drugs Flashcards

Question

Mirtazepine

Answer 1

a2 adrenoceptor antagonist to treat depression range of areas where noradrenaline stored Released to regulate mood

Answer 2

5HT(1A) receptor agonist for anxiety range of areas where noradrenaline stored and released

Answer 3

5HT(1A/D/F) receptor Agonist to treat migrane Trigeminocerebrovascular system involved in migrane generation

Answer 4

Block dopamine transporter to prevent reuptake also at NET and SERT Prolong dopamine action Dopamine mesolimbic pathway Ventral tegmental area of midbrain to nucleus accumbens of forebrain Also Na channel blocker

Answer 5

Antidepressant Block noradrenaline and serotonin transporters prevent dopamine re-uptake to prolongs dopamine action in synapse Range of areas where noradrenaline and serotonin are stored and released affect mood and vegetative behaviours

Answer 6

Block dopamine transporter to prevent dopamine reuptake Prolong dopamine action in synapse Dopamine mesolimbic pathway to reduce nicotine craving

Answer 7

Inhibit MAO-A to reduce monoamine degradation Increases cytoplasmic monoamine concentration and spontaneous leakage into synapse Range of areas where noradrenaline and serotonin stored and released Affect mood and vegetative behaviour Used for depression

Answer 8

Inhibit MAO-B to reduce dopamine degradation Increase available dopamine Nigrostriatal Used for parkinsons

Answer 9

blocks all EAATs Has benzene ring

Answer 10

opioid that binds tightly which inhibits agonist and antagonist binding produces weak signal improves safety low intrinsic efficacy

Answer 11

syngerist between opioid and NA or 5HT pathways Tramadol = u-receptor and SERT Tapentadol = u-receptor and NET means need less morphine for similar effect The modulate descending pathways

Answer 12

inhibit COX1 and COX2 Inhibits prostaglandin release which reduces nociceptors sensitivity Reversible inhibition

Answer 13

release arachidonic acid which is broken down in COX into thromboxane, prostacyclin and prostaglandin (pro-inflammatory mediators) aspirin blocks COX enzymes Inhibits prostaglandin release which decreases inflammation Work best when given early in an attack Act on trigeminal system

Answer 14

activates opioid receptors to reduce Ca2+ influx Reduces Nt release which reduces transmission it can also directly inhibit Addiction, tolerance and overdose common

Answer 15

only N type VGCC blocker approved for chronic pain treatment Mediates Nt release by block Ca2+ influx widely expressed which leads to severe side effects Spinal delivery less tolerance issues

Answer 16

5HT(1D) partial agonist Act at other monoamine receptors Cause vasoconstriction (including coronary vessels) Block trigeminal nerve transmission Adverse effect = nausea and vomiting Not first line

Answer 17

5HT(1B/1D/1F) agonists inhibit trigeminal nerve transmission peripherally (ganglia) and centrally (trigeminal nucleus caudalis) Inhibit release of vasoactive peptide from meningeal blood vessels Stimulate 5HT1B receptors causes vasoconstriction (can't use in CVD) Inhibit release of neuropeptides that cause inflammatory soup Relieve the pain and nausea examples include Sumaptriptan, zolmitriptan, rizatriptan, eletriptan, naratriptan

Answer 18

propranolo and metoprolo have an unknown MOA Side effects are fatigue and bronchoconstriction Contraindications include asthma

Answer 19

pizotifen, cyproheptadine and methysergide prevent 5HT2 receptor induced vasodilation and consequent inflammation Side effects are weight gain, antimuscarinic effects

Answer 20

sodium valproate, gabapentin and topiramate Reduce cortical excitability and alter ion channel activity decrease trigeminal transmission decreased cortical spreading depression Cannot take if pregnant (teratogens) reduce excitability to reduce migrane

Answer 21

Nifedipine and verapamil Decrease Ca2+ entry which reduces cellular excitability Increase reduced sensitisation threshold

Answer 22

5HT and NA transport inhibitors which lead to an increase in available 5Ht and NA which increases inhibition of spinothalamic neurons Block serotonin transport in to have more serotonin binding to reduce pain

Answer 23

CGRP receptor antagonists Compete at sites to prevent CGRP binding which reduces vasodilation can cause live toxicity

Answer 24

Efficacious agonist Its metabolite 6-monoacetylmorphine is more lipophilic than morphine Therefore gets into the brain faster and causes a greater rush inhibit cell that the mu-opioid receptor is on in the brain Get more dopamine release because you are inhibiting the inhibitor (GABA)

Answer 25

mu-agonist which long half life stops withdrawal and craving of heroin without overdose Not as satisfying for abusers combine use with social support to help ween off opioids Still OD risk

Answer 26

occupies opioid receptor and prevents full agonists like heroin having an effect Partial agonism less OD risk than methadone but not all patients are stable on this drug combine with naltrexone to prevent injection

Answer 27

Orally active antagonist Occupies receptor to prevent agonist binding Need to detox before use Poor compliance as does not reduce craving High relapse rate

