USMLE Gen Pharm Flashcards
1
Q
Km: Definition
A
Km = Substrate at 0.5*Vmax
Km reflects the affinity of the enzyme for its substrate
2
Q
Vmax indicates what?
A
Vmax is directly proportional to the enzyme concentration.
3
Q
Relationship between Km and affinity
A
–The lower the Km, the higher the affinity
–Smaller Km means enzyme is saturated earlier, which means that small amounts of substrate are picked up by the enzyme.
4
Q
Reading an inverse curve: Y–intercept equals ?
A
1/Vmax
The higher the Y–intercept the lower the Vmax
5
Q
Reading an inverse curve: X–intercept equals ?
A
(1/–Km)
The further to the right the x–intercept, the greater the Km
6
Q
Reading an inverse curve: Slope equals ?
A
Km/Vmax
7
Q
Reading an inverse curve: Effect of a competitive inhibitor
A
X–intercept farther to the right, meaning Km is greater, because you need more substrate to get the same effect as the competitive inhibitor is hogging the enzyme.
The y–intercept is the same, meaning Vmax hasn’t changed, because there isn’t any more enzyme.
The slope is greater, because Km has increased while Vmax has stayed the same.
8
Q
Reading an inverse curve: Effect of a noncompetitive inhibitor
A
The x–intercept is the same, meaning Km is the same, because the affinity for the enzyme hasn’t changed, there’s just less of it.
The y intercept has increased, meaning Vmax has decreased, because enzyme has been inactivated by the noncompetitive inhibitor
The slope is greater, because Vmax has decreased while Km has stayed the same.
9
Q
Competitive inhibitor: Resemble substrate
A
Yes
10
Q
Competitive inhibitor: Overcome by increased substrate?
A
Yes
11
Q
Competitive inhibitor: Binds active site?
A
Yes
12
Q
Competitive inhibitor: Effect on Vmax
A
Unchanged. The amount of enzyme has not changed.
13
Q
Competitive inhibitor: Effect on Km
A
Increased. A lot more substrate needs to be available to seize the active sites.
14
Q
Noncompetitive inhibitor: Resemble substrate?
A
No
15
Q
Noncompetitive inhibitor: Overcome by increased substrate?
A
No
16
Q
Noncompetitive inhibitor: Binds active site?
A
No
17
Q
Noncompetitive inhibitor: Effect on Vmax
A
Decreased. Takes the enzyme out.
18
Q
Noncompetitive inhibitor: Effect on Km
A
Unchanged. Does not change the affinity for the enzyme.
19
Q
Volume of distribution: Abbreviation
A
Vd
20
Q
Vd: Stands for what?
A
Volume of distribution
21
Q
Volume of distribution: definition
A
Vd = (amount of drug in the body)/(plasma drug concentration)
22
Q
Volume of distribution: What alters it?
A
Liver and kidney disease
23
Q
Where are drugs with a low Vd distributed?
A
plasma
24
Q
Where are drugs with a medium Vd distributed?
A
extracellular space
25
Where are drugs with a high Vd distributed?
tissues
26
Clearance: definition
(rate of elimination of drug)/(plasma drug concentration)
=Vd x Ke where Ke=elimination constant
27
Half life: definition
The time required to change the amount of drug in the body by 1/2 during elimination (or during a constant infusion).
28
What percentage of steady state is a drug at after: 1 half life
50%
29
What percentage of steady state is a drug at after: 2 half lives
75%
30
What percentage of steady state is a drug at after: 3 half lives
87.50%
31
What percentage of steady state is a drug at after: 3.3 half lives
90%
32
What percentage of steady state is a drug at after: 4 half lives
94%
33
How many half lives does it take for a drug to reach the following percentage of steady state: 50%
1 half life
34
How many half lives does it take for a drug to reach the following percentage of steady state: 75%
2 half lives
35
How many half lives does it take for a drug to reach the following percentage of steady state: 87.5%
3 half lives
36
How many half lives does it take for a drug to reach the following percentage of steady state: 90%
3.3 half lives
37
How many half lives does it take for a drug to reach the following percentage of steady state: 94%
4 half lives
38
Cp stands for what?
target plasma concentration
39
What is the abbreviation for target plasma concentration?
Cp
40
In pharmacology, what is F an abbreviation for?
Bioavailability
41
What is the abbreviation in pharmacology for bioavailability?
F
42
Loading dose: Definition
Loading dose = (Cp * Vd)/F (where Cp equals the target plasma concentration, Vd equals volume of distribution, and F equals bioavailability)
43
Maintenance dose: Definition
Maintenance dose = (Cp * CL)/F (where Cp is the target plasma concentration and CL is clearance and F is bioavailability)
44
Zero–order elimination: definition
Constant elimination over time regardless of drug.
45
How does Cp vary with time during zero–order elimination?
Cp decreases linearly with time.
46
Zero–order elimination: Drug examples
–Ethanol
–Phenytoin
–Aspirin (at high concentrations)
47
First–order elimination: definition
Rate of elimination is proportional to drug concentration
48
Zero–order elimination vs First–order elimination: Comparison
Zero–order: Constant amount of drug eliminated per unit time
1st–order: Constant fraction of drug eliminated per unit time
49
How does Cp vary with time during first–order elimination?
Cp decreases exponentially with time.
50
Urine: Which species get trapped in urine?
Ionized species
51
In what kind of environment is the following trapped?: Weak acids
Basic environments
52
In what kind of environment is the following trapped?: Weak bases
Acidic environments
53
In what kind of environment is the following digested?: Weak acids
Acidic environments (below pKa)
54
In what kind of environment is the following digested?: Weak bases
Basic environments (above pKa)
55
How do you treat an overdose of the following?: Weak acids
Bicarbonate
56
How do you treat an overdose of the following?: Weak bases
Ammonium chloride
57
Phase I metabolism: Processes
Cytochrome P450
–reduction
–oxidation
–hydrolysis
58
Phase II metabolism: Processes
Conjugation
–acetylation
–glucuronidation
–sulfation
59
Phase I metabolism: Metabolites
–slightly polar
–water–soluble
–often still active
60
Phase II metabolism: Metabolites
–very polar
–renally excreted
–inactive
61
What phase of metabolism do geriatric patients lose first?
