Chapters 1-3 & 5-7 Flashcards
Adverse Effect
General term for undesirable and potentially harmful drug effect
Chemical Name
Name that defines the chemical composition of a drug
Agonist
Drug that binds to a receptor and activates a physiologic response or drug action
Contraindications
Situations or conditions when a certain drug should not be administered
Antagonist
drug that binds to a receptor and interferes with other drugs or substances from producing a drug effect
Dose
A measurement of the amount of drug that is administered
Drug
Chemical substance that produces a change in the body function
Drug Indications
intended or indicated uses for any drug
ED50
Effective dose 50, or dose that will produce an effect that is half of the maximal response
Generic Name
Nonproprietary name of a drug
controlled substance
drug that has the potential for abuse and thus is regulated by law
LD50
Lethal dose 50, or a dose that will kill 50 percent of the laboratory animals tested
Mechanism of Action
Explanation of how a drug produces its effects
Nonprescription, over the counter (OTC) drug
Drug that can be purchased without the services of a physician
Pharmacology
Study of drugs
Receptor
Specific cellular structure that a drug binds to in order to produce a physiologic effect
Side Effect
Drug effect other than the therapeutic effect that is usually undesirable but not harmful
Site of action
Location within the body where a drug exerts it therapeutic effect, often a specific drug receptor
Therapeutic effect
Desired drug effect to alleviate some condition or symptom of disease
Therapeutic index (TI)
Ration of the LD50 to the ED50 in animal studies
Toxic effect
Undesirable drug effect that implies drug poisoning can be very harmful of life-threatening
Trade Name
Patented proprietary name of a drug sold by a specific drug manufacturer; also referred to as the brand name
What are the Major areas of Pharmacology? (6)
Pharmacodynamics Pharmacokinetics Pharmacotherapeutics Pharmacy Posology Toxicology
Pharmacodynamics
Study of the action of drugs on living tissue
Pharmacokinetics
Study of the processes of drug absorption, distribution, metabolism, and excretion
Pharmacotherapeutics
Study of the use of drugs in treating disease
Pharmacy
Science of preparing and dispensing medicines
Posology
Study of the amount of drug that is required to produce therapeutic effects
Toxicology
Study of the harmful effects of drugs on living tissue
Duration of action
Length of time that a drug continues to produce its effect.
Time-Plasma Drug Concentration or Time response Curve
The relationship of time and the plasma drug concentration
The US Pharmacopoeia/National Formulary (USP/NF)
Official drug list recognized by the US government
The Physicians’ Desk Reference (PDR)
Reference most widely used by physicians, pharmacist, and nurses for info relating to the use of drugs in the practice of medicine
Schedule I (Drugs)
Drugs with high abuse potential and no accepted medical use
Ex- heroin, hallucinogens, marijuana (not to be prescribed)
Schedule II (Drugs)
Drugs with high abuse potential and accepted medical use
Ex- narcotics (morphine and pure codeine) cocaine, amphetamines, short-acting barbiturates (amobarbital, secobarbital), nabilone. No refills without a new written prescription from the physician
Schedule III (Drugs)
Drugs with moderate abuse potential and accepted medical use
Ex- moderate- and intermediate-acting barbiturates Dronabinol, anabolic steroids, preparations containing codeine plus another drug: prescription required, may be refilled five times in 6 months when authorized by the physician
Schedule IV (Drugs)
Drugs with low abuse potential and accepted medical use
Ex- phenobarbital, chloral hydrate, zolpidem (Ambien), anti anxiety drugs (Librium, Valium) prescription required, may be refilled five times in 6 months when authorized by the physician
Schedule V (Drugs)
Drugs with limited abuse potential and accepted medical use
Ex- Narcotic drugs used in limited quantities for antitussive (codeine) and antidiarrheal purposes (diphenoxylate, Lomotil) drugs can be sold only by a registered pharmacist buyer must be 18 years old and show identification. Some states require a prescription for schedule V drugs
Bio-availability
Percentage of the drug dosage that is absorbed
Drug absorption
Entrance of a drug into the bloodstream from its site of administration
Drug addiction
Condition of drug abuse and drug dependence that is characterized by compulsive drug behavior
Drug dependence
Condition of reliance on the use of particular drug, characterized by physical and or psychological dependence
Drug distribution
Passage of a drug from the blood to the tissues and organs of the body
Drug metabolism
The enzymatic bio transformation of the drug into metabolites
Drug excretion
Elimination of the drug from the body
Drug microsomal metabolizing system (DMMS)
Group of enzymes located primarily in the liver that function to metabolize (bio transformation) drugs.
