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Methacholine
- Direct acting cholinomimetic
- -selective for muscarinic receptor
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Bethanechol
- (Urecholine)
- Direct acting cholinomimetic
- -selective for muscarinic receptor
- -used for relief urinary retention; contracts smooth muscle of bladder
- -also used to stimulate gastric muscles
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Pilocarbine
- Direct acting cholinomimetic
- -selective for muscarinic receptor
- -contracts ciliary body to slacken zonular fibers and make the lens round for near vision; this treats glaucoma by opening pores and allowing outflow through canal of Schlemm
- -comes in gel or drops
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Edrophonium
- Indirect acting cholinomimetic
- -does not cross BBB
- -short acting peripheral effects (enzyme regenerates quickly)
- -Tensilon test cus fast acting
-
Tacrine
- Indirect acting cholinomimetic (anti acetylcholinesterase)
- -hydrophobic agent used to treat Alzheimer's
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Donezepil
- Indirect acting cholinomimetic (anti acetylcholinesterase)
- -hydrophobic agent used to treat Alzheimer's
-
Physostigmine
- Indirect acting cholinomimetic (anti acetylcholinesterase)
- -more slowly hydrolyzed by ACHE so has longer duration
- -treats ACHE overdose
-
Neostigmine
- Indirect acting cholinomimetic (anti acetylcholinesterase)
- -more slowly hydrolyzed by ACHE so has longer duration
- -treats bladder atony and post op pseduoobstruction
-
Rivastigmine
- Indirect acting cholinomimetic (anti acetylcholinesterase)
- -more slowly hydrolyzed by ACHE so has longer duration
- -used to treat Alzheimer's along w/ tacrine and donezepil
-
Carbaryl
Insecticide that inhibits ACHE
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Aldicarb
Insecticide that inhibits ACHE
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Malathion
Insecticide that inhibits ACHE
-
Parathion
Insecticide that inhibits ACHE
-
Diazinon
Insecticide that inhibits ACHE
-
Pyridostigmine
-treats myesthenia gravis
-
Pralidoxime
- -is an ACHE regeneator
- -treats ACHE inhibitor overdose
-
Atropine
- -Anti-muscarinic
- -treats ACHE inhibitor overdose
- -block M recepter
- -used for cycloplegia
- -treats bradycardia
-
Scopolamine
- Antimuscarinic
- -prevents motion sickness
-
Ipatropium
- Synthetic Quaternary (does not cross BBB) antimuscarinic
- -bronchodilator for COPD
-
Homatropine Methylbromide
Synthetic Quaternary (does not cross BBB) anti-muscarinic
-
Glycopyrrolate
- Synthetic quaternary (does not cross BBB) anti-muscarinic
- -inhibits GI motility
-
Cyclopentolate
- Synthetic Tertiary (accesses CNS) anti-muscarinic
- -used as mydriatic and cycloplegiac
-
Tropicamide
- Synthetic Tertiary (accesses CNS) anti-muscarinic
- -used as mydriatic and cycloplegiac
-
Benzotropine
- (Cogentin)
- Synthetic Tertiary (accesses CNS) anti-muscarinic
- -use to treat extra-pyramidal effects w/ antipsychotics and Parkinson's
-
Trihexyphenidyl
- (Artane)
- Synthetic Tertiary (accesses CNS) anti-muscarinic
- -use to treat extra-pyramidal effects w/ antipsychotics and Parkinson's
-
Dycylomine
- (Bentyl)
- Synthetic Tertiary (acceses CNS) anti-muscarinic
- -antispasmotic in GI tract (for IBS)
-
Hycosamine Sulfate
- (Levsin)
- Synthetic Tertiary (acceses CNS) anti-muscarinic
- -antispasmotic in GI tract (for IBS)
-
Oxybutynin
- (Ditropan)
- Synthetic Tertiary (acceses CNS) anti-muscarinic
- -used to treat urinary incontinence
-
Tolteridine
- (Detrol)
- Synthetic Tertiary (acceses CNS) anti-muscarinic
- -treats urinary incontinence
-
Epinephrine
- Adrenergic agonist
- -released from adrenal medulla after stimulated by nicotinic preganglionic fiber
- -increasesed systolic BP, HR, SV, CO, arrythmias
- -used for anyphylaxis, cardiac arrest, w/ local anesthesia
- -potent alpha and beta agnoism, more potent beta 2
-
Norepinephrine
- Adrenergic agonist
- -increased systolic and diastolic BP,
- -increased peripheral resistance (this stimulates baroreceptors, which stimulates vagal response, which slows the heart)
- -no vasodilation unlike epi
- -used to treat shock
-
Dopamine
- Adrenergic agonist
- -beta 1 agonism causes positive inotropic effects
- -low doses increases renal blood flow
- -high doses activates alpha 1 and causes vasoconstriction
- -used for cardiogenic and septic shock
-
Isoproterenol
- Non-selective Beta agonist
- -give IV or aerosolized
- -stimulates heart rate in severe bradycardia and heart blocks
-
Dobutamine
- Beta adrenergic agonist and works on alpha too
- -positive inotropic agent (B1)
- -increased BP and HR (though not as much as isoproterentol)
- -postitive inotropic agent in severe CHF
-
Metaproterenol
- Beta 2 selective agonist (used to treat asthma)
