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PHARM/MHD EXAM - 3 > L6 Pharm: Tetracyclines ,Glyclines, Sulfonamides, Chloramphenicol > Flashcards

L6 Pharm: Tetracyclines ,Glyclines, Sulfonamides, Chloramphenicol Flashcards

1
Q

What is an example of a first generation Tetracycline?

Second generation? (2)

A
  1. Tetracycline

2. Doxycylcine, monocycline

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2
Q
  1. What is the mechanism of action of Tetracyclines/Glycylcyclines? (reversible or irreversible)
  2. Prevents the addition of what?
  3. Is it bacteriostatic or bactericidal? How does this change with an increase in concentration?
A
  1. REVERSIBLY binds to the 30s(test) subunit
  2. inhibits the binding of aminoacyl transfer-RNA to the acceptor (A) site on the mRNA-ribosomal complex
    - which prevents addition of amino acid residues on elongating peptide chain

(prevent addition of aminoacyl-tRNA ) - FIRST AID

  1. BACTERIOSTATIC (weird)

bacterioCIDAL at high concentrations

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3
Q

MECHANISMS of RESISTANCE for Tetracyclines/Glycylcyclines

A) Acquisition of genes on mobile elements (plasmids) leads to 3 major mechanisms. State them

B) Is cross- resistance observed? If yes, state for which drugs.

C) which drug is resistant to these resistance mechanisms?

A

A)

  1. Efflux pump
    - decrease accumulation of tetracycline within bacteria
  2. Ribosomal protection protein
    - Cytoplasmic proteins that protects ribosomes from 1st and 2nd generation tetracyclines
  3. Enzymatic Inactivation

B)
Cross-resistance observed between TETRACYCLINES, except for MINOCYCLINE!

C) Tigecycline resistant to these mechanisms

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4
Q

What are the main 5 GRAM POSITIVE AEROBES Tetracyclines can kill?

REMEMBER THE MAIN 1 at least!!!! (stated first)

A
  1. Staph Aureus (MSSA)*** TEST
  2. Strep Pneumo (PSSP)
  3. Bacillus
  4. Listeria
  5. Nocardia
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5
Q

What are the some GRAM NEGATIVE AEROBES Tetracyclines can kill?

A
  1. N. gonorrhea and meningitidis
  2. Haemophilus influenzae (90% susceptible)
  3. Haemophilus ducreyi (chancroid)
  4. Campylobacter jejuni
  5. Helicobacter pylori
  6. Vibrio cholerae, Vibrio vulnificus
  7. Burkholderia pseudomallei (used to be pseudomonas)

NO ACTIVITY AGAINST PSEUDOMONAS!

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6
Q

What miscellaneous bacteria is targeted by Tetracycline?

What 2 gram + anaerobes are targeted by Tetracyclines?

A
  1. Legionella
  2. Chlamydophila
  3. Chlamydia
  4. Mycoplasma
  5. Ureaplasma
  6. Rickettsia
    - bartonella, bordatella, brucella
    pasteurella (ALL THE ELLAS)
    - borrelia
    -treponema
    -leptospira
    -coxiella
    -mycobacterium fortuitum
  7. Actinomyces
  8. Propionibacterium
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7
Q

What gram negative Aerobes are targeted by Tigecycline?

What 2 gram negatives are NOT (test test test)

What 2 Anaerobes?

A
  1. Acinetobacter baumannii
  2. Aeromonas hydrophila
  3. Citrobacter spp.
  4. Escherichia coli
  5. Klebsiella spp.
  6. Serratia marcescens
  7. Stenotrophomonas maltophilia***

TIGECYCLINE HAS NO ACTIVITY AGAINST

  1. proteus
  2. Pseudomonas Aeruginosa

KILLS:

  1. C. Perferingens
  2. BACTEROIDES
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8
Q

What 2 gram negative AEROBES are NOT killed by TIGECYCLINE (test test test)

A

TIGECYCLINE HAS NO ACTIVITY AGAINST

  1. proteus
  2. Pseudomonas Aeruginosa
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9
Q

TIGECYCLINE targets what gram positive aerobes? (greater spectrum than tetracyclines)

(4)

What 2 conditions can TIGECYCLINE NOT be used for?

