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Drugs Flashcards

1
Q

Carbidopa

A

decarboxylase inhibitor (with levadopa as mechanism for reduced conversion to dopamine outside BBB)

Causes nausea due to stimulation of the chemoreceptor trigger zone

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2
Q

Beserazide

A

decarboxylase inhibitor (with levadopa as mechanism for reduced peripheral dopamine conversion)

Causes nausea due to stimulation of the chemoreceptor trigger zone

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3
Q

Ropinirole

A

Dopamine agonist

Side effects: Impulse control disorders, excessive sleepiness, hallucinations

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4
Q

Selegeline

A

MOA-B inhibitor

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5
Q

Tolcapone

A

COMT inhibitor

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6
Q

Pramipexole

A

Dopamine agonist

Side effects: Impulse control disorders, excessive sleepiness, hallucinations

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7
Q

Amantadine

A

In PD, increases dopamine release and inhibits uptake

Side effects: ataxia, slurred speech, confusion, dizziness

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8
Q

Memantine

A

NMDA antagonist

Stimulate Mu Opioid Receptors
- Decreased neuronal excitability (by increasing K+ conductance) and decreased release of neurotransmitters (decreases Ca2+ influx)

Descending Inhibitory pathways

  • Stimulate the periaqueductal gray
  • Inhibit the substantia gelatinosa of the SC (Lamina II)

Limbic System
- Reduces the anxiety of pain.

Moderate Alzheimers (intolerant to Acetylcholinesterase Inhibitor)
Add on drug with Acetylcholinesterase Inhibitors for moderate to severe
Monotherapy in severe Alzheimers

Side effects: Constipation, nausea, respiratory, depression and sleepiness.

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9
Q

Tramadol

A

Weak Opioid via Oral administration

Acts on mu opioid receptors
Interacts with monoaminergic systems

Used for: Post-operative pain or low back pain

Side effects: Nausea, Vomiting, Sweating, Itching, Constipation

In seizures can lower seizure threshold so only used if necessary

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10
Q

Morphine

A

Strong Opioid via Oral, IV, subcutaneous administration

Used for: Post-operative pain, patient controlled analgesia, major trauma

Side effects: Sedation, respiratory depression, constipation, addiction

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11
Q

Methadone

A

Strong Opioid via Oral administration

Used for: Opioid dependence treatment, chronic pain

Side effects: Addiction, sedation, respiratory depression

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12
Q

Baclofen

A

GABA receptor Agonist

Can treat MS, Spinal cord Injuries, Cerebral Palsy

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13
Q

Aspirin

A

Irreversibly binds to COX

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14
Q

Warfarin

A

Anti-coagulant binds to factors II, VII, IX, X (mnemonic 1972)

Side effects: Haemorrhage, teratogenic (can be used in breastfeeding), skin necrosis, purple toes

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15
Q

Rasagaline

A

MAO-B inhibitor

Prevent conversion of Dopamine to DOPAC (in presynaptic neurones)

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16
Q

Tolcapone

A

COMT inhibitor

Prevent degradation from DOPAC to Homovanillic acid

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17
Q

Tetrabanazine

A

Inhibits vesicular storage of dopamine by irreversibly inhibiting Vesicular Monoamine Trasnporter VMAT2

Used in Huntingtons

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18
Q

Amantadine

A

Inhibition of amine uptake, inhibition of MOA activity, release of dopamine from monoaminergic terminals

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19
Q

Levadopa

A

Dopaminergic neurones uptake Levadopa, converted by the enzyme DOPA decarboxylase to dopamine

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20
Q

Rotigotine

A

Post-Synaptic Dopamine Receptor Agonist

Non-selective between D1 and D2. Can be given as a transdermal patch

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21
Q

Chlorpromazine

A

Post-Synaptic Dopamine Receptor Antagonist

Higher affinity for D2 than D1
Used to treat schizophrenia

Side effects:
Extrapyramidal effects:
- Tardive dyskinesia, Dystonia, Parkinsonism, Bradykinesia, Tremor
Weight gain, Postural hypotension, blurred vision, Dry mouth

