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SRNAPharmacology II > BENZODIAZEPINES > Flashcards

BENZODIAZEPINES Flashcards

1
Q

Barbiturates compared to Benzodiazepines have ______and less ________

A

Less tendency for tolerance: potential for abuse
Safe in overdose
Less serious drug interactions
Less addicting than opioids, cocaine, amphetamine, and barbiturates
Benzodiazepines have replaced barbiturates pre-op medications.

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2
Q

Properties of Benzodiazepines

A

Properties of Benzodiazepines
• Highly lipid soluble
• Highly protein bound
• Hypoalbuminemia

Less binding to the benzodiazepines –>Causes enhanced clinical effect
Due to hepatic cirrhosis or chronic renal failure with protein spillage

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3
Q

Benzodiazepine absorption

A

Oral absorption-rapid

IV enters brain rapidly

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4
Q

Mechanism of action of Benzodiazepines.

Do they activate GABA?

A

Mechanism of ACTION
DO NOT activate GABA receptors
• They enhance the affinity of the receptors for GABA
• This leads to enhanced opening of chloride channels, ⇧ chloride conductance and hyper-polarization of the postsynaptic cell membrane, making most post synaptic neurons more resistant to excitation

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5
Q

GABA Receptor
Explain: it is a _________With separate binding sites for __________
Therefore
The basis of _______and why benzo are the

A

GABA Receptor
• Large macromolecule with separate binding sites for benzodiazepines, barbiturates, Etomidate, propofol,
neurosteroids and alcohol
• Therefore benzodiazepines, barbiturates and alcohol can have synergistic effects by acting on the same receptor by different mechanisms
• Results in ⇧ risk for overdose
• Also the basis for cross tolerance and why benzo’s are the first choice drug for alcohol detoxification

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6
Q

KNow midazolam

A

CV effects

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7
Q

Pharmacological Effects of Benzodiazepines

SASAA

A 
Anxiolysis
Sedation
Anticonvulsants
Anterograde amnesia
Skeletal	Muscle Relaxation- spinal cord mediated	
• Not adequate for	surgery,	no ⇩NMB dose
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8
Q

Sedative effects of benzo’s reflect

A

Activation of alpha 1 subunits of GABA

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9
Q

• Anxiolytic, amnesia effect due to

A

alpha-2 subunit activation

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10
Q

Most abundant receptor subtypes is

A

Alpha 1 subunits; 60% of GABA receptors in the brain

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11
Q

Less abundant receptor subtypes

A

Alpha 2 subunits (hippocampus, amygdala)

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12
Q

An important regulator of cardiac function and its physiological effects convey cardioprotection during MI

A

ADENOSINE

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13
Q

Cannot produce an ISOelectric EEG

A

Midazolam

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14
Q

Benzos On EEG

A

Alpha activity decrease

Beta activitiy increase

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15
Q

Side effects on Benzo

A

Fatigue and drowsiness; most common with chronic use

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16
Q

Benzo Sedation subsides usually

A

within 2 weeks

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17
Q

Caution of Benzo use in patients with chronic lung disease why ?

A

characterized by HYPOVENTILATION and DECREASED ARTERIAL OXYGENATION

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18
Q

Acute administration of benzo may cause

A

Transient Anterograde amnesia especially with alcohol

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19
Q

Benzo dependence occur after

A

> 6 months

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20
Q

Benzo withdrawal symptoms include TIA ?

When does it begin?

A
  • Tremulousness
  • Insomnia
  • Agitation
    between 1-5 days
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21
Q

Aging and Liver disease affect ________less than ___________ _____pathways

A

Glucuronidation

Oxidative metabolic pathways.

