Drugs Flashcards
(120 cards)
1
Q
What major neurodegenerative disorder is L-Dopa used in? What is the MOA of L-Dopa?
A
Parkinson’s
L-Dopa is able to cross the BBB - then converted into dopamine by aromatic L-amino-acid decarboxylase - allows the build up of dopamine
2
Q
What disorder is Apomorphine used in? What is its MOA?
A
Parkinson’s
It is a dopamine D2 agonist
3
Q
What disorder is Rotigotine used in? What is its MOA?
A
Parkinson’s
Dopamine receptor agonist
4
Q
What disorder is Cabergoline used in? What is its MOA?
A
Parkinson’s
Long-acting dopamine receptor agonist - high affinity for D2 receptors
5
Q
What disorder is Selegiline used in? What is its MOA?
A
Parkinson’s
Monoamine Oxidase B inhibitor - stops the metabolism of dopamine and enhances its activity in the substantia nigra
6
Q
What disorder is Trihexyphenidyl used in? What is its MOA?
A
Parkinson’s
Selective M1 muscarinic ACh receptor antagonist - partially blocks cholinergic activity in the CNS
7
Q
What disorder is Orphenadrine used in? What is its MOA?
A
Parkinson’s
Antagonist of NMDA receptor; also a muscarinic anticholinergic receptor antagonist
8
Q
What are some of the side effects of trihexyphenidyl?
A
Mydriasis, dryness of mucous membranes and atonic bladder/bowel
9
Q
What disorder is Procyclidine used in? What is its MOA?
A
Parkinson’s
Central muscarinic anticholinergic receptor antagonist
10
Q
What disorder is Entacapone used in? What is its MOA?
A
Parkinson’s
Catechol-O-methyl transferase inhibitor - used to enhance the effects of L-Dopa (increase plasma levels of L-Dopa)
11
Q
What disorder is Tolcapone used in? What is its MOA?
A
Parkinson’s
COMT inhibitor
12
Q
What disorder is Tetrabenazine used in? What is its MOA?
A
Huntington’s
Vesicular amine transporter - depletes serotonin, noradrenaline and dopamine and inhibits the transmission of these
13
Q
What movement disorder is Haloperidol used in? What is its MOA?
A
Huntington’s
Antidopaminergic/antipsychotic drug - affects the D2 receptors
14
Q
What disorder is Olanzapine used in? What is its MOA?
A
Huntington’s
antidopaminergic/antipsychotic drug - antagonises d2 and 5HT2a receptors
15
Q
What movement disorder is Imipramine used in? What is its MOA?
A
Huntington’s
Antidepressant (TCA) - inhibits neuronal uptake of serotonin and noradrenaline
16
Q
What other conditions is Imipramine used in?
A
Depression and pain
17
Q
What movement disorder is Amitriptyline used in? What is its MOA?
A
Huntington’s
TCA - inhibits the uptake of serotonin and noradrenaline
18
Q
What other conditions is Amitriptyline used in?
A
Depression
Neuropathic or cancer pain
19
Q
What are the side effects of amitriptyline?
A
Low BP confusion convulsions dilated pupils hallucinations
20
Q
What receptor/s does morphine act on?
A
mu-opioid receptors
also binds to and inhibits GABA inhibitory interneurones
21
Q
What receptor/s does Pethidine act on?
A
Kappa-opiate receptors (agonist) - it inhibits the release of nociceptive neurotransmitters
22
Q
What receptor/s does Fentanyl act on?
A
Mostly an agonist for mu-opioid receptors
Also binds to kappa and delta receptors
23
Q
What is methadone commonly used for and how does it work?
A
Synthetic opioid that is very similar to morphine (therefore mu agonist) and is used in opioid type drug dependency (such as heroin)
24
Q
What receptor/s does Pentazocine act on?
A
Agonist at the kappa and sigma opioid receptors
weak antagonist action at the mu receptor
25
What receptor/s does Sufentanil act on?
binds to μ-opioid receptors
*works like other opioids by opening calcium-dependent potassium channels
26
What is the other name for paracetamol?
Acetaminophen
27
What is the MOA of paracetamol?
Reduces the active oxidised forms of COX-2
28
What is the other name for aspirin?
