Pharmacology – Drug list -Bristol Year 1 Medical School

Drugs that inhibit Ach release from Pre-Synaptic Neuron -> by blocking choline uptake
Hemicholinium and Triethylcholine

Drug that inhibits Ach release from Pre-Synaptic Neuron -> by preventing Ach packaging in vesicles
Vesamicol

Drug that inhibits Ach release from Pre-Synaptic Neuron -> by depleting/destroying vesicles
Alpha-Latrotoxin – (Toxin made by the Black Spider)

Drugs that inhibit Ach release from Pre-Synaptic Neuron -> by preventing exocytosis
Beta-Bungarotoxin and Botulin Toxin

Nicotinic receptor Agonist
(not broken down by cholinesterases)
Suxamethonium
(- Phase 1 block: prolonged depolarization of nicotinic receptor, Ca2+ is released -> Ca2+ is slowly taken up by SR and the muscle relaxes: this explains muscle flaccidity rather than tetany following fasciculations.
– Phase 2 block: desensitization of the nicotinic receptors at the nerve terminal)

Nicotinic receptor Antagonist
Crurare
(Tubocrurarine + Pancuronium + Vecuronium + Rocuronium + Atracurium + Rocuronium + Mivacurium)

Anticholinesterase -> short acting
(used to diagnose Myasthenia Gravis)
Edrophonium

Anticholinesterase -> medium acting
(used to treat Myasthenia Gravis)
Neostigimine (and Pyridostigmine)

Anticholinesterase -> long lasting
(used as a weapon)
Distigmine (or toxic version Dyflos)

Dyflos poisioning antidote
Pralidoxime

Muscarinic receptor Agonist -> contracts the bladder/treat urinary retention
Bethanecol

Muscarinic receptor Agonist -> treat Glaucoma and Sjorgens syndrome
Pilocarpine

Muscarinic receptor Agonists – (experimental use only)
Carbachol and Methacholine

Muscarinic receptor Agonist -> (usual ones)
Muscarine and Acetylcholine (Ach)

Muscarinic receptor Antagonist -> treat bradychardia following MI/ used with acetylcholinesterase in reversal of non-depolarising block)
Atropine

Muscarinic receptor Antagonist -> treat motion sickness
(similar to Atropine)
Hyoscine

Muscarinic receptor Antagonist -> antispasmodic
Atropine Methonitrate

Muscarinic receptor Antagonist -> offers short term relief of asthma by blocking M3 in lungs
Ipratropium

Muscarinic receptor Antagonists -> causes Mydriasis and Cycloplegia: widening of pupil and offers long distance vision
Tropicamide and Cyclopentolate

Muscarinic receptor Antagonist -> reverse depolarizing block and reduce excessive perspiration
Glycoporonium

Muscarinic receptor Antagonist -> treat urinary incontinence/inhibits contraction of Detrusor muscle
Tolterodine Derafenacin

Drug that inhibits Noradrenaline release from Pre-synaptic neuron -> by activation of pre-synaptic alpha-2 receptors + competing for re-uptake -> inhibits NA production and leads to decrease in [NA] in the synaptic cleft/ treat hypertension
Methyldopa

Drug that inhibits Noradrenaline release from Pre-synaptic neuron -> by destroying NA containing vesicles
Noradrenergic neuron blocking drug

Drugs that inhibits NA, dopamine and serotonin re-uptake causing causing an increase of these molecules in synaptic cleft
Cocaine + Amphetamine + Tricyclic antidepressants (Fluoxetine)

Drug that inhibits Adrenaline re-uptake causing causing an increase of [A] in synaptic cleft + alpha-1 receptor Antagonist
Phenoxybenzamine

Drug that inhibits MAO causing non-vesicular release of NA and an increase of [NA] in synaptic cleft
Antidepressants:
1) Isocarboxazid -> irreversible inhibitor
2) Moclobemide -> reversible inhibitor

Drugs that compete with NA for re-uptake and NA vesicular transporer-> leads to an increase of [NA] in synaptic cleft -> causes rise in BP, Hypertension, Tachycardia which leads to a reflex bradychardia
Displacing agents

alpha-1 receptor Agonists
NA≥A>>ISO

aplha-2 receptor Agonists
A>NA>>ISO + Methyldopa

beta-1 receptor Agonists
ISO>A>NA + Dobutamine and Dopamine

beta-2 receptor Agonists
ISO>A>NA + Salbutamol (used in inhalers)

beta-3 receptor Agonists
ISO>NA=A

alpha-1 receptor Antagonists
Phenoxybenzamine (irriversible) + Phentolamine (reversible) + Prazosin (to treat Raynaud Syndrome -> vasoconstriction in peripheries)

alpha-2 receptor Antagonists
Phenoxybenzamine (irriversible) + Phentolamine (reversible)

beta-1 receptor Antagonists
Note (ABC-> Car.. is a Beta1 and Alph1 antagonist)
Atenolol + Carvedilol + Propranolol (but no longer used clinically)

beta-2 receptor Antagonists
Atenolol + Proparnolol

Na+ ion channel blocker found in Puffer Fish
Tetrodoxin

Pro-drug that encourages the production of Dopamine (its effects weir off as its amount in the blood decreases)
L-DOPA

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
Aspirin (irreversible inhibitor of COX 1+2) +Ibuprofen (competitive reversible inhibitor of COX 1+2) + Paracetamol (selective inhibitor of COX 3)

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Ventolin, Proventil. Pro-Air Generic name: Albuterol Classification: Beta 2 agonist inhaler (SABA, rescue, either MDI or nebulizer via liquid) – bronchodilator Indications: Side Effects: trembling to shaking of hands, arms – “hyperkinesia”, legs or feet. Drowsy/dizzy, headache, dry mouth, arrhythmias …

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