Antibiotics are agents made from living microorganisms, synthetic manufacturing, and genetic engineering that are used

to inhibit
specific bacteria. They can be bacteriostatic, bactericidal, or both. The major classes of antibiotics include: aminoglycosides,
penicillins and penicillinase-resistant drugs, sulfonamides, tetracyclines, and antimycobacterials (e.g. antitubercular and leprostatic)
Others include ketolides, lincosamides, lipoglycopeptides, macrolides, and monobactams.

Antibiotics: Generic and Brand Names

Here is a table of commonly encountered antibiotics, their generic names, and brand names:

Classification Generic Name Brand Name

Aminoglycosides amikacin Amikin

Gentamicin Garamycin
kanamycin Kantrex
neomycin Mycifradin
streptomycin generic
tobramycin TOBI, Tobrex

Carbapenems Doripenem Doribax

Ertapenem Invanz
Imipenem-cilastatin Primaxin
Meropenem Merrem IV

Cephalosporins
• First-Generation cefadroxil generic
cefazolin Zolicef
cephalexin Keflex

• Second-Generation cefaclor Ceclor

cefoxitin generic
cefprozil generic
cefuroxime Zinacef

• Third-Generation cefdinir generic

cefotaxime Claforan
cefpodoxime Vantin
ceftazidime Ceptaz, Tazicef
ceftibuten Cedax
ceftizoxime Cefizox
ceftriaxone Rocephin

• Fourth-Generation cefditoren Spectracef

cefepime Maxipime
ceftaroline Teflaro

Fluoroquinolones ciprofloxacin Cipro

gemifloxacin Factive
levofloxacin Levaquin
moxifloxacin Avelox
norfloxacin Noroxin
ofloxacin Floxin, Ocuflox

Penicillins and Penicillinase- Resistant Antibiotics

• Penicillins penicillin G benzathine Bicillin, Permapen

penicillin G potassium Pfizerpen
penicillin G procaine Wycillin
penicillin V Veetids
 • Extended-Spectrum
Penicillins amoxicillin Amoxil, Trimox
Ampicillin Principen

• Penicillinase-Resistant
Antibiotics nafcillin
oxacillin

Sulfonamides Sulfadiazine generic

sulfasalazine Azulfidine
cotrimoxazole Septra, Bactrim

Tetracyclines demeclocycline Declomycin

doxycycline Doryx, Periostat
minocycline Minocin
tetracycline Sumycin

Antimycobacterials
Antituberculosis
• First-line ethambutol Myambutol
Pyrazinamide Nydrazid
rifampin generic
rifapentine Rifadin, Rimactane streptomycin
generic
• Second-line capreomycin Capastat
cycloserine Seromycin
ethionamide Trecator-SC
rifabutin Mycobutin
Leprostatic dapsone generic

Other Antibiotics
Ketolide telithromycin Ketek
Lincosamides clindamycin Cleocin
lincomycin Lincocin
Lipoglycopeptides telavancin Vibativ
Macrolides azithromycin Zithromax
clarithromycin Biaxin
erythromycin Ery-Tab, Eryc
Monobactam aztreonam Azactam

Spotlight: Bacteria and Antibiotics

• Bacteria are microorganisms that invade the human body through many routes like respiratory, gastrointestinal, and skin.
• Human immune response is activated once bacteria invade the body. As the body tries to rid itself of bacteria, classic signs of
inflammation (e.g. swelling, heat, redness, and pain), fever, and lethargy begin to show up.
• The goal of antibiotic therapy is to decrease the population of invading bacteria to a point at which the human immune system can
effectively deal with the invader.
Aminoglycosides
• Aminoglycosides are a group of antibiotics indicated for infections caused by gram-negative aerobic bacilli
. • They were replaced by newer, less-toxic drugs in treating less serious infections because these drugs have potentially
serious adverse effects.

