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Treatmenta
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Condition Characteristic Pathogens Mitigating Circumstances Recommended Empirical
Treatmenta
Complicated UTI in men E. coli, Proteus, Klebsiella, Mild to moderate illness, no Oralc quinolone for 1014 d
and women Pseudomonas, Serratia, nausea or vomiting:
enterococci, staphylococci outpatient therapy
Severe illness or possible Parenterald ampicillin and
urosepsis: hospitalization gentamicin, quinolone,
required ceftriaxone, aztreonam,
ticarcillin/clavulanate, or
imipenem-cilastatin until
defervescence; then oralc
quinolone or TMP-SMX for
1021 d
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Trimethoprim and TMP-SMX
Fluoroquinolones
Macrocrystalline nitrofurantoin
Penicillins
Cefpodoxime proxetil (and other
Cephalosporins)
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Selectively inhibits
bacterial dihydrofolic
acid reductase, which
converts dihydrofolic
acid to tetrahydrofolic
acid, a step leading to
the synthesis of
purines and ultimately
to DNA.
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Trimethoprim and TMP-SMX
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Pharmacokinetics
Mode of administration
PO (Trimethoprim, and TMP-SMX)
Intravenously (TMP-SMX) .
Trimethoprim is well absorbed from the gut
and distributed widely in body fluids and
tissues, including cerebrospinal fluid.
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Pharmacokinetics
Trimethoprim is more lipid-soluble than
sulfamethoxazole
Trimethoprim has a larger volume of
distribution than sulfamethoxazole.
TMP : SMX = 1 : 5 1:20 peak plasma
concentration
Optimal for the combined effects of these
drugs in vitro.
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Pharmacokinetics
Excretion
About 3050% of the sulfonamide and 5060%
of the trimethoprim (or their respective
metabolites) are excreted in the urine within 24
hours.
The dose should be reduced by half for patients
with creatinine clearances of 1530 mL/min.
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Pharmacokinetics
Concentrates in prostatic fluid and in
vaginal fluid, which are more acidic than
plasma.
Has more antibacterial activity in prostatic and
vaginal fluids than many other antimicrobial
drugs.
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Pharmacokinetics
Drug Half-Life Oral Absorption
Sulfonamides
Pyrimidines
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Adverse Effects
Megaloblastic anemia
Leukopenia
Granulocytopenia
Nausea and vomiting
Drug fever
Vasculitis
Renal damage
CNS disturbances company name
Adverse Effects
Patients with AIDS and pneumocystis pneumonia
have a particularly high frequency of untoward
reactions to trimethoprim-sulfamethoxazole,
Fever
Rashes
Leukopenia
Diarrhea
Elevations of hepatic aminotransferases,
Hyperkalemia
Hyponatremia
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Active against a variety of gram-positive
and gram-negative bacteria.
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Mode of Action
Fluoroquinolones
Inhibiting bacterial
Inhibit bacterial
topoisomerase II (DNA
topoisomerase IV
gyrase)
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Pharmacokinetics
Mode of administration
PO
IV
Well absorbed (bioavailability of 8095%) and
distributed widely in body fluids and tissues.
Serum half-lives range from 3 to 10 hours.
The relatively long half-lives of levofloxacin,
gemifloxacin gatifloxacin, and moxifloxacin permit
once-daily dosing.
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Pharmacokinetics
Oral absorption is impaired by divalent
cations, including those in antacids.
Excretion
Most are eliminated by renal mechanisms,
either tubular secretion or glomerular filtration.
Nonrenally cleared fluoroquinolones are
relatively contraindicated in patients with
hepatic failure.
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Pharmacokinetics
Norfloxacin
The least active of the fluoroquinolones against both
gram-negative and gram-positive organisms.
Minimum inhibitory concentrations (MICs) fourfold to
eightfold higher than those of ciprofloxacin.
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Pharmacokinetics
Ciprofloxacin, enoxacin, lomefloxacin, levofloxacin,
ofloxacin, and pefloxacin (second group of quinolones)
Excellent gram-negative activity.
Moderate to good activity against gram-positive bacteria.
MICs for gram-negative cocci and bacilli, including
Enterobacteriaceae, pseudomonas, neisseria, haemophilus,
and campylobacter, are 12 mcg/mL and often less.
Ciprofloxacin is the most active agent of this group against
gram-negatives, P aeruginosa in particular.
Levofloxacin, the L-isomer of ofloxacin, has superior activity
against gram-positive organisms, including S pneumoniae.
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Pharmacokinetics
Gatifloxacin, gemifloxacin, and moxifloxacin (third
group of fluoroquinolones)
Improved activity against gram-positive organisms,
particularly S pneumoniae and some staphylococci.