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22
Q

Haloperidol

A

Post-Synaptic Dopamine Receptor Antagonist

Higher affinity for D2 than D1
Used to treat schizophrenia

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23
Q

Clozapine

A

Post-Synaptic Dopamine Receptor Antagonist

Higher affinity for D2 than D1
Used to treat schizophrenia

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24
Q

Paracetamol

A

Analgesic

Anti-pyretic and analgesic

Decreases prostaglandin E2-induced reduction (reduce prostaglandins)
Inhibits reuptake of endogenous cannabinoids

Side effects: Nausea and GI bleeding

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25
Q

Ibuprofen

A

NSAID

analgesic and anti-inflammatory

Inhibits activity of COX-1 and COX-2 enzymes
Decreases prostaglandin formation and recruitment of leucocytes
Reduces sensitization
Travel across BBB to have same effect on prostaglandin synthesis in the CNS

Side effects: Long term use can lead to peptic ulcers

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26
Q

Diclofenac

A

NSAID

Inhibit the formation of prostaglandins (longer acting than ibuprofen)
Inhibiting phospholipase A2 and reductions in arachidonic acid

Side effects: higher risk of CV complications
Contraindicated in people with IHD and stroke

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27
Q

Amitriptyline

A

Tricyclic Anti-depressant

Inhibits reuptake of amines
Inhibits sodium channels
L-type Ca2+ channels
Subtypes of K+ channels
Acts on NDMA receptors

Overdose = cardiotoxicity

Side effects:
Weight gain
appetite changes
Muscle stiffness, constipation, urinary retention, dry mouth
Postural hypotension
Nausea nervousness, dizziness
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28
Q

Pregabalin

A

Anticonvulsant

Binding to Alpha-2-Delta-1 subunit of N-type voltages gated Ca2+ channels
Reduction in Ca2+ entry = decreased release of neurotransmitters

Side effects:
Drowsiness, dizziness and headaches

Uncommon -
Peripheral oedema, visual problems, weight gain, confusion

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29
Q

Phenytoin

A

Anti-epileptic

Bind to the inner pore of the Na+ channel in its inactivated state, leads to an increased refractory period

T-type Ca2+ channels: require less depolarization to be activated

L-type Ca2+ channels: allow post-depolarization calcium influx and are slowly inactivated. Inhibiting these channels causes inhibition of calcium influx post-depolarization.

30
Q

Carbamazepine

A

Anti-epileptic

Bind to the inner pore of the Na+ channel in its inactivated state, leads to an increased refractory period

T-type Ca2+ channels: require less depolarization to be activated

L-type Ca2+ channels: allow post-depolarization calcium influx and are slowly inactivated. Inhibiting these channels causes inhibition of calcium influx post-depolarization.

31
Q

Sodium Valporate

A

Anti-epileptic

Bind to the inner pore of the Na+ channel in its inactivated state, leads to an increased refractory period

Used in all types of seizures (not in pregnancy)

32
Q

Ethosuximide

A

Anti-epileptic

USED IN ABSENCE SEZUIRES

T-type Ca2+ channels: require less depolarization to be activated

L-type Ca2+ channels: allow post-depolarization calcium influx and are slowly inactivated. Inhibiting these channels causes inhibition of calcium influx post-depolarization.

33
Q

Lamotragine

A

Anti-epileptic

N and P/Q-type Ca2+ channels: expressed at presynaptically (buttons).
Mediate calcium entry for neurotransmitter release.

34
Q

Levetiracetam

A

Anti-epileptic

Binds to synaptic vesicle glycoprotein, SV2A and inhibits presynaptic Ca2+ channels, reducing neurotransmitter release.

35
Q

Gabapentin

A

Block Alpha 2 Delta 1 subunits of N-type Ca2+ channels.

36
Q

Vigatabrin

A

Anti-epileptic

GABA Modulation

Synthesis: inhibits GABA Transaminase leads to an increase in GABA levels

37
Q

Ondansetron

A

Anti-epileptic

GABA Modulation

Uptake: Inhibits GAT-1 (transporter involved in removing GABA from the synaptic cleft).

38
Q

Tiagabine

A

Anti-epileptic

GABA Modulation

Uptake: Inhibits GAT-1 (transporter involved in removing GABA from the synaptic cleft).

39
Q

Perampanel

A

Anti-epileptic

Glutamate receptors

Antagonist of AMPA receptors/NDMA

40
Q

Disulfiram

A

Alcohol addiction

Aldehyde dehydrogenase inhibitor

41
Q

Bupropion

A

Nicotine addiction

monoamine (especially dopamine) reuptake inhibitor.

