BB2 Drugs Flashcards
State the class of drugs that selegiline belongs to [1]
MOA inhibitor
Name the 7 treatments for addiction [7]
‘Detoxification’
Aversion therapies (Antabuse – disulfiram, acute hang-over after ingesting alcohol via acetaldehyde)
Motivational therapies (groups, AA)
Cognitive-behavioural treatments (coping skills)
Drug substitutes (methadone, NRT)
Treatments for withdrawal relief (clonidine), antagonists (naltrexone), partial agonists (varenicline) etc.
Psychedelics (LSD, Psilocybin) – promise in alcoholism
Name two future pyschedelic drugs that could be used for treatment for addiciton? [2]
Not on drug list
LSD, Psilocybin
Describe how antabuse - disulfiram works to stop
(on the drugs list)
inhibits the enzyme acetaldehyde dehydrogenase, causing many of the effects of a hangover to be felt immediately following alcohol consumption
Which drug is methadone a substitute for? [1]
Heroin
How does Varenicline work to treat nicotine addiction? [1]
Not on drug list
is a selective partial agonist that stimulates the a4b2 nicotine cholinergic receptor
Name a drug used to provide withdrawal relief and its MoA [2]
Not on drug list
Clonidine
Alpha2 agonist used to treat hypertension and addiction
Name a drug that causes patients to temporarily leave vegetative state [1]
Zolpidem
Zolpidem is a drug that causes patients to temporarily leave vegetative state. What is its MoA?
GABA-A antagonist
GABA-A agonist
NMDA Glutamate antagonist
NMDA Glutamate agonist
AMPA Glutamate antagonist
Zolpidem is a drug that causes patients to temporarily leave vegetative state. What is its MoA?
GABA-A antagonist
GABA-A agonist
NMDA Glutamate antagonist
NMDA Glutamate agonist
AMPA Glutamate antagonist
Amantadine helps patients recover from TBI. What is its mechanism of action?
GABA-A antagonist
GABA-A agonist
NMDA Glutamate antagonist
NMDA Glutamate agonist
AMPA Glutamate antagonist
Amantadine helps patients recover from TBI. What is its mechanism of action?
GABA-A antagonist
GABA-A agonist
NMDA Glutamate antagonist AND blocks dopamine reuptake
NMDA Glutamate agonist
AMPA Glutamate antagonist
PVS treatment
Name a drug and describe MoA that may help to recover [3]
Amantadine
* NMDA receptor antagonist and block dopaminergic reuptake
* Improves functional recovery rate
PVS treatment
What is the hypothesis for zolpidem treatment?
Loss of active inhibition from striatum allows GPi to tonically inhibit thalamus and pedunculopontine nucleus, so thalamocortical overactivity
Future treatment for PVS? [1]
Vagal nerve stimulation:
Treatment strategies in AD
Name the drug class [1] and 3 drug examples you prescribe for mild - moderate AD? [3]
Name the drug class [1] and 3 drug examples you prescribe for severe AD? [1]
Mild-Moderate AD:
* Acetylcholinesterase inhibitors(e.g. donepezil, galantamine and rivastigmine)
Severe AD:
* NMDA receptor antagonists (e.g. memantine)
Which of the following treatments for AD is a NMDA glutamate receptor agonist?
memantine
donepezil
galantamine
rivastigmine
Which of the following treatments for AD is a NMDA glutamate receptor agonist?
memantine
donepezil
galantamine
rivastigmine
Which of the following is used for patients with severe AD?
memantine
donepezil
galantamine
rivastigmine
Which of the following is used for patients with severe AD?
memantine
donepezil
galantamine
rivastigmine
donepezil, galantamine & rivastigmine all belong to which drug class? [1]
Acetylcholinesterase inhibitor
rivastigmine is used to treat which pathology?
Parkinsons Disease
Alzeimers Disease
Huntingdons Disease
Epilepsy
rivastigmine is used to treat which pathology?
Parkinsons Disease
Alzeimers Disease
Huntingdons Disease
Epilepsy
Name two drugs used for seizure prophylaxis [2]
Phenytoin
Levetiracetam
How could you manage severe ICP:
Acutely [2]
Long term [1]
Short term:
* mannitol
* hypertonic saline
(shift of water from extravascular space to intravascular space across the BBB-controversy which therapy is better.)
