Basic Pharmacology Flashcards

(44 cards)

1
Q

What drugs are found within the class of benzisoxazoles?

A

Risperidone and its active metabolite Palliperidone

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2
Q

Name a reversible MAOI

A

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

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2
Q

Rauwolfia Serpentina was the natural source of which drug?

A

Reserpine

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

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3
Q

Haloperidol, droperidol and benperidol are which class of drugs

A

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

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4
Q

Delay and Deniker discovered which historical psychiatric drug?

A

Chlorpromazine

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

Delay and Deniker worked under the supervision of Paul Charpentier

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5
Q

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

A

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

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6
Q

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

A

Sodium Valproate (Divalproex)

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7
Q

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

A

Zuclopenthixol and Flupenthixol

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

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8
Q

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

A

Haloperidol, Sertindole, Thioridazine

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9
Q

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

A

Buspirone - it is azaspirone

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10
Q

Olanzapine is which class of drugs?

A

Thienobenzodiazepine
- a relation of clozapine which is a tricyclic dibenzodiazepine

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11
Q

How do secondary amines compare to tertiary amines?

A

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

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12
Q

Seizure risk is particularly higher for which type of drug?

A

Buproprion - it is an aminoketone

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

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13
Q

Name a drug for the treatment of hypersexuality and paraphilias?

A

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

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14
Q

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

A

Taurine Synthetic Analgoue - Acamprosate

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15
Q

Name some advantages to Escitalopram > Citalopram?

A

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

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

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16
Q

Controversial new treatments for Alzheimer’s have targeted?

A

BACE1 - beta secretase enzymes

The enzymatic form that converts APP to Beta amyloid plaques

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17
Q

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

A

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

18
Q

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

A

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

19
Q

Zopiclone belongs to which pharmacological class

A

Cyclopyyrolone

20
Q

What may be used to manage symptoms of opiod withdrawal?

A

Lofexidine - alpha-2 adrenergic agonist

21
Q

Who discovered Imipramine (1958)

A

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

Amitriptyline was later introduced

22
Q

Who discovered Haloperidol from Pethidine?

A

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

Janssen later also synthesised risperidone

23
Q

Who loves cheese

A

Blackwell - discovered the cheese reaction of MAOIs

24
Amisulpride and sulpride belong to which class of psychotropic medications?
Substituted benzamides
25
Name an antipsychotics that is a... a) Dibenzodiazepines b) Dibenzothiazepine c) Thienobenzodiazepine
a) Cloazapine is a dibenzodiazepine b) Quetiapine is dibenzothiazepine c) Olanzapine is a thienobenzodiazepine
26
Which anti-depressants are hydrazine derivatives?
Phenelzine, Isocarboxazid
27
How do Mirtazapine and Mianeserin work?
Noradrenaline and specific serotonin antagonist
28
Agomelatine works as a...
Noradrenaline and Dopamine disinhibitor (later down the line)
29
Reboxetine is a...
Noradrenaline reuptake inhibitor
30
What is the placebo sag?
Loss of placebo effect that is witnessed with repeated administration of placebo drugs
31
How does medication formulation affect placebo response?
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
32
How may a placebo work?
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
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
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
34
Name some facts about buspirone?
- 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
35
Quetiapine has a....
Short half life (7 hours) compared to Olanzapine/Clozapine/Risperidone
36
Name some drugs which undergo very little hepatic metabolism and therefore detectable in urine?
Gabapentin, Lithium, Amisulpride and Sulpride
37
Why can Aripiprazole be dosed at OD
As it has a long half life of 72 hours
38
Pethidine + BLANK can cause a fatal serotonin syndrome?
MAOI - tranylcypromine or phenelzine
39
Name some receptors that Clozapine has effects on
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
40
If someone is presenting with alcohol withdrawal and has severe liver damage what benzodiazepines may be of choice?
Oxazepam or Lorazepam - both short acting
41
What does a high therapeutic index mean?
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
42
Outline the hepatic enzyme inducers or inhibitors?
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
43
Broadly name some medications that undergo metabolism by the P450 system?
Most anti-depressants / antipsychotics Benzodiazepines Warfarin Zolpidem Sodium Valproate Methadone Thyroxine Oestrogen Steroids