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Farmakologi Obat

Gangguan Saraf
M. Bakhriansyah, H., dr., M.Kes,
M.Med.Ed
Bagian Farmakologi FK UNLAM
Banjarbaru
Status Epilepticus
► SE :
ƒ Continues seizures
occuring 30 minutes
(epilepsi foundation)
ƒ More than 30 minutes
of continues seizures
activity or 2 or more
sequential seizures
without full recovery of
consciousness between
seizures (Dodson,
1993).
► Systemicand primary brain changes Æ related to
morbidity and mortality rates
ƒ Decreasing GABA inhibition.
ƒ Increasing blood pressure (early stage) Æ decreasing
ƒ Acidosis (+)
ƒ Pulmonary edema
ƒ Hyperthermia
ƒ Mild leukocytosis
ƒ GABAergic mechanism fails
► Goal of therapy: to treat the epilepsy and to
minimalise the side effects

Principal therapy:
► Monotherapy is better than polypharmacy
► Dosage is increased until the therapeutic effect or
toxicity effect are met.
► Polypharmacy is introduced when monotherapy
does not work
► Avoiding the sudden withdrawal
Treatment flowchart for status
epilepticus
Medications
Fenitoin
Lamotrigin
Karbamazepin

Na Glutamate

STATUS EPILEPTICUS

GABA Ca

Barbiturat Fenitoin
Benzodiazepin Karbamazepin
Asam valproat Asam valproat
Gabapentin Etosuksimid
Atonik,
Parsial Petit mal Grand mal
Mioklonik
First line Karbamazepin Etosuksimid Karbamazepin Asam valproat
Fenitoin Asam valproat Fenitoin
Asam valproat Fenobarbital
Alternative Gabapentin* Klonazepam Primidon Klonazepam
Lamotrigin Asam valproat Felbamat
Primidon Lamotrigin
Fenobarbital
Parkinson disease
►A progressive
neurodegenerative
disorder associated
with loss of
dopaminergic
nigrostriatal neurons.

► Distinctive features:
ƒ Resting tremor, rigidity,
bradikinetia, and
postural instability
Principle therapy
To facilitate action of dopaminergic To suppress action of cholinergic

► Increasing the synthesis ► Blocking muscarinic/


and release of dopamine cholinergic receptor
(L-dopa+karbidopa, (trihexiphenidile,
amantadin) benzathropine,
► Inhibiting dopamin diphenhidramine)
metabolism
(selegilin/deprenil)
► Activating dopamine
receptor (bromocriptine,
pergolide)
Protocol of therapy
Anti cholinergic
Amantadine

L-dopa+karbidopa

Dopamine agonists drugs


MAO B inhibitors
L-dova (levodopa) ► On/off phenomenon
► Dopamine precursor Æ (+) after 3-5 years
inactive form application Æ
► Activated by
mechanism ???
decarboxilase enzyme; Desensitization of
dopamine receptor
ƒ Brain
ƒ Lever & kidneys Æ can ► Not a first line therapy
not pass through BBB
Æ bioavailability Å
countered by
karbidopa/benserazide.
Headache/Cephalgia
► Migraine
► Tension headache
► Cluster headache
Migraine
► Mechanism: ► NSAIDs + caffeine
ƒ Genetic (asetaminophen, acetic
ƒ Vascular salicilic acid, etc)
ƒ Neural ► Serotonin receptor
ƒ Neurotransmitter serotonin agonists (ergotamine,
ƒ Neurotransmitter dopamine dihidroergotamine,
ƒ Activation of symphatic sumatriptane,
nervous system naratriptane, rizatriptane,
zolmatriptane)
► Dopamine antagonist
(metochlopramide, CPZ,
proCPZ)
Protocol of therapy
Mild migraine NSAIDs, or
Serotonin receptor agonist (oral)

Serotonin receptor agonists (oral/nasal/SC), or


Moderate migraine
Dopamine receptor antagonist (oral)

Serotonin receptor agonists (SC/IM/IV), or


Severe migraine
Dopamine receptor antagonist (IM/IV)
NSAIDs
► SE: dispepsia

Stimulator of serotonin (5-HT1) receptors:


1. ergotamine, dihidroergotamine
► Non selective 5-HT1 receptor agonist
► Contra indication: CHD, pregnancy, peripheral
blood vessel constriction, level and kidney
disorders.
Dopamine antagonists Prevention
► Adjuvant therapy ► 3 times per month
► Increasing gut motility ► Beta blockers (propanolol,
► Also could treat: Nausea & timolol)
vomit ► Anti convulsive agents
(valproic acid)
► MAO inhibitors
(phenelzine,
isokarbosazide)
► Serotonergic agents
(metisergide,
siproheptadine)
► Ca antagonist (verapamil)
Tension headache
► Usually bilateral
► Usually following anxiety or depression
► Therapy:
ƒ NSAIDs + coffeine
ƒ Muscle relaxant agents
► Prevention: amitriptiline a.n
Cluster headache
► Periorbitalpain ► Therapy:
(temporal bone pain) ƒ Prednison
► Some signs and ƒ Lithium
symptoms related to ƒ Metisergid
eyes ƒ Ergotamine
► Mechanism: ??? May ƒ Na valproic
be serotonergic ƒ Verapamil
transmission disorder

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