Antiprotozoal drugs Flashcards
Chagas disease specific drugs
Nifurtimox
Ni Fur Ti Mox
and
Benznidazole
Only slows progression, not curative or halting, most effective in the acute phase.
SEs: GI Neuropathic Insomania Seizures
What are the trypanosomes
Bruci and Cruzi
Trypanosomas brucei gambiense and rhodesiense
cause sleeping sickness
and
Trypanosomas cruzi -
causes chagas disease
Drugs for trypanosomiasis without CNS involvment
Suramin
Pentamidine
Pentamidine - also a blood schizonticide for vivax and ovale malria.
Mechanism of the nitroimidazole class.
Metronidazole is of the nitroimidazole class. It inhibits nucleic acid synthesis by disrupting the DNA of microbial cells.[1] This function only occurs when metronidazole is partially reduced, and because this reduction usually happens only in anaerobic cells,
Drugs for Trypanosomiasis with CNS infection
Melarsoprol - arsenic based drug with high toxicity. Only for advanced trypanosomiasis.
many side effects, including cerebral edema, seizures, coma, and death.
Eflornithine - Inhibits Ornithine Decarboxylase.
Also many SEs,
Seizures
Thrombocytopenia and Leukocytopenia.
Drugs for Leishmania
For visceral leishmaniasis: Amphotericin B.
For Mucocutaneous form:
Sodium Stibogluconate
Miltefosine
few side effects
Pentamidine: reserved for resistant cases. Unclear mechanism. Parenteral administration. Severe SEs. Stevens-Johnson syndrome Arrythmias Liver and kidney toxicity.
Drugs for tissue amoebiasis:
Metronidazol
Tinidazol
Ornidazol
Produce cytotoxic products in the presence of anaerobic metabolism.
Nitazoxanide: Broad spectrum anti-protozoal drug, unknown mechanism. low side effects.
Emetine
Derived from the Emetic Ipecac. inhibit protein and DNA synthesis.
Paramycin
Aminoglycoside that inhibits the 30S ribosomal prokaryotic subunit. 2nd line for extraintestinal infecitons.
Drugs for intestinal ameobiasis
Paramycin - aminoglycoside
Diloxanide - unclear mechanism
Idoquinol - unclear mechanism
Have poor absorption and thus high action in the intestine.
name some amoeba infections
Giardia lamblia
Entamoeba histiolytica.
Trichomonas vaginallis
Metronidazole side effects
The Disulfuram like reacion with alcohol
Immediate hangover, vomiting nausea
Tachycardia and palpitations
Metallic taste
Giardia drugs
Metronidazole, Tinidazole
Nitazoxanide
2nd line: paramycin
Trichomonas vaginalis drugs
Nitroimidazoles
Metronidazole and Tinidazole
Toxoplasma gondii drugs
Spiramycin for preggos.
DoC: Sulfamethoxazole and Trimethoprim.
Pneumocystis jiroveci drugs
Sulfamethoxazole and Trimethoprim
Side effects of Sulfamethoxazole and Trimethoprim
The combination potently inhibits the generation of tetrahydrofolate. Sulfonamides -( dihydrofolate synthesis, Trimethoprim -( Dihydrofolate reductase and Tetrahydrofolate synthesis.
Skin rash, potentially lethal Stevens Johnson syndrome
Toxic Edpidermal Necrosis
Thrombocytopenia (no THF, no replicating cells)
Leukocytopenia
Hepatitis
Hyperkalemia
Antihelmithic drugs, just list them
nematodes - roundworms
trematodes - flukes
cestodes - tapeworms
Benzimidazoles Ivermectin Praziquantel Levamisol Niclosamide Pyrantel Pamoate Bithionol
Benzimidazoles, drugs and mechanism
Targets
Albendazole, Mebendazole, Tiabendazole
Inhibits tubulin polymerization of the worms.
Paralysis and death.
Roundworms and Tapeworms. Nematodes and Cestodes.
Extra-intestinal helminth treatment.
Benzimidazoles SEs
GI
Hepatotoxic
Visual disturbance
Teratogenic
Ivermectin mechanism, targets, distribution
SEs
Mechanism: enhances GABA signaling in the worms, paralysis
Oral admin and does not cross the BBB
minimal/no SEs, are only due to inflammation from the worms dying and causing inflammation.
targets: Roundworms. Filariasis, Ascaris lumbricoides, Ancylostoma duodenale, Tricuris trichuria (pinworms)
Niclosamide
mechanism, targets, SE
Inhibits oxidative phosphoylation of Tapeworms
Poor absorption, given orally to work in the intestine. Niclosamide iNtestinal
thus, SEs are mild and essentially just intestinal too.
Targets: Taenia solium and saginata.
Pyrantel Pamoate
mechanism, targets, SE
Inhibits worm AChE and stimulates acetylcholine release.
Depolarizing paralysis.
Orally and poor absorption.
Significant GI side effects and moderate CNS ones.
Axcaris, Necator, Ancylostoma, Enterobius.
Praziquantel
Increases Ca++ permeability of the worm and causes spastic paralysis.
Oral, good absorption and CNS penetration.
SEs:
GI and Dizziness.
Given against flukes and tapeworms.
Levamisol
Depolarizing blockade and paralysis
Oral
GI side effects, mild neurological effects.
Good for roundworms, ascaris lumbricoides, Necator Americanus
Ancylostoma duodenale
Bithionol
Inhibits oxidative phosphorylation, like niclosamide,
but its for Flukes instead of tapeworms.
Specifically its for
Fasciola hepatica, liver fluke.
Its main SE is also Toxic Hepatitis
as well as GI and CNS effects, dizziness, headache.
