Basic Pharmacology

Question 1

What drugs are found within the class of benzisoxazoles?

Answer 1

Risperidone and its active metabolite Palliperidone

Question 2

Name a reversible MAOI

Answer 2

Moclobemide (rMAO-A inhibitor) - reversible MAOIs are preferable given there is less tendency for the cheese reaction

Question 2

Rauwolfia Serpentina was the natural source of which drug?

Answer 2

Reserpine

(Rauwolfia Serpentina is also known as indian snakeroot plan or Sarpaganda)

Question 3

Haloperidol, droperidol and benperidol are which class of drugs

Answer 3

Butyrophenones - these are high potency and have high capacity for EPSEs

Question 4

Delay and Deniker discovered which historical psychiatric drug?

Answer 4

Chlorpromazine

• the sedating antipsychotic delayed peoples cognition and put denks in the mind

Delay and Deniker worked under the supervision of Paul Charpentier

Question 5

Kane led a trial those proved the high clinical effectiveness of which drug?

Answer 5

Kane - Harry Kane has a high clinical effectiveness

Kane proved clozapine was highly clinically effective - outperformed haloperidol and chlorpromazine in a trial of treatment resistant schizophrenia

Question 6

Bowden led a trial showing the effectiveness of which drug agent for acute mania?

Answer 6

Sodium Valproate (Divalproex)

Question 7

Name some pharmacological agents that belong to the class of Thioxamines and what are their side effects?

Answer 7

Zuclopenthixol and Flupenthixol

These agents are moderately sedating, have antimuscarinic properties and extra-pyramidal effects (moderate)

Question 8

What drugs should psychiatrists be most mindful of the effects of QTc prolongation?

Answer 8

Haloperidol, Sertindole, Thioridazine

Question 9

What drug used in short courses for anxiety is a 5-HT1A partial agonist?

Answer 9

Buspirone - it is azaspirone

Question 10

Olanzapine is which class of drugs?

Answer 10

Thienobenzodiazepine
- a relation of clozapine which is a tricyclic dibenzodiazepine

Question 11

How do secondary amines compare to tertiary amines?

Answer 11

Secondary amines include:
- Nortryptiline, Desipramine, Amoxapine, Protryptyline and Duloxetine

These drugs are more potent mg to mg, have more noradrenergic effects reduced anti-cholinergic and reduced histaminic

Tertiary amines boost serotonin and noradrenaline but have more side effects include:
Amitriptyline, Lofepramine, Imipramine, Clomipramine, Dosulepin (Dothiepin), Doxepin, Trimipramine, Butriptyline

Question 12

Seizure risk is particularly higher for which type of drug?

Answer 12

Buproprion - it is an aminoketone

Doses < 300mg a day with slow releases decrease risk significantly

Question 13

Name a drug for the treatment of hypersexuality and paraphilias?

Answer 13

Cyproterone acetate - an anti-androgen prevents testosterone binding to the receptor (testosterone antagonist)

Question 14

A drug which acts a functional glutamatergic NMDA antagonist but increases GABA-ergic function is

Answer 14

Taurine Synthetic Analgoue - Acamprosate

Question 15

Name some advantages to Escitalopram > Citalopram?

Answer 15

Less histaminergic side effects
Not potency for QTc prolongation at higher doses

More effective - likely due to removal of more unrealiable R enantiomer

Question 16

Controversial new treatments for Alzheimer’s have targeted?

Answer 16

BACE1 - beta secretase enzymes

The enzymatic form that converts APP to Beta amyloid plaques

Question 17

Classify the differential mechanisms of Donepezil, Rivastigmine, Galantamine and Memantine

Answer 17

Donepezil - selective and reversible inhibitor of AChE

Rivastigmine - non-competitive and reversible inhibitor of AChE

Galantamine - competitive and reversible inhibitor of AChE

NMDA receptor antagonist - non-competitive

Question 18

Compare and contrast the pros and cons of common dementia drugs?

Answer 18

Donepezil - better tolerated of AChE inhibitors

Rivastigmine - acts on both butylcholine-esterase and acetylcholine-esterate. However more GI side effects due to peripheral effects and delays amount and rate of food absorption

Galantamine - also a nicotene receptor agonist. More GI and neuropsych side effects than Donepezil. Delays rate but not extent of food absorption

Memantine - also 5HT3 receptor antagonist. Non-hepatic metabolism

Question 19

Zopiclone belongs to which pharmacological class

Answer 19

Cyclopyyrolone

Question 20

What may be used to manage symptoms of opiod withdrawal?

Answer 20

Lofexidine - alpha-2 adrenergic agonist

Question 21

Who discovered Imipramine (1958)

Answer 21

Kuhn - the first TCA that was developed for the treatment of endogenous depression.

Amitriptyline was later introduced

Question 22

Who discovered Haloperidol from Pethidine?

Answer 22

Janssen - antipsychotics became known as major tranquilisers with benzodiazepines/barbituates known as minor tranquilisers

Janssen later also synthesised risperidone

Question 23

Who loves cheese

Answer 23

Blackwell - discovered the cheese reaction of MAOIs

Question 24

Amisulpride and sulpride belong to which class of psychotropic medications?

