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Abx Groups Flashcards

1
Q

Natural Penicillins

A
  • PCN G
  • PCN V
  • Beta lactamase susceptible
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2
Q

Beta lactamase resistant Penicillins

Antistaphylococcal PCNs

A
  • Nafcillin
  • Oxacillin
  • Dicloxacillin
  • Methicillin
  • Bulky side chain protects from beta lactamase, but limits them to gram positive only
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3
Q

Extended Spectrum Penicillins

A
  • Amoxicillin/Clavulanate
  • Ampicillin/Sulbactam
  • Pipercillin/Tazobactam
  • Ticarcillin/Tazobactam
  • Increased gram negative coverage due to smaller molecule size
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4
Q

Monobactam

A

Aztreonam

  • only active against aerobic gram neg rods, IV only, CNS penetrance, no cross reactivity with PCN allergy
  • dose adjust in renal failure
  • beta lactamase sensitive
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5
Q

Carbapenems

A
  • Doripenem
  • Ertapenem
  • Imipinem/Cilastin - lowered seizure threshold
  • Meropenem
  • Resistant to beta lactamases, can be hydrolyzed by ESBLs and carbapenemases, IV only, all cover pseudomonas except ertapenem
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6
Q

Macrolides

A
  • Erythromycin - absorption problem, don’t take with food, GI upset, inhibits CYP3A4, used for pertussis, chlamydia
  • Clarithromycin
  • Azithromycin - Zpack, super overused, slow half life, single dose chlamydia tx
  • Bind to 50s subunit, resistance via efflux, reduced permeability, modification of ribosomal binding site
  • D-test - indicates macrolide inducible resistance to Clindamycin by inducible methylase, alters binding site
  • prolongs QT segment
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7
Q

Ketolides

A
  • Telithrolide

- same MOA as macrolides, less resistance, CYP450 inhibitor so drug induced hepatitis

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8
Q

First Gen Cephalosporins

A
  • Cefazolin
  • Cefalexin
  • Renal excretion, no CNS penetrance, active against gram pos cocci (but not enterococci)
  • used for MSSA infection, surgical wound prevention in PCN allergic patients, pan-susceptible E. Coli UTI
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9
Q

Second Gen Cephalosporins

A
  • Cefaclor - serum sickness rxn, not used clinically
  • Cefoxime - IV only, used for perioperative wound prevention and prophylaxis in operations on GI or GU (anaerobes)
  • Cefuroxime - used PO for outpatient resp infections
  • Cefotetan - IV only, used for perioperative wound prevention and prophylaxis in operations on GI or GU (anaerobes), disulfuram-like rxn w alcohol, hypothrombinemia, bleeding
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10
Q

Third Gen Cephalosporins

A
  • Ceftriaxone - IV, CNS penetrance, biliary excretion, overused in ER
  • Cefdinir - oral outpatient, red poop
  • Cefotaxime - IV, CNS penetrance
  • Ceftazidime - antipseudomonal, similar to Aztreonam
  • Cefixime - previously used for gonorrhea
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11
Q

Fourth Gen Cephalosporins

A
  • Cefipime
  • excellent gram neg coverage, increased activity against MDR strep pneumo, drug of choice in neutropenic fever, sepsis in sickle cell patients
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12
Q

Fifth Gen Cephalosporins

A
  • Ceftaroline
  • Ceftolazone/Tazobactam
  • use with ID oversight
  • only cephs w enterococcal activity
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13
Q

Cell Wall Inhibitors

A
  • Vancomycin
  • Televancin - same MOA, less toxicity than Vanc
  • Daptomycin - inserts tail into cell membrane
  • Fosfomycin - enolpyruvate transferase inhibitor
  • Bacitracin - topical for nose and butthole MRSA, inhibits bactoprenols
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14
Q

Tetracyclines

A
  • Doxycyclin - interacts w phenytoin
  • Demeclocyclin - also inhibits action of ADH at collecting duct
  • Tetracyclin
  • Tigecyclin - very broad spectrum, use w ID, pseudomonas and proteus only resistant bugs
  • Minocyclin
  • reversible binding to 30s subunit, take with food but not with dairy, antacids, or metal cations, teratogenic
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15
Q

Lincosamides

A
  • Clindamycin
  • Same MOA as macrolides (50s), good for anaerobes, penetrates abscesses and pus
  • resistance by mutation of binding site, methylase (induced or constitutive) checked with D test
  • tastes like shit
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16
Q

