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PHARMACOLOGY > Pharm PNS III > Flashcards

Pharm PNS III Flashcards

1
Q

For sympathoMIMETICS, which drugs are direct-acting catecholamines?

A
  • epinephrine
  • norepinephrine
  • isoproterenol
  • dopamine
  • dobutamine
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2
Q

For sympathoMIMETICS, which drugs are direct-acting alpha-1 agonists?

A

Phenylephrine

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3
Q

For sympathoMIMETICS, which drugs are non-selective Beta agonists?

A
  • Ractopamine

- Zilpaterol

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4
Q

For sympathoMIMETICS, which drugs are Beta2 agonists?

A
  • Albuterol
  • Terbutaline
  • Clebuterol
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5
Q

For sympathoMIMETICS, which drugs are mixed (direct and indirect acting) agonists?

A
  • ephedrine
  • pseudoephedrine
  • phenylpropanolamine (PPA)
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6
Q

For sympathoLYTICS, which drugs are direct-acting alpha antagonists?

A
  • phenoxybenzamine

- Prazosin

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7
Q

For sympathoLYTICS, which drugs are direct-acting beta antagonists?

A
  • Propanolol
  • Sotalol
  • Atenolol
  • Metoprolol
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8
Q

For sympathoLYTICS, which drugs are direct-acting mixed alpha and beta antagonists?

A

Carvedilol

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9
Q

For sympathoLYTICS, which drugs are indirect-acting antagonists?

A

Reserpine

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10
Q

For D1 receptors what organs can it be found on and what is the action once it has been bound to its substance?

A
  • smooth muscle of blood vessels in most organs
    • JG apparatus
    • renal tubules
  • direct vasodilation
  • natriuresis
    • inhibit 2Na+/K+ ATPase and Na+/H+ exchanger in PCR, ALOH, CCDs
    • diuretic response due to increased RBF and GFR as well as direct natriuresis
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11
Q

For D2 receptors what organs can it be found on and what is the action once it has been bound to its substance?

A
  • post-ganglionic sympathetic nerve terminals
  • glomeruli, renal cortex and renal tubules
  • adrenal cortex (zona glomerulosa cells)
  • chemoreceptor trigger zone in the brain
  • indirect vasodilation –> inhibits NE release from sympathetic terminals (pre-junctional)
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12
Q

Which catecholamines can be found endogenously?

A
  • Epinephrine
  • Norepinephrine
  • Dopamine
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13
Q

What are some general properties for catecholamines?

A
  • direct acting sympathoMIMETICS
  • orly absorbed after oral administration (usually given by injection
  • readily absorbed from respiratory tract –> inhalation is the next best route for absorption and distribution if IV route is not an option
  • SQ absorption is slower for a1 agonists
  • does not readily cross the BBB
  • rapid onset of action and inactivation –> EMERGENCY USE
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14
Q

What are some precautions and adverse effects for catecholamines?

A
  • potent drugs with narrow say margin (if your off by 0.1 your patient may die)
  • very short half life (within minutes)
  • predispose myocardium to tachycardia and tachyarrhythmias
  • altered perfusion leads blood flow to “flight tissue” and vasoconstriction to other vital organs like the kidneys
  • extravasation of NE or Dopamine can cause tissue damage and sloughing
  • cerebral hemorrhage (not so much in vet med)
  • anxiety, restlessness, tremors
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15
Q

Which of the following will result in the least amount of vasodilation?

A. Epinephrine 
B. Norepinephrine 
C. Isoproterenol 
D. Dopamine 
E. Dobutamine
A

B. Norepinephrine

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16
Q

Which of the following causes D1 receptor mediated vasodilation at low doses?

A. Epinephrine 
B. Norepinephrine 
C. Isoproterenol 
D. Dopamine 
E. Dobutamine
A

D. Dopamine

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17
Q

Selective B-2 agonists are primarily used as bronchodilators in the treatment of lower respiratory diseases like asthma and COPD.

A. True
B. False

A

A. true

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18
Q

Which of the following is the drug of choice for treatment of bronchial asthma?

