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Vuck Path/Pharm Test 1
Path/Pharm Test 1
107
Pharmacology
Professional
01/17/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Acetylcholine
Definition
Employed at most unctions of the peripheral nervous system
Term
Norepinephrine
Definition
Released by most postganglionic neurons
Term
Epinephrine
Definition
Released by the adrenal medulla
Term
Cholinergic receptors
Definition
One of 2 basic categories of receptors of the peripheral nervous system; mediated by Ach
Term
Adrenergic receptor
Definition
One of 2 basic categories of receptors of the peripheral nervous system; mediated by epi and NE
Term
Nicotinic N
Nicotinic M
Muscarinic
Definition
Subtypes of cholinergic receptors (Ach)
Term
Alpha 1
Alpha 2
Beta 1
Beta 2
Dopamine
Definition
Subtypes of adrenergic receptors (NE, Epi)
Term
Fig 13-6: Locations of cholinergic and adrenergic receptor subtypes
Definition
NicotinicN receptors are located on the cell bodies of all postganglionic neurons of the parasympathetic and sympathetic nervous systems. NicotinicN receptors are also located on cells of the adrenal medulla.
2. NicotinicM receptors are located on skeletal muscle.
3. Muscarinic receptors are located on all organs regulated by the parasympathetic nervous system (ie., organs innervated by postganglionic parasympathetic nerves). Muscarinic receptors are also located on sweat glands.
4. Adrenergic receptors—alpha, beta, or both—are located on all organs (except sweat glands) regulated by the sympathetic nervous system (ie, organs innervated by postganglionic sympathetic nerves). Adrenergic receptors are also located on organs regulated by epinephrine released from the adrenal medulla.
Term
Autonomic tone
Definition
Only one division provides basal control to organ.
Most organs – predominant tone is PNS.
During emergency– predominant tone is SNS.
Term
Parasympathetic ______ heart rate.
Sympathetic ________ heart rate.
Definition
P: Slows
S: Accelerates
Term
3 principle functions of ANS
Definition
1. Regulate the heart

2. Regulate secretory glands (salivary, gastric, sweat, and bronchial)

3. Regulate smooth muscles (bronchi, blood vessels, urogenital system, and GI tract
Term
Cholinergic NMJ
Definition
[image]
Term
Adrenergic Neuromuscular Junctions
Definition
Term
Disease-producing cellular stresses
Definition
7: hypoxia or ischemia, chemical injury, physical agents, infection, immune reaction, nutritional imbalance, genetic derangements
Term
5 Adaptive responses that help cells survive and maintain function
Definition
Normal
Atrophy: decreased cell size
Hypertrophy: increased cell size
Hyperplasia: increased cell number
Metaplasia: conversion of one cell type to another
Dysplasia: disorderly growth
Term
Molecular targets of cell injury
Definition
1. Cell membrane integrity: Calcium
2. Energy metabolism: Aerobic respiration and ATP production: Reactive Oxygen Species (ROS)
3. Protein synthesis
4. Genes
Term
2 types of reversible cell injury
Definition
1. Hydropic swelling
2. Intracellular accumulation (bruise)
Term

Mechanisms of Cellular Accumulation

Copstead p. 67: Fig. 4-02

Definition
[image]
Term
Chaperone proteins
Definition
Roles  of chaperone proteins in protein refolding and ubiquitin in protein degradation after stress-induced protein damage.
This is how the body repairs aberrant proteins when they’re damaged. What if you don’t have a chaperone protein? (ex. Cystic fibrosis)
Term
2 Types of irreversible cell injury
Definition
1. Necrosis: coagulative, liquefactive, fat, caseous
2. Apoptosis
Term
Ischemia
Definition
Decrease in blood flow
Term
Eschar
Definition
Black, dead tissue
Term

Loss of Cell Membrane Integrity

 

cellular injury as a consequence of intracellular calcium overload

Definition
[image]
Term
Apoptosis vs Necrosis
Definition
[image]
Term
2 Converging Pathways for Apoptosis
Definition
1.Turned on by pathway in mitochondria
2.Death receptor pathway

Drugs target pathways.
Term
ROS
Definition

Reactive Oxygen Species: There are stressors which cause oxygen to have an electron attached to it and hang around as free radicals.  

