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20 Cards in this Set

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  • Back
benzodiazepine [7]
Antianxiety (Anxiolysis)
Amnestic (anterograde amnesia)
Muscle Relaxant
Alcohol withdrawal – use the longer acting such as chlordiazepoxide
make for a good premedication for surgery (midazolam, lorazepam, diazepam)
About same uses as Barbiturates but why use these instead?
About same uses as Barbiturates but why use these instead?
Barbiturates have
1. Low therapeutic index (toxic)
“intoxicatio” side effects
Early non-barbiturate agents
A nonbarbiturate sedative-hypnotic, unrelated chemically to other sedatives, methaqualone is classified as a central nervous-system depressant. Quaaludes and Sopors are pure methaqualone, while Parest, Optimil, and Somnafac are methaqualone hydrochloride. Biphetamine T and Biphetamine T 20 add amphetamine and dextroamphetamine to the methaqualone”
Quite lipid soluble – must be formulated with propylene glycol which can cause venoirritation diazepam formulated with a soybean oil
Must be very careful to not mix with acid salts of other compounds such as opioids otherwise can protonate the nitrogens

Since water soluble at lower than pH of 4, often formulated in acidic solution about pH 3.5 at physiological pH reverts back to lipid soluble form.
benzo SAR
Must have electron withdrawing (electronegative) group at position 7
Triazolo derivatives are more potent (less metabolized).
Have additional phenyl (aryl)
If no triazole ring is present, must have carbonyl at position 2.
Positions 6,7,9 must be unsubstituted.
Substitution at N1 should be small alkyl group
Additional phenyl (aryl) increases activity
Substitution at 2’ with electron withdrawing group increases activity, produces greater amnesia.
No substitution at 4’ position.
benzo's interact with
Interacts with
Adenosine Receptors

Agonist activity increases because inhibits uptake of adenosine
Benzodiazepines bind to the _________ sub-unit of the _______ receptor at an allosteric site which results in increased receptor activity.
Benzo's are an ________ of the GABA receptor, not an _______.

Potency is determined by?
binding affinity – strength of binding
Anatomically, benzo's inhibit neurotransmission in the?
reticular activating system
Benzo S/A'
Slight respiratory depression
Synergistic with opioids
Can be more pronounced with elderly patients
Induction minimally decreases BP, CO and systemic vascular resistance (SVR)
most postent?

fastest elimination?

Not water soluble and Lipophylic
Special Formulation needed
Exception is Midazolam
High protein binding
Midozolam ~ 94%
Lorazapam/Diazepam ~ 99%
Most lipophylic show more of a 3 compartment model
Easily absorbed from GI – but because fairly easily metabolized, significant first pass effect
Slower equilibration time with brian compared with thiopental barbiturate and propofol
Onset depends on distribution to brain which is dependent upon lipophilic character.
Distributed to peripheral tissues
Extent dependent upon lipid solubility
The more lipid soluble (diazepam) rapidly cross placenta
Lipophylic so some amount of perfusion dependency.
Metabilized by cyp p450 enzymes
Cyp 3A
Can be slowed by drug-drug interactions
Cimetidine,erythromycin, antifungals, calcium channel blockers, also fentanyl and grapefruit juice
Elderly – less metabolism due to less perfusion also less protein binding so larger Vd and longer metabolism and clearance
no active metabolites ?
Temazepam/Lorazepam/Oxazepam Those with only Phase II such as lorazepam usually see metabolism the same across all populations

midaz, no phase 2

Diazepam - active metabolites
– can have resurgence of effect also enterohepatic recycling
pharmacodynamic profile doesn’t always well match drug elimination, why?
some active metabolites undergo further metabolism even more slowly than the parent compound
Classified short/long etc by t1/2
Table Summary
Dependent upon kind of metabolism
Does not parallel duration
Cirrhosis of liver/renal insufficiency
Cirrhosis – less plasma protein so less binding and more free drug
Pregnancey – readily crosses placenta
Competitive antagonist
Reverses effects
Quick acting (1-3 minutes)
Short Duration (~ 1 hr)
Non specific antagonist
CNS stimulant that overcome depressions caused by benzodiazepines.