A
  1. MSSA
  2. MRSA
  3. VRE
  4. VSE

NOT FOR

  1. BACTEREMIA
  2. UTI
  • but can use for prostitis (TMP-SMX is better)

DO NOT USE FOR PROTEUS or PSEUDOMONAS!!!

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10
Q

What is the only drug available BOTH PO & IV?

Which drug is ONLY Iv?

Which 2 drugs have high bioavailability? (best absorbed on an empty stomach)

Absorption of tetracyclines/Glycyclines is impaired by what?

A
  1. Doxycyline
  2. Tigecycline

Doxycycline and minocycline(PO) F = 90 to 100%

  1. Impaired by DI & TRI talent cations (same with fluoroquinolone)
    - no use of dairy, calcium, magnesium, iron etc..
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11
Q

tetracyclines/Glycyclines:

Widely distributed to what areas? (MAINLY?)

Minimial ____ penetration

Do not use for ___ or _____

A
  1. PROSTATE
    - synovial fluid
    - seminal fluid
  2. MINIMAL CSF penetration
  3. Do not use for
    - BACTEREMIA
    - UTI
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12
Q

State the elimination of the following:

  1. Demeclocycline/tetracycline
  2. Doxycycline, minocycline
  3. tigecycline

Are dosage adjustments required in the presence of renal insuficiency?

A
  1. TETRACYCLINE - RENAL elimination
    - minimally removed during HD
  2. NON - renal elimination (metabolism)
  3. Tigecycline - NON RENAL
    - biliary
    * * ADJUST WITH LIVER DISEASE**

Do NOT require dosage adjustment in the presence of renal insufficiency. Adjust tigecycline with liver disease
- similar to Linezolid

(unlike vancomycin, daptomycin, AGs)

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13
Q

What are some clinical uses of Tetracyclines/Glycylcyclines?

3 main ones

A
  1. RESPIRATORY infections
    - CAP (use cephalosporin in hospital)
    - PERTUSSIS (decrease colonization, will not decrease infection)
  2. STDS - CHLAMYDIA, syphillis, gonorrhea(use cephalosporin)
  3. ROCKY MOUNTAIN SPOTTED FEVER

+ MALARIA

  • acne
  • SIADH! (demeclocycline)
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14
Q

What drugs are the treatment of choice for ROCKY MOUNTAIN SPOTTED FEVER?

What specific drug is used for POLYMICROBIAL infections? (skin & soft tissue, intrabdominal)

What drug is used for SIADH?

A

Tetracyclines/Glycylcyclines

TIGECYCLINE!

DEMECLOCYCLINE

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15
Q

What are the 3 main adverse effects of Tetracycline/Tigecycline?

A
  1. GI –> NAUSEA & VOMITING
  • tigecycline
  • Diarrhea, pseudomembranous colitis (C. difficile)
  1. Hypersensitivity
  2. Photosensitivity* (DOXYCYCLINE)
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16
Q

What are tetracyclines/tigecyclines contraindicated for?

What is an adverse RENAL effect with outdated tetracycline?

A
  1. PREGNANCY CATEGORY D
    - Discoloration of permanent teeth and decreased bone growth in children
    (don’t be pregnant and taking tigaaaa)
  2. FANCONI-Like syndrome w/ outdated Tetracycline
    - FANCONI fecked up and took TETRA after it was expired and then could not pee
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17
Q

What is Fanconi Like syndrome?

What drug often causes this if a patient uses an outdated prescription?

A
  1. Fanconi syndrome (also known as Fanconi’s syndrome) is a disease of the proximal renal tubules[1] of the kidney in which glucose, amino acids, uric acid, phosphate and bicarbonate are PASSED INTO URINE, instead of being reabsorbed
  2. TETRACYCLINE
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18
Q

What 3 tetracyclines do NOT need to be reduced in renal insufficiency?

Would tetracyclines work for a pregnant women with a legionella pneumonia?

Do Tetracyclines work for prostatis?

