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Pharmacology > Week 4 ~ Autonomic Nervous System > Flashcards

Week 4 ~ Autonomic Nervous System Flashcards

1
Q

What are two other names for Adrenergic Drugs?

A

Adrenergic Agonists

Sympathomimetics

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2
Q

What neurotransmitters does Adrenergic Drugs mimic?

A

Norepinephrine

Epinephrine

Dopamine

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3
Q

What are Adrenergic Receptors and what are the 3 receptors called?

A

Located throughout the body and are receptors for the sympathetic neurotransmitters

  1. A-Adrenergic Receptors
  2. B-Adrenergic Receptors
  3. Dopaminergic Receptors (For Dopamine Only)
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4
Q

What are the A-Adrenergic Agonist Receptors Responses?

A
  1. Vasoconstriction
  2. CNS stipulations
  3. Divided into a1 and a2 receptors
  4. Differentiated by their location on nerves
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5
Q

Where is the A1 Adrenergic Receptors located?

A

On the post synaptic effector cells

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6
Q

Where are the A2 Adrenergic Receptors located?

A

On pre-synaptic nerve terminals. Control the release of neurotransmitters

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7
Q

Functions of B-Adrenergic Receptors?

A

~Bronchial, GI and Uterine smooth muscle relaxation

~ Glycogenolysis

~Cardiac Stimulation

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8
Q

Location of B-Adrenergic Receptors?

A

All are located on postsynaptic effector cells

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9
Q

Where are B1 Adrenergic receptors located?

A

Primarily in the heart

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10
Q

Where are B2 Adrenergic Receptors located?

A

In smooth muscle of the bronchioles, arterioles, and visceral organs

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11
Q

What are the functions of Dopaminergic Receptors?

A

Stimulated by dopamine and cause dilation of the following blood vessels to increase blood flow:

Renal
Mesenteric
Coronary
Cerebral

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12
Q

What’s the receptor and response for receptor for Blood Vessels?

A

A1 and B2 —–> Constriction and dilation

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13
Q

What’s the receptor and response for cardiac muscle?

A

B1 —-> Increased contractility

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14
Q

What’s the Receptor and Response for Atrioventricular Node?

A

B1 —-> Increased Heart Rate

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15
Q

What’s the Receptor and Response for Sinoatrial Node?

A

B1 —-> Increased Heart Rate

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16
Q

What’s the Receptor and Response for Bronchial Muscles?

A

B2 —-> Dilation

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17
Q

What’s the Receptor and Response for Liver?

A

B2 —-> Glycogenolysis

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18
Q

What’s the Receptor and Response for Pupils?

A

A1 —–> Dilation

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19
Q

What are Catecholamines?

A

Substances that produce a sympathomimetic response

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20
Q

What are the Endogenous Catecholamines?

A

Epinephrine

Norepinephrine

Dopamine

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21
Q

What are the Synthetic Catecholamines?

A

Dobutamine

Phenylephrine

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22
Q

What are the 3 mechanism of actions of Sympathomimetics?

A
  1. Direct Acting
  2. Indirect Acting
  3. Mixed Acting
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23
Q

How do Direct-Acting Sympathomimetics work?

A

Binds directly to the receptor and causes a physiological response

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24
Q

How to Indirect-Acting Sympathomimetics work?

A

Cause the release of Catecholamine from storage sites (Vesicles) in the nerve endings. the Catecholamine then binds to the receptors and causes a physiological response

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25
Q

How does Mixed-Acting Sympathomimetics work?

A

Directly stimulates the receptor by binding to it and indirectly stimulates the receptor by causing the release of stored neurotransmitters from the vesicles in the nerve endings.

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26
Q

Actions of A-Adrenergic Receptors?

A

~ Vasoconstriction of blood vessels

~ Relaxation of GI smooth muscles

~ Contraction of the uterus and bladder

~ Male Ejaculation

~ Decreased insulin release

~ Contraction of the ciliary muscles of the eye (Dilated pupils)

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27
Q

Actions of B1 Adrenergic Receptors?

