.

 RENAL PROBLEMS:AMISULPRIDE, RISPERIDONE, SULPRIDE, FLUXETINE,
  VENLAFAXINE, BUSPIRONE, AVOID ANTI CONVULSANT OTHER THAN
  PHENYTOIN.
‫شكرا علي حسن‬

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Psychopharmacology

  • 1. PSYCHOPHARMACOLOGY By: Ahmed Albehairy, M.D Trainer in EBP
  • 2. General Principles of Psychopharmacology - There is no one-diagnosis-one-drug abuse. - Drug selection is related not only to diagnosis but also to the meaning to patient and family influences. - Instructions about the treatment benefits and risks is a must for the patient , relatives and nursing staff.
  • 3. Pharmacological Actions ( Pharmacodynamics- Pharmacokinetics ) Pharmacodynamics, include: - Receptors mechanisms( agonist, antagonist, partial agonist, vs. lithium) . - The dose response curve ( dose response, potency, & clinical efficacy). - Therapeutic index = median toxic dose median effective dose ( high, SSRI vs. low, lithium). - Tolerance, dependence & withdrawal receptors.
  • 4. Pharmacological Actions ( Pharmacodynamics- Pharmacokinetics ) Pharmacokinetics - Absorption: Oral ( drug concentration, GIT ph, & motility). I.M.( DEPOT, 1- WKS). I.V( Fast, high risk of S.E). - Distribution : High (CBF, lipid solubility, & receptor affinity). Vary with age, sex, AT. - Metabolism : metabolic routes( oxidation, reduction, hydrolysis, & conjugation). Active and inactive metabolites. End by liver in feces, sweat , saliva, etc. Half life . Clearance. - Cytochrome P450 enzymes.
  • 5. Pharmacological Actions ( Pharmacodynamics- Pharmacokinetics ) Pharmacokinetics, - Cytochrome P450 enzymes. - ? - Rapid vs. poor metabolizers. - Cyt P 450 Polymorphisms. - 1A2, 2C19, 2C9, 2D6 , 3A3, 4, 5, 7. - Tables ( substrates, inhibitors, & inducers). - Inhibitors e.g. 1A2 Fluvoxamine ------ clomipramine, clozapine, haloperidol. 2C19 Fluxetine, paroxetine -----citalopram, diazepam, propranlol, imipramine. - Inducers e.g. 2C19 Carbamezapine ------- citalopram, diazepam, propranlol, imipramine. 3A3 Carbamezapine ------- carbamezapine, clozapine , TCA, trazodone, verapamil.
  • 6. CLINICAL GUIDELINE Optimum Results = 5 Ds. - Diagnosis: reinvestigate. - Drug selection : diagnosis, drug history, tolerable S.E, lethal dose, & abuse potential. - Dose : low – slow ., effectiveness vs. S.E. - Duration : 3 – 6 wks, long term administration. - Dialogue: Drug information.
  • 7. Special Considerations - Children : high metabolism, low – slow, /kg. - Geriatric : low metabolism , 1/3 adult dose, drug interaction and medical state. - Pregnancy & lactation: avoid drugs esp. in 1st trimester, avoid absolutely ( lithium , anticonvulsant in pregnancy) . ECT is good. - Hepatic and renal problems: half the dose.
  • 8. TREATMENT OF COMMON S.E - Sexual dysfunction : bupopione , Viagra, reassurance, yohimbex, amantadine, cryptoheptadine. - Anxiety in SSRI. - Insomnia of SSRI. - GIT upset. - headache. - Wt gain . - somnolence. - Dry mouth. - Blurred vision. - Orthostatic hypotension. - Urinary retention , constipation.
  • 9. MEDICATION – INDUCED MOVEMENT DISORDERS Movement disorder Drug responsible Treatment Tremor APD, sympathomimetics, propranolol TCA, alcohol, MAO Dystonia APD,TCA, DIPHENYL BZD, A CH HYDRAMINE, METOCLOPRAMODE Akathesia APD,TCA, levo dopa, propranolol reserpine METOCLOPRAMODE Parkinsonism APD,TCA, reserpine, Dec medications., change, A fluxetine, lithium, phenytoin, CH. alcohol withdrawal. TARDIVE DYSKINESIA APD, > 4 Y, age, female ???? Neuroleptic M. syndrome APD Dantrium, fluid, bromocriptine,
