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Pharmacology > Anti Infectives > Flashcards

Anti Infectives Flashcards

1
Q

What are the anaerobic protozoa?

A
  1. Entamoeba histolytica (amebiasis)
    • invasive colitis/ dysentery
    • liver abcess
  2. Giardia lamblia (giardiasis)
    • diarrhea
  3. Trichomonas vaginalis (STD)
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2
Q

Which drugs are used to treat Entamoeba, Giardia, and Trichomonas infection?

A
  • Metronidazole
  • Tinidazole
  • Nitazoxanide
    • Giardia only? (see p4 of notes)
    • Cryptosporiodosis helminths
    • Anaerobic bacteria
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3
Q

Metronidazole

  • MOA
  • IND
  • SE
A
  • MOA
    • generates ROS using paracytic enzymes
  • IND
    • Anaerobic protozoa (Entamoeba, Giardia, Trichomonas)
  • SE
    • Disulfiram effects with alcohol
      • blocks acetaldehyde dehydrogenase
    • CNS effects (rare)
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4
Q

Tinidazole

  • MOA
  • IND
A
  • MOA
    • generates ROS using parasitic enzymes
  • IND
    • metronidazole-resistant anaerobic protozoa
      • Entamoeba
      • Giardia
      • Trichomonas
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5
Q

Nitazoxanide

  • MOA
  • IND
  • SE
A
  • MOA
    • inhibits enzyme that converts pyruvate to acetyl CoA (starves it?)
  • IND
    • Broad spectrum:
      • Giardiasis
      • Cryptosporiodosis
      • Helminths
      • Anaerobic bacteria
  • SE
    • GI upset
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6
Q

What are the therapeutic uses of Chloroquine?

A
  • Erythrocytic forms of Plasmodium (covers all those listed in notes)
  • Prophylaxis and Treatment
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7
Q

What is the MOA of Chloroquine?

A
  • Inhibits heme polymerization
    • cannot remove parasitic waste from compartment
    • parasite dies
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8
Q

What are the contraindications of Chloroquine?

A
  • Epilepsy
  • Myesthenia Gravis
  • Psoriasis
  • G6PD deficiency
    • causes hemolysis
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9
Q

Chloroquine

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Inhibits heme polymerization
      • cannot remove parasitic waste from compartment
      • parasite dies
  • IND
    • Erythrocytic forms of Plasmodium (covers all those listed in notes)
    • Prophylaxis and Treatment
  • SE
    • Hemolysis in G6PD deficiency
  • CON
    • Epilepsy
    • Myesthenia gravis
    • Psoriasis
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10
Q

What is the MOA of Quinine/ Quinidine?

A
  • Inhibits heme polymerization
    • cannot remove parasitic waste from compartment
    • parasite dies
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11
Q

What are the indications of Quinine/ Quinidine?

A
  • **Active **disease only!
  • Erythrocytic forms of Plasmodium
  • Chloroquine- resistant strains
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12
Q

What are the side effects of Quinine/ Quinidine use?

A

prolonged Q-T

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13
Q

What are the contraindications of Quinine/ Quinidine use?

A
  • Epilepsy
  • Myasthenia gravis
  • Tinnitis
  • Optic neuritis
  • G6PD deficiency
    • causes hemolysis
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14
Q

Quinine/Quinidine

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Inhibits heme polymerization
      • cannot remove parasitic waste from compartment
      • parasite dies
  • IND
    • Active disease only!
    • Erythrocytic forms of Plasmodium
    • Chloroquine- resistant strains
  • SE
    • Long QT interval
  • CON
    • Epilepsy
    • Myasthenia gravis
    • Tinnitis
    • Optic neuritis
    • G6PD deficiency
      • causes hemolysis
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15
Q

What is the MOA of Primaquine?

A
  • Inhibits mitochondrial electron transport chain
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16
Q

What are the indications for Primaquine?

A
  • Prophylaxis
  • Hepatic forms of malaria (hypnozoites)
    • P. vivax
    • P. ovale
  • Prevents relapse
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17
Q

What are the side effects of Primaquine?

A

methemoglobinemia

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18
Q

What are the contraindications of Primaquine?

