Rab Drugs Flashcards

1
Q

Epinephrine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • Agonist
  • A1: High
  • A2: High
  • B1: High
  • B2: High
  • B3: Moderate
  • Selectivity: No Selectivity
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2
Q

Norepinephrine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • A1: High
  • A2: High
  • B1: High
  • B2: Low
  • B3: Moderate
  • Selectivity: No Selectivity, Low binding to B2
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3
Q

Oxymetazoline

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • A1 adrenergic Agonist
  • A1: High
  • A2: High
  • B1: High
  • B2: Low
  • B3: Moderate
  • Selectivity: No Selectivity, full a1 partial a2a
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4
Q

Phenylephrine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a1-adrenergic Agonist
  • A1: High
  • A2: Moderate
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Non Selective yet favoring a1
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5
Q

Midodrine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a1-adrenergic Agonist
  • A1: High
  • A2: Low
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Selective for a1
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6
Q

Clonidine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a2-adrenergic Agonist
  • A1: Moderate
  • A2: High
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Non Selective, yet favoring a2
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7
Q

Apraclonidine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a2-adrenergic Agonist
  • A1: Moderate
  • A2: High
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Non Selective, yet favoring a2
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8
Q

Brimonidine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a2-adrenergic Agonist
  • A1: Moderate
  • A2: High
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Non Selective, yet favoring a2
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9
Q

Methyldopa

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a2-adrenergic Agonist
  • A1: Moderate
  • A2: High
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Non selective yet favoring a2
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10
Q

Guanfacine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a2-adrenergic Agonist
  • A1: Low
  • A2: High
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Selective for a2A
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11
Q

Guanabenz

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a2-adrenergic Agonist
  • A1: Low
  • A2: High
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Selective for a2
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12
Q

Isoproterenol

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • Non selective B Agonist Favoring B1
  • A1: Low
  • A2: Low
  • B1: High
  • B2: High
  • B3: High
  • Selectivity: Non-Selective for B
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13
Q

Dopabutamine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • Non selective B Agonist Favoring B1 Agonist
  • A1: Moderate
  • A2: Very Low
  • B1: High
  • B2: Moderate
  • B3: Very Low
  • Selectivity: Selective for B1
  • Increases cardiac output with little vasoconstriction vs NEPI
  • Risk of ischemia arryhytmia much lower then isoproterenol (why iso not used)
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14
Q

Albuterol (salbutamol)

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B2-adrenergic Agonist
  • A1: Very Low
  • A2: Very Low
  • B1: Moderate
  • B2: High
  • B3: Very Low
  • Selectivity: Short acting, Selective for B2
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15
Q

Tertbutaline

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B2-adrenergic Agonist
  • A1: Very Low
  • A2: Very Low
  • B1: Moderate
  • B2: High
  • B3: Very Low
  • Selectivity: Short acting, Selective for B2
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16
Q

Salmeterol

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B2-adrenergic Agonist
  • A1: Very Low
  • A2: Very Low
  • B1: Moderate
  • B2: High
  • B3: Very Low
  • Selectivity: Long Acting, Selective for B2
17
Q

Formoterol

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B2-adrenergic Agonist
  • A1: Very Low
  • A2: Very Low
  • B1: Moderate
  • B2: High
  • B3: Low
  • Selectivity: Long acting, Selective for B2
18
Q

Indacaterol

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B2-adrenergic Agonist
  • A1: Very Low
  • A2: Very Low
  • B1: Moderate
  • B2: High (full)
  • B3: Very Low
  • Selectivity: Ultra long acting, Selective for B2
19
Q

Olodaterol

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B2-adrenergic Agonist
  • A1: Very Low
  • A2: Very Low
  • B1: Moderate
  • B2: High
  • B3: Very Low
  • Selectivity: Ultra long acting, Selective for B2
20
Q

