Pharmacology 120

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Pharmacology 120

Instructor

Susan Dolezal, R.N., M.S.

Introduction: Chapter 1

Definition of Pharmacology: the study of drugs and their actions on living organisms

Nurses need to have medication knowledge because nursing responsibilities include the safe:

Administration of drugs

Assessment of effects of drugs

Intervening to make drug regimens more tolerable

Provision of patient teaching about drugs and the drug regimen

Sources & Evaluation of Drugs

Drugs may come from plants (digoxin, opiates), animals (beef insulin), inorganic compounds (iron & gold salts), or be produced synthetically (Humulin insulin).

The Food & Drug Administration (FDA) regulates the development & sale of drugs

The FDA had established five categories to indicate the potential for systemically absorbed drugs to cause birth defects.

The FDA also determines the abuse potential of controlled substances, and has established categories for ranking these drugs

Drug Approval Process

FDA tightly controls drug testing, to evaluate the safety and effectiveness of new drugs.

Nurse Practice Acts - Every state has its own laws regarding drug administration by nurses. Can get a copy.

In a civil court, the nurse can be prosecuted for giving the wrong drug or dosage, omitting a drug, or giving the drug by the wrong route.

Drug Names

Each drug may have several names

Chemical Name - Describes the drug’s chemical structure (most meaningful to the chemist)

Generic Name - Official name for the drug

- Not owned by any drug company

- Universally accepted (i.e. acetaminophen)

Brand/Trade Name - A registered trademark of a drug company, easier to spell/pronounce (Tylenol) - Cardizem (brand) diltiazem HCL (generic)

Drug Approval: Pregnancy

FDA developed a classification system related to the effects of drugs on unborn child

(fetus)

In drug books and literature, pregnancy category is indicated for most drugs

- A - No risk to fetus based on studies

- B - Little to no risk based on animal studies,

some human studies

- C - Risk indicated based on animal studies. Evaluate risk vs. benefit .

- D - Risk to fetus proved. Risk vs. benefit to mother

- X - Risk proved. Avoid during pregnancy

Controlled Substances Schedule

1970 - The Controlled Substance Act passed to remedy drug abuse/dependence.

Included scheduling of controlled drugs into classifications:

- CI - Illegal drugs (highest abuse potential – i.e. Heroin)

- CII - High potential for abuse (physical & psychological)

& dependency (narcotics, amphetamines, barbiturates)

- CIII - Combo drugs (Codeine preparations) High

potential for abuse/dependency

- CIV - Medium potential for abuse/dependence (anti-anxiety meds such as Valium)

- CV - Limited potential for abuse (Codeine cough syrup)

Over-The-Counter (OTC) Meds

Over-the-counter (OTC) drugs are products that are available without a prescription for self-treatment of various problems

Many patients do not report use of OTC meds, as they do not consider them to be

“real medicines”; health care workers must ask about their use!

OTC meds can still be dangerous if not taken correctly (limit on acetaminophen dosing!), can interact with other medications, and can mask signs & symptoms of underlying disease (headaches & HTN)

Where To Get Information!

• Physician’s Drug Reference (PDR)

Nursing Drug Handbooks

Internet Drug Sites: Drug Formulary at: http://www.intmed.mcw.edu/drug.html

Package inserts that come with new meds

The hospital pharmacist

• 24 hour Walgreen’s or Osco pharmacist!

(Be careful with the review questions/answers in the textbook - they aren’t all correct for Chapter 1!)

Chapter 2: Drugs and the Body

Definition of Pharmacology: the study of drugs and their actions on living organisms

3 Phases for drug action to occur:

1 – Pharmaceutic: how the drug gets into the body

2 – Pharmacokinetic: how the body acts on the drug

3 – Pharmacodynamic: how the drug affects the body

* Please refer to the Terms & Definitions sheet attached to your syllabus!

