Anatomy-physiological Anatomy-physiological peculiarities of vegetative peculiarities of vegetative

nervous snervous sysystem. tem. Anticholinesterase drugsAnticholinesterase drugs

Lector prof. Posokhova K.A.Lector prof. Posokhova K.A.

EfferentEfferent nervous fibres supply nervous fibres supplyskeletal muscles – skeletal muscles – somaticsomatic;;regulate funtions of internal organs - regulate funtions of internal organs -

vegetativevegetative

SynapsSynaps - is a place of contact of long - is a place of contact of long fibre ending (fibre ending (axonaxon) of one neuron with ) of one neuron with a a body of other one or cell of active organ body of other one or cell of active organ ((effector celleffector cell))

Cholinergic synapsCholinergic synaps

Influence of parasympathetic and sympathetic nervous system on Influence of parasympathetic and sympathetic nervous system on function of organsfunction of organs

Eyem. sphincter pupillaem. dilatator pupillaem. ciliaris

contraction (miosis)absent innervationcontraction (close sight)

absent innervationcontraction (midriasis)dilation (far sight)

HeartExcitabilityConductionPower of contractionsFrequency of contraction

dicreasingslowing downdicreasingdicreasing

increasingspeeding upincreasingincreasing

VesselsSkin, mucous membranesMesentraium, organs of abdominal

cavitySkeletal musclesHeart, brain

absent innervation- ’’ -

dilation- ’’ -

contraction- ’’ –

- ’’ – - ’’ –

BronchiCircular musclesGlandular secretion

contractoinincreasing

dilationdecreasing

Stomach, intestinesPerystalticsTonus of sphynctersGlandular secretion

increasing decreasingincreasing

decreasingincreasingdecresing

Urinary bladderDetrusorSphyncter

contractiondilation

dilationcontraction

Glands (secretion)SalivarySweat

incresing (liquid secret, large quantity)

- ’’ -

increasing (small quantity) - ’’ -

Cholinergic Cholinergic nervous fibres are:nervous fibres are:1) 1) preganglionpreganglionicic (sympoathetic and (sympoathetic and

parasypmathetic);parasypmathetic);2) 2) all postgnglionall postgnglionicic parasympathetic; parasympathetic;3) 3) postganglionpostganglionicic sympathetic which sympathetic which

supply supply ssweat glands and vessels of skeletal weat glands and vessels of skeletal muscles;muscles;

4) 4) somatic nerves;somatic nerves;5) 5) nerves which supply adrenal nerves which supply adrenal

medulla medulla andand carotic sinuses; carotic sinuses;6) 6) neurons of CNSneurons of CNS

Adrenergic Adrenergic nervous fibres are: nervous fibres are: 1) 1) postganglionpostganglionicic sympathetic, sympathetic,

except those which supply sweat glands and except those which supply sweat glands and vessels of svessels of skkeletal muscles;eletal muscles;

2) neurons of CNS2) neurons of CNS

Cholinergic drugsCholinergic drugs

1) 1) M-, N-cholinomimetics M-, N-cholinomimetics (acetylcholine, (acetylcholine, carbacholine);carbacholine);

2) 2) Anticholinesterase drugsAnticholinesterase drugs – cholinesterase – cholinesterase inhibitorsinhibitors (proserin, galanthamine hydrobromide, (proserin, galanthamine hydrobromide, pirydostygmine bromide, pirydostygmine bromide, arminearmine););

3) 3) M-, N- cholinoblockers M-, N- cholinoblockers (amisyl, cyclodol); (amisyl, cyclodol); 4) M-cholinomimetics 4) M-cholinomimetics (pilocarpin, aceclidyn);(pilocarpin, aceclidyn);5)5) M-cholinoblockers M-cholinoblockers (atropine sulphate, (atropine sulphate,

platyphyllin hydrotartrate, scopolamine hydrobromide, platyphyllin hydrotartrate, scopolamine hydrobromide, metacinum);metacinum);

6) N-cholinomimetics 6) N-cholinomimetics (cytyton, lobelin);(cytyton, lobelin);7) N-cholinoblockers7) N-cholinoblockers: а) : а) ganglioganglionnblockers blockers

(benzohexonium, pentamin, (benzohexonium, pentamin, hyhygronium, arphonade);gronium, arphonade); б) mб) myyorelaxants orelaxants (tubocurarinum chloride, (tubocurarinum chloride, dytylinum, meldytylinum, mellliktiktiin)n)

AcetylcholineAcetylcholine

Carbacholine Carbacholine

M-, N-M-, N-cholinomimeticscholinomimetics

CarbacholineCarbacholine

0,5-1 % solutions of 0,5-1 % solutions of carbacholine -carbacholine - eye drops for eye drops for treatment of glaucoma treatment of glaucoma

The drug The drug is never used is never used orally orally and with injections becauand with injections becausse of e of its its consideralbe toxicity !consideralbe toxicity !

Amizyl Amizyl

Cyclodol Cyclodol

M-, N-M-, N-cholinoblockerscholinoblockers

AmizylAmizyl

Indications for administrationIndications for administration neurotic disorders, Parcinoson’s disease and neurotic disorders, Parcinoson’s disease and

other extrapyramidal disorders, for premedication other extrapyramidal disorders, for premedication before narcosis, for diseases which are before narcosis, for diseases which are

accompaniedaccompanied with spasm of smooth muscles, for with spasm of smooth muscles, for dilation of pupil in ophtalmology dilation of pupil in ophtalmology

The drug is administered orally 0,001-0,002 g The drug is administered orally 0,001-0,002 g 3-4 times per day, 3-4 times per day,

as eye droppsas eye dropps - - 1-21-2 % solution is used% solution is used Side Side eeffectsffects : dryness of mucous membranes, : dryness of mucous membranes,

tachycardia, dilation of pupils, tachycardia, dilation of pupils, disturbancesdisturbances of of accomodation. accomodation.

