Block Four Flashcards
(284 cards)
1
Q
What are examples of CNS drugs?
A
- Antipsychotics
- Antidepressants
- Anxiolytics
- Hypnotics
- Sedatives
- Antiparkinsonian
- Anticonvulsants
- Muscle relaxants
- CNS stimulants
2
Q
What are examples of neurotransmitters?
A
- Noradrenaline
- Dopamine
- Acetylcholine
- 5-hydroxytryptamine (5-HT, serotonin)
- Gamma-amino butyric acid (GABA)
- Glutamate (an excitatory amino acid)
3
Q
What is the brain region that noradrenaline works on?
A
Hypothalamus, reticular activating system
4
Q
What is the brain function of noradrenaline?
A
- Arousal
- Sleep
- Mood
- Appetite
- Hormone release
- Body temperature
5
Q
What are the receptors of noradrenaline?
A
Adrenergic receptors:
- Alpha 1 and 2
- Beta 1, 2, and 3
6
Q
What are possible illnesses caused by noradrenaline?
A
- Depression,
- Insomnia
- Eating disorders
- Narcolepsy
- ADHD
7
Q
What is the brain region that dopamine works on?
A
- Hypothalamus
- Extrapyramidal pathway
- Limbic system
- Chemoreceptor trigger zone (CTZ)
8
Q
What is the brain function of dopamine?
A
- Skeletal muscle movement
- Behaviour
- Emesis
- Hormone release
9
Q
What are the receptors of dopamine?
A
D1, D2, D3, D4 and D5
10
Q
What are possible illnesses caused by dopamine?
A
- Parkinson’s disease
- Schizophrenia
- Aberrant behaviour
- Psychoses
11
Q
What is the brain region that 5-hydroxytryptamine (5-HT, serotonin) works on?
A
- Hypothalamus
- Reticular activating system
12
Q
What is the brain function of 5-hydroxytryptamine (5-HT, serotonin)?
A
- Pain transmission
- Emesis
13
Q
What are the receptors of 5-hydroxytryptamine (5-HT, serotonin)?
A
- 5-HT1
- 5-HT2
- 5-HT3
- 5-HT4
14
Q
What are possible illnesses caused by 5-hydroxytryptamine (5-HT, serotonin)?
A
- Depression
- ADHD
- Headaches
- Eating disorders
- Insomnia
15
Q
What is the brain region that acetylcholine works on?
A
- Cerebral cortex
- Thalamocortical tracts
- Pyramidal pathway
- Reticular activating system
16
Q
What is the brain function of acetylcholine?
A
- Cognition
- Skeletal muscle movement
- Memory
- Consciousness
17
Q
What are the receptors of acetylcholine?
A
- Muscarinic
- Nicotinic
18
Q
What are possible illnesses caused by acetylcholine?
A
- Parkinson’s disease
- Dementia
- Alzheimer’s disease
19
Q
What is the brain region that gamma-amino butyric acid (GABA) works on?
A
All regions
20
Q
What is the brain function of gamma-amino butyric acid (GABA)?
A
- Motor control
- Memory
- Consciousness
21
Q
What are the receptors of gamma-amino butyric acid (GABA)?
A
- GABAa
- GABAb
22
Q
What are possible illnesses caused by gamma-amino butyric acid (GABA)?
A
- Anxiety
- Insomnia
- Aberrant behaviour
- Epilepsy
23
Q
What are drugs that enhance the actions of GABA?
A
- Benzodiazepines
- Barbiturates
24
Q
What is glutamate?
A
An excitatory amino acid (EAA)
25
Where is glutamate found?
In all regions of the brain
26
What are illnesses associated with glutamate?
- Alzheimer’s
- Huntington’s
- Epilepsy
- Stroke
27
What are opioids?
Neurotransmitters
28
Where are opioid receptors?
Present in the CNS and in the body
29
How do neurotransmission disease occur?
From either too much neurotransmission or not enough
30
What is too much neurotransmission?
Occur when neurons are excited all the time without appropriate stimuli e.g. seizure disorders
31
What is too little neurotransmission?
Occur when too few neurotransmitter molecules are binding to postsynaptic receptors e.g. depression, Parkinsonism
32
What are the two main ways drugs can help chemical imbalances?
- Enhance the activity of he neurotransmitter
| - Block the neurotransmitter actions
33
What are examples of SSRIs?
- Citalopram
- Fluoxetine
- Sertraline
34
What is an example of a RIMAs?
Moclobemide
35
What is an example of a MAOIs?
Tranylcypromine
36
What are drugs used to treat pathological depressive states?
- Irreversible monoamine oxidase inhibitors (MAOIs)
- Reversible monoamine oxidase inhibitors (RIMAs)
- Tricyclic antidepressants (TCAs)
- Selective serotonin reuptake inhibitors (SSRIs)
37
What is an example of an irreversible monoamine oxidase inhibitors (MAOIs)?
Tranylcypromine
38
What are side effects of irreversible monoamine oxidase inhibitors (MAOIs)?
