CNS Flashcards
side effects of ethosuximide (4)
Ethosuximide causes Fatigue GI distress Headache Itchiness Stevens-Johnson syndrome
side effects of benzodiazepines (3)
- sedation
- dependence/tolerance
- respiratory depression (less than barbituates)
side effects of phenytoin (10)
- nystagmus, diplopia
- ataxia
- gingival hyperplasia
- hirsuitism
- megaloblastic anemia, peripheral neuropathy
- teratogen (fetal hydantoin syndrome)
- SLE-like syndrome
- cytochrome P-450 induction
- Stevens-Johnson syndrome
- osteopenia
side effects of carbamezapine (8)
- diplopia
- ataxia
- blood dyscrasia (agranulocytosis, aplastic anemia)
- liver toxicity
- teratogen
- cytochrome P-450 induction
- SIADH
- Stevens-Johnson syndrome
side effects of valproic acid (5)
- GI distress
- hepatotoxicity (measure LFTs)
- neural tube defects in fetus (DO NOT USE IN PREGNANCY)
- tremor
- weight gain
side effects of gabapentin (2)
- sedation
2. ataxia
side effects of phenobarbitol (4)
- sedation
- dependence/tolerance
- cytochrome P-450 induction
- cardiorespiratory depression
side effects of topiramate (4)
- sedation
- mental dulling
- kidney stones
- weight loss
side effects of lamotrigine (1)
- Stevens-Johnson syndrome
epilepsy drugs that cause Stevens-Johnson syndrome (4)
- ethosuximide
- phenytoin
- carbamezapine
- lamotrigine
epilepsy drugs that cause SIADH (1)
- carbamezapine
epilepsy drugs that cause kidney stones (1)
- topiramate
epilepsy drugs that cause SLE-like syndrome (1)
- phenytoin
first line tx absence seizures
ethosuximide
first line tx tonic-clonic seizures (3)
- phenytoin
- carbamezapine
- valproic acid
first line tx simple and complex seizures
carbamezapine
acute tx status epilepticus
benzodiazepines
prophylaxis of status epilepticus
phenytoin
first line tx seizure in neonate
phenobarbital
eclampsia seizures treatment
1st line: MgSO4
2nd line: benzodiazepines
treatment trigeminal neuralgia
carbamezapine
ethosuximide mechanism
blocks thalamic T-type Ca channels
benzodiazepines mechanism
increase GABA-A action
phenytoin mechanism
increase Na channel inactivation (zero-order kinetics)
carbamezapine mechanism
increase Na channel inactivation
valproic acid mechanism
increase Na channel inactivation
increase GABA concentration by inhibiting GABA transaminase
gabapentin mechanism
inhibits high-voltage-activated Ca channels
phenobarbital mechanism
increase GABA-A action
topiramate mechanism
blocks Na channels
increase GABA action
lamotrigine mechanism
blocks voltage-gated Na channels
what is levetiracetam used for?
epilepsy
tigabine mechanism
increase GABA by inhibiting reuptake
vigabatrin mechanism
increase GABA by inhibiting GABA transaminase
what epilepsy drugs cause megaloblastic anemia (1)
- phenytoin
what epilepsy drugs cause agranulocytosis and aplastic anemia (1)
- carbamezapine
what epilepsy drugs cause hepatotoxicity (2)
- carbamezapine
2. valproic acid
drug class phenobarbital
barbituate
drug class pentobarbital
barbituate
drug class thiopental
barbituate
drug class secobarbital
barbituate
barbituate mechanism
facilitate GABA-A action by increase duration of Cl channel opening
can you use barbituates in porphyria?
