Pharm 1: Block 1 Flashcards
1
Q
Define Prescription
A
Prescriber’s order for a specific patient
2
Q
Define “Sig”
A
Signetur
“let it be labeled”
3
Q
What are the two safety categories of prescriptions
A
Legend- federal requires Rx for drug prescription
OTC- considered safe for self-administration
4
Q
FDA determines if a drug should be a legend or OTC based on what?
A
Safety Consideration
5
Q
Who controls and monitors drugs considered to have abusive potentials?
A
DEA
6
Q
Who approves what indications a drugs is used for?
A
FDA
7
Q
Define Labeled Use
A
FDA approved a New Drug Authorization saying drug is safe/effective for an indication
8
Q
Define Unlabeled Use
A
Use of a medication for an indication that has not been approved by the FDA
9
Q
What is the generic name for Neurontin?
A
Gabapentin
10
Q
PAs may be privileged to write Rxs for medication that have been approved and recommended by whom?
A
Pharmacy and Therapeutics Committee
11
Q
What is the military’s Rx form number?
A
DD 1289
12
Q
Rxs for children 12 y/o and younger need to include what other two pieces of info?
A
Age
Weight
13
Q
What are the 4 drug name/classifications?
A
Chemical Name
Drug Name- Trade/Brand, Generic
Pharmacotherapeutic Class
Target Physiologic System
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
15
Q
DoD allows a __ day supply for a maintenance medication
A
90 days
16
Q
How many refills are allowed for Schedules 2-5?
A
2: None
3-5: 5 x in 6mon, what ever happens first
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
18
Q
What are 4 factors that encourage PT noncompliance?
A
Asymptomatic
Inc frequency
Direction difficulty
Side effects
19
Q
Define ASA
Define ATC
A
Aspirin
Around the clock
20
Q
Define HA
Define HTN
Define HOTN
A
Headache
Hypertension
Hypotension
21
Q
Slide 24 25 26 27
A
Abbreviations
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
23
Q
Define Allergic Reaction
A
Immunologic hypersensitivity that occurs after medication use where the drug acts as an Ag in the body
24
Q
Define Idiosyncratic Reaction
A
Abnormal susceptibility to a medication that is peculiar to an individual
Antihistamine causing excitement instead of sedation
25
Who classifies/categorizes controlled substances?
DoJ
| DEA- Office of Diversion Control, Title 21 USC CSA
26
What are the limitations/regulations on filling a Schedule II Rx?
No Federal limit on quantity, limited by State/local law
90 day limit for matinenance
No federal time limit to fill
No refills
27
What happens if a pharmacist fills a Schedule II drug in an emergency situation?
May dispense quantity to adequately treat PT during emergency period
Prescribing practitioner must provide written/signed Rx w/in 7 days
28
What are 3 exception for when a faxed prescription can serve as an original Rx and no further verification is required?
Compounded for direct administration
Long term care facilities
Hospice
29
During what period of instruction is a human embryo's growth disrupted?
Organogenesis- 3-8wks
| Teratogenic agents
30
What does maternal alcohol abuse do to a developing fetus?
Microcephaly
31
What does maternal ACE inhibitor use cause to a developing fetus?
Renal function
32
What does maternal warfin use do to a developing fetus?
Cartilage defects
33
Define Category A Drug
Safe for human and baby
34
Define Category B Drug
No risk to fetus
35
Define Category C Drug
Adverse to fetus
36
Define Category D Drug
Evidence supporting adverse effect to fetus
37
Define Category X Drug
Do not give to pregnant woman
38
FDA required the use of what 3 subsection labeling?
Pregnancy
Lactation
Reproductive risk potential
39
What makes up Tiers 1 and 2 of DoD Formulary?
BCF- 1 & 2, must be carried by all MTFs
ECF- 1&2, must be carried if medical service is offered
UF Drugs- 1&2
40
Define Tier 3 Drugs
Non formulary drugs
41
Define Tier 4 Drugs
Medication is not covered, copayment reduction for required need
42
What is the Uniform Formulary?
