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Tetracyclines, Aminogylcosides

Tetracyclines and macrolides are broad-spectrum antibiotics used to treat various bacterial infections, with tetracyclines being primarily bacteriostatic and macrolides inhibiting protein synthesis. Tetracyclines have specific pharmacokinetics and side effects, including photosensitivity and potential for superinfections, while macrolides like erythromycin are effective against gram-positive and gram-negative bacteria with fewer adverse effects. Aminoglycosides are also discussed, providing bactericidal activity against gram-negative bacteria but with serious potential side effects like ototoxicity and nephrotoxicity.

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0% found this document useful (0 votes)
49 views12 pages

Tetracyclines, Aminogylcosides

Tetracyclines and macrolides are broad-spectrum antibiotics used to treat various bacterial infections, with tetracyclines being primarily bacteriostatic and macrolides inhibiting protein synthesis. Tetracyclines have specific pharmacokinetics and side effects, including photosensitivity and potential for superinfections, while macrolides like erythromycin are effective against gram-positive and gram-negative bacteria with fewer adverse effects. Aminoglycosides are also discussed, providing bactericidal activity against gram-negative bacteria but with serious potential side effects like ototoxicity and nephrotoxicity.

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Freda Morgan
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Tetracyclines are broad-spectrum antibiotics.

They may be classified as:

intermediate-acting compounds such as demeclocycline hydrochloride

long-acting compounds, such as doxycycline hyclate and

minocycline hydrochloride.

Pharmacokinetics
Tetracyclines are absorbed from the stomach and small intestine when taken orally.

Distribution and excretion


Tetracyclines are distributed widely into body tissues and fluids, concentrated in bile, and excreted
primarily by the kidneys. Doxycycline is also excreted in stool. Minocycline undergoes enterohepatic
recirculation.

Pharmacodynamics
All tetracyclines are primarily bacteriostatic, meaning they inhibit the growth or multiplication of bacteria.
They penetrate the bacterial cell by an energy-dependent process. Within the cell, they bind primarily
to a subunit of the ribosome, inhibiting the protein synthesis needed to maintain the bacterial cell.

USES OF TETRACYCLINES
Tetracyclines provide a broad spectrum of activity against:

• gram-positive and gram-negative aerobic and anaerobic bacteria

• spirochetes

• mycoplasma

• rickettsiae

• chlamydiae

• some protozoa.

They can be used against Mycoplasma pneumoniae. Tetracyclines should not be taken with
magnesium and aluminum antacid preparations, milk products containing calcium, oraI ron-containing
drugs, because these substances bind with tetracycline anprevent absor ption of the drug.
Side Effects
Nausea, vomiting, diarrhea, rash, flatulence, abdominal discomfort, headache, photosensitivity,
pruritus, heartburn, color vision changes, teeth discoloration.

Superinfections, severe photosensitivity, angioedema, hyperglycemia, hypertension


Life-threatening:
Blood dyscrasias, hepatotoxicity, intracranial hypertension, pseudomembranous colitis, Stevens-
Johnson syndrome

Nursing Process

Nursing Diagnoses
■ Risk for infection related to invasion of bacteria into respiratory tract
■ Noncompliance with drug regimen related to denial of illness
■ Risk for impaired skin integrity related to adverse effect of tetracycline (sunburn)
■ Imbalanced nutrition: less than body requirements, related to nausea and vomiting.

Nursing Interventions
■ o b t a i n a sample for culture from the infected area, and send to laboratory for culture and
sensitivity test. Anti- biotic therapy can be started after the culture sample has been taken.
■ Administer tetracycline 1 hour before or 2 hours after meals for optimum absorption.
■ Monitor laboratory values for liver and kidney func- tions (in particular, liver enzymes,
blood urea nitrogen, serum creatinine).
■ Record vital signs and urine output.