Phase I
62
Effect on dose/effect curve of: competitive antagonist
Shifts curve to the right, decreasing potency and increasing EC50.
63
Effect on dose/effect curve of: noncompetitive antagonist
Shifts curve downward, decreasing efficacy
64
What is EC50?
Dose causing 50% of maximal effect
65
What is Kd?
Concentration of drug required to bind 50% of receptor sites
66
How many half lives does it take for a drug to reach the following percentage of steady state: 97%
5 half lives
67
What percentage of steady state is a drug at after: 5 half lives
97%
68
Effect on dose/effect curve: Spare receptors
The drug binding and drug effect are independent of each other with effect to the left of binding.
This means that EC50 is lower than Kd, so very little drug needs to bind to get 50% of the effect.
69
Effect on dose/effect curve: Partial agonist
–Lower maximal efficacy
| –Potency independent (amount of dose to get to maximum effect)
70
Therapeutic Index: Definition
#ERROR!
71
Where are nicotinic receptors found?
Preganglionic synapses before:
–Cardiac and smooth muscle (Parasympathetic and Sympathetic)
–Gland cells (Parasympathetic and Sympathetic)
–Nerve terminals (Parasympathetic and Sympathetic)
–Renal vascular smooth muscle (Sympathetic)
Neuromuscular junctions for skeletal muscle
72
What is the neurotransmitter at Nictoinic receptors?
Acetylcholine
73
What is the neurotransmitter at Muscarinic receptors?
Acetylcholine
74
Where are muscarinic receptors found?
Parasympathetic end plates:
–Cardiac and smooth muscle
–Gland cells
–Nerve terminals
Sympathetic end plate:
–Sweat glands
75
Where are D1 receptors found?
Sympathetic:
| Renal vascular smooth muscle
76
What type of G–protein is associated with the following receptor type?: alpha–1
Gq
77
What type of G–protein is associated with the following receptor type?: alpha–2
Gi
78
What type of G–protein is associated with the following receptor type?: beta–1
Gs
79
What type of G–protein is associated with the following receptor type?: beta–2
Gs
80
What type of G–protein is associated with the following receptor type?: M1
Gq
81
What type of G–protein is associated with the following receptor type?: M2
Gi
82
What type of G–protein is associated with the following receptor type?: M3
Gq
83
What type of G–protein is associated with the following receptor type?: D1
Gs
84
What type of G–protein is associated with the following receptor type?: D2
Gi
85
What type of G–protein is associated with the following receptor type?: H1
Gq
86
What type of G–protein is associated with the following receptor type?: H2
Gs
87
What type of G–protein is associated with the following receptor type?: V1
Gq
88
What type of G–protein is associated with the following receptor type?: V2
Gs
89
What types of receptors are associated with the following G–proteins: q
```
–alpha–1
–M1
–M3
–H1
–V1
```
90
What types of receptors are associated with the following G–proteins: i
–alpha–2
–M2
–D2
91
What types of receptors are associated with the following G–proteins: s
```
–beta–1
–beta–2
–D1
–H2
–V2
```
92
What are the major functions of the following receptor type: alpha–1
Increase vascular smooth muscle contraction
93
What are the major functions of the following receptor type: alpha–2
–Decrease sympathetic outflow
| –Decrease insulin release
94
What are the major functions of the following receptor type: beta–1
```
–Increase heart rate
–Increase contractility
–Increase renin release
–Increase lipolysis
–Increase aqueous humor formation
```
95
What are the major functions of the following receptor type: beta–2
–Vasodilation
–Bronchodilation
–Increased glucagon release
96
What are the major functions of the following receptor type: M1
CNS
97
What are the major functions of the following receptor type: M2
Decrease heart rate
98
What are the major functions of the following receptor type: M3
Increase exocrine gland secretions
99
What are the major functions of the following receptor type: D1
Relax renal vascular smooth muscle
100
What are the major functions of the following receptor type: D2
Modulate transmitter release (especially in brain)
101
What are the major functions of the following receptor type: H1
–Increase nasal/bronchial mucus production
–Contraction of bronchioles
–Pruritus
–Pain
102
What are the major functions of the following receptor type: H2
Increased gastric acid secretion
103
What are the major functions of the following receptor type: V1
Increased vascular smooth muscle contraction
104
What are the major functions of the following receptor type: V2
–Increased water permeability and reabsorption in the collecting tubules of the kidney
105
Gq protein pathway
–Receptor stimulated
–Gq protein stimulates Phospholipase C
–Phospholipase C catalyzes the conversion of Lipids to PIP2
–PIP2 splits into IP3 and DAG
IP3 stimulates an increase in Calcium concentration
DAG activates Protein Kinase C
106
Gs protein pathway
```
–Receptor stimulated
–Gs protein stimulates Adenylylcyclase
–Adenylylcyclase
catalyzes conversion of ATP to cAMP
–cAMP activates Protein Kinase A
```
107
Gi protein pathway
–Receptor stimulated
–Gi protein inhibits Adenylylcyclase
–Decreases conversion of ATP to cAMP
–Decreased activation of Protein kinase A
108
Cholinergic pathway (presynaptic events to receptor)
1. Choline transported into presynaptic bulb
2. Acetyl–Coa joints with Choline–ChAT to form acetylcholine, and the two are taken up by a vesicle.
3. The vesicle joins with the cell membrane and ACh is exocytosed
4. ACh is released into the synapse
5. Acetylcholine joints with the Cholinoceptor or is degraded by AChE into Choline + Acetate
109
Hemicholinum: Action and mechanism
Inhibits cholinergic transmission
Mechanism: Inhibits transfer of choline into presynaptic bulb
110
Vesamicol: Action and mechanism
Inhibits cholinergic transmission
Mechanism: Inhibits uptake of ACh into a vesicle in the presynaptic bulb
111
Ca2+: Action on presynaptic vesicles
Stimulates exocytosis of neurotransmitters from presynaptic bulb
112
Botulinum: Action and mechanism
Inhibits cholinergic transmission
Mechanism: Inhibits exocytosis of neurotransmitters from presynaptic bulb
113
Noradrenergic pathway (presynaptic events to receptor)
1. Tyrosine is transferred into the presynaptic bulb
2. Tyrosine is converted into DOPA
3. DOPA is converted to Dopamine
4. Dopamine is converted to Norepinephrine and transferred into a vesicle
5. Norepinephrine is exocytosed from the presynaptic terminal
6. 3 possibilities happen
a. Norepinephrine binds to a beta adrenoreceptor.
b. Norepinephrine is reuptaken by the releasing neuron
c. Norepinephrine binds to an alpha–2 receptor on the releasing neuron
d. It diffuses away/is metabolized.