NO!
side effects of barbituates (4)
- respiratory/cardiovascular depression
- CNS depression (worse with EtOH)
- dependence
- induces cytochrome P-450
overdose tx for barbituates
supportive (maintain breathing and BP)
drug class diazepam
benzodiazepine
drug class lorazepam
benzodiazepine
drug class triazolam
benzodiazepine
drug class temazepam
benzodiazepine
drug class oxazepam
benzodiazepine
drug class midazolam
benzodiazepine
drug class chlordiazepoxide
benzodiazepine
drug class alprazolam
benzodiazepine
mechanism benzodiazepine
facilitate GABA-A action by increase frequency of Cl channel opening
short-acting (more addictive) benzodiazepines
TOM (triazolam, oxazepam, midazolam)
effect of benzodiazepines on sleep
decrease REM sleep
drugs that bind the GABA-A receptor (3)
- barbituates
- benzodiazepines
- EtOH
overdose tx of benzodiazepines
flumazenil (competitive antagonist GABA receptor)
drug class zolpidem
nonbenzodiazepine hypnotic
drug class zaleplon
nonbenzodiazepine hypnotic
drug class esopiclone
nonbenzodiazepine hypnotic
mechanism nonbenzodiazepine hypnotic
BZI subtype of GABA receptor
clinic use of nonbenzodiazepine hypnotic
insomnia
side effects of nonbenzodiazepine hypnotic (3)
- ataxia
- short duration b/c of liver metabolism
- lower risk dependence
anesthetics with less solubility in blood
rapid induction, rapid recovery
anesthetics with greater solubility in lipids
higher potency (1/MAC)
MAC (minimal alveolar concentration)
amount of inhaled anesthetic required to prevent 50% from moving
drug class halothane
inhaled anesthetic
drug class enflurane
inhaled anesthetic
drug class isoflurane
inhaled anesthetic
drug class sevoflurane
inhaled anesthetic
drug class methoxyflurane
inhaled anesthetic
drug class nitrous oxide
inhaled anesthetic
effects of inhaled anesthetics (4)
- myocardial depression
- respiratory depression
- nausea/vomiting
- increased cerebral blood flow
side effect of halothane (1)
- hepatotoxicity
side effect of methoxyflurane (1)
- nephrotoxicity
side effect of enflurane (1)
- seizures
what is malignant hyperthermia?
rare, hereditary. inhaled anesthetics and succinylcholine induce fever and muscle contractions
tx for malignant hyperthermia
dantrolene
what barbituate is used as IV anesthetic
thiopental (high potency, rapid entry and redistribution)
what benzodiazepine is used as an IV anesthetic
midazolam (for endoscopy)
side effects of midazolam anesthetic (3)
- postoperative respiratory depression
- decreased BP
- anterograde amnesia
mechanism of arylcyclohexylamines
PCP analogs, block NMDA receptors
what are arylcyclohexylamines
IV anesthetic
what is ketamine another name for?
arylcyclohexylamines
what opiates are used as IV anesthetic
morphine, fentanyl
what is propofol’s used in anesthesia
sedation in ICU, rapid induction
less postoperative nausea
propofol mechanism
potentiates GABA-A
what are the two groups of local anesthetics
- esters (procaine, cocaine, tetracaine)
2. amides (lidocaine, mepivacaine, bupivacaine)
mechanism local anesthetics
block Na channels (bind activated)
what happens to local anesthetics in infected tissue?
infected tissue = acidic –> alkaline anesthetics are charged, cannot penetrate –> need more
order of nerve blockade
small myelinated > small unmyelinated > large myelinated > large unmyelinated
order of loss of sensation
- pain, 2. temperature, 3. touch, 4. pressure
side effect of bupivacaine
cardiovascular toxicity
side effects of local anesthetics (3)
- CNS excitation
- hypertension
- hypotension
mechanism succinylcholine
ACh-receptor agonist –> prevents contraction
reversing succinylcholine blockade
Phase I (prolonged depolarization): none Phase II (repolarization but blocked): cholinesterase inhibitors
side effects of succinylcholine
- hypercalcemia
- hyperkalemia
- malignant hyperthermia
what neuromuscular blocking drug is depolarizing?
succinylcholine
what neuromuscular blocking drugs are non-depolarizing?
