Definition: drugs which inhibit the delivery of nerve reversible when applied locally scr pd jar adequate levels of nerve dgWork on each part of the nervous system which intervened
First drug: cocaine, Erythroxylon coca leaf alkaloids
Nature:- Not irritating & non-permanent damage to jar the nerves scr- At a brief work, long working period- Wide safety margin- Water Soluble- Stable in solution- Can be sterilized without changing its
Classification
The basic structure of local anesthetics in general consists of three parts, namely a hydrophilic amino group linked by an ester bond (alcohol) or amide with an aromatic group lipofil. The longer the alcohol group, the greater their power anestetiknya, but also increases toxicity.Local anesthesia can be chemically classified into several groups as follows:
a. Ester compound: cocaine and PABA ester (benzocaine, procaine, oksibuprokain, tetrakain)
b. Amide compounds: lidocaine and prilokain, mepivakain, bupivacaine, and cinchokain
c. Others: phenol, benzialkohol and ethyl chloride.
Mechanism of action
* Prevent the occurrence of nerve impulse conduction and
* Place of work mainly in cell membranes
* Inhibition of Na + ion membrane permeability due to membrane depolarization increased excitatory threshold makes
* Excitability <<& smoothness constraints hampered
* Binds to receptors dg yg pd tdpt Na ion channels, the blockade so that the inhibition occurs via membrane ion motion
Pharmacokinetics
1. Resorpsinya of skin and mucus membranes can take place very quickly and well, for example on cocaine, lidocaine, prilokain, and tetrakain. Distribusinyapun progress rapidly to all organs and tissues. Conversely, procaine resorption in kult bad. The speed and duration of labor power is determined by lipofilitas, pKa, degree of binding to proteins and the degree vasodilatasinya.
First drug: cocaine, Erythroxylon coca leaf alkaloids
Nature:- Not irritating & non-permanent damage to jar the nerves scr- At a brief work, long working period- Wide safety margin- Water Soluble- Stable in solution- Can be sterilized without changing its
Classification
The basic structure of local anesthetics in general consists of three parts, namely a hydrophilic amino group linked by an ester bond (alcohol) or amide with an aromatic group lipofil. The longer the alcohol group, the greater their power anestetiknya, but also increases toxicity.Local anesthesia can be chemically classified into several groups as follows:
a. Ester compound: cocaine and PABA ester (benzocaine, procaine, oksibuprokain, tetrakain)
b. Amide compounds: lidocaine and prilokain, mepivakain, bupivacaine, and cinchokain
c. Others: phenol, benzialkohol and ethyl chloride.
Mechanism of action
* Prevent the occurrence of nerve impulse conduction and
* Place of work mainly in cell membranes
* Inhibition of Na + ion membrane permeability due to membrane depolarization increased excitatory threshold makes
* Excitability <<& smoothness constraints hampered
* Binds to receptors dg yg pd tdpt Na ion channels, the blockade so that the inhibition occurs via membrane ion motion
Pharmacokinetics
1. Resorpsinya of skin and mucus membranes can take place very quickly and well, for example on cocaine, lidocaine, prilokain, and tetrakain. Distribusinyapun progress rapidly to all organs and tissues. Conversely, procaine resorption in kult bad. The speed and duration of labor power is determined by lipofilitas, pKa, degree of binding to proteins and the degree vasodilatasinya.
2. Need to avoid the use of local anesthesia in patients with liver damage.
3. Toxicity of local anesthetic depends on the balance between resorption rate and speed of degradation. The speed of resorption and also its toxicity can be minimized by giving vasoconstrictor. Another advantage of vasoconstrictor is renewed labor power and reduced blood loss in the surgical wound. Vasoconstrictor that is used is epineprin and norepineprin.
4. The combination of norepineprin epineprin and should not be used on certain body parts (finger hand / foot, nose, ears, penis) because of the likelihood of ischemia and gangrena (tissue death).
