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Cholinergic Adrenergic (Adrenergic (Sympathetic effects (Dilate pupil,…

- - - - M2
        
        Heart
      - M3
        
        Lungs, secretion, GIT, Pupils
      - M1
        
        Stomach
      - M4 & M5
        
        CNS
    - - N1
        
        skeletal muscle
      - N2
        
        Ganglion, CNS
  - - - Contraindication:
        
        Peptic ulcers
        
        Asthma
      - Diarrhoea/Abdominal cramps
        
        Sweating
        
        Miosis (blurred vision)
        
        Nausea
        
        Urinary urgency
        
        Hypotension/Bradychardia
    - - Choline esters
        
        Acetycholine :fire:
        
        Cannot cross BBB
        
        Broken down very quickly by AChE
        
        Bethanechol :fire:
        
        Resistant to AChE, but still broken down by other choline esterase
        
        Treatment for Gastric atony :check:
        
        Increase detrusor tone, decrease outlet resistance of sphincter
        
        Increase motility and secretion
        
        Treatment for Urinary retention :check:
        
        Cannot cross BBB
        
        Varenicline :fire:
        
        may be associated with suicidal ideation
      - Alkaloids
        
        Pilocarpine :fire:
        
        Treatment for Glaucoma :check:
        
        Contract sphincter of iris
        
        Free entrance of Schlemm's canal help in drainage to relieve pressure
        
        Enhance tone of trabecular meshwork
        
        Treatment for Dry mouth :check:
        
        Promote salivation
        
        Nicotine (low dose) :fire:
        
        Aid for smoking cessation :check:
        
        Ganglionic activation of both muscarinic and adrenergic receptors
        
        Adrenaline release
        
        Heart rate increases
        
        GIT motility increases
        
        Peripheral vasoconstriction
        
        Respiration rate increases
        
        Nausea and vomitting
        
        Skeletal muscle contraction :check:
    - - Reversible
        
        Nicotine (low dose) :fire:
        
        Donepezil :fire:
        
        Crosses BBB readily
        
        For Alzhiemers disease :check:
        
        Physostimine :fire:
        
        Antidote for Atropine posioning :check:
        
        Edrophonium
        
        Not significant, only useful for diagnosis of Myasthenia Gravis
        
        Neostigmine :fire:
        
        Treatment for Gastric atony
        
        Treatment for Urinary retention
        
        Myasthenia gravis :check::
        
        Reversal of nondepolarising neuromuscular blockade :check:
        
        Do not cross BBB
      - Irreversible
        
        Sarin :fire:
        Soman :fire:
        Tabun :fire:
        Parathion :fire:
        Malathion :fire:
        
        Organophosphate poison
        
        Suicide inhibitor
        
        Breaksdown and leave phosphate group on inhibitor
        
        Soman/Tabun
        
        Nerve gas
        
        Parathion/Malathion
        
        Insecticides
        
        Somatic side effects: muscle twitching, weakness, flaccid paralysis
        
        Antidotes:
        
        Pralidoxime :fire: cholinesterase regenerator
        
        Atropine :fire: mACH blockers to reverse effect
        
        1 more item...
  - - - Nicotine (high dose) :fire:
        
        Depolarising blockade
        
        Voltage-sensitive sodium channels become inactivated no longer to open in response to a brief depolarising stimulus
        
        Secondary non-depolarising blockade
        
        Desensitise even after repolarise
        
        Medullary depression, bradycardia and neuromuscular blockade
    - - Non-depolarising
        
        Poor oral absorption
        
        Does not cross BBB
        
        Pancuronium :fire::
        
        For surgical paralysis :check:
        
        Non-depolarising blockade
        
        Can be overcome by cholinesterase inhibitors
        
        Side effect: HISTAMINE RELEASED
        
        Flushing edema, erythema
        
        Rocuronium :fire:
        
        Atracuronium :fire:
        
        Causes paralysis of skeletal muscle
        Onset: Fingers --> Limbs --> Diaphragm
        Recover: Diaphragm --> Limbs --> Fingers
      - Depolarising
        
        Succinylcholine :fire:
        
        For surgical paralysis :check:
        
        Cannot be reversed
        
        Same as nicotine Phase I and Phase II
        
        Side effect:
        
        Malignant hyperthemia
        
        Apnea
        
        Hypotension
    - - Prevent exocytosis of Ach containing synaptic vesicles
    - - Constipation
        
        Dry mouth
        
        Pupils dilate, photophobia
        
        Tacchycardia/Hypertension
        
        Confusion
        
        Urinary retention
        
        Redness due to no sweat
      - Contraindication:
        Narrow angle glaucoma
    - - Atropine :fire:
        
        Treatment for bradycardia :check:
        
        Treatment for poison :check:
        
