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Flashcards in Pharm Deck (212):
1

Effect of epinephrine at low and high dose

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

To prevent the low dose effects of epinephrine (lowered BP), what can you do?

Administer a beta blocker so everything goes to alpha constriction instead of Beta 1 (tachycardia) and beta 2 (vasodilation)

3

Succinylcholine side effects

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

4

Who is predisposed to succinylcholine toxicity of hyperK

pts with burns/myopathies, anything that would cause cell lysis

--Also pts with denervating dzs (quadriplegics)

5

Baclofen

GABAb muscle relaxant

6

Dantrolene

Acts on ryanodine receptors, preventing release of calcium
--good for malignant hyperthermia

7

atracurium side effects

histamine release causing flushing, bronchoconstriction, hypotension.
-Seizures

8

If you're worried about hyperkalemia when giving succinylcholine what is a good alt med

vecuronium/rocuronium these are non-depolarizing AchR blockers

9

affinity of enzyme for substrate

=1/Km

10

Vmax is proportional to

enzyme concentration

11

Michaelis-mentin kinetics means

enzyme rxn follows a hyperbolic curve

12

Which types of drugs are metabolized by the liver?

lipophilic drugs
--can be metabolized and excreted in bile/liver

13

Bioavailability of the drug is calculated through

Area under the curve, comparing oral with IV

14

Side effect of nitroglycerin

headaches and facial flushing from vasodilation of skin and meninges

15

Metformin is contraindicated in patients with

renal failure. Because lactic acid accumulates. In reality, metformin is contraindicated in anyone who might have lactic acidosis (alcoholic, septic, CHF)

16

which drugs require routine thyroid testing

lithium and amiodarone

17

Scopolamine mech

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

18

Pilocarpine mech

muscarinic agonist

19

Efficacy:

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

20

Potency

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

Ed50

Lower the Ed50, high potency

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

22

Phenylephrine

An alpha agonist. Vasopressor used for shock

23

Prazosin

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

24

Dobutamine

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