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A - USMLE Step 1 Pharm > Microbiology - Pharmacology > Flashcards

Microbiology - Pharmacology Flashcards

0
Q

Penicillin G and V - Mechanism + Clinical Use + Toxicity + Resistance

A

G = IV + IM vs. V = Oral
Mechanism - Bind transpeptidases + block the cross-linking of peptidoglycan - B-Lactam Antibiotic
Uses - Gram Positive (S. pneumoniae + actinomyces) + N. menigitidis + T pallidum - Bactericidal
Toxicity - Hypersensitivity Reactions + Hemolytic Anemia
Resistance - B-Lactamase cleaves the B-Lactam Ring (Primarily in Gram (-))

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1
Q

Cell Wall Antibiotics

A

Penicillins + Vancomycin + Bacitracin + Antipseudomonals + Cephalosporins + Carbapenems + Monobactams

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2
Q

Ampicillin + Amoxicillin Mechanism + Clinical Use + Toxicity + Resistance

A

Mechianism - Same inhibitor as penicillin + wider spectrum
Clinical Use - Haemophilus Influenzae + E. Coli + Listeria + Protus mirabilis + Salmonella + Shigella + Enterococci
Toxicity - Hypersensitivity Reaction + Rash + Colitis
Mechanism of Resistance - B-Lactamase (use clavulanic acid to protect the penicillin)

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3
Q

Naficillin - Mechanism + Clinical Use + Toxicity

A

Mechanism - B-Lactam penicillin
Clinical Use - Narrow (Staph except MRSA) –> Use naf for staph
Toxicity - Hypersensitivity + interstitial nephritis

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4
Q

B-Lactamase Inhibitors - Name + Mechanism

A

Inhibit B-Lactam and save penicillins

CAST - Clavulanic Acid + Sulbactam + Tazobactam –> E.g Amoxicillin + Clavulanic Acid = Augmentin

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5
Q

Cephalosporins - Mechanism + Organisms Not Covered + Toxicity

A

Mechanism - B-Lactam drugs that inhibit cell wall synthesis - Bactericidal - Broader specturm
Not Covered - LAME - Listeria + Atypicals (mycoplasma + chlamydia) + MRSA + Enterococci
Toxicity - Hypersensitivity Reactions + Vitamin K Deficiency + Gross reactivity with penicillins + nephrotoxicity + Hemolytic Anemia

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6
Q

1st Generation Cephalosporins - Name and Uses

A

Name - Cefazolin + Cephalexin

Uses - Gram Positive Cocci + Proteus Mirabilis + E Coli + Klebsiella pneumoniae - PEcK

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7
Q

2nd Generation Cephalosporins - Name and Uses

A

Names - Cefoxitin + Cefaclor + Cefuroxime
Uses - Gram Positive, + Haemophilus influenzae + Enterobacter aerogenes + Neisseria + Proteus Mirabilis + E. Coli + Klebsiella Pneumoniae + Serratia marcescens - HEN PEcKS

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8
Q

3rd Generation Cephalosporins - Names and Uses

A

Ceftriaxone - Meningitis + Gonorrhea
Ceftazidime - Pseudomonas
Used for serious resistant gram negative bacteria

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9
Q

4th Generation Cephalosporins - Names and Uses

A

Cefepime - Increased activity against pseudomonas and gram positive organisms - Good CNS Coverage

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10
Q

5th Generation Cephalosporins - Names and Uses

A

Ceftaroline - Broad Spectrum for Gram + and Gram - –> Covers MRSA but not Pseudomonas

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11
Q

Carbapenams - Mechanism + Clinical Use + Toxicity

A

Mechanism - B-Lactamase resistant B-Lactam with CNS Activity + IV Administration
Clinical Uses - Gram (+) Cocci + Gram (-) Rods + Anerobes - Wide spectrum but significant side effects (last resort option)
Toxicity - Gi Distrest + Skin Rash + CNS Toxicity (Seizures) + Renal Insufficiency makes it even worse

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12
Q

Monobacatam - Aztreonam Mechanism + Clinical Use + Toxicity

A

Mechanism - Prevents peptidoglycan cross=linking - Synergist with protein inhibitors + no cross reactivity with penicillin
Uses - Gram (-) Rods only (no Gram (+) impact)
Toxicity - Usually nontoxic - occasional GI symptoms

