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OBAT PADA SARAF

PERIFER
Dr.Muhammad Yusuf,SpS

Agonis muskarinik : Ach,Ester kolin, alkaloid

kolinergik
Antagonis Muskarinik : Atropin, skopolamin,
Obat adrenergik : Epinefrin,Dopamin
Penghambat Adrenergik: Bloker, Bloker
Muscle Relaksan: Baklofen, Tizanidin,
Esperison, Toksin botulinum
Neurotropik : Mecobalamin

Atropin
MECHANISM OF ACTION

Parasympatholytic; menghambat aksi dari


asetilkolin di daerah neuroefektor
parasimpatik post ganglion meningktakan
denyut jantung (HR) in life threatening
bradyarrhythmias.

INDICATIONS

Hemodynamically unstable Bradycardia,


Asystole, Bradycardic (<60 beats a minute)
PEA, keracunan Organophosphate ,
bronchospastic pulmonary disorders.

CONTRAINDICATIONS

Tachycardia, Hypersensitivity, unstable


cardiovascular status in acute hemorrhage
and myocardial ischemia, narrow-angle
glaucoma.

ADVERSE REACTIONS

Headache, dizziness, Palpitations, N/V,


Tachycardia, arrhythmias, anticholinergic
effects (blurred vision, dry mouth, urinary
retention), paradoxical Bradycardia when
pushed slowly or at low doses, flushed, hot,
dry skin.

DOSE/ROUTE, ADULT,

Organophosphate Poisoning Extremely large


doses (2-4mg or higher)
DOSE/ROUTE,PEDEATRIC 0.02 mg/kg IV/IO
push. May double for second dose. Minimum
single dose is 0.1 mg.
ONSET OF ACTION Immediate
PEAK EFFECTS Rapid to 1-2 minutes
DURATION OF ACTION Duration 2-6 hours

Dopamine
Dopamine --catecholamine formed by the

decarboxylation of 3,4-dihydroxyphenylalanine
(DOPA).
central nervous system, especially in the
nigrostriatal tract, and in a few peripheral
sympathetic nerves.
Dopamine menghasilkan efek chronotropic
positif dan inotropik di jantung (myocardium),
hasilnya meningkatkan denyut jantung (heart
rate) and dan kontraksi jantung (cardiac
contractility).

onset of action---- 5 menit


plasma half-life --2minutes,
the duration of action --<10 minutes
The drug is widely distributed in the body but

does not cross the blood-brain barrier to a


significant extent.
Dopamine is metabolized in the liver, kidney,
and plasma by MAO and catechol-Omethyltransferase to the inactive compounds
homovanillic acid (HVA) and 3,4dihydroxyphenylacetic acid.

Metabolism: Renal, hepatic, plasma; 75% to

inactive metabolites by monoamine oxidase


and 25% to norepinephrine
Half-life elimination: 2 minutes
Excretion: Urine (as metabolites)
Clearance: Neonates: Varies and appears to
be age related; clearance is more prolonged
with combined hepatic and renal dysfunction

Dosage
I.V. infusion (administration requires the use of an

infusion pump):
Neonates: 1-20 mcg/kg/minute continuous
infusion, titrate to desired response.
Children: 1-20 mcg/kg/minute, maximum: 50
mcg/kg/minute continuous infusion, titrate to
desired response.
Adults: 1-5 mcg/kg/minute up to 20
mcg/kg/minute, titrate to desired response
(maximum: 50 mcg/kg/minute). Infusion may be
increased by 1-4 mcg/kg/minute at 10- to 30minute intervals until optimal response is
obtained.
If dosages >20-30 mcg/kg/minute are needed, a
more direct-acting pressor may be more beneficial
(ie, epinephrine, norepinephrine).

