Kuliah Anti Parkinson 2009 (English, 2009)

7/27/2019 Kuliah Anti Parkinson 2009 (English, 2009)

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DRUG TREATMENT

PARKINSONS DISEASE

Dr. H. Syahril Aziz, DAFK, Sp.FK, M.Kes.Departement of Pharmacology

Medical Faculty

Sriwijaya University


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Definition

1. Tremor is regular occilative movement andregulararound joint and has special character accordingtoits related activities

2. Chorea is muscle attraction which cannot bedetermined, and irregular that can occur atvariouspart of the body that can disturb general musclemovement.


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3. Athetosis is abnormal movement, slow, and

writhe and it sometimes can remain.4. Ticss is abnormal movement that is regular, andin sudden, tend to return mainly around face and

head and it mostly occur to children.5. Parkinsons is a condition marked by combinationbetween stiff, bradykinesia, tremor, and

instability of postural that can happen in variouscauses, generally it is idiophatic.


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5. Dopamine is derivat catechol aminproduced by gland of adreno medula.Originated from derivat phenylala-nine --- > tyrosine --- > DOPA and Dopaminethrough the process of reaction ofhydroxy lasi and decarboxylasi.katabolisme through the process ofoxidasi ( mono amine oxidase : MAO) orthrough process metilasi ( cathechol-O-methyl transferase COMT ).


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PATOFISIOLOGI

Parkinson happened because of the loweramount of Dopamine in nerve of dopaminergicat Nigra substantia where this dopamin works bypursuing excretion of cells of GABAERGIC instriatum corpus

Drugs can produce Parkinson syndrome is drugwith the character of dopamin receptor

antagonis such as drug of antipsikotik or theoccurance of nerve of nigrostriatal dopaminergiksuch as MPTP ( tetra phenyl methyl hidro-pyridine


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ANTI PARKINSONS DRUGS

1. LEVO DOPA

2. AGONIS DOPAMIN

3. BROMOCRIPTIN

4. PERGOLID

5. MONO AMIN OKSIDASE INHIBITOR

6. KATEKOL-O-METIL- TRANSFERASE INHIBITOR

7. AMANTADIN

8. DRUGS RESISTOR OF ACETYL CHOLINE

9. DIHIDROKSI PHENYL SERINE ( DOPS )


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1. LEVO DOPA

PHARMACOKINETIC

It is easy absorbed through small intestine

especially in empty stomach.

The peak amount is reached 1-2 hour after the

giving.

Duration is 1-3 hours.

Excretion is through urine

1-3 % in the form of intact can enter into the brain

while the rest is metabolized out of brain so that

the giving must be in high dose except when it is

combined with resistor of dekarboksilase dopa


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Clinical Usage It is generally given in the form of combination with

Carbidopa. Levodopa can improve all clinical form

of of Parkinson especially eliminating bradikinesia

In the initial medication 1 / 3 showed good result, 2 /

3 did not show good result and the rest did not show

response at all


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Side Effects

Gastro Intestinal : anorexia, nausea, vomitus.

Cardiovascular : heart disrithmia, tachycardia,

extra systole, ventricular fibrilasi, hypotensi.

Diskinesia.

Behaviour : depression, anxietas, agitation,

insomnia, somnolent, confuse, hallucination,nightmare, euphoria, change of personality


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5. Others : mydriasis, glaucoma, trouble of smell,

urine spit and brown vagina liquid

If there are heavy side effects, DRUGHOLIDAY (the stopping of drug temporarily

until the signs of side effects disappear) must

be done.


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Interaction of Drugs

1. Pyridoxin improve extra metabolism of

levodopa cerebral so that it can reduce its

therapy effect

2. It can not be given together with resistor of

MAO in 2 weeks after drug is discontinued

because it can cause hypertension crisis.


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Contra Indication

1. Don't give it to patient of Psychotic

because can stimulate mental disorder

2. The closed angle Glaukoma.

3. Ulcus Pepticum can occur melena

4. Melanoma


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2. AGONIST DOPAMIN

Some dopamin agonist that have the effect of

anti parkinson such as apomorfin, pyribedil,

lergotril have not been used anymore because

of its heavy side effects


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3. BROMOCRYPTINE

Some generation of ergot is dopaminpartial agonist.

It can be used to depress milk production.

`It is absorbed through GI Tract., the peakamount is 1-2 hour after oral giving,

excretion is through bile dilution and

faeces.

It is the first choice in therapy of parkinsons

disease.


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In everyday practice, medication of

dopaminergik to Parkinson always startedwith combination of carbidova with

levodopa, then followed by the combination

of bromocriptine. Bromocriptine is not generally interacted

with other drugs


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CLINICAL USAGE

1. The giving is always started with small dose

and can be increased little by little. It Is

generally started with dose 7,530 mg /

day2. Can cause hypotensi

3. Medication must be discontinued if there is

trouble of psychiatric, heart dysrithmia,ergotisme or side effects that are difficult to

tolerate


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SIDE EFFECTS

Gastrointestinal : anorexia, nausea, vomiting,constipation, dyspepsia, refluks esophagitis,hematemesis.

