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Pharmacology > 26) Protein Synthesis Inhibitors > Flashcards

26) Protein Synthesis Inhibitors Flashcards

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1
Q

Bacterial protein synthesis inhibitors (30s)

A
  • Aminoglycosides
  • Glycylcycline (Tigecyclin)
  • Tetracycline (t-RNA binding)
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2
Q

Bacterial protein synthesis inhibitors (50s)

A
  • Oxazolines (initiation inhibitors)
  • Peptidyl transferase (Chloramphenicol)
  • Transcription/translocation inhibitors
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3
Q

50s transcription/translocation inhibitors classificaitons

A
  • Macrolides
  • Ketolides
  • Lincosamides
  • Streptogramins
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4
Q

Initiation

A
  • mRNA joins with 30S and with t-fMet-tRNA (t-RNA linked to formylated methionine)
  • 50S joins the 30S/ t-fMet-tRNA to form the 70S complex
  • t-fMet-tRNA occupies the P-site
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5
Q

Elongation

A
  • 30S decodes the codon

- 50S catalyzed the formation of the peptide bond (bond between amino acids)

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6
Q

Termination

A
  • It releases factors that recognize the terminal codon
  • Discharge the newly synthesized protein
  • Dissociates the ribosome-mRNA complex
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7
Q

Aminoglycosides MOA

A
  • Binds to the cytosolic membrane-associated bacterial ribosome
  • Disturbs peptide elongation by changing the shape of 30S ribosomal subunit –> inaccurate mRNA translation
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8
Q

Tetracycline/Glycylcycline MOA

A
  • Binds to the 30S ribosomal subunit
  • Inhibits the binding of aminoacyl-tRNA to the mRNA (A-site= acceptor) translation complex
  • Inhibits initiation of translation
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9
Q

Oxazolidinones MOA

A
  • Binds to ribosomal subunit 50S

- Inhibits the initiation process in protein synthesis by preventing the formation of 50/30S complex

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10
Q

Chloramphenicol MOA

A
  • Prevents protein chain elongation by inhibiting the peptidyl transferase activity of the bacterial ribosome of 50S
  • Leads to the inhibition of peptide bond formation
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11
Q

Macrolides, ketolides, Streptogramins and lincosamide MOA

A
  • Binds to the P binding site of the 50S ribosomal subunit
  • Prevents peptidyl transferase
  • Inhibits translocation step (where the polypeptide is transferred from P to E site) and affects elongation
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12
Q

Aminoglycosides coverage/administration

A
  • Gram-negative

- Not orally bioavailable, given intravenously (IV)

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13
Q

Aminoglycosides and beta-lactam combination

A
  • Beta-lactam increase cell wall permeability and facilitate the uptake of aminoglycosides
  • Boosts its effect
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14
Q

Aminoglycosides side effects

A
  • Ototoxicity (they accumulate in inner ear)
  • Nephrotoxicity (they accumulate in proximal tubule)
  • Neuromuscular blockade (respiratory paralysis)
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15
Q

Aminoglycosides (names)

A
  • Gentamycin
  • Tobramycin
  • Amikacin
  • Streptomycin
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16
Q

Gentamycin warning

A
  • Cross-sensitivity to other aminoglycosides

- Superinfection with CDAD (C. difficile associated diarrhea)

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17
Q

Tobramycin box warning

A
  • Not used during pregnancy (fatal)
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18
Q

ALL aminoglycosides US box warning

A
  • Neurotoxicity (as ototoxicity) and nephrotoxicity; use of potent diuretics
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19
Q

ALL aminoglycosides ADRs

A
  • Electrolyte alteration
  • Hearing impairment
  • Neuromuscular disorder
  • Renal problem
  • Visual disorder
  • Respiratory depression
  • Fever
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20
Q

ALL aminoglycosides cardio ADRs

A
  • Edema
  • Hypo/hypertension
  • Phlebitis
  • Brain disease, confusion, seizure;
  • Alopecia
  • Urticaria;
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21
Q

