CNS Pharmacology Flashcards
(302 cards)
1
Q
Define seizures
A
Focal,periodic ,unpredictable and paroxysmal episodes of rapid firing of neurons in the brain which causes changes in :
Behavioral, sensory and motor changes.
2
Q
2 types of seizures
A
Generalized seizures:
1. GTCS
2. Absence seizures
3. Atonic seizures
4. Myoclonic seizures
5. Infantile spasm
Partial seizures:
1. Simple seizures
2. Complex seizures
3. Simple and complex seizures.
3
Q
MOA of antiepileptic drugs with egs (4)
A
- Prolongation of Na+ channel inactivation
Phenytoin, Carbamazepine, Topiramate,
Valproate, Lamotrigine, Lancosamide, Zonisamide. - Facilitation of GABA mediated chloride channels :
Barbiturates, BZP, Valproate, Vigabatrin, Gabapentin, Tiagabine. - Decrease in excitatory glutamate channels :
Felbamate - Inhibition of T type calcium channels:
Ethosuximide
Valproate
Zonisamide.
4
Q
Seizures are due to …..
A
Decrease in inhibitory GABA channels
Increase in excitatory glutamate channels
5
Q
How is GABA formed ?
A
Glutaminic acid ————>GABA——metab
GABA decarboxylase. GAT
GAT: GABA trans carboxylase:
GABA———> metabolites
GAT-1: reuptake of GABA to presynaptic neurons.
6
Q
MOA of Na+ channel inactivation
A
Normally: Na channel resting stage (closed)—> activated stage (open )—-> inactivated stage ( open)—-> resting stage (closed).
Antiepileptics prolong the activity of these channels; keeping them open in inactivated state. Thus decreasing the rate of recovery of sodium channels.
7
Q
MOA of barbiturates and BZP.
A
Natural GABA: opens the beta subunit of Cl- channels.
Barbiturates: open Ab subunit of cl- channels:
Facilitating GABA to increase duration of cl-channel opening.
GABA mimetic action. Opens the cl-channel by itself.
BZP: acts on ag subunit.
Facilitating the frequency of opening of GABA channels.
8
Q
MOA of valproate and Vigabatrin
A
They inhibit GABA transaminase responsible for degradation of GABA into matabolites.
9
Q
MOA of tiagabine
A
They inhibit GAT-1 channels responsible for reuptake of GABA.
10
Q
MOA of Felbamate
A
Inhibit glutamate NMDA receptors—> decreasing action of glutamate.
11
Q
MOA of ethosuximide
A
Inhibit the low threshold of T type calcium channels—> decreased calcium entry—> decreased firing—>decreased seizures.
12
Q
MOA of valproate (3)
A
- Prolongation of Na channel inactivation
- Facilitate GABA opening of Cl- channels
- Reduce the low threshold of T type calcium channels.
13
Q
MOA of leviracetam
A
Selective binding to synaptic vesicle protein 2A (SV2A).
14
Q
Therapeutic range of carbamazepine
A
4-12 microgm/ml
15
Q
Dose related side effects of carbamazepine (5)
A
- GIT disturbances
- Double/blurred vision
- Vertigo
- Hematological disturbances
- Task performance impairment.
16
Q
Idiosyncratic side effects of carbamazepine (6)
A
- Agranulocytosis
- SJS: (a/w HLA B1502)
- Aplastic anemia
- Hepatic failure
- Rash
- Pancreatitis.
17
Q
Phenytoin is also called ….
Therapeutic range
A
Diphenylhydantoin
10-20 microgm/ml
18
Q
Phenytoin follows ……kinetics
Route of phenytoin administration
………counteracts the action of phenytoin
A
Zero order Kinetics.
IM route.
Folic acid .
19
Q
Side effects of phenytoin
A
PHENYTOIN
P-cyt P450 inhibition
Hirsuitism
Enlarged gums
Nystagmus
Teratogenic-fetal hydantoin syndrome
Osteomalacia
Interference with B12 metabolism(anemia
Neuropathies: vertigo, rash, headache.
20
Q
Side effects of lamotrigine (3)
A
SJS
Lymphohistiocytosis
Visual disturbance.
21
Q
Zonisamide should not be used if you have ……allergy
Side effects of zonisamide (2)
A
Sulfonamide
Renal stones, hypohydrosis
22
Q
Antiepileptic with PR prolongation
A
Lacosamide
23
Q
Side effects of ethosuximide (2)
A
SJS
BMS
24
Q
- GABA receptor agonists
- GABA reuptake inhibitor
- GABA transaminase inhibitor
A
- Phenobarbitone, BZP
- Tiagabine
- Vigabatrin
25
Therapeutic range of phenobarbital
10-40 microgm/ml
26
Side effects of phenobarbitone (7)
1. Sedation
2. Tolerance
3. Dependence
4. Rebound seizures
5. Learning difficulty
6. Hyperactivity
7. Folic acid supplementation- phenytoin increases the metabolism of folic acid as it’s an enzyme inducer.
27
2 drugs c/I in sulfonamide allergy
Zonisamide
Tiagabine
28
Side effects of Tiagabine (4)
Speech and language problems
Renal calculi
Abdominal pain
Psychosis
29
Side effects of vigabatrin (2)
Peripheral visual field loss
SJS
30
Antiepileptics causing SJS (4)
1. Carbamazepine -when ass with HLAB1502
2. Phenytoin
3. Lamotrigine
4. Vigabatrin
31
Speech and language problem is with …..antiepileptic
Word finding difficulty is with ….
Tiagabine
Topiramate
32
Therapeutic range of valproate
50-135 microgm/ml
33
Side effects of valproate (7)
1. Hepatotoxicity
2. Transient alopecia
3. Weight gain
4. Hyperammonemia
5. PCOD
6. Thrombocytopenia
7. Spina bifida
34
Side effects of topiramate (5)
1. Weight loss
2. Word finding difficulty
3. Hypohydrosis
4. Kidney stones
5. Acute angle closure glaucoma
35
Drug reserved for refractory seizures. Importance of the drug
Felbamate
Written consent is needed to transfuse the drug as it causes aplastic anemia .