Pharmacodynamics

Categories of Drug Action

4 categories of drug action: (example!):

- replacement (insulin)

- stimulation of cellular activities (Type II DM meds)

- depression or slowing of cellular activities (SSRIs)

- to interfere with the functioning of foreign cells, such as invading microorganisms or neoplasms (chemotherapeutic agents: antibiotics and cancer medications)

Pharmacodynamics

Receptor Theory

Most receptors are protein in structure and found on cell membranes

Drugs act through receptors either by binding to the receptor to produce a response

(agonist) (i.e. insulin letting glucose into the cell) or by blocking a response

(antagonist) (i.e. SSRIs block removal of serotonin from receptor sites – more serotonin available to cell, less depression)

Almost all drugs lack specific and selective effects; those which are specific (such as penicillin) are said to have selective toxicity.

These other effects may be desirable or harmful (i.e. cancer chemotherapy kills tumor cells, but also causes hair loss & anemia)

Phase 1:

Pharmaceutic

Approximately 80% of drugs are taken by mouth and pharmaceutic (dissolution) is the first phase of drug action. Oral administration is the cheapest & safest way to administer drugs, but stomach acid may interfere – hence the use of binders which are broken down at particular acidity levels, then releasing the active drug.

• In GI tract - drugs need to be in solution to be absorbed

Solids (tablets, capsules) must disintegrate into small particles to dissolve into liquid

(dissolution)

Liquid drugs are already solutions

Pharmaceutic

Disintegration - breakdown of the tablet into smaller particles

Dissolution - dissolving of the smaller particles in GI fluid before absorption

Rate limiting - time it takes the drug to disintegrate and dissolve to become available for the body to absorb it

Pharmaceutic

Drugs dissolve faster in acidic environments

- Older adults/infants have less acid; slower absorption leads to toxicity (WHY?)

Enteric coated tablets do not disintegrate until reaching the alkaline environment of the small intestine – (they are designed to do this) - DO NOT CRUSH them!

Phase 2:

Pharmacokinetics

The process of drug movement to achieve drug action

4 processes: Absorption, Distribution, Metabolism (Biotransformation), and Excretion

(elimination) - ADME

The nurse must be alert to any adverse drug effects and to report such findings promptly

Critical concentration – the amount of drug needed to cause a therapeutic effect; may use a loading dose to achieve more quickly

Phase 2:

Pharmacokinetics

Dynamic Equilibrium of drug concentration is affected by the 4 processes of pharmacokinetics:

Absorption – from the site of entry into the body

Distribution – to the active site

Metabolism (Biotransformation) – in the liver

Excretion (elimination) – from the body

Pharmacokinetics: Absorption

Passage of drug from its site of administration into the blood/circulating body fluids

Rate of absorption depends on the route of administration: Enteral (via GI tract), parenteral (injected), topical (through the skin), inhaled into the lungs, through mucous membranes (sublingual, buccal)

Absorption

Some drugs are absorbed into the small intestine via the extensive mucosal villi.

When is absorption compromised?

Hydrochloric acid (which we all have in our stomachs!) destroys some drugs – so a much larger oral dose must be given to offset the dosage loss. (Compared to dosage of same med given IV or IM.)

Ideally, (for consistent absorption) all oral drugs should be given 1 hour before or 2 hours after meals.

Absorption

Bioavailability is a subcategory of absorption – it refers to the percentage of the administered drug dose that reaches the systemic circulation

Occurs after absorption and hepatic drug metabolism

Oral route is always less than 100% - due to first- pass effect (next slide!)

Intravenous route is usually 100%

Absorption

First Pass Effect: drugs that are taken orally are usually absorbed from the small intestine directly into the portal venous system; the portal veins deliver these absorbed molecules directly into the liver. In the liver, much of the drug becomes inactive & is excreted. Some drugs, such as aspirin & alcohol, do not undergo metabolism in the liver at all; they are absorbed into the body from the lower end of the stomach.

Pharmacokinetics:

Distribution

The ways in which drugs are transported by the circulating body fluids to the sites of action

Influenced by blood flow, affinity to the tissue, and protein binding effect

Drugs are distributed in the plasma (liquid part of the lymph and blood) and are bound by varying degrees to protein (albumin)

Distribution

Portion of drug bound to protein is inactive - not available to receptors; drug must be freed from the protein’s binding site at the tissues.