Pharmaceuticals listed by therapeutic classes determined by DoD P&T committee
43
Define Non-Formulary Unit
Agents not selected for UF
44
Define Basic Core Formulary
List of pharmaceuticals required to be on local formulary
45
Define Extended Core Formulary
Medicatoins used to support specialized scopes of practice than the BCF
46
What happens if an MTF chooses to have an ECF on its formulary?
Must have all ECF medications in that class on the formulary
47
Define Non-Formulary
Medication that can be provided at formulary cost share if the provider supplies information showing there is a medical need/necessity
48
What are the phases of drug development?
```
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
```
49
Define Pharmacokinetics
| Define Pharmacodynamics
What body does to drug
| What drug does to body
50
What do the 4 phases of pharmacokinetics encompass?
ADE
Administration
Systemic circulation
Site of action concentration
51
What are the 4 phases od pharmacokinetics?
ADME
52
What are the pharmacokinetics taken into consideration when determining dosage regimen
```
Bioavailability
Volume of distribution
Drug accumulation
Clearance
Elimination
```
53
What are some factors that determine drug's access to a molecules site of action?
```
Route
Absorption
Distribution
Binding
Metabolism
Clearance
```
54
What happens when a weak acid is placed into an acid medium?
Shift to left, suppresses ionization
55
What happens when a weak acid is placed in an alkaline medium?
Ionization increases
56
What happens when a weak base is placed into an acid medium?
Shift to left, increased ionization
57
What happens when a weak base is placed into an alkaline medium?
Shift to right, suppresses ionization
58
A drugs ability to move from an aqueous to lipid environment depends on what?
Charge
| pH of solution
59
Define Hydrophilic
Hydro: Charged, Polar
Lipo: Uncharged
60
Define the Henderson-Hasselbalch equation
Relationship between ratio of acid to base
61
Define pKa
negative base log of the acid dissociation constant of a solution
Low= acidic
High= basic
62
Ph of a biologic fluid that dissolves a drug affects what two results?
Degree of ionization
| Rate of transport
63
What happens if/when the pKa of a drug equals the pH of the surroundings?
50% ionization occurs
64
Define Weak Acid
H: concentration of protonated/unionized form
A: concentration of ionized/unprotonated form
65
Define Weak Base
BH: concentration of protonated form of base
B: unprotonated concentration
66
How will sodium bicarbonate effect the renal excretion of weak acids?
Increases elimination by increasing urine's pH, turns the weak acid into unprotonated/ionized
67
Alkalinizing urine will have what effect on elimination?
| Acidification of urine will do?
Alk: increases elimination of acidic
Acid: increases basic drug elimination
68
Define Bioavailability
Fraction of unchanged drug reaching the systemic circulation after oral administration
69
What determines/how is bioavailability determined?
Extent of absorption
| First pass metabolism
70
What is an example of a drug that is close to 100% bioavailable?
IV drugs
71
What factors affect passage of drugs across biologic membranes?
Lipid-aqueous partition coefficient (ionization/non-ionized coefficient)
Specific transport
Plasma binding
Perfusion rate
72
____ is the primary site of drug metabolism and _____ is reduced
Liver
| Bioavailability
73
First Pass Metabolism primarily applies to what type of drug but may limit efficacy if ?
Oral administerred
| Efficacy limited if clearance by liver is large
74
What systemic circulation by influence overall first pass metabolism?
Enterohepatic
75
What are 3 ways to obtain better systemic absorption of a drug that has high first-pass effects?
Increased dose
Alternate admin route
Delayed release drug product
76
What are the two drug transport proteins?
Albumin
| A1-acid glycoprotein
77
Drugs bound to ___ proteins are not active and only ____ drugs are active
Plasma
| Free
78
Free drug is available to undergo what two processes?
