Week 4 Flashcards
Types of Natural Pencillin
- Penicillin G aqueous
- Penicillin G procaine and benathine
- Penicillin V (PenVeek, Vi-CillinK
Types of Amino Penicillin
- amoxixillin (Amoxil)
- ampicillin (Omipen)
Antistaphylococcal Penicillin
dicloxacillin (Dynapen)
nafcillin (Nafcil, Unipen)
oxacillin (Prostaphlin)
Antipseudomonal Penicillin
pipercillin (Piperacil)
ticarcillin (Ticar)
B-Lacatamase inhibtors
Ampicillin/sulbactam (unasyn)
amoxicillin/clavulanate (Augmentin)
piperacillin/tazobactam (Zosyn)
ticarcillin/clavulante (Timentin)
1st Generation Cephalosporins
Cefadroxil (druicef) PO
Cefazolin (Ancef, Kefzol) INJ
Cephalexin (Keflex) PO
2nd Generation Cephalosporins
Cefaclor (Ceclor) cefotetan (Cefotan) cefoxitin (Mefoxin) cefprozil (Cefzil) cefuroxime (Zinacef) cefuroxime axetil (Ceftin)
3rd Generation Cephalosporins
cefdinir (Omnicef) cefditoren (Spectracef) cefixime (Suprax) cefotaxime (Clarforan) cefpodoxime (Vantin) ceftazidime (Fortaz) cefibuten (Cedax) ceftriaxone (Rocephine)
Penicillin: Mechanism of action
Interfere with bacterial cell wall synthesis
bind to peptidoglycan layer causing bacterial cell lysis and death
Penicillin: Mechanism of Resistance
1) B-Lactamase/Penicillinase
2) Modified PBP’s (decreased affinity for PCN)
3) Decreased permeability (Gram negative external surfaces that reduce drug permeability)
Types of Macrolides
azithromycin (Z-Pak, Zithromax)
clarithromycin (Biaxin)
erythromycin (multiple brands)
Macrolides: Mechanism of action
inhibits bacterial ribosomal protein synthesis
Macrolides: Antibacterial Spectrum
Respiratory/genital infections (if pt. allerigic to PCN)
Otitis media
Community acquired pneumonia
Pelvic infections caused by Chlamydia trachomatis
Topical for acne
Whooping Cough
Macrolides: ADR
GI intolerance (most common) Cholestatic jaundice Abnormal taste sensations Prolonged QT interval
Drug responsible for metal taste in mouth
Clarithromycin
Antipseudomonal Penicillins: Spectrum Diseases
Nosocomial pneumonia, nosocomial UTI, complicated cellulitis, abdominal infections
Drug interactions with erythromycin and clarithromycin
theophylline warfarin antifungals statins seizure drugs detrol digoxin
Caution with macrolides in patients with what?
Severe hepatic dysfunction
Macrolides: off label uses
erythromycin used to treat diabetic gastroparesis by increasing GI motility and gastric emptying
List of tetracyclines
demeclocycline (Declomycin)
doxycycline (Vibramycin)
minocycline (Minocin)
tetracycline (Sumycin)
Natural Penicillin: Spectrum of Bacteria/Pathogens
Bacteria-Gram Positive Cocci
Pathogens- Strep Viridans, Strep pyogenes, strep pneumonia
Natural Penicillin: Spectrum Diseases
Syphilis, endocarditis, pneumonia, strep throat, group B strep infections
Amino Penicillins: Spectrum of Bacteria/Pathogens
Bacteria- Both gram positive and gram negative
Pathogens- haemophilus influenzae, strep pneumonia, E. coli, proteus mirabilis, enterococcus
Amnio Penicillins: Spectrum Diseases
Sinusitis, throat infections, otitis media, UTI’s
Antipseudomonal Penicillins: Spectrum of Bacteria/Pathogens
Bacteria- gram negative bacilli/rods
Pathogens- pseudomonas aeruginosa, serratia, klebsiella
Antipseudomonal Penicillins: Diseases
Nosocomial pneumonia, nosocomial UTI, complicated cellulitis, abdominal infections
Tetracyclines: Mechanism of Action
inhibits bacterial ribosomal protein synthesis
Tetracyclines: Spectrum
Community acquired pneumonia lyme's disease, rocky mountain spotted fever, tularemia, anthrax treatement pelvic infections acne MRSA
