Pharm Topic 16: Chemo For Protozoan Parasitic Infections

Front 1

Paromomycin Mech and uses

Back 1

Inhibits protein synth by binding to 30s ribosome. Used to treat Luminal phase of Entamoeba Histoltica.

Front 2

Paromomycin Pharmacokinetics (admin, distrib, elim)

Back 2

Given orally but is poorly absorbed, therefore is good for luminal parasites. Excreted in feces.

Front 3

Paromomycin Side effects and drug interactions

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SE: NVD, if absorbed, vertigo, nephro tox, oto tox.
DI: Decreses digitoxin serum []

Front 4

Trichomonas Vaginalis Life cycle, disease, and treatment

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STD, colonizes genitourinal tract. Humans only host.
Disease includes discharge, itching burning.
Treatment = Tinidazole

Front 5

Tinidazole Mech and uses

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Mech: Uses free radicals which react with DNA to kill protozoa.
Uses:
-Trichomonas vaginalis
-Giardia lamblia
-Systemic Entamoeba Histolytica

Front 6

Tinidazole pharmacokinetics (admin, distrib, elim)

Back 6

Admin: Oral, completely absorbed in SI.
Distrib: Widely distributed, including CNS
Elim: Metabolized by CYP3A4 and excreted in urine.

Front 7

Tinidazole Side effects and Drug Interactions

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SE: NVD, metallica taste, rarely siezures, peripheral neuropathy, leuko/neutropenia.
DI: Mixing w/ alcohol can give disulfiram Rx. Effected by CYP3A4 inducers and inhibitors.

Front 8

Giardia Lamblia Life cycle, disease, and treatment

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LC: Inhabits SI, can go to colon where it trasnforms into a cyst, which can be spread via fecal oral.
Dis: Massive diarrhea, pain, malabsorbtion.
Treat: Tinidazole

Front 9

Entamoeba Histolytica Life cycle, disease, and treatment

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LC: Lives in large intestine, but can travel into tissue like liver and lung.
Dis: Bloody stools, liver/lung abcesses.
Treatment: Luminal disease - Paromomycin. Systemic disease - Tinidazole (tinidazole is absorbed in SI and therefore does not make it to colon, therefore need to also give paromomycin).

Front 10

Trypanosoma Brucie Life Cycle, Disease, treatment

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LC: Tse Tse fly bite gets bug into blood, eventually goes to every organ in body including CNS.
Disease: Sleeping sickness. Starts with fever, enlarged nodes, then get CNS involvement and death. 2 types: gambiense is slower, rhodesiense is faster.
Treat: Non CNS = Suramin, Pentamidine (gambiense only). CNS involvement = Melarsoprol, Eflornithine (gambiense only).

Front 11

Suramin Mech and uses

Back 11

Mech: Disrupts energy metabolism.
Used for the non CNS phase of Trypanosoma brucei.

Front 12

Suramin Pharmacokinetics (admin, distrib, elim)

Back 12

Admin: IV
Distrib: Stays in blood, bound to protein
Elim: Not metabolized

Front 13

Suramin Side effects and Drug interactions

Back 13

SE: Pretty toxic. NVD, photophobia, periph neropathy. Kidney damage, blood dyscracias and shock.

Front 14

Pentamidine Mech and uses

Back 14

Mech: Enters via purine transporter and binds to DNA and Topoiso 2.
Disease: Used for Non CNS Trypanosoma brucei gambeinse (not rhodesiense).
Inhilation of aerosols is also used as pneumocysts prophylaxis for aids patients.

Front 15

Pentamidine pharmacokinetics (admin, distrib, elim)

Back 15

Admin: IV
Distrib: No CNS activity, bound to protein

Front 16

Pentamidine side effects and drug interactions

Back 16

SE: Headache, dizziness, breathlessness bracnhycardia, impaired renal function, hypoglycemia, and diabetes.

Front 17

Melarsoprol mech and uses

Back 17

Mech: Reacts with sulfhydrol groups of enzymes involved in generating ATP or in trypanothine production. Mamalian cells arent as effected b/c we can inactivate the drug.
Used to treat CNS involved Trypanosoma brucei.

Front 18

Melarsoprol pharmacokinetcs (admin, distrib, elim)

Back 18

Admin: IV
distrib: Has CNS activity
Elim: Renal

Front 19

Melarsoprol Side effects and drug interactions

Back 19

SE: Encephalopathy, peripheral neropathy, phlebitis myocardial dmg, and hemolytic anemia in G6 deficient.
If one relapses from rhodesiense, second treatment will work.
If one relapses from gambiense, second treatment will probably fail as well.

Front 20

Eflornithine Mech and uses

Back 20

Mech: Inhibits ornithine decarboxylase which is necessary for protein synth.
Used to treat Trypanosoma brucei gambiense (only) with CNS activity.

Front 21

Eflornithine pharmacokinetics (admin, distrib, elim)

Back 21

Admin: Can be given oral
Distrib: Enters CNS, no protein
Elim: Renal

Front 22

Eflornithine side effects and drug interactions

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SE: Anemia, Leikopenia, seizures, thrombocytopenia, DNV.
DI: Additive BM suppression with BM suppressive drugs. Additive ototox with aminoglycosides.

Front 23

Trypmanosoma Cruzi Life cycle, disease, Treatment

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LC: Caused by bed bugs, can get Ramani's sign, has extracellular (acute) and intracellular (chronic) stage.
Disease: Chagas disease
Treatment: Acute = Nifurtimox, Chronic = untreatable.

