Pharmacology 101

Abdelkader Ashour, Ph.D.

1st & 2nd Lectures

Overview
A. Introduction
-Definitions

-Drug Sources -Drug Nomenclature

B. Basic concepts in Pharmacology

-Drug-Body Interactions -Drug Receptors -Drug Receptor Interactions

Pharmacology,

link to other biomedical principles

Pharmacology,
organisms

Definitions

Pharmacology A branch of medical sciences that study drugs and their action on living
Why do nurses study pharmacology? A sound knowledge of basic pharmacologic principles is essential if the nurse is to safely administer medications and to monitor patients who receive these medications

Drug
Any substance that brings about a change in biologic function through its chemical actions

Receptor
A specific protein in either the plasma membrane or interior of a target cell with which a chemical messenger/drug combines

Mechanism of Action
The ways by which drugs can produce therapeutic effects

Dose
The amount of a drug to be administered at one time

Pharmacology,
Effects (therapeutic effect) The desired results of administration of a medication Side Effects (adverse effects) Effects that are harmful and undesired, and that occur in addition to the desired therapeutic effects

Definitions

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

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

The Role of Nurses in Relation to Pharmacology

Nurses play an active role in drug administration
Nurses contribute to the planning and modification of drug therapy from their assessment of patient factors and evaluation of progress or problems occurring during drug therapy
In addition to: the role in patient education and compliance

Nurses share information with other health care professionals to provide the most effective medication regimen for the patient

Nurses have to follow the Five Rights of Medication Administration

1. Right drug

2.
3. 4. 5.

Right dose
Right time Right route Right patient

Drug Sources
1. 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.

2. Animal Sources: Glandular products from animals are used, such as insulin and thyroid. 3. From micro-organisms (fungi, bacteria) Penicillin was discovered by Alexander Fleming in 1928 as a product of penicillium notatum (a mold growing in his lab) 4. Mineral Sources: Some drugs are prepared from minerals, for example, lithium carbonate (an antipsychotic), MgSO4 (a laxative) 5. Synthetic Sources: Laboratories duplicate natural processes, and may modify the products. Frequently this can eliminate side effects and increase 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

Drug Nomenclature
Chemical name represents the exact description of the drugs chemical composition Generic name (non-proprietary)
- simpler than the chemical name and - derived from the chemical name itself - easier to remember Example 1: the chemical name 2-methyl-5-nitroimidazole-l-ethanol is metronidazole. The word methylnitro is condensed to metro and ni-dazole is due to its imidazole ring Example 2: Metoclopramide is the condensed form of the word methoxychloroprocainamide: where Me is retained and th is written as t; chloro is written as clo: and procainamide is written as pramide

Brand or trade name (proprietary) is developed by the company requesting

approval 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.

Overview
A. Introduction
-Definitions

-Drug Sources -Drug Nomenclature

B. Basic concepts in Pharmacology

-Drug-Body Interactions -Drug Receptors - Drug Receptor Interactions

Drug-Body Interactions
Pharmacokinetics
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 of absorption, 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.

Pharmacodynamics
The study of the action or effects of drugs on living organisms

Pharmacokinetics
What the body does to the drug

vs

Pharmacodynamics
What the drug does to the body

Drug Receptors
Receptor/Binding site A specific protein in either the plasma membrane or interior of a target cell with which a ligand/drug combines
It must be selective in choosing ligands/drugs to bind To avoid constant activation of the receptor by promiscuous binding of many different ligands (drugs)

It must change its function upon binding in such a way that the function of the biologic system (cell, tissue, etc) is altered This is necessary for the ligand (drug) to cause a pharmacologic effect

Drug Receptors
Receptor/Binding site A specific protein in either the plasma membrane or interior of a target cell with which a ligand/drug combines
It must be selective in choosing ligands/drugs to bind To avoid constant activation of the receptor by promiscuous binding of many different ligands (drugs)

It must change its function upon binding in such a way that the function of the biologic system (cell, tissue, etc) is altered This is necessary for the ligand (drug) to cause a pharmacologic effect

Drug Receptors
Receptor/Binding site A specific protein in either the plasma membrane or interior of a target cell with which a ligand/drug combines
It must be selective in choosing ligands/drugs to bind To avoid constant activation of the receptor by promiscuous binding of many different ligands (drugs)

It must change its function upon binding in such a way that the function of the biologic system (cell, tissue, etc) is altered This is necessary for the ligand (drug) to cause a pharmacologic effect

Drug Receptor Interactions

The Lock and Key Model of Signal-Receptor Interaction
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 the hormone or neurotransmitter can exert its effects

Agonist
A 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 trigger the 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 prevents binding of acetylcholine (ACh) and similar agonist drugs to the ACh receptor

Drug Receptor Interactions

Lock and key mechanism

Agonist

Receptor

Agonist-Receptor Interaction

Drug Receptor Interactions

Competitive Inhibition

Antagonist

Receptor

DENIED!

Antagonist-Receptor Complex