Drugs Flashcards
How does Levodopa become DA?
L-aromatic amino acid decarboxylase
Sinemet
Levodopa + Carbidopa
Entacapone
COMT inhibitor –> stops metabolism of Levodopa in periphery
Selegiline
Mono-amine oxidase (MAO) inhibitor
Blocks MAO-A and MAO-B (this metabs. DA):
smooths “on-off”
Pramipexole
DA receptor agonist (D2 specific)
Trihexyphenidyl
muscarinic antagonist
used to treat Parkinson’s
Corrects ACh:DA balance… mech unclear
Symmetrel (Amantadine)
NMDA receptor antagonist
Pentamidine
binds DNA
does not cross BBB
use for trypanosoma brucei stage 1
Suramin
(mech unknown)
does not cross BBB
toxic!!
Stage 1 Trypanosoma brucei
Benznidazole and Nifurtimox
mech: increases ROS, via NADH-dependent dehydrogenase
does not cross BBB
Stage 1 trypanosoma brucei
Arsenicals (Melarsoprol)
Use for stage 2 rhodesiense trypanosoma brucei (ASS)
very toxic/death!
crosses BBB
Eflornithine
inhibits ornithine decarboxylase
–static (doesn’t kill)
less toxic
Stage 2 trypanosoma brucei
Eflornithine + Nifurtimox
Eflornithine (-static) crosses BBB
Nifurtimox (-cidal) does not cross BBB
Late stage 2 trypanosoma brucei
Sodium stibogluconate + Meglumine antimonate
used for trypanosoma cruzi = Chagas disease (leishmaniasis)
stops glycolysis and FA beta-ox
Liposomal Amphotericin B
Use for tyrpanosoma cruzi = Chagas disease
Only visceral leishmasiasis (splenomegaly)
use for resistant strains
Sulfadiazine + Pyrimethamine
folate antagonist combo
Toxoplasma gondii (toxoplasmosis)
Spiramycin
macrolide (binds 23s subunit of 50S ribosome blocking protein synthesis)
Use for pregnant mother with toxoplasma
not so toxic to fetus
miltefosine
New drug for treatment of primary amebic meningoencephalitis
only one available
