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73 Cards in this Set
- Front
- Back
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→ alfuzosin
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Pharmacological Class: Selective α1 antagonist, reversible
Mechanism of Action: An antagonist of α1A receptors in the prostate leads to relaxation of smooth muscle in the bladder neck, improving urine flow and decreased symptoms of BPH. Primary Use: Treatment of BPH. PO Unique Pharmacokinetics: None noted. Unique Side Effects: May cause orthostasis, syncope, or dizziness, priaprism. |
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→ doxazosin
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Pharmacological Class: Selective α1 antagonist, reversible
Mechanism of Action: Inhibits postsynaptic α1receptors, results in vasodilation, ↓ TPR and BP. Approximately 50% as potent is as prazosin. Primary Use: Treatment of hypertension alone or with other drugs, treatment of urinary outflow obstruction in assoc. w/BPH Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ phenoxybenzamine
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Pharmacological Class: NON-Selective α1 antagonist, irreversible
Mechanism of Action: Long-lasting noncompetitive α1 blockade of postganglionic synapses in exocrine glands and smooth muscle. Primary Use: Treatment of hypertension associated with pheochromocytoma. Micturition problems. Unique Pharmacokinetics: None noted. Unique Side Effects: Tachycardia, syncope, shock, inhibition of ejaculation. |
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→ phentolamine
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Pharmacological Class: NON-Selective α1 antagonist, reversible
Mechanism of Action: Competitively blocks α1receptors, antagonism of circulating epinephrine and norepinephrine. Primary Use: Treatment of hypertension associated with pheochromocytoma. SubQ Unique Pharmacokinetics: None noted. Unique Side Effects: MI, cerebrovascular spasm and cerebrovascular occlusion have occurred following administration. |
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→ prazosin
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Pharmacological Class: Selective α1 antagonist, reversible
Mechanism of Action: Inhibits postsynaptic α1receptors, results in vasodilation of veins and arterioles, ↓ TPR and BP Primary Use: Treatment of hypertension, Off-label = BPH, Raynaud’s Unique Pharmacokinetics: None noted. (No garlic!) Unique Side Effects: Dizziness, drowziness. |
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→ tamsulosin
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Pharmacological Class: Selective α1 antagonist, reversible
Mechanism of Action: An antagonist of α1A receptors in the prostate leads to relaxation of smooth muscle in the bladder neck, improving urine flow and decreased symptoms of BPH. Primary Use: Treatment of BPH. Unique Pharmacokinetics: None noted. Unique Side Effects: "First-dose" orthostatic hypotension. Headache, abnormal ejaculation, rhinitis |
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→ terazosin
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Pharmacological Class: Selective α1 antagonist, reversible
Mechanism of Action: Inhibits postsynaptic α1receptors, results in vasodilation, ↓ TPR and BP. BPH, relaxes the smooth muscle of the bladder neck. Primary Use: Management of mild to moderate hypertension Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ acetylcholine
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Pharmacological Class: Direct-acting M-agonist (Muscarinic).
Mechanism of Action: Causes contraction of the sphincter muscles of the iris, resulting in miosis and contraction of the ciliary muscle. Primary Use: Produces complete miosis in cataract surgery, used primarily in the eye. Unique Pharmacokinetics: None noted. Unique Side Effects: Transient lenticular opacities, bradycardia, hypotension. |
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→ bethanechol
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Pharmacological Class: Direct-acting M-agonist (Muscarinic).
Mechanism of Action: Stimulates cholinergic receptors in the smooth muscle of the urinary bladder, bladder muscle contraction, and increased ureteral peristaltic waves, GI motility. Primary Use: Urinary retention for neurogenic bladder. PO Unique Pharmacokinetics: Bethanechol may cause a critical fall in blood pressure. Unique Side Effects: Potential for bladder infection. |
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→ carbachol
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Pharmacological Class: Direct-acting M-agonist (Muscarinic).
Mechanism of Action: Synthetic direct-acting cholinergic agent that causes miosis by stimulating muscarinic receptors in the eye. Primary Use: Lowers intraocular pressure in the treatment of glaucoma; causes miosis during surgery. Unique Pharmacokinetics: None noted. Unique Side Effects: Headache, cramps, bladder tightness. |
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→ cevimeline
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Pharmacological Class: Direct-acting M-agonist (Muscarinic).
