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neuropharm Flashcards

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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

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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

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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

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A

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

21
Q

propofol

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A

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

22
Q

ketamine

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A

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

23
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
23
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
24
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
25
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
26
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
27
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
28
baclofen
gaba b receptor agonist in spinal cord multiple spasticity ,dystonia ,multiple sclerosis acts on the back (spinal cord)
29
cyclobenzaprine
acts within the cns mainly brain stem muscle spasticity centrally acting ,structurally related to tcas may cause anticholinergic side effects ,sedation
30
dantrolene
prevents release of ca from sarcoplasmic reticulum of skeletal muscle by inhibiting the ryanodine receptor malignant hyperthermia neuroleptic malignant syndrome
31
tizanidine
a2 agonist acts centrally | muscle spasticity ,multiple sclerosis ,als cerebral palsy
31
tizanidine
a2 agonist acts centrally | muscle spasticity ,multiple sclerosis ,als cerebral palsy
32
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
33
full agonist partial agonist mixed agonist antagonist antagonist
morphine, heroin , meperidine ,methadone ,codeine ,fentanyl bupernorphine nalbuphine ,pentazocine ,butorphanol naloxone ,nalterxone ,methylnatrexone
34
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
35
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
36
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
37
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
38
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
39
glaucoma b blockers
timolol betaxolol carteolol dec aques humor synthesis no pupillary or vision changes
40
glaucoma b blockers
timolol betaxolol carteolol dec aques humor synthesis no pupillary or vision changes
41
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
41
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
42
acetazolamide
dec aqueous humor synthesis via inhibition of carbonic anhydrase no pupillary or vision changes
43
prostaglandins
bimatoprost latanoprost pgf inc aqueous humor via dec resistance of flow through uveoscleral pathway darkens color of iris eyelash growth
44
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

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