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13
Q

Vancomycin - Mechanism + Clinical Use + Toxicity + Resistance

A

Mechanism - Inhibits cell wall peptidoglcan formation by beinding the D-ala D=ala portion - Bactericidal
Uses - Gram Positive only (to large from Gram (-)) + Serious MDR organisms (e.g. C. diff + MRSA)
Toxicity - Well tolerated but NOT without problems –> Nephrotoxicity + Ototoxicity + Thrombophlebitis - Red Man Syndrome (diffuse flushing)
Resistance - Changes D-Ala + D-Ala to D-Ala + D-Lac - Can’t bind anymore

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14
Q

Protein Synthesis Inhibitors - Classes and Names

A

Buy AT 30 CCEL at 50
30S Inhibitors - Aminoglycosides + Tetracyclines
50S Inhibitors - Chloramphenicol + Clindamycin + Erythromycin + Linezolid
Aminoglycosides are the only bactericidal

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15
Q

Aminoglycosides - Drug Names + Mechanism + Clinical Use + Toxicity + Resistance

A

Mean (Amino) GNATS caNNOT kill anaerobes
Names - GNATS - Gentamicin + Neomycin + Amikacin + Tobramycin + Streptomycin (TB Treatment)
Mechanism - 30S Inhibitor - Bactericidal - Inhibit initiation complex + mRNA misreading + block translocation - Require O2
Use - Severe Gram (-) Rod infection - Synergistic with B-Lactams + Neomycin for bowel surgery
Toxicity - NNOT - Nephrotoxicity + Neuromuscular blockade + Ototoxicity + Teratogen —> Keep treatment to less than 5 days
Resistance - Bacterial enzymes inactive the drug

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16
Q

Tetracyclines - Names + Mechanism + Clinical Use + Toxicity + Resistance

A

Names - Tetracycline + Doxycycline + Minocycline +Tigecycline
Mechanism - 30S Inhibitor - Bacteriostatic - Stops Translation
Uses - Rickettsia (RMSF + Typhus) + Chlamydia + Borrelia bungdorferi + M. pneumonia –> Doxy is a second line drug for anthrax and malaria
Special - Doxy - Fecal elimination (okay in renal failure)
Toxicity - GI Disturbances + Photosensitivity - Also affects Ca deposits in teeth and bone growth (contraindicated in children and pregnancy)
Resistance - Increased efflux + decreased intake via bacterial pumps

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17
Q

Macrolides - Names + Mechanism + Clinical Use + Toxicity + Resistance

A

Names - Azithromycin + Clarithromycin + Erythromycin
Mechanism - 50S Inhibitor - Bacteriostatic - Inhibits translocation - Long Lasting (Days –> Z-Pack)
Uses - Atypical Pneumonia (Mycoplasma + Chlamydia + Legionella) + STDs + Gram (+) Cocci (For Otitis Media + Diphtheria + Pertussis)
Toxicity - MACRO - GI Motility + Arrhythmia (Long QT) + Cholestatic Hepatitis + Rash + eOsinophilia
Resistance - Methylation of the 23S rRNA binding site

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18
Q

Chloramphenicol - Mechanism + Clinical Use + Toxicity + Resistance

A

Mechanism - Blocks peptidyltransferased on 50S - Bacteriostatic
Use - Meningitis + RMSF
Toxicity - Anemia + Aplastic Anemia + Gray Baby Syndrome
Resistant - Plasmid enzyme that inactivates the drug

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19
Q

Clindamycin - Mechanism + Clinical Use + Toxicity

A

Mechanism - 50S Translocation Blocker - Bacteriostatic
Use - Anaerobic infections (bacteroides + clostridum perfringens) in lungs and aoral infections + Group A strep - Strong against Gram (+) but worthless against Gram (-) - Treats the anaerobes above the diaphragm vs. Metronidazole treats them below
Toxicity - Highly linked to C. diff and pseudomembranous colitis