Drug tolerance
Decreased drug effect occurring after repeated drug administration
Enzyme induction
Increase in the amount of drug metabolizing enzymes after repeated administration of certain drugs
Enzyme inhibition
Inhibition of drug-metabolizing enzymes by certain drugs
First- pass metabolism
Drug metabolism that occurs in the intestines and liver during oral absorption of drugs into the systemic circulation
Half-life
Time required for the body to reduce the amount of drug in the plasma by one-half.
Individual variation
Difference in the effects of drugs and drug dosages from one person to another
Intramuscular injection (IM)
Route of drug administration – drug is injected into gluteal or deltoid muscles.
Muscle
Intravenous injection (IV)
Route of drug administration drug is injected into a vein
Loading dose
Initial drug dose administered to rapidly achieve therapeutic drug concentrations
Maintenance dose
Dose administered to maintain drug levels in blood in the therapeutic range
Oral administration
Route of drug administration that does not involve the gastrointestinal (GI) tract
Alcoholic Preparations (Drug Form)
Elixirs, spirits,tincutres, and fluid extracts are drugs dissolved in various concentrations of alcohol, usually in the range of 5-20 percent
Aqueous Preparations (Drug Form)
Syrups (a solution of water and sugar to which a drug is added)
Powders (Drug Form)
Powders are drugs or drug extracts that are dried and ground into fine particles
Tablets
Drug powders that have been compressed into a convenient form for swallowing. Usually disintegrate in the stomach more rapidly than most other solid preparations
Troches and Lozenges (Drug Form)
Flattened tablets are allowed to dissolve in the mouth; commonly used for colds and sore throats
Capsules (Drug Form)
Gelatin capsules are used to administer drug powders or liquids; dissolve in the stomach thereby releasing the drug
Delayed- Release Products (Drug Form)
Usually tablets or capsules that are treated with special coatings to that various portions of the drug will dissolve at different rates. Usually contain the equivalent of two or three single dose units. Designed to produce drug effects over extended time
Enteric- Coated Products (Drug Form)
Drug tablet or capsule coated with an acid-resistant substance that will dissolve only in less acidic portions of the intestines. Should be take on an empty stomach with water, either 1 hour before or 2 hours after meals.
Suppositories (Drug Form)
Drugs mixed with a substance (cacao butter) that will melt at body temperature. Are intended for insertion into the rectum, urethra, or vagina.
Ointments (Drug Form)
Or salves are soft, oily substances (petrolatum or lanolin) containing a drug that applied to the skin or in the case of ophthalmic ointments to the eye
Transdermal Products (Drug Form)
Administered through a bandage or patch system. Released from the bandage or patch and is then absorbed through the skin into the systemic circulation. Provides continuous source of drug of 24 hours or more Nitroglycerin estrogen and clonidine are drugs available in this form
Parental Injection (Drug Forms)
Involves the administration fo drugs by needle and syringe Different injection sites such ad subcutaneous (SC) intramuscular (IM) intravenous (IV) and others provide different rates of drug absorption and onset of action. Requires the practice of sterile technique and various safety precautions
Oral Administration (PO) (Routes of Administration)
Safest and most convenient method
30-60 min before significant absorption from the GI tract occurs, therefore the onset of the drug action is delayed
Can be removed (if need be) within the first few hours
Parenteral Administration Include?
Routes of Administration
Any route that does not involve the GI tract, including inhalation, hypodermic injection and topical application.