        Treatment for diarrhoea :check: with diphenoxylate
        
        For ophthalmic examination: ciliary muscle paralysis and mydriasis
      - Benzatropine :fire:
        
        Treatment for Parkinson's :check:
        
        Crosses BBB well
        
        Side effects: everything + amnesia, delirium
      - Scopoloamine :fire:
        
        For motion sickness :check:
        
        Block M1 receptors
        
        For Urinary incontenence :check:
        
        Oral or transdermal patch (effective for 2-3 days)
      - Ipratropium :fire:
        
        Poorly absorbed systematically, minimal CNS effect
        
        Treatment for COPD second line for asthma :check:
        
        Decrease bronchoconstriction and bronco secretion
        
        Minimal side effects due to poor systemic absorption
      - Oxybutynin :fire:
        
        For urinary incontinence :check:
        
        For peptic ulcer :check:
- - - - Non specific
        
        Noradrenaline :fire:
        
        More towards Alpha
        
        Severe hypotension :check:
        
        Adrenaline :fire:
        
        More towards beta
        
        Anaphalytic shock :check:
        
        Used with anesthetic :check:
        
        Vasoconstrict to prevent spread of local anaesthesia
        
        Oxymetazoline :fire:
        
        For alpha receptors only
        
        Used for nasal decongestion :check:
        
        Isoprenaline
        
        For beta receptors (rare used)
      - Specific
        
        Dopamine :fire:
        
        Targets alpha 1 and beta 1
        
        Hypotension, cardiac resuscitation :check:
        
        Phenyleprine :fire:
        
        Targets Alpha 1
        
        Used for nasal decongestion :check:
        
        Dobutamine :fire:
        
        Target beta 1
        
        Congestive heart failure :check:
        
        Salbutamol :fire:
        
        Asthma :check:
        
        Target Beta 2
        
        Terbutaline :fire:
        
        Mirabegron :fire:
        
        For urinary incontinence :check:
        
        Targets Beta 3
        
        Brimonidine :fire:
        
        Targets Alpha 2
        
        Eye drops into eye, to treat glaucoma :check:
    - - Inhibition of enzymatic breakdown of catecholamines
        
        Moclobemide :fire:
        
        Monoamine oxidase (MAO) inhibitors
        
        MAO found on mitochondria surface
        
        Primarily in nerve terminals
        
        Broken down mainly by MAOA
        
        Act as antidepressant :check:
      - Block of reuptake of noradrenaline
        
        Tricyclic Antidepressant :fire:
        
        Act as antidepressant :check:
      - Displacement of NA out of vesicle into terminal
        
        Ephedrine :fire:
        
        Nasal decongestant :check:
        
        Mechanism
        
        Compete with NA for vesicular compartment
        
        Inhibit MAOA
  - - - Prazosin :fire:
        
        Specific for Alpha 1
        
        Used for chronic hypertension :check:
        
        Side effects:
        
        Nasal congestion
        
        Abnormal ejaculation
        
        Drowsiness
        Postural hypotension
        
        Block vasoconstriction = more blood pooling in visceral organs
        
        For urinary symptoms of BPH :check:
      - Atenolol :fire:
        
        Specific for beta 1
        
        Treat hypertension :check:
        
        Use with caution with patients with asthma, may still have beta 2 antagonism
      - Betaxalol :fire:
        
        Specific for beta 1
        
        Used to treat glaucoma :check:
      - Propanolol :fire:
        
        Beta non specific
        
        Used to treat Hypertension :check:
        
        Adverse effect: Bronchoconstriction and heart failure
      - Sotalol :fire:
        
        Beta non specific
        
        Used to treat Arrythmia :check:
        
        Act as beta blocker in Class II
        
        Prolong cardiac action potential duration in class III
        
        Adverse effect: Bronchoconstriction and heart failure
      - Timolol :fire:
        
        Beta non specific
        
        Used to treat Glaucoma :check:
        
        Reduces intraocular pressure by reducing aqueous secretion from ciliary epithelium
    - - Agonist at presynaptic autoreceptors
        
        Dexmedetomidine :fire:
        
        For sedation :check:
      - Decreasing NA synthesis
        
        Inhibit tyrosine hydroxylase
        
        Form false transmitter methylnoradrenaline
        
        Used for hypertension :check:
        
        Adverse effect:
        
        Haemolytic anemia
        
        Hepatotoxicity
  - - - L Dopa
        
        Dopamine
        
        Noradrenaline
        
        Adrenaline
  - - - Both: Shut down GIT, vasoconstriction at visceral organs
      - Alpha 2: salivary
      - Alpha 1: Iris + ejaculation
    - - BETA 2 Stimulate lungs + vasodilation of skeletal
      - BETA 1 Stimulate heart
      - BETA 3 is for bladder + glucose mobilisation