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test 4 Flashcards

1
Q

How are adrenoceptors activated?

A

Through norepi or epi

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2
Q

What do adrenoceptors act on?

A

Act on neurons that release norepi

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3
Q

What does administration of epi cause?

A

Produces similar effects of stimulation of sns

Sympathetic response

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4
Q

What do alpha 1 receptors act on?

A

Vascular smooth muscle
Genitourinary smooth muscle
Intestinal smooth muscle
Heart
Liver

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5
Q

What do alpha 1 receptors do to the vascular smooth muscle?

A

Contraction

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6
Q

What do alpha 1 receptors do to the genitourinary smooth muscle?

A

Contraction

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7
Q

What do alpha 1 receptors do to the intestinal smooth muscle?

A

Relaxation

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8
Q

What do alpha 1 receptors do to the heart?

A

Increase intropy and excitability

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9
Q

What do alpha 1 receptors do to the liver?

A

Glycogenolysis and gluconeogenesis

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10
Q

What do alpha 2 receptors act on?

A

Platelets
Pancreatic beta cells
Nerves
Vascular smooth muscle

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11
Q

What do alpha 2 receptors do to platelets?

A

Aggregation

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12
Q

What do alpha 2 receptors do to the pancreatic beta cells?

A

Decrease insulin secretion

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13
Q

What do alpha 2 receptors do to nerves?

A

Decrease NE release

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14
Q

What do alpha 2 receptors do to vascular smooth muscle?

A

Contraction

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15
Q

What do Beta 1 cells act on?

A

Heart
Renal juxtaglomerular cells

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16
Q

What do beta 1 cells do to the heart?

A

Increase chronotropy and intropy
Increase AV node conduction velocity

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17
Q

What do beta 1 cells do renal juxtaglomerular cells?

A

Increase renin secretion

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18
Q

What do beta 2 cells act on?

A

Smooth muscle
Liver
Skeletal muscle

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19
Q

What do beta 2 cells do to smooth muscle?

A

Relaxation

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20
Q

What do beta 2 cells do to liver?

A

Glycogenolysis
Gluconeogenesis

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21
Q

What do beta 2 cells do to the skeletal muscle?

A

Glycogenolysis and K+ uptake

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22
Q

What receptor is the main cause of ateriole constriction and eye muscle contraction?

A

Alpa 1

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23
Q

What receptor causes the heart to increase rate and force?

A

Beta 1

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24
Q

What receptor causes the lungs to relax?

A

Beta 2

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25
Q

What receptor is responsible for decreased activity of intestines and dilation of skeletal muscle?

A

Beta 2

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26
Q

What are alpha 1 agonists used for?

A

Shock/hypotension
Nasal decongestant

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27
Q

What are alpa 1 antagonists used for?

A

Antihypertensives
BPH

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28
Q

What are alpha 2 agonists used for?

A

Antihypertensives
Glaucoma
Analgesia
Sedatives

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29
Q

What are alpha 2 antagonists used for?

A

We do not use them clinically

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30
Q

What are Beta 1 agonists used for?

A

There are none

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31
Q

What do we use Beta 1 antagonists for?

A

Antihypertensives
Antiarrhythmics

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32
Q

What are beta 2 agonists used for?

A

Bronchodilators
Glaucoma

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33
Q

What are beta 3 agonists used for?

A

Weight loss

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34
Q

What are beta 2 antagonists used for?

A

They are not used clinically

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35
Q

What does stimulation of the alpha 1 receptor cause?

A

Vasoconstriction
Increased peripheral resistance
Increased blood pressure
Mydriasis
Closure of the sphincter of bladder

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36
Q

What does stimulation of the alpha 2 receptor cause?

A

Inhibition of norepinephrine release
Inhibition of ACH release
Inhibition of insulin release

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37
Q

What does stimulation of the beta 1 receptors cause?

A

Tachycardia
Increased lipolysis
Increased myocardial contractility
Increased release of renin

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38
Q

What does stimulation of the beta 2 receptors cause?

A

Vasodilation
Decrease of peripheral resistance
Bronchodilation
Increased glycogenolysis
Increased release of glucagon
Relaxed uterus

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39
Q

What happens to catechols when they are exposed to air?

A

They are oxidized and the solution darkens to a highly colorized product

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40
Q

How are catechols metabolized?

A

By COMT

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41
Q

What are the non selective alpha 1 agonists?

A

Norepi and epi

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42
Q

Why arent NE and E used clinically alot?

