Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
204 Cards in this Set
- Front
- Back
|
From a clinical perspective, what is the most important class of peptide NTs?
|
opioids (just know they are peptides)
|
|
|
Where are the cell bodies of glutamate neurons?
|
Entire CNS
|
|
|
Where are the cell bodies of GABA producing neurons?
|
Entire CNS
|
|
|
Where are the cell bodies of ACh producing neurons?
|
1. Spinal cord anterior horn
2. ANS preganglionic nuclei 3. Parasympathetic ganglia 4. Basal ganglia |
|
|
Where are the cell bodies of NE producing neurons?
|
1. Sympathetic ganglia
2. Pons: Locus ceruleus |
|
|
Where are the cell bodies of Dopamine producing neurons?
|
Midbrain (SN)
|
|
|
Where are the cell bodies of Serotonin producing neurons?
|
Midbrain and pons
|
|
|
Where are the cell bodies of histamine producing neurons?
|
Hypothalamus and midbrain
|
|
|
Where are the cell bodies of glycine producing neurons?
|
Spinal cord and possibly brain stem and retina
|
|
|
Where are the cell bodies of peptide producing neurons?
|
Entire CNS
|
|
|
What are the main actions of glutamate?
|
excitatory neurotransmission
modulation of synaptic plasticity activation of 2nd msgers |
|
|
What are the main actions of GABA?
|
inhibitory neurotransmission
|
|
|
What are the main actions of ACh?
|
1. Muscle contraction
2. Autonomic fcn 3. Parasympathetic fcn 4. Neuromodulation |
|
|
What are the main actions of NE?
|
1. Sympathetic function
2. Neuromodulation in the pons |
|
|
What are the main actions of dopamine?
|
Neuromodulation
|
|
|
What are the main actions of serotonin?
|
Neuromodulation
|
|
|
What is the main action of histamine?
|
Mainly excitatory neuromodulation
|
|
|
What is the main action of glycine?
|
inhibitory neurotransmission
|
|
|
What is the main action of peptide NTs?
|
Neuromodulation
|
|
|
T or F: Opioids work on both the perception and interpretation of pain
|
TRUE
|
|
|
Name 4 amide local anesthetics
|
1. lidocaine
2. bupivacaine 3. mepivacaine 4. ropivacaine Remember there is an "i" before the -aine |
|
|
Name 2 ester local anesthetics
|
1. procaine
2. benzocaine |
|
|
What is the primary MOA of local anesthetics?
|
block Na+ channels preventing generation and conduction of Aps in nerve fibers
|
|
|
What determines the speed of onset of local anesthetics?
|
The pKa of the drug and the pH of the tissue
|
|
|
Why is it difficult to numb necrotic tissue?
|
b/c it is acidic and thus prevents the drug from becoming the active form
|
|
|
The toxicity potential of a local anesthetic is directly proportional to its __
|
lipid solubility
|
|
|
If significant systemic absorption occurs, all local anesthetics will cause __, __ and __
|
cardiotoxicity, arrhythmias, and death
|
|
|
What prolongs the duration of local anesthetics?
|
epinephrine
|
|
|
Where are amide LAs metabolized?
|
in the liver
|
|
|
What is a bad SE of esters that make them unpopular in clinical use?
|
allergic rxn including methemoglobinemia
|
|
|
What are two situations to use ester LAs?
|
1. Benzocaine is used as a topically anesthetic
2. Tetracaine and procaine are used when the pts liver dz prohibits the use of amides. |
|
|
How and where are most ester local anesthetics metabolized?
|
in the serum by pseudocholinesterases (very fast)
|
|
|
Name 5 IV general anesthesia drugs
|
1. Thiopental
2. Propofol 3. Ketamine 4. Fentanyl 5. Dantrolene |
|
|
Which IV general anesthetic should you use if the pt has a risk of malignant hyperthermia?
|
Dantrolene
|
|
|
What class of drug is Thiopental?
|
barbiturate
|
|
|
What class of drug is ketamine?
|
NMDA blocker. It produces dissociative anesthesia (sedation, analgesia, amnesia, dissociation from surroundings)
|
|
|
Which IV GA drug produces dissociative anesthesia?
|
ketamine
|
|
|
What class of drug is fentanyl?
|
opioid
|
|
|
What causes malignant hyperthermia?
|
1. succinylcholine
2. volatile anesthetics |
|
|
What are some sx of malignant hyperthermia?
|
extreme muscle rigidity
|
|
|
Name 2 inhaled anesthetics
|
Nitrous oxide and halothane
|
|
|
What is the MOA of inhaled anesthetics?
