neuropharm Flashcards
benzoz
diazepam, lorazepam,triazolam, temazepam, omaxepam,midazolam, chlordiazepoxide,alprazolam
mechanism:facilitates GABA action by inc frequency of cl channel opening , dec REM sleep,
most have long half lives and active metabolites ATOM
alprazolam triazolam oxazepam midazolam are short acting - higher additive potential
clinical use of benzos
anxiety ,panic disorder, spasticity , status eplipticus ,eclapmsia , detoxification ,night terrors ,sleep walking ,general anesthetic ,hypnotic ,lorazepam ,oxazepam, temazpam ,, can be used in those with liver disease who drink aLOT due to minimal first pass metabolism
adverse effects
dependance ,additive cns depression effects with alchohol and barbiturates ,less respiratory depression and coma than with barbiturates
treat over dose with flumazenil (competitive antagonist at GABA benzodiazepine receptor, can precipitate seizures by causing acute benzodiazpepine withdrawl
barbiturates
phenibarbital ,pentibarbital ,thiopental ,secobarbital
facilitate GABA action by inc duration of cl channel opening thus dec neuron firing
sedative for anxiety seizures insomnia ,induction of anesthesia
barbiturates
phenibarbital ,pentobarbital ,thiopental ,secobarbital
facilitate GABA action by inc duration of cl channel opening thus dec neuron firing
sedative for anxiety seizures insomnia ,induction of anesthesia
adverse effects of barbiturates
resp and cvs depression ,can be fatal ,cns depression,can be exacerbated by alchohol use , dependence, drug interactions ,induces cytochrome p450
overdose treatment is supportive, assist respiration and maintain bp
contraindicated in porphyria
insomnia therapy non benzo hypnotics
zolpidem ,zaleplon ,eszopiclone ,act via bz1 subtype of gaba receptor
a/e
ataxia, headaches ,confusion ,,casue only modest day after pyshcomotor depression and few amnestic effects ,vs older sedative hypnotics
short duration due to rapid metabolism by liver enzymes
effects reversed by flumazenil
dec dependency risk and sleep cycle disturbance
suvorexant ,ramelteon
orexin ,receptor antagonist ,cns depression ,headache,abnormal sleep related activities
contraindications: narcolepsy combination with strong cyp3a4 inhibitors
not recommended in pts with liver disease
limited risk
ramelteon ,melatonin recceptor agonist ,binds ,mlt1 and mlt2 in suprachiasmatic nuclues ,
dizziness ,nausea ,fatigue ,headache
no known risk of dependency
sumatriptan
5ht ib/id agonist
inhibit trigeminal nerve activation , prevent vasoactive peptide release ,induce vasoconstriction
acute migraine ,cluster headache attacks
coronary vasospasm
ce with pts with cad vasospastic angina ,mild paresthesia ,serotonin syndrome
non ergot dopamine agonist
pramipexole ,ropinirole
toxicity nausea ,impulse control disorder,hypotension ,confusion ,
ergot, bromocriptine rarely used toxic
inc dopamine availability amantidine
inc dopamine release dec reuptake ,= peripheral edema ,livedo reticularis ,ataxia
inc L- dopa availability
agents that prevent peripheral pre (bbb) l dopa degradation ,inc l dopa entering in cns ,inc central l dopa available for conversion into dopamine ,n/v
entacapone and tolcapone ,prevents peripheral l dopa degradation to 3-0-methyldopa by inhibiting comt ,used in conjugation with levodopa
prevent dopamine breakdown
agents that act centrally post bbb
selegiline ,rasagiline ,block conversion of dopamine to dopac by selectively inhibiting MAO-b
tolcapone ,crosses bbb and blocks conversion of dopamine to 3mt by inhibiting central comt
curb excess cholinergic activity
benzotropine trihexyphenidyl ,improves tremor and rigidity no effect on bradykinesia
alzheimer disease
donepezil ,rivastigmine galantamine ache inhibitor 1st line treatment n/dizziness contraindicated in pts with cardiac conduction abnormalities
