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Week 4-ANS
Week 4 cards
235
Pharmacology
Graduate
02/21/2013

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Term
Carbidopa MOA
Definition
Inhibits metabolism of levodopa, reducing the needed dosage of l-dopa, and prevents l-dopa toxicity
Term
Carbidopa clinical indications
Definition
Used in combination with levodopa for the treatment of Parkinson's
Term
Cocaine medication class
Definition
Ester local anesthetic
Term
Clinical use of cocaine
Definition
topically applied local anesthetic and vasoconstrictor for ENT procedures
Term
Phenylephrine
Definition
Alpha 1 agonist (a direct-acting sympathomimetic). Has longer duration of activity than catecholamines
Term
Phenylephrine MOA
Definition
Alpha 1 receptor stimulant with little effect on beta-receptors in the heart. Works on vascular smooth muscle to increase peripheral vascular resistance due to vasoconstriction and elevates blood pressure. Marked reflex bradycardia
occurs
Term
Phenylephrine Clinical Indications
Definition
Effective mydriatic (dilates pupils) and decongestant; also used to raise blood pressure. Approved for used in paroxysmal SVT
Term
Bethanechol MOA
Definition
Muscarinic agonist. It has increased activity at muscarinic sites, because it is a direct agonist
Term
Bethanechol Effects
Definition
Activates M1-M3 receptors in all peripheral tissues. It causes increased secretion, smooth muscle contraction (except vascular smooth muscle relaxes), and changes in heart rate
Term
Bethanechol Clinical Application
Definition
Postoperative and neurogenic ileus and urinary retention. It causes contraction of the detrusor muscle and relaxation of the trigone and sphincter to promote voiding
Term
Bethanechol ADR
Definition
Increased cholinergic activity, increase gastric acid secretion, increased GI & GU muscle tone(therapeutic effect), bronchoconstriction, hypotenstion, bradycardia, increased tearing of the eye
Term
Atropine is the prototype for which drug class?
Definition
Muscarinic antagonists
Term
How many amines does atropine have?
Definition
3 (tertiary amine)
Term
Atropine MOA
Definition
Atropine causes reversible blockade of cholinomimetic actions at muscarinic receptors. Atropine is highly selective for muscarinic receptors.
Term
Atropine System Effects
Definition
Cardio- Increased heart rate d/t blockade of vagal slowing. Eye- Pupil dilation. Respiratory- Bronchodilation and reduced secretions. GI-Reduced motility. GU- Reduces bladder spasms. Suppresses sweating.
Term
Atropine Adverse Effects in Children
Definition
Children and especially infants are very sensitive to the hyperthermic effects of atropine. Deaths have occurs with as small of a dose as 2mg.
Term
Atropine ADR
Definition
Treatment with atropine for one organ system almost always produces undesirable effects in other organ systems. ADR dry mouth, mydriasis, tachycardia, hot and flushed skin, agitation, and delirium are common ADR. “Dry as a bone, blind as a bat, red as a beet, mad as a hatter”
Term
Levodopa MOA
Definition
Antiparkinsonian: Transported into the CNS and converted to dopamine; also converted to dopamine in the periphery
Term
Levodopa Pharmacokinetics
Definition
Rapidly absorbed from the small intestine (depends on gastric emptying and pH); delayed by food ingestion. Only 1-3% of drug enters the brain unaltered so given in large amounts if used alone
Term
Clinical Uses of Levodopa
Definition
Parkinson's Disease: Most efficacious therapy (best restuls seen in first few years of Tx, likely because daily dose must be decreased over time to avoid adverse effects). Does not stop progression of parkinsonism but early use decreases mortality
Term
Carbidopa
Definition
Generally given in combination with levodopa - decreases required dosage of levodopa
Term
Levodopa ADR
Definition
GI upset (monitor patients with peptic ulcers carefully); arrhythmias, postural hypotension, HTN; dyskinesias, on-off and wearing-off phenomena; behavioral disturbances; mydriasis. Use with care in patients with skin cancer or lesions
Term
Levodopa Drug Interactions
Definition
1) Vitamin B6 may prevent its therapeutic effect; 2) MAO-I may lead to hypertensive crisis
Term
Levodopa Contraindictaions
Definition
1) Psychoses 2) Angle-closure glaucoma
Term
Epinephrine MOA
Definition
Non-selective agonist of all adrenergic receptors. Agonist at both the alpha and beta receptors.
Term
Epinephrine MOA
Definition
Potent vasoconstrictor and cardiac stimulant. Positive inotropic and chronotropic actions on the heart cause a rise in systolic blood pressure.
Term
Epinephrine classification
Definition
Catecholamines and component of flight-or-flight response within the
sympathetic nervous system
Term
Epinephrine Most Common Uses
Definition
Cardiac arrest, anaphylaxis, asthma attacks
Term
Epinephrine ADR
Definition
Palpitations, Tachycardia, Arrhythmias, Anxiety, HA, Tremors, HTN, Acute Pulmonary Edema. Can lead to loss of intravascular fluid volume and hypotension during anaphylactic reactions
Term
Epinephrine Contraindications
Definition
Use within administration of MAOI, Non anaphylactic shock, requires additional cardiac monitoring
Term
Norepinephrine MOA
Definition
is a sympathomimetic amine that has both alpha-adrenergic activity resulting in peripheral vasoconstriction, and beta-adrenergic activity leading to inotropic stimulation of the heart and coronary artery vasodilation
Term
Major neurotransmitters
Definition
Acetylcholine, norepinephrine, dopamine, epinephrine, others
Term
Norepinephrine ADR
Definition
Cardiac arrest, cardiac dysrythmia, HTN, bradyarrhythmia, urinary retention
Term
Acetylchone (ACh) is released by which part of the ANS?
