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198 Cards in this Set
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glaucoma drugs:
5 categories |
alpha-agonists
beta-blockers diuretics cholinomimetics prostaglandin |
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alpha-agonists that rx glaucoma
|
epinephrine
brimonidine |
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epinephrine for glaucoma
mechanism? |
v aqueous humor synthesis
due to vasoconstriction |
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brimonidine mechanism
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v aqueous humor synthesis
|
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epinephrine s/e
|
mydriasis
stinging do not use in closed-angle glaucoma |
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beta glockers used for glaucoma
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timolol
betaxolol carteolol |
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timolol
betaxolol carteolol rx glaucoma mechanism? |
v aqueous humor secretion
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diuretics used for glaucoma
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acetazolamide
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acetazolamide rx for glaucoma mechanism?
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v aqueous humor secretion by
v HCO3- by inhibition of carbonic anhydrase |
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cholinomimetics used for glaucoma
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direct
--pilocarpine --carbachol indirect --physostigmine --echothiophate |
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cholinomimetics rx glaucoma
s/e |
miosis
cyclospasm |
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cholinomimetics rx glaucoma
mechanism |
^ outflow of aqueous humor
contract ciliary muscle and open trabecular meshwork |
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which cholinomimetic should be used for glaucoma emergencies?
why? |
pilocarpine
very effective at opening meshwork into canal of Schlemm |
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prostaglandins that rx glaucoma include
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latanoprost (PGF 2alpha)
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latanoprost mechanism
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^ outflow of aqueous humor
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latanoprost s/e
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darkens color of iris (browning)
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opioid analgesics include (7)
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heroin
morphine methadone meperidine dextromethorphan fentanyl codeine |
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opioid analgesics mechanism (3 + 2 + 5)
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agonists at opioid receptors
--mu --delta --kappa to open K+ channels close Ca++ channels --> v synaptic transmission - release of --ACh --NE --5-HT --glutamate --substance P |
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opioid receptors include
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mu = morphine
delta = enkephalin kappa = dynorphin |
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opioid analgesics general clinical use
|
pain
acute pulmonary edema |
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dextromethorphan clinical use
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cough suppression
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which opioid is used for cough suppression?
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dextromethorphan
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which opioid is used to rx diarrhea
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loperamide
diphenoxylate |
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loperamide and diphenoxylate are used to rx
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diarrhea
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opioid analgesics: toxicity
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addiction
respiratory depression constipation additive CNS depression miosis (pinpoint pupils) |
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tolerance does not develop to opioid effects _
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miosis
constipation |
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opioid toxicity is treated with
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naloxone
naltrexone |
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naloxone
naltrexone moa |
opioid receptor antagonists
|
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butorphanol moa
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partial agonist at mu
agonist at kappa |
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butorphanol rx
|
pain
|
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butorphanol advantage
s/e |
less respiratory depression than full agonists
causes withdrawl if pt is on full opioid agonist |
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tramadol moa
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very weak opioid agonist
-'s serotonin and NE reuptake |
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tramadol rx
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chronic pain
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tramadol s/e
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similar to opioids
v seizure threshold |
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all the glaucoma drugs
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alpha agonists
--epinephrine --brimonidine beta blockers --timolol betaxolol carteolol diuretics --acetazolamide cholinomimetics direct: --pilocarpine --carbachol indirect --physostigmine --echothiophate prostaglandins --latanoprost |
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latanoprost is __
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a prostaglandin
PGF 2alpha |
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all the epilepsy drugs
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phenytoin
carbamazepine lamotrigine gabapentin topiramate phenobarbital valproic acid ethosuximide benzodiazepines (diazepam, lorazepam) tiagabine vigabatrin levetiracetam |
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first-line for tonic-clonic
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phenytoin
carbamazepine valproic acid |
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first line for status epilepticus
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prophylaxis:
--phenytoin acute: --benzodiazepines |
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first line for absence seizures
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ethosuximide
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phenytoin is first line for _
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tonic clonic
prophylaxis for status epilepticus |
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carbamazepine is first line for _
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tonic clonic
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valproic acid is first-line for _
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tonic clonic
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ethosuximide is first-line for
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absence seizures
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benzodiazepines are first line for _ seizures
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acute status epilepticus
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what drugs treat absence seizures?
