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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
Artesunate, Artemether, Dihydroartermisinin CI
-First trimester of Pregnancy -Children <5 kg
26
Atovaquone and Proguanil (Malarone) Characteristics
Chemoprophylaxis with single folate antagonist no longer recommended --> combo regimens
27
Atovaquone and Proguanil (Malarone) MOA
-Proguanil inhibits DHFR -Atovaquone: Disrupts mitochondrial electron transport in parasite --> disrupt nucleotide synthesis
28
Atovaquone and Proguanil (Malarone) Clinical Uses
Treatment and prophylaxis os chloroquine-resistant P. falciparum
29
Atovaquone and Proguanil (Malarone) AE
-GI -Mild and reversible elevation of liver enzymes
30
Atovaquone and Proguanil (Malarone) CI
Pregnancy
31
Tetracycline, Doxy and Clindamycin MOA
Inhibition of protein synthesis in parasite apicoplast -Slow acting blood schizonticides
32
Tetracycline, Doxy and Clindamycin Clinical use
-Alone for chemoprophylaxis -Ineffective as single agents for malaria treatment --> use in conjunction with quinine
32
Tetracycline, Doxy and Clindamycin AE
-GI -Bone structures -Photoxicity DDI: Interactions to Antacids CI: Preg and children
33
What categories do you think of for uncomplicated malaria?
-Non-Falciparum -Falciparum
34
What categories do you think of for P.Malariae?
-Non-Falciparum Chloroquine or hydroxy.
35
What categories do you think of for P.Ovale and P.vivax?
-Non-Falciparum Chloroquine or hydroxy. PLUS Primaquine (If not G6PD Def)
36
What categories do you think of for Falciparum Malaria?
-Acquired in chloroquine sensitive area -Acquired in chloroquine resistant area -Acquired in mefloquine resistant area
37
What do you treat for Acquired in chloroquine sensitive area
Chloroquine or hydroxy.
38
What do you treat for Acquired in chloroquine resistant area?
-Atov-Pro OR -Artemtether-Lum, OR -Quinine plus Tetra or doxy or clinda OR Mefloquine
39
What do you treat for Acquired in mefloquine resistant area?
-Atov-Pro OR -Artemtether-Lum, OR -Quinine plus Tetra or doxy or clinda
40
What do you treat for complicated malaria
Artesunate (Iv) Switch to oral med to complete regimen
41
Amebiasis Species
Entamoeba Histolytica
42
Two forms of Entamoeba Histolytica
-Cyst -Trophozoite (motile feeding form, causes pathology, invasive disease)
43
Life cycle of Amebiasis
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
Amebiasis: Entamoeba Histolytica Tx
GOAL: Elimate invading trophozoites and eradicate intestinal carriage of organism
45
Asymptomatic treatment of Amebiasis
Iodoquinol or paromomycin
46
Intestinal disease treatment of Amebiasis
Metronizaole followed by paramomycin or iodoquinol
47
extra intestinal disease treatment of Amebiasis
Metronizaole followed by paramomycin or iodoquinol
48
Metronidazole MOA
Prodrug; requires reduction of nitro-group; generation of free radicals -->distruption of DNA --> cell death
49
Metronidazole Clinical use
-Amebiasis, giardiasis, trichomoniasis
50
Trinidazole Clinical use
-Amebiasis, giardiasis, trichomoniasis
51
Paromomycin MOA
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
Paromomycin Clinical use
Amebiasis (for symptomatic patients and together with metronidazole for pt with intestinal disease) -Giardiasis
53
Paromomycin AE
-GI -Rash
54
Iodoquinol MOA
-Unknown, effective against organisms in bowl lumen
55
Iodoquinol AE
-GI (Mild Diarrhea) take with food -Enlargement of thyroid
56
Giardiasis species
Giardia Lambila
57
Giardiasis forms
-Cysts (ingested form and visible outside body) -Trophozoites (Pathology-causing, flagellated, destroyed by gastric acidity)
58
Giardiasis Infection in body
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
Giardiasis Disease
-Fatty, foul smelling diarrhea -Patient with weakened immune system (HIV, cancer, transplant, elderly)
60
Giardiasis Tx
-Metronidazole -Tinidazole -Nitazoxanide ALL SYSTEMIC ACTION -paromomycin (lower efficacy but safe in pregnancy) --> Luminal action
61
Nitazoxanide MOA
Unknown, may interfere with electron transfer reaction -Well absorbed -Used for Giardiasis -Crytispirudosis -infectious diarrhea
61
Nitazoxanide AE
-GI (Abdominal pain and diarrhea)
61
Albendazole characteristics
Broad, mainly GI helminths
62
Albendazole MOA
Interefres with microtubule synthesis (inhibits cell replication) and microtubule dependent glucose reuptake
63
Albendazole PK
-Poor absorption (eat with fatty meal like peanuts or ice cream) -metabolism: hepatic; rapid sulfoxidation to active metabolite
64
Albendazole Clinical use
Effective in treating GI nematodes (poor absorption doesn't limit its use) -Cysticercosis
65
Albendazole AE
GI (mild or long term liver enzymes)
66
Albendazole CI
-Pregnancy -Hepatic Disease
67
Pyrantel Pamoate MOA
Neuromuscular blocking agent --> causes Increase of Ash release and inhibition of Ache --> paralysis of the worm
68
Pyrantel Pamoate PK
Poor absorption --> treatment of luminal organisms
69
Pyrantel Pamoate clinical use
Intestinal helminths: roundworms (pinworms and hookworm)
70
Pyrantel Pamoate AE
GI, Dizziness, elevation of liver enzymes
71
Ivermectin MOA
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
Ivermectin PK
-Does not pass BBB (no CNS GABA effects, wide tissue distribution)
73
Ivermectin clinical use
Several intestinal nematodes (NOT HOOKWORM)
74
Ivermectin clinical use
Several intestinal nematodes (NOT HOOKWORM) -Kills larval stage, not adult worms -strongylodiassis (DOC) -Onchoerciasais (river blindness) DOC
75
Ivermectin AE
-GI -Dermatological (pruitus) -CI Pregnancy
76
Praziquantel MOA
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
Clinical use
-Schistomosiasis (DOC) -Cysticerosias and intestinal tapeworms

PPP II (3 decks)

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