Intramuscular injection (IM)
Intravenous injection (IV)
Inhalation
Topical Application
Ex- most medications – aspirin, sedatives, hypnotics, antibiotics
Sublingual (Routes of Administration)
Takes several Minutes
Buccal (Routes of Administration)
Several minutes
Convenient dosage from for certain drugs
Ex- nitroglycerin in angina pectoris
Rectal (Routes of Administration)
15 to 30 min
When a patient cannot take oral medications and parenteral is no indicated, also for local effects
Ex- analgesics, laxatives
Transdermal (Routes of Administration)
30-60 min
Convenient dosage form that provides continuous absorption and systemic effects over many hours
Ex- nitroglycerin, estrogen
Subcutaneous (SQ)(Routes of Administration)
Into Fat
Several min
For drugs that are inactivated by the GI tract
Ex-insulin
Intramuscular (IM)(Routes of Administration)
Into Muscle
Several min
For drugs that have poor oral absorption, when high blood levels are required and when rapid effects are desired
Ex- narcotic analgesic, antibiotics
Intravenous (IV)(Routes of Administration)
Into Vein
Within 1 minute
In emergency situations where immediate effects are required, also when medications are administered by infusion
Ex- IV fluides (dextrose) nutriment supplementation, antibiotics
Intraarterial(Routes of Administration)
Within 1 min
For local effects within an internal organ
Ex- cancer drugs
Intrathecal(Routes of Administration)
Several minutes
For local effects within the spinal cord
Ex- spinal anesthesia with lidocaine
Inhalation(Routes of Administration)
Within 1 min
For local effects within the respiratory tract
Ex- anti asthmatic medications such as epinephrine
Topical(Routes of Administration)
Within 1 hour
For local effects on the skin, eye, or ear
Ex- creams and ointments
Vaginal(Routes of Administration)
15-30 min
For local effects
Creams, foams, and suppositories
Lipid Solubility(Drug Absorption)
In general, the more lipid soluble a drug is, the faster it will pass through a lipid substance like the cell membrane. With exception of general anesthetics (highly lipid soluble), most drugs are primarily water soluble and only partially lipid soluble
Drug Ionization(Drug Absorption)
Ionized drugs are charged molecules because their atomic structure had los or gained electrons. The molecules then become either positively or negatively charged. In General, ionized drug molecules do not readily cross cell membranes. The unionized(uncharged) form of the drug is required in order for absorption to occur
Drug Formulation (Drug Absorption)
Drug particles can be formulated into different sizes, such as crystals, micronized particles or ultra micronized particles. The smaller the size of the drug particle the faster the rate of dissolution and absorption
What factors determine how much drug reaches any one organ or area of the body? (3)
- Plasma protein binding
- Blood flow
- The presence of specific tissue barriers.
Plasma Protein Binding (Drug Distribution)
Several different proteins (albumin and globulins) are in the plasma and form a circulating protein pool they help regulate osmotic pressure (oncotic pressure) in the blood and transport many hormones and vitamins. Many drugs are attracted to plasma proteins, especially albumin The result is that some drug molecules are bound to plasma proteins while some drug molecules are unbound (free in circulation) only the unbound or free drug molecules can exert a pharmacological effect.
Blood Flow(Drug Distribution)
Largest blood supply – liver, kidney and brain so they are exposed to largest amount of drug.
Adipose tissue receive a relatively poor blood supply so they do no accumulate large amount of drug. However, highly lipid soluble drugs can enter adipose tissue easily where they can accumulate and remain for an extend period of time
Blood- Brain Barrier(Drug Distribution)
An additional lipid barrier that protects the brain by restricting the passage of electrolytes and other water soluble substances.
The brain is composed of large amount of lipid(nerve membranes and myelin)lipid soluble drugs pass readily into the brain. Rule of thumb- a drug must have a certain degree of lipid solubility if it is to penetrate this barrier and gain access to the brain
Drug Excretion (4)
Renal Excretion
GI Excretion
Respiratory Excretion
Miscellaneous
Renal Excretion (Drug Excretion)
After the blood is filtered through the glomerulus of the kidneys, most of the filtered substances are eventually reabsorbed into the blood
Exceptions – urinary waste produces and anything else that is nonabsorbent form.
GI Excretion (Drug Excretion)
After oral administration a certain portion of the drug (un-absorbed) passes through the GI tract and is excreted in the feces.
After the drug is released into the intestines it maybe absorbed from the intestines back into the blood again. Referred to as the enterohepatic cycle.
Miscellaneous (Drug Excretion)
Some drugs and drug metabolites also can be detected in swear, saliva, and milk (lactation)
Respiratory Excretion (Drug Excretion)
Some drugs are metabolized to products that can be exchanged from the blood into the respiratory tract. General anesthetic gases are not totally metabolized. These drugs are excreted primarily by the lungs
Blood Drug Levels
Intensity of drug effect is mainly determined by the concentration of drug in the blood or plasma
List Factors of Individual Variation
- Age
- Weight
- Sex and percent of body fat
- Genetic variation
- Emotional state
- Placebo effect
- Presence of disease
- Patient compliance
Weight (Factors of Individual Variation)
In small individuals the code may have to be reduced. In larger individuals the dose may be to be increased (doesn’t always hold true)
Age(Factors of Individual Variation)
Infants children and elderly are generally more sensitive to actions of drugs than are younger adults
Sex and percent Body Fat
Factors of Individual Variation
Females possess a higher%of body fat and lower % of body water = greater drug effect than males b/c the drug is dissolved into a smaller volume of body fluid. Lipid soluble drugs are more widely distributed and may produce longer duration of action in females than in males. Same concept applies to the difference in the body fat composition between members of the same sex
Genetic Variation
Factors of Individual Variation
Individuals tend to inherit the proteins and enzyme patterns of their parents.