|
They enhance the binding of GABA --> greater Cl- entry --> cell is hyperpolarized --> difficult to depolarize and fire AP
|
|
|
How do you quantify the potency of inhaled anesthetics?
|
median alveolar concentration (MAC). it is the median effective dose
|
|
|
MAC is __ proportional to the potency of the inhaled anesthetics
|
inversely
|
|
|
What are the main opioid receptors?
|
mu, kappa, delta
|
|
|
What are the main actions of opioids?
|
analgesia, euphoria, N/V, constipation, urinary retention, small pupils, sedation, itching, resp depression, addiction, withdrawal
|
|
|
What are 6 strong opioid agonists?
|
Morphine
oxycodone methadone heroine fentanyl meperidine |
|
|
What are 2 medium opioid agonists?
|
hydrocodone, codeine
|
|
|
What is a weak opioid agonist?
|
tramadol
|
|
|
What is a mixed opioid agonist/antagonist?
|
buprenorphine
|
|
|
What are two opioid antagonists?
|
naloxone and naltrexone
|
|
|
What are the major therapeutic uses of opioids?
|
pain, diarrhea, cough
|
|
|
Why is morphine usually given in shots?
|
it has variable oral absorption and significant first pass metabolism
|
|
|
__ is a synthetic opioid which is similar to morphine but is preferred in labor and rarely causes seizures
|
meperidine
|
|
|
Which opioid is good for short-term severe pain (like a fracture) but is also abused?
|
oxycodone
|
|
|
Why opioid is very short acting and frequently used in IV anesthesia and as a patch in terminal cancer pts
|
fentanyl
|
|
|
__ is well absorbed orally; has mild w/d; used for severe pain and heroine w/d
|
methadone
|
|
|
__ is an illicit opioid taken IV and assoc w/ exaggerated eurphoria
|
heroine
|
|
|
__ is less potent than morphine, has good oral absorption, and used for moderate pain and cough suppression
|
codeine
|
|
|
Which opioid is less potent than morphine and frequently used for moderate pain in the ambulatory setting?
|
hydrocodone
|
|
|
__ is a weak agonist used for mild pain
|
tamadol
|
|
|
What opioid antagonist is used to treat opioid OD?
|
naloxone
|
|
|
Which opioid antagonist is used for EtOH-ism treatment?
|
naltrexone
|
|
|
Which mixed agonist/antagonist is used to treat opiate dependence?
|
buprenorphine
|
|
|
NSAIDs inhibit __ production
|
prostaglandin
|
|
|
Why can't pregnant people take NSAIDs?
|
they cause closure of the ductus arteriosus
|
|
|
What are some SE of benzos?
|
sedation/confusion
resp. depression addiction w/d can cause seizure and death |
|
|
When should benzos be avoided?
|
liver dz and glaucoma
|
|
|
T or F: Buspirone has low potential for dependence
|
TRUE
|
|
|
What is buspirone used for?
|
generalized anxiety d/o
|
|
|
What is the MOA of buspirone?
|
mediated by serotonin (5-HT) receptors
|
|
|
What are two barbiturates used today?
|
Phenobarbitol for epilepsy
Thiopental for anesthesia |
|
|
What is a GABA receptor antagonist used for reversing the effects of benzos?
|
flumazenil
|
|
|
What is a long-acting benzo that is used for epilepsy, sleep d/o, and anxiety d/o?
|
Clonazepam
|
|
|
What are 4 medium acting benzos?
|
Alprazolam (Xanax)
Diazepam (Valium) Lorazepam (Ativan) Temazepam (Restoril) |
|
|
What is lorazepam used for?
|
status epilepticus and sedation for procedures
|
|
|
What are 2 short acting benzos?
|
oxazepam (alcohol detox)
midazolam (anesthesia and status epilepticus) |
|
|
What are 3 non-benzos that help you sleep by acting on a subset of the benzo receptors?
|
Zolidem (Ambien)
Zalepon (Sonata) Eszopicolone (Lunesta) |
|
|
Which sleep aid acts on melatonin receptors?
|
Rameltion
|
|
|
What medium acting benzo is used for short term Rx of insomina?
|
Temazepam
|
|
|
Chronic EtOH increases RR for all cause death by __
|
at least 50%
|
|
|
90-95% of EtOH is oxidized to __ in the liver by __
|
acetaldehyde by EtOH dehydrogenase
|
|
|
Describe the metabolism of ethanol
|
EtOH --> acetaldehyde --> acetate --> fatty acids, ketone bodies, cholesterol
|
|
|
What is Disulfiram?
