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House Pharmacology > Antidepressants and antianxiety > Flashcards

Antidepressants and antianxiety Flashcards

1
Q

Biologic hypothesis of depression

________
_____________ theory
_______ – _______

A

Genetics
Monoamine theory
Hormonal – Neuroendocrine

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2
Q

Monoamine theory of depression

Due to a deficit in the monoamine transmitters –___________ and _________ in some regions of the brain

A

norepinephrine and serotonin

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3
Q

Monoamine theory of depression

Supportive evidence
•The monoamines play a role in _________

•Antidepressants act by facilitating __________

•Drugs that ______________

A

arousal and mood

noradrenergic and serotonergic transmission

block monoaminergic synthesis and storage

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4
Q

Examples of drugs that block monoaminergic synthesis and storage

???

A

reserpine, alpha-methyltyrosine, methyldopa

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5
Q

Monoamine hypothesis
Research evidence against monoamine hypothesis

Although levels of norepinephrine and serotonin are increased immediately,
therapeutic effects are seen at _____
Likely a trophic factor

A

2-3 weeks

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6
Q

Neuroendocrine

Depressed patients have a (low or high?) level of cortisol and does not (rise or fall?) when _______________________ test is carried out

This is thought to occur as a result of a deficiency of _____________ to the __________

A

High; fall

dexamethasone suppression

noradrenergic and serotonergic input

hypothalamus

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7
Q

Neuroendocrine

Hypothalamus secretes corticotrophin releasing hormone (CRH) which stimulates the pituitary gland to produce ACTH and this further stimulates cortisol

________ level is also increased
_______ hormone is reduced

A

Prolactin

Growth

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8
Q

Other hypothesis of depression

Low levels of brain derived __________ factors

Increased cortical _______ levels

____________________

A

neurotrophic

glutamate

Neurodegeneration

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9
Q

What antidepressants are?

Drugs used to treat depression- by ___________

Mainly (inhibitory or excitatory?) to increase monoaminergic transmission

A

elevate mood

excitatory

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10
Q

Classification of antidepressants

Reversible monoamine oxidase inhibitor (RIMA) –_________,_______

Selective serotonin reuptake inhibitor –_____,_______,_______,_______,________,_______,________

A

moclobemide, clorgyline

fluoxetine, fluvoxamine, paroxetine, sertraline, citalopram, escitalopram, dapoxetine

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11
Q

Classification of antidepressants

____________(RIMA)

_________ antidepressant
Selective ____________ inhibitor

Serotonin and ———————-

______ antidepressants

A

Reversible monoamine oxidase inhibitor

Tricyclic antidepressant

Selective serotonin reuptake inhibitor

Serotonin and noradrenaline reuptake inhibitors

Atypical

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12
Q

Atypical antidepressants – ______,_______,_________,______,______,_____________

A

trazodone, mianserin, mirtazapine, bupropion, atomoxetine, tianepine

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13
Q

Serotonin and noradrenaline reuptake inhibitors – ________,_______

A

venlafaxine, duloxetine

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14
Q

Monoamine oxidase

MAO – a ___________ enzyme , ________________________ of amines like adrenaline, noradrenaline , dopamine, serotonin

A

mitochondrial

oxidative deamination

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15
Q

Monoamine oxidase

Two type
MAO –A – Present in _____ nerve endings, _________ and human ______. Preference for _______ and _______

MAO –B –Present in _________ areas in the ________ and ________. Preferentially deaminates _________.

A

adrenergic; intestinal mucosa; placenta
5-HT and NA.

serotonergic

brain and platelets

phenylethylamine

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16
Q

Monoamine oxidase

___________ is degraded equally by MAO –A and MAO-B

A

Dopamine

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17
Q

Monoamine oxidase inhibitors

Irreversible – _______ ,———,_______

Reversible
MAO –A __________,__________

MAO –B _____________

A

phenelzine, tranylcypromine, isocarboxazid

Moclobemide, Clorgyline

Selegiline

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18
Q

Selegiline is not used in depression.

T/F

A

T

Antidepressant only at high doses

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19
Q

Irreversible monoamine oxidase inhibitors

(Selective or Non-selective?)

