Chermotherapy....Antibiotics
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| Beta-Lactam Antibiotics | Penicillins
Cephalosporins
Carbaenems
Vancomycin, Telavancin, Aztreonam
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| PENICILLINS | beta-lactam anitbx that weakens the bacterial cell wall
causes bateria to take up excessive water and rupture
bactericidal-kills bacteria
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| Bactericidal | kills sensitive organisms
number of organisms decline rapidly
activation of host immune system not required
MOA: block an essential function of the organism
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| Bacteriostatis | inhibits growth of organism
number of organisms remain the same
activation of host immune system required
MOA: blocks function needed for growth but not survival
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| PENICILLIN G (Benzylpenicllin) | narrow spectrum
given parentally
tx gram-positive cocci
4-salts: potassium PCN-G, Procaine PCN-G, Benzathine PCN-G, Sodium PCN-G
not absorbed well
eliminated in kidney
AE: allergy
Drug int:aminoglycosides, probenecid
PCN V or VK = good oral absorp
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| Penicillinase-Resistant PCNs | NAFCILLIN, OXACILLIN, DICLOXACILLINhighly resistent to beta-lactamases
used against S. Aureus and S. Epidermis
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| Broad Spectrum PCNs (Aminopenicillins) | AMPICILLIN, AMOXICILLIN
tx gram-positive cocci and some gram-negative
AE-rash, diarrhea
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| Extended Spectrum PCNs (Antipseudomonal PCNs) | TICARCILLIN, PIPERACILLIN
used for P. aeruginosa
frequently combined with aminoglycoside to inc. killing of pseudomonal organism, DON'T mix in same solution
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| Cephalosporins-Beta Lactam antibx | most widely used antibxs
MOA: bind to PBP and inhibit cell wall synthesis
bactericidal
given parentally, some orally
AE: allergy, bleeding, thrombophlebitis
Drug Int: probenecid, alcohol, calcium
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| First Generation Cephalosporins | CEFADROXIL, CEPHALEXIN, CEFAZOLIN
mostly gram + organisms, some gram-
destroyed by beta-lactamases
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| Second Generation Cephalosporins | CEFACLOR, CEFPROXIL, CEFUROXIME, CEFOTETAN, CEFOXTIN
more gram + than 1st gen
not as sensitive to beta lactamases
used w/H. influenzae, klebsiella, pneumoncocci, and stahpylocci, OM, sinusitis, and resp tract infections
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| Third Generation Cephalosporins | CEFIXIME, CEFDINIR, CEFDITOREN, CEFPODOXIME, CEFIBUTEN, CEFTAZIDIME, CEFOTAXIME, CEFTRIAXONE
CSF penetration
more active against gram - and anaerobes,
highly resistent to beta lactamases
used for gram - meningitis, gonorrhea, pseudomonas, H. influenz
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| CEFTRIAXONE (Rocephin) | 3rd generation, liver metabolism (not kidney), causes bleeding
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| Fourth Generation Cephalosporins | CEFEPIME
CSF penetration
highest restistance to beta lactamase
highest activity against gram - bacteria and anaerobes
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| Fifth Generation Cephalosporins | CEFAROLINE (new)
effective against MRSA
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| Carbapenems | Beta-lactam antibx, weaken cell wall
broad spectrum
low toxicity-GI and hypersensitivity
can dec valporic acid levels = inc risk of seizures
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| Carbapenem Agents | IMIPENEM-given with cilstatin
MEROPENEM
ETRAPENEM
DORIPENEM-new for uncomplicated UTI, tx psedomonas
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| VANCOMYCIN | cell wall synthesis inhibitor
