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ID Domain Drugs
Antibacterials, HIV drugs, antifungals, etc.
233
Pharmacology
Graduate
10/05/2013

Additional Pharmacology Flashcards

 


 

Cards

Term

Trimethoprim + Sulfamethoxazole

 

Pharmacokinetics

Definition

 - Well absorbed orally

 - High Urine Levels

 - Long Elimination T1/2: taken bid

 - Metabolites less soluble → crystalluria


Term

Sulfamethoxazole + trimethoprim

 

Mechanism of Action

Definition

 - Synergistic combination

 - Inhibit folate synthesis

 - Bacteriacidal

 

 - Sulfamethoxazole: blocks dihydropteroate synthetase

 - Trimethoprim: block dihydrofolate reductase

Term

Sulfamethoxazole + trimethoprim

 

Antimicrobial Spectrum

Definition

 - Gram-negative bacilli: E coliK pneumoniaeProteus spp

 - NOT P aeruginosa

 - MRSA action

Term

Sulfamethoxazole + trimethoprim

 

Mechanism of Resistance

Definition

Trimethoprim: single aa substitution to DHFR promoter causing overproduction; resistance in gram-negative enteric bacteria, stphylococci, H influenzae, and Listeria monocytogenes

 

Sulfamethoxazole: sing aa mutation in E coliS aureusStaphylococcus haemolyticusCampylobacter jejuni, and Helicobacter pyloriS pneumoniae and S pyogenes resistance base on 2 aa duplications in folP gene

Term

Sulfamethoxazole + Trimethoprim

 

Indications

Definition

- UTI

- Skin infections

- MRSA

- Acute bacterial sinusitis if allergic to penicillin

Term

Sulfamethoxazole + Trimethoprim

 

Adverse Effects

Definition

- Hypersensitivity→skin rashes, etc

- Leukopenia

- Hemolytic anemia with G-6-PD deficiency

- GI upset

Term

Antibiotics Commonly used to treat bacterial

UTIs

Definition

1) Sulfamethoxazole + trimethoprim

2) Trimethoprim

3) Nitrofurantoin

4) Fluoroquinolones (ciprofloxacin, levofloxacin)

5) Aminoglycosides (gentamicin, tobramycin)

Term

Nitrofurantoin

 

Pharmacokinetics

Definition

- Well absorbed orally

- Absorption enhanced with food

- Glomerular filtration & tubular secretion → high urine levels

Term

Nitrofurantoin

 

Mechanism of Action

Definition

- Metabolite inhibit DNA, RNA, and protein synthesis

- Bactericidal

 

- Damages bacterial DNA in reduced form

- Reactive intermediates attack ribosomal proteins, respiration, pyruvate metabolism and other macromolecules

Term

Nitrofurantoin

 

Antimicrobial spectrum

Definition
- Gram-negative bacilli: E coliK pneumonia
Term

Nitrofurantoin

 

Mechanisms of Resistance

Definition

- May be chromosomal or plasmid mediated and involves inhibition of Nitrofuran reductase

 - Resistance rare

Term

Nitrofurantoin

 

Indications

Definition
- UTIs
Term

Nitrofurantoin

 

Adverse Effects

Definition

- Nausea/vomiting

- Ineffective when CrCl < 40ml/min

Term

Fluoroquinolones

(Ciprofloxacin, levofloxacin, Moxifloxacin)

 

Pharmacokinetics

Definition

- Well absorbed orally

- High levels in kidney, prostate, and urine

- Long T1/2: taken bid to qd

- Metabolize and excreted in urine

- Moxifloxacin has less renal excretion

Term

Fluoroquinolones

(Ciprofloxacin, Levofloxacin, Moxifloxacin)

 

Mechanism of Action

Definition
- Binds to topoisomerases such as DNA gyrase → inhibits DNA synthesis
Term

Fluoroquinolones

(Ciprofloxacin, Levofloxacin, Moxifloxacin)

 

Antimicrobial Spectrum

Definition

- Gram-negative spectrum, aerobic organisms (E coli → P aeruginosa)

- Variable resistance (low with E coli and K pneumonia, high with P aeruginosa)

- Resistance growing

 

- Repiratory fluoroquniolones have activity against  S pneumoniaeH influenzae, and atypical pathogens

- Low resistance rates in community respiratory infections but high rates with P aeruginosa

Term

Fluoroquinolones

(Ciprofloxacin, Levofloxacin, Moxifloxacin)

 

Mechanism of Resistance

Definition

Three mechanisms known:

1. Some types of efflux pumps can act to decrease intracellular fluoroquinolone concentration

2. Plasmid-mediated resistance genes produce proteins that bind to DNA gyrase and protect it

3. Mutations at key sites in DNA gyrase and topoisomerase IV can decrease their binding affinity to fluoroquinolones

Term

Fluoroquinolones

(Ciprofloxacin, Levofloxacin, Moxifloxacin)

 

Indications

Definition

- UTIs

- Respiratory Tract infections

Term

Fluoroquinolones

(Ciprofloxacin, Levofloxacin)

 

Adverse Effects

Definition

- Nausea

- Insomnia

- Dizziness

- Drug interaction of Cipro and caffeine/theophylline

- Binds to bivalent metal cations

Term

Aminoglycosides

(gentamicin, tobramycin)

 

Pharmacokinetics

Definition

- Not absorbed orally; IV or IM only

- Excreted in urine, not metabolized

- Dosing interval based upon CrCl

(↓CrCl → ↓dosage to avoid renal damage)

Term

Aminoglycosides

(gentamycin, tobramycin)

 

Mechanism of Action

Definition
- Inhibits protein synthesis throughthe 30S subunit
Term

Aminoglycosides

(gentamicin, tobramycin)

 

Antimicrobial spectrum

Definition

- Gram-negative bacilli

- Sometimes used against MRSA in combination

- Resistance, but low rates of resistance in gram-negative rods

Term

Aminoglycosides

(gentamicin, tobramycin)

 

Mechanism of Resistance

Definition

Three mechanisms:

1. Reduced uptake due to transport defect or membrane impermeabilization

2. Altered ribosome binding sites due to mutation

3. Enzymatic modification for aminoglycoside modifying enzymes

Term

Aminoglycosides

(gentamicin, tobramycin)

 

