1
Q
What are the treatments for huntingtin’s
A
tetrabenazine
chlorpromazine
haloperidol, olanzapine, risperidone, quetiapine
2
Q
What is tetrabenzaine
A
- HD treatment
- Inhibitor of vesicular monoamine uptake (VMAT)
- Decreases dopamine, less facilitation of movement-
3
Q
What is chlorpromazine
A
- HD treatment
- DA antagonist, antipsychotic
4
Q
What drugs can treat moderate Alzheimer’s
A
Tacrine
Donepezil
Rivastigmine
Galantamine
All have cholinergic side effects!
5
Q
memantine
A
What is prescribed if acetylcholine esterase inhibitors can’t be tolerated in Alzheimer’s
6
Q
What is used in conjunction with L-DOPA in PD
A
Carbidopa and benserazide
Don’t cross BBB
7
Q
Entacapone and tolcapone
A
PNS drugs for PD treatment
COMT inhibitors
8
Q
What are CNS drugs for PD treatment
A
- Tolcapone inhibits COMT, increases dopamine availability
- Selegiline and rasagiline - MAOb, increase DA availability
9
Q
pramipexole and ropinirole
A
DA agonists used to treat PD
10
Q
Benztropine and phencyclidine
A
mAChR antagonists can used to treat PD
difficult to manage side effects as non-selective
11
Q
amantadine
A
mechanisms not understood
NMDA inhibitor that treats PD
12
Q
What amfetamines are used medically
A
ADHD
modafinil - a2 adrenoreceptor activation, release of 5-HT. bad side effects
13
Q
Convulsants
A
Pentylenetetrazol, penicilin, bicuculline, gabazine, strychnine
14
Q
pentylenetetrazol
A
- induce seizures
- GABAa receptor antagonist
15
Q
penicilin
A
- anti-GABA activity
- used widely as a seizure inducing agent to test anti-convulsives
- does not cross BBB, applied directly to cortical surface
16
Q
strychnine
A
- induces seizures by acting as a glycine antagonist
- small doses given as ‘tonic’ give rise to ‘risus sardonicus’ - facial muscle tetany
- alkaloid from seed of tree nux vomica
- glycine acts as pentameric ligand-gated Cl- channel
17
Q
action of NSAIDs
A
- inhibit both COX-1 and COX-2
- anti-inflammatory, anti-pyretic
- analgesic activity COX-2
- GI issues with COX-1
- COX-2 role in CNS unclear
18
Q
neuropathic treatments
A
- capsaicin - licensed for symptomatic relief
- lidocaine - localised pain
19
Q
opioids - agonist, antagonist, mixed
A
morphine, naloxone, buprenophine
20
Q
buprenophine
A
- opioid
- partial agonist
- reduced abuse potential
- withdrawals not bad
21
Q
nalorphine
A
- opioid
- delta, kappa partial agonist
- some analgesia, low abuse potnetial
- depression
22
Q
pentazocine
A
- opioid
- combines mu antagonism and kappa agonist
23
Q
tramadol
A
- opioid
- weak mu agonist
- weak inhibitor of monoamine reuptake
24
Q
naloxone
A
- 1st opioid discovered
- competitive antagonist of all 3 opioid receptors
- little effect if given alone, can reverse all affects of full agonists
- used to treat respiratory depression in overdoses
25
how do you treat status epilepticus
Benzos: lorazepam, midazolam, diazepam
26
Na+ channel blockers and what for?
epilepsy
- phenytoin
- carbamazepine
- lamotrigine
27
Phenytoin
Na+ channel blocker
stabilises Na.v channels in inactivated state
effective in tonic clonic and partial
worsens absence and myoclonic
28
Side effects of phenytoin
teratogenic, risk of lupus, cerebellar atrophy, acne, gingival overgrowth
29
Carbamazepine
- blocks Na+
- first line for focal
- mood stabiliser, used for neuropathic pain
- also induces CYP3A4
30
Carbamazepine side effects
teratogenic
risk of lupus
worsens juvenile epilepsy
31
Lamotrigine
- anti-convulsant
- sedation
- sleep distrubances
- rash
31
Lamotrigine
- Na+ channel blocker
- 1st line treatment for tonic-clonic!
