Therapeutics Flashcards
SSRI’s mechanism
increase serotonin activity by reducing pre-synaptic reuptake of serotonin after release
…so more serotonin…down regulation of post synaptic receptors
SSRI’s s/e
agitation
nausea
GI disturbance
headache
weight change
sexual dysfunction
suicidal idealation - younger
sertraline safest in
CVD
citalopram s/e
QT prolong
fluoxetine switching
risk of serotonin syndrome
paroxetine stop
discontinuation syndrome
SNRI mechanism
same as SSRI but bind to NA reuptake receptors as well
SNRI s/e
sedation
nausea
sexual dysfunction
mirtazapine mechanism
noradrenergic and specific serotonergic antidepressant - 5HT-2 and 5HT-3 antagonist and H1 activity
mirtazepine
sedation (histamine)
weight gain
TCA uses and examples
if not respond to SSRI’S
newer - lofepramine
older - amitriptyline
TCA s/e
muscarinic and histaminic side effects
QT prolong and arrhythmias
MAOI mechanism
MAOI-A - work on serotonin
MAOI-B - work on dopamine
…both can increase adrenaline
MAOI types
irreversible (more dangerous) - phenelzine, isocarboxazid
reversible (less dangerous) - moclobamide, tranylcypromine
MAOI cautions
potential for significant drug interactions
tyramine reaction leading to hypertensive crisis - avoid cheese, pickled meats, wine and other tyramine products
if changed to another antidepressant, need a washout period (up to 6 weeks)
vortioxetine mechanism
serotonergic activity
vortioxetine s/e
nausea
when use mirtazapine not SSRI
if major weight loss or major sleep difficulty
Anxiety and OCD dose changes
If no initial change, consider increasing
Discontinuation syndrome
Sweating, shakes, agitation, insomnia, headaches, irritability, N+V
…worse if shorter half life (paroxetine and venlafaxine)
Stop paroxetine and venlafaxine
Alternate days of taking or snap in half
Or switch to fluoxetine and then reduce
Serotonin syndrome sx
Headaches, agitation, hypomania, coma, shiver, sweat, hyperthermia, tachycardia, N+V, myoclonus, hyperreflexia, tenor
Serotonin syndrome tx
Fluids and monitor
Antipsychotics mechanism
Reduce levels of dopamine activity at D2 receptors at mesocortical and Mesolimbic pathways
Antipsychotics general s/e
Nigostriatal - movement
Tuberoinfundibular - hypothalamic-pituitary-adrenal axis
Sedation
Extrapyramidal
Weight gain
Acute dystopia - ocuolgyric crisis
Typical v atypical antipsychotics mechanism
Typical - muscarinic and hustaminic receptors
Atypical - serotonergic
Typical antipsychotics examples
Haloperidol
Chlorpromazine
Atypical antipsychotics examples
Clozapine
Olanzapime
Riperidone
Anomaly atypical antipsychotic
Aripiprazole - D2 partial agonist not antagonist so fewer side effects
Typical antipsychotics s/e
Extra pyramidal - bradykinesia, muscle stiffness, tremor, tardive dyskinesia, akathisia
Dizziness
Sexual dysfunction
Atypical antipsychotics s/e
Weight gain
Dyslipidaemia and diabetes
Antipsychotic generally monitoring
FBC, LIPID, LFT, HBA1C, WEIGHT, ECG, BP, PULSE,
Neuroleptic malignant syndrome what and risks
Life threatening reaction to antipsychotics - fever, confusion, muscle rigidity, sweating, autonomic instability
Risk of death due to rhabdomyolysis, renal failure, seizures
Neuroleptic malignant syndrome risk factors
High potency dopamine antagonist ie typical ones, high doses, young men
Neuroleptic malignant syndrome tx
EMERGENCY
stop antipsychotics
Give benzo acutely due to behaviour change
Fluid resuscitation
Reduce temp
Oxygen
Fluids and sodium bicarbonate
Relax muscles with Dantrolene or lorazepam
Extra pyramidal and acute dystonia treatment
Too much acetylcholine in relation to dopamine….reduce by antagonising with procyclidine
Most efficacious antipsychotic
Clozapine
D2 antagonist, 5HT2 antagonist
Used after trying two other ones
Clozapine s/e
Leukopenia
Constipation and fatal bowel obstruction
Hypersalivation
Urinary incontinence
Clozapine agranulocytosis tx
Stop any myelosuppresive drugs
Avoid antipsychotics for a couple of weeks
Consultant haematologist
Avoid infection
Lithium or G-CSF
Beta blocker mechanism
Reducing autonomic activity
Beta blockers c/i
Asthma
Benzodiazepines mechanism
Bind to GABA receptors to potentiate effects of GABA and reduce excitability of neurones
Benzo how long use
Tolerance, dependence
Misuse
<6 weeks
Pregablin mechanism
Binds ro voltage gated calcium channels on neurones reducing neuronal activity
Pregablin indications
Anxiety
Neuropathic pain
Epilepsy
Pregablin s/e
Sedation
Weight gain
Hypnotics types
Benzodiazepines - temazepam, lormatazepam
Non Benzo - zopiclone
< 2 weeks
Mood stabilisers indications
Bipolar
Lithium mechanism
Lowers noradrenaline release and increase serotonin synthesis
Lithium monitoring
Regular serum lithium levels - narrow gap between effective and toxic dose
Lithium other indications
Self harm
Augment antidepressant
Lithium s/e
GI disturbance, metallic taste, dry mouth, fine tremor, polydipsia, polyuria, weight gain
Lithium long term effects
Hypothyroidism
Renal impairment
Lithium toxicity
Confusion, coarse tremor, NAND V, ataxia, seizures
Tx with stop lithium and supportive fluids
Lithium interactions
NSAIDS
loop diuretics
ACEi
1st line tx for bipolar
Quetiapine
Second generation antipsychotics in bipolar
Anticonvulsants in bipolar examples
Sodium valproate
Carbamazepine
Lamotrigine
Anticonvulsants s/e
Sedation
Weight gain
Thrombocytopenia
Drugs for ADD and ADHD
Methylphenidate - CNS stimulants
Atomoxetine - NA re uptake inhibitor
antipsychotics in elderly pts
increased risk of stroke and VTE
mirtazapine
blocks alpha 2 adrenergic receptors - increases release of neurotransmitters
fewer side effects - sedation and increased appetitie
SSRI +NSAID
require PPI
citalopram
QT prolongation
SSRI interactions
warfarin
heparin
NSAIDS
aspirin
tritptans
