Unit 1: Pharmacology resources Flashcards
Drug manufacturers must submit prescription drug label information (prescribing information) in an _______
o Do a Google search for the drug prescribing information o For example: Nexium prescribing information o Then, look for the PDF link from the manufacturer
• The DailyMed System is available online to all. The full prescribing information (FPI) will be organized in a _________ SPL) format o You can even email it to yourself!
electronic format
“structured
product labeling”
WHAT IS THE PERFECT DRUG?? _____ of the drugs we study will meet ALL these criteria!!
• highly potent
• 100% selective for the part of the body being treated
• completely safe
• have no side effects or drug interaction
• be universally affordable.
none
3) What is the basic pharmacological profile for the drugs in a particular class?(usually, this will be labeled as the “CLASS” of drug) ?
absorption degradation and elimination potential drug-drug interactions monitoring requirements use in subpopulations like pediatrics and pregnancy
What is the safety profile of the drug or drug class? What ______ monitoring should be done for this drug.
special patient
What is the safety profile of the drug or drug class? What ______ monitoring should be done for this drug.
special patient
5) What NON-pharmacologic interventions might be included in treating this condition?
• how do they contribute to holistic care of the patient? 6) Selection of drugs for special patient populations:
- age, sex, reproductive status
- comorbidities, medication history, allergies
- cultural issues
- polypharmacy
Drugs change biologic functioning via _____ on cells.
chemical action
______ is the study of how chemicals interact with living systems (cells, organs, organisms) and involves understanding cell biology, receptor theory, biochemistry.
pharmacology
Some drugs are actually chemicals our own body makes called ____.
endogenous substances
Drugs administered to a person are called _____.
exogenous substances
i.e. our bodies make endogenous cortisone every day, and we use exogenous prednisone as a drug
______ is when humans use drugs to treat and prevent disease, sometimes for recreational or religious/cultural use.
Applied pharmacology
______ is the undesirable effects of chemicals on living systems.
Toxicology
______ is the undesirable effects of chemicals on living systems.
Toxicology
______ are harmful drugs and/or inorganic toxins
Poisons
______ are poisons of biologic origin (organics).
Toxins
An ____ is the smallest part of matter, elements are made up of only one type of atom (e.g. Oxygen), molecules (compounds) are composed of more than one type of atom (e.g. H2O).
atom
______ is the total atomic weight of all the atoms in a molecule.
Molecular weight (MW)
_____ exists in three physical states of solid, liquid, gas; these characteristics are determined by ambient pressure & temperature.
matter
_____ are
based on carbon (C), hydrogen (H), oxygen (O), nitrogen (N) and some Sulfur (S). o Often written as “CHONS”…98% of the earth’s crust is made of these chemicals,
including our bodies.
Organic compounds
_______ are elements other than CHONS o may be BULK inorganics (e.g. calcium, sodium) o may be TRACE inorganics (e.g. selenium, boron)
Inorganic compounds
_____ is the solid substance that is dissolved in the liquid o Solvent: the liquid (which is always water in living systems)
Solute
_____ are electrically charged particles in solution.
ions
_____ are positive charged ions.
cations
______ are negatively charged ions.
anions
______ are ions in living systems.
electrolytes
Neutral means no _____ charge.
electrical
pH measures how ___ the solution is which is defined by the concentration of positively charged hydrogen ions (H+)
acidic
____ are chemicals that can accept a hydronium ion (H+) in solution.
bases
The _____ state of the chemical(drug) affects the route of administration possible when the drug is given to the body.
physical state
Liquids or solids can be taken _____.
orally
Liquids can be injected via intravenous, intramuscular, and _____.
intradermal
_____ are inhaled such as anesthetic gases.
gases
The state of matter of a substance depends on the environmental temperature and ______, so normally we think of a drug as existing in liquid, solid or gas state at “standard” room temperature and pressure. Sometimes, we alter the environment
pressure
Example: we compress gases such as oxygen by putting them under pressure in pressurized canisters so that we can transport larger amounts of oxygen in a smaller space (the same number of molecules takes up less space when pressurized into a liquid in the canister)
The size and shape of the chemical (drug) is the ____.
molecular weight (MW)
Drug sizes range from very small (atomic Lithium, MW 7) to huge (like alteplase, t-PA, protein MW 60,000) but the average drug is somewhere in the middle, MW _____.
