NR 668 – Week 4 Psychopharmacology, Psychiatric Mental Health Nurse Practitioner Course,
Lecture Summary and Medication Management Concepts
Pharmacodynamics - ✔✔How the drug effects the body
-therapeutic vs. side effects
• Is it stimulating?
• Is it depressing?
• Does it block something?
-Onset of action
• Route, Dosage
-Duration of action
• Redistribution rate, metabolism rate and excretion rate
-Mechanism of action
• Drugs simply speed up or slow down what is already occurring in the body
-Efficacy
• (Intrinsic activity) After binding, the drugs capacity to cause an effect
-Potency
• The amount of a drug needed to produce a given effect
efficacy examples - ✔✔-Agonist (Efficacy = 100)
-Partial Agonist (Efficacy = > 0 < 100)
-Antagonist (Efficacy = 0.0)
-Inverse Agonist (Efficacy = < 0)
Agonist: - ✔✔Compounds which give maximal response after receptor occupation and
activation.
-Example: Oxycodone
,Partial Agonists: - ✔✔Compounds which activate the receptor but not at the maximal
response.
-Example Buprenorphine (Suboxone) or Buspirone
Antagonist: - ✔✔Blocks the action of an agonist.
-Example: Neuroleptics, Naloxone
Inverse Agonist: - ✔✔Binds to receptor and has the opposite action of an agonist and below
baselinesignal transduction
Pharmacokinetics - ✔✔How the body effects the drug
-Absorption, distribution, metabolism and elimination (ADME)
-Metabolizing the drug via CYP450 through the gut & liver
Bioavailability - ✔✔Absorption: Drugs cross a barrier.
-Involves bioavailability or Quantity of drug reaching circulation/quantityof the drug
administered.
• Our own barriers such as skin and mucous membranes as well as food, molecular weight,
chemical, biological barriers, etc. reduce how much drug is actually absorbed and available. IV
route has 100% bioavailability. All other routes <100%
First pass metabolism - ✔✔-reduces the concentration of a drug
• travels through digestive system & entering the liver.
• reducing the bioavailability of the drug
rate is reduced by: - ✔✔-Route (IV, PO, Rectum, etc.)
-Dosage (Concentration)
, -Lipid Solubility
Drugs that cross the BBB are _____________ - ✔✔fat soluble
Vd: Volume of distribution = ________ - ✔✔amount of drug/concentration
• large Volume of distribution may indicate the drug distributes extensively into the body
• Vd is a theoretical fluid volume necessary to contain the total amount of a drug at the same
concentration observed in the plasma
A patient who is in renal failure would have a increased or decreased Vd? - ✔✔Increased
because of fluid retention
plasma protein binding - ✔✔-cannot leave the circulation easily
-Free (unbound) crosses membranes
-Two drugs that are both highly protein bound will compete with each other
• The unbound fraction goes through metabolism and is responsible for the pharmacologic
effects
-rapid weight loss may result in drugs being released from fat cells
Drugs that are highly protein bound and have a narrow therapeutic index can be dangerous
because: - ✔✔margin of error between therapeutic and toxic is narrow
Metabolism - ✔✔-Mostly in the liver
-Biotransformation or change it to inactive form or make it more water soluble to facilitate
excretion
• transformed substance is called the metabolite.
Lecture Summary and Medication Management Concepts
Pharmacodynamics - ✔✔How the drug effects the body
-therapeutic vs. side effects
• Is it stimulating?
• Is it depressing?
• Does it block something?
-Onset of action
• Route, Dosage
-Duration of action
• Redistribution rate, metabolism rate and excretion rate
-Mechanism of action
• Drugs simply speed up or slow down what is already occurring in the body
-Efficacy
• (Intrinsic activity) After binding, the drugs capacity to cause an effect
-Potency
• The amount of a drug needed to produce a given effect
efficacy examples - ✔✔-Agonist (Efficacy = 100)
-Partial Agonist (Efficacy = > 0 < 100)
-Antagonist (Efficacy = 0.0)
-Inverse Agonist (Efficacy = < 0)
Agonist: - ✔✔Compounds which give maximal response after receptor occupation and
activation.
-Example: Oxycodone
,Partial Agonists: - ✔✔Compounds which activate the receptor but not at the maximal
response.
-Example Buprenorphine (Suboxone) or Buspirone
Antagonist: - ✔✔Blocks the action of an agonist.
-Example: Neuroleptics, Naloxone
Inverse Agonist: - ✔✔Binds to receptor and has the opposite action of an agonist and below
baselinesignal transduction
Pharmacokinetics - ✔✔How the body effects the drug
-Absorption, distribution, metabolism and elimination (ADME)
-Metabolizing the drug via CYP450 through the gut & liver
Bioavailability - ✔✔Absorption: Drugs cross a barrier.
-Involves bioavailability or Quantity of drug reaching circulation/quantityof the drug
administered.
• Our own barriers such as skin and mucous membranes as well as food, molecular weight,
chemical, biological barriers, etc. reduce how much drug is actually absorbed and available. IV
route has 100% bioavailability. All other routes <100%
First pass metabolism - ✔✔-reduces the concentration of a drug
• travels through digestive system & entering the liver.
• reducing the bioavailability of the drug
rate is reduced by: - ✔✔-Route (IV, PO, Rectum, etc.)
-Dosage (Concentration)
, -Lipid Solubility
Drugs that cross the BBB are _____________ - ✔✔fat soluble
Vd: Volume of distribution = ________ - ✔✔amount of drug/concentration
• large Volume of distribution may indicate the drug distributes extensively into the body
• Vd is a theoretical fluid volume necessary to contain the total amount of a drug at the same
concentration observed in the plasma
A patient who is in renal failure would have a increased or decreased Vd? - ✔✔Increased
because of fluid retention
plasma protein binding - ✔✔-cannot leave the circulation easily
-Free (unbound) crosses membranes
-Two drugs that are both highly protein bound will compete with each other
• The unbound fraction goes through metabolism and is responsible for the pharmacologic
effects
-rapid weight loss may result in drugs being released from fat cells
Drugs that are highly protein bound and have a narrow therapeutic index can be dangerous
because: - ✔✔margin of error between therapeutic and toxic is narrow
Metabolism - ✔✔-Mostly in the liver
-Biotransformation or change it to inactive form or make it more water soluble to facilitate
excretion
• transformed substance is called the metabolite.
