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Pharm Exam 3 > Depressants > Flashcards

Depressants Flashcards

1
Q

Inhibitory amino acids

A

GABA and glycine

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2
Q

Excitatory amino acids

A

glutamate and aspartate

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3
Q

Benzodiazepine drugs naming:

A

end in -pam or -lam except clorazepate

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4
Q

selective depressants are

A 
sedative hypnotics
aka:
benzodiazepines
barbiturates
ethanol
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5
Q

non-selective/general depressants:

A

antihistamines

opioid analgesics

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6
Q

sedative anxilytics - what effect?

A
  • exert a calming effect or sedation with concomitant relief of anxiety at relatively low doses
  • depressant effects on psychomotor and cognitive functions
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7
Q

hypnotics - what effects?

A
  • agents that produce drowsiness and encourage the onset and maintenance of sleep
  • hypnotic effects: more rapid onset of sleep; increased duration of stage 2NREM; dec duration of REM and stage 4 NREM
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8
Q

anxiety brain regions affected;

A
  • limbic
  • amygdala - fear
  • hipocampus mood emotion memory
  • prefrontal cortex - cognitive function
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9
Q

Anxiolytic agent groups:

A
  • benzodiazepine sedative hypnotics
  • benzodiazepine anxiolytic
  • benzodiazepine like (Z-drugs)
  • serotonin agonists (5HT1A)
  • beta blockers
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10
Q

Benzodiazepine sedative hypnotic drugs:

A
  • flurazepam
  • temazepam
  • triazolam
  • midazolam
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11
Q

benzodiazepine anxiolytic

A

anxiolytic at low dose - at high dose same sedative hypnotic

  • alprazolam
  • clorazepate
  • diazepam
  • lorazepam
  • oxazepam
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12
Q

benzodiazepine like (Z-drugs)

A
  • *-zolpidem
  • *-eszopiclone

-zaleplon

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13
Q

anxiolytic serotonin agonist?

A

buspirone

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14
Q

anxiolytic beta blocker?

A

propanolol

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15
Q

Depressant agent groups:

A

barbiturates
antihistamines
melatonin agonists
alcohols

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16
Q

barbiturate drugs?

A

phenobarbital - LONG ACTING
pentobarbital
thiopental - SHORT ACTING

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17
Q

antihistamine drugs?

A

hydroxyzine

diphenhydramine

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18
Q

melatonin agonist drugs?

A

ramelteon

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19
Q

alcohol drugs?

A

durrrp - ethanol

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20
Q

dosing of sedative - hypnotics?

A

graded dose dependent depression of CNS:

  • sedation or sleep
  • anesthesia or coma
  • respiratory depression and death
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21
Q

barbiturates and alcohol dose effects:

A

LINEAR relationship bw inc dose and more intense effect - less drug needed to get more intense effect (coma and death)

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22
Q

benzodiazepines and newer hypnotics dose effects:

A

NON LINEAR SLOPE- relationship bw dose and effect tapers off about anesthesia level so need WAY higher dose to get super intense effect = SAFER TO USE

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23
Q

**sedative-hypnotics - uses?

A
  • *1) relief of anxiety
    a) primary:GAD,panic, OCD, PTSD
    b) seconday:acute MI, GI ulcers
  • *2) relief of insomnia
    3) sedation and amnesia
    4) tx of epilepsy and seizures
    5) control of ethanol of other sedative hypnotic withdrawl states
    6) muscle relaxation
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24
Q

most commonly used sedative-hypnotics?

A

benzodiazepines

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25
Q

What is required for benzodiazepine sedative-hypnotic activity?

A

need electronegative substituent in the 7th position (halogen or a nitro group)

26
Q

*benzodiazepines - pharmacokinetics:

A

1) absorption: ORAL;
2) metabolism: LIVERCYP3A4+glucuronidation
a) inactive water soluble (3-OH benzos) glucuronides - rapid metabolism and no activity (lorazepam and oxazepam)
b) weakly active, short lived active metabolites - short duration and metabolites have little clinical significance (alprazolam and triazolam)
c) long lived and active metabolite - 2-keto benzos - ALL EXCEPT: lorazepam, oxazepam, alprazolam, and triazolam - ACTIVE and last a while

27
Q

Inactive water soluble glucuronide drugs? means what?

