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Pharmacology > 25) Transcription Inhibitors > Flashcards

25) Transcription Inhibitors Flashcards

1
Q

Bacterial replication steps

A

1) Unwind DNA helix
2) Separate strands
3) Replication

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2
Q

Topoisomerases

A
  • Removes excess DNA supercoils

- Allows 3 steps to continue

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3
Q

Two types of topoisomerases in bacteria

A
  • Topoisomerase IV

- DNA gyrase

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4
Q

DNA gyrase

A
  • Involved primarily in supporting nascent chain elongation during replication of the chromosome
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5
Q

Topoisomerase IV

A
  • Separates the daughter chromosomes during the terminal stage of DNA replication
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6
Q

Fluoroquinolones

A
  • Ciprofloxacin
  • Levofloxacin
  • Mixofloxacin
  • Nalidixic acid
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7
Q

Fluoroquinolones MOA

A
  • Inhibit both enzymes
  • Topoisomerase IV in (G+)
  • DNA gyrase in (G-)
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8
Q

At high doses of fluoroquinolones

A
  • FQ are bactericidal because they break the double stranded DNA
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9
Q

Box warnings common to all fluoroquinolones

A
  • Irreversible tendinitis and tendon rupture, peripheral neuropathy, and CNS effects.
  • Exacerbation of myasthenia gravis
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10
Q

Contraindications common to all fluoroquinolones

A
  • Hypersensitivity
  • Altered cardia conduction (QT prolongation)
  • Aortic aneurysm
  • Hepatotoxicity
  • Phototoxicity
  • Superinfection with CDAD
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11
Q

Additional contraindications for ciprofloxacin

A
  • Crystalluria

- Hypo/hyperglycemia

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12
Q

Ciprofloxacin ADRs

A
  • Neuromuscular symptoms
  • Headache
  • Insomnia
  • Skin rash
  • Diarrhea
  • Vulvovaginal candidiasis
  • Increased LFTs
  • Asthma
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13
Q

Levofloxacin ADRs

A
  • Edema
  • Headache
  • Skin rash
  • NVD
  • Vaginitis
  • Candidiasis
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14
Q

Moxifloxacin ADRs

A
  • Headache
  • Hyperchloremia
  • Hypokalemia
  • NVD
  • Decreased RBC
  • Leukocytosis
  • Increase neutrophils
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15
Q

Ciprofloxacin pharmacokinetics

A
  • Substrate of OAT1/3
  • Inhibit CYP1A2
  • 20% protein binding
  • Renally excreted
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16
Q

Levofloxacin pharmacokinetics

A
  • Renally eliminated

- 30% protein binding

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17
Q

Moxifloxacin pharmacokinetics

A
  • 40% protein binding

- Hetpatically metabolized

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18
Q

All FQ forms complexes with

A
  • Divalent/trivalent cations

- Reduce drug bioavailability (space 3h before or after taking the FQ)

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19
Q

Sulfonamides: PABA analogue (names)

A
  • Sulfacetamide
  • Sulfadiazene
  • Sulfamethoxazole
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20
Q

Sulfacetamide CI/warning

A
  • Blood dyscrasias
  • Steven Johnson Syndrome (SJS= exfoliative rash with painful joints, anemia, nephritis)
  • Hepatic necrosis
  • Sulfonamide allergy
  • Superinfection
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21
Q

Sulfacetamide ADRs

A
  • Edema
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22
Q

Sulfacetamide pharmacokinetics

A
  • Ophthalmic route/topical
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23
Q

Sulfadiazene CI/warning

A
  • Blood dyscrasias
  • Steven Johnson Syndrome (SJS= exfoliative rash with painful joints, anemia, nephritis)
  • Hepatic necrosis
  • Sulfonamide allergy
  • Superinfection
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24
Q

Sulfadiazene ADRs

A
  • Myocarditis; headache; chills; hallucinations; urticaria; SJS; hypoglycemia; thyroid disorders; anorexia; diarrhea; agranulocytosis; aplastic anemia; hemolytic; thrombocytopenia; hepatitis; lupus erythematosus; tinnitus; periorbital edema; nephrolithiasis; competes with bilirubin for binding to serum albumin causing Kernicterus in newborns
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25
Q

Sulfadiazene pharmacokinetics

A
  • Renally excreted
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26
Q

Sulfamethoxazole

A
  • Bactrim = sulfamethoxazole and trimethoprim
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27
Q

Sulfamethoxazole CI/warnings

A
  • Hypersensitivity to Sulfa; hyperkalemia; hypoglycemia; hyponatremia; thrombocytopenia
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28
Q

Sulfamethoxazole ADRs

A
  • Myocarditis; headache; chills; hallucinations; urticaria; SJS; hypoglycemia; thyroid disorders; anorexia; diarrhea; agranulocytosis; aplastic anemia; hemolytic; thrombocytopenia; hepatitis; lupus erythematosus; tinnitus; periorbital edema; nephrolithiasis; competes with bilirubin for binding to serum albumin causing Kernicterus in newborns
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29
Q

