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shelf pharm > CNS drugs > Flashcards

CNS drugs Flashcards

1
Q

what do all GABAnergic drugs cause as a preliminary response

A

paradoxical disinhibition

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2
Q

what does GABAa activation cause

A

increased chloride entry into the cell. this results in membrane hyperpolarization

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3
Q

what do benzodiazepams do to GABA channels

A

they potentiate GABA. shifts the dose-response to the left. a smaller dose has the same effect. they just increase the frequency of opening the channel.

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4
Q

do benzos have GABAnergic activity

A

no they dont.

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5
Q

what does BZ1 mediate

A

sedation

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6
Q

what does BZ2 mediate

A

cognitive effect. mediates anxiety and impairment. anterograde amnesia.

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7
Q

what is alprazolam used for and why

A

anxiety, panic, phobias. long half-life

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8
Q

what is diazepam used for and why

A

anxiety, preop sedation, muscle relaxation, withdrawal. log half-life

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9
Q

what is lorazepam used for

A

anxiety, preop sedation, statis epilepticus. long half-life

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10
Q

what is midazolam used for

A

preop anesthesia. ultra short half-life

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11
Q

what is temazepam used for

A

sleep disorders. short half life

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12
Q

what is oxazepam

A

sleep disorders and anxiety

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13
Q

barbiturates mechanism

A

prolong the GABA activity. increase the duration of chloride opening. greater hyperpolarization.

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14
Q

are barbs GABAnergic

A

yes. they will open the channels by themselves. they have their own receptors.

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15
Q

what else do the barbs do?

A

inhibit complex I of the electron transport chain. through this mechanism they can cause irreversible toxicity

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16
Q

what are the barbs contraindicated in

A

porphyrias. this occurs because the barbs increase P450’s and all P450s have heme.

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17
Q

is there cross-dependence between the barbs, benzos, and ethanol

A

yes. people who have tolerance to alcohol will also show tolerance to the rest

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18
Q

withdrawal of benzo

A

rebound insomnia, anxiety, seizures when they were used at high doses or for antiepileptic

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19
Q

withdrawal from barbs and ethanol

A

anxiety, agitation, life-threatening seizures (delirium tremens)

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20
Q

what are the important interactions for the CNS depressants

A

their effects are additive with other CNS depressants, such as antihistamines, opiates, anesthetics, beta-blockers

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21
Q

what do barbs do to metabolic panel

A

induce lipid metabolism such as lipid soluble drugs, oral contraceptives, carbamazepine, phenytoin, warfarin

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22
Q

what are the non-BZ drugs

A

zolpidem and zoleplon

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23
Q

what are zolpidem and zoleplon

A

BZ1 agonists, they have less cognitive effects and are used in the treatment of insomnia.

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24
Q

what do we treat benzos with

A

flumazenil

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25
Q

what do all alcohols do to the CNS

A

cause depression. GABAmimetic activity. all alcohols cause metabolic acidosis.

26
Q

what does ethylene glycol do

A

CNS depression, ATN due to crystals in the kidney,metabolic acidosis.

27
Q

what does methanol do

A

causes respiratory failure, acidosis, ocular damage

28
Q

what is the toxic metabolite of ethylene glycol

A

oxalic acid

29
Q

what is the toxic metabolite for methanol

A

formaldehyde

30
Q

what is the toxic metabolite of ethanol

A

acetyladehyde

31
Q

what does ethanol do

A

CNS depression, acidosis

32
Q

what does acute ethanol do to the body

A

N/V, HA, hypotension, combines with folate and thiamine

33
Q

what is chronic alcoholism do to the body

A

hypoglycemia, fatty liver and lipemia, muscle wasting, gout

34
Q

what are the drugs of choice for partial-simple or complex seizures

A

valproic acid, phenytoin, carbamazepine

35
Q

DOC for general tonic clonic

A

valproic acid, phenytoin, carbamazepine

36
Q

DOC for absence seizures

A

ethasuximide and valproic

37
Q

DOC for statis epilepticus

A

lorazepam, diazepam, phenytoin, fosphenytoin

38
Q

what is the mechanism of action for phenytoin

A

decreases axonal conduction by preventing Na+ influx through fast Na channels.

39
Q

what other drug shares phenytoin’s mechanism

A

carbamezepine

40
Q

what is the mechanism of action for benzos

A

increases inhibition by GABA mediated hyperpolarization

41
Q

what other drugs share benzo’s general mechanism?

A

barbiturates, even though this isnt entirely accurate.

42
Q

what is the general mechanism of action for lamotrigine, topiramate, felbrate

A

decreases the excitatory effects of glutamic acid.

43
Q

what is the general mechanism for ethosuximide and valproic acid

A

decreases Ca influx through T type channels in thalamic neurons

44
Q

phenytoin mechanism

A

blocks Na channels in the inactivated state.

45
Q

does phenytoin prevent seizure propagation or initiation

A

does NOT prevent initiation, it does prevent propagation.

46
Q

what are the uses of phenytoin

A

seizure states, except absence.

47
Q

what are the kinetics for phenytoin

A

variable absorption, zero order elimination, nonlinear kinetics. it induces p450

48
Q

SE of phenytoin

A

CNS depression. gingival hyperplasia, hirsutism, osteomalacia, megaloblastic anemia, anaplastic anemia. it is a teratogen responsible for cleft-lip and palate.

49
Q

carbamazepine mechanism

A

identical to phenytoin. sodium channel blocker in the inactivated state.

50
Q

uses of carbamazepine

A

DOC for trigeminal neuralgia. seizure states, and bipolar (manic phase). not for use in absence

51
Q

SE of carbamazepine

A

induces its own metabolism. CNS depression, osteomalacia, megaloblastic anemia, aplastic anemia. exfoliative dermatitis (SJS), increases ADH release. teratogen: causes cleft lip and palate and spina bifida.

52
Q

valproic acid mechanism

A

blocks sodium channels in the inactivated state but also blocks GABA transaminase and increases the GABA. blockade of T-type calcium channels. (similar to phenytoin and ethosuximide)

53
Q

uses of valproic acid

A

seizure states including absence. the manic phase of bipolar. migraine prophylaxis.

54
Q

SE of valproic acid

A

INHIBITS p450. hepatotoxic, thrombocytopenic, pancreatitis, alopecia. teratogen: spina bifida.

55
Q

ethosuximide mechanism

A

blocks t-type calcium channels in the thalamus

56
Q

uses of ethosuximide

A

absence seizures

57
Q

felbrate and lamotrigine

A

blocks sodium and glutamate receptors

58
Q

uses of felbrate and lamotrigine

A

adjuvant to seizure state medicines,

59
Q

SE of felbrate and lamotrigine

A

hepatotoxic, aplastic anemia, SJS.

60
Q

gabapentin mechanism

A

increases the effects of GABA

61
Q

uses of gabapentin

A

seizure states and neuropathic pain esp. postherpetic neuralgia.

62
Q

SE of gabapentin

A

sedation

shelf pharm (20 decks)

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