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YEAR 2 - The Nervous System > Drugs list > Flashcards

Drugs list Flashcards

1
Q

What is the action and some features of amitriptyline?

A
  • Tricyclic antidepressant.
  • Nonspecific monoamine reuptake inhibitor, most importantly SERT and NET.
  • Rarely used nowadays as severe side-effects due to nonspecificity. H1 - sedation M3 - dry mouth, constipation.
  • Cardiotoxic. Previous MCI or history of arrhythmia is major contraindiction.
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2
Q

What is the action and some features of aspirin?

A
  • In the context of neuroscience, involved in pain relief
  • Cyclooxygenase I and II non-competitive, irreversible inhibitor, acetylates them.
  • Reduces synthesis of prostaglandins, reduces inflammation.
    • Prostaglandins sensitise C-fibre pain neurons so aspirin reduces inflammatory pain. NSAID.
  • As a NSAID, used in chronic inflammatory diseases such as rheumatoid arthritis.
  • Causes ototoxicity at high doses.
  • Low doses: mild indigestion, risk of bleeding

Bold are related to neuro

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3
Q

What is the action and some features of buspirone?

A
  • 5-HT1A receptor agonist. Used as an anxiolytic.
  • Agonist of the 5-HT1 receptor on the pre-synaptic membrane, leading to decreased 5-HT release
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4
Q

What is the action and some features of carbamazepine?

A
  • Inhibitor of VGNaC.
  • Preferentially binds to inactive form so inhibits repetitive and sustained firing. Used in epilepsy as an anticonvulsant.
  • [EXTRA] Used to treat trigeminal neuralgia.
  • Side-effects: nausea, drowsiness.
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5
Q

What is the action and some features of chlorpromazine?

A
  • 1st gen/typical antipsychotic, also known as a neuroleptic.
  • D2 antagonist. Used as an antipsychotic in psychoses such as schizophrenia.
  • Only treats positive symptoms.
  • Side-effects: movement problems ( tardive dyskinesia is severe, rare example, also acute muscle stiffness and Parkinsonism), sleepiness, considerable weight gain, hypotension & dizziness
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6
Q

What is the action and some features of clozapine?

A
  • Atypical antipsychotic. Works as a D2 antagonist but is also pretty non-specific, acts at many other receptors.
  • Very effective, works in 1/3 of patients non-responsive to other treatments.
  • Fewer extrapyramidal movmenet disorder side-effects than typical antipsychotics. But limited by non-specificity and toxicity eg. bone marrow toxicity
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7
Q

What is the action and some features of codeine?

A
  • Opioid used as an analgesic.
  • Acts centrally at the µ opioid receptor, inhibits transmission of nociceptive information in the spinal cord as well as causing analgesia by acting directly on the brain eg. PAG.
  • Causes constipation, itchiness and nausea. Addictive - dependence issues.
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8
Q

What is the action and some features of cyclopentolate?

A
  • Muscarinic antagonist.
  • Used in paediatric eye examination as eyedrop to dilate the pupil and prevent accommodation.
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9
Q

What is the action and some features of diazepam?

A
  • Benzodiazepine
  • Binds to specific binding site on GABAA channel. Increases open probability when GABA bound, so potentiates GABA transmission - positive allosteric modulator.
  • Used as an anxiolytic.
  • Used acutely for status epilepticus (single seizure lasting more than five minutes or two or more seizures within a five-minute period without the person returning to normal between them).
  • Used as a sedative and to reduce anxiety before surgery, and as a sedative in ICUs
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10
Q

What is the action and some features of fluoxetine (Prozac)?

A
  • Antidepressant of the SSRI class.
  • Used to treat major depressive disorder, OCD and panic disorder.
  • Can lead to dependence, withdrawal.
  • Side effects:
    • Insomnia
    • GI disturbance
    • Sexual dysfunction
    • Withdrawal effects (emerging evidence)
  • [EXTRA] -> Paradoxically increase the concentration of 5-HT in the synapse, which should be anxiogenic, but they are also proposed to decrease the sensitivity of 5-HT2C receptors on the post-synaptic membrane of certain synapses. Thus, they have anxiolytic effects in some parts of the brain, despite increasing 5-HT
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11
Q

What is the action and some features of furosemide relevant to neuroscience?

A
  • Loop diuretic. Inhibits NKCC.
  • Ototoxic in high doses.
  • Treat hypertension but thiazide diuretics are more commonly used.
    • May be used when tolerance is mounted against thiazides so a stronger diuresis is needed.
  • Treatment of congestive heart failure - relief of oedema by fluid loss and vasodilation. However, reducing circulating volume activates SNS and RAAS, increasing myocardial O2 demand and worsening problem.
  • Electrolyte disturbances also increase risk of MCI.
  • Now rarely used, apart from one-off injection for acute pulmonary oedema after MCI.
  • Side-effects: hypokalcaemia, metabolic alkalosis, hypocalcaemia, hyperuricaemia
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12
Q

What is the action and some features of gentamicin relevant to neuroscience?

