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Pharmacology > 25) Transcription Inhibitors > Flashcards

25) Transcription Inhibitors Flashcards

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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
Sulfadiazene pharmacokinetics
- Renally excreted
26
Sulfamethoxazole
- Bactrim = sulfamethoxazole and trimethoprim
27
Sulfamethoxazole CI/warnings
- Hypersensitivity to Sulfa; hyperkalemia; hypoglycemia; hyponatremia; thrombocytopenia
28
Sulfamethoxazole ADRs
- 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
29
Shared ADR between Bactrim (sulfamethoxazole and trimethoprim) and sulfadiazene
- Competes with bilirubin for binding to serum albumin causing Kernicterus in newborns
30
Sulfamethoxazole pharmacokinetics
- Hepatically metabolized | - Renally excreted
31
Bacteria cannot take up folic acid from environment but from a
- De Novo pathway involving PABA (Para-amino-benzoic acid)
32
RNA polymerase
- Enzyme that responsible for copying a DNA sequence into an RNA sequence during the process of transcription
33
Rifamycin derivatives
- Rifabutin | - Rifampin
34
Rifamycin derivatives MOA
- Inhibition of bacterial mRNA synthesis by inhibiting bacterial DNA-dependent RNA polymerase (RNAP)
35
Rifamycin derivatives are used for
- Tuberculosis | - Mycobacterial infection
36
Rifabutin CI/warnings
- Hematologic toxicity (leukopenia; thrombocytopenia; anemia) - Hypersensitivity - Superinfection - Uveitis
37
Rifabutin ADRs
- Skin rash - Discoloration of urine - Neutropenia - Leukopenia - NV - Flatulence - Abdominal pain - Thrombocytopenia
38
Rifabutin pharmacokinetics
- Substrate and inducer of CYP3A4 | - 85% protein binding
39
Rifampin CI/warning
- Coagulopathy; toxic epidermal necrolysis; flu-like symptoms; hepatotoxicity - Same as Rifabutin (ecvept for uveitis)
40
Rifampin ADRs
- 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
Rifampin pharmacokinetics
- Hepatic metabolism | - 80% protein binding
42
Rifampin is a substrate of
- 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
Rifampin is an inducer of
- BCRP/ABCG2 - CYP1A2 - CYP2B6 - CYP2C19 - CYP2C8 - CYP2C9 - CYP3A4, OATP1B1/1B3 (SLCO1B1/1B3) - P-glycoprotein/ABCB1 - UGT1A1
44
Rifampin is an inhibitor of
- OATP1B1/1B3 (SLCO1B1/1B3)
45
Anti-clostridium agent
- Fidaxomicin (FDX) | - Family of liplamyclins
46
Anti-clostridium agent (Fidaxomicin) MOA
- Bactericidal-type antibiotic | - Inhibits DNA dependent RNA polymerase sigma subunit
47
Anti-clostridium agent (Fidaxomicin) contraindications
- Hypersensitivity
48
Anti-clostridium agent (Fidaxomicin) caution if patient has
- Macrolide sensitivity
49
Anti-clostridium agent (Fidaxomicin) ADRs
- Nausea - GI hemorrhage - Anemia - Neutropenia
50
Anti-clostridium agent (Fidaxomicin) distribution
- Largely confined to the gastrointestinal tract
51
Anti-clostridium agent (Fidaxomicin) metabolism
- Intestinal hydrolysis | - Fecal excretion
52
Nitrofurans
- Nitrofurantoin
53
Nitrofurans (Nitrofurantoin) works by
- Damaging bacterial DNA since its reduced form is highly active
54
Nitrofurans (Nitrofurantoin) MOA
- 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
Nitrofurans (Nitrofurantoin) contraindications
- Anuria, oliguria, or significant impairment of renal function - Previous history of cholestatic jaundice or hepatic dysfunction
56
Nitrofurans (Nitrofurantoin) warnings
- Hepatic reactions (hepatitis; jaundice) - Optic neuritis - Peripheral neuropathy - Pulmonary toxicity - Superinfection - G6PD deficiency patients
57
Nitrofurans (Nitrofurantoin) side effects
- 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
Nitroimidazole (Metronidazole) MOA
- 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
Nitroimidazole (Metronidazole) US box warning
- Carcinogenic
60
Nitroimidazole (Metronidazole) CI/warning
- Hypersensitivity - Neurological disturbances (aseptic meningitis) - Superinfection
61
Nitroimidazole (Metronidazole) caution in patients with
- Blood dyscrasias - Cockayne syndrome (severe hepatotoxicity) - Hepatic impairment - Renal impairment - Seizure
62
Nitroimidazole (Metronidazole) side effects
- 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
Nitroimidazole (Metronidazole) pharmacokinetics
- Well distributed, crosses BBB - Hepatically metabolized - 20% protein binding - Renally excreted
64
Do NOT take Nitroimidazole (Metronidazole) with
- Alcohol abuse | - Can cause disulfiram-like reaction
65
Rifabutin and Rifampin antimycobacterial MOA
- Inhibits DNA-dependent RNA polymerase at the beta subunit | - Prevents chain initiation
66
Isoniazid antimycobacterial MOA
- Inhibits the synthesis of mycolic acids (an essential component of the bacterial cell wall)
67
Pyrazinamide antimycobacterial MOA
- Converted to pyrazinoic acid in susceptible strains of mycobacterium - Inhibit fatty acid synthetase enzyme that produces fatty acid precursors of mycolic acid
68
Ethambutol antimycobacterial MOA
- Inhibits arabinosyl transferase | - Results in impaired mycobacterial cell wall synthesis
69
Antimycobacterials
- Isoniazid (INH) - Pyrazinimide - Ethambutol
70
Isoniazide CI/warning
- US Box warning: hepatitis - Hypersensitivity - Peripheral neuropathies
71
Isoniazide ADRs
- 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
Isoniazide pharmacokinetics
- Hepatically metabolized | - Renally excreted
73
Pyrazinamide CI/warning
- Hypersensitivity - Hepatotoxicity - Caution in patient with alcoholism, diabetes, gout, porphyria, renal impairment
74
Pyrazinamide ADRs
- Malaise - Nausea, vomiting - Anorexia
75
Pyrazinamide pharmacokinetics
- Hepatically metabolized | - Widely distributed including CSF
76
Ethambutol CI/warning
- Hypersensitivity - Hepatic toxicity - Optic neuritis
77
Ethambutol ADRs
- Myocarditis; disorientation; skin rash; hyperuricemia; anorexia; NV; leukopenia; neutropenia; thrombocytopenia; hepatotoxicity; color blindness; visual disturbance; nephritis; pneumonitis
78
Ethambutol pharmacokinetics
- Hepatically metabolized | - Renally excreted
79
ALL three antimycobacterials are substrates AND inhibitors of
- CYP2E1
80
Pharmacogenomic
- NAT2 (N-acetyltransferase-2) | - Responsible for inactivation of INH by hepatic acetylation reaction
81
Slow acetylators (pharmacogenomic category)
- Higher plasma concentration - Longer half lives - Thus, more ADRs
82
Fast acetylators (pharmacogenomic category)
- Lower plasma concentration | - Sorter half lives with diminished responses to standard doses

Pharmacology (27 decks)

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