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3028PHM Human Pharm II > Anti-bacterial > Flashcards

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
Q

Describe how pharmacoenhancement is used with penicillin?

A

The use of probenecid to inhibit renal secretion and inc serum levels of penicillin

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26
Q

What are the class A beta-lactamase enz?

A

Clavulanate/ clavulanic acid

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27
Q

What are the class B beta-lactamase enz?

A

Tazobactam

sulbactam

28
Q

What are the first generation cephalosporins?

A

Cephazolin, cephalexin, cefalotin

29
Q

What are the second generation cephalosporins?

A

cefaclor, cefoxitin, cefuroxime

30
Q

What do the first and second generation cephalosporins have in common?

A

Moderate spectrum drugs

31
Q

What are the 3rd generation cephalosporins?

A

cefotaxime, ceftriaxone, ceftazidime

Extremely good at penetrating the BBB

32
Q

What are the 4th generation cephalosporins?

A

cefepime

33
Q

What do the 3rd and 4th generation cephalosporins have in common?

A

they’re all broad spectrum

34
Q

What are the ADRs of cephalosporins?

A

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
Q

What are the cephalosporins precautions?

A

Allergy to cephalosporins due to penicillin allergy (urticaria, anaphylaxis or intestinal nephritis)

36
Q

List the relevant carbapenems

A

Imipenem (given 6 hrs, high seizure risk)

meropenem (given 8hrly)

ertapenem (given once daily)

37
Q

What inactivates imipenem? How prevent?

A

Renal dehydropeptidase I inactivates

Prevent = cilastin –> inhibits renal dehydropeptidase

38
Q

What are the ADRs of carbapenems?

A

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
Q

Name the monobactams and relevant facts

A

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
Q

What are the relevant glycopeptides and their MOA?

A

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
Q

What are the ADRs of glycopeptides?

A

Reversible ototoxicity = vestibular and cochlear

Excessive infusion = erythematous rash on face and upper body

0% oral absorption, thus IV administration

42
Q

Name the relevant macrolide antibiotics and a unique characteristic of the class

A

Erythromycin (prokinetic –> inc GI motility)
Clarithromycin, azithromycin (anti-inflammatory)

roxithromycin, telithromycin

43
Q

What are the ADRs of macrolides?

A

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
Q

What drugs do macrolides interact with?

A

Erythromycin = Cytochrome P450 inhibitor, inc serum levels (theophylline, carbamazepine, cyclosporine, diazepam, warfarin, lovastatin

Azithromycin, not a sig P450 inhibitor

45
Q

List the lincosamides and their ADRs

A

Clindamycin (freq dosing), lincomycin

ADRs = antibiotic pseudomembranous colitis (there’s more)

46
Q

Name the relevant tetracyclines

A

Doxycycline, minocycline, tetracycline

47
Q

List some ADRs of tetracyclines

A

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
Q

List some tetracycline precautions

A

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
Q

Discuss the use of tetracyclines in children

A

Children <8 = discolour teeth, cause enamel dysplasia –> inc risk of dental carries

Deposits into bone –> deformities and growth inhibition

50
Q

Discuss the use of tetracyclines in pregnancy and breastfeeding

A

Preg = safe in first 18 wks (16wks post conception) –>C/I after this

BF = courses of 7-10 days –> safe

51
Q

List the relevant aminoglycosides and their route of administration

A

Gentamicin, tobramycin, amikacin, streptomycin

Parenteral only (no oral absorption)

52
Q

List ADRs of aminoglycosides

A

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
Q

List some aminoglycoside precautions

A

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
Q

List the relevant quinolones

A

Ciprofloxacin, ofloxacin, gatifloxacin, moxifloxacin

Norfloxacin = poor systemic F, reserved for UTI

55
Q

List quinolone ADRs

A

rash, itch, n/v, diarrhoea, abdominal pain, dyspepsia

56
Q

What are some precautions w/ quinolones?

A

Serious allergic reactions

Elderly = inc risk of tendon damage

57
Q

What drugs interact w/ quinolones?

A

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
Q

List the relevant folate inhibitors

A

Trimethoprim = inhibits tetrahydropholic acid by inhibiting dihydrofolate reductase

Sulfamethoxazole = inhibits conversion of PBA to dihydrofolic acid by inhibiting dihydrotetrasynthase

59
Q

What are some ADRs of folate inhibitors?

A

thrombocytopenia, n/v, fever, hyperkalaemia

photosensitivity, blood dyscrasias

Megaloblastic anaemia, erythema, crystalluria, urinary obstruction, hypoglycaemia, c. diff associated infection

60
Q

Discuss sulfonamide/sulfur allergies

A

Allergic to sulfonamide functional group

Present as = fever, dyspnoea, cough, rash, eosinophilia

serious = anaphylaxis, steven johnson syndrome, serum sickness, hepatitis, vasculitis, pancytopenia

61
Q

What other drugs may someone w/ a sulfur allergy be allergic to?

A

Sulfonyureas

thiazides

frusemide

celecoxib

62
Q

List some precautions for folate inhibitor antibiotics

A

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
Q

What are some C/I for folate inhibitors?

A

Pre-term infants and neonates <4wks = inc risk of kernicterus –> sulphonamides displace bilirubin from plasma

Late pregnancy = neonatal kernicterus, haemolytic anaemia, and jaundice

64
Q

List the relevant nitroimidazole antibiotics

A

Mentronidazole (anaerobic bacteria)

Tinidazole (not in Aus) –> once daily

65
Q

What are some ADRs with nitroimidazole?

A

N/V, anorexia, abdominal pain, metallic taste, CNS effect

Furry tongue, glossitis

Hypersensitivity reaction, dark urine, Stevens Johnson syndrome, seizure

66
Q

What are some precautions with nitroimidazole?

A

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

3028PHM Human Pharm II (17 decks)

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