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PHAL303 > Drugs > Flashcards

Drugs Flashcards

1
Q

Chlorpromazine

A

A classical antipsychotic i.e. a D2 antagonist with a low potency
- results in more sedation and anti-muscarinic side effects and less extra-pyramidal side effects

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2
Q

Clozapine

A
  • Antagonist of 5HT2A, D4, and weakly D2
  • Effective for type II schizophrenia, bipolar, and refractory schizophrenia
  • Side effects include agranulocytosis, and a small incidence (3%) of extrapyramidal side effects due to low occupancy in striatum
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3
Q

Risperidone

A
  • 5HT2 antagonist that also acts at D2
  • More effective at treating negative symptoms than haloperidol, efficacy similar to clozapine
  • few extrapyramidal side effects, sedation, difficulty concentrating`
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4
Q

Quetiapine

A
  • Antagonist of 5HT2A and D2
  • effective for type I & type II schizophrenia and bipolar mania
  • as effective as classicals
  • sedation, dizziness, dry mouth, weight gain, some extrapyramidal effects
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5
Q

Remoxipride

A
  • weak but selective D2 antagonist, with a preference for extrastriatal D2
  • similar efficacy to haloperidol
  • insomnia, tiredness, tremor, difficulty concentrating, akathisia
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6
Q

Haloperidol

A

A potent D2 antagonist and classical anti-psychotic
- has greater extrapyramidal side effects and less sedative and anti-muscarinic side effects

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7
Q

Flumazenil

A

Antagonist at BZD site, thus acts to decrease Cl- conductance, and has an anxiogenic effect

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8
Q

TCAs

A

tricyclic antidepressants, act to increase monoamine levels via inhibiting monoamine uptake mechanisms
- differing selectivity for NA, 5HT
- can also affect histamines, ACh, and a-adrenoreceptors

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9
Q

phenelzine

A

An older MAOi that was non-selective for both MAOa and MAOb
- postural hypotension, anti-cholinergic effects
- hypertensive response to foods containing tyramine, a catecholamine-releasing agent (the “cheese effect”)

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10
Q

MAOi

A

Anti-depressants that act via inhibition of MAO enzymes to prevent monoamine metabolism

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11
Q

moclobemide

A

A selective MAOa inhibitor that mainly acts to prevent breakdown of serotonin
- dizziness, insomnia, nausea

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12
Q

SSRIs

A

selective serotonin reuptake inhibitors
- nausea, vomiting, diarrhoea, constipation, and sexual dysfunction

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13
Q

citaprolam

A

a SSRI with high serotonin selectivity
- results in more dizziness following abrupt discontinutation

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14
Q

fluoxetine

A

a SSRI that mainly affects 5HT, but also NA
- less dizziness following abrupt discontinuation

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15
Q

abrupt discontinuation of SSRIs

A

results in dizziness, likely due to high concentration of 5HT receptors in the vestibular nucleus

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16
Q

Vortioxetine

A

A novel anti-depressant that is a

SSRI, agonist at 5HT-1A, partial agonist at 5HT-1B receptors and antagonist at 5HT-3 and -7 receptors

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17
Q

Vilazodone

A

A novel anti-depressant is a
SSRI and partial agonist at 5HT-1A receptors

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18
Q

Milnacipran/Levomilnacipan

A

Novel anti-depressants that are SNRIs
- Most potent NA reuptake inhibitor among the SNRIs

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19
Q

Order of preference for pharmacological treatment of depression

A

SSRIs>TCAs/SNRIs>MAOi

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20
Q

Lithium

A

Used to treat bipolar mania
- thought to work through depletion of phosphatidyl inositol
- narrow therapeutic window, chronic treatment can lead to thyroid disorders or mild cognitive deterioration

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21
Q

Drugs used to treat bipolar mania

A

Lithium, anti-psychotics, anti-epileptics, dopamine receptor antagonists

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22
Q

Drugs used for seizures (excl absence seizures)

A
  • Valproate
  • Carbamazepine
  • Phenytoin
  • Lamotrigine
  • Levetiracetam
  • Topiramate
  • Gabapentin
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23
Q

Drugs used for focal seizures

A
  • Carbamazepine
  • Topiramate
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24
Q

Drugs used for absence seizures

A
  • Ethosuxamide
  • Valproate
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25
Q

Drugs used for status epilepticus

A
  1. Midazolam
  2. Phenytoin
  3. Phenobarbital
    + Diazepam
26
Q

What are some other uses of anti-epileptic drugs?

