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CNS > Pharma 6: Antidepressant And Antipsychotic Drugs > Flashcards

Pharma 6: Antidepressant And Antipsychotic Drugs Flashcards

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1
Q

Selective Serotonin Reuptake Inhibitors

A

Fluoxetine Citalopram

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2
Q

Fluoxetine Citalopram Selectivity to serotonin transporter

A

300-3000 greater for serotonin than noradrenaline

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3
Q

Fluoxetine, citalopram Adverse effects

A

Safer than TCAs and MAOI so they’ve replaced them

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4
Q

Fluoxetine, citalopram Therapeutic uses

A

-Very effective in treating “moderate” depression - Less effective than TCAs in treating severe depression -Treats bulimia nervosa, OCD, anorexia nervosa, panic disorder.

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5
Q

Pharmacokinetics of Fluoxetine, Citalopram

A
  • Absorbed orally - Fluoxetin—>potent inhibitor of CYP2D6 (metabolized TCAs, antipsychotics, antiarrythmatics, B antagonists) - If pt has hepatic impairment—> reduce dose of SSRI
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6
Q

Fluoxetine, Citalopram Adverse effect

A

-nausea -anxiety -insomnia -anorexia -weight loss -tremors -sexual dysfunction

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7
Q

Antidepressants and <18 years

A

CAUTION! Possibly causes excitement, insomnia aggression in first few weeks Possibly increased suicidal ideation Lower seizure thresholds

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8
Q

Serotonin syndrome Caused by: S/S:

A

All SSRI can potentially cause this especially when used with MAOI Characterized by: tremor, hyperthermia, CV collapse—>death

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9
Q

Discontinuation syndrome Caused by S/S

A

Potentially caused by SSRI after their abrupt withdrawal ((Fluoxetine—>lowest risk due its longer T1/2 and active metabolite)) S/S: headache, malaise, flu like, agitation, irritability, nervousness, sleep difficulties

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10
Q

Venlafaxine, Duloxetine (SNRI) MOA

A

-Inhibit serotonin and noradrenaline reuptake -Little activity at a-adrenergic, muscuranic, histamine receptor—> less of the side effects resulting from these receeptors

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11
Q

Venlafaxine Pharmacokinetics

A

Minimal inhibition or CYP450 Substrate for CYP2D6

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12
Q

VENLAFAXINE Side effects

A

-Nausea -Headache -Sexual Dysfunction -Disziness -Insomnia -Sedation -Constipation High dose—> HTN, TACHYCARDIA

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13
Q

Duloxetine Metabolism

A

Highly metabolized in liver—> inactive metabolites !Avoid in pt with liver dysfunction

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14
Q

Duloxetine side effects

A

Gi (common); nausea, dry mouth, constipation Others: insomnia, dizziness, somnolence, sweating, sexual dysfunction. May increase bp and hr

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15
Q

Duloxetine drug-drug interaction

A

Moderate inhibitor of CYPD26–> increase conc of drugs (antipsychotics) metabolized by it

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16
Q

Tricyclic antidepressants

A

Imipramine

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17
Q

Imipramine MOA

A

TCA Therapeutic —>Inhibit serotonin and noradrenaline reuptake +block serotonergic, a adrenergic, histaminic, muscarinic receptors—> adverse effects?

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18
Q

Imipramine Therapeutic uses

A

Moderate-severe depression Some anxiety disorders eg anxiety attacks

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19
Q

Imipramine Pharmacokinetics

A

Well absorbed orally Metabolized by hepatic microsomal system—> sensitive to agents that induce/inhibit CYP450?

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20
Q

Imipramine Adverse effects

A

Antimuscarinic: blurred vision, dry mouth, urinary retention and constipation A adrenergic block: Orthostatic hypotension, dizziness, reflex tachy CV: arrhythmia and SD Sedation: in first few weeks of use Weight gain

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21
Q

Imipramine Precautions

A

If bipolar pt—> antidepressants may cause a switch to manic behavior Suicidal pt—> LIMITED QUANTITIES OF TCA cuz low TI there4 lethal imipramine dose is 5-6 maximal dose.

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22
Q

TCA Interaction with MAOI

A

Mutual enhancements—> htn, hyperpyrexia, convulsions, coma

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23
Q

TCA Interaction with direct acting adrenergic drugs

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A

Potentiate effects of biogenic amine drugs by preventing their removal from synaptic cleft

