EXAM PREP Flashcards
What are the uses of Metronidazole
Ambebiasis, giardiasis, trichomoniasis, anaerobic bacterial infections
co-administer with Paromycin (luminal agent)
what is the MOA for Metronidazole
Nitro group serves as electron acceptor, forms toxic metabolite that disrupts DNA structure -> cell death
what are the pharmacokinetics of Metronidazole
Oral
hepatic metabolism, excreted in urine
What are the SE/Contraindications of metronidazole
N/V, abdominal pain, metallic taste, seizures, neuropathy, disulfiram effect with alcohol
contra: pregnancy, breast feeding, recent use of disulfiram
What are the uses of Trimethoprim-sulfamethoxazone (TMP-SMX)
aka Bactrim
cyclospora and isopora infections
treatment of choice for P. jirovecci pneumonia
what is the MOA for TMP-SMX
combo provides sequential and synergistic blockade of folate pathway -> inhibition of thymidine synthesis
What are the pharmacokinetics of TMP-SMX
oral or IV infusion
what are the AE/Contraindications for TMP-SMX
Rash, SJS, kernicterus, bone marrow suppression, anemia, renal impairment, hepatotoxicity
Contra: renal disease, newborns and pregnancy
What are the uses for Albendazole
broadly effective against nematodes (round worms)
What is the MOA for Albendazole
binds to microtubules in worms and larvae -> impaired glucose uptake -> glycogen depletion -> degeneration of mitochondria -> release of lysosomes, depletion of ATP -> worm death
What are the pharmacokinetics of Albendazole
oral admin
What are the AE/contraindications of Albendazole
HA, elevated LFTs, liver impairment, bone marrow suppression, seizures, alopecia
Contra: pregnancy
What are the uses of Pyrantel pamoate
alternative to albendazole for infestations with hookworms or pinworms
NOT preferred, newer agents available
what is the MOA for pyrantel pamoate
causes release of Ach and inhibits cholinesterase -> depolarizing neuromuscular blocker -> spastic paralysis and release of helminths
What are the pharmacokinetics of pyrantel pamoate
oral admin
what are the AE/Contraindications of pyrantel pamoate
GI upset, dizziness, drowsiness, HA, insomnia
what are the uses of Praziquantel
flukes and cestodes (tapeworms) and is the DOC for tapeworms and schistosomiasis and other fluke infestations
what is the MOA of Praziquantel
increase cell permeability to Ca2+ in schistosomes -> strong contractions and paralysis of worms -> detachment, death
What are the pharmacokinetics of Praziquantel
Oral
extensively metabolism by CYP3A4
What are the AE/contraindications for Praziquantel
HA, abdominal discomfort, drowsiness, dizziness
patients with cerebral cystocercosis (brain worms) experience CNS AE
avoid co-admin with CYP inducers
what are the uses of Ivermectin
Onchocerciasis (major cause of blindness worldwide) and intestinal stronglyoidasis
head lice
What is the MOA for Ivermectin
binds and activates glutamate-gated Cl-channels in invertebrate nerve/muscle cells -> hyperpolarization -> death
What are the pharmacokinetics of Ivermectin
Oral or topical
does NOT cross BBB
What are the AE/Contraindications for Ivermectin
pruritus, rash, fever, lymph node tenderness, bone and joint pain, neurotoxicity
contra: pregnancy and meningitis
What are the Antiparacitis/anti-helmintics
Metronidazole
Bactrim
Albendazole
Pyrantel pamoate
Praziquantel
Ivermectin
What are the uses for Amphotericin B
widest spectrum of activity of all antifungals
treatment of severe invasive fungal infections
resistance rare, but some resistance is d/t decreased ergosterol content in cell membrane
what is the MOA for Amphotericin B
lipophilic rod-like molecule binds to ergosterol -> forms pores in membrane -> K+ leaks out of cell causing death
What are the pharmacokinetics of Amphotericin B
IV infusion
6-8 weeks of treatment, but can be as long as 3-4mo
onset of action is rapid
low TRUTH IS
little CSF penetration
what needs to be monitored with someone on Amphotericin B
K+ and Mg2+
What are the AE/Contraindications for amphotericin B
infusion reactions, nephrotoxicity, bone marrow suppression, N/V, anemia, phlebitis
contra: renal insufficiency, combo with other nephrotoxic agents
How can nephrotoxicity be reduced with Amphotericin B
Saline loading and increased infusion time
