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PHARMACOLOGY (2nd year) > DR. MABANAG - AMINOGLYCOSIDES, SPECTINOMYCIN & TETRACYCLINE > Flashcards

DR. MABANAG - AMINOGLYCOSIDES, SPECTINOMYCIN & TETRACYCLINE Flashcards

1
Q

BACTERIA RIBOSOMES

A

70 S RIBOSOMES

SUBDIVIDED TO:
50 S
30 S

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2
Q

EUKARYOTES RIBOSOMES

A

80 S RIBOSOMES

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3
Q

How Ribosomes Work

A
  1. The tRNA loaded with particular amino acids enters the ribosome at the A site
  2. The tRNA’s anticodon has to match the codon (group of 3 nucleotides) on the mRNA
  3. In the P site of the ribosome, a peptide bond forms between the previous amino acid and the new amino acid formed
  4. The empty tRNA exits the E site
  5. This process repeats for the whole length of the
    mRNA and the polypeptide chain continues to grow
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4
Q

INHIBITORS OF 30S RIBOSOMAL SUBUNIT

A

A-S-T

○ Aminoglycosides
○ Spectinomycin
○ Tetracycline

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5
Q

INHIBITORS OF 50S RIBOSOMAL SUBUNIT

A

ML-CO

○ Macrolides
○ Lincosamides
○ Chloramphenicol
○ Oxazolidinones

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6
Q

Block the initiation of translation and causes the misreading of mRNA

A

AMINOGLYCOSIDES

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7
Q

Block the attachment of tRNA to the ribosome

A

TETRACYCLINES

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8
Q

Each interferes with a distinct step of protein synthesis

A

STREPTOGRAMINS

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9
Q

Prevent continuation of protein synthesis

A

MACROLIDES

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10
Q

Prevents peptide bonds from being formed

A

CHLORAMPHENICOL

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11
Q

Prevents continuation of protein synthesis

A

LINCOSAMIDES

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12
Q

Interfere with the initiation of protein synthesis

A

OXAZOLIDINONES

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13
Q

Used most widely in combination with other agents to treat drug-resistant organisms

A

AMINOGLYCOSIDES

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14
Q

are better given in combination for added spectrum of activity and synergism

A

AMINOGLYCOSIDES

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15
Q
  • Used in combination with other TB drugs for treatment of mycobacteria infections such as Tuberculosis
  • Outside of the urinary tract, aminoglycosides are not very effective, and it should be added with other drugs.

○ For urinary tract infections, monotherapy is enough

A

AMINOGLYCOSIDES

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16
Q

usually used for TB

A

STREPTOMYCIN (AMINOGLYCOSIDES)

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17
Q

EYE AND EAR INFECTIONS

A

NEOMYCIN (AMINOGLYCOSIDES)

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18
Q

Obsolete. Formerly used as 2nd line drug for TB

A

KANAMYCIN (AMINOGLYCOSIDES)

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19
Q

irreversible inhibitors of protein synthesis (30s and 50s subunit of ribosomes) though the precise mechanism of bacterial activity is still unclear

A

AMINOGLYCOSIDES

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20
Q

3 WAYS IN INHIBITING PROTEIN SYNTHESIS

A
  1. Interference with the initiation complex of
    peptide formation
  2. Misreading of mRNA
    ● Causes incorporation of incorrect amino acids into peptide and results in nonfunctional protein
  3. The breakup of polysomes into nonfunctional monosomes
    ● Occurs simultaneously, the overall effect is irreversible and leads to cell death
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21
Q

○ After IV administration, aminoglycoside concentration is highest in the ____ and in the _____

A

1.KIDNEYS
2. EARS

○ why the side effects are in the kidneys and inner ear
AMINOGLYCOSIDES ADVERSE EFFECTS
1.NEPHROTOXIC
2. OTOTOXIC

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22
Q

in INFECTIVE ENDOCARDITIS

A

Synergistic killing effect

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23
Q

○ Achieve bactericidal activity in the treatment of enterococcal endocarditis

A

Penicillin + aminoglycoside

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24
Q

○ Shorten therapy duration for Viridans streptococcal endocarditis
○ The duration for Viridans streptococcal endocarditis is 2 weeks but the usual duration is longer.

A

Penicillin + aminoglycoside

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25
Q

AMINOGLYCOSIDES ADVERSE EFFECTS

A

1.NEPHROTOXIC
2. OTOTOXIC
3. CURARE LIKE EFFECTS - HIGH DOSE (Reversible by Calcium gluconate or Neostigmine)
4. HYPERSENSITIVITY

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26
Q

Mainly used as a second-line agent for the treatment of tuberculosis

A

STREPTOMYCIN

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27
Q

ENTEROCOCCAL ENDOCARDITIS

2-week therapy: Viridans enterococcal endocarditis

A

Penicillin + Streptomycin:

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28
Q

for susceptible strains when aminoglycoside is selected as adjunct therapy

A

GENTAMICIN

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29
Q

Inhibits in vitro staphylococci and gram-negative bacteria including Enterobacteriaceae and Pseudomonas aeruginosa

A

GENTAMICIN

30
Q

High level Aminoglycoside Resistant Enterococci
(HLARE)

A

STREPTOMYCIN

31
Q

● In cases of drug-resistant meningitis or severe cases of beta-lactam allergy, aminoglycosides are still an alternative.

