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86 Cards in this Set
- Front
- Back
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Aspergillus |
Allergic rxn to inhaled spores = asthma Grows in lung cavitations Fluconazole ineffective! Aflatoxin can cause liver cancer |
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Polyenes (Amphotericin B, Nystatin) |
bind ergosterol, increase cell permeability Amphotericin B, Nystatin |
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Amphotericin B |
IV only! "Amphoterrible" - lots of side effects broad spectrum - systemic mycoses, leishmeniasis, protozoa resistance - rare Liposomal formula reduces toxicity but expensive! Renally Cleared! TOXIC! Pokes holes in our cells too! - anaphylaxis, hypotension, convulsion need adequate hydration - monitor serum electrolytes and creatinine (pre-treat weekly) |
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Nystatin |
topical only! usually for candida |
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Flucytosine |
antimetabolite fungistat converted to fluorouracil which competes w/uracil & interferes w/fungal RNA & protein synthesis resistance - rapid as monotherapy cytotoxic, bone marrow suppressant, anemia, neutropenia, thrombocytopenia |
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Terbinafine |
squalene epoxidase inhibitor oral (systemic) or cream for dermatophytes & onychomycosis (drug of choice) accumulates in nails, hepatotoxic half life = 300hrs |
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Azoles |
block conversion of lanosterol to ergosterol inhibit human CYP450 broad spectrum fungistatics hepatotoxic, decreased testosterone (Ketoconazole) |
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Fluconazole (systemic Azole) |
IV, PO (oral - treatment & prevention of vaginal candidiasis) may inhibit CYP450 & risk of hepatotoxicity though renally cleared Spectrum: candida, coccidioides, histoplasmosa, cryptococcus NOT: Aspergillus, Fusariu, Zygomycetes! AE: reversible hair loss, headache |
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Itraconazole (systemic Azole) |
PO AE: pedal edema, hair loss, hypokalemia, hypertension, black box- may exacerbate CHF (negatively affects contractivity of heart) Spectrum: Aspergillus, Blastomyces, Candida, Cocciodes, Cryptococcus, Histoplasma, Paracoccidiodes |
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Posaconazole (systemic Azole) |
PO Spectrum: Zygomycetes, Aspergillus, azole-resistant Candida, Coccidiodes AE: QTc (systole) prolongation, angioedema |
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Voriconazole (systemic Azole) |
IV Good CNS penetration Spectrum: Aspergillus, Candida (including krusei), Fusarium NOT: Zygomycetes AE: visual disturbance |
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Ketoconazole (systemic Azole) |
shampoo, tabs, creams Use in prostate cancer to reduce testosterone; in hyperadrenal states (Cushings) to reduce adrenal steroids; corticosteroid suppressor Spectrum: tinea corporis, cruris, pedis, versicolor, cutaneous candidiasis, seborrheic dermatitis and dandruff AE: gynecomastia!!! Drug Rxn: Amphotericin |
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Topical Azoles |
Butaconazole Clotrimazole Miconazole - inhibits fatty acid synthesis, fungal oxidases and peroxidases Terconazole - creams, sprays, vaginal creams, suppositories |
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Echinocandins ("-fungin") |
IV only; Interfere w/ synthesis of cell wall by noncompetitive inhibition of beta D-glycan synthase Anidulafungin Caspofungin Micofungin Spectrum: Candida (incl. Azole resistant), Aspergillus AE: hepatic effects (rare), histamine rxns, drug fever, headache hemolysis |
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Griseofulvin (fungistatic) |
cross allergenicity w/beta lactams possible MOA: binds to tubulin, inhibiting function of mitotic spindle Spectrum: cutaneous (Trichophyton, Micosporum, Epidermophyton) Ineffective vs. yeast & dimorphic fungi CYP inducer AE: adverse rxn with ethanol (Disulfram-like rxn); accumulates in skin & nails |
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Miscellaneous Antifungals |
ciclopirox - nail polish (not preferred b/c takes so long to absorb)
undecyclenic acid Iodine - topically; orally for sporotrichosis Gentian Violet |
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DNA Virus |
Poxvirus (smallpox) Herpesvirus (chickenpox, shingles, oral and genital herpes) Adenovirus (conjunctivitis, sore throat) Hepadenavirus (Hepatitis B) Papilloma virus (warts) |
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Anti-Herpesvirus Agents |
MOA: phosphorylated intracellularly by viral kinase & by host cell to become inhibitors of viral DNA sythesis cellular uptake & initial phosphorylation facilitated by HSV thymidine kinase |
