B6

Question 1

Diazepam

Answer 1

Benzodiapeine (linked to GABA-A receptor activation)

MoA: BRs lead to increasing the affinity of GABA for its receptor, enhancing its effects

Use: Affects muscle relaxation, anticonvulsant activity, motor coordination, and memory.

Used for anxiety + as a muscle relaxant

Question 2

Zoplicone

Answer 2

GABABZ agonist

Non-benzodiaepine hynotic

MoA: via by binding the α1, α2, α3 and α5 GABA-A containing receptors as full agonists modulating the GABABZ receptor chloride channel macromolecular complex. This enhances the inhibitory actions of GABA to produce the hypnotic and anxiolytic effects of zopiclone.

Use: Zopiclone is a non-benzodiazepine hypnotic indicated for the short-term treatment of insomnia.

Question 3

Donepezil

Answer 3

Reversible acetyl cholinesterase inhibitor.

MoA: Reversible inhibition of acetylcholinesterase, leading to an increase in acetylcholine at cholinergic synapses, enhancing cholinergic function.

Use: Dementia treatment, though has been used for Alzheimer’s disease.

Question 4

Memantine

Answer 4

Amantadine derivative, is a NMDA receptor antagonist.

Use: Memantine protects against chronically elevated concentrations of glutamate.

Use: Treatment of Dementia

Question 5

Gaviscon

Answer 5

Antacid

MoA: Depends on the formulation

Its main role is to act as an antacid, and as such it neutralize or buffers existing stomach acid, raising stomach acid pH. Gaviscon has no direct effect on stomach acid output. However double action Gaviscon can also prevent reflux and so reduce irritation of the oesophagus.

Use: Heartburn + indigestion

Question 6

Which type of meds are the following?

• Chlorpromazine
• Haloperidol
• Risperidone
• Clozapine

Answer 6

Antipsychotics

Question 7

Chlorpromazine

Answer 7

Phenothiazine based antipsychotic

Use: No longer used as an anti-psychotic drug.

Question 8

Haloperidol

Answer 8

Dopamine receptor antagonist

Use: A psychotropic agent, with sedative and antiemetic activity used to treat schizophrenia.

Question 9

Risperidone

Answer 9

Risperidone is an atypical antipsychotic (multi-target).

Use: Treatment of delusional psychosis, bipolar disorder, and psychotic depression.

Question 10

Clozapine

Answer 10

Psychotropic agent (selective monoaminergic antagonist with high affinity for 5HT2, and D2 receptors).

Use: Clozapine is indicated for the treatment of schizophrenia.

Question 11

Amitriptyline

Answer 11

Noradrenaline/5HT reuptake inhibitor.

Use: Amitriptyline, is a sedating antidepressant, and so can aide sleep patterns..

Question 12

Citalopram

Answer 12

Selective serotonin reuptake Inhibitor (SSRI).

Use: Citalopram is used to treat depression associated with mood disorders.

Question 13

SSRI MoA

Answer 13

Blocking the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, with little effect on norepinephrine and dopamine reuptake. This enhances the actions of serotonin on 5HT1A autoreceptors.

SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs.

Question 14

Venlafaxine

Answer 14

Serotonin reuptake inhibitor

Question 15

Phenelzine

Answer 15

Monoamine oxidase inhibitor.

MoA: irreversibly inhibit monoamine oxidase (MAO)

As phenelzine inhibits MAO, it, therefore, increases the concentration of free amines, most specifically serotonin and norepinephrine. MAO-A inhibition is thought to be more relevant to antidepressant activity as selective MAO-B inhibitors (selegiline), have no antidepressant effects.

Question 16

Methylphenidate

Answer 16

Noradrenaline/dopamine releaser.

Methylphenidate is a CNS stimulant.

Use: treat attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), and narcolepsy.

MoA: Inhibits the sodium dependent dopamine transporter, and therefore blocks dopamine uptake in central adrenergic neurons. This causes increased sympathomimetic activity in the CNS.

Question 17

Lithium

Answer 17

Mood stabilising agent

MoA: The active principle is the Li+, which can displace K+, Na+ and even Ca2+, in several critical neuronal enzymes and neurotransmitter.

Use: Treatment of bipolar disorder, as it counteracts both mania and depression.

Question 18

Buspirone

Answer 18

5HT partial receptor agonist

Use: Buspirone is used to treat generalized anxiety.

• It has benefits in that it does not cause sedation (drowsiness) tolerance or physical dependence.
• It does not cause anticonvulsant or muscle relaxant effects.

Question 19

Thiopental

Answer 19

GABA enhancer
Thiopental is rapid onset short-acting barbiturate

MoA: Binds the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The effect of this is that the post-synaptic inhibitory effect of GABA in the thalamus is prolonged

Recovery after a small dose is rapid, however, repeated IV doses lead to prolonged anaesthesia as fatty tissues act as a reservoir of Thiopental, which is then released over a prolonged period of time.

Use: Hypnosis and anaesthesia, but not analgesia.