Streptogramins

A
  • Quinipristine/ Dalfopristin (Synercid)
  • block transpeptidase on 50s and translocation at 23s
  • Cover PCN resistant gram pos except E. faecalis, no gram neg coverage
  • inhibits CYP3A4, interacts w warfarin, diazepam, NNRTIs, cyclosporine
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17
Q

Chloramphenicol

A
  • binds 50s
  • inactivated by liver glucuronyl transferase
  • Grey baby syndrome
  • inhibits metabolism of phenytoin, tolbutamide, chlorpropamide, and warfarin
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18
Q

Oxalidinones

A
  • Linezolid
  • prevents formation of entire ribosome complex
  • no cross resistance
  • used for VRE
  • reversible and mild hematologic toxicities: thrombocytopenia, anemia, neutropenia
  • also optic/peripheral neuropathy and serotonin syndrome if given w SSRIs
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19
Q

Aminoglycosides

A
  • Gentamicin - naive pseudomonas,
  • Tobramycin - naive pseudomonas, inhaled form for CF
  • Neomycin - too toxic for IV
  • Kanamycin
  • Amikacin - backup if genta or tobra resistant
  • Streptomycin
  • aerobic gram neg bacilli, use in systemic gram neg infections like intra abdominal infections or complicated UTI, no penetration for abscesses
  • synergistic with cell wall drugs, bind 30s
  • nephrotoxic, ototoxic w trough levels less than 2mcg/mL
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20
Q

SABAs

A
  • Albuterol
  • Levalbuterol - L-isomer of albuterol, indicated only for patients with documented ventricular arrhythmia w albuterol. Much more expensive.
  • Rescuers - If used more than 2 days/week, consider increasing controller therapy
  • Beta 2 agonists (activate Gs, increase cAMP, decrease MLCK)
  • Use with spacer
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21
Q

LABAs

A
  • Salmeterol
  • Formoterol
  • Indicaterol - only once daily LABA, only approved for COPD
  • Terbutaline - IV, can also be used in premature labor
  • Controllers, mono therapy contraindicated for asthma and COPD
  • Should only be used in asthma as an adjuvant to ICSs, step down if possible
22
Q

Inhaled Anticholinergics

A
  • Ipratropium Bromide (SAAB)
  • Tiotropium (LAAB)
  • MOA: block acetylcholine, decrease cGMP, cause bronchodilator and decreased mucus production
  • Rescuers, greater role in COPD
23
Q

Calcium affecting

A
  • Magnesium Sulfate
  • CCB by competitive inhibition for divalent cationic sites
  • Side effects: nausea, vomiting, hypotension (bonus w normal saline to prevent), in toxicity decreased deep tendon reflex and rapid development of pulmonary edema
24
Q

Phosphodiesterase Inhibitors

A
  • Theophylline - MOA: inhibiting PDE increases cAMP in adrenal medulla, promotes release of epinephrine, causes brochodilation
    • can help as add-on for some patients, but limited due to side effects, drug interactions, narrow therapeutic window, unpredictable metabolism
  • Roflumilast - PDEI that reduces inflammation but does not bronchodilate
    • selectively inhibits PDE4, use only in severe COPD
  • Controllers
25
Q

Inhaled Corticosteroids

A
  • Beclomethasone
  • Budesonide
  • Fluticasone
  • Triamcinolone
  • Controllers, reduce airway inflammation , maximal response requires treatment for up to 8 weeks
  • prolonged use can increase risk of secondary infection, oral thrush if mouth isn’t rinsed
  • primary treatment for status asthmatic us or acute episodes, but acute broncos past relief requires oral steroids
26
Q

Leukotriene Modifiers

A
  • Zafirlukast
  • Montelukast (Singulair)
    • These two are leukotriene receptor antagonists (LRTAs) of LTD4 receptors
  • Zileuton- 5-lipoxygenase inhibitor, prevents leukotriene formation
  • Controllers, decrease airway edema, constriction and inflammation
  • Depression and suicide black box warnings
27
Q

Mast cell actors

A
  • Cromolyn Sodium - stabilizes plasma membranes of mast cells and eosinophils, preventing degranulation and release of histamine, leukotrienes, other substances
  • Omalizumab - inhibits IgE binding to mast cells and eosinophils, only indicated in step 5 or 6, anaphylaxis risk
  • Controllers
28
Q

