unit 1: general principles

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Pharmacology

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129 Terms

1

Pharmacology

Body of knowledge concerned with the action of chemicals on biologic systems, especially by binding to regulatory molecules (receptors) and activating or inhibiting normal body processes.

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Pharmacology

study of substances that interact with living systems through chemical processes.

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beneficial therapeutic effect

These substances may be chemicals administered to achieve a ___ on some process within the patient or for their toxic effects on regulatory processes in parasites infecting the patient.

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chemical

drug or any chemical which can affect our biological system

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binding site or a receptor

chemicals have a ___, if not, it will not affect any biological change

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receptors

___ are able to regulate (regulatory) function of our body, the drug can either activate or inhibit that function by binding to that receptor.

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Medical pharmacology and toxicology

  • understanding the actions of drugs as chemicals on individual organisms

  • first domain (left)

  • both beneficial & toxic effects

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Pharmacokinetics

  • absorption, distribution, and elimination of drugs

  • how the drug will be handled by the patient

  • movement of the drug into, within, and out of our body

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Pharmacodynamics

  • actions of the chemical on the organism.

  • denotes the actions of the drug on the body, such as mechanism of action and therapeutic and toxic effects

  • how the drug would affect our body

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Environmental toxicology

  • effects of chemicals on all organisms and their survival in groups and as species

  • second domain (right)

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  • increasing resistance

  • discovery of new target processes

  • recognition of new diseases

why are new drugs added every year?

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pharmacology

represents an area where anatomy, biochemistry, genetics, physiology, pathology, clinical medicine, and the environment meet

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pharmacologic tools

many problems that the health practitioner confronts can now be corrected or mitigated using ___

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Pharmacogenomics

  • field of research that studies how a person's genes affect how he or she responds to medications

  • relation of the individual’s genetic makeup to his or her response to specific drugs

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Decoding of the genomes of many species

___ led to the recognition of unsuspected relationships between receptor families and the ways that receptor proteins have evolved.

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discovery of regulatory functions

___ has opened a new area of possible manipulation of the genes—epigenetics—that control pharmacologic responses.

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neighbors of chromosomes and the noncoding regions of DNA on the expression of exons

discovery of regulatory functions are exerted by ___

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small interfering RNAs (siRNAs) and micro-RNAs (miRNAs

discovery that small segments of RNA can interfere with protein synthesis with extreme selectivity has led to investigation of ___ as therapeutic agents.

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antisense oligonucleotides (ANOs)

___, synthesized to be complementary to natural RNA or DNA, can interfere with the readout of genes and the transcription of RNA

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toxic

General principles that the student should remember are:

that all substances can under certain circumstances be ___

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the much greater proportion of impurities

General principles that the student should remember are:

chemicals in botanicals are no different from chemicals in manufactured drugs except for ___

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artificial separation

General principles that the student should remember are:

all dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies. there should be no ___ between scientific medicine and “alternative” or “complementary” medicine

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Pharmacogenomics

  • Finds the exact mechanism of action of drugs

  • Identifies the receptors

  • brought about by the exploration of the human gene

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Drug

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

  • Any substance that can bring about a biological functional change through its chemical actions

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Receptor

  • Specific molecule in the biologic system that plays a regulatory role

  • what is present in our body which plays a regulatory role that can be altered by the drug.

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an agonist (activator) or antagonist (inhibitor)

nature of drugs:

the drug molecule interacts as ___ with a specific target molecule that plays a regulatory role in the biologic system.

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chemical antagonists

nature of drugs:

may interact directly with other drugs

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osmotic agents

nature of drugs:

interact almost exclusively with water molecules.

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Poisons

drugs that have almost exclusively harmful effects

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Paracelsus (1493–1541)

the dose makes the poison,” meaning that any substance can be harmful if taken in the wrong dosage.

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Toxins

defined as poisons of biologic origin synthesized by plants or animals

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alkaloids

Many drugs found in nature are ___, which are molecules that have a basic (alkaline) pH in solution, usually as a result of amine groups in their structure.

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enantiomers

Many biologically important endogenous molecules and exogenous drugs are optically active; that is, they contain one or more asymmetric centers and can exist as ___.

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the appropriate size, electrical charge, shape, and atomic composition

physical nature of drugs:

drug molecule must have ___

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Solid

physical nature of drugs:

  • includes tablets, granules or powder contained inside the capsules.

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Liquid

physical nature of drugs:

  • syrup or suspension.

