Beruflich Dokumente
Kultur Dokumente
to Vancomycin
formation G+
Clinical Uses
Route: IV or IM Multi-drug resistant Staph Route: Topical
Adverse Eff.
Nephrotoxicity Hearing Loss Nephrotoxicity
Absorption
Not well absorbed in GI or CSF Not well absorbed in GI Not well absorbed in GI Poor stability in acid
Termination
Renal Excretion
Resistance
Yes
Notes
Quinopristin/Dalfopristin & Linozolid is used if microbe is vanco resistant more later
Narrow-some G+
-lactamasepenicillinase sensitive
Penicillin V Penicillin H Phenoxymethyl Penicillin Amoxicillin + Clavulanic Acid (Augmentin) Pipercillin + Tazobactam Ticarcillin Cephalosporins -lactam 1st-Cephalexin Inhibits peptidoglycan (via 1st-Cephazolin cross-linkage transpepdidase) nd 2 -Cefaclor 3rd-Cefotaxim 3rd-Cefixime 4th-Cefepime Carbapenem -lactam Imipenem + Inhibits peptidoglycan (via Cilastatin cross-linkage transpepdidase Meropenem Ertapenem Monobactams -lactam Aztreonam Inhibits peptidoglycan
cross-linkage (via transpepdidase More broad than penicillin: 1st generation is narrow for G-, broad for G+ 4th generation is most broad for G- & narrow for G+ More broad than both penicillins & cephalosporins
Penicillinase sensitive Clavulanic Acid:Irreversibl e inhibition of penicillinase Tazobactam: Irreversible inhibition of penicillinase Renal Excretion Augmentin XR is higher dose that is effective against amoxicillin resistant microbes
Broad-G- bacilli
Route: IM
Not well absorbed in GI Not well absorbed in GI Nephrotoxicity ( if combined w/ aminoglycoside) GI upset Nausea Anemia (reversible) Allergy (5%)
Route: IV or IM
Route: Oral Route: IM or IV Route: Oral Route: IM Route: Oral Route: IV or IM Route: IV or IM
Route: IV or IM
Cell Membrane Drugs (Antifungal & Bactericidal) Drug Name Mechanism Spectrum Fungicidal Broad:GPolymyxin
Detergent effect
Clinical Uses
Route: IV or IM
Adverse Eff.
Nephrotoxic
Absorption
Not well absorbed in GI
Termination
Renal Excretion
Resistance
Notes
Doesnt require active replication Can be given w/ Bacteristatic drug
Nystatin Amphotericin B
Fungicidal polyene Disrupts sterol site in membrane Fungicidal polyene Disrupts sterol site in membrane
Route: Topical Route: IV or IM Deep fungal infect. Only in hospitals where renal fn can be monitored
Fungicidal Inhibits synthesis of sterols in membrane Route: IV or IM (can be oral) Fungal menigitis Route: Topical Fungicidal Binds to skin hair and nails Route: Topical Mild GI upset & hepatotoxicity (reversible) Mild GI upset & hepatotoxicity (reversible) Not well absorbed in GI Distributes to CSF
Nucleic Acid Synthesis Inhibitors (Bactericidal) Drug Name Mechanism Spectrum Fluroquinolones Broad:G+ & GCiprofloxacin Inhibit bacilli, some Levofloxacin topoisomerase (prokaryotic enzyme) mycobacteria Rifampin
RNA Synthesis Narrow:G+, few G(like Pen G except no spirochetes)
Clinical Uses
Route: Oral
Adverse Eff.
Dizziness, seizures Mild GI upset cartilage formation (kids) Mild GI upset Orange secretions Mild GI upset Headache Pulmonary Fibrosis (rare)
Absorption
Well absorbed in GI
Termination
Metabolized by liver Renal excretion
Resistance
Notes
Route: Oral
Nitrofurantoin
UTI
Protein Synthesis Inhibitors (Bacteriostatic) Drug Name Mechanism Spectrum Aminoglycosides Broad:G- bacilli Gentamycin Binds to receptor on Amikacin Tobramycin Netilmycin Tetracyclines Tetracycline Oxytetracycline Minocycline Doxycycline Chloramphenicol
Binds 50S subunit & inhibits peptide bond form. Binds to receptor on 30S Subunit Blocks amino-acyltransfer RNA 30S Subunit (bacteriostatic) Causes misread (bactericidal) (main) + TB Broader Broader except w/TB Broadest (last resort)
Clinical Uses
Route: IV or IM
Adverse Eff.
