M2.4 Flashcards
- are used primarily to treat SCHIZOPRENIA
- also effective in other psychotic and manic states
antipsychotics
ANTIPSYCHOTICS are also called
NEUROLEPTICS or MAJOR TRANQUILIZERS
the use of these medications involves a difficult trade-off between the BENEFIT of alleviating psychotic symptoms and the risk of a wide variety of troubling ADVERSE EFFECTS
ANTIPSYHOTICS
ANTIPSYCHOTICS are ____ and DO NOT eliminate chronic thought disorders
NOT CURATIVE
ANTIPSYCHOTICS | CLASSIFICATION
1st gen
Classic drugs
azine & haloperidol
ANTIPSYCHOTICS | CLASSIFICATION
1st gen:
acts on ____
DOPAMINE receptor
DA antagonist
ANTIPSYCHOTICS | CLASSIFICATION
2nd gen
Newer agents
zapine, done
ANTIPSYCHOTICS | CLASSIFICATION
2nd gen:
acts on ____
5HT2 receptor (Serotonin)
5HT2 antagonist
- mental disorder which involves BREAKDOWN of PERSONALITY
- presence of delusions (false beliefs)
- halluciantions
- grossly disorganized thinking in a clear sensorium
PSYCHOSIS
PSYCHOSIS
various types of hallucinations
auditory
visual
tactile
olfactory
PSYCHOSIS
MOST COMMON type of hallucination
auditory
PSYCHOSIS | TYPES
typical baliw
schizophrenia
PSYCHOSIS | TYPES
Depression and Mania
affective disorders
PSYCHOSIS | TYPES
- has other causes
- mental disturbances caused by head injury, alcoholism, or other kinds of organic diseases
organic psychosis
PSYCHOSIS | TYPES
- a psychotic disorder characterized by DISTORTIONS in thinking, perception, emotions, language, sense of self, and behavior
- symptoms are grouped as positive symptoms and negative symptoms
SCHIZOPRENIA
PSYCHOSIS | TYPES
the SYMPTOMS of schizophrenia are grouped as ____ and ____
positive and negative symptoms
PSYCHOSIS | TYPES
SCHIZOPHRENIA:
* USUAL symptoms
* DELUSIONS (often paranoid in nature)
* HALLUCINATIONS, usually in the form of voices, and often exhortatory in their message (paranoia)
* THOUGHT disorder, comprising of wild trains of taught and IRRATIONAL conclusions (leads to irrational actions)
POSITIVE SYMPTOMS
PSYCHOSIS | TYPES
SCHIZOPHRENIA:
POSITIVE symptoms affect ____
MESOCORTICAL SYSTEM
PSYCHOSIS | TYPES
SCHIZOPHRENIA:
* ANTISOCIAL symptoms
* WITHDRAWAL from social contacts
* Flattening of emotional responses
NEGATIVE SYMPTOMS
PSYCHOSIS | TYPES
SCHIZOPHRENIA:
NEGATIVE symptoms affect the ____
MESOLIMBIC SYSTEM
PSYCHOSIS | TYPES
THEORIES | SCHIZOPHRENIA:
schizophrenic gene can be ____
inherited
(HEREDITARY)
PSYCHOSIS | TYPES
THEORIES | SCHIZOPHRENIA:
Neurodevelopmental disorder
- Cortical atrophy (certain part of the brain is small)
- Maternal virus during pregnancy
PSYCHOSIS | TYPES
THEORIES | SCHIZOPHRENIA:
certain chemical causes a defect in “SELECTIVE ATTENTION”
NEUROCHEMICAL THEORY
PSYCHOSIS | TYPES
THEORIES | SCHIZOPHRENIA:
____ or ____ has been proposed to be the cause of schziophrenia and is used as a basis for pharmacotherapy
biochemical imbalances or abnormality in the brain
PSYCHOSIS | TYPES
THEORIES | SCHIZOPHRENIA:
BIOCHEMICAL IMBALANCES
increased SEROTONIN
increased DOPAMINE
decreased GLUTAMATE
PSYCHOSIS | SCHIZOPHRENIA
Hallucinatory effects could be associated with 5-HT2A recpetor and possible 5-HT2C stimulation
SEROTONIN theory (hypothesis)
PSYCHOSIS | SCHIZOPHRENIA
SEROTONIN THEORY:
* modulate the RELEASE of dopamine, norepinephrine, glutamate, GABA, and acetylcholine in the cortex, limbic region, and striatum
5-HT2A & 5-HT2C receptors
PSYCHOSIS | SCHIZOPHRENIA
SEROTONIN THEORY:
* leads to DEPOLARIZATION of GLUTAMATE neurons (only in specific region of the brain) but also STABILIZATION of NMDA receptors
5-HT2A receptor stimulation
PSYCHOSIS | SCHIZOPHRENIA
SEROTONIN THEORY:
* leads to INHIBITION of CORTICAL and LIMBIC dopamine release
5-HT2C receptor stimulation
PSYCHOSIS | SCHIZOPHRENIA
