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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
Ibuprofen
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
26
Diclofenac
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
27
Amitriptyline
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 ```
28
Pregabalin
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
29
Phenytoin
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
Carbamazepine
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
Sodium Valporate
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
Ethosuximide
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
Lamotragine
Anti-epileptic N and P/Q-type Ca2+ channels: expressed at presynaptically (buttons). Mediate calcium entry for neurotransmitter release.
34
Levetiracetam
Anti-epileptic Binds to synaptic vesicle glycoprotein, SV2A and inhibits presynaptic Ca2+ channels, reducing neurotransmitter release.
35
Gabapentin
Block Alpha 2 Delta 1 subunits of N-type Ca2+ channels.
36
Vigatabrin
Anti-epileptic GABA Modulation Synthesis: inhibits GABA Transaminase leads to an increase in GABA levels
37
Ondansetron
Anti-epileptic GABA Modulation Uptake: Inhibits GAT-1 (transporter involved in removing GABA from the synaptic cleft).
38
Tiagabine
Anti-epileptic GABA Modulation Uptake: Inhibits GAT-1 (transporter involved in removing GABA from the synaptic cleft).
39
Perampanel
Anti-epileptic Glutamate receptors Antagonist of AMPA receptors/NDMA
40
Disulfiram
Alcohol addiction Aldehyde dehydrogenase inhibitor
41
Bupropion
Nicotine addiction monoamine (especially dopamine) reuptake inhibitor.
42
Methadone
Opiate addiction opioid agonist
43
Imapramine
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
Phenelzine
Monoamine Oxidase Inhibitor (Irreversible Inhibition of MOA) treatment of atypical depression
45
Moclobemide
Anti-depressant Reversible Monamine Oxidase Inhibitor Side Effects: nausea, agitation, confusion.
46
Citalopram (active enantiomer is escitalopram)
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
Escitalopram
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
fluoxetine
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
Sertraline
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
Venlafaxine
Serotonin Noradrenaline Reuptake Inhibitors (SNRI) Like TCA, block monoamine re-uptake BUT they have no affinity for other targets
51
Trazodone
Serotonin Antagonist and Reuptake Inhibitor (SARI) Antagonism at 5-HT2 and alpha2 adrenergic receptors.
52
Mirtrazapine
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
Tianeptine
Enhancer of serotonin re-uptake, but also has affinity at NMDA/AMPA glutamate receptors
54
Lorazepam
Benzodiazepine Positive allosteric modulators of GABA ``` Side Effects: Change in sleep patterns Daytime sedation Rebound insomnia. Tolerance Dependence. ``` Use of flumazenil in overdose
55
Diazepam
Benzodiazepine Positive allosteric modulators of GABA ``` Side Effects: Change in sleep patterns Daytime sedation Rebound insomnia. Tolerance Dependence. ``` Use of flumazenil in overdose
56
Buspirone
5-HT1A Agonist
57
Sumatriptan
Triptan 5HT1D/B agonist Migraine prevention (Peripherally)
58
framanezumab
CGRP Monoclonal Antibodies Migraine prevention (Centrally)
59
Zolpidem
Hypnotics (Long term use) alpha subunits of GABAa receptors Alpha 1: hypnotic role Alpha 3: anxiolytic effects
60
Donepezil
Acetylcholinesterase Inhibitors Cholinergic forebrain pathways innervating limbic/cortical structures degenerates in AD Inhibiting acetylcholinesterase stops breakdown of acetylcholine Mild to moderate Alzheimers
61
Galamantine
Acetylcholinesterase Inhibitors Cholinergic forebrain pathways innervating limbic/cortical structures degenerates in AD Inhibiting acetylcholinesterase stops breakdown of acetylcholine Mild to moderate Alzheimers
62
Rivastigmine
Acetylcholinesterase Inhibitors Cholinergic forebrain pathways innervating limbic/cortical structures degenerates in AD Inhibiting acetylcholinesterase stops breakdown of acetylcholine Mild to moderate Alzheimers
63
Chlorpromazine
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
fluphenazine
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
Halperidol
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
flupenthixol
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
Risperidone
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
Olanzapine
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
Clozapine
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
Apriprazole
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
Cannabis
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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