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Pharm Exam 3 > Depressants > Flashcards

Depressants Flashcards

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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
What is required for benzodiazepine sedative-hypnotic activity?
need electronegative substituent in the 7th position (halogen or a nitro group)
26
*benzodiazepines - pharmacokinetics:
1) absorption: ORAL; 2) metabolism: **LIVER**CYP3A4+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
Inactive water soluble glucuronide drugs? means what?
- lorazepam and oxazepam - rapid metabolism These two have dosing that is NOT dependent on age 3-OH type
28
weakly active, short lived active metabolite drugs? means what?
- alprazolam and triazolam | - short duration, metabolites dont do much
29
long lived and active metabolite drugs and means what?
- ALL EXCEPT: lorazepam, oxazepam, alprazolam, and triazolam | - long duration?
30
short acting benzodiazepines: LESS THAN 5 HRS
midazolam | triazolam
31
intermediate acting benzodiazepines: | 5-24HRS
* alprazolam * lorazepam * oxazepam * temazepam estazolam clonazepam
32
long lasting benzodiazepines: | LONGER THAN 24HRS
* clorazepate * diazepam * flurazepam chlordiazepoxide prazepam quazepam
33
metabolism age and benzodiazepines:
- 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
Which drug(s) have dosing that is NOT dependent on age?
3-OH type - oxazepam and lorazepam | Ke independent
35
Which drug(s) have dosing that IS influenced by age?
2-keto type - diazepam | Ke dependent
36
**benzodiazepines MOA?
- 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
alpha1 GABA_A receptor subtype is responsible for what effects?
- sedation - anticonvulsant action - anterograde amnesia
38
alpha 2 GABA_A receptor subtype is responsible for what effects?
-anxiolysis
39
*Benzodiazpines - side effects and toxicity:
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
date rape drug and drug type?
flunitrazepam - benzodiazepene
41
Lots of dependence/withdrawl with use of this drug type?
benzodiapenes
42
benzodiazepines - contraindications:
- pregnancy - elderly (altered metabolism = increased sensitivity) - substance abuse concern - sleep disorders - when alertness is requried
43
Benzodiazepines - drug interactions:
* ***1) additive CNS depression: ethanol, opioids, anticonvulsants, phenothiazine, antihistamines, TCA 2) cimetidine, erythromycin - carbamazepine, rifampin, phenytoin 3) estrogens 4) antacids 5) flumazenil
44
benzodiazepines - therapeutic uses:
* **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
benzodiazepine antagonist - drug? - MOA? - metabolism? - effects? - uses?
- 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
reverse effects of benzodiazepines or benzodiazpine related newer hypnotics with what drug?
flumazenil
47
Benzodiazpeine related newer hypnotics (Z-DRUGS) * *-drug names: - clinical use? - MOA? - pharmacokinetics:
* **-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
Barbiturates - drugs names? - clinical uses?
phenobarbital pentobarbital thiopental anesthesia, sedative/hypnotic, anticonvulsant, medically induced coma --> OLDER AND NOT REALLY USED ANYMORE
49
phenobarbital used mainly for what?
anticonvulsant
50
pentobarbital used mainly for waht?
medically induced coma
51
thiopental used mainly for what?
anesthesia
52
barbiturates - pharmacokinetics:
- 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
barbiturates vs benzodiazepines MOA
- benzos increase freqency of opening of the GABA gated Cl channel - barbsopen the same channel for longer
54
Barbiturates MOA:
***-inc the duration of the GABA-gated chloride channel opening = membrane hyperpolarization =neuronal inhibition
55
Ultra short acting - intermediate - long acting barbiturates:
short=thiopental med=pentobarbital long=phenobarbital
56
* melatonin receptor agonist - drug name? - use? - MOA? - metabolism?
* *-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
serotonin receptor agonist: - drug name? - use? - MOA? - metabolism? - AE?
-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
* *beta blockers - Drug name? - uses?
- propranolol | - NOT an anxiolytic but diminishes some of the somatic manifestations of anxiety
59
* *antihistamines - drug names - use?
- hydroxyzine, diphenhydramine - used as mild sedative/relaxant for procedures - anxiolytic via sedative action
60
carbamates - dont worry so much here - drugs? - use?
- meprobamate - CNS acting muscle relaxant - like intermediate acting barbs - potential for abuse
61
* alcohols: - drugs? - uses?
- ethanol - anxiolytic via sedative action - ethanol is probably the oldest and most commonly used anxiolytic

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