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1. Chlordiazepoxidea. AKAb. usesc. how does strychnine work?2. Diazepam= in 1965, was used...
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a. Libriumb. anti-strychnine, sedative, hypnoticc. blocked glycine- inhibitory neurotransmitter...
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1. chemical structure base of BZD's2. 3 components of chemical structure of diazepam
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1. Diazepine ring fused to benzene ring2. diazepine ring fused to benzene ring with phenol...
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Solubility of the following:1. diazepam2. lorazepam3. midazolam
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1. not water-soluble, highly lipophilic2. "almost" water-insoluble; lipophilic but relatively...
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1. Diazepam Solutiona. concentrationb. 4 components of sol'nc. pHd. preservative/ buffer?
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1a. 5mg/mlb.-0.4mL propylene glycol (40%)-0.1mL alcohol (10%)-0.015mL benzyl alcohol (1.5%)-...
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Lorazepam Solution1. concentration2. component3. preservative
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1. 2mg or 4mg/ml2. 0.18 mL polyethylene glycol (18%)3. benzyl alcohol
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Midazolam Solution1. concentration2. components3. preservative4. pH adjusted to ___ by what...
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1. 1 or 5mg/ mL2. 0.8% sodium chloride0.01% disodium edetate1% benzyl alcohol3. benzyl alcohol4....
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Midazolam1. most ___-___2. solubility is dependent on the ___3. explain ring status r/t solubility
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1. lipid-soluble2. pH3. pH<4.0= ring open- water solubleph>4.0+ ring closed- lipid soluble
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Metabolism1. ___ with what 2 principle pathways2. Signficiant diff btw 2 pathways
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1. hepatic= microsomal oxidation (N-dealkylation or aliphatic hydroxylation) and glucuronide...
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1. liver oxidation of midazolam and diazepam2. results in greater ___ ___ of MDZ than DZP3....
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1. imidazole ring of midazolam is oxidized much more quickly than the diazepine ring of other...
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1. Lorazepam= less affected by ___ ___ and by what factors?2. Cimetidine affect on BZD's
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1. enzyme induction/ factors known to alter Cyto450 and other phase I enzymes2. no affect on...
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Metabolites1. Diazepama. ___ ___ metabolitesb. effect on drugc. names2. Midazolama. nameb....
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1a. 2 activeb. add to and prolongs drug effectsc. oxazepam (marketed as drug) and desmethyldiazepam2a....
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Clearance and pharmokinetic classification of the following1. midazolam2. lorazepam3. diazepam
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1. 6-11 ml/kg/min = short lasting2. 0.8-1.8 ml/kg/min = intermediate lasting3. 0.2-0.5 ml/kg/min...
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1. 6 factors that affect kinetics2. induction doses of the 3 BZD's3. best BZD for induction
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1.- age- gender- race- enzyme induction- hepatic/ renal disease- obesity (def affects LZP,...
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1. all BZD's have which 6 effects?- one of which is ___- produced muscle relaxation2. potency=...
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1. sedation, hypnosis, anxiolytic, amnesic, anticonvulsant- centrally2. affinity of BZD for...
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1. compare receptor potency of the 3 BZD's2. BZD Receptora. which receptor?b. location?c. 3...
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1. LZP 5-10x's more potent than DZPMDZ 3-6x's more potent than DZP2a. GABAa receptor complexb....
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Receptor Binding subtypes1. a1 receptors (3 effects)2. a2 receptors (2 effects)3. following...
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1. sedation, anterograde amnesia, anticonvulsant properties2. anxiolysis, muscle relaxation3a....
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1. 6 areas of CNS with highest density of BZD receptors2. 3 areas of lower densities
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1. -olfactory bulb - cerebral cortex - cerebellum - hippocampus - substantia...
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1. Function of agonist at GABAa receptora. opens ___ ___b. ____ cellc. makes ___ to ____2....
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1a. chloride channelsb. hyperpolarizesc. resistant to activation2. binds to GABAa but causes...
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1. onset and DOA of Lor, Diaz, Mid
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- onset of DZP/ MZP= 30-60sec- onset of LZP= 60-120sec (not suitable for induction)- DOA= MZP/...
