Pharmacology Flashcards
(153 cards)
1
Q
Which is the only antidepressant recommended in <18y? why?
A
Fluoxetine
Because of increase in suicidal thoughts in the others
2
Q
What are 4 classes of antidepressants?
A
SSRIs
SNRIs
MAOIs
TCAs
3
Q
Which of the following is not an SSRI:
citalopram, duloxetine, sertraline, paroxetine
A
duloxetine is an SNRI
4
Q
What does SNRI stand for
A
serotonin and noradrenaline reuptake inhibitor
5
Q
SEs SSRI
A
GI bleed, sexual dysfunction, hyponatraemia, increase in suicidal ideation, QT prolongation
6
Q
Any drug that increases the availability of serotonin can cause____?
A
serotonin syndrome
7
Q
Symptoms of serotonin syndrome
A
confusion
delirium
shivering
sweating
BP changes
myoclonus
8
Q
In which situations is serotonin syndrome likely to occur?
A
When initiating an antidepressant, increasing the dose, overdose, adding another AD or switching AD without allowing ‘washout period’ of the last one
9
Q
How can you reduce the risk of GI bleed in SSRI
A
if elderly taking NSAID/aspirin give PPI
10
Q
Which two SSRIs would be good for patients on a lot of medication?
A
Citalopram and sertraline have fewest interactions
11
Q
How should a patient starting an antidepressant be monitored?
A
Review every 1-2w at the start (1w if <30 or suicide risk). Wait at least 4w before deciding it isn’t working. If partial response, keep waiting for another 2-4 more weeks. See them every 2-4w in the first 3m.
If <30 or suicide risk- see frequently until the risk is no longer clinically significant.
12
Q
Name two SNRIs
A
venlafaxine, duloxetine
13
Q
Which SNRI has different side effects to SSRIs?
A
Venlafaxine
14
Q
What extra SEs does venlafaxine have?
A
BP changes, cardiotoxic in overdose
15
Q
How long should you remain on an antidepressant for?
A
about 6m after symptom resolution
16
Q
How are antidepressants metabolised
A
hepatic
17
Q
Can any antidepressants cause withdrawal symptoms?
A
Yes
18
Q
How should you come off antidepressants?
A
Taper over 2-4w
19
Q
What is the action of Mirtazapine?
A
Blocks presynaptic alpha 2 receptors which normally inhibit neurotransmitters via negative feedback. This increases monoamine output
20
Q
Side effects of mirtazipine
A
Dry mouth, drowsiness, wt gain
21
Q
Dothiepin, imipramine and lofepramine are what type of antidepressant?
A
TCA
22
Q
What type of antidepressant has the highest risk of overdose?
A
TCAs except lofepramine
23
Q
Mechanism of TCAs
A
Block monoamine reuptake (each to different extents)
24
Q
SEs TCAs
A
Anticholinergic, antiadrenergic, cardiac arrhythmias, seizures
hypotension, tachycardia, QTc prolongation
25
Which TCA has fewer side effects
Lofepramine, but rarely it causes hepatic toxicity
26
TCAs can be split into what two groups?
Sedating and non-sedating
27
Name some sedating TCA
amitriptyline, clomipramine, dosulepin, doxepin, mianserin, trazodone, trimipramine
28
Name some less sedating TCAs
Imipramine, lofepramine, nortriptyline.
29
Mechanism of MAOIs?
Inhibit breakdown of serotonin, and, to a lesser extent, noradrenaline.
30
Name two MAOIs
phenelzine, tranylcypromine
31
SEs MAOIs
Anticholinergic, antiadrenergic, tyramine reaction
Hypertensive crisis
32
What is a tyramine reaction (SE of MAOI)
HTN and throbbing headache if eat food with lots of tyramine- cheese and red wine. Occasionally fatal.
33
Treatment with _______ is associated with a higher risk of withdrawal effects compared with other antidepressants
Venlafaxine
34
What is the antidepressant general progression of treatment?
1. SSRI
2. Up dose
3. Switch to different SSRI or alternate antidepressant
4. Augment with antipsychotic/lithium etc
5. Combination therapy: Venlafaxine & Mirtazapine, or Olanzapine & Fluoxetine
35
Antipsychotics are split into which two categories?
Typical and atypical
36
Are typical or atypical antipsychotics first line?
Atypical
37
Benefit of atypical antipsychotics?