100 - 1,000
____ must be big enough so that the drug unique enough to have specific biochemical activity. But, if it is TOO large, it may have difficulty moving between body compartments
Size
example: the drug alteplase is very large & cannot leave the vascular space,
works intra-vascular as a thrombolytic clot-buster that we give to patients having a heart attack or stroke
Some _____ come in the racemic form.
drugs
Mirror images around a central axis (called optical chirality, chiral drugs,
stereoisomerism, enantiomer, isomers, dimers, racemes) o ____ based on the rotation around a carbon atom due to the rotation of polarized light
racemes
Racemes with a carbon atom that rotates to the left of polarized light is called _______
left or levo rotatory
Racemes with a carbon atom that rotates to the right of polarized light is called _______
right or dextro-dextrorotatory oriented
______ are therefore mirror images of each other.
isomers
_____ activity of the left/right isomers may vary
biologic
Receptor binding may be different, enzyme activity may be different and may even be ______ in one orientation and helpful in the opposite orientation !
toxic
Biologic systems NORMALLY make right/left versions of ________ synthesized molecules
endogenously
o biologic example: “reverse” T3 from the peripheral tissue de-iodination of T4 o drug example: ofloxacin and levofloxacin (Levaquin) – the levo-rotatory
version of the drug is much more powerful as an antibiotic o Other common example:
• dextrose is simply D-glucose (dextro-rotatory glucose, dextro- glucose), an isomer of glucose that is found in honey and sweet fruits; dextrose (dextrorotatory form of glucose found naturally in animal and plant tissue and also can be derived synthetically from starch)
• Dextrose 5% in water (D5 W) is a “maintenance fluid” and isotonic (iso- osmotic) as administered intravenously and thus does NOT hemolyze cells
• HOWEVER, since the cells take up the glucose and metabolize it, the net effect is as though you are giving PURE WATER (“FREE” water) and is distributed as such throughout the total body water (2/3rd to ICF and 1/3rd to ECF with the ECF fluid distributed one fourth to plasma & three-fourths to interstitial fluid) • think of how things appear in the mirror
• hold up your own hands, thumb to thumb – the right hand and the left hand look like mirror images of each other – but you CANNOT superimpose one hand over the other (due to the “handedness” they are NOT exactly the same!!)
Chemical bonding is when one chemical ____ or associates with another
attaches
______ bonds are less common in drug effects, since they are strong and are rarely reversible
Covalent
Weak bonds more commonly used by drugs; more _____ in action as drug can dissociate (separate) away after the initial bonding
reversible
Electrostatic bonds rely on ______ attraction.
electrical
Hydrophobic (water hating) bonds are very _____.
weak
Sometimes the specific actions of a drug rely on the “fit” into a cell’s enzymes or
______. The better the “fit” using these weak bonds allows for a more ______ drug action
receptors
specific
Inert substances do not bond, but can still have _____ effects, e.g. some anesthetics.
clinical
Laws of thermodynamics promote _____ (disorganization) of substances
entropy ?
Concentration differences (gradients) causes solute to passively diffuse from high to low concentration areas without any _____ being required.
energy.
Remember, the electrical charge of a substance is dependent on the ____ of the solution as well as the acid/base characteristics of the substance.
pH
Hydrophilic ionized (charged) substances are more water _____
soluble
Lipophilic (Hydrophobic): neutral (uncharged) substances are more lipid ______
soluble
Amphiphilic means that the drug is BOTH water AND ____ soluble.
