Pharm Flashcards
1
Q
Effect of epinephrine at low and high dose
A
a-1, B1, B2
Low dose: Beta-2 vasodilation stronger (decrease DBP blood pressure)
High dose: alpha-1 constriction stronger (increase DBP blood pressure)
2
Q
To prevent the low dose effects of epinephrine (lowered BP), what can you do?
A
Administer a beta blocker so everything goes to alpha constriction instead of Beta 1 (tachycardia) and beta 2 (vasodilation)
3
Q
Succinylcholine side effects
A
- hyperkalemia (arrhythmia)
- malignant hyperthermia with halothane
- bradycardia
4
Q
Who is predisposed to succinylcholine toxicity of hyperK
A
pts with burns/myopathies, anything that would cause cell lysis
–Also pts with denervating dzs (quadriplegics)
5
Q
Baclofen
A
GABAb muscle relaxant
6
Q
Dantrolene
A
Acts on ryanodine receptors, preventing release of calcium
–good for malignant hyperthermia
7
Q
atracurium side effects
A
histamine release causing flushing, bronchoconstriction, hypotension.
-Seizures
8
Q
If you’re worried about hyperkalemia when giving succinylcholine what is a good alt med
A
vecuronium/rocuronium these are non-depolarizing AchR blockers
9
Q
affinity of enzyme for substrate
A
=1/Km
10
Q
Vmax is proportional to
A
enzyme concentration
11
Q
Michaelis-mentin kinetics means
A
enzyme rxn follows a hyperbolic curve
12
Q
Which types of drugs are metabolized by the liver?
A
lipophilic drugs
–can be metabolized and excreted in bile/liver
13
Q
Bioavailability of the drug is calculated through
A
Area under the curve, comparing oral with IV
14
Q
Side effect of nitroglycerin
A
headaches and facial flushing from vasodilation of skin and meninges
15
Q
Metformin is contraindicated in patients with
A
renal failure. Because lactic acid accumulates. In reality, metformin is contraindicated in anyone who might have lactic acidosis (alcoholic, septic, CHF)
16
Q
which drugs require routine thyroid testing
A
lithium and amiodarone
17
Q
Scopolamine mech
A
selective muscarinic ACh antagonist that reduces the effect of the cholinesterase inhibitor
18
Q
Pilocarpine mech
A
muscarinic agonist
19
Q
Efficacy:
A
Intrinsic ability of a drug to have a desired outcome, expressed by MAXIMUM activity Emax
20
Q
Potency
A
Dose of a drug required to produce a given effect. Determined by AFFINITY (1/Km) and the AMOUNT of drug able to reach target.
21
Q
Ed50
A
Lower the Ed50, high potency
–Dose of drug required to produce half of the full response
22
Q
Phenylephrine
A
An alpha agonist. Vasopressor used for shock
23
Q
Prazosin
A
Selective alpha-1 BLOCKER for HTN and benign prostatic hyperplasia. Thus, a vasodilator
24
Q
Dobutamine
A
Major B1, some B2 and A1
- Increased contractility
- Small increase in HR
25
Side effect of dobutamine
Increased cardiac conduction velocity=arrhythmias
- -Also, increases myocardial oxygen consumption (higher heart rate and contractility)
- -Nitrates increase heart rate, but also decreases preload, reducing myo o2 consumption
26
Competitive inhibitor effect on Km
Increased
27
noncompetitive inhibitor effect on Km
none
28
which type of inhibitor will decrease potency?
competitive inhibitor
29
which type of inhibitor will affect efficacy?
noncompetitive inhibitor
30
Calculate volume of distribution
amount of drug/plasma drug concentration
31
t1/2 life
=0.7*Vd/CL
32
which type of drugs stay in the blood
large, charge molecules
33
which drugs go to ECF
small hydrophilic molecules
34
which drugs go to all tissues
small lipophilic molecules
35
clearance equation
VdxKe
36
Loading dose
Cp x Vd/F
37
Maintenance dose
Cp x CL/F
38
Which drugs have zero order elimination?
phenytoin
ethanol
aspirin
39
Pt overdoses with weak acid what do you do?
