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pharma C.DAM > 3. Antiprotozoal and antihelminthic drugs > Flashcards

3. Antiprotozoal and antihelminthic drugs Flashcards

1
Q

protozoal infection

A 
Malaria
Amoebiasis
Trypanosomiasis
Leishmaniasis
toxoplasmosis
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2
Q

Malaria stages

A

liver form
erythrocytes form
gametocytes

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3
Q

drugs act on liver form

A

schizonticides

drug - Primaquine

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4
Q

drugs act on erythrocytes form

A

schizonticides

drugs ...
Chloroquine
Mefloquine
Quinine
Artemisinins
Pyrimethamine
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5
Q

drugs act on gametocytes

A

Gametocides

drug - Primaquine

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6
Q

Primaquine

A

schizonticides

Administration: Oral

Given for: P.vivax and ovale (persistent forms)
act on the liver form

Contraindications: G6PD deficiency (testing is obligatory before usage), pregnancy

Adverse effects: well tolerated, with higher dose: GI, rarely leucopenia, methemoglobinemia, hypersensitivity

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7
Q

Chloroquine

A

schizonticides
_concentrates in parasites, inhibit DNA transcription and replication, inhibits heme-polymerase

act on the erythrocytes form
DOC in treatment of P. falciparum malaria (not in resistant strains)

Kinetics: good oral absorption, accumulation in the tissue, penetrate the CNS and traverse the placenta
half-life: 5days (loading dose is necessary)

Adverse effects: well tolerated if not too high dose is given
GI symptoms, visual disturbances (cornea and retina deposits), dizziness, headache, pruritus, QT prolongation

Contraindications: psoriasis, porphyry

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8
Q

Mefloquine

A

schizonticides
act on the erythrocytes form

Pharmacokinetics: good oral absorption | wide distribution | excreted via bile
Clinical use: in MDR forms of P.falciparum, prophylaxis in case of known resistance
Adverse effects: GI and CNS (depression and other psychosis, hallucination, neuropsychiatric reactions), ECG abnormalities

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9
Q

Quinine

A

schizonticides
MOA: interference with heme polymerisation

Pharmacokinetics: Oral | well distributed

act on the erythrocytes form
Clinical use: Severe infection and chloroquine resistant malaria

Adverse effects: quinism (nausea, vomiting tinnitus and vertigo - reversible), QT prolongation, hemolytic anemia
Potentiates neuromuscular blocking agents and elevation of digoxin levels

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10
Q

Artemisinins

A

schizonticides
MOA: most likely creating free radical
Not used as monotherapy though there is no resistance so far

Pharmacokinetics: good absorption (p.o.; IV; IM; rectal)

act on the erythrocytes form
Recommended first-line treatment for MDR P.falciparum malaria
Artesunate + sulfadoxine -
pyrimethamine/mefloquine/amodiaquine
Artemether + lumefantrine

Well tolerated – rarely anemia
High dose QT prolongation & HS

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11
Q

Pyrimethamine

A

schizonticides
act on the erythrocytes form
inhibits dihydrofolate reductase (also affect as a sporontocide - mosquitoes)

In combination with artemisinin derivatives (p.falciparum)
Sulfadiazine + pyrimethamine => against Toxoplasma gondii

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12
Q

first-line treatment for MDR P.falciparum malaria

A

Artesunate + sulfadoxine -
pyrimethamine/mefloquine/amodiaquine
Artemether + lumefantrine

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13
Q

combination of drugs against Toxoplasma gondii

A

Sulfadiazine + pyrimethamine
Pyrimethamine + clindamycin
Trimethoprim + sulfamethoxazole

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14
Q

Primaquine

A

acts on all types of plasmodium gametocytes are destroyed

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15
Q

Amoebiasis location

A

Tissue & luminal

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16
Q

Trypanosomiasis drugs

A 
Pentamidine
Suramin
Melarsoprol
Eflornithine
Nifurtimox
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17
Q

Leishmaniasis location

A

Visceral & Cutaneous

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18
Q

treatment against Tissue amoebas

A

Metronidazole
Tinidazol
Dehydroemetine
Chloroquine

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19
Q

treatment against Luminal amoebas

A

Iodoquinol

Paromomycin

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20
Q

Metronidazole

A

Produces toxic intermediate metabolites (reduction of N2O group) in anaerobic conditions
Bactericidal (and amebicidal)

Spectrum: Anaerobic bacteria (bacteroides and clostridium) | Protozoa (trichomonas, G.lamblia, amoeba, entameba histolytica)

Distribution: good absorption, wide distribution (CNS and abscesses) vaginal and seminal fluids, saliva, breast milk
Administration: Oral, IV and topical
Metabolism: Hepatic oxidation (CYP450) and glucuronidation
Excretion: Urine

Adverse effects: GI (nausea), metallic taste, alcohol-intolerance (disulfiram-like reaction)

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21
Q

Tinidazol

A

2nd generation metronidazole

like metronidazole BUT shorter course of treatment, more expensive

22
Q

Dehydroemetine

A

inhibits protein synthesis

IM injection

23
Q

Chloroquine

A

used in combination with Metronidazole

treats liver abscesses &
for treatment of Tissue amoebas

24
Q

Iodoquinol

A

amoebicidal
E.Histolytica
against Luminal amoebas

no absorption

AE: GI, dose related neuropathy

25
Q

Paromomycin

A

aminoglycoside

amoebicidal
E.Histolytica
against Luminal amoebas

26
Q

Pentamidine

A

Interferes with DNA, RNA, phospholipids and protein synthesis

Spectrum: trypanosoma brucei gambiense (specifically first stage, no CNS involvement), pneumocystis jiroveci

Kinetics: IM or IV
wide distribution but do no enter CNS
exerted slowly in the urine

Adverse effect: renal dysfunction, pancreatitis

27
Q

Suramin

A

Trypnosomicidal

Spectrum: trypanosoma brucei Rhodesiense (specifically first stage, no CNS involvement)

Kinetics: IV
do no enter CNS

Adverse effect: GI, neurological, shock and more!