|
A drug that is toxic when taken w/ EtOH...they get so sick that they don't want to drink anymore (suposedly)
|
|
|
How does Disulfiram work?
|
it blocks aldehyde dehydrogenase so acetaldehyde builds up and causes sickness
|
|
|
What are the most commonly used drugs for mood stabalization in Bipolar d/o?
|
1. Lithium
2. Carbamazepine 3. Valproic acid 4. Lamotrigine |
|
|
What is the MOA of lithium?
|
unknown
|
|
|
What are some common adverse rxns of lithium?
|
HA, dry mouth, polydipsia, polyuria, polyphagia, GI distress (GIVE W/ FOOD), tremor, hypothyroidism, sedation ,etc.
|
|
|
What is the effect of lithium on normal individuals?
|
there is no effect!
|
|
|
Name 5 AEDs
|
1. Phenobarbitol
2. phenytoin 3. carbamazepine 4. valproic acid 5. ethosuximide |
|
|
How are the AEDs metabolized?
|
hepatically by CYP P-450
|
|
|
What drugs must you be careful w/ when a pt is on an AED?
|
Warfarin and isoniazid
|
|
|
What do you use ethosuximide for?
|
Absence seizures (t-type Ca++ channels)
|
|
|
Which AEDs are P450 inducers making other drugs metabolized by P450s lower in []?
|
Carbamazepine, phenytoin and phenobarbitol
|
|
|
Which AED is a P450 inhibitor --> other P450 drugs get higher in []
|
valproic acid
|
|
|
Which class of drugs cause bone marrow suppression?
|
AEDs
|
|
|
What are some SE of AEDs?
|
carbamzepine lower WBC
valproate lowers platelets other bone marrow suppression hepatotoxicity (kids get liver failure w/ valproate) significant hypersensitivity rash teratogens (valproate --> NTDs) osteopenia (phenytoin) |
|
|
Major SE of phenytoin -->
|
gingival hyperplasia
|
|
|
Major SE of valproic acid -->
|
massive weight gain
|
|
|
Major SE of phenobarb -->
|
hyper and stupid
|
|
|
What is the MOA of Phenobartbitol?
|
blocks Na+ channels
facilitates GABA modulates Glutamate |
|
|
What is the MOA of Phenytoin?
|
blocks Na+ channels
|
|
|
What is the MOA of Carbamazepine?
|
blocks Na+ channels
|
|
|
What is the MOA of Valproic acid?
|
blocks Na+ channels
increases brain levels of GABA |
|
|
What is the MOA of ethosuximide?
|
blocks T-type Ca++ channels
|
|
|
What are 2 AEDs that are good for pts w/ hepatic failure?
|
Leviteracetum and gabapentin
|
|
|
Gabapentin is often used off label for what?
|
neuropathic pain
|
|
|
Lamotrigine is often used for what?
|
bipolar d/o
|
|
|
Topiramate is used for what?
|
preventing migraines and weight loss (but makes you stupid)
|
|
|
Where is dopamine produced?
|
SN
ventral tegmentum of brainstem |
|
|
Where is NE produced in the CNS?
|
locus ceruleus of brainstem
|
|
|
Where is Histamine produced in the CNS?
|
hypothalamus
|
|
|
Where is serotonin produced in the CNS?
|
Raphe nucleus of brainstem
|
|
|
Name 2 TCAs
|
1. Amitriptyline
2. Imiprimine |
|
|
Name 4 SSRIs
|
1. Fluoxetine
2. Citalopram 3. Sertraline 4. Paroxetine |
|
|
Name 1 SNRI
|
Venlafaxine
|
|
|
Name 2 MAOIs
|
Tranylcypromine and Phenelzine
|
|
|
Name 2 atypical antidepressants
|
Burproprion
Trazodone |
|
|
What is the MOA of buproprion?
|
blocks re-uptake of NE and DA
|
|
|
What is the MOA of trazodone?
|
blocks post-synaptic 5HT receptors
|
|
|
What is the MOA of MAOIs?
|
inhibit the breakdown of NE and 5HT
|
|
|
Which antidepressant can cause seizures and should be avoided in pts w/ epilepsy?
|
buproprion
|
|
|
What are some SEs of TCAs?
|
dry mouth, constipation, urinary retention, blurred vision, arrhythmia, N/V, sedation
|
|
|
What is a serious SE of MAOIs?
|
Hypertensive crisis if foods high in tyramine are ingested (wine, cheese, chocolate, aged meat, etc.)
|
|
|
What are some SE of SSRIs?