114
Metyrosine: Action and mechanism
Action: Inhibits noradrenergic transmission
Mechanism: Inhibits step where tyrosine is converted into DOPA
115
Reserpine: Action and mechanism
Action: Inhibits noradrenergic transmission
Mechanism: Prevents sequestration of norepinephrine into vesicles
116
Guanethidine: Action and mechanism
Action: Inhibits noradrenergic transmission
Mechanism: Inhibits exocytosis of Norepinephrine from presynaptic bulb
117
Amphetamine: Action and mechanism
Action: Stimulates noradrenergic transmission
Mechanism: Stimulates exocytosis of norepinephrine from presynaptic bulb
118
Tricyclic antidepressant: Mechanism
Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron
119
Cocaine: Mechanism
Decreases reuptake of norepinephrine from synaptic cleft into releasing neuron
120
Angiotensin II: Effect on noradrenergic pre–synaptic neurons
Enhances release of NE
121
Cholinomimetics: Direct agonists
Bethanechol, Carbachol, Pilocarpine, Methacholine
122
Cholinomimetics: Indirect agonists
Neostigmine (AChE inhibitor), Pyridostigmine, Edrophonium, Physostigmine, Echothiophate
123
Use of: Bethanechol
Postoperative and neurogenic ileus and urinary retention
124
Use of: Carbachol
–Glaucoma
–pupillary contraction
–release of intraocular pressure
125
Use of: Pilocarpine
Potent stimulator of:
–Sweat
–Tears
–Saliva
126
Use of: Methacholine
Challenge test for diagnosis of asthma
127
Use of: Neostigmine
AChE inhibitor
–Postoperative/neurogenic ileus/urinary retetnion
–Myasthenia Gravis
–Reversal of neuromuscular junction blockade (postoperative)
–No CNS penetration
128
Use of: Pyridostigmine
–Myasthenia Gravis (increases strength)
| –does penetrate CNS
129
Use of: Edrophonium
Diagnosis of myasthenia gravis (extremely short acting)
130
Use of: Physostigmine
–Glaucoma (crosses blood–brain barrier into CNS)
| –Atropine overdose
131
Use of: Ecthiophate
–Glaucoma
132
Mechanism of indirect cholinomimetics
Increase endogenous ACh
133
Synonym for indirect cholinomimetics
Anticholinesterases
134
Synonym for anticholinesterases
indirect cholinomimetics
135
Bethanechol: mechanism
–Activates bowel and bladder smooth muscle
| –Resistant to AChE
136
Carbachol: mechanism
–Contracts ciliary muscle of eye (open angle)
–Contracts Pupillary sphincter (narrow angle)
–Resistant to AChE
137
Methacholine: mechanism
Stimulates muscarinic receptors in airway when inhaled
138
Symptoms of cholinesterase inhibitor poisoning
DUMBBELS SAC
```
–Diarrhea
–Urination
–Miosis
–Bronchospasm
–Bradycardia
–Excitation of skeletal muscle and CNS
–Lacrimation
–Sweating
–Salivation
–Abdominal Cramping
```
139
Antidote to cholinesterase inhibitor poisoning
–Atropine (muscarinic antagonist) +
| –Pralidoxime (chemical antagonist used to regenerate active cholinesterase)
140
Cholinesterase inhibitors
–Parathion
| –Other organophosphates
141
Cholinoreceptor blockers
```
–Atropine (homatropine, tropicamide)
–Benztropine
–Scopolamine
–Ipratropium
–Methscoplamine (oxybutin, glycopyrrolate)
```
142
Cholinoreceptor blockers used to produce: mydriasis and cycloplegia
Atropine, homatropine, tropicamide
143
Cholinoreceptor blockers used for: Parkinson's disease
Benztropine
144
Cholinoreceptor blockers used for: Motion sickness
Scopolamine
145
Cholinoreceptor blockers used for: Obstructive pulmonary disease
Ipratropium
146
Cholinoreceptor blockers used for: Genitourinary problems
–Methscopolamine
–Oxybutin
–Glycopyrrolate
147
Application of: Atropine
Produce mydriasis and cycloplegia
148
Application of: Homatropine
Produce mydriasis and cycloplegia
149
Application of: Tropicamide
Produce mydriasis and cycloplegia
150
Application of: Benztropine
Parkinson's Disease
151
Application of: Scopolamine
Motion sickness
152
Application of: Ipratropium
Obstructive pulmonary diseases
153
Application of: Methscopolamine
–Reduce urgency in mild cystitis
| –Reduce bladder spasms
154
Application of: Oxybutin
–Reduce urgency in mild cystitis
| –Reduce bladder spasms
155
Application of: Glycopyrrolate
–Reduce urgency in mild cystitis
| –Reduce bladder spasms
156
Glaucoma drugs: Categories
```
–alpha–agonists
–beta–blockers
–diuretics
–cholinomimetics
–prostaglandins
```
157
Glaucoma drugs – alpha agonists:
Epinephrine
| Brimonidine
158
Which glaucoma drug should not be used in closed–angle glaucoma?
