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IPAP > Pharm 1: Block 1 > Flashcards

Pharm 1: Block 1 Flashcards

1
Q

Define Prescription

A

Prescriber’s order for a specific patient

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2
Q

Define “Sig”

A

Signetur

“let it be labeled”

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3
Q

What are the two safety categories of prescriptions

A

Legend- federal requires Rx for drug prescription

OTC- considered safe for self-administration

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4
Q

FDA determines if a drug should be a legend or OTC based on what?

A

Safety Consideration

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5
Q

Who controls and monitors drugs considered to have abusive potentials?

A

DEA

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6
Q

Who approves what indications a drugs is used for?

A

FDA

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7
Q

Define Labeled Use

A

FDA approved a New Drug Authorization saying drug is safe/effective for an indication

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8
Q

Define Unlabeled Use

A

Use of a medication for an indication that has not been approved by the FDA

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9
Q

What is the generic name for Neurontin?

A

Gabapentin

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10
Q

PAs may be privileged to write Rxs for medication that have been approved and recommended by whom?

A

Pharmacy and Therapeutics Committee

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11
Q

What is the military’s Rx form number?

A

DD 1289

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12
Q

Rxs for children 12 y/o and younger need to include what other two pieces of info?

A

Age

Weight

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13
Q

What are the 4 drug name/classifications?

A

Chemical Name
Drug Name- Trade/Brand, Generic
Pharmacotherapeutic Class
Target Physiologic System

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14
Q

What drug name is used by the FDA and which one is used by a company/manufacturer?

A 
Trademark= trade/brand
Generic= FDA
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15
Q

DoD allows a __ day supply for a maintenance medication

A

90 days

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16
Q

How many refills are allowed for Schedules 2-5?

A

2: None

3-5: 5 x in 6mon, what ever happens first

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17
Q

What additional info is added to a hand written prescription for controlled substances?

A

Quantity of meds is written/spelled out in numeric and letters

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18
Q

What are 4 factors that encourage PT noncompliance?

A

Asymptomatic
Inc frequency
Direction difficulty
Side effects

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19
Q

Define ASA

Define ATC

A

Aspirin

Around the clock

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20
Q

Define HA
Define HTN
Define HOTN

A

Headache
Hypertension
Hypotension

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21
Q

Slide 24 25 26 27

A

Abbreviations

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22
Q

What is the difference between adverse drug reaction and medication error?

A

ADR: unexpected/unintended response to a med

ME: event leading to inappropriate medication use

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23
Q

Define Allergic Reaction

A

Immunologic hypersensitivity that occurs after medication use where the drug acts as an Ag in the body

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24
Q

Define Idiosyncratic Reaction

A

Abnormal susceptibility to a medication that is peculiar to an individual
Antihistamine causing excitement instead of sedation

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25
Q

Who classifies/categorizes controlled substances?

A

DoJ

DEA- Office of Diversion Control, Title 21 USC CSA

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26
Q

What are the limitations/regulations on filling a Schedule II Rx?

A

No Federal limit on quantity, limited by State/local law
90 day limit for matinenance
No federal time limit to fill
No refills

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27
Q

What happens if a pharmacist fills a Schedule II drug in an emergency situation?

A

May dispense quantity to adequately treat PT during emergency period
Prescribing practitioner must provide written/signed Rx w/in 7 days

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28
Q

What are 3 exception for when a faxed prescription can serve as an original Rx and no further verification is required?

A

Compounded for direct administration
Long term care facilities
Hospice

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29
Q

During what period of instruction is a human embryo’s growth disrupted?

A

Organogenesis- 3-8wks

Teratogenic agents

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30
Q

What does maternal alcohol abuse do to a developing fetus?

A

Microcephaly

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31
Q

What does maternal ACE inhibitor use cause to a developing fetus?

A

Renal function

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32
Q

What does maternal warfin use do to a developing fetus?

A

Cartilage defects

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33
Q

Define Category A Drug

A

Safe for human and baby

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34
Q

Define Category B Drug

A

No risk to fetus

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35
Q

Define Category C Drug

A

Adverse to fetus

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36
Q

Define Category D Drug

A

Evidence supporting adverse effect to fetus

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37
Q

Define Category X Drug

A

Do not give to pregnant woman

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38
Q

FDA required the use of what 3 subsection labeling?

A

Pregnancy
Lactation
Reproductive risk potential

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39
Q

What makes up Tiers 1 and 2 of DoD Formulary?