MICs of these agents for staphylococci are lower than
those of the second group.
None of these agents is as active as ciprofloxacin against
gram-negative organisms.
Moxifloxacin also has good activity against anaerobic
bacteria.
Because of toxicity, gatifloxacin is no longer available in
the USA.
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Adverse Effects
Extremely well tolerated.
The most common effects are
Nausea, vomiting, and diarrhea. Occasionally,
headache, dizziness, insomnia, skin rash, or
abnormal liver function tests develop.
Photosensitivity has been reported with
lomefloxacin and pefloxacin.
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Adverse Effects
QTc prolongation may occur with gatifloxacin,
levofloxacin, gemifloxacin, and moxifloxacin.
Ideally, these agents should be avoided or used with caution
in patients with
Known QTc interval prolongation or uncorrected hypokalemia;
In those receiving class IA (eg, quinidine or procainamide) or class
III antiarrhythmic agents (sotalol, ibutilide, amiodarone);
In patients receiving other agents known to increase the QTc
interval (eg, erythromycin, tricyclic antidepressants).
Gatifloxacin
Hyperglycemia in diabetic patients
Hypoglycemia in patients also receiving oral hypoglycemic agents.
Withdrawn from sales in the USA in 2006; it may be available
elsewhere.
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Adverse Effects
May damage growing cartilage and cause an
arthropathy.
Not routinely recommended for patients under
18 years of age.
Tendinitis
Rare
Contraindicated during pregnancy.
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Bacteriostatic and bactericidal for many gram-
positive and gram-negative bacteria
but P aeruginosa and many strains of proteus are
resistant.
There is no cross-resistance between
nitrofurantoin and other antimicrobial agents and
resistance emerges slowly.
Thus, it becomes an important alternative oral agent
for treatment of uncomplicated urinary tract infection.
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Pharmacokinetics
Nitrofurantoin is well absorbed after ingestion.
It is metabolized and excreted so rapidly that no
systemic antibacterial action is achieved.
Excreted into the urine by both glomerular
filtration and tubular secretion.
With average daily doses, concentrations of 200
mcg/mL are reached in urine.
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Pharmacokinetics
Dose for urinary tract infection
Adults: 100 mg orally , 4x/day.
It is desirable to keep urinary pH below 5.5,
greatly enhances drug activity.
A single daily dose of nitrofurantoin, 100
mg, can prevent recurrent urinary tract
infections in some women.
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Adverse Effects
Nitrofurantoin is contraindicated in patients
with significant renal insufficiency.
It should not be used to treat upper urinary
tract infection.
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Adverse Effects
Anorexia
Nausea
Vomiting
Neuropathies and hemolytic anemia occur in
G6PD patients.
Rashes
Pulmonary infiltration
Fibrosis
Other hypersensitivity reactions
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Inhibit bacterial growth by interfering with
the transpeptidation reaction of bacterial
cell wall synthesis.
Kill bacterial cells only when they are
actively growing and synthesizing cell wall.
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Penicillins (Amoxicillin, Ampicillin,
Ticarcillin/Clavulanate)
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Penicillins (Amoxicillin, Ampicillin,
Ticarcillin/Clavulanate)
Covalently bind
to the active site Inhibits the Halting
Lactam
of PBPs transpeptidation peptidoglycan Cell dies
antibiotics
(Penicillin- reaction synthesis
binding protein)
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Pharmacokinetics
Oral administration
Acid-stable and relatively well absorbed.
Serum concentrations :
48 mcg/mL (after a 500 mg oral dose)
Absorption is impaired by food (except
amoxicillin)
Should be administered at least 12 hours before or
after a meal.
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Pharmacokinetics
Parenteral administration
Absorption of most penicillins is complete and rapid.
Serum concentrations 30 minutes after an intravenous
injection of 1 g of a penicillin (equivalent to
approximately 1.6 million units of penicillin G) are 20
50 mcg/mL.
Only a small amount of the total drug in serum is
present as free drug, the concentration of which is
determined by protein binding.
Widely distributed in body fluids and tissues with a few
exceptions.
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Pharmacokinetics
Excretion
Rapidly excreted by the kidneys
10% of renal excretion is by glomerular filtration
90% by tubular secretion.
Ampicillin and the extended-spectrum
penicillins are secreted more slowly than
penicillin G and have half-lives of 1 hour.
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Pharmacokinetics
Administration Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
mL/min mL/min
Extended-spectrum penicillins
Amoxicillin 0.250.5 g tid 2040 66% 33%
(PO) mg/kg/d in 3
doses
Ticarcillin 3 g q46h 200300 150200 5075% 2533%
(IV) mg/kg/d in 4 mg/kg/d in 2
6 doses or 3 doses
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Adverse Effects
The penicillins are remarkably nontoxic.
