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Pharmacology > Additional Exam 1 Information > Flashcards

Additional Exam 1 Information Flashcards

1
Q

Clinically relevant inducers

A
  1. Phenobarbital
  2. Phenytoin
  3. Carbamazepine
  4. Rifampin
  5. Ethanol*
  6. St. John’s Wort*
  7. Tobacco smoke (NOT nicotine)*

*don’t need RX

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2
Q

PK toxicokinetic strategies for poisoning

A
  1. Absorption: prevent or decrease absorption of toxin :(decrease rate in)
  2. inhibition of toxication (Prevent conversion to toxic species)
  3. Metabolism: enhance metabolism (detoxication)
  4. Elimination: increase elimination of toxin (increase rate out)
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3
Q

what is an ANDA (abbreviated new drug application) used for?

A

submitted for generic drugs allowing the manufacturer to bypass the expensive and time-consuming clinical trials for an already approved drug.
-only BIOEQUIVALENCE standards must be met

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4
Q

what patient info is required on a prescrption

A

name and address

*age and weight are not legal requirements but helpful in monitoring prescribed dose, esp. in peds

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5
Q

how do local anesthetics get metabolized?

A

hydrolysis by amides

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6
Q

Factors involved in GI absorption interactions

A
  1. disintegrating time
  2. dissolution rate
  3. gastric emptying
  4. absorptive SA
  5. intestinal transient time
  6. pH of lumen fluid
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7
Q

describe Schedule I drugs

A

High abuse potential, no currently accepted medical use, NOT prescribed

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8
Q

Information NOT required in dietary supplement lable

A

-Identification of active principle – not known for many
herbs
-Pharmacokinetic/F data
-Potential interactions with Rx and OTC drugs

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9
Q

What drugs do not have half lives?

A

drugs eliminated by zero order kinetics

-bc elimination rate is independent of the amount of drug in the body

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10
Q

pharmacodynamic interventions for poisoning include ___.

examples discussed include

A

antidotes

ex. acetaminophen–> N-acetylcysteine
methanol/ethylene gylcol–> Ethanol, fomepizole (Antizol)

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11
Q

Post 1994,___ must provide “reasonable”
evidence that the dietary supplement product is safe for human use
-do not have to provide the FDA with evidence that the
product is ___ and ____
-HOWEVER, burden of proof on ____ to show product is
not ___ before use restricted or removed from market

A

manufacturers

safe and effective

FDA

not safe

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12
Q

What CYP isozyme results in:

Codeine intoxication

A

CYP2D6 (UM)

  • due to rapid metabolism to morphine
  • metabolism is activiating
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13
Q

What Schedule of drugs are these?
-Opioids*: Morphine, codeine, OXYCODONE, hydromorphone, HYDROCODONE

  • Stimulants: Methamphetamine, amphetamine, cocaine, methylphenidate
  • Depressants*: BARBITURATES (pentobarbital, secobarbital)
A

Schedule II

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14
Q

How can absorption mechanisms be altered by D-D interactinons?

A
  1. decreased motility = decreased absorption = decreased Cp (**no change in F)
  2. change in pH or formation of insoluble complex= decreased absorption = decreased Cp (**F is changed bc it leads to physiochemical inactivation)
    ex. Tetracycline + antacid milk= decreased absorption= decreased Cp= unresolved infection

*increasing rate of absorption in LESS clinically important

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15
Q

how can you reduce absorption of a drug given by IV that resulted in poisoning?

A
  • activated charcoal
  • back-diffusion of drug from blood w/ ion-trapping in stomach (reduces elimination half-life)
  • best to given 10:1 ratio to toxin

-best to also give osmotic cathartics (ie. sorbitol 70%) to prevent “briquet” formation

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16
Q

how can you manipulates a drugs affinity for a specific receptor? Give an example.

A

change its shape, size or electrical charge

ex. Dobutamine will interact w/ B1-adrenergic receptor on the heart, but no effect on acetylcholine or adenosine receptors at therapeutic levels
- Dobutamine is an agonist of NE

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17
Q

Examples of drugs whose metabolism of active drug results in MORE ACTIVE compound

A

Codeine–> morphine

hydrocodone–> hydromorphone

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18
Q

how can you assess the Benefit-risk ratio for doses of drugs with a quantal dose-response curve?

A
  1. Therapeutic Index: compares MIDPOINTS in the population (ED50 and LD50)
  2. Standard Safety Margin: compares EXTREMES in the population (ED99 and LD1)
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19
Q

____ largely determines the dose necessary to administer to the pateint

A

potency (expressed in dosage units for a particular therapeutic end point ex. 20mg of lisinopril will lower BC by 10-15mg)

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20
Q

what is the difference between a graded dose-response curve and a quantal dose-response curve?

