Smolensk state medical academy
Pharmacology department
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Anticholinergic drugs and drugs acting on autonomic ganglia презентация
Содержание
- 1. Anticholinergic drugs and drugs acting on autonomic ganglia
- 2. ANTICHOLINERGIC DRUGS (Muscarinic receptor antagonists, Atropinics, Parasympatholytics)
- 3. Classification of anticholinergic drugs M, N -
- 4. Classification of cholinergic blockers I. M,
- 5. Muscarinic receptor antagonists 2. Semisynthetic derivatives Homatropine
- 6. Muscarinic receptor antagonists 3. Synthetic compounds Mydriatics:
- 7. Muscarinic receptor antagonists Vasicoselective: Oxybutinine, Flavoxate, Tolterodine Antiparkinsonian: Trihexyphenidyl, Procyclidine, Biperiden
- 8. Classification of anticholinergic drugs N –
- 9. Neuromuscular blocking agents (skeletal muscle relaxants) Non-depolarizing
- 10. Neuromuscular blocking agents (skeletal muscle relaxants) Long-term
- 11. Classification of anticholinergic drugs Ganglion blockers (block
- 12. М-cholinoreceptors Block М-cholinoceptors and prevent from Асh action Inhibit activity of parasympathetic nervous system
- 13. The main pharmacological effects: of М-cholinoblockers Influence
- 14. The main pharmacological effects: of М-cholinoblockers Influence
- 15. The main pharmacological effects: of М-cholinoblockers Influence
- 16. Comparative characteristics of М-cholinoblockers Atropine
- 17. Belladonna
- 18. Black henbane
- 19. DATURA STRAMONIUM
- 20. Atropine High doses cause cortical excitation, restlessness,
- 21. Comparative characteristics of М-cholinoblockers Platyphyllin
- 22. Senecio (groundsel)
- 23. Сomparative characteristics of М-cholinoblockers Pirenzepine,
- 24. Indication for administration of М-cholinoblockers
- 25. Indications for administration of М-cholinoblockers
- 26. Indications for administration of М-cholinoblockers 10.
- 27. Adverse effects of М-cholinoblockers dry mouth
- 28. Poisoning by atropine and atropinics Clinical symptoms
- 29. Poisonning by atropine and its analogues in
- 30. Mesures of first aid in poisonning Removal
- 31. Contraindications: glaucoma myocardium lesion, heart valvular defect, cardiac insufficiency hyperthermia hypertension and tachycardia
- 32. N-cholinoblockers block nicotinic receptor, as a result,
- 33. N-cholinoblockers According to selectivity
- 34. Ganglion blockers block Nn-cholinoceptors in autonomic ganglia of sympathetic and parasympathetic nervous system
- 35. Ganglionic blockers Classification according to chemical structure:
- 36. Ganglion blockers Classification according to duration of
- 37. Mechanism of ganglionic blocker action is related
- 38. Mechanism of ganglionic blocker action other preparations
- 39. Pharmacological effects of ganglion blockers As a
- 40. Pharmacological effects of ganglion blockers As a
- 41. Adverse effects of ganglion blockers Orthostatic collapse
- 42. Contraindications: Hypotension Ischemic heart disease Glaucoma Liver and kidney function disorders
- 43. First aid in overdosage with ganglion blockers
- 44. Skeletal muscle relaxants (neuromuscular blockers) Skeletal muscle
- 45. Pharmacodynamics of muscle relaxants Non-depolarizing (antidepolarizing) muscle
- 46. Depolarizing muscle relaxants Suxamethonium chloride
- 47. Depolarizing muscle relaxants Anticholineasterases potentiate (enhance) action
- 48. Muscle relaxants of mixed action Dioxonium -
- 49. Administration of muscle relaxants Anesthesiology and
- 50. Administration of muscle relaxants They are quaternary
- 51. Adverse effects of muscle relaxants Depolarizing ones:
- 52. Antagonists of muscle relaxants Neostigmine 0.5-2.0mg i.v.,
ANTICHOLINERGIC DRUGS (Muscarinic receptor antagonists, Atropinics, Parasympatholytics) Conventionally, the term “anticholinergic drugs” is restricted to those which block actions of Ach on autonomic effectors and in the CNS exerted through muscarinic
Слайд 2ANTICHOLINERGIC DRUGS (Muscarinic receptor antagonists, Atropinics, Parasympatholytics)
Conventionally, the term “anticholinergic drugs”
is restricted to those which block actions of Ach on autonomic effectors and in the CNS exerted through muscarinic receptors.
