Term
Which DA receptors are stimulatory?
Which DA receptors are inhibitory? |
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Definition
D1 and D5 are Gs coupled and activate adenylyl cyclase.
D2, D3, D4 are Gi coupled and inhibitory |
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Term
| What are some of the pharmacokinetics of typical antipsychs? (6) |
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Definition
Oral or IM
Variable bioavailability
First pass hepatic metabolism with CYP1A2, 2D6, or 3Y4
Renal excretion
t (1/2)-20-30 hrs
takes days to weeks to start working |
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Term
| When would you want to use a short acting IM antipsych? |
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Definition
| for non compliant patients |
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Term
| What should you think about when you see CYP2D6? |
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Definition
| genetic vatiation- through SNPs (small nucleotide polymorphisms) |
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Term
| Which typical antipsych drug blocks D2 receptors and is used for antiemetic effect, hyperactivity, intractible hiccups and psychosis. |
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Definition
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Term
| Which typical antipsych is used for agitated depression |
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Definition
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Term
| What typical antipsych would you use for acute agitation/mania that comes in oral and IM form? |
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Definition
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Term
| What is one of the main advantages of Haloperidol? |
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Definition
| It comes in a immediate acting IM version to treat non compliant pts for acute sx of psychosis, acute agitatoin, delirium agitation, Tourette syndrom. Also comes in oral form. |
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Term
1)Which receptor is mainly blocked by typical antipsychs?
2) What are some of its effects on different parts of the brain? |
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Definition
1)Typical antipsychs mainly block D2 receptor
2) Blocking D2 in mesolimbic pathway causes repression of positive sx (symptoms)
Blocking in basal ganglia causes extrapyramidal effects (tremors) (EPS)
Blocking D2 in tuberoinfundibular system causes increase in serum prolactin |
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Term
| How would blocking D2 receptor in the basal ganglia cause EPS? |
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Definition
| Blocking D2 in basal ganglia blocks the inhibitory indirect pathway which causes a net excitatory effect causing EPS on SNpr and GPi. |
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Term
| What are the effects of an increase in serum prolactin through inhibition of D2 receptors in the tuberoinfundibular pathway? |
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Definition
Hyperprolactinemia causes amenorrhea, devreased libido, gynecomastia and infertility
Normally neuroendocrine neurons in hypothalamus secrete DA which binds to D2 receptors and block secretion or prolactin from pituitary. |
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Term
| What happens when you block 5HT2 receptors |
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Definition
Benefits against negative Sx (maybe)
causes weight gain |
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Term
| How would you get the side effect of orthostatic hypotension from typical antipsychotics? |
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Definition
| Typical antipsychs have some affinity for alpha-1R blocking them causes this sx. |
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Term
| Typical antipsychs also have some affinity for MuscarinicR and H1R what is the side effect of blocking these receptors? |
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Definition
| MuscarinicR-causes blurred vision, constipation, dry mouth, urinary retention Blocking H1R causes drowsiness increased appetite contributes to weight gain. |
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Term
| What is meant by Pokilothermic? Why is it dangerous? What drug causes this? |
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Definition
Typical antipsychs cause this.
It means that you have a lower threshold for change in temperature so when its really hot you can become hyperthermic or when its really cold you get hypothermia. |
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Term
| What is the US Boxed warning in typical antipsychs? |
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Definition
| increases risk of stroke in older pts with dementia related psychosis. |
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Term
| What are some additional adverse effects of typical antipsychotics? |
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Definition
Cannot abruptly discontinue in pregnancy. BUT use in 3rd trimester causes risk of EPS and withdrawal sx in babies.
Typical antipsychs cause lower threshold for seizures causes cadiac arrhythmia and risk of rash, photosensitivity |
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Term
What is Neuroleptic malignant syndrome?
Which drugs cause it? |
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Definition
FALTER-Fever, Autonomic instability (causes unstable BP), Leukocytosis, Tremor, Elevated CPK, Rigidity of muscles.
This is a rare side effect of typical antipsychs |
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Term
| How would you manage neuroleptic malignant syndrome? |
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Definition
| withdraw offending drug, supportive care, benzos, dantrolene, DA agonist. |
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Term
1) Which use of antipsychotics would cause tolerance?
2)Do typical antipsychotics have abuse potential? |
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Definition
1) Tolerance builds to sedatitive effects not the antipsychotic effect.
2) no abuse potential |
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Term
| Which typical antipsychotics have high potency and what is its correlation with EPS, sedative effects, hypotension and anticholinergic effects? |
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Definition
| Fluphenazine and Haloperidol have high potency Causes increase in EPS, low sedative effects, low hypotension and low anticholinergic effect |
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Term
What is the advantage of low potency antipsychotic drugs?
Which ones are they? |
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Definition
Low potency causes low EPS but high sedation, hypotension and anticholinergic effects.
