pharmacology

Question 1

what type of drugs best cross the blood brain barrier?

Answer 1

Hydrophobic drugs

The BBB is made of fat and so is hydrophobic meaning it is easiest for hydrophobic drugs to pass through

Question 2

which one of these neurotransmitters is not a monoamine:

1. dopamine
2. glutamate
   3.noradrenaline
3. 5- Hydroxytryptophan (5-HT, serotonin)

Answer 2

2. Glutamate

(the rest are monoamines)

Question 3

examples of monoamines

Answer 3

dopamine

noradrenaline

5- Hydroxytryptophan (5-HT, serotonin)

Imipramine

Phenelzine

Fluoxetine

Question 4

which nuclei is involved in the serotonin projection pathway

Answer 4

Rostral nucleus and then projects all over the cortex

Question 5

what is the caudal raphe nuclei involved in?

Answer 5

analgesia

Question 6

what is the locus coreuleus involved in?

Answer 6

-arousal, emotion

Question 7

examples of monoamine oxidase inhibitors

Answer 7

-phenelzine (irreversible inhibitor)
-moclobemide (reversible inhibitor)

Question 8

MOA: monoamine oxidase inhibitors

Answer 8

Irreversible (phenelzine) or reversible (Moclobemide) inhibitors of MAO-A and B

Question 9

SE: monoamine oxidase inhibitors

Answer 9

-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

Question 10

Examples of triyclic antidepressants

Answer 10

-Imipramine (most commonly)
-Dosulepin
-Amitriptyline
-Lofepramine

Question 11

MOA: triyclic antidepressants

Answer 11

Block the reuptake of monoamines (mainly noradrenaline and 5-HT) into presynaptic terminals

Question 12

SE: triyclic antidepressants

Answer 12

Anticholinergic: (inhibits parasympathetic, rest and digest)
-Blurred vision
-Dry mouth
-Constipation
-Urinary retention
-Sedation
-Weight gain
-Postural hypotension
-Tachycardia
-Arrythmias
-Cardiotoxic overdose

Question 13

depression is a result of a deficit in what type of neurotransmitters?

Answer 13

depression is a result of a deficit in MONOAMINE transmitters

in particular:
-serotonin (5-HT)
-noradrenaline

Question 14

what drugs can induce low mood?

Answer 14

-drugs that deplete stores of monoamines (e.g. reserpine)

Question 15

how long does it take for most antidepressants to work?

Answer 15

several weeks (they have a delayed reaction)

Question 16

to antidepressants work better for those with more mild or severe depression?

Answer 16

more severe

Question 17

example of SSRIs?

Answer 17

-fluoxetine
-Citalopram/ Escitalopram
-Sertraline
-Paroxetine

Question 18

MofA: SSRIs

Answer 18

-selectively inhibit reuptake of serotonin (5-HT) from the synaptic cleft

Question 19

SE: SSRIs

Answer 19

• 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

Question 20

advantage of using SSRIs over tricyclics?

Answer 20

-SSRIs are more selective than tricyclics and so have less anticholinergic side effects

Question 21

example of fual reuptake inhibitors/ SNRIs ?

Answer 21

-duloxetine
-venlafaxine

Question 22

MofA of SNRIs?

Answer 22

-block the reuptake of monoamines (noradrenaline and 5-HT) into presynaptic terminals

-increase both serotonin and norepinephrine levels

Question 23

SE: SNRIs?

Answer 23

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

Question 24

MofA: Mirtazapine?

Answer 24

-blocks a2, 5-HT2 & 5-HT3

Question 25

SE: Mirtazapine?

Answer 25

-weight gain
-sedation

Question 26

how is lithium normally given?

Answer 26

-as lithium carbonate

Question 27

MofA of lithium

Answer 27

-may block phophatidylinositol pathway (second messanger system)

OR

-inhibit Glycogen synthase Kinase 3-beta

OR

-modulate NO signalling

Question 28

what are the side effects of lithium?

Answer 28

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

Question 29

exmaples of anticonvulsants given for bipolar?

Answer 29

-Valproic acid
-Lamotrigine
-Carbamazepine

Question 30

MofA: anticonvulsants

Answer 30

-very unclear
-perhaps potentiate GABA transmission and therefore block overactive pathways (kindling model of bipolar disorder)

Question 31

SE: Valproate (anticonvulsant)

Answer 31

-Drowsiness
-Ataxia
-CVD effects
-Induces liver enzymes
-tetragenicity (neural tube defect)

Question 32

SE: carbamasepine

Answer 32

-drowsiness
-ataxia
-CVD effects
-induces liver enzymes

Question 33

SE: lamotrigine

Answer 33

-very small risk of Stevens Johnson syndrome

Question 34

examples of antipsychotics

Answer 34

-quetiapine
-atripiprazole
-olanzapine
-lurasidone

Question 35

MofA: antipsychotics

Answer 35

-dopamine antagonism and 5-HT antagonism

Question 36

SE: antipsychotics

Answer 36

-sedation
-weight gain
-metabolic syndrome

Atripiprazole= extra pyramidal side effects