Block 33 Pharmacology Flashcards
Benzodiazepines drug examples?
- diazepam
- lorazepam
- temazepam
SSRI drug examples?
- Citalopram
- Fluoxetine
- Paroxetine
- Sertraline
what are the indications for benzos?
Anxiety disorders, acute behavioural control and rapid tranquillisation
indications for SSRIs?
Depression, anxiety disorders
safety info w benzos?
- co-presribing w opiods can cause increased risk of sedation, coma, resp depression and death
CI for all benzodiazepines?
- acute pulm insufficiency
- marked NM weakness
- can’t be used alone for: chronic psychosis, depression
- sleep apnea syndrome
paraxodical effects of benzos?
- paradoxical increase in hostility and agggression
- ranges from talkativeness and excitement to aggressive and antisocial acts
- increased anxiety and perceptual disorders
side effects of benzos?
- ataxia and confusion - elderly
- resp depression - high dose and IV use
- sleep disorders
- withdrawal syndrome
overdose of benzodiazepines?
- drowsiness, ataxia, dysarthria, nystagmus, and occasionally respiratory depression, and coma
benzos mechanism?
- CNS depressants
- enhances effect at GABA-A receptor -> sedative, hypnotic, and anxiolytic, muscle relaxant, anticonvulsant effect
SSRI drug action?
- seletively inhibit the re-uptake of serotonin
CI for SSRIs?
- poolry controlled SSRI
- manic phase
SSRI - elderly?
care with hyponatreaemia
side effects of SSRIs?
- GI side effect more common
- inc risk of GI bleeding
- inc anxiety and agitation after starting
which SSRIs have a higher risk of drug interactions?
fluoxetine and paroxetine
Which SSRIs can’t be used in long QT syndrome?
- citralopram and escitalopram
- cause QT prolongation
when should a PPI be prescribed w an SSRI?
if ppt also taking NSAIDs
interactions of SSRIS?
- MAOIs - serotonin syndrome
- aspirin
- NSAIDs-> prescribe PPI
- warfarin
SSRI overdose?
- nausea
- vomiting
- nystagmus
- sinus tachyardia
- tremor
- agitation
- convulsions
serotonin syndrome?
marked neuropsychiatric effects, neuromuscular hyperactivity, and autonomic instability, hyperthermia, rhabdomyolysis, renal failure, and coagulopathies may develop.
examples of SNRIs?
- Duloxetine
- Venlafaxine
SNRIs mechanism?
- inhibits reuptake of serotonin and noradrenaline
duloxetine is also used for?
urinary incontinence
SNRI safety info?
- SNRIs in the last month b4 delievry can inc risk of postpartum haemorrhage
side effects of SNRIs?
- Falls
- GI disorders
- sexual dysfunction
- palpitations
- urinary disorders
which SNRI is associated w higher risk of withdrawal?
Venlafaxine
Reboxetine mechanism?
Selective noradrenaline reuptake inhibitor
Indication of Reboxetine?
depression
Cautions of Reboxetine?
- bipolar
- epilepsy
- CVD
- urinary retention
Side effects of Reboxetine?
- accomodation disorder
- anx
- insomnia
- tachycardia
- vasodilation
Interactions of Reboxetine?
- isocardboxazid
- phenelzine - hypertensive crisis
Mirtazapine =
- pre-synaptic alpha-2 adrenoreceptor receptor blocker
- blocks serotonin receptors
- atypical tetracyclic AD
mitrazepine ix?
major depression
cautions of Mirtazapine?
- cardiac disorders
- DM
- mania
- seizures
- urinary retention
- hypotension
- psychosis
side effects of Mirtazapine?
- anx
- inc appetite
- constipation
- confusion
- oedema
examples of TCAs?
- Amitriptyline
- Imipramine
- Lofepramine
indications for tricyclics?
Depression, adjunct for chronic or neuropathic pain
CI of TCAs?
- heart block
- arrhythmias
- manic phase
TCAs- elderly?
- susceptible to side effects
- low initial doses
- monitoring for psychiatric and cardiac side effects
interactions of amitryptiline?
- adrenaline
- bupropion
- cloazpine - hyponatraemia and hypotension
- fluoxetine
- lithium
side effects of amitryptiline?
