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Exam 2
pharm exam 2
88
Pharmacology
Graduate
10/06/2011

Additional Pharmacology Flashcards

 


 

Cards

Term

 

 

Direct acting muscarinic agonists 

Definition
- acetylcholine

- carbachol

- methacholine

- bethanechol

- pilocarpine (Salagen)

- muscarine

- cevimiline (Evoxac)
Term

 

 

Reversible cholinesterase Inhibitors 

Definition
- edrophonium

- physostigmine/eserine

-neostigmine

-pyridostigmine

- rivastigmine

- donepezil

- carbamate insecticides (e.g. Carbaryl)
Term

 

 

Irreversible cholinesterase inhibitors 

Definition
- DFP/diisopropylfurophosphate/isofluorophate & echothisophate

- organophosphate insecticides (Parathion, Malathion)

- nerve gases (used in chemical warfare, e.g. Sarin)
Term

 

 

cGMP phosphodiesterase (PDE-5) inhibitors 

Definition
- Sildenafil (Viagra) -onset 30 m; peak blood lvls 1 h; duration 4 h

-Vardenafil (Levitra) -onset 30 m; peak blood lvls 1 h; duration 4 h

-tadalafil (Cialis) - onset 45 m; duration 36 h because longer half-life

-MOA: inhibit PDE-5, which normally degrades the vasodilatory cGMP; vasodilation = erection

-side effects: may inhibit PDE-5 in peripheral tissues, leading to vasodilation, hypotension, and a subsequent reflex tachycardia (pts. must have CV function assessed before being given these drugs)
Term

 

 

Muscarinic Antagonists 

 

Definition
- atropine, homoscyamine, homoatropine

- scopolamine, methoscopolamine

-dicyclomine

-propantheline

-glycopyrrolate

-ipratropium

-tiatropium

-benzotropine

-trihexyphenidyl

-tolteridine

-oxybutynin

-solifenacin

-tropicamide
Term

 

 

Acetylcholine 

Definition
- muscarinic agonist

-NEVER administered via IV b/c rapidly degraded by plasma "pseudocholinesterase"

-used to tx. glaucoma
Term

 

 

Carbachol 

Definition
- muscarinic agonist; ACh analog

-resistant to hydrolysis by cholinesterases

-stimulates nicotinic + muscarinic receptors

-used to tx. glaucoma
Term

 

 

Methacholine 

Definition
-muscarinic agonist; ACh analog

-stimulates only muscarinic, not nicotinic, receptors

-used for pulmonary function testing in asthmatics
Term

 

 

Bethanechol 

Definition
-muscarinic agonist; ACh analog

-resistant to rapid hydrolysis

-stimulates only muscarinic, not nicotinic, receptors

-used in the tx. of urinary retention; stim. GI motility
Term

 

 

Pilocarpine (Salagen, Ocusert Pilo)

Definition
-muscarinic agonist

-used to tx. glaucoma + xerostomia
Term

 

 

Toxic effects of acetylcholinesterase inhibitors (reversible OR irreversible)  

Definition
- S.L.U.D.G.E

-S -salivation
-L-lacrimation
-U-urination
-D-defecation
-G-GI distress
-E-emesis

-muscle fasciculations followed by paralysis due to desensitization of nicotinic receptors

-bradycardia, hypotension, shock
Term

 

 

Treatment of acute cholinesterase inhibitor poisoning 

Definition
(1) high doses of atropine (2-4 mg IV) + 2 mg IM every 10 min to block muscarinic receptors

(2) if organophosphate (i.e. irreversible) poisoning, follow with pralidoxime to reactivate acetycholinesterase

(3) supportive treatment (i.e. diazepam for seizures)
Term

 

 

Echothiophate

Definition
-irreversible/slowly reversible acetylcholinesterase inhibitor

- used in tx. of glaucoma
Term

 

 

Rivastigmine (Exelon)

Definition
-reversible acetycholinesterase inhibitor

- used in tx. of Alzheimer's disease

-Alzheimer's - loss of cholinergic neurons in nucleus basalis of Meynert

-used along with donepezil
Term

 

