Pharmacokinetics

Learning Objectives

 Be able to explain pharmacokinetics

 Be able to describe the various routes of drug administration
 Understand why some methods may be more optimal for particular clients
 Understand the concept of drug diffusion
 Describe the blood-brain barrier and its function
 Describe the concept of half life and steady state
 Described titration and maintenance dose
 Discuss primary flaws with chemical imbalance theory
 Describe the types of drug tolerance
 Understand the role and relationship between the kidneys and liver in drug metabolism
Pharmacokinetics

How the body acts on psychotropic

medications; the processes by which
drugs are absorbed by the body,
distributed within the body, metabolized
and then excreted.

This Photo by Unknown Author is licensed under CC BY-NC

Drug Absorption

This Photo by Unknown Author is licensed under CC BY-SA

 Absorption –How the drug gets into the bloodstream and
distributed throughout the body, with goal to pass the blood-brain
barrier and into the brain.

4 Main Processes in Distribution – The movement of a drug to and from the blood and
into various tissues of the body
Pharmacokinetics
Metabolism – The breakdown of a drug in the body

Elimination – The removal of a drug from the body

Absorption
Routes of Administration

Oral Administration
1. Most common
2. Taken in pill or liquid
3. Must dissolve in stomach before passing through tract to reach the bloodstream to make
its way across the blood-brain barrier
4. The more fat soluble a drug (lipophilicity), the better able to cross the lipid barriers of
the intestines, blood vessels and neurons.
5. Disadvantages
1. Takes longer to get into the blood stream
2. Absorption rates are determined by body type, age, sex of client and gastro side effects
Absorption
Routes of Administration
Inhalation
1. Predictable
2. Direct route to the pulmonary system
3. Sent directly to the brain via capillaries
4. Most commonly administered via inhaler
5. While vaporizers “vaping” delivers drugs such as nicotine and cannabis with
fewer harmful toxins like carbon monoxide, new findings reveal added
substances such as Vitamin E acetate may be responsible for the recent increase
in vaping illnesses.
Absorption
Routes of Administration
Injection
1. Subcutaneous – just below the skin, slow and prolonged (hormones, Imitrex –
migraines)
2. Intramuscular – slow acting but produce more absorption (antipsychotics,
Avonex for MS)
3. Intravenous – most rapid and precise as is direct into bloodstream *most lethal
potential for overdose
4. Epidural – primarily used for spinal anesthetics such as during childbirth *no
psychotropic medications are administered this route
Absorption
Routes of Administration
Transdermal Administration
1. Drug is administered via patch technology
2. Attached to skin via adhesive
3. Skin is resistant to water passing through but allows fat soluble molecules
4. Allows for controlled rates of absorption
5. Can cause skin irritation
6. Examples include nicotine patches, opioids for pain, contraceptives
Absorption
Routes of Administration
Rectal Administration
1. Less efficient than oral or inhaler
2. Useful for gastro sensitive patients
3. Obvious disadvantages (less desirable route)
4. There are no rectally administered psychotropic medications
Absorption
Routes of Administration
Mucus Membrane
1. Administered via mouth or nose
2. Direct absorption into the bloodstream
3. Advantageous for children trouble swallowing pills or with injection
4. Common drugs include nicotine chews, decongestants, and flu vaccinations
Getting to the Blood Stream

Cell Membrane Permeability refers to the rate of diffusion of molecules through the
membrane. Which membrane it passes through is determined by the route of
administration
Terms
o Phospholipid biolayer are
• two layers of lipid molecules that form a polar membrane, that make up the skin,
muscle and fat cells
• Major components of cell membranes
o Diffusion is the process in which drug molecules pass through gaps of tightly
packed capillaries
Blood-Brain Barrier
 Is made of glial cells with high fat content
 Glial cells surround neurons providing support for and insulation between them, the most
abundant cell types in the CNS.
 Astrocyte is a type of glial cell that makes up the gap known as the blood-brain barrier.
 Survival function to keep foreign elements (eg toxins) out of the brain
https://youtu.be/noWwbvmdhL0

Placental barrier
 Allows for nutrients and oxygen to pass from the mother’s blood to the baby’s blood.
 Breast-feeding has inherent risks to babies as even small doses of medications can lead to toxic
amounts.
Drug Distribution

Drug Binding is the process in which drug molecules will bind to neurotransmitter
receptor sites.

BREAK OUT GROUP DISCUSSION

When chemical interventions alleviate or decrease symptoms, does this mean the
client has a chemical imbalance?

https://www.medicalnewstoday.com/articles/326475
Drug Distribution

 Your body circulates your entire blood volume once per minute

 The route of administration will determine the amount of the drug to reach the bloodstream.

