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Benzo's

Pharm (Test 2)

QuestionAnswer
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