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Side effects

Acetylecholine(Pharmacological actions)

Organ

Bradycardia

-Bradycardia(depressS.A.node-veChronotopic effect*&-Depression of forces of Myocardialcontractility*-veInotropic effect*&                    SlowingA-Vconductingsystem(A.Vnode,A.Vbundle)-veDronotropic effect*

C.V.S

_Heart(Muscarinic Receptor)

 

 

 

 

Hyperacidity&nausea

Vomiting-Abdominal cramps

-Anorexia-diarrhea

 

Increase Tone&Motility&Increase Gastric –Pancreatic-Intestinal secretions

Smooth muscles(M3)receptors

 

-GIT

Urination

Contraction ofDetrusormuscle&Relaxation of VesicalSphincter(Urination)

 

-Urinary tract

Hypotension

Vasodilatation (Hypotension)dueto decreaseofPeripheral vascular resistance*P.V.R*:ArterialBlood Pressure=P.V.R*H.R*Stroke volume&&Stroke volume=(volumeofbloob/1beat)&&C.O.P(Volumeof blood)&&Mean Arterial blood pressure=PVR*COP&&A.CH*decreasesPVR*main factor in decreasing BL.P*

 

-Blood vessels

Bronchoconstriction&cough

Bronchoconstriction&&Increase Bronchialsecretions

 

-Respiratorytract

 

 

Iris circular smooth muscles contraction causing Miosis*DecreasePupilsize*Accommodation to near Vission*&                                                     &Decrease I.O.P*Drainage ofAqueousHumur viaCanalof Schlem*&Contraction ofCiliary body responsible forAccomodation*near vision*&Noeffect of Light reflex *As A.CH causes already miosis(Eyes respond to Light by Miosis)

-Eye

Increasing all body secretions

Increase(Lacrimal &Salivary&Sweat&Bronchial&Gastric&Pancreatic&Intestinal)secretions

Exocrine Glands(Muscarinic receptors)

 

Initial stimulation followed by depression

CNS(Muscarinic receptors)

 

 

A.CH causes(transiet brief depolarization*Tetanic contraction*&A.CH+Eserine* results in A.CHaccummulation&Persistent depolarization*(Initial muscle contraction*fasiculations* followed by relaxation or paralysis*flaccidity* *Desensitization of Nicotinic receptors toA.CH effect*_____Prolonged relaxation

 

Skeletal muscles(Nicotinic receptors)

 

-Smpathetic Ganglia *NErelease*-AdrenalGland*NE,EP*release which inturn causesHypertension*A.CH REVERSAL*

 

Autonomic Ganglia&Adrenal medulla(Nicotinic receptors)

 

Contraindications of Parasympathomimetics

-Peptic ulcer

-Bronchial asthma

-Brady cardia

                                                                                                                             -Anginapectoris

-Hyperthyroidism

-AV block

-Bleeding

 

 

 

Cholineesters(like Acetylecholine)e.g

-Methacholine{Purely muscarinic with serious side effects onHeart never givenI.V&&TTT-Glaucoma-Paroxysmal auricular Tachycardia-Urinaryretention-GIatony-Paralyticileus*complete loss of GIperistalsis-Abdominaldistension}

-Carbachol{nonselective-long duration-dangerous –given topically in Glaucoma}

-Bethanechol{stable against Cholineesterase-purelymuscarinicwith selectivityon GIT&UT}

-Pilocarpine{Naturalalkaloid –strong musarinicwith mild nicotinic activity-1st choice forGlaucoma-Diaphoreticin cases of Anhydrosis-Increases saliva followingIrradiation therapy}

Indirectly-acting Parasympathomimetics

a)Revesible Choline esterase enzyme inhibitors(Prevents A.CHhydrolysis by cholinesterase for short period*2-8*hours)

1)-Physostigmine*Eserine*{3ry amine-nonionized-readily absorbed fromGIT-causes severe Myocardialdepression(Direct&indirect)-applied topically in Glaucoma}

2)-Neostigmine{4ryamine-ionized-poorly absorbed-directstimulanteffecton Skeletal muscles+indirect effect viaA.CH-TTTmuscle weakness associatingMyastheniagravis-Glaucoma&D-tubocurarine poisoning}

3)-Edrophonium{shortacting*20minutes*-direct&indirect stimulanteffect on Skeletalmuscles-Diagnosis ofMyastheniagravis&D-tubocurarinepoisoning}

Myastheniagravis tttby*Pyridostigmine-Ambenonium*

 

b)-IrreversibleCholineesteraseinhibitors(Inhibit Cholineesterasefor days&weeks)

organophosphorous compounds

*Isofluorophate-Echothiophate(topically tttGlaucoma)*

*Prodrugs*Parathion&Malathion(byL.M.E)Converts into active form*Paroxon&Maloxon*{They are highly lipid soluble-highly absorbed reaching all body tissuesevenBrain causing convulsions*stimulation* followed byRespiratory-Vasomotor centers depression-causing high A.CH levels resulting in Excessive*Muscarinic-Nicotinic effects*

-Main causes of Death*Peripheral&CentralRespiratory failure*-Shock(Hypotension-decreased C.O.P-VMcenter depression.