Indications and Usage


Correction of hemodynamic imbalances

present in shock syndrome after MI, trauma,


endotoxic septicemia, open heart surgery, and
renal failure or chronic cardiac
decompensation (eg, CHF).

epinefrin
A sterile solution intended for subcutaneous

or intramuscular injection. When diluted, it


may also be administered intracardially or
intravenously. It may also be administered
intraspinally by adding to anesthetic spinal
fluid mixture. Each milliliter contains 1 mg
Adrenalin (epinephrine) as the hydrochloride

INDICATIONS
respiratory distress bronchospasme,allergic
cardiac arrest due to various causes, but it is not

used in cardiac failure or in hemorrhagic,


traumatic, or cardiogenic shock.
hemostatic agent.
mucosal congestion of hay fever, rhinitis, and
acute sinusitis; to relieve bronchial asthmatic
paroxysms; in syncope due to complete
heart block or carotid sinus hypersensitivity; for
symptomatic relief of serum sickness, urticaria,
angioneurotic edema; for resuscitation in cardiac
arrest following anesthetic accidents; in simple
(open angle) glaucoma; for relaxation of uterine
musculature and to inhibit uterine contractions.
Epinephrine injection can be utilized to prolong

DOSAGE AND ADMINISTRATION


Subcutaneously or intramuscularly

0.2 to 1 mL (mg). Start with a small dose


---For bronchial asthma and certain allergic
manifestations, e.g., angioedema, urticaria, serum
sickness, anaphylactic shock, use epinephrine
subcutaneously. For bronchial asthma in pediatric
patients, administer 0.01 mg/kg or 0.3 mg/m to a
maximum of 0.5 mg subcutaneously, repeated
every four hours if required.
For cardiac resuscitation
A dose of 0.5 mL (0.5 mg) diluted to 10 mL with
sodium chloride injection can be administered
intravenously or intracardially to restore
myocardial contractility.

Ophthalmologic use (for producing

conjunctival decongestion, to control


hemorrhage, produce mydriasis and reduce
intraocular pressure)
Use a concentration of 1:10,000 (0.1 mg/mL) to
1:1,000 (1 mg/mL).
Intraspinal use
Usual dose is 0.2 to 0.4 mL (0.2 to 0.4 mg)
added to anesthetic spinal fluid mixture (may
prolong anesthetic action by limiting absorption).
For use with local anestheticEpinephrine
1:100,000 (0.01 mg/mL) to 1:20,000 (0.05 mg/mL)
is the usual concentration employed with local
anesthetics.

SIDE EFFECTS
Transient and minor side effects of anxiety,

headache, fear, and palpitations often occur


with therapeutic doses, especially in
hyperthyroid individuals. Repeated local
injections can result in necrosis at sites of
injection from vascular constriction.

CONTRAINDICATIONS

Epinephrine is contraindicated in narrow angle


(congestive) glaucoma, shock, Epinephrine is also
contraindicated with local anesthesia of certain
areas, e.g., fingers, toes, because of the danger of
vasoconstriction producing sloughing of tissue; in
labor because it may delay the second stage; in
cardiac dilatation and coronary insufficiency.

Beta Blocker
Beta blockers may be used to treat abnormal

heart rhythms (cardiac arrhythmias) and prevent


abnormally fast heart rates (tachycardias) or
irregular heart rhythms such as premature
ventricular beats. beta blockers can be useful in
treating angina., heart attack,the treatment of
hypertension. Other uses for beta blockers include
the prevention of migraine headaches and the
treatment of certain types of tremors (familial or
hereditary essential tremors).
The beta blockers (with brand names) include:
acebutolol (Sectral), atenolol (Tenormin),
bisoprolol (Zebeta),
metoprol (Lopressor, Lopressor LA, Toprol XL),

Beta blockers, also known as beta-adrenergic

blocking agents, are drugs that block


norepinephrine and epinephrine (adrenaline) from
binding to beta receptors on nerves.
There are three types of beta receptors :
Beta-1 (1) receptors are located in the heart,
eye, and kidneys;
beta (2) receptors are found in the lungs,
gastrointestinal tract, liver, uterus, blood vessels,
and skeletal muscle; and
beta (3) receptors are located in fat cells.