Fewer SEs and may be slightly better at treating negative Sx schizophrenia
38
Which is the most effective antipsychotic? But what are its negatives?
Clozapine
Significant SEs- agranulocytosis- requires regular monitoring (weekly for 18w, then fortnightly for 1y then monthly).
39
When do you prescribe clozapine?
when two antipsychotics have failed
40
Mechanism of action antipsychotics?
Reduce dopamine transmission (D2/D3)
Atypicals- antagonise 5HT2a receptors
Typicals- anticholingergic, antiadrenergic and antihistaminergic.
Unknown why these treat psychosis
May involve ventral striatum
41
antipsychotics route?
Normally oral, can be IM short acting, occasionally IV.
Some (flupenthixol, fluphenazine and risperidone) can be depot injections every 1-4w which improves adherence.
42
Would you use antipsychotics for behavioural disturbance in elderly?
No, risk stroke and reduce glycaemic control. Only one you'd use is risperidone short term.
43
Indications for antipsychotics?
Schizo
Mania
Psycotic depression
Violent/agitated behaviour (haloperidol usually)
Tourette's in lower doses
44
SEs typical antipsychotics
Antidopaminergic:
Movement: parkinsonism, akathisia, tardive dyskinesia, acute dystonic reactions (torticollis, increased tone, oculogyric crisis)
AND
Hyperprolactinaemia: galactorrhoea, breast cancer, amenorrhoea, sexual dysfunction
45
What is an oculogyric crisis?
Keep looking up involuntarily
46
What types of typical antipsychotics have slightly different SEs?
Phenothiazines- blood dyscrasias, retinal pigmentation, photosensitivity, cholestatic jaundice
47
What are the SEs of atypical antipsychotics?
Metabolic- wt gain, T2DM, dyslipidaemia
48
Which atypical antipsychotic has different profile of SEs?
Clozapine:
Nocturnal enuresis, constipation, salivation, BP changes, fever, nausea, seizures, agranulocytosis
49
What are the side effects of all antipsychotics?
C-CHANS
Cardiac (QT prolongation, arrhyth, 2x risk sudden cardiac death)
Anti-Cholinergic (dry mouth, urinary retention, constipation, confusion)
Anti-Histaminergic (sedation)
Anti-Adrenergic (postural hypotension)
Neuroleptic malignant syndrome
Change Seizure threshold
50
What is neuroleptic malignant syndrome?
Increased serum CK, hyperpyrexia, increased muscle tone, confusion, autonomic instability
51
How long should antipsychotics be continued?
1-2y after first episode, but 98% relapse after 2y so often continue for 5y. Many are non-adherent anyway
52
What advice should you give to patients if they decide to stop their antipsychotic?
Taper it over at least 3w as stopping suddenly doubles the risk of relapse
53
What monitoring should be done when starting antipsychotics? And how frequently after starting?
Prior and yearly:
- ECG
- BMI and waist circ
- Bloods: FBC, U&E, lipid profile, HbA1c, glucose, LFTs, prolactin
54
Why can't clozapine and carbemazepine be used together?
Both risk agranulocytosis
55
What is the risk with antipsychotics and metaclopramide?
Extra pyramidal SEs
56
Risk with (IV) erythromycin & quetiapine?
QT prolongation
57
What is the main mood stabiliser?
Lithium
58
Indications for lithium?
Prophylaxis in recurrent uni/bipolar affective disorder
Acutely in mania
Augmentation of ADs in resistant depression
Schizoaffective illness
Control aggression
59
Mechanism of lithium
Unclear
Interacts with all body systems that involve sodium, potassium, calcium and magnesium
probably affects neurotransmitters (serotonin, dopamine, noradrenaline, acetylcholine)
Interferes with cAMP linked receptors- action on kidney and thyroid
60
Route of lithium
Oral
61
Excretion of lithium
Renal
62
Contraindications for lithium
Thyroid disease
Renal disease
Cardiac disease
Addison's disease
63
Monitoring required for lithium?
Prior and 6 monthly: TFTs, eGFR and weight
Serum lithium- weekly at first and then 12 weekly
64
When should serum lithium be monitored in relation to dose?
12h after last dose
65
SEs of lithium at the therapeutic dose
Nausea
fine tremor
wt gain
oedema
polydipsia and polyuria
worse psoriasis and acne
Hypothyroid
66
What is the therapeutic dose of lithium?
