Antibiotics Flashcards

1
Q

Drugs commonly affected by renal function

A

Penicillins (neurotoxic, seizures and coma)

Aminoglycosides (nephro and oto toxic), also avoid during pregnancy

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2
Q

Effect of sulfonamides in neonates

A

Kernicterus (competes for albumin)

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3
Q

Effects of tetracyclines on pregnant and breast feeding women

A

Cross placental barrier and into breast milk, Ca chelation leads to teeth discoloration and slow bone growth.

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4
Q

Who should avoid fluoroquinolones and why?

A

Prepubertal kids–> attack cartilage (damage), arthropathy

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5
Q

What ethnic group are slow acetylators?

A

Asians

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6
Q

Drugs to be avoided in patients with G6PD deficiency

A

Sulfonimides, nitrofurantoin & chloramphenicol. Drugs increase hemolysis due to low levels of glutathione.

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7
Q

Effect of sulfamides on diabetics

A

in combination with sulfonylureas can lead to hypoglycemia. blocks K channel–> depolarizes cell–> Ca influx–> insulin release

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8
Q

Drugs effected by abscess

A

Aminoglycosides inactive at low PH–> drain abscess first

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9
Q

How might parenteral drugs be used orally?

A

Aminoglycosides and vancomycin can be used to reduce gut flora prior to intestinal surgery

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10
Q

What drugs give false positive for Clinitest for urine glucose?

A

Penicillins, cephalosporins & tetracyclines

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11
Q

What is mechanism of action for Sulfonamides?

A

Broad spectrum static inducer of G+/G-. Inhibits dihydropteroate synthase, blocks pteridine fusion with PABA in synthesis of folic acid–> no dUMP–> TMP–> no thymidine

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12
Q

What drug is commonly given with Sulfonamides and why?

A

Trimethoprim, inhibit dihydrofolate reductase–> no tetrahydrofolate.

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13
Q

Trimethoprim

A

inhibits bacterial DHFR. Side effects: blood dyscrasias

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14
Q

Pyrimathamine

A

antimalarial – inhibits protozoal DHFR

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15
Q

Methotrexate

A

DHFR. inhibits mammalian, bacterial & protozoal. Used to treat psoriasis and various cancers.

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16
Q

Pralatrexate

A

DHFR. for T cell lymphomas

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17
Q

Sulfisoxazole

A

Sulfonamide. Oral. w/ erythromycin (a macrolide) for otitis media

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18
Q

Sulfamethoxazole

A

Sulfonamide. Oral. w/ trimethoprim, urinary, respiratory & GI infections

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19
Q

Dapsone

A

Sulfonamide. Oral. Leprosy, Pneumocystis carinii pneumonia

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20
Q

Sulfacetamide

A

Sulfonamide. Topical. Ulcerative blephritis, bacterial conjunctivitis

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21
Q

Silver Sulfadiazine

A

Sulfonamide. Topical. Burns, prevent sepsis. silver helps kill micro organism. watch dose.

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22
Q

Mafenide

A

Sulfonamide. Topical. Burns. Can cause metabolic acidosis by inhibiting carbonic anahydrase.

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23
Q

Side effects of Sulfonamides

A

Crystalluria, kernicterus, blood dyscrasia (caution with topical), Hypersensitivity ( Steven-Johnsons, erythema multiform, Rx fever), hyperkalemia

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24
Q

Rx interactions of Sulfonamides

A

Potentiate effect of sulfanylureas, warfarin

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25
Q

Effect of Fuoroquinolones

A

Broad spectrum cidal. G- (DNA gyrase)/ G+ (DNA topoisomerase 4)

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26
Q

Ciprofloxacin

A

2nd gen Fluoroquinolone less active against S. pneumoniae. Opthalmic, best FQ for G-, Rx interactions: reduced theophylline clearance, inhibits CYP3A4/1A2 (Methadone and tizanidine (muscle relaxant))

27
Q

Ofloxacin

A

2nd gen Fluoroquinolone. Opthalmic. oral

28
Q

Gatifloxacin

A

3rd gen Fluoroquinolone. Opthalmic. Solution

29
Q

Gemifloxacin

A

3rd gen Fluoroquinolone. Respiratory

30
Q

Levofloxacin

A

3rd gen Fluoroquinolone. Respiratory. Ofloxacin isomer. Warning: prolonged Q-T in elderly–> torsades. risk of acute hepititis

31
Q

Moxifloxacin

A

3rd gen Fluoroquinolone. Respiratory. Prolong Q-T in healthy patients, caution if hepatic disease.

