Basic Pharmacology ch. 9 and 10
Terms
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- Drug
- Chemicals used to diagnose, treat, or prevent disease.
- Pharmacology
- The study of drugs and their interactions with the body
- Chemical Discription
- The most detailedname for any drug.States its chemical composition and molecular structure. i.e. ethyl-1-methyl-4-phynylisonipecotate hydrochloride
- Generic Name
- usually suggested by the manufacturer and confirmed by the United States Adopted Name Council. Becomes the FDA official name when listed in the USP. Usually lower case.
- USP
- United States Pharmacopeia.The official standard for information about pharmaceuticals in the United States.
- Brand Name
- Also called trade name or proprietary name. a proper name and should be capitalized. Most mfg. register the name as a trademark.
- What are the 4 main sources of drugs
- Plants, animals, minerals and laboratory(synthetic)
- What are the sources for drug information?
- United States pharmacopeia (USP), Physicians Desk Reference (PDR), Drug Information, Monthly Prescribing Reference, AMA Drug Evaluation
- What are the components of a drug profile
- names, Classification, Mechanism of action, indications, pharmakinetics, side effects, contraindications, dosage, how supplied, special considerations
- Components of a Drug name
- Most frequently include the generic and trade names. Be aware of every name for each med.
- Classification
- The is the broad group to which the drug belongs.
-
mechanism of Action
pharmacodynamics - The way in which a drug causes is effects; its pharmacodynamics. The most important part of what we (EMS) are going to see.
- Pharmacokinetics
- How a drug is absorbed, distributed, metabolized(biotransformed), and excreted; how drugs are transported into and out of the body
- BEAD
-
Biotransformation
Elimination
Absorption
Distribution - Side Effects/Adverse Reaction
- Untoward effect: causes serious side effects. Undesired effects: Mild side effects.
- Routes of administration
- How the drug is given
- Contraindications
- Conditions that make it inappropriate to give the drug when the drug is simply not indicated. a predictable harmful effect will occur is the drug is given in this situation. May coinside with side effects.
- Dosage
- The amount if the drug that should be given
- Special Consideration
- How the drug may affect pediatric, geriatric or pregnant patients.
- pure Food and Drug Act of 1906
- Enacted to improve the quality and labeling of drugs. Named the USP the official source for drug info.
- Harrison Narcotic Act of 1914
- Limited the indiscriminate use of addicting drugs by regulating the importation, manufacture, sale and use of opium, cocaine and their compounds or derivatives.
- Federal Food Drug and Cosmetica Act of 1938
- Empowered the FDA to enforce and set premarket safety standards for drugs.
- Durham Humphry Admendments
- AKA the prescription drug amendments. required pharmacists to have either a written or verbal prescription from a dr. to dispense certain drugs. Also created over the counter meds.
- Comprehensive Drug Abuse Prevention and Control Act
-
AKA Controlled Substances Act. is the most recent majot federal legislation affecting drug sales and use. Repelled and replaced the Harrison Narcotic Act.
5 Schedules of Controlled Substances - Schedule 1
- high Abuse potential, leads to severe dependence, no accepted medical indications. Heroine, LSD, mescaline
- Schedule 2
- High Abuse potential, may leads to severe dependence, accepted medical indications. ie.e. opium, cocaine, morphine, oxycodone, methadone, secorbarbital
- Schedule 3
- Less Abuse potential may lead to moderate or low physical dependence, accepted medical indications. i.e. vicodin, tylenol with codeine
- Schedule 4
- Low abuse potential limited dependence. Diazepam, lorazepam, phenobarbital
- Schedule 5
- lower abuse potential, limited dependence, accepted medical indications. opioids often for cough or diarrhea
- drug laws and regulations
- State, Local , and Federal.
- assay
- Test that determines tje amount and purity of a given chemical in a preparation in the laboratory
- Bioequivalence
- relative therapeutic effectiveness of shemically equivalent drugs
- bioassay
- test to ascertain a drugs availability in a biological model.