given IV, excreted in urine
used for severe infections...narrow spectrum (gram + bacteria), C.Diff, MRSA, staph epidermidis
AE: renal failure, ototoxicity (aminoglycosides will inc risk), RED MAN syndrome, thrombophlebitis
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| AZTREONAM | cell wall synthesis inhibitor
beta lactam antibx
narrow spectrum....only gram -
IV/IM
well tolerated
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| TELAVANCIN | lipoglycoprotein
binds to bacterial cell membran and disrupts fxn, inhibits cell wall synthesis
gram + bacteria only
IV, renal excretion
AE: Redman syndrome, prolong QT interval, avoid during preg
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| FOSFOMYCIN | cell wall synthesis inhibitor
disrupts synthesis of peptidoglycan polymer strands
Oral, excreted in urine and feces
single dose therapy for uncomplicated UTI, infections from E. coli or Enterococcus faecalis
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| Bateriostatic Inhibitors of Protein Synthesis: TETRACYCLINES | broad spectrum antibx, inhibit protein via 30S ribosome subunit, taken up by bacteria thru transport lacking in mammals
works on: Rickettsia, Chlamydia, Brucellosis, Cholera, Mycoplama pneurmoniae, lyme disease, anthrax, h. pylori
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| TETRACYCLINE (sumycin) | short-acting, eliminated by the kidney
food decreases oral absorption, low lipid solubility
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| DEMECLOCYCLINE | Intermediate-acting, eliminated by the kidney
food decreases abosorption, moderate lipid solubility
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| DOXYCLYCLINE, MINOCYCLINE | Long-acting, eliminated by the liver
food decreases oral absorption
MINOCYCLINE-food does not decrease oral absorption
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| Bateriostatic Inhibitors of Protein Synthesis: TETRACYCLINES uses | infections, acne, peptic ulcer disease (h. pylori), peridontal disease, prophylaxis for malaria
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| Bateriostatic Inhibitors of Protein Synthesis: TETRACYCLINES concerns | absorption: milk products, iron supplements, magnesium containing laxatives, and antiacids.....take 2hrs apart
AVOID in renal failure
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| Bateriostatic Inhibitors of Protein Synthesis: TETRACYCLINES adverse effects | N/V/D, discoloration to teeth, AVOID in preg., breast feeding, and children under 8 yrs,
suprainfection-overgrowth of drug resistent organisms especially C. Diff, can lead to CDAD, causing severe diarrhea,
hepatoxicity, renal toxicity, photosensitivity
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| Clostritidum Difficile-associated disease (CDAD) diarrhea | profuse watery diarrhea, abd pain, fever, leukocytosis
can be fatal
tx: vancomycin or metronidazole, fluid, electrolyte replacement
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| Macrolides | ERYTHROMYCIN, CLARITHROMYCIN, AZITHROMYCIN
broad spectrum antibx
inhibit protein synthesis at 50S ribosome
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| Macrolides:ERYTHROMYCIN | can be used if allergic to PCN
used for strep resp infections, drug of choice for Legionnaires disease, whooping cough, diptheria
effective for chlamydia and pneumonia
AE: GI, supra infection, cardiotoxicity,
drug int: can inhibit hepatic metabolism
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| Macrolides: CLARITHROYCIN | used for resp tract infections, mycobaterium avium complex, H. pylori
AE: GI, supra infection, caridotoxicity, can inhibit hepati metabolism = drug int
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| Macrolides: AZITHROMYCIN | used for resp tract infections, chancroid, OM, mycobacterium avium complex, C. trachoatis
AE: minimal GI and drug int.