24
Q

TCA Interaction with ethanol and cns depressants

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A

Toxic sedation

25
TCA Interaction with indirect acting adrenergic drugs
Block effects of indirect acting sympathomimetic drugs by preventing the drugs from reaching their intracellular sites or action
26
MAOI
Phenelzine
27
Phenelzine MOA
Inactivate reversibly/irreversibly MAO—\> accumulation of serotonin, NA and dopamine in synaptic cleft
28
Function of MAO
Inactivates monoamines like norepinephrine, serotonin and dopamine from synaptic vesicle
29
Phenelzine Consequences of inhibiting MAO
Inhibits MAO in the liver and gut that catalyze oxidative deamination of drugs and toxic substances like tyramine → increase in concentration of tyramine and other drug-drug or food-drug interactions
30
Phenelzine Therapeutic uses
1. used in patients who are depressed and are unresponsive or allergic to TCA and SSRI or patients with strong anxiety 2. Patients with atypical depression 3. LAST LINE because of risk of drug driug and drug food interractions.
31
Phenelzine Pharmacokinetics
Well abosorbed orally Metabolized in liver Excreted rapidly in urine
32
Phenelzine Adverse effects
* Drowsiness * orthostatic hypotension * blurred vision * dry mouth * dysuria * constipatiopn * tremors * OD→Convulsions
33
Phenelzine when used with other anti-depressants (SSRI) causes
SEROTONIN SYNDROME
34
Significance of tyramine
* found in aged cheese and meats, chicken liver red wine smoked fish etc * inactivated by MAO in gut * tyramine causes release of large quantities of CATECHOLAMINES from stores in nerve terminals→HYPERTENSIVE CRISIS ie. occipital headache, stiff neck, tachycardia, nausea, hypertension, arrhthmias, seizures, stroke??
35
Atypical Antidepressant
MIRTAZAPINE
36
Mirtazapine MOA
* Antagonizes presynaptic a2-adrenoreceptors→ enhances serotonin and noradrenaline NT * May also antagonize 5-HT2 receptors...antidepression * Potent antihistamine effect →sedating useful for depressed pt with difficulty sleeping * NO ANTIMUSCURANIC (vs TCA) * NO SECUAL DYSFUNCTION (vs SSRI) +increase apetie→weight gain
37
Schizophrenia Pathophysiology
possibly dysfunction of the mesolimbic or mesocortical dopaminergic neuronal pathways
38
Dopamine hypothesis of schizophrenia
* ANTIpsychotic properties are explained by post synaptic dopamine antagonism * Drug induced psychosis is a high risk with drugs that incerease dopamine availability like cocaine, amphetamines, L dopa * Potential complication of PD pt on L dopa
39
Limitations of Dopamine Theory
* doesn't explain cognitive deficits * D-lysergic acid, 5-HT2A agonist also produces psychotic symptoms ie not just dopamine
40
First Generation Antipsychotics
Chlorpromazine Thioridazine Haloperidol
41
FGA MOA
* Block D2 dopamine receptors→ lower dopaminergic NTion in the four dopamine pathways→ antipsychotic effects * Competetive antagonist of H1, M1, a1 adrenoreceptors
42
FGA and extrapyramidal symptoms
Particulary HALOPERIDOl→bind tighlty to dopaminergic neuroreceoptors Less likely with CHLORPROMAZINE→bind weakly
43
SGA drugs
Aripiprazole Clozapine Olanzapine
44
Second generation antipsychotics MOA
"atypical antipsychotics" Antagonize dopamine, srotonin and other receptors
45
SGAs and extrapyramidal symptoms
Lower incidence of EPS than FGA→FIRST LINE
46
SGAs are associated with..
Metabolic side effects: * diabetes * hyperchol * weight gain
47
Antipsychotic effects (on positive symptoms)
All antipsychotics can reduce hallucinations and delusions associated with schizophrenia ie they reudce the postive symptoms by blocking D2R in the mesolimbic system !NOTE: Blocking D2R in the nigrostriate pathway—\> EPS—\> dystonias, parkinson like symptoms, akathisia and tardige dyskinesia. Less so in SGA
48
Negative symptoms of schizophrenia are mostly responsive to
SGA eg Clozapine
49
Antiemetic effect of antipsychotics
All antipsychotics have antiemetic effect due to blocking D2R of the chemoreceptor trigger zone !EXCEPT **aripiprazole**
50
Anitcholonergic effects of antipsychotics
**CHLOROPROMAZINE, CLOZAPINE, OLANZAPINE** produce anticholinergic effects like blurred vision, confusioj and inhibiiot of Gi and ut !anticholinergic effect—\> decrease risk of EPS
51
Other effects of antipsychoyics
* Block a adrenergic receptors—\> orthostatic hypotension and lightheadedness * alter temperature regulating mechanisms—\>poikilothermia * block D2R in pituitary—\>hyperprolactin * potent antagonists of H1 histamine receptors **chlorpromazine, olanzapine, clozapine**—\> sedation * some cause sexual dysfunction
52
Statistics on the adverse effects of antipsychotics
Can occur in virtually all patients and can be significant in 80% of cases
53
Adverse effect—\> EPS
Extrapyramidal motor effects ## Footnote due to disturbance in balance between dopaminergic and cholinergic system * HIGH RISK* **haloperidol, fluphenazine**—\> preferentially block D2R * LOW RISK* **THIORIDAZIN**—\> strong anticholinergic activity
54
Adverse effect—\> tardive dyskinesia
* Due to long term treatment * giving up antipsychotics may reduce symptoms * may be permanent
55
Neuroleptic malignant syndrome
* Potentially fatal * reaction to antipsychotics * must discontinue
56
Other adverse effects of antipsychotics
* drowsines * confusion * dry mouth * urinary retention * constipation * loss of visual accomodation * hypotension * orthostatic hypotension * impaired thermoregulation * amennorrhea * galctorrhea * gynecomastia * infertility * ed * weight gain * exacerbate DM hyperlipidemia * QT prologation **thioridazine**
57
Cautions and contraindications of antipsychotics
* lower seizure threshold * elderly pt with dementia related psychosis→ increased risk of mortality * pt ith mood disorders→monitored for worsening of symptoms and suicidal ideation or behaviors

CNS (28 decks)

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