A

They have limited clinical uses due to selectivity issues and oral bioavailability

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43
Q

Which is used more often? EPi or NOrEpi

A

EPI

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44
Q

Why is epi used?

A

For trauma (stimulation of the Beta 1 - heart muscle) - hypotension

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45
Q

What are the selective alpha 1 agonists?

A

Phenylephrine
Metaraminol
Methoxamine
Tetrahydrozoline
Oxymetazoline

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46
Q

Why do selective alpha 1 agonists have limited cardiac stimulation?

A

They are selective so they have little cardiac activity

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47
Q

What are alpha 1 selective agonists used for?

A

Nasal decongestants
Red eye

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48
Q

Why do selective alpha 1 agonists last longer in the body than E and NE?

A

They have a longer duration of action due to less catechol activity

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49
Q

What are alpha 2 agonists mainly used for?

A

Hypertension, sedative, and epidural enhancer

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50
Q

What are the alpha 1 selective agonists?

A

Clonidine, apraclonidine, brimonidine, Tizanidine, Guanfacine, Guanabenz, Methyldopa

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51
Q

What are apraclonidine and brimonidine used for?

A

Glaucoma and have little systemic effect

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52
Q

What is methyldopa used for?

A

Antihypertensive during pregnancy (metabolized into active compound = methylnorepinephrine)

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53
Q

What are the beta 1 agonists?

A

Dopamine and its analogues

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54
Q

What does Beta 1 agonism do?

A

Increased contractile force of the heart
Cardiac stimulation
We want to avoid this

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55
Q

When are beta 1 drugs used?

A

As a cardiac stimulant post surgery

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56
Q

What are Beta 2 agonists used for?

A

Bronchodilation
Short acting and long acting
Asthma
COPD

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57
Q

What kind of drug is isoproterenol?

A

Beta 2 short acting agonist

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58
Q

Why is isoproterenol not used?

A

It has beta 1 type side effects due to an isopropyl group as the amine side chain
Has a catechol that makes it unstable

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59
Q

What kind of drug is albuterol?

A

Short acting beta 2 agonist

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60
Q

Why is levalbuterol 4 times more potent than albuterol?

A

It is the pure isomer and not the racemic mixture but it is more expensive and time consuming to make

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61
Q

What kind of drug is salmeterol with flucticasone (Advair)?

A

Long acting Beta 2 agonists

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62
Q

What makes a beta 2 agonist long acting?

A

Much higher LogP due to a long lipophilic side chain

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63
Q

What kind of drug is formoterol with budesonide (symbicort)?

A

Long acting beta 2 agonist
4 times more potent than advair

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64
Q

What makes a drug a mixed acting sympathomimetic?

A

It is a drug that acts both directly and indirectly (directly activates receptor and causes release of NE)

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65
Q

What are mixed acting sympathomimetics used for?

A

Nasal decongestant (Sudafed)

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66
Q

What drugs are alpha 1 selective antagonists?

A

Prazosin, Terazosin, Tamsulosin, Doxazosin, Alfuzosin, Sildosin

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67
Q

What do alpha 1 A receptors do?

A

Decrease smooth muscle contraction of the prostate while B is vasculature

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68
Q

What kind of drug is Yohimbe?

A

Alpha 2 agonist

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69
Q

What does yohimbe do?

A

induce hypertension
Increase heart rate
No clinical use but can be used for impotence and orthostatic hypotension

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70
Q

What do Beta 1 antagonists do?

A

Decrease contractile force and decrease blood pressure

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71
Q

What is the difference between olols and alols?

A

Olols are for aryloxypropanolamines
Alols are for arylethanolamines

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72
Q

What do beta blocker do to decrease blood pressure?

A

They compete with catecholamines for Beta 1 and 2 binding to treat hypertension

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73
Q

What are olols used for?

A

Glaucoma and hypertension

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74
Q

What are the ADRs of non selective beta blockers?

A

Fatigue
Bronchoconstriction
Sexual dysfunction
Arrhythmias from withdrawls

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75
Q

What pneumonic device can you use to see if the beta blocker is selective “clean” or not?

A

BEAM (if they start with these letters they are clean as well as Nebivolol and except Metipranolol)

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76
Q

What enzyme converts tyrosine to L DOPA

A

Tyrosine hydroxylase

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77
Q

What molecule inhibits tyrosine hydroxylase?