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| Protein Synthesis Inhibitors: CLINDAMYCIN | broad spectrum
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| Protein Synthesis Inhibitors (oxazolidinones): LINEZOILID | new class
binds to 23S of 50S ribosomal subunit
uses: mulitdrug-resistant gram+ pathogens, VRE, healthcare assoc pneumonia caused by MRSA, comm acquired pnuemonia, strep pneumoniae, staph skin infections
AE: myelosuppression, MOA inhibition (risk of HT
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| Protein Synthesis Inhibitors (ketolides): TELETHROMYCIN | new class 50S ribosomal subunit inhbitor
more activity against Strep Pneumoniae, useful for macrolid/PCN-resistent Strep pneum
used for comm acquired pneumonia (CAP)
AE: hepatoxicity, GI, myasthenia gravis exacerbations, prolong QT,
drug int: CYP450
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| Protein Synthesis Inhibitors (streptogramins):DALFOPRISTIN/QUINUPRISTIN | new class, separately they are bacteriostatic, together = bactericial, safe if allergic to PCN
uses: VRE, MRSA, drug resistant Strep pneum
AE: hepatoxicity, inhibit liver drug metabolizing enzyme
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| Protein Synthesis Inhibitors: CHLORAMPHENICOL | broad spectrum
tx: samonell, H flu, niesseria, strep pneum, B. frag, rickettsiae, clamydiae
bacteriostatic but can be cidal in high concentration
uses: life threatening infections
AE: reversible bone marrow depression, fatal aplastic anemia, gray synd
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| Aminoglycosides: Bacterial Inhibitors of Protein synthesis | can cause serious injury to inner ear and kidney
narrow spectrum: gram - only
given parentally, does not cross BBB
excreted in kidney
AE: nephrotoxicity, ototoxicity, hypersensitiviy, neuromus blockade
given w/PCN to cover gram + and -
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| Aminoglycosides MOA | inhibit protein synthesis by:
binding to 30S subunit, premature termination of synthesis, production of abnormal proteins
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| Aminoglycoside Agents | GENTAMICIN, TOBRAMYCIN, AMIKACIN, KANAMYCIN, STREPTOMYCIN (used in TB), NEOMYCIN (topical), PAROMOMYCIN (for parasites, stays in GI tract)
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| GENTAMYCIN | aminoglycoside
used for serious infections cause by aerobic gram - bacilli (pseudomonas aeruginosa, E. Coli, klebsiella, Serratia, Proteus Mirabilis)
excreted in kidney
AE: nephrotoxicity, otoxicity
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| TOBRAMYCIN | similar to gentamycin except:
more active against pseudomonas aeruginosa
less active against Enterococci and Serratia
more epxensive
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| AMIKACIN | similar to gentamycin except:
broadest sprectrum against gram - bacteria
lowest incidence of resistance
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| Sulfonamides | broad spectrum antibx
analog of PABA
suppress bacterial growth by inhibiting folic acid synthesis
uses: UTI
AE: hypersensitivity (steven-johnson's syn, photosensitivity), hematolytic anemai with G6PD deficiency, Kernicterus (disposition of bilirubin i
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| Short-Acting Sulfonamide | SULFISOXZOLE-only available in combo w/erythromycin
SULFADIAZINE- prophylaxis for meningitis
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| Intermediate-Acting Sulfonamide | SULFMETHOXAZOLE-only available in combo w/trimethoprim
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| Topical Sulfonamide | SULFACETAMIDE-eye infections
SILVER SULFADIAZINE- infections after burns
MAFENIDE-infections after burns
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| TRIMETHOPRIM | suppress synthesis of tetrahydrofolic acid
inhibits dihydrofolate reductase
uses: UTI, used in combo
AE: hematologic effects in pts w/folic acid deficiency, hyperkalemia, AVOID in preg and lactation
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| TRIMETHOPRIM-SULFAMETHOXAZOLE(bactrim) | fixed dose combo, broad spectrum
uses: UTI, pneumonia, GI infections, OM, shigellosis, bronchitis
AE: GI, rash, hypersensitivity, crystalluria, blood dyscraias, CNS effects, AVOID in preg and lactation
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| Fluoroquinolones "floxacin" | CIPROFLOXACIN, levofloxacin, ofloxacin, lomefloxacin, sparfloxacin, moxifloxican, gatifloxacin, norfloxacin, trovafloxicin, alatrofloxacin, gemifloxacin
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| CIPROFLOXACIN | broad spectrum, IV or oral, not good on anaerobes
inhibits bacerial DNA gryase & topoisomerase
IV = bactericidal
uses: resp tract, UTI, bones, joints, skin, soft tissue, traveler's diarrhea, DRUG OF CHOICE for anthrax
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| CIPROFLOXACIN adverse effects, interactions | GI, HA, dizziness, candida of pharynx and vagina, tendon injury, c. diff infection, photosensitivity
Int: absorption decreased by: aluminum or magnesium antiacids, iron, zinc, sucralfae, milk & dairy
can inc warfarin or theophylline levels
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| METRONIDAZOLE (flagyl) | bactericidal
uses: protozoal infections, obligate anaerobe infections, H. Pylori, C. Diff (drug of choice), prophylaxis before sx
AE: disulfurm rxn w/alcohol, neurotoxicity, allergies, superinfections, avoid in 1st trimester
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| DAPTOMYCIN | new (cyclic lipopetides)
bactericidal for all gram + bacteria
uses: staph (MRSA, VRSA), enterococci, streptococci
AE: muscle pain/weakness, minimal drug int.