Epinephrine
159
Epinephrine: Mechanisms and side effects
```
–M:
––Increased outflow of aqueous humor
–E:
––Mydriasis
––Stinging
––Do not use in closed angle glaucoma
```
160
Brimonidine: Mechanisms and side effects
M: Decreased aqueous humor synthesis
E: No pupillary or vision changes
161
Glaucoma drugs – beta blockers:
Timolol
Betaxolol
Carteolol
162
Glaucoma drugs – beta blockers: Mechanism and side effects
M: Decreased aqueous humor secretion
E: No pupillary or vision changes
163
Glaucoma drugs – diuretics: Drugs
Acetazolamide
164
Glaucoma drugs – diuretics: mechanisms and side effects
M: Decreased aqueous humor secretion due to decreased bicarbonate (via inhibition of carbonic anhydrase)
E: No pupillary or vision changes
165
Glaucoma drugs – Cholinomimetics: Drugs
Direct: Pilocarpine, Carbechol
Indirect: Physostigmine, Ecthiopate
166
Glaucoma drugs – Cholinomimetics: Mechanism and Side effects
M:
–Increase outflow of aqueous humor
–Contract ciliary muscle and open trabecular meshwork
–Use pilocarpine in emergencies
–Very effective at opening canal of Schlemm
E:
–Miosis
–Cyclospasm
167
Glaucoma drugs – Prostaglandins: Drugs
Latanoprost (PGF–2alpha)
168
Glaucoma drugs – Prostaglandins: Mechanism and Effects
M: Increase outflow of aqueous humor
E: Darkens color of iris (browning)
169
Atropine: General effects mnemonic
Blocks BUMBLED ASS
```
B: Bradycardia
U: Urination
M: Miosis
B: Bronchospasm
L: Lacrimation
E: Excitation of skeletal muscle and CNS
D: Diarrhea
A: Abdominal cramping
S: Sweating
S: Salivation
```
170
Atropine: Side effects
–Hot as a hare (Increased body temperature; hyperthermia in infants)
–Dry as a bone (Dry mouth and dry skin; Urinary retention in men with prostatic hypertrophy; Constipation)
–Red as a beet (Flushed skin)
–Blind as a bat (Cycloplegia, Acute angle–closure glaucoma in elderly)
–Mad as a hatter (disorientation)
171
Atropine: Mechanism
Muscarinic antagonist
172
Atropine: Effects on organ system: Eye
–Increased pupil dilation
| –Cycloplegia
173
Atropine: Effects on organ system: Airway
–Decreased secretions
174
Atropine: Effects on organ system: Stomach
–Decreased acid secretion
175
Atropine: Effects on organ system: Gut
–Decreased motility
176
Atropine: Effects on organ system: Bladder
–Decreased urgency in cystitis
177
Hexamethonium: Mechanism
Nicotinic ACh receptor antagonist: Ganglionic blocker
178
Hexamethonium: Clinical use
Prevents vagal reflex responses to changes in blood pressure (eg prevents reflex bradycardia caused by NE)
179
Sympathomimetics: Catecholamines: List
```
–Epinephrine
–Norepinephrine
–Isoproterenol
–Dopamine
–Dobutamine
```
180
Sympathomimetics: Non–catecholamines: List
```
–Amphetamine
–Ephedrine
–Phenylephrine
–Albuterol
–terbutaline
–Cocaine
–Clonidine
–Alpha–methyldopa
```
181
Catecholamines: Epinephrine: Mechanism/selectivity
–alpha–1
–alpha–2
–beta–1 (low doses beta–1 selective)
–beta–2
182
Catecholamines: Epinephrine: Applications
–Anaphylaxis
–Glaucoma (open angle)
–Asthma
–Hypotension
183
Catecholamines: Norepinephrine: Mechanism/selectivity
More selective
–alpha–1
–alpha–2
Less selective
–beta–1
184
Catecholamines: Norepinephrine: Applications
Hypotension (but decreased renal perfusion)
185
Catecholamines: Isoproterenol: Mechanism/selectivity
beta–1 = beta–2
186
Catecholamines: Isoproterenol: Applications
AV block (rare)
187
Catecholamines: Dopamine: Mechanism/selectivity
In decreasing order:
–D1=D2
–beta
–alpha
188
Catecholamines: Dopamine: Applications
–Shock (Increased renal perfusion)
| –Heart failure
189
Catecholamines: Dobutamine: Mechanism/selectivity
In decreasing order:
–Beta–1
–Beta–2
190
Catecholamines: Dobutamine: Applications
–Shock
| –Heart failure cardiac stress testing
191
Catecholamines: Amphetamine: Mechanism/selectivity
–Indirect general agonist
| –Releases stored catecholamines
192
Non–catecholamine sympathomimetics: Amphetamine: Applications
–Narcolepsy
–Obesity
–ADD
193
Non–catecholamine sympathomimetics: Ephedrine: Mechanism/selectivity
–Indirect general agonist
| –releases stored catecholamines
194
Non–catecholamine sympathomimetics: Ephedrine: Applications
–Nasal decongestion
–Urinary incontinence
–Hypotension
195
Non–catecholamine sympathomimetics: Phenyephrine: Mechanism/selectivity
alpha–1 more than alpha–2
196
Non–catecholamine sympathomimetics: Phenyephrine: Applications
–Pupil dilator
–Vasoconstriction
–Nasal decongestion
197
Non–catecholamine sympathomimetics: Albuterol: Mechanism/selectivity
Beta–2 > Beta–1
198
Non–catecholamine sympathomimetics: Albuterol: Applications
Asthma
199
Non–catecholamine sympathomimetics: Terbutaline: Mechanism/selectivity
Beta–2 > Beta–1
200
Non–catecholamine sympathomimetics: Terbutaline: Applications
Asthma
201
Non–catecholamine sympathomimetics: Cocaine: Mechanism/selectivity
–Indirect general agonist
| –Uptake inhibitor
202
Non–catecholamine sympathomimetics: Cocaine: Applications
–Vasoconstriction
| –Local anesthesia
203
Non–catecholamine sympathomimetics: Clonidine: Mechanism/selectivity
–Centrally acting alpha–2 agonist
| –Decreases central adrenergic outflow
204
Non–catecholamine sympathomimetics: alpha–methyldopa: Mechanism/selectivity
–Centrally acting alpha–2 agonist
| –Decreases central adrenergic outflow
205
Non–catecholamine sympathomimetics: Clonidine: Applications
Hypertension (especially with renal disease, as there is no decrease in blood flow)
206
Non–catecholamine sympathomimetics: alpha–methyldopa: Applications
Hypertension (especially with renal disease, as there is no decrease in blood flow)
207
Sympathomimetics selective for: alpha–1
–Phenylephrine (alpha–1 more than alpha–2)
| –Norepinephrine (alpha–1 and alpha–2 more than beta–1)
208
Sympathomimetics selective for: alpha–2
–Clonidine
–alpha–methyldopa
–Norepinephrine (alpha–1 and alpha–2 more than beta–1)
–Phenylephrine (alpha–1 more than alpha–2)
–Norepinephrine (alpha–1 and alpha–2 more than beta–1)
209
Sympathomimetics selective for: beta–1
–Dobutamine (beta–1 more than beta–2)
–Isoproterenol (beta–1 = beta–2)
–Epinephrine (at low doses)
–Albuterol, terbutaline (beta–2 more than beta–1)
210
Sympathomimetics selective for: beta–2
