Term
|
Definition
| Gram positive and negative plus Rickettsia, Mycoplasma and Chlamydiae. Not used too much though. Other drugs are better. |
|
|
Term
| Mechanism of Tetracyclines |
|
Definition
| Binds 30S ribosome. Blocks amino-acyl-tRNA binding. |
|
|
Term
| Absorption of tetracyclines |
|
Definition
| Incomplete except for doxycycline and minocycline. Dairy and divalent cations chelate and prevent absorption (except doxy and mino). |
|
|
Term
| Distribution of tetracyclines |
|
Definition
| Widely distributed, BBB, placenta etc.. Minocylcine is very lipophilic and can have sufficient concentration in saliva/tears to treat meningococcal carrier states. |
|
|
Term
| Tetracycline side effects |
|
Definition
Gastrointestinal(most frequent)
Superinfections(Candida, staph, C. diff, esp in diabetics, leukemia or SLE)
Phototoxicity(esp w doxy and demeclocycline)
Bone defects (esp children, contraindicated in pregnancy)
Hepatotoxicity(pregno, liver diseased)
Renal Toxicity(Fanconi syndrome=prox tubule)
Vestibular toxicity(minocycline) |
|
|
Term
|
Definition
Bacteroides fragilis and amp resistant H. influ/CNS anaerobes and life threatening meningitis.
Gram + and -, Rickettsia, mycoplasma and Chlamydiae. |
|
|
Term
| Chloramphenicol mechanism |
|
Definition
| Inhibits protein synthesis by binding 50S. Bacterial static except for highly susceptible strains of H. flu, N.men, and Strep. p. |
|
|
Term
| Chloramphenicol Therapeutic uses |
|
Definition
1. Life threatening meningitis
2. Severe CNS Bacteroides
3. Alternate to tetracyclines for Rickettsial and brucellosis |
|
|
Term
| Absorption and distribution of Chloramphenicol |
|
Definition
| Rapid oral absorption and high distribution(lipophilic, crosses BBB placenta, CSF) |
|
|
Term
| Chloramphenicol excretion. |
|
Definition
| inactivated by liver glucuronyl transferase(90%) some active drug is excreted VIA urine. |
|
|
Term
| Adverse effects of Chloramphenicol |
|
Definition
Dose related anemia/bone marrow suppression.
Aplastic irreversible anemia (often fatal)
Gray Baby Syndrome |
|
|
Term
|
Definition
|
|
Term
| Aminoglycosides chemistry and mechanism |
|
Definition
Basic cations can react w acidic penicillins and deactivate each other.
Binds 30S ribosome and causes mRNA misreads. Bad proteins can insert into membrane and destroy membrane integrity. |
|
|
Term
|
Definition
| Severe aerobic gram (-) nosocomial infections. Ineffective against anaerobes. |
|
|
Term
| Aminoglycosides 3 mechanisms of resistance |
|
Definition
1. Inactivation by plasmid-mediated enzymes that acetylate, phosporylate or adenylate(Amikacin is less susceptible)
2. Alteration of transport system (energy and oxygen dependent)
3. Mutation in Ribosome that binds drug |
|
|
Term
| Aminoglycosides absorption and distribution |
|
Definition
| Poor absorption and only 20% distribution, does not enter CSF or cross placenta |
|
|
Term
| Excretion of Aminoglycosides |
|
Definition
| Glomerular filtration. Elderly, neonates and renally compromised are at risk for toxicity. |
|
|
Term
| Aminoglycosides adverse effects |
|
Definition
1. Neurotoxicity: irreversible damage to hair cells in cochlea and vestibule
2. Nephrotoxicity: (proximal tubule) inhibits phospholipases in lysosomes which burst and release hydrolases into the cytoplasm
3. Neuromuscular blockade: respiratory depression(myasthenia gravis and hypoglycemic are susceptible) Antidote: Calcium gluconate or neostigmine |
|
|
Term
| Drug interactions of Aminoglycosides |
|
Definition
| Penicillins, nephrotoxic drugs(diuretics, cisplatin, cyclosporine, amphotericin B, and Vancomycin). |
|
|
Term
| What combinations are used against Psuedomonas and some gram (-) nifections |
|
Definition
| Aminoglycosides and either penicillin or cephalosporins. |
|
|
Term
| Aminoglycoside prototypes |
|
Definition
Gentamicin (systemically)
Amikacin (systemically)
Neomycin (topical or oral prior to surgery)