- Drug Development Timeline
-
preclinical 1-3 years
Clinical Research 1-10 years (average 5)
NDA review 2 months to 7 years (average 24 months)
Post market Surveillance indefinite - 6 Rights of medication Administration
-
Right Medication
Right Dose
Right Time
Right Route
Right Patient
Right Document - Dose Packaging
- Medication packages contain a single dose for a single patient
- Teratogenic Drug
- medication that may deform or kill the fetus
- FDA Pregnancy Categories
-
A-no risk
B-no studies in pregnant woman(no risk in animals)
C-Adverse effects in animals=Use with caution
D-Fetal Risk Benefits could outweigh risks
X- Fetal Risk-risk outweighs any benefit to mother - Drug Free Availability
- Proportion of a drug available in the body to cause either desired or undesired effects.
- Broselow Tape
- Used to calculate drug doseges in pediatric patients
- Active transport
- requires the use of energy to move a substace.
- Carrier mediated diffusion or facilitated diffusion
- process in which carrier proteins transport large molecules across the cell membrane
- passive transport
- movement of a substance without the use of energy
- diffusion
- movement of a solute from an area of higher concentration to an area of lower concentration
- osmosis
- movement of solvent in a solution from an area of lower concentration to and area of higher concentration.
- Metabolism
- The bodys breaking down of chemicals into different chemicals
- biotransformation
- special name given to the metabolism of drugs. Occurs in the Liver.
- prodrug (parent drug)
- medication that is not active when administered, but whose biotransformation converts it into active metabolites.
- first- pass effect
- the livers partial or complete inactivation of a drug before it reaches the systemic circulation
- oxidation
- the loss of hydrigen atoms or the acceptance of an oxygen atom, This increases the positive charge on the molecule
- hydrolysis
- the breakage of a chemical bond by adding water, or by incorporating a hydroxyl group into one fragment and a hydrogen ion into the other
- enteral route
- delivery of a medication through the gastrointestinal tract
- parental route
- delivery of a medication outside of the gi tract, typically using needles to inject medications onto the circulatory system
- Types of enteral routes
-
Oral
orogastric/nasogastric (OG/NG)
sublingual(SL)
Buccal
Rectal - Types of Parental Routes
- IV, ET, IO, Umbilical, IM, SQ, inhalation/Nebulized, Topical, Transdermal, Nasal, Instillation, Intradermal
- Drug Forms (solid)
-
Pills-easy to swallow
Powders: powder form of tablet
Tablet- powder compressed
Suppositories- rectal or vaginal (mixed with wax)
capsul- gelatin filled with powder or tiny pills - Solutions
- Most common liquid preparation. Generally water based; some may be oil based
- Tinctures
- Prepared using an alcohol extraction process; some alcohol usually remains in the final drug preparation
- Suspensions
- Preparations in which the solid does not dissolve inthe solvent; if left alone the solid portion will precipitate out.
- Emulsions
- medications combined with a fat or oil emulsifier
- Spirits
- Solution of a volatile drug in alcohol
- Elixirs
- Alcohol and water solvent, often with flavoring added to improve the taste
- Syrups
- Sugar, Water and drug solution
- Types of Drug Actions
-
-Binding to a receptor site
-Changing the physical properties of cells
-Chemically combining with other chemicals
-altering a normal metabollic pathway - Receptor
- Specialized protein that combines with a drug resulting in a biochemical effect.
