module 11: basic pharmacology

Basic Pharmacology

What is a medication?

  • a substance used for medical treatment, especially a medicine or drug

Medications helps diagnose, treat, prevent, or manage disease

Differences between Chemical/Generic/Brand Names:

  • chemical:

  • Generic and brand: help providers and patients recognize the product more easily

Medication basics

  • dosage forms: liquids, tablets, capsules, injectables, etc.

  • Mechanism of action: how a drug produces its effect

  • Risk vs. benefit: every medication carries potential benefits and possible risks

Four approaches to treatment

  1. Cure: medications that eradicate or eliminate a disease

  2. Manage: medications that control a chronic condition over time

  3. Alleviate: medications that relieve symptoms but may not address root cause

  4. Prevent: medications that reduce the risk of illness or disease

Pharmacology: science of how drugs interact with living systems

2 Concepts:

  1. Pharmacokinetics: what the body does to the drug

ADME

A- Absorption

D- Distribution

M- Metabolism

E- Excretion

Bioavailability: percentage or fraction of a drug that reaches systemic circulation and can have an effect

Volume of Distribution (vD): theoretical space in the body that the drug appears to occupy; helps explain how widely a drug disperses into tissues

Metabolite: substance formed when the body chemically changes a drug, often in the liver; some metabolites are active and can exert therapeutic or toxic effects

Half-Life: the time it takes for the concentration of a drug in the bloodstream to reduce by half; influences dosing intervals and duration of therapy

  1. Pharmacodynamics: what the drug does to the body

Receptor Binding

  • lock and key

Agonists

  • exert their effect by activating the receptor

Antagonists

  • block other substances from activating the receptor

Key Pharmacology Terms

Drug: substance with therapeutic intent

Active ingredient: component producing the drug’s effect

Indication: the condition the drug is meant to treat

Contraindication: circumstances where a drug shouldn’t be used

Dose: the amount to be taken at one time

Frequency: how often the medication is to be administered

Duration: for how long the medication is to be administered

Quantity: how much medication is to be ordered

Adverse Effect: unintended, undesirable or harmful effect of a medication

Side effect: effect of a medication that are not intended as a part of its therapeutic use

Efficacy: drugs ability to produce desired result

Potency: concentration of drug needed for its effect

Prescription vs. Over-the-Counter (OTC)

  • prescription (RX): requires prescriber authorization, needs pharmacist oversight

  • Over-the-counter (OTC): readily available for self-medication

Dietary Supplements:

  • vitamins, minerals, and herbal products

→ may have therapeutic and adverse effects

→ can interact with medications

→ should be included in a patient’s medication history

Medication Use System

  1. Prescribing

  2. Transcribing

  3. Preparing

  4. Dispensing

  5. Administering

  6. Monitoring

  7. Transitioning

  8. Repeat

Pharmacist Job

  1. Inventory management

  2. Quality improvement

  3. Complicance

  4. Research

  5. Medication safety

  6. Operations

pharmacotherapy: treating disease with drugs

  • lifestyle modifications: changing patient’s diet, exercise, physical surroundings (e.g., removing a pet)

  • decreasing risk factors: eliminating tobacco, alcohol, illicit drugs, etc.

  • surgery:

  • pharmacotherapy: treating w/ prescription or nonprescription medications or dietary supplements

pharmacokinetics:

  • study of movement of drugs through the body

→ therapeutic doses: doses that produce the desired effects in people

some can be toxic to patients

4 Processes!

  1. absorption

  • drug enters the blood

EX: through transdermal patch, inhaled into nose or lungs, taken by mouth, injected, etc

bioavailability: describe ratio between amount of drug that reaches the blood & amount of drug placed into body

→ high bioavailability means most of the drug taken ends up getting into systemic circulation via blood

→ low bioavailability means a small amount of drug reach systemic circulation via blood

  1. distribution

  • movement of the drug through the blood and into various cells or tissues where it exerts its effect

  1. metabolism

  • chemical changes made to the drug by the body

→ often made by the liver but can sometimes be made by gastrointestinal wall, kidneys, lungs, or blood

liver is main metabolizing organ of the body!

→ has enzymes that metabolize drugs into inactive compounds, or metabolites.

→ they are contained in special structures of the liver, CYP 450 system

CYP 1A2 and CYP3A4 are enzymes that cause drugs to interact w/ each other because they both have effects on or are metabolized by specific enzymes in the system

inactive chemical = prodrug

  1. excretion

  • the drug or its metabolites leave the body, usually in urine or feces, sometimes through the lungs

→ can either be excreted as active drugs or inactive metabolites

the amount of drug excreted or metabolized to inactive compounds in a given organ or tissue over a certain amount of time is expressed mathematically

→ the time it takes for the serum drug concentration to decline by one-half is called = drugs half-life

Example of 4 Steps:

Alcohol!

alcohol is absorbed in stomach & first part of small intestine

→ moves through blood and into the brain, where it acts as a CNS depressant (slows down transmission of impulses among nerves in the brain)

  • metabolized in the liver, lungs, urine, and sweat to inactive compounds, including acetaldehyde. amount of acetaldehyde & other metabolites produced is predictably proportional to amount of alcohol in blood & also excreted through lungs and into the breath

pharmacodynamics: relationship between serum or tissue drug levels and drug effects

EX: higher concentration of BP drugs have more antihypertensive effects than do lower concentration

  • alcohol

→ low 50 mg/dL = euphoria

→ 100 mg/dL = impairment motor functions

→ 150-250 mg/dL = nausea and dysphoria

→ 300 mg/dL = loss of consciousness

→ 400 mg/dL = coma, sometimes death

strength of a drug is amount contained in a unit of the product, whether a tablet or tsp of liquid

