Principles of Pharmacology
This phase of drug development uses "normal" (healthy) volunteers to assess safety and biological effects
What is Phase 1
This route of drug administration provides 100% bioavailability
What is Intravenous (IV)
What is the primary treatment for acute metal toxicity?
Chelator or Chelation
What class of antibiotics prevents the synthesis of the peptidoglycan cell wall by targeting the active site of penicillin binding proteins (PBPs)?
Beta-Lactams
Penicillins, Cephalosporins, Carbapenams, Monobactams
This loop diuretic exerts its effects on the NKCC co-transporter of the thick ascending limb of Henle
What is Furosemide
What capillary structure allows only highly lipophilic drugs to enter the brain?
Blood Brain Barrier (BBB)
Drug passage through the BBB is determined by three factors: 1) lipophilicity 2) molecular size 3) P-gp efflux pumps
What process is carried out by the liver in which drugs absorbed in the GI tract are initially activated or inactivated before entering circulation?
First-Pass Metabolism
What is the functional unit that is a precursor for peptidoglycan cell wall synthesis?
Murein (NAM+NAG)
Daptomycin's mechanism of action targets what specific structure?
The Cell Membrane
Daptomycin can target both bacterial and host cell membranes; myocytes/muscle tissue have lots of membrane, hence myopathy/rhabdomyolysis as side effects
This non-beta lactam antibiotic is useful for staphylococcal infections (e.g. MRSA and MRSE); however, resistance mechanisms do arise.
What is Vancomycin
Vancomycin resistant strains of staph. aureus can arise, particularly in healthcare settings.
SGLT2 is a co-transporter that requires energy from a sodium gradient for the reabsorption of glucose by the kidney. What transport process does SGLT2 use?
Secondary Active Transport
Movement of sodium down its concentration gradient is coupled to the transport of glucose
A patient receives Furosemide 40 mg PO. After 1 hour, the drug concentration in the blood is measured giving an apparent volume of distribution of 3.5 L. What is the most likely body fluid compartment where furosemide is distributed?
Plasma or Vascular compartment
Furosemide (loop diuretic) in the body is preferentially bound to albumin and therefore mostly confined to plasma.
Recall:
TBW = 42 L
ECF = 14 L
ISF = 10.5 L
Plasma = 3.5 L
What type of pesticide interferes with nerve action potentials leading to uncontrolled firing causing tremors and seizures?
Chlorinated Hydrocarbons or DDT
DDT (featured in Silent Spring by Rachel Carson) is a type of chlorinated hydrocarbon
Which antibiotic is used as a "last choice" for multiple drug resistant pathogens and side effects can include anemia and "gray baby syndrome"?
Chloramphenicol
A patient with history of hypertension and heart failure has been on an ENaC channel blocker long-term for several years. What medical term correctly describes a likely physiological side effect of this diuretic?
Hyperkalemia
ENaC channel blockers (i.e. Amiloride, Triamterene) are "K-sparing" diuretics because they secondarily inhibit ROMK activity (decrease K+ secretion and increase K+ retention)
What 3 variables are inversely proportional to the rate of flux according to Fick's Law of Diffusion?
Molecular Size, Fluid Viscosity, and Barrier Thickness/Distance
Fick Law: J = D*A*(ΔC/dx)
D ∝ temperature
D ∝ 1/MW
D ∝ 1/viscosity
This compound will increase urine pH and promote the excretion of acidic drugs
What is Sodium Bicarbonate
A bacterium with teichoic acid would stain what color after gram staining with crystal violet?
Purple/Blue.
Gram positive bacteria have thick peptidoglycan cell walls containing teichoic acid. The thick peptidoglycan layer retains the dark purple crystal violet stain. In contrast, gram negatives have an outer membrane that prevents crystal violet from penetrating
On your medical mission trip to a developing country, you unfortunately develop tuberculosis and are immediately given a combination of antibiotics. You wake up the next morning, surprised by the sight of your red colored urine. What antibiotic is the culprit?
Rifamycin or Rifampin
What specific CYP450 enzyme metabolizes Warfarin and activity is induced by charcoal-broiled beef?
CYP1A2
What equation (derived from the Henderson-Hasselbalch equation) gives the ratio of ionized to un-ionized form of a weakly basic drug?
10pKa-pH = [HB+]/[B]
For Weak Acids: 10pH-pKa = [A-]/[HA]
What type of rate of elimination is dependent on drug concentration such that the half-life is always constant and defined by t1/2=0.693/ke?
First-Order Kinetics
What concept defines the evolutionary differences between prokaryotes and eukaryotes which enable antimicrobial agents to target bacteria without harming host cells?
Selective Toxicity
Fluoroquinolones target which 2 specific enzymes? (bonus 200: What process is inhibited?)
What is DNA gyrase and topoisomerase (DNA synthesis)
What penicillin derivative most effective against pseudomonas sp., a gram-negative rod?
Piperacillin
(Pseudomonas is a HY bacteria so knowing which abx are effective against it is clinically useful)