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Pharmacology > The Vascular system > Flashcards

The Vascular system Flashcards

1
Q

• released by the kidneys in response to decreased perfusion

-Converts angiotensinogen to angiotensin 1

A

Renin

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2
Q
  • released by liver

* converted to angiotensin I by renin

A

Angiotensinogen

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3
Q
  • no known activity

* converted to angiotensin II by ACE

A

Angiotensin I

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4
Q
  • causes vasoconstriction, salt retention, vascular growth

* stimulates release of aldosterone

A

Angiotensin II

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5
Q

Blocks renin activity on angiotensinogen

A

Direct renin inhibitor

aliskiren

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6
Q

Prevents ACE from converting angiotensin I to

angiotensin II

A

ACE inhibitors

captopril, enalapril, etc..

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7
Q

Blocks angiotensin II activity at the AT1 receptor

A

Angiotensin receptor blockers

candesartan, valsartan, etc..

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8
Q

Blocks the activity of aldosterone in the kidneys

and other tissues (i.e. heart, smooth muscle)

A 
Aldosterone antagonists 
(eplerenone and spironolactone)
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9
Q

• MOA: Direct renin inhibitor- prevent conversion of angiotensinogen to angiotensin I
• Use: Hypertension
• ADRs: Diarrhea(frequent), dyspepsia(occasional), Hypotension
• Drug-Drug interactions:• Increased levels when combined with CYP3A4 inhibitors like macrolide antibiotics
-Not commonly prescribed

A

Aliskerin

• Brand name: Tekturna®

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10
Q

Most all drugs that target the RAAS system have what side effect?

A

Hypotensin

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11
Q

What 2 things do ace inhibitors decrease?

A

ACE

Kininase II

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12
Q

What is the affect of ACE inhibitor decreasing Kininase II?

A

Increased bradykinin leading to cough and possible angioedema

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13
Q

If the drug ends in -pril, what type of drug is it?

A

ACE inhibitor

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14
Q

What are adverse drug rxns to ACE inhibitors?

Captopril

A

C Cough (up to 10%)
A Angioedema (<1%) / Agranulocytosis (rare)
P Potassium excess (hyperkalemia 1-10%)/Proteinuria (rare)
T Taste change (2-4%)
O Orthostatic hypotension (~5%)
P Pregnancy (contraindication)
R Renal artery stenosis- bilateral (contraindication)
I Increased serum creatinine (1-10%- transient)
L Leukopenia (rare) / Liver Toxicity (rare)

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15
Q

• MOA: inhibits the angiotensin converting enzyme blocking the conversion of angiotensin I to angiotensin II
• Use: Hypertension, heart failure, post-MI, kidney disease
• ADRs: Cough, angioedema, hypotension, acute renal insufficiency, hyperkalemia, taste disturbances/dry mouth(rare)
• Drug-Drug interactions:• NSAIDs- reduced anti-hypertensive effect
• Alcohol- increased anti-hypertensive effect
• General anesthesia- increased anti-hypertensive effect
• Orthostatic hypotension:
• After supine positioning, have patient sit upright for
at least 2 minutes before standing to avoid orthostatic hypotension
• Monitor vital signs
• ACE Inhibitor induced cough may make longer dental procedures
difficult
• If dental surgery is anticipated evaluate risk of hypotensive episode

A

Lisinopril

• Brand name: Prinivil® or Zestril®

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16
Q

If the drug ends in -sartan, what type of drug is it?

A

ARB

Angiotensin Receptor Blocker

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17
Q

What are the 3 adverse drug reactions of ARB?

