CEPHALOSPORINS

 Group of antibiotics chemically and pharmacologically related

to the penicillin.
 First introduced in 1960s; FUNGUS (cephalosporium
acremonium) discovered in seawater (1948)
 Effective against gram + and gram – bacteria
 Resistant to beta-lactamase
 1960 – cephalosporins used with clinical effectiveness
 BACTERICIDAL OR BACTERIOSTATIC depending upon:
 Susceptibility of the organism being treated
 Dose used
 Tissue concentration of the drug
 Rate at which bacteria are multiplying
 CEPHALOSPORINS

 PHARMACOKINETICS
PHARMACODYNAMICS:
{IM} {PO} {IV}
[A]:PO well absorbed ONSET : rapid rapid immediate
[D] :PB 75-85% PEAK : 0.5-2 hrs 0.5-1 hr 5-15’
[M]:SHL – t ½ = 1.5 -2.5 hr DURATION: ----UNKNOWN ---
[E]:unchanged in urine 60%-80%
 BACTERIA
classifications SUSCEPTIBLE
1ST GEN Effective against gram Proteus mirabilis
“fa”/ “pha” (+) and gram (-) Escherichia coli
bacteria (BROAD Klebsiella pneumoniae
SPECTRUM) [strepto & staph}
 Can be destroyed by
B-lactamase
produced by
bacteria [PEcK]
 : RI, Skin,GU, bone,
myocardial
infections
 Cefadroxil,cefazolin,
cephalexin
2ND GEN BROADER PEcK + HEN
“fo”/ “fu” SPECTRUM against Haemophilus
gram (-) bacteria influenzae
(diminished activity Enterobacter
against gram (+) aerogenes
bacteria Neisseria
 NOT affected by B- gonorrhea/meningitidis
3rd GEN BROADER gram (- HENPEcKS
“ft” )activity and less Serratia
activity against marcescens
gram (+) bacteria
than 2nd gen
 Resistance to B-
lactamases
 Ceftriaxone,ceft
azidime,
cefixime,cefdinir
4th gEN Greater action PEcK
“fe” against gram (-) and Staphyloccoci &
minimal action streptococci,
against gram (+) Pseudomonas
organisms aeruginosa
 Resistant to most
B-lactamases
 cefepime
(Maxipime)
SIDE EFFECTS:

 ORAL - GI: Flatulence, NAVDA (bloody stool-

{stop} / {best administered with food or milk –
increase absorption}
 BEST to be taken on an empty stomach
 IF with gastric irritation – take with food
 Fever, rash, pruritus, headaches, vertigo (CNS
symptoms) =HYPERSENSITIVITY RXN {STOP}
 IV/ IM - prolonged /high doses = PHLEBITIS or
THROMBOPHLEBITIS {mgt: use small gauge
needle, large veins, alternate infusion sites}
ADVERSE REACTIONS:
 NEPHROTOXICITY- RENAL FAILURE

 SUPERINFECTIONS

 ANAPHYLAXIS

 DRUG INTERACTIONS:
cefmetazole (1st) DISULFIRAM-LIKE REACTION
cefoperazone (3rd) + ALCOHOL = flushing, dizziness, headache,
Moxalactam NV, muscular cramps, chest pain, palpitions,
dyspnea == may lead to extreme CV
collapse, convulsion & death

 With aminoglycosides/vancomycin === INCREASED

NEPHROTOXICITY
 With anticoagulant or thrombolytics/NSAIDS – increased RISK of
bleeding {monitor blood loss}
 CEPHALOSPORINS

 EDUCATION:
 Administer on an empty stomach
 Refrigerate ORAL suspension

 False urine test for GLUCOSE with use of

clinitest tab or Benedict’s solution, therefore
use blood to check for glucose level.
 TETRACYCLINES

 Isolated from STREPTOMYCES AUREOFACIENS in 1948.

 1st broad spectrum antibiotics effective against gram (+)
bacteria & many organisms [mycobacterium, rickettsiae,
spirochetes, chlamydiae]
 Not effective against S. aureus, Pseudomonas or Proteus
 Can be used against Mycoplasma pneumoniae.
 + Metronidazole and bismuth subsalicylate == useful in
treating Helicobacter pylori (peptic Ulcer)
 ORAL and TOPICAL tetracycline – used to treat severe acne
vulgaris
 Tetracyclines

 MOA
 INHIBIT BACTERIAL P[ROTEIN SYNTHESIS
{Bacteriostatic}
 continuous use of tetra – resulted in bacterial
resistance; increased resistance in the treatment
of pneumococci & gonococci infections
 CLASSIFICATIONS
SHORT ACTING
 tetracycline {Tetracyn, Panmycin} >gram (+), gram (-), RT, skin
disorders, chlamydial, gonnorhea, syphilis, ricketssial
[t ½ = 6-12 hrs]
 oxytetracycline Hcl {terramycin} > UTI
INTERMEDIATE
 demeclocycline HCl (Declomycin) > broad spectrum

[t ½ = 10-17 hrs]
LONG-ACTING (to be taken with food)
 doxycycline hyclate (Vibramycin) > bacterial infection & acne

 minocycline HCl (Minocin) [t ½ = 11-20 hrs]

