Kaplan CNS Pharm Flashcards by Nneka I

sedative-hypnotics: (barbituates and alcohol/benzos) reach a plateau in CNS depression

benzos (ceiling effect)

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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

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sedative-hypnotics: barbituates, alcohol, and benzos cause GABAa activation, increasing (Cl/K) INflux

Cl influx > membrane hyperpolarization

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sedative-hypnotics: barbituates, alcohol, and benzos cause GABAb activation, increasing (Cl/K) EFflux

K efflux > membrane hyperpolarization

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sedative-hypnotics: (barbituates/benzos): potentiate GABA, increase frequency of Cl channel opening, have no GABA mimetic activity

benzos

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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

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sedative-hypnotics: benzos (BZ1/BZ2) mediate sedation

BZ1

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sedative-hypnotics: benzos (BZ1/BZ2) mediate antianxiety and impairment of cognitive function

BZ2

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sedative-hypnotics: benzos (alprazolam/diazepam/lorazepam/midazolam/temazepam/oxazepam) are used for sleep disorders (2)

temazepam and oxazepam (because of half life)

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sedative-hypnotics: benzos (alprazolam/diazepam/lorazepam/midazolam/temazepam/oxazepam) are used for anxiety (3)

alprazolam, diazepam, lorazepam

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sedative-hypnotics: benzos used for preop sedation (lorazepam/midazolam): specifically used for status epilepticus (IV)

lorazepam (midazolam is for anesthesia IV)

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sedative-hypnotics: barbituates (phenobarbital/thiopental) used for seizures

phenobarbital

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sedative-hypnotics: barbituates (phenobarbital/thiopental) used for induction of anesthesia

thiopental

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sedative-hypnotics: barbituates are contraindicated in which special condition relating to metabolism in the liver

porphyria

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sedative-hypnotics: non BZ drugs zolpidem and zaleplon are BZ1 receptor agonists and are used in (anxiety/anesthesia/sleep disorders)

sleep disorders

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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

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sedative-hypnotics: (barbituate/benzo) overdose can be reversed with flumazenil

benzo. (barbituate overdose is CNS depression, there is no antidote)

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sedative-hypnotics: (benzos/barbituates/alcohols) all cause metabolic acidosis and CNS depression through GABA

alcohols

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anticonvulsants: (partial/general tonic clonic/general absence/status epilepticus) use valproic acid, phenytoin, carbamazepine, lamotrigine (2)

partial and general tonic clonic

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anticonvulsants: (partial/general tonic clonic/general absence/status epilepticus) use ethosuximide, valproic acid

general absence

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anticonvulsants: (partial/general tonic clonic/general absence/status epilepticus) use lorazepam, diazepam, phenytoin, fosphenytoin

status epilepticus

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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

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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

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anticonvulsants: ethosuximide blocks T type Ca channels in thalamic neurons and is used for (tonic clonic/absence) seizures.

absence!

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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

local anesthesia: (esters/amides) have two "i's" like lidocaine, bupivacaine, mepivacaine

amides

local anesthesia: nerve fibers most sensitive to blockade are of (larger/smaller) diameter and have (low/high) firing rates

smaller diameter, high firing rates. most sensitive are types B and C nerve fibers

skeletal muscle relaxants: (nondepolarizing/depolarizing) drugs are competitive of ACh

nondepolarizing

skeletal muscle relaxants: (nondepolarizing/depolarizing) drugs are noncompetitive of ACh

depolarizing

skeletal muscle relaxants: (nondepolarizing/depolarizing) drugs are nicotinic antagonists, reversible with AChE inhibitors

nondepolarizing

skeletal muscle relaxants: (nondepolarizing/depolarizing) D-tubocurarine prototype, progressive paralysis, no effects on cardiac and smooth muscle

nondepolarizing

skeletal muscle relaxants: (nondepolarizing/depolarizing) two phase mechanism, rapidly hydrolyzed (short duration), malignant hyperthermia is a concern

depolarizing

skeletal muscle relaxants: (nondepolarizing/depolarizing) example: succinylcholine

depolarizing

skeletal muscle relaxants: (nondepolarizing/depolarizing) examples: atracurium, mivacurium

nondepolarizing

skeletal muscle relaxants: (atracurium/mivacurium) is inactivated to laudanosine, which can cause seizures. Safe in hepatic or renal impairment

atracurium

skeletal muscle relaxants: (atracurium/mivacurium) has a very short duration

mivacurium

opioid analgesics: presynaptic and post synaptic inhibition through G (s/i) coupling

Gi coupling

opioid analgesics: three receptor families: mu, kappa, delta. which is most important to pharmacology?

opioid analgesics: what drug increases pain tolerance and decreases perception of pain? sedates, depresses respiration, increases vasodilation (therefore avoid in head trauma), causes constipation and cramping

morphine

opioid analgesics: full agonists: (meperidine/methadone/codeine) also antimuscarinic, does not constrict pupil, tachycardia, no GI spasm

meperidine

opioid analgesics: full agonists: (meperidine/methadone/codeine) used in maintenance of opiate addict

methadone

opioid analgesics: full agonists: (meperidine/methadone/codeine) cough suppressant, analgesia, used in combo with NSAIDs

codeine

opioid analgesics: mixed agonist/antagonists: nalbuphine and penazocine can result in (euphoria/dysphoria) via kappa receptor agonism. Also cause spinal analgesia

dysphoria (can help avoid addiction)

opioid analgesics: antagonists: (naloxone/naltrexone/methylnaltrexone): IV, reversal for respiratory depression

