Basic Concepts of

Pharmacology

Jan Bazner-Chandler
CPNP, CNS, MSN, RN
Cellular Physiology

 What does a cell do?

 Exchange material
 Obtain energy from nutrients
 Synthesize hormones, neurotransmitters,
enzymes, structural proteins and other complex
molecules
 Duplicate themselves
Pharmacokinetics

 Drugs movement through the body to reach

sites of action, metabolism and excretions
Drug Transport

 What does this have to do with drug

administration?
 Drugs must reach and interact with or cross
the cell membrane to stimulate or inhibit
cellular function
Key Concepts

 Absorption
 Distribution
 Metabolism
 Excretion
 Serum Drug Levels
 Serum Half-life
Oral Drugs

 Dosage is determined by how much of the

drug is required to be taken by mouth to
given the desired affect.
 Bioavailability – portion of the drug that
reaches the systemic circulation
Oral Drugs

 Drug needs to be taken orally – pill v liquid –

size of pill – make up of pill
 Time in the stomach – is the stomach empty
– full – does it make a difference on how drug
is absorbed
 Small intestine – large surface area for
absorption of nutrients and minerals
Amoxicillin Suspension
Amoxicillin Chewable Tablets
Amoxicillin Tablets
What else might influence oral drug
absorption?
 Food in stomach
 Certain juices – grapefruit juice
 Milk – binds with molecules of some drugs so
that the drug is never absorbed
 Orange juice – enhances absorption of iron
taken orally
 The coating on the tablet: chewable, enteric
coated (breakdown occurs in small intestine),
slow release capsules
IM and Sub-Q

 IM – intramuscular – into a muscle group –

pain medications / antibiotics / vaccinations
 Sub-Q – into subcutaneous tissue –
(Coumadin / heparin / Lovenox) (TB test)
Subcutaneous Injection
Intramuscular or IM
Local Administration

 Adhesive patches – pain control,

nitroglycerine patches, hormones, birth
control patches, nicotine patches
 Topical application – sunscreen, antibiotic
ointments, cortisone
 Eye, ear, nose drops
 Vaginal or rectal (PR)
Nitroglycerine Ointment
Nitroglycerine Patch
Eye Drops or Eye Ointment
Ear Drops
Rectal Suppositories
Rectal Suppositories

 Excellent route of administration of

medications for the client that is:
 Vomiting / nausea
 Refuses to take medication PO
 Difficulty swallowing a medication
 Infants – fever or pain medications
Inhaled

 Asthmatic drugs
 Anesthetics
Distribution

 Transportation of drug molecules within the

body
 Drug needs to be carried to the site of the
action
 Need blood to circulate the drug
 Heart, liver, kidneys
Key Concepts of Distribution

 Protein binding – drug molecules need to get

from the blood plasma into the cell
 Protein binding allows part of the drug to be
stored and released as needed
 Some of the drug is stored in muscle, fat and
other body tissues and is gradually released
into the plasma
Just how does the drug get into the cell?

 Drug must pass though the capillary wall

 Blood brain barrier – very effective in keeping
drugs from getting into the central nervous
system or CNS – limits movement of drug
molecules into brain tissue
Blood Brain Barrier

 This is especially important when treating

infections of the brain such as meningitis,
encephalitis, or brain abscess
 Medications must be able to penetrate the
blood brain barrier
 Medications usually given intravenous
Three ways to get in!

 Direct penetration of the membrane

 Protein channels
 Carrier proteins
# 1 Lipid Soluble Drugs

 Lipid soluble drugs are able to dissolve in the

lipid layer of the cell membrane
 No energy expended by the cell
 Passive diffusion
 Oral tablets or capsules must be water soluble to
dissolve in fluids of the stomach and small
intestine
#2 Protein Channels

 Most drug molecules are to big to pass in to

the cell via the channels – small ions such as
sodium and potassium use the protein
channels but their movement is regulated by
gating mechanisms – only small amounts
allowed
# 3 Carrier Proteins

 Molecule needs to bind with a protein that will

transport it from one side of the cell
membrane to another – a drugs structure
determines which carrier will transfer it.
Metabolism

 Method by which the drugs are inactivated or

biotransformed by the body
 Active drugs contain metabolites that are excreted
– skin, urine, stool
 Most drugs metabolized in the liver by
cytochrome P450 (CYP)
What can stop this process?

