Neuropharm Flashcards
what secretes glutamate?
pyramidal cells
NMDA antagonists
ketamine, PCP
gaba a R are
ligand-gated
how does gaba open Cl- channel
binds to alpha subunit
benzos
bind to B subunit of GABA a
and either decrease GABA dissociation at low doses or directly open Cl- at high doses
Gaba b R
metabotropic
Gaba a R
ionotropi
when GABA binds to GABA b R..
K+ open–>closes Ca2+–>efflux K+ and decreases in Ca2+ conductance causes hyperpolarizaton of postsynaptic membrane
baclofen is an
agonist of Gaba b
Gaba c R
only have one subunit ionotropic Cl- channels retnal, spnal cord, pituitary **benzos, barbiturates, baclofen dont affect
2 types of Acetylcholine R
nicotinic- ionotropic
muscarinic- metabotropic
monoamines
one amino group that is connected to an aromatic ring by a 2 C chain
D1 family
D1, D5
–>increases adenylyl cyclase–> produces excitatory response
D2 family
D2, D3, D4
increases phosphodeisiterase–> produces inhibitory response
nigrostriatal pathway
parkinsons
mesolbic pathway
schizo, addiction
mesocortical pathway
schizophrenia
where is NE produced
locus coeruleus
caudal raphe nucleus
where si 5HT produced
raphe nucleus
CB1 R
inhibits GABA and glutmate release
anandamne
endogenous CB1 agonist; attenuates pain
anandamine agonist
THC
cannabdiol
CB2 R location
immune system
mechanisms of ant-epileptic drugs
Na+ channel blockade
Ca2+ channel blockade
GABA agonists
Glutamate antagonists
GABA agonists
barbiturates
benzos
topiramate
what type of Na+ channels do drugs block?
repetitive firing
drugs that act on Na+ channels
phenytoin carbamazepine valproate topiramate lamotrigine
glutamate antagonists
lamotrigine
topiramate
specific inducers of CY0450
phenobarbital ethosuximide phenytoin carbamazepine tobacco/cigs
specific inhibitors of CY0450
erythromycin Ca2+ channel blockers trimethoprim/sulfa fluconazole valproate
inducers, by def
increase clearance and decrease steady-state concentrations of other drugs
inhibitors, by def
decrease clearance and increase steady-state concentrations of other drugs
AED that may actually be synergistic
valproate + lamotrigine
only non-depressants/sedating
phenytoin
lamotrigine
neutral weight change
phenytoin
lamotrigine
levetiracetam
weight gain
carbamazepine
gabapentin
valproate
weight loss
topiramate
AED drugs implicated in osteoporosis
phenobarbital
phenytoin
carbamazepine
what AED do you give to pregant women?
lamotrigine
levetiracetam
topiramate causes
cleft palate defects
valproate causes
neural tube defects/learning disabilities
phenobarbitol mechansm
GABA agonist
phenobarbitol effective for
all seizures except abstinance
esp good for status epilepticus
phenytoin works for
all seizure types; better for focal or secondarily generalized than for primary generalized
phenytoin mechanism
blocks voltage-gated Na+ channel
phenytoin in children
poorly absorbed PO in children, so dont use
what supplements needed wth phenytoin
Ca, Vitamin D, vitamin K, folate
benzos are good for..and drug of choice for.
all seizure types
alcohol withdrawal symptoms
alcohol withdrawal seizures
why are benzos bad
tolerance develops rapidly
mech of benzo
GABA agonist
use of carbamazepine
excellent for focal and secondarily generalized seizures
less effective for prmary generalized
mood stabilizer bipolar
works for neuropathic and trigem neuralgia
carbamazepine mech
Na+ channel blockade
levels of carbamazepine increased by
Ca channel blockers, macrolide antibiotics
ethosuximide used for
only for absence seizures
mech of ethosuximdie
blocks t type Ca channels
valproate uses
all sezures, migranes, bipolar
valproate mech
not well understood
may block Na+ channels
probably also affects GABA levels, Ca2+ and K+ conductance
valproate is sometmes associated wth
elevated ammonia and carnitne deficiency
Gabapentin uses
partial and secondary generalized seizures (not prmary gen)
- good anxiolytic
- sedative
- anti-spasmodic
- peripheral neuropathy pain
gabapentin mech
increases GABA in brain
lamotrgene uses
broad spectrum efficacy aganst all seizure types
-also works for bipolar disorder, neuropathic pain
mech of lamotrigne
probs blocks release of glutamate presynaptically and blocks Na+ channels post-syn
lamotrigine is NOT
sedating
topramate uses
broad spectrum
not particularly good for absence
good for migrane
topiramate mech
Na+ channel blockade
GABA agonist
glutamate antagonist
topiramate is ONLY
an oral preparation
levetracetam use
broad spectrum of use for focal and generalized seizures
fav in hosps
levetiracetam mech
blocks ca2+ channels, interferes with action of SV2 protein which si necessary for exocytosis of NT vescles
levetiracetam toxicity
cognitive and behavioral problems