Indications

Definition

- UTIs

- Combination therapy for MRSA

Term

Aminoglycosides

(gentamicin, tobramycin)

 

Adverse Effects

Definition

- Nephrotoxicity

- Ototoxicity (vesibular and cochlear) → dizziness, tinnitus, deafness (caused by accumulation of the drug)

Term

Antibiotics commonly used to treat

respiratory tract infections

Definition

- Penicillins (Penicillin G, Amoxicillin/ampicillin alone or with β-lactamase inhibitor, piperacillin alone or with β-lactamase inhibitor)

- Cephalosporins (ceftriazone, ceftarolin, ceftazidime, cefepime)

- Macrolides (Erythromycin, clarithromycin, azithromycin)

- Tetracycline (tetracycline, doxycycline)

- Fluoroquinolones (Levofloxacin, Moxifloxacin,Ciprofloxacin)

Term

Penicillin G

 

Pharmacokinetics

Definition

- Typically given parenterally because it is unstable in acidic stomach

- Excreted (filtered and secreted) in urine

- Short T1/2, but probenicid decreases rate of elimination

- Dosing interval increases with decreasing CrCl 

Term

Penicillin G

 

Mechanism of Action

Definition
- Bind to penicillin-binding proteins → lysis or alteration of the bacterial cell
Term

Penicillin G

 

Antimicrobial Spectrum

Definition

- Narrow spectrum

Streptococcal pneumoniae is main use

Term

Penicillin G

 

Mechanism of Resistance

Definition

- Change in PBP mediated by the mecA gene → reduced affinity to PBP2a (resistance)

- Occurs in Streptococcal pneumoniae and others

- Resistance also commonly due to β-lactamase enzymes that can be chromosomal or plasmid-mediated (H influenzae has 30% resistance rate for this reason)

- Use of β-lactamase inhibitor decreases resistance

Term

Penicillin G

 

Indication

Definition

- Respiratory tract infections

- GAS pharyngitis and other GAS infections

- Nonresistant Streptococcal pneumoniae infections

- Gas Gangrene

- Treponema Palldum including during pregnancy

- Erysipelas

Term

Penicillin G

 

Adverse Effects

Definition

- Hypersensitivity: rash → anaphylaxis

- High concetrations can cause seizures

- Diarrhea due to C. difficile due to normal flora clearnace

Term

Amoxicillin/Ampicillin

(Amoxicillin-clavulanate = Augmentin, Ampicillin-sulbactam = Eunicin)

 

Pharmacokinetics

Definition

- Augmentin absorbed orally

- Eunicin administered by IV

- Excreted (filtered and secreted) in urine

- Short T1/2, but probenicid decreases elimination

- Dosing interval increases with decreasing CrCl

Term

Amoxicillin/Ampicillin

(Amoxicillin-clavulanate = Augmentin, Ampicillin-sulbactam = Eunicin)

 

Mechanism of Action

Definition

- Amoxicillin/Ampicillin: bind to penicillin-binding proteins → lysis or alteration of bacterial cell

- Clavulanate/sulbactam: inhibit β-lactamase

Term

Amoxicillin/Ampicillin

(Amoxicillin-clavulanate = Augmentin, Ampicillin-sulbactam = Eunicin)

 

Antimicrobial spectrum

Definition

-Broad spectrum including S pneumoniaeH influenzae

Aerobic (E coli) and anaerobic (B fragilis)

- NOT P aeruginosa

Term

Amoxicillin/Ampicillin

(Amoxicillin-clavulanate = Augmentin, Ampicillin-sulbactam = Eunicin)

 

Mechanisms of Resistance

Definition

- Use of Clavulanate/sulbactam decreases resistance due to β-lactamase enzymes

- Resistance also due to change in PBP mediate by mecA gene mutation → reduces affinity to PBP2a (occurs in Strep pnumoniae)

Term

Amoxicillin/Ampicillin

(Amoxicillin-clavulanate = Augmentin, Ampicillin-sulbactam = Eunicin)

 

Indication

Definition

Streptococcal pyogenes infections

- Respiratory tract infections

- Mixed aerobic-anaerobic infections

 

Term

Amoxicillin/Ampicillin

(Amoxicillin-clavulanate = Augmentin, Ampicillin-sulbactam = Eunicin)

 

Adverse Effects

Definition

- Hypersensitivity: rash → anaphylaxis

- High concentrations can cause seizures

- Diarrhea due to C difficile after clearance of normal flora

Term

Piperacillin

(Piperaccilin-tazobactam = zocin)

 

Pharmacokinetics

Definition

- IV only

- Excreted (filtered and secreted) in urine

- Short T1/2, but probenicid decreases elimination rate

- Dosing interval increases with decreasing CrCl

Term

Piperacillin

(Piperacillin-taxobactam = zocin)

 

Mechanism of Action

Definition

- Piperacillin: binds to penicillin-binding proteins → lysis or alteration of the bacterial cell

- Taxobactam: inhibits β-lactamase

Term

Piperacillin

(Piperacillin-tazobactam = zocin)

 

Antimicrobial Spectrum

Definition
Term

Piperalcillin

(Piperacillin-tazobactam = zocin)

 

Anitimirobial spectrum

Definition
- Extended spectrum: S pneumoniaH influenzaeP aeruginosa
Term

Piperacillin

(Piperacillin-tazobactam = zocin)

 

Mechanism of resistance

Definition
- Change in PBP → reduced affinity (resistance)
Term

Piperacillin

(Piperacillin-tazobactam = zocin)

 

Indications

Definition

- Respiratory tractinfections

- Anaerobic, mixed aerobic-anaerobic infection

P aeruginosa infections

 

Term

Piperacillin

(Piperacillin-tazobactam = zocin)

 

Adverse Effects

Definition

- Hypersensitivity: rash → anaphylaxis

- High concentrations can cause seizures

- Diarrhea due to C difficiles after clearance of normal flora

Term

3rd-generation Cephalosporins

(Ceftriaxone, Ceftaroline, Ceftazidime)

4th-generation Cephalosporin

(Cefepime)

 

Pharmacokinetics

Definition

- Ceftiaxone and Ceftaroline IV only; Ceftazidime and Cefepime IV or IM

- CSF penetration varies, ceftriaxone preferred for meningitis

 - Ceftaroline excreted (filtered and secreted) into urine; ceftriaxone excreted into bile

