PHARMACOLOGY NUHS 2042 ANTIBIOTICS

NAME
LIMI BT gAPAT MIRHANISMA BT MUHININ

DIPLOMA IN NURSING

ANTIBIOTICS
DEFINITION OF ANTIBIOTICS
Antibiotics may be informally defined as the subgroup of anti-infectives that are derived from bacterial sources and are used to treat bacterial infections. Other classes of drugs, most notably the sulfonamides, may be effective antibacterials. Similarly, some antibiotics may have secondary uses, such as the use of demeclocycline (Declomycin, a tetracycline derivative) to treat the syndrome of inappropriate antidiuretic hormone (SIADH) secretion. Other antibiotics may be useful in treating protozoal infections.

PURPOSE
Antibiotics are used for treatment or prevention of bacterial infection.

DESCRIPTION
CLASSIFICATIONS Although there are several classification schemes for antibiotics, based on bacterial spectrum (broad versus narrow) or route of administration (injectable versus oral versus topical), or type of activity (bactericidal vs. bacteriostatic), the most useful is based on chemical structure. Antibiotics within a structural class will generally show similar patterns of effectiveness, toxicity, and allergic potential.

EXAMPLES OF DRUG ANTIOBIOTICS

Penicillins Cephalosporin Fluroquinolones Tetracyclines

PENICILLINS
The penicillins are the oldest class of antibiotics, and have a common chemical structure which they share with the cephalopsorins. The two groups are classed as the beta-lactam antibiotics, and are generally bacteriocidal-that is, they kill bacteria rather than inhibiting growth. The penicillins can be further subdivided. The natural pencillins are based on the original penicillin G structure; penicillinase-resistant penicillins, notably methicillin and oxacillin, are active even in the presence of the bacterial enzyme that inactivates most natural penicillins. Aminopenicillins such as ampicillin and amoxicillin have an extended spectrum of action compared with the natural penicillins; extended spectrum penicillins are effective against a wider range of bacteria. These generally include coverage for Pseudomonas aeruginaosa and may provide the penicillin in combination with a penicillinase inhibitor.

EXAMPLE OF PENICILLINS
Amoxicillin (amoxil,trimox,wymox) Ampicillin Naficillin Penicillin V Potassium Trcarcillin Disodium

Penicillin
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INDICATIONS
Penicillins are indicated for the indicated for prevention and treatment of infections caused by susceptible bacteria. The microorganisms most commonly destroyed by penicillins are gram-positive bacteria,including streptococcus spp.,enterococcus spp.,and staphylococcus spp.most penicillin have little if any ability to kill gram-negative bacteria, althoughts some of the extended spectrum penicillincan do so.

CONTRAINDACTION
Penicillins are usually safe and well-tolerated medications.The only usual contraindaction is known drug allergy.

SIDE EFFECTS
Hypersensitivity may be common, and cross allergenicity with cephalosporins has been reported. Penicillins are classed as category B during pregnancy.

ADVERSE EFFECT OF PENICILLINS

Considering the wide use of penicillin, it is remarkably free toxic effect.pain and rarely abscess formation may be seen at the site of injection. More commoly, sensitization rashes occur either as a result of contact with the drug during or after systemic administration. the rash is often uriticarial and is sometimes resistant to treatment. With ampcillin or amoxicillin the rash is sometimes erythermatous and is particularly fever or lymphoma. It may also appear after the drugs have been stoped. Rarely, penicillin causes an acute anaphylactic reaction with collapse, which can be fatal.

INTERACTIONS
Many drugs interact with penicillin:some have positive effects, and others have harmful effects. The most common and clinically significant drug interactions associated with penicillin use are listed.

NURSING RESPONSIBILITY
Always ask about previous drug reactions before giving a patient a penicillin, cephalosporin, or for that matter, any other drug.

CEPHALOSPORIN
Cephalosporins and the closely related cephamycins and carbapenems, like the pencillins, contain a beta-lactam chemical structure. Consequently, there are patterns of cross-resistance and cross-allergenicity among the drugs in these classes. The "cepha" drugs are among the most diverse classes of antibiotics, and are themselves subgrouped into 1st, 2nd and 3rd generations. Each generation has a broader spectrum of activity than the one before. In addition, cefoxitin, a cephamycin, is highly active against anaerobic bacteria, which offers utility in treatment of abdominal infections. The 3rd generation drugs, cefotaxime, ceftizoxime, ceftriaxone and others, cross the bloodbrain barrier and may be used to treat meningitis and encephalitis. Cephalopsorins are the usually preferred agents for surgical prophylaxis.