Give bicarb--charges molecule for elimination
40
Pt overdoses with weak base. What do you do?
Give ammonium chloride acid NH4Cl--Charges molecule for elimination
41
example of weak acid drugs
aspirin
phenobarbital
methotrexate
42
example of weak base drug
amphetamines
43
Phase I metabolism
reduction, oxidation, hydrolysis with cytochrome P-450. Makes drug more polar but still active
44
Phase II metabolism
glucuronidation, acetylation, sulfation
| --makes polar and inactive metabolites
45
slow acetylators
slow metabolizers of drug. increase risk of side effects
46
First order elimination
constant fraction of drug is excreted
47
Therapeutic index
LD50/ED50
48
Partial agonist effect
decrease efficacy,
| effect on potency is variable
49
therapeutic window is the range btw
minimum effective to minimum toxic dose
50
Sympathetic sweat glands innervated by
AchM
51
Sympathetic renal vasculature innervated by
D/D1
52
Adrenal medulla innervated by
Nicotinic Ach receptor. Does NOT go through the sympathetic chain!
53
Nicotinic ACh receptors are what type of receptors?
Ligand-gated Na/K channels
54
Nn vs Nm receptors?
Nn are nicotinic receptors found in autonomic ganglia Nm are found in neuromuscular junctions
55
What type of receptors are muscarinics?
G protein receptors with 2nd messengers
56
m1
CNS and enteric nervous system
57
m2
decrease heart rate/contractility
58
M3
```
increase exocrine secretions, peristalsis
bladder contraction
bronchoconstriction
ciliary muscle contraction
pupillary sphincter contraction
```
59
alpha 1
vascular contraction
dilation pupillary dilator
intestinal/bladder sphincter contraction
60
alpha2
- CNS mediated decrease in blood pressure
- Decrease aqueous humor fluid production
- inhibition of lipolysis
- inhibition of adrenergic and cholinergic release
- increased platelet aggregation
61
beta 1
causes renin release
62
beta 2
```
vasodilation
bronchodilation
increased heart rate/contractility
ciliary muscle relaxation
aqueous humor production
decreased uterine tone
```
63
D1 receptor
relaxes renal vascular smooth muscle
64
D2 receptor
brain transmitter
65
H1
bronchial mucus
contraction of bronchioles
pruritis
66
H2
gastric acid secretion
67
Vasopressin1
vascular smooth muscle contraction
68
vasopressin2
Increased permeability in collecting tubules
69
Gprotein class of D1, D2
s
| i
70
Gprotein class of H1, H2
q
| s
71
Gprotein class of V1, V2
q
| s
72
Which receptors work through Gq?
```
HAVe 1M&M
H1
A1
V1
M1
M3
```
73
which receptors work through Gi?
M2
A2
D2
74
Describe the Gq pathway
Phospholipase C activated
- converts lipids to PIP2
- PIP2-->DAG and IP3
- IP3 increases [Ca]in
- DAG activates protein kinase C
75
Describe the Gs pathway
Activation of adenylyl cyclase
- incrase cAMP
- Activation of protein kinase A
- [Ca] increases
- myosin light chain kinase increases
76
what controls release of NE?