Mechanism of Action: Binds to muscarinic (cholinergic) receptors, causing an increase in secretion of exocrine glands (including salivary glands). Primary Use: Treatment of symptoms of dry mouth in patients with Sjögren's syndrome. PO Unique Pharmacokinetics: None noted. Unique Side Effects: Diaphoesis. |
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→ methacholine
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Pharmacological Class: Direct-acting M-agonist (Muscarinic).
Mechanism of Action: Stimulates muscarinic, postganglionic parasympathetic receptors, results in smooth muscle contraction of the airways. Primary Use: Diagnosis of bronchial airway hyperactivity, a bronchoconstrictor for diagnostic purposes only! Unique Pharmacokinetics: None noted. Unique Side Effects: Wheezing. |
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→ muscarine
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Pharmacological Class: Direct-acting M-agonist (Muscarinic).
Mechanism of Action: Binds to muscarinic (cholinergic) receptors. Primary Use: a natural product found in certain mushrooms, mimics the action of acetylcholine. Unique Pharmacokinetics: None noted. Unique Side Effects: Characterized by increased salivation, perspiration, and lacrimation; deaths are rare, but may result from cardiac or respiratory failure in severe cases. |
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→ pilocarpine
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Pharmacological Class: Direct-acting M-agonist (Muscarinic).
Mechanism of Action: Directly stimulates cholinergic receptors in the eye causing miosis, loss of accommodation, and lowering of intraocular pressure. Primary Use: Ophthalmic: Management of glaucoma. Oral: Symptomatic treatment of xerostomia caused by salivary gland hypofunction. PO Unique Pharmacokinetics: None noted. Unique Side Effects: Flushing, chills, diaphoresis. |
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→ ambenonium
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Pharmacological Class: Reversible AChE Inhibitor.
Mechanism of Action: Inhibits destruction of acetylcholine by acetylcholinesterase. Primary Use: Treatment of myasthenia gravis. Oral Unique Pharmacokinetics: None noted. Unique Side Effects: Arrhythmias, hypotension. |
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→ demecarium
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Pharmacological Class: Reversible AChE Inhibitor.
Mechanism of Action: A cholinesterase inhibitor with sustained activity Inhibits destruction of acetylcholine by acetylcholinesterase. Primary Use: Treatment of open-angle glaucoma. Eye drops Unique Pharmacokinetics: No longer available in the US. Side Effects: Stinging, burning, lacrimation, iris cysts, lens opacities. |
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→ donepezil
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Pharmacological Class: Reversible AChE Inhibitor. CNS activity
Mechanism of Action: Reversibly and noncompetitively inhibits centrally-active acetylcholinesterase. Results in increased concentrations of acetylcholine available for synaptic transmission in CNS. Primary Use: Treatment of mild to moderate dementia of the Alzheimer's type. PO Unique Pharmacokinetics: Long half-life, 70 hrs. Unique Side Effects: Headache, diarrhea, frequent urination. |
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→ edrophonium
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Pharmacological Class: Reversible AChE Inhibitor.
Mechanism of Action: Inhibits destruction of acetylcholine by acetylcholinesterase. IM, IV Primary Use: Diagnosis and treatment of myasthenia gravis, reversal of nondepolarizing neuromuscular blockers. Unique Pharmacokinetics: None noted. Unique Side Effects: Overdosage can cause cholinergic crisis which may be fatal. |
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→ edrophonium + atropine
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Pharmacological Class: Reversible AChE Inhibitor.
Mechanism of Action: A combination of an anticholinesterase agent, and a parasympatholytic (anticholinergic) drug. Primary Use: Antagonist of nondepolarizing neuromuscular blocking agents, and used in the treatment of respiratory depression caused by curare overdose. IM, IV Unique Pharmacokinetics: None noted. Unique Side Effects: Arrhythmias. |
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→ galantamine
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Pharmacological Class: Reversible AChE Inhibitor. CNS activity
Mechanism of Action: Elevates acetylcholine in cerebral cortex by slowing the degradation of acetylcholine. May increase glutamate and serotonin levels. Primary Use: Treatment of mild to moderate dementia of the Alzheimer's type. PO Unique Pharmacokinetics: 80-100% bioavailable. Unique Side Effects: Phase IV trials have shown increased mortality with galantamine. |
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→ neostigmine
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Pharmacological Class: Reversible AChE Inhibitor.