36
Antiepileptic that causes homicidal ideation.
Perampanel- NMDA receptor antagonist
37
Antiepileptic causing QT prolongation
Other side effects (3)
Retigabine
1. Retina abnormalities
2. Skin discoloration
3. Urinary retention
38
Side effects of leviracetam (3)
Anemia
Leukopenia
Neuropsychiatric symptoms
39
Drug that causes QT interval shortening
Rufinamide
40
MOA of Rufinamide (2)
Inhibits voltage dependent sodium channels
Inhibits mGluR5
41
Lacosamide inhibits ……other than na channels
CMRP-2
42
Side effect of trimethadione
Day blindness due to excessive glare and photophobia - hemeralopia
43
Endogenous anti seizure substance that prevents seizure is ….
Adenosine
44
Rx for partial complex seizures
Vagal nerve stimulation (VNS)
45
DOC for infantile spasm
ACTH
But when with tuberous sclerosis - vigabatrin is DOC
46
DOC for juvenile myoclonic epilepsy
DOC for absence seizures
Valproate
Ethosuximide, valproate
47
DOC for neonatal seizures
Phenobarbitone
48
DOC for post herpetic neuralgia
Gabapentin
49
Antiepileptic Drugs used for migraine prophylaxis (2)
Topiramate
Valproate
50
Drug for lennox gestaut syndrome
Topiramate
51
Seizure of eclampsia DOC
Isoniazid induced seizure
MgSO4
Pyridoxine
52
DOC for partial seizure (3)
Carbamazepine
Valproate
Phenytoin
53
DOC for tonic clonic seizure
Carbamazepine
Phenytoin
Valproic acid
54
Iv for status epileptics
Iv BZP: lorazepam + iv AED: phenytoin/valproate/leveracetam
55
Symptoms of Parkinson’s disease. Why does it occur?
Tremor, rigidity,bradykinesia
Occurs due to destruction of dopaminergic neurons in the brain and an unopposed action of Ach.
56
Why does parkinsons happen only in old age?
Coz as we age, the glutathione gets depleted, which was initially responsible for scavenging the free radicals from ferrous oxide metabolism in the basal ganglia.
57
Drugs given for parkinsons disease (6)
1. Levodopa, carbidopa
2. Da agonists: Non ergots: ropirinole,pramipexole
3. Amantadine
4. COMT inhibitors: tolcapone,entecapone
5. MAOI : selegilline, rasagilline
Anticholinergics: benztropine,trihexyphenidyl
58
DOC for restless leg syndrome
Ropinirole, pramipexole
59
Anti parkinsons drug preferred in age <65yrs old?
Ropirinole, pramipexole ,piribedil
60
Adverse effects of da agonists (3)
1. N/v- act on CTZ
2. Postural hypotension-Da action on bv
3. CNS:
a)increased sleepiness,
b)hallucinations,
c)impulse control disorder (gambling) ,
d) confusion.
61
Eg of ergot da agonist (2)
Bromocriptine, pergolide
62
MOA of amantadine
Indications (3)
Dopamine facilitator
Increase synthesis, release and reuptake of dopamine.
1. Effective against rigidity and bradykinesia
2. Acute exacerbations
3. Reduce levodopa induced dyskinesias
63
Adverse effects of amantadine (3)
Ankle edema
Livedo reticularis
Ataxia
64
Action of levodopa
Levodopa—————->dopamine
DDC
65
Disadvantages of peripheral conversion of dopamine (3)
1. N/v - due to CTZ
2. Postural hypotension-action on bv
3. Heart- arrythmias
66
Late adverse effects of peripheral dopamine (4)
1. Abnormal movements
2. Nightmares
3. End of dose deterioration
4. On-off effect
67
One thing to keep in mind while giving levodopa is ….
Avoid taking multivitamins with it!
Pyridoxine is a cofactor of DDC, enhances conversion of levodopa to dopamine in the bv and reduces the activity of levodopa.
68
What is given along with levodopa?
Carbidopa, benserazide
Peripheral dopa decarboxylase inhibitors
Decrease the peripheral conversion of levodopa to dopamine; so that more levodopa is available in the brain.
69
MOA of COMT inhibitors
Eg of peripherally acting and central acting
Which is preferred and why?
Inhibiting Conversion of levodopa to 3-O Methyldopa by inhibiting COMT.
Peripherally acting: entacapone
Both peripheral and central: tolcapone
Entacapone is preferred as tolcapone is hepatotoxic.
70
Another drug used as monotherapy early in PD is …..
Use.
Selegilline, rasagilline.
Delay the need to start levodopa
71
S/e of MAOB inhibitors
At high doses they inhibit MAOA as well.
Increase in NE/epi- HTN crisis
Increase in 5HT- serotonin syndrome
72
Drug that can only improve tremor but not bradykinesia is….
They are effective in ……
Anticholinergics- trihexylphenydyl, benztropine
Phenothiazine induced PD
73
S/e of anticholinergic drugs (7)
1. Delirium
2. Mydriasis
3. Increased body temp
4. Increased HR,BP
5. Constipation
6. Urinary retention
7. Dry eyes, dry mouth
74
2 drugs used in “off” episodes when levodopa stops working
Safinamide (MAOB inhibitor)
Istradefylline (adenosine receptor antagonist)
75
Drug used to rx hallucination and delusions associated with PD
Pimavanserin- 5HT2A inverse agonist
76
What is deep brain stimulation ?
High frequency stimulation of subthalamic nuclei -mc site
Or globus pallidus internus.
77
A 75 yr old with Parkinson’s disease no longer responding to anticholinergic Rx for tremor and bradykinesia. What combination is the appropriate plan?