The drug The drug is contraindicated is contraindicated in case of glaucoma!in case of glaucoma!

CyclodolCyclodol

Anticholinergic drug, preferably Anticholinergic drug, preferably blocks central N-cholinoreceptors blocks central N-cholinoreceptors and peripheral M-cholinoreceptorsand peripheral M-cholinoreceptors

UsageUsage Parcіnson’s disease, Parcіnson’s disease,

medicamentous parcinsonismmedicamentous parcinsonism

Proserinum,Proserinum,Galanthamini Galanthamini hhydrobromidum,ydrobromidum,

Armin,Armin,

Pirydostygmini bromidumPirydostygmini bromidum

Anticholinesterase Anticholinesterase drugsdrugs

ProserinumProserinum

Proserinum is an anticholinesterase Proserinum is an anticholinesterase drug of reverse action, its effect lasts drug of reverse action, its effect lasts for 2,5-4 hours.for 2,5-4 hours.

Indications for Indications for administrationadministration

Impairment of nerve Impairment of nerve conductionconduction after after

polpolyyomomyyelitis, elitis, paralysisparalysis, , neurities, traumas neurities, traumas

overdosing with M-overdosing with M-cholinoblockerscholinoblockers

Galanthamini Galanthamini hydrobromidumhydrobromidum

Duration of action of Galanthamini Duration of action of Galanthamini hydrobromidum is longer than of hydrobromidum is longer than of Proserinum, that’s why it can be Proserinum, that’s why it can be administered 1-2 times administered 1-2 times perper day day

Indications for administrationIndications for administration

Impairment of nerve Impairment of nerve conductionconduction after polafter polyyomomyyelitis,elitis,

paralysesparalyses, neuritis, traumas, , neuritis, traumas, overdosing with M-cholinoblockersoverdosing with M-cholinoblockers

Pirydostigmini bromide Pirydostigmini bromide (calimin(calimin))

UsageUsage

mmyyasteniaastenia gravis gravis

after traumas, neurafter traumas, neuryyties, ties, paralysesparalyses

in in a a period of recoperiod of recoveryvery after after polpolyyomomyyelitis, encephalitiselitis, encephalitis

Anticholinesterase Anticholinesterase drugsdrugs are are

contraindicatedcontraindicated in casein casess of epilepsia, of epilepsia,

hyperkinesias, bronchial hyperkinesias, bronchial asthma, stenocardia, asthma, stenocardia,

bradycardiabradycardia

nausea, vomiting, dnausea, vomiting, diiarrhea, abdominal arrhea, abdominal painpain

quick contraction of pupils, quick contraction of pupils, disturbance disturbance of visusof visus (spasm of accom (spasm of accomoodation) dation)

increasing of salivation and sweatingincreasing of salivation and sweating bronchospasmbronchospasm tachy- or bradicardiatachy- or bradicardia seizures, excitement, loss of seizures, excitement, loss of

consciousness, comaconsciousness, coma

Death is caused by breath insufficiency, Death is caused by breath insufficiency, bronchospasm and lungs edemabronchospasm and lungs edema

Acute poisoning with Acute poisoning with anticholinesterase drugs (POanticholinesterase drugs (POCC))

TreatmTreatmeent should be started immediately nt should be started immediately (WHO)(WHO)stomach lavage with solution of stomach lavage with solution of Sodium hydrocarbonateSodium hydrocarbonate salt laxatives, enterosorbentssalt laxatives, enterosorbents siphon enemasiphon enema the poison should be carefully washed away from the skinthe poison should be carefully washed away from the skin forced diuresis, in complicated cases - hemosorbtion, forced diuresis, in complicated cases - hemosorbtion,

hemodialhemodialyysissis

UsageUsage of antagonist is necessary!!! – of antagonist is necessary!!! – atropine atropine sulphate.sulphate. It should be introduced intravenously It should be introduced intravenously repeatedlyrepeatedly, 2-4 , 2-4 ml ofml of 0,1 % 0,1 % solution with the interval ofsolution with the interval of 5- 5-10 10 minutes. Appearance of tachycardia, dilation of pupils, minutes. Appearance of tachycardia, dilation of pupils, dryness in the mouth are the criteria of sufficiency of dryness in the mouth are the criteria of sufficiency of atropine sulfate doseatropine sulfate dose..

Also reactivators of cholinesterase which renew activity of Also reactivators of cholinesterase which renew activity of this enzyme are administeredthis enzyme are administered – – dipyroxym, alloxym, dipyroxym, alloxym, isonitrosynisonitrosyn

Treatment of acute poisoningTreatment of acute poisoning

Depending on severity of poisoning Depending on severity of poisoning dipyroxymdipyroxym is introduced once or a few is introduced once or a few times.times. An average dose of the drug in An average dose of the drug in heavy cases isheavy cases is 3-4 3-4 ml of ml of 15 % 15 % solutionsolution. . The total dose ofThe total dose of alloxymalloxym is is 0,4-1,6 0,4-1,6 gg (0,075 (0,075 g every g every 1-3 1-3 hourshours).). If necessary If necessary - artificial ventilation should be - artificial ventilation should be performed to a patientperformed to a patient. . And after And after symptomatic treatment is carried onsymptomatic treatment is carried on..

