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167 Cards in this Set
- Front
- Back
- 3rd side (hint)
What antifungal drug is NOT used to treat systemic fungal infections?
|
Griseofluvin
|
Also absorbed well with a high fat diet
|
|
Itraconazole [Sporanox]Administration
|
Capsule= wide range fungal infections [take with food] Oral solution= Candidiasis [take without food]
Injection= Empiric Tx for febrile neutropenia & blastomycosis [DOC] |
3 forms
|
|
Itraconazole [Sporanox]cautions
|
WARNING for CHF patients!!!
AEs- GI [Nausea], rash, HTN, HA |
|
|
Mepiridine is used in Amphtericin B administration to treat:
|
IV infusion related rxns [rigors, fever, chills; post op]
|
|
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Used to treat onchomycosis of the great toe
|
Terbinafine [Lotramin]
Cicloprox [Loprox] [Penlac] Griseofulvin [Fulvicin UF] *New- Itraconaole [Sporonox] |
4 antifungals
|
|
Ketoconazole [Nizoral] MOA
|
Inhibits fungal CYP450 enzyme [critical in ergosythesis pathway], interupting synthsis of ergosterol---> increased permeability of azoles into cell---> inhibits fungal growth
|
|
|
Ketoconazole Cautions
|
WARNING- Hepatotoxicity
AEs- CNS [Dizzy, HA, somnolence] GI [NV 10%, D, ab pain, hepatotoxicity] Psychiatric- SUICIDAL, SEVERE DEPRESSION [although rare] Miscellaneous- pruritis, fever/chills, IMPOTENCE, GYNECOMASTIA, thrombocytopenia, leukopenia, hemolytic anemia, bulging fontanells, hypersens, oligospermia |
|
|
Ketoconazole Administration
|
BROAD SPECTRUM Antifunal
Systemic- Candidiasis, Oral thrush, histoplasmosis [target lesion],Coccidiomycosis Topical- Tineas & cutaneous candidiasis |
2 Forms
|
|
What antifungals cross CSF?
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Terbinafin [Lotramin]
Flucytosine [Ancobon] Fluconazole [Diflucan] |
3
|
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Which antifungals require dose adjustment for renal PTs?
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Flucytosine [Ancobon]
Fluconazole [Diflucan] |
2 Fs
|
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Ketoconazole Drug Drug Interactions
|
Amphotericin B
Rifampin Other CYP450 metabolized drugs |
3
|
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Itraconazole Drug Interactions
|
CYP 450 metabolized drugs [could lead to seroius cardiac events--> QT elongation, V-Tach, cardiac arrest, sudden death]
|
|
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Lamasil Indication
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Dermatophytosis [Tineas]
|
|
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What antifungal is FUNGICIDAL?
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Lamisil [Terbinafine]
|
|
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What 2 Antifungals are listed as FUNGISTATIC in our notes?
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Flucytosine & Griseofulvin
|
|
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Griseofulvin is FUNGISTATIC against what 3 infections?
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Trihopyton
Microsporum Epidermophyton |
|
|
Griseofulvin MOA
|
Inhibits fungal mitosis by disrupting formation of mitotic spidles & inhibiting fungal mitosis
|
|
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Griseofulvin- length/description of therapy?
|
Requires LONG TERM therapy [weeks-months-up to 6 months]
Must wait for infected keratinized tissue to grow out & be replaced by normal tissue |
Griseofulvin Gooooooooooooo Grow Out
|
|
Griseofulvin Administration
|
Oral [good absorption with high fat diet] but NOT Topical!!!
|
|
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Griseofulvin Drug Interactions
|
Phenobarbital [Dec. Gris.]
Oral Anticoagulants [Gris. INCREASES the rate of their metabolism] ETOH [Gris. potentiates the effects] |
3 major
|
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What antifungals are CYP450 INHIBITORS?
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All Azole Antifungals
|
|
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What antifungal (s) are CYP450 INDUCERS?
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Griseofulvin Fulvicin UF]
|
|
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Why can't you treat Candida with Ketoconazole if a PT is also on Cyclosporin for immunosuppression?
