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Chemo/Antibx
Chermotherapy....Antibiotics
| Term | Definition |
|---|---|
| Beta-Lactam Antibiotics | Penicillins Cephalosporins Carbaenems Vancomycin, Telavancin, Aztreonam |
| PENICILLINS | beta-lactam anitbx that weakens the bacterial cell wall causes bateria to take up excessive water and rupture bactericidal-kills bacteria |
| Bactericidal | kills sensitive organisms number of organisms decline rapidly activation of host immune system not required MOA: block an essential function of the organism |
| 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 |
| 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 |
| Penicillinase-Resistant PCNs | NAFCILLIN, OXACILLIN, DICLOXACILLINhighly resistent to beta-lactamases used against S. Aureus and S. Epidermis |
| Broad Spectrum PCNs (Aminopenicillins) | AMPICILLIN, AMOXICILLIN tx gram-positive cocci and some gram-negative AE-rash, diarrhea |
| 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 |
| 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 |
| First Generation Cephalosporins | CEFADROXIL, CEPHALEXIN, CEFAZOLIN mostly gram + organisms, some gram- destroyed by beta-lactamases |
| 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 |
| 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 |
| CEFTRIAXONE (Rocephin) | 3rd generation, liver metabolism (not kidney), causes bleeding |
| Fourth Generation Cephalosporins | CEFEPIME CSF penetration highest restistance to beta lactamase highest activity against gram - bacteria and anaerobes |
| Fifth Generation Cephalosporins | CEFAROLINE (new) effective against MRSA |
| Carbapenems | Beta-lactam antibx, weaken cell wall broad spectrum low toxicity-GI and hypersensitivity can dec valporic acid levels = inc risk of seizures |
| Carbapenem Agents | IMIPENEM-given with cilstatin MEROPENEM ETRAPENEM DORIPENEM-new for uncomplicated UTI, tx psedomonas |
| 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 |
| AZTREONAM | cell wall synthesis inhibitor beta lactam antibx narrow spectrum....only gram - IV/IM well tolerated |
| 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 |
| 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 |
| 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 |
| TETRACYCLINE (sumycin) | short-acting, eliminated by the kidney food decreases oral absorption, low lipid solubility |
| DEMECLOCYCLINE | Intermediate-acting, eliminated by the kidney food decreases abosorption, moderate lipid solubility |
| DOXYCLYCLINE, MINOCYCLINE | Long-acting, eliminated by the liver food decreases oral absorption MINOCYCLINE-food does not decrease oral absorption |
| Bateriostatic Inhibitors of Protein Synthesis: TETRACYCLINES uses | infections, acne, peptic ulcer disease (h. pylori), peridontal disease, prophylaxis for malaria |
| Bateriostatic Inhibitors of Protein Synthesis: TETRACYCLINES concerns | absorption: milk products, iron supplements, magnesium containing laxatives, and antiacids.....take 2hrs apart AVOID in renal failure |
| 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 |
| Clostritidum Difficile-associated disease (CDAD) diarrhea | profuse watery diarrhea, abd pain, fever, leukocytosis can be fatal tx: vancomycin or metronidazole, fluid, electrolyte replacement |
| Macrolides | ERYTHROMYCIN, CLARITHROMYCIN, AZITHROMYCIN broad spectrum antibx inhibit protein synthesis at 50S ribosome |
| 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 |
| Macrolides: CLARITHROYCIN | used for resp tract infections, mycobaterium avium complex, H. pylori AE: GI, supra infection, caridotoxicity, can inhibit hepati metabolism = drug int |
| Macrolides: AZITHROMYCIN | used for resp tract infections, chancroid, OM, mycobacterium avium complex, C. trachoatis AE: minimal GI and drug int. |
| Protein Synthesis Inhibitors: CLINDAMYCIN | broad spectrum |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 - |
| Aminoglycosides MOA | inhibit protein synthesis by: binding to 30S subunit, premature termination of synthesis, production of abnormal proteins |
