FINAL🎃 Flashcards

1
Q

What does each stage of hemostasis target?

Primary
Secondary
Fibrinolysis

A
Primary = platelets
Secondary = clotting factors
Fibrinolysis = plasmin
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2
Q

What drugs are antiplatelets?

..there are 6

A
PAR1 blockers
PDE inhibitors
COX inhibitors
P2Y12 inhibitors
SSRIs
GP2b3a inhibitors
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3
Q

What is the MOA of Vorapaxar?

AEs?

A

PAR-1 blocker: reversible inhibition of platelet thrombin R’s

AEs: rarely used…

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4
Q

What is the MOA, uses, and AEs of dipyridamole and cilostazol?

A

PDE inhibitors: raise cAMP, resulting in vasodilation, inhibition of platelet activation

Uses: tx thrombocytosis (leukemia)

AEs: inhibit megakaryocyte development + dec. platelet #

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5
Q

What is the MOA, AEs, and use of aspirin?

A

Irreversibly inhibits COX 1 + 2

AEs: inc. bleeding risk
Use: anti-thrombotic

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6
Q

What’s the MOA, AEs, use of nonselective NSAIDs?

A

Reversible inhibit COX 1 + 2
BLOCK ASA BINDING SITE

AE: inc bleeding risk; dec. efficacy of ASA
Use: NOT used as anti-thrombotic

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7
Q

What’s the MOA, AEs of selective NSAIDs?

A

Reversible inhibit COX2&raquo_space; 1

AE: inc. clotting risk

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8
Q

What do P2Y12 inhibitors do?

A

Block ADP (for platelet activation)

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9
Q

What is another name for irreversible P2Y12 inhibitors?

A

Irreversible = thienopyridines

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10
Q

What’s the MOA/interactions for Clopidogrel?

A

Irreversible P2Y12 inhibitor
PRODRUG - 2 STEP PROCESS = SLOWEST ONSET

DDI: omeprazole

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11
Q

What’s MOA/interaction of prasugrel?

A

Irreversible P2Y12 inhibitor
PRODRUG - 1 STEP = FASTER ONSET

DDI: fewer

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12
Q

What are the MOA/limitations of Ticagrelor?

A

Reversible P2Y12 inhibitor - active drug/metabolite

Requires BID dosing
MAX 81mg ASA

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13
Q

What are the MOA/limitations of Cangrelor?

A

Reversible P2Y12 inhibitor - drug active
FASTEST on/off

Interferes w/ thienopyridines
IV ONLY
$$$

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14
Q

What’s the MOA/AE/use of SSRIs?

A

Inhibit platelet activation by serotonin

AE: inc. risk of bleeds
NOT used as anti-thrombotic

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15
Q

What does GP2b3a do?

A

Helps platelets bind vWF and fibrinogen to stick to each other or vessel wall

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16
Q

What are MOA/elimination/onset of Abciximab?

A

GP2b3a inhibitor: persistent binding to receptor (host AB’s may dec. efficacy)

Elimination: proteolytic
effect up to 7 DAYs
$$$

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17
Q

What are MOA/elimination/onset of Eptifibatide?

A

GP2b3a reversible inhibitor (not immunogenic)

Elimination: renal
Effect 4-8 hours
$$

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18
Q

What are MOA/elimination/onset of Tirofiban?

A

GP2b3a reversible inhibitor (not immunogenic)

Elimination: renal
Effect 4-8 hours
$

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19
Q

What’s the MOA/admin/elimination/titration of DABIGATRAN?

A
direct thrombin (CF II) inhibitors 
PO - BID
Elimination: renal (t1/2: 12-17 hrs)
NOT titration but may inc. PTT/INR
NO effect on anti-Xa
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20
Q

What is the reversal agent for DABIGATRAN?

A

Idarucizumab

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21
Q

What’s the MOA/admin/elimination/titration of BIVALIRUDIN?

A
Direct thrombin (CF II) inhibitor 
IV - continuous
Elimination: proteolytic (t1/2 = 25 min)
Titration w/ PTT (may inc. INR)
NO effect on anti-Xa
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22
Q

What’s the MOA/admin/elimination/titration of Argatroban?