Long term:
* extraventricular drain/ external ventricular drain (EVD) or ventriculostomy
Management of epilepsy:
Name 3 drugs target the inactive (intermediate) state of Na channels
Phenytoin
Carbamazepine
Sodium valproate
Phentoin is an anti-seizure drug that targets which channel?
GABA-A
NMDA Glutamate
AMPA Glutamate
Na+
CA2+
Phentoin is an anti-seizure drug that targets which channel?
GABA-A
NMDA Glutamate
AMPA Glutamate
Na+
CA2+
Which of the following should not be used to treat an absence seizure as they may exacerbate it?
Sodium valproate
Lamotrigine
Phenytoin
Pregabalin
Ethosuximide
Which of the following should not be used to treat an absence seizure as they may exacerbate it?
Sodium valproate
Lamotrigine
Phenytoin
Pregabalin
Ethosuximide
Which of the following exhibits zero order kinetics?
Sodium valproate
Lamotrigine
Phenytoin
Pregabalin
Ethosuximide
Which of the following exhibits zero order kinetics?
Sodium valproate
Lamotrigine
Phenytoin
Pregabalin
Ethosuximide
Name three calcium channels that are used as anti-epileptic drugs [3]
Ethosuximide
Gabapentin (in the PBL)
pregabalin (in the PBL)
Q
AEDs
What type of drug class does phenobarbitone and stiripentol belong to? [1]
What is MoA? [1]
phenobarbitone and stiripentol:
Drug class: Barbiturates: GABAA receptor positive allosteric modulators
. Phenobarbitone (leads to microsomal enzyme induction)
Enhances the duration of GABA channel opening. (more GABA; causes more inhibition
Which drug inhibits GABA metabolism? [1]
Vigabatrin
Which drug class increases the frequency of the opening of GABA channels?
Benzodiazepines
Barbiturates
Sulfonamides
GABA agonists
Which drug class increases the frequency of the opening of GABA channels?
Benzodiazepines
Barbiturates
Sulfonamides
GABA agonists
Which drug class increases the duration of the opening of GABA channels?
Benzodiazepines
Barbiturates
Sulfonamides
GABA agonists
Which drug class increases the duration of the opening of GABA channels?
Benzodiazepines
Barbiturates
Sulfonamides
GABA agonists
Which of the following inhibits GABA transaminase to prevent GABA breakdown
Vigabatrin
Levetiracetam
Phenobarbitone
Tiagabine
Which of the following inhibits GABA transaminase to prevent GABA breakdown
Vigabatrin
Levetiracetam
Phenobarbitone
Tiagabine
AEDs
Which of the following targets GAT-1 transporter to inhibit GABA reuptake
Vigabatrin
Levetiracetam
Phenobarbitone
Tiagabine
Which of the following targets GAT-1 transporter to inhibit GABA reuptake
Vigabatrin
Levetiracetam
Phenobarbitone
Tiagabine
Status elipeticus is a medical emergency. Name two drugs used to treat this conditon [2]
Lorezepam (IV)
Diazepam (IV)
Alternatives to AEDs
Name 3 surgical procedures that could be used to treat epilepsy [3]
Lobe resection
Corpus callasotomy (reduces propogation of seizures from one cerebral hemisphere to the next)
Functional hemispherectomy
Alternatives to AEDs
Name a type of diet that could help epilepsy [1]
Name a drug class for a potential new AED [1]
Keto diet
Cannabidiol
Which of the following type of channel does pregabalin target?
Ca2+
GABA
Na+
Glutamate
Which of the following type of channel does pregabalin target?
Ca2+
GABA
Na+
Glutamate
Name a drug that predominately blocks Na+ channels, but also acts on Ca2+ channels [ and causes the presynaptic inhibition of glutamate release.
Lamotrigine
(hint: tri gated?)
