Anti-bacterial Flashcards

1
Q

Which antibiotics target cell wall?

A

Penicillins
Cephalosporins
Carbapenems
Glycopeptides (vancomycin)

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2
Q

Which antibiotics target DNA synthesis?

A

Fluoroquinolones

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3
Q

Which antibiotics target DNA polymerase?

A

rifampin

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4
Q

Which antibiotics binds ribos and inhibit protein synth?

A

Aminoglycosides
tetracyclines
macrolides
Clindamycin
Chloramphenicol
Linezolid

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5
Q

What antibiotic classes are bacteriostatic?

A

Sulfonamides
Tetracyclines
Macrolides
Lincosamides

Stop growth

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6
Q

What antibiotics are bacteriocidal?

A

Cell wall inhibitors (penicillins, cabapenems, monobactams, glycopeptides)

Aminoglycosides (irreversibly inhibit protein synth)

Quinolones (prevent DNA replication through inhibition of DNA uncoiling)

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7
Q

Describe what an antagonistic antibiotic combination is

A

When combined drug has less effect than either of the agents alone

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8
Q

Describe an additive antibiotic combination

A

When combined effect of both drugs is equal to the sum of the individual drug’s independent effects

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9
Q

Describe an synergistic antibiotic combination

A

When the combined effect is greater than the sum of the independent effects

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10
Q

Describe an indifferent antibiotic combination

A

When combined effect is similar to the greater effects produced by either of the drugs alone

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11
Q

What are some examples of synergistic antibiotic combinations?

A

beta-lactam abx + aminoglycosides

glycopeptide abx + aminoglycoside

Sulfamethoxazole + trimethoprim

Amphotericin B + flucytosine

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12
Q

What are some examples of antagonistic antibiotic combinations?

A

Beta-lactamabs + tetracycline OR chloramphenicol

Penicillin + macrolide

Aminoglycoside + chloramphenicol

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13
Q

Which antibiotics have a time-dependent mechanism?

A

Penicillins
Cephalosporins
Glycopeptides
Macrolides
Lincosamides
Tetracyclines

AUC/MIC

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14
Q

Which antibiotics have a concentration-dependent mechanism?

A

Aminoglycosides
Fluoroquinolones

Cmax/MIC

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15
Q

What are the simple penicillins?

A

Benzylepenicillin (PenG), acid labile (destroyed by stomach acid, IV only)

Phenoxymethylpenicillin (PenV), acid stabile (when high [tissue] not required

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16
Q

What are the repository forms of penicillin?

A

Benzathine penicillin

procaine penicillin (more soluble)

*both forms are IM only, IV will kill

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17
Q

What are the anti-staph penicillin?

A

Dicloxacillin, Flucloxacillin = similar pharmacokinetics, antibacterial action, indication

Methicillin

Oxacillin

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18
Q

What are the aminopenicillins?

A

Amoxycillin

Ampicillin

Unable to protect against b-lactamase

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19
Q

What are the antipseudomonal penicillin?

A

Piperacillin, ticarcillin = alone, not resistant to beta lactamase

b-lactamase resistant = piperacillin w/ tazobactam, ticarcillin w/ clavulanic acid

*example of pharmaco-enhancement

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20
Q

What are the common ADRs of penicillin?

A

Diarrhoea, nausea, Superinfections (inc candidiasis = dec lactobacilli)

erythema, exfoliative dermatitis, angioedema

Anaphylactic shock, bronchospasm, serum sickness, electrolyte disturbances (sodium or potassium concentration), steven johnson syndrome, toxic epidermal necrolysis

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21
Q

What are the ADRs of di/flucloxacillin?

A

inc liver enz and bilirubin

Cholestatic hepatitis

Fluclox more hepatic ADRs

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22
Q

What are the ADRs for aminopenicillins?

A

Vomiting, diarrhoea = ampicillin

Pseudo-allergy

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23
Q

What are some antipseudomonal ADRs?

