Major Classes of Antibiotics Flashcards
Group of powerful antibiotics used to
treat serious infections caused by
gram-negative aerobic bacilli
Aminoglycosides
amikacin, gentamicin, kanamycin,
neomycin, streptomycin, tobramycin
Aminoglycosides
Therapeutic Actions and Indications for Aminoglycosides.
- Inhibit protein synthesis in susceptible strains of gram-negative bacteria
- Irreversibly bind to a unit of a bacteria ribosome. Leading to misreading of a genetic code and cell
death - Treat serious infections caused by susceptible strains of gram-negative bacteria (Pseudomonas
auruginosa, E. coli, Proteus species, Kleibsiella Enterobacter-Serratia group, Citrobacter Species,
and Staphylococcus aureus)
Pharmacokinetics of Aminoglycosides
Are poorly absorbed from the GI tract but rapidly absorbed after intramuscular (IM) injections
Contraindications and Cautions for Aminoglycosides
- Known allergy; Renal or hepatic disease; Preexisting hearing loss; Active herpes or mycobacterial infection; Myasthenia gravis or parkinsonism; Lactation
- Do not use for longer than 7 to 10 days
Adverse effects of Aminoglycosides
- CNS: Ototoxicity (deafness, vestibular paralysis), confusion, depression, disorientation, and numbness, tingling, and weakness
- Nephrotoxicity
- GI effects: nausea, vomiting, diarrhea, weight loss, stomatitis, and hepatic toxicity
- Cardiac: palpitations, hypotension, and hypertension
- Hypersentivity: purpura, rash, urticarial, and exfoliative dermatitis
Clinically important drug-drug interactions for Aminoglycosides
- Synergistic bactericidal effect when given with penicillin,
cephalosporins, or ticarcillin - Avoid combining with diuretics, anesthetics
- Are relatively new class of broad-spectrum antibiotics effective against gram-positive and gram-negative bacteria
- meropenem, diropenem, ertapenem, imipenemclistatin
Carbapenems
Therapeutic Actions and Indications for Carbapenems
- Bactericidal
- Inhibit cell membrane synthesis in susceptible bacteria, leading to
cell death - Treat serious infections caused by susceptible strains of S. pneumoniae,Haemophilus influenzae, Moraxella catarrhalis, S.
aureus, Streptococcus pyogenes, E. coli, Peptostreptococcus,
Klebsiella pneumoniae, Clostridium clostridiiforme, Eubacterium
lentum, Bacteroides fragilis, Bacteroides distasonis, Bacteroides
ovatus, Bacteroides thetaiotamicron,, Bacteroides uniformis,
Proteus mirabilis, P. aeruginosa, Acinetobacter baumannii,
Streptococcus agalactiae, Porphyromonas asaccharolytica,
Prevotella bivia - Indicated for treatment of serious intra-abdominal, urinary tract, skin
and skin structure, bone and joint and gynecological infections
Pharmacokinetics of Carbapenems
Rapidly absorbed if given IM
- Contraindications and cautions of Carbapenems
- Known allergy; seizure disorders; meningitis; lactation
- Not for use in patients younger than 18 years old (ertapenem)
- Used with caution in patients with inflammatory bowel disorders (meropenem)
Adverse effects of Carbapenems
- GI: pseudomembranous colitis, Clostridium difficile diarrhea, and nausea and vomiting
- Superinfections
- CNS: headache, dizziness, and altered mental
state
Clinically important drug-drug interactions for Carbapenems
- Not used with Valproic acid
- Avoid using imipenem with vganciclovir
- Avoid using meropenem with probenecid
What major class of Antibiotic has 4 generations?
