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99 Cards in this Set
- Front
- Back
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Sulfonamide affects what enzyme
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dihydropteroate synthase
(competitive inhibition) (PABA --> DHF) |
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Tremothoprim enzyme affected
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inhibit DHF --> THF
block FA synth |
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Quinolones enzyme affected
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inhibit DNA gyrase (topoisomerase)
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What drugs affect folic acid synthesis
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Sulfonamides (PABA --> DHF)
Trimethoprim (DHF--> THF) |
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Trimethoprim AE
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AE
same as for sulfonamides plus HEMATOPOIETIC: LEUKOPENIA, MEGALOBLASTIC ANEMIA |
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sulfonamides moa
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analog of PABA inhibit dihydropteroate synthase
PABA --> DHF cant make purines |
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sulfonamide spectrum
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gram pos
gram neg chlamydia nocardia |
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sulfonamide topical drugs
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silver sulfadiazine
sulfacetamide triple sulfa |
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Silver sulfadiazine
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burns
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sulfacetamide
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ocular infections:
conjunctivitis, corneal ulcer |
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Triple sulfa
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vaginitis
(hemophilius vaginitis) |
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Oral Sulfonamides
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Sulfamethoxazole
Sulfisoxazole Sulfadoxine/pyramethamine Sulfadiazine/pyramethamine Sulfasalazine Dapsone |
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Sulfamethoxazole and Sulfisoxazole used for
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previously untreated UTI
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Sulfonamide AE effect (topical)
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irritation, stinging, burning
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Sulfonamide AE effect (oral)
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Systemic AE:
-Steven Johnson syndrome (fever,rash) -cross-sens w/ other sulfa drugs (sulfa, thiazide, sulfonyl urea) -crystalluria -HEMOLYTIC ANEMIA IF G6PD -kernicterus (newborn) |
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Hemolytic anemia in g6pd
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AE of sulfonamide
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sulfa containing drugs
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-sulfa
-thiazide -sulfonyl urea |
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Sulfonamide resistance
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1) overproduction of PABA
2)change enzyme dihydropteroate synthase 3) decrease permeability |
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Sulfonamide - general
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-bacteriostatic
-inhibits purine synthesis -gram neg,pos, chlamydia,nocardia -topical and oral |
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Trimethoprim spectrum
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gram neg
gram pos chlamydia nocardia |
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Sulfonamide Pharmokinetics
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-rapid GI absorption
-readily distrib (incl CSF) -acetylated at liver (product still toxic but not antimicrobial) |
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Trimethaprim Pharmokinetics
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-rapid GI absorption
-readily distrib (incl CSF) -most excreted uncahnged into urine -some transformed to inactive prods |
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Trimethaprim is usually used w/...
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usu used in combo with SULFONAMIDE --> SYNERGY
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Trimethaprim used alone
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Oral - UTI
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Trimethoprim + Sulfamethoxazole
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SYNERGY!!!
