Autonomic Pharmacology - An Overview Flashcards

1
Q

What type of drug is hexamethonium for neuronal nicotinic receptors?

A

Non-competitive antagonist

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2
Q

How many transmembrane segments are muscarinic receptors made of?

A

7

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3
Q

How many subtypes of muscarinic receptors are there?

A

5

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4
Q

Which muscarinic receptors are important peripherally?

A
  • M1
  • M2
  • M3
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5
Q

What effects do muscarinic agonists have?

A
  • Decreased heart rate
  • Smooth muscle contracts
  • Exocrine glands secrete (eg. sweat, salivation, etc.)
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6
Q

Adverse effects of muscarinic poisoning by an agonist

A
  • Bradycardia and vasodilation = falling BP
  • Increased motility, bronchoconstriction, pupillary constriction
  • Salivation, lacrimation, airway secretions
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7
Q

Treatment of muscarinic poisoning

A

Atropine (muscarinic antagonist)

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8
Q

What is pilocarpine used to treat and how is it administered?

A
  • Glaucoma
  • Topical to the eye
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9
Q

Pilocarpine mechanism of action

A
  • Works on M3 receptors
  • Improves aqueous humor drainage
  • Drops intraocular pressure
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10
Q

3 non-specific muscarinic antagonists

A
  • Atropine
  • Hyoscine
  • Cyclopentolate
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11
Q

Clinical uses of antimuscarinic drugs

A
  • Asthma
  • Bradycardia
  • Decrease secretions and AchEI side effects during surgery
  • Dilate pupils
  • Urinary incontinence
  • Motion sickness
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12
Q

5 main sub-types of adrenoreceptors and what they do

A
  • α1 = contract smooth muscle
  • α2 = pre-synaptic auto-inhibition, vasoconstriction, central inhibition of sympathetic outflow
  • β1 = increase heart rate + contractility
  • β2 = relax smooth muscle
  • β3 = relax bladder smooth muscle, stimulate lipolysis
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13
Q

Main uses of α-adrenoreceptor agonists (which receptor and drug)

A
  • Vasoconstrictors with local anaesthetics (α1, (nor)adrenaline)
  • Nasal decongestants (α1, phenylephrine)
  • Hypertension (α2)
  • Facial erythema in rosacea (α2, brimonidine)
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14
Q

Main uses of α-adrenoreceptor antagonists (which receptor and drug)

A
  • Hypertension (α2, doxazosin)
  • Benign prostatic hyperplasia (α1, tamsulosin)
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15
Q

Main uses of β-adrenoreceptor agonists (which receptor and drug)

A
  • Cardiogenic shock (β1, adrenaline or dobutamine)
  • Anaphylactic shock (adrenaline)
  • Asthma (β2, salbutamol)
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16
Q

Main Uses of β-adrenoreceptor Antagonists

A
  • Angina, cardiac arrhythmias
  • Hypertension
  • Anxiety states
  • (Chronic) heart failure
  • Glaucoma
17
Q

What is the main mechanism for terminating actions of noradrenaline?

A
  • Noradrenaline transporter
  • Na+, Cl- and noradrenaline cotransported
18
Q

What does the noradrenaline transporter enhance?

A

Effects of sympathetic activity

19
Q

What is the noradrenaline transporter inhibited by?

A
  • Cocaine
  • Tricyclic antidepressants (desipramine)
20
Q

What does desipramine have its major effects on?

A

CNS

21
Q

Adverse effects of desipramine

A
  • Tachycardia
  • Dysrhythmia
22
Q

Effects of cocaine

A
  • Euphoria and excitement (CNS action)
  • Tachycardia
  • Increased blood pressure
23
Q

What process do mono-amine oxidase inhibitors block?

A

Breakdown of noradrenaline

24
Q

What is the clinical use for mono-amine oxidase inhibitors?

A

Antidepressants

25
Q

Adverse effects of mono-amine oxidase inhibitors

A
  • Postural hypotension
  • Weight gain
  • Restlessness
  • Insomnia
  • Cheese reaction
26
Q

Examples of mono-amine oxidase inhibitors

A
  • Phenelzine
  • Tranylcypromine
  • Iproniazid
  • Moclobemide
27
Q

Mechanism of action of indirectly acting sympathetic amines

A
  • Transported into nerve terminals by noradrenaline transporters
  • Displace noradrenaline
28
Q

Effects of indirectly acting sympathetic amines

A
  • Bronchodilation
  • Vasoconstriction
  • Positive inotropy
  • Raised blood pressure
29
Q

Examples of indirectly acting sympathetic amines

A
  • Amphetamine
  • Ephedrine
  • Tyramine