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Pharmacology > Drugs Acting on the SNS > Flashcards

Drugs Acting on the SNS Flashcards

0
Q

Occurrence and Function of Catecholamines: NE

A

Principal neurotransmitter
Synthesized in post-ganglionic neurons of SNS and released in adrenergic synapses
Function
- Maintenance of normal sympathetic tone
- Adjust circulatory dynamics

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1
Q

Sympathomimetic Drugs: Catecholamines: Absorption and duration

A

Not well absorbed orally, doesn’t cross BBB

Brief duration

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2
Q

Occurrence and Function of Catecholamines: EPI and DA

A

Stored in chromaffin granules in the adrenal medulla are released following SNS stimulation
- 75% of catecholamines released in humans is EPI
EPI
- Emergency hormone that stimulates metabolism and promotes blood flow to skeletal muscles

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3
Q

Principal catecholamines in the CNS

A

DA and NE

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4
Q

What does metyrosine inhibit

A

Tyrosine hydroxylase resulting in an inability to create DOPA

  • Used in treatment of pheochromocytoma
    • Tumors synthesize huge amounts of catecholamines
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5
Q

What converts DA to NE

A

dopamine-beta-hydroxylase

DA actively transported into vesicles for conversion

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6
Q

What blocks the transport of DA and NE

A

Reserpine depletion of transmitter stores

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7
Q

What blocks the exocytic release of NE

A

Guanethidine and bretylium

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8
Q

What is the action of cocaine and tricyclic antidepressants

A

Block active NE reuptake

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9
Q

How do you diagnose pheochromocytoma?

A

High levels of VMA and metanephrines in the urine

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10
Q

Alpha receptor function

A

Vasoconstriction, mydriasis, contraction of sphincters of gastrointestinal and genitourinary tracts, piloerection, ejaculation

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11
Q

Beta receptor functions

A

Vasodilation(only to skeletal muscles), bronchial relaxation, intestinal and genitourinary wall relaxation, cardiac stimulation, renin release, glycogenolysis, gluconeogenesis, lipolysis

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12
Q

Beta 1 function

A

Cardiac stimulation

Renin release

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13
Q

Beta 2

A

Vasodilation

Bronchodilation

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14
Q

NE receptors

A

Alpha-1
Beta-1
Alpha-2 agonist

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15
Q

EPI receptors

A

Alpha-1, alpha-2, beta-1, beta-2

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16
Q

Isoproterenol

A

Beta-1, Beta-2 stimulation

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17
Q

Consequence of direct cardiovascular actions

A

Compensatory reflex adjustments occur representing indirect drug actions

18
Q

Increase BP triggers what response?

A

Baroreceptor discharge which inhibits SNS and activates vagal (PNS) nerve activity
Results in reflex bradycardia

19
Q

Effects on Metabolism

A

Glycogenolysis stimulated by EPI, iso, and a little by NE
- Glucose released from liver and lactic acid released from muscle
- Mediated by beta receptors
Promote lipolysis
- Increase release of free fatty acids and glycerol from TG
- Activate TG lipase
- Mediated through beta receptor activation
Increase in metabolism

20
Q

Effects on Endocrine

A

Renin secretion stimulation (beta-1)

Insulin secretion stimulation (beta receptors) inhibited by (alpha-2)

21
Q

Effect on CNS

A 
No effect (sympathomimetics don't cross BBB)
Indirect effect from BP response
22
Q

Epinephrine: Use

A 
Oxidation is possible converting from a clear solution to a brownish solution resulting in a decrease in potency
Allergic reaction
   - Antagonist of anaphylactic response
COPD and asthma
   - Beta-2 effect to produce bronchodilation
Local vasoconstriction
Eye
   - Mydriasis
   - Reduces IOP
Cardiac arrest (beta-1 agonist effect)
   - Could be dangerous due to cardiac necrosis due to alpha effect of vasoconstriction
   - Direct trauma
   - Arrhythmia
23
Q

