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CNS Drugs Flashcards

(129 cards)

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1
Q

Hyoscine hydrobromide drug class

A

Muscarinic antagonist

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2
Q

Hyoscine hydrobromide indications

A

Motion sickness

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3
Q

Hyoscine hydrobromide mechanism of action

A

It competitively blocks Muscarinic acetylcholine receptors in the vestibular nuclei and chemoreceptor trigger zone.

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4
Q

Hyoscine hydrobromide ADR

A 
Sedation 
Memory problems
Glaucoma
Dry mouth
Constipation
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5
Q

Cyclizine drug class

A

Histamine 1 receptor antagonists

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6
Q

Cyclizine indications

A

Motion sickness

Morning sickness

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7
Q

Cyclizine mechanism of action

A

It acts centrally on the vestibular nuclei and inhibits histaminergic signals from the vestibular system to the chemoreceptor trigger zone in the medulla.

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8
Q

Cyclizine ADR

A 
Sedation 
Excitation 
Dry mouth 
Constipation 
Urinary retention 
Cardiac toxicity - long QT interval
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9
Q

Cyclizine caution

A

Elderly

Children

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10
Q

Ondansetron drug class

A

5-HT3 receptor antagonist

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11
Q

Ondansetron indications

A

Nausea and vomiting

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12
Q

Ondansetron mechanism of action

A

It can centrally on the chemoreceptor trigger zone and peripherally to reduce GI motility and secretions

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13
Q

Ondansetron ADR

A 
Constipation 
Headache
Elevated liver enzymes 
Long QT syndrome 
Extra-pyramidal effects - Dystonia, Parkinsonism
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14
Q

D2 receptor antagonists examples

A

Metoclopramide
Domperidone
Haloperidol

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15
Q

D2 receptor antagonist indications

A

Nausea and vomiting
Motion sickness
Vertigo

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16
Q

D2 receptor antagonists mechanism of action

A

It increases acetylcholine at Muscarinic receptors in the gut. It promotes gastric emptying by increasing tone of lower oesophageal sphincter, tone of gastric contractions and decreasing the tone of the pylorus.

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17
Q

Metoclopramide ADR

A

Galactorrhoea
Extra-pyramidal effects - Dystonia and Parkinsonism
Sedation
Hypotension