42
Q

Methadone

A

Opiate addiction

opioid agonist

43
Q

Imapramine

A

TCA

Inhibit reuptake of amines

Have affinity for various other receptors e.g. H1, muscarinic alpha-1 and alpha-2 adrenoceptors.

Overdose = cardiotoxicity

Side effects: dry mouth, constipation, urinary retention, weight gain, postural hypotension, sedation

44
Q

Phenelzine

A

Monoamine Oxidase Inhibitor (Irreversible Inhibition of MOA)

treatment of atypical depression

45
Q

Moclobemide

A

Anti-depressant

Reversible Monamine Oxidase Inhibitor

Side Effects: nausea, agitation, confusion.

46
Q

Citalopram (active enantiomer is escitalopram)

A

Selective Serotonin Reuptake Inhibitor (SSRI)

Increased selectivity for serotonin reuptake

NO anticholinergic activity.
NO cardiotoxic effects.
SAFE in overdose.

Side Effects: nausea, headaches, gastrointestinal problems, increased aggression, insomnia, anxiety, sexual dysfunction.

47
Q

Escitalopram

A

Selective Serotonin Reuptake Inhibitor (SSRI)

Increased selectivity for serotonin reuptake

NO anticholinergic activity.
NO cardiotoxic effects.
SAFE in overdose.

Side Effects: nausea, headaches, gastrointestinal problems, increased aggression, insomnia, anxiety, sexual dysfunction.

48
Q

fluoxetine

A

Selective Serotonin Reuptake Inhibitor (SSRI)

Increased selectivity for serotonin reuptake

NO anticholinergic activity.
NO cardiotoxic effects.
SAFE in overdose.

Side Effects: nausea, headaches, gastrointestinal problems, increased aggression, insomnia, anxiety, sexual dysfunction.

49
Q

Sertraline

A

Selective Serotonin Reuptake Inhibitor (SSRI)

Increased selectivity for serotonin reuptake

NO anticholinergic activity.
NO cardiotoxic effects.
SAFE in overdose.

Side Effects: nausea, headaches, gastrointestinal problems, increased aggression, insomnia, anxiety, sexual dysfunction.

50
Q

Venlafaxine

A

Serotonin Noradrenaline Reuptake Inhibitors (SNRI)

Like TCA, block monoamine re-uptake BUT they have no affinity for other targets

51
Q

Trazodone

A

Serotonin Antagonist and Reuptake Inhibitor (SARI)

Antagonism at 5-HT2 and alpha2 adrenergic receptors.

52
Q

Mirtrazapine

A

Noradrenergic and Specific Serotonergic Antidepressants (NaSSA)

Antagonist at alpha-2 adrenergic receptors
Affinity for histamine H1 receptors
Exert antagonist effects at 5HT2 and 5HT3 receptors

Side Effects: sedation, dry mouth, constipation.

53
Q

Tianeptine

A

Enhancer of serotonin re-uptake, but also has affinity at NMDA/AMPA glutamate receptors

54
Q

Lorazepam

A

Benzodiazepine

Positive allosteric modulators of GABA

Side Effects:
Change in sleep patterns
Daytime sedation
Rebound insomnia.
Tolerance
Dependence.

Use of flumazenil in overdose

55
Q

Diazepam

A

Benzodiazepine

Positive allosteric modulators of GABA

Side Effects:
Change in sleep patterns
Daytime sedation
Rebound insomnia.
Tolerance
Dependence.

Use of flumazenil in overdose

56
Q

Buspirone

A

5-HT1A Agonist

57
Q

Sumatriptan

A

Triptan

5HT1D/B agonist

Migraine prevention (Peripherally)

58
Q

framanezumab

A

CGRP Monoclonal Antibodies

Migraine prevention (Centrally)

59
Q

Zolpidem

A

Hypnotics (Long term use)

alpha subunits of GABAa receptors
Alpha 1: hypnotic role
Alpha 3: anxiolytic effects

60
Q

Donepezil

A

Acetylcholinesterase Inhibitors

Cholinergic forebrain pathways innervating limbic/cortical structures degenerates in AD
Inhibiting acetylcholinesterase stops breakdown of acetylcholine

