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Name the 4 adrenergic agonists
- 1. epinephrine (OTC primatene mist)
- 2. pseudoephedrine (sudafed OTC)
- 3. phenylephrine (neo-synephrine, sudafed PE)
- 4. ephedrine
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Norepinephrine and epinephrine both have a common ____________ structure
catecholamine (benzene ring with two OH groups)
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Why cant catecholamine structures be taken orally
they disolve to quickly by MAO and COMT in the intestinal wall and liver this is called first pass effect
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Can Noncatecholamines such as ephedrine be taken orally? Why?
YES, because they metabolize slowly, and they cross the BBB
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Epinephrine (OTC primatene Mist)
- cant be bought OTC but can get online
- stimulates all adrenergic receptors
- Full fight or flight respone
- Catecholamine (no oral)
- must be taken nasal, IV, SQ, or topical
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what are the 5 clinical uses for epinephrine?
- 1. asthma-- Beta2 activity (inhalation)
- 2. treatment of anaphylactic shock (EpiPen)
- 3. combined with local anesthetic to minimize absorption of "local" into bloodstream and maximize duration.
- 4. used as an adjunct in cardiac arrest along with cardioversion
- 5. used to induce hemostasis to reduce bleeding.
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Norepinephrine stimulates all the adrenergic receptors except _____________. It also is used to treat _______ and _______
- Beta 2
- treat shock and hypertension
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Pseudoephedrine (Sudafed--OTC)
- effects all adren recptors
- NON-catecholamines used for nasal decongestion
- Decongestion is a result of nasal vasoconstriction
- no longer OTC but available behind the counter, because METH
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Phenylephrine (Neo-synephrine, sudafed PE)
- Cold formulas are replacing psudoephedrine with phenylephrine
- phenylephrine is NOT better then placebo
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Ephedrine
- an isomer of pseudoephedrine
- in chinese herb mahuang (herb XTC) stimulant
- requires a prescription, but rarely prescribed
- supplements were available OTC, but several deatchs had them removed in 3/2004
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5 Examples of "UPPERS"
- 1. Amphetamine (Benzedrine, crank)
- 2. MDA (methylenedioxyamphetamine--love drug) Mello Drug of America
- 3. MDMA(methylenedioxyamphetamin--XTC)
- 4. Quat (Khat)
- 5. Bath salts
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Amphetamine and methylamphetamine
- synthetic epinephrine with similar structures
- originally for nasal congestion and appetite suppressants
- "ice" free base smokign
- "crystal" hydrochloride salt
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what is the condition called when meth heads hallucinate bugs crawling on themselves
formication
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MDA (methylenedioxyamphetamine--love drug, "mellow drug of america"
- similar structure to amphetamines
- produces self awareness while eliminating anxiety and inhibition. (awesomeness)
- RAVES
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MDMA (methylenedioxymethamphetamines--ecstasy XTC)
- similar to MDA
- changes serotonin receptors permanently ( nothing will ever feel soooo goood)
- 750,000 users in 2000
- briefly legal in 70's
- can increase heart rate, heat stroke, death
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Quat (Khat)
- shrub in Arabian peninsula (yemen) and East Africa
- leaves contain active adrenergic agonists
- chewed to stimulate
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Bath salts
- uppers
- synthetic derivatives of cathinone (not for human consumption)....or are they haha
- 6000 calls in 2011 to poison control
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3 main treatments for hyperactivity
- 1 methylphenidate (ritalin, concerta)
- 2. amphetamine (slow release adderall)
- 3. modafinil (provigil)
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Methylphenidate ( ritalin, concerta)
- used to treat ADHD
- if in short acting form must be give bid or tid can conflict with schedules
- slow relese forms are available
- schedule II widely abused
- reuptake of dopamine and norepinephrrine in the brain
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Dexmethylphenydate (focalin)
a pure enantiomeric (right hand glove) form of methylphenidate
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Amphetamine
- used for ADHD too
- legal, control II, gives a HIGH
- used for study aid in college (glad i got some haha just kidding)
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Modafinil (provigil)
- treats narcolepsy
- increases release monamines like epinephrine
- and norepinephrine
- off label use for ADHD "congnitive enhancement"
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name the 3 things Beta2 agonists cause
- 1. bronchodilation
- 2. uterine relaxation
- 3. glycogenolysis
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how are asthma meds usually administered?
MDI (metered dose inhaler) or DPI (dry powder inhaler)
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what are MDI (metered dose inhaler) filled with
- gas propellant under pressure. when canister is pushed down aerosol mist is sprayed in mouth.
- patient should breathe slowly and deep
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A spacer increases the amount that the drug reaches the lungs by how much
10% to 20% doubles
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Albuterol or salbutamol (ProAir, HFA)
- most common beta2 agonist
- primarily used to stop asthma attack
- onset 5-15 minutes after inhalation
- duration 3-6 hours
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why was chlorofluorcarbons (CFCs) discontinued
what replaced them
- ozone depletion
- replaced by hydrofluoroalkanes which are underpatent $$$$$
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Combivent is a combination of _____ and ____ which are used for
- ipratropium bromide and albuterol
- used for COPD
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