Though nicotinic receptor antagonists also block certain actions of Ach, they are generally reffered to as “ganglion blockers” and “neuromuscular blockers.
Though nicotinic receptor antagonists also block certain actions of Ach, they are generally reffered to as “ganglion blockers” and “neuromuscular blockers.
Слайд 3Classification of anticholinergic drugs
M, N - c h o l i
n e r g i c b l o c k e r s
М – c h o l i n e r g i c b l o c k e r s (antimuscarinic drugs)
N – c h o l i n e r g i c b l o c k e r s:
Neuromuscular blocking agents (skeletal muscle relaxant) - block Nm receptor
Ganglion blockers - block Nn receptors
М – c h o l i n e r g i c b l o c k e r s (antimuscarinic drugs)
N – c h o l i n e r g i c b l o c k e r s:
Neuromuscular blocking agents (skeletal muscle relaxant) - block Nm receptor
Ganglion blockers - block Nn receptors
Слайд 4Classification of cholinergic blockers
I. M, N - c h o l
i n o b l o c k e r s:
Aprofene
М – c h o l i n o b l o c k e r s (Muscarinic receptor antagonists, Atropinics):
1. Natural alkaloids
Atropine sulfate
Hyoscine hydrobromide (Scopolamine)
Platyphylline hydrotartrate
Aprofene
М – c h o l i n o b l o c k e r s (Muscarinic receptor antagonists, Atropinics):
1. Natural alkaloids
Atropine sulfate
Hyoscine hydrobromide (Scopolamine)
Platyphylline hydrotartrate
Слайд 5Muscarinic receptor antagonists
2. Semisynthetic derivatives
Homatropine hydrobromide
Atropine methonitrate
Hyoscine butyl bromide
Ipratropium
bromide (atrovent)
Tiotropium bromide
Tiotropium bromide
Слайд 6Muscarinic receptor antagonists
3. Synthetic compounds
Mydriatics: Cyclopentolate, Tropicamide
Antisecretory-antispasmodics:
Quaternary compounds: Propantheline, Oxyphenonium,
Clidinium, Pipenzolate methylbromide, Isopropamide, Glycopyrrolate
Tertiary amines: Dicyclomine, Valethamate, Pirenzepine
Tertiary amines: Dicyclomine, Valethamate, Pirenzepine
Слайд 7Muscarinic receptor antagonists
Vasicoselective: Oxybutinine, Flavoxate, Tolterodine
Antiparkinsonian: Trihexyphenidyl, Procyclidine, Biperiden
Слайд 8Classification of anticholinergic drugs
N – c h o l i n
o b l o c k e r s
I. Neuromuscular blockers(skeletal muscle relaxants)
Depolarizing ones
Short-term acting (5-10 min)
Suxamethonium cloride
I. Neuromuscular blockers(skeletal muscle relaxants)
Depolarizing ones
Short-term acting (5-10 min)
Suxamethonium cloride
Слайд 9Neuromuscular blocking agents (skeletal muscle relaxants)
Non-depolarizing (anti-depolarizing) muscle relaxant
of competitive type action
Short-term acting (15-20 min)
Mivacurium chloride
Mid-term acting (30-60 min):
Alcuronium chloride
Atracurium besilate
Vecuronium bromide
Cisatracirium besilate
Rocuronium bromide
Short-term acting (15-20 min)
Mivacurium chloride
Mid-term acting (30-60 min):
Alcuronium chloride
Atracurium besilate
Vecuronium bromide
Cisatracirium besilate
Rocuronium bromide
Слайд 10Neuromuscular blocking agents (skeletal muscle relaxants)
