Drugs Flashcards

1
Q

Benserazide (Indication + Mechanism)

A

I: With L-Dopa in Parkinsons disease
M:Inhibits DDC (Dopamine decarboxylase) so stopping decarboxylation of Levodopa (L-Dopa) before it crosses the BBB

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2
Q

Name two MOA-B inhibitors and a common problem with prescribing them

A

Seregiline and Rasagiline. Can’t be eaten with cheese/ wine etc as it prevents them being broken down so causes massive hypertensive crisis

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3
Q

Name two COMT inhibitors, what is their MOA?

A

Tolcapone and Entacapone. They inhibit catechol-O-methyltransferase which slows L-Dopa breakdown

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4
Q

Levodopa (I, M, S.E). What is the problem taking Levodopa long term?

A

I: For Parkinsons disease
M: Is L-Dopa (the amino acid precursor to dopamine which can cross BBB)
S.E: Dyskinesia, hypotension, nausea, extreme emotion
Caution: After prolonged use its effects are lowered and side effects increase

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5
Q

Name two dopamine agonists?

A

Pramipexole (oral) and ropinirole (patch)

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6
Q

What is Apomorphine, when would it be given and how?

A

Dopamine agonist which acts rapidly, given via subcutaneous injection. Often for ‘rescue therapy’ when SE’s of Parkinsons have had an acute flare up

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7
Q

Why must Levodopa be taken at least 40min before meals and why should protein rich meals be avoided?

A

L-Dopa competes with protein from the meals for transport across the BBB

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8
Q

What are the NICE guidelines for early Parkinsons treatment?

A

1st Line: Levodopa > dopamine agonist > MOABI

2nd Line: Anticholinergic/ B-Blocker/ Amantadine

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9
Q

Amantadine (I,M)

A

M: Levodopa induced dyskinesia
M: Blocks NMDA receptor so is glutamate antagonist (blocks striatum inhibition of GPi- therefore increased wanted movement, decreased unwanted)

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10
Q

Phenylephrine (I,M,CI, SE)

A

I: Dilates the pupil, also used as a decongestant (vasoconstrictor)
M: Alpha 1 adrenoceptor agonist
CI: Angle closure glaucoma
SE: Photophobia/ blurred vision

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11
Q

Tropicamide (I, M, CI)

A

I: Pupil dilation (mydrasis)
M: Anticholinergic (Blocks M4 receptor- so stops PNS constricting pupil)
CI: Angle closure glaucoma

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12
Q

Pilocarpine (I, M, CI)

A

I: Pupil constriction/ treat glaucoma/ increase saliva production (to treat dry mouth)
M: M3 receptor agonist (So boosts PNS constrictive action)
CI: Don’t give systemically if have asthma/ COPD (due to bronchoconstriction)

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13
Q
Beta Interferons (I, M, SE's)
(Betaferon, avonex, rebif, extavia)
A

I: Treatment of RRMS
M: Bind to type 1 interferon receptors, changing expression of immunomodulatory proteins in the brain, lowering inflammation
SE’s: Skin reaction at injection site, flu like symptoms for 24hrs

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14
Q

Fingolimod (I, M, SE’s)

A

I: Treating RRMS
M: Binds to Sphingosine (S1) receptor, this blocks lymphocytes from leaving lymph nodes (so less in CNS and less inflammation)
SE: Headahce, fatigue, bradycardia, macular oedema

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15
Q

Amitryptiline (I, M, SE’s)

Also applies to Trimpramine and Amoxapine

A

I: TCA Last choice treatment of MDD/ Anxiety
M: Blocks 5-HT and NA reuptake channels in pre-synaptic membrane
SE’s: Dry mouth, blurred vision, drowsiness, weight gain
(Side effects due to additional blocking of histamine and muscarinic ACh receptors)

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16
Q

Name 5 drugs you could prescribe to help with nerve pain:

A

Gabapentin, pregabalin, caramazepine, TCA’s, opioids

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17
Q

What is the NICE recommended treatment pathway for MDD?