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Ketoconazole inhibits the CYP450 enzymes that inactivate cyclosporin
|
|
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What drug is now used to treat Onchomycosis, but originally was only used for blastomycosis & histoplasmosis in immunocompromised PTs?
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Intraconazole [Sporanox]
|
|
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Itraconazole distribution/penetration
|
Does NOT penetrate CNS, however DOES penetrate most all other body tissue well
|
|
|
Vehicle/Antifungal for topical application in the treatment of onchomycosis?
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Laquer- Cicloprox [PenLac]
Cream- Cicloprox [Loprox], Terbinafine [Lotramin] * Griseofulvin is INEFFECTIVE topically |
|
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CHF "Black Box" Warning
|
Itraconazole [Sporanox]
|
|
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Cicloprox MOA
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Inhibits transport of essential elementsin fungal cell---> problems in synthesis of DNA, RNA, proteins
|
|
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Caspofungin in 2001 was approved for treatment of
|
*Invasive aspergillosis IV Infusion for PTs who can't tolerate standard Tx [AmB, Lipid AmB, Itraconazole]
[Also used to treat candidemia, oropharyndeal/esophageal candidiasis] |
|
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Caspofungin belongs to this class of anti-fungals
|
Glucan Sythesis Inhibitors
Echinocandin |
|
|
Nucelotide Reverse Transcriptase Inhibitors MOA & Target
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Target- HIV
MOA- Phosphorylated by cellular enzymes to nucleotide triphosphate--> Inhibits reverse transcriptase b/c doesn't have 3'OH groups to continue Viral DNA elongation |
|
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Binding site of the nuclotide molecule
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Nucleotides are added to the OH group of the 3' end--> OH of one forms an ester bond with phosphate of another--> eliminates a molecule of H2o
|
|
|
Major toxicities of the reverse transcriptase inhibitors
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Lactic acidosis [esp. Stavudine], hepatotoxicity [mainly Zidovudine], All NRTIS- Renal Toxicities [except ABC], Pancreatitis, Peripheral Neuropathy, Fat redistribution syndrome [suggested]
|
|
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The 4 main Antiviral inducers of the SEs Pancreatitis & Peripheral Neuropathy
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Zalcitibine, Stavudine, Didanosine, Lamivudine [but notes say ALL RTIs cause these 2 SEs
|
|
|
Abacavir [Ziagen] [ABC] Toxicity
|
Some FATAL HYPERSENSITIVITY RXN [Watch PT for signs of respiratory distres- discontinue immediately]; rash, fever, fatigue
|
|
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Numbness & pain in lower extremities [peripheral neuropathy] is a SE that is REVERSIBLE in what NRTI?
|
Didanosine [ddL, Videx]
|
|
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Peripheral Neuropathy is a SE that is NOT ALWAYS REVERSIBLE in what NRTI?
|
Zalcitabine [Hivid]
|
|
|
Which antiviral has been discontinued/taken off the market?
|
Zalcitabine [Hivid]
|
|
|
Didanosine Administration
|
Tablet [ddL]- chew or crush up
Enteric coated capsule [Videx]- DON'T chew, crush |
|
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Lamivudine Drug Interactions
|
Zalcitabine [Lamivudine inhibits phosphorylization of it so it never gets activated]
|
|
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Which antiviral must undergo glucuronidation in the liver b/f it can be excreted renally?
|
Zidovudine [AZT, Retrovir]
|
|
|
NRTIs special MOA slight differences
|
Zidovudine- Non listed
Didanosine-metab to dideoxadenosine triphosphate Zalcitabine- ddC, dideoxycytidine Lamivudine- 3TC Stavudine- dTTT Abacavir-dGTP Tenofovir- diPO4/ doxyadenosine 5'triPO4 |
|
|
Abacavir
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NRTI, competes with dGTP, take orally, FATAL HYPERSENSITIVITY
|
|
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Non-Nucleoside RTIs [NNRTIs] MOA & drugs in class
|
Bind DIRECTLY to HIV reverse transcriptase to inhibit formation of viral DNA; Efavirenz, Delaviridine, Nevirapine, Atripia
|
|
|
HIV Protease MOA
|
Jam the catolytic site of precursor proteins encoded by viral mRNA--> inhibit the enzyme responsible for cleavage of viral polyprotein into essential enzymes [reverse transcriptase, protease, integrase, capsid, & matrix proteins]
|
|
|
What drug is used in combo with Lopinavir to inhibit the CYP-450 metabolism?