HDH

A

Headache / Hypotension
Dizziness
Hyperkalemia

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18
Q

• MOA: Blocks the AT1 receptor of angiotensin II
• Use: Hypertension, heart failure, kidney disease
• ADRs: Hypotension, dizziness, and hyperkalemia
• Drug-Drug interactions:• Sedative medications- increased anti-hypotensive effects
• NSAIDs- reduced anti-hypertensive effect
• General anesthesia- increased anti-hypertensive effect
• Orthostatic hypotension:
• After supine positioning, have patient sit upright for
at least 2 minutes before standing to avoid orthostatic
hypotension
• Monitor vital signs
• If dental surgery is anticipated evaluate risk of hypotensive episode

A

Candesartan

• Brand name: Atacand®

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19
Q
  • MOA: Sacubitril inhibits neprilysin resulting in elevated levels of B-type natriuretic peptide (BNP) and valsartan blocks the angiotensin II AT1 receptor
  • Use: Heart Failure reduced ejection fraction (HFrEF)
  • ADRs: Hypotension (18%), hyperkalemia (12%), angioedema (1-2%)
  • Drug-Drug interactions:• ACE inhibitors- increased risk of angioedema
  • Dental implications: Watch to hypotension upon rising
A

Angiotensin Receptor Neprilsyn Inhibitor (ARNI)

• Brand name: Entresto®

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20
Q

Is there more or less hypotension with ARNI?

A

More

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21
Q

What are the 2 aldosterone antagonists?

A

spironolactone

eplerenone

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22
Q

• MOA: Competitively inhibits the action of aldosterone• May also be referred to as a potassium-sparing diuretic
• Use: Hypertension, heart failure, liver failure, edema, primary hyperaldosteronism
• ADRs: Hyperkalemia, renal insufficiency, gynecomastia(males), dry mouth
• Drug-Drug interactions:• NSAIDs
• reduced anti-hypertensive effect
• Increased risk of nephrotoxicity
• Monitor vital signs
• Assess salivary flow as a factor in caries,
periodontal disease, and candidiasis secondary to
dry mouth from diuretic effect

A

Spironolactone

• Brand name: Aldactone®

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23
Q

___ is responsible for myosin and actin muscle contraction of smooth muscle

A

Ca

24
Q

• Produced in vascular tissue, smooth muscle, brain,

kidney, intestines, and adrenal gland

A

Endothelin-1

25
Q

• Produced in kidney and intestines

A

Endothelin-2

26
Q

• Produced in brain, kidney, intestine, adrenal gland

A

Endothelin-3

27
Q

Endothelin Rc
vasoconstriction, bronchoconstriction, Increased
aldosterone secretion

A

ETA-

28
Q

Endothelin Rc

- vasodilation, inhibition of platelet aggregation

A

• ETB

29
Q

• Activates guanylyl cyclase
resulting in Increases cGMP   [Ca++]
leading to relaxation

A

Nitric Oxide

30
Q 
• Binds to I prostanoid receptor (IP)
• Activates adenylyl cyclase 
resulting in Increase cAMP leading to less [Ca++] 
leading to relaxation 
• Also inhibit platelet aggregation
• PGG2 and PGH2- prostaglandin 
endoperoxide intermediates
• Have some constricting activity
A

• PGI2- prostacyclin

31
Q

Drugs ending in -dipines, what type of drug is it?

A

Dihydropyridine (Ca channel blocker)

32
Q 
\_\_\_\_\_\_\_ CCB
• More selective for calcium 
channels in peripheral 
vasculature 
• More effective for 
hypertension
A

Dihydropyridine

33
Q 
\_\_\_\_\_\_\_\_\_ CCB
• More selective for calcium 
channels in myocardium
• More effective for 
arrhythmias
A

Non-Dihydropyridine

34
Q

• MOA: Blocks L-type calcium channel in the vascular
smooth muscle (Dihydropyridine type)
• Use: Hypertension, and angina
• ADRs:
• Edema (common), dizziness, lightheadedness, hypotension, flushing,
gingival enlargement (rare- more common with DHP type)
• Drug-Drug interactions:
• Hypotension with sedatives, opioids, general and inhaled anesthetics
• NSAIDS reduce blood pressure lowering effect
• Gingival hyperplasia (up to 10%)
• Place on frequent recall to monitor for gingival hyperplasia
• Monitor vital signs
• Orthostatic hypotension:
• After supine positioning, have patient sit upright for at least 2
minutes before standing to avoid orthostatic hypotension
• Use vasoconstrictors and inhaled anesthetics with caution