A
  • Pregnancy
  • G6PD deficiency
    • causes hemolysis
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19
Q

Primaquine

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Mitochondrial electron transport inhibitor
  • IND
    • Prophylaxis
    • Eradicates hepatic forms of malaria
      • hypnozoites of P. vivax and P. ovale
    • Used to prevent relapse
  • SE
    • Methemoglobinemia
  • CON
    • Pregnancy
    • G6PD deficiency
      • causes hemolysis
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20
Q

Sulfadiazine + Pyrimethamine

  • MOA
  • IND
A
  • MOA
    • inhibits folate metabolism (THFR)
  • IND
    • Toxoplasma
      • does not eliminate encysted form
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21
Q

What are nematodes?

A

Round worms

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22
Q

What are Cestodes?

A

Flat worms

(ex: tapeworm)

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23
Q

What are Trematodes?

A

Flukes

(Ex: schistosomiasis)

Wood flute = made from Tree = Treematodes are Flukes

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24
Q

What is the MOA of Ivermectin?

A
  • Kills larvae only!
    • does not cure
  • Induces paralysis via glutamate-gated Cl- channels that release GABA in the neuromuscular junction
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25
Q

What are the indications of Ivermectin?

A
  • Nemotodes only!
  • DOC: Onchoceriasis (river blindness)
  • Strongyloidiasis
  • Cutaneous larvae migrans
  • Scabies
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26
Q

What are the side effects of Ivermectin use?

A
  • Mazzotti-type rxn
    • urticaria
    • tachycardia
    • hypoTN
  • Can affect mammalian GABA receptors in BBB is impaired
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27
Q

Ivermectin

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Kills larvae stage only!
    • Induces paralysis via Cl- channels found only in invertabrates
      • increases GABA
  • IND
    • Nematodes only!
      • DOC: onchocerciasis (river blindness)
      • Strongyloidiasis
      • Cutaneous larvae migrans
      • Scabies
  • SE
    • Mazzotti type rxn
      • urticardia, tachycardia, hypoTN
  • CON
    • affects mammalian GABA receptors in BBB is impaired

Ivan takes Ivermectin

  • Ivan from Sn Lorenzo gets river blindness and is cured by Italian Dr. Mazzotti
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28
Q

What are the mechanisms of resistance to Ivermectin?

A
  • increased expression of P-glycoprotein (P-gp)
  • Change in the glutamate-gated Cl- channels
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29
Q

Pyrantel Pamoate

  • MOA
  • IND
A
  • MOA
    • Depolarizing neuromuscular blocker
      • results in paralysis
      • parasite release
      • passes out of host
  • IND
    • Nematodes
      • hookworm
      • pinworm

P’s: Pyrantel Pamoate causes Paralysis in Pinworms

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30
Q

What drug is good for fighting GI worms?

A

Mebendazole

(low absorption)

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31
Q

What is the MOA of Mebendazole?

A
  • Binds nemotodal ß tubulin
  • Inhibits microtubule polymerization
  • Poorly absorbed in GI: good for battling GI worms
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32
Q

What are the indications of Mebendazole?

A
  • Nemotodes
  • Cestode larva
  • DOC: Cysticercosis
  • DOC: Echinococcosis
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33
Q

Mebendazole

  • MOA
  • IND
  • SE
A
  • MOA
    • binds nematodal ß tubulin
    • inhibits microtubule polmerization
    • Poorly absorbed in GI: good for battling GI worms
  • IND
    • Nematodes
    • Cestodal larva
    • DOC: Cysticercosis
    • DOC: Echinococcosis
  • SE
    • vomiting
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34
Q

Praziquantel

  • MOA
  • IND
  • CON
A
  • MOA
    • paralysis of worms
  • IND
    • DOC: flatworms
    • DOC: schistosomiasis
    • DOC: liver flukes
  • CON
    • Ocular cysticercosis (tapeworm larvae in eye)
      • host response damages eye
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35
Q

What is the DOC to treat flatworms?

A

Prazequantel

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36
Q

What is the DOC to treat schistosomiasis?

A

Prazequantel

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37
Q

What is the DOC to treat liver flukes?

A

Prazequantel

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38
Q

What is the DOC to treat Cysticercosis?

A

Mebendazole

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39
Q

What is the DOC to treat Echinococcosis?

A

Mebendazole

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40
Q

Which drug is used to treat hookworms and pinworms?

A

Pyrantel

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41
Q

What is the DOC to treat onchocerciasis (river blindness)?

A

Ivermectin

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42
Q

What drug combination is used to treat toxoplasma?

