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PPP II > Anti-Malaria Meds > Flashcards

Anti-Malaria Meds Flashcards

1
Q

Name the 2 subcategories of Protozoa

A

-Extraintestinal protozoal infections (plasmodium species)

-intestinal protozoal infections
(entamoeba histolytic giardia lamblia)

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2
Q

Name the 2 subcategories of metazoa

A

-Flatworm (trematodes and cestodes)

-Roundworm(nematodes)-Ascariasis

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3
Q

Describe the Malaria life cycle

A

1) Mosquito takes a bite injecting sporozoite to liver to blood

2) Target of sporozoite is hepatocyte (liver)

3) Replicate in hepatocyte –> schizont stage

4) Ruptures and releases merozoite, which infects the red blood cell. (Final target bc malaria needs hemoglobin)

5) Trophozoite feeds and forms a schizont and gametocytes (replicates)

6) Gametocytes get into the mosquito when the mosquito bites and forms a sporozoite to be able to inject into the next person (cycle)

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4
Q

Quinine and Quinidine MOA

A

Prevent stacking up of heme which will produce radicals and kill the malaria bug (Stacking up makes it less toxic)

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5
Q

PK of Quinine

A

Short 1/2 life, TIT TID PO

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6
Q

Clinical use of Quinine PO

A

Treatment of drug resistant P. Falciparum infection (Because of toxicity and short 1/2 life not used for chemoprophylaxis)

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7
Q

Quinine AE

A

-GI
-Cardiac (QT & Blockade of K Channels)
-Cinchonism (Ears: Tinnitu; eyes: Disturbed vision; CNS: Headaches, dizziness)
-Hematologic (acute hemolytic anemia (in pt with G6PD Def)

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8
Q

CI Quinine

A

-G6PD Deficiency
-CYP2D6
-Pgp

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9
Q

Chloroquine and Hydroxychloroquine MOA

A

Inhibit hem-polymerase activity leading to toxic build up of heme

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10
Q

Chloroquine and Hydroxychloroquine Clinical Uses

A

-Treatment and prophylaxis of non-resistant P.Falciparum and P.Malariae

-Used in combo with primaquine for the eradication of hepatic stages of P. Vivax and P. Ovale

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11
Q

AE of Chloroquine and Hydroxychloroquine

A

-GI
-Cardiac (QT)
-Pruitis (itching)
-Visual disturbances

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12
Q

Is Chloroquine and Hydroxychloroquine safe in pregnancy?

A

Yes

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13
Q

Chloroquine and Hydroxychloroquine CI

A

-Psoriasis
-Ocular Disease

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14
Q

Mefloquine (Lariam) MOA

A

Inhibit hem-polymerase activity leading to toxic build up of heme

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15
Q

Mefloquine (Lariam) Clinical use

A

Prophylaxis (once weekly dosing)
-Treatment of Drug-resistant P.Falciparum

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16
Q

Mefloquine (Lariam) AE

A

-GI
-Cardiac (QT)
-CNS (vivid dreams, headache, anxiety, psychosis, seizures)

CROSSES BBB

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17
Q

Mefloquine (Lariam) CI

A

-Epilepsy, psychosis, schizophrenia, depression, anxiety

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18
Q

Primaquine MOA

A

Unknown, prob generating reactive oxygen species

-Active against hepatic stages P.vivax and P. Ovale
-Highly gametocidal against all four malaria species

CAN KILL HYPNOZOITE STAGE

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19
Q

Primaquine AE

A

-GI
-Cardiac (QT)
-Hematologic Effects (Must test for G6PD deficiency)
-Counsel patients to look for dark or blood colored urine (indicating hemolysis)

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20
Q

Primaquine CI

A

-Patients with G6PD Deficiency
-Pregnancy
CYP1A2 (Warfarin)

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21
Q

Artesunate, Artemether, Dihydroartermisinin MOA

A

Binds to iron, breaks down peroxide bridges –> production of free radicals –> damage parasite

Affects RBC

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22
Q

Artesunate, Artemether, Dihydroartermisinin PK

A

-Rapidly absorbed
-Peak plasma 1-2 hours
-Short 1/2: 1-3 hours

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23
Q

Artesunate, Artemether, Dihydroartermisinin Clinical use

A

-Treatment of uncomplicated falciparum malaria (As artemisinin based combo therapy: Artemether-Lumefantrine (FDA Approved)

