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Year 2 > Drugs - Enzyme and transporters > Flashcards

Drugs - Enzyme and transporters Flashcards

1
Q

What is an enzyme inhibitor

A

A molecule that binds to an enzyme decreasing its activity

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2
Q

What are irreversible inhibitors

A

React with enzyme to change it chemically

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3
Q

What are reversible inhibitors

A

Bind non-covalently

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4
Q

What is the top most prescribed drug

A

Statin

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5
Q

How do statins work

A

Block rate limiting step in cholesterol pathway reducing bad cholesterol:

3-hydroxy-3-methylglutaryl-CoA to Mevalonic Acid

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6
Q

When are ACE inhibitors used

A

For BP

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7
Q

How does the RASS system work

A

Liver - > angiotensinogen -> angiotensin I -> angiotensin II in lung by ACE

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8
Q

What is the role of angiotensin II

A 
Tubular reabsorption of Na and CL
K excretion
H2o retention 
Arteriolar vasoconstriction 
Increased BP
ADH secretion 
Aldosterone secretion
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9
Q

Where is ACE found

A

Surface of pulmonary and renal endothelium

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10
Q

What is the consequence of inhibiting ACE

A

Reduces Angiotensin II levels

Causes reduction in BP

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11
Q

How is Parkinson’s disease treated

A

Many enzyme inhibitors that work in the nigrostriatal pathway to prevent dopaminergic degeneration

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12
Q

How is L-DOPA produced

A

From L-Tyrosine

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13
Q

Process of L-DOPA function

A
  1. L-DOPA crosses BBB from peripheral to CNS
  2. Converted to Dopa Decarboxyl
  3. Dopamine
  4. D1 and D2 receptors
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14
Q

How does carbidopa work

A

Prevents L-DOPA -> Dopamine in periphery to reduce levels

Acts on DDC

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15
Q

How do Tolcapone and Entacapone function

A

Prevent L-DOPA -> 3-methyl DOPA by inhibiting COMT

less dopamine

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16
Q

How do central COMT inhibitors work

A

Work directly in CNS (Tolcapone) by preventing Dopamine -> 3MT

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17
Q

What inhibitors act on MAO-B

A

Selegiline and Rasagiline act on MAO-B in CNS to stop Dopamine -> DOPAC

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18
Q

What dopamine receptor AGONISTS work on D1 and D2 receptors

A 
Pramipexole
Ropinirole
Rotigotine
Pergolide
Bromocryptine
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19
Q

Define transport

A

When molecules move across a cell membrane

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20
Q

What are uriporters

A

Use energy from ATP to pull molecule in

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21
Q

What are symporters

A

Use movement of one molecule to pull another molecule against a conc. gradient (co-transporter)

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22
Q

What are antiporters

A

One substance moves against conc. gradient using energy from a second substance moving DOWN its gradient (co-transporter)

