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144 Cards in this Set

  • Front
  • Back
Mechanism of action of Penicillins
B-lactam antibiotics

Bind penicillin binding proteins to block transpeptidase cross-linking of cell wall
Penicillin
Prototype B-lactam antiobiotic
Methicillin
B-lactam antibiotic

Penicillinase-resistant penicillin b/c bulky R group
Naficillin
B-lactam antibiotic

Penicillinase-resistant penicillin b/c bulky R group
Dicloxicillin
B-lactam antibiotic

Penicillinase-resistant penicillin b/c bulky R group
Ampicillin
B-lactam antibiotic

Wider spectrum than penicillin
Amoxicillin
B-lactam antibiotic

Wider spectrum than penicillin
Ticarcillin
B-lactam antibiotic

Antipseudomonal
Carbenicillin
B-lactam antibiotic

Antipseudomonal
Piperacillin
B-lactam antibiotic

Antipseudomonal
Mechanism of penicillinases (B-lactamases)
Cleave B-lactam ring and inactivate drug, leading to resistance
Clavulonic Acid
Prevents destruction of B-lactam antiobiotics sensitive to penicillinase (B-lactamase)
Mechanism of action of Cephalosporins
B-lactam antibiotics

Block transpeptidase cross-linking of cell wall
Cefazolin
1st generation cephalosporin

B-lactam antibiotic

Less susceptable to penicillinases
Cephalexin
1st generation cephalosporin

B-lactam antibiotic

Less susceptable to penicillinases
Cefoxitin
2nd generation cephalosporin

B-lactam antibiotic

Less susceptible to penicillinases than penicillin
Cefaclor
2nd generation cephalosporin

B-lactam antibiotic

Less susceptible to penicillinases than penicillin
Cefuroxime
2nd generation cephalosporin

B-lactam antibiotic

Less susceptible to penicillinases than penicillin
Ceftriaxone
3rd generation cephalosporin

B-lactam antibiotic

Less susceptible to penicillinases than penicillin

Treats gonorrhea
Cefotaxime
3rd generation cephalosporin

B-lactam antibiotic

Less susceptible to penicillinases than penicillin
Cefazidime
3rd generation cephalosporin

B-lactam antibiotic

Less susceptible to penicillinases than penicillin

Treats pseudomonas
Cefepime
4th generation cephalosporin

B-lactam antibiotic

Less susceptible to penicillinases than penicillin

Treats pseudomonas
Cephalosporins with a methylthiotetraxole group (cefamandole) have this toxicity
Disulfram-like reaction w/ethanol
1st Generation Cephalosporins treat
Gram +

Proteus

E. coli

Klebsiella
2nd Generation Cephalosporins treat
Gram + (but less than 1st gen)

H. influenzae

Enterobacter aerogenes

Neisseria

Proteus

E. coli

Klebsiella
3rd Generation Cephalosporins treat
Serious gram negative infections

Meningitis (penetrate BBB)
Aztreonam is used for
B-lactam antibiotic

Resistant to B-lactamases

Treats Grm - only

No cross allerginicity with penicillins or cephalosporins
Cephalosporins sometimes have cross allerginicity with
Penicillins
Mechanism of B-lactam antibiotics
Inhibit transpeptidase cross linking of cell-wall, thus inhibiting cell-wall formation
Imipenem type, uses, toxicities
Carbapenem

B-lactam antibiotic

B-lactamase resistant

Broad-spectrum but many toxicities

Toxicities include seizures, GI distress, rash

Always administer with cilastatin to block renal metabolism (prevents inactivation in renal tubules)
Meropenem
Carbapenem

B-lactam antibiotic

B-lactamase resistant

Broad-spectrum but many toxicities

Toxicities include seizures, GI distress, rash
Vancomycin
Prevents polymerization of peptidoglycans by binding D-ala D-ala portion of cell wall precursors