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| RIFAMPIN | broad spectrum
used for TB, prophylaxis for meningitis
quick resistence when used alone
induces liver drug-metabolizing enzymes
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| RIFAXIMIN | nonabsorbal analog of rifampin
used for traveler's diarrhea in pts 12 and older
prevent hepatic encephalopathy
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| POLYMYXIN B | broad spectrum topical bactericidal agent
forms pores or holes in memebrane
often found in OTC antibacterial agents
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| BICITRACIN | topical agent
inhibits cell wall synthesis
used for staph infections and A streptococci infections
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| Uncomplicated UTI treatment | SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim)
FOSFOMYCIN
NITROFURANTOIN (macrobid)
FLUROUINOLINES (Cipro or Levofloxacin)
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| Pyelonephritis treatment | SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim)
FLUROUINOLINES (Cipro or Levofloxacin)
SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim)
FLUROUINOLINES (Cipro or Levofloxacin)
CEPHALEXIN, CEFOTAXIME, CEFTRIAXONE
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| Complicated UTI treatment | SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim)
FLUROUINOLINES (Cipro or Levofloxacin)
SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim)
AMOXICILLIN (w/clavulanic acid)
CEPHALEXIN
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| Bacterial Prostatisis Treatment | FLUOROUINOLONES (Cipro) follow by DOXYCYCLINE
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| Urinary Tract Antiseptics: NITROFURANTOIN (macrobid) | bacteriostatic-low concentration
bactericidal-high concentration
uses: lower UTI, prophylaxis, recurrent UTIs
AE: GI, pulmonary rxn, hematologic effecs, peripheral neuropathy, birth defects, CNS effects
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| Urinary Tract Antiseptics: METHANAMINE | prodrug, decomposes into ammonia and formaldehyde causing denaturing of the bacteria
used for chronic lower UTIs
contraindicated in pts with renal disease or liver disease
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| Chlamydia Trachomatis treatment | AZITHROMYCIN, DOXYCYCLINE, ERYTHORMYCIN BASE (infants and children)
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| Gonococcal Infection treatment | FLUOROUINOLINES: 1st drug: CEFTRIAXONE, 2nd drug: AZITHROMYCIN
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| Trichomonas vaginalis treatment | METRONIDAZOLE (flagyl), TINIDAZOLE
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| TB treatment guidelines | must contain 2 or more drugs to which the organism is sensitive
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| First Line TB drug therapy | Isoniazid, rifampin, rifapentine, rifabutin, pyrazinamide, and emthambutol
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| Second Line TB drug therapy | Fluroquinolones (Levofloxacin, moxifloxacin)
Kanamycin, amidacin, capreomycin, streptomycin
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| Other drugs for TB therapy | para-aminosalicylic acid, ethionamide, cycloserine
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| Isoniazid | admin orally/IV, used in active TB (in combo), latent TB (alone or in combo with rifapentine)
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| Isoniazid MOA | inhibits synthesis of mycolic acid, necessary for mycobacterial cell wall, bactericidal to active cells, resistance can develop
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| Isoniazid AE, | hepatoxicity-need monthly levels drawn, peripheral neuropathy, CNS effects (seizures, dizziness, ataxia, depression), anemia-from Vit B6 deficiency, can give pyridoxine to prevent
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| Isoniazid Drug Interactions | inhibitor of liver enzymes, can raise levels of other drugs metabolized by liver, alcohol and other TB drugs can increase hepatoxicity
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| Rifampin | broad spectrum atnibx, inhibits protein systhesis, always give in combo to prevent resistence
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| Rifampin Uses | Active TB, pulmonary TB (drug of choice), other bacterial infections, leprosy
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| Rifampin AE, drug interactions | hepatoxicity, discoloration of urine (red-orange color), accelerates metabolism of OCs, warfarin, HIV drugs = decrease effectiveness
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| Rifapentine and Rifabutin | similar to rifampin
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| Pyrazinamide | bactericidal to M. Tuberculosis, used in combo with other TB drugs to treat active and latent TB