Pharmacodynamic
1. In SSPdapat stimulate CNS became agitated and tremor and clonic convulsions and depression and lead to death (paralysis breath
2. In muscle and ganglion nerve connections can influence the transmission at the neuromuscular connection is reduced muscle response on nerve stimulation
3. In the cardiovascular system: myocardial caused the decrease in excitability, Kec conduction & contraction strength (high KDR Dlm plasma); arteriolar vasodilatation
4. Pd smooth muscle: Unresponsive spasmolytic berhub dg anesthetic effect
5. Onset, intensity, and duration of nerve blockade is determined by the size and anatomical location of nerve.
6. Na + channel is important in muscle cells that can be excited like heart. The effect of cardiac Na + channels is the basis of local anesthetic therapy in the treatment of certain aritmi.
7. Local anesthesia is generally less effective in infected tissue than normal tissue, usually because of local infection resulting in metabolic acidosis
Profile of drug
1. Procaine
a. Pharmacodynamic
* Dose 100-800 mg: mild analgesic, 10-20 max effect ', missing timeout 60'
* Dhidrolisis mjd PABA (para amino benzoic acid) to inhibition of sulfonamide
b. PharmacokineticEsterase
* Absorption fast PABA + dietilaminoetanolHydrolysis* PABA excreted urine Dlm (Btk intact and conjugated)
c. Indication
* Infiltration anesthesia, nerve blocks, epidural, caudal and spinal
* Geriatric: improve sexual activity & FGS kel endocrine (conflicted)
d. Preparations
* 1-2% procaine hydrochloride is an anesthetic infiltrates, 5-20%; spinal anesthesia
2. Lidocaine
a. Pharmacodynamic
* Local anesthesia strong. Tjd faster, stronger LBH, LBH LBH long & extensive procaine dp
* Lar 0.5% lidocaine is an anesthetic infiltrates, 1-2%; block and topical anesthesia
* Effective when without a vasoconstrictor, Kec absorption & tox, years of LBH short
b. Pharmacokinetic
* Easily absorbed dr tmpt injection
* It can penetrate the blood brain barrier
* Metab: liver; ex: urine
c. Indication
* Injection: infiltration anesthesia, nerve blocks, epidural anest, anest caudal, anest mucosa
* Anest infiltrates: 0.25 to 0.50% dg lar or without adrenaline
* Vizard teeth: lar Lido 1-2% adrenaline dg
* Anest surface, anest corneas (lidocaine 2% + adrenaline)
* Reduces heart irritability
3. Dibukain
* Local Anest strong PLG, PLG toxic, long working period
* 15x LBH strong & toxic dg LBH 3x long period of procaine dp
* KDR 0.05 to 0.1%: anest injection; anest urethra from 0.05 to 0.2%; anest spinal: 7.5 to 10 mg
4. Mepivakain HCl
* Similar to lidocaine
* Anest infiltra, regional nerve blockade, spinal anest
* Dosage: Injection is a solution of 1%, 1.5%, 2%
5. Piperakain HCl
* I.v: toks 3x procaine
* Strength anest = procaine
* Use topical: 2% lar to the cornea, 4% for eye ointment; nerve blockade: lar 0.5-1%
6. Tetrakain
* PABA derivatives
* It is a local anesthetic that penetrates the cornea and conjunctiva, the drug is effective after topical administration to the eyes in 30 sec and anesthesia lasted for min. 15 min
* I.v = active & LBH LBH 10x toxic procaine dp
* Dosage and administration: in the eyes of 1 or 2 drops of a solution of 0.5%; ENT: lar 2%
* Contraindications: known the hipersensitiv against tetrakain, ocular inflammation or infection
* Precautions: teranestesi eyes must be protected from dust and bacteriological contamination samapai sensation of a full recovery. Use the old can cause opacity of the cornea
* Adverse effects: local burning feeling can arise and, more rarely is lakrimasi and photophobia
* Storage: Tetrakain eye drops should be stored in tightly closed containers protected from light and do not cooled
7. Prilokain HCL
* Securities fkologi lidocaine mrp
* At & long working long LBH lidocaine dp
* Dosage: KDR 1,2,3%
8. Bupivacaine
This substance inhibits the initiation and transmission of nerve impul in place to stabilize the membrane of nerve. This compound is metabolized in the liver. Anesthesia and usually work for 2-4 hours
