Local anesthesia or local pain substance is a drug on the local use of a reversible obstructive channeling of nerve impulses to the CNS and thereby eliminate or reduce pain, itching - itching, hot or cold. Many other compounds also have the power of such work, but the effect is not reversible and causes permanent damage to nerve cells.
The first local anesthetic was cocaine, an alkaloid obtained from the leaves of a plant reeds in the Andes (Peru).
The first local anesthetic was cocaine, an alkaloid obtained from the leaves of a plant reeds in the Andes (Peru).
REQUIREMENTS
There are several criteria that must be met for a type of drug used as a local anastetikum, among others:
1. Not stimulate tissue
2. Does not cause permanent damage to the nervous system
3. Low systemic toxicity
4. Effective with the road or the use of local injection of the membrane lender
5. Starting work as short as possible, but survived long enough
6. Soluble in water and produce a stable solution, there are also sterilization
2. Does not cause permanent damage to the nervous system
3. Low systemic toxicity
4. Effective with the road or the use of local injection of the membrane lender
5. Starting work as short as possible, but survived long enough
6. Soluble in water and produce a stable solution, there are also sterilization
Classification of local anesthetics
The basic structure of local anstetika generally consist of three parts, namely a hydrophilic-amino group (secondary or tertiary) which is connected by an ester bond (alcohol) or amide with an aromatic group-lipofil. The longer the alcohol group, the greater their power anastetiknya, but also increases toxicity.
Anastetika local chemical can be classified into several groups as follows:
Anastetika local chemical can be classified into several groups as follows:
a. -Ester compound: cocaine and ester-PABA (benzocaine, procaine, oksibuprokain, tetrakain)
b. -Amide compounds: lidocaine and prilokain, mepivakain, bupivacaine, and cinchokain
c. Other: phenol, benzialkohol and etilklorida
All of the above drugs except cocaine is sintetris natural.
b. -Amide compounds: lidocaine and prilokain, mepivakain, bupivacaine, and cinchokain
c. Other: phenol, benzialkohol and etilklorida
All of the above drugs except cocaine is sintetris natural.
It works
Anatetika local flavor with a resulting loss of road some way. For example, by way of temporarily avoiding the formation and transmission of nerve impulses through cell edges. Central mechanism of action is located in the cell membrane. As well as alcohol and barbital, anastetika local forwarding inhibit impulses by way of reducing nerve cell membrane permeability to ions-sodium, which is necessary for proper nerve function. This was due to competition with calcium ions, which are adjacent to the sodium channels in the membrane of neurons. At the same time, due to the decline rate of depolarization, the threshold of sensitivity to electrical stimulation gradually increased, so that finally happened losing the local flavor is reversible.
SECURITIES - OTHER SECURITIES
In addition to the efficacy of local anastetika anatetikanya still has a number of other effects, al disrupt the function of all organs where there is conduction / transmission of multiple impulses.
1. Pressing SSP
2. Pressing the cardiovascular system
3. Vasodilatation
2. Pressing the cardiovascular system
3. Vasodilatation
FAMAKOKINETIK
Resorpsinya of skin and mucus membranes can take place very quickly and well, for example on cocaine, lidocaine, and tetrakain prilokain. Any progress with the rapid distribution to all organs and tissues. Conversely, procaine resorption in bad skin, so it is not useful in local stocks. The speed and duration of labor power is determined by lipofilitas, pKa, degree of binding to proteins and the degree vasodilatasinya.
The structure of local anestetika drug has a direct effect on the therapeutic effect. Everything has a hydrophobic group (an aromatic) related through an alkyl chain to the relatively hydrophilic group (tertiary amine).
Local anestetika onset speed is determined by:
a. drug levels and their potentialLocal anestetika onset speed is determined by:
b. the number of drug binding by proteins and binding of drugs to the local network
c. speed metabolism
d. drug injection site tissue perfusion.
Giving vasoconstrictor (epinephrine) + local anestetika to reduce local blood flow and reduce systemic absorption. Vasoconstrictor should not be used in areas with little collateral circulation and on the fingers or toes and penis. Group ester (procaine, tetrakain) hydrolyzed rapidly into inactive products by plasma cholinesterase and liver esterase. Bupivacaine extensively bound to plasma proteins.
Pharmacodynamic
Onset, intensity, and duration of nerve blockade is determined by the size and anatomical location of nerve. Na + channel is important in muscle cells that can be excited like heart. The effect of cardiac Na + channels is the basis of local anestetika therapy in the treatment of certain arrhythmias (usually used lidocaine). Local Anestetika generally less effective in infected tissue than normal tissue, usually because of local infection resulting in metabolic acidosis, and lower the pH.
SIDE EFFECTS
The side effects are a result of the effect of depression on the CNS and the effects of cardio-depresifnya (suppressing the function of the heart) with symptoms of inhibition of respiration and blood circulation. Local Anastetika can also lead to reactions that often form hipersensitasi exantema, urticaria, and allergic until sometimes bronchopasme anafilaktis shock which can be deadly. Famous in this regard is the ester group substances and tetrakain procaine, which therefore is not used anymore in local stocks. Hipersensitasi reaction was caused by PABA (para-amino-benzoic acid) is formed through hydrolysis. This can negate the effects of PABA antibakteril of sulfonamides, which based on competitive antagonism by PABA, therefore, therapy with a sulfa should not be combined with the use of these esters.
USE
A. By Parenatal
Local Anastetika seering times used in surgery for which general anesthesia is not necessary or desirable. Type of local anatesia the most widely used as an injection is as follows:
• Infiltration anesthesia• Conduction anesthesia
• Spinal anesthesia (intrathecal)
• epidural anesthesia
• Surface Anatesia
B. How to use other oral
Local Anastetika used as a solution to pain in the mouth or suction tablets (sore throat) are also in the form of eye-drops to measure the intraocular pressure or remove foreign objects, as well as ointments for itching or pain in burns and anti-pill-drop hemorrhoids.
Ester compounds often cause allergic skin reactions, then you should dugunakan-amide, a compound which is more rarely result in hipersensitasi.
Ester compounds often cause allergic skin reactions, then you should dugunakan-amide, a compound which is more rarely result in hipersensitasi.
SUBSTANCE - PARENT SUBSTANCE
A. ESTER COMPOUNDS
• Cocaine: benzoylmetilekgonin
• benzocaine: anestesin, etilaminoobenzoat, * benzomid, * Rako.
• procaine: novocaine, etokain, * gerovital (drAslan)
• Lidocaine: lignokain, xylocaine, * EMLA
• Mepivakain: scandicaine, * estradurin
B. Amide COMPOUNDS
• Cinchokain: dibukain, * proctosedyl, * scheriproct
• Artikain: carticaine, * ultracain
C. OTHER
• Etilklorida: kloretan, kloretil
• Phenol: carbolic acid, acidum carbolicum, * calamine lotion
• Benzialkohol
• Artikain: carticaine, * ultracain
C. OTHER
• Etilklorida: kloretan, kloretil
• Phenol: carbolic acid, acidum carbolicum, * calamine lotion
• Benzialkohol
GENERAL Anaesthetics
Anastetika common are drugs that can cause anesthesia or narkosa (Yunan = no, aesthesis = feeling), which is a state of general depression of the central pelpagai in the CNS that is reversible, in which all feelings and consciousness are done, so a bit like a fainting fit.
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