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71 Cards in this Set
- Front
- Back
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partial 5-HTAA agonist
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Buspirone
used in tx of GAD in a pt who does not need sedation or motor impairment |
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SE: sexual disturbance, bruxism, loss of libido
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SSRIs & SNRIs
start slow in pts with BPH |
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DOC for elderly with anxiety disorders
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Lorazepam, oxazepam (benzos)
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prototype, more lipophilic, longest acting, & produces a metabolite that extends its duration of action (benzo family)
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diazepam
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short acting benzos
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triazolam--- rapid onset to facilitate sleep
oxazepam |
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intermediate acting benzos
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alprazolam, lorazepam-- less likely to have hangover effects
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long acting benzos
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associated w/ hangover effect
diazepam, flurazepam, chlordiazepoxide, clorazepate |
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which benzo can be used as an anticonvulsant?
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diazepam
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used when pts have delirium tremors-- only txed in a hospital situation
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benzos
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which one is more GABAemetic at high doses barbiturates or benzos?
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barbiturates bc it binds directly to the binding site of the GABA receptor
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what does binding of GABA to receptors by benzos cause?
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opening of Cl channels allowing an increase in Cl conductance--> hyperpolarization--> inhibits formation of an action potential--> slows everything down.
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Benzos are highly _____, cross ____ rapidly and ______ significantly
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highly lipophilic
cross CNS rapidly redistribute significantly (get stuck in adipose tissue) |
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major metabolite of all benzos
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desmethyldiazepam (extends duration of benzos)
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extensively metabolized by CYP3A4 & CYPC2C19
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almost all benzos.
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which benzo is NOT metaboilzed by CYP?
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clorazepate which is decarboxylated in gastric juice to desmethyldiazepam
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which benzo has the highest incidence of causing anterograde amnesia?
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diazepam (date rape)
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flumazenil
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reverses the sedative effects of benzos by displacing benzos from receptors. Used in benzo overdose.
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benzo's cautious use in 3rd trimester pregnancy why?
1st trimester tetralogy? |
associated w/ floppy baby
1st tri: cleft lip & palate |
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benzos are CI when?
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during nursing
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what can you never ever ever mix with a benzo?
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alcohol and all other CNS depressants (antipsychotic agents, TCA's, opioids)---> respiratory depression, coma, death
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what 7 drugs/ substances inhibit CYP3A4?
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erythromycin
clarithromycin ritonavir itraconozole ketoconazole nefadozone grapefruit juice |
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if your pt has to be on a benzo and a CYP3a4 inhibitor, what benzo should they be on?
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lorazepam or oxazepam
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what is the safest drug to use in anxiety in a pregnant or breast feeding pt?
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buspirone
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rifamin is a CYP450 _____
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inducer
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what are the 2 sedative hypnotics benzodiazepine receptor agonists?
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zolpidem, zaleplon
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if you pt is specifically looking for a way to tx his insomnia short term, what would you prescribe him?
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BZ agonists (zolpidem, zaleplon)
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how do you tx
a) panic attacks b) sxs of sympathetic overdrive c) GAD long term |
a) Benzos
b) B-blockers c) Benzo + antidepressant (SSRI, SNRI) |
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Where do the major noradrenergic tracts come from and project to?
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locus coeruleus--> cortex, cerebellum & spinal cord
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where does the median forebrain bundle arise from?
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lateral tegmental area and projects into the diencephalon (thalamus/ hypothalamus) & spinal cord
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where do the serotonergic neurons arise from and project to? what are these neurons involved in?
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Raphe nuclei (in pons & medulla) and project throughout the cortex, cerebellum & spinal cord.
involved in sensory gating & perception- role in mood, motivation, depression, anxiety, compulsion, psychosis |
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what 3 receptors are consistently down-regulated following long-term antidepressant therapy?
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alpha 2, beta 1 and 5-HT2
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1) too little ____ causes schizophrenia
2) too little ____ causes OCD 3) too little _____ causes parkinson's 4) too little ______ causes seizures 5) too little ____ causes Alzheimer's 6) too much _____ causes chorea 7) too much ______ causes sleep 8) too much _____ causes seizures 9) too much _______ causes CNS depression 10) too much ______ causes delirium |
1) glutamate
2) Serotonin 3) Dopamine 4) GABA 5) Acetylcholine 6) Dopamine 7) Serotonin 8) Glutamate 9) GABA 10) Acetylcholine |
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when you need to identify a GABA neuron, what enzyme do you need to look for?
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glutamic acid decarboxylase which is responsible for converting glutamate to GABA.
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what is the precursor for both IPSPs and EPSPs
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glutamine
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what are the 3 ionotropic glutamate receptors and the 3 metabotropic glutamate receptors? activation of these receptors cause?
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ionotropic: AMPA, kainate and NMDA---> causes increase in na and calcium influx
metabotropic: mGluRs: Gr1 (mGluR1, 5-activates PLC--- autoreceptors or heteroreceptors--- presynaptic) Gr2 (mGluR 2,3- inhibit adenylate cyclase) Gr3 (mGluR 4-8-- inhibit AC- autoreceptor or hetero receptor... presynaptic) |
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what causes calcium influx and the release of glutamate?
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depolarization of the presynaptic terminal
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what three categories of drugs reduce AMPA activation?
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Alcohol, barbiturates & volatile anesthetics---> inhibitors
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each receptor is made of five subunits and each subunit is one of the 3 predominant subtypes (alpha, beta or gamma).
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GABAa receptor
most abundant GABA receptor in CNS |
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what does an activated GABAa receptor cause?