Vilanterol

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B2-adrenergic Agonist
  • A1: Very Low
  • A2: Very Low
  • B1: Moderate
  • B2: High (full)
  • B3: Very Low
  • Selectivity: Ultra long acting, Selective for B2
21
Q

Mirabrigon

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • B3-adrenergic Agonist
  • A1: Very low
  • A2: Very low
  • B1: low
  • B2: low
  • B3: High
  • Selectivity: Selective for B3
  • Bladder relaxation, b3 not expressed many other places
  • Binds some to b1 still so some pounding heart maybe
22
Q

Phenoxybenzamine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • Non selective a adrenergic Antagonist
  • A1: High
  • A2: Moderate
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Irreversible a antagonist
  • Depress baroreflex (a1)
23
Q

Phentolamine

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • Non selective a adrenergic Antagonist
  • A1: High
  • A2: High
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Non selective a antagonist
  • Depress baroreflex (a1)
  • Prevention of necrosis in case of accidental tissue injection of sympathomimetic
24
Q

Prazosin

  • Agonist or Antagonist
  • A1:
  • A2:
  • B1:
  • B2:
  • B3:
  • Selectivity:
A
  • a1-adrenergic Antagonist
  • A1: High
  • A2: Low
  • B1: Very Low
  • B2: Very Low
  • B3: Very Low
  • Selectivity: Selective for a1
  • Must be taken several times a day
  • Reduce Glucose lipid (LDL-CHOL,TG) levels
  • Dizziness and syncope w/first dose
  • nasal stuffiness, hypo, tachy
  • Depress baroreflex (a1)
25
Doxasoin * Agonist or Antagonist * A1: * A2: * B1: * B2: * B3: * Selectivity:
* a1-adrenergic Antagonist * A1: High * A2: Low * B1: Very Low * B2: Very Low * B3: Very Low * Selectivity: Selective for a1 * Once daily * Reduce Glucose lipid (LDL-CHOL,TG) levels * Dizziness and syncope w/first dose * nasal stuffiness, hypo, tachy * Depress baroreflex (a1)
26
Terazosin * Agonist or Antagonist * A1: * A2: * B1: * B2: * B3: * Selectivity:
* a1-adrenergic Antagonist * A1: High * A2: Low * B1: Very Low * B2: Very Low * B3: Very Low * Selectivity: Selective for a1 * Once daily * Reduce Glucose lipid (LDL-CHOL,TG) levels * Dizziness and syncope w/first dose * nasal stuffiness, hypo, tachy * Depress baroreflex (a1)
27
Alfuzosin * Agonist or Antagonist * A1: * A2: * B1: * B2: * B3: * Selectivity:
* a1-adrenergic Antagonist * A1: High * A2: Low * B1: Very Low * B2: Very Low * B3: Very Low * Selectivity: Selective for a1 * SELECTIVE FOR PROSTATE * INDUCES APOPTOSIS OF PROSTATE SMOOTH MUSCLE * Lessened first does effect from proz tera doxa still must be taken multiple times a day *
28
Tamsulosin * Agonist or Antagonist * A1: * A2: * B1: * B2: * B3: * Selectivity:
* a1-adrenergic Antagonist * A1: High (a1A) Moderate (a1D) Low (a1B) * A2: Low * B1: Very Low * B2: Very Low * B3: Very Low * Selectivity: Selective for a1A * INEXPENSIVE AND SELECTIVE FOR PROSTATE * Lessened first does effect from proz tera doxa still must be taken multiple times a day
29
Silodosin * Agonist or Antagonist * A1: * A2: * B1: * B2: * B3: * Selectivity:
* a1-adrenergic Antagonist * A1: High (a1A) low (a1B and a1D) * A2: Low * B1: Very Low * B2: Very Low * B3: Very Low * Selectivity: Selective for A1a * SELECTIVE FOR PROSTATE * Reduce glucose Lipid (LDL-CHOL, TG) levels * Lessened first does effect from proz tera doxa still must be taken multiple times a day
30
Propanolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: High * B3: Low * **Selectivity: Selective for B1 B2** * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: No * a1 antagonist: No * Na Channel Blocker: Yes * NO Production: No * Ca Channel Blocker: No * Lipid solubility: High * Used for situational anxiety (B1) * Approved for infantile hemangiomas * May potentiate and maske signs of hypoglycemia in diabetics * Prevent effect of epi in anaphylaxis