EXAMPLES OF DRUG
 Cefazolin (kefzol,ancef)  Cefditoren pivoxil  Cefoxitin (mefoxin)  Ceftazidime (fortaz,Tazidime)  Cephalexin (keflex,biocef)

USES
These are powerful antibiotic that induce serious side effect do not use for minor infections.
(1) gram-negative bacteria causing bone and joint infections,septicemia(including neonatal sepsis),skin and soft tissue infections(including those from burns), respiratory trac infections, postoperative infections , intra-abdominal infections (including peritonitis), UITs. In combinations with clindamycin for mixed aerobic-naerobic infections. Used for gram-positive bacteria only when other less toxic drugs are either ineffective or contraindicated. Use in CNS pseudomonas infections such as meningitis or ventriculitis is questionable.

(2)

ACTIONS
Broad-spectrum antibiotic believed to inhibits protein synthesis by binding irreversibly to ribosomes (30S subnit) ,thereby interfering with an initation complex between messenger RNA and the 30s subnit. This lead to production of nonfunctional protein. Usually bactericidal due to disruption of the bacterial cytoplasmic membrane.

PHARMACOKINETIC
Poorly absorbed from the GI tract; usually administered parenterally (exceptions: some anteric infections of the GI tract and prior to surgery). Also absorbed from the peritenum,bronchial tree, wounds denuded skin, and joints. Distributed in the extracellular fluid. Crosses the placental barrier,but not the blood brain barrier. Penetration of the CSF is increased when the meanings are inflamed. Rapidly absorbed after IM injections. Peak plasma levels, after IM: usually -2 hr.measurable levels persist for 8-12 hr after a single administration.t : 2-3 hr(increases sharply in impaired kidney function). Ranges of t from 24 to 110 hr hqave been observed. Excreted mainly unchanged in urine.resistance develops slowly.

CONTRAINDICATIONS
Hypersensitivity to aminoglycosides,long-term (except streptomycin for tuberculosis).

SIDE EFFECTS
ototoxicity:both auditory and vestibular damage have been noted. Increased risk with poor renal function and in the elderly.Auditory symstoms include dizziness,nystagmus,vertigo, and ataxia.Renal impairment:Characterized by cylindruria, protienuria, azotemia, hematuria increased/decreases in frequency of urination; increased BUN, NPN, or creatininie; and incearsed thirst.Neurotoxicity: neuromuscular blockade, headache, tremor, lethargy, paresthesia, peripheral neuritis(numbness, tingling, or buring of face/mouth), arachnoiditis, encephalopathy, actue OBS. CNS delpression, characterized by stupor, flaccidity, and rarely,coma, and respiratory depression in infants. Optic neuritis with blurred/loss of vision. GI:N&V, diarrhea inceased salivation, anorexia, pruritus, burning, fever, stomatitis,eosinophilia. Rarely, agaranulocytosis and anaphylaxis. Cross-allergy among aminoglycosides has been observed. Miscellaneous: joint pain, laryngeal edema, pulmonary fibrosis, superinfection.

Nursing intervention to overcome side-effect

1. Monitor VS and I&Q;incease fluids to prevent renal tubule irritations. 2. Monitor drug levels (e.g.,Amikacin levels >30 mcg/ml are considered toxic). 3. With vestibular dydfunction protect by supervised ambulation and side rails; note (potential for) fall hazard. 4. Assess for ototoxicity with pretreatment audiograms. Hearing loss is a doserelated side effect of drug therapy most commonly associated with amikacin, kanamycin, neomycin, or paromomycin. Tinnitus, dizziness, and loss of balance are also signs of vestibular injury and more commonly seen with gentamicin and streptomysin. Deafness may occur several weeks after discontinuing drug. 5. Do not administer concurrently or sequentially with a topical or systemic nephrotoxic or ototoxic drug (e.g.,potent diuretics such as ethacrynic acid or furosemide)unless provider designates benefits outwegiht risks. 6. Observe for neuromuscular blockade with muscular weakness leading to apnea, when administered with a muscle relaxant, after anesthesia, or too rapidly during IV infusion. Have calcium gluconate or neostigmine available to reverse blockade. 7. With IM injections select large musthigh mass such administer deep to prevent tissue and damage. May use ice to relieve pain at injection site. 8. Note cells or casts in the urine, oliguria, protienuria, lowered specific gravity, increasing BUN/creatinine, all of which indicate altered renal function.

