Neuro drugs 2 Flashcards
contrast the MOA of barbs and benzos
Barbs - inc duration of Cl channel opening -dec neuron firing
benzos - inc frequency of Cl - channel firing
both facilitate GABA action
What else binds the GABAa receptor
ETOH - can exacerbate effects of barbs only
benzos are used as competitive inhibitor of ETOH for detox
What are the only short acting Benzos, what are the risks of using them
ATOM - short fuse
Alprazolam
triazolam
oxazepam
midazolam
higher addictive potential
What is used in overdose of benzos
flumazenil
Name the three nonbenzo hypnotics used for insomnia
zolpidem
zaleplon
eszopiclone
ZZZzzZzs
What are some of the long acting benzos? why are they used and what are their risks
diazepam, flurazepam, chlordiazepoxide
less addictive potential, but inc risk of falling in elderly
MOA of nonbenzo hypnotics
bind BZ1 GABA
Describe the relationship of potency and induction time
inc potency, slow induction
dec solubility in the blood = low potency = fast induction
What are the inhaled anesthetics
“fluranes” + halothane + N20
what effects do the inhaled anesthetics have
cardioresp depression
inc cerebral blood flow
What is malignant hyperthermia and what causes it
inhaled anesthetics besides N20, succinylcholine
fever, severe muscle contractions - inherited defect of ryanodine receptor
what is the treatment for malignant hyperthermia , how does it work
dantrolene - blocks ca release from SR of skeletal muscle
which Barb is used for IV anesthetic, what is its use
thiopental
induction and short surgical procedures
What benzo is used for IV anesthetic, what is its most common use
midazolam
most common drug for endoscopy
Name the PCP analog that causes dissociative anesthesia, hallucinations and bad dreams
ketamine
What drug is used for sedation in ICU and for rapid anesthesia, how is it different than thipental
propofol - less post op nausea
What are the local anesthetics
esters: procaine, cocaine, tetracaine
amides: lidocaine, mepivacaine, bupivacine - 2 Is
how do the local anesthetics work
bind to activated Na+ channels and block them
In infected tissue how should you change the use of local anesthetics?
need to inc dose - acidic envt - cant penetrate
Describe the order of nerve blockade
small before large
myelinated before unmyelinated
**small takes precedence (so small umyelinated first to go)
- pain
- temp - preg people get cold
- touch
- pressure -why in giving birth this is the worstq
What local anesthetic can cause methemoglobinemia
benzocaine
what drug is a depolarizing NM blocker
succinylcholine
how do you reverse succinylcholine
phase 1 - cant do anything
phase 2 - use cholinesterase blockers
What are the nondepolarizing NM blockers, how do they work?
“curares”
competitive inhibitors of Ach
how do you reverse nondepolarizing NM blockade
neostigmine
need to give with atropine to prevent bradycardia
baclofen MOA and use
inhibits GABAb at spinal cord level - induces skeletal muscle relaxation - for muscle spasms
cyclobenzaprine MOA and use
central acting skeletal muscle relaxant - also for muscle spasms
what are the s/e of cyclobenzaprine
similar to TCAs
“cyclo”
What are the 5 main parkinson drugs and MOA
BALSA
bromoscriptine - dopamine agonist
amantadine - inc dopamine release and dec uptake
levodopa/ carbidopa - inhibits DOPA decarboxylase
Selegiline - blocks MAOB
Antimuscarinic = benztropine
what is amantadine also used for
antiviral for influenza
What are the COMT inhibitors
central - tolcapone
peripheral - entacapone and tolcapone
What are other dopamine agonists besides bromoscriptine
pramipexole and ropinrole - actually preferred because they are non-ergots
Fill in this sentence: unlike dopamine, LDOPA can ____
cross the BBB and is converted by dopa decarboxylase in the CNS to dopamine
why is carbidopa given with Ldopa
peripheral DOPA decarboxylase inhibitor - inc bioavailability and dec peripheral s/e
what are the s/e of L dopa
arrythmias from inc peripheral formation of catecholamines
can lead to dyskinesia
what are the two types of alzheimer drugs
- memantine - think memory
2. AchE inhibitors - donepezil, galantamine, rivastigmine, tacrine
MOA of memantine
NMDA antagonist = prevents excitotoxicity
what are the NT changes in
- parkinsons
- huntingtons
- parkinsons: dec D2, inc Ach
2. huntingtons: dec GABA, dec Ach, inc dopamine
What are the three main drugs for huntingtons, MOA?
tetrabenzine and reserpine inhibit VMAT - dec D2 release
haloperidol - D2 antagonist
MOA of sumatriptans and use
5HT 1b/d agonists - inhibit Trigem activation , induce vasoconstriction
used for acute migraines and cluster headache attacks
when are sumatriptans contraindicated
CAD or prinzmental angina
adding carbidopa to levodopa regimen can decrease what s/e
- tachyarrythmias
- postural hypotension
- nausea and vomiting
DOES NOT decrease anxiety and agitation effect