Front 24

Nifurtimox Mech and uses

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Mech: Works via free radicals and superoxide anions. Humans can inactivate, parasites cant.
Used for Acute phase of Trypmanosoma Cruzi

Front 25

Nifurtimox Pharmacokinetics (admin, distrib, elim)

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Admin: Oral
Distrib: Well
Elim: Hepatic

Front 26

Nifurtimox side effects and drug interactions

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SE: Anorexia, NV, ataxia, insomnia, dementia, and seizures, periipheral neuropathy.
DI: Alcohol may increase CNS side effects.

Front 27

Leishmania life cycle, disease, Treatment

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LC: L tropica and L braziliensis stay mostly at skin and lymph. Donovani becomes systemic through macs.
Disease: Trop and Braz are cutaneous ulcers. donovani leads to systemic Kala azar leading to wasting, anemia, hepatosplenomegaly and death.
Treat: Sodium Stibogluconate

Front 28

Sodium Stibogluconate mech and uses

Back 28

Mech: Interferes with glycolysis and FA oxidation.
Used to treat Leishmania

Front 29

Sodium Stibogluconate pharmacokinetcs (admin, distrib, elim)

Back 29

Admin: Parenternally repeatedly.
Elim: Renal

Front 30

Sodium Stibogluconate Side effects and drug interactions

Back 30

SE: Thrombophlebitis, NVD, myalgia, arthralgia, headache.

Front 31

Plasmodium Life cycle, disease, treatment

Back 31

LC: P.falciparum and P.malariae once leave liver and enter erythrocyic phase are out of liver. P.vivax and P. ovale keep a reserve in the liver.
Disease: Malaria. Flaciprum infects all ages of RBCs
Treatment: Extra-erythrocytic = primaquine.
Erythrocytic = Chloroquine, Mefloquine, Pyrimethamine and sulfadoxine, Atovaquone and proguanil.

Front 32

Chloroquine Mech and uses

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Mech: Weak base, sits in malaria food vacuoles, prevents heme polymerization, accumulation causes death.
Used to treat erythrocytic phase of malaria

Front 33

Chloroquine pharmacokinetics (admin, distrib, elim)

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Admin: Oral
Elim: Renal

Front 34

Chloroquine Side effects and drug interactions

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SE: Headache, vomiting, skin probs, alopecia, hemolytic anemia in G6 deficient and prolonged QT interval.
DI: Aluminum/magnesium decrease absorbtion, drugs that prolong QT can be additive.

Front 35

Mefloquine Mech and uses

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Mech: Similar to chloroquine, accumulated in vacuole, but does not inhibit heme polymerase.
Used for erythrocytic cycle of malaria.

Front 36

Mefloquine pharmacokinetics (admin, distrib, elim)

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Admin: Oral
Distrib: Enters CNS
Elim: Hepatic

Front 37

Mefloquine side effects and drug interactions

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SE: Nausea, dizziness, nightmares, ataxia, bracycardia. Not for preg.
DI: Too much brachy with BBs, Dont give with drugs that prolong QT

Front 38

Pyrimethamine and sulfadoxine Mech and uses

Back 38

Mech: Pyrimthamine inhibits dihydrofolate reductase, Sulfadoxine interfers with dihydropteroate synthase.
Used for erythrocytic phase of malaria. Used in combo to reduce resistance.

Front 39

Pyrimethamine and sulfadoxine pharmacokinetcs (admin, distrib, elim)

Back 39

Admin: Oral
Distrib: Bound to protein
Elim: Metabolized by liver, excreted by kidney.

Front 40

Pyrimethamine and sulfadoxine side effects and drug interactions

Back 40

SE: Folic acid deficiency, megoblastic anemia, BM suppression, NV, insomnia, steven-johnson syndrome.
DI: Additive BM suppression

Front 41

Atovaquone and proguanil Mech and uses

Back 41

Mech: Atovaquone inhibits parasite mitochondrial electron transport via cytochrome c. Proguanil is metabolized to an active metabolie which inhibits dyhydrofolate reductase.
Used to treat erythrocytic cycle of malaria.

Front 42

Atovaquone and proguanil phrmacokinetics (admin, distrib, elim)

Back 42

Admin: Oral
Distrib: Protein bound
Elim: Atv. eliminated fecal. Pro is converted to an active metabolite, excreted in urine.

Front 43

Atovaquone and proguanil side effects and drug interactions

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SE: NVD, abdominal pain, headache, dizziness, not for preg.
DI: Ato levels decrease when given with tetracycline, rifampin, or metoclopramide.

Front 44

Primaquine Mech and uses

Back 44

Mech: Interferes with pyrimidine syth and mito electron transport. Used for exo-erythrocytic phase of malaria.

Front 45

Primaquine pharmacokinetcs (admin, distrib, elim)

Back 45

Admin: Oral
Elim: metabolized by liver, excreted in urine.

Front 46

Primaquine Side effects and drug interactions

Back 46

SE: NVD, Leukopenia, neutropenia, hemolytic anemia in G6 deficient.
DI: Additive bone marrow suppression.

Front 47

Tertacycline and doxycyline Mech and uses

Back 47

Mech: Inhibit protein translation.
Used for malaria or for prophylaxis to malaria. Not given to pregnant women and kids under 8.

Front 48

Which drugs cause hemolytic anemia in G6 deficient patients.

Back 48

Many children play piano softly:
Melarsoprol, chloroquine, primaqine, Pyrimethamine-sulfadoxine.

Front 49

Which drug has renal tox?

Back 49

Pentamidine

Front 50

Which drugs are not for preg?

Back 50

Pre Menopausal:
Pentamidine, Malarone (Atovaquone and proguanil)

Front 51

Which drugs delay QT?

Back 51

Cardiac Malfunction:
Chloroquine, Mefloquine

Front 52

Which drug is affected by p450?

Back 52

Tinidazole