A

Try each step for 10wks then increase:
Computerised CBT > CBT > SSRI > SNRI > TCA > MAOI

(Recurrence of depression is the norm, 73% over 15yrs)

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18
Q

Propofol (I,M,SE)

A

I: Induction and maintenance of anaesthesia
Given IV as a bolus- Induce in 45sec (one arm brain time)
M: Positive allosteric modulator of GABA A receptor
SE: Low BP, post operative seizures

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19
Q

Isoflurane (I,M,SE)

Or Enflurane

A

I: Induction and maintenance of anaesthesia
Given inhaled (Small and lipid soluble so crosses alveolar membrane)
M: Reduces GAP junction conduction
SE: Low BP (vasodilation), mucus membrane irritation

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20
Q

Name a common GA given a) IV and b) Inhaled

What is a common side effect of GA’s?

A

a) Propofol
b) Isoflurane
Low BP

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21
Q

Suxamethonium (I,M,SE)

A

I: Short term (4min) muscle relaxant, use for intubation
M: Depolarising, nicotinic ACh receptor agonist
SE: Muscle pain, hyperkalemia, hyperthermia

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22
Q

Atracurium (I,M,SE)

A

I: (non depolarising) muscle relaxant
M: Cholinergic ACh receptor antagonist (no ACh activating motor end plate)
SE: Low BP, flushing
Good as naturally hydrolysis in blood (on stable in acid) so doesn’t need healthy kidneys)

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23
Q

Fentanyl (I,M)

A

100x more potent than morphine
I: Opioid analgesic
M: Binds to u opioid receptors (inhibitory G-proteins which hyperpolarise via blocking of Ca and opening of K)

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24
Q

Neostigmine (I,M,SE)

A

I: Reverse muscle relaxants
M: Reversibly inhibits acetyl-cholinesterase so raises synaptic ACh conc
SE: Blurred vision and bradycardia

