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Found. Pharm > Antibiotics: (Mycin, Micin, Vanc, Zolid, Mulin, and other Miscellaneous agents) > Flashcards

Antibiotics: (Mycin, Micin, Vanc, Zolid, Mulin, and other Miscellaneous agents) Flashcards

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1
Q

Macrolides I

History

A

Erythromycin derived from Streptomyces erythreus from soil in the Philippines => Azithromycin developed by modifying erythromycin => Clarithromycin developed by modifying azithromycin

Structure contain 14 member macrocyclic lactone ring => Class name of macrolide

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2
Q

MOA

Macrolides I

A

Inhibit protein synthesis by binding to 50S ribosomal subunit
- Bacteriostatic

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3
Q

Spectrum of Activity

Macrolides I

A

Gram-positives:
- Streptococci (including S.pneumoniae)

Gram-negatives:
- Haemophilus influenzae
- Moraxella catarrhalis

Atypicals:
- Legionella pneumophila
- Chlamydophila pneumoniae
- Mycoplasma pneumoniae

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4
Q

Clinical Uses

Macrolides I

A
  • Community-acquired pneumonia
  • Pertussis
  • Pharyngitis (alternative therapy)
  • Chlamydia
  • Gonorrhea (alternative therapy)
  • H.pylori infection
  • Infectious diarrhea
  • Skin and soft-tissue infections (alternative therapy)
  • Gastroparesis (erythromycin only)
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5
Q

Adverse Effect

Macrolides I

A
  • Nausea, vomiting, diarrhea
    ‒- Erythromycin&raquo_space; clarithromycin, azithromycin
  • Dysgeusia (clarithromycin)
  • QTc prolongation and cardiac events
  • Hepatotoxicity (rare)
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6
Q

FDA Warning: Cardiac Events

Macrolides I

A

Azithromycin (2013): Risk of QTc prolongation and fatal torsades de pointes (based on retrospective study)
- Increased risk of all cause mortality and cardiovascular mortality compared to no antibiotics
- Increased risk of cardiovascular mortality compared with amoxicillin or ciprofloxacin
- Risk higher in patients with known cardiovascular disease

Clarithromycin (2017): Increased risk of death in patients with heart disease (based on 10 year follow up of a randomized controlled trial)
- Evaluated clarithromycin or placebo for atherosclerosis in patients with
coronary heart disease
- Clarithromycin arm had an increased all cause mortality and cardiovascular mortality

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7
Q

DDI

Macrolides I

A

Erthromycin and Clarithromycin more likely to have interactions than azithromycin
Inhibition of; CYP3A4:P- glycoprotein/ABCB1:OATP1/B3
- Erythromycin: Moderate : Yes : No

  • Clarithromycin: Strong : Yes : Yes
  • Azithromycin: Minor : Yes : No

Additive QTc prolongation with other QTc prolonging agents(e.g., amiodarone)

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8
Q

Formulation

Macrolides I

A

Erythromycin:
- Oral: Tablet delayed-release, as base (Ery-tab®)
- Intraveneous: Solution, aslactobionate (Erythrocin®)
- Topical: Gel (Erygel®)
- Topical: Pad (Ery®)

Clarithromycin
- Oral: Tablet (Biaxin®)
- Oral: Suspension: (Biaxin)

Azithromycin:
- Oral: Tablet (Zithromax®, Zithromax Tri-Pak® (500 mg
PO daily x 3 days), Zithromax Z-Pak® (500 mg PO on day 1, then 250 mg PO on days 2-5))
- Suspension (Zithromax®)
- Packet: (Zithromax®)
- Intravenous :Solution (Zithromax®)
- Ophthalmic: Solution (Azasite®)

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9
Q

Linocosamides

History

A

Lincomycin: Isolated from Streptomyces lincolnensis from soil near Lincoln, Nebraska in 1962 (rarely used today)
Clindamycin:
- Developed from lincomycin in 1966
- Routinely used
- One of the first antibiotics associated with Clostridioides difficile infection

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10
Q

Chemical Structure and Mechanism of Action

Lincosamides

A

Inhibit protein sysnthesis by binding to 50S ribosomal subunit
- Can inhibit toxin production in necrotizing infections
- Bacteriostatic

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11
Q

Spectrum of Activity

Lincosamides

A

Gram-positives
- Staphylococci (including MRSA)
- Streptococci (including S.pyogenes)

Anaerobes
- Bacteroidesspp.
- Clostridium perfringens
- Fusobacterium spp.
- Peptostreptococcus spp.