Best drug to treat CAP
Docycycline
Pelvic infection caused by
Chlamydia trachomatis
Tetracyclines :pharmacokinetics
high concentrations achieved in body organs, skin, bone and teeth
Tetracyclines: pharmacokinetics
Metabolized in liver first, then excreted by kidneys
Crosses placenta and excretes into breast milk
Tetracyclines: drug interactions
Chelate with 2+ and 3+ cations (Ca2+, Fe3+)
antacids, multivitamins
milk, cheese
Tetracyclines: ADR
GI intolerance
Photosensitivity
Teeth discoloration
Hypersensitivity reactions
Fatal hepatic toxicity at high doses (rare)
inhibit skeletal growth in developing fetus during pregnancy
Clindamycin: Mechanism of Action
inhibits bacterial ribosomal protein synthesis
Clindamycin: ADR:
hypersensitivity reactions
high incidence of causing Clostridium difficile
Cause non-Clostridium difficile diarrhea, N/V
Clindamycins: Spectrum
excellent anaerobic and gram+ coverage
almost no gram - coverage
alternative to PCN and cephalosporins where gram+ coverage is needed
Clindamycins: commonly used
Diabetic foot cellulitis where gram- not suspected
skin and soft tissue infections w/ PCN allergy
Mild aspiration pneumonias where anaerobe may be present
acne
Staphylococcus aureus (CA-MRSA)
B-Lactamase Inhibitor Combinations: Spectrum of Bacteria/Pathogens
Bacteria- gram positive, enhanced gram negative and anaerobic coverage
Pathogens- “anything that’s stinky”
B-Lactamase Inhibitor Combinations: Spectrum Diseases
diabetic foot ulcers, abscesses, animal bites, abdominal infections, anaerobic infections, polymicrobial infections
Antistaphylococcal Penicillins: Spectrum of Bacteria/Pathogens
Bacteria- gram positive
Pathogens- staph aureus, other staph strains
Antistaphylococcal Penicillins: Spectrum Diseases
Soft tissue and bone infections, endocarditis
Antifolate Drugs: Sulfa Drugs/Sulfonamides
Mafenide Silver sulfadiazine (Silvadene) Sulfacetamide (Cetamide) Sulfadiazine (Microsulfon) Sulfamethoxazole (Bactrim component) Sulfisoxazole (Gantrisin) Triple sulfa vaginal cream (Sultrin)
Antifolate Drugs: Sulfa Drugs: Mechanism of Action
Sulfonamides use up much of the enzyme needed to convert PABA to folic acid, thus decreasing folic acid production.
Antifolate Drugs: Sulfa Drugs: Pharmacokinetics
Well absorbed orally. Distributes throughout body water. Highly protein bound. Metabolized in the liver. Excreted renally.
Antifolate Drugs: Sulfa Drugs: Drug Interactions
With other highly protein bound drugs e.g. warfarin and phenytoin (Dilantin)
Antifolate Drugs: Sulfa Drugs: ADR
Hypersensitivity Reactions
Nephrotoxicity
GI upset, diarrhea
Kernicterus: sulfonamides displace bilirubin from protein binding sites
Rare: aplastic anemia, pancreatitis, thrombocytopenia
Persons allergic to sulfonamides may have cross sensitivity with these medications
Celecoxib (Celebrex) Furosemide (Lasix) Hydrochlorothiazide sulfasalazine (Azulfidine) Zonisamide (Zonegram) Glyburide & Glipizide sulfonylureas
If you are allergic to sulfonamide Rx, then which 3 drugs will the pharmacist call you on (to tell you, you cannot administer these drugs)?
Celecoxib (Celebrex)
Sulfasalazine (Azulfidine)
Zonisamide (Zonegram)
Antifolate Drug: Trimethoprim: Mechanism of Action
Dihydrofolate reductase inhibitor. Dihydrofolate reductase converts folic acid to its active form, tetrahydrofolic acid
Antifolate Drug: Trimethoprim: Pharmacokinetics
Similar to sulfonamides: Well absorbed orally. Distributes throughout body water. Highly protein bound. Metabolized in the liver. Excreted renally.