 

Donepezil (Aricept) 

Definition
-reversible acetylcholinesterase inhibitor

-used in the treatment of Alzheimer's, along with Rivastigmine
Term

 

 

Physostigmine 

Definition
-reversible acetylcholinesterase inhibitor

-used to tx. atropine/muscarinic antagonist poisoning

-nonquaternary - CAN ENTER CNS
Term

 

 

Pyridostigmine 

Definition
- used to tx. Myasthenia gravis

-used by military to protect personnel against nerve agents; "pre-exposure antidotal enhancement"
Term

 

 

Diagnosis and Treatment of Myasthenia Gravis 

Definition
(1) diagnosis - Edrophonium (Tensilon)

(2) tx. - neostigmine, pyridotigmine

*Edrophonium, neostigmine, pyridostigmine quaternary ammonium compounds - DO NOT ENTER CNS
Term

 

 

Pralidoxime 

Definition
-acetycholinesterase reactivator

-not effective with carbamate insecticide poisoning
Term

 

 

Carbamate insecticides (carbaryl) 

Definition
-reversible acetycholinesterase inhibitor

- tx. (1) atropine, but pralidoxime is NOT useful
Term

 

 

DFP/isofluorphate 

Definition
-irreversible acetylcholinesterase inhibitor

-tx. poisoning with (1) atropine, (2) pralidoxime
Term

 

 

Botulinum toxin 

Definition
- toxin prevents release of acetycholine from nerve endings - affects both autonomic nerve endings (classic anticholinergic effects) and NMJ (paralysis)

-death from diaphragmatic paralysis

-tx: symptomatic support + Ab against toxin
Term

 

 

S/S of anti-muscarinic agent poisoning:

Definition
- dry, hot skin
-mydriasis, blurring of vision, photophobia
-CNS stimulation: agitation, hallucinations, seizures
-cessations of GI mobility (no bowel sounds)
-weak, rapid pulse
-tachycardia/tachyarrhythmia

-tx. with physostigmine + other cholinesterase inhibitor; benzodiazepines for seizures
Term

 

 

Atropine

Definition
-muscarinic antagonist

-natural

-racemix mixture of d,l-hyoscyamine; able to get into CNS (vs. homoatropine, which is not!!!)

-causes tachycardia, which may be preceded by a slight bradycardia

-used in the tx. of certain types of MIs where there is an increase in vagal tone (i.e. fall in BP + low cardiac output)

-CNS effects: low dose - sedative effects; mod doses - hallucinogenic effects; high doses - stimulant effects (agitation/seizures)
Term

 

 

Homoatropine 

Definition
-muscarinic antagonist

-synthetic analog of atropine

-does not enter CNS
Term

 

 

Scopolamine 

Definition
-muscarinic antagonist

-natural; structurally similar to atropine

-enters CNS!

-uses of scopolamine similar to atropine, but it has more of a CNS depressant effect (sedation/amnesia)

-used orally/patch form (Transderm Scop) for the prevention of motion sickness/vertigo
Term

 

 

Methscopolamine 

Definition
- muscarinic antagonist

-quaternary analog of scopolamine that does not enter CNS
Term

 

 

Dicyclomine (Bentyl) 

Definition
-muscarinic antagonist

-non-quaternary

-antispasmodic used in the treatment of IBS
Term

 

 

Propantheline (Pro-bathine) 

Definition
-muscarinic antagonist

-quaternary, so no CNS effects!