Cephalosporins
- Effective against gram-positive bacteria that are affected by penicillin G, as well as the gram-negative
bacteria P. mirabilis, E. coli, and K. pneumoniae - cefadroxil, cefazolin, cephalexin
First generation of Cephalosporins
- Effective against previously mentioned strain as well
as H. influenza, Enterobacter aerogenes, and Neisseria species - cefaclor, cefoxitin, cefprozil, cefuroxime
Second generation of Cephalosporins
- Effective against all of the previously mentioned strains, as well as gram-negative bacilli Serratia marcescens
- cefdinir, cefotaxime, ceftibuten, ceftizoxime, ceftriaxone
Third generation cephalosporins
- active against gram-negative and gram-positive organisms including cephalosporin resistant staphylococci
and P. aeruginosa - cefditoren, ceftaroline, cefipime
Fourth generation cephalosporins
Therapeutic Actions and Indications for
Cephalosporins
- Bactericidal and bacteriostatic
- Interfere with cell wall-building ability of bacteria when they divide, that is, they prevent the bacteria from
biosynthesizing the framework of their call walls. The bacteria with weakened cell walls swell and burst as a
result of osmotic pressure within the cell. - Indicated for the treatment of infections caused by susceptible bacteria
Pharmacokinetics of: Cephalosporins
Well absorbed from the GI tract, some IM or IV administration
Contraindications and Cautions for: Cephalosporins
Pharmacokinetics
Adverse effects of: Cephalosporins
- GI: nausea, vomiting, diarrhea, anorexia, abdominal pain, and flatulence, pseudomembranous colitis, bloody diarrhea or abdominal pain
- CNS: headache, dizziness, lethargy, and paresthesias
- Nephrotoxicity, superinfections
Clinically important drug-drug interactions for: Cephalosporins
- Cephalosporins and aminoglycosides increases risk for nephrotoxicity (check BUN and creatinine levels)
- May increase bleeding if given with anticoagulants
- Avoid alcohol for 72 hours after discontinuing the drug
Therapeutic Actions and Indications for: Fluoroquinolones
- interfere with the action of DNA enzymes necessary for the growth and reproduction of the bacteria leading to cell death
- indicated for treating infections caused by susceptible strains of gram-negative bacteria, including E. coli, P.
mirabilis, K. pneumoniae, Enterobacter cloacae, Proteus vulgaris, Proteus rettgeri, Morganella morganii, M. catarrhalis, H. infl uenzae, H.
parainfluenzae, P. eruginosa, Citrobacter freundii, S. aureus, Staphylococcus epidermidis, some Neisseria gonorrhoeae, and group D streptococci infections
frequently include urinary tract, respiratory tract, and
skin infections - anthrax infection, typhoid fever
Pharmacokinetics of: Fluoroquinolones
Absorbed in the GI tract, metabolized in the liver, and excreted in the urine and feces
Contraindications and Cautions for: Fluoroquinolones
- Known allergy; pregnant and lactating
patients - Caution with renal dysfunction
Adverse effects of: Fluoroquinolones
- CNS: Headache, dizziness, insomnia, and depression
- GI: nausea, vomiting, diarrhea, and dry mouth
- Tendinitis and Tendon rupture
- Immune: bone marrow depression
- Others: fever, rash, and photosensitivity
Clinically important drug-drug interactions for: Fluoroquinolones
- Decreased with iron salts, sucralfate, mineral supplements, or antacids
- Cardiac reactions: quinidine, procainamide, amiodarone, sotalol, erythromycin, terfenadine,
pentamidine, tricyclics, phenothiazines) - Increased theophylline levels if taken together
- Increased tendonitis and tendon rupture with corticosteroid
was the first antibiotic introduced for clinical use.
Penicillin and Penicillinase Resistant antibiotics
He used Penicillium molds to produce the original penicillin in the 1920s.