No longer in use because of _________ and _____________

A

Non-selective

drug drug interactions and drug –food interaction (cheese) etc

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20
Q

Irreversible monoamine oxidase inhibitors

Inhibits the enzyme irreversibly – action lasts about ________ until new enzymes are synthesised

A

3 weeks

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21
Q

Irreversible monoamine oxidase inhibitors

Cheese reaction – reaction with ______, some ___,________,_________ extracts.

Release (small or large?) amount of _____ from adrenergic neurons

Leading to dangerous ______________

A

cheese

beers, wine and yeast

Large ; noradrenaline

hypertensive crises

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22
Q

Reversible inhibitors of MAO –A

Moclobemide –

•reversible and (selective or non-selective?)
•Duration of action is ______
•Indicated for ____________ depression

•Less adverse reaction – can be displaced by _______ from enzyme binding site

•Adverse effects – nausea , dizziness

•Drug interactions – rare, caution when prescribing with _____________ and _________

A

selective; 1-2 days

mild to moderate

tyramine

other antidepressants and pethidine

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23
Q

Tricyclic antidepressants

Uptake blocker – inhibit ————- and _________ at the ——— and ——— membranes.

Prolonged accumulation of the monoamines lead to the _______ of the inhibitory presynaptic ______,_______, and _________ auto receptors.

There is also an adaptive change in the postsynaptic receptors leading to _________ noradrenergic and serotonergic transmission.

A

norepinephrine and serotonin transporter

neuronal and platelet ; desensitization

alpha 2, 5HT1A and 5HT1D

enhanced

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24
Q

Tricyclic antidepressants

Inhibits other receptors
_____ adrenergic,

________ receptors

histaminergic effects H__

5-HT__ and 5-HT___

D___ -

A

Alpha

Muscarinic

H1

5-HT1 and 5-HT2

D2 -

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25
Q

Pharmacological actions of Tricyclic antidepressants

CNS - Clinical effects seen within _________ of treatment because there is upregulation of the ________ and _______ receptors in the CNS.

Improved ______ pattern.

A

2 -3 weeks

serotonin and Noradrenaline

sleep

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26
Q

Pharmacokinetics of Tricyclic antidepressants

(Poorly or Well?) but (slowly or rapidly?) absorbed

(Mildly or Highly?) plasma and tissue protein bound

(Small or Large?) vol. of distribution

Metabolism – hepatic microsomal enzyme

A

Well; slowly

Highly ; Large

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27
Q

Pharmacokinetics of Tricyclic antidepressants

Imipramine is ________ to an (active or inactive?) metabolite called __________

Amitriptyline is similarly ________ to __________

(Short or Long?) half-lives

A

demethylated

Active ; desipramine

demethylated; nortriyptyline

Long

28
Q

Adverse effects of Tricyclic antidepressant

________,___________,__________

_____eased appetite and weight ____

A

Sedation, mental confusion , weakness

Incr; gain

29
Q

Adverse effects of Tricyclic antidepressant

Anticholinergic effects –____ mouth, bad taste , (constipation or Diarrhea?) , urinary _______, ________ vision

Lowers ______ threshold and causes ______ in cases of overdose. – less likely with _______ and ________

A

dry; constipation; retention; blurred

seizure; seizures

amitriptyline and imipramine.

30
Q

Adverse effects of of Tricyclic antidepressant

CVS –
______cardia

ECG changes and cardiac arrhythmias – disturbs ___________ especially in the ______

postural _________ –_____ blockade and inhibition of ________

A

Tachy

intraventricular conductance

elderly

hypotension; alpha 1

CVS reflexes

31
Q

Tolerance and dependence of Tricyclic Antidepressant

Tolerance to ________ and ________

Dependence (low or high?).