 - Often longer T1/2 than penicillin

- Dosing dependent on CrCl

Term

3rd-generation Cephalosporins

(Ceftriaxone, Ceftaroline, Ceftazidime)

4th-generation Cephalosporin

(Cefepime)

 

Mechanism of Action

Definition
- Binds to penicillin-binding protein → lysis or alteration of bacterial cells
Term

3rd-generation Cephalosporins

(Ceftriaxone, Ceftaroline, Ceftazidime)

4th-generation Cephalosporin

(Cefepime)

 

Antimicrobial Spectrum

Definition

- 3rd generation active against gram-negative

- Cefepime activite against gram-positive and gram-negative organisms particularly against Enterobacteriaceae

- Action against H influenzae

- Ceftaroline has activity against MRSA

- Ceftaxidime and Cefepime active against Pseudomonas aeruginosa

Term

3rd-generation Cephalosporins

(Ceftriaxone, Ceftaroline, Ceftazidime)

4th-generation Cephalosporin

(Cefepime)

 

Mechanism of Resistance

Definition
Change in PBP → reduced affinity (resistance)
Term

3rd-generation Cephalosporins

(Ceftriaxone, Ceftaroline, Ceftazidime)

4th-generation Cephalosporin

(Cefepime)

 

Indications

Definition

- Respiratory tract infections

- Skin and soft-tissue infections (1st generation mostly, unless infection by MRSA)

- Anaerobic or mixeda aerobic-anaerobic

- GAS pharyngitis

Streptococcal pneumoniae infections

Streptococcal pneumoniae infections

- Neisseria gonorrhea urethritis (ceftriaxone)

- MRSA infections (ceftaroline only)

Psuedomonas aeruginosa infections (cefepime and ceftazidime)

Term

3rd-generation Cephalosporins

(Ceftriaxone, Ceftaroline, Ceftazidime)

4th-generation Cephalosporin

(Cefepime)

 

Adverse Effects

Definition

- Hypersensitivity

- High concentration can cause seizures

- Can lead to overgrowth of other bacteria (Enterococci, C difficile)

Term

Macrolides

(Erthromycin, Clarithromycin, Azithromycin)

 

Pharmacokinetics

Definition

- Orally absorbed

- Newer agents have longer T1/2

- Metabolized by the liver; CYP 450 drug interactions can occur, but not with azithromycin

Term

Macrolides

(Erythromycin, Clarithromycin, Azithromycin)

 

Mechanism of Action

Definition
- Inhibit protein synthesis via the 50S ribosomal subunit
Term

Macrolides

(Erythromycin, Clarithromycin, Azithromycin)

 

Antimicrobial Spectrum

Definition

- Broad spectrum against respiratory pathogens (S pneumoniaeH influenzae, mycoplasma)

- Clarithromycin and azithromycinhave improved activity against H influenzae compared to erythromycin

Term

Macrolides

(Erithromycin, Clarithromycin, Azithromycin)

 

Mechanism of Resistance

Definition

- Resistance i sprimariy due to active efflux and change in the binding site in the ribosome

- High rates of resistance in S pneumoniae

Term

Macrolides

(Erythromycin, Clarithromycin, Azithromycin)

 

Indications

 

Definition
- Bacterial respratory tract infections
Term

Macrolides

(Erythromycin, Clarithromycin, Azithromycin)

 

Adverse Effects

Definition

- GI upset; nausea, vominitin, diarrhea

- Drug interactions; for example clarithromycin + statin may lead to myositis or rhabdmyolysis

- Use with caution in patients with arrythmias because macrolides ↑ QT interval

- Use with caution in patients receiving CYP-3A inhibitors

- Heptatotoxicity

Term

Tetracyclines

(Tetracyclin, Doxycycline)

 

Pharmacokinetics

Definition

- Absorbed orally

- Doxycycline has a long T1/2

- Excreted in urine and feces

- Binding by multivalent cations; should not take with milk or drugs with cations

Term

Tetracyclines

(Tetracyclin, Doxycycline)

 

Mechanism of Action

Definition
- Blocks binding of tRNA to 30X subunit of the ribosome
Term

Tetracyclines

(Tetracycline, Doxycicline)

 

Antimicrobial Spectrum

Definition

- Broad spectrum against respiratory pathogens (S pneumoniaeH influenzae, mycoplasma)

- High rates of resistance in S pneumoniae to tetracycline; doxycycline resistance is lower

Term

Tetracyclines

(Tetracycline, Doxycycline)

 

Mechanism of Resistance

Definition
- Several resistance mechanisms including efflux of antimicrobial and altered bacterial porins that prevent uptake
Term

Tetracyclines

(Tetracyclin, Doxycycline)

 

Indications

Definition
- Bacterial respiratory tract infection
Term

Tetracyclines

(Tetracycline, Doxycycline)

 

Adverse Effects

Definition

- Nausea

- Dizziness

- Photosensitivity

- Teeth discoloration in children

Term

1st-generation Cephalosporins

(Cefazolin, Cephalexin)

3rd-generation Cephalosporin

(Ceftriaxone)

 

Pharmacokinetics

Definition

- Cefazolin usually administered IV or IM; Cephalexin well absorbed orally; Ceftriaxone administered IV or IM

- CSF penetration varies; Ceftriaxone drug of choice for meningitis

- Cefazolin and Cephalexin excreted (filtered and secreted) into urine; Ceftriaxone excreted into bile

- Often longer T1/2 than penicillins

- Dosing dependent upon CrCl

- Cefazolin is highly protein bound

Term

1st-generation Cephalosporins

(Cefazolin, Cephalexin)

3rd-generation Cephalosporin

(Ceftriaxone)

 

Mechanism of Action

Definition
- Bind to penicillin-binding proteins → lysis or alteration of the bacterial cell
Term

1st-generation Cephalosporins

(Cefazolin, Cephalexin)

3rd-generation Cephalosporin

(Ceftriaxone)

 

Antimicrobial Spectrum

Definition

- 1st-generation cephalosporins have good activity against gram-positive organisms (S aureusStreptococci)

- 3rd generation active against gram-negative including H influenzae

Term

1st-generation Cephalosporins

(Cefazolin, Cephalexin)

3rd-generation Cephalosporin

(Ceftriaxone)

 