Bind w/ receptor
| Metabolize/eliminated
79
When/why is plasma protein binding important?
High plasma protein bound drugs- ibuprofen
| Drugs w/ narrow therapeutic index- phenytoin
80
Define Drug Modeling
Describes drug distribution behavior in body by using compartmental models
81
What are 4 characteristics of compartmental models?
Simplification
Non-representative of single tissue
1 / 2 / 3 compartment model
Highly perfused compartments = 1 compartment
82
Define One Compartment Model
Simplest
Comprises all body tissues
Assumes instant distribution through body
83
Define Two Compartment Model
Distribution is not instant
Fist compartment- blood, and highly perfused tissue
Second- less accessible tissues
84
Define Volume of Distribution
Volume that drug distributes and evaluates extensive/limited distribution
"Where the drug goes in body"
85
What is the volume of distribution equation and parts?
Vd=Fdose/Co
F- bioavail
Dose- weight of drug given
C- concentration of drug in blood/plasma
86
What unit of measurement is Volume Distribution (Vd) reflected in?
L
| L/kg
87
Define Small and Large Volume Distribution
Minimal drug distribution
| Extensive drug distribution
88
How does plasma proteins affect volume of distribution?
Drug w/ affinity for protein in plasma will have reduced Vd, decreased plasma proteins will increase Vd
89
What is the major plasma protein involved in drug protein binding?
Albumin
90
What two structures make the BBB?
Capillaries covered in astrocytes
| Endothelial cells making tight junctions
91
How does the placenta affect drug passage?
Lipid solubility facilitates entry
| Placenta is porous, allows large hydrophilic molecules to cross which allows fetal blood levels to increase slowly
92
Metabolic pathways of drugs normally alter drugs in what ways?
Deactivate
Detox
Less active
93
What are the two major type of drug metabolism reactions?
Phase I: Non-synthetic, Cytochrome P450
Phase 2: Synthetic, Glucuronidation
Phase 1 -> Phase 2= conjugation
94
What are examples of Phase 1, Non-Synthetic reactions?
Oxidation
Reduction
Hydroxylations
95
How does Phase 1, Non-Synthetic reactions work?
Introduce function groups to molecules
Converts parent drug to polar metabolite
Causes loss of pharmacologic activity
96
How do Phase 2, Synthetic metabolism reactions work?
Conjugation reactions
Covalent linkage w/ functional group on parent compound
Highly polar conjugates= rapid drug elimination from body
97
Define Inactive Metabolite
Active compound becomes inactivated/detoxed
98
Metabolites that retain similar activities are retaining what part of their molecular structure?
Retain activity of parent compound
99
What does a metabolite with altered activity mean?
Develops different activity from parent drug
100
Define Bioactive Metabolites
Prodrug- inactive substance that must be converted by metabolism to become biologically active
Prodrug= inactive form
101
Define Cytochrome P450 Enzymes
Mixed function oxidases responsible for majority of drug metabolism
102
Define Cytochrome P450 System Substrate
Substance on which enzyme acts
103
Define Cytochrome P450 System Induction
Accelerated metabolism resulting in decreased action of inducing/co-administered drugs
104
Define Cytochrome P450 System Inhibition?
Reduced metabolism of substrates/co-administered drugs metabolized by specific enzyme causing increased action of co-administered drug/substrates
105
What system is behind most clinically important drug/drug interactions?
Cytochrome P450 System
106
Define Chirality
Sereoisomerism
| Geometric property of molecules/ions
107
What are characteristics of chiral molecules?
Non-superposable on mirror image
Rectus- right
Sinister- left
108
Define a Racemic Mixture
Equal mixture of enantiomers
109
What are chiral molecules role in pharmacology?