Non-selective beta blockers, for example,

propranolol (Inderal), block 1 and 2 receptors


Selective beta blockers, for example, metoprolol
(Lopressor, Toprol XL) primarily block 1 receptors
and
Some beta blockers, for example, pindolol
(Visken) have intrinsic sympathomimetic activity
(ISA), can cause an increase in blood pressure and
heart rate.
Labetalol (Normodyne, Trandate) and carvedilol
(Coreg) block beta and alpha-1 receptors.
Blocking alpha receptors adds to the blood vessel
dilating effect of labetalol (Normodyne, Trandate)
and carvedilol (Coreg).

Beta blockers may cause:

diarrhea, stomach cramps, nausea, and vomiting.


Rash, blurred vision, muscle cramps, and fatigue
may also occur.
they slow heart rate, reduce blood pressure, and
may cause heart failure or heart block in patients
with heart problems.
Central nervous system effects of beta blockers
include:
headache, depression, confusion, dizziness,
nightmares, and
hallucinations.
Beta blockers that block 2 receptors may cause
shortness of breath in asthmatics.

Diazepam (Valium)
Mechanism of action: enhance GABA

activity
Clinical effects: decreased resistance to
passive ROM; decreased hyperreflexia;
reduced painful spasms; sedation; reduced
anxiety
Dose: initial 2 mg/day, gradually increase
to maximum 60 mg/day

Diazepam (Valium)
contd
Pediatric dosing: 0.12-0.8 mg/kg/day
Adverse effects: sedation, weakness,

hypotension, memory impairment, ataxia,


confusion, depression
Chronic effects: dependency, withdrawal,
and tolerance possible
Routes of administration: oral,
intravenous, rectal

Baclofen (Lioresal)
Mechanism of action: GABAB agonist
Clinical effects: decreased resistance to

passive ROM, decreased hyperreflexia;


reduced painful spasms; reduced anxiety
Dose: orally 5 mg three times daily, gradually
increase to 20 mg four times daily or higher;
intrathecally initially 50 mcg/day increase to
300-800 mcg/day

Baclofen (Lioresal) contd


Pediatric doses: oral doses not well

established; intrathecal doses 25 mcg/day


initially increase to 274 mcg/day as tolerated
Adverse effects: weakness, sedation,
hypotonia, ataxia, confusion, fatigue,
nausea, liver toxicity
Chronic effects: rapid withdrawal may
cause seizures, confusion, increased
spasticity
Route of administration: oral, intrathecal

Dantrolene sodium
(Dantrium)
Mechanism of action: reduces calcium

release from sarcoplasmic reticulum,


uncouples excitation and contraction of
skeletal muscle
Clinical effects: decreased resistance to
passive ROM, decreased hyperreflexia and
muscle tone, reduced spasms and clonus
Dose: 25 mg twice daily, gradually increase
to 100-200 mg/day, maximum dose 400
mg/day

Dantrolene sodium
(Dantrium) contd
Pediatric doses (age > 5 yrs): 0.5 mg/kg

twice daily, increase by 0.5 mg/kg/day every


week to response
Adverse effects: weakness, drowsiness,
lethargy, nausea, diarrhea
Chronic effects: liver toxicity with dosing
near maximum and in women >50 yrs
Route of administration: oral,
intravenous

Tizanidine (Zanaflex)
Clonidine (Catapres)
Mechanism of action: alpha-2 receptor

agonist
Clinical effects: reduced tone, spasm
frequency, and hyperreflexia
Doses: tizanidine initial 4 mg three times
daily increase to 36 mg/day; clonidine initial
0.1 mg twice daily increase to 2.4 mg/day