A

Graded: graded response from a number of increasing doses in an INDIVIDUAL (used to determine Emax)

Quantal: all or nothing response to a single dose— in a POPULATION (NOT used to determine Emax)

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21
Q

how can you reduce absorption in poisoning

A
  1. emesis (Ipecac)
  2. gastric lavage
  3. activated charcoal
  4. Osmotic catharitcs
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22
Q

generic drugs and brand drugs have the same:

A
  • active ingredient
  • same dosage, intended use, therapeutic effects, side effects, route of administration, risks, safety, and efficacy as the original drug
  • mean bioavailability variation is less than 4%

*pharmacological effects are EXACTLY the same

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23
Q

how can drug-drug interactions affect metabolism

A

**most clinically important

  1. inducers= increased metabolism= decreased Cp= subtherapeutic levels
  2. inhibitors= decreased metabolism= increased Cp= toxic levels

*most interactions occur via effects on CYP450 system

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24
Q

tx of acetaminophen toxicity

A
  • activated charcoal and gastric lavage (best w/in 4 hrs)
  • supportive care
  • N-acetylcysteine: best w/in 12-36 hrs of ingestion (ENCHANCE DETOXIFICATION)
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25
Q

What Schedule of drugs are these?

Opioids: buprenorphine, diphenoxylate-antidiarrheal, codeine-antitussive (in low amounts)

A

Schedule V

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26
Q

considerations for classification of a drug in OTC include:

A
  1. condition is self-diagnosable and self-treatable
  2. whats the products toxicity? habit forming? high dose safety profile?
  3. do benefits of OTC outweigh risks
  4. methods of use preclude OTC availability
  5. directions for safe use- understood by ordinary person
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27
Q

what does ED50 mean for a QUANTAL dose-response curve vs a GRADED dose-response curve

A

Quantal: ED50= dose that initiates therapeutic effect in 50% of test population

Graded: ED50= dose that produces 50% of the maximal response possible for an individual test subject

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28
Q

most drugs display what order kinetics?

A

1st order kinetics

-Rate of elimination is proportional to the concentration of the drug in the plasma

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29
Q

describe the relationship between drug potency and EC50

A

higher potency = lower EC50 and vise versa

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30
Q

Draw the Phase I and Phase II comparison chart

A
  • reference notes

- categories include: Rxn type, enzymes, genetic polymorphism, induce-inhibit, dev. patterns, age changes, saturability

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31
Q

Contraindications of Emetic agents

A
  1. pt is comatose/stuporous (lack of gag reflex–> risk of aspiration)
  2. ingestion of corrosive poisons (strong acids or alkalis)
  3. ingestion of CNS stimulant such as strychnine (risk of seizure)
  4. ingestion of petroleum distillate (risk of pneumonitis)
  5. Pregnancy category C (weight risk vs benefit)
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32
Q

When can clinical trials in humans be performed and how long do they take and how much does it typically cost

A
  • After IND approval
  • takes 2-10 yrs
  • Costs $100-200 million
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33
Q

what 2 drug categories is it advised to use one formulation (brand or generic) consistently?

A
  • *1. Narrow TI: Levothyroxine and anti-epileptic drugs

2. Non-linear (zero order) pharmacokinetics (ex. phenytoin)

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34
Q

5-10% of Caucasians have what CYP isoform?

20% of Asains have have CYP isoform?

A

C: CYP2D6- PM

A: CYP2C19- PM

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35
Q

What is Class X drugs for pregnancy?

examples?

A
  • Contraindicated in pregnancy
  • Risks involved in the use of the drug in a pregnant women clearly outweigh any potential benefits

examples: statins (HMG CoA reductase inhibitor), accutane (isotretinoin)

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36
Q

hepatic metabolism and renal excretion exhibit what order kinetics?

A

1st order kinetics

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37
Q

how does protein-binding and displacement w/ drug-drug interactions effect distribution?
When is this of clinical consequence?

A

displacement of 1st drug from protein by 2nd drug= increased levels of unbound first drug

Of clinical consequence when:

  1. first drug has narrow TI
  2. Vd of 1st drug is small
  3. 2nd drug is started in high doses
  4. Drug response is more rapid than drug distribution
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38
Q

Describe Schedule III drugs

A

Accepted medical use, MODERATE abuse potential and dependence liability

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39
Q

parameters for absorption

A
  1. F

2. rate (estimated by Tmax and Cmax)

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40
Q

what mechanisms can lead to decreased Cp leading to sub-therapeutic levels

A
  • increased drug elimination (most common)

- decreased drug absorption

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41
Q

What is Class C drugs for pregnancy?

examples?

A
  • Risk cannot be ruled out
  • Potential benefits may warrant use of drug in pregnant woman despite potential risks

examples: pseudoephedrine, antidepressants, emetic agents

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42
Q

what phase II enzyme is inducible?

A

glucuronyl transferases – but not to the extent of CYP450

*induced by N-acetylcysteine

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43
Q

Describe Schedule II drugs

A

Accepted medical use, HIGH abuse potential with severe dependence liability

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44
Q

What is Class B drugs for pregnancy?

examples?

A
  • No evidence of risk in humans

examples: opioids (D near term) ondanstetron, acetaminophen, thiazide diuretics

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45
Q

Describe Phase III testing in human trails

A

Phase III: Full scale Clinical trail: Does it work, double blind?