A

Sulfadiazine + Pyrimethamine

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43
Q

Which drug is used to eradicate the hypnozoites of P. vivax and P. ovale?

A

Primaquine

(these are the hepatic forms of malaria)

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44
Q

Which drugs are used to treat Chloroquine- resistant strains of Erythrocytic forms of Plasmodium?

A

Quinine / Quinidine

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45
Q

What is the DOC to treat Erythrocytic forms of Plasmodium?

A

Chloroquine

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46
Q

What is the MOA of Flucytosine?

A
  • Fungistatic
  • Inhibits DNA synthesis
    • cytosine analogue
    • inhibits thymidylate synthase
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47
Q

What are the indications for Flucytosine?

A
  • DOC: chromomycosis (combo w/ itraconazole)
  • DOC: aspergillosis (combo w/ amphotericin B)
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48
Q

What are the side effects of Flucytosine use?

A
  • Bone marrow suppression
  • Cardiotoxic
  • Teratogen
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49
Q

What are the contraindications of Flucytosine?

A
  • Pregnancy
    • teratogen
  • Brivudine
    • anti-viral
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50
Q

Flucytosine (5-FC)

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Fungistatic
    • interferes with DNA synthesis
      • ​cytosine analog
      • inhibits thymidylate synthetase
  • IND
    • DOC: chromomycosis (combo w/ itraconazole)
    • DOC: aspergillosis (combo w/ amphotericin B)
  • SE
    • BM suppression
    • cardiotoxicity
  • CON
    • pregnancy (teratogen)
    • Use with brivudine (anti-viral)
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51
Q

What is the MOA of Griseofulvin?

A
  • Binds tubulin
  • Destabilizes microtubules
    • no mitosis
  • Fungistatic
52
Q

What are the indications for Griseofulvin use?

A
  • Tinea infections
    • Trychophyton
      • tinea cruris
    • Microsporum
      • tinea corpus
    • Epidermophyton
      • tinea pedis
  • (not effective against yeast or dimorphic fungi)
53
Q

What are the side effects of Griseofulvin use?

A
  • Porphyria
  • Hepatic failure
  • SLE
  • Toxic epidermal necrolysis
  • Teratogen
54
Q

Griseofulvin

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Fungistatic
    • Binds tubulin
    • Destabilizes microtubules (no mitotic spindle)
  • IND
    • Tinea infections
      • Trychophyton
        • tinea cruris
      • Microsporum
        • tinea corpus
      • Epidermophyton
        • tinea pedis
    • (not effective against yeast and dimorphic fungi)
  • SE
    • Porphyria
    • Hepatic failure
    • SLE
    • Toxic epidermal necrolysis
  • CON
    • Pregnancy (Teratogen)

Griseofulvin = Grizzly bear in woods

  • Strong = breaks down trees (MTs)
  • Woods = Ringworm (tinea infxn)
  • Poison ivy = skin rxn = SLE, toxic epidermal necrolysis
55
Q

Terbenafine/Butenafine

  • MOA
  • IND
  • SE
  • CON
A
  • Group: Allylamine (Terbenafine), Benzylamine (Butenafine)
  • MOA
    • Fungicidal
    • Inhibit squalene epoxidase (ergosterol cell membrane synthesis)
      • conversion of squalene to lanosterol
  • IND
    • Onchomycosis (terbinafine)
    • Tinea infection
  • SE
    • Stevens-Johnson syndrome
    • Lupus
    • Liver failure
    • Renal failure
  • Steven in a turbin with his squawking, ringworm infested parrot on his shoulder
    • Terbinafine = Turbin
    • Steven = S-J syndrome
    • Squawking = (-) squalene epoxidase
    • Ringworm = treats Tinea
56
Q

Imidazoles

  • MOA
  • IND
  • SE
A
  • Drugs:
    • Ketoconazole
    • Clotrimazole
    • Miconazole
  • MOA
    • Fungicidal** and Fungi_static_**
    • Inhibits ergosterol formation (membrane synthesis)
      • inhibits lanosterol 14-alpha-sterol demethylase
  • IND
    • Ketoconazole
      • coccidioides immitis, Cryptococcus neoformans, Candida, …
    • Others:
      • Infections of stratum corneum, squamous mucosa and cornea
  • SE
    • Ketoconazole
      • liver dysfunction
      • Inhibits P450 3A4 (drug interactions)
    • Decreased steroid hormone synthesis
57
Q

What are the drugs in the Triazole class? What is the MOA?

