psychopharmacology
TRANSCRIPT
PSYCHOPHARMACOLOGY
By: Ahmed Albehairy, M.DTrainer 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 GUIDELINEOptimum 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, TCA, alcohol, MAO
propranolol
Dystonia APD,TCA, DIPHENYL HYDRAMINE, METOCLOPRAMODE
BZD, A CH
Akathesia APD,TCA, levo dopa, reserpine METOCLOPRAMODE
propranolol
Parkinsonism APD,TCA, reserpine, fluxetine, lithium, phenytoin, alcohol withdrawal.
Dec medications., change, A CH.
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, akathesia.biperdin 2- 6 mg, tid
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 LORAZEPAM
1mg bid1mg tid
dystonia, akathesia.
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 EQUAVILANT
HALF LIFE USUAL ADULT 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
CHLORDIAZEPOXIDE
10 INTERMEDIATE 10 – 150 MG TID OE 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 EQUIVALANCY TO 100MG OF CLORPROMAZINE
ADULT DOSEMG
SEDATION EXTRAPYRAMIDAL EFFECT
CHLORPROMAZINE
LOW 100 300-800
HIGH LOW
TRIFLUPERAZINE
HIGH 3.5 6-20 MEDIUM HIGH
FLUPHENAZINE
HIGH 1.5-3 1-20 MEDIUM HIGH
THIORIDAZINE
LOW 100 200-700
HIGH LOW
HALOPERIDOL
HIGH 2.5 6-20 LOW HIGH
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 FLUNOXOLCLOPOXOLHALOPERIDOLPERIDOLIMAPRISPERIDAL GENERIC NAME, DOSE, DURATION
CLOMIPRAMINE
IMIPRAMINE
NORTIPTVLLINE
CITALO
FLUXETINE
FLUVOXAMINE
SERTERALINE
PAROXETINE
TRAZODONE
BUPROPIONE
VENLAFAXINE
MIRTAZAPINE
TIAANEPTIN
NE R I
+++
+++
++++
+ ++ ++ ++ +++
+ + ++ + -
5HT R I
++++
+++
++ ++++
+++
++++
++++
+++++
++ +- +++
+ -
D R I + + + +- + + + + +- ++ + - -
5HT1 BL
+ + ++ +- +- +- +- +- +++
+- +- - -
5HT2 BL
+++
+++
+++
+ ++ + + +- ++++
+- +- ++++
-
ACH BL
+++
+++
++ - + +- +- +- - - - ++ -
H1 BL
+++
+++
+++
++ + - - +- ++ - - +++++
-
A1 BL
+++
+++
+++
+ + + + + +++
- - ++ -
A2 BL
+ + + +- +- + + + ++ +- +- +++
-
D2 BL
++ + + +- + ++ +- +- + - - + -
LITHIUM
MECHANISMINDICATIONSPRECATIONSINTERACTIONSSTOP??????
PSYCHOTROPICS IN PROBLEM AREAS
APD AD ANXIOLYTICS
ANTI CNVALS
EN
OTHERS
HEART PROBLE
M
SULPRIDE,OLANZAPI
NE, QUATIAPIN
E , ZUCLOPEN
TH
MIANSERINE,
MIRTAZEPINE, SSRI,
TRAZODONE
BZD, BUSPAR
BZD, LAMOTRIGI
N, TOPRAMAI
TE, VALPROAT
E
ACOMPROSATE ,
MEMANTINE
LIVER SULPRIDE, PIMOZIDE, ARIPEPRA,
HALDOL
MIANSERINE,
PAROXETINE
LORAZEPAM,
TEMAZEPAM
CARBAMEZ,
TOPRAMAITE
LITHIUM, MEMANTI
NE
RENAL LOXAPINE MIANSERINE, TCA,
TRAZODON
BZD PHENYTOINN
ANTICHOLINEESTR
ASE
DIABETUS
ARIPIPAZ, SULPRIDE, PIMOZIDE, HALDOL
SSRI. TRAZODON
E
BZD, BUSPAR
ACOMPROSATE ,, MODAFIN
IL
PSYCHOTROPICS IN PROBLEM AREAS
APD AD ANXIOLYTICS
ANTI CNVALS
EN
OTHERS
BREAST FEED
SULPRIDE TCA, FLUPENTH
EXOLE
BZD CARBAMEZAPINE,
VALPROATE
EPILEPSY
SULPRIDE, AMISULPRI
DE, HALDOL,
PIMOZIDE, QUATIAPIN
E RISPERIDO
NE
SSRI BZD
GLAUCOMA
HALDOL, RISPERIDO
NE, SULPRIDE
TRAZODONE,
VENLAFAXINE
ACOMPROSATE
, MEMAN
TINELITHIU
M
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.
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