- Affinity
- Force of attraction between a drug and a receptor
- Efficacy
- A drugs ability to cause the expected response
- second messenger
- Chemical that participates in complex cascading reactions that eventually cause a drugs desired effect
- Down Regulation
- binding of a drug or hormone to a target cell receptor that causes the number of receptors to decrease
- Up regulation
- a drug causes the formation of more receptors than normal
- Agonist
- drug that binds to a receptor and causes it to initiate the expected response
- Antagonist
- drug that binds to a receptor but does not cause it to initiate the expected response
- partial agonist
- drug that binds to a receptor and stimulates some of its effects but blocks others
- competitive antagonism
- one drug binds to a receptor and causes the expected effect while also blocking another drug from triggering the same receptor
- noncompetitive antagonism
- the binding of a antagonist causes a deformity of the binding site that prevents an agonist from fitting and binding
- Irreversible Antagonism
- a competitive antagonist permanently binds with a receptor site
- iatrogenic
- a disease or response induced by the actions of a care provider. (physician produced)
- Drug response relationship
- correlation of different amounts of a drug to clinical response
- plasma level profile
- describes the lengths of onset, duration, and termination of action as well as the drugs minimum effective concentration and toxic levels
- Allergic Reaction
- AKA hypersensitivity. Effects occurs as the drug in antigenic and activates the immune system
- idiosyncracy
- drug effect that is unique to the individual, different than seen or expected in the population than general
- Cross Tolerance
- tolerance for a drug that develops after administration of a different drug.
- Tolerance
- decreased response to the same amount of drug after repeated administration
- tachyphylaxis
- rapidly occuring tolerance to a drug, may occur after a single dose. (usually occurs with decongestant and bronchodilation agents)
- cumulative effect
- increased effectiveness when a drug is given in several doses
- Drug Dependence
- the patient becomes accustomed to the drugs presence in his body and will suffer from withdrawal symptoms upon its absence
- Drug interaction
- the effect of one drug alter the response to another
- drug antagonism
- the effects of one drug blocks the response to another
- Summation
- AKA Addictive effect. two drugs that both have the same effect are given together to get the same effect. 1+1=2
- Synergism
- two drugs that both have the same effect that are given together to produce a resonse greater than the sum of their individual responses. 1+1=3
- Potentiation
- One drug enhances the effect of another. i.e. phenergan enhances morphine
- interference
- The direct biochemical interaction between two drugs, one drug affects the pharmacology of another
- onset of action
- the time from administration until a medication reaches it minimum effective concentration
- Minimum effective concentration
- minimum level of a drug needed to cause a given effect
- duration of action
- length of time the amount of drug remains above its minimum effective concentration
- termination of action
- time from when the drug levels drops below its minimum effective concentration until it is eliminated from the body
- therapeutic index (TI)
-
ratio of a drugs lethal dose (LD)for 50% of the population to its effective dose (ED) for 50% of the population.
LD50/ED50 - biologic half-life
- time the body takes to clear one half of a drug
- Drug response factors
- Age, body mass, sex, environment, time of admin, pathology, genetics, psychology
- 6 Rights of drug administration
-
right person
right drug
right dose
right time
right route
right documentation - percutaneous drug administration
- drugs applied to and absorbed through the skin
- transdermal
- slow and steady rate
- mucouse membrane admin
- drugs absorbed through mucous membranes at moderate to rapid rate
- Asepsis (Aseptic)
- a condition free of pathogens
- Local
- limited to one area of the body
- systemic
- throughout the body
- sterile
- free of all forms of life
- medically clean
- careful handling to prevent contamination
- disinfectant
- cleansing agent that is toxic to living tissue. Never use on living tissue
- antiseptic
- cleansing agent that is not toxic to living tissue. used to clean living tissue
- Topical Medication
- material applied to and absorbed through the skin or mucous membrane
- Mucous Membrane Sites of administration
- tongue, Cheek, Eye, Nose, Ear
- Abbreviations for Eye drug administration
-
o.d.-right eye
o.s. - left eye
o.u. - both eyes - Aural Medication
- Drugs administered through the mucous membrane of the ear and ear canal
- Pulmonary Medication Mechanisms
-
Nebulizer
Metered dose inhaler
Endotracheal tube - Metered Dose Inhaler
- Handheld device that produces a medication spray for inhalation
- LEAN
-
Endotracheal Medications
Lidocaine
Epinephrine
Atropine
Naloxone - Lozenge