A
  • lorazepam and oxazepam
  • rapid metabolism

These two have dosing that is NOT dependent on age 3-OH type

28
Q

weakly active, short lived active metabolite drugs? means what?

A
  • alprazolam and triazolam

- short duration, metabolites dont do much

29
Q

long lived and active metabolite drugs and means what?

A
  • ALL EXCEPT: lorazepam, oxazepam, alprazolam, and triazolam

- long duration?

30
Q

short acting benzodiazepines: LESS THAN 5 HRS

A

midazolam

triazolam

31
Q

intermediate acting benzodiazepines:

5-24HRS

A
  • alprazolam
  • lorazepam
  • oxazepam
  • temazepam

estazolam
clonazepam

32
Q

long lasting benzodiazepines:

LONGER THAN 24HRS

A
  • clorazepate
  • diazepam
  • flurazepam

chlordiazepoxide
prazepam
quazepam

33
Q

metabolism age and benzodiazepines:

A
  • older people have altered metabolism

- inc in age related to: dec lean body mass; inc Vd for many lipid soluble drugs; decreased rate of elimination

34
Q

Which drug(s) have dosing that is NOT dependent on age?

A

3-OH type - oxazepam and lorazepam

Ke independent

35
Q

Which drug(s) have dosing that IS influenced by age?

A

2-keto type - diazepam

Ke dependent

36
Q

**benzodiazepines MOA?

A
  • potentiate effects of GABA at the GABA_A receptors (CL ion channels)
  • *** inc frequency of opening and conductance of the Cl channels - bind to BZ sites bw alpha1 and gamma2 subunits to open cahnnels –>influx of Cl –> inc membrane hyperpolarization and overall neuronal inhibition ==potentiate GABAergic inhibition at all levels of the neuraxis
37
Q

alpha1 GABA_A receptor subtype is responsible for what effects?

A
  • sedation
  • anticonvulsant action
  • anterograde amnesia
38
Q

alpha 2 GABA_A receptor subtype is responsible for what effects?

A

-anxiolysis

39
Q

*Benzodiazpines - side effects and toxicity:

A

1) drowsiness and sedation-impaired judgement and confusion
2) ataxia - poor motor coordination
* *3) respiratory depression - dose related - can be lethal if combined with other depressants ex alcohol!**
4) anterograde amnesia - date rape drugs - flunitrazepam
* **5) tolerance (sedative effects) takes 12-14 days to get tolerance
* **6) dependence-physical and physiological - withdrawl
7) dizziness, headache, nausea

40
Q

date rape drug and drug type?

A

flunitrazepam - benzodiazepene

41
Q

Lots of dependence/withdrawl with use of this drug type?

A

benzodiapenes

42
Q

benzodiazepines - contraindications:

A
  • pregnancy
  • elderly (altered metabolism = increased sensitivity)
  • substance abuse concern
  • sleep disorders
  • when alertness is requried
43
Q

Benzodiazepines - drug interactions:

A
  • ***1) additive CNS depression: ethanol, opioids, anticonvulsants, phenothiazine, antihistamines, TCA
    2) cimetidine, erythromycin
  • carbamazepine, rifampin, phenytoin
    3) estrogens
    4) antacids
    5) flumazenil
44
Q

benzodiazepines - therapeutic uses:

A
  • **1) anxiolytic- relieve anxiety
  • **2) sedative-hypnotic - relief of insomnia
    3) conscious sedation - medical procedures
    4) antispasmodic - muscle relaxant
    5) Acute alcohol withdrawl
    6) agitated patients
    7) panic attacks
    8) depression
    9) bipolar
    10) seizures
45
Q

benzodiazepine antagonist

  • drug?
  • MOA?
  • metabolism?
  • effects?
  • uses?
A
  • flumazenil
  • competitive inh binds to BZ receptor - REVERSE EFFECTS OF BENZODIAZEPINES
  • rapidly abs via IV - short duration (~2hrs)- metabolism by liver
  • generalized CNS arousal and anxiogenic
  • -uses: Terminate benzodiazepine induced sedation; diagnosisa nd Tx of benzodiazepine tox
46
Q

reverse effects of benzodiazepines or benzodiazpine related newer hypnotics with what drug?