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| Pyraziamide & Rifampin | treat latent TB
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| Pyraziamide AE | hepatoxicity, nongouty polyarthalgias, hyperuricemia (inhibition of uric acid excretion)
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| Ethambutol | only active against mycobacteria, used in combo w/other drugs, INITIAL tx for TB
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| Ethambutol AE | optic neuritis = blurred vision, visual disturbances, allergic rxns, GI upset
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| Capreomycin | second line drug for TB treatment, injectable antibx, bateriostatic, used for TB resistant to primary agents
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| Capreomycin AE | kidney toxicity, ototoxicity - balance and tinnitus issues
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| Aminoglycosides use in TB tx | Amikacin, Kanamycin, streptomycin, AE: kidney toxicity, ototoxicity
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| Para-aminosalicylic Acid (PAS) | inhibits synthesis of folic acid, used in TB tx
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| Ethionimide | similar to isoniazid, less active, used in TB tx
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| Cycloserine | inhibits cell wall synthesis, used in TB tx
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| Bedaquiline | new drug, faster and better than all other TB drugs, inhibits ATP synthesis, causes prolonged QT interval and hepatoxicity
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| Tx for Active TB induction phase | 4 drugs isoniazid, rifampin, pyrazinamide, ethambutol for 2 months
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| Tx for active TB Continuation phase | Isoniazid and rifampin x 4 months
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| Tx for active TB w/isoniazid resistence | Rifampin, pyrazinamide, themabutol x 6 months
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| Tx for latent TB | Isoniazid 2x/week for 6-9 months OR Isoniazid + rifapentine 1x/week for 3 months
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| Rifampin and HIV | rifampin can interact with drugs used to tx HIV, use RIFABUTIN, = less likely to interact with HIV anitviral drugs
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| Mycobacerium Avium Complex (MAC) | Azithromycin and clarithromycin used prophylactically
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| Tx fo active MAC infection | Azithromycin and clarithromycin + Ethambutol + Rifampin or Rifabutin
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| Paucibacillary Leprosy | skin smears are (-), 1-5 skin lesions, tx: 6 months of rifampin and dapsone
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| Multibacillary Leprosy | skin smears are (+), 6 or > lesions, tx: 12 months of rifampin, dapson, clofazimine
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| Dapsone | inhibit folic acid synthesis, used to tx leprosy
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| Clofazimine | used to tx leprosy, always combined with rifampin or dapsone
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| Polyenes: Amphotericin B | broad spectrum antifungal, binds to ergosterol, increase permeability of fungal cell membrane
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| Polyenes: Amphotericin B toxicity | highly toxic, binds to sterols in mammalian cell walls, used only against progressive and fatal infections, admin IV
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| Polyenes: Amphotericin B uses, AE | used for systemic fungal infections, AE: infusion rxn, nephrotoxicity (infuse saline), hypokalemia, bone marrow suppression
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| Azoles | block synthesis of ergosterol, broad spectrum, alternative to amphotericin B, oral, inhibit CYP450 enzymes, can increase levels of other drugs
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| Azoles: Itraconazole | drug of choice for blastomycsis, histoplasmosis, paracoccidioidomycosis, sportrichosis, and alternaitve for aspergillosis, candidiasis, cocciodiodomycosis
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| Azoles: Itraconazole AE/drug interaction | cardiac suppression, liver injury, inhibitor of CYP450, drugs that raise gastric pH can reduce absorption of itraconazole
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| Other Zoles | ketaconazole -slow acting, fluconazole (diflucan)-yeast infection, voriconazole-drug of choice for aspergillosis
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| Echinocandins-Anidulafungin, Micafungin | disrupt fungal cell wall-used for candida infections, given IV