Mechanism of Resistance

Definition
- Change in penicillin-binding protein → reduced affinity (resistance)
Term

1st-generation Cephalosporins

(Cefazolin, Cephalexin)

3rd-generation Cephalosporin

(Ceftriaxone)

 

Indications

Definition

- Skin and Soft tissue infections

- Group A streptococcal pharyngitis, other streptococcal infections

Staph aureus infections

Term

1st-generation Cephalosporins

(Cefazolin, Cephalexin)

3rd-generation Cephalosporin

(Ceftriaxone)

 

Adverse Effects

Definition

- Hypersensitivity

- High concentrations can cause seizures

- Can lead to overgrowth of other bacteria causing diarrhea (Enterococci, C difficile)

Term
Antibiotics commonly used for skin/soft tissue infections
Definition

- First-generation cephalosporins

- Anitstaphylococcal penicillins

- Ceftriaxone

- Vancomycin

- Clindamycin

- Linezolid

- Daptomycin

Term

Antistaphylococcal penicillins

(Nafcillin)

 

Pharmacokinetcis

Definition

- Usally administered by IV or IM

- Short T1/2, but probenicid decreases elimination rate

- Nafcillin is excreted in bile

- Highly protein bound

Term

Antistaphylcoccal penicillins

(Nafcillin)

 

Mechanism of Action

Definition
Bind to penicillin-binding proteins → lysis or alteration of bacterial cell
Term

Antistaphylococcal Peniccilins

(Nafcillin)

 

Antimicrobial spectrum

Definition

- Activity against gram-positive organsims (S aureus and  Streptococci)

- NOT active against MRSA (PBP2a)

Term

Antistaphylococcal Penicillins

(Nafcillin)

 

Mechanism of Resistance

Definition

- Inactivation by β-lactamases

 - Alterations in PBP

Term

Antistaphylococcal Penicillins

(Nafcillin)

 

Indications

 

Definition

- Skin and soft tissue infection

- Coagulase-negative Staphylococci

S aureus infections

Term

Antistaphylococcal Penicillins

(Nafcillin)

 

Adverse Effects

Definition

- Hypersensitivity (rash → anaphalaxis)

- High concentrations can cause seizures

- Diarrhea caused by C difficile

- Hepatitis

Term

Vancomycin

 

Pharmacokinetics

Definition

- Poorly absorbed, used orally only for treatment of C difficile; IV administration

- Tissue distribution is limited

- Long T1/2 and is extended in renal failure

- Renally excreted by glomerular filtration

Term

Vancomycin

 

Mechanism of Action

Definition
- Glycopeptide antibiotic that binds to cell wall peptides, inhibits proper cell wall synthesis in gram-positive bacteria
Term

Vancomycin

 

Pharmacokinetics

Definition

- Poorly absorbed, used orally only for treatment of C difficile; IV administration

- Tissue distribution is limited

- Long T1/2 and is extended in renal failure

- Renally excreted by glomerular filtration

Term

Vancomycin

 

Mechanism of Action

Definition
- Glycopeptide antibiotic that binds to cell wall peptides and inhibits proper cell wall synthesis in gram-positive bacteria
Term

Vancomycin

 

Antimicrobial spectrum

Definition

- Active against gram-positive cocci (S aureusEnterococcusStreptococci) including MRSA and PRSP (Penicillin-resistant S pneumoniae)

- Active against C difficile

Term

Vancomycin

 

Mechanism of Resistance

Definition
- Acquired resistance in Enterococci due to amino acid changes at binding site
Term

Vancomycin

 

Indications

Definition

- Skin and soft tissue infections

- Coagulase-negative Staphylococci infections

- MRSA infections

Streptoccocus pneumoniae infections

Term

Vancomycin

 

Adverse Effects

Definition

- Rash caused by histamine release

- Nephrotoxic especially with other nephrotoxic drugs such as aminoglycosides

- High concentrations can be ototoxic

- Hematologic Effects such as thrombocytopenia and neutropenia

Term

Clindamycin

 

Pharmacokinetics

Definition

- Absorbed orally

- Well distributed

- Hepatic metabolism

- Biliary and fecal excretion

Term

Clindamycin

 

Mechanism of Action

Definition

- Inhibits proteinsynthesisby inhibiting tRNA binding

- Can inhibit toxin formation

Term

Clindamycin

 

Antimicrobial spectrum

Definition

- Active against gram-positive cocci and anaerobes

- Active against some strains of MRSA; resistance in S aureus is variable

Term

Clindamycin

 

Mechanism of Resistance

Definition
- Cross-resistance with macrolides due to ribosomal methylation
Term

Clindamycin

 

Indications

Definition

- Skin and soft tissue infections

- Anaerobic or Mixed aerobic-anaerobic infections

- Acute bacterial sinusitis

- GAS pharyngitis

- MRSA infections

- Gas gangrene

- Pelvic Inflammatory Disease caused by Neisseria gonorrhoeae

- Impetigo

Term

Clindamycin

 

Adverse Effects

Definition
- Diarrhea especially caused by C difficile; causes such terrible diarrhea that use is limited
Term

Linezolid

 

Pharmacokinetics

Definition

- Oral or IV, 100% bioavailability

- Good tissue distribution including SF

- Metabolized in liver

- Few drug interactions

- Weak MAO inhibitor, can ↑ serotonin levels

Term

Linezolid

 

Mechanism of Action

Definition
- Inhibition of protein synthesis through the 50S ribosome subunit
Term

Linezolid

 

Antimicrobial spectrum

Definition

- Acitve against gram-positive cocci (Staphylococcus, Enterococcus) including MRSA and VRE

- Very active against atypical respiratory pathogens

Term

Linezolid

 

Mechanism of Resistance

Definition

- Resistance is uncommon

- Intrinsic resistance of gram-negtive due to efflux pumps, which actively pump linezolid

- Resistance of gram-positive due to point mutations in 23S ribosomal RNA

Term

Linezolid

 

Indications

Definition

- Skin and soft tissue infections

- Alternative for coagulase negative Staphylococci infections

- MRSA infections

 

Term

Linezolid

 

Adverse Effects

Definition

- Diarrhea

- Headache

- Nausea

- Thrombocytopenia; should monitor platelets

Peripheral neuropathy with long-term use (>3 mos) as used in osteomyelitis

- Serotonin Sydrome (clonus, seizuers, altered mental status, even death) if givenwith and SSRI