- -less beta 2 selective than albuterol
-
Terbutaline
- Beta 2 selective agonist (used to treat asthma)
- -rapid onset and lasts 3-6 hours
-
Albuterol
- Beta 2 selective agonist (used to treat asthma)
- -inhaled or PO
- -peak effect in 15 minutes that lasts 3-4 hours
-
Salmeterol
- Beta 2 selective agonist (used to treat asthma)
- -long lasting agent up to 12 hrs for prevention of brochospasm
-
Formoterol
- Beta 2 selective agonist (used to treat asthma)
- -long lasting agent lasts up to 12 hrs to treat bronchospasms
-
Ritodrine
- Beta 2 selective agonist
- -used to relax uterine muscle and delay premature labor
-
Beta 2 selective agonist adverse affects (3)
- 1. Tremor
- 2. Tachycardia
- 3. Hypokalemia (more common with IV therapy)
-
Cholinoimimetics excess adverse effect (7)
- 1. convulsions and coma
- 2. urination
- 3. miosis (constriction of pupil)
- 4. skeletal muscle contractions
- 5. bradycardia
- 6. increased secretions and bronchoconstriction
- 7. increased GI motility, secretions, and diarrhea
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Phenylephrine
- Alpha 1 adrenergic agonist
- -nasal decongestant
-
Clonidine
- Alpha 2 agonist
- -used to treat HTN
- -PO or transdermal patch
-
Guanfacine
- Alpha 2 adrenergic agonist
- -longer half life than clonidine
-
Guanabenz
- Alpha 2 agonist
- -similar to ganfacine with short half life
- -also sused for ADHD
-
Methyldopa
- Alpha 2 agonist
- -metabolized compound in brain that activates alpha 2 receptors
- -used in pregancy HTN
-
Adverse Events of Alpha 2 (3)
- 1. sedation
- 2. dry mouth
- 3. must taper to avoid withdrawel syndrome
-
Amphetamine
- -used for ADHD, obesity, narcolepsy
- -potent CNS stimulant on alpha and beta actions (indirect)
- -decreased fatigue, increased alertness, elevation of mood, HA, agitation, dysphoria
-
Methylphenidate
- -used for ADHD
- -"Ritalin" is a stimulant but not an amphetamine
-
Ephedrine
-indirect alpha and beta agonist use for appetite suppression
-
Pseudoephedrine
-oral agent for treatment of nasal congestion
-
Prazosin
- Alpha 1 antagonist used to treat HTN and BPH
- (must give initial dose at night to prevent first dose syncope)
-
Terazosin
- Alpha 1 antagonist-used to treat HTN and BPH
- (must give initial dose at night to prevent first dose syncope)
-
Doxazocin
- Alpha 1 antagonist-used to treat HTN and BPH
- (must give initial dose at night to prevent first dose syncope)
-
Tamsulosin
- Selective Alpha 1 antagonist
- -treats BPH with little affect on BP
-
Alpha 1 antoginst adverse affects (3)
- 1. First dose phenomenon
- 2. HA
- 3. dizziness
-
Phentolamine
- Alpha 1 and 2 blocker
- -many side affects, rarely used
-
Phenoxybenzamine
- irreversible blockade of Alpha 1 >> Alpha 2
- -long half life used for pheochromocytoma (rare tumor of adrenal gland)
-
Propanolol
- Beta non-selective agent
- -very lipophilic agent w/ short half life
-
Timolol
- Beta non-selective agent
- -used for glaucoma
-
Pindolol
- Beta non-selective agent
- +ISA (beta blocker but is also partial agonist; at high doses acts like epinephrine)
-
Nadolol
- Beta non-selective agent
- -long 10-20 hr half life
-
Beta Antagonist weird effects (3)
- 1. masks symptoms of hypoglycemia in Type 1 DM
- 2. may increase triglyceride and decrease HDL levels
- 3. may cause fatigue, nightmares, impotence, depression
-
Metoprolol and XL
- Beta 1 selective blocker
- -lipophilic so crosses BBB
- -use for post MI and HTN
- KNOW THIS ONE!!
-
Atenolol
- Beta 1 selective blocker
- -hydrophilic agent so no BBB penetration
-
Esmolol
- Beta 1 selective blocker
- -IV for quick onset and short duration
-
Carvedilol
- Alpha 1 and beta blockers
- -some peripheral vasodilation
-
Labetabol
- Alpha 1 and beta blocker
- (some peripheral vasodilation)
-
Mecamylamine
- Ganglionic blocker
- -secondary amine
-
Trimethaphan
- Ganglionic blocker
- -for malignant HTN
- -obsolete and not in USA
-
Effects of Beta 1 agonist (2)
- 1. increased HR, contractility, velocity, automaticity
- 2. increase renin release
-
Effects of Beta 2 agonist (6)
- 1. relax ciliary muscle for far vision
- 2. increase cardiac contractility
- 3. dilate arterioles and veins in skeletal muscle
- 4. relax respiratory smooth muscle, relax uterine smooth muscle
- 5. increase skeletal muscle contractility
- 6. glycogenolysis and gluconeogensis in the liver (increases glucose)
-
Alpha 1 agonist effects (5)
- 1. arteriole and venous constriction leader to increased PR
- 2. contraction of radial muscle in iris causes Mydriasis (eye dilation)
- 3. contraction of trigone and bladder sphncter (urinary retention)
- 4. ejaculation
- 5. contraction of piloerector muscles, sweaty palms and soles
-
Alpha 2 agonist effects (1)
1. inhibits NE release from brain and ysmpathetic nerves
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