AEDs
Focal Seizures Treatment:
First line: [] or []
Second line: [] or []
First line: carbamazepine or lamotrigine
Second line: sodium valproate or levetiracetam
Management of tonic-clonic seizures is with:
First line: []
Second line: [] or []
Management of tonic-clonic seizures is with:
First line: sodium valproate
Second line: lamotrigine or carbamazepine
Which drugs are used for absence seizures? [2]
ethosuximide, sodium valproate
Myoclonic seizures:
First line: [1]
Other options: [3]
First line: sodium valproate
Other options: lamotrigine, levetiracetam or topiramate
Describe the MoA of sodium channel active drugs like phenytoin and carbamazepine [1]
Stabilises Na+ channels inactivated state to decrease excitability
Primary headaches
Treatment of tension-type headaches [2]
- Take painkillers for symptoms
- Find root causes and treat
Name acute [2] and prophylactic [1] treatment for cluster headaches
Acute:
* oxygen (15L/min 100% through non-rebreather mask – acts as vasoconstrictor);
* -triptans
Prophylactic
* : has to be quick. High dose of verapamil
Where do acute [1] and chronic [1] treatments for migraines target?
Acute:
Acute medication given for migraine primarily acts peripherally, at the trigeminal ganglion
Preventive medication for migraine acts more centrally (i.e. the trigeminal nucleus caudalis)
What drug classes are used to acutely treat migraine? [3]
Triptans: (5HT1D/B agonists)
* Vasoconstrictive Agents
Ditans (5HT1F agonists)
* Neurally Active Anti-Migraine Agent
Gepants: small molecule CGRP receptor antagonists
Name first line treatment for migraine? [1]
Sumatriptan
Describe MoA of triptans [1]
Where are 3 possible sites of action? [3]
Triptans:
* 5-HT1D/B agonists.
* 3 possible sites of action: 1. cranial vasoconstriction, 2. peripheral neuronal inhibition and 3. inhibition of transmission through second order neurones of the trigeminal ganglion.
SCN9A codes for which of the following
TRPM8
TRPV1
ASICS
Nav1.7
SCN9A codes for which of the following
TRPM8
TRPV1
ASICS
Nav1.7
Antiplatelet therapy for stroke? [3]
Aspirin
Aspirin & Clopidogrel
Aspirin and Dipyridamole
What type of family of antidepressants are clomipramine, imipramine, desipramine, amitriptyline, nortriptyline and protriptyline? [1]
TRICYCLIC ANTIDEPRESSANTS (TCAs)
Describe the MoA of TCAs [2]
- Inhibit reuptake of amines on the presynaptic terminal, so 5HT or NA cannot be taken back into neuron
Important AEs of TCAs? [4]
- Dangerous (cardiotoxic) in overdose
- Anti-cholinergic: dry mouth; blurred vision, constipation, urinary retention, aggravation of narrow angle glaucoma, fatigue, postural hypotension, dizziness, loss of libido, arrhythmias
- Antihistaminic: sedation, weight gain.
- Block alpha 1 adrenoreceptors: orthostatic hypotension - blood pressure drops on standing, cardiac effects
As a result aren’t the first choice!
Phenelzine, tranylcypromine belong to which drug class? [1]
MONOAMINE OXIDASE INHIBITORS
Describe the MoA of monoamine oxidase inhibitors such Phenelzine, tranylcypromine [1]
Which type of food interact with MOIs? [1]
Irreversible inhibition of the enzyme monoamine oxidase [1]
Interactions with tyramine-containing food (mature cheese, pickled fish and meat, red wine, beer, broad bean pods, yeast extract)- restrictions continue at least 2 weeks after discontinuation
Why do you have to wait approx. 2 weeks if you want to change treatment away from MAOIs? [1]
The drugs bind irreversibly: wait for at least 50% of enzymes have been replaced to change treatment
What type of drug class are citalopram, fluoxetine, paroxetine sertraline? [1]
SELECTIVE SEROTONIN REUPTAKE INHIBITORS
Which is the most selective SSRI?
citalopram
sertraline
fluoxetine
paroxetine
Which is the most selective SSRI?
citalopram
sertraline
fluoxetine
paroxetine
Moclobemide belongs to which drug class? [1]
REVERSIBLE MONOAMINE OXIDASE INHIBITOR
Which is the safest monoamine oxidisase inhibitor?
Moclobemide
Phenelzine
Tranylcypromine
Which is the safest monoamine oxidisase inhibitor?