A

anticholinergic and hypotensive

Low

32
Q

Drug interactions of Tricyclic antidepressants

Potentiates the action of _____________

Abolishes the antihypertensive effect of _______ and _______ by preventing their _____________________

Potentiates _____ depressants

_____ ,________ displaces TCA from their binding sites causing toxic effects

A

direct sympathomimetics

guanethidine and clonidine; transport into adrenergic nerves

CNS

Phenytoin , aspirin

33
Q

Selective serotonin reuptake inhibitors

Selectively inhibit membrane associated serotonin transporter

T/F

A

T

34
Q

Selective serotonin reuptake inhibitors

(More or Less ?) efficacy compared to TCA especially in severe depression

(more or less?) tolerable

(more or less?) sedative, cognitive, psychomotor effects

______ anticholinergic and alpha adrenergic effects

_____ effect on seizure threshold.

A

Less; more

Less

no

no

35
Q

———- are the First line drugs in depression

A

Selective serotonin reuptake inhibitors

36
Q

Selective serotonin reuptake inhibitors is also used for other conditions like anxiety, phobia and obsessive and compulsive disorders

T/F

A

T

37
Q

Adverse effects of Selective serotonin reuptake inhibitors

Nausea – _____________ stimulation

Nervousness, restlessness, headache, (constipation or diarrhoea?)

Epistaxis, ecchymosis and increased NSAIDS associated blood loss – impairment of _________

A

5HT3 receptor

diarrhoea

platelet function

38
Q

Adverse effects of Selective serotonin reuptake inhibitors

_______– 5HT3 receptor stimulation

Nervousness, restlessness, headache, diarrhoea

_______,_________ and increased ____________ associated blood loss – impairment of platelet function

A

Nausea

Epistaxis, ecchymosis

NSAIDS

39
Q

Drug interactions - SSRI

SSRI are enzyme (inducers or inhibitors ?) leading to ______ levels of TCAs, haloperidol, clozapine, warfarin

Serotonin syndrome – when a patients takes a ____________________ with SSRI.
______,_________,________, and _______

A

inhibitors

elevated

serotonergic drug

Restlessness, agitation, sweating and convulsions

40
Q

Serotonin norepinephrine reuptake inhibitors

Include _______ and _________

More specific for ________ and ________ transporter

A

venlafaxine and duloxetine

serotonin and norepinephrine

41
Q

Serotonin norepinephrine reuptake inhibitors

More likely to cause ____tension compared to SSRI

A

hypo

42
Q

Which is more likely to cause hypotension

SNRI or SSRI

A

Serotonin norepinephrine reuptake inhibitors are More likely to cause hypotension compared to SSRI

43
Q

Atypical antidepressants

Includes _______,__________,__________

________ mechanism of action

A

trazodone, mianserin, bupropion

Variable

44
Q

Uses of antidepressants

Endogenous and major ________
___________ disorders
______ disorders
____________ pain

______________ disorder
______
Migraine
Pruritus

A

depression; Obsessive compulsive

Anxiety ; Neuropathic

Attention deficit hyperactivity

Enuresis

45
Q

Antianxiety drugs
Anxiety disorders are _________ _______ characterized by _______,_________ and concerns or fear about some defined or undefined future threat

A

unpleasant emotional statesm

uneasiness, discomfort

46
Q

Antianxiety drugs

Drugs used to treat these disorders have ___________ effects

A

CNS depressive

47
Q

Classification of antianxiety drugs

List 5

A

Benzodiazepines
Azapirone
Sedative antihistamines
Beta blocker
Selective serotonin reuptake inhibitors

48
Q

Classification of antianxiety drugs

Benzodiazepines – ______,_____,_____,____, and _____
Azapirone –_______,_____,______