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| Echinocandins-Caspofungin | disrupt fungal cell wall-used for aspergillis and candida infections, given IV
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| Pyrimidine Analog: Flucytosine | narrow spectrum antifungal, can develop resistance, disrupts fungal DNA and RNA synthesis
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| Pyrimidine Analog: Flucytosine-uses/AE | used in candida infections, c. neoformans, can be combined with amphotercin B. AE: bone marrow suppresion, hepatoxicity
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| Agents for Superficial Fungal Infections | Azoles, allyamines, polyenes, griseofulvin, ciclopirox
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| Allyamines: Naftifine, Terbuinafine, Butenafine | agent for superficial fungal infection that inhibition of squalene exposidase, which inhibits sysnthesis of ergosterol
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| Polyenes: Nystatin | agent for superficial fungal infection, given orally and topically
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| Griseofulvin | agent for superficial fungal infection that can interact with liver enzymes, not active against candida infections, used for dermatophytic infections
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| Ciclopirox | used for fungal infections of the nails
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| Antiviral: Acyclovir | 1st choice for HSV and VZV, suppresses synthesis of viral DNA, oral/IV/topical, 1/2 life 2hrs. AE: reversible nephrotoxicity tx'd w/slow infusion and hydration,
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| Famciclovir | tx HSV, prodrug converted to penciclovir, longer 1/2 life, higher blood levels than acyclovir
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| Valcyclovir (valtrex) | tx HSV, prodrug converted to acyclovir, longer 1/2 life, higher blood levels, more AE in immunosuppressed pts
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| Foscarnet | tx CMV retinits in AIDS pts, acyclovir resistant HSV and VZV in immunocompromised pts, difficult to administer, not well tolerated, expensive, cause neprhotoxicity and electrolyte and mineral imbalances
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| Penciclovir | topical drug used for cold sores, suppress viral replication, used for recurrent HSV
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| Docosanol (Abreva) | topical drug used for cold sores, blocks viral entry into host cell, used for recurrent HSV
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| Drugs used for Cytomegalovirus (CMV) | suppress replication of viral DNA.
Ganciclovir, Valganciclovir, Cidofovir, Foscarent
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| Valganciclovir | tx CMV, causes bone marrow suppression and some reproductive toxicity
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| Interferon Alfa-2b | tx Hep C, blocks viral entry into cells, synthesis of viral MRNA and proteins & viral assembly release, conjugaed with POLYETHYLENE GLYCOL (PEG) to make long acting interferons
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| Pegasys | Interferon alfa-2a w/ PEG, tx Hep C
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| Pegintron | Interferon alfa-2b w/PEG, tx Hep C
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| Interferon Alfa-2b + Ribavurin (Rebetol) | broad spectrum antiviral, tx Hep C, improve response rates when combined
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| Interferon Alfa-2b + Boceprevir or Telaprevir | protease inhibitors and inhibit HCV replication
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| Interferon Alf-2b adverse effects | flu-like symptoms, depression, bone marrow suppression, thyroid dysfxn, heart damage, Ribavurin is teratogenic and embryolethal can cause hemolytic anemia
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| Interferon Alfa-2b or Peginterfrom Alfa 2a | tx Hep B, given SC
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| Nucleoside Analogs | tx Hep B, given orally inhibits viral DNA synthesis, tx pts with highest risk d/t prolonged tx
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| Nucleoside Analog Agents | lamivudine, adefovir, entecavir, telbivudine, tenofovir
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| Osetamvir (Tamiflu-oral), Zanamivir (Rlenza-oral inhalation) | neuraminidase inhibitor (enzyme for viral replication), used to tx influenza, causes N/V and hypersensitivity rxn
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| Ribavirin | antiviral used to tx RSV, inhaled or oral, category X, can precipitate in mechanical breathing apparatus, should not be used with resp assistance.
