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Exam 5 Flashcards

0
Q

Penicillin V

A

Natural penicillin
Like G, but acid stable
Narrow spec, Gm+, destroyed by beta-lactamase
Given orally, absorption is unstable

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1
Q

Penicillin G

A

Natural penicillin
Narrow spec, mostly Gm+
Destroyed by beta-lactamase
Given IV/IM w/ procaine, hydrolized in stomach acid

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2
Q 
Naficillin
Oxacillin
Cloxacillin
Dicloxacillin
Methicillin
A 
Beta-lactamase resistant penicillins
Narrow spec
Naficillin- Not AFfected by beta-lactamase
Ox- resistant to change
Methicillin- not used, toxic MRSA
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3
Q 
Amoxicillin
Ampicillin
Ticarcillin
Piperacillin
Mezlocillin
Carbenicillin
A

Broad/extended spec penicillins
None are penicillinase resistant!
Ampicillin- causes rash in px with mononucleosis

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4
Q

Sublactam

Clavulanic acid

A

Non-antibiotic beta-lactam ring compounds
Inhibit penicillinase
Usually given in combo with broad spec penicillins to occupy penicillinase

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5
Q

Cephalosporins

Ceph- or cef-

A

Broader spec
Greater resistance to beta-lactamases
Each generation has more Gm- activity & greater resistance than previous
SE: some allergic rxn in penicillin-sensitive px
Possibility of superinfxn

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6
Q

Imipenem

A 
Carbapenem (penicillin analog)
Very broad spec
Given IV
Better vs Gm+
Metabolized in kidney to nephrotoxin, given with cilastatin to inh that enzyme
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7
Q

Meropenem

A 
Carbapenem (penicillin analog)
Resistant to beta-lactamase
Very broad spec
Given IV, enters CNS more readily
More effective against Gm-
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8
Q

Aztreonam

A 
Monobactam
IV/IM
Not affected by beta-lactamases
Only useful with aerobic Gm- (E. coli)
Not x-reactive with penicillin allergic px
SE: seizures
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9
Q

Vancomycin

A

Binds to dialanine residues on subunits of cell walls
Prevents x-linking
Used vs Gm+ staph infxn
IV, except for pseudomembranous colitis (given oral, pseudotopical)
SE: nephrotoxic
Ototoxic
Rapid IV -> causes histamine release (redman/redneck syndrome)
Resistance (dialanine substituted by lactic acid)

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10
Q

Televancin

Dalbavancin

A 
Lipoglycopeptides
Act both like vancomycin and cell membrane distruptors
SE: renal damage
       Fetal damage
       Metallic taste in mouth
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11
Q

Bacitracin

A

Inh recycling of bactoprenol carrier
Used vs Gm+ cells
Only given topically, extremely nephrotoxic

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12
Q

Fosfomycin

A

Blocks synth of n-acetylmuramic acid
Used vs Gm- (E. coli)
For uncomplicated UTI

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13
Q

Cycloserine

A

Inh incorporation of alanine into n-acetylmuramic acid
Used vs Mycobacterium TB
SE: sedation, tremor, psychosis

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14
Q

Erythromycin

A 
Macrolide
Reversible binds to 50s subunit
Inhibits translocation of mRNA
Inhibits binding of tRNA to P site of ribosome 
SE: GI upset
      Strong inh of P450
      Liver damage, cardiac arrhythmias
Used vs Gm+
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15
Q

Clarithromycin
Azithromycin
Telithromycin

A

Macrolides
Inhibit bacterial protein synth by inhibiting an enzyme
C- oral stability, H. pylori
Az- T1/2 of 3 days
T- induces less resistance, readily transported out of cell
SE: inh P450
Severe hepatotoxicity
Worsening MG
Block cholinergic receptors in mm (atropine)