  • 3 yrs
  • 1000-6000 pts (similar to those anticipated for ultimate drug use)
  • Efficacy measured against established therapy
  • Monitor for ADR from chronic use
  • Sometimes omitted for drugs used in serious, life-threatening illnesses (AIDs, CA)–> drugs w/ greatest potential benefit may obtain an accelerated or conditional approval that then requires more definitive clinical trials to be conducted after initial approval
  • Positive results may result in approval of NDA, which is then submitted to FDA
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46
Q

how does a therapeutic index number relate to the saftyness of a drug.
-Most drugs in clinical use have a therapeutic index of

A

higher TI value= safer the drug

-Greater than 10-20

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47
Q

what type of drugs are typically considered to have a “narrow therapeutic index”

A

drugs with less than a 2-4 fold difference in therapeutic vs toxic Cp levels

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48
Q

Potency depends on:

A
  1. affinity that receptor has for that drug

2. efficiency of receptor to generate a response (intrinsic)

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49
Q

when can spare receptors be found?

A
  1. duration of effector is greater than that of the DR interaction
  2. the actual number of receptors exceeds the number of available effector molecules (R increase sensitivity to the agonist as the likelihood of DR interaction increases in proportion to the number of receptors available)
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50
Q

information required on dietary supplement label

A
  1. Name of product - if herb, name of plant-plant part used
  2. Net quantity of contents
  3.   Manufacturer information
  4.   Directions for use

*need to include for medical FOODS too

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51
Q

what phase II enzyme helps with the metabolism of acetaminophen?

A

glutathione-s-transferase (GST)

**glutathione conjugation is extremely important in the detoxification of carcinogens, pollutants and toxic metabolites

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52
Q

What Phase I oxidation reactions are CYP450 dependent?

A
  1. aromatic hydroxylation
  2. aliphatic hydroxylation
  3. epoxidation
  4. Oxidative dealkylation
  5. deamination
  6. desulfuration
  7. dechlorination)
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53
Q

what is the most frequent pathway of drug metabolism

A

oxidation (phase I)

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54
Q

When does zero order kinetics occur? Give examples of drugs this is seen with

A

Occurs due to saturation of hepatic metabolic enzyme systems by drug administration (unlikely w/ renal excretion processes)

ex. ASA, phenytoin, ethanol and with toxic doses for many hepatically eliminated drugs

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55
Q

what does the federal government control in regards to drug regulation?

A

-controls WHAT drugs may be prescribed or sold directly OTC via FDA

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56
Q

The clinical effectiveness of the drug depends on the drug’s _____

A

maximal efficacy

*more important to prescribers than potency

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57
Q

What is the schedule for these types of codeine?

  • Codeine combined w/ non-opioids
  • codeine-antitussive
  • Codeine
  • Hydrocodone
  • Oxycodone +/ non-opioid
A
  • Codeine combined w/ non-opioids= schedule III
  • codeine-antitussive= schedule V
  • Codeine- schedule II
  • Hydrocodone- schedule II
  • Oxycodone +/ non-opioid= schedule II
  • opiod analgesic drugs (fentanyl, morphine, codeine,, Oxycodone +/ non-opioid, hydrocodone +/- non-opioid, methadone) = schedule II
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58
Q

Types of osmotic cathartics and when you would use them

A
  1. Sorbitol 70%- recommended– use w/ charcoal
  2. Magnesium citrate or sulfate: avoid in renal disease or poisonings w/ nephrotoxic agents
  3. sodium sulfate: avoid in CHF or HTN (systemic Na absorption –> fluid overload/edema)
  4. Polyethylene Glycol: use for poisonings w/ sustained-released drugs, metal ions, drug packets
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59
Q

what are extension effects? Give examples

A
  • arise from an extension of therapeutic effects
  • dose-related
  • predictable

ex. insulin lowers BG causing hypoglycemia
heparin tx clots causing bleeding

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60
Q

What does changes in hepatic blood flow affect hepatic clearance?

A

only when the drug has a high extraction rate (metabolism is very efficient)

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61
Q

what drugs tend to accumulate in breast milk?

A

basic compounds (opioid analgesics) by ion trapping bc breast milk is more acidic than plasma (pH 6.5 vs 7.4)

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62
Q 
Convert metric to avoidrupois/ apotheracry/household: VOLUME
0.05ml=
5ml= 
15ml= 
29.56-30 ml=
946 ml=
473ml=
3785ml (3.785L)=
A 
0.05ml= 1 drop
5ml= 1 teaspoon
15ml= 1 tablespoon
29.56-30 ml= 1 fluid oz
946 ml=1 quart
473ml= 1 pint
3785ml (3.785L)= 1 gallon
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63
Q

why are generic drugs cheaper?

A
  • bc manufacturers have not had the expense of developing and marketing a new drug and there is no patent to prevent other companies from making and selling the drug so competition also drives the price down
  • not cheaper bc they are inferior
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64
Q

what is the most rapid and complete method of emptying the stomach

A

gastric lavage (washing of stomach contents w/ saline and removal via nasogastric tube)

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65
Q

chart orders consists of

A
  • name and strenght of med
  • dose
  • route and freq.
  • date
  • signature of prescriber

*duration of therapy or number of doses NOT always indicated– order continues until DC’ed by prescriber or terminated per hospital policy

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66
Q

What CYP isozyme results in:

increased antipsychotic drug toxicity

A

CYP2D6 (PM)