|
Ritonavir
|
|
|
Major SEs of Protease Inhibitors
|
Lipodystrophy, fat redistribution syndrome, elevated TG & cholesterol, glucose intolerance, CYP-450 Inhibition, HEPATIC IMPAIRMENT, parasthesias, NVD
|
|
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DDI of PIs
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Rifampin [decreases effectiveness b/c inhibits CYP-450]
|
|
|
Chronic fat redistribution in abdomen & base of neck caused by PIs is aka:
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"Buffalo hump"
|
|
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Which PI is available as a soft gel?
|
Saquinavir [Invirase, Fortovase]
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|
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Which Antiviral has MORE DRUG INTERACTIONS than any other HIV drug?
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Ritonavir [Norvir]
|
|
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Which PI was specifically stated in our notes to have good oral bioavilability when given WITH FOOD?
|
Saquinavir [Fortovase]
|
|
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Which PI causes kidney stones in 3-4% of PTs?
|
Indinavir [Crixivan]
|
|
|
Ritonavir is a major problem b/c it:
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Induces metabolic enzymes--> induces own metabolism potent inhibitor of cyp3A--> increases levels of many other drugs
|
|
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Which PI seems to be well tolerated in PTs?
|
Nelfinavir [Viracept]
|
|
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Which PI has serious/life-threatening Drug interactions with amiodarone, lidocaine, tricyclic antidepressants, quinidine?
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Amprenovir [Agenerase]
|
|
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Which PI has a drug interaction with ST. JOHN'S WORT?
|
Amprenavir [Agenerase]- ST.JOHN'S decreases the concentration of Ampernavir
|
|
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What's a good PI combo drug, & why?
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Lopinavir + Ritonavir [Lopinavir is completely metabolized by cyp3A; Ritonavir enhances b/c it inhibits cyp3A, so levels of Lopinavir are INCREASED]
|
|
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What are the life-threatening/serious Drug Interactions of Amprenovir [Agenerase]?
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Amiodarone, lidocaine, tricyclic antidepressants, quinidine; St. John's Wort
|
|
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Discuss Hepatic Failure & some specific PIs.
|
1- Increased risk for transaminase elevations [esp. in PTs w/Hep B/C]
2- Ritonavir is assoc. w/ abnormal LFTs in PTs with Viral Hep. 3- Tipranavir increases risk for severe hepatotoxicity in combo with Ritonavir. 4- Amprenavir concentration is increased when a PT has cirrhosis [inc risk of AEs]. |
|
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Tipranavir Drug Interaction [Reaction description]
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Ritonavir [Norvir]- Tipranavir increases risk for severe hepatotoxicity when given in combo with Ritonavir.
|
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Which PIs are listed as cyp3A inhibitors in our notes?
|
Ritonavir & Amprenavir
|
|
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What drug can Ritonavir be given with to enhance it's effects?
|
Liponavir [This combo is called Kaletra]
|
|
|
Effects of AntiHTN meds on PIs:
|
AntiHTN meds are metabolized by cyp450 so may increase or decrease the metabolism of a PI [CCBs & Verapamil are most likely to do this]
|
|
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Of the PIs, Ritonavir [RTV?] most interactions with antihypertensives?
|
CCB & BB
|
|
|
When to/to not adjust therapy for an HIV Pt
|
do NOT change therapy based on 1 viral load result [esp. after vaccination]
|
|
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Acycolvir indications
|
HSV, VZV
|
|
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Acyclovir MOA
|
Competes with dGTP & causes DNA chain termination
|
|
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Acyclovir is the DOC for
|
herpes Simplex Encephalitis
|
|
|
Acyclovir inhibits [active/latent] viruses.
