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IHO > Week 3 drugs > Flashcards

Week 3 drugs Flashcards

1
Q

Primaquine

A

used in radical cure of plasmodium.
Use only after everything is cleared out
goes after hypnozoite in liver
vivax and ovale

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2
Q

what forms of plasmodium are comon to drug resistance

A

falciparum and vivax

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3
Q

atovaquone / proguinil

When good to use?

A

drug of choice to PREVENT if chloroquine resistant. used alternative to prevent in areas non chloroquine resistant
not good if acute attack. Takes awhile to work

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4
Q

chloroquine

A

drug of choice to PREVENT

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5
Q

doxycyline

A

alternative prophylaxis in chloroquine resistant areas

give AFTER infection if resistant to chloroquine (with quinine in FALCIPARUM and VIVAX resistant)

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6
Q

mefloquine and toxic?

A

alternative prophylaxis in chloroquine resistant areas of FALCIPARUM
NEUROPSYCHIATRIC REACTIONS. hence why chloroquine is preferred

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7
Q

primaquine mech and problems

A

unknown mech. maybe make ROS

HEMOLYTIC ANEMIA IF G6PD defient

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8
Q

quinine

A

give AFTER infection if resistant to chloroquine (falciparum and vivax resistance)
+doxy

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9
Q

quinidine

A

Used with doxy for treating SEVERE DISEASE OF ALL PLASMODIUM

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10
Q

artemisinin based combo therapy (ACT)

A

always used in combo therapy

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11
Q

aretesunate

A

given with mefloquine. ALWAYS GIVE IN COMBO

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12
Q

radical cure

A

use primaquine to take out vivax and ovale in liver. last resort

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13
Q

best treatment for acute attack of plasmodium

A

Chloroquine unless falci and vivax resistant!

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14
Q

prophylatic dosing of anti malria

A

lower doses

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15
Q

mechanism of chloroquine

A

inhibits heme polymerase (normally converts FPIX to hemozoin). Result is high levels of FPIX which are toxic to parasite

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16
Q

toxicity of chloroquine

A

none in low dose

if given for acute attack: can cause blindness if large doses over long period of time

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17
Q

mech and toxic of quinine and quinidine

Unique toxic to quinidine?

A

more toxic than chloroquine
same mech and chloroquine
Adverse if acute attack doses: CINCHONISM which is hearing loss, tinnitus, nausea, etc
Quinidine blocks na and k current - CARDIAC PROBLEMS

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18
Q

atovaquone and proguinil mechanism and problems

A

Ato - depolarized parasite mito
pro - inhibits parasite DHFR
Not good if severe malaria
GI PROLEMS are common

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19
Q

artemisinins mech and toxicity

A

produce free radicals
VERY RAPID activity
DO NO USE ALONE to avoid resistance

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20
Q

CCS examples

A

plant alkaloid

dna synthesis inhibitors

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21
Q

CCNS examples

A 
crosslinking agents
anthracycline antibiotics (rubicin)
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22
Q

leucovorin

A

methylated folate. given with methotrexate.
leucovorin rescue
CAN NOT GIVE INTRATHECAL

23
Q

allopurinol

A

xanthine oxidase inhibitor

prevents uric acid build up when giving 6-mercaptapurine or 6-tu

24
Q

6 mercaptopurine and 6 thioguinine

A

activate by HGPRT and inhibits guanylyl kinase

25
Q

f - fluorouracil

A

inhibits thymidylate synthase

26
Q

pemetrexed

A

folic acid analogue that inhibits thymidylate synthase more than DHFR

27
Q

hydroxyurea

A

inhibits ribonucleotide reductase

prevents making deoxynucleotides

28
Q

cytarabine and gemcitabine

A

pyrimidine analogues

inhibits DNA synthesizing enzymes

29
Q

pyrimidine monophosphate kinase

A

converts ump to udp

important in resistance to 5-FU

30
Q

dihidropyrimidine dehydrogenase

A

degrades thymidine nucleotides

defiency leads to sensitivity to 5-fu

31
Q

cyclophosphamide\

steps of activation / degrade

A

first step activated by cyp450
induction of cyp2b6 increases drug activity
final step makes phosphoramide mustard and acrolein

32
Q

crosslinking agents

pharmacokinetics

A

need to convert to electrophile

33
Q

mechlorethamine

A

instantaneous activation

given IV to avoid GI problems

34
Q

acrolein

A

byproduct of cyclophosphamide
toxic: hemorrhagic cystitis (bladder epithelium)
GIVE MESNA to treat

35
Q

ifosfamide

A

Acts slowly
MOST NEUROTOXIC alkylating agent
-causes mental problems

36
Q

crosslinking toxicities

A
  1. myelosuppression
  2. severe nausease and vomiting
  3. vesicant (blistering), avoid oral
    - bad if escapes IV
37
Q

anthryacycline antibiotic toxicities:

A 
unusual cardiomyopathy
extravasation necrosis
myelosuppression
radiation recall reaction
handfoot syndrome
RED urine
38
Q

bleomycin unique mechanism

A

binds to DNA and generates free radicals that cut DNA

causes pile up of cells in g2 with chromosome problems

39
Q

hydrolase

A

found in lungs and skin
Degrades bleomycin
increased activity increases drug resistance along with increased DNA repair (bleomycin resistance)

40
Q

crosslinking agents examples

A

cyclophosphamide
busulfan
melphalan (activated in diff tissues)
mechlorethamine must be given IV

41
Q

intercalating agent examples

A

doxorubicin

42
Q

drugs that cause strand break

A

etoposide

bleomysin

43
Q

etoposide

A

binds with topo2 and dna that results in strand breaks. stays bound to enzyme to prevent repair
S and G2 phase

44
Q

glutathione peroxidase

A

increases resistance to intercalating agents

so does increased p-glycoprotein and change in target

45
Q

etoposide

A

ccs g2 and 2

binds topo2 and causes double strand break

46
Q

TECANS

A

ironotecan and topotecan

cause single strand dna breaks binding topo1

47
Q

ddrugs that cause strand breaks

A

etoposide and bleomycin

48
Q

bleomycin toxicity

A

lungs and skin dont have hydrolase so causes damage

49
Q

most neurotoxic alkylating agent

A

IFOSFAMIDE. causes mental problems

50
Q

hemorrhagic cystis

A

side affect from cyclophosphamide

51
Q

extravasation necrosis (vesciant)

A

can be from anthracyclines (intercelating agents) or from mechlorethamine

52
Q

MESNA

A

given to treat for hemorrhagic cystis from cyclo and byprodu of acrolein

53
Q

capecitabine

A

3 step activation with first 2 in liver

last step by thmidine phosphorylase which is higher in some tumors making better than 5-fu

IHO (9 decks)

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