Kaplan CNS Pharm Flashcards
sedative-hypnotics: (barbituates and alcohol/benzos) reach a plateau in CNS depression
benzos (ceiling effect)
sedative-hypnotics: barbituates, alcohol, and benzos bind to which part of the 5 subunit GABAa complex (GABA binding site/other binding sites)
they have their own binding sites
sedative-hypnotics: barbituates, alcohol, and benzos cause GABAa activation, increasing (Cl/K) INflux
Cl influx > membrane hyperpolarization
sedative-hypnotics: barbituates, alcohol, and benzos cause GABAb activation, increasing (Cl/K) EFflux
K efflux > membrane hyperpolarization
sedative-hypnotics: (barbituates/benzos): potentiate GABA, increase frequency of Cl channel opening, have no GABA mimetic activity
benzos
sedative-hypnotics: (barbituates/benzos): prolong GABA activity, increase duration of Cl channel opening, have GABA mimetic activity at high doses, also inhibit complex I of ETC
barbituates
sedative-hypnotics: benzos (BZ1/BZ2) mediate sedation
BZ1
sedative-hypnotics: benzos (BZ1/BZ2) mediate antianxiety and impairment of cognitive function
BZ2
sedative-hypnotics: benzos (alprazolam/diazepam/lorazepam/midazolam/temazepam/oxazepam) are used for sleep disorders (2)
temazepam and oxazepam (because of half life)
sedative-hypnotics: benzos (alprazolam/diazepam/lorazepam/midazolam/temazepam/oxazepam) are used for anxiety (3)
alprazolam, diazepam, lorazepam
sedative-hypnotics: benzos used for preop sedation (lorazepam/midazolam): specifically used for status epilepticus (IV)
lorazepam (midazolam is for anesthesia IV)
sedative-hypnotics: barbituates (phenobarbital/thiopental) used for seizures
phenobarbital
sedative-hypnotics: barbituates (phenobarbital/thiopental) used for induction of anesthesia
thiopental
sedative-hypnotics: barbituates are contraindicated in which special condition relating to metabolism in the liver
porphyria
sedative-hypnotics: non BZ drugs zolpidem and zaleplon are BZ1 receptor agonists and are used in (anxiety/anesthesia/sleep disorders)
sleep disorders
sedative-hypnotics: non BZ drug buspirone has no effect on GABA, is a 5HT1A partial agonist. Used in (anxiety/anesthesia/sleep disorders)
generalized anxiety disorders
sedative-hypnotics: (barbituate/benzo) overdose can be reversed with flumazenil
benzo. (barbituate overdose is CNS depression, there is no antidote)
sedative-hypnotics: (benzos/barbituates/alcohols) all cause metabolic acidosis and CNS depression through GABA
alcohols
anticonvulsants: (partial/general tonic clonic/general absence/status epilepticus) use valproic acid, phenytoin, carbamazepine, lamotrigine (2)
partial and general tonic clonic
anticonvulsants: (partial/general tonic clonic/general absence/status epilepticus) use ethosuximide, valproic acid
general absence
anticonvulsants: (partial/general tonic clonic/general absence/status epilepticus) use lorazepam, diazepam, phenytoin, fosphenytoin
status epilepticus
anticonvulsants: Phenytoin and carbamazepine both block axonal Na channels in their inactivated state and cannot be used in absence seizures. Only (phenytoin/carbamazepine) can be used for bipolar disorder and causes exfoliative dermatitis
carbamazepine. also causes increased ADH secretion
anticonvulsants: (phenytoin/valproic acid) inhibits GABA transaminase and blocks T type Ca channels. Use in seizure states, mania of bipolar disorders, and migraine prophylaxis
valproic acid
anticonvulsants: ethosuximide blocks T type Ca channels in thalamic neurons and is used for (tonic clonic/absence) seizures.
absence!
anticonvulsants: abrupt withdrawal may result in what life threatening effect
may precipitate seizures
anticonvulsants: felbamate and lamotrigine block Na channels and glutamate receptors. Used in seizure states. (felbamate/lamotrigine) side effect is hepatotoxicity and aplastic anemia
felbamate
anticonvulsants: felbamate and lamotrigine block Na channels and glutamate receptors. Used in seizure states. (felbamate/lamotrigine) side effect is Stevens-Johnson syndrome (dermatitis)
lamotrigine
general anesthesia: (protein bound/free form) in blood
protein bound in blood. must cross the BBB to reach CNS, where it is in the free and lipid soluble form
general anesthesia: inhalants: (nitrous oxide/halothane) rapid onset and recovery, very high MAC value, very low blood-gas ratio, minimal side effects
nitrous oxide. high MAC means low potency. low blood-gas ratio means acts quickly. can result in spontaneous abortions
general anesthesia: inhalants: (nitrous oxide/halothane) family: fluranes like desflurane, sevoflurane
halothane
general anesthesia: inhalants: (nitrous oxide/halothane) low MAC, high blood-gas ratio, can result in malignant hyperthermia
halothane (high potency, takes time to act)
general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): barbituate used for induction of anesthesia, rapid onset and short acting
thiopental. short acting due to redistribution (to fat–lipid soluble)
general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): benzo used for preop sedation, anterograde amnesia, induction. depresses respiratory function
midazolam
general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): looks like MILK. used for induction and maintenance of anesthesia, ANTIEMETIC, CNS and cardiac depressant
propofol
general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): opiate used for induction and maintenance of anesthesia, central analgesic
fentanyl
general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): dissociative anesthetic, hallucinogen, NMDA receptor antagonist, increased intracranial pressure
ketamine
local anesthesia: (ionized/nonionized) form crosses axonal membrane, then (nonionized/ionized) form blocks the inactivated Na channel from within
nonionized form crosses axonal membrane.
ionized form blocks channel
local anesthesia: (esters/amides) metabolized by plasma and tissue esterases
esters
local anesthesia: (esters/amides) metabolized by liver amidases
amides
local anesthesia: (esters/amides) have one “i” like procaine, cocaine, benzocaine
esters