|
ACTIVE ONLY!
|
|
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Ganciclovir [Cytovene] Indications
|
CMV retinitis in ImmC PTs,
CMV DZ & preventative Tx in transplant PTs, CMV congenital in newborns |
|
|
Foscavir [Foscarnet] Indications
|
CNV retinitis, CMV colitis, CMV esophagitis, Acyclovir-resistant HSV/VZV infections
|
|
|
Foscavir [Foscarnet] Toxicities
|
Nephrotoxicity, HA, Fever, NV, Anemia
|
|
|
Foscavir [Foscarnet] Toxicities are increased when...
|
Administered rapid/bolus IV or Injection; Use an infusion pump!
|
|
|
Oral therapy for CMV retinitis is
|
Gancyclovir for AIDS PTs
|
|
|
This anti-CMV drug is most likely to cause additive myelosuppression when administered with Zidovudine
|
Gancyclovir
|
|
|
Ribavirin treats the following in children...
|
RSV in hospitalized children [It's also used to Tx Hep C, Lassa fever, & Hanta virus]
|
|
|
Black Box warnings for Ribavirn
|
Birth defects &/or fetal death, genotoxic & mutagenic, potential carcinogen, causes hemolytic anemia
|
|
|
Name the Anti-Influenza drugs
|
Amantadine & Rimantadine
Zanavamir & Oseltavimir |
|
|
Amantidine & Rimantidine MOA
|
Interfere with viral coating & nucleic acid release of influenza A, but B inhibits the ion channel formed by the viral M2 protein, which promotes dissociation of the ribonucleoprotein complex & uncoating of the viron
|
|
|
Zanavimir & Oseltavimir MOA
|
Neuraminidase inhibitors- inhibit viral neuraminidase; Analogs of salicilic acid & act to block the active site of neuraminidase for influenza A & B with < 2 days symptoms
|
|
|
Anti-Influenza Drugs Indications
|
Amantidine & Rimantidine- Influenza A ONLY
Zanamivir & Oseltavimir- Influenza A & B |
|
|
Used SOLEY in the treatment of influenza A infections
|
Amantidine
|
|
|
The test used to definitavely diagnose HIV infection:
|
ELISA
|
|
|
The nucleoside reverse transcriptase inhibitors MOA
|
Phosphorylated by cellular enzymes to nucleotide triphosphate; inhibits reverse transcriptase; causes viral DNA chain to be terminated if it is incorporated into one b/c it lacks the 3'OH group
|
|
|
Protease Inhibitors suffix
|
"NAVIR"
|
|
|
Drug therapy for HIV should be a combination of 3 drugs:
|
2 NRTIs & 1 potent PI
|
|
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Name the 2 neuraminidase inhibitors we've discussed
|
Zinamivir & Oseltavimir
|
|
|
MOA of Neuroaminidase inhibitors
|
Zinamivir & Oseltavimir inhibit viral neuraminidase, an enzyme that cleaves sialic acid residues resulting in release of viral progeny
|
|
|
Zanamivir is for ages ____
Oseltamivir is for ages ____ With less than ___ days symptoms |
zanimiavir- > 7 YO
Oseltamivir- > 1 YO < 2 days symptoms |
|
|
Discuss Enfuviritide [Fuzeon] Use
|
1st in a new class of anti-HIV drugs known as Fusion Inhibitors; granted accelerated approval on March 13, 2003; used in combo with other antiretroviral agents; No studies of enfuzeon in antiretroviral naive PTs; no results on clinical progression
|
|
|
Fuzeon [Enfuviritide] MOA
|
Blocks HIV's ability to infect healthy immune [CD4] cells; Slows HIV progression in PTs who have developed resistance; blocks gp41 protein; disrupts the structural arrangement necessary for the virus to fuse
|
|
|
High concentration of Hep B virus can be found in the _____ of an infected carrier.
|
High- blood/serum/wound exuda
Mod- Semen/vaginal fl/saliva Low- urine/ feces/ sweat/ tears/ breastmilk |
|
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Oral or esophageal thrush [candida] is considered an AIDS defining Illness along with _____ at what CD4 count?