A
Direct thrombin (CFII) inhibitor
IV - continuous
Elimination: hepatic (t1/2 = 40-50 min)
Titrated w/ PTT (may inc. INR)
NO effect on anti-Xa
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23
Q

What is the reversal agent for factor Xa inhibitors?

A

Andexanet alfa

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24
Q

What’s the MOA/admin/elimination/titration of Rivaroxaban?

A
Factor Xa inhibitor - PO/ qD or BID
Elimination: hepatic (t1/2 = 5-9 hrs)
NOT titrated (but may inc. PTT, INR, anti-Xa)
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25
Q

What’s the MOA/admin/elimination/titration of Apixaban?

A
Factor Xa inhibitor - PO/ BID
Elimination: hepatic (t1/2 = 12 hrs)
NOT titrated (may inc PTT, INR, anti-Xa)
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26
Q

What’s the MOA/admin/elimination/titration of EDOXABAN?

A
Factor Xa inhibitor - PO/ qD
Elimination: renal + hepatic (t1/2 = 10-14 hrs)
NOT titrated (may inc. PTT, INR, anti-Xa)

LESS EFFECTIVE IF CrCL > 95

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27
Q

What does Anti-thrombin (ATIII) do?

A

Made by liver, circulates in blood and inhibits CFs by binding in stable 1:1 complex

Inhibits Xa unbound to platelets and IIa unbound to fibrin

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28
Q

What’s the MOA/AE/elimination/admin of unfractionated heparin (UFH)?

A

Allosteric activation of ATIII - complex formed w/ thrombin + Xa
IV or SQ
Elimination: reticuloendothelial system (macs, ECs) = no renal adjustment
AEs: HIT; osteopenia (prolonged use)

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29
Q

What is the reversal agent for UFH?

A

Protamine

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30
Q

How is UFH monitored?

A

PTT

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31
Q

What’s the MOA/AE/elimination/admin of Enoxaparin, Dalteparin?

A

LMWH: more uniform mixture that binds Xa&raquo_space; IIa
Elimination: renal
QD or BID
AE: lower HIT

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32
Q

What’s the reversal agent for LMWH?

A

Protamine

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33
Q

What’s the MOA/AE/elimination/admin of fondaparinux?

A
Stimulates ATIII to inhibit Xa only
QD dosing (longest t1/2)
SQ
Elimination: renal
AE: does NOT cause HIT
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34
Q

How is fondaparinux monitored?

A

Anti-Xa

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35
Q

What’s the MOA/AE of Warfarin?

A

inhibits VKOR: dec. vitamin K and prevents activation of CFs
AEs: skin necrosis “purple toe syndrome”
Teratogenic, genetic variability

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36
Q

Describe what happens in days 1 and beyond on warfarin

A

Day 1: liver makes fewer CFs, but those already in circulation unaffected
Day 2-4: INR beings inc. - if protein S/C depleted = hyperCOAGUABLE

Days >5: anticoagulation

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37
Q

What are the t1/2s of CF depletion under warfarin?

A

VII = 4-6 hrs greatest effect on INR

C = 8 hrs
S = 30 hrs
X = 48 hrs
II = 72 hrs
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38
Q

What are DDIs associated with warfarin

A

CYP inducers = dec. INR = inc. clotting
(Carbamazepine, phenytoin, rifampin, phenobarbital, CHRONIC EtOH)

CYP inhibitors = inc. INR = inc. bleeding
(Amiodarone, fluconazole, acute EtOH)

Antiplatelets/anticoagulants = no change INR ; inc. bleeding

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39
Q

What are disease interactions with warfarin?

A

Sensitive: hyperthyroidism, decompensated HF, liver disease, malnourishment, low albumin, low body weight

Resistant: hypOthyroidism, high body weight

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40
Q

What’s the MOA and use of citrate?

A

Dec. Ca (required for CFs to localize to membrane)

Use: anticoagulation of stored blood/blood circuits

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41
Q

What is the MOA/use/half-life of alteplase?

A

Fibrinolytic: binds fibrin and converts plasminogen to plasmin in order to break up clot

Use: acute ischemic stroke

SHORT t1/2

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42
Q

What is the MOA/use/half-life of tenecteplase?

