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Semester 2 2021 > Pccol drugs > Flashcards

Pccol drugs Flashcards

1
Q

Aromatic L amino acid decarboxylase

A

It turns L DOPA into dopamine stopping it from entering clinically relevent site

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2
Q

Inhibitors of Aromatic L amino acid decarboxylase

A

Benserazide and carbidopa

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3
Q

Catechol o methyl transferase

A

It transfers a methyl group onto L dopa, stopping it from going into blood brain barrier.

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4
Q

What inhibits COMT

A

Entacapone, opicapone

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5
Q

What are strategies to improve L DOPA

A

INHIBIT
AADC
COMT
MAOB (monoamine oxidase B)

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6
Q

Dopamine agonists

A

These are compounds that activates dopamine receptors to mimic the effect of dopamine.
They mostly target D2
They are either ergotamine or non-ergotamine

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7
Q

Sideeffects of dopamine agonists

A 
impulse control
disorders
cardiac fibrosis,
excessive day time sleepiness
hallucinations
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8
Q

Interferon beta effects

A

used to treat MS
1) Activate JAK/STAT signalling pathway via type 1 IFN receptors 1 binding=> gene expression=> antiviral, immunomodulatory and antiproliferation effects

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9
Q

interferon Beta side-effects

A

fetal malformations category D
Flu like symptoms, headache, thyroid disorders, autoimmunity, depression, allergic reactions, hepatic injury

FHF DATA

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10
Q

Glatiramer acetate

A

example of myelin basic protein mimics

competes with myelin for myelin reactive T cells
upregulate antiinflammatory responses in macrophages
decreases B cells and T cells
may promote remyelination by increasing proliferation and migration of oligodendrocytes

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11
Q

Glatiramer acetate sideffects?

A

no

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12
Q

Fingolimod

A

Sphingosine 1 phosphate receptor modulator

binds to S1P receptors and stops S1P from causing lymphocytes moving

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13
Q

sideeffects of Fingolimod

A

bradycardia, atriventricular block, opportunistic infections, cutaneous malignancies

heart and infections

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14
Q

Teriflunomide

A

interferes with pyramidine syntehsis and stops DNA replication of proliferating T and B cells

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15
Q

side-effects of teriflunomide

A

This stops T and B cells from proliferating by interfering with pyrimidine synthesis

It causes nausea, diarrhea, paraesthesia, limb pain, liver enzyme changes and hair thinning

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16
Q

Dimethyl fumarate

A

antioxidant. In CNS, it decreases cytokine production by activated microglia/astrocytes and increases number of oligodendrite precursor cells.

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17
Q

Common sideeffects of dimethyl fumarate

A

nausea, diarrhea, vomiting, flushing, upper abdominal pain
chemo drug
hobo3
nausea turns into flushing turns into vomiting

upper abdominal pain turns into diarrhea

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18
Q

cladribine

A

Prodrug phosphorylated to an active purine nucleoside analog that inters with DNA synthesis and repair, leading to cell death•Chemotherapeutic drug: also used to treat leukaemias•Preferentially depletes peripheral B and T lymphocytes, other immune and blood cells are preserved•Significant reductions in relapses and disease progression in RRMS •Resultant lymphopenia increases risk of severe infections, also higher rates of tumors •Oral treatment in short cycles with sustained therapeutic effects•Contraindicated in pregnancy (cat D) with on-going concerns about safety

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19
Q

What are three major classes of typical antipsychotics

A

Psychotic titan Baboons

The typical antipsychotics ameliorate positive symptoms of schizophrenia
their major classes are

1) phenthiazines
2) butyrophenones
3) thioxanthenes

They all are potent D2 dopamine antagnoists
they have moderate affinity for alpha adrenergic and 5HT2 receptors
80% receptor occupancy
weak to moderate affinity for D1 and D4 receptors, histamine and acetylcholine receptors

