CLASS: PENICILLINS: cillins Class Penicillin MOA BacterioCIDAL: Weaken the cell wall causing bact. to take up water and RUPTURE Uses - BROAD spectrum: active against a variety of bacteria Adverse effects - - Allergic rxn (common to be allergic to penicillin so ask if allergic and what was the rxn)- 0.4-7% ppl have rxn Rxn can occur minutes to weeks later **Most people have previously consumed penicillin so the rxn can happen on the first dose** Can perform skin test by administering locally to see what happens (rash?) Anaphylaxis- ABC’s and give epinephrine!! If anaphylaxis to penicillin-> don’t give cephalosporin bc MOA is almost identical If minor reaction, can consider giving cephalosporin n/v diarrhea Drug interactions - Aminoglycosides Bacteriostatic abx (tetracyclines- suppress bact.) Probenecid (delayed excretion from kidneys-> toxicity) Warnings/ contraindicatio ns - Bacterial resistance is high bc of high use -> #1 drug with resistance Inability of penicillins to reach their target cell Inactivation of penicillins by bact. Enzymes Production of penicillin-binding proteins (PBP’s) that have a low affinity for penicillins Dose/route Penicillin G Amoxicillin Nafcilin Amoxicillin/clavulanate (augmentin) & Piperacillin/tazobactam (zosyn) IM: stays in system for 30 days PO Absorption in GI is not good so it is not usually given PO-> usually given IV IM (rare) Given IV Common in oncology Kids Pregnancy breastfeeding moms **Reduce dose for pt with renal impairment** s/e Rash diarrhea Important Increased activity against some gram - bacilli - Well tolerated Extends microbe spectrum when combined with penicillinase- sensitive abx CLASS: CEPHALOSPORINS Class Cephalosporin MOA BacteriCIDAL: Disrupt the pathogens cell wall synthesis and causes cell lysis Most effective against cells undergoing active growth and division Uses BROAD spectrum Most widely used group of abx Dose and Route Not absorbed well through the GI tract so usually given IV IM Adverse effects Generally well tolerated Hypersensitivity (rash)-> doesn't necessarily mean allergic Anaphylaxis BLEEDING TENDENCIES (interferes with vit K and prothrombin levels) Thrombophlebitis may occur Drug interactions - Prevacid (proton pump inhibitor) Drugs that promote bleeding** Alcohol (should be avoided, but at least decreased) Warnings/ contraindicatio ns - Bact resistance is high because it is given often Excreted by the kidneys-> reduce dose if pt has renal impairment As you go down: increased ability to reach CSF (cross BBB) ; increased ability to tx resistant bact (MRSA) ; increasingly more active against gram - bact 1st generation 2nd generation 3rd generation 4th generation 5th generation Cephalexin (keflex) Cefoxitin Cefotaxime & Ceftriaxone (rocephin) & ceftazidime (Fortaz) Cefepime Ceftaroline Prophylaxis against infection in surgical pt Rarely used for active infection Very active against gram infections Used to tx hospital associated pneumonias- even those that are resistance like pseudomonas Infections associated with MRSA Crosses BBB Skin infections Able to penetrate CSF **rarely used for active infections** Crosses BBB IV Crosses BBB Ceftriaxone: given IM for gonorrhea Ceftazidime: most effective against pseudomonas aeruginosa (overgrowth of e. Coli) **can cause superinfection-> pseudomembranous colitis s/s: Bloody diarrhea Abdominal pain fever VANCOMYCIN (not a class apparently) MOA Uses Dose and Route BacteriCIDAL: Inhibits cell wall synthesis - Usually given IV bc erratic in GI **if it is FOR a Gi prob or pt is going home, it will be PO Adverse effects Warnings/ contraindicati ons Monitoring Severe infections ONLY!!! STRONGGGGG!!! MRSA Staph epidermidis SEVERE C. DIff Meningitis (can cross CSF) - - Ototoxicity (reversible) Thrombophlebitis Thrombocytopenia Allergy Red man syndrome Should not happen if it is administered correctly Should be given slowly over at least 1 or 2 hours If given too fast or pt is renal impaired-> red man syndrome Red Itching (ants) Hypotensive Tachycardia If person turns red- slow the dose and call provider to see if if it can be