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| Palivizumab (Synagis) | monoclonab antibody used for RSV prevention in preamature infants and those with chronic lung disease, causes hypersensitivity rxns
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| RTIs: Non-Nucleosides | do not get transported into DNA, bind directly to reverse transcriptase,
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| RTIs: Nucleosides/Nucleotides | reverse transcriptase inhibitor used to tx HIV, get transported into DNA, inhibit reverse tanscriptase, can cause lactic acidosis w/steatosis (rare and fatal)
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| RTI: Nucleosides/Nucleotides: Zidovudine (AZT) | tx HIV, given po/IV, short 1/2 life, penetrates CNS, causes anemia, neurtorpenia, and myopathy. used in pregnancy and delivery
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| RTI: Nucleosides/Nucleotides: Didanosine | tx HIV, buffered powder, po, cuases pancreatitis and peripheral neuropathy, causes extensive drug interactions
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| RTI: Nucleosides/Nucleotides: Abacavir | tx HIV, oral, causes fatal hypersensitivity rxn
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| RTI: Nucleosides/Nucleotides: Tenofovir | tx HIV, oral, causes asthenia, HA, GI upset, renal insufficiency
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| Nucleosides/Nucleotides: Efavirenz (Sustiva) | tx HIV, oral, causes rash, CNS side effects, teratogenic, kyperlipidemia, long 1/2 life, interfere with liver enzymes
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| Nucleosides/Nucleotides: Nevirapine | tx HIV, oral, causes rash and hepatoxicity, interfere with liver ezymes
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| Nucleosides/Nucleotides: Delavirdine | tx HIV, oral, causes rash, hepatoxicity, and pancreatitis, interfere with liver enzymes
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| Protease Inhibitors in HIV tx | when used in combo with NRTIs can reduce viral load to undectable levels, all have SE, mostly GI, glucose intolerance, hyperlipidemia, possible bone loss, inhibit liver enzymes, boosted with Ritonavir
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| Protease Inhibitors Agents in HIV TX | Saquinavir, ritonavir, indinavir, delfinavir, amprenavir, fosamprenavir, atazanavir, darunavir tipranavir
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| Integrase Inhibitors in HIV tx: Raltegravir | blocks intergration of viral DNA inot the genetic code of infected cell, NEW class, causes hypersensitivity rxn, indicated for combo thx
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| Fusion Inhibitors in HIV tx: Enfuvirtide | blocks entry of HIV into CD4 cells, 36 amino acid peptide, injected SC 2x/day,
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| CCR5 Antagonist in HIV tx: Maraviroc | block CCR5, metabolized in liver, given orally, causes: fever, cough, rash, liver toxicity, sore muscles, dizziness
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| Tenofovir Emitricitabine | used for HIV pre-exposure prophylaxis (PREP), can reduce infection by 44-73%
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| NNRTI-based Efavirenz + Lamivudine or Emtricitabine + Zidovudine or Tenofovir | used for post-HIV exposure prophylaxis (PEP)
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| Occupational exposure to HIV | no PEP, 2 NRTIs (emtricitabine + tenofovir) and PI-based lopinavir/ritonir + emtricitabine + tenofovir
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| Antiretorviral Therapy (ART) | consists of 3 drugs: 2 from different classes
NNRTI + 2 NRTIs, PI + 2 NRTIs, Raltegravir + 2 NRTIs
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| Ritonavir-protease inhibitor | inhibit P450 the most = drug interactions
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| PI and NNRTI drug interactions | Rifampin most problematic, decreased PI and NNRIT levels by increasing liver enymes, others: viagra, antihistamines, sedatives, drugs that lower cholesterol, anti-fungals, OCs
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| Chloroquine | anti-malarial drug (moderate attack and prophylaxis), active against erythocytic forms of parasite, drug of choice for: p. vivax and p. faheiparum
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| Choroquine MOA, AE | prevents organisms from converting heme (toxic to parasite) to nontoxic metabolites, give oral/IM, causes visual disturbances and GI effects
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| Mefloquine | anti-malarial drug, highly active against erthrocytic forms of P. vivax and P. falcuparum, drug of choice for phrophylaxis in regions wehre chloroquine-resistant P. vivax, and P. falciparum is found
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| Mefloquine MOA, AE | similar to chloroquine, given orally, AE: dose-related n/v, visual disturbances, dizziness, prolonged QT interval, CNS toxicity (vertigo, confusion, convulsions)
