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SRNAPharmacology II > BENZODIAZEPINES > Flashcards

BENZODIAZEPINES Flashcards

(126 cards)

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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
Midazolam water or lipid soluble
WATER
26
Midazolam vs Diazepam potency
2-3 Times more POTENT than DIAZEPAM
27
Midazolam at ph<4 ring is open so it is
WATER SOLUBLE
28
Midazolam at ph>4 ring is CLOSED so it is
HIGHLY LIPID SOLUBLE
29
IV administration of Verset
No venous irritation on injection
30
Midazolam can be mixed with
LR and acidic salts
31
Midazolam Pharmacokinetics : first pass? lipid solubility
First past effect = 50% of drugs reaches systemic circulation HIGHLY LIPID SOLUBLE, CROSS BBB
32
What is the effect equilibration time of midazolam ?
Slow compared to propofol and thiopental (0.9 - 6 minutes)
33
Protein binding of Midazolam
EXTENSIVE PROTEIN BINDING
34
Midazolam long acting or short acting and why?
Short acting | Because of REDISTRIBUTION FROM BRAIN TO inactive site and rapid metabolism
35
Context sensitive half time of MIDAZOLAM ______than diazepam and Lorazepam
LOWER
36
Elimination Half time is __________; compare to diazepam
1-4 hours; | MUCH SHORTER THAN DIAZEPAM.
37
2 patients with high Vd, why?
Elderly Morbidly obese Due to distribution to adipose tissue
38
CNS effects of midazolam is ______Than diazepam
SHORTER
39
Midazolam half time prolonged after
CBP
40
Metabolism of Midazolam
Undergoes extensive HYDROXYLATION by hepatic and small intestine microsomal enzymes
41
Midazolam effect prolonged with drugs that
Inhibit CYP450 ; | E-mycin; CCB, fentanyl, cimetidine
42
Hepatic Clearance of midazolam is 5 times ______ than lorazepan and 10 times _____than diazepam
Greater; Greater
43
Midazolam on CNS
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
44
Midazolam : Does not prevent
increase ICP that is associated with laryngoscopy
45
Benzo and Neuroprotective?
Not been shown to be neuroprotective
46
Midazolam < Can be use to treat seizures ?
Yes, Potent anticonvulsant effect | Can treat Status epilepticus
47
Midazolam lead to ______in ventilation with _______ equivalent to ___________
decrease; 0.15mg/kg IV ; 0.3mg/kg IV
48
Midazolam depression in ventilation is greater with
COPD
49
Rapid administration of Midazolam________ can lead to ______
>0.15mg/kg; TRANSIENT APNEA
50
_________Given with fentanyl 2mcg/kg can lead to
0.05 mg/kg Arterial hypoxemia Hypoventilation
51
IMPORTANT : BENZO
can depress the swallowing reflex and DECREASE UPPER AIRWAY activity
52
Midazolam induction dose | Effect on HR, BP
0.2mg/kg on induction | Decrease systemic BP and INCREASE HR more than diazepam
53
The hemodynamic changes are similar to
thiopental 3-4mg/Kg IV
54
What is NOT ALTERED with Benzo?
CARDIAC OUTPUT
55
Beneficial in Improving CO in patients with CHF
Benzodiazepines.
56
Midazolam and CV
hypovolemia results in enhanced BP LOWERING EFFECT similar to other agents.
57
What is the most commonly used Benzo for preop medications?
MIDAZOLAM
58
Preoperative Medication Dose of __________ before induction provides reliable ______ and ________ in children without producing delay in awakening
0.5mg/kg PO 30 minutes | Sedation and Anxiolysis
59
Given with midazolam enhances the anxiolytic and amnestic effects
SCOPOLAMINE
60
Antegrade amnesia with Midazolam is
Related and parallels the degree of sedation
61
IV sedation : Midazolam vs Diazepam
More rapid onset Greater amnesia Less post op sedation
62
Depression of ventilation has synergistic effects with
Opioids Propofol CNS depressants
63
Induction of Anesthesia : Midazolam Dose
0.1-0.2 mg/kg over 20-60 seconds
64
Compared to midazolam: thiopental
50-100% faster induction
65
Onset of action of midazolam faster with
small dose of opioid
66
Fentanyl precedes the midazolam onset of action
1-3 minutes
67
Midazolam require __________ in ________
Smaller doses in elderly
68
Anesthetic requirements for VA with midazolam are
decrease in a dose dependent manner
69
Awakening after GA is ___________ than when thiopental is used?
1-2.5 times longer
70
N/V with emergence with midazolam?
NO
71
Diazepam is a _________ benzodiazepine with a ______Duration of action compared to midazolam
HIGHLY lipid soluble | Prolonged duration of action
72
Injection of IV and IM may be painful with
Diazepam
73
Pharmacokinetics of Diazepam | Peak ______in adult, _______In children
1 hour | 15-30 minutes
74
Diazepam and Brain
