antiprotozoal- amoebiasis

Question 1

Which protozoa are included?

Answer 1

includes entamoeba histolytica, trichomonas vaginalis and giardia lamblia

Question 2

drugs against tissue amoebas

6 drugs

Answer 2

metronidazol,
tinidazol
ornidazol.
emetine.
dehydroemetine.
chloroquine

Question 3

drugs against amoebas in the intestine.

Answer 3

diloxanide
idoquinol
paromomycine.

Question 4

Iodoquinol
mechanism
kinetics.
adverse
clinical indications: 2

Answer 4

Mechanism of action: not fully understood

Pharmacokinetics: poor absorbtion given orally

Adverse: GI

Clinical indications:
1) in monotherapy for the treatment of intestinal asymptomatic amebiasis
2) in combination for the treatment of intestinal or
extraintestinal amebiasis

Question 5

Diloxanid furoat
Mechanism: 
Kinetics
Adverse
indication

Answer 5

Mechanism of action: not clear

Pharmacokinetics: its metabolite the diloxanid is absorbed

Adverse effects: GI

Clinical indications: alternative compound in asymptomatic amebiasisban

Question 6

Nitroimidazoles- Metronidazole, tinidazole
Mechanism
CLinical indication

Answer 6

Mechanism of action: reactive reduction products have cytotoxic effect

Clinical indications: in combination for intestinal and extraintestinal infections

Question 7

Paromomycin (aminoglycoside)

Answer 7

Mechanism of action: inhibits protein synthesis

Clinical indications: second line drug in intestinal and extraintestinal infections

Question 8

Treatment of giardiasis:

two options for treatment:

Answer 8

First line drugs
1) Nitroimidazoles: metronidazole, tinidazole.

2) Nitazoxanid: broad spectrum antiprotozoal drug, not clear mechanism of action, few side effects.

Second line drugs
1) Paromomycin (aminoglycoside): poor absorbtion given orally.

2) Furazolidon: nitrofuran, oral drug with mainly GI adverse effects
3) Quinacrin: broad spectrum antiprotozoal drug, well absorbed orally,
long elimination half life (5 days), mainly GI adverse effects

Question 9

Treatment of trichomoniasis

Answer 9

Nitroimidazoles: metronidazole, tinidazole

Question 10

Treatment of toxoplasma gondii infection:

3 options

Answer 10

first choice –

1) Spiramycin (in pregnancy), Sulfamethoxazole +Trimethoprim
2) Pyrimethamine + Clindamycin + folinic acid
3) alternative compounds: - Pyrimethamine + Sulfadiazine + folinic acid

Question 11

Treatment of pneumocystis jiroveci infection.

Answer 11

first choice – Sulfamethoxazole +Trimethoprim
alternative compounds:
- Pentamidine or Clindamycin + Primaquine
or Atovaquon

Question 12

Treatment of african trypanosomiasis (gambienese and rhodesience--> acute form):
- Eflornithin
mechanism:
Given- 2 forms.
adverse effects- 3
indicated for- "

Answer 12

mechanism: inhibits ornithin decarboxylase
- given mainly i.v., orally.
- severe adverse effects (GI, seizures, bone marrow
suppression) causes diarrhoea.
- indicated for advanced (CNS) cases

Question 13

Treatment of african trypanosomiasis (gambienese and rhodesience--> acute form):
- Melarsoprol - 
Mechanism:
Given- 1
Adverse: 4.

Answer 13

Mechanism: arsenic containing compound, enzyme inhibitory effect.
- given in slow infusion,
- adverse effects: GI, hepatotoxicity, arrhythmia,
encephalopathy.
- indicated in advanced (CNS) cases.

Question 14

Treatment of african trypanosomiasis (gambienese and rhodesience--> acute form):
Pentamidine
Mechanism:
Indicated- 3
given- 3
kinetics- 2
adverse- 5

Answer 14

Mechanism: effective against several protozoals
- unknown mechanism of action.
Given: IV, IM, aerosol.
Kinetics: half life is about 12 days, no CNS entry.

adverse effects: Pancreatic toxicity (hypoglycemia for some weeks then hyperglycemia), nephrotoxic, hallucination, arrhythmias, hypotension and more.

Indication:

1) it is used in early phase before the CNS involvement
2) other indication is the antimonial resistant leishmaniasis.
3) Pneumocystic jivoecii (usually used prophylatic).
4) it has fungicid effect as well.

Question 15

Treatment of african trypanosomiasis (gambienese and rhodesience--> acute form):
Suramin
Mechanism:
admin
adverse effects: 3
indicated:

Answer 15

• mechanism: – not fully undertsood mechanism of action (inhibits protein synthesis but enzymes as well)

administered i.v., long half life (40-50 days)

• adverse effects: kidney impairment, dermatitis, neuropathy.
• indicated in the early phase, before CNS involvement

Question 16

Treatment of american trypanosomiasis
1) Nifurtimox:
Mechanism:
indicated:
admin:
Adverse:

2) Benznidazol:
mechanism
Route
Adverse:

Answer 16

• Nifurtimox - might act by radical metabolites
• effective mainly in the acute phase
• administrated orally
• adverse effects: GI, neuropathy, seizures
• Benznidazol – inhibits protein synthesis and RNA synthesis
• administrated orally
• adverse effects: GI, neuropathy, psychosi

Question 17

Treatment of leishmaniasis:
Mention 4 drugs and which one do you use for which!
Leishmania donovani-> visceral and kala-azar disease.
leishmania tropia-> cutaneous leishmania.
L. Braziliensis-> mucocutaneous form.

Answer 17

Drugs used for the treatment:

1) Amphotericin B – mainly in the visceral leishmaniasis
2) Miltefosine – orally given in the visceral form

3) pentavalent antimonials:
A) sodium stibogluconate
B) meglumin antimoniat
intravenously administrated drugs for different
leishmania forms with few side effects. 
First choice drugs in mucocutaneous

Question 18

Pentamidine (Drugs used in leishamania)
mechanism
adminstration
adverse effects: 4 
reserved for?

Answer 18

• not fully understood mechanism of action (inhibits protein synthesis,
  inhibits DHFR?)
• parenteral administration
• severe adverse effects: arrhythmias, liver and kidney disturbances, Stevens-Johnson syndrome
• reserve compound in resistant cases

Question 19

sodium stibogluconate
admin- 2
mecha- 1
adverse: 4

Answer 19

administered IV or IM
mechanism unknown
adverse: GI myalgia, headache, QT prolongation.