A

Alpha methyl tyrosine

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78
Q

What enzyme converts LDOPA to dopamine

A

Dopa decarboxylase

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79
Q

What molecule inhibits dopa decarboxylase?

A

Carbidopa

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80
Q

What enzyme converts dopamine to norepinephrine?

A

Dopamine beta hydroxylase

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81
Q

What takes up dopamine into vesicles?

A

VMAT

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82
Q

What inhibits VMAT?

A

Reserpine

83
Q

Why do you need to transport dopamine into a vesicle?

A

MAO will degrade the dopamine in the cell

84
Q

What enzyme converts NE to E?

A

Phenylethanolamine N Methyl transferase

85
Q

What produces E?

A

adrenal medullary cells

86
Q

What are the two ways to terminate catecholamine neurotransmission?

A

Reuptake
Diffusion away from synapse

87
Q

What is the major way to terminate catecholamine neurotransmission?

A

Presynaptic reuptake

88
Q

What blocks reuptake of catecholamines?

A

Cocaine and antidepressants and amphetamines

89
Q

What does COMT do?

A

Metabolizes NE, E, and DA and is excreted into the urine and not reuptaked

90
Q

What kind of G protein is alpha 1?

A

Gq

91
Q

What kind of G protein is alpha 2?

A

Gi

92
Q

What kind of G protein is beta?

A

Gs

93
Q

What does alpha 2 activation do inside of the cell?

A

Inhibits adenylate cyclase (decrease PKA and CAMP and increase K+ so it hyperpolarizes the cell to inhibit it)

94
Q

What does alpha 1 activation do inside the cell?

A

Increase phospholipase C (Increase IP3, DAG, Ca2+ from ER)

95
Q

What is unique of the beta 2 variant of agonist potency?

A

Beta 2 - epinephrine has much greater effect than NE unlike others where they are the same

96
Q

What does systolic tell you?

A

Strength and volume of cardiac output

97
Q

What does diastolic tell you?

A

Peripheral vascular resistance

98
Q

What does mean arterial pressure tell you?

A

Tissue perfusion pressure
Monitered by baroreceptors

99
Q

Heterologous

A

PKA

100
Q

Homologous

A

Beta arrestin
BARK

101
Q

What class is epinephrine and norepinephrine in?

A

Nonselective adrenergic neurotransmitters

102
Q

What does reserpine do?

A

Blocks VMAT
VMAT takes up neurotransmitters into vesicles so they are not degraded by MAO so this would reduce the amount of neurotransmitters available

103
Q

What class of drug is amphetamine?

A

Indirect acting sympathomimetic

104
Q

Why is NE and E not typically used in clinical settings?

A

They have selectivity issues and oral bioavailability issues

105
Q

Which is used more, E or NE?

A

E

106
Q

When is epi used?

A

During trauma situations (trauma based hypotension

107
Q

What class of drug is Phenylephrine?

A

Alpha 1 selective agonist

108
Q

What is phenylephrine used for?

A

Nasal decongestant
Sudafed PE

109
Q

What class of drug is Tetrahydrozoline?

A

Selective alpha 1 agonist
Visine

110
Q

What is tetrahydrozoline?

A

Reduce red eye

111
Q

What class of drug is oxymetazoline?

A

Selective alpha 1 agonist
Afrin

112
Q

What does oxymetazoline do?

A

Used as a nasal decongestant

113
Q

Why do selective alpha 1 agonists have little or minimum cardiac stimulation?

A

Because they are not selective to the beta receptors (beta1) that stimulates the heart

114
Q

Why do selective alpha 1 agonist have a longer duration of action compared to E and NE?

A

Because they do not have catechols so are not sucseptible to COMT

115
Q

What class of drug is clonidine?

A

Selective alpha 2 agonist
Catapres

116
Q

Why is clonidine considered a flag ship compound?

A

It was used as an alpha 1 nasal decongestant but they noticed a significant reduction in blood pressure so they found alpha 2 activation

117
Q

What do alpha 2 receptors primarily do when stimulated?

A

Decrease the amount of NE released into the cleft

118
Q

What class of drug is apraclonidine?

A

Selective alpha 2 agonist
Iopidine

119
Q

What is apraclonidine used for?

A

eye drops for glaucoma

120
Q

What class of drug is brimonidine?

A

Selective alpha 2 agonist
Alphagan P

121
Q

What is brimonidine used for?

A

Glaucoma

122
Q

What class of drug is Guanfacine?