Moclobemide (reversible MOAIs)
Phenelzine (irreversible MOAIs)
Tranylcypromine (irreversible MOAIs)
Anti-depressants
Describe MoA of Agomelatine [2]
Why is this potentially a really good drug? [2]
MoA:
* Agonist at melatonin MT1 & MT2 receptors: important for sleep control
* Antagonist of 5-HT2 receptors
Benefits of Agomelatine:
* improves sleep quality
* less sexual dysfunction than SSRIs;
* anxiolytic effects
* no ‘discontinuation syndrome’
The treatment with the SNRI [] reduces the increased Default Mode Network
connectivity seen in depression
The treatment with the SNRI duloxetine reduces the increased Default Mode Network connectivity seen in depression
How long do antidepressant drugs take to cause action in the body?
Although the level of drug increases in plasma soon after the patient starts taking the medication, there is a delayed onset of action of 1-2 weeks
What changes to drug treatment may trigger antidepressant drug discontinuation syndrome? [3]
What are the symptoms?
A condition that can occur after:
- a decrease in the dose of drug taken
- an interruption of treatment
- abrupt cessation of treatment
Insomnia
Anxiety
Nausea
Headaches
Electric shock sensations
Agitation
Mood swings
Diarrhoea/abdominal cramps
What drug do you give to manage bipolar disorder? [1]
What needs to be considered about this when adminsitering? [1]
Lithium
Narrow therapeutic margin
Which organs need to be monitored when giving lithium for bipolar disorder? [2]
Renal and thyroid function must be checked before treatment (and then at regular intervals during maintenance treatment)
Apart from inhibiting the reuptake of amines, which other receptors do TCAs bind to? [3]
Why is this problematic? [1]
Bind to:
* H1 receptors
* muscarinic receptors
* α1 and α2 adrenoceptors
Causes wide ranging side effects
Look up which TCAs need to know
Which is the first line drug choice for treating depression
TCAs
SNRIs
MAOIs
SSRIs
Which is the first line drug choice for treating depression
TCAs
SNRIs
MAOIs
SSRIs
Which class of drugs can you not use / creates lots of AEs if they eat food like red wine, cheese or mature cheese?
TCAs
SNRIs
MAOIs
SSRIs
Which class of drugs can you not use / creates lots of AEs if they eat food like red wine, cheese or mature cheese?
TCAs
SNRIs
MAOIs
SSRIs
What is the benefit of using SSRIs (citalopram, fluoxetine, paroxetine) with regards to AEs [3]
No anticholinergic activity
No cardiotoxic effects
Safe in overdose
AEs of SSRIs?
· Nausea vomiting
· Dry mouth
· Headache
· Asthenia
· Dizziness
· Anorexia
· Weight loss
· Nervousness
· Tremor
· Convulsions
· Sexual dysfunction
Which of the following is a reversible MAOI?
phenelzine
moclobemide
tranylcypromine
agomelatine
Which of the following is a reversible MAOI?
phenelzine
moclobemide
tranylcypromine
agomelatine
What are the different targets for reverible MAOIs compared to irreversible MOAIs? [2]
Describe the benefits of reversible MAOIs compared to irreversible MAOs [2]
Drug targets:
* Reversible MAOI targets: MOA-A
* Irreversible MAOI targets: MAOA versus MAOB
Differences:
* Reversible is safer than irreversible MAOIs
* Can switch drug classes quicker
Which of the following has the quickest onset?
TCAs
SNRIs
MAOIs
SSRIs
Which of the following has the quickest onset?
TCAs
SNRIs : duloxetine and venlafaxine
MAOIs
SSRIs
Which of the following drug class cause discontinuation syndrome
TCAs
SNRIs
MAOIs
SSRIs
Which of the following drug class cause discontinuation syndrome
TCAs
SNRIs
MAOIs
SSRIs
Depression drugs
Name a noradrenaline reuptake inhibitor used for depression treatment [1]
Reboxetine
Which of the following is noradrenaline reuptake inhibitor?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Which of the following is noradrenaline reuptake inhibitor?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Which of the following is noradrenergic and specific serotonergic antidepressants (NaSSA)?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Which of the following is noradrenergic and specific serotonergic antidepressants?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Which of the following is a serotonergic antagonist and reuptake inhibitor (SARI)?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Which of the following is a serotonergic antagonist and reuptake inhibito (SARI)?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Depression Drugs
Name a serotonergic antagonist and reuptake inhibito (SARI) [1]
Trazodone
Depression drugs
Name a noradrenergic and specific serotonergic antidepressant (NaSSA) [1]
Mirtazapine
Which of the following reduces the increased default mode network connectivity seen in depression?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Which of the following reduces the increased default mode network connectivity seen in depression?
