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Neuro Drugs > Week 2 - Neuro Drugs > Flashcards

Week 2 - Neuro Drugs Flashcards

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1
Q

oral sumatriptan

A

peak plasma concentration 1-2 hours, half life 1-3 hours, dose may be repeated in 1-2 hours, headache relief take 1-3 hours, metabolized by monoamine oxidase in the liver - for migraine

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2
Q

injectable sumatriptan

A

peak plasma concentration 12-15 min, half life 1-3 hours, dose may be repeated in 1-2 hours, headache relief takes 30 min, metabolized by monoamine oxidase in the liver - for migraine

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3
Q

nasal sumatriptan

A

peak plasma concentration of minutes to 1-2 hours, half life 1-3 hours, dose may be repeated in 1-2 hours, headache relief takes 30 min, metabolized by monoamine oxidase in the liver - for migraine

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4
Q

triptan drugs for cluster headache

A

bind to 5HT1b serotonin receptors, vasoconstriction = less pain from cluster headache

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5
Q

triptan drugs for cluster headache

A

binding to 5HT1a receptors in naple nucleus inhibit serotonergic neurons

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6
Q

sumatriptan

A

5HT1d (serotonin) receptor agonist, autoreceptor, blocks release of more serotonin

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7
Q

ergots

A

5HT1d and 5HT1b serotonin receptors, cause vasoconstriction, St. Anthony’s Fire???

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8
Q

triptans

A

cause vasoconstriction of cerebral vessels

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9
Q

buspirone

A

5HT1a serotonin receptor agonist, Tx depression and anxiety

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10
Q

TCA amitriptyline

A

blocks 5HT serotonin reuptake transporter

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11
Q

fluoxeine

A

inhibits 5HT serotonin reuptake transporter, Tx depression, anxiety, OCD

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12
Q

ondanseron

A

5HT3 serotonin receptor antagonist on vagal nerve, decreases nausea

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13
Q

good CNS drugs

A

bactericidal, small, lipophilic, low plasma protein binding, not ligand of brain efflux pumps; ex: rifampin, fluoroquinolones, 3rd gen cephalosporins; increased CNS penetration in newborns and with CNS inflammation; beta-lactam antibiotics block GABA binding –> seizures

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14
Q

ceftriaxone (3rd gen cephalosporin)

A

binds penicillin binding proteins (transpeptidases), streptococci, gram -, crosses BBB, inactivated by beta-lactamases, rx with calcium containing meds making crystals in lungs and kidneys, associated with C. diff

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15
Q

amphotericin B and Nystatin

A

antifungal, polyenes, binds ergosterol in cell membrane making holes, broad - yeast and mold, small excretion, long half life, liposomal form can cross BBB, nystatin (topical) binds cholesterol / decreases renal blood flow / destroys basement membrane, resistance - decreased ergosterol in membrane

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16
Q

Fluconazole, Itraconazole, Voriconazole, Posaconazole

A

antifungal, azoles, fluconazole and voriconazole CNS, binds P450 blocking production of ergosterol -> accumulation of lanosterol, dimorphic and yeast, oral, brain efflux pump substrate, hepatotoxic, neurotoxic, alters hormones, avoid during pregnancy, resistance altered P450 or increase brain efflux pumps, triazole - slow metabolism (low enzyme affinity)

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17
Q

Terbinafine (Lamisil)

A

antifungal, allyamines, inhibits squalene epoxidase -> accumulation of squalene, dermatophytes (skin, hair), topical

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18
Q

Flucytosine

A

antifungal, nucleic acid synthesis inhibitor, converted to 5-fluorouracil in fungi, yeast, oral, CNS, bone marrow suppression (follow pt cell count), resistance loss of enzyme or transporter, combine with amphotericin B to increase uptake

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19
Q

caspofungin

A

antifungal, fungins, echinocandins, inhibits cell wall by blocking beta-d-glucan polysaccharide synthesis, systemic Candida Albicans, IV, large molecule = no CNS, fever, rash at injection

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20
Q

pain

A

sensory and emotional with actual or potential damage

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21
Q

four steps of pain

A

initiated by stimulus, transmitted to brain, perceived as pain, produces reaction

