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Heiman.pharm.abx
Antimicrobials
| Question | Answer |
|---|---|
| Gram Stain | Specimen dyed with crystal violet and iodine. Decolorized with alcohol. Then stained with safranin. First ID test done. |
| Gram Positive | Cells do not colorize with alcohol and appear purple under the microscope. Bacteria surrounded by a thick, rigid porous cell wall made of peptidoglycan. |
| Gram Negative | Cells decolorize with alcohol and take on red color when counterstained with safranin. Bacteria have an additional outer membrane composed of lipopolysaccharide located around the cytoplasmic membrane and the thin peptidoglycan layer. |
| WBC's | Defend the body against invading organisms. Normal 4,500-10,000 cells/mm. Increases in response to infection, stress, inflammatory conditions, leukemia, drugs. |
| Macrophage/Monocyte | Type of WBC. Antigen presenting cell. Surveillance of antigens. |
| Neutrophils | Type of WBC. Defense against bacteria and fungus. |
| Eosinophils | Type of WBC. Defense against parasite. Response against allergic reactions. |
| Basophils | Type of WBC. Allergic response |
| B Lymphocyte | Antibody production. May be see in acute viral infections. |
| Left shift | Ratio of immature to mature WBC's increases. (Neutrophils) |
| MECHANISMS OF ABX ACTION: Inhibition of cell wall synthesis | Most common mechanism of anti-bacterial action. Beta lactams; inhibit peptidoglycan synthesis. (eg. PCN's and cephalosporins. |
| MECHANISMS OF ABX ACTION: Inhibition of protein synthesis; 30S Ribosome site | 30S ribosome site; irreversible binding to 30S ribosome protein. eg. aminoglycosides. Block tRNA binding to 30S ribosomes-mRNA complex, eg. tetracyclines. |
| MECHANISMS OF ABX ACTION: Inhibition of protein synthesis; 50S Ribosome site | Binding to peptidyl transferease component of 50S ribosome blocking peptide elongation, eg. chloramphenicol. Reversible binding of 50S ribosome, eg. macrolides. Interference with binding of amino acid acyl tRNA complex, eg. Clindamycin. |
| MECHANISMS OF ABX ACTION: Alteration of cell membranes | Cationic detergent like activity, eg. Polymixins (topical). Disruption of cytoplasmic membranes, eg. bacitracin (topical). |
| MECHANISMS OF ABX ACTION: Inhibition of Nucleic Acid Synthesis; DNA Effects | Inhibition of DNA gyrases or topoisomerases needed for supercoiling of DNA, eg. quinolones. Metaboliz cytotoxic byproducts disrupt DNA, eg. Metronidazole...needs to be metabolized to active form by bacteria. |
| MECHANISMS OF ABX ACTION: Inhibition of Nucleic Acid Synthesis; RNA Effects (transcription) | Binding to DNA dependent RNA polymerase inhibiting initiation of RNA synthesis, eg. Rifampin. Inhibition of RNA transcription, eg. Bacitracin, topical. |
| MECHANISMS OF ABX ACTION: Antimetabolite Activity | Compete with para-aminobenzoic acid (PABA) preventing synthesis of folic acid, eg. sulfonamides & dapsone. Inhibit dihydrofolate reductase, trimethoprim. |
| Bacteriostatic Drugs | Decrease growth of the bacteria, immune system takes over from there; eg. tretracyclines, chloramphenicol, macrolides. |
| Bactericidal Drugs | Actually kill the organisms. These are better for immunocompromised. eg. beta lactams, aminoglycosides. |
