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Pharmacology > Lectures: ANS 5-8 > Flashcards

Lectures: ANS 5-8 Flashcards

0
Q

selectivity of Alpha adrenergic R subclass

A

1. epinephrine

  1. norepinephrine
  2. (much less) isoproterenol
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1
Q

neurotransmission steps affected by adrenergic agonist drugs

A

Direct-acting: bind to the post-synaptic receptor
In-direct:
- induce release of NE into synapse
- limit re-uptake of NE from synapse

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2
Q

selectivity of beta adrenergic R subclass

A

1. isoproterenol

  1. epinephrine
  2. norepinephrine
    (2 & 3 are almost same affinity)
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3
Q

effects of alpha-1 adrenergic R activity

A
  1. increase BP (vasoconstriction @ skin, renal, splanchnic, lungs)
  2. decrease congestion
    (decrease mucus secretion in upper respiratory tract)
  3. mydriasis (pupillary radial/dilator mm contraction)
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4
Q

effects of alpha-2 adrenergic R activity

A 
decrease BP (via central sympathetic vasomotor center)
--> agonists = anti-hypertensives
* Also: 
some a2 Rs = on PRE-synaptic terminals --> inhibit NE release
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5
Q

effects of beta adrenergic R activity

A
  1. stimulate heart (esp. B1, –> CHF/MIs, shock, etc.)
  2. bronchodilate (relax lower resp. sm. muscle –> COPD/asthma)
  3. decrease uterine contractions (relax bladder and uterus walls)
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6
Q

INdirect acting adrenergic agonists

A
  1. amphetamine
  2. cocaine
  3. tyramine
    (trigger AP-indep. NE release OR block reuptake)
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7
Q

Direct-acting adrenergic agonists (11)

A
  1. albuterol 7. phenylephrine
  2. clonadine 8. methoxamine
  3. dobutamine 9. isoproterenol
  4. dopamine 10. salmeterol
  5. Epinephrine 11. tertbutaline
  6. norepinephrine
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8
Q

catecholamines (list)

A
  1. epinephrine
  2. norepinephrine
  3. dopamine
  4. dobutamine
  5. isoproterenol
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9
Q

non-catecholamines (list)

A
  1. albuterol 5. methoxamine
  2. clonadine 6. salmeterol
  3. ephedrine 7. tertbutaline
  4. phenylephedrine 8. amphetamine*
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10
Q

catecholamines (characteristics)

A
  • Duration of action: short
  • CNS absorption: poor
  • metabolized by COMT/MAO? Yes!
  • Route of administration: Not oral
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11
Q

non-catecholamine adrenergic agonist (characteristics)

A
  • Duration of action: Long
  • CNS absorption: HIGH
  • metabolized by COMT/MAO? not well
  • Route of administration: may be oral
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12
Q

Beta-2 specific adrenergic agonists

A

Beta-1: dobutamine
Beta-2: albuterol, salmeterol, tertbutaline

  • most other adrenergic agonists = mixed selectivity
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13
Q

alpha specific adrenergic agonists

A

alpha-1: methoxamine
alpha-2: clonidine

  • most other adrenergic agonists = mixed selectivity
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14
Q

shock (Sx &Tx)

A

cardiovascular syndrome w/ hypotension, altered mental state, and metabolic acidosis (Sx)

Treatment: increase tissue perfusion, treat cause
	 #1 Dopamine... 2. norepinephrine
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15
Q

neurotransmission steps affected by adrenergic antagonist drugs

A

Mostly only affects post-synaptic receptor binding

*but: Reserpine blocks uptake into vesicles

16
Q

general effects of alpha-1 adrenergic antagonists

A
  1. vasodilation –> decrease BP
  2. smooth muscle relaxation –> relax prostrate/bladder sphincter

==> useful for:
pheochromocytoma, Reynauld’s disease, HTN, BPH

17
Q

general effect of beta adrenergic antagonists

A
  1. decrease CO by block cardiac stimulation
    –> for reducing heart strain after MI,
    & reduce exercise-related angina
  2. decrease BP –> for HTN, hyperthyroidism
  3. decrease intraocular pressure –> for glaucoma
18
Q

Beta adrenergic R antagonists (list)

A
  1. acebutolol 5. nadolol
  2. atenolol 6. pindolol
  3. esmolol 7. propanolol
  4. metroprolol 8. timolol
    * 9. labetAlol (alpha & beta)
19
Q

alpha adrenergic R antagonists (list)

A

(all cause BIG decrease BP –> reflex increase CO)
a-1 selective: (2)
phentolamine, phenoxybenzamine (irrreversible!)
Non-selective: (3)
doxosin, prazosin, terazosin

20
Q

pheochromocytoma

A

a tumor of the adrenal medulla which secretes NE, Epi, and/or Dopamine.
–> increases risk of heart problems (MI, arrhythmias, CHF, stroke, pulmonary edema)
Sx: HTN, severe headache, profuse sweating
Treatment: phenoxybenzamine & phentolamine, or labetalol

21
Q

Reynauld’s disease

A

condition of reduced blood flow to hands spontaneously or after cold stimulus, causing ischemia/cyanosis/erythema.
–> risk of: finger wasting, necrosis/gangrene, ischemic ulcers
treatment:
prazosin/doxosin/terazosin, and phenoxybenzamine
(increase perfusion by BLOCK vasoconstriction)

22
Q

effects of giving phentolamine BEFORE Epi/NE

A

for NE: blocks increase in PVR –> limits NE effect to direct heart effects only (blocks BP change and assoc. reflex changes)

for Epi: –> DEcrease dBP and CO, and aungments reflex response –> increases HR and contractility

23
Q

Benign Prostatic Hypertrophy/hyperplasia (“BPH”)

A

enlarged prostate compresses bladder & makes difficult to urinate and empty bladder.
Sx: strong urge, frequent urination, weak passage of urine, burning on urination, distention
Treatment: doxazosin/terazosin (relax sm. muscle)

24
Q

relative duration of action of beta adrenergic antagonists

A

minutes (shortest): esmolol (only by IV)
hours: acebutolol, metoprolol, pindolol;
propanolol, timolol, atenolol, labetalol
day (longest): nadolol

25
Q

“ISA” (Intrinsic Sympathomimetic Action)

A

= a drug that acts as a partial agonist,
blocks the endogenous NE/Epi/Dopamine, but simultaneously (weakly) stimulates the target receptor.
ie: pindolol & acebutolol
(beta adrenergic antagonists)

26
Q

beta adrenergic R antagonists w/ local anesthetic f(x)

A

= direct block of voltage-gated Na+ channels,

  1. propanolol
  2. pindolol
  3. acebutolo
  4. metoprolol
  5. labetalol
27
Q

beta-1 R specific adrenergic antagonists

A
  • especially good for treating HTN/angina in special case patients
    (ie: asthma/COPD, diabetes) bc has much less effect on lungs and metabolism (B2 Rs).
    1. Acebutolol
    2. Atenolol
    3. Esmolol
    4. Metroprolol

Pharmacology (8 decks)

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