Term

Daptomycin

 

Pharmacokinetics

Definition

- Not absorbed orally; only IV

- High protein binding

- Excreted primarily by the kidneys, 60% unchanged

- T1/2 increases with renal failure- Bound and inactivated by pumonary surfactant in the epithelial lining fluid of the lungs; not good for pneumonia

 

Term

Daptomycin

 

Mechanism of Action

Definition
- Lipopeptide that bind to and alters the cell membrane, leading to loss of ions and cell death
Term

Daptomycin

 

Antimicrobial Spectrum

Definition
- Active against gram-positive pathogens including MRSA, vancomycin-resistant Enterococci and Penicillin-resistant pneumococci
Term

Daptomycin

 

Mechanism of Resistance

Definition
- Resistance is rare and can be due to alterations in the cell membrane leading to reuced drug binding
Term

Daptomycin

 

Indications

Definition

- Skin and soft tissue infections

- Coagulase-negative Staphylococci

- MRSA infection

Term

Daptomycin

 

Adverse Effects

Definition

- Hypersensitivity (fever, rash, etc)

- Effects on the skeletal muscle causing muscle pain or weakness; increases in CPK

Term
Antibiotics commonly used for anaerobic or mixed aerobic-anaerobic infections
Definition

- Penicillins

- Cefoxitin

- Carbapenems

- Metroidazole

- Clindamycin

- Tigecycline

Term

Cefoxitin

 

Pharmacokinetics

Definition

- IV administation

- Excreted in urine

- Short T1/2

Term

Cefoxitin

 

Mechanism of Action

Definition
- Interes with cell wall synthesis
Term

Cefoxitin

 

Antimicrobial spectrum

Definition

- Active against a broad range of gram-negative and gram-positive bacteria including anaerobes

- Inactive against most P aeruginosa and enterococci

- Inactive against MRSA

Term

Cefoxitin

 

Mechanism of Resistance

Definition
- Resistance is prin mediated
Term

Cefoxitin

 

Indications

Definition

- Anaerobic or mixed aerobic-anaerobic infections

- Used with Doxycycline for Pelvic Inflammatory Disease 

Term

Cefoxitin

 

Adverse Effects

Definition
- Diarrhea
Term

Carbapenems

(Imipenem, Meropenem)

 

Pharmacokinetics

Definition

- Not absorbed orally, must be given by IV

- Distributed in the body like penecillin

- Renally eliminated by tubular secretion

- Cilastatin, a DHP II inhibito, prevents inactivation of imipenem in the kidneys

- Doses should be decreased with renal insufficiency

Term

Carbapenems

(Imipenem, Meropenem)

 

Mechanism of Action

Definition

- High affinity for PBP's

- Binds and causes bacteria cell alteration or lysis

Term

Carbapenems

(Imipenem, Meropenem)

 

Antimicrobial spectrum

Definition

- Broad-spectrum activity against aerobic and anaerobic organisms

- Good activity against P aeruginosa

- Resistant to many β-lactamase enzymes

Term

Carbapenem

(Imipenem, Meropenem)

 

Mechanism of Resistance

 

Definition
- Resistance commonly due to loss of porin proteins → decrease in entry of bacteria
Term

Carbapenems

(Imipenem, Meropenem)

 

Indications

Definition

- Anaerobic or mixed aerobic-anaerobic infections

- Gas gangrene

Term

Carbapenems

(Imipenem, Meropenem)

 

Adverse Effects

Definition

- Hypersensitivity reactions; can exhibit cross allergy with other β-lactams

- Nausea

- Seizures with high doses of imipenem/cilastatin

Term

Metronidazole

 

Phamacokinetics

Definition

- Well absorbed; can be given orally or by IV

- Widely distributed into tissues, including CSF

- Long T1/2

- Extensively metabolized into oxidative products

Term

Metronidazole

 

Mechanism of Action

Definition
- Reduction of nitro group → oxidized DNA causing strand breaks
Term

Metronidazole

 

Antimicrobial Spectrum

Definition

- Active against anaerobic bacteria and protozoa

- Anaerobes only

Term

Metronidazole

 

Antimicrobial Spectrum

Definition

- Active against anaerobic bacteria and protozoa

- Anaerobes only

Term

Metronidazole

 

Mechanism of Resistance

Definition

- Low rates of resistance in anaerobic organisms

- Resistance is due to decreased oxidoreductase activity → reduced activation

- Resistant strains have increased levels of LDH

Term

Metronidazole

 

Indications

Definition

- Anaerobic or mixed aerobic-anaerobic infection

- Gas gangrene

- Second line treatment of Pelvic Inflammatory Disease in combination with Azithromycin

Term

Metronidazole

 

Adverse Effects

Definition

- GI symptoms (nausea, anorexia)

- Metallic taste

- Pancreatitis

- Drug interactions when taken with alcohol, warfarin, and phenytoin due to disulfiram reaction

Term

Tigecycline

 

Pharmacokinetics

Definition

- Only IV (not absorbed orally)

- Long T1/2 requiring only twice-daily dosing

- Low serum levels; high tissue concentrations

- Eliminated in feces via biliary excretion; 10% renal clearance so don't need to worry about renal insufficiency

Term

Tigecycline

 

Mechanism of Action

Definition

- A minocycline derivative

- Blocks binding of tRNA to the 30S subunit of ribosome

Term

Tigecycline

 

Antimicrobial Spectrum

Definition

- Broad-spectrum activity against aerobes and anaerobes

- Not active against P aeruginosa

Term

Tigecycline

 

Mechanism of Resistance

Definition
- Resistance due to multidrug efflux pump systems
Term

Tigecycline

 

Indications

Definition

- Anaerobic and mixed aerobic-anaerobic infections

- MRSA infections

Term

Tigecycline

 

Adverse Effects

Definition

- High rate of nausea and vomitin

-Low rates of C difficile diarrhea

- Rare pancreatitis

Term
Antimycobacterial Agents
Definition

- Isoniazid

- Rifampin, Rifabutin

- Ethambutol

- Pyrazinamide

Term

Isoniazid

 

