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Pharmacology > Sweep 1 > Flashcards

Sweep 1 Flashcards

1
Q

4 types of signaling receptors

A

ligand activated ion channels, g protein, tyrosine kinase receptors, ligand activated transcription factors

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2
Q

-zosin

A

alpha 1 blocker

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3
Q

-olol

A

beta blocker-

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4
Q

-ilol, -alol

A

beta blocker with alpha 1 activity

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5
Q

Hyperpolarizing ligand activated ion channet in

A

chlorine

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6
Q

depolarizing ligand activated ion channels are

A

not particularly selective (acetylcholine, serotonin, glutamate)

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7
Q

ligand activated ion channels in the organelle:

A

IP3 mediated calcium release from ER

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8
Q

PIP2 broken down goes to

A

IP3 and DAG

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9
Q

——— breaks down PIP2

A

phospholipase C (beta?)

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10
Q

What protein helps accelerate G protein phosphorylation activity

A

RGS

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11
Q

Affect on ————— - Galphas, Galphai

A

adenylyl cyclase

s = up, i = down

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12
Q

What activates cAMP

A

protein kinase A

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13
Q

PKA phos leads to

A

stuff happening.

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14
Q

Signaling molecules can be embedded in

A

the plasma membrane - GPCRs can liberate them by activating phospholipases

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15
Q

Galphai,o

A

increase phospholipase A2, C

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16
Q

Phospholipase A2 will produce

A

arachidonic acid

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17
Q

arachidonic acid is a source of

A

eicosinoid signaling molecules, prostaglandins

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18
Q

IP3 leads to —- release

A

calcium

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19
Q

—- complex mediates signalling by calcium

A

calcium calmodulin

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20
Q

ca/calmodulin signaling examples

A

NO synthase (relaxes) - endothelial, neuronal

calcium/calmodulin dependent kinase

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21
Q

Most isos of protein kinase C regulated by

A

DAG (allows for more efficient binding of calcium)

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22
Q

GRK recruited by ———, works by

A

Gbeta, G gamma complex

phosphorylating GPCR, leading to beta arrestin binding, which leads to engulfment.

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23
Q

JAK-STAT binding of signalling molecule leads to

A

phosphorylation of receptor by JAK kinase. This leads to 2 stat proteins binding and getting phosphorylated

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24
Q

Once phosphorylated, stat proteins

A

dimerize, and then they go to nucleus to induce transcription.

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25
Q

STAT domains that can be phosphorylated

A

SH2, tyrosine. Phosphorylating binds the two together, allowing for dimerization.

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26
Q

———– mediates biological response to cytokines

A

STAT proteins

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27
Q

The larger the partition coefficient, the

A

more drug to be absorbed.

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28
Q

—- transporters kick drug out of cell

A

ABC

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29
Q

—- transporters important for moving organic acids/bases

A

SLC

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30
Q

—- drugs diffuse quickly from blood

A

lipophilic. Water soluble move through endothelial gaps (slow)

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31
Q

Where are there no gaps in endothelium?

A

BBB

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32
Q

Q/C =

A

Vd - Q = original amount, C = concentration of drug in plasma

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33
Q

How many liters of plasma

A

3

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34
Q

How many liters of insterstitial fluid

A

9

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35
Q

How many liters of cells

A

29

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36
Q

Excretion of drugs strategy

A

make drugs more water soluble.

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37
Q

Excretion process

A

Add or uncover functional group, conjugate

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38
Q

—– are membrane bound enzymes that metabolize drugs

A

microsomes. P450 and cyps here, as well as flavin monooxygenases

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39
Q

ways to metabolize

A

reductiosn, dehalogneation, hydrolysis, glucuronic conjugation

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40
Q

Conjugation usually

A

inactivates drugs, exception is morphine

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41
Q

Microsomal enzymes are designed to remove

A

foreign substances

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42
Q

Non-microsomal metabolism occurs when

A

drug mimics natural substance.

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43
Q

Tyramine can lead to

A

hypertensive crisis when taking MAO inhibitors.

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44
Q

Ingestion of grapefruit juice inactivates

A

CYP3A4 (60% of all met.)

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45
Q

Pharmacokinetic tolerance

A

drug concentration diminished

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46
Q

Pharmacodynamic tolerance

A

drug response diminished

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47
Q

Tyramine is an example of

A

tachyphylaxis. This increases HR and BP by promoting norepinephrine release. Tachy occurs when norepinephrine is depleted.

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48
Q

Phase II conjugation by

A

Nat 1 and 2 nacetyltransferases

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49
Q

NATs conjugate

A

aromatic amines, alcohols, hydroxylamines.

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50
Q

Slow acetylators

A

have drugs stay around longer (NATs). Some good, some bad reactions.

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51
Q

Cytochrome p450

A

CYPs… dummy.

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52
Q

CYP2D6 removes

A

methyl from oxygen.

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53
Q

Muscarinic agonists used to treat dry mouth are metabolizedby

A

CYP2D6. Adverse effects are cholinergic syndrome.

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54
Q

CYP2D6 poor metabolizers for codeine

A

not as much conversion to morphine, not very effective. Ultra metabolizers can experience ab pain.