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chloride influx which hyperpolarizes the postsynaptic cell making it less excitable
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what are the 2 largest classes of drugs that act at allosteric modulator binding sites to enhance GABAergic transmission?
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barbiturates and benzos
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benzo or barbiturate
which one keeps the channel open longer and which one opens it more frequently? |
open longer: barbiturates
more frequently: benzos |
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where are GABAb receptors expressed? what are they?
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spinal cord: heterodimer of GABAb1 and GABAb2.
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what does the GABAb receptor activate? what is the en effect?
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G proteins that are either directly coupled to K+ and calcium channels or coupled through effector protein.
end effect: inc K+ efflux= longer, slower IPSPs and dec in calcium influx--> reduced NT release presynpatically. --> blocks the response of the cell. |
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selective GABAb agonist currently used as a muscle relaxant
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baclofen
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what two categories of drugs block voltage gated sodium channels?
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local anesthetic: lidocaine
antiepileptics: Carbamazepine, phenytoin, valoproic acid |
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what is the goal of an anti-epileptic medication?
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inhibiting spread of impulse
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anxiety & insomnia are associated with ____ serotonin levels and ____ NE level sin the brain?
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dec and incr
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what spikes right before you wake up?
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the noradrenergic pathways--> locus ceruleus releasing NE
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serotonergic projections from the midbrain project to ______, pons ramify in the _____ & _____ and those in the medulla supply _______
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1) cerebral hemispheres
2) brainstem & cerebellum 3) spinal cord |
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what is the main complaint assoc w/ drugs that affect the serotonergic projections in the CNS?
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change in appeptite
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what is the precursor for dopamine & NE? What is the precursor for serotonin?
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dopamine and NE= tyrosine
serotonin= tryptophan |
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which noradrenergic receptor causes a dec in cAMP?
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alpha 2
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what 5-HT receptor is used to tx anxiety, depression and pain? which one is used to relieve migranes?
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1a and 1d
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what 5-HT receptor causes hallucinations when overactivated? what 5- HT receptor causes inc appetite?
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5-HT2a and 5-HTc
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what are the two categories that the dopaminergic projections fall into?
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1) those that arise from substantia nigra
2) those that arise from ventral tegmental nuclei and project to frontal lobe and to nucleus accumbens |
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what disease is caused by excess activity in the dopaminergic pathway?
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schizophrenia
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where are the excitatory dopaminergic receptors located?
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D1- striatum, neocortex
D5- hippocampus & hypothalamus (Ca mobilization & PKC activation) |
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where are the inhibitory dopaminergic receptors located?
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D2- striatum, SNpc, pituitary
D3- olf tubercle, n. accumbens, hypothalamus D4- frontal cortex, medulla, midbrain (dec cAMP and incr K+ currents |
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what G protein corresponds with what Histamine receptor?
H1 H2 H3 |
H1- Gq (incr IP3 and DAG)
H2- Gs (incr cAMP) H3- inhibitory Gi |
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what relays the peripheral transmission signal to CNS neurons and sends it to the brain?
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the dorsal horn
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what do NE & GABAb block? what does it cause?
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calcium influx causing you to feel the sensation of pain
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what are the 3 main opioid receptors? what are they each responsible for?
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mu- respiratory depression, euphoria, analgesia, physical dependence
kappa- sedation, analgesia, miosis delta |
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what major drug classes work at these sites of action:
1) central perception 2) conduction 3) Transmission 4) signal transduction |
1) opioids
2) Na channel blockers 3) opioid, antidepressants, NSAIDs, anticonvulsants, alpha 2 adrenergic agents 4) NSAIDs |
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name the 4 TCA drugs. what is their MOA? AE?
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imipramine, desipramine, amitriptyline, nortriptyline
MOA: block NE & varying activity @ SERT; prevent reuptake 1 (no granules). AE: anticholinergic effects (xerostomia, hydrosis, constipation), orthostatic hypotension, sedation (H1 blockade), seizures, cardiac conduction, weight gain, sexual dysfunction (less than SSRIs) |
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which TCA is used for enuresis? which one is used for neuropathic pain which one is used in the elderly? which one causes seizures & how?
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enuresis: impiramine
neuropathic pain: amitriptyline elderly: nortriptyline Seizures: desipramine (d/t decreased seizure threshold. |
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what drug/ drug interaction with TCA will cause hypoglycemia? what about an increase in therapeutic and toxic effects? increased risk of CNS depression?
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hypoglycemia: d/t insulin or an oral hypoglycemic agent
inc therapeutic: MAOI CNS depression: ETOH |
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These drugs are more active at SERT than NET and have similar AEs to sim to TCAs but less severe
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SNRI's & SSRI's
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name the 3 SNRI's. which one is metablized by CYP450 and you should avoid in hepatic insufficiency or ESRD?
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venlafaxine, desvenlafaxine, duloxetine
duloxetine: cyp450, avoid etc |
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what are the 5 SSRI's. what is the MOA of SSRI's? AE?
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Citalopram, Fluoxetine, Paroxetine, Sertraline, Escitalopram
MOA: blocks ONLY SERT (inc levels of 5HT) AE: dec affinity for cholinergic- adrenergic - H1 receptors, MC GI effects d/t excess 5-HT, sexual dysfunction, HA, |
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what SSRI can cause akathesia? which one has the longest 1/2 life?
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fluoxetine to both
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what drug/ drug interaction with SSRI's can increase seizures? what affect does SSRI have w/ CNS depressants?
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clozapine
synergistic sedative effects w/ other CNS depressants |