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Acyclovir |
oral - genital herpes treatment & suppression; adult varicella-zoster topical - less effective in oral herpes; innefective in genital IV - herpes simplex encephalitis, neonatal herpes simplex virus, serious herpes simplex or varicella-zoster AE: N/D/H; IV: reversible renal toxicity or neuro effects use in immunocompromised! |
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Docosanol |
topical fusion inhibitor - prevents entry into cells and subsequent replication apply w/in 12 hrs of prodrome, 5x daily, healing shortened by 18hrs |
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Penciclovir |
topical fusion inhibitor apply w/in 1 hr of prodrome, every 2hrs for 4 days, healing shortened 17hrs |
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Ganciclovir & Valganciclovir |
Inhibits all herpesviruses but especially active against cytomegalovirus MOA: Inhibits viral DNA synthesis - monophosphorylated by viral thymidine kinas in herpes simplex monophosphorylated by viral phospotransferase in cytomegalovirus AE: myelosupression, neutropenia, GI, CNS, teratogenicity |
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Cidofovir |
MOA: completely inhibits DNA synthesis & incorporating into viral DNA phosphorylation is independent of viral enzyme - activity is maintained vs. thymidine kinase deficient or altered strains of cytomegalovirus or herpes simplex AE: dose dependent proximal tubular nephrotoxicity; administer w/probencid to decrease nephrotoxicity! |
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Foscarnet |
MOA: inhibits herpesvirus DNA polymerase, RNA polymerase and HIV reverse transcriptase without needing phosphorylation! Broad spectrum: cytomegalovirus, acyclovir-resistant HSV and acyclovir-resistant varicella-zoster AE: nephrotoxicity (saline preloading helps), hypocalcemia, arrythmia |
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Ostelamivir & Zanamivir |
MOA: neuraminidase inhibitors - competitively and reversibly inhibit viral neuraminidase resulting in clumping of newly released virions Spectrum: influenza A&B early admin is crucial - replication peaks @ 24-72hrs of onset Oseltamivir (oral) resistance is increasing Zanamivir (nasal) contraindicated in asthma, COPD, kids <7 |
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Amantadine and Rimantadine |
no longer used due to resistance Amantadine - Parkinsonism use |
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Palivizumab |
humanized monoclonal antibody Spectrum: RSV prevention in high risk infants & children AE: upper resp infection, fever, rash |
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Hepatitis A |
self limiting and acute infection w/no potential for chronic vaccine available |
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Hepatitis B |
vaccine available chronic infection (unimmunized) |
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Hepatitis C |
no vaccine 75-85% develop chronic infection |
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Adefovir |
Spectrum: chronic Hepatitis B MOA: inhibits hepatitis B DNA polymerase & reverse transcriptase; causes chain termination after incorporation AE: does-related nephrotoxicity, headache, diarrhea, acute exacerbation of hepatitis B upon discontinuation |
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Entecavir |
Guanosine nucleoside analog MOA: competitively inhibits all 3 functions of Hepatitis B DNA polymerase AE: headache, fatigue, dizziness, hepatomegaly, acute exacerbation of Hepatitis B if discontinued monitor hepatic function! |
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Telbivudine |
Thymidine nucleoside analog Spectrum: Hepatitis B MOA: phosphorylated by cellular kinase, inhibits Hepatitis B DNA polymerase (reverse transcriptase); incorporating into viral DNA causes chain termination AE: N/D, myopathy, fatigue, acute exacerbation of Hep B if discontinued |
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Drugs that cover Hep B & HIV |
Lamivudine Tenofovir |
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Interferon alfa-2b & 2a |
2b - indicated in Hep B & C 2a - indicated in Hep C MOA: Increase protein kinase inhibiting protein synthesis AE: flu-like symptoms, depression, myelosuppression pegylated has replaced it mostly |
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Pegylated interferon alfa 2a and 2b |
2a - Hepatitis B & C 2b - Hepatitis C MOA: increases protein kinase inhibiting protein synthesis slower clearance, longer half life, steadier concentrations = less frequent dosing enhanced by adding Ribavirin! |
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Interferon alphacon-1 |