EX: diazepam 5-mg tablets or amoxicillin suspension 150mg/5mL

  • some drugs have doses that can be therapeutic to one, but toxic to another

Dosage Forms Commonly Used

Solid Dosage Forms

  • pills

→ solid oral dosage forms that are made from a paste; rolled between first finger and thumb, then dried

  • tablets

→ powders that are compressed w/ enough force that they stay together during shipping but not enough force to prevent from dissolving in the body

→ can be swallowed, chewed and then swallowed, dissolved under the tongue or in buccal pouch, sometimes ground up if patient cannot swallow

  • capsules

→ gelatin containers w/ loose powders or timed-release beads inside

→ cheapest and easiest solid oral dosage form to make

Liquid Dosage Forms

  • solutions

→ liquid in which the drug is completely dissolved in the vehicle, making product clear (not necessarily colorless)

→ few oral solutions are used due to bitter taste, rather used for topical preparations (e.g., antibiotic solution used for acne)

  • suspensions

→ common liquid oral dosage form in which the drug is present in small particles in a flavored vehicle, suspensions never clear and must be shaken well to disperse the drug before a dose is measured

→ ex: liquid antibiotics used orally, anti-infective products used in the ears, etc. can be given to those who will not or cannot swallow

  • syrups and elixirs

→ used to mask the bitter taste of medicines. syrups are sweetened vehicles, elixirs contain alcohol

→ ex: most cough syrups and elixirs such as phenobarbital

Topical and Other Dosage Forms

  • creams and ointments

→ semisolid preparations used to deliver drugs to the skin or mucous membranes (nose, vagina). creams are water based and easily washed off, while ointments are fat based and resistant to removal w/ water.

→ ex: hydrocortisone cream and ointment. however they are not always interchangeable (when dealing w/ prescription product, selection must always be what the prescriber intended.

  • lotions (emulsions)

→ lotions, or products used to soften or deliver drugs to the skin = liquid preparations that have 2 phases. can be water phase dispersed into fat phase, OR small lipid globules dispersed in a water phase.

→ ex: calamine lotion & many others (vaseline intensive care & curel) which rehydrate or soften the skin

  • transdermal patches and subdermal inserts

→ drugs delivered through the skin using patches that control the rate of drug administration & through use of inserts that are surgically implanted under the skin

→ ex: nitroderm patches & implanon contraceptive inserts; patients ask if patches can be cut, do NOT advise patient either way without consulting pharmacist first, as each patch has specific instructions

Vaginal, Urethral, and Rectal Dosage Forms

  • suppositories

→ dosage form designed to remain solid at room or refrigerator temperature & to melt and release the drug when inserted into an orifice (opening) of the body

2 most commonly used:

- rectum or vagina, few suppositories are used in urethra of men

→ numerous agents are formulated as rectal suppositories (ex. phenergan, used when patients’ nausea and vomiting are so severe they cannot keep down the oral form of this drug) vaginal suppositories include antifungal agents (monistat)

→ vaginal contraceptives: gels, foams, jellies

Injectable Dosage Forms

  • injectable solutions

→ most are formulated as sterile solutions. depending on specific drug in solution, it can be injected into arteries, veins, or tissues or can be used to make large-volume solutions that are infused into body through a vein, artery, or peritoneal cavity (space around stomach, intestines, liver, etc)

→ be extremely careful to ensure you use right drug and strength. some drugs cannot be given intravenously, some cannot be injected into muscle

  • injectable suspensions

→ few injectable products are formulated as suspensions. they are always injected into muscle where they are absorbed into the blood. NEVER should be injected into veins or arteries, since the particles in them can get stuck in lungs & capillaries, causing serious injury or death.

→ ex: antibiotics; absorbed from intramuscular injections quickly. others, including antipsychotic agents, are made to be absorbed in a 3-4 week period

  • injectable emulsions

→ for when patients are unable to take food by mouth, they must be fed through veins and arteries (parenterally). lipid emulsions provide the fat that people normally get from their diets

→ ex: liposyn, intralipid, nutrilipid

generic name

  • given by the United States Adopted Names (USAN), a joint project of the American Medical Association, the United States Pharmacopeial Convention, and American Pharmacists Association (APhA).

  • any company that markets this drug is required by FDA to place its generic name on package label at least half the size of the company’s own brand name

brand name (trade or proprietary) name

  • given to the company that first marketed or created it.

dosage forms

  • oral

  • injectable

  • intranasal

  • topical administration

common uses

  • drugs officially approved for treatment or prevention of certain disease by FDA are called approved indications

adverse (side) effects

  • drug actions that occur at normal doses of a drug

→ toxic & toxicities refer to those effects that are produced when too much of a drug is used

contraindications/precautions

  • certain drugs either cannot be used or be used w/ caution in patients w/ more than 1 disease.

→ EX: nonprescription cough and cold products can raise blood pressure and affect blood glucose levels

  • another contraindication is patient allergy to a drug. when patients allergic to one drug and react similar to other drugs, they are said to exhibit cross sensitivities. these are then listed as precautions

storage considerations

  • all drugs will degrade or be changed into other substances when exposed to oxygen and/or water

  • rate at which drugs degrade is a function of their chemical structure and conditions under which they are stored.

→ lower temps slow degradation process

→ some drugs must be frozen, others can be stored at room temp but must be protected by extreme temperatures

drug interactions

  • when one drug prevents the absorption of another

  • involves interference w/ or changes in drug metabolism in the liver

  • food and herbal remedies can also interact w/ drugs