Drugs interactions and adverse effect.

Renal damage may occur if gentamicin is combined with furosemide (frusemide). Gentamicin is ototoxic, caursing disorders of balance and hearing, which are doserelated. Gentamine augments the action of curare-like neuromuscular blocking agent. It should be avoided during pregnancy,as it is ototxic to the fetus.

FLUROQUINOLONES
The fluroquinolones are synthetic antibacterial agents, and not derived from bacteria. They are included here because they can be readily interchanged with traditional antibiotics. An earlier, related class of antibacterial agents, the quinolones, were not well absorbed, and could be used only to treat urinary tract infections. The fluroquinolones, which are based on the older group, are broad-spectrum bacteriocidal drugs that are chemically unrelated to the penicillins or the cephaloprosins. They are well distributed into bone tissue, and so well absorbed that in general they are as effective by the oral route as by intravenous infusion.

EXAMPLES OF DRUG  
Ciprofloxacin hydrochloride Levofloxacin

USES
Used for the large number of gram-positive and gram-negative infections.

ACTIONS
Synthetic, broad- spectrum antibectrial agents. The fluorine molecule confers increased activity against garm-negative organisms as well as broadens the spectrum against gram-positive organisms.are bactericidal agenst by interfering with DNA gyrace and topoisomerase IV. DNA gyrace is an enzymes needed for the replications, transcription, and repair of bacterial DNA. Topoisomerase IV plays key role in the partitioning of chromosomal DNA during bacterial cell division.ciprofloxacin, levofloxacin, ofloxacin, and trovafloxacin may be given IV; all fluoroquinolones may be given PO.

PHARMACOKINETICS
Food may delay the absorption of ciprofloxacin, lomefloxacin,and norfloxacin.

CONTRAINDICATIONS
Hypersensitivity to the quinolone group of antibiotic, including cinoxacin and nalidixiic acid.tendinitis or tendon rupture associated with quniolone use. Clients receving disopyramide and amiodarone or other drugs (E.g..,quinidine,procainamed,sotalol.) that prolong the QTc interval and which may cause torsade de pointes. Lactation. Use in children less than 18 years of age. Gatifloxacin with the diabetes mellitus.

SIDE EFFECTS
The following side effects are common to each of the fluoroquinolones antibiotic.GI:n=N&V diarrhea,abdimonal pain or discomfort, dry or paintful mouth, heartburn, dyspepsia, flatulence, constipations, pseudomembranous colitis.CNS: headache, dizziness, malaise, lethargy, fatigue, drowsiness, somnolence, depression insomnia, seizures, paresthesia. Dermatologic: rash,photosensitivity, pruritus(exepts for ciprofloxacin). Hypersensitivity reactions: facial or pharyngeal edema, dyspnea, urticeria, itching, tingling, loss of consciousness, CV collapse. Other: visual disturbances and ophthalmic abnormilities, hearing loss, superinfection, phototoxicity, eosinophillia, crytalluria, Achilles and other tendon inflammation and rupture. Fluoroquinolones, except norfloxacin, may also cause vaginitis, syncope, chills, and edema.

DRUG INTERACTIONS
y Antacids / decrease serum fluoroquinolone levels R/T down GI tract absorption anticoagulants /increase anticoagulants effects. Anticoagulant / increase anticoagulant effects Cimetidine / decrease elimination of fluoroquinolones Cyclosporine / increase risk of nephrotoxicity didanosine / down serum fluoroqurinolone levels R/T down GI tract absoription due to Mg and AI buffers present in didanosine tablets. Iron salts / decrease serum fluoroquinolone levels R/T decrease GI tract absorpyion NSAIDs / increase risk of CNS stimulation and seizures.

y y y

TETRACYCLINES
Tetracyclines got their name because they share a chemical structure that has fourbacteriostatic agents, the tetracyclines may be effective against a wide variety of microorganisms, including rickettsia and amebic parasites.