-antispasmodic used to treat IBS (same as dicyclomine)
Term

 

 

Glycopyrrolate (Robinul) 

Definition
-muscarinic antagonist

-quaternary, doesn't affect CNS

-used pre-op to dry respiratory secretions and inhibit vagal reflexes (i.e. bradycardia)
Term

 

 

Ipratropium (Atrovent) & Tiatropium (Spiriva) 

Definition
- muscarinic antagonist

- quaternary

-used in treatment of asthma & COPD

-Tiatropium - newer drug, longer acting
Term

 

 

Benztropine (Cogentin) & Trihexyphenidyl (Artane) 

Definition
- muscarinic antagonist

-centrally acting

-used in the treatment of idiopathic or drug-induced PD
Term

 

 

Tolterodine (Detrol) 

Definition
-muscarinic antagonist

-used to treat urinary incontinence
Term

 

 

Oxybutynin (Ditropan) 

Definition
-muscarinic antagonist

-used to tx. urinary incontinence
Term

 

 

Solifenacin (VESIcare) 

Definition
-muscarinic antagonist

-used to treat urinary incontinence
Term

 

 

Tropicamide (Midriacyl) 

Definition
-muscarinic antagonist

-used to pupillary dilation for ophtho exam
Term

 

 

Pancuronium (Pavulon) 

Definition
-competitive ACh antagonists that act at the neuromuscular junction
*because competitive, effects can be overcome by cholinesterase inhibitors

-blocks nicotinic receptors during surgery

-promote muscle relaxation
Term

 

 

Succinylcholine (Anectine) 

Definition
-depolarizing neuromuscular blocking drug
*b/c non-competitive, effects cannot be overcome by acetylcholinesterase inhibitors

-initially stimulates nicotinic receptors at the NMJ to cause weak contractions (fasciculations), then causes relaxation and paralysis
Term

 

 

 non-selective adrenergic receptor agonists

Definition
-epinephrine
-norepinephrine
-isopreterenol
-dopamine
Term

 

 

Selective B1 agonists 

Definition
-dobutamine (dobutrex)
Term

 

 

Selective B2 agonists 

Definition
-albuterol
-metaproterenol
-pirbuterol
-salmeterol
-terbutaline

-used as "bronchodilators" (most often as "rescue" inhalers)

-terbutaline used to manage premature labor by causing B2-mediated uterine relaxation
Term

 

 

Selective a1 agonist 

Definition
-phenylephrine
-midodrine (ProAmatine)

-phenylephrine: raises diastolic + mean BP, but with more reflex bradycardia than NE because NE also stimulates B1 in SA node

-uses of phenylephrine: (1) maintain diastolic BP during shock/spinal anesthesia, (2) hemorrhoids, (3) nasal congestion, (4) mydriatic agent (pupillary dilation mediated by a1 receptors), (5) tx. supraventricular tachycardia

-phenylephrine poor oral absorption

-uses of midodrine: (1) orthostatic hypotension (can be given orally), (2) tx. urinary incontinence (a1 constricts urinary sphincter)
Term

 

 

Indirect-acting sympathomimetics 

Definition
-cocaine
-pseudoephedrine (Sudafed) & ephedrine
-amphetamine & methamphetamine
- methylphenidate (Ritalin)
Term

 

 

Epinephrine 

Definition
- selectivity: a1 = a2 = B1 = B2

- at low IV doses, stimulates a2 & B2 receptors --> causes: decrease in diastolic BP, increase in systolic, increase in pulse pressure, but no change in MAP

-at higher doses, a1 & B1 receptors also stimulation --> NOW, increase in diastolic BP, increase in systolic, increase in pulse pressure, increase in MAP

-uses: (1) tx. circulatory collapse during anaphylactic shock, (2) bronchospasm during circulatory shock/asthma, (3) cardiac arrest, (4) bradycardia due to A-V block/sinus, (5) mixed w/ local anesthetics to prolong action at local sites of injection and to minimize local bleeding
Term

 

 

Norepinephrine 

Definition
-adrenergic receptor agonist

-a1 = a2 = B1 >> B2

-both low & high rates of IV infusion increase systolic, diastolic, MAP, and pulse pressure (but to higher degree at high rates)

-CAUSE REFLEX DECREASE IN HEART RATE

-uses: used during spinal anesthesia to prevent drop in MAP
Term

 

 

Isoproterenol 

Definition
-adrenergic agonist

- B1 = B2 >> all others

- both low & high rates decrease diastolic + mean pressures while increasing pulse pressure + heart rate