Used for MRSA and C. diff

Toxicities include red man syndrome (diffuse flushing), nephrotoxic, ototoxic, thrombophlebitis, but well tolerated in general
Mechanism of action of Aminoglycosides
Bind to 30S

Inhibit formation of initiation complex and cause misreading of mRNA

Requires O2 for uptake and is ineffective against anaerobes
This class of drugs requires O2 for uptake and is ineffective against anaerobes
Aminoglycosides
Gentamicin
Aminoglycoside
Neomicin
Aminoglycoside
Amikacin
Aminoglycoside
Tobramycin
Aminoglycoside
-mycin or -micin or -cin

(BUT NOT -thromycin, clindamycin, or vancomycin)
Aminoglycosides

(-thromycin is Macrolides)
This class of drug is synergistic with B-lactam antibiotics
Aminoglycosides

B-lactam breaks cell wall and allows aminoglycosides inside

Especially useful for enterococci
Resistance to vancomycin occurs by
D-ala D-ala is replaced by D-ala D-lac, so vancomycin can't bind

Common in enterococci
Toxicities of Aminoglycosides
Nephrotoxic (especially if used with cephalosporins), Ototoxic (especially if used with loop diuretics), Teratogen
Mechanism of action of tetracyclines
Binds 30S

Prevents attachment of tRNA

Bacteriostatic
Doxycyclin CAN be used in patients with
Renal failure (b/c fecally eliminated)
Milk, antacids, divalent cations inhibit the absorption of this antibiotic in the gut
Doxycyclin
Uses of tetracyclines
V. cholerae, Acne, Chlamydia, Ureaplasma urealyticum, Mycoplasma pneumoniae, Tularemia, H. pylori, Borrelia burgdorfery, Rickettsia

Gets intracellular organisms
Toxicities of tetracyclines
Discolored teeth, inhibited bone growth in children

Photosensitivity

GI distress

Contraindicated in pregnancy
Tetracyclin
Tetracyclin

Treats acne
Doxycyclin
Tetracyclin

Absorbed in gut, can be used in renal failure

Milk, antacids, iron, divalent cations prevent absorption
Demeclocycline
Tetracyclin

ADH antagonist used in SIADH as a diuretic
Minocycline
Tetracyclin
-cyclin or -cycline
Tetracyclines
Mechanism of action of macrolides
Binds 50S (23S part)

Blocks translocation in protein synthesis
Erythromycin
Macrolide
Azithromycin
Macrolide
Clarithromycin
Macrolide
-thromycin
Macrolides
Uses of macrolides
URIs

STDs

Community acquired pneumonias (mycoplasma, legionella, chlamydia, neisseria)

Steptoccocal infections in those allergic to penicillin
Can be used in streptococcal infections in those allergic to penicillin
Macrolides (Erythromycin)
Toxicity includes increased serum concentration of theophyllines, oral anticoagulants
Macrolides
Toxicities of Macrolides
GI discomfort (most common cause of noncompliance)

Acute cholestatic hepatitis

Eosinophilia

Rash

Increased serum concentration of theophyllines, oral anticoagulants
Chloramphenicol
Binds 50S

Inhibits 50S peptidyltransferase activity, inhibiting transpeptidation of protein synthesis

Toxicities include aplastic anemia, gray baby syndrome (b/c lack liver UDP-glucuronyl transferase and can't metabolize drug)
Antibiotic that can cause aplastic anemia (pancytopenia) and gray baby syndrome
Chloramphenicol
Clindamycin
Binds 50S

Blocks peptide bond formation

Treats anaerobic infections above the diaphragm

Toxicity is pseudomembranous colitis
Toxicity is pseudomembranous colitis
Clindamycin

Also possibly ampicillin
Mechanism of action of sulfonamides
PABA antimetabolites that inhibit dihydropteroate synthetase

Blocks folate synthesis
Sulfamethoxazole (SMX)
Sulfonamide
Sulfisoxazole
Sulfonamide
Triple Sulfas
Sulfonamide
Sulfadiazine
Sulfonamide
Sulf-
Sulfonamides
Class of antibiotics that causes hemolysis in G6PD deficient patients
Sulfonamides
Toxicities of sulfonamides
Hypersensitivity

