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

3. Antiprotozoal and antihelminthic drugs Flashcards

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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

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A

2nd generation metronidazole

like metronidazole BUT shorter course of treatment, more expensive

22
Q

Dehydroemetine

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A

inhibits protein synthesis

IM injection

23
Q

Chloroquine

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A

used in combination with Metronidazole

treats liver abscesses &
for treatment of Tissue amoebas

24
Q

Iodoquinol

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A

amoebicidal
E.Histolytica
against Luminal amoebas

no absorption

AE: GI, dose related neuropathy

25
Paromomycin
aminoglycoside amoebicidal E.Histolytica against Luminal amoebas
26
Pentamidine
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
Suramin
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
Melarsoprol
Only drug for 2nd stage Spectrum: trypanosoma brucei Rhodesiense (2nd stage, including CNS involvement) Kinetics: slow IV Adverse effect: Encephalopathy, peripheral neuropathies
29
Eflornithine
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
Nifurtimox
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
Drugs for Leishmaniasis
Sodium stibogluconate Miltefosine Amphotericin B Ketoconazol
32
drugs for Visceral leishmaniasis
Miltefosine | Amphotericin B
33
drugs for Cutaneous leishmaniasis
Ketoconazol
34
Sodium stibogluconate
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
Amphotericin B
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
Miltefosine
Interferes with phospholipids in the parasite | teratogenic
37
Treatment of toxoplasmosis
``` Leucovorin Combination of... Pyrimethamine + clindamycin Trimethoprim + sulfamethoxazole sulfadiazine + pyrimethamine ```
38
Leucovorin
is commonly administered to protect against folate deficiency
39
Trimethoprim + sulfamethoxazole
combination used for prophylaxis of toxoplasmosis and infections caused by P. jirovecii in immunocompromised patients
40
types helminthin
nematodes trematodes cestodes
41
Treatment of nematodes
Benzimidazoles Pyrantel pamoate Ivermectin Diethylcarbamazine (DEC)
42
Treatment of trematodes
Praziquantel
43
Treatment of cestodes
Albendazole Praziquantel Niclosamid
44
types Benzimidazoles
Mebendazole albendazole thiabendazole
45
Mebendazole albendazole thiabendazole
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
Pyrantel pamoate
Poorly absorbed orally - acts intraluminal in the GI MOA: neuromuscular blocking agent (ACh release → causing paralysis) Adverse effects are mild
47
Ivermectin
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
Diethylcarbamazine (DEC)
MOA: immobilizes microfilariae and alters its surface structure DOC: filariasis (wuchereria bancrofti) Orally given Adverse effects: mild + transient: headache, nausea, vomiting
49
Praziquantel
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
Niclosamide
Treatment of cestodes | inhibits oxidative phosphorylation

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