 Enzyme inhibition
 Other drugs
 Combination drugs
 Liver disease
 Impaired blood circulation in person with heart
disease
 Infant with immature livers
 Malnourished people or those on low-protein diets
An important concept!

 First-pass effect – some drugs are

extensively metabolized or broken down in
the liver and only a part of the drug is
released into the systemic circulation
 This is why dosage is important – how much
drug needs to be taken in to give the desired
effect and how often does it need to be taken
Excretion

 Refers to the elimination of the drug from the

body
 Requires adequate functioning of the
circulatory system and organs of excretion
 Kidneys
 Bowels
 Lungs
 Skin
Laboratory Values

 Laboratory values reflecting function of liver

and kidneys need to be looked at.
 BUN and Creatinine – kidney function
 LFT or liver function tests:
 ALT – alamine aminotransferase (elevated in hepatitis)
 AST or SGOT– aspartate aminotransferase – elevated
in liver disease
 ALP – elevated in biliary tract disease
 Bilirubin levels – infants – gallstones in adults
Serum Drug Levels

 Laboratory measurement of the amount of

drug in the blood at a particular time
 A minimum effective concentration (MEC)
must be present before a drug exerts its
action on a cell.
Toxic Levels

 Excessive level of a drug in the body

 Single large dose
 Repeated small doses
 Slow metabolism which allows drug to accumulate
in the body
 Slow excretion from the body by the kidneys or
gastrointestinal tract
Yes, laboratory values are important!

 Serum drug levels indicate the onset, peak

and duration of the drug action
Do we do serum drug levels for all
drugs?
 No
 When do we need them?
 Drugs with narrow margin of safety (digoxin,
aminoglycoside antibiotics, lithium)
 To check to see if the drug is at therapeutic levels
– seizure medications
 When drug overdose is suspected
Important concept!

 Serum half-life or elimination half-life is the

time it takes the serum concentration of the
drug to reach 50%
 A drug with a short half-life requires more frequent
administration
 A drug with a long half-life requires less frequent
administration
Why is this important?

 Half-life determines how often a drug is given

 Daily in the morning
 At bedtime
 Q.I.D - four times a day
 T.I.D – three times a day
 Q4 hours – every four hours
 Q 12 hours – 9 am and 9 pm
Pharmacodynamics

Drug actions on target cells and resulting

cellular biochemical reaction of in simple
terms “What the drug does to the body”.
Receptor Theory

 Most drugs exert their effects by chemically

biding with receptors at the cellular level.
 Receptors are proteins located
 on the surfaces of cell membranes
 within the cells
What do the receptors do?

 The receptors are often described as the lock

into which the drug molecule fits as a key.
 All body cells do not respond to all drugs
even when all the cells are exposed to the
drug.
More is not better!

 Number of receptors site available will effect

drug action so giving a higher dose does not
necessarily produce additional
pharmacological effects.
Variables that effect drug action

 Dosage of the drug refers to frequency, size,

and number of doses
 Ibuprofen (generic) or Advil (trade name)
 Dosage = 250 mg per tablet
 Tablets are enteric coated
 Children over 12 years or adults take 1 to 2 tablet
every 4 to 6 hours
 Not to exceed 6 tablets in 24 hours unless
prescribed by a doctor
Drug Dosing

