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PHARM > Quinolones, Folic Acid (Folate) Antagonists and Urinary Tract Antiseptics > Flashcards

Quinolones, Folic Acid (Folate) Antagonists and Urinary Tract Antiseptics Flashcards

1
Q

4th generation; anaerobic and gram pos activity

A

Moxifloxacin

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2
Q

Avoid ingestion of dairy, sucralfate, aluminum / magnesium containing antacids, iron, zinc, calcium (2 hours before / 3 hours after taking)

A

Fluoroquinolones

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3
Q

Adjust dosages for renal impairment.

A

Quinolones

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4
Q

Dyspnea, chest pains, chills, fever, cough

Hematologic - especially in G-6-PD

Peripheral Neuropathy
Hepatotoxicity
Birth defects
CNS Effects

A

Adverse effects of Nitrofurantoin

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5
Q

Generally well tolerated
N/V/D , headache, dizziness, lightheadedness, confusion, Phototoxicity

Use caution in CNS disorders, Peripheral neuropathy, Glucose dysregulation (Hypo/hyperglycemia)
Prolongation of QT interval.

Increases serum concentrations of Theophylline, Warfarin, Caffeine,Cyclosporine

A

Adverse Effects / Drug Interactions of Fluoroquinolones

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6
Q

Sulfonamides, trimethoprim and cotrimoxazole are all …

A

Folate antagonists

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7
Q

(Birth defects possible, especially it taken during the first trimester and near term)
Secreted in breast milk (<2 months old can cause kernicterus)

It is a preferred drug for UTIs and is the drug of choice for PCP in patients with AIDs and other immunodeficiencies.

A

Cotrimoxazole (bactrim, TMP/SMZ)

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8
Q

Fluoroquinolones are commonly considered as …

A

alternatives for patients with documented SEVERE B-lactam allergies

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9
Q

Folic acid deficiency: You can ____ it by giving folic acid to patients.

1 mg/day folic acid with prenatal vitamin regimen (at a min)

A

reverse

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10
Q

Shows improved gram-pos coverage, maintains gram-neg activity and gains ANAEROBIC coverage.

A

Fourth generation of Fluoroquinolones

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11
Q

The first drugs available for systemic treatment of bacterial infections. Introduced in the 1930s.

Usage declined once PCN was introduced in the 1940s.

Older agents had low solubility which caused urine crystallization and kidney injury. Newer agents are more water soluble which decreases renal risk.

Primarily used and often preferred for acute UTIs (90% are due to Escherichia coli)

A

Sulfonamides

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12
Q

Resistance of fluoroquinolones comes from an ____ in DNA gyrase and topoisomerase 4.

A

Alteration

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13
Q

Achieves high levels in bone, urine (except which quinolone…?), kidney, prostatic tissue, lungs. Low CSF penetration except _____ (low urine levels, not for UTI).

A

ofloxacin

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14
Q

Avoid _____ with decreased renal fxn.

A

Nitrofurantoin

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15
Q

Enhanced activity against gram + (S. pneumoniae) + excellent activity against many anaerobes

Poor activity against P. aeruginosa, resistant to Bacteroides fragilis

CAP, nosocomial pneumonia

Not indicated for UTIs due to poor concentration in the urine*

A

Moxifloxacin (respiratory quinolone)

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16
Q

Most quinolones are excreted renally.

Adjust dosage in renal impairment (except _____, which is excreted by the liver)

A

moxifloxacin

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17
Q

Accumulates and has activity against intracellular organisms (effective against _____ and mycobacteria)

A

chlamydia

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18
Q

These are less used today, have moderate gram-negative, minimal serum concentrations, restricted to the treatment of UNCOMPLICATED UTIs.

A

First generation of Fluoroquinolones

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19
Q

What enzyme does Sulfonamides inhibit? dihydropteroate ______.

A

synthase

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20
Q

precedes all fluoroquinolones and are not clinically used

A

Naldixic Acid

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21
Q

Retain expanded gram-negative activity and show improved activity against atypical organisms and specific gram-pos bacteria.

A

Third generation of Fluoroquinolones

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22
Q

____ is required by all cells to make DNA, RNA, and proteins

Folate antagonists inhibit sequential steps in the synthesis of tetrahydrofolic acid. In the absence of _____, bacteria are unable to synthesize DNA, RNA and proteins

A

Folate; tetrahydrofolate

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23
Q

Ampicillin and Gentamicin

A

Infant UTI tx

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24
Q

Resistance is due to an alteration in dihydrofolate reductase that has a lower affinity for trimethoprim+ efflux pumps and decreased drug permeability.

Rapidly absorbed after oral administration.

High concentrations are achieved in prostatic and vaginal fluids and CSF.

Can produce effects of folic acid deficiency:

  • Megaloblastic anemia
  • Leukopenia
  • Granulocytopenia
A

Trimethoprim

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25
Q

If breast feeding, avoid ____. Avoid Trimeth/Sulfa also in early stages of infancy.