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55
Q

Warfarin metabolized by

A

CYP2C9

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56
Q

CYP2C9 poor metabolizers have bad bleeding issues when taking

A

warfarin

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57
Q

Ryanodine receptors mediate

A

calcium mediated calciumrelease - differs from IP3.

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58
Q

Overactive ryanodine receptors leads to

A

hyperthermia.

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59
Q

Potentiation

A

second drug with diff activity enhances first drug (ex - improving absorption of drug 2 by drug 1)

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60
Q

When digesting alcohol if ——— is allowed to accumulate, you get bad headaches

A

acetaldehyde.

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61
Q

Disulfuram inhibits

A

acetaldehyde dehydrogenase.

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62
Q

Summation

A

combined activity of two drugs on the same site or similar sites.

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63
Q

Additive summation

A

Drug action is interchangeable when dosed at fractions of their EC50.

64
Q

Infra-additive summation

A

Less than additive response when dosed as above.

65
Q

Supra-additive

A

Yield more than additive response when dosed as above.

66
Q

Synergism

A

combined effect of two drugs greater than maximal effect of either drug alone.

67
Q

Pharmaceutical interactions

A

When drugs chemically react with each other (rare)

68
Q

Drugs should never be administered with

A

the same syringe for pharmaceutical interaction reasons.

69
Q

Distribution across plasma membrane can be affected by drugs that:

A
  1. Alter p-glycoprotein activity or levels
  2. Alter pH gradients
  3. Disrupt membrane barriers
70
Q

beta blockers can

A

inhibit blood flow to liver by reducing CO, which inhibits clearance of lidocaine.

71
Q

Electrochemical gradient establishment - minor is

A

sodium potassium atpase pump

72
Q

Electrochemical gradient establishment, major is

A

potential arising from membrane permeabilities

73
Q

Net efflux of potassium is going to continue until the force

A

bringing potassium outside is balanced by the electrical force bringing it back in.

74
Q

The ———– are responsible for maintaining homeostasis

A

autonomic and endocrine systems

75
Q

Sympathetic ns at effector site:

A

epi, norepi

76
Q

Somatic at effector site

A

acetylcholine - nicotinic

77
Q

Parasymp at effector site

A

acetylcholine - muscarinic

78
Q

Endogenous adrenergic amines

A

epi, norepi, dopa

79
Q

endogenous adrenergic amines are made in

A

symp. nerve terminals and adrenal medulla

80
Q

—- receptors are most importnat at presynaptic termini

A

alpha 2

81
Q

—- inhibit norepi and epi release

A

alpha 2

82
Q

Norepi/epi when bound will

A

cause calcium to enter a cell

83
Q

beta 2 on smooth muscle increase

A

pka, diminish calcium levels, phosphorylate/inhibit mlck

84
Q

—– activates PKA

A

cAMP

85
Q

—– inhibits MLCK

A

PKA

86
Q

PKA mediated phosphorylation also activates

A

potassium channels, which leads to hyperpolarization and reduction in cellular calcium.

87
Q

beta 1 receptors on

A

cardiac muscle mainly, also some beta 2

88
Q

beta 1 activate

A

PKA, L-type Calcium channels, increase calcium

89
Q

beta 1 activators can improve

A

contractility of a failing heart. Can lead to arrhythmias

90
Q

Epi concerns with systemic absorption

A

arrhythmias

91
Q

Activation of alpha 1 and beta 2 receptors on vascular tissue will lead to

A

vasoconsttriciton (more alpha than beta)

92
Q

Epi activates

A

alpha 1, beta 1 and 2

93
Q

norepi doesn’t activate

A

beta 2

94
Q

nor at 0.2microg/kg/min

A

alpha 1 stimulated, BP increases, reflex bradycardia

95
Q

bradycardia

A

abnormal slow heart action

96
Q

tachycardia

A

abnormal fast heart action

97
Q

epi at 0.2microg/kg/min

A

stimulates all, alpha dominates

98
Q

norepi at 0.1microg/kg/min

A

stimulates alpha. BPincrease, reflex bradycardia

99
Q

epi at 0.1microg/kg/min

A

stimulates beta more than alpha, beta 2 dominates. BP decreases

100
Q

Activate beta 1

A

increas force of contraction, increase rate.

101
Q

Non vascular smooth muscle - Sphincters - relaxation mediated by

A

alpha receptors with epi/nor

102
Q

Salivary gland norepi/epi net effect

A

Modest secretion with lots of protein - beta 1 for protein.

103
Q

Epi/norepi does’nt

A

get into brain

104
Q

Epinephrine for anaphylaxis:

A

Stimulation of a receptors: Increase blood pressure
Stimulation of b1 receptors: Positive cardiac effects
Stimulation of b2 receptors: Bronchodilation`

105
Q

alpha 2 receptor agonists primarily act in

A

CNS - inhibit norepi and epi release at presynapse - can be used as msucle relaxant,

106
Q

— used primarily in heart failure and cardiogenic shock

A

beta 1 agonists

107
Q

Beta 2 agonists for

A

respiratory bronchodilation, can also vasodilate and relax uterus

108
Q

non selective alpha antagonists block

A

transfer mediated feedback loop (alpha 2). Limited use for humans due to side effects

109
Q

phentolamine

A

non selective alpha antagonist - used to clear up anesthetic effect following dental procedure.