Therapeutic Action
The desired and beneficial action of aminoglycosides is:
• Exert bactericidal effect through inhibition of protein synthesis in susceptible strains of gram-negative bacteria.
Specifically, they bind to a unit of the bacteria ribosomes and cause misreading of the genetic code leading to cell death.
Indications
Aminoglycosides are indicated for the following medical conditions:
• Infections caused by susceptible strains: Pseudomonas aeruginosa, Escherichia coli, Proteus spp., Klebsiella-
Enterobacter-Serratia group, Citrobacter spp., and Staphylococcus spp.
• Serious infections susceptible to penicillin when penicillin is contraindicated.
Here are some important aspects to remember for indication of antibiotics in different age groups:
Children
This age group is very sensitive to GI and CNS adverse effects of antibiotics. Therefore, it is important to monitor
their nutritional and hydration status while on therapy. Oral candidiasis as a superinfection is common in this age group
which makes eating and drinking difficult. Fluoroquinolones are associated with damage to developing cartilage and are
not recommended for growing children. In addition to this, pediatric dosages should be double-checked to decrease the risk
for adverse effects. Most of all, parent education is important in cutting down the unnecessary use of antibiotics in children.
Adults
This age group has the tendency to cure simple manifestations with antibiotics. Therefore, it is important to educate them
that antibiotics are effective only for certain bacteria and not for simple manifestations like common colds, which may be
viral. Storage of unused pills for future infections and sharing antibiotics with symptomatic friends should be avoided and
emphasized in health teachings.
Older adults
Assessing the problem and obtaining appropriate specimens for culture is especially important with this population. Older
patients may be more susceptible to adverse effects of antibiotic therapy.

Pharmacokinetics
Here are the characteristic interactions of aminoglycosides and the body in terms of absorption, distribution, metabolism,
and excretion:

Route Onset Peak Duration

IM, IV Rapid 30-90 min N/A
T1/2: 2-3 h
Metabolism: liver
Excretion: kidney (urine

Contraindications and Cautions

 The following are contraindications and cautions for the use of aminoglycosides:

• Known allergy to aminoglycosides.

• Renal or hepatic disease. Can be exacerbated by aminoglycosides and may interfere with metabolism and excretion of
these drugs.
• Preexisting hearing loss. Can be intensified by toxic drug effects on the auditory nerve.
Active infection with herpes or mycobacterial infections. Can be worsened by the effects of an aminoglycoside on normal
defense mechanisms.
• Myasthenia gravis or parkinsonism. Can be exacerbated by the effects of a particular aminoglycosides on the nervous
system.
• Lactation. Aminoglycosides are excreted in the breast milk and can potentially cause serious effects in the infant.
• Amikacin should not be used for longer than 7-10 days because it is particularly toxic to the bone marrow, kidneys, and
GI.
• Streptomycin is only for special situations because it is very toxic to the 8th cranial nerve and kidney.

Adverse Effects
Use of aminoglycosides may result to these adverse effects:

• CNS: ototoxicity, irreversible deafness, vestibular paralysis, confusion, depression, disorientation, numbness, tingling,
weakness
• Renal: renal failure
• Hematology: bone marrow depression, leading to immunosuppression and resultant superinfections
• GI: nausea, vomiting, diarrhea, weight loss, stomatitis, hepatotoxicity
• CV: palpitations, hypotension, hypertension
• Hypersensitivity reactions: purpura, rash, urticaria, exfoliative dermatitis

Interactions
The following are drug-drug interactions involved in the use of aminoglycosides:
• Penicillins, cephalosporins, ticarcillin: synergistic bactericidal effect
• Diuretics: increased incidence of ototoxicity, nephrotoxicity, and neurotoxicity
• Anesthetics, nondepolarizing NM blockers, succinylcholine, citrate anticoagulated blood: increased NM blockade with
paralysis

Carbapenems
• Carbapenems are a relatively new class of broad-spectrum antibiotics effective against gram-positive and gram-negative
bacteria.

Therapeutic Action
The desired and beneficial action of carbapenems is:
• Exert bactericidal effect by inhibiting cell membrane synthesis in susceptible bacteria, leading to cell death.

Indications
Carbapenems are indicated for the following medical conditions:
• Serious intra-abdominal, urinary tract, skin and skin structure, bone and joint, and gynecological infections.
• Infections caused by susceptible strains: S.pneumoniae, H.influenzae, E.coli, K.pneumoniae, B.fragilis,
P.mirabilis, P.aeruginosa, and P.bivia.

Pharmacokinetics
Here are the characteristic interactions of carbapenems and the body in terms of absorption, distribution, metabolism, and
excretion:

Route Onset Peak Duration

IM, IV Rapid 30-120 min N/A
 T1/2: 4 h
Metabolism: N/A
Excretion: kidney (urine); unchanged

Contraindications and Cautions

The following are contraindications and cautions for the use of carbapenems:
• Known allergy to carbapenems or beta-lactams.
• Seizure disorders. Exacerbated by drugs.
• Meningitis. Safety is not established.
• Lactation. Not known whether drug can cross into breast milk or not.
• Ertapenem is not recommended for use in patients younger than 18 years of age.
• Meropenem is associated with development of pseudomembranous colitis and should be used in caution in patients with
inflammatory bowel disease.