Definition
Cholinergic
Term
Norepinephrine Contraindications
Definition
hypotension related to blood volume deficiency
Term
Where is acetylcholine (ACh) produced?
Definition
In the cytoplasm of the cell
Term
2 components of acetylcholine (ACh) and where they originate
Definition
1) Acetyl-CoA is produced in the mitochondria of the nerve ending, 2) choline is transported into the cell from extracellular fluid via a sodium-dependent transporter
Term
Norepinephrine Classification
Definition
Adrenergic, Sympathomimetic, Vasopressor
Term
Norepinephrine kinetics
Definition
Intravenous = 1-2 minutes
Term
Acetylcholinesterase (AChE)
Definition
Enzyme that usually terminates the action of Acetylcholine (ACh) by splitting it into Acetyl-CoA and choline
Term
Acetylcholine (ACh)
Definition
Neurotransmitter released by cholinergic fibers
Term
Norepinephrine Interactions
Definition
Amitriptyline, Chlorpromazine, Digoxin, Doxepin, Linezolid, Trimipramine
Term
Acetylcholine (ACh) probable roles
Definition
1) The primary transmitter at ANS ganglia, at the somatic neuromuscular junction, and at parasympathetic postganglionic nerve ending. 2) A primary excitatory transmitter to smooth muscles & secretory cells in the ENS (enteric nervous system). 3) Probably also the major neuron-to-neuron (ganglionic) transmitter in the ENS
Term
Acetylcholine (ACh)- a choline ester- kinetics
Definition
Insoluble in lipids- poorly absorbed & poorly distributed into CNS because hydrophilic- rapidly hydrolyzed in GI tract by cholinesterase- must by IV in large amounts- IV bolus has brief effect (5-20 seconds)- IM & SQ have only local effects
Term
Acetylcholine (ACh) MOA
Definition
modifies organ function via 2 mechanisms: 1) Direct- ACh released from parasympathetic nerves activates muscarinic receptors on receptor cells, 2) Indirect- Ach interacts with muscarinic receptors on nerve terminals to inhibit release of their neurotranmitter to modulate effects of parasympathetic & sympathetic nervous systems
Term
Dicyclomine MOA
Definition
Tertiary antimuscarinic drug, intestinal antispasmodic/anticholinergic: Inhibits muscarinic cholinergic receptors in the enteric plexus & on smooth muscle (antagonist at M1)
Term
Dicyclomine ADR and clinical cautions
Definition
At low doses, minimal autonomic effects. At high doses, anticholinergic effects include dry mouth, visual disturbances, urinary retention, constipation, dry eyes, nausea. Contraindicated in glaucoma, use caution in males with prostatic hyperplasia, contraindicated in pregnancy, breastfeeding, < 6 mo old, GI obstruction, MG, obstructive uropathy, reflux esophagitis, severe ulcerative colitis, unstable CV status w/ acute hemorrhage
Term
Dicyclomine clinical uses
Definition
Peptic disease, hypermotility, IBS
Term
Pramipexole MOA
Definition
a nonergot dopamine agonist, exact mechanism of action is unknown
Term
Dicyclomine kinetics
Definition
Well absorbed from gut & conjuctiva, widely distributed, significant levels in CNS within 30 minutes to 1 hour; Bioavailability twice as high with IM over PO, Do not administer IV since may cause thrombosis; Eliminated mostly renally- caution in elderly, T1/2=1.8h
Term
Pramipexole MOA
Definition
its action is believed to be related to its ability to stimulate dopamine receptors in the striatum.
Term
Pramipexole MOA
Definition
Has intrinsic activity at the D(2) subfamily of dopamine receptors, and a higher affinity to the D(3) receptors than the D(2) or D(4) receptors
Term
Pramipexole Uses
Definition
Parkinson's Disease & Restless Leg Syndrome
Term
Pramipexole ADR
Definition
Heart Failure, Sleep attack, Malignant Melanoma, Orthostatic hypotension, EPS movements, hallucinations
Term
Pramipexole Precautions
Definition
increased half-life for elderly patients (12 hours)
Term
Albuterol Beta agonist
Definition
A Sympathomimetic, non-catecholamine
Term
Albuterol Beta agonist MOA:
Definition
MOA: Causes bronchodilation in lungs through Beta-2 receptor stimulation. Also stimulates Beta receptors in heart to increase contractional force and heart rate.
Term
Albuterol Beta agonist ADR:
Definition
Tachycardia, A-Fib, SVT, angina, palpitations, tremors, dizziness
Term
Midodrine Alpha-one-receptor agonist
A prodrug
Definition
A direct-acting, Sympathomimetic
Term
Midodrine Alpha-one-receptor agonist
A prodrug MOA:
Definition
Enzymatically hydrolized to desglymidodrine , a selective alpha-one-receptor agonist to increase blood pressure for those with orthostatic hypotension. Works on the arteriolar and venous alpha-one-receptors.
