Unit 1 - Pharmacologic Principles

Front 1

What is a Drug?

Back 1

Any chemical thataffects the physiologic processes of a living organism.

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Pharmacology

Back 2

Study or science ofdrugs.

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Chemical name

Back 3

describes the drug’s chemical composition and molecular structure

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Generic name

Back 4

(nonproprietary name)

Name given by the United States Adopted Names Council

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Trade name

Back 5

(proprietary name)

The drug has a registered trademark; use of the name is restricted by the drug's patent owner (usually the manufacturer)

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Class Act

Back 6

Drugs with similar characteristics

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Pharmaceutics

Back 7

1. The study ofhow various drug forms influence the way in which the drug affects the body

2. Dissolution-dissolving ofsolid dosage forms and their absorption

3. DrugAbsorption of Various Preparations (drug must dissolve 1st before being absorbed)

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Drug Absorption Rates for Oral Preparations

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FASTEST...

liquids, elixirs, syrups

suspension solutions

powders

capsules

tablets

enteric coated tablets

extended release tablets

...SLOWEST

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Pharmacokinetics

Back 9

The study of what the body does tothe drug.1. Absorption

2. Distribution

3. Metabolism

4. Excretion

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Pharmacokinetics of ABSORPTION

Back 10

Factors affectingabsorption

Bioavailability (extent of rx absorption)

First pass effect (after passes thru liver)

Enteral route

Sublingual buccal routes

Parenteral route: subQ, intradermal, IM

Topical route

Transdermal route

Inhaled route

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*Bioavailability

Back 11

The proportion of a drug or other substance that enters the circulation when introduced into the body and so is able to have an active effect.

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*First Pass Effect

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The metabolism of orally administered drugs by gastrointestinal and hepatic enzymes, resulting in a significant reduction of the amount of unmetabolized drug reaching the systemic circulation.

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Enteral Route

Back 13

The drug is absorbed into the systemic circulation through the oral orgastric mucosa or the small intestine:

Oral

Sublingual

Buccal

Rectal (can also be topical)

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Parenteral Route

Back 14

Any non-oral means of administration, but is generally interpreted as relating to injecting directly into the body (bypasses first-pass effect of the liver):

Intravenous (fastest delivery into the blood circulation)

Intramuscular

Subcutaneous

Intradermal

Intra-arterial

Intrathecal

Intraarticular

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Topical Route

Back 15

Application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes including creams, foams, gels, lotions, and ointments:

Skin (including transdermalpatches)

Eyes

Ears

Nose

Lungs(inhalation)

Rectum

Vagina

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Depot Drug

Back 16

The administration of a sustained-action drug formulation that allows slow release and gradual absorption, so that the active agent can act for much longer periods than is possible with standard injections. Depot injections are usually given deep into a muscle.

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*First Pass Drug Routes

Back 17

Hepatic arterial

Oral

Portal venous

Rectal

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*Non First Pass Drug Routes

Back 18

Aural (instilled in the ear)

Buccal

Inhaled

Intra-arterial

Intramuscular

Intranasal

Intraocular

Intravaginal

Intravenous

Transdermal

Sublingual

Subcutaneous

Front 19

Pharmacokinetics of Distribution

Back 19

Distribution: Transport of a drug by the bloodstream to its site of action by bodilyfluids.

Distribution of an absorbed drug within the body depends on severalfactors:

1. Blood flow

2. Solubility

3. Protein binding > 80% binds toprotein 4. Protein bound and unbound

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Influences on Distribution

(pharmacokinetics)

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1. Influenced byability to travel to the site of action through the blood stream (peripheralvascular or cardiac disease may delay medication distribution).

2. Influenced byability to leave the blood stream by traveling between capillaries’ cells 3. Plasma proteinbinding: Medications compete for protein-binding sites within the bloodstream,primarily albumin.

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Pharmacokinetics of Metabolism

Back 21

Also referred to as *biotransformation*.

A method by which drugs are inactivated or biotransformed by the body.

*An active drug is changed into inactive metabolites, which are then excreted.*

The organ most responsible for the metabolism of drugs is the LIVER.

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Influences on Metabolism

(pharmacokinetics)

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Age: Infants have limitedmedication- metabolizing capacity.

Aging process: risk of accumulation of rx

Hepatic metabolism declines withage

In the genes: increase or decrease metabolism

Environmental effects: smoking, etc.

First-pass-effects

Nutritional status: anorexia, etc

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Pharmacokinetics of Excretion

Back 23

Elimination of drugs from thebody

Kidneyis the primary organ, for excretion.

Liver, bowel, lungs, exocrine glands alsoexcrete.

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Half-life

Back 24

Time required for half (50%) of a given drug to be removed from thebody.

Short half-life: Medications leave the body quickly (4-8 hrs.)