Acetylsalicylic acid
29
What is the MOA for aspirin?
Inhibits the COX1 and COX2 enzymes to decrease the formation of precursors of prostaglandins and thromboxanes
30
What is the MOA of Ibuprofen/diclofenac/ketoprofen?
Inhibits the COX1 and COX2 enzymes to decrease the formation of precursors of prostaglandins and thromboxanes
31
What conditions is Rofecoxib used in? What is the MOA?
Osteoarthritis, rheumatoid arthritis and acute pain
| Inhibits COX-2
32
How does codeine (like most opioids) act as an analgesic?
Codeine's analgesic effects are most likely due to conversion to morphine
Opioids close N-type voltage-operated calcium channels and open calcium-dependent inwardly rectifying potassium channels = hyperpolarisation + reduced neuronal excitability.
33
What condition/s is Carbamazepine used in?
Grand mal and psychomotor/focal seizures (epilepsy) and trigeminal neuralgia
**NOT used in absence seizures
34
What is the MOA of Carbamazepine?
inhibits sustained firing by blocking use-dependent sodium channels
Acts as an analgesic due to ability to block synaptic transmission in the trigeminal nucleus
35
What condition/s is sodium valproate used in?
Epilepsy - absence seizures, tonic clonic seizures (grand mal) and complex partial seizures
36
What is the MOA of sodium valproate?
inhibits sodium channels
| inhibits GABA transaminase = increase in GABA (anticonvulsant)
37
What condition/s is Pregabalin used in?
Neuropathic pain, epilepsy, GAD
38
What is the MOA of Pregabalin?
Acts on the alpha2delta subunit of Ca2+ channels - inhibits release of monoamines
39
What condition/s is Duloxetine used in? What is its MOA?
Used for MDD, GAD and neuropathic pain
Inhibits the reuptake of serotonin and noradrenaline
40
What is Lignocaine/Lidocaine used for? What is its MOA?
Local anaesthetic and cardiac depressant (antiarrhythmia)
Stabilises the neuronal membrane by inhibiting ionic flux required for initiation and conduction of impulses
41
What is Bupivacaine used for? What is its MOA?
Local or regional anaesthesia/anaesthetic
Blocks the generation and conduction of nerve impulses - increases the threshold for electrical activation in the nerve
42
What is Prilocaine used for? What is its MOA?
Local anaesthetic
acts of sodium channels on neuronal cell membranes
43
What is Phenytoin used for? What is its MOA?
Tonic-clonic/grand mal and complex partial seizures
Acts on sodium channels on neuronal cell membranes - limits the spread of seizure activity and reduces seizure propagation
44
What is Lamotrigine used for?
Epilepsy and BPD
45
What is the MOA of Lamotrigine?
Inhibits voltage-sensitive sodium channels
Stabilises the neuronal membranes
Modulates presynaptic NT release of glutamate and aspartate
46
What other channel does Lamotrigine act on?
Ca2+ channels
47
What is Topiramate used for?
Control of partial seizures and grand mal seizures
| Can also be used for migraine prevention
48
What is the MOA of Topiramate?
Blocks sodium channels
Augments GABAa
Inhibits glutamate AMPA/kainate signalling
49
What is Lacosamide used for? What is its MOA?
Adjunctive therapy for partial onset seizures
Inhibits sodium channels
50
What is Zonisamide used for? What is its MOA?
Adjunctive therapy for partial onset seizures
Binds to sodium channels and voltage sensitive calcium channels, which suppresses neuronal depolarisation and hypersynchronisation
51
What is Ethosuximide used for?
Absence seizures
52
What type of channel does Ethosuximide act on?
T-type voltage sensitive Ca2+ channels
53
What kind of drug is Clonazepam? What is its MOA?
Anticonvulsant
Allosteric interactions between central benzodiazepine receptors and GABA receptors
Potentiate the effects of GABA
Increases inhibition of ascending reticular activation system
This blocks cortical and limbic arousal
54
What kind of drug is Phenobarbitone? What is its MOA?