 

Term
Hypoxia vs Ischemia
Definition
[image]
Term
Ischemia Reperfusion Injury
Definition
[image]
Term
Reperfusion injury & stroke
Definition

Cellular edema in stroke patients kills patient.  Brain swells, has nowhere to go, goes through foramen, herniates and dies. 

Term
Other types of cellular injury
Definition
[image]
Term
Programmed senescence theory
Definition

Telomeres are the end caps of chromosomes. They serve to keep the contents of the chromosome in place. Shortening of the telomere is associated with aging and cancer. Telomerase is the enzyme which repairs the telomere. Only certain cell types have telomerase such as germ cells (sperm and ova) and stem cells.

Term

Physiologic changes of aging

p. 83: Table 4-5

 

Definition
Age-related decrease in functional reserve
Inability to adapt to environmental demand
Somatic death
Term
Cell Injury Summary Diagram
Definition
[image]
Term
Signal transduction
Definition
Most often Chemical messengers exert their effects by binding to membrane receptors (proteins) that convert the chemical signal into signals within a cell.
Term
5 Membrane transport types
Definition
Endocytosis, exocytosis (macromolecules)
Electrochemical gradient (ions)
Active transport pumps (Na-K pump; membrane Ca transporters; ABC transporters)
Transport carriers (Na driven; Passive transport carriers;
Channel proteins (integral)
Term
Endocytosis
Definition
receptor-->vesicle-->endosome-->free cholesterol (for example)-->receptor back to cell surface
Term
Na-K pump
Definition
Three Na+ ions bind to sodium-binding sites on the carrier's inner face. At the same time an energy-containing adenosine triphosphate (ATP) molecule produced by the cell's mitochondria binds to the carrier. The ATP breaks apart, transferring its stored energy to the carrier. The carrier then changes shape, releases the three Na+ ions to the outside of the cell, and attracts two K+ ions to its potassium-binding sites. The carrier then returns to its original shape, releasing the two K+ ions and the remnant of the ATP molecule to the inside of the cell. The carrier is now ready for another pumping cycle.
Term
Passive Transport
Definition
Ex: Insulin
receptor-->transport protein translocates to cell surface to grab insulin
Term
Action Potentials
Definition
Always a resting cell membrane which changes. Depolarization is the response to the signal-->contraction. Mediated by voltage-gated ion channels. Triggered by binding of NT which opens the channels.
Term
High or low potassium levels can cause
Definition
arrhythmias, because cell’s ability to respond is different because ion levels off.
Term
3 possible states of voltage-gated sodium channel
Definition
Open--gate open, channel open
Refractory--gate closed, channel open
Closed--gate closed, channel closed
Term
Plasma membrane (cell surface) receptors
Definition
voltage gated (ion channel): activated by NT
ligand-gated (enzyme coupled): activated by ligand (hormone)
G-protein receptors
mechanically-gated: activated by physical compression
other receptors (metaboreceptors)
Term
Cellular communication. 3 primary ways to maintain homeostasis.
Definition
1. Remote by Secreted Molecules: Use receptor proteins inside the target cell and the signal molecule has to
enter the cell to bind to them
2. Direct by Surface Molecules: Display plasma-bound signaling molecules (receptors) that affect the cell itself
and other cells in direct physical contact
3. Direct via Gap Junctions: Form protein channels (gap junctions) that directly coordinate the activities of
adjacent cells
Term
Overview of Signal Transduction
Definition
[image]
Term
Homeostasis
Definition
a state in which all symptoms are in balance at an ideal “set point” despite alterations within the body
Term
Allostasis
Definition
activity necessary to maintain or re-establish homeostasis (several levels)
Carried out by a set of systems that support homeostasis in light of environmental and lifestyle changes
Term
Stress
Definition
Demands that require constant psychological, behavioral and physiological adjustment
Hans Selye 1930s
Term
Stressors: 4 types
Definition
1. psychological (anxiety, worry)
2. environmental (natural disasters)
3. physical (exercise, trauma, illness)
4. immunological (infection, physical illness)
Term
Stressors
Definition
agents or conditions that can produce stress and endanger homeostasis
Term
Risk factors
Definition
not stressors, but conditions or situations that increase the likelihood of encountering a stressor

