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Block 1 - Week 6 > Autonomic Pharmacology > Flashcards

Autonomic Pharmacology Flashcards

(39 cards)

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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

Study These Flashcards
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

Study These Flashcards
A

Drugs that interfere with or block the action of acetylcholine

Produce opposite effect of cholinomimetics

18
Q

Cholinolytic general effects

Study These Flashcards
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

Study These Flashcards
A

Drugs that are antagonists of muscarinic/nicotinic receptors

20
Q

Three examples of direct-acting cholinolytics

Mechanisms of action

Indication

Study These Flashcards
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

Study These Flashcards
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

Study These Flashcards
A

Pralidoxime

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

Which adrenergic receptors react to epinephrine?

Why is this significant?

Study These Flashcards
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

Study These Flashcards
A

Locations:

  • Vascular smooth muscle

Effects:

  • Vasoconstriction (increases BP)
25
a2 Location Effect
Location * Presynaptic nerve terminals Effect * Inhibits norepinephrine release
26
b1 Location Effect
Location * Heart Effect * Increases heart rate and force of contraction
27
b2 Location Effect
Location * Bronchial, bladder, and uterine smooth muscle Effect * Bronchodilation * Urinary retention
28
b3 Location Effect
Location * Bladder and adipose tissue Effect * Urinary retention * Lipolysis
29
Sympathomimetics/Adrenomimetics
Drugs which produce effects similar to the effects of NE/EPI
30
Direct-acting sympathomimetics
Drugs that are agonists of alpha and beta receptors
31
Five examples of sympathomimetic drugs Mechanism of action Indication
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
Indirect-acting sympathomimetics
Drugs that produce sympathomimetic effects either by facilitating the synthesis and release of NE or by inhibiting the reuptake/degradation of NE
33
Two examples of indirect-acting sympathomimetics Mechanism of action Indication
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
Mixed-action sympathomimetics
Drugs the produce sympathomimetic effects by facilitating the release of NE from nerve endings and acting as adrenoceptor agonists
35
Two examples of mixed-action sympathomimetics Mechanism of action Indication
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
Sympatholytics
Drugs that interfere with or block the actions of NE/EPI
37
Direct-acting sympatholytics
Drugs that are _antagonists_ of alpha and beta receptors
38
5 examples of direct-acting sympatholytics Mechanism of action Indication
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
Indirect-acting sympatholytics
Drugs that produce sympatholytic effects either by inhibiting the synthesis or release of NE These drugs are currently not in clinical use

Block 1 - Week 6 (6 decks)

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