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Syrup

physical nature of drugs (liquid):

  • homogeneous

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Suspension

physical nature of drugs (liquid):

  • there would be undissolved particles, it tends to settle down. When you dispense and do not properly shake, the concentration would vary and the effect would also vary because of the varying dose of the drug

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Gas

physical nature of drugs:

  • mostly like anesthetics, aerosolized anesthetics, for those who are nebulizing that is vaporized

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site distant

Drugs are given at a ___ from the intended site of action

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necessary properties

a useful drug must have the ___ to be transported from its site of administration to its site of action

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delayed

The onset of action would be ___ if you give it at a far distant site

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pH differences

alters the degree of ionization of weak acids and bases

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MW 7

drug size & molecular weight:

  • Lithium can be used as chemotherapeutic drug

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MW 50,000

drug size & molecular weight:

  • thrombolytic agents

  • Heparin

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100 MW

drug size & molecular weight:

  • For selective binding

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It could easily be eliminated

Disadvantage of being a small drug

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  • easily be distributed because they can pass through smaller pores or gaps in between blood vessels

  • can diffuse easily

Advantage of being a small drug

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1000 MW

drug size & molecular weight:

  • For traversing to different barriers of the body

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1000 MW

drug size & molecular weight:

  • Cannot move within the body

  • Given directly at the site of action

  • poorly absorbed and poorly distributed in the body

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lower limit

drug size & molecular weight:

  • set by the requirements for specificity of action.

  • prevent its binding to other receptors

  • at least 100 MW units in size

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upper limit

drug size & molecular weight:

  • drugs must be able to move within the body

  • do not diffuse readily between compartments

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complementary

drug shape:

drug’s shape is ___ to that of the receptor site

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Stereoisomerism

drug shape:

Can affect the potency of the drug

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enantiomeric

drug shape:

they exist as ___ pairs

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Carvedilol

drug shape:

  • (S)(-) isomer, potent beta receptor blocker

  • (R)(+) isomer, weak beta receptor blocker

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Ketamine

drug shape:

  • (+) more potent anesthetic and less toxic than the (-)

  • Racemic mixer

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Rational design of drugs

ability to predict the appropriate molecular structure of a drug on the basis of information about its biologic receptor.

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Drug Receptor bonds

Chemical forces or bonds through which the drugs interacts with the receptors

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more selective bonds

Drug Receptor bonds:

Weaker bonds are ___

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Strongest

Drug Receptor bonds: Covalent Bonds

  • cannot be easily dislodged or separated from each other

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Irreversible

Drug Receptor bonds: Covalent Bonds

  • The backside is it is quite ___

  • Aspirin with its receptor, cyclooxygenase

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Electrostatic Bonds

Drug Receptor bonds:

  • More common

  • Weaker than covalent

  • bonds vary from relatively strong linkages between permanently charged ionic molecules to weaker hydrogen bonds and very weak induced dipole interactions

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Hydrophobic Bonds

Drug Receptor bonds:

  • weakest

  • Utilized by highly lipid soluble drugs

  • uncharged areas

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pockets

Hydrophobic Bonds are important in the interactions of highly lipid-soluble drugs with the lipids of cell membranes and perhaps in the interaction of drugs with the internal walls of receptor___.”

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Pharmacodynamics

Drug-Body Interactions:

  • actions of the drug on the body

  • determine the group in which the drug is classified, deciding whether that group is appropriate therapy

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Pharmacokinetics

Drug-Body Interactions:

  • actions of the body on the drug

  • govern the absorption, distribution, and elimination of drugs

  • great practical importance in the choice and administration of a particular drug

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drug ligand molecules

Pharmacodynamic Principles:

Drug actions are mediated through the effects of ___ on drug receptors in the body.

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Drug (D) + receptor-effector (R) → drug-receptor-effector complex → effect

Pharmacodynamic Principles:

A cholinergic drug reaches the acetylcholine. If for example the cholinergic drug is in the muscle, you will experience muscle contraction or muscle twitch. This happens because the cholinergic receptor is an effector.

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D + R → drug-receptor complex → effector molecule → effect

Pharmacodynamic Principles:

  • When the drug reaches and binds to its receptor, the drug-receptor complex produces an intracellular effector. This intracellular effector mediates the action of the drug. The effect would greatly depend on the available effectors inside.

  • The receptor is normally in the cell membrane. When a drug binds to it, it produces or activates the intracellular effector.

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D + R → D-R complex → activation of coupling molecule → effector molecule → effect

Pharmacodynamic Principles:

  • The drug binds to its receptor extracellular and the drug-receptor complex activates a coupling molecule or enzyme inside. The activated coupling molecule or enzyme inside will be the one to produce the effector molecule. And the effector molecule will be the one who will produce the effect.

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Inhibition of metabolism of endogenous activator → increased activator action on an effector molecule → increased effect

Pharmacodynamic Principles:

  • The drug actually doesn't need to bind to the receptor

  • drug will target the endogenous activator or metabolism.