Adrenergic and anticholinergic adverse effects
39
How do irreversible monoamine oxidase inhibitors (MAOIs) work?
Inhibit enzyme monoamine oxidase which normally breaks down noradrenaline, therefore increasing level of noradrenaline
40
What are key concerns around using irreversible monoamine oxidase inhibitors (MAOIs)?
- Dietary restrictions
- Risk of a hypertensive crisis
- Adrenergic adverse effects
- Drug interactions
41
What is an example of a reversible monoamine oxidase inhibitors (RIMAs)?
Moclobemide
42
How do reversible monoamine oxidase inhibitors (RIMAs) work?
Inhibit enzyme monoamine oxidase which normally breaks down noradrenaline, therefore increasing level of noradrenaline
43
What the is advantage that RIMAs have over MAOIs?
Less adverse effects since they are selective and have reversible effects
44
What are the different types of monoamine oxidase enzymes?
- MAO-A
| - MAO-B
45
What are examples of tricyclic antidepressants (TCAs)?
- Amitriptyline
| - Nortriptyline
46
How do tricyclic antidepressants (TCAs) work?
Non-selectively block re-uptake of neurotransmitters
47
What are adverse effects of tricyclic antidepressants (TCAs)?
- Anti-muscarinic (anticholinergic) effects
- Antihistamine effects
- Antiadrenergic effects
- Cardiac dysrhythmias
48
What are key concerns when using tricyclic antidepressants (TCAs)?
- Overdose
- Compliance
- Hypertensive crisis
- Adverse effects
49
Why are SSRIs the main group of antidepressants used?
Due to the milder adverse effect and fewer cardiovascular and antimuscarinic adverse effects
50
What are common adverse effects of SSRIs?
- Nausea
- Nervousness
- Insomnia
- Transient headache
- Diarrhoea
- Sexual dysfunction
- Amenorrhoea
51
What is serotonin syndrome?
Drug induced too much serotonin
52
How does serotonin syndrome occur
When a person takes SSRI and another serotonin elevating drug
53
What is the mode of action of serotonin and noradrenaline re-uptake inhibitors (SNRIs)?
Selectively blocks serotonin and noradrenaline re-uptake
54
What is an example of an serotonin and noradrenaline re-uptake inhibitor (SNRIs)?
Venlafaxine
55
What is the mode of action of tetracyclic antidepressants?
Monoamine re-uptake inhibitor
56
What is the mode of action of noradrenaline re-uptake inhibitors (NRI)?
Selectively blocks the re-uptake of noradrenaline
57
What do noradrenergic and specific serotonergic antidepressant (NaSSA) do?
Increase central noradrenergic and serotonergic neurotransmission
58
What are key clinical consideration with the use of antidepressant?
- Suicide potential
- Time lag before therapeutic effect
- Delayed clearance from the body
- Drug interactions
- May precipitate mania
- Withdrawal symptoms
59
What are examples of first generation (typical) antipsychotics?
- Chlorpromazine
- Haloperidol
- Pericyazine
60
What are examples of second generation (atypical) antipsychotics?
- Clozapine
- Olanzapine
- Quetiapine
- Risperidone
61
What is the definition of psychosis?
Disordered thinking and disturbed emotional tone
62
What is the definition of neurosis?
Normal thinking patterns but disturbed emotional tone
63
When are drugs given for Schizophrenia?
In both the acute phase and for prevention of relapse
64
What are symptoms of Schizophrenia?
- Disordered associations in thinking
- Blunting or loss of affect or feeling
- Accessory symptoms
65
What are the different types of Schizophrenia?
- Positive type
| - Negative type
66
What are characteristics of positive Schizophrenia?
- Delusions
- Hallucinations
- Incongruous behaviour
67
What are characteristics of negative Schizophrenia?
- Apathy
- Lack of motivation
- Social withdrawal
68
Are positive or negative symptoms more responsive to antipsychotics?
Positive type
69
What drug is more effective for negative type of antipsychotics?
Clozapine
70
What is treatment for Schizophrenia?
Combined use of antipsychotic drugs with psychotherapeutic interventions
71
What is organic psychosis?
When psychosis is a symptoms of an organic problem e.g. brain tumour
72
How to treat organic psychosis?
Antipsychotic drugs are used to control agitation, confusion, hallucinations
73
How to treat manic phase of bipolar depression?
Antipsychotic drugs are used in conjunction with lithium or other mood stabilisers
74
What is the mode of action of antipsychotic drugs?
Inhibit dopamine mediated transmission in specific areas of the brain
75
What are the four dopamine pathways?
- Mesolimbic dopamine pathway
- Mesocortical dopamine pathway
- Nigrostratial dopamine pathway
- Tuberoinfundibular dopamine pathway
76
What is the mesolimbic dopamine pathway?
- Involved in emotional disorders, delusions, thought disorders and auditory hallucinations
- Hyperactivity causes positive symptoms of psychosis
77
How do drugs cause a therapeutic effect on the mesolimbic dopamine pathway?