Treatment of acute poisoningTreatment of acute poisoning

MM--cholinergic cholinergic drugsdrugs

MM--cholinomimeticscholinomimetics

MM--cholinoblockerscholinoblockers

MM--cholinomimeticscholinomimetics

Pilocarpini Pilocarpini hydrochloridumhydrochloridum

AceclidinumAceclidinum

Рilocarpini hydrochloridumРilocarpini hydrochloridumPharmacodinamicsPharmacodinamics

Contraction of pupil, improvement of outflow Contraction of pupil, improvement of outflow of intraocular liquid and relief intraocular of intraocular liquid and relief intraocular pressurepressureDilation of eye vesselsDilation of eye vessels

UsageUsage Treatment of glaucomaTreatment of glaucomaImprovement of eye nutrition in a case of Improvement of eye nutrition in a case of thrombosis of retinal central veinthrombosis of retinal central vein, , acute acute obstructionobstruction of retinal arteriesof retinal arteries, , optic nerveoptic nerve atrophy atrophy

Systemic (resorbtive) action of the drug is Systemic (resorbtive) action of the drug is not used because of its high toxicitynot used because of its high toxicity. . The The most dangerous manifestation of poisoning most dangerous manifestation of poisoning with pilocarpinum is edema of lungswith pilocarpinum is edema of lungs

Pilocarpine causes constriction of Pilocarpine causes constriction of pupils (myosis)pupils (myosis)

AceclidinumAceclidinumPharmacodinamics Pharmacodinamics

Miosis, decrease of intraocular pressure, Miosis, decrease of intraocular pressure, spasm of accomodationspasm of accomodation Increase of tonus and peristalsis of smooth Increase of tonus and peristalsis of smooth muscles of digestive tract organs, urinary muscles of digestive tract organs, urinary bladderbladder Increase of tonus of uterus and bronchial Increase of tonus of uterus and bronchial musclesmuscles

UsageUsage treatment of glaucomatreatment of glaucoma prophylaxis and treatment of postoperative prophylaxis and treatment of postoperative atony of stomach, intestines, urinary bladderatony of stomach, intestines, urinary bladder stopping of stopping of post delivery uterus bleedingspost delivery uterus bleedings

The drug is contraindicatedThe drug is contraindicated in case of in case of bronchial asthma, pregnancy, ischemic bronchial asthma, pregnancy, ischemic

heart diseaseheart disease

Clinical signesClinical signes diarrhea, stomachachediarrhea, stomachache contraction of pupilscontraction of pupils, , disorders of accomodationdisorders of accomodation increasing of salivation, vomitingincreasing of salivation, vomiting disorders of breathing because of bronchial spasmdisorders of breathing because of bronchial spasm confusionconfusion, consciousness, seizures, coma, consciousness, seizures, coma

TreatmentTreatment measures for organism purifying form poisonmeasures for organism purifying form poison intravenous introduction ofintravenous introduction of 0,1 % 0,1 % Atropine sulfate Atropine sulfate solutionsolution – 2 – 2 ml everyml every 10 10 min.min. ( (until appearance of until appearance of dryness in mouth and dilation of pupilsdryness in mouth and dilation of pupils)) symptomatic treatmentsymptomatic treatment

Acute poisoningAcute poisoning with substances of M-cholinomimetic actionwith substances of M-cholinomimetic action

(overdosing of drugs, (overdosing of drugs, consumption consumption of of mushrooms of Inocibe family)mushrooms of Inocibe family)

mushrooms of Inocybe familymushrooms of Inocybe family

MM--cholinoblockerscholinoblockers

Atropine sulfateAtropine sulfate Scopolamine hydrobromideScopolamine hydrobromide Platyphyllin hydrotartratePlatyphyllin hydrotartrate

MetacinumMetacinum Dry extract of Belladonna Dry extract of Belladonna

Pharmacokinetics and usage of M-Pharmacokinetics and usage of M-cholinoblockerscholinoblockers

Influence on an eyeInfluence on an eyeDilation of a pupilDilation of a pupil ( (midriasismidriasis))

Increasing of intraocular pressureIncreasing of intraocular pressure

Paralysis of accomodationParalysis of accomodation ( (cycloplegiacycloplegia))

Midriasis and cycloplegiaMidriasis and cycloplegia stay forstay for: : atropineatropine – 7-11 – 7-11 daysdays, , gomatropinegomatropine – 1-2 – 1-2 daysdays, , platyphyllinplatyphyllin – 5-6 – 5-6 hourshours,,

scopolaminescopolamine – 4-5 – 4-5 daysdays

UsageUsageInvestigation of orbital Investigation of orbital fundum fundum (posterior chamber of (posterior chamber of

eye)eye)

Prevention of sPrevention of syynechia (comissures) nechia (comissures) in case of trauma in case of trauma and operations on eyeand operations on eye

ContraindicationContraindicationglaucomaglaucoma

Pharmacodynamics and usage of Pharmacodynamics and usage of M-cholinoblockersM-cholinoblockers

PharmacodynamicsPharmacodynamics Decreasing of function of excretory glandsDecreasing of function of excretory glands, , except mammal except mammal

glandsglands Decreasing of tonus and peristaltic of smooth muscles of Decreasing of tonus and peristaltic of smooth muscles of

digestive tract, bronchi, urinary tractdigestive tract, bronchi, urinary tract

UsageUsage Ulcer disease of stomach and duodenum Ulcer disease of stomach and duodenum

((gastrocepingastrocepin)) Liver, renalLiver, renal, , intestinal colicsintestinal colics

Dyskinesias of gastrointestinal tract, enteritis, colitisDyskinesias of gastrointestinal tract, enteritis, colitis CystitisCystitis

Bronchial spasmBronchial spasm ( (IpratropiiIpratropii bromidebromide - - atroventatrovent))

Other cases of M-cholinoblockers Other cases of M-cholinoblockers administrationadministration

Holding of atropine test in case of Holding of atropine test in case of atrioventricular blockadeatrioventricular blockade ((atropineatropine))

In anesthesiologia for premedicatoinIn anesthesiologia for premedicatoin – – forfor prevention of prevention of bronchial and laryngeal spasmbronchial and laryngeal spasm, , syncopesyncope, , limitationlimitation of salivary and bronchial of salivary and bronchial glands secretionglands secretion ((atropine, scopolamine, atropine, scopolamine, metacinummetacinum))

Poisoning with M-cholinomimetics and POCPoisoning with M-cholinomimetics and POC ((atropineatropine))

SeasicknessSeasickness ( (scopolamine, aeronumscopolamine, aeronum))

