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90 Cards in this Set
- Front
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mechanism of amphotericin B
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-binds to the ergosterol component of fungal cell membranes and alters permeability to allow leakage of ions and other intracellular components
-greater selectivity for fungal membranes which contain ergosterol instead of cholesterol as in mammalian cells |
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broadest-spectrum antifungal and is the drug of choice for major systemic fungal infections, especially in immunocompromised patients
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amphotericin B
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ADRs of amphotericin B
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-infusion reactions: fever, chills, headache, nausea; usually occur 1-3 hr after starting infusion and severity lessens with subsequent dosing; may be managed by pretreatment with NSAIDs, antihistamines and steroids
-nephrotoxicity (80%) ((use lipid formulations to prevent nephrotoxicity)) |
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__ is a synthetic pyrimidine antimetabolite used adjunctively in combination with amphotericin B for treatment of systemic mycoses and meningitis
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Flucytosine (5FC)
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Flucytosine (5FC) is a synthetic pyrimidine antimetabolite used adjunctively in combination with __ for treatment of __ and __
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amphotericin B
systemic mycoses and meningitis |
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how do you take Flucytosine (5FC)?
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it is a well absorbed PO..penetrates CNS
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5FC is transported into fungal cells by a __(not found in mammalian cells) and is then converted to fluorouracil; after several steps the metabolite 5-FdUMP is formed which inhibits thymidylate synthetase, stopping DNA synthesis
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permease
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mechanism of action of azoles
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inhibition of the P450 isoenzyme that converts lanosterol to ergosterol; inhibition of ergosterol production results in deficient fungal membranes with increased permeability, leakage of cellular contents, and inhibition of fungal growth
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what impairs absorption of ketoconazole? what enhances it?
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food, antacids, H2 antagonists, PPIs
acidic cola drinks |
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what are the ADRs of ketoconazole?
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-endocrine: gynecomastia, impotence
-black box warning for hepatotoxicity: rare, serious hepatic dysfunction |
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DIs of ketoconazole
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-Do not take with antacids since gastric acidity is required for dissolution and absorption. If antacids, anticholinergics, H2 blockers, or PPIs are needed, give at least 2 hr after ketoconazole.
-inhibits P450 system |
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antagonizes action of amphotericin B, concurrent use is contraindicated; considered a class effect of azoles
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azoles
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fluconazole: po absorption __ on gastric acidity
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not dependent (like it is in ketoconazole)
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what is fluconazole (diflucan) the DOC for?
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- cryptococcal meningitis (excellent penetration into CSF)
- coccidioidomycosis |
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Itraconazole..is this used orally or topically? does it penetrate the CSF?
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orally
no |
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indication for itraconazole
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Pulse dosing for onychomycosis (fungal nail infections)
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Pulse dosing for onychomycosis (fungal nail infections)
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itraconazole
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1st-line agent for treatment of acute, invasive aspergillosis
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voriconazole
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indications for voriconazole
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-1st-line agent for treatment of acute, invasive aspergillosis
-treatment of nonneutropenic patients with candidemia or deep tissue candidal infection |
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treatment of nonneutropenic patients with candidemia or deep tissue candidal infection
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voriconazole
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prophylaxis of invasive aspergillosis and candidiasis in patients who are severely immunocompromised
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Posaconazole
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indication for Posaconazole
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prophylaxis of invasive aspergillosis and candidiasis in patients who are severely immunocompromised
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ADRs of posaconazole
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- hepatic failure, sometimes severe
- QT prolongation |
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empirical treatment of presumed fungal infections in febrile, neutropenic patients
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Caspofungin
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indication for Caspofungin
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empirical treatment of presumed fungal infections in febrile, neutropenic patients
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OTC 1% cream or solution; treatment of tinea pedis, tinea cruris, and tinea corporis
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clotrimazole
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-interacts with the fungal cell microtubules to disrupt the mitotic spindle and inhibit mitosis
-therapy must be continued until normal tissue replaces infected tissue (weeks to months) |
griseofulvin
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is Griseofulvin fungicidal or fungistatic?
