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87 terms

Pharmacology EXAM 1

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Botulinum Toxin
Cholinergic: blocks ACh release by blocking exocytosis
Methyldopa
Adrenergic: inhibitor of aromatic L-amino acid decarb., "false neurotransmitter", displaces NE (treatment of hypertension)
Darifenacin
nicotinic cholinergic: Muscarinic ACh receptor (newer)
Phenylephrine
a1: selective a1 agonist, increased smooth muscle contraction, genitourinary
Clonidine
a2: a2 agonist, reduced sympathetic outflow, increase smooth muscle relaxation and neurotransmitter inhibition, aggregation of platelets decrease NE release
Dobutamine
B1: selective cardiac stimulation (also a1), increase heart contraction
Terbutaline
B2: selective B2 agonist, select inhibiton of smooth muscle contraction, produces bronchodilation with minimal heart effect
Metroprolol
B1 antagonist: selective B1 receptor blockade, antagonize cardiac actions of catecholamines, less antagonism of bronchioles, decreased renin
Atenlol
B1 antagonist: selective B1 receptor blockade, antagonize cardiac actions of catecholamines, less antagonism of bronchioles, decreased renin
Prazosin
a1 antagonist: selective a1 blockade (reversible), inhibiting vascular smooth muscle contraction (causes relaxation)
Imipramine
adrenergic: tricyclic antidepressant, interfers with NET at adrenergic synapse in CNS/inhibits reuptake, NE accumulates at receptors
Entacapone
adrenergic: COMT inhibitor peripherally, attenuates levadopa toxicity on dopamine neurons--used as an adjunct in Parkinson's
Talcapone
adrenergic: COMT inhibitor in brain, enhances dopamine activity in Parkinson's
Tranylcypromine
adrenergic: irreversible MAO inhibitor, increases bioavailability of tyramine, little direct effect on NE or sympathetic response
Reserpine
adrenergic: inhibits monoamine transport into vesicles, blocks VAMT-2 uptake, destruction of NE by mitochondrial MAO and depletion of adrenergic terminals
Propranolol
B1, B2: nonselective B receptor blockade antagonist
Phenoxybenzamine
a1, a2: nonselective a receptor blockade (irreversible)
Selegiline
adrenergic: selective and irreversible MAO-B inhibitor, adjuct in Parkinson's, less likely to increase BP
Phenelzine
adrenergic: nonselective irreversible MAO inhibitor (antagonist), little direct effect on NE or sympathetic response, potentiation of tyramine(inc. bioavail)
Isocarboxazid
adrenergic: irreversible MAO antagonist, increase bioavail of tyramine in foods containing MAO
Bretylium
adrenergic: prevents release of transmitter (NE by nerve impulses), can transiently stimulate NE release, displace amine from storage sites
Guanedrel
adrenergic: prevents release of transmitter (NE by nerve impulses), can transiently stimulate NE release, displace amine from storage
Guanethidine
adrenergic: prevents release of transmitter (NE by nerve impulses), can transiently stimulate NE release, displace amine from storage
Trimethaplan
nicotinic cholinergic: selective competitive Nn blockade of postsynaptic receptor causing ganglionic blockade
Hexamethonium
nicotinic cholinergic: selective competitive Nn and noncompetitive ganglionic blocking agents
Succinylcholine
depolarizing agent, produces selective neuromuscular blockade
Tubocurarine
nicotinic cholinergic: blockade of postsynaptic receptor, neuromuscular blockade at both motor end plates and autonomic (end plate more)
Pirenzapine
nicotinic cholinergic: new muscarinic agent
Tripitramine
nicotinic cholinergic: new muscarinic agent
Isoproterenol
B1, B2: highest potency agonist of B receptors (lowest for a), mimic transmitter, increase heart contraction and smooth muscle relaxation
Moclobemide
reversible MAO-A selective inhibitor, less likely to cause large increase BP
Pargyline
MAO inhibitor, can increase NE, dopamine, 5HT in brain and tissue
Nialamide
MAO inhibitor, can increase NE, dopamine, 5HT in brain and tissue
Ephedrine
adrenergic: indirect sympathomimetric drug, displaces NE from nerve terminals and extracellular fluid, rapid and brief (increases signaling), tachyphlaxis
Tyramine
adrenergic: adrenomemetric, displaces NE from nerve terminals and extracellular fluid, repeated administration lowers effect (tachyphlaxis)
a-methyltyrosine
adrenergic: interfers with synthesis of NE, depletion of NE, blocks tyrosine hydroxylase, treatment pheochromocytoma
Cocaine
adrenergic: blocks NET, interfers with catecholamine effect, inhibits ACh reputake, transport system blocker, results in accumulation of NE
Yohimbine
a2: selective a2 antagonist, increase insulin secretion, inhibit smooth muscle relaxation (cause contraction)
Hemicholinium
