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Pharmacology > Benzodiazepines > Flashcards

Benzodiazepines Flashcards

1
Q

What do Benzodiazepines do?

A 
Anxiolysis
Sedation
Anticonvulsant action
Spinal cord mediated skeletal muscle relaxation
Anterograde Amnesia
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2
Q

What do we use benzodiazepines for?

A

Pre-Op sedation
Conscious Sedation
Short Procedures such as regional anesthesia placement
Theoretically can be used for induction of anesthesia
Specific uses

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3
Q

MOA of Benzodiazepines

A

GABA Molecule
GABAa- pentameric
2 alpha subunits, 2 beta units and 1 gamma

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4
Q

What subunit of benzo causes sedation

A

alpha-1

5 subunits

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5
Q

What subunit of benzo causes anxiolysis?

A

Alpha-2

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6
Q

GABA Agonist

A

binds to GABAa increasing affinity of receptors for GABA

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7
Q

What change opens in GABA channels

A

Cl, increased frequency of cl channel opening, increased Cl conductance

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8
Q

What occurs with increased Cl conductance

A

post synaptic membrane hyperpolarization. More resistance to excitation= drug effect we are looking for

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9
Q

Generalizations about Benzos

A

Highly lipid soluble, protein bound
Higher margin of safety
Fewer/less serious drug interactions (compared to others)
Anticonvulsant, increased seizure threshold in LAST
Depresses swallowing reflex and upper airway activity
synergistic with other CNS depressants
HPA suppression, inhibit platelet aggregation (unsure if clinically relevant)

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10
Q

LAST

A

Local Anesthetic Systemic Toxicity

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11
Q

Anticonvulsant Characteristics of Benzos

A

Decreased alpha activity
Increased low voltage rapid beta activity
Unable to produce isoelectric EEG

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12
Q

Benzos in Elderly

A

Increased sensitivity due to pharmacokinetics, dose dependent
Aging/liver disease effect on glucuronidation

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13
Q

Structure of Midazolam

A

Substituted imidazole ring makes drug stable in aqueous solution, accounts for rapid metabolism
Water soluble, no preservative, painless injection

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14
Q

Pharmacokinetics of Midazolam (PO)

A

rapid GI absorption (50% reaches systemic circulation= substantial hepatic first pass)
Hepatic/small intestine metabolism

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15
Q

What enzyme breaks down Midazolam

A

P450 CYP3A4-> active, inactive metabolites, cleared by kidneys

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16
Q

Midazolam Elimination Time

A

Elimination 1/2 time 1.9 hours (can be 2x in elderly d/t decreased hepatic BF/Enzyme activity

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17
Q

Midazolam DOA

A

short (15-80 mins) d/t lipid distribution from brain to inactive tissue sites

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18
Q

Pharmacodynamics of Midazolam (CNS)

A

decreases CMRO2/CBF

Cerebral vasomotor response to CO2 stays in tact, does NOT prevent increase in ICP with DL, NO neuroprotective qualities

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19
Q

Pharmacodynamics of Midazolam (Respiratory)

A

DD (0.15 mg/kg) decreases ventilation d/t decreased hypoxic drive

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20
Q

Pharmacodynamics of Midazolam (CV)

A

decreases SVR (coudn increase CO in CHF) enhanced CV changes with other induction drugs in hypovolemic patients, does not attenuate CV response to DL

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21
Q

MIdazolam IV Dose

A

1-2.5 mg adults

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22
Q

Midazolam PO Dose

A

0.5mg/kg q30 mins prior to induction= reliable sedation anxiolysis without delayed wakening

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23
Q

Dose of Midazolam for Paradoxical Vocal Cord Motion Treatment

A

0.5-1mg

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24
Q

Structure of Diazepam

A

insoluble in water
must be dissolved in organic solvent such as propylene glycol which causes pain on injection
Lipid emulsion exists which decreases pain but also slightly decreases bioavailability

25
Q

Pharmacokinetics of Diazepam (PO)

A 
rapid GI absorption
crosses placenta (can be equal or greater than maternal)
26
Q

Two metabolites Diazepam is metabolized into

A

desmethyldiazepam (elimination 1/2 48-96 hours only slightly less potent then parent drug)
Oxazepam- undergo secondary conjugation to form water soluble glucorinide conjugateives, so if something inhibits oxidative metabolism will have further prolongation of effects