Streptomycin (used for TB) |
|
|
Term
|
Definition
tetracycline
doxycycline
minocycline
tigecycline |
|
|
Term
|
Definition
| Inhibits protein synthesis by binding 50S ribosome. Only bacteriostatic. |
|
|
Term
| Therapeutic uses of Macrolides |
|
Definition
1. Common strep URI
2. H. infl otitis media
3. Pneumonias due to Chlamyophillia, mycoplasma and legionella
4. Bordetella (whooping cough, chronic bronchitis, sinusitus.)
5. H. pylori (clarithromycin)
6. Mycobacterium avium in AIDS patients (Clar/azith)
7. Diptheria carriers |
|
|
Term
|
Definition
1. Decreased drug penetration through cell envelope
2. Methylation of ribosome target
3. Hydrolysis of drug (enteric gram (-))
4. Ribosome mutation |
|
|
Term
|
Definition
erythromycin-acid labile
Clarithromycin-acid stable take w food
Azithromycin-acid stable |
|
|
Term
|
Definition
Good into tissue but not CSF.
Azithromycin concentrates in Phagocytes, macrophages and fibroblasts |
|
|
Term
|
Definition
E: CYP3A metabolism
A: unchanged in feces t1/2 = 68hrs
C: 30% in urine, remainder in feces
D: t1/2 = 30-44 hrs |
|
|
Term
| Macrolides adverse effects |
|
Definition
| E: GI upset, ototoxicity, and hepatotoxicity w estolate ester |
|
|
Term
| Drug interactions of Macrolides |
|
Definition
E and C: inhibit CYP3A4 which can cause build up of carbamazepime, glucocorticoids, cyclosporin, digoxin, theophylline, triazolam, valproate and warfarin.
E: Cardiac arrhythmias and QT prolongation |
|
|
Term
|
Definition
Erythromycin
Clarithromycin
Azithromycin
telithromycin |
|
|
Term
| Sulfonamides are only effective against what kind of microorginisms |
|
Definition
| Those that require PABA to synthesize folic acid. |
|
|
Term
| Sulfonamides mechanism of action |
|
Definition
Competively inhibits dihydropteroate synthase, can serve as an alternate substrate causing inactive produts.
Bacteriostatic |
|
|
Term
| Mechanism of trimethoprim |
|
Definition
| Blocks dihydrofolate reductase |
|
|
Term
|
Definition
1. Oral sulfamide of choice
2. High water solubility
3. can be combined with erythromycin to treat otitis media or URI's |
|
|
Term
|
Definition
| High CSF levels, therapeutic within 4 hrs, t1/2=10 hrs, problems with crystalluria |
|
|
Term
|
Definition
| Similar to sulfasoxazole, longer t 1/2 = 11 hrs due to slower absorption/excretion. More likely to cause crystaluria |
|
|
Term
|
Definition
| Synergistic effect. Net result makes it bacteriocidal. |
|
|
Term
|
Definition
| Prodrug, Poorly absorbed, broken down into sulfapyridine(active) and mesalamine(COX inhibitor). Treats IBD, ulcerative colitis, and regional enteritis. Absorption of high doses of sulfapyridine can be toxic |
|
|
Term
|
Definition
| Topical, drug of choice for 2nd and 3rd degree burns. Can cause photosensitivity. Preferred over mafenide. |
|
|
Term
|
Definition
| Ophthlamic topical, treats Chlamydia trachomatis |
|
|
Term
| sulfadoxine-pyramethamine |
|
Definition
| Pyramethamine is similar to TMP in action, sometimes prescribed for parasites |
|
|
Term
|
Definition
| Highly selective for bacterial dihydrofalate reductase |
|
|
Term
|
Definition
| rapid except sulfasalizine |
|
|
Term
| Sulfonamides distribution |
|
Definition
| widely distributed, crosses placenta and can be toxic |
|
|
Term
| Sulfonamides metabolism and excretion |
|
Definition
| Acetylated in liver excreted by glomerular filtration, so renal function is required |
|
|
Term
| Sulfonamides adverse effects |
|
Definition
1. UTI(crystalluria)
2. Hypersensitivity(rash, erythema multiforme, drug fevers, PT)
3. Hematopoetic (rare, bloody dyscrasias, anemia, contraindicated w porphyria patients)
4. Kernicterus (bilirubin displced from albumin in neonates, also passes in breast milk) |
|
|
Term
| Sulfonamides drug interactions |
|
Definition
| Displaces drugs from albumin. Including Sulfonylurea, hypoglycemic drugs, anticoagulants, phenytoin and methotrexate. |
