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Pharmacology > Lecture 3: Drugs Affecting the ANS > Flashcards

Lecture 3: Drugs Affecting the ANS Flashcards

1
Q

Describe the flow chart for “Drugs Affecting the Parasympathetic System”. You do not have to say specific drugs, only the main categories.

A
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2
Q

Name the drugs which are direct muscarinic receptor agonists (cholinomimetic, parasympathomimetic).

A
  • Bethanechol
  • Pilocarpine
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3
Q

What are the uses of Bethanechol?

A

Stimulates an atonic bladder if a patient is experiencing urinary retention (often occurring post-partum or post-operatively) through its effects to relax the urinary sphincter and contract muscles of the bladder. This can help with an enlarged prostate in early stages.

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4
Q

What are potential adverse effects of Bethanechol and what is its duration of action?

A

Adverse effects - includes those expected from cholinergic stimulation, including sweating, salivation, hypotension, nausea, diarrhea, abdominal pain and bronchospasm.

Duration of action = 1 hr.

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5
Q

What are the uses of Pilocarpine?

A

Used primarily in opthamology to produce miosis and decrease intraocular pressure (both which are helpful for glaucoma). Can also be used to increase salivation in patients with dry mouth.

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6
Q

What are the adverse effects of Pilocarpine and what is its duration of action?

A

Adverse effects - If administered orally (instead of in the eye), pilocarpine can cause disturbances of the central nervous system and stimulate profuse sweating and salivation.

Duration: Long-acting (up to 8 hours)

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7
Q

What are the indirect cholinergic agonists (reversible anticholinesterases)?

A
  • Physostygmine
  • Neostigmine, Pyridostigmine, Ambenonium
  • Donepezil hydrochloride
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8
Q

What are the uses of Physostigmine?

A

Increases motility of the GI tract and bladder and can be used in atony of either organ.

Can also be used to treat glaucoma when used opthamologically, but pilocarpine is more effective.

May be used in Alzheimers to increase ACh because physostigmine is able to cross the blood brain barrier (BBB).

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9
Q

What are the adverse effects of Physostigmine? Duration?

A

Adverse effects can include convulsions at high doses, and slowing of the heart rate (bradycardia)

Drug crosses blood, brain barrier (BBB) and can therefore act centrally both therapeutically (alzheimers) as well as to create greater adverse effects.

Duration of action = 2-4 hours

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10
Q

What are the uses of Neostigmine, Pyridostigmine and Ambenonium?

A

Symptomatic treatment of myasthenia gravis.

(Myasthenia gravis is a neuromuscular disorder that causes weakness in skeletal muscles. It is generally considered to be an autoimmune disease.)

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11
Q

What are the adverse effects of Neostigmine, Pyridostigmine and Ambenonium? Duration of effect?

A

Adverse effects – Typical effects of cholinergic stimulation

Special Notes - Unlike physostigmine, these drugs do not enter the CNS. They instead have a greater effect on skeletal muscle and no CNS effects.

Varying duration of action, with neostigmine being the shortest (30min – 2hrs) and the others being 4-8hrs.

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12
Q

What are the uses of Donepezil Hydrochloride? Adverse effectss?

A

Used specifically for Alzheimers dementia because it is lipid soluble and easily crosses the BBB

Adverse effects – Similar to physostigmine… can include convulsions at high doses, and slowing of the heart rate (bradycardia).

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13
Q

Compare Alzheimer’s and dementia.

A
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14
Q

What are the irreversible indirect agonists (anticholinesterases)?

A

Organophosphates (eg. Tabun, Malathione)

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15
Q

What are the uses for organophosphates? What is the mechanism of action?

A

These agents are not used clinically. They are used as pesticides, and in the past have been used in warfare.

Nervous system poison through the permanent inactivation of acetylcholinesterase. Results in the stimulation of both muscarinic and nicotinic receptors through excess actylcholine.

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16
Q

What is the treatment for Organophosphate poisoning?

A

Treatment involves immediate administration of atropine, and ventilation/intubation to avoid respiratory failure.

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17
Q

What are the symptoms of acetylcholinesterase inhibitor poisoning (eg. organophosphates)?