Sir Alexander Fleming
penicillin G benzathine, penicillin G potassium, penicillin G procaine, penicillin V, amoxicillin,
and ampicillin
Penicillin and Penicillinase Resistant antibiotics
Therapeutic Actions and Indications for: Penicillin and Penicillinase Resistant antibiotics
- Produce bactericidal effects by interfering with the ability of susceptible bacteria to build their cell
walls when they are dividing - indicated for the treatment of streptococcal infections, including pharyngitis, tonsillitis, scarlet
fever, and endocarditis; pneumococcal infections; staphylococcal infections; fusospirochetal infections; ratbite fever; diphtheria; anthrax; syphilis; and uncomplicated gonococcal infections,
meningococcal meningitis
Pharmacokinetics of: Penicillin and Penicillinase Resistant antibiotics
- rapidly absorbed from the GI tract, reaching peak levels in 1 hour. They are sensitive to the gastric acid levels in the stomach and should be taken on
an empty stomach to ensure adequate absorption
Contraindications and Cautions for: Penicillin and Penicillinase Resistant antibiotics
- Known allergy
- Caution with renal dysfunction
Adverse effects of: Penicillin and Penicillinase Resistant antibiotics
- GI: nausea, vomiting, diarrhea, abdominal pain, glossitis, stomatitis, gastritis, sore mouth, and furry
tongue - Hypersensitivity: fever, rash, wheezing and anaphylaxis
Clinically important drug-drug interactions for: Penicillin and Penicillinase Resistant antibiotics
- Decreased with tetracycline
- Inactivation of aminoglycosides if given together
- Drugs that inhibit folic acid synthesis
- sulfadiazine, sulfasalazine, cotrimoxazole
Sulfonamides
Therapeutic Actions and Indications for: Sulfonamides
- competitively block paraaminobenzoic acid to prevent the synthesis of folic acid in susceptible bacteria that synthesize their own folates for the
production of RNA and DNA - gram-negative and gram-positive bacteria such as Chlamydia trachomatis and Nocardia and some strains of H. influenzae, E. coli, and P. mirabilis
- treatment for UTIs and trachoma, nocardiosis,
STD’s
Pharmacokinetics of: Sulfonamides
absorbed from the GI tract, metabolized in the liver, and excreted in the urine.
Contraindications and Cautions for: Sulfonamides
- Known allergy, pregnancy and lactation
- Caution with renal disease or history of kidney stones
Adverse effects of: Sulfonamides
- GI: nausea, vomiting, diarrhea, abdominal pain, anorexia, stomatitis, and hepatic injury
- Renal: crystalluria, hematuria, and proteinuria, nephrotic syndrome, toxic nephrosis
- CNS: headache, dizziness, vertigo, ataxia, convulsions, and depression
- Bone marrow depression
- Dermatologic: photosensitivity and rash
Clinically important drug-drug interactions for: Sulfonamides
- tolbutamide, tolazamide, glyburide, glipizide, or chlorpropamide increases hypoglycemia
- cyclosporine increases nephrotoxicity
- were developed as semisyntheticantibiotics
based on the structure of a common soil mold. They are composed of four rings, thus its name. - tetracycline, demeclocycline, doxycycline, minocycline
Tetracycline
Therapeutic Actions and Indications for: Tetracycline
- work by inhibiting protein synthesis in a wide range of bacteria,
leading to the inability of the bacteria to multiply - infections caused by Rickettsiae, Mycoplasma pneumoniae,
Borrelia recurrentis, H. influenzae, Haemophilus ducreyi,Pasteurella
pestis, Pasteurella tularensis, Bartonella bacilliformis, Bacteroides
species, Vibrio comma, Vibrio fetus, Brucella species, E. coli, E.
aerogenes, Shigella species, Acinetobacter calcoaceticus,
Klebsiella species, Diplococcus pneumoniae, and S. aureus;
against agents that cause psittacosis, ornithosis, ymphogranuloma
venereum, and granuloma inguinale; when penicillin is
contraindicated in susceptible infections; and for treatment of acne
and uncomplicated GU infections caused by C. trachomatis - adjunct to protozoal infections
Pharmacokinetics of: Tetracycline
- absorbed adequately, but not completely, from the GI tract. Their absorption is affected by food, iron,
calcium, and other drugs in the stomach. - concentrated in the liver and excreted unchanged in the urine
Contraindications and Cautions for: Tetracycline
- Known allergy, pregnancy and lactation
- Ophthalmic preparation is contraindicated in patients with fungal, mycobacterial, or viral ocular
infections - Used with cautions in children below 8 years old, hepatic or renal dysfunction
Adverse effects of: Tetracycline
- GI: nausea, vomiting, diarrhea, abdominal pain, glossitis, and dysphagia
- Fatal hepatotoxicity
- Skeletal: damage to teeth and bones
- Dermatologic: photosensitivity and rash
Clinically important drug-drug interactions for: Tetracycline
- Decrease effectiveness of penicillin G and oral contraceptives
- Increased digoxin toxicity
- Decreased absorption with from combination with calcium salts, magnesium salts, bismuth salts,
iron, urinary alkalinizers, and charcoal
Clinically important drug-food interactions
Administer on an empty stomach
the group of bacteria that contain the pathogens that cause tuberculosis and leprosy are classified on the basis of their ability to hold a stain even in
the presence of a “destaining” agent such as acid. Because of this property, they are called “acidfast” bacteria.
