Neurochemistry/ Neuropharm/tox Flashcards
pregnancy C?
no human data. animal studies with risk or not avail
Pregnancy category D?
evidence of fetal risk but benefits might outweigh risks
Pregnancy D AEDs? (3)
VPA
Phenytoin
Carbamazepine
Carbamazepine risks w/ pregnancy?
When / how to use?
- cranial facial, neural tube, doll-like faces, long philtrum, palpebral folds
- transient hepatic tox
- if using, supplement w/ vit K, avoid T1
Risk of VPA and pregnancy
VPA! (Neural tube, neurobehavioral, craniofacial, cardiac, w/d sx/liver tox
What is the action of the tetrodoxin pufferfish?
blocks the voltage gated Na channel and prevents action potential (rising phase)
WHat is the presynaptic autonomic ganglion neurotransmitter / receptor?
nicotinic ACh in both PNS and SNS
What is the postganglionic receptor/neurotransmitter in the Parasympathetic nervous system?
muscarinic ACH
What is the post-ganglionic neurotransmitter / receptor of the sympathetic nervous system?
Norepinephrine / adrenergic
Exception: Muscarinic ACh in sweat glands
LEMS pathophys?
Blocks Ca2+ presynaptic channel leading to blockage of ACh release at NMJ
Myasthenia Gravis pathophys?
Abs block ACH receptor on post synaptic membrane in NMJ
Pathophys of Botulinum?
Prevents ACH release at NMJ by blocking SNAP-25 needed for vesicle fusion
Pathophys of autosomal dominant nocturnal frontal epilepsy
Nicotinic ACH receptor defect
Alpha bungarotoxin mechanism of action?
Nicotinic ACH receptor antagonist
Alpha: after the synapse, beta: before the synapse
Beta bungarotoxin (sea snakes) pathophys?
Before the synapse, causes ACH release
Alpha: after the synapse, beta: before the synapse
Latrotoxin (black widow spider)
augments ACh release before the synapse
hypermagnesium and effect on NMJ
competes w/ calcium for uptake, so too much causes decreased release of presynaptic ACh at NMJ
Mechanism of action of Atropine?
counteracts increased muscarinic action during cholinergic crisis
nightshade and jimson weed contain what? effect?
atropine
anticholinergic effect
potential mechanism of action of tick paralysis?
decreased ACh release
5HT3 receptor use?
target of antinausea drugs
Reserpine mechanism of action and issue?
irreversibly inhibits vesicular monoamine transporter (VMAT) and leads to monoamine depletion
A BP med that causes serious depression
What sx (2) best differentiates serotonin syndrome and neuroleptic malignant syndrome?
In serotonin syndrome you get diarrhea and myoclonus
MDMA drug (ecstasy) acts by what mechanisms/effect? (3)
vesicular monoamine release, oxytocin (enactogenic effect) and excitotoxicity
LSD mechanism of action?
5HT-2A partial agonist: hallucinogen
Lorcaserin (Belviq)
5HT-2C: weight loss drug
Write out the Catecholamine receptor types
QISS: Alpha 1 (q), 2 (i), Beta 1 (s), 2 (s)
QIQ: Muscarinic 1 (q), M2 (i), M3 (q)
SI: Dopamine D1 (s), D2 (i)
QS:Histamine H1 (q), H2 (s)
QS: Vasopressin V1(q), V2(s)
Alpha Adrenergic, Muscarinic, and Dopamine 2 are all inhibitory
Histamine and Vasopressin 2 are stimulatory (no inhibitory)
Dopamine pathways (2) in schizophrenia Dopamine pathways (1) in parkinsons
Schizo: mesocortical, mesolimbic
PD: nigrostriatal
tyrosine hydroxylase deficiency causes what disease
rate limiting step for dopamine synthesis
Causes dopa responsive dystonia
D1 like what receptor
effect?
Like D5
Has excitatory effect in striatonigral pathway (caudate, putamen, nucleus accumbens)
D2 like what and what effect?
inhibitory in striatopallidal
like D3, D4
Pathophys of Parkinson’s Dz involving what Dopamine receptors / how?
decreased D1 (less excitatory) increased D2 (inhibitory) --> inhibition of movement
Antipsychotics effect which dopamine receptor system?
D2: blockade (because in schizophrenia there is increased D2 activity)
What are the causes of NMS and tardive dyskinesia?
Excess D2 blockade
Possible treatment of NMS? why effective? (3)
Bromocriptine to overcome D2 blockade
Bromocriptine is a D2>1 agonist
Ropinirole
Pramipexole: D2 agonists
Selegiline mechanism of action?
MAO-B inhibition
effect on DA degradation only
Function of alpha 2 adrenergic receptor
-name three drugs that act at this receptor
an auto/heteroreceptor for negative feedback. Ligand binding inhibits further NE release
1/2. Tenex/clonidine are alpha 2 agonists: decrease NE in synapse
3. Mirtazipine is an alpha 2 antagonist: leads to more NE in synapse
what is the mechanism of the disease Shy Drager syndrome / Multiple system atrophy?
alpha adrenergic degradation
-think alpha synucleinopathy / alpha adrenergic depletion
Cocaine mechanism of action?
NE/E reuptake inhibitor
describe NMDA rec properties
-what nt?
glutamate
- lets in Na, K, (Ca)
- blocked by Mg, so needs depolarization too: for learning
How do phencyclidine and Ketamine work?
Block NMDA (decrease glutamate)
Amnestic shellfish mechanism of action?
Kainate glutamate receptor agonist
chickpea toxicity / lathyrism
AMPA glutamate agonist
What is a treatment of ALS that causes inhibition of release of glutamate
Riluzole