Long half-life: medicationsleave the body more slowly (24+ hrs.)

Example of half-life: if the peak level of a particular drug is 100 mg/Land the measured drug level is 50 mg/L in 8 hrs., then the estimated half-lifeof that drug is 8 hrs.

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Steady State

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Refers to the physiologic state in which the amount of drug removed viaelimination (e.g., renal clearance) is equal to the amount of drug absorbedwith each dose.

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Peak and Trough

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Peak level:highest blood level of a drug

Trough level: lowest blood level of a drug

Toxicity: occurs if thepeak blood level of the drug is too high

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Therapeutic Index

Back 27

The ratio between the dosage of a drug that causes a lethal effect and the dosage that causes a therapeutic effect.

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Pharmacodynamics

Back 28

The study of what the drug doesto the body

1. The mechanism of drug actions in living tissues

2. Therapeuticeffect- A positive change is a faulty physiologic system.

3. Mechanism ofaction- Drugs produce actions (therapeutic effects)

4. Receptorinteraction- A reactive site on the surface or inside of a cell.

5. Drug-Receptor Interaction

6. Enzyme interaction - enzymes break down medications

7. Non-selective interaction - targets cell membrane

8. Selective interaction - inhibits or enhances

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Agonist VS Antagonist

(drug receptor interactions)

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Agonist = causes a reaction

Antagonist = blocks a reaction

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Pharmacotherapeutics

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a. The clinicaluse of drugs to prevent and treat diseases.

b. Defines principles of drug actions—the cellular processes that change in response to the presence of drugmolecules.

c. Drugs areorganized into pharmacologic classes.

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Contraindication

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Any patient condition, speciallya disease state that makes the use of the given medication dangerous for thepatient.

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Acute Therapy

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Often involves more intensivedrug treatment and is implemented in the acutely ill.

ex. ICU

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Maintenance Therapy

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Does not eradicatepre-existing problems the patient may have, but will prevent progression of adisease or condition.

ex. rx for hypertension

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Supplemental (replacement) Therapy

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Supplies the body with a substance needed to maintain normal function.

ex. insulin, hormone replacement

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Palliative Therapy

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Goal is to make the patientas comfortable as possible. Focus is on providing relief from pain, stress.

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Supportive Therapy

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Maintains the integrity of body functions while the patient isrecovering from illness or trauma.

ex. IV fluids

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Prophylactic Therapy

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Drug therapy provided to prevent illness or other undesirable outcomeduring planned events.

ex. pre-op antibiotics, birth control, acne tx...

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Empiric Therapy

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Based on clinical probabilities. It involves drug administration when acertain pathologic condition has a high likelihood of occurrence based on thepatient’s initial presenting symptoms.

ex. antibiotics

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Adverse effects

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Monitor for intended therapeuticaction (beneficial effects) and unintended possible effects (predictableadverse drug reactions).

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Toxic effects

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All drugs are potentially toxic and can have cumulative effects.

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Drug concentration

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Can be an important tool forevaluating the clinical response to drug therapy.

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Patient condition

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A patient’s response to a drugmay vary greatly depending on physiologic and psychological demands.

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Tolerance

Back 43

decreasing responseto repeated drug doses

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Dependence

Back 44

physiologic orpsychological need for a drug

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Physical dependence

Back 45

physiologic need for a drug to avoid physical withdrawal symptoms

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Psychologicaldependence

Back 46

also known as addiction and is the obsessive desire for the euphoriceffects of a drug

(start of addiction)

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Additive effects

Back 47

When two drugs are given together, so smaller doses of each drug can begiven (1 + 1 = 2)

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Synergistic effects

Back 48

Two drugs administered together interact in such a way that theircombined effects are greater than the sum of the effects for each drug givenalone (1 + 1 = greater than 2).

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Antagonistic effects

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Occur when the combination of two drugs results in drug effects thatare less than the sum of the effects for each drug given separately (1 + 1 =less than 2).

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Incompaatibility

Back 50

Two parenteral drugs or solutions are mixed together and the result isa chemical deterioration of one or both of the drugs or the formation of aphysical precipitate.

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Adverse drug event

Back 51

Any undesirable,occurrence involving medications.

*Two most common broad categoriesof adverse drug event are medicationerrors and adverse drug reactions.

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Adverse drug withdrawal event

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Adverse outcome associated with withdrawal of drug therapy too soon.

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Medication errors

Back 53

Preventable situation in which there is a compromise in the “6 rights” of medication use.

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Adverse drug reaction

Back 54

Any reaction to a drug that is unexpectedand undesirable and occurs attherapeutic drug dosages. Caused by processes inside a patient’s body.

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Medication useprocess includes 4 steps:

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1. Prescribing

2. Dispensing

3. Administering

4. Monitoring