-Treatment of complicated falciparum malaria (Artesunate (iv, ir), artemether (ir) can be obtained via CDC

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24
Q

Artesunate, Artemether, Dihydroartermisinin AE

A

-GI
-CNS (Dizziness)

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25
Q

Artesunate, Artemether, Dihydroartermisinin CI

A

-First trimester of Pregnancy
-Children <5 kg

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26
Q

Atovaquone and Proguanil (Malarone) Characteristics

A

Chemoprophylaxis with single folate antagonist no longer recommended –> combo regimens

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27
Q

Atovaquone and Proguanil (Malarone) MOA

A

-Proguanil inhibits DHFR

-Atovaquone: Disrupts mitochondrial electron transport in parasite –> disrupt nucleotide synthesis

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28
Q

Atovaquone and Proguanil (Malarone) Clinical Uses

A

Treatment and prophylaxis os chloroquine-resistant P. falciparum

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29
Q

Atovaquone and Proguanil (Malarone) AE

A

-GI
-Mild and reversible elevation of liver enzymes

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30
Q

Atovaquone and Proguanil (Malarone) CI

A

Pregnancy

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31
Q

Tetracycline, Doxy and Clindamycin MOA

A

Inhibition of protein synthesis in parasite apicoplast
-Slow acting blood schizonticides

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32
Q

Tetracycline, Doxy and Clindamycin Clinical use

A

-Alone for chemoprophylaxis
-Ineffective as single agents for malaria treatment –> use in conjunction with quinine

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32
Q

Tetracycline, Doxy and Clindamycin AE

A

-GI
-Bone structures
-Photoxicity

DDI: Interactions to Antacids

CI: Preg and children

33
Q

What categories do you think of for uncomplicated malaria?

A

-Non-Falciparum
-Falciparum

34
Q

What categories do you think of for P.Malariae?

A

-Non-Falciparum

Chloroquine or hydroxy.

35
Q

What categories do you think of for P.Ovale and P.vivax?

A

-Non-Falciparum

Chloroquine or hydroxy.
PLUS
Primaquine (If not G6PD Def)

36
Q

What categories do you think of for Falciparum Malaria?

A

-Acquired in chloroquine sensitive area
-Acquired in chloroquine resistant area
-Acquired in mefloquine resistant area

37
Q

What do you treat for Acquired in chloroquine sensitive area

A

Chloroquine or hydroxy.

38
Q

What do you treat for Acquired in chloroquine resistant area?

A

-Atov-Pro
OR
-Artemtether-Lum,
OR
-Quinine plus Tetra or doxy or clinda

OR Mefloquine

39
Q

What do you treat for Acquired in mefloquine resistant area?

A

-Atov-Pro
OR
-Artemtether-Lum,
OR
-Quinine plus Tetra or doxy or clinda

40
Q

What do you treat for complicated malaria

A

Artesunate (Iv)

Switch to oral med to complete regimen

41
Q

Amebiasis Species

A

Entamoeba Histolytica

42
Q

Two forms of Entamoeba Histolytica

A

-Cyst
-Trophozoite (motile feeding form, causes pathology, invasive disease)

43
Q

Life cycle of Amebiasis

A

1) Ingestion of contaminated food/water

2) Cysts are resistant to gastric content and pass through to Small intestine

3) In small intestine cysts excess to from trophozoites

4) Trophozoites multiple, colonize the mucus later od colon and form new cysts. Cysts and trophozoites exit in stool

44
Q

Amebiasis: Entamoeba Histolytica Tx

A

GOAL: Elimate invading trophozoites and eradicate intestinal carriage of organism

45
Q

Asymptomatic treatment of Amebiasis

A

Iodoquinol or paromomycin

46
Q

Intestinal disease treatment of Amebiasis

A

Metronizaole followed by paramomycin or iodoquinol

47
Q

extra intestinal disease treatment of Amebiasis

A

Metronizaole followed by paramomycin or iodoquinol

48
Q

Metronidazole MOA

A

Prodrug; requires reduction of nitro-group; generation of free radicals –>distruption of DNA –> cell death

49
Q

Metronidazole Clinical use

A

-Amebiasis, giardiasis, trichomoniasis

50
Q

Trinidazole Clinical use

A

-Amebiasis, giardiasis, trichomoniasis

51
Q

Paromomycin MOA

A

Therapy for amebiasis

Binding to 30s Subunit –> interere with initiation complex –< inhibition of protein synthesis

