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Medicinal Chemistry > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

What theory describes depression?

A

Biogenic amine theory.

Deficiency in NE and 5-HT

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2
Q

What supports the biogenic theory?

A

Drugs that inhibit the reuptake and inhibit metabolism of neurotransmitters

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3
Q

TCAs block the reuptake of what neurotransmitters?

A

NE,DA,5-HT

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4
Q

TCAs can also block what receptors?

A

H1, muscarinic, alpha1 alpha2, D2, 5-HT1, 5-HT2

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5
Q

Which class has a twisted structure?

A

TCAs

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6
Q

TCAs with basic 3’ amine are selective for? 2’ amine?

A

3’ amine = 5-HT
2’ amine = NE
Reuptake transporter

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7
Q

What are the three subclasses of TCAs?

A

Dibenzoazepines
Dibenzocycloheptanes
Dibenzoxepines

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8
Q

How do TCAs differ from typical antipsychotics?

A

Antipsychotics are symmetrical, central ring contains 2 heteroatoms

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9
Q

On a TCA the N-substituent should be what? Why?

A

No longer than a methyl.
Will cause decrease in activity.
Will cause increase in toxicity.

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10
Q

What is bioisosteric?

A

Exchange atom or group to another to create a new compound similar to the parent compound.

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11
Q

The aminoketone drug is used to treat what? Which uptake is blocked?

A

Treats smoking cessation, depression, withdrawal
Blocks DA in ketone form.
Blocks NE when reduce to an alcohol.

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12
Q

What do triazolopyridines do?

A

5-HT2 antagonist
5-HT1 agonist
5-HT reuptake blocker

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13
Q

What are some characteristics of triazolopyridine?

A

Aryl piperazine long chain
Cause hepatotoxicity
Increase sucidial ideation

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14
Q

What is the difference between TCAs and SNRIs?

A

Missing central ring
Cyclohexane in place of aromatic ring
Fewer side effects

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15
Q

What is important about the SNRI that contains an ether off aromatic ring?

A

It is weak DA reuptake inhibitor.

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16
Q

What is important with the SNRI that contains a 3 atom ring?

A

It is used to treat fibromyalgia as well as depression.

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17
Q

What is important about the aryl piperazine long chain that contains an alkyne(triple bond)?

A

It is not a triazolopyridine.

It has a lower risk of hepatotoxicity.

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18
Q

How does the selective a2- antagonist help treat depression?

A

Blocks NE and 5-HT receptors presynaptic

19
Q

The long chain aryl piperazine that contains a 5 member ring, di-amide functions as?

A

5-HT1a agonist
Postsynaptic in limbic cortex
Treats depression

20
Q

The subtype MAO-A metabolizes what?

A

NE & 5-HT

21
Q

The subtype MAO-B metabolizes?

A

DA, phenylethylamines.

22
Q

MAO catalyzes what type of reaction?

A

Oxidative deamination.

Primary amine becomes an aldehyde.

23
Q

What cofactor is needed for MAO to function?

A

FAD becomes FADH.
Radical combination then protonation
Electron transfer then protonation

24
Q

Describe the non selective MAO inhibitors.

A

They contain a hydrazine or hydrazide.

They produce free radicals such as phenethyl, isopropyl, benzyl

25
Q

The non selective MAO that contains a propargylamine, describe its differences.

A

Michael acceptor that alkylates the flavin cofactor.
Conjugated with double and triple bonds.
Its a very reactive electrophile.
Forms an iminium.

26
Q

Describe the selective MAO-A inhibitor.

A

Aryloxypropylamine.
Propargylamine
Blocks metabolism of NE and 5-HT

27
Q

Describe the selective MAO-B inhibitors.

A

Propargylamine
Phenethylamine
Benzylamine- fusion.
Blocks metabolism of DA.

28
Q

Why should patients avoid tyramine when taking an MAOI?

A

Tyramine is converted to a false neurotransmitter

May precipitate hypertensive crisis.

29
Q

Bipolar disorders may result from abnormalities in what?

A

Abnormal G proteins.

Abnormal signaling: adenylase cyclase, phosphoinositide, Na/K/Ca exchange, phospholipase, cAMP

30
Q

What are the causes of bipolar disorder?

A
  1. Genetics
  2. Environment
  3. Stress
  4. Nutrition
  5. Neurotransmitters
31
Q

What are the excitatory neurotransmitters? Inhibitory?

A 
Excitatory= Ne, Da, glu, asp
Inhibitory= gaba, serotonin
32
Q

What causes mania?

What drugs treat?

A

Excess Da and Ne

Da antagonists, a2 agonist

33
Q

What causes depression?

What treats it?

A

Deficiency in Da, Ne, 5-HT

Uptake blockers for da,ne,5-ht and maoi

34
Q

What can cause an increase in Da or NE?

A

Deficiency in GABA treat with benzodiazepine or valproate

Excess glu treat with lamotrigine, lithium

35
Q

What can cause manic episode by disrupting cholinergic-adrenergic balance?
What treatments?

A

Deficiency in Ach.

Treat with cholinesterase inhibitor, central muscarinic agonist

36
Q

What can increase the risk of depressive episodes?

What treatment?

A

Increased Ach levels in CNS

Anticholinergics

37
Q

How do hormones affect bipolar disorder?

A 
Hyperthyroidism = mania
Hypothyroidism = depression
38
Q

What type of pumps can lithium occupy, what effect does it have?

A

Sodium pumps, failure of action potential thus decrease in neurotransmitter release.

39
Q

What are all of the actions of lithium?

A
  1. Suppression IP3 by inhibition of inositol
  2. Normalize G protein, adenylate cyclase
  3. Decrease uptake of 5-HT
  4. Increase sensitivity of 5-HT receptors
  5. Decrease DA synthesis
  6. Increase Gaba activity
  7. Decrease glu activity
  8. Decrease calcium transport into cells
40
Q

What drug can cause nephrogenic diabetes insipidus?

A

Lithium

41
Q

What drug is a succinic semialdehyde dehydrogenase SSD inhibitor? What effect does it have?

A 
Valproic acid
Decrease metabolism of GABA
Blocks GABA uptake
Normalize Na/Ca channel
Decrease inositol and protein kinase C
42
Q

What does the drug containing a diaminotriazine do?

A

Lamotrigine
Blocks voltage sensitive Na and Ca channels
Decrease asp/glu release

43
Q

What receptors do the atypical antipsychotics function at?

A

Weak D2 antagonists

5-HT2a/2c antagonists

44
Q

What drugs block Na and Ca channels?

A

Anticonvulsants

Off label for bipolar disorder

Medicinal Chemistry (3 decks)

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