A

BCF- 1 & 2, must be carried by all MTFs
ECF- 1&2, must be carried if medical service is offered
UF Drugs- 1&2

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40
Q

Define Tier 3 Drugs

A

Non formulary drugs

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41
Q

Define Tier 4 Drugs

A

Medication is not covered, copayment reduction for required need

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42
Q

What is the Uniform Formulary?

A

Pharmaceuticals listed by therapeutic classes determined by DoD P&T committee

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43
Q

Define Non-Formulary Unit

A

Agents not selected for UF

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44
Q

Define Basic Core Formulary

A

List of pharmaceuticals required to be on local formulary

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45
Q

Define Extended Core Formulary

A

Medicatoins used to support specialized scopes of practice than the BCF

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46
Q

What happens if an MTF chooses to have an ECF on its formulary?

A

Must have all ECF medications in that class on the formulary

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47
Q

Define Non-Formulary

A

Medication that can be provided at formulary cost share if the provider supplies information showing there is a medical need/necessity

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48
Q

What are the phases of drug development?

A 
Pre-clinical
Phase 1-4
Pre- animal pharm/tox
1- Healthy volunteers
2- PTs w/ disease/condition
3- Large scale multi-center
4- Post-marketing surveillance
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49
Q

Define Pharmacokinetics

Define Pharmacodynamics

A

What body does to drug

What drug does to body

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50
Q

What do the 4 phases of pharmacokinetics encompass?

A

ADE
Administration
Systemic circulation
Site of action concentration

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51
Q

What are the 4 phases od pharmacokinetics?

A

ADME

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52
Q

What are the pharmacokinetics taken into consideration when determining dosage regimen

A 
Bioavailability
Volume of distribution
Drug accumulation
Clearance
Elimination
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53
Q

What are some factors that determine drug’s access to a molecules site of action?

A 
Route
Absorption
Distribution
Binding
Metabolism
Clearance
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54
Q

What happens when a weak acid is placed into an acid medium?

A

Shift to left, suppresses ionization

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55
Q

What happens when a weak acid is placed in an alkaline medium?

A

Ionization increases

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56
Q

What happens when a weak base is placed into an acid medium?

A

Shift to left, increased ionization

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57
Q

What happens when a weak base is placed into an alkaline medium?

A

Shift to right, suppresses ionization

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58
Q

A drugs ability to move from an aqueous to lipid environment depends on what?

A

Charge

pH of solution

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59
Q

Define Hydrophilic

A

Hydro: Charged, Polar
Lipo: Uncharged

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60
Q

Define the Henderson-Hasselbalch equation

A

Relationship between ratio of acid to base

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61
Q

Define pKa

A

negative base log of the acid dissociation constant of a solution
Low= acidic
High= basic

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62
Q

Ph of a biologic fluid that dissolves a drug affects what two results?

A

Degree of ionization

Rate of transport

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63
Q

What happens if/when the pKa of a drug equals the pH of the surroundings?

A

50% ionization occurs

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64
Q

Define Weak Acid

A

H: concentration of protonated/unionized form
A: concentration of ionized/unprotonated form

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65
Q

Define Weak Base

A

BH: concentration of protonated form of base
B: unprotonated concentration

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66
Q

How will sodium bicarbonate effect the renal excretion of weak acids?

A

Increases elimination by increasing urine’s pH, turns the weak acid into unprotonated/ionized

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67
Q

Alkalinizing urine will have what effect on elimination?

Acidification of urine will do?

A

Alk: increases elimination of acidic
Acid: increases basic drug elimination

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68
Q

Define Bioavailability

A

Fraction of unchanged drug reaching the systemic circulation after oral administration

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69
Q

What determines/how is bioavailability determined?

A

Extent of absorption

First pass metabolism

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70
Q

What is an example of a drug that is close to 100% bioavailable?

A

IV drugs

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71
Q

What factors affect passage of drugs across biologic membranes?

A

Lipid-aqueous partition coefficient (ionization/non-ionized coefficient)
Specific transport
Plasma binding
Perfusion rate

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72
Q

____ is the primary site of drug metabolism and _____ is reduced

A

Liver

Bioavailability

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73
Q

First Pass Metabolism primarily applies to what type of drug but may limit efficacy if ?

A

Oral administerred

Efficacy limited if clearance by liver is large

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74
Q

What systemic circulation by influence overall first pass metabolism?

A

Enterohepatic

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75
Q

What are 3 ways to obtain better systemic absorption of a drug that has high first-pass effects?