Anticonvulsant
Acts on GABAa receptors
Increases synaptic inhibition
Elevates the seizure threshold and reduces the spread of seizure activity from a focus
(may also inhibit Ca2+ channels = decrease in excitatory NT release)
55
What is Levetiracetam used for? What is its MOA?
Adjunctive therapy for partial onset seizures + children with epilepsy
Thought to stimulate synaptic vesicle protein 2A (SV2A)
Inhibits presynaptic Ca2+ channels
Reduces NT release
56
What kind of drug is Tiagabine? What is its MOA?
Anticonvulsant
Targets the GAT-1 transporter
Reduces the removal of GABA from the synaptic cleft
57
kind of drug is Vigabatrin? What is its MOA?
Anticonvulsant
Inhibits GABA transaminase
Increase in GABA
58
What is Perampanel used for? What is its MOA?
Partial onset seizures that may/may not occur with generalised seizures
Non-competitive inhibitor of the AMPA receptor
59
What is Felbamate used in? What is its MOA?
Severe epilepsy
Antagonist of NMDA receptor glycine binding site
May block the effect of the excitatory amino acids
Therefore suppress seizure activity
60
What is Verapamil used for?
Cluster headaches
Angina
Hypertension
61
What type of calcium channels does Verapamil act on? What effect does it have?
Blocks L-type calcium channels
| This reduces ionotropy and chronotropy of the heart
62
What is methysergide used for and what is its MOA?
Used prophylactically in migraine and in vascular headache.
Serotonin antagonist that acts on the CNS- directly stimulating smooth muscle leading to vasoconstriction.
5-HT2B antagonist
63
What are triptans?
Class of migraine specific drugs
| 5-HT1D/B agonist
64
What are CGRP monoclonal antibodies? and give examples
Class of migraine specific drugs
Antibody specifically against calcitonin gene-related peptide (CGRP) as it's been shown that CGRP levels increase during acute migraine attacks.
Examples include erenumab and fremanezumab (end in -mab)
65
What are TCAs?
Tricyclic antidepressants
Prevent the reuptake of 5-HT and NA
Each drug has a different degree of selectivity for monoamines
66
Why do TCAs have side effects
They have an affinity for H1, muscarinic and alpha 1+2 adrenoreceptors
Muscarinic -> dry mouth, blurred vision, constipation
adrenoreceptors -> postural hypotension
67
Give examples of TCAs
Clomipramine
Desipramine
Nortriptyline
protryptyline
68
What are phenelzine, tranylcypromine and iproniazid
Irreversible Monoamine oxidase inhibitors leading to elevated dopamine levels.
Non-selective between MAOa and MAOb so leads to increased tyramine levels from tyramine containing food (cheese effect) leading to high BP and headaches
used to treat Atypical depression (with anxiety, phobia and hypochondria)
69
What is Moclobemide and why is it used
An antidepressant reversibile MAOI with an increased selectivity for MAOa
It is safer than irreversible MAOIs but with side effects of nausea, agitation and confusion
70
What are SSRIs and give an example
Selective serotonin reuptake inhibitor. Have an increased selectivity for serotonin reuptake channels so has no anticholinergic activity. They are safe in overdose but have side effects of nausea, headaches GI problems. Can make symptoms of depression worse in the first few months.
Examples are citalopram (most selective), fluoxetine and paroxetine
71
What is Venlafaxine used for and what class of drug is it
Used to treat depression. It is a serotonin noradrenaline reuptake inhibitor (SNRI)
72
What is Reboxetine and what class is it
Used to treat depression. IT is a noradrenaline reuptake inhibitor (NARI)
73
What is mirtazapine and what is its MOA
Used to treat depression. It is a Noradrenergic and specific seroternergic antidepressant (NaSSA). It Antagonises 5-HT2 and alpha2 adrenergic receptors
74
What is Trazodone used for and what is its MOA
Used to treat depression. It is a Serotonin and Reuptake Inhibitor (SARI). It mainly antagonises 5-HT2 receptors and also inhibits serotonin reuptake
75
What is Agomelatine used for? What is it's MOA? And why might it be preferred to other treatments?
Used to treat depression. It is an agonist at melatonin MT1 and MT2 receptors and an antagonist at 5-HT2c receptors.