Seperate an active enantiomer from a pair to create new drug, reduce side effects, extend presence in PTs
110
Define Zero-Order Kinetics
Metabolic rate is dependent on time and not drug concentration
Linear kinetics
No true half-life
111
Define First-Order Kinetics
Metabolic rate is proportional to drug concentration
Non-linear kinetics
Drug disappears w/ time
Half life is constant
112
What are 4 characteristics of nonlinear kinetics?
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
What are 4 variables that cause alterations in drug metabolism?
Genetic variability
Age
Nutrition
Concurrent Disease
114
Define Child-Pugh Classes A, B, and C
A/B- mild/moderate impairment, no dosage adjustment needed
| C- extended release tablets, not recommended
115
A drugs ability to be reabsorbed from glomerular filtrate is determined by what?
Their lipid solubility
| Charged compounds are poorly re-absorbed
116
Define Clearance
Measure of removal of drug from plasma
| Systemic= renal + hepatic + other
117
What two factors determine a drug's half-life?
| What is it related to?
Clearance
Volume of distribution
Related to duration of action
118
How is drug clearance of an organ determined?
Blood flow
| Extraction ratio of organ
119
Define Creatinine Clearance
Estimated renal function from 24hr UA to estimate GFR by using Serum Creatinine
120
Define the Cockcroft-Gault equation
CrCl= ((140 - age) x kg)) / (Scr x 72)
| Add (0.85) after kg for female PT
121
Define Steady State and it's General Rule
Drug intake is equal to elimination
| 5 half live to reach steady state AND for washout
122
Changes in a drugs concentration do not have an effect on it's ______
Half-life
123
How does No Interval/Short Interval drug administration effect the concentration?
Less fluctuation
Same dosing rate but as an infusion
Cmax and Cmin changes will be minimal
124
How does Longer Interval drug administration change concentration?
More fluctuation
Longer interval, same rate
Cmax and Cmin changes will be higher toward Cmax
125
Regardless of No Interval / Short Interval / Long Interval drug administration, what remains the same?
Average plasma concentration
126
Dosing doesn't change time to steady state as long as _____
Half life remains constant
127
If a fluctuation in plasma concentration occurs, what controls the magnitude of fluctuations?
Controlling dosing interval
Shorter= decreased fluctuation
Longer= increased fluctuation
128
Define Maintenance Dose
Does req'd to replace amount of drug lost from body to maintain plasma concentration
129
What are two benefits of changing a dose interval?
Achieve similar steady-state concentrations
| Limited dosage forms (oral)
130
What is an advantage of changing a dose?
When goal is to maintain steady therapeutic concentrations
131
What are two benefits of changing a dose and interval?
For substantial dose adjustment w/ limited dose forms
| Narrow therapeutic index drugs w/ target concentrations
132
If a drug is given more than once daily then adjust ______
| but if it's given daily or less adjust the _____
Interval
| Dose
133
Define Loading Dose
Higher dose of a drug to raise concentration to desired level or steady state concentration followed by a maintenance dose
134
When is a loading dose used?
When therapeutic concentrations of drug in plasma is needed rapidly/initially
135
Time to reach a steady state concentration depends on ?
Elimination half life
136
What pharmacokinetic variables influence dosage regimens?
Absorption
Volume distribution
Clearance
137
Define Potency
Amount needed to cause a response, determined by half life
138
Define Efficacy
Drugs ability to produce desired result, determined by height of log-dose response curve
More important than potency
139
Define Effectiveness
Degree of success in producing desired effect
140
Graded response takes into account what three variables?
BP
Enzyme activity
Muscle tension
141
Define Quantal Response
Number of subjects showing an all or nothing response
Pain
Death
Number anesthetized
142
The higher a drugs therapeutic index means what?
Safe the drug is and less monitoring is required
143
What is the lab monitoring rule for therapeutic indexes?