A

~ Affect the myocardium, AV node and SA node

~Increased force of heart contraction (+ve inotropic effect)

~Increased heart rate (+ve chronotropic effect)

~Increased conduction through the AV node (+ve dromotropic effect)

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28
Q

Actions of B2 Adrenergic Receptors?

A

~Bronchodilation (Relaxation of the bronchi)

~Uterine Relaxation

~ Glycogenolysis in the liver

~Increased renin secretion in the kidneys

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29
Q

What are the 6 B2-Adrenergic Drugs?

A
  1. Ephedrine
  2. Epinephrine
  3. Formoterol
  4. Salbutamol
  5. Salmeterol Xinafoate
  6. Terbutaline
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30
Q

Adverse Effects of A-Adrenergic?

A

~CNS: headache, restlessness, insomnia, euphoria

~Cardiovascular: Palpitations, tachycardia, vasoconstriction, HTN

~ Loss of appetite, dry mouth, nausea, vomiting

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31
Q

B-Adrenergic Adverse Effects?

A

~ CNS: mild tremors, headache, dizziness, nervousness

~ Cardiovascular: Increased heart rate, palpitations, fluctuations in
Blood pressure

~Sweating, nausea, vomiting, muscle cramps

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32
Q

B-Adrenergic Interactions?

A

Thyroid Preparations

Anti hypertensives

Anesthetic Drugs

Tricyclic Antidepressants

MAOIs

Antihistamines

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33
Q

What are Adrenergic Blockers?

A

Bind to Adrenergic receptors but inhibit or block stimulation of the sympathetic nervous system

*Include A-Blockers and B-Blockers

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34
Q

What are Adrenergic Blockers also known as?

A

Adrenergic Antagonists

Sympatholytics

A-Blockers

B-Blockers

A-B-Blockers

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35
Q

What’s another name for Adrenergic A-Blockers?

A

Ergot Alkaloids

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36
Q

Ergot Alkaloid Indications

A

~Constrict dilated arterioles in the brain

~Migraines

~ Stimulate uterine contractions (oxytocics) to control postpartum
Bleeding

~Treat Hypertension, especially in patients with Pheochromocytoma

~Benign prostatic hyperplasia, decrease resistance to urinary outflow

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37
Q

Common A-Blockers…

A
  • Phentolamine Mesylate
  • Prazosin Hydrochloride
  • Alfuzosin Hydrochloride
  • Doxazosin Mesylate
  • Terazosin Hydrochloride
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38
Q

What does Phentolamine do?

A

*Rogitine

Restores blood flow and prevents tissue necrosis

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39
Q

Contraindications of A-Blockers?

A

Drug Allergy

Peripheral Vascular Disease

Liver and Kidney Disease

Coronary Artery Disease

Peptic Ulcer

Sepsis

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40
Q

A-Blocker Cardiovascular Adverse Effects?

A

Palpitations

Orthodontic Hypotension

Tachycardia

Edema

Dysrhythmias

Chest Pain

T

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41
Q

CNS A-Blocker Adverse Effects?

A

Dizziness

Headache

Drowsiness

Anxiety

Depression

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42
Q

GI A-Blocker Adverse Effects?

A

Nausea

Vomiting

Diarrhea

Constipation

Abdominal pain

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43
Q

What are Adrenergic Drugs?

A

Drugs that stimulate the sympathetic nervous system (SNS)

44
Q

What do B-Blockers do?

A

Block stimulation of B receptors in SNS

Compete with norepinephrine and epinephrine

Include selective and non-selective B-Blockers

45
Q

What do Non-Selective B-Blockers block?

A

Both B1 and B2 Receptors!

46
Q

B1 Receptor location?

A

Located primarily in the heart and are called —->

Cardioselective B-Blockers

47
Q

Where are B2 Receptors located?

