unit 5 drugs Flashcards

1
Q

what is donepezil

A

acetylcholinesterase inhibtor used to treat AD

  • easily enters the CNS and inhibts breakdown of acetylcholine
  • effective tratment for mild to moderae AD when sufficient cholinergic neruons are still present

side effects: mainly autonomic and similar to AChE inhibitors

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2
Q

drugs to treat parkinsons

A

depamine agonists: levodopa and repinrole

monoamine oxidase inhibitors: selegiline and deprenyl

antimuscarinic drugs: benztropine

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3
Q

what is Haloperidol

A

one of the most widely used typical antipsychotics from the butyrophenone class of drugs.

D2 > α1 > D4 > 5HT2A > D1 > H1

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4
Q

what is olanzapine

A

example of a second generation (atypical) drug which can be used for psychosis.

5-HT2A antagonist > D2 antagonist

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5
Q

what is lithium

A
  • small monovalent cation effective against the mainic phase of bipolar disorder
  • can inc serotonin neutrotransmission and dec NE and dopamine neurotransmission
  • causes decrease in precurors for IP3 and DAG synthesis - dec IP3 and DAG when receptors linked to these secondary messangers are activated like muscarinic, α1 and 5-HT2A receptors.
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6
Q

what is imipramine

A
  • Tricyclic antidepressants- heterocyclic compounds (name based on their 3 ringed structure)
  • inhibit reuptake of norepinephrine and serotonin - elevate the conc of them
  • effective in more than 70% of patients but are not used as first lines of treatment due to side effects and drug-drug interactsions
    ex: Imipramine
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7
Q

adverse effects of imipramine

A
  • block caridac sodium channels (simialr to antiarrhythmic quinidine)
  • antagonist muscarinic, histaminic (H1) and α1 receptors: potent antihistamines, anticholinergics and vasodilators (dont want that)
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8
Q

what is fluoxetine

A

brand name = prozac

  • SSRI used to treat depression, panic disorder, anxiety, obsessive compulsive disorder and bulimia
  • less side effects then tricyclics like imipramine but can cause insomnia and sexual dysfunction

* dec reuptake of serotonin

  • also inc sucide rate in youth so dont give to youth
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9
Q

what is phenelzine

A

non-selective and irreversible MAOI

*most widely used MAOI for the treatment of depression

  • decreases metabolism of morepinephrine, dopamine and serotonin
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10
Q

what is bupropion

A
  • antidepressent
  • mechanisms of poorly understoof but modest inhibitor of re-uptake and stimulates release of dopamine and norepinephrine
  • does not block histaminic, adrenergic or muscarinic receptors but still increases dopamine levels (do not use in patietns with psychosis)

*like SSRIs it inhibits CYP2D6 so do not take with other drugs metabolised by that enzyme

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11
Q

what is diazepam

A
  • increases GABAA receptor activation
  • enhances the effect of GABA causing a sedative hypnotic (sleep inducing) and anxiolytic (anti-anxiety) effects
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12
Q

what is phenobarbital

A

barbituarate

  • drugs that act to depress the CNS producing a wide spectrum of effects from mild-sedation to total anesthesia
  • have sedative, hypnotic and anxiolytic activity and also nehance GABA neurotransmission
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13
Q

describe ethanol

A
  • same effects as sedative hypnotics
  • effects are dose-dependent and cause CNS depressino via decreased memrbane excitability and increased GABAA and decrease NMDA receptor activation
  • other effects include:diuresis, decreased myocardial contractility, slurred speech, and impaired judgment.
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14
Q

prescription of clonidine

A

help with autonomic symptoms of withdrawal and low-dose benzodiazepines can be used to treat ethanol withdrawal

*MOA of clonidine described in autonomic and cardiovasuclar pharmacology sections

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15
Q

What is the main excitatory neurotransmitter?

What receptor does it act on?

Mechanism of action?

What decreases the release

what decreases receptor activation

A
  • Glutamate acts on NMDA receptors
  • inc Ca, Na conductance and dec K of the ion channel
  • Morphine, heroin and THC DEC the release of glutamate

PCP and ethanol DEC activation of the receptor

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16
Q

What is the main inhibitory neurotransmitter?

What receptor does it act on?

Mechanism of action?

What decreases the release?

what ____ receptor activation

A
  • GABA acts on GABAA and GABAB receptors
  • GABAA = ion channel, GABA inc Cl conductance

GABAB = G protein, GABA inc K conductance

  • THC, morphine and heroin decrease release of GABA
  • Diazepam, phenobarbital and ethanol inc GABA activation
17
Q

What receptors does acetylcholine act on? what is the mechanism of action at these receptors?

What is an indirect agonist of acetyl choline?

what is a ntagonist of acetylcholine?

A

Acts on:

M1,M3 and M5 G protein receptors: Inc IP3, DAG and dec K+ conductance (excitatory)

M2, M4 G proteins: dec cAMP (inhibitory)

N ion channel: inc Na+ and K+ conductance

Indirect agonsits: donepezil

Antagonist: benztropine

*alzheimers is los of cholinergic projection neurons

18
Q
A
19
Q

What receptors does NE act on and what is the mechanism of action?

What increases the release of NE?

What decreases the release of NE?

What decreases the reuptake?

what decreases the metabolism?

A

α1 G protein receptor: inc IP3, DAG and dec K+ conductance

α2 G protein: dec cAMP (inhibitory)

β1 G protein: Inc cAMP

Inc release = amphetamine and tyramine

dec release = morphine and heroin

dec reuptake: imipramine and cocaine

dec metabolism: phenelzine

20
Q

what receptors does dopamine act on and the mechanism of action?

What increases the synthesis?

what inc release?

what decreases reuptake?

what decreases metabolism?

what is an agonist?

What is an antagonist?

A

Acts on pre and post synaptic D2 g protein receptors

Presynaptic: dec Ca2+ conductance

postsynaptic: inc K+ conductance

inc synthesis = L-DOPA

inc release = amphetamine

dec reuptake = cocaine

dec metabolism = phenelzine and selegiline

D2 agonist = ropinirole

D2 antagonist = haloperidol and olanzapinethe

*parkinsons is loss of nigro-striatal dopamine projection neuron

*excess dopamine neurotransmission in limbic system linked to psychosis/schizophrenia

21
Q

describe the receptors serotonin acts on and the mechanism of action

what increases release?

what decreases reuptake?

what decreases metabolism?

Partial agonists?

Antagonists?

A

5HT1A G protein receptor: dec cAMP and inc K+ conductance

5HT2A G protein: Inc IP3 and DAG and dec K+ conductance

Inc release = amphetamine

dec reuptake = imipramine, fluoxetine and cocaine

dec metabolism = phenelzine

5HT2A partial agonist: LSD

5HT2A antagonist = haloperidol and olanzapine

**reduced monoamine neurotransmission is linked to depression

22
Q

agonist and antagonists to opioid receptor

A

mu receptor

agonist = heroin, morphine and methadone

antagonist = naloxone

23
Q

what binds to cannabinoid receptor

A

= CB1 binds THC

24
Q

what are the 2 receptors olanzapine attacks? which is preferred?

A

5-HT2A > D2

25
Q

what are the two receptors Haloperidol interacts with? which is preferred?

A

D2 > 5-HT2A

26
Q
A
27
Q

whats PCP

A

hallucinogens

NMDA receptor antagonist

28
Q

whats LSD

A

HALLUCINOGEN

5-HT2A partial agonist