Levodopa
Carbidopa
Entacapone
78
Peripheral side effects of arrythmias, postural hypotension, nausea and vomiting of levodopa can be reduced by …..drug?
Carbidopa
79
Anti parkinsons drug that causes vasospasm
Other side effects
Bromocriptine
Other side effects:
1. Fibrosis of heart,lung
2. Retroperitoneal fibrosis
80
What are the natural opioids ?
Morphine
Codeine
“Morning coffee”
81
What are the semisynthetic opioids?
H2O2 + Buprenorphine + Heroin
Hydroxymorphone
Hydrocodone
Oxycodeine
Oxymorphone
82
What are the synthetic opioids ?
Mirinda
Fanta
Thumbs up
Pepsi
Meperidine
Methadine
Fentanyl
Tapendol
Tramadol
Pentazocine
83
What is Pethidine?
Pethidine =meperidine= synthetic opioid
84
What are the opioid receptors ?
Mu: MUSCAR
Miosis
Euphoria
Sedation
Constipation
Analgesia
Respiratory depression
K:kappa
Dysphoria, hallucinations
Delta
85
Analgesia,euphoria,constipation are ….receptors while physical dependence is …..
M2
M1
86
Opioid antagonists at all 3 opioid receptors
Naloxone
Naltrexone
Mu>k>d
87
Distribution of mu receptor (4)
1. Periductal grey
2. Nucleus solitaris
3. Area postrema
4. Dorsal horn
88
Distribution of kappa receptors (6)
1. Cerebral cortex
2. Striatum
3. Midbrain
4. Hippocampus
5. Dorsal horn
6. Medulla
89
Distribution of delta receptors (8)
1. Cerebral cortex
2. Striatum
3. Midbrain
4. Hippocampus
5. Dorsal horn
6. Medulla
7. Trigeminal nucleus
8. Myenteric plexus
90
Distribution of NOP receptors (4)
1. Hippocampus
2. Cerebral cortex
3. Sensory neuron
4. Descending pain control circuit
91
What are the agonist at mu receptor? (3)
Methadone
Endorphin
Endomorphine 1&2
92
What is the agonist at kappa receptor ?
Dynorphin A
93
What is the receptor at delta receptor?
Enkephalin
{ K-D : EnKephalin - delta receptor
D-K: Dynorphin- kappa receptor}
94
Opioid receptor are ……..receptors
Analgesia is by …..
G protein coupled
All 3 M>k>d
95
What are the morphine antagonists ?
Which one is not antagonist ?
Naloxone
Naltrexone
Nalmefene
Nalbuphine = partial agonist
96
Which are the iv and oral morphine antagonist?
Naloxone = iv
Nalmefine= iv , long lasting
Naltrexone = oral , long acting
97
Uses of naltrexone ?
Teer —> 1. Decrease Opioid addiction
2. Decrease Alcohol craving
Thus given as maintenance drug after de addiction.
98
Most potent acting opioid and shortest acting opioid
Most potent: sufentanyl
Shortest: (fastest acting): remifentanyl
99
Opioid agonist drug acting on all 3 receptors
Sufentanyl
100
What are the egs of partial morphine agonists? Which receptors they act?
Pentazocine : partial agonist M
Agonist K
Nalbuphine : agonist k , antagonist m
Butorphanol : agonist k , partial agonist m
Buprenorphine: partial agonist at m
Antagonist at k,d
101
Use of codeine
It is low efficacy
So only used as cough suppressant
102
Codeine is metabolized by ……cytochrome to …….
Cyp P2D6
Morphine by demethylation
Thus inducer in CYP p2D6: toxicity
Inhibition in CYP p2d6: efficacy
103
Peripheral norepinephrine,serotonin reuptake inhibitor:
Causes …..s/e
Tapentadol > tramadol
Serotonin syndrome
104
Respiratory depression ceiling effect is not seen in ….., seen in …..
Morphine
Seen in mixed agonist , antagonist
105
Straub tail reaction seen with ….
Peripheral action of morphine
Constipation by increasing GI transit time and decreasing GI motility
After administration of morphine in rats, they present with a stiff tail due to spasm of the muscle at the base of the tail.
106
Tolerance to morphine is not seen in which effects ?
Miosis
Constipation
Convulsion.
107
C/I of morphine
1. Biliary colic
2. Head trauma
3. Asthma
4. Extreme of age
108
Drug used for CABG anesthesia
Use of morphine in acute LVF
Fentanyl
Decreases preload, afterload , anxiety
109
Morphine Rx for diarrhea (2)
Loperamide
Diphenoxylate
110
Morphine antitussives (4)
Codeine
Dexomethorphan
Noscapine
Levopropoxyphene
111
Use of Pentazocine
…..is more potent than Pentazocine
Post operative pain , oral tablet
Nalbuphine - iv/im , obstetric analgesia
112
Morphine that can be given as nasal spray
Butorphanol
113
Rx for opioid induced constipation (3)
Alvimopan
Methylnaltrexone
Naloxegal
114
Rx for acute exacerbation of MS
Iv methyl prednisolone
115
Drug given to reduce spasticity
Baclofen
116
Drug to improve speed in MS .MOA
Dalfampridine
Potassium channel blocker
117
Antibodies for relapsing MS
Ocrelizumab- anti CD20
Alemtuzumab- anti CD52
118
What are the drugs given to prevent relapses in MS? MOA (8)
1. Beta interferon
2. Glatiramer acetate- synthetic polymer amino acid
3. Fingolimod- sphingosine 1-phosphate receptor
4. Natalizumab- alpha4 integrin antagonist
5. Teriflunomide- pyrimidine synthesis inhibitor
6. Alemtuzumab- anti cd52
7. Ocrelizumab- anti cd20
8. Dimethyl fumarate ,diroximel fumarate
119
Rx for ALS (4)
1. Iv immunoglobulin
2. Plasmapheresis
3. Physical therapy
4. Respiratory support until recovery
Almost all survive ,majority recover completely within weeks to months.
