physio-cholinergic and adrenergic drugs

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  1. Tetanus toxin (from neuro)
    • anaerobic bacillus clostridium tetani--> invades into interneuron by retrograde 
    • enters the PNS by cut or wound and passes to CNS by retrograde

    • causes inhibition of Glycine trasmitter by breaking down synaptobrevin (so vesicle release) 
    • yielding to hyperreflexia,hypertonia in both flexor and extensor muscles (antagonist and agonist muscles)
  2. Strychnine
    • plant alkoid strychnine blocks some glycine receptors in the CNS
    • similar effect as tetanus toxin
  3. Botulinum Toxin
    • inhibit exocytosis of Ach vesciles at presyaptic cleft.
    • -degrades SNAREs (synaptobrevin) necessary for exocytosis-causes muscle weakness, decrease in sweat (hyperhidrosis), cardiac arrhythmia (irregular heart beat)
    • -double vision, difficulty in swallowing, dry mouth, and difficulty in speaking
    • -could be related to eaton-lambert syndrome
    • -Treatment: AchE inhibitors (physostigmine)

    -could be used for reduction of saliva production in parkinson's disease, spasticity hemifacial spasm, neirological conditions
  4. Edrophonium
    • -Ache Inhibitors -short acting (2-10 min) 
    • -inhibit by binding to the enzyme's active site
    • -rapid onset 
    • -useful for diagnosis of muscle weakness (Myathsthenia Gravis and Eaton-Lambert syndrome)
    • hydroxyl group
  5. Neostigmine
    • -AcheE inhibitor 
    • chronic treatment of Myasthenia Gravis 
    • longer acting 
    • direct cholineric agonist affect on Nm receptors
    • reversible 
    • carbamic
  6. physostigmine
    • AchE inhibitor 
    • long lasting 
    • non-polar moleculem so able to cross BBB --> could for CNS anticholinergic toxicity 
    • used as treatment for Eaton-lambert syndrome
  7. Eaton-lambert syndrome (description)
    • autoimmune disease
    • antibody binds to Ca2+ channels, thus cannot release Ach vesicles 
    • treat by increasing half life of Ach by inhibiting AchE. ie. physostigmine
  8. Myasthenia Gravis (description)
    • -autoimmune disease 
    • antibodies blocking ach receptors. (Nm at NMJ)
    • treat with AchE inhibitors ie. neostigmine
  9. Parathion and Malathion
    • AchE inhibitor 
    • irreversible-hydrolyze and make stable complex
    • toxic 
    • used in pesticides 
    • only new receptors can facilitate AchR activity but could take weeks
  10. Succinylcholine
    • nicotinic agonist 
    • blocker depolarizer 
    • keeps binding to Nm junction Ach receptors.
    • desensitize over time 
    • works as agonist, but gives antagonist effect 
    • causes respiratory depression, Bradyarryhthmia, prolonged paralysis
    • could be used as muscle relaxation during anesthesia and surgery
  11. Pancuronium
    • Nicotinic receptor antagnoist 
    • reversible 
    • paralyze skeletal muscles during surgery
    • more selective towards Nm receptor than Nn.
    • Long acting 
    • side effect: hypertension, apnea, bronchospasm,
  12. pilocarpine
    • muscuranic receptor agonist
    • weak base (alkoid),
    • used for treatment of drymouth (xerostomia) in sjogren's syndrome
    • treatment for glaucoma
  13. methacholine
    muscuranic agonist 