given over 3 hrs Kidney toxicity Monitor BUN, creatinine Thrombocytopenia Monitor platelets Prior to dose- get blood level drawn and confirm it is in a safe therapeutic range Too much- kidney damage Too low- won't make a difference CLASS: TETRACYCLINES Class Tetracyclines MOA BacteriostatiC: suppresses bact growth Uses - BROAD spectrum abx (but more narrow than vancomycin) Infectious diseases Peptic ulcer disease Periodontal disease RA Mycoplasma pneumoniae H. pylori Ricketts Lyme Anthrax Rocky mt spotted fever acne Adverse effects - GI irritation Effects bone and teeth Superinfection Hepatotoxicity Renal toxicity Photosensitivity - WEAR SUNSCREEN!! Drug interactions Absorption REDUCED by food- AVOID or SPREAD out Ca (milk) Iron Zinc Mg Antacids Aluminum Warnings/ contraindicatio ns Resistance is increasing Not for use in Children <8 Pregnant women Breast feeding women Will cause teeth to turn brown bc it binds to Ca Will also decrease bone strength Pt counseling Monitoring CLASS: MACROLIDES Erythromycin Class Macrolide (mycin) MOA BacterioSTATIC: Inhibition of protein synthesis Sometimes bactericidal Uses BROAD spectrum Used if pt is allergic to penicillin bc cant give cephalosporin either Active against most gram + and some gram - bact. - Diphtheria Corynebacterium diphtheria Chlamydial infections M. pneumoniae, group A strep pyogenes DRUG OF CHOICE for whooping cough Dose and Route Adverse effects Take on empty stomach with full glass of water - Upper gi pain QT prolongation Sudden cardiac death Superinfections Thrombophlebitis Transient hearing loss - Seizure meds Bipolar meds Warfarin Theophylline (asthma drug) Drug interactions Anything on list Warnings/ contraindicatio ns Safe and free from major Pt counseling Monitoring Clindamycin Class Macrolide MOA BacterioSTATIC: Inhibition of protein synthesis Sometimes bactericidal Uses Usually for wound infections Usually NOT drug of choice Active against most anaerobic bact (gram + and gram -) Indicated for only certain anaerobic infections OUTSIDE the CNS ***ALT. for penicillin*** Dose and Route Take on empty stomach with full glass of water Can be given topically (bact vaginosis) Adverse effects - CDAD (CDIFF) Hepatic toxicity Blood dyscrasias (agranulocytosis, leukopenia) Diarrhea (can be bc infection OR bc the abx) Hypersensitivity reactions Drug interactions Warnings/ contraindicatio ns Pt counseling Monitoring Can PROMOTE severe C. Diff - associated diarrhea (can be fatal!!) Linezolid (zyvox) (no class apparently) Class No class MOA BacterioSTATIC: inhibits protein synthesis Uses Active against multi resistant, gram + pathogens (VRE & MRSA) Dose and Route Can be given long term: > 5 mo Optic neuropathy (reversible) Peripheral neuropathy (reversible) Adverse effects Drug interactions Warnings/ contraindicatio ns Pt counseling Monitoring - Diarrhea n/v HA Myelosuppression (reversible) Low blood cells -> do CBC BEFORE ANEMIA Usually well tolerated and just have n/v AND DIARRHEA - Monoamine oxidase inhibitors (MAOI’s) AMINOGLYCOSIDES Class aminoglycoside MOA Inhibit protein synthesis BacterioCIDAL NARROW spectrum Uses Aerobic gram - bacilli Dose and Route Not absorbed in GI so usually don’t give PO unless issue is in the GI Usually IV Reduce dose for renal impairment Adverse effects Can cause serious injury to inner ear and kidney (damage to renal tubules) **NOT REVERSIBLE** Nephrotoxicity Ototoxicity Hypersensitivity Neuromuscular blockade Blood dyscrasia (RARE) Drug interactions MANY DRUG INTERACTIONS Warnings/ contraindicatio ns Check trough levels Microbial resistance Other ototoxic drugs (vancomycin) Other nephrotoxic drugs Any skeletal muscle relaxants Monitoring CALCIUM GLUCONATE = ANTIDOTE Gentamicin - one that is usually given if pt needs aminoglycoside ***no resistance issue*** Amikacin (Amikin) ***no resistance issue** Used for serious aerobic gram - bacilli - Pseudomonas aeroginosa - E.coli - Klebsiella - Serratia - Proteus miribilis Active against the broadest spectrum of gram - bacilli (still narrow spectrum) DOC when gentamicin is resistant in hospital UTI’S!!! Acute