–Albuterol, terbutaline (beta–2 more than beta–1)
–Isoproterenol (beta–1 = beta–2)
–Dobutamine (beta–1 more than beta–2)
211
Sympathomimetics selective for: None (general agonists)
–Amphetamine
–Ephedrine
–Cocaine
–Epinephrine (alpha and beta)
212
Effect on blood pressure: Norepinephrine
Increases from 100 to 150
Mechanism:
1. Stimulates alpha more than beta
2. Systolic blood pressure goes up along with but more than diastolic blood pressure
3. Mean blood pressure rises
213
Effect on blood pressure: Epinephrine
Mean pressure stays at 100, with wide pulse–pressure (100)
Mechanism:
1. Nonselectively stimulates both alpha and beta receptors
2. Alpha receptors: Systolic blood pressure goes up
AND
beta receptors: Diastolic blood pressure goes down
3. Mean blood pressure stays the same
4. Pulse pressure is wide
214
Effect on blood pressure: Isoproterenol
Mean blood pressure goes down to 50, but pulse–pressure becomes wider (~75).
Mechanism:
1. Stimulates beta more than alpha.
2. Diastolic drops along with but more than systolic blood pressure
3. Mean blood pressure drops with wide pulse pressure
215
Effect on heart rate: Norepinephrine
1. Mean pressure goes up
| 2. Goes down to 50 (reflex bradycardia)
216
Effect on heart rate: Epinephrine
1. Beta–1 receptors are stimulated
| 2. Increases to 100
217
Effect on heart rate: Isoproterenol
1. Beta–1 receptors are stimulated more than alpha receptors
| 2. Increases to ~125
218
Sympathomimetic of choice for: Anaphylaxis
Epinephrine
219
Sympathomimetic of choice for: Open–angle glaucoma
Epinephrine
220
Sympathomimetic of choice for: Asthma
–Albuterol
–Terbutaline
–Epinephrine
221
Sympathomimetic of choice for: Hypotension
–Epinephrine
–Norepinephrine (though with decreased renal perfusion)
–Ephedrine
222
Sympathomimetic of choice for: AV block
Isoproterenol
223
Sympathomimetic of choice for: Shock
–Dopamine (increased renal perfusion)
| –Dobutamine
224
Sympathomimetic of choice for: Heart failure
Dopamine
225
Sympathomimetic of choice for: Heart failure cardiac stress testing
Dobutamine
226
Sympathomimetic of choice for: Narcolepsy
Amphetamine
227
Sympathomimetic of choice for: Obesity
Amphetamine
228
Sympathomimetic of choice for: Attention defecit disorder
Amphetamine
229
Sympathomimetic of choice for: Nasal decongestion
–Ephedrine
| –Phenylephrine
230
Sympathomimetic of choice for: Urinary incontinence
Ephedrine
231
Sympathomimetic of choice for: Dilation of pupils
Phenylephrine
232
Sympathomimetic of choice for: desired vasoconstriction
–Phenylephrine
| –Cocaine
233
Sympathomimetic of choice for: Local anesthesia
Cocaine
234
Sympathomimetic of choice for: Treatment of hypertension
Clonidine and alpha–methyldopa (especially for those with renal disease, no decrease in blood flow to kidney)
235
alpha–blockers: drug list
```
Non–selective
–Irreversible: Phenoxybenzamine
–Reversible: Phentolamine
alpha–1 selective
–Prazosin
–Terazosin
–Doxazosin
alpha–2 selective
–Mirtazapine
```
236
Phenoxybenzamine: Mechanism
irreversible nonselective alpha–blocker
237
Phentolamine: Mechanism
reversible nonselective alpha–blocker
238
Prazosin: Mechanism
alpha–1 blocker
239
Terazosin: Mechanism
alpha–1 blocker
240
Doxazosin: Mechanism
alpha–1 blocker
241
Mirtazapine: Mechanism
alpha–2 blocker
242
Nonselective alpha blockers: Application
Pheochromocytoma
243
alpha–2 blockers: Application
Depression
244
alpha–1 blockers: Application
–Hypertension
| –Urinary retention in BPH
245
Nonselective alpha blockers: Toxicity
–Orthostatic hypotension
| –Reflex tachycardia
246
alpha–2 blockers: Toxicity
–Sedation
–Increase in serum cholesterol
–Increase in appetite
247
alpha–1 blockers: Toxicity
–1st–dose orthostatic hypotension
–dizziness
–headache
248
Which class of alpha blockers should you use for: Pheochromocytoma
Nonselective alpha blockers
249
Which class of alpha blockers should you use for: Hypertension
alpha–1 blockers
250
Which class of alpha blockers should you use for: Urinary retention in bph
alpha–1 blockers
251
Which class of alpha blockers should you use for: Depression
alpha–2 blockers (Mirtazapine)
252
beta–blockers: mechanism in control of: hypertension
–decreased cardiac output
| –decreased renin secretion
253
beta–blockers: mechanism in control of: angina pectoris
1. decreased heart rate and contractility
| 2. result: decreased O2 consumption
254
beta–blockers: mechanism in control of: MI
decrease in mortality (no mechanism given)
255
beta–blockers: mechanism in control of: supraventricular tachycardia
decreased AV conduction velocity
256
beta–blockers: mechanism in control of: congestive heart failure
slows progression (no mechanism given)
257
beta–blockers: mechanism in control of: glaucoma
decreased secretion of aqueous humor
258
which beta–blockers are used in control of: supraventricular tachycardia
–Propranolol
| –Esmolol
259
which beta–blockers are used in control of: glaucoma
Timolol
260
beta–blockers: toxicity: non–CV, non–CNS
–Impotence
| –Asthma exacerbation
261
beta–blockers: toxicity: Cardiovascular
–bradycardia
–AV block
–congestive heart failure
262
beta–blockers: toxicity: CNS
–sedation
| –sleep alterations
263
Non–selective beta blockers
```
–Propranol
–Timolol
–Nadolol
–Pindolol (partial agonist)
–Labetalol (partial agonist)
```
264
beta–1–selective beta–blockers
A BEAM of beta–1 blockers
```
–Acebutolol (partial agonist)
–Betaxolol
–Esmolol (short acting)
–Atenolol
–Metoprolol
```
265
Antidote for: Acetaminophen
N–acetylcysteine
266
Antidote for: Salicylates
1. Alkalinize urine
| 2. Dialysis
267
Antidote for: Anticholinesterases
–Atropine
| –Pralidoxime
268
Antidote for: Organophosphates
–Atropine
| –Pralidoxime
269
Antidote for: Anti–muscarinic anti–cholinergic agents
Physostigmine salicylate
270
Antidote for: beta–blockers
Glucagon
271
Antidote for: Digitalis
1. Stop digitalis
2. Normalize potassium
3. Lidocaine
4. anti–digitalis Fab fragments
5. Magnesium
272
Antidote for: Iron
Deferoxamine
273
Antidote for: Lead
1st line: CaEDTA & Dimercaprol
2nd line?: Penicillamine
Kids: Succimer
(First Aid lists Penicillamine in the antidotes section, but not in the section below, hence the ?)