PK: Poor absorptioon, oral use only, not alone for treatment of extra intestinal disease

52
Q

Paromomycin Clinical use

A

Amebiasis (for symptomatic patients and together with metronidazole for pt with intestinal disease)

-Giardiasis

53
Q

Paromomycin AE

A

-GI
-Rash

54
Q

Iodoquinol MOA

A

-Unknown, effective against organisms in bowl lumen

55
Q

Iodoquinol AE

A

-GI (Mild Diarrhea) take with food
-Enlargement of thyroid

56
Q

Giardiasis species

A

Giardia Lambila

57
Q

Giardiasis forms

A

-Cysts (ingested form and visible outside body)
-Trophozoites (Pathology-causing, flagellated, destroyed by gastric acidity)

58
Q

Giardiasis Infection in body

A

1) Ingestion of contaminated food/water

2) Cysts are resistant to gastric content and pass through to Small intestine

3) In small intestine cysts excess to release 2 trophozoites

4) Trophozoites multiply in the small intestine and attach to villous surface of SI causing abdominal pain, cramping, and dystentery

59
Q

Giardiasis Disease

A

-Fatty, foul smelling diarrhea
-Patient with weakened immune system (HIV, cancer, transplant, elderly)

60
Q

Giardiasis Tx

A

-Metronidazole
-Tinidazole
-Nitazoxanide

ALL SYSTEMIC ACTION

-paromomycin (lower efficacy but safe in pregnancy) –> Luminal action

61
Q

Nitazoxanide MOA

A

Unknown, may interfere with electron transfer reaction

-Well absorbed
-Used for Giardiasis
-Crytispirudosis
-infectious diarrhea

61
Q

Nitazoxanide AE

A

-GI (Abdominal pain and diarrhea)

61
Q

Albendazole characteristics

A

Broad, mainly GI helminths

62
Q

Albendazole MOA

A

Interefres with microtubule synthesis (inhibits cell replication) and microtubule dependent glucose reuptake

63
Q

Albendazole PK

A

-Poor absorption (eat with fatty meal like peanuts or ice cream)
-metabolism: hepatic; rapid sulfoxidation to active metabolite

64
Q

Albendazole Clinical use

A

Effective in treating GI nematodes
(poor absorption doesn’t limit its use)

-Cysticercosis

65
Q

Albendazole AE

A

GI (mild or long term liver enzymes)

66
Q

Albendazole CI

A

-Pregnancy
-Hepatic Disease

67
Q

Pyrantel Pamoate MOA

A

Neuromuscular blocking agent –> causes Increase of Ash release and inhibition of Ache –> paralysis of the worm

68
Q

Pyrantel Pamoate PK

A

Poor absorption –> treatment of luminal organisms

69
Q

Pyrantel Pamoate clinical use

A

Intestinal helminths: roundworms (pinworms and hookworm)

70
Q

Pyrantel Pamoate AE

A

GI, Dizziness, elevation of liver enzymes

71
Q

Ivermectin MOA

A

GABA Agonist?
-Binds with glutamate-gated Cl channels (found only in vertebrate nerve and muscle cells) –> increase permeability of cell membranes to Cl ions –>hyperpolarization of nerve or muscle cell –> death of parasite

72
Q

Ivermectin PK

A

-Does not pass BBB (no CNS GABA effects, wide tissue distribution)

73
Q

Ivermectin clinical use

A

Several intestinal nematodes (NOT HOOKWORM)

74
Q

Ivermectin clinical use

A

Several intestinal nematodes (NOT HOOKWORM)
-Kills larval stage, not adult worms

-strongylodiassis (DOC)
-Onchoerciasais (river blindness) DOC

75
Q

Ivermectin AE

A

-GI
-Dermatological (pruitus)
-CI Pregnancy

76
Q

Praziquantel MOA

A

Increase membrane permeability to Ca –> cause marked contraction and then paralysis (promotes influx of Ca and possibly interacts with variant Ca-channel, which is found in schistosomones and praziquantel sensitive parcites

77
Q

Clinical use

A

-Schistomosiasis (DOC)
-Cysticerosias and intestinal tapeworms

PPP II (3 decks)

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