Summary lectures receptor pharmacology

RECEPTOR PHARMACOLOGY




Inhoudsopgave
Receptorpharmacology list .................................................................................................... 2
Basic principles ..................................................................................................................... 6
Lecture 1 Gosens .................................................................................................................. 7
Lecture 2 Gosens .................................................................................................................13
Lecture 3 Gosens .................................................................................................................19
Lecture 4 Gosens .................................................................................................................26
Lecture 1 Martina Schmidt ....................................................................................................32
Lecture 2 Martina .................................................................................................................46
Lecture 3 Martina .................................................................................................................58
Lecture 4 Martina .................................................................................................................66
Lecture 5 Martina .................................................................................................................72
Lecture 6 Martina .................................................................................................................80
Lecture 1 DOLGA .................................................................................................................83
Lecture 2 DOLGA .................................................................................................................87




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, Receptorpharmacology list



Pharmacology Reinoud Gosens, Amalia Dolga and Martina Schmidt


Please be aware of: The following drugs you need to know for the examination!
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G PROTEINS
Pertussis toxin: permanently inhibits Gi
Cholera toxin: permanently activates Gs


ION CHANNELS
Tetrodotoxin (TTX): depolarization block, block sodium influx
Tetraethylammonium (TEA): still depolarization, hyperpolarisation is gone, potassium blocker


CHOLINERGIC SYSTEM
Acetylcholine
Muscarine: tachycardia, alertness , increase in HR, no charge can enter BBB
Nicotine: targets which are ligand gated ion channels (on muscle and neuronal)
Carbachol: agonist, do not enter BBB, can used by glaucoma
Atropine : antagonist, inhibit Ach, weakening muscle induction, poisoning->physostigmine,
crosses BBB
Pilocarpine : is an agonist (does enter the brain), used by glaucoma, work on muscarinic
receptor, works like carbachol
Pirenzepine: selective for M1 receptors, used by duodenal ulcer, inhibition gastric secretion




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,Pralidoxim :insecticide poising can be reversed->dizzy, sweaty. It can also be used by
chemical warfare (gasses). Pralidoxim can be used after atropine. Antidote of cholinesterase
inhibitor.
Physostigmine: no charge, passes BBB
Neostigmine : can be used to raise the heart activity, is reversible, does not passes BBB
(atropine poising), medium acting, reverse the activation of non-depolarising neuromuscular-
blocking durgs after surgery
Botulinum toxin: inhibits Ach release, by breakdown of proteins
Tiotropium: poor absorption, doesn’t cross BBB, by pulmonary diseases
Succinylcholine: is very strong and causes very long lasting depolarization and activation of
skeletal muscles. Depolarization blocking agent, increase potassium in blood
(suxamethonium) muscle relaxants
Tubocurarine: muscle relaxants, non-depolarizing, block N-receptors


ADRENERGIC SYSTEM
Noradrenaline
Adrenaline
Phenylephrine: a1, locally applying not systemic
Clonidine: alpha 2 specific; capable to inhibit noradrenaline release by coupeling to Gi,
mainly used for its anti-sympathetic effect→less AC→less cAMP→less calcium→less
phosphorylation, oxymetazoline : alpha 2→activate PLC
Isoprenaline: nictoinic receptors neuromuscular junction, ACH
Fenoterol: inhalation of beta 2 mimetic, acute treatment, salbutamol acute treatment
inhalation
Cocaine:block sodium channels, can inhibit re-uptake of adrenaline
Tyramine: dizzy because it, cheese and redwine contain it
Reserpine: hypertension , dopamine decreased, NE and E decrease and serotonin decrease
Prazosine: a1 antagonist, hypertension
Propranolol: antagonist, blockade of B-receptor
Pindolol antagonist if noradrenaline is present. When we have low noradrenaline in the blood




DOPAMINERGIG – PURINERGIC - SEROTINERGIC SYSTEM
Dopamine: vasodilation,
Tyramine: is in cheese and wine
Noradrenaline

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, Adrenaline
Carbidopa
Dopamine synthesis
Levodopa: can cross BBB
Moclobemide
Tranylcypromine
Selegeline
Apomorphine
Bromocriptine
Haloperidol
Amphetamine
Cocaine
Ergotamine
Metoclopramide
Serotonin synthesis
Triptans
Spiperone
Buspirone
LSD
Ondansetron
Fluoxetine
Methysergide
Lorcaserin
Closapine
MAO-A inhibitors
MAO-B inhibitors
Antidepressants acting on SSRI
Adenosine
Suramin
Methylxanthines (theophylline)


LOCAL ANAESTHETICS


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