Pharmacology 1 Flashcards
Introduction. Slides 1-77
What is Pharmacology
Study of drugs and their interactions with the body
Pharmacokinetics
how drugs get in and out of the body (how they MOVE)
Pharmacodynamics
how drugs affect the body (what they DO)
Safety, drug approved for human testing. Small amount of participants
Phase 1
Safety and Dosing. what is the dose and efficacy. Longer then phase 1. ⅓ pass this phase.
Phase 2
Phase 3
Safety and Eficacy. Against the current standard. Bigger sample. Years of investigation. Needs FDA approval for next phase
Phase 4
Post approval surveillance. What effects cause over time.
Important Drug Information
Names
Classification
Mechanism of action
Indications & Contraindications
Dosage & How Supplied
Routes of Administration
Pharmacokinetics
Pharmacodynamics
Side Effects/Adverse Reactions
4-chloro-N-furfuryl-5-sulfamoylanthranilic acid
is
Chemical Name
The name furosemide is the
Generic Name
The name Lasix is the
Brand Name
The names are capitalized
Brand names
The names are are lower case
generics
ACE inhibitors (lisinopril, captopril, enalapril)
-pril
-sartan
Angiotensin Receptor Blockers (losartan, valsartan)
Beta-blockers (metoprolol, labetalol, esmolol, timolol)
-(o)lol
-zepam
Benzodiazepines (lorazepam/Ativan, diazepam/Valium)
Calcium channel blockers (amlodipine, nifedipine)
-dipine
-semide
Loop diuretics (furosemide/Lasix, torsemide)
Antivirals (acyclovir, oseltamivir)
-vir
BZD is
benzodiazepine
CTX is
ceftriaxone
acetaminophen, ibuprofen, fentanyl are By function
Analgesics
haloperidol classified by function is
Antipsychotics
DEA drug scheduling what type of classification is
By therapeutic usefulness versus addiction/abuse potentia
By pregnancy and lactation risk
is a classification of drugs?
Yes
Schedule I means
High abuse potential; no recognized medical purpose
Heroin, marijuana, LSD, peyote are what Drug Schedule
Schedule I
Schedule II means
High abuse potential; legitimate medical purpose
Examples of Schedule II drugs
Opioids: Codeine, fentanyl, hydrocodone, hydromorphone, morphine.
Stimulants: amphetamine (adderall), cocaine, methylphenidate (Ritalin)
Schedule III means
Lower potential for abuse then Schedule II meds
Examples of Schedule III drugs
Opioids: acetaminophen with codeine #3, Nonopioids: anabolic steroids, ketamine
Schedule IV means
Lower potential for abuse then Schedule III drugs.
Examples of Schedule IV drugs
Alprazolam (xanax), diazepam (Valium), lorazepam (Ativan)
Schedule V means
Lower potential for abuse than Schedule IV
Examples of Schedule V drugs
Opioid cough medicine
Pregnancy and Lactation Labeling Rule (2015). What applies only to presciption drugs
A Narrative description
Controlled substances require:
Additional security
* Additional record keeping
* Disposal precautions
* Strict regulations
* Regional variations
* Vary by EMS
If Every milliliter or milligram must be documented. What else has to
- Ordering
- Administration
- Disposal
If Controlled substances are targets of tampering or diversion. What do you have to do
- Inspect vials and ampules
- Suspect tampering if regular doses are ineffective
“The way in which a medication produces the intended response”
Mechanism of Action
How many classes IN TOTAL are in the Vaughan-Williams Classification (1970)
Class Ia, Class Ib, Class Ic, Class II, Class III, Class IV, Class V
Class Ia how does affect the action potential
Class Ia drugs prolong the action potential and has an intermediate effect on the 0 phase of depolarization
Vaughan-Williams Classification (1970). Fast sodium channel blockers
Class Ia and Class Ib
Class Ia drugs
Procainamide
* Quinidine
* Sparteine
Class Ia Indications
Treats ventricular tachycardias, WPW, atrial fibrillation
Class Ib how does affect the action potential
Shorten the action potential of myocardial cell and has a weak effect on the initiation of phase 0 of depolarization
Class Ib Indications
Treats ventricular tachycardias (during/after an MI)
Class Ib drugs
- Lidocaine
- Phenytoin
- Tocainide
Vaughan-Williams Classification (1970). Slow sodium channel blockers
Class Ic
Class Ic how does affect the action potential
do not affect action potential duration and have the strongest effect on the initiation phase 0 of depolarization
Class Ic Indications
