Difference between peniciliin G and V.
G = IV and IM. V = oral. pharmacology micro
Bind penicillin-binding proteins(transpeptidases), block cross linking of peptidoglycans;most effective on G+, also N. Meningitidis, Treponema;hypersensitivy reaction, hemolytic anema. pharmacology micro
bind transpeptidases, penicillanse resistant due to bukly r-group blocking B-Lactamse; S. Aureus, except MRSA; hypersensitivity and interstitial nephritis. pharmacology micro
bind transpeptidases, wide spectrum and more penicillinase sensitive. combo with claculanic acid to protect from B-lactams;kills enterococci(HELPSS)H.iB, E.coli,Listera,Proteus,Salmonella,Shigella,enterococci;hypersensitivity reaction,rash,pseudomemrane colitis. pharmacology micro
Which has better bioavailibility; amoxicllin or ampicillin?
amOxicllin has better Oral bioavilability. pharmacology micro
What does clavulanic acid do?
B-lactamse inhibitor pharmacology micro
transpeptidase inhibitor but extended spectrum;pseduomonas and g- rods, use with claculanic acid due to B-lactamse suspectibilty; hypersensitivity reaction. pharmacology micro
List the B-lactamse inhibitors
(CAST) Clavulanic Acid, Sulbactam,Tazobactem. pharmacology micro
inhibit cell wall synthesis but are less susceptible to B-lactamases, are bactericidal;use depends on generation, there are four;hypersensitivty reactions, vitamin K defiency, increased nephrotoxicity of aminoglycosides. pharmacology micro
give use of cefazolin, cephalexin.
1st generation cephalosporins. PEcK. Proteus, E.coli,Klebsiella. Cefazolin used preop to prevent A.aureus infections. pharmacology micro
give use of cefoxitin, cefaclor,cefuroxime`
2nd generation cephalosporins. HEN PEcKs. H.ib, Enterbacter, Neisseria, Proteus, E.coli,Klebsiella, Serratia. pharmacology micro
give use of ceftriaxone, cefotaxime,ceftazidime
3rd gen. cephalosporins. Serious gram - infections. Ceftriaxone = meningitis and gonorrhea. Ceftazidime = pseudomonas. pharmacology micro
give use of cefepime.
increased activity against pseudomonas and G+ bugs. pharmacology micro
a monobactem resistant to B-lactamases, prevents binding to PBP3 and is synergistic with aminoglycosides;gram - rods only;very nontoxic, some GI upset. pharmacology micro
what transpeptidase inhibitor can be used in penicillin allergy?
aztreonam. pharmacology micro
broad spectrum, B-lactamase resistent but imipenem needs cilastatin to inhibit renal dehydropeptidase. later carbepenems do not;G+ cocci,G- rods, anerobes. used only in life threating events;skin rash, CNS toxicity, seizures. pharmacology micro
inhibits cell wall binding peptidoglycan formation by binding D-ala percursors, is bacterialcidal; G+ only, especially for multidrug resistant onces;NOT - nephrotoxicity, ototoxicity, thrombophlebitis, red man syndrome. pharmacology micro
How is redman syndrome prevented in vancomycin use?
slow infusion and rate and antihistamines. pharmacology micro
How does vancomycin resistant occur?
amino acid change of D-ala D-ala to D-ala D-lac. pharmacology micro
List antibiotic protein synthesis inhibitors
AT 30, CCEL at 50. 30S = Aminoglycosides, Tetracyclines. 50S = Chloramphenicol, Clindamycin, Erythromycin, Linezolid. pharmacology micro
Gentamicin, neomycin, amikacin,tobramycin,streptomycin(mechanism,use,toxicity)
aminoglycosides, bacterialcidal, block translocation but require oxygen for uptake;ineffective in anaerobes,use in gram - rod infections and before bowel surgery; nephrotoxicty, NMJ block, ototoxicity, teratogen. pharmacology micro
how does resistenace to aminoglycosides occur?
transferase enzymes that inactivate the drug by acetylation, phosphorylation, or adenylation. pharmacology micro
tetracycline, doxycycline, demecycline,minocycline(mechanism, use, toxicity)
bacteriostatic, prevents aminoacyl-tRNA binds;Borrela, M. Pneuomo, Rickettsia, Chlamysia; can't take with milk, antacids, iron because ions bind it, GI distress, discoloration of teeth, inhibition of bone growth, contraindication in pregnancy. pharmacology micro
how does resistance to tetracyclines occur?