Reduce dopamine levels
78
What is the mesocortical dopamine pathway?
Low levels of dopamine related activities linked to negative symptoms of schizophrenia
79
How do drugs cause a therapeutic effect on the mesocortical dopamine pathway?
Antipsychotic medications are effective for positive symptoms but less effective with negative symptoms
80
What is the nigrostratial dopamine pathway?
- Controls motor movements and forms part of the extrapyramidal nervous system
- Low levels of dopamine in this pathway results in movement disorders e.g. Parkinson's
81
What is the tuberoinfundibular dopamine pathway?
- Dopamine-related activity here inhibits prolactin release
| - Dopamine antagonist action causes increased prolactin or hyperprolactinaemia?
82
What are symptoms of hyperprolactinaemia?
- Amenorrhoea
- Galactorhoea
- Infertility
- Loss of libido
- Erectile dysfunction
83
What does M1 blockade cause?
Typical antimuscarinic and anticholinergic adverse effects
84
What does H1 blockade cause?
- Weight gain
| - Drowsiness
85
What does A1 blockade cause?
Postural hypotension
86
What are common adverse effects of antipsychotics?
```
Main ones are extrapyramidal adverse effects:
- Akathisia
- Dystonia
- Oculogyric crisis
- Parkinsonism
- Tardive dyskinesia
Also:
- Typical antimuscarinic
- Postural hypotension
- Sedation
- Endocrine effects
- Prolonged Q-T interval
```
87
What is a rare adverse effect of antipsychotics?
Neuroleptic malignant syndrome (NMS)
88
What is a specific adverse effect of Clozapine?
Agranulocytosis
89
What are specific adverse effects of Chlorpromazine?
- Cholestatic jaundice
- Impaired temperature
regulation
- Photosensitivity
- Contact dermatitis
- Ocular changes
- Lowering of seizure threshold
90
What are adverse effects of atypical antipsychotics?
- Acute severe hypertension
- Weigh gain
- Diabetes
- Agranulocytosis
- Hepatic adverse effects
91
What are key concerns with antipsychotics?
- Managing the adverse effects (tardive dyskinesia is irreversible)
- Compliance
- Limited response
- Recurrence
- Cardiovascular health risks including stroke
92
What are examples of common mood stabilisers?
- Lithium carbonate
- Sodium valproate
- Carbamazepine
- Lamotrigine
- Antipyschotics
93
What do therapeutic drugs for bipolar disorder do?
- Treat both acute depressive and acute manic episodes
- Prevent manic or depressive symptoms
- Avoid increasing the risk of mood cycling
94
What is lithium carbonate?
- Takes a week before therapeutic level is reached
| - Narrow therapeutic range, needs monitoring
95
What are symptoms of lithium overdose/toxicity?
1) slight nervousness
2) Abdominal pain, anorexia, nausea, vomiting, mild diarrhoea
3) Giddiness, tremor, ataxia, slurred speech, depression
4) Oliguria, hypovolemia, convulsive movements, coma
5) Potentially fatal outcome – cardiovascular/respiratory failure
96
What are contraindications for lithium carbonate?
- Pregnancy
- Lactation
- Cardiac insufficiency
- Renal insufficiency
97
What are causes of lithium poisoning?
- Changes in salt intake
- Excessive sodium loss
- Excessive dose of lithium
98
How does salt affect lithium?
High salt decreases the effectiveness of lithium
99
What is treatment for lithium overdose?
- Withdrawal of drug
- Increased water and sodium intake
- Restoring fluid and electrolyte imbalances
100
How does sodium valproate work?
- Works the same as lithium against a manic phase
| - More rapid response
101
How does lamotrigine work?
- Prevents manic and depressive relapse
| - Cannot treat acute manic episode
102
How does carbamazepine work?
Has some anti-manic effect
103
What do benzodiazepines act on and do?
- Act on receptors in CNS
| - Activates gamma-aminobutyric acid (GABA) which is an inhibitory neurotransmitter
104
What are common anxiolytics and hypnotics?
- Triazolam
- Midazolam
- Diazepam
- Clonazepam
- Zopiclone
105
How does half-life affect use of triazolam?
- Short half-life is good for the initiation of sleep
| - Longer half-life of approximately 8 hours is used for early morning awakening
106
How does half-life affect use of midazolam?
Very short half-life used to sedate patients
107
What is clonazepam used for?
Anticonvulsants (used for status epileptics)
108
What is diazepam used for?
- Anticonvulsants (used for status epileptics)
| - Muscle relaxant
109
What are key concerns around using anxiolytics and hypnotics?
- Misuse
- Rebound
- Psychotic episodes
- Sedation
- Defects in long term memory
- Deaths when mixed with alcohol
- Ability to cross placenta
110
What is zopiclone?
- Short-acting hypnotic
| - Less adverse effects (physical dependency, rebound insomnia, and tolerance)
111
What are drugs used to treat Parkinson’s disease?