Long-term acting (60-120 min)
Pancuronium bromide
Pipecuronium bromide
Tubocurarine chloride
Mellictinum
Doxacurium
Muscle relaxants of mixed action
Dioxonium
Слайд 11Classification of anticholinergic drugs
Ganglion blockers (block Nn receptors):
Short-term acting ones (10-20
min)
Trepirium iodide
Imechinum
Mid-term acting ones (3-4 hours)
Azamethonium bromide
Hexamethonium benzosulfonate (benzohexonium)
Pachycarpine hydroiodide
Long-term acting ones (8 hours and more)
Pempidine tosylate
Temechinum
Trepirium iodide
Imechinum
Mid-term acting ones (3-4 hours)
Azamethonium bromide
Hexamethonium benzosulfonate (benzohexonium)
Pachycarpine hydroiodide
Long-term acting ones (8 hours and more)
Pempidine tosylate
Temechinum
Слайд 12М-cholinoreceptors
Block М-cholinoceptors and prevent from Асh action
Inhibit activity of parasympathetic nervous
system
Слайд 13The main pharmacological effects:
of М-cholinoblockers
Influence on eye function:
as opposed
to M-cholinomimetics:
dilate pupil (midriasis)
paralyse (relax) accommodation
increase intraocular tension
Influence on smooth muscles:
decrease tone of smooth muscles of GIT, bronchi, biliary and urinary tract
Action on the heart:
tachycardia
increase in atrio-ventricular conduction and myocardium oxygen demand
dilate pupil (midriasis)
paralyse (relax) accommodation
increase intraocular tension
Influence on smooth muscles:
decrease tone of smooth muscles of GIT, bronchi, biliary and urinary tract
Action on the heart:
tachycardia
increase in atrio-ventricular conduction and myocardium oxygen demand
Слайд 14The main pharmacological effects:
of М-cholinoblockers
Influence on gland secretion :
the drugs inhibit
secretion of glands due to block of М3-cholinoceptors of glandular cell membranes
Secretion of salivary, nasopharyngeal, bronchial, gastric, sweet and lachrymal glands decreases
That leads to dryness of the skin and mucous membranes
Secretion of salivary, nasopharyngeal, bronchial, gastric, sweet and lachrymal glands decreases
That leads to dryness of the skin and mucous membranes
Слайд 15The main pharmacological effects:
of М-cholinoblockers
Influence on thermoregulation
Block М3-cholinoreceptors of sweet
glands, inhibit sweet secretion what can lead to thermoregulation disturbance. As a result, body temperature can increase.
Influence on the CNS
Preparations of tertiary structure (Atropine, Hyosyamine, Platyphyllin) pass through blood-brain barrier and take action on the CNS.
At medium therapeutic dose Atropine blocks the relative cholinergic overactivity of basal ganglia, suppresses tremor and rigidity at parkinsonism.
Influence on the CNS
Preparations of tertiary structure (Atropine, Hyosyamine, Platyphyllin) pass through blood-brain barrier and take action on the CNS.
At medium therapeutic dose Atropine blocks the relative cholinergic overactivity of basal ganglia, suppresses tremor and rigidity at parkinsonism.