*metabolism is detoxifying

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67
Q

what are idiosyncratic reactions? Give example

A
  • Genetically determined abnormal response to a drug
  • unpredictable
    ex. prolonged muscle paralysis due to impaired metabolism
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68
Q

what is the difference between a drug and a dietary supplement

A

Drug- therapeutic agent (Rx or OTC) intended to DIAGNOSE, TREAT, CURE, or PREVENT a disease— has been tested to demonstrate safety and efficacy in studies

Dietary supplement- intended to SUPPLEMENT diet and contains a VITAMIN, MINERAL, AMINO ACID, or HERB/BOTANICAL– sold to public w/o prior evidence of safety and efficacy

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69
Q

give an example of a indirect pharmacodynamic effect drug-drug interaction

A

pharmacologic effects of one drug indirectly affects another’s drug action

ex. diuretic (hypokalemia) + digoxin –> enhanced digoxin toxicity

70
Q

What are the 4 main categories of drugs and what are they primarily distinguished by

A
  1. prescription drugs
  2. controlled substances
  3. OTC drugs
  4. dietary supplements

Distinguished by:

  1. were they evaluated for efficacy and safety prior to use in patient
  2. availability by RX only or direct purchase OTC
  3. potential for abuse (physiologic or psychologic dependence)
71
Q

Most common mechanism for drug passage across biological membrane

A

Lipid passive diffusion

*drug must be lipophilic

72
Q

How can you manipulate passive reabsorption in the kidneys?

A

change pH

Acidify w/ NH4Cl / ascorbic acid
Alkalinize w/ NaHCO3

73
Q

what Phase I oxidation reactions are CYP450 independent?

A
  1. Amine oxidases

2. Dehydrogenations (alcohol and aldehyde)

74
Q

Dietary Supplements and herbal medications are NOT inherently safer bc they are natural. They should only be used for:

A
  1. tx of mild, self limiting conditions
  2. Pt can self-diagnose condition
  3. Pt. can self-assess when persistence of condition requires physician visit

ex. diarrhea

75
Q

what is a drug allergy? Example

A
  • adverse response of immunologic origin
  • unpredictable
  • severity is does INDEPENDENT
    ex. Penicillin-induced anaphylactic shock
76
Q

What is the purpose of phase I reactions

A

-usually inserts of unmasks a functional group on the drug (-OH, -SH, -NH2) that renders the molecule more water soluble and the molecule can then undergo conjugation in a phase II rxn

77
Q

what CYP enzyme helps w/ detoxification of acetaminophen

A

CYP2E1

78
Q

What Schedule of drugs are these?

  • Opioids: Codeine combined with non-opioids*
  • Anabolic Steroids: Testosterone and esters, synthetic androgens
  • Cannabinoids: Dronabinol
A

Schedule III drugs

79
Q

how can drug-drug interactions effect excretion?

A
  1. change GFR (ex. aminoglycosides)
  2. change tubular secretion (ex. PCN)
  3. change tubular reabsorption via changing urine pH (ex. amphetamine, ASA)
80
Q

parameters for distribution

A

Vd

81
Q

What is the most important organ for excretion?

A

kidneys

*esp. for water-soluble and non-volatile compounds

82
Q

___ will have NO effect in the absence of the agonist for that receptor

A

Antagonist

*the extent of the effect of an antagonist will depend of the level of “normal tone” mediated by the agonist in that tissue

83
Q

What CYP isozyme results in:

non-response to antidepressants

A

CYP2D6 (UM)

*metabolism is detoxifying

84
Q 
Convert metric to avoidrupois/ apotheracry/household: WEIGHT
1 grain=
1 oz= 
2.2 pounds= 
1 pound=
A

1 grain= 60-65mg
1 oz= 28.35-30 grams
2.2 pounds= 1 kg or 1000 grams
1 pound= 16 oz or 454 grams

85
Q

treatment of methanol and/or ethylene glycol toxicity

A
  1. inhibit rate limiting enzyme (alcohol-DH) w/ ethanol (a competitive inhibitor) or fomepizole to inhibit production to toxic metabolite (INHIBIT TOXICATION)
  2. hemodialysis
  3. Correction of metabolic acidosis w/ sodium bicarb
86
Q

Factors influencing Drug Membrane passage

A
  1. Molecular size
  2. lipid solubility
  3. Degree of ionization
  4. Concentration gradient
87
Q 
what do these abbreviations mean? (used in freq. or timing)
*qd=
*qid=
hs=
stat=
bid=
*qod=
ac=
prn=
tid=
qam=
pc=
A 
qd=every day
qid= 4x a day
hs= at bedtime
stat= immediatel
bid= 2x a day
qod= every other day
ac= before meals
prn= as needed
tid= 3x day
qam= every morning
pc= after meals
88
Q

Describe Schedule V drugs

A
  • Accepted medical use, abuse potential EVEN LESS than drugs in schedule IV
  • Can be obtained without prescription (OTC) in some states (with restrictions)

*Treated like schedule III-IV in Colorado

89
Q

what claims require FDA evaluation and authorization prior to its use?