Tizanidine (Zanaflex)
Clonidine (Catapres)
Pediatric dose: tizanidine dose not

established; clonidine initial 5-10


mcg/kg/day increase gradually to response
Adverse effects: drowsiness, dizziness, dry
mouth, orthostatic hypotension
Chronic effects: rebound hypertension
with rapid withdrawal
Route of administration: oral,
transdermal patch (Clonidine)

Other Drugs for


Spasticity
Cyproheptadine (Periactin): limited

experience
Cannabinoids (Marinol, Cesamet): work in
multiple sclerosis; limited information on
other uses
Orphenadrine (Norflex): short acting
Gabapentin (Neurontin): possibly helpful in
spinal cord injury or multiple sclerosis

Botulinum Toxin (Botox,


Myobloc)
Enters the pre-synaptic terminal and binds

to acetylcholine
Inhibits acetlycholine from entering the
synaptic cleft
Toxin serves as a block at the
neuromuscular unction
Can be administered to a specific muscle
or group via local injection

Botox
Used in tx of pts with focal dystonia as found

in CVA; CP; TBA;Spinal Cord Lesions


Used to restore volitional motor control thus
increasing use of extremities and improving
function, mobility and opportunities to
participate in meaningful occupations
Prevention of joint contraction and fixation

Adverse Effects
Tx limited to a few muscles due to potential

for toxic effects


Effects of tx are temporary (3-6 months)

Eperisone

Eperisone hydrochloride
antispasmodic drug,
relaxing both skeletal muscles and vascular

smooth muscles, and demonstrates a variety of


effects such as reduction of myotonia,
improvement of circulation, and suppression of
the pain reflex.

Indications

Spastic paralysis ,improvement of muscular


hypertonic symptoms in conditions such as
cervical syndrome, periarthritis of the
shoulder, lumbago.

Dosage and administration

In adults, the usual dose of eperisone is 50150 mg per day, in divided doses after meals.

Contraindications

hypersensitivity to the drug.


Cautions
history of hypersensitivity to any medication,
or with disorders of liver function
Weakness, light-headedness, sleepiness or
other symptoms may occur.

Side effects

Shock and Anaphylactic reactions: In the


event of symptoms such as redness,
itching, urticaria, oedema of the face and
other parts of the body, dyspnoea etc,
Oculo-muco-cutaneous syndrome (Stevens
Johnson Syndrome) and Toxic Epidermal
Necrolysis: Serious dermatopathy such as
oculo-muco-cutaneous syndrome (StevensJohnson syndrome) or toxic epidermal
necrolysis may occur. , anaemia, rash,
pruritus, sleepiness, insomnia, headache,
nausea ang vomiting, anorexia, abdominal
pain, diarrhoea, constipation, urinary
retention or incontinence.

Mecobalamin
Indication & Dosage Oral

Peripheral neuropathies
Adult: 1500 mcg/day in 3 divided doses.
Parenteral
Peripheral neuropathies
Adult: 500 mcg daily IM/IV 3 times/wk.
Parenteral
Megaloblastic anaemia caused by vitamin
B12 deficiency
Adult: 500 mcg daily IM/IV 3 times/wk.
Maintenance dose: After about 2 mth of therapy,
reduce dose to single admin of 500 mcg every 1-3
mth.

Adverse Drug Reactions Oral: Anorexia,

nausea, vomiting and diarrhoea. Parenteral:


Rash, headache, hot sensation, diaphoresis
and pain/induration at IM inj site.
Potentially Fatal: Anaphylactoid reactions
(parenteral).

Mechanisme of action
Mecobalamin is the neurologically active

form of vitamin B12 , a water-soluble


vitamin in the body. It is a cofactor in the
enzyme methionine synthase, which
functions to transfer methyl groups for the
regeneration of methionine from
homocysteine. In anaemia, it increases
erythrocyte production by promoting
nucleic acid synthesis in the bone marrow
and by promoting maturation and division
of erythrocytes.

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