ocular pharmacology Flashcards

1
Q

what is the mode of action of most drugs ?

A

the mode of action of most drugs is to inhibit or facilitate neural processes such as action potential transmission or synaptic transmission

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2
Q

what are agonists ?

A

drugs that enhance the effectiveness of neuron

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3
Q

what are antagonists ?

A

suppress specific neuron

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4
Q

where do most ocular drugs work?

A

most ocular drugs use affect nerve/muscle synapses

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5
Q

what is skeletal muscle innervated by?

A
  • innervated by the somatic nervous system
  • ( single motor neuron )
  • releases ACH
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6
Q

what is smooth muscle innervated by ?

A
  • innervated by the autonomic nervous system
  • ( 2 neuron single chain ) separated by a ganglion
  • sympathetic ( close to spinal cord ) and parasympathetic ( close to the effector)
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7
Q

what does sympathetic system release?

A
  • post ganglionic neuron release nor-adrenaline at the effector ( alpha or beta receptors)
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8
Q

what does parasympathetic release?

A
  • post ganglionic fibre releases ACH at the effector ( muscarinic or nicotinic receptors )
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9
Q

explain chemical synapses ?

A
  • depolarisation of synaptic terminal
  • influx of calcium
  • migration of vesicles containing neurotransmitters to migrate to presynaptic membrane
  • fusion of vesicle with presynaptic membrane
  • release of transmitter by exocytosis
  • diffusion of transmitter across cleft down the concentration gradient
  • binding of transmitter to postsynaptic receptors
  • change in postsynaptic membrane permeability leading to IPSPs( open Cl or K you get hyper polarisation) or EPSPs( open Na) depending on ion channel opened
  • inactivation of transmitter ( enzymatic, reuptake into presynaptic neuron)
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10
Q

what are some types of neurotransmitters ?

A
  • Noradrenaline
  • Ach
  • Dopamine
  • Histamine
  • GABA
  • they all have their own set of neurotransmitter receptors
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11
Q

what is function of neurotransmitter receptors?

A

neurotransmitter receptors are important because its the receptors that determine which ions channels are open and shut in the posterior synaptic membrane

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12
Q

what are the 2 basic types of ACH receptors ?2

A
  • Ach can bind to
  • nicotinic - occurs at neuromuscular junction - open Na channels - therefore excitatory
  • muscarinic - open k and cl channels - therefore inhibitory
  • same neurotransmitter but 2 different effects depending on the receptor
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13
Q

what are the methods of transmitter inactivation ?

A
  • diffuse away
  • break it down with enzymes
    enzyme acts on Ach and splits into its components part which are re absorbed into presynaptic neuron
  • take it back up into presynaptic neuron
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14
Q

what enzyme destroys Nor-adrenaline?

A

monoamine oxidase- which is responsible for its reuptake in the presynaptic neuron

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15
Q

where can drug affect a neural and synaptic process?

A

drugs can affect any stage of the neural and synaptic process
1 - drug can affect synthesis of transmitters by stopping it or enhancing it
2- axonal transport -
3- storage of neurotransmitters in the vesicle
4- binding of neurotransmitter to postsynaptic membrane
5- conduction of action potential

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16
Q

what is the simplest drug to facilitate a synape?

A
  • the simplest drug to facilitate a synape would be to apply the neurotransmitter itself
  • this is rarely done as the body has mechanism for neutralising such transmitters
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17
Q

what is the first muscle that may be affected by drugs in the eye?

A
  • iris sphincter muscle
  • contraction causes pupil constriction ( miosis )
  • parasympathetic innervated -( from ciliary ganglion/ IIIrd nerve)
  • Muscarinic Ach receptor
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18
Q

what happens if you put pilocarpine in eye ?

A

binds to muscarinic receptors, acts as an Ach agonist activating Ach receptors and causing pupil constriction (miosis)

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19
Q

what happens if you put anti muscarinics in the eye ( e.g. atropine, tropicamide, cyclopentolate) ?

