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
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
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
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
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
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
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
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
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
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
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
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
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)
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
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
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