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SRNAPharmacology I > Selective PDE III Inhibitors > Flashcards

Selective PDE III Inhibitors Flashcards

1
Q

PDE III inhibitors decreases the degradation of cellular cAMP which results in (ACTION IN CARDIAC MUSCLE)

A

Increase levels of cAMP leads to an increase in intracellular calcium concentration in cardiac muscles and produces POSITIVE inotropic effects and increased speed of relaxation

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2
Q

Agents PDE III also called

A

cyclic AMP-PDE III inhibitors.

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3
Q

Effects of catecholamines are ________ why?

A

increased; because they also increased concentration of cAMP through beta-adrenergic receptors

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4
Q

Milrinone: Useful in the management of acute

A

acute left ventricular dysfunction as may follow cardiac surgery or an acute MI

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5
Q

What is milrinone?
A_________ derivative that is a _______ ________, PDEIII inhibitor that produces dose-dependent positive ________
and _________properties with minimal effect on ________ and ______ _______

A

A bipyridine derivative that is a selective, competitive, PDEIII inhibitor that produces dose-dependent positive inotropic
and vasodilating properties with minimal effect on heart rate and myocardial oxygen consumption

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6
Q

Milrinone

A

Better than inamrinone

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7
Q

Action of Milrinone : Increased are _____and _______
Decreased are :
Unchanged or slightly increased?

A

CO, Contractility
SVR, PVR, (mean pulmonary artery pressure)
afterload, preload, venous return
HR.

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8
Q

Mechanism of action of Milrinone

A

-positive lusitropic (myocardial relaxation) effect
facilitates diastolic relaxation, decreases right and left ventricular end- diastolic pressures (right and left heart filling pressures decreased)
decreases pulmonary capillary wedge pressure
decreased wall tension

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9
Q

Effects of milrinone on SV :

A

Decreased:
Afterload
Preload and venous return to the heart.

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10
Q

Compared with dobutamine, as

A

less tachycardia
move vasodilation
Greater decreases SVR and BP
More effective at decreasing cardiac filling

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11
Q

Compared with dobutamine, as Milrinone

A

less tachycardia
move vasodilation
Greater decreases SVR and BP
More effective at decreasing cardiac filling

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12
Q

Milrinone not used in

A

Severe obstructive aortic or pulmonic valvular disease

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13
Q

The inotropic effects of milrinone are decreased by _____? why?

A

ACIDOSIS; Presumably reflecting decreased cAMP formation in acidotic muscle

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14
Q

Milrinone should be avoided in severe Chronic HF why

A

Increased morbidity and mortality with chronic use.

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15
Q

Loading dose of milrinone

A

50mcg/kg administered over 10 MINUTES

followd by continuous infusion 0.375 -0.75 mcg/kg/min

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16
Q

Elimination half life of milrinone

A
  1. 3 hours
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17
Q

Elimination organ is ______ and_____ of milrinone is excreted ______. Therefore, dose should be decreased in patients with _________

A

Kidneys ; 80% unchanged in urine;

Renal insufficiency.

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18
Q

Adverse effects of MILRINONE

A

HYPOTENSION

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19
Q

What increases the risk of hypotension

What decreases the risk?

A

Loading dose

Slow administration

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20
Q

Milrinone can cause

A

Atrial or ventricular arrythmia

Nonsustained vtach or vfib

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21
Q

Inamrinone

Agent of choice is

A

does everything milrinone
Milrinone does it better
MILRINONE

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22
Q

Non-selective Phosphodiesterase Inhibitors

A

Theophylline and Aminophylline

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23
Q

Is structurally in the class of ________medications and is similar in structure to

A

methylxanthine ; Caffeine

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24
Q

Is a bronchodilating agent that also has anti-inflammatory, immunomodulatory and stimulatory properties

A

bronchodilating

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25
Q

Theophylline has______and is available in both ____ and ______routes

A

several mechanism of actions; IV and PO

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26
Q

Theophylline is recommended IV for the treatment of ________ and _________

A

bronchospasm due to an acute exacerbation of asthma and for reversible airflow obstruction.

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27
Q

Treat primary _______of prematurity

stimulates respiratory medullary centers

A

apnea

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28
Q

Inhibition of these isoenzymes

mediates_______

A

mediates smooth muscle relaxation through accumulation of both intracellular cGMP & cAMP, resulting in bronchodilation of airway smooth muscle

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29
Q

Is a ________ -________ inhibitor of phosphodiesterase enzymes (primarily PDE III and, to a lesser extent, PDE IV).

A

weak, nonselective, competitive

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30
Q

Theophilline puts the patients

A

risk for aspiration

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31
Q

Theophilline Is a competitive antagonist of _____ -_________receptors, resulting in antagonism of ____________ leading to smooth muscle relaxation and bronchodilation

A

A1 and A2 adenosine receptors; bronchoconstriction

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32
Q

Theophilline has several anti-inflammatory effects

A

Inhibits the release of histamine and leukotrienes
Reduces the number of eosinophils and neutrophils
Reversal of glucocorticoid resistance by theophylline

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33
Q

Theophylline: Mechanism of Action

Is a CNS ________

A

Increases the force of contraction of DIAPHRAGMATIC MUSCLES (because of enhanced calcium uptake through adenosine mediated channel)
-stimulant

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34
Q

Theophylline : Is a cardiovascular stimulant by ______ ______therefore HR and CO are _____

A

stimulating the release of endogenous catecholamines ; increased.