A

*Health claims— effect substance has on reducing
risk of or preventing a disease
ex. Ca may reduce the risk of osteoporosis

Structure/function claims DO NOT

90
Q

what are example of drugs with narrow TI that need to be closely monitored for drug-drug interactions

A

warfarin

insulin- antidiabetic agents

91
Q

FDA requires that manufacturers of generic drugs demonstrate their formulation is ______ to brand name formulation, which entails __

A

bioequvialent

  • bioequivalent if:
    1. Rate and F of the active drug is absorbed and becomes available at the site of action is similar to brand name
    2. if 90% CI of the mean AUC and mean Cmax of generic product is within 80-125% of the brand product
92
Q

what method of absorption prevention is best if poison was ingested w/in 60 min.

A

gastic lavage

93
Q

what does the state government control in regards to drug regulation?

A
  • controls WHO can prescribe drugs through licensing process

* exception is federal DEA regulates controlled substance prescribing

94
Q

pharmaceutical equivalent formulations that are bioequivalent means what?

A

-The rate and extent to which the active ingredient is absorbed from a drug FORMULATION and becomes available at the site of action

95
Q

most schedules of drugs have the same risk of developing physiologic and psychologic dependence EXCEPT for

A

Schedule III

Physiologic=  MODERATE
Psychologic= HIGH
96
Q

how can you change tubular reabsorption?

A

change urine pH

  1. increase urine pH=
    - decreased tubular reabsorption for WA= decreased Cp (ex. ASA)
    - increased tubular reabsorption for WB= increased Cp (ex. amphetamine)
  2. decrease urine pH=
    - increased tubular reabsorption for WA= increased Cp
    - decreased tubular reabsorption for WB= decreased Cp
97
Q

Time to reach steady state plateau AND time to eliminate all drug is related to what?

A

Half life of a drug only

-INDEPENDENT OF DRUG DOSE

98
Q

what are pharmaceutical equivalents

A

drug products containing the same:

  • active ingredient in same dosage formulation (capsule, tablet, solution, etc.)
  • that have the same route of administration, and
  • are identical in strength or concentration
99
Q

Prescription Construction components

A
  1. Choice of drug/product
  2. Date*
  3. Identity of the prescriber*
  4. Patient information*
  5. The symbol Rx (latin for recipe-“take thou”
  6. Drug, strength, quantity/formulation*
  7. Directions to patient, aka dosage regimen or signa/”sig”
  8. Chart order in hospitals or similar type inpatient settings- Consists of name/strength/dose/route/frequency of admin/date/signature
  9. Refill information
  10. Childproof container
  11. Signature, DEA number

*indicates required by law

100
Q

what are medical foods?

And what are examples of diseases that can be MANAGED by a medical food?

A
  • a foof which is formulated to be consumed or administered ENERTALLY under the supervision of a physician and is intended for a SPECIFIC dietary management of a disease or condition
    ex. inborn errors of metabolism can be managed by a medical food
  • diseases resulting from essential nutrient deficiencies ARE NOT (ex. sucvy, pellagra)
101
Q

how can drug-drug interactions affect distribution?

A
  1. protein-binding and displacement of 1 drug by other
  2. drug effects blood flow, which can effect clearance

ex. drug decreases CO= decreased hepatic flow= decreased hepatic clearance= increased Cp

102
Q

Effects of drug binding to protein

A
  1. reduces concentration of active, free drug
  2. reduces metabolic degradation and reduce rate of excretion (which leads to decreased elimination rate and increased half life–> prolong drug action)
  3. Decrease volume of distribution (by enhancing apparent solubility in blood)
  4. Decrease ability to enter CNS across BBB
103
Q

Describe Phase II testing in human trails

A

Phase II: Clinical Investigation: Does it work in patients?

  • 2 yrs
  • 200-300 selected patients (ideally w/o other conditions)
  • compare to placebo or existing treatment
  • safety and efficacy evaluated: final dosing and regimen adjusted, may detect broader range of toxicities

*usually done at Universities or Gov. medical centers under IRB suppervision

104
Q

What is Class A drugs for pregnancy?

examples?

A

Controlled studies showed NO risk in 1st trimester
-Possibility of fetal harm appears remote

ex. potassium chloride

105
Q

what is the difference between physical and psychological dependence?

A

physiologic–stop abruptly and if you experience W/D sx

Psychologic – craving, w/o medical complications

106
Q

What CYP isozyme results in:

Insufficient analgesia w/ codeine

A

CYP2D6 (PM)

  • due to failure to metabolize to active metabolite morphine
  • metabolism is activating
107
Q

what type of antagonist can be overcome by increasing [agonist]

A

competitive antagonist

  • shifts curve to the right
  • Emax unchanged, potency decreased, EC50 increased
108
Q

what patients are at higher risk for drug-drug interactions

A
  • elderly
  • in high risk clinical situations: dependent on drug treatment, acute illness, unstable disease
  • renal/hepatic disease
  • have multiple prescribing physicians
109
Q

what is a structure/function claim?

A
  • describes the role of substance intended to maintain the structure or function of the body
  • Do not require preapproval by FDA
  • CANNOT mention SPECIFIC disease
    ex. Ca may help maintain bone health
110
Q

what is the schedule for:

  • Barbiturates
  • Tramadol
  • Benzodiazepines
  • Marijuana
A
  • Barbiturates= 2
  • Tramadol= 4
  • Benzodiazepines= 4
  • Marijuana= 1
111
Q

How can you reduce fluctuations between doses?