A

Increased dose
Alternate admin route
Delayed release drug product

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76
Q

What are the two drug transport proteins?

A

Albumin

A1-acid glycoprotein

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77
Q

Drugs bound to ___ proteins are not active and only ____ drugs are active

A

Plasma

Free

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78
Q

Free drug is available to undergo what two processes?

A

Bind w/ receptor

Metabolize/eliminated

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79
Q

When/why is plasma protein binding important?

A

High plasma protein bound drugs- ibuprofen

Drugs w/ narrow therapeutic index- phenytoin

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80
Q

Define Drug Modeling

A

Describes drug distribution behavior in body by using compartmental models

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81
Q

What are 4 characteristics of compartmental models?

A

Simplification
Non-representative of single tissue
1 / 2 / 3 compartment model
Highly perfused compartments = 1 compartment

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82
Q

Define One Compartment Model

A

Simplest
Comprises all body tissues
Assumes instant distribution through body

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83
Q

Define Two Compartment Model

A

Distribution is not instant
Fist compartment- blood, and highly perfused tissue
Second- less accessible tissues

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84
Q

Define Volume of Distribution

A

Volume that drug distributes and evaluates extensive/limited distribution
“Where the drug goes in body”

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85
Q

What is the volume of distribution equation and parts?

A

Vd=Fdose/Co
F- bioavail
Dose- weight of drug given
C- concentration of drug in blood/plasma

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86
Q

What unit of measurement is Volume Distribution (Vd) reflected in?

A

L

L/kg

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87
Q

Define Small and Large Volume Distribution

A

Minimal drug distribution

Extensive drug distribution

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88
Q

How does plasma proteins affect volume of distribution?

A

Drug w/ affinity for protein in plasma will have reduced Vd, decreased plasma proteins will increase Vd

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89
Q

What is the major plasma protein involved in drug protein binding?

A

Albumin

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90
Q

What two structures make the BBB?

A

Capillaries covered in astrocytes

Endothelial cells making tight junctions

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91
Q

How does the placenta affect drug passage?

A

Lipid solubility facilitates entry

Placenta is porous, allows large hydrophilic molecules to cross which allows fetal blood levels to increase slowly

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92
Q

Metabolic pathways of drugs normally alter drugs in what ways?

A

Deactivate
Detox
Less active

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93
Q

What are the two major type of drug metabolism reactions?

A

Phase I: Non-synthetic, Cytochrome P450
Phase 2: Synthetic, Glucuronidation
Phase 1 -> Phase 2= conjugation

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94
Q

What are examples of Phase 1, Non-Synthetic reactions?

A

Oxidation
Reduction
Hydroxylations

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95
Q

How does Phase 1, Non-Synthetic reactions work?

A

Introduce function groups to molecules
Converts parent drug to polar metabolite
Causes loss of pharmacologic activity

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96
Q

How do Phase 2, Synthetic metabolism reactions work?

A

Conjugation reactions
Covalent linkage w/ functional group on parent compound
Highly polar conjugates= rapid drug elimination from body

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97
Q

Define Inactive Metabolite

A

Active compound becomes inactivated/detoxed

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98
Q

Metabolites that retain similar activities are retaining what part of their molecular structure?

A

Retain activity of parent compound

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99
Q

What does a metabolite with altered activity mean?

A

Develops different activity from parent drug

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100
Q

Define Bioactive Metabolites

A

Prodrug- inactive substance that must be converted by metabolism to become biologically active
Prodrug= inactive form

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101
Q

Define Cytochrome P450 Enzymes

A

Mixed function oxidases responsible for majority of drug metabolism

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102
Q

Define Cytochrome P450 System Substrate

A

Substance on which enzyme acts

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103
Q

Define Cytochrome P450 System Induction

A

Accelerated metabolism resulting in decreased action of inducing/co-administered drugs

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104
Q

Define Cytochrome P450 System Inhibition?

A

Reduced metabolism of substrates/co-administered drugs metabolized by specific enzyme causing increased action of co-administered drug/substrates

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105
Q

What system is behind most clinically important drug/drug interactions?

A

Cytochrome P450 System

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106
Q

Define Chirality

A

Sereoisomerism

Geometric property of molecules/ions

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107
Q

What are characteristics of chiral molecules?

A

Non-superposable on mirror image
Rectus- right
Sinister- left

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108
Q

Define a Racemic Mixture

A

Equal mixture of enantiomers

109
Q

What are chiral molecules role in pharmacology?