A. Norepinephrine
B. Isoproterenol
C. Albuterol
D. Zilpaterol

A

C. Albuterol

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19
Q

What are the mechanisms of action of epinephrine?

A
  • competitive agonist on all alpha and beta receptors (a1, a2, B1, B2)
  • B-1 –> cardiac contractility
  • B-2 –> bronchodilator and vasodilation at low doses
  • a-1 –> vasoconstriction (dose-dependent) and increase venous return to the heart during CPR
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20
Q

What are the routes of administration of epinephrine?

A
  • IV, IM, SQ, inhaled, IO

- NOT PO

21
Q

What is 1:1000 equivalent to in mg/mL?

A

1 mg/mL

22
Q

What are some indications and clinical effects of epinephrine?

A
  • systemic effects
    • cardiopulmonary arrest (CPA)
    • Anaphylaxis/anaphylactoid reactions
    • used as Vasopressor
    • used as positive inotrope (IV CRI)
  • local effects
    • used with local anesthetics to produce
      regional vasoconstriction (potentiate local
      anesthetic)
    • topically used to treat local hemorrhage like
      epistaxis
23
Q

What are some precautions and contraindications of epinephrine?

A
  • cause massive sympathetic output which increases myocardial workload, oxygen demand and oxygen consumption (MVO2) –> myocardial ischemia
  • cardiac arrest
24
Q

What is the mechanism of action of Norepinephrine?

A
  • competitive agonist mainly on a-1 (not active on B-2)

- it is a vasopressor

25
Q

What are some indications of Norepinephrine?

A
  • used where vasopressor support is needed like anesthesia

- used in the treatment of hypotension due to inadequate vascular tone (like in septic shock)

26
Q

What are some precautions of Norepinephrine?

A
  • cardiac arrhythmia/tachyarrhythmias –> to correct this you can discontinue and use another vasopressor
  • NEED TO USE ECG MONITORING AND ARTERIOLE PRESSURE MONITORING
  • caution with certain cardiac diseases
27
Q

What are some clinical effects of Norepinephrine?

A
  • vasoconstriction (a-1 agonist) and is the most important catecholamine vasopressor –> cardiac out put increases due to increase in systolic/diastolic arteriole pressure
  • less of an increase in MvO2 compared to epinephrine
  • no significant bronchodilation because of no B-2 activity
  • no vasodilatory effects counteracting a-1 vasoconstriction
  • stronger vasoconstriction than epinephrine
  • strong vasopressor action –> strong baroreceptor response –> decrease HR and contractility
28
Q

What are some contraindications for Norepinephrine?

A
  • contraindicated in hypertensive patients

- extravasation (if administered outside the vein) can cause tissue damage

29
Q

What are the mechanisms of action for Isoproterenol?

A
  • synthetic catecholamine
  • potent non-specific B-agonist (B1 and B2)
  • no a-adrenergic activity
30
Q

What are some precautions and contraindications of Isoproterenol?

A
  • side effects similar to dopamine and dobutamine like tachycardia, anxiety, tremors and arrhythmias
  • IV CRI must be titrated to effect
  • ECG MONITORING AND ARTERIOLE BLOOD PRESSURE MONITORING
31
Q

What are some indications and clinical effects of Isoproterenol?

A
  • cardiac stimulatory (positive inotropic effect and mild positive chronotropic effect)
  • increase coronary, skeletal, renal, and mesenteric blood flow
  • bronchodilation
  • given IV and paraenternally in people for treatment of asthma
  • not commonly used as other catecholamines
32
Q

What are the mechanisms of action of Dopamine?

A
  • it acts on dopamine receptors with dose dependent effects at alpha and beta receptors
  • its indirect effect is that it stimulates the release of norepinephrine
33
Q

What are the dose dependent factors of Dopamine?