Shared ADR between Bactrim (sulfamethoxazole and trimethoprim) and sulfadiazene

A
  • Competes with bilirubin for binding to serum albumin causing Kernicterus in newborns
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30
Q

Sulfamethoxazole pharmacokinetics

A
  • Hepatically metabolized

- Renally excreted

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31
Q

Bacteria cannot take up folic acid from environment but from a

A
  • De Novo pathway involving PABA (Para-amino-benzoic acid)
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32
Q

RNA polymerase

A
  • Enzyme that responsible for copying a DNA sequence into an RNA sequence during the process of transcription
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33
Q

Rifamycin derivatives

A
  • Rifabutin

- Rifampin

34
Q

Rifamycin derivatives MOA

A
  • Inhibition of bacterial mRNA synthesis by inhibiting bacterial DNA-dependent RNA polymerase (RNAP)
35
Q

Rifamycin derivatives are used for

A
  • Tuberculosis

- Mycobacterial infection

36
Q

Rifabutin CI/warnings

A
  • Hematologic toxicity (leukopenia; thrombocytopenia; anemia)
  • Hypersensitivity
  • Superinfection
  • Uveitis
37
Q

Rifabutin ADRs

A
  • Skin rash
  • Discoloration of urine
  • Neutropenia
  • Leukopenia
  • NV
  • Flatulence
  • Abdominal pain
  • Thrombocytopenia
38
Q

Rifabutin pharmacokinetics

A
  • Substrate and inducer of CYP3A4

- 85% protein binding

39
Q

Rifampin CI/warning

A
  • Coagulopathy; toxic epidermal necrolysis; flu-like symptoms; hepatotoxicity
  • Same as Rifabutin (ecvept for uveitis)
40
Q

Rifampin ADRs

A
  • Decreased blood pressure; flushing; behavioral changes; numbness; headaches; pruritis; urticaria; adrenocortical insufficiency; NVD; flatulence; hemoglobinuria; hematuria; visual disturbances; hemolytic anemia; leukopenia; thrombocytopenia; renal impairment
41
Q

Rifampin pharmacokinetics

A
  • Hepatic metabolism

- 80% protein binding

42
Q

Rifampin is a substrate of

A
  • OATP1B1/1B3 (SLCO1B1/1B3)
  • P-glycoprotein/ABCB1; Induces BCRP/ABCG2, CYP1A2, CYP2B6, CYP2C19, CYP2C8, CYP2C9, CYP3A4, OATP1B1/1B3 (SLCO1B1/1B3), P-glycoprotein/ABCB1, UGT1A1
43
Q

Rifampin is an inducer of

A
  • BCRP/ABCG2
  • CYP1A2
  • CYP2B6
  • CYP2C19
  • CYP2C8
  • CYP2C9
  • CYP3A4, OATP1B1/1B3 (SLCO1B1/1B3)
  • P-glycoprotein/ABCB1
  • UGT1A1
44
Q

Rifampin is an inhibitor of

A
  • OATP1B1/1B3 (SLCO1B1/1B3)
45
Q

Anti-clostridium agent

A
  • Fidaxomicin (FDX)

- Family of liplamyclins

46
Q

Anti-clostridium agent (Fidaxomicin) MOA

A
  • Bactericidal-type antibiotic

- Inhibits DNA dependent RNA polymerase sigma subunit

47
Q

Anti-clostridium agent (Fidaxomicin) contraindications

A
  • Hypersensitivity
48
Q

Anti-clostridium agent (Fidaxomicin) caution if patient has

A
  • Macrolide sensitivity
49
Q

Anti-clostridium agent (Fidaxomicin) ADRs

A
  • Nausea
  • GI hemorrhage
  • Anemia
  • Neutropenia
50
Q

Anti-clostridium agent (Fidaxomicin) distribution

A
  • Largely confined to the gastrointestinal tract
51
Q

Anti-clostridium agent (Fidaxomicin) metabolism

A
  • Intestinal hydrolysis

- Fecal excretion

52
Q

Nitrofurans

A
  • Nitrofurantoin
53
Q

Nitrofurans (Nitrofurantoin) works by

A
  • Damaging bacterial DNA since its reduced form is highly active
54
Q

Nitrofurans (Nitrofurantoin) MOA

A
  • Rapid reduction of nitrofurantoin inside the bacterial cell by flavoproteins (nitrofuran reductase) to multiple reactive intermediates
  • Those attack ribosomal proteins, DNA, respiration, pyruvate metabolism and other macromolecules within the cell
55
Q

Nitrofurans (Nitrofurantoin) contraindications

A
  • Anuria, oliguria, or significant impairment of renal function
  • Previous history of cholestatic jaundice or hepatic dysfunction
56
Q

Nitrofurans (Nitrofurantoin) warnings

A
  • Hepatic reactions (hepatitis; jaundice)
  • Optic neuritis
  • Peripheral neuropathy
  • Pulmonary toxicity
  • Superinfection
  • G6PD deficiency patients
57
Q