Hint: Think DUMB BLESS

A
  • Diarrhea
  • Urination
  • Miosis
  • Bradycardia
  • Bronchoconstriction
  • Lacrimation
  • Excitation (muscle and CNS)
  • Salivation
  • Sweating
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18
Q

What are the direct muscarinic receptor antagonists? (These are anticholinergic or parasympatholytic drugs).

A
  • Atropine
  • Tiotropium bromide
  • Scopolamine
  • Oxybutinin, Tolterodine
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19
Q

What are the uses of Atropine?

A
  • Mydriasis for retinal exam
  • Relaxation of GI tract and bladder
  • Antidote for cholinergic crisis
  • Pre-surgery to decrease secretions
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20
Q

What are the adverse effects of Atropine?

A

Anticholinergic effects:

  • blurry vision
  • constipation
  • decreased peristalsis
  • decreased secretions
  • difficulty urinating
  • fever
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21
Q

What is Scopolamine used for therapeutically?

A

Motion sickness, often used transdermally as a patch

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22
Q

What are potential adverse effects of Scopolamine? More or less side effects than Atropine?

A

Can inhibit short-term memory d/t CNS effects.

More CNS effects than Atropine (limits it’s use because this causes more side effects)

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23
Q

Devil’s Breath or Angel’s Trumpet is a flower with similar properties to scopolamine. What are its effects?

A
  • Lose free will, feel like a zombie
  • Truth telling
  • Respiratory problems
  • Death at high doses
24
Q

What are the uses of Tiotropium bromide? What is it used in conjunction with?

A

Bronchodilator (inhaler) use for COPD. Generally used daily in conjunction with a short acting beta agonist (SABA) and possibly a LABA.

25
Q

Adverse efffect of Tiotropium bromide?

A

Dry mouth

26
Q

What are the uses of Oxybuynin and Tolterodine?

A

Used to relax an overactive/spastic bladder (enuresis), both in children and elderly. Also can be used for neurogenic causes.

27
Q

What are the side effects and contraindications for Oxybutynin and Tolterodine?

A
  • blurred vision from mydriasis
  • decreased perspiration
  • overheating

C/I: Don’t use if person is constipated

28
Q

What is an example of an indirect anticholinergic (blocks ACh release)?

A

Botulinum toxin

29
Q

What are the uses of Botulinum toxin?

A

Cosmetic: Prevents muscle contraction and therefore helps to prevent wrinkles

Therapeutic:

  • Cerebral palsy
  • Hyperhydrosis (decreases sweating through decreased cholinergic stimulation to muscarinic sweat receptors
  • Migraines or nerve pain
  • Torticollis
  • Tourettes syndrome (decreases vocal tics)
30
Q

What are potential adverse effects of Botulinum toxin?

A

Paralysis of unintended areas, difficulty swallowing, difficulty blinking, dry eyes, etc…

31
Q

Describe the flow chart (overarching categories) for drugs affecting the sympathetic nervous system.

A
32
Q

What are examples of sympathetic nervous system direct agonists? (Agonists to adrenergic receptors)

A
  • Epinephrine
  • Oxymetazoline
  • Phenylephrine
  • Albuterol, Salbutamol
  • Salmeterol
33
Q

What is the main therapeutic use of epinephrine as a drug? Adverse effects?

A

Treatment of anaphylactic shock.

Adverse effects:

  • Anxiety
  • Arrhythmias
  • Hypertension
  • Tremor
34
Q

What are the uses of Oxymetazoline and what are potential adverse effects?

A

Uses: Nasal decongestant

Adverse effects: Rebound congestion from overuse

35
Q

Is Oxymetazoline more selective for alpha or beta receptors?

A

More selective for alpha than beta receptors (specific for vasoconstrictive effects).

36
Q

What are the uses of Phenylephrine?

A

Oral administration as a nasal decongestant, or can also be used as intranasal spray.

Also can be used in eyedrops as treatment for conjunctivitis by causing pupillary dilation - mydriasis

37
Q

What are the adverse effects of Phenylephrine? What is one benefit compared to Oxymetazoline?

A

Cardiovascular with systemic/oral use can cause increased blood pressure and overall vasoconstriction.

Oral use does not cause rebound nasal congestion.

38
Q

What are the uses of Albuterol and Salbutamol? Adverse effects?