A

Selective alpha 2 agonist
Tenex, Intuiv

123
Q

What class of drug is alpha methyldopa?

A

Selective alpha 2 agonist
Aldomet

124
Q

What is alpha methyldopa used for?

A

Antihypertensive during pregnancy
It is metabolized into methylnorepinephrine

125
Q

What class of drug is Dobutamine?

A

Beta 1 agonist

126
Q

What is dobutamine used for?

A

Only used as a cardiac stimulant post surgery

127
Q

What do you need for beta 2 selectivity?

A

A t butyl or greater group on the amine
an OH on the beta carbon

128
Q

What class of drug is Isoproterenol?

A

Short acting beta 2 agonist

129
Q

Why is isoproterenol not a good drug?

A

It has beta 1 side effects due to the isopropyl group on the amine
It has a catechol so it is not stable

130
Q

What class of drug is albuterol?

A

short acting beta 2 agonist
Proventil, Ventolin, ProAir

131
Q

What class of drug is levalbuterol?

A

Short acting beta 2 agonist
Xopenex

132
Q

What is the difference between levalbuterol and albuterol?

A

albuterol is a racemic mixture
levalbuterol is the pure active isomer which makes it 4 times for potent as a bronchodilator

133
Q

What is albuterol and levalbuterol used for?

A

it is a rescue inhaler so for acute symptoms

134
Q

What class of drug is salmeterol?

A

Long acting beta 2 agonist
With fluticasone = Advair
Without = serevent

135
Q

What is Salameterol used for?

A

Chronic or daily use for asthma and COPD
NOT FOR ACUTE SYMPTOMS

136
Q

What class of drug is formoterol?

A

LABA

137
Q

What makes a beta 2 agonist long acting?

A

It has a lipophilic long side chain that interacts with the exosite so the drug can keep interacting over and over with the binding site or active site

138
Q

What is the main difference between formoterol and salmeterol?

A

faster onset for formoterol

139
Q

What class of drug is pseudophedrine?

A

Mixed acting sympathomimetic

140
Q

What is the main side effect of pseudophedrine?

A

Increase in blood pressure from indirect activity

141
Q

What class of drug prazosin?

A

Alpha 1 selective antagonist
Minipres

142
Q

What is Minipress used for?

A

Hypertension and BPD (not FDA approved for BPH)

143
Q

What is the difference between alpha 1 A and alpha 1 B?

A

Alpha 1 a has selectivity for the prostate (used for bph)
Alpha 1 B has selectivity for the vasculature (hypertension)

144
Q

What is the USAN for quinazolines?

A

Azosin

145
Q

What class of drug is terazosin?

A

Selective alpha 1 antagonist
Hytrin

146
Q

What is Hytrin used for?

A

Hypertension and BPH

147
Q

What class of drug is tamsulosin?

A

Selective alpha 1 antagonist
Flomax

148
Q

What is tamsulosin used for?

A

BPH

149
Q

What class of drug is doxazosin?

A

Selective alpha 1 antagonist
Cardura

150
Q

What does doxazosin treat?

A

BPH mainly

151
Q

What class of drug is Alfuzosin?

A

Selective alpha 1 antagonist
Uroxatral

152
Q

What is alfuzosin used for?

A

BPH

153
Q

What class of drug is silodosin?

A

Selective alpha 1 antagonist

154
Q

What is silodosin used for?

A

BPH

155
Q

What class of drug is yohimbine?

A

Alpha 2 antagonist
Herbal not FDA approved

156
Q

What does yohimbine treat off label?

A

Impotence
orthostatic hypertension

157
Q

What do selective beta 2 blockers treat?

A

Glaucoma and hypertension

158
Q

What is added to the drug for it to be an antagonist?

A

A bulky side chain

159
Q

What are the adr’s of selective beta blockers?

A

Fatigue
Bronchoconstriction
Sexual dysfunction
Arrhythmias upon withdrawls

160
Q

what pneumonic device is used to see clean beta blockers?

A

BEAM
Plus Nebivolol

161
Q

What is the rate limiting step for making neurotransmitters?

A

Tyrosine to LDOPA through tyrosine hydroxylase

162
Q

How do you get from LDOPA to Dopamine?

A

DOPA decarboxylase

163
Q

How do you get from dopamine to Norepinephrine?

A

Dopamine Beta Hydrolase

164
Q

How do you get from NE to E?

A

Phenylethanolamine N methyl transferase

165
Q

What are the two ways to terminate catecholamine neurotransmission?