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20
Q

Anti-Folate Drugs (2) - Names/Combo + Mechanism + Clinical Use + Toxicity

A

Sulfonamides + Trimethoprim - Almost always used together as TMP-SMX - Bacteriostatic alone but bactericidal together - Used together to avoid resistance
Mechanism - Anti-Folate (Sulfonamides compete with PABA and Trimethoprim inhibits Dihydrofolate reductase) - 2 Steps of same pathway
Use - Uncomplicated UTIs + Shigella + Salmonella + Pneumocystis jirovecii
Toxicity –> TMP –> Treats Marrow Poorly (Megaloblastic anemia + leukopenia)

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21
Q

Fluroquinolones (FQs) - Names + Mechanism + Clinical Use + Toxicity + Resistance

A

Names - Floxacins (E.g. Cirpofloxacin + Levofloaxcin)
Mechanism - Inhibit DNA Gyrase (Topo. II) and Topo IV - Bactericidal - Can’t be taken with antacids - Multiple Generations
Uses - Gram (-) Rods of the Urinary and GI Tracts (E.g. pseudomonas) + Neisseria
Toxicity - LGI Upset + Can damage growing cartilage - Counter indicated in children except those with CF (who get a lot of pseudomonas)
Resistance - Via Chromosome mutations of the DNA gyrase + Plasmid Efflux Pumps

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22
Q

Metronidazole - Mechanism + Clinical Use + Toxicity

A

Mechanism - Anti DNA - Forms free radicals that damage DNA - Bactericidal + Antiprotozoal
Uses –> GET GAP onto the Metro - Giardia + Entamoeba + Trichomonas + Gardnerella vaginalis + Anaerobes (C. Diff) + H. Pylori
Toxicity - Disulfiram reaction (severe flushing + hypotension + tachycardia) + metallic taste (Godzilla eats the metal metro train)

23
Q

Antimycobacterial Drugs - Names

A

RIPE for TB Treatment - Rifampin (RIF) + Isoniazid (INH) + Pyrazinamide (PZA) + Ethanbutol (EMB)

