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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
How does Mixed-Acting Sympathomimetics work?
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.
26
Actions of A-Adrenergic Receptors?
~ 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)
27
Actions of B1 Adrenergic Receptors?
~ 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)
28
Actions of B2 Adrenergic Receptors?
~Bronchodilation (Relaxation of the bronchi) ~Uterine Relaxation ~ Glycogenolysis in the liver ~Increased renin secretion in the kidneys
29
What are the 6 B2-Adrenergic Drugs?
1. Ephedrine 2. Epinephrine 3. Formoterol 4. Salbutamol 5. Salmeterol Xinafoate 6. Terbutaline
30
Adverse Effects of A-Adrenergic?
~CNS: headache, restlessness, insomnia, euphoria ~Cardiovascular: Palpitations, tachycardia, vasoconstriction, HTN ~ Loss of appetite, dry mouth, nausea, vomiting
31
B-Adrenergic Adverse Effects?
~ CNS: mild tremors, headache, dizziness, nervousness ~ Cardiovascular: Increased heart rate, palpitations, fluctuations in Blood pressure ~Sweating, nausea, vomiting, muscle cramps
32
B-Adrenergic Interactions?
Thyroid Preparations Anti hypertensives Anesthetic Drugs Tricyclic Antidepressants MAOIs Antihistamines
33
What are Adrenergic Blockers?
Bind to Adrenergic receptors but inhibit or block stimulation of the sympathetic nervous system *Include A-Blockers and B-Blockers
34
What are Adrenergic Blockers also known as?
Adrenergic Antagonists Sympatholytics A-Blockers B-Blockers A-B-Blockers
35
What's another name for Adrenergic A-Blockers?
Ergot Alkaloids
36
Ergot Alkaloid Indications
~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
37
Common A-Blockers...
* Phentolamine Mesylate * Prazosin Hydrochloride * Alfuzosin Hydrochloride * Doxazosin Mesylate * Terazosin Hydrochloride
38
What does Phentolamine do?
*Rogitine Restores blood flow and prevents tissue necrosis
39
Contraindications of A-Blockers?
Drug Allergy Peripheral Vascular Disease Liver and Kidney Disease Coronary Artery Disease Peptic Ulcer Sepsis
40
A-Blocker Cardiovascular Adverse Effects?
Palpitations Orthodontic Hypotension Tachycardia Edema Dysrhythmias Chest Pain T
41
CNS A-Blocker Adverse Effects?
Dizziness Headache Drowsiness Anxiety Depression
42
GI A-Blocker Adverse Effects?
Nausea Vomiting Diarrhea Constipation Abdominal pain
43
What are Adrenergic Drugs?
Drugs that stimulate the sympathetic nervous system (SNS)
44
What do B-Blockers do?
Block stimulation of B receptors in SNS Compete with norepinephrine and epinephrine Include selective and non-selective B-Blockers
45
What do Non-Selective B-Blockers block?
Both B1 and B2 Receptors!
46
B1 Receptor location?
Located primarily in the heart and are called ----> | Cardioselective B-Blockers
47
Where are B2 Receptors located?
Primarily on smooth muscles of bronchioles and blood vessels
48
Mechanism of action for Cardioselective Blockers?
~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
Nonselective B-Blocker Mechanism of Action?
~Same effects on the heart ~Constriction of bronchioles ~Vasoconstriction of blood vessels
50
B-Blocker Indications?
Antiangina ---> decreases demand for myocardial oxygen Cardio protective ---> inhibits stimulation from Catecholamines Antihypertensive Migraines Glaucoma --> topical use*
51
B-Blocker Contraindications?
Drug allergies Uncompensated heart failure Heart block Cardiogenic shock Bradycardia Pregnancy Severe pulmonary disease
52
B-Blocker interactions with other drugs?
1. Antacids ----> decrease B-Blocker effects 2. Anticholinergics ---> decrease B-Blocker effects 3. Anti diuretics ---> additive hypotensive effects
53
Blood B-Blocker Adverse Effects?
Agranulocytosis Thrombocytopenia
54
Cardiovascular/Peripheral B-Blocker Adverse Effects?
AV block Heart Failure Bradycardia Vascular insufficiency
55
CNS B-Blocker Adverse Effects?
Dizziness Mental Depression Lethargy Hallucinations
56
3 Non-Selective B-Blocker Drugs?
1. Labetalol 2. Propranolol Hydrochloride 3. Sotalol Hydrochloride
57
4 Cardioselective B-Blocker Drugs?
1. Acebutolol Hydrochloride 2. Atenolol 3. Esmolol Hydrochloride 4. Metoprolol Tartrate
58
What are Cholinergic Drugs?
Drugs that stimulate the parasympathetic nervous system
59
What are Cholinergic Drugs also known as?
Cholinergic Agonists or Parasympathomimetics
60
What are the 2 types of Cholinergic Receptors?
1. Nicotinic Receptors | 2. Muscarinic Receptors
61
Where are Nicotinic Receptors located?
Ganglia of both the PSNS and SNS
62
Where are Muscarinic Receptors Located?
Postsynaptically in the effector organs of the PSNS such as: Smooth muscle Cardiac Muscle Glands
63
What is Alzheimer's Disease?
