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Autonomic System Pharmacology > Sympathomimetic Drugs/ Adrenoceptor Agonist > Flashcards

Sympathomimetic Drugs/ Adrenoceptor Agonist Flashcards

1
Q

Receptors present in somatic motor neuron terminals

A

Beta 2 adrenergic

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2
Q

Which receptors binds only to epinephrine

A

Beta 2 adrenergic receptor

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3
Q

Beta 1 location and function

A

Fat cells

Lipolysis

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4
Q

D1 location and function

A

Splanchnic and renal blood vessel

Relaxation of vacuolar smooth muscle->Dilation - Dec peripheral vascular resistance

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5
Q

D2 receptor

A

On presynaptic nerve terminals

F: inhibits NE, inhibit adenylyl cyclase, open K channels and influx of Ca

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6
Q

Beta 3 receptor

A

Lower affinity

Beta 3 resistance to desensitization> beta 1 and 2

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7
Q

Epi has increase activity at which receptors

A

Beta 2

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8
Q

NE is potent at which receptors

A

Alpha 1 and beta 3

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9
Q

Clinical use of phenylephrine and metoxamine

A
  • vasoconstrictor
  • tx hypotension
  • nasal decongestant
  • mydrasis
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10
Q

Alpha 1 agonist

A

Phenylephrine, Metoxamine ( not cathecol derived- not affected by COMPT)
Milodrine (activated- desglymilodrine)
Xylometazoline
Oxymetazoline( high doses cause hypotension due to clonidiine like effect)

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11
Q

Alpha 2 action

A
  • on presynaptic terminal - -ve feedback for NE
  • ## Hypotension
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12
Q

Effect of clonidiine

A

Acts on alpha 2 receptor in brainstem

Hypotension and bradycardia

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13
Q

Action of methyldopa

A
  • antihypertensive

- high doses stimulate postsynaptic vascular alpha 2 receptor-> vasoconstriction and increase BP

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14
Q

Alpha 2 agonist drugs

A 
Clonidine
Guanabenz
Guanfacine
Methyldopa
Moxonidine
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15
Q

If alpha 2 drugs withdrawn to quickly

A

Cause withdrawal symptom’s, and rebound hypertension

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16
Q

Tx of orthostatic hypertension

A

Midodrine

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17
Q

Side effects of alpha 2 drugs

A
  • sedation
  • dry mouth
  • sleep disturbance
  • sexual dysfunctions in males
  • nausea
  • dizziness
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18
Q

Drugs that act on Beta 1 and 2 receptors

A

Isoproterenol

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19
Q

Beta 1 selective drug

A

Dobutamin

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20
Q

Beta 2 selective drugs

A

Albuterol
Terbutaline
Ritodrine
Metaproterenol

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21
Q

Clinical use it epinephrine

A
  • tx for anaphylaxis

- use along with anesthetic -> cause vasoconstriction -> Dec absorption-> prolonging anesthetic

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22
Q

Mixed alpha and beta agonist

A
  • norepinephrine (tx septic shock)
  • epinephrine
  • phenylpropanolol
  • ephedrine
  • pseudoephedrine
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23
Q

Phenylpropanolamine

A 
Mixed adrenergic agonist
Vasoconstriction
Shrink mucosal surface
Otc apatite suppressant
Associated with hemorrhagic stroke
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24
Q

Phenylpropanolamine

A 
Mixed adrenergic agonist
Vasoconstriction
Shrink mucosal surface
Otc apatite suppressant
Associated with hemorrhagic stroke
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25
Q

Pseudoephedrine

A

Mixed adrenergic agonist

Decongestant

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26
Q

Use of ephedrine

A
  • asthma therapy
  • increase skeletal muscle tone-> M. Gravis
  • tx narcolepsy
  • nasal decongestant
  • promote weight loss
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27
Q

Amphetamine like drugs

A
  • amphetamine
  • modafinil
  • methylphenidate
  • phenmetrazine
  • tyramine
  • methamphetamine
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28
Q

Amphetamine roles

A
  • CNS stimulant

- appetite suppressant

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29
Q

Tx ADHD

A

amphetamine like drug: METHYLPHENIDATE

30
Q

Function of modafinil

A
  • inhibit NET and DAT-> increase synaptic NE, dopamine, serotonin, and glutamate
  • decrease GABA
31
Q

Indirect sympathomimetic drug used for Tx of narcolepsy

A

MODAFINIL

32
Q

Tyramine present in what foods

A 
Cheddar cheese
Maramite
Wine
Country ham
Fava beans
33
Q

Patients treated with Mao inhibitors should avoid tyramine containing foods why

A

(Mao metabolises tyramine)

Mao inhibitors -> increased effects of tyramine-> hypertension

34
Q

Catecholamine reuptake inhibitors ( Indirect sympathomimetic)

A 
TCA -imipramine
Atomoxitine, reboxitine
Sibutramine
Duloxitine
Cocaine
35
Q

Is an NE and serotonin reuptake inhibitors cause side effects of orthostatic tachycardia and used to treat urinary incontinence

A

TCA- imipramine

36
Q

NET inhibitor used to treat ADHD

A

Atomoxitine

37
Q

Drugs used to treat ADHD

A
  1. Methylphenidate (amphetamine like)

2. Atomoxitine (NET inhibitor)

38
Q

Serotonin and NE reuptake inhibitor used to as appetite suppressant in obesity

A

Sibutramine

39
Q

Function and use of duloxitine

A
  1. NE and serotonin reuptake inhibitor
  2. antidepressants
  3. Treat fibromyalgia ( musculoskeletal pain)
40
Q

Cocaine effects

A 
Sympathomimetic inhibiting reuptake of NE and especially dopamine in the CNS
Effects: - increase vasoconstriction
- hypertension
- angina pectoris
- mucosal rupture
41
Q