What are the uses of Nystatin
candida infections of skin, mouth, esophagus, intestines, vagina
too toxic for systemic use
What is the MOA of Nystatin
lipophilic rod-like molecule binds to ergosterol -> forms pores in membrane -> K+ leaks out of cell causing death
What are the pharmacokinetics of Nystatin
Powder, Ointment, Cream or Suspension administration
What are the AE/Contraindications of Nystain
topical: local irritation
What are the uses for Flucytosine
systemic mycosis and meningitis caused by candida and cryptococcus
combo with itraconazole for treatment of chromoblastomysocis
combo with ampB - NOT used alone due to resistance
why does Flucytosine have high resistance levels
caused by fungi decreased levels of targeted enzymes
What are the pharmacokinetics of Flucytosine
oral
can cross BBB
dose adjust in renal impaired
what are the AE/Contraindications of Flucytosine
reversible neutropenia, thrombocytopenia and hepatic dysfunction
dose-related bone marrow suppression
More common: N/V/D
What are the uses of Ketoconazole
systemic and superficial mycoses
candida, histoplasma, blastomyces, coccidiioides NOT aspergillius
DO NOT use in combo with ampB
what causes the resistance to Ketoconazole
mutations in C-14 alpha-demethlyase gene -> decreased binding of drug
stains can pump drug out of cells
what is the MOA for Ketoconazole
inhibits C-14alpha-demethylase -> blocks demethylation of lanosterol to ergosterol -> disrupts membrane synthesis
What are the pharmacokinetics of Ketoconazole
oral or topical
requires gastric acid for dissolution and absorption
does NOT penetrate CSF
Hepatic metabolism
What are the AE/contraindications of Ketoconazole
N/V, hepatic necrosis
endocrine effects: gynecomastia, decreased libido, menstrual irregularities
may increase toxicities of drugs metabolized by CPY450
contra: pregnancy
What are the uses of clotrimazole
superficial mycoses, too toxic for systemic use
ringworm, candida
what is the MOA for clotrimazole
inhibits C-14alpha-demethylase -> blocks demethylation of lanosterol to ergosterol -> disrupts membrane synthesis
What are the pharmacokinetics of clotrimazole
topical
what are the AE/contraindications of Clortimazole
contact dermatitis, vulvar irritation, edema
What are the uses of Fluconazole
systemic and superficial mycoses
candida, cryptococcus, coccidioides
NO activity against aspergillus
what is the MOA for fluconazole
inhibits C-14alpha-methylase -> blocks demethylation of lanosterol to ergosterol -> disrupts membrane synthesis
what are the pharmacokinetics of fluconazole
oral or IV admin, not dependent on gastric acid
good CSF penetration
dose adjust in renal impairment
what are the AE/contraindications for Fluconazole
Nausea, HA, rashes, alopecia, SJS
Hepatitis rare
contra: pregnancy
what are the uses of Itraconazole
systemic and superficial ycoses
DOC for blastomycosis, histoplasmosis, and sporotrichosis
alternative to ampB for aspergillosis, candidiasis, and coccidioidomycosis
what is the MOA for Itraconazole
inhibit C-14alpha-methylase -> blocks C-14alpha-demethylation of ianosterol to ergosterol -> disrupts membrane synthesis
what are the pharmacokinetics of Itraconazole
oral admin, requires gastric acid for absoprtion
hepatic metabolism
no dose-adjustment in renal impairment
poor CSF penetration
what are the pharmacokinetics of Itraconazole
oral admin, requires gastric acid for absorption
hepatic metabolism
no dose-adjustment in renal impairment
poor CSF penetration
What are the AE/contraindications for Itraconazole
GI upset, rash, HA, alopecia, abd pain, edema, HTn, hypokalemia, hepatitis rare
serious: Cardiac suppression and liver injury
inhibits CYP3A4-> increase levels of many other drugs
contra: pregnancy, CHF
What are the uses of Capsofungin
systemic mycoses, second line to vericonazole
aspergillus, candida
better tolerated than ampB
NOT active against zygomycetes and crytococcus neoformans
what is the MOA of Capsofungin
inhibits synthesis of beta-1,3-d-glucan and disrupts fungal cell wall
what are the pharmacokinetics of Capsofungin
IV
half life of 9-11 hours
CNS penetration is poor
What are the AE/contraindications of Capsofungin
well tolerated
histamine reaction with infusion
drug interactions with cyclosporine, tacrolimus, rifampin