A

Rare = transient inc in liver enz bilirubin

Bleeding abnormalities w/ high dose = prolonged bleeding, altered platelet aggregation

Hypokalaemia

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24
Q

List penicillin precautions

A

Pregnancy/BF = safe

Renal impairment = dose reduced in renal impaired

Penicillin is incompatible with many substances (inc aminoglycosides), give separately

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25
Describe how pharmacoenhancement is used with penicillin?
The use of probenecid to inhibit renal secretion and inc serum levels of penicillin
26
What are the class A beta-lactamase enz?
Clavulanate/ clavulanic acid
27
What are the class B beta-lactamase enz?
Tazobactam sulbactam
28
What are the first generation cephalosporins?
Cephazolin, cephalexin, cefalotin
29
What are the second generation cephalosporins?
cefaclor, cefoxitin, cefuroxime
30
What do the first and second generation cephalosporins have in common?
Moderate spectrum drugs
31
What are the 3rd generation cephalosporins?
cefotaxime, ceftriaxone, ceftazidime Extremely good at penetrating the BBB
32
What are the 4th generation cephalosporins?
cefepime
33
What do the 3rd and 4th generation cephalosporins have in common?
they're all broad spectrum
34
What are the ADRs of cephalosporins?
Diarrhoea, nausea, rash, electrolyte dist Vom, headache, dizziness, oral/vaginal candidiasis, c. diff associated disease (antibiotic induced pseudomembranous c.diff) Anaphylactic shock, bronchial obstruction, urticaria, haemolytic anaemia, angioedema, steven johnson syndome
35
What are the cephalosporins precautions?
Allergy to cephalosporins due to penicillin allergy (urticaria, anaphylaxis or intestinal nephritis)
36
List the relevant carbapenems
Imipenem (given 6 hrs, high seizure risk) meropenem (given 8hrly) ertapenem (given once daily)
37
What inactivates imipenem? How prevent?
Renal dehydropeptidase I inactivates Prevent = cilastin --> inhibits renal dehydropeptidase
38
What are the ADRs of carbapenems?
Imipenem = Neurotoxicity --> myoclonic activity, confusion, seizures (esp in hx of CNS disorders, renal impairment) Meropenem = less neurotoxic Ertapenem = seizures with CNS disorders or renal disorders
39
Name the monobactams and relevant facts
Aztreonam = less toxic than aminoglycosides, more stable than cephalosporins to AMP c beta-lactamase produced by G-ve organisms susceptible to extended spectrum beta-lactamases (made by Klebsiella, E. coli, Enterobacter species
40
What are the relevant glycopeptides and their MOA?
Vancomycin, teicoplanin MOA = prevent transpeptidase from snipping terminal transpeptidase on glycopeptide of bacteria preventing final stage of bacterial cell wall synthesis Time dependent inhibition of bacterial cell wall cross linking
41
What are the ADRs of glycopeptides?
Reversible ototoxicity = vestibular and cochlear Excessive infusion = erythematous rash on face and upper body 0% oral absorption, thus IV administration
42
Name the relevant macrolide antibiotics and a unique characteristic of the class
Erythromycin (prokinetic --> inc GI motility) Clarithromycin, azithromycin (anti-inflammatory) roxithromycin, telithromycin
43
What are the ADRs of macrolides?
N/V, diarrhoea, abdominal cramps, pain Rash, fixed drug reaction Anaphylaxis, acute resp distress, Stevens-Johnson's syndrome, psychiatric disturbance, hearing loss, seizures Clostridium C.diff associated disease, hepatitis, pancreatitis
44
What drugs do macrolides interact with?
Erythromycin = Cytochrome P450 inhibitor, inc serum levels (theophylline, carbamazepine, cyclosporine, diazepam, warfarin, lovastatin Azithromycin, not a sig P450 inhibitor
45
List the lincosamides and their ADRs
Clindamycin (freq dosing), lincomycin ADRs = antibiotic pseudomembranous colitis (there's more)
46
Name the relevant tetracyclines
Doxycycline, minocycline, tetracycline
47
List some ADRs of tetracyclines
N/V, diarrhoea, epigastric burning, tooth discolouration*, enamel dysplasia, reduced bone growth* Stomatitis, fungal overgrowth nail discolouration, oesophageal ulcers, C. diff associated disease, hepatitis, fatty liver degeneration, allergic reactions
48
List some tetracycline precautions
