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Pharm antibiotics part 2 Flashcards

1
Q

Antimicrobial agents- MOA

A

Part 1: cell wall synthesis and cytoplasmic membrane structure
* betalactams= Penicillins, Cephalosporins, Carbapenems, Monobactam
* glycopeptides= Vancomycin
* cyclic lipopeptide= Daptomycin

Part 1: target DNA or DNA replication
Antimetabolites: sulfonamides and trimethoprim
Fluoroquinolones: Ciprofloxacin, Levofloxacin, Ofloxacin

Now= block production of new proteins= bacterial ribosome
Aminoglycosides: neomycin, Gentamicin, Tobramycin, and amikacin, strptomycin
Tetracyclines: tetracycline, doxycycline, minocycline
Macrolides: Erythromycin, Clarithromycin, Azithromycin
Clindamycin
Linezolid
Chloramphenicol

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2
Q

Aminoglycosides types

A
  1. Gentamicin
  2. Tobramycin
  3. Amikacin
  4. Plazomicin
  5. Streptomycin
  6. Neomycin
  7. Paromomycin
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3
Q

Aminoglycosides MOA

A
  1. cause addition of incorrect aa resulting in synth of abn proteins
  2. cause misreading of mRNA and terminate protein synth
  3. Bind to 30S ribosomes and block the initiation of protein synth
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4
Q

Pharmacodyn and kinetic prop of Aminoglycosides

A
  1. Favorable target: Aerobic Gram - rods and mycobacteria
  2. Postantibiotic effect PAE= persistent suppression of growth after drug done
  3. Conc dependent killing characteristics-> higher conc induce more rapid killing
  4. Synergistic effect= in combo, MC cell wall active agents to help target gram positive bacteria
  5. Absorption= peak conc -> 30-60 min IV and 30-90 min IM
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5
Q

Aminoglycoside Toxicity

A

Nephrotoxicity
Ototoxicity
Neuromuscular blockade

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6
Q

Aminoglyc routes and indications

A

*Neomycin-> topical with Bacitracin and Polymyxin
* Gentamicin: topic, opth, systemic-> Group B streptococcus
* Tobramycin: Inhalation for CF patients with pseudomonas infections
* Streptomycin: second line drug for TB

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7
Q

General Aminoglycosides indications

A
  1. Septicemia
  2. Complicated UTI
  3. complicated Intraabdominal
  4. combo with others for drug resistant organisms
  5. topical drugs in conjunc for Otitis Externa
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8
Q

Otitis External- swimmers ear

mc: STAPH AUREUS AND PSEUDOMONAS AERUGINOSA

A

topical only: Fluoroquinolones ie
* ciprofloxacin
* Ofloxacin

AB with glucocorticoid: hydrocortisone, Dexamethasone, Prednisolone
* Neomycin
* Tobramycin
* Gentamycin
* allllllllll aminoglycosides
* combos: neomycin, polyyxin B, hydrocort= Cortisporin otic
* Combos: tobramycin and dexamth= Tobradex- opthalmic solution

Fluoroquinolones:
* Ciprofloxacin and Ofloxacin
* combos
ciprofloxacin and dexamethasone-Ciprodex
ciprofloxacin and hydrocortisone- Cipro HC Otic

DO NOT GIVE STEROID IN PERFORATED EAR DRUMS

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8
Q

Otitis External- swimmers ear

mc: STAPH AUREUS AND PSEUDOMONAS AERUGINOSA

A

topical only: Fluoroquinolones ie
* ciprofloxacin
* Ofloxacin

AB with glucocorticoid: hydrocortisone, Dexamethasone, Prednisolone
* Neomycin
* Tobramycin
* Gentamycin
* allllllllll aminoglycosides
* combos: neomycin, polyyxin B, hydrocort= Cortisporin otic
* Combos: tobramycin and dexamth= Tobradex- opthalmic solution

