Adrenergic Flashcards

1
Q

Sympathomimetic

A

Catecholamines and adrenergic agonists

  • excitatory action on smooth muscle and glands (blood vessels/ salivary glands)
  • inhibitory action that increases HR and contraction
  • increase glycogenolysis and lipolysis
  • modulate secretion of insulin (decrease) and renin (increase)
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2
Q

Sympatholytic

A

Adrenergic antagonists

- most are competitive antagonists (except phenoxybenzamine)

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3
Q

Catecholamine

A

Norepinephrine
Epinephrine
Isoproternol
Dopamine

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4
Q

Norepinephrine

  • Selectivity
  • Effects
  • Uses
A
sympathetic NT
Selectivity: a1, a2, b1
Effects:
-  vasoconstriction (increase PVR)
- Increase BP
- Can cause reflex bradycardia

Uses:

  • vasoconstrictor in shock
  • elevate blood pressure during reduced sympathetic tone ( anesthesia)
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5
Q

Isoproteronol

A
Synthetic, direct catecholamine
Receptor: Beta 1, Beta 2
Effects:
- decrease PVR
- increase HR
- decrease BP
-bronchodilation

Uses: stimulate HR during bradycardia or heart block

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6
Q

Dopamine

A

Sympathetic NT
Selectivity: DA1, B1, A1
Effects
- Low dose: (DA1): vasodilation of renal and mesentaric arteries
-Medium: (B1): Increase HR, CO, contractility
-High (A1): vasoconstriction, increase PVR

Uses: severe decompensated Heart failure, shock

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7
Q

Dobutamine

A

Synthethetic catecholamine
- racemic but overall effect is B1 agonist

Effects:
- Increase HR, Contractility, CO

Uses: short term cardiac decompensation, cardiac stress testing

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8
Q

Methyldopa

A

-orally active pro-drug
- metabolized in nerve terminals to alpha-methyldopamine and alpha-norepeinephrine
Alpha 2 receptor agonists

Effects
- decrease PVR, HR and CO

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9
Q

Phenylephrine

A

Non-catecholamines
Receptors: alpha 1 adrenergic receptors

Effect:

  • increase systolic and diastolic BP
  • decrease HR
  • decrease blood flow

Uses

  • ophthalmic: mydriatic, decrease hemorrhage, conjuctival decongestion
  • nasal decongestion:
  • treatment of hypotension (IV administration)
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10
Q

Clonidine

A
  • non-catecholamine, direct
  • orally active alpha selective agonist
  • stimulates alpha 2 to reduce sympathetic flow
  • uses: anti-HTN
  • causes prolonged BP lowering
  • Decreases PVR, decrease HR, CO

Adverse effects, dry mouth and sedation, edema and rebound hypertension

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11
Q

Albuterol

A

Non-catecholamine, direct
beta 2 receptors agonist
short acting
Uses: bronchodilation (asthma)

Adverse effects: tremor, anxiety, tachycardia

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12
Q

Salmeterol

A

Non-catecholamine, direct
Beta 2 agonist

-inhalation (long duration of action)
Used: COPD, asthma (noucturnal/persistant)
Slow onset of action so not suitable as monotherapy for acute bronchospasm

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13
Q

Tyramine

A

Indirect direct acting agonist

  • releases NE
  • found in high levels of fermented foods (wine, cheese)
  • normally metabolized by MAO
  • in pts taking MAOi–> increase in tyramine levels–> cause hypertensive crisis
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14
Q

Amphetamine

A
CNS stimulant
- effective orally
-release NE and weak alpha/beta agonist
-depresses appetite
Uses: Narcolepsy, ADD
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15
Q

Ephedrine

A

Direct agonist (a & b) and releases NE

  • effective orally
  • CNS stimulation
  • found in some herbal preparations
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16
Q

Pseudoephedrine

A

-direct a1 agonist (with some beta 2 activity)
- orally effective but less CNS stimulation
Use: nasal decongestant (a1 agonist)

precursor to methamphetamine

17
Q

Guanadrel

A

Adrenergic antagonist
Neuron blocker: disrupt, synthesis, storage, release of NE
- inhibit NE release
- orally active
- long acting
- Taken into adrenergic nerves by NET (inhibited by tricyclics that inhibit NET)