cystitis: lower uti that occurs most in women of clid bearing age Acute uncomplicated pyelonephritis: infection of the kidneys (upper uti) - Common in young children, older adults, women of child bearing age Acute bact prostatitis: inflammation of the prostate caused by local bact infection s/s s/s s/s DOC - Dysuria Urinary urgency and frequency Subprapubic discomfort Pyuria (WBC/pus in urine) Bacteriuria Can be undx bc asymptomatic uncomplicated : Bactrim or nitrofurantoin Resistance exceeds 20%: fluoroquinolones (ciprofloxacin, norfloxacin) Adherence is a concern: single dose fosfomycin - Fever Chills Flank pain Dysuria Urinary frequency and urgency Pyuria Bacteriuria - Mild to moderate: Bactrim Trimethoprim alone, Ciprofloxacin : severe Levofloxacin Severe infection: hospitalization and IV abx - High fever Chills Malaise Myalgia Localized pain Various uti symptoms Responds well to antimicrobial therapy if drug can penetrate deep enough - Drug selection and route depend on organism and severity E Coli: IV agent (fluoroquinoloneciprofloxacin followed by oral agent doxycycline of fluoroquinolone) Vancomycin sensitive e faecalis: iv ampicillin/sulbactam then PO amoxicillin, levofloxacin, doxycycline8 CLASS: SULFONAMIDES Class Sulfonamide MOA BacterioSTATIC: suppress bact growth by inhibiting tetrahydrofolic acid, a derivative of folic acid or folate Uses BROAD spectrum DOC for UTI’s -> hits E.coli - Nocardiosis Chlamydia trachomatis Conjugation therapy for toxoplasmosis/malaria Ulcerative colitis Dose and Route Excreted through Kidneys -> want this tho bc then it will pass through urinary tract to help tx UTIs Adverse effects Only 3% are hypersensitive Stevens-johnsons syndrome Hematologic effects Kernicterus Renal damage from crystalluria More common in african americans and mediterranean populations Warnings/ contraindicatio ns A lot of resistance (especially gonococci, meningococci, streptococci, shigella) May be acquired by spontaneous mutation or by transfer of plasmids that code for abx resistance (R factors) Kernicterus: Bilirubin in the brain Don't give to babies <2mo Don't give to breast feeding moms Don't give to pregnant women after 32 weeks Pt counseling Monitoring Silver Sulfadiazine (silvadene) Trimethoprim/sulfamethoxazole (Bactrim) Used for 2nd and 3rd degree burns - App is usually pain free - Systemic abs. - Mafenide: acidosis - Causes blue/green skin discoloration (avoid face) DOC for ACUTE UTI - Inhibits sequential steps in bacterial folic acid synthesis, making it much more powerful than TMP or SMZ alone - Plasma drug levels Used for - Acute uti - Otitis media - Bronchitis - Shigellosis - Pneumonia caused by pneumocystis jiroveci (recurrence) - Pneumocystitis - Pneumonia - Gi infection a/e - N/v - Rash - Hyperkalemia - HA - Depression - Hallucinations - Hypersensitivity (steven johnsons) - Blood dyscrasias - Kernicterus - Renal damage: crystalluria CLASS: NITROFURANTOIN (Macrodantin) Class ??? MOA Low concentrations: bacterioSTATIC High concentrations: bacterioCIDAL Uses Urinary tract antiseptics Lower UTI’s (bladder and urethra) Prophylaxis Recurrent lower UTI’s Dose and Route Adverse effects - Brown urine Anorexia n/v-> give with food Pulmonary rxn Chills Fever Cough Agranulocytosis Hematological effects Peripheral neuropathy Birth defects -> jaundice or hepatitis Drug interactions Warnings/ contraindicatio ns Pt counseling Monitoring Liver toxicity Not for pregnant women Not for infants <1mo because causes anemia CLASS: FLUOROQUINOLONES Class Floroquinolone MOA Disrupt DNA replication and cell division Uses BROAD spectrum agents with multiple applications Bacteriocidal Adverse effects Usually mild butttt can cause **tendon rupture!!