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35
Q

Theophylline on heart side effects

A

tachycardia

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36
Q

Theophylline has a ______TI

A

Narrow

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37
Q

Theophylline metabolized throught the liver

A

CYP 450

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38
Q

What speeds up the metabolism of Theophylline? Clear better

A

RPPCSC - SMOKING

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39
Q

Theophylline excretion

A

<10%

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40
Q

Aminophylline is _______Theophylline

A

80%

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41
Q

Both theophylline and aminophylline pass freely across the p_____ _______ _______ and produce ______ in ______

A

placenta, into breast milk and into cerebrospinal fluid and can produce toxicity to neonates

42
Q

Mechanism of action of aminophylline

A

Same as theophylline.

43
Q

Therapeutic range of Theophylline

A

5-15 mg/L

44
Q

Affect clearance of theophylline

A

both the clinical status of the patient and medication will alter clearance of theophylline

45
Q

THeophylline 15-25mg/L

A

Tachycardia and palpitations

46
Q

THeophylline 15-25mg/L

A

Tachycardia and palpitations

47
Q

Theophylline. >25mg/L

A

Tachyarrhythmias- PVCs, Vtach

48
Q

Drugs that increase theophylline clearance

A

CYP 450 inducers

49
Q

Drugs that decrease theophylline clearance

A

CYP 450 inhibitors

50
Q

ANESTHASIA Considerations

A

Halothane sensitizes the myocardium to catecholamines, theophylline increases release of endogenous catecholamines
and results in increased risk of ventricular arrhythmias

51
Q

Theophylline =? Crosses the placental barrier

A

toxic to neonates

52
Q

Ketamine and theophylline

A

lower theophylline seizure threshold and increase risk of seizures in patients taking theophylline

53
Q

Discontinuing theophylline without reducing the dose of benzo may lead to

A

Respiratory depression

54
Q

Benzodiazepines such as diazepam and midazolam, Theophylline can decrease the effectiveness of diazepam or midazolam WHY? Therefore

A

-increase CNS concentrations of adenosine which is a potent CNS depressant, while theophylline blocks adenosine receptors.
- Larger doses of these agents may be required to
achieve neuromuscular blockade

55
Q

______ diazepam/midazolam doses may be required to produce a desired level of sedation.

A

Larger

56
Q

Discontinuation of theophylline without reduction of diazepam/midazolam dose may result in ______________

A

respiratory depression

57
Q

The inotropic effects of calcium are enhanced in patients with preexisting _______ or ______

A

-hypocalcemia or hyperkalemia

58
Q

With calcium, ________ in HR and systemic vascular resistance can be seen as well as ________ in systemic vascular resistance and MAP

A

Decreases; increases

59
Q

Calcium when given IV can produce an __________ effect and increased____ _____

A

-positive inotropic; stroke volume

60
Q

Duration of action calcium: ____minutes

A

10-20 minutes

61
Q

The risk of cardiac arrhythmias exist with calcium when _____especially if _______ is present.

A

when IV calcium is given to patients receiving digoxin, especially if hypokalemia is present

62
Q

Calcium chloride contain ______ more elemental calcium than calcium gluconate salt solutions. Typical dose of Calcium chloride is

A

~3 times; 5-10mcg/kg IV.

63
Q

1 gram of calcium chloride________amount of elemental calcium as giving 1gram of calcium gluconate

A

IS NOT THE SAME

64
Q

Calcium is used to :

A

Used to treat cardiac/myocardial depression that
-may follow termination of cardiopulmonary bypass
-may accompany the delivery of volatile anesthetics, the transfusion of citrated
blood or the use of potassium containing cardioplegia solutions

65
Q

Adverse reactions (3)

A

Rapid injection may cause hypotension, a tingling sensation, or a
sense of oppression or “heat wave”
Local “burning” sensation
Irritating to veins and local infiltration may occur

66
Q

PDE-III is found in high concentration in the

A

Myocardium and Vascular Smooth Muscle (VSM)

67
Q

PDE III INhbitors are : (class)

A

non-catecholamine and non-glycoside compounds

68
Q

PDE III inhibitors decreases the degradation of cellular cAMP which results in (ACTION IN SMOOTH MUSCLE)

A

In smooth muscle, increased levels of cAMP produce vasodilation of resistance and capacitance vessels.

69
Q

PDE–III Inhibition improves CO through _______ AND by _______ preload and afterload (aka ______)

A

INOTROPY
DECREASED
Inodilators.

70
Q

Selective PDEIII inhibitors will act _______ of beta adrenergic receptors and will increase ________ in those 3 types of patients?