cholinergic: high-affinity system inhibition, blocks choline uptake with depletion of ACh, synthetic
Vesamicol
cholinergic: blockade of transport system storage vesicle, prevents release/storage of ACh
Acetylcholine
muscarinic agonist: quaternary, produces miosis during eye surgery, side effects: hypotension, bradycardia, flushing, breathing difficulty, corneal edema and clouding
Methacholine
muscarinic agonist: synthetic quarternary choline ester, greater duration/selectivity (than ACh), diagnosis of asthma, side effects: dyspnea (difficult breathing), lightheadedness, headache, pruritus (itching sensation), throat irritation, resistant to AChase, selective cardiovascular M cholinergic receptors
Carbachaol
muscarinic agonist: synthetic quarternary, resistant to cholinersterases, used for glaucoma (miosis and decreased ocular pressure) side effects sweating, shivering, dizzy, increased urination, rhinitis, contract detrusor, increase voiding P, decrease bladder, increase ureteral peristalsis, relax trigone and external sphincter
Bethanecol
muscarinic agonist: synthetic quarternery, resists cholinesterases, treat urinary retention and inadequate emptying, treat gastric atony, treat dry mouth (less sweat that pilo) side effects sweating, shivering, dizzy, increased urination, rhinitis, contract detrusor, increase voiding P, decrease bladder, increase ureteral peristalsis, relax trigone and external sphincter
Cevimeline
muscarinic agonist: treat xerestomia (dry mouth) in Sjoren's, fewer side effects than Pilo., miotic action for treatment of narrow angle glaucoma attack, side effects sweating, shivering, dizzy, increased urination, rhinitis, contract detrusor, increase voiding P, decrease bladder, increase ureteral peristalsis, relax trigone and external sphincter
Pilocarpine
muscarinic agonist: natural, sweat gland sensitive, treats xerestomia (dry mouth) of Sjoren's, treats glaucoma, side effects sweating, shivering, dizzy, increased urination, rhinitis, contract detrusor, increase voiding P, decrease bladder, increase ureteral peristalsis, relax trigone and external sphincter
Metoclopramide
muscarinic agonist: combined cholinergic agonist and dopamine antagonist, replace bethanecol in gastroparesis (inadequate stomach empty) or GERD
Atropine
muscarinic antagonist: natural, no CNS effect, USES: anticholinesterase OD, symptomatic bradycardia, preanesthesia, exsessive salivation/mucus, mushroom antidote, SIDE EFFECTS: arrhythmia, coma, respiratory depression, increase ocular P, tachycardia, constipation, xerostomia, blurred vision (don't use with narrow angle glaucoma)
Scopolamine
muscarinic antagonist: effects CNS, causes CNS depression, drowsiness, amnesia, fatigue and dreamless sleep, can cause euphoria, used for motion sickness (don't use with narrow angle glaucoma)
Homatropine
muscarinic antagonist: synthetic, shorter duration that Atropine, USES: mydriasis (pupil dilation) and cycolpegia (paralyze cilliary) for refraction, acute inflammation of uveal tract, SIDE EFFECT: increase intraocular P, systemic anticholinergic, local irriation, vacular congestion, edema, exudate, eczema
Tropicamide
muscarinic antagonist: myriasis for fundus exam, cyclopegia for refraction, SIDE EFFECTS: cardio events, stinging, blurred vision, photophobia
Dicylomine
muscarinic antagonist: IBS, minor diarrhea, SIDE EFFECTS: increased ocular P, tachycardia, urinary retention, confustion (don't use if narrow angle glaucoma, GI block, myasthenia gravis)
Hyoscyamine
muscarinic antagonist: peptic ulcer disease, IBS, hypermotility SIDE EFFECTS: increase intraocular P, tachycardia, dry mouth, uriniary hesitancy/retention, blurred vision, mydraisis
Methscopalamine
muscarinic antagonist: quarternary, lacks central actions of scopolamine, use in GI disease, peptic ulcer
Glycopyrrolate
muscarinic antagonist: orally to inhibit GI motility, parentally to block vagal stimulation during surgery
Mepenzolate
muscarinic antagonist: peptic ulcer, decrease gastric acid and pepsis, supress colon, SIDE EFFECT: increase intraocular, tachycardia, palpitations, dry mouth, urinary hesitancy and retention, blurred vision, mydriasis
Metoclopramide
muscarinic antagonist: GI motility, prevent chemo vomit, SIDE EFFECT: extrapyramidal, restlessness, drowsiness, fatigue, nausea, dry mouth, diarrhea/constipation (don't use with pheochromocytoma, seizure, antipsych) linked to tardive dyskinesia
Ipratropium
muscarinic antagonist: quarternary, inhaled, for cold (rhinorrhea), COPD, asthma SIDE EFFECTS: paralytic ileus, throat swelling, bad taste, dry mouth; blocks all M
Tiotropium
muscarinic antagonist: quarternary, inhaled, for cold (rhinorrhea), COPD, asthma SIDE EFFECTS: paralytic ileus, throat swelling, bad taste, dry mouth; admin as dry powder
