B6 Flashcards
Diazepam
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
Zoplicone
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.
Donepezil
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.
Memantine
Amantadine derivative, is a NMDA receptor antagonist.
Use: Memantine protects against chronically elevated concentrations of glutamate.
Use: Treatment of Dementia
Gaviscon
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
Which type of meds are the following?
- Chlorpromazine
- Haloperidol
- Risperidone
- Clozapine
Antipsychotics
Chlorpromazine
Phenothiazine based antipsychotic
Use: No longer used as an anti-psychotic drug.
Haloperidol
Dopamine receptor antagonist
Use: A psychotropic agent, with sedative and antiemetic activity used to treat schizophrenia.
Risperidone
Risperidone is an atypical antipsychotic (multi-target).
Use: Treatment of delusional psychosis, bipolar disorder, and psychotic depression.
Clozapine
Psychotropic agent (selective monoaminergic antagonist with high affinity for 5HT2, and D2 receptors).
Use: Clozapine is indicated for the treatment of schizophrenia.
Amitriptyline
Noradrenaline/5HT reuptake inhibitor.
Use: Amitriptyline, is a sedating antidepressant, and so can aide sleep patterns..
Citalopram
Selective serotonin reuptake Inhibitor (SSRI).
Use: Citalopram is used to treat depression associated with mood disorders.
SSRI MoA
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.
Venlafaxine
Serotonin reuptake inhibitor
Phenelzine
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.
Methylphenidate
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.
Lithium
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.
Buspirone
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.
Thiopental
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.