Oral absorbable Sulfonamide drugs

A
  • Sulfisoxazole
  • Sulfamethoxazole
  • Sulfadoxine/Pyrimethamine
  • Sulfamethoxazole/Trimethoprim - p. Jirovecii prophylaxis and tx, toxoplasmosis, prostatitis, good activity against community acquired MRSA
  • displace bilirubin from albumin, pancytopenia, hemolytic anemia in G6PD deficiency, crystallization in urinary tract, photosensitivity, rash, SJS, hypersensitivity rxns that look autoimmune
29
Q

Oral non-absorbable Sulfonamide drug

A
  • Sulfasalazine

- anti inflammatory that is only locally absorbed in but and doesn’t reach systemic levels, used in IBD

30
Q

Topical Sulfonamide Drugs

A
  • Sulfacetamide - eye drops for pink eye and chlamydia trachomatis
  • Silver Sulfadiazine - topical abx used extensively in burn unit
31
Q

Imidazoles

A
  • Ketoconazole - can treat endogenous Cushing’s syndrome
  • Miconazole
  • Clotrimazole
  • Block CYP450 dependent ergosterol precursor production
  • Drug interaction major issue: compete w other drugs if CYP450 inhibitors given
32
Q

Triazoles

A
  • Fluconazole - most frequent for skin, genital, soft tissue, oral, and esophageal candida
  • Voriconazole - most teratogenic, must use contraceptives if on drug, QT prolongation, transient visual or auditory hallucinations
  • Itraconazole - major hepatic toxicity can occur, can cause CHF in patients with pre existing LV dysfunction
  • Block CYP450 dependent ergosterol precursor production
  • Drug interaction major issue: compete w other drugs if CYP450 inhibitors given
33
Q

Other TB tx

A
  • Cycloserine - D-ala analogue, “psych-serine”
  • Para-aminosalicylic acid (PAS) - PABA analogue, MOA Unknown, first TB treatment
  • Dapsone - PABA analogue, competitively inhibits dihydropterate synthetase (like sulfas), used in inflammatory dz, severe hemolysis in G6PD deficiency
  • Clofazimine - orphan drug, red-black skin, crystals in GI, liver, LNs
  • Bedaquiline - inhibits ATP synthase, 5 fold increased risk of all cause death, QT prolongation
  • Pretomanid - experimental, similar to metronidazole, inhibits mycolic acid, protein synthesis, generates NO that augments killing
34
Q

Oral antifungals

A
  • Amphotericin B - nephrotoxic it’s major problem: hypokalemia, hypomagnesia, RTA causing NAGMA, anemia from low EPO
  • Flucytosine - fungal cytosine delaminates converts to 5-FU, which blocks thymidylate synthetase, halting DNA production, used w Ampho B
  • Caspofungin - an echinocandin, prevents cross linkage of chitin with glucans (glucan synthestase), IV only, no CNS penetrance, increases tacrolimus levels, metabolized in liver
  • Griseofulvin - take with fatty food, inhibits micro tubule formation, disrupts mitotic spindle, deposits in precursors or keratin producing cells
  • Terbinafine - inhibits squealing epoxidase, blocking ergosterol synthesis
35
Q

Topical Antifungals

A
  • Naftifine
  • Butenafine
  • Nystatin - swish and swallow
  • Tavaborole - onchomycosis
36
Q

TB Primary use

A
  • Rifampin
  • Isoniazid - Inhibits mycolic acid synthesis, metabolized by NAT2, fast/slow acetylators, can cause hypersensitivity syndromes, methemoglobinemia, peripheral neuritis and neurotoxicity du to pyridoxine deficiency
  • Pyrazinamide - activated by acidic conditions in edge of TB cavity, disrupts cell membrane, accumulates in lung epithelial lining fluid, fast/slow absorbers, can precipitate gout
  • Ethambutol - inhibits arabinosoyl transferase III, loss of red green vision
  • Streptomycin
  • All associated with hepatotoxicity
37
Q

Rifamycins

A
  • Rifampin - strong post abx effect, must be taken on empty stomach, many drug interactions (induces CYP450), poor CNS penetrance, orange body fluids
  • Rifapentine
  • Rifabutin
  • Macrolide abx, enter acid fast bacillus in a concentration dependent manner and bind the beta subunit of DNA dependent RNA polymerase
38
Q

Mucolytics

A
  • Guaifenisin (Mucinex, Mucinex D) - increases respiratory hydration, requires patient to drink lots of water
  • Acetylcysteine - Mucolytic effect related to sulfhydryl group, which reduces disulfide linkages in mucus and lowers viscosity
39
Q

