Autonomic nervous system ( Cholenirgic drugs ) Flashcards
what is the division or classification of Autonomic nervous system drugs
— they are 2
-1-parasympathetic ( cholinergic receptors)
- and this receptors divided into 2
1-muscranic receptor (M) : which follows the mechanism of G-protein receptor
2-Nicotinic Receptors (N) : which follows the Ion channel receptor
-2- Sympathetic ( Adrenergic receptor )
explain the Muscrinc Receptor location and effects
- first of all we need to know that ( Gq ) means: second massinger and thats will :
1- increasing the Calsm
2- decreasing the CMP
and we will refer to it by (+)
—— types of receptor and its location and its effects:
1-M1+ : CNS , (Gastric mucosa , HCL secretion, gall bladder )
2-M2: (heart , bradycardia) + (smooth muscles )
3-M3+:
3-1: bronchial smooth muscles ( bronchi construction)
3-2 : blood vessels ( vasodilation)
3-3: Eye ( Meiosis and gland secretion )
3-4: GIT and urinary ( contractions of the wall and relax of the sphincter)
4-M4: CNS
M5: CNS , cerebral vessels ( no clinical agents )
explain the nectoinc Receptor location and effects
— there is 2 type of them
1- Nectoinc Neural (Nn) : which found in
1-1 CNS
1-2: Adrenal medulla
1-3: autonomic Ganglion
—and its effect on the heart is :
1- Chronotropy : heart rate
2- Iontropy : force of the contraction
3-Dromotropy: conduction of electrical impulse through ( Av node )
————
2-Nectonic Muscular ( Nm) which found in the skeletal muscles
classification of Cholinergic Drugs ( parasympathetic drugs )
—- Cholinergic drugs :
1-cholinergic agonist :
1-1: muscranic agonist: they are two
Direct and indirect
1-2: Nicotinc agonist : they have ganglionic stimulate
2- cholinergic antagonist
what is the Dif of Direct action on the receptor + Dif of indirect action of the receptor
- direct action on the receptor : is mean that the drug changing the vital activity of the drug and bu that changing the effectiveness
-indirect action on the receptor: its inhibit Ach Esterase Enzyme which lead to Accumulation of Ach and staminate both M and N receptors
what is the drug of Muscranic agonist ( direct action on the receptor) you know ?
1- Ach
2-Carbacol
3-Bethanecol
4- Cevimelin
5- Pilocarpine
explain the Ach as Muscranic drug
— Paralogical effect :
1- Cvs M2 : Negative Chomoptropy and Iontropy
2- Blood vessels M3 : vasodilation which lead to hypotension
3- bronchi M3: broncho. construction which will lead to Asthma
3-Eye M3 : contraction of ciliary muscle = meiosis and accumulation of near vision
— chemically : qintryamine thats mean its not passing The BBB and no Side effect of The CNS
— metabolism : by CholinoEstrase
—— no clinical use duo to multiple act
explain the Carbacol Muscranic drug
-Drug : Carbacol 0.1 % Eyedrops
( direct action on the receptor)
-pharamlogical effect:
1- mechanism : stimulates M , N receptors so isn’t selective
2- its cholinoEstrase so its doesn’t metabolised by True or pesdu so it has long duration
-Action : Miosis > and increase out the flow from canal of schalem so its decrease the intraoccular pressure
— Uses : Use Rarely To treat glycoma and only Eyedrops ( locally ) because it has multiple act by stimulating M,N receptors
- side effect : no side effect because it’s given locally
explain the Bethanechol Muscranic drug
-Drug : Bethanechol ( tablets or Subcoutenucily )
-( direct action on the receptor)
-Mechanism : stimulate M receptor Morley in GIT and urinary
-pharmacological effect : contraction of wall and open the sphincters
-use : usually used to treat urin retention
- Forbidden patients :
1- dont give this drug to a patient with enlarged organ like prostate obstruction it will lead to rupture
2- don’t give this drug though IV because its could stimulate M2 in cardiac which could results in sever bradycardia
explain the Cevimelin and Pilocarpine Muscranic drug
-Drug :
1- Pilocarpine 1-5% Eyedrops
2- Cevimeline tablets 30mg for adults
-( direct action on the receptor)
- mechanism for pilocarpine :stamulate M receptor miosis which lead to open the canal of sechlem and tubercle meahwerk and the Equaceumer goes out so the Iop decreases
-pahrmalogical effect : gland secretion
-Uses to treat : dryness of the body or Suögern syndrome
What is the Side effect of Muscrnic drugs
( direct action of the receptor )
-we can shortcut it in words
» DUMBLES
-D: Diarrhia
-U: Urintation
-M: miosis
-B: Bradycardia + Broncho construction
-L : lacrimation
-E: emesses > vomiting + excitation of the CNS
-S: salivation
what kinda of patients we cant describe for them the Direct muscrinc drugs
1- a patient with Bronchial asthma
2- a patient with organic obstruction in the bladder»_space; bethanechol
explain the muscrinc Agonist ( indirect act on the receptor)
— indirect act on receptor: its mean its the drug inhibit the AchE enzyme which results in accumulation of ach and stimulation of both M and N receptor
— type of bonds :
1- Reversible : Anticholino Esterase they do Carbomilation of the Enzyme for 2-3 hours
2- Irreversible : anticholino Estrase yheu do phospharlation and they inhibit the AchE for long duration
what is the drug of Muscranic agonist ( indirect action on the receptor) you know ?
