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 .

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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 .

cortisone Eye. birth control patches. hormones. nitroglycerine patches. nicotine patches Topical application ± sunscreen. ear. nose drops Vaginal or rectal (PR) .Local Administration     Adhesive patches ± pain control. antibiotic ointments.

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

kidneys .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.

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. or brain abscess Medications must be able to penetrate the blood brain barrier Medications usually given intravenous . encephalitis.

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. .

urine. stool  Most drugs metabolized in the liver by cytochrome P450 (CYP) .Metabolism  Method by which the drugs are inactivated or biotransformed by the body Active drugs contain metabolites that are excreted ± skin.

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 .

laboratory values are important!  Serum drug levels indicate the onset.Yes. peak and duration of the drug action .

lithium) To check to see if the drug is at therapeutic levels ± seizure medications When drug overdose is suspected . aminoglycoside antibiotics.Do we do serum drug levels for all drugs?   No When do we need them? Drugs with narrow margin of safety (digoxin.

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 .

D ± three times a day Q4 hours ± every four hours Q 12 hours ± 9 am and 9 pm .Why is this important?  Half-life determines how often a drug is given Daily in the morning At bedtime Q.I.four times a day T.I.D .

Pharmacodynamics Drug actions on target cells and resulting cellular biochemical reaction of in simple terms ³What 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.

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 .Variables that effect drug action  Dosage of the drug refers to frequency.

Drug Dosing  Often the first dose is higher in an effort to bring the therapeutic blood serum levels up quicker .

patch etc . sublingual (under the tongue).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).

Drug ² 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 ² 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 .

000 to 98.Medication Errors   44.000 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 .

safe dose. frequency Date. route. and side effects The nurse should know why the medication is ordered .Medication Orders       Full name of client Generic or trade name of drug Dose. time and signature of provider The nurse will need to look up the medication ordered to know it¶s classification. action. how to administer.

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. pounds. ounces. drams. and quarts . pints.

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 .

when talking about water or similar liquids.Milliliters  mL = milliliter. it is equivalent to one cubic centimeter. This is a VOLUME measurement. it is 1/1000 of a liter. .

Cubic Centimeter  cc = cubic centimeter. it will hold ~5mL of liquid in it. This is also a VOLUME measurement. Most syringes measure their capacity in cc's. . If you have a 5cc syringe.

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 .

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

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