Term
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Definition
| highly selective alpha 1 blocker - does not inc. heart rate |
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Term
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Definition
| selective alpha 1 antagonist - dec. size of prostate |
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Term
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Definition
| selective alpha 1 antagonist - dec. size of prostate - 20 hr half life |
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Term
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Definition
more selective for alpha 1a,1d than alpha 1b (alpha 1b - impt in blood vessels, alpha 1a impt in prostate) - little effect on blood pressure (can be used in pts w/ postural HTN) - Relaxes the prostate, and bladder sphincter - tx for BPH
Side effect: Difficulty w/ ejaculation |
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Term
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Definition
selective alpha antagonist (not quite as selective as Tamsulosin) - little effect on blood pressure (can be used in pts w/ postural HTN) - Relaxes the prostate, and bladder sphincter - tx for BPH
Side effect: Difficulty w/ ejaculation, dizziness |
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Term
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Definition
| alpha 2 selective antagonist marketed as natural alternative to Viagra |
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Term
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Definition
| reversible alpha partial agonists/antagonists |
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Term
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Definition
| Competitive antagonist of alpha 1 and alpha 2 for short term tx of hypertensive crisis of pheochromocytoma, or pts on MAOI's who ingest tyramine or after abrupt withdrawal from clonidine |
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Term
| Phenoxybenzamine (Dibenzyline) |
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Definition
| Irreversible alpha 1 blocker (small amts of alpha 2) - Used for short term (wks before surgery) tx of pheochromocytoma |
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Term
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Definition
Direct cholinergic agonist - Favors M receptors (especially M3)
A: PO and SC
D: Poor lipid solubility; does not X-BBB
DOA: Longer duration of action than ACh due to resistance to cholinesterases
Tx: Used to enhance normal functioning of GI tract and bladder postoperatively |
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Term
| Pilocarpine (Isopto Carpine; Pilorcar) |
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Definition
Direct cholinergic agonist - Favors M receptors
A: PO and ophthalmic drops; well absorbed
D: Good lipid solubility
Tx: wide-angle glaucoma (acts by constricting the ciliary muscle, which opens the meshwork of he canal of Schlemm) - Used to treat xerostomia in pts w/ head and neck cancers |
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Term
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Definition
Direct cholinergic agonist - Favors M receptors
A: PO
D: Moderate lipid solubility
M: Hepatic metabolism by P450 enzymes
E: Parent drug and metabolites excreted in the urine
Tx: Used to treat xerostomia associated with Sjogren's syndrome |
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Term
| Carbachol (Isopto Carbachol) |
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Definition
Direct cholinergic agonist - More Nicotinic activity than Muscarinic
A: ophalmic drops and intraoptic
D: Poor lipid solubility does not X BBB
DOA: Longer duration of action than acetylcholine due to resistance to acetylcholinesterase
Tx: wide-angle glaucoma (acts by constricting the ciliary muscle, which opens the meshwork of the canal of schlemm) |
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Term
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Definition
Indirect cholinergic agonist - reversible bind directly to acetylcholineseterase
A: IM and IV
D: No CNS effects
E: In urine
Tx: Used in diagnosis of myasthenia gravis |
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Term
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Definition
Indirect cholinergic agonist (Carbamate)
A: IM, IV, SC, and PO
M: hyrolyzed by cholinesterases
E: Parent drug and metabolites excreted in urine
Tx: DOC for paralytic ileus and atony of the bladder from surgery - Tx and diagnosis of masthenia gravis - Reversal of NM blockade |
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Term
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Definition
Indirect cholinergic agonist (Carbamate) - Reversibly bind directly to acetylcholineseterase
A: IM, IV, and ophthalmic
M: Hydrolyzed by cholinesterases
E: Parent drug and metabolites excreted in urine
