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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
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
Created by: julzbanks



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