- Levodopa (L-Dopa)
- Sinemet and Madopar
- Pramipexole
- Ropinirole
- Selegiline
- Entacapone
- Nenzatropine
112
How does Parkinson's disease occur?
Decreased number of cells producing dopamine causing low dopamine activity
113
How does drug-induced Parkinsonism occur?
Blockage of the dopamine receptor sites in the substantia nigra causing low dopamine activity
114
What drugs are used for Parkinson's disease only?
- Levodopa
- Sinemet and Madopar
- Pramipexole
- Ropinirole
- Selegiline
- Entacapone
115
What is levodopa (L-Dopa)?
- Precursor of dopamine and can pass through the blood–brain barrier
- Once in brain levodopa converts to dopamine
116
What are adverse effects of levodopa (L-Dopa)?
- GI upset
- Cardiovascular effects
- Psychological effects
117
What can reduce the effects of levodopa (L-Dopa)?
Vitamin B6
118
What does Sinemet (L-Dopa + carbidopa) and Madopar (L-Dopa + benserazide) do?
- Levodopa is quickly metabolised
- An enzyme inhibitor (either carbidopa or benserazide) added to slow metabolism
- Allows more levodopa to enter brain
119
What does entacapone do?
Drug that prevents peripheral conversion of levodopa to dopamine, allowing more levodopa to reach the brain
120
What does selegiline do?
Drug that inhibits the breakdown of dopamine
121
What does pramipexole and ropinirole do?
Uses different mechanisms to mediate dopamine transmission to prevent tolerance
122
What is a drug used for both Parkinson's disease and drug-induced Parkinsonism?
Benzatropine
123
What are adverse effects of Benzatropine?
- Dry mouth
- Blurred vision
- Constipation
- Urine retention
- Tachycardia
124
What are examples of drugs for epilepsy/anticonvulsants?
- Phenytoin
- Carbamazepine
- Sodium valproate
- Diazepam
- Lamotrigine
- Clonazepam
- Gabapentin
125
What are common dose related adverse effects of starting anticonvulsants?
- Sedation
- Tiredness
- Dizziness
- Confusion
- Slurred speech
- Ataxia
- Tremor
- Decreased co-ordination
- Dry mouth
- GI upsets
126
What are the main issues around anticonvulsants?
- Most drugs are suspected teratogens
- Drug-drug interactions
- Increased risk of suicidality
127
What are the different modes of actions of anticonvulsants?
- Affecting the movement of sodium ions across the membrane
- Stabilising the nerve membranes directly
- Affecting the activity of Gamma-amino butyric acid (GABA)
128
What are examples of drugs that affect movement of sodium ions across the membrane
- Phenytoin
| - Carbamazepine
129
What are examples of drugs that affect the activity of Gamma-amino butyric acid (GABA)?
- Clonazepam
| - Diazepam
130
What is the combined action of sodium valproate?
- Triggers release of GABA
- Inhibits sodium channels
- Block subtype of glutamate receptors
131
What is the combined action of lamotrigine?
- Inhibit passage of sodium through voltage sensitive channels
- Reduce the release of glutamate
132
What are characteristics of sodium valproate?
- First line choice for generalised epilepsies
- Drug-drug interactions are common
- Can be used alone or in combination
133
What are characteristics of carbamazepine?
- First line choice for partial epilepsies
- Also used for generalised and mixed epilepsies
- Common drug-drug interactions
- Can be used during pregnancy
134
What are characteristics of lamotrigine?
- Alternative first line choice for partial epilepsies
- Useful for most forms of epilepsy
- Can be used during pregnancy
135
What are characteristics of phenytoin?
- Narrow therapeutic range
- Treats most forms of epilepsy
- Not used widely due to risk of long-term toxicity and narrow therapeutic range
- Specific adverse effects of overgrown gum tissue, slurred speech and liver damage
136
What are characteristics of gabapentin?
Treatment of partial seizures and neuropathic pain
137
What are the characteristics of clonazepam when treating epilepsy?
Treatment for refractory (non-respondent) absence or myoclonic seizures
138
What are the characteristics of diazepam when treating epilepsy?
Treatment for status epilepticus
139
What are the principles of anticonvulsant therapy?
- Use mono therapy if possible
- Start with low dose and increase slowly until therapeutic effect achieved or until adverse effects prevent further increases
- Routine monitoring
- Abrupt discontinuance may induce status epilepticus
- Lower risk of drug-drug interactions
- Lower adverse effects
- Easier monitoring
- Improved compliance
- Lower teratogenicity
140
What are common drugs used for general anaesthesia?
- Propofol (IV)
- Thiopental sodium (IV)
- Isoflurane (inhaled liquid)
- Sevoflurane (inhaled liquid)
- Nitrous oxide (inhaled gas)
141
What are common drugs used for local anaesthesia?
```
Amides:
- Bupivacaine
- Lidocaine (lignocaine)
Esters:
- Tetracaine
```
142
How do general anaesthetics work?
- Depress the CNS
- Ease pain
- Cause loss of consciousness
- Used for major surgery
143
How do local anaesthetics work?