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Isoniazid (INH) - Mechanism + Clinical Use + Toxicity
Mechanism - Pro-drug activated by bacterial KatG to inhibit Mycolic acid synthesis and incorporation into the cell wall (via the FAS II enzyme) --> Leads to lysis Use - Mycobacterium tuberculosis - Only one used for prophylaxis Toxicity - INH - Injures Neurons and Hepatocytes - Pyridoxine (B6) helps reduce toxicity
25
Rimfampin (RIF) - Names + Mechanism + Clinical Use + Toxicity
Names - Rifampin + Rifabutin (less CYP450 involvement) 4 R's of RIF - 1) RNA polymerase inhibitor + 2) Ramps up P450 + 3) Red/Orange Body Fluids + 4) Rapid Resistance if used alone Mechanism - Inhibits RNA synthesis Use - MTB + Helps with Dapsone for leprosy + meningococcal prophylaxis + H. influenzae type B Toxicity - Hepatotoxicity + P450 + Orange/Red Body Fluids
26
Pyrazinamide (PZA) - Mechanism + Clinical Use + Toxicity
Mechanism - Structurally similar to INH - Pro-drug converted via PcnA enzyme - Inhibits the trans-translation (9saving of the ribosome during the inactive state) Use - Mtb (with RIF and INH) Toxicity - Hyperuricemia + Hepatotoxicity
27
Ethambutol (EMB) - Mechanism + Clinical Use + Toxicity
Mechanism - Targets arabinosyl transferases and blocks the formation of the arabinogalactan layer of the Mtb cell wall --> Easier for the immune system to attack the Mtb Use - Mtb Toxicity - Optic neuropathy (Red/Green Colorblindness) - No Children
28
Anti-Fungals - Classes and Names
Cell Membrane Inhibitors (Ergosterol) - Amphotericin B + Azoles + Nystatin Nucleic Acid/DNA Inhibitors - Flucytosine Cell Wall Inhibitor - Echinocandins
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Amphotericin B - Mechanism + Clinical Use + Toxicity
Mechanism - Ampipathic ring that binds ergosterol and forms membrane pores allowing electrolyte leakage and fungal cell death Uses - Broad Spectrum - Drug of choice for serious systemic mycoses (but no CSF access) - Use liposomal preparations to improve packaging + reduce nephrotoxicity Toxicity - Must avoid chronic use - Fever/chills/vomiting + nephrotoxicity + anemia + liver function impairment + IV phlebitis
30
Nystatin - Mechanism + Clinical Use
Mechanism - Same as Amphotericin B - Topical form becasue it is too toxic Use - Oral thrush + diaper rash + vaginal candidiasis
31
Flucytosine - Mechanism + Clinical Use + Toxicity
Mechanism - Converts to 5-FU and inhibits DNA/RNA synthesis Use - Limited spectrum - Primarily meningitis from Cryptococcus (has CSF access) Toxicity - Bone marrow suppression
32
Anti-Fungal - Azoles - Classes + Mechanism + Clinical Use + Toxicity
1st Generation = Imidazole + 2nd Generation = Triazole Mechanism - Inhibits ERG1 protein for ergosterol synthesis - no membrane building + toxic intermediate build-up Use - Miconazole + Clotrimazole are used topically (1st Generation) + Itraconazole (Wide Spectrum but no CSF access) + Fluconazole (chronic suppression of cryptococcus in AIDs patients due to CSF access + long half life) (2nd Generation) Toxicity - Liver disfunction + teratogenic
33
Echinocandins - Name + Mechanism + Clinical Use + Toxicity
Name - All end in Fungin - Caspofungin + Micafungin Mechanism - Inhibits B-Glucan cell wall synthesis - newest class Use - Asperilla + candida Toxicity - GI issues + flushing due to histamine release
34
Terbinafine - Mechanism + Clinical Use + Toxicity
Mechanism - Anti-fungal - inhibits ezymes for ergasterol biosynthesis (ERG1) - Toxic intermediate build up + membrane failure Use - Skin and nail fungal infections Toxicity - GI + hepatotoxicity + bad tase
35
Enfuviritide - Mechanism + Clinical Use + Toxicity + Resistance
Mechanism - Anti HIV Fusion Inhibitor - Binds gp41 - Prevents viral entrance into the CD4 Cell Clinical Use - Anti HIV - 2x Daily Injections Toxicity - Skin Reactions (At injection site) + $$ Resistance - Mutation in gp41
36
Maraviroc - Mechanism + Clinical Use + Toxicity
Mechanism - Anti HIV Fusion inhibitor - Binds human CCR5 preventing co-receptor activation Clinical Use - Anti HIV - 2x oral dosage - Only effective against CCR5 strands Toxicity - P450 Drug Interactions
37
NRTIs - Class + Function + Examples + Toxicity
Nucleotide Reverse Transcriptase Inhibitors - Nucleosides for chain termination prevention in viral replication Prodrugs that must be phosphorylated by cytoplasmic enzymes Examples - Emtricitabine + Tenofovir Toxicity - Can impact Mito. DNA polymerase - Lactic acidosis + muscle weakness
38
Tenofovir - Mechanism + Clinical Use + Toxicity