decrease uptake into cells or increased efflux by pumps. pharmacology micro
Azithromycin, clarithromycin, erythromycin(mechanism,use,toxicity)
bacteriostatic, blocks translocation; atypical pneumonias, chlamydia, gram + cocci; MACRO: increased Motility, arrhythmia, Cholestatic hepatitis, Rash, eOsinophilia. pharmacology micro
how does resitance to macrolides occur?
methylation of 23s rRNA binding site. pharmacology micro
Bacterialstatic, blocks peptidlytransferase; Meningitis in adults, used in power countries due to being cheap; dose dependent anemia, dose independent aplastic anemia, gray baby syndrome. pharmacology micro
what causes grey baby syndrome?
use of chloramphenicol in premature infants, they lack UDO-glucuronyl-transferase. pharmacology micro
How does resistance to chloramphenicol occur?
plasmid-encoded acetyltransferase. pharmacology micro
Bacteriostatic. Blocks peptide transfer; anaerobic infections in lung infections and oral anerobes; C. Diff infection, fever, diarrhea. pharmacology micro
Sulfamethoxazole(SMX), sulfisoxazole, sulfadiazine(mechanism, use, toxicity)
Bacteriostatic, PABA metabolites inhibit dihydropteroate synthase; Gram +, G-, Nocardia, Chlamydia, UTI; hypersensitivty, hemolysis in G6PD, nephrotoxic, kernicterus, displaces other drugs from albumin. pharmacology micro
how does resistance to sulfonamides occur?
altered bacterial dihydropteroate or increased PABA synthesis. pharmacology micro
Bacteriostatic, inhibits bacterial dihydrofolate reductase, blocks folate synthesis; used in UTI, PCP (prophylacis and treatment), shigella, salmonella; megaloblastic anemia, leukopenia, granulocytopenia. pharmacology micro
ciprofloxacin, norfloxacin, levofloxacin, etc...(mechanism, use, toxicity)
bactericidal, inhibits DNA gyrase(topo II and IV);G- rods of urinary and GI tracts, Neisseria, some G+;( lones hurt the bones) tenonitis and tendon rupture, superinfections, don't give to kids or pregnant women due to cartilage damage. pharmacology micro
how does resistance to fluroquinolones occur?
mutation in DNA gyrase or efflux pumps. pharmacology micro
What groups are susceptible to fluorquinolone tendon rupture?
older than 60 or taking prednisone pharmacology micro
Metronidazole(mechanism, use, toxicity)
bacterialcidal, forms free radical toxic metabolites that damge bacterial DNA damage; (GET GAP) Giardia, Entamoeba, trichomonas, Gardnerella, Anaerobes, Pylori; causes disulfiram like reaction, headache, metallic taste. pharmacology micro
decrease synthesis of mycolic acids, bacterial catalase peroxidase(KatG) must activate INH; TB drug, only one used as prophylaxis and in latent TB; peripheral neuropathy, hepatoxic, lupis like drug interaction, pyridoxine antagonist. pharmacology micro
inhibits DNA-dependent RNA polymerase; TB, Leprosy, prophylaxis in meningococcus and Hib type B; hepatotox, p450 inducer, orange body fluids. pharmacology micro
Pyrazinamide(mechanism, use, toxicity)
unknown; TB; hyperuricemia, hepatotoxic. pharmacology micro
decreased carbohydrate polymerization of TB cell wall, blocks arabinosyltransferase; TB; optic neuropathy(red-green color blindness_ pharmacology micro
Amphotericin B(mechanism, use, toxicity)
binds fungal ergosterol, causes holes in membranes; use in systemtic and CNS mycoses infections; fever/chills, hypotension, arrythmias, nephrotoxic, IV phlebitis, must supplement K and MG. pharmacology micro
binds fungal ergosterol;topical only due to high toxicity, used for oral thrush and topical diaper rash or vaginal candidiasis. pharmacology micro
Fluconazole, ketoconazole, clotrimazole, itraconazole, voriconazole(mechanism, use,toxicity)
inhibits fungal ergosterol synthesis by binding p450;Fluconazole for suppression of cryptococcus in AIDs patients, itraconazle for blasto, coccio, histo. pharmacology micro
Flucytosine(mechanism, use, toxicity)
inhibits fungal DNA and RNA synthesis by conversion to 5FU; used in systemic fungal infections, especially cryptococcus; bone marrow suppression. pharmacology micro