A

Primarily on smooth muscles of bronchioles and blood vessels

48
Q

Mechanism of action for Cardioselective Blockers?

A

~Reduces SNS stimulation of the heart

~Decreases heart rate

~ Slows conduction rate through the AV node

~Deceases myocardial contractility thus reducing myocardial oxygen
Demand

49
Q

Nonselective B-Blocker Mechanism of Action?

A

~Same effects on the heart

~Constriction of bronchioles

~Vasoconstriction of blood vessels

50
Q

B-Blocker Indications?

A

Antiangina —> decreases demand for myocardial oxygen

Cardio protective —> inhibits stimulation from Catecholamines

Antihypertensive

Migraines

Glaucoma –> topical use*

51
Q

B-Blocker Contraindications?

A

Drug allergies

Uncompensated heart failure

Heart block

Cardiogenic shock

Bradycardia

Pregnancy

Severe pulmonary disease

52
Q

B-Blocker interactions with other drugs?

A
  1. Antacids —-> decrease B-Blocker effects
  2. Anticholinergics —> decrease B-Blocker effects
  3. Anti diuretics —> additive hypotensive effects
53
Q

Blood B-Blocker Adverse Effects?

A

Agranulocytosis

Thrombocytopenia

54
Q

Cardiovascular/Peripheral B-Blocker Adverse Effects?

A

AV block

Heart Failure

Bradycardia

Vascular insufficiency

55
Q

CNS B-Blocker Adverse Effects?

A

Dizziness

Mental Depression

Lethargy

Hallucinations

56
Q

3 Non-Selective B-Blocker Drugs?

A
  1. Labetalol
  2. Propranolol Hydrochloride
  3. Sotalol Hydrochloride
57
Q

4 Cardioselective B-Blocker Drugs?

A
  1. Acebutolol Hydrochloride
  2. Atenolol
  3. Esmolol Hydrochloride
  4. Metoprolol Tartrate
58
Q

What are Cholinergic Drugs?

A

Drugs that stimulate the parasympathetic nervous system

59
Q

What are Cholinergic Drugs also known as?

A

Cholinergic Agonists or Parasympathomimetics

60
Q

What are the 2 types of Cholinergic Receptors?

A
  1. Nicotinic Receptors

2. Muscarinic Receptors

61
Q

Where are Nicotinic Receptors located?

A

Ganglia of both the PSNS and SNS

62
Q

Where are Muscarinic Receptors Located?

A

Postsynaptically in the effector organs of the PSNS such as:

Smooth muscle
Cardiac Muscle
Glands

63
Q

What is Alzheimer’s Disease?

A

Most common form of dementia in Canada

Progressive and degenerative disease

Impairment of memory, judgement, language, personality

*Brain tissue shrinks as the disease progesses

64
Q

Alzheimer’s Etiolgy

A

Genetic

Environmental

Lifestyle

65
Q

Cholinergic Drug Mechanism of Action

A
  1. Direct Acting —> bind to Cholinergic receptors and activate
  2. Indirect Acting —-> inhibit the enzyme Cholinesterase
    Which breaks down ACh allowing more
    ACh being available at the receptors
66
Q

2 Types of Indirect- Acting Cholinesterase Inhibitors

A

Reversible: Bind to Cholinesterase for a period of minutes/hours

Irreversible: Bind to Cholinesterase and form a permanent covalent
Bond

67
Q

Cholinergic Drug Effects on the Intestine and Bladder?

A

Increase gastric secretions

Increase Gastrointestinal motility

Increased urinary frequency

68
Q

What areas of the body does Cholinergic Drugs effect?

A
  1. Intestines and Bladder
  2. Pupils
  3. Cardiovascular
  4. Respiratory
69
Q

Cholinergic Drug effects on the pupils?

A

Constriction (Miosis)

Reduce Intraocular pressure

70
Q

Cholinergic Drug effects on the cardiovascular system?