Term
Midodrine Alpha-one-receptor agonist
A prodrug ADR:
Definition
Can cause hypertension in supine. May cause bradycardia due to vagal stimulation.
Term
Acetylcholine (ACh) Clinical indications
Definition
Miosis induction, eye surgery
Term
Acetylcholine MOA
Definition
naturally occurring neurohormone, interferes w/ transmission of nerve impluses at all cholinergic sites involving somatic & autonomic nerves, causes pupil constriction when directly applied to iris
Term
Dobutamine MOA-
Definition
A combination of two synthetic isomers which offset each other- the outcome is a primarily β-receptor agonist in cardiac muscle; causes increased cardiac contractility (+ inotrope) through β1 stimulation and a second effect of vasodilation through slight β2 stimulation
Term
Dobutamine: ADR’s
Definition
Increased myocardial oxygen demand leading to angina or arrhythmias in patients with coronary artery disease. Other signif. ADR’s include hypokalemia and platelet inhibition.
Term
Dobutamine: Indications
Definition
Acute heart failure, cardiogenic shock
Term
Benztropine MOA
Definition
Antagonist of muscarinic receptors in basal ganglia (anticholinergic)
Term
Benztropine- Indications
Definition
Anticholinergics antagonize the effect of acetylcholine. This decreases the imbalance between the neurotransmitters acetylcholine and dopamine, which may improve the symptoms of early Parkinson's disease.
Term
Benztropine ADR’s
Definition
Fever, hyperthermia, heat stroke, tachy/bradyarrhythmias, constipation, muscle weakness, tardive dyskinesia, confusion and depression
Term
Benztropine: Special considerations
Definition
On Beer’s Criteria list as not recommended in older adults for prevention of antipsychotic induced extra-pyramidal symptoms. It is also not recommended for the treatment of Parkinson's disease in older adults as more effective agents are available. Avoid use in patients with dementia and cognitive impairment due to the risk of adverse CNS effects.
Term
Pilocarpine MOA
Definition
Muscarinic partial agonist, activates M1-M3 receptors in tissues - results in increased secretion and smooth muscle contraction, except vascular smooth muscle relaxes
Term
Pilocarpine Clinical Use
Definition
Glaucoma; Sjogren's syndrome
Term
Pilocarpine Pharmacokinetics
Definition
Oral lozenge and topical application
Term
Pilocarpine Toxicity
Definition
Excessive parasympathomimetic effects
Term
Rasagiline MOA
Definition
Inhibits monoamine oxidase (MAO) B
Term
Rasagiline Clinical Use
Definition
Used in addition to levodopa to help prolong its effects to help reduce Parkinson's symptoms
Term
Rasagiline Administration and Toxicity
Definition
Given orally, may cause serotonin syndrome when used with meperidine or SSRIs
Term
Donepezil Clinical use
Definition
Used in the treatment of cognitive dysfunction in Alzheimer's patients
Term
Donepezil MOA
Definition
It reversibly and noncompetitively inhibits centrally-active acetylcholinesterase, the enzyme responsible for hydrolysis of acetylcholine which results in increased concentrations of acetylcholine that are available for synaptic transmission
Term
Donepezil dosage
Definition
May be given once daily because of its long half-life. Comes in 5, 10, & 23 mg tablets
Term
Donepezil Pharmocokinetics
Definition
Peak: 3-4 hours, Half-life: 70 hours and 104 hours in subject >55 years old. Metabolized in the liver and >50% is excreted in urine.
Term
Donepezil Considerations
Definition
This drug is a newer drug and is more selective acetylcholinesterase inhibitors and lacks the hepatotoxic effects as older versions
Term
Entacapone Use
Definition
This drug is an Antiparkinsonian Catechol-O-Methyltransferase Inhibitor, which prolong the action of levodopa by diminishing its peripheral metabolism
Term
Entacapone MOA
Definition
This drug is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT), an enzyme with highest activity in the liver, intestinal tract, and kidney, is responsible for catalyzing O-methylation of levodopa to 3-O-methyldopa
Term
Entacapone Pharmocokinetics
Definition
Half-life is approximately 2 hours and needs to be taken (200mg) with each dose of levodopa, up to 5 times daily. This medication is preferred as it isn't hepatotoxic
Term
Entacapone adverse effects
Definition
Relate to increased levodopa exposure and include dyskinesias, nausea, confusion, abdominal pain, orthostatic hypotension, sleep disturbances and an orange discoloration of the urine.
Term
Entacapone considerations
Definition
It is often necessary to lower the daily dose of levodopa by about 30% in the first 48 hours to avoid or reverse some complications
Term
Dicyclomine (MOA)
Definition
Inhibits acetylcholine's muscarinic actions at postganglionic parasympathetic receptors in smooth muscles, secretory glands, and the CNS. Decreases GI motility.