A

INTRATHECAL INJECTION OF GENTAMICIN SULFATE

32
Q

slightly more active vs Serratia marcescens

A

GENTAMICIN

33
Q

slightly more active vs Pseudomonas aeruginosa

A

TOBRAMYCIN

34
Q

Enterococcus faecalis SUSCEPTIBLE TO:

A
  1. GENTAMICIN
    2.TOBRAMYCIN
35
Q

Enterococcus faecum
SUSCEPTIBLE TO:
RESISTANT TO:

A

SUSCEPTIBLE TO: GENTAMICIN
RESISTANT TO: TOBRAMYCIN

36
Q

● Semi-synthetic derivative of Kanamycin- but less toxic
● Better resistance profile than Gentamicin and Tobramycin

37
Q

● Effective against:
○ Proteus spp
○ Pseudomonas
○ Enterobacter
○ Serratia
○ Mycobacterium tuberculosis
● Also a second line treatment for tuberculosis

38
Q

● Same characteristics with Gentamicin and Tobramycin
● May be active against some Gentamicin-resistant and Tobramycin-resistant bacteria

A

NETILMICIN

39
Q

● Active vs G(+) & G(-) bacteria and some mycobacteria
● P. aeruginosa and Streptococci - RESISTANT

A

Aminoglycosides:Neomycin, Kanamycin, Paromycin

40
Q

limited to topical and oral use due to
parenteral toxicity
○ Occurrence of higher resistance compared
to others

41
Q

treatment for MDR TB (obsolete
already) but alternate agents (Amikacin) may be
preferred

42
Q

more on for helminths
○ effective vs visceral leishmaniasis when given parenterally and intestinal Entamoeba histolytica infection

A

PAROMOMYCIN

43
Q

HIGHLY TOXIC
1. NEPHROTOXIC
2.OTOTOXIC

A

Neomycin, Kanamycin, and Paromomycin

44
Q

NEUROMUSCULAR BLOCKADE

A
  1. Inhibition of presynaptic ACh release
  2. ↓ motor end-plate sensitivity to ACh
  3. Interference with Ca+ action at neuroreceptors
45
Q

● 30S attaching antibiotic
● Active in vitro vs G(+) & G(-) bacteria
● Alternative tx for drug-resistant gonorrhea or
gonorrhea in penicillin-allergic patients in 1960s

A

SPECTINOMYCIN

46
Q

crystalline amphoteric substances of low solubility

A

TETRACYCLINE

47
Q

Tetracycline:Classification&Basic Structure

A

Short Acting
○ Tetracycline
○ Oxytetracycline
Intermediate Acting
○ Demeclocycline
○ Methacycline
Long Acting
○ Doxycycline
○Minocycline

48
Q

*Broad spectrum BACTERIOSTATIC antibiotic that inhibits protein synthesis
*Enters microorganism in part by passive diffusion and in part by energy dependent active transport

A

TETRACYCLINE MOA

49
Q

Once inside the cell, it binds irreversibly to 30s ribosomal subunit
○ Blocking the binding of aminoacyl-tRNA to the acceptor site on the mRNA-ribosome complex
○ Prevents addition of amino acids to growing peptide

A

TETRACYCLINE MOA

50
Q

should be taken
on empty stomach

A

Tetracycline & Demeclocycline

51
Q

absorption not
impaired by food

A

Doxycycline & Minocycline

52
Q

widely distributed across tissue and
bodily fluids except CSF

A

TETRACYCLINE

53
Q

Drug of choice for:
○ Rickettsiae
○ Borrelia spp. (Rocky Mountain Spotted
Fever)
○ Lyme disease
○ Anaplasma phagocytophilum
○ Ehrlichia spp.(can affect dogs and humans)

A

TETRACYCLINE

54
Q

Also an excellent drug for:
○ Mycoplasma pneumonia, Chlamydia,
and; Spirochetes
○ Helicobacter pylori
○ G(+) & G(-) bacterial infections
○ Vibrio infections

A

TETRACYCLINES

55
Q

alternative agent for primary and secondary syphilis in patients with penicillin allergy

A

DOXYCYCLINE

56
Q

rarely used antibacterial
○ Used off-label in the treatment of SIADH due of its inhibition of ADH in the renal tubule

