Professional Documents
Culture Documents
Pcol - CNS
Pcol - CNS
Drugs of Alzheimers
•
•
Amyloid Hypothesis amyloid aggregation
-
misfolded protein →
amyloid plaque ↓
-
•
cholinesterase inhibitors
-
Donepezil
1-
AChE & BUCHE
Rivastigmine -
act on both
Galant amine
Amyloid plaque
• NMDA -
R Antagonists 1.) f) glutamate
Glu
:;÷:/
" run .mn
.
amt Of glutamate ↓
Neman time 2.) it ) glial cells
.
↑ 61h
-
↑
acid release
Glut NMDA
-
R =
neuronal death
↓
cat channel opens
↓
Cat influx
↓
too much cat
↓
neuronal rupture
↓
neuronal death
faithgsb
• Glutamate Inhibitors
Adenosine
Lobe / Uzole
iargacept
"
results in ↑
signaling when the Ns is
under stimulated & ↓ signaling when
the Ms is overstimulated → Ns
"
Volume K ? "
Tx : Replace ; Tx : Anti -
cholinergic
agents
Dopamine
cannot be given as medication
exaggeration Ach
-
tremors .
OF
-
it enter BBB ( Blood Brain Barrier)
-
give L-DOPA
BLOOD :
1.) Trine ✗ µ phenidyt
1.) decarboxylase ( 90% gets destroyed ) 2.) Benz tropine -
DOC
2.) WMT
g.) piperidine
BBB a.) prooyclidme
1- DOPA enters brain
}
capbidopq Diphenhydramine
g.)
-
GNS
BEQ )
tolcapone (
-
WMT t )
-
stimulate D receptor
Amantadine
-
↑ release of DOPA
BEQ : -
SE : lived reticular is
levodopa + MAOIs ×
levodopa + Vit .
136 ✗
-
induces decarboxylase
→ more L-DOPA
destroyed
levodopa -1 Antipsychotics ✗
-
antagonistic action
faithgsb
OTHER
diseases
",!÷"""!¥÷
Huntington 's
Wilson 's
disease
disease
v
↑
GABA
Dopamine
Haloperidol
( chelating agents)
Haloperidol
Tourette syndrome
Molindon
faithgsb
?⃝
Anxiolytic / sedatives / Hypnotics
Anxiety
-
ANXIETY
signs & symptoms
disorder
GABA -
A Receptor
bin opening of Cl
% DCI influx
-
GABA GAR p
Channel
1
inside becomes
, act here
Anxiolytic
[
negative >
I
" "" "
hYPerP%ari µ, ,
,, , ,
calming effect
, , ,, , , ,, , , , , , , , , a- channel opening ( FREQUENCY)
g.
,
, , ↑
Zolpidem
social phobia Fear of speaking in front
•
• -
. iaiepion
Of a lot Of people •
Eszopidone
•
Generalized Anxiety -
•
situational Anxiety Disorder ☐ Melatonin -
agonists -
Rame Heon
pure anxiolytic
-
non
-
sedative
•
Bus pirone
•
Ipsa Pirone
Gepirone
•
Benzodiazepines Barbiturates
•
most widely used anxiolytic 1.) ↑ GABA
USES OF BENZODIAZEPINES
Drug Indications
withdrawal states
faithgsb
BENZODIAZEPINES
""°
short -
Acting Intermediate -
Acting
Duration : 2- 8 hours
Duration I -3
Duration : 10-20 hours .