- solid form of medication that slowly dissolve in the mouth, permitting gradual swallowing
- Hepatic Alteration
- change in a medications chemical compoisition that occurs in the liver
- Rectacl Administration
- a good method. Bypasses the liver and absorption in more predictable
- enema
- a liquid bolus of medication that is injected into the rectum
- bolus
- concentrated mass of medication
- Common rectal drugs
- Valium, Versed, Narcan
- Luer Adapter
- Nipple at the end of a syringe
- Luer Lock
- Ability to screw syringe into place
- Hypodermic Needle
- hollow metal tube used with the syringe to administer medication
- gauge
- the size of a needle's diameter. the lower the number the larger the diameter
- Kinds of parental drug containers
-
-glass ampules
- Single and multidose vials
- non constitutional syringe
- prefilled syringe - Ampule (Amp)
- breakable glass vessel containing liquid medication
- Vial
- plastic or glass container with a self sealing top
- non constituted drug vial/mix-o-vial
- vial with two containers, one holding powdered medication and the other holding a liquid mixing solution
- Prefilled/preloaded syringe
- syringe packaged in a tamper proof container with the medication aready in the barrel
- medicated solution
- parental medication packaged in an IV bag and administered as an IV infusion
- infusion
- liquid medication delivered through a vein
- Parenteral routes
- ID, SQ, IM, IV, IO
- intradermal (ID)
- I.e. PPD. Deposit medication into the dermal layer of the skin. 15 degree angle
- Subcutaneous (SQ)
- the layer of loose connective tissue between the skin and the muscle. Pinch skin and go in at a 45 degree angle
- IM sites
- Deltoid, Dorsal Gluteal above pocket to avoid sciatic nerve, Vastus lateralis, Rectus Femoris
- IV Access
- AKA cannulation. surgical puncture of a vein to deliver medication or withdraw blood
- Peripheral venous access
- surgical puncture of a vein in the arm, leg or neck
- Central Venous Access
- Surgical puncture of the internal jugular, subclavian or femoral veins
- Peripherally inserted central catheter
- PICC line threaded into the central circulation via a peripheral site. Used for long term care.
- Huber Needle
- Angled needle that attaches to the ports of a PICC. Only needle that can be used with these ports
- Colloid
- intravenous solutions containing large proteins that cannot pass through capillary membranes
- Crystalloid
- IV solutions that contain electrolytes but lack the larger proteins associated with colloids
- Crystalloid Classes
-
Isotonic
Hypertonic
hypotonic - Isotonic
- state in which solutions on opposite sides of a semipermeable membrane are in equal concentration
- Hypertonic
- State in which a solution has a higher concentraton on one side of a semipermeable membrane than on the other side
- Hypotonic
- state in which a solution has a lower solute concentration on one side of a semipermeable membrane than on the other side.
- Common Colloids
- Plasma Protein Fraction (Plasmanate), Salt Poor Albumin, Dextran, Hespan
- Microdrip
- 60 gtts per 1mL
- macrodrip
- 10 gtts per 1mL
- over the needle catheter/angiocatheter
- semiflexible catheter enclosing a sharp metal stylet.
- heparin lock
- peripheral iv cannula with a distal medication port used for intermittent fluid or medication infusions.
- saline lock
- peripheral iv cannula with a distal medication port used for intermittent fluid or medication infusions. Saline is injected onto the device to maintaain its patency
- Venous access device
- surgicall y implanted port that permits repeated access to central venous circulation
- infusion controller
- gravity flow device that regulates fluids passage through an electromechanical pump
- extravascular
- outside the vein
- infusion pump
- device that delivers fluids and medications under positive pressure
- blood tube
- glass container with color coded, self sealing rubber top
- vacutainer
- device that holds blood tubes
- luer sampling needle
- long, exposed needle that screws into the vacutainer and is inserted directly into the vein
- Brand Name Drugs
- Should be Capatalized, do not contain the (cemical composition or the ",USP" at the end
- Official Name for Drugs
- Not capatilized and contain the ",USP" at the end
- Reference Materials, Sources for Drug information
- USP (United States Pharmacopeia, PDA, Dring Information, Monthly Prescribing Reference, AMA Drug Evaluation
- Physician Drug Reference (PDA)
- A compilation of drug inserts, printed fact sheets that drug mfg. supply, includes 3 indices and a section containing photos of drugs
- Drug Information
- Published by the American Society of Health System Pharmacists. Contains an authoratative listing of monographs on every drug used in the USA
- Monthly Prescribibg Reference
- Designed to Assist physicians in prescribing medication and which are available to treat certain diseases
- AMA Drug Evaluation
- published by the American Medical Association
- Plants (Source of Drugs)
- Oldest Source. Digitalis
- Why is there federal drug regulation?
