PHARMACOTERAPY IN

NEUROLOGY
Wiwik Kusumawati

CONTENS
1. Drug used in Nausea and Vertigo (antiemetics)
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

 Steven is a recently qualified civil engineer who

has epilepsy. He has applied for a post as a project
worker. Because of the hazards presented while
working near moving plant machinery or at
heights, the recruitment standards for the post
adopted by the company excludes employment of
applicants with epilepsy. When this policy was
challenged by the Human Resources manager, the
companys health and safety officer confirmed that
the vacant job was likely to involve work at height
and around hazardous machinery and that it would
not be safe for someone with epilepsy to work in
that environment.

 Sally developed epilepsy after a prolonged febrile convulsion

damaged her brain at the age of 15 months. She was admitted
to hospital and treated according to local protocols.
Later in life, she underachieved both at school and in the
workplace. As a child she was under the care of a
paediatrician. Because her seizures were not controlled, the
paediatrician prescribed a change in drugs that resulted in an
increase in seizures while Sally was studying for her GCSEs.
After this and until she was a young adult, she was seen by a
psychiatrist.
The branch manager of the bank where Sally first worked
found her epilepsy a problem. He pressurised her to stop the
seizures occurring at work. The more pressure, the more
seizures Sally had. She became trapped in such a vicious
circle that there was nothing she could do
but resign.

 She eventually found another job, but the

extra travelling left her very tired and this in
turn increased the seizures. One afternoon,
waiting for a train home, she wandered off
the station platform and onto the line during
a complex partial seizure.
Later, when Sally became pregnant she
asked her GP about the possible risks to her
unborn child. She was told that the epilepsy
medication would already have damaged her
baby. Both Sally and her husband worried
throughout the pregnancy about the baby.

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

 A 69-year-old man presents with a 1-year history of

mild slowness and loss of dexterity. His handwriting
has become smaller, and his wife feels his face is less
expressive and his voice softer. Over the last few
months he has developed a subtle tremor in the right
hand, noted while watching television. His symptoms
developed insidiously but have mildly progressed. He
has no other medical history, but he has noted some
mild depression and constipation over the last 2 years.
His examination demonstrates hypophonia, masked
facies, decreased blink rate, micrographia, and mild
right-sided bradykinesia and rigidity. An intermittent
right upper extremity resting tremor is noted while he
is walking. The rest of his examination and a brain
MRI are normal.

 Mr H. is a 30 year old man who has recently

been diagnosed with early Parkinsons disease.
He has been quite upset and depressed about the
diagnosis and has lost interest in his usual
activities and hobbies. His wife reports that his
tremors and involuntary movements have
worsened. He has been taking the following
medications for 6 months: levodopa(2 g/day) and
sertraline (Zoloft). He now has Cogentin added
to his medications.

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

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