|
oral hairy leukoplakia & TB @ CD4 counts of 200-300
|
|
|
@ CD4 Counts of 200-100, what are the AIDS definfing illnesses?
|
PCP, Histoplasmosis, Cocci, Crypto, toxoplasmosis
|
|
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@ CD4 counts <100, what are the AIDS defining illnesses?
|
HSV, crypto, CMV, MAI
|
|
|
In reference to "AIDS defining illnesses", check for associated pathogens such as":
|
T.pallidium & Hep B
|
|
|
Clinical latency symptoms with viral tendency?
|
Clinical Latency is NOT SYNONYMOUS with viral or immunologic latency!!!!!
|
|
|
Combivir is a combination ...
|
Pill with 150 Lamivudine & 300 mg Zidovudine
|
|
|
Rifampin should be avoided in combination with:
|
Protease inhibitors, Ketoconazole, etc.
|
|
|
Ribaviren's Black Box warning
|
Birth defects/death of fetus, genotoxic & mutagenic, pathogenic carcinogen, hemolytic anemia [may result in worsening cardiac disease]
|
|
|
Drugs & their metabolites can be excreted via:
|
Urine/renal, bile, saliva, sputum, milk
|
|
|
INH excretion
|
Saliva, sputum, milk, renal
|
|
|
Amphotericin B & Rifampin excretion
|
urine & bile
|
|
|
Anti-tubercular agent associated with ototoxicity
|
Streptomycin
|
|
|
INH is metabolized by
|
a liver N-acetyltransferase
|
|
|
TB history/epidemilolgy
|
Leading killer of IDZ worldwide [1/3 infected die; 3 million/year] Men 2x Women; Rate of increase is 0.4% but a lot faster in Africa
|
|
|
The short couse chemotherapy for TB
|
INH & RIF [others are weaker & take longer]
|
|
|
Rifampin is an [inducer/inhibitor] of the CYP-450 system
|
INDUCER
|
|
|
The 2 CYP-450 inducers in this section that we've talked about
|
Griseofulvin & Rifampin
|
|
|
Drug regimen for the treatment of leprosy
|
Dapsone, Clofazimine, Rifampin x 6-24 months
|
|
|
INH is usually administered
|
PO
|
|
|
High risk post exposure to TB should be treated with
|
Isoniazid [INH] 300 mg/day for 12 months
|
|
|
Antibiotics associated with the development of Hepatitis
|
Isonazid [INH] is most closely associated
|
|
|
INH & ____ should be used together whenever possibl
|
Rifampin
|
|
|
Mycobacterium infections include
|
TB, M.bovis, Atypical Mycobacterial Infxn, & M. leprosae
|
|
|
TB therapy began with these 3 drugs:
|
Streptomycin
Isoniazid P-aminosalicylic acid |
|
|
Extrapulmonary TB can be found in:
|
CNS, peritoneum, genitourinary tract, lymph system, skeletal system, pericardium, adrenal glands, liver
|
|
|
TB Etiology:
|
1- Mycobacterium tuberculosis
2- 60 species [aerobic, non-spore-forming rods] 3- Ghon Complex [calcification in hilar lymph nodes] 4- Acid-fast bacilli [AFB]- stain with carbol-fuchsin 5- Cavitary & laryngeal TB- high transimission rate |
|
|
Ghon Complex- From the host’s point of view, the residue of a successful encounter with the tubercle bacillus is
|
a peripheral, rounded scar, less than 1 cm in diameter, in the lower half of the lung. Together with a similar scar in a hilar lymph node, it is known as the Ghon complex.