Antifolate Drug: Trimethoprim: ADR
can produce effects of folate deficiency if given in very high doses
Co-Trimoxazole (Bactrim, Septra): Mechanism of Action
Synergy: shows greater antimicrobial activity than equivalent quantities of either drug used alone
Inhibits 2 sequential steps in the synthesis of active folic acid
Co-Trimoxazole (Bactrim, Septra): ADR
Hypersensitivity Reactions
Nephrotoxicity
GI upset, diarrhea
Kernicterus: sulfonamides displace bilirubin from protein binding sites
Rare: aplastic anemia, pancreatitis, thrombocytopenia
Can produce effects of folate deficiency if given in very high doses
Co-Trimoxazole (Bactrim, Septra): Drug Interactions
With other highly protein bound drugs e.g. warfarin & phenytoin (Dilantin)
Co-Trimoxazole (Bactrim, Septra): Therapeutic Indications
UTI
Prostate Infections
Otitis media, sinusitis, & other resp. infections
Tx & prophylaxis Pneumocystis jiroveci pneumonia
CA-MRSA
What are the main pathogens that Bactrim & Septra target?
Serratia M. catarrhalis H. influenza L. monocytogenes P. mirabilis E. coli
What pathogen is most common in a UTI?
E. coli
ketoconazole: Mechanism of action
alters permeability of fungal cell wall & inhibits several fungal enzymes that causes toxin build up in fungal cell
ketoconazole: Therapeutic uses
OTC dandruff shampoo
orally for systemic fungal infections of lung, bone, skin, ect.
ketoconazole: systemic fungal infections are caused by what?
Blastomyces dermatitidis, Candida albicans, Coccidioides immitis, Histoplasma capsulatum
ketoconazole: pharmacokinetics
1) requires an acidic environment for adequate absorption 2) food, antacids, H2-blockers and proton pump inhibitors impair oral absorption
ketoconazole: drug interactions
significant cytochrome p450 interactions
Ketoconazole: adverse drug reactions
GI upset, N/V, diarrhea, rash
endocrine effects - can inhibit sex steroid synthesis
black box warning: fatal hepatic toxicity can occur
fluconazole: mechanism of action
same as itraconazole: decreases ergosterol synthesis and inhibits cell membrane formation
fluconazole: therapeutic uses
IV & oral: oral and esophageal candidiasis (thrush)
oral: single oral dose effectively treats vulvovaginal candidiasis (yeast infection)
IV & oral: systemic fungal infections of lung, bone, skin
fluconazole: drug interactions
Significant cytochrome p450 interactions
fluconazole: adverse drug reactions
GI upset, N/V, headache, diarrhea, rash
fatal hepatic toxicity can occur
itraconazole: mechanism of action
same as fluconazole: decreases ergosterol synthesis and inhibits cell membrane formation
itraconazole: oral therapeutic use
onychomycosis of the fingernail and toenails
itraconazole: pharmacokinetics
1) capsules and oral solution are not bioequivalent
2) requires acidic environment for absorption
3) food, antacids, H2-blockers and proton pump inhibitors impair oral absorption
itraconazole: drug interactions
significant cytochrome p450 interactions
itraconazole: adverse drug reactions
GI upset, N/V, diarrhea, rash
fatal hepatic toxicity can occur
black box warning: rase cases of serious CV adverse events have occurred. Cation with pts with left ventricular dysfunction or CHF
posaconazole: therapeutic uses
oral: treats thrush in patients refractory to other “azoles”
Prophylaxis of invasive Candida and Aspergillus infections in immunocompromised patients
List the quinolones
ciprofloxacin, gemifloxacin, levofloxacin, lomefloxacin, moxifloxacin, norfloxacin, ofloxacin, sparfloxacin
Quinolone mechanism of action
inhibit the replication of the bacteria by interfering with 2 bacterial enzymes, DNA gyrase and topoisomerase
First line quinolones for community-acquired pneumonias
Levofloxacin and moxifloxicin
most common pathogens for community-acquired pneumonia
Streptococcus pneumonia Haemophilus influenzae Chlamydia pneumoniae Mycopolasma pneumoniae Legionella pneumoniae
Quinolone coverage of bacteria (in general)
excellent gram negative coverage
some gram positive coverage
almost no anaerobic coverage
Quinolone of choice for pseudomonas coverage
Ciprofloxacin
Quinolone spectrum
UTI, prostate infections, CAP, pseudomonas infections, pelvic infections caused by chlamydia trachomatis, anthrax, some skin and soft tissue infections
Quinolone pharmacokinetics
excellent oral absorption, distributes into bone and prostate, high levels in lungs and urine
Quinolone ADRs
GI upset, diarrhea, nausea, hypersensitivity reactions, CNS side effects, prolonged QT interval (torsades), tendon ruptures, bone development abnormalities,
Quinolones are contraindicated in which patients?
pregnancy, breast-feeding, and children under age 18 b/c of bone development abnormalities
griseofulvin: mechanism of action
inhibits fungal cell mitosis at metaphase
griseofulvin: therapeutic uses
treatment of susceptible tinea infections of skin, hair and nails
Vulvovaginal Candidiasis (uncomplicated): choosing which pharmacologic treatment
Therapy is personal preference - cure rates are similar among products. Immediate relief is better achieved with topical products rather than oral.