Sedative antihistamines- _________

Beta blocker – _________

Selective serotonin reuptake inhibitors

A

diazepam, alprazolam, lorazepam, oxazepam and chlordiazepoxide

Buspirone, Gebiprone, Ispapirone

Hydroxyzine

Propanolol

49
Q

Buspirone
No ______ action

(More Or Less?) likely to cause sedation , cognitive impairment

No ________ or ____________ effect

(More or Less ?) likely to cause tolerance or dependence

A

GABA

Less

anticonvulsant or muscle relation

Less

50
Q

Versus

SSRI
_______,________
_______,_________,_______,_________

SNRI
_______,_____,———-,_________,_________

A

Fluoxetine, Paroxetine, Sertraline, Citalopram, Escitalopram, Fluvoxamine

Venlafaxine Duloxetine Desvenlafaxine

Levomilnacipran Milnacipran

51
Q

TCA :Secondary amines
List 4

TCA: Tertiary amines
List 5

MAOl
List 5

A

– Nortriptyline
– Desipramine
– Protriptyline
-Amoxapine

Amitriptyline Imipramine Trimipramine Clomipramine Doxepin

Tranylcypromine Phenelzine Moclobemide Selegiline Isocarboxazid

52
Q

SARI
________,__________

Atypical
______,———,_______,———-,_______

A

Trazodone
Nefazodone

Mirtazapine Bupropion Vilazodone Vortioxetine Varenicline

53
Q

MECHANISM OF ACTION

SSRI
__________ of ____________ in synaptic cleft
– Thus ______ease in _______ levels

SNRI
_________ of ___________________ in synaptic cleft
– Thus ____eased ___________________________ levels

A

Inhibition of serotonin reuptake

Increased ; SEROTONIN

Inhibition of norepinephrine reuptake reuptake

Increased; SEROTONIN and NOREPINEPHRINE

54
Q

Mechanism of Action

TCA
–________ of __________ in synaptic cleft
– Thus _____ease in _______ and _______ levels

MAOI
– (Selective or Nonselective?) inhibition of _________________
– Thus ____eased ______ and _____eased accumulation of, ————-,______,———

A

Inhibition; norepinephrine reuptake

Increase in SEROTONIN and NOREPINEPHRINE

Nonselective ; monoamine oxidase enzyme

Decreased; breakdown; increased

NOREPINEPHRINE, SEROTONIN, epinephrine

55
Q

Mechanism of action

SARI and Atypical
– Block _________________ receptors leading to ____eased activity of _______________ receptors in the CNS

A

postsynaptic type 2 serotonin

Increased

SEROTONIN of type 1 receptors

56
Q

Mechanism of action

– SARI
(Weak or Strong?) inhibition of ___________ leading to ______ease in ______ levels

– Atypical
(Selective or Non-selective?) ______________ causing ___eased ________________________________

A

Weak; serotonin reuptake

Increase; SEROTONIN

Selective; α2-adrenergic antagonist

Increased; SEROTONIN and NOREPINEPHRINE release

57
Q

Adverse effects

SSRI
–_________ disturbance
– ______ dysfunction
–________
– _______
– ____________ syndrome

A

Gastrointestinal

Sexual

Insomnia

Sedation

Serotonin

58
Q

Serotonin syndrome occurs when SSRIs are _____________________

A

combined with MAOI

59
Q

Serotonin syndrome

List the characteristics

A

S hivering
H yperreflexia
I ncreased temperature
V ital signs instability
E ncephalopathy
R estlessness
S weating

60
Q

ADVERSE EFFECT
SNRI
– Similar side effect to _____
– _____tension
– ____lytics
– Insomnia
– Hyper______

A

SSRI

Hyper

Anxio

lipidemia

61
Q

ADVERSE EFFECT
TCA
–____________/________ ————
– _____toxicity
– Tremor
– Weight _____
– _____pyrexia
– ______ dysfunction
–_____________ effects

A

Orthostatic/ Postural hypotension

Cardio

Gain

Hyper ; Sexual

Anti-muscarinic

62
Q

ADVERSE EFFECT
MAOI
– ________ ——-tension
– _____toxicity
– Insomnia
–_____ dysfunction
–______— syndrome
– __________ crisis

A

Orthostatic hypo
Hepato

Sexual; Serotonin

Hypertensive

63
Q

Hypertensive crisis can occur when you combine MAOI with _______ containing foods Also called __________ interaction

A

TYRAMINE

WINE-CHEESE

64
Q

ADVERSE EFFECT

Atypical
– Mirtazapine
Increase ________
Weight _____

– Bupropion
Seizure
Weight _____
___________ DYSFUNCTION

A

appetite; gain

loss; NO SEXUAL

65
Q

ADVERSE EFFECT
SARI

–________
–_______
– Orthostatic hypotension
– Nausea

A

Priapism

Sedation

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