Usefulness
* Anesthesia infiltration
* Block of peripheral nerve and sympathetic
* Dental Anesthesia
* Spinal Anesthesia
* Epidural and caudal anesthesia
* Bupivacaine is not suitable for intravenous regional anesthesia or the use of topical
Contraindications
* Skin infections are adjacent to the injection site or any abnormal bleeding tendency
* Severe anemia
* Heart disease
* Local and epidural anesthesia was not performed in patients with dehydration and hypovolemia
* High levels of bupivacaine in the blood should be avoided in patients with hepatic disorders
Side effects
* The side effects are a result of the depressant effects on CNS and cardio-depresifnya effect (suppressing the function of the heart) with symptoms of inhibition of respiration and blood circulation. Local Anestetika can also cause a reaction that is often a exantema hipersensitasi, urticaria and allergic until sometimes shock bronchospasme anafilaktis which can be deadly. The famous dal; am this are substances procaine and tetrakain ester groups, which therefore is not used anymore in local stocks. Hipersensitasi reaction was caused by PABA (para amino benzoic acid), which is formed through hydrolysis. PABA can negate the effects of sulfonamide antibakteriil. Therefore, therapy with a sulfa should not be combined with the use of these esters.
* CNS effects: depression, stimulation, depending on the neural pathways affected by local anesthesia
* Overdose of local anesthetics can cause:
* Decrease the transmission of impulses in neuromuscular junctions and synapses ganglion
* Causes muscle weakness and paralysis
Provision of Local Anesthesia Techniques
1. Surface anesthesia
2. Infiltration anesthesia
3. Block anesthesia
* Spinal Anesthesia
* Epidurals
* Anesthesia caudal
Use
1. In parenteral local anesthetic often used in surgery.
Type of local anesthesia of the most widely used as an injection is as follows:
a. Infiltration anesthesiaSome injections are given at or around a network that will dianestetisir, resulting in loss of sensation in the skin and the tissue that lies deeper, for example in the practice of ENT (Ear, Nose, Throat) or gum (in a tooth extraction).
b. Conduction anesthesia (peripheral nerve block ade), the injection in the spine at a gathering place for many nerves, especially on the operating arm or leg, and shoulder. It is also used to block the intense pain.
c. Spinal anesthesia (intrathecal), also called the dorsal injection. Drugs injected in the spine that contains cerebrospinal fluid. Thus injection across the outer membranes of the medulla (duramater), usually between the lumbar vertebra to the third and fourth. Thus, anesthesia of the foot / lower body to the breastbone can be reached within a few minutes.
d. Epidurals also ternasuk back injection. Drugs injected in the epidural space, the space between the outer medulla membranes. Injections are given at different locations, such as lumbar for delivery (SC), obstetrics and lower abdominal surgery. In cervical to reach the lost feeling in the neck; in torakal for cuts in the lung and upper abdomen. This method is feasible to use for a long time for surgery or for postoperative pain management.
e. Surface anesthesiaAs injection is widely used as pain by a dentist to pull teeth or for minor surgery such as suturing the skin. Surface anesthesia is also used as a preparation for diagnostic procedures such as bronchoscopy, gastroscopy and sitoskopi.
2.Other UsageLocal anesthesia is used orally as a solution to pain in the mouth or suction tablets (sore throat). Also in the form of eye drops to measure the intraocular pressure or remove foreign objects, as well as ointments for itching or pain of burns.Ester compounds often cause allergic skin reactions, then you should use an amide compound which is more rarely result in hipersensitasi.