Answer 28

Agonist at nicotinic receptors Increases release of adrenaline from adrenal glands Get increased BP, HR, respiration and blood glucose Increases alertness, reduces anxiety and tension Increases dopamine release in reward centres Acts at nucleus accumbens and prefrontal cortex Fast response is what allows the association to be drawn

Answer 29

Patch, gum, nasal spray or inhaler Eliminates smoke exposure Agonist at receptor therefore reduces craving Breaks the cue of cigarette with hit Should be done with CBT

Answer 30

Varenicline (alpha 4 veta 2) and cytisine Reduce craving and smoking satisfaction Side effects like nausea, sleep issues May be better than nicotine replacement therapies

Answer 31

mecamylamine block nicotine reward but no effect on craving Side effects include drowsiness, dizziness and constipation May help reduce smoking when combined with nicotine replacement therapy

Answer 32

antibodies produced that bind nicotine and prevent it crossing the BBB No effect on craving and no better than placebo May have a role in at risk groups and prevention

Answer 33

antidepressant with an unclear MOA some reduction in craving (may be due to inhibiting dopamine uptake) lowers seizure threshold and causes sedation similar effect to replacement therapy

Answer 34

Enhances GABAergic and glycinergic synaptic transmission Leads to increased inhibition Inhibition of Ca channels and activation of K+ channels Get inhibition of glutamate receptor function and inhibition of adenosine transport Effects occur everywhere Individual genetic differences in these proteins contribute to addiction potential may stimulate reward pathway by reducing GABA transmission and allowing dopamine to be more active acts in PFC, amygdala, hippocampus and cerebellum

Answer 35

causes unpleasant flush, palpitations and nausea when consuming alcohol Take before high risk events does not effect craving

Answer 36

may act inhibition of NMDA or may change GABA or glutamate synaptic transmission

Answer 37

Antiepileptic and may alter phosphorylation of Na+,Ca2+, GABA and glutamate receptors/channels May increase GABA and reduce glutamate synaptic transmission reduces drinking but results vary

Answer 38

Increase EndoCBs as they are inhibitors of FAAH which degrades anandamide Therefore have more anandamide around which is an endocannabinoid

Answer 39

Modulate voltage gated ion channels Inhibition and enhancement of inactivation

Answer 40

enhance GABA mediated inhibition Tigabine inhibits GABA transporter 1 positive allosteric modulators May boost GABA in synapse to increase inhibition Benzodiazepines

Answer 41

Interact with synaptic release machinery Bind synaptic vesicle glycoprotein (SV2A)

Answer 42

Block ionotropic glutamate receptors (AMPA)

Answer 43

inhibit Ca2+ channel which block them and stop the release of neurotransmitter Can reduce excitation

Answer 44

Not sure if this works - they assume it just increased the actions of clobazam which led to greater inhibition thus leading to reduces seizures

Answer 45

block NA or 5HT transporters which increases levels of NA and 5HT in the synapse TCAs - block mACh, 5HT, histamine and a-adrenoceptors. Have a narrow TI and they strongly potentiate alcohols effects (high anticholinergic and CVD side effects) SSRI - some action on mACh and histamine. Main action on 5HT (high CNS and GIT side effects and cause increased violence, aggression and suicide behaviours - decrease overtime)

Answer 46

inhibit breakdown of NA, 5HT and DA which increases available monoamines Increase leakage of monoamines into synapse and extracellular space Can cause cheese reaction which is fatal Irreversible and non-selective

Answer 47

block a2 adrenoceptors which increases NA and 5HT release Preferred action on 5HT1

Answer 48

effective for mild-moderate depression short term = inhibit 5HT, NA, DA, GABA and glutamate reuptake. Reduces NA gradient reduces transport Long term = downregulate postsynaptic ß-adrenoceptors and increase post-synaptic 5HT1A and 5HT2 receptors Induces CYP34A so cannot take drugs metabolised by this enzyme or will cause OD

Answer 49

5-hydroytryptophan used for depression precursor to 5HT to boost serotonin levels

Answer 50

can promote onset of sleep Selective (increased affinity) for GABA(A) receptors and increases the number of channels open and opening time which allows more GABA out and more inhibition May act at amygdala, PFC, hypothalamus, striatum, bed nucleus of striatum and hippocampus acts at a1, a2, a3 and a5 (a1 is sedative, a2 and 3 anxiolytic and a3 and a5 myorelaxant Should really only use for one month and should be tapered off

Answer 51

Zolpidem, Zaleplon and Eszopiclone less memory/cognition side effects than BZ Some preference for a1 May produce bizarre sleep behaviours Don't cause daytime sedation But when you stop taking them insomnia may get worse

Answer 52

histamine is arousing H1 inverse agonists block this effect Cross BBB (lipophilic), have low molecular weight and are not PGP target less effective than BZ as don't target all systems Get more daytime sedation, fog, memory issues and lots of side effects

