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Core drugs 202 Flashcards

1
Q

What is Diazepam/valium?

A 
Benzodiazepine
Indirect GABA(A) agonist
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2
Q

How does diazepam work?

A

binds to alpha subunit of GABA(A)
increases affinity for GABA
increases frequency of channel opening
high density of binding sites in amygdala

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3
Q

What is Diazepam used for?

A

treats GAD and panic disorder

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4
Q

What are the effects of diazepam?

A 
Reduces anxiety
causes sedation
reduces convulsions
relaxes muscles
can cause anterograde amnesia
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5
Q

What is chlorpromazine

A

Typical antipsychotic, used to treat schizophrenia, bipolar disorders and hyperkinetic disorders
first antipsychotic discovered

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6
Q

How does chlorpromazine work?

A

potently blocks dopamine D2 type receptors (D1,D2,D3,D4) and has anti-serotonergic and anti-histaminergic properties

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7
Q

What are the effects of chlorpromazine

A

Prevents positive symptoms of schizophrenia.
Side effects: sedation, Parkinsonism and other extra-pyramidal side effects, dyskinesia, hypotension, anticholinergic effects, weight gain

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8
Q

What is haloperidol

A

Typical antipsychotic
potent blocker of dopamine D2 receptors (pro and post synaptic)
more potent than chlorpromazine

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9
Q

What does haloperidol do?

A

potently blocks D2 receptors
increases dopamine turnover so autoreceptors lose inhibition
blockage of post synaptic receptors causes upregulation

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10
Q

What are haloperidol’s effects?

A

prevents positive symptoms of schizophrenia
side effects: weight gain, sedation, temperature dysregulation, anticholinergic side effects, neuroleptic malignant syndrome, hypotension, raised prolactin, extrapyramidal symptoms (Parkinsonism, tardive dyskinesia, dystonia) - system becomes supersensitive to dopamine due to chronic blockade

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11
Q

What is risperidone?

A

atypical antipsychotic

used in long term treatment of schizophrenia and bipolar disorder

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12
Q

Where does risperidone act?

A

D2 receptors and serotonin receptors

more potent at serotonin receptors

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13
Q

Effects of risperidone

A

rapid antimanic effects
Side effects: arrhythmia, raised prolactin (sexual dysfunction and osteoperosis), weight gain, long term effect of glucose regulation
may produce more extrapyramidal side effects than most other atypical antipsychotics

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14
Q

What is clozapine?

A

Atypical antipsychotic

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15
Q

What does clozapine do?

A

Reduces psychosis associated with schizophrenia
Selective dopamine D4 receptor antagonist (brain)
Also acts on 5-HT receptors (antagonist)

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16
Q

Effects of clozapine?

A

Has greatest efficacy in treatment-resistant cases of schizophrenia

Also used for treatment of hyperkinetic disorders

Can improve positive and negative symptoms - without extra-pyramidal side effects

Side effects: weight gain, sedation, hypersalivation, tachycardia, hypotension, neutropenia

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17
Q

What is lithium

A

Mood stabilising drug
used in treatment of bipolar disorder
decreases risk of suicide

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18
Q

How does lithium work?

A

Specific mechanism for mood stabilisation is unknown, but has many modes of action
Interacts with multiple neurotransmitters (5-HT, NA, DA), affects cellular signalling and neurotrophic factors

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19
Q

Side effects of lithium

A

Blood tests taken every 3 months for 1st year - risk of lithium toxicity
Adverse long term effects on kidney function

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20
Q

What is amitryptiline

A

tricyclic antidepressant

used to treat depression, anxiety, chronic pain

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21
Q

How/where does amytriptiline act?

A

Acts on serotonin transporter (SERT) and noradrenaline transporter to prevent reuptake

mechanism in chronic pain is unclear: acts on descending inhibitory pathways (inhibits sodium and calcium channels)

also acts as antihistaminergic and anticholinergic- produces sedative effect

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22
Q

Side effects of amytriptiline

A

constipation, orthostatic hypotension, dry mouth, drowsiness, cardiotoxicity in overdose

23
Q

What is fluoxetine/prozac?

A

SSRI (antidepressant)

24
Q

What does fluoxetine do?

