ANS pharmacology 2

Question 1

○ Propranolol

Answer 1

adrenoceptor antagonist
§ Binds and inhibits B1 and B2
§ Inhibits B1

Question 2

propranolol effects

Answer 2

□ Decreases heard rate and contractility
□ Reduces cardiac output
□ Decrease blood pressure

Question 3

propranolol used for

Answer 3

□ Used to treat

® Angina, hypertension, arrythmias, post-myocardial infarction

Question 4

propanolol side effects

Answer 4

□ May exacerbate bronchoconstriction in asthma
□ May impair circulation in peripheral arterial disease
□ May worsen glycaemia control in diabetic patients

Question 5

○ Metoprolol

Answer 5

§ Binds and inhibits B1 adrenoceptors

§ Reduces cardiac output and lowers blood pressure

Question 6

metoprolol used for

Answer 6

§ Used to treat

□ Angina, hypertension, arrythmias, post myocardial infarction

Question 7

metoprolol side effects

Answer 7

§ Doesn’t block b2 at usual doses
□ May be safer than propranolol in people treated for cardiovascular disease that also suffer for asthma, peripheral vascular disease or diabetes
§ But may block B2 at high doses
□ All beta adrenoceptor antagonists in patients where B2 receptor blockage is problematic

Question 8

Drugs affecting muscarinic cholinoceptors

Answer 8

• Available drugs often lack selectivity

minimal drugs available

Question 9

2 muscarinic cholinoceptor agonists

Answer 9

pilocarpine

atropine

Question 10

• Pilocarpine

Answer 10

○ Muscarinic cholinoceptor agonist

Question 11

pilocarpine used for

Answer 11

○ Delivered topically to the eye
§ Activate M3 receptors on the surface of the constrictor pupillae muscle
§ Constrict the pupil and promote the drainage of aqueous humous
§ Reduce intraocular pressure
○ Occasionally used clinically to treat glaucoma
§ Not first or second line treatment

Question 12

• Atropine

Answer 12

○ Blocks all muscarinic cholinoceptor subtypes

antagonist

Question 13

atropine effects

Answer 13

§ Dries up secretions
□ Saliva, sweat, tears, gut and lung
§ Inhibits smooth muscle contraction
□ Gut, lungs and eye
§ Increases heart rate
○ Also crosses into CNS to block muscarinic receptors
§ Excitatory effects (restlessness, hyperactivity, increase body temp)

Question 14

atropine used for

Answer 14

○ Atropine is a frontline therapy for poisoning with anticholinesterase agents (pesticides, war gasses)
§ Blocks muscarinic cholinoceptor mediated side effects in CNS and PNS

Question 15

• Tiotropium

Answer 15

○ Used for chonic obstrictive pumonary disease (COPD)

○ Dilates the airways and reduces mucus secretion

Question 16

• Tropicamide

Answer 16

○ Used for retinal examination

○ Relaxes ciliary muscle and iris sphincter

Question 17

• Solifenacin

Answer 17

○ Used for urinary incontinence

○ Relaxes the smooth muscle of the bladder, which increases bladder capacity

Question 18

2 drugs inhibiting removal of NT

Answer 18

amphetamine and neostigmine

Question 19

§ Neostigmine

Answer 19

□ Blocks acetyl choline metabolism

Question 20

reuptake of noradrenaline

Answer 20

Most released NA undergoes neuronal reuptake, (by NA transporter, NAT)

Question 21

after reuptake of noradrenlaine

Answer 21

§ transported into vesicles by vesicular monoamine transporter, VMAT
§ Or inactivated by monoamine oxidase, MAO

Question 22

2 inhibitors of NA uptake and metabolism

Answer 22

amphetamine and pseudoephedrine

Question 23

amphetamine

Answer 23

• induces reverse operation of NAT

○ Inhibits VMAT and MAO

Question 24

amphetamine effects

Answer 24

○ May cause vasoconstriction (a-AR) and increase in heart rate and contraction (b-AR)
§ Not used clinically for these effects on the autonomic nervous system
§ Used clinically for CNS effects
□ In children with ADHD

Question 25

- Pseudoephedrine

Answer 25

○ Also increases NA release from adrenergic nerves ○ Use a nasal decongestant is now restricted § Can be converted into methamphetamine

Question 26

Released Ach is metabolised by

Answer 26

enzymes AChE | § Acetylcholinesterase

Question 27

- Anticholinesterase

Answer 27

○ Inhibitor of AchE | ○ Ach not metabolised and accumulates

Question 28

- Anticholinesterase causes

Answer 28

○ Mimics stimulation of the parasympathetic nervous system | § Glandular secretion, smooth muscle contraction, slowing of HR

Question 29

long actin anticholinesterases

Answer 29

war gasses/poisons | DUMBBELSS symptoms

Question 30

DUMBBELSS

Answer 30

``` ® Diarrhoea ® Urination ® Miosis/muscle weakness ® Bronchorrhea/bronchoconstriction ® Bradycardia ® Emesis ® Lacrimation ® Salivation/sweating ® Seizures ```

Question 31

killer Bs

Answer 31

® Excessive bronchochorrhea, bronchoconstriction or bradycardia can all cause death

Question 32

therapy for long acting aticholinesterases

Answer 32

□ Atropine is a frontline therapy ® Because it can block the effects of Ach ® Can cross blood brain barrier and prevent CNS effects

Question 33

medium acting anticholinesterases

Answer 33

□ Hours | □ Neostigmine

Question 34

short acting anticholinesterases

Answer 34

□ Minutes | □ Edrophonium

Question 35

clinical use of anticholinesterases in myasthenia graves

Answer 35

□ Autoimmune disease in which body attacks nicotinic receptors on skeletal muscle □ Extreme skeletal muscle weakness □ Loss of sensitivity to Ach can be overcome but increasing the concentration of Ach in the neuromuscular juction

Question 36

diagnosis of myasthenia graves

Answer 36

® Edrophonium ◊ Used for diagnosis of myasthenia gravis ◊ When administered, it causes an increase in muscle strength in people with myasthenia gravis } Will not cause an increase in muscle strength in people without disease

Question 37

chronic treatment of myasthenia graves

Answer 37

® Neostigmine ◊ Less useful because it needs to be given by injection ® Pyridostigmine ◊ Orally active