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APRN Pharmocology > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

Preclinical Stage of Drug Development

A

Identification and animal testing

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2
Q

Clinical Stage of Drug Development

A

Establish safety and effectiveness in humans

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3
Q

Phase I Clinical Trials

A

Healthy patients; safe dose and pharmacokinetics

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4
Q

Phase II Clinical Trials

A

Treat disease in small number of patients

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5
Q

Phase III Clinical Trials

A

Compare new drug to standard therapy in large number of patients

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6
Q

Graded Drug Response

A

Can be measured continually up to max response; e.g. numerics like BP or HR

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7
Q

Quantal Drug Response

A

Effect is either present or absent

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8
Q

Drug Potency

A

How much drug is required to produce a desired effect

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9
Q

Drug Efficacy

A

Maximum effect a drug can produce

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10
Q

Drug Selectivity

A

Ratio of desired response dose to dose that produces undesired effects

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11
Q

Therapeutic Index

A

Ratio of lethal dose to therapeutic dose of drug

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12
Q

Therapeutic Index of:

2 compared to 10

A

TI of 2 means double the therapeutic dose is lethal where TI of 10 means ten times the therapeutic dose is lethal

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13
Q

Ion Channel Receptors

A

Increase flow of Ions altering electric potential.
Rapid Onset and short duration
ACh; GABA; Excitatory AA

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14
Q

GPCR

A

Work through secondary messengers (cAMP, CA++, IP, DAG)
Available GPCR decreases when stimulated
Risk for rebound when drugs are d/c

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15
Q

Transmembrane Receptors

A

Hormone binding; phosphorylates tyrosine
Insulin

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16
Q

Partial Agonist

A

Bind to receptor sites but don’t activate every receptor
Max response is lower than full agonist

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17
Q

Bioavailability

A

Percentage of the administered drug that is absorbed into central circulation

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18
Q

Ion Trapping

A

Molecules exist as mixture of charged and uncharged ions depending on their pKa and the environmental pH
Only unionized molecules diffuse so an excess number of ionized drugs d/t pH will change distribution

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19
Q

Protein Binding

A

Can increase drug in circulation keeping the drug from working at an active site
Deranged physio like low albumin will change drug concentrations and needs to be accounted for

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20
Q

P-glycoprotein

A

Efflux transporter

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21
Q

MRP1

A

Efflux transporter

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22
Q

BRCA1

A

Efflux transporter

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23
Q

Phase 1 Metabolism

A

Redox reaction
CYP450
Can inactivate or activate a drug

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24
Q

Phase 2 Metabolism

A

Conjugation Reactions
Generally inactivate a drug and make it more hydrophilic for easy excretion

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25
Q

Breakdown CYP3A4*1

A

3-Family
A-Subfamily
4-Individual Enzyme
*1-Mutation from wild type

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26
Q

First-Order Metabolism

A

Fixed fraction of a drug is metabolized per hour
Half-life metabolism

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27
Q

Half-Life Metabolism

A

1st-50%
2nd-75%
3rd-87.5%
4th-93.75%
Drugs are usually dosed at their half life time

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28
Q

Zero Order Metabolism

A

Constant amount of drug is metabolized each hour

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29
Q

Enzyme Induction

A

Increased expression of drug metabolizing enzymes that can speed up or decrease metabolism.

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30
Q

Glomerular Filtration

A

Small unprotein bound drug molecules are filtered into lumen of nephron

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31
Q

Tubular Reabsorption and Secretion

A

Active and passive diffusion between the lumen of the nephron and the blood supply
Some drugs target active transporters here inhibiting movement of molecules

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32
Q

WHO’s 6 step model for drug prescribing

A

Define patient’s problem
Specify therapeutic objective
Choose treatment
Start Treatment
Educate the patient
Monitor Effectiveness

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33
Q

I Can PresCribE A Drug

A

Indication
Contraindications
Precautions
Cost/Compliance
Efficacy
Adverse effects
Dose/Duration/Direction

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34
Q

Legend Drugs

A

Contain “Federal law prohibits dispensing without a prescription” label

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35
Q

Schedule I

A

No Legal Use
Heroin, LSD, mescaline, Illegal Fentanyl

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36
Q

Schedule II

A

No Refills
Narcotics
Stimulants
Barbitals

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37
Q

Schedule III

A

Max 5 refills or 6 months
Narcotics mixed with nonnarcotics
Steroids, testosterone