treats recurrent tachyarrhythmias with abnormal conduction pathways (e.g., WPW)
prevents paroxysmal atrial fibrillation
Class Ic Contraindications
Contraindicated after MI,
Vaughan-Williams Classification (1970). Beta blockers
Class II
Class II how does affect the action potential
bind to B1 and B2 receptors to inhibit their effects
Class II Indications
Prevents reoccurrence of tachycardia, decreases blood pressure
Class II Drugs
Atenolol
* Metoprolol
* Esmolol
* Propranolol
* Carvedilol
Class Ic Drugs
- Flecainide
- Encainide
- Moricizine
Vaughan-Williams Classification (1970). Potassium channel blockers
Class III
Class III how does affect the action potential
interferes with conduction through potassium channels (blocking them), prolonging repolarization (phase 3)
Class III Indications
Treats atrial flutter/fibrillation, ventricular tachycardia, WPW
Class III drugs
- Amiodarone
- Dronedarone
- Dofetilide
Vaughan-Williams Classification (1970). Calcium channel blockers
Class IV
Class IV how does affect the action potential
drugs inhibit the influx of calcium into cardiac and smooth muscle cells, resulting in vasodilation, decreased inotropy, chronotropy, and dromotropy
Class IV Indications
Treats heart failure, atrial flutter/fibrillation, supraventricular tachycardia
Class IV Drugs
- Diltiazem
- Verapamil
Miscellaneous category that includes drugs that do not fit into the traditional Vaughan-Williams classification system for antiarrhythmic medications
Class V
Adenosine MOA :
activates adenosine receptors that cause hyperpolarization of the cell membrane, increasing K efflux and decreasing Ca++ influx, leading to blockade of AV node conduction
Magnesium Sulfate MOA
stabilizing cell membranes, inhibits Ca++ channels and alters Na+ and K+ currents (exact mechanism not understood)
Digoxin MOA:
inbibits Na-K-ATPase pump, leading to increase in intracellular Ca++; enhances contractility and increases vagal tone, which slows conduction through AV node
Basic Concepts. Reasons to give a medication. May be more than one
Indications
Basic Concepts. reasons to not give a medication
Contraindications
amount of medication given, not volume of fluid given
Dose
amount of liquid, not the amount of medication
Volume
amount of medication per volume
Concentration
Various ways medications are supplied. tablets, capsules, powders are
Solid
Various ways medications are supplied. solutions, suspensions, emulsions, syrups, etc are
Liquid
Medication Routes must allow delivery of:
- Delivery of appropriate amount
- Delivery to correct location
Medication Routes. Determined by:
- Physical and chemical properties
- Routes of administration available
- How quickly effects are needed
percentage of unchanged medication that reaches systemic circulation is
Bioavailability:
Medication Routes:
Oral (PO)
Orogastric/nasogastric (OG/NG)
Buccal
Sublingual (SL)
Rectal (PR)
are:
Enteral
Medication Routes. administration anywhere but the digestive track
Parenteral
Medication Routes. Administers at least 2 to 2.5 times the IV dose
Endotracheal Tube
Medication Routes. Bioavailability close to 100%. Rapid absorption
Intranasal (IN)
Medication Routes. Bioavailability = 100%. Onset of action faster than other routes (e.g., IM, IN, oral, etc.)
Intravenous
Infiltration risk is high with what
Sympathomimetics and electrolyte solutions
Medication Routes. Viable alternative when IV access is unattainable
Intraosseous
IO Sites
proximal tibia, distal femur, proximal humerus, distal tibia
Medication Routes. Bioavailability from 75% to 100%, confirm appropiate for this route
Intramuscular (IM)
Medication Routes. Slower absorption
* May prevent adverse cardiovascular effects
Subcutaneous (SC)
Medication Routes. Deliver constant dose of mediation during a long period
* Large quantity of medication
Dermal and Transdermal
Medication Routes. Bioavailability low
Large doses required
Patients must be
Conscious
Alert
Sublingual (SL)
Medication Routes. Preferred over oral route if patient is unresponsive, having seizures, vomiting, unable to swallow
Greater than 90% bioavailability
Unpredictable absorption
Rectal
Mention the processes of how the BODY interacts with the DRUG
Absorption
Distribution
Metabolism (Biotransformation)
Elimination
This process begins from the entrance point to circulation. It is how fast it will get to circulation.