Most of the serious adverse effects are due
to hypersensitivity.
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Adverse Effects
Allergic reactions
Anaphylactic shock (very rare0.05% of recipients);
Serum sickness-type reactions
Now rare
Urticaria, fever, joint swelling, angioneurotic edema,
intense pruritus, and respiratory embarrassment
Occurring 712 days after exposure
A variety of skin rashes.
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Adverse Effects
Oral lesions
Fever
Interstitial nephritis (an autoimmune
reaction to a penicillin-protein complex)
Eosinophilia
Hemolytic anemia and other hematologic
disturbances
Vasculitis
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First Generation
Second Generation
Third Generation
Fourth Generation
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This includes cefadroxil, cefazolin,
cephalexin, cephalothin, cephapirin, and
cephradine.
Very active against gram-positive cocci,
such as
Pneumococci
Streptococci
Staphylococci
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Other Bacterias
o E coli o Indole-positive proteus (X)
o K pneumoniae o Enterobacter (X)
o Proteus mirabilis o Serratia marcescens (X)
o Anaerobic cocci (eg, o Citrobacter (X)
peptococcus, o Acinetobacter (X)
peptostreptococcus) are o Methicillin-resistant strains
usually sensitive of staphylococci (X)
o Bacteroides fragilis (X)
o P aeruginosa (X)
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Pharmacokinetics
Cephalexin, cephradine, and cefadroxil
are absorbed from the gut to a variable extent.
Serum levels are 1520 mcg/mL (After oral
doses of 500 mg)
Urine concentration is usually very high
In most tissues levels are variable and
generally lower than in serum.
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Pharmacokinetics
Cephalexin and cephradine
Orally, 0.250.5 g four times daily (1530 mg/kg/d)
Cefadroxil
IV, 0.51 g twice daily.
Excretion
Mainly by glomerular filtration and tubular secretion
into the urine.
Drugs that block tubular secretion, eg, probenecid,
may increase serum levels substantially.
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Pharmacokinetics
Adjusted Dose as a Percentage of
Normal Dose for Renal Failure
Based on Creatinine Clearance
(Clcr)
Antibiotic (Route Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
of mL/min mL/min
Administration)
First-generation cephalosporins
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Second Generation Cephalosporins
Active against organisms inhibited by first-
generation drugs, but in addition they have
extended gram-negative coverage.
Klebsiellae
Cefamandole, cefuroxime, cefonicid,
ceforanide, and cefaclor
H influenzae
Serratia (X)
B fragilis (X) company name
Second Generation Cephalosporins
Cefoxitin, cefmetazole, and cefotetan
B fragilis
Some serratia strains
H influenzae (X)
Enterococci (X)
P aeruginosa (X)
Enterobacter (X) due to resistance
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Pharmacokinetics
Adjusted Dose as a Percentage of
Normal Dose for Renal Failure
Based on Creatinine Clearance
(Clcr)
Antibiotic Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
(Route of mL/min mL/min
Administration)
Second-generation cephalosporins
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Include cefoperazone, cefotaxime,
ceftazidime, ceftizoxime, ceftriaxone,
cefixime, cefpodoxime proxetil, cefdinir,
cefditoren pivoxil, ceftibuten, and
moxalactam.
Have expanded gram-negative coverage
Able to cross the blood-brain barrier.
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Third Generation Cephalosporins
o Citrobacter o Providencia (X) due to
o S marcescens resistance
o Providencia o Citrobacter (X) due to
o Lactamase-producing resistance
strains of haemophilus and o Ceftizoxime and
neisseria moxalactam
o B fragilis
o Ceftazidime and
cefoperazone o Cefixime and ceftibuten
o P aeruginosa o Pneumococci (X)
o Enterobacter (X) o S aureus (Poor)
o Serratia (X) due to company name
resistance
Pharmacokinetics
Penetrate body fluids and tissues well and, (Except
cefoperazone and all oral cephalosorins)
Cross BBB
Excretion
Cefoperazone and ceftriaxone mainly through the
biliary tract
The others are excreted by the kidney (require dosage
adjustment in renal insufficiency)
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Pharmacokinetics
Adjusted Dose as a Percentage of Normal
Dose for Renal Failure Based on
Creatinine Clearance (Clcr)
Antibiotic (Route of Adult Dose Pediatric Dose1 Neonatal Dose2 Clcr Approx 50 Clcr Approx 10
Administration) mL/min mL/min
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Example: Cefepime.
More resistant to hydrolysis by chromosomal -
lactamases (eg, those produced by enterobacter).
