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145 Cards in this Set

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What was the benefit of Pure food and Drug Act? When was it established?
1906- Had to prove the ingredients, strength, purity, and quality of pharmaceuticals.
What was the Shirley Amendment?
In 1912, had to prove therapeutic benefit - no more false claims!
When was the Federal Food, Drug, and Cosmetic Act established? What was its significance?
1938- it established the FDA, and said that drugs had to be approved by this board to be true to it's therapeutic claim, ingredients, and no lethal side effects
This amendment promised better safety regulation of medications and had to prove safety to be approved by the FDA.
1962- Kefauver-Harris amendment
What was the significance of the Comprehensive Drug Abuse Prevention and Control Act?
1970- controlled dispensing of controlled drugs to prevent abuse and determined Rx vs OTC.
What was the Food and Drug Administration Modernization Act?
1997- make it easier for generic drugs to be made without requiring repeat trials as long as they had the same ingredients.
Describe the 5 schedules of drugs.
C1- no medical use, highest potential for abuse (Heroin)
C2 - accepted use, high risk of abuse (percocet)
C3 - accepted use, less potential for abuse
C4 - accepted use, low potential for abuse
C5 - accepted use, lowest potential for abuse
What are the phases of Drug Development?
1- small number of healthy people (safety)
2 - more people who have target disease (efficacy)
3 - 100s of people, several years
4 - goes to market (we are involved) - post marketin surveilance
What role do providers play during phase 4 of a medication development?
Adverse drug event reporting
What are black box warnings?
Warnings that appear on prescription drugs informing patients of potentially serious side effects.
1 inch = ____ cm
2.54cm
1 tsp = ___ mL
5mL
1kg = ___ lb
2.2 LBs
What is the median effective dose?
the amount that produces the intensity of effect in 50% of individuals
The term "%" represents what?
The rate per 100.
a) %w/v = ___
b) %v/v = ___
c) %w/w = ___
a) grams/100mL
b)mL/100mL
c) grams/100g
1:1000 is equivalent to what?
1gram/ 1000mL solution
1mg/mL
What is the formula to calculate IBW:
Males: 50kg + 2.3*(#in>60)
Females: 45.5 + 2.3*(#in>60)
What is the formula to calculate Adjusted BW?
IBW+ 0.4(ActBW-IBW)
What is the formula for Creatinine clearance?
CrCl= [(140-age)xIBW]/(scr x 72)

*multiply entire thing by 0.85 for females
*if actual <IBW, use actual
*if >65 use Scr=1 or if Scr>1 use bigger number
decreased creatinine clearance indicates what?
Kidneys aren't properly filtering out creatinine
List the 10 "rights" to writing a prescription.
D- drug
R- route
P- patient
A- amount/ dose
T- time/ schedule
D- date
R- refills
R- right to refuse
I- informed consent
D- duration
When should you include a zero with a decimal?
always LEAD and never TRAIL
0.1 and 1

NOT .2 or 2.0
How should you abbreviate "units" and "micrograms"...
you shouldn't. write them out to avoid errors
1) bid means ___
2) tid means ___
3) qid means ___
1. 2x a day
2. 3x a day
3. 4x a day
How would you abbreviate "before meals"?
ac
How would you abbreviate "after meals"?
pc
What is the difference between a prescription and physician's orders?
Orders include medications AND everything else (labs, therapy, etc)
What is the difference between orders and progress notes?
Progress notes (SOAP) describe rationale for orders.
What is a ligand?
the molecule that binds to a receptor (include drugs as well as things like hormones and neurotransmitters)
Ligands may have what actions on a receptor?
Activate or inactivate
Activation of a receptor by a ligand may have what two responses?
Increase or decrease a particular cell function
What is an "agonist"?
a drug that causes the receptor to respond the same way as the naturally occuring substance it mimicks
What is an "Antagonist"?
A drug that binds to a receptor but doesn't produce the response.

(prevents binding of endogenous hormone or neurotransmitter)
What is the difference between a full and partial agonist?
Full agonist = activates receptor with maximal efficacy

Partial agonist = activates the receptor but not with maximal efficacy
What is the difference between a competitive and non-competitive antagonist?
Competitive: binds reversibly to activate the site of the receptor, blocks agonist from binding, but can be overcome by increasing the agonist concentration.