Emotional State
Factors of Individual Variation
An individual who is excited or extremely anxious may require a larger dose of hypnotic or tranquilizer than an individual who is not emotionally stimulated but who still has difficulty sleeping.
Placebo Effect
Factors of Individual Variation
Patients claim an improved condition even though they receive no real drug
Presence of Disease
Factors of Individual Variation
Presence of other diseases that are debilitation or decrease the function of some vial organ usually makes an individual more susceptible to the effects and adverse reactions of drug therapy
Patient Compliance
Factors of Individual Variation
Drug compliance refers to taking a drug exactly as prescribed. If dosages are forgotten or skipped, the drug effects will be reduced or absent. Aka non compliance.
Teratogenic
Cause birth defects.
Incompatibility (Drug Interactions)
Refers to physical alterations of drugs that occur before administration when different drugs are mixed in the same syringe or other container
Addictive Effects (Drug Interactions)
When the combined effect of 2 drugs each producing the same biological response by the same mechanism of action, is equal to the sum of their individual effects.
Summation (Drug Interactions)
When the combined effect of 2 drugs each producing the same biological response but by a different mechanism of action, is equal to the sum of their individual effects
Synergism (Drug Interactions)
When the combined effect of 2 drugs is greater than the sum of their individual effects
Antagonism (Drug Interactions)
When the combined effect of 2 drugs is less than the sum of their individual effects
Creatine
A metabolite of muscle metabolism that Is excreted in the urine in proportion to renal function
Creatinine clearance
A measure of renal creatinine excretion that is used to evaluate renal function
Drug compliance
Following a drug prescription directions exactly as written
Enterohepatic recycling
Process whereby drug is eliminated from the live/biliary tract into the GI tract and then reabsorbed from the GI tract back to the liver
Geriatrics
Medical specialty that deals with individuals over 65 years of age
Mixed- function oxidase system
Drub microsomal metabolizing enzymes (DMMS) that decrease with age and who the rate of drug oxidation metabolism
Polypharmacy
Situation in patients whose treatment involves multiple drug prescriptions
Drug absorption (Elderly)
Decreased intestinal blood flow, surface area and motility delay drug absorption and slow onset of drug action
Drug metabolism (elderly)
Decreased liver blood flow , liver organize, and enzyme concentrations decrease the rate of drug metabolism and increase the duration of intensity of drug action
Drug Distribution (Elderly)
Decreased body water, lean body mass, and plasma proteins along with increased fat content increase plasma drug concentrations and pharmacologic effects
Drug Excretion (elderly)
Age related decreased in renal function and blood flow slow the rate of drug excretion and increase the duration of intensity of drug action
Acetylcholine (ACH)
Neurotransmitter of parasympathetic (cholinergic) nerves; stimulates the cholinergic receptor
Adrenergic
Refers to the nerves that release norepinephrine
Adrenergic receptor
Receptor located on the internal organs that responds to norepinephrine and epinephrine
Afferent nerve
Transmits sensory info from the peripheral organs to the brain and spinal cord (central nervous system)
Autonomic ganglion
The collection of synapses between the pre and post ganglionic nerve fibers
Autonomic nervous system (ANS)
System of nerves that innervate smooth and cardiac muscle (involuntary) of the internal organs and glands
Cholinergic
Refers to nerves that release acetylcholine
Efferent nerve
Carries the appropriate motor response from the brain and spinal cord to the peripheral organs
Cholinergic (muscarinic)receptor
Receptor located on internal organs and glands that responds to acetylcholine
Epinephrine (EPI)
Hormone from adrenal medulla that stimulates adrenergic receptors, especially during times of stress
Fight or flight reaction
Response of the body to intense stress caused by activation of sympathetic division of ANS
Homeostasis
Normal state of balance amount the body’s internal organs
Muscarinic receptor
Cholinergic receptor located on the cell walls of internal organs and glands
Nicotinic receptor
Cholinergic receptor located on autonomic ganglia (Nn) and skeletal muscle (Nm)
Neurotransmitter
Substance that stimulates internal organs to produce characteristic changes associated with sympathetic and parasympathetic divisions.