Clorpromazine and Thioridazine have low potency |
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Term
| Which drugs inhibit CYP2D6? WHat does this cause? |
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Definition
| Chlorpromazine and thioridazine. Inhibiting CYP2D6 increases serum level of antidepressants and other substrates of the enzyme It reduces efficacy of prodrugs that require conversion to active form like codeine. |
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Term
| Which typical antipsych drugs increase QTc interval. What does this cause? |
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Definition
Thioridazine increase QTc interval and leads to risk of arrhythmias
Do not use with other drugs that do this listed in later cards includes TCAs |
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Term
| Would you use drugs with antiadrenergic and or anticholinergic effect with typical antipsychotics? |
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Definition
| No would have an increased risk of side effects. |
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Term
| What are the PKs of atypical antipsychotics? |
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Definition
| oral, IM widely distributed CYP metabolism and phase 2 conjugation exception is ziprasidone some have active metabolites renal and biliary excretion |
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Term
| Why is it dangerous to have more than 80% occupancy of D2 receptors? |
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Definition
| causes EPS up to 60% occupancy has antipsychotic effects |
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Term
| Which receptor type does Chlorpromazine have the more affinity for? |
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Definition
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Term
| Which receptor type does Haloperidol have more affinity for? |
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Definition
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Term
| List some atypical antipsychotics and their respective affinity for receptor type. |
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Definition
Clozapine-D4=alpha1
Olanzapine 5HT2A more than H1> D2>alpha1
Aripoprazole D2= 5HT2A
Quetiapine H1> alpha1 |
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Term
1) Which 2 atpypical antipsychotics have the highest risk of weight gain.
2) What comorbidities are associated with weight gain? |
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Definition
1) Clozapine and Olanzapine
2)hyperglycemia and hyperlipidemia |
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Term
| Which atypical antipsych is the prototype drug and what are some of its side effects? |
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Definition
Clozapine
Seizures, myocarditis, agranulocytosis, atropine-like poisoning at high doses. |
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Term
Why would you want to monitor the dose and levels of Clozapine with someone who smokes?
What other drugs would you not want to prescribe with Colazpine? |
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Definition
Clozapine is metabolized by CYP1A2 and others
Smoking induces CYP1A2. So if pt is in hospital where they cant smoke Clozapine levels increase and when they start smoking again the same dose of clozapine will not work and exacerbate psychotic sx.
Ciprofloxacin; fluvoxamine; theophylline inhibit CYP1A2 |
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Term
Which drug is used to treat refractory chizophrenia and treatment resistant schizophrenia
Which receptors does the drug bind to? |
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Definition
1)Clozapine
2) binds to block D4R=alpha1>5Ht2A decreases EPS |
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Term
Which atypical antipsychotic is used to treat acute mania, schizophrenia, maintenance of bipolar disorder, and irritability/agression associated with autism?
Which receptors does it bind? |
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Definition
1) Risperidone
2) binds to block 5HT2A>D2 |
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Term
| Patient comes in with akathisia, EPS from high levels of atypical antipsychotic. Which one is it? |
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Definition
Risperidone.
Paliperidone is ts active metabolite. |
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Term
Which drug is an analog of clozapine but is cheaper with fewer autonomic adverse effects and no reports of agranulocytosis.
Hint: Uses are schizophrenia, acute agitation (IM) bipolar disorder |
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Definition
Olanzapine
WARNING: causes significant weight gain, sedation, lowers seizure threshold, orthostatic hypotension, increased QTc and EPS at higher doses. |
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Term
| Which one of the atypical drugs is used for depressive episodes associated with bipolar disorder and an adjuct for maintenance tx of bipolar disorder? |
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Definition
Quetiapine
also used for schizophrenia similar to the other atypical drugs
Adverse effects are typical of class. |
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Term
| How does Ziprasidone work? What are its uses? |
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Definition
| blocks D2/5HT2A but agonist of 5HT1A potential antidepressant and anxiolytic effect Uses: same as the other atypical drugs |
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Term
| Why would you not prescribe ziprasidone with thioridazine, pimozide, antiarrhythmics, antilarials like qeuinine, artemether lumefantrine? |
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Definition
| causes QTc prolongation associated with ventricular arrhythmias and DEATH! |
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Term
| Which atypical drug is a partial agonist of D2 and 5HT1A but antagonist of 5HT2A What are some adverse side effects (AE)? |
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Definition
| Ariprazole AE: headache insomnia. dose related akithesia NOTE: no QTc interval prolongation |
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Term
| What is the drug that is mostly prescribed to treat mania but works by blocking inositol? |
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Definition
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Term
| Which drug causes aPolyuria and polydyspsia from diabetes insipidus? |
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Definition
| Lithium due to its blocking effects on ADH. |
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Term
Pt presents to ER with vomitting, profuse diarrhea, gross tremor, slurred speech, hyperreflexia, taxia, coma, convulsions and DEATH
What caused it how would you treat it? |
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Definition
acute toxicity with lithium
TX-supportive care and dialysis |
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Term
| Why is Li+ considered a category D drug? |
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Definition
NOTE: Li+ is mainly distributed in water During pregnancy mother will have greater volume of water so increasing dose during pregnancy needs to be reduced when she gives birth because water level will go down and cause toxicity
Lithium crosses placenta and secreted in breast milk. It can cause Li+ toxicity in fetus cardiac anomalies in the fetus especiallly Ebstein anomaly. |
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Term
| Which drug is used to treat mania but is KNOWN to be tetatogenic? |
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Definition
Valproic acid
efficacy = Li+ give to pts who do not respond to Li+ |
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Term
| Which drug used to treat mania is associated with Stevens Johnsons syndrome specifically in ppl with HLA-B |
|
Definition
Carbamazepine
Lamotrigine can also cause Stevens Johnson Syndrome. |
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Term
| Which drug would not work in acute mania and why? |
|
Definition
| Lamotrigine because it needs to be titrated up slowly. |
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