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38
Q

Schedule IV

A

Benzodiazepines

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39
Q

Schedule V

A

Loperamide
Cough medications

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40
Q

Pharmacological ADR

A

Intrinsic; Predictable based on MOA

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41
Q

Idiosyncratic ADR

A

Unpredictable;
Can be Immune response, receptor mutation, drug-drug, biological system variation

42
Q

Hapten Hypothesis

A

Drugs are LMW molecules that can bind to a protein causing an individuals metabolic pattern to generate reactive metabolites that elicit a reaction

43
Q

Type I Immune ADR

A

IgE mediated; immediate hypersensitivity

44
Q

Type II Immune ADR

A

Antibody dependent cytotoxicity
E.g. Drug induced thrombocytopenia

45
Q

Type III Immune ADR

A

Immune complex hypersensitivity; IgG and IgM; Week or longer
Arthus reaction to Td Vaccine presents as severe vasculitis

46
Q

Type IV ADR

A

Delayed type hypersensitivity; Not antibody mediated; Contact dermatitis

47
Q

Rapid Reaction ADR

A

Immediately after med admin

48
Q

First dose ADR

A

Reaction is unlikely to persist with repeated exposure

49
Q

Early ADR

A

Develop early and generally do not require discontinuation
Slow drug titration can help

50
Q

Intermediate ADR

A

Occur after repeated exposures

51
Q

Late ADR

A

Prolonged exposure; generally predictable as known side effect of medications

52
Q

Genetic Polymorphism

A

Differences of a DNA sequence found in at least 1% of the population

53
Q

Genomics

A

Study of the complete set of genetic information present in an organism

54
Q

Pharmacogenomics

A

Study of the genetic differences between people and the impact that has on the response to pharmaceuticals

55
Q

Poor Metabolizers

A

Lack a working enzyme

56
Q

Intermediate Metabolizers

A

Heterogenous for one working wild type allele and one variant allele

57
Q

Extensive Metabolizers

A

Two standard functioning alleles

58
Q

Ultrarapid Metabolizers

A

More than one functioning copy of a given enzyme

59
Q

CYP2D6 and Codeine

A

CYP2D6 converts prodrug codeine into active metabolite morphine.
PM and UM may receive no benefit from codeine due to either not metabolizing it to active form or metabolizing too quickly

60
Q

CYP2C9 and Warfarin

A

*2 and *3 are PM and resulted in reduced maintenance dosing requirements

61
Q

Herbal Remedies for GI Disorders

A

Caraway
Carob
Psyllium
Senna
Triphala

62
Q

Herbal Immune Boosters

A

Echinacea
Ginseng

63
Q

Herbals For Men’s Health

A

Ashwagandha
Gokshura
Hory Goat Weed
Maca
Saw Palmetto
Yohimbine

64
Q

Herbals for Women’s Heatlh

A

Cranberry
Dong Quai
Raspberry
Shatavari

65
Q

Herbals for Mental Health

A

DHEA
Ginkgo
Kava
Melatonin
SAM-e
St John’s Wort
Valerian

66
Q

Herbals for Pain

A

Chondroitin
Feverfew
Turmeric
While Willow Bark
Wintergreen

67
Q

Entheogens

A

Psychedelics

68
Q

Direct Cost

A

Directly attributed to the disease in question

69
Q

Indirect Cost

A

Costs associated with loss of function or premature death d/t disease

70
Q

Intangible Cost

A

Value place on QOL

71
Q

Cost-Minimization

A

Outcome is clinically identical

72
Q

Cost-effectiveness

A

Different clinical outcome
Justifying of increased cost for incremental outcome improvements

73
Q

Cost-benefit

A

Expressing clinical outcome in monetary units

74
Q

Cost-Utility

A

Cost of treatment compared to outcome of QALY. Year at full health is 1 QALY

Quality adjusted life years

75
Q

____ increases peristaltic action of the lower bowel. Can be overused and create dependency

A

Senna

76
Q

____ used to support the immune system, brain function, and memory

A

Lion’s Mane

77
Q

____ Ayurvedic herb known to increase stamina, libido, and sexual function in men

A

Gokshura

78
Q

____ is a Peruvian herb used to improve sexual behavior

A

Maca

79
Q

____ is known to decrease symptoms of an enlarged prostate due to benign prostatic hyperplasia

A

Saw Palmetto

80
Q

____ is generally believed to enhance the central sexual impulse by blocking the alpha-2 adrenoceptors in the locus coeruleus in the brain