A

DEMECLOCYCLINE

57
Q

● First glycylcycline to be used clinically
● Very broad spectrum - many tetracycline-resistant
strains are susceptible

A

TIGECYCLINE

58
Q

○ Methicillin-resistant Staphylococcus aureus (MRSA)
○ Vancomycin intermediate Staphylococcus aureus (VISA)
○ Vancomycin-resistant Staphylococcus aureus (VRSA)

A

TIGECYCLINE

59
Q

○ Streptococci: Penicillin-susceptible and resistant
○ Enterococci: Vancomycin-resistant strains,
○ Gram-positive rods
○ Enterobacteriaceae including Extended
spectrum beta-lactamase (ESBL)
○ Multidrug-resistant Acinetobacter baumanii

A

TIGECYCLINE

60
Q

ANAEROBES
● Rickettsia, Chlamydia, Legionella, and Rapidly growing mycobacteria
● Proteus, Providencia, P. aeruginosa - intrinsically resistant

A

TIGECYCLINE

61
Q

Tetracycline: Adverse Effects

A
  1. GI TRACT
  2. RENAL (FANCONI-LIKE SYNDROME, NEPHROGENIC DIABETES INSIPIDUS)
  3. BONY STRUCTURES AND TEETH
  4. HYPERSENSITIVITY
  5. FETALHEPATOTOXICITY
  6. DIZZINESS & NAUSEA
  7. DEC. PROTHROMBIN ACTIVITY
  8. PHOTOSENSITIVITY
  9. SUPERINFECTIONS
62
Q

○ ___________ precipitate infections such as:
- Overgrowth of Vaginal candida
- Resistant Intestinal Staphylococci
- Pseudomembranous colitis
secondary to Clostridium difficile (treated by Metronidazole and oral Vancomycin)
- Demeclocycline

A

TETRACYCLINE

63
Q
  1. Which of the following is not an adverse effect of Aminoglycosides?
    a. Ototoxicity
    b. Nephrotoxicity
    c. Neuromuscular blockade
    d. AOTA
    e. NOTA
A

E. NOTA
ALLARE ADVERSE EFFECTS OF AMINOGLYCOSIDES

64
Q
  1. Which of thefollowing is the first glycycycline used clinically?
    a. Minocycline
    b. Tetracycline
    c. Gentamicin
    d. Tigecycline
A

d.tigecycline

65
Q
  1. Which of the following does not act on 30s subunit of ribosome
    a. Aminoglycoside
    b. Tetracycline
    c. Spectinomycin
    d. Linezolid
A

D. LINEZOLID

66
Q
  1. Aminoglycosides’ mechanism of action involves:
    a. Inhibition of DNA synthesis
    b. Inhibition of protein synthesis
    c. Inhibition of carbohydrate synthesis
    d. NOTA
A

b. Inhibition of protein synthesis

67
Q
  1. Which ofthefollowing is not true?
    a. Gentamicin is slightly more active vs
    Serratia marcescens
    b. Tobramycin is slightly more active vs
    Pseudomonas aeruginosa
    c. Enterococcus faecalis - susceptible to
    Tobramycin only
    d. Enterococcus faecum - resistant to
    Tobramycin
A

c. Enterococcus faecalis - susceptible to
Tobramycin only

***SUSCEPTIBLE TO BOTH

68
Q
  1. Antibacterial activity persists beyond the time during which measurable drug is present or serum concentration is below MIC is called:
    a. Post-antibiotic effect
    b. Post-aminoglycoside effect
    c. Post-streptomycin effect
    d. Post-antifungal effect
A

a. Post-antibiotic effect

69
Q
  1. This drug is used off-label in the treatment of SIADH due of its inhibition of ADH in the renal tubule
    a. Streptomycin
    b. Amikacin
    c. Gentamicin
    d. Domocycline
A

d. Domocycline

70
Q
  1. This drug is obsolete. It is formerly used as 2nd line drug for TB
    a. Kanamicin
    b. Streptomycin
    c. Amikacin
    d. Erythromycin
A

a. Kanamicin

71
Q
  1. The absorption of this/these drugs are impaired by food ingestion?
    a. Doxycycline
    b. Minocycline
    c. Tetracycline
    d. Demeclocycline
    e. AANDB
    f. CandD
A

f. CandD
IMPAIRED BY FOOD INGESTION
TETRACYCLINEAND DEMECLOCYCLINE

72
Q
  1. The absorption of this/these drugs are not impaired by food ingestion?
    a. Doxycycline
    b. Minocycline
    c. Tetracycline
    d. Demeclocycline
    e. AandB
    f. CandD
A

e. AandB
NOT INPAIRED BY FOOD INGESTION
DOXYCYCLINE & MINOCYCLINE

PHARMACOLOGY (2nd year) (16 decks)

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