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CNS > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

uses of anti psychotics

A

anti emetic drugs - blocks D/S in CTZ

psychosis - block at mesocortical/mesolimbic

chorea, tics/tourette- block D/S in basal ganglia

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2
Q

typical/ 1st gen/ neuroleptic AP

A

block dopamine/D2 receptor more

effect: controls positive symptoms only (schizophrenia)
hallucination
delusion
aggression/violence

SE: Parkinson’s/EPS
hyperprolactinemia

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3
Q

atypical / 2nd gen AP

A

block serotonin/ 5HT2A receptor more

controls positive + negative symptoms
apathy
amnesia
anhedonia
depression

SE: blocks 5HT: increased appetite - obesity, diabetes, dyslipidemia (metabolic syndrome)
safer than 1st gen

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4
Q

Treatment of psychosis

A

atypical AP
Apipirazole, Ziprasidone, Quetiapine

4 weeks- no response

change to another atypical

4 weeks no response

change to typical AP

4 weeks no response

resistant psychosis: DOC- Clozapine

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5
Q

1st gen AP

A

Phenothiazine (least potent D2 blocker/least effect/ least risk EPS)
Chlorpromazine
Thioridazine
Mesoridazine
Fluphenazine
Perphenazine
Prochlorperazine

Thioxanthenes
Thiothexene
Flupenthixol
Zuclopenthixol

Butyrophenone (most potent D2 blocker / max risk of EPS/ most effective)
Haloperidol
Droperidol
Benperidol
Penfluridol

Miscellaneous
Loxapine
Molindone
Pimozide

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6
Q

least potent 1st gen AP

A

Chlorpromazine>Thioridazine

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7
Q

most potent 1st gen AP

A

Benperidol>Haloperidol

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8
Q

Longest 1st gen AP

A

Penfluridol (once a moth)

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9
Q

1st gen AP used an antiemetic

A

Prochlorperazine (in migraine and violent vomit)

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10
Q

Which 1st gen AP was banned

A

Thioridazine (retinal degeneration)

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11
Q

Droperidol+ fentanyl

A

Neurolept analgesia

Add N2O - neurolept anaesthesia

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12
Q

Chlorpromazine

A

least potent D2 blocker - AP

also blocks histamine - sedation (treatment of pruritic-allergy)

blocks Ach (like atropine - mydriase) : CI in glaucoma

blocks alpha receptor - VD - decreased Bp

Additional use - amphetamine poisoning (psychosis + HTN)

SE: cholestatic jaundice, blue grey skin, cornea verticalkata (by Amiodarone also)

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13
Q

atypical/2nd gen AP

A

5HT2A ANTAGONIST>D2 ANTAGONIST
Clozapine
Olanzapine
Zotepine
Asenapine
Quetiapine
Ziprasidone
Risperidone
Ilaperidone
Sertindole
Paliperdone (pro drug: active form : Risperidone)
Lurasidone

max D2 blockage- risperidone
least D2 blockage - Clozapine

D1/2 PARTIAL AGONIST + 5HT2A ANTAGONIST
Apipiprazole
Brexipiprazole
caripraszine(new)

D2+D3 ANTAGONIST
Sulpiride
Levosulpiride
Amisulpiride

5HT2A INVERSE AGONIST
Pimavanserin

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14
Q

AP which does not act on D2 receptors

A

Pimavanserin (pyschosis in Parkinsons patient)

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15
Q

overall least risk of EPS

A

Pimavanserin>Clozapine

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16
Q

Least risk EPS among typical AP

A

Chlorpromazine>Thioridazine

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17
Q

Max risk Eps among atypical Ap

A

Risperidone

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18
Q

AP in schizophrenia/pyschosis

A

All AP

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19
Q

AP in bipolar disorders

A

Atypical AP
Quetiapine
Clozapine

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20
Q

AP for acute mania

A

inj: all AP

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21
Q

APs for unipolar depression

A

DOC: SSRI

APs used:
Quetiapine
Aripiprazole
Brexipiprazole
Amisulpiride

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22
Q

Risperidone

A

Approved for schizophrenia, autism, BPD
Off label for OCD

23
Q

AP approved for autism

A

Risperidone

24
Q

Drug approved for schizoaffective disorder

A

Paliderdone

25
Q

Rout of administration of AP

A

Oral: all drugs (if compliant)
otherwise, once a month, intramuscular depot injection (Z technique)
Haloperidol
Fluphenazine
Zuclopenthixol
Perphenazine
Paliperdone
Aripiprazole
Risperidone
Olanzapine

intranasal- Loxapine

Sublingual - Asenapine (bypass FPM of liver and ensure high bioavailability)