A

Fibrinolytic: more specific binding to fibrin and more resistant to plasminogen activator inhibitor (PAI-I)

Use: MI
Longer t1/2 = SINGLE BOLUS

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43
Q

What’s the MOA/use of desmopressin (DDAVP)?

A

Binds V2 R’s to trigger release of stored vWF in order to activate platelets

Use: tx bleeding

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44
Q

Distinguish b/w single vs. multiple vs. blood products for coagulopathy

A

Single factor products = hemophilias

Multiple = bleeding (warfarin)

Blood products = (liver failure) contain factors AND fibrinogen

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45
Q

What is the MOA/use of aminocaproic acid, tranexamic acid?

A

Anti-fibrinolytics: competitively inhibit plasmin/plasminogen

Use: control bleeding (surgical, dental, trauma)

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46
Q

What are the irreversible inhibitors (antiplatelets)?

A

Aspirin
Clopidogrel
Prasugrel
Abciximab

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47
Q

Describe acute management for ischemic stroke

A

THROMBOLYTICS (for re-perfusion)

Other:
+ secondary prophylaxis (anti-platelets, warfarin, direct oral anticoagulants- DOACs)
+ control BP (nicardipine, beta blockers, hydralazine, NTP)
+ avoid hypErglycemia

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48
Q

What’s the thrombolytic/fibrinolytic used for ischemic stroke?

A

Alteplase

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49
Q

For secondary prophylaxis, what can patients take if allergic to aspirin?

A

P2Y12 inhibitors

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50
Q

What’s the MOA/AE for nicardipine?

A

DHP-CCB prevents release of internal Ca stores so heart muscle doesn’t respond to signal = vasodilation
IV 1st line for BP CONTROL IN STROKE

AE: headache, peripheral edema, hypOtension, tachycardia, N/V, flushing

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51
Q

Whats AE/DDI for beta blockers?

A

Angina, bronchospasm, insomnia/depression/fatigue/ dec. HDL and inc. TG

DDI: other AV blocking or anti-HTN agents

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52
Q

Differentiate MOA of Esmolol vs. Labetalol

A

(For stroke)
Esmolol: beta1 selective = dec. BP/HR

Labetalol: beta1/2, alpha1, partial beta2 agonist = dec. BP/HR and arterial vasodilation (alpha, beta2)

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53
Q

What’s the MOA/AEs for hydralazine?

A

Directly relaxes arteriolar smooth muscle; may dec. calcium to dec. contraction; vasodilation

AE: headache, hypotension, fluid retention, palpitations, tachycardia

DRUG-INDUCED LUPUS SYNDROME ..typically resolves w/ DC

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54
Q

What’s the MOA/AE/caution for nitroprusside (NTP)?

A

NO will activate guanylate cycylase to inc. cGMP in vascular smooth muscle = venous/arteriolar dilation = dec. AL/BP

AE: hypotension, CN toxicity, thiocyanite toxicity (tinnitus, tremor)
RISK WITH RENAL DISEASE

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55
Q

What products can be given for life threatening/serious bleeding?

A

Vitamin K
Prothrombin complex concentrates (PCC) = Kcentra
Fresh frozen plasma (FFP) blood group specific
Idarucizumab

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56
Q

What BBW is associated with vitamin K?

A

IV admin = risk of anaphylaxis

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57
Q

What AEs are associated with idarucizumab?

A

Hypokalemia, delirium, constipation, pyrexia hypersensitivity, thrombosis

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58
Q

What can be given for subarachnoid hemorrhage?

A

Aminocaproic acid

Nimodopine

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59
Q

What is the MOA/AE of aminocaproic acid?

A

Blocks plasmin:fibrin interaction to inhibit fibrinolysis

AE: hypOtension, bradycardia, myopathy

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60
Q

What’s the MOA/AE of nimodopine?

A

DHP-CCB = arterial vasodilation

AE: hypotension, headache, flushing, edema, nausea, sinus bradycardia

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61
Q

Which beta lactams are not renally eliminated and therefore do not need dose adjustments?

A

Nafcillin
Oxacillin
Ceftriaxone

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62
Q

What cephalosporins pass BBB and can be used to treat meningitis?