274
Antidote for: Arsenic
–Dimercaprol (BAL)
–Succimer
–Penicillamine
275
Antidote for: Gold
–Dimercaprol (BAL)
–Succimer
–Penicillamine
276
Antidote for: Mercury
–Dimercaprol (BAL)
| –Succimer
277
Antidote for: Copper
Penicillamine
278
Antidote for: Cyanide
–Nitrite
–Hydroxocobalamin
–Thiosulfate
279
Antidote for: Methemoglobin
Methylene blue
280
Antidote for: Carbon Monoxide
–100% Oxygen
| –Hyperbaric Oxygen
281
Antidote for: Methanol
–Ethanol
–Dialysis
–Fomepizole
282
Antidote for: Ethylene glycol (antifreeze)
–Ethanol
–Dialysis
–Fomepizole
283
Antidote for: Opioids
Naloxone/naltrexone
284
Antidote for: Benzodiazepines
Flumazenil
285
Antidote for: Tricyclics
NaHCO3 (nonspecific)
286
Antidote for: Heparin
Protamine
287
Antidote for: Warfarin
–Vitamin K
| –Fresh frozen plasma
288
Antidote for: tPA
Aminocaproic acid
289
Antidote for: streptokinase
Aminocaproic acid
290
For what drug(s) is the following an antidote?: N–acetylcysteine
Acetaminophen
291
For what drug(s) is the following an antidote?:
1. Alkalinize urine
2. Dialysis
Salicylates
292
For what drug(s) is the following an antidote?: Atropine
–Anticholinesterases
| –Organophosphates
293
For what drug(s) is the following an antidote?: Pralidoxime
–Anticholinesterases
| –Organophosphates
294
For what drug(s) is the following an antidote?: Physostigmine salicylate
Antimuscarinic, anticholinergic agents
295
For what drug(s) is the following an antidote?: Glucagon
beta–blockers
296
For what drug(s) is the following an antidote?: Deferoxamine
Iron
297
For what drug(s) is the following an antidote?: CaEDTA
Lead
298
For what drug(s) is the following an antidote?: Dimercaprol
Dimercaprol is GLAMorous
–Gold
–Lead
–Arsenic
–Mercury
299
For what drug(s) is the following an antidote?: Succimer
–Lead
–Arsenic
–Mercury
–Gold
300
For what drug(s) is the following an antidote?: Penicillamine
–Lead
–Copper
–Arsenic
–Gold
301
For what drug(s) is the following an antidote?: Nitrite
Cyanide
302
For what drug(s) is the following an antidote?: Hydroxocobalamin
Cyanide
303
For what drug(s) is the following an antidote?: Thiosulfate
Cyanide
304
For what drug(s) is the following an antidote?: Methylene blue
Methemoglobin
305
For what drug(s) is the following an antidote?: Oxygen
Carbon monoxide (Oxygen should be 100% or hyperbaric)
306
For what drug(s) is the following an antidote?: Ethanol
–Methanol
| –Ethylene glycol (antifreeze)
307
For what drug(s) is the following an antidote?: Dialysis
–Methanol
–Ethylene glycol (antifreeze)
–Salicylates
308
For what drug(s) is the following an antidote?: Fomepizole
–Methanol
| –Ethylene glycol (antifreeze)
309
For what drug(s) is the following an antidote?: Naloxone/Naltrexone
Opioids
310
For what drug(s) is the following an antidote?: Flumazenil
Benzodiazepines
311
For what drug(s) is the following an antidote?: NaHCO3
Tricyclic Antidepressants
312
For what drug(s) is the following an antidote?: Protamine
Heparin
313
For what drug(s) is the following an antidote?: Vitamin K
Warfarin
314
For what drug(s) is the following an antidote?: Fresh, frozen plasma
Warfarin
315
For what drug(s) is the following an antidote?: Aminocaproic acid
–tPA
| –streptokinase
316
Lead poisoning: Signs and symptoms
LLEEAADD
```
–Lead Lines on:
––gingivae
––epiphyses of long bones on x–ray
–Encephalopathy
–Erythrocyte basophilic stippling
–Abdominal colic
–sideroblastic Anemia
–wrist Drop
–foot Drop
```
317
Lead poisoning: 1st line treatment for adults
Both:
–Dimercaprol
–EDTA
318
Lead poisoning: 1st line treatment for children
Succimer
| It "sucks" to be a kid who eats lead
319
Causal agent for the following reaction: Atropine–like side effects
Tricyclic Antidepressants
320
Causal agent for the following reaction: Cardiac toxicity
–Doxorubicin (Adriamycin)
| –Daunorubicin
321
Causal agent for the following reaction: Coronary vasospasm
Cocaine
322
Causal agent for the following reaction: Cutaneous flushing
–Niacin
–Ca2+–channel blockers
–Adenosine
–Vancomycin
323
Causal agent for the following reaction: Torsades des pointes
–Class III antiarrhythmics (sotalol)
–Class IA antiarrhytmics (quinidine)
–Cisapride
324
Causal agent for the following reaction: Agranulocytosis
–Clozapine
–Carbamazepine
–Colchicine
325
Causal agent for the following reaction: Aplastic anemia
–Chloramphenicol
–Benzene
–NSAIDs
326
Causal agent for the following reaction: Gray baby syndrome
Chloramphenicol
327
Causal agent for the following reaction: Hemolysis in G6PD–deficient patients