naloxone

opioid analgesics: antagonists: (naloxone/naltrexone/methylnaltrexone): PO, decrease craving for alcohol, used in opiate addiction

naltrexone

opioid analgesics: antagonists: (naloxone/naltrexone/methylnaltrexone): treatment of opioid-induced constipation (does not cross BBB and won't precipitate withdrawal)

methylnaltrexone

opioid analgesics: class triad of acute toxicity

pinpoint pupils, respiratory depression, coma (manage with naloxone)

opioid analgesics: tolerance occurs through receptor desensitization or downregulation, (increasing/decreasing) cAMP levels

increases cAMP levels, undoes Gi coupling, manage withdrawal with clonidine

Parkinson: restore normal DA and (increase/decrease) ACh activity at the muscarinic receptors in the striatum

decrease

Parkinson: (levodopa/tolcapone and entacapone) side effects: dyskinesias, on-off effects, psychosis, hypotension, vomiting

levodopa

Parkinson: (levodopa/tolcapone and entacapone) inhibit COMT

tolcapone and entacapone. COMT converts l-dopa to a partial agonist at DA receptors. these drugs enhance l-dopa efficacy

Parkinson: (tolcapone/entacapone) hepatotoxic

tolcapone

Parkinson: selegiline is a MAO (A/B) inhibitor, so it has no tyramine interactions. Initial Parkinson treatment, adjunt to l-dopa, metabolized to amphetamine

Parkinson: dopamine receptor agonists: (bromocriptine/pramipexole and ropinirole) use for hyperprolactinemia and acromegaly

bromocriptine

Parkinson: drugs (decreasing/increasing) ACh function: benztropine, trihexyphenidyl, diphenhydramine, which are muscarinic blockers

decreasing

Parkinson: amantadine is an antiviral which blocks muscarinic receptors and (increases/decreases) dopamine release

increases dopamine release

schizophrenia: mechanism of drugs: (agonize/block) DA and/or 5HT2 receptors

block!

schizophrenia: side effects from DA blockade include dyskinesias, endocrine dysfunction, (euphoria/dysphoria)

dysphoria (all the dys's!)

antipsychotics: (typicals/atypicals): chlopromazine, thioridazine, fluphenazine, haloperidol

typicals

antipsychotics: (typicals/atypicals): clozapine, olanzapine, risperidone, aripiprazole, quetiapine, ziprasidone

atypicals

depression: (MAO inhibitors/TCAs/SSRIs): phenelzine, tranylcypromine, high dose selegeline

MAOi

depression: (MAO inhibitors/TCAs/SSRIs): amitriptyline, imipramine, clomipramine

TCA

depression: TCA used for neuropathic pain (amitriptyline/imipramine/clomipramine)

amitriptyline

depression: TCA used for enuresis (amitriptyline/imipramine/clomipramine)

imipramine

depression: 3 C's of TCA toxicity

coma, convulsions, cardiotoxicity

depression: (MAO inhibitors/TCAs/SSRIs): fluoxetine, paroxetine, sertraline

SSRIs

depression: (MAO inhibitors/TCAs/SSRIs): citalopram, fluvoxamine

SSRIs

depression: bupropion blocks reuptake of which neurotransmitter

DA (used in smoking cessation)

depression: mirtazapine is a __ (receptor type) antagonist, associated with weight gain, used to treat anorexia

alpha 2 antagonist. increases NE synthesis and release

Bipolar disorder: Lithium (increases/decreases) cAMP

decreases

ADHD: (methylphenidate/atomoxetine): selective NE reuptake inhibitor, TCA side effects 3 C's

atomoxetine

ADHD: (methylphenidate/atomoxetine): amphetamine like, ritalin, side effects include agitation/restlessness

methylphenidate (need to use chronically, then taper off to prevent severe depression)

opioids: established clinical use of morphine: (management of GAD/relief of pain assoc with biliary colic/pulmonary congestion)

pulmonary congestion

opioids: patients taking fentanyl should also be taking what type of drug?

laxative/stool softener

irreversible MAO inhibitors (2)

tranylcypromine; phenelzine

MOAi SEs

- htn crisis (tyramine ingestion) - seratonin syndrome (SSRI/SNRI/tramadol intake) - hypotension (50%)

antidepressents; tramadol/fentanyl/meperedine; lithium; linezolid (MAOi antibiotic) – these drugs ppt what syndrome?

serotonin syndrome

compared to serotonin syndrome; NMS does not have these sx (2)

heperreflexia + ↑bowel sounds

onset w/i 24 hrs hyperreactivity (tremor, clonus, reflexes) tw benzos + cyrpoheptadine resolves w/i 24 hrs (seratonin syndrome/NMS)

serotinin syndrome (SS)

``` onset w/i days to weeks bradyreflexia + severe rigidity caused by dopamine antagonist tw bromocriptine resolves w/i days to weeks ```

NMS

5HT precursor; 5HT metabolite (after MAO digestion)?

tryptophan 5 OH-indole acetic acid (5HIAA) hint: 5hIAA index for serotonin

2 actions of amphetamines

1. ↓ DA/NE reuptake | 2. ↑DA/NE release

lows levels of 5 HIAA in frontal areas are assc with ___

completed suicide

___ treat pain transmission w/ or w/o depression; work at low doses; esp good for neuropathic pain *

TCAs hint: all TCAs are SNRIs

TCA with high antiH1 affinity to help with sleep (doxepin/amitriptyline/nortriptyline)

doxepin

TCA with high anti Ach affinity; also good for sleep (doxepin/amitriptyline/nortriptyline)

amitriptyline hint: nortriptyline = amitr metab (thf intermediate anti-ACh)