26
Q

Adverse effects of D2 blockage

A

Blockage of D2 at pituitary - galactorrhea, amenorrhea, infertility

EPS - blockage of D2 at basal ganglia

Overall max- Haloperidol (typical)
Max among atypical - Risperidone

Least risk - Pimavanserin> Clozapine > Aripiprazole

27
Q

EPS symptoms

A

Neurolept malignant syndrome (Emergency)
Acute muscle dystonia (1st EPS)
Parkinson
Akathisia
Rabbit syndrome
Tardive dyskinesia (after many years

Never APART

28
Q

Acute muscle dystonia

A

sudden spasm of group muscles
torticollis
uprolling of eyes (oculogyric crisis)

inj anticholinergics- Promethazine, Diphenhydramine

29
Q

Parkinsonism

A

Bradykinesia
Resting tremor
Abnormal gait

Oral antiCH - Benzhexol, Promethazine

30
Q

Akathisia

A

most common EPS

Restlessness, inability to sit (increased anxiety)
aggravated by smoking

anti anxiety - DOC: Propranolol - if asthma/muscle spasm - Benzhexol

31
Q

tardive dyskinesia

A

months/years
last EPS
permanent EPS

abnormal excessive movement - choreoathetosis, lip smacking/pouting

super sensitivity of dopamine receptors

no role of antCh
stop antipsychotics- shift to Clozapine - if no response, use dopamine depletion - Tetrabenazine, Valbenazine

32
Q

AP with max wt gain/metabolic syndrome

A

Olanzapine (due to blockage of 5HT2C receptor)

33
Q

AP with least wt gain

A

Aripiprazole
Ziprasidone

34
Q

Ap with weight loss

A

Molindone

35
Q

AP which increase stroke risk

A

Risperidone

36
Q

Ap with risk of cataract

A

Clozapine>Quetiapine

37
Q

AP with risk of QT prolongation

A

Sertindole, Ziprasidone, Quetiapine

38
Q

APs with max and min placental crossing in pregnancy

A

Max - Olanzapine
Min- Quetiapine (safest)

39
Q

Mood stabilisers for BPD

A

Low VOLTAGE

Lithium
Valproate (Divalproex)
Oxcarbazepine / Carbamazepine
Lamotrigine
Topiramate
AP
Gabapentin

Off label - Topiramate, Oxcarbazepine

40
Q

Acute mania

A

Violent/aggressive, talkative , confused

inj Li, AP (started 1st), valproate - if resistant mania, Clozapine iv

41
Q

Maintenance of BPD

A

DOC - oral Li
if more than 4 attacks BPD/year
rapid cycling BPD - DOC: valproate
resistant mania - Clozapine

42
Q

BPD in pregnancy

A

safest - AP
most teratogenic - Valproate

43
Q

Cannot be given in emergency/ICU patients

A

Lithium

44
Q

only in BPD2

A

Lamotrigine

High dose in BPD1(mania) - increased risk of Steven Johnson syndrome/rashes

45
Q

Lithium uses

A

Bipolar disorder
Hypnic headache
Antisuicidal drug
Resistant depression

46
Q

Lithium MOA

A

increases amine/BDNF - inhibits GSK 3 end
decreases amine/BDNF - inhibits inositol monophosphate, inhibits adenylyl cyclase

LiCO3/ LI citrate used for BPD

47
Q

PK of Li

A

route - oral, iv
half life - 1 day
TDM - blood sample for Li is taken 12 hrs after the night dose
No metabolism
excreted unchanged in urine> sweat, saliva, tears, milk
CI: during breastfeeding/lactation
Li stopped >24hrs before surgery

48
Q

Serum levels of Li

A

in mEq/L

0.6-1.0 : used as maintenance of BPD
1.0-1.5 : used for acute mania
>1.5 : Li toxicity starts
>2 : hospitalise the patient
>4 : hemodialysis

49
Q

Adverse effects of Li

A

Leucocytosis - treatment of Felty syndrome
Increase weight/obesity
Tremors - normal doses: fine tremors, toxic doses: coarse tremors
Hypothyroidism goitre - Li inhibits T3/T4 synthesis so increased TSH enlarged thyroid
Increased diarrhoea/ nausea/vomiting (most common side effect)
Urination - Li blocks ADH receptor on kidney (Nephropgenic DI)
Mental - seizures, ataxia, tinnitus
Skin - acneiform eruptions

50
Q

Management of Li toxicity

A

Plenty of saline (NaCl) - increased excretion of Li in urine
Add - mannitol (osmotic diuretics)
if nephrogenic DI- add Amiloride

51
Q

Drug interactions with Li

A

Spironolactone
Tetracycline
ACE inhibitors
NSAID
Diuretics (Thiazide)

Succinylcholine choline - Li increases risk of muscle paralysis
Sulfonylureas - Li increases risk of hypoglycaemia

52
Q

Teratogenicity of Li

A

less compared to Valproate

Ebstein anomaly (cardiac anomaly) - abnormal tricuspid valve, enlarged right atrium, atrial septal defect
Floppy infant (muscle paralysis)
Goitre (hypothyroid)

53
Q
A

CNS (5 decks)

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