Adverse Effects

Use of carbapenems may result to these adverse effects:

• GI: pseudomembranous colitis, C.difficile diarrhea, nausea, vomiting, dehydration and electrolyte imbalance
• CNS: headache, dizziness, altered mental state • Superinfections

Interactions

The following are drug-drug interactions involved in the use of carbapenems:

• Valproic acid: Carbapenems reduce serum valproic acid and this can increase risk of seizures.
• Imipenem and ganciclovir can cause seizures.
• Meropenem and probenecid can lead to toxic levels of meropenem.

Cephalosporins

• Cephalosporins were first introduced in the 1960s. There are currently four generations of cephalosporins, each with
specific spectrum of activity.
• These drugs are similar to penicillins in structure and activity.

Therapeutic Action
The desired and beneficial action of carbapenems is:
• Exert bactericidal and bacteriostatic effects by interfering with the cell-wall building ability of bacteria during cell
division. Therefore, they prevent the bacteria from bio synthesizing the framework of their cell walls.

Indications

Cephalosporins are indicated for the following medical conditions:

• First-generation cephalosporins are effective against the same gram-positive bacteria affected by penicillin G, as
well as gram-negative bacteria P.mirabilis, K.pneumoniae, E.coli.
• Second-generation cephalosporins are effective against previously mentioned strains as well as H.influenzae,
E.aerogenes, and Neisseria spp. These drugs are less effective against gram-positive bacteria.
• Third-generation cephalosporins are effective against all of the previously mentioned strains. They are relatively
weak against gram-positive bacteria but are more potent against gram-negative bacilli, as well as S.marcescens.
• Fourth-generation cephalosporins are active against gram-negative and gram-positive organisms, including
cephalosporin-resistant staphylococci and P.aeruginosa.

Pharmacokinetics
Here are the characteristic interactions of cephalosporins and the body in terms of absorption, distribution,
metabolism, and excretion:
 Route Onset Peak Duration
Oral N/A 30-60 min 8-10 h

T1/2: 30-60 min

Metabolism: N/A Excretion:
kidney (urine); unchanged

Contraindications and Cautions

The following are contraindications and cautions for the use of cephalosporins:

• Known allergy to cephalosporins and beta-lactams. Cross-reactions are common.

• Hepatic or renal impairment. These drugs are toxic to the kidneys and could interfere with the metabolism and
excretion of the drugs.
• Pregnancy and lactation. Potential effects on the fetus and infant are not known; use only if benefits clearly
outweigh the potential risk of toxicity to the fetus or infant.
• Reserve cephalosporins for appropriate situations because cephalosporin-resistant bacteria are appearing in
increasing numbers. Perform culture and sensitivity test before start of therapy.

Adverse Effects

Use of cephalosporins may result to these adverse effects:

• GI: nausea, vomiting, diarrhea, anorexia, abdominal pain, flatulence, pseudomembranous colitis
• CNS: headache, dizziness, lethargy, paresthesias
• Nephrotoxicity in patients who have predisposing renal insufficiency

Superinfections
• Phlebitis and local abscess at the site of IM injection and/or IV administration.

Interactions

The following are drug-drug interactions involved in the use of cephalosporins:

• Aminoglycosides: increased risk for nephrotoxicity
• Oral anticoagulants: increased bleeding
• Alcohol: avoided for 72 hours after discontinuation of the drug to prevent disulfiram-like reaction (e.g. flushing,
throbbing headache, nausea and vomiting, chest pain, palpitations, dyspnea, syncope, vertigo, convulsions, etc.)

Fluoroquinolones

• Fluoroquinolones are a relatively new synthetic class of antibiotics with a broad spectrum of activity.

Therapeutic Action

The desired and beneficial action of fluoroquinolones is:

• Interfere with the action of DNA enzymes necessary for growth and reproduction of the bacteria
. • Has little cross-resistance but misuse of this drug for a short time will lead to existence of resistant strains.