- To protect the public from adulterated and mislabeled drugs
- Durham Humphry Amendment
- Required pharmacists to have either a written or verbal presciption from a physician to dispense drugs
- Schedule I
- High Abuse Potential; may lead to severe dependence; no accepted medical indications; used for research, analysis or instruction only
- Schedule II
- High Abuse Potential; may lead to severe dependence; accepted medical indications
- Schedule III
- Less abuse potential than Schedule I and II; may lead to moderate or low physical dependence or high psychological dependence; accepted medical indications
- Schedule IV
- Low abuse potential compared to Schedule III; limited psychological and/or physical dependence; accepted medical indications
- Schedule V
- Lower abuse potential compared to Schedule IV; may lead to limited physical or psychological dependence; accepted medical indications
- New Drug Development Phase I
- To determine the drug's pharmacokinetics, toxicity and safe dose in humans. Carried out on limited population of volunteers. High risk drugs not carried out on humans
- New Drug Development Phase II
- Drug is tested on limited population of patients who have the disease it is intended to treat. Primary purpose is to find therapeutic drug level
- New Drug Development Phase III
- Main purpose is to refine the usual therapeutic dose and to collect data on side effects. Usually in a double blind study
- New Drug Development Phase IV
- Involves postmarket analysis during conditional approval. MFg. monitors its performance
- FDA Classification of newly approved drugs
- Method utilizes a number and a letter for each new drug in the IND phase or upon NDA review of the FDA.
- IND Phase
- Investigational New Drug. This phase is designated by the FDA if the results of animal testing are satisfactory
- Free Drug Availability
- Proportion of a drug in the body to cause either desired or undesired effects
- Extracellular Fluid in Neonates
- 80% (adults 50%-55%)
- Pharmacodynamics
- How a drug interacts with the body to cause its effects
- Nubain (Nalbuphine)
- Agonist-Antagonist. Stimulates some of the opioid agonists analgesic properties but partially blocks others such as respiratory depression.
- What is the most common second messenger?
- cAMP cyclic adenosine monophosphate
- Naloxone (Narcan)
- Antagonist. Binds to the opiate receptor, but will not initiate pain relief but does block narcotics and its response
- mannitol (osmotrol)
- increases urine output by increasing the bloods osmotic pull
- Prototype
- drug that best demonstrates the classes common properties and illustrates its particular characteristics
- Central Nervous System
- Brain and Spinal Cord
- Peripheral nervous System
- Broken down into Autonomic and Somatic
- Somatic Nervous System
- Controls Voluntary "Motor" functions
- Autonomic Nervous System
- Controls involuntary functions. Broken down into Sympathetic and Parasympathetic
- Sympathestic Nervous System
- Fight or Flight
- Parasympathetic Nervous System
- Feed or Breed
- Morphine
- Opioid Drug. Decreases cardiac preload and afterload. Analgesia, Euphoria, sedation. Useful in MI.
- Non Opioid Analgesic
- Aspirin, Buprofen, acetaminophen
- opioid Antagonist
- reverse effects of opioid drugs, such as narcan
- Adjunct medication
- enhances other drug effects. i.e. valium and versed.
- Opioid Agonist Antagonist
- displays both agonist and antagonist properties. i.e. Nubain and stadol
- Antianxiety and hypnotic drugs
- benzodiazepines and barbituates. Decreases response to stimuli by increasing effectiveness of GABA
- GABA
- Gamma-aminobutyric acid. Chief inhibitory neurotransmitter in the CNS.