| Aminoglycoside Agents | GENTAMICIN, TOBRAMYCIN, AMIKACIN, KANAMYCIN, STREPTOMYCIN (used in TB), NEOMYCIN (topical), PAROMOMYCIN (for parasites, stays in GI tract) |
| 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 |
| TOBRAMYCIN | similar to gentamycin except: more active against pseudomonas aeruginosa less active against Enterococci and Serratia more epxensive |
| AMIKACIN | similar to gentamycin except: broadest sprectrum against gram - bacteria lowest incidence of resistance |
| 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 |
| Short-Acting Sulfonamide | SULFISOXZOLE-only available in combo w/erythromycin SULFADIAZINE- prophylaxis for meningitis |
| Intermediate-Acting Sulfonamide | SULFMETHOXAZOLE-only available in combo w/trimethoprim |
| Topical Sulfonamide | SULFACETAMIDE-eye infections SILVER SULFADIAZINE- infections after burns MAFENIDE-infections after burns |
| 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 |
| 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 |
| Fluoroquinolones "floxacin" | CIPROFLOXACIN, levofloxacin, ofloxacin, lomefloxacin, sparfloxacin, moxifloxican, gatifloxacin, norfloxacin, trovafloxicin, alatrofloxacin, gemifloxacin |
| 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 |
| 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 |
| 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 |
| DAPTOMYCIN | new (cyclic lipopetides) bactericidal for all gram + bacteria uses: staph (MRSA, VRSA), enterococci, streptococci AE: muscle pain/weakness, minimal drug int. |
| RIFAMPIN | broad spectrum used for TB, prophylaxis for meningitis quick resistence when used alone induces liver drug-metabolizing enzymes |
| RIFAXIMIN | nonabsorbal analog of rifampin used for traveler's diarrhea in pts 12 and older prevent hepatic encephalopathy |
| POLYMYXIN B | broad spectrum topical bactericidal agent forms pores or holes in memebrane often found in OTC antibacterial agents |
| BICITRACIN | topical agent inhibits cell wall synthesis used for staph infections and A streptococci infections |
| Uncomplicated UTI treatment | SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim) FOSFOMYCIN NITROFURANTOIN (macrobid) FLUROUINOLINES (Cipro or Levofloxacin) |
| Pyelonephritis treatment | SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim) FLUROUINOLINES (Cipro or Levofloxacin) SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim) FLUROUINOLINES (Cipro or Levofloxacin) CEPHALEXIN, CEFOTAXIME, CEFTRIAXONE |
| Complicated UTI treatment | SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim) FLUROUINOLINES (Cipro or Levofloxacin) SULFAMETHOXAZOLE/TRIMETHOPRIM (bactrim) AMOXICILLIN (w/clavulanic acid) CEPHALEXIN |
| Bacterial Prostatisis Treatment | FLUOROUINOLONES (Cipro) follow by DOXYCYCLINE |
| 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 |
| 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 |
| Chlamydia Trachomatis treatment | AZITHROMYCIN, DOXYCYCLINE, ERYTHORMYCIN BASE (infants and children) |
| Gonococcal Infection treatment | FLUOROUINOLINES: 1st drug: CEFTRIAXONE, 2nd drug: AZITHROMYCIN |
| Trichomonas vaginalis treatment | METRONIDAZOLE (flagyl), TINIDAZOLE |
| TB treatment guidelines | must contain 2 or more drugs to which the organism is sensitive |
| First Line TB drug therapy | Isoniazid, rifampin, rifapentine, rifabutin, pyrazinamide, and emthambutol |
| Second Line TB drug therapy | Fluroquinolones (Levofloxacin, moxifloxacin) Kanamycin, amidacin, capreomycin, streptomycin |
| Other drugs for TB therapy | para-aminosalicylic acid, ethionamide, cycloserine |
| Isoniazid | admin orally/IV, used in active TB (in combo), latent TB (alone or in combo with rifapentine) |
| Isoniazid MOA | inhibits synthesis of mycolic acid, necessary for mycobacterial cell wall, bactericidal to active cells, resistance can develop |
| 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 |
| Isoniazid Drug Interactions | inhibitor of liver enzymes, can raise levels of other drugs metabolized by liver, alcohol and other TB drugs can increase hepatoxicity |