Small index requires plasma concentration monitoring
144
Define Agonist
Drugs that activate a receptor
145
Define Partial Agonist
Drug can act as an agonist or antagonist
146
Define Antagonist
Drug reduces/prevents responses
147
Define Inverse Agonist
Binds to same receptor as agonist but induces response opposite of an agonist
148
Define Competitive Antagonist
Binds to same receptor as agonist but reduces potency and efficacy of agonist
149
Define Irreversible Antagonist
Permanently antagonizes agonist through covalent bonds and prevents agonist binding and reduces efficacy
150
Define Indirect Agonist
Inhibits termination of an action of endogenous agonist
151
Define Allosteric Agonist
Binds to different receptor sight and indirectly blocks agonist
152
Define Drug Specificity
Drug has one effect and only one effect
153
Define Drug Selectivity
Greater selectivity for a receptor means fewer adverse reactions caused
154
General rule is that if a drug dose goes up then ____?
Selectivity goes down
155
Define Down Regulation
Decrease in number of receptors due to continuous prolonged exposure
156
Define Desensitization
Result of down-regulation
| Requires an increase drug concentration to cause desired effect
157
Define Up-Regulation
Increase in number of receptors
| 3rd trimester pregnancy increase of uterine oxytocin receptors
158
Define Supersensitivity/Hypersensitivity
Enhanced response from long term exposure and abrupt cessation of drug
159
Give 4 examples of drugs who do not act at receptors?
Osmotic diuretics
Detergents
Antacids
Chelating agents
160
Define a Chemical Agonist and give an example
Inactivates an agonist by not allowing agonist able to bind to activating receptor
Protamine Sulfate
161
Define Physiologic Antagonist and give an example
Drugs that compete for interacting with opposing regulatory pathways
Epi and Ach
162
Preganglionic neurons originate with ____
| Postganglionic nuerons originate at _____ and terminate at ____
CNS
| Ganglion, effector organ
163
What are the two types of receptors?
```
Nicotinic neural
Nicotinic muscluar (Muscarinic, A, B D)
```
164
What are the neurotransmitters?
Ach
NE
Epi
D
165
Parasympathetic preganglionic nerves originate from _____ and leave via ____
CNS
| Cranial and sacral regions
166
Parasympathetic reganglionic neurons are _____ than postganglion
Longer
167
Sympathetic preganglionic nerves leave the CNS via ____
Thoracic
| Lumbar
168
Sympathetic preganglionic nerves are ____ than postganglion nerves
Shorter
169
Parasympathetic postganglionic nerves result in a ___ response while sympathetic postganglions result in a ___ response
Discrete
| Diffuse
170
3 examples of chemical signaling
Neurotransmitters
Hormones
Local mediators
171
What effects do acetycholinesterase inhibitors have on the body?
Prolong Ach action at muscarinic sites as an indirect agonist
172
Difference between endocrine gland and exocrine gland
Endo- ductless secretion into bloodstream
| Exo- duct secretion to environment
173
M1 muscarinic receptors
Nerves
Salivary/stomach secretions
CNS
174
M2 muscarinic receptors
Cardiac cells
Bladder
Smooth muscle
175
M3 muscarinic receptors
Bladder
Exocrine glands
Smooth muscle
176
Cholinergic agents modulate Ach effects in what 3 ways?
Agonist
Antagonist
Indirect agonist
177
Drugs that mimic or prolong actions of Ach are called ?
Parasympathomimetics
| Cholinomimetics
178
Drugs that antagonize or block actions of Ach are called ?
Anticholinergics
179
Cholinergic agonists cause what effects on the body?
```
DUMBBELLS
Defecation
Urination
Miosis
Bradycardia
Bronchospasm
Emesis
Lacrimation
Lethargy
Salivation
```
180
Sweat and salivary glands increase secretions from what types of stimulation?
Cholinergic and Sympathetic
181
What are the major therapeutic uses for cholinomimetics?
```
Anti-cholinergic OD
Glaucoma
Xerostomia
Reduced GI/GU motility
Alzeihmers
Myasthenia Gravis
Reversal of Curare-induced neuromuscular paralysis
```
182
Don't give cholinergic agonists to PTs with what diseases/illnesses?
