الأكاديمية الدولية للعلوم الصحية
فرع الباحــــــــــــــــــــــــــــة
قســـــــــــــــم الصيــــــــــــــدلة
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
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
Drugs from classes other than the muscle relaxant class are also used to treat spasticity:
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 </TD نشرت فى 13 فبراير 2007
بواسطة eagle
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