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104 Cards in this Set

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18- which of the following terms best describes a receptor located on neuronal terminal that binds a neurotransmitter released from another neuron & decreases release of neurotransmitter from the neuronal terminal?
heteroreceptor
18- type of presynaptic receptor that is also located on the neuronal terminal but binds a defferent neurotransmitter than the one being released from the terminal. the signaling through this type of receptor usually causes decreased release of the neurotransmitter.
heteroreceptor
18- general term for any type of recpetor located on the neuronal terminial
presynaptic receptor
18- receptor located on the postsynaptic membrane
postsynaptic receptor
18- type of presynaptic receptor in which the binding of the same neurotransmitter released from the neuronal terminal decreases further release of that neurotransmitter.
autoreceptor
18- term for a receptor associated with an ion channel and could be located on either pre or post
ionotropic receptor
18- neruotransmitters are made in neurons and released when vesicles fuse with the neuronal membrane. what name is given to this process?
exocytosis. fusion is triggered w influx of ca2+ into presynaptic terminal
18- process whereby receptors and other membrane proteins are recycled back into the neuron
endocytosis
18- the difference btw classical neurotransmitters and neuropeptides
neuropeptides are synthesized in the cell body.
classical neurotransmitters synthesized in vesicles en route or at the neuronal terminal from precursor substances.