Tx: Applied topically for wide-angle glaucoma - Tx of CNS toxicity associated w/ anticolinergic poisoning |
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Term
| Echothiophate (Phospholine iodide) |
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Definition
Indirect cholinergic agonist (organophosphate) - Irreversibly bind to acetycholineseterase)
A: Well absorbed through the skin, lung, gut, and conjunctiva
M: Metabolized (especially in insects) by mixed function oxygenases to active form
Tx: Glaucoma (second line agent)
Tox: 2-PAM reverses |
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Term
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Definition
Indirect cholinergic agonist (organophosphate) - insecticide
A: Well absorbed through the skin, lung, gut, and conjunctiva
M: Metabolized (especially in insects) by mixed function oxygenases to active form
Tx: Glaucoma (second line agent)
Tox: causes most cases of poisoning and death associated w/ organophosphates 2-PAM reverses |
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Term
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Definition
Indirect cholinergic agonist (quaternary alcohol)
A: PO
M: Metabolized by hepatic P450 enzymes
E: Parent drug and metabolites excreted in urine
Tx: Alzheimers |
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Term
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Definition
| Pervents enzyme aging in organophosphate toxicity - must be administered rapidly |
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Term
| Atropine (Sal-Tropine, Isopto Atropine) |
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Definition
Muscarinic Antagonist (Tertiary Amine) - Act as competitive inhibitors - Effects can be overcome by increased concentrations of muscarinic agoinists
A: Endotracheal, IM, IV, PO, SC, and ophthalmic drops
D: well distributed; crosses BBB
M: Hepatic Metabolism
E: Parent drug and metabolites excreted in urine
Tx: Reverse muscarinic or antiacetylcholine sterase poisoning, mydriasis w/ cycloplegia, mydriasis for prolonged periods of time, Cardiac Arrest
Contraindications: Can precipitate acute flaucoma in pts w/ narrow anterior chamber angle, Can precipitate hypertheria in infants, Should not be used in men w/ BPH |
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Term
| Scopolamine (Isopto Hyoscine, Hyoscine) |
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Definition
Muscarinic Antagonists (Tertiary Amine)
A: IM, IV, PO, SC, ophthalmic, or transdermal patch
D: Crosses BBB
M: Hepatic metabolism
E: Metabolites excreted in urine
Tx: Tx and prevention of motion sickness, dilation for eye exams |
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Term
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Definition
Muscarinic Antagonist (quaternary Amine)
A: Inhaled
D: Poorly absorbed; does not X-BBB
E: In urine and feces
Tx: Bronchodilator in asthma and COPD
SE: Can precipitate hyperthermia in infants |
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Term
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Definition
Muscarinic antagonist (M3 selective)
D: not lipid soluble, few CNS side effects (preferred drug in elderly)
Tx: overactive bladder |
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Term
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Definition
Muscarinic antagonist
Tx: used to prevent bladder spasm after prostate surgery |
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Term
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Definition
Muscarinic Antagonist
Tx: used in surgery to block excessive vagal tone, decrease muscarinic side effects when neostigmine or other cholinesterase inhibitors are used to treat myasthenia gravis |
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Term
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Definition
Muscarinic antagonist
Tx: Produces dilation of pupil (myadriasis and cycloplegia); useful for funduscopic examinations
SE: blurred vision, headache, sensitivity to light, risk of antimuscarinc poisoning if enters systemic circulation |
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Term
| Homatropine (Isopto Homatropine) |
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Definition
Muscarinic antagonist
Tx: Produces dilation of pupil (myadriasis and cycloplegia); useful for funduscopic examinations
SE: blurred vision, headache, sensitivity to light, risk of antimuscarinc poisoning if enters systemic circulation |
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Term
| Diphenoxylate-atropine (lomotil) |
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Definition
Muscarinic Antagonist
Tx: Atropine combined with an opoid to prevent diarrhea |
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Term
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Definition
Nondepolarizing NM blocker (Isoquinoline derivative)
