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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)

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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)

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3
Q

Succinylcholine side effects

A
  1. hyperkalemia (arrhythmia)
  2. malignant hyperthermia with halothane
  3. bradycardia
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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)

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5
Q

Baclofen

A

GABAb muscle relaxant

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6
Q

Dantrolene

A

Acts on ryanodine receptors, preventing release of calcium

–good for malignant hyperthermia

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7
Q

atracurium side effects

A

histamine release causing flushing, bronchoconstriction, hypotension.
-Seizures

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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

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9
Q

affinity of enzyme for substrate

A

=1/Km

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10
Q

Vmax is proportional to

A

enzyme concentration

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11
Q

Michaelis-mentin kinetics means

A

enzyme rxn follows a hyperbolic curve

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12
Q

Which types of drugs are metabolized by the liver?

A

lipophilic drugs

–can be metabolized and excreted in bile/liver

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13
Q

Bioavailability of the drug is calculated through

A

Area under the curve, comparing oral with IV

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14
Q

Side effect of nitroglycerin

A

headaches and facial flushing from vasodilation of skin and meninges

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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)

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16
Q

which drugs require routine thyroid testing

A

lithium and amiodarone

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17
Q

Scopolamine mech

A

selective muscarinic ACh antagonist that reduces the effect of the cholinesterase inhibitor

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18
Q

Pilocarpine mech

A

muscarinic agonist

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19
Q

Efficacy:

A

Intrinsic ability of a drug to have a desired outcome, expressed by MAXIMUM activity Emax

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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.

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21
Q

Ed50

A

Lower the Ed50, high potency

–Dose of drug required to produce half of the full response

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22
Q

Phenylephrine

A

An alpha agonist. Vasopressor used for shock

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23
Q

Prazosin

A

Selective alpha-1 BLOCKER for HTN and benign prostatic hyperplasia. Thus, a vasodilator

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24
Q

Dobutamine

A

Major B1, some B2 and A1

  • Increased contractility
  • Small increase in HR
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25
Q

Side effect of dobutamine

A

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
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26
Q

Competitive inhibitor effect on Km

A

Increased

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27
Q

noncompetitive inhibitor effect on Km

A

none

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28
Q

which type of inhibitor will decrease potency?

A

competitive inhibitor

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29
Q

which type of inhibitor will affect efficacy?

A

noncompetitive inhibitor

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30
Q

Calculate volume of distribution

A

amount of drug/plasma drug concentration

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31
Q

t1/2 life

A

=0.7*Vd/CL

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32
Q

which type of drugs stay in the blood

A

large, charge molecules

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33
Q

which drugs go to ECF

A

small hydrophilic molecules

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34
Q

which drugs go to all tissues

A

small lipophilic molecules

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35
Q

clearance equation

A

VdxKe

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36
Q

Loading dose

A

Cp x Vd/F

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37
Q

Maintenance dose

A

Cp x CL/F

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38
Q

Which drugs have zero order elimination?

A

phenytoin
ethanol
aspirin

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39
Q

Pt overdoses with weak acid what do you do?

A

Give bicarb–charges molecule for elimination

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40
Q

Pt overdoses with weak base. What do you do?

A

Give ammonium chloride acid NH4Cl–Charges molecule for elimination

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41
Q

example of weak acid drugs

A

aspirin
phenobarbital
methotrexate

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42
Q

example of weak base drug

A

amphetamines

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43
Q

Phase I metabolism

A

reduction, oxidation, hydrolysis with cytochrome P-450. Makes drug more polar but still active

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44
Q

Phase II metabolism

A

glucuronidation, acetylation, sulfation

–makes polar and inactive metabolites

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45
Q

slow acetylators

A

slow metabolizers of drug. increase risk of side effects

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46
Q

First order elimination

A

constant fraction of drug is excreted

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47
Q

Therapeutic index

A

LD50/ED50

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48
Q

Partial agonist effect

A

decrease efficacy,

effect on potency is variable

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49
Q

therapeutic window is the range btw

A

minimum effective to minimum toxic dose

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50
Q

Sympathetic sweat glands innervated by

A

AchM

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51
Q

Sympathetic renal vasculature innervated by

A

D/D1

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52
Q

Adrenal medulla innervated by

A

Nicotinic Ach receptor. Does NOT go through the sympathetic chain!