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25
Glycopyrrolate (I,M)
I: Dry secretions, slow HR M: Muscarinic antagonist (relaxes smooth muscle and reduces secretions) Used with neostigmine to reverse some of the side effects of increased ACh neostigmine causes
26
Mannitol (I,M)
I: Diuretic, reducing intercranial pressure (ICP), treat cerebral oedema M: Osmotic diuretic, elevates blood plasma osmolarity, drawing fluid out of tissues (also reducing water and Na re uptake in kidney)
27
Paracetamol (M, SE)
M: Inhibition of COX-2 (stopping prostaglandin formation) SE: Renal failure in chronic high dose use Hepatotoxicity, leading to failure within 48hrs in doses over 150mg/kg (21 tablets in 70kg person)
28
``` Sodium Valproate (I, M, SE) Brand name: Depakote ```
I: Treat seizures/ mood stabiliser (i.e. bipolar) M: Inhibits GABA transaminase so increases synaptic GABA conc, so more GABA inhibition SE: Weight gain, dyspepsia, dizziness, drowsiness, NTD in pregnancy (TERATOGEN)
29
Ibuprofen (M, SE, I)
M: NSAID. Non selective COX inhibitor (COX2= decreased prostaglandins, COX1= unwanted GI side effects) SE: Nausea, dyspepsia, GI ulcer/ bleeds I: Beta blockers, anticoag, alcohol
30
Gabapentin (I,M,SE)
I: Neuropathic pain M: Amino acid analogue of GABA, binds to Ca gated channels and reduces Ca entry, reducing excitability SE: Dizziness, weight gain, drowsiness, depression, fatigue
31
Lidocaine (I,M,SE)
I: Local anaesthetic (approx 90min) M: Blocks fast gated sodium channels (prevents depolarisation) SE: Parasthesia (pins and needless). Dizziness and drowsiness if injected too quick
32
What is the mechanism of opioid analgesics?
Binds to mew, delta and K receptors on CNS neurons Close pre-synaptic VG Ca channels (less NT release) Open post-synaptic K channels (hyperpolarise)
33
What are the effects of opioid's on the body?
Analgesia, euphoria, respiratory depression, nausea, constipation, vomitting, depression renal function, pupil constriction, drowsiness TOLERANCE AND DEPENDENCE
34
``` Tricyclic Antidepressants (M, SE) (Amitriptiline, amoxapine, trimipramine) ```
M: Block 5-HT and noradrenaline reuptake transporters, increasing synaptic conc SE: Dry mouth, blurred vision, weight gain (SE Due to additional blocking of post synaptic histamine and muscarinic ACh receptors)
35
Ketamine (I, A)
I: Analgesic or anaesthetic A: Acts on NMDA receptors, also stimulates cardiovascular system
36
Beta-interferons (I,M,SE) | Avonex, Rebif, Betaferon, Extavia
I: Treatment of relapsing- remitting MS (INJECTION) M: Bind to type 1 interferon receptors, changing expression of immunomodulatory proteins in brain (reduces inflammation) SE: Skin reaction at injection site, flu sympt for 24hrs
37
Nataluzimab (I, M, SE)
I: Treatment of MS or crohns M: Monoclonal antibody for alpha4beta1 integrin (which normally allows lymphocytes to move into organs) SE: Opportunistic John Cunningham Virus infection, causing multifocal encephalopathy
38
Baclofen (I, M)
I: To help relieve spasticity in MS M: Agonist at GABA B receptor (GABA inhibits)
39
Methylprednisalone (I,M)
Prednisalone derivative given IV I: Acute inflammation episodes (such as MS) M: Binds to intracellular receptors and modifies transcription and protein synthesis (Prostaglandins and leukotienes)
40
Co-Beneldopa (What disease and what drug combination?)
Treatment of Parkinsons | Combination of L-Dopa (levodopa) and benserazide
41
Selegiline (I,M,SE, Caution) | alternative: rasagiline
I: Slow Parkinson's progression M: MAO-B inhibitor SE: Hypersexuality Caution: Can't take with cheese or wine!
42
Pramipexole and Ropinirole (I, M)
I: Treatment of parkinsons M: Dopamine agonists
43
Entacapone/ Tolcapone (I,M)
I: Treatment for late stage parkinsons M: COMT (Catechol-o-methyl transferase) inhibitor so slows levodopa breakdown
44
Risperidone (I, M, SE)
I: Atypical antipsychotic (Pyschosis, schizophrenia, mania) M: Blocks D2 receptors in limbic system (lowers +ve sympt) Blocks 5-HT2 receptors in mesocortical tract (lowers -ve sympt) SE: Hyperprolactinaemia, weight gain (60-75% blockade for theraputic dose)
45
SNRI (I, M, SE) | Venlafaxine, Duloxetine
I: Depression, anxiety, neuropathic pain M: Inhibits serotonin and noradrenaline reuptake SE: Headache, insomnia, nausea, sexual dysfunction
46
Diazepam (valium)- I, M, SE | Also lorazepam, chlordiazepoxide
I: Benzodiazepine (Short term anxiety, insomnia, anticonvulsant, muscle relaxant) M: Positive allosteric modulator of GABAA receptor SE: Drowsiness, dizziness, reduced coordination and alertness
47
Mirtazapine (I, M, SE)
I: Anti-depressant (MDD) M: Blocks alpha2 adrenoceptors, blocking -ve feedback, increasing synaptic conc SE: Inc appetite, dry mouth, post hypotension, peripheral oedema
48
Give 3 examples of MAO-A inhibitors? | What is a problem prescribing them?