Term
Dicyclomine (Clinical Uses)
Definition
Irritable Bowel Syndrome, other functional GI disorders
Term
Dicyclomine (Side Effects)
Definition
Headache, palpitations, dizziness, blurred vision, constipation, urinary retention
Term
Acetylcholine (MOA)
Definition
interferes with transmission of nerve impulses at all cholinergic sites involving somatic and autonomic nerves. Aceteylcholine released from parasymphathic nerve: 1. Activates Muscarini receptors on effector cells to directly alter organ function 2. interacts with muscarinic receptors on nerve terminals to inhibit the release of neurotransmiters
Term
Acetylcholine (Clinical Uses)
Definition
pupil constriction in eye surgeries, glaucoma treatment
Term
Acetylcholine (Pharmacokinetics)
Definition
Rapidly hydrolyzed (high dose/concentration of IV must be infused to achieve desired effects), poorly absorbed and distributed into CNS,
Term
Acetylcholine (Side Effects)
Definition
cataract, corneal decompensation and edema, optic atrophy
Term
Dobutamine (MOA)
Definition
Stimulates beta1 adrenergic receptors causing increased contraction of heart
Term
Dobutamine (Clinical Use)
Definition
Short term management of cardiac decompensation.
Term
Dobutamine (Side Effects)
Definition
Increased HR, BP, PVC's, chest pain, palpitations
Term
Benztropine (MOA)
Definition
Anticholinergic and antihistaminic drug. Inhibits reuptake of dopamine therby prolonging actions of dopamine
Term
Benztropine (Clinical Use)
Definition
Adjuctive treatment for Parkinsons
Term
Benztropine (Side Effects)
Definition
Tachycardia, confusion, hyperthermia
Term
Acetylcholinesterase
(AChE)
Definition
Enzyme that hydolizes acetylcholine into choline & acetic acid
Term
Donepezil (Aricept)
(MOA)
Definition
REVERSIBLE Acetylcholinesterase (AChE) Inhibitor (aka-partial Acetylcholine agonist)
Blocks AChE from breaking down Acetylcholine
-Crosses BBB
-Metabolized in Liver
-Excreted mostly in Kidney
-Can be given daily
-100% biovailability (administer drug PO)
Term
Donepezil (Aricept)
(Clinical Use)
Definition
Used to treat Alzheimers Disease
Term
Donepezil (Aricept)
(Side Effects)
Definition
S/E: dizziness, lacrimation, incr. salivation, incr. secretions iin GI/resp tract, bronchospasm, bradycardia, abd cramping
Term
Acetylcholinesterase
(AChE) Inhibitors
Definition
Two Types:
1. Irreversible- bind to enzyme (AChE) & render it inactive permanently (ie: insecticides)
2. Reversible- bind to enzyme (AChE) for short time then diffuse away (ie: Donepezil-"Aricept")
Term
Cholinergic Agonist
S/EAcronym:
"DUMBBELLS"
Definition
D- diarrhea
U-urination
M-miosis (pupil constriction)
B-bradycardia
B-brochoconstriction
E-emesis
L-lacrimation (tearing of eyes)
L-lethargy
S-salivation
Term
Catechol-O-Methyltransferase
(COMT)
Definition
COMT= enzyme that metabolizes levodopa
Term
Enacapone
(MOA)
Definition
Catechol-O-Methyltransferase (COMT) Inhibitor:
Drug blocks COMT so peripheral metabolism of levodopa is decreased
(This drug effects peripheral tissue only- not brain)

More levodopa is avail. to cross BBB

**should be given in combination with Levodopa & a dopadecarboxylase inhibitor (ie: Carbodopa)
Term
Enacapone
(Clinical Uses)
Definition
Used in combination with Levodopa and Carbidopa (dopa decarboylase inhibitor) to treat Parkinson's Disease
Term
Enacapone
(Side Effects)
Definition
Drug increases Levodopa exposure & can lead to -dyskinesias, nausea & confusion
*Decrease daily dose of Levodopa by 30% in 1st 48 hrs of using Enacapone to avoid above S/E

Other S/E:
-diarrhea
-abd pain
-ortho hypotension
-sleep disturbances
-orange colored urine
Term
Midodrine MOA
Definition
Selective alpha 1 agonist
Activates phospholipase C - causing increased intracellular Ca+ and vasoconstriction
Term
Midodrine Uses
Definition
Orthostatic hypotension
Causes contraction vascular smooth muscle = Increase BP
Term
Midodrine (side effects)
Definition
HTN when in supine
Goose bumps (piloerection)
urinary retention
Term
Albuterol MOA
Definition
Selective Beta 2 agonist
Term
Albuterol uses
Definition
Bronchodilation
Used: Asthma, CODP, or acute bronchospasms
Available in Aerosol inhaler, nebs, and PO tab/syrup
Term
Albuterol S/E
Definition
Tremors
Tachycardia
Overdose: Arrhythmias
Term
pilocarpine (MOA)
Definition
a parasympathomimetic agent that works directly on muscarinic alkaloids or sythentics to increase secreations, increased smooth muscle contraction and changes in heart rate.
It is used primarily for glaucoma (eye drops/topical), in which the medications causes pupli constriction, ciliary muscle contraction and a decrease in the intraocular pressure.
It can also be used to treat Sjorns syndrome (oral) by increasing secretions of the exocrine glands.
Term
pilocarpine (ADR)
Definition
hypertension, hypotension, decrease heart rate and potiental for cardiac arrhythmias
Term
Rasagiline (MOA)
Definition
Blocks monoamine oxidase B. Monamine oxidase B selectively metabolizes dopamine, therefore the medication will selectively block metabolism of dopamine.
It is used for treating early onset Parkinson's disease and used in conjunction with carbidopa/levodopa pharmacotherapy to prolong the effect of the carbidopa/levodopa in those with advanced Parkinson's disease.