Metronidazole therapeutic uses
DOC for clostridium difficile, good anerobic coverage (abdominal infections, aspiration pnneumonia), protozoal infections
Metronidazole ADR
N/V, headache, metallic taste, anorexia, vertigo, insomnia, seizure
Metronidazole Drug Interactions
Disulfuram reaction with alcohol–severe N/V and abdominal cramps, avoid alcohol during therapy and up to 24 hours after last dose
Nitrofurantoin mechanism of action
inhibits various bacterial enzymes
Oropharyngeal Candidiasis (OPC): treatment for low risk patients
topical antifungals are first-line therapy for OPC
Nitrofurantoin ADR
Discoloration of urine, GI disturbances, hypersensitivity reactions, pulmonary toxicity
Which “big-gun” antifungal is a member of the azole family and often reserved for azole-resistant infections?
voriconazole
Which “big-gun” antifungal is almost always used with other antifungals?
flucytosine
Tinea infections: pathophysiology
1) Infection does not involve living tissue but the superficial layers of skin only
What is Butenafine cream (Lotrimin Ultra) used for?
superficial dermatological fungal infections
What are the OTC antifungals for superficial mycoses?
Butenafine, Butoconazole, Clotrimazole, Miconazole, Nystatin, Terbinafine, Terconazole, Ticonazole, Tolnaftate
Vulvovaginal Candidiasis: pathogens
primarily Candida albicans (90%)
Recurrent Vulvovaginal Candidiasis is more common in what groups of people? (3)
immunocompromised
uncontrolled diabetes
pregnancy
What kinds of alterations in the vaginal environment can increase risk of Vulvovaginal Candidiasis?
pH changes, stress, hormone changes, sexual activity, pregnancy, contraceptive use, douches, antibiotics
Vulvovaginal Candidiasis: non-pharmacologial treatment
1) keep genital area clean and dry, avoid hot tubs
2) avoid constrictive clothing, wear cotton
3) avoid soaps and perfumes in genital area
Community-Acquired Pneumonia (CAP): treatment of adult outpatient co-morbidities
levofloxacin alone, moxifloxacin alone, or a combination of azithromycin, clarithromycin, or doxycycline PLUS either high dose amoxicillin or high dose amox/clavulanate
Pharmacologic Treatment of Recurrent VVC
14 days of an intravaginal product or 2 doses of fluconazole 3 days apart may be used followed by 6 months long-term suppressive therapy
Oropharyngeal Candidiasis (OPC) and Esophageal Candidiasis: pathogens
Candida albicans causes 80% of OPC and esophageal candidiasis
Oropharyngeal Candidiasis (OPC) and Esophageal Candidiasis: epidemiology
1) often occurs in infants, elderly, & immunocompromised
2) 1/3 to 1/2 of older adults develop OPC
Oropharyngeal Candidiasis (OPC) and Esophageal Candidiasis: etiology
1) Most commonly reported ADR of inhaled corticosteroids (37% occurrence)
2) Most common opportunistic infection of HIV patients (80-90% will develop at some time) and is
an extremely common initial manifestation of the disease
Oropharyngeal Candidiasis (OPC) and Esophageal Candidiasis: treatment for low risk patients
topical antifungals are first-line therapy for OPC
Oropharyngeal Candidiasis (OPC): treatment for severe or unresponsive cases
systemic antifungals
Esophageal Candidiasis: treatment
aggressive systemic antifungal therapy
Tinea infections: epidemiology & etiology
1) Tinea infections are second only to acne in frequency of reported skin disease
2) Of all the forms of tinea, tinea pedis is the most common
Tinea infections: pathophysiology
1) Infection does not involve living tissue but the superficial layers of skin only
What are the specific non-pharmacological treatment for Tinea pedis
Change socks two to three times daily and wear protective footwear in public showers & pool areas
Tinea infections: What do you tell pts about topical antifungal treatment?
