Pharm Block 1-ANS

alex0624's version from 2016-05-25 21:47

ANS Receptors

NameTypeEffector enzymeSecond MessengerProtein Type
M1Gqstimulate PLCincreased IP3 and DAGG-protein coupled
M3Gqstimulate PLCincreased IP3 and DAGG-protein coupled
α1Gqstimulate PLCincreased IP3 and DAGG-protein coupled
α2GiInhibit adenylyl cyclaseDecrease cAMPG-protein coupled
M2GiInhibit adenylyl cyclaseDecrease cAMPG-protein coupled
β1,2,3Gsstimulate adenylyl cyclaseIncrease cAMPG-protein coupled
NNm & Nnn/an/aIon channel receptor (Increases Na+ ion movement into cells)

Receptor Location & Function

Question Answer
M1Neurons, CNS Effects
M2Heart, Reduces heart rate…bradycardia
M3Smooth muscle and glands (Contraction (except in blood vessels)… diarrhea, bronchoconstriction, urination, ↑ Secretions ….salivation, stomach acid, sweating, lacrimation. Exocrine glands, ciliary musc. of eye). Pupil and ciliary muscle (Contracts ...Miosis, increased flow of aqueous humor )
NmSkeletal muscle end plate (Contraction of skeletal muscle)
NnGanglions. Stimulation of post gang fibres
α1Blood vessels Pupil (Iris) smooth muscle (Vasoconstriction, Mydriasis sphincter contraction…so Constipation and Urinary retention) & Prostate & Urinary Bladder
α2Presynaptic nerve terminals ( Reduces release of norepinephrine…bradycardia, hypotension)
β1Heart (Contraction, Increased heart rate). JGA, ↑ renin release
β2Smooth muscles ( Relaxation …so bronchodilation, urinary retention, constipation, uterus relaxation. Vascular smooth muscles), Skeletal Muscle (K+ uptake), Pancreatic Beta Cells (Insulin release)
β3Fat tissue (lipolysis)
D1Kidney's (dilates renal vessels). Activates Adenyl Cyclase. Smooth Muscles

Adrenergic Transmission

Question Answer
Affects synthesize of DOPA by blocking Tyrosine HydroxylaseMetyrosine
Affects the storage of NE & Dopamine (Side Effect: Cause Major DEPRESSION). Use for Hypertension. Affects VMAT.Reserpine
Affects the release of NE & Dopamine (Side Effect: Postural hypertension & reflect tachycardia)Bretylium & Guanethidiene
Inhibits Dopamine and Nor-epinephrine reuptakeCocaine & Tricyclic Antidepressants (TCA)

Cholinergic Transmission

Question Answer
Blocks uptake of AchHemicholiniums
Blocks storage of Ach into vesicles.Vesamicol
Blocks release of Ach by affecitng the SNAPS & VAMPSBotulism toxin

