ANS Flashcards
ACh mimetics with Carbomoyl group
Bethanechol and Pilocarpine
AChE poisoning leads to DUMBBEELSS
- D: Diarrhea
- U: Urination
- M: Miosis
- B: Bradycardia
- B: Bronchoconstriction
- E: Emesis
- E: Excitation (CNS and muscles)
- L: Lacrimation
- S: Salivation
- S: Sweating
Action of Botulinum Toxin
binds to synaptobrevin and prevents ACh release
Action of Hemicholinium
Inhibits choline uptake. Choline is precursor of ACh, therefore decrease in Choline causes Decrease in presynaptic ACh
Action of Organophosphates
Phosphorylates AChE active site and inhibits it irreversibly
Affect of Ganglion blocker on Arterioles
Vasodilation and hypotension
Affect of Ganglion blocker on Ciliary muscle
Cycloplegia
Affect of Ganglion blocker on GI tract
Decrease gone and motility leading to constipation
Affect of Ganglion blocker on Heart
Tachycardia
Affect of Ganglion blocker on Iris
Mydriasis
Affect of Ganglion blocker on Salivary gland
Xerostromia
Affect of Ganglion blocker on Salivary gland
Xerostromia
Affect of Ganglion blocker on Sweat gland
Anhydrosis
Affect of Ganglion blocker on Venis
Dilation, Decrease venous return, Decrease CO
Affects of Atropine in increased dosage
- Decreased secretions
- Mydriasis and cycloplegia
- Hyperthermia (Red, Dry Hot)
- Tachycardia (increase QRS)
- Sedation
- Urinary retention and constipation
- Excitation and Hallucinations
Albuterol receptor and action
Beta 2 selective agonist
IV
Albuterol used for
Asthma rescue
Alpha 1 Arterioles action
Causes contration leading to increase TPR, increase Diastolic pressure, and increasing Afterload Leads to Ischemia
Alpha 1 bladder sphincter action
Causes contraction leading to urinary retention
Alpha 1 bladder trigone action
Causes contraction leading to urinary retention
Alpha 1 Eye action
Action on Radial muscle causing Contration - Mydriasis
Alpha 1 Kidney action
Decreases renin release
Alpha 1 Liver action
Increases glycogenolysis
Alpha 1 Male sex organs receptor and action
Affects on Vas deferent causing ejaculation
Alpha 1 prostatic urethra action
Causes contraction leading to urinary retention
Alpha 1 second messenger
Gq -> Increase IP3
Alpha 1 Vein action
Causes Contraction leading to increase venous return and increase preload
Alpha 2 Pancreas action
Decreases insulin secretion
Alpha 2 Platelets action
Causes Aggregation
Alpha 2 prejunctional nerve terminal action
Decrease transmitter release and NE synthesis
Alpha 2 second messenger
Gi -> decrease cAMP
Amphetamines used for
Narcolepys and ADHD
Psychostimulant: Decreases appetite and increases mood and alerness
Atropine used for
Antispasmotic, Antisecretory, management of AChE inhibitor OD, Antidiarrheal, ophthalmology
Benztropine used for
M Blocker used for: Parkinsonism because is it Lipid-soluable and enters CNS Acute extrapyramidal symptoms induced by antipsychotics
Beta 1 Blocker action
Decrease HR, SV and CO
Decrease Renin release
Beta 1 Heart Atrial and ventricular muscle action
Increase force of contraction (positive inotropy) Increase conduction velocity Increase CO Increase O consumption (can worsen angina)
Beta 1 Heart AV node action
Increase conduction velocity (positive dromotorpy)
Beta 1 Heart His-Purkinje action
Increase automaticity and conduction velocity
Beta 1 Heart SA node action
Increase HR (positive chronotropy)
Beta 1 Kidney action
Increase renin release (opposite of alpha 1)
Beta 1 second messenger
Gs -> Increase cAMP
Beta 2 blocker action
May precipitate bronchospasm in asthmatics and vasospasm in patients with vasospastic disorders
Decrease Aqueous humor production (glaucoma)
Blocks glycogenolysis and Gluconeogenesis (mask diabetes)
Increase LDLs and TGs
Beta 2 Blood vessels action
Vasodilation causing decrease TPR, Decrease diastolic pressure and decrease after load
Beta 2 Bronchioles action
causes dilation
Beta 2 Liver action
Increase glycogenolysis and gluconeogenisis
Beta 2 Pancreas action
Increase insulin secretion (opposite of Alpha 2)
Beta 2 second messenger
Gs -> Increase cAMP
Beta 2 Skeletal muscle action
Increase Glycogenolysis (increase glucose) Contractility (tremor)
Beta 2 specific effects of epinephrine
1) smooth muscle relastion: Broncioles, uterus, blood vessels
2) Increase glycogenolysis (muscle and liver)
3) Increase gluconeogensis
4) Increase mobilization and use of fat
Beta 2 Uterus action
causes relaxation of uterus
Beta blockers that are also Intrinsic sympathomimetics (partial agonists)
Acebutolol and Pindolol
Bethanechol AChE hydrolysis
none
Bethanechol used for?