-uses: "pharmacologic provocation" to assist tilt-table tests for diagnosis of unexplained syncopes (vasovagal syncope)
Term

 

 

Dopamine 

Definition
-adrenergic agonist

-D receptor > B1 > a1 >>all others

-D receptors in GI/renal smooth muscle at low doses --> cause vasodilation
-B1 at intermediate doses
-a1 at high doses

-uses: (1) cardiogenic + neurogenic shock
Term

 

 

Dobutamine 

Definition
-selective B1 agonist

-mix of 2 stereoisomers: (1) a1 agonist, (2) potent B1 agonist + a1 antagonist

-B1 stimulation increases cardiac contractility, CO, pulse pressure; no change in diastolic at therapeutic doses

-uses: (1) CHF, (2) shock
Term

 

 

Cocaine 

Definition
-indirect acting sympathomimetic

-MOA: inhibits reuptake of NE

-good local anesthetic, exerts its own local vasoconstrictor action at site of local injection (slows its own loss from site)

-uses: (1) pain relief, (2) epistaxis while doing intubation of trachea through nose
Term

 

 

Pseudoephedrine (Sudafed)/Ephedrine 

Definition
-indirect acting sympathomimetic agent

-stimulates release of NE from nerve endings + stimulates adrenergic receptors DIRECTLY

-uses: (1) treat nasal/bronchial congestions --> promotes nasal & sinus drainage
Term

 

 

Sympathomimetics that must be administered orally

Definition
- a1 agonists: phenylephrine + midodrine

-B2 agonists: albuterol, metaproterenol, pirbuterol, salmeterol, terbutaline

-indirect-acting sympathomimetics (except cocaine) - pseudoephedrine + methamphetamine

-ACTION LASTS HOURS
Term

 

 

Sympathomimetics that must be administered parenterally

Definition
-B1 agonists : dobutamine

-cocaine

-E, NE, isoproterenol, dopamine

-ACTION LASTS FEW MINUTES
Term

 

 

B-blockers 

Definition
Cardioselective B-blockers:
-acebutelol (B1)
-atenolol (B1)
-esmolol (B1) - shortest duration (10 min)
-metoprolo (B1)

Non-selective B-blockers:
-nadolol (B1 + B2)
-pindolol (B1 + B2)
-propranolol (B1 + B2)
-timolol (B1 + B2)

*Labetalol (B-blocker + a-blocker)
Term

 

 

Partial agonists 

Definition
- acebutolol + pindolol

-preserve at least sm. amount of B-receptor function

-DO NOT INTERFERE WITH B2-MEDIATED BV RELAXATION --> CAN DECREASE TPR <--part of their anti-hypertensive mechanism!

-contain "intrinsic sympathetic/sympathomimetic activity (ISA)"
Term

 

 

Cell membrane stabilizing B-blockers 

Definition
-acebutolol + propranolol

-"local anesthetic" action only at high concentrations of the drug; therefore, this property has greater implications during overdosage
Term

 

 

Lipid solubilities of B-blockers 

Definition
-acebutolol - LOW LIPID SOLUBILITY
-atenolol - LOW
-esmolol - LOW
-metoprolol - MEDIUM
-nadolol - LOW
-pindolol - MEDIUM
-propranolol -HIGH
-timolol- MEDIUM

-significance: poorly lipid soluble drugs do not enter the CNS and are excreted, unchanged, through the kidney*; highly lipid soluble drugs DO enter the CNS and are metabolized by the liver before they are excreted

*exception is esmolol, which has low lipid solubility, but is rapidly inactivated by circulating (plasma + red blood cell) esterases
Term

 

 

Labetalol 

Definition
-B- and a1-blocker

- uses: (1) tx. of mod->severe HTN, (2) emergency tx. of hypertensive crisis

-MOA: a1 blockage is the primary mechanism by which this drug exerts its effect( --> decrease in TPR, decrease in MAP (MAP = CO*TPR))

-side effects: a-blockade = orthostatic hypotension (due to decreased vasoconstriction)
Term

 

 

