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Pharmacology drew > test 5 > Flashcards

test 5 Flashcards

1
Q

morphine pharmikokinetics

A

t1/2=2/3 hours, metabolized in the liver(glucuronide formation), readily cross placenta-> respiratory depress the fetus
-standard dose is 10mg SC or IM

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2
Q

morphine drug interactions

A

addative defect with ethos, barbituates, bento, anti psychotics and into depress and anti Histamine
-MAOI- can cause severe hyperpyrexia(esp meperidine)
some anti histamines can increase the analgesic effects of morphine
-same as^ with tricyclic anti depress

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3
Q

opioid drug poisioning

A

triad-
cns depression(stupor or coma)
depressed depth and rate of breathing
pin point pupils (if pt severely hypoxic and near death pupils may dilate)
Treat- respiratory support and ventilation and naloxone (narcotic antagonist)

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4
Q

codiene

on list

A

oral admin
1/12 of morphine- dose 30-60 mg
analgesic for mild to moderate pain, antitusive
only a weak opioid agonist, but in most pts it is demethylated and converted to morphine to give its effect (genetic polymorphism)

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5
Q

Hydromorphone on list

A

similar to morphine but more potent

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6
Q

oxycodone

on list

A

oral admin, (alone or in combination with acetaminophen)

OXYcontin is a sustained release oral prep for chronic pain

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7
Q

hydrocodone

on list

A

orally in combination with acetaminophen for mild-mod pained anti tussive
very highly prescribed
Zohydro is an oral sustained release w/o acetamenophen

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8
Q

meperidine

on list

A

synthetic drug, oral and parenteral admin
1/10 morphine
-though to have less SM effect and less constapation and urine retention( weak support)
-short acting and not used for chronic pain
-used in OB b/c less rest depression of the fetus

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9
Q

Heroine

on list

A

more potent and euphoric than morphine, lasts 4-6 hours
not available for med use in US
injected or snorted

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10
Q

Methadone

on list

A

less euphoric and long-lasting(12-24 hours) than morphine(4-6) or heroine(4-6)
used an analgesic and treat opioid addiction
carefull dosing with monitoring

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11
Q

fentenyl

on list

A

very potent mu agonist(100x morphine)
used in surgery
neuroleptic anesthesia when used with NO gas and dropiridol(inovor)

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12
Q

pentazocine

on list

A

mixed opioid agonist and antagonist
agonist effects dominate- acts at K receptor but only partially at the mu receptor
mu antagonist at high doses
less effective for pain than morphine, less sedation and rest depression
more comon cns stim and hallucination
can ppct withdrawal in opioid addicts
given parenteral

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13
Q

Butorphanol

A 
similar to pentazocine
mixed opioid agonist and antagonist
agonist effects dominate- acts at K receptor but only partially at the mu receptor
mu antagonist at high doses
less effective for pain than morphine, less sedation and rest depression
more comon cns stim and hallucination
can ppct withdrawal in opioid addicts
can be given intranasally
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14
Q

buprenorphine

on list

A

partial agonist at mu R, antagonist at high dose
only slightly less analgesic effect than morphine but MUCH lower abuse potential
reduce craving of heroine addicts ( suboxone- combination this and naloxone to prevent abuse)
injected, sublingual, or intranasal
“Office based treatment of opioid addiction”

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15
Q

Tramadol

on list

A

partial mu agonist
mild to moderate pain used
inhibits synaptic repute of NE and serotonin like tricyclic anti depress
SE resemble other opioids( dizzy,sedate,nausea,constipation)

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16
Q

tapentadol

A

newer drug, like tramadol but higher activity at the Mu R
inhibits NE and 5-HT reuptake
used for moderate to severe pain, schedule 2
high abuse potential

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17
Q

Naloxone

on list

A

pure opioid antagonist- block most mu R, can pact withdrawal
drug for opioid poisioning, can reverse the rest depression
must be parenteral b/c of first pass metabolism
short acting 1-2 hrs

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18
Q

naltrexone

on list

A 
Pure opioid antagonist
long acting (24 hours) and orally given
risk of hepatotox
compliance is problem
must be brought the withdrawal fist before treatment 
used for alcoholics to block cravings
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19
Q

clonidine

A

centrally acting adrenergic neuronal inhibitor
not a prodrug
similar action to methyl dopa as a a2 agonist to dampen simp outflow
lower doses than methyldopa, in patch form
no autoimmune SE, rebound HTN
treatment of: adhd, meno hot flash, stress disorder, nicotine and ethos withdrawal, ALSO TREAT OPIOID WITHDRAWL