A

Seperate an active enantiomer from a pair to create new drug, reduce side effects, extend presence in PTs

110
Q

Define Zero-Order Kinetics

A

Metabolic rate is dependent on time and not drug concentration
Linear kinetics
No true half-life

111
Q

Define First-Order Kinetics

A

Metabolic rate is proportional to drug concentration
Non-linear kinetics
Drug disappears w/ time
Half life is constant

112
Q

What are 4 characteristics of nonlinear kinetics?

A

Area under curve, not proportional to dose
Amount excreted in urine, not proportional to dose
Half life increases w/ high doses
Metabolite ratio changes w/ increased dose

113
Q

What are 4 variables that cause alterations in drug metabolism?

A

Genetic variability
Age
Nutrition
Concurrent Disease

114
Q

Define Child-Pugh Classes A, B, and C

A

A/B- mild/moderate impairment, no dosage adjustment needed

C- extended release tablets, not recommended

115
Q

A drugs ability to be reabsorbed from glomerular filtrate is determined by what?

A

Their lipid solubility

Charged compounds are poorly re-absorbed

116
Q

Define Clearance

A

Measure of removal of drug from plasma

Systemic= renal + hepatic + other

117
Q

What two factors determine a drug’s half-life?

What is it related to?

A

Clearance
Volume of distribution
Related to duration of action

118
Q

How is drug clearance of an organ determined?

A

Blood flow

Extraction ratio of organ

119
Q

Define Creatinine Clearance

A

Estimated renal function from 24hr UA to estimate GFR by using Serum Creatinine

120
Q

Define the Cockcroft-Gault equation

A

CrCl= ((140 - age) x kg)) / (Scr x 72)

Add (0.85) after kg for female PT

121
Q

Define Steady State and it’s General Rule

A

Drug intake is equal to elimination

5 half live to reach steady state AND for washout

122
Q

Changes in a drugs concentration do not have an effect on it’s ______

123
Q

How does No Interval/Short Interval drug administration effect the concentration?

A

Less fluctuation
Same dosing rate but as an infusion
Cmax and Cmin changes will be minimal

124
Q

How does Longer Interval drug administration change concentration?

A

More fluctuation
Longer interval, same rate
Cmax and Cmin changes will be higher toward Cmax

125
Q

Regardless of No Interval / Short Interval / Long Interval drug administration, what remains the same?

A

Average plasma concentration

126
Q

Dosing doesn’t change time to steady state as long as _____

A

Half life remains constant

127
Q

If a fluctuation in plasma concentration occurs, what controls the magnitude of fluctuations?

A

Controlling dosing interval
Shorter= decreased fluctuation
Longer= increased fluctuation

128
Q

Define Maintenance Dose

A

Does req’d to replace amount of drug lost from body to maintain plasma concentration

129
Q

What are two benefits of changing a dose interval?

A

Achieve similar steady-state concentrations

Limited dosage forms (oral)

130
Q

What is an advantage of changing a dose?

A

When goal is to maintain steady therapeutic concentrations

131
Q

What are two benefits of changing a dose and interval?

A

For substantial dose adjustment w/ limited dose forms

Narrow therapeutic index drugs w/ target concentrations

132
Q

If a drug is given more than once daily then adjust ______

but if it’s given daily or less adjust the _____

A

Interval

Dose

133
Q

Define Loading Dose

A

Higher dose of a drug to raise concentration to desired level or steady state concentration followed by a maintenance dose

134
Q

When is a loading dose used?

A

When therapeutic concentrations of drug in plasma is needed rapidly/initially

135
Q

Time to reach a steady state concentration depends on ?

A

Elimination half life

136
Q

What pharmacokinetic variables influence dosage regimens?

A

Absorption
Volume distribution
Clearance

137
Q

Define Potency

A

Amount needed to cause a response, determined by half life

138
Q

Define Efficacy

A

Drugs ability to produce desired result, determined by height of log-dose response curve
More important than potency

139
Q

Define Effectiveness

A

Degree of success in producing desired effect

140
Q

Graded response takes into account what three variables?

A

BP
Enzyme activity
Muscle tension

141
Q

Define Quantal Response

A

Number of subjects showing an all or nothing response
Pain
Death
Number anesthetized

142
Q

The higher a drugs therapeutic index means what?

A

Safe the drug is and less monitoring is required

143
Q

What is the lab monitoring rule for therapeutic indexes?