Non-selective a (a1 + a2) blockers 

Definition
- phenoxybenzamine

-phentolamine
Term

 

 

Selective a1 blockers 

Definition
- prazosin
-terazosin
-doxazosin
-tamsulosin
-alfuzosin
-silodosin
Term

 

 

Phenoxybenzamine 

Definition
-nonselective a-blocker

-MOA: non-competitive inhibition (i.e. binding to a1 + a2 receptors irreversible); only synthesis of new receptors can restore a-adrenergic function

-uses: prevent severe catecholamine-induced HTN that occurs in pheochromocytoma patients during the pre-operative period prior to surgery; better than other drugs because catecholamines cannot over the irreversible blockade

Side effects:
-may inhibit histamine, serotonin, and ACh receptors, too.
-miosis, sedation, drowsiness, vomiting, lethargy (enters CNS)
-shock/circulatory failure (drug increases vasodilation)
Term

 

 

Phentolamine 

Definition
-nonspecific a-blocker

-competitive antagonist (unlike phenoxybenzamine); short acting

-uses:
(1) diagnosis of pheochromocytoma-->"Phentolamine test": following admin, short term drop in BP (35/25 mmHg after 5 mg phentolamine) suggests prescence of pheochromocytoma (normally, 5 mg doesn't cause fall in people w/o pheo)
(2) during surgical removal of pheo (prevents rise in BP due to catecholamines that are released during surgery)
(3) tx. overdose of a-agonist (e.g. NE)
(4) prevent local dermal tissue necrosis that may occur accidentally at sites of injection of a-agonists (due to local vasoconstriction)
(5) New form (OraVerse) used to reverse oral soft-tissue anesthesia resulting from intraoral submucosal injectio of a local anesthetic preparation containg a vasoconstrictor (e.g. E)
Term

 

 

Prazosin 

Definition
-selective a1 blocker

-uses:
(1) *long-term tx. of mild-mod primary hypertension, esp. when given with a diuretic to offset fluid retention*
(2) relax urinary sphincter and prostatic urethra, which relieves the obstructive urinary symptoms of BPH
(3) tx. of Reynaud's
(4) under consideration for tx. of nightmares related to PTSD

Side effects:
-orthostatic hypotension, but usually only sever during the first day of admin ("first dose phenomenon")
-salt + water retention
-some tachycardia
Term

 

 

Doxazosin/Terazosin 

Definition
-selective a1 blockers

-newer drug; MOA + uses almost identical to prazosin, but half-life much longer so may be better for long-term control of conditions like chronic HTN because fewer doses need to be remember by the patient

-(remember: prazosin - used to treat mild-mod primary HTN)
Term

 

 

Tamulosin/Silodosin 

Definition
-selective a1 blocker; more specifically, block a1A receptor (found ONLY in smooth muscle of bladder neck + prostate)

-uses: (1) tx. of BPH

-Tamulosin/Silodosin vs. Prazosin, which is also used to treat BPH -> Tamu/Silo have fewer systemic vascular actions because a1A receptors are found ONLY in neck of bladder/prostate
Term

 

 

Alfuzosin 

Definition
-selective a1 blocker

-uses: (1) tx. BPH --> not receptor sub-type selective like tamsulosin/silodosin, but exhibits "uroselectivity" (mechanism: uroselectivity thought to be due to the accumulation of alfuzosin in prostatic tissue, where it is 2x circulating plasma level)
Term

 

 

Peripherally-acting sympathetic neuronal blockers 

Definition
- decrease availability of the NE to its receptors

- reserpine

-guanethidine (Ismelin)
Term

 

 

Centrally-acting sympathetic neuronal blockers 

Definition
-stimulate a2 receptor sites in brain and indirectly reduce sympathetic neuronal traffic from central sympathetic vasomotor centers to peripheral CV organs via negative FB mechanism

-methyldopa
-clonidine
-guanabenz
-guanfacine
Term

 

 

Reserpine 

Definition
-peripherally acting sympathetic neuronal blocker

-MOA: decreases uptake of intraneuronal DA + NE into storage vesicles --> eventually depletes stored level of NE --> reduces amount released with each subsequent nerve impulse