Apply topically at least 1 inch beyond affected area. Continue tx at least 1 to 2 weeks after clearing
Onychomycosis: treatment
Oral antifungals are required x at least 3 months for toenails and at least 2 months for fingernails.
five classifications of pneumonia
1) Community-acquired pneumonia, 2) Aspiration
pneumonia, 3) Hospital-acquired pneumonia, 4) Ventilator-associated pneumonia, and 5) Healthcare-associated pneumonia
Community-Acquired Pneumonia (CAP): most common pathogen (25-70%)
steptococcus pneumoniae
Community-Acquired Pneumonia (CAP): treatment of adult outpatient otherwise healthy
azithromycin, clarithromycin, erythromycin, or
doxycycline; alternatives include levofloxacin or moxifloxacin
Community-Acquired Pneumonia (CAP): treatment of adult outpatient co-morbidities
levofloxacin alone, moxifloxacin alone, or a combination of azithromycin, clarithromycin, or doxycycline PLUS either high dose amoxicillin or high dose amox/clavulanate
Community-Acquired Pneumonia (CAP): treatment of Pediatric outpatient:
azithromycin or clarithromycin; alternatives include high dose amoxicillin, high dose amoxicillin/clavulanate, or IM ceftriaxone
Community-Acquired Pneumonia (CAP): duration of treatment
Azithromycin - 5 days
Levofloxacin when dosed at 750mg daily - 5 days
all other antibiotics - 7 to 10 days
Gonorrhea: pathogen
Neisseria gonorrhoeae (gram-negative diplococci)
A pt who tests positive for gonorrhea should also be tested for which other STIs?
Chlamydia trachomatis, syphillis, and HIV
Antibiotic tx for gonorrhea should also include coverage against what? With which 2 drugs?
Coverage against Chlamydia trachomatis with Azithromycin or Doxycycline
Gonorrhea: Which class of drugs should you not use in individuals w/ a hx of recent travel to foreign countries w/ known resistance or in men who have sex w/ men?
Fluoroquinolones
Gonorrhea: uncomplicated tx of infx of the cervix, urethra, rectum, or pharynx
ceftriaxone IM plus azithromycin or doxycycline (dual gonococcal coverage + chlamydial coverage)
Gonorrhea: tx in pregnant women
ceftriaxone IM plus azithromycin
Gonorrhea: tx ophthalmic neonatorum prophylaxis
either erythromycin or tetracycline ophthalmic ointment single application
Gonorrhea: tx for cases of severe cephalosporin allergy
azithromycin orally
Chlamydia: pathogen
Chlamydia trachomatis
Chlamydia: best tx options
azithromycin 1g single dose
doxycycline 100mg q12h x 7 days
Chlamydia: other tx alternatives
erythromycin x 7 days
levofloxacin x 7 days
Chlamydia: tx in pregnancy
AVOID fluoroquinolones and tetracyclines!
Macrolides are preferred and Amoxicillin can be an alternative.
Chlamydia: tx of ophthalmic or lung infx in neonates
erythromycin oral x 14 days
Syphillis: pathogen
Treponema pallidum (a spirochete/gram-negative bacteria)
Syphillis: prominence
black men and men who have sex w/ men
Syphillis: primary symptoms
solitary, painless cancre at the site of the infx about 3 wks after exposure
Syphillis: secondary symptoms
systemic symptoms: fatigue, diffuse rash, fever, lymphadenopathy, and genital condyloma latum (flat, wart-like growths)
Syphillis: infx rates in infants to infected mothers
nearly 100%
Syphillis: preferred tx
Benzathine penicillin G IM. Dose & duration vary depending upon stage and HIV status.
Syphillis: alternatives in PCN allergy
ceftriaxone IM, doxycycline, minocycline, tetracycline, erythromycin, or azithromycin
Trichomoniasis: pathogen
Trichomonas vaginalis
Trichomoniasis: tx
Metronidazole or tinidazole
Bacterial Vaginosis: pathogen
Gardenella vaginalis, Prevotella sp., Mycoplasma hominis, and Mobiluncus sp.
Bacterial Vaginosis: tx
oral or intravaginal metronidazole or clindamycin
Pelvic Inflammatory Disease (PID): pathogens
Chlamydia trachomatis
Neisseria gonorrheoeae
Possible anaerobes (Bacteroides, Peptostreptococci)
Possible gran-negative rods (Haemophilus, E. coli)
PID: outpatient tx
ceftriaxone IMx1 + doxycycline x 14 days +or- metronidazole x 14 days
PID: alternative outpatient tx
ceftriaxone can be replaced w/ cefotetan IMx1 + probenecid x 1
PID: inpatient tx
cefotetan IV or cefoxitin IV + doxycycline po or IV
clindamycin IV + gentamicin IV + doxy +or- metronidzole