- Block pain at administration site
- Maintain consciousness
- Used for dental procedures and minor surgery
144
What is the difference between analgesics and anaesthetics?
- Analgesics control pain without loss of sensation
| - Anaesthetics prevent pain by losing sensation
145
What are the stages of anaesthesia?
1) Analgesia or induction
2) Excitement or delirium
3) Surgical
4) Medullary paralysis
146
What occurs in the stage of 'analgesia or induction'?
- Auditory and visual hallucinations
- Speech difficulty
- Smell and pain sensations are lost
147
What occurs in the stage of 'excitement or delirium'?
Loss of consciousness
148
What occurs in the stage of 'surgical'?
- Surgery performed
- Muscle relaxation
- Anaesthesia deepens, respirations become shallow, increased respiratory rate
149
What occurs in the stage of 'medullary paralysis'?
- Toxic stage of anaesthesia
| - Respirations are lost and circulatory collapse occurs
150
How are inhalation anaesthetics absorbed?
Through the lungs into plasma
151
What are adverse effects of inhaled liquid anaesthetics such as isoflurane and sevoflurane?
- Cardiac and respiratory effects
- Cough
- Hypotension
- Arrhythmias
152
What are common adverse effects of nitrous oxide?
- Nausea
- Vomiting
- Reflux
153
How is nitrous oxide best used?
- IV anaesthetic
- Used for analgesic properties
- Not used for anaesthetic properties
154
What are characteristics of propofol?
- Can be used for the induction or maintenance of general anaesthesia
- Rapid onset of action and loss of unconsciousness can occur within 10 seconds
155
What are characteristics of thiopental sodium?
- IV anaesthetic
- Used for induction of anaesthesia
- Potent respiratory depressants
156
What is the mode of action of local anaesthetics?
- Blocks pain transmission between the PNS (nociceptors) and CNS
- Blocks movement of sodium ions through channels in plasma membrane
157
What is lidocaine?
- Effective for producing analgesia
| - Rapid onset and moderate duration of action
158
What is bupivacaine?
- Given during childbirth
- Slow onset
- Long duration
159
What is tetracaine?
Topical preparations
160
What are problems to be aware of when using local anaesthetics?
- Can cause abnormal heartbeat
- Epidural anaesthetic could introduce foreign substances into the CSF
- Overdose can lead to adverse effects (insomnia, visual and auditory disturbances, convulsions, shivering and CNS depression)
- Allergic reactions
161
What are common anaesthetics/analgesics used during childbirth?
- 50% nitrous oxide and 50% oxygen
- Fentanyl
- Bupivicaine
- Pethidine
162
What are characteristics of 50% nitrous oxide and 50% oxygen?
- Rapid onset of action
| - Gas
163
What can prolonged exposure to 50% nitrous oxide and 50% oxygen cause?
- Bone marrow depression
- Teratogenicity
- Increased incidence of spontaneous abortion
164
What is epidural?
A combination of the following drugs are injected into the epidural space (between 1st and 2nd lumbar spine):
- Bupivacaine (local anaesthetic)
- Fentanyl (analgesic)
- Pethidine (analgesic)
165
When is epidural analgesia/anaesthesia is commonly used?
- Prolonged or ineffective labour/contractions
- Where there is a need for rotation/positioning/breech
- Forceps delivery
166
What are potential adverse reactions or complications of epidural anaesthesia?
- Hypotension
- Ineffective labour/reduced effectiveness of voluntary effort – need for forceps
- Post dural puncture headache
- Urine retention
- Nerve root damage
- Paraplegia
167
What are common antiemetic drugs?
- Prochlorperazine
- Promethazine
- Metoclopramide
- Hyoscine
- Ondansetron
168
How do antiemetics work?
By blocking specific receptors, stopping the neurotransmitters from binding to the receptors and hence stopping the vomiting or CTZ from being stimulated
169
What are the five categories of antiemetic drugs?
- Antihistamines (H1-receptor antagonists)
- Antimuscarinics (Muscarinic receptor antagonists)
- Dopamine antagonists (D2-receptor antagonists)
- Phenothiazines
- Serotonin blockers (5-HT3 receptor antagonists)
170
What is an examples of an antihistamine?
Promethazine
171
What is the mode of action of antihistamines (Promethazine)?
Bind to the H1-receptor in the vomiting and vestibular centres, block histamine from binding and hence inhibit or reduce vomiting
172
What are antihistamines (Promethazine) particularly effective for?
- Motion sickness
| - Vertigo
173
What is the main adverse effect of antihistamines (Promethazine)?
Sedation
174
What is an examples of a dopamine antagonists?
Metoclopramide
175
What are dopamine antagonists (Metoclopramide) particularly effective for?
Vomiting caused:
- Delayed gastric emptying
- Infection-induced
- Cytotoxic-induced
- Drug-induced vomiting
176
What are side effects of dopamine antagonists (Metoclopramide)?
