✅Sedative Hypnotic, Neuroleptics, Antidepressants Flashcards by Jerold Justo

Q

Which drugs are considered date rape drugs?

A

Alcohol (most common)
Flunitrazepam (rohypnol)
Gamma-hydroxybutyrate

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Q

Moa of benzodiazepines

A

Gaba A binding to increase freq of chloride channel opening; membrane hyperpolarization

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Q

Usual side effect of benzodiazepines

A

Anterograde amnesia

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Q

Which benzodiazepine has the longest half life?

A

Chlordiazepoxide

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Q

Benzodiazepines and ____ usually cause additive CNS depression

A

Ethanol

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Q

Name the preferred benzodiazepine in the following clinical setting:

Anticonvulsant maintenance

A

Clonazepam

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Q

Name the preferred benzodiazepine in the following clinical setting:

Status epilepticus

A

Lorazepam, diazepam

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Q

Name the preferred benzodiazepine in the following clinical setting:

Skeletal muscle relaxation (cerebral palsy)

A

Diazepam

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Q

Name the preferred benzodiazepine in the following clinical setting:

Panic disorders, phobias

A

Alprazolam, clonazepam

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Q

Name the preferred benzodiazepine in the following clinical setting:

Insomnia

A

Estazolam, flurazepam, triazolam

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Q

Name the preferred benzodiazepine in the following clinical setting:

Anesthesia induction

A

Midazolam, diazepam

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Q

Name the preferred benzodiazepine in the following clinical setting:

Bipolar disorder

A

Clonazepam

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Q

Name the preferred benzodiazepine in the following clinical setting:

Alcohol withdrawal

A

Chlordiazepoxide, diazepam

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Q

Do we use activated charcoal in benzodiazepine poisoning?

A

No. Antidote is flumazenil.

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Q

Toxic dose of benzodiazepine is ____x the therepeutic dose

A

1000x

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Q

MOA of flumazenil

A

Antagonist at benzodiazepine sites on GABA-A receptor

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Q

_____ may occur when flumazenil is administered in a patient who took both TCAs and benzodiazepines

A

Seizures and arrhythmias

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Q

Intermediate acting benzodiazepine

A

Lorazepam

Alprazolam
Clonazepam
Estazolam
Lormetazepam
Nitrazepam
Temazepan

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Q

Long acting benzodiazepine

A

Diazepam

Chlorazepate
Chlordiazepoxise
Flurazepam
Quazepam
Flunitrazepam

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Q

Ultrashort acting barbiturate

A

Thiopental

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Q

Similar drugs as with thiopental

A

Methohexital

Thiamylal

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Q

Moa of barbiturates

A

Bind to GABA A receptor sites (distinct from benzodiazepines); increases duration of chloride channel opening

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Q

Uses of thiopental

A

Anesthesia induction
Increased ICP (dec cerebral blood flow)

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Q

Common side effect of barbiturates

A

Tolerance
Extension of CNS depressant action
Acute intermittent PORPHYRIA

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Short and intermediate acting barbiturate

Pentobarbital

Uses of pentobarbital

Insomia, preoperative sedation

All barbiturates are CYP ____

Inducers

Long acting barbiturate

Phenobarbital Mephobarbital Primidone

Aside from seizure disorders, insomnia, abd status epilepticus, phenobarbital is also used for this disorder. Explain the MOA

Hyperbilirubinemias (Gilbert syndrome) Increase hepatic transport of bile

What enzyme is deficient in acute intermittent porphyria?

HMB synthase (uroporphinogen 1)

What is the most catastrophic symptom of sedative hypnotic withdrawal?

Rebound suicide

What new hypnotic is user mainly for insomnia only

Zolpidem

What drug class is zolpidem in

Imidazopyridine

What is the MOA of zolpidem?

Bind selectively to a subgroup of GABA-a receptors, acting like benzodiazepines to enhance membrane hyperpolarization

What is unique with zolpidem making it specific only for insomnia?

It lacks anti convulsant, anti anxiety and muscle relaxant effects

Effects of zolpidem can be reveresed by?

Flumazenil

Anxiolytic drug used for GAD

Buspirone

Moa of buspirone

Partial agonist at 5Ht1 receptor and possibly D2

What is the notable side effect of buspirone and why is it not popular for usage?

It takes 1 week to take effect SE: nonspecific chest pain, tachycardia, palpitations

Typical antipsychotics are divided into

Phenothiazines Thioxanthenes Butyrophenones Mnemonic: PTB

MOA of classic antipsychotic drugs

Bloackade of brain dopamine receptors especially D2

How many dopamine receptors are there?

