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MHD/PHARM Exam 3 > Tetracyclines + Other Cyclins > Flashcards

Tetracyclines + Other Cyclins Flashcards

1
Q

Tetracycline + Glycylclines: MOA

A

REVERSIBLY Inhibits protein synthesis at 30 S ribosome by preventing the binding of tRNA to A site –> no elongation

bacterioSTATIC

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2
Q

Tetracyclines + glyclyclines: MOR

A

Three MOR:

  1. Efflux protein channels
  2. Ribosomal proteins that protect the ribosome
  3. Enzymatic inactivation of drugs

*MOR is acquired via mobile genetic elements

Tigecycline is RESISTANT to all forms of MOR

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3
Q

Tetracyclines + glyclyclines: Spectrum of Activity

4 catergories

A

Gram + Aerobes
MSSA

Gram - Aerobes
Burkholderia Pseudomallei

Anaerobes

Others-
brucella, legionella, coxiella, Borrelia, chlamydias, mycoplasm, ureaplasma, Rickettsia

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4
Q

Tigecycline: Spectrum of Activity

A

Gram +, Gram -, anaerobes

bacteriodes group

NO: proteus, no pseudomonas

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5
Q

Tetracyclines + glyclyclines, tigecycline: Clinical uses

A

Reserved for treatment of infections due to unusual organisms

Respiratory infections - pertussis
STDS
Prophylaxis for malaria
Rocky MTN spotted fever, Q fever, lyme disease (Borrelia)

Polymicrobial infections

Acne, SSTI, intra-abdominal infections, SIDAH

Tigecycline is NOT used for UTIs or bacteremias

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6
Q

Tetracyclines + glyclyclines, tigecycline: AEs (6)

A

GI - N/V in 30% of the people, increased in Tigecycline

Hypersensitivity

Photosensitivity

Renal - fanconi-like syndrome, renal failure in outdates tetracyclines

Hepatic - increased liver enzymes

*Pregnancy NO NO - category D
Discoloration of permanent teeth, decrease bone growth in kids

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7
Q

Tetracyclines + glyclyclines, tigecycline: Pharmocology

A

Absorption:

Distribution: widely distrubuted, good penetration in synovial fluid, seminal fluid, PROSTATE
NO CSF

Elimination:
Tetra - renal, unchanged
Doxy and minocycline - metabolically eliminated, no RI adj
Tigecycline - biliary adjust for liver disease
Minimally removed via HD

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8
Q

TMP- SMX Bactrim: MOA

A

Synergistically bacterioCIDAL

Inhibition of PURINE synthesis via blocking two different enzymes in the pathway:

PABA (1)—>Dihydrofolic Acid (2) –>tetrahydrofolic acid –> purines

“Sulfas”
SMX inhibits enz 1 : dihydropteroate synthetase

TMP inhibits enz 2: dihydrofolate reductase

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9
Q

TMP- SMX Bactrim: MOR

A

decrease emergence of resistance

Sulfa resistance is widespread

  • PABA overproduction
  • structural change to enz 1 dihydropteroate synthetase
  • PLASMID mediated prod of drug resistance, or decrease permeability

Trimethoprim:

  • chromosomal or plasmid mediated
  • plasmid mediated resistance to the drug
  • changes in cell permeability
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10
Q

TMP- SMX Bactrim: Spectrum of Activity

A

Gram negative aerobes:
Stenotropomas Maltophilia

Gram + aerobes:
* S. Aureus, CA-MRSA*
S. pyogenes
Nocardia
Listeria

others:
*pneumocystis carinni

NO anaerobe activity

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11
Q

TMP- SMX Bactrim: Clinical Use

A

UTIs
Prostatis
Skin infections due to CA-MRSA

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12
Q

TMP- SMX Bactrim: Adverse Effects

A

GI - NVD, glossitis, jaundice, hepatic necrosis
Hypersensitivity - RASH

Hematology: leukopenia, thrombocytopenia

Renal

CNS - H/A, aseptic meningitis, seizures

Others- drug induces lupus, serum sickness like syndrome, crystaluria

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13
Q

TMP- SMX Bactrim: Pharmocology

A

Absorption:
IV and oral, good bioavailability

Distribution:
70% protein bound
Wide, good penetration
lungs, urine, PROSTATE, CSF

