Pharmacology Flashcards
What type of drugs most effectively diffuse across the blood brain barrier?
A. Hydrophilic/ Lipophobic
B. Hydrophobic/ Lipophillic
C. Neither is better than the other
D. None of them do
B
To get into the brain drugs must be lipophillic
E.g. Atenolol is ineffective as anti-anxiety medication as it doesn’t actually enter the brain, but propranolol does and so therefore is effective
What class of antidepressants may be used to treat neuropathic pain?
tricyclics
What are some antidepressant drug classes?
- Monoamine oxidase inhibitors
- Monoamine reuptake inhibitors
- Tricyclics
- SSRIs
- Noradrenaline reuptake inhibitors
What of the following neurotransmitters is not a monoamine?
A. Dopamine
B. Glutamate
C. Noradrenaline
D. 5-HT (Seratonin)
B
Glutamate is not a monoamine
In which nuclei is seratonin producted?
The raphe nuclei of the rostral group
What are some examples of monoamine oxidase inhibitors?
Phenelzine and Moclobemide
What is the mode of action of monoamine oxidase inhibitors?
Irreversable (Phenelzine) or reversable (Moclobemide) inhibitors of MAO- A and B
What are some side effects of monoamine oxidase inhibitors?
- Cheese reaction/hypertensive crisis- caused by MAO-A inhibition in gut and liver by irreversable drugs which prevents breakdown of dietary tyramine
- Potentiates effects of other drugs by decreasing their metabolism
- Insomnia
- Postural hypotension
- Peripheral oedema
Which of the following side effects are more likley to be caused by an SSRI than a tricyclic?
A. Blurred vision
B. Constipation
C. Dry mouth
D. Nausea
E. Urinary retention
D
Tricyclics are anticholinergic and so A, B, C, and E are all classic side effects
Which of the following antidepressants should be avoided in a 57 year old man with ischaemic heart disease who became depressed following an MI 2 months ago?
A. Citalopram
B. Fluoxetine
C. Imipramine
D. Mirtazapine
E. Sertraline
C
Avoid using imipramine in ischameic heart disease
What class do the following antidepressants belong to?
Imipramine, Dosulepin, Amitriptyline, Lofepramine
Tricyclic antidepressants
How do tricyclic antidepressants work?
Block the reuptake of monoamines (mainly noradrenaline and 5-HT) into presynaptic terminals. This means more is avaliable in the cleft
What are some side effects of tricyclic antidepressants?
- Anticholinergic= blurred vision, dry mouth, constipation, urinary retention
- Sedation
- Weight gain
- CV= postural hypotension, tachycardia, arrythmias
- Carditoxic in overdose
How do SSRIs work?
Selectively inhibit the reuptake of seratonin in the synaptic cleft leading to increased seratonin activity
What class of drugs do the following antidepressants belong to?
Fluoxetine, Citalopram, Sertraline
SSRIs
What are some common side effects of SSRIs?
- Nausea
- Headache
- Worsened anxiety
- Transient increase in self harm/ suicidal ideation <25
- Sweating and vivid dreams
- Sexual dysfunction
- Hyponatreamia (elderly)
- Discontinuation effects
How do SNRIs work and what are some examples?
Block the reuptake of monoamines (noradrenaline and 5-HT) into presynsaptic terminals.
Venlaxafine and Duloxetine
Similar side effects to SSRIs
What are the short and long term goals in treatment of Bipolar Disorder?
Acute treatment of symptoms- to reduce mood in episodes of mania and raise mood in episodes of depression
Long term treatment- to stabilise mood and prevent recurrence of both mania and depression (prophylaxis)
What of the following side effects would suggest lithium levels in the toxic range?
A. Ataxia
B. Hypothyroidism
C. Nausea
D. Polyuria
E. Tremor
A
Ataxia suggests toxic levels
The rest of the list are normal side effects
True or False?
Lithium is subject to extensive hepatic metabolism
False- not metabolised at all. Undergoes renal excretion
Lithium ions and sodium ions are indistinguishable to the renal tubules. What will the effect of dehydration be on lithium levels?
A. Decrease in lithium levels
B. Increase in lithium levels
C. No change in lithium levels
B
An increase in lithium levels. If dehydrated the tubules will absorb more Na to pull the water in and so will also absorb more lithium
What are the side effects of lithium?
- Dry mouth/ strange taste
- Polydipsia and polyuria
- Tremor
- Hypothyroidism
- Long term reduced renal function
- Nephropgenic diabetes insipidis
- Weight gain
What are some of the toxic effects of Lithium?
- Vommiting
- Diarrhoea
- Ataxia/ coarse termor
- Drowsiness / altered concious level
- Convuslions
- Coma
A 27 year old women is diagnosed with bipolar disorder. She hopes to get pregnant some time in the future. Which mood stabiliser is to be avoided?
A. Aripiprazole
B. Lamotrigine
C. Lithium
D. Quetiapine
E. Valproic Acid
E is contraindicated
What anticonvulsants are used as mood stabilisers in the treatment of BPD?
Valproic acid, Lamotrigine and Carbamazepine
What are the side effects of the anti-convulsants used as mood stabilisers?
- Valproate and carbamazepine - drowsiness, ataxia, CV effects, induces liver enzymes
- Valproate- teratogenicity (neural tube defects)
- Lamotrigine- very small risk of Stevens-Johnson syndrome