A

-You want tau (dosing interval) MUCH SHORTER than t1/2

  • If tau is less than or equal to t1/2= fluctuate less than 50%** (most drugs do this)
  • if tau is much larger than t1/2= fluctuation is maximal
  • if tau is much shorter than t1/2= little fluctuation
112
Q

FDA has ___ regulatory control over sale and distribution of dietary supplements

A

minimal

113
Q

The single most important determinant of poisoning is ___

A

provision of good SUPPORTIVE CARE (ie. vitals and fluids)

**essential until the toxin is eliminated

114
Q 
Convert metric to avoidrupois/ apotheracry/household: VOLUME
1 drop= 
1 tsp=
1 Tbsp=
1 fluid oz= 
1 quart=
1 pint= 
1 gallon=
A 
1 drop= 0.05 ml
1 tsp= 5ml
1 Tbsp= 15ml
1 fluid oz= 29.56-30ml
1 quart= 946ml
1 pint= 473ml
1 gallon= 3785ml (3.785L)
115
Q

How can we increase elimination?

A
  1. increase conjugation
  2. increase H2O solubility
  3. increase ionization via conjugation
116
Q

Describe Phase IV in new drug evaluation

A

Post-marketing Surveillance

  • manufacturers required to submit reports to FDA of any ADR
  • Studies often continue after approval (on mortality/morbidity/safety)
  • Study groups omitted in phase I and II due to increased risk (preg, kids, elderly, multiple diseases)
  • FDA can REVOKE approval or restricted drug use if unpredictable ADR become apparent
117
Q

What does chelation w/ heavy metals do to help with drug poisoning?

A
  • chelating agents complex w/ free metal ions in body fluids reducing their concentration and thereby promoting the dissociation of metals from functional intracellular macromolecules
  • increases renal elimination and inactivates the metal toxin
118
Q

what does the FDA regulate (fed. gov)

A
  1. Evaluation process for new drugs (safety and efficacy) and removal of unsafe dietary supplements (BUT only AFTER their availability to public)
  2. equivalency of brand vs generic
  3. placement of drugs into RX or OTC catergories (DEA reg. controlled substances)
119
Q

when Identifying prescriber on a prescription, you must include

A

name
address
license classification (professional degree)
phone number

*usually preprinted

120
Q 
Reminder phrases for Rx directions include:
\_\_ for internal use
\_\_ for ointment/lotion
\_\_ for eye, ear, and nose meds
\_\_ for suppository
\_\_ for inhalers
A 
take- for internal use
apply- for ointment/lotion
place/instill- for eye, ear, and nose meds
insert- for suppository
inhale- for inhalers
121
Q

describe the progression of methanol and ethylene glycol toxicity

A

Methanol–> FORMIC ACID–> metabolic acidosis w/in 4-12 hrs–> retinal damage and blindness–> stop breathing–> death

Ethylene glycol–> OXALIC ACID –> deposition of calcium oxalate crystals –> acidosis and acute renal failure

**minimal toxicity until they undergo metabolism

122
Q

what Schedule of drugs are these?
Opioids: Heroin and other synthetic opioids Hallucinogens: LSD, MDMA, peyote, mescaline, psilocybin, phencyclidine (PCP) Marijuana Methaqualone

A

Schedule I

123
Q

What is Class D drugs for pregnancy?

examples?

A
  • Positive evidence of human fetal risk BUT potential benefits may outweigh the potential risks if needed in a life-threatening situation or a serious disease
    examples: Oral anticoagulants, ACE inhibitors/AT1 antagonists, diazepam-lorazepam, alprazolam, paroxetine
124
Q

what type of drug metabolism reaction is most utilized in pro-drugs?

A

esterases (hydrolysis) - phase I

125
Q

Describe Schedule IV drugs

A

Accepted medical use, LOW potential for abuse leading to limited dependence

126
Q

what method of absorption prevention is best if poison was ingested more than 60 min. or if toxin is in enteric coated tablets, or if toxin is hydrocarbon

A

osmotic cathartic

127
Q

Controlled substances are divided into 5 schedules based upon potential for:

A
  1. medical usefulness
  2. abuse potential
  3. degree to which they may lead to physical/psychological dependence if they are abused

(Schedule I= highest for abuse, Schedule V= lowest/limited)

128
Q

what is good at prediciting which drugs will be removed by dialysis/ exchange transfusion

A

drugs w/ low Vd (less thank 1L/kg)

129
Q

what is the toxic dose of acetaminophen

A
  • Single dose greater than 10-20g

- more than 4g/day

130
Q

Describe what efficacy is

A

Emax

-Shows the LIMIT of the DR response at Emax

131
Q

describe the pre-clinical testing phase of a new drug

A
  • animal studies for 5-8 yrs
  • evaluate: pharmacology, metabolism, and toxicity (and chronic toxicity)
  • Attempt to determine safe dosage for human use (highly predictive, but not totally reliable)
  • then submit IND application. NDA filed for specific indication/use
132
Q

what are side effects? Give examples

A

Reactions that are unrelated to the therapeutic goal

  1. same DR interaction for TE but at different organ/system
    ex. B-adrenergic R. lowers BP on heart but causes bronchospasm at lung
  2. unrelated pharmacodynamically to therapeutic response
    ex. Minoxidil (an antihypertensive) causes hypertrichosis
  • dose-dependent
  • predictable
133
Q

what are pharmaceutical alternatives

A

Drug products that have
SAME therapeutic moiety, BUT
-different salts, esters, or complex of that moiety, OR are different dosages forms
ex. capsules vs tablets or 200mg vs 250mg