A

Independently

  1. Patients with myocardial depsression from Beta adrenergic blockers
  2. Pt with down regulation of beta adrenergic receptors
  3. Patient who have become refractory to catecholamine therapy
71
Q

The hemodynamic response produced by PDE inhibitors exceeds that of ______and are _______with catecholamines, therefore, can be used in conjuction with ______

A

Digitalis
synergistic
Digoxin

72
Q

Why was INAMRINONE replaced by milrinone?

A

MORE frequent occurence of THROMBOCYTOPENIA

73
Q

Compared to Inamrinone, milrinone is

A
  • 20 times more potent as inotrope

- has enhanced vasodilatory properties causing a greater decrease in the LVP and BP

74
Q

Which medication has been shown to reverse VASOSPAMS in arterial grafts and is thought to have anti-inflammatory effects?

A

Milrinone

75
Q

Important to know that Theophylline is _____Effective than B2 adrenergic agonist and should only be used______

A

Less; when selective beta 2 adrenergic agonist and corticosteroid fail to produce adequate response.

76
Q

Phosphiesterase enzyme inhbition lead to ?

A

Smooth muscle relaxation through accumulation of both intracellular cGMP and cAMP, resulting in bronchodilation of airway smooth muscle.

77
Q

Some of the adverse effects associated with theophylline appear to be mediated by inhibition of PDE and include?

A 
inhibition of PDE III 
Hypotension
Tachycardia 
Headache 
Emesis
78
Q

Theophylline on CNS

A

Increased alertness

Increased ability to concentrate

79
Q

Stimulates the medullary respiratory centers by

A

Increasing the sensitivity of these centers to CO2

80
Q

Factors decreasing clearance of theophylline?

A

Age (reduced in neonates&Elderly)

Cirrhosis, CHF and fever

81
Q

Which has the most significant factor on increasing clearance for theophylline?

A

SMOKING

82
Q

Adverse effects of theophylline are related to plasma concentrations and at serum concentration greater than

A

20 mcg/ml

83
Q

Adverse effects of theophylline when levels are 15-25

A

NVHTP(Nausea vomiting headache, tachy and palpitation)

84
Q

Adverse effects of theophylline when levels are >25

A

Severe NVHTP
Tachyarrhythmias (PVCs, VTACH)
Seizures and deaths.

85
Q

Theophylline and neuromuscular blockade consideration

A

May antagoniz nondepolarizing neuromuscular blocking effects due to phosphodiesterase inhibition. Larger doses may be needed.

86
Q

Pentoxifylline is used to treat

A

intermittent claudication due to chronic occlusive arterial disease of the limbs.

87
Q

What is pentoxifulline?

Side effect

A

Methylxantine derivative which is a Hemorrheologic agent that increases flexibiltiy of erythrocytes and decreases viscosity of blood , therefore improving capillary blood flow and tissue oxygenation.
Nausea.

88
Q

Glucagon is a

A

polypeptide hormone produced by the alpha cells of the pancreas

89
Q

Glucagon is anti_______and has (effects on heart)
When given as a drug______
Tissues with glucagon receptor_______

A

Antihypoglycemic; Positive inotropic and chronotropic effects
**work as inotrope
Heart.

90
Q

Glucagon interacts with a __________ that stimulates _____ _______which increases the______ _______

A

G protein-coupled receptor (Gs on

the heart that stimulates ADENYLATE CYCLASE which increases the production of cAMP.

91
Q

With glucagon, the increased cAMP in the heart promotes _________

A

calcium ion influx which increases intracellular calcium concentrations and results in positive chronotropic and positive inotropic effects on the heart

92
Q

Does glucagon activate

or bind to beta-adrenergic receptors OR inhibit PDE ?

A

It does not; no

93
Q

Glucagon also evokes and tell nerves to release what?_______

Can be given in GI procedure to

A

The release of catecholamines

Reversing spasms of the sphincter of oddi

94
Q

The principle cardiac indication of glucagon:

A

is to increase myocardial contractility and heart rate in the presence of beta-adrenergic blockade (Used in the treatment of beta-blocker overdose)

95
Q

This drug is used in the treatment of beta-blocker overdose

A

GLUCAGON

96
Q

Rapid IV administration of 1-5mg of glucagon or a continuous infusion of 1-5 mg/hour results in increased
____________

A

increased
stroke volume (increased force of contraction) and heart rate
independent of beta-adrenergic stimulation

97
Q

CV adverse effects of Glucagon :

3

A
  1. Tachycardia that is great enough to interfere with cardiac output may occur
  2. Abrupt increases in heart rate may occur when glucagon is
    given to patients in atrial fibrillation
  3. MAP may increased whereas SVR may stay same or decreased
98
Q

not effective in evoking a sustained positive inotropic and chronotropic effect

A

The chronic administration of glucagon

99
Q

Glucagon side effects

A

Nausea and vomiting that is dose- dependent
Monitor for pulmonary aspiration
Tachycardia and hypertension
HYPOGLYCEMIA (may occur in patients that lack glycogen stores)
HYPOKALEMIA (increased secretion of insulin and subsequent intracellular shift of K+)

100
Q

Glucagon stimulates the release of catecholamines and may cause

A

hypertension in patients with unrecognized

pheochromocytoma’s

SRNAPharmacology I (29 decks)

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