Side effect: orthostatic HTN, sexual dysfunction, muscle weakness, edema

18
Q

Guanethidine

A

Adrenergic antagonist
Neuron blocker: disrupt, synthesis, storage, release of NE
- inhibit NE release
- orally active
- long acting
- Taken into adrenergic nerves by NET (inhibited by tricyclics that inhibit NET)
- polar: does not enter CNS

Side effect: orthostatic HTN, sexual dysfunction, muscle weakness, edema

19
Q

Reserpine

A
Adrenergic antagonist that diffuses into nerves
 does not require NET
- inhibits VMAT2--> depletes NE stores
- enters CNS
-long acting/slow onset

Side effect: sedation, orthostatic HTN, increased gastric acid secretion

20
Q

Phenoxybenzamine

A

alpha adrenergic receptor blockers
Block alpha 1 & 2
- irreversible antagonist
- orally active
-long duration of action (persist for days) requires new receptor synthesis
- produces vasodilation proportional to degree form sympathetic tone

21
Q

Phentolamine

A

alpha adrenergic receptor antagonist

  • orally active, shorter duration of action
  • competitive reversible antagonist
  • block can be overcome by increasing levels of agonists

Uses:

  • HTN
  • Pheochromocytoma
  • reverse soft tissue anesthesia produced by anesthetic

Side effects

  • tachycardia and salt/water retention (edema)
  • Orthostatic hypotension
22
Q

Prazosin

A
  • Selective
  • orally active
  • competitive blocker of alpha 1 receptors

Effects

  • decreases vascular tone in resistance and capacitance ( arteries and veins)
  • produces favorable lipid profile

Uses

  • HTN
  • short term congestive heart failure
  • BHP: relaxes alpha1 mediated contraction of prostate ( which resists urine flow)

Side effects

  • first-dose phenomenon: hypotension and syncope
  • edema
23
Q

Tamsulosin

A
  • alpha 1 receptor antagonist
  • orally active
  • effective for BPD with little effect on BP
24
Q

Propranolol

A

Beta receptor antagonist
- both Beta 1 and 2

Uses
- HTN, Angina, pheochromocytoma, acute MI, migraine prophylaxis

Side effects
- cardiac depression, may increase airway resistance, symptoms of hypoglycemia, sedation, impotence

Use with caution: asthma, congestive heart failure, bradyarrhythmia, AV block, diabetes, hypotension

25
Q

Timolol

A

non-selective beta receptor antagonist
Uses
-treats wide angle glaucoma
- does not affect pupil size or accommodation

use with caution in pt with cardiac disease

26
Q

Metoprolol

A

Beta selective receptor antagonist (2nd)

  • competitive, reversible
  • low doses more selective

Uses

  • similar to propranolol (- HTN, Angina, pheochromocytoma, acute MI, migraine prophylaxis)
  • used to treat heart failure

Side effects:
- cardiac depression, may increase airway resistance (less than propranolol), symptoms of hypoglycemia, sedation, impotence

27
Q

Atenolol

A

Beta receptor antagonist

  • orally active
  • does not penetrate into CNS

Use
- HTN, Angina, pheochromocytoma, acute MI, migraine prophylaxis

28
Q

Labetalol

A

Beta receptor antagonist with CV effect (3rd)

  • competitive antagonist of alpha1 and non selective beta receptors

Use:
HTN (oral)
hypertensive emergency (IV)

29
Q

Carvedilol

A
Beta receptor antagonist with CV effect (3rd)
- competitive antagonist of alpha1 and non selective beta receptors
- anti-inflammatory
- blocks L-type ca at higher doses
Use:
-treat heart failure
- HTN
- Acute MI
30
Q

Epinephrine

  • Selectivity
  • Effects
  • Uses
A

Synthesized in adrenal medulla
Selectivity: a1,a2,b1,b2

Effects:
+ increase HR, contractility, CO
+ increase systolic BP, decrease diastolic BP
+ vasoconstriction, but dilation of skeletal m (dose-dependent); net decrease in PVR
+Bronchodilation
+hyperglycemia
+lipolysis

Uses
+ rapid relief of hypersensitivity to drugs (EPI-pen)
+bradyarrhythmia: restore rhythm in patients in cardiac arrest
+ophthalmic uses: mydriatic, decrease hemorrhage, conjunctival decongestion

31
Q

Side effects of adrenergic agonist

A
Throbbing headache (alpha agonist)
Cerebral hemorrhage: due to increase in systemic BP (alpha)
Increase HR: beta agonist
Angina from increase HR: beta
Cardiac arrhythmia: beta
Restlessness and anxiety