neuropeptides arise from from transcription of neuropeptide gene, processing of neruopeptde mRNA, translation of mRNA into neuropeptide product in ER
18- T or F: classical neurotransmitters have a longer duration of action than neuropeptides?
F: neuropeptides act more as neuromodulators with longer duration of action than classical neurotransmitters.
18- T or F: neuropeptides undergo rapid reuptake into the presynaptic terminal
F
18- classical neurotransmitters are packabed into vesicles and so are neuropeptides-- what are the vessicles for neuropeptides called?
neuropeptides = dense-core vesicles
18- neuropepteides are degraded by ___ in the synapse
peptidases
18- which drug acts by inhibiting neurotrasmitter re-uptake?
fluoxetine (prozac)
selective serotonin reuptake inhibitor (SSRI)
18- pt with metastatic lung cancer is tx'd for chronic pain with daily doses of long-acting morphine formulation & oxycodone for breakthrough pain. he c/o medication no longer working. what is the mechanism to sxplain the lack of effect?
opiod receptors are down-regulated. chronic administration of agonist, opiod agonists morphine an doxy, with cause decrease in number or receptor proteins expressd by neuron in an attempt to decrease the signaling through that pathway and establish homeostasis
19- what is the mechanism of action of benzodiazepines?
potentiating the effect of GABA at chloride ion channels
18- which drug is an antiparkinsonian agent that acts by a strategy known as "precursor loading" which feeds the biosynthectic pathway for the synthesis of dopamine?
levodopa, antiparkinsonian drug
19- Benzos are noted for altering which aspect of sleep?
decreasing REM stage
18- drug used to treat alzheimer's disease by inhibiting the breakdown of Ach
donepezil
19- T or F: Flumazenil is a selective and competative benzo antagonist?
true. it is used for massive OD's, usually IV administration
18- how does morphine work?
opioid agonist acts by receptor activation
19- Zaleplon differs from Zolpidem how?
Zaleplon has a shorter 1/2 life
19- T or F: Alprazolam (xanax) is noted for its lack of sedation
false. Buspirone is a unique, nonsedating axiolytic (5-HT receptor)
delayed onset insomnia tx
fast-acting, short half-life
early-waking insomia tx
slow-acting, long half-life
mid-cylce insomnia tx
fast acting, ulta-short half-life
19- T or F: Flumazenil has the longest elimination half life
false. often Flumazenil has to be given multiple times to counteract a long acting benzo like diazepam
19- what drug produces withdrawal seizure?
alprazolam (xanax)
19- T or F: buspirone has a quick onset of action
false. takes 2 to 4 weeks of daily administration for clinical effectiveness
20- what is the the molecular mechanism underlying the antiepileptic effects of carbamazepine & phenytoin?
prolonging the inactivation of the Na+ ion channel. this leads to a decrease of repetitively firing neurons
20- what is the mechanism of action of ethosuximide & valproic acid?
inhibitng low threshold Ca2+ ion channels, particularly useful in controlling absence seizures
20- which drug potentiates the release of GABA by inhibiting GABA reuptake?
tiagabine (gabitril)
20- what drug increases the release of GABA by vesicular fusion?
gabapentin (neurontin)
20- what antiepileptic agent gained wider therapeutic use also to treat trigeminal neuralgia & the manic phase of bipolar disorder?
cabamazepine
20- what is the drug of choice for treating generalized absence seizures (petit mal) in children?
ethosuximide. acts by inhibiting the low-threshold Ca2+ channels thought to be active during absence seizures
20- which drug blocks glutamate receptor excitation?
topiramate (topamax)
20- what is phenytoin also used for?
mood stabilizer
20- what three mechanisms of action does topiramate (topamax) have?
1. increases Na+ channel inactivation
2. increases GABA
3. blocks glutamate
20- what is the mechanism of action of gabapentin (Neurontin)?
increase release of GABE. exact mechanism unknown
Employee Assistance Program
Available to employee and their families to aid in solving work and personal problems.
20- drugs used to tx ___ have an agonist effect at dopamine receptors
parkinsonism
20- how does tiagabine (gabitril) work?
increases Na+ channel inactivation
& blocks reuptake of neurotransmitters
21- by what mechanism do local anesthetics exert their effects?
blocking voltage-gated Na+ channels in nerves. unprotonated form of the local anesthetic molecule passes through the neuronal membrane and is changed to the protonated form in the cytoplasm where it binds to the inside of the sodium channel protein
21- are action potentials dependent on K+ channels for nerve fiber conductance?
no. increasing K+ conductance and hyperpolarizing nerves would cause inhibition of firing but not total blockade of action potentials
21- do local anesthetics block by a direct action only at the synapse?
no. they can block all along the nerve fiber
21- epinephrine is sometimes added to commercial local anesthetic solutions for which purpose?
decrease the rate of absorption of the local anesthetic by causing vasoconstriction acting at alpha 1 receptors, and thus decreases the amount of systemic absortion of the local.
21- T or F: epinephrine decreases absortion of local anesthetic, therefore decreasing the duration of action of the local
false. it increases the duration of action of the local
21- what characteristic is used to quantitate & compare the potency of gaseous general anesthetics?
minimal alveolar concentration is used to determine potency
defined as the % concetration in the administered air that produces no response to surgical incision in 50% of the subjects
21- T or F: blood:gas partition coefficient, blood:brain partition coefficient, and rate of uptake and elimination are all characteristic of the potency of gaseous gen anesthetics?
false. these are all measures of the characteristics of anesthetics, but do NOT give the potency
21- which inhalational anesthetic can only provide anesthetic effectiveness under hyperbaric conditions?
nitrous oxide (NO), which also has the fastest rate of induction. it is often used for dental procedures (i think this is laughing gas?)
21- muscle rigidity can be a side effect of which IV anesthetic?
fentanyl.
potent opioid agonist given as part of balanced anesthesia. it can cause chest-wall (truncal) regidity bc of interation in the striatum
22- clinical antipsychotic potency for "typical" antipsychotics correlate with actions at which receptor?
dopamine D2.
antipsychotic agents are classified as typical (older with actions at dopamine receptors) and atypical (primarily interact at 5HT receptors)
22- T or F: some of the adverse effects of typical antipsychotic agents are mediated by alpha2 adrenoceptors and muscarinic receptors
T
22- do serotonin receptors correlate to the efficacy of typical or atypical antipsychotics?
atypical
22- what drug is an antipsychotic that can improve both positive and negative symptoms of schizophrenia?
risperidone.
unique dual-acting antipsychotic agent that is an antagonist at both D2 and 5HT2 receptors.
22- what do chlorpromazine, haloperidol, thiothixene, and thioridazine have in common?
they are all older, typical antipsychotics that block dopamine receptors, but with no appreciable affinity for 5 HT receptors
22- which of the following is NOT a class of antidepressants?
- heterocyclic antidepressants
- TCAs
- MAOIs
- acetylcholinesterase inhibitors
- SSRIs
acetylcholinesterase inhibitors, aka indirect-acting choliergic agonist, increase the synaptic concentration of Ach, used in tx of dementia of alzheimer's disease
22- what are some adverse effects of the older TCAs?
orthostatic hypotension
sedation
seizures
weight gain