|
sedation, N/V, drug interactions, sexual dysfunction, sleep disturbance
|
|
|
What is a life-threatening adverse rxn that can happen with antidepressants?
|
serotonin syndrome (get cognitive, autonomic, and somatic effects)
|
|
|
__ is a TCA used for chronic pain, migraine, and depression
|
Amitriptyline
|
|
|
__ is a TCA used for bed wetting and depression
|
Imipramine
|
|
|
__, the prototypial SSRI is used for depression and anxiety
|
Fluoxetine
|
|
|
__ is an SSRI that is helpful in chronic pain and HA
|
Citalopram
|
|
|
__ is a SSRI that has less subtle cognitive effects
|
Sertraline
|
|
|
This SSRI has a tendency to cause weight gain
|
Paroxetine
|
|
|
__ is an SNRI used for HA, neuropathic pain, depression and anxiety w/ less weight gain than SSRIs
|
Venlafaxine
|
|
|
This drug is similar to SSRIs but does not cause weight gain, sedation or sexual dysfunction
|
buproprion
|
|
|
This very sedating antidepressant can cause priapism
|
Trazodone
|
|
|
Why are MAOIs not routinely used?
|
potential for serious adverse effects
|
|
|
What are 2 therapeutic CNS stimulants?
|
amphetamine and methylphenidate
|
|
|
What are the 2 legal uses of amphetamines?
|
ADHD and narcolepsy
|
|
|
What is the MOA of CNS stimulants?
|
affects on vesicular monoamine transporters
|
|
|
What is the MOA of caffeine?
|
It's a CNS stimulant that works as an adenosine receptor antagonist (leads to increased intracellular cAMP)
|
|
|
What is the MOA of nicotine?
|
CNS stimulant giving effect at locus ceruleus and reward effect at limbic system
|
|
|
What is the MOA of cocaine?
|
blocks monoamine reuptake transport into nerve terminals; Na+ channel blocker
|
|
|
What is the MOA of methamphetamine (Crystal meth)?
|
Stimulant that blocks reuptake of dopamine (look out for meth mouth)
|
|
|
What is the MOA of MDMA (ecstasy, X)?
|
Causes release of serotonin, dopamine & NE. Produces distorted sense of time & perception, facilitates interpersonal communcation and sex enhancer
|
|
|
What is the MOA of Lysergic Acid (LSD)?
|
hallucinogen that binds to a specific 5HT post synaptic receptor
|
|
|
What is the MOA of phencylclidine (PCP, angel dust)?
|
hallucinogen that blocks NMDA-type glutamate receptors
|
|
|
What is the MOA of THC (marijuana)?
|
cannabinoid receptor agonist
|
|
|
What is the gold std of Rx of PD?
|
Carbidopa + Levadopa
|
|
|
What are some SE of Levodopa/carbidopa?
|
Psychosis
N/V dyskinesias |
|
|
Why do you give carbidopa and levodopa together?
|
b/c carbidopa prevents the L-dopa from being metabolized in the periphery
|
|
|
What are some dopamine agonists used to treat PD?
|
bromocriptine and pramipexol
|
|
|
What is an MAO-B inhibitor used to treat PD?
|
selegiline
|
|
|
What drug increases release of dopamine to treat PD?
|
amantidine
|
|
|
What anticholinergic drug is used to treat PD?
|
trihexylphenidyl
|
|
|
What environmental toxicant can cause parkinsonism?
|
MPTP
|
|
|
T or F: Defects in Golgi function are thought to potentiate Parkinson's disease
|
False. Defects in mitochondrial function
|
|
|
D1 receptors mediate the __ pathway
|
direct
|
|
|
The direct pathway gives the __ signal
|
go
|
|
|
D2 receptors mediate the __ pathway
|
indirect
|
|
|
The indirect pathway gives the __ signal
|
no go
|
|
|
What is the RLS in dopamine biosynthesis?
|
Tyrosine-3-mono-oxygenase
|
|
|
Why do you give L-Dopa instead of Tyrosine (the precursor to L-Dopa)?
|
b/c there is a deficiency of tyrosine-3-mono-oxygenase
|
|
|
Give the steps in the biosynthesis of dopamine.
|
tyrosine --> L-DOPA --> Dopamine --> homovanillic acid (by MAO)
|
|
|
How is L-DOPA converted to dopamine done?
|
aromatic amino acid decarboxylase (remove COOH from L-DOPA)
|
|
|
What degrades dopamine?
|
MAO-B
|
|
|
Why do you give a Carbi-DOPA (and MAOI) w/ L-DOPA?