how do you avoid histamine reaction with capsofungin
pretreat with diphenhydramine (benadryl)
What are the uses of Griseofulvin
superficial mycoses
dermatophytic infections of the skin, hair and nails
accumulates in keratin-containing tissue
what is the MOA for Griseofulvin
binds to components of microtubules -> inhibits mitosis
what are the pharmacokinetics of Griseofulvin
oral
treatment may be required for 6-12 months
what are the AE/contraindications with Griseofulvin
avoid alcohol
induces CYP enzymes
contra: pregnancy and patients with porphyria
what are the uses of Terbinafine
superficial mycoses
highly active against dermatophytes and less active against candida species
DOC for onychomycosis
What is the MOA of Terbinafine
inhibits squalene epoxidase with resultant inhibition of ergosterol synthesis -> inhibits cell wall synthesis
what are the pharmacokinetics of Terbinafine
oral and topical
6-12 weeks of treatment
What needs to be monitored with Terbinafine treatment
LFTs
what are the AE/Contraindications of terbinafine
diarrhea, dyspepsia, nausea, HA, rash, hepatotoxicity
Contra: lactating women
What are the antifungal medications
Amphotericin B
Nystatin
Flucytosine
Ketoconazole
Clotrimazole
Fluconazole
Intraconazole
Capsofungin
Griseofulvin
terbinafine
What are the uses of Oseltamivir
aka Tamiflu
influenza A and B, decrease course of dz and can be used for prophylaxis
treat patients with higher risk; children <3, adults >65yo, pregnant, pts with comorbidities, morbidly obese, nursing homes
What is the MOA for Oseltamivir
Inhibits neuroamidase, enzyme essential for cleaving virus from its host cell
What are the pharmacokinetics of Oseltamivir
oral - prodrug that is hydrolyzed by the liver to active form
must be admin within 24 -48 hours of symptom onset
dose-adjust in renal impairment
what are the AE/contraindications of Oseltamivir
N/V
take with food to minimize GI effects
what are the uses of amantadine
currently ineffective for viral infections due to rate of resistance
used in PD
what is the MOA for amantadine
inhibits M2 protein
what are the anti-viral flu medications
Oseltamivir (tamiflu)
amantadine (high rate resistance)
What are the uses of Acyclovir
HSV-1, HSV-2, VZV
NO activity against CMV
resistance is building especially in immunocompromised patients
what causes the resistance to Acyclovir
mutation or loss of viral thymidine kinase
What is the MOA of Acyclovir
guanosine analogue that inhibits viral DNA polymerase by chain termination - > inhibits transcription
activated by viral thymidine kinase in infected cells
what are the pharmacokinetics of acyclovir
oral, topical, or IV admin
oral bioavailability low, requires frequent dosing
dose adjust in renal impairment
what are the AE/contraindications of Acyclovir
oral: N/V/D, Ha, vertigo
Topical: local burning sensation
IV: renal failure - can crystalize in renal tubules, neurotoxicity
what are the uses of Valacyclovir
HSV-1, HSV-2, VZV
NO activity against CMV
5x more expensive than Acyclovir
what is the MOA of Valacyclovir
guanosine analogue that inhibits viral DNA polymerase by chan termination -> inhibits transcription
activated by viral thymidine kinase in infected cells
what are the pharmacokinetics of Valacyclovir
prodrug, hydrolyzed to acyclovir in intestines and liver
oral admin
higher bioavailability
3x/day admin
what are the AE/contraindications of Valacyclovir
N/V/D, HA, vertigo
HA more common than acyclovir
what are the uses of Famciclovir
HSV-1, HSV-2 and VZV
No activity against CMV
what is the MOA for Famciclovir
selectively inhibits viral DNA plymerase by chain termination -> inhibits transcription
activated by viral thymidine kinase in infected cells
what are the pharmacokinetics of Famciclovir
prodrug of penciclovir, undergoes intracellular conversion to penciclovir triphosphate
what are the AE/contraindications of Famciclovir
N/V, HA
what are the uses of Foscarnet
CMV retinitis and acyclovir-resistant mucocutatneous HSV and VVZV infection in immunocompromised
what is the MOA of Foscarnet
reversibly blocks pyrophosphate binding site of viral DNA polymerase -> inhibits transcription
what are the pharmacokinetics of Foscarnet
IV admin only
active as administered