0.4-1mmol/L (serum)
67
Symptoms of lithium toxicity
D&V
coarse tremor
slurred speech
ataxia
drowsy and confused
convulsions and coma
68
What is the treatment for lithium toxicity?
Stop the lithium and fluids
69
What could precipitate lithium toxicity?
Dehydration and diuretics
70
What does lithium interact with?
NSAIDs
Calcium Channel Bs
some abx
71
What are 3 other mood stabilisers?
Sodium valproate
Carbemazepine
Lamotrigine
72
What is lamotrigine especially good at as a mood stabiliser?
Preventing depressive episodes
73
SEs sodium valproate?
GI, weight gain, hair loss with curly regrowth, dose related tremor, thrombocytopenia
74
SEs lamotrigine
skin incl SJS
aseptic meningitis
dizziness
diplopia
leucopenia
insomnia
nausesa
75
Which mood stabilisers should be avoided in pregnancy?
Lithium
Lamotrigine
Valproate
76
Are different brands of lithium bioequivalent?
No, should know which brand they are on
77
Does lithium need to be tapered to stop?
Yes
78
SSRI + lithium could lead to what?
Mania
79
What type of diuretic should be used with lithium?
Loop
80
What can NSAIDs do to lithium levels in blood?
Increase
81
Mechanism Valproate?
GABA
82
What is a caution in carbemazepine?
Hepatic enzyme inducer
83
SEs carbemazepine?
agranulocytosis, hyponatraemia.
84
```
Nitrazepam
Flurazepam
Diazepam
Alprazolam
Clobazam
Chlordiazepoxide
```
These are short or long acting benzos?
Long
85
Lorazepam
Loprazolam
Lormetazepam
Temazepam
Short or long acting benzos?
Short
86
What do benzos do?
anxiolytic
sleep inducing
anticonvulsant
muscle relaxant
87
Indications of benzos?
Insomnia
GAD (short term and not for phobias or panic disorders)
Alcohol withdrawal
Control violent behaviour
2nd line for refractory epilepsy
88
Route of benzos?
Usually oral
Sometimes IM, IV, rectal
89
What is it important to consider when giving benzos?
Exclude underlying conditions and consider behavioural alternative treatment
90
Mechanism of benzos
Potentiate the inhibitory effects of GABA (Decreases neuronal excitability)
91
What are some other anxiolytics other than benzos?
Zopiclone and related
Antihistamines
Buspirone
92
SEs benzodiazepines?
Drowsy
Ataxia (falls risk)
Amnesia
Dependence
Disinhibition (may lead to aggression)
Potentiates alcohol and other sedatives- may be a dangerous combo
93
Signs of benzo OD?
Resp depression
Drowsy
Dysarthria
Ataxia
94
Treatment for benzo OD
Flumazenil
| but caution in mixed OD or benzo-dependent pts
95
What is a risk with anything but short term benzo?
Tolerance
96
Withdrawal Sx benzos?
Anxiety
Shakiness
Abdo cramps
Perceptual disturbances
Persecutory delusions
Seizures
97
Why might you get increased dreaming when stopping benzos?
They inhibit REM sleep
98
How long can weaning off iatrogenic benzo dependence take?
months- years
99
What does zopiclone do?
Hypnotic but without the anti-convulsant or muscle relaxing properties
100
Can zopiclone cause dependency?
Yes
101
What is Buspirone? Including mechanism.
Anxiolytic used short term for anxiety. 5HT1a partial agonsit
102
What are the two dementia drugs?
Acetylcholinesterase inhibitors
Memantine
103
Name the three AChE inhibitors
Donepezil
Rivastigmine
Galantamine
104
First line for mild-mod alzheimers?
Any AChEi
105
First line for mild-mod Lewy body? What if this isn't tolerated?
Donezepil or Rivastigmine first line, if not then galantamine
106
Severe lewy body treatment?
donezepil or rivastigmine, if not tolerated then memantine
107
Should you give AChEi or memantine in fronto temporal dementia?
No
108
Donezepil mechanism
Reversible inhibitor of AChE
109
Donezepil cautions in?
asthma/copd
some cardiac
peptic ulcer
110
Donezepil SEs
Mood/behavioural changes
muscle cramps
hallucinations
syncope
Urinary incontinence
Appetite decrease
sleep probs
111
AChEi doses should start ____
low and increase
112
Galantamine mechanism?