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22
Q

local anesthetics

A

prevent transmission by reversible blocking nerve impulse locally, blocks somatic sensory / somatic motor / autonomic transmission, function returns

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23
Q

local anesthetics chemistry

A

weak bases (pKa 8-9), less ionized form if pH is higher, more ionized form if pH is lower

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24
Q

three segments of local anesthetics

A

hydrphobic lipophilic ring (potency, duration, toxicity), intermediate linkage (ester - allergic, amide, hydrophilic domain (amine - onset of action)

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25
routes of local anesthetic administration
topical (hard to pass through skin), peripheral nerve endings, nerve trunks (blocks), spinal cord (epidural), intravenous regional (limb w/ tourniquet)
26
local anesthetics absorption
injected into area, if accidentally injected vascularly can be toxic, use vasoconstrictor (epinephrine) to decrease absorption = more at site / longer duration / higher doses / less toxicity; too much vasoconstrictor can delay healing with tissue edema or necrosis
27
local anesthetics distribution
non-ionized is lipid soluble can cross membrane, ionized charged form inside cell clogs Na channels inside neuron preventing action potential
28
infected tissue
lower pH = more drugs in ionized state that can't enter cells and have effect, for infected tissue must increase dose 60x, for inflammed tissue must increase the dose 6x
29
local anesthetic metabolism
ester-type --> hydrolyzed in plasma, amide-type --> hydrolyzed by hepatic enzyme
30
local anesthetic mechanism of action
blocks neuronal sodium channels (on axons) that are open / inactivated from within cells, more frequent nerve stimulation makes anesthetic work faster because more channels are open / inactive, blocks signals before they go to brain
31
never sensitivity for local anesthetics
small fibers (fire more often) and myelinated fibers (smaller areas of impulse propagation) more sensitive, large fibers recover slower, effects pain / cold / warmth more then touch / deep pressure / motor
32
local anesthetics CNS adverse effects
tongue numbness, tinnitus, vertigo, slurred speech, muscle fasciculations, seizures
33
local anesthetics cardiovascular adverse effects
decreased myocardial excitability, conduction rate, and contraction force, arteriolar dilation, only if accidentally injected vascularly
34
local anesthetics hypersensitivity
rash to anaphylacsis, caused by ester-type
35
topical form of local anesthetic
EMLA (lidocaine +prilocane = lower melting point) to cross unbroken skin, eye / ear / nose / mouth, skin grafts, genital warts, venipuncture, lumbar puncture
36
regional anesthesia with local anesthetic
subcutaneous injection
37
intravenous block with local anesthetic
isolate extremity with tourniquet, inject local anesthetic IV, loss of sensory and motor
38
peripheral nerve block with local anesthetic
conduction block, injected into area of peripheral nerve of plexus
39
eipdural block with local anesthetic
injected into eipdural space at L3/4
40
spinal block with local anesthetic
injected into lumbar subarachnoid space
41
procaine (novocaine)
ester, short acting with vasoconstrictor, metabolized quickly in plasma, not good topical
42
lidocaine (xylocaine)
amide, widely used, metabolized in liver, OD can cause ventricular fibrillation / cardiac arrest, used for all types of local anesthesia
43
mepivacaine (carbocaine)
amide, like lidocaine, not good topically, little longer acting than lidocaine
44
bupivacaine (marcaine)
amide, long acting, potent, epidurals, surgery
45
ropivacaine (Naropin)
amide, long acting, less CNS / cardio toxicity than buoivacaine
46
tetracaine (pontocaine)
ester, topical in eye, nose, throat, spinal
47
cocaine
ester, penetrating, vasoconstrictor, used to be used for ENT - mucous membranes
48
proparacaine (alcaine)
for cornea, antibacterial / antifungal properties
49
dibucaine (nupercainal), benzocaine (americaine)
mucous membrane, skin
50
opioids
affect the way pain is perceived, good for sharp pain, adverse effects --> respiratory depression / sedation / euphoria (abuse) / physcial depedence / tolerance, exogenous substance with morphine-like properties