134
Q 
Convert metric to avoidrupois/ apotheracry/household: WEIGHT
60-65mg = 
1 gram= 
28.35-30 grams=
454 grams= 
1000 grams (or 1 kg)=
A

60-65mg = 1 grain

1 gram= 15.43 gains

28.35-30 grams= 1 oz (437.5 grains)

454 grams= 1 pound (16 oz)

1000 grams (or 1 kg)= 2.2 pounds

135
Q 
what do these abbreviations mean? (used for routes)
*ad=
*od=
IA=
IVPB=
sc, sq=
*as, al=
*os, ol=
IM=
po=
vag=
*au=
*ou=
IV=
pr=
A

*ad= right ear
*od= right eye
IA= intra-arterial
IVPB= IV piggyback
sc, sq= subcutaneous
*as, al= left ear
*os, ol= left eye
IM= intramuscular
po= by mouth, orally
vag= vaginally
*au= both ears
*ou= both eyes
IV= intravenous
pr= per rectum, rectally

136
Q

how can toxic doses affect absorption

A

large amount of ingested drug may slow tablet dissolution, alter GI emptying, or injure GI tract–> alter absorption rate–> delay peak effect

137
Q

Examples of drugs whose metabolism of inactive compound results in active compound (designed to)

A

omeprazole–> a sulfenamide
enalapril–> enalaprilat
valacyclovir–> acyclovir

138
Q

If the FDA approves the NDA, it will allow sales as Rx or OTC w/ stringent controls on __, __ and ___

A

labeling
packaging insert
advertising

*FDA regulates what indication for drug use the manufacturer can place in the package insert and what claims the manufacturer can make in advertising BUT CANNOT regulate how a drug is actually prescribed by physician (off-label use)

139
Q

how does N-acetylcysteine help tx acetaminophen toxicity

A
  • precursor for tluthation synthesis, which helps detox. Ac*

- acts as a neutrophile to inactivate the electrophilic Ac*

140
Q

Describe different mechanisms of transduction signal amplification

A
  1. ligand-ion gated- Fastest– change in membrane potenital
  2. G-Coupled Receptors (fast)– produce effector/ 2nd messenger (cAMP, cGMP, IP3)
  3. Hormone R. or Kinase linked R.- (slow)– change in gene transcription
141
Q

Clinically relevant Inhibitors

A
  1. Cimetidine*
  2. Erythromyocin/ Clarithromycin
  3. Ketoconazole/ Azole antifungals
  4. Fluoxetine (and other SSRIs)
  5. Grapefruit juice*
  6. HIV protease inhibitors
  7. Omprazole*

*don’t need RX

142
Q

how is acetaminophen toxicity eliminated

A

5-10% in phase I via CYP2E1–> produces Ac* when phase II becomes saturated
70-80% in phase II w/ glucuronic acid or sulfate (glucuronidation and sulfate conjugation)

Ac* is DETOXIFIEDby GSH-transferase

143
Q

how might toxic doses affect half life?

A

prolong half life due to saturation of the elimination mechanisms

144
Q

what type of reactions can produce toxic intermediates?

A

Nitro reductions (phase I)

145
Q

what are ways to circumvent or prevent drug-drug interactions in patients

A
  1. Document all meds the patient is on
  2. minimize number of prescription drugs
  3. use alternative non-interacting drug
  4. modify dosing schedule (to compensate for anticipated interaction)
  5. be vigilant w/ patients on drugs with narrow TI or in high risk clinical situation (acute illness, depended on drug tx, have unstable disease)
146
Q

when is hemo/peritoneal dialysis and hemoperfusion good choices for enhancing elimination to help tx poisoning?

A

hemo/peritoneal dialysis:

  • toxins w/ small Vd
  • low protein-binding capacity
  • assists in correction of fluid and electrolyte imbalance

hemoperfusion:

  • toxins w/ high MW
  • poor water solubility
  • Might CAUSE bleeding and electrolyte disturbance
147
Q

Are immediate-release products equivalent to extended-release products of the same active ingredient?

A

NO!

148
Q

what mechanisms can lead to increased Cp leading to toxicity

A
  • reduced elimination (most common)

- protein bound displacement

149
Q

-Product FORMULATION are tested for ____ NOT __

A

bioequivalence NOT the drug’s bioavailabilty

150
Q

Rx directions for a patient should include

A

amount of drug taken, time freq, route of adminstration, duration of therapy

151
Q

What is the purpose of phase II reactions

A

-Endogenous substrate combines w/ pre-exisiting or metabolically inserted functional group (via phase I) on a the drug forming a highly polar (water soluble) conjugate that is readily excreted via the URINE

152
Q

what prescriptions CANNOT be called in

A

controlled substances

153
Q

what 3 sections did the FDA add to recognize shortcomings of pregnancy and breastfeeding in current prescription drug labeling

A
  1. Fetal risk summary- known effects of fetus and risk
  2. Clinical Considerations-effects of use of the drug and RISK OF THE DISEASE to the mother and fetus
  3. Data- details regarding use of drugs in humans and animal studies
154
Q

What CYP isozyme results in:

Decreased efficacy of PPIs for peptic ulcer disease

A

CYP2C19 (PM)

*metabolism is activating

155
Q

what is the relationship between receptors occupied by drug (DR) and response?