|
|
|
Chemotherapy of TB first line therapy
|
1- Isoniazid [INH]
2- Rifampin [RIF] 3- Pyrazinamide 4- Ethambutol 5- Rifabutin [Mycobutin] 6- Rifapentine |
|
|
Second line TB therapy
|
1- Amikacin [Amikin]
2- Ethionamide 3- Aminosalicylic Acid 4- Levofloxacin 5- Capreomycin 6- Moxifloxacin 7- Streptomycin 8- Gatifloxacin 9- Cycloserine |
|
|
Desired outcome of TB treatment
|
1- Identification of new TB case
2- Isolation of active case PT 3- Sample collection 4- TB treatment [Multi drug therapy- @ least 2 active agents] 5- Signs & symptoms resolution 6- Achieving non-infectious state 7- Medication compliance/ cure |
|
|
The MOST ACTIVE agent for treatment of TB is
|
Isoniazid [INH]
|
|
|
INH AB spectrum
|
1- Bacteriostatic against stationary phase
2- Bactericidal against dividing organisms 3- NEVER USED ALONE Given alone, INH administration selects out resistant mutants which necessitates additional agents. |
|
|
Resistance mechanisms agaisnt INH
|
1- Inability of organism to accumulate drug
2- Altered target enzyme [no binding with INH] 3- Excessive enzyme to overwhelm drug *about 10% of TB isolates are INH resistant |
|
|
INH MOA
|
INH inhibits mycolic acid synthesis, an essential part of mycobacterial cell walls.
|
|
|
INH Metabolism/ Excretion
|
Hepatic by acetylation [influenced by genetic predisposition for fast or slow acetylation
*May need to DOSE ADJUST for Liver PTs Renal excretion |
|
|
INH Dose
|
Dose 300 mg QD
—> 6 months [65- 69%] to 12 months [75-93%] |
|
|
INH administration instructions
|
EMPTY stomach, AVOID ANTACIDS w/in 2 hrs of INH
|
|
|
INH is absorbed _____
|
orally [avoid food & aluminum]
|
|
|
INH t 1/2
|
Greater in infected tissues
|
|
|
INH Drug interactions
|
Phenytoin [metabolism inhibited]
|
|
|
Rifampin [RIF] MOA
|
Inhibits RNA synthesis in prokaryotes; NEVER USE ALONE!!!
|
|
|
RIF indications
|
1- Treat carriers of N.meningitidis
A- Prophylaxis for household against meningitis [meningococci or H.influenzae] B- Effective against many gram (+) & gram (-) species 2- MOST ACTIVE ANTI-LEPROSY DRUG |
|
|
The most active anti-leprosy drug is
|
RIF
|
|
|
RIF is administered in what form?
|
Oral
|
|
|
RIF & CNS penetration?
|
Good CNS penetration
|
|
|
RIF & CYP-450
|
INDUCER
|
|
|
RIF & Discoloration
|
Red-orange discoloration in urine, tears, feces, contact lenses
|
|
|
Pyrazinamide is orally effective in combo with
|
INF & RIF
|
|
|
Pyrazinamide Spectrum
|
Bactericidal or Bacterialstatic
[Bactericidal to DIVIDING organisms] |
|
|
Pyrazinamide Metabolism
|
MUST be metabolized to active drug form
[pyrazinoic acid; Resistance to hydrolysis by certain strands of TB] |
|
|
Pyrazinamide distribution
|
Good throughout body, PENETRATES CNS
|
|
|
Pyrazinamide AEs
|
1- Hepatotoxicity/ Liver dysfunction [1-5% of PTs on INF/RIF/Pyrazinamide combo]
2- Gout Attack [ Due to Urate retention] 3- Thrombocytopenia 4- Interstitial Nephritis 5- N& V 6- Anorexia 7- Siderblastic Anemia 8- Rash, urticaria, pruritis |
|
|
Pyrazinamide Dose
|
1- 15-30 mg/kg/day
2- Max- 2 gms/day if on daily regimen; may be administered in twice-weekly doses of 50-70 mg/kg |
|
|
Pyrazinamide CIs
|
1- Severe hepatic damage
2- Acute Gout 3- Pregnancy category C [risk to fetus can’t be ruled out; use only if benefit outweighs risk] |
|
|
When PTs are on Pyrazinamide, you should monitor levels of ...