:
days
Drugs :
Chaplain Died From
Drugs : Charlie
Drugs :
1.) Lorazepam
1.) Clozapine a- fever
special uses :
•
Diazepam > D% for status epilepticus most common side effect : depressant ; sedation
lvalium)
Antidote : Flumazenil
•
ohlordiazepoxide } DOG for alcohol withdrawal
CI : another depressant
( Librium)
e. g. 132-1 alcohol
•
Alprazolam > DOC for panic attack ( non drug)-
( Xanax )
BARBITURATES
short Acting Ultra short-Acting Intermediate Acting long Acting
- -
-
-
faithgsb
SCHIZOPHRENIA
DA Hypothesis : ↑ dopamine
or
↑ serotonin
PSYCHOSIS
4 major parts of the brain affected by dopamine :
Mesolimbic
Antipsychotics
Mesowrtical Nigrostriatal
SE :
movement
HIS / SX f) SISX 1.) Eps
IE : EPs
typical atypical 2.) Hypcrprolactinimia
}
Hallucinations Affective flattening
Delusions / wtrkf.ie#n%1Alogia
"' ""' " "" "" " " P ""
"
-
TYPICAL ATYPICAL
thioridazine Clozapine
thiothixene Olanzapine
flu phenazine Quetiapine
Ziprasidone
Prochloroperazine
Aripiprazote
•
an
typical are high potency
typical vs Atypical
except chlorpromazine &
thioridanñe
>
high potency :
Typical Atypical
/✗ / Hi
potency M High :D
:
slow , ,
Receptor blockade low : M.a.lt
✗ '
H
Manifestations :
✓
positive symptoms ✓
7.) JH -12C : weight gain
hyperiipidimia Negative symptoms ✗ ✓
hyperglycemia
f) 2 ,
: ↓ BP EPs ✓ ✗
C.) H, : sedation
tardive dyskinesia ✓ ✓
faithgsb
Motor Disturbances
Antipsychotic -
induced
•
Acute Dystonia
-
amantadine ITBADJ
• Parkinsonism ↓ dopamine
-
resting tremor
-
and trunk
tongue ,
sets in
typically irreversible
-
once
• Akathisia
-
-
Tx : lower medication dose BB 132 ,
,
,
anticholinergic
•
Neuroleptic Malignant syndrome
-
-
Tx : Dantrolene , bromooriptine ,
amantadine
{
Chemical Classes
Important Uses :
• Phenothiazines
chlorpromazine
}
>
Aliphatic
-
piperidine tnioridazine
Anti emetic
-
>
Proohlorperazine
-
"
" " " "" " " " " "" " "
Anti
chlorpromazine hiccups
-
• Butyrophenones -
haloperidol
Dinydroindolines Molin done
-
Promethaiine Anti -
histamine
•
-
•
Diphenyl butyl piperidine pimozide _
Clozapine
alternative drug when
every
thing tailed
other toxicity
Aripiprazole & Olanzapine Bipolar Disorder
.
•
clozapine
blood
agranulocytosis
'
Tourette
-
>
Molin done Disease
• thioridazine
>
eyes =
pigmentary retinopathy
other uses of antipsychotics
1 cardiotoxic
•
Antiemetic -
blocks D receptors _
prochlorperazine
• -
L U L L
faithgsb
ANTICONVULSANTS
Anticonvulsants
Glu & inhibitory GABA
-
imbalance between excitatory
inside
Glu binds to gamma receptor →
effect : Na Rca channel opening Na & Ca influx • more + • depolarization ☒ seizure formation
inside •
hyperpolarization • prevent seizure
receptor •
Therefore ,
partial seizures
-
simple partial
•
motor ( Jacksonian March)
•
sensory 1 tingling ,
paresthesia)
•
no loss of consciousness ( LOC)
complex partial
-
•
LOC
•
during Loc : hallucinations ,
chewing rubbing
,
Generalized seizures
tonic -
•
clonic 11-2 mins ) -
muscle contractions alternating
with relaxation
children
* Febrile seizure
-
alternations of consciousness lasting 10-30s
-
, ,
☒
Myoclonic
-
trunk muscles
-
no LOC
. faithgsb
Main problem :
ca channel opens
•
pre ganglionic neuron -
open Na channels →
High voltage-gated
slow type ca channel opens
postganglionic neuron -
GM binds to NMDA & AMPA receptors in postsynaptic cleft AMPA : Na goes inside cell µ
Depolarization seizure
prevent reuptake :
1- ) GABA T
Na channel blockers
ca channel blockers
AMPA blockers
Increase sV2A
> NIA stimulants
•
levetiracetam
Felbamate
•
AMPA Inhibitor
•
topiramate
tiagabine
GABA transporter Inhibitor
•
vigabatrin
Valproic Acid
Ethoiuxsimide
lamotrigine
Topiramate
lamotrigine
tonic clonic ilalproio Acid
-
SIE :
Absence Etnosuxsimide
1.) Phenytoin
-
Gingival Hyperplasia
Myoclonic llatproic Acid
.
teratogenic
Atonic Halprin Acid
Phenobarbital
Febrile
Diazepam
New : Lorazepam ,
Old :
Diazepam
Status Epilepticus Phenobarbital
Phenytoin llardiotoxio due to
propylene glycol)
Note : All can be used interchangeably EXCEPT Ethosuxsimide lspecific for Absence seizure)
faithgsb
Antidepressants
Depressant =
↓ NE ↓ serotonin
} Bipolar ANTIDEPRESSANTS
Mania =
↑ NE ↑ serotonin -
neurotransmitter
imbalance
criteria
major (1)
}
1. Anhedonia
2. Depressed mood 12 weeks )
"" "" "" "" "
' Mai " ← " = " " ""
t
appetite
-
1. ↑/↓
depression
2. wt .
gain / wt loss .