Cholinergic drugs

Question Answer
They act by binding directly to Cholinergic receptors (cholinoceptors)Bethanechol, Pilocarpine, Carbachol (Direct acting Cholinergic agonists)
Indirect IRREVERSIBLE cholinergic agonistsEcothiophate, Malathion, Parathion, Sarin (OrganoPhosphates)
Use in isecticidesMalathion, Parathion
Used as a Nerve GasSarin
Rx for Paralytic ileus: It is the condition characterised by reduced bowel movements, inability to pass stools or flatus. Typically use for non-obstructive GI dysmotility: in postoperative ileus, neurogenic ileus patients.Bethanechol
Rx for Urinary retention (Non obstructive): Typically seen in postoperative patients and many other neurological diseasesBethanechol
By stimulating M3 receptors ___increases the bowel movements and bladder contraction.
Have Strong muscarinic stim and less Nicotinic stim.
By stimulating M3 receptors ____increases the bowel movements and bladder contractionBethanechol
Rx for Glaucoma (due to increased intraocular tension): that constrict the pupils and increase draining of the aqueous humor. Only Muscarinic stimulation.Pilocarpine
Rx for Sjogren's syndrome(Xerostomia; keratoconjunctivitis sicca)Pilocarpine
Irreversible Indirect acting Cholinergic agonists used to treat glaucomaEcothiopate
A tertiary amine, lipid soluble. Therefore used in glaucoma treatment~Physostigmine
Mechanism for PhysostigmineReversible inhibition of AChE enzyme- ↑ Ach. It helps by causing miosis- ↑ outflow of aqueous humor- ↓ IOP
Reversible Acetyl Cholinesterase inhibitors used to treat Myasthenia gravisNeostigmine, Pyridostigmine
Has a longer duration of action. So good for maintenance/long term therapy of M. Gravis. Given orally.(long acting)
Used in acute cases of M. Gravis. Given I. V.(short acting(2-3 hrs) IV route. Is lipid insoluble!!!! 4ry amine.Neostigmine
Reversible Acetyl Cholinesterase inhibitor used to diagnose Myasthenia gravis (Tensilon test also called challenge test)Edrophonium
The shortest acting for 5 minutes~. So used in diagnosis of M. Gravis and to differentiate myasthenic and cholinergic crisis by doing a Tensilon testEdrophonium
Indirect Reversible Acetyl cholinesterase inhibitors used to treat Alzheimer’sTacrine, Rivastigmine and Donepezil
Organophosphorous compounds (OP).Ecothiopate, Malathion, Parathion & Sarin
Organophosphorus compounds are irreversible cholinesterase inhibitors. Signs and symptoms are due to ____ (irreversible inhibition) of the enzyme resulting in excess acetylcholinePhosphorylation
1st concern of organophosphate poison is dealing with theBronchoconstriction
A muscarinic receptor blocker (Anticholinergic drug), is given to control signs of muscarinic excess stimulation of OP compounds. Provide until you see: myadriasis, dry mouth and tachycardia. If overdose give Physostigmine.Atropine
This is a Acetylcholine esterase reactivator. This acts by hydrolysing (reactivating) the drug bound enzyme, this should be given as early as possible, before “Aging” of the enzyme during OP poisoning.Pralidoxime (2-PAM)
What type of drugs contrict pupils and increase draining of the aqueous humorMiotics (Rx; glaucoma)
Indirect cholinergic agonists act by ____ “Acetyl cholinesterase” the enzyme required for metabolism of ACh in synapase. Thus increases Acetylcholine level in synapses.Inhibiting
Reverses the central and peripheral signs of muscarinic blockade (Atropine Poising)Physostigmine
-Blood vessels do not have cholinergic innervations. ___________ is the one which causes vasodilatationCirculating acetylcholine
Use for diagnose bronchial asthmaMethacholine test(will worst the symptoms)
Paralysis of the of the ciliary muscle of the eye, resulting in a loss of accommodationCycloplegia

Anticholinergic drugs (M Blockers)

Question Answer
Used To treat Cholinesterase inhibitors / Organophosphate (OP) pesticides poisoning(irreversible Achase inhibitor--> excess of Ach in Muscarinic receptor stimulation--> diahrrea. Give atropine and will reverse the effects. Also produce Mydriasis.Atropine
Drug that treat Heart Block and bradycardiaAtropine
Shortest acting preparation of AtropineTropicamide
Produce mydriasis and cycloplegia in refraction error testing fundoscopy. Can be Atropine but choose tropicamideTropicamide
Rx for Peptic Ulcers.M rec. p in stomach stimulate Histamine and release acid. This drug inhibit this M rep.Pirenzepine
Rx for motion sickness(anti-histamine drug)Scopolamine
Used to treat drug induce Parkinson (Extrapyramidal symptoms). For drug induced parkisonismBenztropine
Used ONLY in asthma/COPDIpratropium Bromide
Rx for GI Pain and Menstrual crampsDicyclomine
Reverses the central and peripheral signs of muscarinic blockade (Atropine Poising)Physostigmine
Acts for 4 hours, is preferred to produce mydriasis and cycloplegia (paralysis of the ciliary muscle of the eye, resulting in a loss of accommodation (side effect)) in refraction error testing and fundoscopyTropicamide
Nicotinic receptors (Nn) or ganglionic blockersHexamethonium, Mecamylamine
Side effect of Hexamethonium, MecamylamineSevere Hypotension