A

will block Ach receptors and result pupil dilation ( mydriasis )

20
Q

what happens to pupil diameter with age?

A
  • resting pupil diameter decreases with age due to a loss of sympathetic tone ( senile miosis )
  • this makes it harder for the old to read in lower light levels
21
Q

what is deadly nightshade ( atropa belladona ?

A

deadly night shade contains atropine which is an anti-muscarinic used by some women to dilate pupil, thus making them look younger

22
Q

what is atropine?

A
  • anti-muscarinic which binds to muscarinic receptors and stops ACH from acting on iris sphincter muscle and the pupils will dilate
23
Q

what happens when you put anticholinesterases ( eserine , physostigmine ) in the eye?

A

will enhance Ach levels and results in sphincter activation and pupil constriction by inactivating acetylcholinesterase

24
Q

what is iris dilator muscle ?

A
  • contraction causes pupil dilation ( mydriasis )
  • sympathetically innervated ( from superior cervical ganglion )
  • Alpha Nor-adrenalin receptors
25
how to activate iris dilator muscle which would cause it to contract which causes dilation ?
use phenylepinephrine which acts as a direct agonists Nor- adrenalin causing pupil dialation
26
how to cause the eye to dilate in the iris dilator muscle ?
use hydroxyamphetamine which acts by increasing the release of NA and hence also causes dilation
27
how to cause the eye to constrict in the iris dilator muscle?
applying alpha-adrenergic blockers, (e.g. thymoxamine ) causing constriction
28
what can you use cocaine for?
cocaine prevents the reuptake of NA and hence causes dilation
29
what is ciliary muscle?
- contraction results in accommodation - parasympathetic innervation ( from ciliary ganglion/IIIrd nerve) - muscarinic Ach receptors
30
how can accommodation be blocked?
- accommodation can be blocked ( cycloplegia ) by muscarinic receptor blockers such as atropine, cyclopentolate, scopolomine or tropicamide
31
what are the ocular skeletal muscle?
6 EOM orbicularis oculi levator palpebrae superioris - they can also be affected by drugs
32
what is botulinum toxin?
inhibits the release of Ach at skeletal neuromuscular junction. it can therefore be used to turn a muscle off
33
what is botulinum toxin used for ?
- alleviate squint - induce eye closure ( botulinum tarsorrhaphy ) - alleviate blepherospasm
34
what can some drugs interfere with ?
- some drugs can interfere with action potential transmission neuron and not affect muscle directly
35
what is action potential ?
``` thereshold depolarisation open Na channels large depolarisation Na channel shut k channel open re-polarisation of neuron retransmitted in neuron through local circuits ```
36
what do ocular anaesthetics work in the cornea?
most ocular topical anaesthetics (e.g. oxybuprocaine, amethocaine and lignocaine ) inhibit corneal sensory neurons by blocking sodium channels - neuron can't depolarise
37
what is Parkinson's disease caused by?
low levels of dopamine in the substantia nigra
38
why can't dopamine be used to treat Parkinson's ?
- it does not cross the blood-brain barrier | - L-dopa, a precursor to dopamine does
39
what can we use for Parkinson's?
- L-dopa, a precursor to dopamine which cross blood-brain barrier and reach substantia nigra
40
how to slow heart down ?
by using beta blockers | the NA receptors on the heart, thereby slowing it down
41
what are monoamines?
``` Noradrenaline dopamine serotonin - these are feel good transmitters - high levels are associated with feeling of well being - low levels= depression ```
42
how to alleviate depression ?
reuptake blockers for monoamines (e.g. prozack) | - raising level of monamine
43
what are the long term effect of drugs?
- if a system is deprived of neurotransmitter for an extended period, the number of receptors will increase ( up regulate)
44
what will happen due to high levels of transmitter?
- result in receptor down regulation | - as a result drugs will become less effective
45
what happens when you stop using a drug?
the number of receptors will be low, even if the body is now producing the right amount of transmitter