ALL aminoglycosides endocrine ADRs

A
  • Hypocalcemia
  • Hypokalemia
  • Hypomagnesemia
  • Hyponatremia
  • Weight loss
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22
Q

ALL aminoglycosides hematologic ADRs

A
  • Agranulocytosis
  • Anemia
  • Eosinophilia
  • Granulocytopenia
  • Leukopenia
  • Purpura
  • Thrombocytopenia
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23
Q

Additional ADR for Tobramycin

A
  • Increase LFTs
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24
Q

ALL aminoglycosides metabolism

A
  • Not known
  • Renally eliminated
  • Poor distribution in CSF and ocular because it is hydrophilic
  • Less than 20% protein binding
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25
Tetracyclines ADRs
- Kidney toxicity and GI distress (contraindicated in renal impairment) - GI distress (esophageal ulceration especially doxycycline) - Cutaneous photosensitivity (especially tetracycline) - Bone development abnormalities in pediatrics (teeth becoming discolored because of UV-absorbed properties of tetracyclines; NOT GIVEN IN CHILDREN)
26
Oral co-administration of tetracyclines with di/tri-valent cations (like calcium, magnesium, aluminum; antacids…) can lead to
- Chelation of tetracycline | - Thus, it decreases absorption
27
Tetracyclines (names)
- Tetracycline - Doxycycline - Minocycline
28
Tetracycline CI/warnings
- Increase BUN - Intracranial hypertension - Photosensitivity - Superinfection and CDAD
29
Tetracycline ADRs
- Thrombophlebitis - Skin photosensitivity - Dental discoloration - Esophagitis - Azotemia - Hepatotoxicity - Renal failure - Tissue hyperpigmentation
30
Tetracycline metabolism
- Major substrate of CYP3A4 - Renal and fecal excretion - Wide distribution but poor to CSF - 60% protein binding - Half life: 6-8 hours
31
Doxycycline ADRs
- Hypertension - Increased lactate dehydrogenase - Increased serum glucose - Diarrhea - Increased serum aspartate aminotransferase - Nasopharyngitis
32
Doxycycline metabolism
- Not known - 90% protein binding - Renal and fecal excretion - Half life: 16 hours
33
Minocycline CI/warnings
- Autoimmune syndrome (lupus-like) - Dizziness, mental alertness - Hepatotoxicity
34
Minocyclin ADRs
- Ddizziness - Urticaria - Tinnitus
35
Minocycline metabolism
- Renal and fecal excretion - 60% protein binding - Half life: 16 hours
36
ALL tetracyclines CI/warning
- Hypersensitivity - Use in infants and children <8 years old or during 2nd/3rd trimester of pregnancy - Breast feeding
37
Macrolides (names)
- Azithromycin - Clarithromycin - Erythromycin - Telithromycin
38
ALL macrolides CI/warning
- Hypersensitivity - QT prolongation - Superinfection and CDAD - Cardiac risk - Exacerbates myasthenia gravis
39
Myesthinea Gravis
- Neuromuscular disorder that causes weakness in the skeletal muscles - Facial paralysis - Difficulty breathing, swallowing and talking - Drooping eyelids - Double vision
40
ALL macrolides ADRs
- Nausea, vomiting, diarrhea - Photosensitivity - Candidiasis
41
Azithromycin ADRs
- Palpitations - Vaginitis - Decreased neutrophils - Increased LFTs - Increases BUN, serum creatinine
42
Azithromycin metabolism
- Extensive distribution (not in CSF) - 50% protein binding - Hepatically metabolized - Renal and biliary excretion
43
Clarithromycin CI/warning
- Hepatic effects
44
Clarithromycin ADRs
- Insomnia - Skin rash - Increased BUN
45
Clarithromycin metabolism
- 50% protein binding - Hepatically metabolized - Renally and excreted in the feces
46
Erythromycin ADRs
- Hearing loss - Hepatitis - Interstitial nephritis
47
Erythromycin metabolism