```
Bradycardia/hypotension
Asthma
Peptic ulcers
GI obstruction
GU obstruction
Parkinson's Disease
```
183
What are the cholinergic agonist effects on eye muscles and pupils?
Radial Iris- a1 SNS conraction, mydriasis
Circular Iris- m3 PNS contraction miosis
Ciliary- B2 SNS relaxation/M3 PNS contraction accomodation
184
How does the eye accomodate for close vision?
Tightens cilliary muscles allowing lens to become more rounded
185
What is the cholinergistic effect on eyes?
Muscarinic receptors contract circular muscles (pinpoint)
Produces a spasm of accommodation
Lens bulges for near vision
186
What is the cholinergistic use for clinic?
Refractive measurements
| Ophthalmoscopic exam of retina
187
What is an example of a cholinergistic drug used in clinic for eyes?
Pilocarpine- cholinergic agonist
188
How do cholinomimetics exert their effect?
Increases resistance to degradation by cholinesterases
| Increases selectivity for muscarinic receptors relative to nicotinic receptors
189
Why is acetylcholine not used in clinic often?
Poor bioavailability, rapidly hydrolyzed by GI tract and inactivated by acetylcholinesterase
190
Acetylcholine is nonspecific for what receptors?
Nicotinic and muscarinic
191
Although not used often, what is a use for acetycholine such as Miochol-E?
Induces miosis for eye procedures
192
What effect does pilocarpine have on the eye?
| What effect does it cause on the rest of the body?
Increases aqueous humor outflow by contracting the ciliary muscle
Stims lacrimal/salivary secretions
193
What is a clinical indication for using Pilocarpine?
Reduce intraocular pressure in glaucoma PTs (angle-closure and open-angle)
194
What medication is prescribed to prevent post-operative intraocular pressure associated with laser surgery?
Pilocarpine
195
What medication is given to PTs w/ Xerostomia?
Pilocarpine
Post radiation therapy for head/neck tumor
Sjogren's Syndrome (autoimmune disease destroys salivary/lacrimal glands)
196
What are the adverse effects of Pilocarpine use?
Miosis
| Decreased far vision
197
What is the normal flow of aqueous humor through the eye? How is this inhibited?
Ciliary body to trabecular mesh work
| Angle-closure: increased IOP from posterior chamber pushes iris against mesh work and closes ocular angle
198
What is the mechanism of action for Bethanechol?
Cholinergic agonist increases bladder muscle tone causing detrusor muscle contractions and trigone sphincter relaxation increasing urination
199
What is the clinical indication for Bethanechol?
Acute postoperative/postpartum non-obstructive urinary retention
Neurogenic atony of bladder w/ retention/ileus
200
What are the contraindications for Bethanechol use?
```
Physical obstruction of GI/GU
Bladder strength is questionable
Asthma
Peptic ulcer disease
Bradycardia
```
201
What is the indirect action of acetylcholinesterase inhibitors?
Inhibit actetylcholinesterase from metabolizing Ach causing a prolonged effect
202
What is the mechanism of action of Edrophonium?
Plant-derived reversible competitive Achesterase inhibitor that increases Ach potency by inhibiting the molecules destruction but is short lasting, 30sec-10m
203
What is the clinical indication for using Endrophonium?
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
What is an example of a medication that Edrophonium would not be useful using to treat?
Depolarizing neuromuscular agents
| Succinylcholine chloride
205
What is the contraindications for using Edrophonium?
GI/GU obstruction
| Bladder wall strength is questionable
206
What is the MOA for Physostigmine Salicylate
Plant derive competitive Achesterase inhibitor that potentiates its action by preventing destruction
207
What is the clinical indication for Physostigmine Salicylate?
Reverse CNS effects of Achergics
| Routine use is not recommended due to adverse effects
208
What are the possible adverse effects of using Physostigmine Salicylate for routine use?