It has an onset of effect within the first week and has less sexual dysfunction than SSRIs. There is also no discontinuation syndrome
76
What is the main treatment for Bipolar disorder and what are it's side effects
Lithium salts. It's exact MOA is unknown but is thought to be associated with glutamate. It's side effects are thirst, nausea, fine tremor, polyuria, weight gain, oedema and acne.
77
What is Disulfiram used for and how does it work
Used to treat chronic alcoholism. Irreversible inhibitor of aldehyde dehyrdogenase, an enzyme used in the metabolism of alcohol. This leads to an accumulation of alcetaldehyde giving symptoms of flushing, systemic vasodilation, respiratory difficulties, nausea and hypotension. Feels similar to a hangover.
78
What is clonidine
Used to treat opiate withdrawal, alcohol withdrawal and nicotine dependancy along with many other things. It has a very complex MOA. It acts on alpha2 adrenoreceptors. In the CNS it acts to reduce blood pressure and reduce sympathetic overactivity
79
What is naltrexone used for and what is its MOA
Alcohol dependence and potentially heroin addiction
It is an Opiate antagonist with highest affinity for the mu receptor but also acts at the kappa and delta receptors in the CNS
80
What is Varenicline used for and what is it's MOA
Used for smoking addiction
It is full agonist of alpha7 nicotinic acetylcholine receptors and alpha4beta2 neuronal nicotinic acetylcholine receptor partial agonist
81
What is Donepezile used to treat and what is its MOA
Mild to moderate dementia/Alzheimer's. It is an Acetylcholinesterase inhibitor. This increases Ach levels which can reduce anxiety, improve motivation, memory and concentration. However, this has mixed results on benefits for behavioural changes and has side effects off a loss of appetite, nausea and vomiting
82
What is Galantamine used to treat and what is its MOA
Mild to moderate dementia/Alzheimer's. It is an Acetylcholinesterase inhibitor. This increases Ach levels which can reduce anxiety, improve motivation, memory and concentration. However, this has mixed results on benefits for behavioural changes and has side effects off a loss of appetite, nausea and vomiting
83
What is Rivastigmine used to treat and what is its MOA
Mild to moderate dementia/Alzheimer's. It is an Acetylcholinesterase inhibitor. This increases Ach levels which can reduce anxiety, improve motivation, memory and concentration. However, this has mixed results on benefits for behavioural changes and has side effects off a loss of appetite, nausea and vomiting
84
What is memantine used for and what side effects may be experienced
Moderate to severe Alzheimer's for those that are intolerant to AChE inhibitors
Dizziness, headaches, tiredness and increased blood pressure
85
What is the MOA of Memantine
An NMDA receptor antagonist
Reduces gutamate excitatory neurotoxicity and has a small benefit on slowing the progression of Alzheimer's symptoms
(cognitive aggression, agitation and delusion)
86
What is Tarenflurbil used for and what is it's MOA
Mild Alzheimer' s
| Modulates the activity of Gamma-secretase so that synthesis of Abeta42 is replaced by Abeta38
87
What type of drug is Chlorpromazine and what is it used for
Typical antipsychotic
| Schizophrenia
88
What type of drug is Thioridazine and what is it used for
Typical antipsychotic
| Schizophrenia
89
What type of drug is Fluphenazine and what is it used for
Typical antipsychotic
| Schizophrenia
90
What type of drug is Haloperidol and what is it used for
Typical antipsychotic
| Schizophrenia
91
What type of drug is Flupenthixol and what is it used for
Typical antipsychotic
| Schizophrenia
92
What type of drug is Risperidone and what is it used for
Atypical antipsychotic
| Schizophrenia
93
What type of drug is Olanzapine and what is it used for
Atypical antipsychotic
| Schizophrenia
94
What type of drug is Clozapine and what is it used for
Atypical antipsychotic
| Schizophrenia
95
What type of drug is Quetiapine and what is it used for
Atypical antipsychotic
| Schizophrenia
96
What type of drug is Paliperidone and what is it used for
Atypical antipsychotic
| Schizophrenia
97
What type of drug is Aripiprazole and what is it used for