ORAL 1) pneumonia: pneumocystis carinii 2) GI infections: Shigella 3) Systemic infections: nocardia, salmonella 4) UTI and resp infection: H.influenza , strep pneum IV pneumonia : pneumocystis carinii |
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Sulfadoxine/pyramethamine
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malaria (long acting)
- - SULFONAMIDE |
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Sulfadiazine/pyramethamine
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toxoplasmosis
- - SULFONAMIDE |
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Sulfasalazine
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Inflammatory bowel disease
-not absorbed -active ingred = 5 amino salicylic acid - - SULFONAMIDE |
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Dapsone
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leprosy
- - SULFONAMIDE |
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Trimethoprim AE
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same like sulfonamide PLUS LEUKOPENIA, MEGALOBLASTIC ANEMIA
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synergistic combo of sulfonamide plus trimethaprim
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sulfamethoxazole + trimethaprim
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Quinolones
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-synthetic flourinated
-inhibit dna gyrase (cant unwind and replicate or transcribe) -doesnt affect our enzyme much |
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Quinolones Group 1
group 2 |
Group 1 = more on Gram neg
Ciprofloxacin Norfloxacin enoxacin lomefloxacin ofloxacin Group 2 = more on gram pos Levofloxacin Moxifloxacin |
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Topical Quinolone
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Ciprofloxacin / Ofloxacin
-superficial ocular infection conjntivitis, corneal ulcer |
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Superficial ocular infection drugs
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Sulfacetamide
Ciprofloxacin/ofloxacin |
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Oral Quinolone
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all group 1 quinolones
Previously untreated UTI Bone, skin suture infection Infectious diarrhea typhoid fever STD - neisseria Anthrax |
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Quinolone Pharmokinetics
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-well absorbed orally
(lowest = norfloxacin) -antacids containing Al or Ca salts delay absorp -small amt biotransformed in liver -most elim in urine |
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Group 2 Quinolones
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levofloxacin
moxifloxacin -respiratory tract infections including community acquired pneumonia (methicillin sens. staph, s. pneumonia) |
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Quinolones AE
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local - irritation, burn
Systemic: -CONTRAIND FOR PREGNANCY (damage growing cartilage) -some PROLONG QT INTERVAL avoid if taking anti-arrythmic or drugs that prolong QT interval (erythromycin, tricycic antidepressant) -nausea, diarrhea, rash, CNS distub, tendonitis |
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IV Quinolone
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Ciprofloxacin
ofloxacin |
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Quinolones - general
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-inhibit dna gyrase
-2 groups - gram negative/ poitive, chlamydia |
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Quinolones resistance
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1) microb mod of DNA gyrase
2) change permeability to drug |
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-floxacin
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quinolone
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Antivirals
BLOCK VIRAL UNCOATING |
(TRICYCLIC AMINES)
AMANTADINE RIMANTADINE -inhibit m2 proton channel in viral envelope |
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antivirals
DECREASE VIRAL RELEASE |
ZANAMIVIR
OSELTAMIVIR -neuraminidase inhibitors |
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antivirals
MIXED ACTING |
RIBAVARIN
guanosine nucleoside analogue -inhibits viral RNA Pol -inhibits GTP synth -blocks mRNA capping |
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antivirals
INHIBIT GENOME REPLICATION |
ACYCLOVIR
TRIFLURIDINE GANCICLOVIR CIDOFOVIR FOSCARNET -inhibit DNA pol |
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antivirals
INHIBIT TRANSLATION OF VIRAL mRNA |
INTERFERONS
-glycoprotein encoded by host cell acts on neighbor cells to inhibit rep, degrade mrna, and inhib peptide elong FOMIVIRSEN -anti mrna nucleotide (cant make important protein for rep) |
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Rimantadine/Amantadine
tricyclic amines |
Influenza A
-work best prophylactically -can treat w/vaccine simult (wont suppress Ab production) Amantadine also initial therapy for Parkinsons (DA) |
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Amantadine Pharmokinetics / other
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-oral
-excreted unchanged into urine (need dosage adjustment for renal impairment) -crosses BBB --> DA release -CNS EFFECTS!!! |
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Rimantadine Pharmokinetics / other