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53
Q

Nicotinic ACh receptors are what type of receptors?

A

Ligand-gated Na/K channels

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54
Q

Nn vs Nm receptors?

A

Nn are nicotinic receptors found in autonomic ganglia Nm are found in neuromuscular junctions

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55
Q

What type of receptors are muscarinics?

A

G protein receptors with 2nd messengers

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56
Q

m1

A

CNS and enteric nervous system

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57
Q

m2

A

decrease heart rate/contractility

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58
Q

M3

A 
increase exocrine secretions, peristalsis
bladder contraction
bronchoconstriction
ciliary muscle contraction
pupillary sphincter contraction
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59
Q

alpha 1

A

vascular contraction
dilation pupillary dilator
intestinal/bladder sphincter contraction

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60
Q

alpha2

A
  • CNS mediated decrease in blood pressure
  • Decrease aqueous humor fluid production
  • inhibition of lipolysis
  • inhibition of adrenergic and cholinergic release
  • increased platelet aggregation
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61
Q

beta 1

A

causes renin release

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62
Q

beta 2

A 
vasodilation
bronchodilation
increased heart rate/contractility
ciliary muscle relaxation
aqueous humor production
decreased uterine tone
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63
Q

D1 receptor

A

relaxes renal vascular smooth muscle

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64
Q

D2 receptor

A

brain transmitter

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65
Q

H1

A

bronchial mucus
contraction of bronchioles
pruritis

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66
Q

H2

A

gastric acid secretion

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67
Q

Vasopressin1

A

vascular smooth muscle contraction

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68
Q

vasopressin2

A

Increased permeability in collecting tubules

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69
Q

Gprotein class of D1, D2

A

s

i

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70
Q

Gprotein class of H1, H2

A

q

s

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71
Q

Gprotein class of V1, V2

A

q

s

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72
Q

Which receptors work through Gq?

A 
HAVe 1M&M
H1
A1
V1
M1
M3
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73
Q

which receptors work through Gi?

A

M2
A2
D2

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74
Q

Describe the Gq pathway

A

Phospholipase C activated

  • converts lipids to PIP2
  • PIP2–>DAG and IP3
  • IP3 increases [Ca]in
  • DAG activates protein kinase C
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75
Q

Describe the Gs pathway

A

Activation of adenylyl cyclase

  • incrase cAMP
  • Activation of protein kinase A
  • [Ca] increases
  • myosin light chain kinase increases
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76
Q

what controls release of NE?

A 
NE negative feedback to alpha-2
AII receptor (+)
M2 receptor (-)
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77
Q

acetylcholine is made from

A

AcetylCoA + Choline ChAT

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78
Q

NE is made from

A

Tyrosine–>dopa-Dopamine–?NE

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79
Q

Hemicholinium

A

blocks choline entry into cholinergic neuron

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80
Q

vesamicol

A

inhibits synthesis of Ach

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81
Q

Botulinum

A

prevents release of ACh

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82
Q

metyrosine

A

inhibits tyrosine–>dopa

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83
Q

reserpine

A

inhibits dopamine–>NE

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84
Q

Cocaine, TCA, amphetamines

A

Inhibit NE reuptake

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85
Q

amphetamines

A

also iincrease release of NE inaddition to reducing reuptake

86
Q

guanethidine

A

inhibits release of NE

87
Q

Bethanechol

A

ACh agonist

-Activates bowel and bladder for postoperative ileus and urinary retention

88
Q

Carbachol

A

Ach agonist

89
Q

Pilocarpine

A

Ach agonist

90
Q

methacholine

A

Ach agonist

91
Q

carbachol indication

A

glaucoma

pupillary contraction

92
Q

pilocarpine indication

A

open and closed angle glaucoma. Contracts ciliary muscle and pupillary sphincter

Causes sweat, tears, and saliva

93
Q

Neostigmine

A

AChE inhibitor

  • MG
  • reversal of NMJ blockate
  • postoperative/neurogenic ileus
94
Q

Does neostigmine penetrate CNS?