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fungistatic..only active against dermatophytes
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-synthetic fungicidal agent which inhibits squalene epoxidase, an essential enzyme in fungal sterol synthesis; produces a deficiency of ergosterol and an accumulation of squalene inside the fungal cell resulting in cell death
-indicated for treatment of onychomycosis of the toenail or fingernail due to dermatophytes |
terbinafine
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indication for terbinafine
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treatment of onychomycosis of the toenail or fingernail due to dermatophytes
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Agents for Topical/Vaginal Candidiasis
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-Nystatin
-Clotrimazole -Miconazole |
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vaginal formulations for local treatment of VVC
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-terconazole
-butoconazole |
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how is Nystatin dosed?
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oral suspension: 5 mL qid (one-half of dose in each side of mouth, “swish and swallow”, retaining the drug as long as possible before swallowing)
-topical for superficial Candida fungal infections of the skin, mucous membranes, and intestinal tract -oral suspension for “swish and swallow” treatment of oral candidiasis (too toxic for systemic administration; not absorbed po) |
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polyene antibiotic similar in structure and mechanism of action to amphotericin B (alters cell membrane permeability); broad-spectrum, may be either fungicidal or fungistatic
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nystatin
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is clotrimazole fungicidal or static?
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cidal
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how is clotrimazole given?
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buccal tablet: indicated for local treatment of oropharyngeal candidiasis (1 troche 5 times qd for 14 days), and for prophylaxis of oropharyngeal candidiasis in immunocompromised patients
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DOC for trichomoniasis
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metronidazole
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metronidazole tx for trichomoniasis guidelines
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- clinical syndromes of vaginitis, nongonococcal urethritis (5% of cases in males), prostatitis
- must also treat sexual partner and practice abstinence until cure is effected (therapy completed and both partners asymptomatic) - preferred regimen is 2 g po single dose |
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DOC for helminthic infections (pinworm, whipworm, roundworm, hookworm)
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Mebendazole: 100 mg chewable tablet
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what is mebendazole the DOC for?
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helminthic infections (pinworm, whipworm, roundworm, and hookworm)
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CDC recommended that neither __ or __ be used for treatment or prophylaxis of influenza in the US until susceptibility is re-established among circulating influenza A viruses
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amantadine nor rimantadine
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ADR of zanamivir
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not recommended for treatment or prophylaxis in patients with underlying airways disease (asthma or COPD) due to risk of serious bronchospasm
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- treatment of uncomplicated acute illness due to influenza virus (Types A and B) in adults and adolescents >= 7 years old who have been symptomatic for <= 2 days
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zanamivir
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treatment of uncomplicated acute illness due to influenza virus in patients > 1 year of age who have been symptomatic for <= 2 days
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oseltamivir
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neuraminidase inhibitors
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zanamivir and oseltamivir
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__is a synthetic guanosine nuceloside analog; in host cells, ribavirin is phosphorylated by cellular kinases to the monophosphate, diphosphate, and triphosphate forms; these forms subsequently interfere with critical reactions needed for viral replication, blocking the synthesis and replication of viral RNA
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ribavirin
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TREATMENT of severe lower respiratory tract infections due to RSV in hospitalized infants and young children
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ribavirin
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indicated for prevention of serious lower respiratory tract disease caused by RSV in high-risk pediatric patients
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palivizumab
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TX of RSV is __
PREVENTION of RSV is __ |
ribavirin
palivizumab |
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acyclovir is phosphorylated in the viral-infected cell by the viral enzyme __; basis for selective toxicity is that this reaction occurs 100 times more rapidly inside the virus-infected cell than in noninfected host cells
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thymidine kinase
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what disease is resistant to acyclovir? why? what diseases are sensitive to it?
