-
super saturated potassium iodide and other iodides treat what?
Sporothrix schenckii. skin sporotrichosis (gardener)
-
Disrupts mitotic spindle, binds microtubules, like colchicine. treats tinea capitis
Griseofulvin
-
Blocks ergosterol synthesis. topical & po for skin & nail infections.
Terbinafine
-
Blocks beta glucan synthase, disturbing integrity of fungal cell wall
Caspofungin (echinocardins class)
-
95% bioavail. No acid concern. Good distribution, good CNS penetration.
Look for P450 interaction. Photosensivity. (triazole 2nd generation).
Voriconazole
-
GI must be pH 4 to absorb. Liver metabolism. No kidney concern. Not so good CNS penetration. Triazole (2nd generation)
Itraconazole
-
good absorption, 97% bioavail., CNS/CSF 70%, all compart. 90% out of kidney. Trizaole (2nd generation azole)
Fluconazole
-
Inhibit enzyme – lanosterol demethylase (P450-dependent enzyme) --> blocks ergosterol synthesis
azoles
-
1st generation azoles, topical only
Imidazoles: Ketoconazole & Clotrimazole & Miconazole
-
Needs low pH (3.0) to dissolve. Less selective for fungal P450 -->
more toxic to humans. Poor CNS distribution. Blocks host steroid
synthesis.
ketoconazole
-
Skin cream, lotion. Topical for Tinea skin infection. Imidazole (1st generation)
Clotrimazole & Miconazole
-
Binds ergosterol in fungal cell membrane
Nystatin, amphotericin B, ambisome
-
Similar to Amphotericin B – more toxic. Topical only.
Nystatin
-
Protease inhibitors
Fosamprenavir, Lopinavir/Ritonavir, Atazanavir
-
Protease inhibitors are not preferred due to ...
- most are not preferred due to short serum t1/2 and All drugs in this
- class are inducers or inhibitors of this CYP450 system. Therefore, a
- high chance of drug-drug interactions
-
Integrase inhibitor. Active against virus with resistance to NRTIs, NNRTIs, and PIs
Raltegravir
-
Eliminated by glucuronidation. no induction or inhibition of P450
Integrase inhibitor, Raltgravir
-
Non-Nucleoside Reverse Transcriptase Inhibitor
Efavirenz
-
bind directly to enzyme, block RNA-dependent DNA Polymerase action
NNRTI - Efavirenz
-
t1/2 40-55 hr, inducer of CYP3A
Efavirenz
-
Nucleoside Reverse Transcriptase Inhibitors - long half life
Zidovudine, Lamivudine, Tenofovir and Emtricitabine
-
incorporated into the growing nucleic acid, cause DNA chain termination
NRTIs : Zidovudine, Lamivudine, Tenofovir and Emtricitabine
-
NRTIs toxicity
Mitochondrial toxicity, Lactic Acidosis, Hepatic Steatosis, hepatotoxicity, Multiorgan failure and Death
-
Fusion inhibitor. binds to the viral surface glycoprotein gp41 and
prevents fusion. Used w/ viruses resistant to NNRTIs and NRTIs and PIs
Enfuvirtide
-
Enfuvirtide effect on P450 system
none
-
CCR5 receptor inhibitor. Active against virus with resistance to PIs, NRTIs and NNRTIs
maraviroc
-
CCR5 receptor inhibitor. Blood conc will change depending on inducer/inhibitor of CYP3A4
maraviroc
-
DNA polymerase inhibitors for anti herpes. IV or topical
Acyclovir, Valcyclovir, Famciclovir, Ganciclovir, Cidofovir and Foscarnet
-
nucleoside analog incorporated into herpes DNA replication
Trifluridine
-
Acyclovir, Valcyclovir, Famciclovir, Ganciclovir, Cidofovir and Foscarnet toxicities
Nephrotoxicity, neurotoxicity
-
Side effect of antiherpes Trifluridine.
burning sensation and edema of eye
-
Blocks DNA polymerase of virus (hepatitis & herpes)
Famciclovir - treats Hep B
-
side effects of Famciclovir
not remarkable
-
inhibitors reverse transcriptase treating Hep B
lamivudine
-
side effects of Lamivudine
GI, headache, fatiqgue, pancreatitis, lactic acidosis. Hypersensitivity
-
Inhibits DNA, RNA synthesis, treating Hep C
ribavirin
-
Side effects of Ribavirin
hemolytic anemia, elevated uric acid, teratogenic
-
Interferon is used to treat
Hep B & C
-
Interferon toxicity
Flu like, bone marrow, neurotoxicity, liver toxicity
-
prodrug that inhibits HBV DNA polymerase
Adefovir DP
-
Adefovir DP side effects
Nephrotoxicity, bone loss, lactacidosis, hepatic steatosis
-
H+ must enter virus via M2 ionic channel to change pH and cause
uncoating and release of RNA. Drugs block ion channel, prevent release
ofRNA
amantadine & rimantadime
-
Side effects of Amantadine & Rimantadine
CNS: insomnia, poor concentration, nervous, hallucination, depression
-
Which one is more prone to resistance for flu virus? Amantadine or Rimantadine?
Amantadine. Due to farmers feeding to chickens
-
Blocks neuraminidase
Oseltamivir and Zanamivir
-
Side effects of Oseltamivir
nausea, vomiting
-
side effects of zanamivir
bronchospasm in asthmatics
-
guanosine analog. blocks dna and rna synthesis
ribavirin
-
Ribavirin is used in
flu & hepatitis
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