Fluoroquinolones:
* Ciprofloxacin and Ofloxacin
* combos
ciprofloxacin and dexamethasone-Ciprodex
ciprofloxacin and hydrocortisone- Cipro HC Otic

DO NOT GIVE STEROID IN PERFORATED EAR DRUMS

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9
Q

Tetracyclines types

A
  1. Chlortetracycline
  2. Minocycline
  3. Doxycycline
  4. Eravacycline
  5. Sarecycline
  6. Omadacycline
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10
Q

Tetracyclines MOA

A
  1. Bacteriostatic
  2. Passive diffusion and transporter uptake
  3. inhibit protein synthesis
  4. aerobic gram + and -
  5. Intracellular bacteria:
    * rickettsiae
    * chlamydiae
    * mycoplasmas
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10
Q

Tetracyclines MOA

A
  1. Bacteriostatic
  2. Passive diffusion and transporter uptake
  3. inhibit protein synthesis
  4. aerobic gram + and -
  5. Intracellular bacteria:
    * rickettsiae
    * chlamydiae
    * mycoplasmas
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11
Q

Pharmacokinetics Doxycycline and Minocycline

absorption, distribution, excretion, classification

A

Absorption
* 95-100% absorbed orally, duodenum, ALL TETRAC IMPAIRED BY MULTIVALENT CATIONS- Ca, Mg, Fe, Al
* Doxycycline and minocycline absorption NOT IMPAIRED BY FOODS

Distribution
* CROSS PLACENTA, NOT INDICATED IN PREGNANCY
* high tissue penetration except CSF

Excretion
* mainly in bile and urine
* Doxycycline: elim by nonrenal mechanisms, no dose adjustment required in renal failure

Classification:
* short acting- regular tetra: 6-8 hours
* long acting- doxy and mino: 16-18 hours

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12
Q

Tetracyclines- Side effects

A
  1. Photosensitivity- doxy is biggest culprit
  2. GI disturbances- dose related, abdominal discomfort, food decrease symptoms
  3. Hepatotoxicity- rare
  4. Audiovestibular- dizziness, vertigo, tinnitis= Doxy and mino
  5. Teeth and bone- calcium attaches to and deposit in bone
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13
Q

Doxycycline/Minocycline indications

broad uses

A
  1. Acne
  2. Rosacea
  3. URI
  4. Pneumonia CAP
  5. Chlamydia
  6. Syphilis
  7. GU
  8. Anthrax
  9. Malaria
  10. tick borne disease
  11. H. Pylori
  12. other= ehrlichiosis, anaplasmosis, plasmodium, mycobacteria
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14
Q

Helicobacter Pylori

H. Pylori

A

4 drug therapy:
1. Proton pump inhibitor PPI
2. Bismuth subsalicylate
3. Tetracycline
4. Metronidazole

Bismuth Quadruple Therapy for 10-14 days

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15
Q

Macrolides types

A
  1. Erythromycin
  2. Clarithromycin
  3. Azithromycin
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16
Q

Macrolides MOA

A

inhibit bacterial synthesis

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17
Q

Macrolides AE

A
  • GI upset
  • acute cholestatic hepatitis-> fever, jaundice, imparied liver fxn
  • Prolonged QT interval- effect potassium ion channels
  • hearing loss and exacerbation of Myasthenia Gravis
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18
Q

Macrolides MOR

A
  1. Target site modification by methylation or mutation= prevents binding of ab to its ribosomal target
  2. Efflux via active pumping
  3. Inactivation via enzymatic process
19
Q

Erythromycin clinical indications

A
  • conjunctivitis/Pneumonia in neonates= Erythromycin ethylsuccinate or estolate
  • Off label as Promotility agent for pt with gastroparesis= helps with constipation too
  • diptheria
  • chlamydia
20
Q