Norepinephrine (NE)
Neurotransmitter of sympathetic (adrenergic) nerves that stimulates the adrenergic receptors
Parasympathetic
Refers to nerves of ANS that originate in the brain and sacral portion of the spinal cord’ they are active when the body is at rest or trying to restore body energy and function
Postganglionic nerve fiber
Autonomic nerve fiber that travels from the autonomic ganglia to the internal organs and glands
Preganglionic nerve fiber
Autonomic nerve fiber that emerges from the cranial nerves and spinal cord and that travel to the autonomic ganglia where it synapse with the postganglionic nerve fibers
CNS =
Central Nervous System
Sympathetic
Refers to nerves of the ANS that originate from the thoracolumbar portion of the spinal cord; they are active when the body is under stress or when it is exerting energy
PNS=
Peripheral nervous system
Somatic division and Visceral Division (Autonomic Nervous System)
Somatic division
branches of the cranial and spinal motor nerves that innervate skeletal muscle (voluntary) Conscious or voluntary control of the cerebral cortex
Visceral Division (Autonomic Nervous System/ ANS)
Branches of the cranial and spinal motor nerves that innervate cardiac and smooth muscle (involuntary) of the internal organs and glands. NOT under Conscious control, are regulated by the hypothalamus and medulla oblongata
Adrenergic Neuronal Blocker
Drug that acts at the neuronal nerve endings to reduce the formation or release of NE
Alpha-adrenergic drug
Drug that stimulates the alpha adrenergic receptors
Alpha-1 adrenergic blocker
Drug that blocks the alpha-1 effects of NE and EPI
Alpha-1 adrenergic receptor
Receptor located on the smooth muscle that mediates smooth muscle contraction
Alpha-2 adrenergic receptor
Receptor located on the adrenergic nerve endings that reduce the release of NE
Beta-1 adrenergic receptor
Receptor located on the heart that increases the heart rate and force of contraction
Beta-2 adrenergic receptor
Receptor located on smooth muscle that relaxes smooth muscle when stimulated
Catecholamine
Refers to norepinephrine, epinephrine and other sympathomimetic compounds that possess the catechol structure
False transmitter
Substance formed in nerve endings that mimics the interferes with the action of the normal neurotransmitter
Non selective beta adrenergic blocker
(refer to page 72 Table 6.2)
Drug that blocks both beta 1 and beta 2 adrenergic receptors
Nonselective beta adrenergic drug
refer to page 72 Table 6.2
Drug that stimulates both beta 1 and beta 2 receptors
selective beta-1 adrenergic blocker
refer to page 72 Table 6.2
Drug that blocks only beta 1 receptors
selective beta-2 adrenergic drug
refer to page 72 Table 6.2
Drug that stimulates only beta 2 receptors at the therapeutic doses
sympatholytic
Refers to the action of an adrenergic blocking drug or an action that decreases sympathetic activity
sympathomimetic
Refers to the action of an adrenergic drug or an action that increases sympathetic activity
Acetylcholinesterase
An enzyme that inactivates acetylcholine
Anticholinergic
Refers to drugs or effects that reduce the activity of the parasympathetic nervous system
Cholinergic
Refers to the nerves and receptors of the parasympathetic nervous system also refers to the drugs that stimulate the system
Muscarinic receptors
An older but more specific term for the cholinergic receptor on smooth and cardiac muscle
Nicotinic-muscle (Nm) receptor
Cholinergic receptor located on both sympathetic and parasympathetic ganglia
Parasympatholytic
Refers to drugs (anticholinergic)that decreases the activity of the para sympathetic nervous system
parasympathomimetic
Refers to drugs (cholinergic) that mimic stimulation of parasympathetic nervous system
Therapeutic Index
Ratio/lethal dose (LD) to effective dose (ED)
larger the TI the safer the drug
True/False The Mechanism of action explains how a drug produces its effects
True- the mechanism of action refers to the specific biochemical actions that occur that allows the drug to produce the desired effect
Competitive Antagonism
when an antagonist and agonist bind to the same receptor and are administered together they compete with each other for the same receptor site. The action produced depends on which occupies the most receptors
Intradermal
Into skin layer
Intracritular
Into Joint (shoulder)
Absorption
passage of substance through the membrane into the blood stream
As a rule of thumb- drugs that are lipid soluable do what?
pass readily to the brain
Prego A
safe to take
Prego B
animal studies show no risk but haven’t been tested on women
Prego C
greater risk than A and B
Prego D
adverse effects to fetus
ONLY GIVEN if the mother absolutely needs it.
Prego x
fetal risk clearly out weighs the benefit
Prego NR
not been rated by FDA
Somatic Nervous System (SNS)
voluntary control of skeletal muscle
Autonomic Nervous System (ANS)
Involuntary Control
Sympathetic
“fight or flight”
Parasympathetic
“talks to during rest and digest”
