pharmacology Flashcards
what type of drugs best cross the blood brain barrier?
Hydrophobic drugs
The BBB is made of fat and so is hydrophobic meaning it is easiest for hydrophobic drugs to pass through
which one of these neurotransmitters is not a monoamine:
- dopamine
- glutamate
3.noradrenaline - 5- Hydroxytryptophan (5-HT, serotonin)
- Glutamate
(the rest are monoamines)
examples of monoamines
dopamine
noradrenaline
5- Hydroxytryptophan (5-HT, serotonin)
Imipramine
Phenelzine
Fluoxetine
which nuclei is involved in the serotonin projection pathway
Rostral nucleus and then projects all over the cortex
what is the caudal raphe nuclei involved in?
analgesia
what is the locus coreuleus involved in?
-arousal, emotion
examples of monoamine oxidase inhibitors
-phenelzine (irreversible inhibitor)
-moclobemide (reversible inhibitor)
MOA: monoamine oxidase inhibitors
Irreversible (phenelzine) or reversible (Moclobemide) inhibitors of MAO-A and B
SE: monoamine oxidase inhibitors
-Hypertensive crisis if patient eats cheese, gravy, yoghurt and any other foods with dopamine and high tyrine
-Increases effects of other drugs (e.g. barbiturates) by decreasing their metabolism
-Insomnia
-Postural hypotension
-Peripheral oedema
Examples of triyclic antidepressants
-Imipramine (most commonly)
-Dosulepin
-Amitriptyline
-Lofepramine
MOA: triyclic antidepressants
Block the reuptake of monoamines (mainly noradrenaline and 5-HT) into presynaptic terminals
SE: triyclic antidepressants
Anticholinergic: (inhibits parasympathetic, rest and digest)
-Blurred vision
-Dry mouth
-Constipation
-Urinary retention
-Sedation
-Weight gain
-Postural hypotension
-Tachycardia
-Arrythmias
-Cardiotoxic overdose
depression is a result of a deficit in what type of neurotransmitters?
depression is a result of a deficit in MONOAMINE transmitters
in particular:
-serotonin (5-HT)
-noradrenaline
what drugs can induce low mood?
-drugs that deplete stores of monoamines (e.g. reserpine)
how long does it take for most antidepressants to work?
several weeks (they have a delayed reaction)
to antidepressants work better for those with more mild or severe depression?
more severe
example of SSRIs?
-fluoxetine
-Citalopram/ Escitalopram
-Sertraline
-Paroxetine
MofA: SSRIs
-selectively inhibit reuptake of serotonin (5-HT) from the synaptic cleft
SE: SSRIs
- Nausea (an decrease appetite and lose weight as SE)
- Headache
- Transient increase in self harm/ suicidal ideation in < 25 years
- Sweating/ vivid dreams
- Sexual dysfunction
- Hyponatraemia (in elderly)
- Discontinuation effects
Paroxetine stopped suddenly can give very bad mental and physical affects
advantage of using SSRIs over tricyclics?
-SSRIs are more selective than tricyclics and so have less anticholinergic side effects
example of fual reuptake inhibitors/ SNRIs ?
-duloxetine
-venlafaxine
MofA of SNRIs?
-block the reuptake of monoamines (noradrenaline and 5-HT) into presynaptic terminals
-increase both serotonin and norepinephrine levels
SE: SNRIs?
Similar to SSRIs:
* Nausea (an decrease appetite and lose weight as SE)
* Headache
* Transient increase in self harm/ suicidal ideation in < 25 years
* Sweating/ vivid dreams
* Sexual dysfunction
* Hyponatraemia (in elderly)
Discontinuation effects
MofA: Mirtazapine?
-blocks a2, 5-HT2 & 5-HT3
SE: Mirtazapine?
-weight gain
-sedation
how is lithium normally given?
-as lithium carbonate
MofA of lithium
-may block phophatidylinositol pathway (second messanger system)
OR
-inhibit Glycogen synthase Kinase 3-beta
OR
-modulate NO signalling
what are the side effects of lithium?
SE:
-dry mouth/strange taste
-polydipsia + poliuria
-tremor
-hypothyroidism
-long term reduced renal function
-nephrogenic diabetes insipidus
-weight gain
TOXIC EFFECTS:
-vomiting
-diarrheoa
-ataxia/ coarse tremor
-drowsiness/altered conscious level
-convulsions
-coma
exmaples of anticonvulsants given for bipolar?
-Valproic acid
-Lamotrigine
-Carbamazepine
MofA: anticonvulsants
-very unclear
-perhaps potentiate GABA transmission and therefore block overactive pathways (kindling model of bipolar disorder)
SE: Valproate (anticonvulsant)
-Drowsiness
-Ataxia
-CVD effects
-Induces liver enzymes
-tetragenicity (neural tube defect)
SE: carbamasepine
-drowsiness
-ataxia
-CVD effects
-induces liver enzymes
SE: lamotrigine
-very small risk of Stevens Johnson syndrome
examples of antipsychotics
-quetiapine
-atripiprazole
-olanzapine
-lurasidone
MofA: antipsychotics
-dopamine antagonism and 5-HT antagonism
SE: antipsychotics
-sedation
-weight gain
-metabolic syndrome
Atripiprazole= extra pyramidal side effects