110
Q

patients with pheochromocytoma can benefit from

A

non selecgive allpha antagonists

111
Q

beta 3 agonists produce

A

vasodilation

112
Q

beta 2 blockers are nonfavorable due to

A

airway closure.

113
Q

useful beta blockers are either

A

beta 1 only or nonselective

114
Q

beta blockers decrease

A

force of heart contraction and HR and BP decrease renin

115
Q

beta blockers w/o isa (intrinsic sympathomimetic activity)

A

decrease HR, plasma renin, CO

116
Q

beta blockers with isa

A

no decrease on cardiac or renin, attenuate agonist driven response.

117
Q

in glaucoma ——- is used to reduce vitrious humor production

A

beta blockers.

118
Q

beta blockers that get into the brain used for

A

migraine and tremor from anxiety

119
Q

some antagonist for alpha and beta, used for

A

hypertension

120
Q

alpha blockers can cause

A

orthostatic hypotension, so be careful when patients taking drugs for hypertension

121
Q

Patient taking beta blockers more at risk for

A

hypertensive crisis after anesthetic due to not having beta 2 response to help balance alpha 1.

122
Q

Cholinergic receptors - two types

A

nicotinic, muscarinic

123
Q

Muscarinic M1,3,5

A

Linked to Galphaq, which activate DAG, IP3 signaling and contraction

124
Q

Muscarinic M2,4

A

Linked to galphai, downregulate adenylate cyclase and lead to relaxation

125
Q

Indirect cholinergic agonist

A

cholinesterase inhibitor

126
Q

Acetylcholine is ———- for muscarinic and nicotinic

A

non-selective

127
Q

carbochol favors ——— receptors

A

muscarinic

128
Q

——- agonists more clinically relevant

A

muscarinic

129
Q

Odd numbered muscarinic receptors activa

A

phospholipase C and lead to Ca release and contraction

130
Q

even numbered muscarinic receptors inhibit

A

adenylcyclase

131
Q

M3 receptors mediate ———– relaxation

A

sphincter, but mediate constriction on ciliary muscles (help with drainiage)

132
Q

M2 on heart can

A

reduce CO

133
Q

Most arteries and veins innervated by

A

symp adrenergic nerves

134
Q

Some blood vessels are innervated by parasympathetic cholinergic or sympathetic cholinergic nerves. These nerves release

A

acetylcholine as their neurotransmitter. Coronary arteries are a prominent example.

135
Q

Vascular endothelial cells express

A

m3 - this increases calcium in endothelial cells, ca/calmodulin leads to NOS upreg. THis leads to vasodilation, as NO increases cGMP production in muscle, which enhances MLCK phosphatase activity

136
Q

M3 on bronchial muscle mediate

A

contraction

137
Q

Secretory glands - m3 mediates

A

release of product

138
Q

———— amine better absorbed than ———- amine

A

tertiary, quarternary - tertiary actually can get through bbb

139
Q

Adverse effects of muscarinics

A

SLUD, Patients with asthma (bronchoconstriction), Cardiovascular disease (vasodilation, reduced cardiac output), ulcer (lacrimation)

140
Q

Anticholinesterases

A

increase cholinesteerase activity

141
Q

Irreversible anticholinesterases

A

fatal

142
Q

Anticholinesterases do not produce muscarinic receptor mediated vasodilation

A

because not much parasymp innervation of vascular endothelium

143
Q

Anticholinesterases can produce vasodilation via

A

autonomic ganglia

144
Q

Physostigmine (tertiary amine) can produce —————— effects through action in the CNS.

A

vasodilatory

145
Q

Pilocarpine and cevimeline (muscarinic agonists) frequently used to treat

A

dry mouth (patient needs functional salivary gland).

146
Q

anticholinesterases used to terminate neuromuscular block in

A

curare like agents

147
Q

Anticholinesterases used to treat

A

myasthania gravis

148
Q

Anticholinesterases that cross BBB used to treat

A

alzheimers

149
Q

Using antimuscarinics places target under control of

A

symp - except for sweat glands, which inhibits sweating and can increase body temp

150
Q

Antimuscarinics can cause eye dilation and lack of

A

accomodation - would cause serious rise in pressure in glaucoma cases

151
Q

Antimuscarinics can be used to produce

A

bronchodiilation and help with COPD

152
Q

Antimuscarinics inhibit gastric

A

motility,secretion at high impractical levels

153
Q

Antimuscarinics block parasymp mediated

A

secretion

154
Q

Antimuscarinics can be used as

A

antidote to anticholinesterases, to decrease salivary flow before procedure, treatment of COPD, dilate pupils

155
Q

Nondepolarizing blockers

A

competitive antagonists of acetylcholine

156
Q

Succinylcholine

A

depolarizing blocker. Two phases of action, chronic activation of achrs and then deacvitation of sodium channels, long term removal of achrs due to desensitization.

Pharmacology (19 decks)

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