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20
Q

methylnaltrexone

A

quaternary salt of naltrexone used specifically for opioid induce constipation
only given parenteral
post operative paralytic ileus
alvimopan and NAloxegol are similar

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21
Q

Acetyl Salicylic Acid

on list

A

Salicyclic Acid Derivatives

irreversible COX-1 and COX 2 inhibitors pKa=3.5

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22
Q

Mesalamine

A

Salicyclic Acid Derivatives

5-amino salicylic acid

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23
Q

Diflunisal

on list

A

Salicyclic Acid Derivatives-REVERSIBLE INHIBITS tisue COX
similar analgesic and anti inflame to aspirin
NO ANTI PYRETIC EFFECTS
t1/2=8-12(3-4x asprin)
acute to long term pain mild to moderate pain management

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24
Q

Indomethacin [IndocinR]

on list

A

Acetic Acid Derivatives
reversible COX1 and COX 2 inhibitors
not recommended in children under 14 b/c hepatotoxicity
aggrevate depressin
SE: headache, CNS disturbances
FDA approved for closing patent ductus arteriosus

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25
Etodolac
Acetic Acid Derivatives | reversible COX1 and COX 2 inhibitors
26
Diclofenac | on list
Acetic Acid Derivatives | reversible COX1 and COX 2 inhibitors
27
Tolmetin | on list
Acetic Acid Derivatives reversible COX1 and COX 2 inhibitors indicated for JRA SE:autoimmune hemolytic anemia
28
Ketorolac | on list
Acetic Acid Derivatives reversible COX1 and COX 2 inhibitors SE: strong headache NO USE in RA or OA
29
Ibuprofen | on list
Propionic Acid Derivatives reversible COX1 and COX 2 inhibitors SE: high hypersensitivity triad of risk-fever rash, internal organ involvement others: ab pain, headache, nausea, vomit, liver damage, meningitis in SLE pts FDA aproved for closing patent ductus arteriosus
30
Naproxen | on list
Propionic Acid Derivatives reversible COX1 and COX 2 inhibitors indicated for JRA
31
Ketoprofen | on list
Propionic Acid Derivatives | reversible COX1 and COX 2 inhibitors
32
Oxaprozin | on list
Propionic Acid Derivatives | reversible COX1 and COX 2 inhibitors
33
Piroxicam (oxicams) | on list
enolic acid derivatives | reversible COX1 and COX 2 inhibitors
34
Meloxicam (oxicams) | on list
enolic acid derivative | reversible COX1 and COX 2 inhibitors
35
Nabumetone | on list
Non acidic compound (Alkanones)
36
Acetaminophen | on list
Para aminophenol derivative
37
Celebrex | on list
COX-2 inhibitor don't give to pts with sulfonamides allergies b/c of similar structure, or have run to other NSAID drugs USE: OA,RA, acute pain, , Dysmenorrhea, familial adenomatous polyposis
38
Misoprostol | on list
Prostaglandin E1 analogue used for anti ulcer effects in pts on long term NSAID therapy PG - protect gastric mucosa by decreasing acid production
39
Hydroxychloroquine Sulfate | on list
Nonbiologic Disease Modifying Antirheumatic Drugs (DMARDs) SE: ocular toxicity ( Bullseye maculopathy) irreversable, dose related damage second line treatment of RA in combo with methotrexate 3rd treatment for JRA in sulfasalazine ineffective
40
Methotrexate | on list
Nonbiologic Disease Modifying Antirheumatic Drugs (DMARDs) USE:1st DMARD of choice in JRA, Adult RA, antineoplastic inhibts dihydrofolate reductase-> interfere w/ DNA synthesis and repair, and replication, signal 3 mech 50 % bound, metabolized to active form, renal excretion tox reduced by leucovorin calcium
41
Sulfasalazine | on list
Nonbiologic Disease Modifying Antirheumatic Drugs (DMARDs)- immunosupressive SE: most serious is neutropenia, moderate serious, anorexia, nausea ,Gastric distress minor skin rash and uticaria, hemolytic anemia don't use in PREG USE: SERVER RA combined with methotrexate and Hydroxychloroquine sulfate #2 DMARD in JRA if Methotrex not tolerated
42
Leflunomide | on list