A
  • low dose: dopamine agonist (D1 and D2 receptors) –> activates visceral dopamine receptors which dilates renal, messenteric, coronary and intracerebral vascular beds
  • medium-low dose:B-1 agonist –> positive inotrope
  • medium-high dose: B-1 agonist –> positive chronotrope and increase cardiac automacity
  • high dose –> a-1 agonist (vasoconstriction)
  • NO B-2 EFFECTS
34
Q

What are some indications and clinical effects of Dopamine?

A
  • vasopressor support
  • treatment of hypotension due to inadequate vascular tone
  • post-arrest vasopressor of choice
  • it is no longer advocated for the use in oliguric renal failure
35
Q

What are some precautions and contraindications of Dopamine?

A
  • IV has potential for necrosis if extravasation occurs
  • contraindicative in hypertensive patients
  • MONITOR ECG AND ARTERIAL BLOOD PRESSURE
  • tachycardia, tachyarrhythmia, fluctuations in blood pressure
36
Q

What are the mechanisms of actions of Dobutamine?

A
  • synthetic B-1 agonist
  • structurally similar to Dopamine
  • No dopamine receptor activity
  • minimal a-1 and B-2 agonism
37
Q

What are some indications and clinical effects of Dobutamine?

A
  • positive inotropic effect in patients that need it
  • moderate positive chronotropic effects
  • treatment of anesthesia associated hypotension where inotropic support is indicated to maintain cardiac output and tissue/organ perfusion
  • increase coronary, skeletal, renal and mesenteric blood flow
38
Q

What are some precautions and contraindications of Dobutamine?

A
  • side effects similar to other catecholamines like tachycardia and/or tachyarrhythmias
  • twitching and seizures
  • tachyphylaxis (acute tolerance)
  • contraindicated with left atrial rupture or in cases where myocardial integrity is a concern like heart disease/failure
39
Q

What are the mechanisms of action of Phenylephrine?

A
  • direct acting a-1 selective agonist (non-catecholamine)
  • vasopressor
  • potent and used more in anesthesia
  • no B-2 effects so vasoconstriction can be severe
40
Q

What are some routes of administration for Phenylephrine?

A
  • IV, ophthalmic drops, oral tablets and liquids (decongestant), intranasal spray (decongestant)
41
Q

What are some indications and clinical effects of Phenylephrine?

A
  • increase in peripheral vascular resistance through systemic vasoconstriction
  • may cause reflex bradycardia
  • treatment of hypotension in dogs and cats
  • systemic vasopressor effects immediately IV and lasts less than 20 minutes
  • local/topical use for vasoconstriction of hemorrhage such as epistaxis and ophthalmic use as a mydriatic agent and aids in treatment of open angle glaucoma
42
Q

What are some precautions and contraindications for Phenylephrine?

A
  • renal and GI vasoconstriction
  • chronic use can rebound nasal congestion
  • contraindicated with hypertension
43
Q

What is the mechanism of action of Ractopamine and Zilpaterol?

A

It is a non-selective agonist of B-1, B-2 and B-3 receptors

44
Q

What are some indications and main effects of Ractopamine and Zilpaterol?

A

it increases the rate of weight gain, feed efficiency and carcass leanness in food animals and can just be added to the food

45
Q

What are some random facts about Albuterol?

A
  • human approved for inhalers
  • Salmeterol and Fluticasone (steroid)
  • most selective B-2 agonist
46
Q

What are some random facts about Terbutaline?

A
  • human approved and in small animal in tablet or injectable form
47
Q

What are some random facts about Clenbuterol?

A
  • veterinary approved oral syrup in equines
  • contraindicated in food animals
  • least affinity to B-2 but more affinity to B-1 (affects heart)
48
Q

What are some precautions and contraindications for Albuterol, Terbutaline, and Clenbuterol?

A
  • cardiac stimulation causes tachycardia
  • vasodilation
  • uterine relaxation –> tocolytic agent and may cause fetal retention
  • contraindications in patients with cardiovascular disease
  • nervousness, sweating, muscle tremors, weakness, and vomiting
  • ARCI class 3 agent so may be prohibited by some equine associations like horse shows
  • receptor down-regulation can occur with chronic use

PHARMACOLOGY (6 decks)

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