| Rifampin | broad spectrum atnibx, inhibits protein systhesis, always give in combo to prevent resistence |
| Rifampin Uses | Active TB, pulmonary TB (drug of choice), other bacterial infections, leprosy |
| Rifampin AE, drug interactions | hepatoxicity, discoloration of urine (red-orange color), accelerates metabolism of OCs, warfarin, HIV drugs = decrease effectiveness |
| Rifapentine and Rifabutin | similar to rifampin |
| Pyrazinamide | bactericidal to M. Tuberculosis, used in combo with other TB drugs to treat active and latent TB |
| Pyraziamide & Rifampin | treat latent TB |
| Pyraziamide AE | hepatoxicity, nongouty polyarthalgias, hyperuricemia (inhibition of uric acid excretion) |
| Ethambutol | only active against mycobacteria, used in combo w/other drugs, INITIAL tx for TB |
| Ethambutol AE | optic neuritis = blurred vision, visual disturbances, allergic rxns, GI upset |
| Capreomycin | second line drug for TB treatment, injectable antibx, bateriostatic, used for TB resistant to primary agents |
| Capreomycin AE | kidney toxicity, ototoxicity - balance and tinnitus issues |
| Aminoglycosides use in TB tx | Amikacin, Kanamycin, streptomycin, AE: kidney toxicity, ototoxicity |
| Para-aminosalicylic Acid (PAS) | inhibits synthesis of folic acid, used in TB tx |
| Ethionimide | similar to isoniazid, less active, used in TB tx |
| Cycloserine | inhibits cell wall synthesis, used in TB tx |
| Bedaquiline | new drug, faster and better than all other TB drugs, inhibits ATP synthesis, causes prolonged QT interval and hepatoxicity |
| Tx for Active TB induction phase | 4 drugs isoniazid, rifampin, pyrazinamide, ethambutol for 2 months |
| Tx for active TB Continuation phase | Isoniazid and rifampin x 4 months |
| Tx for active TB w/isoniazid resistence | Rifampin, pyrazinamide, themabutol x 6 months |
| Tx for latent TB | Isoniazid 2x/week for 6-9 months OR Isoniazid + rifapentine 1x/week for 3 months |
| Rifampin and HIV | rifampin can interact with drugs used to tx HIV, use RIFABUTIN, = less likely to interact with HIV anitviral drugs |
| Mycobacerium Avium Complex (MAC) | Azithromycin and clarithromycin used prophylactically |
| Tx fo active MAC infection | Azithromycin and clarithromycin + Ethambutol + Rifampin or Rifabutin |
| Paucibacillary Leprosy | skin smears are (-), 1-5 skin lesions, tx: 6 months of rifampin and dapsone |
| Multibacillary Leprosy | skin smears are (+), 6 or > lesions, tx: 12 months of rifampin, dapson, clofazimine |
| Dapsone | inhibit folic acid synthesis, used to tx leprosy |
| Clofazimine | used to tx leprosy, always combined with rifampin or dapsone |
| Polyenes: Amphotericin B | broad spectrum antifungal, binds to ergosterol, increase permeability of fungal cell membrane |
| Polyenes: Amphotericin B toxicity | highly toxic, binds to sterols in mammalian cell walls, used only against progressive and fatal infections, admin IV |
| Polyenes: Amphotericin B uses, AE | used for systemic fungal infections, AE: infusion rxn, nephrotoxicity (infuse saline), hypokalemia, bone marrow suppression |
| Azoles | block synthesis of ergosterol, broad spectrum, alternative to amphotericin B, oral, inhibit CYP450 enzymes, can increase levels of other drugs |
| Azoles: Itraconazole | drug of choice for blastomycsis, histoplasmosis, paracoccidioidomycosis, sportrichosis, and alternaitve for aspergillosis, candidiasis, cocciodiodomycosis |
| Azoles: Itraconazole AE/drug interaction | cardiac suppression, liver injury, inhibitor of CYP450, drugs that raise gastric pH can reduce absorption of itraconazole |
| Other Zoles | ketaconazole -slow acting, fluconazole (diflucan)-yeast infection, voriconazole-drug of choice for aspergillosis |
| Echinocandins-Anidulafungin, Micafungin | disrupt fungal cell wall-used for candida infections, given IV |
| Echinocandins-Caspofungin | disrupt fungal cell wall-used for aspergillis and candida infections, given IV |