GastrozepinGastrozepin (Gastrocepinum) (Gastrocepinum)

Side effects of M-chlinoblockersSide effects of M-chlinoblockers Dryness of mucous membranes, dysphagia, Dryness of mucous membranes, dysphagia,

dysphoniadysphonia TachycardiaTachycardia Increasing of intraocular pressure, glaucoma Increasing of intraocular pressure, glaucoma

attackattack Constipation,Constipation, retention of urine (ischuria) retention of urine (ischuria) Formation of bronchial plugs in patients with Formation of bronchial plugs in patients with

bronchial asthmabronchial asthma OverheatingOverheating

M-cholinoblockers are absolutely M-cholinoblockers are absolutely contraindicated in patients with glaucomacontraindicated in patients with glaucoma

Acute poisoning with substances Acute poisoning with substances of M-cholinoblocking actionof M-cholinoblocking action

CausesCauses

Overdosing with drugs of Overdosing with drugs of M-cholinoblockers group M-cholinoblockers group

Consumption of plants, which include Consumption of plants, which include alcaloids of this group alcaloids of this group

BelladonnaBelladonna

Datura stramoniumDatura stramonium

“ “Atropine psychosisAtropine psychosis”: ”: delirium, hallucinations, delirium, hallucinations, disorientation, psychomotor excitement disorientation, psychomotor excitement Redness and dryness of skin, increasing of body Redness and dryness of skin, increasing of body temperaturetemperature Dryness of mucous membranes causes disorders of Dryness of mucous membranes causes disorders of swallowing (dysphagiaswallowing (dysphagia), ), speechspeech ( (dysartria,dysartria, raleness of raleness of voice voice)) ThirstThirst Quick Quick dilation of pupils (midriasis)dilation of pupils (midriasis) PhotophobiaPhotophobia Visus disordersVisus disorders ( (Paralysis of accomodationParalysis of accomodation)) TachycardiaTachycardia Atony of intestinesAtony of intestines Retention of urineRetention of urine

Death is caused by paralysis of breath Death is caused by paralysis of breath centercenter

Symptoms of acute poisoning with Symptoms of acute poisoning with M-cholinoblockersM-cholinoblockers

wash out of stomach withwash out of stomach with 0,5 % 0,5 % Tannin Tannin solutionsolution, laxative agents, , laxative agents, sorbentssorbents, , forced diuresis forced diuresis

Specific antagonistsSpecific antagonists – – anticholinesterase anticholinesterase drugsdrugs: repeated : repeated introduction ofintroduction of proserinum, proserinum, galantaminum, hydrobromidumgalantaminum, hydrobromidum until symptoms of until symptoms of didissappearance appearance of M-cholinoblockersof M-cholinoblockers blockadeblockade

removal of removal of psychomotor excitement psychomotor excitement - - aminasinum, sybazon, barbituratesaminasinum, sybazon, barbiturates

removal removal of tachycardiaof tachycardia – – anaprylineanapryline forfor relief relief of photophobia patient is put to a dark of photophobia patient is put to a dark

roomroom for decreasing of body temperaturefor decreasing of body temperature ice-cube ice-cube

bottles are placed around the patientbottles are placed around the patient In case of considerable depressing of breathing - In case of considerable depressing of breathing -

artificial ventilation with oxygen inhalationartificial ventilation with oxygen inhalation

TREATMENT OF ACUTE POISONING WITH TREATMENT OF ACUTE POISONING WITH M-CHOLINOBLOCKERSM-CHOLINOBLOCKERS

N-cholinergic N-cholinergic drugsdrugs

NN--cholinomimeticscholinomimetics

CytitonCytiton

Lobelin hydrochlorideLobelin hydrochloride

CytitonCytiton

PharmacodynamicsPharmacodynamics increases tone of respiratory center of increases tone of respiratory center of medulla oblongata reflectivelymedulla oblongata reflectively increases arterial pressure due to reflective increases arterial pressure due to reflective excitation of vascular-motor centerexcitation of vascular-motor center

UsageUsage respiratory arrest due to inhalation of respiratory arrest due to inhalation of irritative substancesirritative substances,, traumas, electro-shock, surgical operationstraumas, electro-shock, surgical operations morphine and CO poisoningmorphine and CO poisoning shock and collapse conditions, depression of shock and collapse conditions, depression of blood circulation and breathing in patients blood circulation and breathing in patients with infectious diseaseswith infectious diseases

Clinical pictureClinical picture nausea, vomiting, salivationnausea, vomiting, salivation,, abdominal pain, diarrheaabdominal pain, diarrhea,, dizzinessdizziness,, headacheheadache,, cold sweat, weaknesscold sweat, weakness,, loosing of consciousnessloosing of consciousness,, tachytachy- - or bradycardiaor bradycardia,, cardiac arrhythmiascardiac arrhythmias,, seizuresseizures,, breathing depressionbreathing depression

Death is caused by sharp depression of Death is caused by sharp depression of respiratory center and paralysis of breathing respiratory center and paralysis of breathing musculaturemusculature

Acute poisoning with nicotineAcute poisoning with nicotine

Chronic diseases of respiratory systemChronic diseases of respiratory system, , Lung cancer and Malignant tumors of other Lung cancer and Malignant tumors of other localisationlocalisation,,Ischemic heart diseaseIschemic heart disease,,Obliterating endarteritisObliterating endarteritis, , Gastric and duodenal ulcer diseaseGastric and duodenal ulcer disease

WomenWomenDepression of female sex hormones Depression of female sex hormones production, yellow face, early wrinkles, production, yellow face, early wrinkles, damaging of teeth, harsh voice, sometimes damaging of teeth, harsh voice, sometimes male type hair growthmale type hair growth

MenMenDeep, nonreversible changes of Deep, nonreversible changes of spermatozoidsspermatozoids