Pharmacokinetics

Definition

- Can be administered orally, IV, IM

- Very low protein binding

- Metabolized in the liver by CYP 450, 2C19 and 3A4

- Excreted primarily by the urine, but secondarily in feces

- Inhibits CYP 450 system

Term

Isoniazid

 

Mechanism of Action

Definition

- Bactericidal to rapidly dividing mycobacteria and bacteriostatic if bacteria is slow growing

- Must be activated by KatG

- Acts by blocking fatty acid synthase which inhibits mycolic acid synthesis which is required for the mycobacterial cell wall

Term

Isoniazid

 

Antimicrobial Spectrum

Definition
- Mycobacterium tuberculosis
Term

Isoniazid

 

Mechanism of Resistance

Definition

- Most commonly due to mutation of the catalase-peroxidase (KatG) that reduces its activity, preventing prodrug conversion to the active form

- Another mechansim involves missense mutation of the bacterial genes inhA and KasA, involved in mycolic acid synthesis

- NADH dehydrogenase mutations cause resistance as well

Term

Isoniazid

 

Adverse Effects

Definition

- Rash

- Hepatitis

- Sideroblastic anemia

- Peripheral neuropathy

- Mild CNS effects

- Drug interactions when taken with phenytoin, disulfiram, theophylline

Term

Rifampin

 

Pharmacokinetics

Definition

- Administered orally or by IV

- 90-95% bioavailability

- Metabolized by the intestinal cell wall and liver

- Excreted most in feces, but partially in urine

Term

Rifampin

 

Mechanism of Action

Definition
- Binds to the β subunit of DNA-dependent RNA polymerase and inhibits RNA synthesis
Term

Rifampin

 

Antimicrobial Spectrum

Definition

 - Active against most gram-positive bacteria (Staphylococci) as well as many gram-negative (E coliPseudomonasKlebsiella)

- Active against Neisseria meningitidis and H influenzae

- Active against Mycobacterium tuberculosis

Term

Rifampin

 

Mechanism of Resistance

Definition
- Resistance due to an alteration of the target gene rpoB
Term

Rifampin

 

Indications

Definition

Mycobacterium tuberculosis infections

- MRSA infections in combination therapy

Term

Rifampin

 

Adverse Effects

Definition

- Generally well tolerated

- Nausea, vomiting

- Fever

- Rarely hepatitis

- Hypersensitivity

Term

Ethambutol

 

Pharmacokinetics

Definition

- Administered orally, bioavailability is ~80%

- 10-40% of the drug is bound to plasma protein

- Majority is not metabolized and is renally excreted

Term

Ethambutol

 

Mechanism of Action

Definition
- Inhibits arabinosyl transferase III, disrupting assembly of mycobacterial cell wall
Term

Ethambutol

 

Antimicrobial Spectrum

Definition
- Wide range of activity against mycobacteria only, including M tuberculosis
Term

Ethambutol

 

Mechansim of Resistance

Definition
- Resistance develop via mutation is the embB gene for arabinosyl transferase
Term

Ethambutol

 

Indications

Definition

- TB

- Other mycobacterial infections

Term

Ethambutol

 

Adverse Effects

Definition

- Very few serious adverse effects

- Diminished visual acuity

- Rash

- Fever

Term

Pyrazinamide

 

Pharmacokinetics

Definition

- Well absorbed orally; biovailability is >90%

- Metabolized then excreted by kidney

- Excretion is reduced in renal failure

Term

Pyrazinamide

 

Mechnism of Action

Definition

- Activated by acidic conditions

- Actual mechanism still unknown

Term

Pyrazinamide

 

Antimicrobial Spectrum

Definition

- Active only at acidic pH

M tuberculosis infections

Term

Pyrazinamide

 

Mechanism of Resistance

Definition

- Resistance due to reduced affinity of pyrazinamidase with reduced affinity for pyrazinamide

- Reduced affinity decreases the conversion of pyrazinamide

Term

Pyrazinamide

 

Indications

Definition

M tuberculosis infection

- Co-administration with isoniazid or rifampin has let to a 1/3 reduction in teh duration of anti-TB therapy

Term

Pyrazinamide

 

Adverse Effects

Definition

- Injury to the liver is most serious side effect

- Hyperurecemia in nearly all patients

- Athralgia, anorexia, nausea, vomiting, dysuria, malaise, and fever

Term

Amphotericin B

(Liposomal preparations)

 

Pharmacokinetics

Definition

- Only IV (not well absorbed)

- Higher doses usedfor treatment than deoxycholate

- Widely distributed, but CSF levels are minimal

- Extensively metabolized by the liver

- Initial T1/2 ~ 24, terminal T1/2~15 days

- Achieve lower renal tissue concentration than deoxycholate; concentrated in reticuloendothelial tissues (livere and spleen)

Term

Amphotericin B

(Liposomal preparations)

 

Mechanism of Action

Definition
- Binds to ergosterol in teh fungal cell membrain → leakage of cell contents
Term

Amphotericin B

(Liposomal preparations)

 

Antimicrobial Spectrum

Definition

- Broad-spectrum of activity against most pathogenic fungi, including invasive Aspergillosis

- Resistance is uncommon

Term

Amphoberiticin B

(Liposomal preparations)

 

Mechanism of Resistance

Definition
- Mutants replace ergosterol with certain precursor sterols
Term

Amphotericin B

(Liposomal preparations)

 

Indications

Definition

- Candida infections

- Aspergillus infections

Term

Amphotericin B

(Liposomal preparations)

 

Adverse Effects

Definition

- Infusion reactions (fever, chills, nausea, hypotension, tachycardia, rigors); pretreatment meds often given; least reaction with liposomal preparation

- Nephrotoxicity, the dose-limiting toxicity; sodium loading can help; less nephrotoxicity than with deoxycholate

- Other drugs can add to nephrotoxicity including aminoglycosides, cyclosporine, foscarnet, cisplatin

- Hypokalemia and hypomagnesemia; amelioride can help

- Liver toxicity

Term

Itraconazole

 

Pharmacokinetics

Definition

- Only oral formulation (lipid soluble)

- Variable absorption (improved with food, decreased with drugs that raise stomach pH)

- Poor CSF penetration

- Highly protein bound

- Metabolized in GI tract and liver

- Low urine recovery

- Significant drug-drug interactions: it is a potent inhibitor of CYP 3A4 (antiarrythmics, antiepileptics, antiretrovirals, psychotropics, statins, immunosuppressants, etc.)