- Sedation
- Diarrhoea
- Extrapyramidal effects
177
What is an example of phenothiazines?
Prochlorperazine
178
What are phenothiazines (Prochlorperazine) particularly effective for?
Vomiting caused by:
- Radiation
- Severe morning sickness
- Uraemia
- Infection-induced
- Cytotoxic-induced
- Drug-induced vomiting
179
What are adverse effects of phenothiazines (Prochlorperazine)?
- Sedation
| - Extrapyramidal effects
180
What is an example of antimuscarinics?
Hyoscine
181
What are antimuscarinics (Hyoscine) used for?
Motion sickness
182
What are adverse effects of antimuscarinics (Hyoscine)?
- Dilated pupils
- Tachycardia
- Drowsiness
- Dry mouth
183
What is an example of serotonin blockers?
Ondansetron
184
What are serotonin blockers (Ondansetron) particularly effective for?
- Nausea and vomiting induced by chemotherapeutic drugs
| - Post-operative nausea
185
What are adverse effects of serotonin blockers (Ondansetron)?
- Constipation
- Headaches
- Gastrointestinal upsets
186
What are the main functions of the GI tract?
- Gastric secretion
- The motility of the bowel and expulsion of the faeces
- Vomiting (emesis)
- Formation and excretion of bile
187
What are common ulcer healing drugs?
- H2-receptor antagonists
- Proton-pump inhibitors
- Antacids (weak bases)
- Misoprostol – prostaglandin analogue
- Antimuscarinics
- Antibiotics necessary for eradicating H. pylori
188
What is gastrin?
- A hormone
| - Acts on the gastrin receptor to stimulate production and release of HCl
189
What is acetylcholine?
- A neurotransmitter
| - Released from nerve cells and acts on muscarinic receptors to stimulate production and release of HCl
190
What is histamine?
- A local hormone
| - Released from mast cells and acts on H2- receptors to stimulate production and release of HCl
191
What is prostaglandins roles in the stomach?
- Inhibit gastric acid production
| - Promote formation of the protective mucosal layer
192
What is the mode of action of prostaglandins?
- Binds to the prostaglandin receptor in the parietal cell and inhibit production and release of HCl
- Binds to the PG receptor in the mucous cell to stimulate the release of mucous and bicarbonate ions
193
What are drugs used to treat H. pylori.?
```
Antibiotics such as:
- Clarithromycin
- Metronidazole
- Amoxicillin
Needs a cocktail of medications (three to four antibiotics and ulcer healing drugs)
```
194
What types of drugs decrease gastric acid secretion?
- Proton pump inhibitors
- H2-receptor antagonists
- Anticholinergics
195
What is an example of a proton pump inhibitor?
Omeprazole
196
What are proton pump inhibitors (omeprazole) used for?
- Gastro- oesophageal reflux disease
- NSAID-associated (treatment and prophylaxis)
- H.pylori associated duodenal or gastric ulcers
- Gastro- duodenal erosions
- Zollinger–Ellison syndrome
- Severe reflux oesophagitis
197
What is the mode of actions of proton pump inhibitors (omeprazole)?
Binds to the proton pump and basically stops the secretion of HCl
198
What are adverse effects of proton pump inhibitors (omeprazole)?
- Headaches
- Rashes
- Diarrhoea
- Dizziness
- Mental confusion
- Pain in muscles and joints
- Increased risk of infection
199
What are examples of H2-receptor antagonists?
- Cimetidine
| - Ranitidine
200
What is the mode of actions of H2-receptor antagonists (cimetidine and ranitidine)?
Block the H2-receptors on the parietal cell, stop histamine from binding, and thus stop or decrease the secretion of HCl
201
What are adverse effects cimetidine?
- Headaches
- Dizziness
- Skin rash
- Pruritis
- Diarrhoea or constipation
- Depression
- Mental confusion
- Galactorrhoea
- Reduced sperm count
202
What can cimetidine affect?
- Alters oestrogen metabolism in men which can lead to gynaecomastia
- Affects liver metabolism of many drugs, increasing ther effects
203
What is the half life of omeprazole?
Short, 1 hour
204
What is the half life of cimetidine?
Short, 2 hours
205
What is the half life of ranitidine?
Longer than cimetidine, 3 hours
206
Does ranitidine have more or less adverse effects than cimetidine?
- Fewer adverse effects than cimetidine
| - Less likely to have an effect on liver, fewer drug-drug interactions
207
What are contraindications of H2-receptor antagonists (cimetidine and ranitidine)?
- Pregnancy or lactating mothers
| - Renal impairment (reduced dose)
208
When should cimetidine be administered?
Given with meals and at bedtime
209
When should most H2-receptor antagonists be administered?
Once per day, generally at bedtime
210
What are important rules when administering antacids?
- Do not administer antacids within 1 hour before or after histamine blocking drugs
- When IV administered do not mix with other drugs
211
What is the mode of action of anticholinergics?
Blocks the M1-receptor on the parietal cell, stops acetylcholine from binding, and thus inhibits the production of HCl
212
What are adverse effects of anticholinergics?