Non-bacterial Organisms
- Toxoplasma gondii
- Pneumocystis jirovecii
- Babesia spp.
- Plasmodium spp.

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12
Q

Clinical Uses

Lincosamides

A

Skin and soft- tissue infections

Necrotizing fasciitis

Aspiration pneumonia

Bacterial vaginosis

Pneumocystis pneumonia (in combination with other agents)

Toxoplasmosis (in combination with other agents)

Malaria (in combination with other agents)

Acne vulgaris (topical)

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13
Q

Adverse Effects

Lincosamides

A
  • GI: Diarrhea occurs in up to 20% of patients
  • Clostridioides difficile infection (boxed warning)
    – Clindamycin is considered a high risk antibiotic for causing C.difficile infections
  • Allergic reaction (cutaneous)
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14
Q

Formulation

Lincosamides

A

Clindamycin:
Oral:
- Capsule, hydrochloride Cleocin®
- Solution, palmitate
- hydrochloride Cleocin®

Intravenous Solution: (Cleocin Phosphate®)
Topical:
- Cream, vaginal (Cleocin®, Clindesse®)
- Foam, external (Evoclin®)
- Gel, external (Cleocin-T®, Clindagel®)
- Kit, external (Clindacin ETZ®, Clindacin Pac®)
- Lotion, external (Cleocin-T®)
- Solution, external (Cleocin-T®)
- Suppository, vaginal (Cleocin®)
- Swab, external (Cleocin-T®, Clindacin ETZ)

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15
Q

Clindamycin benzoyl peroxide

A

Topical:

Gel, external
- Acanya®
- BenzaClin®
- BenzaClin with Pump®
- Duac®
- Neuac®
- Onexton®

Kit, external
- Neuac®

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16
Q

Clindamycin and tretinoin

A

Topical Gel, external

  • Veltin®
  • Ziana®
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17
Q

Aminoglycosides

Mycin

A

Streptomycin: First aminoglycoside
- 1940s during screening of soil actinomycetes for antimicrobials
- Produced by Streptomyces griseus

Nomenclature varies
- Name ending in mycin: derived from streptomyces
- Name ending in micin: derived from micromonospora

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18
Q

Aminoglycoside Family

A
  • Streptomycin: Streptomyces griseus:1944
  • Neomycin: Streptomyces fradiae:1949
  • Paramomycin: Streptomyces fradiae:1959: Part of neomycin family
  • Gentamicin: Micromonospora spp. : 1963
  • Tobramycin: Streptomyces tenebrarius: 1967: Natural derivative of kanamycin
  • Amikacin: Streptomyces kanamyceticus: 1972: Semisynthetic derivative of kanamycin
  • Plazomicin: Micromonospora spp.: 2018: Semisynthetic derivative of sisomycin
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19
Q

Chemical Structure

Aminoglycoside

A

Aminoglycosides contain amino sugars linked to an aminocyclitol ring by glycosidic bonds

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20
Q

MOA

A

Inhibit protein synthesis by binding to 30S ribosomal subunit
- Bactericidal activity
- Concentration: dependent killing
- Have post antiboitic effect

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21
Q

Spectrum of Activity

Aminoglycoside

A

Gram (+): limited activity
- May be used in combination with cell-wall active agent

Gram (-): Pesudomonas aeruginosa
- Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumanii,…

Other organisms:
- Mycobacterium tuberculosis, Non-tuberculous
mycobacteria, Some parasites

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22
Q

Clinical Use

aminoglycoside

A
  • In combination for serious gram (-) infections
  • In combination for multi-drug resistant gram (-) infections
  • In combination for gram (+) endocarditis (gentamicin only)
  • Urinary tract infections
  • Mycobacterial infections
  • Hepatic encephalopathy (neomycin, paramomycin)
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23
Q

Adverse Effects

Aminoglycoside

Study These Flashcards
A

Nephrotoxicity
- Occur in 10-20% of patients
- Tend to be reversible

Ototoxicity:
- Manifest as vestibular toxicity or cochlear damage
- Can be irreversible