| Intrinsic Resistance | When a bacteria has a built in resistance to an antibiotic. Gram negative bacteria with PCN resistance; outer membrane layer prohibits transport of PCN in to the cell. |
| Acquired resistance | Transfer of resistance from bacteria to bacteria; eg. plasmids, transposons. OR chromosomal mutation. |
| Types of Acquired Resistance | Development of an altered drug target. Decrease in the concentration of drug that reaches the receptor; decreased membrane permeability, drug efflux pumps, where the bacteria pumps out waste, which is sometimes the abx. |
| Types of Acquired Resistance cont'd | Enzyme inactivation of the drug; ie beta lactamase, or aminoglycoside. |
| PENICILLINS: Mechanism of action | Inhibition of peptidoglycan synthesis resulting in inhibition of cell wall synthesis. |
| PENICILLINS: Natural PCN's | Actually made from mold. Good for gram + cocci, gram + rods, spirochetes (syphillis). Limited gram negative coverage. Penicillin G; IV Both Na & K salts. Penicillin V; oral. |
| PENICILLINS: Beta Lactamase resistant penicillins | Good for beta lactamase producing staph. Examples: Nafcillin (Nafcil) Methicillin (Staphcillin) Oxacillin (Bactocill) Cloxacillin (Cloxapen) Dicloxacillin (Dyanapen) |
| PENICILLINS: Aminopenicillins | Add an amino group. Adds some gram negative coverage for organisms such as H. influenzae, E. coli, Proteus mirabilus. Decreased gram + coverage. Examples: Ampicillin, Amoxicillin |
| PENICILLINS: Beta Lactamase inhibitors | Direct inhibitor of beta-lactamase. Used in combination with penicillin to decrease breakdown by bacterial enzymes. |
| PENICILLINS: Beta Lactamase inhibitors Names | Clavulonic acid Amoxacillin/clavulanate (Augmentin) Ticarcillin/clavulanate (Timentin) Sulbactam Ampicillin/sulbactam (Unasyn) Tazobactam Piperacillin/tazolbactam (Zosyn) |
| PENICILLINS: Kinetics | Some are acid labile and cannot be given orally. Instead given IV. Widely distributed in body water. Excreted mostly unchanged in urine. |
| PENICILLINS: Adverse Effects | Hypersensitivity (Most common adverse effect). Neutropenia (Especially with beta-lactamase resistant drugs). Rash. GI upset. |
| PENICILLINS: Long scting | Penicillin procaine; Levels maintained for- 24 hours. Penicillin benzathine; Levels maintained for 10 days. Benzathine – Procaine combination. |
| CEPHALOSPORINS: Mechanism of Action | Identical to penicillins. Inhibition of cell wall synthesis. |
| CEPHALOSPORINS: Spectrum of Activity | First generation; Gram-positive cocci, Some gram-negative coverage, Some anaerobic coverage. Second generation;Increased gram-negative coverage. Third generation; Extended gram-negative coverage. (Broad spectrum) |
| CEPHALOSPORINS: First generation | Cephalothin (Keflin) Cefazolin (Ancef) Cephalexin (Keflex) Cefadroxil (Duricef) Cephradine (Velocef) |
| CEPHALOSPORINS: Second generation | Cefuroxime (Ceftin, Zinacef) Cefoxitin (Mefoxin) Cefaclor (Ceclor) Cefotetan (Cefotan) Cefprozil (Cefzil) Loracarbef (Lorabid) |
| CEPHALOSPORINS: Third generation | Ceftazidime (Fortaz) Ceftriaxone (Rocephin) Cefotaxime (Claforan) Ceftizoxime (Cefizox) Cefixime (Suprax) Ceftibuten (Cedax) Cefdinir (Omnicef) Cefditoren (Spectracef) Cefoperazone (Cefobid) Cefpodoxime (Vantin) Cefepime (Maxipime) |