A

Uses: Bronchodilation; Short acting and used for acute asthma attacks or situation prevention (exercise or allergies)

Adverse effects: Hypotension, tachycardia, tremor

39
Q

What are the uses and possible adverse effects of Salmeterol?

A

Uses: Asthma (bronchodilator), Chronic obstructive pulmonary disease (COPD)

Adverse effects: Use of salmeterol without the concurrent use of an inhaled corticosteroid can predispose individual to greater chance of life threatening asthma attack.

40
Q

Albuterol, Salbutamol and Salmeterol are selective for which receptor? What is the benefit of this?

A

Receptor selectivity for beta-2 allows greater specificity to the lungs, without as many cardiovascular effects as when both beta-1 and beta-2 receptors are stimulated with non-selective agents.

41
Q

What is the duration of Salmeterol?

A

Salmeterol is a “long-acting beta agonist (LABA)” with a duration of approx 8 hours. It is dosed daily as a preventative/therpeutic measure for COPD and asthma (only with concurrent use of an inhaled corticosteroid).

42
Q

What are the main examples of sympathetic nervous system Indirect Agonists (Increase release of NE/E and/or prevent reuptake)?

A
  • Methylphenidate
  • Cocaine
  • Tyramine
43
Q

What are the uses of methylphenidate? What is the mechanism of action?

A

Uses: Attention Deficit Hyperactivity Disorder (ADHD), Narcolepsy.

Mechanism of action: Blocks reuptake of both NE and dopamine, and also increases their release.

44
Q

What are some potential adverse effects of methylphenidate?

A
  • Adrenergic side effects
  • Anxiety
  • Insomnia
  • Palpitations
  • Sexual dysfunction
  • Sudden cardiac death
  • Urinary retention
45
Q

What are some benefits and concerns about methylphenidate?

A

The drug is considered non-addictive in ADHD patients, but is considered addictive to many people in the general population.

Increased risk of sudden cardiac death is a concern, but the drug does show itself to be 65-80% effective in achieving a symptom reduction of 50% or greater.

46
Q

What are some mixed action sympathetic agonists? (Increase release and agonist to adrenergic receptors)

A
  • Amphetamine
  • Ephedrine and Pseudoephedrine
47
Q

What are the uses of Amphetamine? Adverse effects?

A

Uses: ADHD and narcolepsy

Adverse effects: hypertension, anxiety

48
Q

What actions does amphetamine have on neurotransmitters?

A

Amphetamines have action on increasing E, NE and dopamine.

49
Q

What are the four types of direct antagonists to adrenergic receptors?

A
  • Alpha – 1 Blockers
  • Alpha and beta blockers
  • Non selective beta blocker
  • Cardioselective beta blocker
50
Q

What are the Alpha1 blockers?

A

Prazosin, Terazosin, Doxazosin

51
Q

What are the uses of the Alpha 1 blockers (prazosin, terazosin, doxazosin)?

A

Uses:

  • Benign prostatic hyperplasia (blocks alpha 1 receptors in the prostate and bladder neck, improving urine flow)
  • Hypertension
52
Q

What are the adverse effects of Alpha 1 blockers? Cautions?

A

Adverse effects:

  • Orthostatic hypotension (prevents vasoconstriction)
  • Nasal congestion (potential d/t less vasoconstriction)

Cautions:

  • Interactions with alcohol, other antihypertensive drugs and diuretics because they can all decrease blood pressure
53
Q

What is an example of an alpha and beta blocker? What is its receptor profile for antagonism?

A

Labetolol

Selective alpha 1 antagonism and non selective beta antagonism

54
Q

What are the uses and adverse effects of Labetolol?

A

Uses – Hypertension

Adverse effects – Nausea, dizziness, stuffy nose

55
Q

What are non-selective beta blockers?

A

Propranolol, Timolol

56
Q

What are the uses for non-selective beta blockers (Propranolol and Timolol)?

A
  • Adrenergic induced arrhythmias
  • Chronic angina
  • Glaucoma (Timolol topically in eye)
  • Hypertension
  • Migraines (blocks vasodilation in brain)
57
Q
A

Adverse effects – slow heart rate (bradycardia), hypotension, bronchoconstriction

Special Notes – Timolol is used topically in the eye for glaucoma. Non-selective beta blockers should not be used in asthma

Pharmacology (5 decks)

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