Chronic poisoning with nicotineChronic poisoning with nicotine

N-cholinoblockersN-cholinoblockers

GanglionblockersGanglionblockers Benzohexonium, pentamin, Benzohexonium, pentamin,

hyhronium, pyrilenhyhronium, pyrilen

MyorelaxantsMyorelaxants Tubocurarine chloride, dithylin, Tubocurarine chloride, dithylin,

mellictinmellictin

GanglionblockersGanglionblockers

PHARMACODYNAMICSPHARMACODYNAMICS

Dilation Dilation of peripheralof peripheral vesselsvessels Decreasing ofDecreasing of blood pressureblood pressure Decreasing ofDecreasing of smooth musculature smooth musculature tonetone of internal organsof internal organs ( (bronchi, GI bronchi, GI tract, urinary and bile tractstract, urinary and bile tracts))

Decreasing of Decreasing of glandular secretionglandular secretion: : bronchial, gastric, salivarybronchial, gastric, salivary

BenzohexoniumBenzohexoniumDoes nor penetrate through hemato-Does nor penetrate through hemato-encephalic (blood-brain) barrierencephalic (blood-brain) barrier..Duration of action varies from 3 to 6 hoursDuration of action varies from 3 to 6 hours

UsageUsageHypertensive crisisHypertensive crisisGuided (controlled) hypotoniaGuided (controlled) hypotoniaObliterating endarteritis Spasm of peripheral vessels Intestinal, hepatic, kidney colicsIntestinal, hepatic, kidney colicsGastric ulcerGastric ulcerBronchial asthma, lung emphysema, Bronchial asthma, lung emphysema, lung edemalung edema

PentaminumPentaminumDuration of action–Duration of action– 2-4 2-4 hours hours

UsageUsage

Hypertensive crisisHypertensive crisisObliterating endarteritisObliterating endarteritis Spasm of peripheral vesselsSpasm of peripheral vessels Intestinal, hepatic, nephral colicIntestinal, hepatic, nephral colicGastric ulcerGastric ulcerBronchial asthma, lung emphysemaBronchial asthma, lung emphysema

HygroniumHygroniumEffect develops after Effect develops after 2-3 2-3 minmin, , and and lasts forlasts for 10-15 10-15 min after stopping of min after stopping of infusioninfusion

UsageUsageFor controlled hypotoniaFor controlled hypotoniaFor treatment of nephropathy and For treatment of nephropathy and eclampsiaeclampsiaFor complex therapy of hypertensive For complex therapy of hypertensive crisis, brain edema, lung edemacrisis, brain edema, lung edema

Side effects and complicationsSide effects and complications of ganglioblockers’ administrationof ganglioblockers’ administration

Orthostatic collapseOrthostatic collapseDryness of mucous membranesDryness of mucous membranes

Disturbance of accomodationDisturbance of accomodationGeneral weaknessGeneral weakness

DizzinessDizzinessTachycardiaTachycardia

Atonia of urinary bladder, intestinesAtonia of urinary bladder, intestines ((paralytic ileusparalytic ileus) )

Myorelaxants Myorelaxants

Antidepolarizing type of Antidepolarizing type of actionaction ( (pachicurarepachicurare) )

Tubocurarine chloride, Tubocurarine chloride, anatruxonium, pipecuronium anatruxonium, pipecuronium

bromide, mellictinbromide, mellictin

Depolarizing type of Depolarizing type of actionaction ( (leptocurareleptocurare))

dithylinumdithylinum

Sequence of relaxation of Sequence of relaxation of striped musclesstriped muscles

Small muscles of fingers,toes, Small muscles of fingers,toes, ears, eyes, head, neck, muscles ears, eyes, head, neck, muscles

of extremities, trunc,of extremities, trunc,

Intercostal muscles and Intercostal muscles and diaphragm diaphragm

Reviving of tone is performed in Reviving of tone is performed in reversed sequencereversed sequence

1

1

2

3

4 4

4 4

5

6

7

Tubocurarine chlorideTubocurarine chlorideRelaxation begins afterRelaxation begins after 1-1,5 1-1,5 min after min after

introduction and lasts forintroduction and lasts for 25-40 25-40 minmin

UsageUsage For prolonged relaxation of striped muscles For prolonged relaxation of striped muscles during surgical operationsduring surgical operations For relaxation of muscles while repositioning For relaxation of muscles while repositioning fractured bones and combined dislocationsfractured bones and combined dislocations For prevention of traumatic injuries during For prevention of traumatic injuries during seizure therapy of schizophrenia, during seizure therapy of schizophrenia, during epileptic status, seizures of other ethiology epileptic status, seizures of other ethiology (tetanus)(tetanus)

PROSERINE is introduced PROSERINE is introduced to abolish action of the drugto abolish action of the drug

DithylinumDithylinum

((suxamethonium, succinilcholin, suxamethonium, succinilcholin, listenonlistenon))

Myorelaxation develops afterMyorelaxation develops after 40-60 40-60 sec sec. . Total restoring of muscle tonus comes after Total restoring of muscle tonus comes after 5-10 5-10 minmin..