3. insomnia / hypersonic
4. easy fatigu ability
5. loss of concentration
6- suicidal thoughts
7. suicidal attempts
Reuptake Inhibitors
•
selective serotonin Reuptake Inhibitors
Advantage :
✓ lesser lethality with overdoses
/ !!! !
" "'m :
1.) sertraline -
give 1 Week
3.) Fluovaxine
4.) Paroxetine TCAs
and line :
6) Escitalopram
inhibition of b- HT reuptake
NOA : Allosteric
Rts
•
serotonin Norepinephrine
☐ venlafaxine
☐
Desvenlafaxine
☐ Duloxetine
•
Monoamine oxidase Inhibitors
>
Non-selective
}
also carboxazid
/ & NE
☐ Pnenylezine
"
tranylcypromine
☐
blorgyline
'
MAO -
A I
> MAO BI -
☐
selegiline
☐
Rasagiline
inhibit MAO which metabolizes
MOA : the
eniyme
ME ,
5- HT & dopamine
faithgsb
•
serotonin Receptor Antagonists
☐ Nefa 20 done
☐ 1- random
Remember ! ! !
1A :
Anxiolytic
26 :
Antipsychotic
Atypical Antidepressants
☐ Bupropion
f) Dopamine reuptake
1- 1 DAT
☐ Mirta rapine
f) ✗ 2
Vila 20 done
}
☐ 1-1 SERT
faithgsb
BIPOLAR
108770000 disorder
↑ NE ,
↑ Serotonin
achieving remission
-
80% overall success rate for
MOA :
☐
f) synthesis
lanabolism )
↑
reuptake
f)
↓ Release
↑ ME ↑ destroy
↑ serotonin 1 catabolism)
I/ Receptor sensitivity
-
first
-
Moa :
& NE release
↓
↑ NE metabolism
↓
↑ NE reuptake
↓
b- NE 851ft
-
receptor
sensitivity
-
lithium vs Na
X
-
Pregnant :
☒ii*awmm
Baseline labs Adverse effects
Function Hypothyroidism
thyroid
IT 3,1-4
Electrolytes Decreased Na
lesp sodium)
.
( check Nat
CBO leukooytosis
( ↑ WBC)
if no lithium ,
alternative : chlorpromazine
Mannitol
DOC for lithium toxicity :
osmotic diuretic
no Na
-
effect on
faithgsb
⑧ PD⑧0④8iᵈ⑧ fFB8
"
narcotics
"
-
a.k.a
-
alkaloid :
juice of opium poppy seed
delta receptors in CNS
-
my ,
Kappa ,
Receptors
like loperamide
•
M receptor
*
-
of psychotic
.
•
0 : unknown 1 delta)
• Morphine
choice for all types of pain
-
analgesic of
•
-
opiate withdrawal
☐ Methadone liver CA
•
Heroin
☐ Heroin very thin ( metabolite)
-
diacetylmorphine
partial Agonist can enter BBB & become
-
morphine
t antitussive
☐ Oxycodone
-4 Hydrocodone
☐
Oxy morphine
☐ Hydro morphine
☐ codeine
other ways to classify
a.) Natural
mixed Agonist / Antagonist
☐ Morphine
•
☐ Pentazocine ☐ codeine
Nalbuphine BEQ naloxone
☐
☐ Thebaine -
☐ Naloxone -
snorter -
☐
Apomorphine -
emetic
Naltrexone longer acting
-
☐
☐ -
☐ Hydrocodone -
antitussive
☐
Oxycodone
a Hydro morphine
☐
Oxy morphine
☐ Pentazocine
faithgsb
?⃝
Trust in the Lord with
all your heart
Proverbs 3:5-6