Psychopharmacology Flashcards
MOA of Mirtazapine
Noradrenaline and serotonin specific antidepressant (NaSSa)
5HT2 antagonist, 5HT3 antagonist, H1 antagonist, alpha 1 and alpha 2 antagonist, moderate muscarinic antagonist
MOA of Venlafaxine and Duloxetine
Serotonin and noradrenaline reuptake inhibitor (SNRI)
MOA of Reboxetine
Noradrenaline reuptake inhibitor (NaRI)
MOA of St John’s Wart
Weak MAOI and weak SNRI (also considered by some to be a weak SSRI)
MOA of Trazodone
- Serotonin antagonist and reuptake inhibitor.
Blocks SERT and also antagonist at 5HT2A and 5HT2C.
SERT blockage at 5HT1A (antidepressant effect)
SERT at 5HT2A and 5HT2C (blocks side effects such as insomnia, sexual dysfunction, and anxiety).
MOA of Moclobemide
Reversible inhibitor of monoamine oxidase type A
MOA of Agomelatine
Melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist
MOA of Bupropion
Norepinephrine-dopamine reuptake inhibitor (NDRI), and nicotinic acetylcholine receptor antagonist
MOA of Donepezil
Reversible acetylcholinesterase inhibitor
MOA of Rivastigmine
Reversible acetylcholinesterase inhibitor and butyrylcholinesterase inhibitor
- MOA of Galantamine
- CYP?
- Side effects of Group?
Reversible acetylcholinesterase inhibitor and binds allosterically to the nicotinic acetylcholine receptor
CYP 2D6 and 3A4
GI billed, bradycardia, urinary incontinence, ++ COPD sx, ++ seizure risk.
- MOA of Memantine?
- Half life?
Non-competitive NMDA antagonist
60-80 hours
Non hepatic metabolism
MOA of Valporate?
GABA agonist and NMDA antagonist
Kane did what?
introduced clozapine into clinical practice
Medina discovered What?
Meduna - metrazol therapy
Carlson did what?
Carlsson - developed the first SSRI
Blackwell described what?
Blackwell - first described the ‘cheese effect’ seen in MAOI use
Cade discovered what?
Cade - discovered lithium’s beneficial effect in mania
Kline discovered what?
Kline - discovered use of iproniazid (MAOI)
Charpentier synthesised what?
Charpentier - synthesised chlorpromazine
Delay and Deniker introduced what?
Delay and Deniker - introduced chlorpromazine as a treatment for schizophrenia
Kuhn discovered what?
Kuhn - discovered the antidepressant effects of imipramine
Cerletti and Bini first did what?
Cerletti (and Bini) - first use of ECT
Lurie coined what term?
Lurie - coined the term ‘antidepressant’
Sakes developed what treatment?
Sakel - insulin shock therapy
Moniz developed what?
Moniz - frontal lobotomy for psychosis
Definition of agonist (full)
Medication that binds to a specific receptor producing an effect Identical to that usually produced by the neurotransmitter affecting the receptor.
Full agonists include opioids and benzodiazepines at the Gabba receptor complex.
Antagonist
A compound that binds to a receptor that blocks or reduces the action of another substance at the receptor site.
Drugs for schizophrenia treatment (D2 receptor blockers)
Competitive antagonist
Antagonist that reversibility binds to the receptor at the same binding site as the Agonist but does not produce a response.
Partial agonist
A compound that even when fully occupying the receptor, only elicits a partial Pharmacological response.
Aripiprazole
Buspirone 5HT1A
Buprenorphine partial opioid agonist
Inverse agonist
Is an agent that binds to the same receptor as an agonist for that receptor, but produces opposite pharmacological effect.
Irreversible antagonist
These antagonist find irreversibly to the target site for example older MAOIs
Potency
The amount of drugs needed to produce a particular effect compared with another standard drug with similar receptor profile
Affinity
The ability of the drug to bind to its receptor
Efficacy
The ability of the drug to produce expected response. To drugs maybe equally efficacious but not equally potent
In pharmacokinetics what effects absorption ?
