Meds Flashcards
Hypnotics and anxiolytics
Act on GABA receptors
Impair ability to drive/operate machinery
Tolerance and dependence
Short term, for anxiety (use anti-depressants long term)
Benzodiazepines
Eg. Diazepam (anxiolytic), temazepam (hypnotic), lorazepam (anxiolytic) and triazolam
Mechanism: Enhance GABA at GABA-A receptors
Cautions: Respiratory failure, breast feeding, previous addiction
Adverse effects: Drowsiness, confusion, disinhibition, aggression, dependency and addiction, memory and balance problems
Quite safe in OD alone but dangerous when combined with alcohol or opiates
GABA antagonist Flumazenil used for overdose
Interactions: Potentiate other sedatives (eg alcohol, anti-histamines, anti-depressants, anaesthesia)
Tolerance: 3-14 days
Withdrawal: insomnia, anxiety, sweating, tremor, perceptual disturbance, delirium and seizures. Can manifest from hours to 3 weeks after dose and may persist for months. Use for a maximum of 2-4 weeks for severe, disabling anxiety or insomnia
Barbituates
Avoid as dangerous in overdose
Hypnotic/anxiolytic
Chlormethiazole
Hypnotic/anxiolytic
Conjunctival, nasal and gastric irritation
Stimulant properties addictive
Z drugs
Zopiclone, Zolipidem, Promethazine, Melatonin
Hypnotic (short acting)
GABA-A agonist
Addictive properties similar to benzos
Buspirone
Anxiolytic BUT is a 5-HT-1A receptor agonist
No evidence of addiction or abuse potential
May be less potent than benzos and take 2-3 weeks to develop
Mildly anti-depressant
Antidepressants
Do not alter normal mood
Takes 2-4 weeks to develop
May also be used in anxiety
Not addictive, but some are very toxic in overdose and a discontinuation sundrome may occur
Tricyclics (eg, mechanism, indications, cautions)
Eg. Amitryptaline/dothiepin (sedative), imipramine, lofepramine, clomipramine
Mechanism: 5-HT/noradrenaline re-uptake inhibitors. Takes some weeks to have benefit
Indications: depression, anxiety
Cautions: cardiac disease, glaucoma, prostatism, epilepsy, hepatic impairment, elderly (hyponatraemia/post hypotension risk)
Tricyclics (adverse effects and interactions)
Muscarinic antagonism: dry mouth, blurred vision, constipation, urinary retention, impotence, delirium
Histamine antagonism - sedation and weight gain
Andrenergic antagonism - postural hypotension, sweating
Direct membrane effects - reduced seizure threshold, arrhythmia, heart block
5-HT antagonism - weight gain, weight gain
5-HT/NA re-uptake inhibition - mania
Interactions: Hypertensive crisis with adrenaline or MAOIs
MOAIs
Eg. Phenelzine, moclobemide
Mechanism: Inhibit monoamine oxidase → block 5-HT and NA metabolism → ↑ levels of 5-HT and NA
Cautions: Cardiac disease, epilepsy, hepatic impairment, ECT
Adverse effects: Anticholinergic, hypotension, oedema, fits, neuropathy, drowsiness, delirium, mania, hepatitis, leucopenia
Interactions: hypertensive crisis with sympathomimetics and tricyclics, potentiates CNS depression with opiates. Tyramine reaction (a sympathomimetic) → can’t eat cheese, red meat, alcohol. Restrictions apply for two weeks after drug is stopped
Last resort drug.