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valproic acid
ethosuximide * * = first-line |
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what drugs treat status epilepticus?
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phenytoin
--prophylaxis benzodiazepines (diazepam or lorazepam) --acute |
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what drugs treat tonic clonic seizures?
|
phenytoin *
carbamazepine * lamotrigine gabapentin topiramate phenobarbital valproic acid * levtiracetam |
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what drugs treat simple and complex seizures?
|
everybody except ethosuximide and benzodiazepines
phenytoin carbamazepine lamotrigine gabapentin topiramate phenobarbital valproic acid tiagabine vigabatrin levetiracetam |
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re: seizure table
phenytoin moa |
^ Na+ channel inactivation
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re: seizure table
carbamazepine moa |
^ Na+ channel inactivation
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re: seizure table
lamotrigine moa |
blocks voltage-gated Na+ channels
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re: seizure table
gabapentin moa |
designed as GABA analog
but primarily inhibits HVA (high voltage activated) Ca++ channels |
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re: seizure table
topiramate moa |
blocks Na+ channels
^ GABA action |
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re: seizure table
phenobarbital moa |
^ GABA-A action moa
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re: seizure table
valproic acid moa |
^ Na+ channel inactivation
^ GABA concentration |
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re: seizure table
ethosuximide moa |
blocks thalamic T-type Ca++ channels
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re: seizure table
benzodiazepines moa |
^ GABA-A action
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re: seizure table
tiagabine moa |
inhibits GABA reuptake
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re: seizure table
vigabatrin moa |
irreversibly inhibits GABA transaminase -->
^ GABA |
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re: seizure table
levetiracetam moa |
unknown;
may modulate GABA and glutamate release |
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re: seizure table
phenytoin "notes" |
fosphenytoin for parenteral use
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what seizure drug is also first line for trigeminal neuralgia?
|
carbamazepine
|
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carbamazepine is 1st line for
|
tonic clonic
trigeminal neuralgia |
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re: seizure table
gabapentin rx |
simple
complex tonic-clonic peripheral neuropathy bipolar |
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re: seizure table
lamotrigine rx |
simple
complex tonic-clonic |
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re: seizure table
carbamazepine rx |
simple
complex tonic-clonic* |
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re: seizure table
phenytoin rx |
simple
complex tonic-clonic* |
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re: seizure table
topiramate rx |
simple
complex tonic-clonic |
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re: seizure table
phenobarbital rx |
simple
complex tonic-clonic 1st line in pregnant women, children |
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re: seizure table
valproic acid rx |
simple
complex tonic-clonic* absence myoclonic seizures |
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re: seizure table
ethosuximide rx |
absence seizures
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re: seizure table
benzodiazepines rx |
1st line for acute status epilepticus
2nd-line for seizures of eclampsia |
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re: seizure table
tiagabine rx |
simple
complex |
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re: seizure table
vigabatrin rx |
simple
complex |
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re: seizure table
levetiracetam rx |
simple
complex tonic clonic |
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what rx seizures of eclampsia?