What other drugs are contraindicated in pregnancy?

What drugs contraindicate consuming milk or antacids or enteric feedings (divalent trivalent cations?

What two bus are NOT covered by tigacycline that may be on a polymicrobial infection?

A
  1. DOXYcycline, Minocycline, Tigecycline
  2. NO - Pregnancy Class D (tets)
  3. YEs, penetrate prostate (but TMP - SMX is the drug of choice)
  4. NO FLUOROQUINOLONES no TETRACYCLINEs
  5. FLUROQUINOLONES + Tiga/tetra
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19
Q

What is the mechanism of action of sulfonamides? (which specific enzyme)

Bacteriostatic or cidal?

A
  1. Inhibits Dihydropteroate SYNTHETASE

(no dihydropteroic acid made)

  • Inhibits incorporation of p-aminobenzoic acid (PABA) into tetrahydropteroic acid
    2. BacterioSTATIC

(tidal only in combo with Trimethaprim (TMP))

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20
Q

What is the mechanism of action of Trimethoprim?

Bacteiostatic or cidal?

A
  1. Inhibits Dihydrofolate REDUCTASE
    - blocks conversion of DHF to THF
  2. Bacteriostatic
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21
Q

Is TMP - SMX bacteriocidal or static?

A

BACTERIOCIDAL!!!

  • synergistic activity
  • decreased emergence of resistance

(BACTRIM)

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22
Q

What converts PABA to Dihydrofolic acid?

What drug inhibits this?

What converts dihydrofolic acid to Tetrahydrofolic acid?

What inhibits this and prevents eventual purine formation?

A
  1. Dihydropteroate Synthetase
  2. Sulfamethoxazole
  3. Dyhyfrofolate Reductase
  4. TRIMETHOPRIM
23
Q

What is the mechanism of resistance of SMX?

(3)

TMP?

A
  1. PABA overproduction
  2. Structural change of Dihydropteroate syntheses
  3. Plasmid production of drug resistant DHPS
    or decreased bacterial cell wall permeability to sulfonamides

TMP

  • Chromosomal or plasmid mediated
    1. Plasmid mediated production of DIHYDROFOLATE REDUCTASE resistant to TMP (like SMX)
    2. Change in cell permeability
24
Q

TMP -SMX

  1. Absorption available both ___ and ____
  2. Good distribution to what areas?
  3. Different from Tetracyclines because better able to penetrate _____
  4. Both are eliminated by?
  5. Dose adjustment of Bactrim required with renal insufficiency??? (TEST)
A
  1. ORAL & IV
  2. lungs, urine, PROSTATE
  3. PENETRATES CSF
  4. Both LIVER & KIDNEY
  5. NEED TO ADJUST WITH RENAL INSUFFICIENCY
25
Q

T/F: Dose adjustment of BACTRIM is necessary for renal insufficiency.

A

TRUE!!!!

TEST

26
Q

What are the 5 clinical uses of TMP - SMX? (start with most important)

A
  1. UTI!!! (acute, chronic, recurrent)
  2. Prostatis
  3. Skin infections due to CA-MRSA!
  4. Bacterial sinusitis
  5. NOCARDIA**
27
Q

What drug is the treatment of choice for nocardia? (TEST)

A

TMP -SMX

BACTRIM!!!

28
Q

What are the 5 main clinical uses of TMP - SMX?

A
  1. PNEUMOCYSTIS CARINII pneumonia
  2. Stenotrophomonas
  3. Toxoplasmosis
  4. Listeria Monocytogenes
  5. NOCARDIA
29
Q

TMP-SMXAdverse Effects:

  1. State for GI
  2. State for Hematologic (2 main)
  3. Skin?
A
  1. GI:
  • nausea, vomiting, diarrhea, glossitia
  • jaundice
  • hepatic necrosis
  • FOLLOW RENAL FUNCTION WHEN USING BACTRIM
  1. Hemotologic:
    - LEUKOPENIA, THROMBOCYTOPENIA

eosinophilia
Acute hemolytic anemia, aplastic anemia, agranulocytosis
Megaloblastic anemia (impaired folate usage with prolonged administration)

  1. RASH –> HYPERSENSITIVITY!!!
  2. CNS - headaches, seizures, meningitis
  3. Renal toxicity!!!!
  4. Lupus via Steven JOhnson Syndrome
  5. CRYSTALLURIA
30
Q

What drug causes Leukopenia & thrombocytopenia, hypersensitivity, crystalluria, and Rash as an adverse effect

A

TMP - SMX!!!