DOA: Long
OOA: Slow
E: via kidney (some have minor hepatic elimination as well)
MOA: Competitive inhibition of Ach at the nicotinic receptors of the NMJ
SE: Moderate histamine release, Hypotension (due to histamine release and ganglionic blockade)
Tx: Used by anesthesiologists in the OR for surgical muscular relaxation |
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Term
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Definition
Non-depolarizing NM blocker (steroid derivative)
DOA: Long
OOA: Slow
E: via kidney
SE: Moderate blockade of cardiac muscarinic receptors causing tachycardia, Blocks autonomic ganglia |
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Term
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Definition
Non-depolarizing NM blocker (steroid derivative)
DOA: Intermediate
OOA: Intermediate
M: Hepatic
E: Biliary
SE: Low incidence of toxicity |
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Term
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Definition
Non-depolarizing NM blocker (isoquinolone derivative)
DOA: Short
OOA: Rapid
M: Via plasma cholinesterase
SE: Slight histamine release, Hypotension (due to histamine release and ganglionic blockade) |
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Term
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Definition
Non-depolarizing NM blocker (Steroid derivative)
DOA: Intermediate
OOA: Rapid
M: Hepatic
E: Biliary
SE: Low incidence of toxicity |
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Term
| Succinylcholine (Anectine) |
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Definition
Depolarizing NM blocker (dimer of Ach)
DOA: Short
OOA: Rapid
M: via plasma cholinesterase
MOA: Acts like a nicotinic agonist at NMJ, Causes fasciculations followed by paralysis due to persistent depolarization of the end plate
SE: hyperkalemia, increased intraocular pressure, increased intragastric pressure, muscle pain/damage, slight histamine release, stimulates autonomic ganglia, stimulates cardiac muscarinic receptors causeing bradycardia, interactions w/ other meds (aminoglycosides) |
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Term
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Definition
Non-depolarizing ganglionic blocker (Tertiary ammonium)
A: PO
E: Unchanged in urine
MOA: Competitive inhibitor of Ach at nicotinic receptors on postgonglionic autonomic neurons, Blocks sympathetic ganglia causeing casodilation and decreased HR
Tx: Hypertension
SE: CNS side effects (convulsions, mental changes, tremors, confusion), Hypotension. |
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Term
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Definition
Non-depolarizing ganglion blocker
Tx: not used clinically
MOA: Effects depend on predominant tone of an organ (sympathetic or parasympathetic) |
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Term
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Definition
Catecholamine - alpha 1, alpha 2, beta 1, and beta 2 agonist
A: IV, IM, PO, SC, Intracardiac, endotracheal, and topical
Tx: Lowering intraocular pressure in wide-angle glaucoma, Combined w/ local anesthetics to prolong their action, Topical use for hemostasis, Tx of complete heart block or cardiac arrest, Bronchodilator for Tx of asthma, Tx of anaphylactic shock
SE: HR increase, BP increase (pulse pressure increase), TPR decreases slightly |
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Term
| Norepinephrine (Levophed) |
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Definition
Catecholamine - alpha 1 and alpha 2 agonist, some beta 1 activation
A: IV
Tx: Treatment of hypotension (causes vasoconstriction)
SE: HR decreases (vagal mediated central reflex), BP increases (pulse pressure same), TPR increases |
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Term
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Definition
Catecholamine - beta 1, and beta 2 agonist
A: IM, IV, SC, and inhaled
Tx: Bronchodilator for tx of asthma, Complete heart block or cardiac arrest, Shock
SE: HR increases, BP decreases (pulse pressure increases), TPR decreases |
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Term
| Phenylephrine (Neo-Synephrine) |
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Definition
alpha 1 agonist
Tx: often added in small concentrations to OTC drops to whiten the sclera vai vasoconstriction, Used to vasoconstrict vessels in the nasal mucosa to aid nasal congestion
SE: Causes rebound dilation and redder eyes, irregular heartbeat, Headache, Dizziness, Tremor |
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Term
| Pseudoephedrine (Sudafed) |
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Definition
Alpha agonist
MOA: vasoconstriction of the nasal mucosa
Tx: Vasoconstriction effect on respiratory vasculature casues decrease in nasal congestion
SE: Containdicated in pts w/ HTN, past MI, or hyperthyroidism because it increases BP |