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1st-line: MgSO4
2nd-line: benzodiazepines |
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re: seizure table
_ rx myoclonic seizures |
valproic acid
|
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re: seizure table
_ is 1st line for trigeminal neuralgia |
carbamazepine
|
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re: seizure table
_ is used for peripheral neuropathy, bipolar disorder |
gabapentin
|
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re: seizure table
_ is 1st line in pregnant women, children |
phenobarbital
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epilepsy
benzodiazepines s/e |
STD (caught while having a seizure)
sedation tolerance dependence |
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epilepsy
carbamazepine s/e (9) |
diplopia
ataxia agranulocytosis aplastic anemia liver toxicity ^ P450 teratogenesis SIADH Stevens-Johnson |
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epilepsy
ethosuximide s/e (5) |
fucking give US head
fatigue GI distress urticaria Stevens-Johnson syndrome headache |
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epilepsy
phenobarbital s/e |
STD
^ P450 (Phenobarbital) sedation tolerance dependence |
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epilepsy
phenytoin s/e (10) |
nystagmus
diplopia ataxia sedation peripheral neuropathy gingival hyperplasia hirsutism megaloblastic anemia fetal hydantoin syndrome SLE-like syndrome ^ P450 |
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epilepsy
valproic acid s/e |
--weight gain
--GI distress --rare but fatal hepatotoxicity (measure LFTs) spina bifida -- ¡pregnancy! tremor |
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epilepsy
lamotrigine s/e |
Stevens-Johnson syndrome
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epilepsy
gabapentin s/e |
sedation
ataxia |
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epilepsy
topiramate s/e |
sedation
mental dulling kidney stones weight loss |
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stevens-johnson syndrome (7)
|
prodrome:
--malaise --fever followed by rapid onset of --erythematous --purpuric --macules @ GOO: oral, ocular, genital skin lesions progress to --epidermal necrosis --sloughing |
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how does phenytoin cause _ blood problem?
|
v folate absorption
--> megaloblastic anemia |
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barbiturates include
|
phenobarbital
pentobarbital thiopental secobarbital |
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barbiturates moa
|
^ duration of Cl- channel opening -->
facilitate GABA-A action --> v neuron firing |
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barbiturates clinical use
|
sedative for
anxiety seizures insomnia induction of anesthesia (thiopental) |
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barbiturates s/e
|
dependence
additive CNS depression w. EtOH respiratory or cardiovascular depression ( --> death ) ^ P450 |
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barbiturates contraindications
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porphyria
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treat overdose of barbiturates with
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assist respiration
^ BP |
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barbiturates vs.
benzodiazepines mechanism comparison |
both facilitate GABA-A action
----------------------------------- ^ duration of Cl- channel opening ^ frequency of Cl- channel opening |
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benzodiazepines moa
|
facilitate GABA-A action by
^ frequency of Cl- channel opening |
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sleep change by benzodiazepines
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v REM sleep
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pharmacokinetics of benzodiazepines
|
most have long half-lives
and active metabolites |
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benzos
clinical use |
anxiety
spasticity status epilepticus (lorazepam, diazepam) detoxification (especially alcohol withdrawl -- DTs) night terrors sleepwalking general anesthetic --amnesia --muscle relaxation hypnotic |
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hypnotics do _
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induce sleep
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benzodiazepines s/e
|
dependence
additive CNS depression with EtOH |
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s/e advantage of benzos against barbiturates
|
less:
respiratory depression coma |
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treat o/d of benzos with
|
flumazenil
|
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flumazenil moa
|
competitive antagonist at GABA benzodiazepine receptor
|
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short acting benzodiazepines include:
|
triazolam
oxazepam midazolam TOM |
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_ benzodiazepines have the highest ...
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short-acting benzos
highest addictive potential |
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GABA-A receptor is a _
|
ligand-gated chloride channel
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benzodiazepines include
|
diazepam
lorazepam temazepam chlordiazepoxide alprazolam triazolam oxazepam midazolam |
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nonbenzodiazepine hypnotics include
|
zolpidem
zaleplon eszopiclone |
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ambien is aka
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zolpidem
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nonbenzo hypnotics moa
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act by the BZ1 receptor subtype
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nonbenzo hypnotics are reversed by _
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flumazenil
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zolpidem is a (drug class)
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nonbenzo hypnotic
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zaleplon is a (drug class)
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nonbenzo hypnotic
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eszopiclone is a (drug class)
|
nonbenzo hypnotic
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nonbenzo hypnotics s/e (6)
|
"ACh"
ataxia confusion headaches unlike older sedative hypnotics, they cause --only modest day-after psychomotor depression --few amnestic effects --lower dependence risk than benzos |
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for a drug to penetrate the CNS it must be...