Rapid uptake
75
Volume of Distribution of Diazepam ? women vs men
LArge; LARGER in women than men
76
Does DIAZEPAM CROSS the placenta?
YES; concentration may be greater in fetus than mother
77
DIAZEPAM solubility and protein binding
Highly lipid soluble | Bound to plasma proteins
78
Cirrhosis of liver and renal failure may
Decrease protein binding and INCREASE related adverse events.
79
Diazepam metabolism is by
Hepatic microsomal enzymes
80
There are 2 principles Metabolites are
DESMETHYLDIAZEPAM OXAZEPAM lesser degree temazepam
81
Principal is ___________ slightly _______ and is metabolized more slowly half life _______
DESMETHYLDIAZEPAM; 48-96 hours
82
Ultimately oxidized metabolites are
EXCRETED in urine as Glucuronide conjugated metabolites.
83
Diazepam and Cimetidine
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
Pepcid and diazepam
Pepcid has no effect on diazepam
85
Half time of Diazepam
21-37 hours
86
Liver cirrhosis has up to _______folds in ______elimination half time due to
5 ; INCREASE ; increase vd and Decrease hepatic Blood flow
87
Diazepam and Ventilation effects
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
Caution with Diazepam
Combined with other CNS depressants or patients with COPD may results in exaggerated or prolonged depression of ventilation
89
CO2 curve is NOT shifted to the right with
Diazepam
90
CO2 curve shifted to the right with
OPIOIDS
91
Diazepam induction dose
0.5mg- 1mg/kg
92
Effects of Diazepam of BP, CO and SVR
minimal, SIMILAR TO NATURAL SLEEP
93
What happens with N2O and opioids
Direct myocardial depressant | Decrease in SBP
94
Diazepam and muscle tone
Decreases skeletal muscle tone
95
Diazepam overdose
Serious negative outcomes are UNLIKELY if cardiac and pulmonary functions are supported, and other CNS depressant like alcohol are not present
96
Clinical Use for management of Deliriums Tremors
Diazepam
97
Diazepam peak is
55 minutes
98
Diazepam on MAC
Decreases MAC
99
Diazepam anticonvulsants effects
0.1 mg/kg IV abolishes seizure activity
100
Explain Diazepam anticonvulsants effects
Due to ability to facilitate the actions of INHIBITORY TRANSMITTER GABA
101
Lorazepam potency compared to diazepam and midazolam
More potent sedative and amnestic
102
Metabolism of Lorazepam
Conjugated with glucuronic acid in the liver to form inactive metabolites that are excreted by the kidneys
103
Elimination half time is
10-20 hours
104
Metabolism of lorazepam is not
Entirely dependent of microsomal enzymes | less infuences by increasing age, or CYP inhibitors such as cimetidine
105
Recommended oral dose for pre-op is
50mcg/kg not to exceed 4 mg
106
Peak level of lorazepam? | Amnesia?
2-4 hours | Maximal ANTEROGRADE amnesia lasting up to 6 hours without excessive sedation
107
With lorazepam, large doses=
Greater sedation WITHOUT INCREASED AMNESIA
108
What is the limiting factor when rapid awakening is desired?
Prolonged duration of action
109
Lorazepam Limitations
Slow onset of action
110
Effective in limiting emergence reactions after ketamine
Lorazepam
111
Protein binding of Lorazepam, Diazepam and midazolam
96-98%
112
Compare doses Midazolam Diazepam Lorazepam
0. 15 - 0.3mg 0. 3- 0.5 0. 05
113
Flumazenil, Romazicon
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
Flumazenil effectively antagonizes the benzodiazepine component of
ventilatory depression of combined opioids and benzo
115
Flumazenil Dosing
0.2mg IV (8-15mcg/kg) usually reverses the CNS effects of Benzo with 2 minutes
116
Flumazenil if required
0.1mg IV (To a total of 1mg ) can be given at 60 seconds intervals
117
Flumazenil Doses to decrease the degree of sedation as needed
0.3-0.6mg IV
118
Flumazenil dose required to ABOLISH the therapeutic effcts of benzodiazepines
0.5 to 1 mg
119
In patients that have overdose from unknown substance, failure to respond to 5mg indicates
involvement of other substance.
120
Flumazenil duration of action is
30-60 minutes
121
Alternative to repeated doses is a continuous low dose infusion of
0.1 - 0.4 mg/hr
122
Flumazenil Side effects
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
EXTRA: Benzo with the fastest onset of acton
Midazolam
124
BENZO water insoluble in propelene glycol
Diazepam
125
_____increases the threshold for local anesthetic-induced seizure activity.
DIAZEPAM
126
Not use for induction anesthesia due to slower onset
LORAZEPAM

SRNAPharmacology II (32 decks)

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