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Term
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Definition
alpha 2 agonist
A: PO and transdermal (good for noncompliant pts; provides steady-state blood levels, also fewer side effects)
M: 50% hepatic metabolism
E: Majority excreted unchanged in urine
MOA: Inhibit renin release by inhibiting the sympathetic nervous system, Renin release is the rate limiting step in the renin-angiotensin system
Tx: Hypertension, CHF, as effective as methyldopa but requires lower dose
SE: Many adverse effects associated w/ the inhibition of the sympathetic nervous system due to non-selective nature of these medications, Bronchoconstriction, Hypotension, Bradycardia, Sexual Dysfunction, Xerostomia, Constipation, Drowsiness, dizziness, headache, High dose will cause interaction with alpha 1 receptors leading to vasoconstriction and increased BP. |
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Term
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Definition
Beta 1 agonist
A: IV
M: metabolized in urine and plasma by COMT
E: metabolites excreted in urine
MOA: Leads to an elevation of cAMP and subsequent positive inotropic effects, Low chronotropic activity
Tx: Treatment of acute CHF
SE: Increased HR and BP, Angina |
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Term
| Albuterol (Ventolin, Proventil) |
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Definition
beta-2 adrenergic agonist
A: inhalation and PO
DOA and OOA: short
M: hepatic metabolism
E: Parent drug and metabolites excreted in urine
Tx: Bronchodilators for tx of asthma
SE: Not many SE, Skeletal muscle tremors |
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Term
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Definition
beta-2 agonist
A: IV and PO
Tx:Bronchodilators for tx of asthma, Also used to stop premature contractions in pregnant women
SE: Minimal SE, Skeletal muscle tremor |
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Term
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Definition
alpha and beta agonist - Causes release of NE
A: IM, IV, PO, and SC
Tx: Bronchodilator for Tx of asthma, Tx of nasal congestion, Tx and hypotension and shock
SE: Restlessness, Tremor, Insomnia, Anxiety, Tachycardia |
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Term
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Definition
alpha and beta agonist - Causes release of DA, NE, and 5-HT from nerve terminal
A: PO
Tx: Tx of ADHD, Tx of Narcolepsy, Tx of exogenous obesity
SE: Restlessness, Tremor, Insomnia, Anxiety, Tachycardia |
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Term
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Definition
alpha and beta agonist
MOA: Blocks reuptake of DA, NE and 5-HT, Strong action in DA pathways (pleasure pathways) of the CNS
Tx: Vasoconstrictor and local anesthetic utilized clinically in ENT applications, Stimulation, Euphoria
SE: Strong physiologic dependence, Arrhythmias, Seizures, Respiratory depression, Hypertensive crisis (increased risk of CVA and MI), Psychotic state with LTU |
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Term
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Definition
Indirect acting sympathomimetic
A: IV
MOA: Release of stored catecholamines, has a NE type effect
M: Hydrolyzed by MAO in the gut and liver (no PO admin)
SE: In pts treated w/ MAOI's for depression, tyramine may cause a severe hypertensive crisis |
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Term
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Definition
alpha-1, alpha-2, and beta-1 agonist - (actives D1 receptors in renal vascular beds --> increased renal blood flow) Stimulates NE release
A: IV
M: Metabolized in liver, kidneys, and plasma by MAO and COMT
E: Metabolites excreted in urine
MOA: Causes release of NE at the heart, which leads to beta-adrenergic stimulation, Stimulates beta-1 receptors, Inhibits NE release in the periphery causing vasodilation
Tx: Tx of acute CHF, Also used to tx acute renal failure, shock, and cardiac arrest, Important
SE: Dyspnea, Angina, Tachycardia, Headache, Nausea, Vomiting |
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Term
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Definition
Dopamine receptor agonist (selective D1 agonist)
MOA: Dilation of vascular beds, decreasing BP
Tx: produce rapid decrease of BP in severe HTN |
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Term
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Definition
Non-selective beta blocker
High lipid solubility, high plasma binding
t1/2 = 3-6 hrs
A: PO, IV
ISA: NO
MSA: yes, high
Tx: glaucoma by decreasing production of aqueous humor, Arrhythmias, Hypertension, Angina, Hyperthyroidism, Migraine, Situational phobias |
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Term