|
lipid soluble
or actively transported |
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drugs with v solubility in blood
--> |
rapid induction and recovery times
|
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drugs with ^ solubility in lipids
--> |
^ potency
= 1/MAC |
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MAC =
|
minimal alveolar concentration
at which 50% of the population is anesthetized varies with age |
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N2O solubilities
|
v blood solubility
v lipid solubility |
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halothane solubilities
|
^ blood solubility
^ lipid solubility |
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^ blood solubility of an anesthetic --> _ _ _ _
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slower onset of action
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inhaled anesthetics include
|
inmesh
isoflurane nitrous oxide methoxyflurane enflurane sevoflurane halothane |
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effects of inhaled anesthetics
|
myocardial depression
respiratory depression nausea/emesis ^ cerebral blood flow v cerebral metabolic demand |
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inhaled anesthetics
common s/e |
malignant hyperthermia (rare)
|
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halothane s/e
|
hepatotoxicity
|
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methoxyflurane s/e
|
nephrotoxicity
|
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enflurane s/e
|
proconvulsant
|
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nitrous oxide s/e
|
expansion of trapped gas
|
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IV anesthetics include
|
thiopental
midazolam ketamine morphine, fentanyl propofol |
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thiopental pharmacokinetics
|
high potency
high lipid solubility rapid entry into brain effect terminated by rapid redistribution into tissue and fat |
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thiopental clinical use
|
induction of anesthesia
short surgical procedures |
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thiopental s/e
|
v cerebral blood flow
|
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midazolam clinical use
|
most common drug used for endoscopy;
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midazolam may be used (as an IV anesthetic) adjunctively with _
|
gaseous anesthetics and narcotics
|
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midazolam s/e
|
severe postoperative respiratory depression
v BP amnesia |
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if midazolam overdose
--> v BP, treat it with _ |
flumazenil
|
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ketamine is a _ (drug class)
|
arylcyclohexylamine
|
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ketamine is a _ (~ drug type) and acts as a _ anesthetic
|
PCP analog
dissociative anesthetic |
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ketamine mechanism
|
blocks NMDA receptors
|
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ketamine s/e
|
cardiovascular stimulant
disorientation hallucination bad dreams ^ cerebral blood flow |
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_ IV anesthetic causes
^ cerebral blood flow _ IV anesthetic causes v cerebral blood flow |
ketamine
thiopental |
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morphine, fentanyl
as IV anesthetics they're used as... |
used with other CNS depressants
during general anesthesia |
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propofol clinical use
|
rapid anesthesia induction
short procedures |
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propofol s/e
|
less postoperative nausea than thiopental
|
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propofol moa
|
potentiates GABA-A
|
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ester local anesthetics include
|
procaine
cocaine tetracaine |
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amide local anesthetics include
|
lidocaine
mepivacaine bupivacaine |
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depolarizing neuromuscular blocking drugs include
|
succinylcholine
|
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nondepolarizing neuromuscular blocking drugs include
|
don't TAMPR with her V...
tubucurarine atracurium mivacurium pancuronium rocuronium vecuronium |
|
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succinylcholine s/e
|
hypercalcemia
hyperkalemia |
|
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neuromuscular blocking drugs
use |
muscle paralysis in
surgery mechanical ventilation |
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neuromuscular blocking drugs are selective for _ receptor
|
*motor* nicotinic receptor
|
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succinylcholine blockade phase I vs. phase II
the nature of the block |
prolonged depolarization
repolarized but blocked |
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succinylcholine blockade:
phase I reversal of blockade |
no antidote
block potentiated by cholinesterase inhibitors |
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succinylcholine blockade:
phase II reversal of blockade |
antidote: cholinesterase inhibitors
e.g. neostigmine |
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cholinesterase inhibitors effect on succinylcholine block
|
potentiates phase I of block
antidote for phase II |
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nondepolarizing neuromuscular blockers moa
|
compete with ACh
|
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reversal of tubocurarine &c block
|
cholinesterase inhibitors e.g.