UsageUsage before such manipulations as before such manipulations as tracheal intubation, broncho- and tracheal intubation, broncho- and

esophagoscopia, cystoscopiaesophagoscopia, cystoscopia for reposition of bone fractures, for reposition of bone fractures,

dislocationsdislocations

Insufficiency of Insufficiency of buthyrilcholinesterasebuthyrilcholinesterase

((genetic pathologygenetic pathology))

In this pathology action of dithylinum can In this pathology action of dithylinum can last for several hours, and all this time the last for several hours, and all this time the

patient should be connected to artificial patient should be connected to artificial respiration devicerespiration device

TREATMENTTREATMENT Introduction of fresh-citrate blood Introduction of fresh-citrate blood Direct blood infusion from donnorDirect blood infusion from donnor

Introduction of buthyrilcholinesteraseIntroduction of buthyrilcholinesterase

MellictinMellictin

UsageUsage

For disease and syndrome of ParkinsonFor disease and syndrome of Parkinson, , postencephalitic parkinsonismpostencephalitic parkinsonism,,

disease ofdisease of LittleLittle,,

spinal arachnoiditisspinal arachnoiditis,,

arachnoencephalitisarachnoencephalitis

All myorelaxants are All myorelaxants are contraindicated for patients with contraindicated for patients with

myasteniamyastenia

ADRENERGIC ADRENERGIC DRUGSDRUGS

Adrenergic Adrenergic drugsdrugs

medical substances medical substances

which act in which act in adrenergic synapsesadrenergic synapses

Adrenergic synapsAdrenergic synaps

Smooth muscles of vesselsSmooth muscles of vessels::- skinskin- mucsous membranesmucsous membranes- mesentery mesentery , , - organs of abdominal cavityorgans of abdominal cavity- skeletal musclesskeletal muscles- coronarycoronary- lungslungs- kidneyskidneys- veinsveins

11

11

11 11

22

11

22

11

22

11

ДД11

1 1

Contraction of vesselsContraction of vessels - ’’ -- ’’ - - ’’ -- ’’ - - ’’ -- ’’ - - ’’ -- ’’ -Dilation of vesslesDilation of vesslesContraction of vesselsContraction of vesselsDilation of vesslesDilation of vesslesContraction of vesselsContraction of vesselsDilation of vesslesDilation of vesslesContraction of vesselsContraction of vesselsDilation of vesslesDilation of vesslesContraction of vesselsContraction of vessels

M dillatator pupillaeM dillatator pupillaeCiliary muscleCiliary muscleHeart Heart

11

22 11

Midriasis Midriasis ((dilation of pupildilation of pupil))Dilation Dilation ((far visionfar vision))Increasing of power and frequency of contractionIncreasing of power and frequency of contraction, , conductivity, conductivity,

automatism automatism

Bronchial musclesBronchial musclesBronchial glandsBronchial glands

22

11, , 22

Dilation of bronchiDilation of bronchiDecreasing of secretionDecreasing of secretion, , increasing of secretionincreasing of secretion

Smooth musculature of GI tractSmooth musculature of GI tract::- walls walls - - sphincters sphincters

22, , 22

11 Decreasing of toneDecreasing of tone, , peristaltic peristaltic Increasing of toneIncreasing of tone

Smooth musculature of urinary bladderSmooth musculature of urinary bladder::- wallswalls- sphincterssphincters

22

11

Relaxation Relaxation Contraction Contraction

Liver Liver 22Decomposition of glycogenDecomposition of glycogen

Uterus Uterus 11

22

Contraction Contraction Relaxation Relaxation ((pregnant>not pregnant)pregnant>not pregnant)

Salivary glandsSalivary glands 11

Increasing of Increasing of КК++ , , f amylasef amylase and and НН22ООsecretionsecretion

Sweat glandsSweat glands 11Increasing of secretionIncreasing of secretion

Insulin secretionInsulin secretion 22

Decreasing Decreasing Increasing Increasing

Presynaptic formations of adrenergic neuronsPresynaptic formations of adrenergic neurons 22

11

Decreasing of releasing of nor-adrenalin into synaptic splitDecreasing of releasing of nor-adrenalin into synaptic splitStimulation of releasing of nor-adrenalin into synaptic splitStimulation of releasing of nor-adrenalin into synaptic split

Presynaptic formations of cholinergic neuronsPresynaptic formations of cholinergic neurons 22Stimulation of releasing of acetyl-choline into synaptic splitStimulation of releasing of acetyl-choline into synaptic split

Typical localization of adrenal receptors and changes of functions observed during stimulation of these receptorsTypical localization of adrenal receptors and changes of functions observed during stimulation of these receptors

Adrenomimetics Adrenomimetics а) а) adrenomimetics of direct adrenomimetics of direct

actionaction б) б) adrenomimetics of indirect adrenomimetics of indirect

actionaction or sympathomimeticsor sympathomimetics

Adrenoblockers Adrenoblockers or adrenolyticsor adrenolytics

Sympatholytics Sympatholytics

І. І. Adrenomimetics Adrenomimetics 1.1. - і - і --adrenomimeticsadrenomimetics ( (adrenalin hydrochlorideadrenalin hydrochloride, ,

noradrenalin hydrotartratenoradrenalin hydrotartrate))2. 2. dopaminedopamine-, -, -, -, --adrenomimeticsadrenomimetics (dopamine)(dopamine)3. 3. --adrenomimeticsadrenomimetics ( (mesatonemesatone, , naftizinnaftizin, , galazolinegalazoline))4. 4. --adrenomimeticsadrenomimetics ( (isadrineisadrine, , salbutamolsalbutamol, ,

phenoterolphenoterol, , terbutalinterbutalin, , dobutaminedobutamine))ІІ.ІІ. Sympathomimetics Sympathomimetics ((ephedrineephedrine))ІІІ. ІІІ. AdrenoblockersAdrenoblockers 1. 1. --adrenoblockersadrenoblockers ( (phentolaminephentolamine, , tropaphentropaphen, ,

prasosineprasosine, , pyroxanpyroxan))2.2. --adrenoblockersadrenoblockers ( (anaprilinanaprilin, , athenololathenolol,, talinolol talinolol, ,

acebutololacebutolol))3. 3. - і - і --adrenoblockersadrenoblockers ( (labetalollabetalol))ІІІ. ІІІ. SympatholyticsSympatholytics ((reserpine, octadinereserpine, octadine))