Слайд 16Comparative characteristics of
М-cholinoblockers
Atropine
is an alkaloid contained in belladonna,
black henbane, datura (thornapple, mad apple)
It is well absorbed from GIT and from mucous membranes
Duration of resorptive effect is about 6 hours
Its biotransformation occurs in the liver
it is mainly eliminated by kidney
It is non-selective blocker of М-cholinoceptors
At therapeutic doses it stimulates respiratory, vagal, vasomotor medullary centers
It is well absorbed from GIT and from mucous membranes
Duration of resorptive effect is about 6 hours
Its biotransformation occurs in the liver
it is mainly eliminated by kidney
It is non-selective blocker of М-cholinoceptors
At therapeutic doses it stimulates respiratory, vagal, vasomotor medullary centers
Слайд 20Atropine
High doses cause cortical excitation, restlessness, disorientation, hallucinations and delirium, followed
by respiratory depression and coma.
Слайд 21Comparative characteristics of
М-cholinoblockers
Platyphyllin
alkaloid, contained in plant groundsel
It has
“double” spasmolytic action:
blocks м-cholinoreceptors, i.е. takes neurotropic spasmolytic action
in contrast to other М-cholinoblockers it takes direct myotropic spasmolytic action
Scopolamine
It is characterized by high activity regarding М-cholinoceptors of vestibular apparatus (antimotion sickness property due to depression of vestibular excitation)
It takes depressant and amnestic action on the CNS, induces “twilight sleep” ans has been used as a lie detector or truth serum
blocks м-cholinoreceptors, i.е. takes neurotropic spasmolytic action
in contrast to other М-cholinoblockers it takes direct myotropic spasmolytic action
Scopolamine
It is characterized by high activity regarding М-cholinoceptors of vestibular apparatus (antimotion sickness property due to depression of vestibular excitation)
It takes depressant and amnestic action on the CNS, induces “twilight sleep” ans has been used as a lie detector or truth serum
Слайд 23Сomparative characteristics of
М-cholinoblockers
Pirenzepine, Telenzepine
Act selectively on М1-cholinoreceptors of the
stomach and inhibit gastric gland secretion of hydrochloric acid and pepsinogen
Ipratropium, Tiotropium
Are quaternary atropinics
they more markedly block М-cholinoceptors of smooth muscles of bronchi and cause their dilation
Ipratropium, Tiotropium
Are quaternary atropinics
they more markedly block М-cholinoceptors of smooth muscles of bronchi and cause their dilation
Слайд 24Indication for administration of
М-cholinoblockers
For preanaesthetic medication (Atropine, Glycopyrrolate).
They is used to inhibit bronchial secretion, to block vagal influence for prevention of reflex cardiac arrest and respiratory standstill
For elimination of spasms of smooth muscles of GIT, urinary tract , biliary tract more frequently Dicyclomine, Valethamate, Pipenzolate)
For relief of bronchospasm in COPD and bronchial asthma (Ipratropium, Tiotropium) by inhalation)
Stomach ulcer, hyperacid gastritis to inhibit secretion of HCl (Pirenzepine, Telenzepine, Propantheline)
Hyperkinesia, Parkinsonism (Trihexyphenidyl, Procyclidine, Biperiden)
For elimination of spasms of smooth muscles of GIT, urinary tract , biliary tract more frequently Dicyclomine, Valethamate, Pipenzolate)
For relief of bronchospasm in COPD and bronchial asthma (Ipratropium, Tiotropium) by inhalation)
Stomach ulcer, hyperacid gastritis to inhibit secretion of HCl (Pirenzepine, Telenzepine, Propantheline)
Hyperkinesia, Parkinsonism (Trihexyphenidyl, Procyclidine, Biperiden)
Слайд 25Indications for administration of
М-cholinoblockers
6. In ophthalmology
To dilate pupil for
choice of eyeglasses, for examination of eye fundus (Tropicamide, Cyclopentholate, Homatropine)
eye trauma, iridocyclitis (due to paralysis of accomodation and relaxation of circular muscle of eye pain decreases and healing is accelerated (Atropine)