A
  • Antibiotic of the aminoglycoside class.
  • Acts at 30s subunit to inhibit translation initiation.
  • Like all aminoglycosides, is ototoxic.
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13
Q

What is the action and some features of haloperidol?

A
  • 1st gen/typical antipsychotic, also known as a neuroleptic.
  • D2 antagonist. Used as an antipsychotic in psychoses such as schizophrenia, and to treat tics in Tourette’s.
  • Also used in Huntington’s (improves chorea symptoms)
  • Side-effects: movement problems ( tardive dyskinesia is severe, rare example, also acute muscle stiffness and Parkinsonism), sleepiness, considerable weight gain, hypotension & dizziness
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14
Q

What is the action and some features of ibuprofen?

A
  • Cyclooxygenase I and II reversible, competitive inhibitor.
  • Reduces synthesis of prostaglandins, reduces inflammation. Prostaglandins sensitise C-fibre pain neurons so aspirin reduces inflammatory pain. NSAID.
  • Given after surgical procedures or even preemptively to reduce pain.
  • Side-effects: risk of GI bleeding, rash, gastric reflux
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15
Q

What is the action and some features of isoflurane?

A
  • Inhaled general anaesthetic. Lipophilic.
  • Hypothesised to act by altering membrane fluidity, and binding to and affecting intramembranous portions of ion channels.
  • Mostly used for maintenance of anaesthesia.
  • Side-effects:
    • Sensitises heart to adrenaline - arrhythmia
    • Respiratory depressant
    • Reduces MAP
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16
Q

What is the action and some features of L-DOPA?

A
  • Used to treat Parkinson’s disease. Can cross BBB and is converted into dopamine there.
  • Given with carbidopa (peripheral DOPA decarboxylase inhibitor) to prevent excessive adrenaline and noradrenaline production in the periphery.
  • After about 5 years:
    • Sudden on/off effects, gait freezing
    • Dyskinesias (intense whole-body writhing)
17
Q

What is the action and some features of lithium?

A
  • Used as a mood stabiliser. Used for bipolar disorder, or major depressive disorder that does not respond to other treatments.
  • Inhibits inositol monophosphatase - overactive phosphatidylinositol cycle thought to at least partially underlie bipolar disorder
  • Narrow therapeutic index
  • Common side-effects:
    • Nausea, vomiting
    • Headache
    • Dry mouth/metallic taste in mouth
    • Hand tremors
    • Hypothyroidism
    • Increased thirst and urination
    • Renal damage
18
Q

What is the action and some features of NSAIDs?

A
  • Class of drugs which inhibit COX. Inhibit synthesis of lipid mediators of inflammation - prostaglandins, leukotrienes, PAF. Reduce inflammation and oedema.
  • Prostaglandins sensitise C-fibre pain neurons, so NSAIDs reduce inflammatory pain.
    • Sensitise the nociceptive nerves to excitation by increasing the likelihood of opening of voltage-gated sodium channels
  • Cannot be used to treat neuropathic pain
  • Downsides of NSAID use:
    • COX-1 is constitutively active (eg. produces prostaglandins to support the gastric mucosa) while COX-2 is activated by inflammation
    • Thus, COX-2 selective inhibitors (celecoxib) were developed as analgesics to avoid peptic ulcers associated with NSAID treatment
    • But there is current concern over cardiovascular harm associated with COX-2 inhibition (Vioxx controversy)
  • Contraindicated in patients with peptic ulcers - if used for pain relief, can increase severity of peptic ulcers
19
Q

What is the action and some features of nicotine?

A
  • Agonist of nicotinic acetylcholine receptors.
  • Stimulant at low doses, sedative at increasing doses. Anxiolytic properties.
  • Highly addictive (stimulates dopamine release)
20
Q

What is the action and some features of phenelzine?

A
  • Monoamine oxidase inhibitor, irreversible.
  • Used as an antidepressant, appears to work by increasing synaptic concentration of serotonin and noradrenaline.
21
Q

What is the action and some features of phenytoin?

A
  • Voltage-dependent inhibition of VGNaC, preventing rapid, high-frequency firing.
  • Used to treat status epilepticus acutely, or chronically to prevent seizures occurring.
  • Side-effects include nausea, stomach pain and loss of coordination.
22
Q

What is the action and some features of propofol?

