PharmacologyPharmacology

& the certified athletic trainer& the certified athletic trainer

ATC and DrugsATC and Drugs

Study findingsStudy findings Health advisorHealth advisor Watch dog for Watch dog for

abuseabuse

Terms Terms

Drug vs MedicineDrug vs Medicine PharmacologyPharmacology

– PharmacokineticsPharmacokinetics– PharmacodynamiPharmacodynami

cscs DosingDosing

– StandardStandard– PediatricPediatric– Loading Loading

PotencyPotency

Pharmacology

Pharmacotherapeutics Toxicology

Pharmacokinetics Pharmacodynamics•Drug Absorption / Distribution•Drug Metabolism / Excretion

•Cellular Effects•Systemic Effects

Routes of Routes of AdministrationAdministration

Enteral vs ParenteralEnteral vs Parenteral Systemic EffectsSystemic Effects

– Oral (Ingestion) – liquid, tablets, capsulesOral (Ingestion) – liquid, tablets, capsules Pros and ConsPros and Cons Enteric coated pillsEnteric coated pills Sustained release tablets/capsulesSustained release tablets/capsules

– Injection (Parenteral) – subcutaneous, Injection (Parenteral) – subcutaneous, intravenous, intramuscularintravenous, intramuscular

Pros and ConsPros and Cons

– Other – intranasal, inhalation, sublingual, Other – intranasal, inhalation, sublingual, buccal, rectal, transdermalbuccal, rectal, transdermal

Pros and ConsPros and Cons

Routes of Routes of AdministrationAdministration

Local EffectsLocal Effects– Topical – applied to the skin to treat Topical – applied to the skin to treat

skin conditionsskin conditions– Otic Otic – OpthalmicOpthalmic

PharmacokineticsPharmacokinetics

Refers to movement of drugs Refers to movement of drugs across body membranes to reach across body membranes to reach the target organ the target organ

4 phases (ADME)4 phases (ADME)– AbsorptionAbsorption– DistributionDistribution– Metabolism Metabolism – Elimination Elimination

Pharmacokinetics Pharmacokinetics (phase 1)(phase 1)

Absorption Absorption – from GI tract to bloodstream – ingestionfrom GI tract to bloodstream – ingestion– All other methods go directly into bloodAll other methods go directly into blood– Some drug binds to blood protein, some Some drug binds to blood protein, some

free floatingfree floating BioavailabilityBioavailability – amount of drug – amount of drug

available to use following digestionavailable to use following digestion Exercise’s effect on AbsorptionExercise’s effect on Absorption

– Rate of dissolutionRate of dissolution– Surface AreaSurface Area– Lipid solubilityLipid solubility

Pharmacokinetics Pharmacokinetics (phase 2)(phase 2)

Distribution – movement from Distribution – movement from circulation into tissuescirculation into tissues– Delivered to target areasDelivered to target areas– Exercise increases distributionExercise increases distribution– Affected by poor circulationAffected by poor circulation

How does a drug exert it’s effect?How does a drug exert it’s effect?– Lipid solubility of drug Lipid solubility of drug – ReceptorReceptor– Physical or Chemical meansPhysical or Chemical means

Drug ActionsDrug Actions

Activation (Stimulation) – increase the rate of Activation (Stimulation) – increase the rate of functional activityfunctional activity

Inactivation (Depression) – decrease the rate Inactivation (Depression) – decrease the rate of functional activityof functional activity

Blocking – prevents an action or responseBlocking – prevents an action or response Inhibition – changes cell functioningInhibition – changes cell functioning Substitutive (Replacement) – substitute an Substitutive (Replacement) – substitute an

equivalent substance to restore optimal equivalent substance to restore optimal conditioncondition

Curative – destruction or prevention of growthCurative – destruction or prevention of growth Irritation – abnormal excitation of functionIrritation – abnormal excitation of function

Drugs in the BodyDrugs in the BodyExampleExample Site of action (Target organ) - NeuronSite of action (Target organ) - Neuron

– Synapses – space between axon and Synapses – space between axon and dendritesdendrites

In central and peripheral nervous systemIn central and peripheral nervous system

– Dendrite – receive impulse from adjacent Dendrite – receive impulse from adjacent neuronneuron

– Cell body – processes incoming information; Cell body – processes incoming information; formulate action potentialformulate action potential