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22
Q

Preferred in aging and liver disease , why>

A

LORAZEPAM; because it is metabolized by glucuronidation

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23
Q

Diazepam is metabolized by

A

Hepatic microsomal enzymes to form ACTIVE METABOLITES

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24
Q

This medication have active metabolites

A

DIAZEPAM

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25
Q

Midazolam water or lipid soluble

A

WATER

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26
Q

Midazolam vs Diazepam potency

A

2-3 Times more POTENT than DIAZEPAM

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27
Q

Midazolam at ph<4 ring is open so it is

A

WATER SOLUBLE

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28
Q

Midazolam at ph>4 ring is CLOSED so it is

A

HIGHLY LIPID SOLUBLE

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29
Q

IV administration of Verset

A

No venous irritation on injection

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30
Q

Midazolam can be mixed with

A

LR and acidic salts

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31
Q

Midazolam Pharmacokinetics : first pass? lipid solubility

A

First past effect = 50% of drugs reaches systemic circulation
HIGHLY LIPID SOLUBLE, CROSS BBB

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32
Q

What is the effect equilibration time of midazolam ?

A

Slow compared to propofol and thiopental (0.9 - 6 minutes)

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33
Q

Protein binding of Midazolam

A

EXTENSIVE PROTEIN BINDING

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34
Q

Midazolam long acting or short acting and why?

A

Short acting

Because of REDISTRIBUTION FROM BRAIN TO inactive site and rapid metabolism

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35
Q

Context sensitive half time of MIDAZOLAM ______than diazepam and Lorazepam

A

LOWER

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36
Q

Elimination Half time is __________; compare to diazepam

A

1-4 hours;

MUCH SHORTER THAN DIAZEPAM.

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37
Q

2 patients with high Vd, why?

A

Elderly
Morbidly obese
Due to distribution to adipose tissue

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38
Q

CNS effects of midazolam is ______Than diazepam

A

SHORTER

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39
Q

Midazolam half time prolonged after

A

CBP

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40
Q

Metabolism of Midazolam

A

Undergoes extensive HYDROXYLATION by hepatic and small intestine microsomal enzymes

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41
Q

Midazolam effect prolonged with drugs that

A

Inhibit CYP450 ;

E-mycin; CCB, fentanyl, cimetidine

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42
Q

Hepatic Clearance of midazolam is 5 times ______ than lorazepan and 10 times _____than diazepam

A

Greater; Greater

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43
Q

Midazolam on CNS

A

Decrease CMRO2, and CBF similar to barbiturates and propofol
Cerebral vasomotor responsiveness to CO is preserved
ICP is unchanged
Does not prevent increase ICP ass

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44
Q

Midazolam : Does not prevent

A

increase ICP that is associated with laryngoscopy

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45
Q

Benzo and Neuroprotective?

A

Not been shown to be neuroprotective

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46
Q

Midazolam < Can be use to treat seizures ?

A

Yes, Potent anticonvulsant effect

Can treat Status epilepticus

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47
Q

Midazolam lead to ______in ventilation with _______ equivalent to ___________

A

decrease; 0.15mg/kg IV ; 0.3mg/kg IV

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48
Q

Midazolam depression in ventilation is greater with

A

COPD

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49
Q

Rapid administration of Midazolam________ can lead to ______

A

> 0.15mg/kg; TRANSIENT APNEA

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50
Q

_________Given with fentanyl 2mcg/kg can lead to

A

0.05 mg/kg
Arterial hypoxemia
Hypoventilation

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51
Q

IMPORTANT : BENZO

A

can depress the swallowing reflex and DECREASE UPPER AIRWAY activity

52
Q

Midazolam induction dose

Effect on HR, BP

A

0.2mg/kg on induction

Decrease systemic BP and INCREASE HR more than diazepam

53
Q

The hemodynamic changes are similar to

A

thiopental 3-4mg/Kg IV

54
Q

What is NOT ALTERED with Benzo?

A

CARDIAC OUTPUT

55
Q

Beneficial in Improving CO in patients with CHF

A

Benzodiazepines.

56
Q

Midazolam and CV

A

hypovolemia results in enhanced BP LOWERING EFFECT similar to other agents.

57
Q

What is the most commonly used Benzo for preop medications?