Hemolysis if G6PD deficient

Nephrotoxic

Kernicterus in infants

Displacement of drugs from albumin (ex. warfarin)
Trimethoprim (TMP) mechanism of action
Inhibits bacterial dihydrofolate reductase

Blocks folate synthesis
Pyrimethamine mechanism of action
Inhibits bacterial dihydrofolate reducatase

Blocks folate synthesis
Mechanism of action of fluoroquinolones
Inhibit DNA gyrase (topoisomerase II)
TPM-SMX uses
(Trimethoprim-Sulfamethoxazole)

Recurrent UTIs

Shigella

Salmonella

PCP (Pneumocystic jiroveci) pneumonia
Megaloblastic anemia, leukopenia, granulocytopenia are toxicities of which antibiotic
Trimethoprim
Cannot take this class of drugs with antacids
Fluoroquinolones
Sulfa drugs (for those with sulfa drug allergies) include
Sulfonamides, sulfasalazine, sulfonylureas, thiazide diuretics, acetazolamide, furosemide
Metronidazole mechanism of action
Forms toxic metabolites in the cell wall that damage DNA
Side effects of fluoroquinolones
Damage to cartilage in fetus and children

Tendonitis and tendon rupture in adults

Leg cramps and myalgias in kids

Inhibits GABA --> seizures

GI upset, superinfections, skin rash, headache, dizziness
This type of antibiotic/antiprotozoal produces a disulfram-like type of reaction with alcohol and gives you a metallic taste in your mouth
Metronidazole
Used for anaerobic infections below the diagphragm
Metronidazole
Used for anaerobic infections above the diaphragm
Clindamycin
Mechanism of action of polymixins
Binds cell membrane of bacteria and disrupts osmotic properties

Acts like detergents (cationic, basic)
Toxicities of polymixins
Neurotoxic

ATN
TB prophylaxis
Isoniazid (INH)
TB treatment
Isoniazid (INH), Rifampin, Ethambutol, Pyrazinamide

Also streptomycin?
M. avium-intracellulare prophylaxis
Azithromycin
M. avium-intracellulare treatment
Azithromycin, rifampin, ethambutol, streptomycin
M. leprae treatment
Dapsone, rifampin, elofazimine
This drug used to treat TB can kill TB protected in macrophages because it requires an acidic environment to work
Pyrazinamide
Optic neuropathy (red-green color blindness) is a side effect of this drug used to treat TB
Ethambutol
Mechanism of action of Isoniazid (INH)
Decreases synthesis of mycolic acids (part of mycobacterial cell wall) by inhibiting KatG enzyme
This drug used to treat TB is hepatotoxic, neurotoxic, has SLE-like syndrome, and causes hemolysis if G6PD deficient
INH (Isoniazid)
This drug used to treat TB has different half-lives if slow-vs-fast acetylators
INH (Isoniazid)
Giving vitamin B6 can prevent neurotoxicity associated with this drug used to treat TB
INH (Isoniazid)
Mechanism of action of Rifampin
Inhibits DNA-dependent RNA polymerase, suppressing initiation of RNA chain synthesis
This drug used to treat TB causes orange body fluids
Rifampin
This drug delays resistance for dapsone when used for leprosy
Rifampin
This drug can be used for meningococcal propylaxis and chemoprophylaxis in contacts of children with H. influenzae type B
Rifampin
Treat MRSA with
Vancomycin
Treat VRE with
Linezolid and streptogramins (quinupristin/dalfopristin)
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Mechanism of Amantadine
Blocks viral uncoating (M2 protein) in host cell

Influenza A only

Also causes the release of dopamine from intact nerve terminals
Antiviral that can be used to treat Parkinsons
Amantidine
Amantadine toxicities
Ataxia, dizziness, slurred speech
Mechanism of resistance to Amantidine
Mutated M2 protein