120
MOA of 1st line drugs for Alzheimer’s disease
Donepezil,rivastigmine , galantamine
Inhibit AchE —> increase Ach in brain
121
MOA of memantine
S/e of tacrine
NMDA blocker
Hepatotoxicity
122
Rho kinase inhibitor used for Alzheimer’s disease ,s/e….
Also used for ….
Fasudil
Vasodilatation
Subarachnoid hemorrhage
123
PDE-1 inhibitor used for Alzheimer’s disease
Vinpocetine
124
Area of brain resistant to neurofibrillary tangles
Lateral geniculate body
125
Alcoholic beverage %
1. Malted liquor: beer , stout
Undistilled, from fermentation of cereals
%: 3-6%
2. Wines: undistilled, from fermentation of grapes
%: 16-22%
Spirit: distilled % 40-55
126
C/I of alcohol (5)
1. Peptic ulcer,hyperacidity,gastritis
2. Epilepsy
3. CLD
4. Unstable patients
5. Pregnancy
127
Drugs with disulfiram like effects
Sorry- sulfonylureas-chlorpropamide
Pluto-procarbazine
Cant -cephalosporin-cefotetan,cefoperazone
Go-griseofulvin
To
Mars-metronidazole
128
Define disulfiram effect (5)
1. Flushing,burning sensation
2. Throbbing headache,vomiting
3. Uneasiness,chest tightened
4. Dizziness,visual disturbance,confusion
5. Fainting, circulatory collapse
129
Pharmacokinetics of alcohol (3)
1. Follows zero order kinetic-constant amount is only eliminated
2. Absorption from stomach is slow,from intestine is fast
3. Peak absorption within 30 mins of alcohol intake
130
What are the local effects of alcohol ? (4)
1. Cooling effect -evaporation
2. Astringent -dissolve proteins
3. Counterirritant & rubifactant- redness,burning sensation
4. Hardening and cleaning the skin-hence used for decubitus ulcers
131
What percentage of alcohol is best? Why? And what does it kill?
70% is better than 90/100% due to decreased evaporation with the 70% and prolonged contact with skin.
Degrades bacterial proteins and dissolves lipids hence bactericidal.
No action against : virus,fungi ,spores.
132
Alcohol blood levels and their effects
20mg%: pt is relaxed
30mg%: relaxed but increased talkative
50mg%: yet in control
50-100mg%: careless,free
100mg%: uncoordinated, slurred speech
200mg%: intoxicated: but can walk
300mg%: stupor
400mg%: death
133
Statutory limit of alcohol for driving is …..
Under act ….
30mg%
185 of Indian motor vehicle act 1988
134
Guidelines for safe drinking
1drink =50ml spirit
=150ml wine
=400ml beer
All contain approximately 16g alcohol that becomes blood 30mg/dl in 30 mins of drinking.
135
What is a hangover ? (5)
Headache, laziness,dry mouth, disturbed mood,impaired performance next morning
136
CNS effects of alcohol
2 sensitive areas of brain
Depressant
Increased talkativeness is due to depression of inhibitory centre.
Cortex, reticular activating system
137
Optic neuropathy seen with alcohol is …..
Brain structure feature of alcohol
Retrobulbar optic neuropathy
Centrocecal scotoma
Widened sulci and ventricles
138
Encephalopathy of alcoholism (4)
Wernicke’s + korsakoff syndrome
Opthalmoplegia -6nerve mc
Ataxia
Confusion
Retro and anterograde amnesia
139
Atrophy of ……is seen
Gliosis of ……occurs
EEG changes
Mammillary bodies
Bergman gliosis
Decrease alpha activity
140
Blood lab changes of alcoholism (4)
Increased MCV
Folate deficiency
Sideroblastic anemia
CDT increase - carbohydrate deficient transferrin
141
CVS effect of alcoholism
Small doses : no change in bp
Moderate doses: bp increase,HR increase
Large doses: bp decrease —> atrial fibrillation-holiday heart syndrome
142
Cancers that occur due to alcoholism (5)
Breast
Oral
Esophageal
Rectal
Liver
143
GIT effects of alcohol (6)
Obesity
Diarrhoea
Gastric erosion
Peptic ulcer
Varices
Pancreatitis-Acute and chronic
144
Bx of alcoholics
Mallory bodies +_ neutrophilic infiltrate
145
Liver changes that occur due to alcohol
Fatty liver : reversible
Hepatitis : fever,jaundice ,vomiting
80% progress to Cirrhosis
146
GGT ,SGOT,SGPT changes of liver
GGT: increased >35U
Increased SGOT/ SGPT
147
Psychiatric changes with alcoholism (6)
Personality changes
Depression
Suicidal ideation
Erectile dysfunction
Delayed ejaculation
Morbid jealousy with fixed delusion
148
Testing for alcohol
Blood alcohol level
Widmark’s formula
149
Alcoholism according to jellineks classification
Gamma alcoholism: malignant alcoholism
Epsilon alcoholism: dipsomania-compulsive drinking
150
Max alcohol is in …..organ of body
Proximal small intestine
151
Questionarres to identify alcohol addiction
CAGE
MAST -Michigan alcohol screening test
AUDIT- alcohol use disorder identification test
152
Stages of alcohol withdrawal
Stage 1: within 1-2 days : Acute shakes
Stage 2: after 48hrs: delirium tremens
Visual hallucinations of snakes,bug
Formication: tactile hallucination of insects crawling
Lilliputian hallucination: objects appear small
Stage 3: alcoholic hallucinosis- auditory hallucinations
153
What is Mc Swan’s sign ?
