ANTIPSYCOTICS DRUGS Flashcards
SYMPTOMS CATEGORIES OF SCHIZOPHRENIA
- POSITIVE SYMPTOMS, manifestation like delusions, hallucinations, thought disorder, paranoia, bizarre behavior
- NEGATIVE SYMPTOMS, non manifested, social withdrawal, flattened affect
- COGNITIVE DEFICITS, impairment in attention span, verbal learning, executive of the function, working memory
theory of etiopathogenesis, prevalence, onset and comorbidities of schizophrenia
- genetic theories (susceptibility or mutated gene), viral origin, developmental abnormality (early use of substance of abuse)
- hyperactivity of dopamine neurotransmission responsible for positive symptoms
- 0.5/1 % of population
- positive features in late adolescence or early adulthood
- depression, substance abuse, suicide ideation
antipsychotics drugs are classified in _____ and ______
atypicals have fewer _____ side effects, are more effective against negative symptoms and effective in ______ patients
typical, atypical
motor, treatment-resistant
nature of antipsychotic drygs
- all are dopamine D2 receptor antagonists blocking dopamine effect on cognition/movement regulation/vomiting stimulus/ inhibition of prolactin secretion
- some are not selective blocking also d1, histamine, serotonin receptors responsible for s/e
- block of 5-ht2 receptors (serotonin) have antipsychotic effect
S/E OF ANTYPSYCHOTICS DRUGS
- sedation, weight gain, postural hypotension
- idiosyncratic effect, jaundice, leucopenia, ski reactions
- special care if pts with neurodegenerative diseases (epilepsy/PD, contraindicated in pregnancy and lactation)
PHARMACOKINETICS AND CLINICAL USE OF ANTIPSYCHOTIC DRUGS
- GIVE PO/IM as depot slow release
- relationship between plasma concentration and effect can vary so careful dosage
- long half-life 15*30h
- hepatic metabolism
- use to treat schizophrenia/mania/impulsive behaviors/emesis
- control positive symptoms, long term use prevents recurrence
hypnotics drugs to treat_____
anxiolytics to treat anxiety, panic disorder, ______, ______
insomnia
phobias, PTSD
MOA of benzodiazepine
enhance the action of GABA by helping it bind better to its receptor, allosteric modulation
PHARMACOLOGICAL EFFECTS OF BENZO
- ANXIOLYTIC ACTION, reduce anxiety and depression without antidepressant effect (rebound reflex if discontinued abruptly)
- SEDATION AND SLEEP, reduce the time to fall asleep and duration of the sleep but not the REM stage of sleep
- tolerance can develop
other effects of benzo
- reduction in muscle tone and coordination, helpful in clinical settings like endoscopy
- anticonvulsant, treat seizures
- anterograde amnesia, clinically useful
benzos antagonist and inverse agonist
and pharmacokinetics
- Flumazenil antagonist used to treat overdose or post-op sedation
- beta-carbolines, inverse agonists, bind to the same receptors but have opposite effect. not used
- oral/iv/im administration
- strongly bound to plasma proteins
- accumulates in fat, metabolites in active metabolites
- duration of action varies→ short or long acting
- increased half-life in elderly people because of reduction of clearance in kidneys
unwanted side effects of benzos
- respiratory depression
- drowsiness/amnesia/impaired motor coordination/hangover
- tolerance and dependence both occur, tampering medications
5-HT1A RECEPTORS AGONISTS
- Agonist or partial agonists at serotonin receptors
- potent anxiolytics, unclear MOA, effective in days or weeks
- s/e nausea/dizziness/headache
NON BENZODIAZEPINE HYPNOTICS
(ZOLPIDEM, ZOPICLONE)
- NEw DRUG generation drives the GABA signal increasing it without waiting for endogenous GABA
- advantages vs BZs, rapid onset, short half-life, normal sleep, not myorelaxant, reduced abuse potential
- contraindicated in pregnancy and breastfeeding
LEMBOREXANT
- OREXIN RECEPTOR ANTAGONIST, orexin increases wakefulness/sense of alertness/helps to relax
- RELAXANT EFFECT
- LARGE LIST OF DRUG INTERACTIONS AND FOOD INTERACTIONS
- S/E weakness or dullness
- poor drug choise