31
Pindolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: High * **B3: Moderate\*** * Selectivity: Selective for B1 B2 * Partial B1 agonist: Moderate * Partial B2 agonist: No * Partial B3 agonist: Low * a1 antagonist: No * Na Channel Blocker: Yes * NO Production: Yes * Ca Channel Blocker: No * Lipid solubility: Moderate
32
Timolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: High * B3: Low * Selectivity: Selective for B1 B2 * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: No * a1 antagonist: No * Na Channel Blocker: No * NO Production: No * Ca Channel Blocker: No * Lipid solubility: Moderate * **Used for intraocular hypertension and glaucoma** * Less prone to side effects then propanolol
33
Metoprolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: Moderate * B3: Very Low * Selectivity: Selective for B1 * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: No * a1 antagonist: No * Na Channel Blocker: Yes low * NO Production: No * Ca Channel Blocker: No * Lipid solubility: moderate * Hemodynamically stable acute MI * Reduces mortality/hospitalization in patients with heart failure and those already receiving ace inhibitors, diuretics, and or digoxin * B1 reduce renin release * Crosses BBB
34
Atenolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: Moderate * B3: Very Low * Selectivity: Selective for B1 * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: No * a1 antagonist: No * Na Channel Blocker: No * NO Production: No * Ca Channel Blocker: No * Lipid solubility: low
35
Bisoprolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: Moderate * B3: Very Low * Selectivity: Selective for B1 * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: No * a1 antagonist: No * Na Channel Blocker: No * NO Production: No * Ca Channel Blocker: No * Lipid solubility: low
36
Esmolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: Moderate * B3: Very Low * Selectivity: Selective for B1 * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: No * a1 antagonist: No * Na Channel Blocker: No * NO Production: No * Ca Channel Blocker: No * Lipid solubility: low * Afib/flutter and intraoperative and supraventricular tachycardia * No side effects that will last (hypotension less than 10%)
37
Nebivolol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Very Low * A2: Very Low * B1: High * B2: low * B3: Moderate\* * Selectivity: Selective for B1 * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: Moderate * a1 antagonist: No * Na Channel Blocker: No * NO Production: Yes * Ca Channel Blocker: No * Lipid solubility: low * Alternative/adjunctive treatment of hypertension * ANTIOXIDANT NADPH oxidase inhibitor * Partial b3 agonist also activates nitric oxide synthase for vasodilation * NO release advantage in elderly
38
Labetalol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Moderate * A2: Very Low * B1: High * B2: High\* * B3: Moderate\* * Selectivity: Weaker selectivity but favors B1, B2 * Partial B1 agonist: No * Partial B2 agonist: low * Partial B3 agonist: low * a1 antagonist: Yes * Na Channel Blocker: Yes * NO Production: Yes * Ca Channel Blocker: No * Lipid solubility: low * Negligible amount across BBB
39
Carvedilol * A1: * A2: * B1: * B2: * B3: * Selectivity: * Partial B1 agonist: * Partial B2 agonist: * Partial B3 agonist: * a1 antagonist: * Na Channel Blocker: * NO Production: * Ca Channel Blocker: * Lipid solubility:
* A1: Moderate * A2: Very Low * B1: High * B2: High * B3: Moderate * Selectivity: Weaker selectivity but favors B1, B2 * Partial B1 agonist: No * Partial B2 agonist: No * Partial B3 agonist: No * a1 antagonist: yes * Na Channel Blocker: yes * NO Production: No * Ca Channel Blocker: yes * Lipid solubility: moderate