 Tetracyclines

 frequently prescribed for ORAL use, available also

for IM [cause pain on injection & tissue irritation];
IV route – treat severe infections
 newer ORAL : DOXYCYCLINE, MINOCYCLINE,
METHACYCLINE : rapidly & complete absorbed
 not to be taken with MAGNESIUM and
ALUMINUM preparation (antacids), MILK-
PRODUCTS containing calcium or Iron-containing
drugs == prevent absorption of the drug
 TAKEN on EMPTY STOMACH – 1 hr ac or 2 hrs
pc (except doxycycline & minocycline)
 SIDE EFFECTS and ADVERSE REACTIONS

 GI- NVD {mgt: SFF, ice chips, replace fluids}

 PHOTOSENSITIVITY – sunburn reaction {sunblock, clothing}
 TERATOGENIC EFFECT – not taken 1st trimester – PC : D
 Discolors teeth (irreversible) == not taken last trimester &
children < 8yrs
 Balance difficulty – damage to vestibular part of the inner ear
(minocycline) {safety}
 NEPHROTOXICITY – if given in high doses
 SUPERINFECTION –disrupt microbial flora {oral hygiene}
 Education

S unlight sensitivity
[decomposes in light/heat = TOXIC- store out
of light & extreme heat]
T ake full glass of H20
 antacid, IRON & MILK
P ut drug into empty stomach
 DRUG INTERACTIONS

 ANTACIDS, IRON containing drugs, MILK –

prevent absorption of Tetra {take 2 hrs apart}
 ORAL CONTRACEPTIVES – lessened effect
of OCP
 PENICILLIN – decreased activity of Penicillin
 AMINOGLYCOSIDES – increased risk
Nephrotoxicity
 AMINOGLYCOSIDES
 ACT by inhibiting bacterial protein synthesis (Bactericidal)
 Used against serious infections caused by gram (-) bacteria
[E. coli, Proteus, Pseudomonas & Serratia]
 Cannot be absorbed in the GIT, cannot cross CSF (in adults
only)
 Primarily administered IV
 DOC : Tularemia & Bubonic Plague

 1st aminoglycosides === STREPTOMYCIN SULFATE – used

in treatment f TB; derived from bacterium Streptomyces
griseus in 1944, administered IV
ORAL PREPARATIONS: given to decrease bacteria in the bowel
1)paromomycin -useful in treating intestinal amebiasis &
tapeworm
2)neomycin - used as preoperative bowel antiseptic
Others: (treat pseudomonas)
 Gentamycin (1963)[IM/IV]> against gram (-) esp.

pseudomonas
 Kanamycin [PO/IM/IV] > for hepatic coma
 Tobramycin (1970) [IM/IV] > kill Pseudomonas
 Amikacin (1970) [IM/IV] > effective against Pseudo esp. if
resistant to gentamicin & tobramycin
 Netilmicin (1980) [IM/IV] > less toxic compared to other
aminoglycosides
 PHARMACOKINETICS

Gentamycin Netilmicin(latest)
PC : C (can’t rule out) PC :D (+ risk)

[A} : IM,IV
[M] : T ½ short (SHL)-3-4X a day,
PB – low
[E] : unchanged in URINE
 PHARMACODYNAMICS

Gentamycin Netilmicin(latest)

ONSET :IM/IV : RAPID IM:RAPID, IV- immediate

PEAK :1-2 hrs 0.5-1.5 hr
DURATION : 6-8 hr unknown
 AMINOGLYCOSIDES

 SIDE EFFECTS :
 GI-NAV; rash, numbness, tremors, visual
disturbances, tinnitus, muscle cramps or
weakness, photosensitivity
 ADVERSE REACTIONS:
 URTICARIA, PALPITATIONS
 Thrombocytopenia

 Superinfections- agranulocytosis

 Liver damage
 AMINOGLYCOSIDES

 Most serious:
 OTOXICITY – 8th cranial nerve damage {safety}

 NEPHROTOXICITY – oliguria {slowly administered}

 NEUROTOXICITY- neuromuscular blockade,

numbness

 INTERACTIONS :
 Penicillin – less effective aminoglycoside

 Anticoagulant (Warfarin)– increased its activity

 NURSING INTERVENTIONS
 Monitor periodical audiograms, BUN/creatinine & vestibule
function studies over 10 days therapy
 Adjust renal insufficiency
 Monitor VS, peak and serum levels
 For IV admin., dilute and administer slowly to prevent toxicity
 Monitor I & O, hydrate well before and during therapy (flush in
between)
 If anorexia or nausea occurs, SFF meals
 Establish plan for safely if vestibular nerve effects occur.
 Administer other antibiotics 1 hour before/after amino
 Recommend using sunblock & protective clothing when
exposed to the sun.
 “THE AMINO MICE”
( toxic mice!!!!! )

“I CAN’T “I CAN’T “I CAN’T

HEAR” PEE..” FEEL”

“ONE CAN’T HEAR” – OTOTOXICITY

“ONE CAN’T PEE..” – NEPHROTOXICITY
“ONE CAN’T FEEL” - NEUROTOXICITY
DRUG COMPUTATION
 Captopril 100 mg daily is prescribed. Captopril 25 mg
tablets are on hand.How many tablets will you give?

 The doctor ordered paracetamol 250mg. If the label on

the multidose vial of paracetamol reads 50mg/cc, how
much paracetamol in cc will you give?

 Clindamycin 1g is prescribed. Clindamycin liquid is

labeled 200mg per 5 mL. How much in mL will you give?