G6PD IS PAIN
```
–Isoniazid
–Sulfonamides
–Primaquine
–Aspirin
–Ibuprofen
–Nitrofurantoin
```
328
Causal agent for the following reaction: Thrombotic complications
oral contraceptive pills
329
Causal agent for the following reaction: Cough
ACE inhibitors (not ARBs)
330
Causal agent for the following reaction: Pulmonary fibrosis
–Bleomycin
–Amiodarone
–Busulfan
331
Causal agent for the following reaction: Acute cholestatic hepatitis
Macrolides
332
Causal agent for the following reaction: Focal to massive hepatic necrosis
–Halothane
–Valproic acid
–Acetaminophen
–Amanita phalloides
333
Causal agent for the following reaction: Hepatitis
INH
334
Causal agent for the following reaction: Pseudomembranous colitis
–Clindamycin
| –Ampicillin
335
Causal agent for the following reaction: Adrenocortical insufficiency
Glucocorticoid withdrawal (HPA suppression)
336
Causal agent for the following reaction: Gynecomastia
Some Drugs Create Extra–Awesome Knockers
```
–Spironolactone
–Digitalis
–Cimetidine
–estrogens
–Alcohol (chronic use)
–Ketoconazole
```
337
Causal agent for the following reaction: Hot flashes
Tamoxifen
338
Causal agent for the following reaction: Gingival hyperplasia
Phenytoin
339
Causal agent for the following reaction: Osteoporosis
–Corticosteroids
| –Heparin
340
Causal agent for the following reaction: Photosensitivity
SAT for a photo
–Sulfonamides
–Amiodarone
–Tetracycline
341
Causal agent for the following reaction: SLE–like syndrome
(It's not HIPP to have lupus)
–Hydralazine
–INH
–Procainamide
–Phenytoin
342
Causal agent for the following reaction: Tendonitis, tendon rupture, and cartilage damage
Fluoroquinolones (kids)
343
Causal agent for the following reaction: Fanconi's syndrome
Expired tetracycline
344
Causal agent for the following reaction: Interstitial nephritis
Methicillin
345
Causal agent for the following reaction: Hemorrhagic cystitis
–Cyclophosphamide
| –Ifosfamide
346
Causal agent for the following reaction: Cinchonism
–Quinidine
| –Quinine
347
Causal agent for the following reaction: Diabetes insipidus
–Lithium
| –Demeclocycline
348
Causal agent for the following reaction: Seizures
–Bupropion
| –Imipenem/cilastatin
349
Causal agent for the following reaction: Tardive dyskinesia
Antipsychotics
350
Causal agent for the following reaction: Disulfiram–like reaction
–Metronidazole
–Certain cephalosporins
–Procarbazine
–Sulfonylureas
351
Causal agent for the following reaction: Nephrotoxicity/neurotoxicity
Polymyxins
352
Causal agent for the following reaction: Nephrotoxicity/ototoxicity
–Aminoglycosides
–Loop diuretics
–Cisplatin
353
P–450 Inducers
Queen Barb takes Phen–phen and Strictly Refuses Greasy Carbs
```
–Quinidine (CYP3A4)
–Barbiturates
–Phenytoin
–St. John's Wort
–Rifampin
–Griseofulvin
–Carbamazepine
```
354
P–450 Inhibitors
Inhibitors Quickly Stop Cyber–Kids from Eating Grapefruit
```
–Isoniazid
–Quinidine (CYP2D6)
–Sulfonamides
–Cimetidine
–Ketoconazole
–Erythromycin
–Grapefruit juice
```
355
P–450 inducer or inhibitor: Quinidine
Inhibitor: CYP2D6 (more prominent)
Inducer: CYP3A4
356
P–450 inducer or inhibitor: Barbiturates
Inducer
357
P–450 inducer or inhibitor: Phenytoin
Inducer
358
P–450 inducer or inhibitor: Rifampin
Inducer
359
P–450 inducer or inhibitor: Griseofulvin
Inducer
360
P–450 inducer or inhibitor: Carbamazepine
Inducer
361
P–450 inducer or inhibitor: St. John's wort
Inducer
362
P–450 inducer or inhibitor: Isoniazid
Inhibitor
363
P–450 inducer or inhibitor: Sulfonamides
Inhibitor
364
P–450 inducer or inhibitor: Cimetidine
Inhibitor
365
P–450 inducer or inhibitor: Ketoconazole
Inhibitor
366
P–450 inducer or inhibitor: Erythromycin
Inhibitor
367
P–450 inducer or inhibitor: Grapefruit juice
Inhibitor
368
Active metabolite of ethylene glycol
Oxalic acid
369
Active metabolite of methanol
–Formaldehyde
| –Formic acid
370
Active metabolite of ethanol
Acetaldehyde
371
Pathway and toxicities of metabolism of: ethylene glycol
1. Ethylene glycol is converted by alcohol dehydrogenase to
2. Oxalic acid causes:
–Acidosis
–Nephrotoxicity
372
Pathway and toxicities of metabolism of: methanol
1. Methanol is converted by alcohol dehydrogenase to
2. Formaldehyde and formic acid which cause:
–Severe Acidosis
–Retinal damage
373
Pathway and toxicities of metabolism of: ethanol
1. Ethanol is converted by alcohol dehydrogenase to
2. Acetaldehyde which causes:
–Nausea
–Vomiting
–Headache
–Hypotension
374
What enzyme is inhibited by disulfiram?