28
Q

Melarsoprol

A

Only drug for 2nd stage

Spectrum: trypanosoma brucei Rhodesiense (2nd stage, including CNS involvement)

Kinetics: slow IV

Adverse effect: Encephalopathy, peripheral neuropathies

29
Q

Eflornithine

A

Mechanism of action: inhibits ornithine decarboxylase (irreversible)

Administration: oral or IV

For advanced CNS African trypanosomiasis due to T. b. gambiense (first-line treatment for 2nd stage, CNS involvement)
Other indications: topical solution is used as treatment for unwanted facial hair in women

Adverse effects: Anemia, seizures, temporary hearing loss

30
Q

Nifurtimox

A

Administration: oral

for Trypanosoma cruzii (Chaga’s disease) | 2nd stage T. b. gambiense in combination with eflornithine
Not fully effective, cannot prevent the progression

MOA: generates free radicals → causes toxicity

Excreted in the urine

Adverse effects: GI, peripheral neuropathy, Hypersensitivity

31
Q

Drugs for Leishmaniasis

A

Sodium stibogluconate
Miltefosine
Amphotericin B
Ketoconazol

32
Q

drugs for Visceral leishmaniasis

A

Miltefosine

Amphotericin B

33
Q

drugs for Cutaneous leishmaniasis

A

Ketoconazol

34
Q

Sodium stibogluconate

A

pentavalent antimony (Sb) containing compound

Administration: IV or IM
Distribution: Extravascular

Adverse effects: GI, myalgia, arthralgia, headache, QT-prolongation, rarely hepato-cardio and nephrotoxic

35
Q

Amphotericin B

A

MOA: binds to ergosterol and alters the membrane permeability

Pharmacokinetics: Good distribution, does not enter CNS
Plasma half-life: 15 days
Lipid formulation has better effect and smaller toxicity
Administration: parenterally (IV microcolloid infusion or liposome packed) | intrathecally for candida meningitis | larger amounts can be given in lipid formulation

Spectrum: broad
Candida spp. Cr. Neoformans, aspergillus, dimorphs
Some protozoans (Leishmania and Trypanosoma)

Adverse effects: Low TI | Infusion related toxicity – fever, chills, anemia, thrombophlebitis | Kidney damage, hypotension

36
Q

Miltefosine

A

Interferes with phospholipids in the parasite

teratogenic

37
Q

Treatment of toxoplasmosis

A 
Leucovorin 
Combination of...
Pyrimethamine + clindamycin
Trimethoprim + sulfamethoxazole
sulfadiazine + pyrimethamine
38
Q

Leucovorin

A

is commonly administered to protect against folate deficiency

39
Q

Trimethoprim + sulfamethoxazole

A

combination used for prophylaxis of toxoplasmosis and infections caused by P. jirovecii in immunocompromised patients

40
Q

types helminthin

A

nematodes
trematodes
cestodes

41
Q

Treatment of nematodes

A

Benzimidazoles
Pyrantel pamoate
Ivermectin
Diethylcarbamazine (DEC)

42
Q

Treatment of trematodes

A

Praziquantel

43
Q

Treatment of cestodes

A

Albendazole
Praziquantel
Niclosamid

44
Q

types Benzimidazoles

A

Mebendazole
albendazole
thiabendazole

45
Q

Mebendazole
albendazole
thiabendazole

A

Mechanism of action: Inhibition of polymerization of microtubules and glucose uptake

Good agents against roundworms and tapeworms | also treats fungal

Orally given 
absorption enhanced by high fat meal 
wide distribution
Metabolized in the liver 
excreted by the bille

Adverse effects: Hepatotoxicity (in long treatment - hydatid), (Mebendazole - teratogenic, GI)

46
Q

Pyrantel pamoate

A

Poorly absorbed orally - acts intraluminal in the GI

MOA: neuromuscular blocking agent (ACh release → causing paralysis)

Adverse effects are mild

47
Q

Ivermectin

A

Enhances glutamate gated Cl- channels → paralysis → death

DOC: Strongyloides, cutaneous larva migrans, onchocerca volvulus

Orally given

Adverse effects: teratogenic, mazzotti reaction in the case of onchocerca (fever, headache, dizziness, somnolence, hypotension)

48
Q

Diethylcarbamazine (DEC)

A

MOA: immobilizes microfilariae and alters its surface structure

DOC: filariasis (wuchereria bancrofti)

Orally given

Adverse effects: mild + transient: headache, nausea, vomiting

49
Q

Praziquantel

A

MOA: increases Ca2+ permeability leading to paralysis

Effective against flukes (schistosoma) and tapeworms (taenia saginata, taenia solium)

Orally given (with food)
penetrates through BBB

Adverse effects: nausea, abdominal pain, fever, headache, dizziness, malaise.

Contraindicated in: ocular cysticercosis

50
Q

Niclosamide

A

Treatment of cestodes

inhibits oxidative phosphorylation

pharma C.DAM (17 decks)

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