Nonbiologic Disease Modifying Antirheumatic Drugs (DMARDs) isoxazole immunomodulatory agent MOA: inhibits dihydroorotate dehydroxygenase(pyrimidine synthesis) and is anti proliferative, and is anti inflammatory T1/2 is 2 weeks and highly albumin bound SE: diarrhea, ELEVATED Liver enzyme ALT/AST, immunosupression USE: active RA to reduce S/S NO PREG USE
43
Etanercept | on list
biologic DMARDs- TNFa inhibitor binds TNFa and TNFB, elevated levels of these found in RA pts synovial fluid SE: affect pts ability to fight infection and malignancy serious sepsis can occur USE: moderate to severe active RA combo with methotrexate, moderate to severe JRA(the only FDA aproved), 2x wkly SC inject
44
Infliximab | on list
biologic DMARDs- TNFa inhibitor chimeric IgG1 monoclonal Ab, human constant and murine variable region bionds to TNFa to neutralize and inhibits TNFa binding to its receptor, no affect to TNFB USE: reduce inflammation in chrons pts, active RA in combo with Methyltrexate(in pts not responding to methtrex) T1/2= 9.5 days, SE in notes( infection, hyprsensetvy, HACA)
45
Anakinra | on list
biologic DMARD- NON TNF a inhibitor | IL1R antagonist
46
CYCLOPHOSPHAMIDE | on list
cytotoxic and anti proliferative agent requires metabolic activation via P450 oxidation to alkylating metabolites, CCNS(inhibits nucleotide synthesis) and signal three mechanism -MOA- direct cytotoxicity to T and B cells USE: 7-14 days b4 effects, severe Rheumatologic conditions(RA), Malignant disease-lymphoma, must myloma, retinoblastoma etc 60 %bound to serum protein
47
Azathioprine | on list
MOA: derivative of 6-mercaptopurine, cleaved to 6MP cell cycle specific antimetabolite,inhibit nucleotide synthesis suppress T more than B cells 30% bound to serum protein inhibits adenosine deaminase and IMP-dehydrogenase SE: N/V/D, leukopenia thrombocytopenia, anemia
48
Cyclosporine | on list
t cell suppressant, inhibits SIGNAL 1 inhibiting calcineurin Phosphatases, inhibits release of IL-2 CMI inhibition, REVERSIBLE inhibit T lymphocyte in G0/ G1 90% bound, metabolized by P450 3A(interact w/ azole AF) SE: renal dysfunction, tremor, hirsutism, hypertension, gum hyperplasia, Embryotoxic and fetotoxic USE: prophylaxis of organ rejection kidney/liver/heart, RA and psoriasis (Brand Neoral)
49
MYCOPHENOLATE MOFETIL | on list
Reversible inhibitor of Inosine monophosphate dehydrogenase--> preventing guanosin neucleotide syn inhibits proliferation of t and b cell, suppress Ab production inhibits intercellular adhesion to endothelium, prolongs survival of transplants, 97% bound to plasma albumin (T1/2=17hr) SE: dirrhea, leukpoenia,sepsis, vomiting, infections USE:prophylaxis for rejection of renal,liver,heart transplants used with cyclosporin and corticosteroids
50
MUROMONAB-CD3 | on list
murine monoclonal Ab(IgG2a) blocks TCR(CD3), signal 1 SE: hypersensativity to murine protein USE: renal, liver,pancreas, heart allograft rejection
51
Lymphocyte immune globulin | on list
Serum IgG of horse immunized to human lymphocytes reduces number of T cells in the blood, spleen, and LN SE: sensativity to hosre protein, chills fever vertigo, systemic infections, adverse effects on a fetus USE: minimizes alograft rejection in renal transplant used with antimetabolites and corticosteroids
52
Daclizumab
HUmanized IgG1 monoclonal Ab that binds IL2 R on surface of lymphocytes, 90% HUMAN inhibits signal 3(IL2 binding and IL2 activation of lymphocyte SE: constipation, N/V, ab pain, minor CV(tachy, dyspnea, angina USE: minimizes allograft rejection of renal and cardiac
53
RHo Immune Globulin | on list
concentrated solution of immune globulin from human plasma donors imunized to produce high anti RHo ABs contra indicated in RH+ pts and RH- pts already sensatized USE: prevent erythroblastosis fetalis, prevent immune response of RH- pts to RH+ cells, admin w/in 72hr or birth
54
Immune Gobulin | on list
Used to treat congenital hypogammaglobulinemia, prevent infection in ped HIV pt, treatment of ITP , systemic and local infections and Guillian Barre syndrome
55
Interferon Beta-1b | on list
166 amino acid protein antiproliferative and immunoregulatory activities Used to treat RR MS
56
INF gamma | on list