major action
increase DA, SE
PSYCHOSIS | SCHIZOPHRENIA
inhibitory or excitatory
inhibitory effect
PSYCHOSIS | SCHIZOPHRENIA
DOPAMINE THEORY:
* many antipsychotic drugs strongly BLOCK ____ in thee CNS, especially in the mesolimbic and striatal-frontal system
postsynaptic D2 receptor
PSYCHOSIS | SCHIZOPHRENIA
DOPAMINE THEORY:
* drugs that ____ either AGGRAVATE schizophrenia psychosis or produce PSYCHOSIS DE NOVO in some patients
psychosis de novo - cause psychosis in healthy patients
increase dopaminergic activity
PSYCHOSIS | SCHIZOPHRENIA
DOPAMINE THEORY:
* dopamine-receptor density has been found postmortem to be ____ in the brains of schizophrenic
increased
PSYCHOSIS | SCHIZOPHRENIA
GLUTAMATE THEORY:
* hypofunction of ____ located on GABAergic internuerons, leads to DIMINISHED INHIBITORY influences on neuronal function
NMDA receptors
PSYCHOSIS | SCHIZOPHRENIA
GLUTAMATE THEORY:
* an ____ of downstream glutamatergic activity, which can lead to HYPERSTIMULATION of cortical neruons through non-NMDA receptors
induce disinhibition
PSYCHOSIS | TYPES
- characetrized primarily by CHANGES OF MOOD rather than by thought disorder
- Depression
- Mania
AFFECTIVE DISORDERS
PSYCHOSIS | AFFECTIVE DISORDERS
DOWN phase
depression
PSYCHOSIS | AFFECTIVE DISORDERS
HYPERACTIVE
mania
PSYCHOSIS | AFFECTIVE DISORDERS
TYPES OF DEPRESSIVE SYNDROME
Unipolar
Bipolar
PSYCHOSIS | AFFECTIVE DISORDERS | TYPES OF DEPRESSIVE SYNDROME
- Reactive depression
- Endogenous depression
UNIPOLAR
PSYCHOSIS | AFFECTIVE DISORDERS | TYPES OF DEPRESSIVE SYNDROME
UNIPOLAR:
* caused by external factors clearly associated with STRESSFUL LIFE EVENTS, and accompanied by symptoms of anxiety and agitation
* characterized by a PERIOD OF SHOCK and DEPRESSION which is followed by a period of READJUSTMENT and resolve that life must go on
REACTIVE depression
PSYCHOSIS | AFFECTIVE DISORDERS | TYPES OF DEPRESSIVE SYNDROME
UNIPOLAR:
* UNRELATED to external stress
* may involve psychological DISTURBANCES and MALADJUSTMENTS or BICOHEMICAL DEFECTS in the brain
ENDOGENOUS depression
PSYCHOSIS | AFFECTIVE DISORDERS | TYPES OF DEPRESSIVE SYNDROME
- characterized by ALTERNATING CYCLES of depression and mania
- weeks of depression, then mania
BIPOLAR AFFECTIVE DISORDER
PSYCHOSIS | AFFECTIVE DISORDERS | TYPES OF DEPRESSIVE SYNDROME
BIPOLAR:
____ is the OPPOSITE of depression, with excess exuberance, enthusiasm and self-confidence, accompanied by impulsive actions
MANIA
DRUGS FOR PSYCHOSIS
ANTIPSYCHOTICS:
blockers of ____
DOPAMINE receptors
DRUGS FOR PSYCHOSIS
MOST antipsychotics are ____ in action, meaning they block other receptors such as alpha adrenergic, hsitamine, and serotonin receptors in addition to dopamine receptor
NONSELECTIVE
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
- MOA: block D2 receptors
- ADDITONAL EFFECTS: anti-HAM (Histamine, Alpha1, Muscarinic)
- USE: for POSITIVE symptoms only
1st gen / Classical / Traditional / Typical antipsychotics
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
1st gen:
azine
phenothiazine
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
1st GEN:
peridol
Butyrophenones
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
1st GEN | PHENOTHIAZINE:
aliphatic
promazine
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
1st GEN | PHENOTHIAZINE:
piperazine
phenazine
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
1st GEN | PHENOTHIAZINE:
piperidine
ridazine
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
1st GEN:
* for MANIC phase
BUTRYOPHENONES - “peridol”
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
DOC for PEHNCYCLIDINE overdose and is clinically used also in HUNTINGTON’S disease and TOURETTE’S syndrome
HALOPERIDOL
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