Neuromuscular blockade

24
Q

Therapeutic Drug Monitoring

Study These Flashcards
A

Serum Drug Concentration Monitoring
- Required for IV aminoglycosides
- Minimizes toxicity and resistance
- Maximize efficacy

Types of drug levels vary based on dosing strategy

25
Formulation
- Gentamicin:IV, Opththalmic (Ointment Gentak®) Topical - Tobramycin:IV, Inhalation (Bethkis®, Kitabis Pak®, Tobi®) Ophthalmic (Tobrex®) - Tobramycin and dexamethasone: TobraDex®, TobraDex ST® (Ophthalmic) - Amikcin: IV and inhalation (Suspension:Arikayce®) - Plazomicin: IV (solution: Zemdri) - Streptomycin: Intramuscular/intravenous - Paromomycin: Oral - Neomycin: Oral
26
Glycopeptides | Vancomycin
First glycopeptide antibiotic - Introduced into clinical practice for S.aureus infection - Rarely used adter penicillinase-resistant beta-lactams Gram Positive only: - Staphylococci (including MRSA), Streptococci, Enterococci, Clostridioides difficile,...
27
Chemical Structure | Vancomycin
Tricyclic glycopeptide that contains a 7-membered peptide chain and an attached disaccharide composed of vancosamine and glucose
28
MOA
Inhibit cell wall synthesis - Bind to D-alanyl-D-alanine terminus of cell wall precursors Bactericidal Features of time dependent and concentration dependent activity
29
Clincal Uses | Vancomycin
- Serious gram (+) infection: IV vancomycin ONLY - Clostridiodies difficile infection: PO vancomycin ONLY
30
Adverse Effect | IV Vancomycin
Infusion reaction - Histamine mediated infusion reaction - Not an allergic reaction - Avoided by limiting infusion rate (1000mg/60min) Nephrotoxicity - Incidence is variable - Correlated with high through and high AUC Ototoxicity
31
Therapeutic Drug Monitoring
Serum drug concentration monitoring - Usually required for IV vancomycin ‒ Minimize toxicity, resistance ‒ Maximize efficacy Monitoring strategy is changing - Trough-based -> AUC/MIC-based
32
Formulations
Vanomycine: - IV: Solution - Oral (Capsules: Vancocin®, Solution: Firvanq®)
33
Macrolides III | Fidaxomicin
Macrolide-Like antibiotic - Developed from Dactylsporangium auranticum - Approved in 2011 - Inhibit Bacterial RNA Polymerase - Bactericidal
34
Clinical Uses, Adverse Effects | Fidaxomicin
Narrow Spectrum of Activity - Clostridioides difficile Only used to treat C.difficile infections - Reduced rate of infection recurrence compared with PO vancomycin - Minimal systemic absorption = Minimal adverse effect -
35
Formulation | Fidaxomicin
Fidaxomicin: Oral (Tablet and suspension: Dificid®)
36
Lipopeptide | Daptomycin
Early 1980: produced by streptomyces roseosporus - Clinical trials in 1990s halted to skeletal muscle toxicity but reinteroduced in 2003 with one daily dosing
37
Spectrum of Activity
Gram (+) only: - Staphylococci (including MRSA), Streptococci, Enterococci (including VRE), ... Some strains of enterococci have become daptomycin non- susceptible
38
Clinical Uses | Daptomycin
- Skin and soft-tissue infections - Bacteremia - Endocarditis - Osteomyelitis - Other serious gram-positive infections (cannot be used for pneumonia as it is inactivated by pulmonary surfactant)
39
Adverse Effects | Daptomycin
Generally well tolerated Myopathy and/or rhabdomyolysis - Uncommon - Monitor creatinine phosphokinase (CPK) during treatment
40
Formulation | Daptomycin
Daptomycin: IV (Solution: Cubicin®, Cubicin RF®)
41
Lipoglycopeptides | Telavancin, Dalbavancin, Oritavancin
Semisynthetic derivative of glycopeptides - Longer half-life - Increased Potency FDA Approval - Telavacin (derivative of vancomycin) => Dalbavancin (derivative of teicoplanin) => Oritavancin (derivative of chloroeremomycin)
42
Chemical Structures | Lipoglycopeptides
Contain lipophilic side chains which serve to increase potency and half-life.