Central anti-adrenergic

A 
They are alpha 2 agonist of CNS:
Clonidine
Guanabenz 
Guanfacine
Methyldopa ( alpha methylnorepinephine)
42
Q

Function of central anti adrenergic

A

Dec sympathetic outflow from CNS
cause orthostatic Hypotension
Clonidine- can also cause rebound HPT, sedation

43
Q

Peripheral presynaptic adrenergic

A

Dec NE->Dec bp, orthostatic Hypotension, increase GI motility, Dec urinary retention, bradycardia
Guanethidine - increase infusion-> Dec NE
Guanadrel- same
Bretylium-same and used as antiarrhythmics
Reserpine- block VMAT

44
Q

Postsynaptic alpha antagonist

A 
Phentolamine
Phenoxybenzamine
Prazosin
Doxaosin
Terazosin
Tamsulosin
45
Q

Phentolamine function and use

A 
Antagonist of alpha 1 and alpha 2
- Dec PVR
- hypotension
- antagonises effect of serotonin
- reflex cardiac stimulation ( angina pectoris, arrhythmia)
Uses:. 1.Tx pheochromocytoma
2. Tx cocaine toxicity
3. Tyramine toxicity in patients tx w/ MAO inhibitor
46
Q

Side effects of chronic use of phentolamine

A

Abdominal cramping
Ulceration
Diarrhea

47
Q

Phenoxybenzamine action and function

A

Is no reversible Acts on both alpha 1and 2 receptors present on postsynaptic and presynaptic terminal

  • cause dec in vasoconstriction
  • orthostatic Hypotension
  • tx for pheochromocytoma
48
Q

Prazosin action, uses, side effects

A

Antagonist Acts on alpha 1 receptors

  • orthostatic Hypotension
  • reflex tachycardia

Use:1. tx for PTSD

  1. Tx hypertension
  2. Tx CHF

effects: 1.can cause Prazosin Syncope
2. Chronic use reduce efficacy

49
Q

Terazosin and doxazosin use

A

Alpha 1 Antagonist used to tx BPH

50
Q

Tamsulosin features and use

A

Alpha 1 Antagonist with high BA and t1/2 9-15hrs

Inhibit contraction of prostate-> tx BPH

51
Q

Alpha 2 antagonist

A

Yohimbine

Mert something check sketchy

52
Q

Action of yohimbine and use

A

Alpha 2 antagonist, blocks alpha 2 receptors in medulla in CNS and presynaptic terminal in the periphery -> increase NE release

  1. Increases BP
  2. aphrodisiac- tx ED
53
Q

Quinazoline derivative and use

A

Prazosin (piperazinyl quinazoline)
Silodosin
Alfuzosin
Indoramin

Tx: BPH
And increase risk of prolonged QT

54
Q

Labetalol

A

Alpha 1 and beta antagonist

55
Q

Chlorpromazine and haloparidol

A

Act at dopamine receptor and alpha receptor antagonist

56
Q

Ergot derivatives: ergotamine and dehydroegrotamine

A

Reversible alpha receptor blockage-> partial agonist effect

57
Q

Pharmacokinetics of beta antagonist drugs

A
  1. Increase absorption by oral route
  2. Low BA
  3. Rapid distribution-> large Vd
58
Q

Actionof beta blockers

A
  1. Dec heart rate and contractility and BP
  2. Increase resp tone
  3. Anti arrhythmic
  4. Tx angina pectoris (Dec heart O2 demand), cardiac obstructive hypertrophy,
  5. Tx thyrotoxicosis, anxiety, migraine
  6. Local anesthetic
  7. Antihypertensive (Dec renin)
  8. Aortic dissection
  9. Long term use-> Dec mortality in MI, myocardial arrhythmias
  10. Dec lipolysis, gluconeogenesis-> hypoglycemia ( tx with glucagon)
59
Q

Side effect of beta blocker

A
  1. Worsen heart failure
  2. Dec AV conduction
  3. Respiratory obstruction in patients w/lung disease
  4. Vivid dreams, nightmares, fatigue, and cold extremities
60
Q

Metaprolol

A

Beta 1 selective antagonist

  • tx acute MI, cardiac congestion
  • less effect on asthmatic patients
61
Q

Atenolol

A

Beta 1 selective antagonist

  • do not pass BBB
  • manage hypertension
62
Q

Timolol

A

Non selective beta blocker

  • tx glaucoma ( Dec production of aqueous humor)
  • topical effect
63
Q

Pindolol

A

Beta antagonist and partial agonist

64
Q

Nevibolol

A

Highly selective beta 1

- increase vasodilation -> effect endothelium to produce increase NO

65
Q

Nadolol

A

Non selective beta blocker
Longer duration of action
Tx glaucoma

66
Q

Mixed alpha1 and beta antagonist

A

Labetalol

Carvedolol

67
Q

Dopamine receptor action and gprotein

A

D1 is Gs- vasodilation

D2 is Gi- emesis, inhibition of prolactin

68
Q

Dopamine agonist

A

Fenoldopam- tx hypertension, heart failure, and MI, diuretic.

69
Q

Tx for Parkinson’s disease

A

D2 agonist:
Levadopa
Apmorphine
Bromocriptine

70
Q

Metoclorprimidine and domperidone

A

D2 antagonist

  • increase peristalsis
  • increase gastric emptying
  • constrict sphincter -tx GERD
  • block D2 receptor in CTZ of medulla- antinuasea and antiemetic action
71
Q

Tx orthostatic hypotension

A
  1. Milodrine (alpha 1 agonist)

2. Yohimbine (alpha 2 antagonist)

Autonomic System Pharmacology (4 decks)

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