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-oral
-extensively metabolized (dont need dosage adjustment unless if creatine clearance really low) -less CNS effects than Amantadine |
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Zanamivir/Oseltamivir
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INFLUENZA A AND B
neuraminidase inhibitors (sialic acid not removed so binds hemaglutinin --> aggregation --> less viral release) -use early -good prophylactically, not approved -decreases flu complication |
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Zanamivir info
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-inhaled as dry powder
-poor bioavailability AE: bronchospasm in asthma (flu A and b....neuram inhib) |
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Oseltamivir info
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-prodrug
-well absorbed -nausea, vomit, headache -BIRD FLU (flu a and b...neuram inhib) |
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Ribavarin
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INFLUENZA A AND B
RESP SYNCYTIAL VIRUS VIRAL HEPATITIS (w. interferon) |
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Ribavarin MOA
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nucleoside analogue (guanosine)
MIXED 1)inhibits viral RNA Pol (competes w/ GTP and ATP) 2)Inhibits GTP Synth (inhibits IMP dehydrogenase) 3)blocks mRNA capping (inhibits N7 methyl transferase) lots of mechs --> less resistance |
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Ribavarin Use
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Aerosol:
-Flu A and B -resp synctial virus Oral: -Viral Hepatitis w/ IFN SYNERGY |
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Ribavarin AE
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When used ORAL: (w. IFN for hepatitis)
hemolytic anemia |
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Acyclovir
Trifluridine Ganciclovir MOA |
get phosph by VIRAL THYMIDINE KINASE
(acyclovir --> acyclovir monophosph) then acyclovir monophosph --> acyclovir triphosph via cellular kinase 1) inhibit DNA pol 2) incorp into DNA, terminate elongation |
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Acyclovir USE
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low dose: Herpes 1 and 2
High: Herpes, other trains Herpes encephalitis Herpes keratitis Mucocutaneous infections (immunocomp) IV Varicella zoster (immunocomp) |
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Acyclovir Pharmokin/ AE / Resistance
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IV
topical oral (bad bioavail) AE: 1% encepholopath nephrotoxicity Resistance: alter thymidine kinase |
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Trifluridine USE
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topical
HERPES KERATITIS (DOC) -use if acyclovir resistant |
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Ganciclovir structure/pharmokinetics
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-like acyclovir + CH2OH
IV @ acute oral @ maintenance |
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Ganciclovir USE
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CMV RETINITIS (serious only)
PNEUMONIA DUE TO CMV - KIDNEY TRANSPLANT PATIENTS (with anti-CMV antibody) |
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Ganciclovir AE
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bone marrow suppression
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Ganciclovir General
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CMV RETINITIS (serious bc TOXIC)
:o( - bone marrow suppression |
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Ribavarin
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Flu A and B
Resp syncytial virus oral - viral hepatitis (w. IFN) :O( - causes hemolytic anemia |
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Cidofovir
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nuceloside analogue - cytosine
(dont need viral kinase for phosph) USE: CMV RETINITIS (ganciclovir resistance) -IV (w. probenicid) AE: bone marrow supp renal toxicity |
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Foscarnet MOA
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Pyrophosphate analogue
-interact w/ PPi binding site --> inhibit DNA pol, reverse transcriptase CMV RETINITIS (ganciclovir resistance) AE: decrease renal function |
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CMV RETINITIS
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GANCICLOVIR (serious only bc toxic)
-bone marrow supp, some CNS CIDOFOVIR -bone marrow supp, renal tox FOSCARNET -decrease renal func FOMIVIRSEN -2nd line CMV retinitis (intravitreally) |
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INTERFERONS MOA
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1) kinase inhibits rep (inactivates IF)
2) endonuclease degrades viral mRNA 3) phosphodiesterase degrades tRNA --> inhib peptide elong |
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INTERFERONS pharmokin
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proteins so admin'd
IM subQ topical |
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INTERFERONS use
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Chronic Hepatitis B and C (w. ribavarin --> SYNERGY)
HAIRY CELL LEUKEMIA AIDS RELATED KAPOSI SARCOMA GENITAL WARTS (condyloma acuminatum) HERPES ZOSTER (given early prevent dissemination in cancer pts) HERPES KERATOCONJUNCTIVITIS |