Elimination: Renal and hepatic
**RI adjustment with CrCl

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14
Q

TMP- SMX Bactrim: Drug interactions (3)

A

Drug Interactions
[PHENYTOIN] INCREASES
[WARFARIN] INCREASES = increase anticoag effect
[METHOTREXATE] INCREASES, decreases renal clearance

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15
Q

Chlorampheniocol: MOA

A

Inhibits the 50S subunit, blocking peptide synthesis

bacterioSTATIC

exception bacteriocidial w:
H. influenzae
S. pneumo
N. meningitis

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16
Q

Chlorampheniocol: Mechanism of resistance (3)

A

Ribosomal mutations
decrease cellular permeability / uptake
direct inactivation of drug by ACETYLTRANSFERASE

can lead to massive outbreaks of typhoid fever and shigella
(central and south america, vietnam, india; not used in US)

17
Q

Chlorampheniocol: Spectrum of Activity

A

Gram positive:
NO- S. Aureus, or enterococci

Gram negatives:
NO - Pseudomonas aeruginosa

Anaerobes - both gram - and +

Ricekettsiae
Spirochetes
Chlamydia
Mycoplasm

18
Q

Chlorampheniocol: Clinical Uses

A

None in the US

Rocky MTN spotted fever
penumo, meningitis, typhoid

19
Q

Chlorampheniocol: AEs

A

Gray Baby Syndrome in neonates
(abdominal distension, vomiting, flaccidity, cyanosis, circulatory colapse/death)

Hematologic:
REV. bone marrow suppression
aplastic anemia

Others: 
Optic neuritis
hypersen rxn
anaphylaxis
GI
stomatitis
porphyria
20
Q

Chlorampheniocol: pharmocology

A

Absorption - well absorped via GI tract

Distribution: lipid soluble
not highly protein bound
CSF levesl about 30-50%

Elimination:
metabolized by the liver
enterhepatic ciruculation
excreted y the kidneys

  • DECREASE dose in liver failure
  • not required for RI
21
Q

Nitrofuranton: MOA

A

poorly understood

binds ribosomal proteins, inhibits translation, inhibits bacterial respiration and pyruvate metabolism

22
Q

Nitrofuranton: Mxn of Resistance

A

RARE

Ecoli does make nitrofuranton reductase

23
Q

Nitrofuranton: Spectrum of Activity

A 
E. coli
citrobacter spp
Group B strep
Staph saprophyticus
Enterococcus (including some strains of VRE)

NO: pseudomonas, proteus, providencia, morganella, serratia, acinetobacter

24
Q

Nitrofuranton: Clinical Uses

A

Acute, UNCOMPLICATED UTIs

NOT for:
pyelonephritis
complicated UTIS

25
Q

Nitrofuranton: AEs

A

GI intolerance
Rashes
Acute pulm symptoms, REV hypersensitivity phenomeon
Subacute and chronic pul rxn

26
Q

Nitrofuranton: Pharmocology

A

Absorption: ENHANCED with food; about 50% following oral administration

Distribution: Urine, undetectable serum
NO prostate

Elimination:
Urine/kidney
minor biliary excretion
half life about 30 mins

27
Q

Methenamine: MOA

A

converted in acid pH to ammonia and FORMALDEHYDE

Formaldehyde, nonspecific denaturant of proteins and nucleic acids

28
Q

Methenamine: Mxn of Resistance

A

Alkaline urine, won’t be able to transform the Methenamine to Formaldehyde - no activity

no bacterial resistance to formaledhyde has been described

29
Q

Methenamine: Spectrum of Activity

A

Itself has no antimicrobial activity

Formaldehyde resistance not describe and has BROAD antimicrobial activity

NO: urease producing organisms (proteus)

30
Q

Methenamine: Clinical Uses

A

Suppression or prophylaxis against recurrent UTIs

NO:
established infections
prophylaxis against catheter-associated UTIs

31
Q

Methenamine: AEs

A 
Generally well tolerated
GI intolerance (N/V)
Rashes
Pruritis
bladder irritation
hemorrhagic cystitis at higher doses
32
Q

Methenamine: Pharmocology

A

Absorption: rapid after oral admin

Distribution: broad in tissues

Elimination: renal
half life: 3-4 hours with normal renal function

MHD/PHARM Exam 3 (7 decks)

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