pruified 140 amino acid protein potent phagocyte activating effects, generation of toxic oxygen metabolites within the phagocytes SE: flu like constitutional symptoms USE: treatment of Chronic granulomatous disease, enhancing phagocyte production of superoxide to kill bacteria
57
drugs that can contribute to gout development
``` aspirin diuretics( thiazides) sulfonamide antimicrobials antineoplastics L-DOPA ```
58
NSAIDs in gout
indomethacin, Ibuprofen, Ketoralac stop the acute gouty attack, inhibiting PG avoid the use of aspirin ketoralac injectable, indomethacin- CNS effects
59
Colchicine | on list
traditionally treat acute gout attack, low dose sometimes used to treat reoccurrence inhibits polymerization of tubular into microtubules , reducing leukocyte migration, phagocytosis, and mitosis - inhibits production and release of pro inflammatory mediators SE-BAD dirrhea,N/V,
60
allopurinol | on list
inhibits xanthine oxidase to reduce uric acid formation no effect on acute attacks, but can reduce potential future attacks SE: gouty attack early in therapy, elevated liver enzyme, allergic run DI:^t1/2 theophyilline, inhibts hepatic drug met
61
Febuxostat | on list
newer xantine oxidase inhibitor fewer skin run than allopurinol probably no effect on acute attacks, but can reduce potential future attacks(not in notes) SE: elevated liver enzymes, high cost
62
Probenecid | on list
Uricosuric agent, inhibits anion exchage in proximal tubule, inhibiting Uric acid absorption and secretion, net effect is excretion T1/2=5-8 hr SE:increased risk of stone formation in kidney, contraindicated in kidney stone pts pts must consume adequate amount of water
63
Rasburicase
recombinate urate oxidase/uricase enzyme uric acid--->allantoin approved for management of uric acid levels in pts with leukemia,lymphoma, or solid cancer/c of the high uric acid blood level from cell lysis SE: fever, headache, skin rash,N/V, GI pain, allergy slow IV over several hours
64
pegloticase
``` recombinate urate oxidase/uricase enzyme uric acid--->allantoin used in adults w/ severe refractory gout SE: fever, headache, skin rash,N/V, GI pain, allergy slow IV over several hours ```
65
alprazolam
Benzodiazepine
66
chlordiazepoxide
Benzodiazepine
67
diazepam
Benzodiazepine centrally acting muscle relaxant -facilitates GABA in the SC
68
lorazepam
Benzodiazepine
69
midazolam
Benzodiazepine
70
temazepam
Benzodiazepine
71
triazolam
Benzodiazepine
72
Flumazenil
Benzodiazepine antoagonist
73
butalbitol
barbiturate
74
pentobarbitol
barbiturate
75
phenobarbitol
barbiturate
76
thiopental
barbiturate
77
balcofen
centrally acting muscle relaxant work in BS and SC to modify reflex arc that modulates muscle contraction -agonist at GABAb R in the SC to decrease excitatory NT release abuse potential b/c CNS depress
78
cyclobenzaprine
centrally acting muscle relaxant work in BS and SC to modify reflex arc that modulates muscle contraction very sedating inhibits both GABA and alpha motor system
79
metaxalone
centrally acting muscle relaxant | work in BS and SC to modify reflex arc that modulates muscle contraction
80
tizanidine
centrally acting muscle relaxant work in BS and SC to modify reflex arc that modulates muscle contraction alpha 2 agonist very sedating, SE hypotension
81
alvimopan and naloxegol
similar anti constpation effects as methylnaltrexone but better oral efficacy preferred drug for post operative paralytic ileus
82
anti seisure drugs
valproic acid, toiramate, gabapentin
83
amitryptline
anti depressant | prevention of migraine
84
buspirone
treat mild to mod anxiety, but no resp depress sed-hyp, or muscle relax no GABA, works at 5ht R low abuse potential, used in pts with abuse past high first pass met
85
zolpidem
work at benzo R to promote GABA action(Omega 1) | long acting 6-8
86
zaleplon
work at benzo R to promote GABA action(Omega 1) | short acting 2-4 hr
87
eszopiclone
work at benzo R to promote GABA action(Omega 1) | long acting 6-8

Pharmacology drew (9 decks)

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