A

flumazenil

47
Q

Benzodiazpeine related newer hypnotics (Z-DRUGS)

  • *-drug names:
  • clinical use?
  • MOA?
  • pharmacokinetics:
A
  • **-eszopiclone, zolpidem
  • -management of insomnia
  • selectively bind to BZ receptors on GABA_A receptor and is agonist (only to Alpha1 subunit)
  • rapidly acting
  • short duration -rapid metabolism with in-active metabolites

-also reversed by flumazenil

48
Q

Barbiturates

  • drugs names?
  • clinical uses?
A

phenobarbital
pentobarbital
thiopental

anesthesia, sedative/hypnotic, anticonvulsant, medically induced coma –> OLDER AND NOT REALLY USED ANYMORE

49
Q

phenobarbital used mainly for what?

A

anticonvulsant

50
Q

pentobarbital used mainly for waht?

A

medically induced coma

51
Q

thiopental used mainly for what?

A

anesthesia

52
Q

barbiturates - pharmacokinetics:

A
  • absorption and distribution - varies with lipid solubility
  • metabolism - liver and is slow - has NO active emtabolites unlike benzos
  • excretion - via kidney - needs to be metabolized except phenobarbital to some extent
  • duration of effect - depends on metabolism except thiopental where redistribution limits duration
53
Q

barbiturates vs benzodiazepines MOA

A
  • benzos increase freqency of opening of the GABA gated Cl channel
  • barbsopen the same channel for longer
54
Q

Barbiturates MOA:

A

***-inc the duration of the GABA-gated chloride channel opening
= membrane hyperpolarization
=neuronal inhibition

55
Q

Ultra short acting - intermediate - long acting barbiturates:

A

short=thiopental
med=pentobarbital
long=phenobarbital

56
Q
  • melatonin receptor agonist
  • drug name?
  • use?
  • MOA?
  • metabolism?
A
  • *-ramelteon
  • *-induces sleep onset if pateint cant falls asleep - no dependence!
  • -MOA: melatonin receptor agonist - MT1 (sleep onset); MT2 (circadian pattern)*
  • met: extensive first pass - active met with even longer t1/2
57
Q

serotonin receptor agonist:

  • drug name?
  • use?
  • MOA?
  • metabolism?
  • AE?
A

-buspirone
-non-sedating anxiolytic - less psychomotor impairment compared to benzos - does not affect driving skills! little abuse potential
NO AMNESIA OR MUSCLE RELAXATION
-MOA: Partial agonist at 5HT1A receptors (autoreceptors)
-Met: 2-4 halflive - extensive first pass
-nonspecific chest pain, tachycardia, palpitations, dizziness, nervousness, tinnitus, GI distress

58
Q
  • *beta blockers
  • Drug name?
  • uses?
A
  • propranolol

- NOT an anxiolytic but diminishes some of the somatic manifestations of anxiety

59
Q
  • *antihistamines
  • drug names
  • use?
A
  • hydroxyzine, diphenhydramine
  • used as mild sedative/relaxant for procedures
  • anxiolytic via sedative action
60
Q

carbamates - dont worry so much here

  • drugs?
  • use?
A
  • meprobamate
  • CNS acting muscle relaxant
  • like intermediate acting barbs - potential for abuse
61
Q
  • alcohols:
  • drugs?
  • uses?
A
  • ethanol
  • anxiolytic via sedative action
  • ethanol is probably the oldest and most commonly used anxiolytic

Pharm Exam 3 (11 decks)

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