- tubocurarine
- atracurium
- mivacurium
- pancuronium
- vecuronium
- rocuronium
mechanism of non-depolarizing neuromuscular blocking drugs
competitive ACh antagonist
drug class tubocurarine
non-depolarizing neuromuscular blocking drugs
drug class atracurium
non-depolarizing neuromuscular blocking drugs
drug class mivacurium
non-depolarizing neuromuscular blocking drugs
drug class pancuronium
non-depolarizing neuromuscular blocking drugs
drug class vecuronium
non-depolarizing neuromuscular blocking drugs
drug class rocuronium
non-depolarizing neuromuscular blocking drugs
reversal of blockade from non-depolarizing neuromuscular blocking drugs (3)
- neostigmine (with atropine to prevent muscarinic effects like bradycardia)
- edrophonium
- other cholinesterase inhibitors
mechanism dantrolene
prevents release of Ca from sarcoplasmic reticulum
clinical use dantrolene
malignant hyperthermia and neuroleptic malignant syndrome
Parkinson’s drugs
Bromocriptine (or pramipexole or ropinirole)
Amantadine
L-dopa/carbidopa
Selegiline (or COMT inhibitors entacapone or tolcapone)
Antimuscarinic (benztropine)
tx essential tremor
beta-blocker
carbidopa mechanism
blocks peripheral decarboxylase –> increases L-dopa to brain and decreases peripheral side effects
side effects of L-dopa (2)
- arrhythmias
2. on-off phenomenon
selegiline mechanism
inhibits MAO-B –> increases dopamine
what is donepezil
AChE inhibitor used in Alzheimer’s
what is galantamine
AChE inhibitor used in Alzheimer’s
what is rivastigmine
AChE inhibitor used in Alzheimer’s
side effects of AChE inhibitors used in Alzheimer’s (3)
- nausea
- dizziness
- insomnia
what is memantine
NMDA receptor antagonist used in Alzheimer’s (prevents excitotoxicity)
memantine side effects (3)
- dizziness
- confusion
- hallucinations
what neurotransmitter changes are seen in Huntington’s (GABA, ACh, and dopamine)
decreased GABA, decreased ACh, increased dopamine
what is tetrabenazine
inhibits vesicular monoamine transporter (VMAT), used in Huntington’s
what is reserpine
inhibits vesicular monoamine transporter (VMAT), used in Huntington’s
sumatriptan mechanism
serotonin agonist, inhibits trigeminal nerve activation, induces vasoconstriction
clinical use of sumatriptan
migraine, cluster headache
side effect of sumatriptan
coronary vasospasm
what is butorphanol
mu partial agonist, kappa agonist
clinical use butorphanol
opioid, less respiratory depression
tramadol mechanism
weak opioid agonist, inhibits serotonin and NE reuptake
clinical use tramadol
chronic pain
side effects tramadol
- seizures
2. serotonin syndrome
drug class morphine
opioid (mu)
drug class fentanyl
opioid
drug class codeine
opioid
drug class loperamide
opioid (and diarrhea)
drug class methadone
opioid
drug class meperidine
opioid
drug class dextromethorphan
opioid (and cough suppression)
drug class diphenoxylate
opioid (and diarrhea)
side effects opioids
- respiratory depression
- addiction
- constipation
- miosis
opioid overdose tx
naloxone or naltrexone (opioid receptor antagonists)
alpha agonists used for glaucoma (2)
- epinephrine
2. brimonidine (alpha-2)
beta blockers used for glaucoma (3)
- timolol
- betaxolol
- carteolol
direct cholinomimetics used for glaucoma (2)
- pilocarpine
2. carbachol
indirect cholinomimetics used for glaucoma (2)
- physostigmine
2. echothiophate
cholinomimetics for glaucoma mechanism
constraction ciliary muscle –> increase outflow
which drugs should you not use in closed-angle glaucoma
alpha-agonists (epinephrine and brimonidine) –> cause mydriasis
prostaglandin used for glaucoma
latanoprost (PGF-2alpha)
latanoprost mechanism
increases outflow aqueous humor
which glaucoma treatment darkens the iris
latanoprost
what drug increases survival in ALS?
riluzole (decreases presynaptic glutamate release)