Noncompetitive - irreversible binding or binding to another site that prevents the binding of the activator
What are spare receptors?
In some systems, there are more receptors available than needed to elicit a full response.
In what 5 ways are receptors mediated?
1. desensitization - rapid due to change in receptor conformation (

2. Reduction of receptor number-

3. reduction of receptor-coupled signaling - signaling molecules get depleted

4. Increased metabolic degradation - metabolism increases or eliminates drug faster

5. Tolerance - drug effects reduce due to opposing homeostasis
The ___ is the dose of drug required to produce a given effect.
Potentcy
___ is the probability of drug occupying a receptor at any given instance.
Affinity
What is the "efficacy" of a drug?
The magnitude of effect that can be produced by a drug
____ and -____ are determined by receptor's chemical structure.
Affinity and efficacy
what is pharmacodynamics?
the study of the biochemcial and physiological effects of drugs on the body and their mechanism of action
what is the therapeutic window?
the range of doses of a drug tht elicits a therapeutic response without toxicity
the ratio that describes the dose that produces toxicity to that that produces desired outcome: Td50/ed50
Therapeutic window
___ is the way the body handles the drug and what the body does to the drug.
Pharmacokinetics
What are the 4 stages of pharmacokinetics?
1. absorption
2. distribution
3. metabolism
4. elimination
what are advantages or disadvantages of PO administration?
+: safe, easy, inexpensive
-: irregular absorption, 1st pass in liver, GI upset, pt compliance
What are advantages or disadvantages of SL administration?
+: rapid, no 1st pass in liver, bypasses GI
-: poor penetration of mucosa by many drugs
What are advantages or disadvantages of rectal administration?
+: can be given in unconcsous or vomiting, minimal 1st pass, bypasses GI
-: irregular and incomplete absorption
Advantages or disadvantages of IV administration:
+: rapid, predictable
-: greatest risk of infection, anaphylaxis, embolus, no access
Advantages or disadvantages of IM administration:
+: moderate volumes, faster than SQ
-: can't be used for irritating substances
Advantages or disadvantages of SQ administration?
+: slower absorption, pt can self administer
-: slower than IM, doesn't work in vasoconstriction, can be painful
Advantages or disadvantages of Intraperitoneal administration?
+: large absorbing surface
-: 1st pass effect, risk of adhesion
Advantages or disadvantages of topical administration?
+: local effects
-: local skin irritation
Advantages or disadvantages or inhaled administration?
+: very rapid, useful for gassses, vapors, aerosols
-: difficult to control dose
__ is the study of the role of inheritance in variation of drug response.
pharmacogenomics
___ is responsible for the hydrolysis of Succinylcholine
BChE- pts with variations have decreased metabolism and result in prolonged paraysis
NAT2 catalyzes the acetylation of ___ resulting in __
Isoniazid, hydralazine, procainamide

either slow or fast acytylators
Someone who acetylates slowly may have ___
drug toxicity
___ metabolizes tons of medications like metoprolol, haloperidol, codeine, and fluoxetine.
CYP2D6
Poor metabolizers are at risk for ____ whereas ultra rapid metabolizers are at risk for ___
1. overdose/ toxicity
2. under-dosing
Describe why poor CYP2D6 metabolizers have a different response to codeine/
this gene activates codeine into morphine... so unlike the other drugs, slow metabolizers don't get the active drug andneed more, whereas fast metabolizers risk toxicity
___ is metabolized predominately by CYP2C9, and targets vitamin K epoxide reductase.
Warfarin.
What is an idiosyncratic reaction?
A reaction resulting from interaction between the medication and a unique aspect of the patient's physiology.
TPMT catalyzes __
Thiopurine drugs such as 6-mercaptopurine and azathiprine (immunosuppresants)
TPMT*3A results in ___
decrease in tissue TPMPT resulting in myelosuppression if treated with nomral doses of thiopurines
The ALOX5 gene may have alterations that are the target for which drug?
Zileuton (inhibits enzyme that causes airway inflammation) - asthma
Aminoglycocides are ____ that must be given ____. They are water soluble and do not distribute into adipose. What adjustment should be made when prescribing these?
antibiotics

parenteraly

Dosing should be done with IBW or ABW for most patients
Describe the clearance mechanism for aminoglycocides?
- almost entirely renal

- within 2-3 hours in nml renal funciton, 30-60h in a dialysis pt
Gentamycin and Tobramycin are ____ antibiotics. What is their dose?
Aminoglycosides