Acetaldehyde dehydrogenase
375
What inhibits acetaldehyde dehydrogenase?
Disulfiram
376
Clinical uses/toxicities for: Echinacea
Use: Common cold
Toxicities:
–GI distress
–dizziness
–headache
377
Clinical uses/toxicities for: Ephedra
Uses: As for ephedrine
```
Toxicities:
–CNS and cardiovascular stimulation
At high doses:
–Arrhythmias
–Stroke
–Seizure
```
378
Clinical uses/toxicities for: Feverfew
Use: Migraine
Toxicities:
–GI distress
–Mouth ulcers
–Antiplatelet actions
379
Clinical uses/toxicities for: Ginkgo
Use: Intermittent claudication
```
Toxicities:
–GI distress
–anxiety
–insomnia
–headache
–antiplatelet actions
```
380
Clinical uses/toxicities for: Kava
Use: Chronic anxiety
```
Toxicities:
–GI distress
–sedation
–ataxia
–hepatotoxicity
–phototoxicity
–dermatotoxicity
```
381
Clinical uses/toxicities for: Milk thistle
Use: Viral hepatitis
Toxicities: Loose stools
382
Clinical uses/toxicities for: Saw palmetto
Use: Benign prostatic hyperplasia
Toxicities:
–GI distress
–Decreased libido
–Hypertension
383
Clinical uses/toxicities for: St. John's wort
Use: Mild to moderate depression
Toxicities:
–GI distress and phototoxicity
–serotonin syndrome with SSRIs
–induces P–450 system
384
Clinical uses/toxicities for: DHEA
Uses: Symptomatic improvement in females with SLE or AIDS
Toxicities:
–Androgenization (premenopausal women)
–Estrogenic effects (post menopausal)
–Feminization (young men)
385
Clinical uses/toxicities for: Melatonin
Use:
–Jet lag
–Insomnia
Toxicities:
–Sedation
–Suppresses midcycle LH
–Hypoprolactinemia
386
Category for drug names ending with: –afil
Erectile dysfunction (eg Sildenafil)
387
Category for drug names ending with: –ane
Inhalational general anesthetic (eg Halothane)
388
Category for drug names ending with: –azepam
Benzodiazepine (eg Diazepam)
389
Category for drug names ending with: –azine
Phenothiazine (neuroleptic, antiemetic) (eg Chlorpromazine)
390
Category for drug names ending with: –azole
Antifungal (eg Ketoconazole)
391
Category for drug names ending with: –barbital
Barbiturate (eg Phenobarbital)
392
Category for drug names ending with: –caine
Local anesthetic (eg Lidocaine)
393
Category for drug names ending with: –cillin
Penicillin (eg Methicillin)
394
Category for drug names ending with: –cycline
Antibiotic, protein synthesis inhibitor (Tetracycline)
395
Category for drug names ending with: –ipramine
Tricyclic Antidepressant (eg Imipramine)
396
Category for drug names ending with: –navir
Protease inhibitor (eg Saquinavir)
397
Category for drug names ending with: –olol
beta–blocker (eg Propranolol)
398
Category for drug names ending with: –operidol
Butyrophone (neuroleptic) (eg Haloperidol)
399
Category for drug names ending with: –oxin
Cardiac glycoside (inotropic agent) (eg Digoxin)
400
Category for drug names ending with: –phylline
Methylxanthine (eg Theophylline)
401
Category for drug names ending with: –pril
ACE inhibitor (eg Captopril)
402
Category for drug names ending with: –terol
beta–2 agonist (eg Albuterol)
403
Category for drug names ending with: –tidine
H2 antagonist (eg Cimetidine)
404
Category for drug names ending with: –triptyline
Tricyclic antidepressant (eg Amitryptyline)
405
Category for drug names ending with: –tropin
Pituitary hormone (eg Somatotropin)
406
Category for drug names ending with: –zosin
alpha–1 antagonist (eg Prazosin)
407
Common ending for drug names in the following category: Erectile dysfunction
–afil (eg Slidenafil)
408
Common ending for drug names in the following category: Inhalational general anesthetic
–ane (eg Halothane)
409
Common ending for drug names in the following category: Benzodiazepine
–azepam (eg Diazepam)
410
Common ending for drug names in the following category: Phenothiazine (neuroleptic, antiemetic)
–azine (eg Chlorpromazine)
411
Common ending for drug names in the following category: Antifungal
–azole (eg Ketoconazole)
412
Common ending for drug names in the following category: Barbiturate
–barbital (eg Phenobarbital)
413
Common ending for drug names in the following category: Local anesthetic
–caine (eg Lidocaine)
414
Common ending for drug names in the following category: Penicillin
–cillin (eg Methicillin)
415
Common ending for drug names in the following category: Bacterial protein synthesis inhibitor
–cycline (eg Tetracycline)
416
Common ending for drug names in the following category: Tricyclic antidepressant
–ipramine (Imipramine)
| –triptyline (Amitriptyline)
417
Common ending for drug names in the following category: Protease inhibitor
–navir (Saquinavir) (Mnemonic: Navir tease a pro)
418
Common ending for drug names in the following category: beta–antagonist
–olol (Propranolol)
419
Common ending for drug names in the following category: butyrophenone (neuroleptic)
–operidol (Haloperidol)
420
Common ending for drug names in the following category: Cardiac glycoside
–oxin (Digoxin)
421
Common ending for drug names in the following category: Methylxanthine
–phylline (eg Theophylline)
422
Common ending for drug names in the following category: ACE inhibitor
–pril (Captopril)
423
Common ending for drug names in the following category: beta–2 agonist
–terol (eg Albuterol)
424
Common ending for drug names in the following category: H2 antagonist
–tidine (eg Cimetidine)
425
Common ending for drug names in the following category: Pituitary hormone
–tropin (eg Somatotropin)
426
Common ending for drug names in the following category: alpha–1 antagonist
–zosin (eg Prazosin)