A

Cefuroxime
Ceftriaxone
Cefotaxime
Ceftazidine

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63
Q

What cephalosporins can be used to tx anaerobic (B. Fragilis) infections?

A

Cefoxitin

Cefotetan

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64
Q

What PCN is not impaired by food when administered?

A

Amoxicillin

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65
Q

What AEs associated with PCNs?

A

+Hypersensitivity: skin rash, fever, joint swelling, pruritis, leukopenia, anaphylaxis
+GI: D (killed flora)

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66
Q

What does Ceftaroline treat and not treat?

A

Only beta lactam to tx MRSA

Does NOT treat pseudomonas

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67
Q

What AEs are associated with CSNs?

A

Hypersensitivity, GI distress,
Intolerance to EtOH (Cefotetan inhibits ADH)
Potentially nephrotoxic (mainly 1st gen)

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68
Q

Which CSNs could be used for surgical prophylaxis?

A

1st gen = Cefazolin, cephalexin

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69
Q

How is aztreonam administered?

A

IV

Use if allergic to PCN or CSN

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70
Q

Which carbapenem is coadministered with cilastatin?

A

Imipenem

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71
Q

What AEs are associated with Carbapenems?

A

GI, hypersensitivity, CNS: seizures (imipenem)

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72
Q

What AEs are associated with vancomycin?

A

Hypersensitivity “RED MAN SYNDROME” - cx by histamine

Ototoxicity (mainly when combined w/ aminoglycosides)

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73
Q

What is daptomycin used to treat?

A

VRE, MRSA, VRSA

NOT used in pneumonia - inactivated by surfactant

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74
Q

What AEs/DDI associated with daptomycin?

A

AE: musculoskeletal (pain/weakness)

DDI: HMG-CoA reductase inhibitors - statins - since known to cx myopathy

75
Q

What is telavancin used for?

A

VRE, MRSA, VRSA

76
Q

What AEs are associated with telavancin?

A

GI, CNS: insomnia, headache
◼️Nephrotoxic
◼️Teratogenic

77
Q

What’s AEs/CI/interactions of aminoglycosides?

A

Nephrotoxic, ototoxicity, neuromuscular blockade (could lead to respiratory paralysis @high doses)

CI: renal disease, hearing impairment, pregnancy
DDI: other ototoxic/nephrotoxic drugs

78
Q

What are aminoglycosides used for?

A

Gram negative AEROBES

+ beta lactam = activity vs. gram+

79
Q

What are oxazolidinones used for?

A

Gram+

RESERVED FOR: VRSA, VRE, MRSA

80
Q

What’s AEs/CI/interactions of oxazolidinones?

A

GI distress, Mitochondrial toxicity:

  • hematologic: BM suppression
  • otic/peripheral neuropathy

DDI: Linezolid w/ SSRIs or tyramine-containing foods (since competitive MAO inhibitor)

81
Q

What are tetracyclines used for?

A
Acne (gram+)
Odd:
-brucella
-mycoplasma pneumoniae
-chlamydia ssp (STD, pneumonia)
-rickettsia ssp (Typhus, Rocky)
-borrelia burgdorferi (Lyme)
-Treponema pallidum (syphillis)

Tigecycline can be used vs. VRE/MRSA

82
Q

What’s AEs/CI/interactions of tetracyclines?

A

NO dose adjustments for: doxy and tigecycline

AEs: bone/teeth, GI distress (C. Diff risk), phototoxicity
DDIs: do NOT take with food, dairy, antacids, Ca/Mg/Fe

CI: pregnancy, children

83
Q

What protein synthesis inhibitors can pass BBB?

A

Chloramphenicol

84
Q

What protein synthesis inhibitors can be used vs. anaerobes?

A

Tetracycline
Chloramphenicol
Clindamycin

85
Q

What protein synthesis inhibitors can be used to tx MRSA/VRSA/VRE?

A

Oxazolidinones = available PO!
Tigecycline
Streptogramins

86
Q

What is chloramphenicol active against?

A

Gram +/- aerobes AND anaerobes

87
Q

What does chloramphenicol need to be dose adjusted for?

A

Liver dysfunction

Neonate

88
Q

What’s AEs/CI/interactions of chloramphenicol?