A

Decreased heart rate

Vasodilation

71
Q

Cholinergic Drug effects on the Respiratory System?

A

Bronchial Constriction, narrowed airways

72
Q

Direct-Acting Cholinergic Drugs Indications?

A

*Poorly absorbed from the GIT

Reduce Intraocular pressure

Useful for glaucoma and Intraocular surgery

73
Q

Direct-Acting Cholinergic Drugs for Glaucoma?

A
  1. Acetylcholine
  2. Carbachol
  3. Pilocarpine
74
Q

What’s a Direct Acting Cholinergic Drug that’s absorbed in the GIT?

A

Bethanechol

75
Q

What does Bethanechol do?

A

Increases tone and motility of the bladder and GI tract

Relaxes sphincters in bladder and GI tract, allowing them to empty

76
Q

2 Indirect-Acting Cholinergic Drugs used as an antidote?

A

Neostigmine

Pyridostigmine

77
Q

Indirect Acting Cholinergic Drug Indications?

A

Cause skeletal muscle contractions

Diagnosis and treatment of Myasthenia Gravis

Reverse neuromuscular blocking drugs

Reverse Anticholinergic Poisoning (Antidote)

78
Q

What does Donepezil do?

A

An indirect acting Cholinergic drug that increases concentration of ACh in the pain and improve Cholinergic effects

79
Q

What drug is used to treat or slow progression of Alzheimer’s Disease?

A

Donepezil

80
Q

Cholinergic Drug Contraindications

A

Drug allergy

GI or GU tract obstruction (require surgery)

Bradycardia

Hyperthyroidism

Epilepsy

Hypotension

Parkinson’s Disease

81
Q

Cholinergic Drug Adverse Effects?

A

Cardiovascular: Bradycardia, hypotension

CNS: Headache, dizziness, convulsions

GI: abdominal cramps, nausea/vomiting, increased secretions

Respiratory: Increased bronchial secretions, bronchospasms

Lacrimation, sweating, salivation, loss of binocular accommodation

82
Q

Cholinergic Drug Interactions

A

Anticholinergics

Antihistamines

Sympathomimetics

*Antagonize Cholinergic drugs resulting in decreased responses

83
Q

What are Cholinergic -Blocking Drugs?

A

Drugs that block or inhibit the actions of acetylcholine (ACh) in the parasympathetic nervous system

Also known as Anti -cholinergics

84
Q

Cholinergic-Blocking Drug Mechanism of Action

A
  1. Competitive Antagonists: Compete with ACh
  2. Block ACh at the Muscarinic receptors in the PSNS
    As a result ACh is unable to bind to the receptor site

*Once these drugs bind to receptors, they inhibit nerve transmission at these receptors

85
Q

Natural Cholinergic-Blocking Drugs

A

Atropine

Belladonna

Hyoscyamine

Scopolamine

86
Q

Cholinergic-Blocking Drug Effects

A

Cardiovascular:

     - ---> Small doses decrease heart rate
     - ---> Large doses increase heart rate

CNS:

  - ---> small doses decrease muscle rigidity and tremors
  - ---> large doses cause drowsiness, disorientation

Eye: Dilated pupils

GI: Relax smooth muscle tone of GI tract and decrease intestinal
And gastric secretions

  • Decreased bronchial secretions, salivation, sweating
  • Increased constriction of internal sphincter
  • Dilated bronchial airways
87
Q

Cholinergic-Blocking Drug Indications

A

CNS: Decreased muscle rigidity and muscle tremors used
In Parkinson’s disease

Cardiovascular: Low doses slow the heart rate
High dosses block inhibitory vagal effects and
Results in increased heart rate