51
NSAIDs
good for inflammation
52
opioid receptors
Mu, Kappa, Delta
53
Mu opioid receptor
analgesia, resp. depression, sedation, decreased GI motility, physical dependence
54
Kappa opioid receptor
analgesia, sedation, decreased GI motility
55
Delta opioid receptor
modulates Mu receptor activity
56
opiate
drug made from opium (poppy) - morphine
57
opioids - morphine, methadone, oxycodone (oxycontin), heroin
Mu, Kappa, Delta receptor agonists
58
Naloxone (narcan)
parenteral only, Mu, Kappa, Delta receptor antagonist
59
Naltrexone (trexan, ReVia)
oral, longer lasting, given once ER patient wakes up, prevents alcoholic relapse, Mu, Kappa, Delta receptor antagonist
60
Nalorphine (mixed agonist-antagonist)
opioid, alone morphine-like (K receptor agonist), with morphine reversed effect (Mu receptor antagonist), in dependent pts precipitates withdrawal (Mu receptor agonist), once pt is on Mu receptor agonist can only tapper that drug - can't switch to weaker K receptor agonist (can only use K receptor agonist to start with)
61
buprenorphine (subutex), naloxone (suboxone) - partial agonists
less efficacy than full agonist, used to prevent relapse in opioid addicts and for mild to moderate pain
62
endogenous opioids
normally binds Mu, Kappa, Delta receptors, endorphins (Mu), enkephalins (pain modulation in brain), dynorphins (Kappa)
63
oral opioids
first pass metabolism high, slower onset / action, delayed peak, longer duration, rapidly metab in liver (must elevate oral dose of morphine 6:1 parenteral), methadone only slowly metab oral
64
IV opioids
precise, accurate dose, rapid onset, risk of adverse effects, bolus vs continuous, patient controlled
65
intermuscular or subcutaneous opioids
relatively rapid onset and action, medium duration, subcutaneous pumps can go home with patients
66
spinal opioids
longer duration with lower dose, acts at spinal site, no adverse reaction in brain
67
rectal opioids
easy administration if vomiting
68
buccal/subligual opioids
faster onset and action, avoids first pass metabolism / injection, ex: buprenorphine (subutex, suboxone) and fentanyl lollipop
69
transdermal opioids
fentanyl (duragesic), buprenorphine (transtec_
70
fentanyl deliveries
IV (sublimaze), transdermal (duragesic), buccal (actiq), nasal (instanyl), is 50x more potent than morphine
71
lipid solubility and opioids
more lipid soluble = cross BBB better, creates sense of euphoria, ex: heroin
72
opioid metabolites
longer action with impaired renal function because morphine 6-glucuronide still active, normeperidine has toxic metabolite meperidine (excitotoxic = tremor, twitch, agitation)
73
ascending pain pathway
spinothalamic tract gray in midbrain and VML in thalamus, C or Asigma primary afferent synapses with 2nd order spinothalamic tract neuron in dorsal horn by releasing glutamate and substance P at, opioids do act directly at this synapse
74
descending pain pathway
pain inhibiting from VML and midbrain to synapse in dorsal horn, releases ext serotonin onto inhibitory interneuron that releases inhibitory enkaphalin at original synapse, also releases inhibitory serotonin and norepinephrine at oringial synapse
75
opioid action in cortex
decreased pain perception, altered reaction, euphoria / dysphoris, sedation
76
opioid action in medulla
respiratory depression, coughing, nausea, vomitting
77
opioid action in spinal cord
stimulates reflexes and spinal function
78
opioid action at oculomotor nuclei
pinpoint pupils (slow tolerance)
79
opioid action at vagus nerve
bradycardia, increased GI tone
80
opioid action at GI tract
constipating, spasmogenic, increased segmental contractions without propulsion, decreases defication reflex (slow tolerance) - need bowel progam
81
opioid uses
pre/post anesthetic med, anesthesia, post traumatic pain, cough, labor, terminal illness, diarrhea
82
Naloxone (narcan)
opioid receptor antagonist, injection, reverses opioid OD, prevents alcohol relapse
83
Naltrexone (ReVia)
opioid receptor antagonist, oral effective, longer acting, prevents opioid and alcohol relapse
84
Alvimopan (entereq) and methylnaltrexone (relistor)