memantine
nmda receptor antagonist helps prevent excitotoxicity used for moderate to advanced dementia a/e dizziness,confusion hallucination
als
riluzole, dec neuron glutamate excitotoxicity
inc survival
huntington
tetrabenzine ,
inhibit vesicular ,monoamine transporter,vmat
dec dopamine vesicle packaging and release ,huntington chorea and tardive dyskinesia
desflurane,halothane,enflurane,isoflurane,sevoflurane,methoxyflurane,n20
myocardial depression ,respiratory depression ,post op n/v ,cerebral blood flow inc, inc icp ,dec cerebral metabolic demand
hepatotoxicity ,halothane, nephrotoxicity methoxyflurane,proconvulsant,enflurane ,epliptogenic ,expansion of trapped gas in body cavity 3
malignant hyperthermia
rare lifethreatening condition in which inhaled anesthetics or succinylcholine induce severe muscle contractions and hyper thermia ,susceptibility is often inherited as autosomal dominant with variable penetrance ,mutations in ryanodine receptor cause inc ca release from sarcoplasmic reticulum
treatment dantrolene
thiopental ,midazolam
facilitates gaba a barbiturate ,anesthesia induction ,short surgical procedures
dec cerebral blood flow ,high lipid solubility ,effect terminated by rapid redistribution into tissue ,fat
propofol
potentiates gaba a rapid anesthesia induction ,short procedures ,icu sedation
propofol
potentiates gaba a rapid anesthesia induction ,short procedures ,icu sedation
ketamine
nmda recep antagonist ,dissociative anesthesia ,sympathomimetic ,inc hr inc bp
in cerebral blood flow ,emergence reaction ,possible with disorientation ,hallucination ,vivid dreams
local anesthetics
esters : procaine ,tetracaine ,benzocaine,chlorprocaine
amides : lidocaine , mepivacaine , bupivacaine ,ropivacaine ,prilocaine
mech , block neurotransmission via binding na gated channel on inner portion of channel along nerve fibers ,
most effectively in rapidly firing neurons ,3try amine local anesthetics penetrate membrane in uncharged form, then bind to ion channels as a charged form
local anesthetics
esters : procaine ,tetracaine ,benzocaine,chlorprocaine
amides : lidocaine , mepivacaine , bupivacaine ,ropivacaine ,prilocaine
mech , block neurotransmission via binding na gated channel on inner portion of channel along nerve fibers ,
most effectively in rapidly firing neurons ,3try amine local anesthetics penetrate membrane in uncharged form, then bind to ion channels as a charged form
mechanism of local anesthetics
block neurotransmission via binding to voltage gated na channel on inner portion ,most effective in rapidly firing neurons ,3ry amine local anesthetics penetrate membrane in uncharged form
in infected tissue alkaline anesthetics are charged and cannot penetrate tissue
local anesthetics
order of loss : pain ,temp ,touch ,pressure
minor surgical procedures ,spinal anesthesia ,touch pressure
cns excitation ,severe cvs toxicity bupivacine ,htn ,hypotension ,arrythmias cocaine ,methemoglobinemia benzocaine ,prilocaine
depolarizing neuromuscular blocking agent
succinylcholine ,strong ach recep agonist ,produces sustained depolarization and prevents muscle contraction
reversal of blockade
phase 1 prolonged depolarization
no antidote block potentiated by cholinestrase inhibitors
phase 2 repolarized but blocked ach recep are available but desensitized
maybe reversed by cholinestrase inhibitors
complication ,hyper calcemia ,hyperkalemia,malignant hyperthermia ,inc risk of prolonged muscle paralysis in pts with pseudocholinestrase deficiency
nondepolarizing neuromusclar blocking drugs
atracurium cistracurium ,pancuronium ,rocuronium, tubocurarine ,vecuronium ,ach antagonist
reversal of blockade , sugammadex or cholinesttrase inhibitors ,neostigmine ,edrophonium,