Azythromycin info

Z pack

A
  • long half life and tissue levels
  • short rx course and improved compliance
  • avoid antacids
  • Doesn’t inhibit CYPS
  • Overuse is a problem

some use for Viral too and coincidently feel better @ 5 days

21
Q

Azythromycin info

Z pack

A
  • long half life and tissue levels
  • short rx course and improved compliance
  • avoid antacids
  • Doesn’t inhibit CYPS
  • Overuse is a problem

some use for Viral too and coincidently feel better @ 5 days

22
Q

Azythromycin indications

A
  1. Chancroid (Haemophilus Ducreyi - Gram Neg Bacillus)
  2. Cat scratch disease (Bartonella Henselae)
  3. Community Acquired pneumonia- outpatient
  4. Nongonococcal urethritis
  5. Cervicitis chlamydia trachomatis
  6. others= exacerbations of chronic bronchitis, streptococcal pharyngitis
23
Chancroid- Haemophilus Ducreyi | Gram Negative Bacillus
* STD- painful soft ulcer with erythema surrounding * Adenitis- unilateral tender matted nodes, overlying erythema * Men= penile * women= labia majora (kissing lesions) transfers to other lip TX: Azythromycin oral single dose or Ceftriaxone IM
24
Cat scratch disease
lymphadenopathy, mastoiditis? tx: Azythromycin
25
CAP- community acquired | STreptococus pneumoniae, mycoplasma pneumoniae
No comorb, no recend ab in 90 days: * amoxicillin * Doxycycline * Macrolide Duration= **treat 5 days** Comorbid of heart disease, kidney * Macrolid or Doxy PLUS Oral Beta lactam * monotherapy with Fluoroquinolone
26
Nongonococcal urethritis and cervicitis chlamydia trachomatis
Azithromycin single dose, safe for prego
27
Azithromycin warnings
1. Potentially fatal irregular heart rhythm- mostly for those with pre existing heart disease 2. pyloric stenosis in neonates given azith for pertussis
28
Clarithromycin
* Initial metab is hepatic but PRIMARY metabolite cleared by kidney= **need dosing adjustment for renal failure** * **Less GI SE but no sig difference from erythromycin** * higher cost * highly stable in gastric acid * same drug interactions as erythromycin= WATCH PROLONGED QT Indications: * mycobacterium avium complex- mac * CAP * Acute exacerbation of chronic bronchitis
29
Clarithromycin BLACK BOX WARNING
***heart disease= potential increased risk of heart problems or death that can occur years later**
30
Macrolides Drug interactions
Erythromycin and Clarithromycin inhibit **CYP3A4**-> may increase conc of many drugs such as * **alfentanil and sufentanil** * **Oral anticoagulants- warfarin** * **glibenclamide** * **Azithromycin not reported to have significant interactions**
31
Clindamycin | lincomycin derivative
spectrum: strep, staph, pneumococcus, anaerobes DO NOT PENETRATE GRAM NEG ORGANISMS BC OF OUTER MEM Indications: * skin, soft tissue * with aminoglyc/cephalosporin= penetrating gut wounds, pelvic abscess, septic abortion * Dental prophylaxis in endocarditis * MRSA
32
Chloramphenicol
* Very broad spectrum: + - and anaerobes * res from special plasmid encoded enzyme= acetyltransferase * Rare use: rickettsiae, menigococcus, plage * SE: BM suppression, aplastic anemia, **Gray baby syndrome- drug accum lead to cardiovascular collapse- monitor peak/trough levels** * otc in mexico
33
Linezolid
bacteriostatic and oxazolidinone Indications: Pneumonia, skin infections, mrsa- reserve for multidrug res SE: thrombocytopenia, neutropenia, peripherla and optic neuropathy SEROTONIN SYNDROME->avoid tyramine= weak monomine oxidase inhibitor No renal adjustment needed tyramine is a monamine compound and acts as a catecholaine releasing agent * cured meats, chocolate, beer, most cheese, fava beans, snow peas, avocados, bananas, pineapples, plums, raspberries | linezolid inhibits both forms of monamine oxidase