32
Q

Besifloxacin

A

4th gen Fluoroquinolone. Conjunctivitis

33
Q

Finafloxacin

A

4th gen Fluoroquinolone. Acute otitis externa (swimmers ear), P. Auruginosa and S. aureas. SE-iching and nausea

34
Q

Side effects of Fluoroquinolones

A
  • Phototoxic
  • Peripheral neuropathy
  • Arthropathy
  • Tendon rupture (over 65 or taking steroids)
  • Diabetics (Increse or decrease sugar, insulin or oral hypoglycemic
  • CNS (convulsions and anxiety)
  • Nausea, vomiting and diarrhea (C. diff, fidaxomicin)
35
Q

Rx interactions with Fluoroquinolones

A

Avoid antacids and iron supplements, decrease antibiotic absorption.

36
Q

Effect of Penicillins

A

Cidal, G+ (inhibit transpeptidase, and therefore cell wall synthesis)

37
Q

How do bacteria become resistant to penicillins?

A

Beta lactamase, cleave beta lactame ring of PNC’s

38
Q

Penicillin G

A

benzylPCN – Given IM-IV. Syphilis, meningitis, endocarditis, pneumonia. uric acid and probenecid increase PCN levels. Dosed in units 1 = 0.6 micromgs, 1 mil = 600 mgs

39
Q

What are the 3 forms of PCN G?

A
  • AQUEOUS (Pfizerpen) solution for IM/IV
  • PROCAINE (generic) suspension for IM. Procaine is a local anesthetic that combines with PCN & slows its absorption. It also helps numb the pain of injection. Available w/ benzathine as Bicillin C-R. CAUTION: Procaine is an ester & some patients are allergic to esters.
  • BENZATHINE (Bicillin L-A) suspension for IM. Longest acting.
40
Q

PCN V

A

Phenoxymethyl PCN, is an acid stable form of PCN for oral use. It is dosed in mgs. Food interferes with absorption of most PCNs so give 1hr before or 1 hr after meals.

41
Q

DICLOXACILLIN

A

Beta lactamase resistant PCN. oral.eliminated by biliary & renal excretion, an advantage in hepatic or renal disease. If one organ is failing, the other organ can generally pick up the slack.

42
Q

OXACILLIN

A

Beta lactamase resistant PCN. parenteral.eliminated by biliary & renal excretion, an advantage in hepatic or renal disease. If one organ is failing, the other organ can generally pick up the slack.

43
Q

NAFCILLIN

A

Beta lactamase resistant PCN. parenteral.eliminated by biliary & renal excretion, an advantage in hepatic or renal disease. If one organ is failing, the other organ can generally pick up the slack.

44
Q

Ampicillin

A

Aminopenicillin (extended G- coverage), combined with sulbactam (B lactamase inh) for peritonitis (Bacteroides fragilis). As an oral prep, amoxicillin can be used for peritonitis after IV therapy to finish off the infection.

OTHER USES:  Many infections including otitis media & as prophylaxis before dental procedures in patients at hight risk (prosthetic heart valve or cyanotic heart disease)
45
Q

Amoxicillin

A

AminoPCN (extended G- coverage), combined with Clavulanate, better oral absorption than ampicillin. As an oral prep, amoxicillin can be used for peritonitis after IV therapy to finish off the infection.

OTHER USES:  Many infections including otitis media & as prophylaxis before dental procedures in patients at hight risk (prosthetic heart valve or cyanotic heart disease)
46
Q

Ticarcillin

A

ANTIPSEUDOMONAS PCNs – Active vs some Pseudomonas & some resistant Proteus but still susceptible to PCNases! Combined with Clavulanate

47
Q

Piperacillin

A

ANTIPSEUDOMONAS PCNs – Active vs some Pseudomonas & some resistant Proteus but still susceptible to PCNases! Combined with tazobactam

48
Q

What are the side effects of PCN’s?

A
  • Hypersensitivity-PCN as hapten–>IgE. Characterized by rashes, fever, bronchospasms, serum sickness, Stevens-Johnson syndrome, anaphylaxis.
  • Diarrhea- Lost of normal gut flora.
  • Superinfection- C. difficile, Pseudomembranous colitis–> Fidaxomacin (RNA polymerase inh), cidal, Nausea, vomiting, GI hemorrhage, anemia, neutropenia.
  • Seizure risk- GABA antagonist–> excitation predominates
  • Jarisch-Herxheimer Reaction in 70-90% of patients w/ 2O syphilis several hrs after 1st injection. Resolves spontaneously. Not an allergic reaction. Tx w/ aspirin. Unclear if due to an endotoxin. Causes flu-like Sx (fever, chills, headache, arthralgia)
49
Q

PCN structure

A

Thiazolidine and B-lactam rings with side chain.

50
Q

Cephalosporin structure

A

Dihydrothiazine and B-lactam rings with side chain.

51
Q

What is the advantage of cephalosporins to PCN’s?

A

Resistant to many PCNases

52
Q

1st gen Cephalosporins

A
  • Resist staph PCNases, G+ and G-: PEcK- Proteus mirabilis, E. coli, Klebsiella pneumoniae
  • Cefazolin
  • Cefadroxil
  • Cephalexin
53
Q

2nd gen Cephalosporins

A
  • less G+ and more G-: HNPEcK- H. influenza & some Neisseria, Proteus mirabilis, E. coli, Klebsiella pneumoniae
  • Cefaclor
  • Cefuroxime
  • Cefotetan
  • Cefprozil
54
Q

3rd gen Cephalosporins

A
  • Much less G+ and much more G-
  • Ceftriaxone
  • Cefotaximine
  • Ceftazidime
  • Cefpodoxime
  • Cefdinir
  • Cefixime
  • Ceftibuten
55
Q

4th gen Cephalosporins

A
  • For G- rods resistant to 3rd gen
  • Cefepime
  • Cefditoren
56
Q

Advance generation Cephalosporrins

A
  • Ceftaroline

- Ceftolozane w/ tazobactam

57
Q

Ceftriaxone

A
  • 3rd gen Cephalosporin
  • protein bound - easily displaces bilirubin from albumin. Do not use if < 3 mo old to ↓ risk of kernicterus unless as a single dose for GONORRHOEAE CONJUNCTIVITIS.
      Good activity vs MENINGITIS (generally from Strep pneumoniae & N. meningitidis)
    
      About ½ is excreted in urine & ½ in bile.  This is good if renal or liver failure.  There have been rare reports of ceftriaxone-induced toxic hepatitis.
    
      FDA WARNING:  Do not use w/ Ca2+-containing products in patients ≤  28 days old even if by different routes or might precipitate in lungs & kidneys.  Fatalities have occurred.  In older patients, give Rxs sequentially.  If IV, flush line between Rxs. Prefer waiting 48 hrs between ceftriaxone & any Ca2+-containing product.
    
      Ceftriaxone can cause sludge (pseudolithiasis), particularly in children.  Characterized by nausea, anorexia, epigastric distress, colic.  Reversible when discontinued.
58
Q

Ceftazidime

A
  • 3rd gen Cephalosporin

- Neurologic SE e.g. myoclonus, EEG changes with ↑ risk if epileptic; disorientation

59
Q

Cefdinir

A
  • 3rd gen cephalosporin

- Excreted mostly unchanged. Binds Fe -> ↓ absorption & reddens feces in infants fed formula high in Fe

60
Q

Cefepime

A
  • 4th gen Cephalosporin
  • Good CNS penetration. Neurological SIDE EFFECTS: disorientation, myoclonus, EEG changes - ↑ risk if epileptic. Mostly renal excretion - adjust dose for renal function.
61
Q

Cefditoren

A
  • 4th gen Cephalosporin

- Pro Rx. Hydrolyzed by esterases during absorption

62
Q

Ceftaroline

A
  • Advanced gen Cephalosporin
  • Pro Rx.
  • Community acquired bacterial pneumonia & complicated skin & skin structure infections, including MRSA. Side effects: nausea, diarrhea, rash
63
Q

Ceftolozane

A
  • Advanced gen Cephalosporin
  • For complicated UTIs & kidney infection (pyelonephritis). ↓ efficacy if renal impairment. Also used with metronidazole for complicated intra-abdominal infections. Side effects: nausea, diarrhea, headache, fever (pyrexia)
64
Q

Cephalosporin Side Effects

A

HYPERSENSITIVITY. Risk of cross-allergy w/ PCN greatest for 1st generation but negligible for 2nd & 3rd generation unless there has been a documented severe type-I IgE-mediated reaction to PCN.

Certain cephalosporins might cause some nephrotoxicity but risk is low compared to aminoglycosides.

FDA: risk of immune-mediated hemolytic anemia