Drugs - CNS Flashcards

1
Q

Diazepam/Lorazepam

A

Benzodiazepine (Anxiolytic)

Allosteric modulator of GABA-A receptors
Increased inhibitory effect of GABA, acts on limbic system, thalamus, hypothalamus and cortex, calming effect

Uses: Anxiety, Alcohol withdrawal, muscle spasms, seizures/epilepsy

ADRs: Sleepiness, loss of co-ordination, tolerance, depression

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2
Q

Haloperidol

A

Typical antipsychotic

High Dopamine D2 receptor antagonism

Uses: Schizophrenia, tourettes

ADRs: Tardive dyskinesia (possibly permanent), Neuroleptic malignant syndrome (muscle rigidity, fever, delerium, autonomic instability), Long Q-T

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3
Q

Chlorpromazine

A

Typical antipsychotic

D1, 2, 3, 5 receptor antagonist
5HT-1/2 receptor antagonist
H1 Histamine receptor antagonist
Alpha 1/2 receptor antagonist
M1/2 muscarinic antagonist

Treats: Schizophrenia, Bipolar, ADHD, nausea, vomiting

ADRs: Movement problems (e.g. tardive), sleepiness, dry mouth, orthostatic hypertension, neuroleptic malignant syndrome

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4
Q

Olanzapine

A

Atypical antipsychotic

5HT2A + D2 receptor antagonist

Uses: Schizophrenia, Bipolar, Anxiety, PTSD

ADRs: Weight gain, Extrapyramidal (tremors, muscle rigidity), paradoxical reactions

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5
Q

Risperidone

A

Atypical antipsychotic

5HT2A, 5HT7, D2, Alpha 1/2 antagonist

Uses: Schizophrenia, bipolar, irritability in autism

ADRs: Movement problems (e.g. tardive, less likely than typicals), neuroleptic malignant syndrome, sleepiness, constipation, weight gain

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6
Q

Quetiapine

A

Atypical antipsychotic

Dopamine, serotonin and andrenergic antagonist

Uses: Schizophrenia, Bipolar, Major depressive disorder

ADRs: Dry mouth, Dizziness, Headaches, Hypertension, Orthostatic hypotension, Weight gain, Movement issues (tardive, tremor), NMS

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7
Q

Clozapine

A

Atypical antipsychotic

Dopamine, serotonin, histamine, adrenergic, muscarinic antagonist

Uses: Schizophrenia, bipolar etc. Those intolerant to other anti-psychotics

ADRs: Constipation, muscle stiffness, sedation, tremores, hypotension, weight gain, Extrapyramidal: tardive
Agranulocytosis, leukopenia, neutropenia, seizures, dementia

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8
Q

Valproic acid

A

Anti-mania

Not fully understood, reduces seizure induced reduction in PIP3, blockage of voltage gated sodium channels and increased GABA levels

Treats: Epilepsy, Mania (bipolar), Migranes

ADRs: Nausea, Drowsiness, Dizziness, Vomiting, Weakness, Bleeding, Encephalopathy, Suicidal ideation

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9
Q

Lithium salts

A

Anti-mania

Unknown, increased serotonin? Interactions with NO and hence neuronal plasticity?

Uses: Bipolar, MDD, Schizophrenia

ADRs: Confusion, constipation, Headache, Myoclonus, Hand tremor, Weight gain, Extrapyramidal (muscle rigidity, parkinsonism, dsytonia), Hypothyroidism

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10
Q

Imipramine

A

TCA

Serotonin reuptake inhibiton
Noradrenaline reuptake inhibition
Dopamine reuptake inhibition

Treats: MDD

ADRs: CNS (dizziness, drowsiness, seizures, extrapyramidal), CVS (orthostatic hypotension, tachycardia, dysrhythmia), GI (Dry mouth, paralytic ileus, increased appetite, hepatitis)

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11
Q

Citalopram/Fluoxetine/Sertraline

A

SSRI

Serotonin reuptake inhibitor

Uses: MDD, depression, Panic disorder, anxiety, OCD, Bulimia

ADRs: Sexual dysfunction (lack of arousal, erection, orgasm), drowsiness, insomnia, nausea, weight gain, sweating, BP changes

ADRs particularly prevalent with sertraline

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12
Q

Venlaxafine

A

SNRI

Serotonin noradrenaline reuptake inhibitor

Uses: MDD, Anxiety, Panic disorder, social phobia

ADRs: Suicide, Severe withdrawal, headache, nausea, insomnia, asthenia, dizziness, Sexual side effects (lack of arousal/orgasm)

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13
Q

Orlistat

A

Anti-obesity

Inhibitor of gastric and pancreatic lipases

Uses: Obesity

ADRs: Steatorrhoea, flatus excessivus, fecal incontinence, frequency

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14
Q

Cyclizine

A

H1 antagonist (anti-emetic)

May have effects on the labrynthine apparatus

Uses: Treat nuasea, vomiting, motion sickness, vertigo (post op following opiods and general anaesthesia)

ADRs: Drowsiness, xerostomia, headache, diplopia, dermatitis, urinary retention

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15
Q

Metoclopramide

A

D2 receptor antagonist

Inhibition of D2 receptors in the chemoreceptor trigger zone in the CNS

Uses: Nausea (post op and chemo related)

