The University of the West Indies

Faculty of Medical Sciences

The UWI School of Nursing, Mona
Pharmocodynamics

1. This looks at how the drug changes the body, it looks at the mechanisms of drug action and the
relationship between drug concentration and responses in the body.

Drug actions

 To replace or act as substitutes for missing chemicals

 To increase or stimulate certain cellular activities
 To depress or slow cellular activities
 To interfere with the functioning of foreign cells such as invading microorganisms or neoplasms

2. Drugs are thought to act at specific areas on cell membrane called receptor sites, these sites
react with certain chemicals to cause an effect within the cell.

3. Some drugs interact directly with receptor sites to cause the same activity that natural chemicals
would cause at that site. These drugs are called agonists e.g. insulin.

4. Other drugs act to prevent the breakdown of natural chemicals that are stimulating the receptor
site

5. Other drugs act to prevent the breakdown of natural chemicals therefore the cell function is
inhibited because the drug occupies the receptor sites. These drugs are called antagonist

6. Drugs can also cause their effects by interfering with the enzyme system that acts as catalysts
for various chemical reactions. If a single step in one of the many enzyme system is blocked,
normal cell function is disrupted. Acetazolamide (Diamox) is a diuretic that blocks the enzyme
carbonic anhydrase, which subsequently causes alterations in the hydrogen ion and water
exchange system in the kidneys as well as in the eye

7. Some drugs have selective toxicity, in that the drug has the ability to attack only those systems
found in foreign cells. Penicillin, an antibiotic used to treat bacterial infections has selective
toxicity as it only affects the enzyme system unique to the bacteria causing bacterial cell death
without disrupting normal human cell functioning

8. However some drugs, while destroying foreign cells also destroys normal human cells.

Pharmacokinetics
 1. Absorption – refers to what happens to a drug from the time it is introduced into the
body until it reaches circulating fluids and tissues.
 The length of time a drug takes to produce its effect is dependent on the
absorption
 The more rapid the absorption the more rapid the onset of the drugs
 Drugs are absorbed into cells by passive diffusion and active transport
2. Distribution – transportation of the drug from the site of absorption to the site of action
 The amount blood flow to tissues determines the distribution of the drug
 The heart, liver, kidney and brain receive the most blood supply, while skin, bone
and adipose tissue receive a lower blood supply
 The physical property of the drug also influences its distribution
 Lipid solubility determines how quickly a drug is distributed in the body
 Drugs that are not lipid soluble cannot cross the blood –brain barrier
 Some tissues have the ability to accumulate and store drugs after absorption,
such as bone marrow, teeth eyes and adipose tissue. These tissues are said to
have an affinity for certain medications. Therefore distribution is affected.
 Drugs that bind to protein molecules affect the distribution of the drug. the drug
is unable to reach the target tissue because the protein molecule is large and so
the drug which is bound to protein cannot cross capillary membrane for
distribution
 Please read up on the blood-brain barrier and the fetal-placenta barrier

Metabolism (Biotransformation)

 This is the process of converting the drug into a new less active form and therefore more
easily removed from the body

 The liver is the primary site of drug metabolism in the liver is accomplished by the
hepatic microsomal enzyme system

 Changes in the function of this system can significantly impact on the metabolism of a
drug and so if the liver is not functioning properly then the drug will not be metabolized
as it should be and toxic levels could develop

 Some drugs are totally biotransformed to an inactive form in the liver before they ever
reach the general circulation- first pass effect. A large number of oral drugs are rendered
inactive by the hepatic reactions therefore alternate routes of delivery that bypass the
first pass effect must be considered for these drugs

Excretion
  The rate at which a drug is excreted from the body determines its concentration in
the blood stream and tissues

 Liver disease or renal failure often increases the duration of drug action in the body
because the illness interferes with the natural excretion mechanisms

 Clients with renal failure have a diminished capacity to excrete medications and so
the drug is retained in the body for an extended period

 Doses for these persons must be reduced to avoid toxicity, kidney function must be
close monitored

 The acidity of urine plays an important role in excretion, some drugs are excreted
more quickly in an acidic urine and others in an alkaline urine.

 To speed up the excretion of an acidic drug e.g. aspirin (like in the case of aspirin
over dose) the patient can be given sodium bicarbonate which ionizes the aspirin
and causes it to be excreted more readily

 To speed up the excretion of an alkaline drug e.g. diazepam (like in the case of an
over dose) the patient can be given ammonium chloride. This will acidify the filtrate
and increase the excretion of the drug

Reference

Adams, M.P., Holland, L.M. & Bostwick, P.M. (2014). Pharmacology for nurses: A pathological approach.
New Jersey: Prentice Hall Chapter 5

Karch, A.M. (2006). Focus on nursing pharmacology (3 rd ed.). Philadelphia: Lippincott Williams & Wilkins.
Chapter 3