Modifiable (diet) or non-modifiable (gender, genetic)
Term
Response to Stressors
Definition
Adaptation
Coping
Illness
Term
Allostatic overload
Definition
inadequate adaptation mechanisms or overwhelming allostatic load
inability to maintain homeostasis
Term
Distress
Definition
perceived inability to cope with a stressor
Term
Adaptation
Definition
biopsychosocial process of change in response to new or altered circumstances, internal or external in origin
Term
Coping
Definition
behavioral adaptive response to a stressor using culturally based coping mechanisms
Term
Human Function Curve
Definition
[image]
Term
GAS
Definition
General adaptation syndrome
Term
3 Phases of GAS
Definition
1. Alarm reaction:
fight-or-flight response due to stressful stimulus
Allostatic state: Refers to the activity of various systems in attempting to restore homeostasis
2. Stage of resistance:
The activity of the nervous and endocrine systems in returning the body to homeostasis
3. Stage of exhaustion:
point where body can no longer return to homeostasis
Allostatic overload: “cost” of body’s organs and tissues for an excessive or ineffectively regulated allostatic response
Term
Stress Feedback Loop
Definition
[image]
Term
Feedback Response
Definition
[image]
Term
Stress & Illness
Definition
[image]
Term
Simplified HPA axis Activation
Definition
[image]
Term
Sympathetic vs Parasympathetic
Definition
Sympathetic revs things up: parasympathetic might inhibit. Autonomic nervous system is kind of a 4-way street.

Sympathetic turns on, increases, turn off, decreases. Parasympathetic turns on, decreases, turns off, increases. Important to really understand autonomic nervous system for beta blockers, etc.
Term
Catecholamines as neurohormonal mediators of stress and adaptation
Definition
norepinephrine and epinephrine
Play an integral role in allostasis
Sympathico-adrenal system response mediates the flight-or-fight response
Term
Adrenocortical steroids as neurohormonal mediators of stress and adaptation
Definition
cortisol and aldosterone
Critical to maintenance of homeostasis
May synergize or antagonize effects of catecholamines
Term
Endorphins and enkephalins
Definition
endogenous opioids (body’s natural pain relievers)
Raise pain threshold; produce sedation and euphoria
Term
Immune cytokines (e.g., interleukin-1 IL-1)
Definition
secreted by macrophages during stress response
Enhance immune system response
Term
Consequences of Drug-Drug Interactions
Definition
Intensification of effects
Increased therapeutic effects
Increased adverse effects

Reduction of effects
Reduced therapeutic effects
Reduced adverse effects

Creation of a unique response
Term
4 basic mechanisms of drug-drug interactions
Definition
1. Direct chemical/physical interaction (IV precipitation)
2. Pharmacokinetic interaction (induce vomiting)
3. Pharmacodynamic interaction (inhibitory)
4. Combined toxicity
Term
Risk for serious drug interaction is directly proportional to
Definition
the number of drugs a patient is taking.
Term
Adverse drug reaction
Definition
any noxious, unintended, undesired effect that occurs at a normal drug dose; Elderly and very young
Term
8 Types of Adverse Drug Reactions
Definition
Side effect (recognized during trials, expected)
Toxicity
Allergic reaction- immune
Idiosyncratic effect (weird, rare)
Iatrogenic disease (worsens/causes a disease)
Physical dependence-body adapts to drug exposure
Carcinogenic
Teratagenic (cause mutations)
Term
4 pregnancy risk categories
Definition
1: tested totally safe (there are none)
2: no cause for concern
3: cause for concern
4: known harm--drug of last resort
4
Term
Pediatrics and Drugs
Definition
Variation from neonate to
toddler to adolescent
Neonates/BBB
Protein stores
Dose based on body surface area (BSA)
chart
Children > 1yr similar to adults but metabolize drugs faster
Route of administration varies
Term
Geriatrics and Drugs
Definition
Absorption (not much change)
Distribution
Protein (albumin)
Fat (increased)
Water
Metabolism
hepatic
Excretion
renal
Term
Copstead p. 83
Definition
X
Term
Drug Development Cycle
Definition
Phase 1 – toxicity; studied in healthy people; huge numbers
Phase 2 – efficacy and dosing; appropriate dose to achieve effect
Phase 3 – does this work in the population that has the disease we’re interested in? Can now apply for patent and use.
Phase 4 – post-marketing surveillance; all healthcare workers are part of surveillance—adverse effects must be reported