Term
Bethanechol (MOA)
Definition
A direct cholinergic agonist which stimulates the release of acetylcholine, activating the parasympathetic nervous system. It is muscarinic specific.
Term
Bethanechol (Clinical Use)
Definition
Causes contraction of the detrusor muscle and relaxation of the trigone and sphincter to promote voiding. It is used post-op to promote voiding. Also used for post-op and neurogenic ileus.
Term
Bethanechol (ADR)
Definition
Increased cholinergic activity causing: Increased gastric acid secretion, increased GI and GU muscle tone, abdominal cramps, diarrhea, increased tearing of the eye, bronchoconstriction, hypotension, bradycardia.
Term
Atropine (MOA)
Definition
An anticholinergic, muscarinic antagonist, that blocks the effect of parasympathetic autonomic discharge. It is a tertiary amine alkaloid esters of tropic acid. It increases firing of the SA node and increases conduction through the AV node. Opposes the action of the vagus nerve, blocks acetylcholine receptor sites and decreases bronchial secretions.
Term
Atropine
Definition
Prototype of the muscarinic receptor-blocking drugs
Term
Atropine (Clinical uses)
Definition
It is used to transiently increase heart rate without a change in blood pressure or cardiac output. Used for parasympathomimetic drug poisoning.
Term
Atropine (ADR)
Definition
Mydriasis , cycloplegia, tachycardia, agitation. Remarkably safe in adults. Children, especially infants are very sensitive to the hyperthermic effects. Highly dangerous when overdose occurs in infants or children.
Term
Cocaine (MOA)
Definition
#NAME?
Term
Cocaine Clinical Indices
Definition
#NAME?
Term
Cocaine Adverse effects
Definition
#NAME?
Term
Carbidopa (MOA)
Definition
#NAME?
Term
Carbidopa Clinical Use
Definition
#NAME?
Term
Levodopa MOA
Definition
Dopamine agonist: Once administered, Levodopa is decarboxylated into dopamine. Dopamine does not cross the BBB but Levodopa, the metabolic precursur of dopamine, does
Term
Levodopa administration considerations
Definition
Absorbed rapidly from the small intestine, depends on rate of gastric emptying and pH of gastric contents. Administered with food delays Levodopa getting into the plasma. Has much higher plasma levels when given with a dopa decarboxylase inhibitior (carbidopa)
Term
Levodopa ADR
Definition
GI: anorexia, N/V when not given with decarboxylase inhibitor. Cardiovascular: Arrythmias, tachycardia, postural hypotension. Behavior: depression, anxiety, agitation, changes in personality (more common in people taking Levodopa/decarboxylase inhibitor). Dyskinesias: Occur in 80% of patients taking Levodopa for more than 10 years
Term
Levodopa on/off phenomenon
Definition
Fluctuations in clinical response that are unrelated to the timing of the dose. Off periods of marked akinesia alternate with on periods of improved mobility but often more dyskinesia
Term
Levodopa-avoid administration
Definition
Patients taking MOAI's or within 2 weeks of discontinuing them due to potential for hypertensive crisis
Term
Levodopa contraindications/precautions
Definition
Psychotic patients: may exacerbate mental disturbances. Administer carefully and with monitoring in patients with open angle glaucoma, active peptic ulcer, patietns with history of melanoma
Term
Phenylphrine class
Definition
Sympathomimetic, relatively pure alpha agonist
Term
Phenylphrine indications
Definition
Short term management of acute hypotension (IV) and intranasally as a decongestant to produce local vasoconstriction, also used as a mydriatic agent (dilate pupils) when examining the retina
Term
Epinephrine (EPI) / Norepinephrine (NE)
Definition
Sympathomimetic & Endogenous Catecholamines; Agonists at α1, α2, & β1; EPI also acts on β2; ↑BP, ↑ vasoconstriction, ↑ blood flow, ↑ contractility
Term
Pramipexole
Definition
Dopamine (D3) agonsit; treats mild parkinsonism or acts as adjunct to levodopa
Term
Midodrine MOA
Definition
Desglymidodrine (a metabolite of medodrine) is a selective alpha1 receptor agonist. It activates phospholipase C and causes an increase in intracellular calcium vasoconstriction.
Term
Midodrine Brand Names
Definition
Amatine, ProAmatine, Gutron
Term
Midodrine Clinical Use
Definition
Treatment of orthostatic hypotension that is caused from impaired autonomic nervous system function
Term
Midodrine Adverse Effects
Definition
Hypertension (especially while in supine position) and bradycardia
Term
Midodrine Pharmacokinetics
Definition
Renal excretion
Term
Albuterol MOA
Definition
Beta 2 selective adrenoceptor agonist. It activates adenylyl cyclase.