| Pyrimidine Analog: Flucytosine | narrow spectrum antifungal, can develop resistance, disrupts fungal DNA and RNA synthesis |
| Pyrimidine Analog: Flucytosine-uses/AE | used in candida infections, c. neoformans, can be combined with amphotercin B. AE: bone marrow suppresion, hepatoxicity |
| Agents for Superficial Fungal Infections | Azoles, allyamines, polyenes, griseofulvin, ciclopirox |
| Allyamines: Naftifine, Terbuinafine, Butenafine | agent for superficial fungal infection that inhibition of squalene exposidase, which inhibits sysnthesis of ergosterol |
| Polyenes: Nystatin | agent for superficial fungal infection, given orally and topically |
| Griseofulvin | agent for superficial fungal infection that can interact with liver enzymes, not active against candida infections, used for dermatophytic infections |
| Ciclopirox | used for fungal infections of the nails |
| 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, |
| Famciclovir | tx HSV, prodrug converted to penciclovir, longer 1/2 life, higher blood levels than acyclovir |
| Valcyclovir (valtrex) | tx HSV, prodrug converted to acyclovir, longer 1/2 life, higher blood levels, more AE in immunosuppressed pts |
| 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 |
| Penciclovir | topical drug used for cold sores, suppress viral replication, used for recurrent HSV |
| Docosanol (Abreva) | topical drug used for cold sores, blocks viral entry into host cell, used for recurrent HSV |
| Drugs used for Cytomegalovirus (CMV) | suppress replication of viral DNA. Ganciclovir, Valganciclovir, Cidofovir, Foscarent |
| Valganciclovir | tx CMV, causes bone marrow suppression and some reproductive toxicity |
| 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 |
| Pegasys | Interferon alfa-2a w/ PEG, tx Hep C |
| Pegintron | Interferon alfa-2b w/PEG, tx Hep C |
| Interferon Alfa-2b + Ribavurin (Rebetol) | broad spectrum antiviral, tx Hep C, improve response rates when combined |
| Interferon Alfa-2b + Boceprevir or Telaprevir | protease inhibitors and inhibit HCV replication |
| 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 |
| Interferon Alfa-2b or Peginterfrom Alfa 2a | tx Hep B, given SC |
| Nucleoside Analogs | tx Hep B, given orally inhibits viral DNA synthesis, tx pts with highest risk d/t prolonged tx |
| Nucleoside Analog Agents | lamivudine, adefovir, entecavir, telbivudine, tenofovir |
| Osetamvir (Tamiflu-oral), Zanamivir (Rlenza-oral inhalation) | neuraminidase inhibitor (enzyme for viral replication), used to tx influenza, causes N/V and hypersensitivity rxn |
| Ribavirin | antiviral used to tx RSV, inhaled or oral, category X, can precipitate in mechanical breathing apparatus, should not be used with resp assistance. |
| Palivizumab (Synagis) | monoclonab antibody used for RSV prevention in preamature infants and those with chronic lung disease, causes hypersensitivity rxns |
| RTIs: Non-Nucleosides | do not get transported into DNA, bind directly to reverse transcriptase, |
| 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) |
| 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 |
| RTI: Nucleosides/Nucleotides: Didanosine | tx HIV, buffered powder, po, cuases pancreatitis and peripheral neuropathy, causes extensive drug interactions |
| RTI: Nucleosides/Nucleotides: Abacavir | tx HIV, oral, causes fatal hypersensitivity rxn |
| RTI: Nucleosides/Nucleotides: Tenofovir | tx HIV, oral, causes asthenia, HA, GI upset, renal insufficiency |
| Nucleosides/Nucleotides: Efavirenz (Sustiva) | tx HIV, oral, causes rash, CNS side effects, teratogenic, kyperlipidemia, long 1/2 life, interfere with liver enzymes |
| Nucleosides/Nucleotides: Nevirapine | tx HIV, oral, causes rash and hepatoxicity, interfere with liver ezymes |
| Nucleosides/Nucleotides: Delavirdine | tx HIV, oral, causes rash, hepatoxicity, and pancreatitis, interfere with liver enzymes |
| 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 |
| Protease Inhibitors Agents in HIV TX | Saquinavir, ritonavir, indinavir, delfinavir, amprenavir, fosamprenavir, atazanavir, darunavir tipranavir |