Oxybutynin
muscarinic antagonist: overactive bladder, urge incontinence, SIDE EFFECTS constipation, diarrhea, nausea, dry mouth, erythema, prurits (don't use with narrow angle glaucoma); transdermal, overcome dry mouth and eyes
Trospium
muscarinic antagonist: overactive bladder, urge incontinence, SIDE EFFECTS constipation, diarrhea, nausea, dry mouth, erythema, prurits (don't use with narrow angle glaucoma); quaternary, better tolerated than oxybutynin
Tolterodine
muscarinic antagonist: overactive bladder, urge incontinence, SIDE EFFECTS constipation, diarrhea, nausea, dry mouth, erythema, prurits (don't use with narrow angle glaucoma); potent, urinary bladder selective
Darifenacin
muscarinic antagonist: overactive bladder, urge incontinence, SIDE EFFECTS constipation, diarrhea, nausea, dry mouth, erythema, prurits (don't use with narrow angle glaucoma); potentially block cholinergic bradycardia, block smooth muscle activity
Solifenacin
muscarinic antagonist: overactive bladder, urge incontinence, SIDE EFFECTS constipation, diarrhea, nausea, dry mouth, erythema, prurits (don't use with narrow angle glaucoma); newly approved with favored efficacy:side effect
Flovoxate
muscarinic antagonist: dysuria (painful urination), urgency, urge incontinence, SIDE EFFECT: nausea, vomitting, dry mouth, nervousness, antispasmodic
Benztropine
muscarinic antagonist: Adjunct for Parkinson's, reduces tremor more than bradykinesia, may worsen dementia and cog impairment in old
Trihexyphenidyl
muscarinic antagonist: Adjunct for Parkinson's, reduces tremor more than bradykinesia, may worsen dementia and cog impairment in old
Edrophonium
AChase inhibitor: diagnosis of myasthenia gravis, eaton-lambert syndrome, disorders of muscle weakness, short acting, rapid onset, quarternary
Neostigmine
AChase inhibitor: urinary or GI motility agent, glaucoma, neuromuscular diseases like myasthenia gravis, direct cholinergic agonist of Nm, quarternary, large parental dose, injected into denervated muscle envokes immediate contract, increase GI contract
Pyridostigmine
AChase inhibitor: urinary or GI motility agent, glaucoma, neuromuscular diseases like myasthenia gravis, nonpolar good for combat in CNS of anticholinergic toxicity, quaternary, reversible carbamate inhibitor
Amdenomium
AChase inhibitor: urinary or GI motility agent, glaucoma, neuromuscular diseases like myasthenia gravis
Physostigmine
AChase inhibitor: reversal of anticholinergic toxicity or induced paralysis in surgery, tertiary amine, reversible carbamate inhibitor, parentaerally admin, injection, eye solution/oint
Tacrine
AChase inhibitor: reversible, mild to moderate Alzheimer's, higher affinity, readily crosses BBB, long duration, use limited by hepatoxicity
Donepezil
AChase inhibitor: Alzheimer's, reversible, bind more to active center, crosses BBB, long duration, well tolerate single daily oral dose SIDE EFFECT: nausea, vomit, diarrhea
Rivastigmine
AChase inhibitor: Alzheimer's, high lipid soluble, cross BBB, long duration, similar to donepezil
Galantamine
AChase inhibitor: Alzheimer's, same as donepezil
Echothiophate
AChase inhibitor: quaternary ammonium organophosphate, ophthalmic admin, not skin penetrating, used for open angle glaucoma, topical use, replaced by long lasting cholinesterase inhibitor
Demacarium
AChase inhibitor: Open angle glaucoma, SIDE EFFECT: allergy, ab cramps, diarrhea, burning, red eyes, headache, decreased vision in low light
Pralidoxime
ACh inhibitor: Cholinesterase reactivator, treats anti-Chase intoxication
Procaine
local anesthetic: infiltration, obstetical, low hydrophobicity allows for rapid removal, low potency, excessive amount can decrease sulfanamides
2-chloroprocaine
local anesthetic: infiltration, obstetical, given epidurally before delivery, excessive amount can decrease sulfa drugs
Tetracaine
local anesthetic: topical, spinal (lower half), don't use if hypersensitive to cocaine, high hydrophobicity, longer duration, high potency, don't inject a lot in patients with heart block
Cocaine
local anesthetic: mucosal and ophthamalic, diagnosis of Horner's pupil, medium potency, medium duration, vasoconstrictive, cardiotoxic, euphoric
Lidocaine
local anesthesia: infiltratration, peripheral spinal block, epidural, spinal, topical, Class 1 antiarrhythmic, rapid onset, medium duration, moderate potency, Epi prolongs action
Prilocaine
local anesthesia: dental infiltration, nerve block, doesn't require Epi to prolong
Bupivacaine
local anesthesia: infiltration, regional, epidural, spinal, sympathetic nerve block, high potency, long duration, cardiotoxic limits use
Articaine
local anesthesia: dental, epidural, spinal, regional, largely in dentistry