5-7mg/kg/day either once daily or divided q8 hours
When should aminoglycoside levels be checked?
if given q8- 1 hour after end of infusion and 30 minutes prior to next

if given high dose: two levels at a peak, a second 2-4 half lives later
Vancomycin is usually given ___ except in c.diff. when it is effective ___
parenterally

PO
What is the usual half life of vancomycin?
5-10 hours,
What is the usual dosing of vancomycin?
q8 or q12, increases with renal problems
How is vancomycin cleared?
Renally - approximates creatinine clearance
Vancomycin is used to treat ___, and toxicity results in ___
gram pos bacteria

ototoxicity (deafness
Carbamazepine is used to treat ___ and is usually cleared by ___.
convulsions

metabolic - one metabolitye also has anticonvulsant activity
Carbamazepine is metabolized by ___
CYP3A4
Carbamazepine has many drug interactions and ____
autoinduction
Concomitant treatment of ___ with valproate sodium results in ___
carbamazepine

higher free fraction of carbamazeine
Why is fospheytoin preferred over phenytoin?
phenytoin has propylene glycol and can cause cardiac depression
What is the dose for phenytoin?
200-400mg/day, may use loading dose of 15mg/kg oral or IV
What is the max recommended rate of IV admin of phenytoin and fosphenytoin?
Phenytoin: 50mg/min

Fosphenytoin: 150mg/min
When is phenytoin monitored?
- prior to steady state (steady state takes too long) to ensure avoidance of sustained peaks or troughs
- acute setting: 2-3 days after initiation and then 3-5 days after that
- long term: 3-12 months
___ is the fraction of administered drug that reaches the systemic circulation following administration by any route
Bioavailability
What percent of a drug is bioavailable after IV administration?
100%
During _____ the drug leaves the blood stream and enters the interstitial or cellular fluids.
Drug distribution
Drug distribution is dependent on what?
blood flow,
capillary permeability
drug structure (hydrophobic/ hydrophilic)
The concentration of the drug in the ___ is used to define and monitor therapeutic drug levels
Plasma
The ____ describes the extent to which a drug partitions between the plasma and tissue compartments.
Volume of distribution (Dose/[drug in plasma]
Drugs with large volumes of distribution may require _____ initial doses. (why?)
Higher initial doses because it gets into tissues so fast you need more to establish a therapeutic plasma concentration.
Drugs bound to a protein are (active/inactive)
Inactive - only free, unbound drug can act on a target site and elicit response
The blood-brain barrier is permeable to ___ soluble substances, but not ___.
allows lipid-soluble drugs very rapidly, but not water soluble... (water soluble drugs may be used when you want to exclude the brain in target action)
what type of drugs move easily through the placenta?
Lipid-soluble (water soluble move slowly
What is the fastest equilibrium possible between mother and fetus?
40 mins
___ refers to the removal of a drug from the body without any chemical changes being involved.
Elimination
___ refers to the disappearance of a drug when it is changed chemically into another compound.
Metabolism (biotransformation)
What is a prodrug?
A drug that is administered in an inactive state to promote absorption and is then metabolized into its active form (codeine)
P450 enzymes are metabolized mostly in the ___
Liver
The P450 primarily involves which families?
CYP1, CYP2, and CYP3
Metabolism is primarily ______
P450-dependent oxidation
A non P450 pathway is _____ which oxidizes amino-containing compounds like ____ and ___
monoamine oxidase,

catecholamines and tyramine
Almost all conjugated products are (active/inactive).
inactive
What is the primary mechanism of P450?
induce the expression of enzymes through increased transcription
What are the two types of inhibiition?
Competetive - binds to active site so P450 can't
Irreversible - permanently deactivates P450
Which drugs inhibit P450?
cimetidine, cipro, erythromycin, ketoconazole, OCPs, quinidine, ETOH
Which drugs induce p450?
barbiturates, phenytoin, steroids, isoniazid, rifampin, ETOH
How can ETOH both inhibit and induce P450?
It binds competetively to reduce P450 active sites, but when it does, it also induces
During renal elimination of a drug, non-protein bound drug will be freely filtered during ___
glomerular filtration
Proximal tubular secretion is an _____ process while distal tubular reabsorption occurs ____
secretion = active pumping out

