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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.
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
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
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
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
Holmesglen 2013
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
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
Holmesglen 2013
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%
Holmesglen 2013
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.
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
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
Holmesglen 2013
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