Respiratory System:
Bronchodilation—> chronic bronchitis, COPD, Asthma

Incontinence

IBS

88
Q

Cholinergic Blocking Drug Contradictions

A

Drug Allergy

Narrow Angle Glaucoma

Acute Asthma

Myasthenia Gravis

Acute cardiovascular instability

GI or GU tract obstruction

89
Q

Cholinergic-Blocking Drug Adverse Effects

A

Cardiovascular: Increased heart rate

CNS: excitation, irritability, delirium, disorientation, hallucinations

Eye: Dilated pupils, decreased visual accommodation

GI: Decreased gastric secretions, decreased motility

90
Q

Cholinergic-Blocking Drug Interactions

A

Antihistamines
Monoamine Oxidase Inhibitors (MAOIs)

When given with Cholinergic-blocking drugs, these cause additive Cholinergic effects

91
Q

What’s Parkinson’s Disease?

A

A chronic, progressive, degenerative disorder

Affects the dopamine-producing neurons in the brain

92
Q

What 2 neurotransmitters cause Parkinson’s when they become imbalanced?

A

Dopamine

Acetylcholine (ACh)

93
Q

Parkinson’s Disease Symptoms

A

Rigidity

Tremor

Postural Instablity

Bradykinesia

94
Q

What is Levodopa Therapy?

A

Levodopa is a precursor of dopamine

The blood brain barrier doesn’t allow dopamine to enter but it allows Levodopa to enter

As Parkinson’s progresses it becomes more and more difficult to control with levodopa

95
Q

Other Drug Therapies for Parkinson’s?

A
  1. Anticholinergic Drug
    —> Block the effects of ACh
    —> Used to treat tremors and muscle rigidity
    (Two symptoms caused by excessive Cholinergic activity)
  2. Antihistamines
  3. Dopamine Receptor Agonist (Direct Acting)
96
Q

Parkinson’s disease Anti-Cholinergic Drug?

A

Benztropine

97
Q

Parkinson’s Disease Anti-Histamine Drug Name?

A

Diphenhydramine

98
Q

Parkinson’s Disease Dopamine Receptor Agonist Drugs?

A

Levodopa

Bromocriptine

Levodopa - Carbidopa

99
Q

3 Indirect Acting Dopamine Receptor Agonists for Parkinson’s Disease?

A
  1. Selegiline: MAO-B Inhibitor (Monoamine Oxidase B)
  2. Entacapone: COMT Inhibitor (Catechol Ortho-methyl transferase)
  3. Amatadine: Symmetrel
100
Q

Selegiline Indications?

A

Used in combination with Levodopa or Levodopa-Carbidopa

Used when a patient’s response to Levodopa is fluctuating

101
Q

Adverse Effects of Selegiline?

A 
Nausea
Lightheaded mess
Dizziness
Abdominal Pain
Insomnia
Confusion
Dry Mouth
102
Q

Three Types of Dopaminergic Therapy?

A
  1. Replacement
  2. Direct-Acting/Replacement
  3. Indirect-Acting - Amantadine
    * Adverse effects vary according to dose*
103
Q

What is Anticholinergic Therapy?

A

ACh accumulates because of the imbalance of dopamine

Overstimulation of the Cholinergic excitatory causes:
Muscle Tremors and Muscle Rigidity
Cogwheel Rigidity
Pill-Rolling movement of fingers and head bobbing while at rest

In Parkinson’s it causes smooth muscle relaxation, reduces muscle riding its and akinesia

104
Q

Anticholinergic Therapy Adverse Effects?

A

Drowsiness, confusion, disorientation

Constipation, nausea, vomiting

Urinary Retention, pain on urination

Blurred vision, dilated pupils, dry skin

Decreased salvation, dry mouth

105
Q

Anticholinergic Therapy Interactions?

A

~Enhanced CNS depressant effects with:

alcohol
CNS depressants
Amantadine (Symmetrel)
Antihistamines
Tricyclic Antidepressants
Phenothiazines

Reduced absorption and decreased therapeutic affect with antacids

Pharmacology (6 decks)

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