- 80% protein binding - Hepatically metabolized - Renally excreted and in the feces
48
Telithromycin CI/warning
- US box warning: Contraindicated in myasthenia gravis - Hepatic effects - Syncope - Visual disturbances
49
Telithromycin ADRs
- Headache - Dizziness - Blurred vision - Thrombocytopenia
50
Telithromycin metabolism
- 60% protein binding - Hepatically metabolized - Renally excreted and in the feces
51
Macrolides that are both substrates AND inhibitors of CYP3A4
- Clarithromycin - Erythromycin - Telithromycin
52
Tigecycline (glycylcycline family) CI/warning
- US Box warning of increased mortality - Hypersensitivity - Cross reactivity with tetracyclines - Anti-anabolic effect with tetracycline (increased BUN, azotemia, acidosis, and hyperphosphatemia) - Hepatotoxicity - Photosensitivity - Pancreatitis - Pseudotumor cerebri - Superinfection
53
Tigecycline (glycylcycline family) ADRs
- NVD, headaches - Phlebitis, skin rash - Hyponatremia, hypocalcemia, hypoglycemia - Anorexia, hypoprotenemia - Vaginitis - Candidiasis - Increased INR, LFT, BUN - Eosinophilia - Hyperbilirubinemia
54
Tigecycline (glycylcycline family) metabolism
- Not known - 70% protein binding - Hepatically metabolized and renal/fecal excretion
55
Chloramphenicol CI/warning
- US Box warning: blood dyscrasias (aplastic anemia, hypoplastic anemia, thrombocytopenia, and granulocytopenia) - Hypersensitivity - Gray syndrome (cyanosis) associated with serum levels more than 50mcg/ml - Superinfection with CDAD
56
Chloramphenicol ADRs
- Confusion, delirium - Urticaria, aplastic anemia - Diarrhea - Bone marrow depression - Optic neuritis
57
Chloramphenicol metabolism
- Hepatically metabolized - 40% protein binding - Good distribution including CSF - Renally excreted
58
Clindamycin (lincosamide family) CI/warning
- US Box warning for fatal colitis with CDAD - Hypersensitivity (anaphylactic shock) - Superinfection
59
Clindamycin (lincosamide family) ADRs
- Hypotension, thrombophlebitis - Metallic taste - Rash azotemia - Proteinuria, agranulocytosis - Neutropenia, thrombocytopenia - DRESS syndrome
60
Clindamycin (lincosamide family) metabolsim
- Metabolized by CYP3A4 | - 90% protein binding
61
Linezolid (Oxazolidinone family) CI/warning
- Hypersensitivity - Lactic acidosis - Myelosuppression - Optic neuropathy - Serotonin syndrome (serotonin degradation is MAO mediated; hyperthermia; muscle rigidity; rapid fluctuation in mental signs) - Superinfection
62
Linezolid (Oxazolidinone family) ADRs
- NVD - Decreased WBC and platelets - Skin rash - Increased amylase - Vulvovaginal candidiasis - Increased LFTs, BUN, and creatinine
63
Linezolid (Oxazolidinone family) metabolism
- Inhibits monoamine oxidase - 30% protein binding - Hepatically metabolized
64
Tedizolid (Oxazolidinone family) CI/warning
- Superinfection | - Neutropenia
65
Tedizolid (Oxazolidinone family) ADRs
- Flushing, urticaria - Hypertension, tachycardia - NVD - Oral candidiasis - Visual impairment - Increase LFT - Decrease WBC, platelets, hemoglobin
66
Tedizolid (Oxazolidinone family) metabolism
- Inhibit BCRP/ABCG2 - 80% protein binding - Fecal excretion
67
Quinupristin/dalfopristin | (Streptogramin family) CI/warning
- Hypersensitivity - Arthralgias - Hyperbilirubinemia - Phlebitis - Superinfection
68
Quinupristin/dalfopristin | (Streptogramin family) ADRs
- Thrombophlebitis - Headache - Skin rash - Increased lactate dehydrogenase - NVD - Anemia
69
Quinupristin/dalfopristin | (Streptogramin family) metabolsim
- Inhibit CYP3A4 - Metabolism: conjugated with glutathione - Fecal excretion

Pharmacology (27 decks)

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