RX: postop/neurogenic ileus and urinary retention
Bethanechol works on what receptor
M agonist
Butoxamine receptor and aciton
Beta 2 selective blocker
Cardioselective Beta 1 Blockers are:
Acebutolol
Atenolol
Metoprolol
{ A-M are Beta 1 selective and M-Z are Beta 1 and Beta 2)
Carvedilol receptor and action
Alpha and Beta blocker
Carvedilol used for
Heart failure
Ceyimeline used for?
Dry mouth and dry eyes
Ceyimeline works on what receptor
M agonist
Clinical use of Botulinum Toxin
- Blepharospasm (involuntary contraction of eyelid)
- Strabismus/hyperhydrosis
- dystonia
- cosmetics
Cocaine and TCA action
Prevent reuptake of NE presynaptically
Dobutamine receptor and action
Beta 1 selective agonist
Beta 1 > Beta 2
Dobutamine used for
Congestive heart failure
Donepezil chx
AChE inhibitor that is Lipid-soluable and enters CNS
Donepezil used for?
RX: Alzheimer disease
Echothiophate used for?
RX: Glaucoma
Edrophonium chx:
Short-acting AChE inhibitor that does not cross CNS Compete with ACh for ACh
Edrophonium used for?
DX: Myasthenia Differentiates Myasthenia from cholinergic crisis
Epi and norepi used for
1) Cardiac arrest
2) Adjunction to local anesthetic
3) Hypotension
4) Anaphylaxis (Epi only)
5) Asthma (Epi only)
Epinephrine receptor and action with low dose
Same as Isoproternal (Beta 1 = Beta 2)
Beta 1: Increase HR, SV, CO and pulse Pressure
Beta 2: Decrease TPR and BP
Epinephrine receptors and action in High dose
Like Norepinephrine (Alpha 1, Beta 1, Beta 2)
Alpha 1: Increase TPR and BP
Potential Reflex Bradycardia
Beta 1: Increase HR, SV, CO
Beta 2: Decrease TPR and BP
The affect of Alpha 1 are larger in larger doses than medium doses. Therefore, the difference between medium dose and large dose of Epi is a more prominent increase and BP and reflex Bradycardia
Esmolol receptor, benefit and use
Ulatra short acting Beta 1 blocker used for antiarrhythmia
Ganglion Blocking agents
- Hexamethonium
- Mecamylamine (enters CNS)
Glycopyrrolate and Scopolamine used for
Prevention of laryngospasm in surgery
Importance of Carbomoyl group in Direct-Acting ACh mimetics
Blocks Hydrolysis
Ipratropium used for
M Blocker used for: Asthma and COPD (inhalation) No CNS entry, and no change in mucus viscosity
Isoproterenol side effects
1) Flushing
2) angina
3) arrhythmias
Isoproterenol used for
1) Bronchospasm (B2)
2) Heart block (B1)
3) Bradyarrhythmias (B1)
Isoproternol receptor and action
Beta agonist
Beta 1 = Beta 2
Beta 1: Increase HR, Increase SV, Increase CO and Increase Pule Pressure
Beta 2: Decrease TPR and decrease BP
Labetalol affect
Hypotension with decrease tachycardia due to reflex
Labetalol receptor and action
Reversible alpha 1 antagonist and nonselective Beta antagonist
List of Organophosphates
- Echothiophate
- Soman
- Sarin
- Malathion
- Parathion
Major use of Alpha blockers
1) Hypertension
2) Pheochromocytoma (nonselective)
3) BPH (selective Alpha 1)
Methacholine AChE hydrolysis
little
Methacholine used for?
