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NR 565 Pharmacology Week 1 Study Notes
1. Pharmacokinetics: The study of drug absorption, distribution, metabolism, and excretion in
the body "What the body does to the drug"
2. Factors that affect drug absorption (5): Rate of dissolution Surface area
Blood flow Lipid solubility PH partitioning
3. Factors that affect drug distribution (4): Blood flow to tissues Ability to exit
vascular system Blood-brain barrier Protein- binding capacity
4. Pharmacodynamics: The study of biochemical and physiologic effects of drugs on the body
and the molecular mechanisms by which those effects are produced "What the body does to the drug"
5. Phamacodynamics: 3 mechanisms of action: Receptor Enzyme
Non-selective interactions (i.e. chemo)
6. Types of drug therapy (7): Acute
Maintenance (HTN/bc) Supplemental (insulin) Palliative Supportive (IV fluid) Prophylactic Empirical (broad-spectrum abx)
7. Idiosyncratic Effect: Unexpected response to medication
8. Tolerance: Declining response to a drug
9. Dependence: Physiological/psychological need for a drug; needs drug for normal function
10. Addiction: Compulsive use of a drug despite negative/dangerous effects
11. Drug interactions: drug-drug: When 2 drugs compete for metabolizing en- zymes
12. Drug interactions: food-drug: Grapefruit juice or leafy greens
13. Drug interactions: additive: 1+1 = 2; both provide intended effect
14. Drug interactions: antagonistic: 1+1 = <2; less than desired effect of one or both drugs
15. Drug interactions: synergistic: 1+1 = >2; sum total effect is greater than if given alone
(i.e. lisinopril + HCTZ)
34. Duration: Length of time drug remains active; measured from therapeutic level to when
elimination decreases level below therapeutic range
35. Absorption: The movement into the bloodstream for distribution
36. Bioavailability: The extent to which a medication can be absorbed
37. Absorption: enteral: GI tract > bloodstream > liver = 1st pass effect
38. Causes of decreased enteral absorption: Bariatric surgery (decreased sur- face area)
Vigorous activity (blood shunted away from GI tract) Age (decreased motility)
39. Parenteral medications: No 1st pass effect; 100% available as they enter the bloodstream
40. Topical medication administration sites: Skin, eyes, ears, nose, rectum, vagi- na
41. Purpose of topical medication application: Intended for action at the site of application
42. Transdermal medications: intention: Internal effect
43. Transdermal medications: absorption: Carried through skin to bloodstream; no 1st pass
effect
44. Transdermal medications: sites: Rotate sites to prevent irritation Trunk or
upper extremities with good circulation Avoid scar tissue due to decreased absorption
45. Inhaled medications: Intented for lungs and/or other areas of the body
46. Distribution: transport: Most rapid in areas with high blood flow (major organs) Slower to fat,
skin, and muscles (increased by physical activity)
47. Distribution: elimination: Occurs primarily in the liver and kidneys Watch for
renal/liver toxicity
48. Distribution: decreased albumin: Can increase risk of toxicity in burns, star- vation, negative
nitrogen balance
49. Metabolism: When a substance is irreversibly transformed into metabolites
50. Excretion: Elimination of a substance from the body
51. Agonist: A drug that binds to and activates a receptor
52. Agonist: full: High efficacy, full response
53. Agonist: partial: Lower efficacy, sub-maximal activation when occupying all receptors
54. Agonist: inverse: Produces opposite effect yet binds to the same receptors as agonist
55. Silent antagonist: Neutral antagonist Attenuates/weakens
effects of agonists/inverse agonists Produces functional reduction in signal transduction No intrinsic activity itself
56. Antagonist: Attenuates/weakens effects of an agonist
57. Antagonist: competitive: Binds to same receptors without activation, blocking action of
agonist
58. Antagonist: non-competitive: Binds to allosteric (non-agonist) receptor site to prevent
activation
59. Antagonist: reversible: Binds non-covalently; can be washed out
60. Antagonist: irreversible: Binds covalently; cannot be displaced by competing ligands or
washing
61. Efficacy: How agonists vary in produced response when occupying the same number of
receptors
62. High efficacy: Maximum response, occupying low number of receptors
63. Low efficacy: Cannot produce maximum response, occupies more receptors
64. Therapeutic window: Amount of medication that gives desired effect vs amount that produces
more adverse than desired effects
65. B Max: Maximum amount of drug/radioligand that can bind specifically to recep- tors in a
membrane preparation Used to measure density of receptor site
66. Potency: Concentration of a drug at which it is effective