A

Small index requires plasma concentration monitoring

144
Q

Define Agonist

A

Drugs that activate a receptor

145
Q

Define Partial Agonist

A

Drug can act as an agonist or antagonist

146
Q

Define Antagonist

A

Drug reduces/prevents responses

147
Q

Define Inverse Agonist

A

Binds to same receptor as agonist but induces response opposite of an agonist

148
Q

Define Competitive Antagonist

A

Binds to same receptor as agonist but reduces potency and efficacy of agonist

149
Q

Define Irreversible Antagonist

A

Permanently antagonizes agonist through covalent bonds and prevents agonist binding and reduces efficacy

150
Q

Define Indirect Agonist

A

Inhibits termination of an action of endogenous agonist

151
Q

Define Allosteric Agonist

A

Binds to different receptor sight and indirectly blocks agonist

152
Q

Define Drug Specificity

A

Drug has one effect and only one effect

153
Q

Define Drug Selectivity

A

Greater selectivity for a receptor means fewer adverse reactions caused

154
Q

General rule is that if a drug dose goes up then ____?

A

Selectivity goes down

155
Q

Define Down Regulation

A

Decrease in number of receptors due to continuous prolonged exposure

156
Q

Define Desensitization

A

Result of down-regulation

Requires an increase drug concentration to cause desired effect

157
Q

Define Up-Regulation

A

Increase in number of receptors

3rd trimester pregnancy increase of uterine oxytocin receptors

158
Q

Define Supersensitivity/Hypersensitivity

A

Enhanced response from long term exposure and abrupt cessation of drug

159
Q

Give 4 examples of drugs who do not act at receptors?

A

Osmotic diuretics
Detergents
Antacids
Chelating agents

160
Q

Define a Chemical Agonist and give an example

A

Inactivates an agonist by not allowing agonist able to bind to activating receptor
Protamine Sulfate

161
Q

Define Physiologic Antagonist and give an example

A

Drugs that compete for interacting with opposing regulatory pathways
Epi and Ach

162
Q

Preganglionic neurons originate with ____

Postganglionic nuerons originate at _____ and terminate at ____

A

CNS

Ganglion, effector organ

163
Q

What are the two types of receptors?

A 
Nicotinic neural
Nicotinic muscluar (Muscarinic, A, B D)
164
Q

What are the neurotransmitters?

165
Q

Parasympathetic preganglionic nerves originate from _____ and leave via ____

A

CNS

Cranial and sacral regions

166
Q

Parasympathetic reganglionic neurons are _____ than postganglion

167
Q

Sympathetic preganglionic nerves leave the CNS via ____

A

Thoracic

Lumbar

168
Q

Sympathetic preganglionic nerves are ____ than postganglion nerves

169
Q

Parasympathetic postganglionic nerves result in a ___ response while sympathetic postganglions result in a ___ response

A

Discrete

Diffuse

170
Q

3 examples of chemical signaling

A

Neurotransmitters
Hormones
Local mediators

171
Q

What effects do acetycholinesterase inhibitors have on the body?

A

Prolong Ach action at muscarinic sites as an indirect agonist

172
Q

Difference between endocrine gland and exocrine gland

A

Endo- ductless secretion into bloodstream

Exo- duct secretion to environment

173
Q

M1 muscarinic receptors

A

Nerves
Salivary/stomach secretions
CNS

174
Q

M2 muscarinic receptors

A

Cardiac cells
Bladder
Smooth muscle

175
Q

M3 muscarinic receptors

A

Bladder
Exocrine glands
Smooth muscle

176
Q

Cholinergic agents modulate Ach effects in what 3 ways?

A

Agonist
Antagonist
Indirect agonist

177
Q

Drugs that mimic or prolong actions of Ach are called ?

A

Parasympathomimetics

Cholinomimetics

178
Q

Drugs that antagonize or block actions of Ach are called ?

A

Anticholinergics

179
Q

Cholinergic agonists cause what effects on the body?

A 
DUMBBELLS
Defecation
Urination
Miosis
Bradycardia
Bronchospasm
Emesis
Lacrimation
Lethargy
Salivation
180
Q

Sweat and salivary glands increase secretions from what types of stimulation?

A

Cholinergic and Sympathetic

181
Q

What are the major therapeutic uses for cholinomimetics?

A 
Anti-cholinergic OD
Glaucoma
Xerostomia
Reduced GI/GU motility
Alzeihmers
Myasthenia Gravis
Reversal of Curare-induced neuromuscular paralysis
182
Q

Don’t give cholinergic agonists to PTs with what diseases/illnesses?