Typical anticholinergic adverse effects
213
When should anticholinergics be taken?
Before meals to decrease acid secretion that occurs with eating
214
What are antacids?
Drugs that are used to neutralise gastric acid secretions
215
When should antacids be taken?
1 and 3 hours after meals and at bedtime for a period of 6 weeks
216
What are alginates?
- A mix of calcium and sodium bicarbonate
| - Relieves pain from reflux
217
How do alginates work?
Sodium alginate reacts with acids and produces a viscous jelly which floats on aqueous solutions, thereby providing a barrier to reduce reflux
218
What antacids are used during pregnancy?
- Non-pharmacological measures plus minimal use of safe antacids
- Liquid antacids due to rapid onset
219
What are care concerns when using antacids?
- Administer antacids no sooner than 1 hour after enteric coated preparations are given
- Oral medications should not be taken within 1-2 hours of the time the antacid is taken
- Check drug interactions
- Monitor for constipation or diarrhoea
- Monitor for electrolyte imbalance
220
What are drugs that protect the mucosal layer?
- Bismuth compounds
- Sucralfate
- Misoprostol
221
How does bismuth compounds work?
Bismuth compounds stimulate mucosal bicarbonate and prostaglandin production
222
What are adverse effects of bismuth compounds?
- Nausea
- Vomiting
- Blackening of the tongue and faeces
223
How does sucralfate work?
- Binds to proteins in the ulcer base and forms a protective barrier against bile, acid and pepsin
- Also stimulates secretion of mucous, bicarbonate and prostaglandins
224
How do antacids affect sucralfate?
Antacids decrease the effects of sucralfate
225
What are adverse effects of sucralfate?
- Dizziness
- Nausea
- Constipation
- Dry mouth
- Vomiting
- Headache
- Rashes
226
What is misoprostol used for?
- Prophylaxis
| - Treatment of NSAID-induced ulcers
227
What are adverse effects of misoprostol?
- Diarrhoea
- Abdominal pain
- Cramping
228
What is acid aspiration syndrome?
- Regurgitation and aspiration of the stomach contents into the respiratory tract
- Complication of general anaesthesia
229
What drugs can be given to help prevent acid aspiration syndrome?
- H2-antagonist (e.g. ranitidine) given 1-2 hours before to increase pH and lower volume of gastric fluid
- To directly affect the gastric fluid already produced, an antacid such as sodium citrate is given in addition to or instead
230
What are some common antimotility drugs?
- Loperamide
- Diphenoxylate and atropine
- Codeine
231
What is the mode of action of antimotility drugs?
Stimulate the opioid receptors in the bowel to act on the nerves of the intestine, thereby inhibit peristalsis hence reducing motility and decreasing fluid secretion
232
What is the mode of action of antimotility drugs?
Stimulate the opioid receptors in the bowel to act on the nerves of the intestine, thereby inhibit peristalsis hence reducing motility and decreasing fluid secretion
233
What are adverse effects of antimotility drugs?
- Nausea
- Vomiting
- Abdominal cramps
- Drowsiness
- Potentially constipation
234
When should clinical improvement be seen after administering antimotility drugs?
In 1-3 hours
235
What is the usual line of treatment when treating constipation?
1) Bulking agents
2) Osmotic laxatives
3) Stimulants
4) Faecal softeners
236
What is an example of a bulk forming laxative?
Psyllium
237
What do bulk forming laxatives do?
Absorb water, swell and increase the bulk of the stool which stimulates normal peristalsis
238
When should clinical improvement be seen after administering bulk forming laxatives?
12–72 hours
239
What can bulk forming laxatives cause?
- Flatulence
| - Abdominal pain
240
What are examples of osmotic laxatives?
- Lactulose
| - Macrogols
241
How do osmotic laxatives work?
Reduce absorption of water which softens the stool and increases its bulk, stimulating peristalsis
242
What are adverse effects of osmotic laxatives?
- Bloating
- Flatulence
- Abdominal pain/cramping
- Diarrhoea
243
When should clinical improvement be seen after administering osmotic laxatives?
24-48 hours
244
What are examples of stimulant laxatives?
- Bisacodyl
| - Sennoside B b
245
How do stimulant laxatives work?
Stimulate peristalsis and promote defaecation
246
When should clinical improvement be seen after administering stimulant laxatives?
6-12 hours
247
What are adverse effects of stimulant laxatives?
- Abdominal pain
- Cramping
- Bloating
- Diarrhea
- Nausea
- Vomiting
- Electrolyte disturbances (with prolonged use)
248
What can senna products cause?
Red or yellow discolouration of urine and faeces
249
What are examples of faecal softeners?
Docusate sodium
250
How do faecal softeners work?
Lubricate and soften stool
251
What are adverse effects of faecal softeners?
- Abdominal cramps
- Diarrhoea
- Nausea
- Rash
252
What do look out for when laxatives are being used?