- anticholinergic syndrome
- droswiness
- QT prolongation
amitryptiline overdose?
- high rate of fatality
- dry mouth
- coma
- hypotension
- hypothermia
- resp failure
- arrhythmias
- dilated pupils
lofepramine side effects?
- agranulocytosis
- bone marrow disorders
- cardiac conduction disorders
- gynacomastia
Imipramine cautions?
- hyperthyroidism - high risk of arrhytmias
- inc intraocular pressure
- sig suicide risk
side effects of Imipramine?
- decreased appetite
- arrthymias
- hypotension
- hallucinations, tremors
TCAs mechanism?
- block serotonin, NA, and dopamine reiptake
- also block muscaronic receptors
anticholinergic effects of TCAs?
dry mouth, blurry vision, constipation, and urinary retention
MAOis indications?
Major depression and phobic patients with hypochondriacal features, social anxiety disorder
examples of MAOAi?
- phenelzine
- moclobemide
phenelzine =
non selective MAOI
Moclobemide=
reversible inhibitor of MAOA-A
monoamine oxidase?
- inhibiting this prevents breakdown of serotonin, melatonin, epinephrine, norepinephrine
CI for all MAOI?
- Cerebrovascular disease
- severe CVD
- phaechromocytoma
- manic phase
side effects of MAOI?
- Anx
- hallucinations
- insomnia
- postural hypotension - more common in elderly
- suicidal behavs
when should MAOA be discontinued?
Risk of postural hypotension and hypertensive responses. Discontinue if palpitations or frequent headaches occur.
monitoring for MAOI?
- MONITOR BP -risk of postural hypotension and hypertensive responses
withdrawal from MAOI?
- Agitation
- irritability
- slow speech
- vivid dreams
other symtoms that can occur when discontinuing MAOi?
hallucinations, paranoid delusions
Drugs used for managing opioid withdrawal ?
Methadone & Buprenorphine
methadone Ix?
- opiod dependence
- svr pain
CI of all opiods (includes methadone)
- ARD
- head injury, raised ICP
- risk of paralytic ileus
CI for methadone?
phaechromocytoma
methadone mechanism?
- methadone is a full agonist of the mu-opioid receptor - binds to these receptors in the brain and fully activates them.
- This action can relieve withdrawal symptoms and cravings. Has a long half-life
buprenorphine mechanism?
- partial agonist of the mu-opioid receptor and an antagonist of the kappa-opioid. It binds to the mu-opioid receptors in the brain but only partially activates them.
- This partial activation is enough to alleviate cravings and withdrawal symptoms in individuals with opioid dependence
- displaces other opiods from kappa receptors
drugs causing prolonged QT?
- amiodarone, solatolol
- TCA, SSRIs - espec citalopram
- methadone
- haloperidol
- ondansteron
side effects of all opiods?
- arrhythmias
- euphoric mood
- hallucination
- miosis
- palpitations
- resp depression
- vomiting and nausea - more common on initiation
methadone side effects?
- asthma exacerbation
- hyperprolactinaemia
- hypothermia
- QT prolongation
methadone toxicity?
- long acting opiod - hazardous even in low doses for kids
buprenorphine side effects?
- anxiety
- depression
- diarrhoea
- tremor
effects of ? are only partially reversed by naloxone?
buprenorphine
Drugs used for smoking cessation?
- Nicotine replacement therapy
- Bupropion
- Varenicline
NRT mechanism?
- Reduced cravings due to nicotine addiction
- patches, gum, sprays, tablets, lozenges
cautions of nicotine?
- DM - monitoring of BG needed when initating Tx
- haemodynamically unstable ppts
side effects of nicotine?
- dizziness
- headaches
- hyperhidrosis
- nausea, vomiting
- palpitations
nicotine withdrawal symptoms?
- malaise
- headache
- dizziness
- sleep disturbance
- coughing
- restlessness
- dec HR
- apthous ulcers
Bupropion mechanism?
- dopamine and NA reuptake inhibition ->insomnia
- works on pathways involved in addiction and withdrawal
buprion safety info?
- SS when taken with SSRI and SNRIs
CI of bupropion?
- acute alcohol withdrawal
- acute benzo withdrawal
- bipolar
- EDs
- seizures
side effects of buprion?