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20
Q

Classes of atypical antipsychotics

A 
1)diazepines
dibenzothizepine
benzamide
benzisoxazol
quinolinone derivative

Different Dimension BBQ

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21
Q

Function of atypical antipsychotics

A

ameliorate both positive and negative symptoms of schizophrenia

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22
Q

comparison of atypical antipsychotics vs typical antipsychotics

A

atypical can ameliorate both positive and negative whereas typical can only ameliorate positive

fewer side effects for atypical

and effective in treatment resistant patients

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23
Q

How do atypical antipsychotics work

A

They antagonise D2 receptors with 60% receptor occupancy

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24
Q

clozapine

A

type of atypical antipsychotic

high affinity for D4 receptors

rapidly dissociates from receptors

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25
Q

side effects with antipsychotics

A

tina lecture

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26
Q

Benzodiazepines for sleep

A

Hypnotic•Sedative•Anxiolytic •Amnesic (especially with alcohol, Rohypnol/flunitrazepam)•Produce strange sleep behaviors•Antiepileptic•Range of effects due to expression of GABAAreceptors of different make up expressed in different brain regions/neural circuits.•Benzodiazepine sensitive GABAAreceptors in many brain regions including:ØAmygdalaØPrefrontal cortexØHypothalamusØStriatumØBed nucleus of the striatumØHippocampus

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27
Q

GABA a1 subunit

A

regulate sedative/hypnotic, anticonvulsant

28
Q

GABA a2 subunit

A

anxiolytic

29
Q

GABA a3 and a5 subunits

A

myorelaxant

30
Q

z drugs

A

many of same benefits and problems of Benzodiazepines

some show preference for a1

produces bizarre sleep behaviors

31
Q

side effects of z drugs

A

produce bizarre sleep behavior
like daytime sedation
rebound insomnia on withdrawal

32
Q

issues with benzodiazepine

A 
dependence
amnesia
sleep behavior
falls in elderly
dangerous with other sedatives

San Francisco DAD

33
Q

antihistamine

A

Histamine arousing – part of ARAS•First generation H1inverse agonists (often call antagonists) block this arousing effect•Most of the over-the-counter sedatives/hypnotics•X BBB as lipophillic, low molecular weight, not PGP target•Less effective than BZ (not targeting all systems)•More day-time sedation, fog, memory issues even when drug no longer present

34
Q

sideeffects of antihistamine

A

rinary retention (tricyclics, antipsychotics H1antags)

35
Q

Melatonin

A

Endogenous melatonin synthesized in pineal gland (light, via thalamus reduces melatonin production in pineal gland)•Role unclear but participates in circadian rhythm and sleep.•2 GPCR receptors: MT1:activation promotes sleep onset MT2: activation shifts circadian timing•Administration can ‘reset’ sleep pattern but use in non-circadian insomnia unsure•High doses can cause endocrine problems•Ramelteon, synthetic analogue, used for sleep onset problems and has less rebound insomnia, not controlled substance

36
Q

benzodiazepine for anxiety

A

a2 receptor important for anxiety

no selective drug but alprazolam and clonazepam have higher a2 affinity

z drugs not a good choice as some show a1 prefere

37
Q

SSRI for anxiety

A

fluoxetine, paroxetine

selective serotonin reuptake inhibitors
These are often first choice treatment for anxiety
- less side effects than some other drugs- may allow dual treatment for depression- but very slow to act (as for depression)- sometimes side effects difficult- have discontinuation syndrome•If not successful try another class of drugs
38
Q

how do tetracyclic antidepressants work for depression

A

They block a2 adrenoceptors

they increase NA and 5HT release

preferred action on 5HT1

39
Q

how do monoamine oxidase inhibitors work for depression

A

They inhibit the breakdown of noradrenaline and increase the cytoplasmic pool of monoamines to increase leakage of monoamines into synpase/extracellular space

40
Q

How do selective serotonin repuptake inhibitors work?

A

Little action on mACh and histamine receptors •Preferred action of 5-HT on receptors causes side effects !NAT:SERT potencies <0.02 ie: >50 fold selectivity for SERT !cf. TCAs NAT:SERT potencies 10 – 0.2 (i.e. some up to 10 x more selective for NAT, some equipotent and others up to 5x more selective for SERT)

41
Q

examples of monoamine reuptake inhibitors

A

Tricyclic antidepressants
Selective serotonin reuptake innhibitors

serotonin and noradrenaline reuptake inhibitors

noradrenaline reuptake inhibitors

42
Q

How do drugs control seizures( antiseizure drugs)

A

1) modulating voltage gated ion channels-like phenytoin, carbamazepine, lamotrigine
2) enhancing GABA-mediated inhibition-like benzodiazepines

3) interacting with synaptic release machinery
- e/g levetiracetam which binds synaptic vesicle glycoprotein

4) blocking ionotropic glutamate receptors

43
Q

THC

A

Acts on CB1 cannabinoid receptors abundant in cortex, hippocampus, striatum, ventral midbrain and cerebellum. Thc mimics endocannabinoids.

