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HLTEN507C Administer and monitor medications in the work environment

Pharmacodynamics and pharmacokinetics

HLTEN507C Administer and monitor medications in the work environment

Pharmacology - study of the way in which the function of living organisms is affected by chemical agents (i.e. study of actions & effects). Clinical Pharmacology therapeutic uses of medications/chemical substances on living organisms & treatment of disease states.

Pharmacodynamics and Pharmacokinetics

Pharmaceutics the science of formulating drugs.

Pharmacokinetics
Pharmacokinetics What the body does to drugs Studies the absorption, distribution, metabolism and excretion of drugs Pharmacodynamics What drugs do to the body Studies the interaction the drug with the specific molecules and chemical found in the body

What the body does to drugs


Movement of the drug within the body there are 4 stages of drug administration Absorption Distribution Metabolism Excretion

Absorption
The process by which a drug moves into the blood stream. Rate and amount of drug absorbed depends on: Degree of blood flow to the area Solubility of the drug (lipophilic drugs move more readily across cell membranes) Route of administration - Intravenous (IV) is faster than Intramuscular (IM), then Subcutaneous (subcut) which is faster than Oral

Factors affecting absorption

Formulation e.g. Liquid / slow release etc Presence or absence of food in the stomach Gastric motility Presence of enzymes, bile salts

The pharmaceutical industry has numerous ways of enhancing drug absorption including changing pH, formulation of drug etc.

Holmesglen 2013

HLTEN507C Administer and monitor medications in the work environment

Pharmacodynamics and pharmacokinetics

Drug absorption

Distribution
The process whereby a drug is transported from its site of absorption to its site of action. Vascular areas, such as the major organs, will receive the drug sooner than skin and muscles Distribution is affected by: Chemical and physical properties of the drug Protein binding capacity drugs temporarily bind with proteins to move around the body but it is the free drug which produces the physiological change

http://www.youtube.com/watch?v=xiuWdJYyIKs&feat ure=BF&list=PLE66C8741BD8D6329&index=1

Barriers to Distribution
Blood brain barrier Protective prevents harmful substances that may be present in the blood from entering the brain Some do cross Produce side effect such as sedation from antihistamines Placental & testicular Incomplete physical barrier Relatively non-selective May cause congenital malformations Not much known about testicular barrier

Distribution

http://www.youtube.com/watch?v=kLvYCOSnPDc&fea ture=BF&list=PLE66C8741BD8D6329&index=4

Metabolism
Process whereby a drug is converted to a less active form so that it can be excreted. Most metabolism takes place in the liver and involves enzyme action on the drug (P-450) Metabolism is altered in clients with liver disease, the young and the elderly. Consequence - an accumulation of the active drug in the system leading to toxicity

First pass metabolism


Drugs absorbed from the gastro-intestinal tract enter the hepatic portal system where some or all of the drug may be broken down, reducing the availability of drug for therapeutic use This is known as first-pass effect (metabolism) Some drugs are almost fully destroyed during first pass metabolism (glyceryl trinitrate) First pass effect is the reason why oral and parenteral doses are not equal Drugs given by the parenteral route bypass first pass metabolism

Holmesglen 2013

HLTEN507C Administer and monitor medications in the work environment

Pharmacodynamics and pharmacokinetics

Excretion
Process by which drugs are eliminated from the body Sites of excretion: Kidney: main organ of excretion Liver: Bile -> Intestine -> Faeces Lungs e.g. alcohol, anaesthetic gases Exocrine Glands: relatively few drugs e.g. some cytotoxics active metabolites on the skin Breast Milk some drugs can be excreted Excretion is determined by the chemical composition of the drug

Factors influencing Pharmacokinetics

Developmental factors Gender Diet Environment Cultural, ethnic and genetic factors

Developmental factors
Pregnancy most drugs are contra-indicated during the first trimester Infants smaller doses because of body size and immaturity of organs, particularly kidneys and liver Elderly variable responses to drugs due to physiological changes that accompany aging such as decreased liver and kidney function, decreased protein levels, increased adipose tissue and decreased body fluids

Gender

Most drug research is done on men! Differences in response are related to distribution of body fat, fluid and hormones

Diet
Nutrients can effect the action of a medication E.g. Vitamin K found in green leafy vegetables may counteract the anticoagulant effect of warfarin

Environment / psychological
High temperatures may dilate peripheral blood vessels, intensifying the action of vasodilators. Cold temperatures may cause the opposite effect on vasodilators, but enhance the action of a vasoconstrictor A sedative, or analgesic may not be as effective in a noisy, busy environment Antidepressants may be ineffective if other complimentary therapies are not used as well Assessing the effects of a drug may need to considered in the context of the clients personality and expectations

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Holmesglen 2013

HLTEN507C Administer and monitor medications in the work environment

Pharmacodynamics and pharmacokinetics

Cultural, ethnic and genetic factors


Pharmacogenetics studies the variations in metabolism of drugs due to a clients genetic profile Ethnopharmacology studies the effect of ethnicity on responses to prescribed drugs Cultural factors and practices (values and beliefs) can also affect a drugs action

Dose - effect Relationship


For drugs to be therapeutic, a certain blood level needs to be reached and maintained Therapeutic range (Therapeutic index) Range between minimum effective concentration & toxic level Generally the higher the therapeutic index the safer the drug is Aim for Steady state concentration that maintains therapeutic effect.