|
|
Term
| TMP-SMX sensitive organisms |
|
Definition
1. Gram (-) bacilli
2. Actinomyces, Nocardia
3. Three parasites (AIDs patients) Cyclospora, Isospora, Toxoplasma.
4. One fungus: Pnuemocystis jiroveci
5. Back up drug for 24 others |
|
|
Term
|
Definition
1. Oral Rx for UTI
2. MRSA backup
3. Pneumocystis in AIDs patients
4. URI due to H. flu Strep. P.
5. GI infections (Shigella, Salm., EHEC may increase HUS though) |
|
|
Term
|
Definition
|
|
Term
|
Definition
1. Hypersensitivity (fever, rash, etc)
2. CNS effects (headache, depression and hallucination)
3. Contraindicated in renal disease
4. Megaloblastic anemia in folate deficient patients. |
|
|
Term
|
Definition
| Prodrug, decomposes to formaldehyde and ammonia in acidic conditions. Used for chronic cystitis. |
|
|
Term
|
Definition
1. GI (take with food)
2. Contraindicated with renal or liver disfunction
3. Rashes, hematuria, almbuminuria, and painful/frequent micturition
4. Formaldehyde forms precipitates with sulfamethizole
5. Don't use with drugs that Alkanize urine |
|
|
Term
| What bacteria can alkalize urine |
|
Definition
| Proteus and Pseudomonas can split urea thus alkalizing urine |
|
|
Term
|
Definition
| Reduced by bacteria to products that mediate cell damage. Static at low, cidal at high, needs acidic urine |
|
|
Term
| Nitrofurantoin resistant bacteria |
|
Definition
| Klebsiella, enterobacter and those that alkalize urine (Proteus and Psuedomonas) |
|
|
Term
| Nitrofurantoin absorption and excretion |
|
Definition
| Rapidly absorped and excreted. never reaches high plasma levels, don't give with probenecid due to toxicicity. |
|
|
Term
| What UTI drugs should never be mixed |
|
Definition
| Any methenamine + Any sulfa ▬► An insoluble ppt |
|
|
Term
| Which UTI drug is given with an organic acid? When is this contraindicated? |
|
Definition
| Methenamine, renally impaired. |
|
|
Term
| Nitrofurantoin Toxicities |
|
Definition
GI irritation – common N/V.
Pulmonary and hepatic |
|
|
Term
| Nitrofurantoin Toxicities |
|
Definition
| Turns Urine brown, contraindicated in pregnancy and with decreased renal function. Can have sensory/nueral problems in which case the drug is discontinued. |
|
|
Term
|
Definition
| Blocks cell wall synthesis by inactivating bacterial enolpyruvyl transferase. Single dose adequate for Cystitis, Effective against many enteric gram (-) organisms but *not useful against Pseudomonas |
|
|
Term
|
Definition
| An analgesic for symptomatic relief of UTI pain |
|
|
Term
| Fluoroquinolone’s Mechanism of Action |
|
Definition
They target two enzymes needed for replication of double-stranded DNA:
DNA gyrase (Topoisomerase II)
Topoisomerase IV |
|
|
Term
| Fluoroquinolones spectrum and limitations |
|
Definition
Wide spectrum of both Gram + and -.