A 
Bradycardia/hypotension
Asthma
Peptic ulcers
GI obstruction
GU obstruction
Parkinson's Disease
183
Q

What are the cholinergic agonist effects on eye muscles and pupils?

A

Radial Iris- a1 SNS conraction, mydriasis
Circular Iris- m3 PNS contraction miosis
Ciliary- B2 SNS relaxation/M3 PNS contraction accomodation

184
Q

How does the eye accomodate for close vision?

A

Tightens cilliary muscles allowing lens to become more rounded

185
Q

What is the cholinergistic effect on eyes?

A

Muscarinic receptors contract circular muscles (pinpoint)
Produces a spasm of accommodation
Lens bulges for near vision

186
Q

What is the cholinergistic use for clinic?

A

Refractive measurements

Ophthalmoscopic exam of retina

187
Q

What is an example of a cholinergistic drug used in clinic for eyes?

A

Pilocarpine- cholinergic agonist

188
Q

How do cholinomimetics exert their effect?

A

Increases resistance to degradation by cholinesterases

Increases selectivity for muscarinic receptors relative to nicotinic receptors

189
Q

Why is acetylcholine not used in clinic often?

A

Poor bioavailability, rapidly hydrolyzed by GI tract and inactivated by acetylcholinesterase

190
Q

Acetylcholine is nonspecific for what receptors?

A

Nicotinic and muscarinic

191
Q

Although not used often, what is a use for acetycholine such as Miochol-E?

A

Induces miosis for eye procedures

192
Q

What effect does pilocarpine have on the eye?

What effect does it cause on the rest of the body?

A

Increases aqueous humor outflow by contracting the ciliary muscle
Stims lacrimal/salivary secretions

193
Q

What is a clinical indication for using Pilocarpine?

A

Reduce intraocular pressure in glaucoma PTs (angle-closure and open-angle)

194
Q

What medication is prescribed to prevent post-operative intraocular pressure associated with laser surgery?

A

Pilocarpine

195
Q

What medication is given to PTs w/ Xerostomia?

A

Pilocarpine
Post radiation therapy for head/neck tumor
Sjogren’s Syndrome (autoimmune disease destroys salivary/lacrimal glands)

196
Q

What are the adverse effects of Pilocarpine use?

A

Miosis

Decreased far vision

197
Q

What is the normal flow of aqueous humor through the eye? How is this inhibited?

A

Ciliary body to trabecular mesh work

Angle-closure: increased IOP from posterior chamber pushes iris against mesh work and closes ocular angle

198
Q

What is the mechanism of action for Bethanechol?

A

Cholinergic agonist increases bladder muscle tone causing detrusor muscle contractions and trigone sphincter relaxation increasing urination

199
Q

What is the clinical indication for Bethanechol?

A

Acute postoperative/postpartum non-obstructive urinary retention
Neurogenic atony of bladder w/ retention/ileus

200
Q

What are the contraindications for Bethanechol use?

A 
Physical obstruction of GI/GU
Bladder strength is questionable
Asthma
Peptic ulcer disease
Bradycardia
201
Q

What is the indirect action of acetylcholinesterase inhibitors?

A

Inhibit actetylcholinesterase from metabolizing Ach causing a prolonged effect

202
Q

What is the mechanism of action of Edrophonium?

A

Plant-derived reversible competitive Achesterase inhibitor that increases Ach potency by inhibiting the molecules destruction but is short lasting, 30sec-10m

203
Q

What is the clinical indication for using Endrophonium?

A

Tensilon Test for Myasthenia Gravis and adjunct for treatment
Evaluates emergency Myasthenia crisis
Used as curare antagonist to reverse non-depolarizing neuromuscular blocking agents

204
Q

What is an example of a medication that Edrophonium would not be useful using to treat?

A

Depolarizing neuromuscular agents

Succinylcholine chloride

205
Q

What is the contraindications for using Edrophonium?

A

GI/GU obstruction

Bladder wall strength is questionable

206
Q

What is the MOA for Physostigmine Salicylate

A

Plant derive competitive Achesterase inhibitor that potentiates its action by preventing destruction

207
Q

What is the clinical indication for Physostigmine Salicylate?

A

Reverse CNS effects of Achergics

Routine use is not recommended due to adverse effects

208
Q

What are the possible adverse effects of using Physostigmine Salicylate for routine use?

A

Delirium/agitation
Hallucinations
Hyperthermia
Supraventricular tachycardia

209
Q

What type of monitoring should be used for Physostigmine Salicylate?