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Effects on CNS1. ___ & ___ reduce ___ & ___ in a dose-related manner (equally- good)2....
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1. DZP and MZP/ CBF & CMRO22. light sleep3. incr seizure initiation threshold of local...
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Effect on Respiratory System1. overall effect?2. peak onset of ventilatory depressiona. MDZ?b....
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1. dose-related central respiratory depression2a. rapid- about 3minb. 1-2hoursc. rate of administration...
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Respiratory Effects1. ___ = incr resp depression in ___ - incrs ___ of depression -...
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1. MDZ= COPD - duration - MZP > thiopental2. opioids and BZD's = supra-additive/...
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Effects on CV System1. Hemodynamic effects?2. preservation of ___ ___a. ___>___b. similar...
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1. modest HDY effects2. homeostatic reflex mechanismsa. MDZ> BZD'sb. thiopentalc. severe...
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1. effect of BZD's on pts with left vent. end diastolic pressure increases2. does not block...
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1. NTG effect- dcrs filling pressure and incr CO2. SNS/ stress response to surgery/ intubation3....
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1. Induction doses:a. MZPb. DZPc. LZP (altho, not used for induction)2. Sedation doses: incremental...
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1a. 0.05- 0.15mg/kgb. 0.3-0.5mg/kgc. 0.1mg/kg2a. 0.5- 1mg repeatedb. 2mgc. 0.25mg repeated
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Uses- Sedation1. Pre-op?2. Intra-op?a. monitor ___b. Prop vs MDZ= emergence and resp depressionc....
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1. titrate for effect2a. RRb. emerg= prop faster than MDZresp depress= greater with Propc....
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MDZ1. onset2. time of peak effect3. DOA4. Recovery diff among MDZ, DZP and LZP5. compare level...
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1. more rapid2. 2-3 min (shorter than DZP/ LZP) 3. dose-dependent4. MDZ&DZP= same;...
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Oral Sedation1. DZP2. MDZ
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1. 5-15mg doses for adults= good pre-op2. pediatrics- 0.5mg/kg; onset= 10 min
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1. MDZa. ___ to command and loss of what?b. compared to thiopental?c. amnesia?
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a. unresponsiveness/ loss of eyelash reflexb. less rapidc. more reliable
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Termination of EFfects1. awakening d/t what?2. emergencea. after 10mgb. after induction dose...
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1. redistribution2a. 15 minutesb. 17 minutes3. dose4. longer than thio by 10min; much longer...
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Analgesia Effects1. no ___ effects; provide ___ and ___2. 4 reasons MDZ is better than thiopental3....
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1. analgesia/ amnesia and hypnosis2.- better amnesia- more stable hemodynamics- less requirement...
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1. ____ effects btw combinations of Prop, Alfent, and Versed- greatest of this effect is btw...
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1. synergistic- midazolam and ALfent2. decreased incidence (based on 3 studies; no SR or meta...
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1. most signif contra'd among all 3?2. DZP/ LZP= ___ ___ and ____** give close to IV site**
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1. respiratory depression2. venous irritation and thrombophlebitis
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Flumazenil1. 2 trade names2. ___ antagonist3. ___ intrinsic activity4. law of mass action=...
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1. Anexate and Romazicon2. competitive3. minimal4. affinities and concentrations (** dynamic-...
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Flumazenil1. ___ rapidly2. net result= ___ is reduced over time as compared to ___3. proportion...
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1. cleared2. antogonist/ agonist3. increase/ resedation
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Flumazenil1. chem structure diff from other BZD's2. metabolism and metabolites3. half life...
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1. no phenyl group on bottom- replaced by carbonyl group2. metabolized in the liver; 3 metabolites3....
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Flumazenil1. CNS bad effect2. provides rapid and dependable reversal of which 5 things?3. onset4....
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1. reverses anti-convulsant properties of BZD's2. -unconsciousness-respiratory depression-sedation-...
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1. dose for reversal of BZD's2. diagnosis repeated in coma dose
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1. 0.2mg repeated up to 3.0mg max2. 0.5mg up to 1.0mg max
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a
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a
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