7. Naupathia (motion sickness) – occurs in excitation of М-cholinoreceptors of vestibular apparatus (Scopolamine)
8. Poisoning with M-cholinomimetics and and anticholinesterases (Atropine)
9. In cardiology
Vagal cardiac arrhythmia
Atrioventricular block (Atropine, synthetic analogues)
eye trauma, iridocyclitis (due to paralysis of accomodation and relaxation of circular muscle of eye pain decreases and healing is accelerated (Atropine)
7. Naupathia (motion sickness) – occurs in excitation of М-cholinoreceptors of vestibular apparatus (Scopolamine)
8. Poisoning with M-cholinomimetics and and anticholinesterases (Atropine)
9. In cardiology
Vagal cardiac arrhythmia
Atrioventricular block (Atropine, synthetic analogues)
Слайд 26Indications for administration of
М-cholinoblockers
10. In urology (vasicoselective drugs)
For treatment of
urinary incontinence (detrusor instability)
renal colics (Oxybutinin, Dicyclomine, Flavoxate)
renal colics (Oxybutinin, Dicyclomine, Flavoxate)
Слайд 27Adverse effects of
М-cholinoblockers
dry mouth
dysphagia, speech disturbance (dysarthria)
accomodation disorders
tachycardia
constipation
urinary retention
Слайд 28Poisoning by atropine and atropinics
Clinical symptoms of acute poisonning:
dry flushed and
hot skin, especially over face and neck
hyperthermia,
tachycardia, rapid («galloping») pulse,
shining dilated pipils, accomodation paralysis (blurring of near vision), diplopia, photophobia, intraocular tension increase,
dyspnea (tachypnea),
headache,
Dry mouth and throat, dysphagia, speech disturbance (dysarthria)
Urinary retention,
Excitement, psychotic behaviour, ataxia, delirium, dreadfull hallucinations
hyperthermia,
tachycardia, rapid («galloping») pulse,
shining dilated pipils, accomodation paralysis (blurring of near vision), diplopia, photophobia, intraocular tension increase,
dyspnea (tachypnea),
headache,
Dry mouth and throat, dysphagia, speech disturbance (dysarthria)
Urinary retention,
Excitement, psychotic behaviour, ataxia, delirium, dreadfull hallucinations
Слайд 29Poisonning by atropine and its analogues
in severe cases – convulsion with
loss of consciousness, coma, hypotension;
Phase of excitement can be absent in children,
poisoning is more dangerous for children;
approximate lethal dose of atropine and scopolamine for adults is more 100 мg, for children less 10 years of age – about 10 мg
Phase of excitement can be absent in children,
poisoning is more dangerous for children;
approximate lethal dose of atropine and scopolamine for adults is more 100 мg, for children less 10 years of age – about 10 мg
Слайд 30Mesures of first aid in poisonning
Removal of non-absorbed poison from GIT
gastric
lavage with tannic acid, saline purgatives (MgSO4), activated charcoal
2. “dilution” and elimination of poison from the blood
forced diuresis (i/v saline infusion+diuretic Furosemide)
Administration of pharmacological antagonists: anticholinesterases of reversible action
Physostigmine, Galantamine. They promote accumulation of Асh, which displaces M-cholinoblockers from bond to receptor
4. Symptomatic therapy: tranquilizers, sedatives; physical cooling;
in respiratory impairments - artificial lung ventilation,
in tachycardia – β-adrenoblockers
2. “dilution” and elimination of poison from the blood
forced diuresis (i/v saline infusion+diuretic Furosemide)
Administration of pharmacological antagonists: anticholinesterases of reversible action
Physostigmine, Galantamine. They promote accumulation of Асh, which displaces M-cholinoblockers from bond to receptor
4. Symptomatic therapy: tranquilizers, sedatives; physical cooling;
in respiratory impairments - artificial lung ventilation,
in tachycardia – β-adrenoblockers
Слайд 31Contraindications:
glaucoma
myocardium lesion, heart valvular defect, cardiac insufficiency
hyperthermia
hypertension and tachycardia
Слайд 32N-cholinoblockers
block nicotinic receptor, as a result, they stop transmission of nerve