A
  • Intravenous general anaesthetic.
  • Acts by potentiating GABAA receptors. Prinicpally works as a hypnotic, so requires analgesics (opoids) and muscle relaxants.
  • Most commonly used induction agent by far.
23
Q

What is the action and some features of propranolol relevant to neuroscience?

A
  • Nonspecific β-adrenergic antagonist.
  • Used as an anxiolytic.
  • Used in heart failure. This is to reduce sympathetic drive to reduce myocardial oxygen consumption.
    Also reduce RAAS activation - reduce peripheral vasoconstriction, reduce afterload.
  • Contraindictions - asthma, as it is a β2-antagonist so exacerbates bronchoconstriction, but observations and studies have found that their use does not precipitate asthma attacks
24
Q

What is the action and some features of sumatriptan?

A
  • 5-HT1 agonist. Inhibits release of CGRP, which sensitises trigeminal nociceptive neurons.
  • Used to treat migraine.
25
Q

What is the action and some features of temazepam?

A
  • Binds to specific binding site on GABAA channel.
  • Increases open probability when GABA bound, so potentiates GABA transmission - positive allosteric modulator.
  • Used as a hypnotic to treat insomnia.
  • Used as a sedative and to reduce anxiety before surgery, and as a sedative in ICUs.
26
Q

What is the action and some features of tramadol?

A
  • Opioid used as an analgesic.
  • Acts centrally at the µ opioid receptor, inhibits transmission of nociceptive information in the spinal cord as well as causing analgesia by acting directly on the brain eg. PAG.
  • Causes constipation, itchiness and nausea. Addictive - dependence issues.
27
Q

What is the action and some features of valproate?

A
  • Mechanism of action unclear - may be by blocking VGNaC and increasing brain GABA levels.
  • Inhibits GABA breakdown
  • Used for chronic management of epilepsy, and for treating manic episodes in bipolar disorder.
  • Side-effects: nausea, drowsiness, dizziness, hepatotoxicity.
  • Causes birth defects, particularly spina bifida; must not be taken in pregnancy.
28
Q

What is the action and some features of venlafaxine?

A
  • Serotonin-noradrenaline reuptake inhibitor (SNRI).
  • Increases synaptic serotonin and noradrenaline concentrations.
  • Used to treat major depressive disorder and various anxiety disorders.
29
Q

What is the action and some features of agomelatine?

[EXTRA]

A
  • Melatonin receptor agonist, 5-HT2C and 5-HT2B antagonist .
  • 5-HT2B antagonism makes it an atypical antidepressant .
30
Q

What is the action and some features of doxapram?

[EXTRA]

A
  • Respiratory stimulant, works by stimulating carotid chemoreceptors.
  • Used to stimulate respiration in respiratory failure, and for recovery post-anaesthesia.
  • Side-effects: tachycardia, hypertension, panic attacks
31
Q

What is the action and some features of flumazenil?

[EXTRA]

A
  • GABAA antagonist.
  • Competitive antagonist of benzodiazepines , so used to reverse their action eg. in overdose.
32
Q

What is the action and some features of gabapentin?

[EXTRA]

A
  • Binds to α2δ regulatory subunit of VGCCs, reducing channel delivery to membrane and activation.
  • Newer anti-epileptic, also used to treat neuropathic pain.
  • Side-effects: dizziness, somnolescence, suicidal thoughts
33
Q

What is the action and some features of hyoscine?

[EXTRA]

A
  • Non-specific antimuscarinic. Also known as scopolamine.
  • Used to treat motion sickness and post-operative nausea.
34
Q

What is the action and some features of memantine?

[EXTRA]

A
  • Monoclonal antibody, inhibitor of NMDAR.
  • The only drug approved for Alzheimer’s that isn’t an anticholinesterase. Symptomatic only, not disease-modifying. Small positive improvement in cognition, mood and day-to-day functioning.
  • NMDAR dysfunction Ca2+ entry thought to contribute to neuronal oxidative damage and death, particularly in hippocampus.
35
Q

What is the action and some features of mirtazapine?

[EXTRA]

A
  • Atypical antidepressant.
  • Strongest activity is as H1 antagonist.
  • Also, antagonist of α2 adrenergic receptors, and of 5-HT2A and 5-HT2C serotonergic receptors.
  • α-antagonism thought to lead indirectly to increased activity of 5-HT1A receptors.
  • Noradrenergic and specific serotonergic antidepressant.
36
Q

What is the action and some features of mianserin?

[EXTRA]

A
  • Atypical, tricyclic antidepressant.
  • Inverse agonist of H1 receptor, and inhibitor of various serotonin receptors, particularly 5-HT2 subtypes.

YEAR 2 - The Nervous System (18 decks)

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