Term

Itraconazole

 

Mechanism of Action

Definition
- Interferes with ergesterol synthesis via inhibition of cytochrome dependent 14-α demethylase
Term

Itraconazole

 

Antimicrobial Spectrum

Definition
- Active against many fungal pathogens including Candida spp. and Aspergillosis
Term

Itraconazole

 

Mechanism of Resistance

Definition

- Primary mechanism of resistance in Candida is accumulation of mutation in ERG11, which protect heme in the enzyme pocket from biding to the azole

- Increased azole efflux adds to resistance

- Primary mechanism of resistance in Aspergillus causes increased azole transport and decreased ergosterol content

Term

Itraconazole

 

Indications

Definition

- Candida and Aspergillus infections outside of the CNS

- Chronic Granulomatous Disease as an antifungal

Term

Itraconazole

 

Adverse Effects

Definition

- Nausea, abdominal pain

- Rash

- Hepatitis

- Hypokalemia, edema and hypertension; should be used with caution in CHF patients

Term

Fluconazole

 

Pharmacokinetics

Definition

- IV and PO (100% bioavailability)

- Water soluble → penetrates many tissues

- CSF concentrations are half those in serum

- High urine concentration

- Long T1/2

- Mostly renal excretion; doses decreased in patients with renal failure

- Can inhibit the metabolism of other drugs via CYP 3A4 and CYP2C9

Term

Fluconazole

 

Mechanism of Action

Definition
- Inhibits ergosterol synthesis via inhibition of 14αdemethylase
Term

Fluconazole

 

Antimicrobial Spectrum

Definition
Term

Fluconazole

 

Mechanism of Resistance

Definition

- Primary mechanism of resistance in Candida is accumulation of mutation in ERG11, which protect heme in the enzyme pocket from biding to the azole

- Increased azole efflux adds to resistance

- Primary mechanism of resistance in Aspergillus causes increased azole transport and decreased ergosterol content

Term

Fluconazole

 

Indications

Definition
- Candida infection
Term

Fluconazole

 

Adverse Effects

Definition

- GI upset (nausea, vomiting)

- Skin rash

- Hepatitis

Term

Voriconazole

 

Pharmacokinetics

Definition

-IV and PO; 95% bioavailable

- Good tissue penetration, including CSF

- Metabolized by the liver; renal insufficiency doesn't effect dosing

- Multiple drug interaction; inhibits CYP2C9 (warfarin, phenytoin) and CYP3A4 (tacrolimus, cyclosprine)

Term

Voriconazole

 

Mechanism of Action

Definition
- Inhibits ergosterol synthesis by bolocking activity of 14-α-demethylase
Term

Voriconazole

 

Antimicrobial Spectrum

Definition
- Active against Candida species (including species resistant to fluconazole) and Aspergillus species
Term

Voriconazole

 

Mechanism of Resistance

Definition

- Primary mechanism of resistance in Candida is accumulation of mutation in ERG11, which protect heme in the enzyme pocket from biding to the azole

- Increased azole efflux adds to resistance

- Primary mechanism of resistance in Aspergillus causes increased azole transport and decreased ergosterol content

Term

Voriconazole

 

Indications

Definition

- Aspergillus infection

- (Candida Infection)

Term

Voriconazole

 

Adverse Effects

Definition

- Abnormal vision (blurred, photophobia) occurs in 1/3 of patients and lasts for about 30 minutes

- Nausea, fever, chills

- Rash

- Hepatitis

Term

Caspofungin

 

Pharmacokinetics

Definition

- Only IV

- Widely distributed with a half-life of 10 hours

- Brain and CSF penetration is limited due to high protein binding

- Undergoes hydrolysis and N-acetylation in the liver

- Urine exretion is minimal

- Drugs such as rifampin, phenytoin, and efavirenz can reduce caspofungin levels by increasing its metabolism

Term

Caspofungin

 

Mechanism of Action

Definition

- Inhibits β-glucan synthesis via inhibition of glucan synthetase; this leads to increased cell wall permeability and lysis of the cells

- Fungicidal

Term

Caspofungin

 

Antimicrobial Spectrum

Definition

- Active against Candida species and Aspergillus species

- Maintains activity against fluconazole-resistant Cadida albicans

Term

Caspofungin

 

Indications

Definition

- Candida infections

- Coverage of Aspergillus but not primary treatment of Aspergillus infections

Term

Caspofungin

 

Adverse Effects

Definition

- Phlebitis

- Skin rash, fever, headache, nausea

- Hepatits

Term

5-Fluorocytosine

 

Pharmacokinetics

Definition

- Well absorbed with oral administration

- Widely distributed in the body

- Most excreted unchanged in urine

Term

5-Fluorocytosine

 

Mechanism of Action

Definition
- Inhibits thymidylate synthetase so DNA synthesis is impaired
Term

5-Fluorocytosine

 

Antimicrobial Spectrum

Definition
- Active against Candida spp
Term

5-Fluorocytosine

 

Mechanism of Resistance

Definition
- Can be loss of the permease necessary for cytosine transport or decreased activity of either UPRTase or cytosine deaminase, both of which are necessary for activation
Term

5-Fluorocytosine

 

Indications

Definition
- Candida infections
Term

5-Fluorocytosine

 

Adverse Effects

Definition

- May depress the bone marrow and lead to leukopenia and thrombocytopenia

-Rash, nausea, vomitin, diarrhea

- Severe entercolitis

- Elevated hepatic enzymes

Term
Antifungal Agents
Definition

- Amphotericin B

- Itraconazole

- Fluconazole

- Voriconazole

- Caspofungin

- 5-fluorocytosine

Term

Acyclovir and Valacyclovir

 

Pharmacokinetics

Definition

- Oral acyclovir is poorly absorbed (10%) whereas Valacyclovir, a prodrug, has bioavailability of 55%

- Can also be given by IV

- Widely distributed in the body including brain and CSF

- Eliminated in the Urine

Term

Acyclovir and Valacyclovir

 

Mechanism of Action

Definition

- Active Metabolites inhibit viral replicationby acting as substrates fo and inhibiting viral DNA polymerase (chain termination)

- Phosporylated by viral thymidine kinase to become active

Term

Acyclovir and Valacyclovir

 