```
NE negative feedback to alpha-2
AII receptor (+)
M2 receptor (-)
```
77
acetylcholine is made from
AcetylCoA + Choline ChAT
78
NE is made from
Tyrosine-->dopa-Dopamine--?NE
79
Hemicholinium
blocks choline entry into cholinergic neuron
80
vesamicol
inhibits synthesis of Ach
81
Botulinum
prevents release of ACh
82
metyrosine
inhibits tyrosine-->dopa
83
reserpine
inhibits dopamine-->NE
84
Cocaine, TCA, amphetamines
Inhibit NE reuptake
85
amphetamines
also iincrease release of NE inaddition to reducing reuptake
86
guanethidine
inhibits release of NE
87
Bethanechol
ACh agonist
| -Activates bowel and bladder for postoperative ileus and urinary retention
88
Carbachol
Ach agonist
89
Pilocarpine
Ach agonist
90
methacholine
Ach agonist
91
carbachol indication
glaucoma
| pupillary contraction
92
pilocarpine indication
open and closed angle glaucoma. Contracts ciliary muscle and pupillary sphincter
Causes sweat, tears, and saliva
93
Neostigmine
AChE inhibitor
- MG
- reversal of NMJ blockate
- postoperative/neurogenic ileus
94
Does neostigmine penetrate CNS?
no
95
pyridostigmine
long acting AChE inhibitor for MG
96
Does pyridostigmine cross BBB?
no
97
Edrophonium
used to diagnose myasthenia gravis. short acting AChEI
98
physostigmine indication
atropine poisoning. crosses BBB to reverse ACh block
99
Donepezil mechanism
AChE inhibitor. Increases Ach in the brain for alzheimer's patients
100
organophosphates cause
AChE inhibitor poisoning. Causes too much Acetylcholine!
Sx:
DUMBBELSS
Diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of muscle/CNS, Lacrimation, Sweating, Salivation
101
Antidote for organophosphate poisoning
atropine and pralidoxime
102
What is atropine used for?
pupil dilation, relaxation of the ciliary muscle
| Also to treat bradycardia
103
Atropine tox
```
HOT as ahare
Dry as a bone
MAD as a hatter
RED as a beet
BLIND as a bat
```
104
What do you NOT want to give to someone with acute close angle glaucoma?
Anything that will cause mydriasis (pupil to dilate)
- alpha 1 activator
- epinephrine
- atropine (blocks M3 which activates pupillary sphincter)
105
atropine causes what in men with BPH?
urinary retention
106
atropine causes what in infants?
hyperthermia
107
What is the problem with giving a D2 blockade?
This is how antipsychotics work!
- -will cause depletion of dopamine
- -drug induced parkinsonism (extrapyramidal effects of typical antipsychotics)
108
How do you treat drug induced parkinsonism?
Give anticholinergics like benztropine or amantadine. These inhibit dopamine reuptake
109
What can you use to dilate the eye?
atropine
homatropine
tropicamide
110
mechanism scopolamine
Muscarinic antagonist
111
Ipratropium, tiotropium mechanism
muscarinic antagonist
112
oxybutynin mechanism
muscarinic antagonist
113
glycopyrrolate mechanism
muscarinic antagonist
114
oxybutynin use
reduce urgency in mild cystitis
115
glycopyrrolate use
parenteral: reduce airway secretions before surgery
Oral: drooling or a peptic ulcer
116
epinephrine indications
glucoma (open angle), asthma, hypotension
117
alpha 1 on the eye
pupillary dilator
118
B2 on the eye
ciliary muscle relaxation, aqueous humor production
119
isoproterenol
activates B1 and B2
120
use: isoproterenol
torsade de point and bradyarrhythmia
121
Norepi activates
a1, a2, b1 (less so)
| -mostly a1,a2
122
norepi use
hypotension
123
dopamine use
shock
124
high dose dopamine activates
alpha 1 and alpha 2
125
low dose dopa activates
D1. good for maintaining renal perfusion when treating shock patients
126
medium dose dopa activates
B1, B2
127
dobutamine activates
Mostly B1
128
indications dobutamine
heart failure, cardiac stress stesting
129
phenylephrine indications
hypotension
mydriasis
rhinitis (decongestant0
130
terbutaline activates
B2, some B1
131
terbutaline indications
premature uterine contractions
132
ritodrine activates
B2
133
Applications of Ritodrine
Reduces premature uterine contractions
134
amphetamine and ephdrine mechanism
releases stored catecholamines.
