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Benzo's
Pharm (Test 2)
| Question | Answer |
|---|---|
| What are 5 pharmacologic effects of benzo's? | 1)sedation, 2)anxiolysis, 3)anticonvulsant actions, 4)skeletal muscle relaxation, 5)antegrade amnesia |
| True or False: Benzo muscle relaxation is sufficient for surgical relaxation? | False |
| True or False: Benzos decrease the amount of NMB needed for surgical relaxation? | False |
| Describe the mechanism of action of benzo's. | bind to benzo receptors (part of GABA receptor) which when activated, causes the inc. binding of GABA to its receptor, opening Cl- channel, hyperpolarizing the neuron causing inhibition of the neuron the excitation. |
| What 2 receptors to benzo's have affinity for? | GABA and glycine |
| GABA and glycine are both _____________ neurotransmitters. | inhibitory |
| The enhancement of the GABA inhibitory effect might explain which pharmacologic effect of benzo's? | sedative and anticonvulsant effects |
| The glycine-like inhibition in the spinal cord motor neurons accounts for which pharmacologic effect of benzo's? | relaxation |
| The glycine-like inhibition of afferent conduction in the brainstem accounts for which pharmacologic effect of benzo's? | anxiolysis |
| GABA has separate binding sites for what 3 drugs? | benzo's, barb's, and ETOH |
| Due to its multiple binding sites, if the GABA receptor is activated at more than one site, what happens to the inhibition of the CNS excitation? | synergistic effects |
| For what purpose is midazolam most often administered? | premedication or IV sedation |
| In its aqueous solution, (pH of 3.5) midazolam is ________-soluble. | water |
| At physiologic pH (7.4), midazolam is ________-soluble. | lipid |
| At what pH dose midazolam become lipid soluble? | pH>4 |
| What aspect of midazolam makes this water to lipid soluble change possible? | imidazole ring |
| Does midazolam require a carrier agent? | no |
| Midazolam (is or isn't?) compatible with opioids and LR? | is |
| What routes can midazolam be given? | PO, IM, SL, intranasal, IV |
| True or False: Midazolam is used both for the induction and the maintenance of anesthesia? | true |
| Midazolam causes what kind of cardiac effects? | dec. in BP (SVR dec.), inc. in HR (more than diazepam), no change in CO, effects exaggerated in hypovolemic pts |
| Does midazolam cause a change in CO? | no |
| Midazolam causes what kind of respiratory effects? | dd dec. in ventilation (similar to diazepam), effect exaggerated in COPD pts, apnea (rapid injection of doses >0.15mg/kg IV or when given with opioids) |
| What dose of midazolam is associated with apnea? | >0.15mg/kg IV |
| Midazolam causes what kind of CNS effects? | dec. CRMO, dec. cerebral blood flow, CANNOT cause isoelectric EEG, can treat seizures from local anesthetic toxicity, excitement in <1% of pts |
| How do you treat excitement caused by midazolam admin? | flumazenil |
| True or False: Midazolam can cause an isoelectric EEG needed for cease of circulation during bypass cases. | False |
| What is the onset of midazolam? | 0.9-5.6 min |
| _____% of oral dose of midazolam reaches circulation after hepatic first-pass. | 50% |
| What is the elimination 1/2 time of midazolam? | 1-4 hrs |
| Midazolam's short duration is due to ...? | redistribution |
| How is midazolam metabolized? | hydroxylation by hepatic microsomal oxidative enzymes (CP450) |
| Compare midazolam's hepatic clearance to that of diazepam and lorazepam. | midazolam is 5X faster than lorazepam and 10X faster than diazepam |
| What is the pediatric premedication dose of midazolam? | 0.3-0.5mg/kg PO |
| What is the pediatric PO dose onset of midazolam? | 30 min |
| What is a sedative dose of midazolam? | 1-2.5 mg IV |
| What is an induction dose of midazolam? | 0.1-0.2mg/kg IV (watch for apnea) |
| True or False: Midazolam is not associated with N/V. | True |
| True or False: Midazolam is associated with emergence excitement. | False |
| Diazepam is _________-soluble. | lipid |