A

Amlodipine

• Brand name: Norvasc®

35
Q 
Mechanism of action: 
• Opening KATP channels
• Resulting in hyperpolarization of 
cells
• Turns off voltage dependent Ca++ 
channels
• Lowering the intracellular Ca++ 
concentration 
• Resulting in vascular smooth 
muscle relaxation
A

Minoxidil

36
Q
  • MOA: causes smooth muscle relaxation by opening KATP channels
  • Use: Severe resistant hypertension
  • ADRs: Hair growth, edema, photosensitivity(rare)
  • Drug-Drug interactions:• Reduced anti-hypertensive effect with NSAIDs and sympathomimetic
  • Increased anti-hypertensive effect with sedatives and other drugs used for conscious sedation
A

Minoxidil

• Brand name: Loniten®

37
Q
  • MOA: causes smooth muscle relaxation by increasing intracellular nitric oxide concentrations
  • Use: Hypertensive crisis
  • ADRs: Methemoglobinemia, hypotension, dizziness, thiocyanate toxicity
  • Drug-Drug interactions: • PDE-5 inhibitors (i.e. sildenafil)
  • Dental implications:• none
A

Sodium Nitroprusside

• Brand name: Nitropress®

38
Q 
Proposed MOA:
interference with action 
of IP3 on calcium release 
from sarcoplasmic 
reticulum
A

Hydrazaline

39
Q 
\_\_\_\_ MOA:
Donates a NO which increases cGMP then causing vasodilation
-• Only available for intravenous 
administration
• Used for acute control of 
hypertension
A

Sodium nitroprusside

40
Q

• MOA: Direct acting vasodilator thru interference with action of
IP3 on calcium release from sarcoplasmic reticulum
• Use: Hypertension, and heart failure
• ADRs:
• Headache, palpitations, GI disturbances, flushed face(rare)
• Drug-Drug interactions:
• Reduced anti-hypertensive effect with NSAIDs and
sympathomimetic

A

Hydralazine

• Brand name: Apresoline®

41
Q

Defined by a mean pulmonary artery pressure ≥ 25mmHg at rest

A

Pulmonary hypertension

42
Q

Group ___ pulmonary hypertension:

Pulmonary arterial HTN (PAH) – primary pulmonary HTN

A

Group 1

43
Q

Group ___ pulmonary hypertension:

Pulmonary HTN due to left heart disease

A

Group 2

44
Q

Group ___ pulmonary hypertension:

Pulmonary HTN due to lung disease

A

Group 3

45
Q

Group ___ pulmonary hypertension:

Chronic thromboembolic pulmonary HTN (CTEPH)

A

Group 4

46
Q

Group ___ pulmonary hypertension:

Pulmonary HTN with unclear mechanism

A

Group 5

47
Q

What type of pulmonary hypertension med is offered both orally or parenterally?

A

Prostcyclin analouges

Treprostinil

48
Q 
Mechanism of action: 
• Block the ETA receptor 
• Decreasing the formation of IP3
• Lowering the intracellular Ca++ 
concentration 
• Resulting in vascular smooth 
muscle relaxation
Most  block both ETA and ETB
- but have a high affinity for ETA
A

ERAs Endothelin receptor antagonist

49
Q

• MOA: Endothelin 1 receptor antagonist
• Use: Pulmonary hypertension WHO FC III and IV
• ADRs:
• Headache, flushed face, dyspepsia, liver dysfunction
• Drug-Drug interactions:
• Increased levels when used with ketoconazole
• Pregnancy category- X aka DON’T USE
• Monitor vital signs
• High risk patient
• Acute pulmonary hypertension could occur
• Bleeding gums has been reported with endothelin receptor
antagonists (no specific reports with bosentan)
• Limit or avoid vasoconstrictors
• Low risk of orthostatic hypotension