A

no

95
Q

pyridostigmine

A

long acting AChE inhibitor for MG

96
Q

Does pyridostigmine cross BBB?

A

no

97
Q

Edrophonium

A

used to diagnose myasthenia gravis. short acting AChEI

98
Q

physostigmine indication

A

atropine poisoning. crosses BBB to reverse ACh block

99
Q

Donepezil mechanism

A

AChE inhibitor. Increases Ach in the brain for alzheimer’s patients

100
Q

organophosphates cause

A

AChE inhibitor poisoning. Causes too much Acetylcholine!
Sx:
DUMBBELSS
Diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of muscle/CNS, Lacrimation, Sweating, Salivation

101
Q

Antidote for organophosphate poisoning

A

atropine and pralidoxime

102
Q

What is atropine used for?

A

pupil dilation, relaxation of the ciliary muscle

Also to treat bradycardia

103
Q

Atropine tox

A 
HOT as  ahare
Dry as a bone
MAD as a hatter
RED as a beet
BLIND as a bat
104
Q

What do you NOT want to give to someone with acute close angle glaucoma?

A

Anything that will cause mydriasis (pupil to dilate)

  • alpha 1 activator
  • epinephrine
  • atropine (blocks M3 which activates pupillary sphincter)
105
Q

atropine causes what in men with BPH?

A

urinary retention

106
Q

atropine causes what in infants?

A

hyperthermia

107
Q

What is the problem with giving a D2 blockade?

A

This is how antipsychotics work!

  • -will cause depletion of dopamine
  • -drug induced parkinsonism (extrapyramidal effects of typical antipsychotics)
108
Q

How do you treat drug induced parkinsonism?

A

Give anticholinergics like benztropine or amantadine. These inhibit dopamine reuptake

109
Q

What can you use to dilate the eye?

A

atropine
homatropine
tropicamide

110
Q

mechanism scopolamine

A

Muscarinic antagonist

111
Q

Ipratropium, tiotropium mechanism

A

muscarinic antagonist

112
Q

oxybutynin mechanism

A

muscarinic antagonist

113
Q

glycopyrrolate mechanism

A

muscarinic antagonist

114
Q

oxybutynin use

A

reduce urgency in mild cystitis

115
Q

glycopyrrolate use

A

parenteral: reduce airway secretions before surgery
Oral: drooling or a peptic ulcer

116
Q

epinephrine indications

A

glucoma (open angle), asthma, hypotension

117
Q

alpha 1 on the eye

A

pupillary dilator

118
Q

B2 on the eye

A

ciliary muscle relaxation, aqueous humor production

119
Q

isoproterenol

A

activates B1 and B2

120
Q

use: isoproterenol

A

torsade de point and bradyarrhythmia

121
Q

Norepi activates

A

a1, a2, b1 (less so)

-mostly a1,a2

122
Q

norepi use

A

hypotension

123
Q

dopamine use

A

shock

124
Q

high dose dopamine activates

A

alpha 1 and alpha 2

125
Q

low dose dopa activates

A

D1. good for maintaining renal perfusion when treating shock patients

126
Q

medium dose dopa activates

A

B1, B2

127
Q

dobutamine activates

A

Mostly B1

128
Q

indications dobutamine

A

heart failure, cardiac stress stesting

129
Q

phenylephrine indications

A

hypotension
mydriasis
rhinitis (decongestant0

130
Q

terbutaline activates

A

B2, some B1

131
Q

terbutaline indications

A

premature uterine contractions

132
Q

ritodrine activates

A

B2

133
Q

Applications of Ritodrine

A

Reduces premature uterine contractions

134
Q

amphetamine and ephdrine mechanism

A

releases stored catecholamines.

135
Q

ephedrine indications

A

nasal decongestant

Urinary incontinence

136
Q

What should you never give to someone who has overdosed on cocaine?