neostigmine edrophonium |
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_ used to rx malignant hyperthermia
|
dantrolene
|
|
|
dantrolene moa
|
prevents release of Ca++
from SR of skeletal muscle |
|
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dantrolene rx
|
malignant hyperthermia
neuroleptic malignant syndrome |
|
|
neuroleptic malignant syndrome is a s/e of _
|
antipsychotics
|
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malignant hyperthermia is caused by _
|
inhalation anesthetics
(except N2O) succinylcholine |
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|
parkinsonism is due to _ _
(neurochemical gist) |
loss of dopaminergic neurons
excess cholinergic activity |
|
|
parkinson's drugs
4 strategies |
agonize dopamine receptors
^ dopamine prevent dopamine breakdown curb excess cholinergic activity |
|
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parkinson's drugs that agonize dopamine receptors include
|
bromocriptine
pramipexole ropinirole |
|
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parkinson's drugs that ^ dopamine include
|
amantadine
L-dopa/carbidopa |
|
|
amantadine is an antiviral against influenza A and _
|
rubella
|
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parkinson's drugs that prevent dopamine breakdown
|
selegiline
entacapone tolcapone |
|
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entacapone
tolcapone moa |
COMT inhibitors
prevent L-dopa degradation --> ^ dopamine availability |
|
|
COMT inhibitors used to treat parkinson's
|
entacapone
tolcapone |
|
|
parkinson's drugs that curb excess cholinergic activity
|
benztropine
|
|
|
what symptoms of parkinson's does benztropine treat or not treat?
|
improves tremor, rigidity
little effect on bradykinezia |
|
|
levodopa/carbidopa moa
|
^ dopamine
unlike dopamine, L-dopa can cross BBB L-dopa is converted by dopa decarboxylase in the CNS to dopamine |
|
|
L-dopa/carbidopa rx
|
parkinsonism
|
|
|
L-dopa/carbidopa s/e
|
arrhythmias from peripheral conversion to dopamine
long-term use can --> dyskinesia following administration akinesia between doses |
|
|
carbidopa moa
|
a peripheral decarboxylase inhibitor
given with L-dopa to limit peripheral conversion of L-dopa to dopamine |
|
|
selegiline moa
|
selectively inhibits MAO-B
(which preferentially metabolizes dopamine over NE and 5-HT) thereby increasing the availability of dopamine |
|
|
selegiline rx
|
adjunctive agent to L-dopa
to treat parkinson's |
|
|
selegiline s/e
|
may enhance adverse effects of L-dopa
|
|
|
alzheimer's drugs include
|
memantine
donepezil galantamine rivastigmine |
|
|
memantine moa
|
NMDA receptor antagonist
helps prevent excitotoxicity (mediated by Ca++) |
|
|
memantine s/e
|
dizziness
confusion hallucinations |
|
|
donepezil
galantamine rivastigmine moa |
acetylcholinesterase inhibitors
|
|
|
donepezil
galantamine rivastigmine s/e |
nausea
dizziness insomnia |
|
|
huntington's disease:
what chemical ^ v are there? |
^ dopamine
v GABA + ACh |
|
|
huntington's:
drugs to rx |
reserpine + tetrabenazine
haloperidol |
|
|
reserpine + tetrabenazine moa
|
"amine depleting"
used to treat huntington's |
|
|
haloperidol moa _ _
|
dopamine receptor antagonist
|
|
|
sumatriptan moa
|
5-HT (1B/1D) agonist
--vasoconstriction inhibition of --trigeminal activation and --vasoactive peptide release |
|
|
sumatriptan rx
|
acute migraine
cluster headache attacks |
|
|
sumatriptan s/e
|
coronary vasospasm
¡ in CAD or Prinzmetal's ! mild tingling |