Patient Teaching
General
■ Tell patient to store tetracycline away from light and extreme heat. Tetracycline
decomposes in light and heat, causing the drug to become toxic.
■ Advise patient to check expiration date on bottle of tetracycline; out-of-date tetracycline can be
toxic.
■ I n f o r m female patients who are contemplating pregnancy to avoid taking tetracycline
because of possible teratogenic effect.
■ W a r n parents that children younger than 8 years of age should not take tetracycline
because it can cause discoloration of permanent teeth.
■ Encourage patient to take complete course of tetracycline as prescribed.

Side Effects
■ A d v i s e patient to use sun block and protective clothing during sun exposure.
Photosensitivity is associated with tetracycline.
■ Encourage patient to report signs of a superinfection (mouth ulcers, anal or genital
discharge).
■ A d v i s e patient to use additional contraceptive techniques and not to rely on oral
contraceptives when t a k i n g t h e drug, because e f f e c t i v e n e s s may decrease.
■ Teach patient to use effective oral hygiene several times a day to prevent or alleviate mouth
ulcers (stomatitis).

Macrolides
Macrolides are used to treat a number of common infections.
They include erythromycin and its derivatives, such as:
• erythromycin
• azithromycin
• clarithromycin.

In the patient who’s allergic to penicillin, erythromycin is effective for infections produced by group A
beta-hemolytic streptococci or Streptococcus pneumoniae. It may also be used to treat gonor- rhea
and syphilis in the patient who can’t tolerate penicillin G or

the tetracyclines. Erythromycin may also be used to treat minor staphylococcal infections of the skin.

Pharmacokinetics
Because erythromycin is acid-sensitive, it must be buffered or
have an enteric coating to prevent destruction by gastric acid. Erythromycin is absorbed in the
duodenum. It’s distributed to most tissues and body fluids except, in most cases, for cerebrospinal
fluid (CSF). However, as a class, macrolides can enter the CSF when meninges are inflamed.

Metabolism and excretion


Erythromycin is metabolized by the liver and excreted in bile in high concentrations; small amounts
are excreted in urine. It also crosses the placental barrier and is secreted in breast milk.

Mechanism of action
Macrolides inhibit ribonucleic acid (RNA)–dependent protein synthesis by acting on a small portion of
the ribosome

Uses
Erythromycin has a range of therapeutic uses.

• It provides a broad spectrum of antimicrobial activity against gram-positive and gram-negative


bacteria, including Mycobacterium, Treponema, Mycoplasma, and Chlamydia.

• It’s also effective against pneumococci and group A streptococci.


Staphylococcus aureus is sensitive to erythromycin; however, resistant strains may appear during
therapy.
• Erythromycin is the drug of choice for treating Mycoplasma pneumoniae infections as well as
pneumonia caused by Legionella pneumophila.

Side Effects
Erythromycin produces few adverse effects, which may include:
• epigastric distress
• nausea and vomiting
• diarrhea (especially with large doses)
• rash
• fever
• eosinophilia (an increase in the number of eosinophils, a type of white blood cell)
• anaphylaxis

DRUG DASAGE USES


azithromycin (Zithromax) A: PO: 250-500 mg q12h × 7-14 For upper and lower respiratory
clarithromycin (Biaxin) d tract infections, skin and
PO: 7.5 mg/kg b.i.d.; max: 15 soft-tissue infections,
mg/kg/d Helicobacter pylori and
mycobacterial
species, and gram-positive and
gram-negative organisms.
Report persistent diarrhea.
Pregnancy category: C;
For moderate to severe
infections (e.g., pneumococcal
Erythromycin A: PO: 250-500 mg q6h; max: 4 For moderate to severe
g/d infections (e.g., pneumococcal
C: PO: 20-50 mg/kg q6h; max: 2 pneumonia, acute pelvic
g/d inflammatory disease, intestinal
amebiasis, Legionnaires’
disease, chlamydial infections).
Report persistent diarrhea.
Pregnancy category: B; PB:
Fidaxomicin A: PO: 200 mg b.i.d. for 10 d; For treatment of Clostridium
max: 400 mg/d difficile–associated diarrhea.
May
cause GI bleeding, GI
obstruction, and elevated liver
enzymes.
Pregnancy category: B

Nursing Process
Assessment
■ Assess vital signs and urine output. Report abnormal findings.
■ Check laboratory tests (liver enzyme values) to determine liver function. Order liver enzyme
tests periodically for patients taking large doses of azithromycin for a continuous period.
■ Obtain a history of drugs patient currently takes. The peak level of azithromycin may be
decreased by antacids.

