Pharmacology: Antibiotics/virals for LRTI Flashcards

(47 cards)

1
Q

Amoxicillin & Cefotaxime MOA?

A

Inhibits cell wall synthesis by preferentially binding to specific penicillin-binding-proteins (PBPs) located inside the bacterial cell wall (transpeptidases) → Inhibits peptidoglycan cross-linking in bacterial cell wall → Cell lysis (Bactericidal)

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2
Q

Adverse effects of Amoxicillin & Cefotaxime?

A
  • Nausea/vomiting, diarrhea
  • Mainly hypersensitivity reaction
  • Exhibit cross-sensitivity or cross-allergenicity
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3
Q

Resistance to Amoxicillin & Cefotaxime?

A

Resistance:
- Inactivation of the drug by β-lactamases
- structural differences in PBPs
- presence of permeability barrier (mainly gram -)

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4
Q

How can we avoid inactivation of Amoxicillin by β-lactamase?

A

We give it alongside clavulinic acid (a β-lactamase inhibitor)

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5
Q

What is Clavulinic acid?

A

A β-lactamase inhibitor

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6
Q

Which class of drug does erythromycin belong to?

A

Macrolides

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7
Q

Erythromycin MOA?

A

Inhibits protein synthesis by binding to the 50s subunit of bacterial ribosomes

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8
Q

Which enzyme does erythromycin inhibit? The consequences of that?

A

Cytochrome-P450 (this affects the metabolism of other drugs and destroys gut flora)

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9
Q

Adverse effects of Erythromycin?

A

Adverse effects:
- Hypersensitivity reactions
- GI disturbances, cholestatic jaundice,
- Reversible ototoxicity

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10
Q

Which class of drug is Ciprofloxacin?

A

Fluoroquinolone

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11
Q

MOA of Ciprofloxacin?

A

Inhibits DNA gyrase (topoisomerase II) topoisomerase IV → Inhibits replication of DNA → Cell death (Bactericidal)

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12
Q

Which class of drug is Co-trimoxazole (Sulfamethoxazole & Trimethoprim)?

A

Sulfanomides

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13
Q

MOA of Co-trimoxazole (Sulfamethoxazole & Trimethoprim)?

A

inhibit folate synthesis

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14
Q

Which antibiotic is used to treat Pneumocystis corinii infection in patients with AIDS ?

A

Sulfanomides:
Co-trimoxazole (Sulfamethoxazole & Trimethoprim)

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15
Q

Adverse effects of Co-trimoxazole (Sulfamethoxazole & Trimethoprim)?

A

Adverse effects:
- Nausea/vomiting, headache, mental depression
- Serious effects of sulfonamides are hepatitis, hypersensitivity reactions, bone marrow depression & crystalurea

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16
Q

MOA of Tetracycline?

A

Binds to 30S ribosomal subunit inhibiting protein synthesis

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17
Q

Is Tetracycline bacteriostatic or bactericidal?

A

Bacteriostatic but bactericidal at high concentrations

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18
Q

Tetracycline adverse effects?

A

Adverse effects:
- Diarrhea, vomiting, abdominal pain, anorexia, hepatotoxicity
- Serious effect on developing teeth (permanent yellow/brown)

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19
Q

Which class of drugs does Linezolid belong to?

A

Oxazolidinones

20
Q

Linezolid MOA?

A

Inhibits protein synthesis

21
Q

Linezolid is used to treat ______? And is quite effective in which infections?

A

used to treat MRSA, and quite effective in vancomycin-resistant gram (+) infections

22
Q

Adverse effect of Linezolid? (1)

A

Bone marrow toxicity

23
Q

What type of drug is Vancomycin?

24
Q

MOA of Vancomycin?

A

Acts on cell wall synthesis

  • binds to precursors of cell wall synthesis and inhibits peptidoglycan elongation
  • binding occurs at (D-Ala-D-Ala residue)
25
MOA of Vancomycin?
**Acts on cell wall synthesis** - binds to precursors of cell wall synthesis and **inhibits peptidoglycan elongation** - binding occurs at **(D-Ala-D-Ala residue)**
26
Vancomycin is active against? (3)
1. MRSA 2. S.epidermidis 3. G+ bacteria in p/x allergic to penicillin
27
Adverse effects of Vancomycin? (2)
1. Ototoxicity 2. Nephrotoxicity
28
What type of drug is Chloramphenicol?
Amphenicol
29
Chloramphenicol MOA?
M.O.A: Binds to 50S & inhibits mitochondrial protein synthesis
30
Chloramphenicol adverse effects?
Hematological effects & **Gray baby syndrome**
31
What is Ganciclovir?
An analogue of Acyclovir
32
What is Ganciclovir?
An analogue of Acyclovir
33
Ganciclovir MOA?
M.O.A: Phosphorylated by CMV kinases → forms triphosphate → inhibits CMV DNA polymerase → which **Inhibits viral nucleic acid synthesis**
34
Ganciclovir is active against which viruses?
Active against Herpes virus – H. Simplex, H. Zoster, EBV and CMV
35
How is Ganciclovir usually given? And how is it excreted
IV and is excreted in urine
36
Ganciclovir’s active metabolite attains a higher concentration of where?
Its active metabolite attains higher concentration **inside CMV cells**
37
Ganciclovir adverse effects?
Adverse Effects: o Systemic toxicity is high, bone marrow toxicity (anemia, leukopenia) o rashes, fever, vomiting, **neuropsychiatric disturbances**
38
Ganciclovir adverse effects?
Adverse Effects: o Systemic toxicity is high, bone marrow toxicity (anemia, leukopenia) o rashes, fever, vomiting, **neuropsychiatric disturbances**
39
Which antiviral medication is used only for prophylaxis and treatment of severe CMV infections in immunocompromised patient ?
Ganciclovir
40
Amantadine MOA?
**Uncoating of viral dna** (inhibits replication of influenza virus by **blocking the viral membrane matrix protein (M2)**, required for fusion of viral and host cell membrane)
41
Uses of Amantadine?
- **Influenza-A** (seasonal flu) for reducing fever, congestion, cough for fast recovery - In **Parkinson’s disease (for anticholinergic effects)**
42
Adverse effects and contraindications of Amantadine?
Adverse effects: o Nausea, anorexia, insomnia, dizziness, nightmares o **Mental confusion, & ankle edema** • Contradicted in **CNS disease, GI ulcer, & pregnancy**
43
Compare Rimantadine with Amantidine
Its methyl derivative that’s **more potent, longer acting, better tolerated**, and lower side effects than Amantadine
44
What type of drug is Oseltamivir?
Protease and Release Phase Inhibitors (Neuraminidase inhibitors)
45
Oseltamivir is active against which viruses?
Active against 🐦 - influenza virus (Amantadine sensitive/resistant) - H5N1 (Bird flu) - H1N1 (Swine flu) strain
46
What kind of drug is Palivizumab?
Immunomodulator
47
What can palivizumab prevent?
can prevent **RSV infections**, from high risk of serious respiratory complication in babies