A

beta blockers. Leads to unopposed alpha1 activation

137
Q

effect of Norepi on BP and HR

A

Increase in BP, reflex decrease in HR (mostly alpha-1)

138
Q

effect of isoproterenol on BP and HR

A

Increase in HR (B1)

Drop in BP (Mostly B2)

139
Q

When to use clonidine/a-methyldopa?

A

hypertension in peeps with renal disease (preserves flow to kidneys)

140
Q

How does clonidine work?

A

Centrally at the alpha 2 agonists to decrease sympathetic outflow

141
Q

Indication for phenoxybenzamine?

A

pheos

–before removing tumor–it’s an IRREVERSIBLE alpha blocker!

142
Q

Indication for phentolamine?

A

pts in HTN crisis from eating tyramine while taking MAO-I

–it’s reversible :)

143
Q

What does tyramine do?

A

It is a catecholamine releasing agent

144
Q

terazosin, doxazosin, tamsulosin

prazosin

A

alpha-1 selective blockers

145
Q

Indication for tamsulosin

A

Hypertension, urinary retention in BPH

146
Q

side effect of alpha blockers

A

first dose orthostatic hypotension

147
Q

alpha 2 selective blocker

A

mirtazapine

148
Q

indications of mirtazapine

A

depression.

149
Q

side effect of mirtazapine

A

increased appetite and cholesterol

150
Q

Effect of epi +alpha blockade

A

decreased blood pressure (b2 effect takes over)

151
Q

effect of phenylephrine + alpha blockade

A

Normal blood pressure

152
Q

timolol

A

Decreases secretion of aqueous humor in glaucoma

153
Q

Who do you NOT want to give a beta blocker to?

A

asthmatics (if non-selective)

diabetics (beta 2 increases insulin secretion. blocking it will decrease insulin secretion)

154
Q

side effect of beta blockers

A

impotence, bradycardia, sedation

155
Q

which are the selective beta blockers?

A 
metoprolol
atenolol
acebutolol
betaxolol
esmolol 
(A BEAM of b1blockers)
156
Q

Non-selective beta blockers

A

propranolol
timolol
nadolol
pindolol

157
Q

which beta blockers also work as partial agonists?

A

pindolol and acebutolol

158
Q

which drugs are nonselective alpha and beta blockers?

A

carvedilol and acebutolol

159
Q

Treatment for salicylate overdose

A

NaHCO3

160
Q

Amphetamine overdose

A

NH4Cl

161
Q

Betablocker overdose

A

glucagon

162
Q

atropine overdose

A

physostigmine

163
Q

Treatment for lead poisoning

A

CaEDTA
dimercaprol
succimer
penicillamine

164
Q

Treatment for mercury overdose

A

dimercaprol, succimer

165
Q

Treatment for arsenic/gold

A

dimercaprol, succimer, penicillamine

166
Q

Treatment for copper overdose

A

penicillamine

167
Q

Treatment for methemoglobin

A

vitamin C or methylene blue

168
Q

Treatment for methanol/ethylene glycol

A

fomepizole, dialysis

169
Q

Treatment for TCA overdose

A

NaHCO3 (plasma alkalinization)

170
Q

Treatment of tPA/streptokinase, urokinase overdose?

A

aminocaproic acid

171
Q

Treatment of theophylline overdose

A

Beta blocker

172
Q

P-45o inducers

A 
modafinil
barbiturates
st. john's wort
phenytoin
rifampin
griseofulvin
carbamazepine
chronic alcohol use

Momma barb steals Phenphen and Refuses Greasy Carbs Chronically

173
Q

P-450 inhibitors

A

MAGIC RACKS in GQ

macrolides
amiodarone
grapefruit
Isoniazid
cimetidine
ritonavir
acute alcohol abuse
ciprofloxasin
ketoconazole
sulfonamides
gemfibrozil
quinidine
174
Q

Sulfa drugs

A 
P FACTSSS
probenicid
furosemide
acetazolamide
celecoxib
thiazides
sulfonadmide antibiotics
sulfazalazine
sulfonylureas
175
Q

consequences of sulfa allergies

A

Stevens Johnson, Hemolytic anemia

thrombocytopenia, agranulocytosis

176
Q

remember to:

A

GO THROUGH DRUG RXNS on PG 240!!