Stage of narcosis in acute alcohol intoxication
Deep sleep, miosis,but on pinching the face /neck, they dilate and slowly return to their original size
154
Stages of acute alcohol intoxication
Stage of excitement: well being, euphoric
Stage of incordination:
Slurred speech, blackouts, dilated pupils
Stage of narcosis - mc ewan’s sign
155
Most specific breath alcohol test
Gas chromatography mass spectrometry
156
Principle of drunkalyzer/ breathalyzer
Chemical oxidation
Photometry
Uses the principle that alcohol is easily oxidised to acetic acid by oxidizing agents such as potassium dichromate
157
Rx of acute alcohol intoxication (5)
1. Tracheal suction + PPV
2. Induce vomiting
3. Gastric lavage
4. Iv NaHCO3 + thiamine+ glucose
5. Hasten recovery with hemodialysis
158
C/f of chronic alcoholism
Tolerance
Dependence
Withdrawal sms
159
Rx of chronic alcoholism (5)
1. Social and motivational therapy
2. Substitutinal therapy - long acting diazepam
3. Naltrexone: long acting - decrease relapse, decrease craving
4. Acamprosate: NMDA antagonist
5. Disulfiram-those who sincerely want to leave the habit
160
…….recovers earliest in wernicke’s encephalopathy
Opthalmoparesis
161
Avoid ……in chronic alcoholic why?
Phenytoin
As alcohol is a CYP induced and decrease level of phenytoin ppt seizures
162
Rehab of alcohol
Alcoholic anonymous AA
163
Level of methanol that causes effects
15ml- blindness
30ml- death
164
Rx for methanol poisoning (8)
1. Keep the pt in quiet,dark room
2. Protect eyes from light
3. Supportive measures to maintain ventilation
4. Gastric lavage with NaHCO3
5. If hypokalemia-KCl
6. Ethanol
7. Fomepizole (alcohol dh inhibitor)
8. HD
165
Difference between first generation and second generation antipsychotics
First generation : neuroleptics
D2 blockers
Second generation:
atypical
5HT2A blockers
Less EPS
Benefit in positive and negative sms
166
Antipsychotic that is most potent
DOC for schizophrenia
Risperidone
Atypicals like aripripazole
167
Antipsychotic that can be used for Hyperprolactinemia
Aripripazole as it’s a partial agonist at D2 receptor
168
DOC for schizophrenia in pregnancy
Why is second generation not given?
Haloperidol
Not preferred as there is higher incidence of low birth weight baby and abortion.
169
DOC for resistant schizophrenia
Define resistant schizophrenia
Clozapine
Schizophrenia not responding to 2 or more drugs
170
Uses of clozapine (3)
1. Resistant schizophrenia
2. Tardive dyskinesia
3. Anti suicidal indication
171
S/e of clozapine (6)
1. Sedation
2 Sialorrhoea- wet pillow
3. Weight gain
4. Agranulocytosis
5. Seizures
6. Carditis
172
Labs that must be done when giving clozapine
CBC- agranulocytosis
ECG- carditis
173
Psychotic sms that is most beneficial by neuroleptic drugs
Hallucination and delusion
174
Sms improved in order while giving antipsychotics (4)
1. Biological sms- sleep, appetite
2. Auditory hallucinations
3. Delusion
4. Negative sms
175
How long should antipsychotics be given if no psychotic sms after rx?
1st episode : 2yrs
Subsequent episodes: 5 yrs /indefinitely
176
Max weight gain is for …….why?
Clozapine
Due to blockage of H1 receptor
177
Cause and Rx of tardive dyskinesia
Drug c/i?
Supersensitivity of D2 receptor to prolonged D2 blackage.
Rx:
1. Stop the drug
2. DA deplete drug -VMAT- valbenazine
3. Shift to clozapine
4. Gingko biloba-herbal drug.
C/i: central anticholinergic can worsen TD, hence not given.
178
Doc for L-dopa induced schizophrenia
Pimvanserin
179
DOC for multiple relapses of schizophrenia caused by non compliance
IM formulation:
FGA: fluphenazine
Haloperidol
Zuckopenthixol
SGA: Risperidone
Olanzapine
Paliperidone
180
Problem with tardive dyskinesia
Sms
Can occur even after offending drug has been withdrawn long time back or with Rx for >6months-1yr.
Sms:
abnormal movements
Constant chewing
Puffing of cheeks
Thrusting of tongue
181
Drug causing paradoxical tachycardia
Drug causing malignant hyperthermia. Rx
Quinidine
Succinyl choline
Halothane
——increase calcium from RYR receptor
Rx: dantrolene
182
Define neuroleptic malignant syndrome (3)
Rx? (3)
Rigidity
Hyperthermia
Cv collapse secondary to D2 blockage
1. External cooling
2. Bromocriptine > dantrolene
3. Amantadine
183
Antipsychotics not given to elderly with dementia . Why?
They can increase mortality- stroke.
Eg: Risperidone
Olanzapine
184
What are the positive and negative sms of schizophrenia? Drug of choice ?
Positive : delusion, hallucinations
Negative :
asocial, Alogia, affective blunting
DOC: SGA
Haloperidol- only positive sms rx
185
High potency and low potency typical antipsychotics
Low potency: chlorpropazine, thioridazine
Less EPS
High potency: haloperidol, trifluperazine
High EPS
186
What are the EPS? Timing ? Rx
4 hrs:
Acute dystonia -earliest
Seen mainly in young men and girls <10yr
Oculogyric crisis- upward movement of eyes
Rx: Central anticholinergics
Benzhexol, trihexylphenydyl, promethazine
4 days: akinesia-Parkinsonian sms
4 weeks: akathesia
Mc s/e- desire to move around ; restless
Rx: propanolol
4 months: tardive dyskinesia
Rx: clozapine
187
Antipsychotic c/I in angle closure glaucoma. Why?
Thioridazine- max anticholinergic action
Dry mouth, blurred vision, mydriasis, urine retension.
188
Max sedation is with ……. Antipsychotic
Another side effect is ….