90% of influenza A strains are resistant, so not used anymore
Why is rimantidine safer for the elderly than amantadine
Fewer CNS side effects because does not cross BBB
Zanamivir mechanism of action
Inhibits influenza neuraminidase, which prevents cleavage of progeny virus from surface

Influenza A and B
Oseltamivir mechanism of action
Inhibits influenza neuraminidase, which prevents cleavage of progeny virus from surface

Influenza A and B
-mivir drugs work by
Inhibits influenza neuraminidase, which prevents cleavage of progeny virus from surface

Influenza A and B
Ribavirin mechanism of action, use, toxicities
Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase

Used for RSV, Hep C

Toxicities include: Hemolytic Anemia, Severe Teratogen
Acyclovir mechanism, use

-cyclovir (NOT Ganciclovir)
Guanine nucleotide analog

Monophosphorylated by viral thymadine kinase, triphosphate formed by cellular enzymes

Inhibits viral DNA polymerase by chain termination

Used for HSV, VZV, EBV

NOT USEFUL FOR CMV
Mechanism of resistance to acyclovir
Lack of thymidine kinase
Used on a daily basis to prevent HSV-2 outbreak
Famciclovir
Guanine nucleotide analog that does not require viral thymidine kinase for activation and therefore is useful for CMV
Ganciclovir

Inhibits viral DNA polymerase
Gancyclovir toxicities
Myelosuppression

Renal toxicity

More toxic to host than acyclovir
Foscarnet mechanism of action
Viral DNA polymerase inhibitor that binds to the pyrophosphate binding site of the enzyme

Pyrophosphate analog

Does NOT require activation by viral kinase
-navir
Protease inhibitors used for HIV therapy
Saquinavir
Protease inhibitor used for HIV therapy
Ritonavir
Protease inhibitors used for HIV therapy
Indinavir
Protease inhibitors used for HIV therapy

Toxicity is thrombocytopenia
Nelfinavir
Protease inhibitors used for HIV therapy
Amprenavir
Protease inhibitors used for HIV therapy
Mechanism of action of protease inhibitors
Inhibit assembly of new virus by blocking protease in progeny virions

Used to treat HIV
Lipodystrophy is a toxicity of what type of HIV therapy
Protease Inhibitors
Nucleoside Reverse Transcriptase Inhibitors mechanism of action
Compete with nucleosides and inhibit reverse transcriptase causing chain termination

Used to treat HIV
Non-nucleoside Reverse Transcriptase Inhibitors mechanism of action
Allosterically binds reverse transcriptase and prevents it from interacting with nucleosides

Used to treat HIV
Zidovudine (ZDV or AZT)
NRTI
Didanosine (ddI)
NRTI

Can cause pancreatitis
Zalcitabine (ddC)
NRTI
Stavudine (d4T)
NRTI
Lamivudine (3TC)
NRTI
Abacavir
NRTI
Treatment of HIV that can cause lactic acidosis
NRTIs
Drug used to treat HIV that can cause megaloblastic anemia
Zidovudine
Drug used to prevent mother to child transmission of HIV
Zidovudine
Toxicities of Reverse Transcriptase Inhibitors
Bone marrow suppression

Peripheral Neuropathy

Etc. depending on specific drug
Enfuviritide mechanism and use
Fusion inhibitor

Binds viral gp41 subunit, inhibits conformational change required for fusion with CD4 cells

Used to treat HIV as last resort
Toxicities of Enfuviritide
Hypersensitivity at injection site

Increased risk of bacterial pneumonia
Mechanism, uses, toxicity of Interferons
Glycoproteins from human leukocytes that block various stages of viral RNA and DNA synthesis

Induce ribonuclease that degrades viral mRNA

INF-a used for chronic Hep B and C, Kaposi's sarcoma

INF-B used for MS

INF-y used for NADPH oxidase deficiency

Toxicity is neutropenia
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