EXAMPLES OF DRUG
 Demeclocyline  Doxcycline monohydrate

USES
y infection caused by Rickettsia(Rocky Mountain spotted fever, typhus fever and the typhus group,Q fever, rickettsial pox and tick fevers); Mycoplsma pneumonia; agents of psittacosis and ornithosis;agents of iymphogranuloma venereum and granulamo inguinale; borrelia recurrentis. gram-negative infections caused by Haemophilus ducreyi (chancroid);yersinia pestis (plague) and francisella tularenisi (tularemia). Bartonella bacilliformis, bacteroides species, campylobacter fetus, vibrio cholera (cholera), brucella species (with streptomycin). infections due to Chlamydia trachomatis(lymphogranuloma venereum, trachoma, inclusion conjunctivitis, uncomplicated urethral, endia psittaci(psittacosis), borrelia species(relapsing fever),Ureaplasma urealyticum(nongonococcal urethritis).

ACTION
Tetracyclines inhibit protein synthesis by microorganisms by binding to the ribosomal 30S subunit, thereby interfering with protein synthesis. They block the binding of aminoacyl transfer RNA to the messenger RNA complex. Cell wall synthesis is not inhibited. Are mostly bacteriostatic and are effective only against multiplying bacteria.

PHARMACOKINETICS
Adequately, but incompletely,sorbed from the GI tract. Well distributed thoughout all tissues and fluids and diffuse though noninflamed meninges and the placental barrier. Are deposited in the fetal skeleton and calcifying teeth. t :7-18.6 hr(see individual agents). Increased in the presence of renal impairment. They bind to serum protein (range:20-93%; see individual agents).concentrated in the liver in the bile;excreted mostly unchanged in the urine and feces.

CONTRAINDACTIONS
Use of PO product for streptococcal disease unless organism has been shown to be susceptible. Tetracyclines are not the drug of choice to treat any type of staphylococcal infection. HOW SUPLIED Capsule: 250 mg, 500 mg,;syrup: 125 mg/Ml DOSAGE(usual) Adult : 500 mg 4 times a day or 250 mg 4 times per day. Children over 8 years : 25-50 mg/kg/day in four equal doses. STORAGE Store products below 30 C (86F) protected from light and excessive heat.

SIDE EFFECTS
Demeclocycline may cause increased photosensitivity. Minocycline may cause dizziness. Do not use tetracyclines in children under the age of eight, and specifically avoid during periods of tooth development. Oral tetracyclines bind to anions such as calcium and iron. Although doxycycline and minocycline may be taken with meals, patients must be advised to take other tetracycline antibiotics on an empty stomach, and not to take the drugs with milk or other calcium-rich foods. Expired tetracycline should never be administered. Pregnancy category D. Use during pregnancy may cause alterations in bone development.

INTERACTIONS
There are several significant drug interactions associated with the use of tetracycline. When tetracyclines are taken with antacids, antidiarrheal drugs, dairy products, or iron preparations, the oral absorption of the tetracycline is reduced. Tetracycline can potentiate the effects of oral anticoagulatants, which necessitates more frequent monitoring of anticoagulant effect and possible dosage adjustment. They can also antagonize the effects of bactericidal antibiotics and oral contraceptives. In addition, depending on the dosage, they can cause blood urea nitrogen levels to be increased.

NURSING CONSIDERATIONS
Treat streptococcal infections for at least 10 days Decrease recommended doses and/or extend intervals in those with renal impairment. Food, some dairy products,and antacids containing AI, Ca, or Mg interfere with tetracycline absorption. In renal impairment, decrease the dose or extend dosing intervals. Under no circumstances should outdated tracyclines be given:degradations products of tetracyclines are highly nephrotoxic and may cause a fanconilike syndroms.

NURSING RESPONSIBILITY
Tetracycline tablets should be swallowed whole with the patient sitting or standing and washed down with plenty of water. Absorption is reduced by concurrent administration of iron, calcium or magnesium compounds (including milk).