impulses in corresponding synapses;
N-cholinoceptors are not homogeneous and unequally react to pharmacological analyzers;
thus, N-cholinoceptors of skeletal muscles are sensitive to tubocurarin and not blocked by hexamethonium;
N-cholinoreceptors of vegetative ganglions, to the contrary, are blocked by Hexamethonium and not sensitive to tubocurarin;
so, nicotitinic receptors of skeletal muscles are conditionally designated as Nm-cholinoceptors;
Receptors of vegetative ganglion neurones –
Nn-cholinoceptors
N-cholinoceptors are not homogeneous and unequally react to pharmacological analyzers;
thus, N-cholinoceptors of skeletal muscles are sensitive to tubocurarin and not blocked by hexamethonium;
N-cholinoreceptors of vegetative ganglions, to the contrary, are blocked by Hexamethonium and not sensitive to tubocurarin;
so, nicotitinic receptors of skeletal muscles are conditionally designated as Nm-cholinoceptors;
Receptors of vegetative ganglion neurones –
Nn-cholinoceptors
Слайд 33N-cholinoblockers
According to selectivity of action on this two
types receptors preparations of N-cholinoblockers are divided into 2 groups:
Skeletal muscle relaxants
(block Nm-cholinoceptors) and
Ganglion blockers
(block Nn-cholinoceptors)
Skeletal muscle relaxants
(block Nm-cholinoceptors) and
Ganglion blockers
(block Nn-cholinoceptors)
Слайд 34Ganglion blockers
block Nn-cholinoceptors in autonomic ganglia of sympathetic and parasympathetic nervous
system
Слайд 35Ganglionic blockers
Classification according to chemical structure:
Quaternary ammonium compounds:
Imechinum, Trepirium, Azamethonium, Hexamethonium
they are badly absorbed from GIT
they do not pass to the CNS
Tertiary amines:
Pachicarpine, Pempidine, Temechinum
they are absorbed from intestine
they pass through blood-brain barrier
they are badly absorbed from GIT
they do not pass to the CNS
Tertiary amines:
Pachicarpine, Pempidine, Temechinum
they are absorbed from intestine
they pass through blood-brain barrier
Слайд 36Ganglion blockers
Classification according to duration of action:
Short-term acting (10-20 min)
Trepirium iodide (Hygronium)
Imechinum
Used for controlled hypotension during operations to decrease loss of blood
Mid-term acting (1-4 hours)
Azamethonium bromide
Hexamethonium benzosulfonate
Pachicarpine hydroiodide
used for relief of hypertensic crysis
Long-term acting (6-12 hours)
Pempidine
Temechinum
Imechinum
Used for controlled hypotension during operations to decrease loss of blood
Mid-term acting (1-4 hours)
Azamethonium bromide
Hexamethonium benzosulfonate
Pachicarpine hydroiodide
used for relief of hypertensic crysis
Long-term acting (6-12 hours)
Pempidine
Temechinum
Слайд 37Mechanism of ganglionic blocker action
is related to block of Nn-cholinoceptors in
synapses of vegetative ganglia, medulla of adrenals, sino-carotide zone
the preparations block receptors in sympathetic and parasympathyic ganglia differently
thus, Hexamethonium and Pempidine block ion channels, coupled to Nn-cholinoreceptors
the preparations block receptors in sympathetic and parasympathyic ganglia differently
thus, Hexamethonium and Pempidine block ion channels, coupled to Nn-cholinoreceptors
Слайд 38Mechanism of ganglionic blocker action
other preparations (Imecninum) block recognizing receptor sites
as
a result, ganglion blockers interrupt impulse transmission in ganglia
impulse flow to nerve endings stops
that results in a decrease of noradrenalin release in synapses of vessels
adrenaline secretion in chromaffin cells of adrenal glands decreases
block of parasympathetic ganglions leads to stoppage of impulses to smooth muscles of GIT, bronchi and glands.
impulse flow to nerve endings stops
that results in a decrease of noradrenalin release in synapses of vessels
adrenaline secretion in chromaffin cells of adrenal glands decreases
block of parasympathetic ganglions leads to stoppage of impulses to smooth muscles of GIT, bronchi and glands.