Antimicrobial Spectrum

Definition
- Active against HSV-1, HSV-2 and VZV
Term

Acyclovir and Valacyclovir

 

Mechanism of Resistance

Definition

-Occurs when thymidine kinase (TK) is absent or altered

- Resistance is uncommon in immunocompetent patients

Term

Acyclovir and Valacyclovir

 

Indications

Definition

- Herpes Infection; when taking during pregnancy acyclovir decreases clinical HSV recurrence at the time of delivery and asymptomatic viral shedding at deliver

- Herpes-zoster infection

Term

Acyclovir and Valacyclovir

 

Adverse Effects

Definition

- GI upset and headache

- Renal insufficiency

Term

Amantadine

 

Pharmacokinetics

Definition

- Absorbed orally

- Cleared by both glomerular filtration and tubular secretion

- Half-life is increased in renal insufficiency

Term

Amantadine

 

Mechanism of Action

Definition
- Inhibits replication of influenza A viruses by blocking ion channes function (M2 protein)
Term

Amantadine

 

Antimicrobial Spectrum

Definition

- Acitve against influenza A

- Not active against influenza B

Term

Amantadine

 

Mechanism of Resistance

Definition
- Resistance is common in infulenza A viruses due to mutation in teh M gene
Term

Amantadine

 

Indications

Definition
- Influenza A virus infection
Term

Amantadine

 

Adverse Effects

Definition

- CNS events (nervousness, lightheadedness, insomnia, confusion); these can be enhance by other drugs such as antihistamines and phenyl propanolamine)

- GI upset (nausea, loss of apetits)

- Teratogenic

Term

Oseltamivir

 

Pharmacokinetics

Definition

- Absorbed orally (prodrug)

- Active compound (carboxylate) is excreted by glomerular filtration and tubular secreation

Term

Oseltamivir

 

Mechanism of Action

Definition
- Neuraminidase inhibitor; prevents virus release from infected cells
Term

Oseltamivir

 

Antimicrobial Spectrum

Definition

- Active against influenza A and B viruses

- Resistance is now common in H1N1 strains

Term

Oseltamivir

 

Mechanism of Resistance

Definition
- Resistance due to mutation in the viral neuraminidase
Term

Oseltamivir

 

Indications

Definition
- Influenza A and B infections
Term

Oseltamivir

 

Adverse Effects

Definition

- Nausea, vomiting; these effects are decreased with food

- Headache

- Can be harmful during pregnancy

Term
NRTI
Definition

- Lamivudine (3TC)

- Zidovudine (ZDV, AZT)

- Emtricitabine

- Abacavir

Term

NRTI

 

Mechanism of Action

Definition

- Must first undego intracellular phosphrylation to be active

-Mimic other nucleosides and are incorporated into the DNA strand

- Inhibit the viral reverse transcriptase enzyme thus inhibit transcription of viral RNA into dsDNA

- Halts production of new virions

Term
N
Definition
Term

NRTIs

 

Adverse Effects

Definition

- Lactic Acidosis

- Abacavir = severe hypersensitivity reactons; having a positive HLA-B5701 allele increases the risk of hypersensitivity reactions

- Zidovudine = headache,anemia, neutropenia

Term
NNRTIs
Definition

- Efavirenz

- Rilpivirine

Term

NNRTI

 

Mechanism of Action

Definition
- Binds directly to the reverse transcriptase enzyme; confomation change renders the enzyme inactive
Term

NNRTI

 

Adverse Effects

Definition

- Efavirenz = hepatitis

- Rilpivirine = depressive disorder, not approved if the viral load is > 100,000 copies, taken with a meal

Term
PIs
Definition

- Nelfinavir

- Atazanavir

- Ritonavir

- Darunavir

Term

PI

 

Mechanism of Action

Definition

- Stop the protease enzyme from forming mature virions

- When the PIs bind to the enzyme, HIV is still being produced, but they are considered inactive

- Low dose Ritonavir is used to boost serum levels of the PIs

Term

PIs

 

Adverse Effects

Definition

- Poor absorption

- Drug interactions (P450)

- Lipid abnormalities; should check patient's TGs and cholesterol routinely

- Lipodystrophy, redistribution of fat

- Cause or worsen diabetes

- GI symptoms

Term
Fusion Inhibitors
Definition

- Enfurviritide

- Maraviroc

Term

Fusion Inhibitors

 

Mechanism of Action

Definition

- Enfuviritide = blocks HIV CD4 cell fusion through co-receptors

- Maraviroc = CCR5 antagonists; not effective in cells with CXCR4 receptors

Term

Fusion Inhibitors

 

Pharmacokinetics

Definition

- Enfuviritide = administered SC bid

- Maraviroc = Oral administration

Term

Fusion Inhibitors

 

Adverse Effects

Definition
- Enfuviritide = inflammation at the injection site, eosinophilia, increased rate of bacterial pneumonias
Term
Integrase Inhibitors
Definition

- Raltegravir

- Elvitegravir

Term

Integrase Inhibitors

 

Mechanism of Action

Definition
- Prevents the integrationof the viral DNA (provirus) into the host DNA
Term

Raltegravir

 

Adverse Effects

Definition

- Diarrhea

- Rash

- Increased CPK

Term

Elvitegravir

 

Administration

Definition

- Only available in a comination drug called Stribild (elvitegravir+cobicistat+emtricitabine+tenofovir)

- Cobicistat isnot active against HIV; it inhibits CYP3A4 and enhances other HIV drugs

Term
Anti-malarials
Definition

- Quinine

- Malarone

- Chloroquine

Term

Quinine

 

Pharmacokinetics

Definition

- May be administered orally or IM

- Metabolized by the liver

- Excretedin the urine

Term

Quinine

 

Mechanism of Action

Definition

- Gametocidal

- Active against blood schizonts but not liver stage parasites

- Mechanism is unknown

Term

Quinine

 

Antimicrobial spectrum

Definition
- Gametocidal against P vivaxP ovale, but not P falciparum
Term

Quinine

 

Indications

Definition

P vivax and P ovale infections

- Parental or Oral treatment of Severe Falciparum

 

Term

Quinine

 

Adverse Effects

Definition

- Tinnitus

- Headache,nausea, dizziness

- Flushing

- Visual distrubances

- Together known as Cinchonism

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