Mild to moderate Alzheimers

61
Q

Galamantine

A

Acetylcholinesterase Inhibitors

Cholinergic forebrain pathways innervating limbic/cortical structures degenerates in AD
Inhibiting acetylcholinesterase stops breakdown of acetylcholine

Mild to moderate Alzheimers

62
Q

Rivastigmine

A

Acetylcholinesterase Inhibitors

Cholinergic forebrain pathways innervating limbic/cortical structures degenerates in AD
Inhibiting acetylcholinesterase stops breakdown of acetylcholine

Mild to moderate Alzheimers

63
Q

Chlorpromazine

A

Typical Neuroleptics/First Generation Antipsychotic

Block dopamine receptors

Side effects:
Extrapyramidal effects:
- Tardive dyskinesia
- Dystonia
- Parkinsonism
- Bradykinesia
- Tremor
Weight gain
Postural hypotension
Blurred vision
Dry mouth (muscarinic)
Hypothermia
QT interval prolongation
Sudden death
Hyperprolactinaemia.
64
Q

fluphenazine

A

Typical Neuroleptics/First Generation Antipsychotic

Block dopamine receptors

Side effects:
Extrapyramidal effects:
- Tardive dyskinesia
- Dystonia
- Parkinsonism
- Bradykinesia
- Tremor
Weight gain
Postural hypotension
Blurred vision
Dry mouth (muscarinic)
Hypothermia
QT interval prolongation
Sudden death
Hyperprolactinaemia.
65
Q

Halperidol

A

Typical Neuroleptics/First Generation Antipsychotic

Block dopamine receptors

Side effects:
Extrapyramidal effects:
- Tardive dyskinesia
- Dystonia
- Parkinsonism
- Bradykinesia
- Tremor
Weight gain
Postural hypotension
Blurred vision
Dry mouth (muscarinic)
Hypothermia
QT interval prolongation
Sudden death
Hyperprolactinaemia.
66
Q

flupenthixol

A

Typical Neuroleptics/First Generation Antipsychotic

Block dopamine receptors

Side effects:
Extrapyramidal effects:
- Tardive dyskinesia
- Dystonia
- Parkinsonism
- Bradykinesia
- Tremor
Weight gain
Postural hypotension
Blurred vision
Dry mouth (muscarinic)
Hypothermia
QT interval prolongation
Sudden death
Hyperprolactinaemia.
67
Q

Risperidone

A

Atypical Neuroleptics/Second Generation Antipsychotics

Antagonists at D2 receptors as well as antagonists 5-HT2 receptors.

Less prone to give extrapyramidal effects.
• Improve negative effects/cognitive dysfunction

Side effects:
Significant weight gain 
Dyslipidaemia
T2D (insulin resistance)
Metabolic disturbance
68
Q

Olanzapine

A

Atypical Neuroleptics/Second Generation Antipsychotics

Antagonists at D2 receptors as well as antagonists 5-HT2 receptors.

Less prone to give extrapyramidal effects.
• Improve negative effects/cognitive dysfunction

Side effects:
Significant weight gain 
Dyslipidaemia
T2D (insulin resistance)
Metabolic disturbance
69
Q

Clozapine

A

Atypical Neuroleptics/Second Generation Antipsychotics

Antagonists at D2 receptors as well as antagonists 5-HT2 receptors.

Clozapine is used in patients that are drug resistant

Less prone to give extrapyramidal effects.
• Improve negative effects/cognitive dysfunction

Side effects:
Significant weight gain 
Dyslipidaemia
T2D (insulin resistance)
Metabolic disturbance
Neutropenia (clozapine)
70
Q

Apriprazole

A

Atypical Neuroleptics/Second Generation Antipsychotics

Antagonists at D2 receptors as well as antagonists 5-HT2 receptors.

Less prone to give extrapyramidal effects.
• Improve negative effects/cognitive dysfunction

Side effects:
Significant weight gain 
Dyslipidaemia
T2D (insulin resistance)
Metabolic disturbance
71
Q

Cannabis

A

Activation of CB1 stops Ca2+ from entering the presynaptic cell by closing voltage-gates Ca2+ channels

Therefore, CB receptor stimulation can inhibit tremor/spasticity in MS.

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