A

Yohimbe

81
Q

____ relieve symptoms of menstrual pain, premenstrual syndrome, infrequent periods, recovery from childbirth, menopause, and fatigue/low vitality

A

Dong Quai

82
Q

Raspberry Leaf

A

Relieves morning sickness and uterine relaxant

83
Q

____ is believed to stimulate prostaglandin synthesis and thereby cause vasodilation, increasing tissue perfusion and cerebral blood flow. It reduces platelet-activating factor and erythrocyte aggregation, it should not be taken with anticoagulants or antiplatelet medications.

A

Ginkgo

84
Q

____ used to treat anxiety disorders, fatigue, and insomnia. Like benzodiazepines, ____ has been used in the treatment of seizure activity and for sedation

A

Kava

85
Q

Kava is used to treat ____, ____ , and ____ . Like benzodiazepines, Kava has been used in the treatment of seizure activity and for sedation

A

Anxiety, fatigue, insomnia

86
Q

____ has drug interactions with SSRIs, cyclosporins, BC pills, antidepressants, warfarin, oxycodone and digoxin

A

St John’s Wort

87
Q

____ is extracted from the cartilage of cow trachea and is often combined with glucosamine for the treatment of pain. May potentiate anticoagulants.

A

Chondroitin

88
Q

____ is used most often to treat headache and migraines. It has also been used for toothache, joint pain, asthma, stomachache, menstrual problems, and threatening miscarriage. The assumed mechanism of action is the inhibition of ____ release from platelets

A

Feverfew; Serotonin

89
Q

Feverfew most common adverse reactions were mouth ulcerations, hypersensitivity, and a ____ characterized by moderate to severe pain and joint and muscle stiffness

A

Withdrawal syndrome

90
Q

____ is often combined with chondroitin for the treatment of OA and is thought to stimulate cartilage production and enhance rebuilding of damaged cartilage.

A

Glucosamine

91
Q

____ promising effects have been observed in patients with various pro-inflammatory diseases. Reduced GI effects compared to ____

A

Turmeric; NSAIDs

92
Q

____ has been used for thousands of years as an anti-inflammatory, antipyretic, and analgesic. Has been associated with downregulation of inflammatory mediators

A

White Willow bark

93
Q

____ thought effective in relieving pain from muscle strains, inflamed muscles, ligaments, and joints. Overgenerous application can result in ____ poisoning from absorption into the bloodstream. Patients who are allergic to aspirin or who are taking ____ should not use it.

A

Wintergreen Oil; salicylate; anticoagulants

94
Q

____ can be used for indigestion, flatulence, constipation, and menstrual cramps

A

Caraway

95
Q

____ is often used in combination with a hydrating solution such as Pedialyte to treat diarrhea

A

Carob Powder

96
Q

____ has traditionally been used to treat GI disorders and restore bowel health. A 2007 study evaluated the inhibitory activities of ____ against common bacterial isolates from patients with HIV and supported antibacterial activity by triphala against the isolates

A

Triphala

97
Q

____ has been traditionally used as a general tonic and adaptogen, to improve one’s resistance to adverse conditions and enhance internal induction, phagocytosis, and natural killer, B, and T cells.

A

Ginseng

98
Q

___ is used to strengthen the immune system, enhance stamina, and improve libido. ___ found to have a GABA-mimetic effect and shown to promote formation of dendrites

A

Ashwagandha

99
Q

___ improves fertility and increases sexual drive. Symptoms of tachyarrhythmias, aggressive behavior, and irritability have been noted in older patients

A

Horny Goat Weed

100
Q

Evidence does support the benefit of ___ use in patients with adrenal insufficiency; Patients with ___-sensitive cancers should be discouraged from using ___, as should pregnant and breastfeeding women.

A

DHEA; hormone; DHEA

101
Q

___ is a chemical found naturally in the body produced from methionine, an amino acid found in foods. Used as antidepressant; some cases of mania have been reported in patients with bipolar disorder

A

SAME-e

102
Q

___ seems to inhibit uptake and increase presynaptic release of GABA; however, it is not readily absorbed, is highly unstable, and quickly decomposes. Suggested for anxiety restlessness, and difficulty getting to sleep.

A

Valerian

APRN Pharmocology (5 decks)

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