1st GEN:
thix
thioxanthenes
thiothixine
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
POTENCY
butyrophenos = piperazines > piperidine . thioxanthenes > aliphatic
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
increase HAM affinity
Aliphatic > Thioxanthenes > Piperadine > Piperazine = Butyrophenone
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
- MOA: block 5HT receptor more than D2 receptor, block D4
- USE: for NEGATIVE symptoms
- LESS binding to DA = LESS EPS
2nd gen / ATYPICAL antipsychotics
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
the ONLY atypical WITHOUT EPS effect
EPS - extrapyrimidal syndrome
CLOZAPINE
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
POSITIVE symptoms
1st gen = 2nd gen
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
NEGATIVE symptoms
2nd gen > 1st gen
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ATYPICAL:
* no EPS
* only antipsychotic that REDUCE SUICIDE EFFECT
* causes seizure, agranulocytosis, myocarditis
CLOZAPINE
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ATYPICAL:
CLOZAPINE causes
seizures
agranulocytosis
myocarditis
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ATYPICAL:
* NEWEST
* partial D2 agonist
* LEAST sedating
ARIPIPRAZOLE
prazole but not PPI
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ATYPICAL:
* causes OVERWEIGHT or OBESITY
Olanzapine
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ATYPICAL:
* used for INTRACTABLE HICCUPS
Risperidone
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ATYPICAL:
* causes QT prolongation
Ziprasidone
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ATYPICAL:
* watch out for sedation (VERY SEDATING)
QUETIAPINE
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
decrease level of DA = increase Ach
EPS
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
management for EPD
anticholinergics
antiCHOLINERGICS
Biperiden
Benztropine
Trihexylphenidyl
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
* LOW DA = HIGH PROLACTIN
* galactorrhea, amenorrhea, infertility, decrease libido
HYPERPROLACTINEMIA
a PROLACTIN INHIBITING hormone
DA
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
* rare life threatening
* idiosyncratic
* fever, muscle rigidity, altered mental status, unstable vital sign
MALIGNANT HYPERTHERMIA
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
DOC for MALIGNANT HYPERTHERMIA
DANTROLENE
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECT:
due to H1 receptor blockade
sedation
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
due to alpha1 blocker
orthostatic hypotension
failure to ejaculate
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
due to M receptor blockade
anticholinergic effects
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECT:
by CLOZAPINE
seizure
agranulocytes
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECT:
CARDIAC: Clozapine
myocarditis
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECT:
CARDIAC: Thioridazine, Ziprasidone
QT prolongation
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
by THIORIDAZINE
may cause blindness
RETINAL DEPOSITS
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
by CHLORPROMAZIE
does NOT cause blindness
CORNEAL DEPOSITS
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECT:
common in 2nd gen antipsychotics except in Amilsupride, Molindone, Aripiprazole
weight gain
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECT:
by OLANZAPINE
risk for DM
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
PROTOTYPE
CLOZAPINE
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
ADVERSE EFFECTS:
* occurs with the CHRONIC USE of antipsychotics
* has two main kinds: Acute Dystonias, Tardive Dyskinesia