reabsorption = passive diffusion
Drugs that are simply filtered will be cleared at a rate ___ _than GFR or CrCl.
Similar
Drugs that are filtered and reabsorbed will be cleared at a rate ___ than GFR.
Lower
Drugs that are filtered and actively secreted are cleared at a rate ___ than GFR
higher
In addition to renal elimination, what are 4 other possible routes of elimination?
1. biliary secretion and enterohepatic cycling
2. exhalation
3. sweat
4. secretion in breast milk
What is half life?
The time that it takes for a plasma concentration of a drug to be reduced by 50%
What is the pharmacokinetic parameter that most significantly limits the time course of action at a target?
Clearance of a drug
(Cl renal + hepatic +other)
How many half-lifes until most drugs are considered to be at a "steady state"?
5
In 1st order metabolism, the rate is ___
proportional to the concentration of free drug (LINEAR)
Most P450 drugs are what order metabolism?
1st order
What occurs with zero-order metabolism?
it is non-linear and unpredictable... may be due to saturation, or may start that way
Pharmacokinetic (drug-drug) interactions may occur during what 4 processes?
1. absorption
2. distribution
3. metabolism
4. elimination
The greater the ___ of an inhibiting drug, the more it blocks binding of the other drug.
affinity
Why should you be careful with drinking grapefruit juice and medications?
deactivates the enzyme for metabolism of many medications (3A4)
Vitamin K -____ the effect of warfarin.
decreases
Cheese, wine, cocoa, coffee, and cola all contain ____, which can result in a HTN effect rxn in pts on _____
1. Tyramine
2. MAOIs
Which 4 things can cause interactions with drugs?
1. other drugs
2. foods
3. disease processes
4. Various patient factors
What patient factors may influence drug interactions?
heredity
disease
environment
smoking
diet/nutrition
ETOH
Gender
Age
A premie is ___ (ages)
A neonate is ___
An infant is __
A child is ___
An adolescent is ___
1. <36wks gestation
2. <30 days old
3. 1mo - 1 yr
4. 1-12 yrs
5. 12-18 yrs
What is important to remember about oral absorption in young children?
1. gastric pH alkaline < age 2
2. neonates have irregular and often enhanced absorption
3. intestinal flora depends on diet - breastfed develops flora sooner
What is important regarding rectal administration in kids?
1. Hemorrhoidal veins not part of portal system and avoid 1st pass metabolism
2. erratic absorption
What are possible problems with IM or SQ absorption in children?
Lack of blood flow to undeveloped muscle, highly variable among different children
What 6 factors of distribution differ significantly in the pediatric population?
1. vascular perfusion
2. body composition (more body water and less fat as neonates)
3. Tissue binding characteristics
4. physiochemical properties (more fat, so lipid soluble has increased risk for toxicity)
5. plasma protein binding is lower
6. Route of administration
What is Gray Baby Syndrome?
Babies with deficiency in glucoronidation enzymes that are given an antimicrobial medication (chlorampenicol) have poor feeding, decreased breathing, CV collapse, cyanosis, or death
At what age does GFR appraoch nomral adult levels?
2 years
At what age does tubular secreation or reabsorption in the kidneys reach adult values?
5-7 mos
Elimination in pediatrics has changes that ultimately result in ___ half-lives
longer
IM injections in pediatrics are limited to ___mL
2
Pharmacokinetic changes in the elderly include what 10 main things?
1. unchanged passive diffusion (same bioavailability)
2. Decreased first pass effect (increased bioavailability of some)
3. reduced gastric acids
4. delayed gastric emptying
5. Decreased esophageal motility
6. decreased blood flow
7. loss of SQ fat
8. increased fragility of veins
9. Drug interactions due to metabolism issues
10. Drugs affect GI motility and constipation can affect absoprtion
In what condition would serum albumin levels be altered among elderly pts?
Chronic disease or severe malnutrition
What age-related changes in the kidney ultimately lower the GFR?
- smaller kidney size
-decreased renal blood flow
- decreased functioning nephrons
- decreased renal tubular secretion
After age 40, GFR decreases ___ to ___% every 10 years.
6-10%
In elderly, Serum creatinine _____ reflect creatinine clearance?
does not
What factors result in increased drug-receptor interactions in the elderly?
1. increased sensitivity of the receptor
2. decreased capacity to respond to the drug induced receptor
3. reduced number and affinity of receptors
What factors are important for safe prescribing in the elderly?
1. explore alternatives to medication
2. choose drugs efficiently
3. simplify the regimen
4. educate patients and caregivers
5. review medications
6. therapeutic monitoring