Chapter 1 - Orientation to Pharmacology

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C

HAPTER

1O

RIENTATION

TO

P

HARMACOLOGY

I. F

OUR

B

ASIC

T

ERMS

A. D

RUG

– defined as any chemical that can affect living processes and havetherapeutic applications

B. P

HARMACOLOGY

- defined as the study of drugs and their interactions with livingsystems- encompasses the study of the physical and chemical properties of drugs as well as theirbiochemical and physiologic effects- includes knowledge of the history, sources, and uses of drugs as wellas knowledge of drugabsorption, distribution, metabolism, and excretion

C. C

LINICAL

P

HARMACOLOGY

– defined as the study of drugs in humans (patients aswell as healthy volunteers)- interaction between drugs and people

D. T

HERAPEUTICS

– also known as

pharmacotherapeutics

- defined as the use of drugs to diagnose, prevent, or treat disease or toprevent pregnancy- medical use of drugs

II. P

ROPERTIES

OF

AN

I

DEAL

D

RUG

-

there is no such thing as a perfect drug

A. B

IG

T

HREE

:1. Effectiveness

– an effective drug is one that elicits the responses forwhich it is given.- effectiveness is the most important property a drug can have***

IF A DRUG IS NOT EFFECTIVE, IT SHOULD NOT BEUSED

***

2. Safety

– a safe drug is one that cannot produce harmful effects – evenis administered in very highdoses and for a very long time-

there is no such thing as a safe drug

-

pharmakon

– Greek word meaning poison

3. Selectivity

– one that elicits only the response for which it is given-

there is no such thing as a selective drug: All medications causeside effects

B. A

DDITIONAL

P

ROPERTIES

OF

AN

I

DEAL

D

RUG

1. Reversible Action

– it is important that effects be reversible- we want drug actions to subside within an appropriate time

2. Predictability

– since each patient is unique, the accuracy of certainpredictions cannot beguaranteed

3. Ease of Administration

– an ideal drug should be simple toadminister, the route should beconvenient, and the number of doses per day should be low

a. Benefits:

- it can enhance patient adherence- it can decrease errors in drug administration

4. Freedom from Drug Interactions

– when taking two or more drugs,those drugs can interact withone another in that they either augment or reduce drug responses- possible impact of drug interactions must be considered

5. Low Cost

– an ideal drug would be easy to afford

6. Chemical Stability

– some drugs lose effectiveness during storage;others which are stable on ashelf can rapidly lose effectiveness when put into a solution- losses in efficacy result from chemical instability

7. Possession of a Simple Generic Name

– generic names are usuallycomplex and difficult toremember and pronounce- as a rule, the trade name for a drug is simpler than its genericname

III. T

HERAPEUTIC

O

BJECTIVE

The objective of drug therapy is to provide maximum benefit withminimum harm.

IV. F

ACTORS

THAT

D

ETERMINE

THE

I

NTENSITY

OF

D

RUG

R

ESPONSES

A. A

DMINISTRATION

– dosage size, route and timing of administration are importantdeterminants of drugresponses

B. P

HARMACOKINETICS

– pharmacokinetic processes determine how much of anadministered dose gets to itssites of action

1. Major Pharmacokinetic Processes (impact of the body on drugs):a.

drug absorption

b.

drug distribution

c.

drug metabolism

d.

drug excretion

C. P

HARMACODYNAMICS

(

IMPACT

OF

DRUGS

ON

THE

BODY

)

– once at the site of action,pharmacodynamicprocesses determine the nature and intensity of the response

- initial step leading to a response is the binding of a drug to its receptorwhich is followed by asequence of events the ultimately results in a response

P

RESCRIBED

DOSE

↓↓medication errors

╟

↓patient compliance

╟

A

DMINISTERED

DOSE

↓↓absorption

╟

↓distribution

╟

↓metabolism

╟

↓excretion

╟

C

ONCENTRATION

@S

ITES

OF

A

CTION

Sources of individual variationphysiologic variables

╟

↓pathologic

╟

variables↓genetic

╟

variables↓ drug

╟

interactions↓ drug-receptor interaction

╟

I

NTENSITY

OF

patient’s functional state

╟

R

ESPONSES

placebo effects

╟

D. S

OURCES

OF

I

NDIVIDUAL

V

ARIATION

- characteristics unique to each patient can influence pharmacokineticand pharmacodynamicprocesses and, by doing so, can help determine the patient’sresponse to a drug- sources include drug interactions, physiologic variables (age, gender,weight), pathophysiologicvariables (especially diminished function of the kidneys and liver,the major organs of drugelimination), and genetic variables (can alter the metabolism of drugs and can predispose the patient to unique drug reactions)

***PATIENT ALWAYS HAS THE RIGHT TO REFUSE MEDICIATIONS***Critical Thinking:

What would be the perfect drug for a patient in chronicpain?First of all, there is no perfect drug. Then consider: effectivenessfast actingaffordable

AdministratiPharmacokiPharmacodna

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