Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

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

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

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

MOA

Macrolides I

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Adverse Effect

Macrolides I

A
  • Nausea, vomiting, diarrhea
    ‒- Erythromycin&raquo_space; clarithromycin, azithromycin
  • Dysgeusia (clarithromycin)
  • QTc prolongation and cardiac events
  • Hepatotoxicity (rare)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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®)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Clindamycin benzoyl peroxide

A

Topical:

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

Kit, external
- Neuac®

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Clindamycin and tretinoin

A

Topical Gel, external

  • Veltin®
  • Ziana®
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Chemical Structure

Aminoglycoside

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

MOA

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Adverse Effects

Aminoglycoside

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

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
Q

Formulation

A
  • 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
Q

Glycopeptides

Vancomycin

A

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
Q

Chemical Structure

Vancomycin

A

Tricyclic glycopeptide that contains a 7-membered peptide chain and an attached disaccharide composed of vancosamine and glucose

28
Q

MOA

A

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
Q

Clincal Uses

Vancomycin

A
  • Serious gram (+) infection: IV vancomycin ONLY
  • Clostridiodies difficile infection: PO vancomycin ONLY
30
Q

Adverse Effect

IV Vancomycin

A

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
Q

Therapeutic Drug Monitoring

A

Serum drug concentration monitoring
- Usually required for IV vancomycin
‒ Minimize toxicity, resistance
‒ Maximize efficacy

Monitoring strategy is changing
- Trough-based -> AUC/MIC-based

32
Q

Formulations

A

Vanomycine:
- IV: Solution
- Oral (Capsules: Vancocin®, Solution: Firvanq®)

33
Q

Macrolides III

Fidaxomicin

A

Macrolide-Like antibiotic
- Developed from Dactylsporangium auranticum
- Approved in 2011
- Inhibit Bacterial RNA Polymerase
- Bactericidal

34
Q

Clinical Uses, Adverse Effects

Fidaxomicin

A

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
Q

Formulation

Fidaxomicin

A

Fidaxomicin: Oral (Tablet and suspension: Dificid®)

36
Q

Lipopeptide

Daptomycin

A

Early 1980: produced by streptomyces roseosporus
- Clinical trials in 1990s halted to skeletal muscle toxicity but reinteroduced in 2003 with one daily dosing

37
Q

Spectrum of Activity

A

Gram (+) only:
- Staphylococci (including MRSA), Streptococci, Enterococci (including VRE), …

Some strains of enterococci have become daptomycin non- susceptible

38
Q

Clinical Uses

Daptomycin

A
  • 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
Q

Adverse Effects

Daptomycin

A

Generally well tolerated
Myopathy and/or rhabdomyolysis
- Uncommon
- Monitor creatinine phosphokinase (CPK) during treatment

40
Q

Formulation

Daptomycin

A

Daptomycin: IV (Solution: Cubicin®, Cubicin RF®)

41
Q

Lipoglycopeptides

Telavancin, Dalbavancin, Oritavancin

A

Semisynthetic derivative of glycopeptides
- Longer half-life
- Increased Potency

FDA Approval
- Telavacin (derivative of vancomycin) => Dalbavancin (derivative of teicoplanin) => Oritavancin (derivative of chloroeremomycin)

42
Q

Chemical Structures

Lipoglycopeptides

A

Contain lipophilic side chains which serve to increase potency and half-life.

43
Q

MOA

Lipoglycopeptides

A

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
Q

Clinical Uses

Lipoglycopeptides

A

Telavancin:
- Skin and soft-tissue infections, Hospital-pneumonia, Ventilator-associated pneumonia, Bacteremia

Dalbavancin and Oritavancin: Skin and soft-tissue infections only (single dose)

45
Q

Adverse Effect

lipoglycopeptides

A

Telavancin:
- Infusion reaction (similar to vancomycin)
- Nephrotoxicity (boxed warning)
- QTc prolongation

Dalbavancin and oritavancin
- Infusion reaction (similar to vancomycin)

46
Q

Formulation

Lipoglycopeptides

A

Telavancin: IV (Solution Vibativ®)
Dalbavancin: IV (Solution Dalvance®)
Oritavancin IV (Solution Orbactiv®, Kimyrsa®)

47
Q

Oxazolidinones

Linezolid, Tedizolid

A

Prepared by organic synthesis
- Inhibit protein synthesis by binding to 50s ribosomal subunit
- Bacteriostatic

Gram-positives only;
- Streptococci, Enterococci (some strains of VRE)

48
Q

Clinical Use

Oxazolidnones

A

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
Q

Adverse Effect

Oxazolidinones

A

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
Q

DDI

Oxazolidinones

A

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
Q

Formulation

Oxazolidinones

A

Linezolid: IV (Solution: Zyvox®) and Oral (Tablet, Suspension: Zyvox®)
Tedizolid: IV (Solution: Sivextro®) And Oral (Tablet: Sivextro®)

52
Q

Pleuromutilins

Lefamulin (approved 2019)

A

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
Q

Spectrum of Activity

Lefamulin

A

Gram- positives
- Staphylococci (including MRSA), Streptococci (including S.pneumoniae)

Gram-negatives
- Haemophilus influenzae, Moraxella catarrhalis

Atypicals
- Legionella pneumophila, Chlamydophila pneumoniae, Mycoplasma pneumoniae

54
Q

Clinical Uses and Adverse Effect

Lefamulin

A

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
Q

Formulation

Lefamulin

A

Lefamulin: IV (Solution: Xenleta®) and Oral (Tablet: Xenleta®)

56
Q

IMPORTANT MESSAGE

A
  • 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
Q

IMPORTANT MESSAGE II

A
  • 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)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions