Autonomic Nervous System Drugs Flashcards

1
Q

Epinephrine

A

Class: Nonspecific Sympathetic Agonists (Adrenergic Pharmacology)

Mechanism of action: Direct stimulation of α and β adrenergic receptors

Indication: Local vasoconstriction, hypotension and shock, bronchodilation, allergy

Uses in dentistry: vasoconstriction (less bleeding and makes the analgesia last longer)

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: cardiac (β1 stimulation increases the work of the heart and decreases cardiac efficiency), cerebrovascular, diabetes (increases in circulating blood glucose from stimulation of liver glycogenolysis and glucagon secretion Inhibition of insulin secretion), Parkinson’s disease, thyroid disease
  • Contraindicated drugs: Tricyclic Antidepressants (block reuptake and degradation of epi, leading to more cardiac adverse effects), β-Blockers: (non-selective:block β receptors in the peripheral blood vessels, epi acts as a pure α agonist and blood pressure rises; selective block β1 receptors in heart, at high doses block β 2 receptors in peripheral blood vessels; upper limit: 0.04 mg total per procedure)
  • Which analgesic can the patient take
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2
Q

Methylphenidate (Ritalin, Concerta); Amphetamine (Adderall)

A

Class: α Sympathetic Agonists (Adrenergic Pharmacology)

Mechanism of action: Release of norepinephrine from synaptic vesicle

Indication: ADHD and narcolepsy

Pharmacological effects

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: cardiac risk; abuse and addiction (schedule 2–Ritalin and Adderall); dyskinesia, muscle tightness, bruxism
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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3
Q

Provigil (Modafinil)

A

Class: α1 Sympathetic Agonist (Adrenergic Pharmacology)

Mechanism of action: Inhibitor of dopamine reuptake

Indication: Narcolepsy, shift work disorder

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: mania, delusions, hallucinations, suicidal ideation and aggression, persistent sleepiness
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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4
Q

Clonidine (Catapres)

A

Class: Presynaptic α2 Sympathetic Agonist (Adrenergic Pharmacology)

Mechanism of action: Inverse Agonist–Binds to α2 medullary receptors in the brain which inhibit sympathetic outflow to the body and α receptors in blood vessels are inhibited

Indication: hypertension (oral tablet and patch–Catapres TTS); used with opiates to relieve the pain associated with end-stage cancer (epidural injection)

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider:
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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5
Q

Albuterol (Proventil)

A

Class: β2 Sympathetic Agonist (Adrenergic Pharmacology)

Mechanism of action: Stimulation of β2 receptors in lungs to cause bronchodilation

Indication: Asthma, COPD

Pharmacological effects: Inhaled–β2 receptors in the lungs will receive most of the drug to decrease the chance for adverse effects

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: unusual taste and drying/irritation of the oropharynx
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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6
Q

Terazosin (Hytrin)

A

Class: α Sympathetic Antagonist (Adrenergic Pharmacology)

Mechanism of action: α1 receptor blockade, leading to smooth muscle relaxation

Indication: HTN and benign prostatic hyperplasia

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: Dry mouth, dizziness , orthostatic hypotension
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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7
Q

Tamsulosin (Flomax)

A

Class: α Sympathetic Antagonist (Adrenergic Pharmacology)

Mechanism of action: Blockade of α1A and α1D adrenergic receptor subtypes found only in prostate gland

Indication: Benign prostatic hyperplasia

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider:
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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8
Q

Metoprolol (Toprol XL)

A

Class: Selective β1 Sympathetic Antagonists (Adrenergic Pharmacology)

Mechanism of action: Competitive inhibitors of epinephrine and norepi at β1

Indication: Angina, CHF, HTN

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: Altered taste, lichenoid rxns, orthostatic hypotension
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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9
Q

Propranolol (Inderal)

A

Class: Nonselective β Sympathetic Antagonists (Adrenergic Pharmacology)

Mechanism of action: Non-selective competitive inhibitor of beta receptors

Indication: Cardiovascular Disease, Stage fright, Tremor, Migraine headache

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: Altered taste, lichenoid rxns, orthostatic hypotension; may enhance the pressor response to epinephrine, hypertension and bradycardia
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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10
Q

Carvedilol (Coreg)

A

Class: β Sympathetic Antagonists (Adrenergic Pharmacology)

Mechanism of action: Antagonist at β1 and α1 receptors

Effect: Decrease heart rate and contractility and decrease blood pressure through alpha blockade

Indication: CHF (congestive heart failure)

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider:
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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11
Q

Tacrine (Cognex)

A

Class: Parasympathetic Agonist; Cholinesterase Inhibitors (Cholinergic Pharmacology)

Mechanism of action: Prolong acetylcholine half life in the brain

Indication: Alzheimer’s, Parkinson’s disease with dementia

Pharmacological effects:

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: nausea, diarrhea, vomiting, rhinitis, urinary frequency, bronchospasm, hypotension, arrhythmias (parasympathetic reactions); Contraindicated in asthma, cardiovascular disease, and ulcer
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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12
Q

Pilocarpine (Salagen), Cevimeline (Evoxac)

A

Class: Parasympathetic Agonist; Cholinesterase Inhibitors (Cholinergic Pharmacology)

Mechanism of action: Agonist at muscarinic receptors

Indication: salivary stimulants for dry mouth (doses are individualized for desired effects until adverse reactions become intolerable)

Pharmacological effects: nausea, diarrhea, vomiting, rhinitis, urinary frequency, bronchospasm, hypotension, arrhythmias (parasympathetic reactions); Contraindicated in asthma, cardiovascular disease, and ulcer

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: use with caution in patients with COPD, Parkinson’s disease
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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13
Q

Ipratropium (Atrovent), Tiotropium (Spiriva)

A

Class: Parasympathetic Antagonists; Antimuscarinic Drugs (Cholinergic Pharmacology)

Mechanism of action: Bronchodilation

Indication: Asthma, COPD

Pharmacological effects: Bronchodilation Ipratropium (Atrovent) or in combination inhalation product with albuterol (Combivent Inhaler); Tiotropium (Spiriva) prolonged T ½ used primarily in COPD

How this drug might effect dental treatment of patient

-Adverse effects you have to consider:

  • Contraindicated drugs: Anticholinergic effects are potentiated by antihistamines (this leads to severe dry mouth)
  • Which analgesic can the patient take:
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14
Q

Tolterodine (Detrol), Darifenacin (Enablex)

A

Class: Parasympathetic Antagonists; Antimuscarinic Drugs (Cholinergic Pharmacology)

Mechanism of action: Antispasmodics

Indication: Urinary

Pharmacological effects: Contracts urinary sphincter muscles used in dysuria, urgency, incontinence; Darifenacin (Enablex): M3 selective agent, less dry mouth and constipation

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider:
  • Contraindicated drugs: Anticholinergic effects are potentiated by antihistamines (this leads to severe dry mouth); CYP2D6 Inhibitors may diminish the therapeutic effect of Codeine (Enablex)
  • Which analgesic can the patient take:
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15
Q

Varenicline (Chantix)

A

Class: Parasympathetic Agonist (Cholinergic Pharmacology)

Mechanism of action: Produces agonist activity, while simultaneously preventing nicotine binding to α4β2 receptors

Indication: Smoking cessation

Pharmacological effects: Stimulates receptor-mediated activity, but at a significantly lower level than nicotine

How this drug might effect dental treatment of patient

  • Adverse effects you have to consider: nightmares and psychosis
  • Contraindicated drugs:
  • Which analgesic can the patient take:
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16
Q

Botulinum Toxin Type A Botox

A

Prevents synaptic vesicle fusion with membrane
Focal dystonias
Headache and pain syndromes

17
Q

Function of ANS

A

Sympathetic Arm: Flight or Fight (Dental Appointment)

  • Adrenergic Receptors
  • Norepinephrine

Parasympathetic Arm: Rest and Digest

  • Muscarinic (Cholinergic) Receptors
  • Acetylcholine
18
Q

Effects of Norepinephrine

A
Tachycardia
Vasoconstriction
Bronchodilation
Contraction of urinary sphincter
Decreased GI secretions
Glycogenolysis
Gluconeogenesis
Lipolysis
19
Q

Effects of Acetylcholine

A
Bradycardia
Vasodilation
Bronchoconstriction
Relaxation of urinary sphincter
Increase GI secretions
Sweating
Contraction of iris
SLUD Response:
-Salivation
-Lacrimation
-Urination
-Defecation
20
Q

How Adverse Effects are Avoided

A

Dosage forms selective for 1 tissue
-Examples: inhalers or eye drops
Design drugs that are specific for one type of a receptor
-Examples: M1-M5 for muscarinics; α 1 or 2; β1 or 2 for adrenergic
Adverse Effects are still a problem esp. at higher doses

21
Q

General Mechanisms by which Autonomic Nervous System Drugs Act

A

Influence release of the neurotransmitter
Influence degradation of the neurotransmitter
Influence reuptake of the neurotransmitter
Bind (agonist) or block (antagonist) receptor

22
Q

Drug Class in ANS

A

Adrenergic Pharmacology

Cholinergic Pharmacology

23
Q

Therapeutic Uses of Drugs at Adrenogenic Receptors (Agonists)

A
Bronchodilation in emergency 
-Example:  Epinephrine
ADHD:	
-Examples: Ritalin and Adderall
HTN inverse agonist
-Example: Catapres
Bronchodilation
-Examples:Proventil
24
Q

Therapeutic Uses of Drugs at Adrenegeric Receptors (Antagonists)

A
HTN, Post myocardial infarction, CHF, Treatment of arrhythmias, Ischemic heart disease
-α blocker:  Hytrin
-β blockers::Toprol, Propranolol, Coreg
Benign prostatic hyperplasia:
-α blocker:  Hytrin, Flomax
25
Q

PCOL Effects of β Blockers

A

↓ the force and rate of myocardial contraction
↓ O2 consumption of the heart
↓ of blood pressure in hypertensive patients
CO decreases
HR decreases
Reduction in plasma renin activity
Decrease CNS sympathetic outflow
Alteration in baroreceptor responsiveness

26
Q

Cholinergic Drugs

A

Mimic parasympathetic nervous system stimulation and produce parasympathetic responses
2 Mechanisms:
-Reversible Cholinesterase Inhibition –Prolong t1/2 of acetylcholine at receptor site
-Direct Acting – Bind to and stimulate muscarinic receptors

27
Q

PCOL Effects of Antimuscarinic Drugs

A
GI:↓ motor and secretory responses
Eye:Dilation
Urinary Retention
Respiratory Tract:Relaxation
Salivary Glands:↓ Secretion
28
Q

Therapeutic Uses of Antimuscarinic Drugs

A

Bronchodilation: Asthma and COPD:
-Examples: Ipratropium (Atrovent), Tiotropium (Spiriva)
Urinary: antispasmodics; contracts urinary sphincter muscles used in dysuria, urgency, incontinence
-Examples: Tolterodine (Detrol), Darifenacin (Enablex)–M3 selective agent, less dry mouth and constipation

29
Q

Bronchodilation

A
Asthma and COPD: 
Bronchodilation Ipratropium (Atrovent) or in combination inhalation product with albuterol (Combivent Inhaler)
Tiotropium (Spiriva) prolonged T ½ used primarily in COPD
30
Q

Therapeutic Uses of Drugs at Nicotinic Receptors

A

Only therapeutic use for nicotine: in smoking cessation programs, gum, patches
Neuromuscular junction blockers are used in surgery and intubation –succinylcholine
Botulinum toxin type A-Botox

31
Q

Nicotine

A

α4β2 neuronal nicotinic acetylcholine receptors
Stimulate the central nervous mesolimbic dopamine system
Neuronal mechanism underlying reinforcement and reward experienced upon smoking