Phenelzine, tranylcypromine, moclobomide (Stop serotonin and noradrenaline breakdown) Can't break down tyramine protein (cheese and wine)- Hypertensive crisis
49
SSRI's (Examples, M, SE)
Fluoxetine, sertraline, paroxetine, fluvoxamine M: Stop serotonin reuptake SE: Nausea, headache, drowsiness, sexual dysfunction INCREASED risk of depression and suicide in children!!!
50
Alteplase (I, M, SE)
I: Thrombolysis (t-pa) M: Blinds to thrombus, converts plasminogen to plasmin which degrades the fibrin matrix SE: Bleeds Lots of complications so give ideally within 3hours, can give upto 4.5hrs. Benefits tail off after 1.5hrs.
51
Pancuronium (I, M)
I: Long acting muscle relaxant in surgical procedures M: Non depolarising ACh blocker at motor end plate Metabolised by liver and excreted by kidneys so clearance can be affected by hepatic or renal function
52
Carbamazepine (I, M, SE)
I: Anticonvulsant (also for nerve pain or bipolar) M: Sodium channel blocker SE: Sedation, ataxia, blurred vision, water retention
53
The elimination of Atracurium from the body is slowed by?
Respiratory acidosis
54
Sodium Thiopental (I, M, SE)
I: Given IV for short term induction (15min) of anaesthesia M: Binds to Cl ionopore at GABA-A receptor, opening GABA for longer, causing inhibition (of brain stem resp centre) SE: Slow recovery time (so not given for maintainance)
55
Potassium Chloride (I and effect on cardiac muscle)
I: Electrolyte replacement and treating hypokalemia | Depolarises cardiac muscle cells and stops them firing AP's
56
What is the difference between typical and atypical antipyschotics?
Typical: Only block D2 (chlorpromazine)- SE's include dry mouth, weight gain, drowsiness and lowered libido Atypical: Block D2 and 5-HT (Rispiridone, clozapine, amisulpride)
57
What would the drugs orpenadrine and procyclidine be used for?
Anticholinergics | Balances cholinergic/ dopaminergic levels so therefore can reduce parkinsonian side effects
58
Clozapine (I, M, SE)
I: Antipyschotic (For treatment resistant schizophrenia) M: Blocks D2 receptors in limbic system (+ve sympt) Blocks 5-HT2 receptors in mesocortical tract (-ve sympt) SE: Agranulocytosis (in ~1%, do regular WBC)
59
Name 5 SSRI's
Citalopram, fluoxetine, sertraline, paroxetine, fluvoxamine
60
Name 3 SNRI's
Venlafaxine, duloxetine, desvenlafaxine
61
Pregablin (I, M)
I: Anticonvulsant for neuropathic pain and seizures M: Binds to alpha 2 delta subunit on VGCa2+ channels to limit Ca influx
62
Lithium (I, M)
I: Treating bipolar M: Mood stabiliser, stabilises glutamate (not too much or too little) by acting on the GluR3
63
Midazolam (I, M)
I: Induction of general anaesthesia M: Positive allosteric modulator of GABA-A
64
Lamotrigene (I, M)
I: For epilepsy, type 1 bipolar and depression M: Blocks Na and Ca channels to inhibit glutamate release
65
What is the most important caution for Semisodium Valproate in a F of childbearing age?
Causes folate anatagonism (glutamate formil transferase inhibition) therefore increasing risk of neural tube defects in pregnancy
66
Etomidate (I, M)
I: Induction of general anaesthesia M: Extends GABA-A opening time, so increases Cl in and causes hyperpolarisation (in reticular activating system)
67
Tubocurarine (I, M)
I: Muscle relaxant for surgery (non-depolarising) M: Antagonist for nicotinic ACh receptor
68
Physostigmine (I, M)
I: Used to treat glaucoma M: Inhibits acetylcholinesterase (increasing synaptic ACh)
69
What are the general effects of benzodiazepines?
Enhance the effect of GABA at GABA-A receptor | Sedative, hypnotic (sleep inducing), anxiolytic (anti-anxiety), anti-convulsant and muscle relaxant
70
In what circumstances is ibuprofen contra-indicated?
Allergies to NSAIDS Stomach ulcers Heart failure Severe liver disease
71
How is codeine different to morphine?
It is a pro-drug (metabolised to morphine)
72
Clopidogrel (I, M, SE)
I: Antiplatlet (prophylactic post stroke etc) M: ADP platelet membrane receptor antagonist SE: Haemorrhage
73
Flumazenil (I, M)
I: Treat benzodiazapine overdose M: GABA-A receptor antagonist NB: Has a v.short half life
74
Naloxone (I, M)
I: Treat opioid overdose M: Opioid receptor antagonist
75
Name a drug which could be used to treat the mania phase of bipolar type 1?
Rispiridone
76
Name 3 drug treatments which could be used for GAD
Citalopram (SSRI), Venlafaxine (SNRI), Pregablin
77
Chlorpromazine (I, M)
I: Typical antipyschotic M: Blocks D2 receptors only
78
Amisulpride (I,M)
I: Atypical antipyschotic M: Blocks D2 (in limbic striatum- +ve sympt) and 5-HT in mesocortical pathway -ve sympt)
79
Haloperidol (I,M)
I: Atypical antipyschotic Blocks D2 and 5-HT receptors Schizophrenia, mania, pyschosis etc
80
Reserpine (I,M)
I: Antipyschotic and antihypertensive M: Reduces catecholamines by blocking ATP/Mg pump which puts them in vesicles
81
Phenytoin (I, M)
I: Anti-convulsant M: Blocks Na channels
82
Ticlopidine (I, M)
I: Anti-platelet. Prevention of thrombosis M: Blocks ADP receptor on platelets