43
MOA | Lipoglycopeptides
Same as vancomycin - Telavancin and oritavancin have an additional mechanism: Disrupting cell membrane integrity - Bactericidal Gram-positives only - Streptococci, Enterococci (some strains of VRE),....
44
Clinical Uses | Lipoglycopeptides
Telavancin: - Skin and soft-tissue infections, Hospital-pneumonia, Ventilator-associated pneumonia, Bacteremia Dalbavancin and Oritavancin: Skin and soft-tissue infections only (single dose)
45
Adverse Effect | lipoglycopeptides
Telavancin: - Infusion reaction (similar to vancomycin) - Nephrotoxicity (boxed warning) - QTc prolongation Dalbavancin and oritavancin - Infusion reaction (similar to vancomycin)
46
Formulation | Lipoglycopeptides
Telavancin: IV (Solution Vibativ®) Dalbavancin: IV (Solution Dalvance®) Oritavancin IV (Solution Orbactiv®, Kimyrsa®)
47
Oxazolidinones | Linezolid, Tedizolid
Prepared by organic synthesis - Inhibit protein synthesis by binding to 50s ribosomal subunit - Bacteriostatic Gram-positives only; - Streptococci, Enterococci (some strains of VRE)
48
Clinical Use | Oxazolidnones
Linezolid: - Nosocomial pneumonia (S.aureus or S.pneumoniae), Community-pneumonia (S.aureus or S.pneumoniae), Skin and soft-tissue infections, VRE infections Tedizolid: Skin and soft tissue infection
49
Adverse Effect | Oxazolidinones
Myelosuppression: - Thrombocytopenia is most common blood dyscrasia - Occurs at > 2 week of treatment Mitochondial toxicity - Peripheral neuropathy, optic neuritis, lactic acidosis - Occur at > 4 weeks of treatment Serotonin Syndrome (rare AE is less common with tedizolid
50
DDI | Oxazolidinones
Risk of serotonin syndrome when used with proserotonergic drugs - Linezolid is a reversible, nonselective MAOI - Tedizolid is a weak MAOI (appears to have ↓ risk for this interaction) Signs/symptoms - Agitation, confusion, hallucinations, hyperreflexia, myoclonus, shivering, tachycardia
51
Formulation | Oxazolidinones
Linezolid: IV (Solution: Zyvox®) and Oral (Tablet, Suspension: Zyvox®) Tedizolid: IV (Solution: Sivextro®) And Oral (Tablet: Sivextro®)
52
Pleuromutilins | Lefamulin (approved 2019)
Used in veterinary medicine and topical use in humans (retapamulin) - Due to toxcicity concerns with older products Inhibit protein synthesis by binding to 50S ribosomal subunit - Bactericidal/Bacteriostatic
53
Spectrum of Activity | Lefamulin
Gram- positives - Staphylococci (including MRSA), Streptococci (including S.pneumoniae) Gram-negatives - Haemophilus influenzae, Moraxella catarrhalis Atypicals - Legionella pneumophila, Chlamydophila pneumoniae, Mycoplasma pneumoniae
54
Clinical Uses and Adverse Effect | Lefamulin
Clinical Use: - Community-pneumonia Adverse Effect: - Nausea, Diarrhea, QTc prolongation DDI: - Moderate CYP3A4 inhibitor, - Additive QTc prolongation with other QTc prolonging drugs Contraindication: - Concommitant use with CYP3A3 substrates that prolong QTc
55
Formulation | Lefamulin
Lefamulin: IV (Solution: Xenleta®) and Oral (Tablet: Xenleta®)
56
IMPORTANT MESSAGE
- Many antibioties are derived from natural sources - Macrolides are mainly used for respiratory infections - Clindamycin was one of the first antibiotics to be associated with C. difficile infection - PO Vancomycin and fidaxomicin can be used to treat C. difficile infection
57
IMPORTANT MESSAGE II
- Aminoglycosides have poten Gram-negative activity but limited by toxicities - Vancomycin is GREAT for serious Gram-positive infection in hospital seting - Vancomycin and aminoglycosides require therapeutic drug monitoring - Liinezolid and daptommycin can be used to treat VRE infections

Found. Pharm (14 decks)

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