Indications

Fluoroquinolones are indicated for the following medical conditions:

• Treating infections (respiratory, urinary tract, and skin) caused by susceptible strains: E.coli, P.mirabilis,
K.pneumoniae, P.vulgaris, M.morganii, P.aeruginosa, H.influenzae, S.aureus, S.epidermidis, N.gonorrhoeae, and
group D streptococci.
 Ciprofloxacin was approved in 2001 for prevention of anthrax infection in areas that might be exposed to germ
warfare. It is also effective against typhoid fever.

Pharmacokinetics
Here are the characteristic interactions of fluoroquinolones and the body in terms of absorption,
distribution, metabolism, and excretion:

Route Onset Peak Duration

Oral Varies 60-90 min 4-5 h
IV 10 min 30 min 4-5 h

T1/2: 3.5-4 h
Metabolism: liver
Excretion: liver (bile), kidney (urine)

Contraindications and Cautions

The following are contraindications and cautions for the use of fluoroquinolones:

• Known allergy to fluoroquinolones.

• Pregnancy and lactation. Potential effects on the fetus and infant are not known; use only if benefits clearly outweigh the
potential risk of toxicity to the fetus or infant.
• Seizures. Can be exacerbated by the drugs’ effects on cell membrane channels

Adverse Effects
Use of fluoroquinolones may result to these adverse effects:
• GI: nausea, vomiting, diarrhea, dry mouth
• CNS: headache, dizziness, insomnia, depression
• Immunological: bone marrow depression
• Risk for tendinitis and tendon rupture in patients over age 60, on concurrent steroids, and those with renal, heart, or lung
transplants
• Photosensitivity and severe skin reactions so advise patient to avoid sun and ultraviolet light exposure and to use
protective clothing and sunscreens.

Interactions

The following are drug-drug interactions involved in the use of fluoroquinolones:

• Iron salts, sucralfate, mineral supplements, antacids: increased therapeutic effects of fluoroquinolones. Administration
should be separated by at least 4 hours.
• Quinidine, procainamide, pentamidine, tricyclics, phenothiazines: severe-to-fatal cardiac reactions due to increased QTc
interval and/or torsades de pointes
• Theophylline: inreased theophylline levels because these two drugs have the same metabolic pathway
• Steroids: increased CNS stimulation

Penicillins and Penicillinase-Resistant Antibiotics

• Penicillin was the first antibiotic introduced for clinical use. Various modifications were subsequently made to address
resistant strains and to decrease drug adverse effects.
• Penicillinase-resistant antibiotics were developed to address penicillin-resistant bacteria.

Therapeutic Action

The desired and beneficial action of penicillins and penicillinase-resistant antibiotics is:
 • Exert bactericidal effect by interfering with the ability of susceptible bacteria to build their cell walls when they are
dividing. These drugs prevent the bacteria from bio synthesizing the framework of the cell wall, and the bacteria with
weakened cell walls swell and then burst from osmotic pressure within the cell.

Indications

Penicillins and penicillinase-resistant antibiotics are indicated for the following medical conditions:

• Treatment of streptococcal infections (e.g. pharyngitis, tonsillitis, scarlet fever, endocarditis).

• Treatment of meningococcal meningitis if given at high doses

Pharmacokinetics
Here are the characteristic interactions of penicillins and penicillinase-resistant antibiotics and the body in terms of
absorption, distribution, metabolism, and excretion:
Route Onset Peak Duration
Oral Varies 1h 6-8 h\

T1/2: 1-1.4 h
Metabolism: N/A
Excretion: kidney (urine)

Contraindications and Cautions

The following are contraindications and cautions for the use of penicillins and penicillinase-resistant antibiotics:

• Known allergy to penicillins and cephalosporins.

• Renal disease. Drug excretion is reduced. • Pregnancy and lactation. No adequate studies on the effect on fetus
but these drugs can cause diarrhea and superinfections may occur in the infant.

Adverse Effects
Use of penicillins and penicillinase-resistant antibiotics may result to these adverse effects:

• GI: nausea, vomiting, diarrhea, abdominal pain, glossitis, stomatitis, gastritis, sore mouth, furry tongue
• Pain and inflammation at the injection site can occur with injectable forms of the drugs.
• Hypersensitivity reactions: rash, fever, wheezing, anaphylaxis with repeated exposures
• Superinfections, e.g. yeast infections.

Interactions

The following are drug-drug interactions involved in the use of penicillins and penicillinase-resistant antibiotics:

• Tetracyclines: decrease in effectiveness of penicillins

• Parenteral aminoglycosides: inactivation of aminoglycosides