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Anesthesia Pharm > Benzos And Barbs > Flashcards

Benzos And Barbs Flashcards

1
Q

5 effects benzos

A

Anxiolysis, anterograde amnesia, anticonvulsant, sedation, spinal level muscle relaxation

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2
Q

Benzos DONT do what 3 things

A

Produce enough muscle relaxation for surgery, alter amt of muscle relaxant required, or induce hepatic enzymes

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3
Q

Benzos safer in which ways (3)

A

Less tolerance and abuse potential than barbs and opioids. Greater margin of safety in OD. Have a specific antagonist.

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4
Q

Benzos MOA 2. Don’t do what.

A

Facilitate action of GABA at GABAa, increase affinity of GABAa for its receptor. DONT activate the GABAa receptor

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5
Q

What does affinity for gaba a receptor do 4

A

Enhances opening of cl gated ch, inc cl conductance, hyperpolarizes post-synaptic membrane, inc resistance of post synaptic membrane to excitation

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6
Q

3 things that block gaba a receptor

A

Etoh, benzos, propofol

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7
Q

Generally benzos are what two things

A

Highly lipid soluble and protein bound (albumin)

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8
Q

Versed: solubility, potency, metabolism

A

Water soluble. 2-3x >than diazepam. Extensive hepatic 1st pass effect.

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9
Q

Versed: duration, t 1/2

A

Short (rapid redistribution), 1-6.5 hrs

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10
Q

Versed

How metabolism occurs

A

Hydroxylation from lipid to water soluble compounds in liver- 1 and 4 hydroxy-midazolam. Conjugated and excreted in urine

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11
Q

Versed: renal failure does not alter what

A

Vd, t 1/2, or clearance

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12
Q

Versed CNS effects: potent 2, decreases 2

A

Potent anticonvulsant and amnestied. Decreases CBF and CMRO2

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13
Q

Versed CNS effects: does not do what. Preserves what

A

Does not produce isoelectric EEG, does not attenuate ICP response to laryngoscopy. Preserves cerebrovascular resp to CO2

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14
Q

Versed respiratory effects: ventilation effects, decreases what 2

A

Dose dep vent dec. Hypoxemia/hypoventilation enhanced w/ presence of opioid. Depresses swallowing reflex and dec a/w activity.

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15
Q

Versed CV effects: decreases what, what doesnt change

A

Dec SVR at induction dose (BP decreases after). CO unchanged. Doesnt prevent HR/BP changes w intubation.

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16
Q

Versed dose: premedication in peds, max dose

A

0.25-0.5 mg/kg PO. Max dose 20 mg

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17
Q

Versed dose: IV sedation in adults. As high as what.

A

1-2.5 mg. 5 mg.

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18
Q

Versed dose: induction, timing

A

0.1-0.2 mg/kg over 30-60 secs

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19
Q

Diazepam: solubility, duration, solvents

A

Lipid soluble, prolonged duration. Propylene glycol and benzyl alcohol

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20
Q

Diazepam: pH, injection is what, binding, PO is what

A

6.6ish. Painful IV/IM. Protein bound. Rapid GI absorption.

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21
Q

Diazepam: metabolism

A

Oxidation & n-demethylation to desmethyldiazepam*, oxazepam, and temazepam by hepatic microenzymes. Conjugated to glucaronic acid, renal excretion

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22
Q

Diazepam: what happens to desmethyldiazepam

A

Oxidized, conjugated, and excreted in urine

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23
Q

Valium: ___ inhibits CP450 system

A

Cimetidine

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24
Q

Diazepam and desmethyldiazepam e 1/2t

A

D- 21-37 hrs if healthy, inc w age

DM- 48-96 hrs

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25
Q

Valium compared to versed: cv effects

A

Minimal changes in SVR, BP, CO (<20% decrease)