Term
Albuterol Clinical Use
Definition
Bronchodilation. Symptomatic treatment of asthma and COPD
Term
Albuterol Edverse Effects
Definition
Tremors, Tachycardia, arrythmias
Term
Oxybutynin
Definition
Anticholinergic, Antispasmodic - Inhibits the muscarinic of acetylcholine on smooth muscle that relaxes the bladder smooth muscle thus maximizing urinary capacity & volume decreasing urgency, frequency, & incontinence
Term
Oxybutynin adverse effects
Definition
diarrhea, UTI, constipation, pruritis, angioedema,
Term
Oxybutynin Pharmacokinetics -
Definition
Metabolized - Liver (bypasses 1st pass-effect), Excreted - Kidneys
Term
Clonidine
Definition
(Catapres) - (Antihypertensive) - Stimulates alpha 2adrenergic receptors in the brain reducing sympathetic CNS outflow, decreased peripheral resistance, renal vascular resistance, heart rate, & blood pressure
Term
Clonidine Pharmacokinetics
Definition
Distribution - 20-40% protein binding, Metabolism - Liver, Excreted -Renal, not dialyzable,
Term
Clonidine Adverse Effects
Definition
Headache, dizziness,somnolence, erythema, pruritis, fatigue, xerostoma
Term
Levodopa
Definition
Immediate metabolic precursor of dopamine, enters the brain, where it is decarboxylated to dopamine
Term
Levodopa adverse effects
Definition
immediate- N/V in 80% of patients, hypotension. Long-term-dyskinesia, motor fluctuation, psychiatric SE (vivid dreams, depression, anxiety, agitation, confusion, psychosis), insomnia
Term
Levodopa pharmacokinetics
Definition
rapidly absorbed by the small intestine, but its absorption depends on the rate of gastric emptying and the pH of the gastric contents. Only 1-3% of administered levadopa enters brain unaltered, the remainder is metabolized to dopamine which does not cross the BBB, so it must be given in large doses when given alone.
Term
Levodopa clinical use
Definition
Does not stop progression of parkinsonism, its early initiation lowers the mortality rate. It is particularily effective in relieving bradykinesia and any disabilities resulting from it. Generally given in combination with with carbidopa.
Term
Phenylephrine
Definition
alpha 1 receptor agonist, it constricts blood vessels by stimulating alpha-adrenergic receptors. Not a catechol derivative, it is not inactivated by COMT and has a longer duration of action than the catecholamines. Increase peripheral vascular resistance and blood pressure. It is an effective mydriatic and decongestant and can be used to raise the blood pressure. ADR- arrhythmias, CNS effects (anxiety, HA, insomnia).
Term
Bethanechol
Definition
Affects the parasympathetic nervous system. Muscarinic agonist.
Term
Bethanechol Pharmacokinetics
Definition
Insoluble in lipids
Term
Bethanechol MOA
Definition
Has muscarinic action but no nicotinic action. Both directly and indirectly affects organ function: acetylcholine released from parasympathetic nerves activates the muscarinic receptor on the effector cells to alter organ functions directly; interacts with muscarinic receptors on nerve terminals to inhibit release of neurotransmitters which changes the effects of the parasympathetic nervous system and alters organ function.
Term
Bethanechol effects
Definition
Activates M1-M3
Term
Bethanechol Uses
Definition
Postoperative and neurogenic ileus, urinary retention
Term
Bethanechol Toxicity
Definition
Excessive parasympathomimetic effects, especially bronchospasm in asthmatics
Term
Bethanechol Interactions
Definition
Additive with other parasympathomimetics
Term
Atropine
Definition
Affects the parasympathetic nervous system. Muscarinic agonist.
Term
Atropine Pharmacokinetics
Definition
Well absorbed in gut and conjunctival membranes
Term
Atropine MOA
Definition
Competative antagonism (reversible blockade) of cholinomimetic actions at muscarinic receptors - effectiveness depends on tissue (most sensative: salivary, bronchial, and sweat glands) and source of agonist (exogenously administered cholinoceptor agonists better than endogenously released acetylcholine)
Term
Atropine Effects
Definition
CNS: minimal effects, slower, longer-lasting sedative effect on brain, decreases tremor in Parkinson's
Term
Atropine Uses
Definition
Retinal examination, prevention of synechiae after surgery
Term
Atropine Toxicity
Definition
Increase intraocular pressure in closed-angle glaucoma
Term
Benztropine MOA
Definition
Antagonist at M receptors in the basal ganglia
Term
Benztropine Uses
Definition
reduces tremor and rigidity in those with Parkinson's Disease but have little effect on bradykinesia
Term
Benztopine Effects
Definition
Widely distributed in the body, usually within 30 minutes to one hour. Taken orally. Helps decrease the relatively access of acetylcholine in the body that occurs there is a deficiency of dopaminergic activity in the basal ganglia-striatum system. Daily dose is 1-6mg.
Term
Benztropine ADR
Definition
sedation, mydriasis, urinary retention, constipation, confusion, dry mouth
Term
Dobutamine MOA
Definition
initially considered a relatively beta one selective agonist, but more complex than that. Actions are mostly activation of alpha and beta receptors.
Term
Dobutamine Effects
Definition
Activates adenylyl cyclase, increasing myocardical contractility. Has a positive inotropic effect
Term
Dobutamine Uses
Definition
Used in cardiac shock, acute heart failure, results in increased cardiac output with less reflex tachycardia, requires dose titration to desired effect
Term
Dobutamine ADR
Definition
increased blood pressure and allergic reactions
Term
Pramipexole has preferential affinity for what recptors
Definition
D3 family
Term
Pramipexole effects
Definition
A dopamine recepter agonist used in monotherapy for mild and advanced parkinsonism, allowing the dose of levodopa to be reduced and smooths out response fluctuations
Term
NE
Definition
Norepinephrine
Term
Norepinephrine
Definition
Primary neuro transmitter at most sympathetic post ganlionic nerve endings
Term
EPI
Definition
Epinephrine (adrenaline)
Term
Epinephrine
Definition
Agonist at both Alpha and Beta receptors
Term
Entacapone MOA
Definition
Selective inhibitor of catechol-O-methyltransferase (COMT) used in the treatment of Parkinsons disease. Typically given with levodopa because it reduces metabolism of levodopa and prolongs its action.