135
ephedrine indications
nasal decongestant
| Urinary incontinence
136
What should you never give to someone who has overdosed on cocaine?
beta blockers. Leads to unopposed alpha1 activation
137
effect of Norepi on BP and HR
Increase in BP, reflex decrease in HR (mostly alpha-1)
138
effect of isoproterenol on BP and HR
Increase in HR (B1)
| Drop in BP (Mostly B2)
139
When to use clonidine/a-methyldopa?
hypertension in peeps with renal disease (preserves flow to kidneys)
140
How does clonidine work?
Centrally at the alpha 2 agonists to decrease sympathetic outflow
141
Indication for phenoxybenzamine?
pheos
| --before removing tumor--it's an IRREVERSIBLE alpha blocker!
142
Indication for phentolamine?
pts in HTN crisis from eating tyramine while taking MAO-I
| --it's reversible :)
143
What does tyramine do?
It is a catecholamine releasing agent
144
terazosin, doxazosin, tamsulosin
| prazosin
alpha-1 selective blockers
145
Indication for tamsulosin
Hypertension, urinary retention in BPH
146
side effect of alpha blockers
first dose orthostatic hypotension
147
alpha 2 selective blocker
mirtazapine
148
indications of mirtazapine
depression.
149
side effect of mirtazapine
increased appetite and cholesterol
150
Effect of epi +alpha blockade
decreased blood pressure (b2 effect takes over)
151
effect of phenylephrine + alpha blockade
Normal blood pressure
152
timolol
Decreases secretion of aqueous humor in glaucoma
153
Who do you NOT want to give a beta blocker to?
asthmatics (if non-selective)
| diabetics (beta 2 increases insulin secretion. blocking it will decrease insulin secretion)
154
side effect of beta blockers
impotence, bradycardia, sedation
155
which are the selective beta blockers?
```
metoprolol
atenolol
acebutolol
betaxolol
esmolol
(A BEAM of b1blockers)
```
156
Non-selective beta blockers
propranolol
timolol
nadolol
pindolol
157
which beta blockers also work as partial agonists?
pindolol and acebutolol
158
which drugs are nonselective alpha and beta blockers?
carvedilol and acebutolol
159
Treatment for salicylate overdose
NaHCO3
160
Amphetamine overdose
NH4Cl
161
Betablocker overdose
glucagon
162
atropine overdose
physostigmine
163
Treatment for lead poisoning
CaEDTA
dimercaprol
succimer
penicillamine
164
Treatment for mercury overdose
dimercaprol, succimer
165
Treatment for arsenic/gold
dimercaprol, succimer, penicillamine
166
Treatment for copper overdose
penicillamine
167
Treatment for methemoglobin
vitamin C or methylene blue
168
Treatment for methanol/ethylene glycol
fomepizole, dialysis
169
Treatment for TCA overdose
NaHCO3 (plasma alkalinization)
170
Treatment of tPA/streptokinase, urokinase overdose?
aminocaproic acid
171
Treatment of theophylline overdose
Beta blocker
172
P-45o inducers
```
modafinil
barbiturates
st. john's wort
phenytoin
rifampin
griseofulvin
carbamazepine
chronic alcohol use
```
Momma barb steals Phenphen and Refuses Greasy Carbs Chronically
173
P-450 inhibitors
MAGIC RACKS in GQ
```
macrolides
amiodarone
grapefruit
Isoniazid
cimetidine
ritonavir
acute alcohol abuse
ciprofloxasin
ketoconazole
sulfonamides
gemfibrozil
quinidine
```
174
Sulfa drugs
```
P FACTSSS
probenicid
furosemide
acetazolamide
celecoxib
thiazides
sulfonadmide antibiotics
sulfazalazine
sulfonylureas
```
175
consequences of sulfa allergies
Stevens Johnson, Hemolytic anemia
| thrombocytopenia, agranulocytosis
176
remember to:
GO THROUGH DRUG RXNS on PG 240!!