-in CV system, decreases CO + TPR

-uses: (1) primary HTN

-side effects:
(1) sedation/mental depression (due to depletion in CNS)
(2) postural hypotension
(3) bradycardia
(4) fluid retention
(5) diarrhea (due to unopposed parasympathetic activity)
Term

 

 

Guanethidine 

Definition
-peripherally acting sympathetic neuronal blocker

-MOA: blocks intraneuronal reuptake of DA + NE (like reserpine), but ALSO directly blocks NE release from nerve endings

-NOT USED TO TX. HTN (UNLIKE RESERPINE) IN US

-notable interaction- guanethidine + tricyclic antidepressants: in order for guanethidine to be effective, must be taken up by the reuptake pump; reuptake prevented by antidepressants

-side effects:
(1) bradycardia
(2) orthostatic hypotension
(3) fluid retention
(4) NO CNS effects b/c it cannot enter brain (unlike reserpine)
(5) diarrhea (due to unopposed parasympathetic activity)
Term

 

 

a-Methyldopa/Methyldopa 

Definition
-centrally-acting adrenergic neuronal inhibitor

-pro-drug -> requires metabolism to its active form (methyldopa converted by DOPA decarboxylase to a-methylnorepinephrine) --> a-methylnorepi acts as a2 adrenergic agonist in central vasomotor centers

-causes decrease in renin release, HR, CO, and *TPR*

-use: tx. of HTN during pregnancy (drug does not harm fetus)

-side effects (common to all a2 agonists):
(1) peripheral fluid retention
(2) xerostomia
(3) sedation

-*induces a # of "autoimmune" disorders - (+) Coombs test, although hemolytic anemia is rarely present; abnormal liver function tests during 1st weeks of taking drug*
Term

 

 

Clonidine 

Definition
- centrally acting sympathetic neuronal blocker

- sm. dose required for therapeutic effect; administered transdermally (via patch)

-uses:
(1) tx. of primary HTN
(2) ADHD
(3) migraine
(4) menopausal hot flashes
(5) PTSD
(6) nicotine/alcohol withdrawl


-side effects:
(1) local skin reaction (contact dermatitis)
(2) rebound hypertension if the drug stopped abruptly
Term

 

 

Guanabenz/Guanfacine 

Definition
-centrally acting sympathetic neuronal blockers

-similar to Clonidine

-uses: (1) tx. of primary hypertension

-side effects (beneficial):
(1) lowers total serum cholesterol (may be high in hypertensives)
(2) causes less fluid retention
(3) less sedation and less rebound hypertension than with Clonodine

-Intuniv - Guanfacine for ADHD
Term

 

 

Ganglionic stimulant 

Definition
-nicotine (at low doses*) - acts on nicotinic receptors in autonomic ganglia + in skeletal muscle + in CNS

*at very high doses, nicotine acts as depressant
Term

 

 

Ganglionic blocking agents 

Definition
-mecamylamine

-blocks nicotinic receptors in autonomic ganglia, but not the nicotinic receptors in skeletal muscle (person can still move skeletal muscle)
Term

 

 

L-dopa 

Definition
-used in the treatment of Parkinson's disease

-amino-acid precursor that is transported to brain via active a.a. pump and converted to dopamine by the enzyme L-dopa decarboxylase

-in periphery, the portion of drug that does not cross the BBB, is metabolized by DOPA decarboxylase to form dopamine; peripheral dopamine converted to NE + E (some) & metabolites DOPAC + HVA (mostly)

-side effects:
(1) nausea/vomiting due to stimulation of the chemoreceptor trigger zone (CRTZ) by dopamine in the periphery
(2) tachycardia
(3) arrhythmias
(4) orthostatic hypotension
(5) CNS disturbances: depression, psychosis, hallucinations, nightmares, euphoria
(6) increased libido, release of inhibitions, compulsive behaviors
(7)*choreiform movements - after long term therapy