  • 10. DRUG TREATMENT OF EXTRAPYRAMIDAL DISORDERS Drug name Usual daily dose indications benztropine 1-4 mg , twice per day Acute dystonia, parkinsonism, biperdin 2- 6 mg, tid akathesia. procyclidine 2.5 – 5 mg 2-4 /d Dipheny hydramine 25 mg QID Acute dystonia, parkinsonism, rabbit syndrome. Amantadine 100 – 300 mg parkinsonism, rabbit syndrome. CLONAZEPAM 1mg bid dystonia, akathesia. LORAZEPAM 1mg tid
  • 11. Classification of Psychotherapeutic Drugs - Antipsychotic drugs. - Antidepressant . - Anti manic or mood stabilizers. - Anti anxiety , anxiolytic drugs. - Others ( geriatric , child , addiction , general medications). ??????? Less valid categories
  • 12. PREPRATIONS OF BZD RECEPTORS AGONIST AND ANTAGONIST DRUG DOSE HALF LIFE USUAL ADULT EQUAVILANT DOSE CLONAZEPAM 0.5 LONG 1-6 MG /D BID DIAZEPAM 5 LONG 4-40MG /D BID - QID ALPRAZOLAM 0.25 INTERMEDIATE 0.5-10MG/DBID TO QID LORAZEPAM 1 INTERMEDIATE 1-6 MG /D TID CHLORDIAZEPO 10 INTERMEDIATE 10 – 150 MG TID OE XIDE QID FLURAZEPAM 5 SHORT 15-30 MG CLORAZEOATE 7.5MG SHORT 15 – 60 MG BID OR QID MIDAZOLAM 1.25- 1.7 SHORT 5 – 50 MG PARENTRAL FLUMEZANIL 0.05 SHORT 0.2- 0.5 MG /MININJECTION OVER 3- 10 MIN
  • 13. TYPICAL ANTIPSYCHOTICS DRUG POTENCY EQUIVALA ADULT SEDATION EXTRAPYRAMIDAL NCY TO DOSE EFFECT 100MG OF MG CLORPRO MAZINE CHLORPR LOW 100 300-800 HIGH LOW OMAZINE TRIFLUPE HIGH 3.5 6-20 MEDIUM HIGH RAZINE FLUPHENA HIGH 1.5-3 1-20 MEDIUM HIGH ZINE THIORIDA LOW 100 200-700 HIGH LOW ZINE HALOPERI HIGH 2.5 6-20 LOW HIGH DOL PIMOZIDE HIGH 1 1-10 LOW HIGH
  • 14. ATYPICAL ANTIPSYCHOTICS - NAME . - ????? - CLOZAPINE - RISPERIDONE- OLANZAPINE – QUITIAPINE – ZIPRASIDONE – ARIPIPRAZOLE. - DOSE. - PRCAUTIONS ( MEDICAL STATE OF THE PATIENT , S.E, DRUG INTERACTIONS).
  • 16. CLO IMI NOR CITA FLU FLU SER PAR TRA BUP VEN MIR TIAA MIP PRA TIPT LO XETI VOX TER OXE ZOD ROP LAF TAZ NEP RAM MIN VLLI NE AMI ALIN TINE ONE ION AXI API TIN INE E NE NE E E NE NE NE R +++ +++ +++ + ++ ++ ++ +++ + + ++ + - I + 5HT +++ +++ ++ +++ +++ +++ +++ +++ ++ +- +++ + - RI + + + + ++ DRI + + + +- + + + + +- ++ + - - 5HT1 + + ++ +- +- +- +- +- +++ +- +- - - BL 5HT2 +++ +++ +++ + ++ + + +- +++ +- +- +++ - BL + + ACH +++ +++ ++ - + +- +- +- - - - ++ - BL H1 +++ +++ +++ ++ + - - +- ++ - - +++ - BL ++ A1 +++ +++ +++ + + + + + +++ - - ++ - BL A2 + + + +- +- + + + ++ +- +- +++ - BL D2 ++ + + +- + ++ +- +- + - - + - BL
  • 18. PSYCHOTROPICS IN PROBLEM AREAS APD AD ANXIOLY ANTI OTHERS TICS CNVALSE N HEART SULPRIDE,O MIANSERIN BZD, BZD, ACOMPRO PROBLEM LANZAPINE, E, BUSPAR LAMOTRIGI SATE , QUATIAPIN MIRTAZEPI N, MEMANTI E, NE, SSRI, TOPRAMAIT NE ZUCLOPENT TRAZODONE E, H VALPROATE LIVER SULPRIDE, MIANSERIN LORAZEPAM CARBAMEZ, LITHIUM, PIMOZIDE, E, , TOPRAMAIT MEMANTI ARIPEPRA, PAROXETIN TEMAZEPAM E NE HALDOL E RENAL LOXAPINE MIANSERIN BZD PHENYTOIN ANTICHOL E, TCA, N INEESTRA TRAZODON SE DIABETU ARIPIPAZ, SSRI. BZD, ACOMPRO SULPRIDE, TRAZODONE BUSPAR SATE ,, S PIMOZIDE, MODAFINI HALDOL L
  • 19. PSYCHOTROPICS IN PROBLEM AREAS APD AD ANXIOLY ANTI OTHER TICS CNVALSE S N BREAST SULPRIDE TCA, BZD CARBAMEZ FLUPENTHE APINE, FEED XOLE VALPROATE EPILEPSY SULPRIDE, SSRI BZD AMISULPRI DE, HALDOL, PIMOZIDE, QUATIAPIN E RISPERIDO NE GLAUCO HALDOL, TRAZODON ACOMPR RISPERIDO E, OSATE , MA NE, VENLAFAXI MEMANT SULPRIDE NE INE LITHIUM
  • 20. AVOID THE FOLLOWINGS BREAST FEEDING: ARIPRPRAZOLE, CLOZAPINE, OLANZAPINE, RISPERIDONE, MAAOI, VENLAFAXINE, BUSPIRONE, OTHER ANTIEPILEPTICS. HEAR PROBLEM , CLOZAPINE, PIMOZIDE, THIORIDAZINR, ZIPRASIDONE, TCA, VENLAFAXINE, DISULFRAM , . DIABETUS: OLANZAPINE, MAOI. EPILEPSY, CHLORPROMAZINE, CLOZAPINE, BUPROPION GLAUCOMA: OLANZAPINE, TCA. LIVER PROBLEM: ZOTEPINE, MAOI, BZD, VALPROATE, PHENYTOIN, BARBITURATE. RENAL PROBLEMS:AMISULPRIDE, RISPERIDONE, SULPRIDE, FLUXETINE, VENLAFAXINE, BUSPIRONE, AVOID ANTI CONVULSANT OTHER THAN PHENYTOIN.