Atypical antipsychotic
| Schizophrenia
98
What is the difference between typical and atypical antipsychotics
Both are dopaminergic, but atypical antipsychotics are also serotinergic resulting in less side effects
99
What is the MOA of chlorpromazine and what side effects are common
Antagonist of postsynaptic dopamine receptors (D1 to D4) and serotonin receptors (5-HT1 and 5-HT2)
Extrapyramidal side effects include eight gain, a fall in BP, sedation and sexual dysfunction
100
What is the MOA of Thoridazine and what are its side effects
Antagonist of post synaptic D1 and D2 receptors; blocks alpha adrenergic effect; depresses release of hypothalamic and hypophyseal hormones
Side effects: Affects basal metabolism, body temperature, wakefulness, vasomotor tone and emesis
101
What is the MOA of Fluphenazine and what are its side effects
Antagonist of post synaptic D1 and D2 receptors; depresses release of hypothalamic and hypophyseal hormones
Side effects: Affects basal metabolism, body temperature, wakefulness, vasomotor tone and emesis
102
What is the MOA of Haloperidol and what are it side effects
Competitively blocks post synaptic D2 receptors, eliminates domapne neurotransmission. Also has some effect on 5-HT2 and alpha1 receptors
Extrapyramidal side effects: weight gain, fall in BP, sedation, sexual dysfunction
103
What is the MOA of Flupenthixol
Powerful antagonist of D1 and D2 receptors and alpha-adrenergic receptor antagonist
104
How do atypical antipsychotics affect symptoms
D2 antagonism alleviates positive symptoms whilst 5-HT2a antagonism alleviates negative symptoms
105
What is the MOA of Risperidone
Inhibits D2 and 5-HT2a receptors.
| Antagonist of alpha1 and 2 receptors and H1 receptors
106
What is the MOA of Clozapine and what is it's main side effect
Antagonist of D2 and 5HT2a receptors as well as D4 receptor
| Weakens the immune system and causes agranulocytosis
107
what is the drug of choice in refractory schizophrenia
Clozapine
108
What is Zolpidem used for, whats its MOA and how long does it last
persistent vegetative state (and chronic insomnia)
Indirect GABAa receptor agonist - thought to cause thalamocortical overactivity although there is only anecdotal evidence. Has only lasted 4 hours in anecdotal evidence
109
What is Lorazepam
Benzodiazepine
110
What is Temazepam
Benzodiazepine
111
What is Alprazolam
Benzodiazepine
112
What are Benzodiazepines used for and what are their MOA
Anxiolytic and Insomnia
Binds to the postsynaptic receptors in the GABAa ligand gated chloride channel causing a flow of chlorine into the cell resulting in hyperpolarisation and stabilisation of the plasma membrane
113
What is Eszopiclone used for and what is its MOA
Anxiolytic
| Thought to act on the benzodiazepine receptors as an agonist and interacts with GABA receptor complexes
114
What is Suvorexant used for and what is its MOA
Anxiolytic and insomnia
Selective dual agonist of orexin receptors OX1R and OX2R. It causes a decrease in arousal and wakefulness resulting in indirect sleep promotion
115
What is Buspirone used for and what is its MOA
Anxiolytic
Binds to 5-HT1a receptors on presynaptic neurones in the dorsal raphe and postsynaptic in the hippocampus. It binds to D2 receptors
May have indirect effects on other NT symptoms
116
What is Ipsapirone used for and what is its MOA
Anxiolytic
| Partial agonist of 5-HT1a
117
What is Natalizumab used for and what is its MOA
Multiple sclerosis
Binds to alpha4 subunit of integrins expressed on the surface of all leukocytes - prevents immune cells crossing blood vessel walls and causing inflammation
118
What is Alemtuzumab used for and what is its MOA
Multiple sclerosis
| Binds to CD52 antigen preset on most B and T cells
119
What is Mitoxantrone used for and what is its MOA
Used in worsening Relapsed Remitting Multiple sclerosis and secondary progressive multiple sclerosis
Inhibit B cell, T cell and macrophage proliferation and impairs antigen to reduce inflammation
120
What is Fingolimod used for and what is its MOA
Used in relapsing multiple sclerosis
Sphingosine 1-phosphate receptor modulator; therapeutic effect may be due to reduction of lymphocyte migration into the CNS