Answer 24

Substituted benzamides

Question 25

Name an antipsychotics that is a…

a) Dibenzodiazepines
b) Dibenzothiazepine
c) Thienobenzodiazepine

Answer 25

a) Cloazapine is a dibenzodiazepine

b) Quetiapine is dibenzothiazepine

c) Olanzapine is a thienobenzodiazepine

Question 26

Which anti-depressants are hydrazine derivatives?

Answer 26

Phenelzine, Isocarboxazid

Question 27

How do Mirtazapine and Mianeserin work?

Answer 27

Noradrenaline and specific serotonin antagonist

Question 28

Agomelatine works as a…

Answer 28

Noradrenaline and Dopamine disinhibitor (later down the line)

Question 29

Reboxetine is a…

Answer 29

Noradrenaline reuptake inhibitor

Question 30

What is the placebo sag?

Answer 30

Loss of placebo effect that is witnessed with repeated administration of placebo drugs

Question 31

How does medication formulation affect placebo response?

Answer 31

Capsule > tablets for placebo response

Multiple pills > less pills for placebo response

Injection > oral

Surgery

Pill colour may influence - anxiety green and depression yellow pills showed by Shapiro

Question 32

How may a placebo work?

Answer 32

Natural remission - disease over time wanes and wears. The placebo response may coincide with this

Regression to the mean - repeated measurements on a scale will over congregate to the central point with further measurements

Endogenous opiods

Classical conditioning - pills, injections, tablets are conditioned stimuli that are learnt to associate to treatment response. (unconditioned stimuli being the active medication).

Operant conditioning - selective attention on improvement in symptoms and expectancy of treatment response

Question 33

What side effects are associated with the following drugs

1. Nefazadone
2. Droperidol, Thioridazine
3. Sertindole
4. Thalidomide (analgesic)
5. Nomifensine
6. Zimeldine
7. Remoxipiride(sulpiride group)
8. Mianserin
9. MAOIs
10. Clozapine

Answer 33

1. Nefazadone Hepatotoxicity
2. Droperidol, Thioridazine QT prolongation on ECG
3. Sertindole Sudden cardiac death
4. Thalidomide (analgesic) Phocomelia
5. Nomifensine Hepatotoxicity
6. Zimeldine Hypersensitivity reactions and Guillain-Barre syndrome
7. Remoxipiride(sulpiride group) Aplastic Anaemia
8. Mianserin Blood dyscrasias
9. MAOIs Cheese reactions
10. Clozapine Agranulocytosis

Question 34

Name some facts about buspirone?

Answer 34

• Causes no dependence
• Doesn’t have street value
• Doesn’t cause tolerance
• Can be withdrawn easily
• Has to be dose TDS as has a short half life

Question 35

Quetiapine has a….

Answer 35

Short half life (7 hours) compared to Olanzapine/Clozapine/Risperidone

Question 36

Name some drugs which undergo very little hepatic metabolism and therefore detectable in urine?

Answer 36

Gabapentin, Lithium, Amisulpride and Sulpride

Question 37

Why can Aripiprazole be dosed at OD

Answer 37

As it has a long half life of 72 hours

Question 38

Pethidine + BLANK can cause a fatal serotonin syndrome?

Answer 38

MAOI - tranylcypromine or phenelzine

Question 39

Name some receptors that Clozapine has effects on

Answer 39

Anatgonism:
- D1
- D2 –> weak affinity - at clinically effective doses may only occupy 40-50% of striatal D2 receptors. ? reason why low propensity for EPSEs
- D4 –> strong affinity

• Alpha 1 adrenergic receptors
• H1
• 5-HT2a

Agonism:
- M4 –> ? mechanism behind silaorrhoea

Question 40

If someone is presenting with alcohol withdrawal and has severe liver damage what benzodiazepines may be of choice?

Answer 40

Oxazepam or Lorazepam
- both short acting

Question 41

What does a high therapeutic index mean?

Answer 41

A drug is very safe in relation to clinical effectiveness

Methods of calculating indices include:
- Medium lethal dose (LD-50) / medium effective dose (ED-50)
- Minimum toxic dose / minimum effective dose

Drugs OTC will have a higher therapeutic index i.e paracetamol

Question 42

Outline the hepatic enzyme inducers or inhibitors?

Answer 42

Inducers:

Carbamazepine
Rifampicin
Alcohol (chronic)
Phenytoin

Gresofulvin
Phenobarbitone
Smoking

Inhibitors:

SICK ACES COM GAQ

Sodium Valproate
Isoniazid
Cimetidine
Ketokonazole / Fluconazole

Alcohol (acute)
Chlorphenicol
Erythromycin
Sulfamides

Ciprofloxacin
Omeprazole
Metronidazole

Grapefruit juice
Amiodarone
Quinidine

Question 43

Broadly name some medications that undergo metabolism by the P450 system?

Answer 43

Most anti-depressants / antipsychotics

Benzodiazepines

Warfarin

Zolpidem

Sodium Valproate

Methadone

Thyroxine

Oestrogen

Steroids