A

increases serotonin function by preventing its reuptake
Increased serotonin availability triggers downstream pathways (long term modulatory effects, secondary messenger cascades, gene transcription)

25
what is fluoxetine used for?
treatment for depression, anxiety, OCD, panic disorder, PTSD
26
What are the effects of fluoxetine?
Can be initially anxiolytic - 2/3 weeks until effects are seen low toxicity, safe in overdose Side effects: GI, headache, irritability, reduction of libido
27
What is ibuprofen?
NSAID (analgesis) | useful for acute pain but not effective in chronic pain
28
How does ibuprofen work?
inhibits prostaglandin synthesis and reduces inflammatory response inhibits COX enzymes to prevent prostaglandin synthesis prevents decrease in Na+ channel threshold caused by prostaglandins
29
What is morphine?
opiate (analgesic) most effective drug for pain relief agonist of endogenous opioid system effective in chronic pain
30
How does morphine act?
endogenous opioid receptors which are Gi coupled | Open K+ channels and close Ca2+ channels, causing an inhibitory effect
31
Where does morphine act?
multiple sites of action: brainstem (disinhibition), spinal cord, peripheral (inhibits channels on nociceptors) Different receptor subtypes depending on location - Mu are responsible for most analgesic/rewarding properties
32
Side effects of morphine?
numerous | addiction
33
Paracetamol/acetominophen
Analgesic, not NSAID, exact mechanism of action unknown | not effective in chronic pain
34
What does paracetamol do?
inhibits COX enzymes but doesn't reduce inflammation Acts on descending serotonergic pathways
35
Pizotifen
Anti-migraine used in prevention of migraines limited side effects: weight gain, drowsiness may be used as an antidepressant
36
Carbamezapine
Anticonvulsant used to treat seizure disorders, neuropathic pain and bipolar disorders used for bipolar when unresponsive to lithium - most effective against manic relapse
37
How does carbamezapine work?
competitively inhibit voltage gated Na+ channels - binds its inactive state, prolonging periods between successive firings (lengthens refractory period?) raises threshold for action potential, lowers excitability Exact mechanism for pain relief is unclear - work in spinal cord to reduce excitability
38
sodium valporate
anticonvulsant used to treat epilepsy and bipolar disorder anti-manic - useful in prevention of mania useful in combination with other drugs not to be used in women of child-bearing age
39
Mechanism of sodium valporate?
exact mechanism unclear Actions on GABA intracellular sodium blockade epigenetic modification implicated
40
Phenobarbitone
Barbiturate | used to treat epilepsy
41
How does phenobarbitone work?
``` indirect GABA(A) agonist binds to GABA receptors, increases duration of channel opening increases overall GABAergic activity Epileptic neural discharges are less likely to be transmitted ```
42
phenytoin
anticonvulsant | used to prevent epileptic seizures
43
How does phenytoin work?
frequency and use dependent suppression - blocks Na+ channels responsible for the action potential when neural discharges are of sustained high frequency Obstructs positive feedback which causes maximal seizure activity depressive action doesn't have effect in normal brain state with lower neuronal firing rates
44
Levidopa
dopamine precursor converted to dopamine by dopamine decarboxylase used to treat parkinson's disease: gold standard available in several formulations (oral pills, duodenal infusion)
45
What does levidopa do?
dopamine precursor turned into dopamine by dopamine decarboxylase increases available amount of dopamine in nigostriatal system always combined with dopa decarboxylase inhibitor to prevent peripheral conversion to dopamine
46
Entacapone
COMT inhibitor Administered with L-dopa for treating Parkinson's disease (early stages) inhibits catelchol-O-methyl transferase enzyme which causes dopamine inactivation, so stops dopamine being degraded and keeps it around for longer reduces peripheral metabolism of L-dopa increasing duration of action can make dyskinesia worse and cause diarrhoea
47
Selegiline
Type B MAO inhibitor (MAOi) selective monoamine oxidase inhibitor for dopamine treatment for early stage PD and dementia prevents degradation of dopamine and causes more dopamine to be released on subsequent activations
48
Ropinirole
non-ergot dopamine agonist used to treat Parkinson's bypasses degenerating nigostriatal systems to directly activate dopamine receptors doesn't need enzymatic conversion Stable and long-acting treatment (strong n stable)
49
Donepezil
Acetylcholinesterase inhibitor blocks Ach breakdown, increasing its activity used to treat dementia/ Alzheimer's disease improves cognition and behaviour, eases symptoms
50
Lidocaine/lignocaine
local anaesthetic, applied topically to skin raises threshold for AP generation, lowering excitability Blocks Na+ channels in inactivated state stops action potentials locally (stops nociceptive firing)
51
Propofol
General anaesthetic, used to induce anaesthesia administered by injection/ IV infusion solvent - minimal accumulation short redistribution - half life (4 minutes) painful to inject can have CVS/RS effects
52
Naloxone
opiate antagonist opiate receptor blocker (competitive antagonist) used clinically in emergencies to reverse opiate intoxication
53
Suxamethonium
neuromuscular blocking drug acts on postsynaptic membrane mimics acetylcholine, but hydrolysis is slower, leading to a blockade induces short term paralysis with rapid onset/offset (short half-life of 2 mins) multiple side effects

BSMS202 (8 decks)

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