27
Q

Oxidative pathway of N-desmethylation

A

metabolism of diazepam

28
Q

Pharmacodynamics of Diazepam (respiratory)

A

minima depressant effect

increase PaCO2 not seen until doses reach or exceed 0.2mg/kg

29
Q

Pharmacodynamics of Diazepam (CV)

A

transient depression of baroreceptor mediated HR, could theorectically affect hypovolemic patients
no direct action on SNS
Fentanyl given after?- associated with decreased SVR/BP

30
Q

Uses of Diazepam

A

treatment of delirium
tremens (severe alcohol withdrawal)
anticonvulsant (0.1mg/kg)

31
Q

Pharmacokinetics of Lorazepam (metabolism)

A

conjugated with glucuronic acid in liver makes inactive metabolites then excreted by kidneys

32
Q

Most potent Benzodiazepine

A

lorazepam

33
Q

Pharmacokinetics of Lorazepam (special Characteristics)

A

not as dependent on liver for metabolism, less issues with age, liver failure, enzyme inhibiting drugs

34
Q

Slower Clearance d/t

A

slower hepatic glucoronidation

Compared to Midazolam and Diazepam

35
Q

Pharmacokinetics of Lorazepam

A

Slower Onset of Action (1-2mins)
Longer DOA (6-10 h) due to lower lipid solubility/slower entrance into CNS
Reliable PO/IM absorption

36
Q

PO Pharmacokinetics of Lorazepam

A

max plasma concentration within 2-4 hours, therapeutic range persists for 24-48 hours

37
Q

Volume of Distribution PK of Lorazepam

A

High Vd in Obese= higher elimination 1/2 t

38
Q

Uses of Lorazepam

A

limited due to slow onset, long DOA

effective in limiting incidence of emergence reactions s/p ketamine administration

39
Q

Remimazolam

A

Organ independent metabolism (carboxylic ester moiety) = rapid degradation= fast recovery

40
Q

Oxazepam

A

Active metabolite of diazepam

slow PO absorption

41
Q

Uses of Oxazepam

A

insomnia with night wakings, short total sleep time

42
Q

Alprazolam (Xanax) Uses

A

primary anxiety, panic attacks,

43
Q

How Xanax works

A

inhibition of adrenocorticotrophic hormone/cortisol secretion

44
Q

Uses of Clonazepam

A

seizures

45
Q

uses of flurazepam

A

insomnia, myoclonic/infantile spasms
+ active metabolite = daytime sleepiness
decreased REM

46
Q

Use of Temazepam

A

insonmia

47
Q

Use of Triazolam

A

insomnia with difficulty falling asleep

risk of rebound insomnia with DC

48
Q

Benefits of Ro (investigational)

A

decreased recovery/time to ambulation post-op/use but did not demonstrate any difference in time to discharge compared to others

49
Q

Ro (investigational)

A

similar DOA/onset as otheres, increased plasma clearance

full agonistic activity @ CNS benzodiazepine receptor

50
Q

Flumazenil

A

Benzo reversal Agent

51
Q

Flumazenil Structure

A

similar to benzo but has carbonyl instead of phenyl group

52
Q

Efficiency of Flumazenil depends on

A

amount of free bezno at receptor site

53
Q

MOA of Flumazenil

A

competitive antagonist

54
Q

Use of Flumanzenil

A

0.2mg (effect within 2 mins)
0.1mg every minute for desired effect
0.3-0.6mg total should abolish sedative effects
0.5-1mg: total should achieve complete reversal
IF you have used 5mg total and still having issues, likely another cause

55
Q

DOA of Flumazenil

A

30-60 minutes

be aware could require supplementary doses after this time or low dose infusion (0.1-0.4mg/h) to maintain reversal

56
Q

C/A of Flumazenil

A

Benzo reliant patients esp those using for seizures

seizures noted when used in TCA/antidepressant overdose patients

57
Q

Definition of Benzo

A

A drug with a chemical structure including benzene and diazepine rings

58
Q

NOn- benzodiazepine Definition

A

is a drug with a similar pharmacology but not structure
binds on GABA at same site as benzos
similar effects
increased selectivity for certain GABA subunits= desired effects on sleeping with minimal SE

59
Q

Examples of Non-Benzo

A

Zaleplon (Sonata)
Zolpidem (Ambien)
Eszopicalone (Lunesta)

Pharmacology (14 decks)

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