|
b/c dopamine is rapidly broken down by MAO in the liver. Carbi-DOPA blocks the MAO in the liver and lets all the L-DOPA get to the brain.
|
|
|
What receptor do most parkinson's drugs work on?
|
D2
|
|
|
What does dopamine do in the pituitary gland?
|
prolactin inhibitory factor
|
|
|
What is NMDA?
|
a glutamate receptor (these are in the basal ganglia)
|
|
|
What is the function of NMDA receptor blockers?
|
block inhibitory GABA-ergic neurons going into the basal ganglia
|
|
|
Why do you inhibit DOPA-decarboxylase?
|
b/c DOPA-decarboxylase in the liver. You want to inhibit the peripheral enzymes.
|
|
|
What does carbidopa do?
|
inhibits DOPA-decarboxylase
|
|
|
T or F: D2 antagonists alone can cause acute parkinsonism
|
TRUE
|
|
|
How does MPTP cause PD?
|
it is taken up in the dopaminergic neurons and metabolized to MPP+ which is highly oxidative and causes death of the neurons.
|
|
|
__ in the mesolimbic dopamine system leads to sx such as auditory & visual hallucinations
|
overactivity
|
|
|
__ in the mesolimbic dopamine system leads to negative sx, affective sx, and cognitive sx
|
underactivity
|
|
|
Name 5 antipsychotic drugs
|
1. Chlorpromazine
2. Haloperidol 3. Risperidone 4. Clozapine 5. Olanzapine |
|
|
Name 2 first gen antipsychotics
|
Chlorpromazine (low potency) and haloperidol (high potency)
|
|
|
Name 3 second gen antipsychotics
|
Clozapine, Risperidone, Olanzapine
|
|
|
What is the MOA of 1st gen (typical) antipsychotics?
|
D2 receptor antagonism
|
|
|
What are the main SE of typical antipsychotics?
|
EPS (parkinsonism, tardive dyskinesia, etc.)
Elevate serum prolactin |
|
|
How do you treat the EPS assoc w/ typical antipsychotics?
|
anticholinergics
|
|
|
What is a major risk assoc w/ clozapine?
|
agranulocytosis
|
|
|
What are some SE of 2nd gen antipsychotics?
|
sedation, anticholinergic, ortheostatic hypotension, EPS, arrhythmias, etc.
|
|
|
What is the MOA of 2nd gen antipsychotics?
|
5HT/D2 antagonism
|
|
|
Which class of antipsychotics can cause significant weight gain and metabolic syndrome?
|
2nd gen
|
|
|
What do you treat acute attacks of migraines with?
|
5-HT receptor agonists (serotonergics: triptans and dihydroergotamine)
standard analgesics |
|
|
How does odansetron work for preventing nausea?
|
5HT blocker
|
|
|
What are some bad SE of triptans?
|
Elevation of BP and MI
|
|
|
What is a common SE of dihydroergotamine (DHE)?
|
nausea (treat w/ antiemetics)
|
|
|
What is the basic MOA of Alzheimer's drugs?
|
increase ACh
|
|
|
What are 3 drugs used to treat Alzheimer disease?
|
Donepezil, Rivastigmine, Memantine
|
|
|
What is the MOA of Donepezil and Rivastigmine?
|
ACh-esterase inhibitors (Used for Alzheimer's dz)
|
|
|
What is the MOA of Memantine?
|
Blocks some NMDA receptors linked to excitotoxicity (and thus cell death). Used for Alzeimer's dz
|
|
|
What are some SE of Donepezil and Rivastigmine?
|
N/V, diarrhea, muscle cramps, fatigue, insomnia, syncope
|
|
|
What are four drugs used for surgical paralysis?
|
1. Succinylcholine
2. Vecuronium 3. Rocuronium 4. Pancuronium |
|
|
What is the only depolarizing NMJ blocker used today?
|
Succinylcholine
|
|
|
What is the MOA of the non-depolarizing paralytics (-curoniums)?
|
competitively inhibit ACh at the NMJ
|
|
|
How can you reverse the effects of the non-depolarizers?
|
neostigmine
|
|
|
How can you reverse the effects of succinylcholine?
|
you can't!
|
|
|
Which drug is used exclusively for the "Tensilon test" to dx MG?
|
Edrophonium
|
|
|
What anticholinesterase is used for symptomatic treatment of MG?
|
pyridostigmine
|
|
|
What is the MOA of botulinum toxin?
|
blocks release of ACh
|
|
|
What is the clinical use of botulinum toxin?
|
wrinkles
torticollis and other dystonias |