Delirium/agitation
Hallucinations
Hyperthermia
Supraventricular tachycardia
209
What type of monitoring should be used for Physostigmine Salicylate?
ECG
Vitals
Seizures since it can cross BBB
210
What are the contraindications for using Physostigmine Salicylate?
GI/GU obstruction
Bladder wall integrity is questioned
Respiratory distress/seizures
211
What is the MOA for Neostigmine?
Synthetic competitive inhibitor that prolongs effect by preventing destruction
212
What is the clinical indication for using Neostigmine?
Symptomatic treatment for Myasthenia Gracis
| Reverses nondepolarizing neuromuscular agents
213
What are the two formulations for Neostigmine?
N. Bromide- tablet
| N. Methyl Sulfate- IV
214
Why would the use of Neostigmine be preferred over Physostigmine?
More polar, does not cross CNS, no seizures
215
PTs with what conditions should be warned before using Neostigmine?
Asthma
Peptic Ulcer
Bradycardia
216
What are the contraindications for Neostigmine?
GI/GU obstruction
| Bladder wall integrity is questioned
217
What is the MOA for Pyridostigmine Bromide
Synthetic
218
Pyridostigmine is preferred over neostigmine because?
Longer duration
Fewer GI symptoms
Allows for better transmission of impulses across neuromuscular junction
219
What is the clinical indication for Pyridostigmine Bromide?
Myasthenia Gravis treatment
Reverses nondepolarizing neuromuscular blocking agents
Nerve agent pretreatment pyridostigmine
220
Pyridostigmine Bromide has historically served as _______
Nerve Agent Pyridostigmine Pretreatment (NAPP)
221
What are the cautions for using Pyridostigmine?
Peptic Ulcer
Bradycardia
Asthma
222
What are the contraindications for Pyridostigmine Bromide?
GI/GU obstruction
| Bladder wall integrity is questioned
223
Most noncompetitive (irreversible) Ach inhibitors find their uses as what two things?
Insecticides
| Nerve agents
224
Increased Ach at the nicotinic receptors can lead to what issues?
Seizure
Coma
Cardiac arrhythmia
Respiratory arrest
225
What are examples of Irreversible Acetylcholinesterase Inhibitors?
Ecothipoate- eye drops for glaucoma, target postganglionic ParaSymp junction
Sarin- mimics insecticides
Parathion- insecticide
226
What is the MOA of Echothiophate Iodide?
ONLY noncompetitive Achesterase inhibitor used on a regular basis
227
What is the effect of Echothiophate Iodide on the eye?
Contracts ciliary muscles to increase aqueous humor flow
228
What are the adverse effects of using Echothiophate Iodide for glaucoma?
```
Miosis
Decreased accommodation (far vision)
```
229
What is the MOA of Pralidoxime?
Reactive cholinesterase (mainly outside of CNS) that were inactivated by phosphorylation from organophosphate pesticides
230
What is the most critical part of Pralidoxime's MOA?
Slows aging process of phosphorylated cholinesterase to non-reactive form
Reverses paralysis of respiratory muscles
231
The use of Pralidoxime relieves what symptoms?
Salivation
| Bronchospasm
232
What is the form of Pralidoxime for chemical warfare?
ATNAA- reactive cholinesterase
233
What are the clinical indications for using Pralidoxime?
Treat pesticide poisoning (nerve agents of organophosphate class)
OD of anticholinesterase drugs from treating myasthenia gravis
234
What are the adverse effects of using Pralidoxime?
Anticholinergic effects: anticholinergic drug symptoms
235
How do acetylcholine and acetycholinesterase interact?
Pos charge of acetylcholine attracted to ionic site of acetylcholinesterase
Hydrolysis catalyzed to form choline and acetic acid
236
How do cholinesterase inhibitors and acetylcholinesterases react with each other?
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
How do Pralidoxime and Achesterase react with each other?