A
  • Drugs:
    • Fluconazole
    • Itraconazole
    • Posaconazole
    • Terconazole
    • Voriconazole
  • MOA:​
    • Fungistatic and fungicidal
    • Inhibit 14-alpha-sterol demethylase
      • inhibits ergosterol synthesis
      • disrupts plasma membrane formation
58
Q

Fluconazole

  • MOA
  • IND
  • SE
A
  • MOA
    • Fungistatic and fungicidal
    • Triazole
    • Inhibits ergosterol synthesis
      • disrupts plasma membrane formation
  • IND
    • DOC: systemic candidiasis
    • DOC: cryptococcal meningitis
    • DOC: coccidioidal meningitis
    • NOT effective against aspergillosis
  • SE
    • Hepatotoxicity
    • Inhibits P450 3A4

Candida resistance develops quickly

59
Q

To which triazole does Candida quickly develop resistance?

A

Fluconazole

60
Q

Voriconazole

  • MOA
  • IND
  • SE
A
  • MOA
    • Fungistatic and fungicidal
    • Triazole
    • Inhibits ergosterol synthesis
      • disrupts plasma membrane formation
  • IND
    • DOC: Invasive aspergillosis of the lung
    • DOC: Fusarium (eye)
    • DOC: Scedosporium apiospermum (brain)
  • SE
    • Visual disturbance (only one of group)
    • Hepatotox
    • Inhibits P450 3A4
61
Q

Posaconazole

  • MOA
  • IND
  • SE
A
  • MOA
    • Fungistatic and fungicidal
    • Triazole
    • Inhibits ergosterol synthesis
      • disrupts plasma membrane formation
  • IND
    • Prophylaxis:
      • Aspergillosis
      • Candida
      • (take with meal)
  • SE
    • Hepatotox
    • Inhibits P405 3A4

Posaconazole is Prophylactic

62
Q

Terconazole

  • MOA
  • IND
  • SE
A
  • MOA
    • Fungistatic and fungicidal
    • Triazole
    • Inhibits ergosterol synthesis
      • disrupts plasma membrane formation
  • IND
    • Vulvovaginal candidiasis
  • SE
    • Hepatotox
    • Inhibits P450 3A4
63
Q

Itraconazole

  • MOA
  • IND
  • SE
A
  • MOA
    • Fungistatic and fungicidal
    • Triazole
    • Inhibits ergosterol synthesis
      • disrupts plasma membrane formation
  • IND
    • Long list (see notes)
  • SE
    • Steven’s Johnson rash (only one of group)
    • Hepatotox
    • Inhibits P450 3A4
64
Q

Amphoteracin B

  • MOA
  • IND
  • SE
A
  • (Polyene)
  • MOA
    • Binds to ergosterol
    • alters fungal membrane permeability
  • IND
    • Life threatening infections
      • aspergillosis
      • Cryptococcosis
      • Blastomycosis
  • SE
    • Renal tox
      • limited if given in lipid formulation
    • Hepatotox
    • Cytokine storm
      • high fever, swelling and redness, extreme fatigue and nausea
    • Arrhythmia

**ABC: Amphoteracin B causes Cytokine storm

65
Q

Nystatin

  • MOA
  • IND
  • SE
A
  • (Polyene)
  • MOA
    • bind to ergosterol
    • alter fungal membrane permeability
  • IND
    • mucocutaneous candidiasis
    • thrush
    • candidal vaginitis
  • SE
    • Not listed in notes
66
Q

What drugs are in the echinocandin class? What is the MOA?

A
  • Drugs
    • ANIDULAFUNGIN
    • CAPSOFUNGIN
    • MICAFUNGIN
  • MOA:
    • Fungicidal
    • Inhibits cell wall formation
      • glucan synthase inhibitor
        • inhibits synthesis of β-(1,3)-D-glucans
        • unique target towards filamentous fungi
67
Q

Caspofungin

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Fungicidal
    • Inhibits cell wall formation
      • glucan synthase inhibitor
      • inhibits synthesis of β-(1,3)-D-glucans
        • unique target towards filamentous fungi
  • IND
    • DOC: esophagial candidiasis
    • Aspergillus
  • SE
    • Hepatotox
    • Pruritis
    • Phlebitis
  • CON
    • Use with cyclosporin
68
Q