** Affects achilles tendon Warnings/ contraindicatio ns - Not for use in pt < 18 yo Risk for those >60 yo Risk for those on glucocorticoids Risk for kidney, heart, lung transplant CIPROFLOXACIN Class Floroquinolone MOA Inhibits bact DNA gyrase and topoisomerase II Uses Gram - and + bact DOC for anthrax Infections Resp UTI severe*** GI Bones Joints Skin Soft tissue Dose and Route Adverse effects GI: n/v, diarrhea, abdominal pain CNS: dizziness, HA, restlessness, confusion, seizures, Tendon rupture Phototoxicity Candida infections (pharynx & vagina) Increased risk for C diff infection Older adults Confusion, somnolence, psychosis, visual disturbances Myasthenia gravis Drug interactions Cationic compounds Absorption reduced by: Aluminum Mg Antacids Iron salts Zinc salts Sucralfate Milk and dairy (Ca) Elevate drug levels Theophylline (asthma) Warfarin (anticoagulant) Tinidazole (antifungal) Warnings/ contraindicatio ns Bact resistant S aureus Serratia marcescens Campylobacter jejuni Pseudomonas aeruginosa Neisseria gonorrhoeae Pt counseling Monitoring - CLASS: METRONIDAZOLE (Flagyl) Class Metronidazole MOA BacterioCIDAL Uses - Protozoal infections Infections caused by obligate anaerobes H pylori DOC for C diff **Severe c diff= vancomycin Dose and Route Adverse effects - Neurotoxicity Allergy Superinfections Drug interactions Warnings/ contraindicatio ns Pt counseling Monitoring NO ALCOHOL -> n/v -> death ANTIFUGALSSSSSS CLASS: AMPHOTERICIN B (ABELCET) Class Amphotericin MOA Binds to components of the fungal cell membrane, increasing permeability Uses BROAD spectrum antifungals DOC for most systemic mycoses (internal infections) Dose and Route May be given IV for 6wks to 4mo Adverse effects Usually not given bc toxic infusion rxn (premedicate to avoid rxn, or stop infusion and fix problem) Infusion rxn Nephrotoxicity hyPOkalemia (given w/ 1 L NS to protect the kidneys) Hematologic effects (bone marrow suppression) Drug interactions Warnings/ contraindicatio ns HIGHLY toxic-> should only be employed against infections that are progressive and potentially fatal - Don't give with other nephrotoxic drugs Don't give with K sparing diuretics bc they harm the kidneys too Pt counseling Monitoring ***excretion from body can take 1 year!!!-> need to monitor whole time*** Monitor BUN Creatinine - CLASS: AZOLES Class Azole Uses BROAD spectrum antifungal Use this before amphotericin B Dose and Route Can be given PO (lower toxicity) Drug interactions Interacts with alot of drugs Antacids inhibit/increases levels of other drugs Itraconazole (sporanox) Ketoconazole (nizoral) Fluconazole (diflucan) **#1 azole given** Clotrimazole SKIN Inhibits synthesis of ergosterol -> increases permeability and leakage of cellular components Active against most fungi that cause systemic mycosis and superficial infections Dermatophytes Candida species Inhibits synthesis of ergosterol -> increases permeability and leakage of cellular components Dermatophytic infections and candidiasis of the skin, mouth, throat and vagina Can be taken PO: Safer than amphotericin B a/e Used for Blastomycosis Histoplasmosis Meningitis caused by cryptococcus neoformans Coccidioides immitis vaginal , oropharyngeal, esophageal, disseminated candida a/e DOC for - Blastomycosis Histoplasmosis Paracoccidioidomycosis Sporotrichosis a/e GI n/v, diarrhea Rash HA Abdominal pain Edema **cardiac suppression and liver injury Look at LFT Look at ejection fraction - n/v (give drug with food) Hepatotoxicity Sex hormones impacted Rash, itching Dizziness Fever Chills Constipation Diarrhea Photophobia HA **inhibits CYP3A4 and can increase levels of other drugs a/e - - - Topical administration Stinging Erythema Edema Urticaria Pruritis Peeling Intravaginal Burning Lower ab. Cramps Serious birth defects in 1st trimester to face **inhibits CYP3A4 and can increase levels of other drugs -> wafarin, phenytoin etc. **try this one before Ketoconazole PO bc of the toxicity rt po use CLASS: POLYENE NYSTATIN (Mycostatin) Class Polyene MOA Uses DOC for intestinal candidiasis or oral, but can tx candida infections off the… Skin Mouth Esophagus Vagina If in skin folds-> use powder to avoid adding more moisture Dose and Route When giving PO have pt either swish and spit out or swish and swallow **better to swallow so it coats whole oral cavity Adverse effects Oral GI problems n/v Topical Local irritation Drug interactions Warnings/ contraindicatio ns - Pt counseling Monitoring -