-USUALLY USED IN CONJUNCTION WITH CARBIDOPA
Term

 

 

Carbidopa 

Definition
-used in the treatment of Parkinson's in conjunction with L-dopa

-inhibits DOPA decarboxylase in the periphery, but does not cross BBB

-allows for reduction in the dosage of L-dopa given (b/c less is metabolized in the periphery) + its side effects
Term

 

 

Sinemet 

Definition
- used in the treatment of Parkinson's disease

-combination of L-dopa + Carbidopa

-2 formulations available: 10/100 (C/L), 25/100 (C/L)

-sustained release version: Sinemet CR
Term

 

Bromocryptine (Parlodel) 

 

Pergolide (Permax) 

Definition
-used in the treatment of Parkinson's disease

-ergot-derived non-specific dopamine receptor agonists

-not as effective as L-dopa, but used in patients that cannot tolerate L-dopa

-may decrease severity of "on-off phenomenon"

-*BROMOCRYPTINE HAS ALSO BEEN USED TO TREAT HYPERPROLACTINEMIA-INDUCED AMENNORHEA & GALACTORRHEA BECAUSE IT INHIBITS PROLACTIN SECRETION

-however, bromocryptine no longer recommended for new mothers who do not wish to breast feed because of the risk of psychosis & seizures; a new drug, carbergoline (Dostinex) recommended for hyperprolactinemia
Term

 

Ropinirole (Requip) 

 

Pramipexole (Mirapex) 

Definition
-used in the treatment of Parkinson's disease

-non-ergot derived dopaminergic receptor agonists (preferentially target D2 & D3 receptors)

-being used increasingly as first-line drugs

-side effects the same, but less severe than older dopamine receptor agonists (bromocryptine + pergolide):
(1) choreiform, dyskinetic movements
(2) nausea
(3) dizziness, confusion, sedation, behavioral changes, hallucinations

-Pramipexole (Mirapex) may have antioxidant and neuroprotective effects which may be beneficial for SLOWING THE PROGRESSION of the disease

-both drugs also used in the treatment of "restless leg syndrome"
Term

 

 

Amantadine (Symmetrel) 

Definition
-used in the treatment of Parkinson's disease

-originally used as an anti-viral agent

-stimulates the release of dopamine from nerve endings and may also inhibit its reuptake

-less effective than L-dopa; usually used as a supplement to L-dopa

-side effects:
(1) mental disturbances, hyperexcitability, ataxia, confusion, convulsions
(2) choreiform movements

-excreted by the kidney, so it requires proper kidney function
Term

 

 

Selegiline/Deprenyl (Eldepryl) 

Definition
-used in the treatment of Parkinson's disease

-inhibit MAO-B and consequently the degradation of dopamine by the enzyme in the CNS (MAO-B only present in CNS)*

*at high doses, inhibits MAO in non-specific manner

-used as a supplement for L-dopa; especially useful in the later stages because it can decrease the severity of the "on-off phenomenon"

-some reports that Selegiline may SLOW PROGRESSION of disease by inhibiting the conversion of MPTP to MPP and other toxic metabolites; however, not yet proven!
Term

 

Entacapone (Comtan)

 

Tolcopone (Tasmar) 

Definition
-used in the treatment of Parkinson's disease

-inhibit the metabolism of L-dopa and dopamine by COMT

-approved for used with L-dopa + carbidopa

-side effects due to increased levels of dopamine + other catecholamines (hallucinations, nausea, hypertension)
Term

 

 

Stalevo

Definition
-used in the treatment of Parkinson's disease

-combination product of: L-dopa, carbidopa, entacapone
Term

 

Benztropine (Cogentin) 

 

Trihexyphenidyl (Artane) 

Definition
-used in the treatment of Parkinson's disease

-anticholinergic drugs that reverse the imbalance between ACh + DA that occurs in Parkinson's --> blocks muscarinic receptors AND inhibits synaptic uptake of dopamine

-used for mild Parkinson's; better at treating tremor than rigidity

-drug of choice for treating iatrogenic Parkinson's from DA antagonists
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