A

Nitrofurantoin

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26
Q

What enzyme does Trimethoprim inhibit? dihydrofolate _____.

A

reductase

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27
Q

Sulfamethoxazole + Trimethoprim = greater activity together than each working individually.

A

Cotrimoxazole (bactrim, TMP/SMZ)

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28
Q

Respiratory quinolones

A

Levo and Moxi (also against anaerobes)

29
Q

Genetic disorder in african, asian, middle eastern

A

G-6-PD

30
Q

End in “oflxacin”
“collateral damage”
Used for direct inhibitors of DNA synthesis.

A

Fluoroquinolones

31
Q

Given twice daily in capsule form, and more costly than Nitrofurantoin (given q6hrs, available in capsules/suspension).

A

Microbid

32
Q

Used for protozoal infections, anaerobic infections, bacterial vaginosis/vaginitis, Intra-abdominal infections and Trichomoniasis

A

Metronidazole

33
Q

Use off-label for C. diff, Sexual assault prophylaxis + ceftriaxone and azithromycin or doxycycline) and skin and soft tissue necrotizing infections

A

Metronidazole

34
Q

These are the only fluoroquinolones approved in children but generally should be avoided in this population due to tendonitis

A

Cipro and Levo

35
Q

2nd generations

Double A (aerobic gram neg, atypicals)

Double M (mycoplasma and mycobacteria)

Chlamydia

A

Cipro and Norfloxacin

36
Q

Infrequently prescribed due to poor oral bioavailability (what reaches circulation is poor) and a short half-life

Nonsystemic infections

UTI, prostatitis, infectious diarrhea (unlabeled use)

A

Norfloxacin

37
Q

N/V, epigastric distress, abdominal cramps, unpleasant metallic tastes, yeast infections of the mouth

Avoid use of alcohol during therapy or within 3 days of therapy discontinuation – disulfiram-like reaction

A

Adverse effects and contraindications for Metronidazole

38
Q

Bactericidal, Man Made antibiotics, Broad-Spectrum (than other abx), Use has been closely associated with Clostridium difficile and the spread of antimicrobial resistance

A

Fluoroquinolones

39
Q

Stevens-Johnson syndrome:

Rare reaction with a 25% mortality rate.

Widespread lesions of the skin and mucous membrane

Fever, malaise, toxemia

Discontinue ________ immediately if any type of skin rash is observed.

Do not give to any patient with a history of hypersensitivity reactions to other drugs like, thiazide diuretics, loop diuretics, sulfonylurea-type oral hypoglycemics.

A

Sulfonamide

40
Q

Avoid antacids

Not used for upper UTIs (pyelonephritis).

GI distress is the major side effect.

At higher doses – albuminuria, hematuria, rashes.

Contraindicated in renal insufficiency.

Avoid sulfonamides which react with formaldehyde and increases crystalluria risk and mutual antagonism.

A

Methenamine

41
Q

Nitrofurantoin and Methenamine are used for UTIs ONLY. These are considered _______ (class).

Both concentrate in the urine and neither drug achieves effective antibacterial concentrations in the blood/tissues.

A

Urinary Tract Antiseptics/Antimicrobials

42
Q

IV, PO, Opthalmic, Otic = CLM

A

Quinolone Pharmacokinetics

Cipro, Levo, Moxi

43
Q

Suppresses synthesis of tetrahydrofolic acid.

Similar antibacterial spectrum to sulfonamides.

20 – 50 fold more potent than the sulfonamides.

Most often compounded with sulfamethoxazole to = cotrimazole (Bactrim).

Can be used alone in the treatment of UTIs and bacterial prostatitis (although quinolones are preferred)

A

Trimethoprim

Folate Antagonist

44
Q

Avoid sulfonamide/trimethoprim use in infants < 2 months due to ______ which can be fatal.

A

kernicterus

45
Q

3rd generation; has increased gram pos activity

A

Levofloxacin

46
Q

Hypersensitivity reactions
Rash, drug, fever, photosensitivity
Especially with topical agents.

Blood dyscrasias, hemolytic anemia

Kernicterus in newborns*
Bilirubin induced
Yellow baby syndrome

Crystalluria (renal damage)

A

Adverse side affects of sulfonamides

47
Q

These are well absorbed orally and when used topically may cause systemic effects.

Readily crosses the placenta and can achieve antimicrobial effects and toxicity in the fetus (yellow babies).

Metabolized in the liver by acetylation
Excreted by the kidneys.

A

Sulfonamides

48
Q

Less resistance with the combination than to either drug alone, but still significant resistance has been encountered to E. coli, and MRSA.

Generally administered orally, IV for patients with severe pneumonia caused by PCP.

Readily crosses the BBB.

Adverse effects include: N/V, Hyperkalemia with higher doses. Megaloblastic anemia, leukopenia, thrombocytopenia (possibly fatal).

