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Central Nervous System Drugs

Central Nervous System Drugs

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Published by redroses131
CNS Drugs
CNS Drugs

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Published by: redroses131 on Apr 18, 2013
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10/03/2013

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Central Nervous System Drugs
: By: Mrunal Koche
 
 Anticonvulants
antiarrythmic of the brain
irregularity of the brain
 
 Antiparkinson
lot of new drugs are in the market to manage the symptoms of 
Parkinson’s
 
 
Opioid analgesics
(to relieve pain without losing consciousness)
 
 Anesthetic
,
 Antipsychotic
and
 Antidepressant 
 
 
CNS stimulants
:
 
 Amphetamine
 
o
 
ADHD
Rx:
methylphenidate
 
(ridaline) and
Pemoline
,
Atomoxitine
 why are we giving a stimulant for a kid with hyperactivity, the brain is superactive, so when u give a drug that stimulates the brain, the brain will think it isstimulated, so it
ll calm down.
o
 
NARCOLEPSY
attack of sleep during daytime
 
sudden attack of sleep
thatis accompanied by cataplexy
loss of muscle tone
 
Treat with
Dextroamphetamine
 
 
Modofinil 
 
Used in sleep disorders such as
(SWSD)
 
Shift worksleep disorder
.
 
Doxapram
Treatment as a respiratory stimulant after anesthesia.
 
Stimulants are controlled substances b/c of their
risk of dependence & abuse
.
 
Avoid Coffee with stimulant b/c of its further action as a stimulant
 
Last dose should be 6 hours before bedtime
.
 
CNS Depressants(Sedatives & Hypnotics)
 
 
 
Sedative dosage increase & its effects
 
 
 
Sedation & decrease anxiety
 
Hypnosis, Anesthesia, Respiratory & vasomotor depression and Coma.
o
 
 
Benzodiazepines
 
and
Barbiturates, & GABA
 
 
Activate GABAa receptors
 
inhibitory NT, calm down, decrease the firing in the brain
 
Activation of GABAa receptors leads to
increase in Cl ions
 hyperpolarization (relaxation).
o
 
GABA receptors has 5 receptors, a, b, y, and we don’t care on the other 2
 
o
 
GABA binds to the receptor,
benzos binds to y (BZ receptor)
,
barbiturates bind tobeta receptor 
.
 
o
 
BACLOFEN 
 
binds to GABAb receptors
 
 
GABAb decreases potassium
 
hyperpolarization (
 phase III
)
 
Benzos bind to its own receptors (BZ receptors)
Y site
 
 
BZ1
these drugs are for sleep
 
BZ2
memory, sensory-motor, cognitive
like anxiety
 
Barbiturates bind to
B-stie
 
 
These increase the duration Cl channels that are open.
o
 
So at high doses Barbs open Cl channels but block Na
+
channels.
 
Barbiturates
 
 
 
Phenobarbital 
:
o
 
Long-acting drug for Seizures
.
 
 Amobarbitol 
 ,
Secobarbitol 
 ,
Pentobarbitol 
 
o
 
These are
Intermediate Acting drugs
.
 
Thiopental 
 
o
 
Ultrashort acting used for IV Anesthesia
.
Indications
 
seizures
 
Insomnia
barbs
aren’t
prescribed anymore
 
don’t want to become
addictive, reduced the REM sleep.
Contraindications
o
 
Hypersensitivity, Pregnancy
o
 
IF YOUR TAKING BARB,
DON’T BE DRINKING
CAN LEAD TO
 
 ADDITIVE CNS DEPRESSION
.
o
 
Barbiturates INDUCE CYP450 in the liver thus leading to
increase in liver metabolismof other drugs leading to
Reduced effect of other drugs.
 
Side effects of Barbiturates
 
 
 
Tolerance
(need to increase the dose to get some effect) &
Dependence
 
(Cant’
live without it).
 
Respiratory Distress & Withdrawal syndrome after chronic use
 
Intermitted porphyria
 
due deficiency of 
Porphobilinogen Deaminase
.
 
EFFECTS THE NUERONS
NEUROLOGICAL PAIN
HOW DO WEMANAGE, NEED TO GIVE THEM IV HEME
o
 
PT GONNA COME IN WITH BARBS AND HAVING ABD PAIN
 INTERMITTEND PORHYRIA.
 
Benzodiazepines
 
 
o
 
All the Drugs ending in ‘“
pam
”’
 
o
 
Alprazolam
 
 –
Treatment for Panic Attacks
o
 
Clonazepam
 
 –
Anticonvulsant
o
 
Diazepam
 –
Long-acting anticonvulsant (statis epileptics)
o
 
Flurazepam
 
 –
 
It’s a Prodrug with no REM suppression, Forms an Active metabolite
 
o
 
Midazolam
 
 –
Treatment for Insomnia (& IV anesthetic).
o
 
Lorazepam
 ,
Oxazepam
 ,
Temazepam
(LOT)
 
– 
Are NOT metabolized in the liver, can begiven to Alcoholics
.
 
Side Effects
 
 
 
Sedation
, Disinhibition leading to
Aggressive behavior
 
Anterograde memory amnesia (Bad with Alcohol usage)
 
Rebound withdrawal 
--
 Anxiety & Insomnia
.
Overdosing Benzodiazepines in ER
 
 
 
Give
IV Flumezanil
 
 
New Sleep Disorder Drugs
 
 
o
 
Zolpidem
, &
Zaleplon
 
o
 
These are NOT Benzos, but they do
bind to BZ1 receptors
theseinduce sleep
 
(used only for sleep).
 
Effects can be reversed by
Flumezanil 
.
 
Non-Benzodiazepine Anxiolytics
 
 
 
Buspirone
 
 –
Used to treat Generalized Anxiety disorder
 
Pts will be always worried about everything, more commonin women; symptoms must be for at least 6 months.
o
 
Does NOT affect the GABA receptors, and takes about 1 -2 weeks towork.
o
 
Possible 5HT-1a Agonist, and has NO withdrawal symptoms oraddiction.
 
 Alcohols
:
 
Ethylene Glycol
,
Methanol 
&
Ethanol 
 
All are metabolized by the enzyme
 Alcohol Dehydrogenase
.
 
Ethylene Glycol
(antifreeze)
Glycoaldehyde
Oxalic acid
 
o
 
This can lead to Toxicity
CNS Depression, Metabolic Acidosisand Renal Toxicity.
o
 
Treat with
Fomepizole
 

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