Answer 53

Has a role in circadium rhythm 2 GPCR receptors (m1 activates sleep onset and m2 shifts circadium rhythm) can cause endocrine issue in high doses Ramelteon (synthetic analogue) has less rebound insomnia and is used for issues with sleep onset

Answer 54

not first line Act rapidly but can cause drowsiness a2 and a3 subunit are what are important Acts in the amygdala alprazolam and clonazepam have higher a2 affinity

Answer 55

Bind and stop reuptake which elevates 5HT outside the cell = greater activation 5HT released from raphe nucleus Fluoxetine and paroxetine have less side effects but can be slow acting with some side effects

Answer 56

Pregabalin - acts at alpha2delta subtype of VGCC to increases GABA levels Buspirone - partial 5HT1a agonist for treatment of generalised anxiety disorder. Gi/o coupled receptor with strong expression in amygdala, hippocampus, cortex, DR and septum (targets range of regions) Sometimes use TCAs and MAOIs or SNRIs (duloxetine and venlafaxine)

Answer 57

ameliorate pos symptoms but have little effect on neg and cognitive symptoms potent D2 receptor antagonists with moderate affinity for a-adrenergic and 5HT2 receptors (80% receptor occupancy) Weak to moderate affinity for D1 and D4 receptors, histamine H1 and mACh receptors e.g. phemothiazines, butyrophenones and thioxanthenes

Answer 58

diazepines, dibenzothiazepines, benzamides, benzisoxazols and quinolinone Ameliorate both pos and neg symptoms Greater therapeutic efficacy with fewer side effects effective in treatment resistant patients antagonise D2 receptors with high affinity and/or selectivity (60% receptor occupancy) high affinity for 5HT2 receptors (except benzamides) moderate affinity for a-adrenergic (except benzamides) and D3 receptors Clozapine and olanzapine have high affinity for D4 receptors

Answer 59

Crosses the BBB and can be taken up by neurons and converted into dopamine (however can be converted in periphery) Take with inhibitor of dopa decarboxylase to prevent conversion in periphery AADC (Benserazide and carbidopa) allow more L-DOPA to cross BBB COMT (Entacapone, opicapone, tolcapone) helps with BBB crossing and can also make sure synaptic dopamine sticks around for longer in central system so stops breakdown in synaptic cleft MAOB (rasagiline, selegiline and safinamide) stop dopamine breakdown in synaptic cleft can cause dyskinesia

Answer 60

Directly stimulate DA receptors Use dependent on surviving DA neurons (can't give L-DOPA when neurons are dead) D2R (pramipexole, ropiniole ad piribedil) D1R (apomorphine and rotigotine) Side effects include impulse control disorders, cardiac fibrosis, excessive daytime sleepiness and hallucinations

Answer 61

antagonise the mAChR can be associated with delirium and confusion Amantadine (symmetrel) is a NMDA receptor antagonist which leads to a reduction in glutamatergic overactivity in STN

Answer 62

cholinesterase inhibitors and NMDA antagonists May use antidepressants and neurleptics (modulate NA and 5HT neurotransmission to help with cognition) just used to halt the symptoms but do not effect the disease pathology

Answer 63

SS-secretase inhibitors or Y-secretase inhibitors to target pathology APOE - cholesterol transport and reuptake antibiotic clioquniol and lipoic acid chelate zinc reduce plaque formation in animal studies immunisation with ß-amyloid to reduce plaque formation

Answer 64

enhance learning and memory and facilitate flow of information between hemispheres enhance resistance to chemical or physical assault Piraxetam and pramiracetam enhance release of ACh which has shown cognitive enhancement in rats

Answer 65

looks like serotonin indul core with 2 carbon chain and amine on tail Psilocybin and psilocin which are 5HT2A/2C and 1A agonists that produce perceptual distortion (may help with depression) DMT short psychedelic trips with vivid hallucinations and ego death they agonise various 5HT receptors

Answer 66

looks like dopamine potent 5HT2A agonists Mescaline 5HT1A/2A/2C agonist with effects like altered sense of time, thinking processes and closed eye visual hallucinations 2C-B combination of MDMA and LSD. Entactogen hallucination effects vary dependent on dose Bromo-dragonfly long lasting 2-3 days and selective for 5HT2A

Answer 67

combination of phenthylamine and tryptamine LSD is very potent and produces euphoria, auditory and visual hallucinations, vibrant colours etc. With high doses causing ego death and perceptual distortions LSB less potent than LSD Ergotamine 5HT2A full agonist but acts at 5HT2B/2C and some 5HT1 receptors as well. Also dopamine D2. not psychoactive and used to treat migranes (but can be made into LSD so heavily controlled)

Answer 68

stimulant, entactogen, empathogen with psychedelic properties causes neurons to dump serotonin May help with PTSD

Answer 69

dissociative anaesthetic with hallucinogenic, euphoric and psychedelic properties May help with depression as it adjusts the signalling

drugs Flashcards

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