| CEPHALOSPORINS: Kinetics | Widely distributed in body water. Third generation has good CSF penetration. Most excreted unchanged by kidney. Ceftriaxone excreted hepatically. |
| CEPHALOSPORINS: Adverse effects | Hypersensitivity. Cross-reactivity with penicillins is 5%. Thrombocytopenia. Rash. GI upset. |
| CARBAPENEMS: Mechanism of Action | Inhibits cell wall synthesis |
| CARBAPENEMS: Names | ALL IV: Imipenem/cilastatin (Primaxin) Ertapenem (Invanz) Meropenem (Merrem) Doripenem (Doribax) |
| CARBAPENEMS: Spectrum of Activity | Broad-spectrum; Gram-positive. Gram-negative. Anaerobic. Resitant to beta-lactamases; Meropenem = ertapenem > imipenem Commonly used for abd infections. |
| CARBAPENEMS: Kinetics | Imipenem Metabolized by enzyme found in kidney tubules; Given with cilastatin which inhibits this enzyme. Induces beta – lactamase Ertapenem; 85 – 95% protein bound No liver metabolism, beta lactamase (human, not bacterial). Excreted by kidney. |
| CARBAPENEMS: Kinetics cont'd | Meropenem: Little protein binding. No metabolism. Renally excreted. |
| CARBAPENEMS: Adverse effects | Cross-reactivity with penicillins. Rash. Seizures. Diarrhea. Nausea /vomiting. Edema. |
| Aztreonam: | Mechanism of action: Inhibits cell wall synthesis. Spectrum of activity. Gram-negatives. |
| Aztreonam: | Kinetics: Excreted renally. Adverse effects: No cross-reactivity with penicillins, so can give if allergic to PCN. |
| QUINOLONES: Mechanism of action | Inhibition of DNA gyrase which interferes with DNA supercoiling. |
| QUINOLONES: Spectrum of activity | Gram-positive, gram-negative, some anaerobes. |
| QUINOLONES: Kinetics | Extensive liver metabolism, lots of interactions. Renal excretion of metabolites. |
| QUINOLONES: Adverse effects | GI upset. Rash. Not to be given to children or in pregnancy. |
| QUINOLONES: Names | Ciprofloxacin (Cipro) Levofloxacin (Levaquin, Iquix) Ofloxacin (Floxin) Lomefloxacin (Maxaquin) Moxifloxacin (Avelox, Vigamox) Gatifloxacin (Tequin) Gemifloxacin (Factive) Norfloxacin (Noroxin) Trovafloxacin (Trovan) Besifloxacin (Besivance) |
| SULFONAMIDES: MEchanism of Action | Prevent synthesis of folic acid |
| SULFONAMIDES: Spectrum of activity | Gram-positive, gram-negative. |
| SULFONAMIDES: Kinetics | Good absorption. Highly plasma protein bound. Some liver metabolism. Renal excretion. |
| SULFONAMIDES: Adverse effects | Rash. GI distress. Renal toxicity. Stevens-Johnson. |
| SULFONAMIDES: Names | Sulfisoxazole/erythromycin (Pediazole) Sulfamethoxazole/trimethoprim (Bactrim, Septra) Sulfacetamide (Bleph-10) Ophthalmic Sulfadiazine |
| AMINOGLYCOSIDES: Mechanism of Action | Bind to 30S ribosome inhibiting protein synthesis |
| AMINOGLYCOSIDES: Spectrum of activity | Gram – negative aerobes |
| AMINOGLYCOSIDES: Kinetics | Not orally absorbed Excreted unchanged by kidney |
| AMINOGLYCOSIDES: Adverse effects | Adverse effects Renal toxicity Ototoxicity Rash Neuromuscular blockade |
| AMINOGLYCOSIDES: Names | Gentamicin Topical, IV, IM Tobramycin Topical, IV, IM Amikacin IV, IM Streptomycin IM Netilmicin Neomycin Oral, topical Paromycin (Humatin) Spectinomycin (Trobicin) |
| MACROLIDES: Mechanism of action | Bind to 50S ribosome interfering with protein synthesis |
