Term
| what is the name of the benzodiazapine prototype still commonly used today in dentistry? |
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Definition
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Term
| what is the mechanism of action of benzodiazapine? |
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Definition
| diazepam binds to its particular receptor which is linked to chloride channels that facilitate the actions of the inhibitory neurotransmitter GABA by opening chloride channels and letting Ca++ in causing hyperpolarization- and locking the GABA receptor into a high affinity state- so the probability of GABA binding increases |
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Term
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Definition
| very lipid soluble and is absorbed from the small intesting very rapidly. peak blood levels occur in 1 hr |
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Term
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Definition
| crosses the BBB very readily however only 1% is in free form in the blood. |
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Term
| what is one of the major drawbacks of valium |
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Definition
| prolonged duration of action |
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Term
| what causes valium's prolonged duration of action |
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Definition
is has a long T2 of parent compound- 24-48 hours because of enterohepatic cycling.
also, its metabolites also has long T2's. |
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Term
| what is the schematic of valium's metabolism |
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Definition
| diazepam (t2 of >20 hrs) to nordazepam (t2 of >20 hrs) to oxazepam (t2 of 6-20 hours) to glucuronide |
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Term
| what is the shematic of halcion's metabolism |
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Definition
| halcion (t2 of <6 hrs) to n-hydroxytriazolam (t2 of <6 hrs) |
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Term
| what are the therapeutic effects of diazepam besides anxiolysis? |
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Definition
| increase in seizure threshhold, 2) amnesia (esp when administed parenterally) 3)muscle relaxation (bruxers) 4) analgesia (kind of) |
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Term
| valium adverse side effects |
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Definition
sedation and ataxia- must be accompanied to and from appt. children and elderly esp susceptible
2)respiratory depression- can occur in overdose but is highly unlikely because of LARGE MARGIN OF SAFETY does is 2-10, toxic dose is 700 mg and it is self limiting because based on endogenous GABA
3)thrombophlebitis- due to hemolysis caused by alcohol and propylene glycol used as solvents in IV
4) paradoxical excitement- infrequent to predisposed patients
5)teratogenesis- can cuase cleft palata in 1 trimester |
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Term
| Flumazenil- what is it used for? |
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Definition
used to reverse benzodiazepine 1-5 mg over 2-10 min. it is a competitive antagonist for benzodiazepines and imidazopyridines. it is used for respiratory depression and paradoxical excitement
Thrombophlebitis with IV injection- crystal that have have precipitated can initiate inflammation through direct contact and activation of hageman factor
it can also cause hemolysis due to the alcohol and propylene glycol solvents |
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Term
| Midazolam (versed) what is it used for? |
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Definition
| IV benzodiazepine because much more water soluble than others |
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Term
| how is thrombophlebitis be minimized? |
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Definition
| inject slowly into a large vein- allows the crystal to redissolve and insures rapid dilution |
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Term
| what category drug is valium and why? |
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Definition
| FDA category D- positive evidence that there is human fetal risk involved but some benefits may be worth the risk |
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Term
| Diazpam contraindications |
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Definition
| Narrow angle glaucoma- antimuscarinic activity can block canals of schlem- and cause detached retina- blindess |
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Term
| diazepam disease interactions |
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Definition
liver disease- can prolong the metabolism of valium greatly- increases magnitude and duration of valium
2)myasynthia gravis-can exacerbate this situation
3)COPD- valium has CNS depressant effects |
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Term
| valium adverse drug interactions |
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Definition
1) CNA depressants- with most depressants valium has a additive effect
with alcohol it has a synergitstic effect- avoid alcohol 24 hrs BEFORE AND AFTER
2)disulfiram (ANTABUSE) with IV diazepam this drug will interact with the alcohol in the vehicle to produce toxic aldehyde reactions
3)ritonavir and indinavir- protease inhibitors used to treat HIV patients will inhibit metabolism of valium |
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Term
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Definition
| intermediate acting benzodiazepine agent |
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Term
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Definition
| intermediate acting benzodiazepine |
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Term
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Definition
| intermediate acting benzodiazepam |
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Term
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Definition
| intermediate acting benzodiazipine |
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Term
| what are the characteristics of intermediate acting benzodiazipines? |
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Definition
t2s of 6-24 hrs
shorter duration of action and show little hangover effects
have no intermediate metabolites and are directly glucuronidated so less senstive to changes in liver function
category D drugs too |
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Term
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Definition
| short acting benzodiazipine |
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Term
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Definition
| short acting benzodiazipine |
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Term
| what are the characteristics of shorting acting benzodiazipines? |
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Definition
t2 of less than 6 hrs
shortest recovery but still must be accompanied to and fron office
have active metabolites but these are rapidly metabolized and glucuronidation so no prolongation takes place |
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Term
| which benzodiazipine comes in injectible form and an oral form? and why is this esp. useful? |
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Definition
midazolam- useful for sedating children
oral dose for children= .5kg
always administer in office
never readminister |
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Term
| which benzodiazpine is a category X drug? |
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Definition
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Term
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Definition
1) zolpidem (ambien)
2)zaleplon (sonata7) |
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Term
| ambien mechanism of action |
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Definition
| felt to modulate GABA by bidning to a subunit that is part of GABA receptor complex |
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Term
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Definition
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Term
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Definition
| very short t2- 2 hrs, no active metabolites |
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Term
| who is ambien not contraindicated for? |
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Definition
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Term
| what FDA category is ambien? what DEA schedule is it? |
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Definition
category B - safe for women of child bearing age
schedule IV- little abuse, but you have to keep track of it |
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Term
| how is sonata7 diff than ambien |
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Definition
-very short duration- no residual effect 2 hr after administration
-produces amnesia
-FDA category C
-dose 5-20 for adults |
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