Term
Entacapone Pharmacologic Effects
Definition
Rapidly absorbed, bound to plasma proteins, and metabolized before excretion
Term
Entacapone Adverse Reactions
Definition
Dyskinesias, nausea, confusion, diarrhea, abdominal pain, orthostatic hypotension, sleep disturbances, and orange discoloration of the urine.
Term
Donepezil MOA
Definition
Cholinesterase inhibitor. Inhibits the enzyme acetylcholinesterase which breaks down acetylcholine. Used in the treatment for Alzheimer's disease.
Term
Donepezil Adverse Reactions
Definition
Cause significant adverse effects, including nausea and vomiting, and other peripheral cholinomimetic effects. Use in caution in patients receiving other drugs that inhibit cytochrome P450 enzymes.
Term
acetylcholine (ACh)
Definition
primary excitatory nuerotransmitter released by cholinergic fibers in the autonomic nervous system (ANS) There are two main cholinergic receptors muscarinic and nicotinic
Term
Dicyclomine
Definition
drug with anticholinergic action used for GI disorders such as IBS and minor diarrhea- reduces smooth muscle and secretory activity of the gut
Term
Dicyclomine MOA
Definition
competative antagonism at M3 receptors
Term
Dicyclomine Pharmacokinetics
Definition
short 1/2 life, but action lasts up to 6 hours
Term
Dicyclomine toxicitiy
Definition
tachycardia, confusion, urinary retention, increased intraoccular pressure
Term
Pilocarpine MOA
Definition
Parasympathomimetic; acts as a partial agonist for activation of muscarinic receptors.
Term
Pilocarpine ADR
Definition
Excessive parasympathomimetic effects such as bronchospasm, bradycardia, excessive sweating
Term
Pilocarpine Clinical Uses
Definition
Glaucoma; Sjogren’s syndrome
Term
Rasagiline MOA
Definition
Selectively inhibits MAO-B; also inhibits MAO-A at higher doses. Increases dopamine stores in neurons.
Term
Rasagiline ADR
Definition
May causes serotonin syndrome with meperidine, SSRIs, and tricyclic antidepressants. Avoid all OTC cold preparations.
Term
Rasagiline Clinical Uses
Definition
Parkinson’s disease, used either alone or as an adjunct to prolong the effects of levodopa-carbidopa
Term
Cocaine
Definition
Primary clinical use is for topical anesthesia for ear, nose, and throat procedures where it also serves as a potent vasoconstrictor to reduce bleeding. Being replaced by newly developed drugs due to concerns for systemic toxicity and the regulation involved with dispensing and handling
Term
Cocain MOA
Definition
MOA = Blocks the uptake of dopamine, noradrenaline, and serotonin, through their respective receptors; inhibits voltage-gated sodium channels, which blocks the conduction of action potentials.
Term
Cocain - Nursing Considerations
Definition
Nursing considerations = Highly addictive; increases arterial pressure, produces tachycardia and often produces ventricular arrhythmias. Causes loss of appetite, hyperactivity, and insomnia. Increases risk of intracranial hemorrhage, ischemic stroke, MI, and/or seizures. Overdose can lead to hyperthermia, coma, and death.
Term
Carbidopa
Definition
A decarboxylase inhibitor; increases the efficacy of levodopa. Doubles the amount of levodopa that gets to the blood, and triples the amount that gets to the brain.
Term
DONEPEZIL
Definition
Acetylcholinesterase inhibitor (prevents acetylcholinesterase from breaking down acetylcholine to choline and acetate, thereby increasing cholinergic tone). ADR: related to increased acetylcholine (dizziness, salivation, lacrimation, excessive secretions, bronchospasm)
Term
Phenylephrine
Definition
Selective alpha 1 agonist.
Term
phenylephrine
Definition
locally for nasal decongestion or systemically (IV) to raise blood pressure. Constricts alpha receptor vessels.
Term
levodopa
Definition
used for parkinsons disease as an oral agent that is rapidly absorbed in GI when taken on empty stomach.
Term
levodopa
Definition
crosses BBB, dopamine does not. Used often as first line defense then used in combination with carbidopa to combat decreased effects after 3-4 years.
Term
levodopa
Definition
ADR- take in divided small doses to prevent anorexia and nausea. Fewer GI effects when combination drug Sinimet (carbidopa/levodopa) is used. Asymptomatic postural hypotension, do not use with MOAI's.
Term
levodopa
Definition
Dyskinesias in 80% of people- twitching movements or face or distal extremities.
Term
levodopa
Definition
Behavioral responses of dellusion, hallucination depression or anxiety with administration of sinimet but decreased when levodopa alone. Do NOT use in psychotic pts or thos with angle-closure glaucoma. Use care with peptic ulcers, hx of melanoma.
Term
Bethanechol
Definition
Within the parasympathetic nervous system, bethanechol stimulates muscarinic receptors as a direct agonist in cholinergic transmission. More specific use , negligible to nicotine receptors.
