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46 Cards in this Set
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- Back
- 3rd side (hint)
Botulinum toxin (botox)
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Mechanism: Prevents Ach release into symaptic cleft by block exocytosis
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Effect: Weakening of the muscle and eventual paralysis, treats focal distonias, torticollis, wrinkles, hyperhydrosis (sweating), strabismus (double vision), Blepharospasms (eye twitch)
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Edrophonium
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Mechanism: Reversible Anti-cholinesterase, short-term inhibition of AchE at the synaptic junction thus prolonging the effects of Ach
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Can diagnose MG and Eaton Lambert, too short-acting to be used as treatment
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Neostigmine
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Mechanism: Reversible Anti-cholinesterase, prevents degradation of Ach in the synaptic cleft by AchE
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Treats MG, Eaton Lambert
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Physostigmine
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Mechanism: Reversible Anti-cholinesterase, prevents AchE from breaking down synaptic Ach - can also cross BBB (so treats atropine poisoning)
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Treats Glaucoma (topical).
Reversal of anticholinergic toxicity or induced paralysis in surgery. |
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Reversible Anti-cholinesterases
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Edrophonium, Neostigmine, Pheostigmine
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prolong receptor exposure to Ach by preventing it's degradation in the synaptic cleft by AchE
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Irreversible Anti-Cholinesterase
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Parathion
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Used in nerve gas and pesticide to induce respiratory paralysis
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Neuromuscular nicotinic agonists
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Succinylcholine - depolarization blockade at neuromuscular jcn
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Ach induced desensitization due to over-stimulation causes temporary muscle paralysis, useful during short procedures
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Succinylcholine
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Mechanism: neuromuscular nicotinic agonist:
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Binds nicotinic receptor but is less susceptible to AchE degradation and thus over-stimulates the receptor causing brief paralysis due to desensitization - used pre-surgery
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Neuromuscular nicotinic antagonists
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Pancuronium - non-depolarizing competetive inhibitor
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No depolarization means no contractions so flaccid paralysis - useful during surgery, long-acting
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Pancuronium
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Neuromuscular nicotinic antagonist - non-depolarizing competetive inhibitor, competes for Ach binding spots and prevents action potential
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Flaccid paralysis for surgery
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Muscarinic agonists
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Ach, Pilocarpine, Methacholine, bethanacol
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Pilocarpine (2x) and Methacholine (3x) are much more resistant to AchE and thus increase parasympathetic effects of Ach binding to Muscarinic receptors. Bethanacol is selective for muscarinic (won't effect nicotinic) so most useful systemically
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Pilocarpine
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muscarinic agonist - resists degradation by AchE thus prolonging parasympathetic responses
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Glaucoma (applied topically to avoid side effects) and Sjrogens (dry mouth) by decreasing intra-ocular pressure and increasing salivation/ secretions
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Methacholine
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resistant to AchE degradation thus serves as a strong muscarinic agonist
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Bronchoconstriction - Diagnose but not treat asthma (actually exacerbates symptoms)
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Bethanacoll
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Exclusive affinity for muscarinic receptors, won't bind nicotinic so useful as agonist post-surgery
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Post-surgery clearing of bladder, stimulation of GI motility
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Uses of Atropine
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decreases SLUDGE - salivation, lacrimation, urination, diaphoresis (sweating), GI tract motility, emisis (vomiting)
Increases: pupil dilation, blood pressure |
Can be used as treatment against parasympathetics OR can be poison (kids eating shiny red berries) - side effects include: cardiac arrhythmias, raised intraocular pressure, tachycardia,
constipation, xerostomia and blurred vision |
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Muscarinic antagonist
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Atropine - causes sympathetic symptoms
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increased HR (tachycardia), decreased urination, pupil dilation
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Indirect adrenergeci agonist - Inhibitors of Catecholamine storage
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Amphetamine, PseudoEphedrine
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Amphetamine
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Release NorE, block re-uptake of NorE, weak MAO inhibitor
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treats ADHD and narcolepsy, commonly abused as recreational drug - ecstacy/ MDMA
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Pseudoephedrine
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Indirect Alpha & Beta agonist - Releases all stored catecholamines (Mainly NorE) from vesicles to synaptic termina
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CNS stimulation and nasal/sinus decongestant
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Inhibitor of Catecholamine metabolism
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Iproniazid - MAO inhibitor, prevents re-uptake of NorE
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treats depression but must NOT be used with tyramine containing foods (wine, cheese) because this also releases NorE thus there would be massive wave of sympathetics and emergency hypertensive crisis
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Iproniazid
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MAO inhibitor - increases effects of sympathetics (agonist) by preventing breakdown and recycling of NorE