- abd pain
- anx
- conc impaired
- tremor
- insomnia - don’t take near bedtime
Varenicline mechanism?
selective nicotinic receptor partial agonist
side effects of varenicline?
- nausea - most common
- headache
- insomnoa
- abn dreams
cautions of vareniciline?
- lowered seizure threshold
- history of psychiatric illness
Ix of lithium?
Treatment and prophylaxis of mania, hypomania and depression in bipolar disorder
lithium mechanism?
- reduced glutamate and dopamine
- inc GABA - release and upregulates receptors
CI of lithium?
- low sodium diets
- cardiac disease
- addisions
- dehydration
LT lithium use?
- associated w thyroid disorders and mild cognitive and memory impairment
- monitoring of thyroid function every 6 months
lithium interactions?
- amitryptiline
- acetazolamide
- bupropion
lithium side effects?
- angioedema
- AV block
- delirium
- idiopathic intercranial hypertension
- QT prolongation
lithium toxicity?
- coarse tremor (a fine tremor is seen in therapeutic levels)
- hyperreflexia
- acute confusion
- polyuria
- seizure
- coma
what can lithium toxicity be precipitated by?
- dehydration
- renal failure
- drugs: diuretics (especially thiazides), ACE
inhibitors/angiotensin II receptor blockers, NSAIDs and metronidazole.
lithium is?
teratogenic
lithium safety?
- very narrow therapeutic index
- requires monitoring of serum concs
Mood stablising anticonvulsant drugs?
- Sodium valproate
- Carbamazepine
- Lamotrigine
when are mood stabilising anticonvulsants used?
Treatment and prophylaxis of mania, hypomania and depression in bipolar disorder
sodium valproate is CI in?
- women and girls of childbearing age unless conds of pregnancy prevention programme are met
- severe hepatic dysfunction
- urea cycle disorders - hyperammonaemia risk
valproate -> ? toxicity?
liver
Hair
side effects of valproate?
- alopecia - regrowth may be curly
- abn behaviour
- hepatic disorders
- hallucination
- stupor
when should valproate be withdrawn?
persistent vomiting and abdominal pain, anorexia, jaundice, oedema, malaise, drowsiness, or loss of seizure control.
valproate mechanism?
- voltage gated sodium channel blockage
- inc GABA levels -> anti-manic properties
carbamazepine mechanism?
- sodium channel inhibitor
- serotonin releasing agent
CI of carbamazepine?
- acute porphyrias
- AV conduction abn
- history of BM suppression
side effects of carbamazepine?
- induces P450 enzyme
- drowsiness
- visual disturbances - espec diplopia
- leucopenia and agranulocytosis
- hyponatraemia secondary to syndrome of inappropriate ADH secretion
lamotrigine mx?
binds and inhibits sodium VGC, inhibits glutamate and aspartate release
cautions of lamotrigine?
- PD
- seizures
- brugada syndrome
side effects of lamotrigine?
- aggressgion
- dizziness
- drowsiness
- dry mouth
- rash
skin changes w lamotrigine?
- SJS
- toxic epidermal necrolysis
Atypical antipsychotic drugs?
- Risperidone
- Olanzapine
- Clozapine
- Aripiprazole
- Quetiapine
AP indications?
Psychosis, schizophrenia, rapid tranquillisation, mania
typical AP/ first gen?
- Haloperidol (a butyrophenone)
- Chlorpromazine (a phenothiazine)
- Flupentixol (a thioxanthine)
- Sulpiride (a substituted benzamide)
Atypical AP mechanism?
- antagonism of D2 receptors in the mesolimbic pathway (overactivity leads to positive symptoms)
- antagonism of serotonin, alpha-1 adrenoreceptor, histamine 1
when should risperidone be avoided?
- acute porphyrias
- cataract surgery
- LBD
- prolactin dependent tumours
- dehydration
interactions of risperidone?
- levodopa
- lithium
- methylphenidate
risperidone side effects?
- decreased weight
- vision disorders
- sexual dysfunction
- oedema
olanzapine mechanism?
Olanzapine is a dopamine D1, D2, D4, 5-HT2, histamine- 1-, and muscarinic-receptor antagonist.
CI of olanzapine?