dose adjust in renal impairment
what are the AE/contraindications of Foscarnet
Fever, N/V/D, anemia, HA, fatigue, tremor, irritability, elevated liver enzymes
nephrotoxicity, electrolyte/mineral imbalances, seizures, blood disorders, QT prolongation, dysrhythmias
What are the medications against herpes viruses
acyclovir
valcyclovir
famciclovir
foscarnet
what are the uses of interferons
treatment of HBC and HCV, usually as part of a combination
rarely first line treatment
many other potential uses
what is the MOA for interferons
thought to induce gene transcription of host cell enzymes that inhibit viral RNA
increase phagocytic activity of macrophages
increase cytotoxicity of lymphocytes for target cells
what are the pharmacokinetics of interferons
IV or SubQ
never oral
dose adjust in severe renal disease
what are the AE/contraindications of Interferons
flu-like sx after admin
mood disorders, depression, somnolence, confusion, profound fatigue, weight loss, seizures, myelosuppression, rash, cough, myalgia, alopecia, tinnitus, reversible hearing loss, retinopathy, pneumonitis, cardiotoxicity, autoimmune reaction
what are the uses of Lamivudine
HBV
can be used in HIV-HBV co-infection
growing resistance
what is the MOA of Lamivudine
cytosine analog that inhibits HBV DNA polymerase and works against HIV reverse transcriptase -> inhibits viral DNA synthesis
What are the pharmacokinetics of Lamivudine
oral admin, good absorption
dose adjust in renal impairment
what are the AE/contraindications of Lamivudine
HA, dizziness, pancreatitis
rare: lactic acidosis and hepatomegaly
what are the uses of Entecavir
HBV
weakly active against HIV
typically second-line, not preferred for lamivudine-resistance strains
what is the MOA of Entecavir
phosphorylated to guanosine triphosphase; competes as substrate for HBV DNA polymerase thereby inhibiting the enzyme -> inhibits viral DNA synthesis
what are the pharmacokinetics of Entecavir
oral
dose adjust in renal impairment
what are the AE/contraindications of entecavir
may cause increase ALT levels, mild GI upset, mild hyperglycemia, HA
Rare: lactic acidosis and hepatomegaly
what are the uses of Tenofovir
HBV
typically second-line but PREFERRED for lamivudine-resistance strains
what is the MOA of Tenofovir
Binds HBV DNA polymerase and works against HIV reverse transcriptase -> inhibits replication of HBV
what are the pharmacokinetics of Tenofovir
2 formulations available: tenofovir disoproxil fumarate and tenofovir alafenamide
dose adjust in renal impairment
what are the AE/contraindications of tenofovir
GI effects, rash, hypercholesterolemia, decreased bone mineral density
rare: lactic acidosis and hepatomegaly
what are the uses of Ribavirin
HCV, usually in combo with interferons
NOT preferred treatemnt
severe pediatric RSV
what is the MOA of Ribavirin
inhibits guanine nucleotide synthesis -> inhibits viral transcription and RNA replication
what are the pharmacokinetics of Ribavirin
oral
aerosolized for children
what are the AE/contraindications of Ribavirin
hemolytic anemia
contra: pregnancy
what are the uses of Ledipasvir
direct-acting anativiral
HCV
newer and more expensive
what is the MOA of Ledipasvir
inhibits NS5A protein which plays a role in both viral replication and the assembly of HCV
what are the pharmacokinetics of Ledipasvir
oral
increase gastric pH levels 9more alkalotic) may decrease absorption)
what are the AE/contraindications of Ledipasvir
generally well tolerated
be careful with co-admin with PPIs
what are the uses of Sofosbuvir
direct-acting antiviral
HCV
newer and more expensive
commonly given in combo tablet with Ledipasvir
what is the MOA of Sofosbuvir
inhibits HS5B protein which plays a role both viral replication and assembly of HCV
what are the pharmacokinetics of Sofosbuvir
oral
activated by metabolism
what are the AE/contraindications of Sofosbuvir
HA, fatigue, insomnia
avoid with rifampin , rifapentine, carbamazepine, phenytoin, phenobarbital, oxcarbazepine, tipranavir/ritonavir, amiodarone
What are the antivirals against hepatoviruses
interferons
lamivudine
entecavir
tenofovir
ribavirin
ledipasvir
sofosbuvir
What are nemotodes
round worms
what are cestodes
flat forms
what are trematodes
flukes
what are rhizopods
amoeba