lipid
Water solubility drugs need to get into the “water compartment” (the plasma in our bloodstream) in order to travel to their location of ______ in the body
activity
Lipid solubility drugs need to get past the phospholipid cell membrane to get
out of the bloodstream and into the ______
tissues
Transport proteins (TP): SOME drugs that are more ______ are still able to get across cell membranes due to the presence of a transporter protein (TP) molecule embedded in the cell membrane that carries the drug into the cell
hydrophilic
▪ Examples: the very hydrophilic statin drug, pravastatin (Pravachol), needs a special TP to get into the liver cell and do its work o Toxicity may occur if the drug is able to enter a part of the body where it has
the potential to do harm, theoretical increased risk of adverse effect
_______ drugs can cross the Blood Brain Barrier (BBB)
Lipophilic
The BBB blocks ______ drugs from entering the brain
hydrophilic
Any drug needed to work in the _____ must be lipophilic
brain
▪ example: may affect which antibiotic can be used to treat meningitis o Trapping of drugs can occur in certain areas of the body due to the pH of the body fluids there; not all body fluids are the same pH (urine, semen, breast milk)
▪ example: we can use this to our advantage by choosing drugs that concentrate in the urine and thus can be used to treat urinary tract infections (UTI)
Everything in blood plasma doesn’t get into _____ and the brain
CSF
Once a substance gets into the CSF, the entire brain is exposed to the ______. This can occur if substances are able to cross the BBB o this can occur if substances are injected directly into the ______ (intrathecal drug
injections)
substance
ventricles
________ (astrocyte cells that are supporting cells of the brain) that selectively
absorb substances from the blood
neuroglia
________ between endothelial cells that make up the brain capillaries (brain
capillaries are less “leaky”).
Tight junctions
Brain areas without the BBB include the pituitary, hypothalamus, and _____. Why? in these areas, the brain needs to _______ the body’s internal environment
for regulation of bodily functions.
pineal
sample
What crosses the BBB important clinically? Enters _____: similar to cell membrane rules.
easily
What crosses the BBB? lipid soluble (alcohol, anesthetic agents —lipophilic and water and gases (carbon dioxide, _____)
oxygen
Proteins & Electrolytes or any other large molecules → many therapeutic drugs (e.g. antibiotics) are _____ in plasma & can’t enter CSF.
protein
bound
CLINICAL: difficulty in treating meningitis/encephalitis/cerebral abscesses & brain
dysfunction (e.g. depression) – can’t get some chemicals into the brain.
Therapeutic objectives (target outcomes) are the expected ______ of the drug. These should make sense within the context of the pathophysiology of the condition
benefit
The DOC is the ____.
drug of choice
Usually, the drug of choice (DOC) is first-line therapy for that condition. This means this drug will probably:
o work the ____
o be effective when used alone (monotherapy)
o will have the least ____ to the patient with the condition
best
toxicity
______ are the reason to use the drug (the medical condition)
Indications:
______ are what the Food & Drug Administration (FDA) has legally determined the clinical condition for which the drug should be used – this is called label approved
Label indications
_______ use often clinicians will prescribe drugs that are not label approved for a specific condition because the science of the drug and the available clinical evidence has demonstrated that the drug will work.
OFF label
___________ are possible reasons NOT to use the drug in that particular patient. These reasons may be patient age, sex, reproductive status, allergies,
comorbidities or other factors.
Contraindications
_______ do not give the drug under any circumstances.
Absolute contraindications
_____ the need for the drug is so great as to overcome
the possibility of an adverse drug reaction; the provider should perform extensive documentation in the chart and disclosure of potential risks to the patient – this is a ________
Relative contraindications
“risk/benefit decision”
Legal (Licit) Drugs in the USA consist of ____ classes of licit (legal) drugs. The two classes are prescription (legend) and _____.
two
Over-the-counter (OTC) and Behind-the-counter (BTC)
______ and marketing is subject to federal authority through the Food and Drug Administration (FDA); only drugs approved by the FDA are legal in the USA
drug labeling
The ____ book lists all approved drugs in the USA>
organge
Drugs with abuse potential are further regulated under the restrictive authority of the Drug Enforcement Administration (DEA). These are _____ and are also called “Schedule Drugs”
“controlled substances” (CS)
Controlled substances or schedule drugs are grouped into Schedules ______ based on abuse potential. Federal laws (and sometimes state laws) govern their availability and who may
prescribe
1-V
Some drugs are illegal in the USA due to their ______.
CS schedule
Often you will hear the acronym CSA which refers to the ______(the legislation passed in 1970 that created these “schedules”) which are updated annually
Controlled Substances
Act
_____ (in some years, more than half) of all drugs consumed in the USA are OTC.
Half
____ can be safely self-administered by the lay person for self-limiting conditions that are non- life-threatening, and that do not represent potential for loss of LIFE, LIMB or EYESIGHT.
OTC
Labeling on these OTCs should be such that a ______ can understand indications, contraindications & directions for use.
lay person
