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PHARMACOTERAPY IN

NEUROLOGY

Wiwik Kusumawati
CONTENS
1. Drug used in Nausea and Vertigo (anti-
emetics)
2. Anti-epileptic drugs
3. Drug used in Parkinson

1. Drug used in Nausea and
Vertigo (anti-emetics)
Nausea and Vomiting
Drugs
Vestibular disease
Provocative movement
Migraine
Pregnancy
Nausea and Vomiting
CTZ (Chemoreceptor Triger Zone)
D2 receptor
5HT3 receptor
- BBB
Vomiting centre (lateral reticular formation of the
Medulla)
The vagus nerve
The spinal motor neurones-the abdominal muscles

Classification
Dopamine antagonist : prochlorperazine,
metoclopramide, domperidon
5HT3 antagonist : ondansetron, granisetron
Anticholinergic drugs : hyoscine
Antihistamines : cinnarizine, promethazine,
cyclizine
Drugs
Cytotoxic drugs CTZ
Metoclopramide - Dexamethazone
Ondansetron Dexamethazone
Motion sickness hyoscine, cinnarizine
Vestibular disease antihistamine,
phenothiazines
Pregnancy - promethazine
Drugs
Prochlorperazine
Phenothiazines derivate
Widely used
Less sedative
Severe distonic reaction
Drugs
Metoclopramide
Prokinetic action in the gut increase absorbtion
many drugs
Effective in migraine
Distonic reaction young and females
Domperidon
Does not pass BBB
Rarely causes sedation or extrapyramidal effect
Ondansetron lack side effect but constipation or
headache

2. Anti-epileptic drugs

Epilepsy
A chronic disease in which seizures result
from the abnormal discharge of cerebral
neurones
Partial (focal) seizures
Generalized seizures : tonic clonic (grand
mal), absences (petit mal)
Anti-epileptic drugs
Etiology
Unknown 60 70 %
Heredity
Trauma, infection, tumors, etc.
Precipitating factors
Anti-epileptic drugs
Tonic clonic and partial seizures
Carbamazepine, phenytoine and valproate
Phenoberbitone, primidone and clonazepam
Status epilepticus
A state in which fits follow each other
without consciousness being regained
Clonazepam or diazepam
Chlormethiazole
Mechanism of action
GABA
Reduction Na
+
fluxes
Inhibition spike-generating Ca
+
current
Drugs used in partial and grand
mal seizures
Single drugs is preferred
Carbamazepine and valproate are the first
line drugs
Phenytoine, phenobarbitone : liver enzyme
inducer
Carbamazepine
Is metabolized in liver
Has active metabolite anti convulsant
effect and neurotoxic (nausea, drowsiness,
headache, diplopia and ataxia)
Agranulocytosis idiosyncratic reaction
There is a linier increase in serum
concentration with dosage

Phenytoine
Is hydroxylated in the liver by saturated
enzyme system
More 20 days changing the dose ( steady
state)
The dose may be increase gradually fits
are prevented or nystagmus, ataxia,
dysarthria
A small increase in dose may produce toxic
blood levels of drug
Phenobarbitone
Is the one of metabolite active if primidone
As effective as carbamazepine or pheny
toine for tonic clonic and partial seizures
More sedative
Sudden withdrawal precipitate status
epilepticus
Side effect : cerebellar symptoms,
drowsiness and hiperkinesia
Ethosuximide
Only effective in the treatment of absences
and myoclonic seizures
Valproate
Effective in grand mal and petit mal
epilepsy
Relative lack of sedative effect
Side effect : severe or fatal hepatic toxicity
(idiosyncratic)
Benzodiazepines
clonazepame
Potent anticonvulsant, very sedative
Effective in absences, tonic clonic and
myoclonic seizures
Tolerance with prolonged oral
administration
3. Drug used in Parkinson
Parkinson
Poverty of movement, rigidity and tremor
Decreased levels of dopamine in the basal
ganglia
1/3 develop dementia
Dopamine replacement tx NO
LEVODOPA
A 58 years old woman who presents to the
neurology clinic because of stiffness on her right
side over the last 6 months. It takes her longer to
do things because it take more effort to get
movement started and her muscles feel stiff. For
the last year she feels that she does not think as
quickly and it takes her longer to remember thinks.
She also complains of constipation and decreased
libido for over a year. Recently it has become
difficult to read because the word occasionally
look blurry. These symptoms have affected her
jobs performance as a high school gym teacher
resulting in her contemplating early retirement.


Untuk kasus di atas manakah di antara
kombinasi obat berikut yang merupakan
best therapy ?
A. levodopa + carbidopa.
B. levodopa + bromocriptin.
C. levodopa + apomorphin.
D. amantadin + carbidopa.
E. amantadin + selegilin.

Parkinson
Etiology
Drugs addict pethidine MAO
Degeneration of the nigrostriatal tract
damage mitochondria and cell membrane
Neuroleptic drugs
Classification
MAO Inhibitor : selegiline
Anticholinergic drugs : benzhexol,
benztropine, orphenadrine
Dopaminergic drugs : levodopa,
amantadine, bromocriptine, lysuride,
apomorphine

Levodopa
Immediate precursor of dopamine
Able penetrate the brain
Side effects : nausea-vomiting, psychiatric
disorder, postural hypotension
Bromocriptine
A selective D2 agonist
Combination with levodopa later stages
Side effects : similar to levodopa, inhibits
release prolactine & growth hormon


Apomorphine
D1 and D2 agonist
SC injections
Advanced stages of parkinsonism
Amantadine
Has muscarinic blocking agents
Dopamine release
Modest antiparkinson effect - tolerance
MAO Inhibitor
Selegiline
Reduces metabolism of dopamine in the
brain
Potentiation with levodopa

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