(NOT: sexual dysfxn)
22- sexual dysfuction is i side effect of which drug class?
SSRIs
the newer SSRIs, like fluoxetine, can produce priapism & impotency
22- foods containing tyramine should be avoided with ___ .
MAOIs, which irreversibly inhibit monoamine oxidase, the enzyme that degrades biogenic amine neurotransmitters. this elevates the levels available of release. tyramine in food is not degrade bc MAO enzyme is blocked--
hypertensive crisis might ensue
23- most clinically used opioid analgesics are selective for which type of opioid receptor?
mu receptors. kappa and delta are also a type of opioid receptor that can mediate analgeia, but kappa only plays a minor role with the action of some mixed agonist-antagonist opiods, and delta selective agents have not surfaced in the clinic yet.
23- why does codeine have a greater oral bioavailability compared with morphine?
codeine undergoes less first-pass metabolism. codeine is methylmorphine with the methyl group at the 3 position, the principle site of glucuronide metabolism of morphine. the codeine molecule is therefore somewhat protected from the first-pass effect of hepatic metab.
23- T or F: morphine is conjugated more quickly than codeine
true
23- T or F: codeine is more likely to cause nausea and vomiting in ambulatory patients because opioids increase vestibular sensitivity.
false
morphine is more likely to cause nausea in ambulatory patients compared to reumbent patients bc of an increased vestibular sensitivity
23- does morphine or codeine stimulate "chemoceptor trigger zone" neurons?
morphine
23- does morphine inhibit or induce cough center neurons?
inhibit
23- which opioid is so lipophilic that it is marketed in a skin patch used to treat chronic pain?
fentanyl
23- what two other drugs in this section come in a transdermal patch?
naltrexone & scopolamine
naltrexone is an opioid antagonist used to treat opioid and alcohol dependence.
scopolamine is used for motion sickness
23- why can naloxone be given in repeated doses in the case of an opioid overdose?
naloxone may have a shorter half-life than the opioid agonist. tx of opioid od often required repeated doses of naloxone or continuous IV to compete with the agonist at the receptor.
24- list some mechanisms of action for antiparkinsonism agents
- direct dopamine agonist
- precursor loading
- inhibit dopamine metabolism
- block cholinergic receptors
24- T or F: another mechanism for antiparkinsonism agents is selective dopamine reuptake inhibition
false.
no agents currently available, although it would be a beneficial tx bc it would lead to an increase in synaptic levels of dopamine
24- what is the mechanism of action of bromocriptine?
direct dopamine agonist
24- what is the mechanism of action of L dopa?
precursor loading
24- what is the mechanism of selegiline, an antidepressant also used for the tx of parkinson's?
inhibit dopamine metabolism by selecive MAO-B inhibition. retards the progress of parkinsonism by inhibiting the formation of free radicals from the acion of MAO-B on dopamine
24- what is a mechanism of action of benztropine?
block cholinergic receptors
24- why are cardiac arrhythmias occasionally observed
follow initial dose of L dopa?
direct beta adrenoceptor stimulation by dopamine from metabolism of L dopa to dopatmine. administration of L dopa with carbidopa with decrease the formation of dopamine in the periphery and decrease the likelihood of cardiac abnormalities
24- anticholinergic agents are useful in the tx of parkinosonism bc ___ .
neurotransmitter imbalance in the basal ganglia. the decrease of dopamine projections to the striatum results in a relative abundance of Ach activity.muscarinic antagonists rebalance this
24- what drug causes an increase release of dopamine vesicles?
amantadine (symmetrel)
livedo reticularis (spider veins)
24- baclofen is used to tx muscle spasticity bc ___ .
it is a receptor agonist at GABA B receptors, and is presently the only GABA B receptor agonist approved for the tx of spasticity.
24- what drugs increase GABA action at Cl- ion channels?
sedative-hypnotic agents
what is the drug of choice for absence seizures?
ethosuximide.
a unique adverse effect is hiccoughs
some benzos are used in epilepsy.. what types of seizures are the following used for:
diazepam & lorazepam
Clonazepam
Clorazepate
Diazepam & Lorazepam = status epilepticus
Clonazepam = absence & myoclonic seizures
Clorazepate = partial seizure adjunct
21- which inhaled anesthetic can produce hepatic toxicity?
halothane
21- what is a adverse rx of enflurane?
seizures
21- what is the preferred anesthetic for neurosx?
isoflurane.
this is also the most widely used halogenated inhaled anesthetic at this time (or, whenever this book was printed)
21- what inhaled anesthetic can be used for OB, but can produce fatal nephrotoxicity?
methoxyflurane.
it has a very rapid induction, it is the most potent inhaled anesthetic, but can only be used in short duration (ex: before each labor contration "inhale a hit of metho")
21- why can N2O not be used solely?
MAC is too high (>100)
used for dental procedures
rapid induction (low blood:gas)
25- how does disulfiram (Antabuse) work to tx alcohol dependence?
disulfiram increases circulating acetaldehyde concentrations by inhibiting acetaldehyde dehydrogenase, producing flushing, nausea, and vomiting with concurrent alcohol administration.