Need a drug holiday after stopping before give another drug
SSRIs
eg. Fluoxetine, sertraline, citalopram
Mechanism: 5-HT reuptake inhibitors
Indications: depression, anxiety, panic, OCD, impulse control disorders
Cautions: Renal/hepatic impairment, pregnancy, epilepsy
Adverse effects: short lived - 3 or 4 days following commencement or dose increase, nausea, anorexia, ↑ anxiety. Long term - throughout tx, headache, insomnia, sexual dysfunction, ↑ risk GI bleeds
Interactions: toxicity with MAOIs and anti-migraine drugs such as sumitriptan
Reboxetine
NARI
Depression with anergia, poor motivation and concentration
Caution in renal and hepatic impairment, urinary retention and glaucoma
Adverse effects anticholinergic
Interacts with MOAIs
SNRI
Venlafaxine, duloxetine
Inhibit 5HT, NA, DA uptake
Severe and treatment resistant depression
Anxiety disorders incl panic disorder and OCD
Caution if hx of MI
Adverse similar to SSRIs, also hypertension at higher doses
Avoid use with MAOIs
Trazodone
5-HT receptor antagonism
GAD/non-specific sedative/augment SSRIs/SNRIs
Very safe
Adverse effect - sedation, rare serious side effect is priapism
Mirtazepine
Complex. Adrenergic alpha-2 receptor antagonism → ↑ 5-HT and NA neurotransmission. Also blocks 5-HT2 receptors which helps treat anxiety and 5-HT3 receptors which helps prevent sexual dysfunction. Blocks histamine receptors → sedation
Caution in epilepsy, hepatic/renal impairment, cardiac disorders, urinary retention, DM
Adverse - weight gain, sedation, rarely a reversible agranulocytosis
2nd line or if problems sleeping
Mood stabilisers
Primarily prophylaxis for bipolar
Acute episodes of mania
May also be adjuncts to anti-depressants for depression
Lithium
Mechanism unknown. Therapeutic window very close to toxicity, important to check levels at least 3 monthly (weekly initially).
Also: U+E, eGFR, TFT, weight, calcium at baseline and 6 monthly
Cautions: renal/cardiac impairment, pregnancy, breastfeeding
Interactions: diuretics, NSAIDs, ACE-I, MAOIs, carbamazepine, high dose antipsychotics
Adverse effects: polyuria, polydipsia, fine tremor, GI disturbance, oedema, weight gain, hypothyroidism, goitre, ECG changes; teratogenic (ebstein’s anomaly)
Intoxication: Anorexia, vomiting, diarrhoea, weakness, twitching, coarse tremor, ataxia, drowsiness, confusion, coma → renal and circulatory failure, convulsions and death
Treat toxicity: Sodium chloride and water
Carbemazepine
Anti-epileptic
Mood stabiliser
Not as effective as lithium but less toxic
Adverse effects: drowsiness, neutropenia
Interactions: MAOIs and lithium → neurotoxicity
Sodium Valproate
May be as effective as lithium or better for those with high frequency bipolar, with high proportion of manic episodes.
Adverse effects include hepatic dysfunction, blood disorders, nausea, ataxia and tremor
Lamotrigene
Depressed bipolar disorder and for prophylaxis
Associated with serious and sometimes fatal skin disorder (Stevens-Johnson syndrome)
Introduce drug slowly, warn patients to look out for flu-like symptoms and skin rashes
Other adverse effects - headache, nausea, ataxia
Interactions: other anti-convulsants
Antipsychotics
Schizophrenia, mania, psychotic depression
Short term sedation
Prophylactic in schizophrenia
May take several weeks for anti-psychotic effect to develop
Typical antipsychotics
Mechanism: Block dopamine D2 receptors
Orally or depot
Chlorpromazine, haloperidol
Cautions: cardiovascular and cerebrovascular disease, parkinsonism, epilepsy, pregnancy, breast feeding, renal and hepatic impairment, prostatism, glaucoma
Adverse effects: similar to TCAs plus dystonia of jaw, extraocular muscles and neck, parkinsonism, akathisia, tardive dyskinesia (often irreversible), postural hypotension hyperprolactinaemia → gynaecomastis, galactorrhoea, amenorrhoea, blood dyscrasias, hepatitis, skin rashes and photosensitivity
QT prolongation
Neuroleptic malignant syndrome: rare but potentially fatal: rigidity, hyperpyrexia and clouding of consciousness
Interactions: potentiates hypotensives and sedatives
Typical antipsychotic examples
Grouped according to adverse effects
(S=sedation, A=anticholinergic, E=extrapyridamal)
S+++;A++;E++: Chlorpromazine
S++;A+++;E+: Thioridazine
S+;A+;E+++: Trifluoperazine, Haloperidol, Flupenthixol decanoate/Fluphenozine decanoate (depot)
Sulprimide
Atypical antipsychotic
‘Clean’ dopamine agonist → fewer side effects than typicals, especially fewer extrapyridamal
Avoid in renal impairment
Less sedating but can still be used in acute psychosis