DRUG OF PENICILLINS
Amoxicillin(amoxil,Tri mox, wymox,Others)(B)

PHARMOCOLOGIC USUAL CLASS DOSAGE RANGE

Aminopecillin Pediatric PO:40-90 mg/kg/day divided q8-12h Adult PO:250-500 mg q8h Adult PO/IV/IM:1-12 g/day Divided q4-6h Pediatric 50-400 mg/kg/day divided q4-6h Adult IV:500-1000 mg q4h Pediatric IV:50-200 mg/kg divided q4-6h Adult and pediatric PO;125-500 mg q6-8h Adult and pediatric IV:150-300 mg/kg/day Divided q4-6h Adult IV:150-300 mg/kg/ day divided q4-6h

INDICATIONS
Otitis media;sinusitis; various susceptible respiratory,skin,and urinary tract infections; dental prophylaxis for bacterial endocartiditis;Helicobacter Pylori inferction Primarily infection with gram-negative organisms such as Shigella, Salmonella, Escherichia, Haemophilus, Proteus, and Neisseria spp; infection with some grampositive Infection with penicillinaseProducing staphylococci

Ampicillin(Principen, Totacillin, others)(B)

Aminopecillin

Naficillin (generic only) (B)

Penicillinase-resistant Penicillin

Penicillin V potassium

Natural penicillin

Primarily infection with gramNegative organisms such as Streptococcus (including Streptococcus pnemoniae) and Staphylococcus spp.

Ticarcillin disodium

Extended- spectrum Penicillin

Primarily infection with gram- nergative organisms such as pseudomonas,Escherichia ,proteus, and enterobacter spp.,but also infection with Steptococcous faecalis (Enterococcos).

DRUG OF CEPHALOSPORINS
Cefazolin (Kefzol, Ancef) (B)

PHAMOCOLOGIC USUAL CLASS DOSAGE RANGE

First-generation cephalosporin Adult IV/IM:500-1000 mg q6-8h Pediatric IV/IM:25-50 mg/kg/day Divided q6-8h

INDICATIONS
Comparable to those for cephalexin plus active against some penicillinaseproducing and more gram- negative organisms; preop and postop surgical prophylaxis Infecid tion of respiratory tract and skin caused by selected grampositive and gramnegertive organisms Less coverage of gram-positive organisms, greate coverage of gramnegative and anaerobic organisms More extensive coverage of gramnegative organisms, including pseudomonas spp.

Cefditoren pivoxil

Fourth-generation cephalosporin

Adult and pediatric older than 12 yr PO:200-400 mg bid

Cefoxitin

Second-generation cephalosporin

Adult IV/IM:3-12 g/day divided q4-6h

Ceftidime (Fortanz, Tazidime)

Third- generation cephalosporin

Cephalexin (keflex,biocep) (B)

First-generation cephalosporin

Adult IV/IM:250-2000 mg q8-12h Pediatric IV/IM:30-50 mg/kg/day Divided q8-12h Adult PO:1-4 g/day divided bid-qid. Pediatric PO:125-500 mg bid-qid.

Infections of respiratory and GU tract ,skin, and bone;otitis media caused by various susceptible grampositive and gramNegative organisms

DRUG OF PHARMOCOLOGIC USUAL FLUOROQUINOLONES CLASS DOSAGE RANGE

Ciprofloacin (cipro) Fluoroquinolone Adult* IV: 200-400 mg q12h.

INDICATIONS
Broad grampositive and gramnegative for coverage infections throughout the body. Vrious susceptible bacterial infections.

Levofloxacin( levaquin)

Fluoroquinolone

Adult only IV/PO: 250750 mg once daily.

DRUG OF PHARMOCOLOGIC USUAL TETRACYCLINES CLASS DOSAGE RANGE

Demeclocycline (Declomycin) (D) Tetracycline Adult PO:150 mg qid or 300 mg bid Pediatric older than 8 yr* 6-12 mg/kg divided bid-qid Doxycline (vibramycin, Monodox, others) (D) Tetracycline Adult PO:200 mg first day,then 100 mg daily thereafter Pediatric older than 8 yr* PO:4.4 mg/kg first day followed by 2.2 mg/day daily thereafter

INDICATIONS
Broad antibacterial coverage, including treatment of skin infections and respiratory, GI, and GU tract infection.

Comparable to that for demeclocycline.