Off-label use is somewhat common; ex. Viagra used for heart disease was re-approved for heart disease and marketed under a different label.
Term
Ideal Drug (doesn't exist)
Definition
Effective
Safe
Predictable
Reversible
Affordable
Term
Pharmacokinetics Chart
Definition
[image]
Term
Pharmacodynamics: Dose Response Curves
Definition
[image]
Term
Receptor Theory
Definition
[image]
Term
Clinical application of pharmacodynamics (4)
Definition
Educate patients about their medications
Make PRN decisions (pain, nausea, temp)
Evaluate patients for drug responses (both beneficial and harmful)
Collaborate with physicians about drug therapy
Term
Maximal efficacy
Definition
The largest effect that a drug can produce (height of the curve; see Figure 5-2, A).
Term
4 Drug mechanisms of action
Definition
ion, g-protein, tyrosine, transport to nucleus to activate transcription (this will take a long time)
Term
Properties of receptors: Drugs can only
Definition
Mimic or block the body's own regulatory molecules
Term
4 Primary receptor families
Definition
1, Cell membrane–embedded enzyme.
2, Ligand-gated ion channel.
3, G protein–coupled
receptor system (G = G protein).
4, Transcription factor.
Term
Simple occupancy theory
Definition
Intensity of drug response = # of occupied receptors
Term
Intrinsic activity
Definition
Ability of the drug to activate a receptor upon binding
measure of the ability of a drug once bound to the receptor to generate an effect activating stimulus and producing a change in cellular activity.
Term
Dobutamine
Definition
Mimics NE at cardiac receptors
Term
Agonists _____ receptors.
Definition
activate
Term
Antagonists
Definition
block receptor activation by endogenous regulatory molecules and drugs; they have affinity but no intrinsic activity
blockers
Term
Partial agonists
Definition
Agonists that have only a moderate intrinsic activity.
The maximal effect that a partial agonist can produce is less than that of a full agonist.
Can act as antagonists as well as agonists.
Term
Regulation of receptor sensitivity
Definition
[image]
Term
Receptorless drugs
Definition
Antacids, antiseptics, saline laxatives, chelating agents
Term
Therapeutic Index
Definition
Larger/higher = safer drug
LD50/ED50 = lethal/effective
Term
2 Goals in the clinical application of drug therapy:
Definition
Maximize beneficial effects and minimize harm
Patient safety
Term
P-glycoprotein
Definition
transmembrane protein that transports a wide variety of drugs out of cells
Term
Ions: 3 ways they can be used to target drugs
Definition
1. quaternary ammonium compounods: N and always +
2. pH-dependent ionization: ionize in opposite pH
3. ion trapping (pH partitioning): accumulate on opposite side
Term
ASA
Definition
acetylsalicylic acid
Term
3 factors of drug distribution
Definition
Blood flow to tissues (tumors/abcess)
Exiting the vascular system
Entering cells
Term
Normal cardiac output
Definition
An average resting cardiac output would be 5.6 L/min for a human male and 4.9 L/min for a female.
Term
Only drugs that are ______ or have a ___________ can cross the BBB to a significant degree
Definition
lipid soluble
transport system
due to tight junctions
Term
Protein-binding
Definition
limits free drug available
albumin
Term
Induction
Definition
more enzymes available; ↑ drug metabolism;
CYP450 enzyme system
Term
Inhibition
Definition
less enzymes available;  drug metabolism
CYP450
Term
Renal drug excretion
Definition
Filtrations: drugs from blood to urine (unless protein bound)
Passive Reabsorption: Lipid sol back to blood; polar and ionized stay in urine
Active transport: organic acids and based blood to urine
Secretion
Term
Two plasma drug levels defined
Definition
Minimum effective concentration
Toxic concentration
Therapeutic range
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