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Basic Science Concepts > Enzyme Systems/ MAO inhibitors/Hypertensive crisis/Serotonin Syndrome > Flashcards

Enzyme Systems/ MAO inhibitors/Hypertensive crisis/Serotonin Syndrome Flashcards

1
Q

Acetylcholinesterase:

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - breaks down (ACh) acetylcholine

drugs- donepezil, rivastigmine, galantamine
drug class- acetylcholinesterase inhibitors
“These drugs block the enzyme and prevent it from breaking down the acetylcholine”

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2
Q

(ACh) acetylcholine

A
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3
Q

Angiotensin-converting enzyme:

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - takes Angiotensin I and transforms it into Angiotensin II

drugs- lisinopril/enalapril/ramipril

drug class- ACE inhibitors
“ These drugs block the ACE enzyme and prevent formation of Angiotensin II and prevent vasoconstriction”

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4
Q

Renin is released from the _______

A

Kidneys

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5
Q

Angiotensinogen is released from the ________

A

Liver

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6
Q

Angiotensin II is ______________

A

a potent vasoconstrictor

&

increases aldosterone secretion which leads to retention of Na and H2O

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7
Q

catechol-O-methyltransferase (COMT):

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - breaks down Levodopa

drugs- entacapone
tolcapone? works across bbb?

drug class- COMT inhibitors
“ prevent the breakdown of Levodopa in the peripheral circulation, allowing more to cross the blood brain barrier”

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8
Q

Monoamine oxidase:

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - is responsible for the breakdown of catecholamines (neurotransmitters)

drugs- Tranylcypromine/Phenelzine/Selegiline/Isocarboxazid/Rasagiline/

-Linezolid & Methylene Blue also have activity

drug class- MAO inhibitors

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9
Q

There are MAO inhibitors that are selective and nonselective:

which drugs are selective?

A
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10
Q

MAO inhibitors when used in combination with other MAO inhibitors or other medications that work in similar pathways can result in adverse effects including:

A

Hypertensive Crisis

Serotonin Syndrome

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11
Q

Xanthine oxidase:

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - responsible for the production of Uric acid in the purine metabolism pathway

drugs- Allopurinol, Febuxostat

drug class- Xanthine Oxidase Inhibitors

  • inhibit enzyme and decrease Uric acid production, which brings down Uric acid levels
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12
Q

Goal Uric acid level in someone with Gout?

A
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13
Q

Hypoxanthine gets converted into Xanthine with what enzyme?

A

Xanthine Oxidase

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14
Q

Xanthine gets converted into Uric acid with what enzyme?

A

Xanthine Oxidase

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15
Q

Cyclooxygenase 1 & 2:

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - takes Arachidonic acid and converts it to Prostaglandins (are involved in inflammation processes& symptoms of pain) and Thromboxane A2 (stimulates platelet aggregation, specifically for Cardiovascular system)

drugs- (ibuprofen/naproxen/aspirin)
Block COX enzymes and prevent formation

drug class-NSAIDs

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16
Q

Phosphodiesterase:

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - is responsible for the breakdown of (cGMP) Cyclic Guanosine Monophosphate

drugs- Viagra/Cialis

drug class- PDE-5 inhibitors

prevent the breakdown of cGMP by inhibiting the phosphodiesterase enzyme

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17
Q

(cGMP) Cyclic Guanosine Monophosphate causes:

A

Smooth Muscle relaxant

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18
Q

Vitamin K epoxide reductase (VKOR):

Endogenous effect of enzyme -

what drugs/drug class inhibit?

A

Endogenous effect of enzyme - Converts Vitamin K into its active form “reduced Vitamin K”. This is needed to activate inactive clotting factors

drugs- warfarin

drug class- VKORC1 inhibitor

warfarin impairs the ability to activate clotting factors 2,7,9 & 10. Which helps to treat and prevent blood clots.

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19
Q

carboxylase:

A

takes the inactive clotting factors 2, 7, 9, & 10 and uses reduced Vitamin K (the active form which is required) and puts them in there active state

20
Q

Dopamine acts as a substrate for the enzyme _________ to be changed into _____________

A

MAO & COMT

NE

21
Q

(NE) Norepinephrine acts as a substrate for the enzyme __________ to be changed into ____________

A

MAO

Epi = Epinephrine

22
Q

Serotonin (5-HT) is broken down into harmless metabolites by what enzyme?

A

(MAO) Monoamine oxidase

23
Q

(MAO) Monoamine Oxidase is responsible for the breakdown of ___________

A

catecholamines

24
Q

When MAO inhibitors are used with other medications that increase NE & Epi, there is an increased risk for ___________

A

Hypertensive Crisis (medical emergency)

increases BP, HR rapidly

25
Q

what drugs can contribute to increases in the catecholamines NE and Epi?

A

bupropion
SNRIs
TCAs
amphetamines/stimulants (decongestants and other meds to Tx ADHD)
Linezolid
Methylene Blue
Tyramine-rich foods (aged/fermented/smoked foods including cheeses, pickled harring, wines and beers and air/dried meats) - these are problematic because Tyramine is also broken down by the MAO enzyme.

26
Q

The risk of Hypertensive Crisis when switching from one MAO agent to another can be prevented/decreased by having _______

A

a washout period

27
Q

When multiple drugs are taken that can increase Serotonin, there is increased risk for ___________

A

Serotonin Syndrome

28
Q

what drugs can increase the risk for Serotonin Syndrome when multiple agents are taken?

A

SSRIs
SNRIs Methadone
TCAs Meperidine
mirtazapine Centrally acting analgesics - tapedolol, tramadol
trazodone
St. Johns wart
Opioids
tramadol
Antiemetics (ondansetron)
Buspirone
Lithium - drug activates serotonin receptors
Triptans
ergotamines
dextromethophan (if abused)

29
Q

Serotonin Syndrome Symptoms

A
  • Diaphoresis
  • Agitation = altered mental status
  • Tachycardia
  • Mydriasis = pupil dilation
  • Autonomic instability & hypertension
  • Diarrhea & hyperactive bowel sounds
  • Hyperreflexia
    -Tremor
    -Clonus = muscle contractions

can progress with delirium and seizures, which can be fatal.

30
Q

Triptans like Sumatriptan are __________

A

Serotonin agonists

31
Q
A
32
Q
A
33
Q
A
34
Q

CYP2C19

A
35
Q

CYP2C9

A
36
Q

CYP2CP

A
37
Q

CYP2D6

A
38
Q

CYP2D6

A
39
Q

CYP3A4 inducers:

A
40
Q

CYP3A4 inhibitors:

A
41
Q
A
42
Q
A
43
Q
A
44
Q
A
45
Q
A

Basic Science Concepts (7 decks)

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