Miscellaneous Flashcards
Active metabolites
What is the active metabolite of diazepam
desmethyldiazepam
What is the active metabolite of dothiepin
Dothiepinsulfoxide
What is the active metabolite of fluoxetine
norfluoxetine
What is the active metabolite of imipramine
desipramine
What is the active metabolite of risperidone
9-hydroxyrisperidone
What is the active metabolite of amitriptyline
nortriptyline
What is the active metabolite of codeine
morphine
What are the active metabolite of clozapine
N-desmethylclozapine
Clozapine N-oxide
What is a prodrug?
Drugs that need to be metabolised to become their active form
What is modafinil licensed for?
Excessive sleepiness associated with narcolepsy
What is modafinil used for off license?
OSA
Shift work sleep disorder
Adjunctive treatment for depression
How does modafinil work?
Weak inhibitor of dopamine reuptake
How does agomelatine work?
Antidepressant - agonist at melatonin M1 and M2 receptors and antagonist at 5HT2C receptors
What is a partial agonist?
produces the biological response but cannot produce 100% of the response even at very high doses.
What is a competitive antagonist?
Competitive antagonists bind to the receptor in a reversible way without affecting a biological response. They make the agonist look less potent.
What is an inverse agonist?
Have opposite effects from those of full agonists
What is an agonist antagonist
Some substances can bind to certain receptors and act as an agonist and at other receptors they act as an antagonist.
What drugs have a narrow therapeutic index?
Carbamazepine
Lithium
Phenytoin
Warfarin
Digoxin
Gentamicin
Which psychiatric drugs can interact with oral contraceptives resulting in a reduced contraceptive effect?
St John’s Wort
Carbamazepine
Phenytoin
Topiramate
Barbiturates
What is the most common side effect of sildenafil?
headaches
What area of the body is most commonly affected by tardive dyskinesia?
face
When does tardive dyskinesia worsen?
emotional arousal
Which drugs must be protected from moisture?
sodium valproate
topiramate
Which drug must be protected from sunlight and moisture ?
Zopiclone
Which drug state can produce a biological response?
Drugs unbound in plasma
What APs should be avoided in renal impairment?
Amisulpride
Sulpiride
What is best choice AP in renal impairment ? First and second generation ?
First - haloperidol
Second - olanzapine
which ADs are preferable in renal impairment?
Sertraline
Citalopram
Fluoxetine
Which mood stabilisers are preferred in renal impairment?
Valproate
Lamotrigine
Which anxiolytics are preferred in renal impairment?
Lorazepam
Zopiclone
Which anti-dementia drugs are preferred in renal impairment?
Rivastigmine
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.
Give the calculation for volume of distribution
Amount of drug in the body/concentration in the plasma
Do lipid soluble drugs have a higher or lower volume of distribution? Why?
Higher
Can cross cell membranes more easily and distribute into tissues.
What influences volume of distribution?
the drug’s lipid or water solubility
plasma protein binding
tissue binding.
Which class of drugs are associated with paradoxical reactions?
Benzos
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
What is mechanism of action of flumazenil?
Selective GABA-A antagonist - competitive
What is the half life of flumazenil?
1 hour
What other meds are blocked by flumazenil?
zopiclone
What is range of duration of flumazenil?
20-50 mins
Which AP is most likely to cause priapism and why
Chlorpromazine due to potent alpha-adrenergic blocking properties
What AD is associated with priaprism
trazodone
What are the side effects of histamine H1 blockade?
weight gain
sedation
What are the side effects of alpha 1 blockade
orthostatic hypotension
sedation
sexual dysfunction
priapism
What are the side effects of muscarinic central M1 blockade
agitation
delirium
memory impairment
confusion
seizures
What are the side effects of muscarinic peripheral M1 blockade
dry mouth
ataxia
blurred vision
narrow angle glaucoma
constipation
urinary retention
tachycardia