Chlorpromazine
Cholestatic jaundice
189
Endocrine side effects of antipsychotics
DA blocker- Hyperprolactinemia, amenorrhoea, galactorrhoea
190
DOC for neuroleptic malignant syndrome (3)
Sms of NMS (3)
1. External cooling
2. Bromocriptine > dantrolene
3. Amantadine
Sms: rigidity
Hyperthermia
CV collapse
191
DOC for initial hiccups
DOC for intractable hiccups
Hiccups: initial: baclofen, gabapentin
Intractable :
chlorpromazine + metoclopramide
192
Uses of antipsychotics
1. Psychosis- schizophrenia
2. Others :
Main Anti Psy Cho Tic Hoo
Maniac
Antiemetic - procarbazine, olanzapine
Psychosis L-dopa- pimvanserin
Chorea: hunting tons , syndenhams
Tic disorder: Tourette syndrome
Hiccups
193
Antipsychotic given for chemotherapy induced vomiting
DOC for Tourette syndrome (3)
Olanzapine
1. D2 blocker : pimozide, haloperidol
2. Atypical : risperdone
3. Clonidine
194
Doc for restless leg syndrome
Patch used
Pramipexole, ropirinole - DA agonist
Rotigotine patch
+
Iron replacement for anemia
195
1. Max EPS is with ……
2. Max EPS among atypical antipsychotics
3. Min EPS among atypical antipsychotics
1. Haloperidol
2. Risperidone
3. Clozapine
196
1. Clozapine blocks ……..receptors
2. Max weight gain
3. Least weight gain
4. Drugs causing Qt prolongation
1. 5HT2A, D1,D4, very less D2
2. Clozapine
3 . Ziprasidone, aripripazole
4. Thioridazine, Ziprasidone
197
Long acting (depot) injections of antipsychotics
First generation:
1. Haloperidol
2. Fluphenazine
3. Flupenthixol
Second generation:
1. Risperdone
2. Aripripazole
3. Olanzapine
4. Ziprasidone
198
All antipsychotics cause qt prolongation except ….
Qt prolongation is due to …..
Lurasidone
Inward K+ channel block
199
Eye and skin side effects of chlorpromazine (3)
Corneal and lens deposits : whorl like
Cataracts
Blue-grey skin pigmentation
200
Specific side effect of eye for thioridazine
Quetiapine causes …..
Retinal deposits-salt and pepper
< 800mg/dl
Cataract
201
Haloperidol is DOC for ..(3)
1. Acute schizophrenia
2. Huntingtons chorea
3. Gille’s de la Tourette syndrome
202
Uses of chlorpromazine (5)
1. Psychiatric uses
2. N/V rx
3. Intractable hiccups
4. Preanesthetic meds
5. Skeletal muscle relaxation in tetanus
203
Checking for agranulocytosis in clozapine is ….
CBC weekly X 6 months , then biweekly
204
What are the H3 receptors? What are the uses of inverse agonist at H3 receptor ?
H3 receptor: presynaptic NE release blocker. It’s an autoreceptor.
H1 receptor is necessary for wakefulness
Therefore H3 receptor —> sedation.
H3 inverse agonist : pitolisant, tiprolisant
Increase H1 release—> increase wakefulness .
Used in narcolepsy
205
Other than antipsychotic action, what else does Ziprasidone and aripripazole have?
Antidepressant
Antianxiety actions
206
Antipsychotic with least chances of cognitive dysfunction
Aripripazole- partial agonist
207
Hyperprolactinemia is main side effect for ….(3)
FGA
Risperidone
Amisulpirid
208
DOC for Huntingtons chorea
1. DA depleter- tetrabenazine (block VMAT
2. Haloperidol
209
DOC for syndenhams chorea
Phenobarbital —-> resistant—> haloperidol
210
Action of antidepressants are …..
First line antidepressant
DOC for severe depressant
Slow- 3-4 weeks
SSRI
SNRI > TCA
211
DOC for atypical antidepressant
DOC for Resistant depression
MAOI
Esketamine nasal spray
212
DOC for post partum depression
Brexanolone
213
Doc for fibromyalgia
Fatigue, generalized bodyache, labs normal
Rx: SNRI- Milnacipram
Also used for neuropathic pain
214
Duloxetine s/e
Venlafaxine s/e
Hepatotoxicity
Increase bp, increase HR
215
TCA blocks …(2)
Types
SERT, NET blocker
Tertiary amines: SERT blocker
Eg: clomipramine- max SERT blocker
Secondary amine: NET blocker
216
Max SERT blocker is ……
Doc for premature ejaculation ….
Clomipramine
Dapoxetine
217
S/e of paroxetine (5)
1. Sexual s/e
2. Weight gain
3. Teratogenic- pulm HTN, cardiac septal defect
4. Max sedation
5. Increased withdrawal
218
Antidepressant that exerts protective effect from suicidality
Antidepressant with Qt prolongation (2)
Venlafaxine
TCA, citalopram
219
Antidepressant with dose related CV effect
Antipsychotic with no effect on prolactin (2)
Citalopram
Clozapine
Aripripazole
220
AntiHTN that should not be given with TCA is……
Clonidine
221
Uses of TCA
MiND COP
1. Migraine prophylaxis
2. Neuropathic pain -TCA,SSRI, pregab,gabapentin
3. Depression - effective in severe depression
4. Childhood disease: ADHD,nocturnal enuresis
5. OCD - Clomipramine,SSRI- DOC
6. Pruritus- doxepin
222
DOC for nocturnal enuresis
1. Desmopressin
2. ADHD+ nocturnal enuresis- imipramine
223
Antidepressant used in children
Drugs used for acute vs chronic anxiety
Fluoxetine
Acute: BZP, beta blockers
Chronic : fluovoxamine -SSRI
224
DOC for PTSD (2)
Sertaline
Paroxetine
225
DOC for eating disorder
S/e of fluoxetine (3)
Fluoxetine
S/e:
1. Increase 5HT3-GIT: nausea>diarrhoea
2. Sexual S/E: 5HT2: ED, delayed orgasm
Anorgasmia
3. CNS: anxiety , insomnia
226
Difference between bupropion and buspirone
Bupropion: antidepressants
Smoking cessation
Weight loss
Buspirone: antianxiety-
no anticonvulsant muscle relaxing property
227
What are the transdermal patches we know of? And for what diseases is it used? (4)
Transdermal patches :
1. Depression: selegilline
2 Alzheimer’s: rivastigmine
3. Post menopausal sms: clonidine
4. Parkinsons disease: rotigotine
228
S/e of reserpine
VMAT blocker- depression.