 Often the first dose is higher in an effort to

bring the therapeutic blood serum levels up
quicker
Route

 Route of administration does affect drug

action and client response
 IV the best for rapid response – drug put directly
into the blood stream
 IM in 10 to 15 minutes as it is absorbed into the
blood stream through the muscle
 Topical application of a drug depends on where
applied – skin (condition of skin), sublingual
(under the tongue), patch etc
Drug – Diet interaction

 Food can slow absorption

 Food substances can react with certain drugs
 How to give medication is information
provided in you drug manual
Drug – Drug Interaction

 Some drugs taken together will enhance

each other
 Tylenol with codeine
 Some drugs taken together will interfere with
another drugs actions
 Some drugs are given to decrease or reverse
the toxic effects of a drug
 Narcotic antidote is naloxone
Client Variables

 Age
 Body weight
 Gender
 Ethnicity
 Co-existing medical conditions
Drug Tolerance

 Body becomes accustomed to drug over

period of time
Adverse Effects
 Undesired response
 Allergic reaction
 Drowsiness
 Nausea / vomiting / GI upset
 Liver or kidney damage
 Fevers
 Drug dependency
 Cancinogenicity – ability to cause cancer
 Teratogenicity – cause damage to fetus
Administering Medications

 Five rights
 Right drug
 Right dose
 Right client
 Right route
 Right time
Know your drug

 Clients expect you to be knowledgeable

 You gain this knowledge be looking up
medications
 Drug hand book
 PDA
 Pharmacist
Legal Responsibilities

 The nurse is responsible for

 safe and accurate administration
 having sufficient drug knowledge to recognize and
question erroneous orders
 actions delegated to other persons – LVN cannot
give IV meds
 monitor clients response to a medication
 following safe practices – the five rights
Medication Errors

 44,000 to 98,000 deaths occur each year in

the USA because of medical errors
 JCAHO has set standards that hospitals must
follow to decrease medication errors
 Computerized systems
 Bar coding of medications
 Patient identification system
Medication Systems

 Each facility has a system for administering

medication
 Be familiar with this process
 Need to learn at each new facility
 Basics of medication administration
guidelines should always be observed
Medication Orders
 Full name of client
 Generic or trade name of drug
 Dose, route, frequency
 Date, time and signature of provider
 The nurse will need to look up the medication
ordered to know it’s classification, safe dose,
action, how to administer, and side effects
 The nurse should know why the medication
is ordered
Need to Memorize

 Systems of measures
 Table 3-3 Equivalents
Metric System

 Meter is used for linear measure, gram for

weight and liter for volume
Apothecary System

 Grains, minims, drams, ounces, pounds,

pints, and quarts
Household measures

 Drops, teaspoons, tablespoons and cups

 Important since this is often how people take
medications
Units

 mEq – drugs ordered in number of units per

dose
 Insulin
 heparin
Milliliters

 mL = milliliter. This is a VOLUME

measurement. it is 1/1000 of a liter. when
talking about water or similar liquids, it is
equivalent to one cubic centimeter.
Cubic Centimeter

 cc = cubic centimeter. This is also a

VOLUME measurement. Most syringes
measure their capacity in cc's. If you have a
5cc syringe, it will hold ~5mL of liquid in it.
mL and cc’s
 1 mL = 1cc
 1 cc = 15 to 16 minims
 1 cc = 15 to 16 drops

 Fluids are generally written in cc’s to

standardize the abbreviation – you may see
mL’s written but this abbreviation is being
eliminated
cc’s and household measures

 5 cc = 1 tsp (teaspoon)
 15 cc = 1 tbs (tablespoon)
 30 cc = 1 oz (ounce) = 2 tablespoons
 240 cc = 8 oz or 1 cup
Milligrams

 mg = milligram. This is a WEIGHT

measurement. It is 1/1000 of a gram. the
amount of chemical substance is often
measured in milligrams. For injectable
solutions, this will be reported as a
concentration of weight to volume, such as
mg/ml (milligrams per milliliter).