– Axon – transmits action potentialAxon – transmits action potential– Neurotransmitter – protein chemical Neurotransmitter – protein chemical

messenger that carries an AP across messenger that carries an AP across synapse synapse

Site of ActionSite of Action

Effects on Synapses – either Effects on Synapses – either excitatory or inhibitoryexcitatory or inhibitory

Receptors – protein molecules on a Receptors – protein molecules on a cell membrane that can interact cell membrane that can interact with drugswith drugs

Axon

Dendrite

Neurotransmitter

Axon

Dendrite

Axon

Dendrite

Drug binds to presynaptic receptor

Axon

Dendrite

Drug binds to postsynaptic receptor

Axon

Dendrite

Drug mimics neurotransmitter

Axon

Dendrite

Drug destroys enzyme that should destroy neurotransmitter

+

Agonist

-

Agonist

Antagonist

Factors Affecting Drug Factors Affecting Drug ActionsActions Age – infants and elderly more sensitiveAge – infants and elderly more sensitive Gender – affects women differentlyGender – affects women differently

– Hormones, % body fat, less H2OHormones, % body fat, less H2O Mindset – Mindset – Dosage – Dosage – Potency – Potency – Purity – Purity – Tolerance – Tolerance –

PharmacokineticsPharmacokinetics

Metabolism (phase 3) – clearing of Metabolism (phase 3) – clearing of drugs from the body drugs from the body – LiverLiver– ““First pass effect”First pass effect”– Makes drug inactivativeMakes drug inactivative– Exercise slows metabolismExercise slows metabolism– Liver illness slows metabolism – causes a Liver illness slows metabolism – causes a

buildup of unmetabolized drugbuildup of unmetabolized drug Excretion (phase 4) – removal of drug Excretion (phase 4) – removal of drug

from the bodyfrom the body– Exercise slows excretionExercise slows excretion– Kidney illness slows excretionKidney illness slows excretion

Example of Example of Pharmacokinetic Process Pharmacokinetic Process (Aspirin)(Aspirin) Orally administeredOrally administered Absorbed in Stomach and SIAbsorbed in Stomach and SI 80-90% binds to protein, so 10-20% 80-90% binds to protein, so 10-20%

exits blood and has therapeutic effectexits blood and has therapeutic effect– Compared with 20-50% binding w/ TylenolCompared with 20-50% binding w/ Tylenol

Metabolism begins in blood and ends Metabolism begins in blood and ends in liver – changes to salicylic acidin liver – changes to salicylic acid

Excreted by kidneyExcreted by kidney

Pharmacokinectic Pharmacokinectic Terms Terms Half-lifeHalf-life Duration of ActionDuration of Action MECMEC Toxic Toxic

ConcentrationConcentration Therapeutic Therapeutic

RangeRange Maximal EfficacyMaximal Efficacy

Drug InteractionsDrug Interactions

DefinitionDefinition Depends on many factors…..Depends on many factors….. 2 Types of Interactions2 Types of Interactions

– Pharmacokinetic InteractionsPharmacokinetic Interactions– Pharmacodynamic InteractionsPharmacodynamic Interactions

Additive Effect 2+2=4Additive Effect 2+2=4 Synergistic Effect 2+3=5Synergistic Effect 2+3=5 Antagonistic Effect 2+2=1Antagonistic Effect 2+2=1

Drug Interactions Drug Interactions (con’t)(con’t) Alcohol and FoodsAlcohol and Foods Preventive MethodsPreventive Methods

– LabelLabel– Computerized record keepingComputerized record keeping

Adverse Drug Reactions (ADR)Adverse Drug Reactions (ADR)– AllergiesAllergies– Negative side effectsNegative side effects– Minor or severeMinor or severe– Local or systemicLocal or systemic– Seek Tx and requires discontinuation of Seek Tx and requires discontinuation of

drugdrug

Guidelines for ATC’sGuidelines for ATC’s

Read label for appropriate dosageRead label for appropriate dosage Consider possible interactionsConsider possible interactions Recognize adverse reactions and act Recognize adverse reactions and act

quicklyquickly IV and those absorbed thru thin most IV and those absorbed thru thin most

mucus membrane take effect quicker mucus membrane take effect quicker than oral administrationthan oral administration

Drug effects are maximal at peak Drug effects are maximal at peak concentration level, but ADME can all be concentration level, but ADME can all be affected by a variety of factorsaffected by a variety of factors

Be aware of all meds an athlete is takingBe aware of all meds an athlete is taking