Half-life of drug
The time interval required for the bodys elimination processes to reduce the concentration of the drug in the body by half e.g. Drug half-life is 8 hours, the amount of drug in the body is: Initially 100% After 8 hours- 50% After 24 hours- 12.5%

Peak concentration time profile

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Dose effect relationship


Peak plasma level the highest plasma level achieved by a single dose when the elimination rate equals the absorption rate Onset of action - the time after administration when the body responds to the drug Drug half-life (elimination half life) the time required for the elimination process to reduce the concentration of the drug to one-half what it was at initial administration Plateau a maintained concentration of drug in the plasma during a series of scheduled doses

Steady State Concentration:


Bullock and Manias. p152

Holmesglen 2013

HLTEN507C Administer and monitor medications in the work environment

Pharmacodynamics and pharmacokinetics

Pharmacodynamics What drugs do to the body


The process by which a specific drug produces biochemical or physiological changes in the body. This occurs when the drug interacts with specific molecules and chemicals within the body.

Principles of Drug action

Drugs act by: Modifying a biochemical or physiological response. Increasing or decreasing the effect of a biochemical or physiological response Replacing a deficiency to create a normal physiological response. Controlling changes resulting from disease.

Receptors
Most drugs act on receptors (cellular locks) Receptors, usually a protein, are located on the surface of a cell membrane or within a cell. Cell membranes contain receptors for normally occurring neurotransmitters and hormones Drugs (keys) exert their effects by binding with these receptors (locks). Binding is often referred to as the lock and key principle The effect may be agonistist or antagonistic.

Agonist Activates receptor


Same response as natural (endogenous) chemical in the body Effect proportional to dose & number of receptors If all receptors are saturated then increasing the medication dose has no effect Partial effect sometimes there is less than a maximum effect because all receptors are already bound. Example: Salbutamol (Ventolin)

Antagonist

Receptor Interactivity
Affinity - How well a drug binds to receptor Potency - Amount of drug needed to produce therapeutic effect Specificity Ability of a drug to target a specific site Efficacy Ability of drug to produce an effect at a receptor

Blocks receptor
Prevents the binding of the drug with the receptor competes at the receptor Most are reversible Non-reversible have limited therapeutic use Binds with receptor but does not produce the response (or diminishes the natural response) Examples beta blockers, histamine receptor antagonists

Holmesglen 2013

HLTEN507C Administer and monitor medications in the work environment

Pharmacodynamics and pharmacokinetics

Specificity
Medications that act specifically (specificity) Ability of a drug to produce an action at a specific site Concept of target organ - site of major intended action for medication There may be multiple effects due to location of the same receptors in cells of different organs & tissues. A medication wont have the same effect on all tissues & organs

Cell binding http://www.youtube.com/watch?v=07Tr__R_koE&feature =BF&list=PLE66C8741BD8D6329&index=9binding Agonist and antagonist http://www.youtube.com/watch?v=00DBInWsvrM&NR=1 http://www.youtube.com/watch?v=9ovnnadzhHo&feature =BF&list=PLE66C8741BD8D6329&index=10

Selectivity
A Selective drug acts at a receptor in a particular type of body tissue and produces little effect on similar receptors in other organs. What Determines Drug Selectivity? Chemical structure of the drug Molecular size of the drug Electrical charge of the drug

Drugs acting on Enzymes


An enzymes is a protein catalyst which accelerates the rate at which a metabolic reaction proceeds in the body Drug binds with the enzyme to: Increase or decrease the metabolic reaction Enzyme blockade proton pump inhibitor, ACEI, MAOs, NSAIDS, acarbose, aspirin, methotrexate

Drugs acting on transport mechanisms


Ion channels Receptors are associated with the transport of ions. (e.g. calcium, sodium, potassium) Drugs block or modulate an ion channel causing an increase or decrease in the permeability for the ion e.g. Digoxin, Calcium channel antagonists, opioids

Drugs acting on cell growth and division


Non selective Acts on all cells synthesizing DNA & rapidly dividing Acts at different stages in cell cycle Also includes anti-microbial agents Affect synthesis in bacterial cells Penicillin, Cephalosporins Increase permeability of cell membranes of invading organisms Nystatin, Amphotericin Inhibit bacterial protein synthesis Chloramphenicol, Erythromycin

Holmesglen 2013

HLTEN507C Administer and monitor medications in the work environment

Pharmacodynamics and pharmacokinetics

Drugs acting by physical mechanism


Osmotic drugs Interfere with movement of water across cell membrane (Mannitol, lactulose, movicol) Antacids Neutralise gastric acids & reduce motility (Mylanta, aluminium hydroxide, magnesium hydroxide) Urinary alkalisers Potassium citrate makes acidic urine alkaline. Drugs that lower surface tension De-gas

Revision - Key terms


Absorption Agonist Antagonist Distribution Drug half life Excretion Metabolism Onset of action Peak plasma level Pharmacodynamics Pharmacokinetics Plateau Receptor Therapeutic effect

References
Bryant, B. and Knights, K. 2011. Pharmacology for Health Professionals 3rd edition. Elsevier. Australia. Bullock, S. and Manias, E., 2011. Fundamentals of Pharmacology, 6th edition. Prentice-Hall Health, Pearson Education Australia. Koutoukidis, G., Stainton, K & Hughson, J 2012, Tabbners Nursing Care Theory and Practice, 6th edn, Elsevier, Sydney

Holmesglen 2013

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