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INTERFERONS AE
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AE:
neutropenia --> flu like symptoms -when used with ribavarin --> hemolytic anemia (no synergy of side effects) |
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FOMIVIRSEN MOA
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antisense oligonucleotide
against mRNA for protein needed for viral rep |
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FOMIVIRSEN use
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CMV RETINIS (2nd line)
-intravitreally |
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antifungal
FORM LYTIC ION CHANNEL |
Polyene Macrolide:
AMPHOTERICIN B NYSTATIN (bind sterol in PM, esp ergosterol, form cytotoxic pores) (lysis, decreased ATP) |
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most antifungal drugs target:
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cell membrane (have ergosterol)
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antifungal
DISRUPT NUCLEIC ACID SYNTHESIS |
FLUCYTOSINE
-antimetabolite -converted by fungi to active metab (FU) - inhibits RNA/DNA synthesis |
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antifungal
INHIBITS MITOSIS VIA DISRUPT. CYTOSKELETON |
GRISEOFULVIN
-inhibits microtubules -binds keratin -fungistatic!! |
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antifungal
INHIBITS ERGOSTEROL SYNTHESIS |
selectively inhibits fungal P450 enzyme
-IMIDAZOLE KETACONAZOLE MICONAZOLE CLOTRIMAZOLE (-triazole) inhibits more selectively ITRACONAZOLE FLUCONAZOLE VORICONAZOLE |
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antifungal
INHIBITS SQUALENE OXIDASE |
NAFTIFINE
TERBINAFINE -inhibits SO, increase is toxic decreases ergosterol |
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antifungal
INHIBITS CELL WALL FORMATION |
CASPOFUNGIN
-inhibits Beta 1,3 D- glucan synth (cell wall) |
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Amphotericin B USE
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-broadest spectrum
LIFE THREATENING SYSTEMIC INFECTIONS (doc) invasive Apergillus (w. itraconazole) crypto meningitis (w. flucocystine) histoplasosis dermatophytic mucocutaneous infections |
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Amphotericin B
info AE |
-given as IV liposome
-bad absorption AE: RENAL IMPAIRMENT hypokalemia fairly toxic, binds cholesterol |
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Nystatin USE
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local dermal/oropharyngeal infection
vaginal candidiasis -too toxic for systemic (unlike amphotericin B) just local topical |
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Flucocystine USE / AE
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oral combos (so decrease resistance and toxicity)
CRYPTO. MENINGITIS (w. ampho B) BLASTOMYCOSES (w. itraconazole) AE: narrow ther. window (bc FU metabolite) BONE MARROW TOXICITY!! |
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Griseofulvin USE
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dermaphytosis (nail infection)
extd. treatment after triazoles athletes foot, ringworm |
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Ketoconazole USE
AE |
mucocutaenous candidiases
coccidiomycosis (non-meningeal)- not CNS shampoo - seborr dermatitis AE interferes w/ adrenal/gonadal synthesis interfere w/ human p450 enzymes (use to decrease adrenal steroids in Cushings disease) |
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Miconazole/Clotrimazole USE
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topical antifungal
vulvovaginal candidiases dermatophytic infections oropharyngeal thrush - candidiases (clotrimazole - oral) alt to nystatin |
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Itraconazole USE
AE |
MOST POTENT AZOLE FOR SYSTEMIC INFECTION
PERSISTENT DERMATOPHYTOSIS (doc) EFFECTIVE AGAINST ALL APERGILLUS PREFERRED FOR ENDEMIC HISTOPLASMOSIS AE drug intx (w. non sedating histamine) no effect on steroid synth variable on human p450 |
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Fluconazole USE
AE |
CRYPTO. MENINGITIS (doc)
--good CSF -if life threatening --> ampho B mucocutaneous candidiasis prophylactic for bone marrow transplants - AIDS AE widest therapeutic window :O) |
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Naftidine/Terbinafine
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cutaneous mycoses (topical)
NAIL INFECTIONS - TERBINAFINE! -not affective against candida |
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Caspofungin USE
|
invasive candidiasis
apergillosis (alt to ampho B) -not affective against cryptococcus |
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Voriconazole USE
AE |
invasive Aspergillus (doc)
candida (even if resistant to fluconazole) meningitis (good CSF) AE visual disturbances hepatotoxity inhibit p450 |
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fungus
DERMATOPHYTE doc |
ITRACONAZOLE
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fungus
CANDIDA doc |
FLUCONAZOLE
(if resistant --> voriconazole) |
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fungus
CRYPTOCOCCUS doc |
FLUCONAZOLE (wide ther. window)
also: Flucocystine + Ampho B |
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fungus
ASPERGILLUS doc |
VORICONAZOLE
also: ampho B w. itraconazole(all asp) |