Mycobacteria
What type of Antibiotic is against Mycobacteria? And is also a Antituberculosis Drug.
Antimycobacterials
Tuberculosis can lead to serious damage in the lungs, the GU tract, bones, and the meninges.
Because M. tuberculosis is so slowly growing, the treatment must be continued for (answer).
6 months to 2
years
First line of Antimycobacterials
soniazid, rifampin, pyrazinamide,
ethambutol, streptomycin, rifapentine
Second line of Antimycobacterials
ethionamide, capreomycin,
cycloserine, and rifabutin
Pharmacokinetics of: Antimycobacterials
Generally well absorbed from the GI tract. These drugs, given orally, are metabolized in the liver and excreted in the urine.
Contraindications and Cautions for: Antimycobacterials
Known allergy, hepatic and renal failure,
pregnancy
Adverse effects of: Antimycobacterials
- CNS: neuritis, dizziness, headache, malaise, drowsiness, and hallucinations
- GI: nausea, vomiting, anorexia, stomach upset, and abdominal pain
- Rifampin, rifabutin, and rifapentine: discoloration of body fluids- orange-tinge (urine, sweat, tears)
Clinically important drug-drug interactions for: Antimycobacterials
- Increased toxic liver reaction with INH and rifampin
- Increased metabolism and decreased drug effectiveness with quinidine, metoprolol, propranolol, corticosteroids, oral contraceptives,
oral anticoagulants, oral antidiabetic agents, digoxin, theophylline, methadone, phenytoin, verapamil, cyclosporine, or ketoconazole in
combination with rifampin or rifabutin
- Was first introduced in 2004
- Telithromycin
Ketolides
Therapeutic Actions and Indications for: Ketolides
- block protein synthesis within susceptible bacteria, leading to cell death
- effective against S. pneumoniae, including certain multidrug-resistant strains, H. influenzae, M.
catarrhalis, Chlamydophila pneumoniae, and M.pneumoniae
Pharmacokinetics of: Ketolides
Rapidly absorbed through the GI tract, reaching peak levels in 1 hour
Contraindications and Cautions for: Ketolides
- Known allergy
- with known congenital prolonged QT interval, bradycardia, or any proarrhythmic condition such as hypokalemia with concurrent use of pimozide, cardiac antiarrhythmics,
simvastatin, atorvastatin, or lovastatin and with myasthenia gravis - Use with caution with renal or hepatic impairment, pregnancy and lactating
Adverse effects of: Ketolides
- GI: nausea, vomiting, taste alterations and the potential for pseudomembranous colitis
- Hypersensitivity: anaphylaxis
Clinically important drug-drug interactions for: Ketolides
- Serious adverse effects with pimozide,
simvastatin, lovastatin, or atorvastatine - Increased serum level of digoxin and metoprolol
- Decreased serum levels with rifampin, phenytoin, carbamazepine, or phenobarbital
- Increase GI toxicity with theophylline
- similar to the macrolides but are more toxic
- clindamycin, lincomycin
Lincosamides
Therapeutic Actions and Indications for: Lincosamides
react at almost the same site in bacterial protein synthesis and are effective against the same strains of bacteria
Contraindications and Cautions for: Lincosamides
Use with caution with renal or hepatic impairment, pregnancy and lactating
Pharmacokinetics of: Lincosamides
rapidly absorbed from the GI tract or from IM injections and are metabolized in the liver and excreted in the urine and feces
Adverse effects of: Lincosamides
- GI: fatal pseudomembranous colitis
- Pain, skin infections, and bone marrow depression
- First introduced in 2010
- televancin
Lipoglycopeptides
Therapeutic Actions and Indications for: Lipoglycopeptides
They inhibit bacterial cell wall synthesis by interfering with the polymerization and crosslinking of peptidoglycans. They bind to the bacterial membrane and disrupt the membrane barrier function causing bacterial cell death
Pharmacokinetics of: Lipoglycopeptides
- Available as an IV drug only
Contraindications and Cautions for: Lipoglycopeptides
- Known allergy, pregnancy and lactation
Adverse effects of: Lipoglycopeptides
- GI: nausea, vomiting, taste alterations, diarrhea, loss of appetite, and risk of C. difficile diarrhea
- Nephrotoxicity: foamy urine
- Rapid infusion can cause red man syndrome: flushing, sweating, and hypotension
Clinically important drug-drug interactions for: Lipoglycopeptides
Arrhythmias if combined with other drugs known to prolong QT interval
- are antibiotics that interfere with protein synthesis in susceptible bacteria
- erythromycin, azithromycin, clarithromycin, dirithromycin
Macrolides
Therapeutic Actions and Indications for: Macrolides
may be bactericidal or bacteriostatic, exert their effect by binding to the bacterial cell membrane and changing protein function. This action can
prevent the cell from dividing or cause cell death, depending on the sensitivity of the bacteria and the concentration of the drug.
