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Neuro Pharm

Terms

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Parathion
- indirect-acting cholinergic agonist, organophosphate, irreversible
Isoflurophate
- indirect-acting cholinergic agonist, organophosphate, irreversible
- occasionally used for glaucoma and accommodative esotropia
Echothiophate
- indirect-acting cholinergic agonist, organophosphate, irreversible
- occasionally used for glaucoma and accommodative esotropia
Edrophonium
- indirect-acting cholinergic agonist, reversible
- diagnose myasthenia gravis
Neostigmine
- indirect-acting cholinergic agonist, reversible
- used after anesthesia, treat myasthenia gravis
Physostigmine
- indirect-acting cholinergic agonist, reversible, enters CNS
- glaucoma, atropine O/D, GI atony
Pyridostigmine
- indirect-acting cholinergic agonist, reversible
- long-acting, used for myasthenia gravis treatment
Acetylcholine
- direct-acting cholinergic agonist, M and N receptors
- rarely used to achieve miosis in opthalmic surgery
Bethanechol
- direct-acting cholinergic agonist, mostly M receptors
- stimulates bladder and bowel
Carbachol
- direct-acting cholinergic agonist, M and N receptors
- used rarely for glaucoma and stimulate miosis in surgery
Pilocarpine
- direct-acting cholinergic agonist, M receptors
- great for glaucoma treatment
Methacholine
- direct-acting cholinergic agonist, M receptors
- diagnosis of asthma and bronchial hyperreactivity
Atropine
- muscarinic blocker
- treat bradycardia, stimulate mydriasis and cycloplegia, calm GI and bladder spasms, antidote for organophosphate poisoning
Scopolamine
- muscarinic blocker, more potent CNS effects than atropine
- treat motion sickness
Homatropine
- muscarinic blocker
- stimulate mydriasis and cycloplegia
Cyclopentolate
- muscarinic blocker
- stimulate mydriasis and cycloplegia
Tropicamide
- muscarinic blocker
- stimulate mydriasis and cycloplegia
Pirenzepine
- muscarinic blocker
- blocks M1 receptors and treats gastric ulcers
Tubocurarine
- non-depolarizing competitive nicotinic (muscle) blocker
- muscle relaxant in anesthesia
Pancuronium
- non-depolarizing competitive nicotinic (muscle) blocker
- muscle relaxant in anesthesia
- longer-acting than tubocurarine
Atracurium
- non-depolarizing competitive nicotinic (muscle) blocker
- muscle relaxant in anesthesia
Vecuronium
- non-depolarizing competitive nicotinic (muscle) blocker
- muscle relaxant in anesthesia
Succinylcholine
- depolarizing neuromuscular blocking agent
- used to facilitate rapid intubation ("succ" air)
Nicotine
- nicotinic ganglionic blocker with initial stimulation
Hexamethonium
- non-stimulatory nicotinic ganglionic blocker
Trimethaphan
- non-stimulatory nicotinic ganglionic blocker
Mecamylamine
- non-stimulatory nicotinic ganglionic blocker
Phenylephrine
- a1 agonist
- nasal decongestant, treat hypotension, stimulate mydriasis for ocular exam, terminate episodes of paroxysmal atrial tachycardia (PAT), causes reflex bradycardia
Methoxamine
- a1 agonist
- treat hypotension and PAT
Clonidine
- a2 agonist
- treat hypertension, withdrawal from benzodiazepines and opiates, treat diarrhea in diabetics with neuropathies
Methyldopa
- a2 agonist
Dobutamine
- b1 agonist (slight b2 actions)
- treat unstable CHF and shock
Isoproterenol
- b1 and b2 agonist
- stimulate HR in pts with heart block and bradycardia
Albuterol
- b2 agonist
- treat bronchospasm, asthma, COPD, bronchitis
Metaproterenol
- b2 agonist
- treat bronchospasm, asthma, COPD, bronchitis
Terbutaline
- b2 agonist
- treat bronchospasm, asthma, COPD, bronchitis, can also be used to relax uterus during premature labor
Epinephrine