preipheral opioid receptor antagonist, relieves constipation from opioids, does not cause withdrawal
85
opioid withdrawal
not life-threatening, matches degree of dependence, rhinorrhea, lacrimation, yawning, chills, gossbumps, hyperventiliation, hyperthermia, aches, vomiting, diarrhea, anxiety, hostility
86
methadone (dolophine)
opioid receptor agonist, longer acting, may act on other pain related receptors (neuropathic), addict maintenance programs and pain treatment
87
buprenorphine (naloxone = subaxone)
partial opioid agonist, lower abuse, must be off opioids before starting Tx or will cause withdrawal
88
non-steroidal anti-inflammatory drugs
analgesic, antipyretic, anti-inflammatory - not a steroid
89
NSAIDs action
inhibit COX1 (homeostatic) and COX2 (inflammatory), COX -> prostaglandins -> inflammatory prostaglandins + thromboxane (platelet aggregation) + prostacyclin (decreased platelet aggregation), aspirin irreversibly inhibits, other NSAIDs reversibly inhibit
90
peripheral effects of prostaglandins
reduces stimulation threshold of nociceptors (sensitization)
91
central effects of prostaglandins
basal COX-2 in neurons and glia cause early sensitization to peripheral inflammation
92
NSAIDs - antipyretic
cytokines cause fever in hypothalamus, mediated by prostaglandins from elsewhere
93
NSAIDs pharm effects (salicylates)
respiratory stimulation (medulla), uncouple oxidative phosphorylation, increased O2 / CO2 / metab rate (metabolic acidosis / electrolyte imbalance) --> hyperventilation --> respiratory alkalosis
94
NSAIDs GI effects (salicylates)
epigastric distress (CTZ in medulla), bleeding --> iron def anemia, prostacyclin inhibition of gastric acid secretion gone
95
NSAIDs antithrombic effects (salicyclates)
decreased clotting time, aspirin irreversibly inhibits thromboxane in platelets for aggregation, caution with anticoagulants, stop taking 1 week prior to surgery
96
salcylate toxicity
tinnitus, headache, nausea / vomiting (CNS effect), sweating, thirst, hyperventilation, epigastric distress, repsiratory alkalosis followed by metabolic acidosis, fever
97
Tx aspirin OD
reduce absorption (emesis, gastric lavage, charcoal), correct acid / base and electrolytes
98
aspirin hypersensitivity
middle aged, hx urticaria / asthma, rhinitis / secretions / bronchoconstriction / hypotension, not IgE immune response, from accumulation of leukotrienes in lipoxygenase AA pathway, Tx epinephrine
99
Reye's syndrome
aspirin given during varicella infection, often fatal
100
acetaminophen
not NSAID, analgesic and antipyretic, not anti-inflammator, most actinve in hypothalamus with no peroxidases, does not effect bleeding time / respiration / GI, increased hepatoxicity with ethanol or fasting
101
Tx acetaminophen OD
N-acetylcysteine scavenger drug (like glutathione)
102
Ibuprofen
NSAID, less GI prob, reversible blocks COX, increases bleeding time, good for dysmenorrhea, naproxen - long acting, oxaprozin - long half life
103
Indomethacin
NSAID, most potent COX blocker, high toxicity, high GI prob, headache, ulcers - not used during pregnancy or with psychiatric disorders or ulcers, used for fever / OR / RA / gout
104
Ketorolac
NSAID, IM injection or IV, strong as morphine, combined with morphine to reduce amount of morphine needed, use with suspected drug seekers
105
selective COX2 inhibitors (celexicob)
reduces inflammation, celexicob, lumiracoxib
106
meperidine
opioid, has exotoxic metabolite that can cause agitation and tremors, especially in people with poor kidney function
107
Tx for insomnia and migraines
amitriptyline preferable to sumatripan due to its affinity for H1 histamine receptors and muscarinic receptors
108
prophylactic Tx for N. meningitides
ceftriaxone
109
action of acyclovir
turned into monophosphate by thymadine kinase, converts virus into monophosphate, stops DNA replication by replacing sugar normally bound to guanine
110
triptan-mediated agonism for migraines
agonism of 1b serotonin receptors causes vasoconstriction, agonism of 1d serotonin receptors decreases serotonergic tone
111
agonism of 1b serotonin receptors
cerebral vasoconstriction, for migraines
112
agonism of 1d serotonin receptors
decreases serotonergic tone, for migraines

Neuro Drugs (4 decks)

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