A

Hematologic: aplastic anemia, BM suppression
Gray Baby syndrome
Hypersensitivity

DDIs: potent CYP inhibitor = inc. warfarin, phenytoin, phenobarbital

89
Q

What are macrolides active against?

A

Strep pneumo (1st line)
Legionella penumoniae
Mycobacterium Avium (MAC): infects immunocompromised
Atypical: mycoplasma pneumonia, chlamydia
Campylobacter (diarrhea)

90
Q

What’s AEs/CI/interactions of macrolides?

A

GI (inc. gut motility), hepatotoxicity, cardiac toxicity (QT prolongation)

DDI: CYP/PgP inhibitors except azithromycin

91
Q

What’s clindamycin active against?

A

Gram +
drug of CHOICE for anaerobes “above diaphragm” (aspiration pneumonia, lung abscess)

(Combined with others for anaerobic coverage)

92
Q

What’s AEs/CI/interactions of clindamycin?

A

GI: N/V/D, C-diff’s Pseudomembranous colitis
Hypersensitivity: rash, fever, agranulocytosis

93
Q

What are streptogramins used to tx?

A

Gram+

Reserved for: VRSA, MRSA, VRE (e. Faecium)

94
Q

What’s AEs/CI/interactions of streptogramins?

A

Pain @infusion site; arthalgia/myalgia

DDI: potent CYP inhibitor

95
Q

What subunit does each protein synthesis inhibitor act on?

A

Buy AT 30 = aminoglycosides, tetracyclines

CELL for 50 = chloramphenicol, erythromycin, linezolid, lincosamide (clindamycin)

96
Q

What ABX inhibit DNA replication?

A

Folic acid synthesis inhibitors = TMP/SMX
Quinolone
Metronidazole

97
Q

What is the MOA of TMP/SMX?

A

Sulfonamides inhibit PABA => DHF enzyme (dihydropteroate synthase)

Trimethoprim inhibits DHF => THF enzyme (DHF reductase - also in humans!)

98
Q

What is TMP/SMX active against?

A

Gram+: S. Aureus
H__PEK

NO anaerobic

Fungi: pneumocystis jiroveci

99
Q

What’s AEs/CI/interactions of TMP/SMX?

A

GI, dermatologic (SJS, photodermatitis), hematologic (leukopenia, hemolytic anemia, kernicterus), crystallization of urine, hyperkalemia

DDI: CYP inhibitor (warfarin); drugs that cx hyperkalemia (ACEIs) or spare K+

CI: pregnancy, infants

100
Q

What is the MOA of quinolone?

A

Inhibit topoisomerase II in bacteria

Gram- = "DNA gyrase"
gram+ = Topo IV
101
Q

What quinolone does not need to be dose adjusted for renal failure?

A

Moxifloxacin

102
Q

What is 1st gen quinolone and their activity?

A

Nofloxacin

HNPEK + CApES

103
Q

What is 2nd gen quinolone and activity?

A

Ciprofloxacin, Ofloxacin

Gram+, intestinal (shigella, campylobacter, salmonella)
HNPEK + CAPES

104
Q

What is 3rd gen quinolones and activity?

A

Levofloxacin, Moxifloxacin, Gemifloxacin

Gram+ AEROBES, anaerobes (b. Fragillis), atypical
HNPEK + CApES

105
Q

Which quinolones are best for anaerobic activity?

A

Moxifloxacin

Gemifloxacin

106
Q

What’s CI/interactions of quinolones?

A
CI: pregnancy, children, tendinitis
Myasthenia gravis (since they have neuromuscular blocking activity)

DDIs: other drugs that cause QT prolongation
multivalent cations: take 2 hrs before or 4 AFTER

107
Q

What AEs associated with quinolones?

A

GI, CNS stimulation (dizziness, insomnia, seizures)
Dermatologic: phototoxicity, rash
Musculoskeletal: damage to growing cartilage
Cardiac: QT prolongation (blocks K channels)

108
Q

What’s the MOA of Metronidazole?

A

PRODRUG - requires reduction of nitro group by anaerobic bacteria

Crosses BBB!

109
Q

What does metronidazole have activity against?