Слайд 39Pharmacological effects of ganglion blockers
As a result of block of parasympathetic
ganglia:
arteries, veins, peripheral blood vessels are dilated,
ABP decrease,
t.p.r., pre- and afterload decrease,
tissue microcirculation is improved,
blood congestion in veins increases
uterine tone increases
arteries, veins, peripheral blood vessels are dilated,
ABP decrease,
t.p.r., pre- and afterload decrease,
tissue microcirculation is improved,
blood congestion in veins increases
uterine tone increases
Слайд 40Pharmacological effects of ganglion blockers
As a result of block of parasympathetic
ganglia:
a tone and motility of smooth muscles decrease
secretion of salivary, gastric, bronchial glands decrease
block of reflex reactions
Nowadays ganglion blockers
are used very seldom, as their action is nonselective and so they have many adverse effects
a tone and motility of smooth muscles decrease
secretion of salivary, gastric, bronchial glands decrease
block of reflex reactions
Nowadays ganglion blockers
are used very seldom, as their action is nonselective and so they have many adverse effects
Слайд 41Adverse effects of ganglion blockers
Orthostatic collapse (fall of arterial blood pressure)
Danger
of thrombosis due to slowing-down of blood flow (stasis)
To prevent orthostatic collapse ganglion blockers must be injected in recumbent position and after introduction patient must stay recumbent for 2 hours
Atony of intestine and urinary bladder,
Constipation, urinary retention,
Midriasis, paralysis of accomodation,
Dry mouth, dysphagy, dysarthria (speech disturbance)
To prevent orthostatic collapse ganglion blockers must be injected in recumbent position and after introduction patient must stay recumbent for 2 hours
Atony of intestine and urinary bladder,
Constipation, urinary retention,
Midriasis, paralysis of accomodation,
Dry mouth, dysphagy, dysarthria (speech disturbance)
Слайд 42Contraindications:
Hypotension
Ischemic heart disease
Glaucoma
Liver and kidney function disorders
Слайд 43First aid in overdosage with ganglion blockers
Introduction of pharmacological antagonists (anticholinesterases),
analeptics
Artificial lung ventilation (ALV)
Orthostatic hypotension is releaved by introduction of vasoconstrictive agents (Norepinephrine, Phenylephrine)
Artificial lung ventilation (ALV)
Orthostatic hypotension is releaved by introduction of vasoconstrictive agents (Norepinephrine, Phenylephrine)
Слайд 44Skeletal muscle relaxants (neuromuscular blockers)
Skeletal muscle relaxants (curare-like agents) cause total
relaxation of skeletal muscles due to selective block of
Nm-cholinoceptors and stoppage of neuro-muscular transmission in neuro-muscular synapses – myoparalytic effect (paralysis of skeletal muscles)
Nm-cholinoceptors and stoppage of neuro-muscular transmission in neuro-muscular synapses – myoparalytic effect (paralysis of skeletal muscles)
Слайд 45Pharmacodynamics of muscle relaxants
Non-depolarizing (antidepolarizing) muscle relaxants
Most of them act as
competitive antagonists of Асh
They block Nm-cholinoceptors of postsynaptic membrane of neuromuscular synapse and prevent depolarizing action of Ach
Postsynaptic membrane at that stays non-depolarized
Transmission of impulses from nerve endings to skeletal muscles is blocked, as a result, skeletal muscles are relaxed.
They block Nm-cholinoceptors of postsynaptic membrane of neuromuscular synapse and prevent depolarizing action of Ach
Postsynaptic membrane at that stays non-depolarized
Transmission of impulses from nerve endings to skeletal muscles is blocked, as a result, skeletal muscles are relaxed.