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18
Q

Domperidone ADR

A

Sudden cardiac death due to long QT and VT

Galactorrhoea

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19
Q

Dexamethasone drug class

A

Corticosteriod

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20
Q

Dexamethasone indications

A

Nausea and vomiting

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21
Q

Dexamethasone mechanism of action

A

May act on the chemoreceptor tigger zone

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22
Q

Dexamethasone ADR

A

Insomnia
Increased appetite
Increased blood sugar

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23
Q

Nabilone drug class

A

Cannabinoid

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24
Q

Nabilone ADR

A

Dizziness

Drowsiness

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25
Aprepitant drug class
Neurokinin 1 receptor antagonist
26
Aprepitant indications
Nausea and vomiting
27
Aprepitant mechanism of action
It prevents the action of substance P at the chemoreceptor trigger zone and in peripheral nerves. It boosts the effects of 5HT3 receptor antagonists.
28
Aprepitant ADR
Headache Diarrhoea Constipation Stevens-Johnson syndrome - skin reaction
29
First line drug for motion sickness
Hyoscine hydrobromide
30
D2 receptor antagonist cautions
Obstruction | Risk of perforation
31
First line for Morning sickness in pregnancy
H1 receptor antagonist or D2 receptor antagonist
32
First line for emesis in chemotherapy
Dexamethasone then Ondansetron
33
Nociception definition
The non-conscious neural traffic due to trauma or potential trauma to tissue
34
Pain definition
A complex, unpleasant awareness of sensation modified by experience, expectation, immediate context and culture.
35
Describe the pain reflex ?
``` Nociceptors stimulated Release of substance P and glutamate Afferent nerve stimulated Fibres decussate Action potential ascends Synapse in thalamus Projects to post central gyrus ```
36
Opioid mechanism of action
Agonist binds which leads to a decreased in cAMP. This causes an efflux of potassium. The membrane then becomes hyper polarised. There is decreased production of substance P and GABA which increases dopamine release causing a euphoric effect.
37
What are some strong opioid agonist ?
Morphine Fentanyl Heroin Oxycodone
38
What are some moderate opioid agonist ?
Codeine
39
What is a partial opioid agonist ?
Buprenorphine
40
What is a opioid antagonist ?
Naloxone
41
Which receptor does Morphine have a strong affinity to ?
Mu receptors
42
Morphine ADR
``` Respiratory depression Emesis GI tract side effects Cardiovascular side effects Miosis Histamine release ```
43
Potency and affinity of Fentanyl compared to morphine
More potent | Higher affinity
44
Morphine actions
Analgesia | Euphoria
45
Fentanyl actions
Analgesia | Anaesthetic
46
Fentanyl ADR
Respiratory depression Constipation Vomiting
47
Potency of Codeine compared to morphine
Less potent
48
Codeine actions
Mild to moderate analgesia | Cough depressant
49
Codeine ADR
Constipation | Respiratory depression
50
Buprenorphine affinity compared to morphine
Very high so not easily displaced
51
Buprenorphine actions
Moderate to severe pain | Opioid addiction treatment
52
Buprenorphine ADR
Respiratory depression Low BP Nausea Dizziness
53
Naloxone affinity compared to morphine and Buprenorphine
Greater than morphine but less than Buprenorphine
54
Overdose effects
``` Dependence Vomiting Constipation Hypotension Bradycardia Histamine release Miosis Drowsiness Respiratory depression ```
55
Opioid contraindications
``` Hepatic failure Acute respiratory distress Comatose Head injuries Raised ICP ```
56
What does PGE2 contribute to ?
Regulation of acid secretion in parietal cells
57
What does prostacyclin - PGI2 - contribute to ?
Maintenance of blood flow and mucosal repair
58
What can enhance prostanoids ?
Autacoids such as bradykinin and histamine
59
What can a disturbance of prostanoids lead to ?
Hypertension MI Stoke
60
What homeostatic functions does COX-1 do ?
GI protection Platelet aggregation Vascular resistance
61
What homeostatic functions does COX-2 do ?
Renal homeostasis Tissue repair and healing Reproduction Inhibition of platelet aggregation
62
How do NSAIDs have analgesic effects ?
It blocks PGE2 which reduces peripheral pain fibre sensitivity. This can result in decreased PGE2 synthesis in the dorsal horn causing a decrease in neurotransmitter release. This decreases excitability of neurons in the pain relay pathway.
63
How do NSAIDs have an anti-inflammatory effect ?
NSAIDs reduce production of prostaglandins released at the site of injury. This decreases vasodilation and capillary permeability reducing local swelling.
64
How do NSAIDs have an anti-pyretic effect ?
NSAIDs inhibit the hypothalamic COX-2 where cytokine induced prostaglandin synthesis is elevated results in a reduction in temperature.
65
What has COX-1 selectivity ?
Aspirin
66
Order of increasing COX-2 selectivity (least to most)
``` Ibuprofen Naproxen Diclofenac Celecoxib Etoricoxib ```
67
NSAIDs ADR
``` Dyspepsia Nausea Peptic ulceration Bleeding Perforation Decreased GFR ```
68
NSAIDs cautions
``` Elderly Prolonged use Smoking Alcohol History of peptic ulceration H.Pylori infection Heart failure Underlying CKD ```
69
NSAIDs DDI
``` Aspirin Glucocorticoid steriods Anti-coagulants ACEi ARB Diuretics Warfarin - increased risk of bleeding Methotrexate ```
70
NSAIDs indications
Inflammatory conditions Osteoarthritis Postoperative pain Menorrhagia
71
Paracetamol indications
Mild to moderate pain | Fever
72
Paracetamol mechanism of action
COX-2 selective inhibition in the CNS which decreases pain signals to higher centres
73
Paracetamol overdose effects
Nausea Vomiting Abdominal pain Liver damage
74
Paracetamol overdose treatment
Activated charcoal is overdose is very recently Give N-acetylcysteine
75
Seizure definition