DX: Bronchial hyperreactivity
Methacholine works on what receptor
M>N agonist
Methyl-p-tyrosine action
Prevents Tyrosine Hydroxylase, enzyme that converts Tyrosine into DOPA. Will have decrease DOPA and increase Tyrosine
Mirtazapine receptor and action
Alpha 2 blocker
Mirtazapine used for
Antidepressant
Muscarinic Bladder Receptors and response
- Gq -> Increase IP3
- M3 on Detrusor causing Contraction
- M3 on Trigone/Sphincter causing relaxation Leading to voiding, urinary incontinence
Muscarinic Blood vessels receptors and response
- Gq -> Increase IP3
- M3 causing Dilation No innervation but effect is due to NO/endothelium-derived relaxing factor
Muscarinic Eye Receptors and response
- Gq -> Increase IP3
- M3 on Sphincter causing Miosis
- M3 on Ciliary muscle causing accommodation for near vision via contraction
Muscarinic GI tract Receptors and response
- Gq -> Increase IP3
- M3 on Stomach causing increased Motility
- M1 on Glands causing increased secretion
- M3 on Intestines increasing contraction causing diarrhea
Muscarinic Glands receptors and response
- Gq -> Increase IP3
- M3 causing secretions
Muscarinic Heart Receptors and response
- Gi -> Decrease cAMP
- M2 on SA node causing decrease in HR
- M2 on AV node causing decrease conduction velocity
Muscarinic Lung Receptors and response
- Gq -> Increase IP3
- M3 on Bronchioles causing contraction and Bronchospasm
- M3 on Glands causing Secretion in COPD Decrease FEV1/FVC
Muscarinic Sphincter receptors and response
- Gq -> Increase IP3
- M3 causing relaxation except LES
Nebivolol receptor and action
Beta 1 blocker and stimulates release of NO
Neostigmine chx:
AChE inhibitor that does not cross CNS
Neostigmine used for?
RX: Ileus, Urinary retention, Myasthenia and Reversal of Non-depolarizing NM blockers
Nicotinic second messenger is:
Ion Channel
Norepinephrine receptor and action
Alpha 1, Alpha 2, Beta 1
Alpha 1: Increase TPR and BP
Beta 1: Increase HR, SV, CO, and pulse pressure
Potential for reflex bradycardia
No effect on Beta 2
Only beta blocker to use for hyperthyroidism
Propanolol
Organophosphates that are insecticides
- Malathion
- Parathion
- Sarin
- Soman
Other classes of drugs with anti ACh affects
- Antihistamine
- TCA
- Antipsychotics
- Quinidine
- Amantadine
- Meperdine
Oxybutynin and Tolterodine used for
M3 selective blocker used for: urinary urgency, frequency and incontinence. Use for BPH
Phenoxybenzamine receptor and action
Nonselective alpha blocker
Noncomopetitive inhibitor of alpha receptors
Irreversable
Phentolamine receptor and aciton
Nonselective alpha blocker
Competitive inhibitor of alpha receptors
Reversable
Causes reflex tachycardia
Phenylephrine receptor and action
Alpha 1 agonist that Increases TPR and Increases BP
Has a potential to cause relex bradycardia due to increase in TPR and BP
THere is no change in pulse pressure
Phenylephrine used for
1) Nasal Decongestant
2) Opthalmogloic use without cycloplegia
Physostigmine chx:
Tertiary amine AChE inhibitor that enters CNS
Physostigmine used for?
RX: glaucoma Antidote for Atropine OD
Pilocarpine AChE hyrolysis
None
Pilocarpine special
Crosses CNS
Pilocarpine used for?
- RX: glaucoma (topical), Xerostomia
- DX: CFTR by causing increase in sweating and then test Cl levels
Pilocarpine works on what receptor
M agonist
Pralidosime (2-PAM) action and uses
Regenerates AChE to counteract AChE inhibitor poisoning
- Prazosin
- Doxazosin
- Terazosin
- Tamsulosin
Alpha 1 selective blockers
Doxazosin has a longer t1/2
Prenalterol receptor and action
B1 selective partial agonist
Prenalterol used for
Congestive heart failure
Pyridostigmine chx:
AChE inhibitor that does not cross CNS
Pyridostigmine used for?
RX: Ileus, Urinary retention, Myasthenia and Reversal of Non-depolarizing NM blockers
Salmeterol receptor and action
Beta 2 selective agonist
Slow action
Salmeterol used for
Long term asthma
Sarin is
Organophosphate used for Nerve Gas
Scopolamine used for
M Blocker used for: Motion sickness but causes sedation and short-term memory block
Sotalol receptor and action
Beta blocker and K channel blockers
Tacrine chx
AChE inhibitor that is lipid-soluable and enters CNS
Tacrine used for?
RX: Alzheimers disease
Terbutaline receptor and action
Beta 2 selective agonist
IV
Terbutaline used for
Asthma rescue
Prevention of premature labor by relaxing Uterus
Timolol used for
Glaucoma
Tiotropium used for
M Blocker used for: Asthma and COPD (inhalation) No CNS entry and no change in mucus viscosity
Trihexythenidyl used for
M Blocker used for: Parkinsonism because it is lipid-solvable and enters CNS Acute extrapyramidal symptoms induced by antipsychotics`
Tropicamide used for
M blocker used for: ophthalmology (topical because short acting)
Use of Hexamethonium and Mecamylamine
Prevent baroreceptor reflex
Varenicline used for?
Reinforces affect of Nicotine in smokers
Varenicline works on what receptor
Partial agonist of N receptors
Yohimibe receptor and action
Alpha 2 selective blocker