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bethanecol (Urecholine)
Cholinergic Agonist
Stimulates bladder contraction, used to stimulate urination post-partum and post-op.
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cholinesterase inhibitors
Increase ACh activity.
Used in nerve gas to cause excessive urination/defecation/vomiting.
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atropine
Anticholinergic
Used pre-op to decrease GI motility/secretions
Increases HR (Tx for bradycardia)
Antidote for poisons (insecticides, mushroom toxins) that do damage by inhibiting acetylcholinesterase
Originally used to dilate pupils but had too long of a half life.
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tropicamide (Mydriacyl)
Anticholinergic
Current eyedrop used to dilate eyes with a shorter half life than atropine.
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ipratropium bromide (Atrovent)
Anticholinergic
Inhaler for emphysema and COPD
15min onset lasts for 3-4 hours
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Combivent
Combination of albuterol + Atrovent
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tiotropium bromide (Spiriva)
Anticholinergic
New dry powder inhaler similar to Atrovent.
15min onset last for 5-6 days
Expensive
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oxybutynin (Ditropan and Ditropan XL)
Anticholinergic
Antispasmodic used to tx nocturia and excessive urination.
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tolterodine (Detrol and Detrol LA)
Anticholinergic
Newer bladder antispasmodic.
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Norepinephrine and epinephrine both have a common _______ structure and are rapidly metabolized by MAO and COMT in the _____.
catecholamine
liver
This is an example of the first pass effect.
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Drugs that have a catecholamine structure cannot be given ____.
Orally
Noncatecholamines can be given orally and pass the BBB more efficiently.
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Epinephrine (OTC Primatene Mist)
Catecholamine so must be IV, inhalation, or topical
Stimulates all the adrenergic receptors (Alpha 1 +2 and Beta 1+2; agonist) to produce full fight or flight response.
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What are the clinical uses of epinephrine?
- Asthma (Beta 2)
- Anaphylactic shock (epi pen)
- Adjunct to cardioversion (CLEAR!!) for cardiac arrest
- Reduces bleeding topically
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Norepinephrine stimulate all adrenergic receptors except ___.
Beta 2
Tx for shock and hypotension
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pseudoephedrine (Sudafed - OTC)
Non-catecholamine nasal decongestant
Causes nasal vasoconstriction
Now behind the counter because it can be converted to meth.
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phenylephrine (Neo-synephrine, Sudafed PE)
Replacement for pseudoephedrine in cold formulas yet has shown to be no more effective than placebo.
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ephedrine
Same as pseudoephedrine
Rarely prescribed, in dietary herbal supplements (herbal ecstasy) but has been pulled due to causing death.
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amphetamine (Benzedrine) and methylamphetamine
Synthetic versions of epinephrine; catecholamine
Originally used as nasal decongestant but pts build a tolerance too quickly
Popular street drug either IV (crystal) or smoked in free base form (ice). Causes meth mouth and formication (hallucinations of bugs crawling on skin)
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MDA (methylenedioxyamphetamine)
Similar to amphetamine, Love Drug
Causes energy rush and increased self awareness while eliminating inhibitions and anxiety.
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MDMA (methylenedioxymethamphetamines)
Ecstasy; noncatecholamine
Similar to MDA with more dramatic stimulation of serotonin receptors. Widely popular street drug.
Can cause tachycardia and hyperthermia
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Quat (Khat)
Arabian shrub that has active adrenergic agonists (Cathinone) that is chewed as a stimulant.
I think it is a catecholamine but am not positive
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Bath Salts
Synthetic derivative of cathinon
Got away with sale saying they weren't for human consumption but a ton of recent poison control calls about overdoses has raised awareness.
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methylphenidate (Ritalin, Concerta)
Used to tx hyperactivity like ADHD
Comes in extended release forms
Inhibits reuptake of dopamine and norepinephrine in brain which helps some but not all ADHD people concentrate.
Widely abused and is Schedule II
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dexmethylphenydate (Focalin)
Pure enantiomeric (right hand glove) form of methylphenidate. Was give a black box warning.
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amphetamine in the sustained release form Adderall XR
Also used to tx ADHD
Control II and causes euphoric high; "study drug"
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modafinil (Provigil)
Officially approved for narcolepsy and obstructive sleep apnea; "cognitive enhancement
Increase epinephrine and norepinephrine release.
Off label use for ADHD
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What 3 things to beta-2 agonists cause?
Bronchodilation
Uterine relaxation
Glycogenolysis
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How are asthma drugs typically administered?
- Metered dose inhaler (MDI)
- Dry powder inhaler (DPI)
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What is the most common asthma medicine?
albuterol
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albuterol (salbuterol, ProAir, Proventil HFA, Ventolin HFA)
Beta 2 agonist
Used to stop asthma attack
5-15min onset lasts for 3-6 hours
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salmeterol (Serevent)
Long acting beta 2 agonist; administered using DPI
45 min onset lasts 12 hours
Prophylactic (preventative) use only, can't use it to stop asthma attack.
Should be added to anti-inflammatory, fluticason.
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