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cytomegalovirus (CMV) is resistant since it lacks a specific viral thymidine kinase
herpes simplex virus-1 (HSV1), HSV2, varicella-zoster virus (VZV), Epstein-Barr virus (EBV) |
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ADR of acyclovir
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nephrotoxicity if given as IV bolus or if solubility is exceeded due to tubular precipitation of ACY crystals (give only by slow infusion over at least 1 hr with adequate hydration)
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synthetic analog of ACY; prodrug which is converted intracellularly to an active triphosphate form
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ganciclovir
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spectrum of antiviral activity is similar to ACY with the exception that ganciclovir is __
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active vs. CMV
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antiviral that is active against CMV
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ganciclovir
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ADR of ganciclovir
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myelosuppression
- neutropenia - anemia - thrombocytopenia |
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DIs with ganciclovir
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-nephrotoxic drugs: increased SCr, additive nephrotoxicity
-probenecid: decreased renal clearance of ganciclovir -zidovudine: additive neutropenia and anemia |
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prodrug of the antiviral agent penciclovir
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famciclovir
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indication for famciclovir
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treatment of acute herpes zoster
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treatment of acute herpes zoster
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famciclovir
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prodrug of acyclovir to counter the problems with absorption of ACY
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valacyclovir (also acyclovir)
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2nd-line agent to ganciclovir for CMV
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foscarnet sodium
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indications for foscarnet sodium
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-2nd-line agent to ganciclovir for CMV
-active vs. ganciclovir-resistant CMV and ACY-resistant HSV and VZV |
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ADRs of foscarnet sodium
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-renal dysfunction
-seizures- increased risk with low serum calcium -chelation of divalent cations may cause hypocalcemia; decreased serum calcium may cause seizures; -anemia |
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3rd-line agent for CMV
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cidofovir
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how must cidofovir be given?
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must be administered by slow IV infusion with probenecid and IV saline prehydration
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ADRs of cidofovir
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-nephrotoxicity
-neutropenia |
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ester prodrug of ganciclovir
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valganciclovir
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primary keratoconjunctivitis and recurrent epithelial keratitis due to HSV-1 and HSV-2
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trifluridine
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indicated for treatment of recurrent herpes labialis (cold sores) in adults
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penciclovir
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antiretroviral therapy (ART) should be initiated in all patients with __ or __
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a history of an AIDS-defining illness or with a CD4 count < 350 cells/cmm
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ART should also be initiated, regardless of CD4 count, in patients with the following conditions: (3)
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-pregnancy
-HIV-associated nephropathy -HBV coinfection when treatment of HBV is indicated |
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antiretroviral therapy is recommended for patients with CD4 counts between __cells/cmm
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350-500
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HHART-all of the currently preferred regimens have the following characteristics:(3)
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-at least three antiretroviral drugs are used
-the regimens have combinations of drugs that have different mechanisms of action -class-sparing |
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recommended preferred antiretroviral regimens for initiating treatment in naïve patients
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regimen #1: one NNRTI plus two NRTIs
(efavirenz plus tenofovir/emtricitabine) |
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HAART: regimen #2
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ritonavir boosted PI plus two NRTIs
(atazanavir plus ritonavir tenofovir/emtricitabine or darunavir plus ritonavir tenofovir/emtricitabine) |
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HAART: regimen #3
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INSTI plus two NRTIs
(raltegravir plus tenofovir/emtricitabine) |
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preferred antiretroviral regimen for pregnant women
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lopinavir/ritonavir plus zidovudine/lamivudine
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HAART: __is the essential parameter in decisions to start or modify the drug regimen
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HIV RNA viral load testing
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key factor for deciding whether to initiate antiretroviral therapy and chemoprophylaxis for OIs
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CD4+ cell count
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HIV: strongest predictor of subsequent disease progression and survival
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CD4+ cell count
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treatment of acute HIV infection is considered __at this time
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optional
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resistance testing is of greatest value when performed before or within __
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4 weeks after drugs are discontinued
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NRTI stands for?
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NucleoSide Inhibitors of Viral Reverse Transcriptase
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clas effect ADR of NRTI
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rare cases of lactic acidosis with hepatic steatosis
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ADRs of zidovudine
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myelosuppression, neutropenia, severe anemia
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ADRs of didanosine
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-pancreatitis
-class effect: lactic acidosis and severe hepatomegaly with steatosis -peripheral neuropathy |
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ADR of lamivudine
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peripheral neuropathy
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combivir is a combination of what two drugs?
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lamivudine plus zidovudine
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ADR of abacavir
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hypersensitivity reactions
***screen them for HLA-B*5701 before starting this drug |