Pharmacodynamic
1. In SSPdapat stimulate CNS became agitated and tremor and clonic convulsions and depression and lead to death (paralysis breath
2. In muscle and ganglion nerve connections can influence the transmission at the neuromuscular connection is reduced muscle response on nerve stimulation
3. In the cardiovascular system: myocardial caused the decrease in excitability, Kec conduction & contraction strength (high KDR Dlm plasma); arteriolar vasodilatation
4. Pd smooth muscle: Unresponsive spasmolytic berhub dg anesthetic effect
5. Onset, intensity, and duration of nerve blockade is determined by the size and anatomical location of nerve.
6. Na + channel is important in muscle cells that can be excited like heart. The effect of cardiac Na + channels is the basis of local anesthetic therapy in the treatment of certain aritmi.
7. Local anesthesia is generally less effective in infected tissue than normal tissue, usually because of local infection resulting in metabolic acidosis
Profile of drug
1. Procaine
a. Pharmacodynamic
* Dose 100-800 mg: mild analgesic, 10-20 max effect ', missing timeout 60'
* Dhidrolisis mjd PABA (para amino benzoic acid) to inhibition of sulfonamide
b. PharmacokineticEsterase
* Absorption fast PABA + dietilaminoetanolHydrolysis* PABA excreted urine Dlm (Btk intact and conjugated)
c. Indication
* Infiltration anesthesia, nerve blocks, epidural, caudal and spinal
* Geriatric: improve sexual activity & FGS kel endocrine (conflicted)
d. Preparations
* 1-2% procaine hydrochloride is an anesthetic infiltrates, 5-20%; spinal anesthesia
2. Lidocaine
a. Pharmacodynamic
* Local anesthesia strong. Tjd faster, stronger LBH, LBH LBH long & extensive procaine dp
* Lar 0.5% lidocaine is an anesthetic infiltrates, 1-2%; block and topical anesthesia
* Effective when without a vasoconstrictor, Kec absorption & tox, years of LBH short
b. Pharmacokinetic
* Easily absorbed dr tmpt injection
* It can penetrate the blood brain barrier
* Metab: liver; ex: urine
c. Indication
* Injection: infiltration anesthesia, nerve blocks, epidural anest, anest caudal, anest mucosa
* Anest infiltrates: 0.25 to 0.50% dg lar or without adrenaline
* Vizard teeth: lar Lido 1-2% adrenaline dg
* Anest surface, anest corneas (lidocaine 2% + adrenaline)
* Reduces heart irritability
3. Dibukain
* Local Anest strong PLG, PLG toxic, long working period
* 15x LBH strong & toxic dg LBH 3x long period of procaine dp
* KDR 0.05 to 0.1%: anest injection; anest urethra from 0.05 to 0.2%; anest spinal: 7.5 to 10 mg
4. Mepivakain HCl
* Similar to lidocaine
* Anest infiltra, regional nerve blockade, spinal anest
* Dosage: Injection is a solution of 1%, 1.5%, 2%
5. Piperakain HCl
* I.v: toks 3x procaine
* Strength anest = procaine
* Use topical: 2% lar to the cornea, 4% for eye ointment; nerve blockade: lar 0.5-1%
6. Tetrakain
* PABA derivatives
* It is a local anesthetic that penetrates the cornea and conjunctiva, the drug is effective after topical administration to the eyes in 30 sec and anesthesia lasted for min. 15 min
* I.v = active & LBH LBH 10x toxic procaine dp
* Dosage and administration: in the eyes of 1 or 2 drops of a solution of 0.5%; ENT: lar 2%
* Contraindications: known the hipersensitiv against tetrakain, ocular inflammation or infection
* Precautions: teranestesi eyes must be protected from dust and bacteriological contamination samapai sensation of a full recovery. Use the old can cause opacity of the cornea
* Adverse effects: local burning feeling can arise and, more rarely is lakrimasi and photophobia
* Storage: Tetrakain eye drops should be stored in tightly closed containers protected from light and do not cooled
7. Prilokain HCL
* Securities fkologi lidocaine mrp
* At & long working long LBH lidocaine dp
* Dosage: KDR 1,2,3%
8. Bupivacaine
This substance inhibits the initiation and transmission of nerve impul in place to stabilize the membrane of nerve. This compound is metabolized in the liver. Anesthesia and usually work for 2-4 hours
