Central Nervous System Drugs Flashcards
Drug, indication, class, side effects
Klasifikasi kelas serta cara kerja Diazepam, lorazepam, midazolam
kelas : Benzodiazepin
cara kerja: Agonis receptor GABA (menenangkan)
6 Indikasi diazepam, lorazepam, midazolam
Phobia
anti-anxiety (pre-anesthesia)
insomnia
Muscle spasm
Epilepsi
Sedatif
Apa 2 efek samping dari diazepam, lorazepam, dan midazolam?
ketergantungan dan CNS depression (dose dependent)
ketergantungan kelas benzodiazepin (cth: diazepam,, lorazepam, midazolam) dapat diatasi dengan?
Flumazenil
Kelas terratogen benzodiazepin
D atau X
M & E diazepam, lorazepam, midazolam
M : @ liver become glucoronide
E: @ kidneys
If a patient is tolerant against diazepam (benzodiazepines), drug should be discontinued immediately. T/F?
F. Discontinue gradually.
3 indications for barbiturates
Antianxiety
Anesthesia
Anti-convulsion
common anti-seizure barbiturate
phenobarbital
common short acting barbiturate (induce anesthesia)
sodium thiopental
3 withdrawal symptom of phenobarbital dependent patient
cerebral seizure
psychosis
rem-rebound with nightmare
5 phenobarbital and sodium thiopental side effect
Dose-dependent anterograde amnesia (short term memory loss)
enzyme induction
sleep phase changes
CNS depression
severe withdrawal side effects
4 general withdrawal symptom of phenobarbital and sodium thiopental
tremor
weakness
hypersensitivity
fear
4 drug classes indicated for insomnia, from safest to most risky
- melatonin receptor agonist
low abuse, no rebound insomnia, no significant withdrawal symptom, no dependence, not teratogenic - newer hypnotics
less potential for withdrawal and dependence, teratogen C (human risk cannot be ruled out) - trichloethanol forming structures
no impact on sleep cycle but fast tolerance - Benzodiazepine
dependence, tolerance, teratogen D or X (evidence of risk to human fetus or contraindicated in pregnancy)
Diazepam, lorazepam, midazolam can be used for anesthesia. T/F?
F. Benzodiazepines does not exhibit anesthetic effect even at high doses
2 drugs indicated for insomnia in the class of new hypnotics
zolpidem
zopiclone
drug for insomnia in the class of melatonin receptor agonist
ramelteon
ramelteon A&M
A : rapid oral absorption
M : first pass metabolism result in active metabolite with longer half life
Drug for insomnia that forms trichloethanol
chloral hydrate
4 chloral hydrate side effects
confusion
hepatotoxicity
allergy
nausea
disadvantage of chloral hydrate as insomnia drug, aside from its side effects
fast tolerance
Drug classes indicated to treat anxiety
- Benzodiazepine (enhance GABA)
- Barbiturates (enhance GABA)
- 5-HT receptor agonist
Drug indicated for chronic anxiety that works by enhancing 5-HT receptor
buspirone
Buspirone is an anxiolytic with no sedation. T/F?
T
1 disadvantage of buspirone as an anxiolytic compared to benzodiazepine and barbiturates
needs 1 week to become effective
3 advantages of buspirone (5-ht receptor agonist) compared to barbiturate and benzodiazepine as anxiolytics
no memory loss (vs barbiturate)
no withdrawal symptom (vs barbiturate and benzodiazepine)
no impact on motor skills (vs barbiturate)
4 advantages of Ramelteon (melatonin receptor agonist) as anti insomnia vs zolpidem and diazepam
low potential for abuse
no rebound insomnia (diazepam>zolpidem)
no significant withdrawal symptom (diazepam)
no dependence (diazepam > zolpidem)
Teratogenicity category of zolpidem and zopiclone (new hypnotics)
C
1 advantage of chloral hydrate vs diazepam and zolpidem for insomnia
no impact on sleep cycle
General drug interaction of hypnotics-sedative drugs
additive effect with other CNS-depressant drugs
3 antiepileptic that work as GABA receptor agonist
benzodiazepine
barbiturate
vigabatrin
phenytoin, carbamazepine indication and MOA
antiepileptic, enhance Na+ channel inhibition, therefore delaying action potential
Gabapentin, valproic acid, ethosuximide, pregabalin indication and MOA
antiepileptic, inhibit Ca+, therefore inhibit action potential
Felbamate and rufinamide indication and MOA
antiepileptic, inhibit glutamate receptor, an excitatory neurotransmitter
2 general side effects of antiepileptic
enzyme induction
CNS side effects
general side effect of gabapentin, valproic acid, ethosuximide, phenytoin, felbamate, and vigabatrin
enzyme induction
CNS side effects
Antiepileptic indicated for partial seizures and MOA
gabapentin, inhibit Ca+
the antiepileptic valproic acid is contraindicated in pregnancy (especially during first trimester) because?
it causes fetal malformation (birth defects)
hormonal birth control might not work if taken with phenobarbital. T/F?
T
According to EMA (European medicines agency), valproic acid can be used to treat epilepsy in pregnant women under what conditions?
form of epilepsy is unresponsive to other anti-epileptic drugs
Which anticonvulsant is also used to treat neuropathy (nerve pain) in diabetic patients? which class is it?
Gabapentin, Ca+ channel inhibitor
One function of benzodiazepine is an anxiolytic. Does it has antipsychotic effect?
no, but it does have neurotic effects that help reduce phobias.
Haloperidol and chlorpromazine indication?
Schizophrenia
Haloperidol and chlorpromazine classification and MOA
Typical antipsychotic, block D2 receptor
Risperidone, clozapine, and ziprasidone classification and MOA
atypical antipsychotic, block D2 and other receptors
difference in disadvantages of haloperidol and chlorpromazine compared to risperidone, clozapine, and ziprasidone
Haloperidol and chlorpromazine (typical) : higher risk for movement disorder
risperidone, clozapine, ziprasidone (atypical) : higher risk of metabolic side effect
Major tranquilizers are neuroleptics (depress nerve functions). What is neurolepsis?
Psychomotor slowing
emotional quieting
affective indifference
haloperidol and chlorpromazine could have parkinsons syndrome side effects (involuntary actions). T/F?
T
Side effect of chlorpromazine, haloperidol, risperidone, and clozapine?
Hormonal disorder
Allergy
Vegetative disorder
Epileptic seizure
Hypothermia
Depression
Photosensitization
Impotence
Loss of concentration
Jaundice