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16
Q

Streptomycin

A 
Aminoglycoside
Irreversibly binds to 30S subunit
Can inh tRNA binding all along mRNA 
Including initiation site
Irreversible in mRNA, given IM
SE: very ototoxic
       very nephrotoxic (most common cause of drug-related nephrotox)
       High doses --> decrease ACh and ACh receptors
       Preg cat D
Targets aerobic Gm-
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17
Q 
Gentamycin
Tobramycin
Neomycin
Amikacin
Kanamycin
Netilmicin
A

Aminoglycosides
Inhibit bacterial protein synth by inhibiting an enzyme
Neomycin- VERY nephrotoxic, used topically or orally

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18
Q

Tetracycline

A

Reversible binds to 30S subunit (static!)
Inh binding of tRNA to A site
SE: binds to cations Ca++, Fe++, Al+++
Deposited in bones & teeth of fetus (Preg Cat D)
Degrades with time into renal/hepatotoxin
Targets: rickettsia, spriochetes, helicobacter, legionella

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19
Q

Doxycycline
Minocycline
Tigecycline

A

Tetracyclines
Inh binding of tRNA to A site by binding to 30S subunit
Degrades into renal/hepatotoxin
Less likely to bind to Ca++

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20
Q

Chloramphenicol

A 
Inhibits peptidyl transferase
SE: inh P450
       aplastic anemia
       Grey Baby Syndrome
        metab by Phase II enz, not active in newborn, vasomotor collapse
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21
Q

Clindamycin

Lincomycin

A

Lincosamides
Like erythromycin, inh translocation in ribosome
SE: severe superinfxn with C. difficile
Target: severe anaerobic infxns (penetrating gut wound)
Dental prophy with heart valve

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22
Q

Quinupristin + dalfopristin

A 
Always used together
Q- inh A & P sites
D- inh P site
SE: mm pain
Target: Gm+
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23
Q

Linezolid

A

Inh binding of methionyl tRNA to P site
Prevents initiation of synth process
SE: anemia, pseudomembranous colitis (like all strong antibiotics)