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Definition
Non-selective beta blocker
Moderate lipid solubility, Low plasma binding
t1/2 = 4-5 hrs
A: PO, ophthalmic
ISA: No
MSA: No
Tx: glaucoma, HTN, Angina, Hyperthyroidism |
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Term
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Definition
Selective beta-1 blocker
- moderate lipid solubility - low plasma binding - t1/2 = 3-4 hrs - A: PO, IV - ISA: No - MSA: No - MOA: Tx of HTN via decreased HR, CO, contractility, renin release by kidney, and BP via CNS actions, Tx of angina via decreased HR, contractility, heart work, and oxygen consumption, Tx of hyperthyroidism by blocking thyroxin, which causes beta-1 stimulation of the heart - Tx: HTN, Angina, Hyperthyroidism |
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Term
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Definition
| Selective beta-1 blocker - low lipid solubility - low plasma binding - t1/2 = 6-9 hrs - A: PO, IV - ISA: No - MSA: No - MOA: Tx of HTN via decreased HR, CO, contractility, renin release by kidney, and BP via CNS actions, Tx of angina via decreased HR, contractility, heart work, and oxygen consumption, Tx of hyperthyroidism by blocking thyroxin, which causes beta-1 stimulation of the heart - Tx: HTN, Angina, Hyperthyroidism |
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Term
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Definition
Cardiospecific or beta-1 blockers
Low lipid solubility - low plasma binding - t1/2 = 8-10 min - A: IV - ISA: No - MSA: No - MOA: Tx of HTN via decreased HR, CO, contractility, renin release by kidney, and BP via CNS actions, Tx of angina via decreased HR, contractility, heart work, and oxygen consumption, Tx of hyperthyroidism by blocking thyroxin, which causes beta-1 stimulation of the heart - Tx: Arrhythmias, Heart Failure, Bradycardia, Hypotension. |
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Term
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Definition
Selective beta-1 blocker
Tx: used for the tx of glaucoma, causes less bronchoconstriction when used in the eye than timolol. |
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Term
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Definition
| Non selective beta-blocker - moderate lipid solubility - t1/2 = 3-4 hrs - A: PO - ISA: yes (high) MOA: Has intrinsic sympathomimetic activity - Tx: HTN, Angina.....the risk of bradycardia may be lower, also don't affect plasma lipids as much as other beta blockers |
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Term
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Definition
| Selective beta-1 antagonist (blocker) with intrinsic sympathathomimetic activity - Tx: HTN, Angina.....the risk of bradycardia may be lower, also don't affect plasma lipids as much as other beta blockers |
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Term
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Definition
| Blocks beta-1, beta-2, and alpha-1 receptors - MOA: a-1 blockade leads to relaxation of arterial smooth muscle and decreased blood pressure, B-1 blockade prevents a compensatory increase in heart rate so that the decrease in blood pressure is less likely to cause tachycardia than when alpha-blockers are used alone - A: PO, IV - Tx: HTN |
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Term
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Definition
| Non selective beta-blocker that also blocks alpha-1 receptors - Membrane stabilizer - MOA: Causes vasodilation and decreases BP w/o causing tachycardia - t1/2 = 6-8 hrs - Tx: HTN, CHF - SE: Bradycardia, Dizziness, Hypotension |
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Term
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Definition
| Synthesis inhibitor (Neuronal Blocker) - A: PO - E: majority excreted unchanged in urine - MOA: Blocks tyroine hydroxylase, Interferes w/ DA synthesis, Therefore there is less NE and EPI sectreted by the tumor (pheochromocytoma) - Tx: Used to tx pheochromocytoma (especially in pts w/ metastatic or inoperable disease) - SE: crystalluria, sedation, Diarrhea, Anxiety. |
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Term
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Definition
| blocks transport of Ach into vesicles after formation in the presynaptic neuron terminal |
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Term
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Definition
| blocks release of Ach from presynaptic terminal |
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Term
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Definition
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Term
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Definition
| Blocks the conversion of tyrosine to l-dopa (rate limiting step in DA and NE production) |
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