A

(Anaerobes)
Gram+ = clostridium
Gram- = bacteroides, fusobacterium, prevotella

(Protozoa)
Giardia, trichomonas, entamoeba

110
Q

What’s AEs/CI/interactions of metronidazole?

A

GI (N/V/D, metallic taste, FURRY TONGUE from yeast overgrowth)

  • disulfiram reaction*
  • peripheral neuropathy*

DDI: EtOH, warfarin
CI: pregnancy, seizures, alcoholism

111
Q

What is a CCR5 inhibitor to tx HIV?

A

Maraviroc

112
Q

What is a fusion inhibitor to treat HIV?

A

Enfuviritide

113
Q

Which NRTI is an exception for renal adjustment?

A

Tenofavir alefenamide (TAF)

114
Q

Which NRTI requires allele screening?

A

Abacavir

For sensitivity reaction risk

115
Q

Which NNRTIs can be given on empty stomach vs. food?

A

Empty: efavirenz

Food required: etravirine, rilpivirine

116
Q

What drugs are boosters for HIV?

A

Ritonavir

Cobicistat

117
Q

What drugs are NRTIs?

A
Didanosine
Zidovudine
Lamivudine
Abacavir
Tenofovir
Emtricitabine
118
Q

Which NRTIs have once daily dosing?

A

Tenofavir

Emtricitabine

119
Q

What’s the MOA of NRTIs?

A

Competitively inhibit nucleotide binding to reverse transcriptase = termination of DNA chain

120
Q

What drugs are NNRTIs?

“-vir”

A

Efavirenz
Nevirapine
Etravirine
Rilpivirine

121
Q

What’s the MOA of NNRTIs?

A

Bind to reverse transcriptase to cause a conformational change and disrupt the catalytic center of the RT

122
Q

What drugs are INSTIs?

“-tegra”

A

Raltegravir
Elvitegravir
Dolutegravir

123
Q

What’s the MOA of INSTIs?

A

Interfere with the integration of viral DNA into host DNA

124
Q

What drugs are protease inhibitors (PI)?

“-navir”

A

Atazanavir
Darunavir
Ritonavir
Lopinavir

125
Q

Which PI is used only as a “booster”?

A

Ritonavir

126
Q

What’s the MOA of PIs?

A

Block proteolytic cleavage of protein precursors that are necessary for the production of infectious particles

127
Q

What are tx regimens for HIV therapy?

A

2 NRTIs + _____ (1 NNRTI/PI/INSTI)

128
Q

Differentiate between NRTIs with significant vs. minimal mitochondrial toxicity

A

Significant: didanosine, zidovudine

Minimal: LATE
Lamivudine, abacavir, tenofavir, emtricitabine

129
Q

What NRTI has renal/bone toxicities

A

Tenofavir

New version has less

130
Q

What are class AEs for NRTIs?

A

Mitochondrial toxicity
PLAN
(Pancreatitis, lactic acidosis, anemia, neuropathy)

131
Q

What are NRTI class interactions?

A

FE were compared to others.. (no CYP)

132
Q

What are class AEs for NNRTIs?

A

Rash, hepatotoxic (inc. LFTs)

133
Q

Which (and what) drug is associated with CNS symptoms of (NNRTIs)

A

Efavirenz = vivid nightmares, stoned feeling, TERATOGENIC

134
Q

What are NNRTI class interactions?

A

CYP3A4 inducers (except rilpivirine)

135
Q

What are the INSTI class AEs?

A

Very well tolerated ✔️

GI

136
Q

Which HIV drugs are generally used with a booster?

A

Protease inhibitors

Atazanavir, darunavir, lopinavir

137
Q

What are PI class AEs?

A

Lipodystrophy (less with atazanavir)
Hyperlipidemia
Hyperglycemia
Fat redistribution = “protease pouch”

Hepatotoxicity (inc. LFTs)

138
Q

Which PI can cause unconjugated hyperbilirubinemia ?

A

Atazanavir

139
Q

What PI class interactions are there?

A

CYP - they are all inhibitors

140
Q

What’s the MOA of polyenes (amphotericin B)?

A

Interact with ergosterol in fungal membrane to form artificial pores

141
Q

What’s the clinical use for amphotericin B?