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24
Daptomycin
``` Lipopeptide Disrupts bacterial cell membranes Forms pores in cell membrane SE: mm pain/weakness Eosinophilic pneumonia Targets: aerobic Gm+ (staph/strep skin infxn) ```
25
Fidaxomycin
Inhibits C. difficile RNA polymerase | Given orally, not systemically absorbed
26
Ciprofloxacin | Other -floxacins
Inhibit topoisomerase II/IV No effect on mammalian topoisomerase SE: may damage developing cartilage (no kids or prego) Tendonitis, Achilles' tendon rupture Phototoxicity Worsen MG Target: broad spec acid fast & Gm+/-
27
Sulfonamides
``` Reversible inh dihydropterate synthetase SE: Stevens Johnson Syndrome Hemolytic anemia in G6PDH deficient px Megaloblastic anemia Target: UTI ```
28
Trimethoprim
Inh bacterial dihydrofolate reductase Like methotrexate for bacteria Used in conjunction with sulfamethoxazole SE: megaloblastic anemia (avoided w leucovorin) Target: Gm- bacteria UTIs, concentrates in acidic prostate/vaginal tissue
29
Metronidazole
Prodrug- activated to free radical maker by obligate anaerobes IV for severe anaerobic infxns IV for protozoal infxns (trichomonas, giardiasis) SE: seizures, peripheral neuropathy
30
Nitrofurantoin
Reduced by bacteria to highly active molecule UTI SE: cough, chest pain, brown urine
31
Polymixin B
Binds to (-) charged side of LPS of Gm- bacteria Increases membrane permeability Topical SE: nephrotoxic neurotoxic Reversible neuromuscular blocker (ataxia, perioral paresthesia)
32
Gramicidin
Mix of 3 peptide antibiotics Forms pores in Gm+ bacteria SE: systemic toxicity
33
Neomycin
Aminoglycoside | Topical only
34
Retapamulin
Inh peptidyl transferase | Topical Tx of skin staph/strep infxn
35
Mupirocin
Inhibits bacterial isoleucyl tRNA synthesis For staph infxns Very specific target
36
Isoniazid
``` Antimycobacterial enzyme inhibitor Prodrug, produces inhibitor of multiple mycobac. enzymes Inhibits cell wall synthesis Used for prophy Metabolized by acetylation SE: increased excretion of vit B6 (leads to pellegra) Peripheral neuropathy Optic neuritis Hepatotoxic ```
37
Rifampin
``` Antimycobacterial enzyme inh Inh DNA-dependent RNA polymerase SE: hepatotox Red color in all body fluids Strongly induces P450 (little surprise story) ```
38
Pyrazinamide
Prodrug- converts in macrophages where TB lives Inh fatty acid synth by TB SE: gout, hepatitis
39
Ethambutol
Inh arabinosyl transferase Necessary for cell wall synth SE: optic neuritis Impaired R/G discrimination
40
Bedaquiline
Inh mycobacterial ATP synthetase SE: arrhythmias, death Always used with at least 3 other anti TB drugs
41
Dapsone
Related to sulfonamides | For mycobacterium leprae (Leprosy)
42
Nystatin
Topical polyene antifungal for skin infxn Bind to ergosterol in cell membranes and forms pores Can be given pseudoorally (topical in gut)
43
Natamycin
Topical polyene antifungal for skin infxn | Only antifungal approved for use in eye
44
Tolnaftate Ciclopirox Terbinafine Other -fines
Topical antifungals for ringworm | Terbinafine - liver damage
45
Griseofulvin
Systemic antifungal for nail fungal infxn Taken up by growing skin cells, concentrated in keratin Binds to fungal microtubules, inhibits mitosis SE: headache Induces P450 Allergic rxn (derived from penicillium mold)
46
Terbinafine
``` Inhibits ergosterol synthesis Inh squalene epoxidase (enzyme) Decrease in ergosterol synth (malformed membrane) Increase in squalene buildup (toxic) Metabolized by & inh P450 ```
47
Amphotericin B
``` Systemic polyene antifungal DOC for systemic fungal infxn Binds to ergosterol and forms pores in cell membrane Treat for 2-4 mo. IV or intrathecal SE: "amphoterrible B" Impaired renal fxn >80% Fever, chills, vomiting Convulsions, severe headaches Anemia ```
48
Imidazole Miconazole Ketoconazole
Inh fungal CYP450, including ionosterol 14-alpha demethylase Inhibits ergosterol synthesis Used topical vs candida and ringworm SE: nausea, GI Hepatotoxic Inh of human P450 Decreased adrenal/gonadal steroid synth
49
Fluconazole
Triazole derivative conazoles Fungistatic Lowest effect on human P450 SE: teratogenic, hallucinations, hepatotox
50
Itraconazole
