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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
Q

What are the two types of Nuclear receptors and describe

A

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

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26
Q

Ion channels are?

A

water filled pores in cell membrane that can switch between open and closed states

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27
Q

Rate and direction of ion movement in ion channels is governed by

A

Electrochemical gradient & membrane potential

28
Q

Na, K, Ca and Cl want to move ___ to the cell

A

Na, Ca, Cl into the cell
K out of the cell

29
Q

Ion channels are characterized by

A

Selectivity (what is allowed through) and gating (what will open; voltage or ligand)

30
Q

ligand gated ion channels are aka

A

ionotrophic receptors

31
Q

Describe structure of ligand-gated ion channel

A

Usually have a tetrameric or pentameric structure (5 subunits) consisting of 4 types of subunits α, β, γ, & δ

32
Q

Ligand-gated ion channels are important for ____?

A

Fact synaptic events and neuromuscular junction

33
Q

4 types of ligand-gated ion channels

A

cys loop (e.g., nicotinic)
Ionotropic glutamate (NMDA receptor)
P2X type
Ca2+ release

34
Q

The ANS consists of

A

Sympathetic system
parasympathetic system
enteric system

35
Q

ANS controls

A

heart beat
visceral and smooth muscle
exocrine and some endocrine secretions
energy metabolism

36
Q

Two main neurotransmitters of ANS

A

Acetylcholine
Noradrenaline

37
Q

Preganglionic efferent neurons release ____ onto ______ in ANS

A

Acetylcholine
nicotinic receptors

38
Q

postganglionic efferent neurons release ______ onto _____ in sympathetic system

A

noradrenaline
a&b adrenoreceptors

Exception: adrenal medulla (Ach on nic) and sweat glands (NA on musc)

39
Q

postganglionic efferent neurons release ______ onto _____ in parasympathetic system

A

acetylcholine
muscarinic

40
Q

Nicotinic receptors are ____ with a ____ structure

A

ligand gated ion channels
pentameric structure

41
Q

What are the nicotinic receptor subtypes

A

Ganglionic
CNS
muscle

42
Q

Histamine
What is it?
Where is it found?
What does it do/why important?

A

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
Q

Describe histamine secretion from mast cells

A

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
Q

Describe Histamine receptors

A

H1-4
G-protein coupled
H1-allergic reactions
H2 -gastric acid secretion

Found in most major tissues

45
Q

Histamine binding causes

A

-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
Q

Antihistamines exert their effects by primarily acting on

A

H1 receptors

47
Q

Peptic ulcer drugs act as

A

H2 antagonist

48
Q

Cimetidine

A

H2 antagonist
Peptic ulcer drug

49
Q

Antihistamines act as a ___ and do what to histamine receptors?

A

Inverse agonists
block receptor in an inactive state

50
Q

Diphenhydramine

A

aka benadryl
antihistamine inverse agonist?

51
Q

Centrizine

A

aka reactine
inverse agonist
antihistamine

52
Q

Loratidine

A

aka clathritin
inverse agonist
antihistamine

53
Q

5-Hydroxytryptamine is aka

A

Serotonin

54
Q

5-HT is synthesized from _____ and degraded by ____?

A

tryptophan
monoamine oxidase

55
Q

5-HT functions as a ______

A

local hormone in vascular system and neurotransmitter in CNS

56
Q

5HT is found in

A

enterochromaffin cells
platelets
CNS

57
Q

5HT1 and 5HT2 are for

A

1) vasoconstriction on large vessels and arteries
2) vasodilation on smaller vessels

58
Q

What are the stages of a migraine? Describe

A

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
Q

Migraine origin theories

A

1) vascular origin
2)brain
3) neuroinflammation

60
Q

Sumatriptan

NOTE: -TRIPTAN

A

For Acute migraine
Antimigraine drug
5-HT1 agonist
constrict cerebral arteries and inhibits trigeminal nerve transmission

Unwanted effects: coronary vasoconstriction, dysrhythmia

61
Q

Pizotifen

A

5-HT2 antagonist
antimigraine
Prophylaxis

prevent constriction of cerebral arteries

Unwanted effects: Weight gain, sedation and antimuscarinic effects

62
Q

Cyproheptadine

A

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
Q

Erlotnib

NOTE -NIB

A

Inhibits tyrosine kinase receptors in growth factor signalling

tx: cancers

64
Q

Sunitnib

NOTE: -NIB

A

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
Q

Adalimumab

A

aka humira

Monoclonal antibody against TNFa (tumor necrosis factor)

tx: rheumatoid arthritis, chrohn’s disease

66
Q

A1 and A2 coupled to ____ and cause what effects w/i body

A

Adrenoreceptors
A1: Gq; Constrict SM
A2: Gi: decrease release from nerve terminal

PHARM 203 (4 decks)

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