177
Q

Terbinafine mechanism

A

inhibits squalene 2 3 epoxidase, decreasing ergosterold synthesis

178
Q

ampho mechanism

A

binds to ergosterol in fungal cell MEMBRANE forming pores

179
Q

griseofulvin mechanism

A

binds microtubules and inhibits mitosis

180
Q

caspofungin mechanism

A

binds 1, 3 beta D glucan and blocks glucan synthesis

181
Q

flucytosine mechanism

A

inhibits DNA and RNA synthesis in fungal cells. Used in combo with ampho B for cryptococcus

182
Q

Bosentan mechanism

A

Blocks endothelin receptors. Used to treat primary pulmonary arterial hypertension

183
Q

Entanercept

A

monoclonal antibody that binds TNF-alpha used for RA and psoriasis

184
Q

Drugs that induce CYP 450

A 
Carbamazepine
phenytoin
phenobarbital
griseofulvin
rifampin
185
Q

Drugs that inhibit CYP 450

A 
Grapefruit
Ritonavir
Azoles
Cipro
Cimetidine
Isoniazid
Erythromycin
186
Q

which drugs prolong the QT interval?

A 
Class III antiarrythmics (Potassium Channel blockers)
Amiodarone
Ibutilide
Dofitilide
Sotalol
187
Q

short acting benzos

A

midazolam

triazolam

188
Q

how do u prevent flushing associated with Nitroglycerin?

A

administer aspirin beforehand. Reduces prostaglandins. . nicotinic acid also helps

189
Q

caspaicin works by

A

decreasing the level of substance P in the PNS

190
Q

flucytosine mechanism

A

Replace uracil with 5-FU in fungal mRNA

191
Q

A woman with bradycardia after MI…treatment with?

A

atropine to block vagus from contacting the SA/AV nodes

192
Q

Digoxin and adenosine antiarrythmic effect

A

Slow conduction through AV node

193
Q

Class I A antiarrythmic

A

Blocks sodium channels. Decreases depolarization and phase III repolarization

194
Q

Class IB antiarrythmic

A

Blocks sodium channels in very rapidly depolarizing cells.

195
Q

Class IC antiarrythmic

A

blocks sodium channels and slows phase 0

196
Q

Fenoldopam

A

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
Q

diazoxide

A

arterial vasodilators and decrease HR/contractility

198
Q

hydralazine

A

arterial vasodilator. use in pregnancies.

199
Q

Nitroprusside

A

arterial AND venous dilator, most effective for HTN crisis

200
Q

Tox: nitroprusside

A

cyanide toxicity

201
Q

Side effects of nicardipine

A

A dihydropyridine CCB: tachycardia, flushing, headache

202
Q

Traditional high potency anti-psychotics

A

haloperidol
fluphenazine
pimozide

203
Q

traditional low potency antipsychotics

A

chlorpromazine

thioridazine

204
Q

Benefits of 2nd generation antipsychotics?

A

Improve BOTH positive and negative symptoms. Older 2nd generation antipsychotics only stopped the positive symptoms

205
Q

Side effect of high potency antipsychotics

A

extrapyramidal symptoms.

206
Q

side effect of low potency antipsychotics

A

anticholinergic and histamine side effects

207
Q

dystrophin gene is on

A

X chromosome p21 with a frameshift mutation, resulting in deltion. Becker’s is an insertion of three base pairs, causing a milder form

208
Q

Side effect of methotrexate

A

stomatitis

Hepatotoxicity

209
Q

Side effect of hydroxychloroquin

A

permanent retinal damage

210
Q

main mechanism of nitroglycerin

A

VENOdilator.

211
Q

Platelets predominantly express COX1 or COX 2?

A

COX-1
–expressed in normally functioning tissue
COX2 only expressed in inflammatory tissue

212
Q

How does aspirin cause asthma attacks?

A

leukotriene overproduction in the airways

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