Adrenomimetics Adrenomimetics

Adrenalin (epinephrineAdrenalin (epinephrine)) is a is a hormone of medulla of suprarenal glands which hormone of medulla of suprarenal glands which

is used in a form of a remedyis used in a form of a remedy

adrenaline hydrochlorideadrenaline hydrochloride

It is an adrenomimetic which stimulates It is an adrenomimetic which stimulates

11,- ,- 22-- and and 11,- ,- 22--adrenoreceptorsadrenoreceptors

Administration Administration Cardiac arrest,Cardiac arrest, for examplefor example, , during surgical during surgical

general anesthesia, electric trauma general anesthesia, electric trauma shock (shock (anaphylactic shockanaphylactic shock) and collapse ) and collapse

of different origineof different originebronchial spasmbronchial spasm

hypoglycemic comahypoglycemic coma treatment of open-angle glaucomatreatment of open-angle glaucoma

Noradrenalin hydrotartrateNoradrenalin hydrotartrate ((norepinephrinenorepinephrine))

Is an adrenomimetic of direct action which Is an adrenomimetic of direct action which stimulates stimulates 11-, -, 22- - andand 11--adrenal receptorsadrenal receptors

Administration Administration in cases of acute decreasing of blood in cases of acute decreasing of blood

pressure - shock and collapse conditions, pressure - shock and collapse conditions, surgeries, traumassurgeries, traumas

The drug is absolutely contraindicated The drug is absolutely contraindicated for subcutaneous and intramuscular for subcutaneous and intramuscular

introductionsintroductions

NecrosisNecrosis

Dopamine Dopamine

Drug of a first Drug of a first

choice for treatment of choice for treatment of

shock and collapseshock and collapse of different aetiology, including of different aetiology, including

cardiogenic and hemorrhagiccardiogenic and hemorrhagic

Mesaton Mesaton ((phenylefrinphenylefrin))Is a syntheticIs a synthetic a a11--adrenomimetic drug of direct actionadrenomimetic drug of direct action

Administration Administration acute hypotensive conditionsacute hypotensive conditions,, prophylaxis of decreasing of blood pressure prophylaxis of decreasing of blood pressure in case of infectious diseases, poisoningsin case of infectious diseases, poisonings,,

decreasing of blood pressure during decreasing of blood pressure during narcosis with halothan and cyclopropannarcosis with halothan and cyclopropan

nose drops in case of rhinitisnose drops in case of rhinitis

NaphthysinNaphthysin

XylometazolinXylometazolinareare a a22--adrenomimetics of direct adrenomimetics of direct

actionaction

Usage Usage for rhinitis in a form of nose drops – for rhinitis in a form of nose drops –

1-21-2 dropsdrops 2-3 2-3 times a daytimes a day

It is not recommended for It is not recommended for

chronic coldchronic cold

NAPHAZOLINNAPHAZOLIN

Isadrin Isadrin ((isoprenalinisoprenalin, , novodrinnovodrin, , euspiraneuspiran) )

– – is a synthetic katecholamineis a synthetic katecholamine, , which is a strong which is a strong stimulant ofstimulant of ββ11- і - і ββ22--adrenoreceptorsadrenoreceptors

Administration Administration bradycardiabradycardia, , atrio-ventricular blockadeatrio-ventricular blockade bronchial spasmbronchial spasm complex therapy of some kinds of shockcomplex therapy of some kinds of shock ( (if the if the patient doesn’t have hypovolemiapatient doesn’t have hypovolemia))

Side effectsSide effects nausea, hands tremornausea, hands tremor, , dry mouthdry mouth,, in patients with ischemic heart diseasein patients with ischemic heart disease – – acute acute ischemic attackischemic attack,, heavy cardiac tachyarrhythmiasheavy cardiac tachyarrhythmias, , even fibrillation even fibrillation of ventriclesof ventricles

SalbutamolSalbutamol ((ventolinventolin))

selective selective bb22--adrenomimetic adrenomimetic of direct actionof direct action

Administration Administration inhalations during attacks inhalations during attacks of bronchial asthma and of bronchial asthma and bronchial spasms of other bronchial spasms of other etiologyetiology premature child deliverypremature child delivery, , rapid (vigorous) child rapid (vigorous) child deliverydelivery

Terbutalin Terbutalin ((brikanilbrikanil) ) and and phenoterolphenoterol ( (berotekberotek, , partusistenpartusisten))

are stimulants of mostlyare stimulants of mostly 22--adrenal adrenal receptors. They posses broncholytic and receptors. They posses broncholytic and

tokolytic activitytokolytic activity

Dobutamin Dobutamin

Is a synthetic Is a synthetic 11--adrenomimeticadrenomimetic

Cardiotonic effects of Cardiotonic effects of dobutamin is 5 times dobutamin is 5 times

stronger than action of stronger than action of dopamine dopamine

AdministrationAdministrationsome forms of acute and some forms of acute and

chronic cardiac insufficiencychronic cardiac insufficiency intravenous dropping intravenous dropping

infusion with the speed ofinfusion with the speed of

2,5-10 2,5-10 mcg mcg // ((kgkg..minmin) )

Sympathomimetics Sympathomimetics

Ephedrine hydrochlorideEphedrine hydrochloride (Ephedrini hydrochloridum) (Ephedrini hydrochloridum)

It is an alkaloid of plants ofIt is an alkaloid of plants of Ephedra familyEphedra family, , which which has indirect has indirect αα-, -, ββ--adrenomimeticadrenomimetic ( (sympathomimeticsympathomimetic) ) actionaction

Administration Administration collapse conditions, for prophylaxis of decreasing collapse conditions, for prophylaxis of decreasing of blood pressure before spinal anesthesiaof blood pressure before spinal anesthesia,, infectious infectious diseasesdiseases treatment of rhinitistreatment of rhinitis (2 %, 3 % (2 %, 3 % solution as nose solution as nose dropsdrops).). prophylaxis and elimination of bronchial spasm prophylaxis and elimination of bronchial spasm ((inhalationsinhalations 0,5 %-1 % 0,5 %-1 % solutions of drugsolutions of drug))

