March 12 Exam - set 1 Flashcards
Raloxifene (type)
SERM
Calcitonin analogs (MOA)
decreased osteoclast activity;
blocks renal reabsorption of PO4 and Ca2+
Cinacalet
Calcium receptor potentiator
Binds to Ca-sensing region of CaR to inhibit PTH release
–allosteric modulator .. in presence of Ca2+, it makes it more effective at stimulating receptor
Vitamin D MOA
inc Ca2+ and PO4 abs from gut and reads from renal tubules
Bisphosponates MOA
inhibit bone reabsorption
- reduce formation and dissolution of hydroxyapatite crystals
- inhibit farnesyl-PP synthesis of osteoclasts
Suffix of bisphosphonates
-dronate
Teriparatide
PTH analog (aa 1-34)
Prolia (Denosumab)
Humanized monoclonal AB against RANKL .. binds RANKL to prevent activation of RANK and therefore prevent differentiation of osteoclasts
What is difference about atypical vs typical antipsychotics?
- Better affinity at D2 receptors
- Addition of activity at 5HT2A and others
- Better control over negative and cognitive sx (positive already controlled by typicals)
- Fewer EPS
Key feature of antipsychotics
block of D2 receptors
Dopamine pathways
Mesocortical/mesolimbic
-therapeutic and cognitive activities of D2 antagonists
Nigrostriatal (basal ganglia)
- motor control
- EPS sx arise here
First gen antipsychotics
Penothizaines
Haloperidol
2nd gen antipsychotic
–whats diff about it?
Clozapine
–acquisition of 5HT2A pharmacology
Aripirazole
D2 partial agonist
Classic early and atypical antipsychotics
Chlorpromazine
Haloperidol
Thioridazine
Sulpiride
Atypical antipsychotics
These have acquired 5HT pharm
Clozapine Risperidone Olazapine Ziprasidone Quetiapine Aripiprazole
What are the SSRIs?
Fluoxetine Paroxetine Fluvoxamine Sertraline Escitalopram
(note: -oxeltines inhibit P450s)
What are the SNRIs?
Duloxetine
Venlafaxine
Desvenlafaxine
Which class do TCAs fall under?
SNRIs
What are the TCAs?
Imipramine Amitriptyline Nortriptyline Clomipramine Desipramine
Imipramine
highly anticholinergic
Amitriptyline
activity at many other receptors
sedating
Nortriptyline
secondary amine
desipramine
metabolite of imipramine
secondary amine
Why does it matter if something is secondary vs tertiary amine WRT TCAs?
tertiary amines give rise to secondary metabolites, so administering a tertiary amine means you have a secondary on board as well
Trazidone
5HT2 antagonist
Also 5HT1 partial agonist
weak reuptake blockade
Bupropion (type and MOA)
Unicyclic
DAT, NET, nAChR block
Mirtazapine
Tetracyclic
mixed block at 5HT, alpha AR, histamine, mACh, DAT, NET, SERT
What are some MAOIs?
Selegiline - MAOB selective
Tranylcypromine - nonselective
Phenelzine - nonselective
All are irreversible
What is the difference b/t MAO-A and MOA-B?
MAO-A: found in monoamine expressing neurons in the CNS
MAO-B: found in DA neurons and in cells that need to break down phenylethylamine
Possible MOAs of lithium
Inositol depletion
–inositol may be increased during manic phases
Inhibition of GSK-3
–GSK3 is a multifxnal kinase in the brain and elsewhere