A

DOC for severe infections by aspergillus, candida, cryptococcus, histoplasma

142
Q

What AEs are associated with amphotericin B?

A

Infusion related
Nephrotoxic (administer with saline)
Hypokalemia, hypomagnesemia

143
Q

What’s the MOA and AEs of 5-FC?

A

Penetrates cell wall; deaminated to 5-FU to inhibit DNA/RNA synthesis

AE: Hematologic toxicity (anemia, leukopenia, thrombocytopenia)

144
Q

What’s the activity for 5-FC?

A

(+ AmpB)

Cryptococus

145
Q

What’s the MOA/AEs of the azoles?

A

Azoles inhibit Lanasterol
Terbinafine inhibits squalen epoxidase

AE: N/V hepatotoxicity

146
Q

What are specific AEs for azoles?

Fluconazole, Itraconazole, Voriconazole, Posaconazole, Isavuconazole

A
Fluconazole = GI
Itraconazole = rarely used due to cardiac AEs
Voriconazole = visual disturbances
Posaconazole = well tolerated/ GI
Isavuconazole = GI
147
Q

What are the MOA/AEs of echinocandins?

“-fungins”

A

Inhibit beta-glucan synthase enzyme (* not in humans)

AE: minor, some histamine release (=> flushing, headache, urticaria, pruritis)

148
Q

What’s the spectrum of activity of micafungin?

A

Candida (yeast)

Aspergillus (mold)

149
Q

Compare activities of fluconazole vs. Voriconazole vs. Posaconazole

A
Flu = candida, cryptococcus
Voriconazole = candida, cryptococcus, aspergillus
Posa = candida, cryptococcus, aspergillus, mucormycosis
150
Q

What species are the flat worms?

A

Trematodes (flukes)

Cestodes

151
Q

What species are the roundworms (nematodes)?

A

Ascariasis
Hookworm
Pinworm

152
Q

ANTIMALARIALS

What’s the MOA of quinine and quinidine?

A

Quinine = PO; quinidine = IV
Block heme to hemoglobin = buildup of heme
Blocks trophozoite stage to schizone/gametocytes

153
Q

What’s AEs/CI/interactions of quinine, quinidine?

A

GI, cardiac (QT prolong), CINCHONISM (tinnitus, disturbed vision, dizziness), HEMATOLOGIC (quinine: acute hemolytic anemia if G6PD def.)

DDI: CYP/PgP inhibitor
CI: G6PD deficiency (quinine only)

154
Q

Which drug classes can be used for malaria?

A

Quinolone derivatives
Artemisinin + derivatives
Antifolates
ABX

155
Q

What’s the MOA of chloroquine and hydroxychloroquine?

A

Inhibit heme polymerase activity - toxic buildup

156
Q

What’s AEs/CI/interactions of chloroquine, hydroxychloroquine?

A

GI (n/v/d), cardiac (QT prolong), PRURITIS, VISUAL DISTURBANCES
SAFE in PREGNANCY

CI: psoriasis, ocular disease

157
Q

What are the MOA/AEs/CI for mefloquine?

A

Similar to quinine

GI (n/v/d), cardiac (QT prolong), CNS: vivid dreams, anxiety, HA, psychosis, seizures

CI:
◼️epilepsy, psychosis, schizophrenia, depression, anxiety

158
Q

What’s the MOA/AE/CI/DDI of primaquine?

A

Generates reactive oxygen species? (Active vs. hepatic stage)

GI, cardiac, hematologic: hemolysis/hemolytic anemia (counsel patients to look for dark/blood-colored urine!!!)

CI: G6PD def, pregnancy
DDIs: CYP inducer = caution with warfarin

159
Q

What’s the MOA/AEs/CI of artesunate, artemether, dihydroartemisinin?

A

Bind iron, breakdown peroxide to make free radicals that damage parasite

GI (n/v/d), CNS = dizziness
CI: 1st tri pregnancy, kids <5kg

160
Q

What’s the MOA/AE/CI of atovaquone-proguanil?

A

(Antifolate)
Atovaquone: disrupts NT synthesis; proguanil = DHFR inhibitor

GI (n/v/d, abdominal pain), mild/reversible inc. of liver enzymes
CI: pregnancy

161
Q

What ABX can be used to tx malaria?