Fungistatic triazole deriv for systemic fungal infxn Strongest effect on man P450 Worsens CHF and arrhythmias
51
Posaconazole | Voriconazole
Fungistatic triazole derivs Inhibit fungal P450 V-can cause visual disturbances
52
Flucytosine
``` Antifungal pyramidine analog Inh thymidine synthelase Prodrug, doesn't enter mammalian cells as readily Converted to 5-flurorouracil in fungi SE: used in combo with ampho B GI upset Bone marrow depression Hepatotoxic ```
53
Caspofungin Micafungin Anidulafungin
Fungicidal Inh synth of fungal cell wall component Given slow IV over 91 hours SE: rash, fetal damage
54
Acyclovir
Herpes simplex and zoster Prodrug, inh viral DNA polymerase Must be phosphorylated by a viral kinase Active form incorporates into viral DNA Higher affinity for viral DNA polymerase than human SE: GI upset, renal damage, delirium when given IV
55
Valacyclovir
Prodrug, converts into acyclovir after first pass metabolism Given orally Inhibits viral DNA polymerase
56
Famciclovir
Prodrug, herpes Converted by first pass into acyclovir analog Inhibits viral DNA polymerase
57
Ganciclovir
CMV Prodrug, activated by viral kinase Inh viral DNA polymerase SE: neutropenia, thrombocytopenia, teratogenic
58
Valganciclovir
CMV Converted into ganciclovir by first pass Inh viral DNA polymerase
59
Cidofovir
CMV Prodrug, converted by HOST kinase Only used when virus changed its viral kinase SE: nephrotoxic
60
Foscarnet
CMV Not a prodrug, directly inh viral DNA polymerase Given IV 3x/daily SE: Renal damage
61
``` Lamivudine Adefovir Telbivudine Tenofovir Entecavir ```
Inh Hep B reverse transcriptase LATTE Ade- SE: liver, renal damage TTE- SE: lactic acidosis, hepatomegaly
62
Ribavirin
``` For RSV, not used often Phosphorylated in cell Inhibits RNA-dependent DNA polymerase SE: $1000/day Preg Cat X Hemolytic anemia Deceased pulmonary fxn in infants & cardiac arrest ```
63
Palivizumab
``` RSV Humanized immune system MAB Blocks fusion of virus to target cell by blocking antigen site on RSV Blocks a receptor Used only prophylactically ```
64
Amantadine | Rimantidine
Influenza A Widespread resistance Blocks transporter/ion channel Prevents H+ channels from forming in endosomes SE: renal failure Teratogenic CNS --> dizziness, slurred speech, confusion, nausea
65
Zanamivir | Oseltamivir
``` Influenza A & B Neuraminidase inhibitor Prevents virus from budding off host cell SE: nausea, diarrhea Psychosis, hallucinations ```
66
Recombinant interferon alpha
``` Hep C Cytokines, multiple mechanisms Enhances normal immune cell fxn Inh mRNA processing SE: fatigue flu-like symptoms depression hypertension retinopathy myelosuppression ```
67
Boceprevir Telaprevir Simeprevir
Hep C protease inhibitors | Used in combo with interferon alpha
68
Sofosbuvir
Prodrug Inh Hep C RNA-dependent RNA polymerase Ledipasvir + sofosbuvir = binds protein for HCV replic.
69
``` Didanosine Abacavir Zidovudine Lamivudine Emtricitabine Stavudine Telbivudine ```
Nucleoside analog Reverse Transcriptase Inhibitor DAZ LES-T Phosphorylated in cell, bind to reverse transcriptase SE: life threatening hepatomegaly & lactic acidosis myopathy, anemias, pancreatitis, neuropathies
70
Nevirapine
NNRTI 1st gen Binds to nonactive on RT hepatotoxicity, S-J syndrome
71
Delaviridine
NNRTI 1st gen Hepatotoxic P450 inhibitor
72
Efavirenz
NNRTI 1st gen CNS tox (hallucinations, memory loss) Rash Street drug
73
Etravirine | Rilpivirine
NNRTI 2nd gen | Higher potency, longer T1/2, less SEs
74
``` Saquinavir Ritonavir Indinavir Nelfinavir Atazanavir Darunavir ```
Protease inhibitors -navirs Prevent formation of active viral proteins from peptide precursors Ritonavir- most potent P450 inhibitor SE: altered fat distribution (skinny limbs face, fat gut chest back) increased diabetes
75
Tipranavir | Fosamprenavir
Protease inhibitors -navirs | Contain sulfur molecule, allergy possible
76
Enfuvirtide
Fusion inhibitor Binds to target binding site on virus SE: insomnia
77
Maraviroc
Fusion inhibitor Binds to binding site on Macrophage SE: hepatotox, allergic rxn, increase risk of MI
78
Reltegravir Dolutegravir Elvitegravir
Integrase inhibitor Inh HIV-1 integrase -tegravirs

Pharm Drug Flashcards (4 decks)

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