Mechanism of Action: Inhibits destruction of acetylcholine by acetylcholinesterase which facilitates transmission of impulses across myoneural junction. IM Primary Use: Diagnosis and treatment of myasthenia gravis. Unique Pharmacokinetics: None noted. Unique Side Effects: Arryhthmias, hypotension. |
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→ physostigmine
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Pharmacological Class: Reversible AChE Inhibitor.
Mechanism of Action: Inhibits destruction of acetylcholine by acetylcholinesterase. Primary Use: Reverse toxic CNS effects caused by anticholinergic drugs. IM, IV Unique Pharmacokinetics: None noted. Unique Side Effects: Salivation, perspiration, and emesis. Hypersensitivity possible. |
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→ pyridostigmine
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Pharmacological Class: Reversible AChE Inhibitor.
Mechanism of Action: Inhibits destruction of acetylcholine by acetylcholinesterase. Primary Use: Treatment of myasthenia gravis; antidote for nondepolarizing neuromuscular blockers. IM, IV Unique Pharmacokinetics: None noted. Unique Side Effects: Arrhythmias, convulsions. |
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→ rivastigmine
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Pharmacological Class: Reversible AChE Inhibitor. CNS activity
Mechanism of Action: Elevates acetylcholine in cerebral cortex by slowing the degradation of acetylcholine. Primary Use: Treatment of mild to moderate dementia of the Alzheimer's type. PO Unique Pharmacokinetics: Cigarette use increases clearance by 23%. Unique Side Effects: Headache, dizziness, headache, vomiting, diarrhea. |
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→ tacrine
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Pharmacological Class: Reversible AChE Inhibitor. CNS activity
Mechanism of Action: Elevates acetylcholine in cerebral cortex by slowing the degradation of acetylcholine. Primary Use: Treatment of mild to moderate dementia of the Alzheimer's type. PO Unique Pharmacokinetics: None notable. Unique Side Effects: Headache, diarrhea, frequent urination. |
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→ atracurium
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Pharmacological Class: Neuromuscular Blocking, Non-depolarizing.
Mechanism of Action: A competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects: None noted. |
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→ cis-atracurium
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Pharmacological Class: Neuromuscular Blocking, Non-depolarizing.
Mechanism of Action: A competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects: None noted. |
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→ mivacurium
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Pharmacological Class: Neuromuscular Blocking, Non-depolarizing.
Mechanism of Action: A competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects: None noted. |
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→ pancuronium
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Pharmacological Class: Neuromuscular Blocking, Non-depolarizing.
Mechanism of Action: A competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects:None Noted. |
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→ rocuronium
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Pharmacological Class: Neuromuscular Blocking, Non-depolarizing.
Mechanism of Action: A competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects: None noted. |
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→ succinylcholine
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Pharmacological Class: Neuromuscular Blocking, Depolarizing.
Mechanism of Action: Acts similar to acetylcholine, a competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects: None noted. |
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→ tubocararine
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Pharmacological Class: Neuromuscular Blocking, Non-depolarizing.
Mechanism of Action: A competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Used as a skeletal muscle relaxant to paralyze patients undergoing anaesthesia. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects: None noted. |
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→ vecuronium
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Pharmacological Class: Neuromuscular Blocking, Non-depolarizing.