A

RD is proportional to response
(as depicted by dose-response curve)

RD can reach a max so therefore response levels off too (Emax= all receptors are occupied by drug)

156
Q

what is the primary organ of drug metabolism

A

liver

157
Q

How can you reach a steady state concentration sooner?

A

By giving a loading dose

-increasing MD will only set your [SS] higher

158
Q

what is Ipecac and how does it work?

A
  • an emesis (empties stomach contents rapidly) to REDUCE absorption in poisoning
  • works w/in 15-30 min., may repeat 1x in 20 min.
  • Mechanism: LOCAL irritation and CNS stimulation of chemoreceptor zone (CTZ)

*effective orally, must be given BEFORE charcoal

159
Q

Predisposing factors for hepatocellular damage from acetaminophen toxicity

A
  1. increased CYP2E1 activity
  2. decreased hepatic glutathione content

*both occur w/ excessive alcohol consumption

160
Q

how can an INHALED drug be manipulated for systemic vs local use?

A

volatile gas= systemic

aerosol particles = local

161
Q

Describe Phase I testing in human trails

A

Phase I: Clinical pharmacology: Is it safe, PKs?

  • 1-10 yrs
  • select 20-100 normal healthy volunteers (males 18-45y/o)
  • Toxicity and metabolism studies (look at half-life, absorption, elimination)
  • Determine if animal/human response differs significanly
162
Q

when will low incidence drug effects be missed and why?

A

in Phase I-III

To detect a 2-fold increase in incidence to effect (drug vs non-drug) if:
1 in 100 incidence need 1,800 pts
1 in 1000 incidence need 18,000 pts
1 in 10,000 incidence need 180,000 pts

**practitioners must play active role in reporting ADR

163
Q

What Schedule of drugs are these?

-Opioids: Pentazocine, Butorphanol
-Stimulants: Phentermine, Sibutramine
-Depressants:
Benzodiazepines* (alprazolam, diazepam, triazolam, lorazepam, midazolam)
Zolpidem, zaleplon
Chloral hydrate
Meprobamate
-Tramadol*

A

Schedule IV drugs

164
Q

Protein binding and displacement drug-drug interactions is only of clinical consequence when:

A
  1. displaced drug has narrow therapeutic index
  2. displacing drug is started in high doses
  3. displaced drug has low Vd
  4. Response to drug occurs more rapidly than redistribution
165
Q

bioequivalent products are assumed to be _____

A

therapeutic equivalents (same dosage regimen provides same efficacy and safety)

*requires expensive, time-consuming human trials so not usually determined and NOT required by FDA

166
Q

How can you enhance elimination to help tx poisoning

A
  1. extracorporeal removal (hemo-/peritoneal dialysis and hemoperfusion)
  2. enhance metabolism via induction, inhibition or enhancing detox.
  3. Enhance renal excretion (forced diuresis or block passive tubular reabsorption in kidney via changing urine pH)
  4. Chelation of heavy metals
167
Q

Examples of drugs whose metabolism of active drug results in a toxic metabolite

A

Acetaminophen–> N-acetyl-benzoquinoneimine (hepatotoxic, Ac*)

168
Q

Controlled Drugs Current Requirements for Prescribing

A
  1. a DEA number (physician registers with DEA)
    2.  Schedule I drugs may NOT be prescribed
    3.  All schedule II-III-IV drugs require a prescription (in
    Colorado II-III-IV and V)
    4.  Schedule II must be in ink in prescriber’s handwriting- cannot be telephoned to pharmacist - cannot be
    refilled *cannot fill for more than 90 days
  2. Schedule III and IV (plus V in Colorado) may be
    telephoned to pharmacist- may be refilled up to 5
    times in 6 months (if so noted on prescription)
169
Q

when is standard safety margin used over therapeutic index?

A
  • more reliable if the patient response to the therapeutic and/or toxic effects of a specific drug varies widely
  • more conservative measure than TI and takes into account the EXTREMES of a population, rather than midoints
170
Q

types of pharmacodynamic drug-drug interactions

A
  1. Antagonistic effects: occur when 2 drugs w/ opposite pharmacological effects given together
  2. Synergistic or additive TE: when drugs w/ similar therapeutic effects given together (ex. BB + diuretic= enhaced BP lowering)
  3. Synergistic or additive side effects: similar to above, but involves SE (ex. ethanol and Benzo= increased CNS sedation)
  4. Indirect pharmacodynamic effect: pharmacologic effects of one drug indirectly affects another’s drug action
171
Q

is inhibition or induction faster?

A

inhibition

*w/in hrs while induction requires 48-72 hrs

172
Q

are herbal medications required to show proof of safety, efficacy, purity, and quality control?

A

purity and quality control: Yes- as of 2011

*do not have to show safety or efficacy– burden of proof w/ FDA to show unsafe

Pharmacology (31 decks)

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