| 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 
 | Definition 
 
        | - atropine, homoscyamine, homoatropine 
 - scopolamine, methoscopolamine
 
 -dicyclomine
 
 -propantheline
 
 -glycopyrrolate
 
 -ipratropium
 
 -tiatropium
 
 -benzotropine
 
 -trihexyphenidyl
 
 -tolteridine
 
 -oxybutynin
 
 -solifenacin
 
 -tropicamide
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | - muscarinic agonist 
 -NEVER administered via IV b/c rapidly degraded by plasma "pseudocholinesterase"
 
 -used to tx. glaucoma
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | - muscarinic agonist; ACh analog 
 -resistant to hydrolysis by cholinesterases
 
 -stimulates nicotinic + muscarinic receptors
 
 -used to tx. glaucoma
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | -muscarinic agonist; ACh analog 
 -stimulates only muscarinic, not nicotinic, receptors
 
 -used for pulmonary function testing in asthmatics
 |  | 
        |  | 
        
        | Term 
 | 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 
 | Definition 
 
        | -irreversible/slowly reversible acetylcholinesterase inhibitor 
 - used in tx. of glaucoma
 |  | 
        |  | 
        
        | Term 
 | 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 
 | Definition 
 
        | -reversible acetylcholinesterase inhibitor 
 -used in the treatment of Alzheimer's, along with Rivastigmine
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | -reversible acetylcholinesterase inhibitor 
 -used to tx. atropine/muscarinic antagonist poisoning
 
 -nonquaternary - CAN ENTER CNS
 |  | 
        |  | 
        
        | Term 
 | 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 
 | 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 
 | Definition 
 
        | -irreversible acetylcholinesterase inhibitor 
 -tx. poisoning with (1) atropine, (2) pralidoxime
 |  | 
        |  | 
        
        | Term 
 | 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 
 | 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 
 | Definition 
 
        | -muscarinic antagonist 
 -synthetic analog of atropine
 
 -does not enter CNS
 |  | 
        |  | 
        
        | Term 
 | 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 
 | Definition 
 
        | - muscarinic antagonist 
 -quaternary analog of scopolamine that does not enter CNS
 |  | 
        |  | 
        
        | Term 
 | 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 
 | 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 
 | Definition 
 
        | -muscarinic antagonist 
 -used to treat urinary incontinence
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | -muscarinic antagonist 
 -used to tx. urinary incontinence
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | -muscarinic antagonist 
 -used to treat urinary incontinence
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | -muscarinic antagonist 
 -used to pupillary dilation for ophtho exam
 |  | 
        |  | 
        
        | Term 
 | 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 
 | Definition 
 | 
        |  | 
        
        | Term 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | Definition 
 
        | - prazosin -terazosin
 -doxazosin
 -tamsulosin
 -alfuzosin
 -silodosin
 |  | 
        |  | 
        
        | Term 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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 
 | 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"
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        | Term 
 | 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
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        |  | 
        
        | 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!
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        |  | 
        
        | 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)
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        |  | 
        
        | Term 
 | Definition 
 
        | -used in the treatment of Parkinson's disease 
 -combination product of: L-dopa, carbidopa, entacapone
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        |  | 
        
        | 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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