anticholinergics atropine ,glycopyrolate,are given with cholienestreasehibitors to prevent muscarinic effects
baclofen
gaba b receptor agonist in spinal cord
multiple spasticity ,dystonia ,multiple sclerosis
acts on the back (spinal cord)
cyclobenzaprine
acts within the cns mainly brain stem
muscle spasticity
centrally acting ,structurally related to tcas may cause anticholinergic side effects ,sedation
dantrolene
prevents release of ca from sarcoplasmic reticulum of skeletal muscle by inhibiting the ryanodine receptor
malignant hyperthermia
neuroleptic malignant syndrome
tizanidine
a2 agonist acts centrally
muscle spasticity ,multiple sclerosis ,als cerebral palsy
tizanidine
a2 agonist acts centrally
muscle spasticity ,multiple sclerosis ,als cerebral palsy
opioid analgesics
act as agonist at opioid recep to modulate synaptic transmission ,close presynaptic ca channels open post synaptic k channels dec synaptic transmission ,
inhibit release of ach ,nor epi , 5ht , glutamate ,substance p
full agonist
partial agonist
mixed agonist antagonist
antagonist
morphine, heroin , meperidine ,methadone ,codeine ,fentanyl
bupernorphine
nalbuphine ,pentazocine ,butorphanol
naloxone ,nalterxone ,methylnatrexone
clinical use of opiods
moderate to severe refractory pain ,diarrhea loperamide and diphenoxylate ,actue pulm edeme ,maintanince programs for opiate use disorder methadone buperenorphine ,nalaxone ,neoantal abstinence syndrome ,methadone ,morphine
adverse effects
n/v pruritis ,opiate use disorder resp depression ,constipation ,sphinter or oddi spasm miosis ,additive cns depression ,tolerance does not develop to miosis and constipation ,treat toxicity with naloxone competitive opioid recep antagonist and prevent relapse with naltrexone
pentazocine
k opoid recep agonist and m opioid recep weak antagonist ,
analgesia for moderate to severe pain
can cause opioid withdrawl symptoms if patients is also taking full opioid agonist due to competition
butorphanol
k opioid recep agonist and m opioid recep partial agonist severe pain migraine labor ,,causes less resp depression than full agonist use with full agonist to precipitate withdrawl
tramadol
very weak opoid agonsist also inhibits reuptake of norepi and seretonin
chronic pain
dec seizure threshold seretonin syndrome
slight opioid agonist and seretonin and norepi reuptake inhibitor
used for stubborn pain but can lower seizure threshold
and may cause seretonin syndrome
glaucoma b blockers
timolol betaxolol carteolol
dec aques humor synthesis
no pupillary or vision changes
glaucoma b blockers
timolol betaxolol carteolol
dec aques humor synthesis
no pupillary or vision changes
a agonist
epinephrine apraclonidine brimonidine
dec aqueuos humor synthesis via vasoconstriciton epi
dec humor synthesis apracolindine brimonidine
mydriasis do not use in closed angle glaucoma
blurry vision ocular hyperemia foreign body sensation
ocular allergic reactions occular pruritis
a agonist
epinephrine apraclonidine brimonidine
dec aqueuos humor synthesis via vasoconstriciton epi
dec humor synthesis apracolindine brimonidine
mydriasis do not use in closed angle glaucoma
blurry vision ocular hyperemia foreign body sensation
ocular allergic reactions occular pruritis
acetazolamide
dec aqueous humor synthesis via inhibition of carbonic anhydrase
no pupillary or vision changes
prostaglandins
bimatoprost latanoprost pgf
inc aqueous humor via dec resistance of flow through uveoscleral pathway
darkens color of iris eyelash growth
cholinomimetics m3
direct pilocarpine carbachol indirect physostigmine echotiophate
inc outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular meshwork
use pilocarpine in acute angle closure glaucoma
very effective at opening meshwork into canal of schlemm
miosis contraction of sphinter muscles and cyclospasm contraction of ciliary muscle