    • 3X more resistant to AchE 
    • selective for cardiovascular muscranic receptors. (M3)
  14. Bethaneol
    • -treatment for post-operative, post-partum
    • -increase GI contractility 
    • -urinary tract motility and retention 
    • completely selective for muscuranic receptors
  15. Atropine
    • muscuranic antagonist
    • used for eye exam to dilate pupil
    • side effect: tachycardia, decrease secretion of salivary, bronchial, GIT 
    • competitive antagonist
  16. Hemicolimium
    • prevents choline reuptake at presynaptic
    • (choline-Na cotransport : rate limiting step)
  17. Vesamicol
    prevents storage of Ach (inhibit Ach-H+ antiport)
  18. phenylephrine
    • -alpha 1 agonist 
    • -increase vasoconstriction
    • -nasodecnogenstion, opthalmic hyperemia *visine), treatment of shock 
    • SE: hypertension
  19. alpha-Latrotoxin (from neuro)
    • interferes with exocytosis to promote massive release and depltion of Ach.
    • promotes fusion of synaptotagmin and neurexin --> massive release fast  
    • initial surge of Ach release and irreversible failure of release Ach.
    • contraction then followed by paralysis
    • Black widow spider venom
    • at NMJ
  20. Carbachol (from neuro)
    • act as an agonist 
    • binds to NMJ
    • are insenstitive to AchE, thus undergo prolonged binding and could lead to desensitizing the Ach receptors
    • along with nicotine and succinylcholine, cannot get degraded by AchE
  21. omega-conotoxin (from neuro)
    • cholinergic inhibitor
    • irreversibly binds to calcium channel 
    • inhibit release of Ach vesicles at the nerve terminal (NMJ)
    • leads to flaccid paralysis 
    • snail toxin
  22. Tubocurarine (curare) and Alpha-bungaratoxin (from neuro)
    • binds to Ach recetor (competitive reversible
    • blocks impulse conduction and could lead to flaccid paralysis.
    • at NMJ
    • curare can be used as muscle relaxation during anesthesia and surgery
  23. Hexamathonium (from neuro)
    • effective Ach antagonist --> synapse in sympathetic ganglia 
    • used as treatment for high blood pressure by ganglionic blocking drugs
  24. beta-bungarotixin (sname venom) from neuro
    binds irreversibly ot actin and possibly other cytoskeletal components in cholinergic nerve endings and block Ach release
  25. 4-aminopyridine (from neuro)
    • -inhibit K+channel and prolongs duration of impulses invading the nerve terminal.  
    • Prolonging depolarization of synaptic coutons enhances entry of Ca ions and thus release of Ach
    • used as treatment for lambert-Eaton syndrome
    • causes increase in Ach release
  26. Neomycin and streptomycin (from Neuro)
    • inhibit Ca channel at presynaptic cleft
    • no Ach exocytosis
    • can also block AchR at postsynaptic cleft
    • reversible; thus able to outcompete by increasing Ca concentration 
    • used as Aminoglycoside antibiotics
  27. Benzodiazepines and barbiturates (from neuro)
    • anti-anxiety drug
    • binds to gamma 2 subunits and alpa subunits on GABA(a) receptor (ionotropic) 
    • This causes allosteric change in binding sites, which enhances the binding of GABA too the receptors. 
    • The action will increase inhibition in the amygdala, where the development of fear and anxiety takes place.
  28. Substance P and capsaicin (from neuro)
    • substance P is released from DRG neurons (nociceptors) 
    • substance P = tachykinin 
    • mediates damage and pain sensation 
    • capsaicin -->1) suppress pain by desensitizing vanilloid receptors or 2) suppress "death" primary afferent neurons from spinal cord to decrease release of substance P
  29. 3 endogenous opioid peptide families (from neuro)
    • beta-endorphins
    • Enkephalins 
    • Dynorphins 
    • they dont cross BBB 
    • mechanism: enkephalin exerts presynaptic inhibition at the synpases of nociceptors on projection neuron (DRG neurons)
  30. Dopamine receptor antagonisits (function) from neuro
    • block hallucinations (including L-dopa-induced hallucinations) and delusion 
    • good for treatment of schizophrenia, parkinsno's disease, and huntington's chorea
    • ie. neuroleptics
  31. Bromocriptine (from neuro)
    • dopamine receptor agonist 
    • effective in alleviating the signs of parkinson's disease
  32. tetradotoxin and saxitoxin (from neuro)
    • -blocks Na voltage gated channel at extracellular site;  presynaptic axons of  NMJ
    • -causes flaccid paralysis
    • found in pufferfish since they digest bacteria that synthesize TTX storing poison in tissue. 