Micafungin

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Fungicidal
    • Inhibits cell wall formation
    • glucan synthase inhibitor
      • inhibits synthesis of β-(1,3)-D-glucans
        • unique target towards filamentous fungi
  • IND
    • ​prophylaxis in hematopoietic stem cell transplants
    • Aspergillus
  • SE
    • Hepatic effects
      • increased with sirolimus use
    • Pruritis
    • Phlebitis
  • CON
    • Use of sirolimus
69
Q

Anidulafungin

  • MOA
  • IND
  • SE
A
  • MOA
    • Fungicidal
    • Inhibits cell wall formation
    • glucan synthase inhibitor
      • inhibits synthesis of β-(1,3)-D-glucans
        • unique target towards filamentous fungi
  • IND
    • Not specialized
    • candidemia, systemic fungal infections in immunocompromised (like others in class)
  • SE
    • Pruritis
    • Phlebitis
70
Q

Pentamidine

  • MOA
  • IND
  • SE
A
  • MOA
    • inhibit tRNA and protein sythesis
  • IND
    • Pneumocystis pneumonia (P. jiroveci)
  • SE (red in ppt)
    • EXTREMELY TOXIC
      • Pancreas
      • Kidney
    • fatal arrhythmias: hypo-kalemia & -calcemia
    • inhalation may promote bronchoconstriction
    • dysglycemias
71
Q

TMP-SMX (Trimethoprim / Sumlfamethoxalone)

  • MOA
  • IND
A
  • MOA
    • Inhibits nucleotide synthesis
  • IND
    • Pneumocystis jiroveci pneumonia [PCP]
72
Q

What anti-fungal treatment is preferred for chromomycosis?

A

Flucytosine + Itraconazole

73
Q

What anti-fungal treatment is preferred for aspergillosis?

A

Flucytosine + Amphoteracin B

74
Q

Which anti-fungal drug is the DOC for systemic candidiasis?

A

Fluconazole

75
Q

Which anti-fungal drug is the DOC for cryptococcal meningitis?

A

Fluconazole

76
Q

Which anti-fungal drug is the DOC for coccidioidal meningitis?

A

Fluconazole

77
Q

Which anti-fungal drug is the DOC for invasive aspergillosis of the lung?

A

Voriconazole

78
Q

Which anti-fungal drug is the DOC for fusarium (eye)?

A

Voriconazole

79
Q

Which anti-fungal drug is the DOC for Scedosporium apiospermum (brain)?

A

Voriconazole

80
Q

Which anti-fungal drug is preferred for prophylaxis of aspergillosis and candidiasis?

A

Posaconazole

81
Q

Which anti-fungal drug is the DOC for vulvovaginal candidiasis?

A

Terconazole

82
Q

Which anti-fungal drug is the DOC for esophageal candidiasis?

A

Caspofungin

83
Q

Which anti-fungal drug is preferred for prophylaxis in hematopoeitic stem cell transplants?

A

Micafungin

84
Q

Which anti-fungal drug is preferred for Pneumocystis pneumonia (P. jiroveci)?

A

Pentamidine

TMP-SMX

85
Q

Which anti-fungal drug causes visual disturbances?

A

Voriconazole

86
Q

Which anti-fungal drug causes cytokine storm?

A

Amphoteracin B

87
Q

Which anti-fungal drug is toxic to the pancreas?

A

Pentamidine

88
Q

Doconasol

  • MOA
  • IND
A
  • MOA
    • Inhibits fusion of viral envelope to host cell
  • IND
    • Herpes labialis (Herpes virus)
89
Q

What is the MOA of Foscarnet?

A
  • Inhibits genome replication
    • Phosphate derivative
    • Binds phosphate site on DNA polymerase (inhibits binding)
    • Inhibits nucleotide binding to DNA
90
Q

What are the therapeutic uses of Foscarnet?

A
  • HSV retinitis in AIDS patients
  • Acyclovir-resistant HSV mucocutaneous infection in immunocompromised patients
91
Q

What are the side effects of Foscarnet?