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| Mefloquine drug interactions | ketoconazole can increase levels, rifampin can decrease levels
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| Primaquine | anti-malarial drug, highly active against hepatic forms of p. vivax, used to eradicate P. vivax from liver, active against dormant forms
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| Primaquine AE | oral, take w/food, causes hemolysis especially in pts w/ G6PD deficiency
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| Artemether/Lumefantrine (Coatrem) | Artemisinin Derivative: anti-malarial tx, active against P. faciparu, only for tx not for prophylaxis, oral, taken w/food, active metabolite of drug kills parasite
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| Artemether/Lumefantrine (Coatrem) AE | some CNS effects (HA, dizziness), prolong QT interval, metabolized by CYPs so other drugs can affect levels
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| Artesunate | Artemisinin Derivative: anti-malarial tx (severe attack), drug of choice for severe malaria cases, only available from the CDC, give IV
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| Quinine | anti-malarial tx, used for chloroquine-resistant strains, active against erythrocytic forms only, requires adjunct thx, usually doxycycline, tetracycline, or clindamycin
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| Quinidine Gluconate | anti-malarial tx, only drug approved for parental thx, used in severe cases, should be injected slowly to prevent hypotension and acute circulatory response
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| Atovaquone/Proguamil | anti-malarial tx, prophylaxis and tx of malaria caused by chlorquine-restiant plasmodia, used for both erythocyctic and exoerythrocytic (hepatic) forms
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| Iodoquinol | drug of choice for tx of asymptomatic intestinal amebiasis, can be used in combo w/METRONIDAZOLE for symptomatic and systemic infections, oral, little absorption
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| Metronidazole (Flagyl) uses | active against seeral protozoal species, anaerobic bacteria, used for symptomatic intestinal amebiasis and systemic amebiasis, also girdiasis and trichomoniasis
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| Metronidazone (Flagyl) MOA | prodrug, converted to active form in anaerobic cells, impairs DNA, given oral/IV
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| Metronidazone (Flagyl) AE | Nausea, HA, hypersensitivity rxn, drug int: disulfiram-like effect, drugs that affect CYPA4
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| Tindazole | antiprotozoal drug, similar to metronidazole, longer 1/2 life, more expensive, oral, MOA/uses/AE same as Metronidazole,
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| Giardiasis Tx | Metronidazole, tinidazole, Nitazoxamide
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| Nitazoxanide | approved for C. parvum infections in immunocompetent children (cyptosporidiosis) and diarrhea caused by G. lamblia in adults
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| Nitazoxanide MOA/AE/Drug Int | disrupts protozoal energy metabolism, causes GI upset & yellow discoloration of eyes, binds to proteins, possible intx w/ other protein binding drugs
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| Trichomonisis Tx | Metronidazole, Tinidazole
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| Lice Tx | Permethin (Nix)-topical, pesticide, Malathion-topical, pesticide, Ivermectin-topical, oral, last line)
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| Scabies Tx | Permethrin, Ivermectin
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| Anti-Helmintics (worm infections): Mebendazole | used against pinworms, roundworm, hookworm, whipwork, filariae, decrease glucose transport and ATP = kills worms, oral, minimal absorption, takes 2-3 days to work, well tol,, teratogenic in animals
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| Anti-Helmintics (worm infections): Albendazole | active against round, hook, pin, and tape worms, oral with fatty meal to enhance absorption, prevents microtubule-depenent uptake of glucose in worm, AE: mild liver impairment, bone marrow suppression, teratogenic
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| Anti-Helmintics (worm infections): Pryantel Pamoate | used for pin, hook and round worms, depolarizing neuromuscular blocker, cholinesterase inhibitor = paralyzes worm, minimal amts absorbed, most stays in GI tract
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| Anti-Helmintics (worm infections): Ivermectin | broad spectrum, used for filariae, threadworms, scabes, hookworms, cutaneous lava migrans, paralyzes worm, oral, absorbed systemically, ? teratogenic
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