- non-selective sympathomimetic, stimulates beta at low doses, alpha at high doses
- nasal decongestant, urinary incontinence, hypotension
What is epinephrine reversal?
When given alone, alpha effects lead to increased BP. With an alpha-blocker, epinephrine leads to decreased blood pressure due to b2 activity.
Norepinephrine
- alpha-selective agonist, with some beta activity
- used to treat hypotension, but leads to lowered renal perfusion, last line treatment of shock
Dopamine
- beta-selective at lower doses, stimulates a1 at higher doses
- treatment of shock, increase renal perfusion, and treatment of acute CHF
Tyramine
- indirect-acting sympathomimetic, by-product of tyrosine metabolism, taken up by sympathetic neurons
- metabolized by MAO, so foods high in tyramine are contraindicated in pts taking MAOI's
Amphetamine
- indirect-acting sympathomimetic
- treats ADHD, narcolepsy, and suppresses appetite
Ephedrine
- mixed sympathomimetic (direct & indirect)
- treats urinary incontinence, nasal decongestant, hypotension
Metaraminol
- mixed sympathomimetic
- treats hypotension and terminates PAT episodes
Prazosin
- reversible a1 blocker
- treat hypertension and urinary retention in pts with benign prostatic hypertrophy
- first-dose orthostatic hypotension
Terazosin
- reversible a1 blocker
- treat hypertension and urinary retention in pts with benign prostatic hypertrophy
- first-dose orthostatic hypotension
Doxazosin
- reversible a1 blocker
- treat hypertension and urinary retention in pts with benign prostatic hypertrophy
- first-dose orthostatic hypotension
Phenoxybenzamine
- non-selective, irreversible alpha blocker
- long duration, treat pheochromocytoma, treat pts with benign prostatic hypertrophy (reduces size of prostate)
- orthostatic hypotenstion and reflex tachycardia
Yohimbine
- a2 selective, reversible blocker
- sometimes used to treat impotency
Phentolamine
- reversible, non-selective alpha blocker
- used for short-term treatment of pheochromocytoma-induced hypertension
Atenolol
- b1 selective, reversible blocker
- treats hypertension, MI
Betaxolol
- b1 selective, reversible blocker
Esmolol
- b1 selective, reversible blocker
- very short-acting, used in thyroid storm
Acebutolol
- b1 selective, reversible blocker, intrinsic sympathomimetic activity
- treat hypertension
Metoprolol
- b1 selective, reversible blocker
- treat hypertension, anginal pain, MI
Propranolol
- non-selective beta blocker
- treat HAMATA (Hypertension, Angina, Migraine, Arrhythmia, Thyroid storm, Acute panic syndrome)
Timolol
- non-selective beta blocker
- long half-life, treat glaucoma
Nadolol
- non-selective beta blocker
- long half-life, treat glaucoma
Pindolol
- non-selective beta blocker with sympathomimetic activity
- treat hypertension in pts prone to bradycardia
Labetalol
- non-selective beta blocker with some a1 blockade
- treat hypertension and atrial fibrillation
Carvedilol
- non-selective beta blocker with a1 blockade
- treat hypertension and chronic CHF (not ACUTE!)
Butoxamine
- b2 blocker
- no clinical uses
Guanethedine
- indirect adrenergic antagonist
- treatment of hypertension
Reserpine
- indirect adrenergic antagonist
- rarely used in the clinic to treat hypertension
Tissues with a1 receptors?
Vascular smooth muscle; all but skeletal muscle
GI tract, sphincters
Bladder, sphincter
Radial muscle, iris
Tissues with a2 receptors?
GI tract, wall
Presynaptic adrenergic neurons
(postsynaptic in CNS and blood vessels)
Tissues with b1 receptors?
Salivary glands
Heart
Adipose tissue
Kidney
Tissues with b2 receptors?
Vascular smooth muscle of skeletal muscle
GI tract, wall
Bladder, wall
Bronchioles

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