BACTRIM

31
Q

What are the 3 main drug interactions of TMP - SMX?

A
  1. Phenytoin (increase levels)
  2. Warfarin (increase INR - increase anticoagulant effect & cause bleeding)
  3. Methotrexate
    (decrease renal clearance)
32
Q

Because there is both single and double strength, how does dosing change for someone with renal dysfunction?

A

change to SINGLE dosing (DURHH)

33
Q

What is the mechanism of action of Chloramphenicol?

STATIC or CIDAL? (exception 3)

A
  1. Binds to 50s subunit of 70s ribosome
    - prevents peptide bond formation

(AT 30, CCEL at 50)

  1. STATIC except
    a) H. Influenza
    b) Strep pneumonia
    c) Neisseria meningiditis
34
Q

What is the MAIN mechanism of resistance of Chloramphenicol?

2 others?

A
  1. ACETYLTRANSFERASE inactivation
  2. Reduced permeability/uptake
  3. Ribosomal mutation
35
Q

Chloramphenicol can be administered how?

Is it lipid soluble or protein bound?

When does the dose need to be decreased?

A
  1. ORAL & IV
    (well absorbed by FI)
  2. LIPID SOLUBLE
    - not highly protein bound
  3. Decrease dose in LIVER FAILURE (not renal failure!!! this is one of the few)
36
Q

What drug needs dosage adjustment in LIVER FAILURE

A

Chloramphenicol

37
Q

What drug is:

  1. Unreliable agains STAPH AUREUS & not active against ENTEROCCI? (gram +)
  2. Not active against P. Aeriginosa
A

CHLORAMPHENICOL

38
Q

CHlormaphenicol is used primarily for what 4 atypical bacteria?

A
  1. Rickettsiae
  2. Spirochetes
  3. Chlamydia
  4. Mycoplasma

Rick Spun My Clam with Chloramphenicol

39
Q

What are the clinical uses for Chloramphenicol? (4)

A

None in U.S.

Third and Developing World

  1. Pneumonia
  2. Bacterial meningitis * (pretty good penetration into CSF)
  3. Typhoid fever
  4. Rocky mountain spotted fever (in developing world)
40
Q

What is the MAJOR adverse effect of Chloramphenicol?
(TEST TEST TEST)

What is the second hematology effect?

What are the other major AEs?

A
  1. GRAY BABY SYNDROME:
Abdominal distention
Vomiting
Flaccidity
Cyanosis
Circulatory collapse/Death

“chloramphenicol makes your baby grey”

  1. Aplastic Anemia
    - reversible BM suppression
3. Optic neuritis
Hypersensitivity reaction
Anaphylaxis
GI intolerance (vomiting, diarrhea)
Stomatitis
porphyria
41
Q

What is the function of Nitrofurantoin & Methenamine?

State which does the following:

  1. binds to ribosomal proteins & inhibits translation
    - inhibits bacterial respiration & pyruvate metabolism
  2. converted in acid pH to ammonia and FORMALDEHYDE
A
  1. UTI AGENTS

Nitrofurantoin:

  • binds to ribosomal proteins & inhibits translation
  • inhibits bacterial respiration & pyruvate metabolism
  1. Methenamine:
    - converted in acid pH to ammonia and FORMALDEHYDE

-Formaldehyde – non-specific denaturant of proteins and nucleic acids

42
Q

What is the mechanism of resistance of Nitrofurantoin?

Of Methenamine?

A
  1. E. coli – Chromosomal or plasmid-mediated production of nitrofurantoin reductase
  2. Alkaline urine –> no bacterial resistance to formaldehyde
43
Q

How are the Nitrofurantoin & Methanamine absorbed?

