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BSMS202 > Core drugs 202 > Flashcards

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
Q

what is fluoxetine used for?

A

treatment for depression, anxiety, OCD, panic disorder, PTSD

26
Q

What are the effects of fluoxetine?

A

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
Q

What is ibuprofen?

A

NSAID (analgesis)

useful for acute pain but not effective in chronic pain

28
Q

How does ibuprofen work?

A

inhibits prostaglandin synthesis and reduces inflammatory response
inhibits COX enzymes to prevent prostaglandin synthesis
prevents decrease in Na+ channel threshold caused by prostaglandins

29
Q

What is morphine?

A

opiate (analgesic)
most effective drug for pain relief
agonist of endogenous opioid system
effective in chronic pain

30
Q

How does morphine act?

A

endogenous opioid receptors which are Gi coupled

Open K+ channels and close Ca2+ channels, causing an inhibitory effect

31
Q

Where does morphine act?

A

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
Q

Side effects of morphine?

A

numerous

addiction

33
Q

Paracetamol/acetominophen

A

Analgesic, not NSAID, exact mechanism of action unknown

not effective in chronic pain

34
Q

What does paracetamol do?

A

inhibits COX enzymes but doesn’t reduce inflammation

Acts on descending serotonergic pathways

35
Q

Pizotifen

A

Anti-migraine used in prevention of migraines

limited side effects: weight gain, drowsiness

may be used as an antidepressant

36
Q

Carbamezapine

A

Anticonvulsant

used to treat seizure disorders, neuropathic pain and bipolar disorders

used for bipolar when unresponsive to lithium - most effective against manic relapse

37
Q

How does carbamezapine work?

A

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
Q

sodium valporate

A

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
Q

Mechanism of sodium valporate?

A

exact mechanism unclear
Actions on GABA
intracellular sodium blockade
epigenetic modification implicated

40
Q

Phenobarbitone

A

Barbiturate

used to treat epilepsy

41
Q

How does phenobarbitone work?

A 
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
Q

phenytoin

A

anticonvulsant

used to prevent epileptic seizures

43
Q

How does phenytoin work?

A

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
Q

Levidopa

A

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
Q

What does levidopa do?

A

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
Q

Entacapone

A

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
Q

Selegiline

A

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
Q

Ropinirole

A

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
Q

Donepezil

A

Acetylcholinesterase inhibitor

blocks Ach breakdown, increasing its activity

used to treat dementia/ Alzheimer’s disease

improves cognition and behaviour, eases symptoms

50
Q

Lidocaine/lignocaine

A

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
Q

Propofol

A

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
Q

Naloxone

A

opiate antagonist

opiate receptor blocker (competitive antagonist)
used clinically in emergencies to reverse opiate intoxication

53
Q

Suxamethonium

A

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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