DOPAMINE RECEPTOR

ANTAGONISTS
TYPICAL ANTIPSYCHOTICS
DRA’S
GOOD ORAL ABSORPTION
PEAK PLASMA CONC. AFTER 1 TO 4 HRS
STEADY STATE LEVEL IN 3 TO 5 DAYS
DRA’S EFFECTIVE WHEN 60% D2 RECEPTORS
ARE BLOCKED AT 80% EPS
DEPOT PREPARATIONS- 6 MONTHS TO STEADY
STATE
DRA’S INDICATION
DRUG CLASS EQUIVALE SEDAT AUTONOMIC EPS
NAME NT
ION

FLUPHENAZI PHENOTHIA 2MG + + +++

ZINE
NE

HALOPERIDO BUTYROPH 2 MG + + +++

ENONE
L

CHLORPROM PHENOTHIA 100MG +++ +++ ++

ZINE
AZINE
PRECAUTIONS AND ADVERSE
REACTIONS
 LOWER SEIZURE THRESHOLD
 SEDATION- BLOCK H1 RECEPTORS
 CENTRAL ANTICHOLINERGIC EFFECT-
AGITATION,DISORIENTATION,HALLUCINATION
 CARDIAC EFFECTS-
ARRYHTMIA,DEC.CONTRACTILITY
 ORTHOSTATIC HYPOTENSION
PRECAUTIONS AND ADVERSE
REACTIONS

 HEMATOLOGIC
 PERIPHERAL ANTICHOLINERGIC
EFFECTSINCREASED PROLACTIN
 SEXUAL ADVERSE EFFECTS
 ALLERGIC DERMATITIS
 RETINAL PIGMENTATION
 JAUNDICE
SEROTONIN DOPAMINE
ANTAGONISTS
ATYPICAL ANTIPSYCHOTICS
 SDA
 SEROTONIN TYPE 2 AND DOPAMINE
RECEPTOR BLOCKADE
 MORE SPECIFIC TO MESOLIMBIC SYSTEM
 RAPID DISSOCIATION FROM DA RECEPTOR
 LOWER D2 BLOCKADE THEN DRA’S
 REDUCED EPS AND TARDIVE DYSKINESIA
 TREATMENT FOR SCHIZOPHRENIA
 TREATMENT TO MANIA
 RISPERID OLANZAPI QUETIAPIN ZIPRASIDO CLOZAPIN
ONE NE E NE E

PHARMA ACTIVE HALF LIFE HALF LIFE HALF LIFE 5 HALF LIFE
COLOGY METABOLIT 31 HRS. 7 HOURS TO 10 HRS 12 HRS.
E
SIDE ANXIETY, Inc. SUGAR, DIZZINESS NO WEIGHT SEDATION
EFFECTS EPS WEIGHT, SOMNOLEN GAIN AGRANULO
SEXUAL SGPT, CE ANTIDEP CYTOSIS,HY
EPS TREMOR, WEIGHT EFFECT POTENSION
RHINITIS AKATHISIA GAIN LEAST PROLONG SIALORRHE
EPS QT INT. A
SEIZURES
DOSAGES 1 TO 5 TO 15MG 400 TO 40 TO 25 T0 300MG
4MG/DAY 800MG 160MG

DRUG PAROXETIN DON’T USE

INTERACTI FLUOXETIN WITH
ON PHENYTOIN
DECREASE CARBAMAZ PHENYTOIN CARBAMAZ
LEVEL EPINE EPINE
PHENYTOIN
INCREASE FLUVOXAM
DRUG
ARIPIPRAZOLE

PHARMACOLOGY HALF LIFE 75 TO 96 HRS NON SEDATING

EXCRETED IN MILK PARTIAL D2 AGONIST
DA MODULATOR COMPETE AT D2
PRE AND POST SYNAPTIC RECEPTORS FOR
BINDING ENDOGENOUS DA
INDICATION SCHIZOPHRENIA, MANIA

DOSAGE 15 TO 30 MG

SIDE EFFECT HEADACHE, AGITATION ANXIETY

SOMNOLENCE NAUSEA
HYPOTENSION

DRUG INTERACTION DECREASE: INCREASE:

CARBAMAZEPINE,VALPR KETOCONAZOLE,
ANTI- ANXIETY DRUGS

BENZODIAZEPINES AND DRUGS

ACTING ON BENZODIAZEPINE
RECEPTORS
SHORT HALF LIFE LONG HALF LIFE

TRIAZOLAM (2-3 HRS) DIAZEPAM,CLONAZEPAM

FLURAZEPAM (MORE THAN 100 HRS)

ALPRAZOLAM(8 TO 10 HRS)

MIDAZOLAM
LORAZEPAM, ESTAZOLAM (8 TO 30 HRS)

NO DRUG ACCUMULATION, NO DRUG ACCUMULATION

SEDATION DAYTIME PSYCHOMOTOR IMPAIRMENT

MORE FREQUENT DOSING INCREASED DAYTIME SEDATION

EARLIER AND MORE SEVERE
WITHDRAWAL SYMPTOMS
GREATER REBOUND INSOMNIA AND
ANTEROGRADE AMNESIA
WITHDRAWAL SIGNS/SYMPTOMS
WITHDRAWAL
 AVOID ABRUPT DISCONTINUATION
 SEEN MORE I DRUGS WITH SHORT HALF LIFE
 LOWER 25% OF DOSE PER WEEK
ADVERSE REACTIONS
 SEDATION- RESIDUAL DAYTIME SEDATION
 ANTEROGRADE AMNESIA
 AGGRESSIVE BEHAVIOR- TRIAZOLAM
 RESPIRATORY DEPRESSION
 TERATOGENIC
 HALLUCINATION AND BEHAVIORAL
CHANGES- ZOLPIDEM
PREPARATION: DOSE
EQUIVALENT
DIAZEPAM 5 MG
 CLONAZEPAM- 0.5
 ALPRAZOLAM-0.25
 LORAZEPAM- 1
 CLORAZEPATE-7.5
 MIDAZOLAM-0.25
 TRIAZOLAM-0.125
 ESTAZOLAM-0.33
 ZOLPIDEM-2.5