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treats depression - must avoid Tyramine containing foods because these release NorE too (too much norE=hypertension)
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tricyclic antidepressants
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imipramine - very non-specific but increases NorE in CNS
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block 5HT re-uptake (as well as several receptors)
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catecholamine re-uptake blockers
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Cocaine, imipramine
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Cocaine blocks NET and stops re-uptake of Dopamine and Serotonin (thus the fun effects) - highly addictive drug - cravings caused by depletion of DA from dopaminergic nerve terminals
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Imipramine
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Blocks NorE Transport (NET) to increase it in the CNS
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antidepressant, can also cause cardiac arrythmias
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Non-selective Alpha and Beta agonists
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Oxymetazoline - vasoconstrictor - increases peripheral resistance and blood pressure but no direct effect on heart due to carotid sinus baroreceptor reflex
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nasal decongestion and opthalmic hyperemia - can cause hypertension
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Oxymetazoline
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Non-selective alpha and beta agonist - vasoconstrictor
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Used to treat nasal congestion and high eye pressure
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Alpha 1 agonist
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Phenylephrine - increases vasoconstriction of vascular smooth muscle
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emergency treatment of shock and nasal decongestion
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Alpha 2 agonist
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Clonidine - decreases sympathetic outflow (Gi-inhibitory)
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treats hypertension and drug withdrawal
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Phenylephrine
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Alpha 1 agonist - vasoconstriction
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treats shock and nasal congestion
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Clonidine
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Alpha 2 agonist - decreases sympathetic output, lowers vasoconstriction
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treats hypertension and drug withdrawal
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Non-specific Alpha 1 and Alpha 2 antagonists
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Phenoxybenzamine (irreversible) and phentolamine (reversible) - inhibits sympathetics
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treat pheochromocytoma
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Phenoxybenzamine
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irreversible due to covalent binding - inhibits sympathetics
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treat pheochromocytoma
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phentolamine
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reversible non-specific alpha1/alpha2 antagonist, inhibits sympathetics
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treat pheochromocytoma
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Tamsulosin
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alpha 1 antagonist - selective for smooth muscle of genitourinary tract (alpha 1a)
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treats BPH specifically
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Prazulosin
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alpha 1 antagonist - non-selective
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used to treat BPH
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Beta 1 agonist
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Dobutamine - increases contractility to increase total cardiac output
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acute heart failure
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Dobutamine
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Beta 1 agonist - increases contractility and total cardiac output
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acute heart failure
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Alpha 1 antagonists
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Prazulosin & Tamsulosin
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treat BPH
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Beta 2 agonist
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Albuterol - bronchodilator
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treats acute asthma - short acting
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Albuterol
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Beta 2 agonist - bronchodilation
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treat acute asthma - short acting
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Non-selective beta blocker (B1 antagonist)
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Propanalol
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was used to treat hypertension but replaced now by more selective beta blockers due to side effects including severe bronchoconstriction
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Propanolol
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non-selective beta 1 antagonist (blocker)
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was used to treat hypertension but replaced now by more selective beta blockers due to side effects including severe bronchoconstriction
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Atenolol
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Selective Beta 1 antagonist (blocker)
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treats hypertension with fewer side effects for people with COPD and diabetes
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Selective beta 1 antagonist (blocker)
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Atenolol
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safer treatment for hypertension
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Partial Beta 1 and Beta 2 antagonism
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Pindolol - dulls sympathetic response by competitively binding receptor (prevents NorE from binding)
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hypertension
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Pindolol
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Partial blockage of Beta 1 and Beta 2 - through partial stimulation but prevention of NorE binding and causing full effect it dulls the sympathetic response
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hypertension
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