- Romazicon (flumazenil)
- benzodiazeprine Antagonist(antianxiety, sedative/hypnotic) Reverses sedation
- Antagrade
- After administration of medications
- MAOI
-
Antidepressent Medication
Monoamine oxidase inhibitor. DO NOT EAT CHEESE AND RED WINE (both contain tyramine) - EPS
- Extrapyramidal Symptoms. Common side effects of antipsychotic medications. including muscle tremors and parkinsonism like effects
- mimetic
- to mimic and increase response
- Autonomic ganglia
- groups of autonomic nerve cells located outside the CNS
- preganglionic nerves
- Nerve fibers that extend from the CNS to the autonomic ganglia
- postganglionic nerves
- nerve fibers that extend from the autonomic ganglia to the target tissues
- synapse
- space between nerve cells
- neurotransmitter
- chemical messenger that conducts a nervous impulse across a synapse
- neuron
- nerve cell
- cholinergic
- pertaining to the neurotransmitter acetylcholine
- adrenergic
- pertaining to the neurotransmitter norepinephrine
- Location of ganglia in the sympathetic nervous system
- close to the spinal cord
- Acetylcholine
- Utilized in the preganglionic nerves of the sympathetic nervous system and in both the pre and postganglionic nerves of the parasympathetic nervous system.
- Norepinephrine
- is the postganglionic neurotransmitter of the sympathetic nervous system.
- 2 main types of ACh receptors
- nicotinic and muscarinic
- nicotinic
- muscle. receptors are found at the neuromuscular junction and initiate contraction (somatic)
- Muscarinic
- (organ) found in many organs throughout the body responsible for promoting the parasympathetic response.
- Parasympathomimetics
- Cholinergics. drug or other substance that causes effects like those of the PNS
- Parasympatholytics
- Anticholinergic. drug or tother substance that blocks or inhibits the actions of the PNS
- SLUDGE
- Salivation, Lacrimation, Urination, Defecation, GAstric Motility, Emesis. Adverse effect of cholinergics.
- Atropine
- Muscarinic Cholinergic Antagonist.
- sympathomimetic
- drug or other substance that causes effects like those of the SNS. Adrenergic
- sympatholytic
- drug or other substance that blocks the actions of the SNS. Antiadrenergic.
- Types of Sympathetic receptors
-
Adrenergic
-alpha 1
-alpha 2
-beta 1
-beta 2
Dopaminergic - Alpha 1
-
Response to stimuli
-vasoconstriction
-ejaculation - Alpha 2
-
Response to stimuli
-inhibits the continued release of NE - Beta 1
-
Response to stimuli
-increase HR
-increased conductivity
-increased automaticity
-increased contractility
Renin release - Beta 2
-
Response to stimuli
-Bronchodilation
-Vasodilation
-inhibits uterine contraction
-tremors - dopaminergic
-
response to stimuli
-vasodilation (increased blood flow) to the kidneys - Beta Blockers
- Adrenergic Antagonists. used to treat tachcardia, hypertension, and angina. Causes bronchoconstriction and inhibited glycogenolysis. all end with olol.
- fast potential
- found in myocardial contractile tissue
- Slow potential
- found in av and Sa nodes
- Antidysrhythmic
- used to treat and prevent abnormal cardiac rhythms
-
Vaughn-Williams Claasifications
Sodium Channel Blockers -
Class 1A-widening QRS, Prolonged QT
Class 1B-widening QRS, Prolonged QT (lidocaine)
Class 1C- Prolonged PR, Widening QRS
I- prolonged PR, widening QRS -
Vaughn-Williams Classifications
Beta Blockers - Prolonged PR, bradycardia
-
Vaughn-Williams Classifications
Potassium Channel Blockers -
prolonged QT
indication in VFIB causes initial release of NE. delayed repolarization. -
VAugh-Williams Classifications
Calcium Channel Blockers -
Prolonged PR, bradycardia (verapimil)
decrease SA and AV node automaticity -
Vaughn-Williams Classifications
Misc. - Adenisine, prolonged PR, bradycardia