Duloxetine
Reboxetine
Mirtazapine
Tianeptine
Trazodone
Explain why there is a delayed action for anti-depressant drug action for TCAs [4]
The immediate increase in synaptic concentration of amines
may lead to activation of somatic neuronal autoreceptors
The activated autoreceptors decrease firing of the neurones
During the first weeks of treatment the autoreceptors desensitize
The neurones will return subsequently to the normal firing rate
The inhibition of reuptake continues and the level of amines
continues to be high, resulting in full efficacy
Apart from lithium, name two other drugs used as mood stabilisers [2]
Carbamazepine, sodium valproate
Name two risks of using antidepressant drugs used in bipolar disorder to treat periods of depression? [2]
can precipitate manic episodes or mixed
affective states
induce an increased frequency
in mood change cycles
Which drug class has the highest risk for mania if used to treat depression in bipolar patients?
TCAs
SNRIs
MAOIs
SSRIs
Which drug class has the highest risk for mania if used to treat depression in bipolar patients?
TCAs
SNRIs
MAOIs
SSRIs
Explain the three phases of antidepressant treatment [3]
Acute Treatment
- First 6-12 weeks of treatment; aims at remission (control of symptoms)
- Inadequate early response is associated with poor prognosis
Continuation Treatment
- for 6 months after full symptom control; to maintain remission status and prevent relapse
Maintenance Treatment
- Aims at prevention of recurrence of a further episode of depression.
- Indicated when higher risk of these recurrence; “maintenance dose”.
Name 4 non-pharmacological approaches for mood disorders
Electroconvulsive therapy (treatment-refractory severe depression with suicide risk)
Cognitive behavioural therapy (CBT) (can augment the effects of pharmacological treatment)
Vagal nerve stimulation (especially in chronic depression)
Deep brain stimulation (DBS); subcallosal cingulate white matter – Brodmann area 25)
Which area is the DBS target for treating depression? [1]
What the is the Broadmann area?
21
22
23
24
25
Which area is the DBS target for treating depression: subgenual cingulate cortex
What the is the Broadmann area?
21
22
23
24
25
Name two new therapeutic developments for depression [2]
What types of depression do they speficifically treat? [2]
What are their MoAs? [2]
Esketamine:
* NMDA glutamate receptor antagonist
* treatment-resistant depression
Brexanolone:
* progesterone-related compound, positive modulator of GABAA receptors
* approved for post-partum depression
Which of the following would be used to treat treatment resistant depression
Duloxetine
Esketamine
Mirtazapine
Brexanalone
Trazodone
Which of the following would be used to treat treatment resistant depression
Duloxetine
Esketamine
Mirtazapine
Brexanalone
Trazodone
Which of the following would be used to treat post-partum depression
Duloxetine
Esketamine
Mirtazapine
Brexanalone
Trazodone
Which of the following would be used to treat post-partum depression
Duloxetine
Esketamine
Mirtazapine
Brexanalone
Trazodone
Ketamine blocks NMDA glutamate receptors on GABA neurons.
Which receptors does this have an effect on and what is this response? [2]
Enhances transmission at the glutamatergic synapse: enhances signaling through AMPA glutamate receptors and also increases the level of brain-derived neurotrophic factor, BDNF
Which of the following class of drug causes this symptom?
TCAs
SNRIs
MAOIs
SSRIs
(orthostatic hypotension)
Which of the following class of drug causes this symptom?
TCAs: due to blocking of Block alpha 1 adrenoreceptors
SNRIs
MAOIs
SSRIs
TCAs are toxic to which part of the body? [1]
Cardiotoxic: Blockade of fast sodium channels in myocardial cells slows the action potential and provides a membrane stabilizing effect. The characteristic QRS prolongation seen in TCA overdose occurs secondary to prolongation of phase “0” of the myocardial action potential. T
Which of the following is the most cardiotoxic?
Amitriptyline
Nortriptyline
Citalopram
Sertraline
Fluoxetine
Which of the following is the most cardiotoxic?
Amitriptyline
Nortriptyline
Citalopram
Sertraline
Fluoxetine