|
Monitor levels of LFTs, Uric Acid, follow up of TB symptoms, CXR, & sputum
|
|
|
Ethambutol Spectrum/ resistance/ combination indications
|
1- Bacteriostatic
2- Specific for strains of M.tuberculosis & M.kansasi 3- Resistance- not a big problem if given with other anti-TB agents 4- MUST BE USED IN COMBO [Pyrazinamide, Isoniazid, Rifampin] |
|
|
Ethambutol Kinetics
|
1- Good oral absorption
2- Distributed well throughout body 3- CNS penetration adequate in TB meningitis 4- Excretion- Glomerular Filtration & Tubular Secretion |
|
|
Ethambutol AEs
|
1- Optic Neuritis [results in diminished visual acuity & loss of ability to discriminate b/t red & green]
2- Gout attack [decreased Urate excretion] 3- Toxic effects on discontinuation ARE REVERSED |
|
|
Ethambutol Dose
|
1- Myambutol 100 mg, 400 mg tablets available
2- 15 mg/kg/day PO 3- Max- 1500 mg/day |
|
|
For PTs on Ethambutol, Monitor ...
|
Visual acuity, uric acid, LFTs
|
|
|
Streptomycin MOA
|
MOA- inhibits protein synthesis [aminoglycoside] binds to 30S ribosomal sub unit
|
|
|
Streptomycin duration of treatment
|
Duration- 12 months of MULTI-DRUG therapy [INH, RIF, PYR] MINIMUM
—> Usual treatment of TB is 2 months of [INH, RIF & PYR] followed by 4 months [INH & RIF] —> Streptomycin is added in |
|
|
Streptomycin Dosing
|
Dose- based on body weight
1- Serum concentration: 20-30 mcg/mL 2- Toxic serum levels: > 50 mcg/mL [peak] |
|
|
Streptomycin is usually administered ___ & toxic serum levels are ____
|
IM, > 50mcg/ml
|
|
|
Streptomycin AEs & CIs
|
1- Severe N& V & dizziness, rash, & fever
2- Loss of hearing w/long term use reported CIs- PTs with renal impairment |
|
|
Para- aminosalicylate Na [PAS] Spectrum, MOA, Kinetics
|
a- Spectrum- Bacteriostatic only against M.tuberculosis
b- MOA- inhibits folic acid synthesis—> inhibited bacterial synthesis c- Kinetics 1- Oral administration [take with/after meals or with antacid] 2- Readily absorbed from GI tract |
|
|
Para- aminosalicylate Na [PAS] SEs, dosing, & CIs
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d- SEs
1- NVD 2- peptic ulcer [rare] 3- hemorrhage [rare] e- Dose 1- PAS sodium must not be used alone for treatment of TB 2- Adults: 10-12 g orally per day in 2-4 divided doses f- CIs- Dose adjustment in renal PTs |
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3 DRUG regimen for Leprosy "Hansen's DZ"
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3 Drug Regimen:
a- Dapsone b- Clofazimine c- Rifampin |
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Dapsone Related to ____, indications, MOA
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—> Related to sulfonamides
a- Indications- Bacteriostatic for M.leprae & PCP b- MOA- PABA antagonist [inhibits folate synthesis] |
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Dapsone Kinetics
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1- Good oral bioavailability
2- Metabolism- Hepatic 3- Excretion-Urine 4- Distribution- good throughout whole body |
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Dapsone AEs
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1- Hemolytic Anemia [G6P deficiency]
2- Methemoglobinemia 3- Peripheral Neuropathy 4- Possible dev of Erythema Nodosum leprosum [treat with corticosteroids or thalidomide] |
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Clofazimine [Lamprene] Indications, MOA, Spectrum
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a- Indications- Therpay for Hansen’s Disease [Dapsone resistant- 20% cases] b- MOA- inhibits DNA replication & forms toxic O2 radicals
c- Bacteriacidal against M.leprae |
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Clofazimine AEs
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1- Skin [including retina] & urine colored RED
2- Lesions colored blue-black 3- NOT Erythema Nodosum like Dapsone [b/c it’s anti-inflammatory] |
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Clofazimine CIs
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1- Hypersensitivity to clofazimine
2- Liver or Kidney Damage 3- Pregnancy/Lactation safety not yet established |
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