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Drugs effecting the afferent
innervation
Substances which act in the
area of afferent nerves endings:
 local anesthetics
 astringent
 covering
 adsorbtive
 irritative
Local anesthetics
Local anesthetics
1. Natural compound – aether of
benzoilekgonin cocain
2. Synthetic neutrogen compounds
Aether compounds (derivatives from PABA)
a) easily dilluted in water : novocain (procain),
dicain (tetrakain)
b) badly dilluted in water: anaesthesin
(benzokain), orthokain
Amide compounds: lidocain (xycain),
trimecain, etydocain (duranest), prilocain
(citanest), articain (ultracain), piromecain
(bumekain), marcain (bupivacain)
STRUCTURE OF LOCAL
ANESTHETICS
x
I
(CH2)n
II
N
III
I – lipophilic aromatic group
II – intermediate aliphatic chain
III – hydrophilic amine-group
R
R
Kinds of local anesthesia:
terminal
conductive
infiltrative
Terminal (superficial) anesthesia local anesthetic is spread over mucous
membranes, wounds, ulcers, fresh
granulations
For terminal anesthesia we often
use anaesthesin, dicain, xycain,
trimecain, very rarely – novocain,
because it badly penetrates through
mucous membranes
Conductive (regional) anesthesia - is an
introduction of anesthetic into area of nervous
truncs, ganglia, sensitive roots of spinal cord.
Kinds of regional anesthesia: truncal
(conductive), plexal (anesthesia of nervous
plexuses), paravertebral (anesthesia of nerovus
ganglia), spinal-cord, peridural
For performing of this anesthesia novocain,
xycain, trimecain, ultracain are used
Infiltrative anesthesia – is a mixed
kind of local anesthesia, in which
nervous endings and fibres get turned
off because of layer by layer infiltration
of tissues with a solution of local
anesthetic.
For
infiltrative
anesthesia
novocain, xycain, trimecain,
ultracain
are used
Cocain (Cocainum) – alcaloid, which is
extracted from leaves of South-American
plant Erythroxylon coca. Its local anesthetic
action overwhelms local anesthetic activity
of novocain in 3 times and toxicity is 3-5
times greater
It is used very rarely
only for superficial anesthesia
in stomatology, otholaryngology, urology
in a form of 2-5 % solutions
Erythroxylon coca
TOXICOLOGY OF COCAIN
Acute intoxication: short-time euforia, fear,
tachicardia, exophtalm, dizziness, delirium, loss
of consciousness, seizures, comatous condition,
decreasing of arterial pressure, stop of breathing
Chronic intoxication – cocainism:
psychological and physical addiction, mental
degradation, cretinism, atrophyc disorders,
including perforation of nasal septum, gangrene,
heavy cardiac arrythmias, cardiac arrest
Novocain (Novocainum)
– derivative of
PABA (para-aminobenzoic acid)
usage
infiltrative anesthesia - 0,25-0,5 % solutions
truncal anesthesia - 1-2 % solutions
treatment blockades (paranephral,
vagosympathetic) – 0,25-0,5 % solutions
spinal cord anesthesia - 2-3 ml of 5 %
solution (is introduced into subarachnoid space
on the level higher than first lumbal vertebra)
At recent time novocain was used for depression of
reflexes, central nervous system, heart, in patients with
gastritis, ulcer disease, hypertonic disease, stenocardia,
neurodermitis, spasms of peripheral vessels. In this
case this drug was introduced intravenously or
intramuscularly
Xycain (Lidocain)
it is 2 times stronger (activity regarding)
than novocain with the same toxicity
usage
for all kinds of local anesthesia:
infiltrative - 0,25-0,5 % solutions
conductive – 0,5-2 % solutions
peridural – 0,5 % solution
spinal cord – 5 % solution
terminal – 4-10 % solutions
Xycain (Lidocain)
Xycain eliminates cardiac arrythmias of
ventricular origin, i.e. extrasystolia, fibrillation
of ventricules in acute miocardial infarction. In
this cases xycain is administred intravenously,
dropply, slowly, in a form of
0,2 % solution.
Xycain (lidocain) can be used in individuals, which
are sensybilized towards novocain and other
anesthetics of complexed aehters group (dicain,
anesthesin)
Xycain (Lidocain)
XYCAIN
(LIDOCAIN)
Trimecain
anesthetic avtivity and action duration are
2 times greater, comparatively to novocain,
toxicity is a bit higher
Usage
infiltrative - 0,125 %, 0,25 % and 0,5 %
solutions
truncal - 1 % and 2 % solutions
peridural - 1 %, 2 % solutions
spinal cord - 5 % solution
terminal - 2-5 % solutions
as an antiarythmic drug in cardial arythmias
of ventricular origin - intravenously, at the
begging in a form of 2 % solution very slowly
after - dropply 0,2 % soluiton
Bupivacain (marcain)
one of the most active anesthetics of
prolonged action (onset – 2-20 min, duration
of action – 7 hours)
Usage
infiltrative, truncal, epidural anesthesia
considerable cardiotoxicity !
Articain (ultracain)
usage
infiltrative and conductive
anesthesia
Analgetic action develops
after 1-2 min. after introduction of
the drug, lasts for 1-3,5 hours
in stomatology - combined
drug, which consists of ultracain
and adrenalini hydrochloridum
(epinephrin)
- ultracain D-C
Acute poisoning with local
anesthetics
Symptoms
decreasing of arterial pressure, of heart activity,
cardiac arrest, depression of CNS and breathing,
seizures
Treatment
vasoconstriction drugs (noradrenaline,
adrenaline), cardiotonic (strophantin, corglycon),
antiseizure drugs (sibazone, tiopental-sodium)
Prophilaxis
usage of least possible volume and most possible
dillution of the local anesthetics
Astringent drugs
Organic, of plant origin
tannin, infusion of tea, herba Hyperici,
flores Chamomillae, cortex Quercus
Nonorganic
Bismuthi subnitras, de-nol
Oak tree (bark)
Quercus robur L.
TANNIN
usage
rinsing of mouth, pharynx, larynx – 1-2 %
solution
treatment of burned surfaces, cracks, bedsores
– 3-10 % solutions
gastric lavage in case of poisoning with salts
of heavy metals and alcaloids – 0,5 % solution
Nota bene! Tannin forms nonstable
compounds with morphine, phisostigmine,
atropin, nicotine, cocain
Saint-John’s-wort
(Hypericum perforatum L.)
Matricary
Chamomilla recutita L.
Sage
Salvia officinalis L.
Drugs, which stimulate nervous endings
IRRITATIVE DRUGS
•
•
•
•
•
Ammonium solution
Menthol
Oleum Terpenthini purified
Mustard plaster
Camphor
Leaf Mustard
Brassica juncea
Ammonium solution 10 %
(ammoniac)
Usage
• Unconsciousness (put a cotton ball
moistured with ammonium solution to a
nose)
• In case of alcohol intoxication (orally
5-10 drops of solution dilluted in half of
a glass of water)
• For washing of surgeon’s hands
(rarely) (0,5 % solution)
Thanks for your attention!
Good-bye !
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