229
Longest and shortest acting SSRI
Longest: fluoxetine
Shortest: fluvoxamine
230
Most teratogenic SSRI
Most specific SSRI
Paroxetine
Esitalopram
231
Vilasodone MOA (2)
SERT blocker
Partial agonist at 5HT1A
232
DOC for stress incontinence ; mechanism
Duloxetine
Constricts bladder sphincter
233
Reason for delayed effect of antidepressants (2)
1. Inhibition of autoreceptors
2. Synthesis of brain derieved neuroleptic factor.
234
Drugs that can cause anxiety (5)
1. Bupropion
2. Reserpine
3. Amphetamines
4. CCK
5. SSRI
235
Best DOC for OCD
Resistant OCD
SSRI-fluovoxamine
Clomipramine
236
Best drug for PMS
MOA of TCA (3) and s/e
Fluoxetine
Mu blocker -dry mouth,mydriasis
Alpha blocker -hypotension
H1 blocker - sedation
237
Long term rx for severe anxiety with intermittent panic attacks
Define panic attack. DOC
SSRI
Sudden,severe,spontaneous anxiety attack,feeling of impending doom.
DOC: BZP- alprazolam,clonazepam,lorazepam,diazepam
238
Define panic disorder,DOC
4 or more panic attacks /yr
DOC: SSRI, / buspirone /TCA
239
MOA of buspirone
Partial agonist at 5HT1A
Slow acting anxiolytic
No physical dependence
No withdrawal
240
MOA of Mirtazepine
1. Block presynaptic receptor ->increase NT release
2. 5HT2 blocker
3. 5HT3 blocker
241
S/e of mirtazepine (3)
1. Highly sedative
2. Max weight gain
3. Agranulocytosis-rare
242
Best tolerated TCA is …..
Nortriptyline
243
TCA + D2 blocker is ……
SNRI egs. (3)
Amoxapine
Duloxetine
Venlafaxine
Milnacipran
244
NARI Eg
Noradrenaline reuptake inhibitor
Reboxetine
245
5HT2 antagonist (2)
Nefazodone
Trazodone
246
MOA of bupropion
NDRI- norepinephrine dopamine reuptake inhibitor
Block NET, DAT
No action on 5HT-no sexual s/e
247
MOA of Agomelatine (2)
Melatonin receptor agonist
5HT2C antagonist
248
Less sedating TCA
S/e of TCA
Desipramine
1. Metabolic acidosis
2. Myoclonic seizures-diazepam
3. Increase HR
TCA not removed by HD as it has higher Vd.
TCA lower seizure threshold.
249
S/e of TCA at high doses (2) Rx for TCA poisoning
1. Seizure
2. Cardiac arrhythmia
Iv NAHCO3
250
Rx for sexual dysfunction caused by SSRI
Safest SSRI to use with warfarin
Cryptoheptadine
Sertaline,citalopram- rest all cause bleeding as they affect platelet serotonin levels.
251
SSRI causing SIADH in elderly
SSRI used in GAD, s/e
Fluoxetine
Venlafaxine
Increased Bp
252
……causes seizure in bulimic patients
SSRI safe in acute MI or angina
Bupropion
Sertaline
253
SSRI causing priapism (2)
Trazodone
Nefazodone
254
Nefazodone should not be given along with…..(3) due to risk of ……&……
Terfenadine
Astemizole
Cisapride
Qt prolongation
Hepatic failure
255
………… is a glutamatergic modulator
Eg of NaSSA uses(2)
Tianeptin
Mirtazepine
Noradrenergic Selective serotonin antidepressant
Use: antiemetic, appetite stimulant
256
Non selective MAOI (2)
Phenelzine
Tranylcypromine
257
Reversible and selective MAO A Inhibitor
Moclobemide
258
MOA B selective inhibitor
Selegilline
259
MOA of MAO I
Inhibit MAO irreversibly, increasing NE and serotonin conc in the synapse and improve mood.
260
DOC for cheese reaction
2 syndromes with MAOI
Phentolamine
1. HTN crisis -
ingestion of pressor amines,tryramine containing food.
2. Serotonin syndrome-
MAOI + SSRI
MAOI+ venlafaxine
SSRI alone at high doses .
261
Sms of serotonin syndrome
Rx.
HARMS
Hyperthermia
Autonomic instability
Rigidity
Myoclonus
Seizures
Death
1. Stop the offending drug
2. Cyproheptadine
3. Start SSRI only after 14 days of stopping MAOI
262
DOC for psychotic depression
Drug to reduce craving in cocaine withdrawal
Amoxapine
Desipramine
263
Antidepressant with hepatotoxicity
Nefazodone -withdrawn from market
264
Antidepressant with wakefulness
Bupropion-amphetamine like metabolite
Anxiety
Weight loss
Seizure
265
Antidepressant with sedation (2)
Mirtazepine
Trazodone
Therefore they are used to rx insomnia
266
DOC for narcolepsy
Therapy for borderline personality disorder
Modafinil - mood alert
Dialectical therapy
267
Mood stabilizers eg (4)
1. Lithium
2. Carbamazepine
3. Valproate
4. Lamotrigine
268
Difference between bpd1 and bpd2
BPD 1: Single mania
BPD2: major depression + hypomania
269
Doc for acute mania (4)
1. Antipsychotic + lithium
2. Antipsychotic
3. Valproate
4. Lithium
270
C/f of acute mania (4)
Increased mood/irritability
Decreased sleep
Increased energy
Goal directed activity
271
Doc for rapid control of mania
What are rapid cyclers ? DOC
Olanzapine
>-4 episodes of mania/depression within 1 year.