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constitutive or basal activity

Pharmacodynamics:

  • Some of the receptor pool must exist in Ra form

  • May produce same physiological effect as agonist-induced activity

  • Occurs in the absence of the agonis

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higher affinity

Pharmacodynamics:

Agonists have a much ___ for the Ra configuration and stabilize it, so that a large percentage of the total pool resides in the Ra–D fraction and a large effect is produced

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receptor

Pharmacodynamics:

Agonist binds to and activate the ___

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Full agonist

Pharmacodynamics:

  • Activates receptor-effector system to the maximum extent (Ra-D pool)

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Partial agonist

Pharmacodynamics:

  • Bind to the same receptors and activate them in the same way but do not evoke as great a response, no matter how high the concentration.

  • Such drugs are said to have low intrinsic efficacy

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pindolol, a β-adrenoceptor partial agonist

Pharmacodynamics: Partial agonist:

may act either as an agonist or as an antagonist

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Allosteric modulators

Pharmacodynamics:

  • Binds to a site on the receptor molecule separate from the agonist binding site

  • Modifies receptor activity without blocking agonist activity

  • May increase or decrease response to agonist

  • noncompetitive

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allosteric activator

Pharmacodynamics: Allosteric modulators

when they increase, they are ___

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allosteric inhibitor

Pharmacodynamics: Allosteric modulators

when they decrease, they are ___

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Inverse agonist

Pharmacodynamics:

  • Drug has a stronger affinity for the Ri pool

  • Reduces constitutive activity

  • Results in effects that are opposite of the effects produced by conventional agonist

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Ri

Pharmacodynamics: Inverse agonist

the inactive receptor or the nonfunctional form of the receptor

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Antagonist

Pharmacodynamics:

  • Binds to a receptor, compete with and prevent binding by other molecule

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neutral antagonism

Pharmacodynamics: Antagonist

  • the presence of the antagonist at the receptor site will block access of agonists to the receptor and prevent the usual agonist effect

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lock & key mechanism

drug shape:

<p>drug shape:</p>
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Prodrug

Pharmacokinetics:

  • Inactive precursor

  • Must be administered and converted to the active drug by biologic process inside the body

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Biodisposition

term sometimes used to describe the processes of metabolism and excretion

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Permeation

Movement of Drugs in the Body:

  • Movement of drug molecules into and within the biologic environment

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Aqueous Diffusion

Movement of Drugs in the Body: Permeation

  • Movement of molecules through the watery extracellular and intracellular spaces

  • Membranes of capillaries have small water-filled pores

  • Passive process

  • Governed by Fick’s law

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Fick’s law of Diffusion

knowt flashcard image
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area

Movement of Drugs in the Body: Aqueous Diffusion: Fick’s law of Diffusion

  • the cross-sectional area of the diffusion

<p>Movement of Drugs in the Body: Aqueous Diffusion: Fick’s law of Diffusion</p><ul><li><p>the <strong>cross-sectional area</strong> of the diffusion</p></li></ul>
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permeability coefficient

Movement of Drugs in the Body: Aqueous Diffusion: Fick’s law of Diffusion

  • measure of the mobility of the drug molecules in the medium of the diffusion path

<p>Movement of Drugs in the Body: Aqueous Diffusion: Fick’s law of Diffusion</p><ul><li><p>measure of the <strong>mobility</strong> of the drug molecules in the medium of the diffusion path</p></li></ul>
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thickness

Movement of Drugs in the Body: Aqueous Diffusion: Fick’s law of Diffusion

  • the length of the diffusion

<p>Movement of Drugs in the Body: Aqueous Diffusion: Fick’s law of Diffusion</p><ul><li><p>the <strong>length</strong> of the diffusion</p></li></ul>
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the lipid:aqueous partition coefficient

Movement of Drugs in the Body: Aqueous Diffusion: Fick’s law of Diffusion

  • is a major determinant of mobility of the drug because it determines how readily the drug enters the lipid membrane

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Lipid Diffusion

Movement of Drugs in the Body: Permeation

  • Followed by lipid soluble drugs

  • Movement of molecules through membranes and other lipid structures

  • Most important limiting factor for drug permeation

  • Passive process

  • Governed by Fick’s law

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Henderson-Hasselbalch equation

Movement of Drugs in the Body: Lipid Diffusion

  • the ratio of lipid-soluble form to water-soluble form for a weak acid or weak base is expressed by ___

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Transport by Special Carriers

Movement of Drugs in the Body: Permeation

  • transported across barriers by mechanisms that carry similar endogenous substances

  • Capacity limited

  • Not governed by Fick’s law

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Active Transport

Movement of Drugs in the Body: Permeation: Transport by Special Carriers

  • Needs energy

  • Against a concentration gradient

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Facilitated Diffusion

Movement of Drugs in the Body: Permeation: Transport by Special Carriers

  • no energy

  • downhill

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