| MACROLIDES: Spectrum of activity | Gram-positive, gram-negative, some anaerobes |
| MACROLIDES: Kinetics | Well absorbed. Highly protein bound. Metabolized in liver. |
| MACROLIDES: Adverse effects | GI upset Rash Hepatotoxicity |
| MACROLIDES: Names | Erythromycin Azithromycin (Zithromax) Clarithromycin (Biaxin) |
| TETRACYCLINES: Mechanism of action | Inhibition of protein synthesis |
| TETRACYCLINES: Spectrum of activity | Some gram positive Some gram negative Some anaerobes |
| TETRACYCLINES: Kinetics | Variable liver metabolism Renal excretion |
| TETRACYCLINES: Adverse effects | GI upset. Rash. Tooth discoloration. Photosensitivity. |
| TETRACYCLINES: Names | Tetracycline (Sumycin) Doxycyline (Vibramycin) Minocycline (Minocin) Demeclocyline (Declomycin) Tigecycline (Tygacil) Minocyline derivative – not a true tetracycline. Extended spectrum of activity. |
| METRONIDAZOLE (FLAGYL): Mechanism of action | Interacts with microbe DNA Causing loss of helical structure Results in DNA breakage and inhibition of protein synthesis |
| METRONIDAZOLE (FLAGYL): Spectrum of activity | Anaerobes Gram positive Gram negative Amoeba |
| METRONIDAZOLE (FLAGYL): Kinetics | Well absorbed orally Wide distribution Crosses BBB Crosses placenta Hepatically metabolized Excreted in urine |
| METRONIDAZOLE (FLAGYL): Adverse effects | Nausea Flushing Diarrhea Metallic taste Peripheral neuropathy Thromocytopenia |
| METRONIDAZOLE (FLAGYL): Drug Interactions | CYP450 May increase levels of Warfarin (Coumadin) Benzodiazepines Calcium channel blockers |
| METRONIDAZOLE (FLAGYL): Cautions | Do not ingest alcohol Disulfiram – like reaction Hepatic disease Renal disease |
| CLINDAMYCIN: Mechanism of action | Inhibition of protein synthesis by binding to the 50S ribosome |
| CLINDAMYCIN: Spectrum of activity | Gram – positives Anaerobes |
| CLINDAMYCIN: Kinetics | Good oral absorption Highly protein bound Liver metabolism |
| CLINDAMYCIN: Adverse effects | Adverse effects Rash GI upset C. diff colitis |
| VANCOMYCIN: Mechanism of Action | Inhibition of cell wall synthesis by disruption of peptidoglycan cross-linkage |
| VANCOMYCIN: Spectrum of activity | Gram – positives MRSA |
| VANCOMYCIN: Kinetics | Not absorbed orally Some protein binding Renally excreted |
| VANCOMYCIN: Adverse effects | Red-man syndrome May be related to histamine release Nephrotoxicity Rash |
| LINEZOLID (ZYVOX): Mechanism of action | Binds to 50s ribosome |
| LINEZOLID (ZYVOX): Spectrum of activity | Staph. and Strep. including MRSA, MRSE VRE |
| LINEZOLID (ZYVOX): Kinetics | Good oral absorption CYP metabolism Renal excretion |
| LINEZOLID (ZYVOX): Adverse effects | Diarrhea Rash Anemia |
| Quinupristin / Dalfopristin (Synercid): Mechanism of action | Inhibition of protein synthesis |
| Quinupristin / Dalfopristin (Synercid): Spectrum of activity | Gram – positives, including VRE |
| Quinupristin / Dalfopristin (Synercid): Kinetics | Not absorbed orally CYP metabolism Renal excretion |
| Quinupristin / Dalfopristin (Synercid): Adverse effects | Nausea Diarrhea Arthralgia |
| AZOLES: MEchanism of action | Inhibition of fungal cell membrane formation |
| AZOLES: Kinetics | Good oral absorption Liver metabolism Kidney excretion |
