Anti-Pyschotics (2) Flashcards
What affect does Closapine have on
D4 and 5-HT2
D2
Muscarnic
Blocks D4 and 5‐HT2 receptors
• Little effect on D2
• Muscarinic antagonist
Clozapine (atyipcal) has what effect on + and - symptoms
Improves + symptoms in pts not helped by others
Improves negative symptoms
What are 2 big sideffects of Clozapine
Lowers seizure threshold
can cause fatal agranulocytosis
Effect of Olanzapine on
5-HT2
D1 and D2
D4
Potent 5-HT antagonist
D1, D2 ANTagonist, some D4
What is the side effect profile of olanzapine
few EPS and less seizure concern then Clozapine
Weight gain and diabetes adn possible abuse (snorting)
Combined D2 and 5HT-2 antagonist with greater reduction in negative sypmtoms and less EPS
Risperidone
has less seizure and antimuscarninic acitiviy then Clozapine
Risperidone
What is the active metabolite of Risperidone, how is it administered
Paliperidone
given as injection
Drug with simular effects on schizophrenia as risperidone and olanzapine but with a shorter half life
Quetiapine
What antipyschotic is approved for augmentation in depression
Quetiapine
5-HT2 and D2 antagonist
may ahve 5-HT1a agonist activity, no weight gain
Ziprasidone
A partial D2 agonist and 5HT2 antagonist, also approved for adjunct to tx depression
Aripiprazole
Uses of Antipsychotics
Acute episodes Chronic schizophrenia Manic episodes Schizoaffective Augment depression Tourettes Antiemesis
What drugs do we tx schizoaffective disorder with?
Paliperidone
What antipyschotics can we use to augment depression
Aripiprizole, olanzapine, quetiapine
What meds can we use to tx manic episodes or bipolar disorder
aripriprazole, olanzapine, quetiapine, ziprasidone, risperidone, asenapine
Meds used to tx Tourettes
haloperidole or pimozide
Prevalance of Bipolar Disorder
2.6% of adults and 82.9% are severe
not reporeted by sex or age with onset at 25
Criteria for Manic Episode
Inflated self esteem/grandiosity Decreased need for sleep Talkativeness Flight of ideas Distractibility Increased goal directed activity excess involvement in pleasurable activities
Bipolar I and II has emphasis with changes in
mood and changes in activity
Med used to tx bipolar
Lithium
Monovalaent cation of light alkali
has no effect on normals
blocks manic behavior
Lithium
Lithium, by inhibiting ______ may cause depletion of second messenger PIP2 adn thus reduce release of IP3 and DAG
recycling of inositol substrates
Lithium has complete absorption in ______
peak serum level in _____
6-8 hours
2 to 4 hours
What is the half life of lithium in young adults and elderly
YA: 18-24 hrs
elderly: 30-36
LIthium is ____ to plasma proteins
Has volume of distribtution_____
unbound
Equal to total body water
Lithium has CSF concentration is ______ of plasma concenteation
_____ of single dose is eliminated in urine
40-50%
95%
How do Na levels affect Li levels:
Increased Na excretion causes clinically significant increases in Li levels. ie. Thiazide diuretics, losses of fluids or electrolytes.
Therapeutic window of Li
Effect of ACE and ANGII inhibitors on Li
- Narrow therapeutic window (0.6to1.25mEq/liter. Important to monitor levels.
- ACE inhibitors and AngiotensinII receptor blockers can also raise Li levels
- Fatigue and muscular weakness
- Tremor - may be treated with beta-blockers
- GI symptoms
- Slurred speech and ataxia
side effects of Lithium
Serious toxicity at plasma levels about 2 to 3 times levels
o Impaired consciousness
o Rigidity and hyperactive deep reflexes
o Coma
• Lithium levels are affected by plasma____ levels thus interactions with diuretics and some antihypertensives
sodium
Clinical uses of Lithium
- Treat mania and prevent recurrences of bipolar disease.
- May be useful in preventing recurrences of unipolar depression in some patients.
- Schizoaffective disorder*.
- Cluster Headaches*.
Use to tx bipolar: Acts at sodium channel; CNS side effects such as sedation, confusion and ataxia
Carbamazepine
o Used as first line drug in bipolar disorder; sedating
Valproic acid and divalproex sodium (Depakote)
o antiseizure agents that also acts at sodium channels or glutamate receptors.
o Warning on suicidal ideation.
also used to tx bipolar
Lamotrigene (Lamictal®) and topiramate (Topamax®) –off Label
What can be Rx for initial tx of manic episodes seen in bipolar
haloperidol or clonazepam
a combination of olanzapine and fluoxetine.
o Indicated for bipolar disorder, depressive and treatment resistant major depressive disorder.
Symbyax®