A

Tetracycline, doxycycline, clindamycin

162
Q

How is complicated malaria tx?

A

1st: quinidine + ABX

Artesunate if quinidine unavailable, then switch to PO regimen

163
Q

How is uncomplicated/non-falciparum malaria tx?

A

P. Malariae: chloroquine/hydroxychloroquine

P.ovale/P.vivix: cholorquine/hydroxychloroquine + Primaquine (if not G6PD def.)

164
Q

How is uncomplicated/falciparum malaria tx?

A

Chloro ✅: chloroquine/hydroxychloroquine
Chloro ❌: Atovaquone-Proguanil OR ARtemether OR quinine +ABX OR mefloquine

Mefloquine❌: atovaquone-proguanil OR arthemether OR quinine+ABX

165
Q

Describe antimalaria prophylaxis tx

A

Chloro✅: chloroquine/hydroxychloroquine
chloro❌: atovaquone-proguanil OR doxy OR mefloquine

areas w/ P.vivax: primaquine

anti-relapse Tx: primaquine

166
Q

What drugs are used to tx entamoeba hystolytica/amebiasis?

A

Metronidazole or Tinidazole (systemic)

Paromycin or Iodoquinol (luminal)

167
Q

What’s the tinidazole?

A

Similar to metronidazole (prodrug that will eventually generate free radicals and disrupt DNA to cause cell death)

168
Q

What’s the MOA/AE of paromycin?

A

Aminoglycosides - binds 30S to interfere with initiation complex and inhibit protein synthesis

AE: GI (n/v/d), rash (rare)

SAFER in PREGNANCY

169
Q

What’s the MOA/AE of iodoquinol?

Hint: 🎀

A

..?.. effective vs. organisms in bowel lumen

AE: GI (mild diarrhea - take with meal), ENLARGEMENT OF THYROID

170
Q

What drugs are used to tx giardia lamblia/giardiasis?

A

Metronidazole
Tinidazole
Niazoxanide
Paromycin

171
Q

What’s the MOA/AE of nitazoxamide?

A

??? (May interfere with e- transfer rxn)

AE: GI (diarrhea, abdominal pain)

172
Q

What are tx for nematodes/roundworms?

Ascaris lumbricoides, Necator americans/hookworm, enterobius vermicularis/pinworm

A

Albendazole

Pyrantel pamoate

173
Q

Which nematode can cause anemia?

A

Hookworm

174
Q

Which nematode can cause pruritis in perianal region?

A

Pinworm

175
Q

What’s the MOA/AE/CI of albendazole?

A

Starves the worm - interferes with MT synthesis and glucose uptake

AE: GI (long term use can inc. liver enzymes)
CI: pregnancy, liver disease

176
Q

What’s MOA/AE of pyrantel pamoate?

A

Neuromusuclar blocking agent causes inc. in ACh and inhibition of AChE = paralysis

AE: GI, dizziness, inc. liver enzymes

177
Q

What’s the MOA/AE/CI for ivermectin?

A

Paralyzes worm: binds with gated chloride channels

GI (diarrhea), pruritis
CI: pregnancy

178
Q

What can ivermectin only be used to tx?

A

Ascariasis and hookworm

179
Q

What can be used to treat flatworms (trematodes, cestodes)

A

Praziquantel

180
Q

What is used to treat cysticercosis (invasive cestodes from taenia solium which infects pigs)?

A

Praziquantel + surgery
Anticonvulsant + corticosteroid
Albendazole

181
Q

What’s the MOA/AE of praziquantel?

A

Inc. permeability to Ca (variant channel in parasites) = contraction/paralysis

GI (n/v/d), CNS (headache, dizziness), pruritis

182
Q

What do cephalosporins NOT work on?

A

LAME

Listeria
Atypicals
MRSA (except for Ceftaroline)
Enterococci

183
Q

What tx can be given for community-acquired pneumonia (CAP)?

A

Macrolide
Tetracycline
Fluoroquinolone (LEVOFLOXACIN) discouraged b/c of resistance

184
Q

What should be administered for children with CAP?

A

(S. Pneumo common cx)
Preferred: Amox

Rash from PCN: cephalosporin