EXTRAPYRIMIDAL MOTOR DISTURBANCES
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
AE | EPMD:
* are involuntary movements (muscle spasm, protruding tounge, torticollis, and often a PArkinson-type syndrome)
* REVERSIBLE
ACUTE DYSTONIAS
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
AE | EPMD:
* consist of involuntary movements, often of theFACE and the TOUNGE, but also of the TRUNKS and LIMBS
* IRREVERSIBLE
TARDIVE DYSKINESIA
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
AE | EPM:
incidence of extrapyrimidal effects is LESS with ____
ATYPICAL
bcs they bind to SE
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ONSET OF ACTION
may not be effective for several weeks
DRUGS FOR PSYCHOSIS | NEUROLEPTICS
ONSET OF ACTION:
sedation and side effects
rapidly
PHARMACOLOGY | NEUROLEPTICS
AE:
* Hyperprolactinemia
* Endocrine effects
* Gynecomastia
* Galactorrhea
* Sexual dysnfunction
DOPAMINE-receptore blockade
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
AE:
* difficulty micturition
* constipation
* blurred vision
* dry mouth (xerostomia)
CHLONIERGIC-receptor blockade
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
AE:
* failure to ejaculate
* orthostatic hypotension
* light headedness
ALPHA-ADRENOCEPTOR blockade
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
AE:
* sedation
HISTAMINE blockade
DRUGS FOR PSYCHOSIS | NEUROLEPTICS | ATYPICAL
AE:
* hypothermia
* hyperthermia
SEROTONIN blockade
PHARMACOLOGY | NEUROLEPTICS
- primarily indicated for schizophrenia
- CATATONIC forms of schizo
- best managed by IV benzodiazepines
- also indicated fro schizoaffective disorders
- therapy of psychotic depression and bipolar affective disorder
PSYCHIATRIC INDICATONS
PHARMACOLOGY | NEUROLEPTICS
MONOtherapy of ACUTE BIPOLAR depression
QUETIAPINE
IURASIDONE
OLANZAPINE (in combination with Fluoxetine)
PHARMACOLOGY | NEUROLEPTICS
adjunct to antidepressants in the treatment of UNIPOLAR depression
Aripiprazole
Quetiapine
Olanzapine
PHARMACOLOGY | NEUROLEPTICS
indicated in HIGHLY AGITATED and MANIC patients
haloperidol
PHARMACOLOGY | NEUROLEPTICS
have a specific antidepressant action
Sulpiride
PHARMACOLOGY | NEUROLEPTICS
tx of HUNTINGTON’S chorea
uncontrollable DANCE-like movements
HALOPERIDOL
PHARMACOLOGY | NEUROLEPTICS
NONpsychiatric:
NOT an anti-emetic
THIORIDAZINE
PHARMACOLOGY | NEUROLEPTICS | NONPSYCHIATRIC
anti-emetic
Prochlorperazine
Benzquinamide
PHARMACOLOGY | NEUROLEPTICS | NONPSYCHIATRIC
used in combination with NARCOTIC analgesics for the tx of CHRONIC PAIN with SEVERE ANXIETY
Droperidol & Fentanyl citrate
PHARMACOLOGY | NEUROLEPTICS | NONPSYCHIATRIC
for relief of PRURITUS
Phenothiazines
PHARMACOLOGY | NEUROLEPTICS | NONPSYCHIATRIC
as PREOPERATIVE sedatives
Promethazine
CLINICAL EFFICACY OF ANTIPSYCHOTICS
____ may be needed in controlling symptoms of ACUTE schizophrenia
large doses
CLINICAL EFFICACY OF ANTIPSYCHOTICS
____ antipsychotic treatment is often effective in PREVENTING RECURRENCE of schizophrenic attacks
LONG-TERM
CLINICAL EFFICACY OF ANTIPSYCHOTICS
____ are effective only in 70% of schizophrenic patients
typical antipsychotics
CLINICAL EFFICACY OF ANTIPSYCHOTICS
30% are classes as
treatment resistant
CLINICAL EFFICACY OF ANTIPSYCHOTICS
TYPICAL antipsychotics effectively control the ____ symptoms
POSITIVE
CLINICAL EFFICACY OF ANTIPSYCHOTICS
TYPICAL antipsychotics are INEFFECTIVE in relieving ____ symptoms
NEGATIVEQ
CLINICAL EFFICACY OF ANTIPSYCHOTICS
____ overcome theb SHORTCOMINGS of typical antipsychotics, showing efficacy in “treatment resistant” patient and improving negative & positive symptoms
CLOZAPINE
CLINICAL EFFICACY OF ANTIPSYCHOTICS
the ONLY ATYPICAL antipsychotic drug indicated to REDUCE the RISK of SUICIDE
CLOZAPINE