Term
Bethanechol ADR
Definition
Increased gastric acid secretions, increased GI and GU muscle tone, bronchoconstriction, hypotension, bradycardia, increased tearing of the eye. Often given to promote urination after surgery.
Term
Atropine
Definition
Prototype for antimuscarinics, tertiary amine, causes reversible blockade, antagonist of cholinomimetic actions at muscarinic receptors with parasympathetic system. Used to treat bradycardia and organophosphate poisoning.
Term
Effects of Atropine
Definition
Decreased GI motility, decreased urinary function, decrease in secretions, prevents bronchoconstriction, dilates pupils, confusion, sleepy, and increased heart rate as a reflux from vasodilation. Blocks action of vegus nerve.
Term
Pramipexole
Definition
Dopamine receptor agonist. MOA: Direct agonist at D3 receptors, nonergot. Reduces the symptoms of parkinsonism and smoothes out fluctuations in levodopa response.
Term
Pilocarpine
Definition
Stimulates cholinergic receptors by acting as a direct acting muscarinic (an agononist to the PNS) Has little to no effect at the nicotinic receptors. Activates all 3 "M" receptors causing increased secreation, decreased heart rate, increases GI motility by smooth muscle contraction. Used for glaucoma and Sjogren's syndrome. Can be administered PO or topically. ADR include those associated with increased PNS actions: dizziness, HA, N/V (d/t increased GI motility), urinary frequency, bronchospasm, increased lacrimation, and pupil constriction. Contraindicated in Angle-closure glaucoma. Renal excretion.
Term
Pramipexole
Definition
Adverse Effects: Nausea and vomiting, postural hypotension, dyskinesias, confusion, impulse control disorders and sleepiness
Term
Epinephrine
Definition
Specific sympathomimetic drug. Both alpha and beta receptor agonist. Very potent vasoconstrictor and cardiac stimulant.
Term
Norepinephrine
Definition
Both alpha-1 and alpha-2 receptor agonist. Also activates beta-1 receptors with similar potency as epinephrine. Little effect on beta-2 receptors. Increases peripheral resistance and both diastolic and systolic BP. Baroreflex activation tends to overcome the direct positive chronotropic effects of norepi, but the positive inotropic effects of the heart are maintained.
Term
Epinephrine
Definition
Causes a rise in SBP due to positive inotropic and chronotropic actions on the heart-mainly beta-1 receptors. Also activates beta-2 receptors which can cause dilation in some vessels. This drug functions largely as a hormone, it acts on distant cells.
Term
Rasagiline
Definition
An indirect agonist by acting as an irreversible monoamine oxidase B inhibitor to treat Parkinsonism. This inactivation of MAO leads to increased amounts of dopamine in the CNS. Is used for early symptomatic treatment and as adjunctive therapy to increase the effects of sinemet. ADR include: dizziness, hallucinations, rhinitis, anorexia, N/V, arthralgia, dyskinesia (d/t increased levodopa). Metabolized through the liver, modify in hepatic impairment.
Term
Acetylcholine
Definition
Direct parasympathetic stimulation at muscarinic and nicotinic receptors. Hydophilic molecules- poorly absorbed and distributed in CNS. Hydrolysed in the GI tract.
Term
Acetylcholine organ system effects and ADRs
Definition
Eye: miosis; CV: vasodilation, decreased peripheral vascular resistance; Resp: bronchoconstriction, increased secretions; GI: increased peristalsis, stimulates saliva and gastric glands, relaxes spincters; GU: relaxes sphincters/ muscles, promotes voiding; CNS: alertness- coma, tremors, convulsions. ADRs: nausea/vomiting, urinary urgency, salivation, sweating, vasodilation, bronchconstriction. When targeting one organ system, will have side effects in others.
Term
Dicyclomine
Definition
Anticholinergic drug used for irritable bowel syndrome and diarrhea. Competitive antagonist at M3 receptors. Reduces smooth muscle activity and decreases GI secretions. ADRs: tachycardia, confusion, urinary retention, increased intraocular pressure
Term
MIDODRINE
Definition
Alpha 1 selective agonist. Causes an increase in PVR; increases arteriolar and venous tone which causes a rise in blood pressure. Used to help patients with orthostatic hypotension. Midodrine (Prodrug) is converted to Desglymidodrine (active agent). ADR: Supine HTN, urinary urgency or retention, paresthesias, piloerection, and pruritis.
Term
ALBUTEROL
Definition
Sympathomimetic agent. Beta-2 agonist as well as some Beta-1 activity. Used for bronchodilation. Comes in inhilation and oral form. ADR: Tremor, irritability, insomnia, irregular heartbeat.
Term
Oxybutinin
Definition
Antimuscarinic drug somewhat selective for M3 receptors used in treatment of over active bladder.
Term
Clonidine
Definition
alpha2 selective agonist used to treat hypertension
Term
Cocaine
Definition
Local anesthetic with peripheral sympathomimetic action resulted from transmitter reuptake inhibition at nonadrenergic synapses.At CNS produces short lasting but more intense .amphetamine like psychologycal effect.
Term
Cocaine use
Definition
Restricted to topical anesthesia(ear,nose and throat procedures) to reduce bleeding.Other anesthesics combined with vasoconstrictor are preferred to avoid Cocaine systemic toxicity and handling this controlled substance.
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