Autonomic Pharmacology Flashcards

1
Q

-lytic

A
  • Blocking or impairing
  • Interfering medications
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2
Q

-mimetic

A
  • Mimicking or enhancing
  • Medication that amplifies
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3
Q

Cholinergic Neurotransmitters and Receptors

A
  • Acetylcholine is the NT
  • in the ANS:
    • All parasympathetic and sympathetic pre-ganglionic fibers
    • All parasympathetic post-ganglionic fibers
    • Sympathetic post-ganglionic fiber innervated to sweat glands
  • Two major classes of receptors for acetylcholine:
    • Muscarinic
    • Nicotinic
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4
Q

Muscarinic:

Receptor Type

Neurotransmitter

Subtypes

A
  • Receptor Type: G-Protein Coupled Receptors
  • Neurotransmitter: Acetylcholine
  • Subtypes: M1 through M5
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5
Q

Nicotinic:

Receptor Type

Neurotransmitter

Subtypes

A
  • Receptor Type: Linked to Ion Channels
  • Neurotransmitter: Acetylcholine
  • Subtypes:
    • Muscle-Type on Skeletal Muscle
    • Neuronal-Type (will cover more in block 3)
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6
Q

Cholinergic activation causes what symptoms?

A
  • Diarrhea
  • Urination
  • Miosis (constriction of the pupil)
  • Bradycardia
  • Bronchoconstriction
  • Emesis
  • Lacrimation (the flow of tears)
  • Salivation

Cholinergic = DUMBBELS

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7
Q

M1 Location

A

CNS and peripheral nerves

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8
Q

M2

Location

Effect

A

Location: Heart and presynaptic nerve terminals

Effect:

  • Decrease HR and contractility
  • Inhibits Ach release
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9
Q

M3

Location

Effect

A

Location:

  • Iris constrictor and ciliary muscle
  • Vascular endothelium
  • GI muscle, bladder, uterus
  • Gastric parietal cells
  • Bronchial smooth muscle
  • Exocrine glands

Effect:

  • Contraction miosis/accommodation
  • EDRF release –> vasodilation
  • Increase GI motlity and urination
  • Acid secretion/digestion
  • Bronchoconstriction
  • Salivation/Lacrination
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10
Q

M4 Location

A

CNS neurons

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11
Q

M5

Location

Effect

A

Location: Vascular endothelium

Effect: Vasodilation

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12
Q

Cholinomimetics

A

Drugs which produce effects similar to the effects of Acetylcholine

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13
Q

Direct-acting cholinomimetics

A

Drugs that act as agonists of muscarinic/nicotinic receptors

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14
Q

Three examples of cholinomimetics

Mechanisms of Action

Indication

A

Bethanechol

  • Muscarinic receptor agonist (non-specific)
  • Used to treat urinary retention

Pilocarpine

  • Muscarinic receptor agonist (non-specific)
  • Used to treat glaucoma and Sjogren’s syndrome

Nicotine

  • Nicotinic receptor agonist (non-specific)
  • Used for smoking cessation
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15
Q

Indirect-acting cholinomimetic

A

Drugs that produce cholinomimetic effects either by facilitating synthesis/release of Ach or by inhibiting degredation of Ach

Becuase they incre [Ach] they can have effects at (neuromuscular junctions (nicotinic)

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16
Q

Two examples of indirect-acting cholinomimetics

Mechanism of action

Indication

A

Neostigmine

  • Cholinesterase inhibitor (reversible, intermediate-acting)
  • Used to treat Myasthenia gravis

Donepezil

  • Cholinesterase inhibitor (reversible, intermediate-acting)
  • Used to treat Alzheimer’s disease
17
Q

Cholinolytics definition

A

Drugs that interfere with or block the action of acetylcholine

Produce opposite effect of cholinomimetics

18
Q

Cholinolytic general effects

A

Produce opposite effect of cholinomimetics

Opposite of DUMBBELS:

Constipation (instead of diarrhea)

Urinary retention (instead of urination)

Mydriasis: dialation of pupil (instead of miosis)

Tachycardia (instead of bradycardia)

Bronchodilation (instead of bronchoconstriction)

Decreased GI motility/secretion (instead of emesis)

Dry eyes (instead of lacrimation)

Dry mouth (instead of salivation

19
Q

Direct-acting cholinolytics

A

Drugs that are antagonists of muscarinic/nicotinic receptors

20
Q

Three examples of direct-acting cholinolytics

Mechanisms of action

Indication

A

Atropine

  • Muscarinic receptor antagonist (non-specific)
  • Used to treat cardiac arrest, IBS, and organophosphorus poisoning (a pestiside)

Oxybutynin

  • Muscarinic receptor antagonist (non-specific)
  • Used to treat urinary incontinence

Darifenacin

  • Muscarinic receptor antagonist (M3 specific)
  • Used to treat urinary incontinence
21
Q

Indirect-acting cholinolytic

A

Drugs that produce cholinolytic effects by either inhibiting the synthesis/release of Ach or by promoting the Ach degradation

22
Q

One example of a indirect-acting cholinolytic

Mechanism of action

Indication

A

Pralidoxime

  • Cholinesterase regenerator
  • Used to treat organophosphorus poisoning (a pesticide)
23
Q

Which adrenergic receptors react to epinephrine?