Irreversible effect on vestibular fn
Absorption
Not well absorbed in GI
Termination
Renal Excretion
Resistance
Rapid and common
Notes
Old drug w/ much resistance
Extremely Broad: G+, G-, actinomycetes, Rickettsia, Chlamydia, E. Histolytica, esp. Mycoplasma (TB) Broad: G+, G-, Rickettsia
Route: Oral, IV, IM Route: Oral, IV, IM For young children Route: Oral only E. Histolytica Route: Oral only E. Histolytica Route: Oral
Allergy 5% Brown color on teeth Phototoxicity Opportunistic inf.ections: Broad spec. destroys normal flora Allergy Toxic Bone Marrow Suppression vs. Aplastic anemia Mild GI upset Newborn cardiac toxicity Mild hepatotoxicity
Macrolides Erythromycin
Broad: G+, some G-, esp. Mycoplasma (TB) (like Pen G) Slightly Broader G+, GSlightly Broader for GMainly G+, few G-
Route: Oral
Well absorbed in GI
Route: Oral
Allergy (5%) Colitis-type GI upset Mild Bone Marrow suppression Pain & Inflam. @ site of administration Joint & Muscle Pain GI upset Monitor bone marrow for thrombocytopeni
Liver Metabolism
Vancomycin resistant Drugs Quinupristin/ Binds 50S subunit & peptide bond Dalfopristin inhibits form. Linezolid
Binds 50S subunit & Blocks formation of 70S unit
Broad: Limited to G+ (staph, strep, enterococcus) Slightly Broader: Limited to G+ (staph, strep, enterococcus)
Route: IV
Liver Metabolism Biliary excretion Fecal excretion Liver Metabolism Renal excretion
Route: Oral
Well absorbed in GI
Anti-Metabolite Drugs (Reversible Competitive Antagonists) Drug Name Mechanism Spectrum Clinical Uses Sulfonamides (Sulfa Drugs) Narrow: G+, some Route: Oral Sulfisoxazole PABA Anologs Acetylsulfisoxazole Succinylsulfathiazole TrimethoprimSulfamethoxazole Flucocytosine
folic acid GUsed more often Route: liquid Oral for children
Adverse Eff.
Allergy Bone Marrow suppression CNS toxicity in newborns ( bilirubin)
Absorption
Well absorbed in GI Distributes in TBW & CSF
Termination
Renal excretion
Resistance
Notes
Soluble in urine GI Flora will activate by removing Acetyl group GI Flora will activate by removing Succinyl
Decrease GI Flora prior to surgery Inhibits DHFR & PABA Fungicidal Broader Route: Oral Recurrent UTIs Route: Oral
Distributes to CSF Bone Marrow suppression Mild GI upset Well absorbed in GI Distributed in TBW
Anti-Viral Drugs (non-retroviral) Drug Name Mechanism Anti-Herpes Drugs (non-retroviral) Acyclovir Guanosine
Spectrum
Narrow
Clinical Uses
Route: Topically
Adverse Eff.
Mild GI upset Mild Nephrotoxicity
Absorption
Well absorbed in GI Distributes in CSF Well absorbed in GI Distributes to CSF (not as well as Acyclovir Metabolized by kinases to triphosphate level Metabolized by kinases to triphosphate level Predrug is metabolized by GI flora to activate Distributes to CSF if inflame. meninges Little distributed to CSF Not well absorbed in GI Well tolerated
Termination
Renal Excretion
Resistance
Notes
Valacyclovir Ganciclovor
nucleotide analog DNA synthesis or alters structure & fn Predrug to Acyclovir Guanosine nucleotide analog DNA synthesis or alters structure & fn Thymidine analog DNA synthesis Adenosine analog Inhibits viral DNA polymerase
Idoxuridine
Bone Marrowanemia CNS-dizziness, headaches Teratogenic Too potent for mammalian cells
Vidarabine Adefovir/Dipivoxil
Narrow
Route: Oral Route: Oral Prophylactic & therapeutic Route: Inhalation of fine powder
Oseltamir Zanamivir
Anti-Viral Drugs (non-retroviral) Continued Drug Name Mechanism Spectrum -Interferon Inhibits viral DNA Lamivudine
polymerase
Clinical Uses
Hep B & C DNA Viruses & Hep B virus
Adverse Eff.
Absorption
Termination
Resistance
Notes
Non-nucleoside antiviral
Anti-Viral Drugs (retroviral) Drug Name Mechanism Spectrum Nucleoside reverse transcriptase inhibitors *Zidovudine (AZT) Thymadine analog is Viral specific (not
substrate for viral reverse transcriptase Purine analog is substrate for viral reverse transcriptase
Clinical Uses
Route: Oral
Adverse Eff.
GI upset Anemia GI upset Anemia
Absorption
Termination
Resistance
High rate of mutation in reverse transcriptase
Notes
-OH group stops transcription
*Didanosine
Non-Nucleoside reverse transcriptase inhibitors *Nevirapine *Efavirenz Protease Inhibitors Indinavir Inhibits viral
protease
*Use all three for Tx GI upset Nephotoxicity Hyperglycemia Diabetes Fat redistribution Hyperlipidemia
Very expensive$20,000/yr