basically- if you drink with disulfiram, you get sick
negative reinforcement
23- how do opioids depress respiration?
opioid act directly at the medulla by reducing responsiveness to CO2.
depression of all phases of resp.
25- the degree of of reinforcement for heroin is greater than morphine because ___ .
heroin is distributed more rapidly to the brain.

diacetylmorphine (heroin) is more lipophilic and crosses the BBB faster than morphine
25- name some health hazards of chronic marijuana abuse
- low birth weight in neonates
- decreased testosterone
- anovulatory cycle
- increased fetal malformations
25- T or F: THC in marijuana shows promise as a tx for glaucoma
true
Dronabinol (Marinol) FDA approved formulation of THC
- decrease intraocular pressure in glaucoma pts
- anti-emetic in chemo pts
- appetite stimulant in AIDS pts
25- synesthesia is an effect of which drug of abuse?
LSD
sounds have color &
color has sound
25- crack cocaine is worse than powder cocaine why?
reinforcement is greater with inhalation versus insufflation

aka- snorting is better than smoking, even though the cocaine molecules have the same potency
25- what new drug inhibits ADH alcohol dehydrogenase, for tx of methanol or ethylene glycol poisoning?
fomepizole (Antizol)
blocks ADH
25- what is the order of approach to the tx of alcoholism? (3 drug steps)
1. disulfiram (Antabuse)
2. naltrexone (comes in a skin patch, too)
3. acamprosate calcium (Campral)
25- what is the standard drug tx of methanol or ethylene glycol tox?
IV ethanol-
this is standard tx. ethanol effectively competes for enzymes.

also- fomepizole (Antizol) is a new drug used for methanol or ethylene glycol tox- inhibitor of ADH
25- MDMA, aka ecstasy, is neurotoxic to which type of neurons?
serotonergic neurons
25- what is the mech of action of cocaine?
blocks transporter (re-uptake) of NE, DA
25- what is the mech of action of caffeine?
presynaptic adenosine receptor antagonist
(increases dopamine release)
25- what is the mech of action of nicotine?
agonist at CNS nicotinic cholinergic receptors
25- T or F: nicotine is an MAOI
false.
cigarette smoke, not nicotine, is an MAOI
25- lorazepam is pharmacologic tx for which drug intox?
- amphetamines
- cocaine
- hallucinogens
- marijuana
- phencyclidine
25- which antipsychotic is used to tx psychosis in acute intoxication and for what drugs?
haloperidol
used in tx of amphetamine & phencyclidine intox