A

MIDAZOLAM

58
Q

Preoperative Medication
Dose of __________ before induction provides reliable ______ and ________ in children without producing delay in awakening

A

0.5mg/kg PO 30 minutes

Sedation and Anxiolysis

59
Q

Given with midazolam enhances the anxiolytic and amnestic effects

A

SCOPOLAMINE

60
Q

Antegrade amnesia with Midazolam is

A

Related and parallels the degree of sedation

61
Q

IV sedation : Midazolam vs Diazepam

A

More rapid onset
Greater amnesia
Less post op sedation

62
Q

Depression of ventilation has synergistic effects with

A

Opioids
Propofol
CNS depressants

63
Q

Induction of Anesthesia : Midazolam Dose

A

0.1-0.2 mg/kg over 20-60 seconds

64
Q

Compared to midazolam: thiopental

A

50-100% faster induction

65
Q

Onset of action of midazolam faster with

A

small dose of opioid

66
Q

Fentanyl precedes the midazolam onset of action

A

1-3 minutes

67
Q

Midazolam require __________ in ________

A

Smaller doses in elderly

68
Q

Anesthetic requirements for VA with midazolam are

A

decrease in a dose dependent manner

69
Q

Awakening after GA is ___________ than when thiopental is used?

A

1-2.5 times longer

70
Q

N/V with emergence with midazolam?

A

NO

71
Q

Diazepam is a _________ benzodiazepine with a ______Duration of action compared to midazolam

A

HIGHLY lipid soluble

Prolonged duration of action

72
Q

Injection of IV and IM may be painful with

A

Diazepam

73
Q

Pharmacokinetics of Diazepam

Peak ______in adult, _______In children

A

1 hour

15-30 minutes

74
Q

Diazepam and Brain

A

Rapid uptake

75
Q

Volume of Distribution of Diazepam ? women vs men

A

LArge; LARGER in women than men

76
Q

Does DIAZEPAM CROSS the placenta?

A

YES; concentration may be greater in fetus than mother

77
Q

DIAZEPAM solubility and protein binding

A

Highly lipid soluble

Bound to plasma proteins

78
Q

Cirrhosis of liver and renal failure may

A

Decrease protein binding and INCREASE related adverse events.

79
Q

Diazepam metabolism is by

A

Hepatic microsomal enzymes

80
Q

There are 2 principles Metabolites are

A

DESMETHYLDIAZEPAM
OXAZEPAM
lesser degree temazepam

81
Q

Principal is ___________ slightly _______ and is metabolized more slowly half life _______

A

DESMETHYLDIAZEPAM; 48-96 hours

82
Q

Ultimately oxidized metabolites are

A

EXCRETED in urine as Glucuronide conjugated metabolites.

83
Q

Diazepam and Cimetidine

A

Cimetidine delays hepatic clearance and prolongs the elimination half life of both DIAZEPAM and DESMETHYLDIAZEPAM due to cimetidine’s induced INHIBITION of MICROSOMAL ENZYMES

84
Q

Pepcid and diazepam

A

Pepcid has no effect on diazepam

85
Q

Half time of Diazepam

A

21-37 hours

86
Q

Liver cirrhosis has up to _______folds in ______elimination half time due to

A

5 ; INCREASE ; increase vd and Decrease hepatic Blood flow

87
Q

Diazepam and Ventilation effects

A

Minimal on ventilation
Detectable increase in ventilation not seen up until 0.2mg/kg is given
Sligh increase in PaCO2 due to decrease in TV

88
Q

Caution with Diazepam

A

Combined with other CNS depressants or patients with COPD may results in exaggerated or prolonged depression of ventilation

89
Q

CO2 curve is NOT shifted to the right with

A

Diazepam

90
Q

CO2 curve shifted to the right with

A

OPIOIDS

91
Q

Diazepam induction dose

A

0.5mg- 1mg/kg

92
Q

Effects of Diazepam of BP, CO and SVR

A

minimal, SIMILAR TO NATURAL SLEEP

93
Q

What happens with N2O and opioids

A

Direct myocardial depressant

Decrease in SBP

94
Q

Diazepam and muscle tone

A

Decreases skeletal muscle tone

95
Q

Diazepam overdose

A

Serious negative outcomes are UNLIKELY if cardiac and pulmonary functions are supported, and other CNS depressant like alcohol are not present