indicated in Hep C AE: flu-like symptoms, fever, fatigue, myalgia, rigors, arthralgia, neutropenia indicated for concurrent use with Ribavirin for patients who failed with pegylated interferon-Ribavirin |
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Ribavirin |
Use in combo w/interferon in Hep C guanosine nucleoside analog MOA: phosphorylated by host enzymes, inhibits capping of viral mRNA and RNA dependent polymerase AE: Toxic! Dose dependent hemolytic anemia, fatigue, hyperuricemia, neutropenia (patients exposed to drug shouldn't conceive for @ least 6 months after!) |
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Sofosbuvir |
MOA: inhibits RNA polymerase and is a chain terminator Use in type 1-4 Hep C in combo w/Ribavirin or peginterferon alfa and Ribavirin AE: fatigue, weakness, nausea, decreased hgb, anemia, neutropenia, flu-like symptoms |
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Protease NS3/4A Inhibitors |
boceprevir, simeprevir, telaprevir Spectrum: HCV genotype 1 in combo w/peginterferon and Ribavirin MOA: inhibit HCV replication resistance can occur w/in 4 days with monotherapy Inhibitors and substrates of CYP3A4 (adminstration w/ strong CYP3A4 inducers (rifampin) contraindicated due to decrease in anti-HCV agent) |
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Ledipasvir |
given in combo w/ sofosbuvir inhibits HCV protein necessary for viral replication indicated in Hep C type 1 $1,125/pill |
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Ritonavir |
MOA: protease inhibitor used in HIV off label use is pharmacokinetic booster Strong CYP3A4 inhibitor (increase level of drugs inactivated by CYP3A4) |
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Under Investigation |
2nd generation NS3/NS4A protease inhibitors nucleoside/nucleotide NS5B polymerase inhibitors non-nucleoside NS5B polymerase inhibitors Goal: potent & well tolerated regimens that don't require Ribavirin or interferon |
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HIV Treatment |
check guidelines regularly HAART now ART (antiretroviral therapy)- consists of at least 3 drugs to reduce likelihood of resistance non-compliance causes resistance Drug Combos: avoid combo of same base analogs, overlapping toxicity, drug interactions, consider ease of adherence & comorbidities |
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Drugs for HIV |
Nucleoside/nucleotide reverse transcriptase inhibitors (NRTI) Non-nucleoside reverse transcriptase inhibitors (NNRTI) Protease inhibitors Entry Inhibitors Integrase Inhibitors |
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Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTI) |
Didanosine Abacavir Zidovudine - used IV during labor & deliver to prevent transmission to fetus & given orally for 6wks to newborn! Lamivudine Tenofovir - only nucleotide |
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Nucleoside/Nucleotide Reverse Transcriptace Inhibitors |
MOA: competitive inhibition of HIV-1 reverse transcriptase; incorporation into the growing viral DNA chain which causes premature chain termination due to inhibition of binding with incoming nucleotide require phosphorylation from host kinases! less active as single agents |
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NRTI Adverse Effects |
Most: mitochondrial toxicity, lactic acidoses, hepatic steatosis Zidovudine: insulin resistance, dyslipidemia, bone marrow suppression Abacavir - hypersensitivity rxns Didanosine - pancreatitis & peripheral neuropathy |
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Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) |
Nevirapine Efavirenz Etravirine Delavirdine Rilpivirine |
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Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
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MOA: Bind directly to HIV-1 reverse transcriptase; do not compete w/nucleoside triphosphates; do not require phosphorylation or host enzyme! All substrates for CYP3A4! inducer: nevirapine inhibitor: delavirdine mixed: efavirenz, etravirine |
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NNRTI Adverse Effects
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relatively non-toxic (humans have no reverse transcriptase) GI intolerance, skin rash Efavirenz - CNS effects (dizziness, drowsiness, insomnia, nightmares, headache), teratogenic aviod in 1st trimester or in women likely to conceive! Nevirapine - Stevens-Johnson Syndrome |
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Protease Inhibitors |
Fosamprenavir Indinavir Lopinavir Ritonavir |
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Protease Inhibitors |
MOA: Completely inhibit viral aspartyl protease - prevents metamorphosis of HIV into mature form All substrates of CYP3A4 Nalfinavir & Ritonavir ahve alternative pathways Ritonavir used as an enhancer for other drugs (CYP3A4 inhibitor) |