A

Reuptake (presynaptic is major)
Diffusion away from the synapse

166
Q

What drugs block reuptake?

A

Antidepressants and Cocaine

167
Q

What metabolizes E, NE, and DA and excretes it in the urine?

A

COMT

168
Q

Why is alpha 2 receptor considered an autoreceptor?

A

it is inhibitory and is on the presynaptic neuron unlike the others which are on the postsynaptic neuron

169
Q

How do alpha 2 receptors create an inhibitory response?

A

Increase K currents to hyperpolarize the cell

170
Q

What kind of G coupled receptor is alpha 1?

A

Gq

171
Q

What does Gq alpha 1 receptor do in the cell?

A

Increase IP3, DAG, Ca2+, and turns on phospholipase C

172
Q

What kind of G coupled receptor are the beta receptors?

A

All are Gs

173
Q

Which has a greater effect on beta 2, E or NE?

A

E

174
Q

What does systolic pressure measure?

A

Cardiac output

175
Q

What does diastolic pressure measure?

A

PVR

176
Q

What is mean arterial pressure?

A

Tissue perfusion pressure monitered by baroreceptors

177
Q

Why does phenylephrine help with nasal decongestion?

A

The mucosal membranes are highly vascularized and if you constrict the vasculature, it reduces the pressure in the nose

178
Q

What are two off label uses for clonidine?

A

Sedative
Epidural enhancer

179
Q

What kind of spacer does clonidine and its derivatives have?

A

An N and C spacer

180
Q

What are the three major determinants of action of a drug?

A

Relative potency of amine or drug (is it alpha or beta)
Dominant tone
Reflex and other homeostatic adjustments

181
Q

What is the main difference between reuptake 1 and 2?

A

Reuptake 1 has a high affinity for NE but is slow
Reuptake 2 has a low affinity for NE but is fast (protective mechanism if there is too much NE in the cleft)

182
Q

What are the two ways a receptor can be desensitized?

A

Changes in the receptor or receptor coupling
Receptor sequestration (tachyphylaxis)

183
Q

What is inotropic?

A

Contractile force

184
Q

What is chronotropic?

A

Increase in hr and conduction velocity

185
Q

What is the core drug structure of sympathomimetics?

A

Phenylethanolamine

186
Q

What kind of drug is amphetamine?

A

Indirect acting sympathomimetic

187
Q

How does amphetamine cause an increase in calcium release?

A

Taken in by VMAT and moves NE out into the cytosol. It is a weak MAO inhibitor so it also inhibits the break down of NE and E

188
Q

What is the main difference between amphetamine and tyramine?

A

It is Calcium independent it is metabolized by MAO

189
Q

What kind of drug is methylphenidate?

A

Psychostimulant

Indirect agonist

190
Q

What kind of drug is Concerta?

A

Psychostimulant

indirect agonist

191
Q

How does concerta work in terms of delayed release?

A

Causes osmotic release
Immediate release and then the device delays release to different compartment

192
Q

What is phentermine (adipex P) used to treat?

A

Obesity

193
Q

What drug is a mydriatic agent but wont cause cycoplegia (cilliary muscle constriction)?

A

Phenylephrine

Alpha receptors are not on the cilliary muscle

194
Q

What drug causes an increase of blood pressure and reflex bradycardia?

A

Phenylephrine

195
Q

How do you stop reflex bradycardia from phenylephrine?

A

Add a ganglionic blocer

no ACh on heart so no reflex bradycardia

196
Q

What class of drug is midodrine (orvaten)?

A

Alpha 1 agonist

197
Q

What is midodrine used to treat?

A

Orthostatic hypotension

198
Q

What class of drug is hydroxyamphetamine and tropicamide (Paremyd)?

A

Alpha 1 agonist

199
Q

What does hydroxyamphetamine and tropicamide (Paremyd) treat?

A

It is a mydriatic agent so glaucoma

200
Q

What class of drug is Droxidopa (Northera)?

A

Alpha 1 agonist

201
Q

What is Droxidopa used to treat?

A

Orthostatic hypotension (neurogenic)

Prodrug of NE and E, Metabolized into neurons by the DOPA decarboxylase

202
Q

What kind of drugs are imidazolines?

A

Alpha 1 agonist

203
Q

What are the main side effects of clonidine?

A

Dry mouth

204
Q

What kind of drug is Precedex/dexmedetomidine?

A

Alpha 2 agonist

Sedative for ICU

MPT (5 decks)

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