acute infections caused by susceptible strains of S. pneumoniae, M. pneumoniae, Listeria monocytogenes, and Legionella pneumophila; infections caused by group A betahemolytic streptococci; pelvic inflammatory disease caused by N. gonorrhoeae; upper respiratory tract infections caused by H. influenzae (with sulfonamides); infections caused by
Corynebacterium diphtheriae and Corynebacterium minutissimum (with antitoxin); intestinal amebiasis; and
infections caused by C. trachomatis.
- Prophylaxis for endocarditis before dental procedures in high-risk patients with valvular heart disease who are allergic to penicillin
- Topical macrolides are indicated for the treatment of ocular infections caused by susceptible organisms and for acne vulgaris, and they may also be used prophylactically against infection in minor skin abrasions and for the treatment of skin infections caused by
sensitive organisms.
Pharmacokinetics of: Macrolides
These drugs are absorbed in the GI tract. Erythromycin is metabolized in the liver, with excretion mainly in the bile to feces. Azithromycin
and clarithromycin are mainly excreted unchanged in the urine. Dirithromycin is excreted through the
feces.
Dirithromycin is excreted through the
(answer). .
Feces
Contraindications and Cautions for: Macrolides
- Known allergy and lactation
- Ocular preparations are contraindicated for viral fungal, or mycobacterial infections of the eye
- Use with caution in patients with hepatic dysfunction and in those with renal disease
Clinically important drug-drug interactions for: Macrolides
- Increased digoxin levels when taken together
- Increased effects with anticoagulants,
theophylline, carbamazepine, or corticosteroids
and cyclosporine
Adverse effects of: Macrolides
- GI: abdominal cramping, anorexia, diarrhea, vomiting, and pseudomembranous colitis
- Neurological: confusion, abnormal thinking, and uncontrolled emotions
- Hypersensitivity: rash and anaphylaxis
Clinically important drug-food interaction: Macrolides
Should be taken on an empty stomach
Aztreonam
Monobactam Antibiotics
Therapeutic Actions and Indications for: Monobactam Antibiotics
- disrupts bacterial cell wall synthesis, which promotes leakage of
cellular contents and cell death in susceptible bacteria - indicated for the treatment of urinary tract, skin, intra-abdominal, and gynecological infections, as well as septicemia caused by susceptible bacteria, including E. coli, Enterobacter,
Serratia,Proteus, Salmonella, Providencia, Pseudomonas,
Citrobacter, Haemophilus, Neisseria, and Klebsiella.
Pharmacokinetics of: Monobactam Antibiotics
IV and IM use only and reaches peak effect levels in 1 to 1.5 hours
Contraindications and Cautions for: Monobactam Antibiotics
- Known allergy, pregnancy and lactation
- Renal or hepatic dysfunction
Adverse effects of: Monobactam Antibiotics
- GI: nausea, GI upset, vomiting, and diarrhea
- Hepatic enzyme elevation, inflammation, phlebitis, and discomfort at injection sites
Clinically important drug-drug interactions for: Monobactam Antibiotics
- Incompatible with nafcillin, cephradine, and metronidazole
