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PHARM 203 > L6,L10 > Flashcards

L6,L10 Flashcards

1
Q

Drugs can target…

A

Receptors, ion channels, enzymes, transporters, structural proteins, DNA

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2
Q

Prazosin

A

Antagonist that treats hypertension by acting on A1-adrenoreceptors of SMC and keeps vessel dilated

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3
Q

Nifedapine

A

Treats hypertension via preventing Ca from entering L-type voltage-gated Ca Channel

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4
Q

Ion channel blocker

A

permeation blocked

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5
Q

ion channel modulator

A

increased or decreased probability of opening

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6
Q

Class A GPCR are aka

A

rhodopsin family

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7
Q

GPCR are aka

A

metabotrophic receptors

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8
Q

GPCR are for ____ acting transmitters and hormones

A

slow

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9
Q

GPCR are activated by

A

Agonist and protease mediated cleavage of N terminal

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10
Q

Captopril

A

Treats hypertension by preventing the conversion of angiotensin to angiotensin 1 which constricts the vessel so the vessel stays dilated instead

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11
Q

Bendroflume-thiazide

A

Treats hypertension by prevents reabsorption of Na and Cl which decreases blood volume and pressure

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12
Q

Ligands which bind to Class A GPCR include

A

amine neurotransmitters
neuropeptides
purines
prostanoids
cannabinoids

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13
Q

Class B GPCR are aka

A

secretin/glucagon family

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14
Q

Ligands which bind to Class B GPCR include

A

peptide hormones
(e.g., glucagon, calcitonin, secretin, parathyroid hormone

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15
Q

Class C GPCR are aka

A

metabotrophic glutamate receptor/Ca sensor family

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16
Q

Ligands which bind to Class C GPCR include

A

Glutamate (metabotrophic receptor)
GABA (GABA receptor)
Ca2+

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17
Q

Kinase-linked receptors are activated by?

A

Protein mediators
E.g., growth factors, cytokines, hormones

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18
Q

What are the main types of Kinase-linked receptors?

A

Receptor tyrosine kinases
Receptor Serine/Threonine Kinases
Cytokine receptors

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19
Q

Receptor tyrosine kinases are receptors for? and are important for?

A

Growth Factors
Activating MAPK cascade and regulating gene transcription

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20
Q

Transforming growth factor receptors is an example of?

A

Receptor serine/threonine kinase

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21
Q

Cytokine receptors have intracellular domains that bind and activate___?

A

cytosolic (tyrosine) kinases

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22
Q

cytokine receptors are important for _______

A

Immune and inflammatory responses

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23
Q

Nuclear receptors often reside _____

A

reside in cytosol and translocate to nucleus upon ligand binding

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24
Q

Dexamethasone is a _____ and an example of _____ receptor

A

Antiinflammatory immune inhibiting drug used in COVID 19; increases transcription of inhibiting factor important to immune response
Nuclear receptor