67. Mechanism of Action (MOA): Specific biochemical interaction through which a drug produces
82. Understanding substrates, inhibitors, and induces is crucial when pre- scribing :
Medications for seizures, depression, and psychosis
83. Inhibitors: Medications that inhibit metabolic activity of one or more CYP450 enzymes
Slows/blocks enzyme's metabolic activity that other medications are dependent on
84. Dangers of inhibitors: Can cause increased levels of other meds, prolonged
pharmacological effect, and potential toxicity
85. Inhibitors: VISA CK GQ: Valproate
Isoniazid Sulfonamides Amiodarone Chloramphenicol Ketoconazole Grapefruit Quinidine
86. Inducers: Xenobiotics (medications and environmental agents) that elevate CYP
enzyme activity by increasing enzyme synthesis Additional sites for biotransformation = increased medication metabolism
87. Rifampin: Inducer with short half-life
88. Phenobarbital: Inducer with long half-life
89. Carbamazepine: Potent inducer; metabolized by the same CYP450 enzyme it induces
Start at low dose, increase weekly due to steady decrease in half-life over time
90. Inducers: CRAP GPS: Carbamazepine Rifampin
Alcohol Phenytoin Griseofulvin Phenobarbital Sulfonylureas
91. Prescribing medications during pregnancy/breastfeeding: Physiological changes to the body
can change pharmacodynamic/pharmacokinetic properties of drugs
92. Changes in pregnancy: kidneys: increased GFR = increased drug excretion
93. Changes in pregnancy: liver: Increased hepatic metabolism of some drugs
94. Changes in pregnancy: bowel: Decreased tone and mobility Increased
drug absorption
95. Teratogenesis (prenatal toxicity): Structural or functional birth defects Intrauterine
growth retardation Fetal death
96. Teratogens: Antiepileptic drugs
Tetracyclines Fluoroquinolones Vitamin A in large doses (accutane) Anticoagulants Hormones (diesthylstilbestrol) Alcohol Cocaine
97. Infant/pediatric prescribing: Infants/peds don't process medications the same as adults
Dosage is based on weight or body surface area
98. Infant/pediatric prescribing: IM: Neonates: slow and erratic due to decreased blood flow in
muscles Infancy: increased absorption due to increased blood flow
99. Infant/pediatric prescribing: Transdermal: Thin skin = increased blood flow Increased
absorption Increased risk of toxicity from topical drugs
100. Infant/pediatric prescribing: oral administration: Decreased gastric empty- ing
Increased absorption for stomach-absorbing drugs Decreased absorption for intestine-absorbing drugs Decreased gastric acidity for 24 hours after birth Increased absorption of acid-labile drugs
101. Children younger than 2 have : Markedly faster
absorption
physician oversight
113. Reduced-practice scope: NP is limited in at least one element of practice Must
have formal collaborative agreement with an outside health discipline to provide care
114. Restricted-practice scope: NP requires supervision, delegation, or team
management by outside health discipline to provide care
115. NP fiscal and ethical implications: Adherence to ethical guidelines to protect patients
from harm
116. Ethical prescribing: NP considers mechanism of action, efficacy, safety, and number
of medications
117. Decision making to maintain safety and reduce liability: Provider-patient relationship
H+p on file Discussion of risk factors, side effects, or alternative options Drug monitoring or titration plan if applicable Consultation documentation Avoiding prescribing for self, family, or friends
118. Prescribing considerations for the patient: Cost
Guidelines Availability Interactions Side effects Allergies Hepatic/renal function Need for monitoring Special populations (pregnant, nursing, older adults)
119. 14 key elements of presciption composition: Prescriber contact information Prescriber
name License # (NPI) DEA# (controlled substances) Patient name Allergies
DOB
Medication name Medication strength Quantity Indication Directions-dose and frequency Refills Signature
120. Prescriptions: phone: Convenient
Must contain all elements Schedule II cannot be prescribed or refilled by this method
121. Prescriptions: e-script: Widely accepted
Quick and easy transfer to pharmacy Minimizes errors DEA scheduled drugs can't be ordered electronically
122. Prescriptions: written: Must contain all elements May
have pre-populated info Legible writing Ink Avoid error-prone abbreviations Never sign a blank RX Use tamper-resistant RX
123. Prescriptions: refills: Considered needed monitoring
124. 3 aims of drug monitoring: 1. Therapeutic dosage determination
2.Evaluating adequacy of medication
3.Identifying adverse effects
- Black-box warnings: When a medication is found to have serious/life-threat- ening risks Still eligible for prescription