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Protease Inhibitors Adverse Effects |
Hyperglycemia, hyperlipidemia, lipodystrophy (buffalo hump), hepatotoxicity, GI intolerance, increased bleeding risk for hemophiliacs Indinavir - nephrolithiasis (hydrate!) |
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Entry Inhibitors |
Fusion inhibitor: Enfuvirtide Binds gp41, preventing conformation change required for fusion of viral & cellular membranes Binding inhibitor: Maraviroc Binds to host cell CCR5 receptor to block binding of viral gp120 |
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Enfuvirtide |
Fusion inhibitor Spectrum: HIV expensive (>$3000/month); subcutaneous injection 2/day AE: site rxn 98% (erythema, nodules, cysts); lymphadenopathy, pneumonia, eosiophilia |
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Maraviroc |
Binding inhibitor Tropism testing must be performed to ensure virus uses CCR5 receptor Substrate of CYP3A4 AE: upper resp infection, hepatotoxicity, postural hypotension, mycardial ischemia & MI have been observed |
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Raltegravir |
Integrase strand transfer inhibitor = binds integrase, enzyme essential to replication of HIV-1&2 (inhibits strand transfer and integration of reverse-transcribed HIV DNA into chromosome) AE: increase in creatine Kinase, insomnia, headache, diarrhea, nausea |
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Cobicistat |
CYP3A4 inhibitor not active against HIV! used to "boost" levels of other drugs! |
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General ART |
2 NRTI + protease inhibitor or NNRTI factors influencing choice: resistance pattern, co-morbidity, pregnancy, drug interactions, compliance Enzyme inducers will eliminate contraceptives!! |
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Post Exposure Prophylaxis |
KNOW FACILITY POLICY! Must begin w/in 72hrs of exposure Use PPE! |
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Pre Exposure Prophylaxis (PrEP) |
prevention for persons at high risk for HIV lowered risk 92% must see provider Q3 months for HIV/STD tests tenofovir or emtricitabine or both recommended dosed daily |
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Nematodes (Roundworms) |
Ascaris lumbricoides - most common worldwide! Enterobius vermicularis Necator americanus Loa loa Wuchereria bancrofti |
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Intestinal Nematodes |
Non-invasive: Whipworms (Trichuris trichuria): diarrhea, abdominal pain, rectal prolapse (3rd most common roundworm) Pinworms (Enterobius vermicularis): Perianal itching (scotch tape test), children under 18 & institutionalized people (most common worm in US) |
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Intestinal Nematodes |
Invasive: Ascaris lumbricoides: Warm & humid climates; most common human worm infection fecal-oral transmission (abdominal pain, RUQ pain, vomiting, pancreatitis, abdominal obstruction |
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Intestinal Invasive Nematodes |
Necator americanus and Anclostoma duodenale (hookworms) Diarrhea, pulmonary infiltrate, weight loss, itchy toes, Iron deficiency; diagnose by eggs in feces Strogyloides stercoralis (threadworms): penetrate skin, transport to lungs, swallowed, reach SI; vomiting, bloating, diarrhea, weight loss, anemia, pulmonary symptoms; diagnosed by larvae in feces Trichinella spiralis ingestion of cysts in undercooked meat: abdominal pain, fever, muscle pain; diagnosis via muscle biopsy |
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Blood & Tissue Nematodes |
filariae (adults, threadlike); pre-larval form = microfilariae microfilariae circulate thru blood & lymph - mosquitoes transmit Onchocerca volvulus - river blindness; Africa, Central/South America Filariases (Wuchereria bancrofti & Brugia malayi; Elephantitis; Pacific Islands, Africa, Malay Penninsula, Southeast Asia); Loa loa - African eye worm Dracunculus medinesis - Guinea worm; drinking water |
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Benzimidazoles |
Albendazole, Mebendazole, Thiabendazole MOA: inhibit microtubule synthesis by binding to beta tubulin; reduce glucose uptake Broad spectrum! Use smaller spectrum if possible. AE: low incidence of side effects; increase liver enzymes, pancytopenia Mebendazole = <10% absorbed orally (not good for tissue infections) |
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Albendazole |
oral absorption increased w/ fatty meal give on empty stomach for intestinal parasites and with fatty meal for tissue parasites! monitor blood counts & liver function! |
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Diethylcarbamazine |