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25
What are the two types of Nuclear receptors and describe
Class/type1: Dimerize upon ligand binding, translocate to nucleus, activate/repress gene expression by binding +/- hormone response elements Class/type2: constitutively in nucleus, use lipids/other metabolites as ligands and form heterodimers with Retinoid X receptor
26
Ion channels are?
water filled pores in cell membrane that can switch between open and closed states
27
Rate and direction of ion movement in ion channels is governed by
Electrochemical gradient & membrane potential
28
Na, K, Ca and Cl want to move ___ to the cell
Na, Ca, Cl into the cell K out of the cell
29
Ion channels are characterized by
Selectivity (what is allowed through) and gating (what will open; voltage or ligand)
30
ligand gated ion channels are aka
ionotrophic receptors
31
Describe structure of ligand-gated ion channel
Usually have a tetrameric or pentameric structure (5 subunits) consisting of 4 types of subunits α, β, γ, & δ
32
Ligand-gated ion channels are important for ____?
Fact synaptic events and neuromuscular junction
33
4 types of ligand-gated ion channels
cys loop (e.g., nicotinic) Ionotropic glutamate (NMDA receptor) P2X type Ca2+ release
34
The ANS consists of
Sympathetic system parasympathetic system enteric system
35
ANS controls
heart beat visceral and smooth muscle exocrine and some endocrine secretions energy metabolism
36
Two main neurotransmitters of ANS
Acetylcholine Noradrenaline
37
Preganglionic efferent neurons release ____ onto ______ in ANS
Acetylcholine nicotinic receptors
38
postganglionic efferent neurons release ______ onto _____ in sympathetic system
noradrenaline a&b adrenoreceptors Exception: adrenal medulla (Ach on nic) and sweat glands (NA on musc)
39
postganglionic efferent neurons release ______ onto _____ in parasympathetic system
acetylcholine muscarinic
40
Nicotinic receptors are ____ with a ____ structure
ligand gated ion channels pentameric structure
41
What are the nicotinic receptor subtypes
Ganglionic CNS muscle
42
Histamine What is it? Where is it found? What does it do/why important?
Basic amine derived from histidine Found in most tissues but highest in skin, lungs, GI tract (mucous membranes) but also found in brain (neurotransmitter) and stomach (gastric acid secretion) Tissue histamine is proportional to mast cell content Mediator of immediate allergic and inflammatory reactions
43
Describe histamine secretion from mast cells
Histamine is released during inflammatory and immune reactions Allergen binds to surface of mast cells (IgE mediated), binding causes rise in intracellular Ca levels which causes degranulation Histamine release can also be stimulated from complement system
44
Describe Histamine receptors
H1-4 G-protein coupled H1-allergic reactions H2 -gastric acid secretion Found in most major tissues
45
Histamine binding causes
-Contracts smooth muscle (bronchi/bronchioles, ileum and uterus) -Dilates and increases permeability of blood vessels (Histamine binds H1 in endothelial cells which generates NO which dilates vessels) -Increase HR -Stimulates secretion of gastric acid -Wheal and flare rxn of skin (local vasodilation, increased vascular permeability, migration of immune cells, stimulation of nerve endings (itch/pain))
46
Antihistamines exert their effects by primarily acting on
H1 receptors
47
Peptic ulcer drugs act as
H2 antagonist
48
Cimetidine
H2 antagonist Peptic ulcer drug
49
Antihistamines act as a ___ and do what to histamine receptors?
Inverse agonists block receptor in an inactive state
50
Diphenhydramine
aka benadryl antihistamine inverse agonist?
51
Centrizine
aka reactine inverse agonist antihistamine
52
Loratidine
aka clathritin inverse agonist antihistamine
53
5-Hydroxytryptamine is aka
Serotonin
54
5-HT is synthesized from _____ and degraded by ____?
tryptophan monoamine oxidase
55
5-HT functions as a ______
local hormone in vascular system and neurotransmitter in CNS
56
5HT is found in
enterochromaffin cells platelets CNS
57
5HT1 and 5HT2 are for
1) vasoconstriction on large vessels and arteries 2) vasodilation on smaller vessels
58
What are the stages of a migraine? Describe
1) premonitory phase – nausea, mood changes, sensitivity to light/sound 2) aura – photophobia/phonophobia, visual symptoms 3) headache – moderate/severe headache 4) postdromal phase – fatigue, altered cognition/mood
59
Migraine origin theories
1) vascular origin 2)brain 3) neuroinflammation
60
Sumatriptan NOTE: -TRIPTAN
For Acute migraine Antimigraine drug 5-HT1 agonist constrict cerebral arteries and inhibits trigeminal nerve transmission Unwanted effects: coronary vasoconstriction, dysrhythmia
61
Pizotifen
5-HT2 antagonist antimigraine Prophylaxis prevent constriction of cerebral arteries Unwanted effects: Weight gain, sedation and antimuscarinic effects
62
Cyproheptadine
5-HT2 antagonist antimigraine Prophylaxis Can be used for carcinoid syndrome prevent constriction of cerebral arteries Unwanted effects: Weight gain, sedation and antimuscarinic effects
63
Erlotnib NOTE -NIB
Inhibits tyrosine kinase receptors in growth factor signalling tx: cancers
64
Sunitnib NOTE: -NIB
Inhibits tyrosine kinase receptors in growth factor signalling Inhibits signalling of vascular endothelial factor which stimulates cells to proliferate (req for tumor growth) tx: cancers
65
Adalimumab
aka humira Monoclonal antibody against TNFa (tumor necrosis factor) tx: rheumatoid arthritis, chrohn's disease
66
A1 and A2 coupled to ____ and cause what effects w/i body
Adrenoreceptors A1: Gq; Constrict SM A2: Gi: decrease release from nerve terminal

PHARM 203 (4 decks)

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