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neuropharm Flashcards

1
Q

benzoz

diazepam, lorazepam,triazolam, temazepam, omaxepam,midazolam, chlordiazepoxide,alprazolam

A

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

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2
Q

clinical use of benzos

A

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

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3
Q

adverse effects

A

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

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4
Q

barbiturates

phenibarbital ,pentibarbital ,thiopental ,secobarbital

A

facilitate GABA action by inc duration of cl channel opening thus dec neuron firing
sedative for anxiety seizures insomnia ,induction of anesthesia

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4
Q

barbiturates

phenibarbital ,pentobarbital ,thiopental ,secobarbital

A

facilitate GABA action by inc duration of cl channel opening thus dec neuron firing
sedative for anxiety seizures insomnia ,induction of anesthesia

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5
Q

adverse effects of barbiturates

A

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

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6
Q

insomnia therapy non benzo hypnotics

A

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

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7
Q

suvorexant ,ramelteon

A

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

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8
Q

sumatriptan

A

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

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9
Q

non ergot dopamine agonist

pramipexole ,ropinirole

A

toxicity nausea ,impulse control disorder,hypotension ,confusion ,
ergot, bromocriptine rarely used toxic

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10
Q

inc dopamine availability amantidine

A

inc dopamine release dec reuptake ,= peripheral edema ,livedo reticularis ,ataxia

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11
Q

inc L- dopa availability

A

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

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12
Q

prevent dopamine breakdown

A

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

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13
Q

curb excess cholinergic activity

A

benzotropine trihexyphenidyl ,improves tremor and rigidity no effect on bradykinesia

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14
Q

alzheimer disease

A 
donepezil ,rivastigmine 
galantamine 
ache inhibitor 
1st line treatment
n/dizziness
contraindicated in pts with cardiac conduction abnormalities
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15
Q

memantine

A 
nmda receptor antagonist 
helps prevent excitotoxicity 
used for moderate to advanced dementia 
a/e
dizziness,confusion hallucination
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16
Q

als

A

riluzole, dec neuron glutamate excitotoxicity

inc survival

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17
Q

huntington

A

tetrabenzine ,
inhibit vesicular ,monoamine transporter,vmat
dec dopamine vesicle packaging and release ,huntington chorea and tardive dyskinesia

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18
Q

desflurane,halothane,enflurane,isoflurane,sevoflurane,methoxyflurane,n20

A

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

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19
Q

malignant hyperthermia

A

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

20
Q

thiopental ,midazolam

A

facilitates gaba a barbiturate ,anesthesia induction ,short surgical procedures
dec cerebral blood flow ,high lipid solubility ,effect terminated by rapid redistribution into tissue ,fat

21
Q

propofol

A

potentiates gaba a rapid anesthesia induction ,short procedures ,icu sedation

21
Q

propofol

A

potentiates gaba a rapid anesthesia induction ,short procedures ,icu sedation

22
Q

ketamine

A

nmda recep antagonist ,dissociative anesthesia ,sympathomimetic ,inc hr inc bp
in cerebral blood flow ,emergence reaction ,possible with disorientation ,hallucination ,vivid dreams

23
Q

local anesthetics

A

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

23
Q

local anesthetics

A

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

24
Q

mechanism of local anesthetics

A

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

25
Q

local anesthetics

A

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

26
Q

depolarizing neuromuscular blocking agent

A

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

27
Q

nondepolarizing neuromusclar blocking drugs

A

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

28
Q

baclofen

A

gaba b receptor agonist in spinal cord
multiple spasticity ,dystonia ,multiple sclerosis
acts on the back (spinal cord)

29
Q

cyclobenzaprine

A

acts within the cns mainly brain stem
muscle spasticity
centrally acting ,structurally related to tcas may cause anticholinergic side effects ,sedation

30
Q

dantrolene

A

prevents release of ca from sarcoplasmic reticulum of skeletal muscle by inhibiting the ryanodine receptor
malignant hyperthermia
neuroleptic malignant syndrome

31
Q

tizanidine

A

a2 agonist acts centrally

muscle spasticity ,multiple sclerosis ,als cerebral palsy

31
Q

tizanidine

A

a2 agonist acts centrally

muscle spasticity ,multiple sclerosis ,als cerebral palsy

32
Q

opioid analgesics

A

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

33
Q

full agonist
partial agonist
mixed agonist antagonist
antagonist

A

morphine, heroin , meperidine ,methadone ,codeine ,fentanyl
bupernorphine
nalbuphine ,pentazocine ,butorphanol
naloxone ,nalterxone ,methylnatrexone

34
Q

clinical use of opiods

A

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

35
Q

adverse effects

A

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

36
Q

pentazocine

A

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

37
Q

butorphanol

A

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

38
Q

tramadol

A

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

39
Q

glaucoma b blockers

A

timolol betaxolol carteolol
dec aques humor synthesis
no pupillary or vision changes

40
Q

glaucoma b blockers

A

timolol betaxolol carteolol
dec aques humor synthesis
no pupillary or vision changes

41
Q

a agonist

A

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

41
Q

a agonist

A

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

42
Q

acetazolamide

A

dec aqueous humor synthesis via inhibition of carbonic anhydrase
no pupillary or vision changes

43
Q

prostaglandins

A

bimatoprost latanoprost pgf
inc aqueous humor via dec resistance of flow through uveoscleral pathway
darkens color of iris eyelash growth

44
Q

cholinomimetics m3

A

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

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