Nucleic Acid Synthesis Flashcards

1
Q

Nucleic Acid Synthesis Inhibitors drugs?

A
  1. Fluroquinolones
  2. Metronidazole
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2
Q

Nucleic Acid Synthesis Inhibitors drugs Function?

A

A nucleic acid inhibitor is a type of antibacterial that acts by inhibiting the production of nucleic acids.

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3
Q

Fluoroquinolones

  1. Adjunct admission and substantiation
  2. MOA
  3. MOA for bacteria
A
  1. Take on an empty stomach to increase absorption
  2. Inhibit topoisomerase 2 and topoiosmerase 4
  3. Bacteriosidal(kill bacteria)
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4
Q

Fluoroquinolones absorption impaired by?

A

-Divalent acids
-Shouldn’t be taken with divalent acids like milk, yogurt because that decreases absorption

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5
Q

What is another name for topoisomerase?

A

DNA gyrase

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6
Q

Fluoroquinolones and pH or urine?

A

Fluoroquinolones are acidic

Excessive alkalinity of urine must be avoided as this will increase excretion of drug

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7
Q

Fluoroquinolones suffix?

A

-“-floxacin”

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8
Q

Fluoroquinolones drugs?

A

COMGL–floxacin

Ciprofloxacin
Ofloxacin
Moxifloxacin
Gemifloxacin
Levofloxacin

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9
Q

Ciprofloxacin & Ofloxacin

  1. Gram
  2. CYP450
A
  1. Gram-negative aerobes only
  2. CYP450 Inhibitor
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10
Q

Ciprofloxacin & Ofloxacin

  1. Indications & Prophylaxis
  2. Non-indication
A
  1. Typhoid fever, cystitis, mycobacteria , lower resp tract infections and Nienongococcal prophylaxis
  2. Not for gonorrhea
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11
Q

Fluoroquinolones CYP450?

A

CYP450 Inhibtor

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12
Q

Fluoroquinolone CYP450 and different intensities?

A

Levofloxacin and Ciprofloxacin both inhibit CYP450 BUT Levofloxacin inhibit to a lesser extent

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13
Q

Moxifloxacin, Gemifloxacin and Levofloxacin

  1. Gram bacteria
  2. CYP450
  3. Indications + for TB
  4. Usuage for pseudomonas
  5. B-lactam allergy
A
  1. Gram-positive bacteria
  2. CYP450 Inhibitor
  3. M tuberulosis (Moxifloxacin, Levofloxacin), Lower resp tract, skin & urinary infections sinusitis cacute)
  4. Not for pseudomonas (moxifloxacin)
  5. Reserved for B-lactam allergy
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14
Q

Nalidixic acid and quinolones?

A

Nalidixic acid is used to form quinolones

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15
Q

Nalidixic acid and gram bacteria?

A

Gram -ve bacteria

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16
Q

Nalidixic acid indications?

A

-Acute and chronic lower urinary tract infections

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17
Q

Nalidixic acid mother substance?

A

Quinolone is the mother substance

18
Q

Nalidixic acid and quinolone resistance?

A

Can cause quinolone resistance if not used for a long time

19
Q

Nalidixic acid S/E?

A

-Neurotoxic
-Seizures
-Photosensitivity (main S/E)

20
Q

Nalidixic acid resistance(2) ?

A
  1. Change in permeability
    If bacteria can not enter
    bacteria then it can not be
    active
  2. One or more point mutations in quinolone binding region of target enzyme
21
Q

Fluoroquinolones resistant organisms?

A

SPS

-Staphylococci
-Psedomonas
-Serratia

22
Q

Fluoroquinolones S/E-7?

A

H2PQ SAT

-Seizures(Ciprofloxacin)
-QT-interval prolongation
-Hypoglycaemia/ Hyperglycaemia
-Arthropathy(damage to growing cartilage)
-Hallucinations(rare)
-Tendinitis(rare)
-Photosensitivity

23
Q

Fluoroquinolones DI-5?

