Pharmacology Clear and Simple – Ch. 2 – Basics of Pharmacology

pharmacokinetics
study of metabolism and action of drugs with emphasis on drug cycle

pharmacology
exploration of substances that are used to heal and comfort sick and help us live longer and healthier lives

absorption
how medication enters bloodstream, process by which a substances moves into the bloodstream from site where it was administered

metabolism
aka miotransformation; how our body breaks down the medication into usable components and waste products

medication given by mouth takes ____
much longer to enter bloodstream and to reach site where neeeded than does medication given directly into circulatory system

medication breakdown cycle, length of time
15 minutes to days

a medication taken orally must be transferred through the ______
stomach or intestinal mucosa into the circulating blood

how quickly a medication is absorbed depends on :
how it is administered and whether it’s topical or systemic

drug can be administered in 3 ways?
1. enterally, directly into GI system orally, rectally or through a tube entering this system
2. percutaneously, by intramuscular, intravenous, subcutaneous, or intradermal inection
3. percutaneously, by inhalation, sublingually, topically, or transdermally

4 phases of drug cycle:
1. absorption via gastrointestinal mucosa
2. distribution via circulatory system
3. metabolism via liver
4. excretion via kidneys

liquid medicine acts _____ than pills
faster

fastest way to the blood supply for a drug:
intravenous injection, drug is injected directly into a vein

be careful when administering intravenous medication because:
they could be absorbed too rapidly, like morphine causing patient to become severely hypotensive and stop breathing

other factors that can vary absorption rate:
fat and lipid solubility (ability to dissolve), medication’s pH, med concentration, length of contact, patient’s age, amount of food in stomach, depth of breathing

fat or lipid solubility: factor
the more soluble a medication is in fat or lipids, the more easily it is absorbed through stomach into intestines

pH: factor
low pH (acidic) meds are easily absorbed into stomach; high pH (alkalotic) are less likely to be absorbed effectively

concentration of the medicine: factor
the higher the med concentration, the more easily the med is absorbed

length of contact: factor
longer a topical med is on skin or mucosa, the more easily the med is absorbed

age: factor
both children and older patients absorb more meds through skin than healthy adults, so topical meds are applied in a thin layer

food: factor
a large amount of food slows the absorption of systemic meds; stomach acid facilitates absorption of systemic meds; medication is absorbed faster when stomach acid is increased

depth of breathing: factor
for inhalants, the more deeply patients breathe, the more meds they inhale

distribution
2nd phase of the drug cycle, delivery of the drug to the appropriate site after drug has been absorbed into bloodstream

barriers
physiological barriers, densely packed cells, like blood-placental barrier, blood-brain barrier, blood-testicular barrier

blood-placental barrier function:
helps to filter drugs and other substances passing from mother to fetus and protects fetus

what drugs can cross the blood-placental barrier?
alcohol, cocaine, some OTC drugs; most lipid-soluble drugs; psychotropic drugs

what drugs can’t cross the blood-placental barrier?
water-soluble drugs, antibiotics

blood-testicular barrier function?
protects male reproductive organs from toxins that could damage sperm; very little allowed through; psycotropic drugs can cause decreased libido

metabolism phase:
drug is metabolized by liver, kidneys, and intestines; medication is gradually transformed to a less active or inactive form

a medication is a _____ that the body does not normally require
foreign substance

____ _____ ____ metabolize drugs
liver, kidneys, intestines

_______ does most work of drug metabolism
liver

prodrugs category
a drug is adminstered in its inactive form to become activated through metabolism because the metabolite is the desired treatment

fosamprenavir (Lexica)
drug used to fight AIDS, is a prodrug

insulin given by mouth is____
virtually useless; stomach acid breaks down insulin to an inactive form before it can be absorbed into bloodstream

excretion: define
once a medication has acted in the body, it is excreted

methods of excretion:
through kidneys, or gas in lungs, bile, saliva, sweat glands, breast milk

cumulation
waste products that build up in the body

morphine buildup can cause
diminished or absent respiration

medication may not produce the desired effect if left in system _____
too long

toxic
when a medicine can become toxic or poisonous to the patient

gentamicin
medicine known to be nephrotoxic (toxic to kidneys) and ototoxic (toxic to ears)

potency
a drug’s power or strength, which increases and then decreases over time

taking more than one drug can affect:
potency

agonist:
drug that is taken with another drug so the two can work together; drug combo is more powerful than when taken alone (like Tylenol with Codeine)

synergism:
when each drug is taken separately

medication’s half-life:
length of time required for its concentration of a drug to decrease by 1/2 in the blood plasma and therefore affects the duration of potency for a medication

drugs with a long 1/2 life may need to be taken:
less frequently than those with a short 1/2 life

Antagonist drugs
do opposite by rendering another drug less powerful (like antibiotics taken with birth control pills)

therapeutic level of a drug can be affected by:
other drugs, nutritional factors, body size, environmental factors, gender, and culture

natural and herbal remedies can:
also interact with drugs and affect dosing

every medication carries a risk of:
side effects

side effects:
are usually mild, such as nausea, constipation, or sensitivity to light

adverse reaction:
severe side affect such as shock or death

topical drug has ____ than a systemic one
fewer side effects

diphenhydramine
Benadryl, an anti-inflammatory

side effects are usually classified by:
body system or organ

idiosyncratic reaction
a patient can have a unique reaction to any drug

for a serious reaction, report it to:
MedWatch program, run by the FDA

receptors
sites where medication binds to create a physiological effect

side effects of central nervous system CNS:
agitation, hallucinations, confusion, delirium, disorientation, depression, drowsiness, sedation, decreased respiration & circulation, dizziness & coma

flexeril (cyclobenzaprine) side effects:
dizziness and drowsiness

liver can be ____ if drugs accumulate in it
permanently damaged

these drugs can cause liver damage:
alcohol, acetaminophen, isoniazid, and asprin

jaundice:
sign of liver damage

GI system may suffer …. from medications
the most

GI side effects:
anorexia, nausea, vomiting, constipation, diarrhea; stomach ulcers, colitis

adding yogurt helps to prevent:
diarrhea

high-fiber laxative helps to prevent:
constipation

NSAIDS possible side effect:
ulcers

synthetic prostaglandin misoprostol (Cytotec)
appears to prevent development of ulcers

kidney damage signs:
fluid & electrolyte imbalance and abnormally high potassium levels