- 2nd line for absence
- can worsen myoclonic
- used to treat bipolar
32
Which benzodiazepines act on GABAA receptors in epilepsy
Clobazam - adjunct, treats anxiety
Clonazepam - refractory epilepsy, acts on Ca2+
Diazepam - status epilepticus
33
Tiagabine
- Anti-convulsant
- GAT1 inhibitor
- Side effects = sedation, dizziness
34
Vigabatrin
- Anti-convulsant
- irreversible GABAr inhibitor
- Sabril
- Adjuvant medication
- short plasma half life, once daily is okay
side effects = visual disturbances, teraogenic
35
Sodium valproate
- Anti-convulsant
- extremely useful, bad side effects
- 1st line treatment but don't know its mechanism
- also used for bipolar
- bad teratogenic
36
Side effects of sodium valproate
- liver toxicity
- powerful teratogen
- autistic disorders, anencephaly, spina bifida, limb defects
- cognitive changes
- foetal valproate syndrome
37
Example of gabapentinoids
Gabapentin/pregabalin
38
What does gabapentin do
- anti-convulsants
- similar structure to GABA
- acts on a2d subunit of Ca channel
- increases GAD levels too
- street drugs now - gabbies
39
Ca2+ channel blockers
Ethosuximide, topiramate
40
Ethosuximide
- anti-convulsant
- Ca2+ blocker
- 1st choice for absence
- can worsen others
- side effects = sedation, nausea
41
Levetiracetam
- anti-convulsant
- adjunct for focal
- mechanism unknown
- reduces NT release
- focal, myoclonic and tonic-clonic
- stevens-johnson syndrome
42
Topiramate
- anti-convulsant
- adjunct for focal
- potentiation of GABAa
- blocks AMPA and kainate
- blocks Na and Ca channels
- inhibits carbonic anhydrase
43
Old monoamine oxidase inhibitor drugs
Phenelzine, tranylcypromine, isocarboxazid
Very effective in MDD and bipolar
cause cheese reaction
44
Newer monoamine oxidase inhibitors
molobemide
reversible, no dietary reactions
fewer adverse effects
45
SSRIs
fluoxetine
citalopram, paroxetinem sertraline
46
SNRIs
venlafaxine, duloxetine
47
NRIs
reboxetine, atomoxetine
48
Tricylic anti-depressants
amitryptiline, nortriptyline, imipramine
49
What does mirtazapine do
- noradrenergic and specific serotonergic antidepressant (NaSSA)- acts on receptors rather than reuptake system
- antagonist of a2 adrenoreceptors and 5HT2A receptors
- highly sedating (H2)
- faster onset than other anti-depressants
50
newer treatments of MDD
esketamine and ketamine
psychedelics
agomelatine
51
bipolar treatments
mood stabilisers
- lithium
- anticonvulsants (lamotrigine, valproate)
- olanzipine
52
1st line treatments for schizophreniza
Risperidone, olanzapine, quetiapine
53
What does chlorpromazine do
- old anti-psychotic
- also used for huntingtin's
- first effective psychotic
- side-effects - sedative, galactorrhea
54
Aripiprazole
- anti-psychotic
- partial D2 agonist
- 3rd gen
- benign side effects
55
Risperidone
- 2nd gen anti-psychotic
- moderate risk of EPS and can cause sedation and weight gain
- galactorrhea
56
Haloperidol
- anti-psychotic
- antiemetic and tourette's too
- lower sedative effects, higher risk of EPSP
57
Clozapine
- anti-psychotic
- useful for treatment-resistant patients
- agranulocytosis (WBC death)
58
Barbiturates
- many derivatives
- -barbital suffix
- historically widely used as anxiolytics, anticonvulsants, sedatives, anaesthetic
- fallen out of favour due to danger of OD
59
Barbiturate mechanism of action
- positive allosteric modulator of GABAA receptor
- at higher concentrations can directly activate the receptor
- inhibit AMPA
60
Current uses for barbiturates
medically - thiopental. induction agent in general anaesthesia
criminal justice - lethal injections. sodium thiopental
61
Name four benzodiazepine agonists
- Flunitrazepam
- Diazepam
- Tamazepam
- Nitrazepam
Highly addictive, increase GABAa receptor opening
62
What are examples of benzodiazepine inverse agonist
- proconvulsants
- anxiogenics
63
Clinical uses for benzodiazepines
used to be 1st line treatments for anxiety and sleep disorders, due to tolerance and dependence issue they are used less now
64
what drugs were identified in the 90s with the aim of treating anxiety without the sedative effects
Bretazenil, Alpidem and ocinaplon
DRUG NAMES
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