A

ECG
Vitals
Seizures since it can cross BBB

210
Q

What are the contraindications for using Physostigmine Salicylate?

A

GI/GU obstruction
Bladder wall integrity is questioned
Respiratory distress/seizures

211
Q

What is the MOA for Neostigmine?

A

Synthetic competitive inhibitor that prolongs effect by preventing destruction

212
Q

What is the clinical indication for using Neostigmine?

A

Symptomatic treatment for Myasthenia Gracis

Reverses nondepolarizing neuromuscular agents

213
Q

What are the two formulations for Neostigmine?

A

N. Bromide- tablet

N. Methyl Sulfate- IV

214
Q

Why would the use of Neostigmine be preferred over Physostigmine?

A

More polar, does not cross CNS, no seizures

215
Q

PTs with what conditions should be warned before using Neostigmine?

A

Asthma
Peptic Ulcer
Bradycardia

216
Q

What are the contraindications for Neostigmine?

A

GI/GU obstruction

Bladder wall integrity is questioned

217
Q

What is the MOA for Pyridostigmine Bromide

218
Q

Pyridostigmine is preferred over neostigmine because?

A

Longer duration
Fewer GI symptoms
Allows for better transmission of impulses across neuromuscular junction

219
Q

What is the clinical indication for Pyridostigmine Bromide?

A

Myasthenia Gravis treatment
Reverses nondepolarizing neuromuscular blocking agents
Nerve agent pretreatment pyridostigmine

220
Q

Pyridostigmine Bromide has historically served as _______

A

Nerve Agent Pyridostigmine Pretreatment (NAPP)

221
Q

What are the cautions for using Pyridostigmine?

A

Peptic Ulcer
Bradycardia
Asthma

222
Q

What are the contraindications for Pyridostigmine Bromide?

A

GI/GU obstruction

Bladder wall integrity is questioned

223
Q

Most noncompetitive (irreversible) Ach inhibitors find their uses as what two things?

A

Insecticides

Nerve agents

224
Q

Increased Ach at the nicotinic receptors can lead to what issues?

A

Seizure
Coma
Cardiac arrhythmia
Respiratory arrest

225
Q

What are examples of Irreversible Acetylcholinesterase Inhibitors?

A

Ecothipoate- eye drops for glaucoma, target postganglionic ParaSymp junction
Sarin- mimics insecticides
Parathion- insecticide

226
Q

What is the MOA of Echothiophate Iodide?

A

ONLY noncompetitive Achesterase inhibitor used on a regular basis

227
Q

What is the effect of Echothiophate Iodide on the eye?

A

Contracts ciliary muscles to increase aqueous humor flow

228
Q

What are the adverse effects of using Echothiophate Iodide for glaucoma?

A 
Miosis
Decreased accommodation (far vision)
229
Q

What is the MOA of Pralidoxime?

A

Reactive cholinesterase (mainly outside of CNS) that were inactivated by phosphorylation from organophosphate pesticides

230
Q

What is the most critical part of Pralidoxime’s MOA?

A

Slows aging process of phosphorylated cholinesterase to non-reactive form
Reverses paralysis of respiratory muscles

231
Q

The use of Pralidoxime relieves what symptoms?

A

Salivation

Bronchospasm

232
Q

What is the form of Pralidoxime for chemical warfare?

A

ATNAA- reactive cholinesterase

233
Q

What are the clinical indications for using Pralidoxime?

A

Treat pesticide poisoning (nerve agents of organophosphate class)
OD of anticholinesterase drugs from treating myasthenia gravis

234
Q

What are the adverse effects of using Pralidoxime?

A

Anticholinergic effects: anticholinergic drug symptoms

235
Q

How do acetylcholine and acetycholinesterase interact?

A

Pos charge of acetylcholine attracted to ionic site of acetylcholinesterase
Hydrolysis catalyzed to form choline and acetic acid

236
Q

How do cholinesterase inhibitors and acetylcholinesterases react with each other?

A

Partial pos phosphorus attracted to partial neg serine
Nerve agent binds to serine hydroxyl group on achesterase
Prevent Ach from interacting with cholinesterase enzyme and being broken down

237
Q

How do Pralidoxime and Achesterase react with each other?

A

Pralidoximes N attracted to Ach neg charge
Pralidoxime removes Ach inhibitor
Achesterase regenerated

238
Q

_____ is the major neurotransmitter of the PNS

What other three areas is it seen in?