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26
Q

Valium doses: premedication PO

A

10-15 mg

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27
Q

Valium doses: premedication IV, reduces what

A

0.2 mg/kg, MAC

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28
Q

Valium doses: induction

A

0.5-1 mg/kg IV

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29
Q

Valium doses: anticonvulsant IV, how it works

A

Inhibits activity in hippocampus and limbic system. 0.1 mg/kg IV

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30
Q

Ativan: potency, metabolites

A

5-10x stronger than valium (strongest of all benz0s), inactive metabolites

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31
Q

Ativan: t 1/2, metabolism influence, solvent

A

10-20 hrs. Less affected by liver/age/other drugs. Propylene glycol

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32
Q

Ativan: premedication PO dose, onset

A

50 mcg/kg (max 4 mg). Slow onset limits usefulness, 2 hrs to peak concentration

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33
Q

Flumazenil: how it works

A

Specific competitive benzo antagonist w high affinity for benzo receptors

34
Q

Flumazenil: duration

A

30-60 min

35
Q

Flumazenil: dose, timing, max

A

0.2 mg iv. Wait 2 min. 0.1 mg subsequent at 60 sec intervals. Max 3 mg

36
Q

Flumazenil: can dx what/how, gtt dose

A

Coma, dose 5 mg. Gtt: 0.1-0.4 mg/hr (0.5-1 mcg/kg/min)

37
Q

Flumazenil: antagonizes what. Postop pts dont experience what

A

Depression of ventilation and sedation. Dont experience acute anxiety/stress response

38
Q

Flumazenil metabolism

A

Hepatic metab renal excretion

39
Q

Barbiturates: highly what, purpose. Derived from what

A

Highly alkaline to be bacteriostatic. All derived from barbituric acid: urea+ Malonic acid

40
Q

Barbiturates with which substitutions are sedative/hypnotic

A

2 and 5 carbons

41
Q

Barbiturates: what diff pts of structure do

A

Branch chain at 5 inc hypnotic activity. Phenyl at 5- anticonvulsant (phenobarb). Methyl radical= convulsants (methohexital).

42
Q

Barbs: sulfuration = what, and as inc what

A

Fat soluble. As lipid solubility inc: shorter duration, more rapid onset, inc potency

43
Q

Barbs: which chain more potent, which isomers more potent

A

Long branched chain > potent that straight chain. Levo isomers > potent than dextro isomers.

44
Q

Barbs: only available as what. Oxygen vs sulfur at # 2 leads to

A

Racemic mixtures. O2- oxybarbiturate. S- thiobarbiturate.

45
Q

Relative potency of barbiturates

A

Thiopental and thiamylal about 1. Methohexital 2.5

46
Q

Barb MOA

A

Dec GABA dissociation, enhances gaba activity. Mimics gaba (directly activates cl ch) at receptor. Depresses RAS

47
Q

Barb MOA: how it affects BP, muscle relaxation fx

A

Hypotension by dec transmission in sympathetic ganglia. Dec postsynaptic membrane activity to ach- some muscle relaxation but not enough for sx

48
Q

Barbs: onset, metab, binding

A

Rapid (redistribution), terminates quickly, extensive metab, highly protein bound

49
Q

Barbs: fat: blood partition coefficient, ionization

A
  1. PK 7.6
50
Q

Metabolism of oxybarbs and thiobarbs. What terminates activity

A

Oxy- hepatic. Thio- hepatic and some extra. Side chain oxidation at c#5 to carboxylic acid

51
Q

Barbs: metabolism

A

De sulfuration, hydrolysis opens ring, to water soluble pts. Renal excretion mainly

52
Q

Barbs: t 1/2 tpl. Prolonged in what. T 1/2 methohexital

A

TPL- 11.6. Prolonged in pregnancy d/t protein binding. Meth- 3.9 hrs

53
Q

Barbs CNS fx: decreases what

A

LOC, cerebrovasocontriction, reduces CBF, ICP, and CMRO2. Also decreases IOP

54
Q

Barbs CNS effects: EEG, paradoxical ___, methohexital does what

A

Isoelectric EEG. Excitement. Myoclonus and hiccups

55
Q

Barbs CNS: Doesn’t effect what, small doses do what

A

Doesnt effect SSEP monitoring or cause skel muscle relaxation. Small doses can cause pain

56
Q

Barbs: CV effects.