Nursing Diagnoses
■ Risk for infection related to invasion of bacteria through broken skin
■ Risk for impaired tissue integrity related to azithromycin side effects

Planning
■ Patient’s infection will be controlled and later eliminated.

Nursing Interventions
■ Obtain a sample from infected area and send to laboratory for culture and sensitivity (C&S)
test before starting azithromycin therapy. Antibiotic can be initiated after obtaining culture sample.
■ Monitor vital signs, urine output, and laboratory values, especially liver enzymes: alkaline
phosphatase, alanine aminotransferase, aspartate aminotransferase, and bilirubin.
■ Monitor patient for liver damage resulting from prolonged use and high dosage of
macrolides such as azithromycin. Signs of liver dysfunction include elevated liver enzyme levels
and jaundice.
■ Administer oral azithromycin 1 hour before or 2 hours after meals. Give with a full glass of
water, not fruit juice. Give the drug with food if GI upset occurs. Chewable tablets should be
chewed, not swallowed whole.
■ Dilute in an appropriate amount of solution as indicated in the drug circular for IV
azithromycin.
■ Administer antacids either 2 hours before or 2 hours after azithromycin.

Patient Teaching
General
■ Instruct patient to take full course of antibacterial agent as prescribed. Drug compliance is
most important for all antibacterials (antibiotics).
Teach patient to recognize signs of super infection like the presence of stomatitis.

Aminoglycosides
Aminoglycosides provide effective bactericidal activity against:
The aminoglycoside antibiotics are used against gramnegative bacteria such as E. coli, Proteus
spp., and Pseudomonas spp. Some gram-positive cocci are resistant to aminoglycosides, so
penicillins or cephalosporins may be used.
• mycobacteria
• some protozoa.
Common aminoglycosides
Aminoglycosides currently in use include:
• amikacin sulfate
• gentamicin sulfate
• kanamycin sulfate
• neomycin sulfate
• paromomycin sulfate
• streptomycin sulfate
• tobramycin sulfate.

Pharmacokinetics
Because aminoglycosides are absorbed poorly from the GI tract, they’re usually given
parenterally. After I.V. or I.M. administration, aminoglycoside absorption is rapid and complete.

Distribution
Aminoglycosides are distributed widely in extracellular fluid.
They readily cross the placental barrier, but don’t cross the blood- brain barrier.

Metabolism and excretion


Aminoglycosides aren’t metabolized. They’re excreted primarily unchanged by the kidneys.

Mechanism of Action
Aminoglycosides act as bactericidal drugs (remember, this means they kill bacteria) against
susceptible organisms by binding to the bacterium’s 30S subunit, a specific ribosome in the
microorganism, thereby interrupting protein synthesis and causing the bacterium to die.
Rising resistance
Bacterial resistance to aminoglycosides may be related to:
• failure of the drug to cross the cell membrane
• altered binding to ribosomes
• destruction of the drug by bacterial enzymes.
Some gram-positive enterococci resist aminoglycoside transport across the cell membrane.
When penicillin is used with aminoglycoside therapy, the cell wall is altered, allowing the
aminoglyco- side to penetrate the bacterial cell.

Uses of Aminoglycosides
Aminoglycosides are most useful in treating:
• infections caused by gram-negative bacilli
• serious nosocomial (hospital-acquired) infections, such as gram-negative bacteremia (abnormal
presence of microorganisms in the bloodstream), peritonitis (inflammation of the peritoneum, the
membrane that lines the abdominal cavity), and pneumonia, in critically ill patients
• urinary tract infections (UTIs) caused by enteric bacilli that are resistant to less toxic antibiotics,
such as penicillins and cephalosporins
• infections of the central nervous system (CNS) and the eye (treated with local instillation).
Aminoglycosides are used in combination with penicillins to treat gram-positive organisms, such
as staphylococcal or enterococcal

infections. Combination therapy increases the drugs’ effectiveness.