BUN
blood urea nitrogen

impaired kidneys cannot:
effectively metabolize medications processed in kidneys or excrete most metabolites from all medications

some medicines can cause ____
ototoxicity

oxygen is damaging to the:
eyes

anticancer drugs are especially toxic to:
bone marrow

if WBCs decrease,
you are more likely to have a higher risk of infection

if RBCs decrease,
patients will become anemic, weakness, fatigue, more difficulty in fighting off disease

Coumadin
an anticoagulant, to decrease blood clotting; should be carefully monitored for signs of bleeding, check if levels are toxic

2 medication resources:
1. comprehensive
2. clinical
both are available in print and online

comprehensive medication resources:
in depth and usually available only in print
USP/NF: United States Pharmacopoeial National Formulary
USP/DI: United States Pharmacopoeial Dispensing Information

USP/NF:
official source of medication info for drugs approved by FDA; updated every 5 years, with frequent supplements; provides standards for id, quality, strength, & purity of substances

USP/DI:
has 2 volumes; first is written primarily for prescriber, 2nd written in lay terms for patients to understand

PDR:
Physician’s Desk Reference, a more widely used comprehensive resource; contains info on thousands of drugs, indexed by trade name, generic name, class, and manufacturer, and has color pictures

PDR: white section: Section 1
Manufacturer’s Index; alphabetical listing of manufacturers w/addresses and phone #s

PDR: pink section: Section 2
Brand and generic name index

PDR: blue section: Section 3
Classification Index; lists drugs by classes, like antibiotics and analgesics

PDR: gray section: Section 4
Product Identification Guide; med photos; drugs listed by manufacturer

PDR: white section: Section 5
Product information section; detailed info like on package inserts, alphabetized by manufacturer and then product

PDR: white section: Section 6
Catch-all section: includes controlled substances, FDA pregnancy ratings, FDA phone directory, poison control centers, drug info centers, and look alike/sound alike drug names

FAS:
fetal alcohol syndrome

teratogenic
interferes with normal fetal development

What are the advantages of comprehensive books such as the PDR?
Great to have as a resource, in a hospital setting, and to look, up each drug, and study it, and see possible side effects, and if need for overdose, to contact poison control centers, or adverse side effects, to contact FDA

What are the disadvantages of comprehensive books such as th PDR?
It’s very big and heavy in size, not all information is in one spot, not updated frequently, not easily searchable like the Internet, don’t know if a drug has been recalled quickly enough

pocket guide/drug handbook:
optimal for easy access and often includes info a patient can understand; will indicate routes of drug administration, list appropriate dosages, indications/contraindications, explain how to educate patient regarding medication; some are supplemented with a CDROM or digital download for cell phone device

manufacturer’s package insert:
accompanies all drugs

pharmacist resources:
hospital or community based, can often answer questions for both health-care professionsals and patients when answers can’t be found elsewhere

True or False: Cumulation means a drug causes disease.
T, if buildup occurs, a patient can become very ill

True or False: An antagonist blocks a drug from being effective.
T Antibiotics can prevent birth control pills from being effective

True or False: A drug’s half-life is the time needed to decrease the drug’s plasma concentration by 50%
T

True or False: Psychotropic drugs can cross the blood-brain barrier.
T

True or False: Anticancer drugs do not cross the blood-placenta barrier.
F

True or False: Ototoxicity can damage the eyes.
F, it can cause damage to hearing and balance

True or False: Idiosyncratic means safe for children.
F

True or False: The primary organ of metabolism is the kidneys.
F It’s the liver

True or False: A package insert is a valuable source of info about medications.
T

True or False: BUN is a blood test looking at the function of the kidneys.
T

Which means leaving the body? A: Absorption B: Biotransformation C: Distribution D: Excretion E: Metabolism
D. Excretion

Which means moving through membranes: A: Absorption B. Biotransformation C: Distribution D: Excretion E: Metabolism
A: Absorption

Which means chemical alteration to another substance in the body? A: Absorption B: Biotransformation C: Distribution D: Excretion
B: Biotransformation

Which means moving of the medication from site of administration to the target organ? A: Absorption B: Biotransformation C: Distribution D: Excretion
C. Distribution

Ototoxicity occurs in the? A: Eyes B: Ears C: Liver D: Kidneys E: Brain
B: Ears

Nephrotoxicity occurs in the: A: Eyes B: Ears C: Liver D: Kidneys E: Brain
D: Kidneys

Which of the following are sources of info about medications: A: PDR B:USP/DI C: USP/NF D: Package insert E: all above
E: all of the above

Which term means the point at which a medication has the maximum desired effect? A: Therapeutic level B: Therapeutic range C: Toxic Level D: None of the Above
A: Therapeutic Level

Agonists are taken together to: A: Interact with or counteract each other B: Work together C: Cause great pain D: Relieve great pain
B: Work together

The section of the PDR that is a product identification guide is the? A: White section B: Pink C: Blue D:Gray
D: Gray section

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