34
Nitrofurantoid
**UTI** Metab: liver 75% and 25% urine Indications: UTI, prophylaxis for recurrect UTI (simple cystitis) pseudomonas and proteus resistance SE: GI, Caution iwth G6PD and elderly with pulmonary fibrosis
35
Mupirocin | topicals
topical: cream, ointment, intranasal- not in us Indications: * impetigo * surgical prophylaxis in MRSA carriers * Elimination of MRSA colonization AE: burning/stinging, rhinitis, headache MOA: inhibition of protein synthesis | COVERS BOTH STAPH AUREUS AND STREP PYOGENES, MOST STREP
36
Bacitracin | topical
used for PRevention of disease Usually with neomycin and/or polymyxin B= neomycin is very sensitizing topically= allergic reaction so dont use unless need it MOA: inhibits cell wall synth Targets= + clean area and apply small amount
37
Acne Vulgaris | very common
Disorder of pilosebaceous unit abn desquamation of keratinocytes lining sebaeous follicle= microplug increase in circulating androgens stim the production of sebum into unit favorable for colonization of Cutibacterium acnes C. acnes-> stim t cells and mac-> inflamm and chemotactic factors-> local inflam and induce keratinocyte hyperprolif ## Footnote can effect any age
38
Lifestyle tx of acne
* wash your face * friction and trauma from headbands/straps * application of comedogenic topical agents * chronic exposure to certain industrial compounds * Steroids (topicl, systemic) or PCOS bc tx will solve * other meds: lithium, isoniazid * low glycemic diet
39
Acne tx overview
1. Comedonal acne * topical retinoids * benzoyl peroxide 2. Papular or Cystic inflammatory acne * topicals clindamycin phosphate and erythromycin with benzyl peroxide * oral ab- tetracyclines, tmp-smz, cephalosporins 3. Severe acne * isotretinoin * intralesional injection of triamcinolone acetonide
40
Tretinoin | acne tx
what is it? vitamin A derivative= mods epithelial growht and diff Prego safe? NO, TETRAGENIC EFFECTS IN PREGO Peds? OK in 8 yoa and up SE?- Dryness, redness, swelling, blisters, warmth Strengths? adapalene to tretinoin Patient Education: may flare be4 clinical different in 4 weeks, may start 1-2 times weekly and work up to nightly use to tolerate
41
Benzyl peroxide | acne tx
how does it work? releases free radical oxygen which oxidized bacterial proteins in sebaceous follicles decreasing number of anaerobic bacteria and decreasing irritating type FA warnings= bleaching effects SE: dryness, irritation, itching, peeling, may be combined ## Footnote bleaches sheets
42
Tx for Comedonal acne
1. Topical retinoids: Tretinoin, can flare 2. Benzoyl Peroxide- OTC
43
Topical antibiotics
topical clindamycin and erythromycin is combined with benzyl peroxide in order to prevent development of bacterial resistance
44
Papular or cystic inflammatory acne | resistant to topicla therapy with retinoids or benzoyl peroxide
mild acne: topical antibiotics-> erythromycin or clindamycin Moderate acne: oral-> Doxycycline or mInocycline or TMP-SMX
45
Isotretinoin | Acutane ## Footnote most clearing, quickest, not come back
SEVER ACNE: MOA: vitamin A analog Contraindications: PREGO CAT X, BREASTFEEDING AE: Dry, photosensitive Monitoring: CMP and lipids, PREGNANCY EVERY TIME TWO FORMS OF BIRTH CONTROL MUST BE USED ENROLLED IN MONITORING PROGRAM IPLEDGE
46
Clincal spectrum of acne
comedonal acne neonatal acne rhinophyma acne rosacea acne conglobata
47
Hormonal Acne tx
1. Spironolactone * MOA: decreases testosterone production 2. OCP- * estrogen containing cpc

Pharm (9 decks)

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