Pralidoximes N attracted to Ach neg charge
Pralidoxime removes Ach inhibitor
Achesterase regenerated
238
_____ is the major neurotransmitter of the PNS
| What other three areas is it seen in?
Ach
| CNS, Symp/ParaSymp NS, Somatic NS
239
How can the degeneration effects of Alzheimers be slows?
With drugs that increase Ach concentrations in CNS by inhibiting central Achesterase
240
What are 4 drugs that could be used to increase Ach levels in Alzheimer's PTs?
Tacrine- multiple doses/day, hepatotoxic
Donepezil- daily dose preferred
Galantamine- metabolized by CYP2D6/3A4
Rivastigmine- Patch form better tolerated
241
Nicotine is an example of what type of stimulant?
Ganglionic
242
What effects does Nicotine have at low doses? What effects a high dose?
Low- Depolarizes autonomic ganglia causing euphoria/arousal
| High- blocks autonomic ganglia causing decreased BP and possible respiratory paralysis
243
Where does a greater amount of nicotine absorption take place?
75% smoke held in mouth
| 95% smoke held in lungs
244
Anticholinergic agents block Ach interaction with what type of receptors?
Muscarinic
| Nicotinic
245
Define M Receptor Antagonist
Antimuscarinic
246
Define Nn receptor agonist?
| Why is this not usually used?
Ganglionic blocker
| Blocks both Symp/ParaSymp transmission
247
Defein Nm receptor Agonist
Neuromuscluar/skeltal muscle blocking agent
248
Anticholinergic agent effects are the opposite of ? stimulation
Cholinergic
249
What is the saying for remembering the S/Sx of anticholinergic agents?
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
What are the major therapeutic uses of Anti-Muscarinic agents?
```
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
What are the contraindications for Anticholinergic Agent use?
```
Narrow angle glaucoma
Angina
Alzheimers
Asthma
Diarhhea
Increased heat injuries
Myasthenia gravis
```
252
What is the prototype anticholinergic?
Atropine
253
What are the Anticholinergics for the eye?
Cyclopentolate
| Tropicamide
254
What are the Anticholinergics for GI?
Dicyclomine
| Belladonna Alkaloids
255
What are the Anticholinergics for the lungs?
Ipratropium
| Tiotropium
256
What are the Anticholinergics for GU?
```
Oxybutynin
Darifenacin
Solifenacin
Tolterodine
Fesoterodine
Trospium
```
257
What are the Anticholinergics for Parkinsons?
Benztropine
| Trihexyphenidyl
258
What is the MOA of dopamine?
Inhibits muscarinic actions of Ach on post-gang cholinergic nerves
259
Atropine is a ____ and _____ anticholinergic
Central
| Peripheral
260
What are the pharmacodynamic effects of atropine?
Reduces oral secretions
Relieves broncho constrictions/spasms
Stops vagal cardiac slowing/bradycardia
Asystole
261
What are the clinical indications of atropine?
Mydriatic/cyclopegic diagnostic agent
Bradycardia
Relaxes upper GI
Cholinergic OD
262
What has to be monitored during atropine administration?
HR
BP
Mental status
263
What are the clinical uses for anticholinergics for the eye?
Diagnostic procedures requiring mydriasis and cyclopegia
Refractive measurement
Ophthalmoscopic exam of retina
264
What is the MOA of anticholinergics for the eye?
Produces cycloplegia by paralyzing ciliary muscles
Loss of accommodation
Mydriasis by blocking parasympathetic tone
265
What is the MOA of anticholinergics for GU use?
Dec bladder muscle tone causing detrusor muscle relaxation and sphincter constriction causing urinary retention
266
What is the clinical indication for using anticholiinergics for GI use?
Overactive bladder w/ incontinence, urgency and frequency
267
What are the adverse effects of using anticholinergics for GI use?
Dry mouth
Constipation
Site reaction/itching of patch
268
Stopped on
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