Absorption
On what Absorption relys on
- Medication properties
- Route of administration
- Surface area for absorption
- Concentration
- Age (possible slower oral absorption in children and elderly)
Is the process of distribution of a drug from the sistemic circulation to organs/tissues.
Distribution
What Distribution relys on
Volume of distribution
Methods of distribution
Size of molecule
Charge of molecule, pH
Protein Binding therefore lowers the effect but they will be release little by little
barries that “don´t distribute” drug easly
Blood-brain barrier BBB
Placental Barrier
This barrier has tight junctions and is permeable to lipid-soluble substance
Blood-brain barrier BBB
This process is how the drug is transformed in the body
Metabolism
Where does the Metabolism of drugs occur
Typically occurs in the liver
Drugs are made ___________ to aid in excretion and elimination
more water-soluble
4 ways the drug will be metabolized to
Inactive to active
Active to active metabolite
Active to Partial active
Active to ease to eñiminate
Process of how to drug gets out of the body that occur mostly via the kidneys/urine
Elimination
Pharmacokinetics. time needed in an average person for the metabolism and elimination of 50% of the medication in the plasma
Half-life
What is First Order Elimination
Constant fraction of drug eliminated per unit time
In first order, rate of drug elimination is ___________ to drug plasma concentration
proportional
What is Zero Order Elimination
Constant amount of drug eliminated per unit time
In zero order, rate of drug elimination is ___________ to drug plasma concentration
independent
Drugs stimulate or inhibit a cell’s normal biochemical actions. Part of what is this definition:
Pharmacodynamics
Mention how the DRUG interacts with the BODY
- Binding to receptors (most common mechanism)
- Alter normal metabolic pathways
- Change physical properties of cells
- Combine with other chemicals
Binding to Receptors. causes or enhances the intended receptor effect when bound
Agonist
Binding to Receptors. reduces or performs the opposite of the intended receptor
effect when bound
Antagonist
Competitive, Non-competitive
are what type of receptors
Antagonist
– the force of attraction between a drug and the receptor
Affinity
Potency
– amount of drug needed to initiate cellular response
Efficacy
a drug’s ability to cause an expected result
The peripheral nervous system is divided into afferent and efferent divisions.
The section of the ________ division that controls involuntary bodily functions is known as ____________
EFFERENT, the autonomic nervous system
Time from drug administration until reaching minimum effective concentration
Onset of action
Duration of action
• Length of time the drug remains effective
Termination of action
• Level of drug drops below minimum effective concentration
• A drug’s margin of safety (i.e., how close effective and dangerous doses are)
Therapeutic index
Components of Therapeutic Index
Median lethal dose (LD50)
• Median toxic dose (TD50)
• Median effective dose
Relationship between median effective dose and median lethal dose
• Large difference:
medication is safe
Relationship between median effective dose and median lethal dose
• Small difference:
patient needs to be monitored
Medication Responses – Desired “Therapeutic”
Effect
Amount of drug that is administered that will achieve the intended
effect or response
• Cumulative action
ANTICIPATED, unintended effect of a medication
• Generally “expected” effects
• We know about them!
• Generally mild
• Sometimes good or bad
• Does not interfere with treatment
Side Effect
Adverse Effect means
UNANTICIPATED, unintended effect
of a medication
• General “unexpected” effects
• We don’t know about them!
• Undesirable effect caused by a
medication
• May be severe or life-threatening
• Sometimes called untoward effects
Synergism –occurs
Synergism –occurs when two or more drugs work together to produce
an effect that is greater than the sum of their individual effects
Potentiation – occurs
when one drug, which may have little to no effect on its own, enhances the effect of another drug
“1 + 1= 3”
Synergism
“0.5 + 1= 1^0.5”
Potentiation
prolonged habituation – physical, emotional, behavioral need for a drug to maintain “normal” function
Dependence –
– abnormal tolerance to adverse or therapeutic effects associated with a drug
Habituation
– repeat exposure to a medication within the same class
• Opioids, benzodiazepines
Cross-tolerance
– decreased efficacy or potency after repeated use
Tolerance