A

Cotrimoxazole (bactrim, TMP/SMZ)

49
Q

1st Choice in uncomplicated cystitis.

Broad-spectrum antibacterial.

Bacteriostatic at low concentrations / Bactericidal at high concentrations.

Therapeutic levels are achieved only in urine.

Injures bacteria by damaging DNA after enzymatic conversion to an active form. Used for acute infections of the lower urinary tract and for prophylaxis of recurrent lower UTI*

Avoid with significant renal failure. Category B(pregnancy) but contraindicated at term (38+ weeks)
.

A

Nitrofurantoin

50
Q

Fluoroquinolones MOA is inhibition of 2 bacterial enzymes involved in DNA replication.

A

DNA gyrase, Topoisomerase 4

51
Q

Fluoroquinolones, including _____ , are associated with an increased risk of ____ and ____ rupture in all ages. This risk is further increased in older patients (usually older than 60 years), in patients taking corticosteroid drugs, and in patients with kidney, heart, or lung transplants.

A

ciprofloxacin, tendonitis, tendon

52
Q

Inhibits sequential steps in bacterial folic acid synthesis.

Treats UTIs and respiratory tract infections to include Pneumocystis jirovecii pneumonia (PCP), toxoplasmosis.

Activity against MRSA*
Particularly community-acquired skin and soft tissue infections caused by MRSA.

A

Cotrimoxazole (bactrim, TMP/SMZ)

53
Q

Decomposes under acidic conditions and breaks down into ammonia and formaldehyde.

Formaldehyde acts locally and is toxic to most bacteria.

Bacteria do not develop resistance to formaldehyde which is an advantage of this drug.

Frequently formulated with a weak acid (mandelic acid or hippuric acid) to keep the urine acidic.

Very important: Used for chronic suppressive therapy (not treatment) to reduce the frequency of UTIs**

A

Methenamine

54
Q

Sulfonamides are used primarily for _____.

A

UTIs

55
Q

In many micro-organisms, dihydrofolic acid is synthesized from PABA, p-aminobenzoic acid.

Sulfonamides are synthetic analogs of PABA and therefore ____ ____ ___ for the bacterial enzyme, dihydropteroate synthetase

A

compete with PABA

56
Q

Effective in the treatment of many systemic infections caused by gram neg bacilli

Not useful for S. pneumoniae

Complicated and Uncomplicated UTIs

Traveler’s diarrhea (E.coli)
Typhoid fever (Salmonella typhi),
Tuberculosis (2nd line)

Anthrax (Drug of choice, post exposure prophylaxis)

Best activity against P. aeruginosa (commonly used in cystic fibrosis)

A

Ciprofloxacin

57
Q

Resistance of fluoroquinolones comes from a ____ accumulation of the drug intracellularly.

A

decreased

58
Q

Have expanded gram-negative activity and also some activity against gram-positive and atypical organisms, mycoplasma, chlamydia

A

Second generation of Fluoroquinolones

59
Q

After diffusing into the organism, it interacts with DNA to cause a loss of helical DNA structure resulting in inhibition of protein synthesis and cell death

A

MOA of Metronidazole

60
Q

Avoid fluoroquinolones and nitrofurantoin (in the 3rd trimester) for the tx UTIs during _____.

A

Pregnancy

61
Q

Ciprofloxacin, Levofloxacin, Moxifloxacin, Nalidixic acid, Norfloxacin, Ofloxacin (ophthalmic, more than systemic)

A

Fluoroquinolones

62
Q

1st generation quinolone? Very narrow.

A

Naldixic acid

63
Q

Sulfonamides suppress ___ ___ by inhibiting the synthesis of dihydrofolic acid and the formation of tetrahydrofolate (folic acid derivative)

A

bacterial growth

64
Q

Decreased accumulation of fluoroquinolone intracellularly is due to a decreased number of ____ ____ to the outer membrane of the resistant cell which impairs access to the topoisomerases.

And

Efflux Pumps – Pumps drug out of the cell

A

porin proteins

65
Q

Excellent activity against S. pneumoniae (unlike Cipro)

Complicated and Uncomplicated UTIs

Prostatitis, Skin infections, CAP, nosocomial pneumonia

A

Levofloxacin (respiratory quinolone)

66
Q

Fluoroquinolones, including ciprofloxacin, may exacerbate muscle weakness in persons with ___ ___. Avoid ciprofloxacin in patients with known history of ____ ____.

A

myasthenia gravis

67
Q

Gram negative (E. coli, P. aeruginosa, H. Influenzae)

Atypicals (Legionella, Chlamydiaceae)

Gram positive (streptococci)

Some mycobacteria (Mycobacterium tuberculosis)

A

Antimicrobial spectrum for Fluoroquinolones

68
Q

Narrow-spectrum quinolone antibiotic, used only for

UTIs, Some GI infections

A

Naldixic Acid

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