Nitrofurans (Nitrofurantoin) side effects

A
  • headache; increased serum phosphate; nausea; flatulence; increase LFTs; ECG changes; dermatitis; urine discoloration; aplastic anemia; hemolytic anemia; thrombocytopenia; jaundice; hepatitis; cough; cyanosis; superinfection; pulmonary fibrosis
58
Q

Nitroimidazole (Metronidazole) MOA

A
  • Inhibits nucleic acid synthesis by disrupting the DNA of microbial cells
  • Only occurs when metronidazole is partially reduced (usually happens only in anaerobic bacteria and protozoans…relatively little effect upon human cells or aerobic bacteria)
  • Leads to highly reactive nitro radical anion
59
Q

Nitroimidazole (Metronidazole) US box warning

A
  • Carcinogenic
60
Q

Nitroimidazole (Metronidazole) CI/warning

A
  • Hypersensitivity
  • Neurological disturbances (aseptic meningitis)
  • Superinfection
61
Q

Nitroimidazole (Metronidazole) caution in patients with

A
  • Blood dyscrasias
  • Cockayne syndrome (severe hepatotoxicity)
  • Hepatic impairment
  • Renal impairment
  • Seizure
62
Q

Nitroimidazole (Metronidazole) side effects

A
  • headache; vaginitis; nausea; metallic taste; pruritis; bacterial infection; flu-like symptoms; decrease libido; decreased appetite; anorexia; abdominal pain; DRESS symptoms (drug rash with eosinophilia and systemic: skin rash, fever, lymphadenopathy, and inflammation of the liver, lung, and heart); nasal congestion; polyuria; hepatotoxicity; agranulocytosis, eosinophilia, leukopenia, neutropenia (reversible), thrombocytopenia
63
Q

Nitroimidazole (Metronidazole) pharmacokinetics

A
  • Well distributed, crosses BBB
  • Hepatically metabolized
  • 20% protein binding
  • Renally excreted
64
Q

Do NOT take Nitroimidazole (Metronidazole) with

A
  • Alcohol abuse

- Can cause disulfiram-like reaction

65
Q

Rifabutin and Rifampin antimycobacterial MOA

A
  • Inhibits DNA-dependent RNA polymerase at the beta subunit

- Prevents chain initiation

66
Q

Isoniazid antimycobacterial MOA

A
  • Inhibits the synthesis of mycolic acids (an essential component of the bacterial cell wall)
67
Q

Pyrazinamide antimycobacterial MOA

A
  • Converted to pyrazinoic acid in susceptible strains of mycobacterium
  • Inhibit fatty acid synthetase enzyme that produces fatty acid precursors of mycolic acid
68
Q

Ethambutol antimycobacterial MOA

A
  • Inhibits arabinosyl transferase

- Results in impaired mycobacterial cell wall synthesis

69
Q

Antimycobacterials

A
  • Isoniazid (INH)
  • Pyrazinimide
  • Ethambutol
70
Q

Isoniazide CI/warning

A
  • US Box warning: hepatitis
  • Hypersensitivity
  • Peripheral neuropathies
71
Q

Isoniazide ADRs

A
  • Hepatic: increase LFTs
  • Vasculitis; brain disease; memory impairment; gynecomastia, hyperglycemia, metabolic acidosis, pellagra, pyridoxine deficiency; nausea, pancreatitis, vomiting; agranulocytosis; thrombocytopenia; DRESS syndrome; lupus like syndrome; optic atrophy
72
Q

Isoniazide pharmacokinetics

A
  • Hepatically metabolized

- Renally excreted

73
Q

Pyrazinamide CI/warning

A
  • Hypersensitivity
  • Hepatotoxicity
  • Caution in patient with alcoholism, diabetes, gout, porphyria, renal impairment
74
Q

Pyrazinamide ADRs

A
  • Malaise
  • Nausea, vomiting
  • Anorexia
75
Q

Pyrazinamide pharmacokinetics

A
  • Hepatically metabolized

- Widely distributed including CSF

76
Q

Ethambutol CI/warning

A
  • Hypersensitivity
  • Hepatic toxicity
  • Optic neuritis
77
Q

Ethambutol ADRs

A
  • Myocarditis; disorientation; skin rash; hyperuricemia; anorexia; NV; leukopenia; neutropenia; thrombocytopenia; hepatotoxicity; color blindness; visual disturbance; nephritis; pneumonitis
78
Q

Ethambutol pharmacokinetics

A
  • Hepatically metabolized

- Renally excreted

79
Q

ALL three antimycobacterials are substrates AND inhibitors of

A
  • CYP2E1
80
Q

Pharmacogenomic

A
  • NAT2 (N-acetyltransferase-2)

- Responsible for inactivation of INH by hepatic acetylation reaction

81
Q

Slow acetylators (pharmacogenomic category)

A
  • Higher plasma concentration
  • Longer half lives
  • Thus, more ADRs
82
Q

Fast acetylators (pharmacogenomic category)

A
  • Lower plasma concentration

- Sorter half lives with diminished responses to standard doses

Pharmacology (27 decks)

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