A

Ach

CNS, Symp/ParaSymp NS, Somatic NS

239
Q

How can the degeneration effects of Alzheimers be slows?

A

With drugs that increase Ach concentrations in CNS by inhibiting central Achesterase

240
Q

What are 4 drugs that could be used to increase Ach levels in Alzheimer’s PTs?

A

Tacrine- multiple doses/day, hepatotoxic
Donepezil- daily dose preferred
Galantamine- metabolized by CYP2D6/3A4
Rivastigmine- Patch form better tolerated

241
Q

Nicotine is an example of what type of stimulant?

A

Ganglionic

242
Q

What effects does Nicotine have at low doses? What effects a high dose?

A

Low- Depolarizes autonomic ganglia causing euphoria/arousal

High- blocks autonomic ganglia causing decreased BP and possible respiratory paralysis

243
Q

Where does a greater amount of nicotine absorption take place?

A

75% smoke held in mouth

95% smoke held in lungs

244
Q

Anticholinergic agents block Ach interaction with what type of receptors?

A

Muscarinic

Nicotinic

245
Q

Define M Receptor Antagonist

A

Antimuscarinic

246
Q

Define Nn receptor agonist?

Why is this not usually used?

A

Ganglionic blocker

Blocks both Symp/ParaSymp transmission

247
Q

Defein Nm receptor Agonist

A

Neuromuscluar/skeltal muscle blocking agent

248
Q

Anticholinergic agent effects are the opposite of ? stimulation

A

Cholinergic

249
Q

What is the saying for remembering the S/Sx of anticholinergic agents?

A

Blind as a bat, Mad as a hatter, Red as a beet, Hot as a hare, Dry as a bone,, Bowel/bladder lose their tone,
Heart runs alone

250
Q

What are the major therapeutic uses of Anti-Muscarinic agents?

A 
Reduce glandular/bronchiolar secretions before anesthesis
Induce sedation
Alleviate motion sickness
Reduces vagal stimulation
Ophthalmic mydriasis/cycloplegia
Reduce GI smooth muscle spasms
Treat bronchospasms
Control cholinergic agonist intoxication
Parkinson's Disease
251
Q

What are the contraindications for Anticholinergic Agent use?

A 
Narrow angle glaucoma
Angina
Alzheimers
Asthma
Diarhhea
Increased heat injuries
Myasthenia gravis
252
Q

What is the prototype anticholinergic?

253
Q

What are the Anticholinergics for the eye?

A

Cyclopentolate

Tropicamide

254
Q

What are the Anticholinergics for GI?

A

Dicyclomine

Belladonna Alkaloids

255
Q

What are the Anticholinergics for the lungs?

A

Ipratropium

Tiotropium

256
Q

What are the Anticholinergics for GU?

A 
Oxybutynin
Darifenacin
Solifenacin
Tolterodine
Fesoterodine
Trospium
257
Q

What are the Anticholinergics for Parkinsons?

A

Benztropine

Trihexyphenidyl

258
Q

What is the MOA of dopamine?

A

Inhibits muscarinic actions of Ach on post-gang cholinergic nerves

259
Q

Atropine is a ____ and _____ anticholinergic

A

Central

Peripheral

260
Q

What are the pharmacodynamic effects of atropine?

A

Reduces oral secretions
Relieves broncho constrictions/spasms
Stops vagal cardiac slowing/bradycardia
Asystole

261
Q

What are the clinical indications of atropine?

A

Mydriatic/cyclopegic diagnostic agent
Bradycardia
Relaxes upper GI
Cholinergic OD

262
Q

What has to be monitored during atropine administration?

A

HR
BP
Mental status

263
Q

What are the clinical uses for anticholinergics for the eye?

A

Diagnostic procedures requiring mydriasis and cyclopegia
Refractive measurement
Ophthalmoscopic exam of retina

264
Q

What is the MOA of anticholinergics for the eye?

A

Produces cycloplegia by paralyzing ciliary muscles
Loss of accommodation
Mydriasis by blocking parasympathetic tone

265
Q

What is the MOA of anticholinergics for GU use?

A

Dec bladder muscle tone causing detrusor muscle relaxation and sphincter constriction causing urinary retention

266
Q

What is the clinical indication for using anticholiinergics for GI use?

A

Overactive bladder w/ incontinence, urgency and frequency

267
Q

What are the adverse effects of using anticholinergics for GI use?

A

Dry mouth
Constipation
Site reaction/itching of patch

268
Q

Stopped on

IPAP (212 decks)

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