| AZOLES: Adverse effects | GI upset Liver enzyme elevation Topical – burning or stinging |
| AZOLES: Drug-drug interactions | CYP-450 enzymes |
| AZOLES: Names | Fluconazole (Diflucan) Ketoconazole (Nizoral) Itraconazole (Sporanox) Voriconazole (V - Fend) Clotrimazole (Mycelex) |
| NYSTATIN: | Mechanism of action: Increased cell membrane permeability Kinetics: Not orally absorbed Excreted unchanged in feces Adverse effects: Hypersensitivity Rash |
| TERBUINAFINE (Lamisil): | Mechanism of action: Decreased cell membrane synthesis Kinetics: CYP 450 metabolism Urinary excretion Adverse effects: Rash Diarrhea Anemia |
| AMPHOTERICIN: Mechanism of action | Disruption of fungal cell membrane |
| AMPHOTERICIN:Adverse effects | Chills, fever, myalgias, arthralgias Thrombophlebitis Renal toxicity Hypokalemia, hypomagnesemia |
| AMPHOTERICIN: | IV preparations only:Infuse over at least 2 hours. May need to pretreat with diphenhydramine, acetaminophen, ibuprofen, or hydrocortisone.Test dose used to detect patient who may have anaphylactic reaction to drug. Dose incr. daily until goal achieved. |
| FLUCYTOSINE (ANCOBON): Mechanism of Action | Interference with fungal DNA synthesis. Should not be used alone. |
| CASPOFUNGIN (CANCIDAS): Mechanism of action | Inhibition of fungal cell wall synthesis. No dosage adjustment needed in renal pts. |
| CASPOFUNGIN (CANCIDAS): ADverse effects | Elevated liver enzymes Rash, itching, facial swelling Pulmonary edema ARDS |
| ANTI-VIRALS: Anti – RNA Mechanism of Action | Blocks the un – coating of the virus. |
| ANTI-VIRALS: Anti – RNA Kinectics: | Oral absorption Protein bound Amantadine mostly eliminated unchanged by kidney Rimantadine has liver metabolism |
| ANTI-VIRALS: Anti – RNA Spectrum of Activity | Amantadine (Symmetrel) Influenza A only Rimantadine (Fluvadine) Influenza A and B |
| ANTI-VIRALS: Neuroaminidase Inhibitors Mechanism of Action | Selective inhibitor of influenza A and B virus neuraminidase Inhibits the release of newly formed virus from the surface of infected cells Works in both Influenza A and B |
| ANTI-VIRALS: Neuroaminidase Inhibitors Kinetics | Zanamivir (Relenza):Not orally absorbed,Little metabolism, Renal clearance,Given intranasally. Aseltamivir (Tamiflu): Good oral absorption, Extensive liver metabolism. |
| ANTI-VIRALS: Neuroaminidase Inhibitors Adverse Effects | Rash,GI Upset, Nausea, vomiting, Dizziness, Abnormal Liver Function Tests (Oseltamivir), Bronchospasm (Zanamivir). |
| ANTI-VIRALS: Inhibition of DNA synthesis Mechanism of Action | Competition with enzymes that are needed to make new DNA. This stops virus replication. |
| ANTI-VIRALS: Inhibition of DNA synthesis Kinetics | Metabolized to active drug, Some by virus, Renal excretion. |
| ANTI-VIRALS: Inhibition of DNA synthesis Adverse effects | Nausea/vomiting Rash Liver and kidney dysfunction Headache |
| ANTI-VIRALS: Inhibition of DNA synthesis Spectrum of Action | Herpes Simplex type I and II, Herpes Zoster, CMV, Ganciclovir. |
| ANTI-VIRALS: Inhibition of DNA synthesis Names | Acyclovir (Zovirax) Valacylovir (Valtrex) Famciclovir (Famvir) Penciclovir (Denavir) Ganciclovir (Cytovene) |
Created by:
DianaB
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