Which is enhanced by food?

Are they oral or iv drugs?

A
  1. Nitrofurantoin
    40-50% absorption following oral administration
    - Occurs in small intestine
    ***Enhanced with food!
  2. Methenamine
    Rapid absorption after oral administration
    May be partially degraded by gastric acid

BOTH ORAL!!! (TEST)

44
Q

The following describes which drugs:

  1. Rapid absorption following oral dose
    - Broad distribution in tissue
  2. Large urine concentrations
    Low/undetectable serum concentration
    Therapeutic concentrations not attained in prostate
A
  1. Methenamine

2. Nitrofurantoin

45
Q

How is Nitrofurantoin eliminated?

Methenamine?

A
  1. Eliminated in urine
    - also BILIARY
    = Nitrofurantoin
    (half life of 30 min)
  2. Methenamine: RENAL (longer half life)
46
Q

Which drug is used for the following:

  1. Large urine concentrations
    Low/undetectable serum concentration
    Therapeutic concentrations not attained in prostate

Do not use for:

  • Established infections (ACTIVE)
  • Prophylaxis against catheter-associated UTI
A

METHENAMINE

METHENAMINE = suppression or prophylaxis (NOT USED TO TREAT UTI DIRECLTY AS FIRST LINE OF CHOICE)

prophylaxis to prevent infection in patients ( not for ACTIVE infection)
suppresses growth that would develop into an infection

47
Q

Which drug is used for the following:

Acute, uncomplicated UTIs

Do not use for:

  1. Pyelonephritis
  2. Complicated UTI
A

NITROFURANTOIN

NITROFURANOTIN:
used for simple UTI (not pyelonephritis - infection of kidney)

48
Q

Which drug has the following spectrum of activity:

***E. coli (clue)
Citrobacter, sp.
Group B Streptococcus
Staphylococcus saprophyticus
Enterococcus (including some strains of VRE)
A

Nitrofurantoin

Not active against
Pseudomonas aeruginosa
Proteus
Providencia
Morganella
Serratia
Acinetobacter
49
Q

_____ has no ANTIMICROBIAL activity.

May not be effective against urease producing organisms (Example?)

A
  1. Methenamine

2. Proteus

50
Q

Which drug has the following adverse effects

  1. GI intolerance
  2. Rashes
  3. Acute pulmonary symptoms (REVERSIBLE)

HYPERSENSITIVITY PHENOMEN!!!!

A

Nitrofurantioin (UTI AGENT)

Weeks to months after drug exposure

Rapid onset of fever, cough, dyspnea, myalgia

Peripheral blood eosinophilia and lower lobe pulmonary infiltrates

51
Q

Which drug has the following adverse effect:

  1. Subacute and chronic pulmonary reaction!!!:

Gradual onset of progressive, non-productive cough and dyspnea

Interstitial infiltrate on CXR

Reversible but may lead to pulmonary fibrosis

May have + antinuclear antibodies

Bronchiolitis obliterans and organizing pneumonia reported

A

NITROFURANTOIN

52
Q

What drug causes HEMORRHAGIC CYSTITIS ? Why?

As well as:

GI (nausea, vomiting)
Rash
Pruritis
Bladder irritation

MEGALOBLASTIC ANEMIA

  • Eosoniphilia
  • Hemolytic anemia
  • Hepatitis
  • Peripheral sensory neuropathy
  • aplastic anemia
  • leukopenia
A

METHENAMINE

  • hemorrhagic cystitis due to higher doses which produce a lot of formaldehyde
53
Q

The following describes the dosing of which drug:

  1. Uncomplicated cystitis: 50-100 mg orally q6 hours for 7 days
    Prophylaxis: 50-100 mg by mouth daily
A
  1. Nitrofurantoin
54
Q

The following describes the dosing of which drug:

> 12 years old: 1g twice daily to 4 times daily max
6-12 y/o: 500mg to 1g twice daily
PROPHYLAXIS for UTI

A

Methanamine

PHARM/MHD EXAM - 3 (21 decks)

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