Portion of drug unbound is free, active

- only free drugs can cause a pharmacologic response

- some circulating drugs (anticonvulsants, aminoglycosides) are checked for drug blood levels

Distribution

Need to be aware of the condition of your client - liver or kidney disease = low serum albumin level = less protein-binding sites = excess free drug. What happens?

Remember - The amount of drug that actually reaches the receptor sites determines the extent of pharmacologic activity

Pharmacokinetics:

Metabolism or Biotransformation

Major mechanism of the termination/inactivation of drug action

Liver is primary site where drugs are inactivated by liver enzymes, becoming inactive metabolites or water- soluble substances for excretion

Liver disease alters drug metabolism = drug toxicity d/t a decreased rate of metabolism

Drug removal from the body

Main route is through the urine

Pharmacokinetics:

Excretion

- other routes = bile, feces, lungs, breast

milk, skin, saliva

Urine pH influences excretion

Kidney disease affects excretion (like liver disease, leads to build up of drug and toxicity)

Half-life (t1/2) - the time it takes for 1/2 of a drug to be eliminated; after 5 half-lives,

>96% of drug is eliminated.

Phase 3:

Pharmacodynamics

Def: How the drug affects the body

Drug response can cause a primary or secondary physiologic effect, or both

Primary effect = desirable

Secondary effect = desirable or undesirable (i.e. Benedryl –antihistamine >sleepy)

Pharmacodynamics

Onset, Peak, Duration

Onset of action = time it takes to reach the minimum effective concentration

Peak action = When the drug reaches its highest blood or plasma concentration

Duration of action = Length of time drug has an effect (this is where knowing the t ½ and the condition of the patient’s liver & kidneys comes in handy!)

Pharmacodynamics

Therapeutic Index/Range

Safety of drugs is a major concern

Therapeutic index - estimates the margin of safety of a drug

Low therapeutic index = narrow safety

High therapeutic index = wide safety margin, less danger of toxic effects

Therapeutic range = area between the minimum effective concentration & minimum toxic concentration of a drug

Pharmacodynamics:

Factors Influencing Drug Effects

Info in drug books is based on the reaction (to the drug) on a healthy, 150 # male!

Weight: if < 150 #, normal dosage might prove toxic; if > 150#, normal dose might not cause desired response

Age: children need to have dosages converted appropriately. Older adults usually need lower doses as well, due to decreased plasma proteins, & decreased liver & kidney function.

Factors Influencing Drug Effects (cont.)

• Gender: males have more vascular muscles; so IM injections act more quickly in men than women; women have more fat cells; so drugs deposited in fat (like gas anesthetics) act much longer in women.

Physiological factors: diurnal rhythm of the nervous & endocrine systems, acid-base balance, & electrolyte balance all affect the way the drug works in each individual

Pathological factors: i.e. GI disorders can affect the absorption of many oral drugs; vascular diseases & low B/P affect the distribution of drugs: not enough “umph” to get drug to tissues where it is needed. Liver & kidney disease:

Factors Influencing Drug Effects (cont.)

Genetic factors: cultural differences due to differences in enzyme levels

Immunological factors: drug allergies

Psychological factors: placebo effect: drug works best when patient believes it will work. Health beliefs (trust), & compliance with treatment

Environmental factors: heat & vasodilators for hypertension, sedating drugs & calm, quiet environment

Factors Influencing Drug Effects (cont.)

Tolerance: patient may develop tolerance to drugs over time, requiring larger dose to achieve initial effect.

Cumulation: if drug doses taken too close together, drug accumulates in the body, leading to “overdosage” and toxic effects

Drug-drug interactions: when two or more drugs are taken together, they can increase of decrease the efficacy of one or both drugs. Can occur during all phases (ADME).

Check drug handbook.

Drug-food interactions: i.e. tetracycline & milk

Drug-laboratory interactions: i.e. change in liver enzymes

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