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Pharmacology 101
Abdelkader Ashour, Ph.D.
1st & 2nd Lectures
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B. Basic concepts in Pharmacology-Drug-Body Interactions-Drug Receptors
-Drug Receptor Interactions
Overview
A. Introduction
-Definitions
-Drug Sources
-Drug Nomenclature
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Pharmacology,link to other biomedical principles
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Receptor
A specific protein in either the plasma membrane or interior of a target cell
with which a chemical messenger/drug combines
Pharmacology,Definitions Pharmacology
A branch of medical sciences that study drugs and their action on living
organisms Why do nurses study pharmacology? A sound knowledge of basic pharmacologic
principles is essential if the nurse is to safely administer medications and tomonitor patients who receive these medications
Drug
Any substance that brings about a change in biologic function through itschemical actions
Dose
The amount of a drug to be administered at one time
Mechanism of Action
The ways by which drugs can produce therapeutic effects
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Indications
The reasons for administering a medication or performing a treatment
Contra-indications
Factor that prevents the use of a medication or treatment (e.g., Allergies)
Pharmacology,Definitions
Effects (therapeutic effect)
The desired results of
administration of a medication
Side Effects (adverse effects)
Effects that are harmful and
undesired, and that occur inaddition to the desired therapeuticeffects
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Pharmacology,Definitions Onset
The time it takes for the drug to elicit a therapeutic response
Duration
The time a drug concentration is sufficient to elicit a therapeutic response
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The Role of Nurses in Relation toPharmacology
Nurses share information with other health care professionals to provide themost effective medication regimen for the patient
Nurses play an active role in drug administration
Nurses contribute to the planning and modification of drug therapy from theirassessment of patient factors and evaluation of progress or problemsoccurring during drug therapy
In addition to: the role in patient education and compliance
Nurses have to follow theFive Rights of Medication Administration
1. Right drug2. Right dose
3. Right time
4. Right route
5. Right patient
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Drug Sources1. Plant Sources:Obtained from plant parts or products. Seeds, stem,
roots, leaves, resin, and other parts yield these drugs.
Examples include digoxin from digitalis and morphine from opium.
4. Mineral Sources: Some drugs are prepared from minerals, for example,lithium carbonate (an antipsychotic), MgSO4 (a laxative)
2. Animal Sources: Glandular products from animals are used, such asinsulin and thyroid.
5. Synthetic Sources:Laboratories duplicate natural processes, and maymodify the products. Frequently this can eliminate side effects andincrease the potency of the drug.Examples include sulfonamides, and aspirin.
6. Recombinant proteins:Proteins that are synthesized by expression of
cloned genes in recombinant cells, such as interferons, antibodies
3. From micro-organisms (fungi, bacteria)Penicillin was discovered by
Alexander Fleming in 1928 as a product of penicillium notatum (a moldgrowing in his lab)
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Brand or trade name (proprietary)is developed by the company requestingapproval for the drug and identifies it as the exclusive property of that company.
Example 1:Metrogyl is the trade name for metronidazole.
Example 2:Reglan is the trade name for Metoclopramide.
Example 3:Amoxil is the trade name for amoxycillin.
Example 4:Celebrex is the trade name for Celecoxib.
Drug Nomenclature
Example 1:the chemical name 2-methyl-5-nitroimidazole-l-ethanol ismetronidazole. The word methylnitro is condensed to metro and ni-dazole is dueto its imidazole ring
Example 2:Metoclopramide is the condensed form of the wordmethoxychloroprocainamide: where Me is retained and th is written as t; chlorois written as clo: and procainamide is written as pramide
Chemical namerepresents the exact description of the drugs chemicalcomposition
Generic name (non-proprietary)-simpler than the chemical name and- derived from the chemical name itself- easier to remember
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B. Basic concepts in Pharmacology-Drug-Body Interactions-Drug Receptors
- Drug Receptor Interactions
Overview
A. Introduction
-Definitions
-Drug Sources
-Drug Nomenclature
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Pharmacokinetics (in Greek: "pharmacon" meaning drug, and "kinetikos"meaning putting in motion)
The study of the movement of drugs in the body, including the processes ofabsorption, distribution, metabolism and excretion (ADME)
The drug should be in an adequate concentration at the site of action to
produce its effects. This depends on ADME.
Pharmacokinetics
Pharmacodynamics The study of the action or effects of drugs on living organisms
Pharmacokinetics vs Pharmacodynamics
What the drug does to the bodyWhat the body does to the drug
Drug-Body Interactions
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Receptor/Binding site
A specific protein in either the plasmamembrane or interior of a target cell withwhich a ligand/drug combines
It must be selective in choosing ligands/drugsto bind To avoid constant activation of thereceptor by promiscuous binding of manydifferent ligands (drugs)
It must change its function upon binding insuch a way that the function of the biologicsystem (cell, tissue, etc) is altered This isnecessary for the ligand (drug) to cause a
pharmacologic effect
Drug Receptors
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Receptor/Binding site
A specific protein in either the plasmamembrane or interior of a target cell withwhich a ligand/drug combines
It must be selective in choosing ligands/drugsto bind To avoid constant activation of thereceptor by promiscuous binding of manydifferent ligands (drugs)
It must change its function upon binding insuch a way that the function of the biologicsystem (cell, tissue, etc) is altered This isnecessary for the ligand (drug) to cause a
pharmacologic effect
Drug Receptors
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Receptor/Binding site
A specific protein in either the plasmamembrane or interior of a target cell withwhich a ligand/drug combines
It must be selective in choosing ligands/drugsto bind To avoid constant activation of thereceptor by promiscuous binding of manydifferent ligands (drugs)
It must change its function upon binding insuch a way that the function of the biologicsystem (cell, tissue, etc) is altered This isnecessary for the ligand (drug) to cause a
pharmacologic effect
Drug Receptors
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The Lock and Key Model of Signal-ReceptorInteraction
Ligands such as hormones or neurotransmitters (the"key")affect target cells by binding to specific receptors (the
"lock), which are often located in the cell membrane
This binding "unlocks" the cell's response, so that thehormone or neurotransmitter can exert its effects
Drug Receptor Interactions
AgonistA chemical messenger that binds to a receptor and triggers the cells
response; often refers to a drug that mimics a normal messengers action. For example, pilocarpine is a muscarinic receptor agonist because it can bind to and
activate muscarinic receptors
Antagonist
"A molecule that competes for a receptor with a chemical messenger normally
present in the body. The antagonist binds to the receptor but does not triggerthe cells response For Example, atropine is a muscarinic receptor antagonist because it can bind to
muscarinic receptors but it does not trigger the cells response. In this way, it preventsbinding of acetylcholine (ACh) and similar agonist drugs to the ACh receptor
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Drug Receptor Interactions
Agonist Receptor
Agonist-Receptor
Interaction
Lock and key mechanism
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Antagonist Receptor
Antagonist-Receptor
ComplexDENIED!
CompetitiveInhibition
Drug Receptor Interactions