- unstable angina
- bradycardia
- severe hypotension
- SSS
- acute MI
Interactions of olanzapine?
- smoking - dose adjustment
- clozapine: constipation -> intestinal obstruction
- levodopa
- valproate
olanzapine side effects?
- anticholinergic syndrome
- eosinophilia
- fever
- glycosuria
- sexual dysfunction
stopping AP?
- high risk of relapse if medication stopped after 1-2 yrs
- withdrawal should be gradual and monitored for 2 years for signs of relapse
monitoring for olanzapine?
- blood lipids and weight at baseline,at 3 months, and then yearly
- fasting blood glucose at baseline, at 4–6 months, and then yearly
clozapine mechanism?
dopamine D1, dopamine D2, 5-HT2A, alpha1-adrenoceptor, and muscarinic-receptor antagonist.
clozapine indications?
- Tx resistant schiz
- psychosis in PD
Clozapine - safety info?
- risk of intestinal obstruction, faecal impaction and paralytic ileus
Two,relate them to side effects
CI of clozapine?
- history of neutropenia or agranulocytosis
- bone marrow disorders
- severe CNS depression
- paralytic ileus
monitoring for Clozapine?
- FBC - neutropenia and agranulocytosis
- fatal myocarditis (most commonly in the first 2 months) and cardiomyopathy
constipation & clozapine?
- Impairment of intestinal peristalsis, including constipation, intestinal obstruction, faecal impaction, and paralytic ileus, (including fatal cases) reported
- should be used in caution in ppts taking drugs that can constipate e.g. AM, or w a history of colonic disease or lower abd surgery
clozapine interactions?
- dose adjustment for if smoking started/ stopped
- buprenorphine
- carbamazepine
- halopreidol
clozapine side effects?
- leucocytosis
- speech impairment
- temp reg disorders, sweating abn
- syncope
photosensitisation?
- can occur with higher doses of AP
- should avoid direct sunlight
aripriprazole mechanism?
- partial D2 agonist
- weak serotonin 1 agonist
- 5-HT2 antagonsim
side effects of aripiprazole?
- DM
- MSK stiffness
- vision disorders
quetiapine mechanism?
- dopamine D1 and D2 antagonist
- serotonin, alpha-1 adrenoreceptor and histamine 1 receptor antagonist
Quetiapine interactions?
- lithium
- clozapine
- clarithromycin
quetiapine side effects?
- dyspepsia
- palpitations
- peripheral oedema
- withdrawal
- suicidal behaviour
- syncope
haloperidol mechanosm?
- D2 receptor antagonism
CI for haloperidol?
- congenital QT syndrome
- LBD
- QT-c prolongation
haloperidol interactions
- amiodarone
- apiprazole
- chlorpromazine
- citraopram
- clozapine
- erythromycin
side effects of haloperidol?
- depression
- neuromuscular dysfunction
- psychotic disorder
- vision disorders
chlorpromazine mechanism?
- D2 receptor antagonism
- Blocks α-1 & 5-HT2 > D2 >D1.
CI of chloropromazine?
- CNS depression
- bone marrow depression
- hypotension
- Parkinsonism
- hepatic dysfunction
- glaucoma
- QT prolongation (e.g. drug-induced)
antimuscarinic side effects of chlorpromazine?
- sedation
- blurred vision
- tachycardia,
- dry mouth & dental cavaties,
- constipation,
- difficulty urinating
- toxic doses
- confusional state
chlorpromazine general side effects?
- impaired glucose intolerance
- muscle tone inc
- SLE
- temp reg issues
Flupentixol mechanism?
- primarily D2 receptors
- 5-HT2 receptors
CI for flupentixol?
- circ collapse
- CNS depression
- comatose states
- excitable states, overactive ppts
flupentixol interactions?
- clozapine
- levodopa
flupentixol side effects?
- drowsiness
- dry mouth
- weight gain
- EPS - muscle stiffness, tremors, involuntary movements
Sulpiride mechanism?
- D2 antagonism
CI for Sulpiride?
- CNS depression
- comatose states
- phaechromocytoma
sulpiride side effectS?
- Breast abn
- abn orgasm
- oculogyric crisis
sulpiride interactions?
- levodopa
- lithium