P aeruginosa
Enterobacteriaceae
S aureus
S pneumoniae
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Fourth Generation Cephalosporin
Haemophilus
Neisseria
Penicillin-resistant strains of streptococci
Enterobacter infections
It penetrates well into cerebrospinal fluid
Excretion
It is cleared by the kidneys
Half-life : 2 hours
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Fourth Generation Cephalosporin
Clinical role is similar to that of third-
generation cephalosporins.
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Writing a prescription should be based on a
series of rational steps
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Prescriptions based merely on a desire to satisfy the
patient's psychological need for some type of therapy
are often unsatisfactory and may result in adverse
effects. A specific diagnosis, even if it is tentative, is
required to move to the next step. The diagnosis and
Make a specific the reasoning underlying it should be shared with the
diagnosis patient.
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A therapeutic objective should be chosen for each of
the pathophysiologic processes defined in the
Select a specific preceding step.
therapeutic
objective
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The dosing regimen is determined primarily by the pharmacokinetics of the drug
in that patient. If the patient is known to have disease of the organs required for
elimination of the drug selected, adjustment of the average regimen is needed.
Determine the
appropriate dosing
regimen
The prescriber should be able to describe to the patient the kinds of drug
effects that will be monitored and in what way, including laboratory tests (if
necessary) and signs and symptoms that the patient should report. For
conditions that call for a limited course of therapy (eg, most infections), the
duration of therapy should be made clear so that the patient does not stop
Devise a plan for taking the drug prematurely and understands why the prescription probably
need not be renewed. The prescriber should also specify any changes in the
monitoring the drug's patient's condition that would call for changes in therapy. Major toxicities that
action and determine an require immediate attention should be explained clearly to the patient.
end point for therapy
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The prescriber and other members of the health
team should be prepared to repeat, extend, and
reinforce the information transmitted to the
patient as often as necessary. The more toxic the
Plan a program of drug prescribed, the greater the importance of
patient education this educational program.
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Prescription can be written on any piece of
paper (as long as all of the legal elements
are present)
It usually takes a specific form
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Identity of the prescriber.
Name, license classification (ie, professional degree),
address, and office telephone number.
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Prescription Writing
Drug name [8]
Either the brand name (proprietary name) or the generic name
(nonproprietary name) may be used.
The strength of the medication [9]
Should be written in metric units.
The strength of a solution is usually expressed as the quantity of
solute in sufficient solvent to make 100 mL; for instance, 20%
potassium chloride solution is 20 grams of KCl per deciliter (g/dL)
of final solution. Both the concentration and the volume should be
explicitly written out.
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Prescription Writing
1 grain (gr) = 0.065 grams (g), often rounded to 60 milligrams (mg)
15 gr = 1 g
1 ounce (oz) by volume = 30 milliliters (mL)
1 teaspoonful (tsp) = 5 mL
1 tablespoonful (tbsp) = 15 mL
1 quart (qt) = 1000 mL
1 minim = 1 drop (gtt)
20 drops = 1 mL
2.2 pounds (lb) = 1 kilogram (kg)
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Prescription Writing
The quantity of medication
Should reflect the anticipated duration of
therapy, the cost, the need for continued
contact with the clinic or physician, the
potential for abuse, and the potential for
toxicity or overdose.
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Prescription Writing
The directions for use [11]
Must be both drug-specific and patient-specific.
The simpler the directions, the better.
The fewer the number of doses (and drugs) per
day, the better.
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Example
Ms. GA, was diagnosed with acute uncomplicated cystitis,
infected by E. coli. Non-diabetic, not pregnant.
Treatment:
7-day regimen: macrocrystalline nitrofurantoin.
Available preparation:
Nitrofurantoin (generic, Macrodantin) Oral: 25, 50, 100 mg
capsules, 25 mg/5 mL suspension.
Dose: 100 mg orally , 4x/day for 7 days.
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Example
Macrodantin, 100 mg
#28 capsules
John B. Doe
N/A
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Women who experience frequent
symptomatic UTIs (3 per year on average)
Candidates for long-term administration of low-
dose antibiotics directed at preventing
recurrences.
Advised to avoid spermicide use and to void
soon after intercourse.
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Prophylaxis
Daily or thrice-weekly administration of a single dose of
TMP-SMX (80/400 mg),
TMP alone (100 mg), or
Nitrofurantoin (50 mg)
Fluoroquinolones
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Other patients for whom prophylaxis appears to
have some merit include
Men with chronic prostatitis;
Patients undergoing prostatectomy (during operation
and postoperatively)
Pregnant women with asymptomatic bacteriuria.
All pregnant women should be screened for
bacteriuria in the first trimester and should be
treated if bacteriuria is detected.
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