 

TTT ofOrganophosphorous toxicity

-Artificial Respirationwith Oxygen.

-SpecificAntidotes(Atropine I.V. till fullMydriasis

-Pralidoxime*Cholineesterase Reactivator*-used within 24hrs I.Vbefore Aging occurs

-Symptomatic ttt(fluids-suction of bronchial secretions-Diazepam for convulsions)

Parasympatholytics

1)Muscarinic antagonists(Atropine&Scopolamine)

(3ryamine –well absorbed reaching all tissues even CNScausing stimulation followed bydepression-Comprtitive inhibitor ofA.Chat Muscarinic receptors-causes*Tachycardia proceeded by brief period of Bradycardia duetoVagalstimulation-no effect on bloodvessels-Eye passiveMydriasis*increaseI.O.P*Cycloplegia(Loss of accommodation)*Loss of Lightreflex*NoMiosis*-V.M&Respiratory centers depression-Bronchodilator-decrease bronchial secretions-*0,5-4mg(CNS STIMULANT)*above4mg*CNSdepressant*

Therapeutic uses

-Examination of Eye Fundus(Ophthalmic Examination) in ocular diseases-Used alternatively with Eserine to remove Adhesionbetween IRIS&LENSES(SelectiveTropicamide-Cyclopentolate-Piperiodolate-Eucatropine*shorter mydriatic withoutCycloplegia-Homatropine*shorter mydriatic with Cycloplegia*

-Peptic ulceration*SelectivePirenzpine-Telenzepine*M1blockers

-Antispasmodic*Amprotropine-Oxyphonium-Propantheline-Methantheline-Banthine-Hyoscine*sedative*-Methylscopolamine*

-Bronchial asthma(Bronchodilator*Ipratropium bromide-Tiotropium bromide*without Dryness ofBronchial secretions

-Antiparkinsonian*Benzotropine-Trihexiphenidyl-Biperidin-Cycrimine*

-Preanaesthesia(drying effect-inhibit the inhibitory effect ofGeneral anaesthetics on C.V reflexes

-Antidote forpoisoning with(AllParasympathomimetics*Carbamates-Organophosphorous cpds-D-TC-

-TTT of Motion sickness

-Treatment of Travellers diarrhea.

 

 

SIDE EFFECTS

(ESP.Atropine flush or Fever-Blurring of vision-CNS irritability&insomnia-Urinary retention-Anhydrosis*nosweating*Flushing*-Dryness of mouth)

Contraindications ofAtropine

-Glaucoma-Organic heart disease*CHF-Hypertension*-GIatony-ParalyticIleus-Intestinal obestruction-Constipation-Urinary retention-Tachycardia-Pyloricstenosis-Elders with Prostatic Hypertrophy)

Nicotinic receptor blockers{Skeletal muscle relaxant)

-Centrally acting(ttt muscle spasm*Antispasticity*(Block mono&polysynapticpathways inBrain&Spinalcord)e.g*Baclofen-Dantrolene-Diazepam*

-Peripheraly acting(onSkeletalmuscles&N.M.J)-*INTERRUPTchemical transmission in the Somatic motor nerve**Neuromuscular blockers**

a)-Competitive*Nondepolarizing* ofA.Chat Motorendplate e.g*D-tubocurarine&Gallamine*Flaxidil*&Pancuronium&Vecuronium-Atacuronium-Alcuronium.

b)-Noncompetitive*Depolarizing*(Initial depolarization*muscle contraction*followed by relaxation)e.g*Succinylcholine*Decamethonium*

a&b are used in Preanaesthetic Medication&also with Atropine

Choline esterases* Hydrolysis of Choline esters*

Types

a)_True type*typeI*Hydrolysis of Acetylecholine only present in

-All Autonomic sites in which A.CHacts as neurochemicaltransmitter&N.M.J

-CNS*basalganglia*Renshaw cell*

b)-Pseudo type*typeII*(Butyrylcholineesterase) present in

-Plasma&GIT&RBCS

 

 

 

 

 

Muscle relaxant

A muscle relaxant is a drug which decreases the tone of a muscle. See also Neuromuscular-blocking drugs.

Central acting muscle relaxants

-Benzodiazepines"Diazepam" &Methocarbamol

Unclassified

Here are several other skeletal muscle relaxants which may belong in the above categories:

-Baclofen &Carisoprodol &Chlorzoxazone

-Cyclobenzaprine &Dantrolene &Metaxalone

-Orphenadrine &Pancuronium &Tizanidine

Acting on smooth muscle

Dicyclomine

Other

Drugs from classes other than the muscle relaxant class are also used to treat spasticity:

-Clonidine &Gabapentin

Muscle relaxants (M03) edit

Peripherally acting:

Alcuronium, Atracurium, Cisatracurium, Dimethyltubocurarine, Doxacurium chloride, Fazadinium bromide, Gallamine, Hexafluronium, Mivacurium chloride, Pancuronium, Pipecuronium bromide, Rocuronium bromide, Suxamethonium, Tubocurarine, Vecuronium

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نشرت فى 13 فبراير 2007 بواسطة eagle

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