    -for saxitoxin, found in shellfish
  33. Oxymetazoline
    • alpha 1 and alpha 2 agonist 
    • treat nasal congestion, opthalmic hypermia 
    • alpha 1 is partial and alpha 2 is full agonist 
    • SE: hypertension
  34. Yohimbine
    • alpha 2 antagonist 
    • treat male impotence,
    • SE: increase in sympathetic outflow, hypertension
  35. Clonidine
    • Alpha 2 agonist 
    • treat hypertension and opioid withdrawal, cancer pain 
    • SE: brachycardia, hypotension
  36. Tamuslosin
    • Alpha 1 antagonist
    • treatment for hyperplasia
    • genitourinary smooth m. type
    • SE:  less postual orthostatic due to low BP
  37. phenoxybenzamine
    • alpha 1 & alpha 2 antagonist 
    • non-selective and irreversible 
    • treat pheochromocytomoa 
    • increase in VMA, NE and Epi, 
    • Hypertension and sweating
  38. Rivastigmine
    • AchE inhibitor 
    • can cross BBB 
    • used as treatment for Alzheimer's disease, dementia, cognitive disease
    • reversible
  39. What is cheese reaction?
    • Tyramine, which displaces NE in stored vesicle, are found in wine and cheese 
    • when a patient who is on MAO inhibitor drug consumes cheese or wine, you will have increase NE concentration at the synpase 
    • causes high BP and HR, throbbing headache, nausea
  40. Iproniazid
    • inhibit MAO --> reduced NE degradation, increase NE at synapse
    • used as depression treatment 
    • MAO degrades seratonine, dopamine, NE, epi
    • irreversible and nonselective
  41. Imipramine
    • inhibit NET --> no reuptake of NE
    • used as treatment for depression 
    • increases NE at synaptic cleft
  42. Morphine (name 4 sites of action)
    • mu-enkephaline 
    • analgesic effects 
    • binds to c-fibers from nociceptive (pain) at substatia geltinosa 
    • (descending tract) 

    • 1. nociceptors -->decrease excitability of peripheral sensory neurons 
    • 2. spinal cord --> binds to mu receptor on presynaptic of secondary neuron (inhibit release of glutamate) and post synaptic of primary afferent neuron (hyperpolarize).
    • 3.  supraspinal : activates GABA at periaquaductal gray --> descend down to raphe nucleus in pons, activate to release NE or seratonin (5-HT) 
    • 4. euphoric effect on limbic lobe
  43. Cocaine
    • inhibit reuptake of NE by blocking NET 
    • increases NE at synaptic cleft,
    • blocks not only NE but also uptake of Dopamine, seratonine (5-HT)  
    • also blocks Sodium channel from inside
  44. ephedrine or pseudoephedrine
    • inhibits storage of catecholamine
    • increase in NE activity at B and Alpha receptors
    • banned in the U.S. 
    • uses up NE more so less storage 
    • catecholamines are stored via VMAT in vesicles
  45. Carvedilol
    • -non selective B and alpha 1 antagonist
    • -B1 blockade: decrease in HR
    • -alpha1 blockade: vasodilation 
    • -decrease BP by lowering renin level and vasodilation
  46. propanolol
    • non selective B antagosnit 
    • treatment for hypertension and angioa 
    • SE: worse sedation and dyspnea
  47. Butaxamine
    • B2 antagonist 
    • experiemental, no clinical use
  48. atenolol
    • selective B1 antagosnit 
    • treats hypertension, angia (severe pain in chest) 
    • decrease BP by lowering renin level 
    • SE: sadation, dyspnea
  49. Pindol
    • partial B1 agonist = weak antagonist 
    • treat bradycardia, low cardiac output
    • helps to treat hypertension 
    • used for hypertension with patients with bradycardia or low cardiac output
    • smaller effects in increasing BP and HR or leads to smaller decrease in BP and HR
  50. Salmeterol
    • B2 agonist 
    • longer duration (12-24 hrs) of asthma reliever due to lipophilic feature 
    • used to prevent bronchoconstriction
  51. albuterol
    • asthma reliever 
    • rapid action (15min), short duration (4-6 hrs)
    • B2 agonist 
    • avoid cardiac and skeletal side effect
  52. Dobutamine
    • selective B1 agonist 
    • increase contractility, cardiac output, but NOT heart rate 
    • short half life due to COMT metabolism
    • used for acute management of heart failure
  53. isoproterenol
    • non selective beta agonist 
    • increase in contractility (b1) 
    • relaxation, bronchodilation (b2) 
    • emergency arrythmias, bronchospasm
  54. Phentolamine
    • non selective alpha antagonist 
    • prevents vasoconstriction and decrease blood pressure 
    • reversible 
    • treat pheochromocytoma
  55. amphetamines
    • Catechol amine inhibitor 
    • 1) blocks NET
    • 2) weak inhibitor of MAO
    • 3) displaces stored endogenous Ca from vesicles
  56. Prazosin
    • alpha 1 antagonist
    • treat hypertension and benign prostatic hyperplasia 
    • SE: postural orthostatic, hypotension via 1st dose phenomena
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physio-cholinergic and adrenergic drugs
2013-10-15 05:02:27

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