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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
Rout of administration of AP
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
Adverse effects of D2 blockage
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
EPS symptoms
Neurolept malignant syndrome (Emergency) Acute muscle dystonia (1st EPS) Parkinson Akathisia Rabbit syndrome Tardive dyskinesia (after many years Never APART
28
Acute muscle dystonia
sudden spasm of group muscles torticollis uprolling of eyes (oculogyric crisis) inj anticholinergics- Promethazine, Diphenhydramine
29
Parkinsonism
Bradykinesia Resting tremor Abnormal gait Oral antiCH - Benzhexol, Promethazine
30
Akathisia
most common EPS Restlessness, inability to sit (increased anxiety) aggravated by smoking anti anxiety - DOC: Propranolol - if asthma/muscle spasm - Benzhexol
31
tardive dyskinesia
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
AP with max wt gain/metabolic syndrome
Olanzapine (due to blockage of 5HT2C receptor)
33
AP with least wt gain
Aripiprazole Ziprasidone
34
Ap with weight loss
Molindone
35
AP which increase stroke risk
Risperidone
36
Ap with risk of cataract
Clozapine>Quetiapine
37
AP with risk of QT prolongation
Sertindole, Ziprasidone, Quetiapine
38
APs with max and min placental crossing in pregnancy
Max - Olanzapine Min- Quetiapine (safest)
39
Mood stabilisers for BPD
Low VOLTAGE Lithium Valproate (Divalproex) Oxcarbazepine / Carbamazepine Lamotrigine Topiramate AP Gabapentin Off label - Topiramate, Oxcarbazepine
40
Acute mania
Violent/aggressive, talkative , confused inj Li, AP (started 1st), valproate - if resistant mania, Clozapine iv
41
Maintenance of BPD
DOC - oral Li if more than 4 attacks BPD/year rapid cycling BPD - DOC: valproate resistant mania - Clozapine
42
BPD in pregnancy
safest - AP most teratogenic - Valproate
43
Cannot be given in emergency/ICU patients
Lithium
44
only in BPD2
Lamotrigine High dose in BPD1(mania) - increased risk of Steven Johnson syndrome/rashes
45
Lithium uses
Bipolar disorder Hypnic headache Antisuicidal drug Resistant depression
46
Lithium MOA
increases amine/BDNF - inhibits GSK 3 end decreases amine/BDNF - inhibits inositol monophosphate, inhibits adenylyl cyclase LiCO3/ LI citrate used for BPD
47
PK of Li
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
Serum levels of Li
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
Adverse effects of Li
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
Management of Li toxicity
Plenty of saline (NaCl) - increased excretion of Li in urine Add - mannitol (osmotic diuretics) if nephrogenic DI- add Amiloride
51
Drug interactions with Li
Spironolactone Tetracycline ACE inhibitors NSAID Diuretics (Thiazide) Succinylcholine choline - Li increases risk of muscle paralysis Sulfonylureas - Li increases risk of hypoglycaemia
52
Teratogenicity of Li
less compared to Valproate Ebstein anomaly (cardiac anomaly) - abnormal tricuspid valve, enlarged right atrium, atrial septal defect Floppy infant (muscle paralysis) Goitre (hypothyroid)
53

CNS (5 decks)

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