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

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