Mechanism - NRTIs - Tenofovir already has the first phosphate hidden for fast activation Clinical Use - Anti HIV - Combined with Emtricitabine (NRTI) to form Truvada Toxicity - Minimal - Some P450 interaction but overall very low
39
NNRTIs - Class + Function + Examples + Toxicity
Non-nucleoside reverse transcriptase inhibitors - bind different site of RT then NRTIs - Not pro-drugs (no need to phosphorylate) Examples - Etravirine Toxicity - P450 interaction + raised lived enzymes + rash + counter indicated in pregnancy
40
Etravirine - Mechanism + Clinical Use + Toxicity
Mechanism - NNRTI - Highly effective + escapes resistance Clinical Use - Saved for HIV patients who fail the first line therapy Toxicity - P450 interactions
41
Raltegravir - Class + Mechanism + Clinical Use + Toxicity + Resistance
Class - HIV Integrase inhibitor - Prevents integrase from incorpoating the viral DNA into host DNA Mechanism - Inhibits strand transfer (LTR and U3/U5 addition) Clinical Use - Anti-HIV (No P450 interaction) Toxicity - Hypercholesterolemia Resistance - Integrase Mutations
42
Elvitegravir - NOT BOARDS - Mechanism + Clinical Use
Mechanism - Anti-HIV Integrase Inhibitor Use - Used with Cobicstat which has no intrinsic anti HIV effect but increases the half life of elvitegravir (but Cobicstat has P450)
43
Ritonavir - Class/Others + Mechanism + Clinical Use + Toxicity
Protease Inhibitor - all end in navir - Darunaiv + Atazanavir Mechanism - Inhibit HIV protease from the pol gene so it can't cleave the products of HIV mRNA Clinical Use - Combination therapy for HIV Toxicity - Changes in body fat distribution + hyperlipidemia + GI intolerance + hyperglycemia (diabetic control issues)
44
Tipranavir - Mechanism + Clinical Use + Toxicity
Mechanism - HIV Protease Inhibitor Clinical Use - Last line HIV therapy after resistance to all otehrs Toxicity - Liver Function
45
Acyclovir - Mechanism + Clinical Use + Toxicity + Resistance
Mechanism - Chain terminating nucleoside analog for DNA viruses - Pro drug is phosphorylated by viral thymidine kinase Clinical Use - Oral + Topical for HSV + VZV - Herpes Toxicity - Small renal issues - generally well tolerated Resistance - Mutated viral thymidine kinase
46
Cidofovir - Mechanism + Clinical Use + Toxicity + Resistance
Mechanism - Chain terminating nucleoside analog (with a phosphate) Clinical Use - CMV + Acyclovir resistant HSV Toxicity - Nephrotoxicity - Give with Probenecid to reduce the nephrotoxicity Resistance - mutation in DNA polymerase
47
Granciclovir - Mechanism + Clinical Use + Toxicity
Mechanism - Chain terminating nuceloside analog Clinical Use - Not much - Immunocompermised patients (CMV) Toxicity - Lots - Mutagenic + Carcinogenic + Teratogenic
48
Foscarnet - Mechanism + Clinical Use + Toxicity + Resistance
Mechanism - Blocks viral DNA polymerase + RNA polymerase Clinical Use - CMV when ganciclovir and cidofovir fail + acyclovir resistant HSV Toxicity - Nephrotoxicity Resistance - Mutated DNA Polymerase
49
Amantadine + Rimantadine NOT BOARDS - Mechanism + Clinical Use + Toxicity + Resistance
Mechanism - Block the M2 pump preventing RNA virus (influenza) from leaving the capsid and entering the cytoplasm - Prevent unsheathing Clinical Use - None - Virus is resistant Toxicity - None Resistance- M2 Mutation
50
Zanamivir + Oseltamivir - Mechanism + Clinical Use + Toxicity + Resistance
Mechanism - Prevent RNA virus (influenza) budding - prevent neuramididase from cleaving the sialic acid residues after the virus infects - upon release the virus rebinds the sialic acids on the original host cell Oseltamivir = Tamiflu Clinical Use - Influenza A + B - Zanamivir = Inhaler Toxicity - Minimal GI complaints
51
Interferons - Mechanism + Clinical Use + Toxicity + Resistance
Mechanism - Mimic normally produced human antiviral IFN Clinical Use - Alpha (HBV + HCV + Kaposi Sarcoma) + Beta (MS) + Gamma (CGD) Toxicity - Neuropenia + Myopathy PEG - Added to increase half life
52
Ribavirin (RBV) - Mechanism + Clinical Use + Toxicity
Mechanism - Multiple viral targets via reduced guanosine Clinical Use - Combo therapy with PEG-IFN for HCV Toxicity - Hemolytic Anemia + Teratogen + Psychiatric Affects
53
Telaprevir + Simeprevir (NOT BOARDS) - Mechanism
Mechanism - HCV Protease Inhibitor - significant success rate with PEG-IFN + RBV
54
Sofobuvir - (NOT ON BOARDS) Mechanism + Clinical Use + Toxicity
Mechanism - HCV Chain Terminator - Nucleoside pro-drug like tenofovir Clinical Use - Sometimes with PEG-IFN + RBV ...... Sometimes with just RBV (only oral stand alone treatment) - Once daily pill with high impact on SVR Toxicity - Limited

A - USMLE Step 1 Pharm (11 decks)

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