Cough Suppressants

A
  • Dextromethorphan - SSRI and NMDA blocker at high doses
  • Codeine - unpredictable metabolism
  • Hydrocodeine - unpredictable metabolism
    • These three suppress cough reflex at medullary cough center
  • Benzonatate (Tessalon Pearls) - topical anesthetic action on respiratory stretch receptors
40
Q

Intranasal Corticosteroids

A
  • Beclomethazone (Beconase)
  • Budesonide (Rhinocort)
  • Ciclesonide (Omnaris)
  • Fluticasone (Flonase)
  • Mometasone (Nasonex)
  • Triamciclone (Nasacort)
  • Similar side effect profile to systemic corticosteroids, but much lower risk: adrenal suppression, delayed wound healing, nasal septal perforation, increased intra ocular pressure
41
Q

Intranasal Antihistamine

A
  • Aselastine - Astelin - 40% bioavailability, fecal elimination
  • Olopatadine - Patanase
  • Systemic side effects lessened
42
Q

Systemic Decongestants

A
  • Phenylephrine (Sudafed PE)
  • Pseudoephedrine (Sudafed) - can be converted to meth
  • Combination D products
  • alpha adrenergic agonists
  • Side effects of CV stimulation, CNS stimulation, dizziness, headache, anorexia
43
Q

Topical decongestants

A
  • Phenylephrine (Neo-Synephrine)
  • Naphazoline (Privine)
  • Tetrahydrozoline (Tyzine)
  • Use limited to less than 3 days to prevent rebound congestion
44
Q

Drugs in C. Difficile

A
  • Vancomycin
  • Metronidazole
  • Fidoxamicin
45
Q

Dihydrofolate Reductase Inhibitors

A
  • Trimethoprim
  • Pyrimethamine (Daraprim)
  • complexed to sulfonamides for sequential inhibition
  • Daraprim for toxoplasmosis
46
Q

Floroquinolones

A
  • Nalidixic Acid - unable to reach sufficient serum or tissue levels for systemic infections, used in minor UTI
  • Ciprofloxacin - urinary FQ
  • Ofloxacin - urinary FQ
  • Levofloxacin - respiratory FQ
  • Moxifloxacin - resistant pathogens
  • inhibit topoisomerase 2 and topoisomerase
  • good absorption but avoid cationic meds and such
  • renal excretion except Moxifloxacin
  • black box: tendons fucked, esp if old, renal failure, steroid use
  • QT interval prolonged
  • teratogenic
47
Q

Topical Antibiotics

A
  • Mupirocin - product of P. Flourescens, inactivated staphylococcal isoleucyl tRNA synthetase, big problems with resistance
  • Polymixin B - cationic detergent, disrupts lipid membrane, bind and inactivate endotoxin, gram neg only
  • Polymixin E - cationic detergent, disrupts lipid membrane, bind and inactivate endotoxin, gram neg only
  • Fidoxomicin - non absorbed macrolide, bonds sigma factor in c. Diff required for RNA polymerase binding to promoter
48
Q

First gen oral antihistamine

A
  • Diphenhydramine - Benadryl
  • Doxylamine - Unisom - OTC sleep aid
  • Hydroxyzine - Vistaril - pruritis aid
  • Promethazine - Phenergan
  • Meclizine - AntiVert - motion sickness and vertigo
  • MOA: Competitive H1 receptor antagonism
  • May cause Anticholinergic syndrome
  • Cross BBB and cause sedation
49
Q

2nd gen antihistamines

A
  • Cetrizine - Zyrtec, Zyrtec D
  • Fexofenadine - Allegra, Allegra D
  • Loratidine - Claritin, Claritin D
  • Desloratidine - Clarinex, Clarinex D
  • MOA: H1 receptor competitive antagonism
  • Do not cross BBB as much as 1st gen, safer for use in elderly
  • “D” products are combined with decongestant Pseudoephedrine
50
Q

Urinary antiseptic

A
  • Nitrofurantoin
  • absorbed from GI tract and immediately excreted into the urine
  • some MOA involving highly reactive intermediates
  • contraindicated in renal failure, can cause hemolytic anemia and neuropathy in G6PD deficiency
  • cumulative risk of irreversible pulmonary fibrosis (regular PFTs needed)
51
Q

Oxidative damage

A
  • Metronidazole
  • prodrug w active metabolites that cause oxidative damage
  • anaerobic or parasitic infections
  • accumulates in liver failure
  • disulfiram like rxn
  • first line for C. difficile colitis, giardiasis, entamoeba histolytica, trichomoniasis
  • cumulative neurotoxicity can manifest w seizures and peripheral neuropathy

Antibiotics (3 decks)

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