Mechanism of Action: A competitive antagonist of the AchR in the neuro-muscular junction (NM). Primary Use: Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery. IV Unique Pharmacokinetics: Does not enter CNS, no analgesia or anesthesia. Unique Side Effects: None noted. |
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→ atropine
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker. Primary Use: Ophthalmic: Produce mydriasis Oral: Inhibit saliva Injection: Preoperative medication to inhibit salivation; treatment of bradycardia; AV block Unique Pharmacokinetics: None noted. Unique Side Effects: Arrhythmia, hypotension, palpitation, tachycardia. |
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→ cyclopentolate
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Blocks acetylcholine at parasympathetic sites. Primary Use: Short-acting mydriatic Unique Pharmacokinetics: None noted. Unique Side Effects: 2% solution may result in psychotic reactions and behavioral disturbances in children. |
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→ darifenacin
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Selective antagonist of the M3 muscarinic receptor subtype, demonstrates selectivity for urinary bladder receptors. Primary Use: Treatment of overactive bladder with symptoms of urinary urge incontinence. Unique Pharmacokinetics: None noted. Unique Side Effects: Xerostomia, constipation. |
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→ dicyclomine
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands and the CNS. Primary Use: Treatment of overactive bladder with symptoms of urinary urge incontinence. Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ hyoscyamine
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Blocks the action of acetylcholine, antagonizes histamine and serotonin. Primary Use: Oral: Adjunctive therapy for peptic ulcers, irritable bowel, neurogenic bladder/bowel. Injection: Preoperative antimuscarinic to reduce secretions and block cardiac vagal inhibitory reflexes. Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ ipatropium bromide
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Blocks acetylcholine at parasympathetic sites. Primary Use: A bronchodilator for maintenance treatment of bronchospasm associated with COPD Unique Pharmacokinetics: None noted. Unique Side Effects: Bronchitis, COPD exasperation, upper respiratory tract infections. |
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→ oxybutynin
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, demonstrates selectivity for urinary bladder receptors over salivary receptors. Primary Use: Treatment of patients with an overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence. Unique Pharmacokinetics: Exhibits 20% of the anticholinergic activity of atropine, but 4-10 times the antispasmodic activity. Unique Side Effects: Dizziness, Xerostomia. |
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→ scopalamine
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Blocks acetylcholine at parasympathetic sites. Primary Use: Ophthalmic: Produce mydriasis Oral: Parkinsonism and paralysis agitans Injection: amnesia, sedation Transdermal: Prevention of nausea/vomiting Unique Pharmacokinetics: None noted. Unique Side Effects: Drowsiness, blurred vision. |
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→ solifenacin
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Inhibits muscarinic receptors resulting in decreased urinary bladder contraction, decreased detrusor muscle pressure. Primary Use: Treatment of overactive bladder with symptoms of urinary urge incontinence. Unique Pharmacokinetics: 98% bound to alpha1-acid glycoprotein. Unique Side Effects: Xerostomia, constipation. |
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→ tiotropium bromide
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Blocks acetylcholine at parasympathetic sites. Primary Use: A once-daily maintenance treatment for COPD, not indicated for the initial treatment of acute episodes of bronchospasm (rescue therapy). Unique Pharmacokinetics: None noted. Unique Side Effects: Dry mouth. |
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→ tolterodine
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, demonstrates selectivity for urinary bladder receptors over salivary receptors. Primary Use: Treatment of patients with an overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence. Unique Pharmacokinetics: None noted. Unique Side Effects: Dry mouth. |
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→ tropicamide
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, Blocks acetylcholine at parasympathetic sites. Primary Use: Short-acting mydriatic Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ trospium
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Pharmacological Class: Muscarinic Antagonist.
Mechanism of Action: Competitive, reversible muscarinic blocker, It reduces the smooth muscle tone of the bladder. Primary Use: Treatment of overactive bladder with symptoms of urinary urge incontinence. Unique Pharmacokinetics: None noted. Unique Side Effects: Xerostomia, constipation. |
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→ betaxolol
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Pharmacological Class: Selective β1-receptor blocker.
Mechanism of Action: Competitively blocks β1-receptors, with little or no effect on β2-receptors; reduces intraocular pressure by reducing the production of aqueous humor. Primary Use: Treatment of chronic open-angle glaucoma and ocular hypertension; management of hypertension. Unique Pharmacokinetics: None noted. Unique Side Effects: Ocular hyperemia, decreased sexual ability. |
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→ carteolol
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Pharmacological Class: Non-selective beta-receptor blocker.
Mechanism of Action: Blocks both β1- and β2-adrenergic receptors, has mild intrinsic sympathomimetic activity; has negative inotropic and chronotropic effects and can significantly slow AV nodal conduction. Primary Use: Oral: treatment of hypertension and angina. Ophthalmic: treatment of elevated intraocular pressure such as glaucoma. Unique Pharmacokinetics: None noted. Unique Side Effects: Decreased sexual ability. |
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→ levo-betaxolol
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Pharmacological Class: Selective β1-receptor blocker.
Mechanism of Action: The more active enantiomer of betaxolol. Reduces intraocular pressure by reducing the production of aqueous humor. Primary Use: Treatment of chronic open-angle glaucoma and ocular hypertension. Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ levobundol
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Pharmacological Class: Non-selective beta-receptor blocker.