A
  1. Probenecid-Increase in t1/2 Fluoroquinolones
  2. NSAIDS-Decrease Seizure threshold and increases likelihood of seizures
  3. Antacids/Minerals-decrease absorption of fluoroquinolones
  4. Drugs metabolized by CYP450:
    -Warfarin
    -Theophylline
  5. Oral hypoglycaemic age(Glibenclamide)
24
Q

Fluoroquinolones CI(6) ?

A
  1. G6PD deficiency (risk of haemolytic)
  2. Pregnancy/Lactation
  3. Babies/Children(<18yrs)
  4. Epilepsy & Porphyria-Nalidixic acid
  5. Hepatic/Renal failure
  6. Elderly patients

(2 & 3 effecct teh development of cartilage

25
Metronidazole 1. Incidence of resistance 2. Type of bacteria 3. Admission 4. CSF
1. Decreased incidence of resistance 2. Anaerobic bacteria 3. Orally, IV, rectal & topical 4. Metronidazole can enter the CSF
26
Metronidazole antiprotozoal action?
Trophozoites of: 1. Entamoeba histolytica 2. Trichomonas vaginalis
27
Helicobacteria treatment regime?
Helicobacter pylori (Peptic ulcers) -Metronidazole + Amoxicillini/Azythromycin + PPI (Lansoprazole) (For penicilli allergy)
28
Metronidazole uses?
GAPH 1. Helicobacter pylori (Peptic ulcers) -Metronidazole + Amoxicillini/Azythromycin + PPI (Lansoprazole) (For penicilli allergy) 2. Giardiasis-a diarrheal disease 3. Acute necrotising ulcerative gingivitis 4.Pseuedomembranous colitis
29
Metronidazole MOA?
Production of reactive intermediates Nitroradical anion (Bactericidal)
30
Metronidazole S/E?
1. Dry mouth 2. Metallic taste 3. CNS effects 4. Disulfiram-like effects
31
Metronidazole Disulfiram-like effects?
-Increased acetaldehyde levels -Inhibits alcohol metabolism All the above cause disulfiram side effects
32
Metronidazole DI-5?
1. Moderate CYP2C99 inhibitors-Warfarin 2. Alcohol, Lithium (Increased plasma levels) 3. Phenytoin 4.Cimetidine (CYP450 Inhibitor) 5. Phenobarbitone (CYP450 Inducer)
33
Metronidazole CI?
1. Alcohol-inhibits metabolism of alcohol therefore cannot be taken with alcohol (1st trimester of pregnancy & breastfeeding) 2. CNS Conditions
34
Nitrofurantoin I?
Treatment of uncomplicated lower. urinary tract infetions
35
Nitrofurantoin CI?
-Renal impairment -G6PD deficiency -Known hypersensitivity -Porphyria -Paediatrics infants >3 months -Pregnancy(neonatal haemolytic anaemia -Lactation
36
Nitrofurantoin DI-4?
-Neurotoxic agents: increased potential for neurotoxicity with concurrent use -Probenecid and sulfinpyrazone: Urinary excretion of nitrofurantoin reduced, efficacy reduced and risk of toxicity increased -Quinolone antibacterials:Antagonist in vitro antimicrobial action affected Magnesium trisilicate: Reduced absorption nitrofurantoin
37
Nitrofurantoin S/E?
GIT: Anorexia, nausea, vomiting Respiratory involvement: -Tachycardia CNS: Headache, dizziness
38
Mechanisms of inhibition of DNA synthesis-5?
1. Via the inhibition of nucleotide synthesis 2. By altering the base-pairing characteristics of the template 3. DNA or RNA polimerse inhibition 4. Topoismerase II(DNA gyrus) AND 4 inhibition
39
Ciprofloxacin absorption?
Absorbed rapidly( 7-80%)
40
Ciprofloxacin DI with Theophylline?
Ciprofloxacin inhibits the cytochrome P450 enzyme system Theophylline toxicity-asthma patient
41
Metronidazole mechanism of resistance -4?
1. Decreased uptake 2. Increased removal 3.Decreased activation in bacteria 4. Altered enzymes that convert active metronidazole