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23
Q

Give an example of a symporter

A

NKCC

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24
Q

How do NKCCs work

A

Move ions n the same direction

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25
Why is furosemide a diuretic
Inhibits luminal NKCC in thick ascending loop of hence so Na, Cl and K lost in urine
26
When is Furosemide given
For hypertension and edema
27
What are ENaC channels inhibited by (Epithelial Na Channels)
Amiloride with Thiazide Thiazide targets Na/Cl cotransporters
28
When is amiloride and Thiazide used
Anti-hypertensives
29
What inhibits voltage-gated calcium ion channels
Amlodipine
30
Whats special about amlodipine
Its angioselective that stops movement of Ca into vascular smooth muscle and cardiac cells preventing Ca ion influx Results in vasodilation and peripheral vascular resistance decrease lowering BP + prevents excessive constriction in coronary arteries
31
What drug blocks transmission of action potential by voltage gated Na Channels
Lidocaine
32
When is Lidocaine given
To reduce arrhythmia by blocking signalling in the heart
33
What three states can voltage-gated K+ channels be found in
Closed Open Inactivated
34
Where can voltage gated potassium channels be found
In Beta cells of the islets of langerhans
35
Describe the release of insulin from the pancreas
1. Glucose enters beta cells by GLUT2 2. Glucose phosphorylated to glucose-6-phosphate by glucokinase 3. Glucose used in glycolysis increasing ATP:ADP ratio in cell 4. High ATP:ADP closes ATP-sensitive K+ channel 5. K+ ions accumulate in cell 6. Depolarisation 7. Voltage-gates calcium channels open 8. Causes vesicles containing insulin t one released
36
How many phases are involved in the release on insulin
Two: First -phase: Rapid release Second - phase: Slow release of newly formed vesicles
37
What hormone strongly inhibits the release of insulin
Noradrenaline
38
What three drugs block voltage-gated potassium channels involved in insulin secretion
Repaglinide Nateglinide Sulfonylureal
39
When is repaglinide, nateglinide and sulfonylureal prescribed
Type II diabetes
40
What are ligand-gated ion channels also known as
Ionotropic receptors
41
What is the role of GABA in the CNS
Major inhibitor
42
Where are GABA A receptors found
Post-synaptically
43
What happens when ligand binds to GABA A receptor
Cl- channel opens - hyper polarisation
44
In what way can drugs effect GABA A receptors
Enhance their activation (efficacy)
45
Role of barbiturates
Increase permeability of channel to Cl-
46
When is barbiturate given
Depressant
47
How do Benzodiazepine effect GABA-A receptors
Acts as an agonist (depressant)
48
What two other drugs can effect GABA-A receptors and why do they bring out different outcomes
Steroids (anaesthetics) Picrotoxins (convulsants) They bind to different sites within the child ride channel
49
How do Na/K ATPase work
Pumps 3Na out and 2K into cells
50
What type of transporter is Na/K ATPase
antiporter
51
What drug inhibits the Na/K ATPase and in which part of the body
Digoxin in the myocardium
52
When is digoxin used
Atrial fibrillation, atrial flutter and heart failure
53
What is the consequence of digoxin
Increased intracellular Na and Ca as activity of Na/Ca exchanger decreases Leads to a decrease in heart rate by lengthening cardiac action potential
54
Where are K/H ATPase found
Stomach
55
What type of protein are H/K ATPase
Heterodimeric
56
Define heterodimeric
Product of 2 genes
57
How do K/H ATPase function
Move H+ ions out into stomach lumen and K+ into cell
58
Role of Omeprazole
Inhibits acid secretion by inhibiting H/K ATPase irreversibly
59
Half-life of Omeprazole
1 hour
60
How long does Omeprazole work for
2-3 days
61
Under what conditions is Omeprazole metabolised (activated)
Acid pH which alters its own bioavailability
62
What cell releases PGE2 (Prostaglandin E2)
Chromaffin cells
63
What do PGE2 bind to
EP3 receptors on parietal cells
64
What is the consequence of PGE2 binding
Decreased activity of H/K ATPase - inhibits parietal cells
65
What is the antagonist to PGE2
Histamine
66
What two irreversible inhibitors of ACh esterase
1. Insecticides (Siazinon) | 2. Nerve gas (Sarin)
67
Symptoms of muscarinic receptor irreversible inhibition
Salivation, Defecation, Urination, Bradycardia, Hypotension
68
Symptoms of nicotinic receptor irreversible inhibition
Twitching, severe weakness paralysis, diaphragm
69
Symptoms of irreversible inhibition to the CNS
Confusion Loss of reflexes Convulsion Coma
70
Define Pharmacokinetics
Study of drug metabolism
71
Define xenobiotics
Compounds foreign to an organism's normal biochemistry such as a drug
72
What are the principals of pharmacokinetics
MADE M-etabolism A-bsorption (how will it get in?) D - Distribution (where will it go?) E - xcretion (how does it leave)
73
Where are CYPs found
Inner membrane of mitochondria or ER
74
role of CYPs
Deactivation of drugs (75% of all metabolisms) or bioactivation of drugs

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