Why is this significant?

A

All of them: a1, a2, b1, b2, and b3

This is significant because activation of the sympathetic nervous system leads to the adrenal glands releasing epinephrine into the bloodstream

24
Q

a1

Location

Effects

A

Locations:

  • Vascular smooth muscle

Effects:

  • Vasoconstriction (increases BP)
25
Q

a2

Location

Effect

A

Location

  • Presynaptic nerve terminals

Effect

  • Inhibits norepinephrine release
26
Q

b1

Location

Effect

A

Location

  • Heart

Effect

  • Increases heart rate and force of contraction
27
Q

b2

Location

Effect

A

Location

  • Bronchial, bladder, and uterine smooth muscle

Effect

  • Bronchodilation
  • Urinary retention
28
Q

b3

Location

Effect

A

Location

  • Bladder and adipose tissue

Effect

  • Urinary retention
  • Lipolysis
29
Q

Sympathomimetics/Adrenomimetics

A

Drugs which produce effects similar to the effects of NE/EPI

30
Q

Direct-acting sympathomimetics

A

Drugs that are agonists of alpha and beta receptors

31
Q

Five examples of sympathomimetic drugs

Mechanism of action

Indication

A

Epinephrine

  • Alpha and beta receptor agonist (non-specific)
  • Used to treat anaphylactic shock

Phenylephrine

  • Alpha-1 receptor agonist (causes vasoconstriction)
  • Used to treat nasal congestion

Clonidine

  • Alpha-2 receptor agonist (decrease NE release)
  • Used to treat hypertension

Dobutamine

  • Beta-1 receptor agonist (increase HR and cardiac output)
  • Used to treat cardiogenic shock and acute heart failure

Terbutaline

  • Beta-2 receptor agonist (relaxes bronchial/tracheal smooth muscle)
  • Used to treat asthma
32
Q

Indirect-acting sympathomimetics

A

Drugs that produce sympathomimetic effects either by facilitating the synthesis and release of NE or by inhibiting the reuptake/degradation of NE

33
Q

Two examples of indirect-acting sympathomimetics

Mechanism of action

Indication

A

Amphetamine

  • Facilitate release of NE from sympathetic nerve endings
  • Used to treat ADHD

Selegiline

  • Inhibits NE/EPI metabolizing enzyme monoamine oxidase (MAO)
  • Used to treat the symptoms of Parkinson’s disease
34
Q

Mixed-action sympathomimetics

A

Drugs the produce sympathomimetic effects by facilitating the release of NE from nerve endings and acting as adrenoceptor agonists

35
Q

Two examples of mixed-action sympathomimetics

Mechanism of action

Indication

A

Ephedrine

  • Facilitates NE release (indirect) and activates both alpha and beta receptors (direct)
  • Used to treat nasal congestion

Pseudoephedrine

  • Facilitates NE release (indirect) and activates both alpha and beta receptors (direct)
  • Used to treat nasal congestion
36
Q

Sympatholytics

A

Drugs that interfere with or block the actions of NE/EPI

37
Q

Direct-acting sympatholytics

A

Drugs that are antagonists of alpha and beta receptors

38
Q

5 examples of direct-acting sympatholytics

Mechanism of action

Indication

A

Labetalol

  • Blocks all alpha and beta receptors except alpha-2 (non-specific)
  • Used to treat hypertension

Phenoxybenzamine

  • Alpha blocker, irreversible (non-specific)
  • Used to treat pheochromocytoma (rare adrenal gland tumor)

Doxazosin

  • Alpha-1 blocker
  • Used to treat hypertension and BPH

Propranolol

  • Beta blocker (non-specific)
  • Used to treat hypertension, angina pectoris, and arrhythmias

Atenolol

  • Beta-1 blocker
  • Used to treat hypertension, angina pectoris, and arrhythmias
39
Q

Indirect-acting sympatholytics

A

Drugs that produce sympatholytic effects either by inhibiting the synthesis or release of NE

These drugs are currently not in clinical use