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30 Cards in this Set

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516 BENZODIAZOPINES
516 BENZODIAZOPINES
What are some benzos that can be given pre/post/periop?
1. midazolam
2. lorazepam
3. diasepam
Onset, peak, and duration of versed?
Onset: 30-60 sec

Duration: 15-80 mins

Peak: 3-5 mins
Onset, peak, and duration time for Lorazepam?
Onset: 1-2 mins

Peak 20-30 mins

Duration: 6-10 hrs
What is the ring structure of benzodiazopine?
1. benzene ring

2. 7-member diazepine ring
Actions of benzodiazopine?
1. sedation
2. anxiolysis
3. anticonvulsant
4. ANTEROGRADE amnesia
What they DO NOT do?
1. analgesic effects

2. antidepressant

3. antipsychotic

4. protect stress of intubation.
Clincial uses of benzos?
1. anxiety
2. insomnia
3. sedation and amnesia
4. treats epilepsy and seizure states.
5. balanced anesthetic
Mechanism of action for benzos?
Act on GABA-a receptor

Hyperpolarization of cell

Receptor occupancy determines effect.
a. 20% anxiolysis
b. 30-50% sedation
c. 60% unconsciousness
What are the doses for Preop when using Midazolam?
Kids: 0.5 mg/kg PO 30 mins before (15mg max)

IV: 1-2.5mg
What is the dose for IV sedation (ICU sedation)?
0.5 mg IV load then 1-7 mg/hr IV
What is the dose for IV induction of anesthesia?
0.1 - 0.2 mg/kg
What is the dose for suppression of seizur activity using diazepam?
0.1mg/kg
Pharmacokinetics of benzos?
1. absorption
2. distribution
3. protein binding
Absorption
1. PO (first pass metabolism)

2. IV

3. IM
Distribution
1. dependent on lipid solubility

2. rapid redistribution from brain

3. vol. of distribution
Protein binding
Hypoalbumenia
How are benzos metabolized?
Liver oxidation (cyt P450)

Alcohol increases clearance

No active metabolites for versed.

First pass metabolism
How are benzos eliminated?
Metabolites are excreted in the urine.
What effects do benzos have on the renal system?
NONE
What effects do benzos have on the CNS?
1. dec. CMRO2 and CBF
2. no isoelectric EEG
3. no change in ICP
4. no evidence of neuroprotection.
5. potent anticonvulsant
What effects do benzos have on ventilation?
Decreases it
On cardiovascular?
Minor dec. BP and Inc. HR
Anticonvulsants and how do they work?
Tx local anesthetic induced seizures and delirium tremors.

Work by ability of benzos to facilitate the actions of inhibitory GABA.

NOTE: barbituates work by suppressing the CNS.
What dose of diazepam is effective for lidocaine toxicity, DTs, and status epilepticus?
0.1mg/kg
Why do we like Midazolam so much?
1. 2-3X potent than diazepam (valium).
2. pK 6.15
3. rapid onset
4. short duration
5. PO route

NOTE: NOT FOR PREGNANT WOMEN.
Why we don't like diazepam and lorazepam (ativan):
1. thrombophlebitis and venous irritation.
2. active metabolites
3. slow onset
4. long elimination
What are some drugs that treat insomnia?
1. oxazepam

2. flurazepam
What are some other drugs for insomnia?
1. triazolam
2. alprazolam (xanax)
3. zolpidem (ambien)
4. FLUNITRAZEPAM (ROHYPNOL)
Reversal of benzo and its doses?
Flumazenil

0.1-0.2mg IV repeated up to 3 mg.