177
Terbinafine mechanism
inhibits squalene 2 3 epoxidase, decreasing ergosterold synthesis
178
ampho mechanism
binds to ergosterol in fungal cell MEMBRANE forming pores
179
griseofulvin mechanism
binds microtubules and inhibits mitosis
180
caspofungin mechanism
binds 1, 3 beta D glucan and blocks glucan synthesis
181
flucytosine mechanism
inhibits DNA and RNA synthesis in fungal cells. Used in combo with ampho B for cryptococcus
182
Bosentan mechanism
Blocks endothelin receptors. Used to treat primary pulmonary arterial hypertension
183
Entanercept
monoclonal antibody that binds TNF-alpha used for RA and psoriasis
184
Drugs that induce CYP 450
```
Carbamazepine
phenytoin
phenobarbital
griseofulvin
rifampin
```
185
Drugs that inhibit CYP 450
```
Grapefruit
Ritonavir
Azoles
Cipro
Cimetidine
Isoniazid
Erythromycin
```
186
which drugs prolong the QT interval?
```
Class III antiarrythmics (Potassium Channel blockers)
Amiodarone
Ibutilide
Dofitilide
Sotalol
```
187
short acting benzos
midazolam
| triazolam
188
how do u prevent flushing associated with Nitroglycerin?
administer aspirin beforehand. Reduces prostaglandins. . nicotinic acid also helps
189
caspaicin works by
decreasing the level of substance P in the PNS
190
flucytosine mechanism
Replace uracil with 5-FU in fungal mRNA
191
A woman with bradycardia after MI...treatment with?
atropine to block vagus from contacting the SA/AV nodes
192
Digoxin and adenosine antiarrythmic effect
Slow conduction through AV node
193
Class I A antiarrythmic
Blocks sodium channels. Decreases depolarization and phase III repolarization
194
Class IB antiarrythmic
Blocks sodium channels in very rapidly depolarizing cells.
195
Class IC antiarrythmic
blocks sodium channels and slows phase 0
196
Fenoldopam
Dopamine derivative. D1 agonist ONLY, no effect on alpha/beta.
--reduces vascular resistance by dilating renal, mesenteric, coronary beds
The only agent that improves renal perfusion while lowering blood pressure
197
diazoxide
arterial vasodilators and decrease HR/contractility
198
hydralazine
arterial vasodilator. use in pregnancies.
199
Nitroprusside
arterial AND venous dilator, most effective for HTN crisis
200
Tox: nitroprusside
cyanide toxicity
201
Side effects of nicardipine
A dihydropyridine CCB: tachycardia, flushing, headache
202
Traditional high potency anti-psychotics
haloperidol
fluphenazine
pimozide
203
traditional low potency antipsychotics
chlorpromazine
| thioridazine
204
Benefits of 2nd generation antipsychotics?
Improve BOTH positive and negative symptoms. Older 2nd generation antipsychotics only stopped the positive symptoms
205
Side effect of high potency antipsychotics
extrapyramidal symptoms.
206
side effect of low potency antipsychotics
anticholinergic and histamine side effects
207
dystrophin gene is on
X chromosome p21 with a frameshift mutation, resulting in deltion. Becker's is an insertion of three base pairs, causing a milder form
208
Side effect of methotrexate
stomatitis
| Hepatotoxicity
209
Side effect of hydroxychloroquin
permanent retinal damage
210
main mechanism of nitroglycerin
VENOdilator.
211
Platelets predominantly express COX1 or COX 2?
COX-1
--expressed in normally functioning tissue
COX2 only expressed in inflammatory tissue
212
How does aspirin cause asthma attacks?
leukotriene overproduction in the airways