A
  • bipolar disorder
  • migraine
  • anxiety
  • neuropathic pain
  • tinnitus
27
Q

Carbamazepine

A

Decreases repetitive firing of Na+ channels by stabilising their inactive state
- nausea, dizziness, drowsiness, ataxia and blurred vision, rash; rarely, agranulocytosis (bone marrow fails to make enough granulocytes)

28
Q

Valproate

A
  • inhibiting repetitive firing, by increasing the number of Na+ channels in the inactivated state
  • increasing GABAergic inhibition
  • inhibit T-type calcium channels in thalamus, reducing thalamo-cortical oscillations

nausea, weight gain, transient hair loss, bleeding; rarely, severe hepatic toxicity, birth defects associated with autism and attention issues in children

29
Q

Phenytoin

A

inhibiting repetitive firing, by increasing the number of Na+ channels in the inactivated state

narrow therapeutic window, and unpredictable kinetics across age groups

Mild side effects include: vertigo, ataxia, headache, nystagmus
- At higher concentrations, severe side effects include: confusion, cognitive dysfunction, hyperplasia of the gums, hirsutism, megaloblastic anemia, hypersensitivity reactions, hepatitis, lymph node enlargement
- Can be associated with fetal abnormalities

30
Q

Vigabatrin

A

Inhibits GABA transaminase, thus prevents GABA breakdown

31
Q

Tiagabaine

A

Inhibits GABA reuptake

32
Q

Which drugs are related to psychosis

A

Amphetamines can induce a psychosis
- associated with reduced HPC and AMY volume
- also induce stereotypy
IMPLICATES DA

Ketamine at high doses can cause psychosis
IMPLICATES GLUTAMATE

High frequency of cannabis use in adolescence is linked to increased risk of psychotic symptoms
- mutation in the COMT gene, which is involved in dopamine metabolism, results in increased psychotic symptoms in frequent users
IMPLICATES DA

33
Q

Future directions for anti-psychotics

A
  • minimising side effects
  • developing drugs that are equally effective for negative and positive symptoms
  • targeting different receptors
  • using pharmacogenetics to tailor treatment and identify those at risk of severe side effects
34
Q

Ethosuxamide

A

Treatment for absence seizures

inhibiting T-type calcium channels in the thalamus to reduce thalamo-cortical oscillations

35
Q

agranulocytosis

A

severe reduction of white blood cells

36
Q

Atypical antipsychotics

A

Antipsychotics that do not exert their primary action through D2 antagonism

Overcome adverse effects of classical drugs, especially extrapyramidal side effects

Useful in treatment of type II and refractory schizophrenia

37
Q

List the four general ways antipsychotic drugs work

A
  1. Reducing the synthesis of DA
  2. Reducing DA release
  3. Blocking D2 receptors
  4. Increasing metabolism of DA
38
Q

Objective of anti-psychotics

A
  • treat immediate symptoms
  • provide long term resolution of psychosis
  • allow patient to implement structure and support
39
Q

Extra-pyramidal side effects

A
  • tremor
  • bradykinesia
  • tardive dyskinesia
  • dyskinesia
40
Q

Anticholinergic side effects

A
  • dry mouth
  • blurred vision
  • constipation
41
Q

potency relationship of anti-psychotics

A

Low potency antipsychotics, such as chlorpromazine, produce more sedation and anticholingeric side effects, and fewer extrapyramidal side effects

High potency antipsychotics, such as Haloperidol, produce more extrapyramidal side effects, and less sedation/anticholinergic side effects

There is a linear relationship between clinical potency and affinity at D2

42
Q

L-Dopa

A

L-Dopa, or levodopa, is a precursor to dopamine that is able to cross the blood brain barrier. It is given alongside carbidopa to prevent peripheral metabolism- this increases the amount that reaches the brain from 1% to 10%. Once in the brain, is it up taken by dopaminergic cells and converted into dopamine.