D1-5

Dopamine agonist drugs has this effect on schizophrenia

Exacerbation of schiz

The nucleus accumbens is important for

Addiction

All antipsychotics reduce the _____ symptoms of schiz

Positive

Atypical antipsychotics

Heterocyclics ``` Clozapine Loxapine Olanzapine Risperidone Quetuapine Ziprasidone Aripiprazole ```

Ex of phenothiazines (typical antipsychotic)

Chlorpromazine Thioridazine Fluphenazine

Ex of thioxanthenes (typical antipsychotic)

Thiothexene

Haloperidol is an example of a

Butyrophenone (typical antipsychotic)

Atypical antipsychotics are reported to improve some of the ____sx of schiz

Negative

Endocrine toxicity of antipsychotics

Hyperprolactinemia

Dopaminergic tracts in schiz

``` Mesocortical-mesolimbic Nigrostriatal Tuberoinfundibular Medullary-periventricular Incertohypothalamic ```

Dopaminergic tract responsible for anyicipatory motivational phase of copulatory behavior

Incertohypothalamic

Dopaminergic tract responsible for eating behavior

Medullary-periventricular

Treatment for Neuroleptic induced acute dystonia

Diphenhydramine

Treatment for neuroleptic induced parkinsonism and rabbit syndrome

Benztropine

____ commonly occurs with atypical neuroleptics while _____ with typical

Weight gain | Tremors

MOA of atypical antipsychotics

Blockade or 5HT2 receptors more than D2

____ deposits are usually seen as a sidr effect of chlorpromazine while ___ deposits are seen in thioridazine

Corneal and lens Retinal

Only antipsychotic with fatal overdose

Thioridazine

Typical antipsychotic with major extrapyrimadial dysfunction and NMS as side effect.

Haloperidol

Typical antipsychotic with strongest autonomic effect

Thioridazine

Typical antipsychotic with weakest autonomic effect

Haloperidol

Only atypical antipsychotic that reduces the risk of suicide

Clozapine

Main side effect of clozapine

Agranulocytosis

What are the features of neuroleptic malignant syndrome?

Mnemonic: FEVER ``` Fever Encep Vitals unstable Elevated CPK Rigidity ```

Atypical antipsychotic that causes weight gain, hyperglycemia, hyperlipidemia

Olanzapine

Atypical antipsychotic with somnolence, fatigue, sleep paralysis and hypnagogic hallucinations, cataracts and priapism

Quetiapine

Atypical antipsychotic that is best for elderly bec of less sedative effects

Risperidone

Only antipsychotic aprrived for schiz of the youth

Risperidone

SE of risperidone

Hyperprolactinemia | Photosensitivity

Notable SE of ziprasidone

``` Postural hypotension QT prolongation (TDP) ```

Least sedating atypical antipsychotic

Aripiprazole

One stop drug - typical antipsychotic called haloperidol. Aside from schiz, what diseases can it be used for?

Huntingtons Parkinsons Acute psychotic episodr

Monotherapy with antidepressants in bipolar can precipitate ______

Manic episode

Lithium is a teratogen because it causes

Ebstein's anomaly

Lithium is contraindicated in

Sick sinus syndrome

Overdose with lithium is treated by

Hemodalysis

Treshold for lithium toxicity is

2 meq/L

What is the main hypothesis for mood that is used as basis to treat depression?

Amine hypothesis NE and serotonin are neurotransmitters that function in the pathway of mood

Major classifications of antidepressants

``` TCAs SSRI SNRI Serotonin receptor antagonist Heterocyclic antidepressants ```

Ex of TCAs

Imipramine, amitryptiline

Ex of SSRIs

Fluoxetine, escitalopram, paroxetine, sertraline

Ex of SNRIs

Duloxetine, venlafaxine

Ex of MAOIs

Phenelzine Selegiline Tranylcypromine

MOA of imipramine

Blocks NE and serotonin transporters

Imipramine is used in MDD and what other pertinent indication?

Enuresis especially in children

Notable in TCA overdose

Abnormal QRS complexes morphology Prolonged QRS duration Abnormal size and ratio of R and S waves in AVR

What are the features of TCA overdose?

3 Cs of TCA overdose Coma Convulsions Cardiotoxicity

Treatment of TCA overdose

Supportive measures accdg to symptoms | Administration of bicarbonate (reverses cardiotoxicity)

First line in the treatment of MDD

``` Fluoxetine Paroxetine Escitalopram Sertraline Fluvoxamine ```

SNRI with QT prolongation

Citalopram

Fluoxetine when used with maois can precipitate

Seritonin syndrome

What are the drugs that cause erectile dysfunction?

A SORE PEnis cant Fuck Hard ``` SSRIs Opiates Risperidone Ethanol Propanolol Estrogens Spirinolactone Finasteride HCTZ ```

Which SNRI can cause hypertension?

Venlafaxine

Which SNRI can cause hepatotoxicity?

Duloxetine

Which serotonin receptor antagonist can cause priapism and which caused hepatotoxicity?

Trazodone | Nefazodone

What drugs can cause priapism?

``` Trazodone Papaverine Sildenafil Quetiapine Alprostadil Warfarin Bupropion ```

What are the features of serotonin syndrome?

FAT CHD ``` Fever Agitation Tremor Clonus Hyperreflexia Diaphoresis ```