A
  • Nephrotoxicity
  • Seizure
  • Anemia
92
Q

Foscarnet

  • MOA
  • IND
  • SE
A
  • MOA
    • Inhibits genome replication
      • phosphate derivative
      • inhibits viral DNA polymerase (blocks P binding sites)
      • Inhibits attachment of nucleotides to DNA
  • IND:
    • CMV retinitis in AIDS patients
    • Acyclovir-resistant CMV mucocutaneous infections in immunocompromised
  • SE
    • Nephrotox
    • Seizure
    • Anemia
  • Note:
    • Used with ganciclovir to treat infections resistant to either drug alone

**Foscarnet = Seizure, Anemia, Nephrotoxicity

93
Q

What is the MOA of Acyclovir?

A

Genome replication inhibitor

  • Nucleoside triphosphate analog
    • only converted in infected cells
    • Inhibits viral DNA polymerase
    • DNA chain termination
94
Q

What are the therapeutic uses of parenteral acyclovir treatment?

A
  • HSV encephalitis
  • initial mucocutaneous HSV &VZV in immunocompromised
  • initial severe Herpes Genitalis
  • Neonatal herpes
95
Q

What are the therapeutic uses of oral acyclovir treatment?

A
  • Herpes genitalis
    • treats symptoms only
  • VZV:
    • Chickenpox
    • Shingles
96
Q

What are the therapeutic uses of topical acyclovir treatment?

A
  • Herpes genitalis
  • Recurrent Herpes labialis
  • Mucocutaneous HSV in immunocompromised
97
Q

What are the side effects of Acyclovir treatment?

A
  • Acute interstitial nephritis
  • Hemolytic anemia
  • Phlebitis
98
Q

Acyclovir

  • MOA
  • IND
  • SE
A
  • MOA
    • Inhibits DNA replication
    • Nucleotide triphosphate analog
  • IND: HSV and VZV
    • Parenteral
      • HSV encephalitis
      • Herpes genitalis
      • Neonatal herpes
    • Oral
      • Herpes genitalis (symptoms)
      • VZV: chickenpox, shingles
    • Topical
      • Herpes genitalis
      • Herpes labialis
      • HSV infection in immunocompromised
  • SE
    • Acute interstitial nephritis
    • Hemolytic anemia
    • Phlebitis
99
Q

What are the indications of Valaciclovir?

A
  • Herpes labialis
  • Herpes Genitalis
  • VZV
    • Chickenpox
    • Shingles (Better than acyclovir)
100
Q

What are the side effects of Valaciclovir?

A
  • Acute renal failure
  • Altered/Lost consciousness
  • Blood problems
    • Hemolytic anemia
    • Hemolytic uremic disorder
    • Thrombocytopenia (with bruising)
101
Q

Valaciclovir

  • MOA
  • IND
  • SE
A
  • MOA
    • Prodrug of Acyclovir
  • IND
    • Herpes labialis
    • Herpes genitalis (doesn’t cure)
    • Shingles (more effective than acyclovir)
    • Chickenpox (children)
  • SE
    • Acute renal failure
    • Altered/lost consciousness
    • Blood problems
      • Hemolytic anemia
      • Hemolytic uremic syndrome
      • Thrombocytopenia
102
Q

Ganciclovir

  • MOA
  • IND
  • SE
A
  • MOA
    • nucleotide triphosphate analog
    • inhibits viral DNA polymerase (no chain termination like acyclovir)
  • IND: CMV
    • Oral:
      • CMV retinitis
    • IV:
      • CMV retinitis
      • CMV infection in transplant pts
    • Intravitreal
      • CMV retinitis in AIDS pts
    • Ophthalmic
      • acute hyperkeratosis
  • SE
    • Leukopenia
    • Sepsis
    • Retinal detachment
    • Blurred vision
    • Teratogen, carcinogen, mutagen
103
Q

Valganciclovir

  • MOA
  • IND
  • SE
A
  • MOA
    • Prodrug of Gancyclovir
  • IND
    • CMV retinitis
      • AIDS or transplant pts
  • SE
    • Renal impairment
    • Pancytopenia
    • Retinal detatchment
    • Tremor
    • Teratogen
104
Q

What are the parameters used to determine whether HIV needs to be treated in a patient?