 First pass metabolism is the process when administered orally, the drug is reduced to enzymes
in the gut wall, carried through veins into the liver for further metabolism of the drug.

 Once absorbed into the bloodstream, a drug circulates throughout the body, a process which
may contribute to side effects eg antidepressant medication causing nausea by their effects on
the serotonin receptors rich in the digestive track.
5 Important Pharmacokinetic Terms

Half-life The amount of time required (hours to days) for the initial blood level
of a drug to decrease by 50%, which determines the dosage and
frequency which a drug is prescribed to maintain steady levels in the
body.
Steady state The state when concentration levels reach a plateau in which the
amount being taken is equivalent to what is being eliminated.
Loading dose The initial dose is higher than subsequent dose/s with goal of
achieving therapeutic levels quickly.
Maintenance dose The regular dose that maintains the steady state blood levels in the
therapeutic range.
Titration Balancing (up or down)against the patient’s symptoms
YouTube video
half-life demonstration

https://www.youtube.com/watch?v=8-Qtd6RhfVA
Drug Distribution

Tolerance is defined as the state of reduced responsiveness to the same

dose of the drug.

Dependence is the physical tolerance produced by repeated

administration of a drug along with withdrawal syndrome when the
drug is discontinued.
Drug Distribution
Types of Tolerance

Metabolic tolerance is an increase in the enzymes that metabolize a drug caused by the
presence of that or similarly acting drug (eg nicotine and the neurotransmitter nicotinic)

• Cytochrome P450 enzyme is the most common enzyme system for metabolizing
drugs, produced in the liver to accomplish detoxification (metabolism) of ingested
elements, elevating the enzyme levels to break down the drug more efficiently,
leading to the need for a larger dose; tolerance is determined by the drug, the amount
of the drug, and individual’s body response (eg alprazolam)

• Cross-tolerance is produced when taking a similar drug regularly which results in

the diminished effect of the drug.
Drug Distribution
Types of Tolerance

Cellular tolerance occurs when receptors in the brain adapt to the continued presence of a
drug.
1. Downregulation is when the neuron decreases the number and/or sensitivity of receptors
because of the presence of the drug.
2. Upregulation involves neurons increasing the number of receptors.

Associative tolerance is where one will demonstrate tolerance in some, but not all settings,
such as conditioned stimuli response.

Behavioral tolerance states that when learning a task under the influence of a drug, they tend
to perform better at that task in subsequent engagement in that task when under the influence
of the drug than when sober.
Drug Elimination
Termination of drug action refers to the routes through which a drug is eliminated from
the body typically through the skin, lungs, kidneys, and bile (produced by the liver).

The majority of drugs are excreted by the kidneys by converting them into more water-
soluble compounds.

Most psychotropic drugs have to be fat soluble to pass the blood-brain barrier;

Fat soluble drugs easily cross the membranes of the renal system.

Because kidneys do not completely break down psychotropic medications, the liver will
pick up reabsorbed medications and transform them with enzymes to make them less fat
soluble to allow for excretion in the urine.
Case Study Break Out Discussion
A 53-year-old female is on a regimen of Lithium (mood stabilizer) and Seroquel (atypical
antipsychotic) for Bipolar I Disorder.

She was stable for 6 months without symptoms, despite side effects of weight gain and sedation.

She unexpectedly developed confusion, tremor and agitation.

Lithium levels were shown to be elevated at toxic concentration levels

One week before laboratory testing of her levels, she began taking Tylenol despite warnings about
over the counter medication use without her doctor’s approval.

According to her doctor, Tylenol was reducing urinary clearance of lithium, raising her levels
leading to toxicity.
Case Study Break Out Discussion
Questions about the case

1. Does this case represent an example of pharmacokinetics? Why?

2. Describe what happened to this patient / client once she began
taking Tylenol.
3. How could a nonmedical mental health professional assist this
client with remembering restrictions related to her medication?
Review Questions
1. Define pharmacokinetics

2. Name and describe the 4 main processes of pharmacokinetics

3. Name the 6 routes of administration and explain some advantages /

disadvantages of each.

4. Why is important that psychotropic medications be highly fat soluble?

5. Describe the blood-brain barrier, its function, what it is made of, and how
it affects psychotropic medications.
Review Questions
6. What is the relationship between a drug half-life and the steady state of the
same drug?

7. What is titration? Why is it relevant?

8. What is meant by a maintenance dose?

9. List and describe the different types of drug tolerance

10. What is the relationship between the liver and the kidneys in metabolizing
and excreting drugs?
This Photo by Unknown Author is licensed under CC BY-NC-ND