Usefulness
* Anesthesia infiltration
* Block of peripheral nerve and sympathetic
* Dental Anesthesia
* Spinal Anesthesia
* Epidural and caudal anesthesia
* Bupivacaine is not suitable for intravenous regional anesthesia or the use of topical
Contraindications
* Skin infections are adjacent to the injection site or any abnormal bleeding tendency
* Severe anemia
* Heart disease
* Local and epidural anesthesia was not performed in patients with dehydration and hypovolemia
* High levels of bupivacaine in the blood should be avoided in patients with hepatic disorders
Side effects
* The side effects are a result of the depressant effects on CNS and cardio-depresifnya effect (suppressing the function of the heart) with symptoms of inhibition of respiration and blood circulation. Local Anestetika can also cause a reaction that is often a exantema hipersensitasi, urticaria and allergic until sometimes shock bronchospasme anafilaktis which can be deadly. The famous dal; am this are substances procaine and tetrakain ester groups, which therefore is not used anymore in local stocks. Hipersensitasi reaction was caused by PABA (para amino benzoic acid), which is formed through hydrolysis. PABA can negate the effects of sulfonamide antibakteriil. Therefore, therapy with a sulfa should not be combined with the use of these esters.
* CNS effects: depression, stimulation, depending on the neural pathways affected by local anesthesia
* Overdose of local anesthetics can cause:
* Decrease the transmission of impulses in neuromuscular junctions and synapses ganglion
* Causes muscle weakness and paralysis
Provision of Local Anesthesia Techniques
1. Surface anesthesia
2. Infiltration anesthesia
3. Block anesthesia
* Spinal Anesthesia
* Epidurals
* Anesthesia caudal
Use
1. In parenteral local anesthetic often used in surgery.
Type of local anesthesia of the most widely used as an injection is as follows:
a. Infiltration anesthesiaSome injections are given at or around a network that will dianestetisir, resulting in loss of sensation in the skin and the tissue that lies deeper, for example in the practice of ENT (Ear, Nose, Throat) or gum (in a tooth extraction).
b. Conduction anesthesia (peripheral nerve block ade), the injection in the spine at a gathering place for many nerves, especially on the operating arm or leg, and shoulder. It is also used to block the intense pain.
c. Spinal anesthesia (intrathecal), also called the dorsal injection. Drugs injected in the spine that contains cerebrospinal fluid. Thus injection across the outer membranes of the medulla (duramater), usually between the lumbar vertebra to the third and fourth. Thus, anesthesia of the foot / lower body to the breastbone can be reached within a few minutes.
d. Epidurals also ternasuk back injection. Drugs injected in the epidural space, the space between the outer medulla membranes. Injections are given at different locations, such as lumbar for delivery (SC), obstetrics and lower abdominal surgery. In cervical to reach the lost feeling in the neck; in torakal for cuts in the lung and upper abdomen. This method is feasible to use for a long time for surgery or for postoperative pain management.
e. Surface anesthesiaAs injection is widely used as pain by a dentist to pull teeth or for minor surgery such as suturing the skin. Surface anesthesia is also used as a preparation for diagnostic procedures such as bronchoscopy, gastroscopy and sitoskopi.
2.Other UsageLocal anesthesia is used orally as a solution to pain in the mouth or suction tablets (sore throat). Also in the form of eye drops to measure the intraocular pressure or remove foreign objects, as well as ointments for itching or pain of burns.Ester compounds often cause allergic skin reactions, then you should use an amide compound which is more rarely result in hipersensitasi.
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