EPI: Adverse effects

A

Increase CO without improving efficiency (arrhythmias, angina, etc.)
Extavasation can result in injection site reaction leading to necrosis
- Based off alpha vasoconstriction
- Treated via an alpha antagonist
CNS
- Fear, anxiety, tenseness, restlessness, throbbing headache, tremor, dizziness
Hyperglycemia

24
Q

NE (alpha1 and 2, beta 1): Use (injection)

A

Acute hypotensive emergencies (alpha-1 vasoconstriction)
Dependent on the type of hypotension
- If you have hypovolemic shock do not use
- Shock
- Decrease in perfusion

25
Q

NE: Adverse effects

A

Overstimulation of the heart (beta-1)

26
Q

Isoproterenol (beta-1,2): Use (Inject, inhalation; also oral and sublingual)

A

Bronchodilator in respiratory disorders

Cardiac stimulant in heart block, cardiogenic shock after MI, septicemic shock

27
Q

Isoproterenol: Adverse effects

A

Tachycardia and arrhythmia
Hypotension
Palpitation, anxiety, headache, angina

28
Q

DA (injection): Action

A

Beta-1 receptors in heart increase contractility and HR
High doses may activate vascular alpha-1 receptors causing vasoconstriction
DA receptor stimulation
- Vasodilator effect on renal, mesenteric, coronary, and intracerebral vessels
- Increase blood flow to kidneys

29
Q

DA: uses

A

Shock
HF
ARF
- Dopaminergic receptors

30
Q

DA: adverse effects

A

Tachycardia, arrhythmias, angina, hypertension
Nausea, vomitting
- CTZ (chemoreceptor trigger zone)
Ischemic necrosis with extravasation of large amounts

31
Q

DA: Drug interactions

A 
Many can oxidize CA
Methenothiazine
    - Block dopamine effect
Parkinsons drugs
    - Agonist
32
Q

DA: Administration

A

Dispensed in aqueous solution
Diluted dosage
Via IV

33
Q

Dobutamine: Use and mechanism

A

beta-1 effector

Used in HF

34
Q

Other Sympathomimetics

A 
Group A
   - Alpha adrenergic agents
Group B
   - Mixed; direct/indirect/CNS
Group C
   - Indirect
Group D
   - Beta adrenergic agents
35
Q

Group A: Agents

A

Alpha-1 selective agonists
- Phenylephrine
Alpha-2 selective
- Clonidine

36
Q

Phenylephrine: Action

A

Result of alpha-1 receptor stimulation

  • Vasoconstriction
  • Treatment of acute hypotensive conditions
37
Q

Phenylephrine: Use

A

Treatment of paroxysmal atrial tachycardia
- Vasoconstriction
- Treatment of acute hypotensive conditions
Reduction of regional blood flow
- Hemostasis
- Localizing drug at site of administration
- Decongestants
- Vasoconstriction of the blood vessels in the nasal mucosa
Ophthalmic
- Mydriasis
- Glaucoma
- Allergic hyperemia
- Localizing site of lesion in Horner’s syndrome

38
Q

Clonidine: Action and use

A

Presynaptic

Treats glaucoma

39
Q

Group B (Mixed): agents

A

Ephedrine

Amphetamines

40
Q

Ephedrine: Use

A

Additive in many different preparations

Used to make meth

41
Q

Ephedrine: Effects

A

Bronchodilator and mild stimulating properties

42
Q

Amphetamines: Drug

A

Phenylpropanolamine
- Could be used for appetite suppression however there is a rebound effect
- Decongestant
Push CA out of the storage vesicles and increase the amount of CA in the synapse

43
Q

Group D : Beta selective agents

A

Beta 2
- Metaproterenol
- Bronchodilator
- Could be useful to delay premature delivery
Beta 1
- Dobutamine
- Used for its cardiac stimulation

Pharmacology (13 decks)

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