Aminoglycosides are inactive against anaerobic bacteria. Individual aminoglycosides may have
their own particular usefulness:
• Streptomycin is active against many strains of mycobacteria, including Mycobacterium
tuberculosis, and against the gram-positive bacteria Nocardia and Erysipelothrix.
• Amikacin, gentamicin, and tobramycin are active against Acine- tobacter, Citrobacter,
Enterobacter, Klebsiella, Proteus (indole- positive and indole-negative), Providencia, Serratia,
Escherichia coli, and Pseudomonas aeruginosa.

Drug interactions
Carbenicillin and ticarcillin reduce the effects of amikacin, gen- tamicin, kanamycin, neomycin,
streptomycin, and tobramycin. This is especially true if the penicillin and aminoglycoside are
mixed in the same container or I.V. line.
Adverse reactions to aminoglycosides
Serious adverse reactions limit the use of aminoglycosides. They include:
• neuromuscular reac- tions, ranging from pe- ripheral nerve toxicity to neuromuscular block- ade
• ototoxicity
• renal toxicity.
oral aminoglycosides include:
• nausea and vomiting
• diarrhea.

Amikacin, gentamicin, kanamycin, neomycin, streptomycin, and tobramycin administered with


neuromuscular blockers increase neuromuscular blockade, resulting in increased muscle
relaxation and respiratory distress.
Toxicity to the kidneys may result in renal failure; toxicity to the neurologic system results in
peripheral neuropathy with numbness and tingling of the extremities. The risk of renal toxicity
also increases when amikacin, gentamicin, kanamycin, or tobramycin is taken with cyclosporine,
amphotericin B, or acyclovir.
The symptoms of ototoxicity (damage to the ear) caused by aminoglycosides may be masked by
antiemetic drugs. Loop diuretics taken with aminoglycosides increase the risk of ototoxicity.
Hearing loss may occur in varying degrees and may be irreversible.

Nursing Process
Assessment
■ Record vital signs and urine output. Compare these results with future vital signs and urine
output. An adverse reaction to most aminoglycosides is nephrotoxicity.
■ Assess laboratory results to determine renal and liver functions, including blood urea nitrogen,
serum creatinine, alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase,
and bilirubin. Serum electrolytes should also be checked. Aminoglycosides may decrease serum
potassium and magnesium levels.
■ Obtain a medical history related to renal or hearing disorders. Large doses of
aminoglycosides could cause nephrotoxicity or ototoxicity.
Nursing Diagnoses
■ Risk for infection related to invasion of bacteria
■ Risk for impaired tissue integrity related to aminoglycoside side effect of rash
■ Imbalanced nutrition, less than body requirements, related to inability to ingest food
■ Risk for ineffective peripheral tissue perfusion: renal related

DRUG DOSAGE USES


amikacin sulfate A: IM/IV: 10-15 mg/kg/d q8- Effective against gram-
12h; max: 15 mg/kg/d negative bacteria, including
C: IM/IV: 7.5-22.5 mg/kg/d in those resistant
divided doses; max: to other aminoglycosides.
15 mg/kg/d Used for respiratory tract,
bone, joint,
skin, and soft-tissue
infections. Monitor for hearing
loss,
hepatotoxicity, and
nephrotoxicity. Pregnancy
category: C
Gentamicin A: IM/IV: 3-5 mg/kg/d in 3-4
divided doses
C: IM/IV: 2-2.5 mg/kg q8h
TDM: Peak: 5-8 mcg/mL;
trough: 0.5-2 mcg/mL
Neomycin Bowel prep: Decreases bacteria in the
A: PO: 1 g q1h for 4 doses; bowel and is used as a
then 1 g q4h for 5 doses preoperative bowel antiseptic.
Hepatic coma: Treats skin infections and
A: PO: 1-3 g q6h for 5-6 d; diarrhea caused by E. coli.
max: 12 g/d Pregnancy category: C

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