Adrenergic Recptors & Drugs

Question Answer
Adrenergic Receptors in Prostate & Urinary Bladderα1(Gq)
Adrenergic Receptors in Presynaptic nerve terminals (Inhibition of transmitter release- ↓ sympathetic outflow)α2(Gi)
Adrenergic Receptors in Heart (Contraction, Increased heart rate). JGA, ↑ renin releaseβ1
Adrenergic Receptors in Skeletal Muscle (K+ uptake), Pancreatic Beta Cells (Insulin release)β2
Adrenergic Receptors in Pancreatic Beta Cells (Insulin release)β2
Adrenergic Receptors in Fat tissue (lipolysis)β3
Adrenergic Receptors in Kidney's (dilates renal vessels). Activates Adenyl Cyclase. Smooth MusclesD1
Drug involve in displacement of stored catecholamines from the adrenergic nerve endingAmphetamine, methamphetamine and Tyramine
Drug involve in Inhibition of reuptake of catecholamine’s already releasedCocaine & Tricyclic antidepressants

Adrenergic Recptors & Drugs

Clonidine, Apraclonidine, Tizanidineα2
Isoproterenolβ1, β2
Norepinephrineα1, β1, β2
Epinephrineα1, α2, β1, β2
Dopamine D1, D2
Low Dose of Dopamine activatesD1
Moderate Dose of Dopamine activatesβ1
High Dose of Dopamine activatesα1
Used as mydriatic for retinoscopy (NO cycloplegia) Phenylephrine
α2 selective agonists can be used in treatment of glaucomaApraclonidine, Brimonidine
β antagonists decrease the production of aqueous humor- hence can be used in treatment of glaucomaTimolol
At low epinephrine concentrations, the ___receptors will be occupied because these receptors have a higher affinity of epinephrine β2
At high epinephrine concentrations, the ___receptors will be occupied because there are more of these receptors the predominant effect at high concentrations is vascular smooth muscle contraction. α1
Epi is combined with to reduce the systemic absorption of anesthetic, and increase their duration of actionLidocaine (local anesthetic)
Nasal decongestant to reduce the discomfort of hay fever & the common coldPhenylephrine
Use for Short term hypotensive emergencyPhenylephrine
These drugs are used as topical decongestants because of their ability to promote constriction of the nasal mucosa.Xylometazoline and oxymetazoline
Use for HT in pregnancy (Pre-eclampsia)Clonidine & alpha methyldopa
Side effects: Postural hypotension, dry mouth, sedation, rebound hypertensionClonidine & alpha methyldopa
A clonidine derivative used in glaucomaApraclonidine, Brimonidine
To produce bronchodilation in treatment of Bronchial asthma and COPD. Will produce tachychardia)Albuterol, terbutaline, Salmeterol
Rx for Premature labor, threatened abortionAlbuterol, terbutaline, Salmeterol
Increases the release of monoamines (norepinephrine & dopamine) from their storage sites.Amphetamine
Important chiefly because of its use and misuse as a CNS stimulant. It has marked stimulant effects on mood and alertness and a depressant effect on appetite.Amphetamine
A new amphetamine substitute, used in narcolepsy and is claimed to have fewer adverse effectsModafinil
Rx for Attention-deficit hyperactivity disorder (ADHD) Methylphenidate
Inhibition of transmitter reuptake at noradrenergic synapses.Cocaine
Tachyphylaxis developsEphedrine
If taken orally while taking MAO inhibitors (antidepressants), it produces effects similar to norepinephrine, and can possibly cause a hypertensive crisisTyramine