Mechanism of Action: Blocks both β1- and β2-adrenergic receptors, lowers intraocular pressure by reducing aqueous humor production and possibly increases the outflow of aqueous humor. Primary Use: Ophthalmic: treatment of elevated intraocular pressure such as glaucoma. Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ timolol
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Pharmacological Class: Non-selective beta-receptor blocker.
Mechanism of Action: Blocks both β1- and β2-adrenergic receptors, reduces intraocular pressure by reducing aqueous humor production or possibly outflow. Primary Use: Oral: treatment of hypertension and angina. Ophthalmic: treatment of elevated intraocular pressure such as glaucoma. Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ albuterol
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors with little effect on heart rate Primary Use: Bronchodilator for asthma or COPD; exercise-induced bronchospasm. Inhaled Unique Pharmacokinetics: None noted. Unique Side Effects: Angina, atrial fibrillation, chest discomfort |
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→ apraclonidine
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Pharmacological Class: Selective α2 agonist.
Mechanism of Action: Selective for α2-receptors; reduction of aqueous humor formation Primary Use: Prevention and treatment of postsurgical intraocular pressure (IOP) elevation. Ophthalmic drops Unique Pharmacokinetics: IOP-lowering efficacy decreases over time Unique Side Effects: Discomfort, hyperemia, pruritus |
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→ arformoterol
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors, (R,R)-enantiomer of formoterol, long-acting effect, "LABA" Primary Use: Prevention of bronchospasm Unique Pharmacokinetics: None noted. Unique Side Effects: None noted. |
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→ bitolterol
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors, long-acting effect Primary Use: Maintenance treatment of asthma and in prevention of bronchospasm Unique Pharmacokinetics: Withdrawn from US market in 2001. Unique Side Effects: None noted. |
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→ brimonidine
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Pharmacological Class: Selective α2 agonist.
Mechanism of Action: Selective for α2-receptors; reduction of aqueous humor, increased uveoscleral outflow Primary Use: Reduces elevated intra-ocular pressure in chronic open-angle glaucoma. Ophthalmic drops Unique Pharmacokinetics: None noted Unique Side Effects: Corneal staining, erosion, photophobia |
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→ dipivefrin
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Pharmacological Class: Non-selective α-agonist
Mechanism of Action: Stimulates α/β-adrenergic receptors Increases aqueous humor outflow Primary Use: Reduces elevated pressure in chronic open-angle glaucoma topical drops Unique Pharmacokinetics: Pro-drug of epinephrine Unique Side Effects: Avoid with closed-angle glaucoma |
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→ dobutamine
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Pharmacological Class: Selective β1 –agonist, minor β2and α1
Mechanism of Action: Selectively stimulates β-adrenoreceptors β1 = ↑inotropy and HR, β2 = sm muscle relaxation, α1 = ↑SVR Primary Use: Acute management of decompensated CHF. ↓ reg of receptors occurs in 1 week. IV Unique Pharmacokinetics: Racemic mixture with opposing effects, but more by β1 Unique Side Effects: Arrhythmias, hypotension |
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→ dopamine
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Pharmacological Class: Non-selective Direct sympathomimetic
Mechanism of Action: D1 › β1, β2 ›, α1-agonists Low doses: D1 effects = ↑HR, inotropy Medium: β1 effects = ↑CO, ↓SVR High doses: α1 effects = ↑SVR Primary Use: Enhanced natriuresis for poor renal perfusion Treatment of CHF, hypotension. IV Unique Pharmacokinetics: Inactivated in synapse, and by COMT, MAO Unique Side Effects: Arrhythmias. |
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→ epinephrine
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Pharmacological Class: Non-selective Direct sympathomimetic
Mechanism of Action: β1, β2 , α1 ,α2-agonists Low doses: β effects = ↑HR, inotropy, vasodilation High doses: α effects = ↑SBP and DBP Primary Use: Severe bronchospasm, anaphylaxis. Cardiac arrest, cardiogenic shock, hypotension. Vasoconstrictor w/local anesthetic. IV Unique Pharmacokinetics: Inactivated in synapse, and by COMT, MAO Unique Side Effects: Arrhythmias, MI (↑CO), angina |
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→ formoterol
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors, long-acting effect Primary Use: Maintenance treatment of asthma and in prevention of bronchospasm Unique Pharmacokinetics: Peak effect within 15 minutes. Unique Side Effects: Viral infections. |
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→ isoproterenol
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Pharmacological Class: Non-selective β -agonist
Mechanism of Action: Selectively stimulates β-adrenoreceptors β1 = ↑HR and inotropy β2 = smooth muscle relaxation Primary Use: Ventricular arrhythmias. Used in emergencies to stimulate heart rate with bradycardia or heart block. IV Unique Pharmacokinetics: Metabolized in liver, other tissues by COMT Unique Side Effects: Angina, MI (↑cardiac work), arrhythmias |
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→ metaproterenol
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors, long-acting. Primary Use: Bronchodilator for asthma or COPD; PO, inhaled Unique Pharmacokinetics: Delayed onset, prolonged effects. Unique Side Effects: Tachycardia, nervousness |
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→ metaraminol
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Pharmacological Class: Selective α1 agonist, weak β agonist.