ADRs: Restlessness, focal dystonia, hypertension, hypotension, constipation, depression, headache, extrapyramidal, hyperprolactinaemia (male –> low libido, erectile dysfunction. Female –> mammoplasia, mastodynia, galactorrhoea, amenorrhoea)

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16
Q

Domperidone

A

D2/3 antagonist (peripherally selective)

Blocks actions of dopamine in the central nervous system’s chemoreceptor trigger zone

Uses: Nausea, gastroparesis (delayed stomach emptying (idiopathic))

ADRs: QT prolongation / sudden cardiac death, hyperprolactinaemia (male –> low libido, erectile dysfunction. Female –> mammoplasia, mastodynia, galactorrhoea, amenorrhoea)

17
Q

Odansetron

A

5HT3 antagonist

Chemoreceptor trigger zone receptor inhibition, Enterochromaffin cells in the small intestine serotonin release inhibition (response to serotonin may be vomiting reflex)

Uses; Nausea (post-op, chemo), morning sickness

ADRs: Constipation, dizziness, headache, QT prolongation/SCD,

18
Q

Paracetamol

A

NOAD (non-steroidal analgesic drug)

Not fully understood, assumed COX2 inhibitor without anti-inflammatory action

Uses: Pain, Fever

ADRs: Liver damage

19
Q

Morphine/Codeine

A

Opiate

mu opioid receptor agonist, mimicking the action of endogenous endorphins, enkephalins and dynorphins (analgesia)

Uses: Pain killing (mild to moderate for codeine, moderate to sever for morphine)

ADRs: Respiratory depression, nausea, vomiting, habituation

Codeine = prodrug form of morphine, converted to morphine in first pass.

20
Q

Tramadol

A

Opioid

mu-opioid receptor agonist, mimicking the action of endogenous endorphins, enkephalins and dynorphins
(analgesia)

Uses: Mild to severe pain (less effective for severe pain than morphine)

ADRs: Respiratory depression, nausea, vomiting, habituation

21
Q

Carbamepazine

A

Anti-epileptic

Stabilises the inactivated state of voltage gated Na channels, affected cells are less excitable. Also a GABA agonist, enhancing the effects of inhibitory nerve impulses.

Uses: Epilepsy, neuropathic pain, (bipolar and schizophrenia (off label))

ADRs: Drowsiness,m dizziness, headaches, motor coordination impairment, CNS depression

22
Q

Lamotrigine

A

Anti-epileptic/Anti-convulsant (Voltage gated sodium channel blocker)

Blocks Nav channels as well as L, N, P type Ca2+ channels. This is thought to reduce glutamatergic activity in projections to the ventral striatum and limbic areas

Uses: Epilepsy (focal, tonic clonic), bipolar

ADRs: Severe skin reactions (toxic epidermal necrosis), rash, aseptic meningitis, double vision, pupil constriction, lack of coordination, anxiety, cough, nausea

23
Q

Phenytoin

A

Anti-seizure (Nav blocker)

Voltage dependent blocker of voltage gated sodium channels, enhancing the inactivation state stability

Uses: Seizures (tonic-clonic, focal, absence, status elepticus), VTach, ATach

ADRs: Severe hypotension, arrhythmias, nystagmus, double vision, sedation, reduction in folic acid in plasma, teratogenic

24
Q

Apomorphine

A

Non-selective dopamine agonist

D1 and D2 agonist

Uses: Alcohol and morphine adiction, Parkinsons (induce ‘on periods’), ED

ADRs: Potent emetic

25
Q

Bromocriptine

A

Dopamine agonist

D2 agonist

Uses: Parkinson’s, pituitary tumours, hyperprolactinaemia, NMS

ADRs: Nausea, orthostatic hypotension, headaches, vomiting

26
Q

Levodopa

A

Endogenous chemical

Converted to Dopamine in the CNS, hence increasing the amount of dopamine available to SNc neurones

Uses: Parkinson’s

ADRs: hypotension, arryhthmias, vivid dreams, hallucination (audio, visual), On/Off oscillations, dyskinesia

27
Q

Selegiline

A

Selective, irreversible MAO-B inhibitor

Inhibition of MAO-B results in more dopamine in dopaminergic synaptic clefts

Uses: Parkinson’s

ADRs: dizziness, dry mouth, muscle pain, nausea, tachycardia, hallucinations, chorea

28
Q

Entacapone

A

Reversible COMT inhibitor

Prevents COMT from metabolising L-Dopa, hence allowing L-Dopa to be more effective, increasing the ‘On’ state of Parkinson’s treatment

Use: Parkinson’s

ADRs: Abdo pain, nausea, dyskinesia, diarrhoea,

29
Q

Donepezil

A

Centrally acting, reversible Acetylcholinesterase inhibitor

Helps treat cholinergic deficit in Alzheimer’s

Uses: Alzheimer’s

ADRs: loss of appetite, GI upset, diarrhoea, difficulty sleeping

30
Q

Memantine

A

NMDA antagonist

Uses: Alzheimer’s (moderate-severe)

ADRs: Confusion, dizziness, headache, hallucinations