A

Dec SNS outflow, vasodilation, dec preload, SBP dec, HR increases if normovolemic. Myocardial depression minimal

57
Q

Barb: if SNS not intact, hypovolemia, or large dose given for ICP what happens

A

Significant dec in BP, myocardial depression

58
Q

Barbs: if rapid iv admin what happens. Oral barbs produce minimal what

A

Histamine release. Oral= min cv fx

59
Q

Barb resp fx

A

Dose dep depression of medullary and pontine centers. Dec response to hypoxia and hypercapnia. Apnea.

60
Q

Barb resp fx: depression of what is incomplete

A

Laryngeal and cough reflexes

61
Q

Barb: if not a large enough dose what can happen

A

Stage 2 like response during a/w manipulation, inc risk of laryngospasm and bronchospasm

62
Q

Barb: chronic use does what to metab, which most potent at this

A

Hepatic enzyme induction. Phenobarb most potent.

63
Q

Barbs: inc metabolism of what 5

A

Oral anticoags, phenytoin, TCAs, corticosteroids, vit k

64
Q

Barbs: DONT GIVE TO WHICH PTS and why

A

Porphyria. Stim d amino acid synthetase

65
Q

Barbs: readily crosses what, what happens to sz pts, does what iv

A

Placenta. Metab drugs 2x as fast (esp muscle relaxants). Venous thrombosis

66
Q

Barbs: tolerance and allergies

A

Tolerance rapidly- dose req inc 6 fold. Allergy rare but high mortality

67
Q

Barbs: nv incidence

A

Higher than midaz and propofol. Lower than etomidate, ketamine, and volatiles

68
Q

Barbs: TPL adult dose, dec dose in whom

A

3-5 mg/kg IV. Elderly, 1st trimester preg

69
Q

Barbs: TPL dose peds and infants

A

5-6 mg/kg peds, 7-8 mg/kg infants

70
Q

Barbs: methohexital dose adults and peds

A

1-2 mg/kg iv. 20-30 mg/kg pr peds

71
Q

Duration of single iv induction dose of barbs

A

5-8 min

72
Q

Drugs to not mix w barbs: general 4 and why

A

Opioids, catecholamines, NMBs, versed (all acidic)

73
Q

Drugs to not mix w barbs: 6 specific

A

Pancuronium, vecuronium, atracurium, alfentanil, sufentanil, midazolam

74
Q

Barbs: if __ solution too ___, precipitates. Use what w reconstituting powder

A

LR, acidic. Sterile water or NSS

75
Q

Barbs: intra arterial injection tx general 4

A

NSS dilution. Pnehoxybenzamine. Heparin or urokinase. Brachial plexus or stellate ganglion block.

76
Q

Barbs intra arterial injection: 2 specific

A

Papa Ernie 40-80 mg in 10-20 ml nacl, 5-10 ml lidocaine 1%

77
Q

Porphyrins: 6

A

Hgb, myoglobin, catalase, peroxidase, resp and p450 liver cytochromes

78
Q

How porphyrin attack starts

A

Decrease in heme concentration. Drugs most commonly. Also hormone flux, menstruation, NPO, dehydration, stress, infection

79
Q

S/s porphyria crisis

A

Abd pain, NVD, tachycardia, htn (ans instab), na/k/mg disturb, skel muscle weakness, resp failure, seizure

80
Q

Drugs to avoid w porphyria

A

Ketamine, etomidate, barbiturates

Anesthesia Pharm (12 decks)

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