Factors that can inhibit absorption include food gastric acid or changes in intestinal motility. The ziprasidone is the only antipsychotic his absorption is enhanced by food
What is bio availability?
When the drug is given what is the most bioavailable form?
The fraction of the dose that reaches systemic circulation. When a drug is given IV the bio availability is 100% this is not the case with other modes of administration.
What is bioequivalence?
The measure of comparatbility of plasma levels of two different formulations of the same active compound when given at the same dose and by the same route of administration
How does protein binding affect volume of distribution and plasma concentrations of a medication?
Protein binding affects the volume of distribution. The higher the volume of distribution lower is the plasma concentration.
Warfarin is highly protein bound. What drug in psychiatry can displace warfarin and therefore cause an increase in bleeding risk?
In psychiatry sodium valproate is highly protein bound and can displace warfarin. They operate can also displace carbamazepine phenytoin and topiramate
Define first order kinetics
When a constant fraction of drug is eliminated pay unit time. The rate of clearance depends only on drug concentration. Most psychotropics follow these kinetics.
Define zero order kinetics
And give examples of four types of zero order kinetic medications.
When the clearance system becomes saturated such that a constant amount not a fraction is eliminated. Lithium, depot medications, alcohol and phenytoin follow zero order kinetics
What are the two main phases of drug metabolism?
Phase 1 includes oxidation, reduction and hydrolysis.
Phase 2 consists of conjugation reactions such as glucorinidation and sulphate formation .that can easily be excreted and bile or urine
Name three drugs and undergo direct phase 2 reactions without undergoing a phase one reaction metabolism.
Lorazepam
OxazePam
Temazepam
Define steady state and how many half lives it takes to get to this.
Steady state is reached when the amount of drug administered every day is exactly counterbalance by the amount of drug eliminated.
It takes between 4 to 5 half life’s to reach steady state level.
Loading doses can be used to achieve steady-state more rapidly for example valproate.
Define therapeutic index and given example of the medication that has a low therapeutic index.
The ratio of the minimum plasma concentration causing toxic effects to that of a therapeutic affect. Lithium has a low therapeutic index
Define therapeutic window
The range of plasma concentration within which the medication shows a therapeutic affect
Name the effects of ketamine and any withdrawal features.
Euphoria, disassociation, ataxia, hallucinations, muscle rigidity.
No recognise withdrawal syndrome.
What are the symptoms of LSD use?
Perceptual changes, pupil dilation, tachycardia, sweating, palpitations, tremor, incoordination
What are the effects of cannabis and what are the withdrawal features ?
Relaxation, intense sensory experience, paranoia, anxiety, injected conjunctivae.
Withdrawal features include insomnia, reduced appetite, irritability.
What are the effects of MDMA and what are the withdrawal features?
Increased energy, increase sweating, jaw clenching, euphoria, and hunt sociability, increase response to touch.
Withdrawal features include depression, insomnia, depersonalisation, Derealisation.
What are the effects of amphetamine and What are the withdrawal features?
Increased energy, insomnia, hyperactivity, euphoria, paranoia, reduced appetite.
Withdrawal features include hypersomnia, hyperphagia, depression, irritability, agitation, vivid dreams, increased appetite.
What effects of heroine and what are the withdrawal features?
Euphoria, drowsiness, constipation, pupil constriction, respiratory depression.
Withdrawal features include piloerection, insomnia, restlessness, Dilated Pupils, yawning, sweating, abdominal cramps.
Name 4 secondary amines
Desipramide
Nortriptyline
Protriptyline
Amoxapine
Name Tertiary amines (8)
2 line
4 mine
2 pin
Amytriptyline Imipramine Dothiepin Doxepin Clomipramine Lofepramine Trimipramine Butriptyline
What is clozapine mainly metabolised by?
CYP1A2