A
  • CD4 count
    • if less than 200 T cells/uL
    • consider treatment if 200-350 cells/uL
  • Viral load
    • if over 100,000 RNA copies/uL
  • Symptomatic
105
Q

Enfuvirtide

  • MOA
  • IND
  • SE
A
  • MOA
    • blocks HIV fusion with host membrane by binding gp41
  • IND
    • HIV-1 resistant to other antiretroviral treatments
  • SE
    • Guillen-barre
    • Renal insufficiency
    • Thrombocytopenia

***Enfuvirtide = Enhibits Fusion of Virus HIV

F => G; EnFuvirtide => Guillen barre

106
Q

Maraviroc

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • Chemokine receptor antagonist
    • Binds CCR-5 to prevent binding to HIV gp120
    • inhibits entry
  • IND
    • CCR-5 tropic HIV-1
  • SE
    • Hepatotoxicity (Black box)
    • URI
  • CON
    • Pts with renal impairment

***Maraviroc = Mara gang CCR5

107
Q

What is the MOA of NRTIs?

A
  • Nucleoside Reverse Transcriptase Inhibitors
  • NRTIs are nucleoside analogs
  • Incorporated into DNA by reverse transcriptase
    • chain termination
  • Inhibits host cell DNA polymerase
    • side effects
108
Q

Emtricitabine

  • MOA
  • IND
  • SE
A
  • MOA
    • NRTI
    • Pyrimide congener
  • IND
    • HIV-1
  • SE
    • Lactic acidosis
    • Hepatic steatosis
    • Lipodystrophy
    • Immune reconstitution syndrome (all NRTIs)
      • unmasking of previously acquired opportunistic infection

Note: reduce dose in pt w/ renal impairment

109
Q

Lamivudine

  • MOA
  • IND
  • SE
A
  • MOA
    • NRTI
    • Pyrimidine congener
  • IND
    • HIV
    • Active Chronic HBV
  • SE
    • mildest of the NRTIs
      • “Mild as a Lam”
    • General symptoms
    • Teratogen

Note: reduce dose in pt w/ renal impairment

110
Q

Tenofovir

  • MOA
  • IND
  • SE
A
  • MOA
    • NRTI
    • Adenosine congener
    • competes with dATP at reverse transcriptase
  • IND
    • HIV
    • Chronic HBV
  • SE
    • Renal impairment
    • Lactic acidosis
    • Liver steatosis
    • Lipodystrophy
    • Immune reconstitution syndrome

Note: reduce dose in pt w/ renal impairment

111
Q

Zidovudine

  • MOA
  • IND
  • SE
A
  • MOA
    • NRTI
    • pyrimidine base congener
  • IND
    • HIV
    • Significantly reduces in utero transmission of HIV
  • SE
    • Bone marrow suppression
    • Anemia
    • Hepatotox
    • Steatosis
    • Lipodystrophy
    • Immune reconstitution syndrome

Note: reduce dose in pt w/ renal impairment

112
Q

Efavirenz

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • non-nucleoside reverse transcriptase inhibitor (NNRTI)
    • Binds directly to reverse transcriptase
      • inhibits catalytic site
  • IND
    • HIV
  • SE
    • Hepatotox
    • Immune reconstitution syndrome
    • Psych symptoms (suicide)
    • Stevens Johnson rash
  • CON
    • Pt w/ psych disorder
    • Pregnancy (teratogen)
113
Q

Dolutegravir

  • MOA
  • IND
  • SE
  • CON
A
  • MOA
    • inhibits HIV-1 integrase
      • (-) incorporation of viral DNA into CD4 DNA
  • IND
    • resistant HIV
  • SE
    • Stevens Johnson syndrome
    • Toxic epidermal necrolysis
  • CON
    • Liver disease

**Dolutegravir = (-) HIV Integrase

114
Q

Elvitegravir

  • MOA
  • IND
  • SE
A
  • MOA
    • inhibits HIV integrase
      • (-) insertion of HIV DNA into CD4 DNA
  • IND
    • resitant HIV
  • SE
    • None listed

****Elvitegravir = (-) HIV Integra​se

115
Q

Raltegravir

  • MOA
  • IND
  • SE
A
  • MOA
    • Inhibits HIV integrase
      • (-) insertion of HIV DNA into CD4 DNA
  • IND
    • Resistant HIV
  • SE
    • Immune reconstitution syndrome
    • Stevens Johnson syndrome
    • Teratogen

**Raltegravir = (-) HIV Integra​se

116
Q

Atazanavir

  • MOA
  • IND
  • SE
A
  • MOA
    • Binds to active site of HIV protease
      • Inhibits production of functional viral proteins
  • IND
    • HIV-1
  • SE
    • Best tolerated
    • **Long P-R interval **
    • Elevated bilirubin (most common)
    • Hepatitis*
    • Immune reconstitution syndrome
117
Q