Mechanism of Action: systemic arterial vasoconstriction Primary Use: Treatment of hypotension, particularly as a complication of anesthesia, also used in the treatment of priaprism. IV Unique Pharmacokinetics: None noted Unique Side Effects: Tachycardia, arrhythmias, tissue necrosis. |
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→ methoxamine
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Pharmacological Class: Selective α1 agonist, weak β agonist.
Mechanism of Action: systemic arterial vasoconstriction, vagally-mediated bradycardia Primary Use: Hypotension, supraventricular tachycardia. IV Unique Pharmacokinetics: None noted Unique Side Effects: None noted |
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→ midodrine
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Pharmacological Class: Selective α1 agonist.
Mechanism of Action: Increases arteriolar and venous tone resulting in a rise in blood pressure in patients with orthostatic hypotension Primary Use: Orphan drug: Treatment of orthostatic hypotension. Unique Pharmacokinetics: None noted. Unique Side Effects: Supine hypertension, pruritus, parathesia |
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→ norepinephrine
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Pharmacological Class: Direct sympathomimetic. α1 =α2 › β1
Mechanism of Action: α1 = ↑SVR , α2 = feedback inhib of Epi, NorE β1 = ↑inotropy and HR Net = ↑BP, peripheral vasoconstriction Primary Use: Treatment of shock. Hypotension. Extravasation can lead to tissue necrosis. IV Unique Pharmacokinetics: Administration requires the use of an infusion pump! Unique Side Effects: Angina, Arrhythmias, MI (↑cardiac work) |
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→ oxymetazoline
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Pharmacological Class: Selective α1 agonist.
Mechanism of Action: Vasoconstriction of nasal mucosa Primary Use: Treatment of middle ear infections, rhinitis, the common cold, sinusitis, allergies. Nasal spray Unique Pharmacokinetics: None noted. Unique Side Effects: burning, stinging, dryness, rebound congestion |
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→ phenylephrine
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Pharmacological Class: Selective α1 agonist, weak β agonist.
Mechanism of Action: systemic arterial vasoconstriction, vagally-mediated bradycardia, local vasoconstriction. Primary Use: Hypotension, vascular failure in shock. IV. OTC use: relief of nasal mucosal congestion, treatment of hemorrhoids, relief of redness of the eye due to irritation Unique Pharmacokinetics: None noted Unique Side Effects: Bradycardia, excitability, restlessness |
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→ pirbuterol
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors Primary Use: Prevention of bronchospasm Unique Pharmacokinetics: None noted. Unique Side Effects: Nervousness, tremor. |
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→ salmeterol
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors, “LABA”- long-acting β agonist Primary Use: Maintenance treatment of asthma and in prevention of bronchospasm Unique Pharmacokinetics: Not for acute asthma symptoms! Unique Side Effects: None unique |
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→ terbutaline
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Pharmacological Class: Selective β2 agonist.
Mechanism of Action: Relaxes bronchial smooth muscle by action on β2-receptors, fast-acting Primary Use: Inhaled: bronchodilator; Oral: tocolytic agent Unique Pharmacokinetics: None noted. Unique Side Effects: Tachycardia, hypertension, even fatalities have been associated with excessive use of inhaled sympathomimetics |
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→ xylometazoline
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Pharmacological Class: Selective α1 agonist.
Mechanism of Action: Vasoconstriction of nasal mucosa and conjunctiva Primary Use: Relief of nasal and nasopharyngeal mucosal congestion. Nasal spray Unique Pharmacokinetics: None noted. Unique Side Effects: Drowsiness, dizziness, blurred vision |