Systemic lupus erythematosus Treatment w/ oral retinoids = inc risk of benign intracranial HTN Mindful of co-treatment w/ other hepatotoxic drugs Renal impairment = doxycycline + minocycline can be dose adjusted Hepatic impairment = hepatotoxicity more likely
49
Discuss the use of tetracyclines in children
Children <8 = discolour teeth, cause enamel dysplasia --> inc risk of dental carries Deposits into bone --> deformities and growth inhibition
50
Discuss the use of tetracyclines in pregnancy and breastfeeding
Preg = safe in first 18 wks (16wks post conception) -->C/I after this BF = courses of 7-10 days --> safe
51
List the relevant aminoglycosides and their route of administration
Gentamicin, tobramycin, amikacin, streptomycin Parenteral only (no oral absorption)
52
List ADRs of aminoglycosides
Nephrotoxicity = treatment >7-10 days, gradual non-oliguric renal failure (acute tubular necrosis --> reversible) Ototoxicity = vestibular ototoxicity (n/v, vertigo, nystagmus Cochlea toxicity (hearing loss,= hearing loss, tinnitus, fullness in ear
53
List some aminoglycoside precautions
Allergic reactions, hx of treatment w/ nephrotoxic/ototoxic drugs (inc risk of toxicity) Inc risk of toxicity = tinnitus, vertigo, hearing impairment, abnormal audiogram Neuromuscular disease (e.g. myasthinea gravis)= inc muscle weakness/resp depression Inc risk of neuromuscular ADRs = hypocalcaemia, hypermagnesemia, general anaesthesia, large transfusion of citrate blood Dehydration = inc tox risk/nephrotox + ototox risk
54
List the relevant quinolones
Ciprofloxacin, ofloxacin, gatifloxacin, moxifloxacin Norfloxacin = poor systemic F, reserved for UTI
55
List quinolone ADRs
rash, itch, n/v, diarrhoea, abdominal pain, dyspepsia
56
What are some precautions w/ quinolones?
Serious allergic reactions Elderly = inc risk of tendon damage
57
What drugs interact w/ quinolones?
dairy productions, antacids, iron, zinc, or calcium = influence absorption Inc effects of caffeine = reduce intake Ciprofloxacin = inhibits CYP3A4 Gati/moxifloxacin = do not interact w/ hepatically metabolised drugs
58
List the relevant folate inhibitors
Trimethoprim = inhibits tetrahydropholic acid by inhibiting dihydrofolate reductase Sulfamethoxazole = inhibits conversion of PBA to dihydrofolic acid by inhibiting dihydrotetrasynthase
59
What are some ADRs of folate inhibitors?
thrombocytopenia, n/v, fever, hyperkalaemia photosensitivity, blood dyscrasias Megaloblastic anaemia, erythema, crystalluria, urinary obstruction, hypoglycaemia, c. diff associated infection
60
Discuss sulfonamide/sulfur allergies
Allergic to sulfonamide functional group Present as = fever, dyspnoea, cough, rash, eosinophilia serious = anaphylaxis, steven johnson syndrome, serum sickness, hepatitis, vasculitis, pancytopenia
61
What other drugs may someone w/ a sulfur allergy be allergic to?
Sulfonyureas thiazides frusemide celecoxib
62
List some precautions for folate inhibitor antibiotics
Check G6PD def --> inc risk of haemolysis w/ sulfonamides Slow acetylator phenotype = greater risk of ADRs Low urine pH = risk of crystalluria (esp w/ sulfamethoxazole) Drugs which cause K+ retention = trimethoprim --> hyperkalaemia Renal impairment = inc hyperkalaemia or hyperglycaemia, reduce sulfamethox dose
63
What are some C/I for folate inhibitors?
Pre-term infants and neonates <4wks = inc risk of kernicterus --> sulphonamides displace bilirubin from plasma Late pregnancy = neonatal kernicterus, haemolytic anaemia, and jaundice
64
List the relevant nitroimidazole antibiotics
Mentronidazole (anaerobic bacteria) Tinidazole (not in Aus) --> once daily
65
What are some ADRs with nitroimidazole?
N/V, anorexia, abdominal pain, metallic taste, CNS effect Furry tongue, glossitis Hypersensitivity reaction, dark urine, Stevens Johnson syndrome, seizure
66
What are some precautions with nitroimidazole?
Avoid alcohol --> disulfiram effect Avoid use w/ disulfiram --> psychotic reactions Nitroimidazole = neurotoxic, can aggravate existing neurological disease Can cause leucopenia --> those w/ hx of blood dyscrasias Increases fluorouracil toxicity --> avoid w/ fluorouracil Renal impairment = metabolites accumulate in severe impairment, don't need to adjust dose Hepatic impairment = risk of accumulation and tox, reduce dose