| 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 |
| Fusion Inhibitors in HIV tx: Enfuvirtide | blocks entry of HIV into CD4 cells, 36 amino acid peptide, injected SC 2x/day, |
| CCR5 Antagonist in HIV tx: Maraviroc | block CCR5, metabolized in liver, given orally, causes: fever, cough, rash, liver toxicity, sore muscles, dizziness |
| Tenofovir Emitricitabine | used for HIV pre-exposure prophylaxis (PREP), can reduce infection by 44-73% |
| NNRTI-based Efavirenz + Lamivudine or Emtricitabine + Zidovudine or Tenofovir | used for post-HIV exposure prophylaxis (PEP) |
| Occupational exposure to HIV | no PEP, 2 NRTIs (emtricitabine + tenofovir) and PI-based lopinavir/ritonir + emtricitabine + tenofovir |
| Antiretorviral Therapy (ART) | consists of 3 drugs: 2 from different classes NNRTI + 2 NRTIs, PI + 2 NRTIs, Raltegravir + 2 NRTIs |
| Ritonavir-protease inhibitor | inhibit P450 the most = drug interactions |
| 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 |
| Chloroquine | anti-malarial drug (moderate attack and prophylaxis), active against erythocytic forms of parasite, drug of choice for: p. vivax and p. faheiparum |
| Choroquine MOA, AE | prevents organisms from converting heme (toxic to parasite) to nontoxic metabolites, give oral/IM, causes visual disturbances and GI effects |
| 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 |
| Mefloquine MOA, AE | similar to chloroquine, given orally, AE: dose-related n/v, visual disturbances, dizziness, prolonged QT interval, CNS toxicity (vertigo, confusion, convulsions) |
| Mefloquine drug interactions | ketoconazole can increase levels, rifampin can decrease levels |
| Primaquine | anti-malarial drug, highly active against hepatic forms of p. vivax, used to eradicate P. vivax from liver, active against dormant forms |
| Primaquine AE | oral, take w/food, causes hemolysis especially in pts w/ G6PD deficiency |
| 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 |
| Artemether/Lumefantrine (Coatrem) AE | some CNS effects (HA, dizziness), prolong QT interval, metabolized by CYPs so other drugs can affect levels |
| Artesunate | Artemisinin Derivative: anti-malarial tx (severe attack), drug of choice for severe malaria cases, only available from the CDC, give IV |
| Quinine | anti-malarial tx, used for chloroquine-resistant strains, active against erythrocytic forms only, requires adjunct thx, usually doxycycline, tetracycline, or clindamycin |
| 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 |
| Atovaquone/Proguamil | anti-malarial tx, prophylaxis and tx of malaria caused by chlorquine-restiant plasmodia, used for both erythocyctic and exoerythrocytic (hepatic) forms |
| 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 |
| Metronidazole (Flagyl) uses | active against seeral protozoal species, anaerobic bacteria, used for symptomatic intestinal amebiasis and systemic amebiasis, also girdiasis and trichomoniasis |
| Metronidazone (Flagyl) MOA | prodrug, converted to active form in anaerobic cells, impairs DNA, given oral/IV |
| Metronidazone (Flagyl) AE | Nausea, HA, hypersensitivity rxn, drug int: disulfiram-like effect, drugs that affect CYPA4 |
| Tindazole | antiprotozoal drug, similar to metronidazole, longer 1/2 life, more expensive, oral, MOA/uses/AE same as Metronidazole, |
| Giardiasis Tx | Metronidazole, tinidazole, Nitazoxamide |
| Nitazoxanide | approved for C. parvum infections in immunocompetent children (cyptosporidiosis) and diarrhea caused by G. lamblia in adults |
| 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 |
| Trichomonisis Tx | Metronidazole, Tinidazole |
| Lice Tx | Permethin (Nix)-topical, pesticide, Malathion-topical, pesticide, Ivermectin-topical, oral, last line) |
| Scabies Tx | Permethrin, Ivermectin |
| 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 |
| 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 |
| 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 |
| 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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