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
Alzheimer's Etiolgy
Genetic Environmental Lifestyle
65
Cholinergic Drug Mechanism of Action
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
2 Types of Indirect- Acting Cholinesterase Inhibitors
Reversible: Bind to Cholinesterase for a period of minutes/hours Irreversible: Bind to Cholinesterase and form a permanent covalent Bond
67
Cholinergic Drug Effects on the Intestine and Bladder?
Increase gastric secretions Increase Gastrointestinal motility Increased urinary frequency
68
What areas of the body does Cholinergic Drugs effect?
1. Intestines and Bladder 2. Pupils 3. Cardiovascular 4. Respiratory
69
Cholinergic Drug effects on the pupils?
Constriction (Miosis) Reduce Intraocular pressure
70
Cholinergic Drug effects on the cardiovascular system?
Decreased heart rate Vasodilation
71
Cholinergic Drug effects on the Respiratory System?
Bronchial Constriction, narrowed airways
72
Direct-Acting Cholinergic Drugs Indications?
*Poorly absorbed from the GIT Reduce Intraocular pressure Useful for glaucoma and Intraocular surgery
73
Direct-Acting Cholinergic Drugs for Glaucoma?
1. Acetylcholine 2. Carbachol 3. Pilocarpine
74
What's a Direct Acting Cholinergic Drug that's absorbed in the GIT?
Bethanechol
75
What does Bethanechol do?
Increases tone and motility of the bladder and GI tract Relaxes sphincters in bladder and GI tract, allowing them to empty
76
2 Indirect-Acting Cholinergic Drugs used as an antidote?
Neostigmine Pyridostigmine
77
Indirect Acting Cholinergic Drug Indications?
Cause skeletal muscle contractions Diagnosis and treatment of Myasthenia Gravis Reverse neuromuscular blocking drugs Reverse Anticholinergic Poisoning (Antidote)
78
What does Donepezil do?
An indirect acting Cholinergic drug that increases concentration of ACh in the pain and improve Cholinergic effects
79
What drug is used to treat or slow progression of Alzheimer's Disease?
Donepezil
80
Cholinergic Drug Contraindications
Drug allergy GI or GU tract obstruction (require surgery) Bradycardia Hyperthyroidism Epilepsy Hypotension Parkinson's Disease
81
Cholinergic Drug Adverse Effects?
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
Cholinergic Drug Interactions
Anticholinergics Antihistamines Sympathomimetics *Antagonize Cholinergic drugs resulting in decreased responses
83
What are Cholinergic -Blocking Drugs?
Drugs that block or inhibit the actions of acetylcholine (ACh) in the parasympathetic nervous system *Also known as Anti -cholinergics*
84
Cholinergic-Blocking Drug Mechanism of Action
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
Natural Cholinergic-Blocking Drugs
Atropine Belladonna Hyoscyamine Scopolamine
86
Cholinergic-Blocking Drug Effects
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
Cholinergic-Blocking Drug Indications
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
Cholinergic Blocking Drug Contradictions
Drug Allergy Narrow Angle Glaucoma Acute Asthma Myasthenia Gravis Acute cardiovascular instability GI or GU tract obstruction
89
Cholinergic-Blocking Drug Adverse Effects
Cardiovascular: Increased heart rate CNS: excitation, irritability, delirium, disorientation, hallucinations Eye: Dilated pupils, decreased visual accommodation GI: Decreased gastric secretions, decreased motility
90
Cholinergic-Blocking Drug Interactions
Antihistamines Monoamine Oxidase Inhibitors (MAOIs) *When given with Cholinergic-blocking drugs, these cause additive Cholinergic effects*
91
What's Parkinson's Disease?
A chronic, progressive, degenerative disorder Affects the dopamine-producing neurons in the brain
92
What 2 neurotransmitters cause Parkinson's when they become imbalanced?
Dopamine Acetylcholine (ACh)
93
Parkinson's Disease Symptoms
Rigidity Tremor Postural Instablity Bradykinesia
94
What is Levodopa Therapy?
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
Other Drug Therapies for Parkinson's?
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
Parkinson's disease Anti-Cholinergic Drug?
Benztropine
97
Parkinson's Disease Anti-Histamine Drug Name?
Diphenhydramine
98
Parkinson's Disease Dopamine Receptor Agonist Drugs?
Levodopa Bromocriptine Levodopa - Carbidopa
99
3 Indirect Acting Dopamine Receptor Agonists for Parkinson's Disease?
1. Selegiline: MAO-B Inhibitor (Monoamine Oxidase B) 2. Entacapone: COMT Inhibitor (Catechol Ortho-methyl transferase) 3. Amatadine: Symmetrel
100
Selegiline Indications?
Used in combination with Levodopa or Levodopa-Carbidopa Used when a patient's response to Levodopa is fluctuating
101
Adverse Effects of Selegiline?
``` Nausea Lightheaded mess Dizziness Abdominal Pain Insomnia Confusion Dry Mouth ```
102
Three Types of Dopaminergic Therapy?
1. Replacement 2. Direct-Acting/Replacement 3. Indirect-Acting - Amantadine * Adverse effects vary according to dose*
103
What is Anticholinergic Therapy?
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
Anticholinergic Therapy Adverse Effects?
Drowsiness, confusion, disorientation Constipation, nausea, vomiting Urinary Retention, pain on urination Blurred vision, dilated pupils, dry skin Decreased salvation, dry mouth
105
Anticholinergic Therapy Interactions?
~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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