Limitations:
*Spirochetes are completely resistant
*Anaerobes are mostly resistant: only moderately sensitive to moxifloxacin
*Penicillin-resistant Strep. pneumoniae are mostly resistant
*Resistance is increasing in Staph. aureus and is frequent in MRSA
*Neisseria gonorrhoeae is now likely to be resistant. |
|
|
Term
| Therapeutic Uses of Fluoroquinolones |
|
Definition
*Cipro is #1 for UTIs due to Pseudomonas
*Cipro & levofloxacin are drugs of choice for uncomplicated pyelonephritis
*They are backups to TMP-SMX for commonly occurring uncomplicated cystitis; Bactrim is preferred to minimize development of resistance to FQs. |
|
|
Term
| What drug would be used to treat prostatitis |
|
Definition
|
|
Term
| What drugs are used to treat travelers diarrhea |
|
Definition
*Cipro or Levaquin are good & preferred to TMP-SMX in adults
*Azithromycin (the FQ backup) is preferred in India, Thailand where Campylobacter is resistant to FQs.
*Bactrim is preferred for TD in kids |
|
|
Term
| Prophylaxis after exposure to meningococcus or anthrax |
|
Definition
|
|
Term
| Toxicities of the Fluoroquinolones |
|
Definition
CNS agitation
*Responses range from headache to seizures (1-10%)
*Inhibits by displacing GABA from CNS receptors.
*Agitation more common in elderly patients.
*Insomnia occurs more often in young children*Prolongation of the QT Interval in the heart*FQs contraindicated in pregnant, nursing mothers & children |
|
|
Term
| First generation FQs to know |
|
Definition
| Ciprofloxacin, lomefloxacin |
|
|
Term
| Second generation FQ's to know |
|
Definition
| Gemifloxacin, Levofloxacin, Moxifloxacin |
|
|
Term
| Drug Interactions with FQs |
|
Definition
**FQs are very well absorbed (70-100%) in the absence of multivalent cations.
**Antacids, iron, multivitamins, sucralfate (Al), or didanosine (Al, Mg) chelate FQs & decrease bioavailability by up to 90%; must be staggered in dosing by 2+ hr |
|
|
Term
|
Definition
6-month course of treatment that involves 4 drugs for the first 2 months (isoniazid, rifampin, ethambutol, and pyrazinamide),
Followed by isoniazid and rifampin for the remaining 4 months.
Rifampin in combination with isoniazid for 9 months also is effective therapy for strains susceptible to both agents |
|
|
Term
|
Definition
| TB, primary drug in all regimens, also prophylaxis |
|
|
Term
|
Definition
| excellent tuberculcidal drug, most rapid acting, useful for other bacterial infections |
|
|
Term
| What drugs are used when there is resistance to first line TB drugs |
|
Definition
| Pyrazinamide and Streptomycin |
|
|
Term
| Clinical problems with TB drugs |
|
Definition
Isoniazid (peripheral neuritis, hepatitis)
Rifampin (hepatic toxicity, GI effects, red-orange urine and tears, flu-like symptoms)
Ethambutol (altered visual acuity and impaired ability to peceive green)
Pyrazinamide (hepatic necrosis, precipitate gout)
Streptomycin (ototoxicity, vestibular toxicity, and nephrotoxicity |
|
|
Term
| Adverse effects of Clindamycin |
|
Definition
Diarrhea* (8%)
potential antibiotic associated colitis (overgrowth of C. difficile)
skin rashes* (10%)
Thrombophlebitis* with IV admin. |
|
|
Term
| Adverse effects of Vancomycin |
|
Definition
Nephrotoxicity*
Ototoxicity* (reversible)
Thrombophlebitis*
Red man syndrome |
|
|
Term
| Adverse effects of metronidazole |
|
Definition
frequent GI disturbances* and metallic taste
Neurotoxicity* (dizziness and vertigo)
blood dyscrasias* or neutropenia |
|
|
Term
|
Definition
| Topical, used vs. gram positive cocci |
|
|
Term
|
Definition
used vs. aerobic gram-neg. bacilli
Topical treatment of infections of skin, mucous membranes, eye and ear |
|
|
Term
| Which drug is limited by crystalluria and should be taken with lots of water and bicarbonate. Urine should be >1200 ml per day |
|
Definition
|
|
Term
|
Definition
ras, EGF receptor, PDGF receptor, BRAF, kit, and abl.
There is a specific treatment imatinib (Gleevec) for kit and abl. |
|
|