Слайд 46Depolarizing muscle relaxants
Suxamethonium chloride -
(doubled molecule of
acetylcholine)
interacts with Nm-cholinoreceptors of postsynaptic membrane, causes its stable depolarization
desensitization (loss of sensitivity) of receptors and neuromuscular block occur
A muscle contracts, then relaxes
Microtrauma of fibers and muscle pains are observed in postoperative period
interacts with Nm-cholinoreceptors of postsynaptic membrane, causes its stable depolarization
desensitization (loss of sensitivity) of receptors and neuromuscular block occur
A muscle contracts, then relaxes
Microtrauma of fibers and muscle pains are observed in postoperative period
Слайд 47Depolarizing muscle relaxants
Anticholineasterases potentiate (enhance) action of depolarizing muscle relaxats
Inactivation
of depolarizing muscle relaxants is realized by pseudocholinesterase – butyrylcholinesterase of plood plasma
In overdosage of DMR transfusion of fresh donor blood can be recommended, but not anticholinestarase agents
practically: Artificial lung ventilation (ALV) is performed, in 5-10‘ the drug is destroyed
In overdosage of DMR transfusion of fresh donor blood can be recommended, but not anticholinestarase agents
practically: Artificial lung ventilation (ALV) is performed, in 5-10‘ the drug is destroyed
Слайд 48Muscle relaxants of mixed action
Dioxonium - is seldom used
initially
it acts like depolarizing muscle relaxants (cause depolarization of membrane), then membrane potential is restored, but receptors are blocked for action of acetylcholine similar to antidepolarizing muscle relaxants)
Слайд 49Administration of muscle relaxants
Anesthesiology and surgery:
they used
for relaxation of skeletal muscles in reduction of dislocations, reposition of bone (fractured) fragments, intubation of trachea, endoscopy, laryngospasm, assisted ventillation (ALV)
Convusions, severe cases of tetanus and status epilepticus
Muscles are relaxed in certain order: muscles of face and neck, extremities and trunk, respiratory muscles and diaphragm
Muscle relaxants are used when ALV apparatus is available.
Convusions, severe cases of tetanus and status epilepticus
Muscles are relaxed in certain order: muscles of face and neck, extremities and trunk, respiratory muscles and diaphragm
Muscle relaxants are used when ALV apparatus is available.
Слайд 50Administration of muscle relaxants
They are quaternary ammonium compounds, and so they
badly absorbed from GIT and used only intravenously
A drug Mellictinum is tertiary base, it is a single muscle relaxant in the form of tablets.
It decreases tone of skeletal muscles not producing their paralysis
A drug Mellictinum is tertiary base, it is a single muscle relaxant in the form of tablets.
It decreases tone of skeletal muscles not producing their paralysis
Слайд 51Adverse effects of muscle relaxants
Depolarizing ones:
cardiac arrhythmia, ABP
rise
Muscle pains in postoperative period
↑ intraocular tension and intracranial pressure, myoglobinemia, hyperkaliemia
Antidepolarizing ones:
arterial hypotension,
bradycardia or tachycardia,
myocardium ischemia,
ventricular extrasystoles,
bronchospasm
Muscle pains in postoperative period
↑ intraocular tension and intracranial pressure, myoglobinemia, hyperkaliemia
Antidepolarizing ones:
arterial hypotension,
bradycardia or tachycardia,
myocardium ischemia,
ventricular extrasystoles,
bronchospasm
Слайд 52Antagonists of muscle relaxants
Neostigmine 0.5-2.0mg i.v., preceded by Atropine to block
muscarinic effects, rapidly reverses paralysis induced by competitive neuromuscular blockers
Sugammadex is new antagonist of antidepolarazing muscle relaxants. Its use does not need Atropine.
Sugammadex is new antagonist of antidepolarazing muscle relaxants. Its use does not need Atropine.