DOC: valproate
272
Note of lithium toxicity
>80% lithium is reabsorbed in PCT
Lithium is a competitive inhibitor at na-li channel
1. Acute tubular necrosis- increase excretion of lithium-no toxicity
2. Hyponatremia- increase toxicity
273
Causes of hyponatremia for lithium toxicity (3)
Dehydration
Diarrhoea
Diuretic - thiazide / furosemide/k+ sparing
274
Lithium therapy was started by …….
It is a ……salt
John F cade
Carbonate salt-converted to chloride in stomach
275
MOA of lithium
Inhibit hydrolysis of ionositol-1-p04
276
Only mood stabilizer with anti suicidal action
Psychiatric uses of lithium (4)
Lithium
1. Acute BPD
2. Major depression
3. OCD
4. Schizoaffective disorder
277
Non psychiatric uses of lithium (4)
1. Migraine - cluster headache
2. Neutropenia
3. SIADH
4. Ulcerative colitis
Cyclical vomiting
278
Starting dose of lithium
Care of lithium for a patient undergoing surgery
300mg BD/TDS
Stop it 24 hrs before surgery
279
Blood lithium levels decreased by …..(5)
1. Bronchodilators:
theophylline, aminophylline
2. Verapamil
3. Carbonic anhydrase inhibitors
4. Osmotic diuretics : acetazolamide,mannitol
5. Sodium bicarbonate
280
Doc for prophylaxis of BPD
Signs of lithium toxicity (4)
Lamotrigine
1. N/V/ profuse diarrhoea
2. Coarse tremor
3. Hyperreflexia,
ataxia,
confusion,
convulsion,
4. Death
281
Rx of choice of antipsychotic in pregnancy
1. Acute mania
2. Prophylaxis
1. Antipsychotic
2. Lamotrigine
282
Monitoring for lithium toxicity
T1/2: 24 hrs
Time to steady state- 4-5 t1/2= 4-5 days
Therefore: blood levels taken after 12 hrs after last dose
283
What are the blood tests to be done for lithium toxicity?
Test- tremor fine mc, coarse- overdose
TFT: hypothyroidism, hyperthyroidism
UPT: teratogenic
BC: leucocytosis- increase GCSF
ECG: T wave inversion/ sick sinus/Av block
Weight: gain
Electrolyte- hyperK, hypercalcemia
Edema
KFT- Nephrogenic DI
Others : diarrhea, acne, worsen Psoriasis
284
Therapeutic levels of lithium in
1. Acute mania
2. Prophylaxis of BPD
3. Toxicity
4. Hemodialysis
1. 1-1.0 mEq/L
2. 0.5-1.0 mEq/L
3. >1.5mEq/L
4. >3/>4 mEq/L
285
Sleep cycle stages
Stage 0: first 1/2 hrs, eyes closed only
Stage 1,2,3
Stage 4: deepest stage of sleep
Stage 5: REM
286
Classification of barbiturates
Long acting : phenobarbitone
Short acting: butobarbitone, pentobarbitone
Ultra short acting : thiopentone
287
3 MOA of barbiturates
1. GABA facilitatory action
2. GABA mimetic action- at high doses
3. Glutamate inhibitors through AMPA receptor
288
Sensitive area of the brain where sedative, hypnotics act
Dose dependent action :
Reticular activating system
Sedation —>sleep—>anesthesia —>coma
289
Sleep pattern of using barbiturates
Decrease sleep latency
Increase sleep duration
Sleep architecture disturbed -
REM, stage 3,4 decreased
Stage 0,1,2 increased
290
Uses of barbiturate
Phenothiazine- epilepsy
Thiopentone- anesthesia
291
Barbiturates can cause anterograde amnesia, forget earlier dose was taken and keep taking it again and again—> overdose
Features of barbiturate poisoning (4)
1. Unconscious
2. Respiratory collapses
3. Circulatory collapse
4. Shock
292
Management of barbiturate poisoning (4)
1. Gastric lavage
2. Airway protection
3. IVF - NaHCO3
4. Alkaline diuresis
4. H.D
293
Classification of BZP
Based on uses :
1. Hypnotic:
Diazepam, fluzepam,alprazolam,nitrazepam
2. Antianxiety:
Diazepam, chlorpromazine, oxazepam, lorazepam
3. Seizures
Diazepam,lorazepam,clonazepam
294
Non competitive GABA antagonist
Competitive BZP antagonist
Bicuculine -act in b sub unit
Flumazenil
295
GABA inverse agonists
DMCM- dimethoxymethylcarbomethylcarboline
296
Drug that blocks Cl- channel directly
Picrotoxin
297
Action of BZP (5)
1. Sedation
2. Hypnosis
3. Anticonvulsants
4. Analgesia
5. Anterograde amnesia
298
Advantages of BZP over barbiturate (6)
1. Flat DRC
2. No action on respiratory/CVS/ body syst
3. Minute disturbance in sleep architecture
4. No CYP induction
5. Lower abuse potential
6. Flumazenil- specific antidote
299
DOC for chronic anxiety
DOC for performance anxiety
Chlordiazepoxide
Propanolol
300
BZP drugs given for insomnia (2)
Zolpidem, zaleplon
301
Egs of azapirones
MOA
Uses
Buspirone
Gepirone
Isapirone
Partial agonist of 5HT1A - decrease release of 5HT
No sedation, anticonvulsant or muscle relaxant properties
Ineffective in acute anxiety
302
BZP with active metabolites (5)
Alprazolam
Buspirone
Chlordiazepoxide
Diazepam
Flurazepam
ABCDeF