1-physostigmine
2-Neostigmine
3-Pyredostagmine
4-Edrophenuim
5- Donepezil
6-Rivastigmine
7- Di-isopropyl
8- Fluoro-phosphate
9- Galantamine
explain the Physostigmine Muscranic drug
-Drug : Physostigmine
(indirect act on receptor )
—chemically : its planet alkaloids
- tershally amine > so its more soluble and its high absorbed and Pass BBB
- mechanism: inhibit the achE so Ach increase so stimulate N,M receptor
-action : becs its tershally amine it can pass the BBB so it has central and peripheral effect , central> in CNS its results excitement of the brain
- RoA: it’s used only eyedrops because its non selective and its can pass BBB
— uses: usually used to treat glaucoma and toxins of Atropin
explain the Neostigmine muscranic drug
-Drug : Neostigmine 0,015 T
(indirect act on receptor)
—chemically : its synthatic from the physostigmine, so its quntary amine
so its polar > less absorbed and dont pass BBB
- mechanism: inhibit the achE so Ach increase so stimulate N,M receptor
-action : has only peripheral effect because its cant pass the BBB
— uses: usually used for treat
1- Urin retention ( post operation under one condition which there is no organic obstruction)
2- for paralytic , Elus
3-for toxins of non-depolarised drug ( like mevacurium )
4- treat of myasthenia graves
explain the Pyredostagmine muscranic drug
-drug : Pyredostagmine
(indirect act on receptor)
-mechanism: stimulate N receptor on the skeletal muscles by inhibit achE and no manifested effect on M receptor
-uses : used to treat Mythinaia graves
why do we prefer to use pyredostagmine over Neostagimne
- because its selective
- it has long duration of action 4-6 hours
explain the muscrinc Edeopharium
drug : Edropherium
(indirect act on receptor)
-mechanism: stimulate N receptor on the skeletal muscles by inhibit achE and no manifested effect on M receptor
-pharmalogical effect :
1-used to diagnose the myasthenia graves because it has short duration of action only 5-10 min
2- used to deferentate between
myasthenia graves crises and
cholinrigc crises
explain the muscrinc drugs , Donepezil , galatamine , Rivastgmine
-drug :
1-Donepezil 0,01 Tab
2-galatamine 0,005 tab ,
3-Rivastgmine 0,018 capsule
- mechanism: inhibit achE and increase Ach in the synaptic cleft
-uses : to treat Alzahimar because it can pass the BBB so it has more selectively on the central effect
explain the muscranic drugs
- Di-isopropyl
- Fluro-phosphate
uses to treat glycoma and they are irreversible
explain the muscarnic blockers
— they are 2 types
1- natural compounds : Ex Atropin from the planet Atropepladona
2- syntactic from the Atropin
—- general features of natural compounds
1- they are tarshally amine
2- non selective ( blocks M1, M2,M3 )
-Dif of muscranic blockers: its substance which will block or inhibit the muscranic receptor
explain the Atropin ( muscranic blocker )
— Atropin its the prototype of The muscrinc Blockers
-Attopin : has high affinity to muscranic receptors and prevent the receptors to bind with Ach
— chemically : planet alkaloids, tatshally amine , pass BBB
—Kenatics :
1- absorption : good
2- distribution : all the body include CND
3-metabolism: liver
4-excretion : portion metabolise and another unchanged
— effects :
1-CVS : by blocking the M2 which located in the atrium it will decrease the heart rate and if it high dose > tachycardia
2-blood vessels : which consist of M3 there is nothing will happen because the B.V is non innervated receptor
3-Respiratory system : the bronchi which consist of M3 : inhibit the bronchi construction and it will cause bronchi dilation, passive effect bcs receptor a1 will take lead
4-GIT and urnary : which consist of M3 if get blocked will lead to relax of the wall and close of the sphincter ( could casue a constapation and urin retention )
- and HCL will decrease
5-Exocrine glands : which consist of M3 blocking of the receptor will lead to dryness of all body and hypothermia
6- Eye :1- cycloplegia passive midrosis
2-dryness of the eye
7- CNS : SAD-HC
what is the side effect of Atropin
1- glaucoma
2- tachycardia
3-Constapation + urin retention
4- Dryness