A transient occurrence of signs and symptoms due to abnormal electrical activity in the brain, leading to a disturbance of consciousness, behaviour, emotion, motor function or sensation.
76
Most important excitatory neurotransmitter and the receptor is acts on ?
Glutamate on the NMDA receptor
77
Most important inhibitory neurotransmitter and the receptor it acts on ?
GABA on GABA alpha receptors
78
What can cause a seizure ?
Loss of inhibitory signals or too strong an excitatory ones | This imbalance can happen in any point in the brain and local changes can lead to generalised effects.
79
What can cause an imbalance in the brain to cause a seizure ?
Genetic differences in brain chemistry / receptor structure Drugs Drug withdrawal Strokes and tumours
80
Signs and symptoms of seizures
Shaking and jerking Loss of consciousness Tongue biting Possible aura prior
81
Epilepsy definition
Epilepsy is a tendency towards recurrent seizures unprovoked by a systemic or neurological insult.
82
Potential stimuli for seizures
``` Photogenic Musicogenic Thinking Eating Hot water immersion Reading Orgasm Movement ```
83
Where do generalised seizures originate ?
Originate at a point and rapidly engage both hemispheres
84
Where do focal seizures originate ?
Originate within networks limited to one hemisphere. May be discretely localised or more widely distributed
85
What is a provoked seizure ?
``` Seizures that result from another medical condition such as : Drug use or withdrawal Alcohol withdrawal Head trauma Metabolic disturbances CNS infections ```
86
How to manage a seizure under 5 mins ?
Start a timer and usually seizures will self-terminate without use of drugs
87
What is status epilepticus ?
A seizure lasting more than 5 minutes or more, or multiple seizures without a complete recovery between them.
88
Drug management for Status epilepticus
0-5 mins - Full dose of benzodiazepine 0-15 mins - 2nd full dose of benzodiazepine 15-45 mins - phenytoin or levetiracetam 45 mins + - thiopentone / anaesthesia
89
Investigations for a diagnosis of epilepsy
EEG- record the electrical pattern of activity in the brain | Imaging - MRI
90
Benzodiazepine drug class
GABA alpha agonist
91
Benzodiazepine indications
Termination of a seizure
92
Benzodiazepine mechanism of action
There is increased chloride conductance resulting in more negative resting potential so the action potential is less likely to fire.
93
Benzodiazepine examples
IV lorazepam Diazepam rectally Buccal or intranasal midazolam
94
Carbamazepine drug class
Sodium channel blocker anti-epileptic drug
95
Carbamazepine indication
Epilepsy
96
Carbamazepine mechanism of action
Blocking sodium channels in the central neurones which slows recovery of neurones from inactive to closed states. This reduces neuronal transmission.
97
Carbamazepine ADR
Suicidal thoughts Joint pain Bone marrow failure
98
Phenytoin drug class
Sodium channel blocker anti - epileptic drug
99
Phenytoin indications
Epilepsy | Mainly used in status epilepticus
100
Phenytoin cautions
Exhibits zero order kinetics so there must be care in adjusting doses
101
Phenytoin ADR
Bone marrow supression Hypotension Arrhythmia with IV use
102
Sodium valproate drug class
Anti - epileptic
103
Sodium valproate indications
1st line for generalised epilepsies
104
Sodium valproate ADR
Liver failure Pancreatitis Lethargy
105
Sodium valproate mechanism of action
Mixed GABA alpha effects and sodium channel blockade
106
Lamotrigine drug class
Sodium channel blocker anti - epileptic drugs
107
Lamotrigine indications
Focal epilepsy | Used for generalised epilepsy when sodium valproate is contraindicated
108
Levetiracetam indications
Focal seizures | Generalised seizures
109
Positives of levetiracetam
Safe in pregnancy
110
Levetiracetam mechanism of action
It stops the release of neurotransmitters into synapse and reduces neuronal activity.
111
Levetiracetam drug class
Synaptic vesicle glycoprotein binder - AED
112
Anti-epileptic drug ADR
``` Tiredness Drowsiness Nausea Vomiting Mood changes Suicidal ideation Osteoporosis ```
113
AED DDI
Warfarin Alcohol Decreases effectiveness of oral contraceptive pill and antibiotics CYP inducers - phenytoin, carbamazepine and barbiturates CYP inhibitors - valproate
114
Dopamine receptor agonist examples
Levodopa Co-careldopa Amantadine
115
What is special about co-careldopa ?
Levodopa is used in combination with a peripheral dopa decarboxylase inhibitor. This reduces the dose and side effects. It also increases levodopa reaching the brain.
116
Dopamine receptor agonist indications
Parkinson’s disease
117
Levodopa side effects
Nausea Hypotension Psychosis Tachycardia
118
Levodopa mechanism of action
Levodopa is a prodrug that is converted to dopamine by DOPA decarboxylase. It crosses the blood brain barrier and is decarboxylase to dopamine where it stimulates dopaminergic receptors.
119
Levodopa DDI
Pyridoxine ( vitamin B6 ) increases peripheral breakdown of levodopa. MAOI and levodopa increase risk of hypertensive crisis. Many anti-psychotic drugs block dopamine receptors and have Parkinsonism as a side effect.
120
COMT inhibitor examples
Entacapone | Opicapone
121
COMT inhibitors mechanism of action
No therapeutic effect alone and used alongside levodopa. They reduce the breakdown of levodopa so prolong motor response to levodopa.
122
COMT inhibitor indications
Used alongside levodopa for Parkinson’s disease
123
Examples of impulse control disorders
Pathological gambling Hyper-sexuality Compulsive shopping Punding
124
Dopamine receptor agonist ADR
``` Sedation Hallucinations Confusion Nausea Hypotension ```
125
MAOI examples
Selegiline | Rasagiline
126
MAOI actions
Can be used alone Prolongs the action of levodopa Smooths out motor response
127
Anti-cholinergics examples
Orphenadrine | Procyclidine
128
Anti-cholinergic ADR
Confusion | Drowsiness
129
Anti-cholinergic positive
Treats the tremor

CPT Drugs (9 decks)

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