Caspofungin, micafungin(mechanism, use, toxicity)
inhibits fungal cell wall synthesis by inhibiting B-glucan synthesis; invasive aspergillosis, candida; flushing via histamine releae. pharmacology micro
inhibits fungal squalene epoxidase; treat dermatophytes - toe nail infection especially;abnormal LFT, visual disturbances. pharmacology micro
interferes with microtubules, stops mitosis in fungi;deposits in keratin so used in superficial infections, stops dermatophytes; teratogenic, carcinogenic, confusion, p450 inducer. pharmacology micro
toxoplasmosis pharmacology micro
suramin and melarsoprol use
trypanosoma brucei pharmacology micro
trypanosoma cruzi pharmacology micro
sodium stibogluconate use
leshmaniasis pharmacology micro
blocks formation of heme into hemozoin. Heme accumulates and is toxic to plasmodia;used on all species but falciparum(too much resitance); retinopathy pharmacology micro
lifethreatening malaria pharmacology micro
p. falciparum killing pharmacology micro
inihibits influenza neuraminidase, stops progeny release; treamt of influenze a and b pharmacology micro
inhibits sythesis of guanine nucleotides by competitvely inhibiting IMP dehydrogenase; RSV, chronic hep C; hemolytic anemia, severe teratogen pharmacology micro
Acyclovir,valacyclovir(mechanism, use, toxicity)
Guanosine analog, inhibits viral DNA polymerase; monophosphorylated by thymidine kinase in HSV/VZV so active in lesions and encephalitis, good for prophylaxis, pharmacology micro
used in herpes zoster active infections pharmacology micro
mechanism for resistance to acyclovir
mutated viral thymidine kinase pharmacology micro
guanosine analog, 5'-monophosphate formed by CMV viral kinase, inhibits viral DNA polymerase;CMV infections;leukopenia,neutopenia,thrombocytopenia,renal toxicity pharmacology micro
mechanism for resistance to acyclovir
mutated CMV DNA polymerase or lack of viral kinase pharmacology micro
viral DNA polymerase inhibitor, binds to pyrofosphate binding site, doesn't need viral kinase activation;CMV retinitis when ganciclovir fails and acyclovir restitant HSV; nephrotoxic pharmacology micro
mechanism for resistance to foscarnet
mutated DNA polymerase pharmacology micro
inhibits DNA polymerase, doesn't require activiation by viral kinase; CMV retenitis, acyclovir resistant HSV; nephrotoxic pharmacology micro
HAART consist of what?
[2 NRTI] +[1 NNRTI OR 1 protease inhibitor OR 1 integrase inhibitor] pharmacology micro
give mechanism and toxicity of protease inhibitors
all end in -NAVIR! stops HIV mRNA cleavage into functional parts; hyperglycemia, GI upset, lipodystrophy. pharmacology micro
Ritonavir does what to be a "booster"
inhibits cytochrome p-450, boosting concentration of other drugs. pharmacology micro
Tenofovir, emtricitabine, abacavir, lamivudine, zidovudine, didansoine, stavudine(mechanism,use,toxicity
(NRTI)competitively blocks binding of nucleotide to reverse transcriptase, only tenofovir doesn't need to be activated;all NRTIs, zidovidine used in pregnancy to reduce fetal transmision; bone marrow suppression, lactic acidosis, peripheral neuropathy. pharmacology micro
Nevirapine, Efavirenz, Delavirdine(mechanism,use,toxicity)
(NNRTI) bind at a site different from NRTIs, no don't require activation don't compete with nucleotides; bonow marrow suppression, peripheral neuropathy, lactic acidosis, pharmacology micro
inhibits integrase, which stops HIV integration into host cells;HIV;hypercholesterolemia pharmacology micro
glycoproteins synthesized my virus infected cells, block RNA and DNA virus replication; INFa- chronic hep b and c, Kaposi sarcoma, IFN-b -MS, INF-gamma -NADPH oxidase defiency; neutropenia, myopathy. pharmacology micro
What antibiotics must be avoided in pregnancy?
SAFe Children Take Really Good Care. sulfonamides(kericterus), aminoglycosides(ototox), fluoroquinolones(cartilage damage), Clarithromycin(embryotoxic), Tetracycline(teeth,bone damage),Ribavarin(teratogenic),Griseofulvin(teratogenic),Chloramphenicol(grey baby) pharmacology micro