🎭🌀💊 pharmacology bipolar/psychosis/schizophrenia

5-HT2A and glutamate

schizophrenic pts may present with increase in DA2 upregulation and decrease in?

glutamate or NMDA receptors

is an excitatory neurotransmitter that is depleted in schizophrenic patients

d2 receptor antagonism

an increase in prolactin is an indicator of?

histamine receptors and trace amine receptors? (not sure if I heard him correctly)

for the recitation: what are some of the mu receptors that might be exploited for anti-psychotic drugs? (not sure if I heard him correctly)

true

2nd gen antipsychotic drugs rapidly dissociate from the receptor. true or false

- substantia nigra

- nucleus accumbens

- basal ganglia

- cortex

5-HT2A antagonist increase dopamine where?

clozapine

pimozide

olanzapine

quetiapine

ziprasidone

risperidone

pimanvanserin

atypical antipsychotics

- antimuscarinic

- a1-adrenergic blocker

- anti-histamine

- DA (DA2 & DA4) antagonist

- 5-HT (5-HT2) antagonist

antipsychotic drug receptor activities?

5-HT2A inverse agonist

pimavanserin moa

agranulocytosis

unique side effect of clozapine

clozapine

this typical antipsychotic has very low affinity for DA2 receptor

DA2 and 5-TH1A partial agonists AND 5-HT2A antagonist

aripiprazole and brexpiprazole are?

brex has less EPS effect

brexpiprazole has the moa as aripiprazole. the diff is?

haloperidol

fluphenazine

thioridazine

loxapine

perphenazine

trifluoperazine

thiothiexene

1st generation antipsychotic therapies

tardis dyskinesias

antipsychotics may have risk of extrapyramidal motor symptoms like?

2nd generation antipsychotics

- may improve negative and cognitive symptoms by increasing dopamine release in the prefrontal cortex

- 5-HT2A antagonists:

• Dissociate rapidly from D2 receptors

• Some are 5-HT1A agonists

5-HT2A

aripiprazole and brxipiprazole are DA2 and 5-HT1A partial agonists. What receptor do they antagonize?

cariprazine

this second gen antipsychotic has D2/D3 partial agonist activity

- has 5-HT2A&2B antagonist activity

- NVD

- increase BW

- akathisia

common side effects in 2nd gen antispychotics?

impairment in cognitive function

antagonizing d1 receptor will result in?

antipsychotic, positive relief symptoms, EPS, and increase in prolactin

antagonizing d2 will result in?

- antidepressive and anxiolytics

agonizing 5-HT1A will result in?

improving negative symptoms, cognitive impairment, and decreased EPS

antagonizing 5-HT2A will result in?

antiemetic action

antagonizing 5-HT3 will result in?

pokilothermia - causing over heating due to taking antipsychotics

antipsychotics can cause?

- EPS (extrapyramidal system)

• acute dyskinesias and dystonic reaction

• tardive dyskinesia

• parkinsonism

• akinesia

• akathisia

• neuroleptic malignant syndrome

- orthostatic hypotension

- constipation

- urinary retention, worsening of narrow-angle glaucoma

- confusion, sedation, potentiation of other CNS depressants

- impotence

- altered thermoregulation

- dyscrasias

- CV - orthostasis and/or vasodilation

- anticholinergic effects

- weight gain - H1 receptor

- type 2 diabetes

antipsychotics ADR/SE

weight gain

H1 antagonism will lead to?

anticholinergic effects and reduced EPS

M1 antagonism will lead to?

- tremor

- torticollis

-opistotonus

- oculogyric crises

-dystonia

- restlessness like akinesia or akathisia

- pro epileptogenic

- elevated prolactin

- abnormal thermoregulation

EPS symptoms?

benztropine

- doesn't stop them but just masks them. When they do finally occur, they will happen at a greater and stronger magnitude

anti-convulsant used to mask tremors that can occur when using anti-psychotics?

acetylcholine

innervation of parasympathetic and sympathetic nerves on sweat glands have which post-synaptic nerve transmitter?

dantrolene

- it can't be treated with NSAIDs

malignant hypothermia or neuroleptic malignant syndrome caused by antipsychotics can be cured with?

true

true or false: when taking antipsychotics, you monitor myoglobin, HA1C, and lipid panel as they can cause dyslipidemia, weight gain, and/or type 2 diabetes

ziprasidone

this antipsychotic has a black box warning for prolonging the QTC interval

- lithium

- anticonvulsants

- antipsychotics

- benzo's

drugs for bipolar disorder

pokilothermia

body temperature change from drugs

dopamine and serotonin receptors

(DA2 & 5HT)

receptors that are affected when a patient has psychosis?

- weight gain

-extrapyramidal motor system

- Parkinson - like syndrome

- tardive dyskinesia - dystonia, torticollis, opisthotonus, others

- insulin resistance or TYPE 2 Diabetes

- hyperlipidemia

- orthostatic hypertension (alpha 1)

- increase seizure risk

- dyscrasias (agranulocytosis- esp in clozapine)

- anticholinergic effects

- NMS or malignant hyperthermia-treat with dantrolene

ON THE TEST: For side effects for anti-psychotics make sure to select all that apply

lithium

carbamazepine

valproate

clozapine

drugs to treat BPD?

when lithium aint working

when do u use CBPZ to treat BPD?

b) pokilothermia

Which of the following is an effect of anti-psychotics due to the potential anticholingeric effect which prevents them to sweart

a) hypothermia

b) pokilothermia

c) hyperthermia

D1 receptor

Aside from serotonin, which dopamine receptors are responsible for impulsive behavior?

- lithium

- anticonvulsants

- antipsychotics

- bzds

drugs to treat bipolar disorders?

- inhibits depolarization-mediated and Calcium-dependent release of neurotransmitters

- inhibits IP3/DAG pathway

- inhibits glycogen synthase kinase-3B

lithium moa?

lithium

- inhibits DA transmission

- inhibits glutamate transmission

- enhances GABA transmission

- inhibits glycogen synthase kinase - 3b

- depletes inositol

- hand tremors

- increase urination

- mild thirst

- diarrheea

- vomiting

- drowsiness

- muscular weakness

- lack of coordination

- nephrotoxic above 2.0 mmol/L

lithium ADE?

lithium

has a neuroprotective effect (BDNF and Bcl-2)

- inhibits the intracellular proteins: PKC, MARCKS, GSK-2, IPPase, IMPase

lithium

can compete with sodium at the ion channels and cause CV changed like QTC prolongation

lithium

- mood stabilizer where ADE:

- changes in thyroid function

- cardiac effects

- edema

- renal effects

- skin issues

- preg category D

- toxic blood levels close to therapeutic levels

lamotigrine

- mood stabilizer where ADE:

- dizziness

- headahce

- insomnia

- severe skin reactions like SJS

valproic acids

- mood stabilizer where: headache or ovarian cysts, hyperammonaemia (ammonium in blood)

- can be used alone or in conjunction with lithium

- for pts with mixed mania

TCAs

SSRIS

BZDs

neuroleptics (risperidone, haloperidol, olanzapine)

buspirone

pindolol

gabapentin

inositol

clonidine

trazodone

lithium

OCD drugs?

clompiramine

has the greatest anticholinergic effects of the tricyclics (TCA)