- That the laxative is suitable for the age and general condition of the patient
- Bulk forming laxative: follow with another 250 ml fluid to prevent GI obstruction
- Assess effectiveness of laxative
- In general, avoid the use of stimulant laxatives in the elderly or pregnant women (senna may cause contractions in the third semester)
253
What is the chemical imbalance of depression?
- Low serotonin activity
| - Low noradrenaline activity
254
What is the chemical imbalance of psychoses/schizophrenia?
High dopamine activity
255
What is the chemical imbalance of Parkinson’s disease?
- Low dopamine activity
| - High acetylcholine activity
256
What is the chemical imbalance of anxiety/insomnia?
- High glutamate activity
- Low GABA activity
- Low serotonin activity
257
What is the chemical imbalance of epilepsy?
- High glutamate activity
| - Low GABA activity
258
What is the chemical imbalance of bipolar?
Low noradrenaline OR high adrenaline activity
259
What are drug interactions to look out for with tricyclic antidepressants (TCAs)?
- Other antidepressants
- Antimuscarinics
- Hypnotics
- Anxiolytics
- Anaesthetics
- Antihypertensives
- Caution with anticonvulsants
260
What are drug interactions to look out for with MAOIs?
- Sympathomimetics
- Other antidepressants
- Antihistamines
- Hypnotics
- Anxiolytics
261
What are drug interactions to look out for with SSRIs?
- Other antidepressants
- Anticonvulsants
- Antipsychotics
- Other drugs that increase serotonin (St John's Wort, tramadol)
262
What are properties of citalopram?
- Less drug interactions than other SSRIs
- May cause less nausea than other SSRIs
- Short half-life - caution with discontinuation syndrome
263
What are properties of sertraline?
- Intermediate risk of drug interactions
| - Short half-life - caution with discontinuation syndrome
264
What are properties of fluoxetine?
- Significant number of important drug interactions
- Long half-life (one to two weeks) means slower reversal of adverse effects but discontinuation syndrome unlikely
- Requirement for longer washout period if switching to an alternative antidepressant
- Inhibits hepatic enzyme
265
What is an effect of venlafaxine?
Can increase blood pressure
266
What is discontinuation syndrome?
Occurs when suddenly stopping a drug
267
What is the mode of action of venlafaxine?
Inhibits re-uptake of noradrenaline and serotonin
268
What is the mode of action of fluoxetine?
Selectively inhibits re-uptake of serotonin
269
What are extrapyramidal effects?
ADOPT:
- Akathisia - restlessness, fidgety
- Dystonia – muscle spasms, wry neck, torticollis
- Oculogyric crisis - upward rolling of eye balls
- Parkinsonism - fine tremors, bradykinesia, drooling, shuffling gait
- Tardive dyskinesia - irreversible, occurs with long term use, stereotyped involuntary movements
270
What is the time frame of adverse effects?
Initial adverse effects (hours, days):
- Sedation, postural hypotension, anticholinergic, acute dystonic reactions
Initial weeks (months):
- Akathisia, Parkinsonism, weight gain, endocrine effects
After longer term treatment:
- Tardive dyskinesia (irreversible)
271
What needs to be monitored when using clozapine?
- Blood pressure
- Glucose levels
- Weight
- Constipation
- Lipids
272
What are therapeutic uses of anxiolytics benzodiazepines?
Anxiety and panic disorders
273
What are therapeutic uses of hypnotics and sedative benzodiazepines?
Sleeping disorders
274
What are therapeutic uses of muscle
| relaxants and anticonvulsants benzodiazepines?
Muscle spasms and seizure disorders
275
What are key concerns of benzodiazepines?
- Adverse effects (CNS depression)
- Drug Interactions
- Tolerance and dependence
- Withdrawal symptoms - CNS stimulation
- Can cross placenta and into breast milk
276
What is partial epilepsy?
- Involves a cluster of neurons
| - Present with unilateral symptoms
277
What is generalised epilepsy?
Involves both hemispheres
278
What is status epilepticus?
```
- Continuous series of seizures without
reawakening, may get permanent brain
damage
- Can result from abruptly discontinuing an
anticonvulsant
```
279
What does benztropine do for Parkinson's?
Tries to lower levels of acetylcholine activity
280
What medications are given post surgery?
- Antiemetic
| - Pain relief
281
What are adverse effects of general anaesthetics?
- CV – drop in blood pressure
- CNS – respiratory depression
- Liver – “Halothane Hepatitis”
- Uterus – relaxes uterine muscles
- Malignant hyperthermia – rare
- CTZ - nausea/vomiting
282
What monitoring and care are associated with general
| and local anaesthetics?
- Make sure vital signs and consciousness are monitored
before, during and after
- Use opioids sparingly while client is attempting to
regain consciousness
- Monitor vital signs and conscious state regularly
- Evaluate local anaesthetised areas for sensation and
movement
283
What are the antiemetic receptors?
- Muscarinic
- H1
- D2
- 5HT3
284
What is the first line treatment for diarrhoea?
- Rehydration
| - Electrolyte replacement therapy
