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Pharm 2018-2019 > Kaplan CNS Pharmacology Chapter (includes convulsants) - Unit 3 > Flashcards

Kaplan CNS Pharmacology Chapter (includes convulsants) - Unit 3 Flashcards

1
Q

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

A

benzos (ceiling effect)

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2
Q

sedative-hypnotics: barbituates, alcohol, and benzos bind to which part of the 5 subunit GABAa complex (GABA binding site/other binding sites)

A

they have their own binding sites

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3
Q

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

A

Cl influx > membrane hyperpolarization

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4
Q

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

A

K efflux > membrane hyperpolarization

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5
Q

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

A

benzos

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6
Q

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

A

barbituates

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7
Q

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

A

BZ1

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8
Q

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

A

BZ2

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9
Q

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

A

temazepam and oxazepam (because of half life)

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10
Q

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

A

alprazolam, diazepam, lorazepam

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11
Q

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

A

lorazepam (midazolam is for anesthesia IV)

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12
Q

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

A

phenobarbital

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13
Q

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

A

thiopental

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14
Q

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

A

porphyria

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15
Q

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

A

sleep disorders

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16
Q

sedative-hypnotics: non BZ drug buspirone has no effect on GABA, is a 5HT1A partial agonist. Used in (anxiety/anesthesia/sleep disorders)

A

generalized anxiety disorders

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17
Q

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

A

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

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18
Q

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

A

alcohols

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19
Q

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

A

partial and general tonic clonic

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20
Q

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

A

general absence

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21
Q

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

A

status epilepticus

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22
Q

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

A

carbamazepine. also causes increased ADH secretion

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23
Q

anticonvulsants: (phenytoin/valproic acid) inhibits GABA transaminase and blocks T type Ca channels. Use in seizure states, mania of bipolar disorders, and migraine prophylaxis

A

valproic acid

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24
Q

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

A

absence!

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25
Q

anticonvulsants: abrupt withdrawal may result in what life threatening effect

A

may precipitate seizures

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26
Q

anticonvulsants: felbamate and lamotrigine block Na channels and glutamate receptors. Used in seizure states. (felbamate/lamotrigine) side effect is hepatotoxicity and aplastic anemia

A

felbamate

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27
Q

anticonvulsants: felbamate and lamotrigine block Na channels and glutamate receptors. Used in seizure states. (felbamate/lamotrigine) side effect is Stevens-Johnson syndrome (dermatitis)

A

lamotrigine

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28
Q

general anesthesia: (protein bound/free form) in blood

A

protein bound in blood. must cross the BBB to reach CNS, where it is in the free and lipid soluble form

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29
Q

general anesthesia: inhalants: (nitrous oxide/halothane) rapid onset and recovery, very high MAC value, very low blood-gas ratio, minimal side effects

A

nitrous oxide. high MAC means low potency. low blood-gas ratio means acts quickly. can result in spontaneous abortions

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30
Q

general anesthesia: inhalants: (nitrous oxide/halothane) family: fluranes like desflurane, sevoflurane

A

halothane

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31
Q

general anesthesia: inhalants: (nitrous oxide/halothane) low MAC, high blood-gas ratio, can result in malignant hyperthermia

A

halothane (high potency, takes time to act)

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32
Q

general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): barbituate used for induction of anesthesia, rapid onset and short acting

A

thiopental. short acting due to redistribution (to fat–lipid soluble)

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33
Q

general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): benzo used for preop sedation, anterograde amnesia, induction. depresses respiratory function

A

midazolam

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34
Q

general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): looks like MILK. used for induction and maintenance of anesthesia, ANTIEMETIC, CNS and cardiac depressant

A

propofol

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35
Q

general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): opiate used for induction and maintenance of anesthesia, central analgesic

A

fentanyl

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36
Q

general anesthesia: IV: (thiopental/midazolam/propofol/fentanyl/ketamine): dissociative anesthetic, hallucinogen, NMDA receptor antagonist, increased intracranial pressure

A

ketamine

37
Q

local anesthesia: (ionized/nonionized) form crosses axonal membrane, then (nonionized/ionized) form blocks the inactivated Na channel from within

A

nonionized form crosses axonal membrane.

ionized form blocks channel

38
Q

local anesthesia: (esters/amides) metabolized by plasma and tissue esterases

A

esters

39
Q

local anesthesia: (esters/amides) metabolized by liver amidases

A

amides

40
Q

local anesthesia: (esters/amides) have one “i” like procaine, cocaine, benzocaine

A

esters

41
Q

local anesthesia: (esters/amides) have two “i’s” like lidocaine, bupivacaine, mepivacaine

A

amides

42
Q

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

A

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

43
Q

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

A

nondepolarizing

44
Q

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

A

depolarizing

45
Q

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

A

nondepolarizing

46
Q

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

A

nondepolarizing

47
Q

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

A

depolarizing

48
Q

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

A

depolarizing

49
Q

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

A

nondepolarizing

50
Q

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

A

atracurium

51
Q

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

A

mivacurium

52
Q

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

A

Gi coupling

53
Q

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

A

mu

54
Q

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

A

morphine

55
Q

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

A

meperidine

56
Q

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

A

methadone

57
Q

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

A

codeine

58
Q

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

A

dysphoria (can help avoid addiction)

59
Q

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

A

naloxone

60
Q

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

A

naltrexone

61
Q

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

A

methylnaltrexone

62
Q

opioid analgesics: class triad of acute toxicity

A

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

63
Q

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

A

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

64
Q

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

A

decrease

65
Q

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

A

levodopa

66
Q

Parkinson: (levodopa/tolcapone and entacapone) inhibit COMT

A

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

67
Q

Parkinson: (tolcapone/entacapone) hepatotoxic

A

tolcapone

68
Q

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

A

B

69
Q

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

A

bromocriptine

70
Q

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

A

decreasing

71
Q

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

A

increases dopamine release

72
Q

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

A

block!

73
Q

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

A

dysphoria (all the dys’s!)

74
Q

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

A

typicals

75
Q

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

A

atypicals

76
Q

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

A

MAOi

77
Q

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

A

TCA

78
Q

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

A

amitriptyline

79
Q

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

A

imipramine

80
Q

depression: 3 C’s of TCA toxicity

A

coma, convulsions, cardiotoxicity

81
Q

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

A

SSRIs

82
Q

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

A

SSRIs

83
Q

depression: bupropion blocks reuptake of which neurotransmitter

A

DA (used in smoking cessation)

84
Q

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

A

alpha 2 antagonist. increases NE synthesis and release

85
Q

Bipolar disorder: Lithium (increases/decreases) cAMP

A

decreases

86
Q

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

A

atomoxetine

87
Q

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

A

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

88
Q

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

A

pulmonary congestion

89
Q

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

A

laxative/stool softener

Pharm 2018-2019 (7 decks)

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