| What is used as diazepam's carrier agent? | propylene glycol |
| What is the peak concentration of a PO dose of diazepam? | 1 hr |
| True or False: Diazepam can be given IM, but absorption is unreliable and injection is painful. | True |
| What are some CV effects of diazepam admin? | minimal dec. in BP, CO, and SVR, less effects the barbs and midazolam, synergistic dec. w/ fentanyl, exaggerated w/ hypovolemic pts |
| Which benzo has more synergistic effects when given w/ fentanyl? | midazolam |
| What are some respiratory effects of diazepam admin? | dec. response to CO2, minimal depressant effects until 0.2mg/kg IV, dec. in TV, apnea rarely occurs w/ doses <10mg IV |
| At what dose do we being to see resp. dep. after diazepam admin? | 0.2mg/kg IV |
| At what dose do we being to see apnea after diazepam admin? | >10mg IV |
| What are some CNS effects of diazepam admin? | dec. CMRO, CBF, ICP, relaxes skeletal muscles, dec. MAC up to 30%, anticonvulsant prophylaxis, anxiolysis, amnesia |
| Rank the benzos from highest to lowest amnestic effects. | lorazepam > midazolam > diazepam |
| Rank the benzos from highest to lowest hepatic clearance. | midazolam > lorazepam > diazepam |
| Diazepam can reduce MAC up to _____%. | 30% |
| Does diazepam cross the placental barrier? | yes |
| How is diazepam metabolized? | hepatic microsomal enzymes |
| What are diazepam's metabolites? Active or inactive? | Active: desmethyldiazepam, oxazepam |
| Which of diazepam's metabolites is only slightly less potent than diazepam? | desmethyldiazepam |
| Desmethyldiazepam can account for the return of drowsiness ________ hrs after admin. | 5-8 hrs |
| What is one reason for the prolonged effects of diazepam? | desmethyldiazepam |
| What is the elimination 1/2 life of desmethyldiazepam? | 48-96 hrs |
| What is the elimination 1/2 life of diazepam? | 21-37 hrs |
| The elimination 1/2 life of diazepam can increase by up to _____X in pts with cirrhosis. | 5X |
| What medication can prolong the effect of diazepam? | tagamet |
| What is a typical adult PO dose of diazepam? | 10-15 mg PO |
| What the peak effect time of a PO dose of diazepam? | 55min |
| Lorazepam is _________-soluble. | lipid |
| What are 2 carrier agents for lorazepam? | polyethylene glycol, propylene glycol |
| What are the possible routes of administration of lorazepam? | oral, IM, IV |
| What is one limitation to lorazepam's usefulness? | slow onset, long duration |
| Compare lorazepam's amnestic quality to that of diazepam and midazolam. | greater than diazepam and midazolam |
| Lorazepam's antegrade amnesia can last up to _______hrs/ | 6 hrs |
| Compare lorazepam's lipid solubility to than of diazepam. | Lorazepam is less lipid soluble than diazepam |
| Lorazepam's metabolites are (active or inactive?) | inactive |
| Compare lorazepam's release from the GABA receptor to that of diazepam. | slower (longer effect) |
| What is a typical dose of lorazepam? | 50mcg/kg (up to 4 mg) |
| What is the peak concentration time of lorazepam? | 2-4 hrs |
| What is the elimination 1/2 life of lorazepam? | 10-20 hrs |
| Which benzo has an elimination 1/2 time that is increased by 5X in pts with cirrhosis? | diazepam |
| Which benzo is the most potent amnestic? | lorazepam |
| Which benzo's duration is prolonged in pts taking Tagamet? | diazepam |
| Which benzo has an active metabolite that is only slightly less potent? | diazepam |
| Which benzo is water-soluble upon injection? | midazolam |
| Which benzo has a relaxant effect on skeletal muscle tone? | diazepam |
| which benzo causes the greatest inc. in HR? | midazolam |
| Which benzo is taken up by hepatic first pass, and only 50% of dose reaches circulation? | midazolam |
| Which benzo is the most lipid soluble? | diazepam |
| Which benzo is available SL and intranasal? | midazolam |
| Which benzo is compatible with opioids and LR? | midazolam |
| Which benzo has the greatest hepatic clearance? | midazolam |
| Which benzo has an imidazole ring? | midazolam |
Created by:
lindseymontgomery
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