Darunavir

  • MOA
  • IND
  • SE
A
  • MOA
    • Binds to active site of HIV protease
      • Inhibits production of functional viral proteins
  • IND
    • HIV-1
  • SE
    • Hyperlipidemia*
    • Diabetes*
    • Hepatitis*
    • Immune reconstitution syndrome*
118
Q

Lopinavir

  • MOA
  • IND
  • SE
A
  • MOA
    • Binds to active site of HIV protease
      • Inhibits production of functional viral proteins
  • IND
    • HIV-1
  • SE
    • GI intolerance
    • Hyperlipidemia*
    • Diabetes*
    • Hepatitis
    • Immune reconstitution syndrome*
119
Q

Tipranavir

  • MOA
  • IND
  • SE
A
  • MOA
    • Binds to active site of HIV protease
      • Inhibits production of functional viral proteins
  • IND
    • HIV-1
  • SE
    • Hyperlipidemia*
    • Diabetes*
    • Hepatitis*
    • Immune reconstitution syndrome*
120
Q

Ritonavir

  • MOA
  • IND
  • SE
A
  • MOA
    • Binds to active site of HIV protease
      • Inhibits production of functional viral proteins
    • Increases concentration of other Protease inhibitors
      • inhibits metabolizing enzymes
  • IND
    • HIV-1
  • SE: Highest incidence
    • Diabetes*
      • (-) GLUT 4
      • No glucose to fat/muscle cells
    • Pancreatitis
    • Hepatitis*
    • Arrhythmia (long P-R)
    • Immune reconstitution syndrome*
    • Hyperlipidemia*
121
Q

Rimantadine

  • MOA
  • IND
  • SE
A
  • MOA
    • Inhibits uncoating
    • Blocks M2 proton channel
      • (-) acidification of viral interior
      • (-) viral matrix protein release
      • (-) transfer of viral nucleic acid to host
  • IND
    • Influenza type A
  • SE
    • None listed

Note: high degree of resistance

***Rimantadine = Romantic = Don’t kiss your date if you have the flu

122
Q

Oseltamivir

  • MOA
  • IND
  • SE
A
  • MOA
    • Binds active site of host neuraminidase
    • (-) release of virus from host cells
  • IND
    • Influenze A or B
      • Prophylaxis*
      • Acute illness if used w/i 48 hrs of symptoms
  • SE
    • Neuropsychiatric effects
    • Vomiting
    • Teratogen
123
Q

Entecavir

  • MOA
  • IND
  • SE
A
  • MOA
    • Reverse transcriptase inhibitor
      • purine analog
  • IND
    • Chronic HBV
  • SE
    • Lactic acidosis
    • Hepatomegaly from steatosis
    • Exacerbation of Hepatitis
    • Elevated AST
    • Teratogen
  • CON:
    • Pts w/ AIDS
      • cause resistance to NRTI therapy

Note: adjust dose in renal impairment

**Entcavir = Ent holding an anti-hep C sign

124
Q

Ribavirin

  • MOA
  • IND
  • SE
  • CON
A
  • (Use with IFN 2b to prevent resistance)
  • MOA
    • Purine analog
    • (-) RNA polymerase
    • (-) viral genome replication
  • IND
    • Chronic Hep C
  • SE
    • Hemolytic anemia
    • BM suppression
    • Pancreatitis
    • Arrythmia
  • CON:
    • pregnancy
    • Decompensated liver disease

**Ribavirin = Ribs are in the shape of a C; virin = virus

125
Q

Peginterferon Alpha

  • MOA
  • IND
  • SE
  • CON
A
  • Always use with Ribavirin
  • MOA
    • Induces immune response
  • IND
    • Chronic Hep C
  • SE
    • Exacerbate the following conditions
      • Neuropsych
      • Ischemic
      • Autoimmune
      • Infectious
  • CON
    • Cirrosis
    • HIV pts
126
Q

Telaprivir

  • MOA
  • IND
  • SE
A
  • Must use with Ribavirin and Peginterferon Alpha
  • MOA
    • Protease inhibitor
  • IND
    • Chronic Hep C
  • SE
    • Severe skin rxn
    • Anemia
    • Teratogen

Pharmacology (12 decks)

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