These are presynaptic

44
Q

fatty acid binding protein

A

Transport AEA (anandamide)
it is a fatty acid neurotransmitter and the first endocannabinoid to be discovered.
It is primarily degraded by fatty acid amide hydrolase.
AEA is mediated mostly by CB1 cannabinoid receptors.

45
Q

2AG

A

2 ARACHIDONOYLGLYCEROL is an endocannabinoid and an endogenous agonist of the CB1 receptor and the primary endogenous ligand for CB2. The main difference 2AG has against anandamide is that it is calcium dependent. Broken down by MAGL enzyme

46
Q

Degradative enzymes

A

MAGL (2-AG)

FAAH (AEA)

47
Q

MAGL inhibitor

A

JZL184

48
Q

FAAH inhibitor

A

PF3845

49
Q

nicotine replacement

A

patch, gum, nasal spray, inhaler-eliminates smoke exposure

uncouples temporal cues of smoking from delivery of nicotine

50
Q

Varenicline, cytisine

A

parital agonists -alpha4beta2 nicotinic receptors

They reduce craving, reduce smoking satisfaction

slightly better than NRT

51
Q

Varenicline side-effect

A

nausea

52
Q

Mecamylamine

A

is a non-selective, non-competitive antagonist of the nicotinic acetylcholine receptors

It blocks nicotine reward but has no effect on craving. It can potentially reduce smoking when combined with NRT

53
Q

side effects of mecamylamine

A

significant drowsiness, dizziness and constipation

Different dimension cat

54
Q

Antibodies produced to bind nicotine and preventing it to pass through blood brain barrier

A

No effect on craving

No better than placebo

55
Q

Bupropion

A

is arguably the best approach for long term abstinence. It causes a modest reduction in craving. Mechanism is unknown. Lower seizure threshold and causes sedation

56
Q

Naltrexone for alcohol

A

Naltrexone is an opioid receptor antagonist and it is able to basically stop the feeling of reward of drinking alcohol

57
Q

Disulfiram

A

blocks metabolic enzymes and causes acetaldehyde to build up in liver, making alcohol become extremely unpleasant

58
Q

Acamprosate

A

Used for alcohol addiction
act via inhibition of NMDA receptor

Could also act to change GABA or glutamate synaptic transmission

59
Q

topiramate

A

used for alcohol addiction and epilepsy.

May alter phosphorylation of sodium, calcium, GABA and glutamate receptor channels

Unclear mechanism in addiction-may increase GABA and reduce glutamate synaptic transmission
SIgnificant reduction in drinking but variable results

60
Q

NSAID

A

It inhibits cyclooxygenase and therefore stops the production of inflammatory prostaglandins. this decreases inflammation which is important in migraine theory

61
Q

Ergotamine

A

5HT1d partial agonists
cause vasoconstriction
blocks trigeminal nerve transmission

62
Q

triptans

A

Triptan is a serotonin 1 agonist

5HT1 agonists. tHEY BIND ONTO SEROTONIN RECEPTORS ON BLOOD VESSELS AND NERVE ENDINGS ON BRAIN They inhibit trigeminal nerve transmission peripherally and centrally

They inhibit the release of vasoactive peptides from meningeal blood vessels

They stimulate 5HT1b receptors causing vasoconstriction.

As these blood vessels are constricted, there is less secretion of proinflammatory neuropeptide release including CGRP and substance P

63
Q

side effects with triptans

A

5HT1B receptors are on coronary arteries

64
Q

beta adrenoceptor antagonists

A

propranolol, metoprolol

The Prime Minister has asthma and would die if she had been given beta adrenoceptor antagonists

mechanism of action unknown
not given to people with asthma as side effects include fatigue and bronchoconstriction

65
Q

5HT2 receptor antagonists

A

pizotifen, cyproheptadine, methysergide

prevents 5HT2 receptor induced vasodilation and consequent inflammation

66
Q

side effects of 5HT2 receptor antagonists

A

weight gain, antimuscarinic effects

67
Q

tricyclic antidepressants

A

5HT and NA transport inhibitors. increases 5HT and NA concentrations
inhibition of spinothalamic neurons

Semester 2 2021 (7 decks)

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