SIDE EFFECTSSIDE EFFECTS agitation,agitation, excitementexcitement, , tremortremor, , inconsiderable euphoriainconsiderable euphoria, , insomniainsomnia, , seizuresseizures drug addictiondrug addiction tachyphylaxytachyphylaxy

Adrenoblockers Adrenoblockers

Alfa-Alfa-adrenoblockersadrenoblockers

PhentolaminePhentolamine, , tropaphentropaphenare syntheticare synthetic 11, , 22-а-аdrenoblockersdrenoblockers

administrationadministration diagnostics and symptomatic diagnostics and symptomatic treatment of feochromocytomatreatment of feochromocytoma disturbances of peripheral blood disturbances of peripheral blood circulationcirculation in case of endarteriitis, in case of endarteriitis, Reino’s diseaseReino’s disease,, trophic ulcers, decubitus trophic ulcers, decubitus complex treatment of hypertensive complex treatment of hypertensive crisescrises,, acute cardiac insufficiency acute cardiac insufficiency complex therapy of hypovolemic and complex therapy of hypovolemic and cardiogenic shockcardiogenic shock

Prasosin Prasosin

SelectiveSelective 11-- adrenoblocker adrenoblocker

Administration Administration treatment of arterial hypertensiontreatment of arterial hypertension

Side effectsSide effects““phenomenon of first dosephenomenon of first dose”: ”: sudden sudden decreasing of blood pressure and even decreasing of blood pressure and even development of orthostatic collapse after development of orthostatic collapse after first administrations of the drugfirst administrations of the drug

ProphylaxisProphylaxis: : administration of half-dose administration of half-dose before sleepbefore sleep

Beta-Beta-adrenoblockersadrenoblockers

Anaprilin Anaprilin Is aIs a ββ11- і - і ββ22--adrenoblockeradrenoblocker

Administration Administration ischemic heart diseaseischemic heart disease arterial hypertensionarterial hypertension

cardiac tachyarrhythmiascardiac tachyarrhythmias acute myocardium infarctionacute myocardium infarction

Talinolol or cordanumTalinolol or cordanum

is a cardioselectiveis a cardioselective

ββ--adrenoblockeradrenoblocker

AdministrationAdministration disorders of cardiac rhythmdisorders of cardiac rhythm ((extrasystoliesextrasystolies,, paroxysmal paroxysmal tachycardiatachycardia, , fibrillation and fibrillation and scintillation of atriascintillation of atria)) ischemic heart diseaseischemic heart disease arterial hypertensionarterial hypertension

..

Atenolol Atenolol ((tenormin)tenormin)cardioselelctivecardioselelctive --adrenoblocker with long adrenoblocker with long

duration of actionduration of action

Indications for Indications for administrationadministration

ischemic heart diseaseischemic heart disease arterial hypertensionarterial hypertension cardiac arrhythmiascardiac arrhythmias

acute myocardium infarctionacute myocardium infarction

Acebutolol Acebutolol ((sectralsectral))11--adrenoblocker with inner adrenoblocker with inner sympathomimetic activitysympathomimetic activity

IndicationsIndications disorders of cardiac rhythm disorders of cardiac rhythm (tachyarrhythmias(tachyarrhythmias)) hypertensionhypertension ischemic heart diseaseischemic heart disease

Labetolol Labetolol

-, -, --adrenoblockeradrenoblocker. . The drug blocksThe drug blocks 11, , 22, , 1 1 andand 22--adrenoreceptorsadrenoreceptors

Administration Administration treatment of patients with arterial treatment of patients with arterial

hypertensionhypertension hypertensive crisishypertensive crisis

ContraindicationsContraindications Atrio-ventricular blockadeAtrio-ventricular blockade,,

cardiac insufficiencycardiac insufficiency

CARVEDILOL, NEBIVOLOLCARVEDILOL, NEBIVOLOL

increase the production of NO in increase the production of NO in blood vesselsblood vessels

are used now for chronic cardiac are used now for chronic cardiac insufficiency (congestive heat insufficiency (congestive heat

failure)failure)

SympatholyticsSympatholytics

ReserpinReserpinis a sum of Rauvolfia (plant) alkaloidsis a sum of Rauvolfia (plant) alkaloids. . Maximal hypotensive actionMaximal hypotensive action developsdevelops afterafter 5-7 5-7 daysdays of regular administration of the drugof regular administration of the drug. . After the After the treatment coarsed effect can still stay for two weekstreatment coarsed effect can still stay for two weeks..

Administration Administration treatment of different forms of essential hypertensiontreatment of different forms of essential hypertension(drugs of a second row, second line)(drugs of a second row, second line) ((combined drugs trirezidcombined drugs trirezid, , cristepincristepin, , adelfanadelfan, , brinerdinbrinerdin))

Side effectsSide effects manifestations of parkinsonismmanifestations of parkinsonism fatiguefatigue, , somnolencesomnolence, , depressiondepression,, bradycardiabradycardia increasing of motor and secretory activity of increasing of motor and secretory activity of gastro-intestinal tractgastro-intestinal tract, , acute attacks of ulcer diseaseacute attacks of ulcer disease, , diarrheadiarrhea swelling of nose mucous membrane with swelling of nose mucous membrane with complication of nose breathingcomplication of nose breathing

Octadin Octadin Is a sympatholytic with strong hypotensive effectIs a sympatholytic with strong hypotensive effect. . During administration of the drug decreasing of blood During administration of the drug decreasing of blood pressure develops graduallypressure develops gradually, , afterafter 2-3 2-3 daysdays. . After After abolition of drug administration the effect still stays forabolition of drug administration the effect still stays for 2 2 weeksweeks..

Administration Administration heavy forms of arterial hypertensionheavy forms of arterial hypertension

Side effectsSide effects general weaknessgeneral weakness,, nauseanausea, , vomitingvomiting,, swelling of nose mucous membraneswelling of nose mucous membrane,, diarrheadiarrhea,, liquid retention in the organism,liquid retention in the organism, orthostatic collapseorthostatic collapse