It is effective at managing bradykinesia and rigidity, but is less effective for tremor or balance.

Side effects of L-dopa include: nausea and vomiting, cardiovascular disturbances, and psychiatric disturbances such as psychosis, hallucinations and vivid dreams.

43
Q

“on-off” fluctuations caused by L-dopa

A

After around 5 years there is a decrease in efficacy due to the death of dopaminergic cells in the SNpc. This results in fluctuating efficacy, whereby the levels of dopamine fluctuate outside of the therapeutic window, resulting in dyskinesias when dopamine is excessive high, and ineffective treatment when dopamine drops.

44
Q

What other treatments are used alongside L-Dopa

A

Carbidopa: to reduce peripheral metabolism, resulting in an increase from 1% to 10% of L-dopa reaching brain

Selegiline: selective irreversible inhibitor of MAOb

Bromocriptine: D2 agonist with long half life that reduces “on-off” fluctuations

Anti-muscarinics: improve tremor and rigidity, but nor bradykinesia

45
Q

Epibatidine

A

A plant alkaloid found on the skin of the Epipedobates tricolor frog that has a similar structure to nicotine
- agonist with high potency and affinity at nAChR, produces analgesia and paralysis
- antagonist with low affinity at mAChRs, contributes to muscle paralysis

46
Q

Anatoxin (a.k.a. Very Fast Death Factor)

A

a potent agonist of nAChR, and is not degraded by AChE

causes permanent stimulation at NMJ, leading to loss of co-ordination, muscular fasciculations, convulsions, and eventually death by respiratory paralysis

47
Q

a-Cobratoxin + a-Bungarotoxin

A

potent antagonists of nAChR
- a-Cobratoxin (CbTx) has far greater affinity for NMJ receptors (39pM) than a7 receptors (6nM)

48
Q

Sarin

A

inhibitor of AChE

leads to paralysis, and death by asphyxiation in ≤10 minutes

49
Q

Donepezil

A

A reversible, long-acting, selective inhibitor of acetylcholinesterase (AChE)
- Treats mild-moderate AD

50
Q

Rivastigmine

A
  • Irreversible inhibitor of AChE
  • Treats mild-moderate AD
51
Q

Galantamine

A

AChE inhibitor + PAM of nAChR
- Treats mild-moderate AD

52
Q

Memantine

A

NMDA antagonist used in “treatment” of AD
- Not subsidised
- Has modest effects

53
Q

Name 6 BZDs

A
  • diazepam
  • midazolam
  • triazolam
  • temazepam
  • lorazepam
  • chlordiazepoxide
54
Q

Name two barbiturates

A
  • pentobarbital
  • thiopental
55
Q

Zopiclone

A

A non-BDZ drug that has similar hypnotic/anxiolytic actions

56
Q

Triazolam,

A

A BDZ used primarily for its hypnotic effects due to short half-life

57
Q

Drugs that reduce anxiety, despite not being classically anxiolytic

A
  • Antidepressants (SSRIs, TCAs, and MAOi)
  • Buspirone (partial agonist at 5HT1A)
  • Beta-blockers (Reduces tremor, thus reduces perceived anxiety)
58
Q

BZD mechanism of action

A

Bind to alpha/gamma subunit of GABAa receptors to increase Cl- conduction when GABA is bound
- alpha facilitates binding
- gamma2 required for full BZD response

59
Q

Mechanisms of BZD tolerance

A
  • downregulation of GABAa receptors
  • downregulation of the benzodiazepine recognition site
  • changes to the coupling between the GABA and benzodiazepine binding sites on the receptor complex
60
Q

BZD withdrawal symptoms

A

anxiety, irritability, insomnia, depression, tachycardia, profuse sweating, nausea, perceptual changes, potentially seizure activity

61
Q

How are different anxiety disorders treated

A

PTSD and stress-related anxiety is treated with benzodiazepines such as diazepam. However due to the rapid induction of tolerance in BZDs they are not used for GAD, OCD, or phobias. These are more commonly treated with SSRIs. An exception to this is the use of Xanax (alprazelam) for panic disorder.

62
Q
A

PHAL303 (10 decks)

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