MOA: immobilizes microfilaria & alters surface structure Renally cleared Spectrum: filariases (organelle damage in W. bancrofti) AE: limited & depend on number of microfilaria in blood; don't administer to patients w/onchocerciasis as it worsens eye disease! Can only be obtained from CDC! |
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Doxycycline |
W. bancrofti activity onchocerciasis activity MOA: kills Wolbachia, an intracellular symiont of filarial parasites |
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Ivermectin |
MOA: induces tonic paralysis of musculature; activates glutamate-gated chloride channels; intensifies GABA mediated signals doesn't cross BBB; rapidly absorbed & wide tissue distribution broad spectrum vs. roundworms: strogyloidiasis, onchocerciasis, cutaneous larva migrans, lymphatic filariasis; also used in ectoparasites AE: well tolerated but Mazzotti-like rxn in filarial infection! |
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Mazotti-Like Reaction |
intensity relates to microfilarial burden mild itching, swollen, tender lymph nodes relieved by aspirin & antihistimines; rarely: high fever, tachycardia, hypotension, headache, myalgia, diarrhea, edema Ivermectin - milder side effects than diethylcarbamazine |
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Pyrantel Pamoate |
Poorly absorbed (don't see systemic side effects!) OTC MOA: induces persistent activation of nicotinic acetylcholine receptors & spastic paralysis Spectrum: Pinworms, ascaris, hookworms (heavy infections may require 3-day course) AE: use caution w/liver dysfunction |
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Cestodes (Tapeworms) |
lack digestive tract Diphyllobothrium latum (fish tapeworm); freshwater fish, B12 deficiency in humans Echinococcus granulosus (dog tapeworm); cysts in lungs & liver, anaphylaxis can occur, surgical excision required Taenia solium (pork tapeworm); main cause of human systercosis, central/south america larvae in brain = neurocystercosis (causes seizures) |
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Trematodes (Flukes) |
Clonorchis sinensis (liver fluke; snail, eating raw fish); primary site is biliary tract Schistosoma (blood fluke; tropical freshwater (snail)) Paragonimiasis (lung fluke; snail, eating raw crustaceans); diarrhea, abdominal pain, fever, cough, urticaria |
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Praziquantel |
MOA: Increases permeability of cell membranes to calcium; causes increased muscular activity, contraction, spastic paralysis; causes tegumental damage at high concentrations Spectrum: Schistosomiasis and Chlonorcis sinensis (liver) AE: dose related & transient N/D, headache, dizziness, drowsiness; increased eosinophilia based on number of parasites; contraindicated in ocular cysticercoisis: host response can damage eye |
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Treatment of Trematodes & Cestodes |
Praziquantal for cystercosis, taeniasis, dyphllobothriasis and other tapeworms Niclosamide (not available in US) - salicylamide derivative that inhibits custodial ox-phos Albendazole - cysticercosis and Echinoccocosis (broad spectrum and anti-parasitic) |
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Ectoparasites |
Pediculus humanis capitis (head lice) Pediculus humanis corporis (body lice) Pthrisu pubis (pubic lice) scaroptes scabiei (scabies) |
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Permethrin |
pediculocide & scabicide MOA: interferes w/ sodium transport proteins causing neurotoxicity & paralysis Resistance due to mutations reported in bed bugs (switch to ivermectin or malathion) |
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Lindane |
pediculocide & scabicide MOA: induces neuronal hyperstimulation & eventual paralysis commercial insecticide & topical medication Limit use! Increased potential for neurotoxicity in children & adults <110lbs & patients w/skin disorders |
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Crotamiton |
scabicide w/ unknown mechanism |
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Malathion |
MOA: binds acetylcholinesterase flammable & not for kids <6yrs old |
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Ivermectin |
oral or topical - effective in controlling scabies & lice! |
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Spinosad |
derived from soil bacteria kills live lice & eggs (pretreatment not needed) |
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Treatment for Lice |
use pediculicide (kills adult lice) comb with nit comb (eggs) every 2-3 days, continuing to check for 2-3 wks until all gone machine wash clothing & other items worn 2 days prior to onset, using hot water; can seal in plastic bag & store for 2 weeks soak combs & brushes in hot water & vacuum the floor & furniture |