96
Q

Clinical Use for management of Deliriums Tremors

A

Diazepam

97
Q

Diazepam peak is

A

55 minutes

98
Q

Diazepam on MAC

A

Decreases MAC

99
Q

Diazepam anticonvulsants effects

A

0.1 mg/kg IV abolishes seizure activity

100
Q

Explain Diazepam anticonvulsants effects

A

Due to ability to facilitate the actions of INHIBITORY TRANSMITTER GABA

101
Q

Lorazepam potency compared to diazepam and midazolam

A

More potent sedative and amnestic

102
Q

Metabolism of Lorazepam

A

Conjugated with glucuronic acid in the liver to form inactive metabolites that are excreted by the kidneys

103
Q

Elimination half time is

A

10-20 hours

104
Q

Metabolism of lorazepam is not

A

Entirely dependent of microsomal enzymes

less infuences by increasing age, or CYP inhibitors such as cimetidine

105
Q

Recommended oral dose for pre-op is

A

50mcg/kg not to exceed 4 mg

106
Q

Peak level of lorazepam?

Amnesia?

A

2-4 hours

Maximal ANTEROGRADE amnesia lasting up to 6 hours without excessive sedation

107
Q

With lorazepam, large doses=

A

Greater sedation WITHOUT INCREASED AMNESIA

108
Q

What is the limiting factor when rapid awakening is desired?

A

Prolonged duration of action

109
Q

Lorazepam Limitations

A

Slow onset of action

110
Q

Effective in limiting emergence reactions after ketamine

A

Lorazepam

111
Q

Protein binding of Lorazepam, Diazepam and midazolam

A

96-98%

112
Q

Compare doses
Midazolam
Diazepam
Lorazepam

A
  1. 15 - 0.3mg
  2. 3- 0.5
  3. 05
113
Q

Flumazenil, Romazicon

A

Specific and exclusive benzodiazepine receptor GABA antagonist
it binds to specific sites on the GABA-A receptor, where
it competitively inhibits the binding of the neurotransmitter, GABA, to this receptor

114
Q

Flumazenil effectively antagonizes the benzodiazepine component of

A

ventilatory depression of combined opioids and benzo

115
Q

Flumazenil Dosing

A

0.2mg IV (8-15mcg/kg) usually reverses the CNS effects of Benzo with 2 minutes

116
Q

Flumazenil if required

A

0.1mg IV (To a total of 1mg ) can be given at 60 seconds intervals

117
Q

Flumazenil Doses to decrease the degree of sedation as needed

A

0.3-0.6mg IV

118
Q

Flumazenil dose required to ABOLISH the therapeutic effcts of benzodiazepines

A

0.5 to 1 mg

119
Q

In patients that have overdose from unknown substance, failure to respond to 5mg indicates

A

involvement of other substance.

120
Q

Flumazenil duration of action is

A

30-60 minutes

121
Q

Alternative to repeated doses is a continuous low dose infusion of

A

0.1 - 0.4 mg/hr

122
Q

Flumazenil Side effects

A

NO effects on MAC requirements
May precipitate WITHDRAWAL Seizures in patients with seizure disorders , long term benzos or cyclic antidepressants.
NOT associated with LV systolic function or coronary hemodynamics alterations.

123
Q

EXTRA: Benzo with the fastest onset of acton

A

Midazolam

124
Q

BENZO water insoluble in propelene glycol

A

Diazepam

125
Q

_____increases the threshold for local anesthetic-induced seizure activity.

A

DIAZEPAM

126
Q

Not use for induction anesthesia due to slower onset

A

LORAZEPAM

SRNAPharmacology II (32 decks)

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