Chapter 1 Flashcards
Drug
Drug: Any substance which brings about a change in biological function through its chemical action.
Come in many forms
Solids, e.g pills, tablets
Liquids and gels, e.g. syrup, ointments, creams
Vaporized liquids, e.g. inhalers, nose spray
Gaseous, e.g. anesthesia gas during surgery
Oxygen is a potent drug!!
Drug Routes
Oral – abbreviated “po” (pronounced: “pee-oh”)
Intravenous - abbreviated “IV” (pronounced: “eye-vee”) – injected directly into the vein – very rapid onset
Subcutaneous - abbreviated “SQ” – (pronounced: “sub-Q”) – injected into the subcutaneous fat layer of the skin. Ex: insulin; onset: depends on the medication.
Sublingual - abbreviated “SL” – under the tongue, absorbed by the large vessels in the floor of mouth. Ex: nitroglycerin for chest pain
Transdermal – absorbed through the skin – slow release. Ex: estrogen patch, nicotine patch, opioids (narcotic patch)
Intramuscular - abbreviated “I.M.” – “a shot”; med injected into the muscle; onset = 20-40 minutes; ex: flu vaccine
Pharmacokinetics versus Pharmacodynamics
Pharmacokinetics = Actions by the BODY on the drug.
Pharmacodynamics = Actions by the DRUG on the body.
Pharmacokinetics
Pharmacokinetics = the drug’s actions within the body and how the drug moves to and from the site of action
Actions by the BODY on the drug.
Bioavailability
Bioavailability: The extent to which the active drug or metabolite enters the general circulation, thereby permitting access to the site of action.
Most important concept: protein binding.
Most meds are bound to proteins in the blood, can travel along with the plasma protein in an inactive state, until it reaches its target organ or the body activates the medication.
Diseases that decrease amount of plasma/blood proteins: malnutrition, renal or hepatic problems
Note: all plasma proteins are made in the liver
Pharmacokinetics: 4 processes
Absorption: movement of a drug from the site of administration
Distribution: transport of a drug in the bloodstream
Metabolism: alteration of a drug in the body
Excretion: elimination of the drug or its compound from the body
Absorption
Absorption: the process of drug movement from the site of administration to the systemic circulation.
Many factors influence absorption: acidity of stomach; how fast GI tract is moving (e.g. fast with diarrhea less time for absorption); interference from other meds that may neutralize the drug.
Distribution
The reality: once a drug is in the body, the drug can go throughout the body. Hopefully, the drug will cause the desired action in the desired tissue or organ (Ex: pain). Other organs and body systems may also be affected: causing side-effects (e.g. nausea) or harmful/adverse reactions (e.g. low blood pressure or allergic reactions).
I.V. meds distribute rapidly & cause rapid responses
So, once the drug is in the body, you can’t take it out!
Metabolism
Metabolism: alteration of a drug in the body
The body must metabolism (break down) medications or the med’s actions will last longer than desired or build up to toxic/dangerous levels.
Most metabolism of medications is done in the liver.
Other sites for metabolism: Skeletal muscle, Kidneys, Lungs, Plasma, and Intestinal mucosa
Hepatic (Liver) “Cytochrome P-450” enzyme system: Most medications are broken down through these many enzymes. Cytochrome P-450 is frequently mentioned during discussion of medications and their bioavailability.
Excretion
Excretion: elimination of the drug or its compound from the body
Most excretion of medications is done in the kidney.
Other sites for excretion: the lungs (exhalation), the skin (sweating), the GI tract (defecation)
Drugs are excreted in many forms: doesn’t matter if the drug is an original compound, (parent compound), an active or an inactive metabolite –
Patients with renal (kidney) failure will not be able to excrete drugs efficiently
Drug levels will increase → Patients may experience more adverse effects and toxicity
Dosing: how often should a med be given?
Dosing – factors to consider: onset of action, peak concentration level (highest effective level in the body at that time), duration of action, and half-life.
The range of drug concentration in the blood lies between minimally effective level and a toxic level.
Half-life
The time required to change the amount of drug in the body by one half
Useful to determine the time to attain 50% of steady state; short half-life: wears off faster and give more often
Half Life
The time required to change the amount of drug in the body by one half
Rule: 5 half lives = 97% of drug elimination
Example: med with 4-hour half-life
4h 50%
8h 25%
12h 12.5%
Pharmacodynamics
Pharmacodynamics: the science of the effect of meds on the body and their mechanisms of actionor Actions by the DRUG on the body
Receptors
RECEPTORS are the classic “Lock and Key” mechanism: actions are activated or inhibited when the chemical (or med) interacts with the receptor site; the chemical (med) “turns the key” producing an effect or “blocks the key.”
AGONIST: a chemical/med that binds to receptor activates the receptor → Causes action;
A drug can CAUSE a reaction = AGONIST
ANTAGONIST: Binds to receptor but does not bring about a change and/or blocks other molecules (meds) from binding to the receptor site → Inhibits action;
A drug can PREVENT a reaction = ANTAGONIST
Agonists and Antagonists
Both Agonists and Antagonists are used in drug
therapy
AGONIST: A drug can CAUSE a reaction
Epinephrine/Adrenalin: binds to receptors in the heart (and many other areas) to increase heart rate and force of contraction
ANTAGONIST: A drug can PREVENT a reaction
Naloxone (Narcan): selectively binds and blocks opiate/narcotic receptors in the brain; given I.V. to reverse narcotic overdoses and respiratory arrest from narcotics