A

Bosentan

• Brand name: Tracleer®

50
Q 
Mechanism of action: 
• Inhibit action of PDE5
• Increase intracellular cGMP 
concentration
• Lowering the intracellular Ca++ 
concentration 
• Resulting in vascular smooth 
muscle relaxation
 They are also used 
(more commonly) to treat erectile 
dysfunction
A

PDE5 inhibitors

51
Q

• MOA: Phosphodiesterase 5 inhibitor
• Use: Pulmonary hypertension, erectile dysfunction, and BPH
• ADRs:
• Headache, flushed face, dyspepsia, rash
• Drug-Drug interactions:
• Sodium Nitroprusside- avoid combination- severe hypotension
• Increased levels with CYP 3A4 inhibition (i.e. erythromycin,
clarithromycin, etc.)
• Monitor vital signs
• High risk patient- if using for PAH
• Acute pulmonary hypertension could occur
• Limit or avoid vasoconstrictors
• Avoid use of nitroglycerin of nitroprusside
• Low risk of orthostatic hypotension

A

Sildenafil

• Brand name: Revatio™(PAH) or Viagra®(ED)

52
Q 
Mechanism of action: 
• Bind to prostacyclin receptor (IP)
• Stimulate activity of adenylate 
cyclase (AC)
• Increase intracellular cyclic AMP 
levels 
• Lowering the intracellular Ca++ 
concentration 
• Resulting in vascular smooth 
muscle relaxation
A

Prostacyclin analogues

53
Q
  • MOA: Prostacyclin analogue
  • Use: Pulmonary hypertension
  • ADRs:
  • Headache, flushing, hypotension, infusion site pain
  • jaw pain, inhibition of platelet aggregation (Increased r/o bleeding)
  • Drug-Drug interactions:
  • Other drugs that increased r/o bleeding (i.e. NSAIDS)
  • Monitor vital signs
  • High risk patient
  • Acute pulmonary hypertension could occur
  • Continuous infusion can not be interrupted
  • Increased risk of bleeding
  • Inhibits platelet aggregation
  • Limit or avoid vasoconstrictors
A

Treprostinil

• Brand name: Orenitram®(PO), Tyvaso™(INH), Remodulin™(IV/SQ)

54
Q
  • MOA: IP receptor agonist
  • Use: Pulmonary hypertension Group I
  • ADRs:
  • Flushing, Headache(65%), diarrhea (42%)
  • Jaw pain (26%)
  • Drug-Drug interactions:
  • None noted
  • Monitor vital signs
  • High risk patient
  • Acute pulmonary hypertension could occur
  • Limit or avoid vasoconstrictors
A

Selexipag

• Brand name: Uptravi®

55
Q 
Mechanism of action: 
• Sensitizes guanylyl cyclase to nitric 
oxide but also directly activates 
guanylyl cyclase
• Increase intracellular cGMP 
concentration
• Lowering the intracellular Ca++ 
concentration 
• Resulting in vascular smooth 
muscle relaxation
A

Soluble guanylate cyclase stimulator

56
Q

Soluble guanylate cyclase stimulator

  • MOA: Soluble guanylate cyclase stimulator
  • Use: Pulmonary hypertension group 1 and 4 (CTEPH)
  • ADRs:
  • Hypotension, dyspepsia, headache, edema
  • Drug-Drug interactions:
  • Avoid combination with PDE5 inhibitors
  • Decrease effects with CYP 3A4/2C8 inducers
  • Pregnancy category- X
  • Monitor vital signs
  • High risk patient
  • Acute pulmonary hypertension could occur
  • Limit or avoid vasoconstrictors
  • Increased risk of bleeding
  • Risk of unanticipated bleeding during procedure
A

Riociguat

• Brand name: Adempas®

Pharmacology (12 decks)

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