ANSWERS GRADED A+
✔✔Irreversible Antagonist - ✔✔o Bind permanently to the receptor binding site;
therefore they can not be overcome with agonist.
✔✔Proteins or Glycoproteins - ✔✔o Present on cell surface, on an organelle within the
cell, or in the cytoplasm.
o Finite number of receptors in a given cell.
o Receptor mediated responses plateau upon saturation of all receptors.
o Receptors can be recycled/down-regulated (to be revisited in pain pharmacology).
✔✔Effects of Disease on Pharmacodynamics - ✔✔· Altered response due to:
o Acid-base status
o Electrolyte abnormalities
o Altered intravascular volume
o Tolerance
✔✔Using PK/PD Principles for Drug Therapy Management - ✔✔1. Target-Effect
Strategy
2. Target-concentration strategy
✔✔Target-Effect Strategy - ✔✔o Predetermined efficacy endpoint
Example: Reduction of blood pressure to 120/80 mmHg with Lotensin/benazapril
o Titrate drug to desired effect
· Monitor for efficacy
· If plateau occurs, may need to add additional drug or choose alternative agent.
· Monitor for toxicity
· May require decrease in dose or alternative agent.
✔✔Target-concentration strategy - ✔✔o Predetermined concentration goal
§ Based on population-based PK
§ Target concentration based on efficacy or toxicity
o Know the PK of the drug you are prescribing
§ Presence of an active metabolite?
§ Should the level of the active metabolite be measured?
§ Zero-order or first-order kinetics?
· Does it change with increasing serum concentrations?
✔✔Synergistic - ✔✔when two drugs, used together, have an effect larger than the sum
of each drug's effect(s) by itself
✔✔Rational therapeutics - ✔✔o Knowing, understanding, and implementing general
principles and specific facts about classes of drugs and individual drugs.
, o seeks to maximize therapeutic responses while minimizing therapeutic failures and
medical errors that occur because of "therapeutic wrongs"
(prescribing/dispensing/administering the wrong drug/ wrong dose to the wrong patient
at the wrong time)
✔✔Beta adrenergic blocking agents - ✔✔propranolol
metoprolol
esmolol (short-acting)
atenolol
✔✔Calcium channel blockers - ✔✔amlodipine
nicardipine
verapamil
felodipine
nifedipine
diltiazem
✔✔Angiotensin converting enzyme inhibitors - ✔✔lisinopril
captopril
enalapril
ramipril
benazeprilf
fosinopril
✔✔Side effects of ACE inhibitors - ✔✔cough and angioedema.
✔✔Angiotensin II receptor blocking agents - ✔✔valsartan,
losartan
candesartan
irbesartan
✔✔Angiotensin II Receptor Blockers (ARBs) MOA - ✔✔Lower blood pressure by
blocking the angiotensin II enzyme from causing vasoconstriction
✔✔Alpha-1 adrenergic stimulation - ✔✔results in vasoconstriction and increased blood
pressure
✔✔Alpha-1 adrenergic blockade - ✔✔results in vasodilation and reduced blood
pressure
✔✔Beta-1 adrenergic stimulation - ✔✔results in increased heart rate, increased blood
pressure and increased cardiac output.
✔✔Beta-1 selective blocking agents - ✔✔reduced heart rate, reduced blood pressure
(by reducing vascular smooth muscle tone) and reduced cardiac output.