Reversible inhibitor of AChE with some nicotinic receptor agonist properties
113
Galantamine is available in which two forms?
Modified and immediate release
114
Galantamine cautions?
GI obstruciton or surgery
Urinary outflow obstructin or bladder surgery
Some HD
COPD/severe asthma
seizures
115
SEs galantamine
Skin reactions- SJS
decreased appetite
arrhyth
Mood changes
hallucinations
HTN
muscle spasms
Tremor
116
Galantamine and renal disease?
Avoid if eGFR <9mL/min
117
Rivastigmine mechanism
Reversible non-competitive inhibitor of AChE
118
Rivastigmine routes available
PO or transdermal
119
Rivastigmine cautions
GI ulcers
Bladder outflow obstruction
Hx asthma/copd
Sick sinus synd
Seizures
120
What is the risk with transdermal rivastigmine?
Leave the old patches on and have fatal OD
121
SEs rivastigmine
Appetite decrease
Mood changes
Hyperhidrosis
Hypersalivation
HTN
Movement disorders
Skin reactions
Urinary incontinence
PO: hallucinations, parkinsonism, sleep disorder, gait change
TD: gastric ulcer
122
What should you monitor when the pt is on rivastigmine
body weight
123
Instructions for transdermal administration of rivastigmine
Clean, dry, non-hairy, non-irritated skin on back, upper arm or chest. Remove after 24h. Avoid same site for 14 days.
124
Which AChEi for dementia in a patient who needs modified release?
Galantamine
125
Which AChEi for dementia in a patient who can't tolerate oral medication?
Rivastigmine transdermal
126
Which AChEi for dementia in a patient with history of bladder outflow obstruction?
Donezepil
127
Memantine action (and how does this help dementia)
Glutamate receptor antagonist. Glutamate is the major excitatory neurotransmitter in CNS. Inhibiting its action prevents cell damage.
128
What is a glutamate receptor antagonist also known as?
NMDA receptor antagonist
129
Memantine caution?
Epilepsy and avoid if eGFR <5mL/min
130
SEs memantine
dizziness
headaches
constipation
confusion
worse balance
131
St Johns wort is a complementary medicine used in what?
Depression (mild-mod)
Anxiety
SAD
Sleep disorders
132
Is there evidence for St Johns wort in severe depression
No
133
What is the problem with St John's wort (2)
Interactions
May trigger mania in bipolar
134
What is given for parkinsonian SEs of APs?
Procyclidine (or other antimuscarinics)
135
Can you give procyclidine in tardive dyskinesia?
No it worsens it
136
What does tardive dyskinesia look like?
TD causes stiff, jerky movements of your face and body that you can't control. You might blink your eyes, stick out your tongue, or wave your arms without meaning to do so.
Smacking lips
Flapping arms
Blinking
137
What is akathisia?
Feeling of inner restlessness. V unpleasant.
138
Tardive dyskinesia treatment
Worrying as may be irreversible on withdrawing therapy and treatment is usually ineffective. Treat ASAP
Swap or stop the AP
139
Akathisia treatment
Benzos, propanolol
140
Neurotransmitter in depression, anxiety, ADHD, migraine, OCD
Serotonin
141
Neurotransmitter in alzheimers
Acetylcholine
142
Neurotransmitter in Schiz and parkinsons
Dopamine (increased in schiz and decreased in park)
143
Neurotransmitter in Epileptic seizures and alcohol withdr
GABA
144
GABA is brain on or off?
Off
145
What neurotransmitter is brain 'on'
Glutamate
146
Neurotransmitter in depression decreased (not serotonin)
Noradrenaline
147
Neurotransmitter in migraine, stroke, autism
Glutamate
148
What is the action of monoamine neurotransmitters on the nervous system?
--> second messengers--> increased transcription factors --> increased BDNF --> increase neuroplasticity and neurogenesis in hippocampus
149
What decreases rate of transcription factors (and hence BDNF and neuroplasticity and genesis)?
Cortisol
150
Neurotransmitter in caffeine
Adenosine
151
Neurotransmitter in hunger
Cholecystokinin
152
Neurotransmitter in pain and appetite regulation, co-ordination and learning
Endocannabinoids
153
Neurotransmitters in tobacco
Acetylcholine and dopamine