Cardiovaskular : hypotensi, finger vasospasme,

dysrithmia. Dyskinesia : abnormal movement trouble

If its happen, drug dose has to be decreased

Mental disorder : confusion, delusion,

hallucination.

Others : headache, nasal congestive, difficult ofsleep, infiltrat lungs, erythromeralgia ( redfoot/feet, painful and swollen joint, artralgia)


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CONTRA INDICATION

History of Psychotic.

Cardiovaskular : myocard infark, Raynauld

and Buerger disease.

Patient with hystory of peptic ulcer.


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4. PERGOLIT

It is agonist dopamin

It is often combined with levodopa

It is generally tolerated very well

Average dose is 3 mg / day

It can be combined with levodopa.


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5. MONO AMIN OKSIDASE INHIBITOR

( MAO INHIBITOR )

There are 2 kinds of MAO

MAO A : metabolism of norepinephrine and of

serotonin. MAO B : metabolism of dopamine.

MAO B selective resistor of MAO which

will slow down resolving of dopamin and alsoimproving and lengthening effect of levo dopa


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This drug is used in the form of

combination with dopa levo to overcome

the decreasing of response of dopa levo

The important point is to pay attention on

side effects of hypertension because of

accumulation and release epinephrine in

blood.

Standard dose is 2 x 5 mg after breakfastand lunch


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6. KATEKOL AMIN O TRANSFERASE

INHIBITOR.

This Drug is rarely used in medication of

Parkinson except as addition in the form of

combination


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7. AMANTADIN

It is anti viral drugs which coincidencely

have effect of anti parkinson.

It is unknown clearly Its function as anti

parkinson and anticipated can improve thefunction of Dopaminergic by influencing

sintesa not only excretion but also removal

of dopamin


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Farmakokinetik

The peak level concentration is 1-4 hours after oral giving

duration is 214 hours

Excretion through urine mostly in intact form

Clinical Usage

Less effective compared to levodopa

however can be used to overcome

bradykinesia, rigiditas and tremor parkinson.

Standard dose : 2 x 100 mg / day

Sid ff


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Side effects

1. Central Nerve System : headache, anxiety,depression, iritability, insomnia, agitation,

excitation, hallucination, confusion. Big dose can

cause acute toxic psychosis and convultion.

2. Skin : peripheral oedem.

3. Cardiovaskular : Decompensatio Cordis, postural

hypotensi.

4. GI Tract : anorexia, nausea, dry mouth.

5. Urine retention


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Contra indication

1. Contraindicated at patient with heart

failure

2. Patient with spastic history and epilepsy


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8. DRUG RESISTOR OF ACETYL

CHOLINE

Drug resistor of acetylcholine : antimuscarinic

can be used as anti parkinson because it isdopaminergik

Clinical UsageIt can be used to cure tremor and rigiditasParkinson but it can cause bradycardiaalthoughit is small


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Side effects

Central Nerve System : sleepy, mental disorder,lack of attention,anxiety, confusion, agitation,

delusion, hallucination, change of way of thinking.

GI Tract. : queasy, vomiting, constipation

Heart : takikardia, palpitasi, dysrithmia.

Respiration : tachypneu.

Eye : the increase of pressure of intra okuler,

mydriasis, blurry eyesight

Side effects is tentative and it will lose after drug

is discontinued


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Contra Indication

Prostate Hypertrophy

Gastrointestinal Obstructif for example

stenosis pyloric and ileus obstrukctive.

Close Angle glaucoma.

Don't give it at the same time with anti

histamin and trisiclic anti depressant.


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9. DIHIDROKSI FENIL SERIN ( DOPS )

Lack of norepinephrine in brain to thepatient with parkinson supports the theory

that the patient lacking of dopamin will also

cause lacking of epinefrin The giving of DOPS as norepinefrin

precursor is reported can improve

phenomenon at some cases. This drug is rarely used


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PARKINSON BECAUSE OF DRUG

Drug that can cause Parkinson

Reserpin and Tetrabenazin.

This Drug will remove mono amin biogenik

out of its placebo so that the amount of

dopamin in blood will be decreased

Phenotiazine and haloperidol.

This drug will pursue dopamin reseptor so

that dopamin doesn't have catch point at

target organ.


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Other drugs which is often used to help to

slow down the growth of parkinson's disease

for example : Vitamin E : however still in debate

Neurotropik Vitamin : to give good response

to nerve cell Pyracetam : to help cell of glia nerve gets

better


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GROUP I : OBAT ANESTETIK GAS

DAN ANESTETIK INTRA-

VENA

GROUP II : OBAT ANESTETIK

VOLATIL.

GROUP III : OBAT ANTI KONVULSI

GENERASI KE DUA.

GROUP IV : OBAT-OBAT PRE ANES-

TESI MEDIKASI.


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GROUP V : FENITOIN, FENOBAR-

BITAL DAN KARBAMAZEPIN.GROUP VI : SUKSINIMID, ASAM

VALPROAT, BENZODIAZEPIN

GROUP :ASAM VALPROAT,ASETIL UREA DAN KARBONIK

ANHIDRASE

GROUP VIII : THE APPLICATION OF THETREATMENT OF OTHERDISTURBANCE OF MOVEMENT .

Kuliah Anti Parkinson 2009 (English, 2009)

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