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Miscellaneous Flashcards

Active metabolites

1
Q

What is the active metabolite of diazepam

A

desmethyldiazepam

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1
Q

What is the active metabolite of dothiepin

A

Dothiepinsulfoxide

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2
Q

What is the active metabolite of fluoxetine

A

norfluoxetine

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3
Q

What is the active metabolite of imipramine

A

desipramine

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4
Q

What is the active metabolite of risperidone

A

9-hydroxyrisperidone

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5
Q

What is the active metabolite of amitriptyline

A

nortriptyline

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6
Q

What is the active metabolite of codeine

A

morphine

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7
Q

What are the active metabolite of clozapine

A

N-desmethylclozapine
Clozapine N-oxide

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8
Q

What is a prodrug?

A

Drugs that need to be metabolised to become their active form

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9
Q

What is modafinil licensed for?

A

Excessive sleepiness associated with narcolepsy

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10
Q

What is modafinil used for off license?

A

OSA
Shift work sleep disorder
Adjunctive treatment for depression

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11
Q

How does modafinil work?

A

Weak inhibitor of dopamine reuptake

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12
Q

How does agomelatine work?

A

Antidepressant - agonist at melatonin M1 and M2 receptors and antagonist at 5HT2C receptors

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13
Q

What is a partial agonist?

A

produces the biological response but cannot produce 100% of the response even at very high doses.

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14
Q

What is a competitive antagonist?

A

Competitive antagonists bind to the receptor in a reversible way without affecting a biological response. They make the agonist look less potent.

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15
Q

What is an inverse agonist?

A

Have opposite effects from those of full agonists

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16
Q

What is an agonist antagonist

A

Some substances can bind to certain receptors and act as an agonist and at other receptors they act as an antagonist.

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17
Q

What drugs have a narrow therapeutic index?

A

Carbamazepine
Lithium
Phenytoin
Warfarin
Digoxin
Gentamicin

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18
Q

Which psychiatric drugs can interact with oral contraceptives resulting in a reduced contraceptive effect?

A

St John’s Wort
Carbamazepine
Phenytoin
Topiramate
Barbiturates

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19
Q

What is the most common side effect of sildenafil?

A

headaches

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20
Q

What area of the body is most commonly affected by tardive dyskinesia?

A

face

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21
Q

When does tardive dyskinesia worsen?

A

emotional arousal

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22
Q

Which drugs must be protected from moisture?

A

sodium valproate
topiramate

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23
Q

Which drug must be protected from sunlight and moisture ?

A

Zopiclone

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24
Which drug state can produce a biological response?
Drugs unbound in plasma
25
What APs should be avoided in renal impairment?
Amisulpride Sulpiride
26
What is best choice AP in renal impairment ? First and second generation ?
First - haloperidol Second - olanzapine
27
which ADs are preferable in renal impairment?
Sertraline Citalopram Fluoxetine
28
Which mood stabilisers are preferred in renal impairment?
Valproate Lamotrigine
29
Which anxiolytics are preferred in renal impairment?
Lorazepam Zopiclone
30
Which anti-dementia drugs are preferred in renal impairment?
Rivastigmine
31
What is volume of distribution?
Indicates how a drug distributes in the body. Tells you if a drug concentrates in the plasma or spreads out.
32
Give the calculation for volume of distribution
Amount of drug in the body/concentration in the plasma
33
Do lipid soluble drugs have a higher or lower volume of distribution? Why?
Higher Can cross cell membranes more easily and distribute into tissues.
34
What influences volume of distribution?
the drug's lipid or water solubility plasma protein binding tissue binding.
35
Which class of drugs are associated with paradoxical reactions?
Benzos
36
What are the increased risk factors for disinhibitory drug reactions?
LD Extremes of age Hx of aggression or poor impulse control Benzo with short half life High dose IV admin
37
What is mechanism of action of flumazenil?
Selective GABA-A antagonist - competitive
38
What is the half life of flumazenil?
1 hour
39
What other meds are blocked by flumazenil?
zopiclone
40
What is range of duration of flumazenil?
20-50 mins
41
Which AP is most likely to cause priapism and why
Chlorpromazine due to potent alpha-adrenergic blocking properties
42
What AD is associated with priaprism
trazodone
43
What are the side effects of histamine H1 blockade?
weight gain sedation
44
What are the side effects of alpha 1 blockade
orthostatic hypotension sedation sexual dysfunction priapism
45
What are the side effects of muscarinic central M1 blockade
agitation delirium memory impairment confusion seizures
46
What are the side effects of muscarinic peripheral M1 blockade
dry mouth ataxia blurred vision narrow angle glaucoma constipation urinary retention tachycardia
47
What happens to plasma volume in pregnancy?
it increases
48
what happens to concentration of plasma albumin in pregnancy?
decreases
49
What happens to volume of distribution for lipophilic drugs in pregnancy?
increases
50
What happens to the total plasma concentrations of albumin-bound drugs in pregnancy?
decreases
51
What happens to progesterone levels in pregnancy? what are the effects>?
increase delayed gastric emptying and reduced small intestine motility overall effects on total bioavailability are small
52
What happens to eGFR in pregnancy? What does this lead to?
increases leads to enhanced elimination of some drugs
53
What is modafinil used for?
enhances wakefulness, attention and vigilance Off licence for OSA, shift work sleep disorder, adjunct in depression
54
What is modafinil licensed for?
narcolepsy
55
What is the MOA of modafinil?>
weak inhibitor of dopamine reuptake no affinity for serotonin or norepinephrine transporters
56
What is the mechanism of action of varenicline?
selective nicotine-receptor partial agonistW
57
What is varenicline used for?
smoking cessation
58
Is varenicline safe to use in hepatic im[pairment?
yes
59
How long is varenicline used for in smoking cessation?
12 weeks with additional 12 weeks for those who have successfully stopped smoking
60
What are the side effects of varenicline?
Nasopharyngitis Abnormal dreams, insomnia Headache Nausea
61
How can varenicline affect mental health?
exacerbate underlying psychiatric illness including depression associated with changes in behaviour, anxiety, psychosis, mood swings, aggressive behaviour, depression, suicidal ideation.
62
In what patients should varenicline be used cautiously?
those with cardiovascular disease
63
which meds can precipitate porphyria?
barbiturates benzos sulpiride certain mood stabilisers
64
What are the symptoms of porphyria?
abdo pain mental state changes constipation vomiting muscle weakness
65
What are the effects of histamine H1 blockade?
weight gain sedation
66
What are the side effects of alpha blockres?
Orthostatic hypotension, sedation, sexual dysfunction, priapism
67
What are side effects of muscarinic central M1 blockade?
agitation delirium memory impairment confusion seizures
68
What are the side effects of muscarinic peripheral M1 blockade?
Dry mouth, ataxia, blurred vision, narrow angle glaucoma, constipation, urinary retention, tachycardia

Clinical pharmacology (27 decks)

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