- TERMS
- Core Drugs: Adrenergic. *Note: Although these drugs claim to be B2 selective, they are not really that selective so they will still have affects in other system. I.e. atenolol will affect breathing as well, Salbutamol will affect heart as well to some extent.
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B2 Agonists
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Salbutamol
- Short term relief of asthma by opening airways
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Eformeterol
- Long acting relief of asthma by opening airways
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B1 Antagonists
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Atenolol
- Beta-blocker used in the treatment of Angina by reducing heart rate and contractility. Contraindicated in asthmatics due to worsening of condition via bronchiole constriction.
- ACh production/release
- Core drugs: Cholinergic
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Muscarinic antagonists
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Atropine
- -Good for mydriasis when wanting to look in the eyes. Decreases constriction caused by ACh. -Also good for extreme bradycardia as reduced vagus (parasymp) action promoting a faster heart rate. -Also used in 2nd degree heart block -Also used as an antidote to anticholinesterase poisoning
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Hyoscine
- Antiemetic-particularly motion sickness: cholinergic system is responsible for vestibulo-system and emetic system so by blocking this, relieves symptoms of motion sickness.
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Benztropine (CNS)
- Competitive antagonist used in Parkinson's Dx. Helps to restore inbalance of high ACh, low dopamine levels in these patient.s Side effects are dry-mouth, blurred vision, constipation due to its effects in blocking normal parasymp actions by other muscarinic receptors.
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Botulinum toxin
- Prevents Ach release from nerve terminals at neuromuscular junction. Good for stopping wrinkles if injected at site of NMJ for different facial muscles.
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Anticholinesterase
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Pyridostigmine
- For treatment of Myasthenia Gravis: prolongs action of ACh by inhibiting its degradation so muscles are able to work better. Particularly good on weak muscles such as those in eyes. Problem is it affects at all other receptors too having differing affects
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Neuromuscular blockers
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Suxamethonium
- Depolarizing neuromuscular-junction blocker. Classified as a Nicotinic receptor agonist but acts to block the receptors by keeping them in the open & inactive state. So the 'agonist' name is a little misleading. Acts on skeletal muscle to decrease contraction. Hence used as a muscle relaxant.
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Rocuronium
- NMJ Nicotinic depolarizing blocker like Suxamethonium. Used as a muscle relaxant.
- Problem
-Low HR: B1 agonist
-Premature labor: B2 agonist
-Bronco-constriction: B1 agonist
-Heypertension1: B1 antagonist
-Hypertension 2: beta-1 antagonist
-Tachycardia: beta-1 antagonist
-Benign prostatic hyperplasia: Beta 1 antagonist
-Weak heart contraction: Beta 1 agonist
- Medical scenarios & drugs to use:
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Adrenergic Nerves [Secrete NA & A]Sympathetic NS
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Adrenoceptors (G-protein)
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Alpha
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Alpha 1
- Vascular smooth muscle [Contraction]
- Genitourinary smooth muscle [Contraction]
- Liver [Gluconeogenesis]
- Intestinal Smooth muscle [Relaxation]
- Eye-pupil [Dilation]
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Alpha 2
- Vascular Smooth muscle (again) [Contraction]
- Pre-synaptic nerve terminals [decreases ACh AND NA release]
- Platelets [Promotes aggregation]
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Beta
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Beta 1
- Heart [Increases rate/force]
- Kidney [increases renin secretion]
- Eye-pupil [increased secretions]
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Beta 2
- Vascular smooth muscle [relaxation]
- Uterine smooth muscle [relaxation]
- Bronchial smooth muscle [relaxation-opens airways]
- Liver [Glycogenolysis]
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Cholinergic Nerves [Secrete ACh]Parasympathetic NS
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Cholinoceptors
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Nicotinic (Ion channels)
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Skeletal muscle
- Causes contraction of all skeletal muscle in the body. Without ACh, the muscles relax
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Autonomic ganglia
- Located in all ganglia of the Nervous System-ACh connects all preganglionic neurons with postganglionic neurons whether in the Symp or Parasymp NS
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Muscarinic (G-protein)
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Parasympathetics
- M1-CNS, Gastric & Salivary glands [Increases secretions]
- M2-'Cardiac' receptors [decreases rate/force]
- M3-Glandular/smooth muscle/Exocrine glands [Secretion]. GIT [increases contractions], Bronchi [Constricts but increases bronchiole secretions], vascular endothelial cells [vasodilatation], Pupil [Constriction]
- M4-CNS, Not well understood
- M5-CNS, Not well understood
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Sympathetic cholinergics *Note: these are an exception to the ACh=parasymp rule. Instead the effects are sympathetic in nature. I.e. would help to run away from a lion!
- Sweat glands
- Increases sweating
- Blood vessels (arterioles)
- Induces vasodilation via realease of NO
- Adrenaline & Noradrenaline: Both are released as part of the sympathetic nervous system. Adrenaline is only different in that it is a broken-down version of Noradrenaline and is only produced by the adrenal medulla (stimulated though by ACh at a nicotinic receptor for its release). However, they do have some varying affinities with different receptors. The only one you should be aware of is that adrenaline favours beta receptors over NA. So that's why you give adrenaline when someones airways are closing up (e.g. in an allergic reaction). Also, at low dose, adrenaline favours beta-receptors most strongly, and t high dose alpha-receptors more strongly. So if someone has a heart problem, its best to give them a big hit to get their heart pumping! E.g. dramatic movies where they stick a needle into the drugged out girl's heart and kabooom!!
- Alpha & Beta: These receptors should be thought of together as these are the ones that respond to Adrenaline & Noradrenaline. These are 2 subtypes of each and are located in different areas of the body. Hence Adrenaline/Noradrenaline has differing affects on each receptor.
- Nicotinic & Muscarinic: Always think of these receptor subtypes together. As both of these respond to ACh, i.e. cholinergic nerves only. There are no subtypes of Nicotinic receptors and 5 known subtypes of Muscarinic receptors. All of these receptors are located primarily in specific organs/tissues and hence have different actions.
- Sympathetic Cholinergics: called cholinergic as they transmit ACh. However they have affects that are sympathetic in nature rather than parasymp (which is usually the role of adrenaline and noradrenaline. Hence called Sympathetic Cholinergics.
- Cholinergic: All nerves of the ANS that transmit ACh down the axons. Also the sole neurotransmitter of the SMS (Somatic) causing muscle contraction
- Adrenergic: All nerves of the ANS that transmit the neurotransmitters Adrenaline & Noradrenaline. Hence called "adren"...